Способ получения бензимидазолов

BIOCIDE N-THIOCYANATOMETHOXI-AZAHETEROCYCLEN

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 ...

1-(arylsulfonyl)-4-(piperazin-1-yl)-1h-benzimidazoles as 5-hydroxytryptamine-6 ligands

1-(arylsulfonyl)-4-(piperazin-1-yl)-1h-benzimidazoles as 5-hydroxytryptamine-6 ligands.

2 - Aminobenzimidazoles substituted.

Aminoalkoxyphenyl derivatives process of preparation and compositions containing the same

1-(arylsulfonyl)-4-(piperazin-1-yl)-1h-benzimidazoles as 5-hydroxytryptamine-6 ligands.

1-(arylsulfonyl)-4-(piperazin-1-yl)-1h-benzimidazoles as 5-hydroxytryptamine-6 ligands.

HETERO-CYCLIC CONNECTIONS

4-CHLOR-3-SULFAMOYL-BENZOESAEURE-HYDRAZIDE, PROCEDURE FOR THEIR PRODUCTION, THESE CONNECTIONS ABSTENTIONS of DRUG PREPARATIONS AND USE of the NEW CONNECTIONS TO the PRODUCTION OF DIURETI AND SALT-WITHDRAWING EFFECT DRUG PREPARATIONS.

Procedure for the production of new Benzimidazol derivatives and their pharmaceutical compatible not-toxic salts

SULFONAMIDE WITH ELASTASE INHIBIERENDER EFFECT

Leukotriene synthesis inhibitors

Provided are specific leukotriene synthesis inhibitor compounds and pharmaceutical compositions comprising the compounds and methods of using the compounds and the pharmaceutical compositions in treating, for example, inflammatory diseases or conditions.

Modulators of the integrated stress pathway

Provided herein are compounds of formula (I), compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions. (Formula I).

1-benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives

ALKYLAMINOALKOXYPHENYL DERIVATIVES, PROCESS OF PREPARATION AND COMPOSITIONS CONTAINING THE SAME

QUINOXALINE-DI-N-OXIDES

BRUTON'S TYROSINE KINASE INHIBITORS

Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):

POROUS METAL ORGANIC FRAMEWORK BASED ON PYRROLES AND PYRIDINONES

The present invention relates to a process for preparing a porous metal organic framework containing at least one organic compound coordinated to at least one metal ion, which comprises the step of oxidation of at least one anode containing metal corresponding to the at least one metal ion in a reaction medium in the presence of the at least one organic compound, where the at least one organic compound is a monocyclic, bicyclic or polycyclic ring system which is derived at least from one of the heterocycles selected from the group consisting of pyrrole, alpha-pyridone and gamma-pyridone and has at least two ring nitrogens, where the ring system is unsubstituted or has one or more substituents selected independently from the group consisting of halogen, C1-6-alkyl, phenyl, NH2, NH(C1-6-alkyl), N(C1-6-alkyl)2, OH, Ophenyl and OC1-6-alkyl, where the substituents C1-6-alkyl and phenyl are unsubstituted or have one or more substituents selected independently from the group consisting of halogen, NH2, NH(C1-6-alkyl), N(C1-6-alkyl)2, OH, Ophenyl and OC1-6-alkyl.

Lichtempfindliches Material für photomechanische Reproduktion

Verfahren zur Herstellung von Benzimidazol-Derivaten

Insekticides und acaricides Mittel

Verfahren zur Herstellung von Benzimidazol-N-Oxyden

VERFAHREN ZUR HERSTELLUNG VON 2-CYANOBENZIMIDAZOLEN.

Verfahren zur Herstellung von Salzen von Benzimidazolen

Procédé de préparation de dérivés de la quinoxaline

Verfahren zur Herstellung von Benzimidazolen

Verfahren zur Herstellung von Benzimidazolen

Verfahren zur Herstellung von Benzimidazolen

Mite ovicidal and fungicidal compsns

Process for the preparation of novel 1-sulphonyl- benzimidazoles

1-(АРИЛСУЛЬФОНИЛ)-4-(ПИПЕРАЗИН-1-ИЛ)-1H-БЕНЗИМИДАЗОЛЫ КАК ЛИГАНДЫ 5-ГИДРОКСИТРИПТАМИНА-6

Изобретение касается 1-(арилсульфонил)-4-(пиперазин-1-ил)-1Н-бензимидазолов формулы I: (I) или их таутомера, стреоизомера или фармацевтически приемлемой соли, где значения переменных являются такими, как определено в данном документе, композиций, которые содержат соединения, и способов получения и использования соединений.

1-(АРИЛСУЛЬФОНИЛ)-4-(ПИПЕРАЗИН-1-ИЛ)-1H-БЕНЗИМИДАЗОЛЫ В КАЧЕСТВЕ ЛИГАНДОВ 5-ГИДРОКСИТРИПТАМИНА-6

Изобретение касается 1-(арилсульфонил)-4-(пиперазин-1-ил)-1Н-бензимидазолов формулы I или их таутомера, стереоизомера или фармацевтически приемлемой соли, где значения переменных являются такими, как определено в данном документе, композиций, которые содержат соединения, и способов получения и применения соединений.

Trichlorométhylthiobenzotriazoles

2-4-thiazolyl benzimidazole derivs anthelmintics

(A) Cpds. of general formula (I) R = (1-10C) Oalkyl, Ph, or p-F.C6H4- (B) Acid addn. salts of I. Anthelmintics. Dose 5-125 mg/kg. 2-(3-thiazolin-(2-acetonyl)-4-yl)-5(6)-iso-propoxycarbonylaminobe- nzimidazole (0.1 mol) was heated 1 h. at 180 deg., cooled to 25 deg., dissolved in EtOH at reflux, and cooled 18 h at 0 deg., giving I, m.p. 240-2 deg.

1-(ARYLSULFONYL)-4-(PIPERAZIN-1-YL)-1H-BENZIMIDAZOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS

TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF

Substituted benziomidozole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benziomidazole compounds, as well as pharmaceutical preparations therefore, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

COMPOUNDS AS CRTH2 AND/OR PGD2 RECEPTORS MODULATORS AND THEIR USE FOR TREATING ASTHMA AND ALLERGIC INFLAMMATION

The present invention is directed to compounds, compositions and methods useful for treating inflammatory and immune-related diseases and conditions. The compounds are modulators of prostaglandin D2 (PGD2) receptors including CRTH2 and DP receptors. The subject compounds are carboxylic acid derivatives of formulae (II) and (III): Formula (II), (III), wherein, X represents a divalent linkage selected from -O-, -S(O)k-., -CRaRb-, -C(O)-, -NR8- and -C(NR9)- Y represents a divalent linkage selected from a single bond, -S(O)kNR10-, -C(O)NR10-, (C1-C4)alkylene, hetero(C2-C4)alkyIene, -N(R11)C(O)NR10- -N(R11)S(O)kNR10-, -N(R11)CO2-, -NR11-, -O- and -S(O)k-. Z represents -CO2R12, -C(O)NR12R13 or heteroaryl. L represents a divalent linkage selected from a single bond, (C1-C6)alkylene, (C2-C6)alkenylene, (C2-C6)alkynylene and (C2-C4)heteroalkylene.

BENZOARYLUREIDO COMPOUNDS, AND COMPOSITION FOR PREVENTION OR TREATMENT OF NEURODEGENERATIVE BRAIN DISEASE CONTAINING THE SAME

Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.

