Abstract: Compounds for the treatment of elevated blood glucose levels and the physiological and metabolic disorders arising therefrom are disclosed and comprise novel substituted bicyclic 8-pyrrolidinoxanthines and their derivatives of formula I: wherein the various R groups are hereinafter defined. The present invention also comprises pharmaceutical compositions comprising them as well as processes for the preparation of these compounds. Particular blood glucose disorders treatable thereby include type-2 diabetes, insulin resistance, hyperglycemia, arteriosclerotic diseases and the like.

Abstract: Hsp90 inhibitors are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2?alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula —O—(CH2)n—O—, wherein n is an integer from 0 to 2, preferably 1 or 2, and one of the oxygen is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

Abstract: The treatment of neurological disorders using cephalosporin sulfoxide-containing and/or cephalosporin sulfone-containing compositions and pharmaceutical compositions including oral dosage forms that include cephalosporin sulfoxide and/or sulfone-containing compositions are described.

Abstract: 7-[2-(2-aminothiazol-4-yl)-2-(methylcarbonyloxyimino)acetamido]-3-vinyl-cephem-4-carboxylic acid of formula (I), in the form of a crystalline salt and use thereof, e.g. in the preparation of pure cefdinir. In another aspect this invention relates to the compound of formula (I) in the form of a salt, optionally in crystalline form, wherein the salt is selected from the group consisting of phosphate, hydrogen phosphate, mesylate, tosylate, sulfate, hydrogen sulfate and sulfamate.

Abstract: Disclosed are (N)-methanocarba adenine nucleosides of the formula: as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.

Abstract: The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. The process involves reacting a compound of the formula (III) with 3-(phthalimido)piperidine or an enantiomer thereof where X is a leaving group selected from halogens and sulphonic ester acid residues, and R1 to R3 are as defined herein, to obtain a compound of the formula (II) and deprotecting the obtained compound of the formula (II) to obtain the product xanthines.

Abstract: Process for the preparation of tetrahydropterin and tetrahydropterin derivatives by hydrogenating pterin and pterin derivatives with hydrogen in the presence of a hydrogenating catalyst, in which the hydrogenation is carried out in a polar reaction medium and metal complexes that are soluble in the reaction medium are employed as the hydrogenation catalysts. The process is suited to the hydrogenation, particularly asymmetric hydrogenation, of folic acid, folic acid salts, folic acid esters, folic acid ester salts or dihydroforms thereof, with the proviso that in the event of using folic acid, carboxylic acid salts thereof or dihydroforms thereof the reaction medium is aqueous, and in the event of using folic acid esters, folic acid ester salts or dihydroforms thereof the reaction medium is an alcohol. The process opens up straightforward access to achiral and chiral pterin derivatives.

Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group as defined herein; X is O; R5 is H, C1-C6 alkyl, C5-C6 cycloalkyl, or CHR3OCOC1-C6 alkyl; and R3 is hydrogen, C1-C6 alkyl, C5-C6 cycloalkyl, optionally substituted aryl, or optionally substituted heteroaryl; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.

Abstract: The invention relates to compounds of formula 1 wherein R1-R2 is a guanine derivative; X is oxygen or sulfur; R3 is a heteroaromatic, unsaturated heterocyclyl or an alkynyl group with the double or triple bond connected to CH2; R4 is a linker; and L is a label, a plurality of same or different labels, a bond connecting R4 to R1 forming a cyclic substrate, or a further group —R3—CH2—X—R1-R2. The invention relates also to methods of manufacture of such novel AGT substrates, to intermediates useful in the synthesis of such AGT substrates, and to a method of transferring a label from such AGT substrates to O6-alkylguanine-DNA alkyltransferase (AGT) fusion proteins comprising proteins of interest.

Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.

Abstract: Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.

Abstract: Orally bioavailable prodrugs of sulopenem, e.g., and solvates and hydrates thereof, preparation thereof, formulation thereof, and use to treat and prevent infection in mammals such as humans. This abstract is not limiting to the invention.

Abstract: The present invention relates to pharmaceutical compositions for the treatment or prevention of viral infections comprising as an active principle at least one compound having the general formula (A): wherein U is N or C; X is selected from C1-C10 alkylene, C2-10 alkenylene or C2-10 alkynylene, where each may include one or more intrachain heteroatoms selected from O, S, or NR11, provided any such heteroatom is not adjacent to the N in the ring; R3 is selected from aryl, aryloxy, arylthio, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl-N(R10)—, or heterocycle, where each said substituent is optionally substituted with at least one R17, provided that for cycloalkenyl the double bond is not adjacent to a nitrogen; and the other substituents are described in the specification.

Abstract: A process for preparing xanthine phosphodiesterase V inhibitors, and compounds utilized in said process. The process includes a five-step methodology for efficient synthesis of Compound 5 without intermediate purifications or separations, a dihalogenation step to synthesize Compound 7, and a coupling reaction to produce Compound 9.

Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.

Abstract: In this invention the novel polymorphs of the valacyclovir hydrochloride and methods for preparing these novel polymorphs are provided.

Abstract: Analogs or derivatives of nitrobenzylthioinosine corresponding to formula I: in which R represents an unsubstituted or mono- or polysubstituted phenyl, benzyl or heteroaryl group or a phenyl group condensed with heteroaryl, and R? represents an unsubstituted or mono- or polysubstituted NH—C1-6-alkyl, NH-aryl, NH-heteroaryl, NH—C3-8-cycloalkyl, NH—C1-3-alkyl-aryl, NH—C1-3-alkyl-heteroaryl, N(C1-6-alkyl)2, N(C1-3-alkyl-aryl)2, N(C1-3-alkyl-heteroaryl)2, piperidine, piperazine, morpholine or pyrrolidine group; pharmaceutical compositions comprising such analogs or derivatives, and the use of such analogs or derivatives for treating pain and/or various other diseases.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof; wherein a dashed line indicates the presence or absence of a bond; Y is an organic acid group, or an amide or ester thereof comprising from 1 to 12 carbon atoms; or Y is hydroxymethyl or an ether thereof comprising from 1 to 12 carbon atoms; or Y is a tetrazolyl group; A is —(CH2)6—, cis —CH2CH?CH—(CH2)3—, or —CH2C?C—(CH2)3—, wherein 1 or 2 carbon atoms may be substituted with S or O; or A is —(CH2)m—Ar—(CH2)o— wherein Ar is interarylene or heterointerarylene, the sum of m and o is from 1 to 4, and wherein one CH2 may be replaced with S or O; J is CHOH, C?O, CH2CHOH, or CH2C?O; and Ar1 is aryl, heteroaryl, CH2-aryl, CH2-heteroaryl, O-aryl, O-heteroaryl, S-aryl, or S-heteroaryl.

Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.

Abstract: The present invention provides compounds of the formula which are adenosine A2B receptor antagonists and, thus, may be employed for the treatment of conditions and diseases mediated by the adenosine A2B receptor activity. Such conditions include, but are not limited to, chronic and acute inflammatory diseases involving degranulation of mast cells, e.g., asthma, allergic rhinitis and allergic dermatitis; impaired sensitivity to insulin, e.g., type 2 diabetes, pre-diabetic state, and impaired glucose tolerance; diseases in which angiogenesis is a key component of pathogenesis, e.g., solid tumors and angiogenic retinopathies; apnea of preterm infants; myocardial reperfusion injury; inflammatory bowel disease; autoimmune diseases, such as rheumatoid arthritis, multiple sclerosis, and lupus erythematosis; diseases involving microvascular abnormalities of the retina that are mediated by adenosine A2B receptors, e.g.