Abstract: Novel cyclized N-substituted tetrahydropyridine compounds are disclosed. The compounds have the property of inhibiting calcium induced contraction of the smooth muscle and are adaptable to being employed in the chemotherapeutic treatment of cardiovascular diseases.

Abstract: A process for the preparation of 1,4-dihydropyridine compounds, especially N-substituted 1,4-dihydropyridine compounds, is disclosed. The compounds are useful as cardiovascular agents and also as starting materials for the preparation of certain cyclized compounds which have properties as calcium entry blockers.

Abstract: Topical ocular administration of a dopamine agonist is effective in lowering abnormally elevated intraocular pressure and is useful in the prevention and treatment of glaucoma and related ocular diseases.

Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) or (II): ##STR1## and pharmaceutically acceptable salts thereof the compounds of the formula (II) in which R is hydrogen are disclosed.

Abstract: There is disclosed an overcap for a container with a primary cap for the removal of the contents thereof, whereby the overcap is easily assembled onto the container and completely surrounds the primary cap. When assembled, the overcap prevents access to the primary cap, and when removed, the overcap becomes irreversibly deformed such that visual evidence is clearly apparent that access to the primary cap has been gained. The irreversible deformity consists of tabs connecting the pull-tab to the overcap, and weakened areas in the side of the overcap which must be torn to allow removal of the primary cap.

Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.

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

Abstract: There is disclosed a substituted nitroimidazole compound, 1-methyl-2-methylsulfonyl-4-nitroimidazole which is an antiprotozoal and bactericidal compound with the unique and surprising property of being totally non-mutagenic and thus of a much higher degree of safety than is found with other nitroimidazoles. Compositions and methods for the antiprotozoal and bactericidal uses of such compounds are also disclosed.

Abstract: Labile quaternary ammonium salts of the following formula (I) and (II) are provided: ##STR1## wherein N represents a tertiary aliphatic amine; wherein N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C.sub.1 -C.sub.8 open chain or cyclo alkyl group, a C.sub.1 -C.sub.8 alkoxyalkyl group, a C.sub.1 -C.sub.8 acyloxyalkyl group, a C.sub.1 -C.sub.8 haloalkyl group, a C.sub.1 -C.sub.8 carboxyalkyl group, a C.sub.2 -C.sub.8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C.sub.1 -C.sub.4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R.sub.1 which may be the same or different, represents any member defined by R above with the proviso that R.sub.

Abstract: There is provided a novel drug delivery system which provides for intermittent drug delivery with readily adjustable intervals between drug delivery pulses. This is accomplished by providing a multilayer device in which layers of active drug are readily expandable or erodable when contacted with the environment in which the drug is to be administered. The drug layer is alternated with an inert layer and a multiplicity of such layers are contained within a tube impervious to such environment but provided with an opening into such environment. The multiplicity of such layers is driven along the length of such tube towards the opening. The interval between pulses is determined by the rate the layers are driven along the tube and the sizes of the layers. The duration of the pulse is determined by the rate of expansion or dispersion of the active layer into the environment, wherein the rate of expansion or dispersion is greater than the rate the layers are driven along the tube.

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: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents are represented by the following structural formulae (I) and (II): ##STR1## are disclosed.

Abstract: A glycoprotein phosphotyrosyl protein phosphatase is isolated from human tissues, such as human placental membrane. Upon membrane solubilization and extraction of the enzyme it was subjected to chromatographic purification and isolation. The analytical and biological responses of the enzyme demonstrate that it is novel and readily distinguished from other enzymes previously isolated from similar tissues. The enzyme is a dephosphorylation enzyme of membrane phosphoprotein kinases, and as such has utility as an antidiabetic agent, an antiatherosclerosis agent or an antitumor agent since certain membrane receptor kinases involved in each such biological function involve a phosphorylation mechanism for cell transformation, metabolism and growth and which, when blocked by the instant enzyme, results in a suppression or alteration of the biological function.

Abstract: There is disclosed a series of novel cyclic tetrapeptides related to somatostatin. The compounds have surprisingly been found to have the activity of increasing blood glucose when administered. The compounds are prepared using the solid phase or mixed anhydride synthesis methods and compositions and methods utilizing the novel compounds are also disclosed.

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

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

Abstract: Prodrugs of 3-hydroxy-3-methylglutarylcoenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formula (I): ##STR1## the amido ester moiety of which is in the L-configuration, and pharmaceutically acceptable salts thereof are disclosed.

Abstract: A group of 4-substituted-5-nitroimidazoles is described, having effective antiprotozoal activity with much less mutagenicity than is shown by known 5-nitroimidazoles.

Abstract: There are disclosed novel formulations of avermectin compounds and a substrate which demonstrate markedly enhanced insecticidal activity over that which would be observed with other formulations. Avermectin natural product compounds and certain semisynthetic derivatives thereof are compounds known to be highly effective broad-spectrum antiparasitic and pesticidal agents. However, when such compounds are formulated into the instant composition, the activity observed is increased to at least 10-times that which would be expected. The instant substrate is preferably a highly dispersed, amorphous form of hydrophyllic silicon dioxide.

Abstract: Certain novel cyclic ureas are disclosed herein as dermal penetration enhancers of drug absorption. Also disclosed herein are compositions, methods of treatment and processes for preparing said cyclic urea compounds.