WO2019115008A1 - Dérivés de dialkylaminoarylpipéridinyl-o-phénoxy et de o-benzyloxypropylamino présentant une activité multimodale contre la douleur - Google Patents
Dérivés de dialkylaminoarylpipéridinyl-o-phénoxy et de o-benzyloxypropylamino présentant une activité multimodale contre la douleur Download PDFInfo
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- 0 C*(C*(C)OC(*)*)c1ccccc1** Chemical compound C*(C*(C)OC(*)*)c1ccccc1** 0.000 description 9
- CCJLLAQIRSVRFT-UHFFFAOYSA-N CC(C)(C)OC(N(C)CCC(c1ccccc1)Oc1c(CC=O)cccc1)=O Chemical compound CC(C)(C)OC(N(C)CCC(c1ccccc1)Oc1c(CC=O)cccc1)=O CCJLLAQIRSVRFT-UHFFFAOYSA-N 0.000 description 1
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- A61P25/04—Centrally acting analgesics, e.g. opioids
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- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D211/58—Nitrogen atoms attached in position 4
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Definitions
- the present invention relates to compounds having dual pharmacological activity towards both the a 2 d subunit of the diurage-gated caicium channel, and the m-opioid receptor (MOR or mu-opioid receptor) and more particularly to dialkylaminoarylpiperidinyl-o-phenoxy and o-benzyloxypropylamino derivatives having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.
- MOR m-opioid receptor
- Voltage-gated calcium channels are required for many key functions in the body. Different subtypes of voltage-gated calcium channels have been described (Zamponi et al., Pharmacol Rev. 2015 67:821-70).
- the VGCC are assembled through interactions of different subunits, namely on (Ca v ai), b (Ca v ) a 2 d (Ca v a 2 6) and g (Ca v y).
- the on subunits are the key porous forming units of the channel complex, being responsible for the Ca 2+ conduction and generation of Ca 2+ influx.
- VGCC can be subdivided into low voltage-activated T-type (Ca v 3.1 , Ca v 3.2, and Ca v 3.3), and high voltage-activated L- (Ca v 1.1 through Ca v 1.4), N-(Ca v 2.2), P/Q-(Ca v 2.1 ), and R-(Ca v 2.3) types, depending on the channel forming Cava subunits.
- Current therapeutic agents include drugs targeting L-type Ca v 1.2 calcium channels, particularly 1 ,4-dihydropyridines, which are widely used in the treatment of hypertension.
- T-type (Ca v 3) channels are the target of ethosuximide, widely used in absence epilepsy.
- Ziconotide a peptide blocker of N-type (Ca v 2.2) calcium channels, has been approved as a treatment of intractable pain. (Perret and Luo, 2009, supra ⁇ Vink and Alewood, Br J Pharmacol. 2012 167:970-89.).
- the Ca v 1 and Ca v 2 subfamilies contain an auxiliary a 2 d subunit, which is the therapeutic target of the gabapentinoid drugs of value in certain epilepsies and chronic neuropathic pain.
- a 2 d subunit there are four known a 2 d subunits, each encoded by a unique gene and all possessing splice variants.
- Each a 2 d protein is encoded by a single messenger RNA and is post-translationally cleaved and then linked by disulfide bonds.
- Four genes encoding a 2 d subunits have now been cloned.
- a 2 d-1 was initially cloned from skeletal muscle and shows a fairly ubiquitous distribution.
- the a 2 d-2 and a 2 d-3 subunits were subsequently cloned from brain.
- the most recently identified subunit, a 2 d-4 is largely non-neuronal.
- the human a 2 d-4 protein sequence shares 30, 32 and 61 % identity with the human a 2 d-1 , a 2 d-2 and a 2 d-3 subunits, respectively.
- the gene structure of all a 2 d subunits is similar. All a 2 d subunits show several splice variants (Davies et al., Trends Pharmacol Sci. 2007 28:220-8.; Dolphin AC, Nat Rev Neurosci. 2012 13:542-55., Biochim Biophys Acta.
- the Ca v a25-1 subunit may play an important role in neuropathic pain development (Perret and Luo, 2009, supra Vink and Alewood, 2012, supra).
- Biochemical data have indicated a significant Ca v ct26-1 , but not Ca v oi28-2, subunit upregulation in the spinal dorsal horn, and DRG (dorsal root ganglia) after nerve injury that correlates with neuropathic pain development.
- the Ca v a 2 5-1 subunit (and the Ca v a 2 6-2, but not Ca v a 2 6-3 and Ca v a 2 5-4, subunits) is the binding site for gabapentin which has anti-allodynic/ hyperalgesic properties in patients and animal models.
- injury-induced Ca v cx25-1 subunit upregulation may contribute to the initiation and maintenance of neuropathic pain by altering the properties and/or distribution of VGCC in the subpopulation of DRG neurons and their central terminals, therefore modulating excitability and/or synaptic neuroplasticity in the dorsal horn.
- Intrathecal antisense oligonucleotides against the Ca v( X25-1 subunit can block nerve injury-induced Ca v a 2 5-1 upregulation and prevent the onset of allodynia and reserve established allodynia.
- the a ⁇ d subunits of VGCC form the binding site for gabapentin and pregabalin, which are structural derivatives of the inhibitory neurotransmitter GABA although they do not bind to GABAA, GABAB, or benzodiazepine receptors, or alter GABA regulation in animal brain preparations.
- the binding of gabapentin and pregabalin to the Ca v oi28 subunit results in a reduction in the calcium-dependent release of multiple neurotransmitters, leading to efficacy and tolerability for neuropathic pain management.
- Gabapentinoids may also reduce excitability by inhibiting synaptogenesis (Perret and Luo, 2009, supra ; Vink and Alewood, 2012, supra, Zamponi et al., 2015, supra).
- MOR m-opioid receptor
- MOR agonists are not optimal for the treatment of chronic pain as indicated by the diminished effectiveness of morphine against chronic pain conditions. This is especially proven for the chronic pain conditions of neuropathic or inflammatory origin, in comparison to its high potency against acute pain.
- the finding that chronic pain can lead to MOR down-regulation may offer a molecular basis for the relative lack of efficacy of morphine in long-term treatment settings [Dickenson, A.H., Suzuki, R. Opioids in neuropathic pain: Clues from animal studies. Eur J Pain 9, 1 13-6 (2005)].
- Polypharmacology is a phenomenon in which a drug binds multiple rather than a single target with significant affinity.
- the effect of polypharmacology on therapy can be positive (effective therapy) and/or negative (side effects). Positive and/or negative effects can be caused by binding to the same or different subsets of targets; binding to some targets may have no effect.
- Multi-component drugs or multi-targeting drugs can overcome toxicity and other side effects associated with high doses of single drugs by countering biological compensation, allowing reduced dosage of each compound or accessing context-specific multitarget mechanisms. Because multitarget mechanisms require their targets to be available for coordinated action, one would expect synergies to occur in a narrower range of cellular phenotypes given differential expression of the drug targets than would the activities of single agents.
- An alternative strategy for multitarget therapy is to design a single compound with selective polypharmacology (multi-targeting drug). It has been shown that many approved drugs act on multiple targets. Dosing with a single compound may have advantages over a drug combination in terms of equitable pharmacokinetics and biodistribution. Indeed, troughs in drug exposure due to incompatible pharmacokinetics between components of a combination therapy may create a low-dose window of opportunity where a reduced selection pressure can lead to drug resistance. In terms of drug registration, approval of a single compound acting on multiple targets faces significantly lower regulatory barriers than approval of a combination of new drugs (Hopkins, 2008, supra).
- the present application relates to the advantages of having dual activity, for m- receptor and the a 2 d-1 subunit of voltage-gated calcium channels, in the same molecule to treat chronic pain.
- the present invention relates to compounds having a complementary dual mechanism of action (m-receptor agonist and blocker of the a 2 d subunit, in particular the a 2 d-1 subunit, of voltage-gated calcium channels) which implies a better profile of tolerability than the strong opioids (morphine, oxycodone, fentanyl etc) and/or better efficacy and tolerability than gabapentinoids (pregabalin and gabapentin).
- Pain is multimodal in nature, since in nearly all pain states several mediators, signaling pathways and molecular mechanisms are implicated. Consequently, monomodal therapies fail to provide complete pain relief.
- therapies are a common clinical practice and many efforts are directed to assess the best combination of available drugs in clinical studies (Mao, J., Gold, M.S., Backonja, M.; 2011 ; J. Pain; 12; 157-166).
- the present invention offers a solution by combining in a single compound binding to two different targets relevant for the treatment of pain. This was mainly achieved by providing the compounds according to the invention that bind both to the m-opioid receptor and to the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel.
- a family of structurally distinct dialkylaminoarylpiperidinyl-o-phenoxy and o-benzyloxypropylamino derivatives encompassed by formula (I), which have a dual pharmacological activity towards both the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel, and the m-opioid receptor was identified thus solving the above problem of identifying alternative or improved pain treatments by offering such dual compounds.
- the main object of the invention is directed to a compound having a dual activity binding to the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel and the m-opioid receptor for use in the treatment of pain.
- this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel and the m-opioid receptor it is a very preferred embodiment if the compound has a binding expressed as K, responding to the following scales:
- Ki(p) is preferably ⁇ 1000 nM, more preferably ⁇ 500 nM, even more preferably ⁇ 100 nM.
- K,(a 2 d-1 ) is preferably ⁇ 10000 nM, more preferably ⁇ 5000 nM, even more preferably
- the invention is directed in a main aspect to a compound of general Formula (I),
- Ri, R 2 , R 3 , R 3 ⁇ , R 4 , R 4' , X, Ui, Y 2 and n are as defined below in the detailed description.
- a further object of the invention refers to the processes for preparation of compounds of general formula (I).
- a still further object of the invention refers to the use of intermediate compounds for the preparation of a compound of general formula (I).
- a family of structurally distinct dialkylaminoarylpiperidinyl-o-phenoxy and o-benzyloxypropylamino derivatives encompassed by formula (I), which have a dual pharmacological activity towards both the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel, and the m-opioid receptor was identified, thus solving the above problem of identifying alternative or improved pain treatments by offering such dual compounds.
- the main object of the invention is directed to a compound having a dual activity binding to the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel and the m-opioid receptor, for use in the treatment of pain.
- this invention is aimed at providing a compound or a chemically related series of compounds which act as dual ligands of the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel and the m-opioid receptor, it is a very preferred embodiment if the compound has a binding expressed as K, responding to the following scales:
- Ki(p) is preferably ⁇ 1000 nM, more preferably ⁇ 500 nM, even more preferably ⁇ 100 nM.
- K ⁇ (a 2 d-1) is preferably ⁇ 10000 nM, more preferably ⁇ 5000 nM, even more preferably ⁇ 500 nM or even more preferably ⁇ 100 nM.
- the applicant has surprisingly found that the problem of providing a new effective and alternative for treating pain and pain related disorders can be solved by using a multimodal balanced analgesic approach combining two different synergistic activities in a single drug (i.e., dual ligands which are bifunctional and bind to m-opioid receptor and to a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel), thereby enhancing through the a 2 d blockade without increasing the undesirable side effects.
- This supports the therapeutic value of a dual agent, whereby the a 2 d binding component acts as an intrinsic adjuvant of the MOR binding component.
- a dual compound that possess binding to both the m-opioid receptor and to the 2 d subunit of the voltage-gated calcium channel shows a highly valuable therapeutic potential by achieving an outstanding analgesia (enhanced in respect to the potency of the opioid component alone) with a reduced side-effect profile (safety margin increased compared to that of the opioid component alone) versus existing opioid therapies.
- the dual compounds according to the present invention would in addition show one or more the following functionalities: blockade of the a 2 d subunit, in particular the a 2 d-1 subunit, of the voltage-gated calcium channel and m-opioid receptor agonism
- An antagonist blocks or dampens agonist-mediated responses.
- Known subfunctionalities are neutral antagonists or inverse agonists.
- An agonist increases the activity of the receptor above its basal level.
- Known subfunctionalities are full agonists, or partial agonists.
- the two mechanisms complement each other since MOR agonists are only marginally effective in the treatment of neuropathic pain, while the blockers of the a 2 d subunit, in particular the a 2 d-1 subunit, of voltage-gated calcium channels show outstanding effects in preclinical neuropathic pain models.
- the a 2 d component in particular the a 2 d-1 component, adds unique analgesic actions in opioid-resistant pain.
- the dual approach has clear advantages over MOR agonists in the treatment of chronic pain as lower and better tolerated doses would be needed based on the potentiation of analgesia but not of the adverse events of MOR agonists.
- a further advantage of using designed multiple ligands is a lower risk of drug-drug interactions compared to cocktails or multi-component drugs, thus involving simpler pharmacokinetics and less variability among patients. Additionally, this approach may improve patient compliance and broaden the therapeutic application in relation to monomechanistic drugs, by addressing more complex aetiologies. It is also seen as a way of improving the R&D output obtained using the“one drug-one target” approach, which has been questioned over the last years [Bornot A, Bauer U, Brown A, Firth M, Hellawell C, Engkvist O. Systematic Exploration of Dual-Acting Modulators from a Combined Medicinal Chemistry and Biology Perspective. J. Med. Chem, 56, 1 197-1210 (2013)].
- X is selected from a bond, -[C(R a R b )]p-, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ]pN(R z )C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )[CH 2 ]q-;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2- e alkenyl and substituted or unsubstituted C 2- e alkynyl
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2 .e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci- 6 alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- Yi is— C(RioRio )-; wherein R10 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2- e alkynyl; alternatively, R10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Y 2 is— C(Rio "Rio ) _ i wherein R10 " and R10- are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R10 ⁇ and Rio- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- R 5 are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R5 and Rs ⁇ and/or R 5 and Rs - taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- R6, R6', R6” and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2.6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 6 and R 6 - and/or Re- and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Re and Re ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
- Re is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2 -e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- Re- is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C 2 -e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; alternatively, Re and Rs ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl
- R 3 is selected from substituted or unsubstituted C 1 -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- R 3' is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 4 and R 4 ⁇ are independently selected from halogen, -R 4I , -OR 4I , -NO2, -NR 4i R 4 r, - NR 4i C(0)R r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 4i R 4r , -NR 4i C(0)NR 4 rR 4 r, -SR 41 , -S(0)R i , - S(0) 2 R 4I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4i R 4 r, -OCH 2 CH 2 OR I , -
- R 4i S(0) 2 NR 4r R 4 r and -C(CH 3 ) 2 OR I wherein R 4 I , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- These compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- q is 1 , 2, 3, 4 or 5.
- X is selected from a bond, -[C(R a R b )] P -, - [CH 2 ] p C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )C(0)[CH 2 ] q -, q is 0, 1 , 2, 3, 4 or 5; and if X is selected from -[CH 2 ] p C(0)N(R z )[CH 2 ] q - and -[CH 2 ] p N(R z )[CH 2 ] q -, q is 1 , 2, 3, 4 or 5.
- these compounds according to the invention are optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof.
- the compound according to the invention is a compound of general Formula (I)
- X is selected from a bond, -[C(R a Rb)] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH2] P C(0)N(R z )[CH 2 ]q-, - [CH 2 ] P N(R z )C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2 .e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci-e alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- Yi is— C(RioR-io')-; wherein Rio and Ri 0 are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2- e alkenyl and substituted or unsubstituted C 2- e alkynyl; alternatively, R 10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Y2 is -C(Rio"Rio ) i wherein R 10 ⁇ and Rio- are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2 -e alkynyl; alternatively, R 10” and RKT may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- R5, Rs ⁇ , Rs ” and R5- are independently selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 5 and Rs and/or R 5 and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs ⁇ Rs- and Rs -, if substituted, is substituted with one or more substituent/s selected from -OR51, halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R 51 , Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 .e alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- Re, Re ’ , Re- and R 6 - are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2- e alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, Re and R 6 ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Re and R 6 ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in R 6 , R 6’ R 6 - and Re-, if substituted, is substituted with one or more substituent/s selected from -ORei , halogen, - CN, haloalkyl, haloalkoxy and -NReiRer;
- NR6iS(0)2N wherein Rei , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R I , -OR 7I , -NO2, - NR 7i R 7r , -NR 7I C(0)R 7V , -NR 7i S(0) 2 R r, -S(0) 2 NR 7i R 7r ,
- R I , R r and R 7 r ⁇ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; Re is selected from substituted or unsubstituted Cve alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsub
- R 8 2, R 8 2 ⁇ and R 82" are independently selected from hydrogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 83 S(0)2NR 83' R 83" and -C(CH3)20R 83 are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2.6 alkynyl;
- R2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R 2 , if substituted, is substituted with one or more substituent/s selected from halogen, -R21 , -OR21 , -NO2, -NR21R21', -NR 2i C(0)R2r, -NR2iS(0)2R2i’, -S(0)2NR2iR2r, - NR 2i C(0)NR 2 rR2r, -SR21 , -S(0)R 2 I , -S(0) 2 R 2 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 21 , - C(0)NR 2i R 2 r, -OCH2CH2OR21, -NR2iS(0) 2 NR 2 rR 2 r and -C(CH 3 ) 2 OR2i; wherein R
- R 3I , R 3r and R 3 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2.6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R 3' is selected from hydrogen, substituted or unsubstituted C-i-b alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -e alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R 3' , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR32R32'; wherein R 32 and R 32' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R 4I , -OR 4I , -NO2, -NR 4i R r, - NR 4i C(0)R 4 , -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 41 R 4 r, -NR 41 C(0)NR 4 rR 4 r, -SR 4I , -S(0)R 41 , - S(0) 2 R 4I , -CN, haloalkyl, haloalkoxy, -C(0)OR 4I , -C(0)NR 4i R 4 , -OCH 2 CH 2 OR 4I , -
- R M , R ⁇ and R ⁇ - are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyc!y!;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention is a compound of general Formula (I)
- X is selected from a bond, -[C(R a R b )] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ]pN(R z )C(0)[CH 2 ] q - and -[CH 2 ] p N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2- 6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci- 6 alkyl; if X is selected from a bond, -[C(R a Rb)] P -, -[CH 2 ]pC(0)[CH2]q- and -
- Yi is -C(RioRio )-; wherein R 10 and Ri 0 are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Y2 is— C(Rio "Rio ) ! wherein Rio- and Rio- are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Rio- and Rio- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- R 5 and R 5 ⁇ and/or Rs ⁇ and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs Rs- and Rs ', if substituted, is substituted with one or more substituent/s selected from -OR51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R51, Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2- 6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl;
- Re, Re ⁇ , Re ⁇ and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2- e alkynyl; alternatively, Re and R 6 ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Re and Re ⁇ and/or Re- and Re ⁇ taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in R 6 , Re ⁇ Re- and Re ⁇ , if substituted, is substituted with one or more substituent/s selected from -ORei, halogen, - CN, haloalkyl, haloalkoxy and -NReiRer; wherein the cycloalkyl,
- R61, Rer and R 6 r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- e alkynyl;
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R 7I , -OR 7I , -NO2, - NR 7i R 7 , -NR 7i C(0)R 7 r, -NR 7i S(0) 2 R 7 r, -S(0) 2 NR 71 R 7r ,
- R I , R r and R 7 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2- e alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- NReiS(0)2NR 8 rRer and -C(CH3)20R8i wherein Rei, Rsr and Rer are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C2-6 alkynyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Cre alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein
- the alkyl, alkenyl or alkynyl defined in Re ⁇ if substituted, is substituted with one or more substituent/s selected from -ORs2, halogen, -CN, haloalkyl, haloalkoxy and -NR82R82'; the cyclolakyl defined in R 8 ⁇ , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from 0, halogen, -Rs 2 , -OR82, -NO2, -NR82R82’, -NR82C(0)R82’, -NR82S(0)2Re2', -S(0)2NRe2R82’, - NR8 2 C(0)NR82'R82” -SRe2 , -S(0)Rs2, _ S(0)2R82, - CN, haloalkyl, haloalkoxy, -C(0)0Re2, -C(0)NRe2R82 ⁇ , -
- R 8 3, Rs3 ⁇ and R 8 3" are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R2, if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, -NR21R21', -NR 2i C(0)R 2 r, -NR 2i S(0) 2 R2r, -S(0) 2 NR2iR 2 r, - NR 2i C(0)NR 2 rR2r, -SR21 , -S(0)R 21 , -S(0) 2 R 2i , -CN, haloalkyl, haloalkoxy, -C(0)0R2i, - C(0)NR 2i R 2 r, -OCH2CH2OR21, -NR 21 S(0) 2 NR 21 R21” and -C(CH 3 )20R 2I ; wherein R21, R ⁇
- R31 , R31 ⁇ and R31 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
- R 3' is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R 3' , if substituted, is substituted with one or more substituent/s selected from -OR32, halogen, -CN, haloalkyl, haloalkoxy and -NR32R32'; wherein R32 and R32' are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; R 4 and R 4' are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41', - NR 4i C(0)R 4 r, -
- R 14 , Ri 4 and Ru- are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C 2 -e alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (I )
- Ri, R 2 , R3, R3', R 4 , R 4 ⁇ , X and n are as defined in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (I )
- X is selected from a bond, -[C(R a Rb)] P -, -[CH2] P C(0)[CH2] q -, -[CH2] P C(0)N(R z )[CH2] q -, - [CH 2 ] P N(Rz)C(0)[CH 2 ] q - and -[CH 2 ] P N(Rz)[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci- 6 alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- R 5 , Rs ⁇ , Rs- and R 5 are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R5 and Rs ⁇ and/or Rs- and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- Re, Re ⁇ , Re- and R ⁇ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R6 and Re ⁇ and/or Re- and Re ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R6 and R6 ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
- Re is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2 -6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; alternatively, Re and Retaken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl
- R 3 is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- R 3' is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41 , - NR 4i C(0)R 4 r, -NR4iS(0) 2 R 4 r, -S(0) 2 NR 4i R4r, -NR4iC(0)NR 4 rR 4 r, -SR41 , -S(0)R 41 , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)OR 4 I , -C(0)NR 4 IR 4 I , -OCH2CH2OR41, - NR4iS(0) 2 NR4i'R4r and -C(CH 3 ) 2 OR 4 I; wherein R 41 , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsub
- the compound according to the invention of general Formula (I) is a compound of general Formula (I )
- X is selected from a bond, -[C(R a Rb)] P -, -[CH2] P C(0)[CH 2 ]q-, -[CH 2 ]pC(0)N(Rz)[CH 2 ] q -, - [CH 2 ]pN(R z )C(0)[CH 2 ]q- and -[CH 2 ] p N(R 2 )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R P is selected from hydrogen, halogen, substituted or unsubstituted C 6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2- e alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2 -e alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci-6 alkyl;
- P is 0, 1 , 2, 3, 4 or 5;
- q is 0, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- Rs, Rs ⁇ R5” and R5- are independently selected from hydrogen, halogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2 -6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Rs and Rs ⁇ and/or Rs- and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs ⁇ Rs- and Rs -, if substituted, is substituted with one or more substituent/s selected from -OR 51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R51, Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- Re, Re ⁇ , Re- and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 6 and Re' and/or Re- and Re taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Re and Re ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in R 6 , Re ⁇ Re- and R 6 -, if substituted, is substituted with one or more substituent/s selected from -ORei, halogen, - CN, haloalkyl, haloalkoxy and -NReiRer;
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R 7i , -OR 7I , -N0 2 , - NR 7i R 7r , -NR 7I C(0)R TT , -NR 7i S(0) 2 R r, -S(0) 2 NR 71 R 7r ,
- R 7i S(0) 2 NR 71 R 7 r and -C(CH 3 ) 2 OR 7I ; wherein R 7I , R 7 r and R 7 r are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2- e alkynyl; R 8 is selected from substituted or unsubstituted Ci- 8 alkyl, substituted or unsubstituted C 2-8 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein the alkyl, alkenyl or alkynyl defined in R 8 , if substituted, is substituted with one or more substituent/s selected from -OR 8 I , halogen, -CN, haloal
- R 8 I , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted Ci. 8 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
- R 82 , Re 2 ⁇ and Rs 2" are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- NR83C(0)NR83’R83 R83
- -SR83 , -S(0)Re3, -S(0) 2 R83, — CN, haloalkyl, haloalkoxy, -C(0)0R 83 , -C(0)NR 83 R83 ⁇ , -OCH 2 CH 2 OR8 3 ,
- R 83S(0)2NR83’R83 and -C(CH3)20R83; wherein R 83 , Re 3 ⁇ and R 83 - are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R 2 , if substituted, is substituted with one or more substituent/s selected from halogen, -R 21 , -OR 21 , -NO 2 , -NR 21 R21', wherein R21, R21' and R 2 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R31, R 31' and R 3 r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R 3 ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR 32 R 32 ⁇ ; wherein R 32 and R 32 ⁇ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted C 2- e alkenyl, and substituted or unsubstituted C 2- e alkynyl;
- R 4 and R 4' are independently selected from halogen, -R I , -OR 4 I , -NO2, -NR i R r, - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 4i R r , -NR 4i C(0)NR 4r R 4 r, -SR 4i , -S(0)R i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4i R 4 r, -OCH 2 CH 2 OR 4 I , - NR 41 S(0) 2 NR rR r and -C(CH 3 ) 2 OR I ; wherein R 4 I , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkeny
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l a )
- Ri, R 3 , R 3 , R 4 , R 4 ⁇ , Rg, Rg ⁇ , X, Ui, Y2 and n are as defined in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture Of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l a )
- X is selected from a bond, -[C(R a Rb)] P -, -[CH2]pC(0)[CH 2 ] q -, -[CH2]pC(0)N(R z )[CH2]q-, - [CH 2 ]pN(Rz)C(0)[CH 2 ] q - and -[CH 2 ]pN(Rz)[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2 -e alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl; R z is selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci-e alkyl; p is 0, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- Yi is— C(RI Q RIO )-; wherein R 10 and Ri 0 are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 10 and R 10’ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Y 2 is— C(Rio”Rio ) l wherein R 10 ⁇ and Rio ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, Rio- and Rio- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- R 5 are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R5 and Rs ⁇ and/or R 5 ⁇ and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- Re, Re ⁇ , Re ⁇ and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 6 and R 6' and/or Re- and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Re and R 6 and/or Re- and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
- Re is selected from substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; alternatively, Re and R 8 ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- R 3 is selected from substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- R 3' is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 4 and R 4 ⁇ are independently selected from halogen, -R 4 I , -OR 4 I , -N0 2 , -NR 4i R r, - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R r, -S(0) 2 NR 4 I R 4 V, -NR 4i C(0)NR 4r R 4r , -SR 4i , -S(0)R 4i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4i R 4 r, -OCH 2 CH20R 4 I , - NR 4i S(0) 2 NR 4 rR r and -C(CH 3 ) 2 OR 4 I ; wherein R I , R 4 r and R r are independently selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C
- R 9 and R 9 ⁇ are independently selected from hydrogen, halogen, -R 21 , -OR 21 , -NO2, - NR21 R21’, -NR 21 C(0)R21 ⁇ , -NR2I S(0)2R21', -S(0)2NR2iR2i', - NR2iC(0)NR 2 rR 2 r, -SR21 , -S(0)R 2I , -S(0) 2 R 2I , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r, - OCH 2 CH 2 OR 2I , -NR 2i S(0) 2 NR 2r R 2 r and -C(CH 3 ) 2 OR 21 ; wherein R 2I , R 2 r and R 2 r are independently selected from hydrogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C 2-6 alkenyl,
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l a )
- X is selected from a bond, -[C(R a R b )] P -, -[CH 2 ]pC(0)[CH2] q -, -[CH 2 ]pC(0)N(Rz)[CH2] q -, - [CH 2 ] p N(R z )C(0)[CH 2 ] q - and -[CH 2 ] p N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
- Rb is selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci.6 alkyl; p is 0, 1 , 2, 3, 4 or 5; q is O, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- Yi is— C(RioRio)-; wherein R10 and Ri 0 are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Y 2 is— C(Rio' io )-l wherein R 10” and R 10 - are independently selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2 - 6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, Ri ⁇ r and Rio- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- R 5 , Re ⁇ , R 5” and Rs- are independently selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 - 6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 5 and R 5 ⁇ and/or R 5” and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs ⁇ Rs- and Rs-, if substituted, is substituted with one or more substituent/s selected from -OR51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R 51 , Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 6 , R 6' , R 6" and R 6 - are independently selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 6 and R 6 ⁇ and/or R 6” and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and R 6 and/or Re- and R 6 - taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in R 6 , Re ⁇ Re- and Re-, if substituted, is substituted with one or more substituent/s selected from -OR 61 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRs
- Rer and Rer are independently selected from hydrogen, substituted or unsubstituted Cre alkyl, substituted or unsubstituted C2.6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R 7i , -OR 7I , -NO2, -
- R I , R r and R 7 r are independently selected from hydrogen, substituted or unsubstituted Cre alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -e alkynyl;
- R 8 I , Rer and Rsr are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Ci -8 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein
- the alkyl, alkenyl or alkynyl defined in Re ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 82 , halogen, -CN, haloalkyl, haloalkoxy and -NR 82 R 82" ; the cyclolakyl defined in Re ⁇ , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from 0, halogen, -R 82 , -OR 82 , -NO2, -NR 82 R 82’ , -NR 82 C(0)R 82' , -NR 82 S(0) 2 R 82' , -S(0) 2 NR 82 R 82' , - N R 82 C(0) N R 8 2'R 8 2” , -SR 82 , -S(0)R 82 , -S(0)2R 82 , - CN, haloalkyl,
- NRe3C(0)NRe3’R83 -SR 8 3 , -S(0)R 83 , -S(0)2R 83 , — CN, haloalkyl, haloalkoxy, -C(0)0R 83 , -C(0)NR 83 R 83' , -OCH 2 CH 2 OR 83 ,
- R 83 , R 8 3 ⁇ and R 8 3- are independently selected from hydrogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 3I , R 3 t and R 3r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R 3' is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R 3 ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR32R32'; wherein R 32 and R 32' are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R 4 I , -OR 4 I , -NO 2 , -NR 4i R 4 r, - NR 4i C(0)R 4r , -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 4i R 4 r, -NR 4i C(0)NR 4r R 4r , -SR 4i , -S(0)R 4i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR i R 4r , -OCH 2 CH 2 OR I , - NR 4i S(0) 2 NR 4 R 4r and -C(CH 3 ) 2 OR I ; wherein R 4 I , R r and R r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alken
- R 9 and Rg- are independently selected from hydrogen, halogen, -R 2 I , -OR21 , -NO2, - NR21 R21’, -NR 2i C(0)R 2 r, -NR2iS(0)2R2r, -S(0)2NR2iR2r, - NR2iC(0)NR2i R2i”, -SR21 , -S(0)R 2I , -S(0) 2 R 2I , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r OCH2CH2OR21, -NR2iS(0) 2 NR 2 rR 2 r and -C(CH 3 ) 2 OR2i; wherein R 21 , R 21 ⁇ and R 21 ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or
- R14, Ri b and R - are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l a ’)
- Ri, R 3 , R 3 , R 4 , R 4 ⁇ , R 9 , R 9' , X and n are as defined in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l a ’)
- X is selected from a bond, -[C(R a R b )]p-, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ] p N(R z )C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2 -e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci-e alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5; n is 0 or 1 ;
- R 5 , Rs ⁇ , Rs ” and R 5 are independently selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R5 and Rs ⁇ and/or Rs- and Rs- ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; Re, Re ⁇ , Re- and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2.6 alkynyl; alternatively, Re and R 6 ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and Re ⁇ and
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
- R 8 is selected from substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C 2- s alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C 2 -e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; alternatively, Re and Re ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- R3 is selected from substituted or unsubstituted C-i-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- R3' is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R I , -OR 4 I, -NO 2 , -NR 4i R r , - NR 4i C(0)R 4 r, -NR i S(0) 2 R 4 r, -S(0) 2 NR 4i R r , -NR 4i C(0)NR 4r R 4 r, -SR 4 I , -S(0)R 4i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4 I R I , -OCH2CH 2 OR 4 I , - NR 4i S(0) 2 NR 4 rR 4 r and -C(CH 3 ) 2 0R 4 I ; wherein R I , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstitute
- the compound according to the invention of general Formula (I) is a compound of general Formula (l a ’)
- X is selected from a bond, -[C(R a Rb)] P -, -[CH 2 ] P C(0)[CH2]q-, -[CH2]pC(0)N(Rz)[CH 2 ]q-, - [CH 2 ]pN(Rz)C(0)[CH 2 ] q - and -[CH2]pN(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2 .s alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2- e alkenyl, substituted or unsubstituted C 2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci-e alkyl; p is 0, 1 , 2, 3, 4 or 5; q is O, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- Ri is wherein m is 0, 1 or 2; r is 0, 1 or 2; t is 0, 1 , 2, 3, 4 or 5;
- R5 and Rs ⁇ and/or R 5 - and Rs - taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs ⁇ Rs- and Rs-, if substituted, is substituted with one or more substituent/s selected from -OR 51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R 51 , Rsr and R 51 are independently selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- Re, Re ⁇ , Re- and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R6 and R6 ⁇ and/or R6- and R6- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Re and R 6 ⁇ and/or Re- and Re - taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in R 6 , Re ⁇
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R71, -OR71, -NO2, - NR71R71 ⁇ , -NR 7i C(0)R 7 r, -NR 7i S(0) 2 R7r, -S(0) 2 NR 7i R7r,
- R 71 , R 71 ⁇ and R 71 ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 8I , Rsr and R 8 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Ci -8 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- the alkyl, alkenyl or alkynyl defined in Re ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 82 , halogen, -CN, haloalkyl, haloalkoxy and -NR 8 2R 8 2'; the cyclolakyl defined in Re ⁇ , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from 0, halogen, -R 8 2, -OR 82I -NO2, -NR 8 2R 8 2', -NR 82 C(0)R 82' , -NR 82 S(0) 2 R 82' , -S(0) 2 NR 82 R 82 ⁇ , - N R 82 C(0) N R 8 2'R 8 2 ” , -SR 82 , -S(0)R 82 , -S(0)2R 82 , — CN, haloalkyl, haloalk
- R 83 S(0)2NR 83 , R 83" and -C(CH3)20R 83 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 31 , R 31’ and R 3 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R 3' is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R 3' , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR32R32'; wherein R 32 and R 37 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2.6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R 4 I, -OR 4I , -NO2, -NR 4i R 4 r, - NR 4i C(0)R r, -NR 41 S(0) 2 R 4 r, -S(0) 2 NR 4i R 4r , -NR 41 C(0)NR 4r R 4 r, -SR I , -S(0)R 4i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)OR 4 I , -C(0)NR i R r, -OCH 2 CH 2 OR I , - NR 4i S(0) 2 NR 4 rR 4i - and -C(CH 3 ) 2 OR I ; wherein R 4 I, R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2- e alkenyl
- Rg and Rg ⁇ are independently selected from hydrogen, halogen, -R 2I , -OR 2I , -N0 2 , - NR 2i R 2 r, -NR 2i C(0)R 2 r, -NR 2i S(0) 2 R 2 r, -S(0) 2 NR 2i R 2 r, - NR 2i C(0)NR 2 rR 2 -r, -SR 2I , -S(0)R 2I , -S(0) 2 R 2I , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r, - OCH 2 CH 2 OR 2I , -NR 2I S(0) 2 NR 2I’ R 2I " and -C(CH3) 2 OR 2I ; wherein R 2I , R 2 r and R 2 r are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or
- R I4 , R and R I4 - are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C2-6 alkenyl, unsubstituted C2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l b )
- Ri, R 3 , R 3 ⁇ , R 4 , R 4 , Rg, Rg ⁇ , X, Yi, Y2 and n are as defined below in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l b )
- X is selected from a bond, -[C(R a Rb)] P -, -[CH2] P C(0)[CH 2 ]q-, -[CH2] P C(0)N(R z )[CH 2 ]q-, - [CH 2 ] P N(Rz)C(0)[CH 2 ] q - and -[CH 2 ] P N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2.6 alkenyl and substituted or unsubstituted C 2 -e alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2.6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R a and Ru, taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2 -e alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -
- n O oM ;
- Yi is— C(RioRio)-; wherein R1 0 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2- 6 alkenyl and substituted or unsubstituted C2.6 alkynyl; alternatively, R10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Y2 is— C(Rio"Rio”)-; wherein Rio- and Rio- are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Rio ⁇ and R10- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- R5, Rs ⁇ , Rs" and Rs are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 5 and Rs ⁇ and/or R 5” and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- R 6 , R 6' , Re- and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2 -e alkynyl; alternatively, Re and Re ⁇ and/or Re ⁇ and Re ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and Re ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
- Re is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; alternatively, Re and Re ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- R 3 is selected from substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- R 3 is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R 4I , -OR 4I , -NO2, -NR 4i R 4 r, - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 4i R 4 r, -NR 41 C(0)NR 4i R 4r , -SR 4I , -S(0)R 41 , - S(0) 2 R 4I , -CN, haloalkyl, haloalkoxy, -C(0)OR 4I , -C(0)NR 4i R 4r , -OCH 2 CH 2 OR 4I , - NR 4i S(0) 2 NR 4 rR4r ⁇ and -C(CH3)20R 4i ; wherein R I , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkeny
- R9 and Rg- are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21’, -NR 2i C(0)R 2 r, -NR2iS(0)2R2i ⁇ -S(0)2NR2iR2r, - NR2iC(0)NR2rR2i”, -SR21 , -S(0)R 2I , -S(0) 2 R 2I , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2r , - OCH 2 CH 2 OR 2I , -NR 2i S(0) 2 NR 2 rR 2i” and -C(CH3) 2 OR 2I ; wherein R 2I , R 2 r and R 2 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substitute
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l b )
- X is selected from a bond, -[C(R a Rb)] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ]pN(R z )C(0)[CH 2 ] q - and -[CH 2 ] p N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted C-ve alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C ⁇ -e alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci- 6 alkyl; p is O, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- Yi is— C(R-ioRio')-; wherein Rio and Rio are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2.6 alkenyl and substituted or unsubstituted C 2- e alkynyl; alternatively, Rio and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Y 2 is— C(Rio 'Rio’ " )-; wherein Rio- and Rio- are independently selected from hydrogen, substituted or unsubstituted Ci. 6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Rio- and RKT may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Ri is wherein m is 0, 1 or 2; r is 0, 1 or 2; t is 0, 1 , 2, 3, 4 or 5;
- Rs, Rs', Rs- and Rs- are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Rs and Rs ⁇ and/or Rs- and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R5, Rs ⁇ Rs- and Rs-, if substituted, is substituted with one or more substituent/s selected from -OR51, halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R51, Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2.6 alkynyl;
- R 6 , Re ⁇ , R 6” and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 6 and R 6 ⁇ and/or R 6” and R 6 - ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and R 6 ⁇ and/or R 6 - and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in R 6 , R 6 ⁇ Re- and Re ⁇ , if substituted, is substituted with one or more substituent/s selected from -ORei, halogen, - CN, haloalkyl, haloalkoxy and -NRsi
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R 7I , -OR 7I , -NO2, - R 7r , haloalkyl, haloalkoxy, -C(0)0R i , -C(0)NR 7i R 7r , -OCH 2 CH 2 OR 7I ,
- Re ⁇ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein
- R 83 , R 83 ⁇ and R 83 - are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 31 , R 31' and R 31" are independently selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R 3' is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; wherein the alkyl, alkenyl or alkynyl defined in R 3 , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR32R32'; wherein R 32 and R 32' are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R 4 I , -OR 4 I, -N0 2 , -NR 4i R r, - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 4i R 4r , -NR 4i C(0)NR 4r R 4r , -SR 4 I , -S(0)R 4i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)OR 4 I , -C(0)NR 4i R 4 r, -OCH 2 CH 2 OR 4 I , - NR 4i S(0) 2 NR 4r R 4r and -C(CH 3 ) 2 OR 41 ; wherein R 4I , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2
- R14, Ri b and Ru- are independently selected from hydrogen, unsubstituted C1-6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C 2 -e alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl;
- the compound according to the invention of general Formula (I) is a compound of general Formula (l b ’)
- Ri, R 3 , R 3' , R 4 , R 4 ⁇ , R 9 , R 9' , X and n are as defined below in the detailed description, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l b ’)
- X is selected from a bond, -[C(R a R b )] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ] p N(Rz)C(0)[CH 2 ] q - and -[CH 2 ] p N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2- e alkenyl and substituted or unsubstituted C 2 .e alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2.6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci- 6 alkyl; p is 0, 1 , 2, 3, 4 or 5; q is 0, 1 , 2, 3, 4 or 5; n is 0 or 1 ;
- R 5 , Rs ⁇ , Re ⁇ ' and Rs- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R5 and Rs- and/or Rs- and Rs ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- Re, Re ⁇ , Re- and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Re and Re ⁇ and/or R 6 - and R 6 ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and R6 ⁇ and/or R 6 and Re - taken together with the carbon atom to which they are attached may form a carbonyl group;
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
- Re is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-0 alkenyl, substituted or unsubstituted C 2 -s alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 -6 alkenyl, substituted or unsubstituted C 2- 6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; alternatively, R 8 and Re ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted a Iky I cycloalky I;
- R 3' is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 4 and R 4' are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41', - NR 4i C(0)R 4i' , -NR 4i S(0) 2 R4r, -S(0) 2 NR 4i R4r, -NR 4i C(0)NR 4 rR4r, -SR41 , -S(0)R 4i , - S(0) 2 R 4i , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4i R4i ⁇ , -OCH2CH2OR41, - NR4iS(0) 2 NR 4 rR4r and -C(CH 3 ) 2 OR 4 I ; wherein R 41 , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound of general Formula (l b ’)
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R z is selected from hydrogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C 2- e alkenyl, substituted or unsubstituted C 2 -e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci-e alkyl; p is 0, 1 , 2, 3, 4 or 5; q is O, 1 , 2, 3, 4 or 5;
- n 0 or 1 ;
- R 5 are independently selected from hydrogen, halogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 5 and Rs ⁇ and/or Rs- and R 5 - taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs ⁇ Rs- and Rs ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R 51 , Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- Re, Re ⁇ , Re ⁇ and R 6 - are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 6 and R 6 ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and R 6 ⁇ and/or R 6 ⁇ and Re- taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in Re
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R71, -OR71, -NO2, - NR71R71', -NR 7i C(0)R 7 r, -NR7iS(0) 2 R 7 r, -S(0) 2 NR 7i R7r,
- R71, R71’ and R71 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- Rei , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted Cre alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- Re ⁇ is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C 2-8 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;
- the alkyl, alkenyl or alkynyl defined in Re ⁇ , if substituted, is substituted with one or more substituent/s selected from -ORs2, halogen, -CN, haloalkyl, haloalkoxy and -NR 82 Re2 ; the cyclolakyl defined in Re ⁇ , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from 0, halogen, -Rs 2 , -ORe2, -NO2, -NR82R82', -NR82C(0)R82’, -NR82S(0)2R82', -S(0)2NR82R82', - NR 8 2C(0)NR82'R82 ", -SRS2 , -S(0)R 82 , -S(0) 2 R 82 , -CN, haloalkyl, haloalkoxy, -C(0)0Re2, -C(0)NR 82 R82 ⁇ ,
- R 82 , Rs 2 ⁇ and Re 2 ⁇ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- NR 83 C(0)NR 83 R83 -SRes , -S(0)R 83 , -S(0) 2 R 83 , -CN, haloalkyl, haloalkoxy, -C(0)0R 83 , -C(0)NR 83 R83 ⁇ , -OCH2CH2OR83,
- NR83S(0)2NR83'R83 ' and -C(CH3)20R83 wherein Re 3 , Rs 3’ and Re 3 ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 31 , R 31' and R 31" are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R 3' is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R 3' , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR 3 2R32 ⁇ ; wherein R 32 and R 32 ⁇ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R4 and R 4' are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41', - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 4i R4i , -NR4iC(0)NR 4 vR 4 r, -SR41 , -S(0)R 4i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4 I R 4 I , -OCH 2 CH 2 OR 4 I , - NR 4i S(0) 2 NR 4 rR4r and -C(CH 3 ) 2 OR 4 I ; wherein R41, R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 .e alkeny
- R 9 and Rg ⁇ are independently selected from hydrogen, halogen, -R 2I , -OR 2I , -N0 2 , - NR 2i R 2 r, -NR 2i C(0)R 2 r, -NR 2i S(0) 2 R 2 r, -S(0) 2 NR 2i R 2 r, - NR 2i C(0)NR 2 rR 2 r, -SR 2I , -S(0)R 2I , -S(0) 2 R 2I , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r, - OCH 2 CH 2 OR 2I , -NR 2i S(0) 2 NR 2i' R 2i” and -C(CH 3 ) 2 OR 2I ; wherein R 2I , R 2 r and R 2 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or
- R , RTM ⁇ and Ri are independently selected from hydrogen, unsubstituted
- Ci- 6 alkyl unsubstituted C2-6 alkenyl, unsubstituted C2-6 a!kyny!, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- n means the number of times that -CH 2 - is repeated. The same would apply, when applicable, to general Markush Formulae (I), (I’), (l a ), (l a’ ), (l b ) and (l b ), and to all intermediates of synthesis.
- the expression“the heterocyclyl in Rs-Re" means the heterocyclyl resulting when R 8 and Re form, together with the nitrogen to which they are attached, a heterocyclyl. This heterocyclyl can then be substituted or not.
- This definition is also generally applicable and can be also applied as a definition of any Other cycle (preferably cycloalkyl or heterocycl) formed from two different functional groups like e.g. “the cycle in Ri-Ri“ means the cycle resulting when R, and R, ⁇ form a cycle together with the atom(s) to which they are attached. This cycle can then be substituted or not.
- R6a, R6 b are or could be different from R6 and R6 ⁇ or not.
- R 6c and R 6d are or could be different from R 6 - and Re - or not.
- m’ being 0 or 1 and r’ being 0 or 1 naturally resulting from m being o, 1 or 2 or r being 0, 1 or 2.
- alkyl is understood as meaning saturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses e.g. -CH3 and -CH2-CH3.
- Ci-2-alkyl represents C1- or C2-alkyl
- Ci-3-alkyl represents C1-, C2- or C3-alkyl
- Ci-4-alkyl represents C1 -, C2-, C3- or C4-alkyl
- Ci-s-alkyl represents C1-, C2-, C3-, C4-, or C5-alkyl
- Ci-e-alkyl represents C1-, C2-, C3-, C4-, C5- or C6-alkyl
- Ci-7-alkyl represents C1-, C2-, C3-, C4- , C5-, C6- or C7-alkyl
- Ci-s-alkyl represents C1 -, C2-, C3-, C3-,
- the alkyl radicals are preferably methyl, ethyl, propyl, methylethyl, butyl, 1-methylpropyl, 2-methylpropyl, 1 ,1-dimethylethyl, pentyl, 1 ,1-dimethylpropyl, 1 ,2-dimethylpropyl, 2,2-dimethylpropyl, hexyl, 1- methylpentyl, if substituted also CHF 2 , CF 3 or CH 2 OH etc.
- alkyl is understood in the context of this invention as Ci -8 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, heptyl, or octyl; preferably is Ci -8 alkyl like methyl, ethyl, propyl, butyl, pentyl, or hexyl; more preferably is Ci- 4 alkyl like methyl, ethyl, propyl or butyl.
- Alkenyl is understood as meaning unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses groups like e.g. -CF CH-CH 3 .
- the alkenyl radicals are preferably vinyl (ethenyl), allyl (2-propenyl).
- alkenyl is C 2 -io-alkenyl or C 2-8 -alkenyl like ethylene, propylene, butylene, pentylene, hexylene, heptylene or octylene; or is C2-6- alkenyl like ethylene, propylene, butylene, pentylene, or hexylene; or is C 2-4 -alkenyl, like ethylene, propylene, or butylenes.
- Alkynyl is understood as meaning unsaturated, linear or branched hydrocarbons, which may be unsubstituted or substituted once or several times. It encompasses groups like e.g. -CfC-CF (1-propinyl).
- alkynyl in the context of this invention is C2- 10 - alkynyl or C 2-8 -alkynyl like ethyne, propyne, butyene, pentyne, hexyne, heptyne, or octyne; or is C 2-6 -alkynyl like ethyne, propyne, butyene, pentyne, or hexyne; or is C2-4- alkynyl like ethyne, propyne, butyene, pentyne, or hexyne.
- alkyl also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl
- substituted in the context of this invention is understood as meaning replacement of at least one hydrogen radical on a carbon atom by halogen (F, Cl, Br, I), -NRkRk ⁇ , -SRk, -S(0)Rk, -S(0)2Rk, -ORk, - C(0)R k , -C(0)OR k , -CN, -C(0)NR k R k ⁇ haloalkyl, haloalkoxy, being R k represented by R13, R31, 32, R51, Rei, Rei or RS2 (being Rw represented by R13 ⁇ , R31 ⁇ , R32', Rsr, Rer, Rer or R 82'; being R k represented by R13 ”, R31 ”, R32”, Rsr
- alkyl also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl
- alkenyl, alkynyl or O-alkyl substituted is understood in the context of this invention that any alkyl (also in alkylaryl, alkylheterocyclyl or alkylcycloalkyl), alkenyl, alkynyl or O-alkyl which is substituted with one or more of halogen (F, Cl, Br, I), -NR k R k ⁇ , -OR k , -CN, -SRk, haloalkyl, haloalkoxy, being Rk represented by R13, R31, R32, R51, Rei, Rei or RS2, (being R k ⁇ represented by RI 3 ⁇ , R31', R32', Rsr, Rer, Rsr or R 82 ⁇ ; being Rk” represented by R13 R31 ", R32", Rsr,
- More than one replacement on the same molecule and also on the same carbon atom is possible with the same or different substituents.
- This includes for example 3 hydrogens being replaced on the same C atom, as in the case of CF 3 , or at different places of the same molecule, as in the case of e.g. -CH(OH)-CH CH-CHCi2.
- haloalkyl is understood as meaning an alkyl being substituted once or several times by a halogen (selected from F, Cl, Br, I). It encompasses e.g. -CH 2 CI, -CH 2 F, -CHC , -CHF 2 , -CCI 3 , -CF3 and -CH2-CHCI2.
- haloalkyl is understood in the context of this invention as halogen- substituted Ci-4-alkyl representing halogen substituted C1-, C2-, C3- or C4-alkyl.
- the halogen-substituted alkyl radicals are thus preferably methyl, ethyl, propyl, and butyl.
- Preferred examples include -CH 2 CI, -CH 2 F, -CHCb, -CHF 2 , and -CF 3 .
- haloalkoxy is understood as meaning an -O-alkyl being substituted once or several times by a halogen (selected from F, Cl, Br, I). It encompasses e.g. -OCH2CI, -OCH2F, -OCHC , -OCHF2, -OCCI3, -OCF3 and - OCH2-CHCI2.
- haloalkyl is understood in the context of this invention as halogen-substituted -OCi. 4 -alkyl representing halogen substituted C1 -, C2-, C3- or C4- alkoxy.
- the halogen-substituted alkyl radicals are thus preferably O-methyl, O-ethyl, O-propyl, and O-butyl.
- Preferred examples include -OCH2CI, -OCH2F, -OCHCb, - OCHF2, and -OCF3.
- cycloalkyl is understood as meaning saturated and unsaturated (but not aromatic) cyclic hydrocarbons (without a heteroatom in the ring), which can be unsubstituted or once or several times substituted.
- C3-4- cycloalkyl represents C3- or C4-cycloalkyl
- C 3 -5-cycloalkyl represents C3-, C4- or C5- cycloalkyl
- C3-6-cycloalkyl represents C3-, C4-, C5- or C6-cycloalkyl
- C3-7-cycloalkyl represents C3-, C4-, C5-, C6- or C7-cycloalkyl
- C3-e-cycloalkyl represents C3-, C4-, C5- , C6-, C7- or C8-cycloalkyl
- C4-5-cycloalkyl represents C4- or C5-cycloalkyl
- C4-6- cycloalkyl represents C
- Examples are cyclopropyl, 2-methylcyclopropyl, cyclopropylmethyl, cyclobutyl, cyclopentyl, cyclopentylmethyl, cyclohexyl, cycloheptyl, cyclooctyl, and also adamantyl.
- cycloalkyl is C3-ecycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; or is C 3- 7cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; or is C 3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl, especially cyclopentyl or cyclohexyl.
- Aryl is understood as meaning 5 to 18 (preferably 6 to 14) membered mono or polycyclic ring systems with at least one aromatic ring but without heteroatoms even in only one of the rings.
- Examples are phenyl, naphthyl, fluoranthenyl, fluorenyl, tetralinyl, dihydroindene or indanyl, 9H-fluorenyl or anthracenyl radicals, which can be unsubstituted or once or several times substituted.
- aryl is understood in the context of this invention as phenyl, naphthyl or anthracenyl, preferably is phenyl.
- a heterocyclyl radical or group (also called heterocyclyl hereinafter) is understood asmeaning - especially - 5 to 18 membered mono or polycyclic heterocyclic ring systems, with at least one saturated or unsaturated ring which contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring.
- a heterocyclic group can also be substituted once or several times.
- An heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole, thiazole, benzothiazole, tetrahydropyran, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene,
- a heterocyclyl may contain between 3 and 12 atoms in the ring (preferably 4 to 10 atoms in the ring, or 5 to 8 atoms in the ring, or 5 to 6 atoms in the ring) in case of a heterocyclyl of one saturated or unsaturated ring.
- Such a heterocyclyl may also contain between 5 and 22 atoms in both rings together (preferably 6 to 16 atoms in both rings together, or 7 to 12 atoms in both rings together or 8 to 10 atoms in both rings together) in case of a heterocyclyl of two saturated or unsaturated rings.
- Such a heterocyclyl may also contain between 7 and 32 atoms in the 3 rings together (preferably 10 to 22 atoms in the three rings together, or 12 to 20 atoms in the three rings together or 10 to 18 atoms in the three rings together) in case of a heterocyclyl of three saturated or unsaturated rings.
- Examples include non-aromatic heterocyclyls such as tetrahydropyrane, oxazepane, morpholine, piperidine, pyrrolidine as well as heteroaryls such as furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, thiazole, benzothiazole, indole, benzotriazole, carbazole and quinazoline.
- non-aromatic heterocyclyls such as tetrahydropyrane, oxazepane, morpholine, piperidine, pyrrolidine as well as heteroaryls such as furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, thiazo
- heterocyclyls as understood herein include heteroaryls and non- aromatic heterocyclyls.
- heteroaryl (being equivalent to heteroaromatic radicals or aromatic heterocyclyls, or also to “heterocyclyl containing at least one aromatic ring containing at least one heteroatom”) is an aromatic 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more rings of which at least one aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a 5 to 18 membered mono or polycyclic aromatic heterocyclic ring system of one or two rings of which at least one aromatic ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from furan, benzofuran, thiophene, benzothiophene, pyrrole, pyridine, pyrimidine, pyrazine, quinoline, isoquinoline, phthalazine, benzothiazole, indole, benzotriazole, carbazole, qui
- the non-aromatic heterocyclyl is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more rings of which at least one ring - with this (or these) ring(s) then not being aromatic - contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or two rings of which one or both rings - with this one or two rings then not being aromatic - contain/s one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepam, pyrrolidine, piperidine, piperazine, tetrahydropyran, morpholine, indoline, oxopyrrolidine, benzodioxane, especially is benzodioxane, morpholine, tetrahydropyran, piperidine
- heterocyclyl is defined as a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring.
- it is a 5 to 18 membered mono or polycyclic heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring.
- heterocyclyls include oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, pyridine, pyrimidine, piperidine, piperazine, , benzofuran, benzimidazole, indazole, benzodiazole, thiazole, benzothiazole, tetrahydropyrane, morpholine, indoline, furan, triazole, isoxazole, pyrazole, thiophene, benzothiophene, pyrrole, pyrazine, pyrrolo[2,3b]pyridine, quinoline, isoquinoline, tetrahydroisoquinoline, phthalazine, benzo-1 ,2,5-thiadiazole, indole, benzotriazole, benzoxazole oxopyrrolidine, pyrimidine, benzodioxolane, benzodioxane, carb
- oxopyrrolidine is understood as meaning pyrrolidin-2- one.
- the ring system is defined first as an aromatic heterocyclyl (heteroaryl) if at least one aromatic ring contains a heteroatom. If no aromatic ring contains a heteroatom, then the ring system is defined as a non-aromatic heterocyclyl if at least one non-aromatic ring contains a heteroatom. If no non-aromatic ring contains a heteroatom, then the ring system is defined as an aryl if it contains at least one aryl cycle. If no aryl is present, then the ring system is defined as a cycloalkyl if at least one non-aromatic cyclic hydrocarbon is present.
- alkylaryl is understood as meaning an aryl group (see above) being connected to another atom through a Ci-e-alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times.
- alkylaryl is understood as meaning an aryl group (see above) being connected to another atom through 1 to 4 (-CH 2 -) groups.
- alkylaryl is benzyl (i.e. -Chfe-phenyl).
- alkylheterocyclyl is understood as meaning an heterocyclyl group being connected to another atom through a Ci- 6 -alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times.
