| 摘要 |
(see formula 1) Compounds of general formula (1) are described wherein -W- is (1) =C(Y)- where Y is a halogen atom, or an alkyl or -XR a group where X is -O-, -S(O)m-[where m is zero or an intege r of value 1 or 2], or -N(R b)- where R b is a hydrogen atom or an optionally substituted alkyl group or, (2) =N; L is a -XR, [where R is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group], -C(R11)=C(R1)(R2) or [-CH(R11)]~CH(R1)(R2) group where R11 is a hydrogen or a fluorine atom or a methyl group, and R1 and R2, which may be the same or different, is each a hydrogen or fluorine atom or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, -CO2 R8, [where R8 is a hydrogen atom or an optionally substitute d alkyl, aralkyl, or aryl group], -CONR9R10 [where R9 and R10, which may be the same ar different are as defined for R8], -CSNR9R10, - CN or -NO2group, or R1 and R2 together with the C atom to which they are attached are linked to form an optionally substituted cycloalkyl or cycloalkenyl group and n is zero or the integer 1; Z is (1) a group -C(R3)(R4)C(R5)(R6)(R?7) or -C(R4)=C(R5)(R6) where R3 is a hydrogen or a fluorine atom or an optionally substituted straight or branched alkyl group; R4 is a group selected from -X a L1R12 [where X a is as defined above for X,L1 is a linker group and R12 is a hydrogen atom or a cycloaliphatic, heterocycloaliphatic, or monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms], -Alk1R12 [wher e Alk1 is an optionally substituted straight or branched alkenyl or alkynyl chain optionally containing one or more -O- or -S- atoms or -N(R b)-, carbocyclic or heteroatom-containing groups], -CH2L1R12a [where R12a is as defined for R12 but is not a hydrogen atom]; -X a R12a; or -C(X b)R12 [where X b is an oxygen or sulphur atom]; R5 is a -(CH2)p Ar group where p is zero or an integer 1, 2 or 3 and, Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms R6 i s a hydrogen or a fluorine atom or an optionally substituted alkyl group; R7 is a hydrogen or a fluorine atom or an OR c group where R c is a hydrogen atom or an optionally substituted alkyl or alkenyl group, or an alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group; or Z is (2) a group -C(R4)C(R5)(R6)(R7) where R4 is a group =CH2, or CH(L1)n-R12; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are phosphodiesterase type IV inhibitors acid are useful in th e prophylaxisand treatment of disease such as asthma where an unwanted inflammatory response or muscular spasm is present. unwanted inflammatory response or muscular spasm is present.
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