JP6085866B2 - セリン/トレオニンキナーゼインヒビター - Google Patents
セリン/トレオニンキナーゼインヒビター Download PDFInfo
- Publication number
- JP6085866B2 JP6085866B2 JP2013556817A JP2013556817A JP6085866B2 JP 6085866 B2 JP6085866 B2 JP 6085866B2 JP 2013556817 A JP2013556817 A JP 2013556817A JP 2013556817 A JP2013556817 A JP 2013556817A JP 6085866 B2 JP6085866 B2 JP 6085866B2
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- phenyl
- optionally substituted
- cancer
- hydrogen
- 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
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/052—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161447587P | 2011-02-28 | 2011-02-28 | |
| US61/447,587 | 2011-02-28 | ||
| PCT/US2012/027009 WO2012118850A1 (en) | 2011-02-28 | 2012-02-28 | Serine/threonine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014506930A JP2014506930A (ja) | 2014-03-20 |
| JP2014506930A5 JP2014506930A5 (enExample) | 2015-04-02 |
| JP6085866B2 true JP6085866B2 (ja) | 2017-03-01 |
Family
ID=45852719
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013556817A Active JP6085866B2 (ja) | 2011-02-28 | 2012-02-28 | セリン/トレオニンキナーゼインヒビター |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9133187B2 (enExample) |
| EP (1) | EP2681215B1 (enExample) |
| JP (1) | JP6085866B2 (enExample) |
| KR (1) | KR101961500B1 (enExample) |
| CN (1) | CN103635472B (enExample) |
| BR (1) | BR112013021896A2 (enExample) |
| CA (1) | CA2828478C (enExample) |
| ES (1) | ES2543050T3 (enExample) |
| MX (1) | MX339873B (enExample) |
| RU (1) | RU2013143839A (enExample) |
| WO (1) | WO2012118850A1 (enExample) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101961500B1 (ko) | 2011-02-28 | 2019-03-22 | 어레이 바이오파마 인크. | 세린/트레오닌 키나제 억제제 |
| CA2839699A1 (en) | 2011-06-24 | 2012-12-27 | Amgen Inc. | Trpm8 antagonists and their use in treatments |
| AU2012272898A1 (en) | 2011-06-24 | 2013-04-11 | Amgen Inc. | TRPM8 antagonists and their use in treatments |
| RU2014108140A (ru) | 2011-08-04 | 2015-09-10 | Эррэй Биофарма Инк. | Соединение на основе хинозолина в качестве ингибиторов серен-треониновых киназ |
| JP6089045B2 (ja) * | 2011-12-27 | 2017-03-01 | バイオ−ファーム ソリューションズ カンパニー リミテッド | 痛みの緩和または治療に使用するためのフェニルカルバメート化合物 |
| UA116774C2 (uk) | 2012-03-01 | 2018-05-10 | Еррей Біофарма Інк. | Інгібітори серин/треонінкінази |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| KR20150047597A (ko) | 2012-08-27 | 2015-05-04 | 어레이 바이오파마 인크. | 과증식성 질환의 치료를 위한 세린/트레오닌 키나아제 억제제 |
| BR112015005982A2 (pt) | 2012-09-19 | 2017-07-04 | Novartis Ag | di-hidropirrolidino-pirimidinas como inibidores de quinase |
| RU2015114936A (ru) | 2012-10-16 | 2016-12-10 | Ф. Хоффманн-Ля Рош Аг | Ингибиторы серин/треонинкиназы |
| JPWO2015012328A1 (ja) * | 2013-07-24 | 2017-03-02 | 武田薬品工業株式会社 | 複素環化合物 |
| 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 |
| JP6449293B2 (ja) | 2013-12-06 | 2019-01-09 | ジェネンテック, 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 |
| 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 |
| BR112016015235A2 (pt) | 2013-12-30 | 2017-08-08 | Genentech Inc | Composto, composição farmacêutica, método de inibição da atividade da proteína quinase erk e método de tratamento |
| CN109072311A (zh) | 2016-04-15 | 2018-12-21 | 豪夫迈·罗氏有限公司 | 用于癌症的诊断和治疗方法 |
| MX382339B (es) * | 2016-05-18 | 2025-03-13 | Mirati Therapeutics Inc | Inhibidores g12c de kras. |
| CN111373055B (zh) | 2017-09-08 | 2024-07-23 | 豪夫迈·罗氏有限公司 | 用于癌症的诊断和治疗方法 |
| ES2967094T3 (es) | 2017-09-29 | 2024-04-26 | Mitsubishi Tanabe Pharma Corp | Compuesto de pirrolidina ópticamente activo y procedimiento de producción del mismo |
