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 bis(aminomethyl)phosphinic acid derivatives and process for the preparation of bis(aminomethyl)phosphinic acid derivativesCompounds of the formula VI ##STR1## can be prepared by reaction of a compound of the formula IV ##STR2## with a base to give a compound of the formula Va or Vb ##STR3## and subsequent reaction with carbon nucleophiles; alternatively the compound of the formula VI is prepared by direct reaction of the compound of the formula IV e.g. with R.sup.2 Cu(CN)Li.sub.2, the above substituents having the meanings mentioned.

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: 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 form a 5- to 8-membered heterocyclic ring.

Abstract: Substituted 1,3,2,4-diazadiphosphetidines of formula I ##STR1## where preferably, R.sub.1 and R.sub.2 are branched alkyl or aryl, m and n are 1, p and q are 0, and YR.sub.3 and XR.sub.4 are substituted --O--phenyl or --N(alkyl).sub.2, are excellent stabilizers for organic materials, particularly polyolefins.

Abstract: The present invention provides a phosphorus-containing isoprenoid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is useful as a preventive and therapeutic agent for diseases for which a squalene synthetase inhibiting action is efficacious: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group: R.sup.3 and R.sup.4 each represent a hydrogen atom, a lower alkyl group or an alkali metal; Y represents a group represented by the formula: ##STR2## (wherein R.sup.5 and R.sup.6 each represent a hydrogen atom, a lower alkyl group or an alkali metal or a group represented by the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group or an alkali metal); Z represents a group represented by the Formula: --(CH.

Abstract: The invention relates to a new compound of the formula (1): ##STR1## wherein m.sub.1 =0, 1 or 2, m.sub.2 =0, 1 or 2, m.sub.1 and m.sub.2 are not to be simultaneously 0 or simultaneously 2; n.sub.1 =2-m.sub.1, n.sub.2 =2-m.sub.2 ; R=either H or alkyl with 1 to 8 carbon atoms, R'=alkyl with 1 through 18 carbon atoms, and X=H or OH.The invention also relates to the preparation thereof, the compositions containing them and the application in catatlysis of oxidation of hydrocarbons, particularly in catalysis of oxidation of cyclohexane.

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: Diphosphonic acids of formula (I) are useful as antitumor agents.

Abstract: The invention relates to novel methylenebisphosphonic acid ester amide derivatives of general formula (I), in which formula W.sup.1, W.sup.2, W.sup.3 and W.sup.4 are independently the group OR.sup.1 or the group NR.sup.2 R.sup.3 wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or straight or branched, optionally unsaturated C.sub.1 -C.sub.22 -alkyl, optionally substituted, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl or silyl SiR.sub.3, or the groups R.sup.2 and R.sup.3 form together with the adjacent nitrogen atom a 3 to 10-membered saturated, partly saturated or aromatic heterocyclic ring, wherein in addition to the nitrogen atom, there may be one or two heteroatoms from the group N, O and S, provided that in formula (I) at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is hydroxy and at least one of the groups W.sup.1, W.sup.2, W.sup.3 and W.sup.4 is amino group NR.sup.2 R.sup.3, Q.sup.1 and Q.sup.

Abstract: Diphosphonic acids of formula (I) are disclosed. These compounds are useful as antitumor agents.

Abstract: Novel pharmacologically active methylenebisphosphonates having formula (I) wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are straight or branched, optionally unsaturated C.sub.1 -C.sub.10 -alkyl, optionally unsaturated C.sub.3 -C.sub.10 -cycloalkyl, aryl, aralkyl, silyl SiR.sub.3 or hydrogen, whereby in formula (I) at least one of the groups R.sup.1, R.sup.2, R.sup.3 or R.sup.4 is hydrogen and at least one of the groups is different from hydrogen, Q.sup.1 is hydrogen, hydroxyl, halogen, amino NH.sub.2, or OR', wherein R' is C.sub.1 -C.sub.4 -lower alkyl or acyl, Q.sup.2 is straight or branched, optionally unsaturated C.sub.1 -C.sub.10 -alkyl, -hydroxyalkyl or -aminoalkyl, whereby the oxygen may, as a substituent, contain one group or the nitrogen as a substituent may contain one or two groups, which are C.sub.1 -C.sub.4 -lower alkyl or acyl, or the two substituents of the nitrogen form together with the nitrogen atom a saturated, partly saturated or an aromatic heterocyclic ring, or Q.sup.

