Abstract: A series of quinoline and quinoxaline derivatives, substituted by a fused bicyclic pyridine or pyrimidine moiety attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

Abstract: The invention provides an agent for promoting ocular tissue neuritogenesis, containing N-(1-acetylpiperidin-4-yl)-4-fluorobenzamide or a pharmaceutically acceptable salt thereof, and an agent for promoting corneal neuritogenesis and retinal neuritogenesis, containing N-(1-acetylpiperidin-4-yl)-4-fluorobenzamide or a pharmaceutically acceptable salt thereof. The corneal neuritogenesis promoter can be used for the improvement of corneal sensitivity, treatment of dry eye, or treatment of a corneal epithelial disorder. The retinal neuritogenesis promoter can be used for the improvement of a visual dysfunction.

Abstract: This invention is directed to derivatives of piperidine-2,6-dione, or their organic or inorganic salts thereof, a methods of synthesis of these derivatives, and their application as active pharmaceutical ingredient as inhibitors of TNF? releasing in cells, the derivative of piperidine-2,6-dione being of the general formula (I): wherein n represents 1, 2, 3, 4, 5 or 6; R1 represents from one to four of the same or different substituents selected from F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), N(C1-4 alkyl)2; R2 represents OR3, NR3R4, N(R3)COR4, O2CR5; R3 and R4 represent independently and at each occurrence H or C1-4 alkyl; R5 represents CHR6NR7R8, CHR6NR9C(O)CHR10NR7R8, a heterocycle W or CHR6NR9C(O)W; R6, R9, R10 represent independently and at each occurrence H, or C1-4 alkyl; R7 and R8 represent independently and at each occurrence H, C1-4 alkyl, or R7 and R8 taken together represent 1,3-propylene, 1,4-butylene, 1,5-pentylene, or 1,6-hexylene; W represents four-m

Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.

Abstract: Compounds of formula (I) inhibit HDAC activity, wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.

Abstract: A compound of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Cycloheteroalkenyl Compound”); compositions comprising an effective amount of a Cycloheteroalkenyl Compound; and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Cycloheteroalkenyl Compound are disclosed herein.

Abstract: The present invention encompasses compounds of general formula (1) while the groups R4 to R7 and the units W, L, Qa and QH are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.

Abstract: Disclosed are compounds and compositions of the formula (I) as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula (I).

Abstract: The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.

Abstract: This invention pertains to methods for protecting a propagule or a plant grown therefrom from invertebrate pests comprising contacting the propagule or the locus of the propagule with a biologically effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention also relates to propagules treated with a compound of Formula I and compositions comprising a Formula I compound for coating propagules.

Abstract: A compound of Formula (I): salts thereof, prodrugs thereof, metabolites thereof, pharmaceutical compositions containing such a compound, and use of such compound and compositions to treat diseases mediated by raf, VEGFR, PDGFR, p38 and flt-3.

Abstract: The invention provides methods for enhancing iodine absorption in a thyroid in a subject and treating thyroid cancer by administering to the subject a composition which includes a multi-kinase inhibitor. Furthermore, the invention provides methods for improving a medical diagnostic procedure based on radioactive iodine in a subject by administering to the subject a composition comprising a multi-kinase inhibitor.

Abstract: The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of ?-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.

Abstract: Provided herein are compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.

Abstract: A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which has a PI3 kinase ? inhibitory effect and is useful as a prophylactic or therapeutic agent for articular rheumatism, Crohn's disease, irritable colitis, Sjoegren's syndrome, multiple sclerosis, systemic lupus erythematosus, asthma, atopic dermatitis, arteriosclerosis, organ transplant rejection, cancer, retinopathy, psoriasis, arthrosis deformans, age-related macular degeneration, type II diabetes, insulin resistance, obesity, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), hyperlipemia, etc.

Abstract: The present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and the uses thereof. More specifically, the present invention relates to novel thiazolidinedione derivatives expressed by the following formula (I) and a pharmaceutical composition comprising the same. The novel thiazolidinedione derivatives of formula (I) according to the present invention can be effectively used for the prevention or treatment of cardiovascular disease, gastrointestinal disease and renal disease by inhibiting the activity of 15-hydroxyprostaglandin dehydrogenase (15-PGDH) that decomposes prostaglandins as well as useful for the prevention of hair loss and the stimulation of hair growth, and osteogenic stimulation and wound healing.

