CN114786673A - Cdk抑制剂及其作为药物的用途 - Google Patents

Cdk抑制剂及其作为药物的用途 Download PDF

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Publication number
CN114786673A
CN114786673A CN202080078041.6A CN202080078041A CN114786673A CN 114786673 A CN114786673 A CN 114786673A CN 202080078041 A CN202080078041 A CN 202080078041A CN 114786673 A CN114786673 A CN 114786673A
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alkyl
cycloalkyl
fluoro
membered heterocycloalkyl
compound
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Chinese (zh)
Inventor
陆亮
鲁帕·谢蒂
安德鲁·保罗·库姆斯
戴超峰
劳尔·安德鲁·莱尔
克莱尔·拉佐·贝尔施
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Pruder Therapeutics Ltd
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Pruder Therapeutics Ltd
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Publication of CN114786673A publication Critical patent/CN114786673A/zh
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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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/08—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 two hetero rings linked by a carbon chain containing alicyclic rings
    • 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
    • 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
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/08—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing alicyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • 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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN202080078041.6A 2019-09-11 2020-09-11 Cdk抑制剂及其作为药物的用途 Pending CN114786673A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201962898839P 2019-09-11 2019-09-11
US62/898,839 2019-09-11
US202063005577P 2020-04-06 2020-04-06
US63/005,577 2020-04-06
PCT/US2020/050326 WO2021050824A1 (en) 2019-09-11 2020-09-11 Cdk inhibitors and their use as pharmaceuticals

Publications (1)

Publication Number Publication Date
CN114786673A true CN114786673A (zh) 2022-07-22

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US (3) US20220324830A1 (https=)
EP (1) EP4028005A4 (https=)
JP (1) JP7763489B2 (https=)
KR (1) KR20220079851A (https=)
CN (1) CN114786673A (https=)
AU (1) AU2020345950A1 (https=)
BR (1) BR112022004327A2 (https=)
CA (1) CA3153531A1 (https=)
IL (1) IL291191A (https=)
MX (1) MX2022002946A (https=)
WO (1) WO2021050824A1 (https=)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114605390A (zh) * 2020-12-04 2022-06-10 上海凌达生物医药有限公司 具有cdk激酶抑制活性的化合物、其药物组合物和用途
CN119638640A (zh) * 2024-12-10 2025-03-18 杭州亦宁医药技术有限公司 一种5-溴-2-甲基-3-异丙基-吲唑的制备方法
US12570607B2 (en) 2019-12-09 2026-03-10 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Compound as cyclin-dependent kinase 9 inhibitor and use thereof

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20220079851A (ko) * 2019-09-11 2022-06-14 프렐루드 테라퓨틱스, 인코포레이티드 Cdk 억제제 및 약제로서의 이의 용도
WO2022247785A1 (zh) * 2021-05-24 2022-12-01 石药集团中奇制药技术（石家庄）有限公司 一种周期蛋白依赖性激酶9抑制剂的用途
WO2022247796A1 (zh) * 2021-05-24 2022-12-01 石药集团中奇制药技术（石家庄）有限公司 周期蛋白依赖性激酶9抑制剂的用途
US20230144528A1 (en) * 2021-09-30 2023-05-11 Prelude Therapeutics Incorporated CDK Inhibitors And Their Use As Pharmaceuticals
KR20240115816A (ko) 2021-10-14 2024-07-26 프렐루드 테라퓨틱스, 인코포레이티드 Cdk9 억제제로서 작용하는 치환된 벤즈이미다졸의 결정질 형태 및 이의 용도
WO2025076115A1 (en) * 2023-10-02 2025-04-10 Prelude Therapeutics Incorporated Cdk inhibitors and their use as pharmaceuticals
WO2025189114A1 (en) 2024-03-08 2025-09-12 Prelude Therapeutics Incorporated Cdk inhibitors and their use as pharmaceuticals
WO2026024933A1 (en) * 2024-07-24 2026-01-29 Prelude Therapeutics Incorporated Cdk inhibitors and their use as pharmaceuticals

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US20140275011A1 (en) * 2013-03-13 2014-09-18 Abbvie Inc. Pyridine cdk9 kinase inhibitors

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CN103083643B (zh) 2008-03-27 2015-01-07 雀巢产品技术援助有限公司 增加肽、肽模拟物和其他胃肠道转运蛋白底物吸收的方法
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WO2015108861A1 (en) * 2014-01-14 2015-07-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
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JP2017523214A (ja) * 2014-08-05 2017-08-17 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヘテロ環キナーゼ阻害剤
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KR20220079851A (ko) * 2019-09-11 2022-06-14 프렐루드 테라퓨틱스, 인코포레이티드 Cdk 억제제 및 약제로서의 이의 용도
US12570607B2 (en) * 2019-12-09 2026-03-10 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Compound as cyclin-dependent kinase 9 inhibitor and use thereof
WO2022035799A1 (en) * 2020-08-10 2022-02-17 Prelude Therapeutics Incorporated Heterocycle cdk inhibitors and their use thereof
US11685744B2 (en) * 2020-09-21 2023-06-27 Prelude Therapeutics Incorporated CDK inhibitors and their use as pharmaceuticals
CA3205652A1 (en) * 2020-12-18 2022-06-23 Prelude Therapeutics Incorporated Cdk inhibitors and their use as pharmaceuticals
US20230144528A1 (en) * 2021-09-30 2023-05-11 Prelude Therapeutics Incorporated CDK Inhibitors And Their Use As Pharmaceuticals
KR20240115816A (ko) * 2021-10-14 2024-07-26 프렐루드 테라퓨틱스, 인코포레이티드 Cdk9 억제제로서 작용하는 치환된 벤즈이미다졸의 결정질 형태 및 이의 용도
WO2025076115A1 (en) * 2023-10-02 2025-04-10 Prelude Therapeutics Incorporated Cdk inhibitors and their use as pharmaceuticals

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US20140275011A1 (en) * 2013-03-13 2014-09-18 Abbvie Inc. Pyridine cdk9 kinase inhibitors

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12570607B2 (en) 2019-12-09 2026-03-10 Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. Compound as cyclin-dependent kinase 9 inhibitor and use thereof
CN114605390A (zh) * 2020-12-04 2022-06-10 上海凌达生物医药有限公司 具有cdk激酶抑制活性的化合物、其药物组合物和用途
CN114605390B (zh) * 2020-12-04 2024-08-16 上海凌达生物医药有限公司 具有cdk激酶抑制活性的化合物、其药物组合物和用途
CN119638640A (zh) * 2024-12-10 2025-03-18 杭州亦宁医药技术有限公司 一种5-溴-2-甲基-3-异丙基-吲唑的制备方法

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US12486277B2 (en) 2025-12-02
JP2022548568A (ja) 2022-11-21
CA3153531A1 (en) 2021-03-18
EP4028005A1 (en) 2022-07-20
EP4028005A4 (en) 2023-09-20
IL291191A (en) 2022-05-01
AU2020345950A1 (en) 2022-03-31
US11673893B2 (en) 2023-06-13
KR20220079851A (ko) 2022-06-14
BR112022004327A2 (pt) 2022-05-31
US20230242543A1 (en) 2023-08-03
WO2021050824A1 (en) 2021-03-18
JP7763489B2 (ja) 2025-11-04
US20210070761A1 (en) 2021-03-11
MX2022002946A (es) 2022-06-14
US20220324830A1 (en) 2022-10-13

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