Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.

Abstract: The present invention is related to new 3,4-dihydroberizo[1,2,3]thiadiazine-1,1-dioxide derivatives of the Formula (I), medicaments containing said new compounds, process for the preparation thereof and the use of said derivatives in the medicine. The compounds according to the present invention are suitable for the treatment or prevention of disorders of the central nervous system.

Abstract: Described herein are pharmaceutical compositions comprising therapeutically effective quantities of (i) a KATP channel modulator; and (ii) a CBx modulator. Also described herein are methods of making and using these compositions.

Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.

Abstract: The present invention relates to new benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I), medicaments containing such compounds and the use thereof in the medicine. Benzo[1,2,3]thiadiazine-1,1-dioxide derivatives of the general Formula (I) are suitable for the prevention or treatment of the diseases of the central nervous system.

Abstract: The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.

Abstract: The present invention relates to an oral suspension comprising meloxicam, its preparation and its use in alleviating inflammation and pain in both acute and chronic musculo-skeletal disorders.

Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides HCV polymerase inhibiting compounds having the formula (I): where R1 is cyclobutyl-N(Ra)—, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-. In a non-limiting example, a compound of the present invention is N-[(3-{1-[(cyclobutyl)amino])-4-hydroxy -2-oxo-1,2-dihydro-quinolin-3-yl}-1,1-dioxo-1,4-dihydro-1?6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methane-sulfonamide. The present invention also features compositions comprising the compounds of the present invention or pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and methods of using the same to treat or prevent HCV infection.

Abstract: The invention is directed to 5,6-dihydro-1H-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: Compounds, pharmaceutical compositions, kits and methods useful for inhibiting HDAC, thereby treating a disease state for which HDAC possess activity that contributes to the pathology and/or symptomology of the disease state. The compound is selected from the group consisting of: wherein the variables are as defined herein.

Abstract: The invention is directed to [1,2,4]thiadiazine 1,1-dioxide compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

Abstract: Compositions and methods for treating cancer, including hematologic cancers such as multiple myeloma, are disclosed. In some embodiments, chaetocin, chaetomin, or gliotoxin can be used to treat or ameliorate one or more symptoms or disorders associated with multiple myeloma.

Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound has a superior mineral corticoidreceptorantagonistic action and is useful as an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like, a compound having a fused heterocycle, or a prodrug thereof, or a salt thereof; and an agent for the prophylaxis or treatment of hypertension, cardiac failure and the like.

Abstract: Fused-ring triazole compounds which inhibit proliferation of cells and exhibit a unique and intense fluorescence are provided. Also provided are methods for synthesizing these compounds and methods for using these compounds to inhibit cell proliferation and infection and to label and fluorescently detect selected molecules.

Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

Abstract: The present invention relates to methods and compositions for treating neuropathic pain and neuropsychiatric disorders by administering agents that are effective in reducing the effective amount, inactivating, and/or inhibiting the activity of a Na+—K+-2Cl? (NKCC) cotransporter. In certain embodiments, the Na+—K+-2Cl? co-transporter is NKCC1.

Abstract: The present invention relates to modified amino acids of general formula wherein A, Z, X, n, m, R, R2, R3, R4 and R11 are defined as in claims 1 to 5, their tautomers, their diastereomers, their enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them as well as their use for the production and purification of antibodies and as labelled compounds in RIA- and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.

Abstract: Compounds having the formula are hepatitis C(HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C(HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

Abstract: Inhibitors of indoleamine 2,3-dioxygenase (IDO) are provided as are pharmaceutical compositions containing such inhibitors as well as the use of such inhibitors and compositions for the treatment of a condition in a mammalian subject characterized by pathology of the IDO-mediated tryptophan metabolic pathway. Such conditions may involve suppression of T-cell mediated immune response or may directly result from depletion of tryptophan or accumulation of a product of tryptophan degradation. Specific disease conditions include cataracts, age-related yellowing in the eye, neurodegenerative disorders, mood disorders, cancer and various bacterial/viral infections. IDO inhibitors of this invention are substituted naphthalene and anthracene diones. Novel compounds of this invention include the following taurine-substituted naphthaquinone structure.

Abstract: The present invention describes the use of Notch2 inhibitors for producing a medicament for the treatment of tumours, which tumours are characterised by ligand-independent Notch2 fragments.

