KR950008531A - 11-벤즈알독심-17β-메톡시-17α-메톡시메틸-에스트라디엔 유도체, 이의 제조방법 및 이를 함유하는 약제 - Google Patents

11-벤즈알독심-17β-메톡시-17α-메톡시메틸-에스트라디엔 유도체, 이의 제조방법 및 이를 함유하는 약제 Download PDF

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KR950008531A
KR950008531A KR1019940020993A KR19940020993A KR950008531A KR 950008531 A KR950008531 A KR 950008531A KR 1019940020993 A KR1019940020993 A KR 1019940020993A KR 19940020993 A KR19940020993 A KR 19940020993A KR 950008531 A KR950008531 A KR 950008531A
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phenyl
methoxymethyl
methoxy
estra
dien
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KR1019940020993A
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KR100190775B1 (ko
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슈베르트 게르트
카우프만 귄터
소벡 로타르
오에텔 미카엘
엘거 발터
쿠리쉬코 아나톨리
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디터 타우베르트,칼-하인츠 비티히
예나파름 게엠베하
칼-하인츠 비티히
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0077—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom
    • C07J41/0083—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 substituted in position 11-beta by a carbon atom, further substituted by a group comprising at least one further carbon atom substituted in position 11-beta by an optionally substituted phenyl group not further condensed with other rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • 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
    • A61P5/36—Antigestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)

Abstract

본 발명은 하기 일반식(Ⅰ)의 신규 11-벤즈알독심-에스트라-디엔 유도체 및 약제학적으로 허용가능한 이의 염, 이의 제조방법 및 이를 함유하는 약제에 관한 것이다.
상기 식에서, Z는 -CO-CH3, -CO-O-C2H5, -CO-NH-페닐, -CO-NH-C2H5, -CO-C2H5, -CH3또는 CO-페닐이다.
전술한 화합물은 강한 항게스타겐성 효과와 감소된 글루코코르티코이드 활성을 나타낸다.

Description

11-벤즈알독심-17β-메톡시-17α-메톡시메틸-에스트라디엔 유도체, 이의 제조 방법 및 이를 함유하는 약제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (4)

  1. 하기 일반식(Ⅰ)의 11β-벤즈알독심-에스트라-4, 9-디엔유도체 및 약제학적으로 허용가능한 이의 염.
    상기 식에서, Z는 -CO-CH3, -CO-O-C2H5, -CO-NH-페닐, -CO-NH-C2H|5, -CO-C2H5, -CH3또는 CO-페닐이다.
  2. 제1항에 있어서, 11β-〔4-(아세톡시미노메틸)페닐〕-17β-메톡시-17α-메톡시메틸-에스트라-4, 9-디엔-3-온, 11β-{4-〔(아세톡시카보닐)옥시미노메틸〕페닐}-17β-메톡시-17α-메톡시메틸-에스트라-4, 9-디엔-3-온, 11β-{4-〔(에틸아미노카보닐)옥시미노메틸〕페닐}-17β-메톡시-17α-메톡시메틸-에스트라-4, 9-디엔-3-온, 17β-메톡시-17α-메톡시메틸-11β-{4-〔(페닐아미노카보닐)옥시미노메틸〕페닐}-에스트라-4, 9-디엔-3-온, 11β-〔4-(프로피오닐옥시미노메틸)페닐〕-17β-메톡시-17α-메톡시메틸-에스트라-4, 9-디엔-3-온, 11β-〔4-(메틸옥시미노메틸)페닐〕-17β-하이드록시-17α-메톡시메틸-에스트라-4, 9-디엔-3-온 및 11β-〔4-(벤조일옥시미노메틸)페닐〕-17β-하이드록시-17α-메톡시메틸-에스트라-4, 9-디엔-3-온인 화합물.
  3. 하기 구조식(Ⅱ)의 화합물을 일반적으로 공지된 방법으로 에스테르화 또는 에테르화하고, 필요한 경우, 염으로 전환시킴을 특징으로 하여, 제1항에 다른 일반식(Ⅰ)의 화합물 및 약제학적으로 허용가능한 이의 염을 제조하는 방법.
    상기 식에서, Z는 -CO-CH3, -CO-O-C2H5, -CO-NH-페닐, -CO-NH-C2H5, -CO-C2H5, -CH3또는 CO-페닐이다.
  4. 제1항 또는 제2항에 따른 화합물 하나 이상을 함유함을 특징으로 하는 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940020993A 1993-09-20 1994-08-25 11베타-벤즈알독심-에스트라-4,9-디엔유도체, 이의 제조방법 및 이를 함유하는 약제학적 조성물 KR100190775B1 (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DEP4332284.0 1993-09-20
DE4332284A DE4332284C2 (de) 1993-09-20 1993-09-20 11-Benzaldoxim-17beta-methoxy-17alpha-methoxymethyl-estradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel

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KR950008531A true KR950008531A (ko) 1995-04-19
KR100190775B1 KR100190775B1 (ko) 1999-06-01

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EP (1) EP0648779B1 (ko)
JP (1) JP2696672B2 (ko)
KR (1) KR100190775B1 (ko)
AT (1) ATE149513T1 (ko)
AU (1) AU682373B2 (ko)
CA (1) CA2130515C (ko)
CZ (1) CZ289801B6 (ko)
DE (2) DE4332284C2 (ko)
DK (1) DK0648779T3 (ko)
ES (1) ES2102144T3 (ko)
FI (1) FI112948B (ko)
GR (1) GR3023644T3 (ko)
HU (1) HU219399B (ko)
NO (1) NO304988B1 (ko)
NZ (1) NZ264228A (ko)
PL (1) PL179460B1 (ko)
RU (1) RU2130944C1 (ko)
SK (1) SK280315B6 (ko)
UA (1) UA39101C2 (ko)

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DE4332283A1 (de) * 1993-09-20 1995-04-13 Jenapharm Gmbh Neue 11-Benzaldoximestradien-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende Arzneimittel
US5576310A (en) * 1994-09-20 1996-11-19 Jenapharm Gmbh 11-benzaldoxime-17β-methoxy-17α-methoxymethyl-estrasdiene derivatives, methods for their production and pharmaceuticals containing such compounds
DE19745085A1 (de) * 1997-10-11 1999-04-15 Jenapharm Gmbh 11ß-Benzaldoxim-9alpha,10alpha-epoxy-estr-4-en-Derivate, Verfahren zu ihrer Herstellung und diese Verbindungen enthaltende pharmazeutische Präparate
DE19809845A1 (de) * 1998-03-03 1999-09-09 Jenapharm Gmbh S-substituierte 11beta-Benzaldoxim-estra-4,9-dien-kohlensäurethiolester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zubereitungen
DE19906152B4 (de) 1999-02-10 2005-02-10 Jenapharm Gmbh & Co. Kg Wirkstoffhaltige Laminate für Transdermalsysteme
CO5190694A1 (es) 1999-08-31 2002-08-29 Jenapharm Gmbh And Co Kg Mesoprogestinas (moduladores de receptores de progesterona) como componentes de anticonceptivos femeninos
CA2383659C (en) * 1999-08-31 2009-02-10 Jenapharm Gmbh & Co. Kg Mesoprogestins (progesterone receptor modulators) as a component of compositions for hormone replacement therapy (hrt)
RO122179B1 (ro) 1999-08-31 2009-02-27 Schering Aktiengesellschaft Utilizarea de mezoprogestine pentru tratamentul şi prevenirea afecţiunilor ginecologice benigne, hormon-dependente
US7629334B1 (en) * 1999-08-31 2009-12-08 Bayer Schering Pharma Aktiengesellschaft Mesoprogrestins (progesterone receptor modulations) as a component of compositions for hormone replacement therapy (HRT)
DE19961219A1 (de) * 1999-12-15 2001-07-19 Jenapharm Gmbh 11beta-Phenylestratrien-Derivate mit Fluoralkylgruppen in der aromatischen Seitenkette, deren Herstellung und diese Verbindungen enthaltende pharmazeutische Zusammensetzungen
DE10056677A1 (de) 2000-11-10 2002-05-16 Jenapharm Gmbh Verfahren zur Herstellung von 4-(17a-Alkoxymethyl-17ß-substituierten-3-oxoestra-4,9-dien-11ß-yl)benzaldehyd-(1E)-oxim-Derivaten
DE10056676A1 (de) * 2000-11-10 2002-05-16 Jenapharm Gmbh Verfahren zur Herstellung von 4-/17alpha-substituierten-3-oxoestra-4,9-dien-11beta-yl)benzaldehyd-(1E oder 1Z)-oximen
EP1285927A3 (de) * 2001-08-16 2005-06-29 Schering Aktiengesellschaft Verwendung von Glucocorticoid-Rezeptorantagonisten zur Vorbeugung und Behandlung von Erkrankungen des männlichen Reproduktionssystems
DE10221034A1 (de) * 2002-05-03 2003-11-20 Schering Ag 17alpha-Fluoralkyl-11ß-benzaldoxim-Steroide, Verfahren zu deren Herstellung, diese Steroide enthaltende pharmazeutische Präparate sowie deren Verwendung zur Herstellung von Arzneimitteln
ES2273061T3 (es) * 2002-08-02 2007-05-01 Schering Aktiengesellschaft Agentes moduladores de receptores de progesterona con actividad antigonadotropa elevada para el control de fertilidad femenina y para la terapia por reemplazo hormonal.
DE10236405A1 (de) 2002-08-02 2004-02-19 Schering Ag Progesteronrezeptormodulatoren mit erhöhter antigonadotroper Aktivität für die weibliche Fertilitätskontrolle und Hormonersatztherapie
DE102005059222B4 (de) * 2005-12-08 2007-10-11 Bayer Schering Pharma Ag 11ß-Benzaldoximderivate von D-Homoestra-4,9-dien-3-onen
CA2673128C (en) 2006-10-24 2018-07-03 Repros Therapeutics Inc. Compositions and methods for suppressing endometrial proliferation
TWI539953B (zh) 2008-04-28 2016-07-01 瑞波若斯治療學公司 用於治療乳癌之組成物和方法
CN102906103A (zh) 2010-03-22 2013-01-30 利普生物药剂公司 用于抗孕酮的非毒性递送的组合物和方法

