Salts of phosphonic acids and compositions containing the same

The invention comprises salts of vinylphosphonates having the general formula [CH2=CH-P(O)(OR)-O-]nM in which R is an alkyl group having 1 to 6 carbon atoms or a b -chloroalkyl group having 2 to 6 carbon atoms, M is a metal having a valence of at least 2 and n is the valency of the metal M. Specified metals (M) are magnesium, calcium, strontium, barium, zinc, cadmium, copper, aluminium, iron, cobalt and nickel. The products may be obtained by heating a diester of vinyl phosphonic acid having the general formula CH2=CHP(O)(OR)2 in which R is as defined above with a halide, preferably the chloride of the metal M. Examples are given for the production of: (1) calcium ethyl vinyl phosphonate; (2) calcium n-butyl vinyl phosphonate; (3) calcium isoamyl vinyl phosphonate; (4) cadmium ethyl vinyl phosphonate; (5) cadmium isopropyl vinyl phosphonate; (6) cadmium n-amyl vinyl phosphonate; (7) zinc ethyl vinyl phosphonate; (8) barium ethyl vinyl phosphonate; (9) to (11) barium, cadmium, and zinc methyl ...

PRODUCTION OF 1-PHENYL-VINYL PHOSPHONIC ACID

... 1318809 (1 - Phenylvinyl)phosphonic acid KNAPSACK AG 19 Nov 1971 [8 Dec 1970] 53870/71 Heading C2P (1-Phenylvinyl)phosphonic acid is prepared by heating a suspension of (-hydroxy--methylbenzyl)phosphonic acid or (-chloro--methylbenzyl)phosphonic acid in 1,1,2,2-tetrachloroethane to 110-140‹ C., cooling the reaction mixture, optionally with addition of toluene thereto, and isolating the resulting crystals. Said starting materials are prepared by reacting acetophenone with phosphorus trichloride and glacial acetic acid, and treating the resulting compound with H 2 O or HCl.

Method of preparation of made up antibactérines.

Method of preparation of derived from hydrocarbon acids hydroxy-aminophosphonic.

Process for the preparation of a phosphonic acid and new products obtained by its implementation.

Manufactoring process of antibiotics more particularly the acid (cis-1,2-époxypropyl) phosphonic and of its salts.

PROCEDURE FOR THE PRODUCTION OF NEW PHOSPHONIC ACIDS

AMINOPHOSPHONSÄUREDERIVATE, THEIR ADDITION SALTS AND S1P-REZEPTORMODULATOREN

VERFAHREN ZUR HERSTELLUNG VON NEUEN HYDROXYLAMINO-HYDROCARBYLPHOSPHONSAEUREDERIVATEN

ORGANO PHOSPHORVERBINDUNGEN FOR THE ACTIVATION OF GAMMA/DELTA T CELLS

PROCEDURE FOR THE PRODUCTION OF NEW PHOSPHON SAEUREN

SUBSTITUTED ALPHA AMINO ACIDS WITH PHARMACEUTICAL ACTIVITY.

FARNESYL PROTEINTRANSFERASE INHIBITORS AS ANTI-CANCER MEANS

PROCEDURE FOR the PRODUCTION OF 2-PHENYLETHYLENPHOSPHONS [URE.

PHOSPHONOBERNSTEINSÄUREDERIVATE AND YOUR USE AS DRUGS

Preparation of phosphonic acid derivatives

AMINOPHOSPHONIC ACID DERIVATIVES, ADDITION SALTS THEREOF AND S1P RECEPTOR MODULATORS

Aminophosphonic acid derivatives represented by the general formula (1) (such as 2-amino-5-[4-(3-benzyloxyphenyl-thio)-2-chlorophenyl]-2- methylpentylphosphonic acid mono-esters) exhibit excellent modulatory activity on S1P receptor and are reduced in adverse reaction.

PRODUCTION OF 2-PHENYL-ETHYLENE PHOSPHONIC ACID

THERAPEUTIC BISPHOSPHONATES

The invention provides novel pyrophosphate synthase inhibitors of formula I and formula II as well salts thereof; the invention also provides compositions comprising such inhibitors and methods for their use.

NEW PHOSPHONOSUCCINIC ACID DERIVATIVES, PROCESSES FOR THE PRODUCTION THEREOF AND PHARMACEUTICAL AGENTS CONTAINING THESE COMPOUNDS

Compounds of formula I, (I) in which R1, R2 can be, independently of each other, hydrogen, lower alkyl, cycloalkyl or arylmethyl, R3, R4 can be, independently of each other, hydrogen, lower alkyl or one of the groups -OR6 or -NR7R8 or, together with the atoms to which they are bound, can form a five- to seven-membered carbocyclic ring or a heterocyclic ring containing one to two heteroatoms, R5 denotes lower alkenyl, cycloalkyl, cyclo alkenyl, monocyclic arylalkyl, bicyclic aryl, biaryl or a group of formula a) or b) or, together with R4 and the carbon atom to which it is bound, forms a five- to seven-membered carbocyclic or heterocyclic ring which can be substituted if desired, a) R9-X-alk- b) R6 denotes hydrogen, lower alkyl or arylmethyl, R7, R8 denote, independently of each other, hydrogen or lower alkyl, or together with the nitrogen atom to which they are bound, form a five- to six-membered heterocyclic ring, R9 denotes hydrogen, lower alkyl, lower alkenyl, cycloalkyl, ...

Verfahren zur Herstellung von Vinylphosphonsäuredichlorid

Verfahren zur Herstellung von Vinylphosphonsäure

Verfahren zur Herstellung von Epoxyphosphorverbindungen

Verfahren zur Herstellung von (+)-(cis-1,2-Epoxypropyl)-phosphonsäure und ihrer Derivate

VERFAHREN ZUR HERSTELLUNG VON (CIS-1,2-EPOXYPROPYL)PHOSPHONSAEURE BZW.- PHOSPHONSAEURE SOWIE DEREN SALZE.

Verfahren zum Nachbehandeln von Phosphatschichten

Verfahren zur Herstellung von Vinylphosphonsäure

Phosphonic acid derivs. - plant growth regulators

Compositions containing phosphonic acid derivatives (I) their acid chlorides, anhydrides, hydrolysable mono- and diesters, and salts. R = vinyl-, allyl-, haloethyl-, halopropyl-, methoxyethyl-, carboxymethyl-, phosphonoethyl- pref. cmpds. of general formula (III) X = hal- or -PO(Y)Z Y = Cl- or -OR4 R4 = H-, Na+, Al+, Zn+ or opt. substd. aryl-, arylmethylene-, heterocyclyl-, heterocycly- methylene- or XCH2CH2PO(Z)- Z = Y or opt. substd. opt. unsatd. H/C (e.g. lower alkyl- or C = 18 cycloakyl-) or R4 + Z together may be -O-phi, -OCH2-phi-, -COO-phi-, -CONH phi phi = divalent opt. substd. benzene or heterocyclic ring Plant growth regulants e.g. increase in yield, auxine action, inhibition of growth at extremities and promotion of branching, increase in protein content, falling off of leaves, flowers and fruit, accelerated ripening of fruit, promotion of formation of flowers and fruit, inhibition of flower and seed formation; strengthening of stems; stimulation of seed germination; resistance ...

Verfahren zur Herstellung von cis-Propenylphosphonsäure

Verfahren zum Herstellen von 1-Propinylphosphonsäure

MICRO-BIOLOGICAL PROCEDURE FOR THE PRODUCTION OF NEW OF HYDROXYL-AMINE-SUBSTITUTED OF ALIPHATIC PHOSPHONIC ACIDS.

PROCEDURE FOR THE PRODUCTION OF NEW OF HYDROXYL-AMINE-SUBSTITUTED OF ALIPHATIC PHOSPHONIC ACIDS.

PROCEDURE FOR THE PRODUCTION OF NEW OF HYDROXYL-AMINE-SUBSTITUTED OF ALIPHATIC PHOSPHONIC ACIDS.

PROCEDURE FOR THE PRODUCTION OF NEW OF HYDROXYL-AMINE-SUBSTITUTED OF ALIPHATIC PHOSPHONIC ACIDS.

PROCEDURE FOR THE PRODUCTION OF NEW OF HYDROXYL-AMINE-SUBSTITUTED OF ALIPHATIC PHOSPHONIC ACIDS.

AMINO ACID ISOMERS, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.

ANTI-BACTERIAL COMPOUNDS AND METHODS OF MAKING

QUATERNARY AMINOALKYLENE PHOSPHONIC ACIDS AND METHOD OF PREPARATION

ACIDES 1-PHENYL-1-PHOSPHONIQUES SUBSTITUES ET LEUR UTILISATION

L'INVENTION CONCERNE DES ACIDES 1-PHENYL-VINYL-1-PHOSPHONIQUES COMPORTANT UN SUBSTITUANT R SUR LE RADICAL PHENYLE, R ETANT MIS POUR UN RADICAL ALCOYLE EVENTUELLEMENT SUBSTITUE, EVENTUELLEMENT RAMIFIE, CONTENANT 3 A 20 ATOMES DE CARBONE, AINSI QUE LES SELS, SEMI-ESTERS, SELS DES SEMI-ESTERS ET DIESTERS QUI EN DERIVENT, UN PROCEDE POUR LEUR PREPARATION ET LEUR UTILISATION.

NEW PHOSPHONATES DERIVED FROM CARBOXAMIDES, THEIR MANUFACTORING PROCESS AND PERFORATED THEM PHARMACEUTICAL THE CONTAINER

L'invention concerne des composés de formule générale (I) (CF DESSIN DANS BOPI) dans laquelle, en particulier, R1 représente un résidu farnésyle, V1 représente OH, n, m, R2 , R3 , R4 et Y étant définis dans la description, ainsi que leur procédé de fabrication et leur utilisation pour la fabrication de médicaments destinés au traitement ou à la prévention du cancer, de l'hyperlipidémie de l'hypercholestérolémie, des maladies cardiovasculaires associées, des mycoses et autres infections d'origines fongiques.

INORGANIC MATERIAL, DEVICE, AND ORGANIC ELECTROLUMINESCENT ELEMENT

MAO INHIBITING N-BENZYL-N-PROPARGYL-AMINES USEFUL FOR TREATING OBESITY

The invention provides novel N-benzyl-N-propargyl-amines that are monoamine oxidase inhibitors, but generally exhibit little or no CNS effects.

AMINOALKYLPHOSPHONATES AND RELATED COMPOUNDS AS EDG RECEPTOR AGONISTS

The present invention encompasses compounds of Formula I: Ias well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

PROCESS FOR PREPARING ENANTIOMER-ENRICHED HYDROXYPHOSPHINYL DERIVATIVES

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

VERFAHREN ZUR HERSTELLUNG VON 2-CHLOR-ETHYLPHOSPHONSAEURE

FARNESYL-PROTEINTRANSFERASE INHIBITOREN ALS ANTIKREBSMITTEL

VERFAHREN ZUR HERSTELLUNG UNGESAETTIGTER AMINOSAEUREN

Process for the manufacture of vinyl-phosphonic acid

Vinylphosphonic acid is prepared by reacting vinylphosphonic acid dichloride directly with at least two molar proportions of water in the absence of a solvent at a temperature above 20 DEG C. but not exceeding 300 DEG C. The reaction may be started at a temperature in the range 20-100 DEG C. and the temperature gradually raised to a final temperature of 105-190 DEG C. A polymerisation inhibitor is preferably used above 200 DEG C. An inert gas may be passed through the reaction mixture during reaction. Preferably 2.01 to 2.8 molar proportions of water are used. A mixture of vinylphosphonic acid dichloride with vinylphosphonic acid may be used as starting material. The product may be neutralised with an oxide or hydroxide of an alkali or alkaline earth metal or an aqueous solution of such a base may be used in the reaction. Specification 858,057 is referred to.

PROCESSES FOR INCREASING PLANT RESISTANCE TO DISEASE AND INTERNAL MALFUNCTIONS

... 1334850 Plant growth regulants AMCHEM PRODUCTS Inc 26 Oct 1970 [24 Oct 1969] 50722/70 Addition to 1194433 Heading C1B [Also in Division A5] A process for increasing plant resistance to disease and internal malfunctions comprises applying to the plant or to a focus containing the plant an amount of one or more phosphoric acid derivatives conforming to the general Formula II wherein R is a vinyl, alkyl, haloethyl, halopropyl, methoxyethyl, carboxymethyl or phosphono-ethyl group, and/or the corresponding acid chlorides and/or anhydrides and/or amides and/or hydrolysable mono- and/or diesters and/or salts thereof, sufficient to increase the disease resistance and/or resistance to internal malfunctions of the plant. Preferred phosphoric acid derivatives have the general Formula II shown above in which one of x and y is 0 and the other is 0 or 1; R1 is a vinyl, alkyl, haloethyl, halopropyl, methoxyethyl, carboxymethyl or phosphonoethyl group; R2 is a hydrogen atom or a substituted ...

PROCESS FOR PREPARING SALTS OF ETHYLENE-1,1-DIPHOSPHONIC ACID

... 1,255,123. Salts of ethylene-1,1-diphosphonic acid. MONSANTO CO. 28 May, 1970 [29 May, 1969], No. 25748/70. Addition to 1,204,967. Heading C2P. A salt of ethylene-1;1-diphosphonic acid is prepared by heating at 300‹ to 500‹ C. a salt of 1 -hydroxyethylidene-1,1-diphosphonic acid containing not more than one acidic hydrogen atom per molecule and agitating the particles at least intermittently during heating. The process is preferably carried out in a fluidized bed and in the substantial absence of oxygen. Salts of 1-hydroxyethylidene- 1,1 -diphosphonic acid are prepared by reacting the acid with an alkaline material using at least 3 equivalents of the alkaline material per mole of acid.

PHOSPHONIC ACID, PROCEDURE FOR THE PRODUCTION AND USE AS DRUG ACTIVE SUBSTANCE.

Procedure for the production of a new diastereomeren derivative of (cis-1,2-Epoxypropyl) - phosphonic acid

Procedure for the production of cis Propenylphosphonsäure

VERFAHREN ZUR HERSTELLUNG VON NEUEN PHOSPHONDERIVATEN

Procedure for the production of new Epoxyäthylphosphonsäuren and their salts

NEW ARYL FRUCTOSE-1,6-BISPHOSPHATASE INHIBITORS

INSATIATED AMINO DICARBOXYLIC ACID DERIVATIVES.

NEW VINYLBENZOLDERIVATE

PROCEDURE FOR THE PRODUCTION OF NEW HYDROXYLAMINO HYDROCARBYLPHOSPHONSAEUREDERIVATEN

PRODUCTION OF PHOSPHONIC ACID DERIVATIVES

Cyclohexyl prostaglandin analogs as EP4-receptor agonists

HYDROXYAMINOHYDROCARBONPHOSPHONIC ACID DERIVATIVES

CHEMICAL PROCESSES AND PRODUCTS

ENPP1 inhibitors and their use for the treatment of cancer

Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor is cell impermeable. Also provided are compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of a ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject either before or after administering an ENPP1 inhibitor. The radiation therapy can be administered at a dosage and/or frequency effective to reduce radiation damage to the subject. In certain cases, the method is performed in combination with a chemotherapeutic agent, or a checkpoint inhibitor, or both.

Novel CYP-eicosanoid derivatives

The present invention relates to compounds according to general formula (I) which are analogues of epoxymetabolites produced by cytochrome P450 (CYP) enzymes from omega-3 (n-3) polyunsaturated fatty acids (PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for the treatment or prevention of conditions and diseases associated with inflammation, proliferation, hypertension, coagulation, immune function, pathologic angiogenesis, heart failure and cardiac arrhythmias.

QUATERNARY AMINOALKYLENE PHOSPHONIC ACIDS AND METHOD OF PREPARATION

PROCESS FOR THE MANUFACTURE OF VINYL PHOSPHONIC ACID DERIVATIVES

... of the disclosure: Process for the manufacture of viny1 phosphonic acid derivatives of the formula with R1 being hydrogen or alkyl with 1 to 4, prererably 1 to 2, carbon atoms and n being 1 or 2, which comprises heating to 150-270.degree.C, preferably 170 to 230.degree.C, 2-acetoxyethane phosphonic acid dialkyl esters of the formula , with R2 being alkyl with 1 to 4, preferably 1 to 2, carbon atoms, in the presence of acidic or basic catalysts.

METHOD OF SEPARATING VINYLPHOSPHONIC ACID FROM CRUDE MIXTURES

.ALPHA.-PHOSPHONOSULFONAE SQUALENE SYNTHETASE INHIBITORS AND METHD

... .alpha.-PHOSPHONOSULFONATE SQUALENE SYNTHETASE INHIBITORS AND METHOD .alpha.-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These comounds have the formula wherein R2 is OR5 or R5a; R3 and R5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.

Farnesy:Protein Transferase Inhibitors as Anticancer Agents

CERTAIN PHOSPHINYL DERIVATIVES USEFUL AS NAALADASE INHIBITORS

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.

HYDROXY-PHOSPHINYL DERIVATIVES USEFUL AS NAALADASE INHIBITORS

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.

METHOD FOR PRODUCING VINYL PHOSPHONIC ACID COMPOUNDS

The invention relates to a method for producing vinyl phosphonic acid compounds of general formula (I) wherein R1 and R2 are independently H, C1-16-aryl, C7-12-alkaryl or C7-12-aralkyl radicals, wherein the organic radicals can be substituted by one or several halogen atoms, hydroxyl, acyl or acetoxy groups. Production occurs by reacting phosphoric acid compounds of general formula (II) with acetylene in the presence of a Pd(II) complex and/or a Pd(0) complex or corresponding Pt complexes as a catalyst.

INHIBITORS OF ENPP1 AND METHODS FOR MODULATION OF IMMUNE RESPONSE

CHEMICAL PROCESS (PROCESS FOR PREPARING PROGENYLPHOSPHONIC ACID)

NOUVEAUX AMINOACIDES ISOMERES, LEUR PREPARATION ET LEUR APPLICATION MEDICALE

L'INVENTION CONCERNE LA CHIMIE PHARMACEUTIQUE. ELLE A POUR OBJET LES (-)-D- ISOMERES DE COMPOSES DE FORMULE GENERALE: (CF DESSIN DANS BOPI) OU R REPRESENTE UN RADICAL ALIPHATIQUE EVENTUELLEMENT SUBSTITUE (DE PREFERENCE CH),ET X REPRESENTE UN RADICAL ACIDE, SPECIALEMENT UN RADICAL D'ACIDE PHOSPHONIQUE, D'ACIDE SULFONIQUE, D'ACIDE BORONIQUE OU DE TETRAZOLE,DE MEME QUE LEURS SELS. CES COMPOSES SONT PREFERES POUR LE TRAITEMENT DE CERTAINES AFFECTIONS DU SYSTEME NERVEUX CENTRAL.

EPOXYETHYLPHOSPHONIC ACID DERIVATIVES

PROCESSES FOR PREPARING OLEFINIC ORGANO?PHOSPHORUS COMPOUNDS

PROCESS FOR PREPARING UNSATURATED AMINO ACIDS

Unsatd. amino acids of formula (I) are prepd. by reacting a cpd. of formula (II) with a cpd. of formula (III), and then removing a protective gp. from the product. In the formulas, R1 is OH; R2 is H, alkyl or OH; R3 is H, alkyl; R5 is H or alkyl; R6 is carboxy; R7 is amino; A is alpha, amega-alkylene; B is methylene; Z1 is OH; Z2 is H or OH; Z3 is carboxy; Z4 is amino; R is etherfied gp.; X is reactive esterfied hydroxy. (I) are useful as selective antagonists of NMDA- receptors. Copyright 1997 KIPO ...

AMINOPHOSPHONIC ACID DERIVATIVES, ADDITION SALTS THEREOF AND S1P RECEPTOR MODULATORS

PROCESSO PARA A PREPARACAO DE UM COMPOSTO E DE PREPARACAO DE UM DERIVADO INTRAMOLECULAR,COMPOSICAO E PROCESSO PARA INIBIR A CORROSAO

THERAPEUTIC BISPHOSPHONATES

The invention provides novel pyrophosphate synthase inhibitors of formula I and formula II as well salts thereof; the invention also provides compositions comprising such inhibitors and methods for their use.

FARNESYL:PROTEIN TRANSFERASE INHIBITORS AS ANTICANCER AGENTS

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

ORGANO-PHOSPHOROUS COMPOUNDS FOR ACTIVATING GAMMA/DELTA T CELLS

The invention relates to phosphororganic compounds of general formula (I), to the production thereof, and to their use for activating gamma/delta T cells, for screening inhibitors of the GcpE and of the LytB enzyme as well as for the prophylaxis and treatment of diseases in humans and animals.

METHOD OF SEPARATING VINYLPHOSPHONIC ACID FROM PRODUCT MIXTURES

The invention concerns a method of separating vinylphosphonic acid from product mixtures by extraction with alcohols and/or ketones with at least 5 carbon atoms. The method proposed enables high yields of high-purity vinylphosphonic acid to be obtained from extremely impure product mixtures.

HYDROXY-PHOSPHINYL DERIVATIVES USEFUL AS NAALADASE INHIBITORS

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.

FARNESYL-PROTEINTRANSFERASE INHIBITOREN ALS ANTIKREBSMITTEL

NEUE ARYL FRUCTOSE-1,6-BISPHOSPHATASE INHIBITOREN

SUBSTITUTED AMMONIUM SALTS OF 2-CHLOROETHANEPHOSPHONIC ACID USEFUL FOR INFLUENCING PLANT GROWTH OR BEHAVIOUR

1499189 Quaternary ammonium 2-chloroethylphosphonates BASF AG 6 May 1975 [10 May 1974] 18914/75 Heading C2P [Also in Division C1] The invention comprises quaternary ammonium salts of: (where R is H, C 1-12 alkyl or C 1-12 haloalkyl), the ammonium ion(s) being of formula (where R<SP>1</SP> is a C 2-5 alkyl or alkenyl group, optionally substituted by halo or epoxy, and R<SP>2</SP> is CH 3 or NH 2 , or NR<SP>1</SP>R<SP>2</SP> compositely represents a six-membered hetero ring optionally including an oxygen atom or second nitrogen atom. In the dibasic salts, the two ammonium ions may be the same or different. The above salts are prepared from I (or a metal or NH 4 salt thereof) by reaction with an appropriate quaternary ammonium halide and optionally an acid-binding agent. The inventive salts are used as plant growth regulants (see Division C1).

