Abstract: The present invention provides antibacterial compounds, antibacterial compositions, bacteria-reducing methods, bacteria-reduced substrates/articles made by the methods that employ an antibacterial agent comprising a non-halogenated nitrile-substituted salicylanilide, and processes for producing 5-acyl salicylamides.

Abstract: Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

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 present invention provides an improved process for preparing modafinil, whereby it may be isolated in high purity by a single crystallization. The process produces modafinil free of sulphone products of over-oxidation and other byproducts. The invention further provides new crystalline Forms II–VI of modafinil and processes for preparing them. Each of the new forms is differentiated by a unique powder X-ray diffraction pattern. The invention further provides pharmaceutical compositions containing novel modafinil Forms II–IV and VI.

Abstract: Mixtures of a modafinil compound with a cyclodextrin, methods for their use, and compositions thereof are disclosed, along with complexes comprising a modafinil compound and a cyclodextrin which are taste-masked and suitable for oral consumption in an aqueous solution.

Abstract: The invention relates to a process for the preparation of crystalline forms of the optical enantiomers of modafinil, comprising stages comprising: i) dissolving one of the optical enantiomers of modafinil in a solvent other than ethanol, ii) crystallising the modafinil enantiomer, iii) recovering the crystalline form of the modafinil enantiomer so obtained. The invention also relates to a process for the preparation of the optical enantiomers of modafinil.

Abstract: This invention relates to novel phthalamide derivatives of formula (I) wherein R1, R2, R3, R4, and R5 have the meanings given in the disclosure, to processes for their preparation, and to their use as insecticidal agents in agricultural and horticultural field.

Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of Formula I: (I) wherein Ar1, Ar2, Ar3, L1, L2 and Q areas defined, or a pharmaceutically acceptable salt, solvate, enantiomer or mixture of diastereomers thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and Related Diseases

Abstract: The present invention relates to an androgen receptor alkylating compound, wherein the compound may include, inter alia, an active functional group, which permits the alkylation of the androgen receptor.

Abstract: The invention provides small molecules that act as catalytic antioxidants and methods of use thereof. The compounds can repeatedly bind and destroy reactive oxygen species by serving as substates for enzymes of the methionine sulfoxide reductase (Msr) class. Some embodiments of the catalytic antioxidant compounds are derived from drugs with anti-inflammatory activity due to inhibition of cyclooxygenase enzymes.

Abstract: Colchicine derivatives represented by the formula (I) with a halogen or nitric ester group, or pharmaceutically acceptable salts thereof, are described. Pharmaceutical compositions containing the same as effective components are also described. The colchicine derivatives were found to have anticancer, anti-proliferous and immunosuppressive function. Methods for preparing the colchicines derivatives are also provided.

Abstract: The present invention relates to a new process for the synthesis of racemic and optically active bicalutamide starting from ethyl pyruvate and methyl methacrylate. The present invention discloses processes of preparing bicalutamide intermediates including ethyl-[2-{4-fluorophenyl sulfone}]-2-hydroxy propionate, 1,2-epoxy-2-methyl propionate and 2-hydrox-2-methyl-3-(4-fluorophenylthio) propionic acid. The present invention further discloses micronized rac-bicalutamide and the preparation thereof. The present invention further discloses a new process for the isolation and purification of racemic and optically active bicalutamide.

Abstract: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.

Abstract: Modafinil is effective in improving symptoms of attention deficit hyperactivity disorder and symptoms of multiple sclerosis fatigue. The administration of modafinil is also shown to activate the tuberomamillary neurons of the posterior hypothalamus, and thus exhibits activity in an area of the brain associated with normal wakefulness functions.

Abstract: N-Arylphenylacetamide derivatives represented by the following formula [I]: (wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, —(CH2)m—N(R6)(R7) (m is an integer of from 1 to 4; R6 is hydrogen, C1-4 alkyl, etc., R7 is hydrogen, etc.), etc.; R3 is hydrogen, halogen, etc.; R4 is C6-10 alkyl, —Y—R8 (Y is a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc., R8 is aryl, C3-8 cycloalkyl, C6-15 polycycloalkyl, etc.), etc.; R5 is hydrogen, etc.; and X1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.

Abstract: The present invention provides processes for the preparation of modafinil which includes the step of reacting benzhydrylthiol and chloroacetamide.

Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.

Abstract: The present invention relates to an antiandrogen compound and a method of treating prostate cancer in a patient utilizing the compound. The present invention also relates to a pharmaceutical composition which includes the compound.

Abstract: The present invention relates to pharmaceutically acceptable compounds, including acylguanidine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are particularly useful for the treatment or prophylaxis of neurological injury and neurodegenerative disorders.

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

Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.

Abstract: The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel activity, such as, cardiovascular diseases, for example hypertension, congestive heart failure, arrhythmia and angina.

