1,5-BENZODIAZEPINE DERIVATIVES HAVING CCK AND/OR GASTRIN ANTAGONISTIC ACTIVITY

摘要

COMPOUNDS OF THE GENERAL FORMULA IFORMULA IAND PHYSIOLOGICALLY ACCEPTABLE SALTS THEREOF WHEREIN THE GROUP NR1R2 REPRESENTS A 5-7 MEMBERED SATURED HETEROCYLIC RING WHICH MAY BE SUBSTITUTED NY ONE OR TWO METHYL GROUPS;R3 IS C1-6ALKYL, C3-6CYCLOALKYL OR PHENYL OPTIONALLY SUBSTITUTED BY 1 OR 2 HALOGEN ATOMS;R4 IS PHENYL OR PHENYL SUBSTITUTED BY ONE OR TWO GROUPS SELECTED FROM HALOGEN, C1-4ALKYL, TRIFLUOROMETHYL, TRIFLUOROMETHOXY OR (CH2)NR5 WHEREIN N IS ZERO OR 1 AND R5 REPRESENTS C1-4ALKOXY, HYDROXY, NITRO, CYNO, CO2R6, S(O)PCH3, NR7R8, CONR7R8, SO2NR7CO(C1-4ALKYL), TETRAZOL, CARBOXAMIDOTETRAZOLYL, OR A 3-TRIFLUOROMETHYL 1,2,4-TRIZOLYL;R6 IS HYDROGEN, C1-4ALKYL OR BENZYL;R7 HYDROGEN OR C1-4ALKYL,R8 IS HYDROGEN, C1-4ALKYL, SO2CH3 OR SO2CF3 X REPRESENTS HYDROGEN, C11-4ALKYL OR HALOGEN;@M IS ZERO, 1 OR 2, AND P IS ZERO, 1 OR 2; PROCESSES FOR THEIR PREPARATION AND THEIR USE IN MEDICINE AS ANTAGONISTS OF GASTRIN AND CCK.