| 摘要 |
Compounds of the formula (I): <IMAGE> (I) wherein: X is NR wherein R is hydrogen, C1-6 alkyl; oxygen; sulphur; SO; or SO2; or R and R3 taken together are C4-6 polymethylene; R1 is hydrogen or C1-6 alkyl; and R2 is CN, CR5R6Y where R5 and R6 are independently selected from hydrogen and C1-4 alkyl and Y is selected from hydrogen, OR7 or SR7 where R7 is hydrogen, C1-4 alkyl, C2-4 alkanoyl, and NR8R9 where R8 and R9 are independently hydrogen, C1-4 alkyl, C2-4 alkenyl or C2-4 alkanoyl or R8 and R9 together are C4-6 polymethylene, or COR10 where R10 is C1-4 alkyl, provided that Y is other than hydrogen when R1 is hydrogen; or R2 is hydrogen C1-6 alkyl or phenyl optionally substituted by halogen, CF3, C1-4 alkoxy or C1-4 alkyl; and R1 is CN, CR5R6Y or COR10 as defined for R2 above; or R1 and R2 together form C3-C6 polymethylene optionally substituted by C1-C4 alkyl; R3 is C1-10 alkyl or C3-10 cycloalkyl, either optionally substituted by hydroxy, C1-4 alkoxy, thiol, C1-4 alkylthio or NR11R12 wherein R11 and R12 are independently hydrogen, C1-6 alkyl or C2-7 alkanoyl or together are C3-6 polymethylene; C2-10 alkenyl; or phenyl optionally substituted by one or two of halogen, CF3, C1-4 alkoxy, C1-4 alkyl, hydroxy, nitro, cyano, C2-10 acyloxy, NR13R14 wherein R13 and R14 are independently selected from hydrogen, C1-6 alkyl, C2-7 alkanoyl, C1-6 alkylsulphonyl or COR15 wherein R15 is hydroxy, C1-6 alkoxy or NR16R17 wherein R16 and R17 are independently selected from hydrogen or C1-6 alkyl; or together with R is C4-6 polymethylene; and R4 is hydrogen; or C1-4 alkyl or benzyl optionally substituted in the phenyl ring by one or two of halogen, CF3, C1-4 alkoxy or C1-4 alkyl and is attached at nitrogen atom 1 or 2, are disclosed as having utility in the treatment of inflammatory and allergic disorders. |
