AR079905A1 - Derivados biciclicos de triazol sustituidos como moduladores de gamma secretasa - Google Patents
Derivados biciclicos de triazol sustituidos como moduladores de gamma secretasaInfo
- Publication number
- AR079905A1 AR079905A1 ARP110100125A ARP110100125A AR079905A1 AR 079905 A1 AR079905 A1 AR 079905A1 AR P110100125 A ARP110100125 A AR P110100125A AR P110100125 A ARP110100125 A AR P110100125A AR 079905 A1 AR079905 A1 AR 079905A1
- Authority
- AR
- Argentina
- Prior art keywords
- halo
- aryl1
- substituents
- optionally substituted
- alkyl
- Prior art date
Links
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical group C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 15
- 125000001475 halogen functional group Chemical group 0.000 abstract 9
- 229910052739 hydrogen Inorganic materials 0.000 abstract 9
- 239000001257 hydrogen Substances 0.000 abstract 9
- 125000001424 substituent group Chemical group 0.000 abstract 7
- 150000001875 compounds Chemical class 0.000 abstract 6
- 125000003545 alkoxy group Chemical group 0.000 abstract 5
- 150000002431 hydrogen Chemical class 0.000 abstract 5
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 4
- -1 NR11dR12d Chemical group 0.000 abstract 3
- 125000002757 morpholinyl group Chemical group 0.000 abstract 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 abstract 2
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 2
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 2
- VHNYOQKVZQVBLC-RTCGXNAVSA-N (4r,7e,9as)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one Chemical compound C1([C@@H]2COC[C@@H]3CC\C(C(N32)=O)=C/C=2C=C(C(=CC=2)N2C=C(C)N=C2)OC)=CC(F)=C(F)C(F)=C1 VHNYOQKVZQVBLC-RTCGXNAVSA-N 0.000 abstract 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 abstract 1
- SSTIQTJTCBTBLQ-UHFFFAOYSA-N 5-(4-methoxyphenyl)-n-(4-pyridin-3-ylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine Chemical compound C1=CC(OC)=CC=C1C1=CC=CC2=NC(NC=3C=CC(=CC=3)C=3C=NC=CC=3)=NN12 SSTIQTJTCBTBLQ-UHFFFAOYSA-N 0.000 abstract 1
- NAQWHKZHLFTUFL-UHFFFAOYSA-N 5-(4-methoxyphenyl)-n-[4-(1,3-oxazol-5-yl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-amine Chemical compound C1=CC(OC)=CC=C1C1=CC=CC2=NC(NC=3C=CC(=CC=3)C=3OC=NC=3)=NN12 NAQWHKZHLFTUFL-UHFFFAOYSA-N 0.000 abstract 1
- 101001043818 Mus musculus Interleukin-31 receptor subunit alpha Proteins 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000002541 furyl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 125000001786 isothiazolyl group Chemical group 0.000 abstract 1
- 125000000842 isoxazolyl group Chemical group 0.000 abstract 1
- 125000001715 oxadiazolyl group Chemical group 0.000 abstract 1
- 125000002971 oxazolyl group Chemical group 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000001113 thiadiazolyl group Chemical group 0.000 abstract 1
- 125000000335 thiazolyl group Chemical group 0.000 abstract 1
- 125000001544 thienyl group Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 1
- 229940124648 γ-Secretase Modulator Drugs 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D401/02—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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Biomedical Technology (AREA)
- Medicinal Chemistry (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Psychology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Los compuestos de acuerdo con la presente solicitud son utiles como moduladores de gamma secretasa y para tratar por ejemplo Alzheimer, se refiere además a procesos para preparar dichos compuestos novedosos, composiciones farmacéuticas que comprenden dichos compuestos como ingrediente activo así como al uso de dichos compuestos como medicamento. Reivindicacion 1: Un compuesto de formula (1) o una de sus formas estereoisoméricas, donde Het1 es un heterociclo, que tiene formula (a-1), (a-2), (a-3), o (a-4); R3 es alquilo C1-4; R4, R5, R6, y R8 son cada uno independientemente hidrogeno o alquilo C1-4 sustituidos opcionalmente con uno o más sustituyentes halo; R7a es hidrogeno, halo, o alquilo C1-4; R7b y R7c son cada uno independientemente hidrogeno, halo, ciano, alquiloxi C1-4, cicloalquilo C3-7, o alquilo C1-4 sustituidos opcionalmente con uno