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KR880007497A - 2,3-이치환된 이속사졸리딘, 그의 제조방법, 그를 함유하는 제제 및 그의 용도 - Google Patents

2,3-이치환된 이속사졸리딘, 그의 제조방법, 그를 함유하는 제제 및 그의 용도 Download PDF

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KR880007497A
KR880007497A KR870014373A KR870014373A KR880007497A KR 880007497 A KR880007497 A KR 880007497A KR 870014373 A KR870014373 A KR 870014373A KR 870014373 A KR870014373 A KR 870014373A KR 880007497 A KR880007497 A KR 880007497A
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헨크 스테판
브록스 디이트리히
귄츨러 볼크마르
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하인리히 베커, 베른하르트 베크
훽스트 아크티엔게젤샤프트
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Abstract

내용 없음.

Description

2,3-이치환된 이속사졸리딘, 그의 제조방법, 그를 함유하는 제제 및 그의 용도
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (12)

  1. 일반식(I)의 화합물 및 그의 생리학적으로 허용되는 염.
    상기식에서, A는 a l)각각의 라디칼중 1,2 또는 3개의 수소원자가 카복실, 아미노,(C1-C4)-알킬아미노, 하이드록실, (C1-C4)-알콕시, 할로겐, 디-(C1-C4)-알킬아미노, 카바모일, 설파모일, (C1-C4)-알콕시카보닐, (C6-C12)-아릴 및 (C6-C12)-아릴-(C1-C5)-알킬로 이루어진 그룹으로부터 선택된 1,2 또는 3개의 동일하거나 상이한 라디칼로 임의 치환되거나, 1개의 수소원자가 (C3-C8)-사이클로알킬, (C1-C4)-알킬설포닐, (C1-C4)-알킬설피닐, (C6-C12)-아릴-(C1-C4)-알킬설포닐, (C6-C12)-아릴-(C1-C4)-알킬설피닐, (C6-C12)-아릴옥시, (C3-C9)-헤테로 아릴 및 (C3-C9)-헤테로 아릴옥시로 이루어진 그룹으로 부터 선택된 라디칼에 의해 임의 치환되고 1 또는 2개의 수소원자가 카복실, 아미노, (C1-C4)-알칼아미노, 하이드록실, (C1-C4)-알콕시, 할로겐, 디-(C1-C4)-알킬아미노, 카바모일, 설파모일, (C1-C4)-알콕시카보닐, (C6-C12)-아릴 및 (C6-C12)-아릴-(C1-C5)-알킬로 이루어진 그룹으로부터 선택된 1 또는 2개의 동일하거나 상이한 라디칼에 의해 치환된 (C1-C8)-알킬, (C1-C8)-알카노일, (C1-C8)-알콕시카보닐 또는 (C1-C8)-알킬 설포닐이거나, a 2) (C3-C8)-사이클로알킬, (C6-C12)-아릴, (C6-C12)-아릴설포닐 또는 (C3-C9)-헤테로아릴이거나(여기서, a l) 및 a 2)하에 정의된 라디칼중 (C6-C12)-아릴 또는 (C3-C9)-헤테로아릴은 각각 카복실, 아미노, 니트로, (C1-C4)-알킬아미노, 하이드록실, (C1-C4)-알콕시, 할로겐, 시아노, 디-(C1-C4)-알킬 아미노, 카바모일, 설파모일 및 (C1-C4)-알콕시카보닐로 이루어진 그룹으로부터 선택된 1,2 또는 3개의 동일하거나 상이한 라디칼에 의해 임의 치환된다). 또는 a 3) 일반식(IIa) 또는 (IIb)의 라디칼이며,
