KR960010612A - 2,9- 디아미노- 및 2- 아미노-8- 카르바모일-4- 히드록시- 알칸산 아미드 유도체 - Google Patents

2,9- 디아미노- 및 2- 아미노-8- 카르바모일-4- 히드록시- 알칸산 아미드 유도체 Download PDF

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KR960010612A
KR960010612A KR1019950029994A KR19950029994A KR960010612A KR 960010612 A KR960010612 A KR 960010612A KR 1019950029994 A KR1019950029994 A KR 1019950029994A KR 19950029994 A KR19950029994 A KR 19950029994A KR 960010612 A KR960010612 A KR 960010612A
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South Korea
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amide
amino
hydroxy
butyl
ylcarbonyl
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KR1019950029994A
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라제티 비토리오
뤼에거 하인리히
클라우스 마이바움 위르겐
마 로베르트
그뤼터 마르쿠스
끌로드 꼬헹 니셍
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베르너 발데크
시바-가이기 아게
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Publication of KR960010612A publication Critical patent/KR960010612A/ko

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  • Quinoline Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

본 발명은 고혈압 치료용 의양의 활성 성분으로 사용될 수 있는 하기 일반식(Ⅰ)의 화합물 및 그의 염에 관한 것이다.
상기 식 중, R1은 아릴아미노, N-아릴-N-(저급 알콕시-저급 알킬)-아미노, N-아릴-N-아릴-저급알킬-아미노 또는 고리 질소 원자를 통해 결합되어 있는 헤테로사이클이고, X는 카르보닐 또는 메틸렌기이고, R2및 R3는 서로 독립적으로 수소 또는 저급 아킬이거나 또는 이들이 부착되어 있는 탄소 원자와 함께 시클로알킬리덴기를 형성하고, R4는 소소, 저급 알킬, 저급 알카노일 또는 저급 알콕시카르보닐이고, R5는 히드록실, 저급 알카노일옥시 또는 저급 알콕시카르보닐옥시이고, R6은 수소, 저급 알킬,저급 알케닐, 저급 알키닐, 시클로알킬, 시클로알킬, 저급 알킬, 알릴-저급 알킬 또는 헤테로아릴 고리에 5-7개의 고리 원자를 갖는 헤테로아릴-저급 알킬이고, R7은 수소 또는 저급 알킬이거나 또는 R8은 지방족, 지환족-지방족 또는 헤테로아릴지방족기이다.

Description

2,9-디아미노-및 2-아미노-8-카르바모일-4-히드록시-알칸산 아미드 유도체
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Claims (8)

  1. 하기 일반식(Ⅰ)의 화합물 및 그의 염.
    상기 식 중, R1은아릴아미노, N-아릴-N-(저급 알콕시-저급 알킥)-아미노, N-아릴-N-알릴-저급 알킬-아미노 또는 고리 질소 원자를 통해 결합되어 있는 헤테로사이클이고, X는 카르보닐 또는 메틸렌기이고, R2및 R3는 서로 독립적으로 수소 또는 저급 아킬이거나 또는 이들이 부착되어 있는 탄소 원자와 함께 시클로알킬리덴기를 형서하고, R4는 수소, 저급 알킬, 저급 알카노일 또는 저급 알콕시카르보닐이고, R5는 히드록실, 저급 알카노일옥시 또는 저급 알콕시카르보닐옥시이고, R6은 수소, 저급 알킬, 저급 알케닐, 저급 알키닐, 시클로알킬, 시클로알킬-저급 알킬, 아릴-저급 알킬 또는 헤테로아릴 고리에 5-7개의 고리 원자를 갖는 헤테로아릴-저급 알킬이고, R7은 수소 또는 저급 알킬이거나 또는 R6및 R7은 이들이 부착되어 있는 탄소 원자와 함께 시클로알킬리덴기를 형성하고,R8은 지방족-지방족 또는 헤테로아릴지방족이다.
