Dipeptide derivatives and their production

C - Chemistry – Metallurgy – 07 – K

Patent

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530/5.02

C07K 5/06 (2006.01) C07K 5/065 (2006.01) C07K 5/10 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1181065

DIPEPTIDE DERIVATIVES AND THEIR PRODUCTION ABSTRACT OF THE DISCLOSURE Dipeptide derivatives represented by the formula: Image wherein R represents hydrogen, C1-C6alkyl group, C2-C7alkenyl group, C2-C7 cyanoalkyl group, C2-C7carbamoylalkyl group C3-C10dialkylaminoalkyl group or cyclopropylmethyl group, R1 represents hydrogen, C1-C6 alkyl group, C7-C14 aralkyl group, C7-C14hydroxyaralkyl group, C6-C12aryl group, C2-C7carbamoyl- alkyl group, C2-C7carboxyalkyl group, C1-C6aminoalkyl group, C4-C10guanidylalkyl group, C1-C6mercaptoalkyl group, C2-C7alkyl- thioalkyl group, C9-C15indolylalkyl group or C4-C9imidazolylalkyl group, R2 represents hydrogen, C1-C6alkyl group, C7-C14aralkyl group, C6-C12aryl group, glycyl group or glycyl-glycyl group, R3 represents hydrogen, C1-C6alkyl group or amino-protecting group, R1 and R2 optionally combine to from C2-C4 alkylene group, group R2-N-R3 optionally represents phthalimido group, piperidino group, 4-hydroxy-4-(p-halogenophenyl)piperidino, morpholino, or piperazino group substituted by C1-C6alkyl group or phenyl group, A ring represents benzene ring or pyridine ring optionally substituted by halogen and B ring represents benzene ring or thiophene ring optionally substituted by halogen, trifluromethyl group, methylsulfonyl group, nitro group or C1-C6alkyl group and their acid addition salts, being useful as anxiolytics, sedatives, anticonvulsants, hypnotics, muscle relaxants, or their synthetic intermediates, are prepared.

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