СПОСОБ ПОЛУЧЕНИЯ АМИНОФЕНОКСИПРОИЗВОДНЫХ

FIELD: medicine. SUBSTANCE: desired products have formula I where B, Cy, A, R 3 and R 4 have appropriate values. 4-alkoxyphenyl derivative having formula II where B, Cy, A and X are as mentioned above is used as reagent 1. Amine of HNR 3 R 4, formula where R 3 , R 4 have appropriate values is used as reagent 2. Desired product is isolated in free state or as salt, if desired said salt may be converted into base, and if it is desired base is converted into salt. Structural formula of I and II are as follows: 6995$ 0с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) 307/38//А 61 К 31/34, 31/38, 31/40 ВИ” 2 032 669 ' (51) МПК 13) Сл С 070 209/10, 307/82, 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 4830121/04, 15.06.1990 (30) Приоритет: 07.08.1987 Ш$ 082554 (46) Дата публикации: 10.04.1995 (56) Ссылки: Патент США М 4117128, кл. С 070 307/82, опублик. 1978.Патент Франции М 2341578, кл. С 070 471/04, опублик.1977... Мед. Спет. \. 1970, 13(3), с.359.Срит. ТВег, М, ТЭ ТР, Г (5), с.369.)3п9. Спет., 1977, М, 59(283), с.3-23.Ныегосусе$., 1984, М, 2265), с.1235.Ечг. у. Мед. Спет. Твег., 1977, М, 12(5), с.483.Патент Франции М 2400515, кл. С 070 307/68, опублик.1979 Патент США М 4220645, кл. С 070 41312, опублик.1980.Сваг!ег КВ. "Вгихе|ез Меа!са!", 1969, М 9, с.543...А.М.А., 1982, с.247, с.1911. (71) Заявитель: Санофи (ЕК) (72) Изобретатель: Жан Гюбэн[ВЕ], Пьер Шатлэн[ВЕ], Анри Иньон[ВЕ], Жан Люкшетти[ВЕ], Жан-Мари Маокс[ ВЕ], Жан-Ноэль Валла[ЕК] (73) Патентообладатель: Санофи (ЕК) (54) СПОСОБ ПОЛУЧЕНИЯ АМИНОФЕНОКСИПРОИЗВОДНЫХ (57) Реферат: Использование: в медицине в качестве средства, проявляющего ингибигующую активность в отношении транспортировки кальция, а также гипотензивную активность. Сущность изобретения: продукт - аминофеноксипроизводные ф-лы 1, где В, Су, А, Кзи К имеют соответствующие значения, или их солей. Соединения ф-лы | в дозе 5,89 - 0,12 проявляют анти - Альфа и Бэта эффекты 50% и более. Реагент 1: 4 - ...

4-CHLORO-3-SULFAMOYLBENZOIC ACID HYDRAZIDES SHOWING SALIDIURETIC AND DIURETIC ACTIVITIES

METHOD OF SYNTHESIS OF AMINOALKOXYPHENYL-DERIVATIVES OR THEIR PHARMACEUTICALLY ACCEPTIBLE SALTS

Использование: в качестве антиадре- нэргических средств в медицине. Сущность изобретени : продукт аминоалкоксифе- нильные производные общей формулы Су- B-fcC°C-C-C C-0-A-NRiR2, где В - S- или SOa-rpynna; A - линейный или разветвленный алкиленовый радикал, содержащий 2-5 атомов углерода; RI - Ci-Ci-алкил или AlkАг , где Alk - одинарна  св зь или Ci-Cs-ал- килен; Аг-- пиридил, фенил, 2,3-метиленди- оксифенил или фенил, замещенный одним или несколькими заместител ми, которые могут быть как одинаковыми, так и различными , выбранными из атомов галогена, низших алкильных или алкоксильных групп; R2 - водород или Ст-С алкил, или Rt и R2 вместе образуют Сз-Се-алкилен; Су- инодо- линин-3-ил, индолил, бёнзофурил, бензоти- енил, хинолинил, пирроло (1,2-а) пиридил, 4,5-дигидрофуранил или фенил, при условии , что когда Су - бензо(Ь) фурил или бензо (Ь) тиенил, то В  вл етс  502-гру.ппой, а RI - Afk-Ar или же фармацевтически приемлемые соли. Реагент 1: 4-оксифенил формулы Су-В-СбН4ОН. Реагент 2: X-A-NRiRa, где Х- галоген, С|-С4-алкилсульфонилокси, или С1 С4-арилсульфонилоксигруппа. Услови  реакции:- в присутствии щелочного агента в среде пол рного растворител  при температуре от комнатной до температуры кипени  реакционной смеси. 3 табл. i .- , о ел G

ALKYLAMINALKOXYPHENYL DERIVATIVES, PROCEDURES FOR THE USE AND IT CONTAINING COMPOSITIONS.

Procedure for the production of new Imidazoliumsalzen

Procedure for the production of new Benzimidazolderivaten and their salts

POROUS METAL-ORGANIC STAND MATERIAL BASED ON PYRROLEN AND PYRIDINONEN

ARALKYLAMINALKOXYPHENYL DERIVATIVES, PROCEDURES FOR THE PRODUCTION AND IT CONTAINING COMPOSITIONS.

1-(METHYL SULPHONYL) BENZIMIDAZOLE

ARALKYLAMINOALKOXYPHENYL DERIVATIVES, PROCESS OF PREPARATION AND COMPOSITIONS CONTAINING THE SAME

Compounds as CRTH2 and/or PGD2 receptors modulators and their use for treating asthma and allergic inflammation

1-(ARYLSULFONYL)-4-(PIPERAZIN-1-YL)-1H-BENZIMIDAZOLES AS δ-HYDROXYTRYPTAMINE-6 LIGANDS

2-МЕТИЛ-1-(ФЕНИЛСУЛЬФОНИЛ)-4-ПИПЕРАЗИН-1-ИЛ-1Н-БЕНЗИМИДАЗОЛ, ЕГО ПРИМЕНЕНИЕ И СОДЕРЖАЩАЯ ЕГО КОМПОЗИЦИЯ

The invention relates to 2-methyl-1-(phenylsulfonyl)-4-(piperazin)-1-yl-1H-benzimidazole compounds or a pharmaceutically acceptable salt, pharmaceutical composition and use thereof as a medicament and for modulation of 5-HTactivity.

1- (arylsulfonyl) -4- (pi perazin-i -yl) -ih-benz imidazoles as d-hydroxytryptamine- 6 ligands

Method of preparation of benzimidazoles

Sulfénylindolinones

Formulations and processes for the conservation of citrus fruits, fruits and agricultural produce

BENZIMIDAZOLES SUBSTITUTE FOR the FIGHT AGAINST the PROTOZOA IN the ANIMAL

Aralkylaminoalkoxyphenyl derivatives, process of preparation and compositions containing the same

PROCEDE POUR LA PREPARATION DES BENZIMIDAZOLES

1-Benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives

The present invention relates to 1-benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives of the formula (I) wherein R1 is halogen, (C1-C7)alkoxy, w-methoxyl(C2-C7)alkoxy or (C3-C7)cycloalkoxy; R2 is hydrogen; R3 is R4, (C1-C8)alkylene substituted by R4, (C1-C8)alkylene substituted by (C1-C4)alkoxy, indan, adamantane, cyclohexane substituted by di(C1-C7)alkylamino, hydrocarbon, or (C1-C4)alkoxy(C1-C4)alkoxy; R4 is -NR18R17 group, unsubstituted (C3-C7)cycloalkyl or singly substituted by (C1-C4)alkyl or (C1-C4)alkoxy; unsubstituted phenyl or singly substituted by halogen atom, (C2-C7)alkyl or (C1-C7)alkoxy; pyrrole group; tetrahydropyrane-4-group; piperidine-4- group substituted by R18 at the first position; piperidine-4-group substituted by one (C1-C7)alkyl or one benzyl; or morpholine group; R5 is hydrogen or group -OR7; R6 is (C1-C7)alkyl, nitro group, carboxyl group; guanidine substituted by two (C2-C7)alkyl at the third position; -OR7 group; benzyloxycarbonyl, -CONR19-R20 group ...

1-(ARYLSULFONYL)-4-(PIPERAZIN-1-YL)-1H-BENZIMIDAZOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS

The invention relates to 1-(arylsulfonyl)-4-(piperazin-1-yl)-1H-benzimidazole compounds of the Formula I: or a tautomer, stereoisomer, or pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.

