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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Применить Всего найдено 5489. Отображено 200.
20-05-2008 дата публикации

ПРОИЗВОДНЫЕ БЕНЗОТИАЗОЛА, ХАРАКТЕРИЗУЮЩИЕСЯ АГОНИСТИЧЕСКОЙ АКТИВНОСТЬЮ К БЕТА-2-АДРЕНОРЕЦЕПТОРАМ

Номер: RU2324687C2
Принадлежит: НОВАРТИС АГ (CH)

Изобретение относится к соединениям общей формулы (I) и их фармацевтически приемлемым солям в качестве агонистов β2-адренорецептора, к способу их получения и применению, а также к фармацевтической композиции на их основе. Соединения могут найти применение для лечения состояний, которые можно предотвратить или снизить интенсивность симптомов при активации β2 -адренорецептора, например обструктивных или воспалительных заболеваний дыхательных путей. В общей формуле (I) X означает -R1-Ar-R2 или -Ra-Y; Ar означает фенилен, необязательно замещенный группой из ряда: галоген, гидрокси, C1-С10алкил, C1-С10алкокси, фенил, C1-С10алкокси, замещенный фенильной группой, или фенил, замещенный C1-С10 алкоксигруппой; R1 и R2присоединены к соседним атомам углерода в составе группы Ar, и либо R1 означает C1-С10алкилен, a R2 означает водород, C1-С10алкил или галоген, Ra означает связь или C1-С10алкилен, необязательно замещенный группой из ряда: гидрокси, C1-С10алкокси, C6-С10арил или C7-С14аралкил; Y означает ...

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27-02-2005 дата публикации

СИММЕТРИЧНЫЕ И НЕСИММЕТРИЧНЫЕ ПРОИЗВОДНЫЕ ДИФЕНИЛМОЧЕВИНЫ (ВАРИАНТЫ), ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СПОСОБ ПОДАВЛЕНИЯ РОСТА ОПУХОЛЕВЫХ КЛЕТОК, ОПОСРЕДОВАННОГО КИНАЗОЙ RAF

Номер: RU2247109C2
Принадлежит: БАЙЕР КОПЭРЕЙШН (US)

Изобретение относится к новым производным дифенилмочевины формулы (I) или их фармацевтически приемлемым солям, которые могут быть использованы при лечении опухолей, опосредованных киназой raf. В общей формуле (I) соединений настоящего изобретения: (I) А означает R3 означает Н, галоген, NO2, С1-10алкил, по выбору замещенный галогеном вплоть до полного замещения; С1-10алкокси, по выбору замещенный галогеном вплоть до полного замещения; R4, R5 и R6 каждый независимо означает Н, галоген, NO2, С1-10 алкил, по выбору замещенный галогеном вплоть до полного замещения; С1-10алкокси, по выбору замещенный галогеном вплоть до полного замещения; и либо один из R4, R5 и R6 по выбору означает -X-Y; либо два соседних R4, R5 и R6 могут быть объединены с основным фенильным кольцом с образованием нафтила или индольной группы, замещенной пиридинильной группой, Х означает -CH2-, -S-, -N(СН3)-, -NHC(O)-, -CH2-S-, -S-CH2, -С(O)-, или -О-. Значения других радикалов указаны в формуле изобретения. Изобретение также ...

