CN109963844A - 一类抑制并降解酪氨酸蛋白激酶alk的化合物 - Google Patents

一类抑制并降解酪氨酸蛋白激酶alk的化合物 Download PDF

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CN109963844A
CN109963844A CN201880004044.8A CN201880004044A CN109963844A CN 109963844 A CN109963844 A CN 109963844A CN 201880004044 A CN201880004044 A CN 201880004044A CN 109963844 A CN109963844 A CN 109963844A
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substituent group
alkyl
integer
independently selected
compound
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CN109963844B (zh
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舒永志
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Suzhou Yongmei Pharmaceutical Technology Co.,Ltd.
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Shanghai Meizer Pharmaceuticals Co ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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

本发明提供了一类抑制并降解酪氨酸蛋白激酶ALK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间变性淋巴瘤激酶(ALK)抑制活性,可以用于制备治疗间ALK活性相关的疾病的药物。

Description

PCT国内申请,说明书已公开。

Claims (10)

  1. PCT国内申请,权利要求书已公开。
CN201880004044.8A 2017-09-03 2018-09-02 一类抑制并降解酪氨酸蛋白激酶alk的化合物 Active CN109963844B (zh)

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CN2017107830670 2017-09-03
CN201710783067.0A CN109422733A (zh) 2017-09-03 2017-09-03 一类抑制并降解酪氨酸蛋白激酶alk的化合物
PCT/CN2018/103709 WO2019042444A1 (zh) 2017-09-03 2018-09-02 一类抑制并降解酪氨酸蛋白激酶alk的化合物

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CN201880004044.8A Active CN109963844B (zh) 2017-09-03 2018-09-02 一类抑制并降解酪氨酸蛋白激酶alk的化合物

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Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022089400A1 (zh) * 2020-10-26 2022-05-05 上海美志医药科技有限公司 靶向降解Btk的化合物及其抗肿瘤用途

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
KR20210003804A (ko) * 2018-04-13 2021-01-12 아비나스 오퍼레이션스, 인코포레이티드 세레브론 리간드 및 이를 포함하는 2작용성 화합물
CN110684015A (zh) * 2018-07-06 2020-01-14 四川大学 靶向alk的protac及其应用
WO2020041331A1 (en) 2018-08-20 2020-02-27 Arvinas Operations, Inc. Proteolysis targeting chimeric (protac) compound with e3 ubiquitin ligase binding activity and targeting alpha-synuclein protein for treating neurodegenerative diseases
JP7426124B2 (ja) * 2019-06-12 2024-02-01 シャンハイテック ユニバーシティ Alkタンパク質レギュレーター、及びその抗腫瘍における使用
US20220306659A1 (en) * 2019-08-23 2022-09-29 Beijing Tide Pharmaceutical Co., Ltd. Compound inhibiting and inducing degradation of egfr and alk
US20230265116A1 (en) * 2020-07-16 2023-08-24 Beigene, Ltd. Degradation of (egfr) by conjugation of egfr inhibitors with e3 ligase ligand and methods of use
CN111892578B (zh) * 2020-08-03 2023-10-20 沈阳药科大学 一种靶向降解黏着斑激酶的化合物及应用
WO2022171123A1 (en) * 2021-02-10 2022-08-18 Beigene, Ltd. Egfr degraders and methods of use
WO2022242725A1 (zh) * 2021-05-19 2022-11-24 和径医药科技(上海)有限公司 一类新型蛋白降解剂及其应用
EP4359403A1 (en) * 2021-06-21 2024-05-01 BeiGene Switzerland GmbH (r) -glutarimide crbn ligands and methods of use
KR20240029036A (ko) 2021-06-25 2024-03-05 징 메디슨 테크놀로지 (상하이) 엘티디. 단백질 억제제 또는 분해제, 이를 포함하는 약학적 조성물 및 의학적 용도
CN113735828B (zh) * 2021-09-07 2022-10-28 南方医科大学 一种靶向降解egfr的化合物及其制备方法和应用

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015081813A1 (zh) * 2013-12-03 2015-06-11 上海翰森生物医药科技有限公司 具有alk抑制活性的化合物及其制备与用途
CN104876914A (zh) * 2014-02-28 2015-09-02 山东轩竹医药科技有限公司 嘧啶衍生物类间变性淋巴瘤激酶抑制剂
CN106146468A (zh) * 2015-04-17 2016-11-23 杭州雷索药业有限公司 吡啶酮类蛋白激酶抑制剂
WO2016192132A1 (zh) * 2015-06-04 2016-12-08 湖北生物医药产业技术研究院有限公司 作为alk抑制剂的嘧啶衍生物
WO2017079267A1 (en) * 2015-11-02 2017-05-11 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2016013563A (es) * 2014-04-14 2017-05-09 Arvinas Inc Moduladores de la proteolisis basados en imida y metodos de uso asociados.
CN106336382B (zh) * 2015-07-06 2022-04-05 杭州雷索药业有限公司 4-饱和环基取代的苯胺类蛋白激酶抑制剂
WO2017011371A1 (en) * 2015-07-10 2017-01-19 Arvinas, Inc Mdm2-based modulators of proteolysis and associated methods of use
KR101825065B1 (ko) * 2016-05-24 2018-02-05 한국화학연구원 Alk 단백질의 분해를 유도하는 약학적 조성물 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물
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
CN109516989B (zh) * 2017-09-17 2021-12-31 上海美志医药科技有限公司 一类抑制并降解cdk的化合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015081813A1 (zh) * 2013-12-03 2015-06-11 上海翰森生物医药科技有限公司 具有alk抑制活性的化合物及其制备与用途
CN104876914A (zh) * 2014-02-28 2015-09-02 山东轩竹医药科技有限公司 嘧啶衍生物类间变性淋巴瘤激酶抑制剂
CN106146468A (zh) * 2015-04-17 2016-11-23 杭州雷索药业有限公司 吡啶酮类蛋白激酶抑制剂
WO2016192132A1 (zh) * 2015-06-04 2016-12-08 湖北生物医药产业技术研究院有限公司 作为alk抑制剂的嘧啶衍生物
WO2017079267A1 (en) * 2015-11-02 2017-05-11 Yale University Proteolysis targeting chimera compounds and methods of preparing and using same

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022089400A1 (zh) * 2020-10-26 2022-05-05 上海美志医药科技有限公司 靶向降解Btk的化合物及其抗肿瘤用途

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WO2019042444A1 (zh) 2019-03-07
CN109963844B (zh) 2022-08-12
CN109422733A (zh) 2019-03-05
US20200199106A1 (en) 2020-06-25
US11485726B2 (en) 2022-11-01

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