CN103958502B - 作为丝氨酸/苏氨酸激酶抑制剂的喹唑啉化合物 - Google Patents
作为丝氨酸/苏氨酸激酶抑制剂的喹唑啉化合物 Download PDFInfo
- Publication number
- CN103958502B CN103958502B CN201280049268.3A CN201280049268A CN103958502B CN 103958502 B CN103958502 B CN 103958502B CN 201280049268 A CN201280049268 A CN 201280049268A CN 103958502 B CN103958502 B CN 103958502B
- Authority
- CN
- China
- Prior art keywords
- methyl
- fluoro
- quinazoline
- phenyl
- ylamino
- 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.)
- Active
Links
- 0 *C([C@@]1N(*)CCC1)=O Chemical compound *C([C@@]1N(*)CCC1)=O 0.000 description 3
- JKGZYEBEPLHXOI-UHFFFAOYSA-N CC(COCC1)C1OC Chemical compound CC(COCC1)C1OC JKGZYEBEPLHXOI-UHFFFAOYSA-N 0.000 description 1
- ILKLKYDTEBRGSE-GSUNZCPGSA-N CN1[C@@H](C[AlH2])CCC1 Chemical compound CN1[C@@H](C[AlH2])CCC1 ILKLKYDTEBRGSE-GSUNZCPGSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- C07D401/14—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
- C07D403/14—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
-
- 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
-
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/08—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161515165P | 2011-08-04 | 2011-08-04 | |
| US61/515,165 | 2011-08-04 | ||
| PCT/US2012/049551 WO2013020062A1 (en) | 2011-08-04 | 2012-08-03 | Quinazoline compounds as serine/threonine kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103958502A CN103958502A (zh) | 2014-07-30 |
| CN103958502B true CN103958502B (zh) | 2016-02-10 |
Family
ID=47003195
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280049268.3A Active CN103958502B (zh) | 2011-08-04 | 2012-08-03 | 作为丝氨酸/苏氨酸激酶抑制剂的喹唑啉化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9187462B2 (https=) |
| EP (1) | EP2739618B1 (https=) |
| JP (1) | JP6097289B2 (https=) |
| KR (1) | KR101979042B1 (https=) |
| CN (1) | CN103958502B (https=) |
| BR (1) | BR112014002675A2 (https=) |
| CA (1) | CA2844058A1 (https=) |
| ES (1) | ES2552989T3 (https=) |
| MX (1) | MX340756B (https=) |
| RU (1) | RU2014108140A (https=) |
| WO (1) | WO2013020062A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103635472B (zh) | 2011-02-28 | 2018-01-12 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| JP6097289B2 (ja) | 2011-08-04 | 2017-03-15 | アレイ バイオファーマ、インコーポレイテッド | セリン／スレオニンキナーゼインヒビターとしてのキナゾリン化合物 |
| HUE053994T2 (hu) | 2012-03-01 | 2021-08-30 | Array Biopharma Inc | Szerin/treonin kináz inhibitorok |
| AR092253A1 (es) | 2012-08-27 | 2015-04-08 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa |
| JP2015533151A (ja) | 2012-10-16 | 2015-11-19 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | セリン／スレオニンキナーゼ阻害剤 |
| CN103254142B (zh) * | 2013-04-26 | 2015-10-28 | 浙江工业大学 | 4-[4-(2-取代氨基乙酰氨基)苯胺基]喹唑啉类衍生物及制备和应用 |
| US9532987B2 (en) | 2013-09-05 | 2017-01-03 | Genentech, Inc. | Use of a combination of a MEK inhibitor and an ERK inhibitor for treatment of hyperproliferative diseases |
| EP3077401B1 (en) | 2013-12-06 | 2018-04-18 | Genentech, Inc. | Serine/threonine kinase inhibitors |
| JP6642942B2 (ja) * | 2013-12-30 | 2020-02-12 | アレイ バイオファーマ、インコーポレイテッド | セリン／トレオニンキナーゼ阻害剤 |
| KR102379517B1 (ko) * | 2013-12-30 | 2022-03-25 | 제넨테크, 인크. | 세린/트레오닌 키나아제 억제제 |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| WO2017180581A1 (en) | 2016-04-15 | 2017-10-19 | Genentech, Inc. | Diagnostic and therapeutic methods for cancer |
