KR920006326A - 새로운 아미노산 유도체, 그것의 제조방법 및 그것을 함유하는 약학적 조성물 - Google Patents

새로운 아미노산 유도체, 그것의 제조방법 및 그것을 함유하는 약학적 조성물 Download PDF

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KR920006326A
KR920006326A KR1019910016085A KR910016085A KR920006326A KR 920006326 A KR920006326 A KR 920006326A KR 1019910016085 A KR1019910016085 A KR 1019910016085A KR 910016085 A KR910016085 A KR 910016085A KR 920006326 A KR920006326 A KR 920006326A
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compound
methyl
morpholinocarbonyl
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thiomorpholinocarbonyl
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게이지 헴미
마사히로 네야
히로시 마루사와
신야 와따나베
마사시 하시모또
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후지사와 도모끼찌로오
후지사와 약구힝고교 가부시끼가이샤
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Priority claimed from GB919105580A external-priority patent/GB9105580D0/en
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Publication of KR920006326A publication Critical patent/KR920006326A/ko

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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
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Abstract

내용 없음

Description

새로운 아미노산 유도체, 그것의 제조방법 및 그것을 함유하는 약학적 조성물
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (14)

  1. 하기의 구조식을 갖는 화합물 및 그것의 약학적으로 허용되는 염.
    상기식에서, R1은 모르폴리노카보닐, 티오모르폴리노카보닐, 헥사하이드로-1H-아제핀-1-일카보닐. 옥타하이드로아조신-1-일카보닐, 피페리디노카보닐, 저급 알카노일, 디프로필카바모일, 테트라하이드로 이소퀴놀릴카보닐 또는 헤테로고리기이며, R2는 저급 알킬 R3는 아릴 및 사이클로(저급)알킬로 구성된 그룹에서 선택된 치환체와 치환될 수 있는 저급 알킬, R4는 저급 알킬, X는 저급 알킬렌, Y1은 단일 결합 또는(여기에서, R5는 저급알킬, Y2는 -NH- 또는 -O-인데, 1)R1이 모르폴리노카보닐이고, Y1이일때 2)R1이 모르폴리노카보닐 또는 티오모르폴리노 카보닐이고, Y1이 단일 결합이고, Y2가 -O-일때; 또는 3)
    R1이 저급 알카노일이고, Y2가 -O-일때, R3가 이소부틸, 2-에틸부틸 또는 아릴 및 사이클로(저급)알킬로 구성된 그룹에서 선택된 치환체와 치환된 저급 알킬 인것.
  2. 제1항에 있어서, R1은 모르폴리노카보닐, 티오모르폴리노카보닐, 헥사하이드로-1H-아제핀-1-일카보닐. 옥타하이드로아조신-1-일카보닐, 피페리디노카보닐 또는 저급 알카노일이고, R3가 저급 알킬이며, Y2가 -NH-인 것으로, R1이 모르폴리노카보닐이고, Y1이일때, R3가 이소부틸 또는 2-에틸부틸인것.
  3. 제2항에 있어서, R1이 티오모르폴리노카보닐, 헥사하이드로-1H-아제핀-1-일카보닐, 피페리디노카보닐 또는 저급 알카노일이고, Y1이인것.
  4. 제2항에 있어서, R1이 모르폴리카보닐, 티오모르폴리노카보닐, 헥사하이드로-1H-아제핀-1-일카보닐 또는 저급 알카노일이고, R3가 이소부틸 또는 2-에틸부틸 인것.
  5. 제4항에 있어서, R1이 모르폴리노카보닐 또는 티오모르폴리노카보닐이고, R2가 메틸, R3가 메틸, X가 에틸렌이며, Y1이 단일결합 또는(여기에서 R5는 메틸)인것.
  6. 제5항에 있어서, 화합물이 (2S,3S)-2-[Nα-[N-메틸-N-{2-(N-모르폴리노카보닐
    -N-메틸아미노)에틸}아미노카보닐]-L-페닐알라닐]-Nα-메틸-L-히스티딜]아미노-1-사이클로헥실-3-하이드록시-5-메틸헥산, 그것의 하이드로클로라이드, 그것의 황산염, 그것의 메탄설폰산염 또는 그것의 벤젠 설폰산염인것.
  7. 제5항에 있어서, 화합물이 (2S,3S)-2-[Nα-[N-메틸-N-{2-(N-모르폴리노카보닐
    -N-메틸아미노)에틸}아미노카보닐]-L-페닐알라닐]-Nα-메틸-L-히스티딜]아미노-1-사이클로헥실-3-하이드록시-5-메틸헥산, 또는 그것의 하이드로클로라이드인것.
  8. 제5항에 있어서, 화합물이 (2S,3S)-2-[Nα-[N-메틸-N-{2-(N-모르폴리노카보닐
    -N-메틸아미노)에틸}아미노카보닐]-L-페닐알라닐]-Nα-메틸-L-히스티딜]아미노-1-사이클로헥실-3-하이드록시-5-에틸헵탄 또는 그것의 하이드로클로라이드인것.
  9. 제5항에 있어서, 화합물이 (2S,3S)-2-[Nα-[N-메틸-N-{2-(N-모르폴리노카보닐
    -N-메틸아미노)에틸}아미노카보닐]-L-페닐알라닐]-Nα-메틸-L-히스티딜]아미노-1-사이클로헥실-3-하이드록시-5-에틸헵탄 또는 그것의 하이드로클로라이드인것.
  10. 하기식의 화합물.
    (상기식에서, R7은 수소 또는 N-보호기이고, R2및 R3는 각각 상기 정의된 바와 같다) 또는 아미노기에서 그것의 반응성 유도체 또는 그것의 염;과 하기식의 화합물.
    (상기식에서, R1, R4, X, Y1및 Y2는 각각 상기 정의된 바와 같다) 또는 카복시기에서 그것의 반응성 유도체 또는 그것의 염;을 반응시키고, 필요하다면 N-보호기를 제거하는 것을 포함하는 하기식의 화합물 또는 그것의 염을 제조하는 방법.
    상기식에서, R1은 모르폴리노카보닐, 티오모르폴리노카보닐, 헥사하이드로-1H-아제핀-1-일카보닐. 옥타하이드로아조신-1-일카보닐, 피페리디노카보닐, 저급 알카노일, 디프로필카바모일, 테트라하이드로 이소퀴놀릴카보닐 또는 헤테로 고리기이며, R2는 저급 알킬 R3는 아릴 및 사이클로(저급)알킬로 구성된 그룹에서 선택된 치환체와 치환될 수 있는 저급 알킬, R4는 저급 알킬, X는 저급 알킬렌, Y1은 단일 결합 또는(여기에서, R5는 저급알킬, Y2는 -NH- 또는 -O-인데, 1)R1이 모르폴리노카보닐이고, Y1이일때 2)R1이 모르폴리노카보닐 또는 티오모르폴리 노카보닐이고, Y1이 단일 결합이고, Y2가 -O-일때; 또는 3)R1이 저급 알카노일이고, Y2가 -O-일때, R3는 이소부틸, 2-에틸부틸 또는 아릴 및 사이클로(저급)알킬로 구성된 그룹에서 선택된 치환체와 치환된 저급 알킬이다.
  11. 약학적으로 허용되고, 실질적으로 비독성인 담체나 부형제와 결합된 형태로 제1항의 화합물을 활성성문으로 함유한 약학적 조성물.
  12. 제1항의 화합물을 약제로 사용하는 것.
  13. 인간 및 동물에 있어서, 제1항의 화합물을 투여하는 것을 포함하는 고혈압, 심장병, 신장질환 또는 녹내장의 치료 및/또는 예방법.
  14. 인간 및 동물에 있어서, 고혈압, 심장병, 신장질환 또는 녹내장의 치료 및/또는 예방용 의약의 제조에 제1항의 화합물을 사용하는 것.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019910016085A 1990-09-17 1991-09-16 새로운 아미노산 유도체, 그것의 제조방법 및 그것을 함유하는 약학적 조성물 KR920006326A (ko)

