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: 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 a process for the preparation of symmetrically substituted phosphoric acid diesters of long-chain linear or branched alcohols of chain length C.sub.4 to C.sub.22.

Abstract: A versatile reagent with a non-nucleotide monomeric unit having a ligand, and first and second coupling groups which are linked to the non-nucleotide monomeric unit. The ligand can be either a chemical moiety, such as a label or intercalator, or a linking arm which can be linked to such a moiety. Such reagent permits preparation of versatile nucleotide/non-nucleotide polymers, having any desired sequence of nucleotide and non-nucleotide monomeric units, each of the latter of which bear a desired ligand. These polymers can for example, be used as probes which can exhibit enhanced sensitivity and/or which are capable of detecting a genus of nucleotides each species of which has a common target nucleotide sequence of interest bridged by different sequences not of interest.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme 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 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 invention relates to a process for preparing alkali metal salts and/or alkaline earth metal salts of alkylphosphonous acids and dialkylphosphinic acids from elemental yellow phosphorus and alkyl halides, which comprises carrying out the reaction in the presence of aqueous alkali metal hydroxide or alkaline earth metal hydroxide or mixtures thereof. The invention likewise relates to the use of the compounds prepared by the process according to the invention for preparing flame retardants, extraction media and plant protection agents.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to novel methods of using phosphonate derivatives, hydroxyphosphinyl derivatives, and phosphoramidate derivatives to inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme 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 includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.

Abstract: The invention relates to amphiphilic compounds of the general formula (I) with at least two hydrophilic and at least two hydrophobic groups based on di, oligo or polyolethers. The amphiphilic compounds of this invention are highly surface active and are suitable as emulsifiers, demulsifiers, detergents, dispersants and hydrotropes for industrial and domestic purposes, e.g. in the fields of metalworking, ore separation, surface treatment, washing and cleaning, cosmetics, medicine and food processing and preparation.

Abstract: The invention relates to a process for preparing dialkylphosphinate salts, which comprisesa) reacting elemental yellow phosphorus with alkyl halides in the presence of alkali metal hydroxide or alkaline earth metal hydroxide to form a mixture which comprises as main constituents the salts of alkylphosphonous, phosphorous and hypophosphorous acids,b) adjusting the mixture to a pH below 7 and then reacting the mixture with olefins in the presence of a free-radical initiator andc) reacting the dialkylphosphinic acids obtained according to b) and/or alkali metal salts thereof with metal compounds of Mg, Ca, Al, Sb, Sn, Ge, Ti, Zn, Fe, Zr, Ce, Bi, Sr, Mn, Li, Na and/or K to give the metal dialkylphosphinate salts.The invention likewise relates to the use of the metal dialkylphosphinate salts prepared by the process according to the invention to prepare flame retardants.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.

Abstract: A novel phosphoric acid-amino acid complex salt is provided which manifests insolubility in a neutral or alkaline aqueous solution and solubility in an acidic aqueous solution and has a basic amino acid, an alkaline earth metal, and phosphoric acid as main components thereof. An additive composition containing the complex salt and used in a feed for ruminant mammals excels in protection in the first compartment of the stomach of a ruminant mammal and solubility in the fourth compartment of the stomach. This additive composition improves the nutrition of the feed with respect to such a basic amino acid as lysine, a substance frequently missing in the feed for ruminant mammals.

Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.

Abstract: A bis(1,1,3,3-tetramethylbutyl)phosphinic acid compound represented by the formula (1) and an extracting agent using the same for separating Co from an aged electroless Ni plating solution.

Abstract: A process for synthesizing disulfides and sulfhydryl compounds which are useful pharmaceuticals. The process includes a two step, single pot process for preparing disulfides from an alkenyl sulfonate salt. The disulfides are useful as toxicity mitigating agents of chemotherapeutic drugs, such as certain platinum complexes, and as use therapeutic drugs for a variety of conditions in mammals.The two step process involves first the conversion of the starting reagent to a mercaptane sulfonate, then an oxidation to the desired disulfide.

Abstract: Salts of phosphonous acids are useful as flame retardants in plastics. Preferred salts are calcium or aluminum salts of phenylphosphonous acid and of methanephosphonous acid. Plastic molding materials rendered flame-retardant in this way are useful for manufacturing molded parts, especially electrical components, mechanical components, plugs, mounts, housings, coverings, sheathings and overcoatings.

