CA2506799A1 - Modulateurs de la kinase a lignee evolutive mixte - Google Patents
Modulateurs de la kinase a lignee evolutive mixte Download PDFInfo
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- CA2506799A1 CA2506799A1 CA002506799A CA2506799A CA2506799A1 CA 2506799 A1 CA2506799 A1 CA 2506799A1 CA 002506799 A CA002506799 A CA 002506799A CA 2506799 A CA2506799 A CA 2506799A CA 2506799 A1 CA2506799 A1 CA 2506799A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- dihydro
- alkoxy
- pyridin
- pyrrolo
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 108090001035 mitogen-activated protein kinase kinase kinase 12 Proteins 0.000 title description 12
- 102100025180 Mitogen-activated protein kinase kinase kinase 12 Human genes 0.000 title description 4
- 150000001875 compounds Chemical class 0.000 claims abstract description 142
- 238000000034 method Methods 0.000 claims abstract description 56
- 150000003839 salts Chemical class 0.000 claims abstract description 31
- 206010007559 Cardiac failure congestive Diseases 0.000 claims abstract description 24
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 9
- 239000003085 diluting agent Substances 0.000 claims abstract description 8
- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 4
- -1 amino, hydroxy Chemical group 0.000 claims description 288
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 50
- 229910052757 nitrogen Inorganic materials 0.000 claims description 48
- 125000000217 alkyl group Chemical group 0.000 claims description 39
- 125000000623 heterocyclic group Chemical group 0.000 claims description 39
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 37
- 125000001424 substituent group Chemical group 0.000 claims description 33
- 125000003118 aryl group Chemical group 0.000 claims description 27
- 206010019280 Heart failures Diseases 0.000 claims description 23
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 22
- 101100295738 Gallus gallus COR3 gene Proteins 0.000 claims description 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 11
- 239000001257 hydrogen Substances 0.000 claims description 11
- 229910052739 hydrogen Inorganic materials 0.000 claims description 11
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 9
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 9
- 229910052727 yttrium Inorganic materials 0.000 claims description 8
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- 125000005265 dialkylamine group Chemical group 0.000 claims description 7
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 6
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims description 5
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- 125000005059 halophenyl group Chemical group 0.000 claims description 4
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- XZGLNCKSNVGDNX-UHFFFAOYSA-N 5-methyl-2h-tetrazole Chemical compound CC=1N=NNN=1 XZGLNCKSNVGDNX-UHFFFAOYSA-N 0.000 claims description 2
- 125000004786 difluoromethoxy group Chemical group [H]C(F)(F)O* 0.000 claims description 2
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- 239000003937 drug carrier Substances 0.000 claims description 2
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- 238000000844 transformation Methods 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 125000004044 trifluoroacetyl group Chemical group FC(C(=O)*)(F)F 0.000 description 1
- 125000000025 triisopropylsilyl group Chemical group C(C)(C)[Si](C(C)C)(C(C)C)* 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 239000012588 trypsin Substances 0.000 description 1
- 241000701161 unidentified adenovirus Species 0.000 description 1
- 239000013598 vector Substances 0.000 description 1
- 229920002554 vinyl polymer Polymers 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 239000002023 wood Substances 0.000 description 1
- 229940071104 xylenesulfonate Drugs 0.000 description 1
- PVURAUIMVICLOH-UHFFFAOYSA-M zinc;cyclohexane;bromide Chemical compound Br[Zn+].C1CC[CH-]CC1 PVURAUIMVICLOH-UHFFFAOYSA-M 0.000 description 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
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Cardiology (AREA)
- Hospice & Palliative Care (AREA)
- Heart & Thoracic Surgery (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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La présente invention a trait à un composé de formule (I), ou à un sel pharmaceutiquement acceptable de celui-ci comportant une quantité efficace d'un composé de formule (I) en combinaison avec un support approprié, un diluant, ou un excipient, et des procédés de traitement de troubles physiologiques, notamment l'insuffisance cardiaque globale, comprenant l'administration à un patient d'une quantité efficace d'un composé de formule (I).