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: A method of prevention or treatment of a cholesterol-associated tumor is provided which comprises administering a therapeutically effective amount of an azetidinone-based cholesterol absorption inhibitor, preferably ezetimibe (SCH 58235) and/or its phenolic glucuronide, or at least one ezetimibe analog, e.g., SCH 48461 and SCH 58053, to a patient wherein the patient is either at risk of developing a cholesterol-associated tumor or already exhibits a cholesterol-associated tumor. Formulations of ezetimibe are also provided for the prevention or treatment of a cholesterol-associated tumor further comprising at least one other anticancer agent.

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 present invention provides processes for the preparation of modafinil which includes the step of reacting benzhydrylthiol and chloroacetamide.

Abstract: The invention concerns compounds of formula (I): R—A—R? wherein: A is as defined in the description; R represent, a group (V), wherein R?a and R?a are as defined in the description, or R forms with A a cyclic structure as defined in the description; R? represents a (CH2)t—R2 group wherein q, t, and R2 are as defined in the description. The invention is useful for preparing medicines.

Abstract: A composition and method for delivering sulfur to skin and absorbing irritants in the skin. A high sorption base is employed which comprises non-swelling clay, gum, swelling clay, silicon and combinations thereof. The absorption of the irritants does not hinder the delivery of the active ingredient to the skin.

Abstract: The present invention provides an improved process for preparing modafinil, whereby it may be isolated in high purity by a single crystallization. The process produces modafinil free of sulphone products of over-oxidation and other byproducts. The invention further provides new crystalline Forms II-VI of modafinil and processes for preparing them. Each of the new forms is differentiated by a unique powder X-ray diffraction pattern. The invention further provides pharmaceutical compositions containing novel modafinil Forms II-IV and VI.

Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.

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: An amine derivative, its tautomeric or stereoisomeric form, or a salt thereof which has vanilloid receptor 1 (VR1) antagonistic activity, is disclosed. The amine derivative has an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, incontinence and/or inflammatory disorders.

Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: 1

Abstract: The present invention is directed to solid oral dosage forms comprising surface-treated particles comprising modafinil particles and a hydrophilic treating agent, methods of making the same, and uses thereof

Abstract: N-Arylphenylacetamide derivatives represented by the following formula [I]: 1

Abstract: There is disclosed a pharmaceutical composition comprising gabapentin or an analogue thereof (pregabalin or tiagabine) and an &agr;-aminoamide and its analgesic use. A synergistic effect of the respective analgesic activities without concomitant increase of side effects was observed.

Abstract: Methods of controlling a pest such as an insect pest comprise administering to said pest a pesticidally effective amount of a non-peptide TMOF analog (also referred to as an “active compound” or “pesticidal compound” herein). Compositions and compounds useful for carrying out such methods are also disclosed.

Abstract: Compounds of formula (I) 1

Abstract: Compositions and methods for the treatment of depressive disorders through the administration of modafinil with antidepressants.

Abstract: Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group —C(O)—(CHR4)m—AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R3; R3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R2; and R4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed.

Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.

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

Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a CNS-penetrant NK-1 receptor antagonist (e.g., a substance P receptor antagonist) in combination with an antidepressant or an anxiolytic agent. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a CNS-penetrant NK-1 receptor antagonist and an anxiolytic agent or antidepressant.

Abstract: Benzamide compounds of Formula VII are prepared by reacting a benzoate compound of Formula V with an amine to obtain a benzamide compound of Formula VI, and then treating the benzamide VI with an amine deprotecting agent to obtain the benzamide VII; wherein R1 and R2 are each independently H, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, aryl, or substituted aryl; R3 is alkyl, -alkylaryl, or aryl; and P* is an amino protective group.

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: A microbicidal composition containing: (a) at least one non-halogenated 2-alkyl-4-isothiazolin-3-one selected from substituted and unsubstituted 2-(C1-C4)alkyl-4-isothiazolin-3-ones; and (b) at least one of 2,2′-dithiobis(N-methylbenzamide) and 2-methylbenzisothiazolone.

Abstract: Novel formulations combining a non-steroidal anti-inflammatory drug (NSAID) such as flunixin, with a fluorinated chloramphenicol or thiamphenicol derivative antibiotic such as florfenicol are disclosed. Methods for using such formulations in the treatment and prevention of infectious diseases of bovines and swine, including bovine respiratory disease and swine respiratory disease, are also disclosed.

Abstract: A formulation that includes a mixture of at least one antibiotic, at least one analgesic, and at least one solvent is provided. The antibiotic and the analgesic are dissolved in the solvent to form a formulation that is suitable for veterinary applications. This formulation can be administered to animals as a pour-on or an injectable formulation.

Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; n is 0, 1, or 2; and each linker is independently an isostere of —NHCONH— or of —N?N— or of —NHCO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.