CN114829342A - 一种蛋白降解剂化合物的制备方法和应用 - Google Patents

一种蛋白降解剂化合物的制备方法和应用 Download PDF

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CN114829342A
CN114829342A CN202080087926.2A CN202080087926A CN114829342A CN 114829342 A CN114829342 A CN 114829342A CN 202080087926 A CN202080087926 A CN 202080087926A CN 114829342 A CN114829342 A CN 114829342A
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alkyl
compound
radical
pharmaceutically acceptable
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陆洪福
邢唯强
齐保建
彭建彪
郭海兵
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Shanghai Jiyu Pharmaceutical Technology Co ltd
Jiangxi Jemincare Group Co Ltd
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Shanghai Jiyu Pharmaceutical Technology Co ltd
Jiangxi Jemincare Group Co Ltd
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • 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
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    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

提供一种蛋白降解剂化合物的制备方法和应用，具体地，提供式(Ⅰ)所示化合物及其药效上可接受的盐，以及该化合物作为雄激素受体(AR)降解的应用。

Description

PCT国内申请，说明书已公开。

Claims (24)

  1. PCT国内申请，权利要求书已公开。
CN202080087926.2A 2019-12-23 2020-12-23 一种蛋白降解剂化合物的制备方法和应用 Pending CN114829342A (zh)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
CN2019113426490 2019-12-23
CN201911342649 2019-12-23
CN2020102006826 2020-03-20
CN202010200682 2020-03-20
CN202010496353 2020-06-03
CN2020104963530 2020-06-03
CN202011486334 2020-12-16
CN2020114863346 2020-12-16
PCT/CN2020/138572 WO2021129653A1 (zh) 2019-12-23 2020-12-23 一种蛋白降解剂化合物的制备方法和应用

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CN114829342A true CN114829342A (zh) 2022-07-29

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CN202011545626.2A Active CN113087704B (zh) 2019-12-23 2020-12-23 一种蛋白降解剂化合物的制备方法和应用

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US (1) US20230111119A1 (zh)
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CN (2) CN114829342A (zh)
AU (1) AU2020414151A1 (zh)
BR (1) BR112022012385A2 (zh)
CA (1) CA3162523A1 (zh)
CL (1) CL2022001724A1 (zh)
CO (1) CO2022010305A2 (zh)
EC (1) ECSP22056811A (zh)
IL (1) IL294225A (zh)
JO (1) JOP20220159A1 (zh)
MX (1) MX2022007885A (zh)
PE (1) PE20230114A1 (zh)
TW (1) TWI755992B (zh)
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CN118638043A (zh) 2019-12-19 2024-09-13 阿尔维纳斯运营股份有限公司 用于雄激素受体的靶向降解的化合物和方法
EP4146642A1 (en) 2020-05-09 2023-03-15 Arvinas Operations, Inc. Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
CN113801098B (zh) 2020-06-12 2023-05-30 上海济煜医药科技有限公司 酞嗪酮类化合物及其制备方法和医药用途
US12097261B2 (en) 2021-05-07 2024-09-24 Kymera Therapeutics, Inc. CDK2 degraders and uses thereof
EP4367112A1 (en) 2021-07-09 2024-05-15 Plexium, Inc. Aryl compounds and pharmaceutical compositions that modulate ikzf2
WO2024002289A1 (en) * 2022-06-30 2024-01-04 Anhorn Medicines Co., Ltd. Protein degradation compounds and methods of use
WO2024012570A1 (zh) * 2022-07-15 2024-01-18 西藏海思科制药有限公司 一种含氮杂环衍生物及其组合物和药学上的应用
US11957759B1 (en) 2022-09-07 2024-04-16 Arvinas Operations, Inc. Rapidly accelerated fibrosarcoma (RAF) degrading compounds and associated methods of use

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CN107428734A (zh) * 2015-01-20 2017-12-01 阿尔维纳斯股份有限公司 用于雄激素受体的靶向降解的化合物和方法
WO2018098280A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use
WO2018098275A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use
CN110506039A (zh) * 2016-10-11 2019-11-26 阿尔维纳斯股份有限公司 用于雄激素受体靶向降解的化合物和方法

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US20180228907A1 (en) * 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same

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CN107428734A (zh) * 2015-01-20 2017-12-01 阿尔维纳斯股份有限公司 用于雄激素受体的靶向降解的化合物和方法
CN110506039A (zh) * 2016-10-11 2019-11-26 阿尔维纳斯股份有限公司 用于雄激素受体靶向降解的化合物和方法
WO2018098280A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use
WO2018098275A1 (en) * 2016-11-22 2018-05-31 Dana-Farber Cancer Institute, Inc. Degradation of bruton's tyrosine kinase (btk) by conjugation of btk inhibitors with e3 ligase ligand and methods of use

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MX2022007885A (es) 2022-09-19
US20230111119A1 (en) 2023-04-13
KR20220120629A (ko) 2022-08-30
CA3162523A1 (en) 2021-07-01
ECSP22056811A (es) 2022-12-30
BR112022012385A2 (pt) 2022-08-30
JP2023508097A (ja) 2023-02-28
ZA202208051B (en) 2023-11-29
AU2020414151A1 (en) 2022-08-25
IL294225A (en) 2022-08-01
TWI755992B (zh) 2022-02-21
CO2022010305A2 (es) 2022-08-09
JOP20220159A1 (ar) 2023-01-30
EP4083020A4 (en) 2024-01-24
CN113087704A (zh) 2021-07-09
WO2021129653A1 (zh) 2021-07-01
EP4083020A1 (en) 2022-11-02
TW202128662A (zh) 2021-08-01
CN113087704B (zh) 2023-09-08
CL2022001724A1 (es) 2023-02-24
PE20230114A1 (es) 2023-01-27

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