KR920019814A - 아미노산 유도체 - Google Patents

아미노산 유도체 Download PDF

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KR920019814A
KR920019814A KR1019920006339A KR920006339A KR920019814A KR 920019814 A KR920019814 A KR 920019814A KR 1019920006339 A KR1019920006339 A KR 1019920006339A KR 920006339 A KR920006339 A KR 920006339A KR 920019814 A KR920019814 A KR 920019814A
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South Korea
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ylmethyl
alkyl
hydrogen
group
substituted
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KR1019920006339A
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English (en)
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브란카 퀴리코
하이츠 마리-폴르
나이트하르트 베르너
스타들러 하인츠
피아이라 에릭
보스틀 볼프강
Original Assignee
프리돌린 클라우스너, 롤란트 보러
에프. 호프만-라 로슈 에이지
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Application filed by 프리돌린 클라우스너, 롤란트 보러, 에프. 호프만-라 로슈 에이지 filed Critical 프리돌린 클라우스너, 롤란트 보러
Publication of KR920019814A publication Critical patent/KR920019814A/ko

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    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
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    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06—Dipeptides
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    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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Abstract

내용 없음

Description

아미노산 유도체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (34)

  1. 광학적으로 순수한 부분입체이성질체, 부분입체이성질체의 혼합물, 부분입체이성질성 라세미체 또는 부분입체이성질성라세미체의 혼합물 형태의 일반식(Ⅰ)의 아미노산 유도체 및 이들 화합물들의 약제학적으로 이용 가능한 염.
    상기 식에서, R1은 사이클로알킬, 페닐, 치환된 페닐, 나프틸, 티에닐, 피리딜, 퀴놀릴, 이소퀴놀릴 또는 벤질이고, R2는 수소 또는 메틸이며, R3는 수소, 하이드록시, 알킬, 알콕시, 알케닐옥시, 알킬티오, 알킬티오알킬 또는 알콕시카보닐, 또는 이미다졸-1-일메틸, 이미다졸-2-일메틸 또는 이미다졸-4-일메틸(이는 각각 탄소원자 및/또는 질소원자상에서 메틸화될 수 있다), 2-아미노이미다졸-4-일메틸, 5-요오도이미다졸-4-일메틸, 피라졸-1-일메틸, 피라졸-3-일메틸, 티아졸-2-일메틸, 티아졸-4-일메틸, 티아졸-5-일메틸, 2-아미노티아졸-4-일메틸, 티에닐메틸, 푸라닐메틸, 피리딜메틸, 아미노카보닐, 아미노카보닐알킬 또는 알콕시카보닐알킬이고, R4는 사이클로알킬, 치환된 사이클로알킬, 페닐 또는 할로페닐이며, R5는 사이클로알킬, 사이클로알킬알킬 또는 알킬이고, B는 황원자 또는 설피닐 또는 설포닐 그룹이며, A는 그룹(a)