Abstract: A bis(1,1,3,3-tetramethylbutyl)phosphinic acid compound represented by the formula (1) and an extracting agent using the same for separating Co from an aged electroless Ni plating solution. A di(1,1,3,3-tetramethylbutyl)phosphine is produced by carrying out a reaction between phosphine and trimethylpentene in the presence of an organic solvent and a catalyst, then said phosphine is reacted with an oxidizing agent or sulfur to obtain the compound (1): ##STR1## (wherein X.sup.1 and X.sup.2 are O or S).

Abstract: Disclosed is a method and solution for providing corrosion protection for electrical contact members. The contact members are exposed to the solution, which in one embodiment includes a phosphonate, a lubricant, and a solvent. In a preferred embodiment, the phosphonate is phosphonic acid, the lubricant is polyphenyl ether or tricresylphosphate, and the solvent includes an isoparaffinic hydrocarbon. In a further embodiment, the lubricant can be omitted from the solution.

Abstract: To provide 2,5-dicarboxyphenyl phosphonic acid and a process for the preparation thereof, comprising the steps of: forming a reaction liquid phase by supplying a 2,5-dialkylphenyl phosphonic acid, a solvent, a cobalt salt, a manganese salt and/or a cerium salt, and bromine or a bromine compound into a reaction zone; and supplying oxygen into the reaction liquid phase by bringing an oxygen-containing gas into contact with the reaction liquid phase by supplying an oxygen-containing gas into the above-mentioned reaction zone.

Abstract: New diphosphines in the form of ammonium carboxylates, sulfonates or phosphonates having a singly or multiply charged diphosphine anion and the corresponding number of ammonium cations as counter ions, and a process for their preparation useful as ligand in rhodium catalyst systems for hydroformylation of olefins.

Abstract: Tetracyclic compounds having the following structure are described: ##STR1## wherein R.sub.1 -R.sub.10 are as defined. The tetracyclic compounds are capable of potent effects on steroid sensitive tissues and have demonstrated increased uterine weight, antiovulatory effects and potent steroid receptor binding. The compounds have therapeutic utility in reproductive applications such as fertility control, labor induction, ovulation induction and spermatogenesis. Methods for preparing the tetracyclic compounds from substituted indanones are also described.

Abstract: Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N;(c) Q is covalent bond; O; or S;(d) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is C.sub.1 -C.sub.8 alkyl;(e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims.are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.

Abstract: The present invention includes compositions and methods of treatment for glutamate abnormalities and associated nervous tissue insult in a animal by inhibition of NAALADase enzyme. Compositions include glutamate-derived hydroxyphosphinyl derivative compounds, acidic peptide analogs, phosphinic acid derivatives and mixtures thereof that inhibit NAALADase enzyme activity and their use for treating glutamate abnormalities such as created by global and focal ischemia.

Abstract: The present invention relates to a process for preparing vinylphosphonic acids of the formula ##STR1## in which m is an integer from 1 to 20 by heating 2-chloroethylphosphonic acids of the formula ##STR2## in which n is an integer equal to or smaller than m, if desired in the form of a solution, in the absence or presence of a catalyst to a temperature of 180 to 350.degree. C. and eliminating hydrogen chloride and, where appropriate, water under atmospheric pressure or reduced pressure and, if desired, hydrolysing the vinylphosphonic acids of the formula (I).

Abstract: A process for synthesizing disulfides and sulfhydryl compounds which are useful pharmaceuticals. The process includes a two step, single pot process for preparing disulfides from an alkenyl sulfonate salt. The disulfides are useful as toxicity mitigating agents of chemotherapeutic drugs, such as certain platinum complexes, and as use therapeutic drugs for a variety of conditions in mammals.The two step process involves first the conversion of the starting reagent to a mercaptane sulfonate, then an oxidation to the desired disulfide.

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: Styrene phosphonic acid (SPA) can be formed the reaction of phosphorous acid with acetophenone, preferably in the presence of a Lewis acid catalyst, to form a hydroxy adduct intermediate thereof which is then reacted with acetic anhydride to form the acyl derivative of the hydroxy adduct, followed by removal of an acetic acid moiety therefrom, preferably in the presence of an acidic catalyst, to form the styrene phosphonic acid product.

