Abstract: A pharmaceutical tablet comprising modafinil particles, wherein more than 5% of the modafinil particles have a diameter of more than 200 microns, less than 5% of the modafinil particles have a diameter of more than 800 microns, and the tablet has a disintegration time of less than 20 minutes.

Abstract: The invention relates to processes for preparing, and pharmaceutical compositions of, modafinil dosage forms for oral administration. The dosage forms include a mixture of coarse and fine particles of modafinil. The process for preparing modafinil oral dosage forms includes forming a dosage form that includes about 7%-25% by weight of modafinil particles having diameters greater than 220 &mgr;m and about 75%-93% by weight of modafinil particles having diameters less than 220 &mgr;m.

Abstract: In one aspect, the present invention provides a method of inhibiting an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with an amount of an Edg-3 receptor inhibitor sufficient to inhibit the Edg-3 receptor mediated biological activity. Preferably, the inhibitor is not a phospholipid.

Abstract: The present invention relates to a novel class of androgen receptor targeting agents (ARTA), which contain a haloacetamide or azide moiety and are alkylating agents.

Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.

Abstract: This invention is directed generally to heteroarylsulfonylmethyl hydroxamic acids and amides that, inter alia, tend to inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to compositions of such compounds; intermediates for the syntheses of such compounds; methods for making such compounds; and methods for treating conditions associated with MMP, tumor necrosis factors (or “TNFs”), and/or aggrecanase activity, particularly pathological conditions.

Abstract: Compositions and methods for improving recovery following general anesthesia are provided. The composition comprises an effective dose of modafinil. Modafinil has been shown to reduce the symptoms associated with post-operative general anesthesia, improving the recovery form anesthesia.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: The use of 3-benzolphenylacetic acids and derivatives, including nepafenac, to treat neurodegenerative retinal disorders is disclosed.

Abstract: The present invention is directed to benzophenone compounds useful in the inhibition of HIV reverse transcriptase, particularly its resistant varieties.

Abstract: Compositions of modafinil and methods of treating neurologically related conditions with the administration of modafinil. Also compositions that include modafinil and one or more excipients such as diluents, disintegrants, binders and lubricants.

Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.

Abstract: The present invention relates to novel cinnamide compounds that are useful for treating inflammatory and immune diseases and cerebral vasospasm, to pharmaceutical compositions containing these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.

Abstract: The invention provides an oral pharmaceutical composition comprising modafinil particles, wherein at least about 5% of said modafinil particles have a diameter greater than 200 &mgr;.

Abstract: Modafinil polymorphic forms of modafinil racemate, methods of preparation thereof, pharmaceutical compositions and methods of therapeutic treatment involving modafinil polymorphic forms.

Abstract: Inhibitors of the cellular sodium/hydrogen exchangers show an inhibiting effect on the secretion of von-Willebrand factor and/or increased expression of P-selectin. These inhibitors can therefore be employed for the treatment of thrombotic and inflammatory disorders.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII): useful in treating Alzheimer's disease and other similar diseases.

Abstract: Novel sulphones of Formula I are disclosed. The novel compounds modulate the action of gamma secretase, and hence find use in the treatment or prevention of Alzheimer's disease.

Abstract: The invention describes novel nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one nitrosated and/or nitrosylated cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent.

Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.

Abstract: The present invention provides for methods of treating and preventing cardiac hypertrophy. Class II HDACs, which are known to participate in regulation of chromatin structure and gene expression, have been shown to have beneficial effects on cardiac hypertrophy. Surprisingly, the present invention demonstrates that HDAC inhibitors inhibit cardiac hypertrophy by inhibiting fetal cardiac gene expression and interfering with sarcomeric organization.

Abstract: PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other 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 mammals, including humans.

Abstract: This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: A cancer remedy comprising a compound represented by the following formula as an active ingredient: 1

Abstract: The present invention is related to compositions of modafinil, including compositions of modafinil and one or more diluents, disintegrants, binders and lubricants, and the processes for their preparation thereof.

Abstract: Pentafluorosulfanylbenzoylguanidines of the formula I and II 1

Abstract: The topical use of certain flurbiprofen amide derivatives and ketorolac amide derivatives to treat ophthalmic angiogenesis-related and inflammatory disorders of the posterior segment of the eye is disclosed.

Abstract: Novel compounds of the general formula: and pharmaceutically acceptable acid addition salts thereof, wherein the compounds are useful in therapy to protect skeletal muscles against damage resulting from trauma or to protect skeletal muscles subsequent to muscle or systemic diseases such as intermittent claudication, to treat shock conditions, to preserve donor tissue and organs used in transplants, in the treatment of cardiovascular diseases including atrial and ventricular arrhythmias, Prinzmetal's (variant) angina, stable angina, and exercise induced angina, congestive heart disease, and myocardial infarction.

Abstract: The use of 3-benzolphenylacetic acids and derivatives, including nepafenac, to treat neurodegenerative retinal disorders is disclosed.