o más sustituyentes halo; Xa es CH o N; Xb es O o S; A1 es CR9 o N; donde R9 es hidrogeno, halo, o alquiloxi C1-4; A2, A3 y A4 son cada uno independientemente CH o N; con la condicion de que como máximo dos de A1, A2, A3 y A4 sean N; L1 es O, carbonilo, NR10, NH-(C=O), o (C=O)-NH; donde R10 es hidrogeno o alquilo C1-4; R1 y -L2-R2 se toman juntos para formar un radical bivalente -R1-R2-L2- que tiene formula -(CH2)m-n-Y-(CH2)n (b-1); -(CH2)n-Y-(CH2)m-n- (b-2); -CH=CH-CH=CH- (b-3); -CH=CH-N=CH- (b-4); -CH=N-CH=CH- (b-5); -(CH2)q-r-Y-(CH2)r-1,2-bencenodiil- (b-6); -(CH2)r-Y-(CH2)q-r-1,2-bencenodiil- (b-7); donde (b-1) o (b-2) pueden contener un enlace insaturado; donde (b-1), (b-2) o el radical que contiene un enlace insaturado, pueden estar sustituidos en uno o más átomos de carbono con uno o, cuando es posible, dos sustituyentes, cada uno seleccionado independientemente del grupo integrado por arilo1, (C=O)-arilo1, O-arilo1, NR13d-arilo1, alquilC1-4carbonilo, halo, hidroxi y alquilo C1-4 sustituidos opcionalmente con uno o más sustituyentes halo; donde (b-3), (b-4) o (b-5) pueden estar sustituidos, cuando es posible, con uno o más sustituyentes, cada uno seleccionado independientemente del grupo integrado por arilo1, 1-piperidinilo, 1-pirrolidinilo, 4-morfolinilo, (C=O)-arilo1, O-arilo1, NR13f-arilo1, alquilC1-4carbonilo y alquilo C1-4 sustituidos opcionalmente con uno o más sustituyentes halo; donde dichos 1-piperidinilo, 1-pirrolidinilo o 4-morfolinilo pueden estar sustituidos con uno o más grupos trifluorometilo; donde (b-6) o (b-7) pueden estar sustituidos en uno o más grupos CH2 con uno o, cuando es posible, dos sustituyentes, cada uno seleccionado independientemente del grupo integrado por arilo1, (C=O)-arilo1, O-arilo1, NR13e-arilo1, alquilC1-4carbonilo, halo, hidroxi y alquilo C1-4, sustituidos opcionalmente con uno o más sustituyentes halo; y donde (b-6) o (b-7) pueden estar sustituidos en el resto 1,2-bencenodiil- con uno o más sustituyentes, cada uno seleccionado independientemente del grupo integrado por halo, alquiloxi C1-4, ciano, NR11dR12d, morfolinilo y alquilo C1-4, sustituidos opcionalmente con uno o más sustituyentes halo; Y representa un enlace directo, NR14 u O; donde R14 es hidrogeno, arilo1, (C=O)-arilo1, alquilC1-4,carbonilo o alquilo C1-4, sustituidos opcionalmente con uno o más sustituyentes halo; m representa 3 o 4; n representa 1; q representa 3, 4, 5 o 6; r representa 0, 1, 2 o 3; donde cada arilo1 representa independientemente fenilo sustituido opcionalmente con uno o más sustituyentes, cada uno seleccionado independientemente del grupo integrado por halo, alquiloxi C1-4, ciano, NR11eR12e, morfolinilo y alquilo C1-4, sustituidos opcionalmente con uno o más sustituyentes halo; o un heteroarilo de 5 o 6 miembros seleccionado del grupo integrado por furanilo, tiofenilo, pirazolilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, tiadiazolilo, oxadiazolilo, piridinilo, pirimidinilo, piridazinilo y pirazinilo, donde dicho heteroarilo de 5 o 6 miembros puede estar sustituido con uno o más sustituyentes, cada uno seleccionado independientemente del grupo integrado por halo, alquiloxi C1-4, ciano, NR11fR12f, morfolinilo y alquilo C1-4 sustituidos opcionalmente con uno o más sustituyentes halo; cada R11d, R11e y R11f es independientemente hidrogeno, alquilo C1-4 o alquilC1-4carbonilo; cada R12d, R12e y R12f es independientemente hidrogeno o alquilo C1-4; cada R13d, R13e y R13f es independientemente hidrogeno o alquilo C1-4 sustituidos opcionalmente con uno o más sustituyentes, cada uno seleccionado independientemente del grupo integrado por halo y cicloalquilo C3-7; o una de sus sales de adicion farmacéuticamente aceptables o uno de sus solvatos; con la condicion de que el compuesto no es 5-(4-metoxifenil)-N-[4-(5-oxazolil)fenil]-[1,2,4]triazolo[1,5-a]piridin-2-amina, 5-(4-metoxifenil)-N-[4-(3- piridinil)fenil]-[1,2,4]triazolo[1,5-a]piridin-2-amina, o 5-(4-metoxifenil)-N-[6-(1H-pirazol-4-il)-3-piridinil]-[1,2,4]triazolo[1,5-a]piridin-2-amina.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP10150892 | 2010-01-15 | ||
| EP10171292 | 2010-07-29 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR079905A1 true AR079905A1 (es) | 2012-02-29 |
Family
ID=43569255
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100124A AR079904A1 (es) | 2010-01-15 | 2011-01-14 | Derivados de triazol sustituidos como moduladores de la gamma secretasa |
| ARP110100125A AR079905A1 (es) | 2010-01-15 | 2011-01-14 | Derivados biciclicos de triazol sustituidos como moduladores de gamma secretasa |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110100124A AR079904A1 (es) | 2010-01-15 | 2011-01-14 | Derivados de triazol sustituidos como moduladores de la gamma secretasa |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US9145399B2 (es) |
| EP (2) | EP2523955B1 (es) |
| JP (2) | JP5824464B2 (es) |
| KR (2) | KR20120123677A (es) |
| CN (2) | CN102803261A (es) |
| AR (2) | AR079904A1 (es) |
| AU (2) | AU2011206635B2 (es) |
| BR (2) | BR112012017310A2 (es) |
| CA (2) | CA2784765A1 (es) |
| CL (2) | CL2012001956A1 (es) |
| EA (2) | EA021776B1 (es) |
| ES (2) | ES2512840T3 (es) |
| IL (2) | IL220840A (es) |
| MX (2) | MX2012008259A (es) |
| NZ (2) | NZ600648A (es) |
| PE (2) | PE20121511A1 (es) |
| PH (2) | PH12012501381A1 (es) |
| SG (2) | SG182506A1 (es) |
| TW (2) | TWI473807B (es) |
| WO (2) | WO2011086099A1 (es) |
| ZA (2) | ZA201205240B (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2481715T3 (es) | 2009-02-06 | 2014-07-31 | Janssen Pharmaceuticals, Inc. | Compuestos heterocíclicos bicíclicos sustituidos novedosos como moduladores de gamma-secretasa |
| AU2010262036B2 (en) | 2009-05-07 | 2014-10-30 | Cellzome Limited | Novel substituted indazole and aza-indazole derivatives as gamma secretase modulators |
| BRPI1009637A2 (pt) * | 2009-06-05 | 2019-04-30 | Cephalon, Inc | composto, composição e uso de um composto |
| BR112012000915A2 (pt) | 2009-07-15 | 2019-09-24 | Janssen Pharmaceuticals Inc | derivados de triazol e imidazol substituídos como moduladores de gama secretase. |
| EP2343294A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Substituted triazolopyridines |
| EP2343297A1 (en) | 2009-11-30 | 2011-07-13 | Bayer Schering Pharma AG | Triazolopyridines |
| CA2784765A1 (en) | 2010-01-15 | 2011-07-21 | Janssen Pharmaceuticals, Inc. | Novel substituted bicyclic triazole derivatives as gamma secretase modulators |
| UY33452A (es) | 2010-06-16 | 2012-01-31 | Bayer Schering Pharma Ag | Triazolopiridinas sustituidas |
| SG188296A1 (en) * | 2010-08-27 | 2013-04-30 | Merck Patent Gmbh | Triazolopyrazine derivatives |
| BR112013004746A2 (pt) | 2010-09-02 | 2016-06-07 | Takeda Pharmaceutical | "composto, medicamento, inibidor da produção de beta-amilóide, modulador de gama-secretase, métodos para inibir a produção de beta-amilóide, para modular gama-secretase, e para prevenir ou tratar deficiência cognitiva branda ou mal de alzheimer, e, uso do composto." |
| CN103502225B (zh) | 2011-03-24 | 2015-11-25 | 杨森制药公司 | 作为γ分泌酶调节剂的经取代的三唑基哌嗪以及三唑基哌啶衍生物 |
| AU2012285931B2 (en) | 2011-07-15 | 2017-01-12 | Cellzome Limited | Novel substituted indole derivatives as gamma secretase modulators |
| UA112096C2 (uk) | 2011-12-12 | 2016-07-25 | Байєр Інтеллектуал Проперті Гмбх | Заміщені триазолопіридини та їх застосування як інгібіторів ttk |
| JP6479476B2 (ja) * | 2012-02-21 | 2019-03-06 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | ＳｙｋチロシンキナーゼインヒビターおよびＧＣＮ２セリンキナーゼインヒビターとしての８−置換２−アミノー［１，２，４］トリアゾロ［１，５−Ａ］ピラジン類 |
| EP2822948B1 (en) * | 2012-03-07 | 2016-04-06 | Merck Patent GmbH | Triazolopyrazine derivatives |
| ES2605946T3 (es) | 2012-03-14 | 2017-03-17 | Bayer Intellectual Property Gmbh | Imidazopiridazinas sustituidas |
| KR102096625B1 (ko) | 2012-05-16 | 2020-04-03 | 얀센 파마슈티칼즈, 인코포레이티드 | (무엇보다도) 알츠하이머병의 치료에 유용한 치환 3,4-디하이드로-2h-피리도[1,2-a]피라진-1,6-디온 유도체 |
| CN103508957B (zh) * | 2012-06-25 | 2017-02-08 | 中国科学院上海药物研究所 | 羟乙基吡唑类化合物或氨乙基吡唑类化合物及其制备方法和用途 |
| US20140010783A1 (en) * | 2012-07-06 | 2014-01-09 | Hoffmann-La Roche Inc. | Antiviral compounds |
| EP2687528A1 (en) | 2012-07-17 | 2014-01-22 | Ares Trading S.A. | Fused triazole derivatives as gamma secretase modulators |
| JOP20180012A1 (ar) * | 2012-08-07 | 2019-01-30 | Janssen Pharmaceutica Nv | عملية السلفنة باستخدام نونافلوروبوتانيسولفونيل فلوريد |
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