CN1805748B - 作为raf激酶抑制剂的2-氨基嘧啶衍生物 - Google Patents
作为raf激酶抑制剂的2-氨基嘧啶衍生物 Download PDFInfo
- Publication number
- CN1805748B CN1805748B CN2004800163287A CN200480016328A CN1805748B CN 1805748 B CN1805748 B CN 1805748B CN 2004800163287 A CN2004800163287 A CN 2004800163287A CN 200480016328 A CN200480016328 A CN 200480016328A CN 1805748 B CN1805748 B CN 1805748B
- Authority
- CN
- China
- Prior art keywords
- halogen
- alkyl
- compound
- alkoxy
- amino
- 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.)
- Expired - Fee Related
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- 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
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/02—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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US47870903P | 2003-06-13 | 2003-06-13 | |
| US60/478,709 | 2003-06-13 | ||
| PCT/EP2004/006317 WO2004110452A1 (en) | 2003-06-13 | 2004-06-11 | 2-aminopyrimidine derivatives as raf kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1805748A CN1805748A (zh) | 2006-07-19 |
| CN1805748B true CN1805748B (zh) | 2010-05-26 |
Family
ID=33551850
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2004800163287A Expired - Fee Related CN1805748B (zh) | 2003-06-13 | 2004-06-11 | 作为raf激酶抑制剂的2-氨基嘧啶衍生物 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20060293340A1 (enExample) |
| EP (1) | EP1635835B1 (enExample) |
| JP (1) | JP2006527230A (enExample) |
| CN (1) | CN1805748B (enExample) |
| AT (1) | ATE454152T1 (enExample) |
| AU (1) | AU2004246800B2 (enExample) |
| BR (1) | BRPI0411365A (enExample) |
| CA (1) | CA2529090A1 (enExample) |
| DE (1) | DE602004024988D1 (enExample) |
| ES (1) | ES2338557T3 (enExample) |
| MX (1) | MXPA05013349A (enExample) |
| PL (1) | PL1635835T3 (enExample) |
| PT (1) | PT1635835E (enExample) |
| WO (1) | WO2004110452A1 (enExample) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7939541B2 (en) | 2004-09-09 | 2011-05-10 | Natco Pharma Limited | Intermediates and a process employing the intermediates for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide |
| US8735415B2 (en) | 2004-09-09 | 2014-05-27 | Natco Pharma Limited | Acid addition salts of (3,5-Bis trifluoromethyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide |
| UA94570C2 (en) * | 2004-09-09 | 2011-05-25 | Натко Фарма Лимитед | Phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase |
| CN1939910A (zh) | 2004-12-31 | 2007-04-04 | 孙飘扬 | 氨基嘧啶类化合物及其盐和其制备方法与药物用途 |
| CN1972917B (zh) * | 2004-12-31 | 2010-08-25 | 孙飘扬 | 氨基嘧啶类化合物及其盐和其制备方法与药物用途 |
| MX2007011866A (es) * | 2005-02-25 | 2007-10-10 | Novartis Ag | Combinacion farmaceutica de inhibidores de bcr-abl y raf. |
| KR100674813B1 (ko) * | 2005-08-05 | 2007-01-29 | 일양약품주식회사 | N-페닐-2-피리미딘-아민 유도체 및 그의 제조방법 |
| EA200870217A1 (ru) * | 2006-01-30 | 2009-02-27 | Экселиксис, Инк. | 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции |
| WO2008020203A1 (en) * | 2006-08-17 | 2008-02-21 | Astrazeneca Ab | Pyridinylquinaz0linamine derivatives and their use as b-raf inhibitors |
| ES2496592T3 (es) | 2006-11-16 | 2014-09-19 | F.I.S.- Fabbrica Italiana Sintetici S.P.A. | Proceso para la preparación de Imatinib y compuestos intermedios del mismo |
| JP5160637B2 (ja) * | 2007-05-04 | 2013-03-13 | アイアールエム・リミテッド・ライアビリティ・カンパニー | c−kitおよびPDGFRキナーゼインヒビターとしての化合物および組成物 |
| US9062023B2 (en) | 2007-06-07 | 2015-06-23 | Intra-Cellular Therapies, Inc. | Heterocycle compounds and uses thereof |
| US8367686B2 (en) | 2007-06-07 | 2013-02-05 | Intra-Cellular Therapies, Inc. | Heterocycle compounds and uses thereof |
