Abstract: The present invention relates to a use of D-chiro-inositol, pinitol, or analog compounds thereof for preventing or treating female menopausal symptoms. The active ingredient compound of the present invention has an effect of increasing the activity of female hormones by increasing the blood concentration of 17?-estradiol and lowering the blood concentration of sex hormone-binding globulin. Therefore, the active ingredient compound of the present invention can be developed as a drug or a nutraceutical for preventing, alleviating or treating female menopausal symptoms. The active ingredient of the present invention is derived from a natural product, and thus, unlike an agonist of female sex hormones or chemically synthesized sex hormones, has very few side effects when applied to the human body.

Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.

Abstract: The present invention relates to unsaturated diphosphine monoxides, to a process for preparation thereof and to the use thereof as flame retardants.

Abstract: Mixtures of three types of linear, branched or cyclic phosphates are useful flame retardants, especially for thermoplastic resins or as functional additives in polymer matrices.

Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.

Abstract: The invention pertains to an oligomer or polymer substituted by one or more bisacylphosphine oxide moieties, characterized in that said bisacylphosphine oxide moiety is linked via the phosphorous atom, optionally via a spacer group, to the oligomer or polymer backbone; as well as to specifically functionalized bisacylphosphine oxides, suitable to prepare said polymers or oligomers.

Abstract: The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, ?-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.

Abstract: The invention relates to the use of para-coumaric acid or para-hydroxycinnamic acid derivatives in cosmetic or dermatological compositions, specifically to the use of at least one compound derived from para-coumaric acid having a general formula (I) below: in which, especially, Z represents an oxygen or an —NH— group; X and Y are identical and each represent a CH or CH2 group, as an active principle with depigmenting, free-radical-scavenging and/or antiinflammatory is activity. The invention also relates to the use of the above compounds for cosmetic care or for the preparation of a pharmaceutical composition, especially for depigmenting an area of skin, having antiradical and/or antiinflammatory activity.

Abstract: The present invention provides a chemical compound or a salt thereof having the chemical formula of: wherein said R is H or citrate and wherein at least one R is citrate. The salt of the chemical compound is the Na+, K+, Mg2+, or Ca2+ salt of said chemical compound. The chemical compound is a chelator which chelates sodium, potassium or lithium, magnesium, calcium, copper, iron, lead, zinc, aluminum, mercury, cadmium, or chromium. It is also be used as an artery plaque dissolver and/or to treat age-related degenerative disorders, such as Alzheimer's disease. The present invention also provides a method for producing the phytic citrate compound and/or its salt.

Abstract: The present invention relates to novel compounds which are capable as acting as fluorescent sensors or which are precursors for these and for the use of these for the assay of biological processes such as posttranslational modifications of biological molecules such as phosphorylation, de-phosphorylation, proteolytic cleavage, phosphodiesterase mediated hydrolysis of cyclic nucleotides, methylation, acetylation of proteins peptides, DNA, lipids and the detection of biomolecule interactions (e.g., protein-protein interactions). A small molecule sensor is described which can associate to phosphorylated biological targets via metal ion—phosphate association. The association event can be monitored as fluorescence quench, sensitized emission, fluorescence polarization or a combination thereof.

Abstract: The present invention concerns conjugate compounds comprising a bisphosphonate covalently bonded to a prostatic acid phosphatase inhibitor and compositions comprising such conjugates. Methods for treating and inhibiting prostate cancer bone metastases, and determining whether a conjugate is useful for such treatment are also provided. In some instances, the bisphosphonate is alendronate, and it is covalently bonded to either tartaric acid or glyceric acid.

Abstract: The invention relates to thermoplastic molding compositions comprising A) from 39 to 99% by weight of at least one thermoplastic polymer, B) from 1 to 60% by weight of a flame-retardant component comprising B1) a compound of the formula (I), and C) from 0 to 60% by weight of further additives, where the percentages by weight are always based on the total weight of components A) to C) and their total is 100% by weight, and also to processes for the preparation of these molding compositions, to the use of these molding compositions for the production of moldings, of fibers, of foams, or of foils, and also to the resultant moldings, fibers, foams, or foils and moreover to the use of the compound of the formula (I) as flame retardant for thermoplastic polymers.

Abstract: The present invention relates to hydroxy-bisphosphonic acid derivatives corresponding to general formula (I): in which: -n and m denote, independently of one another, an integer ranging from 1 to 4, —X denotes an oxygen atom or an N—R3 group, —R1 and R3 denote, independently of one another, a linear or branched C1 to C6 alkyl group, and —R2 denotes a residue of a molecule of therapeutic or diagnostic interest, or pharmaceutically acceptable salts of said derivatives, and also the method for the preparation thereof and the therapeutic or diagnostic use thereof.

