CN114901661A - 新型K-Ras G12C抑制剂 - Google Patents
新型K-Ras G12C抑制剂 Download PDFInfo
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- CN114901661A CN114901661A CN202080090785.XA CN202080090785A CN114901661A CN 114901661 A CN114901661 A CN 114901661A CN 202080090785 A CN202080090785 A CN 202080090785A CN 114901661 A CN114901661 A CN 114901661A
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- alkyl
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
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- 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
- C07D403/14—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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Abstract
本发明涉及一种式(1)所示的化合物及其制备方法,及式(1)化合物、其各光学异构体、其各晶型、其药学上可接受的盐、其水合物或其溶剂合物作为G12C突变体K‑Ras蛋白不可逆抑制剂在制备抗肿瘤等Ras相关疾病的药物中的用途。
Description
PCT国内申请,说明书已公开。
Claims (11)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2019113866448 | 2019-12-27 | ||
CN201911386644.8A CN113045565A (zh) | 2019-12-27 | 2019-12-27 | 新型K-Ras G12C抑制剂 |
PCT/CN2020/139544 WO2021129824A1 (zh) | 2019-12-27 | 2020-12-25 | 新型K-Ras G12C抑制剂 |
Publications (1)
Publication Number | Publication Date |
---|---|
CN114901661A true CN114901661A (zh) | 2022-08-12 |
Family
ID=76507334
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201911386644.8A Pending CN113045565A (zh) | 2019-12-27 | 2019-12-27 | 新型K-Ras G12C抑制剂 |
CN202080090785.XA Pending CN114901661A (zh) | 2019-12-27 | 2020-12-25 | 新型K-Ras G12C抑制剂 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN201911386644.8A Pending CN113045565A (zh) | 2019-12-27 | 2019-12-27 | 新型K-Ras G12C抑制剂 |
Country Status (2)
Country | Link |
---|---|
CN (2) | CN113045565A (zh) |
WO (1) | WO2021129824A1 (zh) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
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 |
IL292438A (en) | 2019-10-28 | 2022-06-01 | Merck Sharp & Dohme | Small molecules that inhibit the g12c mutant of kras |
IL294048A (en) | 2019-12-20 | 2022-08-01 | Mirati Therapeutics Inc | sos1 inhibitors |
AU2021344830A1 (en) | 2020-09-03 | 2023-04-06 | Revolution Medicines, Inc. | Use of SOS1 inhibitors to treat malignancies with SHP2 mutations |
KR20230067635A (ko) | 2020-09-15 | 2023-05-16 | 레볼루션 메디슨즈, 인크. | 암의 치료에서 ras 억제제로서 인돌 유도체 |
WO2022235870A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Ras inhibitors for the treatment of cancer |
CR20230570A (es) | 2021-05-05 | 2024-01-22 | Revolution Medicines Inc | Inhibidores de ras |
WO2022247760A1 (zh) * | 2021-05-22 | 2022-12-01 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物,及其制备和治疗用途 |
WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
CN117677398A (zh) | 2021-07-27 | 2024-03-08 | 东丽株式会社 | 用于癌的治疗和/或预防的药品 |
AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
WO2023081840A1 (en) * | 2021-11-05 | 2023-05-11 | Frontier Medicines Corporation | Kras g12c inhibitors |
TW202340214A (zh) | 2021-12-17 | 2023-10-16 | 美商健臻公司 | 做為shp2抑制劑之吡唑并吡𠯤化合物 |
TW202342485A (zh) * | 2022-02-07 | 2023-11-01 | 美商新領域醫藥公司 | 癌症治療方法 |
EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
WO2023172940A1 (en) | 2022-03-08 | 2023-09-14 | Revolution Medicines, Inc. | Methods for treating immune refractory lung cancer |
WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
WO2023240189A1 (en) * | 2022-06-10 | 2023-12-14 | Bristol-Myers Squibb Company | Tetrahydropyrido 3,4-d pyrimidine derivatives as kras inhibitors |
WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2018064510A1 (en) * | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
WO2019099524A1 (en) * | 2017-11-15 | 2019-05-23 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
CN109843856A (zh) * | 2016-05-18 | 2019-06-04 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
JP2019085414A (ja) * | 2013-03-15 | 2019-06-06 | アラクセス ファーマ エルエルシー | Kras g12cの共有結合性阻害剤 |
US20190194192A1 (en) * | 2017-12-21 | 2019-06-27 | Boehringer Ingelheim International Gmbh | Novel benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors |
US20190270743A1 (en) * | 2017-11-15 | 2019-09-05 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
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 |
WO2019195609A2 (en) * | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
-
2019
- 2019-12-27 CN CN201911386644.8A patent/CN113045565A/zh active Pending
-
2020
- 2020-12-25 CN CN202080090785.XA patent/CN114901661A/zh active Pending
- 2020-12-25 WO PCT/CN2020/139544 patent/WO2021129824A1/zh active Application Filing
Patent Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2019085414A (ja) * | 2013-03-15 | 2019-06-06 | アラクセス ファーマ エルエルシー | Kras g12cの共有結合性阻害剤 |
CN109843856A (zh) * | 2016-05-18 | 2019-06-04 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
WO2018064510A1 (en) * | 2016-09-29 | 2018-04-05 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
WO2019099524A1 (en) * | 2017-11-15 | 2019-05-23 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
US20190270743A1 (en) * | 2017-11-15 | 2019-09-05 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
US20190194192A1 (en) * | 2017-12-21 | 2019-06-27 | Boehringer Ingelheim International Gmbh | Novel benzylamino substituted pyridopyrimidinones and derivatives as sos1 inhibitors |
WO2019195609A2 (en) * | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
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 |
Also Published As
Publication number | Publication date |
---|---|
CN113045565A (zh) | 2021-06-29 |
WO2021129824A1 (zh) | 2021-07-01 |
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