Abstract: The present invention provides methods, pharmaceutical compositions and kits for treating joint pain and/or improving sleep using a SERM of formula (I): 1

Abstract: Disclosed are methods of treating certain cytokine mediated diseases or conditions using novel aromatic heterocyclic compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein.

Abstract: The present invention provides an antiproliferative compound having the structural formula wherein X is oxygen, nitrogen or sulfur; Y is selected from the group consisting of oxygen, nitrogen and sulfur wherein when Y is oxygen or nitrogen, n is 1 and when Y is sulfur, n is 0. Also provided is a method for inducing apoptosis in a cell comprising administering a composition comprising a compound.

Abstract: The present invention provides methods for inducing apoptosis in a cell, the methods generally involving contacting the cell with an agent that reduces the level and/or activity of RabGGT. The present invention further provides methods for treating a disorder related to unwanted cell proliferation in an individual, the methods generally involving administering to the individual an agent that reduces the level and/or activity of RabGGT. The present invention further provides methods for reducing apoptosis in a cell, the methods generally involving increasing the level and/or activity of RabGGT in the cell. The present invention further provides methods for treating disorders associated with excessive apoptosis. The present invention further provides methods for identifying a cell that is amenable to treatment with the methods of the present invention. The present invention further provides methods for modulating a binding event between RabGGT and a RabGGT interacting protein.

Abstract: The invention relates to novel isoquinolines and their use as anticonvulsants and in the treatment of a variety of disorders.

Abstract: Compounds of formula (I) 1

Abstract: The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes for preparing compounds of Formula (I) or Formula (I(a)).

Abstract: Compounds of the formula I 1

Abstract: Disclosed are the preparation and pharmaceutical use of novel noncyclic 1,3-dicarbonyl compounds of formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Y, Z, Q, Ar and n are as defined in the specification. These compounds, as peroxisome proliferator-activated receptor (PPAR) dual agonists for both RXR/PPARgamma and RXR/PPARalpha heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders.

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

Abstract: Compounds of formula (I) 1

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: Acyl guanidine compounds of the following Formula 1

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

Abstract: The present invention relates to methods for the prevention or treatment of pain by the inhibition of p38 MAP kinase.

Abstract: Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.

Abstract: The present invention relates to an antipruritic agent comprising a nociceptin antagonist as an active ingredient. The nociceptin antagonist can be used as a preventive or remedy for diseases associated with itching (for example, atopic dermatitis and urticaria), local pruritus cutaneous caused by insect excretion and secretion, nodular prurigo, kidney dialysis, diabetes, blood disease, liver disease, kidney disease, incretion and metabolic disorder, viscera malignant tumor, hyperthyroidism, autoimmune disease, multiple sclerosis, neurologic disease, psychoneurosis, allergic conjunctivitis, spring catarrh, atopic keratoconjunctivitis, or itching caused by excess use of laxuries and drugs because it has excellent scrtaching behavior suppressing effect, that is, antiitching effect and antipruritic effect.

Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds 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 neurohormonal antagonists especially urotensin II antagonists.

Abstract: Amides of the general formula I 1

Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic, infectious and cell proliferative diseases or conditions are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism, infection and cell proliferation. The subject compounds contain a fused heterobicyclic ring.

Abstract: Cholesteryl ster transfer protein inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain oth r plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

Abstract: A selective chemotherapy method includes the step of contacting tumor cells with a mineral ascorbate/vitamin C metabolite composition. A chemotherapeutic composition comprises the mineral ascorbate/vitamin C metabolite composition in a pharmacologically acceptable intravenous carrier.

Abstract: The present invention relates to acylated, heteroaryl-condensed cycloalkenylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.

Abstract: The bioavailability of an ophthalmologically active compound is increased by its provision in a dosage of ophthalmic treatment liquid which takes the form of a jet or stream of droplets. Such a jet or stream can be directed or targeted at a particular site in the eye where the compound can be best absorbed.

