Abstract: The present invention relates to an amorphous form of Sumatriptan succinate of Formula (1). The present invention also relates to process for the preparation of an amorphous form of Sumatriptan succinate. The process for the preparation of an amorphous form of Sumatriptan succinate comprises refluxing an aqueous mixture of Sumatriptan or its succinate salt in alcoholic solvents such as methanol or nitrile solvents such as acetonitrile followed by evaporation of the solvent from the filtrate. The resulting residue is triturated with water immiscible aromatic or aliphatic hydrocarbon solvents such as cyclohexane to afford an amorphous form of Sumatriptan succinate.

Abstract: The invention relates to new, inexpensive electropolymers capable of light-induced grafting, onto which specific identification probes can be easily grafted and having optimum capacity for interaction with the target analytes (DNA/DNAc, PNA/PNAc, enzyme/substrate/Antibody/Antigen). These electropolymers capable of light-induced grafting are, for example, poly(pyrrole-benzophenone). Benzophenone forms sites for light-induced grafting. The invention also covers the mono and oligomers which make up these novel electropolymers capable of light-induced grafting. Another object of the invention is the process for their manufacture, as well as electronic biosensors containing these electropolymers capable of being grafted and/or grafted by probes for the analysis of biomolecules.

Abstract: The present invention provides a series of compounds having structural formulas wherein n1 is 1 to 5, n2 is 1 to 4 and m is 1 to 3; X is O or NH; Y is CH2, O, S, NH, NR; R is selected from the group consisting a straight-chain aliphatic group, a branched-chain aliphatic group and an alicyclic group; wherein R? is selected from the group consisting of hydrogen, methyl and ethyl; when Y is O, n1 is not 1; and wherein X and R? are independently optionally substituted at C2, C3 or C4 in compounds of Fomula IV or a pharmaceutically acceptable salt thereof. Also provided is a method of inactivating antigen-specific T cells in a n individual.

Abstract: The present invention relates to novel cathepsin S inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.

Abstract: A compound represented by the formula (I) wherein one of R1 and R2 is a hydrogen atom or a substituent and the other is an optionally substituted cyclic group; W is a bond or a divalent aliphatic hydrocarbon group; Y is a group of the formula: —OR3 (wherein R3 is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted acyl group) or an optionally esterified or amidated carboxyl group, or a salt thereof or a prodrug thereof has a superior insulin secretion promoting action and a hypoglycemic action and shows low toxicity. Therefore, the compound is useful as a pharmaceutical agent, particularly as an agent for the prophylaxis or treatment of diabetes and diabetic complications, and the like.

Abstract: Diketoacids of Formula A are useful as inhibitors of viral polymerases. In particular hepatitis C virus RNA dependent RNA polymerase (HCV RdRp), hepatitis B virus polymerase (HBV pol) and reverse transcriptase of human immunodeficiency virus (HIV RT): The group R may be broadly chosen and is an organic moiety which contains 2 to 24 carbon atoms and includes an optionally cyclic or heterocyclic group in which the atom directly bonded to the adjacent carbonyl in the diketoacid is part of the ring structure.

Abstract: Disclosed are methods of making aryl intermediate compounds of the formula (A) which are useful in the production of heteroaryl ureas, Y and P are defined herein below.

Abstract: Process for the preparation of a compound with enhanced optical purity wherein a mixture of the enantiomers of a chiral compound of formula 1 wherein: R1 represents an alkyl or an aryl group R2 represents H, an alkyl or an aryl group Y represents an alkyl group, an aryl group, (CH2)nCOOH, (CH2)n—COOR, (CH2)n—CONRR?, CH2OH, or C?N wherein R and R? independently represent H, an alkyl or aryl group, and n represents 0 or 1, is brought into contact with an enzyme having peptide deformylase activity with a bivalent metal ion as a cofactor wherein the metal is chosen from the groups 5–11 of the periodic system, or for the preparation of a formylated compound with enhanced optical purity from a mixture of the enantiomers of the corresponding not formulated chiral compound in the presence of a formylation agent. Preferably the peptide deformylase is chosen from the class EC 3.5.2.27 or EC 3.5.1.31, and contains the sequences of (I) HEXXH, (ii) EGCLS and (iii) GXGXAAXQ.

Abstract: Synthesis process of 5-benzyl-3-furfuryl alcohol including the reduction reaction with NaBH4 or with sodium dihydro bis-(2-methoxyethoxy)aluminium hydride of 3-benzyl-5-hydroxymethyl-5-carboxyalkyl isoxazoline to give 3-benzyl-5,5-bis(hydroxymethyl)isoxazoline which, through subsequent reduction in the presence of a weak protic acid and consequent rearrangement with strong aqueous acid, gives 5-benzyl-3-furfuryl alcohol.

Abstract: Disclosed is a method for the hydrogenation of tetrahydroxybutane in the presence of supported rhenium catalysts and an acid to form tetrahydrofuran and its precursors.

Abstract: To provide a producing method of an optically active ?-amino acid useful as intermediate for the production of medicines, agricultural chemicals and physiologically active substances, by means of a catalytic and asymmetric synthesis method of high performance and a high enantiomeric excess, without requiring additional procedures such as introduction and removal of protecting group and so on. A producing method of an optically active ?-amino acids which comprises subjecting an enamine to an asymmetric hydrogenation.

Abstract: The invention relates to the use of novel cyclohexyl analogues of E-type prostaglandins as EP4 agonists, in general, and, in particular as ocular hypotensives. The cyclohexyl analogues used in accordance with the invention are represented by the following formula I: wherein the wavy segments represent ? or ? bond, dashed line represents the presence or absence of a bond W, Y, Z, R, R1, R2 and R3 are as defined in the specification.

Abstract: The invention provides compositions and methods for isolating phenolic compounds, particularly isoflavones, from aqueous extracts of plant materials that contain such compounds. The process comprising: (a) providing an aqueous plant extract at a first pH less than 10, the aqueous plant extract comprising a plurality of phenolic compounds; (b) extracting the aqueous plant extract with a first organic solvent to yield a first organic extract; (c) extracting the first organic extract with an aqueous phase of pH greater than 10 to yield a phenol rich aqueous phase; (d) adjusting the pH of the phenol rich aqueous phase to a pH of less than 9; and (e) isolating the phenolic compounds from the phenol rich aqueous phase.

Abstract: Substituted pyranoindoles useful for lowering and controlling IOP and glaucoma are disclosed.

Abstract: A subject of the invention is the compounds of formula (I): in which either R1 and R2=H, OH, alkyl optionally substituted, or NR1 form with the carbon carrying NR1R2 a double bond and R2 is XRa, X being O, NH OR N-alkyl and Ra being H, alkyl optionally substituted, or R2 is e-N?C(—N-d)-N(f)-g R3=H, OH, CH3 R4=H, OH R=chain containing up to 30 carbon atoms, optionally containing one or more heteroatoms, one or more heterocycles, T=H, CH3, CH2CONH2, CH2C?N, (CH2)2NH2, (CH2)2Nalk+X? Y=H, OH, Halogen, OSO3H W=H, OH Z=H or CH3. The products have of the antifungal properties.

Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

Abstract: This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglandin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: The invention relates to dissolving an anionic dye/cationic polymer complex comprising the step of applying to the complex a water-soluble solvent having a dielectric constant from 20 to 43 at standard temperature and pressure.

Abstract: A catalyst includes a cyclic imide compound having an N-substituted cyclic imide skeleton represented by following Formula (I): wherein X is an oxygen atom or a hydroxyl group, and having a solubility parameter of less than or equal to 26 [(MPa)1/2] as determined by Fedors method. The catalyst may further comprise a metallic compound. By allowing (A) a compound capable of forming a radical to react with (B) a radical scavenging compound in the presence of the catalyst, an addition or substitution reaction product between the compound (A) and the compound (B) or a derivative thereof can be obtained.

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.