Benzodiazepine derivatives

Details Benzodiazepine derivatives Benzodiazepine derivatives

C - Chemistry, Metallurgy

07

D

167/210, 260/240

C07D 403/12 (2006.01) A61K 31/55 (2006.01) C07D 403/14 (2006.01) C07K 5/078 (2006.01) C07K 5/097 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1334589

There are described compounds of the formula: Image wherein R1 is halogen, heterocyclic group which may have one or more suitable substituent(s), aryl which may have one or more suitable substituent(s), -NH-R5 (in which R5 is hydrogen, lower alkanoyl or hydroxy(lower)- alkyl), -S-R6 (in which R6 is lower alkyl, lower alkyl substituted with carboxy and amino, lower alkyl substituted with protected carboxy and protected amino, or pyridyl), -O-R7 (in which R7 is hydrogen, hydroxy protective group, lower alkyl, lower alkenyl, ar(lower)alkyl, halo(lower)alkyl, amino(lower)alkyl, protected amino(lower)alkyl, or piperazinyl(lower)alkyl which may have lower alkyl), -CONH-R8 (in which R8 is cyano, carbamoyl(lower)alkyl, carboxy(lower)- alkyl, protected carboxy(lower)alkyl, or lower alkyl substituted with carbamoyl and aryl ), or -Z-R9 [in which R9 is hydrogen or lower Image alkyl, and Z is Image (wherein R10 is hydroxy, lower alkoxy or amino) or Image (wherein R11 is carboxy or protected carboxy and R12 is hydrogen; or R11 is halogen and R12 is halogen)], R2 is aryl which may have one or more suitable substituent(s), R3 is hydrogen or halogen, R4 is hydrogen, halogen or lower alkoxy and A is lower alkylene, and pharmaceutically acceptable salts thereof. These compounds are cholecystokinin (CCK) antagonists and can therefore be used as therapeutical agents for emesis, pancreatitis, satiety and appetite control, pain control,insulinoma, gastroparesis, acute obstruc- tive cholecystitis, irritable bowel disease, carcinoma of pancreas and the like. Also described are the preparation of these compounds and salts, pharma- ceutical compositions containing same and the treatment of various diseases as mentioned above, using these compounds or salts.

604941

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