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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CN201680020252.8A
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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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/4353—Heterocyclic 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
    • A61K31/437—Heterocyclic 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
    • 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
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

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***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)

* Cited by examiner, † Cited by third party
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CN109311870A (zh) * 2016-04-01 2019-02-05 芝诺罗耶尔蒂里程碑有限责任公司 ***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***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

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2018007079A (es) 2015-12-09 2018-11-12 The Board Of Trustees Of Univ Of Illinois Reguladores a la baja del receptor de estrogeno selectivo de benzotiofeno.
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
US10149839B2 (en) 2016-07-25 2018-12-11 Astrazeneca Ab Chemical compounds
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
ES2907759T3 (es) 2016-10-24 2022-04-26 Astrazeneca Ab Derivados de 6,7,8,9-tetrahidro-3h-pirazolo[4,3-f]isoquinolina útiles en el tratamiento del cáncer
WO2018081168A2 (en) 2016-10-24 2018-05-03 The Board Of Trustees Of The University Of Illinois Benzothiophene-based selective mixed estrogen receptor downregulators
AU2018205262A1 (en) 2017-01-06 2019-07-11 G1 Therapeutics, Inc. Combination therapy for the treatment of cancer
EP3494116B1 (en) 2017-01-30 2019-10-23 Astrazeneca AB Estrogen receptor modulators
WO2019168999A1 (en) 2018-02-28 2019-09-06 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
US20220220107A1 (en) * 2019-05-24 2022-07-14 Zhejiang Hisun Pharmaceutical Co., Ltd. Crystal forms of acrylic acid derivatives, preparation method therefor and use thereof
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

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WO2005070930A2 (en) * 2004-01-23 2005-08-04 Chiron Corporation Tetrahydrocarboline compounds as anticancer agents
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CN109362222A (zh) * 2016-02-05 2019-02-19 益方生物科技（上海）有限公司 选择性***受体降解物及其用途

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GB2483736B (en) 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
AU2014358850A1 (en) 2013-12-06 2016-06-16 F. Hoffmann-La Roche Ag Estrogen receptor modulator for the treatment of locally advanced or metastatic estrogen receptor positive breast cancer

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WO2005070930A2 (en) * 2004-01-23 2005-08-04 Chiron Corporation Tetrahydrocarboline compounds as anticancer agents
US20100003324A1 (en) * 2008-07-03 2010-01-07 Osteogenex Inc. Vinpocetine and eburn amonine derivatives for promoting bone growth
WO2014191726A1 (en) * 2013-05-28 2014-12-04 Astrazeneca Ab Chemical compounds
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SAVI,CHRIS DE等: "Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic Acid (AZD9496),...", 《JOURNAL OF MEDICINAL CHEMISTRY》 *

Cited By (10)

* 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***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***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***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 ***受体调节剂
US11065233B2 (en) 2016-04-01 2021-07-20 Recurium Ip Holdings, Llc Estrogen receptor modulators
US11065234B2 (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 ***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 ***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

Also Published As

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

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