Heterocyclic THR-# receptor agonist compound and preparation method and use therefor

A chemical compound shown in formula (I) below and an isomer thereof or a pharmaceutically acceptable salt thereof. The compound improves THR-β agonistic activity while also improving selectivity for THR-α, thereby improving pharmaceutical quality.

Phosphorous organic compounds and their use.

The invention relates to phosphourous organic compounds of general formula (I), wherein B is an ether group of formula (II)or a keto group of formula (III)or a pentagonal or hexagonal cyclic compound. The invention also relates to the use of these compounds for producing drugs for treatment or prevention of human or animal infections due to viruses, bacteria, fungi or parasites, as well as their use as fungicide, bactericide and herbecide in plants.

Phosphorus organic compounds and their use

DIARYLHARNSTOFFDERIVATE AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS

SUBSTITUTED CYCLOHEXANE DERIVATIVES FOR THE TREATMENT OF DISEASES

PHOSPHONOBERNSTEINSÄUREDERIVATE AND YOUR USE AS DRUGS

Metabotropic glutamate receptor ligand derivatives as naaladase inhibitors

ALL - CIS - 1,3,5 TRIAMINO - 2,4,6 CYCLOHEXANTRIOL DERIVATIVES

CUBANE DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR ANTAGONISTS AND PROCESS FOR THEIR PREPARATION

The present invention relates to therapeutically active cubane compounds, a method of preparing the same, and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases of the central nervous system related to the metabotropic glutamate receptor system.

SUBSTITUTED CYCLOHEXANE DERIVATIVES FOR THE TREATMENT OF DISEASES

Abstract Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I

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, ...

4(3)SUBSTITUTED-4(3)-AMINOMETHYL-(THIO)PYRAN OR -PIPERIDINE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1D) and (1E), or a pharmaceutically acceptable salt thereof, wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; and X is -O-, -S-, -S(O)-, -S(O)2-, or NR'1 wherein R'1 is hydrogen, straight or branched alkyl of from 1 to 6 carbons, or benzyl, -C(O)R'2 wherein R'2 is straight or branched alkyl of 1 to 6 carbons, benzyl or phenyl or -CO2R'3 wherein R'3 is straight or branched alkyl of from 1 to 6 carbons, or benzyl wherein the benzyl or phenyl groups can be unsubstituted or substituted by from 1 to 3 substituents selected from halogen, trifluoromethyl, and nitro, are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS.

RECEPTOR MODULATORS EXCITING AMINO ACIDS

CARBOXYTETRALINPHOSPHONIC ACIDS AND PROCESS FOR THEIR PREPARATION

PROCESS

((CYCLO) ALKYL SUBSTITUTED) - .GAMMA. - AMINOBUTYRIC ACID OF DERIVATIVES (=GABA ANALOGUES), THEIR PRODUCTION AND THEIR USE WITH THE TREATMENT OF NEUROLOGICAL ILLNESSES

PROCEDURE.

.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.

COMPOUNDS AND THEIR USE

NITRIC OXIDE DONORS, COMPOSITIONS AND METHODS OF USE

The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating ...

PHOSPHORUS-CONTAINING MIXTURES, PROCESSES FOR PREPARING THEM AND USE THEREOF

((CYCLO)ALKYL SUBSTITUIERTE)-.GAMMA.-AMINOBUTTERSÄURE DERIVATE (=GABA ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

DIARYLHARNSTOFFDERIVATE UND DEREN VERWENDUNG ALS CHLORIDKANALBLOCKER

TREATMENT OF STEEL WITH ORGANIC PHOSPHONIC OR PHOSPHONOUS ACIDS

... 1418966 Treating phosphated steel CIBAGEIGY AG 7 Oct 1974 [6 Oct 1973] 46794/73 Heading C7U Phosphated mild steel is contacted with a solution containing a compound in which R1 is an aryl or substituted aryl grouping each of 6-20 C atoms, or alkyl with up to 6 C, R2 is H or R1 and R2 together form a 6-membered carbocyclic ring, R3 is H or an acyl grouping containing 2 or 3 C atoms and R4 is a straight or branched alkyl grouping containing up to 20 C atoms, cycloalkyl containing 5 or 6 C atoms, an aralkyl or substituted aralkyl grouping or an aralkylene phosphonic acid grouping containing up to 20 C atoms, A is a saturated divalent alkylene radical containing up to 6 C atoms, X= PO 3 H 2 or PO 2 H 2 and m = 0, 1 or 2 and n is 0 or 1, or a water soluble salt thereof. Said salt may be a Na, K, NH 4 or triethanolamine salt, the steel may have a zinc- or ferric phosphate coating, and application is by spraying or immersion, to enhance corrosion ...

1-ARYL-ALKYLIDENE-INDENYL DERIVATIVES OF TETRAZOLES AND SULPHONIC AND PHOSPHONIC ACIDS

... 1418950 1-Aralkylidene-indene derivatives MERCK & CO Inc 3 Dec 1973 [6 Dec 1972] 55832/73 Headings C2C and C2P Novel compounds I in which R 2 is hydrogen, alkyl, haloalkyl, alkenyl or alkynyl, R 4 , R 5 , R 6 , R 7 , R 8 and R 9 each are hydrogen, alkyl, acyloxy, aryloxy, alkoxy, nitro, amino (which may be acylated or mono- or di-alkylated), alkenyl, alkynyl, alkenyloxy, dialkyaminoalkyl, alkylated sulphanyl, alkylthio, alkylsulphuryl, alkylsulphoxyl, hydroxy, hydroxyalkyl acyl, halo, cyano, carboxy, carbalkoxy, carbamido, haloalkyl, cycoalkyl or cycloalkyloxy, X is alkylene, alkenylene, alkynylene, O, S carbonyl, imino or alkylimino n is 0 or 1, Ar is aryl or heteroaryl and R 3 is a group of Formula II in which M is hydrogen, alkyl or a cation and R1 and R4 are hydrogen or C 1 -C 5 alkyl are prepared by reacting a compound III with an aldehyde R 8 R 9 -Ar-(X) n -CHO. Compounds I in which X is -O- are also prepared by reacting a compound III in which R 3 is -CH 2 -COOC ...

ANTAGONIST OF ATTRACTION-TRANSFERRING AMINO ACIDS

1-SUBSTITUIERTE-1-AMINOMETHYL-CYCLOALKAN of DERIVATIVES (= GABAPENTIN ANALOGUES), THEIR PRODUCTION AND THEIR USE WITH the TREATMENT OF NEUROLOGICAL ILLNESSES

Substituted cyclohexane derivatives for the treatment of diseases

Alpha-phosphonosulfonate squalene synthetase inhibitors and method

Cubane derivatives as metabotropic glutamate receptor antagonists and process for their preparation

SUBSTITUTED INDENYL ACID COMPOUNDS

SUBSTITUTED INDENYLALKANOLS

Anticorrosive coating of steel

Anticorrosive coating of steel

New containing compounds of the phosphorus, proceeded for their preparation and their uses

Novel carbocyclic phosphonic acid compounds

The flotation tendencies of pigments in paints, particularly alkyd paints, are inhibited by incorporating therein, preferably at the milling stage, a phosphonic compound of the formula wherein Z is OH or halogen, Y is a -COOR radical wherein R is either (i) C1-C4 alkyl or (ii) a (CH2CH2O)n-R1 radical wherein R1 is either C1-C4 alkyl or C(O)R11 wherein R11 is C1-C4 alkyl and n is 1 or 2. Specified pigments are titanium dioxide, phthalocyanine blue and arylamide yellow and the alkyd resin may be a long oil linseed (or medium oil)/ phthalic/pentaerythritol alkyd. The paint may be a stoving lacquer in which an alkyd resin, e.g. a castor/phthalic/glycerol alkyd is used in conjunction with an amino resin, e.g. an unmodified butylated melamine formaldehyde resin and in this case the phosphonic compound is added (as a solution in ethylene glycol ethyl ether) to the latter before mixing with the alkyd resin. The paints may be made up in xylol or white spirit and may contain cobalt ...

ALL-CIS-1,3,5-TRIAMINO2,4,6-CYCLOHEXANTRIOLDERIVATE, YOUR USE, PROCEDURE FOR YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL ONE PREPARATIONS.

MODULATORS OF BY AMINO ACIDS SUGGEST-CASH RECEPTORS

Cubane derivatives as metabotropic glutamate receptor antagonists and process for their preparation

1-substituted-1-aminomethyl-cycloalkane derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders

Vitamin d derivatives with phosphorous atoms in the side chains

DIARYLUREA DERIVATIVES AND THEIR USE AS CHLORIDE CHANNEL BLOCKERS

The present invention relates to novel diarylurea derivatives represented by general formula (I) useful as chloride channel blockers. In other aspects th e invention relates to the use of these compounds in a method for therapy, suc h as for the treatment of bone metabolic diseases, diseases responsive to modulation of the mast cell or basophil activity, diseases responsive to inhibition of angiogenesis, or sickle cell anaemia, and to pharmaceutical compositions comprising the compounds of the invention.

4(3)SUBSTITUTED-4(3)-AMINOMETHYL-(THIO)PYRAN OR -PIPERIDINE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1D) and (1E), or a pharmaceutically acceptable sal t thereof, wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; and X is -O-, -S-, -S(O)-, -S(O)2-, or NR'1 wherein R'1 is hydrogen, straight or branched alkyl of from 1 to 6 carbons, or benzyl, -C(O)R'2 wherein R'2 is straight or branched alkyl of 1 to 6 carbons, benzyl or phenyl or -CO2R'3 wherein R'3 is straight or branched alkyl of from 1 to 6 carbons, or benzyl wherein the benzyl or phenyl groups can be unsubstituted or substituted by from 1 to 3 substituents selected from halogen, trifluoromethyl, and nitro, are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS.

ALL-Cis-1,3,5-TRIAMINO-2,4,6-CYCLOHEXANETRIOL DERIVATIVES

An all-cis-1,3,5-triamino-2,4,6-trihydroxy cyclohexane of formula (I) , its acid salt, or quat. ammonium salt are prepd. In the formulas, R1-R6= each H, alkyl or -CO-alkyl (alkyl= C1-8 and may contain at least 1 functional gp. capable of coordinating with metal cations), at least one of R1-R6= (un)substd. alkyl or -CO-alkyl. Phloroglucinol is used as a starting material for the prepn. of (I) which may subsequently be quaternised by alkylation to give corresp. mono-, di- and tri-quat. prods. The prods. are useful for treating iron accumulation and as ligands. Copyright 1997 KIPO ...

Antagonists of specific excitatory amino acid neurotransmitter receptors having increased potency

The invention pertains to novel, potent anticonvulsants, analgesics, cognition enhancers and neuroprotectants achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to ω-[2-(phosphonoalkylenyl)-cycloalkyl]-2-aminoalkanoic acids having general formula: см. иллюстрацию в PDF-документе wherein R1 and R2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl (C1 to C6), alkyl (C7 to C12), fatty acid chain (C13 to C24), aryl, aralkyl, hydroxyl; the stereoisomers being in their resolved or racemic form; n and m=0,1,2 or 3; z=0,1 or 2; the cycloalkyl ring being replaced with the cycloalkenyl ring; and the pharmaceutically acceptable salts and derivatives thereof.

Sulphonic acid containing indenyl derivatives

New substituted indenyl methyl sulfonic acids and derivatives thereof which have anti-inflammatory, antipyretic and analgesic activity. Also included are methods of preparing said indenyl compounds, pharmaceutical compositions having said indenyl compounds as an active ingredient and methods of treating inflammation by administration of said indenyl compounds.

((CYCLO)ALKYL SUBSTITUIERTE)-.GAMMA.-AMINOBUTTERSÄURE DERIVATE (=GABA ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

Neue, substituierte Cyclopentylaminderivate, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel

((CYCLO)ALKYL SUBSTITUTED)-GAMMA-AMINOBUTYRIC ACID DERIVATIVES (=GABA ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1A) and (1B) are disclosed and are useful as agent s in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates useful in the preparation are also disclosed.

NITRIC OXIDE DONORS, COMPOSITIONS AND METHODS OF USE

The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating ...

1-ARYL-ALKYLIDENE-INDENYL DERIVATIVES OF TETRAZOLES AND SULPHONIC AND PHOSPHONIC ACIDS

DERIVATIVES OF 1-SUBSTITUÍDO-1-AMINOMETIL-CICLOALCANO (=ANÁLOGOS OF GABAPENTINA), ITS PREPARATION AND ITS USE IN the TREATMENT OF NEUROLOGICAL RIOTS

PHOSPHOSUCCINIC ACID DERIVATIVES AND THEIR USE AS MEDICAMENTS

Compounds have formula (I), in which R1, R2 may represent independently from each other hydrogen, lower alkyl, cycloalkyl or arylmethyl; R3, R4 may represent independently from each other hydrogen, lower alkyl, or one of the groups -OR6 or -NR7R8, or they may form together with the atoms to which they are bound a five- to seven-membered carbocyclic ring or an heterocyclic ring containing one or two heteroatoms; R5 stands for lower alkenyl, cycloalkyl, cycloalkenyl, monocyclic arylalkyl, bicyclic aryl, biaryl or a group having formulae (a): R9-X-alk- or (b), or forms together with R4 and the carbon atom to which it is bound a possibly substituted five- to seven-membered carbocyclic or heterocyclic ring; R6 stands for hydrogen, lower alkyl or arylmethyl; R7, R8 represent independently from each other hydrogen or lower alkyl or form together with the nitrogen atom to which they are bound a five- or six-membered heterocyclic ring; R9 stands for hydrogen, lower alkyl, lower alkenyl, cycloalkyl ...

Excitatory amino acid receptor modulators

Compounds of the formula см. иллюстрацию в PDF-документе in which R1 and R2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.

Excitatory amino acid antagonists

An unexpectedly more potent isomer of 2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a known excitatory amino acid antagonist, pharmaceutical compositions including this isomer and methods of using this isomer to antagonize excitatory amino acid receptors.

СРЕДСТВО ДЛЯ ИНГИБИРОВАНИЯ ГЛЮКОЗО-6-ФОСФАТАЗНОЙ СИСТЕМЫ ПЕЧЕНИ МЛЕКОПИТАЮЩИХ

Предложено средство для ингибирования глюкозо-6-фосфатазной системы печени млекопитающих. Средство представляет собой сложные эфиры производных циклогексана общей формулы I где A-B, R3, R4, R5, Y и Z имеют указанные значения. Изобретение расширяет арсенал средств указанного назначения. 2 з.п. ф-лы, 5 табл.

INDENYLAETHYLTETRAZOLE, -SULFONSAEUREN UND -PHOSPHORSAEUREN

ALL-CIS-1,3,5-TRIAMINO-2,4,6-CYCLOHEXANETRIOL DERIVATIVES, THEIR USE, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL PREPARATIONS CONTAINING THEM

... all-cis-1,3,5-Triamino-2,4,6-trihydroxycyclohexane derivatives corresponding to the general formula I wherein the symbols R1, R2, R3, R4, R5 and R6 are identical or different and represent hydrogen atoms, alkyl groups or -CO-alkyl groups wherein the alkyl in the alkyl or -CO-alkyl group has 1 to 18 carbon atoms and the alkyl and -CO-alkyl groups may contain, independently of one another, one or more identical or different functional groups, and at least one of the groups R1 to R6 is one of the above mentioned unsubstituted or substituted alkyl groups or -CO-alkyl groups, and their salts with pharmacologically conventionally used inorganic or organic acids and their quaternary ammonium salts, processes for their preparation and their use, and pharmaceutical preparations containing these compounds.

EXCITATORY AMINO ACID ANTAGONISTS

... 2097910 9210099 PCTABS00013 An unexpectedly more potent isomer of 2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a known excitatory amino acid antagonist, pharmaceutical compositions including this isomer and methods of using this isomer to antagonize excitatory amino acid receptors.

SUBSTITUTED INDENYLALKANOLS

1-SUBSTITUIERTE-1-AMINOMETHYL-CYCLOALKAN DERIVATE (= GABAPENTIN ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

Substituierte Cyclohexan-Derivate zur Behandlung von Krankheiten

ALL-CIS-1,3,5-TRIAMINO-2,4,6-CYCLOHEXANTRIOL-DERIVATE, VERFAHREN ZU IHRER HERSTELLUNG UND SIE ENTHALTENDE PHARMAZEUTISCHE PRAEPARATE

Excitatory amino acid receptor modulators

EXCITATORY AMINO ACID RECEPTOR MODULATORS

Compounds of formula (I) in which R1 and R2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.

1-SUBSTITUTED-1-AMINOMETHYL-CYCLOALKANE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from (1), (2), (3), (4), (5) wherein \Ablank; is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

1-ARYL-ALKYLIDENE-INDENYL DERIVATIVES OF TETRAZOLES AND SULPHONIC AND PHOSPHONIC ACIDS

Derivados de cubana como antagonistas de receptor de glutamato metabotrópico e processo para a sua preparação

-4(3)-İkameli -4(3)- aminometil-(tio) piran veya- piperidin türevleri (=Gabapentin analogları), hazırlanmaları ve nörolojik hastalıkların tedavisinde kullanımları

PHOSPHOSUCCINIC ACID DERIVATIVES AND THEIR USE AS MEDICAMENTS

KORROSIONSSCHUTZ VON STAHL

Bleach fixing bath for processing exposed colour photographic material

A bleach fixing bath comprises a content of a non-nitrogenous phosphono carboxylic acid with at least 2 carboxylic acid groups.

CARBOXYTETRALINPHOSPHONSAEUREN SOWIE EIN VERFAHREN ZU IHRER HERSTELLUNG

Phosphorous organic compounds and their use

Phosphorous organic compounds and their use

Phosphosuccinic acid derivatives and their use as medicaments

EXCITATORY AMINO ACID RECEPTOR MODULATORS

Compounds of formula (I) in which R1 and R2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.

