KR950017940A - β₃작용약으로서 유용한 카테콜아민 대용약 - Google Patents

β₃작용약으로서 유용한 카테콜아민 대용약 Download PDF

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KR950017940A
KR950017940A KR1019940035583A KR19940035583A KR950017940A KR 950017940 A KR950017940 A KR 950017940A KR 1019940035583 A KR1019940035583 A KR 1019940035583A KR 19940035583 A KR19940035583 A KR 19940035583A KR 950017940 A KR950017940 A KR 950017940A
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amino
hydroxy
ethyl
methanesulfonamide
phenyl
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엔. 와쉬번 윌리엄
지로트라 라빈다 엔
엠. 쉐 필립
비. 미킬리네니 아마렌드라
엠. 포스 캐쓰린
마써 아빈드
개베이 애쉬비니쿠마르
에스. 비사찌 그레고리
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니콜라스 피. 말라테스테닉
브리스톨-마이어즈 스퀴브 캄파니
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Abstract

본 발명은 하기 일반식(Ⅰ)의 화합물 또는 제약학적 허용가능한 그의 염에 관한 것이다.
상기 식 및 본 명세서에서, A는 결합, -(CH2)n- 또는 -CH(B)-(여기서, n은 1 내지 3의 정수이고, B는 -CN, -CON(R9)R9또는 -CO2R7임)이고, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 히드록시, 알콕시, -CH2OH, 시아노, -C(O)OR7, -CO2H, -CONH2, 테트리졸, -CH2NH2또는 할로겐이고, R3은 수소, 알킬, 헤테로환 또는이고, R4는 수소, 알킬 또는 B이고, R5, R5, R8, R8'및 R8＂는 독립적으로 수소, 알콕시, 저급 알킬, 할로겐 -OH, -CN, -(CH2)nNR6COR7, -CON(R6)R6, -CON(R6)OR6, CO2R6, -SR7, -SOR7, -SO2R7, -N(R6)SO2R 1, -N(R6)6, -NR6COR7, -OCH2CO(NR6)R6, -OCH2CO2R7또는 아릴이거나, 또는 R5와 R5'또는 R8와 R8'는 이들이 결합되어 있는 탄소원자와 함께 아릴 또는 헤테로환을 형성할 수 있고, R6와 R6'는 독립적으로 수소 또는 저급 알킬이고, R7은 저급 알킬이고, R9는 독립적으로 수소, 알킬, 시클로알킬, 아릴알킬, 아릴 또는 헤테로아릴 이거나, 또는 R9와 R9'는 이들이 결합되어 있는 질소 원자와 함께 헤테로환을 형성할 수 있고, 단, A가 결합 또는 -(CH2)n이고 R3이 수소 또는 비치환 알킬일 때 R4는 B 또한 치환 알킬이다. 이들 화합물은 베타 3아드레날린 작동성 수용체 작동약이고, 따라서, 예를 들면 당뇨병, 비만증 및 위장 질환의 치료에 유용하다.

Description

β3작용약으로서 유용한 카테콜아민 대용약
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (22)

  1. 하기 일반식(Ⅰ)의 화합물 및 제약학적 허용가능한 그의 염.
    상기 식 중, A는 결합, -(CH2)n- 또는 -CH(B)-(여기서, n은 1 내지 3의 정수이고, B는 -CN, -CON(R9)R9또는 -CO2R7임)이고, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 히드록시, 알콕시, -CH2OH, 시아노, -C(O)OR7, -CO2H, -CONH2, 테트라졸, -CH2NH2또는 할로겐이고, R3은 수소, 알킬, 헤테로환 또는이고, R4는 수소, 알킬 또는 B이고, R5, R5, R8, R8'및 R8＂는 독립적으로 수소, 알콕시, 저급 알킬, 할로겐 -OH, -CN, -(CH2)nNR6COR7, -CON(R6)R6, -CON(R6)OR6, CO2R6, -SR7, -SOR7, -SO2R7, -N(R6)SO2R1, -N(R6)6', -NR6COR7, -OCH2CONR6R6', -OCH2CO2R7또는 아릴이거나, 또는 R5와 R5'또는 R8와 R8'는 이들이 결합되어 있는 탄소원자와 함께 아릴 또는 헤테로환을 형성할 수 있고, R6와 R6'는 독립적으로 수소 또는 저급 알킬이고, R7은 저급 알킬이고, R9킨 R9'는 독립적으로 수소, 알킬, 시클로알킬, 아릴알킬, 아릴 또는 헤테로아릴이거나, 또는 R9와 R9'는 이들이 결합되어 있는 질소 원자와 함께 헤테로환을 형성할 수 있고, 단, A가 결합 또는 -(CH2)n이고 R3이 수소 또는 비치환 알킬일때 R4는 B 또한 치환 알킬이다.
