Способ получения бензтиазолсульфенамидов

Способ получения тиазолсульфенамидов

Improvements in vulcanization accelerators

The invention comprises N-(thiocarbamythio) - 2 - benzothiazolesulphenamides of the formula wherein R, R1 and R11 are hydrogen, alkyl, cycloalkyl or aralkyl radicals, or R1 and R11 together with the nitrogen atom to which they are attached represent a saturated monocyclic residue. R, R1 and R11 may be methyl, ethyl, n-propyl, isopropyl, n-butyl, sec.-butyl, tert.-butyl, n-amyl, 2-ethylhexyl, cyclohexyl, methylcyclohexyl, benzyl and/or b -phenethyl, and R1 and R11 taken together may be pentamethylene and oxydiethylene. The compounds are prepared by reacting an S-(thiocarbamyl)-hydrosulphamine of the formula with 2 - benzothiazolesulphenyl chloride in the presence of a tertiary aliphatic amine. Specified tertiary amines are triethylamine, tripropylamine, tributylamine, triamylamine and N-methylmorpholine. The examples describe the preparation of N-ethyl-N1-(dimethylthiocarbamylthio)-, N - methyl - N1 - (dimethylthiocarbamylthio) -, N - isopropyl ...

A new benzothiazole sulfenamide of a tertiary cycloalkyl amine

Natural rubber and rubbery butadiene-styrene, butadiene - acrylonitrile copolymers, polyisoprenes and polybutadienes are vulcanized by heating (e.g. to 260 DEG -400 DEG F.) with sulphur in the presence of a relatively small amount (e.g. 0.1 to 10 per cent of the weight of rubber) of N-(1-methylcyclopentyl)-2-benzothiazolesulphenamide as accelerator. In an example, in which the rubber is smoked sheet, the mix also contains HAF carbon black, zinc oxide, refined pine gum (softener), stearic acid and an antioxidant; in an example, in which the rubber is an emulsion-polymerized butadiene-styrene copolymer, the mix also contains HAF carbon black, processing oil, zinc oxide, stearic acid and phenyl-b -naphthylamine. The process is particularly applicable to tyres containing furnace blacks (e.g. ISAF and SAF in addition to HAF). The sulphur may be replaced by a sulphur-donor (e.g. a phenol polysulphide, a xanthogen polysulphide, a thiuram di- or poly-sulphide or an amine polysulphide).ALSO:The ...

Improvements in manufacture of n-alkyl-and n-cycloalkylbis-(2-benzothiazolesulphen)amides

N - alkyl - and N - cycloalkyl - bis-(2 - benzothiazolesulphen) amides are prepared by the gradual addition of an appropriate primary alkylamine or primary cycloalkylamine to 2-benzthiazolesulphenyl chloride in approximately 3 : 2 molar ratio, respectively, at a temperature in the range from -40 DEG to 0 DEG C. The reaction may be conducted in a solvent such as n-hexane, methylene or ethylene chloride, carbon tetrachloride, benzene, toluene or chlorobenzene. The examples describe the preparation of N-isopropylbis-(2-benzothiazolesulphen) amide, N - cyclohexylbis - (2 - benzothiazolesulphen) amide, N-methylbis-(2-benzothiazolesulphen) amide and N-ethylbis-(2-benzothiazolesulphen) amide. The 2-benzothiazolesulphenyl chloride may be prepared by treating benzothiazolyl disulphide with chlorine in one of the solvents specified above.

N-(propynyl)-2-(thiazole) sulfenamides

Natural or synthetic rubber is vulcanized in the presence of sulphur or a sulphur-donor type vulcanization agent and an N-(propynyl)-2-(thiazole) sulphenamide vulcanization accelerator of the formula:- wherein R1 and R2 are hydrogen or alkyl radicals or, together with the ethylene nucleus to which they are attached, form an alicyclic or aromatic ring, R3 is hydrogen or an alkyl radical, R4 is a substituted or unsubstituted hydrocarbon radical, or R3 and R4, together with the carbon atom to which they are attached, represent a cyclic hydrocarbon radical.ALSO:The invention comprises N-(propynyl)-2-(thiazole) sulphenamides of the formula: wherein R1 and R2 are hydrogen or alkyl radicals, or together with the ethylene nucleus to which they are attached form an alicyclic or aromatic ring, R3 is hydrogen or an alkyl radical and R4 is a substituted or unsubstituted hydrocarbon radical, or R3 and R4, together with the carbon atom to which they are ...

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use.

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof: in which: R.1 is vinyl or ethyl; and R2 is a group R3, R4CH2~, or R5R6C=CH-; wherein each of R3 and R4 is an azabicyclic ring system or R5 and R^ together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

Carbamoyloxy derivatives of mutiline and their use as antibacterials.

Derivatives of mutiline of formula (1a)and pharmaceutically acceptable salts and derivatives thereof, in which r1 is ethyl or vinyl, y is a carbamoyloxy group, which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Novel compounds

Novel compounds.

Compounds of formula (1a)and pharmaceutically acceptable salts and derivativews thereof in which y is a carbamoyloxy group, in which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Carbamoyloxy derivatives of mutiline and their useas antibacterials.

Carb moylo y der vativ s of utiline and their use as antibacterials

Novel compounds

Novel compounds

PNA MONOMER AND PRELIMINARY STAGE

CA IX-specific inhibitors

Novel imaging composition and uses thereof

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

Carbamoyloxy derivatives of mutiline and their use as antibacterials

PROCESS FOR THE PRODUCTION OF THIAZOLYL-2- SULPHENAMIDES

ABSTRACT This invention relates to a process for the production of benzthiazolyl sulphenamides corresponding to the following general formula: in which a corresponding 2-mercaptobenzthiazole or a dibenzthiazolyl-2,2'-disulphide is reacted with a primary or secondary amine at temperatures of from 0 to 100°C in the presence of ammonia, oxygen, a copper-containing catalyst and a reaction medium consisting to an excess of the primary or secondary amine or of a mixture of that amine with water and/or a water-miscible organic solvent. Benzthiazolyl sulphenamides are valuable vulcanization accelerators.

MANUFACTURE OF SULFENAMIDES

ABSTRACT OF THE DISCLOSURE A process for the manufacture of sulfenamides by the oxidation of a mixture of 2-mercaptobenzothiazole and the appropriate amine in a critical amount of water and/or organic solvent produces a pure product of good quality and high yield. The amount of water should be in the range of from 10 to 30% by weight based on the total reaction mixture.

PROCEDE DE PREPARATION DE THIAZOLSULFENAMIDES

HYDANTOIN DERIVATIVES

The present invention relates to novel hydantoin derivatives, processes for producing said hydantoin derivatives, pharmaceutical compositions containing at least one of said hydantoin derivatives as aldose reductase inhibitors and novel intermediate compounds in the synthesis of said hydantoin derivatives. The present invention is based on the selection of a hydantoin which is bonded by a sulfonyl group to various substituents at the 1-position of the hydantoin skeleton. The compounds of the present invention have a strong inhibitory activity against aldose reductase. These compounds are extremely useful for the treatment and/or prevention of various forms of diabetic complications based on the accumulation of polyol metabolites.

PROCESS FOR THE MANUFACTURE OF A SULFENIMIDE

A process for the manufacture of a sulfenimide by reacting sulfenamide in slurry with an organic water immiscible solvent with an acid to yield a solvent slurry comprising sulfenimide product. The product i s recovered from the solvent slurry by a method comprising the addition of water to the solvent slurry and the isolating of the product by a single filtration step. While water is added to the solvent slurry an azeotrope of solvent and water may be distilled under vacuum until substantially all solvent is separated from product and product becomes part of an aqueous slurry. Alternatively, water may be added to the solvent slurry while the resulting mixture is being agitated, followed by filtering the mixture in the single filtration step for recovery of product from the mixture.

PROCEDE DE PREPARATION DE THIAZOLSULFENAMIDES

PROCEDE DE FABRICATION DE BIS(BENZOTHIAZYLSULFENE) AMIDES

Verfahren zur Herstellung eines Sulfenamids.

Procédé de préparation de sulfonamides hétérocycliques substitués

Verfahren zur Darstellung eines Sulfenamides.

Verfahren zur Herstellung eines Sulfenamids.

Verfahren zur Herstellung von Sulfonylsenfölen

Verfahren zur Herstellung N-trifluormethylierter Sulfenamide

Procedimento per la preparazione di solfonammidi eterocicliche

Procédé de fabrication de bis(benzothiazylsulfène)amides

[...] DE [...][...] DE.

PROCEDURE FOR THE PRODUCTION OF N-CYCLOHEXYLBENZOTHIAZOL-2-SULFENAMID.

KARBAMOILOKSIPROIZVODNYE MUTILIN AND THEIR USE AS ANTIBACTERIAL AGENTS

ПРОИЗВОДНЫЕ N-(АРИЛСУЛЬФОНИЛ)БЕТА-АМИНОКИСЛОТ, СОДЕРЖАЩИЕ ЗАМЕЩЕННУЮ АМИНОМЕТИЛЬНУЮ ГРУППУ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Данное изобретение относится к соединениям, имеющим формулу (I). Указанные соединения обладают аффинитетом к брадикининовым рецепторам с селективностью в отношении B1 рецепторов, и они могут быть использованы для приготовления лекарств, которые предназначены для лечения или предупреждения персистирующих или хронических воспалительных заболеваний и воспалительных патологий.

DERIVATIVES OF N - (ARYLSULFONYL) BETA - AMINO ACIDS, CONTAINING SUBSTITUTED AMINOMETILNUYu GROUP, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

New nitrogenized organic compounds

Process for the preparation of new compositions of sulfènamides

Sophisticated method of preparation of chemicals, and sophisticated chemicals obtained using this process

NEW METHOD OF PREPARATION OF THE BENZOTHIAZOLE-SULFENAMIDES

Improvements with the preparation of heterocyclic sulphonamides

Process to prepare taxol

PNA monomer and precursor

This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

СПОСОБ КАТАЛИТИЧЕСКОГО ОКИСЛЕНИЯ ТИОЛА ИЛИ ЕГО СОЛИ ИЛИ ДИТИОКАРБАМИНОВОЙ КИСЛОТЫ ИЛИ ЕЕ СОЛЕЙ

Каталитическое окисление тиолов или тиоловых солей, дитиокарбаминовых кислот или их солей с использованием кислорода, необязательно в присутствии первичного или вторичного амина проводят с использованием угольного катализатора, свободного от металлического порфиразина или производного порфиразина. 1 с. и 11 з.п. ф-лы.

СУЛЬФЕНАМИД, УСКОРИТЕЛЬ ВУЛКАНИЗАЦИИ КАУЧУКА, СОДЕРЖАЩИЙ СУЛЬФЕНАМИД И СПОСОБ ПОЛУЧЕНИЯ УСКОРИТЕЛЯ ВУЛКАНИЗАЦИИ

1. N-алкил-N-третбутилбензотиазол-2-сульфенамид, представленный формулой [I]: ! ! где R означает этил, н-пропил или н-бутил. ! 2. Ускоритель вулканизации каучука, отличающийся тем, что содержит N-алкил-N-третбутилбензотиазол-2-сульфенамид, представленный формулой [I]: ! ! где R означает этил, н-пропил или н-бутил. ! 3. Способ получения N-алкил-N-третбутилбензотиазол-2-сульфенамида, представленного формулой [I], отличающийся тем, что включает взаимодействие N-алкил-N-третбутилхлорамина, представленного формулой [II], бис(бензотиазол-2-ил)дисульфида и N-алкил-третбутиламина в присутствии N-алкил-третбутиламина, который взят в двукратном мольном количестве к моль бис(бензотиазол-2-ил)дисульфида в растворителе: ! ! где R означает этил, н-пропил или н-бутил. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2010 131 168 (13) A (51) МПК C07D 277/80 (2006.01) C08K 5/47 (2006.01) C08L 21/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (71) Заявитель(и): ОУТИ СИНКО КЕМИКАЛ ИНДАСТРИАЛ КО., ЛТД. (JP) (21)(22) Заявка: 2010131168/04, 24.12.2008 Приоритет(ы): (30) Конвенционный приоритет: 27.12.2007 JP 2007-337035 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 27.07.2010 (87) Публикация заявки РСТ: WO 2009/084538 (09.07.2009) R U (54) СУЛЬФЕНАМИД, УСКОРИТЕЛЬ ВУЛКАНИЗАЦИИ КАУЧУКА, СОДЕРЖАЩИЙ СУЛЬФЕНАМИД И СПОСОБ ПОЛУЧЕНИЯ УСКОРИТЕЛЯ ВУЛКАНИЗАЦИИ (57) Формула изобретения 1. N-алкил-N-третбутилбензотиазол-2-сульфенамид, представленный формулой [I]: где R означает этил, н-пропил или н-бутил. 2. Ускоритель вулканизации каучука, отличающийся тем, что содержит N-алкил-Nтретбутилбензотиазол-2-сульфенамид, представленный формулой [I]: где R означает этил, н-пропил или н-бутил. 3. Способ получения N-алкил-N-третбутилбензотиазол-2-сульфенамида, представленного формулой [I], отличающийся тем, что включает взаимодействие Nалкил-N-третбутилхлорамина, представленного формулой [II], бис(бензотиазол-2ил)дисульфида и N-алкил-третбутиламина в присутствии ...

СПОСОБ ПОЛУЧЕНИЯ N-АЛКИЛ-2-БЕНЗТИАЗОЛИЛСУЛЬФЕНИМИДОВ, ОБОРУДОВАНИЕ ДЛЯ ИХ ПОЛУЧЕНИЯ И СПОСОБ ИХ ОЧИСТКИ

... 1. Способ получения N-алкил-2-бензтиазолилсульфенимидов общей формулы I (I) где R представляет собой неразветвленный или разветвленный С1-С12-алкил или C3-С9 -циклоалкил, посредством взаимодействия 2-бензтиазолилсульфенилхлорида с избытком соответствующего алкиламина в инертной реакционной среде, отличающийся тем, что взаимодействие сульфенилхлорида с соответствующим алкиламином проводят при температуре от 5 до 15°С с использованием 10-100% избытка концентрированного алкиламина, по сравнению с теоретическим количеством, т.е. 3,3-6 эквивалентов алкиламина на 2 эквивалента сульфенилхлорида, в то время как влагу оборудования, растворитель, исходный материал удаляют перегонкой части растворителя азеотропной перегонкой при атмосферном или пониженном давлении, и возможный остаточный дисульфид удаляют добавлением водного гидроксида натрия при температуре 20-50°С, тогда как сульфенимид отделяют фильтрованием. 2. Способ по п.1, отличающийся тем, что взаимодействие сульфенилхлорида с соответствующим ...

Herstellung substituierter Thiazolsulfenamide

Verfahren zur Herstellung N-trifluormethylierter Sulfenamide

PROCESS FOR THE PREPARATION OF BENZOTHIAZOLE SULFENE AMIDES

AMINOMETHYLGRUPPEN ENTHALTENDE N-(ARYLSULFONYL)BETA-AMINOSÄURE-DERIVATE, VERFAHREN ZU DEREN HERSTELLUNG SOWIE DEREN PHARMAZEUTISCHE ZUBEREITUNGEN

Preparation of n-alkyl-and n-cyclo-alkylbis (2-benzothiazolesulfen) amides

N-alkyl and N-cycloalkyl-bis-(2-Benzothiazolesulfen) amides are produced by reacting one mole of an N-alkyl or N-cycloalkyl-2-benzothiazolesulfenamide under substantially anhydrous conditions with one half equivalent of an acid having an ionisation constant Ka of above 1 x 10-3 at 25 DEG C. Acids include hydrogen chloride, hydrogen bromide, 100% sulphuric acid, chloroacetic acid, bromoacetic acid, cyanoacetic acid, dichloroacetic acid, trichloroacetic acid, o-chlorobenzoic acid, o-bromobenzoic acid, o-nitrobenzoic acid, 3,5-dinitrobenzoic acid. The reaction may be carried out in an inert organic solvent and at a temperature between -20 DEG C. and 100 DEG C. U.S.A. Specifications 2,807,620, 2,860,142, 2,873,277 and 2,889,331 are referred to.

PREPARATION OF BENZOTHIAZOLE-2-SULPHENAMIDES

METHOD FOR THE PRODUCTION OF N-CYCLOHEXYLBENZOTHIAZOLE-2-SULFENAMIDE

Improvements in or relating to rubber vulcanisation

Products suitable for use as accelerators for the vulcanization of rubber are prepared by reacting an isocyclic saturated organic base with a mercaptoarylthiazole or di- or polysulphide thereof, or with thiuram di- or polysulphide or with aryldithiocarboxylic acid disulphides. Starting materials comprise decahydro-a -and b -naphthylamine, bornylamine, dibornylamine, methylbornylamine, ethylbornylamine, carylamine, cyclohexylamine, dicyclohexylamine, cyclohexylmethylamine, cyclohexylethylamine on the one hand, and mercaptobenzthiazole, mercaptotolylthiazole, mercaptonaphthothiazole, dibenzthiazyl di- and polysulphides, tetramethylthiuram di- and polysulphides, tetraethylthiuramdisulphide, dithiobenzoic acid disulphide and dithiosalicylic acid disulphide. The products are relatively stable and give no offensive odour to the vulcanized rubber. In use, these accelerators may be incorporated with other substances modifying the vulcanization of the rubber mix, for example diphenylguanidine. In ...

Production of improved physical forms of heat-sensitive materials

A powdered material which decomposes in the molten state is converted directly into a molten film which is then solidified and flaked. The material on being melted is heated to such a temperature and for such a time as to avoid substantial decomposition and is then cooled to effect crystallization and avoid supercooling. Heating may be by a steam-heated roll. Cooling may be by a warm water-heated roll or by direct heat-exchange with a gaseous or liquid cooling medium. The powder may be fed by a vibratory spreader feeder, screw conveyer or vibrating screen to an upper heating applicator roll and the resulting molten film transferred to a lower cooling flaking roll provided with a stationary flaking knife. Materials specified are acid-polymerized 2,2,4-trimethyl dihydroquinoline containing 5% of stearic acid and the following thiazolesulphenamides: N - cyclohexyl - 2 - benzothiazolesulphenamide, N - tertbutyl - 2 - benzothiazolesulphenamide, 2 - (2,6 - dimethyl morpholinylmercapto)benzthiazole ...

PROCEDURE FOR THE CATALYTIC OXIDATION OF THIOLEN

PROCEDURE FOR the PRODUCTION OF N-ALKYL OR n CYCLOALKYL-2-BENZOLTHIAZOLESULFENIMIDEN

PROCEDURE FOR PRODUCTION OF TAXOL

HYDANTOIN DERIVATIVES

Catalytic oxidation process

MODULATORS OF INDOLEAMINE 2,3-DIOXYGENASE

Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of HIV; including the prevention of the progression of AIDS and general immunosuppression.

