Disclosed herein are certain imidazo[1,5-a]pyridines, and pharmaceutical compositions containing them as the active ingredient for treatment and promotion of healing of peptic ulcer disease by virtue of their antisecretory and cytoprotective properties.
Compounds of the formula ##STR1## wherein R.sub.1 represents cyano, nitro or C.sub.1 -C.sub.4 -alkyl or the 7,8-dihydro derivative thereof or the 5,6,7,8 tetrahydro derivative of the formula ##STR2## wherein R.sub.1 is as defined under formula Ia and R.sub.2 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen etherified or esterified hydroxy or mercapto, carboxy-C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkanoyl, to stereoisomers, mixtures of these stereoisomers and salts of these compounds are disclosed as well as their preparation, pharmaceutical compositions containing the same and the use thereof as inhibitors of aromatase activity.
Disclosed are e.g. novel 5-(carboxyalkyl)imidazo[1,5-a]pyridines, their derivatives and methods of synthesis. Said compounds are useful as selective thromboxane synthetase inhibitors for the treatment of diseases such as cerebral ischaemia, shock, thrombosis and ischaemic heart disease.
Aphthous ulcers and other lesions of the mucosal, submucosal, epidermal, dermal or subcutaneous tissue of the mouth are treated by a method comprising administering to a patient suffering from such lesion a topical preparation containing sucralfate as an essential ingredient. The invention is also drawn to a preparation comprising sucralfate as an essential ingredient, and a method for preparing the same. The sucralfate is combined with an appropriate pharmaceutical medium to form a homogenous mixture which can then be dispersed in other media to form a preparation useful for topical application to the lesion.
Disclosed are compounds of the formula I ##STR1## or a 5,6,7,8-tetrahydro derivative thereof, wherein R.sub.1 is hydrogen, halogen, lower alkyl, lower alkoxy, hydroxy, or aryl-lower alkoxy in which aryl represents phenyl or phenyl substituted by lower alkoxy, lower alkyl, halogen or trifluoromethyl; R.sub.2 represents hydrogen, halogen, or lower alkyl; C represents carboxy, lower alkoxycarbonyl, unsubstituted or mono- or di-(lower alkyl) substituted carbamoyl, cyano, formyl, hydroxymethyl, 5-tetrazolyl, dihydro-2-oxazolyl, dihydro-2-oxazolyl substituted by lower alkyl, or hydroxycarbamoyl; and (a) A represents ethenylene or ethenylene substituted by lower alkyl; B is straight chain or branched alkylene of 1 to 12 carbon atoms, alkynylene or alkenylene of 2 to 12 carbon atoms, phenylene-lower alkylene, phenylene-lower alkenylene, phenylene, or phenylene-(thio or oxy)-lower alkylene; or (b) A represents a direct bond; B represents lower alkylenephenylene, phenylene lower alkylene, phenylene, lower alkylene-(thio or oxy)-lower alkylene, lower alkylene-(thio or oxy)-phenylene, phenylene-(thio or oxy)-lower alkylene, phenylene-lower alkenylene, lower alkylenephenylene-lower alkenylene, or straight chain or branched alkadienylene of 5 to 12 carbon atoms; or a pharmaceutically acceptable salt thereof; and methods of synthesis thereof. Said compounds are useful as selective thromboxane synthetase inhibitors for the treatment of diseases such as cerebral ischaemia, shock, thrombosis and ischaemic heart disease.
