Abstract: Compounds of the formula ##STR1## wherein: pounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.
Abstract: The invention relates to novel N-alkylnorscopines wherein the alkyl group may have 2 to 10 carbon atoms, which are useful in the preparation of valuable pharmaceutical compositions. These compounds may be prepared from the corresponding N-alkylnorscopolamines by hydrogenolysis with complex hydrides, which reaction is preferably carried out with sodium borohydride in ethanol at ambient temperature.
Abstract: The invention herein relates to novel quaternary 6,11-dihydro-dibenzo-[b,e]-thiepine-11-N-alkylnorscopine ethers, the preparation thereof, and their use as spasmolytics or bronchospasmolytics.
Abstract: The invention relates to new products, namely endo-8,8-dialkyl-8-azoniabicyclo [3.2.1] octane-6,7-exo-epoxy-3-alkylcarboxylates, of formula: ##STR1## in which R.sub.1 and R.sub.2, which can be the same or different, are linear or branched alkyl radicals of 1-5 C atoms or cycloalkyl radicals of 3-6 C atoms;R.sub.3 and R.sub.4, which can be the same or different, are alkyl radicals of 1-6 C atoms;X.sup.- is a halide ion.The new compounds are powerful spasmolytics.
Abstract: 3.alpha.-Benzoylamino-2.beta.-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding 2.beta.,3.beta.-epoxy-nortropane with benzylamine in the presence of phenol.
Abstract: 3.alpha.-Benzylamino-2.beta.-hydroxy-nortropanes substituted in the 8-position by an alkoxycarbonyl or alkanoyl group, useful as analgesics, are prepared by reacting the corresponding 2.beta.,3.beta.-epoxy-nortropane with enzylamine in the presence of phenol.
Abstract: N-substituted-14-hydroxy-3-substituted-morphinan derivatives have been found to possess potent narcotic agonist or antagonist activity. In particular, the compound N-Cyclobutylmethyl-3,14-dihydroxymorpinan has been found to posess potent agonist/antagonist activity as a non-narcotic analgesic. An improved total snythesis of these compounds is described herein from the starting material 2-(p-methoxybenzyl)-1,2,3,4,5,6,7,8-octahydroisoquinoline. A preferred feature of the process involves borane reduction of 2-cyclobutylcarbonyl-9,10-dihydroxy-1-(p-methoxybenzyl)perhydroisoquinolin e (Va) to provide the corresponding cyclobutylmethyl derivative complexed with borane which is converted directly to N-cyclobutylmethyl-14.beta.-hydroxy-3-methoxymorphinan (LVa) by treating with acid.
Abstract: [2]Benzopyrano[3,4-c]pyridine derivatives characterized by having a 2,3,4,4a,6,10b-hexahydro-1H-[2]benzopyrano[3,4-c]pyridine nucleus bearing a substituent at position 6 are disclosed. The nucleus can be optionally further substituted at positions 2,3,4,6 and on the aromatic ring. The derivatives are useful diuretic, anorexic, antidepressant, anticonvulsant and antihypertensive agents. Methods for their preparation and use also are disclosed.
Type:
Grant
Filed:
December 20, 1976
Date of Patent:
January 2, 1979
Assignee:
Ayerst, McKenna and Harrison, Ltd.
Inventors:
Jean A. Gauthier, Leslie G. Humber, Clara Revesz