- alkylheterocyclyl is understood as meaning an heterocyclyl group (see above) being connected to another atom through 1 to 4 (-CH2-) groups.
- alkylheterocyclyl is -Chfe-pyridine.
- alkylcycloalkyl is understood as meaning an cycloalkyl group being connected to another atom through a Ci- 6 -alkyl (see above) which may be branched or linear and is unsubstituted or substituted once or several times.
- alkylcycloalkyl is understood as meaning a cycloalkyl group (see above) being connected to another atom through 1 to 4 (-CH 2 -) groups.
- alkylcycloalkyl is -CH 2 -cyclopropyl.
- the aryl is a monocyclic aryl. More preferably the aryl is a 5, 6 or 7 membered monocyclic aryl. Even more preferably the aryl is a 5 or 6 membered monocyclic aryl.
- the heteroaryl is a monocyclic heteroaryl. More preferably the heteroaryl is a 5, 6 or 7 membered monocyclic heteroaryl. Even more preferably the heteroaryl is a 5 or 6 membered monocyclic heteroaryl.
- the non-aromatic heterocyclyl is a monocyclic non-aromatic heterocyclyl. More preferably the non-aromatic heterocyclyl is a 4, 5, 6 or 7 membered monocyclic non-aromatic heterocyclyl. Even more preferably the non-aromatic heterocyclyl is a 5 or 6 membered monocyclic non-aromatic heterocyclyl.
- the cycloalkyl is a monocyclic cycloalkyl. More preferably the cycloalkyl is a 3, 4, 5, 6, 7 or 8 membered monocyclic cycloalkyl. Even more preferably the cycloalkyl is a 3, 4, 5 or 6 membered monocyclic cycloalkyl.
- aryl including alkyl-aryl
- cycloalkyl including alkyl-cycloalkyl
- heterocyclyl including alkyl-heterocyclyl
- aryl including alkyl-aryl
- cycloalkyl including alkyl- cycloalkyl
- heterocyclyl including alkyl-heterocyclyl
- any aryl, cycloalkyl and heterocyclyl which is substituted is substituted (also in an alyklaryl, alkylcycloalkyl or alkylheterocyclyl) with one or more of halogen (F, Cl, Br, I), -R k ,-ORk, -CN , -NO2 , -NRkRk” ⁇ , NR k C(0)Rk’, - NRkS(0)2Rk ⁇ , -S(0)2NRkRk ⁇ , -NRkC(0)NRk Rk”, haloalkyl, haloalkoxy, -SRk , -S(0)Rk or S(0) 2 R k , or substituted or unsubstit
- cycloalkyl including alkyl-cycloalkyl
- heterocyclyl including alkylheterocyclyl
- non-aromatic heterocyclyl including non-aromatic alkyl- heterocyclyl
- a ring system is a system consisting of at least one ring of connected atoms but including also systems in which two or more rings of connected atoms are joined with “joined” meaning that the respective rings are sharing one (like a spiro structure), two or more atoms being a member or members of both joined rings.
- leaving group means a molecular fragment that departs with a pair of electrons in heterolytic bond cleavage.
- Leaving groups can be anions or neutral molecules. Common anionic leaving groups are halides such as CI-, Br- and I-, and sulfonate esters, such as tosylate (TsO-) or mesylate.
- salt is to be understood as meaning any form of the active compound used according to the invention in which it assumes an ionic form or is charged and is coupled with a counter-ion (a cation or anion) or is in solution.
- a counter-ion a cation or anion
- complexes of the active compound with other molecules and ions in particular complexes via ionic interactions.
- physiologically acceptable salt means in the context of this invention any salt that is physiologically tolerated (most of the time meaning not being toxic- especially not caused by the counter-ion) if used appropriately for a treatment especially if used on or applied to humans and/or mammals.
- physiologically acceptable salts can be formed with cations or bases and in the context of this invention is understood as meaning salts of at least one of the compounds used according to the invention - usually a (deprotonated) acid - as an anion with at least one, preferably inorganic, cation which is physiologically tolerated - especially if used on humans and/or mammals.
- the salts of the alkali metals and alkaline earth metals are particularly preferred, and also those with NH 4 , but in particular (mono)- or (di)sodium, (mono)- or (di)potassium, magnesium or calcium salts.
- Physiologically acceptable salts can also be formed with anions or acids and in the context of this invention is understood as meaning salts of at least one of the compounds used according to the invention as the cation with at least one anion which are physiologically tolerated - especially if used on humans and/or mammals.
- the salt formed with a physiologically tolerated acid that is to say salts of the particular active compound with inorganic or organic acids which are physiologically tolerated - especially if used on humans and/or mammals.
- physiologically tolerated salts of particular acids are salts of: hydrochloric acid, hydrobromic acid, sulfuric acid, methanesulfonic acid, formic acid, acetic acid, oxalic acid, succinic acid, malic acid, tartaric acid, mandelic acid, fumaric acid, lactic acid or citric acid.
- the compounds of the invention may be present in crystalline form or in the form of free compounds like a free base or acid.
- solvate any compound that is a solvate of a compound according to the invention like a compound according to general formula I defined above is understood to be also covered by the scope of the invention. Methods of solvation are generally known within the art. Suitable solvates are pharmaceutically acceptable solvates.
- the term“solvate” according to this invention is to be understood as meaning any form of the active compound according to the invention in which this compound has attached to it via non- covalent binding another molecule (most likely a polar solvent). Especially preferred examples include hydrates and alcoholates, like methanolates or ethanolates.
- prodrug is used in its broadest sense and encompasses those derivatives that are converted in vivo to the compounds of the invention. Such derivatives would readily occur to those skilled in the art, and include, depending on the functional groups present in the molecule and without limitation, the following derivatives of the present compounds: esters, amino acid esters, phosphate esters, metal salts sulfonate esters, carbamates, and amides. Examples of well known methods of producing a prodrug of a given acting compound are known to those skilled in the art and can be found e.g. in Krogsgaard-Larsen et al.“Textbook of Drug design and Discovery” Taylor & Francis (April 2002).
- the compounds of the invention are also meant to include compounds which differ only in the presence of one or more isotopically enriched atoms.
- compounds having the present structures except for the replacement of a hydrogen by a deuterium or tritium, or the replacement of a carbon by 13 C- or 14 C-enriched carbon or of a nitrogen by 15 N-enriched nitrogen are within the scope of this invention. This would especially also apply to the provisos described above so that any mentioning of hydrogen or any ⁇ ” in a formula would also cover deuterium or tritium.
- the compounds of formula (I) as well as their salts or solvates of the compounds are preferably in pharmaceutically acceptable or substantially pure form.
- pharmaceutically acceptable form is meant, inter alia, having a pharmaceutically acceptable level of purity excluding normal pharmaceutical additives such as diluents and carriers, and including no material considered toxic at normal dosage levels.
- Purity levels for the drug substance are preferably above 50%, more preferably above 70%, most preferably above 90%. In a preferred embodiment it is above 95% of the compound of formula (I), or of its salts. This applies also to its solvates or prodrugs.
- the compound according to the invention of general Formula (I) is a compound wherein
- X is selected from a bond, -[C(R a R b )] P -, -[CH2] p C(0)[CH 2 ]q-, -[CH2] P C(0)N(R z )[CH2] q -, - [CH 2 ] P N(Rz)C(0)[CH 2 ] q - and -[CH 2 ] P N(R z )[CH 2 ] q -;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- X is selected from a bond, -[C(R a R b )] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ] p N(R z )C(0)[CH 2 ] q - and -[CH 2 ] p N(R 2 )[CH 2 ] q -; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- -X-Ri is selected from -Ri, -[C(R a R b )]p-Ri, -[CH 2 ] p C(0)[CH 2 ]q-Ri, [CH 2 ] p C(0)N(Rz)[CH 2 ] q -Ri, -[CH 2 ] p N(R z )C(0)[CH 2 ] q -Ri and -[CH 2 ] p N(R z )[CH 2 ] q -Ri; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R a is selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2- e alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R b is selected from hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkyny!; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- the compound according to the invention of general Formula (I) is a compound wherein
- X is selected from a bond, -[CH 2 ] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ] p N(R z )C(0)[CH 2 ] q - and -[CH 2 ] p N(R z )[CH 2 ] q -; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R z is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci- 6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rz is selected from hydrogen, substituted or unsubstituted C alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci- 6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein p is 0, 1 , 2, 3, 4 or 5; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of genera! Formula (I) is a compound wherein q is O, 1 , 2, 3, 4 or 5; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein n is 0 or 1 ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Yi is— C(R-ioRio’)-; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Y 2 is— C(Rio' Rio ) ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 3 is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 3 is selected from substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 3 is selected from substituted or unsubstituted Ci-e alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 3 ⁇ is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R3' is selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 4 and R 4' are independently selected from halogen, -R 4 I , -OR 4 I , -NO2, -NR 4i R 4r , - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 41 R 4r , -NR 4i C(0)NR r R 4i ⁇ , -SR 4 I , -S(0)R 1 , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)OR 4 I , -C(0)NR 4i R 4r , -OCH 2 CH 2 OR 4 I , - NR 4i S(0) 2 NR 4 rR 4t' and -C(CH3) 2 OR 4 I ; wherein R 4 I , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 al
- the compound according to the invention of general Formula (I) is a compound wherein
- R 4 and R 4' are independently selected from halogen, -R I , -OR 4I , -N0 2 , -NR i R 4 r, - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R r, -S(0) 2 NR 4I R 4I , -NR 4i C(0)NR 4r R 4i , -SR 4I , -S(0)R i , - S(0) 2 R 4I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4i R r, -OCH 2 CH 2 OR I , - NR 4i S(0) 2 NR 4i' R 4i” and -C(CH3) 2 OR 4I ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers,
- R 5 are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2.6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 5 and R 5 ⁇ and/or R 5 - and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R, Rs ⁇ , Rs and Rs- are independently selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rs, Rs ⁇ , Rs- and Rs- are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, Rs and Rs ⁇ and/or Rs- and Rs - taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein R 5 , Rs ⁇ , Rs- and Rs - are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein R 5 , RS ⁇ , Rs- and Rs- are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- the compound according to the invention of general Formula (I) is a compound wherein
- Re, Re ⁇ , Re ⁇ and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 6 and R6 ⁇ and/or Re- and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and R 6 ⁇ and/or R 6 - and R 6 ⁇ taken together with the carbon atom to which they are attached may form a carbonyl group; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re, Re ⁇ , Re ⁇ and R 6 ⁇ are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re, Re ⁇ , Re- and Re- are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2 -e alkynyl; alternatively, R 6 and Re ⁇ and/or R 6 - and Re- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R6 and R6 ⁇ and/or R6- and R 6 taken together with the carbon atom to which they are attached may form a carbonyl group; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R6, Re ⁇ , R6” and R ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re, Re ⁇ , Re- and R 6 are independently selected from hydrogen and substituted or unsubstituted C alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- the compound according to the invention of general Formula (I) is a compound wherein
- R 6 and Re' taken together with the carbon atom to which they are attached form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- the compound according to the invention of general Formula (I) is a compound wherein
- the compound according to the invention of general Formula (I) is a compound wherein
- R 6 and R 6 "' taken together with the carbon atom to which they are attached form a carbonyl group; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- the compound according to the invention of general Formula (I) is a compound wherein
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rs is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalky! and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rs is selected from substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rs is substituted or unsubstituted Ci-s alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Ci-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalky! and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re ⁇ is selected from hydrogen and substituted or unsubstituted C1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re and Re ⁇ taken together with the nitrogen atom to which they are attached form a substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rg and Rg ⁇ are independently selected from hydrogen, halogen, -R21, -OR21, -N0 2 , - NR 2i R 2 r, -NR 2i C(0)R 2 r, -NR 2i S(0) 2 R 2 r, -S(0) 2 NR 2i R 2 r, - NR 2i C(0)NR 2 rR 2 r, -SR 2 I , -S(0)R 2 I , -S(0) 2 R 2 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r, - OCH 2 CH 2 OR 2 I , -NR 2i S(0) 2 NR 2i' R 2i” and -C(CH3) 2 OR 2 I ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereois
- the compound according to the invention of general Formula (I) is a compound wherein
- Rg and Rg ⁇ are independently selected from hydrogen, halogen and -CN; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 10 and Ri 0 are independently selected from hydrogen, substituted or unsubstituted Ci. e alkyl, substituted or unsubstituted C 2- 6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, R 10 and Rio may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 10 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci- e alkyl, substituted or unsubstituted C 2- 6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein R1 0 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci. 6 alkyl optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R1 0 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci. 6 alkyl optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 10 and Re form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rio ⁇ and Rio- are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2 - 6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rio- and R 10 - are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rio ⁇ and Rio- form with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 13 and R I3 ⁇ are independently selected from hydrogen, unsubstituted Ci- 6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 13 and Ri 3' are independently selected from hydrogen and unsubstituted C 1 -6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Ri4, Rn and R ⁇ - are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C 2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 14 , Ri 4’ and R H - are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 21 , R 21' and R 21" are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 21 , R 21 ⁇ and R 21 ⁇ are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 31 , R 31' and R 31" are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 31 , R 31' and R 3 r are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 32 and R 32' are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 32 and R 32' are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 41 , R 41' and R 4 r are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2 -6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 41 , R 41' and R 41” are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 51 , R 51' and R 51” are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R51 , R51' and R51” are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein Rei , R 61' and Rer are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- Rei , R 61' and Rer are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the
