Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.

Abstract: There are disclosed novel avermectin compounds wherein the glycosyl side chain is substituted with, or replaced by an alkyl ester group in a Reformatsky reaction. The compounds are prepared by reacting an .alpha.-halogenated ester to a 4'-, 4"- or 13-keto-avermectin derivative in the presence of a reducing agent. The avermectin compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests.

Abstract: A matrix or monolithic drug delivery system for the controlled release of carbidopa and levodopa consists of the two drugs uniformly dispersed in a polymer vehicle at a concentration that is greater than the solubility of either drug in the polymer. Treatment of parkinsonism with the controlled release formulation provides several advantages over treatment with the standard carbidopa/levodopa combinations presently employed.

Abstract: Novel method of increasing litter size in monogastric domestic animals by administering an avermectin or milbemycin compound during mid-gestation.

Abstract: Certain substituted hexahydroarylquinolizines and pharmaceutically acceptable salts thereof are peripherally selective .alpha..sub.2 -adrenoceptor antagonists. The compounds are adapted to be employed for the treatment of certain pathological disorders such as hypertension, diabetes, disorders involving platelet aggregation and the like without side effects attributable to effect on the central nervous system.

Abstract: There are disclosed novel avermectin reduction products. The compounds are prepared by selective catalytic hydrogenation of avermectin-like compounds or by reaction of selected double bonds with electrophylic reagents. The reduced avermectin compounds have utility as anti-parasitic agents and compositions for that use are also disclosed. The compounds are also highly potent insecticides against agricultural pests. The reduced avermectin compounds have increased stability towards light which prolongs their insecticidal activities when applied to field crops subject to irradiation by sunlight.

Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.

Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.

Abstract: The muscle relaxant (E)-3-(9-chloro-5,6-dihydro-11H-pyrrolo[2,1-b][3]benzazepin-11-ylidene-N,N -dimethyl-1-propanamine is prepared by the geometric stereoselective dehydration of the intermediate carbinol with acidic agents and organic bases and low temperatures.

Abstract: Aromatic sulfonamides with a saturated heterocycle fused thereto are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: Heterocyclic aminoethanols of the formula:Het--CHOH--CH.sub.2 --NH-aralkylwhere Het is a 6-10 membered N-heterocycle are disclosed. The compounds are useful as pharmaceuticals.

Abstract: The compounds of the following structural formula (I) ##STR1## ar 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) synthase inhibitors and useful as antihypercholesterolemic agents for the treatment of disease in which the inhibition of cholesterol biosynthesis would be useful, such as arteriosclerosis, hyperlipidemia and familial hypercholesterolemia.

Abstract: Novel 5-amino or substituted amino 1,2,3-triazoles are disclosed as having anticoccidial activity. The compounds are useful for controlling coccidiosis when administered in minor quantities to animals, in particular to poultry, usually in admixture with animal sustenance.

Abstract: Pyrolysis of substituted salicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)benzamide. Similarly, substituted 6-azasalicylate O(N,N-dialkyl)thiocarbamates yielded the corresponding N,N-dialkyl-2-(methylthio)-6-aza-benzamide.

Abstract: An enantioselective synthesis of 1,3,4,6,7,12b(S)-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-one provides a key intermediate for the preparation of the .alpha..sub.2 -adrenergic antagonist (2R,12bS)-N-(1,3,4,6,7,12-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin-2-yl) -N-methyl-2-hydroxyethanesulfonamide hydrochloride, useful as an anti-depressant.

Abstract: The instant invention is directed to a drug delivery device for the controlled release of beneficial agents and drugs into an environment of use comprising:(A) a core composition comprising(a) a water insoluble, non-diffusible charged resin entity, and(b) a diffusible, water soluble ionizable therapeutically active ingredient carrying the same charge as said resin entity; and(B) a substantially imperforate water-insoluble wall surrounding said core composition, prepared from a semipermeable material substantially impermeable to the core composition and permeable to the passage of an external fluid in the environment of use, with said wall having a hole(s) for release of the therapeutic agent through the water insoluble wall.

Abstract: Alkane sulfonamides with an electron withdrawing function .beta. to the sulfonamide group are topically effective carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and glaucoma.

Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.

Abstract: Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.

Abstract: Novel fused polycyclic and bridged compounds are disclosed which are useful as calcium entry blockers.