Abstract: Muscarinic receptor antagonists of formula (I), and their pharmaceutically acceptable salts, wherein Y is --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O--, --(CH.sub.2).sub.2 O-- or --CH.sub.2 S--; R is --CH or --CONH.sub.2 ; and R.sup.1 is a group of formula (a), where R.sup.2 and R.sup.3 are each independently H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --(CH.sub.2).sub.n OH, halo, trifluoromethyl, cyano, --(CH.sub.2).sub.n NR.sup.4 R.sup.5, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), --CH(OH)(C.sub.1 -C.sub.4 alkyl), --C(OH)(C.sub.1 -C.sub.4 alkyl.sub.2, --SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n CONR.sup.6 R.sup.7 or --(CH.sub.2).sub.n COO(C.sub.1 -C.sub.4 alkyl); R.sup.4 is H or C.sub.1 -C.sub.4 alkyl; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkysulphonyl; R.sup.6 and R.sup.7 are each independently H or C.sub.1 -C.sub.4 alkyl; and n is 0, 1 or 2. The compounds are particularly useful in treating irritable bowel syndrome.

Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH.dbd.CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; and 2-(pyriolidino)alkanols pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.

Abstract: A process for preparing a compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, which comprises reacting a piperazine salt of the formula ##STR2## with an alkyl halide containing compound of the formula ##STR3## in water with a reagent to neutralize the hydrohalic acid and heating the mixture under conditions which are suitable to effect the coupling of said piperazine salt with said alkyl halide containing compound.

Abstract: A stable liquid oral prebrushing composition for loosening and removing plaque present on dental surfaces has a pH of about 7.2 to about 7.9 and comprises dialkali metal pyrophosphate salts, tetraalkali metal pyrophosphate salts or mixtures thereof, together with sodium lauryl sulfate in amounts effective for removal of plaque when the composition is applied to dental surfaces.

Abstract: The present invention relates to novel heterocyclic derivatives of the formulaAr--W--Hetwherein Ar, W and Het are as defined below, and related compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as regulators of the action of angiotensin II in mammals. The compounds of this invention are useful in the treatment and prevention of hypertension, glaucoma, renal disease, congestive heart failure, cognitive dysfunction, and other conditions in which the action of angiotensin II is implicated. This invention also relates to pharmaceutical compositions containing these compounds and to methods of inhibiting angiotensin II in mammals by administration of such compounds.

Abstract: A process for producing tertiary amine-sulphur trioxide complexes of the general formulaR.sub.3 N:SO.sub.3where R is a either methyl, ethyl, or propyl or the group R.sub.3 N is pyridyl comprising forming a reaction mixture of chlorosulfonic acid, pyridine or other tertiary amine R.sub.3 N, where R is previously defined and a chlorinated organic solvent. Gaseous ammonia is passed into the reaction mixture in order to recover amine from amine hydrochloride which is formed as a by-product of the reaction. Since the amine is more soluble in the chlorinated solvent than ammonium chloride that is co-produced, the reaction of the amine with chlorosulfonic acid to produce R.sub.3 N:SO.sub.3 is favored.

Abstract: The present invention relates to processes and intermediates for the preparation of spiro-heteroazolones. The latter compounds are useful as aldose reductase inhibitors.

Abstract: There are disclosed preparative processes and hypoglycemic compounds of the formula ##STR1## wherein R is hydrogen or C1 to C3 alkyl;R.sup.1 and R.sup.2 are taken together and are carbonyl; or R.sup.1 and R.sup.2 are taken separately, wherein R.sup.1 is hydrogen or R.sup.4 and R.sup.2 is--COR.sup.5 and COOR.sup.5 ;R.sup.3, R.sup.4 and R.sup.5 are each independently C1 to C9 alkyl, C3 to C7 cycloalkyl, phenyl, naphthyl, furyl, benzofuryl or thienyl or one of said groups mono- or disubstituted with C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 alkoxy-carbonyl, trifluoromethyl, fluoro or chloro; and n is 0 or 1; or pharmaceutically acceptable cationic salts thereof.