- the compound according to the invention of general Formula (I) is a compound wherein R 61 , R 6 V and Rer are independently selected from hydrogen and substituted or unsubstituted Cre alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- Rn, R 71 ⁇ and R 7 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2 -e alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 71 , R 71' and R 71” are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 71 is selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rr and Rsr are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2.6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rei , Rsr and R 8 r are independently selected from hydrogen and substituted or unsubstituted Ci- 6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein R S2 , R S2' and R 82 ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re 2 , Re 2' and R 82 - are independently selected from hydrogen and substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re 3 , Re 3' and Re 3 ⁇ are independently selected from hydrogen, substituted or unsubstituted Ci-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 83 , R 83' and Re 3 are independently selected from hydrogen and substituted or unsubstituted Ci-e alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Yi is— C(RioRio)-; wherein R10 and Rio are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Yi is— C(RioRio)-
- the compound according to the invention of general Formula (I) is a compound wherein
- Y 2 is— C(Rio"Rio )-; wherein Rio- and Rur are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, Rio- and Rur may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- Rio- and Rur are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkeny
- the compound according to the invention of general Formula (I) is a compound wherein Y 2 is -C(Rio"Rio")-; wherein Rio- and R KT are independently selected from hydrogen and substituted or unsubstituted Ci-e alkyl; alternatively, Rio- and Rio- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl or heterocyclyl in R 2 , if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, -NR21R21', -NR 2i C(0)R 2 r, -NR2iS(0)2R2r, -S(0)2NR2iR2r, - NR2iC(0)NR2rR2i", -SR21 , -S(0)R2i, -S(0)2R2i, -CN, haloalkyl, haloalkoxy, -C(0)OR 2I , - C(0)NR 2i R 2 r, -OCH2CH2OR21, -NR2iS(0)2NR2rR2i’’ and -C(CH3)20R2i; wherein R 21 , Riv and R 21
- R 3I , R 3r and R 3 r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2- e alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- R 3' is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2.6 alkynyl; wherein, the alkyl, alkenyl or alkynyl defined in R3 , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR32R32'; wherein R 32 and R 32 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably
- the compound according to the invention of general Formula (I) is a compound wherein
- R 5 , Rs ⁇ , Rs- and Rs- are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2 -e alkynyl; alternatively, R 5 and R 5 ⁇ and/or R 5 and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs ⁇ Rs- and Rs-, if substituted, is substituted with one or more substituent/s selected from -OR 51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R 5I , Rsr and R 5 r are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Rs, Rs , Rs- and Rs- are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; alternatively, Rs and Rs ⁇ and/or Rs and Rs ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl;
- alkyl, alkenyl or alkynyl defined in R 5 , Rs Rs- and Rs ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R 51 , Rsr and R 5 r are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein
- Re, Re ⁇ , Re ⁇ and Re ⁇ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2.6 alkynyl; alternatively, Re and Re ⁇ and/or Re ⁇ and Re ⁇ taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Re and Re ⁇ and/or R 6 ⁇ and R 6 ⁇ taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in Re, Re ⁇ Re ⁇ and Re-, if substituted, is substituted with one or more substituent/s selected from -OR 6 I , halogen, - CN, haloalkyl, haloalkoxy and -NReiRer; wherein the cycloalkyl,
- the compound according to the invention of general Formula (I) is a compound wherein
- R6, R6', R6” and Re- are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R 6 and R 6 ⁇ and/or R 6 - and R 6 - taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and R 6 ⁇ and/or R 6 - and Re - taken together with the carbon atom to which they are attached may form a carbonyl group; wherein the alkyl, alkenyl or alkynyl defined in R 6 , R 6 ⁇ R 6 - and R 6 , if substituted, is substituted with one or more substituent/s selected from -ORei, halogen, - CN, haloalkyl, haloalkoxy and -NReiR
- the compound according to the invention of general Formula (I) is a compound wherein
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R 7 I , -OR 7 I , -NO2, - -NR 7i S(0) 2 R 7 r, -S(0) 2 NR 7i R 7 r, -S(0)R 7i , -S(0) 2 R 7i , -CN, haloalkyl, haloalkoxy, -C(0)0R 7i , -C(0)NR 7i R 7r , -OCH 2 CH 2 OR 7 I , NR 7i S(0) 2 NR 7i ' R 7i” and -C(CH 3 ) 2 OR 7 I ; wherein R 7 I , R 7 r and R 7 r ⁇ are independently selected from hydrogen, substituted or unsubstitute
- the compound according to the invention of general Formula (I) is a compound wherein
- Rer and Rer are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- Rs' is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein
- the alkyl, alkenyl or alkynyl defined in R 8 ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 8 2, halogen, -CN, haloalkyl, haloalkoxy and -NR 82 R 8 2'; the cyclolakyl defined in R 8 ⁇ , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from 0, halogen, -R 8 2, -OR 8 2, -NO2, -NR 8 2R 8 2’, -NR 82 C(0)R 82' , -NR 82 S(0)2R82’, -S(0) 2 NR 82 R 82 ⁇ , - NR 82 C(0)NR82'R82”, -SR82 , -S(0)Rs2, -S(0)2R82, — CN, haloalkyl, haloalkoxy, -C(0)0R 82 ,
- the compound according to the invention of general Formula (I) is a compound wherein
- NR83C(0)NR83'R83 -SR83 , -S(0)Re3, -S(0) 2 R 83 , - CN, haloalkyl, haloalkoxy, -C(0)0R 83 , -C(0)NR 83 R83', -OCH2CH2OR83,
- the compound according to the invention of general Formula (I) is a compound wherein
- R g and Rg ⁇ are independently selected from hydrogen, halogen, -R 2I , -OR21, -NO2, - NR21 R21 , -NR 2i C(0)R 2 r, -NR2iS(0)2R2i', -S(0)2NR2iR2r, - NR2iC(0)NR2i R2i", -SR21 , -S(0)R 2 I , -S(0) 2 R 2 I , -CN, haloalkyl, haloalkoxy, -C(0)0R 21 , -C(0)NR2iR 2 r, - OCH2CH2OR21, -NR21 S(0)2NR2i’R2i” and -C(CH3)20R2i; wherein R21, R21' and R21” are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstitute
- the compound according to the invention of general Formula (I) is a compound wherein the aryl or heterocyclyl in R 2 , if substituted, is substituted with one or more substituent/s selected from halogen, -R21, -OR21, -NO2, -NR21R21 ⁇ , -NR2iC(0)R 2 r, -NR2iS(0)2R 2 r, - S(0) 2 NR 2i R 2 r, - NR 2i C(0)NR 2 rR 2 r, -SR21 , -S(0)R 2i , -S(0) 2 R2i, -CN, haloalkyl, haloalkoxy, -C(0)0R2i, -C(0)NR2iR2r, -OCH2CH2OR21, -NR2iS(0)2NR2rR2r and - C(CH 3 ) 2 OR 2I ; wherein R21, R 2 r and R21” are independently selected from
- R31 , R31' and R31 are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 3 ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR32, halogen, -CN, haloalkyl, haloalkoxy and -NR32R32'; wherein R32 and R32- are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 5 , Rs ⁇ Rs and Rs ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR51, halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr;
- R51 , Rsr and R 5 I ⁇ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2- e alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 6 , Re ⁇ Re ⁇ and Re ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR61, halogen, - CN, haloalkyl, haloalkoxy and -NReiRer;
- R 6 I , R 6 r and Rer are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of general Formula (I) is a compound wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R 71 , -OR 71 , -NO 2 , -
- R 71 , R 7 r and R 71 are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R 82 , R 8 2 ⁇ and R 8 2 ⁇ are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R 83 , R 8 3 and R 83 - are independently selected from hydrogen, substituted or unsubstituted Ci -8 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the aryl or heterocyclyl in R 2 , if substituted, is substituted with one or more substituent/s selected from halogen, -R21 , -OR 2I , -N0 2 , -NR 2i R 2r , -NR 2i C(0)R 2 r, -NR 2i S(0) 2 R 2r , - S(0) 2 NR 2i R 2 , - NR 2i C(0)NR 2 rR 2i” , -SR 2 I , -S(0)R 2i , -S(0) 2 R 2i , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r, -OCH 2 CH 2 OR 2I , -NR 2i S(0) 2 NR 2 rR 2i” and - C(CH 3 ) 2 OR 2
- the compound according to the according to the invention of general Formula (I) is a compound wherein the aryl or heterocyclyl in R 2 , if substituted, is substituted with one or more substituent/s selected from halogen and -CN; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 3 , if substituted, is substituted with one or more substituent/s selected from -OR31 , halogen, -CN, haloalkyl, haloalkoxy and -NR31 R31'; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R3, also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from -OR31 , halogen, -CN, haloalkyl, haloalkoxy and -NR31 R31'; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 3 , if substituted, is substituted with one or more substituent/s of halogen ⁇ ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 3 , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s of halogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein wherein the cycloalkyl in R 3 , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected -R 31 , -OR 31 , halogen, - CN, haloalkyl, haloalkoxy and -NR31R31 ⁇ ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 3 ⁇ , if substituted, is substituted with one or more substituent/s selected from -OR 32 , halogen, -CN, haloalkyl, haloalkoxy and -NR 32 R 32 ⁇ ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 5 , R 5 ⁇ Rs- and R5-, if substituted, is substituted with one or more substituent/s selected from -OR 51 , halogen, - CN, haloalkyl, haloalkoxy and -NRsiRsr; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl, as defined in R 5 -R 5' and/or Rs-Rs- , if substituted, is substituted with one or more substituent/s selected from selected from -R 51 , -OR 51 , halogen, -CN, haloalkyl, haloalkoxy and -NRsiRsr; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 6 , Re ⁇ Re- and Re-, if substituted, is substituted with one or more substituent/s selected from -OR61, halogen, -CN, haloalkyl, haloalkoxy and - R6iR6i ⁇ ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl, as defined in R 6 -R 6' and/or Re-Re ’ ⁇ , if substituted, is substituted with one or more substituent/s selected from halogen, -R 6 I , - ORei, -NReiRer, -CN, haloalkyl, haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s selected from halogen, -R71, -OR71, -NO2, - NR71R71 ⁇ , -NR 7i C(0)R 7i' , -NR 7i S(0) 2 R 7 r, -S(0) 2 NR 7i R7r,
- the compound according to the according to the invention of general Formula (I) is a compound wherein the aryl or heterocyclyl, as defined in R 7 , if substituted, is substituted with one or more substituent/s of halogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in Re, if substituted, is substituted with one or more substituent/s selected from -OR 8 I , halogen, -CN, haloalkyl, haloalkoxy and -NReiRer; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in R 8 , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from -OR 8 I , halogen, -CN, haloalkyl, haloalkoxy and -NRsiRsr; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding sait thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the cycloalkyl defined in R 8 , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from halogen, -R 8 I , - OR 8 I , -NRsiRsr, -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in Re ⁇ , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from - ORS 2 , halogen, -CN, haloalkyl, haloalkoxy and -NR 82 RB2'; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the alkyl, alkenyl or alkynyl defined in Re ⁇ , if substituted, is substituted with one or more substituent/s selected from -ORs 2 , halogen, -CN, haloalkyl, haloalkoxy and -NR 82 R82 ⁇ ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- NR82S(0)2NR82’R82 ⁇ ' and -C(CH 3 )20R 82 optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein the cyclolakyl defined in Re ⁇ , also in alkylcycloalkyl, if substituted, is substituted with one or more substituent/s selected from halogen, -Rs 2 , - OR S2 , -NR 82 R 82' , -CN, haloalkyl and haloalkoxy; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- NR83C(0)NR83’R83 m , -SR83 , -S(0)Re3, -S(0) 2 R 83 , - CN, haloalkyl, haloalkoxy, -C(0)ORe3, -C(0)NR 83 R83 ⁇ , -OCH2CH2OR83,
- NR83S(0)2NR83’R83” 3nd -C(CH3)20Re3 optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the invention of genera! Formula (I) is a compound wherein any cycloalkyl, also in alkylcycloalkyl, if substituted and the substitution has not been defined otherwise, it is substituted with one or more substituent/s selected from -R 14 , - OR 14 , halogen, -CN, haloalkyl, haloalkoxy and -NR 14 R 14' optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in an mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- X is a bond, -[C(R a R b )] P -, -[C(R a R b )] p C(0)[C(R c Rd)]q-, -[C(R a R b )]pC(0)N(R z )[C(R c Rd)] q - , -[C(R a R b )]pN(R z )C(0)[C(R c Rd)]q- or -[C(R a R b )] p N(R z )[C(R c Rd)] q -;
- R z is selected from hydrogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C 2.6 alkenyl, substituted or unsubstituted C 2.6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci- 6 alkyl;
- R a is selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R b is selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; alternatively, R a and R b , taken together with the carbon atom to which they are attached, may form a substituted or unsubstituted cycloalkyl;
- R c is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl;
- R d is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- X is a bond, - -[C(R a Rb)]pN( optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R z is selected from hydrogen, substituted or unsubstituted C 1 -6 alkyl, substituted or unsubstituted C 2.6 alkenyl, substituted or unsubstituted C 2 -6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and - C(0)-Ci- 6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R a is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- Rb is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound according to the according to the invention of general Formula (I) is a compound wherein R a and R b , taken together with the carbon atom to which they are attached, form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R c is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R d is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein X is selected from a bond, -[CH 2 ] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ] p N(R z )C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )[CH 2 ] q -; preferably X is selected from a bond, -[CH 2 ] p -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ]pN(R z )C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )[CH 2 ] q -; more preferably bond or a substituted or unsubstituted group selected from -CH
- Ri is and/or
- R z is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2- e alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci- 6 alkyl; preferably R z is selected from hydrogen; and/or p is 0, 1 , 2, 3, 4 or 5; preferably p is 0, 1 or 2; and/or q is 0, 1 , 2, 3, 4 or 5; preferably q is 0 or 1 ; and/or
- Yi is -C(RioRio )-; preferably Yi is -CH 2 -; and/or Y2 is -C(RioRio ⁇ )-; preferably and/or n is 0 or 1 ; and/or m is O or l ; and/or r is 0 or 1 ; and/or t is 0 or 1 ;
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, preferably R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, more preferably R 2 is a substituted or unsubstituted group selected from phenyl and thiophen; and/or
- R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably R 3 is substituted or unsubstituted C 1-6 alkyl; more preferably R 3 is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; and/or
- R 3' is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably R 3 is hydrogen or substituted or unsubstituted methyl; and/or
- R 4 and RA ⁇ are independently selected from halogen, -R 4 I , -OR 4I , -N0 2 , -NR 4i R 4 r, - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 , -S(0) 2 NR 4i R 4 , -NR 4i C(0)NR 4r R 4r , -SR 4 I , -S(0)R 41 , - S(0) 2 R 4I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4I R 4I , -OCH 2 CH 2 OR 4 I , - NR 4i S(0) 2 NR 4 rR 4 r and -C(CH 3 ) 2 OR 4 I ; preferably R 4 and R 4 ⁇ are both hydrogen; and/or
- Rs, Rs ⁇ , Rs- and Rs ⁇ are independently selected from hydrogen, halogen, substituted or unsubstituted C alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; preferably Rs, Rs ⁇ , Rs- and Rs ⁇ are all hydrogen; alternatively, Rs and Rs ⁇ and/or Rs- and Rs taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl and/or
- Re, Re ⁇ , Re ⁇ and Rs- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2- e alkenyl and substituted or unsubstituted C 2-6 alkynyl; preferably R 6 , Re ⁇ , R 6 and R 6 are all hydrogen; alternatively, R 6 and R 6 ⁇ and/or R 6 - and R 6 taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, R 6 and Rs ⁇ and/or Re- and R 6 ⁇ taken together with the carbon atom to which they are attached may form a carbonyl group; and/or R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; preferably R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; more preferably
- Re is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably Re is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl; and/or
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -e alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably Re ⁇ is selected from hydrogen and substituted or unsubstituted methyl; and/or