    R1은 b 1) 수소, 또는 b 2) a 1) 또는 a 2)에서 정의한 A와 같고, c 1) R2및 R2'는 동일하거나 상이하며 수소 또는 메틸이고, R3및 R3'는 동일하거나 상이하며 수소: 또는 아미노, 벤질옥시카보닐아미노, 하이드록실, 카복실, 카바모일, 구아니디노, 우레이도, 머캅토, 메틸머캅토, 페닐, 4-클로로페닐, 4-플루오로 페닐, 4-니트로 페닐, 4-메톡시페닐, 4-하이드록시 페닐, 프탈이미도, 4-이미다졸릴, 3-인돌릴, 2-티에닐, 3-티에닐, 2-피리딜, 3-피리딜 또는 사이클로헥실에 의해 임의로 일치환된 (C1-C6)-알킬이거나, c 2) R3및 R3'및/또는 R2'및 R3'각각은 함께 CH2그룹이 산소에 의해 치환될 수 있는 [-CH2-CH2-CH2-]이거나, 또는 c 3) R2및 R3및/또는 R2'및 R3'각각은 함께을 나타내며, B는 카보닐, 티오카보닐, 카비미도일, N-(C1-C3)-알킬-카비미도일, N-(C1-C3)-알콕시-카비미도일, 설피닐, CR5R6또는 직접 결합이고, d 1) R5및 R6는 동일하거나 상이하며, 수소,(C1-C8)-알킬 또는 (C3-C8)-사이클로알킬이거나, 또는 d 2) R5및 R6는 함께 1 또는 2개의 CH2그룹이 산소, 황 및/또는 NR7에 의해 임의로 치환되는 -[CH2]m-(여기에서, m은 4 또는 5이다)이고, D는 이미노, N-메틸이미노, 옥시, 메틸렌 또는 직접 결합을 나타내고, E는 카보닐, C=NR7, C=N-OR7또는 설피닐이거나, F가 결합인 경우 또한 하이드록시메틸렌일 수 있으며, R7은 d l) 에서 정의된 R5와 동일하며, F는 옥시, 이미노, N-메틸이미노 또는 직접 결합을 나타내고, R4는 각각의 알킬이 카복실, 아미노, (C1-C4)-알킬아미노, 하이드록실, (C1-C4)-알콕시, 할로겐, 디(C1-C4)-알킬아미노, 카바모일, (C1-C4)-알콕시카보닐, (C6-C12)-아릴 및 (C6-C12)-아릴-(C1-C5)-알킬로 이루어진 그룹으로부터 선택된 1 또는 2개의 동일하거나 상이한 라디칼에 의해 임의 치환되고, 각각의 (C6-C12)-아릴 또는 (C3-C9)-헤테로아릴이 카복실, 시아노, 아미노, 니트로, (C1-C4)-알킬아미노, 하이드록실, (C1-C4)-알콕시, 할로겐, 디-(C1-C4)-알킬아미노, 카바모일, 설파모일 및 (C1-C4)-알콕시카보닐로 이루어진 그룹으로부터 선택된 1,2 또는 3개의 동일하거나 상이한 라디칼에 의해 임의 치환된 (C1-C6)-알킬, (C3-C6)-사이클로알킬, (C6-C12)-아릴, (C6-C12)-아릴-(C1-C5)-알킬, (C6-C12)-아릴옥시-(C1-C5)-알킬, (C3-C9)-헤테로 아릴-(C1-C5)-알킬이며, R8은 c 1)에서 정의된 R3와 동일하다.
  2. 제1항에 있어서, A가 임의 치환된 (C1-C8)-알킬, (C1-C8)-알카노일 또는 임의 치환된 (C1-C8)-알콕시카보닐, 또는 제1항에서 a 3)에 정의된 바와 같은 일반식(I)의 화합물.
  3. 제1항 또는 2항에 있어서, R8가 수소인 일반식(I)의 화합물.
  4. 제1항 내지 3항중 어느 한 항에 있어서, B가 카보닐, 티오카보닐 또는 CR5R6(여기서 R5및 R8는 H이다)인 일반식(I)의 화합물.
  5. 제1항 내지 4항중 어느 한 항에 있어서, D가 이미노, 옥시 또는 메틸렌인 일반식(I)의 화합물.
  6. 제1항 내지 5항중 어느 한 항에 있어서, E카 카보닐인 일반식(I)의 화합물.
  7. 제1항 내지 6항중 어느 한 항에 있어서, F가 옥시 또는 직접 결합인 일반식(I)의 화합물.
  8. 제1항 내지 7항중 어느 한 항에 있어서, R4가 임의 치환된 (C6-C12)-아릴, 또는 알킬 잔기가 임의르 치환되고/되거나 아릴 잔기가 임의로 치환된 (C6-C12)-아릴-(C1-C5)-알킬인 일반식(I)의 화합물.
  9. 반응물들로부터 공지된 방법으로 화합물을 제조하고 경우에 따라서 하나 또는 그 이상의 임시로 도입된 보호그룹(들)을 제거하고, 경우에 따라서 카보닐 그룹을 티아 동족체로 전환시키고, 경우에 따라서 생성된 일반식(I)의 화합물을 그의 생리학적으로 허용되는 염으로 전환시킴을 특징으로 하여, 제1항 내지 8항중 어느 한 항에 따른 일반식(I)의 화합물을 제조하는 방법.
  10. 제1항 내지 8항중 어느 한 항에 따른 화합물의, 프롤릴 하이드록실라제 저해제로서의 용도.
  11. 제1항 내지 8항중 어느 한 항에 따른 화합물의, 약제로서의 용도.
  12. 제1항 내지 8항중 어느 한 항에 따른 화합물 및 생리학적으로 허용되는 비이클을 함유하는 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019870014373A 1986-12-17 1987-12-17 2, 3-이치환된 이속사졸리딘, 그의 제조방법, 그를 함유하는 제제 및 그의 용도 KR960010349B1 (ko)

