CN107530329B - 用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物 - Google Patents
用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物 Download PDFInfo
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- CN107530329B CN107530329B CN201680014422.1A CN201680014422A CN107530329B CN 107530329 B CN107530329 B CN 107530329B CN 201680014422 A CN201680014422 A CN 201680014422A CN 107530329 B CN107530329 B CN 107530329B
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- pyrazolo
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D487/04—Ortho-condensed systems
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- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN1128CH2015 | 2015-03-09 | ||
| IN1128/CHE/2015 | 2015-03-09 | ||
| PCT/IB2016/051302 WO2016142855A2 (en) | 2015-03-09 | 2016-03-08 | Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107530329A CN107530329A (zh) | 2018-01-02 |
| CN107530329B true CN107530329B (zh) | 2021-10-08 |
Family
ID=56879301
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680014422.1A Active CN107530329B (zh) | 2015-03-09 | 2016-03-08 | 用作CDK抑制剂的吡唑并[1,5-a][1,3,5]三嗪和吡唑并[1,5-a]嘧啶衍生物 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US11186576B2 (enExample) |
| EP (1) | EP3268000B1 (enExample) |
| JP (1) | JP6789962B2 (enExample) |
| CN (1) | CN107530329B (enExample) |
| CA (1) | CA2978170C (enExample) |
| ES (1) | ES2899196T3 (enExample) |
| WO (1) | WO2016142855A2 (enExample) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9180127B2 (en) | 2009-12-29 | 2015-11-10 | Dana-Farber Cancer Institute, Inc. | Type II Raf kinase inhibitors |
| EP3569598A1 (en) | 2011-11-17 | 2019-11-20 | Dana Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| JP6491202B2 (ja) | 2013-10-18 | 2019-03-27 | デイナ ファーバー キャンサー インスティチュート,インコーポレイテッド | サイクリン依存性キナーゼ7(cdk7)の多環阻害剤 |
| WO2015154022A1 (en) * | 2014-04-05 | 2015-10-08 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| HK1245260A1 (zh) | 2014-12-23 | 2018-08-24 | Dana-Farber Cancer Institute, Inc. | 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂 |
| EP3268000B1 (en) * | 2015-03-09 | 2021-08-04 | Aurigene Discovery Technologies Limited | Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors |
| JP6861166B2 (ja) * | 2015-03-27 | 2021-04-21 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
| US11142507B2 (en) | 2015-09-09 | 2021-10-12 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| WO2019023468A1 (en) | 2017-07-28 | 2019-01-31 | Nimbus Lakshmi, Inc. | TYK2 INHIBITORS AND USES THEREOF |
| TWI703149B (zh) * | 2017-11-16 | 2020-09-01 | 美商美國禮來大藥廠 | 用於抑制cdk7之化合物 |
| CA3095568A1 (en) * | 2018-03-29 | 2019-10-03 | Takeda Pharmaceutical Company Limited | Heterocyclic compound |
| AU2019250504B2 (en) * | 2018-04-11 | 2023-05-18 | Lead Discovery Center Gmbh | Pharmaceutically active pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives |
| IL277770B2 (en) * | 2018-04-11 | 2024-01-01 | Qurient Co Ltd | Pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives as selective inhibitor of cyclin dependent kinase |
| EP3810132A4 (en) | 2018-06-25 | 2022-06-22 | Dana-Farber Cancer Institute, Inc. | TAIRE FAMILY KINASE INHIBITORS AND RELATED USES |
| PT3710446T (pt) * | 2018-07-20 | 2022-09-20 | Lilly Co Eli | Compostos úteis para inibir cdk7 |
| CN110835345A (zh) * | 2018-08-17 | 2020-02-25 | 中国科学院上海药物研究所 | 一类细胞周期依赖性激酶的降解剂、其制备方法、药物组合物及其用途 |
| PE20212196A1 (es) | 2018-10-30 | 2021-11-16 | Kronos Bio Inc | Compuestos, composiciones, y metodos para modular la actividad cdk9 |
