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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (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 (34)
| 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 |
| JP2014517074A (ja) | 2011-06-24 | 2014-07-17 | アムジエン・インコーポレーテツド | Trpm8アンタゴニストおよび治療におけるそれらの使用 |
| MY157429A (en) | 2011-06-24 | 2016-06-15 | Amgen Inc | Trpm8 antagonists and their use in treatments |
| 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 |
| KR101795562B1 (ko) * | 2011-12-27 | 2017-11-08 | (주)바이오팜솔루션즈 | 뇌졸중의 치료 또는 예방에 사용되는 페닐카바메이트 화합물 |
| HRP20180591T1 (hr) | 2012-03-01 | 2018-05-18 | Array Biopharma, Inc. | Inhibitori kinaze serina ili treonina |
| US8952009B2 (en) | 2012-08-06 | 2015-02-10 | Amgen Inc. | Chroman derivatives as TRPM8 inhibitors |
| RU2644947C2 (ru) | 2012-08-27 | 2018-02-15 | Аррэй Байофарма Инк. | Ингибиторы серин/треонин киназы для лечения гиперпролиферативных заболеваний |
| AU2013318283A1 (en) * | 2012-09-19 | 2015-03-05 | Novartis Ag | Dihydropyrrolidino-pyrimidines as kinase inhibitors |
| MX2015004615A (es) | 2012-10-16 | 2015-07-17 | Hoffmann La Roche | Inhibidores de serina/treonina cinasa. |
| 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 |
| EP3077401B1 (en) | 2013-12-06 | 2018-04-18 | Genentech, Inc. | Serine/threonine kinase inhibitors |
| MX375902B (es) | 2013-12-30 | 2025-03-07 | Genentech Inc | Inhibidores de serina/treonina cinasa. |
| CA2934679C (en) * | 2013-12-30 | 2023-02-28 | Genentech, Inc. | Serine/threonine kinase inhibitors |
| EP3443114A1 (en) | 2016-04-15 | 2019-02-20 | H. Hoffnabb-La Roche Ag | Diagnostic and therapeutic methods for cancer |
| CN109843856B (zh) * | 2016-05-18 | 2023-05-02 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
| AU2018329925B2 (en) | 2017-09-08 | 2025-05-29 | F. Hoffmann-La Roche Ag | Diagnostic and therapeutic methods for cancer |
| EP4273141A1 (en) | 2017-09-29 | 2023-11-08 | Mitsubishi Tanabe Pharma Corporation | Optically active pyrrolidine compound and method for producing same |
| WO2019094311A1 (en) | 2017-11-08 | 2019-05-16 | Merck Sharp & Dohme Corp. | Prmt5 inhibitors |
| WO2019158579A1 (en) | 2018-02-13 | 2019-08-22 | 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 |
| MX2021011823A (es) | 2019-03-29 | 2021-10-22 | Jiangsu Hengrui Medicine Co | Derivado pirroloheterociclico, metodo de preparacion del mismo y su aplicacion en medicina. |
| TW202110837A (zh) * | 2019-05-24 | 2021-03-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 氫化吡啶并嘧啶類衍生物、其製備方法及其在醫藥上的應用 |
| 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 |
| 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 |
| KR20230079120A (ko) | 2020-09-29 | 2023-06-05 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 피롤로 헤테로고리계 유도체의 결정형 및 이의 제조 방법 |
| 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 |
| WO2024088296A1 (zh) * | 2022-10-25 | 2024-05-02 | 上海拓界生物医药科技有限公司 | 哌啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| IT202200024963A1 (it) * | 2022-12-05 | 2024-06-05 | Angelini Pharma S P A | Composti attivatori dei canali potassio Kv7.2/Kv7.3 |
| CN121969619A (zh) * | 2023-10-23 | 2026-05-01 | 上海拓界生物医药科技有限公司 | 一种含有噻唑基的哌啶并嘧啶类衍生物、其制备方法及其医药上的应用 |
| 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 |
| WO2026067627A1 (zh) * | 2024-09-26 | 2026-04-02 | 江苏恒瑞医药股份有限公司 | 一种降解剂及其用途 |
Family Cites Families (40)
| 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 |
| ES2262137T3 (es) | 1993-10-01 | 2006-11-16 | Novartis Ag | Derivados de pirimidinamina farmacologicamente activos y procedimientos para su preparacion. |
| US5543523A (en) | 1994-11-15 | 1996-08-06 | Regents Of The University Of Minnesota | Method and intermediates for the synthesis of korupensamines |
| HUP0001140A3 (en) | 1996-12-05 | 2002-05-28 | Amgen Inc Thousand Oaks | Substituted pyrimidinone and pyridone compounds and methods of use |
| US6602872B1 (en) | 1999-12-13 | 2003-08-05 | Merck & Co., Inc. | Substituted pyridazines having cytokine inhibitory activity |
| ATE293962T1 (de) | 2000-02-25 | 2005-05-15 | Hoffmann La Roche | Adenosin-rezeptor modulatoren |
