KR950700318A - 알칼리 금속 8,9-데하이드로에스트론 설페이트 에스테르(Alkali metal 8,9-dehydroestrone sulfate esters) - Google Patents

알칼리 금속 8,9-데하이드로에스트론 설페이트 에스테르(Alkali metal 8,9-dehydroestrone sulfate esters)

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KR950700318A
KR950700318A KR1019940702962A KR19940702962A KR950700318A KR 950700318 A KR950700318 A KR 950700318A KR 1019940702962 A KR1019940702962 A KR 1019940702962A KR 19940702962 A KR19940702962 A KR 19940702962A KR 950700318 A KR950700318 A KR 950700318A
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dehydroestrone
alkali metal
sulfate
salt
composition
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KR100256861B1 (ko
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키루간도스 라베엔드라나트 파놀릴
안토니 위치토우스키 존
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이곤 이. 버그
아메리칸 홈 프러덕츠 코포레이션
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • 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
    • C07J1/0059—Estrane derivatives substituted in position 17 by a keto group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61P5/36—Antigestagens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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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Abstract

본 발명은 8,9-데하이드로에스트론의 알칼리 금속염, 이의 설페이트 에스테르의 염 및 이의 안정한 조성물, 이의 제조방법 및 에스트로겐 대체 요법 및 심혈관 보호에 있어서의 용도를 제공한다.

Description

알칼리 금속 8,9-데하이드로에스트론 설페이트 에스테르(Alkali metal 8,9-dehydroestrone sulfate esters)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (28)

  1. 8,9-데하이드로에스트론의 알칼리 금속염.
  2. 제1항에 있어서, 알칼리 금속이 나트륨, 칼륨 또는 리튬인 화합물.
  3. 8,9-데하이드로에스트론을 알칼리 금속 염기로 처리하여 이의 알칼리 금속염을 수득함을 포함하여, 8,9-데하이드로에스트론의 알칼리 금속염을 제조하는 방법.
  4. 제13항에 있어서, 알칼리 금속 염기가 수소화나트륨, 수소화칼륨 또는 n-부틸리튬인 방법.
  5. 필수적으로 8,9-데하이드로에스트론-3-설페이트 에스테르의 알칼리 금속염으로 이루어지는 조성물.
  6. 제5항에 있어서, 알칼리 금속이 나트륨, 칼륨 또는 리튬인 조성물.
  7. 다른 에스트로겐성 스테로이드를 함유하지 않는 8,9-데하이드로에스트론-3-설페이트 에스테르의 약제학적으로 허용되는 염.
  8. 제7항에 있어서, 약제학적으로 허용되는 염이 알칼리 금속염인 화합물.
  9. 제8항에 있어서, 알칼리 금속이 나트륨, 칼륨 또는 리튬인 화합물.
  10. 제7항에 있어서, 칼슘 8,9-데하이드로에스트론-3-설페이트인 화합물.
  11. 제7항에 있어서, 마그네슘 8,9-데하이드로에스트론-3-설페이트인 화합물.
  12. 제7항에 있어서, 암모늄 8,9-데하이드로에스트론-3-설페이트인 화합물.
  13. 제7항에 있어서, 아민의 알킬 잔기의 탄소수가 1내지 6인 8,9-데하이드로에스트론-3-설페이트의 알킬아민염인 화합물.
  14. 제13항에 있어서, 8,9-데하이드로에스트론-3-설페이트의 에틸아민 염인 화합물.
  15. 제7항에 있어서, 아민의 알킬 잔기의 탄소수가 1 내지 6인 8,9-데하이드로에스트론-3-설페이트의 디알킬아민 염인 화합물.
  16. 제15항에 있어서, 8,9-데하이드로에스트론-3-설페이트의 디메틸아민 염인 화합물.
  17. 트리에틸아민-설퍼트리옥사이드를 안정화량의 트리스(하이드록시메틸)아미노메탄의 존재하에 극성 비양자성 용매 속에서 8,9-데하이드로에스트론의 알칼리 금속염과 반응시킴을 포함하여, 8,9-데하이드로에스트론-3-설페이트의 알칼리 금속염을 함유하는 안정한 조성물을 제조하는 방법.
  18. 트리에틸아민-설퍼트리옥사이드를 극성 비양자성 용매 속에서 8,9-데하이드로에스트론의 알칼리 금속염과 반응시키고, 반응 혼합물에 안정화량의 트리스(하이드록시메틸)아미노메탄을 가한 다음, 8,9-데하이드로에스트론의 알칼리 금속염과 트리스(하이드록시메틸)아미노메탄의 안정한 혼합물을 회수함을 포함하여, 8,9-데하이드로에스트론-3-설페이트의 알칼리 금속염을 함유하는 안정한 조성물을 제조하는 방법.
  19. 8,9-데하이드로에스트론-3-설페이트의 알칼리 금속염을 트리스(하이드록시메틸)아미노메탄과 혼합하여 포함하는, 다른 에스트로겐성 스테로이드를 함유하지 않는 조성물.
  20. 제19항에 있어서, 트리스(하이드록시메틸)아미노메탄 : 8,9-데하이드로에스트론-3-설페이트의 알칼리 금속염의 비가 1 : 0.5 내지 0.5 : 1인 조성물.
  21. 제5항 내지 제16항 중의 어느 한 항에서 청구한 조성물과 약제학적으로 허용되는 담체를 포함하는 약제학적 조성물.
  22. 에스트로겐 결핍의 대체, 유즙분비의 억제, 멈프스성 고환염의 예방 및 치료, 및 동맥경화증 및 노인성 골다공증의 치료용 약제를 제조하기 위한, 제5항 내지 제16항 중의 어느 한 항에서 청구한 조성물의 용도.
  23. 제5항 내지 제16항 중의 어느 한 항에서 청구한 조성물과 약제학적으로 허용되는 담체를 포함하는 수의용 조성물.
  24. 미성숙 암컷, 실금, 거세한 암캐의 질염, 자궁 무력증, 자궁농증 및 보유된 태아막의 대체 요법용 수의 약제를 제조하기 위한, 제5항 내지 제16항 중의 어느 한 항에서 청구한 조성물의 용도.
  25. 동맥경화증 치료를 요하는 환자에게 유효량의 8,9-데하이드로에스트론 또는 8,9-데하이드로에스트론 설페이트 에스테르의 염을 투여함을 포함하여 동맥경화증을 치료하는 방법.
  26. 제25항에 있어서, 8,9-데하이드로에스트론 설페이트 에스테르의 염이 칼슘, 마그네슘, 암모늄, 알킬아민 또는 디알킬아민 염(여기서, 아민의 알킬 그룹의 탄소수는 1 내지 6이다)인 방법.
  27. 동맥경화증이 있는 환자에게 동맥경화증 치료량의 8,9-데하이드로에스트론 또는 8,9-데하이드로에스트론 설페이트 에스테르의 염을 함유하는 약제학적 조성물을 경구 또는 비경구 투여함을 포함하여 동맥경화증 발생에 수반되는 동맥 손상을 제거하는 방법.
  28. 8,9-데하이드로에스트론-3-설페이트 에스테르를 알칼리 금속 수산화물, 알칼리 토금속 수산화물, 아민, 암모니아 또는 수산화암모늄으로부터 선택된 염기로 처리함을 포함하여, 제7항에서 청구한 약제학적으로 허용되는 염을 제조하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019940702962A 1992-02-26 1993-02-19 알칼리금속8,9-데하이드로에스트론 설페이트 에스테르, 이의 제조방법 및 이를 포함하는 약제학적 조성물 KR100256861B1 (ko)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US07/841,694 US5210081A (en) 1992-02-26 1992-02-26 Alkali metal 8,9-dehydroestrone sulfate esters
US7/841694 1992-02-26
US07/841,694 1992-02-26
PCT/US1993/001500 WO1993017036A1 (en) 1992-02-26 1993-02-19 Alkali metal 8,9-dehydroestrone sulfate esters