- Ra and Ra ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- Rg and Rg ⁇ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21', -NR 2i C(0)R 2 r, -NR2iS(0)2R2r, -S(0)2NR2iR2r, - NR2iC(0)NR2rR2r, -SR21 , -S(0)R 2 I , -S(0) 2 R 2 I , -CN, haloalkyl, haloalkoxy, -C(0)OR 2 I , -C(0)NR 2i R 2 r, - OCH2CH2OR21, -NR2iS(0)2NR2i'R2r and -C(CH3)20R2i; preferably Rg and Rg ⁇ are selected from hydrogen, halogen and -CN; more preferably Rg and Rg ⁇ are selected from hydrogen, fluorine and -CN; and/or R 10 and Rio are independently selected from hydrogen, substituted or unsubstit
- Rio ⁇ and Rio- are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2 - 6 alkynyl; preferably Rio- and Rio- are both hydrogen; alternatively, Rio- and R 10 - may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; preferably Rio- and Rio- form, with the carbon atom to which they are attached, a substituted or unsubstituted cyclopropyl;
- R 13 and RI 3 ⁇ are independently selected from hydrogen, unsubstituted C 1.6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl; and/or
- R 14 , Ri b and Rn- are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C 2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; and/or
- R 21 , R 21 ' and R 21 ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 -6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; and/or R 31 , R 31 ' and R 3 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; and/or
- R 32 and R 32' are independently selected from hydrogen, substituted or unsubstituted Ci- e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; and/or
- R 41 , R 4 r and R 41" are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; preferably R 41 is hydrogen; and/or
- R 51 , Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- R 6i , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted Cre alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; and/or
- R 71 , R 71 ' and R 71" are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably R 71 is hydrogen; and/or Rei, Rer and R 8 r are independently selected from hydrogen, substituted or unsubstituted Ci-a alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; and/or RS2, RS2' and Ra2 ” are independently selected from hydrogen, substituted or unsubstituted Ci-a alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; and/or
- RS3, RS3' and Ra3 ⁇ are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- X is selected from a bond, -[CH 2 ] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ] p N(Rz)C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )[CH 2 ] q -; preferably X is selected from a bond,
- R z is selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci- 6 alkyl; preferably R z is selected from hydrogen; and/or p is 0, 1 , 2, 3, 4 or 5; preferably p is 0, 1 or 2; and/or q is 0, 1 , 2, 3, 4 or 5; preferably q is 0 or 1 ; and/or
- Yi is -C(RioRio ⁇ )-; preferably Y1 is -CH2-; and/or
- Y2 is -C(RioRio )-; preferably and/or n is 0 or 1 ; and/or m is 0 or 1 ; and/or r is 0 or 1 ; and/or t is 0 or 1 ;
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, preferably R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl, more preferably R 2 is a substituted or unsubstituted group selected from phenyl and thiophen; and/or R 3 is selected from substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;preferably R 3 is substituted or unsubstituted C 1-6 alkyl; more preferably R 3 is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; and/or
- R 3 is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2- e alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably R 3' is hydrogen or substituted or unsubstituted methyl; and/or R 4 and R ⁇ are independently selected from halogen, -R 4 I , -OR 4 I, -N0 2 , -NR 4i R r, - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 4i R 4r , -NR 4i C(0)NR 4r R r, -SR 4 I , -S(0)R 4i , - S(0) 2 R 4 I , -CN, haloalkyl, haloalkoxy, -C(0)OR 4 I , -C(0)NR 41 R 4 r, -OCH 2 CH 2 OR 41
- R5, Rs ⁇ , Rs- and Rs ⁇ are independently selected from hydrogen, halogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; preferably Rs, Rs ⁇ , Rs- and Rs - are all hydrogen; alternatively, Rs and Rs ⁇ and/or Rs- and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl and/or
- Re, Re ⁇ , Re- and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci-s alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2- e alkynyl; preferably Re, Re ⁇ , Re- and Re- are all hydrogen; - alternatively, R 6 and R 6 ⁇ and/or R 6 ⁇ and Rs- taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; alternatively, Rs and R 6 ⁇ and/or R 6 - and Rs - taken together with the carbon atom to which they are attached may form a carbonyl group; and/or
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; preferably R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted aromatic heterocyclyl; more preferably R 7 is selected from substituted or unsubstituted phenyl and substituted or unsubstituted pyridine and substituted or unsubstituted thiophen;
- Re is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably Re is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl; and/or
- Re ⁇ is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably Re ⁇ is selected from hydrogen and substituted or unsubstituted methyl; and/or
- Re and Re ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl;
- Rg and Rg ⁇ are independently selected from hydrogen, halogen, -R21, -OR21, -N0 2 , - NR21R21 ⁇ , -NR 2i C(0)R 2 r, -NR2iS(0)2R2r, -S(0)2NR2iR2r, - NR2iC(0)NR2i R2i”, -SR21 , -S(0)R 2 I , -S(0) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C(0)OR 2 I , -C(0)NR 2i R 2 r, - OCH2CH2OR21, -NR2iS(0)2NR 2 rR2i " and -C(CH 3 )20R2i; preferably Rg and Rg ⁇ are selected from hydrogen, halogen and -CN; more preferably Rg and Rg ⁇ are selected from hydrogen, fluorine and -CN; and/or
- R10 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci- e alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R10 and R ⁇ are both hydrogen; alternatively, R 10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl;
- Rio- and/or Rio- and Rio- are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2 - e alkynyl; preferably R io ⁇ and Rio- are both hydrogen; alternatively, Rio- and Rio- may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; preferably Rio ⁇ and Rio- form, with the carbon atom to which they are attached, a substituted or unsubstituted cyclopropyl;
- R 13 and Ri 3' are independently selected from hydrogen, unsubstituted C 1 -6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl; and/or
- R 14 , Ri 4’ and R 14 are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C 2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; and/or
- R 21 , R 21’ and R 21 ⁇ are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; and/or
- R 31 , R 31 ' and R 31 " are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; and/or
- R 32 and R 32 are independently selected from hydrogen, substituted or unsubstituted Ci. 6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; and/or
- R41 , R 4 r and R41 " are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-8 alkenyl and substituted or unsubstituted C 2-6 alkynyl; preferably R41 is hydrogen; and/or
- R51 , Rsr and Rsr are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- R 61 , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; and/or
- R71 , R71' and R71 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 -6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably R71 is hydrogen; and/or
- Rei , Rsr and R 8 r are independently selected from hydrogen, substituted or unsubstituted Ci -8 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; and/or
- R 82 , Re and R 82 are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2- 6 alkynyl; and/or RS3, Re3' and R83- are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- X is selected from a bond, -[CH 2 ] P -, -[CH 2 ]pC(0)[CH 2 ]q-, -[CH 2 ] p C(0)N(R z )[CH 2 ] q -, - [CH 2 ] p N(R z )C(0)[CH 2 ]q- and -[CH 2 ] p N(R z )[CH 2 ] q -; and/or p is 0, 1 , 2, 3, 4 or 5; and/or q is 0, 1 , 2, 3, 4 or 5; and/or n is 0 or 1 ;
- Yi is -C(RioRio )-;
- Y 2 is— C(Rio'Rio ) ! and/or Ri is and/or m is 0, 1 or 2; and/or r is 0, 1 or 2;
- R z is selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci- 6 alkyl; wherein the alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or
- the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2 -6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkenyl is preferably selected from
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, wherein the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine
- R 3 is selected from substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein
- the alkyl is C1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the Ci- 6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl or ethyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C3
- R 3' is selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl;
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C 1-6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- R 4 and R 4 are independently selected from halogen, -R 4 I , -OR 4 I, -NO2, -NR 4i R 4 r, - NR 4i C(0)R 4r , -NR 4i S(0) 2 R 4 r, -S(0) 2 NR 41 R 4r , -NR 4i C(0)NR 4 rR 4r , -SR 41 , -S(0)R 4i , - S(0) 2 R 4I , -CN, haloalkyl, haloalkoxy, -C(0)0R 4i , -C(0)NR 4i R 4r , -OCH 2 CH 2 OR 4 I , - NR 4 IS(0) 2 NR 4 I R 4 I ” and -C(CH 3 ) 2 OR 4 I ; wherein
- the alkyl is C 1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl;
- R 5 , R 5 , R 5 ” and R 5 ”' are independently selected from hydrogen, halogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2- e alkenyl and substituted or unsubstituted C 2-6 alkynyl; wherein
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; alternatively, R 5 and R 5 ⁇ and/or R 5” and R 5 taken together with the carbon atom to which they are attached may form a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl,
- Re, Re ⁇ , Re- and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; wherein the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; alternatively, Re and R 6 ⁇ and/or Re
- the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C 3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; alternatively, Re and Re ⁇ and/or Re- and R 6 ⁇ taken together with the carbon atom to which they are attached may form a carbonyl group;
- R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl;
- the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine, piperidine, piperazine, benzofuran, benzimidazole, indazole, benzothiazole, benzodiazole
- Re is selected from substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein the alkyl is C1.6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl or ethyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene
- Rs is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, substituted or unsubstituted C 2 -e alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; wherein the alkyl is C 1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C 1-6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hex
- Rg and Rg ⁇ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21’, -NR 2i C(0)R 2 r, -NR2iS(0)2R2r, -S(0)2NR2iR2r, - NR2iC(0)NR2i’R2i”, -SR21 , -S(0)R 21 , -S(0) 2 R 21 , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r, - OCH2CH2OR21, -NR 2i S(0) 2 NR 2 rR2r and -C(CH 3 ) 2 OR 2 I; wherein the alkyl is C 1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2- methyl propyl; and/or
- R1 0 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2- 6 alkenyl and substituted or unsubstituted C 2 -e alkynyl; wherein
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- R 10 and Rio ⁇ may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; wherein the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; and/or
- R 10 - and Ri ⁇ r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2- e alkynyl; wherein
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or
- the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C 3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl; and/or
- R 13 and RI 3 ⁇ are independently selected from hydrogen, unsubstituted C 1-6 alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl;
- Ci-ealkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or
- R 14 , R I4 ⁇ and Ru- are independently selected from hydrogen, unsubstituted Ci-s alkyl, unsubstituted C 2 -e alkenyl, unsubstituted C 2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; wherein
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkyl like cyclopropy
- R 21 , R 21' and R 21” are independently selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; wherein
- the Ci. 6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C 1-6 alkyl is methyl, ethyl or propyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- R31, R31' and R31" are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C 2 -6 alkynyl; wherein the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methyl propyl; and/or the C 2 -6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- R32 and R32' are independently selected from hydrogen, substituted or unsubstituted Ci-6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; wherein the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- R41 , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2 -e alkenyl and substituted or unsubstituted C2-6 alkynyl; wherein
- the Ci- 6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C 1-6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or
- R 51 , Rsr and R 51" are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; wherein the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- R 61 , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; wherein the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C 1-6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/
- R 71 , R 71' and R 7 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably, the C 1-6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or
- Rer and R 8 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; wherein
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or
- RS2, RS 2 ⁇ and R 82 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or
- R83, S 3' and R 83” are independently selected from hydrogen, substituted or unsubstituted C 1.6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl;
- the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R z as defined in any of the embodiments of the present invention, the alkyl is Ci- 6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R 2 as defined in any of the embodiments of the present invention, the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R3 as defined in any of the embodiments of the present invention, the alkyl is C1.6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl or ethyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyl, hexyl, isopropyl
- the compound is a compound, wherein in R 3' as defined in any of the embodiments of the present invention, the C 1.6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C 1-6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form
- the compound is a compound, wherein in R 4 and R 4 ⁇ as defined in any of the embodiments of the present invention, the alkyl is Ci -6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the alkyl is Ci -6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers,
- the compound is a compound, wherein in Rs, Rs ⁇ , Rs ⁇ and Rs - as defined in any of the embodiments of the present invention, the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at
- the compound is a compound, wherein in R 5 , Rs ⁇ , Rs ⁇ and Rs- as defined in any of the embodiments of the present invention, the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C 3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R 6 , R 6 ⁇ , R 6 - and Re- as defined in any of the embodiments of the present invention, the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R 6 , !3 ⁇ 4', R 6 - and Re- as defined in any of the embodiments of the present invention, the cycloalkyl is C3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two
- the compound is a compound, wherein in R 7 as defined in any of the embodiments of the present invention, the aryl is selected from phenyl, naphthyl, or anthracene; preferably is naphthyl and phenyl; preferably the aryl is phenyl; and/or the heterocyclyl is a heterocyclic ring system of one or more saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring; preferably is a heterocyclic ring system of one or two saturated or unsaturated rings of which at least one ring contains one or more heteroatoms selected from the group consisting of nitrogen, oxygen and/or sulfur in the ring, more preferably is selected from oxazepan, pyrrolidine, imidazole, oxadiazole, tetrazole, azetidine, pyridine, pyrimidine
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in Rs as defined in any of the embodiments of the present invention, the alkyl is Ci_ 6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the C1-6 alkyl is methyl or ethyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyl, hexyl, isopropyl
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in Rs as defined in any of the embodiments of the present invention, the alkyl is C 1-6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the Ci_ 6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2 -e -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in Rg and Rg as defined in any of the embodiments of the present invention, the alkyl is Ci- 6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2- methylpropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the alkyl is Ci- 6 alkyl like methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2- methylpropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers,
