СУЛЬФОНАМИДНЫЕ ИНГИБИТОРЫ HIY - АСПАРТИЛ-ПРОТЕАЗЫ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ЛЕЧЕНИЯ, СПОСОБ ИДЕНТИФИКАЦИИ ИНГИБИТОРА

Изобретение относится к новому классу сульфонамидов, которые являются ингибиторами аспартил-протеазы формулы I. Изобретение относится к новому классу H1У аспартил-протеазных ингибиторов, отличающемуся специфическими структурными и физико-химическими характеристиками. Изобретение относится также к фармацевтическим композициям, содержащим эти соединения. Соединения и фармацевтические композиции изобретения особенно подходят для ингибирования Н1У-1 и Н1У-2 протеазной активности, и, соответственно, их можно с выгодой использовать в качестве вирусных агентов против Н1У-1 и Н1У-2 вирусов. Изобретение относится также к способам ингибирования активности Н1У аспартил-протеазы, за счет использования соединений настоящего изобретения, и способам скринирования соединений по их анти-HIУ активности. 5 с. и 21 з.п. ф-лы, 3 ил., 8 табл.

ГЕТЕРОАРОМАТИЧЕСКИЕ ПРОИЗВОДНЫЕ МОЧЕВИНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ АКТИВАТОРОВ ГЛЮКОКИНАЗЫ

... 1. Соединение общей формулы (I) где R1 представляет собой С3-8-циклоалкил, С3-8-циклоалкенил, С3-8-гетероциклил, С3-8-гетероциклоалкенил, конденсированный арил-С3-8-циклоалкил или конденсированный гетероарил-С3-8-циклоалкил, каждый из которых возможно замещен одним или более чем одним заместителем R3, R4, R5 и R6; R2 представляет собой С3-8-циклоалкил, С3-8 -циклоалкенил, С3-8-гетероциклил, С3-8-гетероциклоалкенил, конденсированный арил-С3-8-циклоалкил или конденсированный гетероарил-С3-8-циклоалкил, каждый из которых возможно замещен одним или более чем одним заместителем R30, R31, R32 и R33, и R3, R4, R5, R6, R30, R31, R32 и R33 независимо выбраны из группы, состоящей из галогена, нитро, циано, гидрокси, оксо, карбокси, -CF3; либо - NR10R11; либо С1-6-алкила, С2-6-алкенила, С2-6-алкинила, С3-8-циклоалкила, С3-8-циклоалкил-С1-6-алкила, арила, арил-С1-6-алкила, гетероарил-С1-6-алкила, С1-6-алкокси, С3-6-циклоалкил-С1-6-алкокси, арил-С1-6-алкокси, гетероарила, гетероарил-С1-6-алкокси, арилокси ...

АЦИЛАМИНОЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ КОНДЕНСИРОВАННЫХ ЦИКЛОПЕНТАНКАРБОНОВЫХ КИСЛОТ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ФАРМАЦЕВТИЧЕСКИХ СРЕДСТВ

... 1. Соединение формулы I в любой из его стереоизомерных форм или сочетании стереоизомерных форм в любом соотношении, или его физиологически приемлемая соль, или физиологически приемлемый сольват любого из них ! ! где кольцо A является циклоалкановым кольцом с числом членов от 3 до 7, бензольным кольцом или моноциклическим 5-членным или 6-членным ароматическим гетероциклическим кольцом, содержащим 1 или 2 одинаковых или разных гетерочленов кольца, выбранных из группы, содержащей N, N(R0), O и S, причем циклоалкановое кольцо может необязательно иметь один или более одинаковых или разных заместителей, выбранных из группы, содержащей фтор и (C1-C4)-алкил, а бензольное и гетероциклическое кольца могут необязательно иметь один или более одинаковых или разных заместителей, выбранных из группы, содержащей галоген, R1, HO-, R1-O-, R1-C(O)-O-, R1-S(O)2-O-, R1-S(O)m-, H2N-, R1-NH-, R1-N(R1)-, R1-C(O)-NH-, R1-C(O)-N(R71)-, R1-S(O)2-NH-, R1-S(O)2-N(R71)-, R1-C(O)-, HO-C(O)-, R1-O-C(O)-, H2N-C(O)-, R1 ...

DIAMID-DERIVATE VON HETEROCYCLISCHEN DICARBONSÄUREN, INSEKTIZIDE FÜR ACKER- UND GARTENBAU UND EIN VERFAHREN ZU IHRER VERWENDUNG

NEUE SULFENAMIDE, VERFAHREN ZU IHRER HERSTELLUNG, IHRE VERWENDUNG IN ARZNEIMITTELN UND DEREN HERSTELLUNG

Sulfonamid inhibitoren von Hiv-aspartyl Protease

TETRAHYDROFURANYL (THF) ENTHALTENDE SULFONAMIDINHIBITOREN DER ASPARTYL-PROTEASE

ANTIDIABETISCHE MITTEL

2-(thio)phosphoryloxy-2-heterocyclylvinyl alkyl sulphides - - with insecticidal and acaricidal activity

Cpds. of formula (I):- (where R ad R2 are 1-6C alkyl; R1 is 1-6C alkyl or alkoxy; X is O or S;) and Het is a 5-membered heterocycle contg. 1-3 heteroatoms and opt. mono- or polysubstd. by lower alkyl) have insecticidal and acaricidal activity. They may be prepd. by (a) reacting R1(RO)P(S)Hal with Het-CO-CH2SR2 (II) in the pres. of an acid binder, or (b) reacting (II) with SO2Cl2 and then with (RO)3P without isolating the intermediate.

THF-containing sulfonamide inhibitors of aspartyl protease.

The present invention relates to a class of TKF-containing sulfonamide aspartyl protease inhibitors having the structure of formula I: D OH D1 I I ITHF—R-NH—CH—CH—CH2——N—S02E (I) . This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.

Novel sulfonamide inhibitors aspartyl protease.

The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of hiv aspartyl protease inhibitors characterized by specific structural and characterized by specific structural and physicochemical features this invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting hiv-1 and hiv-2 protease activity and consequently, may be advantageously used as anti-viral agents against the hiv-1 and hiv-2 viruses. This invention also relates to methods for inhibiting the activity of hiv aspartly protease using the compounds of this invention and methods for screening compounds for ant-hiv activity ...

THF-containing sulfonamide inhibitors of aspartyl protease

NOVEL SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE

New addition salts of angiotensinconverting enzymeir preparation and pharmaceutical compositions coninhibitors with no donor acids, a process for the taining them

N,N' -substituted-1,3-diamino -2-hydroxypropane derivatives.

Disclosed are compounds of the formula (0, wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of betasec-retase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.

Substituted aryl thioureas and related compounds; inhibitors of viral replication

N,N'-substituted-1,3-diamino-2-hydroxypropane derivatives.

Substituted aryl thioureas and related compounds, inhibitors of viral replication.

The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/ or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

Substituted aryl thioureas and related compounds; inhibitors of viral replication

THF-containing sulfonamide inhibitors of aspartyl protease

Substituted aryl thioureas and related compounds; inhibitors of viral replication

NOVEL SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE

New addition salts of angiotensinconverting enzymeir preparation and pharmaceutical compositions coninhibitors with no donor acids, a process for the taining them

VERFAHREN ZUR HERSTELLUNG NEUER THIADIAZOLDERIVATE UND IHRER SALZE

SUBSTITUTED 1,2,5-OXADIAZOL-2-OXIDE FOR APPLICATION AS DRUG AND IT ABSTENTIONS DRUG.

SUBSTITUTED FURAZANE.

HERBICIDES HETERO-CYCLIC CONNECTIONS.

HETERO-CYCLIC CONNECTIONS CONTAINING COMPOSITIONS AND YOUR USE AS HERBICIDES.

PHARMACEUTICAL COMPOSITIONS.

DIAMID DERIVATIVES OF HETERO-CYCLIC DICARBONIC ACIDS, INSECTICIDES FOR FIELD AND HORTICULTURE AND A PROCEDURE FOR YOUR USE

ANTIDIABETI MEANS

SULFONAMIDE INHIBITORE OF HIV ASPARTYL PROTEASE

Substrates and screening methods for transport proteins

Heteroaryl-ureas and their use as glucokinase activators

This invention relates to compounds that are of formula (I) wherein A is heteroaryl and R and R are both cyclic residues, that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial .

N-(1,2,5-oxadiazol-3-yl) benzamides and the use thereof as herbicides

The invention relates to N-(1,2,5-oxadiazol-3-yl) benzamides of the general formula (I) as herbicides. In said formula (I), X, Y, Z, and R represent groups such as hydrogen, organic groups such as alkyl, and other groups such as halogen.

Cathepsin cysteine protease inhibitors

1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase

NO- and H2S- releasing compounds

This disclosure relates to novel compounds containing an H ...

Method of treating diabetes and related disease states

Method of treating diabetes and related disease states

THF-containing sulfonamide inhibitors of aspartyl protease

Sulfonamide inhibitors of hiv-aspartyl protease

COMPOSITIONS CONTAINING HETEROCYCLIC COMPOUNDS AND THEIR USE AS HERBICIDES

CATHEPSIN CYSTEINE PROTEASE INHIBITORS

This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

COMPOSITIONS CONTAINING HETEROCYCLIC COMPOUNDS AND THEIR USE AS HERBICIDES

Composition containing heterocyclic compounds are described which include an amide group, can act as herbicides and be defined by the general formula: in which: R is a linear or branched alkyl group containing from 1 to 6 carbon atoms; - the phenyl group; - a phenyl group having a substituent, or several substituents, which may be identical or different from each other, selected from the halogens and alkyl (C1-C4), oxyalkyl (C1-C4), halogenoalkyl (C1-C4) and nitro groups; R1 is a linear or branched alkyl group containing from 1 to 12 carbon atoms; - a linear or branched alkyl group containing from 1 to 12 carbon atoms substituted with one or more halogen atoms: - a cycloalkyl group containing from 3 to 8 carbon atoms; - a (methyleneoxy)alkyl (C1-C5) group; - a (methyleneoxy)phenyl group; - a (methyleneoxy)phenyl group having one or more substituents in the ring which are selected from halogen, (C1-C4) alkyl, (C1-C4)halogenoalkyl groups; - the phenyl group; - the benzyl group; - a ...

DERIVATIVES OF 1,2,5-THIADIAZOLE-1-OXIDES AND 1,1- DIOXIDESAS HISTAMINE H2-ANTAGONISTS

A compound of the formula wherein p is 1 or 2; n is an integer of from 2 to 4 inclusive; R2 and R3 each are independently hydrogen, (lower)alkyl, (lower)alkenyl, (lowerl)alkynyl, cyclo(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, hydroxy(lower)alkyl, (lower)alkoxy(lower)alkyl, (lower)alkylthio(lower)alkyl, amino (lower)alkyl, (lower)alkylamino(lower)alkyl, di(lower)alkylamino(lower)alkyl, pyrrolidino(lower)alkyl, piperidino (lower)alkyl, morpholino (lower)alkyl, piperazino(lower)alkyl, pyridyl(lower)alkyl, amino, (lower)alkylamino, di(lower)alkylamino, 2,2,2-trifiuoroethyl, 2-fluoroethyl, hydroxy, (lower)alkoxy, 2,3-dihydroxypropyl, cyano, cyano(lower)alkyl, amidino, (lower)alkylamidino, A'-(CH2)m,Z'(CH2)n,-, phenyl, phenyl(lower)alkyl substituted phenyl or substituted phenyl(lower)alkyl, wherein the phenyl ring may contain one or two substituents independently selected from (lower)alkyl, hydroxy, (lower)alkoxy and halogen, or one substituent selected from methylenedioxy, trifluoromethyl ...

CEPHALOSPORINS

ANTIBACTERIAL AGENTS 7-¢D-(.alpha.-Amino-a-phenyl-, 2-thienyl-and 3-thienylacetamido!-3-(thiazol-2-yl)carbonyl-thiomethyl-3-cephem-4-carboxylic acid and 7-¢D-(.alpha.-amino-a-phenyl-, 2-thienyl- and 3thienylacetamido!-3-(5-methylthiazol-2-yl)carbon-ylthiomethyl-3-cephem-4-carboxylic acid and 7-¢D-(.alpha.-Amino-.alpha.-phenyl-, 2-thienyl- and 3thienylacetamido!-3-(3-methyl-1,2,5-oxadiazol-4-yl)-carbonylthiomethyl-3-cephem-4-carboxylic acids and their pharmaceutically acceptable salts are valuable as antibacterial agents, as nutritional supplements in animal feeds, as agents for the treatment of mastitis in cattle and as therepeutic agents in poultry and animals, including man. The compounds are especially useful in the treatment, particularly by oral administration, of infectious diseases caused by many Gram-positive and Gram-negative bacteria. Also included within the invention are easily cleavable esters of the above acids and pharmaceutically acceptable acid addition salts of said esters ...

PRODUCTION OF ISOCYANATES

A furoxan, especially one in which the furoxan ring is fused to a strained aliphatic ring system, is heated in the presence of sulphur dioxide to give an isocyanate. The process enables furoxans, such as dicyclopentadiene furoxan, which ring-open at temperatures <180.degree.C to be converted into isocyanates. In the absence of sulphur dioxide, may be difficult to control the reaction and, in some cases, no isocyanate is obtained. Diisocyanates prepared by the process may be converted into polyurethanes by reaction with suitable hydroxylic compounds.

PRODUCTION OF ISOCYANATES

SUBSTITUTED FURAZANES

N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE

ANTIDIABETIC AGENTS

The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.

THF-CONTAINING SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE

The present invention relates to a class of THF-containing sulfonamides whic h are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activit y and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.

Produit pour le lavage dans de l'eau dure.

3-amino-4-phenyl-furazans

... 3-Amino-4-phenyl-furazans. Title cpds. of formula (I): (where R1 is halogen, NO2, CF3, lower alkoxy or lower alkylthio; R2 is H, lower alkyl or lower alkoxy and R3 is H or lower alkoxy), which are C.N.S. depressants, anticonvulsants and muscle relaxants, are prepd. by hydrolyzing cpds. of formula (II): (where X is the acyl residue of an org. acid). The hydrolysis is carried out with e.g. an alkali(ne earth) hydroxide or a mineral acid, pref. in a hydroxylic solvent.

Verfahren zur Herstellung von neuen Furazanderivaten

Furoxane derivatives used as anti convulsive

Furoxane derivatives used as anti-convulsive. Cpds. of formula:- (where R1 is halogen, nitro, trifluoromethyl, lower alkoxy or alkylthio, or, in o- or m-position a lower alkyl, R2 is H, lower alkyl or alkoxy, R3 is H or lower alkoxy) are prepared by reacting cpd. of formula:- with 1 mol. equivalent ammonia in presence of oxidant, preferably an equivalent amount of potassiumferricyanide.

Furoxane derivatives used as anti convulsive

Furoxane derivatives used as anti-convulsives Cpds. of formula:- (where R1 is halogen, nitro, fluoromethyl, lower alkoxy or alkylthio or, in o- or m-position, lower alkyl, R2 is H, lower alkyl or alkoxy and R3 is H or lower alkoxy) are produced by reacting cpd. of formula:- with 1 mol. equivalent ammonia in presence of oxidant.

Pharmaceutical furazan derivs prodn

Pharmaceutical furazan derivs. prodn. Compounds possessing depressant, anticonvulsive and muscle-relaxing properties have formula: (in which R1 is a halogen, NO2, CF3, a lower alkoxy or alkylthio group, R2 is H a lower alkyl or alkoxy gp. and R3 is H or a lower alkoxy gp). These cpds. can be prodcued by reacting hydroxylamine hydrochloride with a compound of formula: (where R4 is H or a lower alkyl).

Verfahren zur Herstellung von neuen Furazanderivaten

Verfahren zur Herstellung von neuen Furazanderivaten

Verfahren zur Herstellung von neuen Furazanderivaten

Verfahren zur Herstellung von neuen Furazanderivaten

Verfahren zur Herstellung von neuen Furazanderivaten

Pharmaceutical furazan derivs prodn

Pharmaceutical furazan derivs. prodn. Cpds. possessing depressant, anticonvulsive and muscle-relaxing properties have formula: (in which R1 is H or a lower alkyl, and R2 is a lower alkyl in the m or o-position). These compounds are produced by reducing (pref. with zinc in dilute acetic acid or with SnCl2 in a CH3COOH-HCl mixture) a compound of the formula.

Pharmaceutical furazan derivs prodn

Pharmaceutical furazan derivs. prodn. Compounds possessing depressant, anticonvulsive and muscle-relaxing properties have formula: (in which R1 is H or a lower alkyl, and R2 is a lower alkyl in the m- or o-position). These compounds are produced by boiling in a strong mineral acid a compound of formula: (where R3 is a lower alkyl).

Pharmaceutical furazan derivs prodn

Pharmaceutical furazan derivs. prodn. Cpds. possessing depressant, anticonvulsive and muscle relaxing properties have formula: (in which R1 is H or lower alkyl, and R2 is a lower alkyl in the m- or o-position). These compounds are produced by the Hoffmann reaction from the compound.

Pharmaceutical furazan deriv prodn

Pharmaceutical furazan deriv. prodn. Compounds possessing depressant, anticonvulsive and muscle-relaxing properties, have the general formula: (where R1 is H or a lower alkyl, and R2 is a lower alkyl occupying the m- or o-position). These compounds are produced by reacting hydroxylamine hydrochloride with (where R3 is H or lower alkyl).

Pharmaceutical furazan derivs prodn

Pharmaceutical furazan derivs prodn. Cpds. possessing depressant, anticonvulsive and muscle-relaxing properties, have formula: (in which R1 is a halogen, NO2, CF3, a lower alkoxy or alkythio group, R2 is H, a lower alkyl or alkoxy group, and R3 is H or a lower alkoxy group). These compounds can be produced by boiling in a strong mineral acid a compound of the formula: (in which R4 is a lower alkyl).

Pharmaceutical furazan derivatives prodn

Pharmaceutical furazan derivatives prodn. Cpds. possessing depressant, anticonvulsive and muscle-relaxing properties, have the general formula: (in which R1 is a halogen, NO2, CF3, a lower alkoxy or alkylthio group, R2 is H, a lower alkyl or alkoxy group, and R3 is H or a lower alkoxy group). These compounds can be produced by reducing (preferably with Zn in dilute acetic acid, or with SnCl2 in a CH3COOH-HCl mixture) a cpd. of the formula.

Pharmaceutical furazan derivatives prodn

Pharmaceutical furazan derivatives prodn. Cpds. possessing depressant, anticonvulsive and muscle-relaxing properties have the general formula: (in which R1 is a halogen, NO2, CF3, a lower alkoxy or alkylthio group, R2 is H, a lower alkyl or alkoxy group, R3 is H or a lower alkoxy group). These compounds can be produced by the Hoffman reaction from a compound of the formula: (in which R1, R2 and R3 are as above).