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KR950700318A true KR950700318A (ko) 1995-01-16
KR100256861B1 KR100256861B1 (ko) 2000-08-01

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ATE174342T1 (de) 1998-12-15
FI943903A0 (fi) 1994-08-25
DE69322497D1 (de) 1999-01-21
GR3029620T3 (en) 1999-06-30
CA2089707A1 (en) 1993-08-27
DK0628052T3 (da) 1999-07-12
AU711571B2 (en) 1999-10-14
LV12240A (lv) 1999-03-20
AR042262A2 (es) 2005-06-15
ES2125975T3 (es) 1999-03-16
JPH07504197A (ja) 1995-05-11
US6169082B1 (en) 2001-01-02
HK1020282A1 (en) 2000-04-07
MX9300969A (es) 1993-09-01
FI115915B (fi) 2005-08-15
EP0864583A2 (en) 1998-09-16
AU2007697A (en) 1997-07-03
JP3715645B2 (ja) 2005-11-09
DE69334073T2 (de) 2007-02-01
AU3726093A (en) 1993-09-13
US5210081A (en) 1993-05-11
FI943903A (fi) 1994-08-25
ZA93746B (en) 1994-08-03
HUT67553A (en) 1995-04-28
WO1993017036A1 (en) 1993-09-02
LV12240B (en) 1999-06-20
HU211971A9 (en) 1996-01-29
KR100256861B1 (ko) 2000-08-01
ES2274555T3 (es) 2007-05-16
DE69322497T2 (de) 1999-05-06
TW257677B (ko) 1995-09-21
AR042345A2 (es) 2005-06-15
DK0864583T3 (da) 2006-12-04
HU9402457D0 (en) 1994-10-28
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ATE342272T1 (de) 2006-11-15
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EP0864583A3 (en) 2004-07-21
HK1011369A1 (en) 1999-07-09
US5288717A (en) 1994-02-22
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AU677181B2 (en) 1997-04-17

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