CN109952295A - 一种cdk4/6抑制剂及其制备方法和应用 - Google Patents

一种cdk4/6抑制剂及其制备方法和应用 Download PDF

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Publication number
CN109952295A
CN109952295A CN201780049731.7A CN201780049731A CN109952295A CN 109952295 A CN109952295 A CN 109952295A CN 201780049731 A CN201780049731 A CN 201780049731A CN 109952295 A CN109952295 A CN 109952295A
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base
alkyl
heterocyclic ring
compound
cancer
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CN109952295B (zh
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刘世强
周远峰
吴雪松
包如迪
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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Jiangsu Hansoh Pharmaceutical Group Co Ltd
Shanghai Hansoh Biomedical Co Ltd
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Priority claimed from CN201710157847.4A external-priority patent/CN107793399A/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
    • A61K31/495—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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

Abstract

本发明涉及一种具有式(Ⅰ)结构的CDK4/6抑制剂及其制备方法和应用。本发明所开发的式(Ⅰ)系列化合物对CDK4/6激酶活性具有很强的抑制作用，可广泛应用于制备预防和/或治疗癌症或肿瘤相关疾病特别是膀胱癌、卵巢癌、腹膜癌、胰腺癌、乳腺癌、子宫癌、子宫颈癌、子宫内膜癌、前列腺癌、雌性生殖道癌、睾丸癌、胃肠道间质瘤或前列腺肿瘤等疾病的药物，有望开发成新一代CDK4/6抑制剂药物。

Description

PCT国内申请，说明书已公开。

Claims (17)

  1. PCT国内申请，权利要求书已公开。
CN201780049731.7A 2016-09-07 2017-09-06 一种cdk4/6抑制剂及其制备方法和应用 Active CN109952295B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN2016108091544 2016-09-07
CN201610809154 2016-09-07
CN201710157847.4A CN107793399A (zh) 2016-09-07 2017-03-16 Cdk4/6抑制剂及其制备方法和应用
CN2017101578474 2017-03-16
CN201710338488 2017-05-15
CN2017103384882 2017-05-15
PCT/CN2017/100679 WO2018045957A1 (zh) 2016-09-07 2017-09-06 一种cdk4/6抑制剂及其制备方法和应用

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CN109952295A true CN109952295A (zh) 2019-06-28
CN109952295B CN109952295B (zh) 2021-04-06

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CN201780050147.3A Active CN109963842B (zh) 2016-09-07 2017-09-06 苯并咪唑类化合物激酶抑制剂及其制备方法和应用
CN202011099789.2A Active CN112250669B (zh) 2016-09-07 2017-09-06 苯并咪唑类化合物激酶抑制剂及其制备方法和应用
CN201780049731.7A Active CN109952295B (zh) 2016-09-07 2017-09-06 一种cdk4/6抑制剂及其制备方法和应用

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CN201780050147.3A Active CN109963842B (zh) 2016-09-07 2017-09-06 苯并咪唑类化合物激酶抑制剂及其制备方法和应用
CN202011099789.2A Active CN112250669B (zh) 2016-09-07 2017-09-06 苯并咪唑类化合物激酶抑制剂及其制备方法和应用

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TW (1) TWI765908B (zh)
WO (2) WO2018045957A1 (zh)

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CN110156754A (zh) * 2018-02-10 2019-08-23 杭州百诚医药科技股份有限公司 一种三取代嘧啶衍生物对蛋白激酶的抑制作用
CN113248500A (zh) * 2021-06-10 2021-08-13 中国药科大学 氮杂吲哚嘧啶胺杂环化合物及其制备方法和应用
CN115246822A (zh) * 2021-04-27 2022-10-28 中国科学院上海药物研究所 嘧啶类化合物及其制备方法和用途