Abstract: The present invention provides a compound of the formula: wherein ring A is an optionally substituted 5 to 10-membered aromatic ring; R1 and R2 are the same or different and each is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X is a bond and the like; and L is a divalent hydrocarbon group, and a salt thereof, except 3-(aminomethyl)-2,6,7-trimethyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-2-methyl-4-phenyl-1(2H)-isoquinolinone, 3-(aminomethyl)-6-chloro-2-methyl-4-phenyl-1(2H)-isoquinolinone and 3-(aminomethyl)-2-isopropyl-4-phenyl-1(2H)-isoquinolinone. The compound shows a superior peptidase-inhibitory activity and is useful as an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: The present invention provides novel pharmaceutically acceptable salts of the compounds of Formula (I) and Formula (Ia), as well as methods for using the pharmaceutically acceptable salts, and also provides processes for making compounds of Formula (I) and Formula (Ia), or the pharmaceutically acceptable salts thereof. Compounds of formula (I) and formula (Ia) are useful for the treatment of neurological disorders, especially migraine.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, &bgr;-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: A 3,4-dihydroisoquinoline derivative compound of formula (I) or a non-toxic salt thereof and a pharmaceutical agent comprising it as active ingredient (wherein all symbols have the same meaning as described in the specification). The compound of formula (I) has agonizing activity on CB2 receptor and therefore it is useful for the prophilaxis and/or treatment of various diseases such as asthma, nasal allergy, atopic dermatitis, autoimmune diseases, rheumatoid arthritis, immune dysfunction, postoperative pain, carcinomatous pain, etc.

Abstract: The invention discloses methods for the chronic administration of adenosine, which contrary to the acute delivery of the drug by injection or infusion, acts in desensitizing adenosine receptors towards the action of adenosine. The methods and oral compositions of adenosine triphosphate (ATP), which is degraded to adenosine in vivo, can be used in the treatment of disorders and diseases that are therapeutically targeted by agonists or antagonists of adenosine receptors. One example is the stimulation of lipolysis in achieving weight loss in humans and in the treatment of obesity.

Abstract: mGluR5 antagonists are used for the treatment and prevention of disorders, including Fragile X, autism, mental retardation, schizophrenia and Down's Syndrome. The methods of the invention can be used to treat epilepsy and anxiety in a human having Fragile X syndrome, autism, mental retardation, schizophrenia and Down's Syndrome.

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: The present invention provides compounds of Formula I or Formula II, or the pharmaceutically acceptable salts or prodrugs thereof, pharmaceutical compositions comprising compounds or Formula I or Formula II, and methods for treating neurological disorders and neurodegenerative diseases, particularly migraine.

Abstract: The present invention provides novel compounds of Formula (I), or the pharmaceutically acceptable salts or prodrugs thereof, and methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine.

Abstract: This invention relates to the use of chemical compounds showing non-competitive and selective GluR5 antagonist or partial agonist activity for treating diseases that are responsive to modulation of an aspartate or a glutamate receptor. Moreover the invention provides chemical compounds for use according to the invention, as well as pharmaceutical compositions comprising the chemical compounds, and methods of treating diseases or disorders or conditions responsive to modulation of an aspartate or a glutamate receptor.

Abstract: This invention relates to novel compounds represented by the general formula [I] 1

Abstract: A new method is described here for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroiso-quinoline-3-carboxamide comprising the following steps:

Abstract: The present invention relates to a composition useful for hepatoprotection, said composition comprising polar extract of plant Cryptolepis Buchanani and/or fractions of the said extract, and optionally pharmaceutically acceptable additives and a method of producing said composition and also a method of treating a subject using said composition.

Abstract: Compounds of formula (I), compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal).

Abstract: 1

Abstract: This invention is directed to compounds of the formula 1

Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to &bgr;-aminotetralin-derived ureas that are potent antagonists or agonists of VR1 which are useful for the treatment and prevention of inflammatory and other pain conditions in mammals.

Abstract: Compounds which are useful as potassium channel inhibitors and which because of their slow off-rates are especially useful for the treatment of cardiac arrhythmias are described.

Abstract: This invention is directed to novel (substituted)acyl dipeptidyl ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.

Abstract: This invention relates to a keratinocyte-proliferation inhibitor comprising as active ingredient a compound having an activity of inhibiting the solubilization of heparin-binding EGF-like growth factor bound to cell membranes and a compound of the formula (I); 1

Abstract: This invention relates to novel phenyl ureas useful in the treatment of disease states mediated by the chemokine, Interleukin-3 (IL-3)

Abstract: The present invention provides stable formulations of ACE inhibitors, especially enalapril maleate, that can be manufactured in a time efficient, cost effective manner. Such formulations can be prepared simply and on a large industrial scale. The present invention also provides methods for the preparation of stable formulations of ACE inhibitors, especially enalapril maleate.

Abstract: The invention is a pharmaceutical composition comprising a carboxyalkylether of the formula (I) wherein R1, R2, R3, and R4 include alkyl, alkenyl, and alkynyl, m and n are integers from 2 to 9, Y1 and Y2 include COOH, CHO, tetrazole, COOR5 where R5 is alkyl, alkenyl, or alkynyl, or a pharmaceutically acceptable salt therof, and an antihypertensive agent, said composition being useful for treating vascular diseases.

Abstract: The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.

Abstract: Ophthalmic compositions containing Lipoxin A4 and its analogs and methods of their use for treating dry eve are disclosed.

Abstract: Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.