Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.

Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

Abstract: Compounds having neutral endopeptidase (NEP) and/or human soluble endopeptidase (hSEP) inhibitory activity corresponding to the formula I, wherein the substituents R1, R2, R3 and R4 have the meanings given in the description and also pharmaceutical compositions containing these compounds, in particular pharmaceutical compositions suitable for treating or inhibiting cardiovascular diseases, sexual dysfunction and/or adverse conditions associated with apoptosis.

Abstract: The invention encompasses compounds as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.

Abstract: Methods are disclosed for treating hyperalgesia associated with irritable bowel syndrome comprising administering a direct and selective inhibitor of MLCK.

Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.

Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.

Abstract: Compounds of the formula I: where A, B, X, Y, Z, k, R1, R2 and R3 are those defined herein, and compositions comprising the same. The present invention also provides methods for preparing compounds of formula I and using the same in treating p38 mediated disorders in a patient.

Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.

Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.

Abstract: The invention concerns compounds of general formula (I) wherein: R1, R2, R3, R4, R5 and R6 are as defined in Claim 1. The compounds are useful in the treatment of pathologies related to the insulin-resistance syndrome.

Abstract: Novel methods for inhibiting angiogenesis and treating diseases associated with angiogenesis are described. The methods may comprise administering to a patient an effective amount of a 1,2-dithiol-3-thione derivative or metabolite thereof. Preferred compounds for use in the methods include 5-(2-pyrazinyl)-4methyl-1,2-dithiol-3-thione (Oltipraz) and its metabolites.

Abstract: The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I The present invention also provides methods for the use thereof to inhibit ?-secretase (BACE) and treat ?-amyloid deposits and neurofibrillary tangles.

Abstract: The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.

Abstract: Quinoline- and isoquinoline-based compounds exhibiting ATP-utilizing enzyme inhibitory activity, methods of using compounds exhibiting ATP-utilizing enzyme inhibitory activity, and compositions comprising compounds exhibiting ATP-utilizing enzyme inhibitory activity, are disclosed.

Abstract: Disclosed are novel quinoline compounds of formula (I), processes for their preparation, compositions containing them and their use in the treatment of CNS disorders.

Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.

Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.

Abstract: The present invention discloses compounds which, are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: The present application describes compounds according to both Formulas I and II, pharmaceutical compositions comprising at least one compound according to either Formula I or II and optionally one or more additional therapeutic agents, and methods of treatment using the compounds according to Formulas I and II both alone and in combination with one or more additional therapeutic agents. The compounds have the following general formulas: including all prodrugs, solvates, pharmaceutically acceptable salts and stereoisomers, wherein R1, R2, R3, R4 and R5 are described herein.

Abstract: Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA/NR2B antagonists useful for treating neurological conditions such as, for example, pain, Parkinson's disease, Alzheimer's disease, epilepsy, depression, anxiety, ischemic brain injury including stroke, and other conditions.

Abstract: Use of a compound of formula (I) wherein R1 is selected from alkyl, aryl, alkoxy, aryloxy, 0thioalkyl, thioaryl, CN, halo, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from N, O or S-containing heteroaryl groups, wherein the heteroaryl group is attached via an unsaturated carbon atom which is adjacent to one or two N, O or S-heteroatom(s), other than ortho, ortho-disubstituted heteroaryl groups; R3 is selected from H, alkyl, COR8, CONR9R10, CONR8NR9R10, CO2R11 and SO2R11; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an (NR5R6) group then R5 and R6 may be linked to form a heterocyclic ring; R7 is selected from alkyl and aryl; R8, R9 and R10 are independently selected from H, alkyl and aryl, or R9 and R10 may be linked to form a heterocyclic ring, or where R8, R9 and R10 are in a (CONR8NR9R10) group, R8 and R9 may be linked to form a heterocyclic group; and R11, is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or pro

Abstract: This invention provides quinazoline analogs of Formula I: where A is bonded to at least one of the carbons at the 5, 6, 7 or 8 position of the bicyclic ring, and the ring is substituted by up to two independent R3 groups. The invention also includes methods of using compounds of Formula I as type I receptor tyrosine kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract: The invention relates to novel sulfamic acid amides of General Formula (I) and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.

Abstract: The invention relates to therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3?, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).

Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.

Abstract: Compounds of Formula (I): inhibit the processing of APP by gamma-secretase, and hence are useful for treatment or prevention of Alzheimer's disease.

Abstract: Formula (I) compounds are described: (I) where the groups are as defined in the description here below, the racemic mixtures, their individual enantiomers, their individual diastereoisomers, their mixtures, and their pharmaceutically acceptable salts. Said compounds are topoisomerase I inhibitors.

Abstract: The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: In its many embodiments, the present invention provides a novel class of imidazo[1,2-a]pyridine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: Carbamate of general formula (I), wherein R1, R2, and R3 are H, OH, NO2, SH, CN, F, Cl, Br, I, COOH, CONH2, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylsulfanyl, (C1-C4)-alkylsulfinyl, (C1-C4)-alkylsulfonyl, (C1-C4)-alkoxyl optionally substituted with one or several F, and (C1-C4)-alkyl optionally substituted with one or several F or OH; R4 is cycloalkyl, phenyl, heteroaryl or a bicyclic ring system; R5 is cycloalkyl, (C5-C10)-alkyl, a substituted (C1-C10)-alkyl; and X? is a physiologically acceptable anion. Carbamate (I) is selective M3 receptor antagonists versus M2 receptor and may be used for the treatment of urinary incontinence (particularly, the one caused by overactive bladder), irritable bowel syndrome, and respiratory disorders (particularly, chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema, and rhinitis), as well as in ophthalmic interventions.

Abstract: Specific phenylalanine derivatives or pharmaceutically acceptable salts thereof have an antagonistic effect on the ? 4 integrins and, therefore, are usable as therapeutic agents or preventive agents for diseases in which ? 4 integrin-depending adhesion process participates in the pathology, such as inflammatory diseases, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract: Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy.

Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is C or N, and R1, R2, R2a, R2b, R2c, R3, Y, A, m, n, X2, X3 and X4 are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract: This invention relates to compounds which are represented by the general formula [I] [in which A stands for a group of the following formula [ao] or [b0] Ar1, Ar2 and Ar3 stand for optionally substituted phenyl; k stands for 0 or 1; m, n and s stand for 0, 1 or 2; R1 stands for hydrogen or optionally substituted lower alkyl; R2, R3, R4 and R5 either stand for hydrogen or optionally substituted lower alkyl, or R2 and R3, or R4 and R5 together stand for trimethylene and the like; R60 stands for hydrogen, alkyl, or the like; R61 and R71 either stand for alkyl and the like, or together stand for trimethylene and the like; X stands for carbonyl or methylene; Y stands for nitrogen or methine; and Q? stands for anion], and the like. The compounds of the invention exhibit selective antagonism to muscarinic M3 receptors, and therefore are useful as safe and effective agents showing little side effect, for treating diseases of the respiratory, urinary and digestive systems.

Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.

Abstract: The invention relates to the use of N-substituted indole-3-glyoxylamides of the general Formula I: and to pharmaceutical compositions having antitumor action.

Abstract: The present invention relates to alkyne compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1 and R2 have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one alkyne according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract: The present invention relates to polymorphs of the 3-pyrrole substituted 2-indolinone compound 5-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidenemethyl)-2,4-dimethyl-1H-pyrrole-3-carboxylic acid (2-pyrrolidin-1-yl-ethyl)-amide.

Abstract: The present invention is directed to novel spiro-benzo[C]chromene derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

Abstract: This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substituted derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.

Abstract: Endothelial nitric oxide production is enhanced by administration of arginine or lysine as a dietary supplement. Enhanced nitric oxide production from arginine supplementation improves vascular function and structure. Additional compounds may be administered with arginine or lysine to further enhance nitric oxide activity, including calcium, vitamin B6, vitamin B12, vitamin C, vitamin B, coenzyme Q, carotene, or glutathione.

Abstract: Oil-in-water emulsions comprised of: (a) a polyol poly-12-hydroxystearate polyester; (b) an alkyl polyglycoside; (c) an oil; and (d) from 5 to 30% by weight water. When used as paper additives, the emulsions significantly improve the softness and feel of the paper products.

Abstract: A recycled plastic material is made from laser-engraved thermoplastic, metal-containing thermoplastic, thermoplastic used in an inkjet apparatus, or thermoplastic to which an ink or its composition have stuck. This recycled plastic material is manufactured by pulverizing any of these thermoplastics, cleaning the pulverized thermoplastic, removing a cleaning solution from the cleaned thermoplastic to dry it, and removing the dried thermoplastic solid matter other than the thermoplastic.

Abstract: A method of manufacturing an improved clarity, low haze, low melt flow rate homopolymer polypropylene and thermoformed parts therefrom using an additive package such that the additive package alone provides the improved qualities, and process adjustments at the thermoforming stage are not required. The additive package does not contain a phosphite antioxidant, and the homopolymer polypropylene is either virgin material or virgin material mixed with at least 25 percent reground homopolymer polypropylene of the improved formulation described herein and combined with the improved clarity additive package.

Abstract: An electrically and ionically conductive porous material including a thermoplastic binder and one or more of anion exchange moieties or cation exchange moieties or mixtures thereof and/or one or more of a protein capture resin and an electrically conductive material. The thermoplastic binder immobilizes the moieties with respect to each other but does not substantially coat the moieties and forms the electrically conductive porous material. A wafer of the material and a method of making the material and wafer are disclosed.

Abstract: Compounds of formula (I) where: {R1 is methyl, ethyl, cycloalkyl or optionally substituted aryl; Z is arylene or a group of formula —(CHR4)n-, where R4 is hydrogen, hydroxy or alkyl, and n is a number from 0 to 6; Y is carbonyl or a —CH2— group; Q is a residue of a mono- or poly-hydroxyl compound having from I to 6 hydroxy groups; and x is a number from I to 6; and esters thereof} are useful as sensitizers for use in radiationcurable compositions.

Abstract: Polymer particles are irradiated with radiation from a high energy source to increase the water or other fluid absorbency of the particles. Products manufactured using the activated particles include protective undergarments, bandages, kitty litter, and spill clean up materials.