  2. 제1항에 있어서, R1이 아닐리노, 나프틸아미노, 비치환되거나 페닐 또는 나프틸 부분이 C1-C4알콕시, C1-C4알콕시카르보닐, 카르바모일- C1-C4알콕시, C1-C4알카노일아미노-C1-C4알킬,C1-C4알카르보닐아미노-C1-C4알킬, 할로겐 및(또는 )-산화될 수 있는 피리딜에 의해 일치환 또는 이치환된 N-페닐-(C1-C4알콕시-C1-C4알킬)아미노 또는 N-페닐-N-(페닐-C1-C4알킬)아미노 또는 비치환되거나 각각 C1-C4알킬, 히드록시-C1-C4알킬, C1-C4알콕시, C1-C4알킬, C3-C5알케닐옥시-C1-C4알킬, C1-C4알콕시-C1-C4알콕시-C1-C4알콕시-C1-C4알킬, C1-C4알콕시카르보닐아미노-C1-C4알킬, C1-C4알콕시이미노-C1-C4알킬, 카르복시, C1-C7알콕시카르보닐, 시아노, 카르바모일, N-C1-C7알킬카르바모일, N-N-디-C1-C4알킬카르바모일, C1-C4알콕시-C1-C4알킬카르바모일, N-카르복시-C1-C4알킬카르바모일, 모르폴리노카르보닐, C1-C4알콕시, C1-C4알콕시-C1-C4알콕시, 1-7알카노일옥시, 벤조일옥시, C1-C4알카노일아미노알아미토, N- C1-C4알카르바모일아미노 또는 5원 또는 6원 N-N-(1-옥소-저급 아킬렌)아미노 또는 N,N-(1-옥소-2-옥사-저급 알킬렌)아미노, C1-C7알카노일, 옥소, 니트로, C1-C4알칸술포닐, 및(또는) 할로겐에 의해-, 이- 또는 삼치환된 피롤리디노, 피페리디노ㅡ 피레라지노, 모르폴리노 또는 티오모르폴리노, 인돌린-1-일, 이소인돌린-2-일, 2,3-디히드로벤즈이미다졸-1-일, 1,2,3,4,5-테트라히드로퀴놀-1-일, 1,2,3,4-테트라히드로이소퀴놀-2-일, 1,2,3,4-테트라히드로-1,3-벤조디아진-1-일, 1,2,3,4-테트라히드로-1,4-벤조디아진-1-일, S, S-이산화될 수 있는 3,4-디히드로-2H-1,4-벤조사진-4-일, 3,4-디히드로-2H-디히드로-2H-1,3-벤조티아진-1-일, 3,4,5,6,7-헥사히드로- 2H1,4-벤족사진-4-일, 3,4,5,6,7,8-헥사히드로-2H-1,4-벤즈티아진-4-일, 2,3,4,5-테트라히드로-1H-1-벤즈[6,7-b]아제핀-1-일 또는 5,6-디히드로페나트리딘-5-일이고, X가 카르보닐이고, R2및 R3가 서로 독립적이고 수소 또는 C1-C4알킬이거나 또는 이들이 부착되어 있는 탄소 원자와 함께 3 내지 8원 시클로알킬리덴을 형성하고, R4가 수소 또는 C1-C4알킬이고, R5가 히드록실이고, R6이 수소, C1-C4알킬, , 3 내지 8원 시클로알킬, 또는 페닐-C1-C4알킬이고, R7이 수소이거나 또는 R6및 R7이 이들이 부착되어 있는 탄소 원자와 함 3 내지 8원시클로알킬리덴을 형성하고, R8이 C1-C4알킬, C1-C4알콕시-C1-C4알킬, 아미노-C1-C4알킬, N-C1-C4알킬아미노-C1-C4알킬, N,N-디-C1-C4알킬아미노-C1-C4알킬, 5 또는 6원 N, N-저급 알킬렌아미노-C1-C4알킬 및 N, N-(아자)-, N,N-(옥사)-, N,N-(티아)-저급 알킬렌아미노-C1-C4알킬, 카르바모일-C1-C4알킬, N-C1-C4알킬카르바모일, N, N-디-C1-C4알킬카르바모일, 시아노-C1-C4알킬 또는 피리딜-C1-C4알킬인, 일반식(Ⅰ)의 화합물 및 그의 염, 특히 그의 제약상 허용되는 염.
