АРИЛПИПЕРАЗИНОВЫЕ ПРОИЗВОДНЫЕ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ И СПОСОБЫ ЛЕЧЕНИЯ

Изобретение относится к новым арилпиперазиновым производным общей формулы I и их фармацевтически приемлемым солям, сложным эфирам, где Y представляет О; Q представляет СН; X, Z и Z' каждый независимо представляют СН или N; m=0-1; n=0-4; R1 и R2 независимо выбирают из Н, F, Cl, Br, OCH3, OC2H5, OCH2CF3, СН3, С2Н5, СF3, изопропилокси; R3 представляет Н; R4 и R5 представляют Н или фенил, за исключением того, что R1 представляет Н, R2 представляет Н, Cl или CF3, R3, R4 и R5=Н, Y=0, и Q=CH, если m=0 и n=1; и также за исключением того, что R1 представляет Н, R2 представляет OCH3, R3, R4 и R5=H, Y=0, Q=CH, если m=0 и n=2. Изобретение также относится к способам получения этих соединений, фармацевтической композиции на их основе, обладающей уроселективной антогонистической активностью в отношении к α1-адренорецепторам, и способам лечения доброкачественной гипертрофии предстательной железы, сосудистых заболеваний, застойной сердечной недостаточности и гипертензии. Технический результат - получение ...

ПРОИЗВОДНОЕ БЕНЗОЛА, ЗАМЕЩЕННОЕ 1,2-ДИ(ЦИКЛИЧЕСКОЙ ГРУППОЙ)

Изобретение относится к новым соединениям, представленным следующей общей формулой (1), или к их солям: ! ! где R10 представляет собой циклогексил, необязательно замещенный заместителем, выбранным из группы А1, или циклогексенил, необязательно замещенный заместителем, выбранным из группы А1, R30, R31 и R32 представляют собой водород, R40 представляет собой С1-10алкил, необязательно замещенный заместителем, выбранным из группы D1, n равно целому числу 0 или 1, X1 представляет собой азот, и R20, R21, R22 и R23 независимо представляют собой водород, за исключением случая, когда R20, R21, R22 и R23 все представляют собой водород, С1-6 алкилтио, необязательно замещенный заместителем, выбранным из группы F1, C2-7 алкоксикарбонил, C1-6 алкил, замещенный заместителем, выбранным из группы W1, C1-6 алкил, замещенный заместителем, выбранным из группы К1, C1-6 алкокси, замещенный заместителем, выбранным из группы W1, 5-6-членную гетероциклическую группу, которая представляет собой неароматическое насыщенное ...

ФЕНИЛЭТИЛ- И ФЕНИЛПРОПИЛАМИНОВЫЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЙ ПРЕПАРАТ

Описываются новые соединения формулы I, которые будут полезными при лечении психитрических нарушений, например шизофрении и других психозов, патологического страха, депрессии и маниакально-депрессивных психозов, в которой Z представляет собой насыщенную или ненасыщенную цепь с 3-6 атомами углерода, m является числом 2 или 3, R 1 представляет собой атом водорода или С 1 -C 4 -алкил нормального или разветвленного строения, R 2 , R 3 и R 13 находятся в орто-, мета- или параположении фенильного кольца, являются одинаковыми или разными и выбраны из следующих групп: Н, ОН, OR 14 , галогена, CO 2 R 9 , СN, СF 3 , NO 2 , СОСH 3 , OSO 2 CF 3 , OSO 2 СН 3 , CONR 10 R 11 , OCOR 12 , где R 9 , R 12 и R 14 представляют собой C 1 -C 4 -алкил нормального или разветвленного строения, R 10 и R 11 , одинаковые или разные, представляют собой водород или C 1 -C 6 -алкил нормального или разветвленного строения, в которой R представляет собой группу формулы Ia, в которой R 4 и R 5 являются одинаковыми или разными, и когда они разные, то представляют собой атом водорода, С 1 -C 5 -алкил нормального или разветвленного строения или замещенный или незамещенный циклоалкил, и когда они одинаковые, то представляют собой С 1 -C 5 -алкил нормального или разветвленного строения или R 4 и R 5 вместе образуют группу где n 1 является числом 3-7, или формулы II, в которой R 6 представляет собой атом водорода или C 1 -C 6 -алкил нормального или разветвленного строения, R 7 представляет собой замещенный или незамещенный циклоалкил или R 6 и R 7 вместе образуют группу , где n 2 является числом 3-6, или формулы III, в которой W представляет собой необязательно замещенное карбоциклическое кольцо (или кольца) или необязательно замещенную метиленовую группу, и R 8 представляет собой C 1 -C 5 -алкил нормального или разветвленного строения или фенил, n 3 является числом 0-2, или формулы IV, в которой W представляет собой необязательно замещенное карбоциклическое кольцо (кольца) или необязательно замещенную ...

PHENYLETHYL-UND PHENYLPROPYLAMINE

(N)-Haloalkyl nitrogen-contg. heterocyclics prodn. - by reacting (N)-heterocyclics e.g. barbiturates with bis-haloalkyl sulphates, e.g. bis-chloroethyl sulphate

In a new process for the prond. of N-haloalkylated N-contg. heterocyclic cpds. (esp. bis(haloalkyl)-barbiturates), an alkali metal salt of an N-contg. heterocyclic cpd. is reacted with a bis(haloalkyl) sulphate. Of the prods. obtainable by this process, the following are claimed as new cpds: N,N'-bis(chloroethyl)phenobarbital; N,N'-bis(chloroethyl)pentobarbital; N,N'-bis(chloroethyl)amylobarbital; N-chloroethyl-ethosuximide; N-chloroethylglutethimide; N-chloroethyl-diphenylhydantoin; and N,N -bis(chloroethyl)-diphenylhydantoin. N,N'-bis(ahlomethyl) derivs. of the hypnotic/anticonvulsant phenobarbital have only anticonvulsant activity without hypnotic effects. The specifically claimed new cpds. are all derived from known anticonvulsant agents. In an example, a mixture of 0.35 g phenobarbital, 1.5g K2CO3, 15ml absolute EtOH and 1.6 ml bis(chloroethyl) sulphate is refluxed 1 hr., then worked up to give 0.22 g (39%) N,N'-bis(chlorethyl)phenobarbital.

DERIVATE VON BENZHYDRYLOXYAETHYLPIPERAZINEN, VERFAHREN ZU IHRER HERSTELLUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE ZUSAMMENSETZUNGEN.

Compositions and methods

Active Sulphonamides

... 1,161,062. Sulphonamides. ED. GEISTLICH SOHNE AG. FUR CHEMISCHE INDUSTRIE. 2 Sept., 1966 [19 Oct., 1965], No. 44246/65. Heading C2C. Novel sulphonamides of Formula I in which R represents an aryl or araliphatic group substituted in the aromatic ring by at least one sulphonamido group, the nitrogen atom of which may be joined to a further ring substituent, and R1, R2, R3 and R4, which may be the same or different, are hydrogen atoms or C 1-5 alkyl groups, at least one of R1, R2, R3 and R4 being other than hydrogen, and their salts with bases, are prepared by reacting a compound of formula RNH 2 with a succinic acid derivative of formula HOOC-CR1R2-CR3R4-COOH or a reactive derivative thereof, and, if necessary, cyclizing the intermediate hemisuccinyl compound of Formula II (or its isomer in which the hemisuccinyl group is attached to the carbonyl group adjacent to R3 and R< ...

Iodinated Carboxyacylamino-Benzoic Acids

... 1,191,016. Iodinated carboxyacylaminobenzoic acids; 5-substituted-3-amino-and-nitrobenzoic acids. STERLING DRUG Inc. 11 May, 1967 [17 May, 1966], No. 57399/68. Divided out of 1,191,015. Heading C2C. The invention comprises compounds of the general formula wherein Y1 is an alkylene bridge having from two to eight carbon atoms or such a group interrupted by from one to three non-adjacent oxygen or sulphur atoms; R is H, H 2 N, (lower alkanoyl)- NH, (lower alkanoyl)N(lower alkyl), (lower alkanoyl)N(hydroxy-lower alkyl), (lower alkoxylower alkanoyl)NH, (lower alkoxy-lower alkanoyl)N(lower alkyl), HOOC, (lower alkyl)- NHCO, HOOC-Y1-CO-NH, lower alkyl. OOC-Y1-CO-NH, HOOC-Y1-CO-N- (lower alkyl) or HOOC-Y1-CON(hydroxylower alkyl); R1 is hydrogen, lower alkyl, or hydroxy-lower alkyl, and R11 is hydrogen or lower alkyl, " lower alkyl " and " lower alkoxy " are groups containing from 1 to 4 carbon atoms and " lower alkanoyl" is a group ...

Maleimide and succinimide derivatives and preparation and use thereof

Maleimide and succinimide derivatives and preparation and use thereof, said derivatives having the general formulae and wherein R, R1, R2 and R3 are each hydrogen or various substituents. The compounds may be made by acylation of the corresponding derivative unsubstituted on nitrogen. They may be formulated into herbicidal compositions and used as pre- and post-emergence herbicides. The compounds can also be used as chemical intermediates.

PYRROLIDINE-2, 5-DIONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE AS IDO1 INHIBITORS

PYRROLIDINE-2, 5-DIONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE AS IDO1 INHIBITORS

Derived from benzhydryloxyéthyl-piperazine, processes of obtaining and pharmaceutical compositions the container.

PYRROLIDINE-2, 5-DIONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE AS IDO1 INHIBITORS

3,4-DISUBSTITUIERTE ACYLANILIDDERIVATE AND THEIR USE AS ANDROGEN RECEPTOR SUPPRESSOREN

Process for the preparation of 3-substituted enantiomerically pure succinimides

The present patent relates to a process for the preparation of enantiomerically pure 3-mono- or disubstituted succinimides of the general formula I, characterized in that an enantiomerically pure (S)- pyroglutamic acid of the general formula II which is mono- or disubstituted in position 4 is oxidatively decarboxylated and converted in another oxidation step into the target compound. Variation of the radicals R1 and R2 in the mono- or disubstitution of the (S)-pyroglutamic acid which is temporarily reduced to the alcohol and provided with an acetal protective group controlling the alkylation thus permits targeted preparation of enantiomerically pure potential antiepileptics of the succinimide type used therapeutically. Starting from (R)-pyroglutamic acid, it is possible by an analogous reaction sequence to obtain the respective antipodes. ...

COPOLYMERISIERBARE METHINUND ANTHRACHINONVERBINDUNGEN AND ARTICLE THEREBY

UNTIL MARK AMINE ACID, UNTIL MARK A IMIDE AND HARDENED PRODUCT OF IT

TITANOCENE, THEIR USE AND N-SUBSTITUTING FLUORANILINE.

OPTICALLY PURE ONES 4-AMINO-3-HYDROXY-CARBONSAEUREDERIVATE AND PROCEDURE FOR the STEREOSPEZIFI PRODUCTION.

Micro-biological procedure for the production of a new, insecticide effective substance

Procedure for the production of new Succinimidderivate and their salts

PROCEDURE AND REAGENT FUR N-ALKYLATING UREIDES

Compositions for the treatment of pulmonary fibrosis

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

Copolymerizable methine and anthraquinone compounds and articles containing them

This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methine compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.

1-ALKYLPIPERAZINYL-PYRROLIDIN-2, 5-DIONE DERIVATIVES AS ADRENERGIC RECEPTOR ANTAGONIST

Low shrinkage thermosetting resin compositions and methods of use therefor

PLANT GROWTH REGULATING AND HERBICIDAL CYCLOALKANE CARBOXYLIC ACID DERIVATIVES

Reverse hydroxamate inhibitors of matrix metalloproteinases

PLANT GROWTH REGULATING AND HERBICIDAL CYCLOALKANE CARBOXYLIC ACID DERIVATIVES

Succinimide derivatives which inhibit retinoic acid metabolism

Synthesis of bisindolylmalimides

COPOLYMERIZABLE METHINE AND ANTHRAQUINONE COMPOUNDS AND ARTICLES CONTAINING THEM

2,6-DIETHYL-4-METHYL-PHENYL-SUBSTITUTED TETRAMIC ACID DERIVATIVES

The invention relates to the novel 2,6-diethyl-4-methyl-phenyl-substituted tetramic acid derivatives of formula (I), wherein A, B, D and G are defined as above. The invention also relates to several methods and intermediate products for producing said derivatives and to their use as pesticides and/or herbicides, and to selectively herbicidal agents which comprise the 2,6- diethyl-4-methyl-phenyl-substituted tetramic acid derivatives of formula (I) and at least one compound that improves crop safety.

METAL SALT/AMINE COMPLEXES

COMPOSITIONS FOR THE TREATMENT OF FIBROSIS AND FIBROSIS-RELATED CONDITIONS

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of fibrosis and fibrosis-related conditions, the compounds having the formula:

ALKENYLSUCCINIMIDE IN LIQUID HYDROCARBON FUEL

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

A compound of formula (I) is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

N-HYDROXYFORMAMIDE DERIVATIVES AS INHIBITORS OF MATRIX METALLOPROTEINASES

Compounds having formula (I) are matrix metalloproteinase inhibitors. Also disclosed are matrix metalloproteinase-inhibiting compositions and methods of inhibiting matrix metalloproteinase in a mammal.

Procédé de préparation d'une succinimide substituée.

