KR880011126A - 벤조디아제핀 동족체 - Google Patents

벤조디아제핀 동족체 Download PDF

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KR880011126A
KR880011126A KR1019880002698A KR880002698A KR880011126A KR 880011126 A KR880011126 A KR 880011126A KR 1019880002698 A KR1019880002698 A KR 1019880002698A KR 880002698 A KR880002698 A KR 880002698A KR 880011126 A KR880011126 A KR 880011126A
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dihydro
benzodiazepin
phenyl
methyl
oxo
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KR960012197B1 (ko
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이.에반스 벤
엠.프라이딩거 로저
보크 마크 지
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제임스 에프.노턴
머크 앤드 캄파니 인코포레이티드
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Abstract

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Description

벤조디아제핀 동족체
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (18)

  1. 일반식 (Ⅱ)의 화합물 및 그의 약제학적으로 허용되는 염.
    상기식에서, R1은 H, C1-C6선형 또는 측쇄 알킬, 저급 알케닐, 저급알키닐, -X12COOR6, -X11- 시클로저급알킬, -X12NR4R5, -X12CONR4R5, -X12CN, 또는 -X11CX1 10이고 ; R2는 H, 저급알킬, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, 저급알킬, 저급알콕시, 저급알킬티오, 카복실, 카복시저급알킬, 니트로, -CF3, 또는 하이드록시일 수 있다), 2-, 3-, 4-피리딜,
    R7인 경우,이며, 단, R3가인 경우, R10은 H 또는 -CH3가 아니고 ; R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일- 또는 이-치환된 포화 또는 불포화 4 내지 7원 헤테로시클릭환 또는 벤조융합된 4 내지 7원 헤테로사이클릭환, 또는 0 및 NCH3로 부터 선택된 제2의 헤테로 원자를 추가로 함유하는 상기 헤테로사이클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환체(들)은 독립적으로 C1-C4알킬로 부터 선택되고 ; R6는 H, 저급알킬, 시클로저급알킬, 치환 또는 비치환된 페닐, 또는 치환 또는 비치환된 페닐저급알킬(여기서, 페닐 또는 페닐저급알킬 치환체는 1 또는 2개의 할로, 저급알킬, 저급알콕시, 니트로, 또는 CF3일 수 있다)이며 ; R7은 α -또는 β-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, -NO2, -OH, -X11NR4R5, 저급알킬 CF3, CN, SCF3, C=CH, CH2SCF3,CCHF2, SH, sph, PO3H, 저급알콕시, 저급알킬티오, 또는 COOH이다), 2-, 3-, 4-피리딜,
    R8은 H, 저급알킬, 시클로저급알킬, -X12CONH2, -X12COOR6, -X12-시클로저급알킬, -X12NR4R5, 또는
    이며 ; R9 및 R10은 독립적으로 H, -OH, 또는 -CH3이고 ; R11 및 R12는 독립적으로 저급알킬 또는 시클로저급알킬이며 ; R13은 H, 저급알킬, 아실, C, 또는 시클로저급알킬 이고 ; R14는 저급알킬 페닐저급알킬 이며 ; R15는 H, 저급알킬,또는 -NH2이고 ; R16은 α- 또는 β-나프틸 또는 2-인돌릴이며 ; R18은 이고, 그의 인접한 임의의 이중결합…이 불포화된 경우에 0 이고, 그의 인접한 임의의 이중결합…이 포화된 경우에는 1이며, 단, R13이 0이고, P가 1이며,…이 불포화된 경우는 제외하며, q는 0 내지 4이고, r은 1 또는 2이며 ; X1은 H, -NO2, CF3, CN, OH, 저급알킬, 할로, 저급알킬티오, 저급알콕시, -X11COOR6, -X11NR4R5이고 ; X2및 X3는 독립적으로 H, -OH, -NO2, -COOR6, NO2또는 할로이며 ; X6은 0 또는 HH이고 ; X7은 O, S, HH, 또는 NR15이며, 단 R1이 H가 아니 경우 X7이 NR15일 수 있으며 ; X8은 H, 저급알킬이고 ; X9및 Xa 9는 독립적으로 NR18또는 0이며 ; X10은 F, Cl, 또는 Br이고 ; X11은 부재하거나 C1-4선형 또는 측쇄 알킬리덴이며 ; X12는 C1-4선형 또는 측쇄 알킬리덴이고 ;…는 포화 또는 불포화된 결합이며 ; 단, Xr1이 7 위치에서 Cl이고, R1은 H이며, R2는 비치환된 페닐인 경우, R3는 NHCO(CH2)3C6H5또는 NHCOC6H5가 아니다.
  2. 제1항에 있어서, R1이 H, C1-C6선형 또는 측쇄 알킬, -X12COOR6, -X11-시클로저급알킬, -X12NR4R5또는 -X12CONR4R5이고 ; R2는 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, 저급알킬, 저급알콕시, 저급알킬티오, 카복실, 카복시저급알킬, 니트로, -CF3, 또는 하이드록시일 수 있다), 2-, 3-, 4-피리딜,또는 -X12COOR6이며 ; R3는 이고 ; R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일- 또는 이-치환된 포화 또는 불포화 4 내지 7원 헤테로사이클릭환 또는 벤조융합된 4 내지 7원 헤테로사이클릭환, 또는 0 및 NCH3로 부터 선택된 제2의 헤테로원자를 추가로 함유하는 상기 헤테로시클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환체(들)은 독립적으로 C1-C4알킬로 부터 선택되고 ; R6는 H, C1-C4직쇄 또는 측쇄 알킬 또는 C3-C6시클로알킬이며 ; R7은 α - 또는 β-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, -NO2, -OH, -X11NR4R5, 저급알킬, CF3, CN, SCF3,SH, sph, 저급알콕시, 저급알킬티오 또는 카복시이다), 2-, 3-, 4-피리딜,
    R8은 H, 저급알킬 또는 시클로저급알킬이며 ; R9및 R10독립적으로 H, -OH, 또는 -CH3이고, R13은 H, 저급알킬, 아실, 0, 또는 시클로저급알킬이고, R18은 H 또는 저급알킬이며 ; P는 그의 인접한 임의의 이중결합…이 불포화된 경우에 0이고, 그의 인접한 임의의 이중결합…이 포화된 경우에는 1이며, 단, R13이 0이고, P가 1이며,…이 불포화된 경우는 제외하면, q는 0 내지 2이고 ; r은 1 또는 2이며, X1은 H, -NO2, CF3, CN, 저급알킬, 할로, 저급알킬티오, 또는 -X11COOR6이고 ; X2및 X3는 독립적으로 H, -NO2, 할로, 저급알킬티오, 저급알킬 또는 저급알콕시이며 ,X4는 S, O, 또는 NR8이고 ; X5는 H, CF3, CN, -COOR6, NO2또는 할로이며 ,X6는 0 또는 HH이고 ; X7은 O, S이며, X9및 Xa 9는 독립적으로 NR18또는 0이고 ; X11은 부재하거나 C1-4선형 알킬리덴이며 ; X12는 C1-4선형 또는 측쇄 알킬리덴이고 ; 는 포화 또는 불포화된 결합인 화합물 및 그의 약제학적으로 허용되는 염.
  3. 제2항에 있어서, R1이 H, C1-C3선형 또는 측쇄 알킬, -X12COOR6, -X12CONH4R5이고 ; R2는 치환 또는 비치환된 페닐(여기에서, 치환체는 1또는 2개의 할로, 저급알킬, 카복실, 니트로 또는 CF3일 수 있다) ; -X12COOR6; 2-, 3-, 4-피리딜이며 ; R3는또는또는이고 ; R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일-또는 이-치환된 포화 또는 불포화 4 내지 7원 헤테로시클릭환 또는 벤조융합된 4 내지 7원 헤테로사이클릭환, 또는 0 및 NCH3로 부터 선택된 제2의 헤테로원자를 추가로 함유하는 상기 헤테로시클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환체(들)은 독립적으로 C1-C4알킬로 부터 선택되며 ; R6는 H, C1-C4직쇄 또는 측쇄 알킬이고 ; R7은 ?? - 또는 ??-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, -NO2, -OH, -NR4R5, 저급알킬, CF3, CN, 또는 저급알콕시일 수 있다), 2-, 3-, 4-피리딜,
    R9및 R10은 H, 또는 -OH이고 ; P는 그의 인접한 임의의 이중결합…이 불포화된 경우에 0이고, 그의 인접한 임의의 이중결합…이 포화된 경우에는 1이며, (R13)p의 p는 0이고 ; r은 1 또는 2이며 ; X1은 H, -NO2, CF3, 저급알킬 또는 할로이고 ; X2및 X3는 독립적으로 H, -NO2, 할로, 저급알킬, 또는 저급알콕시이며 ; X4는 0 또는 NR8이고 ; X7은 0 또는 S이며 ; X12는 선형 또는 측쇄 알킬리덴이고 ;…은 포화 또는 불포화된 결합인 화합물 및 그의 약제학적으로 허용되는 염.
  4. 제3항에 있어서, R1이 H, C,-C2선형 알킬, -X12COOR6, -X12CONR4R5이고, R2는 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, 저급알킬, 니트로 CF3일 수 있다) ; -X12COOR6; 2-, 3-, 4-피리딜이며, R3는또는또는이고, R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일- 또는 이-치환된 포화 또는 불포화 4 내지 7원 헤테로시클릭환 또는 벤조융합된 4 내지 7원 헤테로시클릭환, 또근 0 및 NCH3로 부터 선택된 제2의 헤테로원자를 추가로 함유하는 상기 헤테로시클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환체(들)은 독립적으로 C1-C4알킬로 부터 선택되며 ; R6는 H, C1-C3직쇄 알킬이고 ; R7은 α - 또는 β-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로 -NO2, NH2, 메틸, 에틸, CF3, CN, 또는 저급알콕시일 수 있다), 2-, 3-, 4-피리딜,
    R10은 H, 또는 OH이고 ; P는 (R10)p에서 1이고, (R9)p및 (R13)p에서는 0이며, 4,5 위치의…는 불포화되며 ; 3,4 위치의…는 포화되며 ; r은 1 또는 2이며 ; X1은 H, -NO2, CF3, 저급알킬 또는 할로이며, X4는 H, -NO2, 할로 또는 저급알킬이고 ; X7는 O, NH, NCH3이며, X7는 0 또는 S 이고 ; X12는 C1-2선형 알킬리덴인 화합물 및 그의 약제학적으로 허용되는 염.
  5. 제4항에 있어서, R1이 H, CH3, CH2CH3, CH2COOH, CH2COOEt, CH2CON(Et)2, 또는 CH2CH2COOEt이고 ; R2는 페닐, 2-F-페닐, 4-CH3-페닐, 2-, 3-, 또는 4-피리딜이며 ;
    R10은 H 또는 -OH이며 ; P는(R10)p에서 1이고, (R9)p및 (R13)p에서는 0이며, r은 1이고 ; X1은 H, 7-Cl, 8-CH3, 9-CH3이며 ; X7은 O 또는 S이고 ; 4,5 위치의…는 불포화되고 3,4 위치의…는 포화된 화합물 및 그의 약제학적으로 허용되는 염.
  6. 제1항에 있어서, 3(R)-N-(4-클로로페닐)-N'-(2,3-디하이드로-1-메틸-5-페 닐-2-옥소-lH-1,4-벤조디아제핀-3-일)우레아, 3-벤조일-1,3-디하이드로-3-하이드록시-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 5-(2-플루오로페닐)-1,3-디하이드로-3-하이드록시-3-(4-메톡시-벤조일)-1-메틸-2H-1,4-벤조디아제핀-2-온, N- (2,3-디하이드로-1-메틸-2-옥소-5(3-메틸페닐)-lH-1,4-벤조디아제핀-3-일)-N'-(페닐메틸)우레아, N-(2,3-디하이드로-1-에틸-2-옥소-5-페닐-lH-1,4-벤조디아제 핀-3-일)N'-(3-메톡시페닐)우레아, 3-(S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-3-(3-메톡시페닐)-2-프로페나미드, 3-((((4-클로로페닐)아미노)카보닐)아미노-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제 핀-1-프로파노산 에틸 에스테르, 3(RS)-1,3-디하이드로(2-인돌카보닐아미노)-5-페 닐-2H-1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이드로-3(RS)-(2-인돌카보닐-아미노)-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3(RS)-(2-인돌카보닐아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메틸-3(RS)-[2-(1-메틸인돌)-카보닐아미노]-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메틸-3(RS)-(4-클로로페닐카보닐)-아미노-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3(RS)-(2-인돌-카보닐아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페 닐)-1-메틸-3-(RS)-[2'-(1'-메틸인돌)카보닐아미노]-2H-1,4-벤조디아제핀-2-온, 3(S)-(-)-1,3-디하이드로-3-(2-인돌카보닐아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(2-인돌-카보닐아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-3-(4-클로로벤조일아미노)-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(-) -1,3-디하이드로-3-(4-브로모벤조일아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3-(RS)-(2-인돌카보닐아미노)-2H-1,4 -벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(4-클로로페닐카보닐)아미노-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이드로-5-(2-플루오로페닐:-3(RS)-(2-인돌카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이 드로-3-(RS)-(5-플루오로인돌2-카보닐아미노)-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(1-메틸인돌2-카보닐아미노)-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)3-(RS)- (2-벤조푸란카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메틸-3- (RS)-(4-클로로페닐카보닐)-아미노-5-페닐-2H-1,4-벤조디아제핀-2-온, 3(5)-(+) -3-(3-브로모벤조일아미노)-1,3-디하이드로-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-3-(4-브로모벤조일아미노)-1,3-디하이드로-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(4-요오도-벤조일아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3 (S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(3-요오도-벤조일아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3-(RS)-(2-인돌) -카보닐아미노-2H-1,4-벤조디아제핀-2-티온, 3(S)-(2-인돌카보닐)아미노-1,3-디 하이드로-5-페닐-2H-1,4-벤조디아제핀-2-온, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-3-페닐-3-프로페나미드, 3-((((4-클로로페닐)아미노)카보닐)아미노)-5-(2-플루오로페닐)-2,3-디하이드로-2-옥소-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-4-트리플루오로메틸)-벤자미드, 3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-1H-1,4-벤조디아제 핀-1-아세트산 에틸 에스테르,-5-(2-플루오로페닐)-2,3-디하이드로-2-((IH-인돌-2-일카보닐)아미노)-2-옥소-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, 4-브로모-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-벤자미드, N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조디 아제핀-3-일)-4-(트리플루오로메틸)-벤자미드,(S)-N-(5-(2-플루로오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조디아제핀-5-일)4-(트리플루오메틸)-벤자미 드, 3-((((4-클로로페닐)아미노)카보닐)아미노)-N, N-디 에틸-2,3-디하이드로-2-옥소-5-(페닐-lH-1,4-벤조디아제핀-1-아세타미드, 1-((3-((((4-클로로페닐)아미노)카보닐)아미노)-2, 3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-일)-아세 틸)피롤리딘, 1-((3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-일)-아세틸)-4-메틸피페라진, 3-(((4-클로로페닐) 아세틸)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-페닐우레아, N-(2,3-디 하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(4-메틸페닐)-우레아, N-(2-클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, N-(4-니트로페닐)-N'(2,3-디하이로-1-메틸-2-옥소-5-페 닐-lH-1,4-벤조디아제핀-3-일)-우레아, N-(2,4-디클로로페닐)-N'(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메틸페닐)-우레아,N- (2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-니트로페닐)-우레아, N-(3-클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, (R)-N- (2,3-디하디드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, (S)-N-(2,3-디하이 드로-1-메틸-2-옥소-5-페닐1H-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-N'- (2-니트로페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(2-플구오로페닐)-우레아, N-3(브로모페닐)N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐1H-1,4-벤조디아제핀-3-일)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀3-일)-N'-1-나프탈레닐-우레아,(S) -N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀3-일)-N'-(2-클로로페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디 아제핀3-일)-N'-(3-메틸페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀3-일)-N'-(3-브로모페닐)-우레아,1-{[(3-((((3-메톡시페 닐)아미노)카보닐)아미노]-2,3-디하이드로-2-옥소5-페닐-lH-1,4-벤조디아제핀-1-일]아세핀}피롤리딘, 1-{[3-(((3-메톡시페닐)아미노)카보닐)아미노]-N, N-디에틸 -2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, 3-{[((2-클로로페닐)아미노)카보닐)아미노]-N, N-디에틸-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, 3-N-(2,3-디하이드로-1-메틸-2-옥소-5-페 닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, 3-N-(2,3-디하이드로-1,9 -디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, N- (3-메톡시페닐)-N'-(2,3-디하이드로-1,9-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, 3-N-(2,3-디하이드로1-메틸-2-옥소-5-(P-톨릴)-1H-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, N-(3-메톡시페닐)-N'-(2,3-디하이드-1-메틸-2-옥소-5-(P-톨릴)-lH-1,4-벤조더아제핀-3-일)-우레아, (R)-N-(2,3-디하이 드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-N'-(4-메틸페닐)-우레아, 3-N-(2,3-디하이드로-1,8-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일) -lH-인돌-2-카복사미드, N-(3-메톡시페닐)-N'-(2,3-디하이드로-1,8-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아 또는 (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-클로로페닐)-우레아인 화합물.
  7. 제6항에 있어서, 3(RS)-1,3-디하이드로(2-인돌카보닐아미노)-5-페닐-2H- 1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이드로-3(RS)-(2-인돌카보닐-아미 노)-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(2-인돌카보닐아미노)-1-메틸-5-페닐-2H-1,4-벤조이다제핀-2-온, 1,3-디하이드로-1-메틸-3(RS) -[2-(1-메틸인돌)-카보닐아미노]-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이 드로-1-메틸-3(RS)-(4-클로로페닐귀보닐)-아미노-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3(RS)-(2-인돌-카보닐아미노-1-메틸-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-1-메 틸-3(RS)-[2'-(1'-메틸인돌)카보닐아미노]-2H-1,4-벤조이다제핀-2-온, 3(S)-(-)- 1,3-디하이드로-3-(2-인돌카보닐아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(2-인돌-카보닐아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-3-(4-클로로벤조일아미노)-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(-)-1,3-디 하이드로-3-(4-브로모벤조일아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로-3-(RS)-(2-인돌카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(4-클로로페닐카페닐보닐아미노-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이드로-5-(2-플루오로-3(RS)-(2-인돌카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5- (RS)-(5-플루오로인돌페닐-2-카보닐아미노)-5-(2-플루오로페닐)-2H-1,4-벤조이다제핀-2-온, 1,3-디하이드로-3-(RS)-(1-메틸인돌-2-카보닐아미노)-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3-(RS)- (2-벤조푸란카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메틸-3- (RS)-(4-클로로페닐카노닐)-아미노-5-페닐-2H-1,4-벤조디아제핀-2-온, 3(S)-(+) -3-(3-브로모벤조일아미노)-1,3-디하이드로-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-3-(4-브로모벤조일아미노)-1,3-디하이드로-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(4-요오도-벤조일아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, (S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(3-요오드-벤조일아미노)-1-메틸--2H-1,4-벤조디아제핀-2-온, 1,3-디하이드-5-(2-플루오로페닐)-3(RS)-(2-인돌) -카보닐아미노-2H-1,4-벤조디아제핀-2-티온, 3(S)-(2-인돌카보닐)아미노-1,3-디하이드로-5-페닐-2H-1,4-벤조디아제핀-2-온, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-3-페닐-2-프로페나미드, 3N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-2-아미노-4-클로로벤자미드, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-4-(트리플루오로메틸)-벤자미드, 5-(2-플루오로페닐)-2,3-디하이드로-3-((1H-인돌-2-일카보닐)아미노)-2-옥소-lH-1,4-벤조디아제핀-1-아세트산 에틸 아세테르, 4-브로모-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아페닐-3-일) -벤자미드, N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-1H-1,4-벤조 디아제핀-3-일)-4-(트리플루오로페닐)-벤자미드, (S)-N-(5-(2-플로오로페닐)-2,3디하이드로-1-메틸-2-옥소-1H-1,4-벤조피아제핀-3-일)-4-(트리플루오로메틸)-벤자미드, N-(2-클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)우레아, N-(2,4-디클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-N'-(2-니트로페닐)-우레아, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(2-클로로페닐)-우레아, 3-N-(2,3-디하이드로-9-메틸-2-옥소-5-페닐-lH-(1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, 3-N-(2,3-디하이드로-1,9-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, 3-N- (2,3-디하이드로-1-메틸-2-옥소-5-(P-톨릴)-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, N-(3-메톡시페닐) -N'-(2,3-디하이드로-1-메틸-2-옥소-5-(P-톨릴)-lH-1,4-벤조디아제핀-3-일)-우레아, 3-N-(2,3-디하이드로-1,8-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드 및 N-(3-메톡시페닐) -N'-(2,3-디하이드로-1,8-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아인, 화합물.
  8. 제6항에 있어서, 3-((((4-클로로페닐)아미노)카보닐)아미노)-5-(2-플루오로페 닐)-2,3-디하이드로2-옥소-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, 3-(((( 4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, 3-((((4-클로로페닐)아미노)카보닐)아미노-N, N-디에틸-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, 1- ((3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-일)-아세틸)피롤리딘, 1-((3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-일)-아세틸)-4-메틸피페라진, 3-(((4-클로로페닐)아세틸)아미노)-2,3-디하이드로-2-옥소-5-페-lH- 1,4-벤조디아제핀-1-아세트산 에틸 에스테르, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH1,4-벤조피아제핀-3-일)-N'-페닐우레아, 에스테르, N-(4-니트로페닐) -N-(2,3-디하이드로-1-메틸-5-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아,(R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조아세핀-3-일)-N'-(3-메톡시페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메틸페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-브로모페닐)-우레아, 1-{[3-[(((3-메톡시페닐)아미노)카보닐)아미노]-2,3-디하이드로-3-옥소-5-페닐-lH-1,4-벤조디아제핀-1-일]아세틸}피롤리딘, 1-{[((3-메톡시페닐)아미노)카보닐)아미노]-N, N-디에 틸-2,3-디하이드로-2-옥소-5-페닐-1H-1,4-벤조디아제핀-1-아세타미드, 3-{[((2-클로로페닐)아미노)카보닐)아미노]-N, N-디에틸-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(4-메틸페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메틸페닐)-우레아인 화합물.
  9. 폴레시스토키닌 수응체 또는 가스트린 수용체를 각기 일반식 (Ⅰ)의 화합물 또는 그의 약제학적으로 허용되는 염과 접촉시킴을 특징으로 하여, 콜레시스토키닌 또는 가스트린이 각각 콜레시스토키닌 수용체 또는 가스트린 수용체에 결합하는데 길항하는 방법.
