Abstract: An improved cholesterol-lowering tablet is manufactured by blending tablet grade cholestyramine with an appropriate amount of lubricant and directly compressing into elongated tablets having a specified thickness. These inner tablets are successfully film coated using aqueous film-coating processes without tablet preheating and by simultaneous spray-drying.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of acyclic derivatives of imidazolone compounds of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of phenyl derivatives of imidazolone compounds of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: The crystalline, stable methanesulfonate salt of nefazodone showed significantly higher intrinsic dissolution in water and THAM buffer (pH 7.5) compared to other salts of nefazodone. The faster dissolution rate of this salt at neutral pH suggests better dissolution and absorption in the intestine, allowing controlled release of nefazodone for oral formulations.

Abstract: An improved method for orally administering buspirone to a human subject wherein the bioavailability of buspirone is increased and its elimination, metabolite formation, and variability of these pharmacokinetic parameters is decreased, the improvement comprises the concurrent administration of a sufficient amount of nefazodone to effect these pharmacokinetic changes for orally administered buspirone.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of cyanoguanidine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: Improved oral dosage formulations for acid-labile dideoxy purine nucleoside derivatives such as ddA, ddI, and ddG, have been developed by incorporating selected water-insoluble buffering systems in the formulation. These novel formulations provide reduced mass dosage units in the form of convenient, palatable chewable/dispersible tablets or a dry powder sachet. The reduced mass requirement, necessary to allow tablets of reasonable size, was achieved in part by an unexpected 20 to 25% increase in drug bioavailability resulting from use of the selected buffering systems comprised of an insoluble magnesium antacid agent and either dihydroxyaluminum sodium carbonate or calcium carbonate.

Abstract: A series of pyridinyl tri-substituted benzamide derivatives of general structure ##STR1## wherein the symbols R.sup.1, R.sup.2, X and n are described in detail in the specification, are useful as anticonvulsants agents.

Abstract: Nefazodone and its pharmaceutically acceptable salts are useful in prophylactic treatment of recurrent headache disorders, as, in particular, vascular and migraine headaches.

Abstract: Nefazodone and its pharmaceutically acceptable salts are useful in alleviation of post traumatic stress disorder.

Abstract: Certain indanyl piperidines are useful as melatonergic agents and can treat various CNS disorders. They are useful in treating sleep disorders and other conditions related to circadian rhythms.

Abstract: A series of 5-amino-6-cyclohexyl-4-hydroxy-hexanamide derivatives of Formula I have been synthesized. ##STR1## As inhibitors of the production of .beta.-amyloid protein from .beta.-amyloid precursor protein, these compounds are expected to be effective in treating patients suffering from or susceptible to conditions or disorders linked to brain accumulation of .beta.-amyloid protein; e.g., Alzheimer's Disease and Down's Syndrome.

Abstract: An economical process, amenable to large-scale production, is disclosed for the preparation of 2',3'-didehydro-3'-deoxythymidine (d4T) from 5-methyluridine. The process employs a novel, 5'-,acyl-2'.alpha.-halo-3'.alpha.-alkanesulfonylthymidine intermediate as well as a highly efficient and practical deprotection, isolation and purification procedure for the d4T product.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperidine and tetrahydropyridine derivatives of 4-phenyl-1,4-dihydropyridines of Formula I. ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of piperazine and homopiperazine derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: A series of novel 5-(3,4-diamino-1,2,5-thiadiazole and S-oxide) derivatives of indolylalkylpiperazinyl pyridines and pyrimidines of Formula I are intended for use in the alleviation of vascular headaches. ##STR1## In Formula I, X is selected from S, SO and SO.sub.2.

Abstract: Certain 3-amino-cycloalkanyl and cycloalkenyl derivatives of 5-cyano-substituted indoles of Formula I are useful antidepressant agents. ##STR1## The substituent R.sup.1 is hydrogen or C.sub.1-4 alkyl and R.sup.2 is C.sub.1-4 alkyl or --(CH.sub.2).sub.p --Ar with Ar being a phenyl, pyridinyl, pyrimidinyl or 1,4-benzodioxan-2-yl moiety. The symbol m is zero or 1, n is 1 to 3 and p is zero or 1 to 4.

Abstract: The present invention concerns an improved process of making d4T from 5-MU. Another aspect of the invention relates to useful intermediates produced during the process.

Abstract: A series of novel serotonergic indolyl derivatives of cycloalkanyl- and cycloalkenyl-amines of Formula I are intended for use in the alleviation of vascular headaches.

Abstract: A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of nitrogen heterocyclic derivatives of 4-phenyl-1,4-dihydropyridines of Formula (I). ##STR1## As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.