PREPARATION OF CIS-PROPENYLPHOSPHONIC ACID AND DERIVATIVES THEREOF

... 1,249,073. Preparing cis-propenyl phosphonic acids and derivatives thereof. MERCK & CO. Inc. 12 May, 1969 [15 May, 1968], No. 23986/69. Heading C2C. A cis-olefinic compound of the formula CH 3 CH=CHP(O)(OR) 2 wherein R is H, a univalent substituted or unsubstituted hydrocarbon radical or an equivalent of a cation which may be a metal, NH 4 or amine cation, the two R's being the same or different, is obtained by treating a compound of the formula wherein X is halogen, Y is halogen or OH or an acyloxy, sulphonyloxy or nitrosyl group and R is as defined above with an appropriate reagent selected from a reducing metal (e.g. zinc), a reducing metal salt (e.g. chromous chloride or stannous chloride), sodium sulphite, sodium iodide, diphenyl telluride, a triaryl phosphine, a trialkyl phosphine and a trialkyl phosphite. The halohydrin compound in which Y is OH may be obtained by reacting the (+) isomer of the cis-epoxide of the formula with a hydrogen halide which is preferably bubbled into a solution ...

PRODUCTION OF CIS-1,2-PROPENYLPHOSPHONIC ACID

... 1,237,232. cis-1,2-propenyl phosphonic acid and intermediates therefor. MERCK & CO. Inc. 24 Oct., 1968 [15 May, 1968], No. 50628/68. Heading C2C. cis-1,2-Propenylphosphonic acid (I) is obtained by reacting phosphorus trichloride with at least two equivalents of a C 1 -C 5 alkyl, or C 2 -C 5 alkenyl alcohol or an alkalkyl alcohol, or a phenol, or with at least one equivalent of a dihydric phenol, e.g. catechol or of a C 2 -C 5 alkylene glycol in an inert organic solvent, reacting the resulting diorgano phosphorochloridite (II) with propargyl alcohol to form a 2- propynyl di-organo-phosphite (III), rearranging the latter to form the corresponding allenyl phosphonic acid diester (IV), hydrogenating the latter to form the cis-1,2-propenyl phosphonic acid diester (V) and cleaving the latter to form the free cis-1,2-propenyl phosphonic acid (I), the process being generally carried out without isolating the intermediate compounds. The 2-propynyl diorganophosphite (III) gradually rearranges on ...

PHOSPHONOCARBONSÄURE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF DEGENERATIVE JOINT ILLNESSES

PRODUCTION OF 1-PHENYLVINYL-1-PHOSPHONSÄURE

(((2-AMINO-3,4-DIOXO-1-CYCLOBUTEN-1 YL) AMINO>ALKYL>SÄUREDERIVATE.

Procedure for the production of new (±) - (cis-1,2-Epoxypropyl) - phosphonic acid connections

Method for preparing conjugated diene phosphonate compounds

It is provided a method for preparing conjugated diene phosphonate compounds with high reactivity, which can be used to prepare a variety of phosphonate-bearing conjugated dienes. Some of those dienes will become reactive monomers to make polymers and co-polymers. The said method comprises the step of reacting α, β- or β, γ-unsaturated ketones or aldehydes with phosphorus acid or its derivates optionally in a mixture of acetic anhydride and/or acetic acid, to obtain a conjugated diene phosphonate compound having the formula (III)

N-substituted acrylamides, preparation method and use thereof

This invention relates to new monomers prepared from phosphorus-containing diene monomers and (meth)acrylonitrile via Ritter reactions, and the preparation method thereof. The polymer of these monomers can be utilized in various applications such as water treatment, rheology modifier, surface modification, etc. The monomers have the following structure (II), Wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 represent, independently, hydrogen, alkyl, aryl, alkaryl, aralkyl, cycloalkyl, heterocycloalkyl, or alkenyl groups; R 6 and R 7 represents R 9 O, and R 10 respectively wherein R 9 and R 10 represents hydrogen, alkyl, aryl, alkaryl, aralkyl, cycloalkyl, alkenyl groups, or metals selected from the group consisting of Na, Li, Ca; Rs represents H, or CH 3 .

Method of coating an inorganic substrate with a stable organic layer

A method for coating a metallic or inorganic substrate is described, such as metal or glass supports, with an organic layer comprising conjugated diene phosphinate or phosphonate compounds.

NOVEL CYP-EICOSANOID DERIVATIVES

The present invention relates to compounds according to general formula (I) which are analogues of epoxymetabolites produced by cytochrome P450 (CYP) enzymes from omega-3 (n-3) polyunsaturated fatty acids (PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for C the treatment or prevention of conditions and diseases associated with inflammation, proliferation, hypertension, coagulation, immune function, pathologic angiogenesis, heart failure and cardiac arrhythmias. 2. The compound according to , wherein E is a group represented by the general formula (III); and P , and I are defined as in .4. The compound according to or , wherein P represents a group —(CH)X , —(CH)X , —(CH)X , or —(CH)X; wherein X is defined as in .7. The compound according to , wherein E is a group represented by the general formula (IV); one of Rand Rrepresents a hydrogen atom and the other represents a fluorine atom , hydroxy , —NH , C-Calkyl , C-Calkoxy , —C(═O)-aryl , —C(═O)C-Calkyl , or —SO(C-Calkyl); or —SOaryl; wherein any of the foregoing C-Calkyl , C-Calkoxy , or aryl are optionally substituted with one , two or three substituents independently selected from the group consisting of —NH , —NH(C-C)alkyl , —N(C-C)dialkyl , C-Calkylcarbonyloxy- , C-Calkoxycarbonyloxy- , C-Calkylcarbonylthio- , C-Calkylaminocarbonyl- , di(C-C)alkylaminocarbonyl- , fluorine or chlorine atom , and hydroxy; or Rand Rare taken together to form a 5-membered or 6-membered ring , which ring is optionally substituted with one , two or three substituents independently selected from the group consisting of —NH , —NH(C-C)alkyl , —N(C-C)dialkyl , C-Calkylcarbonyloxy- , C-Calkoxycarbonyloxy- , C-Calkylcarbonylthio- , C-Calkylaminocarbonyl- , di(C-C)alkylaminocarbonyl- , fluorine or chlorine atom , and hydroxy; and P and I are defined as in .8. The compound according to , wherein E is a group represented by the general ...

Crosslinking Monomers With at Least One Sulfur Atom

The invention relates to a cross-linking monomer with at least one sulfur atom, representable by a structure of formula (I) 2. The monomer according to claim 1 , wherein group Vhas at least one aromatic and/or heteroaromatic residue.3. The monomer according to claim 2 , wherein the aromatic and/or heteroaromatic residue of group Vis a monocyclic residue.4. The monomer according to claim 1 , wherein Lis a linear claim 1 , branched claim 1 , or cyclic alkylene group with 2 to 10 carbon atoms claim 1 , in which one or more non-adjacent CHgroups is/are not substituted or is/are substituted with —RC═CR— claim 1 , —C≡C— claim 1 , —(C═O)— claim 1 , —(C═S)— claim 1 , —(C═NR)— claim 1 , —C(═O)O— claim 1 , —C(═O)NR— claim 1 , —NR— claim 1 , P(═O)(R) claim 1 , —[CH(CH)P(═O)(OR)]— claim 1 , —O— claim 1 , —S— claim 1 , —(SO)— claim 1 , or (—SO)— claim 1 , wherein x is an integer in a range of 0 to 6.5. The monomer according to claim 1 , wherein the hydrolyzable group Ris an alkyl residue with 1 to 4 claim 1 , carbon atoms.14. A curable composition for use in dental medicine claim 1 , comprising at least one monomer according to .16. (canceled)17. The monomer according to claim 2 , wherein group Vhas at least one aromatic residue.18. The monomer according to claim 3 , wherein the aromatic and/or heteroaromatic residue of group Vis a phenyl or phenylene residue.19. The monomer according to claim 4 , x is an integer in a range of 1 to 5.20. The monomer according to claim 5 , wherein the hydrolyzable group Ris an alkyl residue with 2 claim 5 , carbon atoms.21. The monomer according to claim 6 , wherein{'sup': '2', 'Vis a saturated or unsaturated, aliphatic and/or heteroaliphatic group with 3 to 6 carbon atoms; an aromatic or heteroaromatic group with 4 to 12 carbon atoms or a group with 6 to 14 carbon atoms, which comprises at least one hydrocarbon residue with 3 to 5 carbon atoms.'}22. The monomer according to claim 8 , wherein claim 8 , each time it occurs claim 8 , Ris H or a ...

Hydrocarbyl Tin Complex of Alkynyl Phosphonic Acid with Antitumor Activity and Application Thereof

Hydrocarbyl tin complexs of alkynyl phosphonic acid with antitumor activity and their application are provided. Tests are conducted to evaluate activity, showing that the provided complexs have much stronger activity than cisplatin. The provided hydrocarbyl tin complexs can be potential candidate as a clinical antitumor drug.

B-Ketophosphonic Acids And Dental Materials Based Thereon

β-Ketophosphonic acid according to general formula I: 2. β-Ketophosphonic acid according to claim 1 , wherein{'sub': 2', '15, 'A=an aliphatic C-Cradical which can be interrupted by —O—,'}n=1 or 2,m=1 or 2,{'sub': 1', '4, 'X=a C-C-alkylene radical or is absent, and'}{'sub': 2', '2', '2', '3', '1', '7, 'sup': 2', '3', '4', '2', '3', '4, 'PG=vinyl, allyl, CH═CR—CO—Y— or RO—CO—C(═CH)—CH—Y—, wherein Y is O or NRor is absent, Ris H or CHand Rand Rindependently of each other are each H or C-C-alkyl.'}3. β-Ketophosphonic acid according to claim 2 , wherein{'sub': 1', '10, 'A=a linear aliphatic C-Cradical which can be interrupted by 1 or 2 —O—,'}n=1,m=1 or 2,{'sub': 1', '2, 'X=a C-Cradical or is absent,'}{'sub': 2', '2', '2', '3', '3', '2', '5', '3', '2', '5, 'sup': 2', '4', '3', '2', '3', '4, 'PG=CH═CR—CO—Y—, wherein Y is O or NR, or RO—CO—C(═CH)—CH—Y—, wherein Y is O, and wherein Ris H or CH, Ris CHor CHand Ris H, CHor CH.'}4. Dental material claim 1 , characterized in that it comprises at least one β-ketophosphonic acid according to .5. Dental material according to claim 4 , which additionally comprises at least one initiator for free radical polymerization.6. Dental material according to claim 4 , which additionally comprises a further monomer which can undergo free radical polymerization.7. Dental material according to claim 6 , which comprises as further monomer one or more mono- and/or polyfunctional (meth)acrylic acid derivatives and/or (meth)acrylamide derivatives.8. Dental material according to claim 4 , which additionally comprises at least one solvent.9. Dental material according to claim 8 , which comprises as solvent water or a mixture of water and a polar organic solvent.10. Dental material according to claim 4 , which comprisesa) 0.1 to 50 wt.-% of β-ketophosphonic acid of general formula I,b) 0.01 to 10 wt.-% of initiator,c) 0 to 80 wt.-% of further monomer,d) 0 to 80 wt.-% of filler,e) 0 to 70 wt.-% of solvent.11. Dental material according to for use as an ...

Novel alkenyl and beta-substituted phrosphonates as antimicrobial agents

The present disclosure relates to novel compounds, pharmaceutical compositions, and methods for treating or preventing microbial infection caused by parasites or bacteria, such as Plasmodium falciparum or related Plasmodium parasite species and Mycobacterium tuberculosis or related Mycobacterium bacteria species. The compounds are α,β-unsaturated analogs of fosmidomycin and can inhibit deoxyxylulose phosphate reductoisomerase (Dxr) in many microbes, such as P. falciparum.

ACIDIC HYBRID MONOMERS AND DENTAL MATERIALS BASED THEREON

Acidic monomer according to Formula I: 2. The acidic monomer of claim 1 , whereinPG=vinyl, allyl, CH2=CR3-CO—Y— or R4O—CO—C(═CH2)-CH2-Y—.3. The acidic monomer of claim 1 , wherein the variables of Formula I have the following meanings:{'sub': 1', '10, 'sup': '1', 'A=linear or branched C-Caliphatic group, which can be interrupted by one or more —O—, —S—, —CO—O—, —O—CO—NH—, —HN—CO—NH— or —CO—NR—,'}{'sup': '1', 'R=H,'}{'sub': '2', 'X=—CH— or absent,'}{'sub': '2', 'sup': '3', 'PG=CH═CR—CO—Y—,'}{'sup': '5', 'Y=O or NR,'}{'sup': '3', 'sub': '3', 'R=H or CH,'}{'sup': '5', 'sub': 1', '4, 'R=H or a C-Calkyl group'}n=1 or 2,m=1,p=1, andq=1.4. The acidic monomer of claim 3 , wherein the variables of Formula I have the following meanings:{'sub': 3', '10, 'sup': '1', 'A=linear or branched C-Caliphatic group, which can be interrupted by one —O—, —S—, —CO—O—, —O—CO—NH—, —HN—CO—NH— or —CO—NR—,'}{'sup': '1', 'R=H,'}X=absent,{'sub': '2', 'sup': '3', 'PG=CH═CR—CO—Y—,'}{'sup': '5', 'Y=O or NR,'}{'sup': '3', 'sub': '3', 'R=H or CH,'}{'sup': '5', 'sub': 1', '3, 'R=H or a C-Calkyl group'}n=1 or 2,m=1,p=1,q=1.5. The acidic monomer of claim 3 , wherein the dihydrogen phosphate group —O—PO(OH)and the phosphonic acid group —PO(OH)are bound to the same carbon atom.6. Dental material which comprises at least one acidic monomer according to .7. The dental material of claim 6 , which comprises 0.1 to 50 wt.-% of the acidic monomer according to Formula I claim 6 , based on the total weight of the dental material.8. The dental material of claim 6 , which comprises 1 and 20 wt.-% of the acidic monomer according to Formula I claim 6 , based on the total weight of the dental material.9. The dental material of which comprises at least one additional radically polymerizable monomer and also at least one initiator for the radical polymerization.10. The dental material of claim 9 , which comprises at least one multifunctional (meth)acrylate or a mixtures of mono- and multifunctional (meth)acrylates.11. ...

PROCESS FOR THE PREPARATION OF PHOSPHONIC ACID MONOMERS

A simple, commercially viable process for the preparation of phosphonic acid monomers containing essentially no diester or inorganic phosphorous acid compounds is disclosed. 2. The process of wherein the contacting is conducted in the presence of a polymerization inhibitor.3. The process of wherein the contacting is conducted in the temperature range of 70 to 170° C.4. The process of wherein the contacting is conducted in the temperature range of 130 to 140° C.5. The process of wherein the contacting is conducted in the pressure range of 0 to 760 mmHg.6. The process of wherein the contacting is conducted in the pressure range of 450 to 550 mmHg.7. The process of wherein from 0.5 to 10 moles of MAA is employed per mole of phosphorus reactant.8. The process of wherein the MAA is employed in the range of 1 to 3 moles per mole of phosphorus reactant.9. The process of wherein the MAA is employed in the range of 1.5 to 2 moles per mole of phosphorus reactant.10. The process of wherein the inhibitor is selected from the group consisting of phenothiazine claim 1 , 4-hydroxy-TEMPO claim 1 , methoxy hydroquinone claim 1 , and hydroquinone.11. The process of wherein the product is substantially free of inorganic phosphorous acids.12. The process of wherein the product is substantially free of diester cross-linkers.13. The process of wherein the contacting is conducted in the substantial absence of added solvent. This application claims priority from provisional application Ser. No. 61/733,438, filed Dec. 5, 2012, which is incorporated herein by reference in its entirety.The invention relates to a process for preparing phosphonic acid monomers.Polymers containing phosphorus acid groups are useful in many applications including coatings and adhesives. The phosphorus acid groups provide improved adhesion of the polymer to metal substrates, form crosslinks in the presence of divalent metal ions, and promote adsorption of the polymer to pigment particles, such as titanium dioxide, ...

Phosphonsäuren enthaltendes Dentalmaterial

Gegenstand der Erfindung sind Dentalmaterialien, die hydrolysestabile Phosphonsäuren mit ethylenisch ungesättigten Doppelbindungen enthalten und die sich besonders als Haftvermittler eignen.

n-substituted acrylamides, method for its preparation and use.

Compounds of the agonists and antagonists of the receptor of sphingosine-1-phosphate

1. Соединение формулы I ! ! где D представляет H, N(R5)2 или OR6; ! X представляет CH, C(CH3) или N; ! Y представляет CH2, O, S или NR3; где R3 представляет водород или линейный или разветвленный (С1-С10) алкил; ! A представляет H, гидрокси, -CH2OH, -CH(OH)CH3, -C(O)-OCH3, -C(OH)(CH3)2, -O(CH2)tCOOH, -C(O)-NR6, необязательно замещенный -(CH2)n-P(=O)(OR7)(OR7), необязательно замещенный -(CH2)n-O-P(=O)(OR7)(OR7), необязательно замещенный -(CH2)n-P(=O)(OR7)(R7), -CH=CH-P(=O)(OR7)(OR7), C(O)-NHCH3, CN, COOR6 или -R4-COOH, где R4 представляет линейный или разветвленный(C1-C20) алкилен, линейный или разветвленный (C1-C20) алкенилен, линейный или разветвленный(C1-C20) алкинилен, (C3-C20)циклоалкил, или необязательно замещенный азетидинил; ! R1 и R2 независимо выбраны из группы, состоящей из водорода, CF3, галогена, (C1-C20) алкила, (C1-C20) алкокси, замещенного (C3-C20) циклоалкилом алкила, замещенного (C3-C20) циклоалкилом алкокси, (C2-C20) алкенила, замещенного арилом (C2-C20) алкенила, (C2-C20) алкинила, замещенного арилом (C2-C20) алкинила, арила, замещенного арилом (C1-C20)алкила, замещенного гетероарилом (C2-C20)алкила, замещенного арилом алкокси, замещенного гетероарилом алкокси, замещенного алкилом арила, арилалкила, замещенного арилом арилалкила, замещенного арилалкилом арилалкила, CN и -O-индолизинила; ! где такие R1 и R2 группы могут быть необязательно замещенными одним или несколькими заместителями, независимо выбранными из (C1-C20) алкила, CF3, галогена, гидрокси, (C1-C20) алкокси, OCF3 и CN; ! где один или несколько атомов углерода в группах R1 или R2 могут быть независимо замещены непероксидным кислородом, серой или NR8; ! где R8 представляет водород или (C1-C20) алкилгруппу; ! где один из R1 и R2 является иным, чем водород и где группы алкил, алкенил и алкинил в R1 и R2 являются необязательно замещенным (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2009 128 062 (13) A (51) МПК A01N 43/50 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ...

Composition for regulating plant growth

CHEMICAL COMPOUNDS, PHARMACEUTICAL CMPOSITION, CONTAINING THEM, THEIR APPLICATION (VERSIONS) AND METHOD OF BINDING ERα AND ERβ -ESTROGEN RECEPTORS

FIELD: chemistry. SUBSTANCE: invention relates to novel compounds of formula (I), including its pharmaceutically acceptable salts, solvates, ethers and amides, possessing ability to bind ERα- and ERβ-estrogen receptors, to pharmaceutical composition based on them, to versions of applying claimed compounds in medication preparation and to method of binding ERα- and ERβ-estrogen receptors. (I), where R 1 represents H, OH or C 1-12 alkoxy, or halogen; R 2 represents H, OH or halogen; R 3 represents C 1-12 alkyl, halogeno-C 1-12 alkyl, C 3-10 cycloalkyl, C 1-12 alkoxy or C 1-12 alkoxyC 1-12 alkyl; R 4 represents H or C 1-12 alkoxy; R 5 represents H, halogen or halogeno-C 1-12 alkyl; R 6 represents -(Y) z -R 7 ; R 8 represents phenyl or 5- or 6-member heteroaryl, containing N, O or S as heteroatom, where said phenyl and heteroaryl are possibly substituted with OH, halogeno, halogenoC 1-12 alkyl or C 1-12 alkoxy. Values R 7 , Y and z are presented in invention formula. EFFECT: novel compounds possess useful biological properties. 19 cl, 7 dwg, 1 tbl, 70 ex

7-substituted quinone metides as inhibitors for unsaturated monomers

유효량의 7-아릴 퀴논 메티드 화합물을 혼입하는 것에 의해 단량체 제조공정 동안 즉시 중합가능한 불포화 단량체의 조기 중합을 감소시키기 위한 조성물 및 방법이 제공된다. By incorporating an effective amount of a 7-aryl quinone methide compound, compositions and methods are provided for reducing premature polymerization of unsaturated polymerizable monomers during the monomer preparation process.

