Abstract: The present invention relates to a novel process for preparing 1-halo-3-trialkylsilanyl-benzenes from 1,3-dihalo-benzenes which are useful intermediates in the preparation of 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones which are useful for the treatment of Alzheimer's disease and senile dementia.

Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.

Abstract: This invention relates to novel carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.

Abstract: 2,4,5-Tri(4-methoxyphenyl)-4,5-dihydroimidazole, or a pharmaceutically acceptable salt thereof, is employed as a cancer drug potentiator or as an antimetastis drug.

Abstract: 1,3-Substituted-8-(oxo-substituted cycloalkyl)xanthines and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds include the cis and trans isomers of 1,3-dipropyl-8-(3-hydroxycyclopentyl)xanthine and the cis and trans isomers of 1,3-dipropyl-8-(4-hydroxycyclohexyl)xanthine. The compounds are potent and selective bronchodilators and/or cardiotonic agents.

Abstract: A group of four stereoisomers and their pharmaceutically acceptable salts are disclosed. The stereoisomers have formula I. ##STR1## In Formula I the asymmetric centers a and b may be the same or different and have either the absolute R or S configuration. Also disclosed are pharmaceutical compositions containing the stereoisomers and use of the stereoisomers as antihypertensive agents, as peripheral and cerebral vasodilators and as coronary therapeutic agents.The preferred compound is (R,R)-1-azabicyclo[2.2.2]oct-3-yl methyl 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylate.

Abstract: Dihydrofuranone compounds having anticholinergic activity are described. The compounds have the formula: ##STR1## wherein: R.sub.1 is hydrogen or lower alkyl,R.sub.2 is hydrogen or lower alkyl,R.sub.3 is hydrogen or lower alkyl, andPh is phenyl.Also described are the lower alkyl quaternary and acid addition salts of the compounds. Pharmaceutical compositions effective as anticholinergics and methods utilizing such compounds are disclosed.

Abstract: Furanone compounds and compositions having anticholinergic activity are described. The compounds have the formula: ##STR1## wherein: the dashed line indicates either the 4,5-unsaturated or the 4,5-dihydrofuranone ring;R.sub.1 and R.sub.2 may be the same or different and are hydrogen, thienyl, furanyl, or cycloalkyl (C.sub.3 -C.sub.6), benzyl, phenyl, substituted phenyl or substituted benzyl wherein the phenyl or benzyl group may be substituted with halogen, trifluoromethyl, lower alkyl, lower alkoxy or hydroxy;R.sub.3, R.sub.4 and R.sub.5 may be the same or different and are hydrogen, lower alkyl, lower alkyl substituted with a halogen, alkoxy, amino or carboxylic acid group, an alkyl or alkylene bridge between R.sub.4 and R.sub.5 or R.sub.3 and the ring N, trifluoromethyl, nitro, a cycloalkyl group containing 3 to 6 carbons, halogen, benzyl, phenyl, substituted phenyl or substituted benzyl, for which the substituents are the same as those set forth for R.sub.1 and R.sub.2 substituted benzyl or phenyl.R.sub.

Abstract: 1-Phenyl-7-substituted-hept-5-yn-2-ones substituted with a C.sub.1 to C.sub.7 alkyl, C.sub.3 to C.sub.6 cycloalkyl, aryl, heteroaryl or heterocycloalkyl group at the 1-position and an amino, a dialkylamino, a piperidyl, a pyrrolidyl or a hexahydroazepinyl group at the 7-position are disclosed which may have one or two substituents in addition to the phenyl group at the 1-position and also may have a p-fluoro substituent on the phenyl group. The preferred compounds are, 1-cyclohexyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one, 1-cyclobutyl-1-phenyl-1-hydroxy-7-dimethylaminohept-5-yn-2-one and 1-cyclo-1-phenyl-1-hydroxy-7-ethylaminohept-5-yn-2-one.The compounds are highly specific M.sub.1 -AChR antagonists with relatively prolonged duration of activity.

Abstract: 1,3-Alkyl substituted-8-phenylxanthines in which the straight chain alkyl substituents are different and pharmaceutically acceptable salts of such compounds are disclosed. Preferred compounds have 1-n-propyl-3-methyl and 1-methyl-3-n-propyl substituents. The compounds are potent bronchodilators.

Abstract: A solid medicament dispensing device having a cover and tray to provide a container for a cartridge for the solid medicament. The cover has hinged panel members and the tray an opening in the floor. When the hinged panel members are moved against the cartridge, it forces the medicament out of the cartridge and through the tray opening. The dispensing device is particularly suited for dispensing large dosages of capsules.

Abstract: A method for treating angina, epilepsy and hypertension by achieving vasodilation, anti-angina or anti-convulsant effect in a patient is described. The method involves transdermally administering to a patient in need of vasodilation or anti-convulsant effect the compound known as (+)(2S,3S)-acetoxy-8-chloro-5-(2-dimethylaminoethyl)-2,3-dihydro-2-(4-meth oxyphenyl)-1,5-benzothiazepin-4-(5H)-one in an amount sufficient to achieve desired systemic vasodilation, anti-angina or anti-convulsant levels of the compound.