Abstract: A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a ?-(substituted-amino)amide, a ?-(substituted-amino)acid ester, or a ?-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.

Abstract: Compounds of formula (I) and compositions comprising a compound of formula (I) for treating disorders related to TRPA1 are described herein.

Abstract: The present invention relates to a method for producing a nucleoside derivative represented by formula (2), comprising the step of reducing a nucleoside of formula (1) in the presence of a noble metal catalyst comprising a carrier and a noble metal supported thereby, selected from the group consisting of (A) a homogeneously supported catalyst where the specific surface area of the noble metal is 95.0 m2/g or more and the particle size of the noble metal is 4.3 nm or less, and (B) a surface-loaded catalyst where the specific surface area of the noble metal is 56.0 m2/g or more and the particle size of the noble metal is 8.0 nm or less, wherein R1 is hydrogen or a protective group, R2 is NH2 or OH, R3 is an acyl group, and X is a chlorine or bromine atom. According to the present invention, the yield can be made equal even when the amount of catalyst is smaller than that used for the conventional products.

Abstract: This invention relates to novel purinyl derivatives of formula Ia or Ib Wherein the symbols are as defined in the Specification and of pharmaceutically acceptable salts thereof useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.

Abstract: The present application provides for a compound of Formula (I) or (II): or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.

Abstract: A compound represented by Formula I, wherein M represents Na+, K+, NH4+, or Cs+; and 1) when Y represents SO42?: when m=1, then n=1; and when m=0.5, then n=1.5; and 2) when Y represents PO43?, when m=1, then n=2. The compound has good solubility and high bioavailability and can be formulated into oral pharmaceutical preparations and pharmaceutical preparations for injections.

Abstract: A process for the preparation of valganciclovir with triacetyl ganciclovir (V) as a starting material, comprising the following steps: selective hydrolysis, reacting with a coupling agent and CBZ valine and a solvent, followed by hydrolysis under basic conditions and hydrogenolysis in the presence of a catalyst.

Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.

Abstract: The invention relates to compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of formula (I).

Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.

Abstract: The present invention includes novel carbapenem derivatives having structural formula (I) or (II): wherein R1, R2, R3, R4 are described in the specification. The present invention also provides pharmaceutical compositions comprising the novel carbapenem derivatives and the use of the novel carbapenem derivatives for treating infectious diseases.

Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

Abstract: The present invention provides 2,6-disubstituted purine compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional 2,6-disubstituted purine compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided.

Abstract: Inhibitors of the enzyme beta-lactamase of formula (I): are provided. The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.

Abstract: The present invention relates to novel carbapenem derivatives and belongs to pharmaceutical field. Specifically, the present invention relates to the compounds as represented by formula (1), pharmaceutically acceptable salts, hydrolysable esters, isomers and intermediates thereof, wherein R1, R2, R3, R4 are described as in the description. The present invention also relates to the processes for the preparation of these compounds, to the pharmaceutical compositions comprising these compounds, and to their use for the manufacture of a medicament for the treatment and/or prevention of infectious diseases.

Abstract: The present invention provides a method by which a 6-hydroxyethyl penam compound represented by General Formula (2) below can be produced with a high selectivity: wherein R represents a hydrogen atom or a protective group for carboxylic acid and X2 represents a halogen atom; the method including the steps of reacting a Grignard reagent with a halogeno penam compound represented by General Formula (1) below: wherein R and X2 are the same as above, and X1 represents a halogen atom; reacting the generated compound with an amine compound; and further reacting the generated compound with acetaldehyde.

Abstract: A process for the preparation of a carbapenem of formula (I): in amorphous form wherein R represents hydrogen or COOM and M represents hydrogen or sodium the process including condensing a compound of formula (II): wherein P? denotes a carboxy protecting group, with a compound of formula (III): wherein P? denotes a carboxy protecting group, in the presence of a base to yield a compound of formula (IV): deprotecting both the protecting groups in the compound of formula (IV) in the presence or absence of a sodium ion source, a solvent and in the presence or absence of CO2, gas, extracting the product into an aqueous medium, quenching the aqueous layer of into an alcohol at a temperature, and isolating the carbapenem compound of formula (I) in amorphous form.

Abstract: Provided are substituted purinyl-pyrazol derivatives of the following formula (I), or a pharmaceutically acceptable salt thereof, and their use as potassium channel modulating agents, as well as pharmaceutical compositions having such derivatives that are useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels: wherein R1 represents hydrogen or alkyl; one of R2, R3 and R4 represents alkyl, hydroxy-alkyl, alkoxy-alkyl, halo, trifluoromethyl, trifluoromethoxy, hydroxy or alkoxy; and the other two of R2, R3 and R4, independently of each other, represent hydrogen, alkyl, hydroxy-alkyl, alkoxy-alkyl, halo, trifluoromethyl, trifluoromethoxy, hydroxy or alkoxy; R5 represents phenyl optionally substituted with one or more substituents selected from the group consisting of alkyl, halo, trifluoromethyl, trifluoromethoxy, alkoxy and cyano; and R6 represents R?OC(?O)—, wherein R? represents alkyl, alkoxy, alkoxy-alkyl or adamantanyl.

Abstract: The present invention relates to therapeutically active xanthine derivative compounds of Formula (I): corresponding processes for manufacture of said derivatives, pharmaceutical formulations containing and uses of such compounds in therapy, particularly in treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.