SULFENAMIDE-CONTAINING LIPOXYGENASE INHIBITOR

ПРОИЗВОДНЫЕ 1-БЕНЗОЛСУЛЬФОНИЛ-1,3-ДИГИДРО-2Н-БЕНЗИМИДАЗОЛ-2-ОНА, СПОСОБ ИХ ПОЛУЧЕНИЯ, СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention describes new derivatives of 1-benzene-sulfonyl-1,3-dihydro-2H-benzimidazole-2-one of the formula (I) where values R 1 -R 3 ,R 5 and R 6 , m are given in point 1 of the claim and pharmaceutical composition based on their. Compounds of the formula (I) show affinity to vasopressin and oxytocin receptors and can be used for treatment of patients with sicknesses of central and peripheral nervous systems, cardiovascular system, renal and gastric spheres and in sexual behavior disorders in human and animals. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 5 cl, 4 tbl, 116 ex ДУС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ” 2135 477‘ 13) СЛ С 07 О 235/26, А 61 К 31/415 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 94027577/04, 29.07.1994 (30) Приоритет: 30.07.1993 ЕК 93 09403 (46) Дата публикации: 27.08.1999 (56) Ссылки: ЗЦ 2027709, 1995. ЕР 0469984 А, 1992. ЕР 0469984 А2, 1992. ЕР 0382185 АЗ, 1990. КУ 2057126 СЛ, 27.03.96. (98) Адрес для переписки: 129010, Москва, ул.Б.Спасская, д.25, стр.3, ООО "Союзпатент" (71) Заявитель: Санофи (ЕК) (72) Изобретатель: Ален Ди Мальта (ЕКВ), Жорж Гарсиа (ЕК), Даниель Меттефе (ЕК), Дино Низато (1Т), Ришар Ру (ЕК), Клодин Серрадей-Легаль (ЕК) (73) Патентообладатель: Санофи (ЕК) (54) ПРОИЗВОДНЫЕ 1-БЕНЗОЛСУЛЬФОНИЛ-1,3-ДИГИДРО-2Н-БЕНЗИМИДАЗОЛ-2-ОНА, СПОСОБ ИХ ПОЛУЧЕНИЯ, СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ (57) Реферат: Описываются новые — производные 1-бензолсульфонил-1 ,3-дигидро- 2Н-бензимидазол-2-она формулы (1, где значения К 1-Кз, К5, Кб и т указаны в п.1 формулы, их способ получения и фармацевтическая композиция на их основе. Соединения формулы (1) обладают сродством к рецепторам вазопрессина и оцитоцина. Они пригодны для лечения заболеваний центральной и периферической нервной системы, — сердечно-сосудистой — системы, почечной и желудочной сфер и при расстройствах сексуального поведения ...

AMINOBENZIMIDAZOLE

HETEROAROMATIC ETHER HERBICIDES

Benzimidazoles and process for their preparation

Novel benzimidazoles of the formula (wherein Ph is 1,2-phenylene which may be alkyl, etherified hydroxy, alkylenedioxy, halogen, CF3, NO2, NH2, dialkylamino, alkanoyl, benzoyl, toluoyl, pyridoyl or sulphamoyl substituted; R is an aliphatic, araliphatic, aryl or heterocyclic aryl group; A is an alkylene group and Am is a primary, secondary or tertiary amino group), N-oxides thereof, and acid-addition salts and quaternary ammonium derivatives of these compounds are prepared (1) from the free N-hydroxy-benzimidazoles and reactive esters of the compounds Am-A-OH; (2) from the N-(O-A-X) benzimidazoles in which X is a reactively esterified hydroxy group and the compounds H-Am; and (3) by reduction with a light metal hydride of the N-(O-Ac-Am) benzimidazoles in which Ac is alkanoylene. Products may be interconverted, e.g. substituents may be introduced into or removed from an amino group, and amino groups and their N-oxides may be interconverted. 1 - Hydoxy - 2 - R - benzimidazole ...

1-AMINO-OR SUBSTITUTED AMINO BENZIMIDAZOLES

... 1398051 Benzimidazole derivative compositions MERCK & CO INC 2 Jan 1973 [7 Jan 1972] 249/73 Headings A5B and A5E [Also in Divisions A2 and. C2] Pharmaceutical and fungicidal compositions comprise a compound of formula (I): wherein R 2 is aryl, orthohaloaryl, a heteroaromatic radical containing from 1 to 3 hetero atoms selected from nitrogen, oxygen and sul- X # phur, or -NHCR 1 wherein R 1 is C 1-6 alkyl, C 1-6 alkoxy, C 4-8 cycloalkyl, C 4-8 cycloalkyloxy, aryl, haloaryl, aryloxy, amino, C 1-6 alkylamino, di (C 1-6 alkyl) amino, anilino, pyrrolidino, piperidino, morpholino, piperazino or a heteroaromatic radical containing from 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur, X is oxygen or sulphur, R 5 and R 6 are H, halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio, phenyl, halophenyl, phenoxy, phenylthio, amino, C 1-6 alkylamino, di (C 1-6 X # alkyl) amino or -NHCR 1 wherein R 1 and X are as defined above, provided that when R 5 and R 6 are other than halogen at least ...

Procedure for the production of new Benzimidazolderivate and their salts

HETEROAROMATIC ETHER AS HERBICIDES.

BIOCIDE N-THIOCYANATOMETHOXY-AZAHETEROCYCLEN

Photo-sensitive material for photo-mechanical reproduction and procedure for the production of printing forms with this material

Procedure for the production of new Benzimidazolderivaten and their salts

PROCEDURE FOR THE PRODUCTION OF NEW BENZIMIDAZOLDERIVATEN

PROCEDURE FOR THE PRODUCTION OF NEW BENZIMIDAZOLDERIVATEN

SUBSTITUTED 1-SULFONYLBENZIMIDAZOLES

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R1, R2, R2', R3, R3', R4, R4', R5, R5', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

CYSTEINE PROTEASE AND SERINE PROTEASE INHIBITORS

The present invention is directed to irreversible inhibitors of serine and cysteine proteases which most preferably contain a 1-oxytriazole or 1oxyimidazole functionality. Methods for the use of the protease inhibitors are also described.

SULFONAMIDE DERIVATIVES

Sulfonamide derivatives of the formula (I) (I) wherein R1 is, inter alia, alkyl, alkoxy, hydroxy, keto, nitro, halogen, trihalomethyl, cyano, amidino and -COOR7 (in which R7 is hydrogen or alkyl), n is an integer from 0 to 5; is a carbocyclic ring or heterocyclic ring; is in which R2 and R3 each is hydrogen, alkyl, alkoxy, halogen, trihalomethyl or phenyl, or R2 and R3, taken together, represent alkylidene, or is in which R2 and R3, taken together with the carbon atom to which they are attached represent cycloalkyl; R4 is alkyl or alkoxy or two of R4, attached to the benzene nucleus at ortho positions relative to each other, taken together, represent alkylene; m is an integer from 0 to 4; and

BENZIMIDAZOLE COMPOSITIONS USED AS INSECTICIDES AND ACARICIDES

Quinoxaline-di-n-oxides

2-METHYL-1-(PHENYLSULFONYL)-4-(PIPERAZIN-1-YL)-1H-BENZIMIDAZOLE AS 5-HYDROXYTRYPTAMINE-6 LIGAND

ANALOGUES FOR THE TREATMENT OR PREVENTION OF FLAVIVIRUS INFECTIONS

Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R 1 , R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 ', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Bruton's tyrosine kinase inhibitors

Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I): ...

ПРОИЗВОДНЫЕ 1-БЕНЗОЛСУЛЬФОНИЛ-1,3-ДИГИДРО-2Н-БЕНЗИМИДАЗОЛ-2-ОНА, СПОСОБ ИХ ПОЛУЧЕНИЯ, СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Изобретение относится к производным 1-бензолсульфонил-1,3-дигидро-2Н-бензимидазол-2-она формулы Iих получению и содержащим их фармацевтическим композициям. Эти соединения обладают сродством к рецепторам вазопрессина и оцитоцина. Изобретение относится также к способу получения названных соединений к фармацевтической композиции на их основе.

