CN101801955B - 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 - Google Patents
作为akt蛋白激酶抑制剂的嘧啶基环戊烷 Download PDFInfo
- Publication number
- CN101801955B CN101801955B CN2008801058695A CN200880105869A CN101801955B CN 101801955 B CN101801955 B CN 101801955B CN 2008801058695 A CN2008801058695 A CN 2008801058695A CN 200880105869 A CN200880105869 A CN 200880105869A CN 101801955 B CN101801955 B CN 101801955B
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- China
- Prior art keywords
- dihydro
- cyclopenta
- piperazine
- pyrimidine
- ethyl ketone
- 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.)
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- 0 C*C(*)(CCC1)*C1C(*)C(N(CC1)CC(*)N1c1c(C(*)(*)CC2(*)*)c2ncn1)=O Chemical compound C*C(*)(CCC1)*C1C(*)C(N(CC1)CC(*)N1c1c(C(*)(*)CC2(*)*)c2ncn1)=O 0.000 description 2
- BFUXYUZDQJWVOS-GRDDELGYSA-N CC(CC1(F)F)C2=C1NC(C)N=C2N(CC1)CCN1C([C@H]([C@H]1NC(C)(C)CC1)c(cc1)ccc1Cl)=O Chemical compound CC(CC1(F)F)C2=C1NC(C)N=C2N(CC1)CCN1C([C@H]([C@H]1NC(C)(C)CC1)c(cc1)ccc1Cl)=O BFUXYUZDQJWVOS-GRDDELGYSA-N 0.000 description 1
- YVPFVJHORLYXKT-MONBJTKQSA-N C[C@H]1c2c(N(CC3)CCN3C([C@H]([C@H]3NCCCC3)c(cc3)ccc3Cl)=O)ncnc2CC1 Chemical compound C[C@H]1c2c(N(CC3)CCN3C([C@H]([C@H]3NCCCC3)c(cc3)ccc3Cl)=O)ncnc2CC1 YVPFVJHORLYXKT-MONBJTKQSA-N 0.000 description 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
- C07D403/02—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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- 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
- 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
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Communicable Diseases (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Psychology (AREA)
- Child & Adolescent Psychology (AREA)
- Virology (AREA)
- Emergency Medicine (AREA)
- Transplantation (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Ophthalmology & Optometry (AREA)
- Vascular Medicine (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94813807P | 2007-07-05 | 2007-07-05 | |
| US60/948,138 | 2007-07-05 | ||
| US2008808P | 2008-01-09 | 2008-01-09 | |
| US61/020,088 | 2008-01-09 | ||
| PCT/US2008/069144 WO2009006567A2 (en) | 2007-07-05 | 2008-07-03 | Pyrimidyl cyclopentanes as akt protein kinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310128477.3A Division CN103396409B (zh) | 2007-07-05 | 2008-07-03 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101801955A CN101801955A (zh) | 2010-08-11 |
| CN101801955B true CN101801955B (zh) | 2013-05-08 |
Family
ID=40076864
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2008801058695A Active CN101801955B (zh) | 2007-07-05 | 2008-07-03 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
| CN201310128477.3A Active CN103396409B (zh) | 2007-07-05 | 2008-07-03 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310128477.3A Active CN103396409B (zh) | 2007-07-05 | 2008-07-03 | 作为akt蛋白激酶抑制剂的嘧啶基环戊烷 |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8618097B2 (enExample) |
| EP (1) | EP2170863B1 (enExample) |
| JP (2) | JP5628028B2 (enExample) |
| KR (2) | KR20150089099A (enExample) |
| CN (2) | CN101801955B (enExample) |
| AR (1) | AR067413A1 (enExample) |
| AU (1) | AU2008272830B8 (enExample) |
| BR (1) | BRPI0813999A2 (enExample) |
| CA (1) | CA2692502C (enExample) |
| CO (1) | CO6251283A2 (enExample) |
| CR (1) | CR11229A (enExample) |
| EC (1) | ECSP109937A (enExample) |
| ES (1) | ES2551352T3 (enExample) |
| MA (1) | MA31679B1 (enExample) |
| NZ (1) | NZ582692A (enExample) |
| RU (1) | RU2486181C2 (enExample) |
| SG (1) | SG185274A1 (enExample) |
| TW (1) | TWI450720B (enExample) |
| WO (1) | WO2009006567A2 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2729424T3 (es) | 2006-09-20 | 2019-11-04 | Aerie Pharmaceuticals Inc | Inhibidores de Rho cinasa |
| US8455513B2 (en) | 2007-01-10 | 2013-06-04 | Aerie Pharmaceuticals, Inc. | 6-aminoisoquinoline compounds |
| US8846683B2 (en) | 2007-07-05 | 2014-09-30 | Array Biopharma, Inc. | Pyrimidyl cyclopentanes as Akt protein kinase inhibitors |
| US9409886B2 (en) | 2007-07-05 | 2016-08-09 | Array Biopharma Inc. | Pyrimidyl cyclopentanes as AKT protein kinase inhibitors |
