KR970704771A - 에스트라-1,3,5(10)-트리엔 유도체를 함유한 약제학적 조성물(Pharmaceutical compositions containing Estra-1,3,5(10)-triene Derivatives) - Google Patents

에스트라-1,3,5(10)-트리엔 유도체를 함유한 약제학적 조성물(Pharmaceutical compositions containing Estra-1,3,5(10)-triene Derivatives) Download PDF

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KR970704771A
KR970704771A KR1019970700812A KR19970700812A KR970704771A KR 970704771 A KR970704771 A KR 970704771A KR 1019970700812 A KR1019970700812 A KR 1019970700812A KR 19970700812 A KR19970700812 A KR 19970700812A KR 970704771 A KR970704771 A KR 970704771A
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hydroxy
estra
sulfamate
triene
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엘거 발터
슈바르츠 지그프리트
레더젠 구드룬
슈나이더 비르기트
지만 한스-요하임
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디에터 타우베르트, 미카엘 오에텔
제나팜 게엠베하
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    • C07J—STEROIDS
    • C07J53/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by condensation with a carbocyclic rings or by formation of an additional ring by means of a direct link between two ring carbon atoms, including carboxyclic rings fused to the cyclopenta(a)hydrophenanthrene skeleton are included in this class
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    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • 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
    • 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
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P15/18—Feminine 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
    • 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
    • A61P5/18—Drugs for disorders of the endocrine system of the parathyroid 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
    • 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
    • C07J41/0072—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed

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Abstract

본 발명은 하기 일반식의 그룹을 그의 C3 위치에 가지는 에스트라-1,3,5(10)-트리엔 유도체를 활성 성분으로서 가지는 약제학적 제제에 관한 것이다.
R-SO2-O-
상기 식에서, R은 R1R2N 그룹이며, 이겨에서 R1및 R2는 서로 독립적이고 수소 원자, C1-C5알킬을 나타내거나, 질소 원자와 함께 4 내지 6개의 탄소 원자를 가진 폴리메틸렌 이미노 라디칼을 나타내거나, 모르폴리노 라디칼을 나타낸다.
본 발명에 의한 제제는 호르몬성 피임 및 호르몬 대체 요법(HRT)용으로 사용되어 질 수 있다. 그것들은 낮은 간성 발정원성을 나타낸다.

Description

에스트라-1,3,5(10)-트리엔 유도체를 함유한 약제학적 조성물(Pharmaceutical compositions containing Estra-1,3,5(10)-triene Derivatives).
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (5)