    〔여기에서, R6, R7및 R8은 각각 독립적으로 수소 또는 알킬이고, R9는 수소, 알킬, 하이드록시알킬, 아미노, 알콕시카보닐아미노 또는 벤질옥시카보닐 아미노이며, n은 0 또는 1의 정수이고, X는 그룹 Y-CO- 또는 n이 정수 1인 경우 그룹 Z-O-〔여기에서, Y는 사이클로알킬아미노, 설포알킬아미노 또는 비스알콕시알킬아미노, 또는 피리딜알킬아미노 또는 모르폴리노알킬아미노(이는 각각 아미노 그룹에서 알킬에 의해 치환될 수 있다) ; 피라지닐알킬아미노(이는 질소원자 및/또는 아미노 그룹에서 알킬에 의해 치환될 수 있다) ; 4-피페리디닐알킬아미노(이는 질소 원자에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐 또는 하이드록시알킬에 의해 치환되고/되거나 아미노 그룹에서 ; 알킬에 의해 치환될 수 있다) ; 알콕시카보닐알킬 아미노, 하이드록시알콕시알킬아미노, 하이드록시알킬아미노, 비스하이드록시알틸아미노, 그룹 (RA)(RB)N-(여기에서, RA및 RB는 각각 독립적으로 수소 또는 알킬이거나 이들이 결합된 질소원자와 함께 포화된 5- 또는 6-원 헤테로사이클릭 환〈이는 추가의 헤테로원자로서 추가의 질소원자 또는 산소 또는 황원자를 함유하거나 옥소 그룹을 지닐 수 있거나(이로써 황원자는 또한 설피닐 또는 설포닐 그룹의 형태로 존재할 수 있다), 1개 또는 2개의 탄소원자 상에 알킬, 하이드록시, 하이드록시알킬 또는 알콕시알콕시에 의해 치환되거나 존재할 수 있는 제2질소 원자 상에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐 또는 하이드록시알킬에 의해 치환될 수 있거나, 임의로 존재하는 제2질소 원자는 산소원자, 알콕시알콕시알콕시, 사이클로알킬알콕시, 1, 3-디메틸디옥솔란-2-일알콕시, 그룹 (RA)(RB)N-알콕시, 천연 아미노데스옥시 당의 잔기 또는 R9이 수소 또는 알킬이 아닌 경우 또한 알콕시를 지닐 수 있다〉이다)이고, Z는 C5-C17알킬카보닐, 벤조일, 알콕시알킬카보닐, 사이클로알킬카보닐, 아미노알킬카보닐(이는 질소 원자에서 알콕시카보닐 또는 벤질옥시카보닐에 의해 치환될 수 있다) ; 알킬아미노카보닐, 페닐아미노카보닐 또는 R9가 수소 또는 알킬이 아닌 경우 또한 수소이다〕이다〕이다.
  2. 제1항에 있어서, R1이 사이클로알킬, 페닐, 치환된 페닐, 나프틸, 티에닐, 피리딜, 퀴놀릴, 이소퀴놀릴 또는 벤질이고, R2가 수소 또는 메틸이며, R3이 수소, 하이드록시, 알킬, 알콕시, 알케닐옥시, 알킬티오, 알킬티오알킬, 또는 알콕시카보닐, 또는 이미다졸-2-일메틸 또는 이미다졸-4-일메틸(이는 각각 탄소원자 및/또는 질소원자상에서 메틸화될 수 있다), 2-아미노이미다졸-4-일메틸, 5-요오도이미다졸-4-일메틸, 티아졸-4-일메틸, 티에닐메틸, 푸라닐메틸, 피리딜메틸, 아미노카보닐, 아미노카보닐알킬 또는 알콕시카보닐알킬이고, R4가 사이클로알킬, 치환된 사이클로알킬, 페닐 또는 할로페닐이며, R5가 사이클로알킬, 사이클로알킬알킬 또는 알킬이고, B가 황원자 또는 설피닐 또는 설포닐 그룹이며, R6, R7및 R8이 각각 독립적으로 수소 또는 알킬이고, R9가 수소, 알킬, 하이드록시알킬, 아미노, 알콕시카보닐아미노 또는 벤질옥시카보닐아미노이며, n이 0 또는 1의 정수이고, X가 그룹 Y-CO- 또는 n이 정수 1인 경우 그룹 Z-O-〔여기에서, Y는 사이클로알킬아미노, 설포알킬아미노, 비스알콕시알킬아미노, 또는 피리딜알킬아미노, 또는 4-피페리디닐알킬아미노(이는 질소원자에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐 또는 하이드록시알킬에 의해 치환될 수 있다) ; 알콕시카보닐알킬아미노, 하이드록시알콕시알킬아미노, 비스하이드록시알킬아미노, 그룹 (RA)(RB)N-(여기에서, RA및 RB는 각각 독립적으로 수소 또는 알킬이거나 이들이 결합된 질소원자와 함께 포화된 5- 또는 6-원 헤테로사이클릭 환〈이는 추가의 헤테로원자로서 추가의 질소원자 또는 산소 또는 황원자를 함유하거나(이로써 황원자는 또한 설피닐 또는 설포닐 그룹의 형태로 존재할 수 있다), 1개의 또는 2개의 탄소원자 상에서 알킬, 하이드록시, 하이드록시알킬 또는 알콕시알콕시에 의해 치환되거나 존재할 수 있는 제2질소 원자상에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐 또는 하이드록시알킬에 의해 치환될 수 있거나, 옥소그룹, 알콕시알콕시알콕시, 사이클로알킬알콕시, 1, 3-디메틸디옥솔란-2-일알콕시, 그룹(RA)(RB)N-알콕시, 천연 아미노데스옥시 당의 잔기 또는 R9이 수소 또는 알킬이 아닌 경우 또한 알콕시를 지닐 수 있다〉이다)이고, Z는 C5-C17- 알킬카보닐, 벤조일, 알콕시알킬카보닐, 사이클로알킬카보닐, 아미노알킬카보닐(이는 질소 원자에서 알콕시카보닐 또는 벤질옥시카보닐에 의해 치환될 수 있다) ; 알킬아미노카보닐, 페닐아미노카보닐 또는 R9가 수소 또는 알킬이 아닌 경우 또한 수소이다〕인 화합물.
