CN114341128A - 双功能蛋白降解靶向嵌合体类化合物及其制备方法和医药用途 - Google Patents

双功能蛋白降解靶向嵌合体类化合物及其制备方法和医药用途 Download PDF

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CN114341128A
CN114341128A CN202180005070.4A CN202180005070A CN114341128A CN 114341128 A CN114341128 A CN 114341128A CN 202180005070 A CN202180005070 A CN 202180005070A CN 114341128 A CN114341128 A CN 114341128A
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alkyl
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radical
cycloalkyl
halogen
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CN114341128B (zh
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司聚同
姜美锋
张丽云
樊平平
刘涛
刘备
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Ancureall Pharmaceutical Shanghai Co Ltd
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Abstract

一种双功能蛋白降解靶向嵌合体类化合物及其制备方法和医药用途。具体而言，涉及一种通式(I)所示的化合物及其制备方法，以及其用于降解和抑制FLT3酪氨酸蛋白激酶的用途，特别是在预防和/或治疗人类疾病包括癌症中的用途。所述化合物一端含有与E3泛素连接酶结合的基团，另一端含有与FLT3酪氨酸蛋白激酶结合的基团，通过连接子相连接，能够使得FLT3位于泛素连接酶的附近，其表现出广泛的药理活性与降解和抑制FLT3酪氨酸蛋白激酶的双功能相一致。其中，通式(I)中各基团的定义与说明书中的定义相同。

Description

PCT国内申请，说明书已公开。

Claims (21)

  1. PCT国内申请，权利要求书已公开。
CN202180005070.4A 2020-07-24 2021-07-22 双功能蛋白降解靶向嵌合体类化合物及其制备方法和医药用途 Active CN114341128B (zh)

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TW202346293A (zh) * 2022-04-29 2023-12-01 大陸商四川海思科製藥有限公司 含氮雜環衍生物及其组合物和藥學上的應用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106458993A (zh) * 2014-04-14 2017-02-22 阿尔维纳斯股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
CN107176951A (zh) * 2016-03-11 2017-09-19 恩瑞生物医药科技（上海）有限公司 一种脲类化合物、其制备方法及其医药用途
WO2018237026A1 (en) * 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS
WO2019199816A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same

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CA2979070A1 (en) * 2015-03-18 2016-09-22 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
US20180147202A1 (en) * 2015-06-05 2018-05-31 Arvinas, Inc. TANK-BINDING KINASE-1 PROTACs AND ASSOCIATED METHODS OF USE
CN112574174B (zh) * 2019-09-27 2021-12-07 恩瑞生物医药科技（上海）有限公司 蛋白降解靶向嵌合体类化合物及其制备方法和医药用途

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106458993A (zh) * 2014-04-14 2017-02-22 阿尔维纳斯股份有限公司 基于酰亚胺的蛋白水解调节剂和相关使用方法
CN107176951A (zh) * 2016-03-11 2017-09-19 恩瑞生物医药科技（上海）有限公司 一种脲类化合物、其制备方法及其医药用途
WO2018237026A1 (en) * 2017-06-20 2018-12-27 C4 Therapeutics, Inc. N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS
WO2019199816A1 (en) * 2018-04-13 2019-10-17 Arvinas Operations, Inc. Cereblon ligands and bifunctional compounds comprising the same

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