Abstract: Variously substituted 3,5-dihydroxy-6,8-nonadienoic acids and esters, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.

Abstract: The present invention relates to novel 3-amino-piperidine derivatives and related nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, Y and m are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. The invention also relates to novel intermediates used in the synthesis of compounds of the formula I.

Abstract: Certain 1H-indazole-3-acetic acid derivatives, and their pharmaceutically-acceptable esters and salts, are inhibitors of the aldose reductase enzyme, and so are useful in the treatment of diabetic complications.

Abstract: Hypoglycemic thiazolidine-2,4-dione derivatives of the formula ##STR1## wherein the dotted line represents a bond or no bond;V is --CH.dbd.CH--, --N.dbd.CH--, --CH.dbd.N--, S, O or NR;W is S, SO, SO.sub.2, SO.sub.2 NR.sup.1, NR.sup.1 SO.sub.2, CONR.sup.1 or NR.sup.1 CO;X is S, O, NR.sup.2, --CH.dbd.N-- or --N.dbd.CH;Y is CH or N;Z is hydrogen, (C.sub.1 -C.sub.7)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, phenyl, pyridyl, furyl, thienyl or phenyl mono- or disubstituted with the same or different groups which are (C.sub.1 -C.sub.3)alkyl, trifluoromethyl, (C.sub.1 -C.sub.3)alkoxy, fluoro, chloro or bromo;Z.sup.1 is hydrogen or (C.sub.1 -C.sub.3)alkyl;R, R.sup.1 and R.sup.2 are each independently hydrogen or (C.sub.1 -C.sub.4); andn is 1, 2 or 3;a pharmaceutically acceptable cationic salt thereof; or a pharmaceutically acceptable acid addition salt thereof when the compound contains a basic nitrogen.

Abstract: Intermediates and a stepwise process for the conversion of D-methionine or certain of its derivatives to optically active compounds of the formula ##STR1## wherein R is (C.sub.1 -C.sub.3)alkyl, phenyl or tolyl. The latter compounds are in turn useful as an intermediate in the preparation of penem antibiotic 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid and corresponding pharmaceutically acceptable salts and esters.

Abstract: Certain benzylphosphonic acid compounds, and their pharmaceutically-acceptable salts, are inhibitors of tyrosine kinase enzymes, and so are useful for the control of tyrosine kinase dependent diseases (e.g., cancer, atherosclerosis).

Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a transsubstituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.

Abstract: A series of imidazo[4,5-c]pyridines which inhibit platelet activating factor (PAF) and also block leukotriene D4 receptors are useful in treating asthma, arthritis, psoriasis, gastrointestinal distress, myocardial infarction, stroke and shock.

Abstract: Antibacterial compounds of the formula ##STR1## wherein n is 0 or 1, R is hydrogen or a radical forming an ester hydrolyzable under physiological conditions, and R.sup.1 is hydrogen or methyl; the pharmaceuticallyacceptable cationic salts thereof when R is hydrogen; pharmaceutical compositions thereof; a method of treating bacterial infections therewith; and intermediates useful in the synthesis of said compounds.

Abstract: Diastereomeric 5R,6S-6-(1R-hydroxyethyl)-2-(1S-oxo-3R-thiolanylthio)-2-penem-3-carboxylic acid and 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid, and pharmaceutically-acceptable salts and in vivo hydrolyzable esters thereof, useful as systemic antibacterial agents; and intermediates and processes which are useful in the said synthesis of said diastereoisomers.

Abstract: The monohydrate of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)ethyl)-6-chloro-1,3-dihydr o-2H-indole-2-one hydrochloride has advantageous stability for formulation as a neuroleptic agent.

Abstract: There is disclosed a low calorie fat substitute comprising a non-flowable aqueous phase and an oil phase, with the interaction between said aqueous and oil phases resulting in a pourable emulsion. Also disclosed are food compositions containing pourable and nonpourable emulsions.