Abstract: The invention 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 relates to a process for the preparation of 15-pentadecanolide by hydrogenating 15-pentadecenolide and to its use.

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: Novel derivatives of ascorbic acid and compositions comprising them are provided. The novel derivatives are of the following general formula (I): where R1 is a C2-C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1-C17 alkyl ; R2 is a group of the following formula (II) wherein R5 or R6 are the same or different and represent hydrogen, a C1-C4 alkyl, or R5 is C1-C4 alkyl group and R6 is a metal cation or ammonium cation; R3 or R4 are the same or different and represent hydrogen, C2-C22 saturated or unsaturated fatty acid residues, amino acid residues, or a C1-C17 alkyl.

Abstract: A method and composition for the treatment of HIV infection, HBV infection, or abnormal cellular proliferation in humans and other host animals is disclosed that includes the administration of an effective amount of a 1,3-oxaselenolane nucleoside or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.

Abstract: The invention relates to calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propylcarb-amate, to processes for its preparation, and to its use in the treatment of diseases caused by retroviruses.

Abstract: Compounds of formula (I) wherein the substituent groups defined by R1, R2, R3 and R4 are each independently selected of H, C(═O)R, P(═O)R′R″, S(═O)R′R″, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstituted aryl; wherein each of the R′, R″ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, substituted or unsubstituted C1-C18 alkyl, substituted or unsubstituted C2-C18 alkenyl, substituted or unsubstituted C2-C18 alkynyl, substituted or unsubstitued aryl; wherein R1, R2, R3 could form part of a heterocyclic ring; R2 can be independently an internal salt; wherein X1, X2 and X3 on formula (I) are independently placed in any particular position of the chain and independently selected of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′

Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.

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

Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.

Abstract: A process for preparing a high-purity ascorbic acid-2-monophosphate salt in a convenient manner and in a high yield, comprising hydrolyzing an ascorbic acid-2-polyphosphate or a salt thereof in the presence of magnesium ion at a pH of 7 or more.

Abstract: A process for preparing a high-purity ascorbic acid-2-monophosphate salt in a convenient manner and in a high yield, comprising hydrolyzing an ascorbic acid-2-polyphosphate or a salt thereof in the presence of magnesium ion at a pH of 7 or more.

Abstract: A process for producing an ascorbic acid-2-phosphoric ester salt, where an ascorbic acid-2-phosphoric ester salt solution reduced in the content of excess phosphoric acid or a salt thereof mingled in the solution can be obtained from a solution containing an ascorbic acid-2-phosphoric ester or a salt thereof and a phosphoric acid or a salt thereof, with industrially high efficiency. A process for producing an alkaline earth metal salt of an ascorbic acid-2-phosphoric ester, comprising adding an alkaline earth metal compound to a stock solution containing an ascorbic acid-2-phosphoric ester or a salt thereof and a phosphoric acid or a salt thereof, at a liquid temperature of 0 to 30° C. to adjust the pH to 8.5 to 10.5.

Abstract: Chiral phosphine ligands derived from chiral natural products including D-mannitol and tartaric acid. The ligands contain one or more 5-membered phospholane rings with multiple chiral centers, and provide high stereoselectivity in asymmetric reactions.

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: Radioicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 (wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the like) and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.

Abstract: A process for separating L-ascorbyl 2-monophosphate from a mixture of the products of the desalting of the product mixture obtained from the phosphorylation under basic conditions of an L-ascorbic acid salt is described. This process is characterized by passing an aqueous solution of the desalted mixture containing among other components the desired L-ascorbyl 2-monophosphate through a column of a basic anion exchange resin, with resulting adsorption of the components onto the resin, desorbing among other adsorbed components the L-ascorbyl 2-monophosphate from the resin using as the eluent an aqueous alkali hydroxide solution, and collecting from the eluate the fraction which contains as its principal dissolved component the desired L-ascorbyl 2-monophosphate in the form of the appropriate mono-alkali metal salt.

