Abstract: The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.

Abstract: The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction

Abstract: The present invention is directed to compounds which are inhibitors of the beta-secretase enzyme and which are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.

Abstract: Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals.

Abstract: This invention relates to methods for treating sexual dysfunction, by administering a compound of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl radical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. The compound may also be administered in combination with at least one organic nitrate or NO donor, or in combination with at least one compound which inhibits the breakdown of cyclic guanosine monophosphate (cGMP).

Abstract: A method of inhibiting or effecting the activity of protein kinase activity which comprises contacting a protein kinase with a compound of formula (I) being a derivative of a furanose or pyranose form of a monosaccharide, or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.

Abstract: Use of a combination of two vitamin compounds, i.e. riboflavin (also known as vitamin B2) and nicotinic acid (also referred to as niacin) or, as an alternative thereto, the corresponding amide, i.e. nicotinamide or niacinamide (also known as vitamin PP) for the systemic treatment of various forms of itching, such as, e.g., pruritus associated with renal insufficiency or failure (i.e. uremic pruritus), and of pruritus forms that are not connected with primary organic affections, as well as for the treatment of a number of non-infective internal affections of a substantially inflammatory nature, such as e.g., urticaria and/or angioedema, asthma, allergic rhinitis and allergic oculorhinitis.

Abstract: The present invention makes availables assays and reagents inhibiting paracrine and/or autocrine signals produced by a hedgehog protein or aberrant activation of a hedgehog signal transduction pathway, e.g., which involve the use of a steroidal alkaloid or other small molecule.

Abstract: The invention concerns dihydroimidazo[5,1-a]-?-carboline compounds of general formula (I) wherein in particular, R1, R2, R3, R4, R6 and R7, identical or different, independently of one another, present a hydrogen, halogen atom, an alkyl, hydroxyl, alkoxy, trihalogenoalkyl, alkylamino, dialkylamino, aryl, arylalkyl, carboxy, alkylcarbonyloxy, acyl, aryloxy or arylalkoxy group; R5 represents a hydrogen atom, an alkyl or arylalkyl group; and their isomers as well as their addition salts to a pharmaceutically acceptable acid. The inventive compounds are for use in medicine, in particular as hypnotics.

Abstract: The invention is based in part on the discovery that nonselective ? agonists that possess ? receptor-mediated effects in addition to their ? agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective ? agonists. The invention includes a number of new compounds having both nonselective ? opioid receptor agonist activity and additional activity at ? opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain imaging.

Abstract: A pharmaceutical composition comprising a compound of Formula I wherein R1 is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benzimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R5)(R6) wherein one of R5 and R6 is selected from H and and the other is selected from carboxy, carboxy-loweralkyl and lower alkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R2 and R3 are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S-, loweralkyl, and Z(O)OR7 wherein Z is selected from C and S and R7 is selected from H, lower alkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described.

Abstract: The present invention relates to novel 5-substituted 7-azaindole compounds of formula (I), their use in the inhibition of c-Jun N-terminal kinases, their use in medicine and particularly in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.

Abstract: The present invention relates to compounds that bind to chemokine receptors, and having the formula wherein each A, X, Y, R1, R2 and R3 are substituents. The present invention also relates to methods of using such compounds, such as in treating HIV infection and inflammatory conditions such as rheumatoid arthritis. Furthermore, the present invention relates to methods to elevate progenitor and stem cell counts, as well as methods to elevate white blood cell counts, using such compounds.

Abstract: The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c? or N?; R1 is C2–C6 alkyl, substituted C2–C6 alkyl, C3–C7 cycloalkyl, substituted C3–C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1–C3 n-alkyl, C3–C6 cycloalkyl-C1–C3 alkyl, or a group of formula II (II) provided that when R1 is C2–C6 alkyl or substituted C2–C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)?, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1–C3 alkyl; R5 is hydrogen, C1–C3 alkyl, or C3–C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1–C6 alkyl; and n is an integer from 1 to 6 inclusively.

Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity

Abstract: The invention relates to ?-amino-N-hydroxy-acetamide derivatives of formula I, wherein R is di-lower alkyl amino, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and including 10, and n represents an integer from 0 up to and including 10, and salts thereof; to processes for their preparation, pharmaceutical compositions comprising said hydroxamic acid derivatives, the use of such hydroxamic acid derivatives as medicaments, and a method of treating conditions or diseases mediated by matrix-degrading metalloproteinases (MMP's) using said derivatives alone or in combination with one or more other therapeutic agents.

Abstract: Compounds of the formula provide pharmacological agents which are inhibitors of PTPases, in particular, the compounds of formula I inhibit PTP-1B and TC PTP, and thus may be employed for the treatment of conditions associated with PTPase activity. The compounds of the present invention may also be employed for inhibition of other enzymes with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula I may be employed for prevention or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels.

Abstract: This invention discloses and claims a compound conforming to the general formula (I): Wherein R1, R2, R?2, R3, R4 and R5 are as described herein. The compounds of the present invention exhibit an inhibitory effect on the production of ?-amyloid peptide (?-A4) by inhibition of gamma protease. Therefore, the compounds of the present invention are useful in the treatment of pathologies such as senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy and/or cerebrovascular disorders.

Abstract: Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to 3-amido-1,2-benzoisoxazole derivatives and their salts represented by formula 1, processes for preparation and usees thereof. More particularly, it relates to a method for improving its bioavailability introducing amino acid residue to the amine group of a 3-amido-1,2-benzoisoxazole. The compounds according to the present invention are used as an antagonist against Leukotriene-B-4 receptor, an inhibitor or therapeutics of osteoroposis, thus inhibiting osteolysis and stimulating osteogensis.

Abstract: This invention provides methods of inhibiting plasminogen activator inhibitor-1 (PAI-1) in a mammal, utilizing compounds of the formula: wherein: A is C or N; B is O, S, N, or CH?CH; X is CO, CH(OH), CH2, or —CH—S-2-benzothiazole; Y is H, alkyl, or halo; Z is O, S, or N; R is H, nitro, alkyl, alkoxy, halo, or CF3; R1 is alkyl, aryl, aralkyl, halo, Het-alkyl, or optionally substituted aryl; Het is G is O, S, or N; R2 is H, halo, alkyl, or —OR5; R3 and R4 are H, halo, alkyl, aryl, nitro, amino, alkylsulfoamide, arylsulfoamide, cycloalkyl, heterocycle, or optionally substituted aryl; R5 is H, alkyl, —CH(R7)R8, —C(CH2)nCO2R9, —C(CH3)2CO2R9, CH(R7)(CH2)nCO2R9, or —CH(R7)C6H4CO2R9; R6 is alkylene; R7 is H, alkyl, aryl, aralkyl, cycloalkyl, phthalic acid, or Q-alkyl; Q is R8 is —CO2R11, —CONHR11, tetrazole, or —PO3R11; R9 is H, alkyl, aryl, or aralkyl; W is O, N, or S; R11 is H, alkyl, aryl, or aralkyl; n=1-6; or a pharmaceutically acceptable salt or ester form thereof.

Abstract: The present invention relates to a class of substituted 1,2,4-triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.

Abstract: Thiaxozle, oxazole, imidazole, isoxazole and isoxazoline compounds of the formula wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is selected from the various optionally substituted aromatic radicals defined in the specification, B is hydrogen, alkyl or phenyl, R1 and R2 are independently hydrogen, alkyl or cycloalkyl or R1 and R2 taken together with the carbon atom which carries them, form a carbocycle with 3 to 7 members and ? is —NH46R47 or —OR48, R46 and R47 are independently hydrogen, alkyl, cycloalkyl or —(CH2)kCOOR51, R51 is alkyl or haloalkyl and R48 is hydrogen or alkyl having advantageous pharmacological properties which allow their use in therapeutics, for treating neurodegenerative disorders or pain.

Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.

Abstract: Progesterone receptor modulators of formula I, or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein, are useful for contraception and hormone replacement therapy are described. Also provided are products containing these compounds.

Abstract: Compounds represented by formula (I) wherein all symbols represent the same meanings as described in specification and salts thereof. Since the compound represented by the formula (I) binds and antagonizes to DP receptor, it is useful for the prevention or treatment against the disease such as allergic disorder, diseases accompanied with itching, secondary diseases generated by behaviors caused by itching, inflammation, chronic obstructive pulmonary disease, ischemic reperfusion disorder, pleuritis complicated by rheumatoid arthritis, cerebrovascular disease, and ulcerative colitis.

Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.

Abstract: This invention provides O-?-acyloxyalkyl ethers of the venlafaxine metabolite 4-[2-(Dimehtylamino-1-(1-hydroxycyclohexyl)ethyl]phenol, represented by Formula (I): wherein the variables R1 and R2 are defined herein, and where the configuration at the steriogenic center (*) may be R, S, or RS (the racemate).

Abstract: The present invention relates to compounds having the formula: salts thereof; compositions comprising one or more of the compounds and/or salts thereof; methods of using; and methods of making.

Abstract: Novel 3,3-diphenylpropylamines of the formula and stereoisomers and physiologically acceptable acid addition salt thereof; wherein R1, R2, R3, R4, R5, and R6 are as defined herein; methods of use thereof; and pharmaceutical compositions thereof.

Abstract: Methods of forming germicidal aromatic dialdehydes by hydrolyzing acetals are disclosed. Compositions and kits including both germicidal aromatic dialdehydes and acetals that are capable of being converted to germicides are disclosed. In one aspect, an acetal may be converted to germicide gradually in a deployed germicidal solution to accommodate for loss of the germicide or otherwise to modify the germicidal efficacy of the deployed germicidal solution.

Abstract: Pharmaceutical compositions containing plant essential oils, natural or synthetic, or mixtures or derivatives thereof, for the prevention and treatment of soft tissue cancer in mammals.

Abstract: An aqueous viscoelastic surfactant (VES) fluid foamed or energized with carbon dioxide, in which the VES is more compatible with the carbon dioxide, is made by the addition of one or more than one synergistic co-surfactant. The synergist co-surfactant includes quaternary amines and ethoxylated carboxylates having a hydrophobic chain shorter than the hydrophobic chain of the VES. Improved compatibility is evidenced for a given surfactant concentration either by formation and maintenance of a foam under conditions at which the foam could not otherwise have been formed or maintained, or by either higher viscosity of the foamed fluid at a given temperature or longer foam life at a given temperature or a higher temperature at which useful fluid viscosity can be generated or maintained for a useful time. The aqueous carbon dioxide foamed fluids may be used in acidizing, acid fracturing, gravel packing, diversion, and well cleanout.

Abstract: A sol having high oxidation purity and containing diantimony pentoxide particles having a primary particle size of from 2 to 50 nm and a Sb2O3/Sb2O5 weight ratio of at most 4 wt % is prepared by reacting a diantimony trioxide with an aqueous hydrogen peroxide solution in the presence of tunastate or molybdate.

Abstract: Synthetic methods for the preparation of hydrophobic organics aerogels. One method involves the sol-gel polymerization of 1,3-dimethoxybenzene or 1,3,5-trimethoxybenzene with formaldehyde in non-aqueous solvents. Using a procedure analogous to the preparation of resorcinol-formaldehyde (RF) aerogels, this approach generates wet gels that can be dried using either supercritical solvent extraction to generate the new organic aerogels or air dried to produce an xerogel. Other methods involve the sol-gel polymerization of 1,3,5 trihydroxy benzene (phloroglucinol) or 1,3 dihydroxy benzene (resorcinol) and various aldehydes in non-aqueous solvents. These methods use a procedure analogous to the one-step base and two-step base/acid catalyzed polycondensation of phloroglucinol and formaldehyde, but the base catalyst used is triethylamine. These methods can be applied to a variety of other sol-gel precursors and solvent systems.

Abstract: Compounds of formula (I), wherein R1 is hydrogen or alkyl; R2 is C1-C4alkoxy or a morpholino radical; and R3 is hydrogen or C1-C4alkoxy, are suitable for improving the solubility of specific photoinitiators in formulations and accordingly enhance the storage stability of formulations comprising a photoinitiator and compounds of formula (I)

Abstract: A polymerization process with elevated productivity using a coordination catalyst, wherein electromagnetic radiation is applied during polymerization. The irradiation of light greatly increases the activity of the coordination catalyst.

Abstract: An ultraviolet (UV) light curable formulation useful for repairing composite materials, comprising: an acrylic oligomer, an acrylic monomer, and a photoinitiator. This formulation may include fiberglass. The photoinitiator can be a combination of a bis-acylphosphine oxide and an alpha hydroxy ketone. The formulation can cure rapidly, such as in about 20 minutes. The cured formulation can have a Tg above 150° C.

Abstract: An ultraviolet (UV) light curable formulation useful for repairing composite materials, comprising: an acrylic oligomer, an acrylic monomer, and a photoinitiator. This formulation may include fiberglass. The photoinitiator can be a combination of a bis-acylphosphine oxide and an alpha hydroxy ketone. The formulation can cure rapidly, such as in about 20 minutes. The cured formulation can have a Tg above 150° C.

Abstract: The present invention relates generally to radiation-curable ink formulations, and particularly, but not by way of limitation, to a family of radiation-curable ink formulations specifically for flexographic and screen printing applications. The inventive ink formulations are based on multifunctional acrylate resins formed by the reaction of acrylate monomers and oligomers with ?-keto esters (e.g., acetoacetates), ?-diketones (e.g., 2,4-pentanedione), ?-keto amides (e.g., acetoacetanilide, acetoacetamide), and/or other ?-dicarbonyl compounds that can participate in Michael addition reactions.