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CN108794452B (zh) 2017-05-05 2021-05-28 上海时莱生物技术有限公司 具有激酶抑制活性的化合物、其制备方法和用途
WO2019126731A1 (en) 2017-12-22 2019-06-27 Petra Pharma Corporation Aminopyridine derivatives as phosphatidylinositol phosphate kinase inhibitors
EP3801529B1 (en) 2018-05-25 2023-10-11 OncoCube Therapeutics LLC Highly potent tacc3 inhibitor as a novel anticancer drug candidate
AU2019310595B2 (en) * 2018-07-27 2022-11-24 1200 Pharma Llc CDK inhibitors and uses thereof
CN110790748B (zh) * 2018-08-02 2022-04-19 江苏豪森药业集团有限公司 细胞周期蛋白依赖性激酶抑制剂的对甲苯磺酸盐晶型及其制备方法和用途
CN111138413B (zh) * 2018-11-01 2022-11-04 江苏豪森药业集团有限公司 一种细胞周期蛋白依赖性激酶抑制剂的制备方法及其中间体
CN111606889B (zh) * 2019-02-25 2023-03-07 上海翰森生物医药科技有限公司 4-(1-环丙基-1h-吲哚-3-基)-n-苯基嘧啶-2-胺衍生物的制备方法
BR112021022105A2 (pt) * 2019-05-05 2021-12-28 Qilu Regor Therapeutics Inc Inibidores de cdk
CN110305125B (zh) * 2019-06-06 2021-09-03 山东新华制药股份有限公司 5-嘧啶-6-氧-吡唑并吡啶类衍生物及其制备方法和应用
CN112574191B (zh) * 2019-09-29 2024-01-23 南京圣和药业股份有限公司 异噁唑杂环类化合物及其应用
WO2022113003A1 (en) 2020-11-27 2022-06-02 Rhizen Pharmaceuticals Ag Cdk inhibitors
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
EP4323351A1 (en) * 2021-04-12 2024-02-21 A2A Pharmaceuticals, Inc. Compositions and methods for treating cancer
CN113135898B (zh) * 2021-04-15 2022-02-11 中国药科大学 一种抗癌喹喔啉嘧啶胺杂环化合物及其制备方法和应用
CN113264920B (zh) * 2021-05-10 2022-09-02 中国药科大学 一种嘧啶苯并六元环母核的cdk6抑制剂及其制备方法和应用
WO2024051702A1 (zh) * 2022-09-05 2024-03-14 浙江同源康医药股份有限公司 用作cdk4激酶抑制剂的化合物及其应用

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CN104529904B (zh) * 2015-01-09 2016-08-31 苏州明锐医药科技有限公司 玻玛西尼的制备方法
CN106467517B (zh) * 2015-08-14 2019-09-06 正大天晴药业集团股份有限公司 氘修饰的Abemaciclib衍生物

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Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110156754A (zh) * 2018-02-10 2019-08-23 杭州百诚医药科技股份有限公司 一种三取代嘧啶衍生物对蛋白激酶的抑制作用
CN110156754B (zh) * 2018-02-10 2023-10-03 杭州百诚医药科技股份有限公司 一种三取代嘧啶衍生物对蛋白激酶的抑制作用
CN115246822A (zh) * 2021-04-27 2022-10-28 中国科学院上海药物研究所 嘧啶类化合物及其制备方法和用途
CN113248500A (zh) * 2021-06-10 2021-08-13 中国药科大学 氮杂吲哚嘧啶胺杂环化合物及其制备方法和应用

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CN112250669B (zh) 2022-02-25
CN109952295B (zh) 2021-04-06
CN112225724A (zh) 2021-01-15
WO2018045957A1 (zh) 2018-03-15
CN109963842B (zh) 2020-11-03
CN109963842A (zh) 2019-07-02
TWI765908B (zh) 2022-06-01
WO2018045956A1 (zh) 2018-03-15
TW201811771A (zh) 2018-04-01
CN112250669A (zh) 2021-01-22
CN112225724B (zh) 2022-04-29

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