Abstract: Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein: Y1A and Y1B are independently Y1; RX1 and RX2 are independently RX; Y1 is ?O, —O(RX), ?S, —N(RX), —N(O)(RX), —N(ORX), —N(O)(ORX), or —N(N(RX)(RX)); RX is independently R1, R2, R4, W3, or a protecting group; R1 is independently —H or alkyl of 1 to 18 carbon atoms; R2 is independently R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups; R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or R3d; R3a is —H, —F, —Cl, —Br, —I, —CF3, —CN, N3, —NO2, or —OR4; R3b is ?O, —O(R4), ?S, —N(R4), —N(O)(R4), —N(OR4), —N(O)(OR4), or —N(N(R4)(R4)); R3c is —R4, —N(R4)(R4), —SR4, —S(O)R4, —S(O)2R4, —S(O)(OR4), —S(O)2(OR4), —OC(R3b)R4, —OC(R3b)OR4, —OC(R3b)(N(R4)(R4)), —SC(R3b)R4, —SC(R3b)OR4, —SC(R3b)(

Abstract: This invention relates to novel compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by one of the following structural formulas: wherein the values of R1, R2, Y1 and Y2 are described herein.

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 provides substituted 8-[6-amino-3-pyridyl]xanthines such as the following: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

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

Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.

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: [Object] It is to provide a novel compound useful for preventing and/or treating diseases that involves 11?-hydroxysteroid dehydrogenase 1 (in particular diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome). [Means to Solve the Object] A 1,2-diazetidin-3-one derivative represented by the following general formula (1) or salt thereof, or their solvate.

Abstract: The present invention relates to purine-based cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, inflammatory disorders, hepatic disorders, and a combination thereof.

Abstract: The present invention relates to new cephem compounds useful for the treatment of bacterial infections of formula I: The invention also relates to methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and to methods of treatment using the compounds. The new cephem compounds are stable, exhibit good solubility, and are particularly well suited for, e.g., parenteral administration for the treatment of bacterial infections.

Abstract: Novel crystals of a pyrrolidylthiocarbapenem derivative having excellent stability is provided. According to the present invention, a crystal of (+)-(4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3[[(3S,5S)-5-(sulfamoylaminomethyl)p yrrolidin-3-yl]thio]-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2?) of about 13.04, 14.98, 15.88, 16.62, 20.62, 21.06, 22.18, 23.90, 26.08, 28.22 and 28.98 (degrees) and a crystal of said compound having a diffraction pattern in powder X-ray diffraction having main peaks at diffraction angles (2?) of about 6.62, 13.04, 15.44, 16.58, 17.64, 20.88, 23.26, 25.02 and 25.52 (degrees) are provided.

Abstract: The invention 8-aminothioxanthines and the derivatives of formula I wherein the various R groups and substituents are comprised of a number of different (C1-C10)-alkyl, cycloalkyl, aryl, alkene, alkyne, etc. groups and derivatives thereof which are hereinafter more specifically defined for the treatment of metabolic disorders such as type-2 diabetes, hyperglycemia, arteriosclerotic diseases and the like.

Abstract: It is to provide a novel compound useful for preventing and/or treating diseases that involves 11?-hydroxysteroid dehydrogenase 1, particularly diabetes, insulin resistance, diabetes complication, obesity, dyslipidemia, hypertension, fatty liver, or metabolic syndrome. It is an 1-adamantyl azetidin-2-one derivative represented by the following general formula (1) or salt thereof, or their solvate.

Abstract: The present invention provides ?-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of ?-methyl carbapenems which are useful as antibacterial agents.

Abstract: The present invention relates to a method for crystallization of (2R)-2-{(3S,4S)-3-[(1R)-1-(tert-butyldimethylsilyloxy)ethyl]-2-oxoazetidin-4-yl}propionic acid, and is characterized in that crystallization is carried out by mixing a solution containing the compound with a substituted aromatic hydrocarbon solvent and/or a halogenated hydrocarbon solvent. The method can provide a crystal of the compound with a high purity and a high yield while the content of 2S isomer is kept at a low level.

Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.

Abstract: The present invention relates to novel polymorph of Ceftiofur sodium as a crystalline product. The present invention also provides a process for the preparation of crystalline Ceftiofur sodium of formula (I).

Abstract: The present invention relates to compounds and uses of compounds which interact with chitinase enzymes, in particular the inhibition of those enzymes.

Abstract: Disclosed herein is a compound comprising a formula or a pharmaceutically acceptable salt or a prodrug or a metabolite thereof; Y is 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 substituted with S or O; and D is aryl or heteroaryl. Methods of use are also disclosed.

Abstract: A process for the preparation of 2-fluoroadenine with a purity of at least 98% (HPLC Area) is presented. Such very high purity degree of at least 98% (HPLC Area) is obtained directly on the crude product after reacting 2,6-diaminopurine in an amount of anhydrous fluorinating agent; heating the resulting reaction mixture; quenching the heated reaction mixture; separating the solid obtained thereby; and washing and separating the solid, without recrystallization and/or any further purification steps.