CN106103445B - 作为cdk抑制剂的吡唑并[1,5-a]嘧啶-5,7-二胺化合物和它们的治疗用途 - Google Patents

作为cdk抑制剂的吡唑并[1,5-a]嘧啶-5,7-二胺化合物和它们的治疗用途 Download PDF

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Publication number
CN106103445B
CN106103445B CN201580011502.7A CN201580011502A CN106103445B CN 106103445 B CN106103445 B CN 106103445B CN 201580011502 A CN201580011502 A CN 201580011502A CN 106103445 B CN106103445 B CN 106103445B
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CN106103445A (zh
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亚历山大·波恩德克
塞巴斯蒂安·克罗尔
安东尼·巴雷特
马修·富克特
布赖恩·斯拉弗
西马克·阿里
查尔斯·库姆斯
詹姆士·帕特里克·希德尔
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Ip2 Ipo Innovation Co Ltd
Emory University
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Imperial Innovations Ltd
Cancer Research Technology Ltd
Emory University
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    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201580011502.7A 2014-02-21 2015-02-20 作为cdk抑制剂的吡唑并[1,5-a]嘧啶-5,7-二胺化合物和它们的治疗用途 Active CN106103445B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB201403093A GB201403093D0 (en) 2014-02-21 2014-02-21 Therapeutic compounds and their use
GB1403093.6 2014-02-21
PCT/GB2015/050494 WO2015124941A1 (en) 2014-02-21 2015-02-20 Pyrazolo[1,5-a]pyrimidine-5,7-diamine compounds as cdk inhibitors and their therapeutic use

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CN106103445A CN106103445A (zh) 2016-11-09
CN106103445B true CN106103445B (zh) 2019-08-09

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AU (1) AU2015220560B2 (https=)
BR (1) BR112016018633B1 (https=)
CA (1) CA2939786C (https=)
CY (1) CY1121588T1 (https=)
DK (1) DK3107914T3 (https=)
ES (1) ES2721268T3 (https=)
GB (1) GB201403093D0 (https=)
HR (1) HRP20190685T1 (https=)
HU (1) HUE043122T2 (https=)
LT (1) LT3107914T (https=)
ME (1) ME03427B (https=)
NZ (1) NZ724323A (https=)
PL (1) PL3107914T3 (https=)
PT (1) PT3107914T (https=)
RS (1) RS58704B1 (https=)
SI (1) SI3107914T1 (https=)
SM (1) SMT201900266T1 (https=)
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WO (1) WO2015124941A1 (https=)

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CR20190157A (es) 2016-08-31 2019-08-13 Agios Pharmaceuticals Inc Inhibidores de procesos metabólicos celulares
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EP3666770A4 (en) * 2017-08-07 2021-04-07 Joint Stock Company "Biocad" NEW HETEROCYCLIC COMPOUNDS AS CDK8 / 19 INHIBITORS
US20200197392A1 (en) * 2017-08-15 2020-06-25 The Brigham & Women's Hospital, Inc. Compositions and methods for treating tuberous sclerosis complex
GB201715194D0 (en) * 2017-09-20 2017-11-01 Carrick Therapeutics Ltd Compounds and their therapeutic use
TWI703149B (zh) * 2017-11-16 2020-09-01 美商美國禮來大藥廠 用於抑制cdk7之化合物
EP3774810A1 (en) * 2018-04-11 2021-02-17 Qurient Co. Ltd. Pyrazolo-triazine and/or pyrazolo-pyrimidine derivatives as selective inhibitor of cyclin dependent kinase
EP3787629A4 (en) 2018-05-02 2022-01-05 Kinnate Biopharma Inc. CYCLINE-DEPENDENT KINASE INHIBITORS
SG11202013175SA (en) 2018-06-29 2021-01-28 Kinnate Biopharma Inc Inhibitors of cyclin-dependent kinases
AU2019370200B2 (en) 2018-10-30 2024-12-19 Kronos Bio, Inc. Compounds, compositions, and methods for modulating CDK9 activity
US12304913B2 (en) 2018-11-14 2025-05-20 Ube Industries, Ltd. Dihydropyrrolopyrazole derivative
CN109860354B (zh) * 2018-12-28 2020-05-19 南京邮电大学 同质集成红外光子芯片及其制备方法
US20220144841A1 (en) * 2019-03-13 2022-05-12 The Translational Genomics Research Institute Trisubstituted pyrazolo [1,5-a] pyrimidine compounds as cdk7 inhibitors
CN114269742B (zh) * 2019-07-10 2024-07-16 常州千红生化制药股份有限公司 作为治疗剂的4-(咪唑并[1,2-a]吡啶-3-基)-N-(吡啶基)嘧啶-2-胺的衍生物
CN114901284A (zh) * 2019-10-29 2022-08-12 希洛斯医药品股份有限公司 用细胞周期蛋白依赖性激酶7(cdk7)抑制剂治疗生物标志物鉴定的患者的癌症的方法
GB201918541D0 (en) 2019-12-16 2020-01-29 Carrick Therapeutics Ltd Therapeutic compounds and their use
US20230106032A1 (en) * 2020-03-06 2023-04-06 Bayer Aktiengesellschaft Imidazotriazines acting on cancer via inhibition of cdk12
WO2021216828A1 (en) * 2020-04-24 2021-10-28 Massachusetts Institute Of Technology Chimeric degraders of cyclin-dependent kinase 9 and uses thereof
US20240109898A1 (en) * 2021-01-22 2024-04-04 Shanghai Haiyan Pharmaceutical Technology Co., Ltd. Substituted pyrazolo[1,5-a]pyrimidine-7-amine derivatives, compositions and pharmaceutical uses thereof
AU2022271290A1 (en) 2021-05-07 2023-11-23 Kymera Therapeutics, Inc. Cdk2 degraders and uses thereof
GB202108572D0 (en) * 2021-06-16 2021-07-28 Carrick Therapeutics Ltd Therapeutic compounds and their use
WO2023001061A1 (en) * 2021-07-17 2023-01-26 Jingrui Biopharma Co., Ltd. Cdk7 selective inhibitors as anticancer agents
AU2022398230A1 (en) * 2021-11-24 2024-06-13 Kronos Bio, Inc. Polymorphic and salt forms of (1s,3s)-n1-(5-(pentan-3- yl)pyrazolo[1,5-a]pyrimidin-7-yl)cyclopentane-1,3-diamine
WO2024102447A1 (en) * 2022-11-10 2024-05-16 Emory University Uses of hydroimidazopyridopyrimidinone derivatives for managing aneurysms or other vascular conditions or diseases
EP4671245A1 (en) * 2023-02-20 2025-12-31 Jiangsu Chia Tai Fenghai Pharmaceutical Co., Ltd. HETEROAROMATIC CYCLIC COMPOUND SERVING AS A CDK7 KINASE INHIBITOR, ITS PREPARATION AND USE
CN120712267A (zh) * 2023-02-21 2025-09-26 杭州德睿智药科技有限公司 作为CDKs抑制剂的新型并杂环类新化合物及其应用
WO2025006569A1 (en) 2023-06-27 2025-01-02 Arvinas Operations, Inc. Combinations of estrogen receptor degraders and cdk7 inhibitors for the treatment of cancer
WO2025057087A1 (en) 2023-09-11 2025-03-20 Assia Chemical Industries Ltd. Solid state forms of samuraciclib
WO2025208097A1 (en) * 2024-03-29 2025-10-02 The Translational Genomics Research Institute Cdk7 inhibitors and methods of use thereof
WO2025208104A1 (en) * 2024-03-29 2025-10-02 The Translational Genomics Research Institute Cdk7 inhibitors and methods of use thereof
WO2026024674A1 (en) 2024-07-22 2026-01-29 Genesis Therapeutics, Inc. Methods of treating skp2-associated cancers
WO2026057043A1 (zh) * 2024-09-14 2026-03-19 正大天晴药业集团股份有限公司 作为cdk抑制剂的三并环化合物及其应用
EP4717312A1 (en) * 2024-09-27 2026-04-01 Perha Pharmaceuticals Pyrazolo[1,5-a]pyrimidine derivatives useful as a medicament

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AU2015220560A1 (en) 2016-10-06
US20160362410A1 (en) 2016-12-15
NZ724323A (en) 2022-02-25
CY1121588T1 (el) 2020-05-29
US10414772B2 (en) 2019-09-17
RS58704B1 (sr) 2019-06-28
HRP20190685T1 (hr) 2019-06-14
ME03427B (me) 2020-01-20
WO2015124941A1 (en) 2015-08-27
DK3107914T3 (en) 2019-04-29
SI3107914T1 (sl) 2019-05-31
BR112016018633B1 (pt) 2022-08-30
ES2721268T3 (es) 2019-07-30
HUE043122T2 (hu) 2019-08-28
US9932344B2 (en) 2018-04-03
LT3107914T (lt) 2019-05-27
US20180273540A1 (en) 2018-09-27
CN106103445A (zh) 2016-11-09
JP2017506250A (ja) 2017-03-02
PL3107914T3 (pl) 2019-09-30
CA2939786A1 (en) 2015-08-27
PT3107914T (pt) 2019-05-20
EP3107914A1 (en) 2016-12-28
BR112016018633A2 (https=) 2017-08-08
EP3107914B8 (en) 2019-07-17
GB201403093D0 (en) 2014-04-09
AU2015220560B2 (en) 2019-05-16
US20210253583A1 (en) 2021-08-19
CA2939786C (en) 2022-03-08
US11566029B2 (en) 2023-01-31
JP6498212B2 (ja) 2019-04-10
US20200055862A1 (en) 2020-02-20
SMT201900266T1 (it) 2019-07-11
US10927119B2 (en) 2021-02-23
TR201905647T4 (tr) 2019-05-21
EP3107914B1 (en) 2019-01-30

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Address after: England Atsushi

Co-patentee after: British Emperor Innovation Co., Ltd.

Patentee after: IP2 IPO Innovation Co., Ltd.

Co-patentee after: Emory University

Address before: Great Britain

Co-patentee before: British Emperor Innovation Co., Ltd.

Patentee before: Cancer Research Technology Co., Ltd.

Co-patentee before: Emory University

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