    상기식에서, R1은 H, C1-C6선형 또는 측쇄 알킬, 저급 알케닐, 저급 알키닐, -X12COOR6, X12-시클로저급 알킬, -X12NR4R5, -X12CONR4R5, -X12CN, 또는 -X11CX3 10이고 : R2는 N, 저급 알킬, 치환 또는 비치환된 페닐(여기에서, 치환체는 1또는 2개의 할로, 저급 알킬, 저급 알콕시, 저급 알킬티오, 카복실, 카복시저급 알킬, 니트로, -CH3, 또는 하이드록시일 수 있다), 2-, 3-, 4-피리딜,
    -X11NR18SO2(CH2)qR7또는-R7이고 ; R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일- 또는 이-치환된 포화 또는 분포화된 4 내지 7원 헤테로시클릭환 또는 벤조융합된 4 내지 7원 헤테로시클릭환 또는 O 및 NCH3로 부터 선택된 제2의 헤테로원자를 추가로 함유하는 상기 헤테로시클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환제(들)은 독립적으로 C1-C4알킬로 부터 선택되며, R6는 H 저급 알킬, 시클로저급 알킬, 치환 또는 비치환된 페닐, 또는 치환 또는 비치환된 페닐저급 알킬(여기서, 페닐 또는 페닐저급 알킬 치환제는 1또는 2개의 할로, 저급 알킬, 저급 알콕시, 니트로, 또는 CF3인 수 있다)이며 : R7및 Ra 7은 독립적으로 ?? - 또는 ??-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, -NO2, -OH, -X11NR4R5, 저급 알킬, CF3, CN, SCF3, C CH, CH2SCF3,OCHF2, SH, SPh, PO3H, 저급 알콕시, 저급 알킬티오, 또는 COOH이다), 2-,3-, 4-피리딜,
    R8은 H 저급 알킬, 시클로저급 알킬, -X12CONH2, -X12COOR6, -X12-시클로저급 알킬, -X12NR4R5, 또는
    이며 ; R9및 R10은 독립적으로 H, -OH, 또는 -CH3이고 R11및 R12는 독립적으로 저급알킬 또는 시클로저급알킬이며 : R13은 H, 저급알킬, 아실, 0, 또는 시클로저급알킬이고 : R14는 저급알킬 또는 페닐저급알킬이며 : R15는 H, 저급알킬,, 또는 -NH2이고 R18은 H, 저급알킬, 또는 아실이며 : P는 그의 인접한 임의의 이중결합이 불포화된 경우에 0이고, 그의 인접한 임의의 이중결합…이 포화된 경우에는 1이며, 단, R13이 0이고, P가 1이며, 이 불포화된 경우는 제외하며 q는 0내지 4이고 : r은 1 또는 2이며 : X,은 H, -NO2, CF3, CN, OH, 저급알킬, 할로, 저금알킬티오, 저급알콕시, -X11COOR6, 또는 -X11NR4R5이고 X2및 X3는 독립적이고 H, -OH, -NO2, 할로, 저급알킬티오, 저급알킬 또는 저급알콕시이며 : X4는 S, O, CH2, NR18또는 NR8이고 : X5는 H, CF3, CN, -COOR6, NO2또는 할로이며 : X8는 O 또는 HH이고 : X7은 O, S, HH, 또는 NR15이며, 단, R1이 H가 아닌 경우에만 X7이 NR15일수 있으며 X8은 H, 저급알킬이고 : X9및 Xa 9는 독립적으로 NR18또는 O이며 : X10은 F, Cl, 또는 Br이고 : X11은 부재하거나 C1-4선형 또는 측쇄 알킬리덴 이며 : X12는 C134선형 또는 측쇄 알킬리덴이고 :…는 포화 또는 불포화된 결합이다 ;
  10. 제9항에 있어서, R1은 H, C1-C6선형 또는 측쇄 알킬, -X12COOR6, -X11-시클로저급알킬, -X12CONR4R5이고 : R1는 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, 저급알킬, 저급알콕시, 저급알킬터오, 카복실, 카복시저급알킬, 니트로, -CF3, 또는 하이드록시일수 있다), 2-, 3-, 4-피리딜,또는 -X12COOR6이며 : R3는
    R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일-또는 이-치환된 포화 또는 불포화 4 내지 7원 헤테로시클릭환 또는 벤조융합된 4 내지 7원 헤테로시클릭환, 또는 O 및 NCH3로부터 선택된 제2의 헤테로원자를 추가로 함유하는 상기 헤테로시클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환체(들)은 독립적으로 C1-C4알킬로부터 선택되고 R6는 H, C1-C4직쇄 또는 측쇄 알킬 또는 C3-C6시클로알킬이며 : R7은 α - 또는 β-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, -NO2, OH, -X11NR4R5, 저급알킬, CF3, CN, SCF3,SH, SPh, 지급알콕시, 저급알킬티오 또는 카복시이다), 2-, 3-, 4-피리딜,
    R8은 H, 저급알킬 또는 시클로저급알킬이며 : R9및 R10은 독립적으로 H, -OH, 또는 -CH3이고 : R13은 H, 저급알킬, 아실, O, 또는 시클로저급알킬이며 : R18은 H 또는 저급알킬이며 : P는 그의 인접한 임의의 이중결합…이 불포화된 경우에 O이고, 그의 인접한 임의의 이중결합…이 포화된 경우에는 1이며, 단, R13이 O이고, P가 1이며,…이 불포화된 경우는 제외하며 : q는 0내지 2이고 : r는 1 또는 2이며 X1은 H, -NO2, CF3, CN, 저급알킬, 할로, 저급알킬티오, 또는 -X11COOR6이고 : X2및 X3는 독립적으로 H, -NO2, 할로, 저급알킬티오, 저급알킬 또는 저급알콕시이며 : X4는 S, O, 또는 NR8이고 : X5는 H, CF3, CN, -COOR6, NO2또는 할로이며 : X6는 O 또는 HH이고 : X7은 O, S이며, X9및 Xa 9는 독립적으로 NR8또는 O이고 : X11은 부재하거나 C1-4, 선형 알킬리덴이며 : X12는 C1-4선형 또는 측쇄 알킬리덴이고 : 는 포화 또는 불포화된 결합인 화합물 또는 그의 약제학적으로 허용되는 염과 접촉시키는 방법.
  11. 제10항에 있어서, R1은 H, C1-C3선형 또는 측쇄 알킬, -X12COOR6, -X12CONR4R5이고 : R2는 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, 저급알킬, 카복실, 니트로, 또는 -CF3일수있다) : -X12COOR6: 2-, 3-, 4-피리딜이며 : R3는또는이고 : R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일- 또는 이-치환된 포화 또는 불포화 4 내지 7원 헤테로시클릭환 또는 벤조융합된 4 내지 7원 헤테로시클릭환, 또는 O 및 NCH3로부터 선택된 제2의 헤테로원자를 추가로 함유하는 상기 헤테로시클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환체(들)은 독립적으로 C1-C4알킬로부터 선택되고 : R6는 H, C1-C4직쇄 또는 측쇄 알킬이고 : R7은 α - 또는 β-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, -NO2, -OH, -NR4R5, 저급알킬, CF3, CN, 또는 저급알콕시이다), 2-, 3-, 4-피리딜,
    R9및 R10은 독립적으로 H, 또는 -OH이고 : P는 그의 인접한 임의의 이중결합…이 불포화된 경우에 0이고, 그의 인접한 임의의…이중결합이 포화된 경우에는 1이며, (R13)p에서는 0이고 : r는 1 또는 2이며 : X1은 H, -NO2, CF3, 저급알킬, 또는 할로이고 : X2및 X3는 독립적으로 H, -NO2, 할로, 저급알킬 또는 저급알콕시이며 : X4는 0, 또는 NR8이고 : X7은 O, 또는 S이고 : X12는 C1-2선형 또는 측쇄 알킬리덴이고 :…는 포화 또는 불포화된 결합인 화합물 또는 그의 약제학적으로 허용되는 염과 접촉시키는 방법.
  12. 제11항에 있어서, R1이 H, C1-C2선형 알킬, -X12COOR6-X12CONR4R5이고 : R2는 치환 또는 비치환된 페닐(여기에서, 치환체는 할로, 저급알킬, 니트로, -CF3일수 있다), 2-, 3-, 4-피리딜 또는 X12COOR6이며 : R3 또는이고 ; R4및 R5는 독립적으로 R6이거나, 또는 NR4R5그룹의 N과 함께 비치환되거나 일- 또는 이-치환된 포화 또는 불포화 4 내지 7원 헤테로시클릭환 또는 벤조융합된 4 내지 7원 헤테로시클린환, 또는 O 및 NCH3로부터 선택된 제2의 헤테로원자를 추가로 함유하는 상기 헤테로시클릭환 또는 상기 벤조융합된 헤테로시클릭환이고, 치환체(들)은 독립적으로 C1-C4알킬로부터 선택되며 R6는 H, C1-C3직쇄 알킬이고 : R7은 ?? - 또는 ??-나프틸, 치환 또는 비치환된 페닐(여기에서, 치환체는 1 또는 2개의 할로, -NO2, NH2, 메틸, 에틸, CF3, CN 또는 저급알콕시일수 있다), 2-, 3-, 4-피리딜,
    R10은 H, 또는 OH이고 : P는 (R10)P에서 1이고, (R9)P 및 (R13)P에서는 0이며, 4,5위치의…는 불포화되고, 3,4위치의…는 포화되며 : r은 1 또는 2이며 : X1은 H, -NO2, CF3, 저급알킬 또는 할로이며 : X2은 H, -NO2, 할로 또는 저급알킬이고 : X4는 O, NH, NCH3이며 : X7는 O 또는 S이고 : X12는 C1-2선형 알킬리덴이며 :…는 포화 또는 불포화 결합인 화합물 또는 그의 약제학적으로 허용되는 염과 접촉시키는 방법.
  13. 제12항에 있어서, R1이 H, CH3, CH2CH3, CH2COOH, CH2COOEt, CH2CON(Et)2,또는 CH3CH2COOEt이고 :R2는 페닐, 2-F페닐, 4-CH3-페닐, 2-, 3-, 4-피리딜이며 : R3는
    R10은 H, 또는 -OH이고 P는 (R10)P에서 1이고, (R9)P 및 (R13)P에서는 0이며, 4,5위치의…는 불포화되고 3,4위치의…는 포화되며 : r은 1이고 : X1은 H, 7-Cl, 8-CH3, 9-CH3이며 : X7은 O 또는 S이고 : 는 포화 또는 불포화 결합인 화합물 또는 그의 약제학적으로 허용되는 염과 접촉시키는 방법.
