Abstract: The present invention relates to a compound of formula (I) in which: -m is an integer from 0 to 3, preferably from 0 to 2; n is an integer from 0 to 3, preferably from 0 to 2; m+n?1; EAG is an electro-attractive group chosen independently from among a halogen atom, an NO2, CF3, CCI3, CN, CO2H, (C?O)NR2, CH?NR, (C?S)OR, (C?O)SR, CS2R, SO2R, SO2NR2, SO3R, P(O)(OR)2, P(O)(R)2, B(OR)2 group where R is a (C1-C6) alkyl radical, a phenyl group or a hydrogen atom; A is a saturated or unsaturated, linear or branched hydrocarbon chain including 1 to 10 atoms of carbon; and R1 and R2 each represent independently from one another a hydrogen atom, a CO-(Ci-C6)-alkyl, (C1-C6) alkyl, phenyl or phenyl-(C1-C6)-alkyl group, in which R1 and R2 form, together with the nitrogen atom they carry, a 5- to 15-member heterocycle, optionally substituted by a (C1-C6) alkyl group; including its stereoisomers and the mixtures thereof, or a pharmaceutically acceptable salt of same.

Abstract: The present invention provides a novel process for reducing palladium content in fosaprepitant dimeglumine.

Abstract: This invention is directed to compounds, which are PDE9 enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula (I). The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I). The present invention further provides a compound of formula (I) for use in a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula (I).

Abstract: Disclosed herein are compounds and compositions useful for reducing the risk of infection. In particular, disclosed herein are mandelic acid condensation polymers, compositions comprising such compounds, processes for producing such compounds, and methods of using such compounds.

Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds represented by the general formula (I) are described. Also described, are pharmaceutical compositions including these compounds and the use of these compounds and compositions for the treatment of chemokine-mediated pathologies.

Abstract: The present invention discloses an economic, simple, azide and aziridine complexity free process for the synthesis of osletamivir phosphate (Tamiflu) by stereospecific amidoalkylation of imidazothiazolone from easily available L-cysteine via Ramberg-Backlund reaction and Sharpless-Reich protocol.

Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).

Abstract: Inhibitors of protein tyrosine phosphatases are disclosed. The inhibitors include hydroxyindole carboxylic acids having a linker and an amine scaffold that are potent inhibitors of Src homology 2-domain containing protein tyrosine phosphatase-2.

Abstract: The present invention provides imidazothiadiazole compounds of Formula (I); Wherein W, Y, R0, R2, R4, Ra, Rb, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

Abstract: Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease.

Abstract: The present invention relates to a crystal of 1-ethyl-7-methyl-3-{4-[(3-methyl-3H-imidazo[4,5-b]pyridin-2-yl)oxy]phenyl}-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one useful as a prophylactic or therapeutic agent for schizophrenia and the like, which shows an X-ray powder diffraction pattern having characteristic peaks at interplaner spacings (d) of 13.59 plus or minus 0.2 and 6.76 plus or minus 0.2 Angstroms in powder X-ray diffraction.

Abstract: A spherical morphology of the high explosive tetranitroglycoluril (TNGU) has been discovered. This new morphology exhibits approximately a twofold improvement in the response of the material to impact, more than a one and a half fold improvement in friction and the same high resistance to electrostatic discharge over non-spherical TNGU produced by other methods.

Abstract: The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.

Abstract: Provided are a semiconductor material for an organic transistor having a high charge mobility, solvent solubility, oxidation stability, and satisfactory film formability, and an organic thin-film transistor using the semiconductor material. The organic semiconductor material for an organic transistor is a seven-ring-fused heterocyclic compound having benzene rings at both ends, and having, therebetween, rings of a structure in which benzene rings A and pyrrole rings B are fused in the order of A-B-A-B-A. The fused heterocyclic compound may be substituted with an alkyl group, an alkenyl group, an alkynyl group, or an aromatic group. In addition, the organic thin-film transistor includes a semiconductor layer using the compound.

Abstract: The present invention belongs to the technical field of agricultural fungicides and discloses a 2-mercaptobenzothiazole manganese zinc, preparation method therefor and application thereof. The chemical structure of the 2-mercaptobenzothiazole manganese zinc is shown as the above formula. Wherein m, n and n? are positive integers, m=2(n+n?), n?n?, n:n?=1:1˜9:1. Materials are prepared according to the stoichiometric ratio of the target products; 2-mercaptobenzothiazole is dissolved in sodium hydroxide solution. The aqueous solution of water-soluble manganese salts and water-soluble zinc salts solution are successively added to 2-mercaptobenzothiazole sodium solution under stirring, followed by stirring for mixing well, then the solution being allowed to stand, filtered and washed with water to obtain filter cake, and then dried in vacuum to obtain 2-mercaptobenzothiazole manganese zinc. The present 2-mercaptobenzothiazole manganese zinc may be used as an agricultural fungicide.

Abstract: The present invention is directed to a pure enantiomer of 1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, in particular, (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone. The present invention is also directed a crystal structure of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a pharmaceutical composition of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, a method of inhibiting PDE10 with (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone, and a process and particular individual intermediates used in the production of (S)-1-(5-(4-chloro-3,5-dimethoxyphenyl)furan-2-yl)-2-ethoxy-2-(4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl)ethanone.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein n, L, X, Ra, Rb, R1, R2 and R3 their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.

Abstract: The present invention is directed compositions for delivery of RNA interference (RNAi) triggers to integrin positive tumor cells in vivo. The compositions comprise RGD ligand-targeted amphipathic membrane active polyamines reversibly modified with enzyme cleavable dipeptide-amidobenzyl-carbonate masking agents. Modification masks membrane activity of the polymer while reversibility provides physiological responsiveness. The reversibly modified polyamines (dynamic polyconjugate or conjugate) are further covalently linked to an RNAi trigger.

Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.