Phenylalanine derivative and proteinase inhibitor

Details Phenylalanine derivative and proteinase inhibitor Phenylalanine derivative and proteinase inhibitor

C - Chemistry, Metallurgy

07

K

260/259, 260/295

C07K 5/06 (2006.01) C07C 233/57 (2006.01) C07C 233/63 (2006.01) C07C 257/00 (2006.01) C07C 311/30 (2006.01) C07C 311/35 (2006.01) C07C 323/31 (2006.01) C07D 207/16 (2006.01) C07D 211/16 (2006.01) C07D 211/32 (2006.01) C07D 211/58 (2006.01) C07D 211/62 (2006.01) C07D 213/30 (2006.01) C07D 213/40 (2006.01) C07D 213/643 (2006.01) C07D 213/75 (2006.01) C07D 239/42 (2006.01) C07D 295/185 (2006.01) C07D 307/14 (2006.01) C07D 401/12 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1297633

y PHENYLALANINE DERIVATIVE AND PROTEINASE INHIBITOR ABSTRACT OF THE DISCLOSURE A phenylalanine derivative having the formula (I): Image (I) where R1 and R2 are independently hydrogen provided that both R1 and R2 are not hydrogen at the same time; C1-C8 alkyl which may be substituted with hydroxy, hydroxycarbonyl, C1-C4 alkoxycarbonyl, C1-C4 alkylmercapto, C1-C4 alkoxy, carbamoyl, sulfamoyl, pyridyl, or phenyl which may further be substituted with nitro, C1-C4 alkoxy, or halogen; C6-C8 cycloalkyl which may be substituted with hydroxy, C1-C4 alkoxy, hydroxylcarbonyl, C1-C4 alkoxycarbonyl, or C1-C4 alkyl; phenyl which may be substituted with halogen, nitro, trifluoromethyl, C1-C4 alkoxy, C1-C4 alkylmercapto, C1-C4 alkylcarbonyl, phenylcarbonyl, hydroxycarbonyl, C1-C4 alkoxycarbonyl, carbamoyl, sulfamoyl, amidino, pyridylcarbonyl, or C1-C6 alkyl which may further be substituted with C1-C4 alkyl- carbonyl, hydroxycarbonyl, or C1-C4 alkoxycarbonyl; pyridyl which may be substituted with halogen or C1-C4 alkoxy; pyrimidyl; N-benzylazacyclohexyl; and R1 and R2 may form with the nitrogen atom attached thereto a ring structure as morpholino; thiomorpholino; or piperadyl which may be substituted with phenylcarbonyl, benzyl, or C1-C4 alkyl; pyrrolidyl which may be substituted with hydroxycarbonyl or C1-C4 alkoxycarbonyl; and pyperidine substituted with C1-C4 alkyl, phenyl C1-C4 alkyl, phenylcarbonyl, or C1-C4 alkoxycarbonyl; X is hydrogen; nitro; amino; or -OZ wherein Z is hydrogen; C1-C4 alkyl; C2-C4 alkenyl; benzyl which may be substituted with halogen, C1-C4 alkyl, nitro, trifluoromethyl, hydroxycarbonyl, C1-C4 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 C1-C4 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. This phenylalanine derivative is effective as a proteinase inhibitor.

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