KR102111792B1 - 에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물 - Google Patents

에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물 Download PDF

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KR102111792B1
KR102111792B1 KR1020187030877A KR20187030877A KR102111792B1 KR 102111792 B1 KR102111792 B1 KR 102111792B1 KR 1020187030877 A KR1020187030877 A KR 1020187030877A KR 20187030877 A KR20187030877 A KR 20187030877A KR 102111792 B1 KR102111792 B1 KR 102111792B1
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KR20180128456A (ko
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젠위 루
찰스 제트. 딩
리홍 후
후이준 허
슈후이 첸
지아창 동
티에-린 왕
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뤄신 바이오테크놀러지 (상하이) 컴퍼니 리미티드
산둥 뤄신 파마슈티컬 그룹 스탁 컴퍼니 리미티드
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Assigned to 뤄신 헬스케어 사이언스 앤드 테크놀로지 디벨롭먼트 (베이징) 리미티드 reassignment 뤄신 헬스케어 사이언스 앤드 테크놀로지 디벨롭먼트 (베이징) 리미티드 권리의 전부이전등록 Assignors: 뤄신 파마슈티컬 (상하이) 컴퍼니 리미티드, 산둥 뤄신 파마슈티컬 그룹 스탁 컴퍼니 리미티드
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/10Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32Antioestrogens
    • 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/06Heterocyclic 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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
KR1020187030877A 2016-03-25 2017-03-24 에스트로겐 수용체 하향 조절제로서의 치환된 인돌 화합물 Active KR102111792B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201610180518.7 2016-03-25
CN201610180518 2016-03-25
CN201610867918 2016-09-29
CN201610867918.5 2016-09-29
PCT/CN2017/078139 WO2017162206A1 (zh) 2016-03-25 2017-03-24 作为雌激素受体降解剂的吲哚并取代哌啶类化合物

Publications (2)

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KR20180128456A KR20180128456A (ko) 2018-12-03
KR102111792B1 true KR102111792B1 (ko) 2020-05-18

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US (1) US10519143B2 (enExample)
EP (1) EP3434668B1 (enExample)
JP (1) JP6790222B2 (enExample)
KR (1) KR102111792B1 (enExample)
CN (1) CN108884035B (enExample)
AU (1) AU2017239348B2 (enExample)
CA (1) CA3018801C (enExample)
ES (1) ES2821407T3 (enExample)
RU (1) RU2722441C2 (enExample)
SG (1) SG11201808363TA (enExample)
WO (1) WO2017162206A1 (enExample)

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CN111032627B (zh) * 2017-09-25 2023-10-20 罗欣健康科技发展(北京)有限公司 一种雌激素受体抑制剂的晶型及其制备方法
JP7571006B2 (ja) 2018-08-17 2024-10-22 ジェネンテック, インコーポレイテッド 乳がんの処置のための診断的および治療的方法
WO2020108154A1 (zh) 2018-11-28 2020-06-04 罗欣药业(上海)有限公司 一种雌激素受体下调剂的盐型、晶型及其制备方法
EP3889133B1 (en) 2018-12-17 2026-01-28 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. 4-[[2-[[5-[1-(1h-indol-2-yl)-2-(phenyl)-1-ethen-1-yl]-2-pyridinyl]oxy]ethyl]amino]-2-butenamide derivatives for the treatment of estrogen receptor positive breast cancer
CN116891461A (zh) * 2022-03-30 2023-10-17 罗欣药业(上海)有限公司 一种serd中间体的合成方法

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TW397821B (en) * 1996-04-19 2000-07-11 American Home Produits Corp 3-[4-(2-phenyl-indole-1-ylmethyl)-phenyl]-acrylamides and 2-phenyl-1-[4-(amino-1-yl-alk-1-ynyl)-benzyl]-1H-indol-5-ol as well as pharmaceutical compositions of estrogenic agents thereof
US20100317635A1 (en) * 2009-06-16 2010-12-16 Endorecherche, Inc. Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators
GB0917571D0 (en) 2009-10-07 2009-11-25 Karobio Ab Novel estrogen receptor ligands
GB2483736B (en) * 2010-09-16 2012-08-29 Aragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
US9499538B2 (en) 2012-03-20 2016-11-22 Seragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof
SG11201607339VA (en) * 2014-03-13 2016-10-28 Hoffmann La Roche Methods and compositions for modulating estrogen receptor mutants
WO2015136016A2 (en) * 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag Therapeutic combinations with estrogen receptor modulators

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AU2017239348A1 (en) 2018-11-15
US10519143B2 (en) 2019-12-31
HK1256936A1 (zh) 2019-10-04
RU2018135203A3 (enExample) 2020-04-27
ES2821407T8 (es) 2022-02-02
EP3434668A4 (en) 2019-08-14
ES2821407T3 (es) 2021-04-26
RU2722441C2 (ru) 2020-06-01
CA3018801A1 (en) 2017-09-28
KR20180128456A (ko) 2018-12-03
JP2019512550A (ja) 2019-05-16
SG11201808363TA (en) 2018-10-30
AU2017239348B2 (en) 2020-03-12
CA3018801C (en) 2020-06-23
EP3434668B1 (en) 2020-08-26
EP3434668A1 (en) 2019-01-30
WO2017162206A1 (zh) 2017-09-28
CN108884035B (zh) 2020-03-13
US20190106414A1 (en) 2019-04-11
JP6790222B2 (ja) 2020-11-25
CN108884035A (zh) 2018-11-23
RU2018135203A (ru) 2020-04-27

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