CN113423703A - 含氮杂环类衍生物调节剂、其制备方法和应用 - Google Patents
含氮杂环类衍生物调节剂、其制备方法和应用 Download PDFInfo
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- CN113423703A CN113423703A CN202080012820.6A CN202080012820A CN113423703A CN 113423703 A CN113423703 A CN 113423703A CN 202080012820 A CN202080012820 A CN 202080012820A CN 113423703 A CN113423703 A CN 113423703A
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- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical group C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- VLLMWSRANPNYQX-UHFFFAOYSA-N thiadiazole Chemical compound C1=CSN=N1.C1=CSN=N1 VLLMWSRANPNYQX-UHFFFAOYSA-N 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
- FYSNRJHAOHDILO-UHFFFAOYSA-N thionyl chloride Substances ClS(Cl)=O FYSNRJHAOHDILO-UHFFFAOYSA-N 0.000 description 1
- GKASDNZWUGIAMG-UHFFFAOYSA-N triethyl orthoformate Chemical compound CCOC(OCC)OCC GKASDNZWUGIAMG-UHFFFAOYSA-N 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 238000011144 upstream manufacturing Methods 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
Classifications
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- 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
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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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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- A—HUMAN NECESSITIES
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- 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
- A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
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- 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
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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
-
- 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
- C07D471/10—Spiro-condensed systems
-
- 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
- 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
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- Chemical & Material Sciences (AREA)
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- Medicinal Chemistry (AREA)
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- General Health & Medical Sciences (AREA)
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- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
公开了一种含氮杂环类衍生物调节剂、其制备方法和应用。特别地，公开了通式(I)所示的化合物、其制备方法及含有该化合物的药物组合物，及其作为KRAS G12C突变抑制剂，在治疗白血病、神经母细胞瘤、黑色素瘤、乳腺癌、肺癌及其结肠癌等疾病或病症的用途，其中通式(I)中的各取代基与说明书中的定义相同。
Description
PCT国内申请，说明书已公开。
Claims (42)
- PCT国内申请，权利要求书已公开。
Priority Applications (2)
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|---|---|---|---|
| CN202410959825.XA CN118745177A (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN202410959819.4A CN118745176A (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
Applications Claiming Priority (13)
| Application Number | Priority Date | Filing Date | Title |
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| CN201910457161 | 2019-05-29 | ||
| CN2019104571616 | 2019-05-29 | ||
| CN201910918582 | 2019-09-26 | ||
| CN2019109185824 | 2019-09-26 | ||
| CN201911018909 | 2019-10-24 | ||
| CN2019110189099 | 2019-10-24 | ||
| CN201911090171 | 2019-11-08 | ||
| CN2019110901717 | 2019-11-08 | ||
| CN201911382159 | 2019-12-27 | ||
| CN2019113821593 | 2019-12-27 | ||
| CN202010451270 | 2020-05-25 | ||
| CN202010451270X | 2020-05-25 | ||
| PCT/CN2020/093285 WO2020239077A1 (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
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| CN202410959819.4A Division CN118745176A (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN202410959825.XA Division CN118745177A (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
Publications (2)
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| CN113423703A true CN113423703A (zh) | 2021-09-21 |
| CN113423703B CN113423703B (zh) | 2024-08-02 |
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| CN202410959825.XA Pending CN118745177A (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN202080012820.6A Active CN113423703B (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