BENZIMIDAZOLES AND A PROCESS FOR THEIR PREPARATION

... 1,267,999. Benzimidazoles. ELI LILLY & CO. 2 May, 1969 [3 May, 1968], No. 57611/70. Divided out of 1,267,998. Heading C2C. Compounds of formulµ wherein R is R11OCO or R111R1111NCS-, in which R1 is hydrogen, fluorine, chlorine, bromine, C 1-5 alkoxy, C 1-5 alkyl or nitro, R11 is C 1-5 alkyl or haloalkyl, C 2-5 alkonyl or haloalkenyl or C 2-5 alkynyl, R111 and R1111 are hydrogen, C 1-5 alkyl or phenyl or in combination a pentamethylene or tetramethylene chain, and n is 1 to 3, Y is hydrogen or fluorine, Z is hydrogen, fluorine, chlorine, -CF 3 or -CF 2 CF 3 , and halo is fluorine, chlorine or bromine, are prepared by reaction of a corresponding N-unsubstituted benzimidazole with an alkali metal alkoxide to form an alkali metal salt, and reacting this with a compound of formula R-X wherein X is a halogen atom. The compounds of the invention have insecticidal and acaricidal activity. Reference has been directed by the Comptroller ...

BENZIMIDAZOLES AND A PROCESS FOR THEIR PREPARATION

... 1,268,000. Benzimidazoles. ELI LILLY & CO. 2 May, 1969 [3 May, 1968], No. 57613/70. Divided out of 1,267,998. Heading C2C. Compounds of formulae wherein Y is hydrogen or fluorine and Z is hydrogen, fluorine, chlorine, -CF 3 or -CF 2 CF 3 , are prepared by cyclization of a corresponding o - phenylene diamine by heating with a compound of formula Z-CF 2 -COOH. The products have insecticidal and acaricidal activity. 3 - Nitro - 5 - trifluoromethyl - o - phenylene diamine is prepared by reaction of 2,6-dinitro- 4 - trifluoromethyl - 1 - chlorobenzene with ammonium hydroxide to give 2,6-dinitro-4-trifluoromethylaniline, followed by reaction of this with ammonium polysulphide. Reference has been directed by the Comptroller to Specifications 1,087,561 and 1,159,789.

2-SUBSTITUTED POLYHALOBENZIMIDAZOLES

... 1286603 Benzimidazoles MERCK & CO Inc 21 Sept 1970 [26 Sept 1969] 44896/70 Heading C2C The invention comprises compounds of formula and their salts with alkali or alkaline earth metals, and with pharmaceutically acceptable amines and acids, wherein R is CN, CSNH 2 , CSNH alkyl, CSN(alkyl) 2 , S-alkyl, SO 2 alkyl or 2-thiazolin-2-yl ; R 1 , R 2 , R 3 , R 4 are each F, Cl, Br or I, or one of them may be H; and R 5 is H, alkyl, alkoxyalkyl, C 2-6 alkenyl, carboxyalkyl, carboalkoxyalkyl, C 1-6 alkanoyl, aminoalkyl, alkylaminoalkyl or dialkylaminoalkyl, and when R is CN, R 5 may also be OH, alkoxy, carboxyalkoxy, carboalkoxyalkoxy, sulphoalkoxy or amino-C 2-6 -alkoxy (possibly N-alkyl or N,N- dialkyl substituted). In examples, these compounds are prepared by (1) (R=CN : Ia) dehydrating with SOCl 2 the tri- or tetra-halo- 2-formylbenzimidazole oxime, reacting the tri- or terra-halo-2-chlorobenzimidazole with NaCN, or reacting the tri- or tetra-halo-2-trichloromethylbenimidozole (II) with NH 3 ...

VERFAHREN ZUR HERSTELLUNG VON NEUEN BENZIMIDAZOLDERIVATEN

Procedure for the production of new Benzimidazolderivaten and their salts

Milbenovizid and fungicide

Transcription factor modulating compounds and methods of use thereof

Substituted benziomidozole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benziomidazole compounds, as well as pharmaceutical preparations therefore, in, ., reducing antibiotic resistance and inhibiting biofilms.

Transcription factor modulating compounds and methods of use thereof

SULFONYLDIAZOLES AND N-(FLUOROSULFONYL)AZOLES, AND METHODS OF MAKING THE SAME

The present disclosure provides methods for producing N-(fluorosulfonyl)azoles, sulfonyldiazoles, or related derivatives thereof; and the related products including N- (fluorosulfonyl)azoles, sulfonyldiazoles, and related derivatives thereof. For example, an N- (fluorosulfonyl)azole is obtained by reaction of sulfuryl fluoride with an azoles, an azole anion compound, a silylazole, or a combination thereof. Symmetric and asymmetric sulfonyldiazoles are obtained by further reaction of such an N-(fluorosulfonyl)azole with azoles, azole anion compounds, or silylazoles. A sulfonyldiazole can be also produced by reacting sulfuryl fluoride with an azole, a silylazole, or a combination thereof in one pot.

ARALKYLAMINOALKOXYPHENYL DERIVATIVES, PROCESS OF PREPARATION AND COMPOSITIONS CONTAINING THE SAME

Disclosed are new aminoalkoxyphenyl derivatives of formula: (1) in which B is -S-, -SO- or -SO2; R1 and R2 are hydrogen, methyl, ethyl or halogen; A is alkylene 2-hydroxypropylene; R3 is hydrogen or alkyl ; R4 is pyridyl, phenyl, 2,3methylenedioxyphenyl or 3,4-methylenedioxyphenyl; Alk is a single bond or an alkylene; Cy represents a group of formula : or or (D) (E) or or (F) (G) (H) in which R is hydrogen, alkyl, cycloalkyl, benzyl or phenyl; R5 and R6 together with the carbon atom to which they are attached forms mono- or di-cyclic carboxylic group; an aromatic 5-membered heterocyclic group or a 6- to 10membered mono- or di-cyclic heterocyclic group; R7 and R8 each are hydrogen, alkyl or phenyl or together represent a 6-membered carbocyclic ring; R9 is O or Si;R10 is O, S or N-R11; R12 and R13, each are hydrogen, alkyl or benzol, with the proviso that Cy does not represent a l-indolizinyl group, as well as their N-oxide derivatives and their pharmaceutically ...

NEW SUBSTITUTED BIPHENYL ANALOGUES AS DUAL INHIBITORS OF AROMATASE AND SULFATASE

The present invention relates to new biphenyl derivatives of formula 3. A compound according to claim 1 , wherein L is a linker selected from —CH2- and —NH—; or any pharmaceutically acceptable salt thereof.4. A compound according to claim 1 , wherein A represents an aromatic bicyclic ring of 9 ring members claim 1 , containing at least two nitrogen atoms as ring member claim 1 , and being optionally substituted by one or more substituents selected from halo; or any pharmaceutically acceptable salt thereof.5. A compound according to claim 1 , wherein A represents an aromatic bicyclic ring of 9 ring members claim 1 , containing from two to four nitrogen atoms as ring member claim 1 , and being optionally substituted by one or more substituents selected from halo claim 1 , the bicyclic ring being the fusion of a ring of 5 ring members and a ring of 6 ring members; or any pharmaceutically acceptable salt thereof.6. A compound according to claim 1 , wherein A represents an aromatic bicyclic ring of 9 ring members claim 1 , containing from two to four nitrogen atoms as ring member claim 1 , and being optionally substituted by one or more substituents selected from halo claim 1 , the bicyclic ring being the fusion of a ring of 5 ring members and a ring of 6 ring members claim 1 , the ring of 5 ring members containing at least 2 nitrogen atoms and being linked to the linker L; or any pharmaceutically acceptable salt thereof.8. A compound according to claim 1 , wherein A represents a unsubstituted ring; or any pharmaceutically acceptable salt thereof.9. A compound according to claim 1 , wherein the B ring contains at least one nitrogen atom as ring member; or any pharmaceutically acceptable salt thereof.10. A compound according to claim 1 , wherein the B ring contains from one or two nitrogen atoms as ring member; or any pharmaceutically acceptable salt thereof.12. A compound according to claim 1 , wherein the C ring contains no nitrogen atom as ring member; or any ...