Abstract: Compounds of formula (I), ##STR1## wherein R is a biphenyl group optionally substituted, by one or more substituents, the same or different selected among halogen atoms, hydroxy groups, alkoxy, alkyl thioalkyl or alkoxycarbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety, C.sub.1 -C.sub.3 alkyl groups containing one or more fluorine atoms, carboxy groups, nitro groups, amino or aminocarbonyl groups, acylamino groups, aminosulphonyl groups, momo- or di-alkylamino groups having from 1 to 6 carbon atoms in the alkyl moiety, mono- or di-alkylamino-carbonyl groups having from 1 to 6 carbon atoms in the alkyl moiety; R.sub.1 is a hydrogen atom, a straight or branched C.sub.1 -C.sub.

Abstract: The present disclosure relates to dipeptidase inhibitors, and more particularly, to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme inhibitors which are proposed as novel agents for the treatment of prostate cancer. NAALADase is enzyme which is a membrane-bound metalloprotease which hydrolyzes the dipeptide, N-acetyl-L-aspartate-L-glutamate (NAAG) to yield glutamate and N-acetylaspartate. The compounds of the present invention include phosphinic acid derivatives that inhibit NAALADase enzyme activity and which have been found useful for inhibiting the growth of prostate cancer cells.

Abstract: Preparing O,O'-diesters of thiophosphoric acid, O-monoesters of thiophosphonic acid or thiophosphinic acids and their salts, from diesters of phosphorous acid, monoesters of phosphorous acids or phosphinous acids and sulphur in the presence of an aqueous solution of an auxiliary base. The solutions can be used in further syntheses or as extraction agent for cations.

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 peptides described are modified with the phosphine group and are useful for marking with .sup.99m Tc and .sup.186-188 Re or paramagnetic agents for use in diagnosis and radiotherapy; in particular chelating compounds having the co-ordinating sets PN.sub.2 X, where X is --S, --O, COO--, PN.sub.3, P.sub.2 N.sub.3 and P.sub.2 N.sub.2 are described.

Abstract: Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops, these compounds having the general structure: ##STR1## These Polar compounds are particularly useful for systemic control of pests.

Abstract: Unsaturated compounds which can be dissolved in aqueous based solvents, such as ethylenic or acetylenic carboxylate or alcohols with less than 10 carbon atoms, especially maleic and/or acrylic acid or propargyl alcohol, are reacted with alkali metal phosphite in aqueous solution at neutral or alkaline pH in the presence of free radical initiators such as persulphate to form threshold scale and corrosion inhibitors.

Abstract: A versatile reagent with a non-nucleotide monomeric unit having a ligand, and first and second coupling groups which are linked to the non-nucleotide monomeric unit. The ligand can be either a chemical moiety, such as a label or intercalator, or a linking arm which can be linked to such a moiety. Such reagent permits preparation of versatile nucleotide/non-nucleotide polymers, having any desired sequence of nucleotide and non-nucleotide monomeric units, each of the latter of which bear a desired ligand. These polymers can for example, be used as probes which can exhibit enhanced sensitivity and/or which are capable of detecting a genus of nucleotides each species of which has a common target nucleotide sequence of interest bridged by different sequences not of interest.

Abstract: The compounds disclosed inhibit the prenylation of several proteins. These compounds are potent inhibitors of famesyl-protein transferase and geranylgeranyl-protein transferase. Further contained in this invention are chemotherapeutic compositions containing these prenyl-transferase inhibitors and methods for their production.

Abstract: This invention embodies a process for releasing acidic organic compounds in high yield and good purity from aqueous solutions of their salts which comprises converting the salts by carbon dioxide to their corresponding free acidic organic compounds and metal hydrogen carbonates, removing the acidic organic compounds from the mixture by extraction with an essentially water-insoluble organic solvent, and re-extracting the organic phase with carbon dioxide containing water. Using this process, the acidic organic compounds are completely released from their corresponding salts, i.e., the organic solution is free of salt. The acidic organic compounds released by the claimed process are organic compounds which contain acidic protons which can be replaced by metals. Some examples are carboxylic acids, sulfonic acids, phosphonic acids, phenols, naphthols, and aliphatic alcohols.

Abstract: A solid, non-hygroscopic salt of the Formula (I) ##STR1## wherein R.sup.1 is hydroxy or alkyl;A is C.sub.1 to C.sub.

