CN114630832A - 一种嘧啶并环衍生物及其在医药上的应用 - Google Patents
一种嘧啶并环衍生物及其在医药上的应用 Download PDFInfo
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- CN114630832A CN114630832A CN202080061791.2A CN202080061791A CN114630832A CN 114630832 A CN114630832 A CN 114630832A CN 202080061791 A CN202080061791 A CN 202080061791A CN 114630832 A CN114630832 A CN 114630832A
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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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D487/10—Spiro-condensed systems
-
- 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
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
Abstract
本发明涉及通式(I)所述的化合物或者其立体异构体、氘代物、溶剂化物、前药、代谢产物、共晶或药学上可接受的盐。本发明还涉及所述化合物的中间体和制备方法,以及在制备预防或治疗与KRAS G12C活性或表达量相关疾病的药物中的应用。
Description
PCT国内申请,说明书已公开。
Claims (21)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (13)
Application Number | Priority Date | Filing Date | Title |
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CN201911115896 | 2019-11-15 | ||
CN2019111158967 | 2019-11-15 | ||
CN201911293807 | 2019-12-18 | ||
CN2019112938078 | 2019-12-18 | ||
CN2020103860217 | 2020-05-09 | ||
CN202010386021 | 2020-05-09 | ||
CN202010499217 | 2020-06-05 | ||
CN2020104992177 | 2020-06-05 | ||
CN202010609971 | 2020-06-30 | ||
CN2020106099711 | 2020-06-30 | ||
CN2020112001496 | 2020-11-03 | ||
CN202011200149 | 2020-11-03 | ||
PCT/CN2020/128033 WO2021093758A1 (zh) | 2019-11-15 | 2020-11-11 | 一种嘧啶并环衍生物及其在医药上的应用 |
Publications (1)
Publication Number | Publication Date |
---|---|
CN114630832A true CN114630832A (zh) | 2022-06-14 |
Family
ID=75911780
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN202080061791.2A Pending CN114630832A (zh) | 2019-11-15 | 2020-11-11 | 一种嘧啶并环衍生物及其在医药上的应用 |
Country Status (3)
Country | Link |
---|---|
CN (1) | CN114630832A (zh) |
TW (1) | TWI760919B (zh) |
WO (1) | WO2021093758A1 (zh) |
Families Citing this family (16)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
JP2022517222A (ja) | 2019-01-10 | 2022-03-07 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12c阻害剤 |
JP2022546043A (ja) | 2019-08-29 | 2022-11-02 | ミラティ セラピューティクス, インコーポレイテッド | Kras g12d阻害剤 |
KR20220091480A (ko) | 2019-09-24 | 2022-06-30 | 미라티 테라퓨틱스, 인크. | 병용 요법 |
WO2021086833A1 (en) | 2019-10-28 | 2021-05-06 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
BR112022012106A2 (pt) | 2019-12-20 | 2022-09-20 | Mirati Therapeutics Inc | Inibidores de sos1 |
WO2021139748A1 (en) * | 2020-01-08 | 2021-07-15 | Ascentage Pharma (Suzhou) Co., Ltd. | Spirocyclic tetrahydroquinazolines |
WO2022040469A1 (en) * | 2020-08-19 | 2022-02-24 | The Trustees Of The Stevens Institute Of Technology | Spiro compounds as kras inhibitors |
US20230107642A1 (en) | 2020-12-18 | 2023-04-06 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
CN114685502A (zh) * | 2020-12-25 | 2022-07-01 | 由理生物医药(上海)有限公司 | 作为kras-g12c抑制剂的螺环类化合物 |
CN114805311A (zh) * | 2021-01-21 | 2022-07-29 | 苏州亚盛药业有限公司 | 螺环茚 |
WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
WO2023143623A1 (zh) * | 2022-01-30 | 2023-08-03 | 上海医药集团股份有限公司 | 一种喹啉类化合物及其应用 |
WO2023154766A1 (en) | 2022-02-09 | 2023-08-17 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
