KR960700266A - 신규 결장- 또는 회장-특이성 스테로이드 유도체(Novel Colon-or lleum-Specific Steroid Derivatives) - Google Patents

신규 결장- 또는 회장-특이성 스테로이드 유도체(Novel Colon-or lleum-Specific Steroid Derivatives)

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Publication number
KR960700266A
KR960700266A KR1019950702801A KR19950702801A KR960700266A KR 960700266 A KR960700266 A KR 960700266A KR 1019950702801 A KR1019950702801 A KR 1019950702801A KR 19950702801 A KR19950702801 A KR 19950702801A KR 960700266 A KR960700266 A KR 960700266A
Authority
KR
South Korea
Prior art keywords
compound
sugar
gcs
epimer
general formula
Prior art date
Application number
KR1019950702801A
Other languages
English (en)
Inventor
랄프 레나르트 브라트산트
페터 에드만
토마스 회그베르크
스티나브리트 닐쓴
브로르 아르네 탈렌
얀 에릭 울미우스
Original Assignee
클래스 빌헬름슨
아스트라 악티에볼라크
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from SE9300030A external-priority patent/SE9300030D0/xx
Priority claimed from SE9300082A external-priority patent/SE9300082D0/xx
Application filed by 클래스 빌헬름슨, 아스트라 악티에볼라크 filed Critical 클래스 빌헬름슨
Publication of KR960700266A publication Critical patent/KR960700266A/ko

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/0026—Oxygen-containing hetero ring cyclic ketals
    • C07J71/0031—Oxygen-containing hetero ring cyclic ketals at positions 16, 17
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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]

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

본 발명은 염증성 장 점에 GCS를 결장-또는 회장-특이적으로 전달하기 위한, 당에 당피질성스테로이드(GCS)가 화학적으로 결합된 일반식 GCS1-0-당1인 신규의 화합물 및 그의 제조 방법 및 이 화합물을 함유하는 제약 제제 및 이들 화합물의 치료용으로서의 용도에 관한 것이다.

Description

신규 결장-또는 회장-특이성 스테로이드 유도체(Novel Colon-or lleum-Specific Steroid Derivatives)
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (24)

  1. 하기 일반식의 화합물 또는 그의 제약상 및 약물학상 허용되는 염.
    GCS1-O-당1
    상기 식에서, GCS1는 에피머 혼합물 또는 상응하는 순수한 22R-에피머 또는 22S-에피머로서의 하기 일반식(Ⅰ)의 기 또는 하기 일반식(Ⅱ)의 기로부터 선택된, 간에서의 1차 통과 대사율이 높은 당피질성스테로이드(GCS1-OH)이고;
    [상기 식에서, X1및 X2는 동일 또는 상이하며 수소, 불소, 염소 또는 브롬 치환체이고, X3는 불소, 염소 또는 브롬 치환체이며, R은 탄소 원자수 1-9의 탄화수소쇄이고, 식 주의 1,2-위치는 포화되거나 또는 이중 결합이다]당1은 모노사카리드, 디사카리드 또는 올리고사카리드의 잔기이며; GCS는 글리코사이드 결합을 통하여 21-위치에서 당에 결합된다.
  2. 제1항에 있어서, GCS1이 일반식(Ⅰ)의 22R-에피머인 화합물.
  3. 제1항에 있어서, GCS1이 일반식(Ⅲ)의 부데소니드 잔기
    의 22R-에피머 또는 하기 일반식(Ⅳ)
    의 22R-에피머 또는 하기 일반식(Ⅴ)
    의 22R-에피머 화합물.
  4. 제1항 내지 3항 중 어느 한 항에 있어서, 당1-OH가 D-글루코오스, D-갈락토오스, D-셀로비오스 또는 D-락토오스인 화합물.
  5. 제1항 내지 3항 중 어느 한 항에 있어서, 당1-OH가 D-글루쿠론산 또는 D-갈락투론산인 화합물.
  6. 제1항에 있어서, 당1-OH가 β-결합된 D-글루코오스인 화합물.
  7. 제1항에 있어서, 당1-OH가 β-결합된 D-글루쿠론산인 화합물.
  8. 제2항에 있어서, 당1-OH가 β-결합된 D-글루코오스인 화합물.
  9. 제2항에 있어서, 당1-OH가 β-결합된 D-글루쿠론산인 화합물.
  10. 제3항에 있어서, 당1-OH가 β-결합된 D-글루코오스인 화합물.
  11. 제3항에 있어서, 당1-OH가 β-결합된 D-글루쿠론산인 화합물.
  12. 제2항에 있어서, (22R)-16α,17α-부틸리덴디옥시-6α,9α-디플루오로-11β-히드록시-4-프레그렌-3,20-디온-31-일β-D-글루코피라노사이드인 화합물.
  13. 제2항에 있어서, (22R)-16α,17α-부틸리덴디옥시-11β-히드록시프레그나-1,4-디엘-3,20-디온-21-일β-D-글루코피라노사이드인 화합물.
  14. 제2항에 있어서, 나트륨[(22R)-16α,17α-부틸리덴디옥시-6α-9α-디플루오로-11β-히드록시-4-프레그렌-3,20-디온-21-일-β-D-글루코피라노사이드]우로네이트인 화합물.
  15. 제2항에 있어서, 나트륨[(22R)-16α,17α-부틸리덴디옥시-11β-히드록시프레그나-1,4-디엔-3,20-디온-21-일-β-D-글루코피라노사이드]우로네이트인 화합물.
  16. 당을 하기 일반식(Ⅵ), (ⅥA)(ⅥB) 또는 (Ⅶ)의 GCS1-OH와 축합시키는 것으로 이루어진 제1항에 따른 화합물의 제조 방법.
    상기 식에서, X1, X2, X3, R C1-C2결합은 제1항에서 정의한 바와 같다.
  17. 제16항에 있어서, 제2항 내지 15항 중의 어느 한 항의 화합물의 제조 방법.
  18. 활성 성분으로서, 제1항 내지 제15항 중 어느 한 항에 따른 화합물을 함유하는 제약 조성물.
  19. 제18항에 있어서, 단위 투여 형태인 제약 조성물.
  20. 제18항 또는 19항에 있어서, 제약상 허용되는 담체와 배합된 활성 성분으로 이루어진 제약 조성물.
  21. 치료용으로 사용하기 위한 제1항의 화합물의 용도.
  22. 염증성 장 점막의 치료에 사용되는 의약의 제조를 위한 제1항에 따른 화합물의 용도.
  23. 제22항에 있어서, 궤양성 대장염의 치료에 사용되는 의약의 제조를 위한 화합물의 용도.
  24. 제22항에 있어서, 크론병의 치료에 사용되는 의약의 제조를 위한 화합물의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950702801A 1993-01-08 1993-12-17 신규 결장- 또는 회장-특이성 스테로이드 유도체(Novel Colon-or lleum-Specific Steroid Derivatives) KR960700266A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
SE9300030A SE9300030D0 (sv) 1993-01-08 1993-01-08 Novel colon- or ileum-specific steroid derivatives
SE9300082A SE9300082D0 (sv) 1993-01-14 1993-01-14 Novel colon- or ileum-specific steroid derivatives
SE9300030-5 1993-01-14
SE9300082-6 1993-01-14
PCT/SE1993/001081 WO1994015947A1 (en) 1993-01-08 1993-12-17 Novel colon- or ileum-specific steroid derivatives

Publications (1)

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KR960700266A true KR960700266A (ko) 1996-01-19

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ID=26661623

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KR1019950702801A KR960700266A (ko) 1993-01-08 1993-12-17 신규 결장- 또는 회장-특이성 스테로이드 유도체(Novel Colon-or lleum-Specific Steroid Derivatives)

Country Status (22)

Country Link
US (2) US5908833A (ko)
EP (1) EP0678097B1 (ko)
JP (1) JP3366640B2 (ko)
KR (1) KR960700266A (ko)
AT (1) ATE183192T1 (ko)
BR (1) BR9307746A (ko)
CA (1) CA2152374A1 (ko)
CZ (1) CZ171095A3 (ko)
DK (1) DK0678097T3 (ko)
ES (1) ES2137353T3 (ko)
FI (1) FI953358A0 (ko)
GR (1) GR3031789T3 (ko)
HU (1) HU221584B (ko)
IS (1) IS4111A (ko)
LV (1) LV10961B (ko)
NO (1) NO305367B1 (ko)
NZ (1) NZ259596A (ko)
PL (1) PL178307B1 (ko)
RU (1) RU95115547A (ko)
SK (1) SK87295A3 (ko)
TW (1) TW261615B (ko)
WO (1) WO1994015947A1 (ko)

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HU9502087D0 (en) 1995-09-28
EP0678097B1 (en) 1999-08-11
US6140308A (en) 2000-10-31
CZ171095A3 (en) 1996-01-17
SK87295A3 (en) 1996-04-03
EP0678097A1 (en) 1995-10-25
GR3031789T3 (en) 2000-02-29
ATE183192T1 (de) 1999-08-15
PL178307B1 (pl) 2000-04-28
DK0678097T3 (da) 2000-02-07
HUT73227A (en) 1996-07-29
AU678803B2 (en) 1997-06-12
AU5844794A (en) 1994-08-15
US5908833A (en) 1999-06-01
TW261615B (ko) 1995-11-01
ES2137353T3 (es) 1999-12-16
JP3366640B2 (ja) 2003-01-14
PL309777A1 (en) 1995-11-13
RU95115547A (ru) 1997-06-10
WO1994015947A1 (en) 1994-07-21
FI953358A (fi) 1995-07-07
IS4111A (is) 1994-07-09
FI953358A0 (fi) 1995-07-07
BR9307746A (pt) 1995-11-14
CA2152374A1 (en) 1994-07-21
LV10961B (en) 1996-08-20
NZ259596A (en) 1997-04-24
HU221584B (hu) 2002-11-28
NO952683D0 (no) 1995-07-06
LV10961A (lv) 1995-12-20
NO952683L (no) 1995-07-06
NO305367B1 (no) 1999-05-18
JPH08505616A (ja) 1996-06-18

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