Patent TW-346488-B (TW)
Title: Arylsulfonylamino hydroxamic acid derivatives, method of preparing the same and pharmaceutical composition comprising the same
Inventor: ROBINSON RALPH P
IPC: A61K31/5375
Filed: 1996-04-19
Granted: 1998-12-01
Abstract: A compound of the formula (formula) or the pharmaceutically acceptable salts thereof, in which n is 1 to 6; X is hydroxy, (C1 -C6)alkoxy or NR1 R2 in which R1 and R2 are each independently selected from the group consisting of hydrogen, (C1 -C6)alkyl, piperidino, (C1-C6)alkylpiperidino, (C6 -C10)arylpiperidino, (C5-C9)heteroarylpiperidino, (C6-C10)aryl(C1-C6)alkylpiperidino, (C5-C9)heteroaryl(C1-C6)alkylpiperidino, (C1-C6)acylpiperidino, (C6-C10)aryl, (C5-C9)heteroaryl, (C6-C10)aryl(C1-C6)alkyl, (C5-C9)heteroaryl(C1-C6)alkyl, (C6-C10)aryl(C6-C10)aryl, (C6-C10)aryl(C6-C10)aryl(C1-C6)alkyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C6)alkyl, R5(C2-C6)alkyl, (C1-C5)alkyl(CHR5)(C1-C6)alkyl)in which R5 is hydroxyl), (C1-C6)acyloxy, (C1-C6)alkoxy, piperazine, (C1-C6)amido, (C1-C6)alkylthio, (C6-C10)arylthio, (C1-C6)alkylsulfinyl, (C6-C10)arylsulfinyl, (C1 -C6)alkylsulfoxyl, (C6 -C10)arylsulfoxyl, amino, (C1 -C6)alkylamino, ((C1 -C6)alkyl)2 amino; and CH(R7)COR8 in which R7 is hydrogen, (C1 -C6)alkyl, (C6 -C10)aryl(C1 -C6)alkyl, (C1 -C6)alkylthio(C1 -C6)alkyl, (C6 -C10)arylthio(C1 -C6)alkyl, (C1 -C6)alkylsulfinyl(C1 -C6)alkyl, (C6 -C10)arylsulfinyl(C1 -C6)alkyl, (C1 -C6)alkylsulfonyl(C1 C6)alkyl, (C6 -C10)arylsulfonyl(C1 -C6)alkyl, hydroxy(C1 -C6)alkyl, amino(C1 -C6)alkyl, (C1 -C6)alkylamino(C1 -C6)alkyl, ((C1 -C6)alkyl)2 amino(C1 -C6)alkyl, R9 R10 NCO(C1 -C6)alkyl or R9 OCO(C1 -C6)alkyl in which R9 and R10 are each independently selected from the group consisting of hydrogen, (C1 -C6)alkyl, and (C6 -C10)aryl(C1 -C6)alkyl and R8 is R11 O or R11 R12 N in which R11 and R12 are each independently selected from the group consisting of hydrogen, (C1 -C6)alkyl, and (C6 -C10)aryl(C1 -C6)alkyl; R3 and R4 are each independently selected from the group consisting of hydrogen, (C1 -C6)alkyl, trifluoromethyl, trifluoromethyl(C1 -C6)alkyl, (C1 -C6)alkyl (difluoromethylene), (C1 -C3)alkyl(difluoromethylene)(C1 -C3)alkyl, (C6 -C10)aryl, (C6 -C10)aryl(C1 -C6)alkyl, (C6 -C10)aryl(C6 -C10)aryl, (C6 -C10)aryl(C6 -C10)aryl(C1 -C6)alkyl (C3 -C6)cycloalkyl,(C3 -C6)cycloalkyl(C1 -C6)alkyl, hydroxy(C1 -C6)alkyl, (C1 -C6)acyloxy(C1 -C6)alkyl, (C1 -C6)alkoxy(C1 -C6)alkyl, (C1 -C6)acylamino(C1 -C6)alkyl, (C6 -C10)aryl (C1 -C6)alkoxy(C1 -C6)alkyl, (C1 -C6)alkylthio(C1 -C6)alkyl, (C6 -C10)arylthio(C1 -C6)alkyl, (C1 -C6)alkylsulfinyl(C1 -C6)alkyl, (C6 -C10)arylsulfinyl(C1 -C6)alkyl, (C1 -C6)alkylsulfonyl(C1 -C6)alkyl, (C6 -C10)arylsulfonyl(C1 -C6)alkyl, amino(C1 -C6)alkyl, (C1 -C6)alkylamino(C1 -C6)alkyl, (C1 -C6)alkylamino)2 (C1 -C6)alkyl, R13 CO(C1 -C6)alkyl in which R13 is R20 O or R20 R21 N in which R20 and R21 are each independently selected from the group consisting of hydrogen, (C1 -C6)alkyl, or (C6 -C10)aryl(C1 -C6)alkyl; or R3 and R4 or R20 and R21 may be taken together to form a (C3 -C6)cycloalkyl, oxacyclohexyl, or thiocyclohexyl; and Ar is (C6 -C10)aryl, (C1 -C6)alkyl(C6 -C10)aryl, (C1 -C6)alkoxy (C6 -C10)aryl, ((C1 -C6)alkoxy)2 (C6 -C10)aryl, or (C6 -C10)aryloxy(C6 -C10)aryl; with the proviso that when either R1 or R2 is CH(R7)COR8 in which R7 and R8 are as defined above, the other R1 or R2 is hydrogen, (C1 -C6)alkyl or benzyl.