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AU580843B2 (en) * 1985-02-07 1989-02-02 Schering Aktiengesellschaft 11``-phenyl-gonanes, their manufacture and pharmaceutical preparations containing them
DE3504421A1 (de) * 1985-02-07 1986-08-07 Schering AG, 1000 Berlin und 4709 Bergkamen Neue 11ss-phenyl-gonane, deren herstellung und diese enthaltende pharmazeutische praeparate
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CA2130515C (en) 2001-07-17
HUT68315A (en) 1995-06-28
KR100190775B1 (ko) 1999-06-01
RU94029667A (ru) 1996-06-27
HU219399B (hu) 2001-04-28
NO942952D0 (no) 1994-08-09
PL305091A1 (en) 1995-04-03
AU7035194A (en) 1995-03-30
JP2696672B2 (ja) 1998-01-14
FI112948B (fi) 2004-02-13
DE59401919D1 (de) 1997-04-10
DK0648779T3 (da) 1997-09-15
PL179460B1 (pl) 2000-09-29
NZ264228A (en) 1995-04-27
RU2130944C1 (ru) 1999-05-27
ES2102144T3 (es) 1997-07-16
SK280315B6 (sk) 1999-11-08
UA39101C2 (uk) 2001-06-15
SK95894A3 (en) 1995-04-12
EP0648779A2 (de) 1995-04-19
NO304988B1 (no) 1999-03-15
EP0648779A3 (de) 1995-08-09
DE4332284A1 (de) 1995-03-23
GR3023644T3 (en) 1997-08-29
DE4332284C2 (de) 1997-05-28
NO942952L (no) 1995-03-21
CZ289801B6 (cs) 2002-04-17
HU9402695D0 (en) 1994-11-28
FI943688A (fi) 1995-03-21
CZ196994A3 (en) 1995-04-12
CA2130515A1 (en) 1995-03-21
AU682373B2 (en) 1997-10-02
EP0648779B1 (de) 1997-03-05
ATE149513T1 (de) 1997-03-15
JPH07149790A (ja) 1995-06-13
FI943688A0 (fi) 1994-08-09

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