| 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 |
| JP4530852B2 (ja) * | 2002-07-15 | 2010-08-25 | メルク・シャープ・エンド・ドーム・コーポレイション | 糖尿病治療のためのピペリジノピリミジンジペプチジルペプチダーゼ阻害剤 |
| 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 |
| DE602005024382D1 (de) | 2004-04-13 | 2010-12-09 | Astellas Pharma Inc | Polycyclische pyrimidine als kaliumionenkanal-modulatoren |
| 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 |
| AR053712A1 (es) | 2005-04-18 | 2007-05-16 | Neurogen Corp | Heteroarilos sustituidos, antagonistas de cb1 (receptor 1 canabinoide) |
| US20100022531A1 (en) * | 2005-09-01 | 2010-01-28 | 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 |
| EP1984331B1 (en) | 2006-02-16 | 2010-10-20 | Schering Corporation | Pyrrolidine derivatives as erk inhibitors |
| CA2651072A1 (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 |
| MX2009001913A (es) | 2006-08-23 | 2009-03-06 | Pfizer Prod Inc | Compuestos de pirimidona como inhibidores de gsk-3. |
| 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 |
| WO2008079933A2 (en) | 2006-12-22 | 2008-07-03 | Novartis Ag | Heteroaryl-heteroaryl compounds as cdk inhibitors for the treatment of cancer, inflammation and viral infections |
| JP5363350B2 (ja) * | 2007-03-19 | 2013-12-11 | 武田薬品工業株式会社 | Mapk/erkキナーゼ阻害剤 |
| WO2009011904A1 (en) * | 2007-07-19 | 2009-01-22 | Renovis, Inc. | Compounds useful as faah modulators and uses thereof |
| ES2535166T3 (es) | 2007-09-04 | 2015-05-06 | The Scripps Research Institute | Pirimidinil-aminas sustituidas como inhibidores de proteína-quinasas |
| WO2009061761A2 (en) | 2007-11-06 | 2009-05-14 | E. I. Du Pont De Nemours And Company | Fungicidal heterocyclic amines |
| US20090246198A1 (en) * | 2008-03-31 | 2009-10-01 | Takeda Pharmaceutical Company Limited | Mapk/erk kinase inhibitors and methods of use thereof |
| MX2010014572A (es) | 2008-06-27 | 2011-03-24 | Novartis Ag | Compuestos organicos. |
| NZ603525A (en) | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| EP2370413B1 (en) | 2008-12-08 | 2015-08-05 | Arena Pharmaceuticals, Inc. | Modulators of the prostacyclin (pgi2) receptor useful for the treatment of disorders related thereto |
| 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 |
| HRP20180591T1 (hr) | 2012-03-01 | 2018-05-18 | Array Biopharma, Inc. | Inhibitori kinaze serina ili treonina |
| RU2644947C2 (ru) | 2012-08-27 | 2018-02-15 | Аррэй Байофарма Инк. | Ингибиторы серин/треонин киназы для лечения гиперпролиферативных заболеваний |
-
2012
- 2012-02-28 CN CN201280020897.3A patent/CN103635472B/zh active Active
- 2012-02-28 EP EP20120709429 patent/EP2681215B1/en active Active
- 2012-02-28 BR BR112013021896A patent/BR112013021896A2/pt not_active Application Discontinuation
- 2012-02-28 WO PCT/US2012/027009 patent/WO2012118850A1/en not_active Ceased
- 2012-02-28 MX MX2013009877A patent/MX339873B/es active IP Right Grant
- 2012-02-28 RU RU2013143839/04A patent/RU2013143839A/ru not_active Application Discontinuation
- 2012-02-28 ES ES12709429.0T patent/ES2543050T3/es active Active
- 2012-02-28 US US14/002,079 patent/US9133187B2/en active Active
- 2012-02-28 KR KR1020137025269A patent/KR101961500B1/ko not_active Expired - Fee Related
- 2012-02-28 JP JP2013556817A patent/JP6085866B2/ja active Active
- 2012-02-28 CA CA2828478A patent/CA2828478C/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| ES2543050T3 (es) | 2015-08-14 |
| EP2681215A1 (en) | 2014-01-08 |
| JP2014506930A (ja) | 2014-03-20 |
| KR20140014190A (ko) | 2014-02-05 |
| BR112013021896A2 (pt) | 2016-11-08 |
| CA2828478A1 (en) | 2012-09-07 |
| RU2013143839A (ru) | 2015-04-10 |
| EP2681215B1 (en) | 2015-04-22 |
| CA2828478C (en) | 2019-12-31 |
| CN103635472B (zh) | 2018-01-12 |
| WO2012118850A1 (en) | 2012-09-07 |
| MX2013009877A (es) | 2014-02-11 |
| US9133187B2 (en) | 2015-09-15 |
| US20130338140A1 (en) | 2013-12-19 |
| MX339873B (es) | 2016-06-15 |
| CN103635472A (zh) | 2014-03-12 |
| KR101961500B1 (ko) | 2019-03-22 |
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