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| CN202410959819.4A Pending CN118745176A (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN202410959825.XA Pending CN118745177A (zh) | 2019-05-29 | 2020-05-29 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20220213100A1 (zh) |
| EP (1) | EP3978490A4 (zh) |
| JP (1) | JP2022534765A (zh) |
| KR (1) | KR20220027879A (zh) |
| CN (3) | CN118745176A (zh) |
| AU (1) | AU2020282473A1 (zh) |
| CA (1) | CA3139769A1 (zh) |
| TW (1) | TW202110843A (zh) |
| WO (1) | WO2020239077A1 (zh) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN112047937A (zh) * | 2019-06-06 | 2020-12-08 | 劲方医药科技(上海)有限公司 | 四氢吡啶并[3,4-d]嘧啶-2(1H)-酮类化合物，其制法与医药上的用途 |
| CN112851663A (zh) * | 2019-11-12 | 2021-05-28 | 博瑞生物医药（苏州）股份有限公司 | 一种并杂环化合物及其用途 |
| CN113105448A (zh) * | 2020-01-13 | 2021-07-13 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| CN113544128A (zh) * | 2019-06-26 | 2021-10-22 | 微境生物医药科技(上海)有限公司 | Kras-g12c抑制剂 |
| CN116120315A (zh) * | 2023-04-19 | 2023-05-16 | 山东绿叶制药有限公司 | 一种kras g12c抑制剂及其应用 |
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| US12065430B2 (en) | 2018-10-26 | 2024-08-20 | Taiho Pharmaceutical Co., Ltd. | Indazole compound or salt thereof |
| CR20220230A (es) | 2019-10-28 | 2022-06-15 | Merck Sharp & Dohme | Inhibidores de pequeñas moléculas de mutante g12c de kras |
| WO2021139678A1 (zh) * | 2020-01-07 | 2021-07-15 | 广州百霆医药科技有限公司 | 吡啶并嘧啶类kras g12c突变蛋白抑制剂 |
| CN114671866A (zh) * | 2020-12-25 | 2022-06-28 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| EP4092026A4 (en) * | 2020-01-13 | 2024-03-06 | Suzhou Zelgen Biopharmaceutical Co., Ltd. | ARYL OR HETEROARYL PYRIDONE OR PYRIMIDINE DERIVATIVE, PREPARATION METHOD AND USE THEREOF |
| CN112159405B (zh) * | 2020-02-04 | 2021-09-14 | 广州必贝特医药技术有限公司 | 吡啶并嘧啶酮类化合物及其应用 |
| US20230099858A1 (en) * | 2020-02-20 | 2023-03-30 | Beta Pharma, Inc. | Pyridopyrimidine derivatives as kras inhibitors |
| WO2021175199A1 (zh) * | 2020-03-02 | 2021-09-10 | 上海喆邺生物科技有限公司 | 一类芳香杂环类化合物及其在药物中的应用 |
| WO2021219072A1 (zh) * | 2020-04-30 | 2021-11-04 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物的制备及其应用方法 |
| WO2021249563A1 (zh) * | 2020-06-12 | 2021-12-16 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| CN115052870B (zh) * | 2020-08-02 | 2024-02-20 | 上海喆邺生物科技有限公司 | 一种芳香类化合物及其在抗肿瘤药物中的应用 |
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| WO2022121839A1 (zh) * | 2020-12-08 | 2022-06-16 | 上海和誉生物医药科技有限公司 | 吡啶并[2,3-d]嘧啶-2(1H)-酮衍生物及其制备方法和应用 |
| WO2022133038A1 (en) * | 2020-12-16 | 2022-06-23 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| WO2022127847A1 (zh) * | 2020-12-17 | 2022-06-23 | 广东东阳光药业有限公司 | 嘧啶酮衍生物及其在药物中的应用 |
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| CN115215847A (zh) * | 2021-04-16 | 2022-10-21 | 中国科学院上海药物研究所 | 一类kras-sos1抑制剂、其制备方法及其应用 |
| 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 |
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| AU2022336415A1 (en) | 2021-09-01 | 2024-01-04 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112047937A (zh) * | 2019-06-06 | 2020-12-08 | 劲方医药科技(上海)有限公司 | 四氢吡啶并[3,4-d]嘧啶-2(1H)-酮类化合物，其制法与医药上的用途 |
| CN113544128A (zh) * | 2019-06-26 | 2021-10-22 | 微境生物医药科技(上海)有限公司 | Kras-g12c抑制剂 |
| CN113544128B (zh) * | 2019-06-26 | 2023-12-08 | 微境生物医药科技(上海)有限公司 | Kras-g12c抑制剂 |
| CN112851663A (zh) * | 2019-11-12 | 2021-05-28 | 博瑞生物医药（苏州）股份有限公司 | 一种并杂环化合物及其用途 |
| CN112851663B (zh) * | 2019-11-12 | 2023-07-18 | 博瑞生物医药（苏州）股份有限公司 | 一种并杂环化合物及其用途 |
| CN113105448A (zh) * | 2020-01-13 | 2021-07-13 | 苏州泽璟生物制药股份有限公司 | 芳基或杂芳基并吡啶酮或嘧啶酮类衍生物及其制备方法和应用 |
| CN116120315A (zh) * | 2023-04-19 | 2023-05-16 | 山东绿叶制药有限公司 | 一种kras g12c抑制剂及其应用 |
| CN116120315B (zh) * | 2023-04-19 | 2023-06-09 | 山东绿叶制药有限公司 | 一种kras g12c抑制剂及其应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| TW202110843A (zh) | 2021-03-16 |
| JP2022534765A (ja) | 2022-08-03 |
| CN118745176A (zh) | 2024-10-08 |
| US20220213100A1 (en) | 2022-07-07 |
| CA3139769A1 (en) | 2020-12-03 |
| EP3978490A4 (en) | 2023-04-19 |
| WO2020239077A1 (zh) | 2020-12-03 |
| AU2020282473A1 (en) | 2022-01-06 |
| CN118745177A (zh) | 2024-10-08 |
| EP3978490A1 (en) | 2022-04-06 |
| CN113423703B (zh) | 2024-08-02 |
| KR20220027879A (ko) | 2022-03-08 |
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