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42832202P | 2002-11-21 | 2002-11-21 | |
| US60/428,322 | 2002-11-21 | ||
| PCT/US2003/035036 WO2004048383A1 (fr) | 2002-11-21 | 2003-11-12 | Modulateurs de la kinase a lignee evolutive mixte |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2506799A1 true CA2506799A1 (fr) | 2004-06-10 |
Family
ID=32393381
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002506799A Abandoned CA2506799A1 (fr) | 2002-11-21 | 2003-11-12 | Modulateurs de la kinase a lignee evolutive mixte |
Country Status (5)
| Country | Link |
|---|---|
| EP (1) | EP1567528A1 (fr) |
| JP (1) | JP2006522735A (fr) |
| AU (1) | AU2003298611A1 (fr) |
| CA (1) | CA2506799A1 (fr) |
| WO (1) | WO2004048383A1 (fr) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA80571C2 (en) | 2002-11-22 | 2007-10-10 | Lilly Co Eli | Quinolinyl-pyrrolopyrazoles |
| CR9465A (es) * | 2005-03-25 | 2008-06-19 | Surface Logix Inc | Compuestos mejorados farmacocineticamente |
| EP1910370B1 (fr) * | 2005-07-22 | 2015-04-22 | Eli Lilly And Company | Pyrrolo [1,2-b] pyrazole monohydraté porteur d'une substitution pyridin quinoline en tant qu'inhibiteur du facteur de croissance tgf-bêta |
| US7919519B2 (en) | 2005-11-23 | 2011-04-05 | Epix Pharmaceuticals Inc. | S1P receptor modulating compounds and use thereof |
| EP1965807A4 (fr) * | 2005-11-23 | 2010-10-27 | Epix Delaware Inc | Composes modulateurs du recepteur s1p et utilisation associee |
| JP2009530389A (ja) | 2006-03-21 | 2009-08-27 | エピックス デラウェア, インコーポレイテッド | S1p受容体調節化合物及びその使用 |
| BRPI0713350B1 (pt) | 2006-06-26 | 2022-04-12 | Akebia Therapeutics Inc | Composto, e, composição |
| MX2009010060A (es) * | 2007-03-21 | 2010-01-20 | Epix Pharm Inc | Compuestos moduladores del receptor de esfingosin-1-fosfato y uso de los mismos. |
| ES2360929T3 (es) | 2007-09-20 | 2011-06-10 | Amgen Inc. | Derivados del ácido 1-(4-(4-bencilbenzamido)-bencil)azetidin-3-carboxílico y compuestos relacionados como moduladores del receptor s1p para el tratamiento de trastornos inmunitarios. |
| DE102009001438A1 (de) | 2009-03-10 | 2010-09-16 | Bayer Schering Pharma Aktiengesellschaft | Carbonylamino-substituierte Anilino-Pyrimidinderivate als Tyk-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| DE102009015070A1 (de) | 2009-03-30 | 2010-10-14 | Bayer Schering Pharma Aktiengesellschaft | Aminocabonylamino-substituierte Anilino-Pyrimidinderivate als Tyk-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel |
| EP2717870B1 (fr) | 2011-06-06 | 2017-09-27 | Akebia Therapeutics Inc. | Composition pour la stabilisation du facteur-2 alpha inductible par l'hypoxie utile pour le traitement du cancer |
| NO2686520T3 (fr) | 2011-06-06 | 2018-03-17 | ||
| SG10201910773VA (en) | 2013-06-13 | 2020-01-30 | Akebia Therapeutics Inc | Compositions and methods for treating anemia |
| AU2016209126A1 (en) | 2015-01-23 | 2017-08-10 | Akebia Therapeutics, Inc. | Solid forms of 2-(5-(3-fluorophenyl)-3-hydroxypicolinamido)acetic acid, compositions, and uses thereof |
| US11324734B2 (en) | 2015-04-01 | 2022-05-10 | Akebia Therapeutics, Inc. | Compositions and methods for treating anemia |
| ES2918924T3 (es) | 2015-04-01 | 2022-07-21 | Rigel Pharmaceuticals Inc | Inhibidores de TGF-beta |
| EP3492461B1 (fr) | 2016-07-29 | 2024-10-23 | Shanghai Yingli Pharmaceutical Co. Ltd. | Composé aromatique hétérocyclique azoté, son procédé de préparation, composition pharmaceutique à base de celui-ci et son application |
| CN110066276B (zh) | 2018-01-24 | 2020-09-18 | 上海璎黎药业有限公司 | 芳香杂环化合物、其中间体、制备方法、药物组合物和应用 |
| CN110066277B (zh) | 2018-01-24 | 2021-07-23 | 上海璎黎药业有限公司 | 芳香杂环取代烯烃化合物、其制备方法、药物组合物和应用 |
| EP3790863A1 (fr) | 2018-05-09 | 2021-03-17 | Akebia Therapeutics Inc. | Procédé de préparation d'acide 2-[[5-(3-chlorophényl)-3-hydroxypyridine-2-carbonyl] amino]acétique |
| CN114437082B (zh) * | 2020-11-06 | 2025-04-04 | 江苏先声药业有限公司 | 喹啉类化合物 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5356897A (en) * | 1991-09-09 | 1994-10-18 | Fujisawa Pharmaceutical Co., Ltd. | 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines |
| EP1397364B1 (fr) * | 2001-05-24 | 2007-07-25 | Eli Lilly And Company | Derives de pyrrole utilises comme agents pharmaceutiques |
-
2003
- 2003-11-12 CA CA002506799A patent/CA2506799A1/fr not_active Abandoned
- 2003-11-12 AU AU2003298611A patent/AU2003298611A1/en not_active Abandoned
- 2003-11-12 EP EP03796362A patent/EP1567528A1/fr not_active Withdrawn
- 2003-11-12 JP JP2004555371A patent/JP2006522735A/ja not_active Withdrawn
- 2003-11-12 WO PCT/US2003/035036 patent/WO2004048383A1/fr not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004048383A1 (fr) | 2004-06-10 |
| JP2006522735A (ja) | 2006-10-05 |
| EP1567528A1 (fr) | 2005-08-31 |
| AU2003298611A1 (en) | 2004-06-18 |
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