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27-06-2009 дата публикации

ПРОИЗВОДНЫЕ БЕНЗИМИДАЗОЛА, БЕНЗОТИАЗОЛА И БЕНЗОКСАЗОЛА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ LTA4H

Номер: RU2359970C2

Изобретение относится к соединениям формулы (II) в качестве ингибитора лейкотриен А4-гидролазы (LTA4H) и их энантиомерам, рацематам и фармацевтически приемлемым солям, а также к способам лечения, способу ингибирования и фармацевтической композиции на их основе. Соединения могут найти применение для лечения и профилактики заболеваний, опосредованных LTA4H, например астмы, хронической обструктивной болезни легких, атеросклероза, ревматоидного артрита, рассеянного склероза, воспалительного заболевания кишечника и псориаза. В общей формуле (II) ! ! X выбран из группы, состоящей из О и S; Y выбран из группы, состоящей из СН2 и О; R4 представляет собой Н; R6 представляет собой Н или F; и R2' определен как R2, a R3' определен как R3, как следует ниже: R2 и R3, каждый, независимо выбран из группы, состоящей из А) Н, С1-7алкила, С3-7циклоалкила, где каждый из заместителей А) независимо замещен 0 или 1 RQ, и каждый из указанных RQ является заместителем при углероде, который, по крайней мере, на один ...

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27-06-2007 дата публикации

ПРОИЗВОДНЫЕ ТИАЗОЛА, ИМЕЮЩИЕ АНТАГОНИСТИЧЕСКУЮ, АГОНИСТИЧЕСКУЮ ИЛИ ЧАСТИЧНО АГОНИСТИЧЕСКУЮ СВ1-АКТИВНОСТЬ

Номер: RU2301804C2

Изобретение относится к новым производным тиазола, которые являются сильными антагонистами, агонистами или частичными агонистами каннабиноидного CB1 рецептора. Соединения имеют общую формулу (I) в которой R и R1-R4 имеют значения, приведенные в формуле изобретения. Изобретение также относится к применению соединений формулы (I) или их стереоизомеров для получения фармацевтической композиции, и относится к промежуточным соединениям формулы (V) в которой R2 и R8 имеют значения, приведенные в формуле изобретения. 3 н. и 2 з.п. ф-лы, 1 табл.

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19-06-1995 дата публикации

ПРОИЗВОДНЫЕ 2-ИМИНО-БЕНЗОТИАЗОЛИНОВ, ИХ ЭНАНТИОМЕРЫ ПРИ НАЛИЧИИ АСИММЕТРИЧНОГО ЦЕНТРА И ИХ КИСЛОТНО-АДДИТИВНЫЕ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Номер: RU2037489C1
Принадлежит: Рон-Пуленк Санте (FR)

Сущность изобретения: производные 2-иминобензотиазолинов ф-лы I, где R1 -полифтор C1-C4 алкил или полифтор C1-C4 алкоксигруппа, R2 -группа ф-лы CH2[CH(R4)]n-R3, где R3-qu-(C1-C4) алкиламиногруппа, 1-пиперидинил, 1-пирролидинил, меркаптогруппа, C1-C4 ацилтиогруппа, C1-C4 алкилтиогруппа, C1-C4 алкилсульфинил- или C1-C4 алкилсульфонилгруппа: R4 -атом водорода или C1-C4 алкил и n=0 или 1: или R2 -группа ф-лы II, их энантиомеры при наличии асимметричного центра, их кислотно-аддитивные фармацевтически приемлемые соли и фармацевтическая композиция на их основе. Структура соединения ф-лы I и II (см. чертеж). 2 с.п. ф-лы, 1 ил.

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27-06-1998 дата публикации

ПРОИЗВОДНЫЕ 7-(2-АМИНОЭТИЛ)БЕНЗОТИАЗОЛОНА ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ, ПРОИЗВОДНЫЕ N-[2-(4-ГИДРОКСИ-2-ОКСО-3H-1,3-БЕНЗОТИАЗОЛ-7-ИЛ)ЭТИЛАМИДА]ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ПРОЯВЛЯЮЩАЯ АГОНИСТИЧЕСКУЮ АКТИВНОСТЬ В ОТНОШЕНИИ β2-АДРЕНОРЕЦЕПТОРОВ

