CN104936971B - 具有抗癌活性的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‑二醇的酯类衍生物及其制备方法 - Google Patents

具有抗癌活性的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‑二醇的酯类衍生物及其制备方法 Download PDF

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CN104936971B
CN104936971B CN201380069374.2A CN201380069374A CN104936971B CN 104936971 B CN104936971 B CN 104936971B CN 201380069374 A CN201380069374 A CN 201380069374A CN 104936971 B CN104936971 B CN 104936971B
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substituent
formula
carbon
enoyl
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CN104936971A (zh
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焦亚奇
王九成
胡忍乐
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Xian Libang Pharmaceutical Technology Co Ltd
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Xian Libang Pharmaceutical Technology Co Ltd
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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
    • 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
    • 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

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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)
CN201380069374.2A 2013-04-18 2013-04-18 具有抗癌活性的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‑二醇的酯类衍生物及其制备方法 Active CN104936971B (zh)

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
CN104936971A CN104936971A (zh) 2015-09-23
CN104936971B true CN104936971B (zh) 2017-10-13

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CN201380069374.2A Active CN104936971B (zh) 2013-04-18 2013-04-18 具有抗癌活性的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‑二醇的酯类衍生物及其制备方法

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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4212864A (en) * 1976-11-26 1980-07-15 Akzona Incorporated Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same
CN102753564A (zh) * 2009-11-30 2012-10-24 安德斯有限责任公司 6-取代的雌二醇衍生物及其使用方法

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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
DE4218743C2 (de) * 1992-06-04 2001-10-25 Schering Ag Verfahren zur Herstellung C(7)-substituierter Estra-1,3,5(10)-triene sowie neue Ausgangsprodukte für dieses Verfahren
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
CN100395259C (zh) * 2004-04-28 2008-06-18 江苏豪森药业股份有限公司 甾体类衍生物
US7790910B2 (en) * 2004-07-27 2010-09-07 Sicor Inc. Process for the preparation of 7α-alkylated 19-norsteroids
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 (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4212864A (en) * 1976-11-26 1980-07-15 Akzona Incorporated Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same
CN102753564A (zh) * 2009-11-30 2012-10-24 安德斯有限责任公司 6-取代的雌二醇衍生物及其使用方法

Also Published As

Publication number Publication date
US20160060288A1 (en) 2016-03-03
EP2987799A4 (en) 2016-10-05
KR20150143842A (ko) 2015-12-23
CA2909418A1 (en) 2014-10-23
EP2987799B1 (en) 2020-04-08
EP2987799A1 (en) 2016-02-24
KR102046415B1 (ko) 2019-12-02
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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