The method of obtaining 2-phenylethylene phosphonic acid

(((2-amino-3,4-dioxo-1-cyclo-buten-1-yl)amino)alkyl)-acid derivatives

일반식(I)의 화합물 또는 이의 약제학적으로 허용되는 염은 신경보호제로 유용하다. Compounds of formula (I) or pharmaceutically acceptable salts thereof are useful as neuroprotective agents. [일반식 I] [Formula I] 상기식에서, R 1 은 수소, 알킬 또는 페닐알킬이고; R 2 은 수소, 알킬, 알케닐 또는 페닐알킬이거나; R 1 및 R 2 는 함께 -CH 2 CH 2 -, -CH 2 C(R 6 )(R 7 )CH 2 -또는 -CH 2 C(R 6 ) (R 9 )-C(R 10 )(R 11 )CH 2 -(여기서 R 6 , R 8 및 R 10 은 독립적으로 수소, 탄소수 1 내지 6의 알킬 또는 하이드륵실 R 7 , R 9 및 R 11 은 독립적으로 수소 또는 탄소수 1 내지 6의 알킬이다)이고; A는 알킬켄 또는 알켈닐렌이며; X는 CO2R3(여기서, R3는 수소 또는 알킬이다), P(O)(OR 4 )(OR 5 )(여기서, R 4 및 R 5 는 독립적으로 수소 또는 알킬이다), 3,5-디옥소-1,2,4-옥사디아졸리딘-2-일 또는 5-테트라졸릴이다. Wherein R 1 is hydrogen, alkyl or phenylalkyl; R 2 is hydrogen, alkyl, alkenyl or phenylalkyl; R 1 and R 2 together are —CH 2 CH 2 —, —CH 2 C (R 6 ) (R 7 ) CH 2 — or —CH 2 C (R 6 ) (R 9 ) —C (R 10 ) (R 11) CH 2 - (wherein R 6, R 8 and R 10 are independently hydrogen, C 1 -C 6 alkyl or hydroxy reuksil of R 7, R 9 and R 11 are independently hydrogen or alkyl having 1 to 6 carbon atoms) ego; A is alkylken or alkenylene; X is CO 2 R 3, where R 3 is hydrogen or alkyl, P (O) (OR 4 ) (OR 5 ), where R 4 and R 5 are independently hydrogen or alkyl, 3,5-dioxo- 1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl.

New derivatives of CYP eicosanoids

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2016 133 336 A (51) МПК C07C 309/11 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ 2016133336, 21.01.2015 (21)(22) Заявка: Приоритет(ы): (30) Конвенционный приоритет: 22.01.2014 US 61/930,031 (86) Заявка PCT: EP 2015/000105 (21.01.2015) (87) Публикация заявки PCT: WO 2015/110262 (30.07.2015) R U (54) Новые производные CYP-эйкозаноидов (57) Формула изобретения 1. Соединение общей формулы (I): или его фармацевтически приемлемая соль, где Р представляет собой группу, представленную общей формулой (II): где В представляет собой связь углерод-углерод; -О- или -S-; n равен 0 или представляет собой целое число от 3 до 8; и k равен 0 или 1; при условии, что, если n равен 0, k равен 1; X представляет собой группу: ; ; ; ; ; ; ; ; Стр.: 1 A 2 0 1 6 1 3 3 3 3 6 A Адрес для переписки: 190000, г. Санкт-Петербург, БОКС-1125 2 0 1 6 1 3 3 3 3 6 (72) Автор(ы): ШУНК Вольф-Хаген (DE), МЮЛЛЕР Доминик (DE), ФИШЕР Роберт (DE), ВАЛЛУКАТ Герд (DE), КОНКЕЛЬ Анна (DE), ФАЛЬК Джон Рассел (US) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 22.08.2016 R U (43) Дата публикации заявки: 28.02.2018 Бюл. № 07 (71) Заявитель(и): МАКС-ДЕЛБРЮК-ЦЕНТРУМ ФЮР МОЛЕКУЛЯРЕ МЕДИЦИН (DE), БОРД ОФ РЕДЖЕНТС, ЗЕ ЮНИВЕРСИТИ ОФ ТЕХАС СИСТЕМ (US) ; ; ; ; ; ; ; ; ; ; ; или . R11 представляет собой C1-С6алкильную группу, которая необязательно содержит в качестве заместителей один или более атом (-ов) фтора или хлора; или С3-С6циклоалкильную группу, которая необязательно содержит в качестве заместителей один или более атом (-ов) фтора или хлора или гидроксильную (-ые) группу (группы); R2 представляет собой -NHR3; -NR20R21; -OR22; -(OCH2-CH2)iR23; моно- или дисахарид, или их производное, которые присоединены к -С(О) посредством сложноэфирной связи через 1-O-, 3-O- или 6-O-положение сахарида; или выбран из группы, состоящей из: A 2 0 1 6 1 3 3 3 3 6 A -NH(C1-С6алкил), -NH(С3-С6циклоалкил), -NH(арил) или -O(С1-С6алкилдиил)O( ...

NEW ARILY FRUCTOSO-1, 6-BISPHOSPHATASE INHIBITORS

Production of ice 1 propenylphosphonic acid

ß-ketophosphonic acids and all dental materials based thereon

Acidic hybrid monomer and dental materials based on it

Patent FR2251567B1

Patent FR2270263A1

Patent FR2242397A1

NOVEL PHOSPHONATE DERIVATIVES, THEIR PREPARATION PROCESS AND THEIR USE AS MODULATORS OF THE ACTIVITY OF TGAMMA9 DELTA2 LYMPHOCYTES

Process for the preparation of vinylphosphonic acid derivatives and the use thereof

Abstract of the disclosures A process for the preparation of vinylphosphonic acid derivatives by heating 2-chloroethanephosphonic acid derivatlves which contain 2-chloroethyl ester groups to temperatures of from 150 to 230°C.

Manufacturing process of vinyl phosphonic acid

Derivatives of [([2- (amino -3,4-dioxo -1-cyclobutene -1-yl)amino]alkyl)] acids

FIELD: organic chemistry. SUBSTANCE: product of the formula (I) where R 1 hydrogen, C 1 -C 6 -alkyl or phenylalkyl with C 7 -C 12 ; R 2 hydrogen, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl or phenylalkyl with C 7 -C 12 or R 1 and R 2 together a group CH 2 -CH 2 -(CH 2 )-CR 6 R 7 -CH 2 or -(CH 2 )-CR 8 R 9 -CR 10 R 11 -CH 2 - in which R 6 , R 8 , R 10 independently each of other hydrogen, C 1 -C 6 -alkyl or hydroxyl; R 7 , R 9 , R 11 independently each of other hydrogen or C 1 -C 6 -alkyl; A C 1 -C 6 -alkylene or C 1 -C 6 -alkenylene; X a group -C(O)OR 3 at R 3 hydrogen, C 1 -C 6 -alkyl or P(O)(OR 4 )(OR 5 ) at R 4 , R 5 independently each of other hydrogen, C 1 -C 6 -alkyl, 3,5-dioxo -1,2,4-oxadiazolidine-2-yl or 5-tetrazolyl, or their pharmaceutically acceptable salts. Reagent 1: compounds of the formula (II) where R 1 as indicated above, R 12 alkoxy, aralkoxy-substituted group containing C 1 -C 5 or C 7 -C 12/ . Reagent 2: compound of the formula HNR 2 -A-X where R 2 , A and X as indicated above. Reaction conditions: in the medium of solvent, at the room temperature or at heating. Synthesized compounds were used as anticonvulsive and neuroprotective agents at excessive release of exciting amino acids. EFFECT: improved method of synthesis. 1 tbl 9506$0с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК С 07Е 9/38, 9/40, А 61 К 31/195, ВИ” 2 039 035 ' 13) СЛ С 07С 227/16, 227/26, 227/32, 31/66 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5010645/04, 20.01.1992 (30) Приоритет: 22.01.1991 Ц$ 07/644157; 07/806861 (46) Дата публикации: 09.07.1995 (56) Ссылки: Уоткинс Дж.К, Эванс Р.Х., Алли. Ве\у. Рвагтасо! Тох!со|, 1981, 21, с.165.Леман Дж. и др. /.РПагтасо! Ехр. ТПег, 1988, 246, с.65.Шмутц М. и др. АБ$ Зос. Меигоза, 1988, 14, с.864.Патент США М 4761405, кл. С О7Е 9/38, 1988. (71) Заявитель: Американ Хоум Продактс Корпорейшн (ЦЗ) (72) Изобретатель: Уильям Алвин Кинни[ЧЗ}], Динна Колетг Гаррисон[ 0$] (73) Патентообладатель: ...

Treatment of phosphating layers

Novel phosphonic acid compounds and method of preparation

Novel phosphonic acid-containing compounds such as (2-(4-ethylphenyl)ethenyl)-phosphonic acid and esters thereof are disclosed. A method preparation of the phosphonic acids comprising contacting a diethylenically unsaturated aromatic compound and phosphorus pentachloride in the present of sulfur dioxide is also disclosed. The compounds of this invention are useful as monomers for the preparation of polymers having enhanced anti-corrosive properties.

PROCESS FOR PREPARING AN ALIPHATIC PHOSPHONIC ACID

Die Erfindung betrifft ein Verfahren zur Herstellung einer aliphatischen Phosphonsaeure fuer die Anwendung in der Landwirtschaft als Pflanzenschutzmittel. Fuer die Herstellung einer aliphatischen Phosphonsaeure der Formelwird ein Diester der aliphatischen Phosphonsaeure der allgemeinen Formelzusammen mit wasserfreiem Halogenwasserstoff in eine Reaktionszone gebracht. R1 und R2 bedeuten substituierte und unsubstituierte Aryl-, Alkyl- und Alkenylgruppen mit 1 bis 6 Kohlenstoffatomen u. a. Erfindungsgemaess wird das Volumen der Reaktionszone durch kontinuierliche Zugabe des Reaktanten Diester der aliphatischen Phosphonsaeure ueber 60% der Gesamtreaktionszeit bei etwa 80 bis 95% der Kapazitaet der Reaktanten und/oder Produkte gehalten, indem der genannte Reaktant in einer Menge zugegeben wird, so dass der genannte Reaktant und/oder die Produkte waehrend der Zugabe des Reaktanten immer mindestens 80% des Volumens der Reaktionszone ausfuellen. The invention relates to a process for preparing an aliphatic phosphonic acid for use in agriculture as a plant protection product. For the preparation of an aliphatic phosphonic acid of the formula, a diester of the aliphatic phosphonic acid of the general formula is placed in a reaction zone together with anhydrous hydrogen halide. R1 and R2 represent substituted and unsubstituted aryl, alkyl and alkenyl groups having 1 to 6 carbon atoms and the like. a. According to the invention, the volume of the reaction zone is maintained at about 80-95% of the capacity of the reactants and / or products by continuous addition of the aliphatic phosphonic acid diester reactant over 60% of the total reaction time by adding said reactant in an amount such that said Reactant and / or the products during the addition of the reactant always fill at least 80% of the volume of the reaction zone.

Organophosphorus compounds for the activation of gamma/delta t-cells

The present invention describes organophosphorus compounds of general formula (III) (see formula III) 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.

Inhibitors of NAALADase enzyme activity

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 α-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.

Novel phosphonic acid compounds and method of preparation

Novel phosphonic acid-containing compounds such as (2-(4-ethenylphenyl)ethenyl)-phosphonic acid and esters thereof are disclosed. A method of preparation of the phosphonic acids comprising contacting a diethylenically unsaturated aromatic compound and phosphorus pentachloride in the presence of sulfur dioxide is also disclosed. The compounds of this invention are useful as monomers for the preparation of polymers having enhanced anti-corrosive properties.

Growth regulation process

A growth regulation process involving certain phosphonic acid compounds having the general formula: ##STR1## The growth regulation process of the present invention relates mainly, though not entirely, to the inducement of an ethylene response or ethylene-type response in plants and part thereof including, but not limited to, stems, roots, leaves, flowers, buds, and harvested as well as unharvested fruit. The method of the present invention produces a wide variety of plant growth responses including: 1. Increasing yields 2. Auxin activity 3. Inhibition of terminal growth, control of apical dominance, increase in branching and increase in tillering 4. Changing bio-chemical composition of plant or portions thereof 5. Abscission of foliage, flowers and fruit 6. Hastening ripening and color promotion in fruit 7. Increasing flowering and fruiting 8. Abortion or inhibition of flowering and seed development 9. Prevention of lodging 10. Stimulation of seed germination and breaking of dormancy 11. Resistance to freeze injury 12. Hormone or epinasty effects 13. Interaction with other growth regulators 14. Interaction with herbicides 15. Disease resistance

OMAETTADE AMINOSYROR.