| AU2018329925B2 (en) | 2017-09-08 | 2025-05-29 | F. Hoffmann-La Roche Ag | Diagnostic and therapeutic methods for cancer |
| EP3752200A1 (en) | 2018-02-13 | 2020-12-23 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| EP3787629A4 (en) | 2018-05-02 | 2022-01-05 | Kinnate Biopharma Inc. | CYCLINE-DEPENDENT KINASE INHIBITORS |
| SG11202013175SA (en) | 2018-06-29 | 2021-01-28 | Kinnate Biopharma Inc | Inhibitors of cyclin-dependent kinases |
| TWI721623B (zh) | 2018-10-31 | 2021-03-11 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| TW202136261A (zh) | 2018-10-31 | 2021-10-01 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| US11453681B2 (en) | 2019-05-23 | 2022-09-27 | Gilead Sciences, Inc. | Substituted eneoxindoles and uses thereof |
| EP4048261A4 (en) | 2019-10-25 | 2023-11-22 | Merck Sharp & Dohme LLC | N-(HETEROARYL)-QUINAZOLINE-2-AMINE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF |
| CN115448864B (zh) * | 2022-08-26 | 2023-12-22 | 上海方予健康医药科技有限公司 | 3-氟-3-（1-羟乙基）吡咯烷-1-羧酸叔丁酯的制备方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007125405A2 (en) * | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| US20090246198A1 (en) * | 2008-03-31 | 2009-10-01 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors and methods of use thereof |
Family Cites Families (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPH08503971A (ja) | 1993-10-01 | 1996-04-30 | チバ−ガイギー アクチェンゲゼルシャフト | ピリミジンアミン誘導体及びその調製のための方法 |
| WO1995009851A1 (en) | 1993-10-01 | 1995-04-13 | Ciba-Geigy Ag | Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof |
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| IL130181A0 (en) | 1996-12-05 | 2000-06-01 | Amgen Inc | Substituted pyrimidone and pyridone compounds and methods of use |
| US6602872B1 (en) | 1999-12-13 | 2003-08-05 | Merck & Co., Inc. | Substituted pyridazines having cytokine inhibitory activity |
| JP4064671B2 (ja) | 2000-02-25 | 2008-03-19 | エフ．ホフマン−ラ ロシュ アーゲー | アデノシン受容体モジュレーター |
| KR20070058022A (ko) | 2000-04-26 | 2007-06-07 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 배변을 촉진하는 의약 조성물 |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| CA2485166A1 (en) | 2002-05-21 | 2003-12-04 | Amgen Inc. | Substituted pyrimidinone and pyridinone compounds |
| US7208498B2 (en) | 2002-07-15 | 2007-04-24 | Merck & Co., Inc. | Piperidino pyrimidine dipeptidyl peptidase inhibitors for the treatment of diabetes |
| TW200533357A (en) | 2004-01-08 | 2005-10-16 | Millennium Pharm Inc | 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases |
| GEP20084360B (en) * | 2004-02-04 | 2008-04-29 | Pfizer Prod Inc | Substituted quinoline compounds |
| WO2005099711A1 (en) | 2004-04-13 | 2005-10-27 | Icagen, Inc. | Polycyclic pyrimidines as potassium ion channel modulators |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| JP2008510766A (ja) | 2004-08-27 | 2008-04-10 | ゲーペーツェー ビオテック アーゲー | ピリミジン誘導体 |
| GB0420722D0 (en) | 2004-09-17 | 2004-10-20 | Addex Pharmaceuticals Sa | Novel allosteric modulators |
| GB0428514D0 (en) | 2004-12-31 | 2005-02-09 | Prosidion Ltd | Compounds |
| CA2606288A1 (en) | 2005-04-18 | 2006-10-26 | Neurogen Corporation | Subtituted heteroaryl cb1 antagonists |
| US7572809B2 (en) | 2005-12-19 | 2009-08-11 | Hoffmann-La Roche Inc. | Isoquinoline aminopyrazole derivatives |