Abstract: The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by —Y1-A1- or —Y2—C(?O)— wherein Y1 is a group such as —C(?O)—, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.

Abstract: The present invention features imidazolidinone compounds and pharmaceutical compositions of imidazolidinone compounds. The compounds of the invention are utilized in methods of treating a deubiquitination-related disorder in a subject and inhibiting p97-associated deubiquitination.

Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract: The invention relates to methods for detecting the presence of a compound of formula I in a biological test sample: where R2, R3, and R4 are as defined in the specification; or a salt thereof.

Abstract: Invented is a method of treating cancer or a pre-cancerous syndrome in a mammal, including a human, in need thereof which comprises the administration of an effective amount of a non-peptide thrombopoietin (TPO) receptor agonist to such mammal, suitably a human.

Abstract: The present invention provides a method for inducing apoptosis in selected cells by aggravating ER-stress. The aggravation of ER-stress is achieved in a specific manner by inhibiting SERCA (sarcoplasmic/endoplasmic reticulum calcium ATPase), leading to elevated level of cytoplasmic calcium concentration, yet without inhibiting the activity of COX-2 (cyclooxygenase-2) or triggering the release of histamine. Induction of apoptosis may be enhanced by first inducing or further aggravating ER-stress through inhibition of proteasome or proteases. Also provided are compounds and compositions useful as ER-stress aggravating agents, methods for screening, selecting, identifying and designing the same and methods for treating diseased conditions by inducing apoptosis through specific and selective aggravation of ER-stress.

Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.

Abstract: A composition comprised of an active agent that is 4-methoxy-N-(3,5-bis-(1-pyrrolidinyl)-4-hydroxy benzyl)benzene sulfonamide or a pharmaceutically acceptable salt thereof is intravenously administered to a subject, substantially evenly over a period of greater than about 15 minutes, to avoid disadvantageous hemodynamic effects, including systemic diastolic and systolic hypotension, to can occur with rapid intravenous or even short-term infusion administration of the active agent.

Abstract: This invention provides compounds, compositions and methods for treating a cognitive disorder or memory disorder in animals that result from aging or other neurodegenerative condition. In particular, compounds of this invention can stimulate neural cell growth, increased amounts of cells containing a key enzyme needed for production of the cholinergic neurotransmitter, and can improve memory and cognitive function in animals who have experienced a loss of memory or cognitive function.

Abstract: In one aspect, the invention relates to compounds of formula I: where Y, R1, R2, n, and Q are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

Abstract: The subject invention relates to novel soluble forms of planar ring structured organic compounds including flavonoids, and their production. The invention also includes the use of these novel formulations of planar ring structured organic compounds in the preparation of formulations and products. The invention also relates to a wide variety of applications of the formulations of the invention. The subject invention includes novel soluble forms and various formulations of flavonoids. Further, the invention includes novel methods of manufacturing the flavonoid formulations. The invention also relates to a wide variety of applications of the flavonoid formulations.

Abstract: A pharmaceutical composition comprising a docusate; an osmotic laxative; and a benzoate.

Abstract: Membrane transporter-targeted therapeutic agents and methods of making and using the same.

Abstract: Disclosed is a novel composition which has an effect on promoting production of collagen. The composition has high photostability and is free from side effects such as those of retinoids. Specifically disclosed is a composition for promoting collagen production which contains one or more compounds selected from the group consisting of D-aspartic acid, D-alanine, derivatives and/or salts thereof. The composition may be used for the purpose of suppressing and/or improving skin a condition. The skin condition may include but is not limited to photoaging and/or wrinkles. The composition may be used for an external preparation for the skin or food. The composition may be a composition for promoting type I collagen production.

Abstract: The invention relates to a new prescription of NAC in the treatment of endometriosis and of indications associated with endometriosis, in a human or mammalian animal patient. In addition an effective dose regimen of NAC in the treatment of endometriosis is proposed. In one embodiment of the present invention the prescribed treatment regimen may be used e.g. in order to control the frequency and the intensity of pain symptoms (dysmenorrhea, dyspareunia and acyclic chronic pelvic pain), to reduce the size of endometriotic lesions eventually up to their disappearance, to reduce recurrences after surgery and/or to improve fertility. Side effects of this treatment are virtually absent and, in particular, this treatment does not hinder pregnancy.

Abstract: The present invention relates to salts of 3-pentylphenylacetic acid and their pharmaceutical uses. Particular aspects of the invention relate to the use of those salts in the prevention and/or treatment of various diseases and conditions in subjects, including the prevention and treatment of (i) blood disorders, (ii) renal disorders and renal disorder complications; (iii) inflammatory-related diseases; and/or (iv) oxidative stress related disorders.

Abstract: The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.

Abstract: Benzamide derivatives of formulae I and II, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof, and pharmaceutical compositions comprising the same, are described and have therapeutic utility, particularly in the treatment of diabetes, obesity, and related conditions and disorders: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, and R12 are defined as provided herein.

Abstract: Desensitizing drug products, methods of making desensitizing drug products, and methods of using desensitizing drug products including delivery of desensitizing drug products. In one embodiment, the desensitizing drug products are male genital desensitizers that comprise one or anesthetic agents and one or more melting point depressing agents.

Abstract: Methods and reagents for the formation of disulfide bonds, particularly in proteins, peptides and amino acids. The methods and reagents are particularly useful for the controlled glycosylation of proteins, peptides and amino acids. The methods utilize thiosulfonate or selenenylsulfide compounds as reagents or intermediates. Some proteins and peptides comprising selenenyl-sulfide groups also form part of the invention.

Abstract: A first object of the invention is a process for thickening of an aqueous composition, through the introduction into the said composition for thickening of at least one polymer, characterized in that the said polymer contains at least one anionic monomer, which is an organophosphate monomer.

Abstract: Process for the preparation of ethanol and/or higher alcohols comprising the steps of: (a) providing an alcohol synthesis gas comprising carbon monoxide and hydrogen in a molar ratio of higher than 0.5; (c) adding an amount of methanol and/or higher alcohols to the synthesis gas to obtain a synthesis gas mixture. (d) converting the synthesis gas mixture from step (c) in presence of one or more catalysts catalysing the conversion of the synthesis gas mixture into a ethanol and/or higher alcohols containing product; and (e) withdrawing the product from step (d), wherein the synthesis gas is purified by removing iron and nickel carbonyl compounds prior or after the addition methanol and/or higher alcohols to the synthesis gas and optionally (I) cooling the withdrawn product in step (e); and (g) contacting the cooled product with a hydrogenation catalyst.

Abstract: The present invention relates to polyesters that can be prepared from renewable resources and/or recycled materials and the production process thereof. In particular, hydroxyl-functional or carboxyl-functional polyesters containing moieties of terephthalic acid and/or isophthalic acid, ethylene glycol, a dianhydrohexitol, and of one or more linear chain dicarboxylic acids are provided. Further, the polyesters have a number average molecular weight, as measured by gel permeation chromatography, of from 400 to 15000 daltons, more preferably from 550 to 15000 daltons. The polyesters of the invention can basically be prepared from recycled polyethylene terephthalate and from renewable polyacids and/or polyols. The present invention further provides a process to produce such polyesters via glycolysis of a polyethylene terepthalate and/or a polyethylene isophthalate with a dianhydrohexitol.

Abstract: A method of forming a porous material having improved compressive strength, includes forming an aerogel precursor that includes a polymer having a functional group capable of undergoing a crosslinking reaction dispersed in a dispersion medium. The precursor also includes a crosslinking agent. The aerogel precursor is frozen so that the dispersion is solidified, and freeze dried to sublime the dispersion medium and form the porous material. The crosslinking agent is reacted with the functional group to effect crosslinking, thus improving the compressive strength of the porous material.

Abstract: A process for the manufacture of a fiber or foil comprising at least one optionally functionalized polymer with a high Tg selected from the group consisting of poly(aryl ether sulfone) (PAES), poly(aryl ether ketone) (PAEK) and aromatic polyimide, comprising the steps of (aa) providing a solution comprising at least 45 wt. % of the polymer, and at least 20 wt. %, of at least one halogen-free organic solvent (S1) for the polymer, both wt % based upon the weight of the solution; (bb) pushing the solution through a nozzle; and (cc) introducing the solution into a coagulation bath comprising: (cc1) at least one liquid (L1) in which the polymer is insoluble, and optionally (cc2) at least one organic solvent (S2) for the polymer, identical to or different from the organic solvent (S1), to form a fiber or foil. A fiber or foil obtained by this process as well as to fibers or foils with specific porosity features and/or mechanical properties.

Abstract: An isocyanate reactive composition for making a polyurethane foam includes a tertiary amine urethane catalyst comprising a di(C1-C4)alkyl fatty alkyl amine and a polyester polyol. The use of one or more of fatty alkyl tertiary amine serves to reduce hydrolysis of the polyester polyol in the isocyanate reactive composition.

