EA201000325A1 - Производные 2-гетероариламинопиримидина в качестве ингибиторов киназ - Google Patents
Производные 2-гетероариламинопиримидина в качестве ингибиторов киназInfo
- Publication number
- EA201000325A1 EA201000325A1 EA201000325A EA201000325A EA201000325A1 EA 201000325 A1 EA201000325 A1 EA 201000325A1 EA 201000325 A EA201000325 A EA 201000325A EA 201000325 A EA201000325 A EA 201000325A EA 201000325 A1 EA201000325 A1 EA 201000325A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- raf
- compounds
- abl
- ameliorate
- treat
- Prior art date
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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
- C07D401/02—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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
- A61P9/12—Antihypertensives
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
В настоящем изобретении предлагаются соединения формулы (I)и их фармацевтические композиции, которые используют в качестве ингибиторов протеинкиназ, а также способы применения указанных соединений для лечения, снижения интенсивности симптомов или профилактики состояния, связанного с аномальной или разрегулированной активностью киназы. В некоторых вариантах осуществления настоящего изобретения предлагаются способы применения указанных соединений для лечения, снижения интенсивности симптомов или профилактики заболеваний или нарушений, при которых наблюдается аномальная активность киназ c-kit, PDGFRα, PDGFRβ, CSF1R, Abl, BCR-Abl, CSK, JNK1, JNK2, p38, p70S6K, TGFβ, SRC, EGFR, trkB, FGFR3, Fes, Lck, Syk, RAF, MKK4, MKK6, SAPK2β, BRK, Fms, KDR, c-raf или b-raf.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US95724007P | 2007-08-22 | 2007-08-22 | |
PCT/US2008/073438 WO2009026204A1 (en) | 2007-08-22 | 2008-08-18 | 2-heteroarylamino-pyrimidine derivatives as kinase inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201000325A1 true EA201000325A1 (ru) | 2010-10-29 |
EA017392B1 EA017392B1 (ru) | 2012-12-28 |
Family
ID=39930713
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201000325A EA017392B1 (ru) | 2007-08-22 | 2008-08-18 | Производные 2-гетероариламинопиримидина в качестве ингибиторов киназ |
Country Status (13)
Country | Link |
---|---|
US (1) | US8288540B2 (ru) |
EP (1) | EP2190836B1 (ru) |
JP (1) | JP5303557B2 (ru) |
KR (1) | KR101171488B1 (ru) |
CN (1) | CN101784539A (ru) |
AT (1) | ATE520682T1 (ru) |
AU (1) | AU2008289135B2 (ru) |
BR (1) | BRPI0815572A2 (ru) |
CA (1) | CA2697077C (ru) |
EA (1) | EA017392B1 (ru) |
ES (1) | ES2368876T3 (ru) |
MX (1) | MX2010002005A (ru) |
WO (1) | WO2009026204A1 (ru) |
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CA2687931C (en) | 2007-05-31 | 2016-05-24 | Boehringer Ingelheim International Gmbh | Ccr2 receptor antagonists and uses thereof |
KR20120107538A (ko) | 2007-08-22 | 2012-10-02 | 아이알엠 엘엘씨 | 키나제 억제제로서의 5-(4-(할로알콕시)페닐)피리미딘-2-아민 화합물 및 조성물 |
PE20120061A1 (es) | 2008-12-19 | 2012-02-19 | Boehringer Ingelheim Int | Derivados de pirimidina como antagonistas del receptor ccr2 |
PT3091012T (pt) | 2009-12-17 | 2018-06-27 | Centrexion Therapeutics Corp | Antagonistas do receptor ccr2 e suas utilizações |
