Abstract: Compounds useful as surface coating agents, including compounds of the formula: 1

Abstract: Compounds useful as surface coating agents, including compounds of the formula: wherein X1 comprises a first photoreactive species; X2 comprises a second photoreactive species; Y comprises a nonpolymeric core molecule comprising an aromatic group; and Z comprises at least one charged group. The Y core can include an aromatic group such as a benzene radical, the charged groups Z can be independently selected from the organic acids that include sulfonic acid, carboxylic acid, and phosphoric acid, and the photoreactive species of X1 and X2 can independently be aryl ketones, such as those selected from the group acetophenone, benzophenone, anthraquinone, anthrone, and anthrone-like heterocycles, and their substituted derivatives.

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: The invention provides a compound of formula (I): 1

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: The invention provides a compound of formula (I): 1

Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and conditions related to diabetes.

Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related conditions.

Abstract: The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

Abstract: Preparations of pyrophosphate analogues, including phosphonoformic acid, bisphosphonic acid, and phosphonoacetic acid derivatives, exhibiting antiviral activity. Such compounds, are used directly, or as prodrugs, in compositions and methods for treating viral infections, including but not limited to HIV, herpesviruses including HSV, EBV, VZV, CMV, HHV-6 and HHV-8 (Kaposi's sarcoma); HPV; rhinoviruses; and hepatitis-linked viruses. Compounds of the present invention for use as antiviral agents or their intermediates include sulfur-containing, polyhydroxy, and lipophilic derivatives of phosphonoformic acid.

Abstract: A process for oxidizing a hydroxymethylphosphonic acid compound to produce a formylphosphonic acid compound is described. The oxidation reaction is carried out in the presence of an oxidant and a catalyst. For example, hydroxymethylphosphonic acid (HMPA) is oxidized by oxygen or hydrogen peroxide in the presence of a copper-containing catalyst to give formylphosphonic acid (FPA). Formylphosphonic acid can then be reacted with glycine to produce a condensation product which, upon hydrogenation, yields glyphosate. Glyphosate can be incorporated into various formulations for use as a herbicide. In addition to glycine, formylphosphonic acid can also be reacted with ammonia, ethanolamine, or other primary amines to form a precursor compound, which can be converted to glyphosate.

Abstract: Preparation of phosphonoformic acid analogues containing one, two, three, or more sulfur atoms are described, with specific examples. Such compounds, not excluding cognates, derivatives, and homologues thereof, are proposed to be used directly, or as prodrugs, in treating viral infections, including but not limited to HIV, herpesviruses including HSV, EBV, VZV, CMV, HSV-6 and HSV-8 (Kaposi's sarcoma); HPV; rhinoviruses; and hepatitis-linked viruses. They are also proposed to be used in treating neoplasms, and for diagnosis and therapy of diseases of bone metabolism. The compounds of the present invention are also designed as to create novel biologically active compounds or prodrugs.

Abstract: An improved hydrolysis process comprising a process for the preparation of 2-carboxyalkyl(aryl)phosphinic acid using a controlled addition of water to an acrylation reaction mixture, and control of the temperature. Preparation of 2-carboxyalkyl(aryl)phosphinic acid cyclic anhydride is disclosed using a controlled addition of water, wherein up to about one mole of water per mole of dichloro(aryl)-phosphine charged to the acrylation reaction is added, and temperature is controlled.

Abstract: There is described the use of a compound represented by general formulae (I), (II) or (III), for the inhibition of matrix metalloproteinases (MMP), wherein X1 is oxygen or sulfur, R1 is OH, SH, CH2OH, CH2SH or NHOH, R2 is a residue of 2 to 10 hydrocarbon backbone atoms, which binds to the amino acid 161 of HNC, said residue being saturated or unsaturated, linear or branched, and contains preferably homocyclic or heterocyclic structures, X2 is oxygen or sulfur and binds as hydrogen acceptor on amino acid 160 of HNC, Y is a residue which binds to the S1′ pocket of HNC and consists of at least 4 backbone atoms Z1-Z2-Z3-Z4-R3, and R3 is n-propyl, isopropyl, isobutyl or a residue with at least 4 backbone atoms, which is not larger than a tricyclic ring system. These compounds bind to MMPs in a manner different from the mode of binding of the inhibitors of the state of the art.

Abstract: Glufosinate and the 2-methyl analog thereof can be prepared in a multi-step synthesis from methylphosphorus compounds (II) with unsaturated keto compounds (III) via adducts (IV), subsequent reaction under the conditions of a Strecker synthesis and finally hydrolysis of the aminonitrile (V): Step 1: Step 2: Step 3: Hydrolysis of (V) to give glufosinate Depending on process conditions and substrates, various compounds can be identified as adducts (IV).

Abstract: The present invention is directed to multibinding compounds which are &bgr;3 adrenergic receptor agonists and are therefore useful in the treatment and prevention of metabolic disorders such as obesity, diabetes, and the like.

Abstract: Opticallly active adsorbents based on network polymerized derivative of dicarboxylic acids, diamines or diols which are chemically bonded to a carrier. The derivatives can be polymerized by radical polymerization or through hydrosilylation in the presence of a solid carrier. The optically active adsorbents are usable for chromatographic separation of racemic mixtures of enantiomers.