Abstract: The invention provides, inter alia, novel bisphosphonate compounds and methods of making and using. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor cell growth inhibition, activation of gammadelta T cells, inhibition of farnesyldiphosphate (FPPS) and/or undecaprenyldiphosphate synthase enzymes, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases. In regards to certain embodiments, a surprising advance has been the recognition that certain structural features can significantly enhance the activity of the compounds. For example, the presence of particular cationic species e.g., phosphonium, sulfonium, and arsonium moieties can contribute to desirable functional activity when positioned near a bisphosphonate moiety. In other embodiments of non-nitrogen containing bisphosphonates, terphenyl and benzyl bisphosphonate compounds and methods are provided. Further variations are also provided.

Abstract: The present invention provides novel bisphosphonate conjugates, pharmaceutical compositions comprising bisphosphonate conjugates and methods of using such analogs in the treatment of bone cancer, bone-related diseases, bone infection, bone inflammation, and diseases of the soft tissues surrounding bones.

Abstract: The present invention relates to solid amorphous and crystalline forms of ibandronate sodium.

Abstract: A system which is suitable as a catalyst for the hydrocyanation of olefinically unsaturated compounds and comprises a) Ni(0) b) a compound which complexes Ni(0) as a ligand and contains trivalent phosphorus, c) a Lewis acid and d) a compound of the formula M Rn where M: Al or Ti R: identical or different monovalent alkoxy radicals, in which case a plurality of alkoxy radicals may be bonded together, and additionally, in the case that M=Al, R may be identical or different monovalent alkyl radicals, in which case a plurality of alkyl radicals may be bonded together or one or more alkyl radicals may be bonded to one or more of the abovementioned alkoxy radicals, n: valency of M, and processes for hydrocyanating an olefinically unsaturated compound in the presence of such a system.

Abstract: The present invention provides a chemical compound or a salt thereof having the chemical formula of: wherein said R is H or citrate and wherein at least one R is citrate. The salt of the chemical compound is the Na+, K+, Mg2+, or Ca2+ salt of said chemical compound. The chemical compound is a chelator which chelates sodium, potassium or lithium, magnesium, calcium, copper, iron, lead, zinc, aluminum, mercury, cadmium, or chromium. It is also be used as an artery plaque dissolver and/or to treat age-related degenerative disorders, such as Alzheimer's disease. The present invention also provides a method for producing the phytic citrate compound and/or its salt.

Abstract: Novel phosphonate compounds are provided including a phosphonoglyoxylamide ester, an ?-keto phosphonophosphinate ester, a carbonylbisphosphonate analog of a nucleotide, and a diazomethylenebisphosphonate analog of a nucleotide, as well as methods of making synthetically and medically useful ?-keto phosphonate compounds.

Abstract: The present invention describes organophosphorus compounds of general formula (I) their preparation and their uses in the activation of gamma/delta T-cells, in the screening of GcpE and LytB enzyme inhibitors and in the prophylaxis and treatment of diseases in humans and animals.

Abstract: Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.

Abstract: The present invention discloses mono-, bis- and tris-nonylcyclohexylphosphite esters, polyolefin compositions stabilized against the deleterious effects of melt processing, heat aging and exposure to combustion products of natural gas which comprise the nonylcyclohexylphosphite esters as stabilizers, and a process towards stabilizing polyolefin compositions by incorporating in or applying thereto the nonylcyclohexylphosphite esters.

Abstract: Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): R1 and R2 are independently —H, an electron withdrawing group or a C1–C10 alkyl group. Y is a covalent bond, a substituted methylene group, an unsubstituted methylene group or —CR1R2P(O)(OH)—. R3 is a hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a substituted hydrocarbyl group optionally comprising one or more amine, ammonium, ether, thioether or phenylene linking groups, a heteroaryl group, a substituted heteroaryl group or a phenyl group substituted with one or more groups selected from —Cl, —Br, —F, —CN, —NO2, —ORa, —N(Ra)2, —COORa, —CON(Ra)2, —CORa, —S(O)Ra, —S(O)2Ra, —S(O)2N(Ra)2, —NRaS(O)2Ra, —NRaCORa, a halogenated lower alkyl group, an aryl group, a substituted aryl group, or a halogenated alkoxy group. Each Ra is independently —H, lower alkyl, substituted lower alkyl, aryl or substituted aryl.

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: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: A novel antioxidant has the advantages of both the hindered phenols and the phosphite antioxidant is prepared from phosphorus trichloride and 2,5-di-tert-butylhydroquinone, such as tetrakis-(2,5-di-tert-butyl-4-hydroxyphenyl)-2,5-di-tert-butyl-hydroquinonediyl diphosphite.

Abstract: The invention provides compounds of formula I: wherein X, R1, R2, and n have any of the values defined in the specification, and their pharmaceutically acceptable salts. The compounds are useful, for example, for blocking prenylation transferase enzymes, for probing or diagnosing protein prenylation processes, and for treating cancer in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and intermediates useful for the synthesis of compounds of formula I.

Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biologically active compounds, and the compounds which may be synthesized from such intermediates.

Abstract: Disclosed is a phosphate transport inhibiting compound represented by Structural Formula (I): 1

Abstract: The invention concerns compounds CH3—R1—(CH1)2—R2 wherein: R1 is selected among a tertiary alcohol; a 1,2-diol; a halohydrine; an apoxide; an alkene; an aldehyde or an &agr;-hydroxyaldehyde; and R2 is selected among a methylenediphosphonate; a difluoromethylenediphosphonate; or a monofluoromethylenediphosphoneate. The invention also concerns the uses of said compounds as selective inhibitors of T&ggr;9&dgr;2 lymphocytes, and their uses, in particular for therapeutic purposes.

Abstract: Compounds of formula (I), wherein each of R and R′ are independently selected from hydrogen, a hydroxyl group, a carboxyl group, an alkyl, aryl or alkaryl group or a hydroxy or carboxy substituted alkyl, aryl or alkaryl group, provided that R R′, together have a total of less than 23 carbon atoms, R″ may either be hydrogen or a CHR═CR1 group or be selected from the same categories as R′″; R′″ is a group, or polymeric chain comprising from 1 to 100,000 groups, said group or groups being derived form at least one ethylenically unsaturated compound wherein the double bond is activated by an adjacent electron withdrawing group, and n is greater than 1 are novel, are useful corrosion inhibitors and are valuable intermediates in preparing telomers for use in water treatment.

Abstract: A flame retardant composition is produced by mixing a flammable organic material with an organic phosphorus-inorganic phosphorus oxyacid compound or its salts. The organic phosphorus-inorganic phosphorus oxyacid compounds are produced by reacting an organic phosphorus compound with an inorganic phosphorus oxyacid. The organic phosphorus-inorganic phosphorus oxyacid compound may be reacted with a basic salt forming compound. The flammable organic material such as thermoplastic resins are made less flammable by melting-kneading the flammable material with the organic phosphorus-inorganic phosphorus oxyacid compound or it's basic salt, carbonization auxiliaries, a metal-containing compound having a carbonization acceleration effect, a comb-like polymer and a filler.

Abstract: The invention provides compounds of formula I: 1

Abstract: Chiral, unsymmetrical bidentate organophosphorus ligands of the formula (I) are reacted with transition metal centers to form complexes with catalytic activity. The compounds contain chiral bicycloaliphatic skeletons. Synthesis of the bidentate ligands proceeds from norbornyl derivatives.

Abstract: 3,3′-Substituted chiral biaryl phosphine and phosphinite ligands and metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. The metal complexes are useful as catalysts in asymmetric reactions, such as, hydrogenation, hydride transfer, allylic alkylation, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, olefin metathesis, hydrocarboxylation, isomerization, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition, epoxidation, kinetic resolution and [m+n] cycloaddition. The metal complexes are particularly effective in Ru-catalyzed asymmetric hydrogenation of beta-ketoesters to beta-hydroxyesters and Ru-catalyzed asymmetric hydrogenation of enamides to beta amino acids.

Abstract: A description is given of compounds of the formula in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.

Abstract: The present invention provides novel compounds that function as immunological adjuvants when co-administered with antigens, including, antigens used as vaccines for any disease or condition amenable to vaccination. The invention also provides adjuvant formulations comprising the novel compounds of the invention and methods for immunizing humans and non-human animals.

Abstract: Novel chiral amidophosphine-phosphinite compounds, which are present in (R) and (S) form, of the general formula wherein R1 signifies alkyl, cycloalkyl or aralkyl, R2 signifies alkyl, cycloalkyl, aralkyl or aryl and R3 and R4 each independently signify alkyl, cycloalkyl, aralkyl, aryl or heteroaryl or R3 and R4 together with the respective phosphorus atom signify a 9-dibenzophospholyl, 9-phosphabicyclo[3.3.1]nonyl or 9-phosphabicyclo[4.2.1]nonyl group and * denotes a chiral center, are manufactured by reacting a compound of the general formula R1C(OH)—CONHR2 (III) with a disubstituted chlorophosphane of the general formula R3R4PCl (IV) in a solvent and in the presence of a base.

Abstract: Disclosed are novel bicyclic tris(anhydride)s useful as intermediates in the synthesis of biolologically active compounds, and the compounds which may be synthesized from such intermediates.