  3. 제1항 또는 2항에 있어서, R1이 사이클로알킬, 페닐, 치환된 페닐, 나프틸, 티에닐 또는 피리딜, 특히 사이클로헥실, 페닐, 나프틸 또는 티에닐, 특히 페닐인 화합물.
  4. 제1항 내지 3항중 어느 한 항에 있어서, R2가 수소인 화합물.
  5. 제1항 내지 4항중 어느 한 항에 있어서, R3가 수소, 하이드록시, 알킬, 알콕시, 알릴옥시, 알킬티오, 알킬티오메틸, 알콕시카보닐, 이미다졸-1-일메틸, 이미다졸-4-일메틸, 2-아미노이미다졸-4-일메틸, 5-요오드이미다졸-4-일메틸, 피라졸-1-일메틸, 티아졸-4-일메틸, 티엔-2-일메틸, 푸란-2-일메틸, 피리딜 메틸 또는 아미노카보닐 특히 수소, 하이드록시, C1-C4-알킬, C1-C4-알콕시, 알릴옥시, C1-C4-알킬티오, C1-C4-알킬티오메틸, C1-C4-알콕시카보닐, 이미다졸-4-일메틸, 티아졸-4-일메틸 또는 피리딜메틸, 특히 이미다졸-4-일메틸 또는 3-피리딜메틸인 화합물.
  6. 제1항 내지 5항중 어느 한 항에 있어서, R4가 사이클로알킬 또는 페닐, 특히 사이클로헥실인 화합물.
  7. 제1항 내지 6항중 어느 한 항에 있어서, R5가 사이클로알킬 또는 알킬, 특히 사이클로프로필, 이소프로필 또는 부틸, 특히 사이클로프로필인 화합물.
  8. 제1항 내지 7항중 어느 한 항에 있어서, B가 설포닐인 화합물.
  9. 제1항 내지 8항중 어느 한 항에 있어서, R6및 R7이 수소 또는 C1-C4-알킬, 특히 메틸인 화합물.
  10. 제1항 내지 9항중 어느 한 항에 있어서, R8이 수소인 화합물.
  11. 제1항 내지 10항중 어느 한 항에 있어서, R9가 수소, 하이드록시알킬, 아미노, C1-C4-알콕시카보닐아미노 또는 벤질옥시카보닐아미노, 특히 수소, 3급-부톡시카보닐아미노 또는 벤질옥시카보닐아미노, 특히 수소인 화합물.
  12. 제1항 내지 11항중 어느 한 항에 있어서, n이 정수 0인 화합물.
  13. 제1항 내지 12항중 어느 한 항에 있어서, Y가 사이클로알킬아미노, 설포알킬아미노, 비스알콕시알킬아미노, 피리딜알킬아미노(이는 각각 아미노 그룹에서 알킬에 의해 치환될 수 있다) ; 4-피페리디닐알킬아미노(이는 질소 원자에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐, 또는 하이드록시알킬에 의해 치환될 수 있다) ; 알콕시카보닐알킬아미노, 하이드록시알콕시알킬아미노, 하이드록시알킬아미노, 비스하이드록시알킬아미노 또는 그룹〔여기에서, RA및 RB는 각각 독립적으로 수소 또는 알킬이거나 이들이 결합된 질소 원자와 함께 포화된 5- 또는 6-원 헤테로사이클릭 환(이는 추가의 질소원자 또는 산소 또는 황원자를 함유하거나 (이로써 황원자는 또는 설피닐 또는 설포닐 그룹의 형태로 존재할 수 있다), 1개 또는 2개의 탄소원자 상에서 알킬, 하이드록시, 하이드록시알킬 또는 알콕시알킬에 의해 치환되거나 존재할 수 있는 제2질소 원자상에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐 또는 하이드록시알킬에 의해 치환될 수 있다)이다〕, 특히 그룹 (Ra)(Rb)N-, 특히 피롤리디닐, 피레리디닐, 피페라지닐, 모르폴리닐, 티오모르폴리닐, 2-하이드록시메틸피롤리디닐, 3-하이드록시피롤리디닐, 3, 4-디하이드록시피롤리디닐, 4-하이드록시피페리디닐, 4-옥소피페리디닐, 3, 5-디메틸모르폴리닐, 4, 4-디옥소티오모르폴리닐, 4-옥소티오모르폴리닐, 벤질옥시카보닐아미노 -C1-C4- 알킬카보닐 또는 2, 6-디메틸모르폴리닐, 특히 모르폴리닐인 화합물.
  14. 제1항 내지 10항중 어느 한 항에 있어서, Z가 알콕시알킬카보닐, 사이클로알킬카보닐, 아미노알킬카보닐(이는 질소 원자에서 알콕시카보닐 또는 벤질옥시카보닐에 의해 치환될 수 있다), 또는 알킬아미노카보닐, 바람직하게는 C1-C4-알콕시-C1-C4-알킬카보닐, 사이클로프로필카보닐, 3급-부톡시카보닐아미노-C1-C4-알킬카보닐 또는 C1-C4-알킬아미노카보닐인 화합물.
  15. 제1항 내지 13항중 어느 한 항에 있어서, R1이 사이클로헥실, 페닐, 나프틸 또는 티에닐이고, R2가 수소이며, R3이 수소, 하이드록시, C1-C4-알킬, C1-C4-알콕시, 알릴옥시, C1-C4-알킬티오, C1-C4-알킬티오메틸, C1-C|4-알콕시카보닐, 이미다졸-4-일메틸, 티아졸-4-일메틸 또는 피리딜메틸이고, R4가 사이클로헥실이며, R5가 사이클로프로필, 이소프로필 또는 이소부틸이고, B가 설포닐이며, R6및 R7이 각각 메틸이고, R8이 수소이며, R9가 수소, 3급-부톡시카보닐아미노 또는 벤질옥시카보닐아미노이고, n이 0의 정수이며, Y가 피롤리디닐, 피페리디닐, 피페라지닐, 모르폴리닐, 티오모르폴리닐, 2-하이드록시메틸피롤리디닐, 3-하이드록시피롤리디닐, 3, 4-디하이드록시피롤리디닐, 4-하이드록시피페리디닐, 4-옥소피페리디닐, 3, 5-디메틸모르폴리닐, 4, 4-디옥소티오모르폴리닐, 4-옥소티오모르폴리닐 또는 2, 6-디메틸모프폴리닐인 화합물.