| MX2008010635A (es) | 2006-02-16 | 2008-10-28 | Schering Corp | Derivados de pirrolidina como inhibidores de cinasa regulada por señales extracelulares. |
| DE102006035202A1 (de) | 2006-07-29 | 2008-01-31 | Lanxess Deutschland Gmbh | Konservierungsmittel auf Basis von Carbonsäureanhydriden |
| US20100292205A1 (en) | 2006-08-23 | 2010-11-18 | Pfizer Inc. | Pyrimidone Compounds As GSK-3 Inhibitors |
| WO2008039882A1 (en) | 2006-09-30 | 2008-04-03 | Sanofi-Aventis U.S. Llc | A combination of niacin and a prostaglandin d2 receptor antagonist |
| CA2672518A1 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Organic compounds and their uses |
| US8530480B2 (en) | 2007-09-04 | 2013-09-10 | The Scripps Research Institute | Substituted pyrimidinyl-amines as protein kinase inhibitors |
| CN101902912A (zh) | 2007-11-06 | 2010-12-01 | 纳幕尔杜邦公司 | 杀真菌杂环胺 |
| TWI546290B (zh) | 2008-06-27 | 2016-08-21 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| EP2307379A2 (en) | 2008-06-27 | 2011-04-13 | Novartis AG | Organic compounds |
| PT2370413E (pt) | 2008-12-08 | 2015-10-23 | Arena Pharm Inc | Moduladores do recetor da prostaciclina (pgi2) úteis para o tratamento de distúrbios relacionados com o mesmo |
| CN103635472B (zh) | 2011-02-28 | 2018-01-12 | 阵列生物制药公司 | 丝氨酸/苏氨酸激酶抑制剂 |
| JP6097289B2 (ja) | 2011-08-04 | 2017-03-15 | アレイ バイオファーマ、インコーポレイテッド | セリン／スレオニンキナーゼインヒビターとしてのキナゾリン化合物 |
| HUE053994T2 (hu) | 2012-03-01 | 2021-08-30 | Array Biopharma Inc | Szerin/treonin kináz inhibitorok |
| AR092253A1 (es) | 2012-08-27 | 2015-04-08 | Array Biopharma Inc | Inhibidores de serina/treonina cinasa |
-
2012
- 2012-08-03 JP JP2014524111A patent/JP6097289B2/ja active Active
- 2012-08-03 KR KR1020147005731A patent/KR101979042B1/ko not_active Expired - Fee Related
- 2012-08-03 MX MX2014001389A patent/MX340756B/es active IP Right Grant
- 2012-08-03 US US14/237,143 patent/US9187462B2/en active Active
- 2012-08-03 EP EP12769775.3A patent/EP2739618B1/en active Active
- 2012-08-03 RU RU2014108140/04A patent/RU2014108140A/ru not_active Application Discontinuation
- 2012-08-03 WO PCT/US2012/049551 patent/WO2013020062A1/en not_active Ceased
- 2012-08-03 CN CN201280049268.3A patent/CN103958502B/zh active Active
- 2012-08-03 BR BR112014002675A patent/BR112014002675A2/pt not_active IP Right Cessation
- 2012-08-03 ES ES12769775.3T patent/ES2552989T3/es active Active
- 2012-08-03 CA CA2844058A patent/CA2844058A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007125405A2 (en) * | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| US20090246198A1 (en) * | 2008-03-31 | 2009-10-01 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors and methods of use thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| MX340756B (es) | 2016-07-25 |
| MX2014001389A (es) | 2014-11-13 |
| HK1199248A1 (zh) | 2015-06-26 |
| EP2739618B1 (en) | 2015-09-16 |
| CA2844058A1 (en) | 2013-02-07 |
| RU2014108140A (ru) | 2015-09-10 |
| JP2014521696A (ja) | 2014-08-28 |
| WO2013020062A1 (en) | 2013-02-07 |
| BR112014002675A2 (pt) | 2017-02-21 |
| HK1199021A1 (zh) | 2015-06-19 |
| CN103958502A (zh) | 2014-07-30 |
| KR20140062057A (ko) | 2014-05-22 |
| JP6097289B2 (ja) | 2017-03-15 |
| KR101979042B1 (ko) | 2019-05-15 |
| EP2739618A1 (en) | 2014-06-11 |
| US9187462B2 (en) | 2015-11-17 |
| US20150087664A1 (en) | 2015-03-26 |
| ES2552989T3 (es) | 2015-12-03 |
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