  2. 제1항에 있어서, A가 결합, -(CH2)n- (여기서, n은 1 임) 또는 -CH(B)-이고, R3이 수소, 알킬 또는이고, R5및 R5'가 독립적으로 수소, 할로겐, 저급 알킬, 알콕시, CON(R6)R6'또는 CON(R6)OR6'이고, 벤질성 히드록실의 입체 중심이 (R) 배위를 갖는 화합물.
  3. 제1항에 있어서, A가 결합이고, R1이 저급 알킬이고, R3이이고, R4가 수소 또는 알킬이고, R5및 R8이 모두 -CN, CON(R6)R6', CON(R6)OR6', 히드록시, 알콕시 또는 -CH2Y(여기서, Y는 -CN, 알콕시, CON(R6)R6', CO2R7또는 -N(R6)SO2R1이거나, 또는 R5, R5',R8및 R8'이 이들이 결합되어 있는 탄소원자와 함께 아릴 또는 헤테로환을 형성하고, 벤질성 히드록실의 입체 중심이 (R) 배위를 갖는 화합물.
  4. 제1항에 있어서, A가 결합이고, R1이 저급 알킬이고, R3이 수소 또는 알킬이고, R4가 -CON(R9)R9'이고, R5가 -CN, -CON(R6)OR6', -CON(R6)R6', 히드록시 또는 알콕시이고, R3및 R4치환체를 함유하는 입체 중심의 배위가 (S)이고, 벤질성 히드록실의 입체 중심이 (R) 배위를 갖는 화합물.
  5. 제1항에 있어서, A가 -CH2-이고, R1이 저급 알킬이고, R3이이고, R4가 수소, 알킬, -CN 또는 -CON(R9)R9'이고, R5가 수소, 할로겐 또는 -CF3이고, R8이 -CN, -CON(R6)R6', -CON(R6)OR6', 히드록시, 저급 아킬 또는 알콕시이거나, 또는 R8및 R8'이 이들이 결합되어 있는 탄소 원자와 함께 아릴 또는 헤테로환을 형성하고, R4가 수소일 경우 R3및 R4치환체를 함유하는 입체 중심의 배위 (R)이고, 벤질성 히드록실의 입체 중심이 (R) 배위를 갖는 화합물.
  6. 제1항에 있어서, A가 -CH(B)-(여기서, B는 -CN, -CON(R9)R9'임)이고, R1이 저급 알킬이고, R3및 R4가 수소 또는 알킬이고, R5가 -CN, -CON(R6)R6', -CON(R6)OR6', 히드록시 또는 알콕시이고, 벤질성히드록실의 입체 중심이 (R) 배위를 갖는 화합물.
  7. 제1항에 있어서, N-[5-[2-[1-(3, 4-디메톡시페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[1, 2-디페닐에틸)아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[1-히드록시-2-[[1-(4-메톡시페닐)-2-페닐에틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(3-메톡시페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(2, 4-디메톡시페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(3, 4-디클로로페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(4-메틸술포닐페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(3, 4-디메틸페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(3, 4-디에틸페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-페닐-2-(4-메톡시페닐)-에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[1-(4-메톡시페닐)-2-(4-메톡시페닐)-에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[비스(4-메톡시페닐)-에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[1-히드록시-2-[[(4-메톡시페닐)페닐메틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, α-[[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)-아미노]페닐]에틸]아미노]메틸]벤젠아세트산, 에탈 에스테르, α-[[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]메틸]-3, 4-디메톡시벤젠아세트산, 메틸 에스테르, α-[[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]메틸]-N, N-디메틸벤젠아세트아미드, (R), (R)-N-[5-1-[히드록시-2-[[1-(3, 4-디메톡시페닐)-2-페닐에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R)-N-[5-2-[[비스(4-메톡시페닐)메틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, (R)-N-[5[2-[[비스(4-플루오로페닐)메틸]아미노]-1-히드록시-에틸]-2-히드록시페닐]메탄술폰아미드, (R), (S)-N-[5-[1-(히드록시-2-[[1-(3, 4-디메톡시페닐)-2-페닐에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (트레오)-β-[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-α-페닐-벤젠프로판산, 메틸 에스테르, 부분 입체 이성질체, A, (트레오)-β-[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-α-페닐-벤젠프로판산, 메틸 에스테르, 부분 입체 이성질체, B, (에리트로)-β-[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-α-페닐-벤젠프로판산, 메틸 에스테르, 부분 입체 이성질체, A, (에리트로)-β-[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-α-페닐-벤젠프로판산, 메틸 에스테르, 부분 입체 이성질체, B, N-[3-[2-[[1-(3, 4-디메톡시페닐)-2-페닐에틸]아미노]-1-히드록시에틸]페닐]메탄술폰아미드, (R)-N-[3-[2-[[비스(4-메톡시페닐)-메틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, (R, R)-N-[3-[2-[[1-(3, 4-디메톡시페닐)-2-페닐에틸]아미노]-1-히드록시에틸]페닐]메탄술폰아미드, ε-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]벤젠헵탄산, 메틸 에스테르, ε-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]벤젠헵탄산, N-[5-[1-히드록시-2-[[6-히드록시-1-(페닐메틸)헥실]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, ε-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-N, N-디메틸벤젠헵탄아미드, ε-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-N디메틸벤젠헵탄아미드, ε-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-3, 4-디메톡시벤젠헵탄산, 메틸 에스테르, N-[2-[1-히드록시-5-[(R)-1-히드록시-2-[[2-페닐-1-(4-피리딜)에틸]아미노]에틸]페닐]메탄술폰아미드, α-[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시벤젠아세트아미드, 이설질체 A, α-[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시벤젠아세트아미드, 이설질체 B, (R)-α-[[2-히드록시-2-[4-히드록시
    -3-[(메틸술포닐)아미노]페닐]에틸]아미노]-α-(4-메톡시페닐)-4-메톡시벤젠-아세트아미드, 4-[[[5-[2-[[2-(3, 4-디메톡시페닐]에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]아미노]슬포닐]벤조산, 메틸 에스테르, N-[5-[2-[[2-(3, 4-디메톡시페닐)에틸]아미노]-1-히드록시에틸-2-히드록시페닐]벤젠메탄술폰아미드, N-[5-[2-[[2-(3, 