  3. 제1항에 있어서, R1이 하기 일반식(Ⅰa) 또는 (Ⅰb)의 기
    (상기 식 중, A는 직접 결합, 메틸렌, 에틸렌, 이미노, 옥시 또는 티오기이고, R9은 C1-C4알콕시-C1-C4알킬,, C3-C5알케닐옥시-C1-C4알킬, C1-C4알콕시-C1-C4알콕시-C1-C4알킬, C1-C4알콕시카르보닐아미노-C1-C4알킬, C1-C4알콕시이미노-C1-C4알킬, 페닐, C1-C4알콕시카르보닐, 시아노, 카르바모일, N-C1-C4알킬카르바모일, C1-C4알콕시-C1-C4알킬카르바모일, C1-C4알콕시, C1-C4알콕시-C1-C4알시, C1-C7알카노일옥시, 벤조일옥시, N-C1-C4알킬카르바모일아미노, C1-C4알미노, C1-C7알콕시카르보닐아미노, 3 내지 6언 시클로알킬카르보밀 아미노, C1-C4알콕시, C1-C4알카노일아미노, 또는 5 또는 6원, N, N-(1-옥소-저급 알킬렌)아미노 또는 N,N-(1-옥소-2-옥사-저급 알킬렌)아미노이거나, 또는 N-C1-C4알킬카르바모일아미노이고, R10은 수소 또는C1-C4알킬이고, R11은 수소 또는 할로겐이고, R12는 C1-C4알콕시-C1-C4알킬임)이고, X가 카르보닐이고, R2및 R3이 서로 독립적으로 수소 또는 C1-C4알킬이거나 또는 이들이 부착되어 있는 탄소 원자와 함께 3 내지 8원 시클로알킬리덴을 형성하고, R4가 수소 또는 C1-C4알카노일이고, R5가 히드록실이고, r6이 수소, C1-C4알킬, 3 내지 8원 시클로알킬, 또는 페닐-C1-C4알킬이고, R7이 수소이고, R8이 C1-C7알킬, C1-C4알콕시-C1-C4알킬, 아미노-C1-C4알킬, N-C1-C4알킬아미노-C1-C4알킬, N,N-디-C1-C4알킬아미노,C1-C4알킬, 5또는 6원, N,N-저급 알킬렌아미노-C1-C4알킬 또는 N,N-(아자), N,N-(옥사)-또는 N,N-(티아)-저급 알킬렌아미노-C1-C4알킬, 또는 피리딜-C1-C4알킬인, 일반식(Ⅰ)의 화합물 및 그의 염, 특히 그의 제약상 허용되는 염.
  4. 제1항에 있어서, 하기 일반식(Ⅰc)의 화합물 또는 그의 염.
    상기 식 중, R1, R2, R3, R4, R5, R6, R7, R8, R8, R9, R10및 R11은 제1항, 제2항에 또는 제3항에서 정의한 바와 같다.
  5. 제1항에 있어서, 하기 일반식(Ⅰd)의 화합물 또는 그의 염.
    상기 식 중, A는 메질렌, 옥시 또는 티오기이고, R2및 R3는 C1-C4알킬이고, R4는 수소 또는 C1-C4알카노일이고, R5는 C1-C4알킬 또는 페닐-C1-C4알킬이고, R5은 C1-C7알킬이고, R9은 C1-C4알콕시카르보닐아미노, C1-C4알콕시-C1-C4알콕시-C1-C4알킬, C1-C4알콕시-C1-C4알킬 또는 N-C1-C4알킬카르바모일이다.
  6. 4(S)-아미노-3(S)-히드록시-1(R), 6,6-트리메틸-헵타디카르복실산-1-(N-부틸)아미드-7-[N-(4-브로모나프트-1-일)]아미드; 4(S)-아미노-4(S)-히드록시-2(R), 7,7,-트리메리ㅌ-8-(5,6-디히드로페난트리디노카르보닐)-옥탄산 (N-부틸)아미드; 4(S)-아미노-4(S)-히드록시-2(R),7,7,-트리메틸-8-(1,2,3,4-테트라히드로이소퀴놀린-2-일카르보닐)-옥탄산 (N-부틸)아미드; 4(S)-아미노-3-(S)-히드록시-1(R),6,6-트리메틸헵탄디카르복실산-1-(N-부틸)아미드-7-[N-[[2-(포르밀아미노메틸)페닐]아미드; 4(S)-포르밀아미노-3-(S)-히드록시-1-(R)6,6-트리메틸헵탄디카르복실산-1-(N-부틸)아미드-7-(N-페닐)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7,-트리메틸-8-[3(R)-또는 3(S)-에톡시카르보닐피페리딘-1-일카르보닐]옥탄산(N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2-(R),7,7,-트리메틸-8-[3(R)-또는 3(S)-에톡시카르보닐피페리딘-1-일카르보닐]옥탄산(N-부틸)아미노-4(S)-히드록시-2(R),7,7-트리메틸-9-(1,2,3,4-테트라히드로퀴놀린-1-일)-노난산(N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2-(R),7,7-트리메틸-8-[3(R,S)-카르복시-1,2,3,4-테르라히트로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2-(R),7,7,-트리메틸-8-[-2(R,S)-에톡시카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드, 또는 그의 염; 5(S)-포르밀아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-에톡시카르보닐-4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드;5(S)-아미노-4(S)-히드록시-2(R),7,7,-트리메틸-8-[2(R,S)-메톡시카르보닐-3,4-디히드로-2H-1,4-벤즈티아진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-에톡시카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-t-부톡시카르보닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; (S)-아미노-4(S)-히드록시-2(R),7,7,-트리메틸-8-[3(R)-또는 3(S)-메토기카르보닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7,-트리메틸-8-[3(R,S)-디메틸아미노카르보닐-1,2,3,4-테르라히드로퀴퀴놀린-1-일카르보닐]-옥탄산(N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-부틸아미노카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)-아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-부틸아미노카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드, 또는 그의 염; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-모르폴리노카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드, 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)아세틸-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-글리시닐카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-에톡시카르보닐-1,2,3,4-테르라히드로퀴놀린-2H-1-일카르보닐]-옥탄산 (N-부틸)아미드 또는 그의 염; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-이소프로폭시카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[6-브로모-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[6-브로모-3(R,S)-에톡시카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-디메틸-8-[2(R,S)-메톡시카르보닐-3,4-디히드로-2H-1,4-벤조티아진-1,4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3,3-비스-(메톡시카르보닐)-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-이소프로필-7,7-디메틸-8-[2(R,S)-메톡시카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-이소프로필-7,7-디메틸-8-[2(R,S)-메톡시카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-t-부톡시카르보닐아미노-4-(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[2(R,S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[2(R,S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-이소프로필-7,7-디메틸-8-(1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-이소프로필-7,7-디메틸-8-(1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-이소프로필-7,7-디메틸-8-2(R,S)-카르바모일-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-메톡시카르보닐-3.4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-이소프로필-7,7-디메틸-8-[3(R,S)-히드록시메틸-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 4(S)-아미노-3-(S)-히드록시-(R),6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)아미드-7-[N-[2-(3-피리딜)페닐]아미드; 4(S)-아미노-3(S)-히드록시-1(R)-6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)-아미드-7[N-(2-N-옥시도-3-피리딜)페닐]아미드; 5(S)-포르밀아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[(2(R,S)-메톡시카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐-]]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-7,7-트리메틸-8-S,S-디옥소-3,4-디히드로-1H-2,4-벤조티아진-4-일카르보닐)옥탄산 (N-부틸)-아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-메톡시카르보닐-3.4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-이소프로필-7,7-트리메틸-8-(7-니트로-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-메톡시카르보닐-3.4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-이소프로필-7,7-디메틸-8-[3(R,S)-에톡시카르보닐-7-니트로-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-메톡시카르보닐-3.4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-에톡시카르보닐-2(R,S)-메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R,S)-메톡시카르보닐-3.4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-이소프로필-7,7-트리메틸-8-[3(R,S)-메틸술포닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-메틸술포닐-1,2,3,4-테르라히드로퀴나졸린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-메틸카르보닐아미노--1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 4(S)-아미노-3(S)-히드록시-1(R)-6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)이미드-7-[N-(2-카르바모일에톡시페닐)아미드; 4(S)-아미노-3(S)-히드록시-1(R)-6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)이미드-7-[N-(2-카르바모일메톡시-5-메톡시페닐)아미드; 4(S)-아미노-3(S)-히드록시-1(R)-6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)아미드-7-[N-2-(카르바모일메톡시-4-(메톡시카르보닐)페닐)아미드; 4(S)-아미노-3(S)-히드록시-1(R)-6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)아미드-7-[N-2-(카르바모일메톡시-5-(메톡시카르보닐)페닐)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-이소프로필-7,7-디메틸-8-[3(R,S)-메틸아미노카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-메톡시메틸-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-포르밀아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[2(R,S)-메톡아미노카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[3-아세틸-2,3디히드로-1H-벤즈이미다조-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-에틸술포닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-메틸카르보닐옥시-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[2(R,S)-메틸카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[4-아세틸-3(R,S)-메틸아미노카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-메틸아미노카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐)-옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[2(R,S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(S)-이소프로필-7,7-트리메틸-8-[2(R,S)-메톡시에틸아미노카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R), 7(S)-디메틸-8-[2(R,S)-에톡시카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-포르밀아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-2(R)-벤질-4(S)-히드록시-7,7-디메틸-8-[3(R) 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-2(R)-부틸-4(S)-히드록시-7,7-디메틸-8-[3(R) 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4-(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-1,2,3,4-테트라히드로퀴나졸린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-페닐카르보닐옥시-1,2,3,4-테르탈히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-시아노-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-t-부톡시카르보닐아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-메톡시카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-메톡시카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7(R)-디메틸-8-[2(R,S)-에톡시카르보닐-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-메톡시-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-메톡시메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R) 또는 -3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R) 또는 -3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-아릴옥시메틸-3,4-디히드로--2H-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R)7,7-트리메틸-8-[2(R,S)-프로필옥시메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-메톡시메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-이소프로필-7,7-디메틸-8-[2(R( 또는 -2(S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[2(R)- 또는 -2(S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-메틸아미노카르보닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐메틸]시클로프로필]-2(R)-메틸-헥산산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-메톡시에틸카르보닐-3,4-디히드로-2H-1,4--일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-2(S)-이소프로필-7,7-디메틸-8-[3(R,S)-메톡시메틸-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-2(S)-히드록시-2(R)7,7-트리메틸-8-[3(R) 또는 3(S)-에톡시카르보닐인돌린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R) 또는 3(S)-에톡시카르보닐인돌린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R) 또는 3(S)-에톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린일카르-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R)- 또는 3(S)-메틸아미노카르보닐아미노-1,2,3,4-테트라히드로퀴놀린일카르-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R) 또는 3(R,S)-페닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R,S)-메톡시카르보닐-4-옥소-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R,S)-알릴아미노카르보닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R,S)-메톡시카르보닐아미노메틸-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 4(S)-히드록시-2(S)-이소프로필-5(S)-메탄술포닐아미노-7,7-디메틸-8-[2(R)- 또는 (S)-메틸아미노카르보닐-3,4-디히드로-2H-1,4-벤조티아진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R,S)-알릴아미노카르보닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R,S)--N-N-디메틸아미노에틸-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[2(R,S)-메톡시이미노메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R,S)-카르바모일-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)7,7-트리메틸-8-[3(R)- 또는 3(S)-에톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-에톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-프로필옥시카르보닐아미드-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-프로필옥시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)(디옥솔란-2-일)-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; (S)-아미노-4(S)-히드록시-2,2,7,7,-테트라메틸-8-[3-(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-(2-옥소-옥사졸리딘-3-일)-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-3(R,S)-메톡시메톡시메틸-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)(디옥솔란-2-일)-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)(알릴옥시메틸-1,2,3,4-테트라히드로퀴놀린]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)(메톡시에톡시메틸-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-(2-옥소피롤리딘-1-일)-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-6-[1-[2(R)- 