WO2024041621A1 (en) * | 2022-08-25 | 2024-02-29 | Jacobio Pharmaceuticals Co., Ltd. | K-ras mutant protein inhibitors |
WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
Citations (9)
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---|---|---|---|---|
US20140288045A1 (en) * | 2013-03-15 | 2014-09-25 | Araxes Pharma Llc | Covalent inhibitors of kras g12c |
US20160297774A1 (en) * | 2015-04-10 | 2016-10-13 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
CN109843856A (zh) * | 2016-05-18 | 2019-06-04 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
CN110036010A (zh) * | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
US20190248767A1 (en) * | 2018-02-09 | 2019-08-15 | Pfizer Inc. | Tetrahydroquinazoline Derivatives Useful as Anticancer Agents |
CN110256421A (zh) * | 2019-06-26 | 2019-09-20 | 微境生物医药科技(上海)有限公司 | Kras-g12c抑制剂 |
CN112119075A (zh) * | 2018-08-16 | 2020-12-22 | 豪夫迈·罗氏有限公司 | 稠环化合物 |
CN113087700A (zh) * | 2020-01-08 | 2021-07-09 | 苏州亚盛药业有限公司 | 螺环四氢喹唑啉 |
CN114096544A (zh) * | 2019-05-20 | 2022-02-25 | 加州理工学院 | Kras g12c抑制剂及其用途 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
TWI659021B (zh) * | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Kras g12c之抑制劑 |
EP3377481A1 (en) * | 2015-11-16 | 2018-09-26 | Araxes Pharma LLC | 2-substituted quinazoline compounds comprising a substituted heterocyclic group and methods of use thereof |
JOP20190186A1 (ar) * | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
JOP20190272A1 (ar) * | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
CN110869358A (zh) * | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
-
2020
- 2020-11-11 TW TW109139393A patent/TWI760919B/zh not_active IP Right Cessation
- 2020-11-11 WO PCT/CN2020/128033 patent/WO2021093758A1/zh active Application Filing
- 2020-11-11 CN CN202080061791.2A patent/CN114630832A/zh active Pending
Patent Citations (10)
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US20140288045A1 (en) * | 2013-03-15 | 2014-09-25 | Araxes Pharma Llc | Covalent inhibitors of kras g12c |
US20160297774A1 (en) * | 2015-04-10 | 2016-10-13 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
CN109843856A (zh) * | 2016-05-18 | 2019-06-04 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
CN110036010A (zh) * | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
US20190248767A1 (en) * | 2018-02-09 | 2019-08-15 | Pfizer Inc. | Tetrahydroquinazoline Derivatives Useful as Anticancer Agents |
TW201942116A (zh) * | 2018-02-09 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌劑之四氫喹唑啉衍生物 |
CN112119075A (zh) * | 2018-08-16 | 2020-12-22 | 豪夫迈·罗氏有限公司 | 稠环化合物 |
CN114096544A (zh) * | 2019-05-20 | 2022-02-25 | 加州理工学院 | Kras g12c抑制剂及其用途 |
CN110256421A (zh) * | 2019-06-26 | 2019-09-20 | 微境生物医药科技(上海)有限公司 | Kras-g12c抑制剂 |
CN113087700A (zh) * | 2020-01-08 | 2021-07-09 | 苏州亚盛药业有限公司 | 螺环四氢喹唑啉 |
Non-Patent Citations (1)
Title |
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叶炜芃等: "奥沙利铂或伊立替康联合氟尿嘧啶在 KRAS 突变型的晚期结直肠癌一线化疗中的疗效比较", 《岭南现代临床外科》, vol. 16, no. 5, pages 553 - 556 * |
Also Published As
Publication number | Publication date |
---|---|
WO2021093758A1 (zh) | 2021-05-20 |
TWI760919B (zh) | 2022-04-11 |
TW202128672A (zh) | 2021-08-01 |
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