- the compound is a compound, wherein in R 10 and Rio as defined in any of the embodiments of the present invention, the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or ‘ diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R 10 and R ⁇ as defined in any of the embodiments of the present invention, the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C 3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enanti
- the compound is a compound, wherein in Rio- and R 10 as defined in any of the embodiments of the present invention, the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R 10 ⁇ and Rio- as defined in any of the embodiments of the present invention, the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, or cyclooctyl; preferably is C 3-7 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, or cycloheptyl; more preferably from C 3-6 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl; preferably the cycloalkyl is cyclopropyl;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R 13 and Ri 3 as defined in any of the embodiments of the present invention, the Ci-ealkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne;
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R14, RH ⁇ and R14 as defined in any of the embodiments of the present invention, the Ci-6alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; and/or the cycloalkyl is C 3-8 cycloalkyl like cyclopropyl, cyclobutyl, cyclopentyl,
- stereoisomers optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein in R21, R 2 r and R21 as defined in any of the embodiments of the present invention,
- the C1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C1-6 alkyl is methyl, ethyl or propyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers
- the compound is a compound, wherein in R31 , R 3 r and R 3 r as defined in any of the embodiments of the present invention,
- the Ci-ealkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate
- the compound is a compound, wherein in R 32 and R 32 ⁇ as defined in any of the embodiments of the present invention,
- the Ci- 6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate
- the compound is a compound, wherein in R 4I , R 4 r and R 4 r as defined in any of the embodiments of the present invention,
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the Ci -6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or
- the compound is a compound, wherein in R 51 , Rsr and Rsr as defined in any of the embodiments of the present invention,
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate
- the compound is a compound, wherein in R 61 , R 6 r and Rer as defined in any of the embodiments of the present invention, the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl, more preferably the C 1-6 alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastere
- the compound is a compound, wherein in R 71 , R 7 r and R 7 r as defined in any of the embodiments of the present invention,
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; preferably the Ci-e alkyl is methyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a
- the compound is a compound, wherein in Rei, Rer and Rer as defined in any of the embodiments of the present invention,
- the Ci- 6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate
- the Ci- 6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C 2-6 -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate
- the compound is a compound, wherein in R 83 , Re3' and R 83 ⁇ as defined in any of the embodiments of the present invention,
- the C 1-6 alkyl is preferably selected from methyl, ethyl, propyl, butyl, pentyl, hexyl, isopropyl, or 2-methylpropyl; and/or the C 2-6 -alkenyl is preferably selected from ethylene, propylene, butylene, pentylene, hexylene, isopropylene and isobutylene; and/or the C -alkynyl is preferably selected from ethyne, propyne, butyne, pentyne, hexyne, isopropyne and isobutyne; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein p is 0, 1 , 2, 3, 4 or 5; preferably p is 0, 1 or 2; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein q is 0, 1 , 2, 3, 4 or 5; preferably q is 0 or 1 ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein n is 0 or 1 ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein m is 0 or 1 ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein r is 0 or 1 ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein t is 0 or 1 ; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- X is selected from a X is selected from a bond, -[CH 2 ] P -, -[CH 2 ] P C(0)[CH2]q-, - [CH 2 ] p C(0)N(R z )[CH 2 ]q-, -[CH 2 ]pN(Rz)C(0)[CH 2 ] q - and -[CH 2 ] p N(R z )[CH 2 ] q -; preferably X is selected from a bond, -[CH 2 ] P -, -[CH 2 ] p C(0)[CH 2 ] q -, -[CH 2 ] p N(R z )C(0)[CH 2 ]q- and - [CH 2 ] p N(Rz)[CH 2 ]q-; more preferably bond or a substituted or unsubstituted group selected from -CH 2 -, -CH 2 CH 2 - , C(O), -
- the compound is a compound, wherein
- Yi is -C(RioRio')-; preferably Yi is -CH 2 -; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- Y 2 is -C(RioRio')-; preferably optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R z is selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkylcycloalkyl and -C(0)-Ci-e alkyl; preferably R z is selected from hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R 2 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl, preferably R 2 is a substituted or unsubstituted group selected from phenyl and thienyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R 3 is selected from substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl;preferably R 3 is substituted or unsubstituted C 1-6 alkyl; more preferably R 3 is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R 3' is selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably R 3' is hydrogen or substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R 4 and R 4' are independently selected from halogen, -R41, -OR41, -NO2, -NR41R41', - NR 4i C(0)R 4 r, -NR 4i S(0) 2 R 4 r, -S(0) 2 NR4iR4r, -NR4iC(0)NR 4 rR 4 r, -SR41 , -S(0)R 4i , - S(0) 2 R 4i , -CN, haloalkyl, haloalkoxy, -C(0)OR4i, -C(0)NR 4i R4r, -OCH2CH2OR41, - NR4iS(0)2 R4rR4i” and -C(CH3)20R4i; wherein R 41 , R 4 r and R 4 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted
- the compound is a compound, wherein
- R 5 , Rs ⁇ , Rs and R 5 - are all hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein Re, R 6' , R 6" and Re- are independently selected from hydrogen, halogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C alkenyl and substituted or unsubstituted C 2-6 alkynyl; preferably R 6 , R 6 ⁇ , R 6 - and Re- are all hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding soivate thereof.
- the compound is a compound, wherein
- R 6 , R 6' and/or R 6 may form a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- the compound is a compound, wherein R 7 is selected from substituted or unsubstituted aryl and substituted or unsubstituted heterocyclyl; preferably R 7 is selected from substituted or unsubstituted phenyl and substituted or unsubstituted pyridinyl and substituted or unsubstituted thienyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- Re is selected from substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably Rs is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- Rs is selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C2-6 alkenyl, substituted or unsubstituted C2-6 alkynyl, substituted or unsubstituted cycloalkyl and substituted or unsubstituted alkylcycloalkyl; preferably Re ⁇ is selected from hydrogen and substituted or unsubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- Re and R 8 ⁇ taken together with the nitrogen atom to which they are attached may form a substituted or unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- Rg and Rg ⁇ are independently selected from hydrogen, halogen, -R21, -OR21, -NO2, - NR21R21', -NR 2i C(0)R 2 r, -NR2iS(0)2R2r, -S(0)2NR2iR2r, - NR2iC(0)NR2rR2i'', -SR21 , -S(0)R 2 I , -S(0) 2 R 2i , -CN, haloalkyl, haloalkoxy, -C(0)0R 2i , -C(0)NR 2i R 2 r, - OCH2CH2OR21, -NR 2i S(0) 2 NR 2 rR 2i ⁇ ' and -C(CH 3 )20R2i; preferably Rg and Rg ⁇ are selected from hydrogen, halogen and -CN; more preferably Rg and Rg ⁇ are selected from hydrogen, fluorine and -CN; optionally in form of one of the stereoiso
- the compound is a compound, wherein
- R10 and Rio are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; preferably R10 and Rio are both hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R10 and Re form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- Rio ⁇ and Rio- are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2- e alkynyl; preferably Rio- and Rio- are both hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein Rio ⁇ and R 10 - may form, with the carbon atom to which they are attached, a substituted or unsubstituted cycloalkyl; preferably R KT and R 10 ' form, with the carbon atom to which they are attached, a substituted or unsubstituted cyclopropyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R 13 and R I3 ⁇ are independently selected from hydrogen, unsubstituted Ci-e alkyl, unsubstituted C 2-6 alkenyl, and unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R 14 , R M' and R 14 are independently selected from hydrogen, unsubstituted C1. 6 alkyl, unsubstituted C 2-6 alkenyl, unsubstituted C 2-6 alkynyl, unsubstituted aryl, unsubstituted cycloalkyl and unsubstituted heterocyclyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R21 , R21 ' and R 2 r are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R31 , R31' and R31 are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R32 and R32' are independently selected from hydrogen, substituted or unsubstituted Ci- 6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R41 , R41 ' and R41 " are independently selected from hydrogen, substituted or unsubstituted C1-6 alkyl, substituted or unsubstituted C2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; preferably R41 is hydrogen; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R51 , R51 ' and Rsr are independently selected from hydrogen, substituted or unsubstituted C1.6 alkyl, substituted or unsubstituted C2-6 alkenyl, and substituted or unsubstituted C2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein R 6 I , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted Cre alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2.6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- R 6 I , Rer and Rer are independently selected from hydrogen, substituted or unsubstituted Cre alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2.6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diaste
- the compound is a compound, wherein
- R 71 , R 71' and R 71” are independently selected from hydrogen, substituted or unsubstituted Ci -6 alkyl, substituted or unsubstituted C 2 -e alkenyl, and substituted or unsubstituted C 2-6 alkynyl; preferably R 71 is hydrogen or substituted or unsubstituted C 1-6 alkyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- Rr and R 8 r are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R 82 , R S2 ⁇ and Re are independently selected from hydrogen, substituted or unsubstituted Ci-e alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein
- R S3 , R S3 ⁇ and Rs 3 are independently selected from hydrogen, substituted or unsubstituted C 1-6 alkyl, substituted or unsubstituted C 2-6 alkenyl, and substituted or unsubstituted C 2-6 alkynyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- the compound is a compound, wherein p is 0, 1 or 2; and/or q is 0 or 1 ; and/or n is 0 or 1 ; and/or m is 0 or 1. and/or r is 0 or 1. and/or t is 0 or 1. and/or
- X is selected from a bond or a substituted or unsubstituted group selected from -CH 2 -, -CH 2 CH 2 - , C(O), -CH 2 C(0)-, -CH 2 CH 2 C(0)-, -NHC(0)CH 2 - and NHC(0)CH 2 CH 2 -; and/or
- Yi is -CH 2 -;
- R z is hydrogen
- Ri is and/or
- R 2 is a substituted or unsubstituted group selected from phenyl and thienyl; and/or
- R 3 is substituted or unsubstituted C 1-6 alkyl; more preferably R 3 is substituted or unsubstituted methyl or substituted or unsubstituted ethyl; and/or
- R 3' is hydrogen or substituted or unsubstituted methyl
- R 4 and R 4' are both hydrogen; and/or
- Re, Re ⁇ , R 6” and R 6 are all hydrogen; and/or
- R 7 is selected from substituted or unsubstituted phenyl and substituted or unsubstituted pyridinyl and substituted or unsubstituted thienyl; and/or
- Re is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl;
- Re ⁇ is selected from hydrogen and substituted or unsubstituted methyl; and/or R g and Rg ⁇ are selected from hydrogen, halogen and -CN; more preferably Rg and Rg ⁇ are selected from hydrogen, fluorine and -CN; and/or
- R 10 and Rio ⁇ are both hydrogen; and/or
- R 41 is hydrogen
- R 71 is hydrogen or substituted or insubstituted methyl; optionally in form of one of the stereoisomers, preferably enantiomers or diastereomers, a racemate or in form of a mixture of at least two of the stereoisomers, preferably enantiomers and/or diastereomers, in any mixing ratio, or a corresponding salt thereof, or a corresponding solvate thereof.
- p is 0, 1 or 2.
- n 0 or 1.
- m is 0 or 1.
- r is 0 or 1.
- t is 0 or 1.
- n and r are both 0.
- n and r are both 1.
- X is selected from a bond or a substituted or unsubstituted group selected from -CH 2 -, -CH2CH2- , C(O), -CH 2 C(0)-, -CH 2 CH 2 C(0)-, -NHC(0)CH 2 - and NHC(0)CH 2 CH2-.
- Yi and Y 2 are both -CH 2 -.
- R z is hydrogen
- R2 is a substituted or unsubstituted group selected from phenyl and thienyl.
- R 3 is substituted or unsubstituted Ci -6 alkyl; more preferably R 3 is substituted or unsubstituted methyl or substituted or unsubstituted ethyl.
- R 3' is hydrogen or substituted or unsubstituted methyl.
- R 3 is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl, while R 3 ⁇ is selected from substituted or unsubstituted methyl and hydrogen.
- R 3 is substituted or unsubstituted methyl, while R 3 ⁇ is selected from substituted or unsubstituted methyl and hydrogen.
- R 3 ⁇ is selected from substituted or unsubstituted methyl and hydrogen.
- R 3 is substituted or unsubstituted ethyl, while R 3 - is hydrogen.
- R 3 and R 3 ⁇ are both substituted or unsubstituted methyl.
- R 4 and R 4' are both hydrogen.
- Rs, Rs ⁇ , Rs- and R5 are all hydrogen.
- Re, Re ⁇ , R 6" and Re- are all hydrogen.
- R 7 is selected from substituted or unsubstituted phenyl and substituted or unsubstituted pyridinyl and substituted or unsubstituted thienyl.
- Re is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl.
- Re ⁇ is selected from hydrogen and substituted or unsubstituted methyl.
- Rs is selected from substituted or unsubstituted methyl and substituted or unsubstituted ethyl, while Rs ⁇ is selected from hydrogen and substituted or unsubstituted methyl.
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Abstract
La présente invention concerne des dérivés de dialkylaminoarylpipéridinyl-o-phénoxy et de obenzyloxypropylamino présentant une activité pharmacologique double à la fois envers la sous-unité α2δ, en particulier la sous-unité α2δ-1, du canal calcique sensible à la tension et du récepteur opioïde µ, des procédés de préparation de ces composés, des compositions pharmaceutiques les comprenant, ainsi que leur utilisation thérapeutique, en particulier pour traiter la douleur.
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| EP17382842.7 | 2017-12-12 | ||
| EP17382842 | 2017-12-12 |
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| WO2019115008A1 true WO2019115008A1 (fr) | 2019-06-20 |
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| PCT/EP2018/000554 Ceased WO2019115008A1 (fr) | 2017-12-12 | 2018-12-11 | Dérivés de dialkylaminoarylpipéridinyl-o-phénoxy et de o-benzyloxypropylamino présentant une activité multimodale contre la douleur |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3858439A1 (fr) * | 2020-02-03 | 2021-08-04 | Esteve Pharmaceuticals, S.A. | Dérivés d'amides ayant une activité pluri-modale contre la douleur |
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| US20100311782A1 (en) * | 2009-06-08 | 2010-12-09 | Adolor Corporation | Substituted piperidinylpropanoic acid compounds and methods of their use |
| WO2017191304A1 (fr) * | 2016-05-06 | 2017-11-09 | Laboratorios Del Dr. Esteve, S.A. | Composés de tétrahydropyrimidodiazépine et de tétrahydropyridodiazépine pour le traitement de la douleur et des affections associées à la douleur |
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2018
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| US20100311782A1 (en) * | 2009-06-08 | 2010-12-09 | Adolor Corporation | Substituted piperidinylpropanoic acid compounds and methods of their use |
| WO2017191304A1 (fr) * | 2016-05-06 | 2017-11-09 | Laboratorios Del Dr. Esteve, S.A. | Composés de tétrahydropyrimidodiazépine et de tétrahydropyridodiazépine pour le traitement de la douleur et des affections associées à la douleur |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3858439A1 (fr) * | 2020-02-03 | 2021-08-04 | Esteve Pharmaceuticals, S.A. | Dérivés d'amides ayant une activité pluri-modale contre la douleur |
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