发明名称 1,5-BENZODIAZEPINE DERIVATIVES USEFUL AS CCK OR GASTRIN ANTAGONISTS
摘要 <p>Compounds of formula (I) wherein R1 represents a phenyl, C¿3-7?cycloalkyl, c7-11 bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C7-11 bridgedcycloalkyl group; R?2¿ represents a phenyl group optionally substituted by 1 or 2 substituents selected from halogen, C¿1-4?alkyl, C1-4alkylthio, cyano, nitro, trifluoromethyl, trifluoromethoxy, (CH2)nR?4¿ or O(CH¿2)pR?4 wherein R4 represents hydroxy, C¿1-4?alkoxy, CO2R?5 or NR6R7¿; n is zero or 1; p is an integer from 1 to 4; R3 represents the group AlkNR8R9; R5 represents hydrogen or C¿1-4?alkyl; R?6¿ represents hydrogen or C¿1-4?alkyl; R?7¿ represents hydrogen, C¿1-4?alkyl, acyl, or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R?6 and R7¿ together with the nitrogen atom to which they are attached form a 5-7 saturated heterocyclic ring which contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C¿1-4?alkyl or hydroxy groups. R?8 and R9¿ independently represent hydrogen, C¿1-4?alkyl or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R?8 or R9¿ together with the nitrogen atom which they are attached represent a 5-7 saturated heterocyclic ring which may contain an additional heteroatom selected from oxygen, sulphur or nitrogen and/or may be substituted by 1 or 2 C¿1-4?alkyl or hydroxy groups; Alk represents a straight or branched C2-6alkylene chain optionally substituted by a hydroxyl group; R?10¿ represents hydrogen or a halogen atom; m is zero, 1 or 2; X is oxygen or NH; and pharmaceutically acceptable salts and or metabolically labile esters thereof are antagonists of gastrin and CCK.</p>
申请公布号 WO1995003285(A1) 申请公布日期 1995.02.02
申请号 EP1994002353 申请日期 1994.07.18
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