Trisubstituted phenyl derivatives as phosphodiesterase...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/24 (2006.01) A61K 31/275 (2006.01) A61K 31/33 (2006.01) C07C 255/37 (2006.01) C07D 207/337 (2006.01) C07D 213/30 (2006.01) C07D 213/73 (2006.01) C07D 213/75 (2006.01) C07D 237/08 (2006.01) C07D 239/26 (2006.01) C07D 241/12 (2006.01) C07D 263/32 (2006.01) C07D 307/54 (2006.01) C07D 333/24 (2006.01)

Patent

CA 2135480

Compounds of general formula (1) are described wherein Y is a halogen atom or a group -OR1, where R1 is an optionally substituted alkyl group; X is -O-, -S- or -N(R7)-, where R7 is a hydrogen atom or an alkyl group; R2 is an optionally substituted cycloalkyl or cycloalkenyl group; R3 and R4, which may be the same or different, is each a hydrogen atom or an alkyl; -CO2R8 (when R8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), -CONR9R10 (where R9 and R10 which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), -CSNR9R10, -CN, - CH2CN group; Z is -(CH2)o- (where n is zero or an integer 1, 2 or 3;R5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R6 is a hydrogen atom or a hydroxyl group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.

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