CN109952304A - 一类抑制并降解cdk的化合物 - Google Patents
一类抑制并降解cdk的化合物 Download PDFInfo
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- CN109952304A CN109952304A CN201880004082.3A CN201880004082A CN109952304A CN 109952304 A CN109952304 A CN 109952304A CN 201880004082 A CN201880004082 A CN 201880004082A CN 109952304 A CN109952304 A CN 109952304A
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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
- 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
- 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
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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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
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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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- 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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- 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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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
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Abstract
本发明提供了一类抑制并降解CDK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周期蛋白依赖性激酶CDK抑制活性,可以用于制备治疗CDK活性相关的疾病的药物。
Description
PCT国内申请,说明书已公开。
Claims (10)
- PCT国内申请,权利要求书已公开。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN201710837228.XA CN109516989B (zh) | 2017-09-17 | 2017-09-17 | 一类抑制并降解cdk的化合物 |
CN201710837228X | 2017-09-17 | ||
PCT/CN2018/105713 WO2019052535A1 (zh) | 2017-09-17 | 2018-09-14 | 一类抑制并降解cdk的化合物 |
Publications (2)
Publication Number | Publication Date |
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CN109952304A true CN109952304A (zh) | 2019-06-28 |
CN109952304B CN109952304B (zh) | 2021-08-24 |
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CN201710837228.XA Active CN109516989B (zh) | 2017-09-17 | 2017-09-17 | 一类抑制并降解cdk的化合物 |
CN201880004082.3A Active CN109952304B (zh) | 2017-09-17 | 2018-09-14 | 一类抑制并降解cdk的化合物 |
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CN201710837228.XA Active CN109516989B (zh) | 2017-09-17 | 2017-09-17 | 一类抑制并降解cdk的化合物 |
Country Status (3)
Country | Link |
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US (1) | US11236090B2 (zh) |
CN (2) | CN109516989B (zh) |
WO (1) | WO2019052535A1 (zh) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN109422733A (zh) * | 2017-09-03 | 2019-03-05 | 上海美志医药科技有限公司 | 一类抑制并降解酪氨酸蛋白激酶alk的化合物 |
IL275490B2 (en) | 2017-12-22 | 2024-05-01 | Ravenna Pharmaceuticals Inc | Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors |
EP3827000A4 (en) * | 2018-07-23 | 2022-03-30 | Dana-Farber Cancer Institute, Inc. | DEGRADATION OF CYCLINE DEPENDENT KINASE 4/6 (CDK4/6) BY CONJUGATION OF CDK4/6 INHIBITORS WITH LIGASE E3 LIGAND AND METHODS OF USE |
CN110305126A (zh) * | 2019-06-19 | 2019-10-08 | 浙江省医学科学院 | 一种基于crbn配体诱导cdk4/6降解的化合物及其制备方法、药物组合物和应用 |
CA3186548A1 (en) * | 2020-07-21 | 2022-01-27 | Song Hee Lee | Compound for androgen receptor degradation, and pharmaceutical use thereof |
WO2023177451A1 (en) * | 2022-03-18 | 2023-09-21 | EnhancedBio Inc. | Compounds and methods for the targeted degradation of cyclin dependent kinases |
WO2023207875A1 (en) * | 2022-04-25 | 2023-11-02 | Onquality Pharmaceuticals China Ltd. | Cdk inhibitors, pharmaceutical compositions, and therapeutic applications |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2014063061A1 (en) * | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
WO2016015605A1 (en) * | 2014-07-26 | 2016-02-04 | Sunshine Lake Pharma Co., Ltd. | Compounds as cdk small-molecule inhibitors and uses thereof |
WO2017185031A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
WO2018106870A1 (en) * | 2016-12-08 | 2018-06-14 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating cdk4/6-mediated cancer |
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2017
- 2017-09-17 CN CN201710837228.XA patent/CN109516989B/zh active Active
-
2018
- 2018-09-14 WO PCT/CN2018/105713 patent/WO2019052535A1/zh active Application Filing
- 2018-09-14 CN CN201880004082.3A patent/CN109952304B/zh active Active
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2020
- 2020-03-17 US US16/821,845 patent/US11236090B2/en active Active
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2014063061A1 (en) * | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
WO2016015605A1 (en) * | 2014-07-26 | 2016-02-04 | Sunshine Lake Pharma Co., Ltd. | Compounds as cdk small-molecule inhibitors and uses thereof |
WO2017185031A1 (en) * | 2016-04-22 | 2017-10-26 | Dana-Farber Cancer Institute, Inc. | Degradation of cyclin-dependent kinase 4/6 (cdk4/6) by conjugation of cdk4/6 inhibitors with e3 ligase ligand and methods of use |
WO2018106870A1 (en) * | 2016-12-08 | 2018-06-14 | Icahn School Of Medicine At Mount Sinai | Compositions and methods for treating cdk4/6-mediated cancer |
Also Published As
Publication number | Publication date |
---|---|
CN109516989A (zh) | 2019-03-26 |
CN109952304B (zh) | 2021-08-24 |
CN109516989B (zh) | 2021-12-31 |
US20200216450A1 (en) | 2020-07-09 |
US11236090B2 (en) | 2022-02-01 |
WO2019052535A1 (zh) | 2019-03-21 |
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