KR860001123A - 신규의 9α-플루오로-또는 클로로-코티코스 테로이드 에스테르와 이들의 제조방법 - Google Patents

신규의 9α-플루오로-또는 클로로-코티코스 테로이드 에스테르와 이들의 제조방법 Download PDF

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KR860001123A
KR860001123A KR1019850005291A KR850005291A KR860001123A KR 860001123 A KR860001123 A KR 860001123A KR 1019850005291 A KR1019850005291 A KR 1019850005291A KR 850005291 A KR850005291 A KR 850005291A KR 860001123 A KR860001123 A KR 860001123A
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chloro
dione
methylpregna
diene
trihydroxy
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KR1019850005291A
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KR880001238B1 (ko
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빌락스 이반 (외 2)
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엘리쟈베드 발더
호비온 인터 리미티드
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    • 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
    • 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
    • C07J5/0046—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 substituted in position 17 alfa
    • C07J5/0061—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 substituted in position 17 alfa substituted in position 16
    • C07J5/0069—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 substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group
    • C07J5/0076—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 substituted in position 17 alfa substituted in position 16 by a saturated or unsaturated hydrocarbon group by an alkyl group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/008—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21
    • C07J7/0085—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms substituted in position 21 by an halogen atom

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Rheumatology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)

Abstract

내용 없음

Description

신규의 9α-플루오로-또는 클로로-코티코스 테로이드 에스테르와 이들의 제조방법
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 구조식(Ⅱ)의 혼합물을 HCI 또는HF와 반응시키는 것을 특징으로 하는 9α-플루오로-또는 클로로-17,21-디하이드록시코티코스테로이드의 17,21-디아실레이트와 9α-플루오로-또는 클로로-17-하이드록시-코티코스테로이드의 17-아실레이트인 구조식(Ⅰ)의 화합물의 제조방법.
  3. (여기서, Y는 염소 또는 OR1,R2과 R2는 탄소원자수 2 내지 6개인 아실기 또는 벤조일기로 R1과 R2는 같은 분자내에서 서로 같거나 또는 다르며, R3는 α-또는 β-배향의 메틸 또는 불소이고, X는 염소 또는 불소,결합은 포화 또는 불포화 결합이다.)
  5. (여기서, Y,R2그리고 R3,는 상기와 같다)
  6. 제1항에 있어서, HCI 또는 HF는 그 과량을 유기용매 또는 물에 용해시켜서 사용한다는 것과 반응온도는 -60℃~+20℃로 조절한다는 것.
  7. 제2항에 있어서, 반응 온도는 바람직하게는 -20℃~+10℃이라는 것
  8. 제1항과 2항에 있어서, 반응의 최종생성물은 약 0℃의 온도에서 비용매를 사용하여 혼합물로부터 단리해 낸다는 것과 이때의 반응 혼합물의 최종 pH는 3-7이라는 것
  9. 제4항에 있어서, 비용매는 물과 얼음이라는 것과 pH는 탄산나트륨, 중탄산나트륨, 암모니아용액 또는 유기아민을 사용하여 조절한다는 것
  10. 구조식(Ⅰ)의 어느 하나의 화합물과 약학적으로 허용되는 캐리어(carrier)로 된 약학적 조성물.
  11. 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17,21-디아세테이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17,-디아세테이트 21-프로피오네이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17-아세테이트-21-부티레이트, 9α-클로로-11β,17α,21-프리하이드록시-16α-메틸프레그나-1,4디엔-3,20-디온17-아세테이트 21-발레레이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17-아세테이트 21-벤조에이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17-프로피오세테이트 21-아세테이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17-디프로피오네이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17-프로피오네이트 21-부틸레이트, 9α-클로로-11,β,17α,21-트리하이드록시- 16α-메틸프레그나-1,4-디엔-3,20-디온 17-프로피오네이트 21-발레레이트, 9α-클로로트-11,β,17α,21-리하이드록시-16α-메틸프레그나-1,4-디엔-3,20-디온 17-프로피오네이트 21-벤조에이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17-부티레이트 21-아세테이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17-부티레이트 21-프로피오네이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17 ,21-디부티레이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-엔디- 3, 20-디온 17-부티레이트 21-발레레이트. 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17-부티레이트 21-벤조에이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17-발레레이드 21-아세테이트, 9α-클로로- 11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17-발레레이트 21-프로피오네이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나 -1,4-디엔- 3, 20-디온 17-발레레이트 21-부티레이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17,21-디발레레이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17-발레레이트 21-벤조에이트, 9α-클로로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17 -프로피오네이트 21-부티레이트, 9α-플루오로-11,β,17α,21-트리하이드록시-16α-메틸프레그나-1,4-디엔- 3, 20-디온 17-발레레이트 21-부티레이트중의 어느 하나와 약학적으로 허용되는 캐리어(carrier)로 된 약학적 조성물.
  12. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019850005291A 1984-07-25 1985-07-24 9α-플루오로-또는 클로로-코티코스테로이드 에스테르의 제조방법 KR880001238B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
PT78973 1984-07-25
PT78973A PT78973A (en) 1984-07-25 1984-07-25 New preparation process of the 9alpha-fluoro 17,21-acylates or hidroxilades in 17 and 21 chloro-corticosteroid
PT78,973 1984-07-25

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KR860001123A true KR860001123A (ko) 1986-02-22
KR880001238B1 KR880001238B1 (ko) 1988-07-12

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US (1) US5026693A (ko)
EP (1) EP0170500B1 (ko)
JP (2) JPS6153297A (ko)
KR (1) KR880001238B1 (ko)
AT (1) ATE57384T1 (ko)
AU (1) AU571986B2 (ko)
CA (1) CA1307257C (ko)
DE (1) DE3580072D1 (ko)
DK (1) DK167617B1 (ko)
ES (1) ES8606878A1 (ko)
HK (1) HK107990A (ko)
IE (1) IE58941B1 (ko)
IL (1) IL75871A (ko)
NZ (1) NZ212876A (ko)
PT (1) PT78973A (ko)
ZA (1) ZA855621B (ko)

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DE4333920A1 (de) 1993-10-05 1995-04-13 Hoechst Ag Corticoid-17,21-dicarbonsäureester sowie Corticosteroid-17-carbonsäureester-21-kohlensäureester, Verfahren zu deren Herstellung und diese enthaltende Arzneimittel
US5981517A (en) * 1996-05-09 1999-11-09 Soft Drugs, Inc. Androstene derivatives
JP7106773B1 (ja) * 2022-01-25 2022-07-26 同仁医薬化工株式会社 ステロイド１７α，２１－ジエステル類の製造方法

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Also Published As

Publication number Publication date
KR880001238B1 (ko) 1988-07-12
US5026693A (en) 1991-06-25
IL75871A0 (en) 1985-11-29
HK107990A (en) 1990-12-28
ZA855621B (en) 1986-03-26
JPS6153297A (ja) 1986-03-17
NZ212876A (en) 1988-05-30
IL75871A (en) 1989-05-15
IE58941B1 (en) 1993-12-01
JPH0215559B2 (ko) 1990-04-12
IE851851L (en) 1986-01-25
ES8606878A1 (es) 1986-06-01
AU571986B2 (en) 1988-04-28
PT78973A (en) 1984-08-01
EP0170500A2 (en) 1986-02-05
EP0170500A3 (en) 1986-06-11
EP0170500B1 (en) 1990-10-10
JPS6354392A (ja) 1988-03-08
ES545560A0 (es) 1986-06-01
DK334585D0 (da) 1985-07-23
DK167617B1 (da) 1993-11-29
AU4530685A (en) 1986-01-30
ATE57384T1 (de) 1990-10-15
DE3580072D1 (de) 1990-11-15
CA1307257C (en) 1992-09-08
JPH037679B2 (ko) 1991-02-04
DK334585A (da) 1986-01-26

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