Abstract: Compounds of formula III, wherein R6 und R7 signify identical or different secondary phosphino; R8 is —CH2—OH, —CH2—NH2—, —CH2O——B—FU, —CH2—NH2—B—FU, or —O—B—FU; R9 has the same significance as R8 or is C1-C4-alkyl or C1-C4-alkoxy; or R8 and R9 together signify HOCH(CH2—O—)2, H2NCH—(CH2—O—)2, FU—B—OCH(CH2—O—)2 or FU—B—HNCH(CH2—O—)2; B is a bridging group; and FU is a functional group. The compounds may be bonded to inorganic or organic carriers. Their d-8 metal complexes are valuable catalysts for the enantioselective hydrogenation of prochiral organic compounds with carbon multiple bonds or carbon/hetero atom multiple bonds.

Abstract: A high-purity L-ascorbic acid-2-phosphoric acid potassium crystal having excellent stability, and a method for simply producing the high-purity L-ascorbic acid-2-phosphoric acid potassium in a high yield by adding dropwise a solution containing L-ascorbic acid-2-phosphoric potassium to methanol or simultaneously mixing methanol and a solution containing L-ascorbic acid-2-phosphoric acid potassium. By the production method of the present invention, high-purity L-ascorbic acid-2-phosphoric acid potassium crystal having excellent stability can be simply produced in a high yield. The L-ascorbic acid-2-phosphoric acid potassium crystal obtained by the production method of the present invention is used for feedstuff, cosmetic materials, medical products, food additive and the like.

Abstract: Processes for preparing compounds of the formula (I) are described: P1OOC—CH(OH)—CHR1—CONH—Z wherein P1 is hydrogen or a protecting group, Z is a group —CHR2COOP2 or —CHR2CONR3R4 wherein P2 is hydrogen or a protecting group and R1-R4 are values known in the TNF-inhibitor art. The compounds of the formula (I) are useful in inhibiting TNF and one or more matrix metalloproteinase enzymes. One intermediate in a process of the invention is formula (II).

Abstract: A process for preparing salts of ascorbyl 2-phosphoric esters of the formula I, ##STR1## where the variables have the following meanings: M is sodium, potassium, magnesium, aluminum; ##STR2## k.sym. is the valence and m=equivalents, where the product of k.multidot.m can be from 3 to 5,comprisesa) dissolving calcium L-ascorbate-2-phosphate in an aqueous solution of ascorbyl 2-phosphoric esters at a pH of from 0.5 to 4,b) removing the calcium ions from the resulting solution,c) adjusting the pH of the solution which remains to from 7 to 11 by means of sodium, potassium, magnesium or aluminum salts andd) isolating the salts of the ascorbyl 2-phosphoric ester of the formula I.

Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: Compounds represented by the general formula (I) or pharmacologically acceptable salts thereof: ##STR1## (where R is a group --NHCHR.sub.1 R.sub.2, --N(CHR.sub.1 R.sub.2).sub.2, --N(CHR.sub.1 R.sub.2)CHR.sub.3 R.sub.4, --N.sup.+ (CHR.sub.1 R.sub.2).sub.3, --N.sup.+ (CHR.sub.1 R.sub.2).sub.2 CHR.sub.3 R.sub.4 or --N.sup.+ (CHR.sub.1 R.sub.2)(CHR.sub.3 R.sub.4)CHR.sub.5 R.sub.6 (where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, are each a hydrogen atom, an alkyl group, an alkenyl group, an aryl group or an aralkyl group, or an alkyl, alkenyl, aryl or aralkyl group which is substituted by at least one substituent selected from the group consisting of a halogen atom, a hydroxyl group, a lower alkoxy group, a lower alkylacyloxy group, a lower alkylacyl group, a lower alkoxycarbonyl group, a nitro group, a cyano group and a heterocyclic group, with CHR.sub.1 R.sub.2, CHR.sub.3 R.sub.4 or CHR.sub.5 R.sub.

Abstract: The process for manufacturing ascorbic acid 2-mono-phosphates from ascorbic acid 2-polyphosphates, in particular 2-triphosphates by subjecting the ascorbic acid 2-triphosphates to drying conditions.

