AU2017239348B2 - Substituted-indole compounds as estrogen receptor down-regulators - Google Patents

Substituted-indole compounds as estrogen receptor down-regulators Download PDF

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Publication number
AU2017239348B2
AU2017239348B2 AU2017239348A AU2017239348A AU2017239348B2 AU 2017239348 B2 AU2017239348 B2 AU 2017239348B2 AU 2017239348 A AU2017239348 A AU 2017239348A AU 2017239348 A AU2017239348 A AU 2017239348A AU 2017239348 B2 AU2017239348 B2 AU 2017239348B2
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compound
group
cooh
alkyl
pharmaceutically acceptable
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AU2017239348A1 (en
Inventor
Shuhui Chen
Charles Z. Ding
Jiaqiang Dong
Huijun HE
Lihong Hu
Jianyu LU
Tie-Lin Wang
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Luoxin Healthcare Science And Technology Development Beijing Ltd
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Luoxin Healthcare Science And Tech Development Beijing Ltd
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Assigned to SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD., Luoxin Pharmaceutical (Shanghai) Co., Ltd. reassignment SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD. Amend patent request/document other than specification (104) Assignors: LUOXIN BIOTECHNOLOGY (SHANGHAI) CO., LTD, SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.
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Assigned to Luoxin Healthcare Science and Technology Development (Beijing) Ltd. reassignment Luoxin Healthcare Science and Technology Development (Beijing) Ltd. Request for Assignment Assignors: Luoxin Pharmaceutical (Shanghai) Co., Ltd., SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.
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    • 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
    • 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
    • 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
    • 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

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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)
AU2017239348A 2016-03-25 2017-03-24 Substituted-indole compounds as estrogen receptor down-regulators Active AU2017239348B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201610180518.7 2016-03-25
CN201610180518 2016-03-25
CN201610867918.5 2016-09-29
CN201610867918 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
AU2017239348A1 AU2017239348A1 (en) 2018-11-15
AU2017239348B2 true AU2017239348B2 (en) 2020-03-12

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
AU2017239348A Active AU2017239348B2 (en) 2016-03-25 2017-03-24 Substituted-indole compounds as estrogen receptor down-regulators

Country Status (11)

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 (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012037411A2 (en) * 2010-09-16 2012-03-22 Aragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof

Family Cites Families (6)

* 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
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
NZ630124A (en) 2012-03-20 2016-01-29 Seragon Pharmaceuticals Inc Estrogen receptor modulators and uses thereof
KR20160124909A (ko) * 2014-03-13 2016-10-28 에프. 호프만-라 로슈 아게 에스트로겐 수용체 조절제를 함유하는 치료 조합물
KR20160132029A (ko) * 2014-03-13 2016-11-16 에프. 호프만-라 로슈 아게 에스트로젠 수용체 돌연변이체의 조절을 위한 방법 및 조성물

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012037411A2 (en) * 2010-09-16 2012-03-22 Aragon Pharmaceuticals, Inc. Estrogen receptor modulators and uses thereof

Also Published As

Publication number Publication date
CN108884035B (zh) 2020-03-13
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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Legal Events

Date Code Title Description
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE INVENTION TITLE TO READ SUBSTITUTED-INDOLE COMPOUNDS AS ESTROGEN RECEPTOR DOWN-REGULATORS

HB Alteration of name in register

Owner name: LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD.

Free format text: FORMER NAME(S): LUOXIN BIOTECHNOLOGY (SHANGHAI) CO., LTD; SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

Owner name: SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LT

Free format text: FORMER NAME(S): LUOXIN BIOTECHNOLOGY (SHANGHAI) CO., LTD; SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.

FGA Letters patent sealed or granted (standard patent)
PC Assignment registered

Owner name: LUOXIN HEALTHCARE SCIENCE AND TECHNOLOGY DEVELOPMENT (BEIJING) LTD.

Free format text: FORMER OWNER(S): SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD.; LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD.