Abstract: The instant invention is improved gamma amino butyric acid analogs, processes for their preparation, and methods of using them as agents for treating epilepsy and other neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal damage, and inflammation.

Abstract: The present invention relates to 5-heterocyclo-pyrazoles of the formula I: wherein ring W, m, n, and R1 through R5 are as defined in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as arthritis, colon cancer, and Alzheimer's disease in mammals, preferably humans, dogs, cats and livestock animals.

Abstract: This invention relates to methods of preparing sodium-hydrogen exchanger type 1 (NHE-1) inhibitors of formula I′ and methods of preparing pharmaceutical compositions comprising such NHE-1 inhibitors.

Abstract: The present invention relates to compounds of the formula wherein R1, R2, R3, X, Y and the dashed line are defined as in the specification, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. These compounds are useful as psychotherapeutic agents.

Abstract: The present invention is directed to controlled-release (CR) oral pharmaceutical dosage forms of 5,8,14-triazatetracyclo[10.3.1.02,11.04,9]-hexadeca-2(11),3,5,7,9-pentaene, 1, and pharmaceutically acceptable salts thereof, and methods of using them to reduce nicotine addiction or aiding in the cessation or lessening of tobacco use while reducing nausea as an adverse effect. The present invention also relates to an immediate-release (IR) low dosage composition having a stable formulation with uniform drug distribution and potency.

Abstract: The present invention relates to compounds of the formula 1

Abstract: The present invention provides isolated polynucleotide molecules comprising nucleotide sequences encoding GRA1, GRA2, SAG1, MIC1 and MAG1 proteins from Neospora caninum, as well as recombinant vectors, transformed host cells, and recombinantly-expressed proteins. The present invention further provides a polynucleotide molecule comprising the nucleotide sequence of the bidirectional GRA1/MAG1 promoter of N. caninum. The present invention further provides genetic constructs based on the polynucleotide molecules of the present invention that are useful in preparing modified strains of Neospora cells for use in vaccines against neosporosis.

Abstract: The present invention provides a reproducible M. bovis challenge model and methods for reliably inducing and establishing a disease or disorder caused by infection with M. bovis by administering to an animal an effective amount of a M. bovis culture. The challenge culture of the present invention is administered in an amount sufficient to elicit M. bovis specific cellular or humoral immune responses. The M. bovis challenge model in accordance with the present invention can be used to evaluate the efficacy of potential vaccines.

Abstract: The present invention is directed to a polymorph of the citrate salt of 4-(3,4-dichlorophenyl)-2-[2-(4-methylpiperazin-1-yl)-benzylidene]-thiomorpholin-3-one: 1

Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R2 and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R2 and R3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8)n wherein n is an integer from 0 to 5. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts and solvates thereof, wherein R2 is —CH2NHSO2—A—R3, —CONR10—A1—R11, —X—NR12a—Y—NR13R14 or —CO—NR18—X1—NR12—Y—NR13R14; R19, where R19 is a C-linked, 5-membered aromatic heterocycle containing either (i) from 1 to 4 ring nitrogen atoms or (ii) 1 or 2 ring nitrogen atoms and 1 oxygen or 1 sulphur ring atom, said heterocycle being optionally substituted by C1-C6 alkyl, said C1-C6 alkyl being optionally substituted by phenyl, —OH, C1-C6 alkoxy or —NR20R21 and R1, A, R3, R10, R11, X, R12a, Y, R13, R14, R18, X1, R21 and R22 are as defined in the specification. The invention also relates to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds and the uses of such compounds as adenosine A2a receptor agonists.

Abstract: A process for the purification of 2-methoxy-5-trifluoro-methoxy benzaldehyde oil in which the oil is converted to amine by reaction of a nitroaniline with the oil; the imine is isolated as a solid; and the solid imine is converted back to the 2-methoxy-5-trifluoromethoxy benzaldehyde oil. The nitroaniline is selected from the group consisting of 3-nitroaniline, 3-methyl-2-nitroaniline, 4-methyl-2-nitroaniline, 2 methyl-3-nitroaniline and 4-methyl-3-nitroaniline.

Abstract: This invention provides a compound of the formula (I): 1

Abstract: Pharmaceutical compositions are disclosed for the treatment of obesity, an overweight condition and compulsive overeating. The pharmaceutical compositions are comprised of a therapeutically effective combination of a nicotine receptor partial agonist and an anti-obesity agent or weight loss facilitator or promoter and a pharmaceutically acceptable carrier. The method of using these compounds is also disclosed.

Abstract: The invention provides thiazolidinedione, oxadiazolidinedione, and triazolone compounds of Formula (I) which compounds are thyroid receptor ligands. The invention further provides pharmaceutical compositions and kits comprising such compounds and methods of treating obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer, diabetes, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesterolemia, depression, and osteoporosis using such compounds.

Abstract: The present invention provides methods and kits for improving or maintaining vascular health, including preventing myocardial infarction or stroke; maintaining or improving vascular reactivity; treating acute or chronic renal failure, peripheral arterial occlusive disease, coronary artery disease, or Raynaud's phenomenon; or lowering plasma levels of Lp(a) using an estrogen agonist/antagonist.

Abstract: Antibiotic compositions comprising an equilibrium mixture of azalide isomers, water, and one or more acids, and methods for preparing such compositions, are disclosed. The antibiotic compositions can be advantageously stabilized by adding one or more water-miscible co-solvents. In a preferred embodiment, the one or more co-solvents is propylene glycol.

Abstract: This invention relates to the identification of an orphan G-protein coupled receptor MRGX2 (and variants thereof) as a receptor of neuropeptides such as but not limited to cortistatin, somatostatin, Bam 13-22, &agr;-MSH, neuropeptide FF, dynorphin A and substance P, and the use of such neuropeptides (and structurally related molecules) as modulators for MRGX2. It also relates to screening methods to identify agonists and antagonists for this neuropeptide receptor.

Abstract: This invention relates to small molecules that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such small molecules in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds. The invention further relates to small molecules that are selective for erbB2 receptor over the erbB1 receptor, wherein said erbB2 inhibitor has a range of selectivities for erbB2 over erbB1 between 50-1500.

Abstract: The present invention relates to a transcription regulatory region of a myostatin gene. In particular, the invention relates to a 2.5 kb polynucleotide immediately 5′ to the myostatin coding sequence, its nucleotide sequence and methods of using this regulatory region, and fragments thereof. The present invention relates to the use of the myostatin promoter of the present invention to direct expression of a target gene in a tissue specific manner, i.e. muscle tissue. The present invention relates to the use of the myostatin promoter of the present invention in high throughput screens to identify test compounds which inhibit myostatin promoter activity or myostatin expression.