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 ...

АМИНОБЕНЗОФЕНОНЫ

Изобретение относится к новым производным аминобензофенонов общей формулы I, обладающих свойствами ингибитора интерлейкина-1β(IL-1β) и фактора некроза опухоли(ТМР-α). Соединения могут найти применение для получения лекарственного средства для лечения и профилактики заболеваний, связанных с регулирующей системой цитокинов, таких как воспалительные заболевания. Изобретение также относится к фармацевтическим композициям и применению. В общей формуле I ! ! Х является кислородом; R1 является (C1-C3)алкилом, R2 является одним или более, одинаковыми или разными заместителями, выбранными из группы, включающей водород и галоген; R3 является одним или более, одинаковыми или разными заместителями, выбранными из группы, включающей водород и галоген, R4 является водородом, R5 является водородом, R6 является (C1-C10)алкил-гетероциклилом, (C1-C10)алкилом, (C2-C10)олефиновой группой, гетероциклилом, Y1R21, Y2R22 или Y4R24; где (C1-C10)алкил, (C2-C10)олефиновая группа замещены одним или более одинаковыми ...

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, R1 представляет собой атом водорода или С1-C4-алкил нормального или разветвленного строения, R2, R3 и R13 находятся в орто-, мета- или параположении фенильного кольца, являются одинаковыми или разными и выбраны из следующих групп: Н, ОН, OR14, галогена, CO2R9, СN, СF3, NO2, СОСH3, OSO2CF3, OSO2СН3, CONR10R11, OCOR12, где R9, R12 и R14 представляют собой C1-C4-алкил нормального или разветвленного строения, R10 и R11, одинаковые или разные, представляют собой водород или C1-C6-алкил нормального или разветвленного строения, в которой R представляет собой группу формулы Ia, в которой R4 и R5 являются одинаковыми или разными, и когда они разные, то представляют собой атом ...

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 5-АМИНО-2,4,6-ТРИИОДО- 1, 3-БЕНЗОЛКАРБОНОВОЙ КИСЛОТЫ

Использование: в медицине, в частности в качестве рентгено-контрастных веществ. Сущность изобретения: продукт - производственные 5-амино-2,4,6-трииодо-1,3-бензокарбоновой кислоты ф-лы 1, где Y простая связь или -CH2-CH2-,CH2-O,-OCH2,-CH2 или кислород; R1 и R2 разные или равные группа: HO-CH2-CH(OH)-CH2-; [HOCH2]CH;-(CH2)2OH;CH-CH2(OH)-CH(CH2 OH)- HO-CH2-CH(OH)-CH(CH2OH)-;R3-R4(3) и R водород, метил, этоксил; R5-R6 и R водород, алкил, гидроксил, метоксил, этоксил. Реагент 1: соединения ф-лы 2. Условия реакции: проведение циклизации реагента 1. Структура соединений ф-лы 1 и 2: 5 табл.

ПРОИЗВОДНЫЕ 2-ФЕНОКСИ И 2-ФЕНИЛСУЛЬФОНАМИДА С ССR3 АНТАГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ ДЛЯ ЛЕЧЕНИЯ АСТМЫ И ДРУГИХ ВОСПАЛИТЕЛЬНЫХ ИЛИ ИММУНОЛОГИЧЕСКИХ ЗАБОЛЕВАНИЙ

... 1. Производное бензолсульфонамида, имеющее формулу (I), его таутомерные и стереоизомерные формы и его соли где Х представляет О или S; R1 представляет водород, галоген, гидрокси, нитро, циано, С1-6алкоксикарбонил, амино, С1-6алкиламино, ди(С1-6алкил)амино, С1-6алканоил, фенил, С1-6алкил, необязательно замещенный одним, двумя или тремя галогенами, или С1-6алкокси, необязательно замещенный одним, двумя или тремя галогенами; R2 представляет водород, галоген, гидрокси, нитро, циано, С1-6алкоксикарбонил, С1-6алкиламино, ди(С1-6алкил)амино, С1-6 алканоил, фенил, С1-6алкил, необязательно замещенный одним, двумя или тремя галогенами, или С1-6алкокси, необязательно замещенный одним, двумя или тремя галогенами; R3 представляет водород, галоген, гидрокси, нитро, циано, амино, карбокси, тетразолил, С1-6алкокси, С1-6алкоксикарбонил, С1-6алканоил, С1-6 алканоиламино, С1-6алкил, необязательно замещенный одним, двумя или тремя галогенами или гидрокси; R4 представляет или где R40 представляет С1-6алкил, ...

ОСНОВНЫЕ ЛИНЕЙНЫЕ СОЕДИНЕНИЯ NK-2 АНТАГОНИСТА И СОДЕРЖАЩИЕ ИХ ЛЕКАРСТВЕННЫЕ ВЕЩЕСТВА

... 1. Соединение общей формулы (I) где X1 представляет собой группу -NR6-CO-, -СО-, -NR6-CS-; R1 представляет собой арильную группу, выбранную из пиридина, тиофена, бензола, нафталина, дифенила, фенилтиофена, бензотиофена, бензофурана, N-индола, замещенного группой R7, где указанная арильная группа может быть также замещенной одной или несколькими независимыми группами, выбранными из группы, состоящей из галогена, С1-С6-алкила, необязательно замещенного не более, чем тремя атомами фтора (то есть, трифторметила), С1-С6-алкилоксила, необязательно замещенного не более, чем тремя атомами фтора (то есть трифторметилоксильной группы), -ОН, -NHR7, -N(R7)2, -SR7, -CONHR7, -COR7, -COOR7, -R8COOR7, -OR8COOR7, -R8COR7, -CONHR7, -R8CONHR7, -NHCOR7, -нитро, где R7 представляет собой водород или С1-С6-алкил с неразветвленной или разветвленной цепью, и R8 представляет собой С1-С6-алкиленовую группу с неразветвленной или разветвленной цепью; R6 выбран из группы, состоящей из водорода или С1-С6-алкила с неразветвленной ...

НОВЫЕ ФЕНИЛАЛКИЛЬНЫЕ АНАЛОГИ ДИАМИНОВ И АМИДОВ

... 1. Рацемические или энантиомерно обогащенные соединения фенилалкилдиаминов или амидов формулы (I) где m имеет значение 0-2; и n имеет значение 1-4; Х и Y независимо выбраны из группы, состоящей из водорода, низшего алкила, содержащего от 1 до 8 атомов углерода, галогена, выбранного из F, Cl, Br и I, алкокси, содержащего от 1 до 3 атомов углерода, нитро, гидрокси или трифторметила; R1 и R2 независимо являются водородом, низшим алкилом, бензилом, замещенным бензилом, фенилалкилом, замещенньм фенилалкилом, бензоилом, замещенньм бензоилом, формилом, ацетилом, фенилацетилом, замещенньм фенилацетилом, метансульфонилом, бензолсульфонилом или замещенным бензолсульфонилом; и Z является 5-7-членными алифатическими циклическими соединениями аминов, включая пирролидин, пиперидин, гексаметиленимин, морфолин, 4-бензилпиперидин, N-бензилпиперазин или замещенный 4-бензоилпиперидин или их производные общей формулы (II) или (II’) где X’ и Y’ независимо выбраны из группы, состоящей из водорода, низшего алкила ...

МОЛЕКУЛЫ-ИНГИБИТОРЫ БЕЛКА УБИКВИТИН-СПЕЦИФИЧЕСКОЙ ПРОТЕАЗЫ 7

Изобретение относится к области органической химии, медицины, к молекулам-ингибиторам белка убиквитин-специфической протеазы 7 (USP7), применяемым для лечения злокачественных новообразований, причем указанные ингибиторы имеют формулы (I), где А, В, R1, R2, R3, X, z определены в формуле изобретения. Изобретение позволяет расширить арсенал ингибиторов USP7 в качестве лекарственных средств для лечения онкологических заболеваний, обеспечивает увеличение благоприятного влияния на выживаемость организмов при лечении злокачественных новообразований, например, таких как множественную миелому, колоректальный рак, рак простаты, рак яичника, рак мочевого пузыря, урогенитальный рак, плоскоклеточный рак пищевода, хронический лимфатический лейкоз, медуллобластому, рак толстой кишки, рак молочной железы, рак печени, рак почек, рак поджелудочной железы, рак легкого, нейробластому, остеосаркому или острую миелоидную лейкемию. 5 з.п. ф-лы, 19 ил., 3 табл., 10 пр.

(ПОЛИ)СУЛЬФИДСОДЕРЖАЩИЕ ПОЛИЦИТРАКОНИМИДЫ И ПОЛИИТАКОНИМИДЫ, ВУЛКАНИЗОВАННАЯ СЕРОЙ КАУЧУКОВАЯ КОМПОЗИЦИЯ, СПОСОБ ВУЛКАНИЗАЦИИ, АГЕНТ ПРОТИВ ПЕРЕВУЛКАНИЗАЦИИ, ИЗДЕЛИЕ ИЗ ВУЛКАНИЗОВАННОГО КАУЧУКА

Предложены новые (поли)сульфидсодержащие полицитраконимиды и полиитаконимиды, способ серной вулканизации каучука с применением указанных новых полицитраконимидов и полиитаконимидов, продукт серной вулканизации каучука и изделия, выполненные из этого продукта. Новые (поли) сульфидсодержащие полицитраконимиды и полиитаконимиды применяют в качестве антиреверсионных агентов в процессе серной вулканизации каучука.

СПОСОБЫ ПОЛУЧЕНИЯ N6-((2-АЗИДОЭТОКСИ)КАРБОНИЛ)ЛИЗИНА

В настоящем изобретении раскрыты методы получения N6-((2-азидоэтокси)карбонил)лизина, синтеза его промежуточных соединений и конкретные промежуточные соединения и пути их применения. N6-((2-азидоэтокси)карбонил)лизин и его два энантиомера, N6-((2-азидоэтокси)карбонил)-L-лизин и N6-((2-азидоэтокси)карбонил)-D-лизин являются пригодными для получения полипептидов и белков в качестве средств изучения и терапевтических продуктов. Способ получения целевого соединения формулы (VI) или его соли включает осуществление реакции соединения формулы (III) с кислотой. Технический результат - воспроизводимый способ, обеспечивающий высокий выход целевого продукта и увеличение безопасности применения промежуточных соединений. 8 н. и 3 з.п. ф-лы, 5 ил., 5 табл., 12 пр.

Способ получения имидов дикарбоновых кислот

Способ получения производных спиротетралинсукцинимидов

Способ получения -(аминофенил)алифатических карбоновых кислот или их солей

Способ получения производных простого дифенилового эфира

Novel diphenyl ether hydrazine derivatives, particularly 2-nitro-5 (nucleus-substituted phenoxy) phenylhydrazine derivatives are provided. They are useful as a selective herbicide having a high herbicidal activity and residual efficacy.

Способ получения производных -метил-3,4 диоксифенилаланина или их солей

Способ получения активных сульфамидов

VERFAHREN ZUR HERSTELLUNG VON SUCCINIMID

PHENYLETHYL-UND PHENYLPROPYLAMINE

(N)-alkenylation of amide-type cpds. - by reaction with alkenyl ester using platinum-Gp. metal catalyst

Prepn. of N-alkenyl derivs. (I) of amide-type cpds. of formula (II):-R-X-NH-R1 (where R and R1 are aliphatic), alicyclic, aromatic or heterocyclic gps., or together can form a ring; X is CO, SO2 or another electron-withdrawing gp.) is carried out by reacting (II) with an alkenyl ester (III) in the presence of a Pt-group metal catalyst. Cpds. (I) can be used as monomers for preparing homo-or copolymers. In an example, N-vinylcaprolactam is prepd. from caprolactam and vinyl acetate.

Neue Zwischenverbindungen zur Herstellung von Guanidinderivaten, ihre Herstellung und Verwendung

Imido-percarbonsäuren

Heilungsverfahren unter Verwendung katalytischer Antikörper

ZIELLIPOSOMEN UND VERFAHREN ZUR KUPPLUNG VON LIPOSOMEN-PROTEINEN

GUANIDINOBENZOIC ESTER DERIVATIVE, A PROCESS FOR PREPARING SAME AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

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

ERZEUGUNG EGALER FAERBUNGEN AUF GEBILDEN AUS POLYACRYLNITRIL

Verfahren zur Herstellung von Succinimid

Novel acrylic acid amides

The invention relates to novel acrylic acid amides of the formula in which A, B, R<1> and Q are as defined in the text, to processes for their preparation, and to fungicidal compositions which are characterised in that they contain compounds of the formula (I).

1,2-DIOXETAN-VERBINDUNGEN ALS CHEMILUMINESZIERENDE MARKIERUNGEN FUER ORGANISCHE UND BIOLOGISCHE MOLEKUELE.

HEMMUNG DER p38 KINASE UNTER VERWENDUNG VON SYMMETRISCHEN UND ASYMMETRISCHEN DIPHENYLHARNSTOFFEN

Schicht mit selektiv perfluorierter Oberfläche

The present invention concerns new methods for producing substrates with surfaces that are covalently linked to at least one type of hapten or biological macromolecule with reduced nonspecific biological macromolecule adsorption In another aspect the invention concerns substrates with surfaces that are covalently linked to at least one type of hapten showing reduced nonspecific interactions with circulating compounds and the use of these substrates for the quantitative detection of at least one type of haptenspecific biological macromolecule receptor in particular a haptenspecific antibody in a test probe Further the invention concerns substrates with surfaces that are covalently linked to at least one type of biological macromolecule in particular one type of antibody showing reduced nonspecific interactions with circulating compounds and the use of these substrates for the quantitative detection of at least one type of hapten in a test probe In another aspect the invention is related ...

