| abstract |
A phenylalanine derivative having the formula (I):n where R' and R 2 are independently hydrogen provided that both R' and R 2 are nof hydrogen at the same time;n C 1 -C 5 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, C 1 -C 4 alkyl- mercapto, C,-C4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C 1 -C 4 alkoxy, or halogen; C 6 -C 3 cycloalkyl which may be substituted with hydroxy, C 1 -C 4 alkoxy, hydroxylcarbonyl, C 1 -C 4 alkoxycarbonyl, or C 1 -C 4 alkyl; phenyl which may be substituted with halogen, nitro, trifluoromethyl, C,-C 4 alkoxy, C 1 -C 4 alkylmer- capto, C 1 -C 4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C 1 -C 6 alkyl which may further be substituted with C 1 -C 4 alkylcarbonyl, hydroxycarbonyl, or C 1 -C 4 alkoxycarbonyl; pyridyl which may be substituted with halogen or C 1 -C 4 alkoxy; pyrimidyl; N-benzylazacyclohexyl; and R' and R 2 may form with the nitrogen atom attached thereto a ring structure as morpholino; thiomorpholino; or piperidyl which may be substituted with phenylcarbonyl, benzyl, or C 1 -C 4 alkyl; pyrrolidyl which may be substituted with hydroxycarbonyl or C 1 -C 4 alkoxycarbonyl; and piperidine substituted with C 1 -C 4 alkyl, phenyl C 1 -C 4 alkyl, phenylcarbonyl, or C,-C 4 alkoxycarbonyl; X is hydrogen; nitro; amino; or -OZ wherein Z is hydrogen: C 1 -C 4 alkyl; C 2 -C 4 alkenyl; benzyl which may be substituted with halogen, C 1 -C 4 alkyl, nitro, trifluoromethyl, hydroxycarbonyl, C 1 -C 4 alkoxycarbonyl, or cyano; phenylcarbonylmethyl, pyridylmethyl; phenyl which may be substituted with nitro or halogen; pyridyl or pyrimidyl which may be substituted with nitro; phenylsulfonyl which may be substituted with C 1 -C 4 alkyl; or benzyloxycarbonyl which may be substituted with halogen; n is 4 to 10; and the mark indicates that the configuration of the carbon may be either one of D-configuration, L-configuration and DL-configuration or a pharmaceutical acceptable salt thereof. n This phenylalanine derivative is effective as a proteinase inhibitor. |