Abstract: Compounds of formula (I): wherein: A represents thienyl, furyl, pyrrolyl, oxathiol, thiazole, isothiazole, oxazole or imidazole, represents a single bond or a double bond, R1 represents hydrogen, linear or branched (C1-C6)alkyl optionally substituted by one or more groups selected from halogen or (C1-C6)alkoxy-(C1-C6)alkyl, R2 represents hydrogen or linear or branched (C1-C6)alkyl group optionally substituted by one or more halogen, R3 represents hydrogen or a group selected from linear or branched (C1-C6)alkyl, CONHR? and SO2NHR? wherein R? represents linear or branched (C1-C6)alkyl, its enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same, which are useful as AMPA inhibitors.

Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.

Abstract: The invention is directed to pyrro[1,2-b]pyridazinone compounds of Formula I and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus: wherein R4 is selected from Ring A is 5 or 6- membered aryl or heterocyclyl, and the remaining substituents are defined herein.

Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.

Abstract: The invention relates to the use of diketodithiopiperazine antibiotics, in particular chaetocin and gliotoxin, for the preparation of pharmaceutical compositions for antitumor therapy.

Abstract: The invention is directed to pyridazinone compounds of Formula I and pharmaceutical compositions containing compounds of Formula I wherein R1 and R2 are independently H, alkyl, cycloalkyl, aryl, or heterocyclyl; and Ring A is 5 or 6-membered aryl or heterocyclyl. The invention also encompasses methods of using a compound of Formula I in the treatment of hepatitis C virus infections.

Abstract: The present invention provides HCV polymerase inhibiting compounds having the formula (I): where R1 is cyclobutyl—N(Ra)-, n is 1, 2, 3 or 4, and at least one R5 is RaSO2N(Rj)alkyl-, In a non-limiting example, a compound of the present invention is N-[(3-{1-[(cyclobutyl)amino])-4-hydroxy -2-oxo-1,2-dihydro-quinolin-3-yl}-1,1-dioxo-1,4-dihydro-1?6-thieno[2,3-e][1,2,4]thiadiazin-7-yl)methyl]methane-sulfonamide. The present invention also features compositions comprising the compounds of the present invention or pharmaceutically acceptable salts, stereoisomers or tautomers thereof, and methods of using the same to treat or prevent HCV infection.

Abstract: Compounds having the formula are hepatitis C(HCV) polymerase inhibitors. Also disclosed are a composition and method for inhibiting hepatitis C(HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.

Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.

Abstract: Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.

Abstract: The present invention is directed to cyclic sulfonamide derivatives of formula I: or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.

Abstract: The present invention is directed to substituted benzothiadiazinedioxide derivatives of formula I: or a pharmaceutically acceptable salt, stereoisomer or tautomer thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorders, cognitive disorders, diabetic neuropathy, pain, and other diseases or disorders.

Abstract: Compounds of the formula I: and pharmaceutically acceptable salts thereof wherein X is N, Y is S, Z is —(CRaRb)r—, A is —NR3, m is 2, n is 1, q is 2, R2 is optioinally substituted aryl or optionally substituted heteroaryl, and p, R1, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I for treatment of central nervous system diseases.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is

Abstract: A method and composition for preventing prostate cancer and/or reducing PSA levels and/or alleviating the symptoms of BPH (Benign Prostatic Hyperplasia) or PIN (prostatic intraepithelial neoplasia) by administration of an effective amount of a mixture of flavopereirine and alstonine. A method and composition for treating low-grade prostate cancer and preventing the onset of metastatic disease and/or reducing the doubling time of PSA levels in men with positive biopsies showing relatively low Gleason scores and morphologies characteristic of non-invasive, slow-progressing prostate cancer. The flavopereirine and alstonine can be in the form of natural extracts derived from Pao Pereira and Rauwolfia Vomitoria, respectively. Alternatively, these two active compounds can be administered in purified form. The composition can be in included in a kit along with instructions for use in a treatment regimen.

Abstract: Use of 7-oxa-2-thia-1,5-diazabicyclo[3.3.1]nonane-2,2-dione (“cyclotaurolidin”) for the preparation of antimicrobial formulations, in particular antimicrobial solutions for technical or medical purposes and of aqueous lock solutions for catheters and port systems for preventing infections and sepsis of patients.

