СПОСОБ ПОЛУЧЕНИЯ 1,4-ДИ-N-ОКИСИ-2,3-ДИМЕТИЛХИНОКСАЛИНА

Изобретение относится к химии гетероциклических соединений, а именно к способу получения 1,4-ди-N-окиси-2,3-диметилхиноксалина, и может найти применение в производстве лекарственных препаратов диоксидина хиноксидина. Описывается способ получения 1,4-ди-N-окиси-2,3-диметилхиноксалина конденсацией бензофуроксана и метилэтилкетона в органических низших спиртах в присутствии амина, при этом в качестве амина используют каталитическое количество гидрокарбоната аммония. Технический результат - предложен удобный, безопасный и экономичный способ получения целевого продукта, реализуемого в типовой аппаратуре. 2 з.п. ф-лы.

СПОСОБ ПОЛУЧЕНИЯ N-ОКСИДОВ 1-ГИДРОКСИ-3-(п-R-ФЕНАЦИЛ)-1,2,4a,5,6,7,8,8a-ОКТАГИДРО-2-ХИНОКСАЛОНОВ

Способ получения N-оксидов 1-гидрокси-3-(п-R-фенацил)-1,2,4а,5,6,7,8,8а-октагидро-2-хиноксалонов общей формулы I где R-OCH3, Cl, отличающийся тем, что 5-арил-2,3-дигидрофуран-2,3-дион общей формулы II где R-Cl или OCH3, подвергают кипячению с эквимолярным количеством 1,2-дигидроксиламиноциклогексана в среде абсолютного органического растворителя.

Способ получения производных 2-формилхиноксалиноксим-1,4диоксида

Способ получения 2-формил-3-карбонамидохиноксалин-ди- -окисей

Способ получения производных 1,4-диокиси хиноксалин-2карбоксамида или их солей

Способ получения производных метилхиноксалин-1,4-диоксида

Novel compounds of the general formula (I> <IMAGE> wherein R<1> stands for hydrogen or lower alkyl, R<2> is hydroxy and R<3> is hydrogen, or R<2> and R<3> form together a valence bond, Q represents a carbon or nitrogen atom, A is hydrogen, hydroxymethyl, lower alkyl, phenyl-lower alkyl or lower alkoxycarbonyl, n is 0 or 1, B stands for nitro, cyano, halogen, optionally halogeno- or nitro-substituted phenyl, pyridyl, quinolyl or a group of the general formula (IV), <IMAGE> in which R<5> is hydrogen or lower alkylcarbonyl and R<4> stands for nitro, amino, trifluoromethyl, lower alkyl or lower alkoxy, or A and B, together with the adjacent carbon atom to which they are attached, form a 5- or 6-membered, optionally substituted heterocyclic ring which contains not more than two identical or different nitrogen and/or oxygen and/or sulfur heteroatom(s) and optionally one or two exocyclic oxygen atom(s) and/or sulfur atom(s) and/or imino group(s), with the proviso that if Q represents a nitrogen atom, n is O and B stands for a group of the general formula (IV), and with the further proviso that if Q represents a carbon atom, B is other than a group of the general formula (IV), or a biologically acceptable acid addition salt of a compound of the general formula (I) with basic character, have antimicrobial activity and are of value as feed additives for use in animal husbandry.

Способ получения производных хиноксалиндиоксида

Способ получения производных хиноксалин-1,4-диоксида

Способ получения производных 2-хиноксалинил-1,4-диоксида

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 2-ХИНОКСАЛИНШ1- 1 , 4-ДИОКСИДА формулы I «J он М I i О где R - группа HOj -CH-CHj или 4-оксо 2 тион-5-тиаэолидинил, отличающийс  тем, что соединение формулы подвергают взаимодействию с соединением формулы И - R, где R имеет указанное значение, в присутствии основного катализатора , такого как пиперидин или гидроокись щелочного металла.

Способ получения метил-(2-хиноксалинилметилен)-карбазат-диоксида

Способ получения 3-замещенных -(2-хиноксалинилметилен)-карбазат , диоксида

Antibacterial 2-formyl-quinoxaline 1,4-di:oxide imine derivs. - prepd. e.g. by reaction of benzo:furoxane cpds. with alpha, beta-unsatd aldehyde e.g. crotonaldehyde imine(s)

New 2-formylquinoxaline 1,4-dioxide imine derivs. are cpds. of formula (I) where R1 and R2 are H or halogen; R3 is alkyl or cycloalkyl; and R4 is H, alkyl or aryl. (I) are useful as intermediates for antibacterially and nutritively active hydrazones of 2-formylquinoxaline 1,4-dioxides (DE 1620114).

Mittel zur Bekaempfung von Nematoden

VERFAHREN ZUR HERSTELLUNG DES CARBOMETHOXYHYDRAZONS DES 2-FORMYLCHINOXALIN- 1,4-DI-N-OXYDS

VERFAHREN ZUR HERSTELLUNG VON SUBSTITUIERTEN TETRALINEN, CHROMANEN UND VERWANDTEN VERBINDUNGEN, DIE BEI DER BEHANDLUNG VON ASTHMA VERWENDET WERDEN KOENNEN

CHINOLIN- UND CHINOXALIN-VERBINDUNGEN DIE DEN VON BLUTPLÄTTCHEN ABSTAMMMENDEN WACHSTUMSFAKTOR UND/ODER PDGF- UND P56lck-TYROSIN-KINASE HEMMEN

QUINOXALINE DERIVATIVES

... 1,237,438. Quinoxaline-1,4-dioxide derivatives. IMPERIAL CHEMICAL INDUSTRIES Ltd. 28 May, 1969 [17 June, 1968; 12 Sept., 1968], Nos. 28678/68 and 43452/68. Heading C2C. [Also in Division A5] Novel quinoxaline-1,4-dioxide derivatives of the formula wherein R1 is H, formyl, alkylcarbonyl, (haloalkyl)-carbonyl, alkoxycarbonylalkylcarbonyl, alkanesulphonyl, or alkoxycarbonyl and R2 is H or alkyl, but excluding 5-acetamidoquinoxaline-1,4-dioxide are prepared by oxidizing the corresponding 5-substituted quinoxaline derivative. 5-Amino-quinoxaline-1,4-dioxide is prepared by hydrolysing 5-trifluoroacetamidoquinoxaline-1,4-dioxide with sodium hydroxide. 7 - Methyl - 5 - acetamido., 5 - propionamido- and 5 - trifluoroacetamido - quinoxalines are prepared by reacting 5-aminoquinoxaline with the appropriate acid anhydride. 5 - Butyramido-, 5 - chloroacetamido- and 5- dichloroacetamido-quinoxalines are prepared by reacting 5-aminoquinoxaline with the corresponding acid chloride. 5 ...

3-METHYL-2-QUINOXALINECARBOXAMIDE-DI-N-OXIDES

... 1325581 Quinoxaline - 1,4 - di - N - oxides PFIZER Inc 9 July 1970 [22 July 1969 (2) 28 Jan 1970] 33489/70 Heading C2C [Also in Division A5] The invention comprises novel quinoxaline derivatives of the Formula III wherein X is a 6- or 7-position substituent selected from H, CH 3 , OCH 3 , Cl, F, CF 3 , sulphamoyl, N-methyl or N,N-dimethylsulphamoyl; Y is 6- or 7-position substituent selected from H, CH 3 , OCH 3 or Cl; R1 is H, CH 3 or CH 2 CH 3 ; R11 is C 1-4 alkyl N(R 3 )R 4 , C 1-4 alkyl OR 5 or C 1-4 alkyl COR 6 , wherein R 3 is H, R 4 is H or C 1-4 alkanoyl; or R 3 and R 4 when taken together with the N atom to which they are attached are 1 - [4 - (C 1-4 alkyl)piperazinyl]; R 5 is C 1-4 alkanoyl, R 6 is OH or NR 7 R 8 wherein R 7 and R 8 are H, CH 3 or CH 5 CH 3 ; or R1 and R11 when taken together with the N atom to which they are attached form a piperazine ring of the formula wherein W is C 1-4 alkyl, C 1-4 alkanoyl, CONH 2 , C 1-4 alkoxycarbonyl ...

2-1-PIPERAZINYL-QUINOXALINE COMPOUNDS HAVING PHARMACEUTICAL ACTIVITY

... 1440722 2 - (11 - Piperazinyl) - quinoxaline compounds MERCK & CO Inc 8 July 1974 [13 July 1973 29 April 1974] 30176/74 Heading C2C Novel 2 - (11 - piperazinyl) - quinoxaline compounds of the formula in which the dotted line indicates that the compounds are saturated or ethylenically unsaturated at the 3,4-position; R1 is oxygen; each of n and m is 0 or 1; R4 is oxygen, hydrogen, alkyl, or aminoalkyl and R3 is hydrogen, alkyl, alkoxycarbonyl, alkanoyl, aryl, substituted aryl, alkylthio, arylthio, alkoxy, amino, keto, alkylamino, dialkylamino, hydroxy, halo, carboxy, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl or alkylimino; or R4 and R3 are joined to form, together with the adjacent nitrogen and carbon atoms of the quinoxaline nucleus, a 5-to-7-membered ring; each of R5, R6, R7 and R8 is hydrogen, allyl, haloalkyl, haloalkylthio, arylalkyl, cycloalkyl, aroyl, alkyl, nitro, alkanoyl, ...

2-Halomethyl-Quinoxaline-1,4-di-N-Oxide-3-Carboxylic Acid Amides

... 1,188,249. 2 - Halomethyl - quinoxaline -1,4- di - N - oxide - 3 - carboxylic acid amide derivatives. FARBENFABRIKEN BAYER A.G. 3 Oct., 1968 [4 Oct., 1967], No. 47012/68. Heading C2C. Novel 2 - halomethyl quinoxaline - 1,4 - di- N - oxide - 3 - carboxylic acid amide derivatives of the general formula wherein R 1 is a hydrogen or chlorine atom or a C 1-4 alkyl or C 1-4 alkoxy group; R 2 is a hydrogen atom or an alkyl group optionally substituted by a hydroxy, C 1-4 alkoxy, C 1-5 carbalkoxy, acyloxy or mono- or di-C 1-4 alkylamino radical; R 3 is a hydrogen atom or an alkyl group optionally substituted by a hydroxy, C 1-4 alkoxy, C 1-5 carbalkoxy, acyloxy or mono- or di-C 1-4 alkylamino radical or, when R 2 is a hydrogen atom, a cyclohexyl group; or R 2 and R 3 , together with the nitrogen atom to which they are attached, form a 5- or 6-membered saturated heterocyclic ring which may contain a further nitrogen atom or an oxygen atom and the further nitrogen atom may be attached to a C 1-4 ...

2-TRIFLUOROMETHYL-QUINOXALINE-DI-N-OXIDES

... 1315524 Trifluoromethyl-quinoxaline-di-N- oxides PFIZER Inc 5 May 1970 [5 Feb 1970] 21671/70 Headings C2C and C2P Novel quinoxaline-di-N-oxides having the formulae wherein X is in the 6- or 7-position and is H, Cl, F, CH 3 , CH 3 O, CF 3 , SO 2 NH 2 , SO 2 NH(CH 3 ) or SO 2 N(CH 3 ) 2 ; Z is H, COOH, -COOC 1-4 alkyl, CONH 2 , Cl, F, Br, -SC 1-4 alkyl, -SOC 1-4 alkyl, -SO 2 C 1-4 alkyl, OH, -O-C 1-4 alkyl, -O.CO-C 1-3 alkyl, -NH 2 , -NHR1 or -NR1 2 (where R1 is C 1-4 alkyl), -N(CH 3 ) 3 or -ONO 2 ; R 1 is H or C 1-4 alkyl; R is H, -CO.O.C 1-4 alkyl, CONH 2 , Cl, Br, F, CN, -O-C 1-4 alkyl, -S-C 1-4 alkyl, -SOC 1-4 alkyl, -SO 2 C 1-4 alkyl, -NH 2 , -NHR1 or -NR1 2 (where R1 is C 1-4 alkyl), w,w,w-trifluoro C 1-4 alkyl, CF 3 CO, phenyl, cycloalkyl, di-(C 1-4 alkyl)N.CH 2 CH 2 -, -COR 2 , -CHO or -CH=N-R 5 , wherein R 5 is NHCONH 2 , NHCSNH 2 , NHC(NH)NH 2 , NHR 6 , NHCOOR 7 , NHCOR 8 , OR 9 , where R 6 is C 1-4 alkyl, benzyl, or C 2-4 hydroxyalkyl ...

QUINOXALINE-1,4-DIOXIDE DERIVATIVES

... 1462960 Quinoxaline-1,4-dioxide derivatives CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA RT 15 May 1974 [16 May 1973] 21632/74 Heading C2C Novel compounds of the Formula I wherein R is hydrogen, halogen, alkyl, alkoxy, nitro, cyano, carboxy, carbamoyl or alkoxycarbonyl and n is 1 or 2 where all alkyl groups have up to 6 carbon atoms and salts thereof where such exist, with the proviso that at least one R is other than hydrogen may be prepared by reacting a benzofuroxan of the Formula II with methyl-glyoxalaldoxime The process for preparing the compound I wherein all R groups are hydrogen is also claimed. Antimicrobial compositions comprise as active ingredient at least one compound of the Formula I (including that wherein all R groups are hydrogen) together with a carrier or diluent suitable for oral or parenteral administration.

PRODUCTION OF QUINOXALINE-DI-N-OXIDES AND BENZIMIDAZOLE MONO- AND DI-N-OXIDES

... 1,215,815. Quinoxaline and benzimidazole N- oxides. RESEARCH CORP. 20 Dec., 1967, No. 57874/67. Heading C2C. A process for producing quinoxaline di-N- oxides, benzimidazole-di-N-oxides and 1-hydroxybenzimidazole-3-oxides comprises reacting an isobenzofuroxan with a compound containing a methylene group which is activated by two electron withdrawing groups or a compound containing a methylene group which is activated by one electron withdrawing group, said one electron withdrawing group being a nitro group or a carbonyl group of a ketone or an aldehyde, in the presence of a base with the proviso in some cases that when a keto group is present in the molecule said base is not ammonia nor a primary aliphatic or cycloaliphatic amine. Examples of such compounds containing activated methylene groups include ketones, aldehydes, #-diketones, #-keto ester, malonic esters and nitroalkanes. The B ring of the heterocycle may be substituted by alkyl, cycloalkyl, aryl, aralkyl, alkoxy, carboxy, esterified ...

QUINOXALINE-DI-N-OXIDE-LACTONES

... 1,254,339. Quinoxaline-di-N-oxide-lactones. FARBENFABRIKEN BAYER A.G. 5 Nov., 1969 [8 Nov., 1968], No. 54242/69. Heading C2C. The invention comprises quinoxaline-di-N- oxide lactones of the general formula in which R 1 and R 2 (which may be the same or different) are hydrogen atoms, alkyl radicals containing 1-8 carbon atoms or chlorine atoms and a process for the preparation thereof in which a 2-acyloxy-methyl-3-carboxamidoquinoxaline-di-oxide-(1,4) of the general formula in which R 1 and R 2 (which may be the same or different) are hydrogen atoms, alkyl radicals having 1 to 8 carbon atoms or chlorine atoms, R 3 and R 4 (which may be the same or different) are hydrogen atoms, optionally substituted aliphatic radicals, optionally substituted aromatic radicals, or in the case where R 3 and R 4 are aliphatic they may form part of a 5- or 6-membered heterocyclic ring system and R 5 is an optionally substituted aliphatic or aromatic radical is reacted in a diluent with at least the theoretically ...

DERIVATIVES OF QUINOXALINE-1,4-DIOXIDES

9,10-DIHYDRO-9,10-METHANOANTHRACENE N-OXIDE DERIVATIVES AND THE PRODUCTION THEREOF

Novel dihydroxyhexanoic acid derivatives.

FUNGICIDES

Nitrogenated heterocyclic compound and agricultural or horticultural fungicide

Novel dihydroxyhexanoic acid derivatives.

Dihydroxyhexanoic acid derivatives of the greneral formula are useful to treat inflammation and other immune disorders.

Fungicides

Compounds having ...

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases.

This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor tyrosine kinase and/or tyrosine kinase, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or t cell activation and proliferation ...

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p56lck tyrosine kinases.

Quinoline and quhoxaline compounds which inhibit platelet-derived growth factor and /or p561ck tyrosine kinases.

FUNGICIDES

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Novel dihydroxyexanoic acid derivatives

Nitrogenated heterocyclic compound and agricultural or horticultural fungicide

Quinoline and quinoxaline compounds which inhibit platelet-derived growt factor and/or p561ck tyrosine kinases

Pesticides compositions.

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or p561ck tyrosine kinases

Quinoline and quinoxaline compounds which inhibit platelet-derived growt factor and/or p561 ck tyrosine kinases

New compositions for the weeding of the rice plantations.

Process for the preparation of new heterocyclic compounds.

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Quinoline and quinoxaline compounds which inhibit platelet-derived growth factor and/or P561CK tyrosine kinases

Novel dihydroxyexanoic acid derivatives

Nitrogenated heterocyclic compound and agricultural or horticultural fungicide

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

PROCEDURE FOR the PRODUCTION of NEW 2-FORMYLCHINOXALIN-1,4-DIOXID-ZYANACETYLHYDRAZO E

VERFAHREN ZUR HERSTELLUNG VON NEUEN CHINOXALIN-1,4-DIOXID-DERIVATEN UND VON DEREN SALZEN UND ISOMEREN

VERFAHREN ZUR HERSTELLUNG VON 2-FORMYL-CHINOXALIN-1,4-DIOXYD-OXIM-DERIVATEN

VERFAHREN ZUR HERSTELLUNG VON CHINOXALIN- -1,4-DIOXID-DERIVATEN

PROCEDURE FOR the PRODUCTION OF NEW ONES 3-SUBSTITUIERTEN CHINOXALIN-2-CARBOXAMID-1,4-DIOXIDEN AND THEIR SOUR ADDITION SALTS

PROCEDURE FOR THE PRODUCTION OF NEW CHINOXALIN-1,4-DIOXYD-DERIVATEN

PROCEDURE FOR the PRODUCTION OF 2-CARBOXAMIDEN of the 3-METHYLCHINOXALIN-N-1,4-DIOXID

PROCEDURE FOR THE PRODUCTION OF NEW CHINOXALIN-1,4-DIOXID-DERIVATEN AND OF THEIR SALTS AND ISOMERS

PROCEDURE FOR the PRODUCTION OF NEW CHINOXALIN DI - n OXIDE DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF A CHINOXALINVERBINDUNG

NEW CONDENSED HETERO-CYCLIC CONNECTIONS AND YOUR USE FOR CURES.

CHINOXALINVERBINDUNGEN AND THEIR PRODUCTION AND USE.

2 (2-HALO-4 (6-HALOQUINOXALIN-2YLOXY) PHENOXY) PROP. ION|URE DERIVATIVES, PROCEDURES FOR THEIR PRODUCTION, THESE CONTAINING HERBICIDES COMPOSITIONS AND YOUR USE AS HERBICIDES.

CONDENSED HETERO-CYCLIC CONNECTIONS, THEIR PRODUCTION AND USE

PROCEDURE FOR the PRODUCTION OF 2-CARBOXYPYRAZIN-4 OXIDES.

Procedure for the production of new Chinoxalinderivaten

Procedure for the production of 2-Hydroxyäthylestern of 2-Chinoxalincarbonsäure-1,4-di-N-oxyden

Procedure for the production new substituted Chinoxalin 1,4-dioxyde and their salts

PROCEDURE FOR THE PRODUCTION OF CHINOXALINCARBOXAMID-1,4-DIOXIDEN

PROCEDURE FOR THE PRODUCTION OF NEW CHINOXALIN DI N OXIDDERIVATEN

PROCEDURE FOR the PRODUCTION of the SCHIFF' BASES of the 2-FORMYL-CHINOXALIN-1,4-DIOXYDS

Procedure for the production of 1,6-Dihydroxyphenazin-5,10-dioxydderivaten

CHINOXALIN-2,3 (1H, 4H) - DIONE AS DRUGS

CONDENSED PYRAZINDERIVAT

Procedure for the production of new at the amide in ticking off substituted 2-Methyl-3-amidino-chinoxalin-di-N-oxiden (1,4),

Procedure for the production of the Chinoxalin di N OXIDE aldehyde

CHINOLIN AND CHINOXALIN CONNECTIONS THE OF BLOOD PANEL ABSTAMMMENDEN GROWTH FACTOR AND/OR PDGF AND P56LCK-TYROSIN-KINASE RESTRAINING

Procedure for the production of new 2-Amino-3-amidino-chinoxalin-di-N-oxyden

Procedure for the production of new 2-Methyl-3-carbonsäureamido-chinoxalin-di-N-oxiden (1,4)

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

GLYCINE RECEPTOR ANTAGONIST AND YOUR USE

QUINOXALINE COMPOUNDS AND THEIR PREPARATION AND USE

QUINOXALINE DERIVATIVES

HAPTEN CONJUGATES FOR TARGET DETECTION

Embodiments of hapten conjugates including a hapten, an optional linker, and a peroxidase-activatable aryl moiety are disclosed. In some embodiments, the peroxidase-activatable aryl moiety is tyramine or a tyramine derivative. Embodiments of methods for making and using the hapten conjugates also are disclosed. In particular embodiments, the hapten conjugates are used in a signal amplification assay. In certain embodiments, the hapten is an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, or 7-diethylamino-3-carboxycoumarin. The hapten is coupled to the peroxidase-activatable aryl moiety directly or indirectly via a linker. In certain embodiments, the hapten conjugates are used in multiplexed assays. 1. A hapten conjugate , comprising:a hapten selected from an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an azoaryl, a benzodiazepine, 2,3,6,7-tetrahydro-11-oxo-1H,5H,11H-[1]benzopyrano[6,7,8-ij]quinolizine-10-carboxylic acid, or 7-diethylamino-3-carboxycoumarin;a linker; anda tyramine or a tyramine derivative.2. (canceled)6. (canceled)811.-. (canceled)1332.-. (canceled)33. A method , comprising:(a) immobilizing a first peroxidase on a first target in a sample, wherein the first peroxidase is capable of reacting with a peroxidase-activatable aryl moiety;(b) contacting the sample with a solution comprising a first hapten conjugate, the first hapten conjugate comprising a first hapten selected from an oxazole, a pyrazole, a thiazole, a benzofurazan, a triterpene, a urea, a thiourea other than a rhodamine thiourea, a nitroaryl other than dinitrophenyl or trinitrophenyl, a rotenoid, a cyclolignan, a heterobiaryl, an ...

