| 摘要 |
A compound of formula (I) wherein X is O, S, SO or SO2; R1 is halogen, trihalomethyl, -OH, C1-7alkyl, C1-4alkoxy, trifluoromethoxy, phenoxy, cyclohexylmethyloxy, pyridylmethoxy, cinnamyloxy, naphthylmethoxy, phenoxymethyl, -CH2-OH, -CH2-CH2-OH, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, benzylthio, acetyl, nitro or cyano, or phenyl, phenylC1-4alkyl or phenyl-C1-4alkoxy each phenyl group thereof being optionally substituted by halogen, CF3, C1-4alkyl or C1-4alkoxy; R2 is H, halogen, trihalomethyl, C1-4alkoxy, C1-7alkyl, phenethyl or benzyloxy; R3 H, halogen, CF3, OH, C1-7alkyl, C1-4alkoxy, benzyloxy, phenyl or C1-4alkoxymethyl; each of R4 and R5, independently is H or a residue of formula (a) wherein each of R8 and R9, independently, is H or C1-4alkyl optionally substituted by halogen; and n is an integer from 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof; or a compound of formula (II) wherein R1a is halogen, trihalomethyl, C1-4alkyl, C1-4alkoxy, C1-4alkylthio, C1-4alkylsulifinyl, C1-4alkyl-sulfonyl, aralkyl, optionally substituted phenoxy or aralkyloxy; R2a is H, halogen, trihalomethyl, C1-4alkyl, C1-4alkoxy, aralkyl or aralkyloxy; R3a is H, halogen, CF3, C1-4alkyl, C1-4alkoxy, C1-4alkylthio or benzyloxy; R4a is H, C1-4alkyl, phenyl, optionally substituted benzyl or benzoyl, or lower aliphatic C1-5acyl; R5a is H, monohalomethyl, C1-4alkyl, C1-4alkoxy-methyl, C1-4alkyl-thiomethyl, hydroxyethyl, hydroxypropyl, phenyl, aralkyl, C2-4alkenyl or -alkynyl; R6a is H or C1-4alkyl; R7a is H, C1-4alkyl or a residue of formula (a) as defined above, Xa is O, S, SO or SO2; and na is an integer of 1 to 4; or a pharmaceutically acceptable salt, hydrate, solvate, isomer or prodrug thereof, for use in a method of treatment, optionally of an autoimmune condition, wherein said compound of formula (I) or (II) is administered at a dosage lower than the standard daily dosage of said compound during the initial period of treatment and then is increased, optionally stepwise, up to the standard daily dosage of said compound. |
