Abstract: The present invention provides multifunctional monomers, including, but not limited to include multifunctional methylene malonate and methylene beta-ketoester monomers; methods for producing the same; and compositions and products formed therefrom. The multifunctional monomers of the invention may be produced by transesterification or by direct synthesis from monofunctional methylene malonate monomers or methylene beta-ketoester monomers. The present invention further compositions and products formed from methylene beta-ketoester monomers of the invention, including monomer-based products (e.g., inks, adhesives, coatings, sealants or reactive molding) and polymer-based products (e.g., fibers, films, sheets, medical polymers, composite polymers and surfactants).

Abstract: Killing of bed bugs is accomplished by bringing the bed bugs into contact with a toxic amount of at least one of the compounds of the structure (I) wherein X is —OH, ?O, or —O(O)CR, wherein R is selected from H and a branched or straight chain, saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 11 carbon atoms; R1 is H or CH3; R2 is H or CH3; R3 is H or a branched or straight chain, saturated or unsaturated hydrocarbyl group with zero to three double bonds and from 1 to 11 carbon atoms; and wherein the compounds of structure (I) contain from 6 to 20 total carbon atoms in the compounds.

Abstract: Provided herein are novel solid state forms of tapentadol salts, process for their preparation, pharmaceutical compositions, and method of treating thereof. The tapentadol salts include an L-(?)-camphorsulfonate salt, a dibenzoyl-(L)-tartrate salt, a dibenzoyl-(D)-tartrate salt, a malate salt, a maleate salt, or a salicylate salt.

Abstract: Process for the preparation of racemic ?-amino acids or of glycine, wherein the corresponding ?-hydroxycarboxylic acid, selected from hydroxyacetic acid, lactic acid, malic acid, ?-hydroxyglutamic acid, isocitric acid, tartronic acid and tartaric acid, or at least one salt of the corresponding ?-hydroxycarboxylic acid is reacted in the presence of at least one heterogeneous catalyst which comprises at least one transition metal, in the presence of hydrogen with at least one nitrogen compound (c), where the nitrogen compound (c) is selected from primary and secondary amines and ammonia.

Abstract: A novel process is described which allows N-isopropyl(meth)acrylamide to be obtained in high purity and yield in a simple manner, by reacting methacrylic anhydride with isopropylamine, optionally in a solvent.

Abstract: A novelprocess for the preparation of N—[N-[3-(3-hydroxy-4-methoxyphenyl)-propyl]-L-?-aspartyl]-L-phenylalanine-1-methyl ester is described. It comprises, reacting isovanillin or its derivative with vinyl acetate followed by reductive condensation with L-[?-aspartyl]-L-phenylalanine-1-methyl ester.

Abstract: Mew tranilast complexes and new tranilast cocrystais are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di?hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.

Abstract: The invention provides new polymorphs of N—[(R)-1-[(S)-1-(4-aminomethyl-benzylcarbamoyl)-2-phenyl-ethylcarbamoyl]-2-(4-ethoxy-phenyl)-ethyl]-benzamide hydrochloride, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.

Abstract: A method for producing xylylene diisocyanate includes a thermal decomposition step of thermally decomposing xylylene dicarbamate; a first separation step of separating, from the thermal decomposition product obtained in the thermal decomposition step, an isocyanate-containing component containing xylylene diisocyanate as a main component and an alcohol-containing component containing alcohol as a main component and containing xylylene diisocyanate as a subcomponent; a second separation step of separating xylylene dicarbamate and alcohol from the alcohol-containing component obtained in the first separation step; and a returning step of returning xylylene dicarbamate obtained in the second separation step to the thermal decomposition step.

Abstract: Augmented or synergized anti-inflammatory constructs are disclosed including terpenes covalently conjugated with other anti-inflammatory molecules such as nonsteroidal anti-inflammatory drugs, vanilloids, amino acids and polyamines; and anti-inflammatory molecules covalently conjugated with specific amino acids. For the latter, further conjugation with a choline bioisostere further augments the anti-inflammatory activity.

Abstract: Disclosed is a urea plant comprising an additional reactor. With reference to the regular components of a urea plant, including a recovery section and a high pressure carbamate condenser, the additional reactor is positioned between the recovery section and the high pressure carbamate condenser. The invention also relates to a process for the synthesis of urea, comprising an additional reaction step converting, at an earlier stage than conventional, recovered carbamate into urea.

Abstract: A method for producing compounds containing a bis(perfluoroalkylsulfonyl)methyl group or salts thereof, wherein the compounds have high acidity and hydrophobicity and are useful as raw material compounds for a resin.

Abstract: Compositions comprising branched C10 mercaptans selected from the group consisting of 5-methyl-1-mercapto-nonane, 3-propyl-1-mercapto-heptane, 4-ethyl-1-mercapto-octane, 2-butyl-1-mercapto-hexane, 5-methyl-2-mercapto-nonane, 3-propyl-2-mercapto-heptane, 4-ethyl-2-mercapto-octane, 5-methyl-5-mercapto-nonane, and combinations thereof.

Abstract: Biodegradable computed tomography (CT) contrast agents comprising a polyiodinated aryl contrast agent that is crosslinked by an organic disulfide are described herein. The contrast agents can be used to image a tissue region by administering an effective amount of the biodegradable CT contrast agent to a subject, allowing a sufficient amount of time for the biodegradable CT contrast agent to enter the tissue region, and performing x-ray computed tomography imaging of the tissue region of the subject.

Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

Abstract: The present invention relates to a compound of Formula (I) or (II) or a salt thereof, wherein R is described herein. The compounds are novel hydroxy-proline analog inhibitors of the ASCT1 and ASCT2 neutral amino acid transporters.

Abstract: The present invention provides compounds belonging to 3-acyloxyindole compounds or 3-acyl-4-hydroxycoumarin compounds, a tautomer or geometric isomer thereof, or a salt thereof and methods for producing the same, which compounds are useful as antibacterial agent and as therapeutic drugs against infectious diseases.

Abstract: Indirubin is the major active anti-tumor component of a traditional Chinese herbal medicine used for treatment of chronic myelogenous leukemia (CML). One aspect of the invention relates to a method of treating CML using at least one indirubin derivative compound or a pharmaceutical composition thereof. Indirubin derivatives (IRDs) potently inhibited Signal Transducer and Activator of Transcription 5 (Stat5) protein in CML cells. Compound IRD 810 inhibits Bcr-Abl/Stat5 or Src/Stat5 signaling in human KCL-22 CML and imatinib-resistant human KCL-22 CML cells expressing the T315I mutant Bcr-Abl. Previous studies indicate that SFKs cooperate with Bcr-Abl to activate downstream Stat5 signaling. Activation of Stat5 was strongly blocked by IRD 810 in CML cells. IRDs disclosed herein have been identified as potent inhibitors of Bcr-Abl/Stat5 or SFK/Stat5 signaling pathway.

Abstract: The present invention relates to an industrially feasible and economically viable process for the preparation of methylphenidate hydrochloride of formula I and its intermediates thereof.

Abstract: The invention concerns a new process for preparing 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]-propionic acid methyl ester or 3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepine-4-yl]propionic acid methyl ester benzene sulfonate (P) which comprises reacting 3-[(S)-7-bromo-2-((R and/or S)-2-hydroxy-propylamino)-5-pyridin-2-yl-3H-benzo[e][1,4]diazepin-3-yl]-propionic acid methyl ester of formula (EM) with an oxidizing agent and optionally treating the reaction product under acidic conditions, such as to produce the compound of formula (F) or the compound (P), and new compounds useful as starting material or as intermediate for performing that process.

Abstract: This invention relates to compounds of Formula I: and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CFTR potentiator.

Abstract: A method is provided for N-alkylation of acridine compounds by reduction of acridines to corresponding acridans to improve the reactivity of the acridine nitrogen, and subsequent N-alkylation of the acridans in ionic liquid solvents to provide the corresponding acridinium compounds in high yield. This inventive process improves chemical conversion, and does not require the use of highly toxic alkylating agents, such as 1,3-propane sultone.

Abstract: The present invention relates to a novel process for preparing 3,5-bis(fluoroalkyl)pyrazole derivatives from ?,?-dihaloamines.

Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.

Abstract: This invention relates to methods for treating bone disease associated with osteoclast activation using HDAC6 selective inhibitors, e.g., small molecule inhibitors such as reverse amide compounds.

Abstract: The present invention describes new amino pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel amino pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors.

Abstract: The invention relates to besylate and tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl}acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses.

Abstract: The present invention provides a compound of Formula (I) and a salt thereof, wherein, m is an integer of 2 to 7, and R is independently at least one selected from the group consisting of hydrogen and C1-C20 alkyl. The compound promotes apoptosis in cancer cell and inhibits its growth. The present invention also provides a pharmaceutical composition which comprises the compound of Formula (I), a salt thereof and a pharmaceutically acceptable carrier. The present invention further provides a method for production of the pharmaceutical composition used for treating cancer.

Abstract: Disclosed herein are novel antifungal compounds of Formula 1, containing fluconazole pharmacophore moieties coupled with other moieties including aryl enones and chalcones and pharmaceutically acceptable salts thereof, methods for preparing these compounds and pharmaceutical preparations containing these novel compounds for prevention and treatment of fungal infections.

Abstract: Process for the selective N-sulfonylation of oxindoles, in particular process for the N-sulfonylation of 3-triazinyloxindoles, and also N-sulfonyl-substituted 3-triazinyloxindoles and the use of N-sulfonyl-substituted oxindoles and of N-sulfonyl-substituted 3-triazinyloxindoles as intermediates for the synthesis of fine chemicals and of active ingredients in the field of pharmacy and agriculture, and also the use of these compounds as active ingredients in the field of agriculture.

Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.

Abstract: A tetrazolinone compound represented by formula (1): Wherein R1, R2, R3, and R11 each represents a halogen atom, a C1-C6 alkyl group, etc.; R4 and R5 each represents a hydrogen atom, a halogen atom, a C1-C3 alkyl group, etc.; R6 represents a C1-C3 alkyl group optionally having one or more halogen atoms, etc.; R7, R8, and R9 each represents a hydrogen atom, a halogen atom, etc.; R10 represents a C1-C3 alkyl group, etc.; and R12 represents a phenyl group optionally having one or more atoms or groups selected from Group P3, a phenoxy group optionally having one or more atoms or groups Group P3, etc., has excellent control activity against pests.

Abstract: The present invention regards compositions and methods for the modulation of amidases capable of hydrolyzing N-acylethanolamines useable in the therapy of inflammatory diseases. In particular, the present invention regards a compound of general formula (I): enantiomers, diastereoisomers, racemes and mixtures, polymorphs, salts, solvates thereof, wherein: (a) R is a linear alkyl radical having 13 to 19 carbon atoms or alkenyl radical having 13 to 19 carbon atoms carrying a double bond; (b) X is 0 or S; (c) Y is a 2 or 3 carbon atom alkylene residue, optionally substituted with one or two groups equal or different from each other and selected from among the group consisting of: —CH3, —CH2OH, —COOCH3, —COOH. Y may preferably be: —CH2—CH2—, —CH2—CH2—CH2—, CH(CH3)—CH2—, —CH2—CH(CH3)—, —CH2—C(CH3)2—, —CH2—CH(CH2OH)—, —CH2—C((CH2OH)2)—, —CH?CH—, —CH2—CH(COOCH3)—, —CH2—CH(COOH)—, for use as a medicine.