TREATING PROTEIN FOLDING DISORDERS WITH SMALL MOLECULE CFTR CORRECTORS

Novel CFTR corrector compounds that are effective in rescuing halide efflux in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of screening for CFTR corrector compounds are also described herein. The methods of screening include contacting a cell that endogenously expresses a CFTR mutation with the compound to be screened and detecting a rescue of halide efflux from the cell. 158-. (canceled)6058. The method of claim , wherein L is —CH—.6158. The method of claim , wherein L is —CH—CH—.6258. The method of claim , wherein Z is substituted or unsubstituted aryl.6358. The method of claim , wherein the protein folding disorder is cystic fibrosis.65. The method of claim 63 , wherein the protein folding disorder is cystic fibrosis.68. The method of claim 65 , wherein the protein folding disorder is cystic fibrosis. This application claims priority to U.S. Provisional Application No. 61/486,929, filed May 17, 2011, which is incorporated herein by reference in its entirety.This invention was made with government support under Grant Nos. NIDDK R01 DK060065 and NIDDK Phase I SBIR DK084658 awarded by the National Institutes of Health. The government has certain rights in the invention.Cystic fibrosis is an example of a protein folding disorder. It is a hereditary disease caused by mutations in a gene encoding the cystic fibrosis transmembrane conductance regulator (CFTR). The CFTR gene encodes a chloride channel that is expressed in multiple epithelial cell types. A common CFTR mutation, delF508, causes the failure of CFTR to traffic correctly to the plasma membrane because of protein misfolding. The delF508 mutation is estimated to account for 90% of mutant alleles. Because of its high degree of incidence in the cystic fibrosis population, delF508-CFTR is a prime target for cystic fibrosis ...

Quinoxaline Compounds and Derivatives

The present invention provides oxazine compounds, method of using and method of making oxazine compounds and its pharmaceutical use. 4. The composition of claim 3 , wherein A is an N and B claim 3 , B′ and A′ are C; or wherein A is an O and B claim 3 , B′ and A′ are C. This patent application is a Divisional application and claims priority based on U.S. patent application Ser. No. 13/428,616, which is a non-provisional patent application of U.S. provisional patent application 61/467,323 filed on Mar. 24, 2011 and entitled “Quinoxaline Compounds and Derivatives”, and U.S. provisional patent application 61/467,335 filed on Mar. 24, 2011 and entitled “Aromatic Neuroprotecting Compounds and Derivatives Thereof” the content of each of which is hereby incorporated by reference in its entirety.Not Applicable.Not Applicable.Not Applicable.The present invention relates in general to the field of pharmaceutical compositions and synthesis, and more particularly, to novel compositions and methods for preparing the compound and its pharmaceutical use.U.S. Patent Application Publication No. 2009/0286797, entitled, Novel Quinoxaline Derivatives and Their Medical Use discloses novel quinoxaline derivatives having medical utility, to use of the quinoxaline derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the quinoxaline derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to positive modulation of AMPA receptor mediated synaptic responses.U.S. Pat. No. 3,759,912, entitled, Quinoxalines discloses a Quinoxaline useful as broad spectrum antimicrobials in human and veterinary medicine; novel intermediates useful in their preparation; processes for their production from the appropriate quinoxaline, N-monoxide quinoxaline, quinoxaline carboxylic acid or furazan oxide are disclosed.The present invention provides a compound of ...

Quaternary heteroatom containing compounds

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.

COMPOUNDS AND METHODS FOR ANALYSIS AND SYNTHESIS OF SACCHARIDE COMPOUNDS

Provided is an isotope-labelled compound having a general formula IIa′, S-Y′-BIM, wherein S is a sugar moiety, Y′ is an isotope-containing sensor moiety and BIM is a benzimidazole. The compound may be used as an agent for saccharide analysis by magnetic resonance spectroscopy (NMR). A new glycan sequencing method and a glycoprotein synthesis method by using these compounds are also provided. 1. An isotope-labelled compound having a general formula IIa′ , S-Y′-BIM , wherein S is a sugar moiety , Y′ is an isotope-containing sensor moiety and BIM is a benzimidazole.2. The isotope-labelled compound of claim 1 , which is used as an agent for saccharide analysis by magnetic resonance spectroscopy (NMR).3. The isotope labelled compound of claim 1 , wherein the isotope-containing sensor moiety is an isotope.4. The isotope labelled compound of claim 3 , wherein the isotope is an isotope of hydrogen or halogen.5. The isotope labelled compound of claim 4 , wherein the isotope is selected from the group consisting of H claim 4 , H claim 4 , H claim 4 , F claim 4 , Cl claim 4 , Cl claim 4 , Br claim 4 , and Br.6. The isotope labelled compound of claim 3 , wherein the isotope is selected from the group consisting of H claim 3 , H claim 3 , H claim 3 , B claim 3 , B claim 3 , B claim 3 , C claim 3 , C claim 3 , C claim 3 , N claim 3 , N claim 3 , O claim 3 , O claim 3 , F claim 3 , P claim 3 , S claim 3 , Cl claim 3 , Cl claim 3 , Br claim 3 , and Br.7. The isotope labelled compound of claim 1 , which is selected from the group consisting of(1R,2S,3R)-1-(5-fluoro-1H-benzo[d]imidazole-2-yl)butane-1,2,3,4-tetraol;(1S,2R,3S,4R)-1-(5-fluoro-1H-benzo[d]imidazole-2-yl)pentane-1,2,3,4-tetraol;(1S,2R,3S,4R)-1-(5-fluoro-1H-benzo[d]imidazole-2-yl)pentane-1,2,3,4,5-pentaol;(1S,2R,3S)-1-(5-fluoro-1H-benzo[d]imidazole-2-yl)-1,2,3,4-tetrahydroxy pentanoic acid;N-((1 S,2R,3S,4R)-1-(5-fluoro-1H-benzo[d]imidazol-2-yl)-2,3,4,5-tetrahydroxypentyl)-acetamide;(2R,3S,4R,5S)-5-amino-5-(5-fluoro-1H-benzo ...

QUATERNARY HETEROATOM CONTAINING COMPOUNDS

The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): 130-. (canceled)32. The compound of claim 31 , wherein Rand Rcombine to form a carbonyl group.33. The compound of claim 31 , wherein Rand Y combine to form a ring with Q claim 31 , the ring including between 3 and 12 ring atoms.34. The compound of claim 33 , wherein the ring includes between 4 and 7 ring atoms.37. The compound of claim 36 , wherein the compound comprises one of a (+) enantiomer of the compound or a (−) enantiomer of the compound in an enantiomeric excess of greater than 50%.39. The compound of claim 38 , wherein the compound comprises one of a (+) enantiomer of the compound or a (−) enantiomer of the compound in an enantiomeric excess of greater than 50%.40. The compound of claim 38 , wherein:{'sup': '1', 'Ris selected from halogen, alkyl, optionally substituted aralkyl, optionally substituted alkoxycarbonylalkyl, optionally substituted cyanoalkyl, and optionally substituted hydroxyalkyl; and'}{'sup': 6', '9', '10, 'R, R, and Rare independently selected at each occurrence from aralkyloxy, aralkoxycarbonyl, heteroaryloxy, acyl, arylcarbonyl, aralkylcarbonyl, arylsulfonyl, alkoxycarbonyl, and aryloxycarbonyl.'}41. The compound of claim 40 , wherein:{'sup': '6', 'X is —NR—;'}{'sup': 7', '7, 'Z is selected from —C(O)— and —CRR—;'}{'sup': 7', '7, 'A at each occurrence is —CRR—;'}{'sup': 10', '11', '11, 'W is selected from —NR— and —CRR—; and'}n is 0-2.42. The compound of claim 41 , wherein n is 1.43. The compound of claim 38 , wherein:X is —O—;{'sup': 7', '7, 'Z is selected from —C(O)— and —CRR—;'}{'sup': 7', '7, 'A at each occurrence is —CRR—;'}{'sup': 10', '11', '11, 'W is selected from —NR—, and —CRR—; and'}n is 0-2.45. The method of claim 44 , wherein:{'sup': '6', 'X is —NR—;'}{'sup': 7', '7, 'A at each occurrence is —CRR—;'}{'sup': 10', '11', '11, 'W is selected from — ...

Heterocyclic Naphthoquinones Derivatives for Use in the Treatment of Cancers Including Cushing Disease

The present invention concerns heterocyclic naphthoquinones derivatives for use in the treatment of Cushing disease and other cancers, in particular via the inhibition of Ubiquitin Specific Proteases (USP) 8 and/or 2. 6. The method according to claim 1 , wherein Rrepresents a C-Clinear or branched alkyl group claim 1 , a C-Ccycloalkyl group claim 1 , an aryl claim 1 , a C-C-membered heteroaryl;{'sub': 1', '10', '3', '10', '5', '10, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'said C-Clinear or branched alkyl group, C-Ccycloalkyl group and C-C-membered heteroaryl being optionally substituted as defined in ;'}{'sub': 5', '10, 'claim-text': [{'sub': 1', '10, 'a C-Clinear or branched alkyl group;'}, {'sub': 3', '10, 'a C-Ccycloalkyl group;'}, {'sub': 1', '10', '3', '10', 'ii', 'ii', 'ii, 'a phenyl optionally substituted by at least one group selected from a C-Clinear or branched alkyl group, a C-Ccycloalkyl group, an halogen, a —ORgroup, an amine of formula —NR′R″, a nitrile or a nitro group;'}, '—F;', {'sub': i', 'i', 'i, 'a —ORgroup; two adjacent —ORgroups forming possibly with the two C atoms bearing said —ORgroups a 1,4-dioxane ring;'}, {'sub': i', 'i, 'an amine of formula —NR′R″;'}, 'a nitrile;', 'a nitro group;', {'sub': '3', 'a CFgroup.'}], 'said aryl or C-C-membered heteroaryl being optionally substituted by at least one group selected from8. The method according to claim 1 , wherein said cancer is selected from the group comprising prostate cancer claim 1 , bladder cancer claim 1 , breast cancer claim 1 , lung cancer claim 1 , colorectal cancer claim 1 , pituitary adenomas and Cushing's disease.9. The method according to claim 1 , wherein the compound is administered in an amount effect to inhibit USP2 and/or USP8.10. The method according to wherein the compound is administered in an amount effective to inhibit USP2 claim 9 , and said cancer being selected from the group comprising prostate cancer claim 9 , bladder cancer and breast cancer.12. The method ...

CRYSTALLINE COMPOUNDS

Provided herein are various polymorph forms of N-(3-{[(2Z)-3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]sulfamoyl}phenyl)-2-methylalaninamide. 1. Polymorph E of N-(3-{[(2Z)-3-[(2-chloro-5-methoxyphenyl)amino]quinoxalin-2(1H)-ylidene]sulfamoyl}phenyl)-2-methylalaninamide.2. The polymorph of claim 1 , wherein the polymorph exhibits an X-ray powder diffraction pattern having characteristic peaks expressed in degrees 2-Theta at angles of 18.3°±0.3° and 24.4°±0.3°.3. The polymorph of claim 1 , wherein the polymorph exhibits characteristic peaks at angles of 18.8°±0.3° and 23.7°±0.3°.4. The polymorph of claim 1 , wherein the polymorph exhibits characteristic peaks at angles of 10.1°±0.3° and 28.3°±0.3°.5. The polymorph of claim 1 , wherein the polymorph exhibits characteristic peaks at angles of 9.8°±0.3° and 23.2°±0.3°.6. The polymorph of claim 1 , wherein the polymorph exhibits characteristic peaks at angles of 9.8°±0.3° claim 1 , 10.1°±0.3° claim 1 , 18.3°±0.3° claim 1 , 18.8°±0.3° claim 1 , 23.2°±0.3° claim 1 , 23.7°±0.3° claim 1 , 28.3 °±0.3° and 24.4°±0.3°.7. The polymorph of claim 1 , wherein the polymorph exhibits an X-ray powder diffraction pattern substantially in accordance with and Table 1.8. The polymorph of claim 1 , wherein the polymorph exhibits an FT-IR spectrum having characteristic peaks expressed in units of cm−1 at values of about 1682 claim 1 , about 1296 and about 1136.9. The polymorph of claim 1 , wherein the polymorph exhibits an FT-IR spectrum substantially in accordance with .10. The polymorph of claim 1 , wherein the polymorph exhibits a differential scanning calorimetry thermogram having a characteristic peak at a temperature of 232.6±2° C.11. The polymorph of claim 1 , wherein the polymorph exhibits a differential scanning calorimetry thermogram substantially in accordance with .12. The polymorph of claim 1 , wherein the polymorph exhibits a melting point of about 230-235° C.13. The polymorph of claim 12 , wherein the polymorph ...

PRODUCTION METHOD FOR 3,3-DIMETHYL-3,4-DIHYDRO-1H-QUINOXALIN-2-ONE DERIVATIVE AND INTERMEDIATE FOR SAID PRODUCTION METHOD

An object is to provide a novel production method suitable for industrial production of a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and a synthetic intermediate for the method. Provided is a method for producing a compound represented by formula (1): 3. The production method according to claim 2 , wherein{'sup': '1', 'Rin formula (6) is a hydrogen atom.'}7. The production method according to claim 6 , wherein{'sup': '1', 'Rin formula (6) is a hydrogen atom.'}11. The compound or the salt thereof according to claim 10 , whereinthe compound represented by formula (2) or the salt thereof is methyl 2-bromo-5-(1-methoxycarbonyl-1-methylethyl)aminobenzoate.13. The compound or the salt thereof according to claim 12 , whereinthe compound represented by formula (6) or the salt thereof is selected from the group consisting of 2-bromo-5-(1-carboxy-1-methylethyl)aminobenzoic acid and methyl 2-bromo-5-(1-carboxy-1-methylethyl)aminobenzoate.15. The production method according to claim 14 , wherein the step of introducing X is conducted by reacting the compound represented by formula (8) or the salt thereof with a halogenating agent selected from the group consisting of chlorine claim 14 , bromine claim 14 , 1 claim 14 ,3-dibromo-5 claim 14 ,5-dimethylhydantoin claim 14 , N-chlorosuccinimide claim 14 , N-bromosuccinimide claim 14 , tetrabutylammonium tribromide claim 14 , dimethylaminopyridine tribromide claim 14 , and 2 claim 14 ,4 claim 14 ,4 claim 14 ,6-tetrabromo-2 claim 14 ,5-cyclohexadienone.19. The compound or the salt thereof according to claim 18 , wherein the compound represented by formula (8) or the salt thereof is 8-methoxycarbonyl-3 claim 18 ,3-dimethyl-3 claim 18 ,4-dihydro-1H-quinoxalin-2-one. The present invention relates to a method for producing a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative and also to intermediates for the production method.As a 3,3-dimethyl-3,4-dihydro-1H-quinoxalin-2-one derivative, for example, Patent Literature 1 ...

Phosphatidylinositol 3-Kinase Inhibitors for the Treatment of Lymphoproliferative Malignancies

Methods are provided for treating a lymphoproliferative malignancy to a patient in need of such treatment, comprising administering to the patient an effective amount of compound A as described herein. 2. The method of claim 1 , wherein the Compound A or pharmaceutically acceptable salt thereof is administered at a continuous once daily dose in capsule form of about 600 mg.3. The method of claim 1 , wherein the Compound A or pharmaceutically acceptable salt thereof is administered at a continuous once daily dose in tablet form of about 200 to about 600 mg.4. The method of claim 1 , wherein the Compound A or pharmaceutically acceptable salt thereof is administered at a continuous once daily dose in tablet form of about 400 mg.54. The method of any of - claims 1 , wherein the patient fasts prior to the administration.65. The method of any of - claims 1 , wherein the lymphoproliferative malignancy is chronic lymphocytic leukemia/small lymphocytic lymphoma claims 1 , Hodgkin's lymphoma claims 1 , Waldenstrom's macroglobulinemia claims 1 , follicular lymphoma claims 1 , or diffuse large B-cell lymphoma or transformed lymphoma.76. The method of any of - claims 1 , wherein the lymphoproliferative malignancy is relapsed or refractory.87. The method of any of - claims 1 , wherein the effective amount produces at least one therapeutic effect selected from the group consisting of reduction in size of a tumor claims 1 , reduction in metastasis claims 1 , complete remission claims 1 , partial remission claims 1 , stable disease claims 1 , increase in overall response rate claims 1 , or a pathologic complete response. This application claims the benefit of priority of U.S. Provisional Application No. 61/553,990, filed Nov. 1, 2011, and U.S. Provisional Application No. 61/568,189, filed Dec. 8, 2011, the entire contents of which are incorporated herein by reference.Lymphoproliferative malignancies, including lymphomas and lymphocytic leukemia, are common malignancies with an ...

Compounds

Novel phenazine derivatives, methods for their preparation and their medical use, in particular as anti-neoplastic agents and anti-infective agents, are provided. Novel methods for the preparation of iodinin and myxin are also provided. 2. A compound as claimed in claim 1 , wherein any aryl group present is an optionally substituted phenyl group claim 1 , preferably unsubstituted phenyl.3. A compound as claimed in claim 1 , wherein any substituents which may be present on any one of groups Rto Rare independently selected from the following:halogen (e.g. F, Cl, Br or I),{'sub': 1-6', '1-3, 'Calkyl (preferably Calkyl, e.g. methyl),'}{'sub': 2', '2', '2', '2', '2', '1-6', '1-3, '—OR′, —SR′, —COR′, —CO(O)R′, —OC(O)NR′, —C(O)NR′, —S(O)R′, —S(O)R′, —S(O)OR′ and —S(O)NR′(where each R′ is independently selected from H or Calkyl (preferably Calkyl, e.g. methyl)),'}{'sub': 1-4', '3, 'Chaloalkyl (e.g. CF),'}—CN, and{'sub': '2', '—NO.'}4. A compound as claimed in claim 1 , wherein each of Rto Ris hydrogen.5. A compound as claimed in claim 1 ,{'sub': '1', 'wherein Ris hydrogen or methyl.'}6. A compound as claimed in claim 1 ,{'sub': 1-8', '1-6', '1-3', '1-6', '1-3, 'wherein L is a linker which is a Calkylene group (preferably a Calkylene group) optionally substituted by one or more groups selected from Calkyl (e.g. methyl), hydroxy, Calkoxy (preferably Calkoxy, e.g. methoxy),'}{'sub': '1-3', 'wherein one or more methylene groups within the backbone of the linker (e.g. one, two or three methylene groups) may each additionally be replaced by a group selected from —O—, —S—, —NH—, —NR—(where R is hydrogen or Calkyl, e.g. methyl), and —CO—,'}and wherein two adjacent methylene groups within the backbone of the linker may each additionally carry substituents which, together with the intervening atoms of the linker backbone, form an optionally substituted, saturated ring, preferably a 5- or 6-membered ring (e.g. a 5- or 6-membered ring in which one or more of the ring atoms (e.g. two ...

INDICATION OF NAPHTHO[2,3-F]QUINOXALINE-7,12-DIONE COMPOUND IN ALLEVIATING PAIN

Disclosed are naphtho[2,3-f]quinoxaline compounds and pharmaceutical composition thereof. The compounds of the invention have been demonstrated as having analgesic effects and therefore may be applicable for use as a novel agent in relieving acute or chronic pain. 2. The method as claimed in claim 1 , wherein the pain is one of an acute pain and a chronic pain caused by one selected from a group consisting of an inflammation claim 1 , an injury claim 1 , and a neuropathy.3. The method as claimed in claim 1 , wherein the pain is one of an acute pain and a chronic pain caused by one of a cancer and a cancer treatment.5. The method as claimed in claim 4 , wherein the pain is one of an acute pain and a chronic pain caused by one selected from a group consisting of an inflammation claim 4 , an injury claim 4 , and a neuropathy.6. The method as claimed in claim 4 , wherein the pain is one of an acute pain and a chronic pain caused by one of a cancer and a cancer treatment.8. The method as claimed in claim 7 , wherein the pharmaceutical compound is administered to the subject with a pharmaceutical excipient. This application claims benefit under 35 U.S.C. §119 of Taiwan Application No. 103108518, filed Mar. 11, 2014, the contents of which are incorporated by reference as if fully set forth.The present invention relates to naphtho[2,3-f]quinoxaline compounds and pharmaceutical compositions thereof, which demonstrates analgesic effects. In particular, the present invention relates to an application in the pharmaceutical field.Naphtho[2,3-f]quinoxaline-7,12-dione compounds such as Formula I and Formula II are kinds of anthraquinone derivatives containing a heterocyclic group, where the synthesis and the effectiveness of the compounds to inhibit cancer cell activity through stabilizing G-quadruplex construction to suppress telomerase activity are both disclosed in Taiwan Patent Application No. 097112087.The R4 is selected from hydrogen or methyl.The known tricyclic ...

Cancer Cell Growth Inhibitor, Anticancer Agent, and Method for Screening Same, as well as Novel Compound

A cancer cell proliferation inhibitor including at least one selected from compounds represented by Structural Formulae (1) to (8), wherein the cancer cell is at least one of a cancer cell overexpressing a wild-type epidermal growth factor receptor and a cancer cell expressing an epidermal growth factor receptor mutant vIII. 2. (canceled)4. The anti-cancer agent according to claim 3 , wherein the cancer is glioblastoma.5. A method for screening at least one of a cancer cell proliferation inhibitor and an anti-cancer agent claim 3 , the method comprising:culturing a NIH3T3 cell expressing an epidermal growth factor receptor mutant vIII in a medium including a test substance under an environment without an adhesion scaffold;culturing a NIH3T3 cell in a medium including the test substance under an environment with an adhesion scaffold; andevaluating the test substance as having an activity as at least one of the cancer cell proliferation inhibitor and the anti-cancer agent when the test substance does not inhibit proliferation of the NIH3T3 cell, but inhibits proliferation of the NIH3T3 cell expressing an epidermal growth factor receptor mutant vIII.9. The method for inhibiting proliferation of a cancer cell according to claim 8 , wherein the method uses at least one selected from the compounds represented by Structural Formulae (1) claim 8 , (6) claim 8 , and (8).11. The method according to claim 10 , wherein the cancer is glioblastoma. The present invention relates to a cancer cell proliferation inhibitor that is capable of inhibiting proliferation of at least one of a cancer cell overexpressing a wild-type epidermal growth factor receptor and a cancer cell expressing an epidermal growth factor receptor mutant vIII; an anti-cancer agent that includes the cancer cell proliferation inhibitor; a screening method of the cancer cell proliferation inhibitor or the anti-cancer agent; and a novel compound suitable for the cancer cell proliferation inhibitor and the anti- ...

Compounds and methods for analysis and synthesis of saccharide compounds, and method for quantitating saccharide

Provided is a method for quantitating a saccharide in a liquid sample. The method comprises incubating the liquid sample with 2,3-naphthalenediamine in the presence of iodine to allow a naphthimidazole group to be linked to the saccharide to obtain a first mixture; obtaining an 1 H-NMR spectrum of the first mixture; and comparing, in said 1 H-NMR spectrum, the intensity or integral of a proton signal corresponding to the saccharide to the intensity or integral of a proton signal corresponding to an internal standard present in the first mixture.

Quaternary heteroatom containing compounds

with a transition metal catalyst and under alkylation conditions as valence and stability permit.

New quinolinium dyes and borates in photopolymerizable compositions

Dye compounds of the formula (see fig.1) (I),wherein X is for example CH, C-CH3 or +NOR L; R is inter alia C1-C6alkyl; R1 is for example C1-C8alkoxy or C1-C12alkyl; s is 0 to 4; R2 is for example hydrogen; Ar is for example a group , . (E); Y inter alia is C1-C6alkyl or C1-C6alkoxy; r in the formula (A) is 0 to 5, in the formulae (B) and (E) is 0 to 9 and in the formula (D) is 0 to 7; and L is an anion; in combination with an electron donor compound, especially a borate compound, are suitable as photoinitiators for the photopolymerization of radically polymerizable compositions.

Polymerisable composition

Compounds of formula (I), wherein X is CH, C-CH3, C-Cl, C-O-C1-C8alkyl or N; R is C1-C6alkyl, benzyl, CH2COOR3 or a group (a); R1 is C1-C8alkoxy, C1-C12alkyl, halogen, NO2, benzyloxy or phenyloxy, wherein the phenylring in the benzyloxy or phenyloxy group is unsubstituted or substituted by C1-C12alkyl, C1-C6alkoxy, halogen or CF3; R2 is C1-C8alkoxy, C1-C12alkyl, benzyloxy or phenyloxy, wherein the phenylring in the benzyloxy or phenyloxy group is unsubstituted or substituted by C1-C12alkyl, C1-C6alkoxy, halogen or CF3; R3 is hydrogen, C1-C12 alkyl or benzyl; Y is unsubstituted or C1-C6alkoxy-substituted C1-C6alkyl, or Y is C1-C6alkoxy, halogen, CF3, NO2, CF3O, benzyloxy or phenyloxy, wherein the phenylring in the benzyloxy or phenyloxy group is unsubstituted or substituted by C1-C12alkyl, C1-C6alkoxy, halogen or CF3 or, if n is two and both Y are alkoxy these alkoxy groups may form a dioxolane or dioxane fused to the phenyl of the styril residue; n is 1 to 4, preferably 1; and L is an anion; are useful as photoinitiators, especially in combination with borate anions.

Quorum sensing inhibitor against pathogenic microorganism and antibiotic composition therefrom

PURPOSE: A quorum sensing inhibitor and an antibacterial composition using the same are provided to suppress quorum sensing between bacteria, and to prevent or treat infection or diseases. CONSTITUTION: An antibacterial composition using a quorum sensing inhibitor against a pathogenic microorganism contains 1-(5-bromothiophene-2-sulfonyl)-1H pyrazole of chemical formula 1 as an active ingredient. The antibacterial composition is a pharmaceutical composition, a feed composition, a food composition, and a food additive composition.

Nitrogenated heterocyclic compound and agricultural or horticultural bactericidal agent

농원예용 살균제는 식 (I) (식 중, R 은 CR 1 R 2 R 3 으로 나타내는 기 또는 시아노기를 나타내고, R 1 ∼ R 3 은 수소 원자, 알킬기, 수산기 등을 나타내고, X 1 은 할로게노기 등을 나타내고, m 은 0 ∼ 5 중 어느 정수이고, X 2 는 할로게노기 등을 나타내고, n 은 0 ∼ 3 중 어느 정수이고, B 는 탄소 원자 또는 질소 원자를 나타내고, D 는 5 ∼ 7 원자 탄화수소 고리를 나타내고, A 1 ∼ A 4 는 탄소 원자 또는 질소 원자를 나타내지만, B 가 탄소 원자인 경우, A 1 ∼ A 4 모두가 탄소 원자인 경우는 없다) 로 나타내는 함질소 헤테로 고리 화합물 및 그 염으로부터 선택되는 적어도 1 종을 유효 성분으로서 함유한다. The antimicrobial agent for agricultural or horticultural use has the formula (I) (Wherein R represents a group represented by CR 1 R 2 R 3 or a cyano group, R 1 to R 3 represent a hydrogen atom, an alkyl group, a hydroxyl group, etc., X 1 represents a halogeno group, - and any of the five integers, X 2 denotes the like halogeno, n is any integer of 0 ~ 3, B represents a carbon atom or a nitrogen atom, D represents a 5 to 7 atom hydrocarbon ring, a 1 To A 4 represent a carbon atom or a nitrogen atom, provided that when B is a carbon atom, all of A 1 to A 4 may not be carbon atoms) and at least one As an active ingredient.

Synthesis method of quinoxaline derivatives by microwave irradiation

Methods and compositions for inhibiting cell proliferative disorders

The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers characterized by over-activity or inappropriate activity HER2 or EGFR.

Method of producing derivatives of quinoxaline-1,4-dioxide

Quinoxaline-1,4-derivatives are described having the general formula /I/ and biologically acceptable salts thereof, <IMAGE> wherein Q is hydrogen or methyl, R1 represents hydrogen, cyano, lower alkanoyl or nitro or halogen, R2 stands for cyano, lower alkanoyl, or a group of the general formula -COOR3, -CONR4R5 or -CO-NH-NR4R5, and R3 represents hydrogen or C1-18 alkyl, C6-12 aryl or C6-10 aryl-/C1-4 alkyl/ optionally substituted by halogen or hydroxy, whereby the aromatic ring of the said groups may optionally contain 1-3 identical or different substituents selected from lower alkyl or alkoxy, amino, nitro, halogen and/or hydroxy, R4 and R5 are various substituents, or R4 and R5 represent, together with the adjacent nitrogen atom, a 5 or 6 membered heterocyclic group optionally substituted by a further nitrogen or oxygen atom, with the proviso that if Q represents hydrogen and R2 stands for carboxy, R1 may denote only other than hydrogen. Processes for the preparation of the above compounds and fodder concentrates, fodder additives or fodders containing the said compounds are also described. The new compounds of the general formula /I/ possess weight-gain increasing and antibacterial effects and can be used to advantage in animal husbandry.

Polymerisable composition

Polymerisable composition

Compounds of formula (I), wherein X is CH, C-CH3, C-Cl, C-O-C1-C8alkyl or N; R is C1-C6alkyl, benzyl, CH2COOR3 or a group (a); R1 is C1-C8alkoxy, C1-C12alkyl, halogen, NO2, benzyloxy or phenyloxy, wherein the phenylring in the benzyloxy or phenyloxy group is unsubstituted or substituted by C1-C12alkyl, C1-C6alkoxy, halogen or CF3; R2 is C1-C8alkoxy, C1-C12alkyl, benzyloxy or phenyloxy, wherein the phenylring in the benzyloxy or phenyloxy group is unsubstituted or substituted by C1-C12alkyl, C1-C6alkoxy, halogen or CF3; R3 is hydrogen, C1-C12 alkyl or benzyl; Y is unsubstituted or C1-C6alkoxy-substituted C1-C6alkyl, or Y is C1-C6alkoxy, halogen, CF3, NO2, CF3O, benzyloxy or phenyloxy, wherein the phenylring in the benzyloxy or phenyloxy group is unsubstituted or substituted by C1-C12alkyl, C1-C6alkoxy, halogen or CF3 or, if n is two and both Y are alkoxy these alkoxy groups may form a dioxolane or dioxane fused to the phenyl of the styril residue; n is 1 to 4, preferably 1; and L is an anion; are useful as photoinitiators, especially in combination with borate anions.

Method of destroying unwanted plants

СПОСОБ УНИЧТОЖЕНИЯ НЕЖЕЛАТЕЛЬНОЙ РАСТИТЕЛЬНОСТИ .путеМ;обработки ее или почвы, на которой она произрастает, производными азотсодержащего гетероциклического соединени , отличающийс  тем, что, с целью повышени  эффективности способа, в качестве производного азотсодержащего гетероциклического соединени  используют соединение общей формулы METHOD FOR DESTROYING UNDESIRABLE VEGETATION by means of treating it or the soil on which it grows, derivatives of a nitrogen-containing heterocyclic compound, characterized in that, in order to increase the efficiency of the method, a compound of the general formula containing nitrogen is used as a nitrogen-containing heterocyclic compound.

Aminemethylene-quinoxaline-1,4-dioxide as well as preparation method and application thereof

本发明公开了一种胺亚甲基-喹喔啉-1，4-二氧化物的制备方法为：乙酰甲喹与双－（二甲胺）甲烷或双－（二乙胺）甲烷或双－（哌啶）甲烷发生曼尼希反应生成胺亚甲基-喹喔啉-1，4-二氧化物。本发明合成的胺亚甲基-喹喔啉-1，4-二氧化物(a、b、c)是由本申请人在喹的基础上合成的一种新型兽药，不溶于水，可溶于二氧六环和二甲亚砜，其结构母环和喹乙醇结构母环(喹叨嗪)相同。其活性实验表明，对大肠杆菌C 83-1 ，绿脓杆菌C 79-6 ，沙门氏菌 1014 ，克雷伯菌 219 等具有良好的抑菌活性。其中，本发明制备的哌啶亚甲基-喹喔啉-1，4-二氧化物（c）最好，可作为一种新型兽药，在治疗细菌性疾病方面得到应用。

Quinoxaline derivatives having inhibitory activity against histone deacetylase and preparation thereof

발명은 하기 화학식 1의 퀴녹살린 유도체, 이의 제조방법 및 이를 함유하는 항암 조성물에 관한 것으로, 본 발명의 퀴녹살린 유도체는 히스톤 디아세틸라제의 효소활성을 효과적으로 억제하여 종양세포의 증식을 억제할 수 있다. The present invention relates to a quinoxaline derivative of Formula 1, a method for preparing the same, and an anticancer composition containing the same, wherein the quinoxaline derivative of the present invention can effectively inhibit the enzymatic activity of histone deacetylase to inhibit the proliferation of tumor cells. . 상기 식에서, Where R 1 은 히드록시, 할로겐, 알킬옥시, 알킬, 아미노, 알킬아미노, 카르복실, 니트로, 아미드 및 술폰으로 이루어진 군으로부터 선택된 하나 이상의 치환체로 치환되거나 치환되지 않은, 아릴, 헤테로아릴 또는 C 3-8 사이클로알킬이고, 이때 상기 헤테로아릴은 고리 중에 질소, 황 또는 산소를 하나 이상 포함하며; R 1 is aryl, heteroaryl or C 3-8 unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxy, halogen, alkyloxy, alkyl, amino, alkylamino, carboxyl, nitro, amide and sulfone Cycloalkyl, wherein the heteroaryl comprises one or more nitrogen, sulfur or oxygen in the ring; R 2 는 수소 또는 아릴알킬이고; R 2 is hydrogen or arylalkyl; A는 O, S, CH 2 , 술폰(SO 2 ), 술폭사이드(SO), CONH, NHCO, NX 또는 NXSO 2 (이때, X는 수소, C 1-5 알킬, 또는 독립적으로 상기 R 1 과 동일하게 정의된다)이고; A is O, S, CH 2 , sulfone (SO 2 ), sulfoxide (SO), CONH, NHCO, NX or NXSO 2 , wherein X is hydrogen, C 1-5 alkyl, or is independently the same as R 1 Is defined as; n은 0, 1, 2 또는 3이다. n is 0, 1, 2 or 3.

The method of obtaining 1-4-methyl-3- (2-quinoxalinylmethylene) carbazate

A kind of synthetic method of N- acetyl group quinoxaline -2- amide and its derivative

本发明公开了一种N‑乙酰基喹喔啉‑2‑酰胺及其衍生物的合成方法：以式Ⅰ或式Ⅲ所示的喹喔啉‑2‑甲醛为起始物，溶于混合溶剂中，在铜催化剂和氧化剂作用下，于40～80℃反应3～12小时，所得反应液经后处理分别得到式Ⅱ或式Ⅳ所示的N‑乙酰基喹喔啉‑2‑酰胺及其衍生物；所述的铜催化剂为三氟甲磺酸铜、醋酸铜或氯化铜；所述的氧化剂为过硫酸铵、过硫酸钾、2,3‑二氯‑5,6‑二氰基‑1,4‑苯醌或70％wt的过氧化叔丁醇水溶液中的一种或一种以上的混合物；所述的混合溶剂为体积比为5～100:1的乙腈和水的混合溶液；所述的催化剂与所述的氧化剂、式Ⅰ所示的喹喔啉‑2‑甲醛的物质的量之比为0.01～0.3：1～1.2：1。

A kind of synthetic method of -2 C-3 aroyl compounds of (1H) -one of quinoxaline

本发明公开了一种喹喔啉‑2(1H)‑酮C‑3位芳酰基化合物的合成方法，该方法是在空气气氛下，喹喔啉‑2(1H)‑酮衍生物、芳酰肼和过硫酸盐一锅反应生成喹喔啉‑2(1H)‑酮C‑3位芳酰基化合物。该方法具有原料易得、操作简便、反应条件、温和、反应选择性及产率高、底物官能团兼容性优异等特点。

Fodder for livestock

Novel compounds of the general formula (I> <IMAGE> wherein R<1> stands for hydrogen or lower alkyl, R<2> is hydroxy and R<3> is hydrogen, or R<2> and R<3> form together a valence bond, Q represents a carbon or nitrogen atom, A is hydrogen, hydroxymethyl, lower alkyl, phenyl-lower alkyl or lower alkoxycarbonyl, n is 0 or 1, B stands for nitro, cyano, halogen, optionally halogeno- or nitro-substituted phenyl, pyridyl, quinolyl or a group of the general formula (IV), <IMAGE> in which R<5> is hydrogen or lower alkylcarbonyl and R<4> stands for nitro, amino, trifluoromethyl, lower alkyl or lower alkoxy, or A and B, together with the adjacent carbon atom to which they are attached, form a 5- or 6-membered, optionally substituted heterocyclic ring which contains not more than two identical or different nitrogen and/or oxygen and/or sulfur heteroatom(s) and optionally one or two exocyclic oxygen atom(s) and/or sulfur atom(s) and/or imino group(s), with the proviso that if Q represents a nitrogen atom, n is O and B stands for a group of the general formula (IV), and with the further proviso that if Q represents a carbon atom, B is other than a group of the general formula (IV), or a biologically acceptable acid addition salt of a compound of the general formula (I) with basic character, have antimicrobial activity and are of value as feed additives for use in animal husbandry.

Method of producing rs-(2-quinoxalinyl-1,4-dioxide)-(4'-oxo-2'-tione-5'-tiazolidinyl)-methanol

СПОСОБ ПОЛУЧЕНИЯ RS- WAY OF OBTAINING RS-

Quinoxaline-di-N-oxide-lactones

Condensed heterocyclic compounds and its preparation method and application

由上式代表的新化合物及其盐，它们的制备和应 用。 其具有优良的抑制ACAT活性，降低血液胆固 醇以及抑制速激肽受体活性。

3-methyl-quinoxaline-2-carboxylic acid chemical synthesis method based on ionic liquid system

本发明属于化学合成技术领域，具体涉及一种新的基于离子液体系的高得率、高纯度、易操作的3-甲基-喹噁啉-2-羧酸化学合成方法：以邻苯二胺和α-卤代-β-酮酯为原料，采用离子液体作为溶剂体系和催化剂，经环化和水解两步反应，成功合成了目标产物3-甲基-喹噁啉-2-羧酸。本发明的核心是基于离子液体的溶剂特性和催化剂特性进行创新，使得环化反应室温下即可进行，产物得率和纯度都很高，且反应时间比较短，可降低能耗；同时，离子液体是一种不挥发的溶剂，能活化重复使用，可降低成本和减少对环境的污染。

Method of obtaining rs-(2-quinoxalinyl-1,4-dioxide)-(4-oxo-2-thion-5-thiazolinidyl)-methanol

Novel compounds of the general formula (I> <IMAGE> wherein R<1> stands for hydrogen or lower alkyl, R<2> is hydroxy and R<3> is hydrogen, or R<2> and R<3> form together a valence bond, Q represents a carbon or nitrogen atom, A is hydrogen, hydroxymethyl, lower alkyl, phenyl-lower alkyl or lower alkoxycarbonyl, n is 0 or 1, B stands for nitro, cyano, halogen, optionally halogeno- or nitro-substituted phenyl, pyridyl, quinolyl or a group of the general formula (IV), <IMAGE> in which R<5> is hydrogen or lower alkylcarbonyl and R<4> stands for nitro, amino, trifluoromethyl, lower alkyl or lower alkoxy, or A and B, together with the adjacent carbon atom to which they are attached, form a 5- or 6-membered, optionally substituted heterocyclic ring which contains not more than two identical or different nitrogen and/or oxygen and/or sulfur heteroatom(s) and optionally one or two exocyclic oxygen atom(s) and/or sulfur atom(s) and/or imino group(s), with the proviso that if Q represents a nitrogen atom, n is O and B stands for a group of the general formula (IV), and with the further proviso that if Q represents a carbon atom, B is other than a group of the general formula (IV), or a biologically acceptable acid addition salt of a compound of the general formula (I) with basic character, have antimicrobial activity and are of value as feed additives for use in animal husbandry.

The double aryl ureas of quinokysalines with VEGFR-2 and B-raf double inhibition effect and its derivative, preparation method and applications

本发明公开了一种具有VEGFR‑2/B‑Raf双重抑制活性的喹喔啉酮双芳基脲及其衍生物，其药学上可接受的盐，溶剂合物、其前药、其中间体、其代谢物或者是含有这种化合物作为活性物质的药物组合物，其结构通式如式(I)所示： 其中，R 1 、R 2 、R、Q、Y和Ar中的每一个都如本文中所定义。本发明还阐述了它们的制备方法、它们作为药物的用途和它们在治疗肿瘤中的应用。本发明的化合物疗效确切，毒副作用小，丰富了现有技术中用于与VEGFR‑2和(或)B‑Raf表达异常所引起疾病治疗药物的抑制剂的种类，有望成为治疗指数较高的可用于临床的药物。

Quinoxaline-1,4-dioxide derivatives possessing ability to gain increase in weight of animals

Novel compounds of the general formula (I> <IMAGE> wherein R<1> stands for hydrogen or lower alkyl, R<2> is hydroxy and R<3> is hydrogen, or R<2> and R<3> form together a valence bond, Q represents a carbon or nitrogen atom, A is hydrogen, hydroxymethyl, lower alkyl, phenyl-lower alkyl or lower alkoxycarbonyl, n is 0 or 1, B stands for nitro, cyano, halogen, optionally halogeno- or nitro-substituted phenyl, pyridyl, quinolyl or a group of the general formula (IV), <IMAGE> in which R<5> is hydrogen or lower alkylcarbonyl and R<4> stands for nitro, amino, trifluoromethyl, lower alkyl or lower alkoxy, or A and B, together with the adjacent carbon atom to which they are attached, form a 5- or 6-membered, optionally substituted heterocyclic ring which contains not more than two identical or different nitrogen and/or oxygen and/or sulfur heteroatom(s) and optionally one or two exocyclic oxygen atom(s) and/or sulfur atom(s) and/or imino group(s), with the proviso that if Q represents a nitrogen atom, n is O and B stands for a group of the general formula (IV), and with the further proviso that if Q represents a carbon atom, B is other than a group of the general formula (IV), or a biologically acceptable acid addition salt of a compound of the general formula (I) with basic character, have antimicrobial activity and are of value as feed additives for use in animal husbandry.

3-methyl-2-(methoxy styrene keto)-quinoxaline-1,4-dioxide, and preparation method and application thereof

本发明公开了3-甲基-2-（甲氧基苯乙烯酮基）-喹喔啉-1，4-二氧化物，其制备方法，采用一步法将乙酰甲喹与甲氧基苯甲醛通过羟醛缩合生成3-甲基-2-（甲氧基苯乙烯酮基）-喹喔啉-1，4-二氧化物。其活性实验表明，对大肠杆菌、金色葡萄球菌、绿脓杆菌、枯草芽孢杆菌等具有良好的抑菌活性。通过促生长及药物残留的研究，3-甲基-2-(甲氧基苯乙烯酮基)-喹喔啉-1,4-二氧化物（a）有较好的促生长作用，并且使用安全。本发明制备的3-甲基-2-(甲氧基苯乙烯酮基)-喹喔啉-1,4-二氧化物（a）可作为一种畜禽的抗菌促生长兽药饲料添加剂可以得到广泛应用。

Novel herbicides

Method of producing derivatives of 2-oxomethylquinoxaline-1,4-dioxide

New 2-hydroxymethyl-quinoxaline-1, 4-dioxide derivatives of the general formula (I) (FORMULA) wherein A represents an amino group, or a group of the general formula -NH-COOR<u1>u, wherein R<u1>u stands for a C<u2-4>u alkyl group, or a group of the general formula -NH-CX-NH<u2>u, wherein X denotes an oxygen or sulfur atom, or a group of the formula -NH-C(NH)-NH<u2>u, or a group of the general formula -NH-R<u2>u, wherein R<u2>u represents a C<u1-6>u alkyl, a phenyl, a benzyl, a hydroxyl or a hydroxy-(C<u2-4>ualkyl) group, or a group of the general formula -NH-CO-R<u3>u, wherein R<u3>u stands for a C<u1-20>u alkyl group or a phenyl group optionally substituted by one, two or three identical or different substituent(s) selected from the group consisting of nitro, hydroxyl, amino, C<u1-3>u alkoxy and halogen; a naphtyl group optionally substituted by a hydroxyl group a phenyl- (C<u1-3>u alkyl) group, a pyridyl, a piperidyl, a pyrazinyl, a pyrimidyl, a 1,2,4-triazinyl, a furyl, a nitrofuryl or an //c,//c-diphenyl-//c-hydroxymethyl group. Due to their antimicrobial and weight-gain increasing effects, the new compounds of the general formula (I) can serve as active ingredients of pharmaceutical or veterinary compositions, particularly fodder concentrates, fodder additives and fodders. The invention relates also to the preparation of the new compounds of the general formula (I) and the compositions containing same.

Condensed heterocyclic compounds, their production and use

With antibacterial activity quinoxalines-N1,N4Dioxide derivative

本发明属于药物化学合成技术领域，具体涉及具有抗菌活性的喹噁啉‑N 1 ,N 4 ‑二氧化物衍生物。本发明还包括该衍生物的制备及其抗菌活性测试。其中新合成的化合物是以N‑氧化苯并呋咱为原料，与丙二腈在碱性条件下发生贝鲁特反应，得到3‑氨基‑2‑氰基‑喹噁啉‑N 1 ,N 4 ‑二氧化物之后再与合适的酰氯反应得到一系列具有2‑氰基‑3‑酰胺基喹噁啉‑N 1 ,N 4 ‑二氧化物。体外抑菌活性测试结果显示：对人结核分支杆菌和牛结核分枝杆菌具有较好的抑菌活性；对金黄色葡萄球菌，肺炎链球菌，大肠杆菌和巴氏杆菌也具有抑菌活性。本发明还公开了作为靶标抗菌药物的化合物的结构式。

Method of producing quinoxaline derivatives

Novel compounds of the general formula (I> <IMAGE> wherein R<1> stands for hydrogen or lower alkyl, R<2> is hydroxy and R<3> is hydrogen, or R<2> and R<3> form together a valence bond, Q represents a carbon or nitrogen atom, A is hydrogen, hydroxymethyl, lower alkyl, phenyl-lower alkyl or lower alkoxycarbonyl, n is 0 or 1, B stands for nitro, cyano, halogen, optionally halogeno- or nitro-substituted phenyl, pyridyl, quinolyl or a group of the general formula (IV), <IMAGE> in which R<5> is hydrogen or lower alkylcarbonyl and R<4> stands for nitro, amino, trifluoromethyl, lower alkyl or lower alkoxy, or A and B, together with the adjacent carbon atom to which they are attached, form a 5- or 6-membered, optionally substituted heterocyclic ring which contains not more than two identical or different nitrogen and/or oxygen and/or sulfur heteroatom(s) and optionally one or two exocyclic oxygen atom(s) and/or sulfur atom(s) and/or imino group(s), with the proviso that if Q represents a nitrogen atom, n is O and B stands for a group of the general formula (IV), and with the further proviso that if Q represents a carbon atom, B is other than a group of the general formula (IV), or a biologically acceptable acid addition salt of a compound of the general formula (I) with basic character, have antimicrobial activity and are of value as feed additives for use in animal husbandry.

Synthetic method of 3-tert-butyl-N-methylquinoxaline-2 (1H) -ketone compound

本发明公开了一种3‑叔丁基‑N‑甲基喹喔啉‑2(1H)‑酮化合物的合成方法，该方法是在空气气氛下，N‑甲基喹喔啉‑2(1H)‑酮、肼基叔丁酯和过硫酸盐一锅反应合成3‑叔丁基‑N‑甲基喹喔啉‑2(1H)‑酮化合物。该方法具有原料易得、操作简便、反应条件温和、反应区域选择性及产率高等特点。

Sulfonamide compound

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to sulfonamide compound of the where R 1 means alkyl, alkenyl, alkynyl; A means optionally substituted heterocyclic group excepting for benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyl and 2,3-dihydrobenzoxazinyl; X means alkylene, oxa-group, oxa-(lower)-alkylene; R 2 means optionally substituted aryl, substituted biphenyl, its salt and pharmaceutical composition comprising this compound. The proposed sulfonamide compound is effective in treatment of diseases since it is able to decrease blood glucose level, to inhibit activity of cGMP-PDE (phosphodiesterase) and especially activity of PDE-V, to exhibit relaxing effect with respect to smooth muscles. Also, it exhibits bronchodilating activity, vasodilating activity, activity associated with suppression of smooth muscle cells and antiallergic activity. EFFECT: valuable medicinal properties of compound. 8 cl, 1 tbl, 399 ex ссчебс ПЧ сэ (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ” 2 199 532 ' С 070 215/48, 333/56, 333/54, (51) МПК? 13) С2 405/12, 409/42, 471/04, 487/04, 495/04, А 61 К 31/381 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 2000101813/04, 24.06.1998 (24) Дата начала действия патента: 24.06.1998 (30) Приоритет: 27.06.1997 УР 9/208295 24.04.1998 УР 10/114718 (46) Дата публикации: 27.02.2003 (56) Ссылки: ЗЧ 644790 А, 20.04.1979. \М!О 93/19067 АЛ, 30.09.1993. ЕР 507594 А 1,07.10.1992. (85) Дата перевода заявки РСТ на национальную фазу: 27.01.2000 (86) Заявка РСТ: УР 98/02877 (24.06.1998) (87) Публикация РСТ: М/О 99/00372 (07.01.1999) (98) Адрес для переписки: 129010, Москва, ул. Большая Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Н.Г. Лебедевой, рег.№ 112 (71) Заявитель: ФУДЗИСАВА ФАРМАСЬЮТИКАЛ КО., ЛТД. (4Р) (72) Изобретатель: КАЯКИРИ Хироси (+Р), АБЕ Йосито (УР), ХАМАСИМА Хитоси (/Р), САВАДА Хитоси (.Р), МИЗУТАНИ Цуйоси (/Р), ЯМАСАКИ Норицугу (ШР), ОНОМУРА ...

Agricultural antibacterial agent

2-Formylquinoxaline-1,4-dioxide-cyanoacetylhydrazone, process for its preparation and compositions with this compound

Method of preparing substituted quinoxalinediones or salts thereof

Photoinitiator system for photopolymerizable compositions containing a new styryl-substituted o-alkylated quinolium dye compound as electron acceptor, preferably with a borate compound as electron donor

New styryl-substituted, o-alkylated aromatic nitrogen-heterocyclic amine oxides used as electron acceptors in photostarter systems for photopolymerizable compositions, optionally in combination with electron donors, especially new borate compounds. Compound(s) of formula (I) are new: in which: X = CH, CCH3, C-Cl, CO-(1-8C alkyl) or <+>NOR L<->; R = 1-6C alkyl, benzyl, CH2COOR3, -Ar' or -CH2COAr'; Ar' = phenyl substituted with r groups Y1; R1 = 1-8C alkoxy, 1-12C alkyl, halogen, NO2, benzyloxy or phenoxy (both optionally ring-substituted with 1-12C alkyl, 1-6C alkoxy, halogen or CF3); s = 0-4; R2 = H, 1-8C alkoxy, 1-12C alkyl, benzyloxy or phenoxy (optionally substituted as above); R3 = H, 1-12C alkyl or benzyl; Ar = phenyl (A), biphenyl (B), -phenylene-CH=CH-phenyl (C), naphthyl (D), anthryl (E), pyrenyl (F), phenanthryl (G), a group of formula (H), (J) or (K), or -phenylene-N(phenyl)2 (L) (all except L optionally substituted with r groups Y); Y = 1-6C alkyl (optionally substituted with 1-6C alkoxy), or 1-6C alkoxy, halogen, CF3, NO2, CF3O, benxyloxy or phenoxy (both optionally ring-substituted as above), or if r = 2 or more and two Y groups are alkoxy, these alkoxy groups may form a condensed dioxolan or dioxan ring; Y1 = as for Y (excepting condensed-ring dioxolan and dioxan systems); W = O, S or CH2; W1 = O, S, C(R4)2 or CO; R4 = as for R2 (optionally ring-substituted with 1-12C alkyl or 1-6C alkoxy); r = 0-5 in formula (A) and in the groups -CH2COAr' and -Ar', r = 0-9 in formulae (B), (C), (E), (F), (G), r = 0-7 in (D), 0-3 in (H), 0-5 in (J) and 0-7 in (K), provided that if Ar = group (A), then R = 1-6C alkyl, benzyl, -CH2COOR3 or -CH2COAr', X is not <+>NOR L<->, r = 2-5 and L is an anion. Independent claims are also included for (a) a photo-starter system containing compound(s) (I) and optionally electron-donor compound(s); (b) compositions containing (A) polymerizable ethylenic compound(s) and (B) photo-starter ...

Treating protein folding disorders with small molecule cftr correctors

Patent FR2399416B1

Process for the preparation of a new series of schiff bases

Novel Compound and Anti-viral Composition Comprising the Same

본 발명은 하기 화학식 2로 표현되는 화합물, 하기 화학식 1 또는 화학식 2로 표현되는 화합물 또는 이의 약제학적으로 허용 가능한 염을 유효성분으로 함유하는 약학 조성물 및 사료 첨가제에 관한 것으로, 상기 화합물을 유효성분으로 함유하는 조성물들은 다른 정상 세포에 세포독성이 없어 안전하면서도, 돼지 호흡기 생식기 증후군 바이러스와 같이 질병을 유발시키는 바이러스의 증식 및 감염을 효과적으로 억제할 수 있으므로 바이러스 질환 예방 또는 치료제로 사용될 수 있다. [화학식 1] [화학식 2] The present invention relates to a pharmaceutical composition containing a compound represented by the following general formula (2), a compound represented by the following general formula (1) or (2) or a pharmaceutically acceptable salt thereof as an active ingredient, and a feed additive, Can be used safely because they are not cytotoxic to other normal cells and can be effectively used for preventing or treating viral diseases because they can effectively inhibit the proliferation and infection of viruses that cause disease such as swine respiratory tract syndrome virus. [Chemical Formula 1] (2)

Treatment of Mareks disease - with 2-sulphanilamidoimidazole or benzimi-dazole

Patent FR2210347B3

Process for the production of heterocyclic chlorine compounds

Quinoxaline n-oxides

Quinoxaline N-oxides. Compds. (I), useful as anti-bacterial agents (where R1 is a heterocyclic residue, R2 is H, a heterocyclic residue, an opt. substd. aliphatic hydrocarbon residue, an opt. substd. aryl residue, acyl, or carboxylic group opt. functionally modified and pH is opt. substd. o-phenylene) are prepd. by known methods for forming quinoxaline N-oxides esp. the reaction between a benzofuroxane and a vinyl deriv. R4.CH=C(R5)R6 where R4 and R5 form R1 and R2 and R6 is a group eliminated in the reaction.

Process for the preparation of quinoxaline di-nu-oxides

Patent FR2220524B1

Patent FR2210347A1

Patent FR2022925A1

PROCESS FOR THE PREPARATION OF 2-METHYLENE-QUINOXALINE-1,4-DIOXIDE DERIVATIVES

PROCEDE DE PREPARATION DE DERIVES DE 2-METHYLENE-QUINOXALINE-1,4-DIOXYDE REPRESENTES PAR LA FORMULE GENERALE I CI-APRES: (CF DESSIN DANS BOPI) CES DERIVES SONT OBTENUS PAR DESHYDRATATION DES 2-HYDROXYMETHYL-QUINOXALINE-1,4-DIOXYDES CORRESPONDANTS, A CHAUD OU EN PRESENCE D'AGENT DESHYDRATANT. PROCESS FOR PREPARING 2-METHYLENE-QUINOXALINE-1,4-DIOXIDE DERIVATIVES REPRESENTED BY GENERAL FORMULA I BELOW: (CF DRAWING IN BOPI) THESE DERIVATIVES ARE OBTAINED BY DEHYDRATION OF 2-HYDROXYMETHALYL-1,4- QUINO CORRESPONDING DIOXIDES, HOT OR IN THE PRESENCE OF DEHYDRATING AGENT.

Copper myxin prepn - from myxin and cupric salt in aq system

Copper myxin (the cupric complex of myxin) is prepd. is reacting myxin (6-methoxy-1-phenazinol 5, 10-dioxide) with a water-soluble cupric salt (pref. cupric acetate monohydrate) in an aqs. system. This avoids risks due to the thermal lability of myxin, and is a rapid process giving high yields of flowable, crystalline copper myxin which does not agglomerate on standing and which has desirable slow release characteristics. The title cpd. has broad-spectrum antimicrobial activity, being partic. active against gram +ve and -ve bacteria, fungi, protozoa and helminths.

Food supplement for livestock

METHYL-QUINOXALINE-1,4-DIOXIDE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND FOOD COMPOSITIONS CONTAINING THEM

Hydroxyquinoxalinecarboxylic acids and process for their preparation

(2)-Benzylidene amino guanidino quinoxaline dioxides - are antibacterials and anticoccidials prepd. from an amino guanidine and a (2)-formyl quinoxaline dioxide

Patent FR4837M

Industrial antimicrobial/mildew-proofing agents, algicides and antifouling agents containing n-quinoxalylanilines

Industrial antimicrobial/mildew-proofing agents, algicides and antifouling agents containing N-quinoxalylanilines represented by general formula (1), wherein R1 and R2 independently represent each H, halogeno, CF3, C1-5 alkyl, C1-5 alkoxy or NO2; R3 represents H, halogeno or C1-5 alkyl; R4 represents H, C1-5 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-6 alkylcarbonyl, C1-5 alkylsulfonyl or optionally halogenated C1-5 alkylsulfenyl; X and Y independently represent each NO2, CF3 or halogeno; Z represents H, halogeno, C1-5 alkoxy or optionally halogenated, nitrated or hydroxylated phenoxy; m and n independently represent each 0 or 1 provided that m and n are not 1 at the same time; and j and k independently represent each 0, 1, 2 or 3, provided that j + k is not more than 3.

2,3-disubstd-quinoxaline-1,4-dioxides - bactericides and amoebicides

Title cpds. are of formula (I): (where R1 is Ph opt. substd. by 1-7C alkyl, 1-7C O alkyl, hal, or CF3; R2 is CONR3R4 and R3 and R4 = H or 1-7C alkyl or R3+R4 = 1-7C alkylene opt. contg. an O, S or N atom). (I) is prepd. by e.g. condensing benzofuroxan with R5R7C=CHR6 where R5 is a labile (carbonium ion generating) residue and R6 and R7 = R1 and R2.

Pseudothymine compsns - as growth promoters in animal feedstuffs or additives

(1) Animal feedstuffs contain 10-500 ppm, pref. 50-200 ppm, pseudothymin (2,4-dioxo-6-methyl-1,2,3,4-tetrahydro-pyrimidine) (I) in addition to other conventional ingredients. (2) additives for animal feedstuffs contain 0.1-10%, pref. 0.5-2% (I). (I) are growth promoting agents probably acting by inhibiting monoaminooxidase. LD50 (p.o. rats) is >12 g/kg. Growth trials on rats were made using (I) and a control and compared against results obtained using aureomycin. The comparison was favourable.

Derivatives of 1, 2, 3, 4-tetrahydrophenazine-5, 10-dioxides and processes for their preparation and use

1,2,3,4-Tetrahydrophenazine-5,10-dioxide derivatives and processes for their preparation and use.

Food composition for animals and its preparation process

Patent FR2256758B1

NEW SULFONYLHYDRAZONES 1,4-DIOXO- AND 4-OXOQUINOXALINE-2-CARBOXALDEHYDE AND THEIR APPLICATION AS ANTIBACTERIAL AGENTS

L'invention concerne certaines nouvelles sulfonylhydrazones de 1,4-dioxgnoXaline-2-carboxaldéhyde ou de 4-oxoquinoxaline-2-carboxaldéhyde et certains de leurs dérivés. Elle concerne également des compositions destinées à l'alimentation des animaux, additionnées de ces composés. Les composés de l'invention ont la propriété d'activer la croissance des animaux et d'améliorer le rendement d'assimilation des aliments. The invention relates to certain novel 1,4-dioxgnoXaline-2-carboxaldehyde or 4-oxoquinoxaline-2-carboxaldehyde sulfonylhydrazones and certain derivatives thereof. It also relates to compositions intended for animal feed, with the addition of these compounds. The compounds of the invention have the property of activating the growth of animals and of improving the yield of food assimilation.

Patent FR2182957B1

Patent FR2025909B1

Patent FR2205325A1

Method for inhibiting tumor cells with new derivatives of 3-trifluoromethylquinoxaline 1,4-dioxide

FIELD: chemistry. SUBSTANCE: invention relates to new derivatives of 3-trifluoromethylquinoxaline 1,4-dioxide containing a diamine residue in the benzene moiety of the quinoxaline ring as well as its pharmacologically acceptable salts, hydrates, corresponding to the formula: EFFECT: new derivatives of 3-trifluoromethylquinoxaline 1,4-dioxide capable of inhibiting the division of tumor cells. 9 cl, 2 tbl, 50 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 746 395 C1 (51) МПК C07D 241/52 (2006.01) A61K 31/498 (2006.01) A61P 35/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 241/52 (2021.02); A61K 31/498 (2021.02); A61P 35/00 (2021.02) (21)(22) Заявка: 2020124152, 21.07.2020 (24) Дата начала отсчета срока действия патента: Дата регистрации: Приоритет(ы): (22) Дата подачи заявки: 21.07.2020 (45) Опубликовано: 13.04.2021 Бюл. № 11 (54) СПОСОБ ИНГИБИРОВАНИЯ ОПУХОЛЕВЫХ КЛЕТОК НОВЫМИ ПРОИЗВОДНЫМИ 3ТРИФТОРМЕТИЛХИНОКСАЛИН 1,4-ДИОКСИДА (57) Реферат: Изобретение относится к новым производным 3-трифторметилхиноксалин 1,4-диоксида, содержащим остаток диамина в бензольном фрагменте хиноксалинового цикла, а также его . Технический фармакологически приемлемые соли, гидраты, соответствующим формуле: результат: получены новые производные 3трифторметилхиноксалин 1,4-диоксида, способные ингибировать деление опухолевых клеток. 2 н. и 7 з.п. ф-лы, 2 табл., 50 пр. R U 2 7 4 6 3 9 5 (56) Список документов, цитированных в отчете о поиске: Mery Santivañez-Veliz et al., Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis, Bioorganic & Medicinal Chemistry Letters, 26, 2188-2193, 2016. Silvia Pérez-Silanes et al., Synthesis and biological evaluation of quinoxaline di-N-oxide (см. прод.) (56) (продолжение): derivatives with in vitro trypanocidal activity, Bioorganic & Medicinal Chemistry Letters, 26, 903-906, 2016. CN 110551072 A, 10. ...

Patent FR2220524A1

Patent FR2228440B3

Patent FR2255908B1

Patent FR2377388B1

Manufacture of quinoxaline derivatives

ALKYLSULFONYLMETHYL AND ALKYLSULFINYLMETHYLQUINOXALINE-1,4-DIOXIDES USEFUL AS GROWTH PROMOTERS

Process for the preparation of phenazine derivatives

Patent FR2182957A1

Fungicidal composition for agricultural use

Patent FR2311546B1

Process for the preparation of 2-methylene- quinoxaline-1,4-dioxide derivatives

ABSTRACT The invention relates to a process for the prapara-ion of 2-methylene-1,4-dioxide derivatives of the general formula /I/ wherein A represents a hydroxyl or an amino group, or a group of the general formula -NH-COOR1, wherein R1 denotes a C1-4 alkyl group; or a group of the general formula -NH-CX-NH2, wherein X stands for oxygen or sulfur; or a group of the formula -NH-C/=NH/-NH2; or a group of the general formula -NH-R2, wherein R2 represents C1-6 alkyl, ohenyl, benzyl, hydroxyl or hydroxy-/C2-4 alkyl/; or a group of the general formula -NH-CO-R3, wherein R3 stands for a C1-20 alkyl group, a phenyl group optionally substituted by one, tno or three identical or different substituent/s/ selected from the group consisting of hydroxyl, amino, nitro, C1-4 alkyl, C1-4 alkoxy or halogen; a piperidyl, a pyridyl, a furyl, a nitro-furyl, a pyrazinyl, a pyrimidyl, a naphthyl, a hydroxy-naphthyl, a phenylalkyl, an 1,2,4-triazinyl, an .alpha.,.alpha.--diphenyl-.alpha.-hydroxymethyl, a cyanomethyl, a halomethyl or a hydroxymethyl group, characterized by dehydrating a compound of the general formula /II/ wherein A has the same meanings as above. The compounds of the general formula /I/ possessing bactericidal and weight-gain increasing properties can be obtained in a high purity with an excellent yield by the process according to the invention.

2-alkoxycarbonyl-hydrazonomethyl-quinoxaline 1,4-dioxides - obtd. by treating hydrazonomethyl-quinoxaline 1,4-dioxides with carbonyl halides, then with alcohols

Quinoxaline dioxides of formula (I): (where R is H, alkyl, alkoxy, CF3 or ahlo; R1 is alkyl or alkoxyethyl) are prepd. by reaction of carbonyl halides with hydrazones of formula (II): then treating the product with an alcohol of formula: R1OH. Process is specif. for 2-methoxy-carbonyl-hydrazonomethyl-quinoxaline 1,4-dioxide and (I) are urinary antiseptics.