Abstract: 3-(6-Quinolylmethyl)-4H-imidazol-4-one derivatives corresponding to the formula (I): ##STR1## in which R.sub.1 represents an unbranched or branched (C.sub.2 -C.sub.5) alkyl group,R.sub.2 and R.sub.3 represent, each independently of one another, either a hydrogen atom, or an unbranched or branched (C.sub.1 -C.sub.5)alkyl group, or a (CH.sub.2).sub.n -aryl group where n=0 to 3, or R.sub.2 and R.sub.3 with the imidazole ring can form a spirocyclo(C.sub.3 -C.sub.8)alkyl group,as well as their addition salts with pharmaceutically acceptable acids and bases.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or (C.sub.1 -C.sub.6)alkyl; R.sup.2 is phenyl, pyridyl, thienyl or furyl, and R.sup.2 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo, and trifluoromethyl; R.sup.3 is phenyl, naphthyl, pyridyl, thienyl or furyl, and R.sup.3 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo and trifluoromethyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.
Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl or phenyl;R.sup.1 is hydrogen, lower alkyl, phenyl, halo, hydroxy, lower alkoxy or trifluoromethyl;R.sup.2 is phenyl, phenylloweralkyl, thienyl, furyl, pyrrolyl, pyridyl, benzothienyl, benzofuryl, indolyl, quinolinyl, or any of the foregoing substituted with halo, lower alkyl, lower alkylcarbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl;R.sup.3 is hydrogen, lower alkyl or phenyl; ##STR2## R.sup.
Type:
Grant
Filed:
August 28, 1992
Date of Patent:
January 25, 1994
Assignee:
American Home Products Corporation
Inventors:
Jerauld S. Skotnicki, Robert M. Kearney
Abstract: A plastic organic photochromic article, typically a lens such as an ophthalmic lens or a window such as a vehicle roof light, comprisig a plastics host material having a photochromic compound incorporated therein or applied thereto, the article exhibiting the following properties, measured at Air Mass 2 at 25.degree. C.:(a) an integrated visible transmission in the faded state (B.IVT) ranging from 90 to 25%,(b) an integrated visible transmission in the darkened state (D.IVT) ranging from 1 to 50%, preferably 4 to 30%,(c) the rate of darkening of the article when it is exposed to actinic radiation is such that 88% of the darkening range is achieved in 30 seconds or less, i.e. T.sub.88 .ltoreq.30 secs,(d) the rate of fading of the article from its fully darkened condition is such that more than 60% of the optical density range is recovered in 60 seconds, i.e. % ODG-1.gtoreq.60%, and(e) the induced optical density of the article, i.e.