또는 2(S)-메틸아미노카르보닐-3,4-디히드로-2H-1,벤조티아진-4-일카르보닐메틸]시클로프로필--2(R)-메틸-헥산산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-6-[1-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐메틸]시클로프로필--2(R)-메틸-헥산산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-6-[1-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐메틸]시클로프로필--2(R)-메틸-헥산산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3,(R,S)-메톡시에톡시-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐메틸]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3,(R,S)-프로필옥시-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐메틸]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(S),이소프로필-7,7-디메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐메틸]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-메톡시메틸옥시-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-시클로프로필카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)- 또는 3(S)-알릴옥시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)- 또는 3(S)-알릴옥시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 4(S)-아미노-3(S)-히드록시--1-(R),6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)아미드-7[N-페닐,N-페네틸]아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-메탈아미노카르보닐옥시-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[2(R,S)- 또는 2(S)-메톡시메틸옥시메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[2(R,S)- 또는 2(S)-메톡시메틸옥시메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-(메탈아미노카르보닐)인돌린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-포르밀아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-에틸카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-펜틸-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R,S)-메톡시에틸-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아세틀아미도-4(S)-히드록시-[2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-2(R)-에틸-4(S)-2(R)-에틸-4(S)-히드록시-7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-(2-메틸)프로필-7,7-디메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-(2-메틸)프로필-7,7-디메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-메틸)아미드; 5(S)-아미노-2(R)-벤질-4-(S)-히드록시-7,7-디메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-메틸)아미드; 5(S)-아미노-4(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[2(R)- 또는 2(S)-메톡시카르보닐아미노-3,4-디히드로-2H-1,4-벤족사진-4일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-메톡시프로필-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-메톡시카르보닐아미노-2,3,4,5-테르라히드로-1H-벤즈[6,7-b-아제핀-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-메톡시카르보닐-1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-프로필아미노-4(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[2(R)- 또는 2(S)-메톡시메톡시메틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-프로필아미노-4(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-히드록시-2(R),7,7-트리메틸-8-[2(R,S)-메톡시에틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-2(S)-이소프로필-7,7-디메틸-8-[2(R)- 또는 2(S)-메톡시에틸-3,4-디히드로-2H-1,4-벤족사진-4-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-프로필아미노-4(S)-히드록시-2(R)-7,7-트리메틸-8-[3부틸-2,3-디히드로-4(H)-퀴나졸리논1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R)-7,7-트리메틸-8-[3(R,S)-(2-카르바모일)에틸-1.,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-프로필아미노-4(S)-히드록시-2(S)-이소프로필-7,7-디메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트리히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-2(R)-부트-2-에닐-4(S)-히드록시-7,7-디메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R,S)-메톡시카르보닐-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드-7-(N-나프트-1-일)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-(1,2,3,4-테르라히드로퀴놀린-1-일카르보닐]-옥탄산 (N-부틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-(2,3-디히드로인돌-1-일카르보닐]-옥탄산 (N-부틸)아미드; 4(S)-아미노-3(S)-히드록시-1(R),6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)아미드-7-(N-페닐)아미드; 4(S)-아미노-3(S)-히드록시-1(R),6,6-트리메틸-헵탄디카르복실산-1-(N-부틸)아미드-7-(N-부틸)아미드-7-[N-[2-메톡시카르보닐아미노메틸)페닐]]아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산-N-(2-모르폴린-4-일-에틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산-N-(2-(1-아세틸)-피페리딘-4-일-에틸)아미드; 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산-N-(2-모르폴린-4-일-옥소-에틸)아미드; 또는 5(S)-아미노-4(S)-히드록시-2(R),7,7-트리메틸-8-[3(R)- 또는 3(S)-메톡시카르보닐아미노-1,2,3,4-테트라히드로퀴놀린-1-일카르보닐]옥탄산-N-(2-카르바모일-2-메틸-프로필)아미드, 또는 각 경우에 그의 염.
  7. 통상의 제약 부형제 이외에 제약상 활성 성분으로서 유리 형태 또는 제약상 허용되는 염 형태의 제1항 내지 제8항 중 어느 한 항에 따른 화합물을 포함하는 제제.