Abstract: Photoinitiator compounds comprising both a photoactive moiety and an amine functionality, bonded to a polyhedral oligomeric silsesquioxane, which photoinitiator is represented by formula (1) or (1?) wherein n is 2m; m is an integer of 2 to 30; the sum of n?+a is an integer 4-60; n? is an even-numbered integer; a is an even- or uneven-numbered integer; and for example different A C1-C12alkyl, or a photoactive moiety Q1, or a group of formula (2); E for example is a direct bond, L is linear or branched C1-C3alkylene, preferably propylene; R1 and R2 for example are a photoactive moiety Q, or C2-20alkyl; Q is for example a group of formula (4); Z2 is for example C1-C6alkylene which is unsubstituted or substituted by one or more OR6; and R6, R12, R13 and R14 for example are hydrogen; are especially suitable as low-migrating photoinitiators.

Abstract: A coating composition includes a UV curable film forming resin; a thixotropic and/or pseudoplastic anti-settling agent selected from at least one of an amine salt of a synthetic wax, a microcrystalline cellulose compound (MCC), a urea urethane, or a urethane enzymatically modified starch; a mar/scratch resistant additive selected from at least one of a mineral abrasive, glass particles, and ceramic particles; and water.

Abstract: Release agents with increased affinity toward nano-imprint lithography template surfaces interact strongly with the template during separation of the template from the solidified resist in a nano-imprint lithography process. The strong interaction between the surfactant and the template surface reduces the amount of surfactant pulled off the template surface during separation of a patterned layer from the template in an imprint lithography cycle. Maintaining more surfactant associated with the surface of the template after the separation of the patterned layer from the template may reduce the amount of surfactant needed in a liquid resist to achieve suitable release of the solidified resist from the template during an imprint lithography process. Strong association of the release agent with the surface of the template facilitates the formation of ultra-thin residual layers and dense fine features in nano-imprint lithography.

Abstract: An optical synthetic resin composed of: a synthetic resin; and fine particles dispersed in the synthetic resin at a ratio of 0.1 vol % or more to 50 vol % or less, each having a maximum length of 1 nm or more to 30 nm or less, in which part of surfaces of the fine particles are modified with functional groups which themselves repel each other, and a distance between two arbitrary adjacent fine particles among the fine particles is in a range of 0.1 nm or more to 500 nm or less. The two arbitrary adjacent fine particles attract each other with an intermolecular force, thereby making it possible to provide an optical composite deviating from an additivity range.

Abstract: In one aspect, the invention relates to silicone prepolymer compositions comprising a silicone prepolymer and a solvent. A soluble silicone prepolymer can be provided having increased average silicon content, thereby attaining a desired oxygen permeability. A solvent can be provided with a desired balance between hydrophilicity and hydrophobicity by selection and modification of the solvent molecular structure, resulting in molded polymer films and articles that exhibit minimal or nonexistent eye irritation and exhibit highly transparent products. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: A protective coating applied to the underwater portion of a marine vessel operable to inhibit the growth of marine foulants. The coating comprises a polymer, a marine biocide, a preservative, an antimicrobial agent, and optionally a coloring agent. In certain embodiments, the marine biocide, preservative, and optional antimicrobial agent are chemically bonded with the polymer thereby significantly reducing the ability of the biocide, preservative, and antimicrobial agent to leach from the coating into the surrounding environment.

Abstract: The present invention relates to a water dispersion for ink-jet printing including two kinds of carbon blacks (a) and (b) and a water-insoluble polymer which adheres to a surface of the respective carbon blacks (a) and (b), wherein the carbon black (a) has an acid group content of from 0 to 200 ?mol/g and the carbon black (b) has an acid group content of more than 200 ?mol/g but not more than 1000 ?mol/g, and a difference between acid group contents of the carbon blacks (a) and (b) is from 100 to 1000 ?mol/g, and a water-based ink for ink-jet printing which contains the water dispersion. The water-based ink is excellent in image density, fixing property, high lighter fastness, image uniformity, ejection reliability and storage stability.

Abstract: The invention relates to encapsulated rubber additives in the form of microcapsules having a polymer capsule wall and a core which comprises at least one rubber additive. The invention likewise relates to a method for the production of microcapsules of this type. The microcapsules according to the invention are used during vulcanization of natural and synthetic rubbers.