Tri-substituted phenyl derivatives and their use in pharmaceutical compositions and methods of treatment
AssigneeCelltech Limited
InventorsEwan C. Boyd, Michael A. W. Eaton, Graham J. Warrellow
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AssigneeCelltech Limited
InventorsEwan C. Boyd, Michael A. W. Eaton, Graham J. Warrellow
Estimating the term…
Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.5)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.
A compound of formula (1) ##STR9## wherein:
A compound of formula (2) ##STR10## wherein:
A compound of formula (8) ##STR11## wherein:
A pharmaceutical composition comprising a compound of formula (1) ##STR12## wherein:
A method for preventing or treating an inflammatory disease in a patient comprising administering to said patient, in combination with a pharmaceutically acceptable carrier, a selective inhibitor of a phosphodiesterase (PDE) IV isoenzyme in an amount sufficient to elevate intracellular levels of adenosine 3',5'-cyclic monophosphate (cAMP), said inhibitor comprising a compound of the formula:
Dependencies are inferred from the claim text.