Abstract: Compounds, compositions and methods are provided for selectively activating chaperone-mediated autophagy (CMA), protecting cells from oxidative stress, proteotoxicity and lipotoxicity, and/or antagonizing activity of retinoic acid receptor alpha (RAR?) in subjects in need thereof.

Abstract: The present invention relates to a process for manufacturing 4-propargylated amino-benzoxazinones of formula (I), comprising the following steps: step a) preparing propargyl chloride by reacting propargyl alcohol with thionyl chloride optionally in the presence of a catalyst; and step b) reacting the propargyl chloride prepared in step (a) with a NH-benzoxazinone of formula (II); wherein the variables are defined according to the description.

Abstract: Disclosed herein are novel C17-heteroaryl derivatives of oleanolic acid, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example, as antioxidant inflammation modulators, and compositions thereof are also provided.

Abstract: The present invention provides a solid form and compositions thereof, which are useful as metal chelators and which exhibit desirable characteristics for the same.

Abstract: The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.

Abstract: The present invention relates to a process for the preparation of 3-aroyl-5-aminobenzofuran derivatives useful as antiarrhythmic drugs which avoids the use of nitro intermediates.

Abstract: The invention is generally directed to a process of producing purified gamma- and/or delta-tocotrienols from tocol-rich oils or distillates, such as rice bran oil deodorizer distillate or palm oil. The process produces a gamma- and/or delta-tocotrienol-rich fraction in a high proportion of ?-T3 and/or ?-T3 while minimizing the presence of alpha isomers from the tocol-rich oil or distillate. The ?-T3- and/or ?-T3-rich fraction comprises about 95% of total tocols, with the process yielding ?-T3 in approximately 10% and ?-T3 in about 3%, with each having purity in excess of approximately 95%. The process utilizes flash or other low pressure chromatography to provide rapid isolation of gamma- and/or delta-tocotrienol from the tocol-rich oil or distillate.

Abstract: Various embodiments of the present invention relate to, among other things, compounds that are inhibitors of Memapsin 1 and, as a result, are effective in the treatment of Alzheimer's disease or diabetes (e.g., Type 2 diabetes).

Abstract: A method for producing glycolide (GL) by heating a glycolic acid oligomer (GAO) to depolymerize the GAO. The method for producing GL comprises: a step 1 of heating a mixture containing a GAO having a terminal COOH concentration of 400 eq/t or less and a polar organic solvent to a GAO depolymerization temperature under ambient pressure or reduced pressure; a step 2 of continuing the heating at the temperature for depolymerizing of the GAO and then codistilling out the produced GL and the solvent from the depolymerization reaction system to the outside the reaction system; and a step 3 of obtaining GL from the codistillation product. In the method for producing GL, the GAO is preferably prepared by a GAO production method which comprises a step of condensing glycolic acid (GA) and a dehydration step of continuing the heating together with a polar organic solvent or a depolymerization reaction solution to allow the GA condensation reaction to continue.

Abstract: Disclosed are beta and gamma-amino isoquinoline amide compounds and substituted benzamide compounds. In particular, the invention provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of the invention are useful in the treatment of a variety of diseases and conditions including eye diseases such as glaucoma, cardiovascular diseases, and diseases characterized by abnormal growth, such as cancers. The invention further provides compositions containing the beta or gamma-amino isoquinoline amide compounds or substituted benzamide compounds.

Abstract: 4,6-difluorodibenzothiophene compounds of formula I the preparation thereof, the use thereof as components in liquid-crystalline media and electro-optical display elements which contain the liquid-crystalline media.

Abstract: A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.

Abstract: The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Provided are compounds represented by the formula: where R, Y3, R1, R2, R3, R4, R6, G, R7, E1, E2, A, B, W, X, Y and Z are as defined herein.

Abstract: Compounds of general Formulas (I), (IA), (IB) are described, along with compositions containing the same and methods of use thereof, inhibiting the hedgehog pathway in a cell or inhibiting unwanted proliferation of a cell.

Abstract: Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein.