KR910002895A - 펩티딜 아미노디올 레닌 억제제 - Google Patents

펩티딜 아미노디올 레닌 억제제 Download PDF

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KR910002895A
KR910002895A KR1019900011293A KR900011293A KR910002895A KR 910002895 A KR910002895 A KR 910002895A KR 1019900011293 A KR1019900011293 A KR 1019900011293A KR 900011293 A KR900011293 A KR 900011293A KR 910002895 A KR910002895 A KR 910002895A
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amino
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에이치. 로젠버그 사울
피.스피나 케네스
알.크롤리 스티블
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챨스 엠.브록
애보트 라보라토리즈
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • C07D213/02—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
    • C07D213/04—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
    • 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
    • C07D213/36—Radicals substituted by singly-bound nitrogen atoms
    • C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
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  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

내용 없음.

Description

펩티딜 아미노디올 레닌 억제제
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (11)

  1. 일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염, 에스테르 또는 프로드럭,
    상기식에서, A는 헤테로사이클릭, (헤테로사이클릭)알킬, (알콕시) (알킬)아미노알킬, (알콕시)아미노알킬, 치환된 카보닐옥시 또는 치환된 카보닐옥시 유사체이고; R1은 저급 알킬, 작용화 알킬, 아릴옥시, 티오아릴옥시 또는 아릴아미노이며; W는 -C(O)-또는 -CH(OH)-이고; U는 -CH2-또는-N(R2)-(여기서 R2는 수소 또는 저급 알킬이다)이며; R3은 저급 알킬, 알케닐, 알콕시알킬, 티오알콕시알킬, ((알콕시)알콕시)알킬, 아릴 알킬 또는 (헤테로 사이클릭)알킬이고; R4는 저급, 사이클로알킬알킬 또는 아릴알킬이며; R5는 수소, 저급알킬, 알케닐, 포르밀 또는 하이드록시 알킬이고; R8은 -OH 또는 -NH2이며; D는 작용화 메틸렌이다.
  2. 제1항에 있어서 A가 R13-Q-CH2-〔여기서 R13은 ((헤테로사이클릭)알킬)(알킬)아미노 또는 헤테로 사이클릭이고 Q는 -C(O)- 또는 -S(O)2-이다〕이고, R1이 아릴알킬이며, W가 -C(O)-이고, U가 -NH-이고, R3가 (헤테로사이클릭)알킬이며, R4가 사이클로헥실메틸이고, R5가 수소이며, R8이 -OH이고 D가 -CH(OH)CH2CH(CH3)2인 화합물
  3. 제2항에 있어서 A가 R13-C(O)-CH2-〔여기서 R13은 N-(피리딘-2-일에틸)-N-메틸아미노이다.〕이거나 A가 R13-S(O)2-CH2-〔여기서 R13은 N-메틸아제티딘-3-일 이다〕이고; R1이 벤질이며; R3이 티아졸릴메틸 또는 피라졸릴메틸인 화합물.
  4. 일반식(Ⅱ)의 화합물 또는 이의 약제학적으로 허용되는 염, 에스테르 또는 프로드럭,
    상기식에서, A는 R13-Q-CH2이고, 여기서 R13은 (1) 헤테로사이클릭 또는 (2) ((헤테로사이클릭)알킬)(알킬)아미노이고, Q-(1) -C(O)- 또는 (2) -S(O)2-이며, R1은 (헤테로사이클릭)알킬이며, R4는 사이클로헥실메틸이다.
  5. (2S, 3R, 4S)-2-아미노-1-사이클로핵실-3,4-디하이드록시-6-메틸헵탄의 (2R)-2-벤질-3-((2-피리딘-2-일에틸)(메틸)아미노카보닐)프로피오닐-L-(1-피라졸릴) Ala아미드; (2S, 3R, 4S)-2-아미노-1-사이클로핵실-3,4-디하이드록시-6-메틸헵탄의 (2R)-2-벤질-3-((2-피리딘-2-일에틸)(메틸)아미노카보닐)프로피오닐)-L-(4-티아졸릴) Ala아미드; (2S, 3R, 4S)-2-아미노-1-사이클로핵실-3,4-디하이드록시-6-메틸헵탄의 (2R)-2-벤질-3-(1-메틸아제티딘-3-일 설포닐)프로피오닐-L-(4-티아졸릴) Ala아미드; 및 (2S, 3R, 4S)-2-아미노-1-사이클로핵실-3,4-디하이드록시-6-메틸헵탄의 (2R)-2-벤질-3-((2-몰플린-4-일에틸)(메틸)아미노카보닐)프로피오닐-L-(1-피라졸릴) Ala아미드; 또는 이의 약제학적으로 허용되는 염, 에스테르 또는 프로드럭 중에서 선택된 화합물.
  6. 레닌 억제 치료를 필요로 하는 포유류에게 제1항의 화합물을 치료 유효량 투여함을 특징으로하여 레닌을 억제하는 방법.
  7. 고혈압 또는 울형성 심부전증의 치료를 필요로하는 포유류에게 치료 유효량의 제1항의 화합물을 단독으로 또는 기타 고혈압 치료제와 함께 투여함을 특징으로 하여, 고혈압 또는 율혈성 심부전증을 치료하는 방법.
  8. 약제학적 담체 및 치료 유효량의 제1항의 화합물을 함유함을 특징으로 하는 레닌 억제용 약제학적 조성물.
  9. 약제학적 담체 및 치료 유효량의 제1항의 화합물을 단독으로 또는 기타 고혈압 치료제와 함게 함유함을 특징으로 하는, 고혈압 또는 심부전증 치료용 약제학적 조성물.
  10. 일반식(1)의 화합물 또는 이의 활성화 유도체를 일반식(2)의 아민과 반응시킴을 특징으로 하여, 제1항의 화합물을 제조하는 방법.
    상기식에서 A, R1, R3, R4, R5, W, U 및 D는 제1항에서 정의한 바와 같다.
  11. a) 일반식(4)의 화합물 또는 이의 활성화 유도체를 일반식(2)의 아민과 반응시킨 다음, b) N-보호 그룹을 제거하고, 생성된 아민을 일반식(6)의 화합물 또는 이의 활성화 유도체와 커플링시킴을 특징으로 하여, W가 -C(O)-이고 U가 -N(R2)-인 제1항의 화합물을 제조하는 방법.
    상기식에서 A, R1, R2, R3, R4, R5, R8및 D는 제1항에서 정의한 바와 같고, P1은 N-보호그룹이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019900011293A 1989-07-26 1990-07-25 펩티딜 아미노디올 레닌 억제제 KR910002895A (ko)

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US38583689A 1989-07-26 1989-07-26
US385836 1989-07-26
US544072 1990-06-29
US07/544,072 US5063208A (en) 1989-07-26 1990-06-29 Peptidyl aminodiol renin inhibitors

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