  14. 제9항에 있어서, 화합물이 3(RS)-1,3-디하이드로(2-인돌카보닐아미노)-5-페 닐-2H-1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이드로-3(RS)-(2-인돌카보닐-아미노)-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3(RS)-(2-인돌카보닐아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메틸-3(RS)-[2-(1-메틸인돌)-카보닐아미노]-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메틸-3(RS)-(4-클로로페닐카보닐)-아미노-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3(RS)-(2-인돌-카보닐아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페 닐)-1-메틸-3-(RS)-[2'-(1'-메틸인돌)카보닐아미노]-2H-1,4-벤조디아제핀-2-온, 3(S)-(-)-1,3-디하이드로-3-(2-인돌카보닐아미노)-1-메틸-5-페닐-2H-1,4-벤조디 아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(2-인돌-카보닐아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-3-(4-클로로벤조일아미노)-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(-)- 1,3-디하이드로-3-(4-브로모벤조일아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로 -5-(2-플루오로페닐)-3-(RS)-(2-인돌카보닐아미노) -2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(4-클로로페닐카보닐)아미노-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이드로-5-(2-플루오로페닐)-3(RS)-(2-인돌카보닐아미노-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(5-플루오로인돌-2-카보닐아미노)-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(1-메틸인돌-2-카보닐아미노) -5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3-(RS)-(2-벤조푸란카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이 드로-1-메틸-3-(RS)-(4-클로로페닐카보닐)-아미노-5-페닐-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-3-(3-브로모벤조일아미노)-1,3-디하이드로-5-(2-플루오로페닐) -1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-3-(4-브로모벤조일아미노)-1,3-디하이드로-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3 (4-요오도-벤조일아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(3-요오도-벤조일아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페 닐)-3-(RS)-(2-인돌)-카보닐아미노-2H-1,4-벤조디아제핀-2-티온, 3(S)-(2-인돌카보닐)아미노-1,3-디하이드로-5-페닐-2H-1,4-벤조디아제핀-2-온, (S)-N-(2,3-디 하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-3-페닐-2-프로페나미드, 3-((((4-클로로페닐)아미노)카보닐)아미노)-5-(2-플루오로페닐)-2,3-디하이 드로-2-옥소-lH-t,4-벤조디아제핀-1-아세트산 에틸 에스테르, 3-N-(2,3-디하이 드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-2-아미노-4-클로로벤자미드, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일) -4-(트리플루오로메틸)-벤자미드,3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디 하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르,5- (2-플루오로페닐)-2,3-디하이드로-3-((IH-인돌-2-일카보닐)아미노)-2-옥소-lH-1,4-벤조디아제핀-1-아세트산 메틸 에스테르, 4-브로모-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-벤자미드, N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조디아제핀-3-일)-4-(트리플루오로메틸)-벤자미드, (S)-N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조 디아제핀-3-일)-4-(트리플루오로메틸)-벤자미드, 3-((((4-클로로페닐)아미노)카보닐)아미노)-N, N-디에틸-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, 1-((3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조더아제핀-1-일)-아세틸)피롤리딘, 1-((3-((((4-클로로페피닐) 아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-일)-아세틸)-4-메틸피페라진, 3-(((4-클로로페닐)아세틸)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시 페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-페닐우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(4-메 틸페 닐)-우레아, N- (2-클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레 아, N-(4-니트로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디 아제핀-3-일)-우레아, N-(2,4-디클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-N'-(3-메틸페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-니트로페닐)-우레 아, N-(3-클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디 아제핀-3-일)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, N-(2,3-디 하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(2-니트로페닐) -우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일) -N'-(2-플루오로페닐)-3-우레아, N-(3-브로모페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-N'-1-나프탈레닐-우레아, (S)-N- (2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(2-클로로페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디 아제핀-3-일)-N'-(3-메틸페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-브로모페닐)-우레아, 1-{[3-[3- [((( 3-메톡시페닐)아미노)카보닐)아미노] -2,3-디하이드로-2-옥소-5-페닐-1H-1,4-벤조디아제핀-1-일]아세틸}피롤리딘, 3-{[(((3-메톡시페닐)아미노)카보닐)아미노]-N, N-디에틸-2,3-디하이드로-2-옥소-5-펜닐-lH-1,4-벤조디아제핀-1-아세타미드, 3-{[(((2-클로로페닐)아미노)카보닐)아미노]-N,N-디에틸-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, 3-N-(2,3-디하이드로-9-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, 3-N-(2,3-디하이드로-1,9-디메틸-2-옥소-5-페닐-lH-1,4-벤조더아제핀-3-일)-lH-인돌-2-카복사미드, N-(3-메톡시페닐)-N'-(2,3-디하이드로-1,9-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, 3-N-(2,3-디하이드로-1-메틸-2-옥소-5-(P-톨릴)-lH -1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, N-(3-메틸페닐)-N'-(2,3-디하이 드로-1-메틸-2-옥소-5-(P-톨릴)-lH-1,4-벤조디아제핀-3-일)-우레아, (R)-N-2,3 디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(4-메틸페닐) -우레아, 3-N-(2,3-디하이드로-1,8-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀 -3-일)-lH-인돌-2-카복사미드, N-(3-메톡시페닌)N'-(2,3-디하이드로-1,8-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아 또는 (R)-N-(2,3-디하미드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-클로로페닐)-우레아로 이루어진 그룹으로부터 선택되는 방법.