Abstract: N-acyl aminomethylene phosphonates are provided having a group defined by the following general formula: ##STR1## wherein R.sub.1 is hydrogen, an aliphatic radical having 1 to 25 carbon atoms, or an aromatic radical having 6 to 25 carbon atoms; R.sub.2 is hydrogen, an aliphatic radical having 1 to 25 carbon atoms, or an aromatic radical having 6 to 25 carbon atoms; and R.sub.3 is a group remaining after reaction of a hydroxyl group-containing or epoxy group-containing polymer with an acidic hydrogen of a ##STR2## group. Also provided are waterborne coating compositions containing metallic pigments which are normally reactive with water or moisture to release hydrogen gas, stabilized against gassing by incorporation of these N-acyl aminomethylene phosphonates into the waterborne coating compositions.

Abstract: A compound of the formula (I) ##STR1## in which R.sub.1 is e.g. phosphate,R.sub.2 is e.g. phosphate or OH, andR.sub.4 is e.g. ##STR2## are suitable Calcium antagonists and useful e.g. for the treatment of cardio-vascular diseases.

Abstract: Novel pharmaceutically active bisphosphonic acid derivatives of formula (I), in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently are C.sub.1 -C.sub.22 -alkyl, C.sub.2 -C.sub.22 -alkenyl, C.sub.2 -C.sub.22 -alkynyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.3 -C.sub.10 -cycloalkenyl, aryl, aralkyl, silyl and hydrogen, and R.sup.4 is different from hydrogen, Q.sup.1 is hydrogen, fluorine, chlorine, bromine or iodine, and Q.sup.2 is chlorine, bromine or iodine, including the stereoisomers, such as the geometrical isomers and optically active isomers, of the compounds, as well as the pharmaceutically acceptable salts of the compounds.

Abstract: Phosphonic acid squalene synthetase inhibitors are provided which are effective in lowering serum cholesterol and have the formula ##STR1## wherein m is 0 to 3, n is 1 to 5, Y.sup.1 and Y.sup.2 are H or halogen, R.sup.2, R.sup.3 and R.sup.4 are H, metal ion, C.sub.1 to C.sub.8 alkyl, C.sub.3 to C.sub.12 alkenyl, or prodrug ester, and R.sup.1 is a substituted or unsubstituted heteroaryl group or a substituted phenyl group.

Abstract: Provided are novel dialkyl (dialkoxyphosphinyl)methyl phosphates of formula ##STR1## which am useful as anti-inflammatory and anti-arthritic agents. The compounds are synthesized from the reaction of tetraethyl oxiranylidenebisphosphonate and unsubstituted or alkyl-amines. Representative compounds include 2-(benzylamino)-1-(diethoxyphosphinyl)ethyl phosphonic acid diethyl ester, 1-(diethoxyphosphinyl)-2-[2'-(1', 2', 3', 4'-tetrahydro)napthylamino]ethyl phosphonic acid diethyl ester, 2-(3-fluorobenzylamino)-1-(diethoxyphosphinyl)ethyl phosphonic acid diethyl ester, and 5,5 -dimethyl-2-[2-(3-fluorobenzyl)amino-1-[(5,5-dimethyl-1,3,2-dioxaphosphori nan-2-yl)oxy]ethyl]-1,3,2-dioxaphosphorinane P,2-dioxide.

Abstract: Novel bisphosphonates comprise compounds of the formula (I) ##STR1## wherein m and l are independently 1 or 2; R.sub.1 represents hydrogen, a lower alkyl group, or an alkali metal cation; R.sub.2 represents hydrogen, a lower alkyl group or an alkali metal cation; Y represents .dbd.0 or .dbd.N--OH, or --OH and X represents --(CH.sub.2).sub.n --, a branched alkylene group, or a branched or straight alkenylene or alkynylene chain optionally substituted by one or more oxygen or nitrogen atoms, wherein n is an integer from 3 to 24. Further definitions of X are included in the description.

