CN113490669A - 一类具有降解Btk活性的化合物 - Google Patents
一类具有降解Btk活性的化合物 Download PDFInfo
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- CN113490669A CN113490669A CN202080018195.6A CN202080018195A CN113490669A CN 113490669 A CN113490669 A CN 113490669A CN 202080018195 A CN202080018195 A CN 202080018195A CN 113490669 A CN113490669 A CN 113490669A
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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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/02—Immunomodulators
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- 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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Abstract
本发明提供了一类具有降解Btk活性的化合物,具体地,本发明提供了一种如下式I所示的化合物;其中,各基团的定义如说明书中所述。本发明的化合物具有很好的Btk抑制活性并能将Btk降解,可以用于制备治疗Btk活性相关的疾病的药物。
Description
PCT国内申请,说明书已公开。
Claims (14)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201910158020 | 2019-03-02 | ||
CN2019101580204 | 2019-03-02 | ||
CN2019101616583 | 2019-03-05 | ||
CN201910161658.3A CN111662294A (zh) | 2019-03-05 | 2019-03-05 | 一类具有降解Btk活性的化合物 |
PCT/CN2020/077404 WO2020177657A1 (zh) | 2019-03-02 | 2020-03-02 | 一类具有降解Btk活性的化合物 |
Publications (2)
Publication Number | Publication Date |
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CN113490669A true CN113490669A (zh) | 2021-10-08 |
CN113490669B CN113490669B (zh) | 2022-12-30 |
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Application Number | Title | Priority Date | Filing Date |
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CN202080018195.6A Active CN113490669B (zh) | 2019-03-02 | 2020-03-02 | 一类具有降解Btk活性的化合物 |
Country Status (2)
Country | Link |
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CN (1) | CN113490669B (zh) |
WO (1) | WO2020177657A1 (zh) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN115611902A (zh) * | 2021-07-15 | 2023-01-17 | 标新生物医药科技(上海)有限公司 | 基于布鲁顿酪氨酸激酶配体设计的蛋白降解化合物及其应用 |
CN114409658B (zh) * | 2022-04-02 | 2022-06-07 | 水木未来(北京)科技有限公司 | 一种同时调节btk和ikzf3的双功能化合物 |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN109422752B (zh) * | 2017-09-03 | 2023-04-07 | 上海美志医药科技有限公司 | 一类具有抑制并降解布鲁顿酪氨酸蛋白激酶Btk活性的化合物 |
WO2019127008A1 (zh) * | 2017-12-26 | 2019-07-04 | 清华大学 | 一种靶向降解btk的化合物及其应用 |
EP3746426A4 (en) * | 2018-01-29 | 2021-12-29 | Dana Farber Cancer Institute, Inc. | Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use |
US11028088B2 (en) * | 2018-03-10 | 2021-06-08 | Yale University | Modulators of BTK proteolysis and methods of use |
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2020
- 2020-03-02 WO PCT/CN2020/077404 patent/WO2020177657A1/zh active Application Filing
- 2020-03-02 CN CN202080018195.6A patent/CN113490669B/zh active Active
Non-Patent Citations (3)
Title |
---|
CHRISTOPHER P. TINWORTH ET AL: ""PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding"", 《AMERICAN CHEMICAL SOCIETY》 * |
S. KRAJCOVICOVA ET AL: ""Solid-phase synthesis for thalidomide-based proteolysis-targeting chimeras (PROTAC)"", 《THE ROYAL SOCIETY OF CHEMISTRY》 * |
Y. SUN ET AL: ""PROTAC-induced BTK degradation as a novel therapy for mutated BTK C481S induced ibrutinib-resistant B-cell malignancies"", 《CELL RESEARCH》 * |
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Publication number | Publication date |
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CN113490669B (zh) | 2022-12-30 |
WO2020177657A1 (zh) | 2020-09-10 |
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