| US10947234B2 (en) | 2017-11-08 | 2021-03-16 | Merck Sharp & Dohme Corp. | PRMT5 inhibitors |
| US20210008047A1 (en) | 2018-02-13 | 2021-01-14 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| WO2020192750A1 (zh) | 2019-03-28 | 2020-10-01 | 江苏恒瑞医药股份有限公司 | 噻吩并杂环类衍生物、其制备方法及其在医药上的应用 |
| BR112021018924A2 (pt) | 2019-03-29 | 2022-02-01 | Jiangsu Hengrui Medicine Co | Derivado de heterocíclico pirrol, método de preparação do mesmo e aplicação do mesmo em medicamento |
| CN113825757B (zh) | 2019-05-24 | 2023-10-20 | 江苏恒瑞医药股份有限公司 | 取代的稠合双环类衍生物、其制备方法及其在医药上的应用 |
| WO2020238791A1 (zh) * | 2019-05-24 | 2020-12-03 | 江苏恒瑞医药股份有限公司 | 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| CN111170929A (zh) * | 2019-12-12 | 2020-05-19 | 北京达因高科儿童药物研究院有限公司 | 一种由末端烯烃制备β-氨基醇的方法 |
| ES3033417T3 (en) * | 2020-09-25 | 2025-08-04 | Janssen Pharmaceutica Nv | Cyclin-dependent kinase 7 (cdk7) non-covalent inhibitors |
| CN116437915B (zh) | 2020-09-29 | 2025-03-18 | 江苏恒瑞医药股份有限公司 | 一种吡咯并杂环类衍生物的晶型及其制备方法 |
| CN115040522B (zh) * | 2022-06-30 | 2024-02-06 | 牡丹江医学院 | 一种用于治疗肺癌的药物及其制备方法 |
| KR20250091232A (ko) * | 2022-10-25 | 2025-06-20 | 투오지에 바이오텍 (상하이) 컴퍼니 리미티드 | 피페리디노피리미딘계 유도체, 이의 제조 방법 및 이의 의학적 응용 |
| IT202200024963A1 (it) * | 2022-12-05 | 2024-06-05 | Angelini Pharma S P A | Composti attivatori dei canali potassio Kv7.2/Kv7.3 |
| TW202535869A (zh) * | 2023-10-23 | 2025-09-16 | 大陸商上海拓界生物醫藥科技有限公司 | 一種含有噻唑基的哌啶并嘧啶類衍生物、其製備方法及其醫藥上的應用 |
| WO2025223512A1 (zh) * | 2024-04-24 | 2025-10-30 | 江苏恒瑞医药股份有限公司 | 一种二氢吡啶并嘧啶衍生物的可药用盐、结晶形式及用途 |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5705502A (en) | 1993-10-01 | 1998-01-06 | Novartis Corporation | Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof |
| WO1995009847A1 (en) | 1993-10-01 | 1995-04-13 | Ciba-Geigy Ag | 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 |
| BR9713863A (pt) | 1996-12-05 | 2000-03-14 | Amgen Inc | Composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, processos de profilaxia ou tratamento, para abaixar as concentrações no plasma, para diminuir a produção de prostaglandinas, e, para diminuir a atividade de enzima ciclooxigenase |
| US6602872B1 (en) | 1999-12-13 | 2003-08-05 | Merck & Co., Inc. | Substituted pyridazines having cytokine inhibitory activity |
| EP1261327B1 (en) | 2000-02-25 | 2005-04-27 | F.Hoffmann-La Roche Ag | Adenosine receptor modulators |
| 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 |
| WO2003099808A1 (en) | 2002-05-21 | 2003-12-04 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| ATE451369T1 (de) | 2002-07-15 | 2009-12-15 | Merck & Co Inc | Piperidinopyrimidindipeptidylpeptidaseinhibitor n zur behandlung von diabetes |
| US7419978B2 (en) * | 2003-10-22 | 2008-09-02 | Bristol-Myers Squibb Company | Phenyl-aniline substituted bicyclic compounds useful as kinase inhibitors |
| 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 |
| AU2005232745A1 (en) | 2004-04-13 | 2005-10-27 | Astellas Pharma Inc. | Polycyclic pyrimidines as potassium ion channel modulators |
| PE20060426A1 (es) | 2004-06-02 | 2006-06-28 | Schering Corp | DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa |
| US7429604B2 (en) | 2004-06-15 | 2008-09-30 | Bristol Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| WO2006021458A2 (en) | 2004-08-27 | 2006-03-02 | Gpc Biotech Ag | Pyrimidine derivatives |
| 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 |
| EP1871762A2 (en) | 2005-04-18 | 2008-01-02 | Neurogen Corporation | Subtituted heteroaryl cb1 antagonists |
| WO2007028022A2 (en) * | 2005-09-01 | 2007-03-08 | Renovis, Inc. | Novel compounds as p2x7 modulators and uses thereof |
| US7572809B2 (en) | 2005-12-19 | 2009-08-11 | Hoffmann-La Roche Inc. | Isoquinoline aminopyrazole derivatives |
