Abstract: Provided are: eushearilides; a method for producing eushearilides; a production intermediate; and a pharmaceutical composition containing eushearilides. By having the Wittig reaction process, Mukaiyama Aldol reaction process and Macrolactonizaion process serve as key processes, eushearilides represented by formula (I) are efficiently produced.

Abstract: The present invention relates to fosamprenavir calcium (Ia) substantially free of isomer impurity, (3R) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propyl carbamate (Ib), and its process for preparation thereof. The present invention also provides fosamprenavir calcium intermediate, (S)-3-tetrahydrofuranyl-N-succinimidyl carbonate (IIa) substantially free of (R)-3-tetrahydrofuranylsuccinimidyl carbonate (IIb) and its process for preparation thereof.

Abstract: Compounds which are trehalose-6-phosphate or trehalose-6-phosphonate precursors of formula (I) or agriculturally acceptable salts thereof are provided: (I) The compounds are useful in increasing starch production in plants.

Abstract: The main object of the present invention relates to a novel crystalline form of Fosemprenavir Calcium designated as Form A. Another object of the present invention relates to a process for the preparation of Crystalline Form A of Fosemprenavir Calcium. Yet another object of the present invention relates to crystalline Forma A of Fosemprenavir Calcium characterized by a PXRD diffraction having reflections at about 3.1±0.2, 4.4±0.2, 5.0±0.2, 6.3±0.2, 7.4±0.2, 8.0±0.2, 2?.

Abstract: Crystalline Forms of fosamprenavir calcium are disclosed, processes for its preparation and pharmaceutical compositions therefrom. The process for the preparation of fosamprenavir calcium crystalline Form H1, comprises: a) suspending fosamprenavir calcium in a nitrile solvent; b) heating the suspension obtained in step (a) at reflux; c) optionally adding a solvent to the reaction mass obtained in step (b); d) cooling the reaction mass at below 35 degrees Centigrade; and e) isolating fosamprenavir calcium crystalline Form H1. Another process for the preparation of substantially pure amorphous fosamprenavir calcium, which comprises: a) dissolving fosamprenavir calcium in an ester solvent; b) a portion of solvent from the solution obtained in step (a) until at least separation of fosamprenavir calcium as solid occurs; and c) isolating substantially pure amorphous fosamprenavir calcium.

Abstract: The present invention relates to fosamprenavir calcium (Ia) substantially free of isomer impurity, (3R)tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propyl carbamate (Ib), and its process for preparation thereof. The present invention also provides fosamprenavir calcium intermediate, (S)-3-tetrahydrofuranyl-N-succinimidyl carbonate (IIa) substantially free of (R)-3-tetrahydrofuranylsuccinimidyl carbonate (IIb) and its process for preparation thereof.

Abstract: The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.

Abstract: The present invention relates to fosamprenavir calcium (Ia) substantially free of isomer impurity, (3R) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propyl carbamate (Ib), and its process for preparation thereof. The present invention also provides fosamprenavir calcium intermediate, (S)-3-tetrahydrofuranyl-N-succinimidyl carbonate (IIa) substantially free of (R)-3-tetrahydrofuranylsuccinimidyl carbonate (IIb) and its process for preparation thereof.

Abstract: The present invention provides a new class of solids supports for synthesis of modified oligomers of nucleic acids, and nucleic acid probes that have a format expediently synthesized on the new supports. Exemplary solid supports include at least one quencher bound through a linker to the solid support. Various exemplary embodiments include a moiety that stabilizes a duplex, triplex or higher order aggregation (e.g., hybridization) of nucleic acids of which the oligomer of the invention is a component. Other components of the solid support include moieties that stabilize aggregations of nucleic acids, e.g., intercalators, minor groove binding moieties, bases modified with a stabilizing moiety (e.g., alkynyl moieties, and fluoroalkyl moieties), and conformational stabilizing moieties, such as those described in commonly owned U.S. Patent Application Publication No. 2007/0059752.

Abstract: The trivalent phosphorous atom of a compound is reacted with a reagent in such a manner that a stable phosphate mimetic or a specifier is formed. Phosphoramidites with a phosphorous atom containing at least one hydroxyl residue which is provided with a protective group are reacted for this purpose with a free hydroxyl group: In the first synthesis cycle the hydroxyl group is linked to a solid support via a cleavable or non-cleavable linker. In further synthesis cycles the hydroxyl group is created by cleavage of the protective group from the growing oligomer. This results in formation of a phosphorous acid triester which is reacted with azides. By selecting suitable monomers for the synthesis which have a defined stereoconformation compounds of Formula 1 are produced in a stereocontrolled manner.

Abstract: The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.

Abstract: The main object of the present invention relates to novel crystalline form of Fosamprenavir Calcium designated as Form A. Another object of the present invention relates to a process for the preparation of Crystalline Form A of Fosamprenavir Calcium. Yet another object of the present invention relates to crystalline Form A of Fosamprenavir Calcium characterized by an PXRD diffraction having reflections at about 3.1±0.2, 4.4±0.2, 5.0±0.2, 6.3±0.2, 7.4±0.2, 8.0±0.2, 28.

Abstract: Addition compounds of a) alkylphosphonous acid derivatives of the formula A-P(?O)(OX)—H (I) and b) diester-forming olefins of formula (II) Methods for the production of the addition compounds and the use thereof are also disclosed.

Abstract: An alkylphenol-free liquid polymeric phosphite is described of general Structure IV illustrated below wherein each R1, R2, R3 and R4 can be the same or different and independently selected from the group consisting of C1-20 alkyl, C3-22 alkenyl, C6-40 cycloalkyl, C7-40 cycloalkylene, C1-20 methoxy alkyl glycol ethers, C1-20 alkyl glycol ethers, and or Y—OH; Y is selected from the group consisting of C2-40 alkylene, C2-40 alkyl lactone, —R7—N(R8)—R9—, wherein R7, R8 and R9 are independently selected from the group previously defined for R1, R2, R3 and R4, now further including H; m is an integral value ranging from 2 to 100 inclusive; and x is an integral value ranging from 1 to 1,000. The alkylphenol-free liquid polymeric phosphite is useful in reducing phosphite migration within polymers.

Abstract: Preparation method of fosamprenavir derivatives is disclosed. The compound shown by formula II or its ammonium salt is reacted with a metal ion source in solvent to obtain the compound shown by formula Iii. After isolating and purifying, the compound shown by formula III is catalytically reduced to the compound shown by formula I. In the formula, X is metal ion. Preferably, the metal ion source is a calcium ion source, sodium ion source, or potassium ion source, and X is calcium ion, sodium ion, or potassium ion. The solvent is methanol, ethanol, n-propanol, isopropanol, n-butanol, or sec-butanol. The catalytic reduction is carried out by using hydrogen as a reducing agent in the presence of palladium on carbon catalyst. The ammonium salt is methylamine salt, dimethylamine salt, ethylamine salt, diethylamine salt, isopropylamine salt, dibutylamine salt, dipropylamine salt, t-butylamine salt, or dicyclohexylamine salt.

Abstract: The present invention relates to fosamprenavir calcium (Ia) substantially free of isomer impurity, (3R) tetrahydro -3 -furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propyl carbamate (Ib), and its process for preparation thereof. The present invention also provides fosamprenavir calcium intermediate, (S)-3-tetrahydrofuranyl-N-succinimidyl carbonate (IIa) substantially free of (R)-3-tetrahydrofuranylsuccinimidyl carbonate (IIb) and its process for preparation thereof.

Abstract: This invention relates to acyclic and abasic nucleosides and oligonucleotides prepared therefrom. For instance, oligonucleotides can be prepared having one or more of the following formulas (I-III):, or isomers thereof.

Abstract: The present invention relates to process for the preparation of fosamprenavir calcium.

Abstract: The present invention relates to a crystalline form of fosamprenavir calcium. The crystalline form of the present invention is designated as Form II of fosamprenavir calcium. The present invention also relates to a process for the preparation of crystalline Form II of fosamprenavir calcium. The present invention further relates to a pharmaceutical composition comprising crystalline Form II of fosamprenavir calcium. The present invention relates further to a method of treating a HIV infection using crystalline Form II of fosamprenariv calium.

Abstract: The present invention provides an anti-plant virus agent which exhibits preventative and therapeutic effects on plant virus diseases. The anti-plant virus agent of the present invention is characterized by containing at least one compound selected from the group consisting of ascorbic acid derivatives represented by Formula (I) (wherein, R1 to R4 each independently represents a hydrogen atom, —SO3H, —PO3H2, a glycosyl group, or —COR11, wherein R11 represents an unsubstituted or substituted C1-30 alkyl group, or an unsubstituted or substituted C2-30 alkenyl group, with the proviso that R1 to R4 may not all be hydrogen atoms at the same time), and salts thereof.

Abstract: The invention relates to the use of radical traps in detergents and cleaners in order to improve cleaning performance, in particular for dirt containing polymerizable dyes.

Abstract: The present invention relates to amorphous Fosamprenavir calcium and processes for its preparation, a pharmaceutical composition comprising it and a method for treating a HIV infection therewith.

Abstract: Novel Fostriecin (or FST) derivatives represented by formula (I), the pharmaceutical compositions and preparation methods thereof. The pharmaceutical uses of these compounds, especially the use for the preparation of pharmaceutical compositions for treating tumor, inhibiting cell over growth, or lowering myocardial infarction and the injury to cells.

Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, 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 invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.

Abstract: An alkylphenol-free liquid polymeric phosphite is described of general Structure IV illustrated below wherein each R1, R2, R3 and R4 can be the same or different and independently selected from the group consisting of C1-20 alkyl, C3-22 alkenyl, C6-40 cycloalkyl, C7-40 cycloalkylene, C1-20 methoxy alkyl glycol ethers, C1-20 alkyl glycol ethers, and or Y—OH; Y is selected from the group consisting of C2-40 alkylene, C2-40 alkyl lactone, —R7—N(R8)—R9—, wherein R7, R8 and R9 are independently selected from the group previously defined for R1, R2, R3 and R4, now further including H; m is an integral value ranging from 2 to 100 inclusive; and x is an integral value ranging from 1 to 1,000. The alkylphenol-free liquid polymeric phosphite is useful in reducing phosphite migration within polymers.

Abstract: The invention relates to addition compounds of a) alkylphosphonous acid derivatives of the formula A-P(?O)(OX)—H (I) in which A represents C2-C18-alkyl, C2-C18-alkylene, C6-C18-arylalkyl, C6-C18-arylalkyl, optionally substituted, and X represents H, C1-C18-alkyl, C6-C18-aryl, C6-C18-arylalkyl, C6-C18-alkylaryl, optionally substituted C2-C18-alkylene, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K, H and/or a protonated nitrogenous base, and b) diester-forming olefins of formula (II) in which R2, R4 are identical or different from each other and represent CO2H, CO2R5, R6—CO2H, R6—CO2R5 and R1, R3 are identical or different from each other and represent H, R5; or R1, R4 are identical or different from each other and represent CO2H, CO2R5, R6—CO2H, R6—CO2R5 and R2, R3 are identical or different from each other and represent H, R5; or R2, R4 are identical or different from each other and represent —CO—O—CO—, —CO—S—CO—, —CO—NR1—CO—, —CO—PR1—CO— and R1, R3 are identical or different f

Abstract: Process for preparation of fosamprenavir and its intermediate salts using novel phthalimide intermediates.

Abstract: The present invention relates to solid state forms of fosamprenavir calcium salt, process for preparing said solid state forms, and pharmaceutical compositions thereof.

Abstract: The subject matters of the invention are: a crystallographic model of the binding site and a modulator regulating the catalytic activity of phosphofructokinase (PFK), a method of designing, selecting and producing a PFK modulator, a computer based method for the analysis of the interaction between the modulator and PFK, a computer-based method the analysis of molecular structures, a method of assessing the ability of the potential modulator to interact in the binding site on the PFK surface, a method of providing data for generating structures and/or performing design for ligands binding PFK, PFK homologues or analogues, complexes of PFK with a potential modulator, or complexes of PFK homologues or analogues with potential modulators, a computer system.

Abstract: The present invention relates to a stabilized vitamin C derivative with a peptide molecule linked to vitamin C or a pharmaceutically acceptable salt thereof, a method of preparing the same, and a composition containing the same.

Abstract: The invention concerns novel phosphonate derivatives, preparation method, use thereof as ligands modulating T ?9?2 lymphocyte activity and pharmaceutical compositions comprising them.

Abstract: A method of determining an amount of total PON1 in a sample of a subject is disclosed. The method comprises: (a) contacting the sample with a compound being capable of generating at least one spectrophotometrically detectable moiety upon contact with PON1, under conditions wherein the generating is not dependent on a PON1 status; and (b) spectrophotometrically measuring a level of the moiety, thereby determining an amount of total PON1 in the sample. Kits for measuring total PON1 levels comprising the compounds are also disclosed.

Abstract: The present invention relates to a novel delivery system for delivering therapeutic agents into living cells, and more particularly, to novel chemical moieties that are designed capable of targeting and/or penetrating cells or other targets of interest and further capable of binding therapeutic agents to be delivered to these cells, and to delivery systems containing same.

Abstract: The invention relates to a composition containing a particulate solid, an organic or aqueous medium, and a compound with a head group derived from phosphoric acid or sulphuric acid. The invention further relates to novel compounds, and the use of the compound as a dispersant.

Abstract: A method is described for synthesizing and administering carotenoid compounds with improved antioxidant characteristics. In some embodiments, extension or improvement of conjugation may be employed in structural modification of carotenoids. In other embodiments, reduction of ring/chain steric hindrance may improve the lambda max, and hence, the overall antioxidant capability, of particular compounds. In other embodiments, introduction and/or increase in synthetic handles for conjugation may improve the stoichiometric ratios of conjugating moieties to the polyene backbone. The methods may be used to improve natural and/or synthetic compounds for medicinal application in the treatment of disease.

Abstract: The present invention provides methods of treating creatine responsive states, such as a neurological disorder (i.e., Huntington's disease, Parkinson's disease, amyotrophic lateral sclerosis, muscular dystrophy, Charcot Marie Tooth syndrome, Alzheimer's disease, or creatine transporter defect) or a skin disorder, by administering a creatine-ascorbyl derivative.

Abstract: An ascorbic acid derivative, which is a compound represented by the following general formula (1) or a salt thereof: [Chemical Formula 11] (wherein X and Y each represents H or a protective group for OH, R1 and R2 each represents an alkyl group having from 1 to 19 carbon atoms, which may be linear or branched, and the total number of carbon atoms in R1 and R2 is an integer of 5 to 22).

Abstract: The present application describes deuterium-enriched fosamprenavir, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present invention relates to a sodium salt represented by average formula (I): (wherein, m1, n1, m2 and n2 respectively and independently represent a positive number of 0 0r 2 or less, provided that m1+n1=2, m2+n2=2, 0<m1+m2<4 and 0<n1+n2<4), a method for producing the same, and a method for inhibiting decomposition of a sodium salt represented by general formula (IV): [CHEMICAL 4] comprising: having the sodium salt represented by general formula (IV) in the presence of the sodium salt represented by average formula (I), and according to the present invention the stability over time of the sodium salt represented by general formula (IV) is improved.

Abstract: The invention is related to phosphorus substituted anti-infective 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: It is an object to provide an L-ascorbic acid derivative which can keep the L-ascorbic acid stable to heat and light and thus has a long shelf life, which is high in permeability into the skin, which can be quickly hydrolyzed by phosphatase, an enzyme that is ubiquitous in vivo, and which exhibits physiological activities that are inherent to L-ascorbic acid and beneficial to health, a method for producing such an L-ascorbic acid derivative, and a skin-whitening cosmetic material. There is provided an ascorbic acid derivative comprising an L-ascorbic acid-2-phosphate ester or a salt thereof wherein the phosphate ester has a branched alkyl group, the L-ascorbic acid-2-phosphate ester being of formula [13].

Abstract: An ascorbic acid derivative, which is a compound represented by the following general formula (1) or a salt thereof: [Chemical Formula 11] (1)(wherein X and Y each represents H or a protective group for OH, R1 and R2 each represents an alkyl group having from 1 to 19 carbon atoms, which may be linear or branched, and the total number of carbon atoms in R1 R2 is an integer of 5 to 22).

Abstract: One aspect of the present invention relates to differentially protected glycosyl phosphates. Another aspect of the present invention relates to the preparation of glycosyl phosphates from glycal precursors. In another aspect of the present invention, glycosyl phosphates are used as glycosyl donors in glycosylation reactions.

Abstract: The present invention relates to chiral diphosphorus compounds and their transition metal complexes, to a process for preparing chiral diphosphorus compounds and their transition metal complexes and also to their use in asymmetric syntheses.

Abstract: 2-Decarboxy-2-phosphinico prostaglandin derivatives are disclosed. These derivatives comprise a modified ?-chain and an ?-chain bonded to a ring structure. The modified ?-chain has a 2-decarboxy-2-phosphinico group. The derivatives can be used to treat a variety of pharmaceutical and cosmetic conditions.

Abstract: The present invention concerns novel unsymmetrical chiral diphosphines of a mixed aliphatic-aromatic type and processes for synthesizing them, complexes of these compounds and their use as catalysts.

Abstract: 2-Decarboxy-2-phosphinico prostaglandin derivatives are disclosed. These derivatives comprise a modified ?-chain and an ?-chain bonded to a ring structure. The modified ?-chain has a 2-decarboxy-2-phosphinico group. The derivatives can be used to treat a variety of pharmaceutical and cosmetic conditions.

Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.

Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.