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GB909020305A GB9020305D0 (en) 1990-09-17 1990-09-17 New amino acid derivatives,a process for the preparation thereof and pharmaceutical composition comprising the same
GB9020305.0 1990-09-17
GB919105580A GB9105580D0 (en) 1991-03-15 1991-03-15 New amino acid derivatives,a process for the preparation thereof and pharmaceutical composition comprising the same
GB9105580.6 1991-03-15

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PT98984A (pt) 1992-07-31
JPH08283244A (ja) 1996-10-29
FI914309A0 (fi) 1991-09-13
IL99389A0 (en) 1992-08-18
US5491132A (en) 1996-02-13
FI914309A (fi) 1992-03-18
RU2057124C1 (ru) 1996-03-27
CN1063691A (zh) 1992-08-19
JPH04279570A (ja) 1992-10-05
IE913220A1 (en) 1992-02-25
JP2641823B2 (ja) 1997-08-20
HUT59419A (en) 1992-05-28
NO913644L (no) 1992-03-18
AU646076B2 (en) 1994-02-03
CA2051455A1 (en) 1992-03-18
TW212176B (ko) 1993-09-01
NO913644D0 (no) 1991-09-16
AU8379091A (en) 1992-03-19
EP0476515A1 (en) 1992-03-25
HU912979D0 (en) 1992-01-28
CN1030922C (zh) 1996-02-07

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