AR049711A1 - HETEROCICLIC COMPOUNDS CONDENSED AS INHIBITORS OF ALDOSTERONE SINTASA; PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OR PREVENTION OF DISEASES RELATED TO HYPERALDOSTERISM AND EXCESSIVE CORTISO RELEASE - Google Patents
HETEROCICLIC COMPOUNDS CONDENSED AS INHIBITORS OF ALDOSTERONE SINTASA; PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OR PREVENTION OF DISEASES RELATED TO HYPERALDOSTERISM AND EXCESSIVE CORTISO RELEASEInfo
- Publication number
- AR049711A1 AR049711A1 ARP050102846A ARP050102846A AR049711A1 AR 049711 A1 AR049711 A1 AR 049711A1 AR P050102846 A ARP050102846 A AR P050102846A AR P050102846 A ARP050102846 A AR P050102846A AR 049711 A1 AR049711 A1 AR 049711A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- alkylcarbonyl
- halogen
- heterocyclyl
- carboxyalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- PQSUYGKTWSAVDQ-ZVIOFETBSA-N Aldosterone Chemical compound C([C@@]1([C@@H](C(=O)CO)CC[C@H]1[C@@H]1CC2)C=O)[C@H](O)[C@@H]1[C@]1(C)C2=CC(=O)CC1 PQSUYGKTWSAVDQ-ZVIOFETBSA-N 0.000 title abstract 2
- PQSUYGKTWSAVDQ-UHFFFAOYSA-N Aldosterone Natural products C1CC2C3CCC(C(=O)CO)C3(C=O)CC(O)C2C2(C)C1=CC(=O)CC2 PQSUYGKTWSAVDQ-UHFFFAOYSA-N 0.000 title abstract 2
- 229960002478 aldosterone Drugs 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 230000002265 prevention Effects 0.000 title 1
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 abstract 7
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 6
- 150000002367 halogens Chemical class 0.000 abstract 6
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 5
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000004043 oxo group Chemical group O=* 0.000 abstract 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 5
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 2
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 2
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 abstract 1
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 229960000890 hydrocortisone Drugs 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 230000002285 radioactive effect Effects 0.000 abstract 1
- 125000004665 trialkylsilyl group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/06—Peri-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/06—Drugs for disorders of the endocrine system of the anterior pituitary hormones, e.g. TSH, ACTH, FSH, LH, PRL, GH
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
- A61P5/40—Mineralocorticosteroids, e.g. aldosterone; Drugs increasing or potentiating the activity of mineralocorticosteroids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/06—Peri-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Endocrinology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Uso de estos compuestos como medicamentos, en particular como inhibidores de la cintaza de aldosterona y de la liberacion de cortisol. Se proveen asimismo composiciones farmacéuticas que los contienen como principio activo. Reivindicacion 1: Compuesto de la formula general (1), en la que: V es C o, si X es C, también es N; W es C o, si Z es un enlace y X es C, también es N; X es C o, si Z es un enlace, también es N; Y es C; Z es C o un enlace; en donde V e Y forman, con inclusion de X, un anillo heterocíclico o carbocíclico de 5-9 miembros, no sustituido o sustituido con 1-4 de alquilo C1-8, alquilcarbonilo C0-8, halogeno, ciano, oxo, trifluormetilo, alcoxi C1-8 o alcoxicarbonilo C1-8; R1 es alquilo C1-8, cicloalquilo C3-8, alquenilo C2-8, alquinilo C2-8, arilalquilo C0-4 o heterociclilalquilo C0-4 insaturado, cuyos radicales no están sustituidos o están sustituidos con 1-4 de alquilo C1-8, alquilcarbonilo C0-8, halogeno, ciano, oxo, trifluorometilo, alquilcarbonilamino C0-8, alquilcarbonilC0-8alquilaminoC1-8, carbamoilo, mono o dialquilaminocarbonilo C1-8, carboxialquilo C0-4, alcoxi C1-8, alcoxicarbonilo C1-8, heterociclilo o arilo, donde el heterociclilo o el arilo pueden estar sustituidos con 