Abstract: The present invention relates to a novel process for refining Cefmetazole sodium, comprising the steps of: 1) dissolving Cefmetazole sodium material in water, and extracting after adding a water-immiscible organic solvent(s), followed by separating the organic phase containing impurities, to provide an aqueous phase containing Cefmetazole sodium; 2) treating by adding an alkoxide of alkali metal or alkaline earth metal into the above aqueous phase, followed by filtrating the precipitate, to provide an aqueous filtrate; and 3) adding ethanol or acetone in the aqueous solution and recrystallizing, followed by centrifuging and washing the resultant crystals, to provide the refined and purified Cefmetazole sodium after drying. The purity of Cefmetazole sodium material can be greatly improved by the process of the present invention.

Abstract: Compounds of the formula (I), in which R, X, Y, Z, R3 and R4 have the meanings indicated in claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.

Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is methyl, ethyl or isopropyl, and the other is H; R3 and R4 are each independently H, branched or unbranched C1-C6 alkyl, or aryl, and wherein at least one of R3 and R4 is other than H; R5 is a branched or unbranched C1-C5 alkyl group or a C1-C6 cycloalkyl group, each of which may be optionally substituted with one or more OH groups; R6, R7, R8 and R9 are each independently H, halogen, NO2, OH, OMe, CN, NH2, COOH, CONH2, or SO2NH2. A further aspect of the invention relates to pharmaceutical compositions comprising compounds of formula 1, and the use of said compounds in treating proliferative disorders, viral disorders, stroke, alopecia, CNS disorders, neurodegenerative disorders, or diabetes.

Abstract: The present invention provides purine analog compounds, as well as compositions and methods of using them, for example, to prevent or treat various diseases and disorders in human and non-human animals.

Abstract: Cyclic acetals can be produced in a reactive distillation apparatus by combining a polyhydroxyl compound and an aldehyde. High concentrations of cyclic acetals are removed as liquid products from the column while water is removed as an overhead vapor stream.

Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogs of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogs significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogs for treatment of heart failure has been expanded.

Abstract: The present invention relates to the crystalline form of carbapenems derivative or hydrate thereof and the preparation methods thereof. Specifically, the present invention relates to the crystalline form of carbapenem derivative (4R,5S,6S)-6-((R)-1-hydroxyethyl)-4-methyl-7-oxo-3-(((3S,5S)-5-((4-sulfamoylbenzyl)carbamoyl)pyrrolidin-3-yl)thio)-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid as represented by formula (I) or hydrate thereof, characterized in that the X-ray powder diffraction pattern thereof using Cu-Ka radiation represented as 2? has characteristic peaks at 18.9±0.2, 19.4±0.2, 21.0±0.2, 21.7±0.2, and 23.4±0.2, the preparation methods thereof, and the use thereof in the preparation of medicament for treating and/or preventing infectious diseases, as well as a pharmaceutical composition comprising such compound and one or more pharmaceutical carriers and/or diluents.

Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)quinoline derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.

Abstract: The invention features compounds of formula (I): The compounds are useful as antibacterial agents, especially again Clostridium difficile-associated diseases.

Abstract: The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides processes for preparation of compounds of formula (I).

Abstract: Disclosed are A3 adenosine receptor antagonists and/or partial agonists of formula (I): wherein R1 to R5 are as described herein, as well as pharmaceutical compositions thereof and methods of use thereof. The antagonists or partial agonists find use in treating a number of diseases including cancer, glaucoma, inflammatory diseases, asthma, stroke, myocardial infarction, allergic reactions, rhinitis, poison ivy induced responses, urticaria, scleroderma, arthritis, brain arteriole diameter constriction, bronchoconstriction, and myocardial ischemia, as well as in preventing cardiac ischemia. Also disclosed are radiolabeled compounds of formula (I) and the use thereof in diagnostic imaging of tissues and organs.

Abstract: In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions.

Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.

Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.

Abstract: A novel arylpiperazine-containing purine derivatives and a pharmaceutical composition comprising the same as an active ingredient, which are useful for preventing or treating depressive disorders, are provided.

Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.

Abstract: A compound of the formula: and pharmaceutical compositions for the treatment or prevention of pain.

Abstract: The present invention discloses a physical nano-complex for preventing and treating cancer and a method for manufacturing the same. The composition contains EGCG and nanogold, wherein the ratio of the EGCG to the nanogold is in a range from 23:0.5˜23:10 (ppm/ppm). The present invention further discloses a method for manufacturing the composition, wherein the method is to mix the EGCG and the nanogold sufficiently by an ultrasonication process, which makes the EGCG and the nanogold combine to each other well.

Abstract: The present invention relates to an improved process for the preparation of Tenofovir Disoproxil and its pharmaceutically acceptable salts comprising the steps of: a) esterifying Tenofovir with chloromethyl isopropyl carbonate in presence of a base, phase transfer catalyst and optionally dehydrating agent, in a suitable solvent; b) optionally purifying Tenofovir Disoproxil; and c) converting of Tenofovir Disoproxil into its pharmaceutically acceptable salts. The present invention further relates to a process for the preparation of Tenofovir by reacting 1-(6-amino-purin-9-yl)-propan-2-ol with toluene-4-sulfonic acid diethoxy phosphoryl methyl ester in presence of a base in a non-polar solvent medium followed by hydrolysis.

Abstract: The present invention provides an improved process for stereoselective preparation of 5-fluoro-1-(2R,5S)-[2-(hydroxymethyl)-1,3-oxathiolan-5-yl]cytosine and pharmaceutically acceptable salts thereof.