4-디메톡시페닐)에틸]아미노]-1-히드록시에틸-2-히드록시페닐]벤젠메탄술폰아미드, N-[5-[2-[[비스(4-메톡시메틸페닐)메틸]아미노]-1-히드록시페닐]-2-히드록시페닐]메틸술폰아미드, (R), (R)-N-[5-[2-[[1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, (R), (S)-N-[5-[2-[[1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[2-[[비스(4-메톡시페닐)에틸]아미노]-1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, N-[2-히드록시-5-[(R)-1-히드록시-2-[[2-페닐-1-(3-티에닐)에틸]아미노]에틸]페닐]메탄술폰아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(4-메톡시페닐)-2-(4-플루오로페닐)-에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-메톡시페닐)-2-(4-플루오로페닐)-에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(4-히드록시페닐)-2-(4-플루오로페닐)-에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-히드록시페닐)-2-(4-플루오로페닐)-에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-페닐메톡시페닐)-2-(4-플루오로페닐)-에틸]아미노]에틸]-2(히드록시)페닐]메탄술폰아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(4-메톡시페닐)-2-(3-트리플루오로메틸페닐)에틸]아미노]에틸]-2(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-메톡시페닐)-2-(3-트리플루오로메틸페닐)에틸]아미노]에틸]-2(히드록시)페닐]메탄술폰아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(4-디플루오로메톡시페닐)-2-(4-플루오로페닐)에틸]아미노]에틸]-2(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-디플루오로메톡시페닐)-2-(4-플루오로페닐)에틸]아미노]에틸]-2(히드록시)페닐]메탄술폰아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(4-디플루오로메톡시페닐)-2-(페닐)에틸]아미노]에틸]-2(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-디플루오로메톡시페닐)-2-(페닐)에틸]아미노]에틸]-2(히드록시)페닐]메탄술폰아미드, (R)-N-[5-[2-[[비스-(4-디플루오로메톡시페닐)에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, (R), (R)-N-[3-[2-[[1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, (R), (R)-N-[3-[2-[[1-(4-디플루오로메톡시페닐)-2-(4-플루오로페닐)에틸]아미노]-1-히드록시에틸]페닐]메탄술폰아미드, (R), (S)-N-[3-[2-[[1-(4-디플루오로메톡시페닐)-2-(4-플루오로페닐)에틸]아미노]-1-히드록시에틸]페닐]메탄술폰아미드, (R), (R)-N-[5-[2-[[1-(4-디플루오로메톡시페닐)-2-(4-플루오로페닐)에틸]아미노]-1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, (R), (S)-N-[5-[2-[[1-(4-디플루오로메톡시페닐)-2-(4-플루오로페닐)에틸]아미노]-1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, N-[5-[2-[[1, 2-디페닐-1-(트리플루오로메틸]에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, α-[[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]메틸-3, 4-디메톡시-N, N-디메틸-벤젠아세트아미드, 부분 입체 이설질체 A, α-[[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]메틸-3, 4-디메톡시-N, N-디메틸-벤젠아세트아미드, 부분 입체 이설질체 B, N-[5-2-[[(R)1-(3, 4-디메톡시페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, N-[5-2-[[(R)1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시에틸]-2-클로로페닐]메탄술폰아미드, N-[5-2-[[(R)1-(1, 3-벤조디옥솔-5-일)
    -2-페닐에틸]아미노]-1-히드록시에틸]-2-메톡시페닐]메탄술폰아미드, (R), (R)-N-[5-2-[[1-(1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, (R), (R)-N-[5-2-[[1-(1, 3-디메톡시페닐)-2-페닐에틸]아미노]-1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, (R)-N-[5-2-[[비스-(4-디플루오로메톡시페닐]메틸]아미노]-1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, α-[[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]메틸-3, 4-디메톡시-N-(페닐)벤젠아세트아미드, α-[[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]메틸-3, 4-디메톡시-N-(페닐메틸)
    -벤젠아세트아미드, α-[[[(R)-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]메틸-3, 4-디메톡시-N-(페닐에틸)-벤젠아세트아미드, (R), (R)-N-[5-[1-(히드록시)-2-[[1-(3, 4-디메틸페닐-2-페닐에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R)-N-[5-[1-(히드록시-2-[[1-(4-히드록시페닐)-2-(2-티에닐)에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R)-N-[5-[2-[[비스[4-(2-메톡시-2-옥소에톡시)페닐]메틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탄술폰아미드, (R), (R)-N-[5-[2-[[1-(1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]
    -1-히드록시에틸]-2-플루오로페닐]메탄술폰아미드, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤조산, 메틸 에스테르, (R), (S)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤조산, 메틸 에스테르, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤조산, (R), (S)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤조산, (R), (S)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤조산, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]-N-메틸벤즈아미드, (R), (R)-N-[5-[1-(히드록시-2-[[1-(2-나프탈레닐)-2-(페닐)에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-(히드록시-2-[[1-(2-나프탈레닐)