| JP5511680B2 (ja) | 2007-12-19 | 2014-06-04 | キャンサー・リサーチ・テクノロジー・リミテッド | ピリド[2,3−b]ピラジン−8−置換化合物及びその使用 |
| JP2011513332A (ja) * | 2008-02-29 | 2011-04-28 | アレイ バイオファーマ、インコーポレイテッド | 癌の治療のためのraf阻害剤としてのn−(6−アミノピリジン−3−イル)−3−(スルホンアミド)ベンズアミド誘導体 |
| JP2011513329A (ja) * | 2008-02-29 | 2011-04-28 | アレイ バイオファーマ、インコーポレイテッド | RAF阻害化合物として使用されるイミダゾ[4,5−b]ピリジン誘導体 |
| CA2716951A1 (en) * | 2008-02-29 | 2009-09-11 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
| JP2011513331A (ja) * | 2008-02-29 | 2011-04-28 | アレイ バイオファーマ、インコーポレイテッド | ピラゾール[3,4−b]ピリジンRAF阻害剤 |
| US8067422B2 (en) | 2008-03-04 | 2011-11-29 | Natco Pharma Limited | Crystal form of phenylamino pyrimidine derivatives |
| WO2010068863A2 (en) | 2008-12-12 | 2010-06-17 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimidine compounds and methods of making and using same |
| WO2010100127A1 (en) | 2009-03-04 | 2010-09-10 | Novartis Ag | Disubstituted imidazole derivatives as modulators of raf kinase |
| JP6166534B2 (ja) | 2009-08-05 | 2017-07-19 | イントラ−セルラー・セラピーズ・インコーポレイテッドIntra−Cellular Therapies, Inc. | 新規調節タンパク質および阻害剤 |
| CA2780892C (en) * | 2009-11-13 | 2017-02-14 | Genosco | Kinase inhibitors |
| NZ601085A (en) | 2010-02-01 | 2015-04-24 | Cancer Rec Tech Ltd | 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy |
| SG185664A1 (en) * | 2010-05-11 | 2012-12-28 | Mahesh Kandula | 4, 6 -dibenzoylamino- 2 -methyl- pyrimidine derivatives and their use for the treatment of cancer |
| US8334292B1 (en) | 2010-06-14 | 2012-12-18 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimidine compounds and methods of making and using same |
| US8551479B2 (en) * | 2010-09-10 | 2013-10-08 | Oncomed Pharmaceuticals, Inc. | Methods for treating melanoma |
| KR20130116291A (ko) * | 2010-11-19 | 2013-10-23 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | Braf 억제제를 이용한 치료 방법 |
| GB201320729D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB201320732D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Methods of chemical synthesis |
| JP6795518B2 (ja) * | 2015-04-23 | 2020-12-02 | インヒビカーセ セラピューティクス,インコーポレーテッド | キナーゼを阻害する組成物及び方法 |
| CN108586439A (zh) * | 2018-06-03 | 2018-09-28 | 刘思良 | 一种Raf激酶抑制剂及其在癌症治疗中的应用 |
| CN108864060A (zh) * | 2018-06-03 | 2018-11-23 | 刘思良 | 一种重氮类衍生物及其在癌症治疗中的应用 |
| CN108484587A (zh) * | 2018-06-03 | 2018-09-04 | 刘思良 | 一种Raf激酶抑制剂及其在癌症治疗中的应用 |
| CN108610336A (zh) * | 2018-06-03 | 2018-10-02 | 刘思良 | 一种重氮类衍生物及其在癌症治疗中的应用 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| TW202100520A (zh) | 2019-03-05 | 2021-01-01 | 美商英塞特公司 | 作為cdk2 抑制劑之吡唑基嘧啶基胺化合物 |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| WO2020223558A1 (en) | 2019-05-01 | 2020-11-05 | Incyte Corporation | Tricyclic amine compounds as cdk2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| TW202115024A (zh) | 2019-08-14 | 2021-04-16 | 美商英塞特公司 | 作為cdk2 抑制劑之咪唑基嘧啶基胺化合物 |
| CN119930610A (zh) | 2019-10-11 | 2025-05-06 | 因赛特公司 | 作为cdk2抑制剂的双环胺 |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| CN118891251A (zh) * | 2022-02-03 | 2024-11-01 | 奈可萨斯医药有限公司 | 芳基烃受体激动剂及其用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6180631B1 (en) * | 1997-10-06 | 2001-01-30 | Asta Medica Aktiengesellschaft | Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds |
| WO2002022597A1 (en) * | 2000-09-13 | 2002-03-21 | Novartis Ag | N-phenyl-2-pyrimidine-amine derivatives |
| WO2002093164A2 (en) * | 2001-05-16 | 2002-11-21 | Axxima Pharmaceuticals Ag | Pyridylpyrimidine derivatives as effective compounds against prion diseases |