Excitatory amino acid receptor modulators

ANTAGONISTEN REIZÜBERTRAGENDER AMINOSÄUREN

New amino-cyclopentane carboxylic and phosphonic acid derivatives

... 2-Aminocyclopentane(carboxylic or phosphonic) acid derivatives of formula (I) are new. R1, R2 = H, halo, 3-6C cycloalkyl, or 1-8C alkyl (optionally mono- or disubstituted by halo, OH, Ph, COOH or n-alkoxy or alkoxycarbonyl; R3, R4 = halo, or 1-8C alkyl or cycloalkyl with up to 8C (both optionally mono- or disubstituted by halo, OH, Ph, COOH, alkoxy, acyl or alkoxycarbonyl); R5 = H, 1-8C alkyl (optionally mono- or disubstituted by OH, CHO, acyl, Ar or COAr), 1-8C acyl, COAr or SO2R8; Ar = phenyl (optionally mono- or disubstituted by halo, NO2, CN or alkyl); R6 = H or 1-8C alkyl (optionally substituted by Ph); or R5+ R6 =CHR8; R7 = COAR9 or P(X)(X'R10)2; A = O, S or NH; X, X<1> = O or S; R8 = 1-8C alkyl, COAr' or Ar'; Ar' = phenyl (optionally mono-, di- or trisubstituted by halo, OH, NO2, CN, CF3, OCF3, COOH, alkyl, alkoxy or alkoxycarbonyl); R9 = H, 1-8C alkyl (optionally mono-, di- or trisubstituted by OH, halo, NO2, CN, COOH, CF3, OCF3, alkoxy or SO2R8) or Ph (optionally mono-, di- or ...

4(3)substituted-4(3)-aminomethyl-(thio)pyran or -piperidine derivatives (=gabapentin analogues), their preparation and their use in the treatment of neurological disorders

PHOSPHOROUS ORGANIC COMPOUNDS AND THEIR USE

The invention relates to phosphorous organic compounds of general formula (I), wherein B is an ether group of formula (II) or a keto group of formula (III) or a pentagonal or hexagonal cyclic compound. The invention also relates to the use of these compounds for producing drugs for treatment or prevention of human or animal infections due to viruses, bacteria, fungi or parasites, as well as their use as fungicide, bactericide and herbicide in plants.

CUBAN DERIVATIVES AS ANTAGONISTIC OF RECEIVER OF GLUTAMATO METABOTRÓPICO AND PROCESS FOR ITS PREPARATION

Nitric oxide donors, compositions and methods of use related applications

The invention describes novel nitric oxide donors and novel compositions comprising at least one nitric oxide donor. The invention also provides novel compositions comprising at least one nitric oxide donor, and, optionally, at least one therapeutic agent. The compounds and compositions of the invention can also be bound to a matrix. The invention also provides methods for treating cardiovascular diseases, for the inhibition of platelet aggregation and platelet adhesion caused by the exposure of blood to a medical device, for treating pathological conditions resulting from abnormal cell proliferation; transplantation rejections, autoimmune, inflammatory, proliferative, hyperproliferative, vascular diseases; for reducing scar tissue or for inhibiting wound contraction, particularly the prophylactic and/or therapeutic treatment of restenosis by administering the nitric oxide donor optionally in combination with at least one therapeutic agent. The invention also provides methods for treating ...

All-cis-1,3,5-triamino-2,4,6,-cyclohexanetriol derivatives, their use, processes for their preparation and pharmaceutical preparations containing them

All-cis-1,3,5-Triamino-2,4,6-trihydroxycyclohexane derivatives corresponding to the general formula I I wherein the symbols R1, R2, R3, R4, R5 and R6 are identical or different and represent hydrogen atoms, alkyl groups or -CO-alkyl groups wherein the alkyl in the alkyl or -CO-alkyl group has 1 to 18 carbon atoms and the alkyl and -CO-alkyl groups may contain, independently of one another, one or more identical or different functional groups, and at least one of the groups R1 to R6 is one of the above mentioned unsubstituted or substituted alkyl groups or -CO-alkyl groups, and their salts with pharmacologically conventionally used inorganic or organic acids and their quaternary ammonium salts, processes for their preparation and their use, and pharmaceutical preparations containing these compounds.

1-SUBSTITUIERTE-1-AMINOMETHYL-CYCLOALKAN DERIVATE (= GABAPENTIN ANALOGA), DEREN HERSTELLUNG UND DEREN VERWENDUNG BEI DER BEHANDLUNG VON NEUROLOGISCHEN ERKRANKUNGEN

Novel amines as pharmaceutical agents

Alpha-phosphonosulfinate squalene synthetase inhibitors and method

1-SUBSTITUTED-1-AMINOMETHYL-CYCLOALKANE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1), (1C), (1F), (1G) and (1H) or a pharmaceutical acceptable salt thereof wherein n is an integer of from 0 to 2; m is an integer of from 0 to 3; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A' is a bridged ring selected from (1), (2), (3), (4), (5) wherein is the point of attachment; Z1 to Z4 are each independently selected from hydrogen and methyl; o is an integer of from 1 to 4; and p is an integer of from 0 to 2. In formula (1) above R cannot be sulfonic acid when m is 2 and n is 1 are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially irritable bowel syndrome.

((CYCLO)ALKYL SUBSTITUTED)-GAMMA-AMINOBUTYRIC ACID DERIVATIVES (=GABA ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1A) and (1B) or a pharmaceutically acceptable salt thereof wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; A is hydrogen or methyl; and B is (a), straight or branched alkyl of from 1 to 11 carbons, or -(CH2)1-4-Y-(CH2)0-4-phenyl wherein Y is -O-, -S-, -NR'3 wherein R'3 is alkyl of from 1 to 6 carbons, cycloalkyl of from 3 to 8 carbons, benzyl or phenyl wherein benzyl or phenyl can be unsubstituted or substituted with from 1 to 3 substituents each independently selected from alkyl, alkoxy, halogen, hydroxy, carboxy, carboalkoxy, trifluoromethyl, and nitro are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS. Processes for the preparation and intermediates ...

.ALPHA.-PHOSPHONOSULFINATE SQUALENE SYNTHETASE INHIBITORS AND METHOD

... .alpha.-Phosphonosulfinate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula wherein R2 is OR5 or R5a; R3 and R5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R5a is alkyl, arylalkyl or aryl; R4 is H or pharmaceutically acceptable cation;, 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.

SUBSTITUTED INDENYL ACID COMPOUNDS

4(3)SUBSTITUTED-4(3)-AMINOMETHYL-(THIO)PYRAN OR -PIPERIDINE DERIVATIVES (=GABAPENTIN ANALOGUES), THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISORDERS

Novel amines of formulas (1D) and (1E), or a pharmaceutically acceptable salt thereof, wherein: n is an integer of from 0 to 2; R is sulfonamide, amide, phosphonic acid, heterocycle, sulfonic acid, or hydroxamic acid; and X is -O-, -S-, -S(O)-, -S(O)2-, or NR'1 wherein R'1 is hydrogen, straight or branched alkyl of from 1 to 6 carbons, or benzyl, -C(O)R'2 wherein R'2 is straight or branched alkyl of 1 to 6 carbons, benzyl or phenyl or -CO2R'3 wherein R'3 is straight or branched alkyl of from 1 to 6 carbons, or benzyl wherein the benzyl or phenyl groups can be unsubstituted or substituted by from 1 to 3 substituents selected from halogen, trifluoromethyl, and nitro, are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammatory diseases, and gastrointestinal disorders, especially IBS.

Process for the preparation of vinylphosphonic acid or vinylpyrophonic acid

The disclosure relates to a process for making derivatives of vinylphosphonic acid or vinylpyrophosphonic acid by reacting a ketone with phosphorus trichloride in the presence of phosphorous acid by using the ketone, phosphorous acid and phosphorus trichloride in a molar ratio of 2:1:1, 1 mol phosphorous acid being replaceable by a further mol phosphorus trichloride and 3 mols water.

Modulatoren von durch Aminosäuren anregbare Rezeptoren

New phosphororganic compounds; useful for treatment of bacterial, viral and parasitic infection, and as herbicides or for treating infections in plants

Phosphororganic compounds (I) are new. Phosphororganic compounds and their salts, esters or amides of formula (I) are new. R1, R2 = independently H, halo, OX1 or OX2, or alkyl, hydroxyalkyl, alkenyl, alkynyl, aryl, acyl, cycloalkyl, aralkyl or heterocyclyl (all optionally substituted); X1, X2 = independently H, or alkyl, hydroxyalkyl, alkenyl, alkynyl, aryl, acyl, cycloalkyl, aralkyl or heterocyclyl (all optionally substituted); B = -A1-O-A2-C(Y)(Z), -A3-CO-A4 or a 5- or 6-membered cyclic (preferably heterocyclic) group containing O or N heteroatom(s); A1, A2, A3, A4 = independently alkylene, alkenylene or hydroxyalkylene (one of A1 and A2 or A3 or A4 may also be absent); R3, R4 = independently H, halo, OX3 or OX4, or 1-26C alkyl or hydroxyalkyl, 2-26C alkenyl or alkynyl, or aryl, acyl, cycloalkyl, aralkyl or heterocyclyl (all optionally substituted); X3, X4 = independently H, silyl, an organic or inorganic cation (especially a metal from groups 1, 2 or 3 of the periodic table, ammonium ...

Proton conducting materials

Materials are provided that may be useful as ionomers or polymer ionomers, including compounds including bis sulfonyl imide groups which may be highly fluorinated and may be polymers.

Novel Compounds, Pharmaceutical Compositions Containing Same, Methods of Use for Same, and Methods for Preparing Same

The present invention relates to novel pharmaceutical compositions containing the same, and methods of use for a variety of therapeutically valuable uses including, but not limited to, treating obesity by inhibiting the activity of Glycerol 3-phosphate acyltransferase (GPAT).

ALKYNE AND ALKENE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE-1 RECEPTOR MODULATORS

The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to claim 1 , wherein:{'img': {'@id': 'CUSTOM-CHARACTER-00015', '@he': '3.89mm', '@wi': '6.69mm', '@file': 'US20130150331A1-20130613-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'sup': 14', '15, '“” represents a double bond “—CR═CR—”.'}3. A compound according to claim 1 , wherein:{'sup': '1', 'sub': '2', 'Lis CH.'}4. A compound according to claim 1 , wherein:{'sup': '1', 'Lis O, S or NH.'}7. A compound according to claim 1 , selected from:[3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propyl]phosphonic acid; and3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propanoic acid.8. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , diluents or carrier.9. A pharmaceutical composition according to claim 8 , wherein the compound is selected from:[3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propyl]phosphonic acid; and3-({4-[(1E)-4-(3,4-dimethylphenyl)-3-(3-fluorophenyl)but-1-en-1-yl]benzyl}amino)propanoic acid. This application is a Divisional of U.S. patent application Ser. No. 13/305,398, filed Nov. 28, 2011, which claims the benefit of U.S. Provisional Application Ser. No. 61/419,278 filed Dec. 3, 2010, both of which are hereby incorporated by reference in their entirety.The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals, as modulators of sphingosine-1-phosphate receptors. The invention relates specifically to the use of ...

NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY

The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. A compound according to claim 1 , wherein:{'sup': 1', '10, 'Ris N or C—R;'}{'sup': '2', 'Ris optionally substituted aromatic heterocycle or optionally substituted cycloalkenyl;'}{'sup': 3', '11', '12', '13', '14, 'Ris O, N—R, CH—Ror S, —CR═CR—, —C(O) or —C≡C—;'}{'sup': '4', 'Ris H, optionally substituted aromatic heterocycle, optionally substituted non-aromatic heterocycle, optionally substituted cycloalkyl, optionally substituted cycloalkenyl or optionally substituted aryl;'}{'sup': '5', 'sub': 1-3', '1-3, 'Ris H, halogen, hydroxyl, —OCalkyl, or Calkyl;'}{'sup': '6', 'sub': 1-3', '1-3, 'Ris H, Calkyl, halogen, hydroxyl or —OCalkyl;'}{'sup': '7', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': '8', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': 9', '15, 'sub': 3', '2', '2', '3-6', '2, 'Ris —OPOH, —COOH, —P(O)(OH), —Calkyl, —S(O)OH, —P(O)MeOH, —P(O)(H)OH or —OR;'}{'sup': '10', 'sub': 1-6', '1-3, 'Ris H, Calkyl, halogen, hydroxyl or —OCalkyl;'}{'sup': '11', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '12', 'sub': 1-3', '1-3, 'Ris H, Calkyl, halogen, hydroxyl, —OCalkyl or amino;'}{'sup': '13', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '14', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': '15', 'sub': '1-3', 'Ris H or Calkyl;'}{'sup': 16', '17, 'L is CHR, O, S, NRor —C(O)—;'}a is 0, 1, 2, 3, 4 or 5;b is 0, 1, 2, 3, 4 or 5;c is 0 or 1;d is 0, 1, 2 or 3;{'sup': '16', 'sub': 1-3', '1-3, 'Ris H, Calkyl, —OCalkyl, halogen, hydroxyl or amino, and'}{'sup': '17', 'sub': '1-3', 'Ris H or Calkyl;'}with the provisos:{'sup': 3', '11', '17, 'a). when Ris O, N—R, or S, and b is 0 or 1 then L is not O, S, or NR; and'}{'sup': '9', 'sub': 3', '2', '2', '2, 'b). when Ris —OPOH, —COOH, —P(O)(OH), —S(O)OH, —P(O)MeOH or —P(O)(H)OH'}then d is not 0; and{'sup': 9', '15, 'c). when Ris ORthen d is not ...

Proton conducting materials

Materials are provided that may be useful as ionomers or polymer ionomers, including compounds including bis sulfonyl imide groups which may be highly fluorinated and may be polymers.

FUSED AROMATIC PTP-1B INHIBITORS

The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes. 112-. (canceled)16. The pharmaceutical composition of wherein said biguanide is metformin.17. The pharmaceutical composition of wherein said dipeptidyl peptidase IV inhibitor is one of sitagliptin claim 15 , saxagliptin claim 15 , or vildagliptin claim 15 , or a pharmaceutically acceptable salt of each thereof.18. The pharmaceutical composition of wherein said dipeptidyl peptidase IV inhibitor is sitagliptin or a pharmaceutically acceptable salt thereof.19. The pharmaceutical composition of wherein said second compound is a sulfonylurea.20. The pharmaceutical composition of wherein said sulfonylurea is glimepiride or glipizide.21. The pharmaceutical composition of wherein said PPAR gamma agonist is pioglitazone or rosiglitazone.23. The method of claim 22 , wherein said biguanide is metformin.24. The method of claim 22 , wherein said dipeptidyl peptidase IV inhibitor is one of sitagliptin claim 22 , saxagliptin claim 22 , and vildagliptin claim 22 , or a pharmaceutically acceptable salt of each thereof claim 22 , or combinations thereof.25. The method of claim 22 , wherein said dipeptidyl peptidase IV inhibitor is sitagliptin or a pharmaceutically acceptable salt thereof.26. The method of wherein said second compound is a sulfonylurea.27. The method of wherein said PPAR gamma agonist is pioglitazone or rosiglitazone. This invention relates to a novel class of phosphonic acid derivatives that are inhibitors of PTP-1B and that may be advantageous in the treatment of Type 2 diabetes and other PTP-1B mediated diseases.Protein tyrosine phosphatases are a large family of transmembrane or intracellular enzymes that dephosphorylate substrates involved in ...

PHENYL BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS

The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. The method according to claim 1 , wherein the mammal is a human.10. The method according to claim 1 , wherein the compound of Formula I is selected from:[3-({[5-(4-hexylphenyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;[3-({[4-(4-hexylphenyl)-1-naphthyl]methyl}amino)propyl]phosphonic acid;2-({[5-(4-hexylphenyl)quinolin-8-yl]methyl}amino)ethyl dihydrogen phosphate;3-({[5-(4-hexylphenyl)quinolin-8-yl]methyl}amino)propanoic acid;{3-[({5-[4-(3-phenylpropyl)phenyl]quinolin-8-yl}methyl)amino]propyl}phosphonic acid;(3-{[(5-{4-[3-(2-methylphenyl)propyl]phenyl}quinolin-8-yl)methyl]amino}propyl)phosphonic acid;[3-({[5-(4-hexylphenyl)quinolin-8-yl]methyl}amino)butyl]phosphonic acid;{3-[({5-[3-fluoro-4-(3-phenylpropyl)phenyl]quinolin-8-yl}methyl)amino]propyl}phosphonic acid;[3-({[5-(2-fluoro-4-heptylphenyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;[3-({[5-(3-fluoro-4-heptylphenyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;{3-[({5-[4-(3-ethylheptyl)phenyl]quinolin-8-yl}methyl)amino]propyl}phosphonic acid;[3-({[5-(4-octylphenyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;[3-({[5-(3-fluoro-4-hexylphenyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;{3-[({5-[4-(2-cyclohexylethyl)phenyl]quinolin-8-yl}methyl)amino]propyl}phosphonic acid;2-({[5-(4-hexylphenyl)quinolin-8-yl]methyl}amino)ethanol;(3-{[(5-{3-fluoro-4-[3-(2-methylphenyl)propyl]phenyl}quinolin-8-yl)methyl]amino}propyl)phosphonic acid;(3-{[(5-{3-fluoro-4-[3-(3-methylphenyl)propyl]phenyl}quinolin-8-yl)methyl]amino}propyl)phosphonic acid;(3-{[(5-{3-fluoro-4-[3-(4-methylphenyl)propyl]phenyl}quinolin-8-yl)methyl]amino}propyl)phosphonic acid;{3-[({5-[4-(3-ethylheptyl)-3-fluorophenyl]quinolin-8-yl}methyl)amino]propyl}phosphonic acid;{3-[({5-[4-(2- ...

SUBSTITUTED BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS

The present invention relates to novel substituted bicyclic methyl amine derivatives which are useful as sphingosine-1-phosphate receptors modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors. 8. The method according to claim 1 , wherein the compound is selected from:(3-{[(5-decylquinolin-8-yl)methyl]amino}propyl)phosphonic acid;(3-{[(5-dec-1-yn-1-ylquinolin-8-yl)methyl]amino}propyl)phosphonic acid;[3-({[5-(7-phenylhept-1-yn-1-yl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;[3-({[5-(6-phenylhex-1-yn-1-yl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;[3-({[5-(7-phenylheptyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;(3-{[(5-dec-1-yn-1-ylquinolin-8-yl)methyl]amino}butyl)phosphonic acid;[3-({[5-(6-phenylhexyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;[3-({[5-(5-phenylpent-1-yn-1-yl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;[3-({[5-(5-phenylpentyl)quinolin-8-yl]methyl}amino)propyl]phosphonic acid;2-({[5-(6-phenylhexyl)quinolin-8-yl]methyl}amino)ethanol;2-({[5-(6-phenylhexyl)quinolin-8-yl]methyl}amino)ethyl dihydrogen phosphate;{3-[({5-[6-(3-methoxyphenyl)hex-1-yn-1-yl]quinolin-8-yl}methyl)amino]propyl}phosphonic acid;{3-[({5-[6-(3-methoxyphenyl)hexyl]quinolin-8-yl}methyl)amino]propyl}phosphonic acid;{3-[({5-[6-(3-methoxyphenyl)hexyl]-5,6,7,8-tetrahydroquinolin-8-yl}methyl)amino]propyl}phosphonic acid;{3-[({4-[(1E)dec-1-en-1-yl]-1-naphthyl}methyl)amino]propyl}phosphonic acid;[3-({[4-(6-phenylhex-1-yn-1-yl)-1-naphthyl]methyl}amino)propyl]phosphonic acid;2-({[4-(6-phenylhexyl)-1-naphthyl]methyl}amino)ethanol;2-({[4-(6-phenylhexyl)-1-naphthyl]methyl}amino)ethyl dihydrogen phosphate;[3-({[4-(6-phenylhexyl)-1-naphthyl]methyl}amino)propyl]phosphonic acid;{3-[({4-[6-(3-methoxyphenyl)hex-1-yn-1-yl]-1-naphthyl}methyl)amino]propyl}phosphonic acid;2-[({4-[6-(3-methoxyphenyl)hex-1-yn-1-yl]-1-naphthyl}methyl)amino]ethyl dihydrogen phosphate;{3-[({4-[6-(3-methoxyphenyl)hexyl]-1- ...

NOVEL OXIME DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS

The present invention relates to novel oxime derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 2. The method according to claim 1 , wherein: Lis CH.3. The method according to claim 1 , wherein: Lis O.11. The method according to claim 1 , wherein said compound selected from:3-({4-[({[(1E)-2-(3,5-difluorophenyl)-3-(3,4-dimethylphenyl)-1-methylpropylidene]amino}oxy)methyl]benzyl}amino)propanoic acid;[3-({4-[({[(1E)-2-(3,5-difluorophenyl)-3-(3,4-dimethylphenyl)-1-methylpropylidene]amino}oxy)methyl]benzyl}amino)propyl]phosphonic acid;[3-({4-[({[(1E)-2-(3-chlorophenyl)-3-(3,4-dimethylphenyl)-1-methylpropylidene]amino}oxy)methyl]benzyl}amino)propyl]phosphonic acid;3-[(4-{(1E)-N-[3-(3,4-dimethylphenyl)-2-(3-methylphenyl)propoxy]ethanimidoyl}benzyl)amino]propanoic acid;3-[(4-{(1E)-N-[2-(3-chlorophenyl)-3-(3,4-dimethylphenyl)propoxy]ethanimidoyl}benzyl)amino]propanoic acid;{3-[(4-{(1E)-N-[2-(3-chlorophenyl)-3-(3,4-dimethylphenyl)propoxy]ethanimidoyl}benzyl)amino]propyl}phosphonic acid;{3-[(4-{(1E)-N-[3-(3,4-dimethylphenyl)-2-(3-methylphenyl)propoxy]ethanimidoyl}benzyl)amino]propyl}phosphonic acid;[3-({4-[(1E)-N-{2-[(3,4-dimethylphenyl)sulfonyl]-2-(3-fluorophenyl)ethoxy}ethanimidoyl]benzyl}amino)propyl]phosphonic acid;3-({4-[(1E)-N-{2-[(3,4-dimethylphenyl)thio]-2-(3-fluorophenyl)ethoxy}ethanimidoyl]benzyl}amino)propanoic acid;{3-[(4-{[({(1E)-2-(3-chlorophenyl)-2-[(3,4-dimethylphenyl)thio]-1-methylethylidene}amino)oxy]methyl}benzyl)amino]propyl}phosphonic acid;3-[(4-{[({(1E)-2-(3-chlorophenyl)-2-[(3,4-dimethylphenyl)thio]-1-methylethylidene}amino)oxy]methyl}benzyl)amino]propanoic acid;3-({4-[({[(1E)-2-(3-chlorophenyl)-2-(3,4-dimethylphenoxy)-1-methylethylidene]amino}oxy)methyl]benzyl}amino)propanoic acid;[3-({4-[({[(1E)-2-(3-chlorophenyl)-2-(3,4-dimethylphenoxy)-1-methylethylidene]amino}oxy)methyl]benzyl}amino)propyl]phosphonic acid;3-[(4-{(1E)-N-[2-(3- ...

NOVEL BISPHOSPHONIC ACID COMPOUND

It is intended to provide a novel bisphosphonic acid compound or a salt thereof which shows a remarkable inhibitory effect on ectopic calcification, and a pharmaceutical composition comprising the same. The present invention provides a bisphosphonic acid compound represented by the following formula (1) or a pharmaceutically acceptable salt thereof: 2: The bisphosphonic acid compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'img': {'@id': 'CUSTOM-CHARACTER-00009', '@he': '2.46mm', '@wi': '6.01mm', '@file': 'US20190002482A1-20190103-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, 'wherein is a single bond.'}3: The bisphosphonic acid compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sub': 3-8', '3-8', '1-6', '1-6', '6-10, 'wherein A is a Csaturated cyclic hydrocarbon or a Csaturated heterocyclic ring comprising a sulfur atom or an oxygen atom, wherein the saturated cyclic hydrocarbon or the saturated heterocyclic ring is optionally substituted by 1 to 4 groups selected from the group consisting of a Calkyl group, a Calkoxy group, a Caryloxy group and a halogen atom.'}4: The bisphosphonic acid compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2, 'sub': '1-6', 'wherein Rand Rare each independently a Calkyl group, a halogen atom or a hydrogen atom.'}5: A pharmaceutical composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the bisphosohonic acid compound according to or a salt thereof.'}6: A prophylactic drug for a disease associated with ectopic calcification claim 1 , the prophylactic drug comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the bisphosphonic acid compound according to or a salt thereof as an active ingredient.'}7: A method for producing a prophylactic drug for a disease associated with ectopic calcification claim 1 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001 ...

METHODS TO MODULATE RAC1 IMPORT AND TO TREAT PULMONARY FIBROSIS

The invention provides methods for treating fibrosis, as well as methods for modulating mitochondrial peroxide production in a cell, and methods for modulating the import of Rac1 into the mitochondria of a cell. 13-. (canceled)6. A method to modulate mitochondrial peroxide production in a cell comprising contacting the cell with a compound of formula I claim 4 , formula II or formula III as described in claim 4 , or a pharmaceutically acceptable salt or prodrug thereof.7. A method to modulate mitochondrial peroxide production in a cell comprising contacting the cell with a compound of formula I as described in claim 4 , or a pharmaceutically acceptable salt or prodrug thereof.8. A method to modulate the import of Rac1 into the mitochondria of a cell comprising contacting the cell with a compound of formula I claim 4 , formula II or formula III as described in claim 4 , or a pharmaceutically acceptable salt or prodrug thereof.9. A method to modulate the import of Rac1 into the mitochondria of a cell comprising contacting the cell with a compound of formula I as described in claim 4 , or a pharmaceutically acceptable salt or prodrug thereof.1021-. (canceled)2325-. (canceled)2738-. (canceled)4042-. (canceled)4449-. (canceled)50. The method of wherein the compound is:tetramethyl (E)-1,1-bis(4,8-dimethyl-nona-3,7-dienyl)-1,1-bisphosphonate,tetraethyl 4,8-dimethyl-3,7-nonadienyl-1,1-bisphosphonate,tetraethyl (2E,6E)-1-(3-methyl-but-2-enyl)-3,7,11-trimethyl-dodeca-2,6,10-trienyl-1,1-bisphosphonate,1-(3,7-dimethyl-octa-2,6-dienyl)-4,8-dimethyl-nona-3,7-dienyl-1,1-bisphosphonic acid, tetrasodium salt,tetrapivaloyloxymethyl (E)-1,1-bis(4,8-dimethyl-nona-3,7-dienyl)-1,1-bisphosphonate, or(2E,6E)-1-(3-methyl-but-2-enyl)-3,7,11-trimethyl-dodeca-2,6,10-triene-1,1-bisphosphonate, or a pharmaceutically acceptable salt or prodrug thereof.51. The compound of claim 4 , which is a compound of formula II claim 4 , or a pharmaceutically acceptable salt or prodrug thereof.5264-. (canceled ...

PHOSPHONATE LINKERS AND THEIR USE TO FACILITATE CELLULAR RETENTION OF COMPOUNDS

Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitates cellular retention of the compound are described. 15-. (canceled)7. The compound of claim 6 , wherein the payload is a therapeutic agent claim 6 , a detectable label claim 6 , radionuclide claim 6 , or protecting group.8. The compound of claim 6 , wherein the therapeutic agent is a cytotoxic agent claim 6 , an anti-inflammatory agent claim 6 , peptide claim 6 , or nucleic acid or nucleic acid analog.9. The compound of claim 8 , wherein the anti-inflammatory agent is a glucocorticoid receptor agonist.10. The compound of claim 8 , wherein the anti-inflammatory agent is Cortisol claim 8 , cortisone acetate claim 8 , beclometasone claim 8 , prednisone claim 8 , prednisolone claim 8 , methylprednisolone claim 8 , betamethasone claim 8 , trimcinolone claim 8 , budesonide claim 8 , dexamethasone claim 8 , fluticasone claim 8 , or mometasone.11. The compound of claim 6 , wherein the targeting ligand is an antibody or monoclonal antibody (e.g. claim 6 , chimeric claim 6 , humanized claim 6 , or human) claim 6 , ligand for a receptor claim 6 , lectin claim 6 , saccharide claim 6 , poly(ethylene glycol) claim 6 , polysaccharide claim 6 , or polyamino acid.12. The compound of claim 6 , wherein the targeting ligand is a chimeric claim 6 , humanized claim 6 , or human anti-Her2 antibody claim 6 , anti-CD4 antibody claim 6 , anti-CD20 antibody claim 6 , anti-EGFR antibody claim 6 , anti-CD22 antibody claim 6 , anti-CD23 antibody claim 6 , anti-CD25 antibody claim 6 , anti-CD52 antibody claim 6 , anti-CD30 antibody claim 6 , anti-CD33 antibody claim 6 , anti-CD40L antibody claim 6 , anti-CD70 antibody claim 6 , anti-CD74 antibody claim 6 , anti-CD80 antibody claim 6 , anti-CD163 antibody claim 6 , anti-Mucl8 antibody claim 6 , anti-integrin antibody claim 6 , anti-PSMA antibody claim 6 , anti-CEA antibody claim 6 , anti-CDl Ia antibody ...

HYPOPHOSPHOROUS ACID DERIVATIVES HAVING ANTIHYPERALGIC ACTIVITY AND BIOLOGICAL APPLICATIONS THEREOF

The invention relates to hypophosphorous acid derivatives of formula (I) wherein —X is H or OH, —R represents one or several radicals R-R, identical or different, two of R-Roptionally occupying the same position on the phenyl group, one to four of R-Rbeing H and the others being selected in the group comprising -0-(CH)—COOH; —S—(CH)—COOH; —NH—(CH)—COOH; -0-(CH,R′)—COOH; —O—(CH)—OH; OR′, —R′ being a C-Calkyl radical; —OH; —COOH; halogen, particularly —F, —CI, —Br, —I, —CF; —OCF; —N0; —CH═CH—COOH; —(CH)—COOH; O—(CH)—P0H; O—(CF)—P0H; O—(CH)—S0H; O—(CH)—CONHOH; O—(CH)-tetrazol; O—(CH)-hydroxyisoxazol—n=1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers. 2. The hypophosphorous acid derivatives of claim 1 , having a ECwith respect to mGlu4<0.2 μM.3. The hypophosphorous acid derivatives of claim 2 , having a ECwith respect to mGlu7<15 μM.4. The hypophosphorous acid derivatives of claim 3 , wherein X=—OH and R represents one substituent in para claim 3 , or two substituents in meta and para claim 3 , or three substituents two in meta and one in para claim 3 , respectively.5. The hypophosphorous acid derivatives of claim 4 , wherein the phenyl group is substituted by —O—(CH)—COOH claim 4 , with n=1 or —S—(CH)—COOH with n=1.6. The hypophosphorous acid derivatives of claim 4 , wherein the phenyl group is substituted by two substituents claim 4 , one being —O—(CH)—COOH with preferably n=1 claim 4 , and the other is OR′ claim 4 , with R′ preferably being —CHor CF.7. The hypophosphorous acid derivatives of claim 4 , wherein the phenyl group is substituted by three substituents claim 4 , one being —O—(CH)—COOH with preferably n=1 claim 4 , the second one is —OR′ claim 4 , with R preferably being —CHand the third one is —F claim 4 , —Cl claim 4 , —I or —CO.8. The hypophosphorous acid derivatives of claim 1 , having a ECwith respect to mGlu4< about 1 μM.9. The hypophosphorous acid derivatives of claim 8 , wherein X=—OH or H and R ...

Beta-hydroxy-gamma-aminophosphonates for Treating Immune Disorders

The present disclosure provides methods of treating, ameliorating, or preventing immune disorders, allergic disorders, or inflammatory disorders, or combinations thereof, or providing hepatoprotection in subject. In one aspect, the method comprises administering to a subject a therapeutically effective amount of a β-hydroxy-γ-aminophosphonate or β-amino-γ-aminophosphonate. 2. The method of claim 1 , wherein a compound having Formula I claim 1 , or a pharmaceutically acceptable hydrate claim 1 , crystalline form or amorphous form thereof claim 1 , or a stereoisomer thereof claim 1 , is administered to said subject.5. The method of claim 4 , wherein X is iodide.6. The method according to claim 1 , where said compound having Formula I or said compound having Formula II is administered to said subject as part of a pharmaceutical composition comprising one or more pharmaceutically acceptable excipients.7. The method according to claim 1 , wherein the production of T helper cells is stimulated.8. The method according to claim 1 , wherein the production of cytotoxic T cells is stimulated.9. The method according to claim 1 , wherein the production Tcells is stimulated.11. The method according to claim 10 , wherein a compound having Formula I claim 10 , or a pharmaceutically acceptable hydrate claim 10 , crystalline form or amorphous form thereof claim 10 , or a stereoisomer thereof claim 10 , is administered to said subject.14. The method according to claim 13 , wherein X is iodide.15. The method according to claim 10 , where said compound having Formula I or said compound having Formula II is administered to said subject as part of a pharmaceutical composition comprising one or more pharmaceutically acceptable excipients.16. The method according to for the treatment of an immune disorder.17. The method according to claim 16 , wherein said immune disorder is an autoimmune disorder.18. The method according to claim 10 , wherein said immune disorder claim 10 , allergic ...

PHOSPONATE LINKERS AND THEIR USE TO FACILITATE CELLULAR RETENTION OF COMPOUNDS

Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitates cellular retention of the compound are described. 2. The compound of claim 1 , wherein the payload is a therapeutic agent claim 1 , a detectable label claim 1 , radionuclide claim 1 , or protecting group.3. The compound of claim 1 , wherein the therapeutic agent is a cytotoxic agent claim 1 , an anti-inflammatory agent claim 1 , peptide claim 1 , or nucleic acid or nucleic acid analog.4. The compound of claim 3 , wherein the anti-inflammatory agent is a glucocorticoid receptor agonist.5. The compound of claim 3 , wherein the anti-inflammatory agent is Cortisol claim 3 , cortisone acetate claim 3 , beclometasone claim 3 , prednisone claim 3 , prednisolone claim 3 , methylprednisolone claim 3 , betamethasone claim 3 , trimcinolone claim 3 , budesonide claim 3 , dexamethasone claim 3 , fluticasone claim 3 , or mometasone.7. The compound of claim 6 , wherein the payload is a therapeutic agent claim 6 , a detectable label claim 6 , radionuclide claim 6 , or protecting group.8. The compound of claim 6 , wherein the therapeutic agent is a cytotoxic agent claim 6 , an anti-inflammatory agent claim 6 , peptide claim 6 , or nucleic acid or nucleic acid analog.9. The compound of claim 8 , wherein the anti-inflammatory agent is a glucocorticoid receptor agonist.10. The compound of claim 8 , wherein the anti-inflammatory agent is Cortisol claim 8 , cortisone acetate claim 8 , beclometasone claim 8 , prednisone claim 8 , prednisolone claim 8 , methylprednisolone claim 8 , betamethasone claim 8 , trimcinolone claim 8 , budesonide claim 8 , dexamethasone claim 8 , fluticasone claim 8 , or mometasone.11. The compound of claim 6 , wherein the targeting ligand is an antibody or monoclonal antibody (e.g. claim 6 , chimeric claim 6 , humanized claim 6 , or human) claim 6 , ligand for a receptor claim 6 , lectin claim 6 , saccharide claim 6 , ...

NOVEL FUSED PYRIMIDINE DERIVATIVES FOR INHIBITION OF TYROSINE KINASE ACTIVITY

The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient. 3. The compound of claim 1 , wherein the compound of formula (I) is selected from the group consisting of:N-(3-((2-((4-(4-methylpiperazin-1-yl)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-((2-((4-(4-isopropylpiperazin-1-yl)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-((2-((4-morpholinophenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-((2-((4-((dimethylamino)methyl)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-((2-((4-((4-(dimethylamino)piperidin-1-yl)methyl)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-((2-((3-fluoro-4-(1-methylpiperazin-4-yl)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-((2-((4-(2-dimethylamino)ethyl)amino)-3-fluorophenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-((2-((3-fluoro-4-((1-methylpiperidin-4-yl)amino)phenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide;N-(3-(2-(3-methoxy-4-(4-methyl-piperazin-1-yl)-phenylamino)-furo[3,2-d]pyrimidin-4-yloxy)-phenyl)-acrylamide; andN-(3-((2-((4-sulfamoylphenyl)amino)furo[3,2-d]pyrimidin-4-yl)oxy)phenyl)acrylamide.4. A pharmaceutical composition comprising the compound of formula (I) or its pharmaceutically acceptable salt of as an active ingredient and a pharmaceutically acceptable carrier.5. A pharmaceutical composition comprising the compound of formula (I) or its pharmaceutically acceptable salt of as an active ingredient and a pharmaceutically acceptable carrier.6. A pharmaceutical composition comprising the compound of formula (I) or its pharmaceutically acceptable salt of as an active ingredient and a pharmaceutically acceptable carrier.7. A ...

FUSED AROMATIC PTP-1B INHIBITORS

The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown (Formula I) above and methods of treating or preventing PTP-1B mediated diseases, including diabetes. 112-. (canceled)18. The method of claim 13 , wherein said cancer is breast cancer.19. The method of claim 13 , wherein said cancer is prostate cancer.20. The method of claim 13 , wherein said cancer is ovarian cancer.21. The method of claim 13 , wherein said cancer is multiple myeloma.22. The method of claim 13 , wherein said cancer is leukemia.23. The method of claim 13 , wherein said cancer is melanoma.24. The method of claim 13 , wherein said cancer is lymphoma.25. The method of claim 13 , wherein said cancer is renal cancer.26. The method of claim 13 , wherein said cancer is bladder cancer. This invention relates to a novel class of phosphonic acid derivatives that are inhibitors of PTP-1B and that may be advantageous in the treatment of Type 2 diabetes and other PTP-1B mediated diseases.Protein tyrosine phosphatases are a large family of transmembrane or intracellular enzymes that dephosphorylate substrates involved in a variety of regulatory processes (Fischer et al., 1991, Science 253:401-406). Protein tyrosine phosphatase-1B (PTP-1B) is a ˜50 kd intracellular protein present in abundant amounts in various human tissues (Charbonneau et al., 1989, Proc. Natl. Acad. Sci. USA 86:5252-5256; Goldstein, 1993, Receptor 3:1-15).Numerous proteins are substrates of PTP-1B. One important substrate is the insulin receptor. The binding of insulin to its receptor results in autophosphorylation of the receptor, most notably on tyrosines 1146, 1150, and 1151 in the kinase catalytic domain (White & Kahn, 1994, J. Biol. Chem. 269:1-4). This causes activation of the insulin receptor tyrosine kinase, which phosphorylates the various insulin receptor ...

ALLENE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS

The present invention relates to allene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 3. A compound according to wherein:{'sup': '1', 'sub': '2', 'Lis CH.'}4. A compound according to wherein:{'sup': '2', 'sub': '2', 'Lis CH.'}6. A compound according to selected from:[3-({4-[3-(3,5-Difluorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-3-(2-thienyl)benzyl}amino)propyl]phosphonic acid;[3-({4-[3-(3,5-Difluorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-3-(2-furyl)benzyl}amino)propyl]phosphonic acid;[3-({4-[3-(3,5-Difluorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-2-ethylbenzyl}amino)propyl]phosphonic acid;[3-({4-[3-(3-Chlorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-2-methylbenzyl}amino)propyl]phosphonic acid; and[3-({4-[3-(3-Chlorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-2-ethylbenzyl}amino)propyl]phosphonic acid.7. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.8. A pharmaceutical composition according to wherein the compound is selected from:[3-({4-[3-(3,5-Difluorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-3-(2-thienyl)benzyl}amino)propyl]phosphonic acid;[3-({4-[3-(3,5-Difluorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-3-(2-furyl)benzyl}amino)propyl]phosphonic acid;[3-({4-[3-(3,5-Difluorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-2-ethylbenzyl}amino)propyl]phosphonic acid;[3-({4-[3-(3-Chlorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-2-methylbenzyl}amino)propyl]phosphonic acid; and[3-({4-[3-(3-Chlorophenyl)-4-(3,4-dimethylphenyl)buta-1,2-dien-1-yl]-2-ethylbenzyl}amino)propyl]phosphonic acid.10. A method of claim 9 , wherein the pharmaceutical composition is administered to the mammal to treat ocular diseases claim 9 , wet and dry age- ...

NOVEL PEROXIDE STABILIZERS

Methods for stabilizing one or more peroxide compounds in solution comprising adding to the solution an effective amount of at least one compound selected from the group comprising (i) cyclic carbonates; (ii) poly-phosphonic acid chelating agents and salts thereof, and alkaline pH adjusting agents with a pKb value of up to 3.0, wherein the w/w ratio of the poly-phosphonic acid chelating agent or salt thereof to alkali or alkaline earth metal hydroxide is from about 1:1 to about 50:1; and (iii) mixtures thereof. Also disclosed are solutions comprising the above compounds, uses of the above compounds to stabilize peroxide compounds in solutions, and compounds recited above for use as novel stabilizers. 1. A method of stabilizing a peroxide compound in a solution comprising adding to the solution an effective amount of poly-phosphonic acid chelating agents or salts thereof , and alkaline pH adjusting agents with a pKb value of up to 3.0 , wherein the w/w ratio of the poly-phosphonic acid chelating agent or salt thereof to alkali or alkaline earth metal hydroxide is from about 1:1 to about 50:1.2. The method of claim 1 , wherein the solution is free of quaternary ammonium compounds.3. The method of claim 1 , wherein the peroxide compound is selected from the group comprising hydrogen peroxide claim 1 , hydrogen peroxide adducts claim 1 , group IIIA oxidizing agents claim 1 , or hydrogen peroxide donors of group VIA oxidizing agents claim 1 , group VA oxidizing agents claim 1 , group VIIA oxidizing agents claim 1 , sodium peroxide claim 1 , ureal peroxide claim 1 , perboric acid claim 1 , sodium/potassium perborate claim 1 , sodium persulfate claim 1 , calcium peroxide claim 1 , lithium peroxide claim 1 , sodium peroxide claim 1 , dibenzoyl peroxide claim 1 , diacetyl peroxide claim 1 , di(n-propyl) peroxydicarbonate claim 1 , butyl peroxybenzoate claim 1 , butyl hydroperoxide claim 1 , ethylidene peroxide claim 1 , ethyl hydroperoxide claim 1 , peroximonosulfuric acid ...

NOVEL AROMATIC THIO COMPOUNDS AS RECEPTOR MODULATORS

The present invention relates to novel aromatic thio derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 5. A compound according to claim 1 , wherein:{'sup': 7', '7a, 'Ris CR;'}{'sup': '11', 'Ris H; and'}{'sup': '12', 'Ris H.'}6. A compound according to claim claim 1 , 1 wherein:{'sup': '1', 'Ris S;'}{'sup': 7', '7a, 'Ris CR;'}{'sup': '11', 'Ris H;'}{'sup': '12', 'Ris H;'}{'sup': '13', 'Ris H; and'}{'sup': '14', 'Ris H.'}7. A compound according to claim claim 1 , 1 wherein:{'sup': '1', 'Ris S;'}{'sup': 7', '7a, 'Ris CR;'}{'sup': '11', 'Ris H;'}{'sup': '12', 'Ris H;'}{'sup': '13', 'Ris H;'}{'sup': '14', 'Ris H;'}{'sup': '17', 'Ris H; and'}{'sup': '18', 'Ris H.'}8. A compound according to claim claim 1 , 1 wherein:{'sup': '1', 'Ris S;'}{'sup': 7', '7a, 'Ris CR;'}{'sup': '11', 'Ris H;'}{'sup': '12', 'Ris H;'}{'sup': '13', 'Ris H;'}{'sup': '14', 'Ris H;'}{'sup': '15', 'Ris H;'}{'sup': '16', 'Ris H;'}{'sup': '17', 'Ris H; and'}{'sup': '18', 'Ris H.'}9. A compound according to claim 1 , wherein:{'sup': '1', 'Ris S;'}{'sup': 7', '7a, 'Ris CR;'}{'sup': '8', 'Ris H;'}{'sup': '10', 'Ris H;'}{'sup': '11', 'Ris H;'}{'sup': '12', 'Ris H;'}{'sup': '13', 'Ris H;'}{'sup': '14', 'Ris H;'}{'sup': '15', 'Ris H;'}{'sup': '16', 'Ris H;'}{'sup': '17', 'Ris H; and'}{'sup': '18', 'Ris H.'}10. A compound according to wherein:{'sup': '1', 'Ris S;'}{'sup': '2', 'Ris H, D, F;'}{'sup': '3', 'Ris H, D, F;'}{'sup': '4', 'Ris H, D, F;'}{'sup': '5', 'Ris H, D, F;'}{'sup': '6', 'Ris H, D, F;'}{'sup': 7', '7a, 'Ris CR;'}{'sup': '8', 'Ris H;'}{'sup': '10', 'Ris H;'}{'sup': '11', 'Ris H;'}{'sup': '12', 'Ris H;'}{'sup': '13', 'Ris H;'}{'sup': '14', 'Ris H;'}{'sup': '15', 'Ris H;'}{'sup': '16', 'Ris H;'}{'sup': '17', 'Ris H; and'}{'sup': '18', 'Ris H.'}12. A compound according to selected from:[3-({3-bromo-4-[(5-phenylpentyl)thio]benzyl}amino)propyl]phosphonic acid;[3-({4-[(5- ...

BICYCLIC METHYL AMINE DERIVATIVES AS SPHINGOSINE-1 PHOSPHATE RECEPTORS MODULATORS

The present invention relates to novel bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 4. The method according to claim 1 , wherein the compound of Formula I is selected from:[3-({[7-(4-hexylphenyl)-2,3-dihydro-1H-inden-4-yl]methyl}amino)propyl]phosphonic acid; and[3-({[7-(4-hexylphenyl)-1-benzofuran-4-yl]methyl}amino)propyl]phosphonic.5. The method according to claim 1 , wherein the mammal is a human.7. The method according to claim 6 , wherein the compound is:[3-({[4-(4-hexylphenyl)-1-benzofuran-7-yl]methyl}amino)propyl]phosphonic acid.8. The method according to claim 5 , wherein the mammal is a human. This application is a divisional patent application of United States Non-provisional patent application Ser. No. 13/446,575, filed Apr. 13, 2012, which claims the benefit of U.S. Provisional Application Ser. No. 61/475,352, filed Apr. 14, 2011, which are hereby incorporated in their entirety by reference.The present invention relates to novel phenyl bicyclic methyl amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat disorders associated with sphingosine-1-phosphate (S1P) receptor modulation.Sphingosine-1 phosphate is stored in relatively high concentrations in human platelets, which lack the enzymes responsible for its catabolism, and it is released into the blood stream upon activation of physiological stimuli, such as growth factors, cytokines, and receptor agonists and antigens. It may also have a critical role in platelet aggregation and thrombosis and could aggravate cardiovascular diseases. On the other hand the relatively high concentration of the metabolite in high-density ...

Bicyclic aryl sphingosine 1-phosphate analogs

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Quinazoline and Indole Compounds to Treat Medical Disorders

Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided.

NOVEL PEROXIDE STABILIZERS

Methods for stabilizing one or more peroxide compounds in solution comprising adding to the solution an effective amount of at least one compound selected from the group comprising (i) cyclic carbonates; (ii) poly-phosphonic acid chelating agents and salts thereof, and alkaline pH adjusting agents with a pKb value of up to 3.0, wherein the w/w ratio of the poly-phosphonic acid chelating agent or salt thereof to alkali or alkaline earth metal hydroxide is from about 1:1 to about 50:1; and (iii) mixtures thereof. Also disclosed are solutions comprising the above compounds, uses of the above compounds to stabilize peroxide compounds in solutions, and compounds recited above for use as novel stabilizers. 1. A method of stabilizing a peroxide compound in a solution comprising adding to the solution an effective amount of at least one compound selected from the group comprising (i) cyclic carbonates; (ii) poly-phosphonic acid chelating agents and salts thereof , and alkaline pH adjusting agents with a pKb value of up to 3.0 , wherein the w/w ratio of the poly-phosphonic acid chelating agent or salt thereof to alkali or alkaline earth metal hydroxide is from about 1:1 to about 50:1; and (iii) mixtures thereof.2. The method of claim 1 , wherein the solution is free of quaternary ammonium compounds.3. The method of claim 1 , wherein the peroxide compound is selected from the group comprising hydrogen peroxide claim 1 , hydrogen peroxide adducts claim 1 , group IIIA oxidizing agents claim 1 , or hydrogen peroxide donors of group VIA oxidizing agents claim 1 , group VA oxidizing agents claim 1 , group VIIA oxidizing agents claim 1 , sodium peroxide claim 1 , ureal peroxide claim 1 , perboric acid claim 1 , sodium/potassium perborate claim 1 , sodium persulfate claim 1 , calcium peroxide claim 1 , lithium peroxide claim 1 , sodium peroxide claim 1 , dibenzoyl peroxide claim 1 , diacetyl peroxide claim 1 , di(n-propyl) peroxydicarbonate claim 1 , butyl peroxybenzoate claim 1 , ...

ALKENE DERIVATIVES AS SPHINGOSINE 1-PHOSPHATE (S1P) RECEPTOR MODULATORS

The present invention relates to alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors. 6. A compound according to wherein Lis S(O).7. A compound according to wherein Lis S.8. A compound according to wherein Lis O.9. A compound according to wherein Ris carboxylic acid.10. A compound according to wherein Ris POH.11. A compound according to wherein Lis CH.12. A compound according to wherein Lis CH.13. A compound according to selected from:{3-[(4-{[(5E)-5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hex-5-en-1-yl]sulfanyl}benzyl)amino]propyl}phosphonic acid;3-[(4-{[(5E)-5-(3,5-difluorophenyl)-6-(3,4-dimethylphenyl)hex-5-en-1-yl]sulfanyl}benzyl)amino]propanoic acid;3-[(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]sulfanyl}benzyl)amino]propanoic acid;3-[(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]sulfinyl}benzyl)amino]propanoic acid;3-[(4-{[(4E)-4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]sulfinyl}benzyl)amino]propanoic acid;{3-[(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)amino]propyl}phosphonic acid;3-[(4-{[(4E)-4-(3,5-difluorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)amino]propanoic acid;3-[(4-{[(4E)-4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)amino]propanoic acid;{3-[(4-{[(4E)-4-(3-chlorophenyl)-5-(3,4-dimethylphenyl)pent-4-en-1-yl]oxy}benzyl)amino]propyl}phosphonic acid; and3-[(4-{[(3E)-3-(3-Chlorophenyl)-4-(3,4-dimethylphenyl)but-3-en-1-yl]sulfinyl}benzyl)amino]propanoic acid.14. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.15. The pharmaceutical composition according to claim 14 , wherein the compound is selected from:{3-[(4-{[(5E)-5-(3,5-difluorophenyl)-6-(3,4- ...

HETEROCYCLIC THR-B RECEPTOR AGONIST COMPOUND AND PREPARATION METHOD AND USE THEREFOR

A chemical compound shown in formula (I) below and an isomer thereof or a pharmaceutically acceptable salt thereof. The compound improves THR-β agonistic activity while also improving selectivity for THR-α, thereby improving pharmaceutical quality. 2. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 1 , characterized in that Rand Rare each independently selected from F claim 1 , Cl claim 1 , Br claim 1 , or —CH.3. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 2 , characterized in that Rand Rare both Cl.4. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 2 , characterized in that Rand Rare both —CH.5. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 1 , characterized in that Ris selected from H or —CH.6. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 1 , characterized in that n is 1 or 2.7. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 6 , characterized in that n is 1.8. The compound or a pharmaceutically acceptable salt W isomer thereof as claimed in claim 1 , characterized in that X is —CH—.9. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 1 , characterized in that Y is —O—.10. The compound or an isomer thereof or a pharmaceutically acceptable salt thereof as claimed in claim 1 , characterized in that V is an unsubstituted phenyl group claim 1 , a phenyl group substituted with at least one substituent selected from a halogen atom claim 1 , a trifluoromethyl group claim 1 , a Calkyl group or a Calkoxyl group claim 1 , an unsubstituted five- to six-membered monocyclic heteroaryl group containing 1 or 2 heteroatoms selected from N claim 1 , S or O claim 1 , or a five- to six-membered monocyclic heteroaryl ...

Compositions and methods for using fixed biological samples in partition-based assays

The present disclosure provides compositions and methods for using fixed biological samples in partition-based assays. In at least one embodiment, the disclosure provides a composition comprising a fixed biological sample and an un-fixing agent contained in a partition, such as a discrete droplet. In some embodiments, the disclosure provides un-fixing agent compounds capable of catalytically cleaving crosslinks in fixed biological samples, particularly crosslinked nucleic acids, such as RNA.

PHOSPHONIC ACID COMPOUNDS AS SPHINGOSINE-1-PHOSPHATE RECEPTOR MODULATORS

The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Quinazoline and Indole Compounds to Treat Medical Disorders

Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided. 5. A pharmaceutical composition comprising an effective amount of a compound of and a pharmaceutically acceptable excipient.6. A method for the treatment of a disorder mediated by Complement Factor B claim 1 , comprising administering an effective amount of a compound of to a host in need thereof or its pharmaceutically acceptable salt claim 1 , optionally in a pharmaceutically acceptable carrier.7. The method of claim 6 , wherein the host is a human.8. The method of claim 7 , wherein the disorder is age-related macular degeneration (AMD).9. The method of claim 7 , wherein the disorder is retinal degeneration claim 7 , ophthalmic disease claim 7 , multiple sclerosis claim 7 , arthritis claim 7 , or COPD.10. The method of claim 7 , wherein the disorder is an ophthalmic disease.11. The method of claim 7 , wherein the disorder is paroxysmal nocturnal hemoglobinuria (PNH).12. The method of claim 7 , wherein the disorder is a respiratory disease.13. The method of claim 7 , wherein the disorder is a cardiovascular disease.14. The method of claim 7 , wherein the disorder is atypical or typical hemolytic uremic syndrome.15. The method of claim 7 , wherein the disorder is rheumatoid arthritis.16. The method of claim 7 , wherein the disorder is C3 glomerulonephritis. This application is a continuation of U.S. patent application Ser. No. 16/226,378, filed Dec. 19, 2018, which is a continuation of International Application No. PCT/US2017/039587, filed with the Patent Cooperation Treaty, U.S. Receiving Office on Jun. 27, 2017, which claims the benefit of priority to U.S. Application No. 62/355,273, filed Jun. 27, 2016, and U.S. Application No. 62/471,799 filed Mar. 15, 2017, each of which is incorporated by reference herein for all purposes.The Complement system is a part of the innate immune system that does not adapt to changes over the course of the host's life, but is ...

Stat3 dimerization inhibitors

The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

STAT3 DIMERIZATION INHIBITORS

The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.

CASR AGONISTS

By searching various kinds of compounds having CaSR agonistic activity, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise the compound. More specifically, the present invention provides CaSR agonistic agents, pharmaceutical compositions, preventive or therapeutic agents for diarrhea and kokumi-imparting agents each of which comprise a glutamic acid derivative having CaSR agonistic activity or pharmaceutically acceptable salts thereof. 114-. (canceled)18. The glutamic acid derivative or pharmaceutically acceptable salt thereof according to claim 15 ,{'sub': '2', 'wherein Ris a sulfonic acid group, a carboxylic acid group, or a phosphonic acid group.'}20. The glutamic acid derivative or pharmaceutically acceptable salt thereof according to claim 19 , wherein Ris a halogeno group.21. A pharmaceutical composition comprising the glutamic acid derivative or pharmaceutically acceptable salt thereof according to .22. A pharmaceutical composition comprising the glutamic acid derivative or pharmaceutically acceptable salt thereof according to .23. A method of activating a calcium sensing receptor comprising administering an effective amount of the glutamic acid derivative or pharmaceutically acceptable salt thereof of to a subject.24. A method of imparting kokumi to a food or drink comprising incorporating an effective amount of the glutamic acid derivative or pharmaceutically acceptable salt thereof of into a food or drink.25. The glutamic acid derivative or pharmaceutically acceptable salt thereof of claim 15 , which is N-(5-chloro-2-hydroxy-3-sulfophenyl)-L-glutamine.26. The glutamic acid derivative or pharmaceutically acceptable salt thereof of claim 15 , wherein X is methylene.27. The glutamic acid derivative or pharmaceutically acceptable salt thereof of claim 15 , which is{'sup': '5', 'N-(5-chloro-2-hydroxy-3-sulfophenyl)-L-glutamine,'}{'sup ...

BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS

Compounds that have agonist activity at one or more of the SP receptors are provided. The compounds are sphin-gosine analogs that, after phosphorylation, can behave as agonists at SP receptors. 6. The method of claim 1 , wherein Tis —C(O)(OR) claim 1 , —C(O)N(R)S(OR) claim 1 , —O—P(O)(OR)OR claim 1 , —P(O)(OR) claim 1 , tetrazolyl or —S(O)OR.7. The method of claim 1 , wherein Xis an electron withdrawing group.8. The method of claim 1 , wherein Rand Rare both hydrogen claim 1 , and Ris fluoro claim 1 , chloro claim 1 , bromo claim 1 , iodo claim 1 , methyl claim 1 , trifluoromethyl claim 1 , ethyl claim 1 , propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , i-butyl claim 1 , t-butyl claim 1 , n-pentyl claim 1 , isopentyl claim 1 , 1 claim 1 ,1-dimethylpropyl claim 1 , neopentyl claim 1 , cyclopentyl claim 1 , n-hexyl claim 1 , cyclohexyl claim 1 , methoxy claim 1 , trifluoromethoxy claim 1 , ethoxy claim 1 , n-propoxy claim 1 , i-propoxy claim 1 , n-butoxy claim 1 , i-butoxy claim 1 , t-butoxy claim 1 , n-pentyloxy claim 1 , i-pentyloxy claim 1 , 1 claim 1 ,1-dimethylpropoxy claim 1 , neopentyloxy claim 1 , cyclopentyloxy claim 1 , n-hexyloxy claim 1 , or cyclohexyloxy.11. The method of claim 1 , wherein the compound is selected from the group consisting of:3-((6-(trans-4-tert-butylcyclohexyloxy)naphthalen-2-yl)methylamino)-N-(phenylsulfonyl)propanamide;3-((6-(trans-4-tert-butylcyclohexyloxy)-5-(trifluoromethyl)naphthalen-2-yl)methylamino)-N-(phenylsulfonyl)propanamide;2-((6-(trans-4-tert-butylcyclohexyloxy)naphthalen-2-yl)methylamino)propanoic acid;3-((6-(trans-4-tert-butylcyclohexyloxy)naphthalen-2-yl)methylamino)butanoic acid;2-(((6-(trans-4-tert-butylcyclohexyloxy)naphthalen-2-yl)methyl)(methyl)amino) acetic acid;3-((6-(trans-4-tert-butylcyclohexyloxy)naphthalen-2-yl)methylamino)propanoic acid;3-(((6-(trans-4-tert-butylcyclohexyloxy)naphthalen-2-yl)methyl)(methyl)amino) propanoic acid;1-((6-(trans-4-tert-butylcyclohexyloxy)naphthalen-2-yl)methyl)azetidine-3- ...

BICYCLIC ARYL SPHINGOSINE 1-PHOSPHATE ANALOGS

Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors. 1106-. (canceled)108. The method of claim 107 , wherein Tis —C(O)(OR) claim 107 , —C(O)N(R)S(OR) claim 107 , —O—P(O)(OR)OR claim 107 , —P(O)(OR) claim 107 , tetrazolyl or —S(O)OR.109. The method of claim 107 , wherein Rand Rare both hydrogen claim 107 , and Ris fluoro claim 107 , chloro claim 107 , bromo claim 107 , iodo claim 107 , methyl claim 107 , trifluoromethyl claim 107 , ethyl claim 107 , propyl claim 107 , isopropyl claim 107 , n-butyl claim 107 , i-butyl claim 107 , t-butyl claim 107 , n-pentyl claim 107 , isopentyl claim 107 , 1 claim 107 ,1-dimethylpropyl claim 107 , neopentyl claim 107 , cyclopentyl claim 107 , n-hexyl claim 107 , cyclohexyl claim 107 , methoxy claim 107 , trifluoromethoxy claim 107 , ethoxy claim 107 , n-propoxy claim 107 , i-propoxy claim 107 , n-butoxy claim 107 , i-butoxy claim 107 , t-butoxy claim 107 , n-pentyloxy claim 107 , i-pentyloxy claim 107 , 1 claim 107 ,1-dimethylpropoxy claim 107 , neopentyloxy claim 107 , cyclopentyloxy claim 107 , n-hexyloxy claim 107 , or cyclohexyloxy.112. The method of claim 107 , further comprising administering to said mammal an effective amount of one or more drugs selected from the group consisting of: a corticosteroid claim 107 , a bronchodilator claim 107 , an antiasthmatic claim 107 , an antiinflammatory claim 107 , an antirheumatic claim 107 , an immunosuppressant claim 107 , an antimetabolite claim 107 , an immunomodulator claim 107 , an antipsoriatic claim 107 , and an antidiabetic.114. The method of claim 113 , wherein Tis —C(O)(OR) claim 113 , —C(O)N(R)S(OR) claim 113 , —O—P(O)(OR)OR claim 113 , —P(O)(OR) claim 113 , tetrazolyl or —S(O)OR.115. The method of claim 113 , wherein Rand Rare both hydrogen claim 113 , and Ris fluoro claim 113 , chloro claim 113 , bromo claim 113 , iodo claim 113 , ...

METHOD FOR PRODUCING PHENYLPHOSPHONIC ACID METAL SALT COMPOSITION, AND CRYSTAL NUCLEATING AGENT THEREFROM

A method for producing a phenylphosphonic acid metal salt composition, including reacting a phenylphosphonic acid compound (a) with a metal salt, metal oxide or metal hydroxide (b) that is present in an amount beyond the equivalent, the phenylphosphonic acid metal salt composition containing phenylphosphonic acid metal salt, and a surplus amount of the metal salt, the metal oxide or the surplus metal hydroxide (b). A crystal nucleating agent comprises the phenylphosphonic acid metal salt composition produced by the method. 2. The method according to claim 1 , wherein the reaction of the phenylphosphonic acid compound (a) with the metal salt claim 1 , metal oxide or metal hydroxide (b) is carried out in the presence of particles of the metal salt claim 1 , metal oxide or metal hydroxide (b).3. The method according to claim 1 , wherein the reaction of the phenylphosphonic acid compound (a) with the metal salt claim 1 , metal oxide or metal hydroxide (b) is carried out in a solvent that hardly dissolves the metal salt claim 1 , metal oxide or metal hydroxide (b).4. The method according to claim 1 , wherein the reaction of the phenylphosphonic acid compound (a) with the metal salt claim 1 , metal oxide or metal hydroxide (b) is carried out in a molar ratio of (b):(a) of 100:0.01 to 100:90.5. The method according to claim 1 , wherein the metal of the metal salt claim 1 , metal oxide or metal hydroxide (b) is zinc claim 1 , calcium or manganese.6. The method according to claim 5 , wherein the metal of the metal salt claim 5 , metal oxide or metal hydroxide (b) is zinc or calcium.7. The method according to claim 6 , wherein the metal salt claim 6 , metal oxide or metal hydroxide (b) is zinc oxide or calcium carbonate.8. The method according to claim 1 , wherein a molar ratio of the metal salt claim 1 , metal oxide or metal hydroxide (b) to the phenylphosphonic acid compound (a) for the reaction is from 100:0.01 to 100:30.9. The method according to claim 1 , wherein a molar ...

STAT3 DIMERIZATION INHIBITORS

The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein. 2. The compound of claim 1 , wherein Ris H claim 1 , C-Calkyl claim 1 , C(O)C-Calkyl claim 1 , COC-Calkyl claim 1 , benzyl claim 1 , 4-piperidyl claim 1 , 3-(4-pyridyl) claim 1 , or pyridinyl.5. The compound of claim 4 , wherein Ris cyclohexyl.6. The compound of claim 1 , wherein Ris OH claim 1 , Cl claim 1 , F claim 1 , Br claim 1 , I claim 1 , OCH claim 1 , C-Calkyl claim 1 , 4-piperidyl claim 1 , 3-(4-pyridyl) claim 1 , morpholinyl claim 1 , phenyl claim 1 , or pyridinyl.8. The compound of claim 7 , wherein X is O.9. The compound of claim 1 , wherein Ris OPh.10. The compound of claim 1 , wherein Ris H or OCH.11. The compound of claim 1 , wherein the compound has a formula shown in Table 3.14. The compound of claim 13 , wherein Ris H claim 13 , C-Calkyl claim 13 , C(O)C-Calkyl claim 13 , COC-Calkyl claim 13 , benzyl claim 13 , 4-piperidyl claim 13 , 3-(4-pyridyl) claim 13 , or pyridinyl.17. The compound of claim 16 , wherein Ris cyclohexyl.18. The compound of claim 13 , wherein Ris OH claim 13 , Cl claim 13 , F claim 13 , Br claim 13 , I claim 13 , OCH claim 13 , C-Calkyl claim 13 , 4-piperidyl claim 13 , 3-(4-pyridyl) claim 13 , morpholinyl claim 13 , phenyl claim 13 , or pyridinyl.20. The compound of claim 19 , wherein X is O.21. The compound of claim 13 , wherein Ris OPh.22. The compound of claim 13 , wherein Ris H or OCH.23. The compound ...

INFRARED-ABSORBING COMPOSITION, INFRARED-CUT FILTER, AND IMAGING OPTICAL SYSTEM

An infrared-absorbing composition according to the present invention includes: an infrared absorber formed by a phosphonic acid represented by the following formula (a) and copper ion; and a phosphoric acid ester allowing the infrared absorber to be dispersed. The phosphoric acid ester includes at least one of a phosphoric acid diester and a phosphoric acid monoester. Ris a phenyl group or a phenyl group in which at least one hydrogen atom is substituted by a halogen atom. When molar contents of the phosphonic acid, the copper ion, and the phosphoric acid ester are respectively defined as Cmol, Cmol, and Cmol and a total molar content of reactive hydroxy groups is defined as Cmol, the relations C/C<1 and C/C>1.95 are satisfied. 3. The infrared-absorbing composition according to claim 1 , wherein the relation 0.20≤C/C≤0.85 is satisfied.4. The infrared-absorbing composition according to claim 1 , wherein the relation C/C≥2.842-0.765×C/Cis satisfied.5. The infrared-absorbing composition according to claim 1 , further comprising a matrix component.6. The infrared-absorbing composition according to claim 5 , wherein the matrix component is a polysiloxane.7. An infrared-cut filter comprising:a transparent dielectric substrate; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an infrared-absorbing layer provided on at least one principal surface of the transparent dielectric substrate and formed by the infrared-absorbing composition according to .'}8. An imaging optical system comprising the infrared-cut filter according to . The present invention relates to an infrared-absorbing composition, an infrared-cut filter, and an imaging optical system.In imaging apparatuses such as digital cameras, silicon (Si)-based two-dimensional image sensors such as a charge coupled device (CCD) and a complementary metal oxide semiconductor (CMOS) are used as imaging sensors. Such a Si-based imaging sensor is sensitive to light of wavelengths in the infrared region and has wavelength ...

COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract. 136-. (canceled)38. (canceled)39. (canceled) ...

MODIFIED GRAPHENE, METHOD OF PRODUCING MODIFIED GRAPHENE, MODIFIED GRAPHENE-RESIN COMPOSITE, MODIFIED GRAPHENE SHEET, AND MODIFIED GRAPHENE DISPERSION

The modified graphene includes a structure represented by the following formula (I), wherein the modified graphene has a ratio (g/d) of an intensity “g” of a G band to an intensity “d” of a D band of 1.0 or more in a Raman spectroscopy spectrum thereof: 2. The modified graphene according to claim 1 , wherein in the formula (I) claim 1 , the Ar1 represents a phenylene group claim 1 , a biphenylene group claim 1 , a triphenylene group claim 1 , or a naphthalene group claim 1 , the X1 represents a single bond claim 1 , the Y1 represents a carboxylic acid group claim 1 , and the n1 represents from 1 to 6.4. The modified graphene according to claim 1 , wherein in the formula (I) claim 1 , the Ar1 represents a phenylene group claim 1 , the X1 represents a single bond claim 1 , the Y1 represents a nitro group claim 1 , and the n1 represents from 1 to 3.7. The modified graphene according to claim 1 , wherein when the Y1 in the formula (I) represents a group claim 1 , a number of moles of the group with respect to 1 g of the modified graphene is 0.10 mmol or more.8. The modified graphene according to claim 7 , wherein when the Y1 in the formula (I) represents a group claim 7 , the number of moles of the group with respect to 1 g of the modified graphene is 0.10 mmol or more and 1.20 mmol or less.10. The method of producing a modified graphene according to claim 9 , further comprising producing the compound represented by the formula (V) through abstraction of a hydrogen atom from a compound represented by the following formula (VI):{'br': None, 'sub': '2', 'HN—NH-A1\u2003\u2003(VI)'}in the formula (VI), A1 is the same as the A1 in the formula (V).11. The method of producing a modified graphene according to claim 10 , further comprising producing the compound represented by the formula (V) through use of at least one ofa compound in which in the A1, the Ar1 represents a phenylene group, the X1 represents a single bond, and the Y1 represents a carboxylic acid group, ora ...

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. 2. The compound of which is a compound of formula I claim 1 , or a salt thereof.3. The compound of which is a compound of formula II claim 1 , or a salt thereof.4. The compound of wherein Ris an unsaturated (C-C)alkyl chain.5. The compound of wherein X is —(CH)- or —(CH)CH(CH)- and m is an integer from 1 to 2.6. The compound of wherein Ris an unsaturated (C-C)alkyl chain.8. The compound of wherein Ris a saturated or unsaturated (C-C)alkyl chain that comprises one or more aryl rings in the chain.10. The compound of wherein Ris a unsaturated (C-C)alkyl chain that comprises a heteroaryl ring in the chain.11. The compound of wherein the heteroaryl ring is indolyl.1312. The compound of any one of - wherein Ris H or methyl.14. The compound of wherein Ris methyl.15. The compound of wherein X is —(CH)- or —(CH)CH(CH)- and m is 1.16. The compound of wherein X is —(CH)- or —(CH)CH(CH)- and m is 2.1714. The compound of any of - wherein Ris a saturated or unsaturated (C-C)alkyl chain.1914. The compound of any of - wherein Ris a saturated or unsaturated (C-C)alkyl chain that comprises one or more aryl or heteroaryl rings in the chain.21. The compound of wherein Y is —(CH)- or —(CH)CH(CH)- and n is an integer from 1 to 2.22. The compound of wherein Ris a saturated or unsaturated (C-C)alkyl chain that is optionally substituted with one or more halo claim 3 , cyano claim 3 , nitro claim 3 , carboxy claim 3 , trifluoromethyl claim 3 , trifluoromethoxy claim 3 , aryl claim 3 , heteroaryl claim 3 , NRR claim 3 , or S(O)NRR.23. The compound of wherein Ris an unsaturated (C-C)alkyl chain that is optionally substituted with one or more halo claim 3 , cyano claim 3 , nitro claim 3 , carboxy claim 3 , trifluoromethyl claim 3 , trifluoromethoxy claim 3 , aryl claim 3 , heteroaryl claim ...

ELECTRONIC SWITCHING ELEMENT

An electronic switching element () which comprises, in this sequence, a first electrode (), a molecular layer () bonded to a substrate, and a second electrode (), where the molecular layer essentially consists of compounds of the formula I indicated in claim in which a mesogenic radical is bonded to the substrate via a spacer group (Sp) by means of an anchor group (G), is suitable for the production of components () as memristive device for digital information storage. 2120. Electronic switching element () according to claim 1 , characterised in that the first electrode () represents the substrate for the molecular layer.3122182018. Electronic switching element () according to claim 1 , characterised in that a diode () claim 1 , which represents the substrate for the molecular layer () claim 1 , is arranged between the first electrode () and the molecular layer ().41222426242620. Electronic switching element () according to claim 3 , characterised in that the diode () comprises an n+-doped layer () and a p+-doped layer () claim 3 , where the n+-doped layer () or the p+-doped layer () is designed as a combined electrode together with a semiconducting first electrode ().51221618. Electronic switching element () according to claim 1 , characterised in that a diode () is arranged between the second electrode () and the molecular layer ().611818. Electronic element () according to claim 1 , characterised in that an interlayer is arranged between the substrate and the molecular layer () claim 1 , where the interlayer is selected from an oxidic or fluoridic material and in that the molecular layer () is bonded to this oxidic or fluoridic interlayer.71. Electronic switching element () according to claim 6 , characterised in that the oxidic or fluoridic interlayer is formed from TiO claim 6 , AlO claim 6 , HfO claim 6 , SiOor LiF.81. Electronic switching element () according to claim 6 , characterised in that the anchor group (G) of the compounds of the formula I claim 6 , ...

SELF-ASSEMBLED MONOLAYERS OF PHOSPHONIC ACIDS AS DIELECTRIC SURFACES FOR HIGH-PERFORMANCE ORGANIC THIN FILM TRANSISTORS

Cycloalkylalkylphosphonic acids are presented that are useful for forming a self-assembled monolayer (SAM) on a surface of a metal oxide layer. The combined SAM and metal oxide layer form the dielectric layer of an organic thin film transistor (OTFT). The OTFT can be formed with p-type and n-type organic semiconductor layers on the SAM. The OTFT display superior field effect mobilities and air stabilities to other SAMs and the SAMS of cycloalkylalkylphosphonic acids allow deposition of the organic semiconductors by either vapor deposition or solution processing techniques. 2. The cycloalkylalkylphosphonic acid or dialkyl cycloalkylalkylphosphonate ester according to claim 1 , wherein the cycloalkylalkylphosphonic acid is 12-cyclohexyldodecylphosphonic acid (CDPA).3. The cycloalkylalkylphosphonic acid or dialkyl cycloalkylalkylphosphonate ester according to claim 1 , wherein the dialkyl cycloalkylalkylphosphonate ester is diethyl-12-cyclohexyldodecylphosphonate.4. A method of preparing a cycloalkylalkylphosphonic acid claim 1 , according to claim 1 , comprising:providing a halogen substituted cycloalkane;forming a cycloalkylmagnesium halide from the halogen substituted cycloalkane;combining the cycloalkylmagnesium halide with an α,ω-dihalogen substituted n-alkane to form an α-halo-ω-cycloalkylalkane;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'combining the α-halo-ω-cycloalkylalkane with a trialkyl phosphite to form a dialkyl cycloalkylalkylphosphonate ester, according to ;'}combining the dialkyl cycloalkylalkylphosphonate ester with trimethylsilicon bromide in a first step and with water in a second step to form a cycloalkylalkylphosphonic acid; wherein the cycloalkane is cyclopentane, cyclohexane, cycloheptane, or cyclooctane; wherein the halogen and dihalogen are independently Cl, Br, or I; wherein the n-alkane is n-hexane, n-heptane, n-octane, n-nonane, n-decane, n-undecane, n-dodecane, n-tridecane, n-tetradecane, n-pentadecane, n-hexadecane, n-heptadecane, ...

LIGHT-ABSORBING COMPOSITION AND OPTICAL FILTER

A light-absorbing composition according to the present invention includes: a light absorber formed by a phosphonic acid represented by the following formula (a) and copper ion, the light absorber being dispersed in the light-absorbing composition; a phosphoric acid ester allowing the light absorber to be dispersed; and a curable resin. When the light-absorbing composition is applied and cured on one principal surface of a transparent dielectric substrate to form a laminate consisting of a light-absorbing layer being a cured product of the light-absorbing composition and the transparent dielectric substrate, the laminate satisfies predetermined requirements. 2. The light-absorbing composition according to claim 1 , wherein the ratio of the content of the phosphonic acid to the content of the phosphoric acid ester is 0.10 to 0.48 on a mass basis claim 1 , and the ratio of the content of the phosphonic acid to the content of the copper ion is 0.45 to 0.80 on an amount-of-substance basis.5. The optical filter according to claim 4 , wherein in the light-absorbing layer claim 4 , the ratio of the content of the phosphonic acid to the content of the phosphoric acid ester is 0.10 to 0.48 on a mass basis claim 4 , and the ratio of the content of the phosphonic acid to the content of the copper ion is 0.45 to 0.80 on an amount-of-substance basis.7. The optical filter according to claim 4 , wherein the light-absorbing layer has a thickness of 30 μm to 800 μm.8. The optical filter according to claim 4 , further comprising an infrared-reflecting film formed by alternating layers of different materials having different refractive indices. The present invention relates to a light-absorbing composition and an optical filter.In imaging apparatuses employing an imaging sensor such as a charge coupled device (CCD) or a complementary metal oxide semiconductor (CMOS), any of various optical filters is disposed ahead of the imaging sensor in order to obtain an image with good color ...

PROCESS FOR SYNTHESIZING AZO COMPOUNDS

A process for synthesizing an azo compound by oxidation of a hydrogen compound in the presence of a catalyst and a compound of formula (I) is described in which R, Rand R 1. A process for synthesizing an azo compound , said process comprising the steps of: {'br': None, 'sub': 1', '2', '3', '3', '2', '2, '(R)(R)C(PO(R))\u2003\u2003(I)'}, 'a) reacting an oxidizing agent with a hydrazo compound, at least one catalyst and at least one compound of formula (I)wherein{'sub': 1', '2, 'Rand R, which may be identical or different, are chosen independently of each other from a hydrogen atom, a saturated or unsaturated, linear, branched or cyclic, optionally substituted hydrocarbon chain, —OH and —O-alkyl, where “alkyl” represents a saturated, optionally substituted, linear or branched hydrocarbon chain comprising from 1 to 6 carbon atoms; and'}{'sub': '3', 'Ris chosen from a hydrogen atom and metal or ammonium ions;'}so as to form a solution containing an azo compound;b) recovering all or part of the reaction mixture obtained in step a);c) separating the reaction mixture recovered into a fraction containing the azo compound and a fraction of residual aqueous liquors; andd) recovering, and optionally washing and drying, the azo compound obtained.2. The process as claimed in claim 1 , wherein the compound of formula (I) is chosen from [1-hydroxy-1-(H-imidazol-1-yl)ethane-1 claim 1 ,1-diyl]diphosphonic acid or one of its salts claim 1 , hydroxymethylenediphosphonic acid claim 1 , 1-hydroxylethylidene-1 claim 1 ,1-diphosphonic acid (HEDP) and 1-hydroxybutanediphosphonic acid claim 1 , in their acid form or in the form of their salts.3. The process as claimed in claim 1 , wherein the hydrazo compound is chosen from symmetrical hydrazo compounds bearing nitrogen-based functional groups.4. The process as claimed in claim 1 , wherein the oxidizing agent is chosen from inorganic peroxide derivatives.5. The process as claimed in claim 1 , wherein the catalyst comprises a water-soluble ...

Electronic switching element

The invention relates to an electronic switching element (1), which comprises in this order a first electrode (16), a molecular layer (18), which is bonded to a substrate, and a second electrode (20), wherein the molecular layer essentially consists of compounds of formula (I) indicated in claim 1, wherein a mesogenic group is bonded to the substrate via a spacer group (Sp) by means of an anchor group (G). The electronic switching element is suitable for the production of components (1) as a memristive device for digital information storage.

Phosphonate linkers and their use to facilitate cellular retention of compounds

Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitates cellular retention of the compound are described.

Phosphonate linkers and their use to facilitate cellular retention of compounds

Phosphonate linkers and their use for delivering compounds with passive cell permeability into a cell wherein the phosphonate group facilitateS cellular retention of the compound are described.

ANTIBACTERIAL COMPOSITIONS BASED ON CHLORESIDINE FOR DERMATOLOGICAL USE AND PROCEDURE FOR THEIR PREPARATION.

NOVEL AMINOPHENYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION PROCESS AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Способ получени производных дифосфоновой кислоты или их натриевых солей

Изобретение касаетс  фосфорорганических веществ, в частности получени  производных диофосфоновой кислоты общей формулы 1 HET-A-C[OH][P(O)(OH) 2 ] 2 , где HET = пиридил, 1,2,4-триазолил, имидазолил [он может быть замещен бензилом], 1,2,3-триазолил [он может быть замещен бензилом, 4-метилбензилом или 4-аминометилбензилом] A-H- или изонасыщенна  C 2 -4 -цепь, или их натриевых солей, которые оказывают вли ние на кальциевый обмен и могут быть использованы в медицине. Цель изобретени  - создание новых более активных соединений указанного класса. Синтез целевых соединений ведут реакцией карбоновой кислоты общей формулы п: HET-A-C[O]OH, где HET и A (см.выше) подвергают взаимодействию с фосфористой кислотой и треххлористым фосфором в среде хлорбензола при нагревании с последующим гидролизом сол ной кислотой при нагревании и выделением целевого прдукта в виде свободного производного дифосфоновой кислоты или ее соли. Новые соединени  снижают гиперкальцеамию в дозе 0,1-1,0 мг/кг и имеют низкую токсичность [против 10 мг] кг дл  1-оксиэтан-1,1- дифосфоновой кислоты] 1 табл.

Preparation of layered zirconium phosphite sulfophenylphosphonates and their use as a catalyst

The present invention provides zirconium phosphite sulfophenylphosphonates having the following formula Zr(HPO.sub.3).sub.m (HPO.sub.4).sub.n (PO.sub.3 C.sub.6 H.sub.5).sub.y (PO 3 C 6 H 4 SO 3 H) z wherein m+n=x; x+y+z=2; 0.4≦x≦1.7; 0≦y≦1.6; and 0.01≦z≦0.8. The present invention also discloses a method of preparing these zirconium phosphite sulfophenylphosphonates and their use as a catalyst.

Novel fused pyrimidine derivatives for inhibition of tyrosine kinase activity

FIELD: chemistry. SUBSTANCE: present invention relates to a novel fused pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof, having Bruton's tyrosine kinase inhibitory activity (ECT). Compounds can be used for preparing a drug for preventing or treating Bruton's tyrosine kinase mediated cancers and tumours, such as leukaemia, lymphoma, B-cell lymphoma, T-cell lymphoma, myeloma, acute lymphoid leukaemia (ALL), chronic lymphoid leukaemia (CLL), etc; inflammatory diseases, such as arthritis, rheumatoid arthritis, spondyloarthropathy, gouty arthritis, osteoarthritis, Still's disease, other arthritic conditions, lupus, etc; autoimmune diseases and immunologically mediated diseases, including Sjorgen's syndrome, autoimmune thyroiditis, hives, multiple sclerosis, sclerodermatitis, rejection of transplanted organs, heterotransplantation, idiopathic thrombocytopenic purpura (ITP), Parkinson's disease, Alzheimer's disease, associated with diabetes disease, pelvic inflammation, allergic rhinitis, allergic bronchitis, Hodgkin disease, non-Hodgkins lymphoma, multiple myeloma, myelodysplastic syndrome (MDS), myeloproliferative neoplasms (MPN), diffuse large B-cell lymphoma, follicular lymphoma, etc. In compounds of formula (I) . W is O; X is NH, O, SO or SO 2 ; Y denotes a hydrogen atom, halogen atom, C 1-6 alkyl or C 1-6 alkoxy, each of A and B independently denotes a hydrogen atom, halogen atom or di(C 1-6 alkyl)aminomethyl; Z is selected from a group consisting of formulae Z2, Z4, Z28, Z61, Z100, Z113, Z138, Z164, Z168 and Z189 . EFFECT: treating different diseases. 10 cl, 3 dwg, 19 tbl, 237 ex

FIRE RESISTANT FOAMING POLYMERS

1. Огнестойкие вспениваемые полимеры, содержащие по меньшей мере один агент вспенивания, отличающиеся тем, что они содержат в качестве огнезащитного средства по меньшей мере одно из следующих фосфорсодержащих соединений:- фосфорсодержащее соединение формулы ((Ia):10-гидрокси-9,10-дигидро-9-окса-10-фосфафенантрен-10-окид (DOPO-OH)- или его соли формулы (Ib):- или его гидролизаты формулы (Ic), имеющие открытое кольцо:.2. Вспениваемые полимеры по п.1, отличающиеся тем, что остаток Rпредставляет собой органический или неорганический катион.3. Вспениваемые полимеры по п.1 или 2, отличающиеся тем, что остаток Rпредставляет собой соль четвертичного аммониевого соединенияили четвертичного фосфониевого соединения4. Вспениваемые полимеры по п.1 или 2, отличающиеся тем, что в общей формуле (Ib) или (Ic) остаток Rпредставляет собой, а фосфорсодержащее соединение представляет собой соль аммония 10-гидрокси-9,10-дигидро-9-окса-10-фосфафенантрен-10-оксида:5. Вспениваемые полимеры по п.1 или 2, отличающиеся тем, что в общей формуле (Ib) или (Ic) остаток Rпредставляет собой гуанидин, а фосфорсодержащее соединение представляет собой соль гуанидина 10-гидрокси-9,10-дигидро-9-окса-10-фосфафенантрен-10-оксида:6. Вспениваемые полимеры по п.1 или 2, отличающиеся тем, что в общей формуле (Ib) или (Ic) остаток Rпредставляет собой меламин, а фосфорсодержащее соединение представляет собой соль меламина 10-гидрокси-9,10-дигидро-9-окса-10-фосфафенантрен-10-оксида:7. Вспениваемые полимеры по п.1, отличающиеся тем, что фосфорсодержащее соединение(я) содержится(атся) в количестве от 0,5 до 25 вес.%, в частности, от 1 до 15 вес.%, от общего веса полимера.8. Вспениваемые полимеры по п.1, отличающиеся тем, что о РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C08J 9/00 (13) 2013 151 091 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013151091/04, 17.04.2012 (71) Заявитель(и): СУНПОР КУНСТШТОФ ГЕЗЕЛЬШАФТ М.Б.Х. (AT) Приоритет(ы): (30) ...

Electronics switching element

电子切换元件(1)，其按此顺序包含第一电极(20)，结合至基板的分子层(18)，和第二电极(16)，其中分子层基本上由权利要求1中所示的式I化合物组成，其中介晶基团是经由间隔基团(Sp)通过锚定基团(G)结合至基板，所述电子切换元件(1)适于生产作为用于数字信息存储的忆阻器件的组件(1)。

Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.

Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract

Combinations for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders

The present disclosure is directed to a pharmaceutical composition comprising a compound of formula (X), in combination with another active agent, and to the use of said composition in methods for the treatment of disorders associated with fluid retention or salt overload or gastrointestinal tract disorders, such as irritable bowel syndrome and constipation associated with cystic fibrosis. The methods generally comprise administering to a mammal in need thereof a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto.

Compounds and methods for inhibiting NHE-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract.

ALKINIC AND ALKENE DERIVATIVES AS MODULATORS OF THE RECEPTOR OF SINGINGIN-1-PHOSPHATE-1

1. Соединение, имеющее Формулу I, его энантиомеры, диастереоизомеры, гидраты, сольваты, кристаллические формы и индивидуальные изомеры, таутомеры или их фармацевтически приемлемые соли,где:«» представляет двойную связь «-CR=CR-» или тройную связь «-C≡C-»;A является Cарилом, гетероциклом, Cциклоалкилом или Cциклоалкенилом;B является Cарилом, гетероциклом, Cциклоалкилом или Cциклоалкенилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется H, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, Cарилом, гетероциклом, Cциклоалкилом, Cциклоалкенилом, NRRили гидроксилом;Rодинаково или независимо является галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Lявляется O, S, NH или CH;Rявляется H или Cалкилом;Lявляется CHRили O;Rявляется H, OPOH, карбоновой кислотой, гидроксилом, POH, -S(O)H, -P(O)MeOH или -P(O)(H)OH;Rявляется H или Cалкилом;a равен 0, 1, 2 или 3;b равен 0 или 1;Rявляется H или Cалкилом;Rявляется H или Cалкилом;Rявляется H, гидроксилом или Cалкилом;Rявляется H или Cалкилом;Rявляется O, S, C(O) или CH; иc равен 0 или 1;при условии, что соединение Формулы I не имеет структуру.2. Соединение по п.1, отличающееся тем, что:«» представляет двойную связь «-CR=CR-».3. Соединение по п.1, отличающееся тем, что:«» представляет тройную связь «-C≡C-».4. Соединение по п.1, отличающееся тем, что:Lявляется CH.5. Соединение по п.1, отличающееся тем, что:Lявляется O, S � РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 43/23 (13) 2013 129 484 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013129484/04, 28. ...

Novel fused pyrimidine derivatives for inhibition of tyrosine kinase activity

Настоящее изобретение относится к новому конденсированному пиримидиновому производному формулы (I) или его фармацевтически приемлемой соли. Соединения могут найти применение для получения лекарственного средства для профилактики или лечения раков, опухолей, воспалительных заболеваний, опосредованных по меньшей мере одной киназой, выбранной из группы, состоящей из тирозинкиназы Брутона (BTK), Janus киназы 3 (JAK3), индуцируемой интерлейкином-2 Т-клеточной киназы (ITK), киназы покоящихся лимфоцитов (RLK) и тирозинкиназы костного мозга (ВМХ). В соединении формулы (I) W представляет собой S; X представляет собой О, NH, S, SO или SO 2 ; Y представляет собой атом водорода, атом галогена, С 1-6 алкил или С 1-6 алкокси; каждый из А и В независимо представляет собой атом водорода, атом галогена или ди(С 1-6 алкил)аминометил; где необязательно С 1-6 алкил является частично ненасыщенным или содержит С 3-6 циклоалкильный фрагмент, Z выбирают из группы, состоящей из формул Z1-Z203. Формулы Z1-Z203 указаны в пункте 1 формулы изобретения. 6 н. и 12 з.п. ф-лы, 3 ил., 19 табл., 247 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: (19) RU (51) МПК C07D 495/04 A61K 31/519 A61P 35/00 A61P 29/00 A61P 25/28 A61P 17/00 A61P 19/02 (13) 2 585 177 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2013102881/04, 20.06.2011 (24) Дата начала отсчета срока действия патента: 20.06.2011 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 27.07.2014 Бюл. № 21 (45) Опубликовано: 27.05.2016 Бюл. № 15 (56) Список документов, цитированных в отчете о поиске: WO 9802438 A1, 22.01.1998. SHOWALTER; HOLLIS H D; ET AL., Tyrosine (73) Патентообладатель(и): ХАНМИ САЙЕНС КО., ЛТД. (KR) Kinase Inhibitors. 16. 6,5,6-Tricyclic Benzothieno [3,2-d]pyrimidines and Pyrimido[5,4-b]- and -[4,5b]indoles as Potent Inhibitors of the Epidermal Growth Factor Receptor Tyrosine Kinase, J. Med. Chem., ...

Substituted cyclohexane derivatives for treating diseases

본 발명은 포유동물에서 간의 글루즈-6-포스파타제 시스템의 억제제로서 사용하기 위한 다음 일반식(Ⅰ)의 사이클로 헥산 유도체의 에스테르에 관한 것이다. 상기식에서, A-B, R 3 ,R 4 ,R 5 ,Y및 Z는 명세서에서 정의한 바와 같다. 당해 화합물은 약제학적 제제를 제조하는데 적합하다.

NEW OXIME DERIVATIVES AS MODULATORS OF THE RECEPTOR OF SINGINGIN-1-PHOSPHATE (S1P)

1. Соединение, имеющее Формулу I, его энантиомеры, диастереоизомеры, гидраты, сольваты, кристаллические формы и индивидуальные изомеры, таутомеры или их фармацевтически приемлемые соли,где:А является Сарилом, гетероциклом, Сциклоалкилом или Сциклоалкенилом;В является Сарилом, гетероциклом, Сциклоалкилом или Сциклоалкенилом;Rявляется Н, галогеном, -ОСалкилом, Салкилом, CN, C(O)R, NRRили гидроксилом;Rявляется Н, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется Н, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется Н, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется Н, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется Н, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется Н, галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Rявляется галогеном, -OCалкилом, Cалкилом, CN, C(O)R, NRRили гидроксилом;Lявляется О, С(O), S, NH или СН;Rявляется О, S или СН;Rявляется Н или Cалкилом;Lявляется CHR, О, S, NRили -С(O)-;D является группой формулыили,указывает точку присоединения к остальной части молекулы;Rявляется Н, ОРОН, карбоновой кислотой, РОН, Салкилом, -S(O)H, -Р(O)МеОН, -Р(O)(Н)ОН или OR;Rявляется Н или Cалкилом;а равен 0, 1 или 2;b равен 0 или 1;с равен 0, 1, 2 или 3;Rявляется Н, Cалкилом;Rявляется Н или Cалкилом; иRявляется Н или Cалкилом;Rявляется Н, ОН или Cалкилом; иRявляется Н или Cалкилом.2. Соединение по п.1, отличающееся тем, что Lявляется О.3. Соединение по п.1, отличающееся тем, что Lявляется S.4. Соединение по п.1, отличающееся тем, что Lявляется СН.5. Соединение по п.1, отличающееся тем, чтоD является группой формулы,указывает точку присоединения к остальной части молекулы.6. Соединение по п.1, отличающееся тем, ч� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2013 130 027 A (51) МПК A61K 31/197 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013130027/04, 18.11.2011 (71) Заявитель(и): ...

Process for producing 2-substituted-1,3-propylidenedipho sphonate derivatives

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Novel bisphosphonic acid compound

FIELD: medicine; pharmaceuticals. SUBSTANCE: invention relates to a bisphosphonic acid compound represented by following formula (1) or a pharmaceutically acceptable salt thereof: . In formula (1): ------ is a single bond or double bond, A is a saturated cyclic hydrocarbon C3–8 (saturated cyclic hydrocarbon is optionally substituted with 1–4 groups selected from a group consisting of a C1–6-alkyl group, C6–10-aryloxy groups and halogen atoms), R 1 and R 2 each independently represent a C1–6-alkyl group, a halogen atom or a hydrogen atom. Also disclosed is a pharmaceutical composition, a preventive or therapeutic drug for treating a disease associated with ectopic calcification, use of the compound of formula (1) and a method for preventing or treating a disease associated with ectopic calcification. EFFECT: disclosed compound of the present invention or salt thereof excellently inhibits ectopic calcification. 7 cl, 7 tbl, 62 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 731 615 C2 (51) МПК C07F 9/38 (2006.01) A61K 31/663 (2006.01) A61P 9/00 (2006.01) A61P 9/10 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК A61K 31/663 (2020.02); A61P 9/00 (2020.02); C07F 9/38 (2020.02) (21)(22) Заявка: 2018130994, 27.01.2017 (24) Дата начала отсчета срока действия патента: Дата регистрации: 07.09.2020 29.01.2016 JP 2016-027405 (43) Дата публикации заявки: 03.03.2020 Бюл. № 7 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 29.08.2018 (86) Заявка PCT: JP 2017/002855 (27.01.2017) (87) Публикация заявки PCT: R U 2 7 3 1 6 1 5 WO 2017/131127 (03.08.2017) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (54) НОВОЕ СОЕДИНЕНИЕ БИСФОСФОНОВОЙ КИСЛОТЫ (57) Реферат: Изобретение относится к соединению одинарную связь или двойную связь, А бисфосфоновой кислоты, представленному представляет собой насыщенный циклический следующей формулой (1) или его ...

Bisphosphonate squalene synthetase inhibitors and method

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 1 , R 2 , R 3 and R 4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester; R 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.

Light-emitting material for organic electroluminescent device, organic electroluminescent device using same, and material for organic electroluminescent device

Disclosed are a fused compound having excellent emission wavelength control and luminous efficiency, a method for manufacturing the same, and an organic electronic device including the fused compound. According to the present invention, the performance of a structure is excellent.

Method for preparing a solution of a rare-earth organophosphate in an organic solvent

本发明的稀土有机磷酸盐在有机溶剂中的溶液的制备方法在于，在选自水、硝酸、盐酸、乙酸、甲酸和丙酸以及这些酸的稀土盐的促进剂存在下，在该溶剂中使选自稀土的氧化物、氢氧化物、碳酸盐和羟基碳酸盐的稀土化合物与有机含磷酸反应。促进剂的使用使得可以简化该方法、降低反应时间并获得残余固体含量可以低的溶液。

CaSR agonist

CaSR 효능제 활성을 가지는 많은 다양한 화합물을 탐색하고, 당해 화합물을 함유하는 CaSR 효능제, 의약 조성물, 설사 예방 또는 치료제 및 코쿠미 부여제를 제공한다. CaSR 효능제 활성을 갖는 글루탐산 유도체 또는 이의 약제학적으로 허용되는 염을 함유하는 것을 특징으로 하는 CaSR 효능제, 의약 조성물, 설사 예방 또는 치료제 및 코쿠미 부여제를 제공한다. A large number of compounds having CaSR agonist activity are searched and a CaSR agonist, a pharmaceutical composition, a diarrhea preventive or therapeutic agent, and a kokumi agent containing the compound are provided. A CaSR agonist, a pharmaceutical composition, a diarrhea preventive or therapeutic agent, and a kokumi agent, characterized by containing a glutamate derivative having CaSR agonist activity or a pharmaceutically acceptable salt thereof.

SUBSTITUTED Bicyclic Methylamine derivatives as Modulators of sphingosine-1-phosphate receptors

1. Соединение формулы I, его отдельные энантиомеры, отдельные диастереоизомеры и отдельные изомеры, отдельные таутомеры или его фармацевтически приемлемая сольгдепредставляет одинарную связьили двойную связьпредставляет одинарную связьили двойную связьили тройную связьА представляет собой замещенный или незамещенный Сарил, замещенный или незамещенный гетероцикл, замещенный или незамещенный Сциклоалкил, замещенный или незамещенный Сциклоалкенил или Н;Rпредставляет собой Н, галоген, -OCалкил, замещенный или незамещенный Cалкил, CN, C(O)R, NRRили гидроксил;Rпредставляет собой Н, галоген, замещенный или незамещенный Cалкил, C(O)Rили гидроксил;Rпредставляет собой ОРОН, карбоновую. кислоту, РОН, Cалкил, -S(O)H, -Р(O)МеОН, -Р(O)(Н)ОН или OR;Rпредставляет собой Н, галоген, -OCалкил, замещенный или незамещенный Cалкил, CN, C(O)R, NRRили гидроксил;Rпредставляет собой Н, галоген, -OCалкил, замещенный или незамещенный Cалкил, CN, C(O)R, NRRили гидроксил;Rпредставляет собой Н, галоген, -OCалкил, замещенный или незамещенный Cалкил, CN, C(O)R, NRRили гидроксил;Rпредставляет собой Н, ORили замещенный или незамещенный Cалкил;Rпредставляет собой Н или замещенный или незамещенный Cалкил;Rпредставляет собой Н или замещенный или незамещенный Cалкил;Rпредставляет собой Н или замещенный или незамещенный Cалкил;Lпредставляет собой О, S, NH или CH;Lпредставляет собой О, S, NH или СН;а равен 0 или 1;b равен 0, 1, 2 или 3;с равен 1, 2, 3 или 4;d равен 1, 2 или 3; при условии, чтоесли а равен 1, топредставляет собойилиилиилиилиилииесли а равен 0, то Rпредставляет собой О, S, NH или СН.2. Соединение по п.1, отличающееся тем, что:представляет двойную связьпредставляет одинарную связьили тройную связьА представл РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2013 150 332 A (51) МПК C07D 215/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013150332/04, 13.04.2012 (71) Заявитель(и): АЛЛЕРГАН, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет ...

Bicyclic signal transduction inhibitors, compositions containing them & uses thereof

This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula as defined herein.

Phosphorus containing flame retardants

200℃ 초과의 온도에서 가열된 특정 포스폰산염은, 열 안정적이고, 고효율이며, 중합체에서 난연첨가제로서 사용되기에 매우 적당한 난연제 재료를 생성한다. 본 발명의 난연제는 조성물 중에서 단독 난연제로서 사용될 수 있거나, 또는 기타 다른 난연제, 상승제 또는 보조제와 합하여져 사용될 수 있다. Certain phosphonates heated at temperatures above 200° C. produce flame retardant materials that are heat stable, highly efficient, and very suitable for use as flame retardant additives in polymers. The flame retardant of the present invention may be used as a single flame retardant in the composition, or may be used in combination with other flame retardants, synergists or auxiliary agents.

Quinazoline and indole compounds to treat medical disorders

Phosphonated oligomers of maleic acid

Quinazoline and indole compounds to treat medical disorders

【課題】補体Ｂ因子の阻害剤として作用する化合物、該阻害剤の使用方法及び該阻害剤を作製するプロセスを提供する。【解決手段】具体的には、１－（４－（４－アミノ－８－フルオロ－６，７－ジメトキシキナゾリン－２－イル）ピペラジン－１－イル）－２－（チアゾリジン－２－イル）エタン－１－オンヒドロクロリド（化合物１）等の化合物を提供する。【選択図】なし

Substituted methylene diphosphonic acid compounds and detergent compositions

Novel fused pyrimidine derivatives for inhibition of tyrosine kinase activity

본 발명은 타이로신 카이네이즈 활성 억제 효과를 갖는 신규 융합 피리미딘 유도체에 관한 것으로, 본 발명의 신규 화합물을 활성성분으로 함유하는 약학 조성물은 암, 종양, 염증성 질환, 자가면역 질환 또는 면역학적으로 매개된 질환을 치료하거나 예방하는 효과를 제공한다.

Compounds and methods for inhibiting nhe-mediated antiport in the treatment of disorders associated with fluid retention or salt overload and gastrointestinal tract disorders

본 발명은 심부전 (특히, 울혈성 심부전), 만성 신장질환, 말기 신장 질환, 간 질환, 및 퍼옥시좀 증식인자-활성화된 수용체 (PPAR) 감마 아고니스트-유도된 체액 저류와 같은 체액 저류 또는 염 과부하와 연관된 장애를 치료하기 위한 화합물 및 방법에 관한 것이다. 본 발명은 또한, 고혈압을 치료하기 위한 화합물 및 방법에 관한 것이다. 본 발명은 또한, 위장관 장애와 연관된 통증의 치료 또는 감소를 포함하는, 위장관 장애의 치료를 위한 화합물 및 방법에 관한 것이다. 상기 방법은 일반적으로, 필요한 포유동물에게 위장 (GI)관 내에서 그 안의 나트륨 이온 및 수소 이온의 NHE-매개된 역수송을 억제하는데 실질적으로 활성이 되도록 디자인된 화합물 또는 이러한 화합물을 포함하는 약제학적 조성물의 약제학적 유효량을 투여하는 것을 포함한다. 더욱 특히, 상기 방법은 필요한 포유동물에게 GI관 내에서의 나트륨 이온 및 수소 이온의 NHE-3, -2 및/또는 -8 매개된 역수송을 억제하고, 상피세포의 층, 더욱 특히 GI관의 상피층에 대해서 실질적으로 불투과성이 되도록 디자인된 화합물 또는 이러한 화합물을 포함하는 약제학적 조성물의 약제학적 유효량을 투여하는 것을 포함한다. 화합물이 실질적으로 불투과성인 결과로, 이것은 흡수되지 않고, 따라서 그에 대한 다른 내부 기관 (예를 들어, 간, 심장, 뇌 등)의 노출이 제한되도록 본질적으로 전신적으로 비-생체이용성이다. 본 발명은 또한, 포유동물에게 이러한 화합물을 유체-흡수성 폴리머와 함께 투여함으로써 조합물이 상술한 바와 같이 작용하고, 또한 GI관 내에 존재하는 유체 및/또는 염을 격리시키는 능력을 제공하도록 하는 방법에 관한 것이다.

Polymerizable acrylophosphonic acid that is hydrolytically stable

Novel acrylic phosphonic acid compounds are claimed Acrylic phosphonic acid compounds (I) of formula (1) are claimed. Independent claims are included for: (i) a dental material containing the acrylic phosphonic acid (I) and (ii) polymers and copolymers prepared by (co)polymerization of the acrylic phosphonic acid (I). R<1> = 1-10C alkylene or 6-14 C alkylene; R<2> = H, 1-10C alkyl or 6-10C aryl; Y = oxygen, sulfur, 1-8C alkylene or is missing; n = 1-5; X = CN when 1 is 1 and Z is missing; X = CONR<3> with R<3> equal to H, 1-10C alkyl or 6-10C aryl whereby when n is 1, Z is H or 1-10C alkyl or phenyl and when n=2-5, Z is an aliphatic, aromatic or araliphatic 1-14C hydrocarbon whereby Z and R<3> may form part of an overall ring

QUINAZOLINE AND INDOLE COMPOUNDS FOR THE TREATMENT OF MEDICAL DISORDERS

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2018 145 364 A (51) МПК A61K 31/517 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2018145364, 27.06.2017 (71) Заявитель(и): АЧИЛЛИОН ФАРМАСЬЮТИКАЛС, ИНК. (US) Приоритет(ы): (30) Конвенционный приоритет: 27.06.2016 US 62/355,273; 15.03.2017 US 62/471,799 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 28.01.2019 US 2017/039587 (27.06.2017) (87) Публикация заявки PCT: WO 2018/005552 (04.01.2018) R U (54) ХИНАЗОЛИНОВЫЕ И ИНДОЛЬНЫЕ СОЕДИНЕНИЯ ДЛЯ ЛЕЧЕНИЯ МЕДИЦИНСКИХ НАРУШЕНИЙ (57) Формула изобретения 1. Соединение формулы A 2 0 1 8 1 4 5 3 6 4 A Адрес для переписки: 119019, Москва, ул. Гоголевский бульвар, 11 2 0 1 8 1 4 5 3 6 4 (86) Заявка PCT: R U (43) Дата публикации заявки: 28.07.2020 Бюл. № 22 (72) Автор(ы): ВАЙЛС Джейсон Аллан (US), ФАДКЕ Авинаш (US) или его фармацевтически приемлемая соль, изотопный аналог, пролекарство или выделенный изомер необязательно в фармацевтически приемлемом носителе; где: А выбран из: А1 и А2; В выбран из: В1 и В2; С выбран из: С1 и С2; L выбран из: L1 и L2; по меньшей мере один из А, В, С или L выбран из: А2, В2, С2 или L2, соответственно; А1 представляет собой R1 и R2 независимо выбраны из: водорода, C1-С6алкила, С1-С4алкоксиС1-С4алкила, Стр.: 1 галогенС1-С4алкила, арила, гетероарила, арилалкила, гетероарилалкила, алкенила, алкинила, циклоалкила, циклоалкилалкила, гетероциклила и гетероциклоалкила; R3 и R4 независимо выбраны из: водорода, галогена, амино, С1-С6алкила, С1-С4 алкоксиС1-С4алкила, галогенС1-С4алкила, арила, гетероарила, арилалкила, гетероарилалкила, гидроксила, циано, меркапто, тиоалкила, нитро, алкокси, галогеналкокси, алкенила, алкинила, циклоалкила, циклоалкилалкила, гетероциклила, гетероциклоалкила, арилокси, -S(O)2R1, -S(O)2OH, -S(O)2NH2, -S(O)R1, -S(O)OH, -S(O) NH2 -P(O)(OR1)2, -P(O)(OH)2, B(OH)2, -Si(Rl)3, -COOH, -СООалкила, -С(O)алкила, -С(S) алкила, -COOR1, -C(O)R1, -C(S)R1, -C(O)NH2, -C(S)NH2, - ...

Infrared absorbent composition, infrared cut filter, and imaging optical system

본 발명에 따르는 적외선 흡수성 조성물은, 하기 식 (a)로 표시되는 포스폰산과 구리 이온에 의해서 형성된 적외선 흡수제와, 적외선 흡수제를 분산시키는 인산에스테르를 함유한다. 인산에스테르는, 인산디에스테르 및 인산모노에스테르 중 적어도 한쪽을 포함한다. R 1 은, 페닐기 또는 적어도 1개의 수소 원자가 할로겐 원자로 치환된 페닐기이다. 포스폰산, 구리 이온, 및 인산에스테르의 몰 기준의 함유량을 각각 C A 몰, C C 몰, 및 C E 몰이라고 정의하고, 또한, 반응성 수산기의 몰 기준의 함유량을 C H 몰이라고 정의했을 때, C A /C E ＜1, 또한, C H /C C ＞1.95의 관계를 만족한다. The infrared absorbent composition according to the present invention contains an infrared absorber formed by phosphonic acid represented by the following formula (a) and copper ions, and a phosphoric acid ester for dispersing the infrared absorber. The phosphoric acid ester contains at least one of a phosphoric acid diester and a phosphoric acid monoester. R 1 is a phenyl group or a phenyl group in which at least one hydrogen atom is replaced with a halogen atom. When the molar-based content of phosphonic acid, copper ion, and phosphate ester is defined as C A mol, C C mol, and C E mol, respectively, and when the molar-based content of the reactive hydroxyl group is defined as C H mol, C A / C E <1 and C H / C C > 1.95.

PROCESS FOR PREPARING A SOLUTION OF A RARE EARTH ORGANOPHOSPHATE IN AN ORGANIC SOLVENT

Le procédé de l'invention pour la préparation d'une solution d'un organophosphate de terre rare dans un solvant organique consiste à faire réagir dans ce solvant un composé de terre rare choisi parmi les oxydes, les hydroxydes, les carbonates et les hydroxycarbonates de terre rare avec un acide organophosphoré et en présence d'un promoteur choisi parmi l'eau, les acides nitrique, chlorhydrique, acétique, formique et propionique et les sels de terres rares de ces acides. L'emploi d'un promoteur permet de simplifier le procédé, de réduire le temps de réaction et d'obtenir une solution dont la teneur en solide résiduel peut être faible. The process of the invention for the preparation of a solution of a rare earth organophosphate in an organic solvent comprises reacting in this solvent a rare earth compound selected from oxides, hydroxides, carbonates and hydroxycarbonates of rare earth with an organophosphorus acid and in the presence of a promoter selected from water, nitric, hydrochloric, acetic, formic and propionic acids and the rare earth salts of these acids. The use of a promoter makes it possible to simplify the process, to reduce the reaction time and to obtain a solution whose residual solid content may be low.

Process for the preparation of 2-substituted 1,3-propylidene diphosphone derivatives

Bicyclic signal transduction inhibitors, compositions containing them & uses thereof

This invention concerns compounds for inhibiting intracellular signal transduction, especially intracellular signal transduction mediated by one or more molecular interactions involving a phosphotyrosine-containing protein. This invention also relates to pharmaceutical compositions containing the compounds and prophylactic and therapeutic methods involving pharmaceutical and veterinary administration of the compounds. The compounds are of the formula (I) as defined herein.

Patent FR2309607B1

NEW AMINOPHENYLPHOSPHONIC ACID DERIVATIVES, THEIR PROCESS FOR PREPARATION AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Composé de formule (I) (CF DESSIN DANS BOPI) dans laquelle: R1 , R2 identiques ou différents, représentent un atome d'hydrogène, d'halogène, un groupement alkyle, alkoxy, nitro ou trihalogénométhyle, X représente CO ou SO2 , A représente l'un quelconque des groupements tels que définis dans la description, leurs isomères ainsi que leurs sels d'addition à une base pharmaceutiquement acceptable. Médicaments. Compound of formula (I) (CF DRAWING IN BOPI) in which: R1, R2, identical or different, represent a hydrogen or halogen atom, an alkyl, alkoxy, nitro or trihalomethyl group, X represents CO or SO2, A represents any one of the groups as defined in the description, their isomers as well as their addition salts with a pharmaceutically acceptable base. Medicines.

Bath and process for producing shiny zinc coatings by electroplating

NOVEL URANYLE ION CAPTURING AGENTS AND PROCESS FOR THEIR PREPARATION

AGENTS DE CAPTURE DES IONS URANYLE. ILS SONT CONSTITUES PAR DES COMPOSES COMPRENANT UN POLYMERE LIE CHIMIQUEMENT A AU MOINS UN DES GROUPEMENTS X, X ET X D'UN COMPOSE MACROCYCLIQUE REPRESENTE PAR LA FORMULE GENERALE: (CF DESSIN DANS BOPI) TRAITEMENT NOTAMMENT DE L'EAU DE MER, POUR EN EXTRAIRE LES IONS URANYLE. URANYLE ION CAPTURING AGENTS. THEY ARE CONSTITUTED BY COMPOUNDS INCLUDING A POLYMER CHEMICALLY BOUND TO AT LEAST ONE OF THE X, X AND X GROUPS OF A MACROCYCLIC COMPOUND REPRESENTED BY THE GENERAL FORMULA: (CF DRAWING IN BOPI) TREATMENT IN PARTICULAR OF SEA WATER, FOR EXTRACT URANYLE IONS.

Antagonists of specific excitatory amino acid neurotransmitter receptors

Abstract of the Disclosure Inventors: Waclaw Janusz Rzeszotarski, Robert Lee Hudkins, Maria Elizabeth Guzewska Invention: Antagonists of Specific Excitatory Amino Acid Neurotransmitter Receptors The invention pertains to novel, potent anticonvulsants, analgesics and cognition enhancers achieving their action through the antagonism of specific excitatory amino acid neurotransmitter receptors. In particular, the invention is directed to .omega.-[2-phosphonoalkylenyl)phenyl]-2-aminoalkanoic acids having general formula: Wherein R1 and R2 are the same or different and are selected from the group consisting of hydrogen, lower alkyl, halogen, -CH=CH-CH=CH=, amino, nitro, trifluoromethyl or cyano; n and m = 0, 1, 2 or 3; and the pharmaceutically acceptable salts and derivatives thereof. Examples of specific preferred compounds of general formula are selected from the group consisting of: 4-[2-phosphonomethylphenyl]-2-aminobutanoic acid, ethyl 3-[2-(2 (2-diethylphosphonoethyl)phenyl]-2-acetamido-2-carboethoxypropanoate, 3-[2-phosphonomethyl)phenyl]-2-aminopropanoic acid, ethyl 3-[2-(3-bromopropyl)phenyl]-2-acetamido-3-carboethoxypropanoate, ethyl 3-[2-(3-diethylphosphonopropyl)phenyl]-2-acetamido-2-carboethoxypropanoate, ethyl 3-[2-(3-phosphonopropyl) phenyl]-2-aminopropanoic acid, ethyl 5-[2-(diethylphosphonomethyl)-phenyl]-2- acetamido-2-carboethoxypentanoate, and 5-[2-phosphonomethylphenyl]-2-aminopentanoic acid.

Carbon paper - leucoauramine coating gives more light stable copies in alcohol duplicating process

Carbon paper consists of a coated support containing a leucoauramine of general formula:- where A, B are opt. subst. 1:4-arylene, R is H, OH, alkoxy; amino, alkyl, aralkyl, or cycloalkyl opt. substd. X is H, hydrocarbon which may contain heterocycles and be substituted or R and X form opt. substd. heterocycle. R1-4 are H, opt. substd. alkyl, aralkyl, cycloalkyl, or aryl or may form a heterocycle with the N atom. Y is sulpho, sulphino, sulphato, sulphito, thiosulphato, thiosulphono, thiosulphine carboxyl, or thiocarboxyl or D-E where D is O, S or a direct link and E is where F is H, hydrocarbon or the O atoms may be S, or if Y is joined to a cyclic system it can be OH or SH; n = 1-3. The coating is preferably 8-50 g/m2 and contains 45-55% leucoauramino.

Light absorbing composition and optical filter

本发明的光吸收性组合物含有光吸收剂、固化性树脂、以及烷氧基硅烷。烷氧基硅烷包含二烷氧基硅烷。由于光吸收性组合物的烷氧基硅烷包含二烷氧基硅烷，因此在光吸收层中形成具有硅氧烷键的牢固的骨架，并且容易通过二烷氧基硅烷所具有的有机官能团而对光吸收层赋予所期望的柔软性。

Patent FR2469410B1

Patent FR2253043B1

Substd. propane-(1,3)-diphosphonic and-diphosphinic acids - useful as corrosion- and scaling inhibitors

Propane-1,3-diphosphon-(or -in)ic acids are of formula (I) and their salts are new: In the formula, R1 and R2 are each H when a or b = 1, or, when a or b = 0, opt. substd. 1-8C alkyl or opt. substd. Ph; R3 is H, opt. substd. 1-4C alkyl, opt. substd. Ph; F, Cl, Br, OH, 1-8C alkoxy, carboxyl or -P(O)-(O)a-R1OH; R4 is H, 1-4C alkyl, 2-3C alkenyl, opt. substd. Ph, carboxyl, F, Cl or -P(O)-(O)a-R1OH; R3 and R4 may also form a divalent radical -(CH2)n-, where n = 3-5. R5 is H, 1-4C opt. substd. alkyl, (Me)-carboxymethyl or carboxyethyl, a succinyl gp. or -CHR4-CHR3-P(O)-(O)a-R1-OH or -CH2-P(O)-(O)a-R1OH; R6 is opt. substd. Ph or when R5 = carboxymethyl, is carboxy. a and b are each 0 or 1, or a salt of cpd. (I). Cpds. (I) are useful as corrosion inhibitors and antiscale agents, which are added to liquors to protect metallic surfaces that they contact.

NOVEL MIXED AMINOBENZYLIC ACID DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

The invention concerns a compound of formula (I) in which: R1, R2, R'1, R'2, identical or different, represent a hydrogen, halogen atom, an alkyl, alkoxy, hydroxy, nitro or trihalogenomethyl group, or R1 and R2 (respectively R'1 and R'2) form together with the benzene nucleus which bears them a naphthyl or anthracenyl group; X represents C=T, SO2, CH2, or X-A1-X represents the group (a) in which T represents an oxygen atom or a sulphur atom; A1 represents any one of the groups as defined in the description; A2, A3, identical or different, represent an alkylene group or a single bond; R3, R4, identical or different, represent any one of the groups as defined in the description. The invention also concerns its isomers as well as its additive salts to a pharmaceutically acceptable base. The invention is useful for the preparation of medicines.

Phosphonates contg. a P-32 or P-33 radionuclide - prepd. by reaction of labelled phosphorus trichloride and acid

(A) Cpds. of the fllowing formulae labelled with the radio-isotopes 32P or 33P are stated to be new: and the labelled cpds. 1,2-dicarboxyethylene-1-phosphonic acid and ethylene-1,1-diphosphonic acid. (R=H or CH2OH; n=3-10; R1=H, 1-20C alkyl, 2-20C alkenyl, aryl, phenylethyl, benzyl, halo, OH, opt. substd. amino, carboxymethyl, CH2PO3H2, CHOH.PO3H2 or - [CH2C(PO3H2)2]n'H; n' = 1-15; R2 = H, alkyl, NH2, benzyl, halo, OH, CH2COOH, CH2PO3H2 or CH2CH2PO3H2; m=3-9; R3=H or alkyl; p=2-4; X and Y = H or OH). Salts of these cpds. are included. (B) Claims are restricted to compsns. for treatment of tumours contg. these cpds. The cpds. may be used in the treatment of calcareous tumours, such as primary- and metastic bone tumours and tumours which calcify soft tissue. They may also be used in combined therapy with other chemotherapeutic agents. The cpds. have a high selectivity for calcareous tumours of up to 40:1 with respect to normal bone. They have very low soft-tissue retention and few side-effects.

Method of producing solution of organophosphate of rare-earth element in organic solvent

FIELD: chemistry. SUBSTANCE: present invention relates to a method of producing a solution of an organophosphate rare-earth element in an organic solvent. According to the method, organophosphoric acid, in the presence of said solvent, reacts with a rare-earth element compound selected from oxides, hydroxides, carbonates and hydroxycarbonates of a rare-earth element, where the reaction takes place in the presence of a promoter selected from nitric, hydrochloric, acetic, methanoic and propionic acid and salts of rare-earth elements and said acids. EFFECT: invention simplifies the method, cuts duration of the reaction and enables to obtain a solution with low content of residual solid substances. 6 cl, 7 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 441 013 (13) C2 (51) МПК C07F C08F 5/00 4/52 (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010108164/04, 08.07.2008 (24) Дата начала отсчета срока действия патента: 08.07.2008 (73) Патентообладатель(и): РОДИА ОПЕРАСЬОН (FR) R U Приоритет(ы): (30) Конвенционный приоритет: 08.08.2007 FR 0705766 (72) Автор(ы): МАТИВЕ Тома (FR) (43) Дата публикации заявки: 20.09.2011 Бюл. № 26 2 4 4 1 0 1 3 (45) Опубликовано: 27.01.2012 Бюл. № 3 (56) Список документов, цитированных в отчете о поиске: ЕР 0924214 А, 23.06.1999. WO 00/64910 А1, 02.11.2000. US 6767927 В1, 27.07.2004. RU 2301236 С, 20.06.2007. 2 4 4 1 0 1 3 R U (86) Заявка PCT: EP 2008/058849 (08.07.2008) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 09.03.2010 (87) Публикация заявки РСТ: WO 2009/019100 (12.02.2009) Адрес для переписки: 129090, Москва, ул.Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной (54) СПОСОБ ПОЛУЧЕНИЯ РАСТВОРА ОРГАНОФОСФАТА РЕДКОЗЕМЕЛЬНОГО ЭЛЕМЕНТА В ОРГАНИЧЕСКОМ РАСТВОРИТЕЛЕ (57) Реферат: Настоящее изобретение относится к способу получения раствора органофосфата редкоземельного элемента в органическом растворителе. ...

Oral compositions delaying tartar formation

NOVEL CHLORHEXIDINE SALTS AND ANTIBACTERIAL COMPOSITION CONTAINING THE SAME

L'INVENTION A TRAIT AU DOMAINE DE LA CHIMIE PHARMACEUTIQUE. ELLE CONCERNE LES SELS TELS QUE LE DISORBATE, LE DINALIDIXATE ET LE DIPHOSPHANILATE DE LA CHLORHEXIDINE. LES COMPOSES DE L'INVENTION SONT DOUES D'ACTIVITE ANTIBACTERIENNE. ILS EXERCENT UN EFFET SYNERGIQUE COMPARATIVEMENT A DES CONCENTRATIONS SIMILAIRES DE CHLORHEXIDINE ET DE L'ACIDE LIBRE CORRESPONDANT. L'INVENTION CONCERNE AUSSI DES COMPOSITIONS DERMATOLOGIQUES RENFERMANT CES NOUVEAUX SELS. THE INVENTION RELATES TO THE FIELD OF PHARMACEUTICAL CHEMISTRY. IT CONCERNS SALTS SUCH AS CHLORHEXIDINE DISORBATE, DINALIDIXATE AND DIPHOSPHANILATE. THE COMPOUNDS OF THE INVENTION HAVE ANTIBACTERIAL ACTIVITY. THEY EXERCISE A SYNERGIC EFFECT COMPARED TO SIMILAR CONCENTRATIONS OF CHLORHEXIDINE AND THE CORRESPONDING FREE ACID. THE INVENTION ALSO CONCERNS DERMATOLOGICAL COMPOSITIONS CONTAINING THESE NEW SALTS.