Verfahren zur Darstellung heterocyclischer Verbindungen

Verfahren zur Herstellung von Sulfonamiden

Procédé de préparation de triiodo-anilides

Anticonvulsant and diuretic sulphonamido phenylalkyl-succinimides

A. alpha-Alkyl succinimide sulphamido derivs. of general formula (I):- - R = an aryl- or araliphatic group substd. in the aromatic ring with at least one sulphonamide group, the N-atom of which may be connected to form another cyclic substituent. Preferred group: - R = - R1, R2, R3 and R4 are same or different and: H, or 1-5C alkyl; at least one of R1-4 is not H - R5 = one or more halogen atoms, aliphatic hydrocarbon, etherhydroxy or acylamino groups - R6 and R7 are same or different and: H, heterocyclic groups such as pyridyl, pyrimidyl or imidazolyl groups, or aliphatic hydrocarbon groups possible substd. with oxo, hydroxyl, carboxyl or esterified carboxyl, amino or alkylamino groups. R6 and R7 together with the N atom may form a heterocyclic group such as piperidyl or piperazinyl - R5 may also be a carboxyl group or form together with NR6R7 a -CO -NH -SO2 chain. - B. Pharmaceutically acceptable salts of A with bases such as alkali metal, ammonia or amine salts. - The new cpds. have very ...

Antielektrostatische Polyamidformteile

Verfahren zur Herstellung von neuen Succinimidoderivaten

Procédé de préparation de nouveaux dérivés du N-phénylsuccinimide, et leur utilisation dans une composition microbicide

Mikrobizides Präparat und Verwendung desselben

VERFAHREN ZUR HERSTELLUNG VON NEUEN SUCCINIMIDODERIVATEN.

Verfahren zur Herstellung des Antibiotikums MM. 4086

PROCEDURE FOR THE PRODUCTION OF METAL SALT AMINE COMPLEXES.

MARK A IMIDE AND SUKZINIMID DERIVATIVES, PROCEDURES FOR THE PRODUCTION THE SAME AS WELL AS HERBICIDES CONTAINING THESE DERIVATIVES.

DERIVATIVES OF PYRROLIDINE - 2, 5 - DIONE, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USING AS INHIBITORS OF IDO1

ПРОИЗВОДНЫЕ 2,6-ДИЭТИЛ-4-МЕТИЛФЕНИЛЗАМЕЩЕННОЙ ТЕТРАМОВОЙ КИСЛОТЫ

Изобретение относится к новым производным 2,6-диэтил-4-метилфенилзамещенной тетрамовой кислоты формулы (I) где А, В, D и G имеют значения, приведенные в описании, к нескольким способам их получения и к промежуточным продуктам, необходимым для их получения, а также к их применению в качестве средств для борьбы с вредителями и/или гербицидов, а также селективные гербицидные средства, которые содержат производные 2,6-диэтил-4-метилфенилзамещенной тетрамовой кислоты формулы (I), с одной стороны, и, как минимум, одно соединение, улучшающее переносимость гербицидов культурными растениями, с другой стороны.

СПОСОБ ПОЛУЧЕНИЯ 2,6-ДИЭТИЛ-4-МЕТИЛФЕНИЛУКСУСНОЙ КИСЛОТЫ

Описывается способ получения 2,6-диэтил-4-метилфенилуксусной кислоты формулы (I) который заключается в том, что 2,6-диэтил-2-метилбромбензола формулы (II) подвергают взаимодействию с трет-бутилацеатом при необходимости в присутствии основания, фосфинового лиганда, палладиевого соединения и разбавителя с последующим взаимодействием с кислотой или же 2,6-диэтил-4-метилфенилмалондинитрил формулы (III) подвергают взаимодействию с кислотой при необходимости в присутствии разбавителя. 2,6-Диэтил-4-метилфенилуксусную кислоту в виде галоидангидрида применяют в качестве реагента для получения гербицидно активных производных 2,6-диэтил-4- метилфенилзамещенной тетрамовой кислоты.

METHOD OF OBTAINING THE DIESTERS

MANUFACTORING PROCESS OF COMPOSE INCLUDING/UNDERSTANDING FUNCTIONS NITRILES

CHEMICAL COMPOUNDS AND PREPARATION THEREOF

SALT COMPLEXES OF METALS AND AMINES USABLE FOR the EPOXY RESIN HARDENING

HERBICIDE COMPOSITION

COMPOSITIONS FOR THE TREATMENT OF PULMONARY FIBROSIS

METHODS AND COMPOSITIONS FOR THE TARGET-LOCALIZED ANCHORING OF DETECTABLE LABEL

Highly reactive functionalized substrates and linker molecules for use in the detection of molecular targets and other analytes of interest are provided as are kits, reaction mixtures and methods utilizing the same.

METHOD FOR PRODUCING PYRROLIDONES FROM SUCCINATES FROM FERMENTATION BROTHS

The invention relates to a method for producing a compound (II) or a composition containing the compound (II), a composition containing succinimide, and a composition which is produced according to said inventive method.

METHOD AND REAGENTS FOR N-ALKYLATING UREIDES

A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure (I) with an alkylating agent of structure (III) in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N'-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

Ethylenically unsaturated imidazidolidinone monomers

Classes of urea functional compounds and compositions containing the same are disclosed which are particularly suitable for use as a wet adhesion promoters in coatings, especially in aqueous emulsion systems used to make latex paints. Compositions containing the same, as well as additional uses thereof are also disclosed.

Retroviral protease inhibiting compounds

A compound of the formula: см. иллюстрацию в PDF-документе is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Method for inhibiting differentiation of osteoclast and pharmaceutical composition comprising thereof

The present invention is for method of treating metabolic bone disease, new compounds and pharmaceutical compositions comprising the active ingredients having inhibition effects on osteoclast differentiation. The pharmaceutical composition comprising new compounds according to the present invention can be used as medicines for treating metabolic bone diseases such as bone metastatic cancer, solid cancer bone metastasis, musculoskeletal complication by solid cancer bone metastasis, hypercalcemia by malignant tumor, multiple myeloma, primary bone tumor, osteoporosis, rheumatoid arthritis, osteoarthritis, periodontal disease, inflammatory resorption of alveolar bone, inflammatory resorption of bone, and Paget's disease.

Retroviral protease inhibiting compounds

A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.

ЧЕТВЕРТИЧНЫЕ АММОНИЕВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ДОБАВОК К ТОПЛИВУ ИЛИ СМАЗОЧНЫМ МАТЕРИАЛАМ

FIELD: chemistry. SUBSTANCE: invention relates to an improved method of producing a diesel fuel composition. Method comprises producing quaternary ammonium compound by reaction (a) a tertiary amine of formula R 1 R 2 R 3 N, with (b) epoxide selected from styrene oxide, ethylene oxide, propylene oxide, butylene oxide, epoxy hexane, octene oxide, stilbene oxide, other oxides of alkyls and alkenyls containing from 2 to 50 carbon atoms, glycidyl ethers and glycidyl ethers, in the presence of (c) a monoacid or a mono-ester of a diacid, comprising a hydrocarbyl moiety containing at least 6 carbon atoms; and mixing quaternary ammonium compound with diesel fuel. In tertiary amine R 1 R 2 R 3 N each of R 1 , R 2 and R 3 is independently selected from an alkyl or hydroxyalkyl group containing 1 to 10 carbon atoms; or R 1 is an alkyl group containing 1 to 10 carbon atoms; R 2 represents an alkyl group containing 1 to 10 carbon atoms, and R 3 is a succinimide fragment having formula , where R is a hydrocarbyl group containing 6 to 400 carbon atoms, and L is ethylene, propylene or butylene. Preferably, quaternary ammonium compound has formula where R 1 , R 2 and R 3 are as defined above; R 4 , R 5 , R 6 and R 7 are determined based on epoxide, as defined above; and R includes an alkyl or alkenyl moiety containing at least 6 carbon atoms, and where RCOO - is a residue of said monoacid or a monoether of diacid. Method may involve addition of one or more additional detergents into the diesel composition. Invention also relates to a method of improving operational characteristics of a diesel engine. Proposed method comprises production of diesel fuel composition by said method and combustion of said diesel fuel composition in engine. Diesel engine has a fuel injection system which includes a high pressure fuel injection (HPFI) system in which fuel pressure exceeds 1350 bar (1.35⋅10 8 Pa). Improvement of operational characteristics occurs as a result of counteraction to deposits in ...

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7 ВУ“” 2017135950"” АЗ Дата публикации: 16.08.2019 Форма № 18 ИЗ,ПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2017135950/04(06269Т) 18.03.2016 РСТ/АЧ2016/000095 18.03.2016 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 2015900979 18.03.2015 АО Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) Композиции для лечения фиброза и связанных с фиброзом состояний Заявитель: ВЕКТУС БАЙОСИСТЕМС ЛИМИТЕД, АЧ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. П см. Примечания [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 39/15 (2006.01) С07О 207/408 (2006.01) Аб1К 31/165 (2006.01) С07С 47/575 (2006.01) С07О 207/448 (2006.01) Аб/1К 31/192 (2006.01) С07С 65/03 (2006.01) С07О 209/48 (2006.01) Аб1К 31/381 (2006.01) С07С 211/29 (2006.01) (070 233/78 (2006.01) Аб/1К 31/42 (2006.01) С07С 217/48 (2006.01) (070 261/14 (2006.01) Аб1Р 1/12 (2006.01) С07О 207/267 (2006.01) (070 263/42 (2006.01) Аб1Р 9/10 (2006.01) С07О 207/36 (2006.01) (070 263/44 (2006.01) Аб1Р 13/12 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С ...

2-АЛКОКСИ-6-АЛКИЛФЕНИЛЗАМЕЩЕННЫЕ СПИРОЦИКЛИЧЕСКИЕ ПРОИЗВОДНЫЕ ТЕТРАМОВОЙ КИСЛОТЫ

... 1. Соединения формулы (I),в которой X означает алкокси,Y означает алкил иZ означает алкил с 2-6 атомами углерода,А означает водород, соответственно при необходимости замещенный галогеном алкил, алкенил, алкоксиалкил, алкилтиоалкил, насыщенный или ненасыщенный, при необходимости замещенный циклоалкил, в котором по меньшей мере один кольцевой атом при необходимости замещен гетероатомом, или соответственно при необходимости замещенный галогеном, алкилом, галогеналкилом, алкокси, галогеналкокси, циано или нитро арил, арилалкил или гетарил,В означает водород, алкил или алкоксиалкил, илиА и В совместно с атомом углерода, к которому они присоединены, означают насыщенное или ненасыщенное, при необходимости содержащее по меньшей мере один гетероатом кольцо с 4-8 атомами углерода, которое при необходимости замещено алкилом, алкокси или галогеналкилом,D означает водород или при необходимости замещенный остаток, выбранный из ряда, включающего алкил, алкенил, алкинил, алкоксиалкил, алкилтиоалкил, насыщенный ...

Способ получения производных малеинимида и сукцинимида

Maleimide and succinimide derivatives and preparation and use thereof, said derivatives having the general formulae <IMAGE> and <IMAGE> wherein R, R1, R2 and R3 are each hydrogen or various substituents. The compounds may be made by acylation of the corresponding derivative unsubstituted on nitrogen. They may be formulated into herbicidal compositions and used as pre- and post-emergence herbicides. The compounds can also be used as chemical intermediates.

N-GESCHÜTZTE/N-SUBSTITUIERTE BETA-AMINOHYDROXYSULFONATE

Verfahren zur Herstellung eines substituierten Bernsteinsaeureimids

Methyl alpha-(Methylsuccinimido) Acrylate

... 1,187,070. Insecticides. BEECHAM GROUP Ltd. 7 Oct., 1968 [14 Oct., 1967], No. 46945/ 67. Heading A5E. [Also in Division C2] Methyl -(methylsuccinimido) acrylate of formula: [Division C2] is a contact insecticide against flies, moths and beetles. It may be used as a vapour, in solution e.g. in acetone or dimethylsulphoxide or in admixture with flour. It may also be used for moth-proofing wool.

PROCESS FOR ISOLATION OF ORGANIC COMPOUNDS AND LITHIUM SALT COMPLEXES USEFUL IN SUCH PROCESS

Iodinated Imido-Benzoic Acids

... 1,191,015. Iodophenyl imides; N-(3-carboxy- 5-nitro and amino-phenyl)-imides. STERLING DRUG Inc. 11 May, 1967 [17 May, 1966], No. 21897/67. Heading C2C. The invention comprises compounds of the general formula wherein Y is a lower alkylene group having from 2 to 6 carbon atoms such that 2 or 3 carbon atoms separate the carbonyl groups, or a 1,3-propylene group having from 2 to 4-carbon atoms wherein the 2-carbon atom is replaced by O, S, SO or SO 2 ; R is H, H 2 N, (lower alkanoyl)NH, (lower alkanoyl)N(lower alkyl), (lower alkoxy-lower alkanoyl)NH, (lower alkoxy-lower alkanoyl)N(lower alkyl), HOOC, (lower alkyl) NHCO, or HOOC-Y-CO-N-(lower alkyl) wherein Y is as defined above, and wherein "lower alkyl" and "lower alkoxy" are groups containing from 1 to 4 carbon atoms and "lower alkanyol" is a group containing from 1 to 6 carbon atoms, and the pharmaceutically acceptable salts thereof. The compounds may be prepared by the following methods: (a) when R is other than -NH 2 , (lower alkanoyl ...

N-GESCHÜTZTE/N-SUBSTITUTING BETA AMINOHYDROXYSULFONATE

Procedure for the production of new Succinimidderivate and their salts

Anti-electrostatic formed things from synthetic PP

TOPISCH ANTI-ANDROGEN FOR HAIR LOSS AND OTHER HYPERCANDROGENS OF CONDITIONS

VERFAHREN ZUR HERSTELLUNG 3-SUBSTITUIERTER ENANTIOMERENREINER SUCCINIMIDE

VERFAHREN ZUR HERSTELLUNG VON NEUEN, GESAETTIGTEN UND PARTIELL GESAETTIGTEN N-ACRYL-PYRROL-2,5-DION -DERIVATEN

DERIVATIVES OF BENZHYDRYLOXYAETHYLPIPERAZINEN, PROCEDURES FOR YOUR PRODUCTION AND THESE CONTAINING PHARMACEUTICAL COMPOSITIONS.

CONNECTIONS THE RETROVIRALE PROTEASE RESTRAINING

Procedure for the production of new N-Methyl-α-methyl-α-phenyl-β-äthylsuccinimids

Fluorinated melt additives for thermoplastic polymers

N-LALOALKYLATED N-CONTAINING HETEROCYCLES

Fluorinated melt additives for thermoplastic polymers

RETROVIRAL PROTEASE INHIBITING COMPOUNDS

The compound of formula I or a pharmaceutically acceptable salt, ester or prodrug thereof, in combination with a reverse transcriptase inhibitor or a combination of such inhibitors, or a combination of such compound with another HIV protease inhibitor, or combination of such inhibitors, is useful in treating HIV infection.

DIPHENYL ETHER AMIDES AND S-METHYL-N-(4-)4'-CHLOROPHENOXY) PHENYL) THIOLCARBAMATE

Compounds having the formula in which X is chloro or methyl; n is zero, one or two: Y is chloro or trifluormethyl; R1 is hydrogen, alkyl, lower alkoxy, lower haloalkyl, thio-lower alkyl, or alkenyl: R2 is hydrogen, lower alkoxy-alkyl or lower alkenoyl; or R1 and R2 taken together is or in which Y is hydrogen, n is o, R1 is thiomethyl and R2 is hydrogen. The compounds are useful as post-emergence herbicides, particularly as post-emergence, post-flooding herbicides, for use in connection with rice cultivation.

N-(3,5-DIHALOPHENYL)-IMIDE COMPOUNDS

PROCESS FOR THE PREPARATION OF DIESTERS

La présente invention concerne un procédé de fabrication de diesters à partir de composés imides ou dinitriles. Elle se rapporte plus particulièrement à un procédé de fabrication de composés diesters à partir de composés dinitriles mettant en AEuvre une hydrolyse en phase vapeur de composés dinitriles en présence d'alcool pour obtenir des composés diesters. Elle concerne encore plus particulièrement un procédé de fabrication de diesters à partir de composés dinitriles ramifiés tels que le méthylglutaronitrile ou les composés dinitriles ramifiés obtenus comme sous produits dans le procédé de fabrication de l'adiponitrile par hydrocyanation du butadiène.

METHOD AND REAGENTS FOR N-ALKYLATING UREIDES

A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure (I) with an alkylating agent of structure (III) in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be hydride or amine. A preferred process comprises Nalkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N'-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

СПОСОБ ПОЛУЧЕНИЯ 2,6-ДИЭТИЛ-4-МЕТИЛФЕНИЛУКСУСНОЙ КИСЛОТЫ

Описывается способ получения 2,6-диэтил-4-метилфенилуксусной кислоты формулы (I) который заключается в том, что 2,6-диэтил-2-метилбромбензола формулы (II) подвергают взаимодействию с трет-бутилацеатом, при необходимости в присутствии основания, фосфинового лиганда, палладиевого соединения и разбавителя, с последующим взаимодействием с кислотой или же 2,6-диэтил-4-метилфенилмалондинитрил формулы (III) подвергают взаимодействию с кислотой, при необходимости в присутствии разбавителя. 2,6-Диэтил-4-метилфенилуксусную кислоту в виде галоидангидрида применяют в качестве реагента для получения гербицидно активных производных 2,6-диэтил-4-метилфенилзамещенной тетрамовой кислоты.

PROCESS FOR PRODUCING COMPOUNDS COMPRISING NITRILE FUNCTIONS

The production of compounds comprising nitrile functions and of cyclic imide compounds is described. Further described, is the production of compounds comprising nitrile functions from compounds comprising carboxylic functions, optionally of natural and renewable origin, and from a mixture N of dinitriles comprising 2-methylglutaronitrile (MGN), 2-ethylsuccinonitrile (ESN) and adiponitrile (AdN). 1. A process for preparing at least one nitrile of general formula I{'br': None, 'sub': v', '1', 'w, '(NC)—R—(CN)\u2003\u2003(I)'} {'br': None, 'sub': x', '1', 'y, '(HOOC)—R—(COOH)\u2003\u2003(II)'}, 'and at least cyclic imides 3-methylglutarimide and 3-ethylsuccinimide, by reacting at least one carboxylic acid of general formula II'}and a mixture N of dinitriles comprising 2-methylglutaronitrile (MGN), 2-ethylsuccinonitrile (ESN) and adiponitrile (AdN),whereinx, y are equal to 0 or 1 with (x+y) equal to 1 or 2,v, w are equal to 0 or 1 with (v+w) equal to 1 or 2, and from 4 carbon atoms to 34 carbon atoms when (x+y) is equal to 2, and', 'from 2 carbon atoms to 22 carbon atoms when (x+y) is equal to 1., 'R1 represents a linear or branched, saturated or unsaturated hydrocarbon-based group which can comprise heteroatoms, comprising2. The process as defined in claim 1 , wherein the mixture N of dinitriles is a mixture resulting from the process for producing adiponitrile by double hydrocyanation of butadiene.3. The process as defined in claim 1 , wherein the mixture N of dinitriles has the following composition by weight:2-Methylglutaronitrile from 70% to 95%,2-Ethylsuccinonitrile from 5% to 30%, andAdiponitrile from 0% to 10%, andwherein the remaining portion of the composition is composed of various impurities.4. The process as defined in claim 1 , wherein the compound of formula II is derived from a renewable matter of vegetable or animal origin.5. The process as defined in claim 4 , wherein the compound of formula II is selected from the group consisting of a caproic acid ...

DIARYLAMINE-BASED COMPOUND, ANTI-AGING AGENT, AND POLYMER COMPOSITION

The present invention provides a diarylamine-based compound represented by General Formula (1): 5. The diarylamine-based compound according to claim 1 , wherein Aand Aare a 1 claim 1 ,4-phenylene group.8. The composition according to claim 7 , wherein Rand Reach independently represent a linear or branched Cto Calkyl group which may have a substituent claim 7 , or a phenyl group which may have a substituent.10. The composition according to claim 1 , wherein a weight ratio of the diarylamine-based compound to the condensed heterocyclic compound is 30:1 to 1:30 as “diarylamine-based compound:condensed heterocyclic compound”.11. An antioxidant comprising the diarylamine-based compound according to claim 1 , or the composition according to any one of to .12. The antioxidant according to claim 11 , wherein the antioxidant is an antioxidant for a polymer.13. A polymer composition comprising a polymer and the antioxidant according to .14. The polymer composition according to claim 13 , wherein the polymer is a synthetic resin.15. The polymer composition according to claim 13 , wherein the polymer is a rubber.16. The polymer composition according to claim 15 , wherein the rubber is an acrylic rubber.17. The polymer composition according to claim 13 , wherein a content of the antioxidant is 0.05 to 30 parts by weight relative to 100 parts by weight of the polymer.18. An antioxidant comprising the composition according to . The disclosure relates to a novel diarylamine-based compound which has an excellent antioxidant effect on polymer materials required to have high heat resistance (for example, heat resistance in a high temperature range of 190° C. or more) and can be suitably used as an antioxidant, and an antioxidant and a polymer composition comprising such a diarylamine-based compound.With development of petrochemistry, polymers composed of organic compounds have contributed to human development in a variety of forms such as plastics, rubber, fibers, and films. Because ...

SYNTHESIS OF THERAPEUTIC AND DIAGNOSTIC DRUGS CENTERED ON REGIOSELECTIVE AND STEREOSELECTIVE RING OPENING OF AZIRIDINIUM IONS

Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds. 2. The method of claim 1 , further comprising:converting a substituted β amino alcohol to a substituted alkylating agent;converting the substituted alkylating agent to the substituted aziridinium ion; andstereoselectively or regioselectively reacting the aziridinium ion with a nucleophile to obtain the compound.4. The method of claim 2 , further comprising:{'sub': 4', '2', '3', '3', '6', '4, 'converting the substituted alkylating agent to the aziridinium ion in the presence of halosequestering agent comprising AgClO, AgOTf, AgCO, AgOTs, AgNO, AgSbF, or AgBF; and'}stereoselectively or regioselectively reacting the aziridinium ion in situ with a nucleophile to obtain the compound.6. The method of claim 5 , further comprising:{'sub': 4', '2', '3', '3', '6', '4, 'converting the substituted alkylating agent to the aziridinium ion in the presence of halosequestering agent comprising AgClO, AgOTf, AgCO, AgOTs, AgNO, AgSbF, or AgBF; and'}stereoselectively or regioselectively reacting the aziridinium ion in situ with the nucleophile in the presence of a base to obtain the compound.7. The method of claim 5 , further comprising:converting a substituted β amino alcohol to a substituted alkylating agent;converting the substituted alkylating agent to the substituted aziridinium ion; andstereoselectively or regioselectively reacting the aziridinium ion with a nucleophile to obtain the compound, wherein the reaction occurs without isolation of any intermediate compound.9. The method of claim 8 , further comprising removing a protecting group comprising an amino claim 8 , a carboxyl claim 8 , or a hydroxyl protecting group from the compound using a deprotection reaction.10. The method of claim 9 , further comprising converting a nitro group in the compound to an amino ...

Prodrugs of fumarates and their use in treating various diseases

The present invention provides compounds of formula (I), wherein: R 1 is unsubstituted C 1 -C 6 alkyl; L a is substituted or unsubstituted C 1 -C 6 alkyl linker, substituted or unsubstituted C 3 -C 10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R 2 and R 3 are each, independently, H, substituted or unsubstituted C 1 -C 6 alkyl, or substituted or unsubstituted C 6 -C 10 aryl; or alternatively, R 2 and R 3 , together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

Prodrugs of Fumarates and Their Use in Treating Various Diseases

The present invention provides compounds of formula (I), 2. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt thereof.3. A method of treating multiple sclerosis in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of the compound of .4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 16/221,884, filed Dec. 17, 2018, which is a continuation of U.S. application Ser. No. 15/683,189, filed Aug. 22, 2017, now U.S. Pat. No. 10,189,855, issued Jan. 29, 2019, which is a divisional of U.S. application Ser. No. 14/744,325, filed Jun. 19, 2015, now abandoned, which is a continuation of U.S. application Ser. No. 14/180,687, filed Feb. 14, 2014, now U.S. Pat. No. 9,090,558, issued Jul. 28, 2015, which claims the benefit of U.S. Provisional Application No. 61/782,445, filed on Mar. 14, 2013. The entire teachings of the above applications are incorporated herein by reference.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or inflammatory processes including psoriasis (Joshi and Strebel, WO 1999/ ...

Diesel Detergent Without A Low Molecular Weight Penalty

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 1. A composition comprising a quaternary ammonium salt , wherein the quaternary ammonium salt comprises the reaction product of: (i) at least one tertiary amino group, and', '(ii) a hydrocarbyl-substituent derived from a hydrocarbon having a number average molecular weight of from about 100 to about 500;, 'a) a compound comprising a non-quaternized amide and/or ester detergent havingb) a quaternizing agent suitable for converting the tertiary amino group of compound (a) to a quaternary nitrogen.2. The composition of claim wherein 1 component b) , the quaternizing agent suitable for converting the tertiary amino group of compound a) to a quaternary nitrogen , comprises:(a) dialkyl sulfates;(b) benzyl halides;(c) hydrocarbyl substituted carbonates;(d) hydrocarbyl epoxides;(e) esters of carboxylic acids and/or polycarboxylic acids;(f) any combination thereof;wherein the quaternizing agent may optionally be used in combination with an acid.3. A diesel fuel comprising the composition of .4. The diesel fuel of claim 3 , wherein the diesel fuel is ultra-low sulfur diesel fuel.5. The diesel fuel of claim 3 , wherein the quaternary ammonium salt is present from about 10 to about 500 ppm.6. A method of minimizing creation of internal diesel injector deposits while additionally reducing the level of pre-existing internal diesel injector deposits comprising the step of supplying to a diesel engine a diesel fuel composition comprising (A) diesel fuel; and (B) a composition according to .7. The method of wherein the diesel engine comprises common rail diesel injectors. This application is a continuation application of U.S. application Ser. No. 14/434,985 which claims priority to PCT Application Serial No. PCT/US2013/ ...

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

The present invention provides compounds of formula (I), 2. The compound of claim 1 , wherein Ris methyl.3. The compound according to claim 1 , wherein Lis substituted or unsubstituted C-Calkyl linker.4. The compound according to claim 1 , wherein Ris substituted or unsubstituted C-Calkyl and Ris H.5. The compound according to claim 1 , wherein Rand R claim 1 , together with the nitrogen atom to which they are attached claim 1 , form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N claim 1 , O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N claim 1 , O and S.10. A method of treating a neurological disease by administering to a subject in need thereof a therapeutically effective amount of a compound according to or a pharmaceutically acceptable salt claim 1 , polymorph claim 1 , hydrate claim 1 , solvate or co-crystal thereof.11. The method of claim 10 , wherein the neurological disease is multiple sclerosis.12. The method of claim 10 , wherein the neurological disease is relapsing-remitting multiple sclerosis.13. The method of claim 1 , wherein the compound of formula (I) is a pharmaceutically acceptable salt.14. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) a therapeutically effective amount of a compound of ;'}and(ii) a pharmaceutically acceptable carrier or excipient.15. The composition of claim 14 , wherein the therapeutically effective amount is sufficient for the treatment of multiple sclerosis.16. (canceled) This application is a continuation of U.S. application Ser. No. 14/180,687, filed Feb. 14, 2014 which claims the benefit of U.S. Provisional Application No. 61/782,445, filed on Mar. 14, 2013. The entire teachings of the above applications are incorporated herein by reference.The present invention relates to various prodrugs of monomethyl fumarate. In ...

Quaternary ammonium compounds as fuel or lubricant additives

A quaternary ammonium compound which is the reaction product of: (a) a tertiary amine having a molecular weight of less than 1000; (b) an acid-activated alkylating agent; and (c) a diacid including an optionally substituted hydrocarbyl moiety having at least (5) carbon atoms.

QUATERNARY AMMONIUM COMPOUNDS AS FUEL OR LUBRICANT ADDITIVES

A quaternary ammonium compound of formula (X), wherein R, R, Rand Ris each individually an optionally substituted alkyl, alkenyl or aryl group and R includes an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms. 2. A quaternary ammonium compound which is the reaction product of:(a) a tertiary amine;(b) an acid-activated alkylating agent; and(c) an acid including an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms.3. A quaternary ammonium compound according to wherein component (b) is an epoxide.4. A quaternary ammonium compound according to wherein component (c) is selected from a monoacid claim 2 , diacid claim 2 , monoester of a diacid claim 2 , a polyacid or a partial ester of a polyacid.5. A quaternary ammonium compound according to wherein component (c) is selected from a monoacid claim 4 , diacid or a monoester of a diacid.7. A quaternary ammonium compound according to wherein component (c) is a monoester of a diacid.10. A method of preparing a quaternary ammonium salt claim 6 , the method comprising reacting (a) a tertiary amine with (b) an acid-derived alkylating agent in the presence of (c) acid including an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms.11. An additive composition comprising one or more quaternary ammonium compounds as claimed in and a diluent or carrier.12. A lubricating composition comprising as an additive one or more quaternary ammonium compounds as claimed in .13. A fuel composition comprising as an additive one or more quaternary ammonium compounds as claimed in .14. A fuel composition according to wherein the fuel is diesel fuel.15. A fuel composition according to which comprises one or more further detergents selected from:(i) an additional quaternary ammonium salt additive which is not one of the one or more quaternary ammonium compounds;(ii) the product of a Mannich reaction between an aldehyde, an amine and an optionally substituted phenol;(iii) the ...

FUNCTIONALIZED POLYMERS CONTAINING POLYAMINE SUCCINIMIDE FOR ANTIFOULING IN HYDROCARBON REFINING PROCESSES

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon. 2. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises polypropylene.3. The compound of claim 2 , wherein the polypropylene is selected from the group consisting of atactic polypropylene claim 2 , isotactic polypropylene claim 2 , syndiotactic polypropylene claim 2 , amorphous polypropylene claim 2 , polypropylene including isotactic crystallizable units claim 2 , polypropylene including syndiotactic crystallizable units claim 2 , and polypropylene including meso diads constituting from about 30% to about 99.5% of the total diads of the polypropylene.4. The compound of claim 2 , wherein at least one of R claim 2 , R claim 2 , and Rhas a number-averaged molecular weight of from about 300 to about 30000 g/mol.5. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises polyethylene.6. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises poly(ethylene-co-propylene).7. The compound of claim 6 , wherein at least one of R claim 6 , R claim 6 , and Rcomprises from about 1 mole % to about 90 mole % of ethylene units and from about 99 mole % to about 10 mole % propylene units.8. The compound of claim 7 , wherein at least one of R claim 7 , R claim 7 , and Rcomprises from about 10 mole % to about 50 mole % of ethylene units.9. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises poly(higher alpha-olefin) claim 1 , the higher alpha-olefin including two or more carbon atoms on each side chain.10. The compound of claim 1 , wherein at least one of R claim 1 , R claim 1 , and Rcomprises polypropylene-co-higher alpha- ...

Prodrugs of fumarates and their use in treating various diseases

The present invention provides compounds of formula (I), wherein: R 1 is unsubstituted C 1 -C 6 alkyl; L a is substituted or unsubstituted C 1 -C 6 alkyl linker, substituted or unsubstituted C 3 -C 10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R 2 and R 3 are each, independently, H, substituted or unsubstituted C 1 -C 6 alkyl, or substituted or unsubstituted C 6 -C 10 aryl; or alternatively, R 2 and R 3 , together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

CYCLOALKANE CARBOXYLIC ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS

The present invention relates to compounds of formula 1 3. A compound according to claim 1 , wherein R represents hydrogen.7. A compound according to claim 1 , wherein X represents —O—CH— claim 1 , —S—CH— or —CH—CH—.8. A compound according to claim 1 , wherein Y represents hydrogen claim 1 , Cl claim 1 , F claim 1 , methyl claim 1 , ethyl claim 1 , methoxy or —CH—OH.9. A compound according to claim 8 , wherein Y represents ethyl or methoxy.11. A compound according to claim 10 , wherein Z represents —(CH)— or —CH—N(CH)—.13. A compound according to selected from the group consisting oftrans-4-[([1-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid ethyl ester;trans-4-[([1-(2,3-Dihydro-1-benzofuran-5-yl)ethyl]{4-[2-(2,5-dioxo-pyrrolidin-1-yl)ethoxy]-3-methoxybenzyl}amino)methyl]-cyclohexanecarboxylic acid;cis-4-[([1-(2,3-Dihydro-1-benzofuran-5-yl)ethyl]{4-[2-(2,5-dioxo-pyrrolidin-1-yl)ethoxy]-3-methoxybenzyl}amino)methyl]-cyclohexanecarboxylic acid;trans-4-[([(R)-1-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(S)-1-(2,3-Dihydro-benzofuran-5-yl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(S)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]cyclohexanecarboxylic acid;trans-4-[([(R)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methoxy-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(S)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methyl-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;cis-4-[([(S)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin-1-yl)-ethoxy]-3-methyl-benzyl}-amino)-methyl]-cyclohexanecarboxylic acid;trans-4-[([(R)-1-(4-Chloro-phenyl)-ethyl]-{4-[2-(2,5-dioxo-pyrrolidin ...

TREATMENT METHOD UTILIZING PYRROLIDINE-2, 5-DIONE DERIVATIVES AS IDO1 INHIBITORS

Uses of compound of Formula I: 2. The method according to claim 1 , wherein the brain cancer is selected from glioblastomas and medulloblastomas; the intraepithelial neoplasms is selected from Bowen's disease and Paget's disease; the oral cancer is squamous cell carcinoma; the ovarian cancer is selected from those arising from epithelial cells claim 1 , stromal cells claim 1 , germ cells and mesenchymal cells; the renal cancer is selected from adenocarcinoma and Wilms tumor; the sarcomas is selected from leiomyosarcoma claim 1 , rhabdomyosarcoma claim 1 , liposarcoma claim 1 , fibrosarcoma and osteosarcoma; the skin cancer is selected from melanoma claim 1 , Kaposi's sarcoma claim 1 , basocellular cancer and squamous cell cancer; the testicular cancer is selected from germinal tumors seminomas claim 1 , and non-seminomas selected from teratomas and choriocarcinomas; and the thyroid cancer is selected from thyroid adenocarcinoma and medullary carcinoma.3. The method according to claim 1 , wherein the lymphoid disorders are selected from acute lymphocytic leukemia and chronic lymphoproliferative disorders.4. The method according to claim 3 , wherein the chronic lymphoproliferative disorders are selected from lymphomas claim 3 , myelomas and chronic lymphoid leukemias.5. The method according to claim 4 , wherein the lymphomas are selected from Hodgkin's disease claim 4 , non-Hodgkin's lymphoma lymphomas claim 4 , and lymphocytic lymphomas; and the chronic lymphoid leukemias are selected from T cell chronic lymphoid leukemias and B cell chronic lymphoid leukemias.6. The method according to claim 1 , wherein Qrepresents H and X represents —NH—.7. The method according to claim 1 , wherein Rand Reach independently represent H or halo.8. The method according to claim 7 , wherein the halo is F.10. The method according to claim 9 , wherein the method comprises delivering approximately equal molar amounts of the compound of Formula I′ and the compound of Formula I″.11. The ...

FUMARATE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE

Fumarate compounds, pharmaceutical compositions comprising the fumarate compounds, and methods of using fumarate compounds and pharmaceutical compositions for treating neurodegenerative, inflammatory, and autoimmune disorders including multiple sclerosis, psoriasis, irritable bowel disorder, ulcerative colitis, arthritis, chronic obstructive pulmonary disease, asthma, Parkinson's disease, Huntington's disease, and amyotrophic lateral sclerosis are disclosed. 2. The compound according to claim 1 , wherein Ris chosen from hydrogen claim 1 , methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n-butyl claim 1 , tert-butyl claim 1 , phenyl claim 1 , benzyl claim 1 , (1 claim 1 ,3-dioxoisoindolin-2-yl) claim 1 , (2 claim 1 ,5-dioxopyrrolidin-1-yl) claim 1 , (2 claim 1 ,5-dioxopyrrol-1-yl) claim 1 , indol-1-yl claim 1 , morpholin-4-yl claim 1 , 1 claim 1 ,3-oxazinan-3-yl claim 1 , oxazolidin-3-yl claim 1 , (1-oxoisoindolin-2-yl) claim 1 , (2-oxomorpholin-4-yl) claim 1 , (4-oxo-1-piperidyl) claim 1 , (2-oxopyrrolidin-1-yl) claim 1 , (3-oxopyrrolidin-1-yl) claim 1 , 1-piperidyl claim 1 , tetrazol-1-yl claim 1 , triazol-1-yl claim 1 , 1 claim 1 ,2 claim 1 ,4-triazol-4-yl claim 1 , 1-benzoyloxyethyl claim 1 , benzoyloxymethyl claim 1 , (1 claim 1 ,3-dimethyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (1 claim 1 ,3-dimethyl-2-oxo-imidazolidin-4-yl) claim 1 , (2 claim 1 ,5-dioxoimidazolidin-4-yl) claim 1 , (2 claim 1 ,5-dioxopyrrolidin-3-yl) claim 1 , (1-methyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (3-methyl-2 claim 1 ,5-dioxo-imidazolidin-4-yl) claim 1 , (1-methyl-2 claim 1 ,5-dioxo-pyrrolidin-3-yl) claim 1 , (5-methyl-2-oxo-1 claim 1 ,3-dioxol-4-yl)methyl claim 1 , (3-methyl-2-oxo-oxazolidin-4-yl) claim 1 , (3-methyl-2-oxo-oxazolidin-5-yl) claim 1 , (1-methyl-2-oxo-pyrrolidin-3-yl) claim 1 , (1-methyl-5-oxo-pyrrolidin-2-yl) claim 1 , (1-methyl-5-oxo-pyrrolidin-3-yl) claim 1 , 1-(2-methylpropanoyloxy)ethyl claim 1 , 2-methylpropanoyloxymethyl ...

DIESEL DETERGENT WITHOUT A LOW MOLECULAR WEIGHT PENALTY

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 1. A composition comprising a quaternary ammonium salt , wherein the quaternary ammonium salt comprises the reaction product of: (i) at least one tertiary amino group, and', '(ii) a hydrocarbyl-substituent derived from a hydrocarbon having a number average molecular weight of from about 100 to about 500;, 'a) a compound comprising'}b) a quaternizing agent suitable for converting the tertiary amino group of compound (a) to a quaternary nitrogen.2. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group and at least one hydrocarbyl-substituent claim 1 , comprises:(I) the condensation product of an acylating agent substituted with the hydrocarbyl-substituent of a)ii) and a compound having an oxygen or nitrogen atom capable of condensing the acylating agent wherein the condensation product has at least one tertiary amino group;(II) an amine substituted with the hydrocarbyl-substituent of a)ii), wherein the amine has at least one tertiary amino group and the hydrocarbyl-substituent is a polyalkene-substituent;(III) a compound containing at least one hydrocarbyl-substituent of a)ii) and at least one tertiary amino group, wherein the hydrocarbyl-substituent is a polyester group;(IV) a compound containing at least one hydrocarbyl-substituent of a)ii) and at least one tertiary amino group, wherein the hydrocarbyl-substituent is a polyether group; or(V) any combination thereof.3. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group claim 1 , comprises the condensation product of a hydrocarbyl-substituted acylating agent and a compound having an oxygen or nitrogen atom capable of condensing with said ...

METHODS FOR TREATING LEISHMANIASIS

Methods are provided to inhibit proliferation of parasites, and in particular with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can used to provide prophylaxis or treatment to a patient in need of treatment against leishmaniasis disease. 2Leishmania donovani. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone has in vitro toxicity against greater than Amphotericin B.3. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone has an in vitro selectivity index greater than Amphotericin B.4Leishmania donovani. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone has an ICvalue against promastigotes and amastigotes lower than Amphotericin B.5. (canceled)6. (canceled)9. The method according to claim 1 , wherein each R is aryl claim 1 , halo-substituted aryl claim 1 , aliphatic claim 1 , halo-substituted aliphatic claim 1 , or alkenyl.10. (canceled)11. The method according to claim 1 , wherein Q is an aryl-imido substituent.12. The method according to claim 1 , wherein each R is aryl claim 1 , optionally having halogen substitution.15. The method according to claim 14 , wherein Y is a meta-substitutent.16. The method according to claim 14 , wherein Y is an ortho-substitutent.17. The method according to claim 14 , wherein Y is a para-substitutent.18. The method according to claim 13 , wherein Y is bromo claim 13 , chloro or fluoro.19. The method according to claim 13 , wherein X is chloro.20. The method according to claim 19 , wherein X is chloro and Y is chloro.21. The method according to claim 1 , wherein the imido-substituted 1 claim 1 ,4-naphthoquinone is selected from the group consisting of IMDNQ2 claim 1 , IMDNQ3 and IMDNQ4.22. The method according to claim 7 , wherein R is a C-Calkyl claim 7 , optionally having halogen substitution.23. The method according to claim 22 , wherein ...

DIESEL DETERGENT WITHOUT A LOW MOLECULAR WEIGHT PENALTY

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 1. A composition comprising a quaternary ammonium salt , wherein the quaternary ammonium salt comprises the reaction product of: (i) at least one tertiary amino group, and', '(ii) a hydrocarbyl-substituent derived from a hydrocarbon having a number average molecular weight of from about 100 to about 500;, 'a) a compound comprising'}b) a quaternizing agent suitable for converting the tertiary amino group of compound (a) to a quaternary nitrogen.2. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group and at least one hydrocarbyl-substituent claim 1 , comprises:(I) the condensation product of an acylating agent substituted with the hydrocarbyl-substituent of a)ii) and a compound having an oxygen or nitrogen atom capable of condensing the acylating agent wherein the condensation product has at least one tertiary amino group;(II) an amine substituted with the hydrocarbyl-substituent of a)ii), wherein the amine has at least one tertiary amino group and the hydrocarbyl-substituent is a polyalkene-substituent;(III) a compound containing at least one hydrocarbyl-substituent of a)ii) and at least one tertiary amino group, wherein the hydrocarbyl-substituent is a polyester group; or(IV) any combination thereof.3. The composition of wherein component a) claim 1 , the compound comprising at least one tertiary amino group claim 1 , comprises the condensation product of a hydrocarbyl-substituted acylating agent and a compound having an oxygen or nitrogen atom capable of condensing with said acylating agent and further having at least one tertiary amino group; andwherein the hydrocarbyl-substituted acylating agent is polyisobutylene succinic anhydride and the ...

Diesel Detergent Without A Low Molecular Weight Penalty

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors. 2. A diesel fuel comprising the composition of .3. The diesel fuel of claim 2 , wherein the diesel fuel is ultra-low sulfur diesel fuel.4. The diesel fuel of claim 2 , wherein the quaternary ammonium salt is present from about 10 to about 500 ppm.5. A method of minimizing creation of internal diesel injector deposits while additionally reducing the level of pre-existing internal diesel injector deposits comprising the step of supplying to a diesel engine a diesel fuel composition comprising (A) diesel fuel; and (B) a composition according to .6. The method of wherein the diesel engine comprises common rail diesel injectors.7. A gasoline fuel comprising the composition of . This application is a continuation application of U.S. application Ser. No. 16/223,485, which is a continuation of U.S. application Ser. No. 14/434,985 filed on Apr. 10, 2015, granted as U.S. Pat. No. 10,202,559 on Feb. 12, 2019, which claims priority to PCT Application Serial No. PCT/US2013/066135 filed on Oct. 22, 2013 which claims benefit of U.S. Provisional Application Ser. No. 61/717,161 filed on Oct. 23, 2012.The composition of the present invention is related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors.It is well known that liquid fuel contains components that can degrade during engine operation and form deposits. These deposits can lead to incomplete combustion of the fuel resulting in higher emission and poorer fuel economy. Fuel additives, such as detergents, are well known additives in liquid fuels to help with control or minimize deposit formation. As ...

COMPOSITIONS FOR THE TREATMENT OF PULMONARY FIBROSIS

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions. 4. A method of prophylactically or therapeutically treating pulmonary fibrosis claim 1 , or a related condition in a subject with pulmonary fibrosis or at risk of developing pulmonary fibrosis claim 1 , the method comprising administering to the subject an effective amount of a compound according to .715-. (canceled)16. The method according to claim 4 , wherein the subject at risk of developing pulmonary fibrosis:has been exposed to gases, smoke, chemicals, asbestos fibres or dusts;has an autoimmune disorder, viral infection or bacterial infection of the lung;has received radiation therapy for lung or breast cancer;has a genetic predisposition; oris a cigarette smoker.17. The method according to claim 4 , wherein claim 4 , the related condition is selected from pulmonary hypertension claim 4 , right-sided heart failure claim 4 , respiratory failure claim 4 , hypoxia claim 4 , cough claim 4 , formation of blood clots claim 4 , pneumonia and lung cancer18. The method according to claim 4 , wherein the treatment:prevents, reduces or slows the progression of pulmonary fibrosis; orreduces established pulmonary fibrosis.19. The method according to claim 5 , wherein the subject at risk of developing pulmonary fibrosis:has been exposed to gases, smoke, chemicals, asbestos fibres or dusts;has an autoimmune disorder, viral infection or bacterial infection of the lung;has received radiation therapy for lung or breast cancer;has a genetic predisposition; oris a cigarette smoker.20. The method according to claim 5 , wherein claim 5 , the related condition is selected from pulmonary hypertension claim 5 , right-sided heart failure claim 5 , respiratory failure claim 5 , hypoxia claim 5 , cough claim 5 , formation of blood clots claim 5 , pneumonia and lung cancer21. The method according to claim 5 , wherein the treatment: ...

Synthesis of Succinimides and Quaternary Ammonium Ions for Use in Making Molecular Sieves

The present invention relates to the synthesis of succinimides, in particular to a method for the synthesis of a succinimide compound, comprising the step of reacting an alkyne, with carbon monoxide and ammonia or an amine, in the presence of an iron catalyst, wherein the reaction is carried out in an amine liquid phase and/or in the absence of an ether solvent. The succinimides may be reduced to quaternary ammonium cations which may be used as structure directing agents in the synthesis of molecular sieves. 115.-. (canceled)16. A process for producing a molecular sieve , the process comprising the steps of:{'sup': −', '+, '(i) preparing a synthesis mixture capable of forming a molecular sieve, said synthesis mixture comprising a source selected from a source of a tetravalent element Y, a source of a trivalent element X, or a mixture of a source of tetravalent element Y and a source of trivalent element X, and optionally a source of pentavelent element Z, optionally a source of hydroxide ions, optionally a source of halide ions W, and optionally a source of alkali metal ions M, the synthesis mixture further comprising a structure directing agent Q comprising a cation comprising a pyrrolidinium group in which the ring nitrogen is a quaternary ammonium nitrogen and in which at least one, and preferably both, of the 3- and the 4-positions on the pyrrolidinium ring is substituted with a substituent group other than hydrogen;'}(ii) heating said synthesis mixture under crystallization conditions for a time of from about 1 to about 100 days to form crystals of said molecular sieve; and(iii) recovering said crystals of the molecular sieve from the synthesis mixture.17. The process as claimed in claim 16 , wherein the synthesis mixture does not contain any pentavelent element Z.18. The process as claimed in claim 16 , wherein the synthesis mixture contains a pentavelent element Z claim 16 , preferably phosphorus.19. The process as claimed in or as claimed in claim 16 , ...

PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF ENZALUTAMIDE

The present invention provides processes for the preparation of enzalutamide. 4. The process according to or , wherein the reaction of the compound of Formula II with the compound of Formula III to give the compound of Formula IV is carried out in a solvent selected from the group consisting of water , dimethyl sulfoxide , esters , ethers , alcohols , hydrocarbons , halogenated hydrocarbons , amides , and mixtures thereof.5. The process according to or , wherein the reaction of the compound of Formula IV with the compound of Formula V is carried out in a solvent selected from the group consisting of water , dimethyl sulfoxide , esters , ethers , alcohols , hydrocarbons , halogenated hydrocarbons , and mixtures thereof.7. (canceled)8. The process according to claim 6 , wherein the reaction of the compound of Formula VI with the compound R—OH to give the compound of Formula V is carried out in the presence of a coupling agent selected from the group consisting of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride claim 6 , N claim 6 ,N′-dicyclohexylcarbodiimide claim 6 , thionyl chloride claim 6 , and oxalyl chloride.9. The process according to claim 6 , wherein the reaction of the compound of Formula VI with the compound R—OH to give the compound of Formula V is carried out in the presence of a solvent selected from the group consisting of water claim 6 , esters claim 6 , halogenated hydrocarbons claim 6 , ethers claim 6 , alcohols claim 6 , hydrocarbons claim 6 , amides claim 6 , and mixtures thereof.10. The process according to claim 6 , wherein the reaction of the compound of Formula VI with the compound R—OH to give the compound of Formula V is carried out in the presence of N claim 6 ,N-dimethylaminopyridine.13. Use of a compound of Formula IV for the preparation of enzalutamide.14. Use of a compound of Formula V for the preparation of enzalutamide.16. The process according to claim 14 , wherein the reaction of the compound of Formula V with the ...

Improved Synthesis Of Succinimides And Quaternary Ammonium Ions For Use In Making Molecular Sieves

The present invention relates to the synthesis of succinimides, in particular to a method for the synthesis of a succinimide compound, comprising the step of reacting an alkyne, with carbon monoxide and ammonia or an amine, in the presence of an iron catalyst, wherein the reaction is carried out in an amine liquid phase and/or in the absence of an ether solvent. The succinimides may be reduced to quaternary ammonium cations which may be used as structure directing agents in the synthesis of molecular sieves.

PYRROLIDINE-2, 5-DIONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE AS IDO1 INHIBITORS

The present invention relates to compound of Formula I

QUATERNARY AMMONIUM COMPOUNDS AS FUEL OR LUBRICANT ADDITIVES

A quaternary ammonium compound of formula (X): 1. A method of preparing a fuel composition , said method comprising: preparing a quaternary ammonium compound by reacting:{'sup': 1', '2', '3, '(a) a tertiary amine of formula RRRN with;'}(b) an epoxide; in the presence of(c) a monoester of a diacid including an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms;{'sup': 1', '2', '3, 'wherein R, Rand Rare each independently selected from an optionally substituted alkyl, alkenyl or aryl group; and mixing the quaternary ammonium compound into a fuel.'}2. A method according to wherein each of Rand Ris independently alkyl claim 1 , alkenyl or aryl group having from 1 to 50 carbon atoms optionally substituted with one or more groups selected from halo (especially chloro and fluoro) claim 1 , hydroxy claim 1 , alkoxy claim 1 , keto claim 1 , acyl claim 1 , cyano claim 1 , mercapto claim 1 , alkylmercapto claim 1 , dialkylamino claim 1 , nitro claim 1 , nitroso claim 1 , and sulphoxy.3. A method according to wherein Ris an alkyl or alkenyl group having from 1 to 50 carbon atoms optionally substituted with one or more substituents selected from halo (especially chloro and fluoro) claim 1 , hydroxy claim 1 , alkoxy claim 1 , keto claim 1 , acyl claim 1 , cyano claim 1 , mercapto claim 1 , alkylmercapto claim 1 , amino claim 1 , alkylamino claim 1 , nitro claim 1 , nitroso claim 1 , sulphoxy claim 1 , amido claim 1 , alkyamido claim 1 , imido and alkylimido.4. A method according to wherein Ris an alkyl or alkenyl group optionally substituted with alkoxy or hydroxy groups.5. A method according to wherein each of Rand Ris an unsubstituted alkyl group or a hydroxy substituted alkyl group.9. A method according to wherein each of R claim 1 , Rand Ris selected from an alkyl or hydroxyl alkyl group having 1 to 10 carbon atoms.10. A method according to wherein epoxide (b) is selected from styrene oxide claim 1 , ethylene oxide claim 1 , propylene oxide claim 1 , ...

PROCESS FOR PREPARING INTERMEDIATES FOR THE SYNTHESIS OF OPTICALLY ACTIVE BETA-AMINO ALCOHOLS BY ENZYMATIC REDUCTION AND NOVEL SYNTHESIS INTERMEDIATES

Subject-matter of the present invention is a process for preparing intermediates for the synthesis of optically active beta-amino alcohols by enzymatic reduction of the corresponding beta-amino ketones. Subject-matter of the invention are also said novel synthesis intermediates and the use thereof in the preparation of active pharmaceutical ingredients, among which vilanterol and the salts thereof. 2. The process according to claim 1 , wherein said two Pr protective groups claim 1 , together with the oxygen atoms to which they are bound claim 1 , form a cycle fused with the benzene.4. The process according to claim 1 , wherein said imide is succinimide.5. The process according to claim 1 , wherein said enzymatic reduction is carried out by at least one oxidoreductase enzyme.6. The process according to claim 5 , wherein said oxidoreductase enzyme has a sequence selected from the sequences SEQ ID No: 1 and SEQ ID No: 2 or has an amino acid sequence having at least 60% of the amino acids identical to the amino acid sequence of SEQ ID NO: 1 and SEQ ID NO:2.7. The process according to claim 6 , wherein said oxidoreductase enzyme has the sequence SEQ ID No: 1.8. The process according to claim 1 , wherein said enzymatic reduction is carried out by at least one oxidoreductase enzyme claim 1 , in the presence of at least one cofactor and at least one co-substrate regenerating said cofactor.10. (canceled)11. The process according to claim 3 , wherein said imide is succinimide.12. The process according to claim 5 , wherein said oxidoreductase enzyme has an amino acid sequence having at least 80% of the amino acids identical to the amino acid sequence of SEQ ID NO: 1 and SEQ ID NO:2.13. The process according to claim 5 , wherein said oxidoreductase enzyme has an amino acid sequence having at least 90% of the amino acids identical to the amino acid sequence of SEQ ID NO: 1 and SEQ ID NO:2. A subject-matter of the present invention is a process for preparing intermediates for the ...

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

The present invention provides compounds of formula (I), 2. A pharmaceutical composition comprising the compound of or a pharmaceutically acceptable salt thereof.3. A method of treating multiple sclerosis in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of the compound of .4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of a composition of . This application is a continuation of U.S. application Ser. No. 15/683,189, filed Aug. 22, 2017, which is a divisional of U.S. application Ser. No. 14/744,325, filed Jun. 19, 2015, now abandoned, which is a continuation of U.S. application Ser. No. 14/180,687, filed Feb. 14, 2014, now U.S. Pat. No. 9,090,558, issued Jul. 28, 2015, which claims the benefit of U.S. Provisional Application No. 61/782,445, filed on Mar. 14, 2013. The entire teachings of the above applications are incorporated herein by reference.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions involving immunological, autoimmune, and/or inflammatory processes including psoriasis (Joshi and Strebel, WO 1999/49858; U.S. Pat. No. 6,277,882; Mrowietz and Asadullah, 2005, 111(1), 43-48; and Yazdi and Mrowietz, 2008, 26, 522-526); asthma and chronic ...

Diesel detergent without a low molecular weight penalty

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors.

Diesel detergent without a low molecular weight penalty

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors.

Methods and compositions for the target-localized anchoring of detectable label

Highly reactive functionalized substrates and linker molecules for use in the detection of molecular targets and other analytes of interest are provided as are kits, reaction mixtures and methods utilizing the same.

用于可检测的标记的靶标定位锚定的方法和组合物

本发明提供了用于检测分子靶标和其它目标分析物的高反应性的官能化的基底和接头分子，还提供了利用它们的试剂盒、反应混合物和方法。

Aqueous coating compositions including the reaction product of maleic anhydride with an unsaturated compound and an amine

The invention includes an aqueous coating composition having a substituted succinimide compound, wherein the substituted succinimide compound has an acid value of at least about 30 mg KOH/g of the substituted succinimide compound. The substituted succinimide compound may be the reaction product of an unsaturated oil comprising at least one non-aromatic unsaturated carbon-carbon bond, a polymer derived from the unsaturated oil, or a combination thereof with maleic anhydride and a primary amine.

Prodrugs of Fumarates and Their Use in Treating Various Diseases

The present invention provides compounds of formula (I), 2. A pharmaceutical composition comprising the compound of claim 1 , or a pharmaceutically acceptable salt thereof.3. A method of treating multiple sclerosis in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of the compound of .4. A method of treating multiple sclerosis in a subject in need thereof claim 2 , comprising administering to the subject a therapeutically effective amount of the composition of . This application is a continuation of U.S. application Ser. No. 16/987,581, filed Aug. 7, 2020, which is a continuation of U.S. application Ser. No. 16/221,884, filed Dec. 17, 2018, now abandoned, which is a continuation of U.S. application Ser. No. 15/683,189, filed Aug. 22, 2017, now U.S. Pat. No. 10,189,855, issued Jan. 29, 2019, which is a divisional of U.S. application Ser. No. 14/744,325, filed Jun. 19, 2015, now abandoned, which is a continuation of U.S. application Ser. No. 14/180,687, filed Feb. 14, 2014, now U.S. Pat. No. 9,090,558, issued Jul. 28, 2015, which claims the benefit of U.S. Provisional Application No. 61/782,445, filed on Mar. 14, 2013. The entire teachings of the above applications are incorporated herein by reference.The present invention relates to various prodrugs of monomethyl fumarate. In particular, the present invention relates to derivatives of monomethyl fumarate which offer improved properties relative to dimethyl fumarate. The invention also relates to methods of treating various diseases.Fumaric acid esters (FAEs) are approved in Germany for the treatment of psoriasis, are being evaluated in the United States for the treatment of psoriasis and multiple sclerosis, and have been proposed for use in treating a wide range of immunological, autoimmune, and inflammatory diseases and conditions.FAEs and other fumaric acid derivatives have been proposed for use in treating a wide-variety of diseases and conditions ...

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for refining process; and (ii) adding an additive to the crude hydrocarbon.

Functionalized polymers containing polyamine succinimide for antifouling in hydrocarbon refining processes

A multipurpose chemical additives (MPC) is disclosed to mitigate fouling in hydrocarbon refinery processes, such as in a heat exchanger. A method for reducing fouling of a hydrocarbon is also disclosed that includes (i) providing a crude hydrocarbon for a refining process; and (ii) adding an additive to the crude hydrocarbon.

用于治疗纤维化和纤维化相关病症的组合物

本发明涉及新的化合物及其预防性治疗和/或治疗性治疗纤维化及纤维化相关病症的用途。

Compositions for treating fibrosis and fibrosis-related conditions

FIELD: chemistry.SUBSTANCE: present invention relates to a novel compound of formula:or to its pharmacologically acceptable salt. In said structural formulas A is selected from: partially saturated or unsaturated 5- or 6-member heterocyclyl selected from pyrrolyl, pyrazolyl, imidazolyl, triazolyl, imidazolidinyl, pyrrolidinyl, pyrrolidinylidene, dihydropyrrolyl, isoxazolyl-dihydrooxazolyl, isoxazolidinyl, oxazolidinyl and oxazolyl, where said partially saturated or unsaturated 5- or 6-member heterocyclyl is optionally substituted with one or more oxo, Calkyl, amino, hydroxyl or halogen; Calkoxylamine; Calkylamine, optionally substituted with one or more substitutes, which are Calkyl, Chaloalkyl, hydroxyl or halogen; Calkyl-carboxylic acid; Calkylhydroxyl; saturated or unsaturated Calkyl-bicyclic-heterocyclyl, selected from indolyl, isoindolyl, indolinyl and isoindolinyl, where said saturated or unsaturated Calkyl-bicyclic-heterocyclyl is optionally substituted with one or more oxo; and saturated or unsaturated Calkoxy-bicyclic-heterocyclyl, selected from indolyl, isoindolyl, indolinyl and isoindolinyl, where said Calkoxy-bicyclic-heterocyclyl is optionally substituted with one or more oxo.EFFECT: compound is used for preventive or therapeutic treatment of fibrosis.27 cl, 22 dwg, 15 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 39/15 (2006.01) C07C 47/575 (2006.01) C07C 65/03 (2006.01) C07C 211/29 (2006.01) C07C 217/48 (2006.01) C07D 207/267 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 207/36 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 207/408 (2006.01) C07D 207/448 (2006.01) C07D 209/48 (2006.01) (12) (13) 2 712 140 C2 C07D 233/78 (2006.01) C07D 261/14 (2006.01) C07D 263/42 (2006.01) C07D 263/44 (2006.01) A61K 31/165 (2006.01) A61K 31/192 (2006.01) A61K 31/381 (2006.01) A61K 31/42 (2006.01) A61P 1/12 (2006.01) (см. продолжение) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК (21)(22) Заявка: 2017135950, 18.03.2016 18.03.2016 (73) Патентообладатель(и): ВЕКТУС БАЙОСИСТЕМС ...

저분자량 불이익이 없는 디젤 청정제

본 발명의 조성물은 4차 암모늄 염 청정제 및 디젤 인젝터 침전물을 감소시키고 디젤 인젝터에 존재하는 침전물을 제거하거나 청소하기 위해 연료 조성물에 사용되는 상기 4차 암모늄 염 청정제의 용도에 관한 것이다.

저분자량 불이익이 없는 디젤 청정제

본 발명의 조성물은 4차 암모늄 염 청정제 및 디젤 인젝터 침전물을 감소시키고 디젤 인젝터에 존재하는 침전물을 제거하거나 청소하기 위해 연료 조성물에 사용되는 상기 4차 암모늄 염 청정제의 용도에 관한 것이다.

섬유증 및 섬유증 관련 질병 치료용 조성물

본 발명은 섬유증 및 섬유증 관련 질병의 예방 및/또는 치료에서의 신규 화합물 및 이의 용도에 관한 것이다.

Diesel detergent without a low molecular weight penalty

본 발명의 조성물은 4차 암모늄 염 청정제 및 디젤 인젝터 침전물을 감소시키고 디젤 인젝터에 존재하는 침전물을 제거하거나 청소하기 위해 연료 조성물에 사용되는 상기 4차 암모늄 염 청정제의 용도에 관한 것이다. The composition of the present invention relates to a quaternary ammonium salt detergent and the use of said quaternary ammonium salt detergent for use in fuel compositions to reduce diesel injector deposits and to remove or clean up deposits present in diesel injectors.

Композиции для лечения фиброза и связанных с фиброзом состояний

Diesel detergent without a low molecular weight penalty

본 발명의 조성물은 4차 암모늄 염 청정제 및 디젤 인젝터 침전물을 감소시키고 디젤 인젝터에 존재하는 침전물을 제거하거나 청소하기 위해 연료 조성물에 사용되는 상기 4차 암모늄 염 청정제의 용도에 관한 것이다. The composition of the present invention relates to a quaternary ammonium salt detergent and the use of said quaternary ammonium salt detergent for use in fuel compositions to reduce diesel injector deposits and to remove or clean up deposits present in diesel injectors.

Diesel detergent without a low molecular weight penalty

The composition of the present invention related to a quaternary ammonium salt detergent and the use of such quaternary ammonium salt detergents in a fuel composition to reduce diesel injector deposits and remove or clean up existing deposits on the diesel injectors.

Titanocenes, the use thereof, and n-substituted fluoroanilines

Titanocenes containing two 5-membered cyclodienyl gropus, for example cyclopentadienyl, and one or two 6-membered carbocyclic or 5- or 6-membered heterocyclic aromatic rings which are substituted by a fluorine atom in at least one of the two ortho-positions to the titanium-carbon bond and contain, as further substituents, a substituted amino radical, are suitable as photoinitiators for radiation-induced polymerization of ethylenically unsaturated compounds.

Composition for the treatment of pulmonary fibrosis

본 발명은 폐 섬유증 및/또는 관련 질환의 예방 및/또는 치료학적 치료에서의 화합물 및 이의 용도에 관한 것이다. The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related diseases.

Aqueous coating compositions including reaction product of maleic anhydride with unsaturated compound and amine

FIELD: chemistry.SUBSTANCE: invention relates to an aqueous coating compositions including a substituted succinimide compound, wherein the substituted succinimide compound has an acidity value of 30 to 300 mg KOH/g of the substituted succinimide compound. Said substituted succinimide compound is a reaction product of an unsaturated oil containing at least one non-aromatic unsaturated carbon-carbon bond, a polymer derived from an unsaturated oil, and a combination thereof, maleic anhydride and a compound of general NHRCOOH formula in which R can be an alkyl or aryl group with 2 to 30 carbon atoms and in which the amino group is separated from the acid group by more than one carbon atom. Also, the substrate and process for preparing an aqueous coating composition are described.EFFECT: technical result is the provision of coatings resistant to delamination, as well as improved adhesion and corrosion resistance on metal substrates.8 cl, 1 dwg, 4 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) (19) RU (11) (13) 2 663 171 C2 (51) МПК C09D 5/08 (2006.01) C09D 201/00 (2006.01) C09D 191/00 (2006.01) C09F 7/00 (2006.01) C23F 11/173 (2006.01) C23F 11/14 (2006.01) B65D 23/02 (2006.01) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК B65D 23/02 (2018.05); C07D 207/40 (2018.05); C07D 207/408 (2018.05); C09D 125/08 (2018.05); C09D 133/00 (2018.05); C09D 163/00 (2018.05); C09D 173/02 (2018.05); C09D 175/04 (2018.05); C09D 191/005 (2018.05); C09D 5/00 (2018.05); C09D 7/00 (2018.05); C09D 7/45 (2018.05); C09F 7/00 (2018.05); C23F 11/00 (2018.05) (24) Дата начала отсчета срока действия патента: 19.09.2013 Дата регистрации: 01.08.2018 Приоритет(ы): (30) Конвенционный приоритет: (73) Патентообладатель(и): АКЦО НОБЕЛЬ КОАТИНГС ИНТЕРНЭШНЛ Б.В. (NL) (56) Список документов, цитированных в отчете о поиске: US 20090029155 A1, 29.01.2009. US 19.09.2012 US 61/702,789; 11.10.2012 EP 12188180.9; 25.04.2013 US 61/815,814 (43) Дата публикации заявки: 10.11.2016 Бюл. № 31 ( ...

Quaternary ammonium compounds as additives to fuel or lubricants

FIELD: machine building. SUBSTANCE: invention relates to a novel diesel fuel composition which contains as an additive one or more quaternary ammonium compounds of formula (X) , (X'), where each of R 0 , R 1 , R 2 and R 3 independently represents C 1 -C 6 alkyl group optionally substituted with a hydroxy group and/or alkoxy group, and A is CHRCH 2 , where R is a polyisobutenyl group having a molecular weight of 260 to 1000, or C 10 -C 24 alkyl or alkenyl group. Preferably, the composition contains a quaternary ammonium compound (X'), where each of R 1 , R 2 and R 3 and A have values given above, each of R 4 , R 5 , R 6 and R 7 is independently selected from hydrogen or alkyl group, optionally substituted with hydroxy group and/or alkoxy group. Compound (X) can be a reaction product of (a) a tertiary amine of formula R 1 R 2 R 3 N, molecular weight of which is less than 1000; (b) epoxide of formula ; and (c) a diacid of formula HOOCCHRCH 2 COOH, where R is a polyisobutenyl group having a molecular weight of 260 to 1000, or C 10 -C 24 alkyl group, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 and R 7 have values given above. Invention also relates to a method of improving operational characteristics of a diesel engine by burning said composition in an engine. Engine represents a diesel engine with a fuel injection system, which includes a high pressure fuel injection system (HPFI), in which fuel pressure exceeds 1350 bar (1.35⋅10 8 Pa). Use of additive counteracts formation of deposits in engine, in particular formation of internal deposits in injectors of diesel engine and external deposits on nozzles of diesel engine, including deposits on injector nozzle and deposits on nozzle tip, and also formation of deposits on fuel filter. Use of the additive in the composition also helps to maintain purity or purification of the engine. EFFECT: use of fuel with the proposed additive in comparison with the known additive leads to increase of torque and increases average flow ...

Aryl sulfide derivatives and aryl sulfoxide derivatives as acaricides and insecticides

The invention relates to aryl sulfide derivatives and aryl sulfoxide derivatives, use thereof as acaricides and insecticides for controlling animal pests, and methods and intermediate products for the production thereof. The aryl sulfide derivatives and aryl sulfoxide derivatives have the general structure (I) in which the respective groups have the meanings as cited in the description.

Quaternary ammonium compounds as fuel or lubricant additives

(a) 1000 미만의 분자량을 갖는 3급 아민; (b) 산-활성화된 알킬화제; 및 (c) 적어도 5개의 탄소 원자를 갖는 임의로 치환된 히드로카르빌 모이어티를 포함하는 이산의 반응 생성물인 4급 암모늄 화합물이 제공된다. (a) a tertiary amine having a molecular weight of less than 1000; (b) acid-activated alkylating agents; and (c) a diacid comprising an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms.

AQUEOUS COMPOSITIONS FOR COATING, INCLUDING THE PRODUCT OF THE REACTION OF MALEIC ANHYDRIDE WITH AN UNSATURATED COMPOUND AND AMINE

1. Водная композиция для покрытия, включающая замещенное соединение сукцинимида, где замещенное соединение сукцинимида имеет величину кислотности, по меньшей мере, 30 мг КОН/г замещенного соединения сукцинимида, и где замещенное соединение сукцинимида является продуктом реакцииa) ненасыщенного масла, содержащего по меньшей мере, одну неароматическую ненасыщенную связь углерод-углерод, полимера, производного от ненасыщенного масла или их комбинации;b) малеинового ангидрида; иc) первичного амина с общей формулой NHRCOOH, в которой R может быть алкильной группой или арильной группой с примерно от 2 до примерно 30 атомами углерода и в которой амино (-NH) группа и кислотная (-СООН) группа первичного амина отделены более чем одним атомом углерода.2. Водная композиция для покрытия по п. 1, где водная композиция для покрытия дополнительно содержит связующий полимер, и где замещенное соединение сукцинимида содержит от более чем 0 до примерно 10 вес.% композиции для покрытия.3. Водная композиция для покрытия по п. 2, где связующий полимер включает акриловый полимер, стирол-акриловый полимер, полиуретановый полимер, алкидный полимер, эпоксидный полимер или смесь, или гибридный сополимер из них.4. Водная композиция для покрытия по пп. 1-3, где средневесовая молекулярная масса замещенного соединения сукцинимида составляет от примерно 400 до примерно 10000 дальтонов.5. Водная композиция для покрытия по пп. 1-3, где величина кислотности замещенного соединения сукцинимида составляет от примерно 30 до примерно 300 мг КОН/г замещенного соединения сукцинимида.6. Водная композиция для покрытия по пп. 1-3, где замещенное соединение сукцинимида является частично или полностью нейтрализованным для РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C09D 5/00 (13) 2015 113 442 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2015113442, 19.09.2013 (71) Заявитель(и): АКЦО НОБЕЛЬ КОАТИНГС ИНТЕРНЭШНЛ Б.В. (NL) Приоритет(ы): (30) Конвенционный ...

Composition for treating pulmonary fibrosis

본 발명은 폐 섬유증 및/또는 관련 질환의 예방 및/또는 치료학적 치료에서의 화합물 및 이의 용도에 관한 것이다.

New compounds for inhibiting differentiation of osteoclast and pharmaceutical composition comprising thereof

PURPOSE: A pharmaceutical composition containing a novel compound is provided to effectively suppress osteoclast differentiation and to be used as a therapeutic agent for treating bone metabolic diseases. CONSTITUTION: A novel compound with an effect of suppressing osteoclast differentiation contains a compound of chemical formula I-a or I-b or pharmaceutically acceptable salt thereof. A pharmaceutical composition for preventing or treating bone metabolic diseases contains the compound of chemical formula I-a or I-b or pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition contains 1-(4-chlorophenyl)-3,4-diphenyl-1H-pyrrole-2,5-dione as an active ingredient.

Dispersant reaction product with antioxidant capability

분산제 반응 생성물에 산화방지 부분이 융합되어, 상기 분산제 반응 생성물이 하나는 슬러지와 관련된 극성 도메인 및 오일 용해성을 위한 히드로카르빌 도메인인 2 개 이상의 구조적 도메인을 유지하면서 산화방지제로서 기능할 수 있고, 그리하여 상기 분산제가 슬러지를 현탁시키고 슬러지 전구체의 응집 및 그을음을 예방하기 위한 화학제로서 작용할 수 있어서, 후자가 내부 기관 부품에 해롭게 침착되는 대신에, 예를 들어 여과에 의해서 시스템으로부터 쉽게 제거될 수 있는 신규 크랭크케이스 분산제 반응 생성물뿐만 아니라, 이같은 신규 분산제를 혼입하는 윤활 조성물 및, 예를 들어 상기 윤활 조성물로 윤활되는 기관. The antioxidant moiety is fused to the dispersant reaction product so that the dispersant reaction product can function as an antioxidant while maintaining at least two structural domains, one of which is a polar domain associated with sludge and a hydrocarbyl domain for oil solubility. The dispersant may act as a chemical to suspend sludge and prevent flocculation and sooting of the sludge precursors, so that the latter can be easily removed from the system, for example by filtration, instead of being detrimentally deposited on the internal organ parts. A crankcase dispersant reaction product, as well as a lubricating composition incorporating such a novel dispersant and, for example, an engine lubricated with the lubricating composition. 산화방지제, 분산제 반응 생성물, 윤활 조성물 Antioxidant, dispersant reaction product, lubricating composition

Compositions for pulmonary fibrosis treatment

FIELD: biochemistry. SUBSTANCE: present invention relates to a compound of the formula or its pharmacologically acceptable salt, wherein: B is selected from a group consisting of: R 1 and R 3 independently represent CH or N; R 2 represents CH or С=O; R 5 -R 9 independently represent С or N; Q is independently selected from an alkyl, hydroxy, amino, and substituted amine selected from a group consisting of -NHSO 2 CH 3 , -NHCOH, -NHCONHCH 3 , -NHCONHCH 2 CH 3 , -NHSO 2 NHCH 3 , -NHSO 2 NHCH 2 CH 3 and -NHCOCH 3 ; n is equal to 0, 1 or 2; D represents: R 10 -R 14 independently represent С, N or S; Т is independently selected from С 1-6 alkyl and halogen; and m is equal to 0, 1, 2, 3 or 4, in this case, D cannot be an unsubstituted phenyl, and Q cannot be a hydroxy when n is 1 and all R 5 -R 9 represent С. In addition, the invention relates to the compound and its pharmacologically acceptable salt, to a method for the preventive or therapeutic treatment of pulmonary fibrosis or a related condition in a subject with pulmonary fibrosis or at risk of developing pulmonary fibrosis, including the introduction of the above compounds, as well as to the use of these compounds for the manufacture of a drug for the preventive or therapeutic treatment of pulmonary fibrosis. EFFECT: new compounds that can be useful in treatment of pulmonary fibrosis have been obtained and described. 16 cl, 5 dwg, 3 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07C 235/34 (2006.01) C07D 213/56 (2006.01) C07D 333/24 (2006.01) C07D 207/327 (2006.01) C07D 307/54 (2006.01) C07D 231/12 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА C07D 239/26 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ C07D 277/30 (2006.01) C07D 261/08 (2006.01) C07C 235/78 (2006.01) (12) (13) 2 747 801 C2 C07C 237/20 (2006.01) C07H 15/203 (2006.01) A61K 31/165 (2006.01) A61K 31/381 (2006.01) A61K 31/402 (2006.01) A61K 31/4418 (2006.01) A61K 31/415 (2006.01) A61K 31/426 (2006.01) A61K 31/192 (2006.01) (см. продолжение) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ ( ...

Method and reagents for N-alkylating ureides

A method of N-alkoxyalkylating ureides according to the invention comprises reacting a ureide of structure I with an alkylating agent of structure III in the presence of a basic catalyst in an aprotic reaction medium. The ureide may be a 5,5-disubstituted barbituric acid, or it may be phenytoin, glutethimide, and ethosuximide. The alkylating agent is an ester of a sulfonic acid. The base may be a hydride or amine. A preferred process comprises N-alkoxyalkylating 5,5-diphenyl-barbituric acid with methoxymethyl methanesulfonate in the presence of di-isopropyl ethyl amine and isolating the resultant N,N′-bismethoxymethyl-5,5-diphenyl-barbituric acid. The invention also contemplates the novel compounds N-methoxymethyl-5,5-diphenylbarbituric acid, N-methoxymethyl ethosuximide, and N-methoxymethyl glutethimide, and a method comprising administering them to a patient.

Dispersant reaction product with antioxidant capability

一种其中熔合了抗氧化剂片断的新颖曲轴箱分散剂反应产物，因而该分散剂反应产物可以发挥抗氧化剂的功能同时保留至少两种结构畴，一种是能与污泥缔合的极性畴和一种油溶性的烃基畴，因此，该分散剂可以充当一种能使污泥悬浮并防止污泥前体和烟尘附聚的化学剂，使得后者可以诸如通过过滤而容易地从该系统中除去而不是有害地沉积到内燃机部件上，以及掺入了这样的新颖分散剂的润滑剂组合物和，例如，用这样的润滑剂组合物润滑的发动机。

Compositions for the treatment of pulmonary fibrosis

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2019 104 161 A (51) МПК C07C 235/34 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2019104161, 28.07.2017 (71) Заявитель(и): ВЕКТУС БАЙОСИСТЕМС ЛИМИТЕД (AU) Приоритет(ы): (30) Конвенционный приоритет: 28.07.2016 AU 2016902978 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 28.02.2019 R U (43) Дата публикации заявки: 28.08.2020 Бюл. № 25 (72) Автор(ы): ДАГГЭН Карен Аннетт (AU) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2018/018091 (01.02.2018) A Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ" (54) Композиции для лечения легочного фиброза R U 1. Соединение формулы: A 2 0 1 9 1 0 4 1 6 1 (57) Формула изобретения 2 0 1 9 1 0 4 1 6 1 AU 2017/050784 (28.07.2017) или его фармакологически приемлемые соль, стереоизомер, диастереомер, энантиомер, рацемат, гидрат и/или сольват, где: В выбран из группы, состоящей из: Стр.: 1 R1, R3 и R4 независимо представляют собой С, СН, СН2, О, N, NH или S; R2 представляет собой С, СН, СН2, N, NH, C-CF3, CH-CF3 или С=O; R5-R9 независимо представляют собой С или N; Q независимо выбран из галогена, алкила, гидрокси, амино и замещенного амино; n равно 0, 1, 2, 3, 4 или 5; D представляет собой: R U A 2 0 1 9 1 0 4 1 6 1 2 0 1 9 1 0 4 1 6 1 A R U R10-R14 независимо представляют собой С, N, О или S; Т независимо выбран из С1-6алкила, галогена, С0-6алкилкарбоновой кислоты, амино, гидрокси и С1-6алкокси; и m равно 0, 1, 2, 3 или 4, при этом D не может представлять собой незамещенный фенил, и Q не может представлять собой гидрокси, когда n равно 1, и все R5-R9 представляют собой С. 2. Соединение по п. 1, где соединение выбрано из группы, состоящей из: Стр.: 2 A 2 0 1 9 1 0 4 1 6 1 A 2 0 1 9 1 0 4 1 6 1 R U R U Стр.: 3 A 2 0 1 9 1 0 4 1 6 1 A 2 0 1 9 1 0 4 1 6 1 R U R U Стр.: 4 или их фармакологически приемлемых соли, стереоизомера, диастереомера, энантиомера, рацемата, гидрата и/или сольвата. 3. Соединение формулы: ...

Amide derivative

　本発明は、部分発作及び／又は全般発作の種々てんかん発作に対する治療薬若しくは予防薬として有用な式（Ｉ）の化合物又はその塩［式中、Ａ環及びＢ環は、それぞれ独立して、アリール環等を表し、Ｌは、結合、Ｃ １－６ アルキレン等を表し、Ａｌｋは、結合、Ｃ １－６ アルキレン等を表し、Ｘは、－ＣＯＮＲ ７ Ｒ ８ 、－ＳＯ ２ ＮＲ ７ Ｒ ８ 等を表し、Ｒ １ 、Ｒ ２ 及びＲ ３ は、同一又は異なって、水素原子、ハロゲン等を表し、Ｒ ４ 及びＲ ５ は、それぞれ独立して、水素原子、ハロゲン等を表し、Ｒ ７ 、Ｒ ８ 等は、それぞれ独立して、水素原子、Ｃ １－６ アルキル等を表す］を提供する。

Patent RU2016104250A3

ВИ“? 2016104250” АЗ Дата публикации: 25.04.2018 Форма № 18 ИЗПМ-2011 Федеральная служба по интеллектуальной собственности Федеральное государственное бюджетное учреждение 5 «Федеральный институт промышленной собственности» (ФИПС) ОТЧЕТ О ПОИСКЕ 1. . ИДЕНТИФИКАЦИЯ ЗАЯВКИ Регистрационный номер Дата подачи 2016104250/04(006762) 28.07.2014 РСТ/СВ2014/052311 28.07.2014 Приоритет установлен по дате: [ ] подачи заявки [ ] поступления дополнительных материалов от к ранее поданной заявке № [ ] приоритета по первоначальной заявке № из которой данная заявка выделена [ ] подачи первоначальной заявки № из которой данная заявка выделена [ ] подачи ранее поданной заявки № [Х] подачи первой(ых) заявки(ок) в государстве-участнике Парижской конвенции (31) Номер первой(ых) заявки(ок) (32) Дата подачи первой(ых) заявки(ок) (33) Код страны 1. 1313423.4 26.07.2013 СВ Название изобретения (полезной модели): [Х] - как заявлено; [ ] - уточненное (см. Примечания) ЧЕТВЕРТИЧНЫЕ АММОНИЕВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ДОБАВОК К ТОПЛИВУ ИЛИ СМАЗОЧНЫМ МАТЕРИАЛАМ Заявитель: ИННОСПЕК ЛИМИТЕД, СВ 2. ЕДИНСТВО ИЗОБРЕТЕНИЯ [Х] соблюдено [ ] не соблюдено. Пояснения: см. Примечания 3. ФОРМУЛА ИЗОБРЕТЕНИЯ: [Х] приняты во внимание все пункты (см. Примечания) [ ] приняты во внимание следующие пункты: [ ] принята во внимание измененная формула изобретения (см. Примечания) 4. КЛАССИФИКАЦИЯ ОБЪЕКТА ИЗОБРЕТЕНИЯ (ПОЛЕЗНОЙ МОДЕЛИ) (Указываются индексы МПК и индикатор текущей версии) С07С 211/62 (2006.01) С 1ОГ. 1/188 (2006.01) СТОМ 133/04 (2006.01) С1ОГ. 1/232 (2006.01) С 10Г. 10/06 (2006.01) С1ОГ. 1/222 (2006.01) С 10Г. 10/18 (2006.01) 5. ОБЛАСТЬ ПОИСКА 5.1 Проверенный минимум документации РСТ (указывается индексами МПК) С07С 211/62, СЛОТ, 1/232, СЛОТ, 1/222, СТОГ, 1/188, СЛОГ, 10/06, СТОГ, 10/18, С1ОМ 133/04 5.2 Другая проверенная документация в той мере, в какой она включена в поисковые подборки: 5.3 Электронные базы данных, использованные при поиске (название базы, и если, возможно, поисковые термины): СТРО, РЕРАТБ ...

Local application of antiandrogen against hair fall out and other hyperandrogenic states

FIELD: organic chemistry, cosmetology. SUBSTANCE: the present innovation deals with new compounds of 2-hydroxy-2 methyl- N-(4-X-3- (trifluoromethyl)phenyl)-3- perfluoracylamino)propionamide, where X means nitro, cyano or halogen, and perfluoracylamino contains 2-3 carbon atoms and 0-1 hydrogen atom. The mentioned compounds specifically inhibit and/or eliminate receptors of head skin androgens and, thus, could be applied as cosmetic substance in case of cutaneous disorders caused by excess of androgens, such as hair fall out, hirsutism, acne and androgenic alopecia. EFFECT: higher efficiency of application. 11 cl, 11 ex, 4 tbl оОо6б$59ссс ПЧ сэ (19) РОССИЙСКОЕ — АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ ФЕДЕРАЦИИ ВЦ 2 225 390 (51) МПК? (13) С2 61 Р 5/28 К ПАТЕНТУ РОССИЙСКОЙ (21), (22) Заявка: 2001130354/04 , 25.05.2000 (24) Дата начала действия патента: 25.05.2000 (30) Приоритет: 11.02.2000 14$ — 09/502,376 (43) Дата публикации заявки: 20.07.2003 (46) Дата публикации: 10.03.2004 (56) Ссылки: Ч$ 4 636 505 А, 13.01.1987. 0$ 4 282 218 А, 04.08.1981. КУ 2 132 327 С1, 21.06.1999. (85) Дата перевода заявки РСТ на национальную фазу: 12.11.2001 (86) Заявка РСТ: 4$ 00/14792 (25.05.2000) (87) Публикация РСТ: УМО 01/58854 (16.08.2001) (98) Адрес для переписки: 129010, Москва, ул. Б. Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", Н.Г.Лебедевой (72) Изобретатель: СОВАК Милос (ЦЗ), СЕЛИГСОН Аллен Л. (4$), КЭМПИОН Брайан (4$), БРАУН Джэйсон В. (4$) (73) Патентообладатель: БАИОФИЗИКА, ИНК. (1$) (74) Патентный поверенный: Лебедева Наталья Георгиевна (54) Местное применение антиандрогена от выпадения волос и других гиперандрогенных СОСТОЯНИЙ (57) Изобретение относится к органической химии, в частности к новым соединениям 2-гидрокси-2-метил-М№-(4-Х-3-(трифторметил) фенил)-3-(перфторациламино)пропионамид а, в которых Х означает нитро, циано или галоген, а перфторациламино содержит 2-3 атома углерода и 0-1 атом водорода. Указанные соединения — ...

Methods and compositions for the target-localized anchoring of detectable label

Highly reactive functionalized substrates and linker molecules for use in the detection of molecular targets and other analytes of interest are provided as are kits, reaction mixtures and methods utilizing the same.

FUMARATES AS A DEVELOPMENT AND THEIR APPLICATION IN THE TREATMENT OF DIFFERENT DISEASES

Настоящее изобретение предоставляет соединения формулы (I) и его фармацевтические композиции. The present invention provides compounds of formula (I) and pharmaceutical compositions thereof.

Small molecules useful in the treatment of inflammatory disease

A method treating or preventing inflammatory and immune cell-mediated diseases by the administration of certain novel and known small molecules. Exemplary of the novel compounds are those of structural formulas (a), (b), (c), (d), (e) and (f).

BENZHYDRYLOXYETHYL-PIPERAZINE DERIVATIVES, METHODS OF OBTAINING THEM AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

LA PRESENTE INVENTION CONCERNE DES DERIVES DE LA BENZHYDRYLOXYETHYL-PIPERAZINE DE FORMULE : (CF DESSIN DANS BOPI) ELLE CONCERNE EGALEMENT DES PROCEDES D'OBTENTION DESDITS DERIVES ET DES COMPOSITIONS PHARMACEUTIQUES LES CONTENANT. LESDITS DERIVES PRESENTENT UNE ACTIVITE ANTIHISTAMINIQUE, SANS COMPOSANTE SEDATIVE. THE PRESENT INVENTION CONCERNS BENZHYDRYLOXYETHYL-PIPERAZINE DERIVATIVES OF FORMULA: (CF DRAWING IN BOPI) IT ALSO CONCERNS PROCESSES FOR OBTAINING SUCH DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. THE SAID DERIVATIVES PRESENT ANTIHISTAMINIC ACTIVITY, WITHOUT SEDATIVE COMPONENT.

NEW DERIVATIVES OF MALEINIMIDE AND SUCCINIMIDE USEFUL AS HERBICIDES

L'invention concerne des composés chimiques nouveaux. Il s'agit de composés de formules générales : The invention relates to novel chemical compounds. These are compounds of general formulas:

IMPROVED PROCESS FOR ISOLATING ORGANIC AND LITHIUM SALT COMPLEXES USEFUL IN THIS PROCESS

PROCESS FOR THE STEREOSPECIFIC SYNTHESIS OF 4-AMINO-3-HYDROXY-CARBOXYLIC ACIDS

IMPROVED PROCESS FOR ISOLATING ORGANIC AND LITHIUM SALT COMPLEX COMPOUNDS USEFUL IN THIS PROCESS

PROCEDE PERFECTIONNE POUR ISOLER DES COMPOSES ORGANIQUES A PARTIR DE PRODUITS BRUTS OU MELANGES DE REACTION PAR DISSOLUTION DESDITS PRODUITS BRUTS OU MELANGES DE REACTION DANS UN SOLVANT ORGANIQUE NON HYDROXYLE, MISE EN CONTACT DE LA SOLUTION RESULTANTE AVEC UN SEL METALLIQUE POUR FORMER UN COMPLEXE SOLIDE DE SEL METALLIQUE, SEPARATION DUDIT COMPLEXE DE SEL METALLIQUE ET DECOMPOSITION DUDIT COMPLEXE DE SEL METALLIQUE POUR RECUPERER UN PRODUIT PUR. ON UTILISE COMME SEL METALLIQUE UN SEL DE LITHIUM. PERFECTED PROCESS FOR ISOLATING ORGANIC COMPOUNDS FROM CRUDE PRODUCTS OR MIXTURES OF REACTION BY DISSOLUTION OF SAID CRUDE PRODUCTS OR MIXTURES OF REACTION IN AN ORGANIC NON-HYDROXYL SOLVENT, CONTACT OF THE RESULTING SOLUTION WITH A METALLIC SALT SOLID TO FORM A SOLID METALLIC SALT METALLIC, SEPARATION OF THE METAL SALT COMPLEX AND DECOMPOSITION OF THE METAL SALT COMPLEX TO RECOVER A PURE PRODUCT. A LITHIUM SALT IS USED AS A METAL SALT.

Preparation of n-ethyl-alpha. alpha-dimethylsuccinimide

Process for manufacturing alpha-phenyl-succinimides

Triacylated amidoxime derivatives, synthesis thereof and industrial applications thereof especially as crosslinking agents for polyolefins

New triacylated amidoxime derivatives, synthesis thereof and industrial applications thereof, especially as crosslinking agents for polyolefins, in particular of high density polyethylene, are described. These compounds correspond to the general formula: in which R and R<1> are monovalent organic radicals, and R<2> and R<3> are also monovalent organic radicals or form, with each other, an aliphatic, alicyclic or aromatic divalent radical -Z-. They can be prepared by a process which comprises the halogenation of an aldoxime in the hydroxamoyl halide form, which is then acylated and then reacted with an alkaline imide.

POLYAZOTAL COMPOUNDS COMPRISING TWO IMIDE-TYPE TERMINAL CYCLES, THEIR PREPARATIONS AND THEIR USES.

Manufacturing process of nu-methyl-alpha-phenyl-alpha-methyl-succinimide

Retroviral protease inhibiting compounds

Inhibitors of HIV protease are provided. When bound to HIV protease, the inhibitors are characterized by a unique three-dimensional conformation and orientation relative to the S1, S1', S2, S2', S3, and S3' subsites of the protease. Pharmaceutical compositions containing the inhibitors and methods of treating HIV infection are also provided.

Alkenylsuccinimide in liquid hydrocarbon fuel

FUEL COMPOSITIONS CONTAINING A NOVEL DETERGENT ABSTRACT A liquid hydrocarbon fuel composition comprising fuel and a detergent amount of alkenylsuccinimide is characterized in that alkenylsuccinic acidor anhydride, wherein the alkenyl is derived from a designated olefinic mixture composition, is reacted with a polyalkylamine polyamine of the formula NH2-(RNH)n R-NH2 wherein R is alkylene having from 1 to 5 carbon atoms and n is from 0 to 10.

Patent RU2019104161A3

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2019 104 161 A (51) МПК C07C 235/34 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2019104161, 28.07.2017 (71) Заявитель(и): ВЕКТУС БАЙОСИСТЕМС ЛИМИТЕД (AU) Приоритет(ы): (30) Конвенционный приоритет: 28.07.2016 AU 2016902978 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 28.02.2019 R U (43) Дата публикации заявки: 28.08.2020 Бюл. № 25 (72) Автор(ы): ДАГГЭН Карен Аннетт (AU) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2018/018091 (01.02.2018) A Адрес для переписки: 191036, Санкт-Петербург, а/я 24, "НЕВИНПАТ" (54) Композиции для лечения легочного фиброза R U 1. Соединение формулы: A 2 0 1 9 1 0 4 1 6 1 (57) Формула изобретения 2 0 1 9 1 0 4 1 6 1 AU 2017/050784 (28.07.2017) или его фармакологически приемлемые соль, стереоизомер, диастереомер, энантиомер, рацемат, гидрат и/или сольват, где: В выбран из группы, состоящей из: Стр.: 1 R1, R3 и R4 независимо представляют собой С, СН, СН2, О, N, NH или S; R2 представляет собой С, СН, СН2, N, NH, C-CF3, CH-CF3 или С=O; R5-R9 независимо представляют собой С или N; Q независимо выбран из галогена, алкила, гидрокси, амино и замещенного амино; n равно 0, 1, 2, 3, 4 или 5; D представляет собой: R U A 2 0 1 9 1 0 4 1 6 1 2 0 1 9 1 0 4 1 6 1 A R U R10-R14 независимо представляют собой С, N, О или S; Т независимо выбран из С1-6алкила, галогена, С0-6алкилкарбоновой кислоты, амино, гидрокси и С1-6алкокси; и m равно 0, 1, 2, 3 или 4, при этом D не может представлять собой незамещенный фенил, и Q не может представлять собой гидрокси, когда n равно 1, и все R5-R9 представляют собой С. 2. Соединение по п. 1, где соединение выбрано из группы, состоящей из: Стр.: 2 A 2 0 1 9 1 0 4 1 6 1 A 2 0 1 9 1 0 4 1 6 1 R U R U Стр.: 3 A 2 0 1 9 1 0 4 1 6 1 A 2 0 1 9 1 0 4 1 6 1 R U R U Стр.: 4 или их фармакологически приемлемых соли, стереоизомера, диастереомера, энантиомера, рацемата, гидрата и/или сольвата. 3. Соединение формулы: ...

N-aryl cyclic imides preparation

N-aryl imides of the formula CO-N(Aryl)-CO-A (where A is an opt. subst. divalent hydrocarbon residue, residue with 2 or 3 C-atoms between the two carbonyl gps. and Aryl is an opt. subst. carbocyclic or heterocyclic aromatic residue), which are useful as intermediates (e.g. for dyes, pesticides and medicines) are prepd. in excellent yield by either (a) reacting a dicarboxylic acid HOOC-A-COOH or its anhydride CO-A-CO-O with an amide Aryl-NH2 or (b) intramolecularly acylating a dicarboxylic acid monoamide HOOC-A-CO-NH Aryl, the reaction in either case being carried out in the presence of a basic catalyst (pref. NEt3) at not >150 degrees C, pref. 110-150 degrees C (esp. ca 140 degrees C).

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하기 화학식 X의 4급 암모늄 화합물이 제공된다: <화학식 X> 상기 식에서, R 0 , R, R 2 및 R 3 은 각각 독립적으로 임의로 치환된 알킬, 알케닐 또는 아릴 기이고, R은 적어도 5개의 탄소 원자를 갖는 임의로 치환된 히드로카르빌 모이어티를 포함하는 포함한다. Quaternary ammonium compounds of formula (X) are provided: <Formula X> wherein R 0 , R , R 2 and R 3 are each independently an optionally substituted alkyl, alkenyl or aryl group, wherein R comprises an optionally substituted hydrocarbyl moiety having at least 5 carbon atoms. do.

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