1-4 de alquilo C1-8, alquilcarbonilo C0-8, halogeno, alquilsulfonilo C1-8, ciano, oxo, trialquilsililo C1-4, trifluormetoxi, trifluormetilo, alquilcarbonilamino C0-6, alquilcarbonilC0-8alquilaminoC1-8amino, carbamoilo, mono- o dialquilaminocarbonilo C1-8, carboxialquilo C0-4, alcoxi C1-8 o alcoxicarbonilo C1-8; R2 a) es hidrogeno; o b) es alquilo C1-8, cicloalquilo C3-8, halogeno, carboxialquilo C1-4, alcoxiC1-4carbonilalquiloC0-4, alquilcarbonilo C0-4, arilalquilo C0-4 o heterociclilalquilo C0-4 insaturado, cuyos radicales no están sustituidos o están sustituidos con 1-4 de alquilo C1-8, alquilcarbonilo C0-8, halogeno, ciano, oxo, trifluormetilo, alquilcarbonilamino C0-8, alquilcarbonilC0-8alquilaminoC1-8, mono- o dialquilaminocarbonilo C1-8, carboxialquilo C0-4, alcoxi C1-8, alcoxicarbonilo C1-8, heterociclilo o arilo, donde el heterociclilo o el arilo pueden estar sustituidos con 1-4 de alquilo C1-8, alquilcarbonilo C0-8, halogeno, ciano, oxo, trifluormetilo, alquilcarbonilamino C0-8, alquilcarbonilC0-8alquilaminoC1-8, carbamoilo, mono- o dialquilaminocarbonilo C1-8, carboxialquilo C0-4, alcoxi C1-8 o alcoxicarbonilo C1-8; n es un numero 0, 1 o 2; y su sal, profármaco o compuesto en el que uno o más átomos se reemplazan por sus isotopos estables no radiactivos, especialmente sales utilizables farmacéuticamente.Use of these compounds as medicaments, in particular as inhibitors of aldosterone tapeza and cortisol release. Pharmaceutical compositions are also provided which contain them as active ingredient. Claim 1: Compound of the general formula (1), wherein: V is C or, if X is C, it is also N; W is C or, if Z is a link and X is C, it is also N; X is C or, if Z is a link, it is also N; Yes c; Z is C or a link; wherein V and Y form, including X, a 5-9 membered heterocyclic or carbocyclic ring, unsubstituted or substituted with 1-4 of C1-8 alkyl, C0-8 alkylcarbonyl, halogen, cyano, oxo, trifluoromethyl, C1-8 alkoxy or C1-8 alkoxycarbonyl; R1 is C1-8 alkyl, C3-8 cycloalkyl, C2-8 alkenyl, C2-8 alkynyl, C0-4 arylalkyl or unsaturated C0-4 heterocyclyl alkyl, the radicals of which are unsubstituted or substituted with 1-4 of C1-8 alkyl , C0-8 alkylcarbonyl, halogen, cyano, oxo, trifluoromethyl, C0-8 alkylcarbonylaminoC0-8alkylcarbonylC1-8, carbamoyl, mono or dialkylaminocarbonyl C1-8, carboxyalkyl C0-4, C1-8 alkoxy, C1-8 alkoxycarbonyl, heterocyclyl or aryl, where the heterocyclyl or aryl may be substituted with 1-4 of C1-8 alkyl, C0-8 alkylcarbonyl, halogen, C1-8 alkylsulfonyl, cyano, oxo, C1-4 trialkylsilyl, trifluoromethoxy, trifluoromethyl, C0- alkylcarbonylamino 6, C0-8 alkylcarbonylC1-8alkylamino, carbamoyl, mono- or dialkylaminocarbonyl C1-8, carboxyalkyl C0-4, C1-8 alkoxy or C1-8 alkoxycarbonyl; R2 a) is hydrogen; or b) is C1-8 alkyl, C3-8 cycloalkyl, halogen, C1-4 carboxyalkyl, C1-4 alkoxycarbonylC0-4, C0-4 alkylcarbonyl, C0-4 arylalkyl or unsaturated C0-4 heterocyclyl alkyl, the radicals of which are unsubstituted or substituted with 1-4 of C1-8 alkyl, C0-8 alkylcarbonyl, halogen, cyano, oxo, trifluoromethyl, C0-8 alkylcarbonylamino, C0-8 alkylcarbonylC1-8, mono- or dialkylaminocarbonyl C1-8, carboxyalkyl C0-4, C1- alkoxy 8, C1-8 alkoxycarbonyl, heterocyclyl or aryl, where the heterocyclyl or aryl can be substituted with 1-4 of C1-8 alkyl, C0-8 alkylcarbonyl, halogen, cyano, oxo, trifluoromethyl, C0-8 alkylcarbonylamino, C0- alkylcarbonyl C 1-8 alkylamino, carbamoyl, mono- or C 1-8 dialkylaminocarbonyl, C 0-4 carboxyalkyl, C 1-8 alkoxy or C 1-8 alkoxycarbonyl; n is a number 0, 1 or 2; and its salt, prodrug or compound in which one or more atoms are replaced by their stable non-radioactive isotopes, especially pharmaceutically usable salts.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CH11562004 | 2004-07-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR049711A1 true AR049711A1 (en) | 2006-08-30 |
Family
ID=35457694
