Abstract: The invention relates to new products of formula (I): in which: Y represents oxygen or sulphur, Z represents C?CH2, CH—CH3 or CH2, R1 represents hydrogen, morpholinyl or the radical. In which the two nitrogen atoms are linear or form a cyclic radical, X represents carbonyl, alkylene or alkenylene, linear or branched, containing at most 6 carbon atoms optionally interrupted by oxygen or sulphur, R4, R5 and R6 represent hydrogen, a protective group of the nitrogen, alkyl, cycloalkyl, aryl and arylalkyl optionally substituted, R2 represents alkyl optionally substituted by aryl, heteroaryl or —NR4R5, R3 represents alkyl, cycloalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl optionally substituted, these products being in all isomer forms and the salts, as medicaments.

Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): wherein: W is —O—, —N(R1)—, C(O), S(O)t; (where t is 0, 1 or 2), N(R1)S(O)2, S(O)2N(R1), C(O)N(R1) or N(R1)C(O)N(R1); and V is C(O), C(S), C(O)N(R1)—, C(O)O—, S(O)2—, S(O)2N(R1)— or C(R11)H; and x, y, R1, R2, R3, R4, R5, R6, R7, R7a, R8, R8a, R9, R9a, R10 and R10a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Abstract: Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a UCP and/or Fas antibody or other inhibitor, or combination thereof, and a therapeutically acceptable amount of a fatty acid metabolism inhibitor and/or a therapeutically acceptable amount of a glucose metabolism inhibitor, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an antibody against UCP and/or Fas antigen with an oxirane carboxylic acid, represented by etomoxir, and/or with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.

Abstract: This invention relates to the use of nicotine receptor agonists for treating inflammatory diseases, including a variety of pulmonary diseases. Such agonists have fewer side effects than other anti-inflammatory drugs, such as steroids. Moreover, these agonists can be used alone or in combination with other anti-inflammatory drugs to alleviate pulmonary diseases.

Abstract: A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and processes for producing such novel forms are also provided.

Abstract: Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).

Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, TNF-? or combinations thereof.

Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: Disclosed is a method of treating a non-cardiovascular disorder characterized by an abnormal persistent sodium current in a subject in need of treatment thereof, said method comprising administering to the subject an effective amount of a compound of Formula (I): wherein: m is 1 or 2; R1, R2, R3, R4, and R5 are each independently selected from the group consisting of hydrogen, halo, CF3, CN, OR22, SR22, N(R22)2, S(=O)R22, SO2N(R22)2, C(?O)R22, alkylamido, alkyl, alkenyl, morpholino, and pyrrolyl, wherein the alkyl substituent is optionally substituted with one substituent selected from the group consisting of OR22, or R2 and R3 together or R4 and R5 together can be alkylene; R6, R7, and R8 are each independently selected from the group consisting of H and alkyl; R9, R10, R11, R12, R13, R14, R15, and R16 are each independently selected from the group consisting of H and alkyl, or wherein one or more of R9 and R10, R11 and R12, R13 and R14, and R15 and R16 are together ?O; R17, R18, R19, R20 and R21 are eac

Abstract: The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.

Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Abstract: 3-cyanonaphthalene-1-carboxylic acid perhydroxyalkylmethyl-piperazine compounds of formula I which are antagonistic to tachykinin receptors, pharmaceutical compositions containing such compounds, methods of using such compounds for the treatment and/or inhibition of various diseases and disorders, processes for preparing such piperazine compounds, and intermediate products of these processes.

Abstract: A method for rendering a carboxyl-containing polymer surface resistant to microbial growth, the method comprising: (i) reacting the carboxyl-containing polymer surface with a metal borohydride in a solvent system comprising a water-soluble alcohol having one to three hydroxy groups and one to four carbon atoms, and optionally up to about fifty percent water, in a temperature range having a minimum of about 60° C. and a maximum of about 80° C., and for an amount of time sufficient for reducing carboxyl groups on the carboxyl-containing polymer surface to surface hydroxymethyl groups without altering the nature of the bulk of the polymer; and either: (iia) converting hydroxy groups of the surface hydroxymethyl groups to leaving groups and displacing the leaving groups with one or a combination of antimicrobial agents; or (iib) displacing the hydrogen atoms of the hydroxy groups of the surface hydroxymethyl groups with one or a combination of antimicrobial agents.

Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.

Abstract: An insecticide composition is provided for killing insects comprising a metal sequestering agent and an insecticide. The composition is particularly useful for killing scale insects, particularly Cycad Asian Scale insects that are hosted by plants of the cycad phyta division. Since the scale insect's shell includes calcium, the metal sequestering agent, when combined with an insecticide and/or fungicide, substantially increases the likelihood that the insecticide and/or fungicide will come into contact with the insect and kill the insect.

Abstract: Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.

Abstract: Disclosed are compounds of the formula: wherein R8 represents a cyclic and acyclic moiety to which is bound an imidazolylalkyl group; R9 represents a carbamate, urea, amide or sulfonamide group; and the remaining substituents are as defined herein. Also disclosed is a method of treating cancer and a method of inhibiting farnesyl protein transferase using the disclosed compounds.

Abstract: Compounds of general formula (I) in which R1, A1, A2 and R2 have any of the meanings given in the specification, have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.