Aminoalkylphosphonates and related compounds as agonists of EDG receptors

本発明は、式（ＩＩ）の化合物ならびにそれらの医薬適合性の塩および水和物を包含する。本化合物は、骨髄、臓器および組織移植拒絶反応などの免疫媒介疾患および状態の治療に有用である。医薬組成物および使用法も包含する。 【化１６】

PROCESS FOR THE PREPARATION OF 4-SUBSTITUTED 2-AMINOALQU-3-ENOIC ACIDS

ß-KETOPHOSPHONIC ACIDS AND DENTAL MATERIALS BASED THEREON

The invent relates to a ß-Ketophosphonic acid according to the general formula (I), in which A = an aliphatic C 1 -C 18 radical, which can be interrupted by -O-, -S-, -CO-O-, -O-CO-O-; n = 1, 2, 3 or 4; m = 1 or 2 ist; X is omitted or is a C 1 -C 10 radical, which can be interrupted by -O-, -S-, -CO-O-, -O-CO-NH- or -CO-NR 1 , wherein R 1 is H or C 1 -C 7 alkyl; and PG = a radically polymerxizable group. The ß-Ketophosphonic acids are suitable in particular for the production of dental materials.

Preparation method of (2-phosphonic acid-propylene) malonic acid

本发明公开了一种减水剂单体（2‑膦酸‑亚丙基）丙二酸的制备方法，具体使用异丙烯膦酸和丙二酸通过迈克尔加成，氯化，脱氯化氢等反应步骤，合成（2‑膦酸‑亚丙基）丙二酸，实现了单元内膦酸基和羧基的共存，（2‑膦酸‑亚丙基）丙二酸继续和烯基聚氧乙烯醚大单体聚合制备的聚羧酸系减水剂，不但具有高分散性，高坍落保持性，且缓凝效果突出，适应多种使用低活性填料制备的混凝土，同时还有效降低了减水剂的单位用量。

Method for preparing conjugated diene phosphonate compounds

It is provided a method for preparing conjugated diene phosphonate compounds with high reactivity, which can be used to prepare a variety of phosphonate-bearing conjugated dienes. Some of those dienes will become reactive monomers to make polymers and co-polymers. The said method comprises the step of reacting α, β- or β, γ-unsaturated ketones or aldehydes with phosphorus acid or its derivates optionally in a mixture of acetic anhydride and/or acetic acid, to obtain a conjugated diene phosphonate compound having the formula (III)

A process for the preparation of phosphonic acid monomers

Comprise the Non-aqueous electrolyte and lithium secondary battery of the phosphonate derivative containing silicyl ester group

本发明提供一种包含含有甲硅烷基酯基的膦酸衍生物的非水电解液。

Novel compounds for modulating cell proliferation

Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.

Process for making derivatives of vinylphosphonic acid or vinylpyrophosphonic acid

The disclosure relates to a process for making derivatives of vinylpyrophosphonic acid, wherein a ketone is reacted with tetraphosphorus hexoxide (P 4 O 6 ) in the presence of a catalytically active proportion of a proton-yielding substance at elevated temperature. Vinylphosphonic acid derivatives are obtained by hydrolyzing the vinylpyrophosphonic acid derivatives with an equivalent proportion of water. More particularly, the ketone used is a compound of the following general formula ##STR1## in which either R stands exclusively for a halogen and R' either stands for a halogen or hydrogen, a halogen-substituted or unsubstituted alkyl, aryl, alkaryl or aralkyl group having from 1 to 18 carbon atoms, and R" stands for an alkyl, aryl, alkaryl, aralkyl or alkenyl group having from 1 to 18 carbon atoms, or R" stands exclusively for an alkenyl group having from 2 to 18 carbon atoms and R and R' being identical or different each stand for hydrogen or a halogen or a halogen-substituted or unsubstituted alkyl, aryl, alkaryl or aralkyl group having from 1 to 18 carbon atoms.

Novel aryl fructose-1,6-bisphosphatase inhibitors

Novel FBPase inhibitors of formula (I) are useful in the treatment of diabet es and other conditions associated with elevated blood glucose.

New derivatives of cyp-eicosanoids

FIELD: medicine; pharmaceuticals. SUBSTANCE: invention relates to a compound of general formula P-E-I (I) or a pharmaceutically acceptable salt thereof, wherein P is a group represented by general formula -(CH 2 ) n -B-(CH 2 ) k -X (II), where B is a carbon-carbon bond; n is 0 or is integer from 3 to 8; and k is 0 or 1; provided that, if n is equal to 0, k is equal to 1; X is a group whose structure is given in the claim, wherein R 1 represents a hydroxyl group; R 2 is -NHR 3 ; where R 3 is (SO 2 R 30 ); R 30 represents C 6 aryl group; R 4 denotes phenyl substituted with -OH; h equals 0; each of R 6 and R 7 independently represents a hydroxyl group; -O(C 1 -C 6 )alkyl group or -O(C 1 -C 6 )alkyldiyl-O(C=O)(C 1 -C 6 ) alkyl group; each of R 8 and R 8' independently represents a hydrogen atom; -C(=O)C 1 -C 6 alkyl; R 9 is C 1 -C 6 alkyl or C 6 aryl; g is equal to 2; X 1 is NH; E represents a group represented by general formula (III) or (IV), where each of R 12 and R 13 independently represents a hydrogen atom; I is -(CH 2 ) m -Y, where Y is a group (a), where each of R 40 and R 41 is a hydrogen atom; R 42 is a methyl group; m is equal to 3 or 4, provided that when E is a group according to general formula (IV), m is 3; and where L and T both represent a carbon atom. . EFFECT: compounds of formula (I) are intended for treating or preventing ventricular arrhythmia or atrial fibrillation; compounds are also intended for treating a condition or disease, on which the positive effect of introduction of derivatives of polyunsaturated fatty acids (PUFA) omega-3 (n-3), wherein administering to a patient in need thereof at least one compound of formula (I) in an amount effective for treating a condition or disease in which introduction of derivatives of PUFA n-3 has a positive effect. 13 cl, 1 dwg, 10 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 309/21 (2006.01) C07C 311/51 (2006.01) C07C 323/41 (2006.01) C07D 277/82 (2006.01) C07D 291/04 (2006.01) C07F 9/30 (2006.01 ...

Method for preparing conjugated diene phosphonate compounds

It is provided a method for preparing conjugated diene phosphonate compounds with high reactivity, which can be used to prepare a variety of phosphonate-bearing conjugated dienes. Some of those dienes will become reactive monomers to make polymers and co-polymers. The said method comprises the step of reacting α, β- or β, γ- unsaturated ketones or aldehydes with phosphorous acid or its derivates optionally in a mixture of acetic anhydride and/or acetic acid, to obtain a conjugated diene phosphonate compound having the formula (III)

Process for the production of aliphatic phosphonic acids

An improvement in the process for the manufacture of aliphatic phosphonic acid, the improvement comprising maintaining the reaction zone volume at about 80 to 95 percent capacity of reactants and/or products by continuously adding diester of aliphatic phosphonic acid reactant up to about 60 percent of the total reaction time, said reactant being added in an amount sufficient such that said reactants and/or products will always be present in said reactor so as to occupy at least 80 percent of the reaction zone volume during said reactant addition.

CHEMICAL COMPOUNDS

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2006 145 200 (13) A (51) ÌÏÊ C07C 65/26 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2006145200/04, 21.06.2005 (71) Çà âèòåëü(è): ÑìèòÊëàéí Áè÷åì Êîðïîðåéøí (US) (30) Êîíâåíöèîííûé ïðèîðèòåò: 22.06.2004 US 60/581,913 (43) Äàòà ïóáëèêàöèè çà âêè: 27.07.2008 Áþë. ¹ 21 (87) Ïóáëèêàöè PCT: WO 2006/002185 (05.01.2006) Àäðåñ äë ïåðåïèñêè: 191036, Ñàíêò-Ïåòåðáóðã, à/ 24, "ÍÅÂÈÍÏÀÒ", ïàò.ïîâ. À.Â.Ïîëèêàðïîâó R U (57) Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ôîðìóëû (I): , A 2 0 0 6 1 4 5 2 0 0 A (54) ÕÈÌÈ×ÅÑÊÈÅ ÑÎÅÄÈÍÅÍÈß âêëþ÷à åãî ñîëè, ñîëüâàòû è ôàðìàêîëîãè÷åñêè ôóíêöèîíàëüíûå ïðîèçâîäíûå, ãäå: R 1 ïðåäñòàâë åò ñîáîé Í, ÎÍ, àëêîêñè èëè ãàëîãåí; R 2 ïðåäñòàâë åò ñîáîé Í, ÎÍ èëè ãàëîãåí; R 3 ïðåäñòàâë åò ñîáîé àëêèë, ãàëîãåíîàëêèë, öèêëîàëêèë, àëêîêñè èëè àëêîêñèàëêèë; R 4 ïðåäñòàâë åò ñîáîé Í èëè àëêîêñè; R 5 ïðåäñòàâë åò ñîáîé Í, ãàëîãåí èëè ãàëîãåíîàëêèë; R 6 ïðåäñòàâë åò ñîáîé -(Y)z-R 7; z ðàâíî 0 èëè 1; Ñòðàíèöà: 1 RU 2 0 0 6 1 4 5 2 0 0 (86) Çà âêà PCT: US 2005/021963 (21.06.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 22.01.2007 (72) Àâòîð(û): ÕÅÉÐ Äåííèñ (US), ÔÀÍà Äæèíã (US), ÍÀÂÀÑ Òðåòèé Ôðýíê (US), ÊÀÒÀÌÐÅÄÄÈ Ñóááà Ðåääè (US), ÏÅÊÕÀÌ Äæåííèôåð Ïóë (US), ÒÅÐÍÁÓËË Ôèëèï Ñòþàðò (US), ÌÈËËÅÐ Ààðîí Áýéí (US), ÀÊÂÀÁÈ-ÀÌÅÉÎ Àäâîà (US) Y ïðåäñòàâë åò ñîáîé -шÑ- èëè -CR e=CR f-; êîãäà z ðàâíî 0, òîãäà R 7 ïðåäñòàâë åò ñîáîé àëêèë, àëêîêñè, àðèë, ãåòåðîàðèë, ãåòåðîöèêëèë, öèàíî, -CO2R a, -(CH2)tCO2R a, -O(CH2)tCO2R a, -O(CH2)tCN, -(ÑÍ2)tÎÍ, -O(CH2)tOH, -O(CH2)t A 2 0 0 6 1 4 5 2 0 0 R U A Ñòðàíèöà: 2 2 0 0 6 1 4 5 2 0 0 êîãäà z ðàâíî 1, òîãäà R 7 ïðåäñòàâë åò ñîáîé -CO2Í, -(ÑÍ2)tCO2Í, -(CH2)tOH, -CONR aR b èëè -PO3HR a; R a ïðåäñòàâë åò ñîáîé àëêèë, öèêëîàëêèë, àðèë, ãåòåðîàðèë èëè ãåòåðîöèêëèë; R b ïðåäñòàâë åò ñîáîé àëêèë, öèêëîàëêèë, àðèë, ãåòåðîàðèë èëè ãåòåðîöèêëèë; R c ïðåäñòàâë åò ñîáîé àëêèë, öèêëîàëêèë, àðèë, ãåòåðîàðèë èëè ...