| ATE485268T1 (de) | 2006-02-16 | 2010-11-15 | Schering Corp | Pyrrolidin-derivate als erk-hemmer |
| WO2007125405A2 (en) | 2006-05-01 | 2007-11-08 | Pfizer Products Inc. | Substituted 2-amino-fused heterocyclic compounds |
| 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 |
| US7897762B2 (en) * | 2006-09-14 | 2011-03-01 | Deciphera Pharmaceuticals, Llc | Kinase inhibitors useful for the treatment of proliferative diseases |
| WO2008039882A1 (en) | 2006-09-30 | 2008-04-03 | Sanofi-Aventis U.S. Llc | A combination of niacin and a prostaglandin d2 receptor antagonist |
| EP2094682A2 (en) | 2006-12-22 | 2009-09-02 | Novartis AG | Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections |
| US8063066B2 (en) * | 2007-03-19 | 2011-11-22 | Takeda Pharmaceutical Company Limited | MAPK/ERK kinase inhibitors |
| WO2009011904A1 (en) * | 2007-07-19 | 2009-01-22 | Renovis, Inc. | Compounds useful as faah modulators and uses thereof |
| JP5611826B2 (ja) | 2007-09-04 | 2014-10-22 | ザ スクリプス リサーチ インスティテュート | タンパク質キナーゼ阻害剤としての置換されたピリミジニル−アミン |
| WO2009061761A2 (en) | 2007-11-06 | 2009-05-14 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic amines |
| WO2009146034A2 (en) * | 2008-03-31 | 2009-12-03 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors and methods of use thereof |
| WO2009156484A2 (en) | 2008-06-27 | 2009-12-30 | Novartis Ag | Organic compounds |
| EP2361248B1 (en) | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds and uses thereof |
| WO2010077275A1 (en) | 2008-12-08 | 2010-07-08 | Arena Pharmaceuticals, Inc. | Modulators of the prostacyclin (pgi2) receptor useful for the treatment of disorders related thereto |
| KR101961500B1 (ko) | 2011-02-28 | 2019-03-22 | 어레이 바이오파마 인크. | 세린/트레오닌 키나제 억제제 |
| RU2014108140A (ru) | 2011-08-04 | 2015-09-10 | Эррэй Биофарма Инк. | Соединение на основе хинозолина в качестве ингибиторов серен-треониновых киназ |
| UA116774C2 (uk) | 2012-03-01 | 2018-05-10 | Еррей Біофарма Інк. | Інгібітори серин/треонінкінази |
| KR20150047597A (ko) | 2012-08-27 | 2015-05-04 | 어레이 바이오파마 인크. | 과증식성 질환의 치료를 위한 세린/트레오닌 키나아제 억제제 |
-
2012
- 2012-02-28 KR KR1020137025269A patent/KR101961500B1/ko not_active Expired - Fee Related
- 2012-02-28 BR BR112013021896A patent/BR112013021896A2/pt not_active Application Discontinuation
- 2012-02-28 JP JP2013556817A patent/JP6085866B2/ja active Active
- 2012-02-28 EP EP20120709429 patent/EP2681215B1/en active Active
- 2012-02-28 WO PCT/US2012/027009 patent/WO2012118850A1/en not_active Ceased
- 2012-02-28 CA CA2828478A patent/CA2828478C/en not_active Expired - Fee Related
- 2012-02-28 ES ES12709429.0T patent/ES2543050T3/es active Active
- 2012-02-28 MX MX2013009877A patent/MX339873B/es active IP Right Grant
- 2012-02-28 CN CN201280020897.3A patent/CN103635472B/zh active Active
- 2012-02-28 US US14/002,079 patent/US9133187B2/en active Active
- 2012-02-28 RU RU2013143839/04A patent/RU2013143839A/ru not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| MX339873B (es) | 2016-06-15 |
| US9133187B2 (en) | 2015-09-15 |
| CN103635472A (zh) | 2014-03-12 |
| KR20140014190A (ko) | 2014-02-05 |
| EP2681215B1 (en) | 2015-04-22 |
| CA2828478A1 (en) | 2012-09-07 |
| MX2013009877A (es) | 2014-02-11 |
| ES2543050T3 (es) | 2015-08-14 |
| RU2013143839A (ru) | 2015-04-10 |
| JP2014506930A (ja) | 2014-03-20 |
| WO2012118850A1 (en) | 2012-09-07 |
| CN103635472B (zh) | 2018-01-12 |
| CA2828478C (en) | 2019-12-31 |
| BR112013021896A2 (pt) | 2016-11-08 |
| EP2681215A1 (en) | 2014-01-08 |
| US20130338140A1 (en) | 2013-12-19 |
| KR101961500B1 (ko) | 2019-03-22 |
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