Tri-substituted (aryl or heteroaryl) derivatives and pharmaceutical compositions containing the same

• Main Authors: ALEXANDER; RIKKI P, WARRELLOW; GRAHAM J, BOYD; EWAN C, HEAD; JOHN C
• Format: Patent
• Language: English
• Published: 22.04.1997
• Edition: 6
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY

Compounds of the general formula (1) (1) are described wherein Y is halogen or -OR1, where R1 is a substituted or unsubstituted alkyl; X is -O-, -S- or -N(R8)-, where R8 is hydrogen or alkyl; R2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R3 is hydrogen, halogen or -OR9, where R9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R4 and R5, which may be the same or different, are each -(CH2)nAr, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R6 is hydrogen or substituted or unsubstituted alkyl; R7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases. Compounds of the general formula (1) (1) are described wherein Y is halogen or -OR1, where R1 is a substituted or unsubstituted alkyl; X is -O-, -S- or -N(R8)-, where R8 is hydrogen or alkyl; R2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R3 is hydrogen, halogen or -OR9, where R9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R4 and R5, which may be the same or different, are each -(CH2)nAr, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R6 is hydrogen or substituted or unsubstituted alkyl; R7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases.