KR102046415B1 - 항암 활성을 갖는 7-α-[9-(4,4,5,5,5-펜타플루오로펜틸설피닐)노닐]-에스트라-1,3,5(10)-트리엔-3,17β-디올의 에스테르 유도체 및 그의 제조 방법 - Google Patents

항암 활성을 갖는 7-α-[9-(4,4,5,5,5-펜타플루오로펜틸설피닐)노닐]-에스트라-1,3,5(10)-트리엔-3,17β-디올의 에스테르 유도체 및 그의 제조 방법 Download PDF

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KR102046415B1
KR102046415B1 KR1020157033007A KR20157033007A KR102046415B1 KR 102046415 B1 KR102046415 B1 KR 102046415B1 KR 1020157033007 A KR1020157033007 A KR 1020157033007A KR 20157033007 A KR20157033007 A KR 20157033007A KR 102046415 B1 KR102046415 B1 KR 102046415B1
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South Korea
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compound
ethylpyridine
formula
methyl
substituent
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Korean (ko)
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KR20150143842A (ko
Inventor
야퀴 지아오
지우청 왕
런러 후
Original Assignee
시안 리방 파마슈티컬 테크놀로지 컴퍼니 리미티드
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    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074—Esters
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • 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
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051—Estrane derivatives
    • C07J1/0066—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007—Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020157033007A 2013-04-18 2013-04-18 항암 활성을 갖는 7-α-[9-(4,4,5,5,5-펜타플루오로펜틸설피닐)노닐]-에스트라-1,3,5(10)-트리엔-3,17β-디올의 에스테르 유도체 및 그의 제조 방법 Expired - Fee Related KR102046415B1 (ko)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/CN2013/074363 WO2014169462A1 (zh) 2013-04-18 2013-04-18 具有抗癌活性的7-α-[9-(4,4,5,5,-五氟戊基亚硫酰基)壬基]-雌甾-1,3,5(10)-三烯-3,17β-二醇的酯类衍生物及其制备方法

Publications (2)

Publication Number Publication Date
KR20150143842A KR20150143842A (ko) 2015-12-23
KR102046415B1 true KR102046415B1 (ko) 2019-12-02

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KR1020157033007A Expired - Fee Related KR102046415B1 (ko) 2013-04-18 2013-04-18 항암 활성을 갖는 7-α-[9-(4,4,5,5,5-펜타플루오로펜틸설피닐)노닐]-에스트라-1,3,5(10)-트리엔-3,17β-디올의 에스테르 유도체 및 그의 제조 방법

Country Status (8)

Country Link
US (1) US20160060288A1 (https=)
EP (1) EP2987799B1 (https=)
JP (1) JP6356218B2 (https=)
KR (1) KR102046415B1 (https=)
CN (1) CN104936971B (https=)
AU (1) AU2013386732B2 (https=)
CA (1) CA2909418A1 (https=)
WO (1) WO2014169462A1 (https=)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2014169456A1 (zh) * 2013-04-18 2014-10-23 西安力邦医药科技有限责任公司 7-α-[9-(4,4,5,5,5-五氟戊基亚硫酰基)壬基]-雌甾-1,3,5(10)-三烯-3,17β-二醇及其衍生物的用途
JP7384903B2 (ja) * 2018-05-24 2023-11-21 ケーアイ ファーマシューティカルズ，リミテッド・ライアビリティ・カンパニー フルベストラントのプロドラッグ
EP4061376A4 (en) * 2019-11-24 2024-03-13 Kashiv Biosciences, LLC Prodrugs of fulvestrant

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4218743A1 (de) * 1992-06-04 1993-12-09 Schering Ag Verfahren zur Herstellung C(7)-substituierter Estra-1,3,5(10)-triene sowie neue Ausgangsprodukte für dieses Verfahren
WO2005105823A1 (fr) * 2004-04-28 2005-11-10 Jiangsu Hansen Pharmaceutical Co., Ltd. Derives steroidiens
US20060030552A1 (en) * 2004-07-27 2006-02-09 Macdonald Peter L Process for the preparation of 7alpha-alkylated 19-norsteroids