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

PROCESS FOR THE PRODUCTION OF THIAZOLYL-2- SULPHENAMIDES

AZABICYCLIC CARBAMOYLOXY MUTILIN DERIVATIVES FOR ANTIBACTERIAL USE

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R1 is vinyl or ethyl; and R2 is a group R3, R4CH2-, or R5R6C=CH-; wherein each of R3 and R4 is an azabicyclic ring system or R5 and R6 together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

N-(ARYLSULFONYL)BETA-AMINOACID DERIVATIVES WITH SUBSTITUTED AMINOMETHYL GROUP, A METHOD FOR OBTAINING THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THEREOF

СЕЛЕКТИВНЫЕ ИНГИБИТОРЫ ММР-12 И ММР-13 НА ОСНОВЕ ГИДРОКСАМОВОЙ КИСЛОТЫ

В заявке описано соединение формулы (I) которое является ингибитором ММР-12 и/или ММР-13 и поэтому его можно использовать для лечения нарушения или заболевания, характеризующегося аномальной активностью ММР-12 и/или ММР-13. В соответствии с этим соединение формулы (I) можно использовать для лечения нарушений или заболеваний, опосредуемых ММР-12 и/или ММР-13. В заключение в заявке также описана фармацевтическая композиция, которая включает соединение формулы (I).

带有取代氨甲基的N-(芳基磺酰基)-β-氨基酸衍生物、其制备方法和含有该化合物的药物组合物

... 本发明涉及具有通式(I)的化合物。此化合物表现出对缓激肽受体的亲合性，同时对受体B1具有选择性：它们能够用于制备药物，用来治疗或预防炎性的病理和持久性或慢性炎性疾病。 ...

N (propynyl) - 2 (thiazole) sulfénamides and their application to the vulcanization of rubber

Manufactoring process of sulfénamides

NOUVEAU PROCEDE DE PREPARATION DES BENZOTHIAZOLE-SULFENAMIDES

PROCEDE POUR LA PREPARATION DES BENZOTHIAZOLE-SULFENAMIDES CARACTERISE EN CE QUE L'ON FAIT REAGIR UNE DISULFURE DE BENZOTHIAZYLE AVEC UN MELANGE COMPRENANT UN HALOGENOHYDRATE D'AMINE ET UN DERIVE N-HALOGENE D'AMINE.

NEW METHOD OF PREPARATION OF THE BENZOTHIAZOLE-SULFENAMIDES

METHOD OF PREPARATION OF BENZOTHIAZOLYL-SULFENAMIDES

Method of preparation of benzothiazyl-2-dicycloalkyl-sulfènamides

PROCESS FOR PREPARING [...]

PROCESS FOR THE PRODUCTION OF PURE BENZTHIAZYL-SULPHEAMIDES

PROCESS FOR THE PREPARATION OF MORFOLIDA OF THE ACID BENZOTIAZOLILSULFENICO

N-acylsulphonamides and their preparation.

composto e acelerador de vulcanização para borracha

SULFENAMIDE, VULCANIZATION ACCELERATOR CONTAINING THE SULFENAMIDE FOR RUBBER, AND PROCESS FOR PRODUCING THE SAME

A sulfonamide-based vulcanization accelerator is provided which acts sufficiently slowly on a vulcanization reaction, generates no carcinogenic nitrosamine, and is free from hygienic or environmental problems such as bioaccumulation. Also provided is an N-alkyl-N-t-butylbenzothiazole-2-sulfenamide represented by formula (I). The vulcanization accelerator for rubbers contains this compound. Furthermore provided is a process for producing the same. [Chemical formula 1] [R represents methyl, ethyl, n-propyl, or n-butyl.] ...

TOPICALLY ACTIVE OCULAR BENZOTHIAZOLE SULFONAMIDE CARBONIC ANHYDRASE INHIBITORS

This invention is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R6 is hydrogen or lower alkyl; each R1 is hydrogen, lower alkyl, halogen, nitro, trihaloalkyl, lower alkoxy, formyl, lower alkanoyl, loweralkylamino or diloweralkylamino; Y is (II) or (III); X is O, S or NR5; R2 is OR7 or NR7R8; each R3 and R4 are independently hydrogen or lower alkyl; R5, R7 and R8 are independently hydrogen or lower alkyl; n is 0-3 and m is 0-6. These compounds are useful for treating glaucoma or assessing corneal function in mammals.

METHOD OF MAKING 2-BENZOTHIAZOLE SULFENAMIDES

Process for preparing benzothiazolesulphenamides

Benzothiazolesulphenamides can be prepared in high yield and purity from dibenzothiazolyl disulphide and a primary or secondary amine in the absence of an oxidizing agent in a water-immiscible organic solvent and in the presence of aqueous alkali by presenting a solution of the amine in the organic solvent and adding dibenzothiazolyl disulphide and aqueous alkali either simultaneously or in succession.

Process for the preparation of benzothiazole-2-sulphenamides

In a process for the production of benzothiazole-2-sulphenamides, a 2-mercaptobenzothiazole in the form of a particulate solid or a dispersion of a particulate solid in a liquid carrier is added gradually and concurrently with an aqueous solution of sodium hypochlorite to a solution of an amine in a mixture of water and a water-miscible organic solvent, the amount of amine being not more than 1.25 moles per mole of 2-mercaptobenzothiazole. A feature of the process is that it represents a significant improvement over prior art methods for the production of sulphenamides derived from secondary amines such as dicyclohexylamine and diisopropylamine.

СПОСОБ КАТАЛИТИЧЕСКОГО ОКИСЛЕНИЯ

Каталитическое окисление тиолов или тиоловых солей, дитиокарбаминовых кислот или их солей с использованием кислорода, необязательно в присутствии первичного или вторичного амина, проводят с использованием угольного катализатора, свободного от металлического комплекса порфиразина или производного порфиразина.

PROCESS FOR PREPARING SULFENAMIDES

... 1,220,566. Sulphenamides. MONSANTO CO. 18 Aug., 1969 [19 Aug., 1968], No. 41063/69. Heading C2C. An N-substituted 2-thiazolesulphenamide is converted to a differently N-substituted 2- thiazolesulphenamide by reaction with an amine having at least one replaceable nitrogen and having a boiling point higher than that of the amine by-product derived by the addition of H to the amide radical of the starting material sulphenamide, and removing said by-product amine from the reaction zone, the reaction being carried out at a temperature of at least the boiling point of the by-product amine at the reaction pressure. A solvent is optionally used, and at least part of the reaction may be effected under reduced pressure. Examples prepare: 2 - (morpholinothio)-, 2 - (2,6 - dimethylmorpholinothio) -, 2 - piperidinothio -, 2 - pyrrolidinothio, 2 - (2,5 - dimethylpyrrolidinothio) - and 2 - (hexahydroazepin - 1 - ylthio) - benzothiazoles; N- cyclohexyl- and N-benzyl-2-benzothiazolesulphenamides; and trimethylenebis ...

PROCEDURE FOR THE PRODUCTION FROM N-ALKYL TO (THIAZOLYL) SULFENIMIDEN

PROCEDURE FOR THE PRODUCTION OF STORABLE BENZOTHIAZOLSULFENAMIDEN.

MORE OXAZOLIDINESTER

AZABICYCLIACHE CARBAMOYLOXY MUTILIN OF DERIVATIVES AS ANTIBACTERIAL MEANS

PROCEDURE FOR THE PRODUCTION OF N-ALKYL-2 BENZTHIAZOLYLSULFENIMIDEN AND PROCEEDING FOR OF THEM AUFREINIGUNG

CA IX-specific inhibitors

CA IX-SPECIFIC INHIBITORS Abstract Therapeutic methods for inhibiting the growth of preneoplastic/ neoplastic vertebrate cells that abnormally express MN protein are disclosed. Screening assays are provided for identifying compounds, preferably membrane impermeant compounds, which inhibit the enzymatic activity of MN protein/ polypeptides and that are useful for treating patients with preneoplastic/neoplastic disease. Further methods are disclosed for the preparation of positively-charged, membrane-impermeant heterocyclic sulfonamide CA inhibitors with high affinity for the membrane-bound carbonic anhydrase CA IX. Preferred CA IX 10 specific inhibitors are aromatic and heterocylic sulfonamides, preferably that are membrane impermeant. Particularly preferred CA IX-specific inhibitors are pyridinium derivatives of such aromatic and heterocyclic sulfonamides. The CA LX-specific inhibitors of the invention can also be used diagnostically/prognostically for preneoplastic/neoplastic disease, ...

Rubber crawler

The present invention provides a rubber crawler with high durability by using the rubber composition, wherein said rubber composition exhibits enhanced adherence between rubber and metal reinforcing material, such as steel cord and the like, particularly adherence after heat aging and under high humidity, without using vulcanizing retarder, such as CTP, which has possibility of generating problems, such as blooming and lowering rubber physical properties after vulcanization; using vulcanization accelerator having the adequate vulcanization retarding effect exerting excellent working ability; lowering rubber scorching as much as possible. The rubber crawler of the present invention comprises a rubber composition as the treatment rubber thereof, which comprises in the amount of 0.1 to 10 parts by weight of sulfenamide-containing vulcanization accelerator, 0.03 to 3 parts by weight of cobalt-containing composition as the equivalent amount of cobalt and 0.3 to 10 parts by weight of sulfur, relative to 100 parts by weight of rubber component.

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 2. The conjugate of claim 1 , wherein L is OR.3. The conjugate of claim 2 , wherein R is Cto Calkyl.4. The conjugate of claim 2 , wherein OR is selected from O-p-toluenesulfonate claim 2 , O-methanesulfonate claim 2 , O-trifluoromethanesulfonate claim 2 , O-benzenesulfonate claim 2 , and O-m-nitrobenzenesulfonate.5. The conjugate of claim 1 , wherein the target molecule is a polypeptide.6. The conjugate of claim 5 , wherein the polypeptide is an antibody.7. The conjugate of claim 6 , wherein the antibody is selected from trastuzumab claim 6 , rituximab and cetuximab.8. The conjugate of claim 1 , wherein the target molecule is a peptide.9. The conjugate of claim 8 , wherein the peptide is a targeting peptide.10. The conjugate of claim 9 , wherein the targeting peptide is selected from a cyclic RGD sequence claim 9 , bombesin and glu-N(CO)N-lys PSMA. This application is a Continuation of U.S. patent application Ser. No. 15/963,599, filed Apr. 26, 2018, which is a Continuation of U.S. patent application Ser. No. 15/518,333, filed Apr. 11, 2017, now U.S. Pat. No. 9,980,930, issued on May 29, 2018 and is a National Stage Application, filed under 35 U.S.C. 371, of International Application No. PCT/AU2015/050640, filed on Oct. 16, 2015, which claims priority to, and the benefit of, AU Application No. 2014904138, filed Oct. 16, 2014. The contents of each of these applications are incorporated by reference in their entirety.The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting ...

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 115-. (canceled)17. The conjugate of claim 16 , wherein L is OR.18. The conjugate of claim 17 , wherein R is Cto Calkyl.19. The conjugate of claim 17 , wherein OR is selected from O-p-toluenesulfonate claim 17 , O-methanesulfonate claim 17 , O-trifluoromethanesulfonate claim 17 , O-benzenesulfonate claim 17 , and O-m-nitrobenzenesulfonate.20. The conjugate of claim 16 , wherein the target molecule is a polypeptide.21. The conjugate of claim 20 , wherein the polypeptide is an antibody.22. The conjugate of claim 21 , wherein the antibody is selected from trastuzumab claim 21 , rituximab and cetuximab.23. The conjugate of claim 16 , wherein the target molecule is a peptide.24. The conjugate of claim 23 , wherein the peptide is a targeting peptide.25. The conjugate of claim 24 , wherein the targeting peptide is selected from a cyclic RGD sequence claim 24 , bombesin and glu-N(CO)N-lys PSMA. The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting radionuclide that is used in medical imaging applications. In particular, it is used in positron emission tomography (PET) for cancer detection and imaging. It has a longer half-life (t=79.3 hours) than other radionuclides used for medical imaging, such as F. For example, F has a tof 110 minutes, which means that its use requires close proximity to a cyclotron facility and rapid and high-yielding synthesis techniques for the preparation of the agents into which it is incorporated. Zr is not plagued by these same problems, which makes ...

MIXTURE OF N-(1,3-BENZOTHIAZOL-2-YLSULFANYL)-2-METHYL-CYCLOHEXANAMINE AND N-(1,3-BENZOTHIAZOL-2-YLSULFANYL)-4-METHYL-CYCLOHEXANAMINE

A composition comprising compound (I) of formula and compound (II) of formula wherein Rand Rindependently from each other are a linear alkyl group with 1 to 4 carbon atoms and R, R, Rto Rand Rto Rindependently from each other are a hydrogen atom or a linear alkyl group with 1 to 4 carbon atoms. 2: The composition according claim 1 , wherein both Rand Rare a methyl group.3: The composition according to claim 1 , wherein R claim 1 , R claim 1 , Rto Rand Rto Rare a hydrogen atom.4: The composition according to claim 1 , wherein a weight ratio of the compound (I) to the compound (II) is from 1:10 to 10:1.5: The composition according to any of claim 1 , wherein a weight ratio of the compound (I) to the compound (II) is from 1:3 to 3:1.6: The composition according to claim 1 , comprising: at least 50% by weight of the compounds (I) and (II).7: A method for accelerating vulcanization claim 1 , the method comprising: accelerating vulcanization with the composition according to as a vulcanization accelerator.8: A rubber composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the composition according to .'} The present invention relates to a composition comprising compound (I) of formulaand compound (II) of formulawherein Rand Rindependently from each other are a linear alkyl group with 1 to 4 carbon atoms and R, R, Rto Rand Rto Rindependently from each other are a hydrogen atom or a linear alkyl group with 1 to 4 carbon atomsBenzothiazolylsulfenamides may be used as vulcanization accelerators. A standard vulcanization accelerator is, for example benzothiazolylsulfenamide is N-(1,3-benzothiazol-2-ylsulfanyl)cyclohexanamine, shortly referred to as CBS. A process for the synthesis of CBS by reacting primary amines with salts of mercapto benzothiazol is described in EP-A 1449 837. CBS is a solid with a melting point of from 96 to 102° C. (1 bar).EP-A 2256 157 discloses derivatives of N-(1,3-benzothiazol-2-ylsulfanyl)-cyclohexanamine and their use as ...

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 1. A radionuclide complex of a compound of formula (I):or a pharmaceutically acceptable salt thereof, wherein L is a leaving group. This application is a Continuation of U.S. patent application Ser. No. 16/511,577, filed Jul. 15, 2019, which is a Continuation of U.S. patent application Ser. No. 15/963,599, filed Apr. 26, 2018, now U.S. Pat. No. 10,398,660 issued on Sep. 3, 2019, which is a Continuation of U.S. patent application Ser. No. 15/518,333, filed Apr. 11, 2017, now U.S. Pat. No. 9,980,930, issued on May 29, 2018 and is a National Stage Application, filed under 35 U.S.C. 371, of International Application No. PCT/AU2015/050640, filed on Oct. 16, 2015, which claims priority to, and the benefit of, AU Application No. 2014904138, filed Oct. 16, 2014. The contents of each of these applications are incorporated by reference in their entirety.The present invention relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. The present invention also relates to compositions including the compounds, and to methods of imaging patients using the compounds.Zirconium-89 (Zr) is a positron-emitting radionuclide that is used in medical imaging applications. In particular, it is used in positron emission tomography (PET) for cancer detection and imaging. It has a longer half-life (t=79.3 hours) than other radionuclides used for medical imaging, such as F. For example, F has a tof 110 minutes, which means that its use requires close proximity to a cyclotron facility and rapid and high-yielding synthesis techniques for the preparation of the agents into which it is incorporated. Zr is not plagued by these same problems, which makes Zr particularly attractive for use in ...

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours. 2. The radionuclide complex of claim 1 , wherein L is OR.3. The radionuclide complex of claim 2 , wherein R is selected from Cto Calkyl claim 2 , Cto Cheteroalkyl claim 2 , Cto Calkene claim 2 , C2 to Cm alkyne and aryl claim 2 , each of which is optionally substituted.4. The radionuclide complex of claim 3 , wherein R is Cto Calkyl claim 3 , preferably Cto Calkyl claim 3 , more preferably methyl or ethyl claim 3 , even more preferably ethyl.5. The radionuclide complex of claim 1 , wherein the leaving group is selected from OCHCH claim 1 , O-p-toluenesulfonate claim 1 , O-methanesulfonate claim 1 , O-trifluoromethanesulfonate claim 1 , O-benzenesulfonate claim 1 , O-m-nitrobenzenesulfonate claim 1 , cyanate claim 1 , azide and halogen.6. The radionuclide complex of claim 1 , wherein the radionuclide is selected from radioisotopes of zirconium claim 1 , gallium claim 1 , lutetium claim 1 , holmium claim 1 , scandium claim 1 , titanium claim 1 , indium and niobium.7. The radionuclide complex of wherein the radionuclide is a radioisotope of zirconium claim 6 , gallium or indium.8. The radionuclide complex of claim 7 , wherein the radionuclide is a radioisotope of zirconium.9. The radionuclide complex of further conjugated to a target molecule to form a radionuclide-labelled conjugate.10. The radionuclide-labelled conjugate of claim 9 , wherein the target molecule is a polypeptide.11. The radionuclide-labelled complex of wherein the complex or conjugate has improved affinity when compared to with DFO-Ph-NCS or a conjugate of DFO-Ph-NCS and the target molecule.12. A method of imaging a patient claim 1 , the method including:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'administering to a patient the radionuclide-labelled conjugate of ; and'}imaging said patient.13. ...

Pna monomer and precursor

Sulphenamide, sulphenamide-containing rubber accelerator, and method of producing rubber accelerator

FIELD: chemistry. SUBSTANCE: invention relates to N-alkyl-N-tert-butylbenzotriazole-2-sulphenamide of formula , where R denotes ethyl, n-propyl or n-butyl. The invention also relates to a rubber accelerator, which is a compound of formula [I], and a method of producing N-alkyl-N-tert-butylbenzotriazole-2-sulphenamide. EFFECT: positive effect of rubber acceleration and solving environmental problems associated with bioaccumulation when using N-alkyl-N-tert-butylbenzotriazole-2-sulphenamide. 3 cl, 6 tbl, 14 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 453 541 (13) C2 (51) МПК C07D 277/80 (2006.01) C08K 5/47 (2006.01) C08L 21/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21)(22) Заявка: 2010131168/04, 24.12.2008 (24) Дата начала отсчета срока действия патента: 24.12.2008 (43) Дата публикации заявки: 10.02.2012 Бюл. № 4 (73) Патентообладатель(и): ОУТИ СИНКО КЕМИКАЛ ИНДАСТРИАЛ КО.,ЛТД. (JP) C 2 2 4 5 3 5 4 1 C 2 R U (56) Список документов, цитированных в отчете о поиске: C.-D. WACKER et al: "New sulfonamide accelerators derived from 'safe' amines for the rubber and tyre industry" IARC, vol.105, 1991, p.592-594. JP 59-172483 A, 29.09.1984. JP 2005139082 A, 02.06.2005. JP 48-11214 B1, 11.04.1973 & US 3,658,828 A, 25.04.1972. IGNATZHOOVER, F. ET AL.: "Delayed action accelerated sulfur vulcanization of high diene (см. прод.) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 27.07.2010 (86) Заявка PCT: JP 2008/073440 (24.12.2008) (87) Публикация заявки РСТ: WO 2009/084538 (09.07.2009) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры" (54) СУЛЬФЕНАМИД, УСКОРИТЕЛЬ ВУЛКАНИЗАЦИИ КАУЧУКА, СОДЕРЖАЩИЙ СУЛЬФЕНАМИД, И СПОСОБ ПОЛУЧЕНИЯ УСКОРИТЕЛЯ ВУЛКАНИЗАЦИИ (57) Реферат: Изобретение относится к N-алкил-N-третбутилбензотиазол-2-сульфенамиду, представленному формулой [I], где R означает этил, н-пропил или н-бутил. Также изобретение относится к ускорителю ...

Synthetic method for accelerator DZ by using methanol as solvent

本发明公开了一种以甲醇为溶剂生产促进剂DZ的合成方法，以甲醇为溶剂、次氯酸钠为氧化剂、以M-Na盐为原料，其特征是：将24%硫酸50g加入到已有43克二环己胺和200～800ml甲醇的反应器中，在30-60℃、转速为800转/分钟的条件下，使硫酸充分和二环己胺反应，再滴加98g M-Na盐；然后以5ml/分钟的流速加入有效氯为12-18.0/100ml的氧化剂次氯酸钠，同时控制反应溶液的pH8-11，滴加时间为2小时，反应完毕后抽滤、水洗、过滤、干燥得橡胶促进剂DZ产品。促进剂DZ的纯度达到99%以上。该方法过程简单，生产成本低，易于工业化，产品DZ收率高，质量好。

Modulators of indolamine-2,3-dioxygenase

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2018 112 749 A (51) МПК C07D 403/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2018112749, 22.09.2016 (71) Заявитель(и): ГлаксоСмитКлайн Интеллекчуал Проперти (N 2) Лимитед (GB) Приоритет(ы): (30) Конвенционный приоритет: 24.09.2015 US 62/222,880 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 24.04.2018 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2017/051353 (30.03.2017) (54) Модуляторы индоламин-2,3-диоксигеназы (57) Формула изобретения 1. Соединение, имеющее структуру формулы I: A 2 0 1 8 1 1 2 7 4 9 A Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ" или его фармацевтически приемлемая соль, где: X представляет собой W представляет собой CR4; Y представляет собой CR5; V представляет собой CR6; R U 2 0 1 8 1 1 2 7 4 9 IB 2016/055674 (22.09.2016) R U (43) Дата публикации заявки: 24.10.2019 Бюл. № 30 (72) Автор(ы): ЧОН Пек Йок (US), ДЕ ЛА РОЗА Марта (US), ДИКСОН Гамильтон (US), КАЗМЕРСКИЙ Веслав Мечислав (US), САМАНО Висенте (US), ТАЙ Винсент Винг-Фай (US) выбран из группы, состоящей из следующих структур: R1 выбран из группы, состоящей из -СО2Н, тетразол-5-ила, -NHSO2R11 и -CONHSO2R12; R2 выбран из группы, состоящей из -Н, -ОН, -Cl, -F и -ОСН3; Стр.: 1 R3 представляет собой -Н; R4 выбран из группы, состоящей из -Н и -F; R5 выбран из группы, состоящей из -Н и -F; R6 выбран из группы, состоящей из -Н, -F и -Cl; R7 и R8 независимо выбраны из группы, состоящей из следующих структур: R10 выбран из группы, состоящей из следующих структур: 2 0 1 8 1 1 2 7 4 9 2. Соединение или соль по п. 1, где R1 выбран из -СО2Н или тетразол-5-ила. 3. Соединение или соль по п. 1, где R10 выбран из 4. Соединение или соль по п. 1, где R10 представляет собой 5. Соединение или соль по п. 1, где R10 представляет собой 6. Соединение или соль по п. 1, где R10 представляет собой 7. Соединение или его фармацевтически приемлемая соль, выбранные из группы, ...

Indoleamine 2,3-dioxygenase modulator

Novel imaging composition and uses thereof

A kind of technique of sodium hypochlorite synthesis vulcanization accelerator N, N- dicyclohexyl -2-[4-morpholinodithio sulfenamide

本发明是一种次氯酸钠合成硫化促进剂N,N‑二环己基‑2‑苯并噻唑次磺酰胺的工艺，包括的步骤有：(1)二环己胺和盐酸的反应；(2)次氯酸钠氧化反应；(3)DZ生成。本发明所述的一种次氯酸钠合成硫化促进剂N,N‑二环己基‑2‑苯并噻唑次磺酰胺的工艺，过程简单，不需同时滴加三种原料，不需控制反应液的PH值，易于工业化，使用的二环己胺适量，合成出的促进剂DZ的纯度达到98.5％以上。收率达到了95％以上，水相中只有氯化钠单一盐分，可回收利用。

New image forming composition and application thereof

本申请中讨论的发明涉及当与合适的金属中心结合时，特别用于肿瘤成像时用作成像剂的异羟肟酸类化合物。

Process for the manufacture of a sulfenimide

본 발명은 산으로 유기-물이 혼합되지 않는 용매를 갖는 슬러리내 설펜아미드를 반응시켜서 설펜이미드 생성물을 포함하는 용매 슬러리를 수득하는 설펜이미드의 제조방법에 관한 것으로서, The present invention relates to a method for preparing sulfenimide in which a sulfenamide in a slurry having a solvent in which an organic-water is not mixed with an acid is reacted to obtain a solvent slurry containing a sulfenimide product. 상기 생성물이 용매 슬러리로부터 물을 용매 슬러리로 첨가하고, 단일 여과 공정으로 생성물을 분리하는 방법으로 용매 슬러리에서 회수되고, 물이 용매 슬러리로 첨가되고, 용매 및 물의 공비 혼합물이 진공하에서 거의 모든 용매가 생성물에서 분리되고, 생성물이 수성 슬러리의 일부가 될 때까지 증류되며, 선택적으로 물이 용매 슬러리로 첨가되어 생성된 혼합물이 교반되고, 혼합물에서 생성물을 회수하기위해서 단일 여과 공정으로 혼합물을 여과하는 것을 특징으로 한다. The product is recovered from the solvent slurry by adding water from the solvent slurry into the solvent slurry and separating the product in a single filtration process, water is added into the solvent slurry, and the azeotrope of the solvent and water is Separation from the product, distillation until the product is part of the aqueous slurry, optionally water is added to the solvent slurry, the resulting mixture is stirred, and the mixture is filtered in a single filtration process to recover the product from the mixture. It features.

The conditioning agent of indole amine 2,3-dioxygenase

提供了化合物及其药学上可接受的盐，其药物组合物，其制备方法，及其用于预防和/或治疗HIV；包括预防AIDS和一般免疫抑制的进展的方法。

The method of producing thiazolsulfenamides

Synthesis method for producing accelerator N, N-dicyclohexyl-2-benzothiazolyl sulfenamide by taking methanol as solvent

本发明公开了一种以甲醇为溶剂生产促进剂N,N-二环己基-2-苯并噻唑次磺酰胺的合成方法，将熔融的粗M50-80g加入到已有45-72克二环己胺和600ml甲醇的反应器中，在60-100℃范围、转速为800转/分钟的条件下，使粗M充分和二环己胺反应，然后以5ml/分钟的流速加入有效氯为12-18mg/100ml的氧化剂次氯酸钠，同时控制反应溶液的pH8-11，滴加时间为2小时，反应完毕后抽滤、水洗、过滤、干燥得橡胶促进剂DZ产品。促进剂DZ的纯度达到95％以上。该方法过程简单，生产成本低，易于工业化，产品DZ收率高，质量好。

Manufacture of n-arylthiazole-2-sulfenamide

NOVEL N- (ARYLSULFONYL) BETA-AMINOACIDS DERIVATIVES COMPRISING A SUBSTITUTED AMINOMETHYL GROUP, THEIR PREPARATION METHOD AND THE PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME

Rubber vulcanization accelerators

Improved process for manufacturing nu-alkyl and nu-cycloalkylbis (2-benzothiazolesulfene) amides

Benzothiazole sulphinamide vulcanisation - accelerators

Prepn. of benzothiazole - sulphinamides-2 of formula (where R and R' are both isopropyl, both beta-cyanoethyl, or together with N form piperidino or 2', 6' dimethyl morpholino) by oxidn. of the corresponding sulphonamide with Nacl in aqueous alkali pref. sodium (bi) carbonate at less than 30 degrees C. Useful as rubber vulcanisation accelerators.

Manufacturing process of 2-benzthiazylsulfenomorpholide

Patent FR2118544A5

Self-extinguishing resins and processes for their preparation

Method of making PNA oligomers

This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

Novel manufacture of benzothiazylsulfenamide

Method for preparing n, n-diisopropylbenzothiazyl-2-sulfenamide

Process for the preparation of benzothiazolyl sulphenic acid morpholide

PROCESS FOR THE PREPARATION OF BENZOTHIAZOLYL SULPHENIC ACID MORPHOLIDE Abstract of the Disclosure A process for the preparation of 2-benzothiazolyl sulphenic acid morpholide in an aqueous medium wherein the reaction product is separated in the molten state by heating the suspension with melting of the solid reaction product, subsequent rapid separation of the melt phase from the aqueous phase, and removal of volatile constituents still present in the melt phase, the sum of residence times amount-ing to not more than 15 minutes. Le A 18 561

PNA monomer and precursor

This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R′; J is sulfur or oxygen; R′, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural α-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.

METHOD FOR PRODUCING BENZOTHIAZOLYL SULFEN AMIDES

PROCESS FOR MANUFACTURING BIS (BENZOTHIAZYLSULFENE)

2-Thio-morpholino-benzothiazole prodn. - from 2-mercapto-benzothiazole, or corresp. di:sulphide, and excess morpholine, useful vulcanisation accelerator, fungicide and antioxidant

Process for sulfenimides

An improved process for producing N-alkyl or N-cycloalkyl-2-benzothiazole sulfenimides uses aliphatic hydrocarbons as a reaction medium in converting N-alkyl or N-cycloalkyl-2-benzothiazole sulfenamides to the corresponding sulfenimides by reaction with an acid.

Synthetic method for rubber vulcanizing accelerator CZ with sodium hypochlorite as oxidizing agent

本发明提出以次氯酸钠为氧化剂合成橡胶硫化促进剂CZ的方法；按85％～90％促进剂M与环己胺按重量比为1：1.5计，将环己胺加入到氧化釜中，再把质量含量85％～90％促进剂M与异丙醇的重量比为1：1.5的料浆加到含有环己胺氧化釜中，在40-60℃、转速为400-600转/分钟的条件下，向溶液中滴加次氯酸钠溶液，70-120分钟后，取样观察，用淀粉碘化钾试纸判断反应终点，当试纸变黑时，停止滴加次氯酸钠，产品经抽滤、水洗、过滤、干燥得橡胶促进剂CZ产品。该方法过程简单，直接用M为原料，用异丙醇代替水的M打浆，使生产的废水较老工艺减少60％以上，促进剂CZ的纯度达到98％以上。收率达到了95％以上。

Manufacture of nu-alkyl- and nu-cycloalkyl bis (2-benzothiazolesulfen) amides

Preparation of 2-benzothiazolyl sulfene morpholide

2-Benzothiazyl sulphene morpholide is manufactured by treating 2-benzothiazolyl disulphide in an inert organic solvent with at least an equimolecular proportion each of N-chloromorpholine and of morpholine in the presence of an acid acceptor. Preferred solvents are hydrocarbons and halogenated hydrocarbons of the benzene series, whilst the acid acceptor is advantageously an amine, preferably a tertiary amine or excess of morpholine. The N-chloromorpholine may be prepared by chlorinating morpholine in situ in the solvent to be used in the condensation. The acid acceptor may be regenerated for further use by treating it, either in the reaction mixture or after separation and re-slurrying in an anhydrous inert solvent, with ammonia and separating the ammonium chloride formed. When morpholine is used it may be chlorinated before being recycled. In examples (1) 1 mol. of 2-benzothiazolyl disulphide is added to a solution of 1 mol. of N-chloromorpholine and 2 mols. of morpholine in toluene, which is then stirred at 30-45 DEG C., after which the mixture is saturated with anhydrous ammonia, the ammonium chloride formed is filtered off, morpholine is extracted with water and the toluene steam distilled (2) the toluene in (1) is replaced by chlorobenzene and the proportion of morpholine is increased slightly.

Rubber vulcanization process

Selective estrogen receptor modulators

Benzothiazole-2-sulphonyl-ureas and a process for their manufacture

The invention comprises benzthiazole-2-sulphonyl ureas of the formula <FORM:0875584/IV (b)/1> and physiologically tolerable salts thereof with bases, wherein R1 is a saturated or unsaturated aliphatic or cycloaliphatic hydrocarbon radical of 2-8 carbon atoms or a phenylalkyl radical containing 2-4 carbon atoms in the alkyl chain. Suitably R1 is an alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl radical of 2 to 8 carbon atoms, or a phenylalkyl radical, specific examples of the latter being b -phenylethyl, g -phenylpropyl and d -phenylbutyl groups. The compounds are prepared by treating benzothiazole-2-sulphonamide, preferably in the form of its alkalimetal salt, with an isocyanate R1NCO or with a compound which is converted to an isocyanate in the course of the reaction, such as a carbamic acid halide or carboxylic acid azide. The products are used for the oral treatment of diabetes (see Group VI). Examples describe the preparation of N1-butyl-, N1-hexyl-, N1-cyclohexyl-, N1-propyl-, N1-allyl- and N1-(b -phenylethyl)-N-benzothiazole-2-sulphonyl-urea. Specifications 808,071, 808,072, 808,073, 814,234, 815,885 and 822,090 are referred to.ALSO:Preparations for oral administration for lowering the blood sugar level comprise a benzothiazole-2-sulphonylurea of the general formula <FORM:0875584/VI/1> (wherein R1 represents a saturated or unsaturated aliphatic or cycloaliphatic hydrocarbon radical of 2-8 carbon atoms or a phenylalkyl radical with 2-4 carbon atoms in the alkyl chain) or a physiologically acceptable salt thereof with a base, in admixture with a pharmaceutically suitable carrier. Instead of administering a preformed salt, the sulphonylurea may be administered in the presence of a salt-forming substance, e.g. ammonia, an alkali or alkaline-earth metal hydroxide, and alkali metal carbonate or bicarbonate, or an organic base. Specifications 808,071, 808,072, 808,073, 814,234, 815,885 and 822,090.

PNA monomer and precursor

本申请涉及用来制备PNA(肽核酸)寡聚物的通式(I)的单体，并提供了合成预定序列PNA寡聚物和随机序列PNA寡聚物的方法：其中，R’、R1、R2、R3、R4分别为H、卤素、烷基、硝基、腈、烷氧基、卤化的烷基、卤化的烷氧基、苯基或卤化的苯基，RS是H或被保护或未被保护的天然或非天然α-氨基酸侧链；和B是天然或非天然的核酸碱基，其中，当所述核酸碱基具有环外氨基官能团时，所述官能团受保护基保护，所述保护基在酸性条件下不稳定但在硫醇的存在下，在弱碱性至中等碱性条件下稳定。

Patent FR2206761A5

It is a kind of using 2- benzothiazolyl mercaptans and tert-butylamine as the clean synthesis process of Material synthesis vulcanization accelerator TBSI

本发明是一种以2‑硫醇基苯并噻唑和叔丁胺为原料合成硫化促进剂TBSI的清洁合成工艺，包括如下步骤：(1)中间产物的水溶液的生成；(2)制作MBT浆液；(3)TBSI的合成。本发明所述的一种以2‑硫醇基苯并噻唑和叔丁胺为原料合成硫化促进剂TBSI的清洁合成工艺，反应整体收率可高到90％以上，产物TBSI经HPLC测试纯度可高达97％；在提高原料转化率和产物收率的同时，降低三废产生量，降低生产成本，提高工艺的产业化可行性。

Catalytic oxidation process

Catalytic oxidation of thiol or thiol salts or dithiocarbamic acids or their salts using oxygen, optionally in the presence of a primary or secondary amine, is accomplished with a carbon catalyst which contains no metal complex of porphyrazine or of a derivative of porphyrazine.

Process for producing benzothiazolyl-2-sulphenamides

Process for the preparation of benzothiazolyl-2-sulphen-amides Akzo nv, Arnhem Abstract: The process for the preparation of benzothia-zolyl-2-sulphenamides, by reacting a 2-mercaptobenzo-thiazole or dibenzothiazolyl 2,2'-disulphide with a primary or secondary aliphatic or cycloaliphatic amine in the presence of hydrogen peroxide as oxidizing agent in an aqueous medium is distinguished in that an aqueous hydrogen peroxide solution is metered at a temperature in the range from 30 to 70°C into an aqueous suspension of the respective amine and the 2-mercaptobenzothiazole or dibenzothiazolyl 2,2'-disulphide in a ratio in the range between 1.0 and 1.5 mol of amine per mole of 2-mercapto-benzothiazole or per equivalent of dibenzothiazolyl 2,2'-disulphide, preferably in a quantity of below 1.35 mol per mole of 2-mercaptobenzothiazole or per equivalent of dibenzothiazolyl 2,2'-disulphide over a period of at least 60 minutes. The total quantity of water in the reaction mixture should not exceed 1500 g per mole of 2-mercaptobenzothiazole. An environmentally friendly and economic process is provided for the preparation of benzothiazolyl-2-sulphenamides in high yield and with high selectivity.

Improvements relating to the preparation of substituted heterocyclic sulfonamides and their intermediates

Improvements in or relating to the reaction of organic mercaptans with formaldehyde and ammonia

A product containing more than one molecular proportion of formaldehyde and less than one molecular proportion of ammonia combined with each molecular proportion of mercaptothiazole is prepared by heating 3 mols. of a mercaptothiazole with at least 5 mols. of formaldehyde and about 1 mol. of ammonia in aqueous medium. The product probably has the formula: (RS)3C6H10O2N, where R is a thiazyl radical, e.g. 4-methyl or 4-ethyl thiazyl, or dihydrothiazyl, and is preferably arylene thiazyl, e.g. naphthothiazyl, or 6-nitro-, 5-chloro-, 4-methyl- or 4-phenyl benzothiazyl. In the above cases the 2-mercapto derivative is used in the reaction. In an example, mercaptobenzothiazole (1.2 mols.) and 37 per cent formaldehyde (2 mols.) in suspension in aqueous sodium carbonate (just alkaline) are heated with ammonium hydroxide (0.46 mols.) at about 90 DEG C. to give a product C27H22O2N4S6. The Specification as open to inspection under Sect. 91 states that the group R may be any organic group, and specifies butyl, amyl, lauryl, phenyl and b -naphthyl. This subject-matter does not appear in the Specification as accepted.ALSO:The product obtained by heating 3 mols. of a mercaptothiazole with at least five mols. of formaldehyde and about 1 mol. of aqueous ammonia (see Group IV (b)), and which contains more than one molecular proportion of formaldehyde and less than one molecular proportion of ammonia combined with each molecular proportion of the thiazole, is used to accelerate the vulcanization of rubber and to treat tyre cord to improve the adhesion. The product probably has the formula (RS)3C6H10O2N, where R is thiazyl, and preferably arylene thiazyl, e.g. benzothiazyl or chloro- and methyl-benzothiazyl. The Specification as open to inspection under Sect. 91 states that R may be any organic group, e.g. butyl, lauryl, phenyl, and naphthyl. This subject-matter does not appear in the Specification as accepted.

Synthetic method for rubber vulcanization accelerator NS by solvent method

本发明公开了一种溶剂法生产橡胶硫化促进剂NS的方法，其特征是按甲醇与叔丁胺的体积比为0.6～0.8：1的混合液加入到氧化釜中，在30-60℃、转速为800转/分钟的条件下，以2ml/分钟的流速，加入质量比1:1促进剂M：甲醇的料浆；同时以1ml/分钟的流速，向溶液中滴加质量含量为12-18％的次氯酸钠溶液，90分钟后，取样观察，用淀粉碘化钾试纸判断反应终点，当试纸变黑时，停止滴加氯酸钠，开始蒸馏回收甲醇；产品经抽滤、水洗、过滤、干燥得橡胶促进剂NS产品。该方法过程简单，用甲醇代替水，使生产的废水较老工艺减少80%以上。本工艺易于工业化，使用的叔丁胺少，促进剂NS的收率达到99%以上。

Process for the preparation of sulfenamides of mercaptoarylene thiazoles

Carbamoyloxy derivatives of mutiline and their use as antibacterials

Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Stabilized benzothiazolesulfenamide composition and method of preparing the same

Process for the preparation of Benzthiazolyl-2-sulfen- (2 ', 6'-dimethylmorpholiden)

Compounds and compositions for treating conditions associated with NLRP activity

在一个方面，具有式AA的化合物或其药学上可接受的盐的特征在于：式AA或其药学上可接受的盐，其中式A中示出的变量可以如本文中任何地方所定义。

Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same

Spoj formule: naznačen time, da: - R1 predstavlja fenilvinilnu skupinu; fenilnu skupinu, nesupstituiranu ili supstituiranu jednom ili više puta s R6 koji mogu biti identični ili različiti; naftilnu skupinu, nesupstituiranu ili supstituiranu jednom ili više puta s R6 koji mogu biti identični ili različiti; tetrahidronaftilnu skupinu, nafto[2,3-d][1,3]dioksol-6-il skupinu, heterociklički radikal odabran između kinolil, izokinolil, 1-benzofur-2-il, 2,1,3-benzoksadiazol-4-il, 2,1,3-benzotiadiazol-4-il, 1,3-benzotiazol-2-il, 1-benzotiofen-2-il, 1H-pirazol-4-il, tien-2-il, 5-izoksazoltien-2-il, benzotien-2-il, tieno[2,3-c]pirid-2-il; navedeni heterociklički radikali mogu biti nesupstituirani ili supstiturani jednom ili više puta s R6 koji mogu biti identični ili različiti; - R2 predstavlja vodik ili (C1-C4) alkilnu skupinu i R3 predstavlja fenilnu skupinu, nesupstituiranu ili supstituiranu jednom ili više puta s R7 koji mogu biti identični ili različiti; heterociklički radikal odabran između benzo[1,3]dioksol-5-il, koji može biti supstituiran na poziciji 2 s dva atoma fluora; 2,1,3-benzotiadiazol-5-il, 2,3-dihidrobenzo[1,4]dioksin-6-il, 1-benzofur-2-il; 1-benzofur-5-il; benzofuril, furil i tien-2-il; tien-3-il; - ili alternativno R2 predstavlja fenilnu skupinu, nesupstituiranu ili supstituiranu jednom ili više puta s R6 koji mogu biti identični ili različiti; heterociklički radikal odabran između benzo[1,3]dioksol-5-il, piridil i indanil, i R3 predstavlja vodik; - R4 predstavlja skupinu -CONR8R9; skupinu -CSNR8R9; skupinu -COR13; fenilnu skupinu, nesupstituiranu ili supstituiranu jednom ili više puta s R10; heterociklički radikal odabran između piridil, imidazolil, furil, benzimidazolil, benzotiazol-2-il i benzo[1,3]dioksol-5-il, navedeni heterociklički radikali mogu biti nesupstituirani ili supstiturani jednom ili više puta s metilnom skupinom ili atomom halogena- R5 predstavlja skupinu -CH2NR11R12 ili -CH2N(O)NR11R12;- R6 predstavlja atom halogena; (C1-C4) alkilnu ...

Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure.

Novel carboxylic acid esters of 5-hydroxy-2-benzothiazolesulfonamide are shown to be useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions including drops and inserts are also disclosed, as well as methods for preparing the novel compounds.

Production of nu-alkyl- and nu-cycloalkyl-bis- (2-benzothiazolesulfene) amides

Triphenylethylene Derivatives as Selective Estrogen Receptor Modulators and Pharmaceutical Compositions Containing Them

Patent SU402221A3

Carbamoyloxy derivatives of methiline and their use as antimicrobial agents

본 발명은 하기 화학식 (1A)의 화합물 또는 약제학적으로 허용되는 염, 및 이들의 유도체의 머틸린의 유도체에 관한 것이며, 이들은 박테리아 감염 치료에 유용하다. (화학식 1A) 상기 식에서, R은 에틸 또는 비닐이며, Y는 N-원자가 비치환되거나, 일치환 또는 이치환된 카르바모일옥시기이다.

Catalytic Oxidation Process

선택적으로 1차 혹은 2차아민의 존재하에서, 포르피라진 혹은 포르피라진 유도체의 금속착물을 포함하지 않는 탄소촉매와 함께 산소를 이용하여, 티올 혹은 티올의 염 혹은 디티오카르빔산 혹은 그의 염에 대한 촉매산하를 실행하였다.

METHOD FOR PRODUCING BIS-BENZTHIAZOLYL-ALKYL-SULFENIMIDES

Method for synthesizing rubber vulcanization accelerator CZ

本发明公开了一种合成橡胶硫化促进剂CZ方法，以双氧水、硫酸混合为氧化剂、以M-Na盐，环己胺为原料，其特征是按摩尔比硫酸∶双氧水∶水为1∶2.05～2.3∶7，配氧化剂；按环己胺∶M-Na盐摩尔比为1∶1；往反应釜中投加环己胺、在30～60℃、转速为600～1200转/分钟的条件下，以1.5～2.5毫摩尔/分钟的流速滴加M-Na盐，同时滴加氧化剂，氧化剂滴加速度和量以氧化剂中硫酸摩尔数∶M-Na盐摩尔数比为1∶2滴加0.15摩尔，滴加时间为2～3小时，反应完毕后抽滤、水洗、过滤、干燥得橡胶促进剂CZ产品。促进剂CZ的纯度达到98.5%，收率达到了97%，该方法过程简单，且易于工业化生产。

METHOD FOR PRODUCING BENZOTHIAZOLE SULFEN AMIDES

Production method of N-cyclohexyl-2-benzothiazole sulfenamide

本发明公开了N‑环己基‑2‑苯并噻唑次磺酰胺生产制备技术领域的一种N‑环己基‑2‑苯并噻唑次磺酰胺的生产方法，包括以下步骤：一：在氧化罐加入浓度为15~17%的环己胺，搅拌环己胺溶液并加入2‑硫醇基苯并噻唑形成混合液，环己胺与2‑硫醇基苯并噻唑的胺比为2.3；二：对混合液充分搅拌，然后冷却至35℃，再向混合液中缓慢滴加浓度为5%的次氯酸钠溶液形成反应液，直到有N‑环己基‑2‑苯并噻唑次磺酰胺生成，反应液中2‑硫醇基苯并噻唑黄色颗粒消失为止；三：搅拌氧化后的反应液并倒入吸滤槽中过滤，滤出的N‑环己基‑2‑苯并噻唑次磺酰胺用热水洗至中性，然后离心甩干并使用热风吹干制得成品。本方案通过优化生产工艺，提高了目标物的生成率并减少了反应物的浪费。

Derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing same

The invention relates to compounds of formula: These compounds show affinity for the bradykinin receptors with selectivity towards the B 1 receptors; they may be used for the preparation of medicinal products intended for treating or preventing inflammation pathologies and persistent or chronic inflammatory diseases.

N-(arylsulphonyl)beta-amino acid derivatives comprising a substituted aminomethyl group, process for preparing them and pharmaceutical compositions containing them

The invention relates to compounds having formula (I). Said compounds have an affinity for bradykinin receptors with a selectivity for B1 receptors and they can be used to prepare medicaments that are intended to treat or prevent persistent or chronic inflammatory diseases and inflammation pathologies.

Unsymmetrical dialkyl thiazole sulfenamides

Patent FR2076855A5

METHOD FOR THE CATALYTIC OXYDATION OF THIOLES

Process for the preparation of benzothiazolesulfenamides.

A process for the preparation of benzothiazole-sulfenamides in which a benzothiazyl disulfide is reacted with a mixture comprising an amine halogenhydrate and an N-halogen amine derivative.

A kind of method of Co catalysts oxygen method synthesis N cyclohexyl 2 benzothiazole sulfenamide

本发明公开了硫化促进剂N‑环己基‑2‑苯并噻唑次磺酰胺的制备方法，该种方法将2‑巯基苯并噻唑、环己胺、钴催化剂置于高压反应釜中，以水为溶剂进行反应，反应完毕后，过滤、洗涤、干燥，得到N‑环己基‑2‑苯并噻唑次磺酰胺。本发明方法具有原料易得方法简单，催化效率高，溶剂环保，得到的产品纯度高，后处理简单等特点。

Process for the preparation of N, N-diisopropylbenzthiazolyl-2-sulfenamide

Use of derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group in the preparation of medicaments for the treatment of pain or inflammation

Process of production of N-alkyl-2-benzthiazolylsulfeneimides and method of their purification

Spôsob výroby N-alkyl-2-benztiazolylsulfénimidov vzorca (I) reakciou 2-benztiazolylsulfenylchloridus nadbytkom príslušného alkylamínu v bezvodom reakčnom médiu. Odstránenie vody a vlhkosti z reakčného prostredia sa zabezpečuje azeotropickou destiláciou časti rozpúšťadla. Spôsob rieši aj zachytávanie nadbytočného amínu extrakciou vodou na jeho opätovné využitie v procese, odstránenie neskonvertovanej suroviny zo surového produktu chemickou rafináciou vodným roztokom lúhu a extrakciu vedľajších produktov a smôl rozplavením produktu v organickomrozpúšťadle s cieľom získať čistý benztiazolylsulfénimid s obsahom účinnej látky nie nižším ako 95 %, použiteľný ako urýchľovač vulkanizácie v gumárskych zmesiach.

Imaging composition and uses thereof

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

Topically active ocular benzothiazole sulfonamide carbonic anhydrase inhibitors

This invention is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof wherein R6 is hydrogen or lower alkyl; each R1 is hydrogen, lower alkyl, halogen, nitro, trihaloalkyl, lower alkoxy, formyl, lower alkanoyl, loweralkylamino or diloweralkylamino; Y is (II) or (III); X is O, S or NR5; R2 is OR7 or NR7R8; each R3 and R4 are independently hydrogen or lower alkyl; R5, R7 and R8 are independently hydrogen or lower alkyl; n is 0-3 and m is 0-6. These compounds are useful for treating glaucoma or assessing corneal function in mammals.

Novel derivatives of n-(arylsulfonyl)beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and pharmaceutical compositions containing same

A találmány az (I) általános képletű vegyületekre vonatkozik, aképletben R1 jelentése fenilvinilcsoport, adott esetben helyettesítettfenil-, naftil-, tetrahidronaftil- vagy heterociklusos csoport; R2jelentése hidrogénatom vagy alkilcsoport, és R3 jelentése adott esetben helyettesített fenil- vagyheterociklusos csoport; vagy R2 jelentése adott esetben helyettesítettfenil- vagy heterociklusos csoport, és R3 jelentése hidrogénatom; R4jelentése adott esetben helyettesített karbamoil- vagytiokarbamoilcsoport, fenilkarbonil-, tiazolkarbonil- vagypiridilkarbonilcsoport; R5 jelentése adott esetben helyettesítettaminometilcsoport. A vegyületek a bradikinin receptorok iránt mutatnakaffinitást és a B1 receptorok vonatkozásában szelektívek; olyangyógyszertermékek előállítására használhatók, amelyek gyulladásospatológiák és tartós vagy krónikus gyulladásos betegségek kezelésérevagy megelőzésére alkalmasak. A találmány tárgya továbbá az (I)általános képletű vegyületek előállítására vonatkozó eljárás, valamintannak intermedierjei. Ó The present invention relates to compounds of formula I wherein R1 is phenylvinyl, optionally substituted phenyl, naphthyl, tetrahydronaphthyl or heterocyclic; R 2 is hydrogen or alkyl, and R 3 is optionally substituted phenyl or heterocyclic; or R2 is optionally substituted phenyl or heterocycle, and R3 is hydrogen; R4 is optionally substituted carbamoyl or thiocarbamoyl, phenylcarbonyl, thiazolecarbonyl or pyridylcarbonyl; R5 is optionally substituted aminomethyl. The compounds show affinity for bradykinin receptors and are selective for B1 receptors; for use in the manufacture of pharmaceutical products useful in the treatment or prevention of inflammatory pathologies and chronic or chronic inflammatory diseases. The present invention also relates to a process for the preparation of compounds of formula I and intermediates thereof. HE

Sulfenamide, Vulcanization Accelerator Containing the Sulfenamide for Rubber, and Process for Producing the Same

술펜아미드 가황촉진제는 발암성의 가황 반응을 천천히 일어나게 함으로써 발암성의 니트로소아민을 생성하지 않으며 생물농축과 같은 환경 위생 문제에 대해서 자유롭다. 식 [Ⅰ]로 표현된 N-알킬-N-t-부틸벤조티아졸-2-술펜아미드를 포함하는 고무용 가황촉진제와 이러한 가황촉진제 제조 방법에 관한 발명을 제공한다. [화학식 1] 상기 R기는 메틸, 에틸, n-프로필 또는 n-부틸을 나타낸다. Sulfenamide vulcanization accelerators do not produce carcinogenic nitrosoamines by slowly causing carcinogenic vulcanization reactions and are free for environmental hygiene problems such as bioconcentration. Provided are a vulcanization accelerator for rubber comprising N-alkyl-Nt-butylbenzothiazole-2-sulfenamide represented by formula [I] and a method for producing such a vulcanization accelerator. [Formula 1] The R group represents methyl, ethyl, n-propyl or n-butyl.

Vulcanizable rubber composition and method of vulcanizing rubber

Derivatives of n-(arylsulfonyl) beta-aminoacids comprising a substituted aminomethyl group, the preparation method thereof and the pharmaceutical compositions containing them

The preparation method of accelerator CZ

本发明属于化工合成技术领域，具体涉及一种硫化促进剂CZ的制备方法，打浆成盐、氧化、抽滤水洗、干燥、即得。本发明采用分步氧化法，即反应前期采用氧气氧化，后期采用次氯酸钠氧化的工艺，有效降低次氯酸钠氧化法产生废水的含盐量，具有工艺简单、成本低、对环境污染少等优点，是一条绿色环保的具有工业应用价值的工艺路线。

Self-extinguishing resins containing free radical initiators

An alkenyl aromatic polymer composition containing a halogen flameproofing agent also contains a free radical initiator which is a sulphenamide, a hydrazone, an organic disulphide, an azo compound, a quinone imine, or a -a 1-diphenyl-a -methoxybibenzyl as a flameproofing adjuvant. In the examples 28 different free radical initiators and 10 different halogen flameproofing agents are used. Polymers exemplified are polystyrene, polyvinyl toluene, and copolymers of styrene with a -methyl styrene, acrylonitrile or butadiene. Other polymers specified include polychlorostyrene. The adjuvants are incorporated in the polymer composition by dissolving the ingredients in a common solvent, e.g. methyl chloride, and then rapidly evaporating the solvent to give a foamed structure; by impregnation under pressure of polymer granules with the adjuvants in aqueous emulsion (and optionally with a blowing agent such as n-pentane if a foamable resin is required); or, in the case of those adjuvants that do not generally inhibit polymerization, by polymerization of the alkenyl aromatic monomers in the presence of the adjuvants.

Selective hydroxamic acid based mmp-12 and mmp-13 inhibitors

The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP- 13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).

N-substd.- benzothiazol-2-sulphonamide(s) - used in small amts. as anti-scorch agents for natural and diene rubbers

N-substd. benzothiazol-2-sulphonamides of formula (I) is new. In (I) R is (substd.) benzothiazolyl of formula (II), X is halogen, lower alkyl, lower alkoxy, acetamido or nitro; R1 is H, halogen, (cyclo)alkyl, benzyl, phenyl opt. substd. by halogen, lower alkyl or nitro, naphthyl or R2-5 and R2 is (cyclo)alkyl, benzyl, trichloromethyl, naphthyl or phenyl opt. substd. by halogen, lower alkyl, nitro or carboxy. (I) are anti-scorch agents for natural- and diene rubbers. (I) can be used in small amts. and produces rubbers with good properties. (I) can also be used as stabilisers for rubbers and resins, pharmaceuticals, agricultural chemicals, corrosion inhibitor for metals, an additive for lubricants and their intermediates.

METHOD FOR THE PRODUCTION OF SULFEN AMIDES

Method for producing rubber vulcanization accelerator NS by two-dropping method

本发明公开了两滴法生产橡胶硫化促进剂NS的方法；按质量含量85％～90％M与叔丁胺的重量比为1：1.5，将叔丁胺加入到氧化釜中，在40-60℃、转速为600转/分钟的条件下，以2ml/分钟的流速，滴加质量比1:1.5促进剂M：异丙醇的料浆，同时以1ml/分钟的流速，向溶液中滴加有效氯为16-18mg/100ml的次氯酸钠溶液，90分钟后，用淀粉碘化钾试纸判断反应终点，当试纸变黑时，停止滴加次氯酸钠，产品经抽滤、水洗、过滤、干燥得橡胶促进剂NS产品。该方法过程简单，省去了M提纯工序和用异丙醇代替水，使生产废水较老工艺减少60％以上，合成出的促进剂NS的纯度达到98％以上。收率达到了95％以上。

Compounds and compositions for treating conditions associated with nlrp activity

In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: Formula AA or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein.

PROCESS FOR THE PREPARATION OF N-CYCLOHEXYLBENZOTHIAZOLE-2-SULFENAMIDE

PROCEDE DE PREPARATION DE N-CYCLOHEXYLBENZOTHIAZOLE-2-SULFENAMIDE. LE PROCEDE CONSTITE A FAIRE TOUT D'ABORD REAGIR LE 2-MERCAPTOBENZOTHIAZOLE SUR UN EXCES DE CYCLOHEXYLAMINE ET A OXYDER ENSUITE LA SOLUTION DE SEL DE CYCLOHEXYLAMINE AU MOYEN DE L'OXYDANT, PAR EXEMPLE DU TYPE DE L'HYPOCHLORITE DE SODIUM. ON ELIMINE PAR FILTRATION LES SOUS-PRODUITS DE L'OXYDATION. ON PEUT UTILISER LE 2-MERCAPTOBENZOTHIAZOLE SOUS LA FORME DU PRODUIT BRUT FORME PAR LA REACTION A HAUTE PRESSION DE L'ANILINE, DU DISULFURE DE CARBONE ET DU SOUFRE.

Derivatives of N-(arylsulfonyl)-beta-amino acids comprising a aminomethyl group, preparation method thereof, pharmaceutical compositions containing same and the use of them

The invention relates to compounds having formula (I), witch have an affinity for bradykinin receptors with a selectivity for B1 receptors and they can be used to prepare medicaments that are intended to treat or prevent persistent or chronic inflammatory diseases and inflammation pathologies.

Topically active ocular benzothiazole sulfonamide carbonic anhydrase inhibitors

This invention is directed to compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R 6 is hydrogen or lower alkyl; each R 1 is hydrogen, lower alkyl, halogen, nitro, trihaloalkyl, lower alkoxy, formyl, lower alkanoyl, loweralkylamino or diloweralkylamino ##STR2## X is O, S or NR 5 ; R 2 is OR 7 or NR 7 R 8 ; each R 3 and R 4 are independently hydrogen or lower alkyl; R 5 R 7 and R 8 are independently hydrogen or lower alkyl; n is 0-3 and m is 0-6. These compounds are useful for treating glaucoma or assessing corneal function in mammals.