Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods For inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: This invention provides methods for using novel substituted pyrimidine compounds, derivatives and analogs thereof to treat diseases such as cancer. Examples of compounds and derivatives for use in the methods are (E)-5-(2-bromovinyl)-2?-deoxy-5?-uridyl phenyl L-alaninylphosphoramidate and (E)-5-(2-bromovinyl)-2?-deoxy-5?-uridyl phenyl L-alaninyl monophosphate.

Abstract: The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.

Abstract: The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing, whether chronobiologic or light-induced, and in particular skin ageing caused by decrease of skin elasticity and/or by collagen degradation in the structure of tissues.

Abstract: Methods and compositions for enhancing the activity and/or duration of action of soft anti-inflammatory steroids of the haloalkyl 17?-alkoxy-11?-hydroxyandrost-4-en-3-one-17?-carboxylate type and the corresponding ?1,4 compounds and of anti-inflammatory steroids of the hydrocortisone and prednisolone type are described. The enhancing agents have the formula: wherein R is H or C1-C4 alkyl; Z1 is carbonyl or ?-hydroxymethylene; X1 is —O— or —S—; R5 is —OH, —OR6, —OCOOR6 or —OCOR7 wherein R6 is C1-C4 alkyl and R7 is C1-C4 alkyl, fluoromethyl or chloromethyl; and the dotted line in ring A indicates that the 1,2-linkage is saturated or unsaturated; with the proviso that when R is C1-C4 alkyl, then R5 is —OH.

Abstract: The invention relates to new 2-substituted estra-1,3,5(10)-trien-17-ones of formula I as well as their pharmaceutically acceptable salts, their methods of manufacture and use as medicaments for prophylaxis and/or therapy of estrogen-dependent diseases that can be influenced by the inhibition of 17?-hydroxy steroid dehydrogenase type 1.

Abstract: A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.

Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogen

Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I

Abstract: Pharmaceutically active diazepanes, e.g. useful for treating disorders or diseases mediated by LFA-1/ICAM-1, LFA-1/ICAM-2, LFA-1/ICAM-3 or LFA-1/JAM-1 interactions.

Abstract: This invention is directed to a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, Z, m, n, o, p and r are as defined herein, its preparation, pharmaceutical composition and use as an adenosine A3 receptor ligand preferably an antagonist.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R, R1, R2, R5, R6a, R6b, J, K, X and Z are as described in the specification.

Abstract: The invention relates to heterocyclic derivatives of formula (I), wherein R2 is amino, a group OR4 or a group —Y—R5 where R4 is hydrogen or C1-4alkyl, Y is C1-4alkylene, R5 is hydrogen, halo, hydroxy, C1-2alkoxy, C1-2alkoxyC1-2alkoxyC1-4, or a group NR7R8 where R7 and R8 are independently selected from hydrogen, C1-2alkyl, hydroxyC1-2alkyl or alkoxyC1-2alkyl, or R7 and R8 together with the nitrogen atom to which they are attached form a saturated 5-6-membered heterocyclic ring which optionally contains an additional heteroatom; n is one or two and each R1 is independently selected from halo, haloC1-2alkyl, hydroxy, oxo, amino, C1-2alkylamino or di-C1-2dialkylamino; or a pharmaceutically acceptable salt thereof. These compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals.

Abstract: The present invention is directed to fused-aryl and heteroaryl derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: The instant invention relates to a combination of an alpha-2-delta ligand and a PDEV inhibitor for use in therapy, particularly in the treatment of pain, particularly neuropathic pain. Particularly preferred alpha-2-delta ligands are gabapentin and pregabalin. A particularly preferred PDEV inhibitors is sildenafil.

Abstract: The present invention relates to crystalline forms of 5-chloro-6-{2,6-difluoro-4-[3-(methylamino)propoxy]phenyl}-N-[(1S)-2,2,2-trifluoro-1-methylethyl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine salts; processes for the production thereof; pharmaceutical compositions thereof; and methods for inhibiting tumor growth therewith.

Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Abstract: The invention relates to pyrimidines and uses thereof, including to inhibit lysophosphatidic acid acyltransferase ? (LPAAT-?) activity and/or proliferation of cells such as tumor-cells.

Abstract: Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.

Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.

Abstract: 7-azaindoles inhibit phosphodiesterase 4 (PDE4). Methods for preparing these compounds are also provided.

Abstract: The present invention relates to a compound represented by Formula (I): and pharmaceutically acceptable salts. Compounds of the present invention inhibit Aurora kinase, making them especially suitable for the treatment of a number of diseases, including solid tumor cancers and hematological cancers.

Abstract: The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: Certain novel piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

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: A method of treating angiogenesis-implicated disorders by selecting a subject predisposed to an angiogenesis-implicated disorder and then administering an effective amount of an endogenous aryl hydrocarbon receptor ligand or its analogs according to a formula as disclosed herein is disclosed.

Abstract: The invention relates to triazolo-thiazole analogues of epothilone A and epothilone B.

Abstract: Compounds of Formula 1 where X is S and the variables have the meaning defined in the specification are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors, and as such have no or only minimal cardivascular and/or sedatory activity. These compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2B adrenergic receptors. Compounds of Formula 1 where X is O also have the advantageous property that they have no or only minimal cardivascular and/or sedatory activity and are useful for treating pain and other conditions with no or only minimal cardivascular and/or sedatory activity.

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazole compounds represented by Formula (II): are useful in providing compounds to assay for such therapeutically useful compounds.

Abstract: Pharmaceutical compositions of a benzimidazole or a benzimidazole derivative are disclosed. For example, in certain embodiments the pharmaceutical compositions include a benzimidazole, PEG 400, and a dipolar aprotic solvent. In other embodiments, pharmaceutical compositions include a benzimidazole, an oil, a dipolar aproptic solvent, and a surfactant. In certain embodiments, the benzimidazole is mebendezole. The pharmaceutical compositions are formulated for delivery to a subject by any means, and include formulations for oral and parenteral delivery.

Abstract: The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.

Abstract: Therapeutic methods of treatment, compositions and foodstuffs are described which contain isoflavone compounds described by general formula (I), 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.

Abstract: 1,2-substituted 5-pyrrolidinone compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, renal dysfunction, an immune deficiency disorder, dry eye, ichthyosis, elevated intraocular pressure, sleep disorder, or gastric ulcer, inflammatory disorders and other diseases and disorders associated with the prostaglandin family of compounds.

Abstract: Aminophosphonate and amino bisphosphonate compounds and methods for their preparation are provided. Also provided are pharmaceutical and agricultural compositions containing the compounds. The compounds and compositions are useful in methods for treatment of various diseases, including, inflammation, autoimmune disease, cardiovascular disease, bacterial infection, viral disease, abnormal cell proliferation, bone resorption disease, osteoporosis, or parasitic disease and in various agricultural methods, including, methods of eradicating weeds.

Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.

Abstract: Compounds that provide for sustained systemic concentrations of GABA analogs following oral administration to animals are disclosed. Pharmaceutical compositions including, and methods using, such compounds are also disclosed.

Abstract: The present invention is directed to a procedure for making an enantiomerically enriched compound containing a hydronaphthalene ring structure. The process involves reacting oxabenzonorbornadienes with nucleophiles using rhodium as a catalyst and in the presence of a phosphine ligand. The compounds synthesized may be used in pharmaceutical preparations for the treatment of a variety of diseases and conditions.

Abstract: A process for producing synthetic hydrocarbons that reacts carbon dioxide, obtained from seawater of air, and hydrogen obtained from water, with a catalyst in a chemical process such as reverse water gas shift combined with Fischer Tropsch synthesis. The hydrogen is produced by nuclear reactor electricity, nuclear waste heat conversion, ocean thermal energy conversion, or any other source that is fossil fuel-free, such as wind or wave energy. The process can be either land based or sea based.

Abstract: The photocurable resin composition in the first aspect of the invention comprises, as essential components, (A) a binder resin having photopolymerizable functional groups and (B) inorganic superfine particles in the order of sub-micron which can be dispersed in a colloidal form; the photocurable resin composition in the second aspect comprises, as essential components, (C) a binder resin containing photopolymerizable functional groups and (D) hydrophobic fine silica particles; and the photocurable resin composition in the third aspect comprises, as essential components, (E) a binder resin containing acrylic resin and urethane acrylate resin and/or polyester acrylate having photopolymerizable functional groups and (F) an organometallic coupling agent.

Abstract: An ink set comprises a black ink which contains a black pigment, resin particles having carboxyl group, a first pH-adjusting agent, a water-soluble organic solvent, and water, and a color ink which contains a coloring pigment, resin particles, a second pH-adjusting agent, a water-soluble organic solvent, and water. The pH of the black ink is not less than 7.8, and the pH of the color ink is not more than 4.5. Any bleeding of the black ink is not caused even when an image is formed on a cloth or the like with the ink set. Even when the cloth is washed, then the ink is not lost from the image formation objective, and the initial image density is maintained.

Abstract: The invention relates to dialkylphosphinic salts of the formula (I) where R1, R2 identical or different, are C1-C6-alkyl, linear or branched M is Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Li, Na, K and/or is a protonated nitrogen base; m is from 1 to 4; wherein the telomer content is from 0.01 to 6% by weight. The invention also relates to glare use in flame retardant compositions, and to flame-retardant polymer molding compositions and flame-retardant polymer moldings which comprise these dialkylphosphinic salts.

Abstract: Polymerized oils (heat-bodied oils) were hydrogenated to make a semi-crystalline wax-like material. The process of the present invention yields hydrogenated polymerized oils that can be used as bio-renewable replacements for micro-crystalline wax and petrolatums raw materials in products that are comprised of such materials. The present invention is directed to a composition comprising a hydrogenated polymerized oil, a composition consisting essentially of a hydrogenated polymerized oil and a process of preparing a hydrogenated polymerized oil. The present invention is also directed to a composition comprising a hydrogenated blown oil, a composition consisting essentially of a hydrogenated blown oil and a process for preparing a hydrogenated blown oil.

Abstract: Described is a low-emission adhesive, whose polymers are dissolved in a mixture of acetone and ethanol. The adhesive is characterized by very low emissions of solvents, with otherwise equally good properties compared to standard solvent-synthetic resin based adhesives. In particular with respect to viscosity and spreadability, surface tension, depth of penetration, wettability, simplicity and speed of processing, as well as adhesion, gluing strength and adhesive spectrum, the adhesive of the invention is equal to other adhesives based on solvents and thus superior to dispersion-adhesives that are based on aqueous solutions. Due to its low solvent emissions and absence of chlorinated solvents, the present adhesive is suitable for applications for which only dispersion-adhesives that are based on aqueous dispersions were reserved until now. This is true in particular for applications in enclosed spaces. The adhesive is very suitable for gluing of wooden floors in internal construction work.

Abstract: Polymeric compositions and methods of making same having improved coefficient of friction and blocking properties. The polymeric compositions include a linear low density polyethylene with additives such as a fluoroelastomer and an acid scavenger. The polymeric compositions may further comprise other additives such as antiblock agents, slip agents, stabilization additives, or combinations thereof. The methods include adding additives such as a fluoroelastomer and an acid scavenger to a polymer resin and forming end use articles such as film from the polymeric compositions.

Abstract: Toughened compositions from polyhydroxyalkanoate (PHA), preferably PHB reactively blended with maleated poly butadiene and with an epoxidized natural or synthetic rubber are described. The compositions preferably include clay nanoparticles which can be organically modified and can be exfoliated by the blend. The compositions can be used in a variety of applications, including automotive uses.

Abstract: The rubber composition and the material suitable for preparing the rubber composition show high gas-barrier properties and being free from inhibition of vulcanization. The rubber composition is essentially composed of a rubber and a layered mineral filler treated with short chain alkyl ammonium salt.

Abstract: A mixture of at least two compounds each having at least two double bonds, said mixture having a WFR from 200 to 600 g/mol of double bond and at least two of said compounds each comprising at least two (meth)acrylic esters as double bond component, WFR being given by: ? i = 1 n ? ? i ? MW i / Z i = WFR ? ? where ? ? i = 1 n ? ? i = 1 ?i is equal to the molar fraction of compound (i) in said mixture, n is equal to the number of compounds in said mixture and n is ?2, Zi is equal to the number of double bonds in said compound (i), MWi is equal to the molecular weight of said compound (i).

Abstract: The object of the invention is to provide a means to enhance the drying property of a coating film formed as a vibration damper and repressing the occurrence of crack and expansion in the surface of the coating film. The task mentioned above is accomplished by using a thickener for vibration damper, which contains a polymer comprising an alkali-soluble monomer unit and an associating monomer unit. The alkali-soluble monomer unit may possess a carboxyl group, a sulfonic acid group, or a phosphoric acid group, or a salt thereof. The associating monomer unit may possess in a side chain thereof a group represented by the formula, —(R1—O)n—X—R2, (wherein R1 denotes methylene group, ethylene group, propylene group or butylene group, n denotes a number in the range of 10-300, X denotes a direct bond, —C(?O)—, or —C(?O)NH—, and R2 denotes a hydrocarbon group of 6-30 carbon atoms).

Abstract: A silicone composition comprising (A) an organopolysiloxane having at least one lower alkenyl group in a molecule, (B) an organohydrogenpolysiloxane having at least two SiH groups in a molecule, (C) a platinum catalyst, and (D) at least one compound selected from among indoline, 1,2,3-triazole, 1,2,4-triazole, imidazole, indazole, benzoxazole, 2-hydroxybenzoxazole, 5-benzyloxyindole, 1,2-benzisoxazole, 2,1-benzisoxazole, and 1,3-benzodioxole cures effectively into a transparent rubbery or gel product having flame retardance.

Abstract: In order, in the case of a moulding composition for the production of sanitary-ware components, comprising a methyl-methacrylate-based syrup and from 50 to 85%, expressed in terms of the moulding composition, of an inorganic filler, to obtain an improvement in the scratch-proofness and the abrasion resistance of the shaped components which are obtained therefrom, it is proposed that the composition furthermore comprise elastomer particles or elastomer particle aggregates having a particle size <100 ?m in an amount in the range of 5% by weight to <20% by weight, expressed in terms of the mass of the syrup.