Chemical connections

Foreliggende oppfinnelse vedrører nye forbindelser med forskjellige terapeutiske anvendelser, mer spesielt nye naftalenforbindelser som er spesielt nyttige for selektiv østrogenreseptormodulering.

Methods of cancer treatment using naaladase inhibitors

Phosphorus-substituted isoprenoid derivative

A phosphorus-substituted isoprenoid derivative represented by general formula (I) or a pharmacologically acceptable salt thereof, useful for preventing and treating diseases for which a squalene synthetase inhibition is efficacious. In formula (I), R¹ and R² represent each hydrogen, lower alkyl, cycloalkyl, alkenyl, alkynyl, aryl which may be substituted, arylalkyl which may be substituted on the aryl moiety, heteroaryl or heteroarylalkyl; R³ and R⁴ represent each hydrogen, lower alkyl or alkali metal; Y represents -P(O)(OR⁵)(OR⁶) (wherein R⁵ and R⁶ represent each hydrogen, lower alkyl or alkali metal) or -CO₂R⁷ (wherein R⁷ represents hydrogen, lower alkyl or alkali metal); Z represents -(CH₂) m - (wherein m represents an integer of 0 or 1 to 3), -(CH₂) p -CH=CH-(CH₂) q - (wherein m represents 0 or 1 and q represents 1 or 2), or -A-NR⁸-(CH₂) r - (wherein R⁸ represents hydrogen or lower alkyl, A represents C₁ to C₅ alkylene, and r represents an integer of 0 or 1 to 5); and n represents an integer of 0 or 1 to 5.

METHOD FOR PRODUCING VINYLPHOSPHONIC ACID

Chemical compounds

本发明涉及具有各种治疗用途的新化合物，更尤其是新的萘化合物，尤其是它们可用于选择性雌激素受体调节。

[[2-(amino-3,4-dioxo-1-cyclobuten-1-yl)amino]alkyl]-acid derivatives

A compound of the formula: in which R1 is hydrogen, alkyl or phenylalkyl; R2 is hydrogen, alkyl, alkenyl or phenylalkyl; or R1 and R2 taken together are -CH2CH2-, -CH2C(R6)(R7)CH2- or -CH2C(R8)(R9)-C(R10)(R11)CH2-, where R6, R8 and R10 are, independently, hydrogen, alkyl of 1 to 6 carbon atoms or hydroxyl and R7, R9 and R11 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; A is alkylene or alkenylene; X is CO2R3 in which R3 is hydrogen or alkyl, P(O)(OR4)(OR5) in which R4 and R5 are, independently, hydrogen or alkyl, 3,5-dioxo-1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl; or a pharmaceutically acceptable salt thereof are useful as neuroprotectants.

Processes and compositions for the regulation of plant growth

Zinant phosphinyl derivatives are naaldase inhibitors

Aminophosphonic acid derivative, salt thereof, and modulator of s1p receptor

Aminophosphonic acid derivatives (e.g., 2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentylphosphonate monoester) are represented by the following general formula (1): (see formula 1) and act as effective S1P receptor modulators while posing less side effects.

Novel unsaturated amino acid

(57)【要約】 【課題】 本発明は、Ｎ−メチル−Ｄ−アスパラギン酸 感受性レセプターの遮断に反応する疾病の治療に適する 新規化合物の提供を課題とする。 【解決手段】 本発明は、（２Ｒ）−Ｅ−２−アミノ− ４−メチル−５−ホスホノ−３−ペンテン酸エチルエス テルに関する。

Certain phosphinyl derivatives useful as naaladase inhibitors

(2-amino-3,4-dioxo-1-cyclobuten-1-yl) amino alkyl acid derivatives; precursors therefor and pharmaceutical compositions

((2-Amino-3,4-dioxo -1-cyclo-buten-1-yl) amino)alkyl)acid derivs. of formula (I) and their salts are new: R1 = H, 1-6C alkyl or 7-12C phenylalkyl; R2 = H, 1-6C alkyl, 2-6C alkenyl or 7-12C phenylalkyl; or R1 + R2 = Z; Z = -CH2CH2-, -CH2C(R6)(R7)CH2- or -CH2C(R8)(R9)-C(R10)(R11)CH2-; R6, R8, R10 = H, 1-6C alkyl or OH; R7, R9, R11 = H or 1-6C alkyl; A = 1-6C alkylene or 2-6C alkenylene; X = CO2R3, P(O)(OR4)(OR5), 3,5-dioxo-1,2,4-oxadiazolidin-2-yl or 5-tetrazolyl; R3 = H or 1-6C alkyl; R4, R5 = H or 1-6C alkyl. Also claimed are intermediates of formula (XII) and their salts: X2 = CN, COOR14, -PO(OR15)(OR16), 3,5-dioxo-1,2,4-oxadiazolidinyl or opt. protected 5-tetrazolyl; R12 = alkoxy or aralkoxy leaving gp.; R13 = H, 1-6C alkyl, 2-6C alkenyl, 7-12C phenylalkyl or NHP; R14 = H, 1-6C alkyl or carboxyl protecting gp.; R15, R16 = H or 1-6C alkyl; P = amino protecting gp.

Preparation method and application of straight-chain double-bond hydrogenation catalyst

本发明公开了直链双键加氢催化剂的制备方法，包括：步骤一、将活性炭于水中蒸煮；步骤二、将水处理后活性炭于双氧水中蒸煮；步骤三、将双氧水处理后活性炭微波真空处理；步骤四、将含有乙氧基化烷基硫酸钠的氯化钯溶液与微波处理后活性炭混合，陈化，得到催化剂前驱体；或者为，将含有乙氧基化烷基硫酸钠、氯化钯和氯化铂的溶液与微波处理后活性炭混合，陈化，得到催化剂前驱体；步骤五、还原、活化，得到直链双键加氢催化剂。此外，本发明还提供利用该催化剂催化合成磷霉素中间体的方法。采用本发明方法得到的催化剂在催化合成磷霉素中间体顺丙烯磷酸反应中显现出良好催化性能，选择性为93.0％～98.5％，收率为55.8％～59.1％。

Unsaturated amino acids

Phosphorus-contg. unsaturated amino acids of formula (I) and their salts are new: R1 = hydroxy or etherified hydroxy; R2 = H, alkyl, hydroxy or etherified hydroxy; R3 = H, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl; R4 = H, alkyl or arl; R5 = H or alkyl; R6 = carboxy or esterified or amidated carboxy; R7 0 amino opt. substd. by alkyl or aryl; A = opt. alkyl-substd. 1-3C alpha, omega-alkylene or a direct bond; B = methyleue or direct bond; provided that A and B are both direct bonds. Specifically claimed are 9 cpds. including E-2-amino-5- phosphono-3-pentenoic acid, E-2-amino-4-methyl-5-phosphono -3-pentenoic acid, and E-2-amino-4-methyl -5-phosphono-3-pentenoic acid ethyl ester.

Enpp1 inhibitors and their use for the treatment of cancer.

Se proporcionan compuestos, composiciones y métodos para la inhibición de ENPP1. Aspectos de los métodos de la presente incluyen poner en contacto una muestra con un inhibidor de ENPP1 para inhibir la actividad de hidrólisis de cGAMP de ENPP1. En algunos casos, el inhibidor de ENPP1 es impermeable a las células. También se proporcionan composiciones y métodos para tratar el cáncer. Aspectos de los métodos incluyen administrarle a un sujeto una cantidad terapéuticamente eficaz de un inhibidor de ENPP1 para tratar el cáncer del sujeto. En determinados casos, el cáncer es un cáncer de tumor sólido. También se proporcionan métodos para administrar radioterapia a un sujeto ya sea antes o después de administrar un inhibidor de ENPP1. La radioterapia puede administrarse a una dosificación y/o frecuencia eficaz para reducir el daño de radiación al sujeto. En determinados casos, el método se realiza en combinación con un agente quimioterapéutico, o un inhibidor del punto de control o ambos.

Method for preparing conjugated diene phosphonate compounds

Process for the after-treatment of phosphate coatings

Phosphatized metal surfaces such as iron or steel are after treated with solutions of an alkene phosphonic acid having two or three carbon atoms per molecule and dried at a temperature not exceeding 200 DEG C. The alkene phosphonic acid such as vinyl phosphonic acid is dissolved in water, an aliphatic alcohol containing 1-4 carbon atoms per molecule or a mixture of such an alcohol with water. The concentration of the phosphonic acid in solution is 0.02-0.5% by weight and the treatment may be effected by immersion, spraying or flooding.

METHOD FOR PRODUCING VINYPHOPHONIC ACID DERIVATIVES

Novel geranylgeranyl-derivatives, process for the preparation thereof and related pharmaceutical compositions

The present invention relates to novel geranylgeranyl-derivatives and the pharmaceutically acceptable salts thereof having antiproliferative acitivity in eukaryotic cells with respect to the inhibition of protein geranylgeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process for the preparation thereof.

Inorganic material, device and organic electroluminescent device

【課題】高い効率および素子寿命の長い有機デバイスに用いられる無機材料を提供する、特に、該有機デバイスに用いる電極材料を提供する。 【解決手段】下記一般式（１）で表されるリン酸化合物で表される化合物で修飾されたことを特徴とする無機材料。 一般式（１） Ｔ−Ｌ−Ｒ 〔式中、Ｔは窒素原子を２つ以上含有する電荷輸送部位を表す。Ｌは２価の連結基または単結合を表す。Ｒは−ＰＯ（ＯＨ） ２ 又は−ＳｉＸ １ Ｘ ２ Ｘ ３ を表す。Ｘ １ 、Ｘ ２ 、Ｘ ３ は脱離基を表す。一分子中の−ＰＯ（ＯＨ） ２ 又は−ＳｉＸ １ Ｘ ２ Ｘ ３ の個数は１個である。〕 【選択図】なし

Patent FR2055037A5

Prodrugs of naaladase inhibitors

The present invention relates to the prodrugs of NAALADase inhibitors, pharmaceutical compositions comprising the same, and methods of using the same to treat glutamate abnormalities and prostate diseases.

Geranylgeranyl-derivatives, process for the preparation thereof and related pharmaceutical compositions

The present invention relates to novel geranylgeranyl derivatives and the pharmaceutically acceptable salts thereof having antiproliferative activity in eukaryotic cells with respect to the inhibition of protein geranygeranylation. The invention also relates to the pharmaceutical compositions containing the novel derivatives and to the process of preparation thereof.

Sphingosine-1 -phosphate receptor agonist and antagonist compounds

Phosphono-acid-phosphino-aminoalenic acids

Phosphorus-contg. unsaturated amino acids of formula (I) and their salts are new: R1 = hydroxy or etherified hydroxy; R2 = H, alkyl, hydroxy or etherified hydroxy; R3 = H, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl; R4 = H, alkyl or arl; R5 = H or alkyl; R6 = carboxy or esterified or amidated carboxy; R7 0 amino opt. substd. by alkyl or aryl; A = opt. alkyl-substd. 1-3C alpha, omega-alkylene or a direct bond; B = methyleue or direct bond; provided that A and B are both direct bonds. Specifically claimed are 9 cpds. including E-2-amino-5- phosphono-3-pentenoic acid, E-2-amino-4-methyl-5-phosphono -3-pentenoic acid, and E-2-amino-4-methyl -5-phosphono-3-pentenoic acid ethyl ester.

Farnesyl: protein transferase inhibitors as anticancer agents

本发明涉及某些法呢基；蛋白质转移酶的抑制剂，它作为抗肿瘤剂是有用的。

Hydroxyaminohydrocarbonphosphonic acid derivatives and production and use thereof

Methods of cancer treatment using naaladase inhibitors

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.

Patent RU2020112299A3

Therapeutic cyclopentane derivatives

Disclosed herein is a compound having a structure [(I)] or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

ENPP1 Inhibitors and Their Use for the Treatment of Cancer

Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor is cell impermeable. Also provided are compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of a ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject either before or after administering an ENPP1 inhibitor. The radiation therapy can be administered at a dosage and/or frequency effective to reduce radiation damage to the subject. In certain cases, the method is performed in combination with a chemotherapeutic agent, or a checkpoint inhibitor, or both.

Methods for cancer treatment using inhibitors of naaladase

FIELD: medicine, oncology, biochemistry. SUBSTANCE: invention proposes new methods for inhibition of activity NAALADase, methods for suppression of proliferation of tumor cells and methods for cancer treatment using inhibitors of NAALADase. Methods are characterized by using new medicinal agents - inhibitors of NAALADase that represent N-acetylated alpha-bound acid dipeptidase catabolizing N-acetylglutamate and N- acetylaspartate and glutamic acid. EFFECT: valuable medicinal properties of inhibitors, expanded assortment of agents of claimed designation. 73 cl, 6 dwg, 4 tbl, 65 ex

Prodrugs of naaladase inhibitors

Non-halogen flame retardant polymers

Non-halogenated monomers that can be polymerized into flame retardant polymers, and processes to produce the monomers and polymers is provided. In a simplest aspect, there is provided a monomer composition that can comprise a) a group derived from one of a (meth)acrylic acid, (meth)acrylamide, or vinylbenzene, b) a polyphosphate moiety, and c) an amine species. In the monomer composition, the ethylenically unsaturated monomer of (a) is covalently bonded directly or through a linking group to the moiety of b), forming a precursor monomer unit. The amine species of c) is in complex with the precursor monomer unit. The polymer can be a homopolymer of the monomer composition, or a copolymer of the monomer composition having varying a), b) and c). In one embodiment, the polymer can additionally comprise ethylenically unsaturated monomers not covalently bonded to a polyphosphate moiety.

Novel aryl fructose-1,6-bisphosphatase inhibitors

NOVEL ISOMERIC AMINO ACIDS, THEIR PREPARATION AND MEDICAL APPLICATION

L'INVENTION CONCERNE LA CHIMIE PHARMACEUTIQUE. ELLE A POUR OBJET LES (-)-D- ISOMERES DE COMPOSES DE FORMULE GENERALE: (CF DESSIN DANS BOPI) OU R REPRESENTE UN RADICAL ALIPHATIQUE EVENTUELLEMENT SUBSTITUE (DE PREFERENCE CH),ET X REPRESENTE UN RADICAL ACIDE, SPECIALEMENT UN RADICAL D'ACIDE PHOSPHONIQUE, D'ACIDE SULFONIQUE, D'ACIDE BORONIQUE OU DE TETRAZOLE,DE MEME QUE LEURS SELS. CES COMPOSES SONT PREFERES POUR LE TRAITEMENT DE CERTAINES AFFECTIONS DU SYSTEME NERVEUX CENTRAL.

PROCESS FOR THE PREPARATION OF VINYL PHOSPHONESEUREDERIVATES

Verfahren zum Herstellen von Vinylphosphonsaeurederivaten durch Erhitzen von 2-Chlorethanphosphonsaeurederivaten, die 2- Chlorethylestergruppen enthalten, auf Temperaturen von 150-230 Grad C. A process for preparing vinylphosphonic acid derivatives by heating 2-chloroethanephosphonic acid derivatives containing 2-chloroethyl ester groups at temperatures of 150-230 degrees C.

Fluoroalkenyl compounds and their use as pest control agents

Fluorinated alkene compounds having structure (I) wherein Q is -(C=S)-R1, -(C=W)-R2, or -(P=W)R3R4; wherein W is O or S; and R1 to R4 are as defined in claim 1; are useful for controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds are particularly useful for systemic control of pests.

Acrylamide, Preparation Method And The Use that N-replaces

本发明涉及由含磷的二烯单体和(甲基)丙烯腈经由里特反应制备的新型单体及其制备方法。这些单体的聚合物可用于多种用途，例如水处理、流变改性剂、表面改性等。所述单体具有以下结构(II)，其中R 1 、R 2 、R 3 、R 4 、R 5 、R 6 和R 7 独立地代表氢、烷基、芳基、烷芳基、芳烷基、环烷基、杂环烷基或烯基；R 6 和R 7 分别代表R 9 O和R 10 O，其中R 9 和R 10 代表氢、烷基、芳基、烷芳基、芳烷基、环烷基、烯基或选自Na、Li、Ca的金属；R 8 代表H或CH 3 。

Hydrolytically stable and polymerizable acrylic phosphonic acid

Hydrolysis-stable and polymerizable acrylated mono- and diphosphonic acids, which are 2-(dihydroxyphosphoryl-oxa-alkyl)-acrylic acids or esters or corresponding bis compounds, and their stereoisomers and mixtures are new. Hydrolysis-stable and polymerizable acrylated mono- and diphosphonic acids, which are 2-(dihydroxyphosphoryl-oxa-alkyl)-acrylic acids or esters or corresponding bis compounds of formula (I), and their stereoisomers and mixtures are new; R<1> = H, 1-10 carbon (C) alkyl or 6-10C aryl; R<2> = H, F, 1-5C alkyl or phenyl; R<3> = 1-8C alkylene or phenylene or is absent; Y = oxygen (-O-), sulfur (-S-), 1-8 C alkylene or is absent; n = 1 or 2; X = H, F, 1-5C alkyl or 6-12C aryl if n = 1; X = 1-10C alkylene, 6-10C arylene, 7-20C arylenealkylene or is absent if n = 2; The individual alkyl, aryl, alkylene, arylene, phenyl, phenylene and arylenealkylene groups may have substituent(s). Independent claims are also included for (a) (co)polymers obtained by (co)polymerization of (I); and (b) the preparation of (I).

Non-halogen flame retardant polymkeric substance

本发明提供可被聚合成阻燃剂聚合物的非卤化单体，和产生单体和聚合物的方法。在最简单的方面中，提供一种单体组合物，其可包含a)衍生自(甲基)丙烯酸、(甲基)丙烯酰胺、或乙烯基苯之一的基团，b)多磷酸酯部分，和c)胺类物质。在单体组合物中，(a)的烯属不饱和单体直接或通过连接基团共价地键合到b)的部分，形成前体单体单元。c)的胺类物质与前体单体单元络合。该聚合物可以为单体组合物的均聚物，或具有不同的a)、b)和c)的单体组合物的共聚物。在一个实施方案中，聚合物可另外包含未共价键合到多磷酸酯部分的烯属不饱和单体。

Sphingosine-1 -phosphate receptor agonist and antagonist compounds.

La presente invención se dirige a agentes novedosos, potentes y selectivos, los cuales son agonistas o antagonistas del uno omás de los receptores individuales de la familia del receptor S1P. Los compuestos de la presente invención son útiles como terapéuticos para tratar condiciones médicas asociadas con agonismo o antagonismo de los receptores individuales de la familia del receptor S1P.

Novel vinylbenzene derivatives

Compounds represented by general formula (I) and salts thereof, which are useful as glaucoma remedies, wherein R1 is H, lower alkyl or phenyl, the phenyl being optionally substituted with lower alkyl, hydroxyl, lower alkoxy, halogeno, nitro or phenyl; R?2 and R3¿ are each independently H, halogeno or lower alkyl; R?4 and R5¿ are each independently H, lower alkyl or carboxyl, or a group derived therefrom through esterification; and R6 is carboxyl or phosphono, or a group derived from either through esterification.

7-substituted quinone methides as inhibitors for unsaturated monomers

Ethylenically unsaturated monomers are protected from premature polymerization during manufacture and storage by the incorporation therein of an effective stabilizing amount of a 7-substituted quinone methide compound of formula I: (see formula I) wherein R1 and R2 are independently alkyl of 4 to 18 carbon atoms, cycloalkyl of 5 to 12 carbon atoms or phenylalkyl of 7 to 15 carbon atoms, and R3 is -CN, -COOH, - COOR4 ,- COR5,- OCOR6,- CONR7R8 or -PO(OR9)2 where R4 is alkyl of 1 to 18 carbon atoms, cycloalkyl of 5 to 12 carbon atoms, phenyl or benzyl, R5 is alkyl of 1 to 18 carbon atoms, aryl of 6 to 10 carbon atoms or said aryl substituted by one or two alkyl of 1 to 4 carbon atoms or by hydroxyl, R6 is alkyl of 1 to 18 carbon atoms, aryl of 6 to 10 carbon atoms or said aryl substituted by one or two alkyl of 1 to 4 carbon atoms or by hydroxyl, R7 and R8 are independently hydrogen, alkyl of 1 to 18 carbon atoms or said alkyl substituted by alkylamino of 1 to 4 carbon atoms, by dialkylamino of 2 to 8 carbon atoms or by hydroxyl; benzyl, aryl of 6 to 10 carbon atoms or said aryl substituted by alkyl of 1 to 4 carbon atoms, by alkylamino of 1 to 4 carbon atoms, by dialkylamino of 2 to 8 carbon atoms, by phenylamino or by hydroxyl, or -NR7R8 is morpholino, piperidino or pyrrolidino, and R9 is hydrogen or alkyl of 1 to 18 carbon atoms.

Process for preparing vinyl-phosphonic acid

1. A process for preparing vinylphosphonic acid, which is characterized by heating dialkyl 2-acetoxyethanephosphonates of the general formula see diagramm : EP0065739,P5,F1 in which R denotes alkyl groups having 1 to 4 carbon atoms, at 150 to 270 degrees C in the presence of acid or basic catalysts, reacting the resulting reaction product with orthoesters of the general formula R'C(OR)3 in which R' denotes hydrogen, C1 -C4 -alkyl or C1 -C4 -alkoxy and R denotes alkyl groups having 1 to 4, preferably 1 to 2, carbon atoms, at 30 to 200 degrees C and hydrolyzing the resulting vinylphosphonic acid diesters with water at temperatures between 130 and 230 degrees C while simultaneously distilling off the alcohols formed.