Abstract: The present invention provides compounds represented by the following general formula [I] and salts thereof, which are useful as therapeutic agents for glaucoma, wherein R1 is H, lower alkyl or phenyl, and the phenyl can be substituted by lower alkyl, hydroxy, lower alkoxy, halogen, nitro or phenyl; R2 and R3, being the same or different, are H, halogen or lower alkyl; R4 and R5, being the same or different, are H, lower alkyl or carboxyl or ester thereof; and R6 is carboxyl or phosphono or ester thereof.

Abstract: Processes for producing 2-carboxyalkyl(phenyl)phosphinic acid comprising hydrolyzing the reaction mixture produced from the reaction of dichloro(phenyl)phosphine with a carboxylic acid in the presence of water, wherein the hydrolysis is conducted with reduced levels of water.

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: Formylphosphonic acid derivatives are prepared by the catalytic decomposition of a (phosphonomethyl)amine N-oxide compound to form the formylphosphonic acid derivative and a dephosphonomethylated amine.

Abstract: An improved process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.

Abstract: Phosphonic acid agents are synthesized and characterized which are potent inhibitors of angiogenesis, tumorigenesis and metalloproteinase activity. Their method of use for the inhibition of angiogenesis and metalloproteinase and the treatment of tumors is also shown.

Abstract: Disclosed is a method for the preparation of 3-(hydroxyphenylphosphinyl)-propanoic acid which is commonly used as a flame retardant for polyester resins. The preparation of 3-(hydroxyphenylphosphinyl)-propanoic acid is attained by the condensation of phenylphosphonous dichloride and acrylic acid and the hydrolysis of the condensate. In the condensation, the mole ratio of phenylphosphonous dichloride to acrylic acid is within the range of 1:1.1 to 1:1.25. Under a pressure of greater than 1 atm, acrylic acid is added at 65.about.110.degree.C. at an amount more by 10.about.25 mole % than that of phenylphosphonous dichloride and the condensation is carried out at a temperature of 70.about.100.degree. C. under at greater than 1 atm, to produce 3-(hydroxyphenylphosphinyl)-propanoic acid at high yields with desired color.

Abstract: The present invention relate to phosphinic alkanoic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising the same, and methods of using the same to inhibit NAALADase activity and to treat glutamate abnormalities and prostate diseases.

Abstract: A process for the manufacture of formylphosphonic acid derivatives is reported. An aminomethylphosphonic acid substrate is contacted with a reagent selected from the group consisting of water, an alcohol, a phenol compound, and mixtures thereof and an oxidizing gas in the presence of a catalyst to form a reaction product mixture containing a formylphosphonic acid derivative and the conditions under which said contacting is carried out are controlled so that no more than 50% of the formylphosphonic acid derivative formed in the reaction product mixture is consumed by reaction with the reagent.

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: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate 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, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

Abstract: The present invention relates to asymmetric syntheses and intermediates for preparing enantiomer-enriched hydroxyphosphinyl derivatives.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate 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, and to treat prostate diseases, especially using the compounds of the present invention for the inhibition of the growth of prostate cancer cells.

Abstract: A dialkyl dialkoxycarbonylphenylphosphonate which is useful as a resin modifier, a process for producing the same in high yield at a low cost, and a process for producing a dicarboxyphenylphosphonic acid in high yield at a low cost are described.The process for producing a dialkyl dialkoxycarbonylphenylphosphonate comprises heating and reacting a dialkoxycarbonylphenyl halide with a trialkyl phosphate in the presence of a catalyst comprising an element of group VIII of the periodic table (such as an alumina supported palladium catalyst) and hydrolyzing the obtained dialkyl dialkoxycarbonylphenylphosphonate in the presence of an acid or base to produce a dicarboxyphenylphosphonic acid.

Abstract: The present invention is based upon the surprising discovery that NAALADase inhibitors exhibit a significant inhibitory effect on the growth of prostate cancer cells. The present disclosure relates to methods of treating diseases of the prostate, in particular prostate cancer, using novel compositions which inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity in humans and warm-blooded animals. Furthermore, as NAALADase has been found in other tissues of the body it may serve as a cancer associated protein and thus NAALADase inhibitors would be expected to show efficacy in the treatment of other forms of cancer.

Abstract: The present invention includes compounds, compositions, and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include phosphonate derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia and for treatment of prostate disease and prostate cancer by inhibition of NAALADase enzyme.

Abstract: There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.

Abstract: The present invention relates to catalytic asymmetric hydrogenation of phosphorus analogs of itaconic acid to synthesize novel optically active phosphono succinates.

