Abstract: Disclosed are novel inhibitors of Chk-1 and methods of using the same for therapy.

Abstract: The present invention provides compounds of formula (I) the prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein Ra, Rb, R1, and R2 are as defined herein; pharmaceutical compositions thereof; and uses thereof.

Abstract: Compounds of the current invention relate to rifamycin derivatives having antimicrobial activities, including activities against drug-resistant microorganisms. More specifically, compounds of the current invention relate to a series of novel spiro rifamycin derivatives which have demonstrated potent antimicrobial activity.

Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.

Abstract: Inhibitors of MIF are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with MIF activity. The inhibitors of MIF have the following structures: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, X, Y and Z are as defined herein. Compositions containing an inhibitor of MIF in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Abstract: Compounds are provided which are antagonists of chemokine receptor activity.

Abstract: Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRF1 receptors, including human CRF1 receptors. The invention thus includes methods for treatment of disorders and diseases associated with CRF1 receptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.

Abstract: The present invention is directed to compounds of the formula: that are antagonists of CGRP receptors and that are useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.

Abstract: Novel cycloalkyl compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to novel triazole compounds of formula (I), their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them. More particularly, the present invention relates to novel triazoles of the general formula (I) their derivatives, their analogs, their tautomeric forms, their regioisomers, their rotamers, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them.

Abstract: Compounds of formula (I): wherein: A is as defined in the description, Y represents a group selected from an oxygen atom and a methylene group, R2 represents a hydrogen atom and in that case: R3 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl, aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) and SO2CF3, or R2 and R3 form a bond, R1 represents a group selected from a hydrogen atom and the groups linear or branched (C1–C6)alkyl, aryl and aryl-(C1–C6)alkyl (in which the alkyl moiety is linear or branched) or a linear or branched (C1–C6)alkylene chain, Z1 and Z2 each represent a hydrogen atom or Z1 and Z2, together with the carbon atoms carrying them, form a phenyl group. Medicaments.

Abstract: Methods for the synthesis of CCI-779 and proline-CCI-779 are described, including a method involving lipase-catalyzed acetylation of 42-hydroxy of rapamycin with a vinyl ester of 2,2-bis(hydroxymethyl) propionic acid in an organic solvent followed by deprotection. Also provided are products containing proline-CCI-779 and uses thereof.

Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.

Abstract: Certain Alpha- and Beta-amino acid hydroxyethylamino sulfamic acid derivatives represented by the following formula are useful as retroviral protease inhibitors:

Abstract: 4-Tetrazolyl-4-phenylpiperidine Compounds, compositions comprising an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound, methods for treating or preventing pain or diarrhea in an animal comprising administering to an animal in need thereof an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound and methods for stimulating opioid-receptor function in a cell comprising contacting a cell capable of expressing an opioid receptor with an effective amount of a 4-Tetrazolyl-4-phenylpiperidine Compound are disclosed.

Abstract: Novel VEGFR-2 and VEGFR-3 inhibitory anthranilamide pyridones and their use as pharmaceutical agents for treating diseases that are triggered by persistent angiogenesis are selected.

Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.

Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.

Abstract: N-Heterocyclic derivatives of the following formula: where m, n, p, A1, R1, R2, R3 and R4 are described herein, as well as other N-heterocyclic derivatives, are useful as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.

Abstract: Universal linkers, their facile processes of manufacture and methods of using the same are provided.

Abstract: The present invention relates to organic molecules capable of modulating, regulating and/or inhibiting protein kinase signal transduction. Such compounds are useful for the treatment of diseases related to unregulated protein kinase signal transduction, including cell proliferative diseases such as cancer, atherosclerosis, arthritis and restenosis and metabolic diseases such as diabetes. The present invention features indolinone compounds that potently inhibit protein kinases and related products and methods. Inhibitors specific to the FLK protein kinase can be obtained by adding chemical substituents to the 3-[(indole-3-yl)methylene]-2-indolinone, in particular at the 1? position of the indole ring. Indolinone compounds that specifically inhibit the FLK and platelet derived growth factor protein kinases can harbor a tetrahydroindole or cyclopentano-b-pyrrol moiety.

Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.

Abstract: The invention relates to acyloxypyrrolidine derivatives of general formula (I): in which: R1 represents a hydrogen atom, a (C1–C6)alkyl, a (C3–C6)cycloalkyl, a group —CH2CH2COOH or a group —NR2R3; R2 and R3 each represent, independently, a hydrogen atom or a (C1–C6)alkyl. Also disclosed and claimed are the method of preparation of the compounds of the invention and their application in therapeutics.

Abstract: The invention relates to derivatives of indole-3-carboxamide having general formula (I): wherein: R1 represents a C3–C10 alkyl, a C5–C10 carbocyclic radical that is unsubstituted or substituted one or more times with a methyl group; R2 represents a hydrogen atom or a (C1–C4)alkyl group; R3 represents a halogen atom or a (C1–C4)alkyl group; R4 represents a hydrogen or halogen atom or a (C1–C4)alkyl group; R5 represents a (C1–C4)alkyl group or a trifluoromethyl; X represents a sulfur atom, an —NHSO2— group or an —SO2— group; and n is equal to 2 or 3. The invention also relates to a method of preparing the aforementioned derivatives and to the application of same in therapeutics.

Abstract: Certain ?-, ?-, and ?-amino acid derivatives are disclosed as selective GlyT2 inhibitors for the treatment of central nervous system (CNS) conditions such as muscle spasticity, tinnitus, epilepsy and neuropathic pain.

Abstract: A process for the manufacture of new crystalline salts of N-[2-(dimethylamino)ethyl]-1,2-dithiolane-3-pentanamide (racemic and chiral forms) is described. Such salts are stable, crystalline and have very good solubility in water. The salts exhibit antioxidant properties. They inhibit collagenase and elastase enzymes. They have excellent anti acne activity in addition tyrosinase inhibition. They are, by themselves and in combination with other known agents, important cosmetic ingredients.

Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.

Abstract: A compound is described. In particular, a non-steroidal sulphamate compound is described. The compound is suitable for use as an inhibitor of oestrone sulphatase. The compound is of general Formula (A), wherein R1–R6 are independently selected from H, halo, hydroxy, sulphamate, alkyl and substituted variants or salts thereof; but wherein at least one of R1–R6 is a sulphamate group; and wherein X is any one of S, NH, a substituted N, CH2, or a substituted C.

Abstract: Therapeutic methods of treatment, compositions and foodstuffs are described which contain isoflavone compounds described by general formula (1), in which Z is H, R1 is H, or RACO where RA is C1-10alkyl or an amino acid, R2 is H, OH, or ORB where RB is an amino acid, or CORA where RA is as previously defined, W is H, A is H or OH, and B is selected from (a), (b), (c), or W is H, and A and B taken together form a six-membered ring selected from (d), or W, A and B taken with the groups with which they are associated comprise (e), or W and A taken together with the groups with which they are associated comprise (f) and B is (g) wherein R3 is H, CORA where RA is as previously defined, CO2Rc where RC is C1-10alkyl, or CORB where RB is as previously defined, R4 is H, CORD where RD is H, OH, C1-10alkyl or an amino acid, CO2RC where RC is as previously defined, CORE where RE is H, C1-10alkyl or an amino acid, COOH, CORC where RC is as previously defined, or CONHRE where RE is as previously defined, R5 is H, CORC where

Abstract: A compound represented by the following formula (I) wherein R1 is a lower alkyl group, R2 is a hydrogen, a halogen, a cyano group, a lower alkyl group or a lower alkoxy group, and n is 0 or 1, which has a calpain inhibitory activity, is provided.

Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss.

Abstract: This invention relates to the regulation of vascular endothelium biocompatibility and to the inhibition of vessel wall cell and other types of cell hyperplasia following vessel wall dysfunction and/or injury. More particularly, the invention relates to the dietetic and pharmaceutical preparations of 13-hydroxyoctadeca-9Z, 11E-dienoic acid (13-HODE) and its use in reducing or inhibiting vessel wall hyperlasia and restoring vessel wall biocompatibility.

Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta p

Abstract: A method of stimulating the expression of endothelial NO-synthase in a mammal, which method comprises administering a physiologically active amount of 4-fluoro-N-indan- 2-yl benzamide according to the formula (I) to the said mammal.

Abstract: The present invention provides 4-substituted-2-azetidinone compounds, bicyclic 2-5-diketopiperazine compounds, and pharmaceutical compositions thereof that are potent, safe and effective neuroprotective agents. Due to their strong central nervous system (CNS) activity, the compounds can be used to enhance memory and to treat a variety of neurological disorders. The compounds are particularly useful for treating neurological disorders caused by, or associated with, CNS trauma.

Abstract: Novel methods for treating and preventing acute and/or chronic pancreatitis are described. Additionally, novel methods for inducing liver regeneration are described. The methods may comprise administering to a patient an effective amount of a metabolically stable analogue of spermidine and/or spermine. Preferred compounds for use in the methods may include 1-methylspermidine, 1-methylspermine and 1,12-dimethylspermine.

Abstract: The present invention relates to a method for reducing adhesions associated with post-operative surgery. The present method comprises administering or affixing a polymeric composition preferably comprising chain extended, coupled or crosslinked polyester/poly(oxyalkylene) ABA triblocks or AB diblocks having favorable EO/LA ratios to a site in the body which has been subjected to trauma, e.g. by surgery, excision or inflammatory disease. In the present invention, the polymeric material provides a barrier to prevent or reduce the extent of adhesions forming.

Abstract: The subject invention provides microemulsions having, as one component thereof, electron-deficient aromatic rings, e.g.. di(trifluoromethyi) benzene, for efficient separation and/or isolation of target molecules, e.g., bupivacaine.

Abstract: The present invention provides a dissolution method for saturated polyester capable of recycling saturated polyester used in fibers, a film, a bottle and others with ease and a low cost, a solution decomposing saturated polyester and a decomposition method using the solution.

Abstract: Process for the preparation of foamed thermoplastic polyurethanes characterized in that the foaming of the thermoplastic polyurethane is carried out in the presence of thermally expandable microspheres.

Abstract: Compositions suitable for use as base coats and varnishes, preferably for use in combination with electrostatic of set inks printed onto plastics substrates, particularly polycarbonate compact discs. They contain a photopolymerisable material, a photoinitiator, an inorganic transfer agent and heavy metal salt, preferably a metallic carboxylate. They have a good shelf life and good adhesion after hardening with ultraviolet light.

Abstract: The present invention relates to UV-curable compositions, the process for preparing the compositions and to the use of the curable compositions. The compositions contain: a) at least one oxetane compound; b) at least one polyfunctional cycloaliphatic epoxy compound; c) at least one multifunctional hydroxy compound; and d) at least one curing agent.

Abstract: The invention relates to a method for inhibiting the growth of microorganisms in a latex, especially a sterically stabilised or cationic stabilised latex and to a composition for use in the method comprising a polymeric biguanide and an isothiazolinone of the Formula (1). wherein: R is H, alkyl, cycloalkyl or aralkyl; and Y and Z each independently are H, halogen or C1-4-alkyl or Y and Z together with the carbon atoms to which they are attached form an optionally substituted 5 or 6 membered ring.

Abstract: Laser-markable pigments which are distinguished by the fact that an absorber is coated with a marker and optionally with a diffusion barrier are described. Further, processes for the preparation of the laser-markable pigments and methods for using them are described. The absorber is preferably an inorganic pigment or a filler. The marker is preferably an intrinsically laser-markable polymer, particularly a polyethylene terephthalate, acrylonitrile-butadiene-styrene, polystyrene, polyphenylene ether, liquid-crystal polymer or polyphenylene sulfide.

Abstract: The present invention is a biodegradable resin composition having excellent physical properties such as strength, water-resistance, molding workability, thermal-resistance, and suitable for a molded article for various electric products. The biodegradable resin composition of the present invention contains a biodegradable resin and filler coated with a biodegradable coating resin in which the filler coated with the biodegradable coating resin is contained within the biodegradable resin. Preferable aspects are such as an aspect that the filler is at least one of mica, talc and montmorillonite, an aspect that a filler content of the biodegradable resin is in the range of 5 mass % to 50 mass %, an aspect that an average diameter of the filler is in the range of 0.01 ?m to 200 ?m, and an aspect that the biodegradable resin is polylactic acid.

Abstract: A modified asphalt composition is provided comprising at least one plastomer, at least one elastomer, at least one crosslinking agent and asphalt. More specifically, a modified asphalt composition is provided comprising an oxidized polyethylene, a styrene-butadiene-styrene block copolymer, sulfur, and asphalt. A hot mix asphalt composition is also provided comprising the modified asphalt composition and aggregate. Processes for producing the modified asphalt composition and the hot mix asphalt composition are also provided as well as articles produced from these inventive compositions.

Abstract: In one embodiment, a colored polymeric resin composition, comprises: a polymeric resin; and a 1,8-diaminoanthraquinone derivative having a purity of greater than or equal to about 90 wt % and having a Formula (VIII): wherein R2–R7 are, individually, selected from the group consisting of a hydrogen atom, a hydroxyl group, an alkoxy group, an aryloxy group, an aliphatic group, an aromatic group, a heterocyclic group, a halogen atom, a cyano group, a nitro group, —COR9, —COOR9, —NR9R10, —NR10COR11, —NR10SO2R11, —CONR9R10, —CONHSO2R11, and —SO2NHCOR11; in which R9 and R10 are, individually, selected from the group consisting of a hydrogen atom, an aliphatic group, an aromatic group, and a heterocyclic group; wherein R11 is selected from the group consisting of an aliphatic group, an aromatic group, and a heterocyclic group; and wherein R is selected from the group consisting of hydrogen, an alkyl group containing 1 to 20 carbon atoms, a cycloalkyl group containing 3 to 20 carbon atoms, an allyl group containi

Abstract: A resin composition having excellent dispersibility, discoloration resistance and antimicrobial properties by blending a resin (A) with an antimicrobial agent (B) in which at least one kind of metal ion selected from the group consisting of silver, copper, zinc and tin is supported on zeolite, and an antimicrobial agent (C) that includes a silver ion-containing phosphate as an active ingredient, or an antimicrobial agent (D) made of a soluble glass powder containing silver ion.

Abstract: Coating materials comprising at least one electrically conductive pigment (A1) having an at least bimodal particle size distribution and at least one binder, the pigment/binder ratio being >1.5:1, can be used as coil coating materials.