1,5-benzodiazepine derivatives having cck and/or gastrin...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 403/06 (2006.01) A61K 31/55 (2006.01) C07D 401/14 (2006.01) C07D 403/14 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01) C07K 5/078 (2006.01) C07K 5/08 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2158972

Compounds of general formula (I) and physiologically acceptable salts thereof wherein the group NR1R2, represents a 5-7 membered saturated heterocyclic ring which may be substituted by 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, cyano, CO2R6, S(O)pCH3, NR7R8, CONR7R8, SO2NR7CO(C1-4alkyl), tetrazolyl, carboxamidotetraxolyl, or a 3-trifluoromethyl 1,2,4-triazolyl; R6 is hydrogen, C1-4alkyl or benzyl; R7 is hydrogen or C1-4alkyl, R8 is hydrogen, C1-4alkyl, SO2CH3 or SO2CF3, X represents hydrogen, C1-4alkyl 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.

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