Abstract: A method of detecting the presence of a substance being monitored in a medium, selected from the group of substances including organophosphorus compounds and the metal ions Zn, Be and Bi, including the steps of: providing a 1,2-dioxetane phenyl phosphate compound; providing a phosphatase that catalytically degrades the 1,2-dioxetane phenyl phosphate compound to produce light, the catalytic activity of the phosphatase toward 1,2-dioxetane phenyl phosphate compound being altered by the substance being monitored; exposing the 1,2-dioxetane phenyl phosphate compound and the phosphatase together to a medium which may contain the substance being monitored; detecting light produced after the exposing step; and determining, from the detected light, the presence and concentration in the medium of the substance being monitored.

Abstract: Inhibitors of E-, P- and L-selectin binding are synthesized by an aldol addition reaction between a glycoside aldehyde precursor and dihydroxyacetone phosphate or a derivative thereof. The addition reaction is catalyzed by aldolase. The inhibitors exhibit an activity comparable to sialyl Lewis X with respect to the E-selectin binding assay and high activities in the P- and L-selectin binding assays. The inhibitors are employable for blocking neutrophil inflamatory conditions.

Abstract: This invention provides a phosphoric diester of formula (I) which is available on di-esterification of phosphoric acid with L-ascorbic acid involving its 5-hydroxyl group and tocopherol involving its hydroxyl group or a pharmacologically acceptable salt thereof. ##STR1## The compound of the invention can be used with advantage as an antioxidant (radical-scavenging) agent and a prophylactic and therapeutic agent for ischemic organ disorders (e.g. myocardial infarction, heart failure, arrhythmia, cerebral infarction, stroke (cerebral apoplexy), renal failure, etc.).

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: The present invention relates to a new 3-aryl-4-hydroxy-.DELTA..sup.3 -dihydrofuranone derivatives of the general formula (I) ##STR1## in which the radicals A, B, G, X, Y, Z and n have the meaning given in the description, to a plurality of processes for their preparation, and to their use as pesticides.

Abstract: The bisphosphonates of formula (III)R.sub.2 --X--(CW).sub.m1 --CR.sub.3 R.sub.4 --CH.sub.2 --CM[PO--(OR.sub.1).sub.2 ].sub.2 (III)bicyclic bisphosphonates (V), and cyclic bisphosphonates (VII) are useful as antiarthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.

Abstract: A process for reducing the phosphate content in waste water from the preparation of salts of ascorbic acid 2-monophosphate comprisesA. treating the waste water from the crystallization of the metal salts of ascorbic acid 2-monophosphate with an alkali metal or alkaline earth metal hypochlorite, chlorine or H.sub.2 O.sub.2,andB. precipitating, at a pH of 9-12, the inorganic phosphate which has been produced from organically bound phosphorus and/or was present in the waste water, especially as calcium phosphate.

Abstract: The invention relates to a process for the preparation of ascorbic acid-2-phosphate, which comprises reacting ascorbic acid or araboascorbic acid with ATP to produce ascorbic acid-2-phosphate in an aqueous medium in the presence of an effective amount of an enzyme derived from a microorganism and capable of catalyzing the enzymatic reaction of ascorbic acid or araboascorbic acid with ATP to produce ascorbic acid-2-phosphate and recovering the resultant ascorbic acid-2-phosphate from the reaction solution.

Abstract: Enantioselective hydroformylation of vinyl compounds using a catalyst composition of a chiral carbohydrate phosphorous ligand with a Rh, Pt, Co or Ir metal, to produce chiral 2-substituted propanals, wherein the phosphorous of the ligand is substituted with electron withdrawing groups.

Abstract: A method for the synthesis of a plurality of oligonucleotides comprising the steps of(i) forming a first oligonucleotide on a first cleavable link attached to a solid support;(ii) attaching to the first oligonucleotide a cleavable linker moiety;(iii) forming a second oligonucleotide on the cleavable linker moiety; and(iv) cleaving the first cleavable link and the cleavable linker moiety to give a plurality of oligonucleotides; wherein the cleavable linker moiety is of the Formula (1): ##STR1## in which A.sup.1, A.sup.2 and E are as defined herein, and novel compounds which may be used in the operation of the method.

Abstract: Metal salts or substitutted or non-substituted ammonium salts of ascorbic acid derivatives can be produced in high yield by treating an acidic aqueous solution containing ascorbic acid-2-phosphate or ascorbic acid-2-sulfate with a porous adsorbent such as activated carbon, followed by treating the adsorbent with a basic aqueous solution containing e.g. a metal salt of an organic acid or substituted or non-substituted ammonium salt ion to elute the desired salt of ascorbic acid derivative.

Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases, ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.

Abstract: Novel anti-inflammatory furanone compounds have the following formula: ##STR1## where R.sub.1 independently is H, or alkyl of 1 to 9 carbons and n is an integer having the values of 1 or 2, and where when n is 1 the R.sub.1 group is attached to the 5 position of the 2-furanone, when n is 2 then R.sub.1 is attached to both the 3 and 5 positions, with the proviso that when n is 1 then R.sub.1 is not H; Y.sub.1 is H, alkyl of 1 to 20 carbons, phenyl C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkenyl containing one or more olefinic bonds, where R.sub.3 is H, C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkenyl containing one or more olefinic bonds, phenyl, halogen substituted phenyl or C.sub.1 -C.sub.6 alkyl substituted phenyl, with the proviso that when Y.sub.1 is CO--OR.sub.3 or CONHR.sub.3 then R.sub.3 is not hydrogen; Y.sub.2 is H, an alkyl group of 1 to 25 carbons, or phenyl.

Abstract: There are disclosed compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, alkyl, cycloalkyl, arylalkyl, --(CH.sub.2).sub.r CH.dbd.CH.sub.2, --(CH.sub.2).sub.s OY, --(CH.sub.2).sub.t CH(OZ)CH.sub.3, or Ar;X is O, S, or NR.sup.2 ;Y and Z are each, independently, hydrogen, alkyl, or --COR.sup.3 ;R.sup.2 and R.sup.3 are each, independently, hydrogen, alkyl, or arylalkyl;Ar is an aryl radical that may be optionally substituted;m=1-5;n=0-1;p=1-9;r=0-6;s=2-6; andt=0-6or a pharmaceutically acceptable salt thereof which are useful as antiinflammatory agents.

Abstract: Novel compounds of the formula (1), ##STR1## in which R.sub.1 is hydrogen or acyl, R.sub.2 to R.sub.5 are independently hydrogen, chloro, alkyl phenylalkyl, aryl, cycloalkyl, alkoxy, alkylthio, hydroxy, amino or substituted amino, R.sub.6 is hydrogen, R.sub.7 to R.sub.10 are independently hydrogen, alkyl or alkoxy, R.sub.17 or R.sub.19 is hydrogen or alkyl, and R.sub.18 is hydrogen, alkyl, aralkyl or aryl, are described for use as stabilizers for organic materials against thermal, oxidative or light-induced degradation.

Abstract: A process for isolating the calcium salt of ascorbyl 2-monophosphate from aqueous alkaline reaction mixtures as are obtained on reaction of ascorbic acid with a molar excess of phosphorus oxychloride in the presence of a tertiary amine while maintaining a pH of from 12 to 13 during the reaction by means of an aqueous alkali metal hydroxide solution, which comprisesa) starting from a reaction mixture which has been obtained by reacting ascorbic acid with phosphorus oxychloride in the presence of pyridine while maintaining a pH of from 12 to 13 by means of an aqueous potassium hydroxide solution,b) precipitating, as potassium magnesium phosphate, the phosphate ions which have been formed in this reaction by means of magnesium chloride in amounts of about 1 mol per mol of phosphate ions,c) removing the potassium magnesium phosphate,d) distilling the remaining aqueous solution to remove the pyridine together with part of the water,e) reacting the resulting aqueous solution with calcium chloride andf) isolating th

Abstract: A new compound, which we have named Leustroducsin H, has formula (I): ##STR1## and pharmaceutically acceptable salts thereof. This compound may be prepared by hydrolysis of naturally occurring Leustroducsins and the compound may be used for the treatment or prophylaxis of thrombocytopenia.

Abstract: Monoalkylated benzofuran adducts provide high temperature stable lubricant fluids having not only excellent thermal stability, but good low-temperature properties and excellent additive solubility as well.

Abstract: New compounds, which we have named the "Leustroducsins" have the formula (I): ##STR1## in which R represents a 5-methylhexanoyloxy group, a 6-methyloctanoyloxy group or a 7-methyloctanoyloxy group, and salts thereof, and may be prepared by fermentation using a microorganism of the genus Streptomyces, especially a strain of the species Streptomyces platensis, such as strain SANK 60191 (FERM BP-3288). These compounds may be used for the treatment or prophylaxis of: adverse reactions resulting from cancer chemotherapy or radiotherapy; infections; cancer; cerebral dysfunction; and fungal infections.

Abstract: The invention relates to new derivatives of macrocyclic lactones, a process for their preparation, a pyrolysis process using these new derivatives and the use of the pyrolysis products for the preparation of saturated macrocyclic lactones.

Abstract: Anti-inflammatory 4-substituted 2-furanones are made from intermediates having the formulas: ##STR1##

Abstract: Antibiotic substances having the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein.

Abstract: Presented are a glycyrrhetic acid derivative of the following formula ##STR1## or a pharmacologically acceptable salt thereof, which has antioxidant, antiinflammatory and/or antiallergic activity, a process for producing said compound or salt, and an antioxidant, antiinflammatory and/or antiallergic composition comprising said compound or salt.

Abstract: Compounds of the formula ##STR1## in which R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.2, CO--O--R.sub.2, CO--NH--R.sub.2, or PO(OR.sub.2).sub.2 or PO(OR.sub.2)R.sub.2, where R.sub.2 independently is H, alkyl of 1 to 20 carbons, phenyl, or lower alkyl substituted phenyl or halogen substituted phenyl; n is an integer between 8 to 14; Y is H, alkyl having 1-20 carbon atoms, aryl[lower alkyl], aryl, lower alkyl[aryl], alkenyl containing one or more olephinic bonds and 1-20 carbon atoms, CO--R.sub.3, CO--OR.sub.3, CONHR.sub.3, SO.sub.2 R.sub.3, SO.sub.2 NHR.sub.3 where R.sub.3 is aryl[lower alkyl], aryl, lower alkyl[aryl], alkenyl containing one or more olephinic bonds and 1-20 carbon atoms, further Y is PO(OH).sub.2, PO(OH)OR.sub.4, PO(OH)R.sub.4 PO(OR.sub.4).sub.2, where R.sub.4 is independently alkyl of 1-20 carbons or phenyl, have anti-inflammatory activity.

Abstract: A process for the preparation of ascorbic acid-2-phosphate, which comprises reacting ascorbic acid or araboascorbic acid with a phosphate donor other than ATP in an aqueous medium in the presence of an effective amount of an enzyme derived and capable of preferentially catalyzing the enzymatic phosphorylation in the 2-position of ascorbic acid or araboascorbic acid by said phosphate donor, and recovering the resultant ascorbic acid-2-phosphate from the reaction solution.

Abstract: The invention is concerned with a process for the manufacture of ascorbyl phosphates, namely of phosphates of the formula ##STR1## wherein M.sup.k.sym. denotes a cation, k.sup..sym. denotes the valency and m denotes the equivalents, with the proviso that the product from k.m=3, by phsophorylating ascorbic acid.k is 1 to 3, especially 1 or 2.The process comprises using pre-formed sodium (or potassium) dichlorophosphate as the phosphorylating reagent, adding ascorbic acid to this pre-formed phosphorylating reagent in aqueous solution, especially at pH values between about 11.0 and about 13.0, in the presence of a water-soluble trialkylamine as the catalyst and at temperatures between about +10.degree. C. and about -8.degree. C., especially at temperatures below 0.degree. C., and, if desired, trans-salting the I which is obtained as the sodium (or potassium) salt and/or, if desired, purifying via an amine salt.