  16. (S)-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕-α-〔(S)-α-〔〔〔1-〔〔2-하이드록시-1-(하이드록시메틸)-1-메틸에틸〕카바모일〕-1-메틸에틸〕설포닐〕메틸〕하이드로신남아미도〕이미다졸-4-프로피온아미드, N-(3급-부톡시카보닐)글리신 2-〔〔(R 또는 S)-2-〔〔(S)-1-〔〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕카바모일〕-2-이미다졸-4-일메틸〕카바모일〕-3-페닐프로필〕설포닐〕-2-메틸프로필, 에스테르, 사이클로프로필메틸 2-〔〔(R)-2-〔〔(S)-1-〔〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디-하이드록시프로필〕카바모일〕-2-이미다졸-4-일에틸〕카바모일〕-3-페닐프로필〕설포닐〕-2-메틸프로피오네이트, (S)-α-〔(R 또는 S)-α-〔〔〔1-(2-피리딜메틸)카바모일〕-1-메틸에틸〕설포닐〕메틸〔하이드로신남아미도〕-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕이미다졸-4-프로피온아미드 또는 (S)-α-〔(R 또는 S〔〔〔1-〔(1-벤질-4-피페리디닐)카바모일〕-1-메틸에틸〕설포닐〕메틸〕하이드로신남아미도〕-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕이미다졸-4-프로피온아미드.
  17. 2-〔2-〔〔(S)-2-〔〔(S)-1-〔〔(2S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕카바모일〕-2-이미다졸-4-일메틸〕카바모일〕-3-페닐프로필〕설포닐〕-2-메틸프로피온아미도〕-2-데옥시-D-글루코피라노즈, 2-〔〔(S 또는 R)-2-〔〔(S)-1-〔〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕카바모일〕-2-이미다졸-4-일에틸〕카바모일〕-3-페닐프로필〕설포닐〕-2-메틸프로필메톡시아세테이트, 3급-부틸〔(R)-2-〔〔(S 또는 R)-2-〔〔(S)-1-〔〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프필-2, 3-디하이드록시프로필〕카바모일〕-2-이미다졸-4-일에틸〕카바모일〕-3-페닐프로필〕설포닐〕-2-(모르폴리노카보닐)에틸〕카바메이트, (S)-α-〔(R 또는 S)-α〔〔〔1-〔비스(2-메톡시에틸)카바모일〕-1-메틸에틸〕설포닐〕메틸〕하이드로신남아미도〕-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕이미다졸-4-프로피온아미드 또는 (S)-α-〔(S 또는 R)-α-〔〔〔1(R)-2-아미노-2-(모르폴리노카보닐)에틸〕설포닐〕메틸〕하이드로신남아미도〕-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕이미다졸-4-프로피온아미도.
  18. (S 또는 R)-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕-α-〔(S)-α-〔〔〔1-메틸-1-〔모르폴리노카보닐〕에틸〕설포닐〕메틸〕하이드로신남아미도〕-3-(티아졸릴-4-일)프로피온아미도.
  19. 3급-부틸〔(S)-2-〔〔(S 또는 R)-2-〔〔(S)-1-〔〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕카바모일〕-2-이미다졸-4-일에틸〕카바모일〕-3-페닐프로필〕설포닐〕-1-(메톡시카보닐)-2-메틸프로필〕카바메이트.
  20. (S)-N-〔(1S, 2R, 3S)-1-(사이클로렉실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕-α-〔(S)-α-〔〔〔1-(모르폴리노카보닐)-1-메틸에틸〕설포닐〕메틸〕하이드로신남아미도〕이미다졸-4-프로피온아미드.
  21. (S)-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕-α-〔(S)-α-〔〔〔1-〔(4-하이드록시피페리디노)카보닐〕-1-메틸에틸〕설포닐〕메틸〕하이드로신남아미도〕이미다졸-4-프로피온아미드.
  22. (S 또는 R)-N-〔(1S, 2R, 3S)-1-(사이클로헥실메틸)-3-사이클로프로필-2, 3-디하이드록시프로필〕-α-〔(S)-α-〔〔〔1-메틸-1〔모르폴리노카보닐〕에틸〕설포닐〕메틸〕하이드로신남아미도〕-3-(피리딘-3-일)프로피온아미드.
  23. 일반식(Ⅲ), (Ⅴ) 및 (ⅩⅩⅡ)의 화합물.