Abstract: The invention relates to compounds of formula (I): wherein: R1 represents hydrogen, alkyl or cycloalkyl, R2 represents hydrogen, halogen or hydroxy, A represents CR3R4 or NR3 wherein R3 and R4 are as defined in the description, Y represents an alkylene chain as described in the description, X represents NR5R6, S(O)nR7, OR8, C(O)R9, amidino or a heterocycle, their isomers, and addition salts thereof; and medicinal products containing the same which are useful in the prevention or treatment of diseases associated with AMPA flux.

Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, X represents oxygen or sulphur, Y represents oxygen, sulphur or NR wherein R represents hydrogen or alkyl, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts Medicaments.

Abstract: Compounds of formula (I): wherein: R1 represents aryl or heteroaryl, R2 represents hydrogen, halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or halogen, their isomers and also their addition salts. Medicaments.

Abstract: Compounds of formula (I): wherein: R1 represents a heterocycle, R2 represents hydrogen, a halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with the adjacent —CHR3—, forms the ring wherein m represents 1, 2 or 3, R5 represents hydrogen or a halogen, their isomers, and also addition salts thereof.

Abstract: Compounds of formula (I): wherein: R1 represents hydrogen, a halogen or alkyl, R1a represents hydrogen or alkyl, R2 represents hydrogen, a halogen or hydroxy, A represents CR4R5 or NR4, R3 represents hydrogen, alkyl or cycloalkyl, R4 represents hydrogen or alkyl, or A represents nitrogen and, together with the adjacent —CHR3—, forms the ring ?wherein m represents 1, 2 or 3, R5 represents hydrogen or a halogen, X is as defined in the description, their isomers, and also addition salts thereof.

Abstract: Fused-ring triazole compounds which inhibit proliferation of cells and exhibit a unique and intense fluorescence are provided. Also provided are methods for synthesizing these compounds and methods for using these compounds to inhibit cell proliferation and infection and to label and fluorescently detect selected molecules.

Abstract: A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(?O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.

Abstract: Disclosed are methods and compositions for regulating the melanin content of mammalian melanocytes; regulating pigmentation in mammalian skin, hair, wool or fur; treating or preventing various skin and proliferative disorders; by administration of various compounds, including alcohols, diols and/or triols and their analogues.

Abstract: Compounds of formula I are p38 inhibitors: or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen or alkyl; R2 alkyl, haloalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heteroalkylsubstituted cycloalkyl, heterosubstituted cycloalkyl, heteroalkyl, cyanoalkyl, heterocyclyl, heterocyclylalkyl, or —Y1—C(O)—Y2—R11 (where Y1 and Y2 are independently either absent or an alkylene group and R11 is hydrogen, alkyl, haloalkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino); R3 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, heterosubstituted cycloalkyl, heterocyclyl, aryl, aralkyl, haloalkyl, heteroalkyl, cyanoalkyl, -alkylene-C(?O)—R4 (where R4 is hydrogen, alkyl, hydroxy, alkoxy, amino, monoalkylamino or dialkylamino), or acyl; Ar1 is aryl; X1 is O, NR5 or S, where R5 is hydrogen or alkyl; and X2 is a bond, O, NR6, S or CH2, where R6 is hydrogen or alkyl.

Abstract: Novel compounds of formulae (I) to (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.

Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereon wherein —Z1—Z2— is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a

Abstract: A wood treatment concentrate includes, by weight; (a) 0.1-10% of an active wood treatment chemical, (b) 50-99% of a microemulsion concentrate including: (i) 0.03-80%, preferably 40-70%, of a castor oil ethoxylate or tristyryl phenol ethoxylate, (ii) 0-10%, preferably 0.005-6%, of an ethoxylated phosphoric acid ester as pH buffer, (iii) 0.002-40%, preferably 0.05-29%, of a N—C8-C18 alkyl pyrrolidone and (iv) 0-60%, preferably 0.15-40%, of a N—C1-C4 alkyl pyrrolidone, and (v) 0-30%, preferably 0.5-15%, of an ethylene oxide/propylene oxide block copolymer; and (c) 1-50% of a substituted phenol. The use formulation includes (d) water of dilution.