Abstract: The present invention is directed to presqualene diphosphate (PSDP) analogs having an active region of natural PSDP and a metabolic transformation region resistant to rapid intracellular inactivation in vivo. For example, PSDP and its stable analogs can inhibit neutrophil signal transduction events in cellular activation that result in the generation of active oxygen species, regulation of leukocyte adherence, both homotypic (leukocyte-leukocyte) or heterotypic adherence with leukocytes and epithelial cells of mucosal origin or endothelial cells of vascular origin. These analogs can also be used to regulate leukocyte-dependent tissue injury.

Abstract: This invention is directed to process for making a composition having the formula (I): ##STR1## wherein R.sup.3, R.sup.4, and R.sup.5 are independently hydrogen, substituted or unsubstituted hydrocarbyl, or an agronomically acceptable cation. The process comprises contacting a solution with a noble metal catalyst and introducing oxygen into the solution. The solution contains an N-substituted glyphosate having the formula (II): ##STR2## wherein R.sup.1 and R.sup.2 are independently hydrogen, halogen, --PO.sub.3 H.sub.2, --SO.sub.3 H, --NO.sub.2, or substituted or unsubstituted hydrocarbyl other than --CO.sub.2 H. R.sup.3, R.sup.4, and R.sup.5 are as defined for formula (I).This invention also relates to an oxidation catalyst comprising a noble metal having a hydrophobic electroactive molecular species adsorbed thereon.

Abstract: A description is given of compounds of the formula ##STR1## in which the general symbols are as defined in claim 1, and of their zirconium, bismuth and calcium salts, and of the salts with the compounds of the formula II ##STR2## in which the general symbols are as defined in claim 1, as corrosion inhibitors in coating compositions for protecting metallic surfaces.

Abstract: Phospholipid derivatives containing higher elements of the Vth main group (P, As, Sb, Bi), their method of preparation and antineoplastic and antimicrobially active medications that can be prepared from the phospholipid derivatives.

Abstract: Novel chemotherapeutic agents having utility in treating infectious diseases such as periodontal disease, certain urinary tract infections, and infectious urinary tract stones, are obtained by combining chemically a diphosphonate compound with a therapeutic agent effective against the foregoing diseases.

Abstract: Wittig-type reagents and methods of preparation and use thereof for preparing .alpha.,.beta.-unsaturated phosphonate esters from aldehydes and ketones are disclosed. The Wittig-type reagents have the following formulae: ##STR1## wherein X represents triflate, halide, BF.sub.4, SbF.sub.6, or ClO.sub.4 ; R.sub.1 represents alkyl, aryl or arylalkyl; and R.sub.2 represents alkyl, aryl or arylalkyl, provided that R.sub.1 and R.sub.2 not represent phenyl at the same time. The Wittig reagent diethyl phosphono-methylidenetriphenylphosphorane (1b) has been successfully synthesized for the first time via its phosphonium triflate salt (4a), by treating diethyl phosphonomethyltriflate with triphenylphosphine according to the disclosed method. The procedure has been applied to the synthesis of other new Wittig-type reagents such as phosphoranes and phosphonium salts. The new Wittig reagents thus synthesized were treated with various aldehydes and an activated ketone, affording the corresponding .alpha.,.beta.

Abstract: Tertiary phosphines of the formula (I) ##STR1## in which X is a phosphinate or phosphonate group, are prepared by a palladium-catalyzed coupling of p-, m- or o-bromofluorobenzenes with alkyl akylphosphonous acid ester or alkyl alkylphosphite ester and reacting the resulting alkyl fluorophenylphosphinates or alkyl fluorophenylphosphonates with a metal phosphide.

Abstract: A process for extracting metal values, especially zinc values, from aqueous solutions of metal salts, which comprises contacting the aqueous solution with an organic phase comprising a compound of the formula, ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4, independently, represents an optionally substituted hydrocarbyl or hydrocarbyloxy group or R.sup.1 and R.sup.2 together with the attached phosphorus atom and/or R.sup.3 and R.sup.4 together with the attached phosphorus atom from a 5- to 8-membered heterocyclic ring.

Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.

Abstract: Lubricant and fuel compositions containing a small additive concentration of a novel organo-phosphorus composition based on phosphite-derived hydroxyl compounds and amine phosphates possess excellent antiwear properties coupled with good extreme pressure activities. Additional antioxidation, cleanliness, antifatigue, high temperature stabilizing, and friction modifying properties are expected. Both the phosphite-hydroxy moiety and the amine phosphate moiety are believed to provide the basis for the synergistic antiwear and EP property of these novel additives.

Abstract: This invention is directed to a method for stimulating the proliferation of V.gamma.2V.delta.2 T cells comprising contacting V.gamma.2V.delta.2 T cells with a V.gamma.2V.delta.2 T cell proliferation stimulating amount of a compound selected from the group consisting of a monoalkyl phosphate and an alkenyl pyrophosphate.