Some of the compounds described herein contain olefinic double bonds, and unless specified otherwise, are meant to include both E and Z geometric isomers.
Salts The pharmaceutical compositions of the present invention comprise a compound of Formula I as an active ingredient or a pharmaceutically acceptable salt, thereof, and may also contain a pharmaceutically acceptable carrier and optionally other therapeutic ingredients.
Within this genus of compounds of formula Ic ##STR8## there is a sub-genes wherein: R alkyl, especially hydrogen, p-methyl and p-ethyl.
It will also be of use in the treatment of Alzheimer's disease, for decreasing bone loss particularly in postmenopausal women (i.e. Within this sub-genus, the 3-pyridinyl isomers, such as those of formula Ic, are particularly preferred.This invention relates to methods of treating cyclooxygenase mediated diseases and certain pharmaceutical compositions therefor. 4, 1996) discloses compounds represented by Formula A as being useful in the treatment of COX-2 mediated diseases, by virtue of their selective inhibition of COX-2 rather than COX-1.Non-steroidal, antiinflammatory drugs exert most of their antiinflammatory, analgesic and antipyretic activity and inhibit hormone-induced uterine contractions and certain types of cancer growth through inhibition of prostaglandin G/H synthase, also known as cyclooxygenase. We have now discovered that a subset of the compounds represented by A, in which --J--K--L-- is --NCHCH--, X is a bond, R are not both hydrogen show unexpectedly superior selectivity for the inhibition of COX-2 over COX-1 and/or superior potency as compared to the closest species disclosed in 96/10012.Optical Isomers--Diastereomers--Geometric Isomers Some of the compounds described herein contain one or more asymmetric centres and may thus give rise to diastereomers and optical isomers.The present invention is meant to comprehend such possible diastereomers as well as their racemic and resolved, enantiomerically pure forms and pharmaceutically acceptable salts thereof.