Abstract: The present invention relates to a method for detecting an agent for use in the treatment of herpes virus infection and use of known agents, such as 2,2′-dithiobisbenzamide (DIBA) and azodicarbonamide (ADA), and unknown agents, which selectively eject zinc bound to a zinc finger protein, for the manufacture of a medicament for the treatment of herpesvirus infections.

Abstract: The present invention provides a prophylactic and therapeutic medicament for ophthalmic diseases, especially ophthalmic inflammatory diseases and corneal ulcer, comprising as an active ingredient a compound represented by the formula (I): or a pharmacologically acceptable salt or hydrate thereof.

Abstract: Systemic delivery of Modafinil to the nasal mucous membrane elicits rapid systemic therapeutic response with reduced side effects compared to current methods of administration.

Abstract: The present invention provides an AP-1 activation inhibitor, NF-kappa B activation inhibitor, inflammatory cytokine production inhibitor, matrix metalloprotease production inhibitor, inflammatory cell adhesion molecule expression inhibitor, anti-inflammatory agent, antirheumatic agent, immunosuppressant, cancer metastasis inhibitor, remedy for arteriosclerosis and antiviral agent which contain the benzene derivative of the following general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: The present invention is directed to a pharmaceutical composition containing a cancer-treating effective amount of a class of prostacyclin derivatives, and a pharmaceutically acceptable carrier, and to kits and methods of employing the same for the treatment of cancer.

Abstract: Compounds of the invention are useful in inhibiting thrombin and treating blood coagulation and cardiovascular disorders and have the following structure: wherein R3 is hydrogen or halogen, and u is N or CH.

Abstract: This invention is directed to a pharmaceutical composition comprising the sodium-hydrogen exchanger (NHE) inhibitor cariporide and an angiotensin converting enzyme (ACE) inhibitor which exhibits unexpectedly efficacious properties for preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life, and to methods of preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life comprising administering pharmaceutically effective amounts of the sodium-hydrogen exchange inhibitor cariporide and an ACE inhibitor.

Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.

Abstract: The use of compounds of the formula 1

Abstract: This invention relates to the inhibition of histone deacetylase (HDAC) expression and enzymatic activity. The invention provides methods and reagents for inhibiting HDAC-4 and HDAC-1 by inhibiting expression at the nucleic acid level or inhibiting enzymatic activity at the protein level.

Abstract: The present invention provides a phthalamide derivative of the formula (I): wherein A1 is (substituted) C1-C8 alkylene, (substituted) C3-C8 alkenylene, (substituted) C3-C8 alkynylene, etc., R1 is H, (halo) C3-C6 cycloalkyl, (substituted) phenyl, (substituted) heterocycle, —A2—R4, etc., R2 and R3 are H, C3-C6 cycloalkyl, —A2—R4, etc., A2 is —C(═O)—, —C(═S)— or —C(═NR5)—, R4 is H, alkyl, (substituted) phenyl, (substituted) heterocycle, etc., X and Y are halogen, cyano, nitro, (halo) C1-C6 alkyl, (halo) C1-C6 alkoxy, etc., l is 0-4, m is 0-5, n is 0-2; and an agrohorticultural insecticide containing said compound as active ingredient and exhibiting an excellent insecticidal effect.

Abstract: Pharmaceutical compositions of modafinil compounds, including pharmaceutical, non-aqueous compositions of modafinil compounds in organic solvents and pharmaceutical compositions of a modafinil compound in solid dispersions, are disclosed, along with their use in the treatment of diseases.

Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.

Abstract: Novel sulphones of formula I are disclosed: 1

Abstract: The invention relates to novel diphenyl derivatives, to processes for their preparation and to their use in medicaments.

Abstract: Benzhydrylsulphinyl derivatives are used to prevent the sleepiness associated with pain medication. Such derivatives selectively antagonize the hypnogenic effect of anti-pain treatment, such as morphine, without affecting the analgesic activity of the treatment and without creating other disadvantages. Methods of treatment and pharmaceutical compositions are provided.

Abstract: Provided are an anti-inflammatory agent containing, as an active ingredient, at least one selected from amino acid derivatives represented by formula (I) wherein Ar represents an optionally substituted 2-hydroxyaryl group, n is 0 or 1, R2 represents a hydrogen atom or a side chain of an &agr;-amino acid or &bgr;-amino acid, X represents —O— or —NH—, R1 represents a hydrogen atom or a group that forms, together with R2 and an adjacent atoms, a cyclic structure of pyroglutamic acid, and R3 represents a hydrogen atom, an alkyl group having from 1 to 22 carbon atoms or an alkenyl group having from 2 to 22 carbon atoms, and salts thereof, and toiletries or skin external products containing the same. The anti-inflammatory agent of the invention inhibits expression of an inflammatory protein and activation of a gene transcription control factor that participates therein, and exhibits a good feeling upon use and a safety.

Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of multiple sclerosis.

Abstract: Novel non-steroidal ligands for the estrogen receptor which possess tissue-dependent estrogenic and antiestrogenic activity as well as methods for making the same and their applications in treating a variety of disease states.

Abstract: Substituted condensation products of N-benzyl-3-indenylacetamides with heterocyclic aldehydes and other such inhibitors are useful for the treatment of lupus erythematosus.