Anti convulsive furoxane derivative

Anti-convulsive furoxane derivative. Cpds. of formula:- (where R1 is halogen, nitro, trifluoromethyl, lower alkoxy or alkylthio or, in o- or m-position a lower alkyl, R is H, lower alkyl or alkoxy and R3 is H or lower alkoxy), such as 3-amino-4-(3-4-xylyl)-furoxane are obtained by reacting cpd. of formula:- with 1 mol. equivalent ammonia in presence of oxidant, preferably an equivalent amount of potassiumferricyanide, in aq. medium.

Verfahren zur Herstellung von neuen Furazanderivaten

3,4-DISUBSTITUIERTE-1,2,5-THIADIAZOL-1-OXIDE AND 1,1-DIOXIDE, PROCEDURE FOR YOUR PRODUCTION AND IT ABSTENTION PHARMACEUTICAL PREPARATIONS.

1,2,5-Thiadiazole 1-oxide and 1,1-di:oxide derivs. - useful as anti-ulcer agents

... 1,2,5-thiadiazole 1-oxides and 1,1-dioxides of formula (I) and their salts, hydrates, solvates and N-oxides are new where R1 is OH or NR2R3; R2 and R3 are H, lower alkyl alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, aminoalkyl, mono- or dialkylaminoalkyl, pyrrolidino-, piperidino-, morpholino-, piperazino- or pyridylalkyl, NH2, alkylamino, dialkylamino, CH2CF3, CH2CH2F, OH, alkoxy, 2,3-dihydroxypropyl, CN, cyanoalkyl, amidino, alkylamidino, A(CH2)mZ(CH2)n, or phenyl or phenylalkyl opt. ring-substd. by 1 or 2 gps. , provided that R2 and R3 are not both cycloalkyl, opt. substd. phenyl, NH2, (di)alkylamino, OH, alkoxy, CN, (alkyl) amidino or A(CH2)mZ(CH2)n; or R2+R3 is CH2CH2X(CH2)r, where r is 1-3 and X is CH2, S, O or NR4, provided that X is CH2 when r is 1; R4 is H, alkyl, alkenyl, alkynyl, alkanoyl or benzoyl. Each m is 0-2; each n is 2-4; each Z is S, O, or CH2; each A is a phenyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, triazolyl ...

METHOD OF SYNTHESIS OF INHIBITOR INDOLAMIN - 2, 3 - DIOXYGENASE MIMETIC ARE INTRODUCED

COMPOSITION OF HERBICIDE AND SAFENERU

Thf-containing sulfonamide inhibitors of aspartyl protease

МОДУЛЯТОРЫ ИНДОЛАМИН-2,3-ДИОКСИГЕНАЗЫ И ИХ ПРИМЕНЕНИЕ

Данное изобретение касается модуляторов индоламин-2,3-диоксигеназы (IDO), а также композиций, которые их содержат, и способов лечения.

ТГФ-СОДЕРЖАЩИЕ СУЛЬФОНАМИДНЫЕ ИНГИБИТОРЫ АСПАРТИЛ-ПРОТЕАЗЫ

МОДУЛЯТОРЫ ИНДОЛАМИН 2,3-ДИОКСИГЕНАЗЫ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Настоящее изобретение относится к модуляторам индоламин 2,3-диоксигеназы (IDO), а также к композициям, их содержащим, и способам лечения.

НЕСТЕРОИДНЫЕ (ГЕТЕРО)ЦИКЛИЧЕСКИ ЗАМЕЩЕННЫЕ АЦИЛАНИЛИДЫ, ОБЛАДАЮЩИЕ СМЕШАННЫМ ГЕСТАГЕННЫМ И АНДРОГЕННЫМ ДЕЙСТВИЕМ

... 1. Соединения общей формулы I в которой R1и R2 являются одинаковыми или различными и обозначают атом водорода, C1-C5алкильную группу или атом галогена, а также вместе с C-атомом цепи образуют кольцо, имеющее в общей сложности 3-7 членов, R3 обозначает C1-C5алкильную группу или частично либо полностью фторированную C1-C5алкильную группу, A обозначает моно- либо бициклическое карбоциклическое или гетероциклическое ароматическое кольцо, которое необязательно замещено одним или несколькими остатками, выбранными из атомов галогена, C1-C5 алкильных групп, C2-C5алкенильных групп -CR5=CR6R7, где R5, R6и R7 являются одинаковыми или различными и независимо друг от друга обозначают атомы водорода или C1-C5алкильные группы, гидроксигрупп, гидроксигрупп, которые несут C1-C10ацильную группу, C3-C10карбалкоксиалкильную группу, C2-C5цианалкильную группу, незамещенную либо замещенную C3-C10аллильную группу, незамещенную либо замещенную C3-C10пропаргильную группу, C2-C5алкоксиалкильную группу, частично либо ...

BENZAMIDE COMPOUNDS AND THEIR USE AS HERBICIDES

N-(1,2,5-OXADIAZOL-3-YL)BENZAMIDES AND THE USE THEREOF AS HERBICIDES

N,N'−SUBSTITUTED−1,3−DIAMINO−2−HYDROXYPROPANE DERIVATIVES

COMPOSITION FROM HERBICIDE AND PROTECTIVE AGENT

HERBICIDALLY ACTING AMIDES OF BENZOIC ACIDS

1.2, 5 - oxadiazoles as inhibitors of indolamin - 2, 3 - dioxygenase mimetic are introduced

N-(1,2,5-OXADIAZOL-3-YL)-, N-(1,3,4-OXADIAZOL-2-YL)-, N-(TETRAZOL-5-YL)- UND N-(TRIAZOL-5-YL)-ARYLCARBONSAUREAMIDE UND IHRE VERWENDUNG ALS HERBIZIDE

NEW ADDITION SALTS OF ANGIOTENSIN-CONVERTING ENZYME INHIBITORS WITH NO DONOR ACIDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

THF-Containing Sulfonamide Inhibitors of Aspartyl Protease

(54) Sulfonamide Inhibitors of HIV-Aspartyl Protease, Pharmaceutical Composition and Method for Identification of Inhibitor

Process for the synthesis of an indoleamine 2,3-dioxygenase inhibitor

Kilogram-grade preparation method of 3,3'-diamino-4,4'-azoxyfurazan

1,2,5-Thiadiazole 1-oxide and 1,1-di:oxide derivs. - useful as anti-ulcer agents

PROCESS FOR THE SYNTHESIS OF AN INHIBITOR OF 2, 3 DIOXYGENASE

Substituted Esters as Cannabinoid-1 Receptor Modulators

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness.

New compounds, pharmaceutical compositions and uses thereof

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF USING THE SAME

The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. 2. The compound of wherein Ring A is heterocyclyl optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.3. The compound of wherein Ring A is 5- or 6-membered heterocyclyl optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.4. The compound of wherein Ring A is 5-membered heterocyclyl optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.5. The compound of wherein Ring A is 5-membered heterocyclyl containing at least one ring-forming N atom and Ring A is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.6. The compound of wherein Ring A is 5-membered heterocyclyl containing at least one ring-forming O atom and Ring A is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.7. The compound of wherein Ring A is 5-membered heterocyclyl containing at least one ring-forming O atom and containing at least one ring-forming N atom claim 1 , and Ring A is optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 R.10. The compound of wherein Ris H claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , or C(O)OR.11. The compound of wherein Ris H.12. The compound of wherein Ris H.13. The compound of wherein a and b are both 0.14. The compound of wherein Ris aryl claim 1 , cycloalkyl claim 1 , heteroaryl claim 1 , or heterocycloalkyl claim 1 , each optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 substituents independently selected from halo claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Chaloalkyl claim 1 , Chydroxyalkyl claim 1 , Cy claim 1 , CN claim 1 , NO claim 1 , OR claim 1 , SR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , C(O)OR claim 1 , OC(O)R claim 1 , OC(O)NRR claim 1 , NRC(O)NRR claim 1 , NRR claim 1 , NRC(O)R claim 1 , NRC(O)OR claim 1 , C(═NR)NRR claim 1 , NRC(═NR)NRR claim 1 , P(R) claim 1 , P( ...

Modulators of sperm hypermobility and uses thereof

The invention provides novel compositions and compounds that inhibit CatSper channel activity, that preferentially inhibits sperm hyperactivity over sperm motility, or both. The compounds of the invention are useful as contraceptive agents that may be adminstered to males, females, or concurrently to both sexual partners. The invention further provides methods of conducting drug discovery business and of conducting a reproductive medicine business. The invention also provides methods of identifying compounds that modulate sperm hypermotility.

N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase

The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.

1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3-Dioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. 1174-. (canceled)176. The method of claim 175 , wherein the antibody is an anti-CTLA-4 antibody.177. The method of claim 175 , wherein the antibody is an anti-PD-1 antibody.179. The method of claim 178 , wherein Ris NH.180. The method of claim 178 , wherein Ris Br.181. The method of claim 178 , wherein Ris F.182. The method of claim 178 , wherein n is 2.183. The method of claim 178 , wherein said compound is selected from:4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide;N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-({2-[(methylsulfonyl)amino]ethyl}amino)-1,2,5-oxadiazole-3-carboximidamide;4-({3-[(aminosulfonyl)amino]propyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide;N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-({3-[(methylsulfonyl)amino]propyl} amino)-1,2,5-oxadiazole-3-carboximidamide;4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-chloro-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide;N-(3-chloro-4-fluorophenyl)-N′-hydroxy-4-({2-[(methylsulfonyl)amino]ethyl}amino)-1,2,5-oxadiazole-3-carboximidamide;4-({3-[(aminosulfonyl)amino]propyl}amino)-N-(3-chloro-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide;N-(3-chloro-4-fluorophenyl)-N′-hydroxy-4-({3-[(methylsulfonyl)amino]propyl}amino)-1,2,5-oxadiazole-3-carboximidamide;4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-[4-fluoro-3-(trifluoromethyl)phenyl]-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide;N-[4-fluoro-3-(trifluoromethyl)phenyl]-N′-hydroxy-4-({2-[(methylsulfonyl)amino]ethyl}-amino)-1,2,5-oxadiazole-3-carboximidamide;4-({3-[(aminosulfonyl)amino]propyl}amino)-N-[4-fluoro-3-(trifluoromethyl)phenyl]-N′-hydroxy-1,2,5- ...

5-membered ring heteroaromatic derivatives having npy y5 receptor antagonistic activity

This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R 1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R 2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.

FUROXAN COMPOUND, AND MANUFACTURING METHOD FOR SAME

The present invention provides: a furoxan compound having a fluorine atom as a substituent group on the ring structure thereof; and a novel nitric oxide donor including the compound. The present invention relates to a fluorofuroxan compound represented by general formula (1) or (2). The compound of formula (1) can be manufactured by reacting a fluoride salt with a nitrofuroxan compound to substitute the nitro group with a fluoro group. The compound of formula (2) can be manufactured by subjecting the compounds of formula (1) to isomerization by irradiation with light. 2. A nitric oxide donor comprising the fluorofuroxan compound according to .5. The fluorofuroxan compound according to claim 1 ,{'sup': '1', 'wherein Rrepresents an alkyl group having 1 to 30 carbon atoms, an alkenyl group having 2 to 30 carbon atoms, an alkynyl group having 2 to 30 carbon atoms, or an aryl group having 4 to 30 carbon atoms.'}6. The fluorofuroxan compound according to claim 1 ,{'sup': '1', 'wherein Rrepresents an aryl group having 4 to 30 carbon atoms.'} The present invention relates to a novel furoxan compound and a method for manufacturing the same.Nitric oxide is one of neurotransmitters and is known to have vasodilatory action and memory enhancing action. For this reason, nitric oxide has been studied to apply to a drug for treating epilepsy or Alzheimer type dementia. Nitric oxide is also a central substance of action mechanism of nitroglycerin as a drug for angina pectoris and VIAGRA as a drug for erectile dysfunction.In recent years, furoxan (1,2,5-oxadiazole-2-oxide) has attracted attention as a compound that releases nitric oxide under physiological conditions and is expected as a new medical lead compound (for example, see Non-Patent Literatures 1 and 2).However, although the nitric oxide-releasing ability exhibited by the furoxan compound is largely dependent on the position and property of the substituent on the ring structure, only a limited number of methods for ...

Modulators of indoleamine 2,3-dioxygenase and methods of using the same

The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.

1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. 1174-. (canceled)175. A method of treating cervical cancer in a patient , comprising administering to said patient a therapeutically effective amount of a compound , which is 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1 ,2 ,5-oxadiazole-3-carboximidamide , or a pharmaceutically acceptable salt thereof , in combination with an antibody therapeutic , wherein the treating is inhibiting or ameliorating the cancer.176. The method of claim 175 , wherein the antibody therapeutic is an anti-PD-1 antibody.177. The method of claim 175 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.178. A method of treating cervical cancer in a patient claim 175 , comprising administering to said patient a therapeutically effective amount of a compound claim 175 , which is 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1 claim 175 ,2 claim 175 ,5-oxadiazole-3-carboximidamide in combination with an antibody therapeutic claim 175 , wherein the treating is inhibiting or ameliorating the cancer.179. The method of claim 178 , wherein the antibody therapeutic is an anti-PD-1 antibody.180. The method of claim 178 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.181. The method of claim 178 , wherein the compound and the antibody therapeutic are administered simultaneously.182. The method of claim 178 , wherein the compound and the antibody therapeutic are administered sequentially.183. The method of claim 179 , wherein the compound and the antibody therapeutic are administered simultaneously.184. The method of claim 179 , wherein the compound and the antibody therapeutic are administered sequentially.185. The ...

MODULATOR OF INDOLEAMINE 2,3-DIOXYGENASE, PREPARATION METHOD AND USE THEREOF

The present invention relates to a modulator of 1,2,5-oxadiazole indoleamine-(2,3)-dioxygenase, a preparation method and use thereof, more particularly to compounds of Formula I and Formula II, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, and their use in preparing drugs for treating cancers, neurodegenerative diseases, eye diseases, mental disorders, depression, anxiety disorders, Alzheimer's diseases and/or autoimmune diseases. Specific meanings of R substituents in Formula I and Formula II are consistent with the description of the specification. 5. The method according to claim 4 , wherein the solvent comprises one or more of methyl alcohol claim 4 , ethyl alcohol claim 4 , dichloromethane claim 4 , trichloromethane claim 4 , acetonitrile claim 4 , DMF claim 4 , DMA claim 4 , DMSO claim 4 , THF or toluene.6. The method according to claim 4 , wherein the reaction temperature ranges from 0° C. to 200° C.7. A pharmaceutical composition claim 1 , comprising the compound of Formula I and/or Formula II claim 1 , the isomer thereof claim 1 , the pharmaceutically acceptable salt or the pharmaceutically acceptable solvate thereof according to claim 1 , and a pharmaceutically acceptable carrier and/or auxiliary agent.8. A method for preventing and/or treating indoleamine-(2 claim 1 ,3)-dioxygenase-mediated disease in a subject comprising administering to the subject the compound of .9. The method according to claim 8 , wherein the indoleamine-(2 claim 8 ,3)-dioxygenase-mediated disease is cancer claim 8 , neurodegenerative disease claim 8 , eye disease claim 8 , mental disorder claim 8 , depression claim 8 , anxiety disorder claim 8 , Alzheimer's disease and/or autoimmune disease.10. A method of inhibiting indoleamine-(2 claim 1 ,3)-dioxygenase comprising contacting indoleamine-(2 claim 1 ,3)-dioxygenase the with the compound of .11. A method of reducing inflammation in a subject comprising administering to the ...

INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR, PREPARATION METHOD THEREFOR, AND APPLICATION

The present invention relates to an indoleamine 2,3-dioxygenase inhibitor having the structure of formula (I), a preparation method therefor, and an application. The IDO inhibitor is an N′-hydroxyl-N-phenylformamidine derivative, which has a high inhibitory activity on IDO, effectively inhibits IDO activity, and may also be used to inhibit patient immunosuppression. The inhibitor may be widely applied to treat or prevent cancers or tumors, viral infections, depression, neurodegenerative disorders, trauma, age-related cataracts, organ transplant rejection or autoimmune diseases, and has the potential to be developed into a new generation of immunosuppressors. 10. A pharmaceutical composition comprising a therapeutically effective amount of the compound of formula (I) claim 1 , the stereoisomer or the pharmaceutically acceptable salt thereof according to claim 1 , and a pharmaceutically acceptable carrier.1113.-. (canceled)14. A method for modulating the activity of indoleamine 2 claim 10 ,3-dioxygenase claim 10 , comprising contacting the pharmaceutical composition according to with indoleamine 2 claim 10 ,3-dioxygenase.15. A method for inhibiting immunosuppression in a subject claim 10 , comprising administering a therapeutically effective amount of the pharmaceutical composition according to to the subject.16. The method according to claim 14 , wherein the modulation is an inhibitory effect.17. A method for treating or preventing a cancer or tumor claim 10 , viral infection claim 10 , depression claim 10 , neurodegenerative disorder claim 10 , trauma claim 10 , age-related cataract claim 10 , organ transplant rejection or autoimmune disease in a subject claim 10 , comprising administering to the subject the pharmaceutical composition according to .18. The method according to claim 17 , wherein the cancer or tumor is selected from the group consisting of lung cancer claim 17 , bone cancer claim 17 , gastric cancer claim 17 , pancreatic cancer claim 17 , skin cancer ...

INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR, PREPARATION METHOD THEREFOR AND USE THEREOF

A compound is represented by formula (I). A pharmaceutical composition contains the compound of formula (I). The compound is used in the preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound exhibits inhibition effect on IDO protease and metabolizes stably in the body. The compound or pharmaceutical composition thereof can be used for preparing an IDO inhibitor drug, and can also be used for preparing a drug for preventing and/or treating diseases having IDO-mediated tryptophan metabolic pathway pathological features. 10. The use of compounds claim 1 , or optical isomers thereof claim 1 , or cis- and trans-isomers thereof claim 1 , or isotope compounds thereof claim 1 , or solvates thereof claim 1 , or pharmaceutically acceptable salts thereof claim 1 , or pro-drugs thereof claim 1 , or tautomers thereof claim 1 , or mesomers thereof claim 1 , or racemates thereof claim 1 , or enantiomers thereof claim 1 , or diastereoisomers thereof claim 1 , or mixtures thereof claim 1 , or metabolites thereof claim 1 , or metabolic precursors thereof according to claim 1 , in the preparation of drugs for the prevention and/or treatment of diseases with pathological characteristics of IDO mediated tryptophan metabolism pathway.11. The use according to claim 10 , characterized in that said diseases with pathological characteristics of IDO mediated tryptophan metabolism pathway are selected from cancer claim 10 , myelodysplastic syndrome claim 10 , Alzheimer's disease claim 10 , autoimmune disease claim 10 , depression claim 10 , anxiety disorder claim 10 , cataract claim 10 , psychological disorder and AIDS; in which said cancer is preferably breast cancer claim 10 , cervical cancer claim 10 , colon cancer claim 10 , lung cancer claim 10 , gastric cancer claim 10 , rectal cancer claim 10 , pancreatic cancer claim 10 , brain cancer claim 10 , skin cancer claim 10 , oral cancer claim 10 , prostate cancer claim 10 , bone cancer claim 10 , kidney cancer claim ...