PROCESS FOR PRODUCING DIACYLAMINOACETOANILIDE DERIVATIVES

... 1420564 Preparation of -aliphatic acyl-- diacylamino-acetanilide derivatives FUJI PHOTO FILM CO Ltd 11 Feb 1974 [15 Feb 1973] 06216/74 Heading C2C -Aliphatic acyl--diacylamino-acetanilide derivatives are obtained by reacting the corresponding -aliphatic acyl--halogenoacetanilide derivative with the corresponding diacylamine derivative in the presence of a base (e.g. NaOH, KOH, (C 2 H 5 ) 3 N, diazabicyclooctane) and in an organic amide (e.g. lactam, urea) or sulphoxide as solvent. [Aliphatic acyl denotes that the carbonyl carbon is attached to a non-aromatic carbon atom.] Preferred solvents are those having a dielectric constant at 20‹ C. of 30 or more, particularly dimethylformamide, dimethylsulphoxide, dimethylacetamide, hexamethylphosphoramide, N-methyl-2-pyrrolidone and tetramethylurea. The following reaction sequences illustrate the condensation wherein R1 is an alkyl, alkenyl, cycloalkyl or aralkyl radical, R2 is an aromatic radical, X is a halogen atom and Z represents ...

AROMATIC AMIDES AND THEIR USE AS COUPLERS FOR PHOTOGRAPHIC MATERIALS

... 1310627 Amides KONISHIROKU PHOTO INDUSTRY CO Ltd 14 May 1971 [14 May 1970] 15018/71 Heading C2C [Also in Division G2] The invention comprises compounds of the formula where X is H, halogen, alkoxy of 1-4 carbon atoms, alkyl of 1-4 carbon atoms or aryloxy, Y is COOR 2 , COOCH(R 1 )-COOR 2 , NHCOR 3 or where R 1 is alkyl of 1-4 carbon atoms, R 2 is hydrocarbyl of 8-18 carbon atoms and COR 3 is acyl of 9-25 carbon atoms. The compounds are prepared by reacting together compounds of the formulae ...

Compounds containing a dicarboximido group

The invention comprises compounds of formula where R1 is H or C1- 4 alkyl which may be substituted, R3 is a straight or branched chain alkylene group, X is halogen or a C1- 4 alkyl or alkoxy group, n is 1-4 and Y is the atoms necessary to complete a dicarboximido group. The compounds are prepared by condensing an N-aminoalkyl-tetrahydroquinoline with a dicarboxylic acid anhydride and are used in the preparation of azo dyes (see Specification 1,073,227). In examples, the preparation of N - b - succinimidoethyl - 2,7 - dimethyl1,2,3,4 - tetrahydroquinoline and N-b -succinimidoethyl - 1,2,3,4 - tetrahydroquinoline is described.

Improvements in or relating to aryloxy propanols and the manufacture thereof

Novel 1 - amino - 3 - aryloxy - 2 - propanols of the general formula wherein R is hydrogen, C1- 6 alkyl, C1- 6 alkoxy, halogen, trifluoromethyl, nitro, phenyl or styryl and R1 is hydrogen or C1- 6 alkyl, are prepared by (a) reacting ammonia with the corresponding 1,2 - epoxy - 3 - aryloxypropane, or (b) hydrolysing the corresponding N-[3-aryloxy-2-hydroxypropyl] succinimide, or (c) reacting hexamethylene tetramine with the 1,2-epoxy-3-aryloxypropane and hydrolysing the resulting addition product, or (d) hydrogenolysis of an N - benzylamino - 3 - aryloxy - 2 - propanol. Methods (a), (b) and (c) are used for compounds where R1 is hydrogen and method (d) where R1 is C1- 6 alkyl.

Cyclohexene Derivatives and Process for the Preparation thereof

... 1,177,616. Rodenticides containing cyclohexenedicycloximides. CHINOIN GYOGYSZER ES VEGYESZETI TERMEKEK GYARA R.T. 11 Jan., 1967 [20 Jan., 1966; 26 Jan., 1966], No. 1499/67. Heading ASE. '[Also in Division C2] Rodenticidal compositions comprise at least one compound of the general formula: or the corresponding N-unsubstituted analogues or a salt thereof (where A is -O-, -CH 2 - or =C=CR 1 R 2 or where A is replaced by hydrogen atoms in positions 3 and 6, R 1 and R 2 are phenyl or pyridyl groups which can be substituted by a nitro, amino or halo group and B is a hydrogen atom or the group -C(OH)R 1 R 2 provided that, in the N- carbamyl compounds, if A is -CH 2 -, B is not hydrogen) as active ingredient are made up in combination with suitable solid or liquid carriers and may be the form of powders, sprays, solutions, emulsions or suspension. Preferred compounds are N-carbamoyl-5-(-hydroxy--Z-pyridylbenzyl)-7- (-2-pyridylbenzylidene)-5-norbornene-2, 3-dicarboximide, N-carbamoyl-endo-cis-3, ...

SUBSTITUTED (4-HYDROXYPHENYLTHIOALKYL) DERIVATIVES AND THEIR USE AS STABILIZER FOR POLYMERIC MATERIALS

SUBSTITUTED 1-ARYLAMINE-2,BETA-DICYANBUTANES AND THEIR USE AS DYESTUFF INTERMEDIATES

... 1418211 N - (2,4 - dicyanobutyl)arylamines GAF CORP 4 May 1973 [16 May 1972] 21433/73 Heading C2C [Also in Division C4] The invention comprises compounds of general Formula I wherein Ar is an aryl radical devoid of substituents in the position para to the amine substituent and R a hydrogen atom or an optionally substituted alkyl group and also the quaternary ammonium salts, cyclic amides and cyclic imides of those compounds in which R contains an amino group such as are represented by (i) general Formulae VII wherein Ar is naphthyl or a phenyl radical of Formula II wherein R 1 and R 2 are independently hydrogen C 1-7 alkyl, C 1-7 alkoxy, halogen, CF 3 , R 3 CONH or R 3 OCO wherein R 3 is C 1-7 alkyl or phenyl; R 5 is a straight or branched C 1-7 alkylene group and -#N(R 4 ) 3 is -#N(R 4 1,R 4 11,R 4 111) in which R 4 1, B 4 11 and R 4 111 are independently C 1-5 alkyl or C 7-14 aralkyl or -#N(R 4 ) 3 is a group of Formula (A) in which ...

Process for the preparation of substituted oxazolidones

Oxazolidones-(2) substituted in the 5-position are prepared by reaction of triglycidyl isocyanurate of the general formula at elevated temperatures with organic nitrogen containing compounds which contain a hydrogen atom capable of reacting with epoxide compounds attached to the nitrogen atom, for example secondary amines, heterocyclic nitrogen compounds, open chain or cyclic sulphonic or carboxylic acid amides, open chain or cyclic imides, which may also contain substituents which are insert to or react only slowly with epoxides. Novel products include 5-[(N-methyl-N-phenyl) - aminomethyl] - oxazolidone - (2), N (p nitrophenyl) - N - [(oxazolidone - (2) - yl - (5)) - methyl] - acetamide, 5 - (phthalimidomethyl) - oxazolidone - (2), N - methyl - N - [(oxazolidone - (2) - yl - (5)) - methyl] - p - toluenesulphonamide, N - [(oxazolidone - (2)-yl - (5)) - methyl] - saccharin, 5 - piperidinomethyl - oxazolidone - (2) and 5 - morpholinomethyl-oxazolidone-(2). Tris - (2 - ...

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< ...

Crysanthemic acid esters, methods of making them, and insecticidal compositions including them

The invention comprises crysanthemic acid esters of the formula wherein G represents in which R1 and R2 are hydrogen or a methyl group, R3 and R4 are hydrogen or a methyl or phenyl group; and R5 is hydrogen or a methyl or ethyl group. The compounds are made by esterification, using known methods, of crysanthemic acid with an imide of the formula Specified methods include (a) esterification using an acid catalyst with azeotropic removal of water, (b) tranesterification of the methyl, ethyl or propyl esters of the acid in the presence of a basic catalyst, (c) reacting the hydroxy imide with the acid halide in the presence of a tertiary base, (d) refluxing the imide with the acid anhydride, (e) reacting the imide derivative of the formula in which A is halogen, with free acid in the presence of a tertiary amine, or with an alkali metal or ammonium salt of the acid. The esters are used as insecticides (see Division ...

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.

METAL SALT AMINE XOMPLEXES

Hydroxamic acid derivatives as inhibitors of the production on human cd23 and of the tnf release

Pre-organized tricyclic integrase inhibitor compounds

Pre-organized tricyclic anhibitor coumpounds

Hydroxamic acid derivatives as inhibitors of the production of human CD23 and of the tnf relaease.

Compounds of formula (i)wherein: r is methyl substituted by one to three groups selected from alkyl, aryl, alkenyl, and alkynyl, n is 0 or 1, r1 is arylmethyl or heterocyclmethyl, r2 is alkyl, alkenyl, cycloalkyl or cycloalkenyl, and r3 is hydrogen, alkyl, alkenyl, alkynyl or aryl; are useful in the treatment of disorders mediated by s-cd23.

Pre-organized tricyclic integrase inhibitor compounds

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

TERTIARY AMINOACIDS, PROCESS FOR THEIR MANUFACTURE AND COMPOSITIONS CONTAINING THEM

Method of preparation of cyclic tertiary amoebas.

Hydroxamic acid derivatives as inhibitors of the production of human cd23 and of the tnf release.

New nitrogenized heterocyclic compounds, compositions the container, their preparation and their application to reduce the loss of moisture of plants and to increase the output of cultures.

Pesticidal polyhaloalkene derivative.

Pre-organized tricyclic integrase inhibitor compounds.

Esters of acid amino.

Tertiary amino-acids.

Process for the preparation of tertiary amino-acids.

Pre-organized tricyclic integrase inhibitor compounds

Hydroxamic acid derivatives as inhibitors of the production on human cd23 and of the tnf release

PROCEDURES FOR the PRODUCTION OF NEW ONE, HETERO-CYCLIC SUBSTITUTED 5-SULFAMOYLBENZOESAEUREDERIVATEN AND YOUR SALTS

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. ...

Procedure for the production of new hetero-cyclic connections and their salts

Procedure for the production of new hetero-cyclic connections and their salts

INITIATOR FUR THE LIVING RADICAL POLYMERIZATION WITH A TO REACTION WITH POLYPEPTIDEN OR SUCH BEFAHIGTEN FUNCTIONAL GROUP, THEREBY PRESERVATION COMB POLYMER, POLYPETIDKONJUGATE AND FROM THIS PRESERVATION MEDICINE MATERIAL

MASS MARKINGS

PROCEDURE FOR THE IDENTIFICATION OF PROTEINS NON--PURPOSEFUL ON DRUGS

CARBAMINSÄUREDERIVATE CONTAINING AN AMIDE GROUP FOR THE TREATMENT OF MALARIA

VERFAHREN ZUR HERSTELLUNG VON NEUEN HETEROCYCLISCH SUBSTITUIERTEN 5-SULFAMOYL- BENZOESAEUREDERIVATEN UND IHREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN, HETEROCYCLISCH SUBSTITUIERTEN 5-SULFAMOYLBENZOESAEUREDERIVATEN UND IHREN SALZEN

FETTALKOHOL DRUG KONJUGATE ONE

PROCEDURES FOR the PRODUCTION OF NEW ONE, HETERO-CYCLIC SUBSTITUTED 5-SULFAMOYLBENZOESAEUREDERIVATEN AND YOUR SALTS

INHIBITORS OF MYCOBAKTERIEN

PROCEDURES FOR the PRODUCTION OF NEW HETERO-CYCLIC SUBSTITUTED 5-SULFAMOYL BENZOIC ACID DERIVATIVES AND YOUR SALTS

PROCEDURE FOR THE PRODUCTION OF NEW SUBSTITUTED BENZYLE AMINES AND OF THEIR SALTS

PROCEDURE FOR THE PRODUCTION OF N-SUCCINIMIDYLCARBONATEN

NEW INTERMEDIATE CONNECTIONS TO THE PRODUCTION OF GUANIDINDERIVATEN, YOUR PRODUCTION AND USE

MARKING OF PROTEINS

VERFAHREN ZUR HERSTELLUNG VON N-SUCCINIMIDYLCARBONATEN

TITANOCENE, THEIR USE AND N-SUBSTITUTING FLUORANILINE.

9-ANTHRYLALKYL-VERBINDUNGEN, YOUR PRODUCTION AND YOUR USE.

PROCEDURE FOR the PRODUCTION OF 5-GLIEDRIGEN, NITROGENOUS ONE HETERO AROMATICS.

PROCEDURE FOR the PRODUCTION OF 2-OXO-PYRROLIDIN N-ALKYLAMIDEN

PROCEDURE FOR THE PRODUCTION OF NEW PEPTID DERIVATIVES

COMPOSITIONS, CONCENTRATES, LUBRICANT PREPARATIONS, FUEL PREPARATION AND IMPROVEMENT PROCEDURE THE FUEL ECONOMY OF COMBUSTION ENGINES.

PHTHALIMIDOPEROXIHEXANSÄURE, PROCEDURE FOR THEIR PRODUCTION AND THEIR USE

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

HEXAHYDROPYRROLO (2,1-A) ISOCHINOLINDERIVATE.

GUANIDINOBENZOESAEUREESTERDERIVATE, A PROCEDURE FOR THEIR PRODUCTION AND THESE CONTAINING PHARMACEUTICAL COMPOSITIONS.

BIFUNCTIONAL KUPPLER.

