Abstract: The present invention is directed to a chemically stable pharmaceutical composition containing ibuprofen in combination with terfenadine, wherein the oxidation of terfenadine to terfenadone is prevented by the presence in the composition of an .alpha.-hydroxy carboxylic acid.

Abstract: This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

Abstract: This invention relates to compounds of the formula ##STR1## where R.sub.1 -R.sub.6, X and Y are as defined in the specification, which are useful for the treatment of various memory dysfunctions characterized by a cholinergic deficit and thus may be indicated in the treatment of Alzheimer's disease.

Abstract: The present invention relates to novel benzenesulfonylimine derivatives and their use as inhibitors of Interleukin-1 (IL-1) action. Such inhibitors are useful in the treatment of various disease states as disclosed herein including: rheumatoid arthritis, multiple sclerosis, diabetes mellitus, atherosclerosis, septic shock and pulmonary fibrosis.

Abstract: The present invention is directed to a new class of 3-amido and 3-sulfamido-indolyl NMDA antagonists and their use in the treatment of a number of disease states.

Abstract: The invention relates to sulfonamidocarbonylpyridine-2-carboxesteramides and their pyridine-N-oxides according to the formula I ##STR1## Said compounds are used as pharmaceuticals against fibrotic disorders, as fibrosuppressants and as inhibitors of proline hydroxylase.

Abstract: The present invention is directed to 5-HT.sub.2 antagonists and their use as agents in the treatment of obsessive-compulsive disorders (OCD). The invention is particularly directed to the compound (+)-.alpha.-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidine methanol which is a member of a class of 5-HT.sub.2 antagonists known as N-aralkyl piperidinemethanol derivatives which are potent and selective inhibitors of the binding of serotonin at the 5-HT.sub.2 receptor site.

Abstract: This invention is directed to pyridinyloxazole-2-ones which are useful in inhibiting metastasis in patients having cancer. The pyridinyloxazole-2-ones act to inhibit protein kinase C and thereby modulate metastasis in patients having cancer.

Abstract: The present invention is directed to a new class of 4-sulfanimide-quinoline derivatives and to their use as NMDA antagonists.

Abstract: This invention relates to 4- and 6-carbamates related to physostigmine of the formula ##STR1## where R.sub.1 is alkyl, cycloalkyl, bicycloalkyl, aryl or arylloweralkyl; R.sub.2 is hydrogen or alkyl or the group --NR.sub.1 R.sub.2 taken together forms a monocyclic or bicyclic ring of 5 to 12 carbons; m is 0, 1, or 2; each X is independently hydrogen, halogen, loweralkyl, nitro or amino; and the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and optical isomers and racemic mixtures thereof. This invention also relates to novel intermediates useful in the preparation of the 4- and 6-carbamates. The compounds of this invention display utility for alleviating various memory dysfunctions characterized by a decreased cholinergic function, such as Alzheimer's disease.

Abstract: The present invention is new 3-(heterocyclic)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-(heterocyclic)-propenoic acid derivatives are useful as NMDA antagonist.

Abstract: The present invention is new 3-(indol-3-yl)-propenoic acid derivatives and pharmaceutical compositions thereof. These new 3-indolyl-3-yl-prpopenoic acid derivatives are useful as NMDA antagonist.

Abstract: The present invention is directed to a new class of 3-amido and 3-sulfamido-indolyl NMDA antagonists and their use in the treatment of a number of disease states.

Abstract: The present invention is directed towards a process for producing a superior tasting pharmaceutical composition having porous granules produced through in situ gas generation using effervescence-producing ingredients. The method disclosed herein is especially suitable for producing superior tasting antacid tablets as well as superior tasting calcium supplements.

Abstract: The present invention is directed to a new class of 2-optionally substituted-4-piperazine-benzothiophene derivatives of the formula ##STR1## in which Y is represented by hydrogen or C.sub.1-3 alkyl; R is represented by a substituent selected from the group consisting of hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen, --CF.sub.3, --OCF.sub.3, and --OH; R.sub.1 is represented by hydrogen, cycloalkyl, C.sub.1-6 alkyl, phenyl optionally substituted, phenylalkyl, or phenylamidoalkyl; X is represented by hydrogen, --(CH.sub.2).sub.n X.sub.1, CH=CHX.sub.1 or CHX.sub.2 --(CH.sub.2).sub.q --CH.sub.3 ; n is an integer from 0-2; q is either the integer 0 or 1; X.sub.1 is represented by --OH--,--OR.sub.2, --NR.sub.2 R.sub.3, --CO.sub.2 R.sub.2, --CONR.sub.2 R.sub.3, --CN, or --COR.sub.2 ; R.sub.2 and R.sub.3 are each independently represented by hydrogen, C.sub.1-4 alkyl, phenyl optionally substituted, phenylalkyl, or R.sub.2 and R.sub.3 together form a (CH.sub.2).sub.m cycloalkyl, where m=2- 6; X.sub.2 is --OR.

Abstract: Novel 5-acyl-2-(1H)pyridinones and their use as cardiotonic agents. Typical of the compounds is 5-acetyl-1,2-dihydro-6-methyl-2-oxo-3-pyridinecarbonitrile which is prepared by condensing anionic cyano acetamide with 3-[(dimethylamino)methylenyl]-2,4-pentanedione in an inert organic solvent.

Abstract: The compound (R)-2-[(phenylisopropyl)amino]adenosine whose structure is given below: ##STR1## (R)-2-[(phenylisopropyl)amino]adenosine is about two orders of magnitude greater in its selectivity between the A-1 and A-2 adenosine receptors than its diastereoisomer. This compound is useful for lowering blood pressure.

Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.

Abstract: The present invention pertains to a process for producing a 2-imidazolone from a ureidoacetal. The ureidoacetal is subjected to an acid catalyzed condensation in order to produce the 2-imidazolone. The reaction is conducted in an alcoholic solvent in order to minimize the production of a polymeric by-product.

Abstract: Seizures are ameliorated with certain benzothiazepines.