Nonaqueous Electrolyte and Nonaqueous Secondary Battery

The purpose of the present invention is to provide a nonaqueous electrolyte that contains acetonitrile having an excellent balance between viscosity and the dielectric constant and a fluorine-containing inorganic lithium salt, wherein the generation of complex cations comprising a transition metal and acetonitrile is suppressed, excellent load characteristics are exhibited, and increases in internal resistance upon repeated charge/discharge cycles are suppressed; a further purpose of the present invention is to provide a nonaqueous secondary battery. The present invention relates to a nonaqueous electrolyte which contains: a nonaqueous solvent comprising acetonitrile; a fluorine-containing inorganic lithium salt; and a specific nitrogenous cyclic compound typified by benzotriazole. 2. The non-aqueous electrolyte solution according to claim 1 , wherein the non-aqueous solvent contains acetonitrile in 20 to 100% by volume.3. The non-aqueous electrolyte solution according to claim 1 , wherein Rof the compound represented by the general formula (1) above is an alkyl group having 1 to 4 carbon atoms claim 1 , bis(N claim 1 ,N′-alkyl)aminomethyl group claim 1 , or bis(N claim 1 ,N′-alkyl)aminoethyl group.4. The non-aqueous electrolyte solution according to claim 1 , wherein content of the compound represented by general formula (1) above is 0.01 to 10 parts by mass claim 1 , relative to 100 parts by mass of the non-aqueous electrolyte solution.5. The non-aqueous electrolyte solution according to claim 1 , wherein the fluorine-containing inorganic lithium salt contains LiPF.6. A non-aqueous secondary battery comprising:a positive electrode having a positive electrode active material layer containing at least one transition metal element selected from Ni, Mn, and Co, on one surface or both surfaces of a current collector;a negative electrode having a negative electrode active material layer on one surface or both surfaces of another current collector; and{'claim-ref': {'@ ...

Aryl hydrocarbon receptor activators

Small molecule AhR ligands are disclosed. The ligands can induce the differentiation of Tr1 cells to suppress pathogenic immune responses without inducing nonspecific immune suppression. Methods of treatment of autoimmune diseases using the AhR ligands are also disclosed.

N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides

The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.

METHOD FOR PHOTOCLEAVAGE OF AMIDE BONDS

The present disclosure provides a method for photocleavage of an amide bond, the method has mild reaction conditions and can realize the cleavage of amide bonds by using light. The method comprises the following steps: subjecting 2,4-dinitrofluorobenzene to a reaction with an amino group of a substance represented by structural formula I with an α-amino acid at the end to produce a compound 1 represented by structural formula II; then under light irradiation, subjecting the compound 1 to a cleavage reaction of amide bond; 2. The method for photocleavage of the amide bond according to claim 1 , wherein comprising the following steps: dissolving 2 claim 1 ,4-dinitrofluorobenzene in an organic solvent claim 1 , then dissolving the substance represented by structural formula I with an α-amino acid at the end and NaHCOin water claim 1 , mixing the two in a reaction vessel claim 1 , and stirring and refluxing at 40-100° C. under darkness for 3-10 h.3. The method for photocleavage of the amide bond according to claim 1 , wherein the light irradiation wavelength range is 250-550 nm.4. The method for photocleavage of the amide bond according to claim 1 , wherein the light irradiation time is 0.1 second to 6 h.5. The method for photocleavage of the amide bond according to claim 2 , wherein the organic solvent is an organic solvent capable of partially or completely dissolving the target lysate claim 2 , i.e. compound 1.6. The method for photocleavage of the amide bond according to claim 5 , wherein the organic solvent is one or a combination of dimethyl sulfoxide claim 5 , alcohol claim 5 , ketone claim 5 , nitrile claim 5 , ether claim 5 , and amide.7. The method for photocleavage of the amide bond according to claim 6 , wherein the alcohol is methanol claim 6 , ethanol claim 6 , butanol claim 6 , ethylene glycol claim 6 , n-octanol or isopropanol; the ketone is acetone claim 6 , methyl ethyl ketone claim 6 , methyl isobutyl ketone or cyclohexanone; the nitrile is ...

Transcription factor modulating compounds and methods of use thereof

Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

Transcription factor modulating compounds and methods of use thereof

Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of using substituted benzimidazole compounds, in, e.g., reducing virulence and infectivity, inhibiting biofilms and treating bacterial infections, are also provided.

Actinic ray-sensitive or radiation-sensitive resin composition, actinic ray-sensitive or radiation-sensitive film and pattern forming method using the same

Improved method of preparing lansoprazole

본 발명은 란소프라졸의 개선된 제조방법에 관한 것으로서, 본 발명의 방법에 따르면, 출발물질인 하이드록시메틸피리딘 유도체를 포스핀 화합물과 아조디카복실레이트 화합물의 존재하에서 벤즈이미다졸 유도체와 반응시킨 후, 생성된 화합물을 유기 라디칼 촉매 존재하에서 산화시킴으로써 하기 구조식 (1)의 란소프라졸(2-[3-메틸-4-(2,2,2-트리플루오로에톡시)-2-피리딜]메틸설피닐-1H-벤즈이미다졸)을 고수율로 간편하게 제조할 수 있다. The present invention relates to an improved method for preparing lansoprazole. According to the method of the present invention, after reacting a hydroxymethylpyridine derivative as a starting material with a benzimidazole derivative in the presence of a phosphine compound and an azodicarboxylate compound, Lansoprazole (2- [3-methyl-4- (2,2,2-trifluoroethoxy) -2-pyridyl] methylsulfinyl of the following structural formula (1) by oxidizing the resulting compound in the presence of an organic radical catalyst -1H-benzimidazole) can be conveniently prepared in high yield. (1) (One)

Benzimidazoles compound and application thereof

本发明提供了一类苯并咪唑类化合物及其应用，所述化合物具有通式(I)的结构。该通式化合物由对2‑(3,4,5‑三羟基苯基)‑1H‑苯并咪唑的1位和/或6位进行化合物修饰(即分别引入R 1 和R 2 )而获得。本发明的苯并咪唑类化合物能模拟Bim,在体外和细胞内竞争性结合和拮抗Bcl‑2/Mcl‑1蛋白，从而诱导细胞凋亡，是一类活性很高的凋亡诱导剂和抗肿瘤化合物。

Non-aqueous liquid electrolyte and non-aqueous secondary battery

본 발명은 점도와 비유전율의 밸런스가 우수한 아세토니트릴 및 불소 함유 무기 리튬염을 함유하는 비수계 전해액에 있어서, 전이 금속과 아세토니트릴을 포함하는 착체 양이온의 생성을 억제하고, 우수한 부하 특성을 발휘함과 함께, 충방전 사이클을 반복했을 때의 내부 저항의 증가를 억제할 수 있는 비수계 전해액 및 비수계 이차 전지를 제공하는 것을 목적으로 한다. 본 발명은 아세토니트릴을 포함하는 비수계 용매와, 불소 함유 무기 리튬염과, 벤조트리아졸로 대표되는 특정한 질소 함유 환상 화합물을 함유하는 비수계 전해액 등에 관한 것이다. The present invention suppresses the formation of complex cations containing a transition metal and acetonitrile in a non-aqueous liquid electrolyte containing acetonitrile and a fluorine-containing inorganic lithium salt having excellent balance of viscosity and relative dielectric constant, and exhibits excellent load characteristics And an object of the present invention is to provide a non-aqueous liquid electrolyte and a non-aqueous secondary battery capable of suppressing an increase in internal resistance when the charge / discharge cycle is repeated. The present invention relates to a nonaqueous solvent containing acetonitrile, a fluorine-containing inorganic lithium salt, and a non-aqueous electrolyte containing a specific nitrogen-containing cyclic compound represented by benzotriazole.

Sulfonamide derivatives

본 발명은 하기 화학식 1로 표시되며 엘라스타제에 대한 억제 효능을 갖는 설폰아미드 유도체, 이의 비독성 염, 산 부가염 또는 용매화합물에 관한 것이다. The present invention relates to sulfonamide derivatives, non-toxic salts, acid addition salts or solvates thereof, which are represented by the following formula (1) and have inhibitory efficacy against elastase. [화학식 1] [Formula 1]

Analogues for the treatment or prevention of flavivirus infections

Compounds represented by formula I or pharmaceutically acceptable salts thereof, wherein A, B, B′, X, Y, R 1 , R 2 , R 2 ′, R 3 , R 3 ′, R 4 , R 4 ′, R 5 , R 5 ′, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Analogues for the treatment or prevention of flavivirus infections

Compounds represented by formula I as described herein or pharmaceutically acceptable salts thereof, wherein A, B, B', X, Y, R 1 , R 2 , R 2 ', R 3 , R 3 ', R 4 , R 4 ', R 5 , R 5 ', m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.

Analogues for the treatment or prevention of flavivirus infections

式I表示的化合物或其药学上可接受的盐，其中A、B、B’、X、Y、R 1 、R 2 、R 2 ’、R 3 、R 3 ’、R 4 、R 4 ’、R 5 、R 5 ’、m、n或p如说明书中所定义，其用于治疗黄病毒科病毒感染。

Method of preparing sulfonylbenzimidazoles

Sulphonylbenzimidazoles of the formula I <IMAGE> in which R1, R2 and R3 have the meaning given in Patent Claim 1, are obtained by reaction of a corresponding tautomeric benzimidazole (i.e. a compound I which contains an H atom which can be located on the N atom 3, instead of the SO2R1 group) with a sulphonyl chloride R1SO2Cl. Resulting isomers can be separated. The compounds I are very useful as medicaments for the control of viruses.

Patent FR2181654A1

Patent FR2070090A1

Sulfenylbenzazoles

Sulfenylbenzimidazoles derived from quinoline

Sulfenylindoles

N-sulfonylbenzimidazolone derivatives, their preparation, pharmaceutical compositions containing them.

Sulfenylated derivatives of vinylbenzimidazoles

Trichloromethylthiobenzimidazoles

Antibacterial agents

The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X=NH Y=CO, CS, -C(=N-CN) or X and Y together form an alkene, or C3-C5 cycloalkyl; R1 is -COOH; R2 is an electron withdrawing group; R4 is an optionally substituted aryl. The compounds of formula I are antibacterial agents that are useful for sterilization sanitation, antisepsis, and disinfection.

Heterocyclic Compounds

ANALOGY PROCEDURE FOR THE PREPARATION OF THERAPEUTIC ACTIVE 4-CHLORO-3-SULFAMOYLBENZOIC ACID HYDRAZIDES

1-(Arylsulfonyl)-4-(Piperazin-1-yl)-1H-Benzimidazoles as 5-Hydroxytryptamine-6 Ligands

Acaricidal benzimidazole derivs

Acaricidal benzimidazole derivs. Novel cpds. (I) with acaricidal activity: where X = H, Hal, NO2, CF3, CH3SO2-, C2H5SO2-, CN; n = 1-4; R1 = H, (Ph)3C-, (p-Cl-Ph)3C-, COOR6 (R6 = alkyl, phenyl) when R2 = CHCL2CF2- or (b) R1 = OH, OR3 (R3 = alkyl, 2,4-dinitrophenyl), OCOOR6, O-CO-R5 (R5 = alkyl, alkenyl, phenyl) when R2 = CHCL2CF2-, CF2Cl-, MeO-CF2-, Cl2C=CCl-, CF3 provided that R1 is not = OH when R2 = CF3 or (c) R1 = H, Rhal when R2 = -S-Rhal provided that Rhal is identical for R1, R2 and = CHClFCF2-, CHF2CF2-, CF3CHFCF2-, CH2Cl-CF2-, CH2Br-CF2-, CHCl2-CF2-.

Heterocyclic compounds

Benzimidazoles

Preparation method of N-substituted sulfonamide derivative

本发明公开了一种N-取代磺酰胺衍生物的制备方法，包括：以NBS或NIS作氧化剂，唑类化合物与芳亚磺酸钠在有机溶剂中发生反应，反应完全之后经过后处理得到所述的N-取代磺酰胺衍生物。该制备方法以唑类化合物和芳亚磺酸钠作为底物合成N-取代磺酰胺衍生物，反应原料廉价易得，制备方法简单。

Heterocyclic compounds

Η παρούσα εφεύρεση σχετίζεται με ενώσεις οι οποίες είναι αναστολείς της απακετυλάσης της ιστόνης. Περισσότερο δε ειδικότερα, η παρούσα εφεύρεση σχετίζεται με ετεροκυκλικές ενώσεις και μεθόδους για την παρασκευή αυτών. Αυτές οι ενώσεις μπορεί να είναι χρήσιμες ως φάρμακα για την αγωγή των υπερπλαστικών διαταραχών ως επίσης και άλλων παθήσεων ενέχοντας, σχετιζόμενες σε ή που συσχετίζονται με ένζυμα έχοντα δραστηριότητες της απακετυλάσης της ιστόνης (HDAC). The present invention relates to compounds which are histone deacetylase inhibitors. More particularly, the present invention relates to heterocyclic compounds and methods for their preparation. These compounds may be useful as drugs for the treatment of hyperplastic disorders as well as other diseases involving, associated with or associated with enzymes having histone deacetylase (HDAC) activities.

Heterocyclic compounds

1-SULFONYLBENZIMIDAZOLES SUBSTITUTES

Photosensitive material for photomechanical reproduction

1-(perhaloalkanesulphenyl)-2-(alkoxycarbonyl - fungici

1-(Perhaloalkanesulphenyl)-2-(alkoxycarbonylaminomethyl)-benzimid- azoles; fungicides Cpds. of formula (I): (where R = one or more optional halogen, alkyl, aryl, alkoxy, alkylthio, CN or NO2 groups; R1 = alkyl, alkenyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl or heteroaralkyl, with one or more optional halogen, alkoxy, CN or NO2 substits.; R11 = H or alkyl; R111 = SCH3, -SCH2H5 or -SCH=CH2 opt. having H atoms replaced by halogen; R1111 = alkyl, alkenyl, phenyl, naphthyl, or heteroaryl, with one or more opt. halogen, alkyl, phenyl, alkoxy, alkylthio, CN or NO2 substits.), are fungicides and general pesticides. The cpds. are pref. prepd. by the reaction of an alkyl halide, R111-X with a benzimidazole of formula (II): (substits. being as above).

Aralkylaminoalkoxyphenyl derivatives, process of preparation and compositions containing the same

2-methyl-1-(phenylsulfonyl)-4-(piperazin-1-yl)-1h-benzimidazole as 5-hydroxytryptamine-6 ligand

1-Benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives, their preparation and pharmaceutical compositions containing them

Patent FR2181654B1

Method of 4-chloro-3-sulfamoylbenzoic acid synthesis

The novel compounds according to the invention correspond to the general formula I <IMAGE> in which R represents hydrogen, a trifluoromethyl or carboxyl group, an alkoxycarbonyl group having 2-5 carbon atoms, a cyano, benzoyl or sulphamoyl group or an alkylsulphonyl group having 1-4 carbon atoms, R<1> represents hydrogen, an alkylthio or alkylsulphonyl group each having 1-4 carbon atoms, a straight or branched alkyl group having 1-4 carbon atoms, or a benzylthio, benzylsulphonyl, phenyl, hydroxyl or thiol group and R<2> represents hydrogen or chlorine. <??>The novel compounds act as diuretics and saluretics and have a hypotensive action.

PROCESS FOR THE PREPARATION OF ARALQUILAMINOALCOXYPHENYL DERIVATIVES

1-benzenesulphonyl-1,3-dihydrobenzimidazol-2-one derivatives and medicaments

ADJUSTMENT OF THERAPEUTIC FREQUENCY OF THERAPEUTIC

PROCEDURE FOR THE PREPARATION OF AMINOAL COCOXYPHENYL DERIVATIVES.

Actinic ray-sensitive or radiation-sensitive resin composition, and, actinic ray-sensitive or radiation-sensitive film and pattern forming method, each using the same

본 발명의 감활성광선성 또는 감방사선성 수지 조성물은 하기 일반식(N1)으로 나타내어지는 질소 함유 화합물(N)을 함유한다. [상기 일반식(N1)에 있어서, X는 헤테로 원자를 포함하는 기를 나타내고, L은 단일 결합 또는 알킬렌기를 나타내고, R 2 는 치환기를 나타내고, 복수 존재하는 경우에는 서로 같아도 좋고 달라도 좋고, 복수의 R 2 가 서로 결합하여 환을 형성하여도 좋고, R 3 은 수소 원자 또는 치환기를 나타내고, 또한 n은 0~4의 정수를 나타낸다.]

1- (ARILSULFONIL) -4- (PIPERAZIN-1-IL) -1H-BENZIMIDAZOLES AS LIGANDS OF 5-HYDROXYTHYRIPTAMINE-6

La invención se refiere a compuestos 1-(arilsulfonil)-4-(piperazin-1-il)-1H-benzimidazol de la fórmula I: o una sal farmacéuticamente aceptable de éste (succinato), como ligandos de 5-hidroxitriptamina-6 en donde las variables constitutivas son como se definen en la presente. The invention relates to compounds 1- (arylsulfonyl) -4- (piperazin-1-yl) -1H-benzimidazole of the formula I: or a pharmaceutically acceptable salt thereof (succinate), as 5-hydroxytryptamine-6 ligands in where the constitutive variables are as defined herein.

4-CHLORINE-3-SULFAMOYL-BENZOESAEURE-HYDRAZIDE, METHOD FOR THE PRODUCTION THEREOF, MEDICINAL PRODUCTS CONTAINING THESE COMPOUNDS, AND USE OF THE NEW COMPOUNDS FOR THE PRODUCTION OF DIURETIC AND SALT-MEDICATING AGENTS.

The novel compounds according to the invention correspond to the general formula I <IMAGE> in which R represents hydrogen, a trifluoromethyl or carboxyl group, an alkoxycarbonyl group having 2-5 carbon atoms, a cyano, benzoyl or sulphamoyl group or an alkylsulphonyl group having 1-4 carbon atoms, R<1> represents hydrogen, an alkylthio or alkylsulphonyl group each having 1-4 carbon atoms, a straight or branched alkyl group having 1-4 carbon atoms, or a benzylthio, benzylsulphonyl, phenyl, hydroxyl or thiol group and R<2> represents hydrogen or chlorine. <??>The novel compounds act as diuretics and saluretics and have a hypotensive action.

Sulfenylated bis-benzimidazoles

Patent FR1555336A

Patent FR2276821B1

Benzo five-membered nitrogen heterocyclic piperidine or piperazine derivatives and preparation methods and pharmaceutical compositions thereof

Compounds of formula (I) and its pharmaceutically acceptable salts are described wherein R 1 , R 2 , X, Y, A, B are as defined in the specification. Also disclosed are methods for preparing the compounds of formula (I) or pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the compounds of formula (I) or pharmaceutically acceptable salts thereof.

AMINOBENZIMIDAZOLES

Actinic ray-sensitive or radiation-sensitive resin composition, and, actinic ray-sensitive or radiation-sensitive film and pattern forming method, each using the same

An actinic ray-sensitive or radiation-sensitive resin composition in the present invention contains a nitrogen-containing compound (N) which is represented by the following general formula (N1):wherein, in the general formula (N1), X represents a group including a hetero atom; L represents a single bond or an alkylene group; R 2 represents a substituent, in the case where a plurality of R 2 's are present, they may be the same as or different from each other and a plurality of R 2 's may be bonded to each other to form a ring;R 3 represents a hydrogen atom or a substituent; and n represents an integer of 0 to 4.

Benzo five-membered nitrogen heterocyclic piperidine or piperazine derivatives and preparation methods and pharmaceutical compositions thereof

Aralkylaminoalkoxyphenyl derivatives, process of preparation and compositions containing the same

The present invention relates to aminoalkoxy­phenyl derivatives of formula : in which : B represents a -S-, -SO- of SO₂- group, and C y is an organic cyclic group. These compounds are calcium inhibitors and are useful for the treatment of pathological syndroms of the cardiovascular system.

Antibacterial agents

The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X=NH Y=CO, CS, -C(=N-CN) or X and Y together form an alkene, or C3-C5 cycloalkyl; R1 is -COOH; R2 is an electron withdrawing group; R4 is an optionally substituted aryl. The compounds of formula I are antibacterial agents that are useful for sterilization sanitation, antisepsis, and disinfection.

Transcription factor modulating compounds and methods of use thereof

Substituted benziomidozole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benziomidazole compounds, as well as pharmaceutical preparations therefore, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

hexahydro-5H-benzo [ d ] imidazole-5-ketone derivative and preparation method and application thereof

本发明涉及化学合成领域，具体为六氢‑5H‑苯并[d]咪唑‑5‑酮类衍生物及其制备方法和应用；本发明使用1,3,5‑三嗪烷和醌胺在三氟甲磺酸铟催化高效合成六氢‑5H‑苯并[d]咪唑‑5‑酮类衍生物。反应操作简单，一步构造含双氮苯并五元环产物，方法简洁高效，且后处理方便，产率普遍很高，产品在制备过程中无需惰性气体保护，底物适用性广、操作简单、适合大量合成。

PROCEDURE FOR THE PREPARATION OF NEW 4-CHLORO-3-SULFAMOYL BENZOIC HYDRAZIDES.

Aromatic heterocyclic derivatives and its application on drug

本发明提供一些芳杂环类衍生物或其立体异构体，互变异构体，氮氧化物，溶剂化物，代谢产物，药学上可接受的盐或前药，用于治疗阿尔茨海默症。本发明还公开了含有这样的化合物的药物组合物和使用本发明化合物或其药物组合物治疗阿尔茨海默症的方法。

Non-aqueous electrolyte and non-aqueous secondary battery

本発明は、粘度と比誘電率とのバランスに優れたアセトニトリル、及びフッ素含有無機リチウム塩を含有する非水系電解液において、遷移金属とアセトニトリルとからなる錯体カチオンの生成を抑制し、優れた負荷特性を発揮するとともに、充放電サイクルを繰り返した際の内部抵抗の増加を抑制することができる非水系電解液及び非水系二次電池を提供することを目的とする。本発明は、アセトニトリルを含む非水系溶媒と、フッ素含有無機リチウム塩と、ベンゾトリアゾールに代表される特定の窒素含有環状化合物と、を含有する非水系電解液などに関する。 The present invention suppresses the formation of a complex cation composed of a transition metal and acetonitrile in a non-aqueous electrolyte containing acetonitrile and a fluorine-containing inorganic lithium salt with an excellent balance between viscosity and relative dielectric constant, and has an excellent load. An object of the present invention is to provide a non-aqueous electrolyte solution and a non-aqueous secondary battery that exhibit characteristics and can suppress an increase in internal resistance when a charge / discharge cycle is repeated. The present invention relates to a non-aqueous electrolyte solution containing a non-aqueous solvent containing acetonitrile, a fluorine-containing inorganic lithium salt, and a specific nitrogen-containing cyclic compound typified by benzotriazole.

Sulfenamide-containing lipoxygenase inhibitor

1-benzenesulfonyl-1,3-dihydro-2h-benzimidazol-2-one derivatives

entitled: 1-Benzenesulfonyl-1,3-dihydro-2H-benzimidazol-2-one derivatives in the name of: SANOFI ABSTRACT OF THE DISCLOSURE The present invention relates to 1-benzenesulfonyl-1,3-dihydro-2N-benzimidazol-2-one derivatives of the formula : (I) to their preparation and to the pharmaceutical compositions in which they are present. These derivatives have an affinity for the vasopressin and oxytocin receptors.

Halogeno-Alkane-Sulphenyl Heterocyclics

1,173,149. Fungicides containing sulphenyl heterocyclics. DYNACHIM. 5 Dec., 1966 [6 Dec., 1965 (4); 28 March, 1966; 4 April, 1966; 29 April, 1966; 2 May, 1966 (2); 9 June, 1966; 10 June, 1966; 6 Oct., 1966; 21 Oct., 1966], No. 54364/66. Headings A5B and A5E. [Also in Division C2] A fungicidal composition comprises one or more of the compounds of formula I wherein either W represents a direct bond, X and Y together represent one of the linkages -N=N-, CR<SP>1</SP>=CR<SP>2</SP>-, -S-o-Ï-, -O-o-Ï-, -N=CR<SP>4</SP>-or -N=CR<SP>5</SP>-, and Z represents a benzene ring optionally substituted with one or more alkyl and/or alkoxy and/or nitro and/or halogen and/or -CF 3 groups; or in which W is a -CO- linkage, and either X and Y together represent a -N=N- linkage and Z is as defined above, or X and Y together represent a -CO-linkage and Z represents a benzene, cyclohexane or cyclopentane ring fused elsewhere to a corresponding -CO-NH-CO- ring structure optionally N-substituted with a further -S.A radical; and wherein A is either a methyl group substituted with 2 or 3 similar or disimilar halogens or an ethyl or ethylene group substituted with at least two similar or dissimilar halogens with the proviso that when X and Y together signify or -N=N- and W is a direct bond A is not dihalofluoromethyl wherein the halo atoms which may be the same or different are F, Cl or Br; while R<SP>1</SP> and R<SP>2</SP> which may be the same or different each represents a hydrogen atom or an alkyl, aralkyl, aryl, cyano or cyanoalkyl group and R<SP>2</SP> may be bromine; R<SP>3</SP> represents a phenyl, furyl or thiemyl radical optionally substituted by one or more halogens and/or alkyl and/or alkoxy and/or nitro groups; R<SP>4</SP> represents a hydrogen atom, or an alkyl, aralkyl or aryl radical, optionally substituted with one or more halogen and/or nitro and/or alkoxy and/or alkyl- ...

Modulators of the integrated stress pathway

Provided herein are compounds of formula (I), compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases, disorders and conditions. (Formula I).

N-sulfonylbenzimidazolone derivatives, their preparation, pharmaceutical compositions containing them.

L'invention concerne des dérivés N-sulfonylbenzimidazolones de formule: (CF DESSIN DANS BOPI) et leurs sels éventuels, ainsi que leur préparation et les compositions pharmaceutiques en contenant. Ces composés ont une affinité pour les récepteurs de la vasopressine et/ou de l'ocytocine. The invention relates to N-sulfonylbenzimidazolones derivatives of the formula: (CF DRAWING IN BOPI) and their possible salts, as well as their preparation and pharmaceutical compositions containing them. These compounds have an affinity for vasopressin and / or oxytocin receptors.

Method for Preparation of Benzimidazole Derivatives

본 발명은 벤즈이미다졸 유도체의 제조방법 및 이에 의하여 제조된 화합물에 관한 것이다.

Porous metal organic framework based on pyrroles and pyridinones

The present invention relates to a process for preparing a porous metal organic framework containing at least one organic compound coordinated to at least one metal ion, which comprises the step of oxidation of at least one anode containing metal corresponding to the at least one metal ion in a reaction medium in the presence of the at least one organic compound, where the at least one organic compound is a monocyclic, bicyclic or polycyclic ring system which is derived at least from one of the heterocycles selected from the group consisting of pyrrole, alpha-pyridone and gamma-pyridone and has at least two ring nitrogens, where the ring system is unsubstituted or has one or more substituents selected independently from the group consisting of halogen, C1-6-alkyl, phenyl, NH2, NH(C1-6-alkyl), N(C1-6-alkyl)2, OH, Ophenyl and OC1-6-alkyl, where the substituents C1-6-alkyl and phenyl are unsubstituted or have one or more substituents selected independently from the group consisting of halogen, NH2, NH(C1-6-alkyl), N(C1-6-alkyl)2, OH, Ophenyl and OC1-6-alkyl.

Hydroxamate compounds, use thereof and synthesizing method for the same

Nonaqueous electrolyte and nonaqueous secondary battery

Heterocyclic compounds

본 발명은 히스톤 탈아세틸화효소(HDAC)의 억제제인 화합물에 관한 것이다. 더욱 상세하게는, 본 발명은 헤테로시클릭 화합물 및 이의 제조방법에 관한 것이다. 이들 화합물은 히스톤 탈아세틸화효소 (HDAC) 활성을 갖는 효소를 포함하는, 그 효소에 관한, 또는 그 효소에 관련된 기타 질병뿐만 아니라 증식 장애의 치료용 의약으로서 유용할 수 있다. The present invention relates to compounds that are inhibitors of histone deacetylase (HDAC). More specifically, the present invention relates to heterocyclic compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases related to, or related to, the enzyme, including enzymes having histone deacetylase (HDAC) activity. 히스톤 탈아세틸화효소, 헤테로시클릭 화합물 Histone deacetylase, heterocyclic compound

Sulfonamide imidazole salt compound and preparation method and application thereof

本发明公开了一种磺酰胺咪唑盐化合物及其制备方法，所述制备方法主要包括以下步骤：将咪唑类化合物溶于二氯甲烷，与磺酸酐或者磺酰氟在0℃下进行反应，反应一段时间后，减压蒸馏除去溶剂，再用二氯甲烷萃取，干燥，抽滤，然后加入三氟甲磺酸烷基酯，反应时间8‑12h，得到磺酰胺咪唑盐的粗品，经重结晶提纯得到磺酰胺咪唑盐，再将所得的磺酰胺咪唑盐在光催化条件下进行脱二氧化硫产生自由基，该发明涵盖的磺酰胺咪唑盐化合物不仅具有化学性质稳定、成本低、易提纯等优点以外，且由于有机离子盐结构的引入，能够适应各种自由基反应。通过改变咪唑结构，能够选择性生成各种碳自由基，这为有机化学和药物合成提供了便利。

Method for producing hydrazides of 4-chlor-3-sulfamoylbenzoic acid of their pharmaceutically available salts

Использование: в качестве соединени , обладающего диуретическим и салидиуре- тическим действием. Сущность: продукт формулы: Изобретение относитс  к способу получени  новых гидразидов 4-хлор-З-сульфа- моилбензойной кислоты общей формулы: N V, UA(О Щ-ы где RI - алкил (Ci-C4) - тио-группа, алкил (Ci-C4) сульфонильна , бензилтио-группа H-co-(CU-ci SO.jNH2 где RI - алкил Ci-4 - тио-группа, алкил(С1- С4)сульфонильна , бензилтио-группа или меркапто-группа, Ra - атом водорода, RS - трифторметил, карбоксильна , алкокси-(С2 С5)карбонильна , циано-группа, бензоиль- на ,сул ьфамоильна или алкил()сульфонильна  группа. Реагент I: 2-аминофенилгидразиновое производное общей формулы: . -t HI XNH-NH-CO-O-C1 Ч где R4 и Rs - водород или вместе группу- СНМ(СНзЬ- Реагент 2: сероуглерод, этилк- сантат кали  или тиофосген. Удаление защитной группы в щелочной среде и выделение целевого продукта, где Ri-SH или ал- килируют полученное соединение и удал ют защитную группу в щелочной среде и выдел ют целевой продукт, или полученное соединение окисл ют с последующим гидролизом в щелочной среде. 2 табл. или меркапто-группа; Ra-атом водорода, Ra - трифторметил, карбоксильна , алкокси - () карбонильна , циано-группа, бензо- ильна , сульфамоильна  или алкил (Ci-C4) сульфонильна  группа. Соединени  общей формулы (I) обладают диуретическим и салидиуретическим действием. Цель изобретени  - синтез новых диуретиков в р ду бензимидазолов по своей 00 со о о Os со

Aminoalkoxyphenyl derivatives, their preparation and pharmaceutical and veterinary compositions containing them

Process for the preparation of substituted benzimidazole-1-oxides

Process for preparing novel imidazole salts

Onium salt of nitrogen-containing heteroaryl compound and pest control agent

A compound represented by formula (I) or formula (II) has a pest control effect. (In the formulae, Q 1 represents a pyrazine ring or the like; G 1 represents a nitrogen atom or a carbon atom; X 1 represents an alkyl group or the like; m represents the number of X 1 moieties; A represents an oxygen atom or the like; Y represents a single bond or the like; Q 2 represents a benzene ring or the like; X 2 represents an alkyl group, an aryl group or the like; X 3 represents a halogeno group or the like; n represents the number of X 3 moieties; Z q- represents a counter ion; and q represents 1 or 2.)

Aminobenzimidazoles