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 |
|---|---|---|---|---|
| NZ597579A (en) | 2009-07-02 | 2013-06-28 | Sanofi Sa | Novel (6-oxo-1, 6-dihydro-pyrimidin-2-yl)-amide derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors |
| CN102574852B (zh) * | 2009-10-23 | 2014-06-25 | 伊莱利利公司 | Akt抑制剂 |
| PT2694510E (pt) | 2011-04-07 | 2016-02-08 | Bayer Pharma AG | Imidazopiridazinas como inibidores da akt quinase |
| JP5695800B2 (ja) * | 2011-07-09 | 2015-04-08 | 山東軒竹医薬科技有限公司 | ジペプチジルペプチダーゼ−ｉｖ阻害剤の塩の結晶形ｉ、及びその製造方法並びにその応用 |
| DK2755958T3 (en) | 2011-09-12 | 2017-09-25 | Merck Patent Gmbh | AMINOPYRIMIDINE DERIVATIVES USED AS MODULATORS OF KINASE ACTIVITY |
| US9145392B2 (en) * | 2011-09-12 | 2015-09-29 | Merck Patent Gmbh | Imidazole amines as modulators of kinase activity |
| CN105102435A (zh) | 2012-11-16 | 2015-11-25 | 默克专利有限公司 | 用作激酶活性调节剂的新颖的咪唑-哌啶基衍生物 |
| CA2890288A1 (en) * | 2012-11-16 | 2014-05-22 | Merck Patent Gmbh | Novel heterocyclic derivatives as modulators of kinase activity |
| HK1218756A1 (zh) * | 2013-03-11 | 2017-03-10 | 默克专利有限公司 | 用作激酶活性调节剂的6-[4-(1h-咪唑-2-基)哌啶-1-基]嘧啶-4-胺衍生物 |
| RU2690679C2 (ru) * | 2014-02-11 | 2019-06-05 | Мерк Патент Гмбх | Новые пиримидинимидазоламины в качестве модуляторов активности киназы |
| TW201718574A (zh) | 2015-08-12 | 2017-06-01 | 美國禮來大藥廠 | Ｃｇｒｐ受體拮抗劑 |
| JP6576553B2 (ja) | 2016-05-20 | 2019-09-18 | 大鵬薬品工業株式会社 | 新規５Ｈ−ピロロ［２，３−ｄ］ピリミジン−６（７Ｈ）−オン誘導体 |
| CN118530260A (zh) * | 2020-03-17 | 2024-08-23 | 江苏恒瑞医药股份有限公司 | 稠合二环类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| US20250145641A1 (en) | 2021-09-17 | 2025-05-08 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Fused bicyclic derivative, pharmaceutically acceptable salt, crystal form thereof and preparation method therefor |
| CN119403807A (zh) * | 2022-07-05 | 2025-02-07 | 大鹏药品工业株式会社 | 5H－吡咯并［2,3－d］嘧啶－6（7H）－酮及其盐体的结晶 |
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 |
|---|---|---|---|---|
| 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 |
| US7994172B2 (en) | 2004-12-28 | 2011-08-09 | Exelixis, Inc. | [1H-pyrazolo[3, 4-D]pyrimidin-4-yl]-piperidine or -piperazine compounds as serine-theoronine kinase modulators (P70s6k, Atk1 and Atk2) for the treatment of immunological, inflammatory and proliferative diseases |
| JP5114395B2 (ja) | 2005-06-30 | 2013-01-09 | プロシディオン・リミテッド | Ｇｐｃｒアゴニスト |
| WO2007125310A2 (en) | 2006-04-25 | 2007-11-08 | Astex Therapeutics Limited | Pharmaceutical combinations of pk inhibitors and other active agents |
| EP2043655A2 (en) | 2006-04-25 | 2009-04-08 | Astex Therapeutics Limited | Purine and deazapurine derivatives as pharmaceutical compounds |
| 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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