Abstract: Disclosed is a process for removing by-product phosphorus-containing (PO.sub.x) materials, alendronate and alendronate byproducts from crude mother liquors in an omega amino-1-hydroxy-C.sub.2 -C.sub.6 alkylidene-1,1-bisphosphonic acid synthesis process, e.g. alendronate sodium. Calcium chloride is added first to the crude mother liquors, then calcium oxide to precipitate the PO.sub.x materials, then neutralized to about pH 7 to complete precipitation. Substantially all of the alendronate sodium active ingredient is removed from the precipitate. Following filtration, the PO.sub.x filtercake can then be disposed of by incineration, landfilling or reclamation of usable phosphorus as fertilizer. The remaining filtrate can then be further treated in an environmentally acceptable manner by wastewater treatment or recycling to the process.

Abstract: A series of tetrahydrophenanthrenes are useful as inhibitors of 5.alpha.-reductase.

Abstract: A coolant or antifreeze composition has one or more glycols or glycol ethers in combination with water, one or more additives, and an effective amount of one or more perfluoro-gem-diphosphonates as corrosion inhibitors.

Abstract: The invention provides compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein [D] is the residue of a drug having a reactive functional group, said functional group being attached, directly or through a bridging group, via an oxygen-phosphorus bond to the phosphorus atom of the ##STR2## moiety; R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.12 aralkyl; R.sub.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.4 -C.sub.9 heteroaryl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloheteroalkyl or C.sub.7 -C.sub.12 aralkyl; and R.sub.3 is selected from the group consisting of C.sub.1 -C.sub.8 alkyl; C.sub.2 -C.sub.8 alkenyl having one or two double bonds; (C.sub.3 -C.sub.7 cycloalkyl)--C.sub.r H.sub.2r -- wherein r is zero, one, two or three, the cycloalkyl portion being unsubstituted or bearing 1 or 2 C.sub.1 -C.sub.4 alkyl substituents on the ring portion; (C.sub.6 -C.sub.10 aryloxy)C.sub.1 -C.sub.

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 anti-arthritic agents and do not have the side effects of anti-arthritic agents which are prostaglandin synthetase inhibitors.

Abstract: A solid, non-hygroscopic salt of the Formula (I) ##STR1## wherein R.sup.1 is dydroxy or alkyl;A is C.sub.1 to C.sub.

Abstract: A soybean lecithin based topical liniment and method of making the same is disclosed. The liniment utilizes soybean lecithin as a base and major ingredient and as the emulsifier which is mixed with plant oils, natural menthol, calcium stearate, and magnesium stearate. The soybean lecithin, plant oils, natural menthol, calcium stearate, and magnesium stearate are mixed together in predetermined relative proportions with the amount of soybean lecithin being greater than the sum of the amounts of the plant oils, natural menthol, calcium stearate, and magnesium stearate. The soybean lecithin, plant oils, natural menthol, calcium stearate, and magnesium stearate are added to one another and mixed together in a predetermined sequence to prevent precipitation and provide a homogenous mixture having a viscosity suitable for topical application.

Abstract: A process for forming 1-phenylvinyl-1-phosphonic acid utilizes reacting a mixture of phosphorus trihalide, such as phosphorus trichloride, and acetophenone with water, under conditions in which the water is gradually added to the mixture with cooling to form a reaction mixture, which can be sparged of excess acetophenone with aqueous acid while under vacuum, comprising the 1-phenylvinyl-1-phosphonic acid. This product can be recovered from the reaction mixture by recrystallization from aqueous mineral acid, such as hydrochloric acid.

Abstract: Method of separating vinylphosphonic acid from crude mixtures.The invention relates to a method for separating vinylphosphonic acid from crude mixtures, the separation being carried out by extraction with alcohols and/or ketones, which in each case comprise at least 5 carbon atoms.According to the invention, vinylphosphonic acid can be obtained in high purity and good yield from highly contaminated crude mixtures.

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: A cycloalkyl phosphorus compound is obtained by the catalytic hydrogenation of a substituted or unsubstituted aryl phosphonic acid using a heterogeneous catalyst which is a Group VIII metal on carbon. The hydrogenation is preferably effected in water. The catalyst can be ruthenium or carbon. When phenylphosphonic acid is used as the starting material, a yield of about 95% of essentially pure cyclohexylphosphonic acid can be obtained.