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DEP3643012.9 1986-12-17
DE19863643012 DE3643012A1 (de) 1986-12-17 1986-12-17 2,3-disubstituierte isoxazolidine, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung

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DD284030A5 (de) 1988-11-24 1990-10-31 Hoechst Ag,De Verfahren zur herstellung von peptiden mit bradykinin-antagonistischer wirkung
DE3842197A1 (de) * 1988-12-15 1990-06-21 Hoechst Ag Rasch spaltbares substrat fuer die hiv-protease
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NO875263D0 (no) 1987-12-16
DE3782149D1 (ko) 1992-11-12
EP0271865A3 (en) 1990-02-07
FI875503A0 (fi) 1987-12-15
NO875263L (no) 1988-06-20
PT86380B (pt) 1990-11-20
CA1338484C (en) 1996-07-23
EP0271865B1 (de) 1992-10-07
JPS63165374A (ja) 1988-07-08
NZ222921A (en) 1989-08-29
KR960010349B1 (ko) 1996-07-30
DE3643012A1 (de) 1988-06-30
ES2052539T3 (es) 1994-07-16
DK662087D0 (da) 1987-12-16
DK662087A (da) 1988-06-18
AR246528A1 (es) 1994-08-31
NO175058C (ko) 1994-08-24
US5422342A (en) 1995-06-06
EP0271865A2 (de) 1988-06-22
FI875503A (fi) 1988-06-18
GR3006699T3 (ko) 1993-06-30
DK171894B1 (da) 1997-08-04
NO175058B (no) 1994-05-16
IE61034B1 (en) 1994-09-07
AU599177B2 (en) 1990-07-12
ATE81344T1 (de) 1992-10-15
ZA879400B (en) 1988-07-27
PH24746A (en) 1990-10-01
IL84841A0 (en) 1988-06-30
FI88303B (fi) 1993-01-15
US5610146A (en) 1997-03-11
PT86380A (de) 1988-01-01
JP2703912B2 (ja) 1998-01-26
AU8258987A (en) 1988-06-23
HUT47956A (en) 1989-04-28
FI88303C (fi) 1993-04-26
IE873418L (en) 1988-06-17
IL84841A (en) 1992-07-15
HU201961B (en) 1991-01-28

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