JP2013526507A (ja) | 2010-05-12 | 2013-06-24 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規ccr2受容体アンタゴニスト、その製造方法及び薬物としてのその使用 |
US8946218B2 (en) | 2010-05-12 | 2015-02-03 | Boehringer Ingelheim International Gmbh | CCR2 receptor antagonists, method for producing the same, and use thereof as medicaments |
US8841313B2 (en) | 2010-05-17 | 2014-09-23 | Boehringer Ingelheim International Gmbh | CCR2 antagonists and uses thereof |
JP5636094B2 (ja) | 2010-05-25 | 2014-12-03 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | Ccr2受容体アンタゴニスト |
EP2576538B1 (en) * | 2010-06-01 | 2015-10-28 | Boehringer Ingelheim International GmbH | New CCR2 antagonists |
AU2011283684B2 (en) | 2010-07-29 | 2015-08-27 | Rigel Pharmaceuticals, Inc. | AMPK-activating heterocyclic compounds and methods for using the same |
JP5786258B2 (ja) | 2011-07-15 | 2015-09-30 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規かつ選択的なccr2拮抗薬 |
BR112014001714A2 (pt) | 2011-07-26 | 2017-02-14 | Gruenenthal Gmbh | derivados de carboxamida e ureia aromáticos bicíclicos substituídos como ligantes de receptor vaniloide |
JO3405B1 (ar) | 2013-01-09 | 2019-10-20 | Regeneron Pharma | الأجسام المضادة لمضاد مستقبل عامل النمو المشتق من الصفائح الدموية - بيتا واستخداماتها |
EP3007689B1 (en) | 2013-01-10 | 2018-03-07 | Pulmokine, Inc. | Non-selective kinase inhibitors |
EP3036262A4 (en) | 2013-08-22 | 2017-03-01 | Acceleron Pharma Inc. | Tgf-beta receptor type ii variants and uses thereof |
CN104458675A (zh) * | 2013-09-12 | 2015-03-25 | 中国药科大学 | 一种筛选干细胞因子受体激酶抑制剂高通量筛选方法 |
CN104458674A (zh) * | 2013-09-12 | 2015-03-25 | 中国药科大学 | 一种筛选血管内皮生长因子1激酶抑制剂高通量筛选方法 |
CN106132403B (zh) | 2013-10-11 | 2020-04-28 | 普尔莫凯恩股份有限公司 | 喷雾干燥制剂 |
EP3685848B1 (en) | 2013-11-21 | 2021-09-15 | The Brigham and Women's Hospital, Inc. | Compositions and methods for treating pulmonary hypertension |
CN106794233B (zh) | 2014-08-01 | 2021-11-12 | 布里格姆及妇女医院股份有限公司 | 与肺动脉高压的治疗有关的组合物和方法 |
MX2017017177A (es) | 2015-07-02 | 2018-11-09 | Centrexion Therapeutics Corp | Citrato de (4-((3r,4r)-3-metoxitetrahidro-piran-4-ilamino)piperidi n-1-il)(5-metil-6-(((2r,6s)-6-(p-tolil)tetrahidro-2h-piran-2-il)m etilamino)pirimidin-4il) metanona. |
KR20180035884A (ko) | 2015-08-04 | 2018-04-06 | 악셀레론 파마 인코포레이티드 | 골수증식성 장애를 치료하기 위한 방법 |
WO2017066193A1 (en) | 2015-10-15 | 2017-04-20 | Princeton Drug Discovery, Llc | Novel inhibitors of protein kinases |
EP3481753B1 (en) | 2016-07-06 | 2020-11-04 | Tomra Systems ASA | Device and method for singulation of used beverage or food containers |
CA3041679A1 (en) | 2016-10-27 | 2018-05-03 | Lawrence S. ZISMAN | Combination therapy for treating pulmonary hypertension |
KR20240023201A (ko) | 2017-05-04 | 2024-02-20 | 악셀레론 파마 인코포레이티드 | Tgf-베타 수용체 유형 ii 융합 단백질 및 이의 용도 |
WO2018214866A1 (zh) * | 2017-05-24 | 2018-11-29 | 上海和誉生物医药科技有限公司 | 一种氮杂芳基衍生物、其制备方法和在药学上的应用 |
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EP0164204A1 (en) | 1984-05-12 | 1985-12-11 | FISONS plc | Novel pharmaceutically useful pyrimidines |
CA2148931A1 (en) | 1993-10-01 | 1995-04-13 | Jurg Zimmermann | Pyrimidineamine derivatives and processes for the preparation thereof |
