Abstract: Hypocholesterolemic substituted 2-azetidinone compounds of the formula: are disclosed, as well as a methods of lowering cholesterol by administering said compounds, pharmaceutical compositions containing them, and the combination of a substituted 2-azetidinone cholesterol-lowering agent and a cholesterol biosynthesis inhibitor for the treatment and prevention of atherosclerosis.

Abstract: Compounds of formula I: ##STR1## wherein, ring C, A--B, R.sup.1, n, R.sup.2, and R.sup.3 have any of the meanings given in the specification, and their pharmaceutically acceptable salts are useful in the treatment of urinery incontinence. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.

Abstract: The invention concerns pharmaceutically useful compounds of the formula I, in which A.sup.1, A.sup.2, A.sup.3, A.sup.4, B.sup.1, m, Ar, W, X, Y, Z and R.sup.1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Abstract: A method for the systematic and efficient synthetic preparation and identification of metabolites of a pharmaceutical product in order to study possible toxic and/or otherwise biologically-active metabolites of such pharmaceutical products as early and conveniently as possible in the very expensive drug development process, comprising adding samples of the pharmaceutical product to a series of combinations of a synthetic metalloporphyrin (SMP) with a synthetic metalloporphyrin-co-oxidizing reagent in the presence of a suitable solvent, under specified conditions, in a manner such that each sample of pharmaceutical product is reacted with a different combination of synthetic metalloporphyrin, SMP-co-oxidizing reagent and solvent, followed by separation and isolation of the resulting oxidative products, then confirmation of the identity of metabolites from the pre-identified oxidative products by appropriate animal model studies, and subjecting the actual metabolites prepared in larger quantities by the above m

Abstract: The present invention relates to pyridazino?4,5-b!quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino?4,5-b!quinolines as active ingredient, and methods for the treatment of neurological disorders.

Abstract: Novel compounds useful in the preparation of enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, namely 5(S)-(3-methyl-5-isoxazolyl)-2-pyrrolidinone, 3-methyl-5-(1-methyl-2-pyrrolidinyl)-5-hydroxy-4,5-dihydro-isoxazole, and 1-(1-methyl-2(S)-pyrrolidinyl)-1,3-butanedione-3-oxime.

Abstract: Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.

Abstract: Selective and potent cholinergic ligands selective for neuronal nicotinic cholinergic channel receptors, which ligands have the formula: ##STR1## as well as pharmaceutically-acceptable salts or prodrugs thereof, which are useful in the treatment of dementias, attentional hyperactivity disorder, or substance abuse withdrawal characterized by decreased cholinergic function, one of which is also an analgesic agent, and one of which is an agent useful for treating anxiety associated with cognitive impairment.

Abstract: A novel process for preparing enantiomerically-pure 3-methyl-5-(1-(C.sub.1 -C.sub.3 -alkyl)-2-pyrrolidinyl)isoxazole in high yield, wherein a protected pyrrolidine or 2-oxo-pyrrolidine starting material is reacted with a suitable organic anion and a resulting beta-keto oxime intermediate is cyclized and dehydrated, as well as intermediates useful in the preparation thereof.

Abstract: Novel isoxazole isothiazole and pyrazole compounds of the formula: ##STR1## wherein A, R.sup.1, and R.sup.2 are specifically defined, or pharmaceutical salts thereof, are selective and potent cholinergic ligands at neuronal nicotinic receptors, useful in the treatment of cognitive, neurological and mental disorders characterized by decreased cholinergic function, as well as in the treatment of alcohol intoxication and petit real absence epilepsy.

Abstract: Compounds of the formula: ##STR1## useful as regulators of nitric oxide synthase that indirectly modulate cyclic guanosine monophosphate (cGMP), pharmaceutical compositions thereof, for treating disorders of vascular smooth muscles, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, sickle cell anemia and diabetes.

Abstract: 2-Nitroaryl or 2-cyanoaryl compounds of the formula ##STR1## pharmaceutical compositions thereof, intermediates useful in the preparation of these compounds, and methods for treating disorders of vascular smooth muscles or diseases of the cartilage, macrophages, neurons, platelets, bronchial smooth muscles, optic muscles and gastrointestinal smooth muscles, in addition to sickle cell anemia, diabetes, synovitis, chondroarthritis and osteoarthritis by employing these compounds.

Abstract: Analogs of CCK-tetrapeptides, which analogs have the formula ##STR1## wherein A, B, D, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are specifically defined, having activity as CCK antagonists, useful in the treatment or prevention of disorders of the gastrointestinal, central nervous, appetite regulating or pain regulating systems.

Abstract: Peptide analog type-B CCK receptor ligands or pharmaceutically-acceptable salts thereof, which are useful for treating central nervous system disorders, substance abuse, gastrointestinal disorders, endocrine disorders, eating-related disorders and for the treatment of shock, respiratory and cardiocirculatory insufficiencies.

Abstract: Selective and potent nicotinic agonists of the formula: ##STR1## including pharmaceutically-acceptable salts or prodrugs thereof, useful in the treatment of dementias, attentional hyperactivity disorder, anxiety associated with cognitive impairment, or substance abuse withdrawal characterized by decreased cholinergic function.

Abstract: Pharmaceutical compositions comprising a therapeutically effective amount of (+) 2-methylpiperidine and a pharmaceutically-acceptable carrier or diluent, as well as to a method of treating cognitive, neurological and mental disorders, which are characterized by decreased cholinergic function in humans and lower mammals, by administration of (+)2-methylpiperidine, optionally with a nicotinic agonist.

Abstract: Selective and potent Type-A CCK receptor agonists of formula (I):X--Y--Z--Q (I)or a pharmaceutically acceptable salt thereof, wherein,X is selected from ##STR1## Y is selected from ##STR2## Z is ##STR3## and Q is ##STR4## or pharmaceutically-acceptable salts thereof, useful in the treatment of gastrointestinal disorders (including gallbladder disorders), central nervous system disorders, insulin-related disorders and pain, as well as in appetite regulation.

Abstract: Compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein m is 0, 1 or 2 and n is 0 or 1;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is C.sub.1 -C.sub.6 -alkyl substituted with a heterocyclic group or C.sub.7 -C.sub.16 -arylalkyl, wherein the aryl group is unsubstituted or substituted with from one to three non-hydrogen members independently selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkyl, halo-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxy, amino and C.sub.1 -C.sub.6 -alkylamino;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, halogen, and halo-C.sub.1 -C.sub.6 -alkyl, or any two of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 taken together form a methylenedioxy group; andR.sup.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl.

Abstract: Aza-spirocyclic compounds of formula (I) ##STR1## which enhance cortical cholinergic neurotransmission.

Abstract: Compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein M is 0, 1 or 2 and n is 0 or 1;R.sup.1 is hydrogen or lower alkyl;R.sup.2 is C.sub.1 -C.sub.6 -alkyl substituted with a heterocyclic group or C.sub.7 -C.sub.16 -arylalkyl, wherein the aryl group is unsubstituted or substituted with from one to three non-hydrogen members independently selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkyl, halo-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, hydroxy, amino and C.sub.1 -C.sub.6 -alkylamino;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, halogen, and halo-C.sub.1 -C.sub.6 -alkyl, or any two of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 taken together form a methylenedioxy group; andR.sup.7 is hydrogen or C.sub.1 -C.sub.6 -alkyl.