  8. a)하기 일반식(Ⅱ)의 화합물 또는 그 염을 하기 일반식(Ⅲ)의 화합물과 축합 반응시켜 아민 또는 아미드 결합을형성하고, 이 때 반응에 관여하는 기를 제외한 반응 성분들 중에 존재하는 유리 관응기들을 보호된 형태로 존재하며, 이어서 존재하는 보호기를 제거하거나
    (상기 식 중, Y는 유리 히드록실 또는 방응성 관능기로 개질된 히드록실이고, X, R1, R2, R3, R4, R5, R6, R7, 및 R8은 하기 정의된 바와 같음), 또는 b)하기 일반식(Ⅳ)의 화합물 또는 반응성 아미노기를 갖는 그의 반응성 유도체와 축합 반응시켜 아미드결합을 형성하고, 이 때, 반응에 관여하는 기를 제외한 반응 성분들 중에 존재하는 유리 관능기들은 보호된 형태로 존재하며, 이어서 존재하는 보호기를 제거하거나
    (상기 식 중, R1, X, R2, R3, R4, R5, R6, R7, 및 R8은 하기 정의된 바와 같음), 또는 c)R5가 히드록실이고 다른 치환체느 ㄴ하기 정의한 바와 같은 하기 일반식(Ⅰ)의 화합물을 제조하기 위해서는, 반응에 관여하는 케토기를 제외하 ㄴ유리 관응기들이 보호된 형태로 존재하는 하기 일반식(Ⅵ)의 화합물 또는 그의 염에서 케토기를 히드록시메틸렌으로 환원시키고, 존재하는 보호기르 ㄹ제거하너가
    (상기 식 중, R1, X, R2, R3, R4, R5, R6, R7, 및 R8은 하기 정의된 바와 같음), 또는 d) R6 이 알킬, 아랄킬 또는 헤테로아랄킬, 특히 메틸이고, R7이 수소이며, 다른 치환체는 하기 정의한 바와 같은 하기 일반식(Ⅰ)의 화합물을 제조하기 위해서는 , 유리 관능기들이 보호된 형태로 존재하는 하기 일반식(Ⅶ)의 화합물 또는 바람직한 경우 그의 염에서 R6기를 목적하는 R6기로 환원시키거나
    (상기 식 중, R6'는 알킬리덴, 아릴알킬리덴 또는 헤테로아랄킬리덴, 특히 메틸렌이고, R1, X, R2, R3, R4, R5, R6, R7, 및 R8은 하기 정의된 바와 같음), 또는 e) R4가 수소이고, 다른 치환체는 하기 정의한 바와 같은 일반식(Ⅰ)의 화합물을 제조하기 위해서는, 유리 관능기들이 보호된 형태로 존재하기 하기 일반식(Ⅷ)의 화합믈 또는 적절한 경우 그의 염에서 아지도기를 아미노기로 환원시키고, 존재하는 보호기를 제거하고,
    (상기 식 중,R1, X, R2, R3, R4, R5, R6, R7, 및 R8은 하기 정의된 바와 같음) 각 경우에 필요에 따라, 상기 a) 내지 e) 의 방법들 중 어느 하나에 의해 얻을 수 있는 1개 이상의 염 형성기를 갖는 일반식(Ⅰ)의 화합물을 그 염으로 전환시키거나, 또는 얻을 수 있는 염을 유리 화합물 또는 다른 염으로 전환시키고/전환시키거나 적절한 경우 얻어질 수 있는 이성질체들의 혼합물을 분리시키고/분리시키거나 일반식(Ⅰ)의 화합물을 일반식(Ⅰ)의 다른 화합물로 전환시키는 것을 포함하는, 하기 일반식(Ⅰ)의 화합물 및 그의 염의 제조 방법.
    ( 상기 식 중, R1은 아릴아미노, N-아릴-N-(저급 알콕시-저급 알킬)-아미노, N-아릴-N-알릴-저급알킬-아미노 또는 고리 질소 원자를 통해 결합되어 있는 헤테로사이클이고, X는 카르보닐 또는 메틸렌기이고, R2및 R3는 서로 독립적으로 수소 또는 저급 알킬이거나 또는 이들이 부착되어 있는 탄소 원자와 함께 시클로알킬리덴기를 형성하고, R4는 수소, 저급 알킬, 저급 알카노일 또는 저급 알콕시카르보닐이고, R5는 히드록실, 저급 알카노일옥시 또는 저급 알콕시카르보닐옥시이고, R6은 수소, 저급 알킬, 저급 알케닐, 저급 알키닐, 시클로알키르, 시클로알킬-저급 알킬, 아릴-저급 알킬 또는 헤테로아릴 고리에 5-7개의 고리 원자를 갖는 헤테로아릴-저급 알킬이고, R7은 수소 또는 저급 알킬이거나 또는 R6및 R7은 이들이 부착되어 있는 탄소 원자와 함께 시클로알킬리덴기를 형성하고, R8은 지방족,지한족-지방족 또는 헤테로아릴지방족기이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019950029994A 1994-09-15 1995-09-14 2,9- 디아미노- 및 2- 아미노-8- 카르바모일-4- 히드록시- 알칸산 아미드 유도체 KR960010612A (ko)

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