| EP2242755B1 (en) | 2008-01-08 | 2012-09-12 | Array Biopharma, Inc. | Pyrrolopyridines as kinase inhibitors |
| WO2009089462A1 (en) | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | 5h-cyclopenta[d]pyrimidines as akt protein kinase inhibitors |
| CA2711692A1 (en) * | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentane as akt protein kinase inhibitor |
| WO2009089459A1 (en) | 2008-01-09 | 2009-07-16 | Array Biopharma Inc. | Hydroxylated pyrimidyl cyclopentanes as akt protein kinase inhibitors |
| JP5512545B2 (ja) * | 2008-01-09 | 2014-06-04 | アレイ バイオファーマ、インコーポレイテッド | Aktタンパク質キナーゼ阻害剤としてのピリミジルシクロペンタン類 |
| EP2242757B1 (en) | 2008-01-09 | 2012-08-01 | Array Biopharma, Inc. | Pyrazolopyridines as kinase inhibitors |
| US8450344B2 (en) | 2008-07-25 | 2013-05-28 | Aerie Pharmaceuticals, Inc. | Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds |
| CA2760562C (en) | 2009-05-01 | 2016-07-19 | Aerie Pharmaceuticals, Inc. | Dual mechanism inhibitors for the treatment of disease |
| KR20130058672A (ko) | 2010-04-16 | 2013-06-04 | 제넨테크, 인크. | PI3K/AKT 키나제 경로 억제제 효능에 대한 예측 바이오마커로서의 FOXO3a |
| RU2635193C2 (ru) | 2011-04-01 | 2017-11-09 | Дженентек, Инк. | Биомаркеры для прогнозирования чувствительности к противоопухолевой терапии |
| HUE051254T2 (hu) | 2012-05-17 | 2021-03-01 | Genentech Inc | Egy AKT-gátló pirimidin-ciklopentán vegyület amorf formája, annak kompozíciói és eljárásai |
| US9452990B2 (en) | 2012-06-20 | 2016-09-27 | Novartis Ag | Complement pathway modulators and uses thereof |
| CA2901126C (en) | 2013-02-25 | 2022-01-25 | Genentech, Inc. | Methods and compositions for detecting and treating drug resistant akt mutant |
| PT3811943T (pt) | 2013-03-15 | 2023-03-15 | Aerie Pharmaceuticals Inc | Composto para uso no tratamento de distúrbios oculares |
| JP6832946B2 (ja) * | 2015-11-17 | 2021-02-24 | アエリエ ファーマシューティカルズ インコーポレイテッド | キナーゼ阻害剤およびその中間体の調製方法 |
| US9643927B1 (en) | 2015-11-17 | 2017-05-09 | Aerie Pharmaceuticals, Inc. | Process for the preparation of kinase inhibitors and intermediates thereof |
| US10722484B2 (en) | 2016-03-09 | 2020-07-28 | K-Gen, Inc. | Methods of cancer treatment |
| CN109640966A (zh) | 2016-08-31 | 2019-04-16 | 爱瑞制药公司 | 眼用组合物 |
| EP3532464A4 (en) | 2016-10-28 | 2020-07-08 | Icahn School of Medicine at Mount Sinai | COMPOSITIONS AND METHODS FOR THE TREATMENT OF EZH2 MEDIATION CANCER |
| SG11201908179UA (en) | 2017-03-31 | 2019-10-30 | Aerie Pharmaceuticals Inc | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| AU2019231689A1 (en) * | 2018-03-06 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Serine threonine kinase (AKT) degradation / disruption compounds and methods of use |
| MX2020010420A (es) * | 2018-04-04 | 2020-12-11 | Arvinas Operations Inc | Moduladores de la proteólisis y métodos asociados de uso. |
| CA3104298A1 (en) | 2018-06-21 | 2019-12-26 | Icahn School Of Medicine At Mount Sinai | Wd40 repeat domain protein 5 (wdr5) degradation / disruption compounds and methods of use |
| WO2020056345A1 (en) | 2018-09-14 | 2020-03-19 | Aerie Pharmaceuticals, Inc. | Aryl cyclopropyl-amino-isoquinolinyl amide compounds |
| WO2020198526A2 (en) * | 2019-03-27 | 2020-10-01 | St. Jude Children's Research Hospital | Small molecule modulators of pank |
| CA3137916A1 (en) | 2019-05-06 | 2020-11-12 | Ichan School Of Medicine At Mount Sinai | Heterobifunctional compounds as degraders of hpk1 |
| US12103924B2 (en) | 2020-06-01 | 2024-10-01 | Icahn School Of Medicine At Mount Sinai | Mitogen-activated protein kinase kinase (MEK) degradation compounds and methods of use |
| WO2023109540A1 (zh) * | 2021-12-17 | 2023-06-22 | 中国医药研究开发中心有限公司 | 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途 |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and uses related thereto |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040009968A1 (en) * | 2002-01-25 | 2004-01-15 | Hayley Binch | Indazole compounds useful as protein kinase inhibitors |
| EP1803710A1 (en) * | 2004-10-20 | 2007-07-04 | Astellas Pharma Inc. | Pyrimidine derivative condensed with non-aromatic ring |
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