    -2-(페닐)에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R), (S)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤젠아세트산, 메틸 에스테르, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤젠아세트산, 메틸 에스테르, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤젠아세트산, (R, R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]-N-페닐메틸벤즈아미드, (R, R)-N-(2-히드록시에틸)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]-벤즈아미드, (R, R)-N-[3-[2-[[1-(1, 3-벤조디옥솔-5-일)-2-(4-플루오로페닐)에틸]아미노]-1-히드록시에틸]-2-히드록시페닐]메탈술폰아미드, (R), (S)-N-(1, 3-디메틸에틸)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-메톡시벤젠아세트아미드, (R), (S)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-N-페닐벤벤아세트아미드, (R), (S)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-N-메틸-N-페닐벤젠아세트아미드, (R), (S)-N-(1, 3-벤조디옥솔-5-일)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시벤젠아세트아미드, (R), (S)-N-(4-클로로페닐)-α-[[-2-히드록시-2-[4-히드록록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-α-메틸-N-페닐벤아세트아미드, (R), (R)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-N-페닐벤젠아세트아미드, (R), (S)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-N-페닐벤젠아세트아미드, (R), (R)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-N-(페닐메틸)벤젠아세트아미드, (R), (S)-N-(시클로헥실)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시벤젠아세트아미드, (R, R)-N-히드록시-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤즈아미드, (R), (S)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-N-페닐벤젠프로판아미드, (R), (R)-α-[[-2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-N-페닐벤젠프로판아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-메톡시페닐)-2-옥소-2-(1-피페리디닐)에틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]-N-메틸벤젠아세트아미드, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]-N, N-디메틸벤젠아세트아미드, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]-벤젠아세트아미드, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]벤즈아미드, (R), (R)-4-[1-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-2-페닐에틸]-N, N-디메틸벤젠아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(1-나프탈레닐-2-페닐에틸]아미노]에틸]-2-(히드록시)페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(1-나프탈레닐-2-페닐에틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(4-메톡시-1-나프탈레닐)-2-페닐에틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(4-메톡시-1-나프탈레닐)-2-페닐에틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, N-[5-[(R)-1-(히드록시-2-[[1-(벤조[b]티오펜-5-일)-2-페닐에틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, (R), (R)-N-[5-[1-히드록시-2-[[1-(4-메톡시-3-피리디닐)-2-페닐에틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, (R), -N-[5-[1-히드록시-2-[[1-(2, 4-디메톡시-3-피리디닐)-2-페닐에틸틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, (R), (S)-N-[5-[1-히드록시-2-[[1-(2, 4디메톡시-3-피리디닐)-2-페닐에틸틸]아미노]에틸]-2-히드록시페닐]메탄술폰아미드, (R), (S)-N-(1, 3-벤조디옥솔-5-일)-α-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-4-메톡시-α-메틸벤젠아세트아미드, (R), (R), (R)-N-[5-[2-[[1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시프로필]-2-히드록시페닐]메탄술폰아미드, (R), (S), (R)-N-[5-[2-[[1-(1, 3-벤조디옥솔-5-일)-2-페닐에틸]아미노]-1-히드록시프로필]-2-히드록시페닐]메탄술폰아미드, (R), (S)-N-(4-클로로페닐)-α-[[2-히드록시-2-[4-히드록시-3-[(메틸술포닐)아미노]페닐]에틸]아미노]-α-메틸-4-메톡시벤젠아세트아미드, 또는 이들의 제약학상 허용되는 염인 화합물.
  8. 제1항 기재의 화합물 및 제약학상 허용되는 담체로 이루어진 제약 조성물.
  9. 제8항 기재의 조성물 치료 유효량을 당뇨병의 치료를 필요로 하는 포유동물종에 투여하는 것으로 이루어진 당뇨병의 치료 방법.
  10. 제8항 기재의 조성물 치료 유효량을 비만증의 치료를 필요로 하는 포유동물종에 투여하는 것으로 이루어진 비만증의 치료 방법.
  11. 제8항 기재의 조성물 치료 유효량을 장 운동항진증의 치료를 필요로 하는 포유동물 종에 투여하는 것으로 이루어진 장 운동항진중의 치료 방법.
  12. 제1항 기재의 화합물과 베타1또는 베타2아드레날린작동성 차단제 또는 흥분제 및 제약학상 허용되는 담체로 이루어진 제약 조성물.
  13. 제12항 기재의 조성물 치료 유효량을 당뇨병의 치료를 필요로 하는 포유동물 종에 투여하는 것으로 이루어진 당뇨병의 치료방법.