COMPOSITIONS, CONCENTRATES, LUBRICANT COMPOSITION, FUEL COMPOSITION, AND IMPROVEMENT PROCEDURE THE FUEL ECONOMY OF COMBUSTION ENGINES

Procedure for the Verätherung alcoholic hydroxyl groups of basic connections

N-ACYLSULFONAMID-APOPTOSIs-PROMOTER

Procedure for the production of new hetero-cyclic connections and their salts

Procedure for the production of new hetero-cyclic connections and their salts

NEW PLEUROMUTILINDERIVATE

2-Phenoxy- and 2-Phenylsulfonamide Derivatives with CCR3 Antagonistic Activity for the Treatment of Inflammatory or Immunological Disorders

Provided herein are 2-phenoxy- and 2-phenylsulfonamide derivatives with CCR3 antagonistic activity. These compounds are useful for the treatment of diseases associated with CCR3 activity, including but not limited to, atopic dermatitis, allergic rhinitis, rheumatoid arthritis, Grave's disease, HIV infection, Alzheimer's disease, atherosclerosis and other inflammatory and/or immunological disorders. 117.-. (canceled)22. The method of claim 18 , wherein the compound claim 18 , its tautomeric or stereoisomeric form claim 18 , or a physiologically acceptable salt thereof claim 18 , is selected from the group consisting of:(R)—N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-5-cyano-2-(3,5-dichloro-phenoxy)-benzenesulfonamide;(S)—N-(1-Aza-bicyclo[2.2.2]oct-3-yl)-5-cyano-2-(3,5-dichloro-phenoxy)-benzenesulfonamide;N-(1-aza-bicyclo[2.2.2]oct-3-yl)-2-(3,5-dichloro-phenylsulfanyl)-5-nitro-benzenesulfonamide; and(R)-5-cyano-2-(3,5-dichlorophenoxy)-N-(2-(2,5-dioxopyrrolidin-1-yl)ethyl)-N-(1-aza-bicyclo[2.2.2]oct-3-yl)benzenesulfonamide.23. The method of claim 18 , wherein the compound claim 18 , its tautomeric or stereoisomeric form claim 18 , or a physiologically acceptable salt thereof is formulated with one or more pharmaceutically acceptable excipients.24. The method of claim 23 , wherein the excipient is an inert substance selected from the group consisting of a carrier claim 23 , a diluent claim 23 , a flavoring agent claim 23 , a sweetener claim 23 , a lubricant claim 23 , a solubilizer claim 23 , a suspending agent claim 23 , a binder claim 23 , a tablet disintegrating agent and an encapsulating agent. The present invention relates to a benzenesulfonamide derivative, which is useful as an active ingredient of pharmaceutical preparations. The benzenesulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor 3) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of ...

Methods and compositions for radiohalogen protein labeling

Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [ 125 I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.

AMINOBENZOIC ACID DERIVATIVES FOR USE AS ANTI-INFLAMMATORY AGENTS, ANTI-METASTATIC AGENTS AND/OR ANTICANCER AGENTS

There are provided compounds of formula (I) 113-. (canceled)1538-. (canceled)39. The method of claim 57 , wherein said cancer cell growth is inhibited by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to an untreated subject.40. (canceled)41. The method of claim 57 , wherein a relative STAT1 activation of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.42. The method of claim 57 , or wherein a relative STAT3 activation of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.43. The method of claim 57 , wherein a CD40 expression of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.44. The method of claim 57 , wherein a MHC-II expression of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.45. The method of claim 57 , wherein a production of NO of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 , about 60% claim 57 , about 70% or about 80% relative to untreated cancer cells.46. The method of claim 57 , wherein TNFα/NFκB and/or IL6/STAT3 signaling pathways of said cells is decreased by at least about 10% claim 57 , about 20% claim 57 , about 30% claim 57 , about 40% claim 57 , about 50% claim 57 ...

HYDROXYAROMATIC SUCCINIMIDE DETERGENTS FOR LUBRICATING COMPOSITIONS

A lubricating composition includes an oil of lubricating viscosity and an N-substituted hydroxyaromatic succinimide or a salt thereof. 1. A lubricating composition comprising:an oil of lubricating viscosity; andan N-substituted hydroxyaromatic succinimide or a salt thereof.2. The composition of claim 1 , wherein the hydroxyaromatic succinimide includes a hydrocarbyl group of at least 8 carbon atoms.3. The composition of claim 1 , wherein the hydrocarbyl group is attached to the succinimide ring.4. The composition of claim 1 , wherein the hydrocarbyl group is a linear alkyl or linear alkenyl group.5. The composition of claim 1 , wherein the hydroxyaromatic succinimide is a succinimide derivative of a hydroxyaromatic amine.6. The composition of claim 5 , wherein the hydroxyaromatic amine is an aminophenol.8. The composition of claim 7 , wherein Ris selected from hydrocarbyl groups of at least 10 or at least 12 claim 7 , or at least 14 claim 7 , or at least 16 claim 7 , or at least 18 carbon atoms.9. The composition of claim 7 , wherein Ris selected from hydrocarbyl groups of up to 30 carbon atoms claim 7 , or up to 28 carbon atoms claim 7 , or up to 26 carbon atoms claim 7 , or up to 24 carbon atoms claim 7 , or up to 22 carbon atoms.10. The composition of claim 7 , wherein Ris selected from alkyl and alkenyl groups of at least 10 carbon atoms claim 7 , or at least 12 carbon atoms claim 7 , or at least 14 carbon atoms claim 7 , or at least 16 carbon atoms claim 7 , or at least 18 carbon atoms.11. The composition of claim 7 , wherein Ris selected from alkyl and alkenyl groups of up to 30 carbon atoms claim 7 , or up to 28 carbon atoms claim 7 , or up to 26 carbon atoms claim 7 , or up to 24 carbon atoms claim 7 , or up to 22 carbon atoms.12. The composition of claim 7 , wherein Ris selected from linear alkyl and alkenyl groups.13. The composition of claim 7 , wherein n is 0.14. The composition of claim 7 , wherein n is at least 1 and Ris selected from alkyl and alkenyl ...

METHOD FOR CONVERSION OF DIAMMONIUM SUCCINATE IN FERMENTATION BROTH TO 2-PYRROLIDONE AND N-METHYLPYRROLIDONE

This invention relates to a process for preparing 2-pyrrolidone (also called 2-pyrrolidinone) and N-methylpyrrolidone (also called N-methylpyrrolidinone) from diammonium succinate in fermentation broth. In the first stage of this invention, renewable carbon resources are utilized to produce diammonium succinate through biological fermentation. In the second stage of this present invention, diammonium succinate is converted into 2-pyrrolidone and N-methylpyrrolidone through a two step reaction. Both the steps of the reaction leading to the production of 2-pyrrolidone and N-methylpyrrolidone are carried out in a solvent phase to prevent the loss of succinimide through hydrolysis. 1. A process for preparing succinimide comprising the steps of:(a) providing a fermentation broth comprising diammonium succinate;(b) adding a polar organic solvent with boiling point higher than that of water to said fermentation broth;(c) evaporating water in said fermentation broth;(d) raising temperature of said fermentation broth to at least 120° C. to convert said diammonium succinate to succinimide.2. The Process according to claim 1 , wherein said fermentation broth is a concentrated fermentation broth.3. The process according to claim 1 , wherein said fermentation broth is subjected to ultrafiltration process before converting diammonium succinate to succinimide.4. The process according to claim 1 , wherein said fermentation broth is subjected to adsorption process to remove sugars and amino acids in the fermentation broth.5. The process according to claim 1 , wherein said polar organic solvent is selected from a group consisting of diglyme claim 1 , triglyme claim 1 , tetraglyme claim 1 , propylene glycol claim 1 , dimethylsulfoxide claim 1 , dimethylformamide claim 1 , dimethylacetamide claim 1 , dimethylsulfone claim 1 , sulfolane claim 1 , polyethylene glycol claim 1 , butoxytriglycol claim 1 , N-methylpyrrolidone claim 1 , 2-pyrrolidone claim 1 , gammabutyrolactone claim 1 , ...

CRYSTAL FORM A OF 2-(2, 5-DIOXOPYRROLIDIN-1YL) ETHYL METHYL FUMARATE, PREPARATION METHOD THEREFOR AND USE THEREOF

A crystal form A of 2-(2, 5-dioxopyrrolidin-1yl)ethyl methyl fumarate has a good light irradiation stability, high-temperature stability and high-humidity stability. 1. A crystal form A of 2-(2 , 5-dioxopyrrolidin-1yl)ethyl methyl fumarate , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has characteristic peaks at 2θ diffraction angles of 13.5±0.2° , 17.9±0.2° , 23.0±0.2° and 27.3±0.2°.2. The crystal form A of claim 1 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 13.3±0.2° claim 1 , and 18.2±0.2°.3. The crystal form A of claim 2 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 19.3±0.2° claim 2 , and 19.6±0.2°.4. The crystal form A of claim 3 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 16.6±0.2° claim 3 , 20.9±0.2° claim 3 , 22.0±0.2° claim 3 , 24.3±0.2° claim 3 , 25.3±0.2° claim 3 , and 30.6±0.2°.5. The crystal form A of claim 4 , wherein the X-ray powder diffraction thereof using Cu-Kα radiation has further characteristic peaks at 2θ diffraction angles of 6.92±0.2° claim 4 , 11.5±0.2° claim 4 , 16.1±0.2° claim 4 , 23.7±0.2° claim 4 , 26.9±0.2° claim 4 , and 31.1±0.2°.9. The crystal form A of claim 1 , wherein the crystal form A has an X-ray powder refraction pattern substantially as shown in .10. The crystal form A of claim 1 , wherein the crystal form A has a characteristic endothermic peak in a temperature range of 96.0° C.-107.0° C. measured by differential scanning calorimetry.11. The crystal form A of claim 1 , wherein the crystal form A has a differential scanning calorimetry curve substantially as shown in .12. The crystal form A of claim 1 , wherein the crystal form A has a weight loss of less than 0.01% before a temperature of 125° C. in its thermo gravimetric analysis curve.13. The ...

PROCESSES FOR THE CONVERGENT SYNTHESIS OF CALICHEAMICIN DERIVATIVES

This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates. 2. The process of wherein the purifying of step (e) comprises the use of reverse phase high performance liquid chromatography having a mobile phase of about pH 7.0 to 9.0 followed by normal phase chromatography.5. The process of wherein the purifying of step (e) comprises the use of a reverse phase high performance liquid chromatography having a mobile phase of about pH 7.0 to 9.0 followed with a normal phase chromatography.9. A process according to claim 1 , wherein Alkis an alkylene of 2 to 5 carbon atoms claim 1 , and Spis an oxygen atom.10. A process according to claim 9 , wherein Alkis an alkylene of 3 carbon atoms.11. A process according to claim 1 , wherein Zis alkyl of 1 to 3 carbon atoms.12. A process according to claim 1 , wherein Ar is 1 claim 1 ,2- claim 1 , 1 claim 1 ,3- claim 1 , or 1 claim 1 ,4-phenylene claim 1 , or 1 claim 1 ,2- claim 1 , 1 claim 1 ,3- claim 1 , 1 claim 1 ,4- claim 1 , 1 claim 1 ,5- claim 1 , 1 claim 1 ,6- claim 1 , 1 claim 1 ,7- claim 1 , 1 claim 1 ,8- claim 1 , 2 claim 1 ,3- claim 1 , 2 claim 1 ,6- claim 1 , or 2 claim 1 ,7-naphthylidene.13. A process according to claim 12 , wherein Ar is 1 claim 12 ,4-phenylene.14. A process according to claim 1 , wherein Q is —NNHCO—.15. A process according to claim 1 , wherein Sp is straight or branched-chain divalent or trivalent alkyl radical of 1 to 12 carbon atoms.16. A process according to claim 15 , wherein Sp is straight or branched-chain divalent or trivalent alkyl radical of 1 to 6 carbon atoms.17. The process according to claim 1 , wherein the alcohol solvent is methanol.18. The process according to claim 1 , wherein the inert solvent is acetonitrile.19. The process according to claim 1 , wherein alkyl carboxylic acid is acetic acid.20. The process according to claim 1 , wherein the inert organic solvent is ...

ANTIFIBRINOLYTIC COMPOUNDS

The present invention provides novel antifibrinilytic compounds, processes for their preparation, pharmaceutical and veterinary compositions thereof, and their use in medicine, in particular for the treatment of bleeding. 1. A compound of formula III:{'br': None, 'sup': 1', '1', '5, 'sub': '2', 'R—CH—X—R\u2003\u2003(III)'} [{'sup': 1', '6', '6', '7', '+', '6', '7', '8', '+', '9', '10, 'sub': '2', 'Ris —NH, —NHR, NRR—NRRRor —SRR;'}, {'sup': 5', '12', '13', '14', '15, 'sub': '2', 'Ris —C(O)R, —SOR, —P(O)RR, nitro or nitroso;'}, {'sup': 6', '7', '9', '10', '6', '7, 'sub': 1', '4', '1', '4, 'R, R, R8, Rand Rare independently (C-C)alkyl or halo(C-C)alkyl, or Rand R, together with the N atom to which they are attached form an aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, or pyrrolyl group;'}, {'sup': 12', '13', '14', '15, 'sub': 1', '4', '1', '4, 'R, R, Rand Rare independently hydroxyl, —O—(C-C)alkyl or —(C-C)alkyl; and'}, {'sup': '1', 'Xis trans cyclohexan-1,4-diyl;'}, {'sup': 1', '2, 'sub': '2', 'with the proviso that Rin not NHwhen Ris COOH, or'}, 'a pharmaceutically acceptable salt thereof., 'wherein2. The compound of claim 1 , of formula IIIa:{'br': None, 'sup': 9', '10', '+', '5, 'sub': '2', 'RRS—CH—X—R\u2003\u2003(IIIa)'}or a pharmaceutically acceptable salt thereof.3. The compound of claim 1 , of formula IIIb:{'br': None, 'sup': 9', '10', '+', '1', '12, 'sub': '2', 'RRS—CH—X—C(O)R\u2003\u2003(IIIb)'}or a pharmaceutically acceptable salt thereof.4. The compound of claim 1 , wherein Ris hydroxyl or —O—(C-C)alkyl or a pharmaceutically acceptable salt thereof.5. The compound of claim 4 , wherein Ris hydroxyl claim 4 , or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein. Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 1 , or a pharmaceutically acceptable salt thereof.7. The compound of claim 6 , wherein Rand Rare both methyl claim 6 , or a pharmaceutically acceptable salt thereof. This application claims priority ...

PROCESS FOR MICROWAVE ASSISTED SYNTHESIS OF N-METHYL PYRROLIDONE

The present invention relates to a process for microwave assisted synthesis of N-methyl pyrrolidone (NMP). Particularly the process relates to the synthesis of N-methyl succinimide or corresponding analogues by using microwave irradiation which on hydrogenation in the presence of a hydrogenating catalyst gives N-methyl pyrrolidone. Compared to the conventional heating microwave process requires less energy inputs and reduces the reaction time drastically from 5-6 h to 2-5 min. 1. A process for synthesis of N-methyl pyrrolidone , said process comprising the steps of:(a) reacting a dicarboxylic acid or corresponding anhydride with non-aqueous methylamine with a molar ratio in the range 1:1 to 1:10 in solid state using microwave irradiation in the range of 600-900 W for a period of 1 to 10 minutes to obtain an intermediate N-methyl imide;(b) separating and purifying the intermediate N-methyl imide thus formed; and(c) converting the intermediate N-methyl imide to N-methyl pyrrolidone.2. The process according to claim 1 , wherein said dicarboxylic acid or anhydride is selected from the group consisting of maleic acid claim 1 , maleic anhydride claim 1 , succinic acid claim 1 , succinic anhydride and an analog thereof.3. The process according to claim 1 , wherein said non aqueous methylamine is selected from the group consisting of anhydrous methylamine claim 1 , methylamine in THF and methylamine hydrochloride.4. The process according to claim 1 , wherein an organic solvent is used for separating the intermediate N-methyl imide thus formed.5. The process according to claim 4 , wherein the organic solvent is selected from the group consisting of chloroform claim 4 , ethyl acetate claim 4 , dichloromethane and toluene.6. The process according to claim 1 , wherein purifying the intermediate N-methyl imide comprises subjecting the intermediate N-methyl imide to a crystallization process.7. The process according to claim 1 , wherein converting the intermediate N-methyl imide ...

SUBSTITUTED B-AMINO ACID DERIVATIVES AS CXCR3 RECEPTOR ANTAGONISTS

The present invention relates to compounds of formula 1 3. A compound according to claim 1 , wherein Rrepresents hydrogen.6. A compound according to claim 1 , wherein X represents an O atom.7. A compound according to claim 1 , wherein Y represents halogen or a —CH claim 1 , —CHor —OCHgroup.8. A compound according to claim 7 , wherein Y represents Cl claim 7 , F or a —CH claim 7 , —CHor —OCHgroup.9. A compound according to claim 1 , wherein Z represents a (CH) claim 1 , CHN(CH) or CH═N(CH) group.10. A compound according to claim 9 , wherein Z represents a (CH)group.11. A compound according to claim 1 , wherein{'sub': 1-4', '3-6, 'R represents hydrogen or a —Calkyl, —Ccycloalkyl or fluorophenyl group; and'}R′ represents hydrogen.15. A method for the preventive or therapeutic treatment of a CXCR3 receptor mediated disease or disorder claim 1 , the method comprising the administration to a patient in need thereof of a pharmaceutically effective amount of a compound according to .16. The method according to wherein the disease or disorder is selected from the group consisting of COPD claim 15 , psoriasis claim 15 , graft/transplant rejection claim 15 , ophthalmological disease claim 15 , celiac disease claim 15 , inflammatory bowel disease (IBD) claim 15 , type 1 diabetes claim 15 , myasthenia gravis (MG) claim 15 , multiple sclerosis (MS) and other neuroinflammatory diseases claim 15 , lupus claim 15 , rheumatoid arthritis (RA) and lichen planus.17. A pharmaceutical composition comprising at least one compound according to and at least one pharmaceutically acceptable excipient. The present invention relates to compounds that are useful as an active ingredient of a medicament for preventive and/or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines.Chemokines are a large family of small soluble proteins of about 8 to 10 kDa in size. One of the major roles of chemokines is to direct the migration of immune cells. The mechanism by which the ...

SUBSTITUTED ISOINDOLINE-1,3-DIONE DERIVATIVES

This invention relates to novel substituted isoindoline-1,3-dione derivatives and pharmaceutically acceptable salts thereof. More specifically, the invention relates to novel substituted isoindoline-1,3-dione derivatives that are analogues of apremilast. This invention also provides compositions comprising a compound of this invention and a carrier and the use of disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering apremilast. 2. The compound of claim 1 , wherein Ris CHor CD; and Yis H.6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. The compound of claim 1 , wherein Ris CDCD.14. A compound of claim 13 , having predominantly the (S) configuration.15. A compound of claim 13 , having predominantly the (R) configuration.17. A compound of claim 1 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.18. A composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt of said compound; and an acceptable carrier.19. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt of said compound; and an acceptable carrier claim 1 , wherein the composition is suitable for the treatment of a disease selected from the group consisting of septic shock claim 1 , sepsis claim 1 , endotoxic shock claim 1 , hemodynamic shock and sepsis syndrome claim 1 , post ischemic reperfusion injury claim 1 , malaria claim 1 , mycobacterial infection claim 1 , meningitis claim 1 , psoriasis claim 1 , sarcoidosis claim 1 , psoriatic arthritis claim 1 , Behçet's Disease claim 1 , prurigo nodularis claim 1 , lupus claim 1 , uveitis claim 1 , congestive heart failure claim 1 , fibrotic disease claim 1 , cachexia claim 1 , graft rejection claim 1 , cancer claim 1 , autoimmune disease claim 1 , opportunistic infections in AIDS claim 1 , ...

Inactivation Method

The present invention relates to the field of thermostable enzymes, methods for their inactivation, and related uses, kits and reagents. In particular, the invention relates to a method for reversible inactivation of thermophilic enzymes by chemical modification under aqueous or non-aqueous conditions.

New nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio)molecules; precursors and conjugates thereof

Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio) molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conformconform.torespective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.

AMINOBENZOIC ACID DERIVATIVES FOR USE AS ANTI-INFLAMMATORY AGENTS, ANTI-METASTATIC AGENTS AND/OR ANTICANCER AGENTS

There are provided compounds of formula (I) in which R, R, R, Rand Q can represent various different possibilities. These compounds can be useful as anticancer agents as well as anti-inflammatory agents, anti-proliferative agents and/or anti-metastatic agents. 3. The compound of claim 2 , wherein{'sub': '2', 'Ris H, unsubstituted member chosen from acetyl and propiolyl;'}{'sub': 'A', 'Q is Q;'}{'sub': '5', 'Ris H, unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': '6', 'Ris Boc, H, or an unsubstituted member chosen from acetyl and propiolyl.'}5. The compound of claim 4 , wherein{'sub': '2', 'Ris H, unsubstituted member chosen from acetyl and propiolyl;'}{'sub': 'A', 'Q is Q;'}{'sub': '5', 'Ris H, unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': '6', 'Ris Boc, H, or an unsubstituted member chosen from acetyl and propiolyl.'}7. The compound of claim 6 , wherein{'sub': '2', 'Ris H, unsubstituted member chosen from acetyl and propiolyl;'}{'sub': 'A', 'Q is Q;'}{'sub': '5', 'Ris H, unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': '6', 'Ris Boc, H, or an unsubstituted member chosen from acetyl and propiolyl.'}9. The compound of claim 8 , wherein{'sub': '2', 'Ris H or unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': 7', '1', '8', '3', '6, 'Ris an unsubstituted member chosen from C-Calkyl, C-Ccycloalkyl, phenyl, furanyl, thiophenyl, pyridinyl, naphthyl, quinolyl and isoquinolyl.'}11. The compound of claim 10 , wherein{'sub': '2', 'Ris H or an unsubstituted member chosen from acetyl and propiolyl; and'}{'sub': 7', '1', '8', '3', '6, 'Ris an unsubstituted member chosen from C-Calkyl, C-Ccycloalkyl, phenyl, furanyl, thiophenyl, pyridinyl, naphthyl, quinolyl and isoquinolyl.'}1535-. (canceled)36. A method for treating cancer or at least one cancer chosen from melanoma claim 1 , breast cancer claim 1 , uterine cancer claim 1 , ovarian cancer claim 1 , prostate cancer and bladder cancer claim 1 , said ...

BISMALEIMIDE RESINS FOR ONE DROP FILL SEALANT APPLICATION

The present invention relates to curable novel bismaleimide resins and prepolymers, methods of manufacture. Particularly useful applications include one drop fill sealant used in liquid crystal assembly. In particular, the inventive polymers and compositions are useful in the assembly of LCD panels. The present invention relates to monomers and oligomers useful as sealants and particularly as one drop fill sealants for liquid crystal applications. In particular, the present invention permits assembly of LCD panels without migration of the sealant resin into the liquid crystal or vice versa during LCD assembly and/or curing of the resin.The one drop fill (“ODF”) process is becoming the mainstream process in the assembly of LCD panels in display applications, replacing the conventional vacuum injection technology to meet faster manufacturing process demands. In the ODF process, first, a sealant is dispensed on an electrode-equipped substrate to form a frame of a display element, and liquid crystals are dropped inside the depicted frame. In the next step of the assembly, another electrode equipped substrate is joined thereto under vacuum. Then, the sealant undergoes a curing process, either by a combination of UV and thermal or by thermal only process.The ODF method has a few problems in that the sealant material in the uncured state comes into contact with the liquid crystal during the assembly process. This could cause reduction in electro-optical properties of the liquid crystal by resin migration into the liquid crystal or vice versa, or because of ionic impurities that may be present. Hence, design of resin systems for sealant material that show good liquid crystal resistance (less contamination) along with good adhesion and moisture barrier properties has remained a challenge.The present invention relates to unique resins and ODF compositions made therefrom.In one aspect of the invention there is provided a resin comprising the structure I:In another aspect of ...

ALKENYL SUCCINIMIDES AND USE AS NATURAL GAS HYDRATE INHIBITORS

Disclosed are succinimide-based compounds used in compositions and methods for inhibiting natural gas hydrate agglomerates. The succinimide-based compounds are reaction products of an alkenyl succinic anhydride and an amine or amine alcohol. 1. A composition comprising at least one succinimide-based compound to inhibit formation of natural gas hydrate agglomerates , the at least one succinimide-based compound formed by a reaction between an alkenyl succinic anhydride with an amine or amine alcohol.2. The composition of claim 1 , wherein the amine comprises primary claim 1 , secondary or tertiary amine.3. The composition of claim 1 , wherein the amine is a dibutylaminopropylenediamine claim 1 , a dibutylaminopropylenediamine with an additional aminopropylamino moiety claim 1 , or combination thereof.4. The composition of claim 1 , wherein succinimide-based compounds is from about 1 wt/v % to about 80 wt/v % based on the composition.5. The composition of claim 1 , wherein the composition further comprises one or more thermodynamic gas hydrate inhibitors claim 1 , kinetic gas hydrate inhibitors claim 1 , anti-agglomerants claim 1 , asphaltene inhibitors claim 1 , paraffin inhibitors claim 1 , scale inhibitors claim 1 , emulsifiers claim 1 , water clarifiers claim 1 , dispersants claim 1 , emulsion breakers claim 1 , or any combination thereof.6. A composition comprising:a fluid; and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the at least one succinimide-based compounds of .'}7. The composition of claim 1 , wherein the succinimide-based compounds are about is about 1000 ppm to 50 claim 1 ,000 ppm.8. The composition of claim 1 , wherein the fluid comprises water claim 1 , natural gas claim 1 , and liquid hydrocarbon.10. A method of inhibiting formation of agglomerates of natural gas hydrates comprising:introducing into a fluid a composition comprising at least one succinimide-based compound to inhibit formation of agglomerates of natural gas hydrates, the at least ...

RESIST UNDERLAYER FILM-FORMING COMPOSITION

A resist underlayer film forming composition contains a reaction product of an aromatic compound (A) having 6 to 60 carbon atoms and a compound represented by formula (B), and a solvent. (In the formula, X represent an oxygen atom or a nitrogen atom; Y represents a single bond, an oxygen atom or a nitrogen atom; X and Y may combine with each other to form a ring; and each of R, R, Rand Rindependently represents a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, a cyclic alkyl group having 3 to 8 carbon atoms or an aromatic group having 6 to 10 carbon atoms; provided that Ris present only in cases where X is a nitrogen atom, and Ris present only in cases where Y is a nitrogen atom.) 2. The resist underlayer film-forming composition according to claim 1 , wherein X and Y in formula (B) are each an oxygen atom or a nitrogen atom.4. The resist underlayer film-forming composition according to claim 1 , wherein the aromatic compound (A) comprises one or more benzene rings claim 1 , one or more naphthalene rings claim 1 , one or more anthracene rings claim 1 , one or more pyrene rings claim 1 , or a combination thereof.5. The resist underlayer film-forming composition according to claim 1 , wherein the aromatic compound (A) comprises two or more benzene rings claim 1 , two or more naphthalene rings claim 1 , two or more anthracene rings claim 1 , two or more pyrene rings claim 1 , or a combination thereof.6. The resist underlayer film-forming composition according to claim 1 , further comprising a crosslinking agent.7. The resist underlayer film-forming composition according to claim 1 , further comprising an acid and/or an acid generator.8. The resist underlayer film-forming composition according to claim 1 , wherein the solvent has a boiling point of 160° C. or higher.9. A resist underlayer film claim 1 , which is a baked product of a coating film comprising the resist underlayer film-forming composition according to .10. A method for manufacturing a ...

Synergistic Blends Of Anti-Agglomerant Gas Hydrate Inhibitors With Quaternary Alkyl Ammonium Compounds

The present disclosure relates to a gas hydrate inhibitor composition comprising from an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1) 1. A gas hydrate inhibitor composition comprising [{'br': None, 'sup': 5', '1', '2', '3', '+', '−, '[R-L-N(R)(R)(R)]X\u2003\u2003(1)'}, 'wherein', {'sup': 1', '2', '1', '2, 'each of Rand Ris independently an alkyl group having from 1 to 5 carbon atoms; or wherein the nitrogen atom and the Rand Rgroups together form a substituted or unsubstituted heterocyclic group;'}, {'sup': '3', 'Ris present or not as hydrogen or an alkyl group having from 1 to 8 carbon atoms which optionally bears a hydroxy group or a carboxy group in the 2-position;'}, 'L is a linking moiety comprising an optionally substituted hydrocarbyl group having at least 2 adjacent carbon atoms, at least one heteroatom selected from nitrogen and oxygen, and optionally one or more further heteroatoms;', {'sup': '5', 'Ris a hydrocarbyl group having from 6 to 22 carbon atoms; and'}, {'sup': −', '3, 'X is present as an anion when Ris present; and'}], 'A) from 5 to 95 weight-% of an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1)'}{'sub': 8', '18, 'B) from 5 to 95 weight-% of a cationic surfactant which is selected from di(C-Calkyl)dimethyl ammonium salts.'}2. The gas hydrate inhibitor composition according to claim 1 , wherein Rand Rindependently are alkyl groups having from 3 to 5 carbon atoms.3. The gas hydrate inhibitor composition according to wherein Ris an alkyl or alkenyl group having between 8 and 20 carbon atoms.4. The gas hydrate inhibitor composition according to claim 1 , wherein Ris present as hydrogen or as a methyl group.5. The gas hydrate inhibitor according to claim 1 , wherein X is selected from the group consisting of hydroxide claim 1 , carboxylate claim 1 , halide claim 1 , ...

Synergistic Blends Of Anti-Agglomerant Gas Hydrate Inhibitors With Alkoxylates Of Fatty Alcohols, Fatty Amines And Fatty Acids

The present disclosure relates to a gas hydrate inhibitor composition comprising an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1) 1. A gas hydrate inhibitor composition comprising [{'br': None, 'sup': 5', '1', '2', '3', 'q+', '−, 'sub': 'q', '[R-L-N(R)(R)(R)][X]\u2003\u2003(1)'}, 'wherein', {'sup': 1', '2', '1', '2, 'each of Rand Ris independently an alkyl group having from 1 to 5 carbon atoms; or wherein the nitrogen atom and the Rand Rgroups together form a substituted or unsubstituted heterocyclic group;'}, {'sup': '3', 'Ris present or not as hydrogen or an alkyl group having from 1 to 8 carbon atoms which optionally bears a hydroxy group in the 2-position;'}, 'L is a linking moiety comprising an optionally substituted hydrocarbyl group having at least 2 adjacent carbon atoms, at least one heteroatom selected from nitrogen and oxygen, and optionally one or more further heteroatoms;', {'sup': '5', 'Ris a hydrocarbyl group having from 6 to 22 carbon atoms;'}, {'sup': −', '3, 'X is present as an anion when Ris present;'}, 'q is 0 or an integer from 1 to 7; and, 'A) from 5 to 95 weight-% of an amphiphile having a hydrophobic tail linked to a hydrophilic head group by a linking moiety, the amphiphile having the general formula (1)'}{'sub': 8', '18', '8', '18', '8', '18', '8', '18, 'B) from 5 to 95 weight-% of a nonionic surfactant which is selected from alkoxylated C-Cfatty alcohols, alkoxylated C-Cfatty amines, alkoxylated C-Cfatty acids and alkoxylated C-Cfatty acid amides.'}2. The gas hydrate inhibitor composition according to claim 1 , wherein Rand Rindependently are alkyl groups having from 3 to 5 carbon atoms claim 1 , more preferably 4 or 5 and most preferably 4 carbon atoms.3. The gas hydrate inhibitor composition according to claim 1 , wherein Ris an alkyl or alkenyl group having from 8 to 20 carbon atoms.4. The gas hydrate inhibitor composition according to claim 1 , ...

Process for the Preparation of 2-Alkoxymethyl-1,4-Benzenediamines

A process for synthesizing 2-methoxymethyl-1,4-benzenediamine (V-a), its derivatives of formula (V) and the salts thereof, which comprises a radical halogenation step of formula (II). The final product can be 2-methoxymethyl-1,4-benzenediamine of formula (IV-a). 6. The process according to claim 4 , wherein the amine protection step a) claim 4 , radical halogenation step b) claim 4 , alkylating step c) and deprotection step d) are performed successively. A process to synthesize 2-alkoxymethyl-1,4-benzenediamines (V), its derivatives, and salts thereof, comprising the protection of sensitive amine functionalities, radical halogenation mediated by halogenating agents, and alkoxylation. These compounds may be used as couplers and/or primary intermediates in compositions for dyeing keratin fibers.CA 2,576,189 discloses the application of combinations of 2-methoxymethyl-1,4-benzenediamine (V-a) with various couplers and primary intermediates in oxidative dyeing compositions. U.S. Pat. No. 2,273,564 discloses a process to synthesize substituted 1,4-benzenediamine compounds with a substituent on the 2 position. U.S. Pat. No. 6,648,923 B1 discloses a process to synthesize 2-methoxymethyl-1,4-benzenediamine and the salts thereof.The previous syntheses described above to reach 2-alkoxymethyl-1,4-benzenediamines, their derivatives, and salts thereof are not completely satisfactory.Therefore, there is a need for a simple, industrially applicable, efficient, not expensive and high yield process to synthesize 2-alkoxymethyl-1,4-benzenediamines, their derivatives of formula (V), and salts thereof.The key step of the process of this invention is a radical halogenation of the N-protected- or the N,N′diprotected-2-methyl-1,4-benzenediamine derivatives of formula (II) as key intermediates.A new process has now been developed to synthesize 2-alkoxymethyl-1,4-benzenediamines (V), its derivatives, and salts thereof, which permits a production of said compounds in a novel, high yield, ...

Process for Preparing 5-biphenyl-4-amino-2-methyl Pentanoic Acid

The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, 3. A compound according to wherein the compound according to formula (2) claim 1 , or tautomer claim 1 , or salt thereof claim 1 , is in crystalline form.4. A compound according to wherein the compound according to formula (2-a) claim 2 , or tautomer claim 2 , or salt thereof claim 2 , is in crystalline form.5. A compound according to claim 1 , wherein in the compound of formula (2-a) R1 is hydrogen or a nitrogen protecting group selected from pivaloyl and t-butyloxycarbonyl (BOC).13. A process according to claim 6 , wherein R1 and R2 are hydrogen and R3 is an ethyl group. This application is a Divisional application of Ser. No. 13/333,437, filed Dec. 21, 2011, which is a Divisional application of Ser. No. 12/522,767, filed Jul. 10, 2009, which is a National Phase Application of PCT/EP2008/000142, filed Jan. 10, 2008, which claims benefit of EP 07/100,451.9, filed Jan. 10, 2008.The present invention relates to pyrrolidin-2-ones according to formula (1), or salts thereof,wherein R1 is hydrogen or a nitrogen protecting group, as defined herein, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester, or salt thereof.Endogenous atrial natriuretic peptides (ANP), also called atrial natriuretic factors (ANF), have diuretic, natriuretic and vasorelaxant functions in mammals. The natural ANF peptides are metabolically inactivated, in particular by a degrading enzyme which has been recognized to correspond to the enzyme neutral endopeptidase (NEP, EC 3.4.24.11), which is also responsible for e.g. the metabolic inactivation of enkephalins.In the art biaryl substituted phosphonic acid derivatives are known which are useful as neutral endopeptidase (NEP) inhibitors, e.g. as inhibitors of the ANF-degrading enzyme in ...

CONTINUOUS HIGH SHEAR REACTOR MELT PROCESSING METHODS TO SYNTHESIZE HETEROCYCLIC MONOMERS AND COMPOSITIONS THEREOF

The invention provides novel methods of synthesizing new monofunctional and/or multifunctional heterocyclic monomers and the formulation of new alloys of said monomers from base reactants via a continuous solvent-free, or alternatively in-solvent, one-step high shear reactor methodology designed to reduce the minor isomer formation and to eliminate the need for post-processing purification, as well as the ability to disperse reinforcements and additives while synthesizing such heterocyclic monomers and monomer alloys created and to the synthesis of related compositions. 5. A method to melt synthesize a monofunctional benzoxazine monomer , maleimide monomer , or both , from a known variant of at least one base reactant , the method comprising:utilizing in a reactor at least one base reactant from a batch of pre-blended reactants for the synthesis, wherein the at least one base reactant is a phenol, amine, paraformaldehyde, or a combination thereof, andforming the monofunctional benzoxazine monomer, maleimide monomer, or both, using a continuous, high shear reactor at a processing temperature of from about 90° C. to about 200° C. and a residence time of about 30 to about 60 seconds for benzoxazines and about 160° C. to about 300° C. and a residence time of about 90 seconds for maleimides,wherein the monofunctional benzoxazine monomer, maleimide monomer, or both, is a room temperature solid.6. The method of claim 5 , wherein the at least one base reactant is fed to the reactor independently from at least one other base reactant.7. The method of claim 6 , wherein the monofunctional benzoxazine monomer claim 6 , maleimide monomer claim 6 , or both claim 6 , is a room temperature liquid.8. The method of claim 5 , further comprising melt synthesizing the major isomer of the monofunctional benzoxazine monomer claim 5 , maleimide monomer claim 5 , or both claim 5 , wherein the monomer is a room temperature solid claim 5 , and minimizing the formation of any minor isomer.9. ...

New nucleophile-reactive sulfonated compounds for the (radio)labelling of (bio) molecules; precursors and conjugates thereof

Nucleophile-reactive sulfonated compounds used as precursors to (radio)labelled (bio)molecules are produced by pre-introduction of a nucleophilic compound R* through an unusual nucleophile-induced ring-opening reaction of the sultone moiety of the precursor. The precursors and compounds conform to respective formulae (Ip) and (I): Also disclosed are methods for producing these precursors and compounds, as well as for conjugation of these compounds with (bio)molecules, and to the drugs obtained by this method.

PROCESS FOR THE SYNTHESIS OF AMIDE BONDS WITH THE AID OF NOVEL CATALYSTS

The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents containing an anion of the formula (I), to the novel reagents, and to the preparation thereof. 1. Process for the production of an amide bond by reaction of an acid with a primary or secondary amine in the presence of a base with the aid of an amide linking reagent , characterised in that use is made of at least one amide linking reagent containing an anion of the formula (I) ,{'br': None, 'sub': n', '2n+1', 'y', '6-y, 'sup': '−', '[P(CF)F]\u2003\u2003(I),'}wheren stands on each occurrence, independently, for 1, 2, 3, 4, 5, 6, 7 or 8 andy stands for 1, 2, 3 or 4.2. Process according to claim 1 , in which use is made of amide linking reagents containing anions of the formula (I) in which the variable n stands on each occurrence claim 1 , independently claim 1 , for 2 claim 1 , 3 or 4.3. Process according to claim 1 , in which use is made of amide linking reagents containing anions of the formula (I) selected from the group [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] claim 1 , [(CF)PF] and [(CF)PF].4. Process according to claim 1 , characterised in that the cation of the amide linking reagent is a uronium claim 1 , thiouronium claim 1 , guanidinium claim 1 , aminium claim 1 , carbonium claim 1 , imidazolium or phosphonium cation.5. Process according to claim 1 , characterised in that a peptide bond is produced.7. Compounds according to claim 6 , where FAP stands for [(CF)PF] Or [(n-CF)PF]. The invention relates to a process for the production of amide bonds, in particular peptide bonds, with the aid of novel amide linking reagents as catalysts, to the novel reagents, and to the preparation thereof.Modern standard processes for peptide synthesis use effective peptide linking reagents. The formation of amide bonds is likewise of importance for the ...

Branched Discrete PEG Constructs

Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues. 2. The substantially pure compound of claim 1 , wherein A comprises a preferential locator that binds with a biological moiety claim 1 , said preferential locator being one or more of a cell surface and matrix antigen claim 1 , transport protein claim 1 , or receptor protein.3. The substantially pure compound of claim 2 , wherein said preferential locator A is one or more of an antibody claim 2 , antibody fragment claim 2 , engineered antibody claim 2 , engineered fragment claim 2 , peptide substrate claim 2 , peptomimetic substrate claim 2 , cytokine claim 2 , aptamer claim 2 , siRNA claim 2 , vitamin claim 2 , or steroid.4. The substantially pure compound of claim 1 , wherein A is a nanoparticle claim 1 , microparticle claim 1 , engineered molecular scaffold that contains multiple functionalities claim 1 , or an engineered chemically reactable group.5. The substantially pure compound of claim 1 , wherein A is a chemically reactable moiety being one or more of an alkyl or aryl functionalized 1° or 2° amine claim 1 , hydroxyl claim 1 , aldehyde claim 1 , ketone claim 1 , carboxylate claim 1 , active carboxylate ester ...

Branched Discrete PEG Constructs

Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues. 122-. (canceled)2310. A method of externally imaging an antibody , antibody fragment , or a peptide attached to an externally imagable radiolabel , which comprises attaching said imagable radiolabel to and said antibody , antibody fragment , or a peptide to the structure of claim , wherein RG is said radiolabel and A comprises said antibody , antibody fragment , or a peptide.24. The method of claim 23 , wherein said antibody has been generated against a tumor associated glycoprotein.25. The method of claim 24 , wherein said antibody comprises B72.3 claim 24 , CC49 claim 24 , V59 claim 24 , or 3E8.26. The method of claim 25 , wherein said antibody comprises CC49 claim 25 , domain deleted CC49 claim 25 , CC49 fragments claim 25 , including Fab′ claim 25 , CC49 diabodies claim 25 , CC49 scFv claim 25 , and single chains derived therefrom.27. The method of claim 23 , wherein said antibody comprises 3E8 claim 23 , domain deleted 3E8 claim 23 , 3E8 fragments claim 23 , 3E8 diabodies claim 23 , and single chains derived therefrom.2831-. (canceled) This application claims benefit of application Ser. No. 61/528,915 ...

ANTIFIBRINOLYTIC COMPOUNDS

The present invention provides novel antifibrinilytic compounds, processes for their preparation, pharmaceutical and veterinary compositions thereof, and their use in medicine, in particular for the treatment of bleeding. 4. The compound of claim 1 , wherein Ris hydroxyl or —O—(C-C)alkyl claim 1 , or a pharmaceutically acceptable salt thereof.5. The compound of claim 4 , wherein Ris hydroxyl claim 4 , or a pharmaceutically acceptable salts thereof.6. The compound according to claim 1 , wherein Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 1 , or a pharmaceutically acceptable salts thereof.7. The compound of claim 6 , wherein Rand Rare both methyl claim 6 , or a pharmaceutically acceptable salts thereof.8. The compound according to claim 2 , wherein Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 2 , or a pharmaceutically acceptable salts thereof.9. The compound according to claim 3 , wherein .Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 3 , or a pharmaceutically acceptable salts thereof.10. The compound according to claim 4 , wherein .Rand Rare independently (C-C)alkyl or halo(C-C)alkyl claim 4 , or a pharmaceutically acceptable salts thereof.11. The compound of claim 8 , wherein Rand Rare both methyl claim 8 , or a pharmaceutically acceptable salts thereof.12. The compound of claim 9 , wherein Rand Rare both methyl claim 9 , or a pharmaceutically acceptable salts thereof.13. The compound of claim 10 , wherein Rand Rare both methyl claim 10 , or a pharmaceutically acceptable salts thereof. The present invention relates to novel antifibrinolytic compounds, processes for their preparation, pharmaceutical compositions thereof, and their use in medicine, particularly for the treatment of bleeding.A major goal in surgery, as well as treatment of major tissue damage, is to avoid or minimize bleeding to ensure the formation of stable and secure haemostatic plugs that are not easily dissolved by fibrinolytic enzymes. It is of importance ...

Material for forming organic film, substrate for manufacturing semiconductor device, method for forming organic film, patterning process, and compound for forming organic film

An object of the present invention is to provide: a compound containing an imide group which is not only cured under film formation conditions of inert gas as well as air, generates no by-product and has excellent heat resistance and properties of filling and planarizing a pattern formed on a substrate, but can also form an organic underlayer film with favorable adhesion to a substrate. The present invention provides a material for forming an organic film, including: (A) a compound for forming an organic film shown by the following general formula (1A) or (1B); and (B) an organic solvent, noting that in the general formula (1A), when W 1 represents any of R 1 does not represent any of

COMPOUND, SUBSTRATE FOR PATTERN FORMATION, PHOTODEGRADABLE COUPLING AGENT, PATTERN FORMATION METHOD, AND TRANSISTOR PRODUCTION METHOD

Provided is a compound represented by Formula (1). 2. The compound according to claim 1 , wherein Ror Rrepresents any of a methyl group claim 1 , an isopropyl group claim 1 , or a tert-butyl group.3. A substrate for pattern formation claim 1 , which has a surface chemically modified by the compound according to .4. A photodegradable coupling agent which is formed of the compound according to .5. A pattern formation method of forming a pattern on a surface of an object to be treated claim 1 , comprising:aminating at least a part of the surface of the object to be treated to form an aminated surface;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'chemically modifying the aminated surface using the compound according to ;'}irradiating the chemically modified surface to be treated with light in a predetermined pattern to generate a latent image formed of a hydrophilic region and a water-repellent region; anddisposing a pattern forming material in the hydrophilic region or the water-repellent region.6. The pattern formation method according to claim 5 ,wherein the predetermined pattern corresponds to a circuit pattern for an electronic device.7. The pattern formation method according to claim 5 ,wherein the pattern forming material contains a conductive material, a semiconductor material, or an insulating material.8. The pattern formation method according to claim 7 ,wherein the conductive material is formed of a conductive fine particle dispersion liquid.9. The pattern formation method according to claim 7 ,wherein the semiconductor material is formed of an organic semiconductor material dispersion liquid.10. A pattern formation method of forming a pattern on a surface of an object to be treated claim 7 , comprising:aminating at least a part of the surface of the object to be treated to form an aminated surface;{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'chemically modifying the aminated surface using the compound according to ;'}irradiating the chemically ...

Metodo para acoplamiento de liposomas.

N-substituted imides as polymerization initiators

The invention relates to novel N-substituted imides and polymerizable compositions com¬ prising these N-substituted imides. The invention further relates to the use of N-substituted imides as polymerization initiators. The imides are compounds of the formula (I) and (II) wherein n is 1 or 2; m is 1 or 2; R1 and R2 are each, independently of one another, hydrogen, C1-C18alkyl, C1-C-18alkenyl C6-C14aryl, aralkyl, C5-C12cycloalkyl, each of which may be substituted by halogen, C1-C4-alkyl, hydroxy, C1-C6alkoxy, carbonyl, C1-C6alkoxycarbonyl; or R1 and R2 together with the adjacent -CO-N-CO- group may form a monocyclic, bicyclic or polycyclic ring, said ring having up to 50 non hydrogen atoms and wherein said ring may contain the structural element (formula III) more than once; R3 if n is 1, is C1-C18alkyl, C6-C14aryl, aralkyl, C5-C12cycloalkyl, OR10 or SR11, NR12R13; wherein R3 if n is 2, is C2-C12alkylene, C6-C14arylene, xylylene R4 and R5, correspond to R1 and R2; R6 if n is 1, is hydrogen, C1-C18alkyl, C6-C14aryl, aralkyl, C5-C12cycloalkyl, NR14R15; wherein R6 if n is 2, is C2-C12alkylene, C6-C14arylene, xylylene; R7 is hydrogen, C1-C18alkyl, C6-C14aryl, aralkyl, C5-C12cycloalkyl, each of which may be substituted by halogen, C1-C4-alkyl, hydroxy, C1-C6alkoxy, carbonyl, C1-C6alkoxy- carbonyl; or R7 and R14 or R7 and R15 form together with the N-atom attached to R7 a 5- 6 membered ring, optionally interrupted by -NH-, -N(C1-C8alkyl)-, -O- and/or S-atoms.

Method for protein-liposome coupling

This invention relates to a method for synthesizing a substantially pure reactive lipid including, for example, N-[4-(p-maleimidophenyl)-butyryl]phosphatidylethanolamine (MPB-PE) and related compositions. The compositions of the present invention are useful as coupling agents and may be incorporated into liposomes and subsequently coupled to proteins, cofactors and a number of other molecules. A preferred coupling method is also disclosed as are protein conjugates.

Chemically reactive pyrenyloxy sulfonic acid dyes

The invention relates to novel fluorescent dyes based on the following pyrenyloxy sulfonic acid structure: ##STR1## wherein at least one of R 1 , R 2 , R 3 , and R 4 is --OCH 2 C(O)OCH 3 , --OCH 2 CON(O)H, --OCH 2 CON 3 , --OCH 2 CONHNH 2 , ##STR2## or --CH 2 CONH(CH 2 ) n NH 2 where n is an integer from 1 to 10; at least one of R 1 , R 2 , R 3 , and R 4 is sulfonic acid or alkali salts of sulfonic acid; and all other of R 1 , R 2 , R 3 , and R 4 are hydrogen or a hydroxyl group. The new reagents contain functional groups typically found in biomolecules or polymers. The spectral properties of the fluorescent dyes are sufficiently different in wavelengths and intensity from fluorescein as to permit simultaneous use of both dyes with minimum interference. The dyes have narrower spectral band-widths and smaller Stokes' shifts than other reactive dyes with similar spectral properties, do not show appreciable sensitivity to pH, have higher solubilities in aqueous solvents and have good quantum yields and photostability.

Production of polysuccinimide and derivatives thereof in a sulfur-containing solvent

Polysuccinimide of varying molecular weight has been prepared in a solvent system by heat polymerization of aspartic acid. The solvent system includes a sulfur oxygen acid and a sulfur oxygen acid salt. In a preferred embodiment, aspartic acid is polymerized in a liquid solvent reaction mixture at a temperature in the range of about 110° C. to about 320° C.

광반응성 중합체 및 이의 제조 방법

본 발명은 주쇄에 다중고리 화합물을 포함하는 광반응성 중합체 및 이의 중합 방법에 관한 것이다. 본 발명에 따른 광반응성 중합체는 유리전이온도가 높은 다중고리 화합물을 주쇄로서 포함하기 때문에 열적안정성이 우수하며, 빈 격자자리가 상대적으로 크기 때문에, 광반응기가 고분자 주쇄 내에서 비교적 자유롭게 이동할 수 있어, 기존의 액정표시소자용 배향막 제조용 고분자 재료의 단점으로 지적되어오던 느린 광반응 속도라는 단점을 개선할 수 있다.

Fluorinated n, n-bis-imides

Case 6297 ASC/kmf FLUORINATED N,N-BIS-IMIDES Abstract This invention relates to novel fluorinated N,N-bis-imides of the formula wherein R is a bivalent radical of the formula or

Novel organic compound and method for producing radioactive halogen-labeled organic compound using the same

(과제) 방사성 할로겐으로 치환된 신-1-아미노- 3-시클로부탄카르복실산을, 선택적으로 제조하기 위한 표식 전구체 화합물 및 상기 화합물을 사용한 방사성 할로겐으로 치환된 신-1-아미노-3-시클로부탄카르복실산의 제조 방법을 제공한다. (Tasks) Marker precursor compound for the selective preparation of syn-1-amino-3-cyclobutanecarboxylic acid substituted with radioactive halogen and syn-1-amino-3-cyclo substituted with radiohalogen using the compound Provided is a method for producing butanecarboxylic acid. (해결 수단) 아미노기의 보호기를 프탈이미드기로 한 표식 전구체를 사용한다. 이 표식 전구체를 방사성 할로겐으로 표식하고, 탈보호를 행함으로써, syn형의 방사성 할로겐으로 치환된 1-아미노-3-시클로부탄카르복실산을 선택적으로 제조할 수 있다. (Solution means) The labeled precursor which used the protecting group of an amino group as a phthalimide group is used. By labeling this labeled precursor with a radioactive halogen and performing deprotection, the 1-amino-3-cyclobutanecarboxylic acid substituted with syn-type radioactive halogen can be selectively produced. 방사성 할로겐 표식 유기화합물 Radioactive Halogen Labeled Organic Compounds

Reactions catalyzed by chromium (III) carboxylates

Reactions of ring systems, such as aziridines, oxetanes and oxiranes with carboxylic acids, anhydrides, imides, lactones and carbonate esters are catalyzed by C 3 -C 60 , substituted or unsubstituted, straight or branched-chained, alkyl, aryl, or aralkyl carboxylate Cr +3 salts, preferably chromium +3 octoate. The catalysts also accelerate the reaction of hydroxy compounds with anhydrides, and of thiiranes with anhydrides. The catalysts selectively enhance the conversion of ring systems to form monomers, prepolymers, copolymers, functional end-group monomers, functional end-group prepolymers, and functional end-group polymers rather than forming homopolymers. By varying the catalyst concentration, molar ratios, and reaction temperatures, the reaction time required to form the desired product can be controlled.

Use of chromium (iii) carboxylates as a catalyst

The use of C3-C60, substituted or unsubstituted, straight or branch-chained, alkyl, aryl, or aralkyl carboxylate Cr+3 salts, preferably chromium +3 octoate, as catalysts for the reaction of ring systems, such as aziridines, oxiranes, oxetanes and thiiranes with carboxylic acids, anhydrides, lactone and carbonate esters are disclosed. The use of chromium (Cr+3) salt catalysts for accelerating the reaction of hydroxy compounds with anhydrides, lactones, and carbonate esters are also disclosed. These reactions can occur in single or polymer reactions. The chromium +3 carboxylate catalyst increases the reaction rates by orders of magnitude and selectively reacts the ring systems to form monomers, prepolymers, copolymers, functional end-group monomers, functional end-group prepolymers, and functional end-group polymers rather than forming homopolymers. By varying the catalyst concentration, molar ratios, and reaction temperatures, the reaction time required to form the desired product can be controlled.

N-замещенные имиды как инициаторы полимеризации

1. Соединения формул I и IIив которых n обозначает 1 или 2;m обозначает 1 или 2;Rи Rкаждый независимо друг от друга обозначает водородный атом, С-Салкил, С-Салкенил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, С-Салкоксикарбонилом; или Rи Rсовместно со смежной группой -CO-N-CO- могут образовывать моноциклическое, бициклическое или полициклическое кольцо, причем указанное кольцо содержит до 50 неводородных атомов и указанное кольцо может включать больше одного структурного элементаR, если n обозначает 1, обозначает С-Салкил, С-Салкенил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, C-Салкоксикарбонилом; или Rобозначает ORили SR, NRR, где Rобозначает С-Салкил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, C-Салкоксикарбонилом; Rобозначает С-Салкил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, С-Салкокси, карбонилом, C-Салкоксикарбонилом; a Rи Rнезависимо друг от друга обозначают водородный атом, С-Салкил, С-Сарил, аралкил, С-Сциклоалкил, каждый из которых может быть замещен атомом галогена, С-Салкилом, гидроксилом, C-Салкокси, карбонилом, C-Салкоксикарбонилом; или Rи Rобразуют совместно с атомом N, к которому они присоединяются, 5- или 6-членное кольцо, необязательно прерываемое -NH-, -N(C-Cалкил)-, -О- и/или атомами S, R, если n обозначает 2, обозначает С-Салкилен, С-Салкенилен, С-Сарилен, ксилилен при условии, что исключаются след� ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2007 121 503 (13) A (51) ÌÏÊ C08F 4/00 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007121503/04, 31.10.2005 (71) Çà âèòåëü(è): ÖÈÁÀ ÑÏÅØÈÀËÒÈ ÊÅÌÈÊÝËÇ ÕÎËÄÈÍà ÈÍÊ. (CH) (30) ...

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.

Method of obtaining diphenyl ether derivatives

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ДИФЕНИЛОВОГО ПРОСТОГО ЭФИРА общей формулы где А и В - галоген, галоидзамещенный низший, ал к ил, тип-0 - 3, причем m + п 0-3; - водород, низший С -С -алкил , циклогексил или фенил, отличающийс  тем, что соединени  общей формулы II JL подвергают взаимодействию с алкилгидразином общей формулы 111 Б-г . (Л RiNHNC Кз где X - атом галогена, нитрогруппа или феноксигруппа формулы (А) т. :л (В)л. где А, В, т, п, К,-Кз меют указанУ1 ные значени . THE WAY OF OBTAINING DERIVATIVE DIPHENYL ETHER ETHER OF A GENERAL FORMULA where A and B are halogen, halogen-substituted lower, al kil, type-0 - 3, with m + n 0-3; is hydrogen, lower C -C alkyl, cyclohexyl or phenyl, characterized in that the compounds of general formula II JL are reacted with alkyl hydrazine of general formula 111 G-d. (L RiNHNC Кз where X is a halogen atom, a nitro group or a phenoxy group of the formula (A) t.: L (B) l. Where A, B, t, n, K, -Ks have the specified values.

Amino or hydrazino peroxides, derivatives and their uses

This invention relates to novel reactive amino or hydrazino peroxides (hereinafter generally referred to as "AHP's") and derivatives all having a Structure A: (P--R11--X--(--NH--).sub.x --R22--).sub.y --Q].sub.z A in which the definitions of P, R11, R22, X, Q and x, y and z are given in the Summary of The Invention section, for example, 4,4-di-(t-butylperoxy)pentanohydrazide (I-1), and the use of these novel compounds in curing unsaturated polyester resins, in initiating polymerization of ethylenically unsaturated monomers, for modifying rheology, for crosslinking and curing olefin polymers and elastomers, for producing novel graft and block copolymers, and for producing novel polymers with covalently bound performance additive functions.

Process for preparing amino or hydrazino peroxides, derivatives and their uses

This invention relates to procedures for preparing novel reactive amino or hydrazino peroxides (hereinafter generally referred to as "AHP's") and derivatives all having a Structure A: ##STR1## in which the definitions of P, R11, R22, X, Q and x, y and z are given in the Summary Of The Invention section, for example, 4,4-di-(t-butylperoxy)pentanohydrazide (I-1), and the use of these novel compounds in curing unsaturated polyester resins, in initiating polynerization of ethylenically unsaturated monomers, for modifying rheology, for crosslinking and curing olefin polymers and elastoiners, for producing novel graft and block copolymers, and for producing novel polymers with covalently bound performance additive functions.

Process for preparing block or graft copolymers using amino or hydrazino peroxides

This invention relates to novel reactive amino or hydrazino peroxides (hereinafter generally referred to as "AHP's") and derivatives all having a Structure A: ##STR1## in which the definitions of P, R11, R22, X, Q and x, y and z are given in the Summary Of The Invention section, for example, 4,4-di-(t-butylperoxy)pentanohydrazide (I-1), and the use of these novel compounds in curing unsaturated polyester resins, in initiating polymerization of ethylenically unsaturated monomers, for modifying rheology, for crosslinking and curing olefin polymers and elastomers, for producing novel graft and block copolymers, and for producing novel polymers with covalently bound performance additive functions.

Process for curing polymers using amino or hydrazino peroxides

This invention relates to novel reactive amino or hydrazino peroxides (hereinafter generally referred to as "AHP's") and derivatives all having a Structure A: ##STR1## in which the definitions of P, R11, R22, X, Q and x, y and z are given in the Summary Of The Invention section, for example, 4,4-di-(t-butylperoxy)pentanohydrazide (I-1), and the use of these novel compounds in curing unsaturated polyester resins, in initiating polymerization of ethylenically unsaturated monomers, for modifying rheology, for crosslinking and curing olefin polymers and elastomers, for producing novel graft and block copolymers, and for producing novel polymers with covalently bound performance additive functions.

Process for increasing the bleaching efficiency of an inorganic persalt or of hydrogen peroxide

A process for increasing the bleaching efficiency of an inorganic persalt or hydrogen peroxide by adding to said persalt or H₂O₂ an activating agent. The activating agent is an acetylated gluconic acid derivative, such as N-methyl pentaacetyl gluconamide, N-methyl-N-acetyl pentaacetyl gluconamide, N-methyl-N-acetyl pentaacetyl gluconamide or tetraacetyl gluconolactone. The invention also relates to the acetylated gluconic acid derivatives themselves.

Novel vinyl carbonate and vinyl carbamate contact lens material monomers

Novel monomers of the general formula ##STR1## where b is 0 or 1, a is 1, 2, 3 or 4, R 2 is a monovalent alkyl radical and R is an organic radical. The novel monomers may be employed to produce novel copolymers useful as hydrogel, soft non-hydrogel and/or rigid gas permeable contact lens materials.

Novel polycation compound and bleach composition containing the same

The product and preparation method of micro Nano material, its surface hydrophilic substance covalent modification

本发明公开了一种微纳米材料、其表面用亲水物质共价修饰的产物及制备方法；微纳米材料表面含羧基或潜在羧基并转变成活泼酯；表面用亲水物质共价修饰的产物，由表面活泼酯与含脂肪族伯胺或/和脂肪族仲胺的亲水化合物或/和亲水聚合物为修试剂成酰胺键共价修饰而得；制备时，用含羧基或/和潜在羧基单体在聚合材料表面生成足够多羧基或/和潜在羧基并转变成活泼酯，再与带脂肪族伯胺和/或仲胺、潜在兼性离子基团、亲水连接臂且体积适中的修饰剂成酰胺键获得共价修饰层；在共价修饰产物表面重复生成活泼酯后与亲水修饰剂成酰胺键的过程实现多层共价修饰，用中等体积亲水修饰剂高效覆盖微纳米材料表面而显著降低修饰产物对生物分子非特异吸附。

Manufacturing method of cyclic N-vinyl carboxylic acid amide

본 발명은, 출발 물질로서, 값싸면서도 용이하게 얻을 수가 있는 고리형 카르복실산 에스테르와 모노에탄올아민을 사용하여 안전하면서도 저가로 고리형 N-비닐 카르복실산 아미드를 안정되게 제조하는 방법을 제공한다. 본 발명의 방법은 고리형 카르복실산 에스테르와 모노에탄올아민을 액체상에서 분자간 탈수 반응 (제1-단계 반응) 시켜 고리형 N-(2-히드록시에틸) 카르복실산 아미드를 제조하는 단계 그 다음에는 이 고리형 N-(2-히드록시에틸) 카르복실산 아미드를 알칼리 금속 원소 및/또는 알칼리 토금속 원소 및 규소를 함유하는 산화물 촉매의 존재하에 기체상에서 분자내 탈수 반응 (제2-단계 반응) 시켜 고리형 N-비닐 카르복실산 아미드를 제조하는 단계로 구성되어 있다. The present invention provides a method for stably producing a cyclic N-vinyl carboxylic acid amide safely and inexpensively by using a cyclic carboxylic acid ester and a monoethanolamine which can be obtained cheaply and easily as a starting material. . The process of the present invention comprises the steps of intermolecular dehydration (first-step reaction) of a cyclic carboxylic acid ester and a monoethanolamine in a liquid phase to prepare a cyclic N- (2-hydroxyethyl) carboxylic acid amide. Intramolecular dehydration reaction of this cyclic N- (2-hydroxyethyl) carboxylic acid amide in the gas phase in the presence of an oxide catalyst containing an alkali metal element and / or an alkaline earth metal element and silicon (second-stage reaction) To form a cyclic N-vinyl carboxylic acid amide.

Methods and compositions for radiohalogen protein labeling

Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [ 125 I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.

Branched discrette PEG constructs

Disclosed are general and "substantially pure" branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologies like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, "A", a group that is reactive with a biologic material that creates "A", which is a biologically reactive group, connected through ~~~~~~ to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, ——, having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 d PEG residues.

Method of producing derivatives of diphenyl ester

Novel diphenyl ether hydrazine derivatives, particularly 2-nitro-5 (nucleus-substituted phenoxy) phenylhydrazine derivatives are provided. They are useful as a selective herbicide having a high herbicidal activity and residual efficacy.

Method of preparing heterocycle substituted derivatives of 5-sulfomoylbensoic acid or its salts

Alkyd resin composition of multifunctional hydroxyphthalimide monomer compound

本发明涉及醇酸树脂组合物，其包含a.1‑60重量％的根据式Ia、Ib、Ic或Ie之任一的酰亚胺化合物，其中R1是H或C1‑C20任选取代的烃基；R2和R5独立地为H或C1‑C20烃基；R3和R4独立地为H或C1‑C20烃基；R6是H或甲基；R7和R8独立地为H、甲基或乙基；b.10‑40重量％的数均羟基官能度≥2.0的醇；c.30‑70重量％的脂肪酸或植物油；d.0‑50重量％的能够酯化的单官能和/或多官能化合物，所述化合物与a、b和c中使用的化合物不同；其中相对于化合物a、b、c和d的总重量来确定所述重量％，

Method of preparing 2-oxopyrrolidine-n-alkylamides

2-Oxo-pyrrolidine-N-alkylamides of the formula I in which n is 1 to 4 are prepared by electrolytic reduction of a corresponding 2,5-dioxopyrrolidine-N-alkylamide. The latter is obtained simply from the corresponding omega-haloalkylamide by condensation with sodium succinimide. The final products have therapeutic significance.

Preparation of an activated polymer ester for protein conjugation

The present invention is a process for preparing an activated ester of polyethylene glycol or a polyoxyethylated polyol. After the activated ester is prepared, it can be reacted with a protein to form a polymer/protein conjugate. Conjugation with a polymer can reduce the protein's immunogenicity, increase its solubility, and increase its circulating in vivo half-life. Preferred proteins are IL-2, CSFs, and interferons.

Reactive mass labels

A mass label for labelling and detecting a biological molecule by mass spectroscopy, which label comprises the following structure: X-L-M wherein X is a mass marker moiety comprising the following group: formula (I), wherein the cyclic unit is aromatic or aliphatic and comprises from 0-3 double bonds independently between any two adjacent atoms; each Z is independently N, N(R 1 ), C(R 1 ), CO, CO(R 1 ), C(R 1 ) 2 , O or S; X is N, C or C(R 1 ); each R 1 is independently H, a substituted or unsubstituted straight or branched C 1 -C 6 alkyl group, a substituted or unsubstituted aliphatic cyclic group, a substituted or unsubstituted aromatic group or a substituted or unsubstituted heterocyclic group; and y is an integer from 0-10, L is a cleavable linker comprising an amide bond and M is a mass normalization moiety.

Glycerol derivative

N-substituted imides as polymerisation initiators

FIELD: chemistry. SUBSTANCE: invention relates to novel N-substituted imides of formulae I and II where n stands for 1; m stands for 1; R 1 and R 2 , R 4 and R 5 together with adjacent group -CO-N-CO- form 5 or 6-member monocyclic ring, optionally saturated and probably substituted with C 1-18 alkyl, condensed ring system, which in addition to monocyclic core ring, determined above, contains one or two C 6 aromatic or C 6 aliphatic rings; R 3 stands for NR 12 R 13 , where R 12 and R 13 independently on each other represent C 1-18 alkyl, C 5 - 12 cycloalkyl, each of which can be substituted with C 1-4 alkyl; R 6 represents C 6-10 aryl, C 1-18 alkyl, C 6-10 ar-C 1 -C 18 alkyl, C 5 -C 12 cycloalkyl, each of which is optionally substituted with C 1 -C 4 alkyl; R 7 represents C 1 -C 18 alkyl, C 6 -C 10 aryl, C 6 -C 10 ar-C 1 -C 18 alkyl, C 5 -C 12 cycloalkyl, each of which is optionally substituted with C 1 -C 4 alkyl. EFFECT: obtaining novel compounds, which are used as initiators of radical thermal polymerisation (RTP) in hardener for coatings, hardened by free-radical polymerisation. 8 cl, 12 ex (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) 2 396 256 (13) C2 (51) МПК C07D C07D C07D C08F 207/40 (2006.01) 209/48 (2006.01) 221/14 (2006.01) 4/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2007121503/04, 31.10.2005 (24) Дата начала отсчета срока действия патента: 31.10.2005 (45) Опубликовано: 10.08.2010 Бюл. № 22 (56) Список документов, цитированных в отчете о поиске: US 3928493, 23.12.1975. J.Org.Chem., v.40, n.l5, 1975, p.2215-2220. ANALES DE QUIMICA, v.70, 1974, p.908-913. RU 2002133210/04, 20.09.2004. 2 3 9 6 2 5 6 R U (86) Заявка PCT: EP 2005/055646 (31.10.2005) C 2 C 2 (85) Дата перевода заявки PCT на национальную фазу: 09.06.2007 (87) Публикация PCT: WO 2006/051047 (18.05.2006) Адрес для переписки: 101000, Москва, М.Златоустинский пер., 10, кв.15, "ЕВРОМАРКПАТ", пат.пов. И.А. ...

Analogs of calicheamicin gamma1I, method of making and using the same

Chimeric analogs of calicheamicin that include an analog of calicheamicinone linked to an ester or glycoside, (-)-calicheamicinone and its analogs are disclosed.

Herbicide composition

1. ГЕРБИЦИДНАЯ КОМПОЗИЦИЯ в форме эмульгирующегос  концентрата , содержаща  активное вещество производное дифенилового эфира, . эмульгатор - солпол и растворитель бензол , отличающа с  тем, что, с целью повышени  гербицидной активности, она содержит в качестве производного дифенилового эфира соединение общей формулы Аг-0 где Аг - фенил, моно-, ди- или трихлорфенил, 4-метилфенил 4-трифторметилфенил, 2-хлор-4-метилфенил, 2-хлор-4-трифторметилфенил , 2,4-дихлор-6-фторфенил , R группы RI RI или I L-N-N CR4R5 N-NRzHj в которых R - водород, алкил , метоксикарбонил, этоксикарбонил, феноксикарбонил , ацетил Ri - водород, метил, этиЛ; R - водород, метил, фёниг метоксикарбонилметил, N - метил, аминосульфонил. а также С(О) R -rpynna, СО в которой R - алкил , хлорметил, 1-хлорэтил , метоксиметил, С -С алкоксй , фенокси, меток- сикарбонил, этоксикарбонил , бензил, 2-

Process for the preparation of 5-membered nitrogen containing heteroaromatics

내용없음. None.

A kind of preparation method of n-hydroxysuccinimide

本发明涉及一种N‑羟基琥珀酰亚胺的制备方法，属于药物中间体合成技术领域。为了解决现有的腐蚀性强污染大且设备要求高的问题，提供一种N‑羟基琥珀酰亚胺的制备方法，该方法包括在PBS缓冲液的存在下，将壳聚糖与N‑羟基琥珀酰亚胺基‑4‑叠氮基苯甲酸酯在微波加热辅助的条件下进行点击化学反应，得到N‑羟基琥珀酰亚胺。本发明能够使有效的起到分子内加热发生点击化学反应，减少了反应过程中温度梯度变化的影响，使实现缩短反应时间和高转化率，实现提高产物收率和纯度的效果。

Vinyl carbonate and vinyl carbamate contact lens material monomers

Novel monomers of the general formula ##STR1## where b is 0 or 1, a is 1, 2, 3 or 4, R 2 is a monovalent alkyl radical and R is an organic radical. The novel monomers may be employed to produce novel copolymers useful as hydrogel, soft non-hydrogel and/or rigid gas permeable contact lens materials.

N-substituted imides as polymerization initiators

본 발명은 신규한 N-치환된 이미드 및 상기 N-치환된 이미드를 포함하는 중합성 조성물에 관한 것이다. 본 발명은 추가로 중합 개시제로서의 N-치환된 이미드의 용도에 관한 것이다. 상기 이미드는 화학식 I 및 화학식 II의 화합물이다. 화학식 I 화학식 II 위의 화학식 I 및 II에서, n은 1 또는 2이고, m은 1 또는 2이고, R 1 및 R 2 는 각각 서로 독립적으로 수소; 각각 할로겐, C 1 -C 4 알킬, 하이드록시, C 1 -C 6 알콕시, 카보닐, C 1 -C 6 알콕시카보닐에 의해 치환될 수 있는 C 1 -C 18 알킬, C 1 -C 18 알케닐, C 6 -C 14 아릴, 아르알킬, C 5 -C 12 사이클로알킬이거나; R 1 과 R 2 는, 인접한 -CO-N-CO- 그룹과 함께, 비수소원자를 50개 이하 갖고 화학식 의 구조 단위를 하나 이상 함유할 수 있는, 모노사이클릭, 비사이클릭 또는 폴리사이클릭 환을 형성할 수 있고, R 3 은, n이 1인 경우, C 1 -C 18 알킬, C 6 -C 14 아릴, 아르알킬, C 5 -C 12 사이클로알킬이거나; OR 10 또는 SR 11 , NR 12 R 13 이고, R 3 은, n이 2인 경우, C 2 -C 12 알킬렌, C 6 -C 14 아릴렌, 크실릴렌이고, R 4 및 R 5 는 R 1 및 R 2 에 상응하고, R 6 은, n이 1인 경우, 수소, C 1 -C 18 알킬, C 6 -C 14 아릴, 아르알킬, C 5 -C 12 사이클로알킬, NR 14 R 15 이고, R 6 은, n이 2인 경우, C 2 -C 12 알킬렌, C 6 -C 14 아릴렌, 크실릴렌이며, R 7 은 수소; 각각 할로겐, C 1 -C 4 알킬, 하이드록시, C 1 -C 6 알콕시, 카보닐, C 1 -C 6 알콕시카보닐에 의해 치환될 수 있는 C 1 -C 18 알킬, C 6 -C 14 아릴, 아르알킬, C 5 -C 12 사이클로알킬이거나; R 7 과 R 14 또는 R 7 과 R 15 는, R 7 에 결합한 N 원자와 함께, -NH-, -N(C 1 -C 8 알킬)-, -O- 및/또는 -S- 원자에 의해 임의로 차단된 5원 또는 6원 환을 형성한다. N-치환된 이미드, 중합 개시제, 열 경화, 이원 경화, 이중 경화.

Novel organic compound and method for producing radioactive halogen-labeled organic compound using the same

(과제) 방사성 할로겐으로 치환된 신-1-아미노- 3-시클로부탄카르복실산을, 선택적으로 제조하기 위한 표식 전구체 화합물 및 상기 화합물을 사용한 방사성 할로겐으로 치환된 신-1-아미노-3-시클로부탄카르복실산의 제조 방법을 제공한다. (해결 수단) 아미노기의 보호기를 프탈이미드기로 한 표식 전구체를 사용한다. 이 표식 전구체를 방사성 할로겐으로 표식하고, 탈보호를 행함으로써, syn형의 방사성 할로겐으로 치환된 1-아미노-3-시클로부탄카르복실산을 선택적으로 제조할 수 있다. 방사성 할로겐 표식 유기화합물

Copolymers of vinyl carbonate and vinyl carbamate as contact lens material

PROCESS FOR PREPARATION OF AN ENZYME CONJUGATE AND USEFUL COUPLING REAGENT FOR THIS EFFECT

a. Procédé de préparation d'un conjugué d'enzyme et réactif de couplage utile à cet effet b. On fait réagir une macromolécule contenant des groupes amino avec un radical R, réactif vis-à-vis de groupes amino, d'un réactif de couplage ayant la formule : at. A process for preparing an enzyme conjugate and a coupling reagent useful therefor b. A macromolecule containing amino groups is reacted with an R radical, reactive with amino groups, of a coupling reagent having the formula:

Methods and compositions for radiohalogen protein labeling

Methods and compositions are provided for labeling proteins with radiohalogen-label reagents. Radiohalogen-labeled proteins may be used for imaging studies, as therapeutics and in diagnostic tests. The [125I] HIP-DOTA label reagent 6 is prepared by an efficient and convenient process.

DIPHENYL ETHER HYDRAZINES, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS HERBICIDES

L'INVENTION A POUR OBJET DE NOUVELLES HYDRAZINES D'ETHER DIPHENYLIQUE, EN PARTICULIER DES 2-NITRO-5-(PHENOXY SUBSTITUE) PHENYL-HYDRAZINES, UTILISABLES NOTAMMENT COMME HERBICIDES SELECTIFS. THE OBJECT OF THE INVENTION IS NEW HYDRAZINES OF DIPHENYL ETHER, IN PARTICULAR 2-NITRO-5- (PHENOXY SUBSTITUTES) PHENYL-HYDRAZINES, USED IN PARTICULAR AS SELECTIVE HERBICIDES.

NOVEL STABLE ACTIVE CARBAMATES, THEIR PREPARATION PROCESS AND THEIR USE FOR THE PREPARATION OF UREA

Substd. alkylene diamines for fixing dyes - prepd by condensation of alkylene diamines with diacyl cpds

N-acyloyl N'-alkyl alkylene diamines of formula (I): (where R is bivalent aliphatic, cycloaliphatic, aromatic or bicyclic forming with dicarbonyl amino a 5, 6 or 7 cycle; R1 is H or 8-12C alkyl, R2 is 8-22C alkyl; n- is 2-6), are used to promote the fixing of basic dyes to acrylic polymer fibres or acid modified polyesters and combine the excellent fixing props. of permanent fixers with the advantages of temporary fixers (better bath usage, short exhaustion times) without loss of effectiveness. (I) are prepd. by condensing N-alkyl alkylene diamines H2N-(CH2)nN(R')(R'') with a diacyl cpd. R-(C(=O)-X)2 (where each X is Cl, Br, -OH or may be together -O-).

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.

SUBSTITUTED 4-HYDROXYPHENYLTHIOALKYL DERIVATIVES, COMPOSITIONS CONTAINING THEM AND PROCESS FOR THEIR USE

Produced derivatives of dimethylbiguanide and applications as medicaments.

Patent FR2440943B1

METAL CHELATION COMPOUND, RADIOPHARMACEUTICAL, MANUFACTURING METHOD THEREOF AND DIAGNOSTIC KIT

Guanidinobenzoic ester derivative

Abstract of the Disclosure A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thromhosis. wherein X represents a group of the formula: in which Y is a group of the formula: -(CH2)m-, m being an integer of 2 or 3, or or a group of the formula: -OR in which R is a hydrogen atom or a lower alkyl group, and n represents an lnteger of 1 to 5.

Patent FR2201299A1

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).

?-Sulfone imides and preparation thereof

본 발명은 하나 이상의 이미드 기와 하나 이상의 술폰기를 포함하는 신규한 β-술폰 이미드 화합물과 그의 제조 방법을 제공한다. The present invention provides novel β-sulfone imide compounds comprising at least one imide group and at least one sulfone group and methods for their preparation. 비닐술폰, 이미드, β-술폰이미드, 제조방법 Vinyl sulfone, imide, β-sulfonimide, production method

N-acylpolyimides and their preparation process

Patent FR2520358B1

PERFECTED PROCESS FOR PREPARING ALPHA-METHYL-3,4-DIHYDROXYPHENYLALANINE ESTERS

Orange-navy blue azo dyes - used for polyester(s), also for cellulose acetate and polyamide

Azo dyes are of formula (I): are new: In (I) D is residue of a diazo component; R is H or opt. substd. aliphatic, cycloaliphatic, araliphatic or aromatic gp. or the gp. A' -X-CO-Y-A2-Z;R'=H, Me, Et, MeO or EtO; R2=H, Cl, Br, Me, Et, MeO, EtO, 1-4C aekanoylamino, benzoylamino, or 1-4C alkoxycarbonylamine; A'=2-4C alkylene; A2=1-4C alkylene; X= a direct bond, -O- or -NH-Z is heterocyclo e.g. (where B=H or Cl and n=0,1,2,3 or 4). Used as orange-red-violet-navy blue dyes for synthetic and semi-synthetic fibres, esp. polyesters, but also cellulose acetates and polyamides, having good fastness to light, wetting and heat-fixing.

Tertiary aryl amino acids

Method for the prepn. of alpha-(tert-aminophenyl) aliphatic carboxylic acids with the general formula (I) where R1=hydrogen or lower alkyl R2=hydrogen or hydrocarbon group with aliphatic or cycloaliphatic character, optionally unsatd. R3=opt. substd. hydrocarbon with aliphatic or cycloaliphatic character such as alkyl, alkenyl, alkoxy-alkyl, amino-alkyl, cycloalkyl, cycloalkenyl, cycloalkyl-alkyl, or cycloalkenylalkyl, and where there is a heteroatom this is sepd. from the nitrogen by at least two carbon atoms. R4=group with an aromatic character. Ph=1-3- or 1-4 phenylene group. and the functional acid- and amino-derivs. of (I). The cpds. with the formula (I) show anti-inflammatory activity.

Patent FR2015493A1

Isoindoline derivatives, processes for the preparation of these compounds and their use

Patent IN151843B

N, N-BIS-IMIDES FLUORES.

La présente invention concerne de nouveaux N,N-bis-imides fluorés de formule (CF DESSIN DANS BOPI) où R est un radial bivalent de formule (CF DESSIN DANS BOPI) Les composés sont tout particulièrement utiles comme monomères dans la préparation de polymères à haute performance.

Anti-inflammatory tert-aminophenyl aliphatic acids

Cpds. of general formula (I) or their functional derivs. and pharm. accept. salts. (I) R3R4N-Ph-CR1R2.COOH R1 = H, lower alkyl R2 = H, aliph. or cycloaliph. hydrocarbyl gp. Ph = phenylene residue, opt. substd. R3 = lower alkyl/alkenyl/HO-alkyl/alkoxyalkyl/aminoalkyl R4 = aliph., cycloaliph. or araliph. hydrocarbyl gp. opt. substd. (R2, R3 and R4 together contain is not 3C). alpha-(4-Me2N-phenyl)propionic acid (II); alpha-(4-methylethylaminophenyl)propionic acid and its Et ester. As anti-inflammatory agents. (a) A mixt. of 4-Me2N-acetophenone (50 g), morpholine (150 ml), S (9 g) and toluene-p-SO3H (2 g.) is refluxed for 15 hrs. to give 4-Me2N-phenylthioacetomorpholide, m.p.138-140 deg. (acetone), which (21 g.) is refluxed with conc. HCl (200 ml) for 2 hrs., the mixt. evapd. under reduced press. and the residue refluxed with satd. EtOH-HCl (75 ml) for 15 hrs. to give Et 4-Me2N-phenylacetate HCl, m.p.132-4 deg. (b) The free Et ester (from 10 g. salt) in ether is added dropwise to a mixt. of liq. NH3 (500 ml), Na (1.26 g.) and Fe(NO3)3.9H2O (crystal); after stirring for 1 hr., MeI (6.9 g.) is added dropwise and after a further 2 hrs., working up and hydrolysis with 25% NaOH yields (II), m.p.128-130 deg. (ether-petrol).

Alpha-amino-aldehydes prepn - by oxo reaction of amino-alkenes using a rhodium carbonyl catalyst

Material for forming organic film, substrate for manufacturing semiconductor device, method for forming organic film, patterning process, and compound for forming organic film

본 발명은 공기 중 뿐만이 아니라, 불활성 가스 중에서의 성막 조건에서도 경화하고, 부생물이 발생하지 않으며, 내열성이나, 기판에 형성된 패턴의 매립이나 평탄화 특성이 우수할 뿐만이 아니라, 기판에의 밀착성이 양호한 유기 하층막을 형성할 수 있는 이미드기를 함유하는 화합물을 제공하는 것을 목적으로 한다. 본 발명은 유기막 형성용 재료로서, (A) 하기 일반식 (1A) 또는 (1B)로 표시되는 유기막 형성용 화합물, 및 (B) 유기 용제를 함유하는 것임을 특징으로 하는 유기막 형성용 재료를 제공한다. 단, 상기 일반식 (1A)에 있어서, W 1 이 중 어느 하나일 때, R 1 은 중 어느 하나가 아니다. The present invention cures not only in air but also under the conditions of film formation in an inert gas, does not generate by-products, has excellent heat resistance, excellent embedding and planarization characteristics of patterns formed on the substrate, and good adhesion to the substrate. An object of the present invention is to provide a compound containing an imide group capable of forming an underlayer film. The present invention is a material for forming an organic film, comprising (A) a compound for forming an organic film represented by the following general formula (1A) or (1B), and (B) an organic solvent. provides However, in the general formula (1A), W 1 is When any one of R 1 is not one of

Curable epoxy resin compositions

LIGHT-REACTIVE POLYMER AND METHOD FOR THE PRODUCTION THEREOF

Detection of markers in nascent proteins

The invention is directed to methods for the non-radioactive labeling, detection, quantitation and isolation of nascent proteins translated in a cellular or cell-free translation system. tRNA molecules are misaminoacylated with non-radioactive markers which may be non-native amino acids, amino acid analogs or derivatives, or substances recognized by the protein synthesizing machinery. Markers may comprise cleavable moieties, detectable labels, reporter properties wherein markers incorporated into protein can be distinguished from unincorporated markers, or coupling agents which facilitate the detection and isolation of nascent,protein from other components of the translation system. The invention also comprises proteins prepared using misaminoacylated tRNAs which can be utilized in pharmaceutical compositions for the treatment of diseases and disorders in humans and other mammals, and kits which may be used for the detection of diseases and disorders.