PAIN-RELIEVING COMPOSITIONS AND USES THEREFOR

Compositions and methods are for inducing, promoting or otherwise facilitating pain relief. More particularly, sub-normovasodilatory doses of nitric oxide donors are used in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. In some applications of the method, nitric oxide donors can be administered by any suitable route so as to provide concentrations of NO that are about ½ to 10times those known to induce vasodilation in normal circulations. 125-. (canceled)271. A compound according to claim wherein one of Rand Ris —COH and the other is ethyl.281. A compound according to claim wherein one of Rand Ris —C(O)NHand the other is ethyl.291. A compound according to claim wherein one of Rand Ris —COH and the other is isopropyl.301. A compound according to claim wherein one of Rand Ris —CONHand the other is isopropyl.311. A compound according to claim wherein one of Rand Ris —COH and the other is 4-fluorophenyl.321. A compound according to claim wherein one of Rand Ris —C(O)CFand the other is phenyl.331. A compound according to claim wherein one of Rand Ris —COH and the other is isopropyl.341. A compound according to claim wherein one of Rand Ris —CONHand the other is 4-fluorophenyl.351. A compound according to claim wherein one of Rand Ris —CONHand the other is 4-methoxyphenyl.361. A compound according to claim wherein one of Rand Ris methyl and the other is Calkylphenyl substituted with hydroxyl.3711. A compound according to claim wherein the hydroxyl is substituted on the alkyl group.381. A compound according to claim wherein one of Rand Ris methyl and the other is ethyl substituted with a hydroxyl group.391. A compound according to claim wherein one of Rand Ris methyl and the other is —CHN(alkyl).4014. A compound according to claim wherein the —CHN(alkyl)is —CHN(ethyl). This application is a Continuation application of U.S. application Ser. No. 12/494,183, filed Jun. 29, 2009, which ...

SULFOXIMINE, SULFONIMIDAMIDE, SULFONDIIMINE AND DIIMIDOSULFONAMIDE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE

Provided are certain IDO inhibitors or pharmaceutically acceptable salts thereof which can inhibit enzymatic activity of indoleamine 2,3-dioxygenase (IDO) and may be useful for the treatment of diseases and disorders mediated by IDO. In addition, pharmaceutical compositions thereof and methods of use thereof are also provided. 3. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein L is selected from —(CH)— claim 1 , —CHCHCH— claim 1 , —CHCHCH— claim 1 , —(CH)— and —(CRR)O(CRR)—.4. (canceled)5. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein X is O.6. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein W is aryl claim 1 , wherein aryl is unsubstituted or substituted with at least one substituent independently selected from R.7. A compound of or a pharmaceutically acceptable salt thereof claim 6 , wherein W is phenyl claim 6 , wherein phenyl is unsubstituted or substituted with at least one substituent independently selected from halogen claim 6 , ethynyl claim 6 , CN and —CF.8. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein W is heteroaryl claim 1 , wherein heteroaryl is unsubstituted or substituted with at least one substituent independently selected from R.9. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen claim 1 , and/or Ris hydrogen claim 1 , and/or Ris hydrogen.1011.-. (canceled)12. A compound of or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently selected from hydrogen claim 1 , Calkyl and Ccycloalkyl claim 1 , wherein alkyl and cycloalkyl are independently unsubstituted or substituted with at least one substituent independently selected from R.13. A compound of or a pharmaceutically acceptable salt thereof claim 12 , wherein Ris selected from hydrogen and methyl.14. A compound of or a ...

INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR, METHOD FOR PREPARATION AND USE THEREOF

The present invention provides a novel indoleamine 2,3-dioxygenase inhibitor, a preparation method thereof, and a pharmaceutical composition, in which the definitions of n, Y, Z, R, R, R, and Rare as stated in the specification. Also provided is a use of the aforementioned compound and pharmaceutically acceptable salts and isomers thereof in the preparation of a drug for indoleamine 2,3-dioxygenase (IDO) related disease, specifically a use in the treatment of major diseases such as cancer, Alzheimer's, depression, cataract, etc. The compound of the invention has improved activity, potential medicinal value, and wide market prospects. 2. The compound claim 1 , the salt or isomer thereof according to claim 1 , characterized in that the groups Z and Rare taken together form a 5-8 membered heterocycloalkyl.3. The compound claim 1 , the salt or isomer thereof according to claim 1 , characterized in that Y claim 1 , Z and Rare taken together form a 5-8 membered heterocycloalkyl.8. A pharmaceutical composition claim 1 , which contains a therapeutically effective amount of the compound of formula I or formula II or the pharmaceutically acceptable salt or isomer thereof as an active ingredient claim 1 , and one or more pharmaceutically acceptable carriers claim 1 , diluents or excipients.9. A method of treating a disease associated with indoleamine 2 claim 1 ,3-dioxygenase claim 1 , which comprises administering a therapeutically effective amount of the compound according to or a salt or isomer thereof to a subject in need thereof.10. The method according to claim 9 , characterized in that the diseases is a tumor claim 9 , Alzheimer's disease claim 9 , depression claim 9 , cataract and the like.12. A method of treating a disease associated with indoleamine 2 claim 8 ,3-dioxygenase claim 8 , which comprises administering a therapeutically effective amount of the compound according to the pharmaceutical composition according to to a subject in need thereof.13. The method ...

NOVEL SUBSTITUTED SULFOXIMINE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS

Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein m is 0 claim 1 , 1 claim 1 , 2 or 3; p is 0 claim 1 , 1 or 2;{'img': {'@id': 'CUSTOM-CHARACTER-00008', '@he': '2.79mm', '@wi': '5.33mm', '@file': 'US20200095212A1-20200326-P00001.TIF', '@alt': 'custom-character', '@img-content': 'character', '@img-format': 'tif'}, '“” is a single bond;'}X is selected from —NH—, —S— and —O—;{'sup': '1', 'each occurrence of Ris independently selected from (a) hydrogen and (b) halogen;'}{'sup': '2', 'sub': '1-4', 'each occurrence of Ris independently selected from (a) hydrogen (b) —OH and (c) Calkyl;'}{'sup': '4', 'sub': '1-4', 'Ris selected from (a) hydrogen and (b) Calkyl;'}{'sup': '5', 'sub': 1-4', '3-6, 'Ris selected from (a) Calkyl optionally substituted with —OH and (b) Ccycloalkyl; and'}{'sup': '6', 'sub': 1-4', '2, 'Ris selected from (a) hydrogen, (b) Calkyl, (c) —CN and (d) —C(O)—NH.'}4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein:m is 2, 3 or 4;{'sup': '1', 'each occurrence of Ris independently selected from (a) hydrogen, (b) Cl and (c) F;'}{'sup': '2', 'each occurrence of Ris independently selected from (a) hydrogen, (b) —OH, (c) methyl, (d) ethyl and (e) propyl;'}{'sup': '5', 'Ris selected from (a) methyl, (b) ethyl and (c) propyl; and'}{'sup': '6', 'sub': '2', 'Ris selected from (a) hydrogen, (b) methyl, (c) ethyl, (d) —CN and (e) —C(O)—NH.'}9. The compound of claim 8 , or a pharmaceutically acceptable salt thereof claim 8 , wherein: q ...

Il-17a modulators and uses thereof

The disclosure herein provides compounds and pharmaceutical compositions for the modulation of IL-17A useful for the treatment of inflammatory conditions, such as psoriasis.

NOVEL SUBSTITUTED N'-HYDROXYCARBAMIMIDOYL-1,2,5-OXADIAZOLE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE IDO INHIBITORS

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 ,wherein m is 1 or 2; n is 1 or 2; and p is 0, 1 or 2;{'sup': a', 'b', 'a', 'a', 'b, 'sub': '1-6', 'W is selected from (a) —CRR— and (b) —NR—; wherein each occurrence of Rand Ris independently selected from the group consisting of (a) hydrogen and (b) Calkyl, optionally substituted with —OH;'} (a) hydrogen;', {'sub': '1-6', '(b) Calkyl, optionally substituted with one to three substituents independently selected from the group consisting of (i) —OH and (ii) halogen;'}, {'sub': '3-6', '(c) Ccycloalkyl, optionally substituted with —OH;'}, {'sub': 'q', 'sup': 'c', 'claim-text': (i) hydrogen,', {'sub': 1-6', '3-6, '(ii) —Calkyl, optionally substituted with one to three substituents independently selected from the group consisting of (1) halogen, (2) —OH, (3) —O-methyl and (4) —Ccycloalkyl,'}, {'sub': '1-6', '(iii) —O—Calkyl, and'}, {'sub': '1-6', '(iv) a 5- or 6-membered heterocyclyl, optionally substituted with one to four substituents independently selected from the group consisting of (1) halogen, (2) Calkyl and (3) —OH;'}], '(d) —(C═O)—(NH)—R, wherein q is 0 or 1; and Ris selected from the group consisting of, {'sub': 2', '2, '(e) —S(O)—NH;'}, {'sub': 2', '1-6, '(f) —S(O)—Calkyl; and'}, {'sub': 1-6', '1-6, '(g) a 4-, 5- or 6-membered heterocyclyl, optionally substituted with one to four substituents independently selected from the group consisting of (i) halogen, (ii) Calkyl, (iii) oxo and (iv) —C(O)—Calkyl, optionally substituted with ...

PAIN-RELIEVING COMPOSITIONS AND USES THEREFOR

Compositions and methods are for inducing, promoting or otherwise facilitating pain relief. More particularly, sub-doses of nitric oxide donors are used in the therapeutic management of vertebrate animals including humans, for the prevention or alleviation of pain, especially neuropathic pain. In some applications of the method, nitric oxide donors can be administered by any suitable route so as to provide concentrations of NO that are about ½ to 10times those known to induce vasodilation in normal circulations. 125.-. (canceled)27. The compound according to wherein one of Rand Ris methyl.28. The compound according to wherein one of Rand Ris methyl and the other is Calkylphenyl substituted with hydroxyl.29. The compound according to wherein the hydroxyl is substituted on the alkyl group.30. The compound according to wherein one of Rand Ris methyl and the other is ethyl substituted with hydroxyl.31. The compound according to wherein one of Rand Ris methyl and the other is —CHN(ethyl). This application is a Continuation Application of U.S. application Ser. No. 14/466,795, filed Aug. 22, 2014, which is a Continuation Application of U.S. application Ser. No. 12/494,183, filed Jun. 29, 2009, now issued as U.S. Pat. No. 8,822,509 on Sep. 2, 2014, which is a Continuation-in-Part Application of International Application No. PCT/AU2008/000003, filed Jan. 2, 2008, designating the U.S. and published in English on Jul. 10, 2008 as WO 2008/080194, which claims the benefit of Australian Application No. 2006907305, filed Dec. 29, 2006, Australian Application No. 2008903394, filed Jul. 2, 2008, Australian Application No. 2008904197, filed Aug. 15, 2008, and Australian Application No. 2009901445, filed Apr. 3, 2009, all of which are incorporated by reference in their entireties.This invention relates generally to compositions and methods for inducing, promoting or otherwise facilitating pain relief. More particularly, the present invention relates to the use of sub-normovasodilatory ...

NO- AND H2S- RELEASING COMPOUNDS

This disclosure relates to novel compounds containing an HS releasing moiety and a nitric oxide (NO) releasing moiety covalently linked with a core (e.g., a salicylic acid moiety) and the use of such compounds in treating inflammatory diseases, including cancers. Therapeutic potency of these compounds is significantly higher than NSAIDs containing a HS-releasing moiety alone (HS-NSAIDs) and NSAID containing a NO-releasing moiety alone (NO-NSAIDs). The compounds, in addition, exhibit reduced side effect, e.g., reduced stomach ulcers, upon administration. 171-. (canceled)89. A method of treating an inflammatory disease claim 72 , comprising administering to a subject in need thereof an effective amount of a compound of .90. The method of claim 89 , wherein the inflammatory disease is cancer claim 89 , rheumatoid arthritis claim 89 , intestine inflammation claim 89 , stomach ulcer claim 89 , a cardiovascular disease claim 89 , or a neurodegenerative disease.91. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient. The present application claims the benefit of U.S. Provisional Patent Applications 61/523,513, filed Aug. 15, 2011, 61/615,700, filed Mar. 26, 2012, and 61/635,624, filed Apr. 19, 2012. Each of the foregoing applications is herein incorporated by reference in its entirety.This invention relates to anti-inflammatory compounds capable of releasing NO and HS, and compositions and methods of using such compounds.Non-steroidal anti-inflammatory drugs (NSAIDs) are prototypical agents for treatment of inflammatory conditions. NSAIDs may also have utility as therapeutic agents against many forms of cancers. Reviewed in K. Kashfi, Anti-Inflammatory Agents as Cancer Therapeutics, pp. 31-89 in Contemporary Aspects of Biomedical Research: Drug Discovery, Advances in Pharmacol., S. Enna and M. Williams (ed.), 2009, vol. 57, Elsevier, Inc. Long-term use of NSAIDs, however, may lead to serious side effects including ...

BENZAMIDE COMPOUNDS AND THEIR USE AS HERBICIDES II

The invention relates to benzamides of formula I, 2. The compound as claimed in claim 1 , or an agriculturally suitable salt thereof claim 1 , where Q is Q.3. The compound as claimed in claim 1 , or an agriculturally suitable salt thereof claim 1 , where Q is Q.4. The compound as claimed in claim 1 , or an agriculturally suitable salt thereof claim 1 , where Q is Q.5. The compound as claimed in claim 1 , or an agriculturally suitable salt thereof claim 1 , where Q is Q.6. The compound as claimed in claim 1 , or an agriculturally suitable salt thereof claim 1 , where Ris selected from the group consisting of halogen claim 1 , nitro claim 1 , C-C-alkyl claim 1 , C-C-alkoxy-C-C-alkoxy-Z claim 1 , R—S(O)—Z.7. The compound as claimed in claim 6 , or an agriculturally suitable salt thereof claim 6 , where Ris selected from the group consisting of halogen and C-C-alkyl.8. The compound as claimed in claim 1 , or an agriculturally suitable salt thereof claim 1 , where Ris RRNC(O)NR—Z claim 1 , where Ris selected from the group consisting of hydrogen and C-C-alkyl.9. The compound as claimed in claim 1 , or an agriculturally suitable salt thereof claim 1 , where Zin Ris a covalent bond and Rand Rindependently of each other are selected from the group consisting of C-C-alkyl claim 1 , C-C-cycloalkyl claim 1 , C-C-cycloalkyl-C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , phenyl claim 1 , and heterocyclyl claim 1 , where heterocyclyl is a 5- or 6-membered monocyclic saturated claim 1 , partially unsaturated or aromatic heterocycle claim 1 , which contains 1 claim 1 , 2 claim 1 , 3 or 4 heteroatoms as ring members claim 1 , which are selected from the group consisting of O claim 1 , N and S claim 1 , where phenyl and heterocyclyl are unsubstituted or substituted by 1 claim 1 , 2 claim 1 , 3 or 4 groups claim 1 , which are identical or different and selected from the group consisting of halogen claim 1 , C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-alkoxy and C-C-haloalkoxy.10. The ...

Azasteroidal Mimics

An azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic is formed via an oxocycloalkenyl isoxazolium anhydrobase and its dimer. The dimer can be used to form mono- and dihydrazones, which can be an azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic. A method of preparation of the dimer and the azasteroid mimic or an intermediate for the preparation of an azasteroid and azasteroid mimic occurs with hydrazonation and, optionally, a subsequent dehydrazonation. The dimer can be converted by inserting a nitrogen atom into the six membered ring of to a C-17 position cyclohexenone moiety of the dimer to yield a reduced tetrazolo[1,5-a]azepin-8-yl group. A subsequent hydrozone formation at a benzylic ketone can be carried out to generate an azasteroid mimic with a (triazol-4-yl)imino substituent. Monohydrazones can be converted to their thione equivalents.

INDOLEAMINE-2,3-DIOXYGENASE INHIBITOR AND PREPARATION METHOD THEREFOR

Disclosed are a compound represented by general formula I and a preparation method therefor. The compound can be used as indoleamine-2,3-dioxygenase inhibitor to prepare medicines for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases. 3. The compound represented by formula (I) of claim 2 , wherein Ris C-Calkyl;{'sup': '2', 'Ris H or —CN;'}{'sup': 3', '4, 'Rand Rare each independently H;'}{'sup': 9', '9, 'sub': 6', '10', '1', '6', '1', '6', '3', '5, 'Ris C-Caryl, five or six membered heteroaryl; Rcan be substituted with one or more substituents selected from the group consisting of: halogen, C-Calkyl, C-Calkoxy, hydroxy, amino, nitro, aldehyde group, —CF, —CN, —SF.'}4. The compound represented by formula (I) of claim 3 , wherein Ris C-Calkyl;{'sup': 9', '9, 'sub': 6', '10', '1', '6', '1', '6', '3', '5, 'Ris C-Caryl, five or six membered heteroaryl; Rcan be substituted with one or more substituents selected from the group consisting of: halogen, C-Calkyl, C-Calkoxy, hydroxy, —CF, —CN, —SF.'}6. The compound represented by formula (I) of claim 1 , wherein the compound is:(±)(Z)—N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-((2-(thio-methyl sulfoxide imine) ethyl)amino)-1,2,5-oxadiazole-3-carboxamidine;(+)(Z)—N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-((2-(thio-methyl sulfoxide imine) ethyl)amino)-1,2,5-oxadiazole-3-carboxamidine;(−) (Z)—N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-((2-(thio-methyl sulfoxide imine) ethyl)amino)-1,2,5-oxadiazole-3-carboxamidine;(±)(Z)—N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-((3-(thio-methyl sulfoxide imine) propyl)amino)-1,2,5-oxadiazole-3-carboxamidine;(+)(Z)—N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-((3-(thio-methyl sulfoxide imine) propyl)amino)-1,2,5-oxadiazole-3-carboxamidine;(−)(Z)—N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-((3-(thio-methyl sulfoxide imine) propyl)amino)-1,2,5-oxadiazole-3-carboxamidine;(±)(Z)—N-(3-bromo-4-fluorophenyl)-N′-hydroxy-4-((4-(thio-methyl sulfoxide imine) butyl)amino)-1,2,5-oxadiazole-3-carboxamidine ...