  15. 제9항에 있어서, 콜레시스토키닌이 콜레시스토키닌 수용체에 결합하는데 길항하기 위한 것이며, 화합물이 3(RS)-1,3-디하이드로(2-인돌카보닐아미노)-5-페닐-2H-1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이드로-3 (RS)-(2-인돌카보닐-아미노)-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3 (RS)-(2-인돌카보닐아미노)-1-메틸-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메 틸-3 (RS)-[2-(1-메틸인돌)-카보닐아미노]-5-페닐-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-1-메틸-3 (RS)-(4-클로로페닐카보닐)-아미노-5-(2-플루오로페 닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3(RS)-(2-인돌-카보닐아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-1-메틸-3 (RS)-[2'-(1'-메틸인돌)카보닐아미노]-2H-1,4-벤조디아제핀-2-온, 3(S)-(-)-1,3-디하이드로-3-(2-인돌카보닐아미노)-1-메틸-3-페닐-2H-1,4 -벤조디아제핀-2◎온, 3(S)-(+)-1,3--디하이드로-3-(2-플루오로페닐)-3-(2-인돌-카보닐아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-3-( 4-클로로벤조일아미노)-5-(2-플루오로페닐)-1-메 틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(-)-1,3-디하이드로-3-(4-브로모벤조일아미노)-1-메틸-5-페닐-2H-1,4-벤조 디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3-(RS)-(2-인돌카보닐아미 노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)- (4-클로로페닐카보닐)아미노-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1-카복시메틸-1,3-디하이 드로-5-(2-플루오로페닐)-3(RS)-(2-인돌카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(5-플루오로린돌-2-카보닐아미노)-5-(2-플루오로페 닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-3-(RS)-(1-메틸인돌-2-카오닐아미노)-5-(2-플루오로페닐)-2H-1,4-벤조디아제핀-2-온, 1,3-디하이드로-5-(2-플루오로페닐)-3-(RS)-(2-벤조푸란카보닐아미노)-2H-1,4-벤조디아제핀-2-온, 1,3-디 하이드로-1-메틸-3-(RS)-(4-클로로페닐카보닐)-아미노-5-페닐2H-1,4-벤조디아제 핀-2-온, 3(S)-(+)-3-(3-브로모벤조일아미노)-1,3-디하이드로-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-3-(4-브로모벤조일아미노)-1,3 -디하이드로-5-(2-플루오로페닐)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+) -1,3-디하이드로-5-(2-플루오로페닐)-3-(4-요오도-벤조일아미노)-1-메틸-2H-1,4-벤조디아제핀-2-온, 3(S)-(+)-1,3-디하이드로-5-(2-플루오로페닐)-3-(3-요오도-벤조일아미노)-1-메틸-2H-1,4-벤조디아제핀-1-온, 1,3-디하이드로-5-(2-플루오로 페닐)-3-(RS)-(2-인돌)-카보닐아미노-2H-1,4-벤조디아제핀-2-티온, 3(S)-(2-인돌카보닐)아미노-1,3-디하이드로-5-페닐-2H-1,4-벤조디아제핀-2-온, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-3-페닐-2-프로페나미드, 3-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일) 2-아미노-4-클로로벤자미드, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-4-(트리플루오로메틸)-벤자미드, 5-(2-플루오로페닐) -2,3-디 하이드로-3-((1H-인돌-2-일-카보닐)아미노)2-옥소-lH-1.4-벤조디아제핀-1-아세트산 에틸 에스테르, 4-브로모-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-벤자미드, N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조디아제핀-3-일)-4-(트리플루오로메틸)-벤자미드, (S) -N-(5-(2-플루오로페닐)-2,3-디하이드로-1-메틸-2-옥소-lH-1,4-벤조디아제핀-3-일)-4-(트리플루오로메틴)-벤자미드, N-(2-클로로페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, N-(2,4-디클로로페닐)-N' -(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, (S) -N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(2-니트로페닐)-우레아, (S)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-N'-(2-클로로페닐)-우레아, 3-N-(2,3-디하이드로-9-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복시미드, 3-N-(2,3-디하이드로-1,9-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드, 3-N-(2,3-디하이드로-1-메틸-2-옥소-5-(P-톨릴)-lH -1,4-벤조디 아제핀-3-일)-lH-인돌-2-카복사피드, N-(2-메톡시페닐)-N'-(2,3-디하이드로-1-메틸-2-옥소-5-(P-톨릴)-lH-1,4-벤조디아제핀-3-일)-우레아, 3-N-( 2,3-디하이드로-1,8-디메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-lH-인돌-2-카복사미드 및 N-(3-메톡시페닐)-N'-(2,3-디하이드로-1,8-디메틸-2-옥소-5-페 닐-lH-1,4-벤조디아제핀-3-일)-우레아로 이루어진 그룹으로부터 선택되는 방법.
  16. 제9항에 있어서, 가스트린이 가스트린 수용체에 결합하는데 길항하기 위한 것이며 화합물이 3-((((4-클로로페닐)아미노)카보닐)아미노)-5-(2-플루오로페닐)-2, 3-디하이드로-2-옥소-lH-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, 3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-1H-1,4-벤조디아제핀-1-아세트산 에틸 에스테르, 3-((((4-클로로페닐)아미노)카보닐)아미노)-N,N-디에틸-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, 3-((((4-클로로페닐)아미노)카보닐)아미노)-2,3-디하이드로-2-옥소-5-페닐-1H-1,4-벤조디아제핀-1-일)-아세틸)피롤리딘, 1-((3-((((4-클로로페닐)아미노)카보닐)아미 노)-2,3-디하이드로-2-옥소-5-페닐-1H-1,4-벤조디아제핀-1-일)-아세틸)-4-메틴퍼페라진, 3-(((4-클로로페닐)아세틸)아미노)-2,3-디하이드로-2-옥소-5-페닐-lH-1, 4-벤조디아제-1-아세트산 에틸 에스테르, N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-페닐우레아, N-(4-니트로페닐)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-우레아, (R)-N(2,3-디 하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메톡시페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-레틸페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-브로모페닐)-우레아, 1-{[3-[(((메톡시페닐)아미노)카보닐)아미노]-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-일]아세틸 )피롤리딘, 3-{[(((3-메톡시페닐)아미노)카보닐)아미노}-N,N-디에틸-2,3-디 하이드로-2-옥소-5-페닐IH-1,4-벤조디아제핀-1-아세타미드, 3-{[((2-클로로페닐) 아미노)카보닐)아미노)-N,N-디에틸-2,3-디하이드로-2-옥소-5-페닐-lH-1,4-벤조디아제핀-1-아세타미드, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-1H-1,4-벤조디아제핀-3-일)-N'-(4-메틸페닐)-우레아, (R)-N-(2,3-디하이드로-1-메틸-2-옥소-5-페닐-lH-1,4-벤조디아제핀-3-일)-N'-(3-메틸페닐)-우레아로 이루어진 그룹으로부터 선택되는 방법.
  17. 제9항에 있어서, 동물의 위장관 장애, 중추신경계 장애를 치료하거나 또는 식욕을 조절하기 위해 치료학적 유효량의 상기 혼합물을 사용하는 방법.
  18. 콜레시스토키닌 수용체 또는 가스트린 수용체를 각기 제1항에 따른 화합물 또는 그의 약체학적으로 허용되는 염과 접촉시켜 콜레시스토키닌 또는 가스트린이 각각 콜레시스토키닌 수용체 또는 가스트린 수용체에 결합하는 것에 길항하는 유용한, 치료학적 유효량의 제1항의 화합물 및 약제학적으로 허용되는 담체를 함유하는 약제학적 조성물.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
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HK157196A (en) 1996-08-23
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AU1313388A (en) 1988-09-15
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ATE106401T1 (de) 1994-06-15
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