1,5-benzodiazepine derivatives useful as cck or gastrin antagonists

PCT No. PCT/EP94/02352 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Jul. 18, 1994 PCT Pub. No. WO95/03284 PCT Pub. Date Feb. 2, 1995Compounds of general formula (I) (I) wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11bridgedcycloalkyl or C1-6alkyl group which alkyl group m...

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Hauptverfasser: STEFANO POLINELLI, MARIO PELLEGATTI, GIOVANNI CUROTTO
Format: Patent
Sprache:eng
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Zusammenfassung:PCT No. PCT/EP94/02352 Sec. 371 Date Nov. 4, 1996 Sec. 102(e) Date Nov. 4, 1996 PCT Filed Jul. 18, 1994 PCT Pub. No. WO95/03284 PCT Pub. Date Feb. 2, 1995Compounds of general formula (I) (I) wherein R1 represents a phenyl, C3-7cycloalkyl, C7-11bridgedcycloalkyl or C1-6alkyl group which alkyl group may be substituted by a hydroxy, phenyl, C1-6alkoxycarbonyl, C3-7cycloalkyl, or C3-7bridgedcycloalkyl group; R2 represents phenyl substituted by a group (CH2)nNR4R5, O(CH2)pR6, or (CH2)nCO2R11; R3 represents phenyl optionally substituted by one or 2 halogen atoms; R4 represents hydrogen or C1-4alkyl; R5 represents acyl, or C2-4alkyl substituted by one or more hydroxy; carboxyl and/or amino groups or R4 and R5 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 C1-4alkyl or hydroxy groups. R6 represents hydroxy, C1-4alkoxy, CO2R7 or NR8R9; R7 represents hydrogen or C1-4alkyl or a metabolically labile ester group; R8 represents hydrogen, C1-4, acyl or C2-6alkyl substituted by one or more hydroxy, carboxyl and/or amino groups or R8 and R9 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 C1-4alkyl or hydroxy groups; R10 represents hydrogen or a halogen atom; R11 represents a metabolically labile ester group; m is zero, 1 or 2; n is zero or 1; p is an integer from 1 to 4; X represents oxygen or NH and pharmaceutically acceptable, salts thereof are antagonists of gastrin and CCK.