Herbicidally Active Arylcarboxylic Acid Amides

Benzamides of the general formula (I) are described as herbicides. 3. A herbicidal composition comprising a herbicidally active content of at least one compound of the formula (I) or salt as claimed in .4. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.5. A method of controlling unwanted plants claim 1 , comprising applying an effective amount of at least one compound of formula (I) or salt as claimed in or a herbicidal composition thereof to one or more plants or to a site of unwanted vegetation.6. A product comprising a compound of formula (I) or salt as claimed in or a herbicidal composition thereof for controlling one or more unwanted plants.7. The product as claimed in claim 6 , wherein the compound of formula (I) or salt is used for controlling one or more unwanted plants in one or more crops of useful plants.8. The product as claimed in claim 7 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of the herbicides, especially that of the herbicides for selective control of broad-leaved weeds and weed grasses in crops of useful plants.WO 2012/028579 A1 discloses N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides and use thereof as herbicides. WO 2012/126932 A1 describes N-(1,3,4-oxadiazol-2-yl)arylcarboxamides and use thereof as herbicides. The active ingredients described therein do not always exhibit sufficient activity against harmful plants and/or some do not have sufficient compatibility with some important crop plants such as cereal species, corn and rice.It is an object of the present invention to provide alternative herbicidally active ingredients. This object is achieved by the arylcarboxamides of the invention that are described hereinafter, which bear an alkyl or cycloalkyl radical in the 2 position, a sulfur radical in the 3 position and a cycloalkyl radical in the 4 position.The present invention thus provides arylcarboxamides of the formula (I) ...

SUBSTITUTED OXADIAZOLE CHEMICAL COMPOUND AND COMPOSITION CONTAINING SAID CHEMICAL COMPOUND AND USE THEREOF

Provided are a substituted oxadiazole chemical compound and composition containing said chemical compound and use thereof; said substituted oxadiazole chemical compound is the oxadiazole chemical compound as represented by formula (I), or its crystalline form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate, or solvent compound. The disclosed substituted oxadiazole chemical compound and composition containing said chemical compound are capable of inhibiting indoleamine 2,3-dioxygenase; it also has better pharmacokinetic parameter attributes and is capable of improving the drug concentration of the chemical compound in an animal body, thus improving the therapeutic efficacy and safety of the drug. 113.. (canceled)15. The substituted oxadiazole compound according to claim 14 , wherein R claim 14 , R claim 14 , and Rare each independently deuterium or hydrogen.16. The substituted oxadiazole compound according to claim 14 , wherein Rand Rare each independently deuterium or hydrogen.17. The substituted oxadiazole compound according to claim 14 , wherein Rand Rare each independently deuterium or hydrogen.18. The substituted oxadiazole compound according to claim 14 , wherein Rand Rare deuterium.19. The substituted oxadiazole compound according to claim 14 , wherein at least one of R claim 14 , R claim 14 , and Ris deuterium.20. The substituted oxadiazole compound according to claim 18 , wherein at least one of R claim 18 , R claim 18 , and Ris deuterium.21. The substituted oxadiazole compound according to claim 14 , wherein Rand Rare deuterium.22. The substituted oxadiazole compound according to claim 18 , wherein Rand Rare deuterium.23. The substituted oxadiazole compound according to claim 19 , wherein Rand Rare deuterium.24. The substituted oxadiazole compound according to claim 20 , wherein Rand Rare deuterium.30. A pharmaceutical composition claim 20 , comprising:{'claim-ref': {'@idref': 'CLM-00014', 'claim 14'}, 'the substituted oxadiazole compound ...

SUBSTITUTED HYDOXAMIC ACIDS AND USES THEREOF

This invention provides compounds of formula (I): 2. The compound of claim 1 , wherein G is —R claim 1 , —V—R claim 1 , —V-L-R claim 1 , -L-V—R claim 1 , or -L-R.3. The compound of claim 2 , wherein:{'sup': 2a', '1, 'Ris R;'}{'sup': '2b', 'Ris G;'}{'sup': 2c', '1, 'Ris R; and'}{'sup': '2d', 'sub': '1', 'Ris R.'}4. The compound of claim 2 , wherein:{'sup': 2a', '1, 'Ris R;'}{'sup': 2b', '1, 'Ris R;'}{'sup': '2c', 'Ris G; and'}{'sup': 2d', '1, 'Ris R.'}5. The compound of claim 2 , wherein:{'sub': 1', '1, 'sup': 3', '3', '3, 'G is —V—R, -L-R, or —R;'}{'sub': 1', '2', '2', '2, 'Lis —CH— or —CHCH—; and'}{'sub': 1', '2, 'sup': 4a', '4a', '4a', '4a', '4a', '4a', '4a, 'Vis —N(R)—, —N(R)—C(O)—, —C(O)—N(R)—, —N(R)—SO—, —O—, —N(R)—C(O)—O—, or —N(R)—C(O)—N(R)—.'}6. The compound of claim 2 , wherein:{'sup': '1a', 'each occurrence of Ris independently hydrogen, fluoro, trifluoromethyl, or methyl;'}{'sup': '1b', 'each occurrence of Ris hydrogen;'}{'sup': '1c', 'Ris hydrogen, hydroxy, fluoro, trifluoromethyl, or methyl;'}{'sup': '1', 'each occurrence of Ris independently hydrogen, chloro, fluoro, cyano, hydroxy, methoxy, ethoxy, trifluoromethyl, methyl, or ethyl.'}7. The compound of claim 2 , wherein:{'sup': 3', '5dd, 'each substitutable carbon chain atom in Ris unsubstituted or substituted with 1-2 occurrences of R;'}{'sup': 3', '5', '5aa, 'sub': '2', 'each substitutable saturated ring carbon atom in Ris unsubstituted or substituted with ═O, ═C(R), or —R;'}{'sup': 3', '5a, 'each substitutable unsaturated ring carbon atom in Ris unsubstituted or is substituted with —R;'}{'sup': 3', '9b, 'claim-text': [{'sup': 5a', '5', '5', '5', '5', '6', '6', '6', '4', '4', '4', '6', '4', '4', '4', '6', '4', '6', '4', '4', '6', '4', '4', '5a, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '1-6, 'each Ris independently halogen, —NO, —CN, —C(R)═C(R), —C≡C—R, —OR, —SR, —S(O)R, —SOR, —SON(R), —N(R), —NRC(O)R, —NRC(O)N(R), —NRCOR, —OC(O)N(R), —C(O)R, —C(O)N(R), —N(R)SOR, —N(R) ...

BENZENESULFONAMIDE DERIVATIVES AS INVERSE AGONISTS OF RETINOID-RELATED ORPHAN RECEPTOR GAMMA (ROR GAMMA (T))

Benzenesulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonist of retinoid-related orphan receptor gamma (RORγt) are described. A pharmaceutical composition including such compounds, as well as the use thereof for the topical and/or oral treatment of RORγt receptor-medicated inflammatory diseases, in particular acne, psoriasis and/or atopic dermatitis are also described. 3. Compound as claimed in or , characterized in that L represents a single bond.10. Compound as claimed in any one of the preceding claims , as a medicament.11. Compound as claimed in any one of the preceding claims , for its use in the treatment of inflammatory disorders and/or autoimmune diseases mediated by the RORγt receptor.12. Compound as claimed in claim 10 , for its use in the treatment of acne.13. Compound as claimed in claim 10 , for its use in the treatment of psoriasis.14. Pharmaceutical composition comprising one or more compounds as defined in any one of to .15. Pharmaceutical composition as claimed in claim 14 , characterized for its use for treating inflammatory disorders and/or autoimmune diseases mediated by the RORγt receptor claim 14 , especially acne claim 14 , atopic dermatitis and/or psoriasis. The present invention relates to particular sulfonamide derivatives, to the pharmaceutically acceptable addition salts thereof, hydrates thereof and/or solvates thereof, and also to the use thereof as inverse agonist of the retinoid-related orphan receptor gamma RORγt.The invention also relates to a pharmaceutical composition comprising such compounds and also to the use thereof for the topical and/or oral treatment of inflammatory diseases mediated by the RORγt receptors, especially acne, atopic dermatitis and/or psoriasis.The nuclear receptors form a large family (known as a superfamily) of transcription factors which correspond to proteins that are capable of being ...

1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. 1174-. (canceled)175. A compound , which is 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1 ,2 ,5-oxadiazole-3-carboximidamide , wherein one or more hydrogen atoms are replaced by deuterium; or a pharmaceutically acceptable salt thereof.176. A pharmaceutical composition comprising the compound of claim 175 , or a pharmaceutically acceptable salt thereof claim 175 , and a pharmaceutically acceptable excipient or carrier.177. A compound claim 175 , which is 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1 claim 175 ,2 claim 175 ,5-oxadiazole-3-carboximidamide claim 175 , wherein one or more hydrogen atoms are replaced by deuterium.178. A pharmaceutical composition comprising the compound of claim 177 , or a pharmaceutically acceptable salt thereof claim 177 , and a pharmaceutically acceptable excipient or carrier. This application is a continuation of U.S. Ser. No. 15/422,876, filed Feb. 27, 2017, U.S. Ser. No. 15/093,420, filed Apr. 7, 2016, which is a continuation of U.S. Ser. No. 14/661,191, filed Mar. 18, 2015, which is a continuation of U.S. Ser. No. 14/322,362, filed Jul. 2, 2014, which is a continuation of U.S. Ser. No. 13/294,711, filed Nov. 11, 2011, which is a divisional of U.S. Ser. No. 12/498,782, filed Jul. 7, 2009, which claims the benefit of U.S. Ser. No. 61/078,876, filed Jul. 8, 2008 and U.S. Ser. No. 61/150,873, filed Feb. 9, 2009, the disclosures of each of which are incorporated herein by reference in their entireties.The present invention is directed to 1,2,5-oxadiazole derivatives which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other ...

Amide compounds, methods for preparation, and use thereof as agents for the treatment and prevention of diseases caused by rna- and/or dna-containing viruses, and concomitant diseases

The present invention relates to medicine and includes a method for preventing and treating diseases caused by RNA- and DNA-containing viruses, and concomitant diseases, wherein the method comprises the use of an effective amount of compounds of general formula I or pharmaceutically acceptable salts thereof. The invention also relates to methods for preparing said compounds, pharmaceutical compositions for the prevention or treatment of diseases caused by RNA- and DNA-containing viruses, said compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable salt thereof. The invention addresses the object of providing a novel agent effective in the treatment of diseases caused by an RNA-containing virus belonging to the Enterovirus, Metapneumovirus, Pneumovirus, Respirovirus, or Alfa-coronavirus genus, and/or by a DNA-containing virus belonging to the Adenoviridae and/or Herpesviridae family, and in the prevention and treatment of asthma exacerbation, chronic obstructive pulmonary disease, mucoviscidosis, conjunctivitis, gastroenteritis, hepatitis, myocarditis; in the prevention and treatment of rhinorrhea, acute and infectious rhinitis, pharyngitis, nasopharyngitis, tonsillitis, laryngitis, laryngotracheitis, laryngotracheobronchitis, bronchitis, bronchiolitis, pneumonia, or airway obstructive syndrome.

Radiofluorinated carboximidamides as ido targeting pet tracer for cancer imaging

Radiofluorinated carboximidamides are disclosed as selective IDO enzyme radioligands and generate specific binding in accordance with IDO expression in vitro. MicroPET experiments indicate [18F]IDO49 specifically accumulate in IDO-expressing tumors which confirmed by Western blot and IHC analysis supported. Using Hela tumor bearing models with IFN-γ treatment confirmed that [18F]IDO49 accumulation in the IFN-γ treatment tumor mouse. These results can have implications that [18F]IDO49 has substantial potential as an imaging agent that targets IDO in tumors.

HERBICIDALLY ACTIVE BENXZOIC ACID AMIDES

The invention relates to benzoic acid amides of general formula (I) as herbicides. In formula (I) X, Z and R represent radicals such as alkyl and cycloalkyl. Q represents a 5-membered heterocycle. 3. A herbicidal composition comprising a herbicidally active content of at least one compound of formula (I) or salt as claimed in .4. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.5. A method of controlling unwanted plants claim 1 , comprising applying an effective amount of at least one compound of formula (I) or salt as claimed in or a herbicidal composition thereof to one or more plants or to a site of the unwanted vegetation.6. A product comprising a compound of formula (I) or salt as claimed in or a herbicidal composition thereof for controlling one or more unwanted plants.7. A product as claimed in claim 6 , wherein the compound of formula (I) or salt is used for controlling one or more unwanted plants in one or more crops of useful plants.8. Product as claimed in claim 7 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of the herbicides, especially that of the herbicides for selective control of broad-leaved weeds and weed grasses in crops of useful plants.WO 2011/035874 A1 discloses N-(1,2,5-oxadiazol-3-yl)benzamides and use thereof as herbicides. WO 2012/028579 A1 describes N-(tetrazol-5-yl)- and N-(triazole-5-yl)arylcarboxamides and their use as herbicides. WO 2012/126932 A1 describes N-(1,3,4-oxadiazol-2-yl)benzamides and use thereof as herbicides. The active ingredients described therein do not always exhibit sufficient activity against harmful plants and/or some do not have sufficient compatibility with some important crop plants such as cereal species, corn and rice. DATABASE PubChem Compound [Online], NCBI; 30 Nov. 2012, Database accession no. CID 67053732 cites the compound 2,4-dimethyl-3-methylsulfonylbenzoic acid.It is an object of the present invention ...

INGENOL-3-ACYLATES III AND INGENOL-3-CARBAMATES

The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis. 146-. (canceled)48. A compound according to ;wherein R is heteroaryl which may optionally be substituted by one or more substituents independently selected from R7,or R is heterocycloalkyl or heterocycloalkenyl, each of which may optionally be substituted by one or more substituents independently selected from R8;R7 represents halogen, cyano, hydroxyl;{'sub': 1', '4', '2', '4', '3', '7, 'or R7 represents (C-C)alkyl, (C-C)-alkenyl, (C-C)-cycloalkyl, heterocycloalkyl, aryl, heteroaryl, each of which is optionally substituted by one or more substituents independently selected from R9;'}or R7 represents —NRaCORb, —CONRaRb, —COORc, —OCORa, —ORa, —OCONRaRb, —NRaCOORb, —NRaCONRaRb, —NRaSO2NRaRb, —NRaSO2Rb, —SO2NRaRb, —SO2Ra, —S(O)Ra, —SRa;{'sub': 1', '4', '1', '4, 'R9 represents halogen, cyano, hydroxy, (C-C)alkyl, halo(C-C)alkyl, —NRaCORb, —COORc, —OCORa, —CONRaRb, —OCONRaRb, —NRaCOORb, —NRaCONRaRb, —NRaSO2NRaRb, —NRaSO2Rb, —SO2NRaRb, —SO2Ra, —S(O)Ra, —ORa, —SRa, ═O;'}R8 represents halogen, cyano, hydroxyl;{'sub': 1', '4', '2', '4', '3', '7, 'or R8 represents (C-C)-alkyl, (C-C)alkenyl, aryl, heteroaryl, (C-C)-cycloalkyl, heterocycloalkyl, each of which is optionally substituted by one or more substituents independently selected from R10,'}or R8 represents —NRaCORb, —COORc, —OCORa, —CONRaRb, —OCONRaRb, —NRaCOORb, —NRaCONRaRb, —NRaSO2NRaRb, —NRaSO2Rb, —SO2NRaRb, —SO2Ra, —S(O)Ra ...

1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

Formulations and electronic devices

A formulation comprising at least one solvent and at least two different functional compounds of formula (I) AB] k   (I) wherein A is a functional structural element, the structural element serving as host material, as a unit that has hole-injection and/or hole-transport properties, as a unit t at has electron-injection and/or electron-transport properties, as a unit which has light-emitting properties, or as a unit which improves the transfer from the singlet state to the triplet state of light-emitting compounds; B is a solubility-promoting structural element; and k is an integer in the range from 1 to 20; the molecular weight of the functional compound is at least 550 g/mol, and the solubility-promoting structural element B conforms to the general formula (L-I)

BICYCLIC ARYLCARBOXYLIC ACID AMIDES AND THEIR USE AS HERBICIDES

Bicyclic arylcarboxamides of the general formula (I) are described as herbicides. 4. A herbicidal composition claim 1 , comprising a herbicidally active content of at least one bicyclic arylcarboxamide of the formula (I) or salt as claimed in .5. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.6. The herbicidal composition as claimed in claim 4 , comprising at least one further pesticidally active substance from the group consisting of insecticides claim 4 , acaricides claim 4 , herbicides claim 4 , fungicides claim 4 , safeners claim 4 , and growth regulators.7. The herbicidal composition as claimed in claim 6 , comprising a safener.8. The herbicidal composition as claimed in claim 7 , comprising cyprosulfamide claim 7 , cloquintocet-mexyl claim 7 , mefenpyr-diethyl or isoxadifen-ethyl.9. A method for controlling unwanted plants claim 1 , comprising applying an effective amount of at least one bicyclic arylcarboxamide of the formula (I) or salt as claimed in or a herbicidal composition thereof to the plants or to a site of unwanted vegetation.10. A product comprising a bicyclic arylcarboxamide of the formula (I) or salt as claimed in or herbicidal composition thereof for controlling unwanted plants.11. A product as claimed in claim 10 , wherein the bicyclic arylcarboxamide of the formula (I) or salt is used for controlling unwanted plants in one or more crops of useful plants.12. A product as claimed in claim 11 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of the herbicides, especially that of the herbicides for selective control of broad-leaved weeds and weed grasses in crops of useful plants.WO 2013/064457 A1 discloses N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides and nicotinamides that bear particular substituents in the 5 position of the aryl ring as herbicides. WO2013092834 A1 discloses N-(tetrazol-5-yl)arylcarboxamides and nicotinamides that are ...

Ingenol-3-acylates iii and ingenol-3-carbamates

The invention relates to compounds of general formula I wherein R is heteroaryl optionally substituted by R7; or R is heterocycloalkyl or heterocycloalkenyl, optionally substituted by R8; or R is X wherein X is —NR11R12; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.

Sulfonyl amidine as indoleamine-2,3-dioxygenase inhibitor, and preparation method therefor and use thereof

Provided in the present application are a sulfonyl amidine as represented by formula (I) as an indoleamine-2,3-dioxygenase inhibitor, and a preparation method therefor and the use thereof. The compound of formula (I) in the present application can be used as an indoleamine-2,3-dioxygenase inhibitor in the preparation of a drug for preventing and/or treating indoleamine-2,3-dioxygenase-mediated diseases.

MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF USING THE SAME

The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. 137-. (canceled)39. The compound of claim 38 , wherein a is 0 and b is 0.40. The compound of claim 38 , which is 3-(4-amino-1 claim 38 ,2 claim 38 ,5-oxadiazol-3-yl)-4-(3-bromo-4-fluorophenyl)-1 claim 38 ,2 claim 38 ,4-oxadiazol-5 (4H)-one.42. The compound of claim 41 , wherein a is 0 and b is 0.43. The compound of claim 41 , wherein Ris H.44. The compound of claim 41 , which is 4-amino-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1 claim 41 ,2 claim 41 ,5-oxadiazole-3-carboximidamide. This application is a continuation of U.S. Ser. No. 15/632,986 filed on Jun. 26, 2017, which is a continuation of U.S. Ser. No. 14/478,622 filed on Sep. 5, 2014, which is a continuation of U.S. Ser. No. 13/734,263 filed on Jan. 4, 2013, now U.S. Pat. No. 8,846,726, which is a continuation of U.S. Ser. No. 13/220,406 filed on Aug. 29, 2011, now U.S. Pat. No. 8,372,870, which is a divisional of U.S. Ser. No. 11/430,441, filed May 9, 2006, now U.S. Pat. No. 8,034,953, which claims the benefit of U.S. Provisional Application No. 60/679,507, filed May 10, 2005, each of which is incorporated herein by reference in its entirety.The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Tryptophan (Trp) is an essential amino acid required for the biosynthesis of proteins, niacin and the neurotransmitter 5-hydroxytryptamine (serotonin). The enzyme indoleamine 2,3-dioxygenase (also known as INDO or IDO) catalyzes the first and rate limiting step in the degradation of L-tryptophan to N-formyl-kynurenine. In human cells, a depletion of Trp resulting from IDO activity is a prominent gamma interferon (IFN-γ)-inducible antimicrobial effector mechanism. IFN-γ stimulation induces activation of IDO, which leads to a depletion of Trp, thereby arresting the growth of Trp-dependent ...

1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

NOVEL VIRAL REPLICATION INHIBITORS

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds. 6. The compound of claim 1 , wherein{'sup': 1', '1a', '1b', '1c', '2', '3', '3', '4', '5', '4', '5', '4', '2', '4', '2', '3', '2', '4', '5, 'sub': 2', '2', '1-6', '1-6', '1-6, 'claim-text': {'sub': 1-6', '1-6', '2', '3', '3', '2', '1-4', '2', '1-4', '1-6, 'and wherein said Calkyl, aryl, and heterocycle are optionally substituted with one, two, or three substituents selected from hydroxyl, ═O, —O—C(O)Me, cyano, —C(O)OH, —C(O)OCalkyl, —NH, —NHCH; —N(CH), —NH—C(═O)O—Calkyl; —S(O)Calkyl, and —O—Calkyl;'}, 'each Z, Z, Z, and Zis independently selected from the group consisting of halogen, hydroxyl, —OZ, —O—C(═O)Z, ═O, —S(═O)Z, —S(═O)NZZ, trifluoromethyl, trifluoromethoxy, —NZZ, —NZC(═O)Z, —NZC(═O)—OZ, cyano, —C(═O)Z, —C(═O)OZ, —C(═O)NZZ, Calkyl, heteroCalkyl, aryl, heterocycle, and heterocycle-Calkyl;'}{'sup': '2', 'sub': 1-6', '1-6, 'claim-text': {'sub': 1-6', '1-6', '2', '1-4', '1-4', '2', '3', '2, 'wherein said Calkyl, and aryl, are optionally substituted with one, two, or three substituents selected from hydroxyl, halogen, difluoromethyl, —O—Calkyl, —S(═O)Calkyl, —C(═O)OH, —C(═O)O—Calkyl, —NH, and —N(CH), pyrrolidinyl, piperidinyl, and piperazinyl;'}, 'each Zis independently selected from ...

Substituted ketoxime benzoylamides

What are described are substituted ketoxime benzoylamides of the general formula (I) as herbicides. In this formula (I), R 1′ , R 2′ , X, Y and W are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is an oxadiazole, tetrazole or triazole radical.

NOVEL SUBSTITUTED N'-HYDROXYCARBAMIMIDOYL-1,2,5-OXADIAZOLE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE (IDO) INHIBITORS

Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein: m is 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3; n is 1 claim 1 , 2 claim 1 , or 3;X is —S— or —NH—; (a) hydrogen,', {'sub': 1-6', '2, '(b) Calkyl, optionally substituted with one to three substituents independently selected from the group consisting of (i) —OH, (ii) halogen, and (iii) —NH,'}, {'sub': 3-6', '2', '2', '2', '1-6, '(c) Ccycloalkyl, optionally substituted with one to three substituents independently selected from the group consisting of (i) NH, (ii) —NH—S(O)—NHand (iii) —NH—C(O)—Calkyl, optionally substituted with —OH,'}, {'sub': '4-6', '(d) Ccycloalkenyl, optionally substituted with an oxo,'}, {'sup': a', 'a, 'claim-text': (i) hydrogen,', {'sub': 1-6', '2', '1-6, '(ii) —Calkyl, optionally substituted with one to three substituents independently selected from the group consisting of (1) halogen, (2) —OH and (3) —S(O)—Calkyl,'}, {'sub': '1-6', '(iii) —Calkoxy, and'}, {'sub': '3-6', '(iv) —Ccycloalkyl,'}], '(e) —(C═O)—NH—R, wherein Ris selected from the group consisting of, {'sup': x', 'y', 'x', 'y, 'claim-text': (i) hydrogen,', {'sup': a', 'a, 'sub': 1-6', '2', '1-6', '3-6, '(ii) —(C═O)—R, wherein Ris selected from the group consisting of (1) hydrogen, and (2) —Calkyl, optionally substituted with one to three substituents independently selected from halogen and —CN, (3) —NH, (4) —NH—Calkyl, optionally substituted with —OH, —O-methyl, or —CN, and (5) —NH—Ccycloalkyl,'}, {'sub': 2', '2, '(iii) —S(O)—NH ...

PROCESS FOR THE SYNTHESIS OF AN INDOLEAMINE 2,3-DIOXYGENASE INHIBITOR

The present application is directed to processes and intermediates for making 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1,2,5-oxadiazole-3-carboximidamide, which is an inhibitor of indoleamine 2,3-dioxygenase, useful in the treatment of cancer and other disorders. 166-. (canceled)68. The compound of claim 67 , or a salt thereof claim 67 , wherein Ris Calkenyl-Calkyl or phenyl-Calkyl claim 67 , wherein said phenyl-Calkyl is optionally substituted by 1 claim 67 , 2 claim 67 , or 3 independently selected Calkoxy groups.69. The compound of claim 67 , or a salt thereof claim 67 , wherein Ris allyl.70. The compound of claim 67 , or a salt thereof claim 67 , wherein Ris 4-methoxybenzyl.71. The compound of claim 67 , or a salt thereof claim 67 , wherein Ris Calkyl.72. The compound of claim 67 , or a salt thereof claim 67 , wherein Ris Calkyl.73. The compound of claim 67 , or a salt thereof claim 67 , wherein Ris tert-butyl.74. The compound of claim 67 , or a salt thereof claim 67 , wherein Ris butyl.75. The compound of claim 67 , wherein the compound of Formula F16 is tert-butyl allyl(N-allyl-N-(2-(4-(4-(3-bromo-4-fluorophenyl)-5-oxo-4 claim 67 ,5-dihydro-1 claim 67 ,2 claim 67 ,4-oxadiazol-3-yl)-1 claim 67 ,2 claim 67 ,5-oxadiazol-3-ylamino)ethyl)sulfamoyl)carbamate claim 67 , or a salt thereof.76. The compound of claim 67 , wherein the compound of Formula F16 is tert-butyl allyl(N-allyl-N-(2-(4-(4-(3-bromo-4-fluorophenyl)-5-oxo-4 claim 67 ,5-dihydro-1 claim 67 ,2 claim 67 ,4-oxadiazol-3-yl)-1 claim 67 ,2 claim 67 ,5-oxadiazol-3-ylamino)ethyl)sulfamoyl)carbamate.77. The compound of claim 67 , wherein the compound of Formula F16 is tert-butyl (4-methoxybenzyl)-(N-(4-methoxybenzyl)-N-(2-(4-(4-(3-bromo-4-fluorophenyl)-5-oxo-4 claim 67 ,5-dihydro-1 claim 67 ,2 claim 67 ,4-oxadiazol-3-yl)-1 claim 67 ,2 claim 67 ,5-oxadiazol-3-ylamino)ethyl)sulfamoyl)carbamate claim 67 , or a salt thereof.78. The compound of claim 67 , wherein the compound of ...

SYNTHESIS OF 3,4-BIS(4-NITRO-1,2,5-OXADIAZOL-3-YL)-1,2,5-OXADIAZOLE-N-OXIDE (DNTF) USING 3-CHLOROCARBOHYDROXYMOYL-4-NITRO-1,2,5-OXADIAZOLE

A novel method for preparing 3-chlorocarbohydroxymoyl-4-nitro-1,2,5-oxadiazole by reacting 4-amino-3-chlorocarbohydroxymoyl-1,2,5-oxadiazole with HOand a tungsten based catalyst and use of the prepared 3-chlorocarbohydroxymoyl-4-nitro-1,2,5-oxadiazole for synthesizing 3,4-Bis(4-nitro-1,2,5-oxadizaol-3-yl)-1,2,5-oxadiazole-N-oxide (DNTF). 1. The process for preparing 3-chlorohydroximoyl-4-nitro-1 ,2 ,5-oxadiazole comprising the steps of:{'sub': 2', '2, '(a) reacting 4-amino-3-chlorocarbohydroxymoyl-1,2,5-oxadiazole in the presence of a tungsten based catalyst and aqueous HO;'}(b) heating the solution at greater than 30° C. to produce 3-amino-4-chlorohydroximoyl 1-2,4-oxadiazole in solution;(c) isolating the 3-chiorohydroximoyl-4-nitro-1,2,5-oxadiazole from the solution.2. The process of wherein the tungsten based catalyst is (Bmim)WO.3. The compound claim 1 , 3-chlorohydroximoyl-4-nitro-1 claim 1 ,2 claim 1 ,5-oxadiazole claim 1 , prepared according to the process of .4. A process for preparing 3 claim 1 ,4-Bis(4-nitro-1 claim 1 ,2 claim 1 ,5-oxadizaol-3-yl)-1 claim 1 ,2 claim 1 ,5-oxadiazole-N-oxide (DNTF) comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(a) dissolving 3-chlorohydroximoyl-4-nitro-1,2,5-oxadiazole prepared according to the process of in diethyl ether;'}(b) adding drop-wise a solution of potassium carbonate;(c) stirring the mixture;(d) isolating the DNTF from the organic layer. The present application is a non-provisional application that claims the benefit of the provisional patent application entitled “Synthesis Method for Preparation of 3,4-Bis(4-nitro-t,2,5-oxadizaol-3-yl)-1,2,5-oxadiazole-N-oxide (DNTF)” filed Mar. 12, 2015, as Ser. No. 62/131,972.The inventions described herein may be manufactured and used by or for the United States Government for government purposes without payment of any royalties.A process for producing 3,4-Bis(4-nitro-1,2,5-oxadizaol-3-yl)-1,2,5-oxadiazole-N-oxide (DNTF), an energetic material, through a novel ...

NO- AND H2S- RELEASING COMPOUNDS

This disclosure relates to compounds containing both an NO-releasing moiety and an HS-releasing moiety and the use of such compounds in treating inflammatory diseases, including cancers. 171-. (canceled)75. The compound of claim 74 , wherein R claim 74 , R claim 74 , R claim 74 , R claim 74 , R claim 74 , and Ris H; and Ris CH.77. A method of treating an inflammatory disease claim 72 , comprising administering to a subject in need thereof an effective amount of a compound of .7889. The method of claim claim 72 , wherein the inflammatory disease is cancer claim 72 , rheumatoid arthritis claim 72 , intestine inflammation claim 72 , stomach ulcer claim 72 , a cardiovascular disease claim 72 , or a neurodegenerative disease.79. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable excipient. The present application claims the benefit of U.S. Provisional Patent Applications 61/523,513, filed Aug. 15, 2011, 61/615,700, filed Mar. 26, 2012, and 61/635,624, filed Apr. 19, 2012. Each of the foregoing applications is herein incorporated by reference in its entirety.This invention relates to anti-inflammatory compounds capable of releasing NO and HS, and compositions and methods of using such compounds.Non-steroidal anti-inflammatory drugs (NSAIDs) are prototypical agents for treatment of inflammatory conditions. NSAIDs may also have utility as therapeutic agents against many forms of cancers. Reviewed in K. Kashfi, Anti-Inflammatory Agents as Cancer Therapeutics, pp. 31-89 in Contemporary Aspects of Biomedical Research: Drug Discovery, Advances in Pharmacol., S. Enna and M. Williams (ed.), 2009, vol. 57, Elsevier, Inc. Long-term use of NSAIDs, however, may lead to serious side effects including gastrointestinal and renal side effects.Recognition that endogenous gaseous mediators, nitric oxide (NO) and hydrogen sulfide (HS) can increase mucosal defense mechanisms has led to the development of NO- and HS-releasing NSAIDs with ...

MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF USING THE SAME

The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof. 28-. (canceled)10. The compound of wherein Ris H claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , or C(O)OR.11. The compound of wherein Ris H.12. The compound of wherein Ris H.13. The compound of wherein a and b are both 0.14. (canceled)15. The compound of wherein Ris aryl or heteroaryl each optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 substituents independently selected from halo claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Chaloalkyl claim 1 , Chydroxyalkyl claim 1 , Cy claim 1 , CN claim 1 , NO claim 1 , OR claim 1 , SR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , C(O)OR claim 1 , OC(O)R claim 1 , OC(O)NRR claim 1 , NRC(O)NRR claim 1 , NRR claim 1 , NRC(O)R claim 1 , NRC(O)OR claim 1 , C(═NR)NRR claim 1 , NRC(═NR)NRR claim 1 , P(R) claim 1 , P(OR) claim 1 , P(O)RR claim 1 , P(O)OROR claim 1 , S(O)R claim 1 , S(O)NRR claim 1 , S(O)R claim 1 , and S(O)NRR.16. The compound of wherein Ris phenyl optionally substituted by 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 or 5 substituents independently selected from halo claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Calkynyl claim 1 , Chaloalkyl claim 1 , Chydroxyalkyl claim 1 , Cy claim 1 , CN claim 1 , NO claim 1 , OR claim 1 , SR claim 1 , C(O)R claim 1 , C(O)NRR claim 1 , C(O)OR claim 1 , OC(O)R claim 1 , OC(O)NRR claim 1 , NRC(O)NRR claim 1 , NRR claim 1 , NRC(O)R claim 1 , NRC(O)OR claim 1 , C(═NR)NRR claim 1 , NRC(═NR)NRR claim 1 , P(R) claim 1 , P(OR) claim 1 , P(O)RR claim 1 , P(O)OROR claim 1 , S(O)R claim 1 , S(O)NRR claim 1 , S(O)R claim 1 , and S(O)NRR.17. The compound of wherein r and s are both 0.18. The compound of wherein q claim 1 , r claim 1 , and s are all 0.19. The compound of wherein Yis (CRR)or (CRR)C(O)(CRR).20. The compound of wherein Ris H.21. The compound of wherein n and p are both 0.22. The compound of wherein Xis (CRR) ...

Acylated N-(1,2,5-oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)-aryl carboxamides, and use thereof as herbicides

Acylated N-(1,2,5-oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)-, N-(tetrazol-5-yl)- and N-(triazol-5-yl)-aryl carboxamides, and use thereof as herbicides 4. A herbicidal composition claim 1 , comprising a herbicidally active content of at least one acylated N-(1 claim 1 ,2 claim 1 ,5-oxadiazol-3-yl)- claim 1 , N-(1 claim 1 ,3 claim 1 ,4-oxadiazol-2-yl)- claim 1 , N-(tetrazol-5-yl)- or N-(triazol-5-yl)-aryl carboxamide and/or salt as claimed in .5. The herbicidal composition as claimed in in a mixture with one or more formulation auxiliaries.6. The herbicidal composition as claimed in claim 5 , comprising a further herbicide.7. A method of controlling one or more unwanted plants claim 1 , comprising applying an effective amount of at least one compound of formula (I) and/or salt as claimed in or a herbicidal composition thereof to the plants or to a site of unwanted vegetation.8. A product comprising a compound of formula (I) and/or salt as claimed in or a herbicidal composition thereof for controlling one or more unwanted plants.9. The product as claimed in claim 8 , wherein the compound of the formula (I) and/or salt is used for controlling one or more unwanted plants in one or more crops of useful plants.10. The product as claimed in claim 9 , wherein the useful plants are transgenic useful plants. The invention relates to the technical field of the herbicides, especially that of the herbicides for selective control of weeds and weed grasses in crops of useful plants.WO 2011/035874 A1 describes N-(1,2,5-oxadiazol-3-yl)arylcarboxamides as herbicides. WO 2012/028579 A1 discloses herbicidally active N-(tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides. WO 2012/126932 A1 describes N-(1,3,4-oxadiazol-2-yl)arylcarboxamides as herbicides.AL Y, A. S. ET AL: “Synthesis and reactions of some derivatives of 2-amino-5-(4-pyridyl)-1,3,4-oxadiazole”, EGYPTIAN JOURNAL OF PHARMACEUTICAL SCIENCES, 33(3-4), 699-711, 1992, discloses the compound N-benzoyl-N-[5-(pyridin-4-yl)-1,3,4- ...

NOVEL VIRAL REPLICATION INHIBITORS

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds. 4. (canceled)6. (canceled)7. A method of treatment or prevention of a flavivirus infection in an animal claim 1 , mammal or human claim 1 , comprising administrating an effective amount of a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , optionally in combination with one or more other medicines claim 1 , to an animal claim 1 , mammal or human in need thereof.8. (canceled)12. (canceled)14. (canceled)15. The method according to claim 9 , wherein the flavivirus infection is an infection with a Dengue virus or a yellow fever virus.16. A pharmaceutical composition comprising a pharmaceutically acceptable carrier claim 1 , and as active ingredient an effective amount of the compound according to or a pharmaceutically acceptable salt thereof.17. A method for the preparation of the compound according to comprising the step ofreacting an imine with an aldehyde under umpolung conditions in the presence of a thiazolium catalyst to obtain the desired compounds of the invention; orreacting a ketone derivative having a methylene adjacent to the carbonyl under halogenation conditions to obtain an alpha-halogenoketone, andsubstitute the previously obtained alpha- ...

SUBSTITUTED N-HYDROXYAMIDINOHETEROCYCLES AS MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE

The invention provides modulators of indoleamine 2,3-dioxygenase (IDO1) and their use in the prophylaxis and/or treatment of IDO1-mediated diseases. Specifically, the present invention provides compounds according to Formula (I) an enantiomer, diastereomer, tautomer or pharmaceutically acceptable salt thereof. 5. The compound according to or , wherein{'sub': 1-6', '2', '2', '2', '1-6', '1-6', '2', '2', '2', '2', '2', '1-6', '2', '1-6', '3-6', '6-10, 'sup': 2', '2', '2', '2', '2', '2', '2', '2, 'claim-text': {'sub': 1-6', '1-6', '1-6', '1-6', '0-6', '1-6', '2', '1-6', '2', '2', '2', '2', '2', '3-6', '2, 'sup': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'claim-text': {'sub': 2', '2', '3, 'wherein alkyl, alkylene, cycloalkyl, heterocycloalkyl and heteroaryl are unsubstituted or substituted with 1 to 3 substituents independently selected from the group consisting of halogen, OH, CN, NH, oxo and OS(O)CH.'}, 'wherein cycloalkyl, heterocycloalkyl, aryl and heteroaryl are unsubstituted or substituted with 1 to 7 substituents independently selected from the group consisting of halogen, OH, oxo, CN, C-alkyl, halo-C-alkyl, hydroxy-C-alkyl, O—C-alkyl, C-alkylene-C(O)OR, S(O)—C-alkyl, S(O)—C-alkyl, N(R), C(O)N(R), S(O)N(R), NRS(O)NR, C- cycloalkyl, 3- to 6-membered heterocycloalkyl, S(O)(═NR)R, S(O)(═NR)N(R)and heteroaryl'}, 'D is hydrogen, C-fluoroalkyl, N(R), C(O)OH, CN, C(O)OR, CH(NH)C(O)OH, S(O)C-alkyl, S(O)C-alkyl, S(O)N(R), NRS(O)N(R), NRS(O)C-alkyl, C(O)N(R), S(O)(═NR)C-alkyl, Ccycloalkyl, 4- to 8-membered mono- or bicyclic heterocycloalkyl containing 1, 2 or 3 heteroatoms independently selected from the group consisting of O, S and N, C-aryl, or 5- to 10-membered mono- or bicyclic heteroaryl containing 1, 2, 3 or 4 heteroatoms selected from O, S and N,'}6. The compound according to or , wherein{'sub': 1-6', '2', '2', '2', '1-6', '2', '2', '2', '3-6', '6-10, 'sup': 2', '2', '2, 'claim-text': {'sub': 1-6', '1-6', '1-6', '0-6', '1-6', '2', '1-6', '2', '2', '2', '2', '3 ...

1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.

AMINOINDANE-, AMINOTETRAHYDRONAPHTHALENE- AND AMINOBENZOCYCLOBUTANE-DERIVED PRMT5-INHIBITORS

A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; Ris H or Me; Ris optionally one or more halo or methyl groups; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand R(if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from H and Me; Ris selected from OH, —NH, —C(═O)NH, and —CHOH; Ris either H or Me; Ris either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted Cheteroaryl. 26-. (canceled)7. A compound according to claim 1 , wherein Rrepresents one to four Me or halo groups.8. A compound according to claim 1 , wherein:{'sup': 2a', '2b', '2c', '2d, '(a) R, R, Rand R(if present) are all H; or'}{'sup': 2a', '2b', '2c', '2d, 'sub': '2', '(b) of formula Ia or Ib, wherein R, R, Rand Rare comprised of three H and one Me or CHOH group; or'}{'sup': 2a', '2b', '2c', '2d, '(c) of formula Ia or Ib, wherein R, R, Rand Rare comprised of two H and two Me groups; or'}{'sup': 2a', '2b, 'sub': '2', '(d) of formula Ic, wherein Ris H and Ris a Me or CHOH group; or'}{'sup': 2a', '2b, 'sub': '2', '(e) of formula Ic, wherein Rand Rare each a Me or CHOH group.'}917-. (canceled)18. A compound according to claim 1 , wherein:{'sup': 3a', '3b, '(a) Ris H and Ris Me, or'}{'sup': 3a', '3b, '(b) Rand Rare both H, or'}{'sup': 3a', '3b, '(c) Rand Rare both Me.'}1925.-. (canceled)28. A compound according to claim 1 , wherein the compound is a racemate at the carbon atom to which Rand Rare attached.29. A compound according to claim 1 , wherein the compound is a single enantiomer at the carbon atom to which Rand Rare attached.3031-. (canceled)32. A compound according to claim 1 , wherein the optional substituents on A are independently selected from the group consisting of: Calkyl claim 1 , Cfluoroalkyl claim 1 , Ccycloalkyl claim 1 , Cheteroaryl claim 1 , Cheteroaryl ...

ORGANIC DYES INCORPORATING THE OXADIAZOLE MOIETY FOR EFFICIENT DYE-SENSITIZED SOLAR CELLS

An oxadiazole dye for use as an organic photosensitizer. The oxadiazole dye comprising donor-π-spacer-acceptor type molecules in which at least one of an oxadiazole group acts as a π-conjugated bridge (spacer), a naphthyl unit acts as an electron-donating unit, a carboxyl group act as an electron acceptor group, and a cyano group acts as an anchor group. An optional thiophene group acts as part of the π-conjugated bridge (spacer). The dye for use as organic photosensitizers in a dye-sensitized solar cell. The dye for use in photodynamic therapies. Computational DFT and time dependent DFT (TD-DFT) modeling techniques showing Light Harvesting Efficiency (LHE), Free Energy for Electron Injection (ΔG), Excitation Energies, and Frontier Molecular Orbitals (FMOs) indicate that the series of dye comprise a more negative ΔGand a higher LHE value; resulting in a higher incident photon to current efficiency (IPCE). 2. The dye sensitized solar cell of claim 1 , wherein the light absorbing compound of formula (I) is an (E) isomer.3. The dye sensitized solar cell of claim 1 , wherein the light absorbing compound of formula (I) is a (Z) isomer.4. The compound of selected from the group consisting of:(E)-2-Cyano-3-(5-(5-(naphthalen-2-yl)-1,3,4-oxadiazol-2-yl)thiophen-2-yl)-acrylic acid;(E)-2-Cyano-3-(5-(5-(naphthalen-2-yl)-1,2,3-oxadiazol-4-yl)thiophen-2-yl)-acrylic acid;(E)-2-Cyano-3-(5-(5-(naphthalen-2-yl)-1,2,4-oxadiazol-3-yl)thiophen-2yl)-acrylic acid;(E)-2-Cyano-3-(5-(4-(naphthalen-2-yl)-1,2,5-oxadiazol-3-yl)thiophen-2yl)-acrylic acid;(E)-2-Cyano-3-(5-(naphthalen-2-yl)-1,3,4-oxadiazol-2-yl)-acrylic acid;(E)-2-Cyano-3-(5-(naphthalen-2-yl)-1,2,3-oxadiazol-4-yl)-acrylic acid;(E)-2-Cyano-3-(5-(naphthalen-2-yl)-1,2,4-oxadiazol-3-yl)-acrylic acid;(E)-2-Cyano-3-(4-(naphthalen-2-yl)-1,2,5-oxadiazol-3-yl)-acrylic acid;(Z)-2-Cyano-3-(5-(5-(naphthalen-2-yl)-1,3,4-oxadiazol-2-yl)thiophen-2-yl)-acrylic acid;(Z)-2-Cyano-3-(5-(5-(naphthalen-2-yl)-1,2,3-oxadiazol-4-yl)thiophen-2-yl)-acrylic ...

IMINO-UREA DERIVATIVES

The present invention relates to the field of medicines, and in particular to an imino-urea derivative containing a furan structure and a composition thereof. The derivative and the composition thereof can be used in the manufacture of a medicament for treating a disease pathologically characterized by indoleamine 2,3-dioxygenase-mediated tryptophan metabolic pathway. The present invention also relates to a method for preparing the derivative and an intermediate thereof. 2. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , characterized in that R claim 1 , Rare each independently selected from the group consisting of the following substituents: Calkyl claim 1 , carbonyl claim 1 , Calkoxy claim 1 , sulfonyl claim 1 , amidino claim 1 , sulfinyl claim 1 , which is substituted by one or more substituents selected from group consisting of: halogen claim 1 , hydroxy claim 1 , carboxy claim 1 , carbonyl claim 1 , aldehyde group claim 1 , cyano claim 1 , amino claim 1 , aryl claim 1 , heteroaryl claim 1 , Calkyl claim 1 , Ccycloalkyl claim 1 , Calkenyl claim 1 , Ccycloalkenyl; wherein claim 1 , the carboxy claim 1 , carbonyl claim 1 , aldehyde group claim 1 , cyano claim 1 , amino claim 1 , aryl claim 1 , heteroaryl claim 1 , Ccycloalkyl claim 1 , Calkenyl claim 1 , Ccycloalkenyl as the substituents of Calkyl claim 1 , carbonyl claim 1 , Calkoxy claim 1 , sulfonyl claim 1 , amidino or sulfinyl are optionally substituted by one or more substituents selected from group consisting of: H claim 1 , halogen claim 1 , Calkyl claim 1 , carbonyl claim 1 , Calkoxy claim 1 , sulfinyl and sulfonyl; the halogen is selected from the group consisting of F claim 1 , Cl claim 1 , Br and I.3. The compound or a pharmaceutically acceptable salt thereof according to claim 1 , characterized in that R claim 1 , Rare each independently selected from the group consisting of the following substituents: H claim 1 , methyl claim 1 , ethyl claim 1 , propyl claim 1 , ...

PET PROBES OF RADIOFLUORINATED CARBOXIMIDAMIDES FOR IDO-TARGETED IMAGING

F labeled IDO1 imaging constructs are constructed for positron emission tomography (PET). Synthetic methodology involves the coupling of a 1-fluoro-2-halo-4-aminobenzene and a 4-amino-N-hydroxy-1,2,5-oxadiazole-3-carboximidoyl chloride wherein at least one of the coupled compounds comprises an F. The F labeled IDO1 imaging constructs are useful for imaging cancer cells in a patient. 4. The method according to claim 3 , wherein providing a 4-amino-N-hydroxy-1 claim 3 ,2 claim 3 ,5-oxadiazole-3-carboximidoyl chloride comprises:providing a 2-halo-N,N,N-trimethyl-4-nitrobenzenaminium trifluoromethanesulfonate;combining the 2-halo-N,N,N-trimethyl-4-nitrobenzenaminium trifluoromethanesulfonate with cryptated potassium fluoride in an organic solvent to form a 1-fluoro-2-halo-4-nitrobenzene;{'sub': '4', 'combining the 1-fluoro-2-halo-4-nitrobenzene with NaBHand a Pd/C catalyst in an organic solvent to form the 1-fluoro-2-halo-4-aminobenzene.'}5. A method of performing positron emission tomography (PET) claim 1 , comprising injecting a solution comprising an F labeled IDO1 imaging construct according to into a patient suspected of having cancer.7. The method according to claim 5 , wherein the cancer is breast cancer.8. The method according to claim 5 , further comprising administering a treatment for the cancer to the patient before claim 5 , during claim 5 , or after injecting the solution.9. The method according to claim 8 , wherein the treatment comprises administration of surgery claim 8 , radiation claim 8 , chemotherapy claim 8 , immunotherapy claim 8 , or a combination of two or more of the foregoing.10. The method according to claim 8 , wherein the cancer is one in which indoleamine 2 claim 8 ,3-dioxygenase-1 (IDO1) is over-expressed relative to normal tissue.11. The method according to claim 8 , wherein the treatment comprises administering an inhibitor of indoleamine 2 claim 8 ,3-dioxygenase-1 (IDO1) to the patient.12. The method according to claim 8 , wherein the ...

BENZAMIDE COMPOUNDS AND THEIR USE AS HERBICIDES

The present invention relates to benzamide compounds of formula (I), the N-oxides and the salts thereof (I), where the variables are as defined in the claims and the description. The invention also relates to compositions comprising such compounds and to the use of such compounds for controlling unwanted vegetation. 2. The compound of claim 1 , where Q is Q.3. The compound of claim 1 , where Q is Q.4. The compound of claim 1 , where Q is Q.5. The compound of claim 1 , where Ris selected from the group consisting of halogen claim 1 , nitro claim 1 , cyano claim 1 , C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-alkoxy claim 1 , C-C-alkoxy-C-C-alkoxy-Z- and R—S(O)—Z-.6. The compound of claim 5 , where Ris selected from the group consisting of halogen claim 5 , C-C-alkyl and C-C-alkoxy.7. The compound of claim 1 , where{'sup': '2a', 'sub': 1', '6', '1', '6', '3', '7', '3', '7', '1', '4', '1', '6', '1', '4', '1', '4', '1', '4', '1', '4, 'Ris selected from the group consisting of hydrogen, C-C-alkyl, C-C-alkoxy, C-C-cycloalkyl, C-C-cycloalkyl-C-C-alkyl, C-C-haloalkyl, phenyl, benzyl, and heterocyclyl, where heterocyclyl is a 5- or 6-membered monocyclic saturated, partially unsaturated or aromatic heterocycle which contains 1, 2, 3 or 4 heteroatoms as ring members which are selected from the group consisting of O, N and S, where phenyl, benzyl and heterocyclyl are unsubstituted or substituted by 1, 2, 3 or 4 groups which are identical or different and selected from the group consisting of halogen, C-C-alkyl, C-C-haloalkyl, C-C-alkoxy and C-C-haloalkoxy; and'}{'sup': '2b', 'sub': 1', '6', '3', '7', '3', '7', '1', '4', '1', '6', '1', '4', '1', '4', '1', '4', '1', '4, 'Ris selected from the group consisting of hydrogen, C-C-alkyl, C-C-cycloalkyl, C-C-cycloalkyl-C-C-alkyl, C-C-haloalkyl, phenyl, benzyl and heterocyclyl, where heterocyclyl is a 5- or 6-membered monocyclic saturated, partially unsaturated or aromatic heterocycle which contains 1, 2, 3 or 4 heteroatoms as ring ...

1,2,5-Oxadiazoles As Inhibitors Of Indoleamine 2,3- Dioxygenase

The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives. 1174-. (canceled)175. A method of treating a cancer selected from renal cancer , lung cancer , and head and neck cancer in a patient , comprising administering to said patient a therapeutically effective amount of a compound , which is 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1 ,2 ,5-oxadiazole-3-carboximidamide , or a pharmaceutically acceptable salt thereof in combination with an antibody therapeutic.176. The method of claim 175 , wherein the cancer is renal cancer.177. The method of claim 176 , wherein the antibody therapeutic is an anti-PD-1 antibody.178. The method of claim 176 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.179. The method of claim 175 , wherein the cancer is lung cancer.180. The method of claim 179 , wherein the antibody therapeutic is an anti-PD-1 antibody.181. The method of claim 179 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.182. The method of claim 175 , wherein the cancer is head and neck cancer.183. The method of claim 182 , wherein the antibody therapeutic is an anti-PD-1 antibody.184. The method of claim 182 , wherein the antibody therapeutic is an anti-CTLA-4 antibody.185. A method of treating a cancer selected from renal cancer claim 182 , lung cancer claim 182 , and head and neck cancer in a patient claim 182 , comprising administering to said patient a therapeutically effective amount of a compound claim 182 , which is 4-({2-[(aminosulfonyl)amino]ethyl}amino)-N-(3-bromo-4-fluorophenyl)-N′-hydroxy-1 claim 182 ,2 claim 182 ,5-oxadiazole-3-carboximidamide in combination with an antibody therapeutic.186. The method of claim 185 , wherein the cancer is renal cancer.187. The ...

NOVEL COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS

Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein:{'sup': '1', 'claim-text': (a) halogen,', {'sub': '1-6', '(b) Calkyl, optionally substituted with one to four halogens, and'}, '(c) CN; and, 'Ris aryl, optionally substituted with one to four substituents independently selected from{'sup': 2', '3, 'claim-text': [{'sup': '4', '(a) R,'}, {'sup': '4', '(b) OR,'}, {'sup': '4', '(c) NH—R,'}, '(d) halogen, and', {'sub': '3-6', '(e) Ccycloalkyl;'}], 'each occurrence of Rand Ris independently selected from{'sup': 2', '3, 'or alternatively, Rand Rtogether form an oxo group;'}{'sup': 2', '3, 'sub': '3-6', 'or alternatively, Rand Rtogether with the carbon to which they are attached form a Ccycloalkyl group.'}4. The compound of claim 1 , wherein:X is S,{'sup': '1', 'claim-text': (a) halogen,', {'sub': '1-6', '(b) Calkyl, optionally substituted with one to four halogens, and'}, '(c) CN; and, 'Ris phenyl, optionally substituted with one to four substituents independently selected from{'sup': 2', '3, 'claim-text': [{'sup': '4', '(a) R,'}, '(b) OH,', {'sup': '4', '(c) NH—R, and'}, '(d) halogen;, 'each occurrence of Rand Ris independently selected from{'sup': 2', '3, 'or alternatively, Rand Rtogether form an oxo group.'}5. The compound of claim 1 , wherein:each occurrence of aryl is phenyl; andeach occurrence of the 4-, 5- or 6-membered heterocyclyl is independently selected from: azetidinyl, 1,2,5-thiadiazolidinyl, imidazolidinyl, oxazolidinyl, oxetanyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, tetrahydropyranyl ...

Methods of detecting Lp-PLA2 activity

This invention relates to a method for measuring enzymatically active Lipoprotein-associated Phospholipase A2 (Lp-PLA2) in a sample. Further, this invention relates to a Hybrid Immunocapture method for measuring enzymatically active Lp-PLA2 in a sample. Specifically, this invention relates to a Hybrid Immunocapture method for measuring enzymatically active Lp-PLA2 in a sample utilizing an enzymatically active Lp-PLA2 standard. In addition, this invention relates to a kit for measuring enzymatically active Lp-PLA2 in a sample. Specifically, this invention relates to a kit for measuring enzymatically active Lp-PLA2 in a sample containing an enzymatically active Lp-PLA2 standard.

Acylated n-(1,2,5-oxadiazole-3-yl)-, n-(1,3,4-oxadiazole-2-yl)-, n-(tetrazole-5-yl)- and n-(triazole-5-yl)-aryl carboxamides, and use thereof as herbicides

Described are acylated N-(1,2,5-oxadiazole-3-yl)-, N-(1,3,4-oxadiazole-2-yl)-, N-(tetrazole-5-yl)- and N-(triazole-5-yl)-aryl carboxamides of formula (I) and the use thereof as herbicides. In said formula (I), R, V, X, Y, and Z are groups such as hydrogen, organic groups such as alkyl, and other groups such as halogens. Q represents an oxadiazole, tetrazole or triazole group. W represents CY or N.

HAPTENES, HAPTEN CONJUGATES, COMPOSITIONS THEREOF, AND METHODS FOR PRODUCING AND USING THEREOF

Haptens, hapten conjugates, compositions thereof and method for their preparation and use

A method for performing a multiplexed diagnostic assay, such as for two or more different targets in a sample, is described. One embodiment comprised contacting the sample with two or more specific binding moieties that bind specifically to two or more different targets. The two or more specific binding moieties are conjugated to different haptens, and at least one of the haptens is an oxazole, a pyrazole, a thiazole, a nitroaryl compound other than dinitrophenyl, a benzofurazan, a triterpene, a urea, a thiourea, a rotenoid, a coumarin, a cyclolignan, a heterobiaryl, an azo aryl, or a benzodiazepine. The sample is contacted with two or more different anti-hapten antibodies that can be detected separately. The two or more different anti-hapten antibodies may be conjugated to different detectable labels.

Modulators of sperm hypermotility and uses thereof

The invention provides novel compositions and compounds that inhibit CatSper channel activity, that preferentially inhibits sperm hyperactivity over sperm motility, or both. The compounds of the invention are useful as contraceptive agents that may be adminstered to males, females, or concurrently to both sexual partners. The invention further provides methods of conducting drug discovery business and of conducting a reproductive medicine business. The invention also provides methods of identifying compounds that modulate sperm hypermotility.

Calpain modulators and therapeutic uses thereof

Bridged spiro[2,4]heptane derivatives as alx and/or fprl2 receptor agonists

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to bridged spiro[2.4]heptane derivatives of formula (I), wherein W means -CH 2 CH 2 - or -CH=CH-; Z means -C(O)NR 3 -* or -CH 2 NR 4 C(O)-*, Y means a bond or (C 1 -C 4 )alkane diyl group, R 1 -R 4 are those as specified in the description, to preparing and using them as ALX and/or FPRL2 receptor agonists applicable for treating inflammatory and obstructive respiratory diseases. EFFECT: preparing the compositions for treating the inflammatory and obstructive respiratory diseases. 14 cl, 1 tbl, 422 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 233/58 C07C 233/60 C07C 233/63 C07D 211/26 C07D 207/09 C07D 213/40 ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 231/12 ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 233/64 C07D 235/14 C07D 239/30 (12) ОПИСАНИЕ (21)(22) Заявка: (13) 2 540 274 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) C07D C07D C07D C07D C07D A61K A61K A61K A61K A61P 249/08 277/28 277/62 307/52 319/12 31/44 31/40 31/426 31/427 11/00 C2 (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2011151277/04, 17.05.2010 (24) Дата начала отсчета срока действия патента: 17.05.2010 18.05.2009 IB PCT/IB2009/052056 (45) Опубликовано: 10.02.2015 Бюл. № 4 (73) Патентообладатель(и): АКТЕЛИОН ФАРМАСЬЮТИКЛЗ ЛТД (CH) 2 5 4 0 2 7 4 R U 2005047899 A2, 26.05.2005 . BANNENBERG G L: "Anti-inflammatory actions of lipoxins" EXPERT OPINION ON THERAPEUTIC PATENTS 2007, vol. 17, no. 6, pages 591-605. BURLI R W ET AL: "Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents" BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, 2006, vol. 16, no. 14, pages 3713-3718 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 19.12.2011 (86) Заявка PCT: IB 2010/052170 (17.05.2010) (87) Публикация заявки PCT: WO 2010/134014 (25.11.2010) Адрес для переписки: 105082, Москва, Спартаковский пер., д. 2, стр. 1, секция 1, ...

Amides n- (1,2,5-oxadiazol-3-yl) -, n- (1,3,4-oxadiazol-2-yl) -, n- (tetrazol-5-yl) - and n-(triazole 5-yl)-aryl carboxylic acids and their use as herbicides

FIELD: chemistry. SUBSTANCE: invention relates to amides of N-(1,2,5-oxadiazol-3-yl)-, N-(1,3,4-oxadiazol-2-yl)- and N-(tetrazol-5-yl)- aryl carboxylic acids of formula , wherein R is alkyl with 1-6 carbon atoms, alkenyl of 2-6 carbon atoms, alkynyl of 2-6 carbon atoms, (alkyl of 1-6 carbon atoms)-OR 1 , (alkyl with 1-6 carbon atoms) -COOR 1 , (alkyl with 1-6 carbon atoms)-CN, or benzyl, W is CY, X and Z, which in each case independently from one another represent halogen, alkyl with 1-6 carbon atoms, haloalkyl with 1-6 carbon atoms, or S(O) n R 2 , Y is halogen, S(O) n R 2 or 5-membered partially saturated heteroaryl having 2 heteroatoms selected from N, O, substituted by s residues of cyanogroup, V is hydrogen,R 1 is alkyl with 1-6 carbon atoms, R 2 is alkyl with 1-6 carbon atoms, n is 0. 1 or 2, s is 1, Q is a rwsidue of Q1, Q3 or Q4, R 6 is alkyl with 1-6 carbon atoms or alkynyl with 2-6 carbon atoms, where these 2 above-mentioned residues in each case are substituted by s residues from the group, consisting from phenyl, R 8 is alkyl with 1-6 carbon atoms or halogen, R 9 is alkyl with 1-6 carbon atoms, s is 0 or 1. The invention also relates to herbicidal agents. EFFECT: obtained new compound of formula (I), having a high herbicidal activity. 5 cl, 340 tbl, 3 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 619 102 C1 (51) МПК C07D 257/04 (2006.01) C07D 271/08 (2006.01) C07D 271/113 (2006.01) C07D 413/12 (2006.01) A01N 43/713 (2006.01) A01N 43/824 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A01N 43/832 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A01P 13/00 (2006.01) (12) ФОРМУЛА (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ 2014128456, 10.12.2012 (24) Дата начала отсчета срока действия патента: 10.12.2012 Дата регистрации: Приоритет(ы): (30) Конвенционный приоритет: 13.12.2011 EP 11193166.3 (73) Патентообладатель(и): БАЙЕР ИНТЕЛЛЕКТУЭЛЬ ПРОПЕРТИ ГМБХ (DE) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 14.07.2014 (56) Список документов, цитированных в ...

杂环脲类化合物及其药物组合物和应用

本发明涉及杂环脲类化合物，具体公开了杂环脲类化合物的吲哚胺‑2,3‑双加氧酶抑制剂，解决现有免疫治疗药物疗效弱、毒副作用较大的缺陷等问题。本发明还提供了杂环脲类化合物的吲哚胺‑2,3‑双加氧酶制剂的制备方法，以及上述杂环脲类化合物的吲哚胺‑2,3‑双加氧酶制剂或其药学上可接受的盐的在制备治疗或预防肿瘤的药物中的药物中的用途。

Гербицидно-активные кетосультамы и дикетопиридины

1. Механизм для преобразования неравномерного вращательного движения лопастей роторно-лопастного двигателя внутреннего сгорания в равномерное вращение вала, состоящий из корпуса, вала, размещенного в корпусе с возможностью вращения, лопастей, установленных на валу с возможностью свободного вращения и делящих полость корпуса на четыре камеры переменного объема, двух установленных на валу зубчатых колес с внешними зубчатыми венцами, эксцентриков, выполненных в виде цилиндрических выемок на лопастях, шатунов в виде колец, установленных в эксцентриках с возможностью свободного вращения, зубчатых колес с внутренним зубчатым венцом, жеско установленных в шатунах и кинематически взаимодействующих с установленными на валу зубчатыми колесами с внешним зубчатым венцом, радиальных направляющих, выполненных на шатунах, редукторов, кинематически взаимодействующих посредством установленных на водилах осей с радиальными направляющими и предназначенных для передачи шатунам дополнительного вращательного движения от вала.2. Механизм по п. 1, отличающийся тем, что радиальные направляющие выполнены на водиле редуктора, а ось качания шатуна выполнена в виде цапфы и кинематически связана с радиальными направляющими.3. Механизм по пп. 1 и 2, отличающийся тем, что эксцентрики выполнены в виде кулачков, установленных с возможностью свободного вращения на валу и жестко соединенных с лопастями, а шатун установлен на эксцентрике с возможностью свободного вращения вокруг его оси. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2013 114 184 (13) A (51) МПК C07D 471/04 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (71) Заявитель(и): БАЙЕР ИНТЕЛЛЕКТУЭЛЬ ПРОПЕРТИ ГМБХ (DE) (21)(22) Заявка: 2013114184/04, 29.08.2011 Приоритет(ы): (30) Конвенционный приоритет: 01.09.2010 EP 10174905.9 R U (54) ГЕРБИЦИДНО-АКТИВНЫЕ КЕТОСУЛЬТАМЫ И ДИКЕТОПИРИДИНЫ (57) Формула изобретения 1. Механизм для преобразования неравномерного вращательного движения лопастей роторно-лопастного ...

Haptens, hapten conjugates, compositions thereof and methods of making and using them

IDO1 inhibitor and preparation method and application thereof

一类作为吲哚胺‑2,3‑双加氧酶1(IDO1)抑制剂的化合物，及其在与IDO1相关疾病领域的应用。具体为式(Ⅰ)所示化合物及其药学上可接受的盐。

Heteroaromatic derivatives of urea and use thereof as glucokinase activators

FIELD: chemistry. SUBSTANCE: invention relates to compounds of general formula (I) and to their pharmaceutically acceptable salts, optical isomers or their mixture as glucokinase activators. In general formula (I) where R 1 is C 3-8 -cycloalkyl, C 3-8 -cycloalkenyl, a 6-member heterocyclyl with 1 nitrogen atom, condensed phenyl-C 3-8 -cycloalkyl, each of which is possibly substituted with one or two substitutes R 3 , R 4 , R 5 and R 6 ; R 2 is C 3-8 -cycloalkyl, a 5-6-member heterocyclyl with 1-2 heteroatoms selected from N, O, or S, each of which can be substituted with one or two substitutes R 30 , R 31 , R 32 and R 33 , and R 3 , R 4 , R 5 , R 6 , R 30 , R 31 , R 32 and R 33 are independently selected from a group consisting of halogen, hydroxy, oxo, -CF 3 ; or -NR 10 R 12 ; or C 1-6 -alkyl, phenyl, C 1-6 -alkoxy, C 1-6 -alkyl-C(O)-O-C 1-6 -alkyl, each of which is possibly substituted with one substitute independently selected from R 12 ; or -C(O)-R 27 , -S(O) 2 -R 27 ; or two substitutes selected from R 3 , R 4 , R 5 and R 6 or R 30 , R 31 , R 32 and R 33 , bonded to the same atom or to neighbouring atoms, together form a -O-(CH 2 ) 2 -O- radical; R 10 and R 11 independently represent hydrogen, C 1-6 -alkyl, -C(O)-C 1-6 -alkyl, -C(O)-O- C 1-6 -alkyl, -S(O) 2 - C 1-6 -alkyl; R 27 is C 1-6 -alkyl, C 1-6 -alkoxy, C 3-8 -cycloalkyl, C 3-8 -cycloalkyl-C 1-6 -alkyl, phenyl, phenyl-C 1-6 -alkyl, a 5-6-member heteroaryl with 1-2 heteroatoms selected from N or S, a 6-member heteroaryl-C 1-6 -alkyl with 1 nitrogen atom, a 6-member heterocyclyl-C 1-6 -alkyl with 1-2 heteroatoms selected from N or O, R 10 R 11 -N- C 1-6 -alkyl, each of which is possibly substituted with one substitute independently selected from R 12 ; R 12 is a halogen, CF 3 , C 1-6 -alkoxy, -NR 10 R 11 ; A is a 5-9-member heteroaryl with 1-3 heteroatoms selected from N, O or S, which is possibly substituted with one or two substitutes independently selected from R 7 , R 8 and R 9 ; R 7 , R 8 and R 9 are ...

Substituted isophthalic acid diamides

The invention relates to substituted isophthalic acid diamides and to their use as herbicides. Disclosed are isophthalic acid diamides having general formula (I) as herbicides. In this formula (I), Z 1 and Z 2 represent radicals such as alkyl, cycloalkyl and phenyl. W 1 and W 2 represent radicals such as hydrogen, alkyl, cycloalkyl and halogen. Q represents a heterocyclic ring such as tetrazolyl.

Substituted isophthalic acid diamides

The invention relates to substituted isophthalic acid diamides and to their use as herbicides. Disclosed are isophthalic acid diamides having general formula (I) as herbicides. In this formula (I), Z 1 and Z 2 represent radicals such as alkyl, cycloalkyl and phenyl. Q represents a heterocyclic ring such as tetrazolyl.

Substituted isophthalic acid diamides and their use as herbicides

The invention relates to isophthalic acid diamides having general formula (I) as herbicides. In this formula (I), X and Y represent radicals such as hydrogen, alkyl and halogen. Z 1 and Z 2 represent radicals such as alkyl, cycloalkyl and phenyl. Q represents a heterocyclic ring such as tetrazolyl.

Substituted isophthalic acid diamides

Es werden Isopthalsäurediamide der allgemeinen Formel (I) als Herbizide beschrieben. In dieser Formel (I) stehen X, Y und Z für Reste wie Wasserstoff, Alkyl und Halogen. Q steht für einen heterocyclischen Ring wie Tetrazolyl.

Formulations and electronic devices

The present invention relates to a formulation, comprising at least one solvent and at least two functional compounds of the general formula (I), wherein A is a functional structural element, B is a solubility-promoting structural element, and k is an integer in the range of 1 to 20, the molecular weight of the functional compound is at least 550 g/mol, and the solubility-promoting structural element B corresponds to the general formula (L-I), wherein Ar 1 and Ar 2 are an aryl or heteroaryl group independently of each other, which aryl or heteroaryl group can be substituted with one or more arbitrary groups R, each instance of X is N or CR 2 , preferably CH, independently of each other, R 1 and R 2 , independently of each other, are hydrogen, a straight-chain alkyl, alkoxy, or thioalkoxy group having 1 to 40 C atoms or a branched or cyclic alkyl, alkyoxy, or thioalkoxy group having 3 to 40 C atoms or a silyl group or a substituted keto group having 1 to 40 C atoms, an alkoxy carbonyl group having 2 to 40 C atoms, an aryloxy carbonyl group having 7 to 40 C atoms, a cyano group (-CN), a carbamoyl group (-C(=O)NH 2 ), a haloformyl group (-C(=O)-X, wherein X represents a halogen atom), a formyl group (-C(=O)-H), an isocyano group, an isocyanate group, a thiocyanate group, or a thioisocyanate group, a hydroxy group, a nitro group, a CF 3 group, Cl, Br, F, a group that can be cross-linked, or a substituted or unsubstituted aromatic or heteroaromatic ring system having 5 to 60 ring atoms, or an aryloxy or heteroaryloxy group having 5 to 60 ring atoms, or a combination of said systems, wherein one or more of the groups R 1 and/or R 2 can form a mono- or polycyclic, aliphatic, or aromatic ring system with each other and/or with the ring to which the group R 1 is bonded; and I is 0, 1, 2, 3, or 4; wherein the dashed bond indicates the bond to the functional structural element A. The present invention further relates to electronic devices that contain mixtures of said ...

Nitric oxide donator type β elemene derivatives and its production and use

本发明属于β‑榄香烯衍生物的制备技术领域，具体公开了一种一氧化氮供体型β‑榄香烯衍生物、其制备方法及用途。该β‑榄香烯衍生物及其可药用盐的具有通式M，其中，X为O；或同时含有酯基和胺基的基团；R 1 代表不含或任选地含有一个至三个取代基的C 1‑10 烷基，C 6‑12 环烷基，C 6‑12 芳基，C 2‑10 烯基，C 2‑10 炔基或C 2‑10 醚基；R 2 代表不含或任选地含有一个至三个取代基的C 1‑10 烷基，C 6‑12 环烷基，C 6‑12 芳基，C 2‑10 烯基，C 2‑10 炔基或C 4‑22 的醚基。所述一氧化氮供体型β‑榄香烯衍生物及其可药用盐可用于抗肿瘤药物的制备。

Calcium receptor modulating agents

The compounds of the invention are represented by the following general structure or a pharmaceutically acceptable salt thereof, and compositions containing them, wherein the variables are defined herein, and their use to reduce or inhibit PTH secretion, including methods for reducing or inhibiting PTH secretion and methods for treatment or prophylaxis of diseases associated with bone disorders, such as osteoporosis, or associated with excessive secretion of PTH, such as hyperparathyroidism. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Substituted 1,2,5-oxadiazole compounds and their use as herbicides

本发明涉及式I的取代的1,2,5-噁二唑化合物及其N-氧化物和盐，以及包含它们的组合物。本发明还涉及1,2,5-噁二唑化合物或包含该类化合物的组合物在防治不希望的植物生长中的用途。此外，本发明涉及施用该类化合物的方法。在式I中，各变量具有下列含义：R例如为氢、氰基、硝基、卤素、C 1 -C 6 烷基、C 3 -C 7 环烷基、C 3 -C 7 环烷基-C 1 -C 4 烷基、C 1 -C 6 卤代烷基、C 2 -C 6 链烯基、C 2 -C 6 卤代链烯基、C 2 -C 6 炔基、C 2 -C 6 卤代炔基、C 1 -C 4 烷氧基-C 1 -C 4 烷基、C 1 -C 4 卤代烷氧基-C 1 -C 4 烷基、O-R a 、Z-S(O) n -R b 、Z-C(＝O)-R c 、Z-C(＝O)-OR d 、Z-C(＝O)-NR e R f 、Z-NR g R h 、Z-苯基和Z-杂环基；R 1 例如为Z 1 -氰基、卤素、硝基、C 1 -C 8 烷基、C 2 -C 8 链烯基、C 2 -C 8 炔基、C 1 -C 8 卤代烷基、C 1 -C 8 烷氧基、C 1 -C 4 烷氧基-C 1 -C 4 烷基、Z 1 -C 1 -C 4 烷氧基-C 1 -C 4 烷氧基、C 1 -C 4 烷硫基-C 1 -C 4 烷基、Z 1 -C 1 -C 4 烷硫基-C 1 -C 4 烷硫基、C 2 -C 6 链烯氧基、C 2 -C 6 炔氧基、C 1 -C 6 卤代烷氧基、C 1 -C 4 卤代烷氧基-C 1 -C 4 烷基、Z 1 -C 1 -C 4 卤代烷氧基-C 1 -C 4 烷氧基、Z 1 -S(O) k -R 1b 、Z 1 -苯氧基或Z 1 -杂环氧基；R 3 相同或不同且例如为氢、卤素、Z 2 -OH、Z 2 -NO 2 、Z 2 -氰基、C 1 -C 6 烷基、C 2 -C 8 链烯基、C 2 -C 8 炔基、Z 2 -C 3 -C 10 环烷基、Z 2 -C 3 -C 10 环烷氧基、C 1 -C 8 卤代烷基、Z 2 -C 1 -C 8 烷氧基、Z 2 -C 1 -C 8 卤代烷氧基、Z 2 -C 1 -C 4 烷氧基-C 1 -C 4 烷氧基、Z 2 -C 1 -C 4 烷硫基-C 1 -C 4 烷硫基、Z 2 -C 2 -C 8 链烯氧基、Z 2 -C 2 -C 8 炔氧基、Z 2 -C 1 -C 8 卤代烷氧基、Z 2 -C 2 -C 8 卤代链烯氧基、Z 2 -C 2 -C 8 卤代炔氧基、Z 2 -C 1 -C 4 卤代烷氧基-C 1 -C 4 烷氧基、Z 2 -(三-C 1 -C 4 烷基)甲硅烷基、Z 2 -S(O) k -R 2b 、Z 2 -C(＝O)-R 2c 、Z 2 -C(＝O)-OR 2d 、Z 2 -C(＝O)-NR 2e R 2f 、Z 2 -NR 2g R 2h 、Z 2a -苯基和Z 2a -杂环基；R 4 选自氢、卤素、氰基、硝基、C 1 -C 4 烷基和C 1 -C 4 卤代烷基；R 5 选自氢、卤素、C 1 -C 4 烷基和C 1 -C 4 卤代烷基；条件是基团R 4 和R 5 中至少一个不为氢；n为0、1或2；k为0、1或2。

Inhibitors of histone deacetylase and prodrugs thereof

The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.

Modulators of indoleamine 2,3-dioxygenase and methods of using the same

본 발명은 인돌아민 2,3-디옥시게나제(IDO)의 조절제 및 이의 조성물 및 약제학적 방법에 관한 것이다. The present invention relates to modulators of indoleamine 2,3-dioxygenase (IDO) and compositions and pharmaceutical methods thereof. 인돌아민 2,3-디옥시게나제의 조절제, 트립토판, 억제, IDO-관련된 질환, IDO-관련된 면역억제 Modulators of indoleamine 2,3-dioxygenase, tryptophan, inhibition, IDO-associated diseases, IDO-associated immunosuppression

Acylated N- (1,2, 5-oxadiazol-3-yl) -, N- (1,3, 4-oxadiazol-2-yl) -, N- (tetrazol-5-yl) -and N- (triazol-5-yl) -arylcarboxamides and their use as herbicides

本发明记载了式(I)的酰化的N‑(1,2,5‑噁二唑‑3‑基)‑、N‑(1,3,4‑噁二唑‑2‑基)‑、N‑(四唑‑5‑基)‑和N‑(三唑‑5‑基)‑芳基羧酰胺及其作为除草剂的用途。在所述式(I)中，R、V、X、Y和Z是基团如氢、有机基团如烷基和其他基团如卤素。Q代表噁二唑、三唑或四唑基团。W代表CY或N，

Process for preparing 3,4-bis-substituted 1,2,5-oxa-diazol-2-oxides or their pharmaceutically acceptable acid addition salts

1. Способ получения 3,4-бис-замещенных1,2,5-оксадиазол-2-окисей общей формулы 1 О R N ЛТ 0 где R - NHR, -NHR ORz - NHRSCOR -N-X; где R - .-алкил, циклопентил, циклогексил; RZ и R - С -С -алкил; (CHj), где n - 2,3 или 4; (СН,)..-, где m - 1,2 или 3; - г - - --у- . -R- метокси, этокси, амине, метиламине, этиламине, диметиламине, диэтиламино; (СН2)р-; -(CH2)2-0-(CHj)j-; Y « СНз (CH2)2-N-(CH,),4, 5 или 6, р илиих фармакологически приемлемых кислетне-аддитивных селей, отличающийсятем, что ексамоил хлорид общей формулы II К-СО-С-С1 II NOH где R имеет указанные значения, О) подвергают циклодимеризации в среде растворителя или диспергатора в присутствииоснования при температуре от О до 50&deg;С с последующим вьщелением целевого продукта в свободном виде или в виде соли. 2.Способ ПОП.1, отличающийсятем, чте в качестве растворителяиспользуют диметштфермамидили диметилсульфоксид, N-метнлпирролидон, низший алифатический спирт, диэтиловый эфир, воду или их смеси. 3.Способ ПОП.1, отличающийс я тем, что в качестве основанияиспользуют фтеричный или третичньйамин, гидроокись или карбонат, или бикарбонат, или ацетат щелочного металла-. 1. The method of obtaining 3,4-bis-substituted 1,2,2-oxadiazole-2-oxides of the general formula 1 O R N LT 0 where R is NHR, —NHR ORz is NHRSCOR-N-X; where R is.-alkyl, cyclopentyl, cyclohexyl; RZ and R - C-C-alkyl; (CHj), where n is 2.3 or 4; (CH,) ..-, where m - 1,2 or 3; - g - - - -. -R-methoxy, ethoxy, amine, methylamine, ethylamine, dimethylamine, diethylamino; (CH2) p-; - (CH2) 2-0- (CHj) j-; Y "CH3 (CH2) 2-N- (CH,), 4, 5 or 6, p or their pharmacologically acceptable acid-additive mudflows, characterized in that Examoyl chloride of the general formula II K-CO-C-C1 II NOH where R has the indicated values, O), are subjected to cyclodimerization in the medium of a solvent or dispersant in the presence of a base at a temperature from 0 to 50 ° C, followed by allocation of the target product in free form or in the form of a salt. 2. Method POP ...

N, n'-substituted-1,3-diamino-2-hydroxypropane derivatives

Disclosed are compounds of the formula (I), wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of betasecretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.

Substituted aryl thioureas and related compounds; inhibitors of viral replication

The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A 1 , A 2 , R 1 , R 2 , V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

Novel viral replication inhibitors

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.

Viral replication inhibitors

The present invention relates to a series of novel compounds, methods to prevent or treat viral infections in animals by using the novel compounds and to said novel compounds for use as a medicine, more preferably for use as a medicine to treat or prevent viral infections, particularly infections with RNA viruses, more particularly infections with viruses belonging to the family of the Flaviviridae, and yet more particularly infections with the Dengue virus. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of viral infections. The invention also relates to processes for preparation of the compounds.

HERBICIDO-ACTIVE OXYMETHER-SUBSTITUTED BENZOILAMIDES

1. Бензоиламид формулы (I) или его солигде заместители имеют следующие значения:Q представляет собой радикал Q1, Q2, Q3 или Q4,R представляет собой -CH=N-OR, -CH-O-N=CRR,X представляет собой нитро, галоген, циано, формил, родано, (C-C)-алкил, галоген-(C-C)-алкил, (C-C)-алкенил, галоген-(C-C)-алкенил, (C-C)-алкинил, галоген-(C-C)-алкинил, (C-C)-циклоалкил, галоген-(C-C)-циклоалкил, (C-C)-циклоалкил-(C-C)-алкил, галоген-(C-C)-циклоалкил-(C-C)-алкил, COR, COOR, OCOOR, NRCOOR, C(O)N(R), NRC(O)N(R), OC(O)N(R), C(O)NROR, OR, OCOR, OSOR, S(O)R, SOOR, SON(R), NRSOR, NROR, (C-C)-алкил-S(O)R, (C-C)-алкил-OR, (C-C)-алкил-OCOR, (C-C)-алкил-OSOR, (C-C)-алкил-COR, (C-C)-алкил-SOOR, (C-C)-алкил-CON(R), (C-C)алкил-SON(R), (C-C)-алкил-NRCOR, (C-C)-алкил-NRSOR, N(R), P(O)(OR), CHP(O)(OR), гетероарил, гетероциклил, фенил, (C-C)-алкил-гетероарил или (C-C)-алкил-гетероциклил, где каждый из последних пяти указанных радикалов замещен радикалами, выбранными из группы, включающей галоген, нитро, циано, (C-C)-алкил, галоген-(C-C)-алкил, S(O)-(C-C)-алкил, (C-C)-алкокси и галоген-(C-C)-алкокси, и где гетероциклил несет n оксогрупп,Υ представляет собой нитро, галоген, циано, формил, родано, (C-C)-алкил, галоген-(C-C)-алкил, (C-C)-алкенил, галоген-(C-C)-алкенил, (C-C)-алкинил, галоген-(C-C)-алкинил, (C-C)-циклоалкил, галоген-(C-C)-циклоалкил, (C-C)-циклоалкил-(C-C)-алкил, галоген-(C-C)-циклоалкил-(C-C)-алкил, COR, COOR, OCOOR, NRCOOR, C(O)N(R), NRC(O)N(R), OC(O)N(R)C(O)NROR, OR, OSOR, S(O)R, SOOR, SON(R), NRSOR, NRCOR, (C-C)-алкил-S(O)R, (C-C)-алкил-OR, (C-C)-алкил-OCOR, (C-C)-алкил-OSOR, (C-C)-алкил-COR, (C-C)-алкил-SOOR, (C-C)-алкил-CON(R), (C-C)-алкил-SON(R), (C-C)-алкил-NRCOR, (C-C)-алкил-NRSOR, N(R), P(O)(OR), гетероарил, гетероциклил или фенил, где каждый из последних трех указанных радикалов замещен радикалами, выбранными из группы, включающей галоген, нитро, циано, (C-C)-алкил, галоген-(C-C)-алкил, (C-C)-циклоалкил, S(O)-(C-C)-алкил, (C-C)-алкокси и галоген-(C-C)-алкокси, и где ...

Oxime-ether-substituted benzoylamides having herbicidal activity

Α-substituted glycineamide derivative

The present invention provides: a novel α-substituted glycineamide derivative or a pharmacologically acceptable salt thereof; a pharmaceutical composition containing the α-substituted glycineamide derivative or a pharmacologically acceptable salt thereof; and a use of the α-substituted glycineamide derivative or a pharmacologically acceptable salt thereof for medical purposes. The present invention provides a compound which has an inhibitory activity on TRPM8 and is represented by general formula (I) [wherein A 1 represents a C 6-10 aryl group or the like; A 2 represents a C 6-10 aryl group or the like; X represents CH or the like; Y represents -CR 1 R 2 - or the like; R 1 and R 2 independently represent a hydrogen atom or the like; R 3 and R 4 independently represent a halogen atom or the like; and n represents 1 or 2] or a pharmacologically acceptable salt thereof. The compound (I) according to the present invention can be used as a therapeutic or prophylactic agent for diseases or conditions associated with afferent nerve hyperexcitability or injury.

Amidine derivative, preparation method thereof, pharmaceutical composition and application

本发明公开了一类脒类衍生物、及其制法和药物组合物与用途。具体而言，涉及通式I所示的脒类衍生物，其可药用盐，其立体异构体及其制备方法，含有一个或多个这化合物的组合物，和该类化合物在治疗与IDO1有关的疾病如癌症、感染性疾病、自身免疫性疾病方面的用途。

Patent RU2019110034A3

ВУ“? 2019110034`” АЗ Дата публикации: 28.01.2021 Форма № 18 ИЗИМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2019110034/04(019241Т) 27.09.2017 РСТД52017/053629 27.09.2017 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 62/401,093 28.09.2016 05 2. 62/459,461 15.02.2017 05 3. 62/554,939 06.09.2017 05 Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) МОДУЛЯТОРЫ КАЛЬПАИНА И ИХ ТЕРАПЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ Заявитель: БЛЭЙД ТЕРАПЬЮТИКС, ИНК., 05 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 233/05 (2006.01) (070 285/10 (2006.01) (070 413/12 (2006.01) (070 207/16 (2006.01) С07р 307/68 (2006.01) (070 413/14 (2006.01) С07О 209/20 (2006.01) С07О 307/84 (2006.01) (070 417/04 (2006.01) (070 209/42 (2006.01) (070 319/08 (2006.01) (070 417/14 (2006.01) (070 231/14 (2006.01) (070 333/38 (2006.01) (070 487/04 (2006.01) (070 233/90 (2006.01) (070 401/04 (2006.01) Аб/1К 31/4155 (2006.01) (070 235/18 (2006.01) (070 401/14 (2006.01) Аб/1К 31/4178 (2006.01) С07О 249/06 (2006.01) С07р 403/04 (2006.01) Аб/1К ...

Novel oxime derivatives of 3,5-seco-4-nor-cholestane, pharmaceutical compositions containing same, and method for production thereof

FIELD: chemistry. SUBSTANCE: invention relates to oxime derivatives of 3,5-seco-4-nor-cholestane of formula (I) use thereof as medicinal agents, having cytoprotective, specifically neuroprotective, cardioprotective and/or hepatoprotective action, as well as pharmaceutical compositions based thereon. In formula (I) R 1 is -CH 3 , R 2 is C 1 -C 8 alkyl group, optionally substituted with 1-4 substitutes selected from a halogen atom, a hydroxyl group or a group of formula R c -Q-(CH 2 ) n - (A), in which (i) n is an integer which can assume any value from 1 to 4; and (ii) Q is an oxygen atom or a -NR a group, in which R a is selected from a hydrogen atom or a C 1 -C 6 alkyl group, and R c is a hydrogen atom or a group of one of the formulae (C) or (D) or (iii) Q is a -O-C(O)- group or a -NR a -C(O)- group, in which R a is as defined earlier, and R c is a hydrogen atom or C 1 -C 6 alkyl, aryl, heteroaryl group, heterocycle, R 3 is a hydrogen atom; R 4 is a hydrogen atom; R 5 is a hydrogen atom or hydroxylamino group (-NH 2 -OH); or R 4 and R 5 togethr form an additional carbon-carbon bond between carbon atoms to which they are bonded; R 6 is a hydrogen atom; R 7 is a group selected from (G1, G2, G3, G4, G5 or G6) optionally substituted with a halogen atom or hydroxyl group. EFFECT: improved properties of compounds. 22 cl, 2 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 508 289 (13) C2 (51) МПК C07C 401/00 (2006.01) A61K 31/15 (2006.01) A61P 25/28 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2011131855/04, 17.12.2009 (24) Дата начала отсчета срока действия патента: 17.12.2009 (73) Патентообладатель(и): ТРОФО (FR) (43) Дата публикации заявки: 10.02.2013 Бюл. № 4 2 5 0 8 2 8 9 (45) Опубликовано: 27.02.2014 Бюл. № 6 (56) Список документов, цитированных в отчете о поиске: US 20080275130 A1, 06.11.2008. WO 20070101925, 13.09.2007. RU 2007112950 A, 20.10.2008. 2 5 0 8 2 8 9 R U (86) Заявка PCT: FR 2009/001434 (17. ...

New substituted n'-hydroxycarbamimidoyl-1,2,5-oxadiazole compounds as inhibitors of indolamine-2,3-dioxygenase (ido)

FIELD: chemistry.SUBSTANCE: invention relates to the field of pharmaceutical chemistry, namely, to a compound by the formula (Ib) or a pharmaceutically acceptable salt thereof. Wherein, in the formula (Ib), m represents 1 or 2; R is selected from the group consisting of: (a) -(C=O)-(NH)q-Rc, wherein q represents 0 or 1; and Rcis selected from the group consisting of: (i) hydrogen, (ii) -C1-4alkyl optionally substituted with one or two -OH, (iii) -C3-6cycloalkyl optionally substituted with -OH; (b) -S(O)2-NH2; and (c) -S(O)2-C1-4alkyl; R1is independently selected from (a) hydrogen and (b) halogen; and R2are independently selected from (a) hydrogen and (b) –OH. The invention also relates to a pharmaceutical composition and a method for treatment based on compounds by the formula (Ib), and to an application thereof.(Ib)EFFECT: compounds by the formula (Ib) as inhibitors of the IDO enzyme.9 cl, 3 tbl, 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 765 371 C2 (51) МПК C07D 271/08 (2006.01) C07D 413/12 (2006.01) A61K 31/4245 (2006.01) A61K 31/454 (2006.01) A61P 25/00 (2006.01) A61P 27/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61P 31/12 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61P 35/00 (2006.01) A61P 37/06 (2006.01) A61P 43/00 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 271/08 (2021.05); C07D 413/12 (2021.05); A61K 31/4245 (2021.05); A61K 31/454 (2021.05); A61P 25/00 (2021.05); A61P 27/12 (2021.05); A61P 31/12 (2021.05); A61P 35/00 (2021.05); A61P 37/06 (2021.05); A61P 43/00 (2021.05) 2019130589, 23.03.2018 (73) Патентообладатель(и): МЕРК ШАРП ЭНД ДОУМ КОРП. (US) (86) Заявка PCT: (56) Список документов, цитированных в отчете о поиске: US 2007/0173524 А1, 26.07.2007. US 2011/0165188 А1, 07.07.2011. AUSTIN et al.: "Carborane-Containing Hydroxyamidine Scaffolds as Novel Inhibitors of Indoleamine 2,3Dioxygenase 1 (ID01)", Aust. J. Chem., 2015, vol.68, no.12, p.1866 - 1870. US 2010/0015178 А1, 21.01.2010. WO 2007/075598 A2, 05.07.2007. EA 200702455 A1, 28.04.2008. 23 ...

Il-17a modulators and uses thereof

The disclosure herein provides compounds and pharmaceutical compositions for the modulation of IL-17A useful for the treatment of inflammatory conditions, such as psoriasis.

Method of obtaining derivatives of 1,2,5-oxadizol-3,4-bis-carbonic acid or their pharmaceutically acceptable acid-additive salts

Способ получени  производных 1,2,5-оксадиазол-З,4-бис-карбоновой кислоты общей структурной формулы (i| COR // N К 0 где R - группа -NHR -NIPR ; R2 - алкил, содержащий 1-6 атомов углерода, циклопенткл, циклогексил, аралкил, кото-- - рый может-быть незамещен или замещен 1 или 2 метоксигруппами , 2-пиридил-метил, -CHj-CH5-(CH2)m -ОСН,-груп па , в которой п) 0, и-пи 1,2-оксиэтил, 2-диэтил-амиа . но-этил; R и R - независимо друг от друга низший алкил или R и R вместе с атомом азота, с которым они св заны, образуют морЛолин, пиперидил или пирролил, или их фармаколог1гчески приемлемых кислотно-аддитивных солей, отличающийс  тем, что амид 1,2,5-оксадиазол-2-оксид-3,4-бис-карО ) боновой кислоты структурной формуCOR лы II N Л , NO/ 0 в которой R имеет указанные значени  , подвергают восстановлению три(Сд-С алкил )фосфитом, или три(С -С4-алкил)фосфином , или трифенилфосфином в инертном растворите ле при нагревании с последующим выделением целевого продукта в свободном виде или в виде соли. The method of obtaining 1,2,5-oxadiazole-3 derivatives, 4-bis-carboxylic acid of the general structural formula (i | COR // N K 0 where R is -NHR -NIPR group; R2 is alkyl containing 1-6 carbon atoms , cyclopentyl, cyclohexyl, aralkyl, which - ry can be unsubstituted or substituted by 1 or 2 methoxy groups, 2-pyridyl-methyl, -CHj-CH5- (CH2) m -OCH, -group pa, in which n) 0 , and-pi 1,2-hydroxyethyl, 2-diethyl-amia. no-ethyl; R and R are independently of each other lower alkyl or R and R together with the nitrogen atom to which they are bound form morLoline, piperidyl or pyrrolyl, or their pharmacologically acceptable acid addition salts, characterized in that amide 1,2, 5-oxadiazole-2-oxide-3,4-bis-carO) bonoic acid of the structural form COR ly II N L, NO / 0 in which R has the indicated values, is subjected to reduction of three (C-C alkyl) phosphite, or three (C -C4-alkyl) phosphine, or triphenylphosphine in an inert solvent when heated, followed by separation of the target product in the ...

Herbicidal 3 - ( sulfin- /sulfonimidoyl) - benzamides

Es werden Suifin- und Sulfonimidoylbenzamide der allgemeinen Formel (S) als Herbizide beschrieben. (I) In dieser Formel (I) stehen R, R', R", X, W und Z für Reste wie Wasserstoff, organische Reste wie Alkyl, und andere Reste wie Halogen. Q steht für einen Tetrazolyl-, Triazolyl oder Oxadiazolylrest.

N-(1,2,5-oxadiazol-3-yl)-, n-(1,3,4-oxadiazol-2-yl), n-(tetrazol-5-yl)- und n-(triazol-5-yl)-aryl carboxylic acid amides and use of same as herbicides