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050102846A AR049711A1 (en) | 2004-07-09 | 2005-07-08 | HETEROCICLIC COMPOUNDS CONDENSED AS INHIBITORS OF ALDOSTERONE SINTASA; PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM AND THEIR USE IN THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OR PREVENTION OF DISEASES RELATED TO HYPERALDOSTERISM AND EXCESSIVE CORTISO RELEASE |
Country Status (3)
| Country | Link |
|---|---|
| AR (1) | AR049711A1 (en) |
| TW (1) | TW200611897A (en) |
| WO (1) | WO2006005726A2 (en) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1842543A1 (en) * | 2006-04-05 | 2007-10-10 | Speedel Pharma AG | Pharmaceutical composition coprising an aldosterone synthase inhibitor and a mineralcorticoid receptor antagonist |
| TW200808813A (en) * | 2006-04-12 | 2008-02-16 | Speedel Experimenta Ag | Imidazo compounds |
| EP1886695A1 (en) * | 2006-06-27 | 2008-02-13 | Speedel Experimenta AG | Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist |
| JP5420761B2 (en) | 2009-05-28 | 2014-02-19 | ノバルティス アーゲー | Substituted aminopropionic acid derivatives as neprilysin inhibitors |
| EP2435402B1 (en) | 2009-05-28 | 2016-04-13 | Novartis AG | Substituted aminobutyric derivatives as neprilysin inhibitors |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors |
| US8673974B2 (en) | 2010-11-16 | 2014-03-18 | Novartis Ag | Substituted amino bisphenyl pentanoic acid derivatives as NEP inhibitors |
| CN103648495A (en) | 2011-07-08 | 2014-03-19 | 诺华股份有限公司 | Methods of treating atherosclerosis in subjects with high triglycerides |
| UY35144A (en) | 2012-11-20 | 2014-06-30 | Novartis Ag | APELINE SYNTHETIC LINEAR MIMETICS FOR THE CARDIAC INSUFFICIENCY TREATMENT |
| EA028583B1 (en) | 2013-02-14 | 2017-12-29 | Новартис Аг | Substituted bisphenyl butanoic phosphonic acid derivatives as nep (neutral endopeptidase) inhibitors |
| KR20160031551A (en) | 2013-07-25 | 2016-03-22 | 노파르티스 아게 | Cyclic polypeptides for the treatment of heart failure |
| HK1218252A1 (en) | 2013-07-25 | 2017-02-10 | Novartis Ag | Bioconjugates of synthetic apelin polypeptides |
| CR20170338A (en) | 2015-01-23 | 2017-09-12 | Novartis Ag | CONJUGATES OF FATTY ACIDS AND SYNTHETIC APPEAL WITH GREATER HALF LIFE |
| JOP20190086A1 (en) | 2016-10-21 | 2019-04-18 | Novartis Ag | Naphthyridinone derivatives and their use in the treatment of arrhythmia |
| UY38072A (en) | 2018-02-07 | 2019-10-01 | Novartis Ag | COMPOSITIONS DERIVED FROM BUTANOIC ESTER SUBSTITUTED WITH BISPHENYL AS INHIBITORS OF NEP, COMPOSITIONS AND COMBINATIONS OF THE SAME |
| UY38485A (en) | 2018-11-27 | 2020-06-30 | Novartis Ag | CYCLIC TETRAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN / KEXIN TYPE 9 (PCSK9) INHIBITORS, METHOD OF TREATMENT, USE AND PREPARATION |
| EP3887363A1 (en) | 2018-11-27 | 2021-10-06 | Novartis AG | Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder |
| EP3887388A1 (en) | 2018-11-27 | 2021-10-06 | Novartis AG | Cyclic peptides as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorders |
| WO2023084449A1 (en) | 2021-11-12 | 2023-05-19 | Novartis Ag | Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder |
| AR127698A1 (en) | 2021-11-23 | 2024-02-21 | Novartis Ag | NAFTYRIDINOONE DERIVATIVES FOR THE TREATMENT OF A DISEASE OR DISORDER |
| US20240391941A1 (en) | 2023-05-24 | 2024-11-28 | Novartis Ag | Naphthyridinone derivatives for the treatment of a disease or disorder |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2494636A1 (en) * | 2002-08-07 | 2004-02-19 | Novartis Ag | Organic compounds as agents for the treatment of aldosterone mediated conditions |
-
2005
- 2005-07-08 WO PCT/EP2005/053272 patent/WO2006005726A2/en not_active Ceased
- 2005-07-08 AR ARP050102846A patent/AR049711A1/en unknown
- 2005-07-08 TW TW094123144A patent/TW200611897A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2006005726A3 (en) | 2006-05-04 |
| WO2006005726A2 (en) | 2006-01-19 |
| TW200611897A (en) | 2006-04-16 |
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