TWI422587B - Ａｋｔ及ｐ７０ ｓ６激酶抑制劑 - Google Patents
Ａｋｔ及ｐ７０ ｓ６激酶抑制劑 Download PDFInfo
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- TWI422587B TWI422587B TW098136731A TW98136731A TWI422587B TW I422587 B TWI422587 B TW I422587B TW 098136731 A TW098136731 A TW 098136731A TW 98136731 A TW98136731 A TW 98136731A TW I422587 B TWI422587 B TW I422587B
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- Prior art keywords
- compound
- phenyl
- ethyl
- imidazol
- fluoro
- Prior art date
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- 108010013238 70-kDa Ribosomal Protein S6 Kinases Proteins 0.000 title description 13
- 229940043355 kinase inhibitor Drugs 0.000 title description 7
- 239000003757 phosphotransferase inhibitor Substances 0.000 title description 7
- 150000001875 compounds Chemical class 0.000 claims description 166
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- 150000003839 salts Chemical class 0.000 claims description 49
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- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 21
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- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 12
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- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims description 3
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Classifications
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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- 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
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- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
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| US11327308P | 2008-11-11 | 2008-11-11 |
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| TW201022268A TW201022268A (en) | 2010-06-16 |
| TWI422587B true TWI422587B (zh) | 2014-01-11 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CA2767064C (fr) | 2009-07-02 | 2017-11-07 | Sanofi | Nouveaux derives de (6-oxo-1,6-dihydro-pyrimidin-2-yl)-amide, leur preparation et leur utilisation pharmaceutique comme inhibiteurs de phosphorylation d'akt(pkb) |
| JP5581390B2 (ja) * | 2009-10-23 | 2014-08-27 | イーライ リリー アンド カンパニー | Ａｋｔ阻害剤 |
| WO2012136776A1 (en) | 2011-04-07 | 2012-10-11 | Bayer Intellectual Property Gmbh | Imidazopyridazines as akt kinase inhibitors |
| US8927572B2 (en) * | 2011-07-09 | 2015-01-06 | Xuanzhu Pharma Co., Ltd. | Crystal form I of salt of a dipeptidyl peptidase-IV inhibitor and preparation method and use thereof |
| MX346095B (es) | 2011-09-12 | 2017-03-07 | Merck Patent Gmbh | Nuevas imidazol-aminas como moduladores de la actividad de cinasas. |
| HUE034979T2 (en) | 2011-09-12 | 2018-05-02 | Merck Patent Gmbh | Aminopyrimidine derivatives for use as modulators of kinase activity |
| US9580443B2 (en) | 2012-11-16 | 2017-02-28 | Merck Patent Gmbh | Heterocyclic derivatives as modulators of kinase activity |
| EP3299362B1 (en) * | 2012-11-16 | 2020-04-22 | Merck Patent GmbH | Imidazol-piperidinyl derivatives as modulators of kinase activity |
| ES2746756T3 (es) * | 2013-03-11 | 2020-03-06 | Merck Patent Gmbh | Derivados de 6-[4-(1H-imidazol-2-il)piperidin-1-il]pirimidin-4-amina como moduladores de la actividad cinasa |
| BR112016015285A8 (pt) * | 2014-02-11 | 2020-06-09 | Merck Patent Gmbh | pirimidina imidazol aminas como moduladores da atividade de quinase, seus usos e seu processo de preparação, composição farmacêutica, e kit |
| TW201718574A (zh) | 2015-08-12 | 2017-06-01 | 美國禮來大藥廠 | Ｃｇｒｐ受體拮抗劑 |
| MX374576B (es) * | 2016-05-20 | 2025-03-06 | Taiho Pharmaceutical Co Ltd | Derivado de 5h-pirrolo[2,3-d]pirimidin-6(7h)-ona novedoso. |
| BR112022017856A2 (pt) * | 2020-03-17 | 2022-11-01 | Jiangsu Hengrui Pharmaceuticals Co Ltd | Derivado bicíclico fundido, método de preparação do mesmo e uso farmacêutico do mesmo |
| CN113444110B (zh) * | 2020-03-25 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 四氢吡咯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| TW202328138A (zh) | 2021-09-17 | 2023-07-16 | 大陸商江蘇恒瑞醫藥股份有限公司 | 稠合二環類衍生物的可藥用鹽、晶型及其製備方法 |
| JPWO2024009977A1 (cg-RX-API-DMAC7.html) * | 2022-07-05 | 2024-01-11 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006091450A1 (en) * | 2005-02-18 | 2006-08-31 | Lexicon Genetics Incorporated | 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds |
| WO2008075109A1 (en) * | 2006-12-21 | 2008-06-26 | Astex Therapeutics Limited | Substituted piperidines having protein kinase inhibiting activity |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| JP5213229B2 (ja) | 2004-04-23 | 2013-06-19 | エグゼリクシス， インコーポレイテッド | キナーゼ調節因子および使用方法 |
| MY179032A (en) | 2004-10-25 | 2020-10-26 | Cancer Research Tech Ltd | Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors |
| CA2590961C (en) | 2004-12-28 | 2013-11-26 | Exelixis, Inc. | [1h-pyrazolo[3,4-d]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-threonine kinase modulators (p70s6k, atk1 and atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| US20090325924A1 (en) | 2005-06-30 | 2009-12-31 | Stuart Edward | GPCR Agonists |
| WO2007125321A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| WO2007125310A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Pharmaceutical combinations of pk inhibitors and other active agents |
| WO2008012635A2 (en) | 2006-07-26 | 2008-01-31 | Pfizer Products Inc. | Amine derivatives useful as anticancer agents |
| UA99284C2 (ru) | 2007-05-11 | 2012-08-10 | Елі Ліллі Енд Компані | ИНГИБИТОРЫ р70 S6-КИНАЗЫ |
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Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006091450A1 (en) * | 2005-02-18 | 2006-08-31 | Lexicon Genetics Incorporated | 4-piperidin-1-yl-7h-pyrrolo[2,3-d]pyrimidine compounds |
| WO2008075109A1 (en) * | 2006-12-21 | 2008-06-26 | Astex Therapeutics Limited | Substituted piperidines having protein kinase inhibiting activity |
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