  1. C3 위치에 하기 일반식의 그룹을 가지는 에스트라-1,3,5(10)-트리엔 유도체를 활성 성분으로서 함유하는 약제학적 제제:
    R-SO2-O-
    상기 식에서, R은 R1R2N 그룹이며, 여기에서 R1및 R2는 서로 독립적으로 수소 원자 또는 C1-C5알킬 라디칼을 나타내거나, 질소 원자와 함께 4내지 6개의 탄소 원자를 가진 폴리메틸렌 이미노 라디칼 또는 모르폴리노 라디칼을 나타낸다.
  2. 제 1항에 있어서, 하기 일반식 (I)의 활성 성분을 함유함을 특징으로 하는 약제학적 제제:
    상기 식에서, R은 R1R2N이며, R1및 R2는 서로 독립적으로 수소 원자 또는 C1-C5알킬을 나타내거나, 질소 원자와 함께 4 내지 6개의 탄소 원자를 가진 폴리메틸렌 이미노 라디칼 또는 모르폴리노 라디칼을 나타내고, R3은 수소 원자, 하이드록시 그룹, 또는 1 내지 5개의 탄소 원자를 가진 알콕시 그룹이며, R4는 수소 원자 또는 C1-C5알킬 라디칼이고, R5는 수소 원자, 하이드록시 그룹, 에스테르화된 하이드록시 그룹, 또는 1 내지 5개의 탄소 원자를 가진 할로알킬 또는 알콕시그룹이며 R6및 R7은 수소 원자이거나, 함께 메틸렌 그룹을 형성하고, R8, R9및 R10은 서로 독립적으로 수소 원자 또는 하이드록시 그룹을 나타내며, 단, 환 B는 임의로 1 또는 2개의 이중결합을 함유하거나, 임의로 R9는 5개 이하의 탄소 원자를 가진 알키닐 라디칼이거나, R9및 R10은 함께 산소 원자를 나타내거나 그룹이며 R6및 R9는 비닐렌 또는 에틸렌 그룹을 나타낸다.
  3. 제 1항 또는 제 2항에 있어서, 17β-하이드록시-에스트라-1,3,5(10)-트리엔-3-일 설파메이트, 17β-하이드록시-에스트라-1,3,5(10)-트리엔-3-일 N,N-디에틸-설파메이트, 17β-하이드록시-에스트라-1,3,5(10)-트리엔-3-일 N,N-디메틸-설파메이트,17β-하이드록시-에스트라-1,3,5(10),7-테트라엔-3-일 N,N-디에틸-설파메이트, 17β-하이드록시-에스트라-1,3,5(10),6,8-펜타엔-3-일 N,N-디메틸-설파메이트, 17-옥소-에스트라-1,3,5(10)-트리엔-3-일 설파메이트, 17-옥소-에스트라-1,3,5(10)-트리엔-3-일 N,N-디메틸-설파메이트, 17-옥소-에스트라-1,3,5(10)-트리엔-3-일 N,N-디에틸-설파메이트, 16α,17β-디하이드록시-에스트라-1,3,5(10)-트리엔-3-일 설파메이트, 16α, 17β-디하이드록시-에스트라1,3,5(10)-트리엔-3일 N,N-디에틸-설파메이트, 2,17β-디하이드록시-에스트라-1,3,5(10)-트리엔-3-일 N,N-디메틸-설파메이트, 2-메톡시-17β-하이드록시-에스트라-1,3,5(10)-트리엔-3-일 N,N-디에틸-설파메이트, 17β-하이드록시-19-노르-17α프레그나-1,3,5(10)-트리엔-20-인-3일 설파메이트, 17β-하이드록시-19-노르-17α-프레그나-1,3,5(10)-트리엔-20-인-3-일 N-메틸-설파메이트, 17β-하이드록시-19-노르-17α-프레그나-1,3,5(10)-트리엔-20-인-3-일 N,N-디메틸-설파메이트, 17β-하이드록시-19-노르-17α-프레그나-1,3,5(10)-트리엔-20-인-3-일N, N-디에틸-설파메이트 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10)-트리엔-3-일 피롤리디노설포네이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10)-트리엔-3-일 피롤리디노설포네이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10)-트리엔-3-일 N-메틸-설파메이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10)-트리엔-3-일 모르폴리노설포네이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10)-트리엔-3-일 N-메틸-설파메이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10)-트리엔-3-일 설파메이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10),7-테트라엔-3-일 N,N-디메틸-설파메이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10),6,8-펜타엔-3-일 N,N-디에틸-설파메이트, 17β-하이드록시-14α,15α-메틸렌-에스트라-1,3,5(10),8-테트라엔-3-일 N,N-디메틸-설파메이트, 11β-클로로메틸-17β-하이드록시-에스트라-1,3,5(10)-트리엔-3-일 N,N-디메틸-설파메이트,17β-하이드록시-14α,17α-비닐렌-에스트라-1,3,5(10)-트리엔-3-일 N,N-디에틸-설파메이트, 14α,17α-에틸렌-17β-하이드록시-에스트라-1,3,5(10)-트리엔-3-일 피롤리디노설포네이트, 16α,17β-디하이드록시-14α,17α-에틸렌-에스트라-1,3,5(10)-트리엔-3-일 N,N-디에틸-설파메이트, 17β-하이드록시-7α-메틸-에스트라-1,3,5(10)-트리엔-3,11β-디일 3-N,N-디메틸-설파메이트-11-니트레이트 또는 17β-하이드록시-11β-메톡시-19-노르-17α-프레그나-1,3,5(10)-트리엔-20-인-3-일 N,N-디메틸-설파메이트를 함유함을 특징으로 하는 약제학적 제제.
  4. 제 1항 내지 제 3항에 있어서, 정제, 조절 방출형 정제, 로젠지(lozenge), 환제, 캅셀제, 필름 정제 및 조절 방출형 필름 정제의 형태인 에스트라-1,3-5(10)-트리엔 유도체를 함유한 약제학적 제제.
  5. 제 1항 내지 제 4항중 어느 한 항에 있어서, 호르몬성 피임, 폐경기 호르몬 대체 요법, 및 유방암 및 전립 선암과 같은 부인과적 및 남성병학적 질환 치료용 약제학적 제제.
KR1019970700812A 1994-08-09 1995-07-03 에스트라-1,3,5(10)-트리엔 유도체를 함유한 약제학적 조성물 KR100243537B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE4429398A DE4429398C2 (de) 1994-08-09 1994-08-09 Verwendung von Estra-1,3,5(10)-trien-Derivaten zur hormonalen Kontrazeption
DEP4429398.4 1994-08-09
PCT/DE1995/000879 WO1996005217A1 (de) 1994-08-09 1995-07-03 Pharmazeutische zusammensetzungen mit estra-1,3,5(10)-trien-derivaten

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KR970704771A true KR970704771A (ko) 1997-09-06
KR100243537B1 KR100243537B1 (ko) 2000-02-01

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GB9625334D0 (en) * 1996-12-05 1997-01-22 Imperial College Compound
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