    상기 식에서, A는 그룹(a)
    이고,
    B는 황 원자 또는 설피닐 또는 설포닐 그룹이며, R1은 사이클로알킬, 페닐, 치환된 페닐, 나프틸, 티에닐, 피리딜, 퀴놀릴, 이소퀴놀릴 또는 벤질이고, R2는 수소 도는 메틸이며, R3는 수소, 하이드록시, 알킬, 알콕시, 알케닐옥시, 알킬티오, 알킬티오알킬 또는 알콕시카보닐, 또는 이미다졸-1-일메틸, 이미다졸-2-일메틸 또는 이미다졸-4-일메틸(이는 각각 탄소원자 및/또는 질소원자상에서 메틸화될 수 있다), 2-아미노이미다졸-4-일메틸, 5-요오도이미다졸-4-일메틸, 피라졸-1-일메틸, 피라졸-3-일메틸, 티아졸-2-일메틸, 티아졸-4-일메틸, 티아졸-5-일메틸, 2-아미노티아졸-4-일메틸, 티에닐메틸, 푸라닐메틸, 피리딜메틸, 아미노카보닐, 아미노카보닐알킬 또는 알콕시카보닐알킬이고, R6, R7및 R8은 각각 독립적으로 수소 또는 알킬이며, R9는 수소, 알킬, 하이드록시알킬, 아미노,알콕시카보닐아미노 또는 벤질옥시카보닐아미노이고, n은 0 또는 1의 정수이며, X는 그룹 Y-CO- 또는 n이 정수 1인 경우 그룹 Z-O-〔여기에서, Y는 사이클로알킬아미노, 설포알킬아미노, 비스알콕시알킬아미노, 또는 피리딜알킬아미노 또는 모르폴리노알킬아미노(이는 각각 아미노 그룹에서 알킬에 의해 치환될 수 있다) ; 피라지닐알킬아미노(이는 질소 원자 및/또는 아미노 그룹에서 알킬에 의해 치환될 수 있다) ; 4-피페리디닐알킬아미노(이는 질소원자에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐 또는 하이드록시알킬에 의해 치환되고/되거나 아미노 그룹에서 알킬에 의해 치환될 수 있다) ; 알콕시카보닐알킬아미노, 하이드록시알콕시알킬아미노, 하이드록시알킬아미노, 비스하이드록시알킬아미노, 그룹 (RA)(RB)N-(여기에서, Ra및 Rb는 각각 독립적으로 수소 또는 알킬이거나 이들이 결합된 질소원자와 함께 포화된 5- 또는 6-원 헤테로사이클릭 환〈이는 추가의 헤테로 원자로서 추가의 질소원자 또는 산소 또는 황원자를 함유하거나 옥소 그룹을 지닐 수 있거나(이로써 황 원자는 또한 설피닐 또는 설포닐 그룹의 형태로 존재할 수 있다), 1개 또는 2개의 탄소원자 상에서 알킬, 하이드록시, 하이드록시알킬 또는 알콕시알콕시에 의해 치환되거나 존재할 수 있는 제2질소 원자상에서 알킬, 벤질, 벤질옥시카보닐, 알콕시카보닐 또는 하이드록시알킬에 의해 치환될 수 있거나, 임의로 존재하는 제2질소 원자는 산소원자, 알콕시알콕시알콕시, 사이클로알킬알콕시, 1, 3-디메틸디옥솔란-2-일알콕시, 그룹 (Ra)(Rb)N-알콕시, 천연 아미노데스옥시 당의 잔기 또는 R9이 수소 또는 알킬이 아닌 경우 또한 알콕시를 지닐 수 있다〉이다)이고, Z는 C5-C17-알킬카보닐, 벤조일, 알콕시알킬카보닐, 사이클로알킬카보닐, 아미노알킬카보닐(이는 질소 원자에서 알콕시카보닐 또는 벤질옥시카보닐에 의해 치환될 수 있다) ; 알킬아미노카보닐, 페닐아미노카보닐 또는 R9가 수소 또는 알킬이 아닌 경우 또한 수소이다〕이다.
  24. 제1항 내지 22항중 어느 한 항에 있어서, 치료학적 활성 물질로서 사용하기 위한 아미노산 유도체.
