CN115715291A - 布鲁顿酪氨酸激酶抑制剂及其制备方法 - Google Patents
布鲁顿酪氨酸激酶抑制剂及其制备方法 Download PDFInfo
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- CN115715291A CN115715291A CN202180035678.1A CN202180035678A CN115715291A CN 115715291 A CN115715291 A CN 115715291A CN 202180035678 A CN202180035678 A CN 202180035678A CN 115715291 A CN115715291 A CN 115715291A
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- methyl
- pyridin
- dimethyl
- pyrrolo
- amino
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- -1 3 ' - (hydroxymethyl) -1-methyl-5- ((5- (2-methyl-4- (oxetan-3-yl) piperazin-1-yl) pyridin-2-yl) amino) -6-oxo-1,6-dihydro- [3,4' -bipyridine ] -2' -yl Chemical group 0.000 claims description 131
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- GETQZCLCWQTVFV-UHFFFAOYSA-N trimethylamine Chemical class CN(C)C GETQZCLCWQTVFV-UHFFFAOYSA-N 0.000 description 1
- QOWQDMIPYOKNHP-UHFFFAOYSA-N triphenoxy phosphate Chemical compound C=1C=CC=CC=1OOP(OOC=1C=CC=CC=1)(=O)OOC1=CC=CC=C1 QOWQDMIPYOKNHP-UHFFFAOYSA-N 0.000 description 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
- JQSHBVHOMNKWFT-DTORHVGOSA-N varenicline Chemical compound C12=CC3=NC=CN=C3C=C2[C@H]2C[C@@H]1CNC2 JQSHBVHOMNKWFT-DTORHVGOSA-N 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- 239000011592 zinc chloride Substances 0.000 description 1
- 235000005074 zinc chloride Nutrition 0.000 description 1
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- 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
- A61K31/495—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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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
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- 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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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
一类布鲁顿酪氨酸激酶抑制剂及其制备方法和在医药领域的应用,所述布鲁顿酪氨酸激酶抑制剂可用于预防和/或治疗与布鲁顿酪氨酸激酶介导的相关疾病,如自身免疫性疾病、癌症或炎症类疾病等。所提供的化合物,经实验研究,其对布鲁顿酪氨酸激酶靶点的选择性高,体内动物实验能表现出优异的药效作用。
Description
PCT国内申请,说明书已公开。
Claims (12)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
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CN202010558345 | 2020-06-18 | ||
CN2020105583454 | 2020-06-18 | ||
PCT/CN2021/100901 WO2021254483A1 (zh) | 2020-06-18 | 2021-06-18 | 布鲁顿酪氨酸激酶抑制剂及其制备方法 |
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US (1) | US20230348471A1 (zh) |
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Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103038233A (zh) * | 2010-05-07 | 2013-04-10 | 吉利德康涅狄格有限公司 | 吡啶酮和氮杂吡啶酮化合物及使用方法 |
CN104024255A (zh) * | 2011-11-03 | 2014-09-03 | 霍夫曼-拉罗奇有限公司 | 作为btk活性的抑制剂的烷基化哌嗪化合物 |
CN104105697A (zh) * | 2011-11-03 | 2014-10-15 | 霍夫曼-拉罗奇有限公司 | 二环哌嗪化合物 |
CN104125959A (zh) * | 2011-11-03 | 2014-10-29 | 霍夫曼-拉罗奇有限公司 | 作为btk活性的抑制剂的杂芳基吡啶酮和氮杂-吡啶酮化合物 |
CN110446710A (zh) * | 2016-12-15 | 2019-11-12 | 豪夫迈·罗氏有限公司 | 制备btk抑制剂的方法 |
-
2021
- 2021-06-18 CN CN202180035678.1A patent/CN115715291A/zh active Pending
- 2021-06-18 WO PCT/CN2021/100901 patent/WO2021254483A1/zh active Application Filing
- 2021-06-18 US US18/002,133 patent/US20230348471A1/en active Pending
Patent Citations (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103038233A (zh) * | 2010-05-07 | 2013-04-10 | 吉利德康涅狄格有限公司 | 吡啶酮和氮杂吡啶酮化合物及使用方法 |
CN104024255A (zh) * | 2011-11-03 | 2014-09-03 | 霍夫曼-拉罗奇有限公司 | 作为btk活性的抑制剂的烷基化哌嗪化合物 |
CN104105697A (zh) * | 2011-11-03 | 2014-10-15 | 霍夫曼-拉罗奇有限公司 | 二环哌嗪化合物 |
CN104125959A (zh) * | 2011-11-03 | 2014-10-29 | 霍夫曼-拉罗奇有限公司 | 作为btk活性的抑制剂的杂芳基吡啶酮和氮杂-吡啶酮化合物 |
CN110446710A (zh) * | 2016-12-15 | 2019-11-12 | 豪夫迈·罗氏有限公司 | 制备btk抑制剂的方法 |
Non-Patent Citations (1)
Title |
---|
JAMES J. CRAWFORD 等: "Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton’s Tyrosine Kinase Inhibitor in Early Clinical Development", 《JOURNAL OF MEDICINAL CHEMISTRY》, vol. 61, no. 6, 19 February 2018 (2018-02-19), pages 2227 - 2245, XP055685494, DOI: 10.1021/acs.jmedchem.7b01712 * |
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