Abstract: A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof wherein m, n, X, Ar, R1, R2, R3, R4 and R5 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: The invention relates to an in vitro method for diagnosing essential tremor wherein a mutation of dopamine D3 receptor gene or protein is sought. The invention further relates to the use of a ligand having anti-dopamine D3 receptor activity for treatment of essential tremor.

Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).

Abstract: This invention relates to methods for treating a patient suffering from neuropathic or nociceptive pain which may be mechanical, visceral, and/or inflammatory in nature, comprising administering a therapeutically effective amount of Ranolazine to a patient in need thereof.

Abstract: Compound of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.

Abstract: The invention provides a therapeutic method for treating at least one symptom of Alzheimer's disease in a mammal, such as a human, wherein the toxicity of a pathogen of ? amyloid peptide mammalian cells is implicated and inhibition of the subsequently-induced pathological pathways is desired comprising administering to a mammal in need of such therapy, an effective amount of a benzoylpiperazine derivative, including pharmaceutically acceptable salts thereof.

Abstract: The invention relates to the use, as agent for depigmenting and/or whitening the skin, in particular for eliminating pigmentary spots and/or senescence spots, and/or as anti-browning agents, of a compound of formula (I): R1—CHOH—CH(NH—COR2)(CH2OH)??(I) in which R1 denotes a C11 to C21 alkyl radical, and R2 denotes a linear, optionally hydroxylated C11-C19 hydrocarbon-based radical, with the hydroxyl group being in the alpha-position with respect to the carbonyl, which may comprise one or more ethylenic unsaturations, in particular one or two ethylenic unsaturations. The invention also relates to a cosmetic process for depigmenting and/or lightening skin exhibiting pigmentation spots, comprising the application to the skin of a composition comprising, in a physiologically acceptable medium, a compound of formula (I).

Abstract: The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.

Abstract: The present invention relates to the compounds of the general formula (I), a composition for and a method of treating breast cancer or other proliferative disorders in a subject using a compound of general formula [I], wherein the substituents are as defined in the specification.

Abstract: The present invention refers to the use of compounds binding to the sigma receptor for the treatment of metabolic syndrome.

Abstract: The present invention relates to method of reversing left ventricle remodeling by combined administration of therapeutically effective amounts ranolazine and at least one co-remodeling agent, which may be an ACE inhibitor, an ARB, or a beta-blocker. The method finds utility in the treatment of heart failure. This invention also relates to pharmaceutical formulations that are suitable for such combined administration.

Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.

Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are styrenyl derivative compounds, including but not limited to stilbene derivative compounds, and compositions comprising these compounds, that are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.

Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.

Abstract: The present invention is directed to compounds represented by the formula (1): B-D-Z (1), wherein B represent the following formula (B-1), (B-2) or (B-3); A represents an optionally substituted imidazole or pyrazole group; E represents the following formula (1a); X represents an oxygen atom, the formula: SOu, or the formula: N—R9; Y represents a carbon atom or a nitrogen atom; D represents an oxygen atom, a sulfur atom or the formula (1a); Z represents (a chroman-2-yl group, a chroman-4-yl group, a 2,3-dihydrobenzofuran-2-yl group, a 2,3-dihydrobenzofuran-3-yl group, etc.) which is substituted with NHR10 or OR11)] or pharmaceutically acceptable salts thereof, and to antioxidants, therapeutic agents for kidney diseases or cerebrovascular disorder, and retinal oxidative damage inhibitors, which include the compounds as the active ingredient.

Abstract: The present invention is disubstituted amines of formula (I) and disubstituted amines of formula (II) useful in treating Alzheimer's disease and other similar diseases.

Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.

Abstract: The present invention relates to a chemical genus of biaryl substituted heterocycle inhibitors of LTA4H (leukotriene A4 hydrolase) useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.

Abstract: The present invention discloses compounds of Formula I wherein V, W, Y, Z, R1, R2, R3, R4, d, m, n, p and r are herein defined, said compounds being 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: An object of the present invention provides a novel compound having the anti-viral activity, particularly, the HIV integrase inhibitory activity, and a drug containing the same, particularly, an anti-HIV drug.

Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Use of 1,4-bis(3-aminoalkyl)piperazine derivatives as defined in formula I or II for the manufacture of a pharmaceutical composition intended for the treatment of neurodegenerative diseases, related neurodegenerative diseases, developmental diseases or cancer. The instant invention is also directed to some specific 1,4-bis(3-aminoalkyl)piperazine derivatives and pharmaceutical composition including them.

Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

Abstract: Compounds as modulators of peroxisome proliferator activated receptors, pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.

Abstract: The present invention provides a catechol-based derivative and a pharmaceutical acceptable salt therefrom and a solvate therefrom. A pharmaceutical composition for preventing or treating diabetics and ischemics, comprising a catechol-based derivative of formula (I) and at least one selected from the group consisting of a pharmaceutical excipient, a diluent and a carrier.

Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, use in the reduction of A? peptide in vivo, use in modulating APP processing, and use in modulating the activity of APP secretase.

Abstract: Compounds of general formula (I) in which R1 and R0 have any of the meanings given in the specification have affinity for sigma receptors and are useful in the treatment of disorders of the central nervous system.

Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.

Abstract: The use of cinnarizine and dimenhydrinate or their physiologically compatible salts in combination is described for the treatment of vertigo of any genesis.

Abstract: N-Benzoyl arylsulfonamides having the formula are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.