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: 2-Benzyl-4-(4-pyridyl)thiazoles and derivatives thereof have been made from converting a benzyl cyanide to the corresponding thioamide followed by condensation with a 4-bromoacetylpyridine. The thiazole derivatives are found to be effective immunoregulants.

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

Abstract: Thiophene-2-sulfonamides with a 5-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.

Abstract: N-substituted fused-heterocyclic carboxamide derivatives, for example, N-(2,2-diphenylethenyl)-3-hydroxythieno[3,2-b]thiophene-2-carboxamide can be prepared by ring closure between an appropriately substituted halo-thiophene ester, e.g., methyl 3-bromo-thiophene-2-carboxylate, and mercaptoacetamide followed by condensation with diphenylacetaldehyde. Alternatively, the ring closure can be carried out between an appropriately substituted mercaptothiophene ester, e.g., methyl 3-mercaptothiophene-2-carboxylate and a haloacetamide to afford the fused-heterocyclic intermediate, 3-hydroxythieno[3,2-b]thiophene-2-carboxamide. N-alkenylation of the intermediate will then lead to the final products.

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: Substituted 1-oxa-dethiacephalosporins are found to be effective elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

Abstract: A process for the preparation of (S)- or L-3-(3,4-dihydroxyphenyl)alanine (L-dopa) is described. The process utilizes water as reaction process solvent and proceeds via formation of an intermediate which can be kinetically resolved in a polar solvent to a precursor of the desired isomer and in which the undesired isomer can be efficiently racemized for reuse.

Abstract: 6-Hydroxy-2-(2-hydroxy-4-methoxyphenyl)benzofuran derivatives and related pharmaceutical compositions and methods of treatment are disclosed. The compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, they are useful therapuetic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.

Abstract: Phenylalkyl-2,3-dihydrobenzofurans and analogs were prepared by (1) nucleophilic substitution involving an appropriately substituted 2,3-dihydrobenzofuranol (or 2,3-dihydrobenzopyranol) and a cinnamylhalide followed by reduction; or (2) by Wittig reaction involving a halomethyl derivative of 2,3-dihydrobenzofuran (or 2,3-dihydrobenzopyran and an aryl or a heteroaryl aldehyde followed by reduction. These compounds were found to be potent anti-inflammatory agents.

Abstract: .beta.-Lactam derivatives and analogs are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.

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: 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: Medicarpin derivatives and related pharmaceutical compositions and methods of treatment are disclosed. The compounds are useful as inhibitors of mammalian leukotriene biosynthesis. As such, they are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation.

Abstract: Substituted 2,3,3a,6-tetrahydro-6-oxobenzofuran derivatives have been prepared. These neolignans are found to have potent and specific PAF (Platelet-Activating-Factor) antagonistic activities and thereby useful in the treatment of various diseases or disorders mediated by PAF, for example, pain, fever, inflammation, cardiovascular disorder, asthma, lung edema, allergic disorders, skin diseases, psoriasis, toxic shock syndrome and adult respiratory distress syndrome.

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: Tetrazolyl derivatives of .beta.-lactams are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.