Abstract: There are provided a water dispersion for ink-jet printing comprising colorant-containing water-insoluble graft polymer particles in which the water-insoluble graft polymer contains a main chain which is a polymer chain containing a constitutional unit derived from a salt-forming group-containing monomer (a) and a constitutional unit derived from an aromatic ring-containing (meth)acrylate monomer (b), and a side chain which is a polymer chain containing a constitutional unit derived from a hydrophobic monomer (c); a water-based ink for ink-jet printing using the water dispersion; and an ink-jet printing method using the water-based ink. In accordance with the present invention, printed images or characters formed on a coated paper are excellent in gloss, image clarity and image clarity property including both of the image clarity and the gloss, and printed images or characters formed on an ordinary paper exhibit a high print density.

Abstract: TAC and additives are mixed in a mixture solvent of dichloromethane, methanol and n-butanol to obtain a dispersion solution. The dispersion solution is heated to become a low concentration dope whose concentration is 19.3 wt. %. The low concentration dope is fed with a pump, and supplied through a flash nozzle to a concentrating apparatus to performing flash evaporation of the solvent in the concentrating apparatus. Thus part of the solvent in the low concentration dope evaporates to obtain a condensed dope. The part of the solvent is condensed on a condensation surface to obtain a condensed solvent. The condensed solvent flows through a pipe out of the concentrating apparatus. The high concentration dope has a solid content of 22.3 wt. %, and drawn through a pump. As the solid content of the high concentration dope is high, a polymer film having the self-supporting property can be easily formed of the high concentration dope in a film production line.

Abstract: A polymeric composite is provided which has improved stain preventative properties by virtue of inclusion of at least one compound having multiple functional groups capable of reacting with tannins contained in a tannin containing cellulosic material present in the composite, and a method for its production and prevention of water stains thereon.

Abstract: The present invention discloses mono-, bis- and tris-nonylcyclohexylphosphite esters, polyolefin compositions stabilized against the deleterious effects of melt processing, heat aging and exposure to combustion products of natural gas which comprise the nonylcyclohexylphosphite esters as stabilizers, and a process towards stabilizing polyolefin compositions by incorporating in or applying thereto the nonylcyclohexylphosphite esters.

Abstract: A conductive roller or a conductive belt is composed of a conductive elastomer composition including a polymer composition having a plurality of carbon-to-carbon double bonds and containing not less than 40 mol % of ethylene oxide; an organometallic salt containing a fluoro group or/and a sulfonyl group; and an elastomer having a plurality of carbon-to-carbon double bonds.

Abstract: The invention relates to a multicomponent composition for photodegradable and biodegradable plastic articles, and the use of said composition in the manufacture of various disposable and packaging plastic articles and the articles made therefrom. The multicomponent composition does not contain starch, and is a multicomponent compounded composition of new bioactive material of chitin, casein and the like, with biodegradable aid component, photodegradable and auto-oxidation catalysis component, and nonmetallic minerals and the like. Under natural condition, the degraded material can be utilized by microorganism to release carbon dioxide and water, and acts as an eco-friendly plastic material.

Abstract: Processes for utilizing various emulsion polymerization procedures for preparing aqueous nanocomposite dispersions are disclosed. The disclosed processes include both in-situ polymerizations in the presence of at least partially exfoliated, lightly modified clays as well as admixtures of polymer dispersions with at least partially exfoliated, lightly modified clay dispersions. The disclosed nanocomposite dispersions are useful for preparing a variety of materials, such as coatings, adhesives, caulks, sealants, plastics additives, and thermoplastic resins. Processes for preparing polymer nanocomposite powders and use of these powders as plastic resin and plastics additives are also disclosed.

Abstract: The present invention has for its object to provide an emulsion polymer resin composition adapted to give a coating film having an excellent appearance in terms of gloss, image sharpness, and apparent thickness, be satisfactory in curability and storage stability, contribute to cost reduction, express satisfactory coating film properties such as hardness, high impact resistance, scratch resistance, acid rain resistance, and weather resistance, and be conducive to a reduced VOC level, a curable composition comprising the above emulsion polymer resin composition and a crosslinking agent, and a cured coating film formed from the above curable composition. The present invention is an emulsion polymer resin composition which contains a hydroxyl group and a functional group reactive with the hydroxyl group within the same particle and has a weight average molecular weight of not less than 10000 but not more than 500000.

Abstract: The present invention relates to a multistage process including at least two steps for making a heat and oil resistant preroxide-cured thermoplastic vulcanizates (TPV) based on hydrogenated carboxiated nitrile butadiene rubber (HXNBR) and at least one polyamide. TPV's according to the present invention have improved properties and morphology over known TPV's prepared in single-stage processes.