| WO2003022833A1 (en) * | 2001-09-05 | 2003-03-20 | Smithkline Beecham Plc | Pyridylfurans and pyrroles as raf kinase inhibitors |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5521184A (en) * | 1992-04-03 | 1996-05-28 | Ciba-Geigy Corporation | Pyrimidine derivatives and processes for the preparation thereof |
| TW225528B (enExample) * | 1992-04-03 | 1994-06-21 | Ciba Geigy Ag | |
| GB9924092D0 (en) * | 1999-10-13 | 1999-12-15 | Zeneca Ltd | Pyrimidine derivatives |
| GB0201508D0 (en) * | 2002-01-23 | 2002-03-13 | Novartis Ag | Organic compounds |
| GB0202873D0 (en) * | 2002-02-07 | 2002-03-27 | Novartis Ag | Organic compounds |
| WO2003070173A2 (en) * | 2002-02-15 | 2003-08-28 | Sympore Gmbh | Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof |
| JP4552650B2 (ja) * | 2002-06-28 | 2010-09-29 | 日本新薬株式会社 | アミド誘導体及び医薬 |
| US7144911B2 (en) * | 2002-12-31 | 2006-12-05 | Deciphera Pharmaceuticals Llc | Anti-inflammatory medicaments |
| GB2398565A (en) * | 2003-02-18 | 2004-08-25 | Cipla Ltd | Imatinib preparation and salts |
-
2004
- 2004-06-11 PT PT04739809T patent/PT1635835E/pt unknown
- 2004-06-11 ES ES04739809T patent/ES2338557T3/es not_active Expired - Lifetime
- 2004-06-11 CN CN2004800163287A patent/CN1805748B/zh not_active Expired - Fee Related
- 2004-06-11 DE DE602004024988T patent/DE602004024988D1/de not_active Expired - Lifetime
- 2004-06-11 AU AU2004246800A patent/AU2004246800B2/en not_active Ceased
- 2004-06-11 CA CA002529090A patent/CA2529090A1/en not_active Abandoned
- 2004-06-11 AT AT04739809T patent/ATE454152T1/de not_active IP Right Cessation
- 2004-06-11 MX MXPA05013349A patent/MXPA05013349A/es active IP Right Grant
- 2004-06-11 BR BRPI0411365-9A patent/BRPI0411365A/pt not_active IP Right Cessation
- 2004-06-11 PL PL04739809T patent/PL1635835T3/pl unknown
- 2004-06-11 US US10/560,352 patent/US20060293340A1/en not_active Abandoned
- 2004-06-11 EP EP04739809A patent/EP1635835B1/en not_active Expired - Lifetime
- 2004-06-11 JP JP2006515898A patent/JP2006527230A/ja active Pending
- 2004-06-11 WO PCT/EP2004/006317 patent/WO2004110452A1/en not_active Ceased
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6180631B1 (en) * | 1997-10-06 | 2001-01-30 | Asta Medica Aktiengesellschaft | Methods of modulating serine/threonine protein kinase function with 5-azaquinoxaline-based compounds |
| WO2002022597A1 (en) * | 2000-09-13 | 2002-03-21 | Novartis Ag | N-phenyl-2-pyrimidine-amine derivatives |
| WO2002093164A2 (en) * | 2001-05-16 | 2002-11-21 | Axxima Pharmaceuticals Ag | Pyridylpyrimidine derivatives as effective compounds against prion diseases |
| WO2003022833A1 (en) * | 2001-09-05 | 2003-03-20 | Smithkline Beecham Plc | Pyridylfurans and pyrroles as raf kinase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0411365A (pt) | 2006-07-25 |
| AU2004246800A1 (en) | 2004-12-23 |
| PT1635835E (pt) | 2010-03-17 |
| AU2004246800B2 (en) | 2008-12-04 |
| PL1635835T3 (pl) | 2010-06-30 |
| DE602004024988D1 (de) | 2010-02-25 |
| ATE454152T1 (de) | 2010-01-15 |
| CN1805748A (zh) | 2006-07-19 |
| WO2004110452A1 (en) | 2004-12-23 |
| EP1635835B1 (en) | 2010-01-06 |
| ES2338557T3 (es) | 2010-05-10 |
| JP2006527230A (ja) | 2006-11-30 |
| CA2529090A1 (en) | 2004-12-23 |
| US20060293340A1 (en) | 2006-12-28 |
| MXPA05013349A (es) | 2006-03-09 |
| EP1635835A1 (en) | 2006-03-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| C17 | Cessation of patent right | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20100526 Termination date: 20110611 |