  25. 제1항 내지 22항중 어느 한 항에 있어서, 고혈압 및 심부전증의 조절 또는 예방에 사용하기 위한 아미노산 유도체.
  26. (a) 일반식(Ⅱ)의 화합물을 일반식(Ⅲ)의 산 또는 이의 활성화된 유도체와 반응시키거나, (b) 일반식(Ⅳ)의 화합물을 일반식(Ⅴ)의 산 또는 이의 활성화된 유도체와 반응시키거나, (c) A가 유리 1급 또는 2급 아미노 그룹 및/또는 유리 1급 또는 2급 하이드록시 그룹을 갖는 일반식(Ⅰ)의 화합물을 제조하기 위해, 일반식(Ⅰa)의 화합물로부터 N- 또는 O- 보호그룹(들)을 절단시키고, (d) 필요한 경우, 부분입체이성질성 라세미체의 혼합물을 부분입체이성질성 라세미체 또는 광학적으로 순수한 부분입체이성질체로 분리시키고/시키거나, (e) 필요한 경우, 부분입체이성체의 혼합물을 광학적으로 순수한 부분입체이성체로 분리시키고/시키거나, (f) 필요한 경우, 상기 단계들에서 수득된 화합물을 약제학적으로 이용가능한 염으로 전환시킴을 특징으로 하여, 제1항 내지 22항에 따른 화합물을 제조하는 방법.
    상기 식에서, R31은 수소, 알킬, 알킬티오알킬 또는 알콕시카보닐, 또는 이미다졸-1-일메틸, 이미다졸-2-일메틸 또는 이미다졸-4-일메틸(이는 각각 탄소원자 및/또는 질소원자 상에서 메틸화될 수 있다), 2-아미노이미다졸-4-일메틸, 5-요오드이미다졸-4-일메틸, 피라졸-1-일메틸, 피라졸-3-일메틸, 티아졸-2-일
    메틸, 티아졸-4-일메틸, 티아졸-5-일메틸, 2-아미노티아졸-4-일메틸, 티에닐메틸, 푸라닐메틸, 피리딜메틸, 아미노카보닐, 아미노카보닐알킬 또는 알콕시카보닐알킬이고, R1내지 R5, A 및 B는 제1항에서 정의한 바와 같고, A1은 A가 N- 또는 O- 보호그룹을 갖는 경우 A에서의 정의와 같다.
  27. 제1항 내지 22항중 어느 한 항에 따른 아미노산 유도체 및 치료학적 불활성 부형제를 함유하는 약제.
  28. 제1항 내지 22항중 어느 한 항에 따른 아미노산 유도체 및 치료학적 불활성 부형제를 함유하는 고혈압 및 심부전증을 조절 또는 예방하기 위한 약제.
  29. 질환을 조절 또는 예방하기 위한 제1항 내지 22항중 어느 한 항에 따른 아미노산 유도체의 용도.
  30. 고혈압 및 심부전증을 조절 또는 예방하기 위한 제1항 내지 22항중 어느 한 항에 따른 아미노산 유도체의 용도.
  31. 고혈압 및/또는 심부전증에 대한 약제를 제조하기 위한 제1항 내지 22항중 어느 한 항에 있어서, 제26항에 따른 아미노산 유도체의 용도.
  32. 제1항 내지 22항중 어느 한 항에 있어서, 제 26항에 따른 방법 또는 이의 화학적 등가법에 의해 제조된 아미노산 유도체.
  33. 명세서에 기술된 바와 같은 발명.
  34. 고혈압 및/또는 심부전증의 치료가 필요한 환자에게 제1항 내지 22항중 어느 한 항에 따른 아미노산 유도체의 유효량을 투여함을 특징으로 하여, 고혈압 및/또는 심부전증을 치료하거나 예방하는 방법.
    ※ 참고사항 : 최초출원 내용에 의하여 공개되는 것임.
KR1019920006339A 1991-04-17 1992-04-16 아미노산 유도체 KR920019814A (ko)

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