Abstract: This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

Abstract: This invention provides indole and benzimidazole 15-lipoxygenase (15-LO) inhibitors of the formula where one of Y1 and Y2 is CH, N, or NH, and the other is R3 includes H, halo. HN2, COOH, alkyl; R4 includes halo, alkyl, and alkoxy; Z is C, CH, or NR5; R5 is H or oxycabonyl; and each X is independently H, alkyl, alkoxy, or halo.

Abstract: The present invention provides methods of modulating mammalian, particularly human, stem cell and progenitor cell differentiation to regulate and control the differentiation and maturation of these cells along specific cell and tissue lineages. The methods of the invention relate to the use of certain small organic molecules to modulate the differentiation of stem cell populations along specific cell and tissue lineages, particularly embryonic-like stem cells originating from a postpartum placenta or stem cells isolated form sources such as cord blood. The invention also relates to the treatment or prevention of myelodysplastic syndrome or myeloproliferative syndrome, or symptoms thereof, comprising administration of JNK or MKK inhibitors, alone or in combination, as well as with or without the use of unconditioned cells or cells conditioned in accordance with other aspects of the invention.

Abstract: The present invention is directed to a method of treating overweight and/or obesity and eating disorders such as binge-eating disorders, bulimia nervosa and anorexia nervosa. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of zonisamide (1,2-benzisoxazole-3-methanesulfonamide). The present method provides a sustained and significant weight loss in an overweight subject. The method can be used in conjunction with other therapeutic agents/methods commonly used to treat overweight and eating disorders thus enhancing the therapeutic effect of reducing weight and regulating eating disorders.

Abstract: The present application describes aryl sulfonyls of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein D, E, and M are defined below, are effective factor Xa inhibitors.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.

Abstract: Compounds of the formula inhibit the activity of endothelin. The symbols are defined as follows: R1, R2 and R3 are each independently (a) hydrogen, except that R1 is other than hydrogen; (b) alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, cycloalkylalkyl, cycloalkenyl, cycloalkenylalkyl, aryl, aryloxy, aralkyl or aralkoxy, any of which may be substituted with Z1, Z2 and Z3; (c) halo; (d) hydroxyl; (e) cyano; (f) nitro; (g) —C(O)H or —C(O)R6; (h) —CO2H or —CO2R6; (i) —SH, —S(O)nR6, —S(O)m—OH, —S(O)m—OR6, —O—S(O)m—R6, —O—S(O)mOH or —O—S(O)m—OR6; (j) —Z4—NR7R8; or (k) —Z4—N(R11)—Z5—NR9R10; and the remaining symbols are as defined in the specification.

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: from its corresponding 3-cyano-4-fluorophenyl-pyrazole and intermediates useful therein.

Abstract: 3-(4,5-Dihydroisoxazol-3-yl)-substituted benzoylcyclohexenone derivatives of the formula I in which the substituents A and R1 to R12 are as defined in the description and their agriculturally useful salts are described. The compounds have herbicidal action.

Abstract: Described are heterocycle-substituted cyclohexylamines of formula (I), and their pharmaceutically acceptable salts thereof. The compounds of formula (I) are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease.

Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereosomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.

Abstract: Provided herein are novel heteroaromatic substituted cyclopropanes of the Formula (I): 1

Abstract: This invention relates generally to tetracyclic tetrahydroquinoline compounds, and analogues thereof, and pharmaceutically acceptable salt forms thereof, which are selective inhibitors of serine protease enzymes, especially factor VIIa; pharmaceutical compositions containing the same; and methods of using the same as anticoagulant agents for modulation of the coagulation cascade.

Abstract: Methods and compositions are disclosed that provide acetylcholinesterase inhibitors for the prevention and treatment of diseases and disorders of the central nervous system, including dementia such as Alzheimer's disease, to the central nervous system via intranasal delivery. The methods and compositions of the present invention provide therapeutic concentrations of the acetylcholinesterase inhibitor in the cerebrospinal fluid of a mammal without the attendant disadvantages, risks and side effects of oral or injection delivery.

Abstract: The present invention relates to the process for the preparation of the compound of Formula I: 1

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1

Abstract: The invention relates to vitamin D derivatives of formula (I), processes for the production thereof and uses thereof: wherein Y1, Y2, R1-R6, Q and Z are as defined herein.

Abstract: The invention relates to a kit comprising a pharmaceutical composition containing repinotan or a physiologically acceptable salt of repinotan, and a means for the determination of the concentration of repinotan or its metabolites in body fluids, and also new pharmaceutical compositions containing repinotan or a physiologically acceptable salt of repinotan, and processes for their preparation.

Abstract: The invention provides non-steroidal ligands for the glucocorticoid receptor, methods for making non-steroidal ligands of the glucocorticoid receptor, compositions of non-steroidal ligands of the glucocorticoid receptor and methods of using non-steroidal ligands and compositions of non-steroidal ligands of the glucocorticoid receptor for treating or preventing diseases (e.g., obesity, diabetes, depression, neurodegeneration or an inflammatory disease) associated with glucocorticoid binding to the glucocorticoid receptor.

Abstract: This invention provides estrogen receptor modulators of formula 1, having the structure 1

Abstract: The invention provides compounds of formula (I) wherein n, A, R1, R2 and R3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: The present application describes N-[4-(1H-imidazol-1-yl)-2-fluorophenyl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides and derivatives thereof of, which are useful as inhibitors of factor Xa.

Abstract: The use of an activator or ligand of a peroxisome proliferator-activated receptor, other than PPAR&ggr;, or pharmaceutically acceptable derivative of said activator or ligand, in the manufacture of a medicament for the treatment or prophylaxis of bone disease allows, for the first time, bone anabolism to enhance the deposition of bone in conditions which would benefit from increased bone deposition. The reverse, where there is inhibition and/or retardation of bone deposition is also facilitated.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides bisarylamines, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety and motor neuron diseases) and as neuroprotective agents (e.g., to prevent stroke and the like) by opening potassium channels associated with the onset or recurrence of the indicated conditions.

Abstract: The invention is directed to inhibition of p38-a kinase using compounds of the formula 1

Abstract: 1 The invention relates to 3-(4,5-dihydroisoxazole-5-yl)benzoylpyrazole of the formula (I), wherein the variables have the following meanings: R1, R1 represent hydrogen, nitro, halogen, cyano, alkyl, halogenalkyl, alkoxy, halogenalkoxy, alkylthio, halogenalkylthio, alkylsulfinyl, halogenalkylsulfinyl, alkylsulfonyl or halogenalkylsulfonyl; hydrogen, R3 represents halogen or alkyl; R4 represents hydrogen or alkyl; R5, R6 represent hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl R3 or carbonyl, wherein the latter six groups can be substituted; R7 represents halogen, cyano, hydroxy, alkyl, halogenalkyl, alkoxy, halogenalkoxy, alkylthio, halogenalkylthio, alkylsulfinyl, halogenalkylsulfinyl, alkylsulfonyl, halogenalkylsulfonyl, amino, alkylamino, dialkylamino, dialkoxymethyl, hydroxyiminoalkyl, alkoxyiminoalkyl or optionally substituted carbonyl; R11 represents optionally substituted pyrazole that is bound in the 4 position and that carries a hydroxy group or a derivative the

Abstract: A class of aryloxyacetic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

Abstract: This invention provides compounds of Formula I having the structure 1

Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like.

Abstract: The invention provides compounds of the formula I 1

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: The present invention relates to compounds of formula 1, wherein R1, R2, R3 and R4 are defined as in the specification. These compounds are useful as psychotherapeutic agents.

Abstract: The present invention is directed to a method of treating headache, including migraine. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of zonisamide. The methods of the present invention are useful in relieving headache. The compounds of the present method can also be used in conjunction with other therapeutic agents commonly used to treat headache thus enhancing the therapeutic effect of reducing headache.

Abstract: Efficacious remedies for male sterility which are in the form of preparations containing as the active ingredient an adenosine A1 antagonist.

Abstract: Compounds of the formula: 1

Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.

Abstract: A method of treating neuropathic pain and its progression is disclosed comprising administering to a subject a compound of formula wherein R is hydrogen or a halogen atom, R2 and R3 are the same or different and are each hydrogen or a straight or branched alkyl having 1 to 3 carbon atoms, and one of X and Y is a carbon atom and another is a nitrogen atoms, provided that the methanesulfonamide group is bonded to the carbon atom of either X and Y, exemplified by zonisamide.

Abstract: A compound represented by the formula: wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; R2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.

Abstract: This invention is directed to physiologically active compounds of formula (I) 1

Abstract: Chemically stable pharmaceutical formulations comprising a therapeutically effective amount of a material of formula I are provided which formulations contain a stabilizer system comprising an organic carboxylic acid containing more than 1 carboxylic acid group and an antioxidant. The preferred organic carboxylic acid is citric acid and the preferred antioxidants are ascorbic acid and butylated hydroxytoluene, which antioxidants are preferred to be used in admixture. The chemically stable pharmaceutical formulations are particularly useful for treating Irritable Bowel Syndrome (IBS) in mammals and comprises administering to the mammal needing treatment an effective dose of the above chemically stable pharmaceutical formulation. The stabilizer system is also effective for use in other pharmaceutical formulations containing active ingredients having oxidizable groups such as amino, phenolic, hydryoxyl amino, aldehyde, unsaturated compounds, sulfoxide, sulfone and mercapto.

Abstract: This invention relates generally to nitrogen containing heterobicycles of formulas A and B: which are inhibitors of trypsin-like serine protease enzymes, especially factor Xa, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.

Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.

Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: The invention relates to substituted and unsubstituted 3H-benzo[1,2,3]oxathiazole 2,2-dioxides, 1,3-dihydrobenzo[1,2,5]thiadiazole 2,2-dioxides and 1,3-dihydro-benzo [c]isothiazole 2,2-dioxides, to their preparation and to their use in medicaments.

Abstract: A process is provided for preparing an oral fast-melt composition of a selective cyclooxygenase-2 inhibitory drug comprising (a) a step of wet granulating the selective cyclooxygenase-2 inhibitory drug together with a binding agent selected from gums, polypeptides, natural and modified starches, cellulosic materials, alginic acid and salts thereof, polyethylene glycol, polyvinylpyrrolidone, polymethacrylates, silicate salts and bentonites, and (b) a step of blending with the drug a saccharide of low moldability, wherein the above steps (a) and (b) occur in any order or simultaneously to result in formation of granules. Optionally the process further comprises (c) a step of blending the granules with at least one of a lubricant, a sweetening agent and a flavoring agent to form a tableting blend, and (d) a step of compressing the tableting blend to form oral fast-melt tablets. Also provided is a composition prepared by such a process.

Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

Abstract: This invention is directed to an amorphous 5-(4-aminosulfonyl-3-fluorophenyl)-4-cyclohexyl-2-methyloxazole compound, substantially free of crystals, methods for preparing the compound and pharmaceutical compositions containing the compound.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.