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CN107428758A - 丙烯酸类衍生物、其制备方法及其在医药上的用途 - Google Patents

丙烯酸类衍生物、其制备方法及其在医药上的用途 Download PDF

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Publication number
CN107428758A
CN107428758A CN201680020252.8A CN201680020252A CN107428758A CN 107428758 A CN107428758 A CN 107428758A CN 201680020252 A CN201680020252 A CN 201680020252A CN 107428758 A CN107428758 A CN 107428758A
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alkyl
aryl
heteroaryl
heterocycle
halogen
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CN107428758B (zh
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关东亮
盛首
盛首一
白骅
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Zhejiang Hisun Pharmaceutical Co Ltd
Shanghai Aryl Pharmtech Co Ltd
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Zhejiang Hisun Pharmaceutical Co Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

本发明涉及一种通式(I)所示的丙烯酸类衍生物、其立体异构体、互变异构体或其可药用的盐,它们的制备方法,含有它们的药物组合物,以及它们作为治疗剂,特别是作为选择性雌激素受体下调剂(SERD)的用途,其中通式(I)各取代基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。
CN201680020252.8A 2015-11-12 2016-10-11 丙烯酸类衍生物、其制备方法及其在医药上的用途 Active CN107428758B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201510771111 2015-11-12
CN2015107711117 2015-11-12
PCT/CN2016/101768 WO2017080338A1 (zh) 2015-11-12 2016-10-11 丙烯酸类衍生物、其制备方法及其在医药上的用途

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CN107428758A true CN107428758A (zh) 2017-12-01
CN107428758B CN107428758B (zh) 2020-08-04

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US (1) US10519148B2 (zh)
EP (1) EP3378861B1 (zh)
JP (1) JP6592197B2 (zh)
KR (1) KR102099159B1 (zh)
CN (1) CN107428758B (zh)
CA (1) CA3011391C (zh)
TW (1) TWI615393B (zh)
WO (1) WO2017080338A1 (zh)

Cited By (4)

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Publication number Priority date Publication date Assignee Title
CN109311870A (zh) * 2016-04-01 2019-02-05 芝诺罗耶尔蒂里程碑有限责任公司 雌激素受体调节剂
CN109362222A (zh) * 2016-02-05 2019-02-19 益方生物科技(上海)有限公司 选择性雌激素受体降解物及其用途
WO2021228210A1 (zh) * 2020-05-15 2021-11-18 江苏先声药业有限公司 吡咯烷类化合物及其应用
US11278532B2 (en) 2019-08-06 2022-03-22 Recurium Ip Holdings, Llc Estrogen receptor modulators for treating mutants

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CA3008020C (en) 2015-12-09 2024-02-20 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective estrogen receptor downregulators
TW201803870A (zh) 2016-04-20 2018-02-01 阿斯特捷利康公司 化學化合物
WO2018001232A1 (zh) * 2016-06-29 2018-01-04 浙江海正药业股份有限公司 丙烯酸类衍生物及其制备方法和其在医药上的用途
WO2018019793A1 (en) 2016-07-25 2018-02-01 Astrazeneca Ab N-(2-(4-((1r,3r)-3-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indol-1-yl)phenoxy)ethyl)propan-1-amine derivatives and related compounds as selective down-regulators of the estrogen receptor for treating cancer
CN107814798B (zh) * 2016-09-14 2020-11-03 四川科伦博泰生物医药股份有限公司 3-取代丙烯酸类化合物及其制备方法和用途
SI3640251T1 (sl) 2016-10-24 2022-04-29 Astrazeneca Ab Derivati 6,7,8,9-tetrahidro-3H-pirazolo(4,3-f)izokinolina uporabni v zdravljenju raka
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
EP3565558B1 (en) 2017-01-06 2023-12-06 G1 Therapeutics, Inc. Combination therapy with a serd compound and a cdk4/6 inhibitor for the treatment of cancer
DK3494116T3 (da) 2017-01-30 2020-01-27 Astrazeneca Østrogenreceptormodulatorer
AU2019229256A1 (en) 2018-02-28 2020-09-17 Ferro Therapeutics, Inc. Compounds with ferroptosis inducing activity and methods of their use
US11040964B2 (en) 2019-02-27 2021-06-22 Ferro Therapeutics, Inc. Compounds and methods of use
WO2020238733A1 (zh) 2019-05-24 2020-12-03 浙江海正药业股份有限公司 丙烯酸类衍生物的晶型及其制备方法和用途
CN110746340A (zh) * 2019-11-07 2020-02-04 上海易恩化学技术有限公司 一种5-甲氧基-2-甲基色胺的合成方法
CN116574054A (zh) * 2023-05-15 2023-08-11 南京中医药大学 选择性雌激素受体下调剂化合物、制备方法及用途

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Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109362222A (zh) * 2016-02-05 2019-02-19 益方生物科技(上海)有限公司 选择性雌激素受体降解物及其用途
CN109362222B (zh) * 2016-02-05 2021-03-19 益方生物科技(上海)股份有限公司 选择性雌激素受体降解物及其用途
CN113004273A (zh) * 2016-02-05 2021-06-22 益方生物科技(上海)股份有限公司 选择性雌激素受体降解物及其用途
CN109311870A (zh) * 2016-04-01 2019-02-05 芝诺罗耶尔蒂里程碑有限责任公司 雌激素受体调节剂
US11065234B2 (en) 2016-04-01 2021-07-20 Recurium Ip Holdings, Llc Estrogen receptor modulators
US11065233B2 (en) 2016-04-01 2021-07-20 Recurium Ip Holdings, Llc Estrogen receptor modulators
CN109311870B (zh) * 2016-04-01 2021-09-21 里科瑞尔姆Ip控股有限责任公司 雌激素受体调节剂
CN113717170A (zh) * 2016-04-01 2021-11-30 里科瑞尔姆Ip控股有限责任公司 雌激素受体调节剂
US11278532B2 (en) 2019-08-06 2022-03-22 Recurium Ip Holdings, Llc Estrogen receptor modulators for treating mutants
WO2021228210A1 (zh) * 2020-05-15 2021-11-18 江苏先声药业有限公司 吡咯烷类化合物及其应用
CN115836068A (zh) * 2020-05-15 2023-03-21 先声药业有限公司 吡咯烷类化合物及其应用

Also Published As

Publication number Publication date
US20180291019A1 (en) 2018-10-11
US10519148B2 (en) 2019-12-31
EP3378861A1 (en) 2018-09-26
EP3378861A4 (en) 2019-06-26
TW201716406A (zh) 2017-05-16
CA3011391A1 (en) 2017-05-18
EP3378861B1 (en) 2021-08-04
CN107428758B (zh) 2020-08-04
WO2017080338A1 (zh) 2017-05-18
CA3011391C (en) 2021-02-09
JP2018535216A (ja) 2018-11-29
KR102099159B1 (ko) 2020-04-10
KR20180080245A (ko) 2018-07-11
TWI615393B (zh) 2018-02-21
JP6592197B2 (ja) 2019-10-16

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