  14. 제12항 기재의 조성물 치료 유효량을 비만증의 치료를 필요로 하는 포유동물 종에 투여하는 것으로 이루어진 비만증의 치료방법.
  15. 제12항 기재의 조성물 치료 유효량을 위장 질환의 치료를 필요로 하는 포유동물 종에 투여하는 것으로 이루어진 위장 질환의 치료방법.
  16. 하기 일반식(Ⅲ)의 화합물.
    상기 식 중, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 할로겐, 시아노, CO2R7, CONH2, CH2OPro', OR7또는 O-Pro'(여기서, Pro'는 적합한 보호기, 예를 들면 벤질 또는 t-부틸디메틸실릴임)이고, R6은 수소 또는 저급 알킬이고, Pro는 적합한 보호기, 예를 들면 트리에틸실릴이고, L은 이탈기, 예를 들면 요오다이드, 트리플레이트 또는 브로마이드이다.
  17. 하기 일반식(ⅩⅩⅡ)의 화합물.
    상기 식 중, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 할로겐, 시아노, CO2R7, CONH2, CH2OPro', OR7또는 O-Pro'(여기서, Pro'는 적합한 보호기, 예를 들면 벤질 또는 t-부틸디메틸실릴임)이다.
  18. 하기 일반식(ⅩⅩⅩⅧ)의 화합물.
    상기 식 중, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 할로겐, 시아노, CO2R7, CONH2, CH2OPro', OR7또는 O-Pro'(여기서, Pro'는 적합한 보호기, 예를 들면 벤질 또는 t-부틸디메틸실릴임)이고, R6은 수소 또는 저급 알킬이다.
  19. 하기 일반식(Ⅲa)의 화합물.
    상기 식 중, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 할로겐, 시아노, CO2R7, CONH2, CH2OPro', OR7또는 O-Pro'(여기서, Pro'는 적합한 보호기, 예를 들면 벤질 또는 t-부틸디메틸실릴임)이고, R6은 수소 또는 저급 알킬이다.
  20. 하기 일반식(Ⅰ)의 화합물 또는 제약학적 허용가능한 그의 염.
    상기 식 중, A는 결합, -(CH2)n- 또는 -CH(B)-(여기서, n은 1 내지 3의 정수이고, B는 -CN, -CON(R6)R6또는 -CO2R7임)이고, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 히드록시, 알콕시 또는 할로겐이고, R3는 수소, 치환 알킬, 헤테로환 또는이고, R4는 수소, 알킬 또는 B이고, R5, R5, R8, R8'는 독립적으로 수소, 알콕시, 저급 알킬, 할로겐 -OH, -CN, -(CH2)nNR6COR7, -CON(R6)R6, CO2R7, -SR7, -SOR7, -SO2R7, -N(R6)SO2R1, -N(R6)6, -NR6COR7, -OCH2CO(NR6)R6또는 -OCH2CO2R7이거나, 또는 R5와 R5'또는 R8과 R8'는 함께 헤테로환을 형성할 수 있고, R6및 R6'는 독립적으로 수소 또는 저급 알킬이고, R7은 저급 알킬이고, 단, A가 결합 또는 -(CH2)n이고 R3이 수소일 때, R4는 수소 또는 비치환 알킬 이외의 것이다.
  21. 하기 일반식(Ⅲ)의 화합물.
    상기 식 중, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 불소 또는 O-Pro'(여기서, Pro'는 적합한 보호기, 예를 들면 벤질 또는 t-부틸디메틸실릴임)이고, R6은 수소 또는 저급 알킬이고, Pro는 적합한 보호기, 예를 들면 트리에틸실릴이고, L은 이탈기, 예를 들면 요오다이드, 트리플레이트 또는 브로마이드이다.
  22. 하기 일반식(ⅩⅩⅡ)의 화합물.
    상기 식 중, R1은 저급 알킬, 아릴 또는 아릴알킬이고, R2는 수소, 불소 또는 O-Pro'(여기서, Pro'는 적합한 보호기, 예를 들면 벤질 또는 t-부틸디메틸실릴임)이다.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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US5776983A (en) 1998-07-07
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