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GB0222514D0 (en) | 2002-09-27 | 2002-11-06 | Novartis Ag | Organic compounds |
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KR20070084067A (ko) | 2004-10-13 | 2007-08-24 | 와이어쓰 | N-벤젠설포닐 치환 아닐리노-피리미딘 동족체 |
AU2005325676A1 (en) | 2004-12-23 | 2006-08-03 | Deciphera Pharmaceuticals, Llc | Anti-inflammatory medicaments |
EP1835934A4 (en) | 2004-12-23 | 2010-07-28 | Deciphera Pharmaceuticals Llc | ENZYME MODULATORS AND TREATMENTS |
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KR100674813B1 (ko) | 2005-08-05 | 2007-01-29 | 일양약품주식회사 | N-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 |
AU2006297089B2 (en) * | 2005-09-27 | 2012-05-03 | Irm Llc | Diarylamine-containing compounds and compositions, and their use as modulators of c-kit receptors |
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BRPI0718677A2 (pt) | 2006-11-03 | 2013-11-26 | Irm Llc | Compostos e composições como inibidores de quinases proteicas |
WO2008137794A1 (en) | 2007-05-04 | 2008-11-13 | Irm Llc | Compounds and compositions as c-kit and pdgfr kinase inhibitors |
ATE544761T1 (de) | 2007-05-04 | 2012-02-15 | Irm Llc | Pyrimidinderivate und zusammensetzungen als c-kit-und pdgfr-kinasehemmer |
KR20120107538A (ko) | 2007-08-22 | 2012-10-02 | 아이알엠 엘엘씨 | 키나제 억제제로서의 5-(4-(할로알콕시)페닐)피리미딘-2-아민 화합물 및 조성물 |
-
2008
- 2008-08-18 BR BRPI0815572-0A2A patent/BRPI0815572A2/pt not_active IP Right Cessation
- 2008-08-18 WO PCT/US2008/073438 patent/WO2009026204A1/en active Application Filing
- 2008-08-18 CA CA2697077A patent/CA2697077C/en not_active Expired - Fee Related
- 2008-08-18 KR KR1020107006078A patent/KR101171488B1/ko not_active IP Right Cessation
- 2008-08-18 AU AU2008289135A patent/AU2008289135B2/en not_active Ceased
- 2008-08-18 US US12/673,948 patent/US8288540B2/en not_active Expired - Fee Related
- 2008-08-18 MX MX2010002005A patent/MX2010002005A/es active IP Right Grant
- 2008-08-18 EP EP08798064A patent/EP2190836B1/en not_active Not-in-force
- 2008-08-18 CN CN200880103912A patent/CN101784539A/zh active Pending
- 2008-08-18 ES ES08798064T patent/ES2368876T3/es active Active
- 2008-08-18 AT AT08798064T patent/ATE520682T1/de not_active IP Right Cessation
- 2008-08-18 EA EA201000325A patent/EA017392B1/ru not_active IP Right Cessation
- 2008-08-18 JP JP2010521961A patent/JP5303557B2/ja not_active Expired - Fee Related
Also Published As
Publication number | Publication date |
---|---|
MX2010002005A (es) | 2010-03-11 |
AU2008289135B2 (en) | 2012-02-23 |
AU2008289135A1 (en) | 2009-02-26 |
WO2009026204A1 (en) | 2009-02-26 |
EP2190836A1 (en) | 2010-06-02 |
CN101784539A (zh) | 2010-07-21 |
US8288540B2 (en) | 2012-10-16 |
EP2190836B1 (en) | 2011-08-17 |
US20110053952A1 (en) | 2011-03-03 |
JP5303557B2 (ja) | 2013-10-02 |
KR101171488B1 (ko) | 2012-08-07 |
ATE520682T1 (de) | 2011-09-15 |
CA2697077A1 (en) | 2009-02-26 |
KR20100050554A (ko) | 2010-05-13 |
CA2697077C (en) | 2012-10-16 |
BRPI0815572A2 (pt) | 2015-02-18 |
JP2010536865A (ja) | 2010-12-02 |
EA017392B1 (ru) | 2012-12-28 |
ES2368876T3 (es) | 2011-11-23 |
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