CN108884035B - 作为雌激素受体下调剂的取代吲哚类化合物 - Google Patents

作为雌激素受体下调剂的取代吲哚类化合物 Download PDF

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Publication number
CN108884035B
CN108884035B CN201780019970.8A CN201780019970A CN108884035B CN 108884035 B CN108884035 B CN 108884035B CN 201780019970 A CN201780019970 A CN 201780019970A CN 108884035 B CN108884035 B CN 108884035B
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pharmaceutically acceptable
acceptable salt
solution
added
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CN108884035A (zh
Inventor
陆剑宇
丁照中
胡利红
贺辉君
陈曙辉
董加强
王铁林
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Luoxin Health Technology Development Beijing Co ltd
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Luoxin Biotechnology Shanghai Co ltd
Shandong Luoxin Pharmaceutical Group Co Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic 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
    • 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
    • A61K31/40—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
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/32—Antioestrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/06—Heterocyclic 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

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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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Indole Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201780019970.8A 2016-03-25 2017-03-24 作为雌激素受体下调剂的取代吲哚类化合物 Active CN108884035B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201610180518 2016-03-25
CN2016101805187 2016-03-25
CN201610867918 2016-09-29
CN2016108679185 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)

Publication Number Publication Date
CN108884035A CN108884035A (zh) 2018-11-23
CN108884035B true CN108884035B (zh) 2020-03-13

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Country Link
US (1) US10519143B2 (cg-RX-API-DMAC7.html)
EP (1) EP3434668B1 (cg-RX-API-DMAC7.html)
JP (1) JP6790222B2 (cg-RX-API-DMAC7.html)
KR (1) KR102111792B1 (cg-RX-API-DMAC7.html)
CN (1) CN108884035B (cg-RX-API-DMAC7.html)
AU (1) AU2017239348B2 (cg-RX-API-DMAC7.html)
CA (1) CA3018801C (cg-RX-API-DMAC7.html)
ES (1) ES2821407T3 (cg-RX-API-DMAC7.html)
RU (1) RU2722441C2 (cg-RX-API-DMAC7.html)
SG (1) SG11201808363TA (cg-RX-API-DMAC7.html)
WO (1) WO2017162206A1 (cg-RX-API-DMAC7.html)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CN113490850B (zh) 2018-08-17 2024-12-06 基因泰克公司 用于治疗乳腺癌的诊断和治疗方法
KR102858291B1 (ko) * 2018-11-28 2025-09-12 뤄신 파마슈티컬 (상하이) 컴퍼니 리미티드 에스트로겐 수용체 하향 조절제의 염 형태와 결정형, 및 이의 제조방법
BR112021011728A8 (pt) * 2018-12-17 2023-01-31 Chia Tai Tianqing Pharmaceutical Group Co Ltd Antagonista do receptor de estrogênio
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

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011042474A1 (en) * 2009-10-07 2011-04-14 Karo Bio Ab Novel estrogen receptor ligands
CN102458404A (zh) * 2009-06-16 2012-05-16 恩多研究公司 以性类固醇前驱物组合选择性雌激素受体调节物治疗热潮红、血管舒缩症状及夜汗的技术
CN103189361A (zh) * 2010-09-16 2013-07-03 亚拉冈制药公司 雌激素受体调节剂及其用途
CN104220426A (zh) * 2012-03-20 2014-12-17 塞拉根制药公司 雌激素受体调节剂及其用途
WO2015136017A1 (en) * 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag 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

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102458404A (zh) * 2009-06-16 2012-05-16 恩多研究公司 以性类固醇前驱物组合选择性雌激素受体调节物治疗热潮红、血管舒缩症状及夜汗的技术
WO2011042474A1 (en) * 2009-10-07 2011-04-14 Karo Bio Ab Novel estrogen receptor ligands
CN103189361A (zh) * 2010-09-16 2013-07-03 亚拉冈制药公司 雌激素受体调节剂及其用途
CN104220426A (zh) * 2012-03-20 2014-12-17 塞拉根制药公司 雌激素受体调节剂及其用途
WO2015136017A1 (en) * 2014-03-13 2015-09-17 F. Hoffmann-La Roche Ag 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

Also Published As

Publication number Publication date
AU2017239348B2 (en) 2020-03-12
JP6790222B2 (ja) 2020-11-25
US10519143B2 (en) 2019-12-31
EP3434668A4 (en) 2019-08-14
ES2821407T8 (es) 2022-02-02
RU2018135203A3 (cg-RX-API-DMAC7.html) 2020-04-27
CA3018801A1 (en) 2017-09-28
CN108884035A (zh) 2018-11-23
KR20180128456A (ko) 2018-12-03
ES2821407T3 (es) 2021-04-26
RU2018135203A (ru) 2020-04-27
HK1256936A1 (zh) 2019-10-04
US20190106414A1 (en) 2019-04-11
AU2017239348A1 (en) 2018-11-15
EP3434668B1 (en) 2020-08-26
KR102111792B1 (ko) 2020-05-18
EP3434668A1 (en) 2019-01-30
RU2722441C2 (ru) 2020-06-01
SG11201808363TA (en) 2018-10-30
CA3018801C (en) 2020-06-23
JP2019512550A (ja) 2019-05-16
WO2017162206A1 (zh) 2017-09-28

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