Abstract: The present invention relates to phosphonsulfonates and the pharmaceutically-acceptable salts and esters thereof, having the following structure according to formula (I): ##STR1## The present invention further relates to pharmaceutical compositions containing a safe and effective amount of a compound of the present invention, and pharmaceutically-acceptable excipients. Finally, the present invention relates to methods for treating or preventing pathological conditions characterized by abnormal calcium and phosphate metabolism in humans or other mammals, including treating or preventing osteoporosis and arthritis, especially rheumatoid arthritis and osteoarthritis. This method comprises administering to a human or other mammal in need of such treatment of a safe and effective amount of a compound or composition of the present invention.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: 1 A process for producing a purified organophosphorus alkyl ester compound in which the reaction mixture obtained by reacting a dichlorophosphine derivative with (meth)acrylic acid is esterified with a lower monool, and the resulting reaction mixture is neutralized with an alkali metal hydroxide or alkaline earth metal hydroxide either in a solid form or in the form of an aqueous solution and purified; 2 a process for producing a purified organophosphorus hydroxyalkyl ester compound or an alkylene glycol solution thereof which comprises subjecting the purified organophosphorus alkyl ester compound obtained by process 1 to transesterification with an alkylene glycol; 3 a reactive flame retardant comprising the purified organophosphorus alkyl ester compound obtained by process 1; and 4 a reactive flame retardant comprising the purified organophosphorus hydroxyalkyl ester compound or alkylene glycol solution obtained by process 2.

Abstract: Compounds of formula I are disclosed, ##STR1## as well as processes for their production and pharmaceutical agents containing these compounds suitable for treating disorders of calcium metabolism.

Abstract: This invention relates to an improved process for the production of 2-phosphono-butane-1,2,4-tricarboxylic acid (PBTC) and the alkali metal salts thereof, in which process dialkyl phosphite, preferably dimethyl or diethyl phosphite, and ethene-1,2-dicarboxylic acid dialkyl ester, in particular the dimethyl or diethyl ester of maleic acid and/or fumaric acid, are initially reacted in the presence of a basic catalyst to yield a phosphonosuccinic acid tetraalkyl ester, the resultant ester is thereupon reacted without further working up with acrylic acid alkyl ester, preferably methyl or ethyl acrylate, in the presence of an alkaline catalyst and the reaction product obtained in this manner is saponified without further working up to yield PBTC or the alkali metal salts thereof. The product when mixed with bleaching lye exhibits reduced chlorine depletion.

Abstract: The present invention provides arylthioalkyl- and arylthioalkenylphosphonic acids and derivatives thereof having the structural formula I ##STR1## Further provided are compositions and methods comprising those compounds for the control of undesirable plant species.

Abstract: The invention relates to caged compounds for the study of biological processes, where the caged compound has a photoremoveable .alpha.-carboxy-substituted o-nitrobenzyl group. Covalent attachment of the substituted o-nitrobenzyl to a parent compound yields a caged compound with biological and/or physical properties that are significantly altered from the original properties of the parent compound. Illumination of the caged compounds to cleave the photoremoveable group yields the parent compound with its original properties restored.

Abstract: The present invention relates to a method for the synthesis of foscarnet, i.e. trisodium phosphonoformate hexahydrate, comprising the steps of adding sodium hydroxide to water, heating the aqueous sodium hydroxide solution to 50.degree. C., adding triethyl phosphonoformate to said solution at 50.degree. C., heating the reaction mixture to reflux for about 1 hour, cooling of the reaction mixture and filtering-off of the product.

Abstract: The present invention provides a compound which has a fluoroalkyl group, a lipophilic group (an alkyl group) and a hydrophilic group in the same molecule.

Abstract: The present invention relates to certain inhibitors of farnesyl:protein transferase which are useful as antineoplastic agents.

Abstract: PLA.sub.2 inhibitors selected from the group consisting of ##STR1## wherein A is selected from the group consisting of ##STR2## and Z, W, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, X, X' and Y are as defined herein.

Abstract: The invention relates to acyl-(2'-hydroxydiphenyl-2-yl)-phosphinic acid salts of formula (I) ##STR1## in which each of the radicals R.sup.1, R.sup.2 and R.sup.3 may be included singly or multiply and in which R.sup.1 and R.sup.2 are mutually independently hydrogen, an alkyl or alkoxy radical with 1 to 6 carbon atoms or halogen with an atomic number of 9 to 35; R.sup.3 means the same as R.sup.1 or R.sup.2 ; Ar is an aromatic hydrocarbon radical with 6 to 10 carbon atoms; and Me is a cation of at least one alkaline metal or N(R.sup.4).sub.4 + in which the radicals R.sup.4 are the same or different and stand for an alkyl radical with 1 to 6 carbon atoms. The invention also relates to a process for producing these compounds (I) and their use as photoinitiators in photopolymerisable materials, preferably on an aqueous basis.

Abstract: Phosphonic (co) telomers of the type described in U.S. Pat. Nos. 4,046,707 and 4,681,686 and European Patent Application 360746 may be produced by an aqueous process comprising (a) reacting hypophosphorous acid with a carbonyl compound which is preferably an aldehyde, a ketone or an imine, (b) reacting the product of (a) with an olefin or olefins in the presence of a suitable initiator especially a free radical initiator, and (c) converting the product obtained from (b) to a phosphonic (co) telomer, e.g., by reaction with hypochlorite. The (co) telomer products are useful as scale inhibitors in aqueous systems.

Abstract: The present invention is directed to farnesyl pyrophosphate analogs which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention, and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.