Abstract: A compound having the formula ##STR1## where X is a radical of myo-inositol or a radical of a configuration isomer thereof where at least one R is ##STR2## where Y is (1) oxygen, (2) a straight or branched alkyl with 1-10 carbon atoms, where Z is ##STR3## where A.sup.1 and A.sup.2 are the same or different and are hydrogen or methyl and n is 3-10, or ##STR4## where A.sup.1 and A.sup.2 are hydrogen or methyl and where m is 1-5, where R.sup.1 is hydrogen, straight or branched alkyl, aryl or alkaryl, alkoxy or aryloxy, where R.sup.2 is(1) R.sup.1,(2) hydroxyl, or(3) OZOCOR.sup.1,and where the remaining R is/are hydroxyl.

Abstract: Diarylphosphinous acid aryl esters are made by the disclosed process. These compounds are useful for stabilizing plastics, in particular polymerization plastics, and hence can be incorporated into a plastic molding composition.

Abstract: Phosphonic acid squalene synthetase inhibitors are provided which are effective in lowering serum cholesterol and have the formula ##STR1## wherein m is 0 to 3, n is 1 to 5, Y.sup.1 and Y.sup.2 are H or halogen, R.sup.2, R.sup.3 and R.sup.4 are H, metal ion, C.sub.1 to C.sub.8 alkyl, C.sub.3 to C.sub.12 alkenyl, or prodrug ester, and R.sup.1 is a substituted or unsubstituted heteroaryl group or a substituted phenyl group.

Abstract: New derivatives of cyclohexane in substantially pure form suitable as pharmaceutical, foodstuff or as a stabilizer.

Abstract: New derivatives of cyclohexane in substantially pure form suitable as a pharmaceutical, foodstuff or as a stabilizer.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## wherein m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or 4;Y.sup.1 and Y.sup.2 are H or halogen;R.sup.2, R.sup.3 and R.sup.4 may be the same or different and are independently H, metal ion, C.sub.1 to C.sub.8 alkyl or C.sub.3 to C.sub.12 alkenyl;X is O, S, NH or NCH.sub.2 R.sup.15 wherein R.sup.15 is H or C.sub.1 to C.sub.5 alkyl; andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein;and when m is o, X is other than S; and if m is o and X is O, then n is 1, 2, 3 or 4; including all stereoisomers thereof.

Abstract: Polyether bis-phosphonic acid compounds are disclosed which have the formula (HO).sub.2 OP--R--(OR').sub.n --OR--PO(OH).sub.2 where R is selected from the group consisting of methylene and ethylene, R' is selected from the group consisting of ethylene and ethylene substituted with one or more methyl groups, and n is an integer from 1 to 4, water soluble salts thereof, and esters thereof with alkyl groups having from 1 to 6 carbon atoms.

Abstract: Hydroxyphosphinyl phosphonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.2, R.sup.3 and R.sup.4 are independently H, alkyl, metal ion or a prodrug ester; and R.sup.1 is a lipophilic group which contains at least 6 carbons and is alkyl, alkenyl, alkynyl, mixed alkenylalkynyl, a hetero-containing moiety as defined herein, or a phenylalkyl or phenylalkenyl group including those containing a biphenyl group.

Abstract: Vitamin D derivatives corresponding to the following formula I ##STR1## in which R.sub.1 denotes a substituted alkyl group having 1 to 15 carbon atoms, in particular the side chains of vitamin D.sub.2 (C.sup.20 to C.sup.28) or D.sub.3 (C.sup.20 to C.sup.

Abstract: The invention relates to acyloxymethyl esters of bisphosphonic acids, halo-bisphosphonic acids and hydroxy-bisphosphonic acids which exhibit oral bioavailability and are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.

Abstract: The invention provides 3-deoxy-3-substituted analogs of phosphatidylinositol which are useful to inhibit the growth of mammalian cells, i.e., to treat neoplastic conditions and other proliferative disorders of mammalian cells.

Abstract: A method is provided for preparing a phosphonic acid ester having the structure ##STR1## wherein R.sup.1 is farnesyl or a derivative or analog thereof, and R.sup.2 is lower alkyl, by treating a farnesyl halide R.sup.1 Hal(Hal.dbd.Cl,Br,I) with an alkoxide of the structure ##STR2## wherein M is an alkali metal and R.sup.2c is lower alkyl. The resulting phosphonic acid ester is an intermediate in preparing a squalene synthetase inhibitor which is used for inhibiting cholesterol biosynthesis.

Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## and analogs thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester;R.sup.5 is H, halogen or lower alkyl;Zq is substituted alkenyl, substituted alkynyl, mixed alkenyl-alkynyl or substituted phenylalkyl or, phenylalkenyl or phenylalkynyl, or alkyl, including all stereoisomers thereof.New methods for using such compounds to inhibit cholesterol biosynthesis are also provided.

Abstract: New derivatives of cyclohexane in substantially pure form suitable as a pharmaceutical, foodstuff or as a stabilizer.

Abstract: This invention relates to a methylenediphosphonic acid compound expressed by the formula (1). The compound has a marked effect as an anti-inflammatory agent or, more particularly, against inflammations accompanying disturbances in bone metabolism.

Abstract: Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A.sub.2. Methods of making and using the compounds are also disclosed.

Abstract: Vitamin D derivatives corresponding to the following formula I ##STR1## in which R.sub.1 denotes a substituted alkyl group having 1 to 15 carbon atoms, in particular the side chains of vitamin D.sub.2 (C.sup.20 to C.sup.28) or D.sub.3 (C.sup.20 to C.sup.

Abstract: The N-phosphorylation of basic nitrogenous drug compounds to produce pro-drugs with enhanced water solubility or lipid solubility, or reduced toxicity, is disclosed. Drugs containing amine, amidine, guadinine, isourea, isothiourea an biguanide functions may be converted to such pro-drugs. The pro-drugs are hydrolyzed in the body, regenerating the original drugs with the release of a salt of phsophoric acid.

Abstract: The disclosure is directed to a compound which is a reaction product of at least one phosphonic acid group of an alpha-aminomethylene phosphonic acid containing at least one group corresponding to the formula, ##STR1## with an epoxy group of a compound containing at least one epoxy group. The disclosure is also directed to waterborne coating compositions, organic solvent-borne coating compositions, and powder coating compositions containing the aforesaid reaction product.

Abstract: A method of treating diabetes or complications of diabetes is disclosed. In this method a pharmaceutically effective amount of at least one isomer of inositol triphosphate is administered to a human or an animal in need thereof.

Abstract: A method of reducing the negative effect of cadmium or aluminum ion or free-radicals in body tissues and a method of preventing or alleviating certain diseases and conditions by administering to a human or an animal a pharmaceutical composition comprising an amount of at least one specific isomer of inositol triphosphate sufficient to obtain said prevention or alleviation.

Abstract: A method of reducing or eliminating adverse effects of a pharmaceutical composition or a drug is disclosed. The method comprises administering to an animal or a human an amount of at least one specific isomer of inositol triphosphate sufficient to reduce or eliminate said adverse effects.

Abstract: Preparation of a semi-crystalline catalyst for curing coating compositions wherein an isocyanate-sulfonate or -phosphonate is made by a Michael addition followed by chain extension with an isocyanate.

Abstract: A method of producing organo-phophorus polymers is disclosed. The polymers will exhibit zero shrinkage and even expansion, will be useful in high voltage, high temperature electrical applications and will exhibit mechanical strength and flame retardant properties.

Abstract: Polyfunctional hexasubstituted benzene derivatives wherein at least three of the substituents are saturated carbon chains having from 1 to 21 carbon atoms and functional groups containing hetero functionalities at the ends of the carbon chains and the remainder of the 6 substituents are either saturated carbon chains containing from 1 to 21 carbon atoms or saturated carbon chains containing from 1 to 21 carbon atoms having a functional group including a hetero functional group containing N, O, S, P, or Si at the end of the chains. These derivatives are made by reacting a disubstituted alkyne wherein one or both of the substituents are saturated carbon chains having 1 to 21 carbon atoms to which hetero functional groups are attached with a palladium catalyst and isolating the resulting hexasubstituted benzene derivative.

Abstract: Disclosed herein are phosphoric acid esters of myoinositol, which are represented by the following general formula (I): ##STR1## and their salts, as well as a preparation process thereof. The myoinositol derivatives can each be obtained by causing a phosphorylating agent to act on a myoinositol derivative substituted with catalytic reduction removable substituent groups at the positions other than those desired to be substituted by phosphoric acid residual groups and then catalytically reducing the thus-phosphorylated myoinositol.

Abstract: Substituted aminomethylenebis(phosphonic acid) derivatives represented by the general formula: ##STR1## in which R.sup.1, R.sup.2 R.sup.3 and R.sup.4 may be the same or different, each represents a hydrogen atom or a lower alkyl group; "m" is zero or represents an integer from 1 to 4; and a ring "A" represents a cycloalkenyl group having 5 to 8 carbon atoms, a bicycloheptyl group, a bicycloheptenyl group or a saturated heterocyclic group having 4 to 7 carbon atoms and containing an oxygen atom, a sulfur atom, a sulfinyl group (--SO--) or a sulfonyl group (--SO.sub.2 --),or pharmaceutically acceptable salts thereof.

Abstract: A process for regioselectively preparing phosphorylated cyclitols, in particular phosphorylated inositols such as myo-inositol 1,4,5-tris(phosphate) and myo-inositol 1,3,4,5-tetrakis(phosphate). Novel cyclitols produced by means of this process are also described.

Abstract: This invention provides a 1,1,2-triaryl-1-butene derivative of the formula ##STR1## wherein R.sub.1 and R.sub.2 each represent a lower alkyl group, one of R.sub.3 and R.sub.4 is a lower alkyl group and the other is a group of the formula ##STR2## (in which R.sub.5 is a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom or --OPO(OH).sub.2 group); or a pharmacologically acceptable salt thereof, its preparation and agents containing the derivative for treating mammary cancer and anovulatory infertility.

Abstract: Included are halogenated phosphate-phosphites and their acid halides and acids. The halogenated phosphate-phosphites can be prepared by a process comprising serially contacing(A) a phosphorus trihalide with a triol;(B) a halogenating agent; and(C) an oxirane or an alcohol;under conditions sufficient to prepare the halogenated phosphate-phosphite. Steps (A) and (B) can prepare their acid halides. Use of water in step (C) can prepare their acids. For example, 3-((bis(2-chloroethoxy)phosphino)oxy)(2-bromoethyl-2-methylpropyl, 2-bromoethyl, 2-chloroethyl)phosphorate can be prepared from 2-methyl-2-(hydroxymethyl)-1,3-propanediol; phosphorus trichloride; bromine; and ethylene oxide.Also included is use of the compounds as a hyraulic fluid or flame retardant. For example, polyurethanes can be rendered less flammable with the halogenated phosphate-phosphite flame retardant.

Abstract: The present invention relates to products of the formula ##STR1## where R.sub.1 is H or alkyl, n is an integer from 0 to 10, and R.sub.2 is chosen from amongst H, unsubstituted or substituted alkyl radicals, a ##STR2## group, a substituted or unsubstituted phenyl radical, a ##STR3## group, where X is oxygen or sulfur, or a heterocyclic radical with 5 or 6 members, which may or may not be fused to a benzene ring and R.sub.3 is H or OH.The present invention also relates to a process for the preparation of the products of the formula (I), and to the drugs, having in particular an anti-inflammatory effect, containing a product of formula (I).

Abstract: A process for regioselectively preparing phosphorylated cyclitols, in particular phosphorylated inositols such as myo-inositol 1,4,5-tris(phosphate) and myo-inositol 1,3,4,5-tetrakis(phosphate). Novel cyclitols produced by means of this process are also described.