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NL7613248A (nl) * 1976-11-26 1978-05-30 Akzo Nv Werkwijze voor het bereiden van nieuwe steroid- esters.
GB8327256D0 (en) * 1983-10-12 1983-11-16 Ici Plc Steroid derivatives
US5183514A (en) 1991-04-01 1993-02-02 Texaco Chemical Company Process for dissolving or removing rigid polyurethane foam by contacting with 1,2-dimethyl imidazole
IL112778A0 (en) * 1994-03-04 1995-05-26 Merck & Co Inc Substituted heterocycles, their preparation and pharmaceutical compositions containing them
DE19635525A1 (de) * 1996-08-20 1998-02-26 Schering Ag 7alpha-(xi-Aminoalkyl)-estratriene, Verfahren zu deren Herstellung, pharmazeutische Präparate, die diese 7alpha(xi-Aminoalkyl-estratriene enthalten sowie deren Verwendung zur Herstellung von Arzneimitteln
AR015500A1 (es) * 1997-12-23 2001-05-02 Schering Ag 11 BETA-HALoGENO-ESTRATRIENOS SUSTITUIDOS EN 7 ALFA, PROCEDIMIENTO PARA ELABORAR PREPARADOS FARMACEUTICOS QUE CONTIENEN TALES 11 BETA-HALOGENO-ESTRATRIENOSSUSTITUIDOS EN 7 ALFA, ASI COMO SU UTILIZACION EN LA ELABORACION DE MEDICAMENTOS.
GB0000313D0 (en) 2000-01-10 2000-03-01 Astrazeneca Uk Ltd Formulation
JP2005524630A (ja) * 2002-01-14 2005-08-18 ノルディック・ビオサイエンス・エー／エス エストロゲン受容体を介する軟骨破壊の抑制
US10174070B2 (en) * 2005-09-30 2019-01-08 Endece Llc 6-substituted estradiol derivatives and methods of use
JP5256042B2 (ja) * 2005-11-22 2013-08-07 インサイト・コーポレイション 癌の処置のための併用療法
JP2011514349A (ja) * 2008-03-07 2011-05-06 サイドース・エルエルシー フルベストラント配合物
CN102600073B (zh) * 2012-03-31 2014-01-01 莱普德制药有限公司 以乳酸酯为基础的氟维司群或其衍生物油性制剂及其制备方法
WO2014169456A1 (zh) * 2013-04-18 2014-10-23 西安力邦医药科技有限责任公司 7-α-[9-(4,4,5,5,5-五氟戊基亚硫酰基)壬基]-雌甾-1,3,5(10)-三烯-3,17β-二醇及其衍生物的用途
US9271990B2 (en) * 2014-02-14 2016-03-01 Fresenius Kabi Usa, Llc Fulvestrant formulations

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4218743A1 (de) * 1992-06-04 1993-12-09 Schering Ag Verfahren zur Herstellung C(7)-substituierter Estra-1,3,5(10)-triene sowie neue Ausgangsprodukte für dieses Verfahren
WO2005105823A1 (fr) * 2004-04-28 2005-11-10 Jiangsu Hansen Pharmaceutical Co., Ltd. Derives steroidiens
US20060030552A1 (en) * 2004-07-27 2006-02-09 Macdonald Peter L Process for the preparation of 7alpha-alkylated 19-norsteroids

Also Published As

Publication number Publication date
US20160060288A1 (en) 2016-03-03
EP2987799A4 (en) 2016-10-05
CN104936971B (zh) 2017-10-13
KR20150143842A (ko) 2015-12-23
CA2909418A1 (en) 2014-10-23
EP2987799B1 (en) 2020-04-08
EP2987799A1 (en) 2016-02-24
WO2014169462A1 (zh) 2014-10-23
CN104936971A (zh) 2015-09-23
AU2013386732B2 (en) 2018-10-18
JP2016517849A (ja) 2016-06-20
AU2013386732A1 (en) 2015-09-24
JP6356218B2 (ja) 2018-07-11

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