| US20220144841A1 (en) * | 2019-03-13 | 2022-05-12 | The Translational Genomics Research Institute | Trisubstituted pyrazolo [1,5-a] pyrimidine compounds as cdk7 inhibitors |
| CN112125908B (zh) * | 2019-06-25 | 2023-11-03 | 隆泰申医药科技(南京)有限公司 | Cdk激酶抑制剂、其制备方法、药物组合物和应用 |
| MX2022006052A (es) * | 2019-11-22 | 2022-08-15 | Univ California | Inhibidores de la caspasa 6 y usos de los mismos. |
| TW202146416A (zh) * | 2019-12-11 | 2021-12-16 | 德商拜耳廠股份有限公司 | 吡唑并三𠯤 |
| EP4079733A1 (en) * | 2019-12-20 | 2022-10-26 | Evopoint Biosciences Co., Ltd. | Heterocyclic compound, and pharmaceutical composition thereof, preparation method therefor, intermediate thereof and application thereof |
| CN110950871B (zh) * | 2019-12-25 | 2022-05-17 | 陕西师范大学 | 2-取代-4-芳氨基吡唑并三嗪衍生物及制备抗肿瘤药物的应用 |
| CN111393447B (zh) * | 2020-05-14 | 2021-01-15 | 苏州信诺维医药科技有限公司 | 一种嘧啶并吡唑类化合物、其制备方法及应用 |
| TWI783480B (zh) * | 2020-05-27 | 2022-11-11 | 美商美國禮來大藥廠 | 用於抑制cdk7之化合物 |
| WO2022033552A1 (zh) * | 2020-08-12 | 2022-02-17 | 隆泰申医药科技(南京) 有限公司 | Cdk激酶抑制剂、其制备方法、药物组合物和应用 |
| CN114133394B (zh) * | 2020-08-12 | 2023-12-08 | 赛诺哈勃药业(成都)有限公司 | 一种选择性针对细胞周期依赖性激酶12活性的化合物、制备方法及医药用途 |
| EP4320110A1 (en) * | 2021-04-09 | 2024-02-14 | Universität Basel | Triazine derivative as covalent inhibitors of pi3k |
| CN115340524B (zh) * | 2021-05-14 | 2024-05-28 | 重庆博腾制药科技股份有限公司 | 一种(s)-去甲烟碱甲基化制备(s)-尼古丁的方法 |
| US20250042903A1 (en) * | 2021-06-17 | 2025-02-06 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Triazine inhibitors of cyclin-dependent kinases |
| CN113801119B (zh) * | 2021-08-30 | 2022-09-30 | 新乡医学院 | 一种吡唑并[1,3,5]三嗪类化合物的合成方法 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| CN114181217B (zh) * | 2022-01-10 | 2022-12-27 | 陕西师范大学 | 吡唑并[1,5-a][1,3,5]三嗪衍生物及其盐和在制备抗癌药物中的应用 |
| WO2023227125A1 (zh) * | 2022-05-26 | 2023-11-30 | 杭州德睿智药科技有限公司 | 作为CDKs抑制剂的新型并杂环类新化合物及其应用 |
| CN119790056A (zh) * | 2022-09-30 | 2025-04-08 | 楚浦创制(武汉)医药科技有限公司 | 三并环类衍生物、药物组合物以及应用 |
| WO2024125532A1 (zh) * | 2022-12-12 | 2024-06-20 | 杭州德睿智药科技有限公司 | 作为CDKs抑制剂的新型并杂环类新化合物及其应用 |
| CN120712267A (zh) * | 2023-02-21 | 2025-09-26 | 杭州德睿智药科技有限公司 | 作为CDKs抑制剂的新型并杂环类新化合物及其应用 |
| WO2025040170A1 (zh) * | 2023-08-24 | 2025-02-27 | 杭州德睿智药科技有限公司 | 作为CDKs抑制剂的新型并杂环类新化合物及其应用 |
| CN119707984A (zh) * | 2023-09-28 | 2025-03-28 | 中国科学院上海药物研究所 | 吡唑并三嗪及吡唑并嘧啶衍生物、其制备方法、药物组合物及其用途 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| WO2008036277A1 (en) * | 2006-09-18 | 2008-03-27 | Polaris Group | Pyraz0l0(l,5-a) (1, 3, 5) triazine and pyrazolo (1, 5-a) pyrimidine derivatives useful as protein kinase inhibitors |
| WO2008151304A1 (en) * | 2007-06-05 | 2008-12-11 | Emory University | Selective inhibitors for cyclin-dependent kinases |
| CN104350054A (zh) * | 2012-03-01 | 2015-02-11 | 利德探索中心有限公司 | 作为选择性细胞周期蛋白依赖性激酶抑制剂的吡唑并-三嗪衍生物 |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0203542A3 (en) | 1999-08-12 | 2003-07-28 | Upjohn Co | 3(5)-amino-pyrazole derivatives, process for their preparation, their use and pharmaceutical compositions containing the same |
| US8084457B2 (en) | 2003-09-15 | 2011-12-27 | Lead Discovery Center Gmbh | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| EP1833819A1 (en) | 2004-12-30 | 2007-09-19 | Astex Therapeutics Limited | Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases |
| US20100160324A1 (en) | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| US20070078136A1 (en) | 2005-09-22 | 2007-04-05 | Bristol-Myers Squibb Company | Fused heterocyclic compounds useful as kinase modulators |
| EP2320895A2 (en) | 2008-07-03 | 2011-05-18 | Exelixis, Inc. | Cdk modulators |
| FR2943058B1 (fr) * | 2009-03-11 | 2011-06-03 | Centre Nat Rech Scient | Derives de pyrazolo°1,5-a!-1,3,5-triazines, leur preparation et leur application en therapeutique. |
| WO2012045195A1 (en) | 2010-10-09 | 2012-04-12 | Abbott Laboratories | Pyrrolopyrimidines as fak and alk inhibiters for treatment of cancers and other diseases |
| EP2634189A1 (en) | 2012-03-01 | 2013-09-04 | Lead Discovery Center GmbH | Pyrazolo-triazine derivatives as selective cyclin-dependent kinase inhibitors |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| EP2968339A4 (en) * | 2013-03-15 | 2017-02-15 | Celgene Avilomics Research, Inc. | Mk2 inhibitors and uses thereof |
| WO2015154022A1 (en) | 2014-04-05 | 2015-10-08 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| EP3268000B1 (en) * | 2015-03-09 | 2021-08-04 | Aurigene Discovery Technologies Limited | Pyrazolo[1,5-a][1,3,5]triazine and pyrazolo[1,5-a]pyrimidine derivatives as cdk inhibitors |
| JP6861166B2 (ja) | 2015-03-27 | 2021-04-21 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
| DK3302448T3 (da) * | 2015-06-04 | 2024-02-05 | Aurigene Oncology Ltd | Erstattede heterocyclylafledninger som cdk-inhibitore |
-
2016
- 2016-03-08 EP EP16761176.3A patent/EP3268000B1/en active Active
- 2016-03-08 US US15/557,028 patent/US11186576B2/en active Active
- 2016-03-08 CA CA2978170A patent/CA2978170C/en active Active
- 2016-03-08 CN CN201680014422.1A patent/CN107530329B/zh active Active
- 2016-03-08 ES ES16761176T patent/ES2899196T3/es active Active
- 2016-03-08 WO PCT/IB2016/051302 patent/WO2016142855A2/en not_active Ceased
- 2016-03-08 JP JP2017546949A patent/JP6789962B2/ja not_active Expired - Fee Related
-
2021
- 2021-10-01 US US17/492,282 patent/US20220281871A1/en not_active Abandoned
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6194410B1 (en) * | 1998-03-11 | 2001-02-27 | Hoffman-La Roche Inc. | Pyrazolopyrimidine and pyrazolines and process for preparation thereof |
| WO2008036277A1 (en) * | 2006-09-18 | 2008-03-27 | Polaris Group | Pyraz0l0(l,5-a) (1, 3, 5) triazine and pyrazolo (1, 5-a) pyrimidine derivatives useful as protein kinase inhibitors |
| WO2008151304A1 (en) * | 2007-06-05 | 2008-12-11 | Emory University | Selective inhibitors for cyclin-dependent kinases |
| CN104350054A (zh) * | 2012-03-01 | 2015-02-11 | 利德探索中心有限公司 | 作为选择性细胞周期蛋白依赖性激酶抑制剂的吡唑并-三嗪衍生物 |
Non-Patent Citations (1)
| Title |
|---|
| Synthesis and Structure-Activity Relationship of a New Series of Potent Angiotensin II Receptor Antagonists: Pyrazolo(1,5-a)pyrimidine Derivatives";SHIOTA, T. et.al.;《CHEMICAL & PHARMACEUTICAL BULLETIN》;19991231;第47卷(第7期);928–938 * |
Also Published As
| Publication number | Publication date |
|---|---|
| US20220281871A1 (en) | 2022-09-08 |
| ES2899196T3 (es) | 2022-03-10 |
| EP3268000B1 (en) | 2021-08-04 |
| CA2978170C (en) | 2024-02-27 |
| CA2978170A1 (en) | 2016-09-15 |
| EP3268000A4 (en) | 2018-08-22 |
| JP2018507877A (ja) | 2018-03-22 |
| US20180258092A9 (en) | 2018-09-13 |
| US11186576B2 (en) | 2021-11-30 |
| EP3268000A2 (en) | 2018-01-17 |
| US20180057497A1 (en) | 2018-03-01 |
| CN107530329A (zh) | 2018-01-02 |
| WO2016142855A2 (en) | 2016-09-15 |
| WO2016142855A3 (en) | 2016-11-03 |
| JP6789962B2 (ja) | 2020-11-25 |
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Address after: Karnataka Patentee after: Oregini Oncology Co.,Ltd. Address before: Karnataka Patentee before: AURIGENE DISCOVERY TECHNOLOGIES Ltd. |
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