Номер: RU2114108C1

Использование: в химии гетероциклических соединений, проявляющих агонистическую активность в отношении β2-адренорецепторов. Сущность изобретения: производные 7-(2-аминоэтил)бензтиазолона формулы I где X и Y независимо означают -S(O)n- или -O-, n означает 0,1 или 2, p, q и r независимо означают 2 или 3, Z означает фенил с возможным замещением галогеном, -OR1, NO2 или NH2 или Z представляет собой 5- или 6-членный ненасыщенный гетероцикл, содержащий N или S, при этом R1 означает водород или алкил C1 - C6 или их фармацевтически приемлемые соли. Описаны способы их получения и содержащие их фармацевтические композиции, а также промежуточные соединения для их получения формулы Va где p, q и r, X, Y имеют указанные значения, а Z - фенил, необязательно замещенный атомом галогена, NO2, NH2 или OR1, где R1 - H или C1 - C6-алкил. 4 с. и 7 з.п.ф-лы, 3 табл.

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27-07-2006 дата публикации

БЕНЗИМИДАЗОЛЬНЫЕ, БЕНЗТИАЗОЛЬНЫЕ И БЕНЗОКСАЗОЛЬНЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ LTA4H

Номер: RU2006102510A
Принадлежит:

... 1. Способ лечения или предупреждения LТА4Н-опосредованного состояния у субъекта, предусматривающий введение субъекту терапевтически эффективного количества, по крайней мере, одного модулятора LТА4Н, выбранного из соединений формулы (I) где Х выбран из группы, состоящей из NR5, О и S, где R5 представляет собой один из Н и СН3; Y выбран из группы, состоящей из СН2 и О; Z выбран из группы, состоящей из О и связи; W выбран из группы, состоящей из СН2 и CHR1-СН2, где R1 представляет собой Н или ОН, и где связанная с R1 углеродная группа в указанном CHR1-СН2 не связана непосредственно с атомом азота, с которым связан указанный W; R4 выбран из группы, состоящей из Н, ОСН3, Cl, F, Br, I, ОН, NH2, CN, CF3 и СН3; R6 представляет собой Н или F; и R2 и R3 каждый независимо выбран из группы, состоящей из А) Н, С1-7алкила, С3-7алкенила, где атом углерода в указанном алкениле, который связан с атомом азота, имеет только простые связи; С3-7алкинила, где атом углерода в указанном алкиниле, который связан ...

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10-01-2009 дата публикации

ПРОИЗВОДНЫЕ 5-ГИДРОКСИБЕНЗОТИАЗОЛА В КАЧЕСТВЕ АГОНИСТОВ β2 АДРЕНОРЕЦЕПТОРОВ

Номер: RU2007124329A
Принадлежит:

... 1. Соединение формулы I в свободной форме, или в форме соли, или сольвата, где Т означает водород или C1-С10 алкил, необязательно замещенный в одном, двух или трех положениях группой C1-С10алкокси, -NR1R2, 5- или 6-членным гетероциклическим циклом, содержащим в цикле по меньшей мере один гетероатом, выбранный из группы, включающей атом азота, кислорода и серы, или Сз-С15карбоциклической группой, причем указанная С3-С15 карбоциклическая группа необязательно замещена в одном, двух или трех положениях группой галоген, C1-С10 алкил, С3-С10циклоалкил, галоген(С1-С10)алкил, -NR3R4, 5- или 6-членным гетероциклическим циклом, содержащим в цикле по меньшей мере один гетероатом, выбранный из группы, включающей атомы азота, кислорода и серы, или группой С1-С12 алкокси, необязательно замещенной в одном, двух или трех положениях С6-С10 арилом, или Т означает С3-С15карбоциклическую группу, необязательно замещенную в одном, двух или трех положениях группой галоген, C1-С10 алкил, С3-С10 циклоалкил, галоген ...

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20-06-2003 дата публикации

НОВЫЙ СПОСОБ ПОЛУЧЕНИЯ СОЕДИНЕНИЙ БЕНЗОТИАЗОЛОНА

Номер: RU2001126357A
Принадлежит:

... 1. Способ получения соединения формулы (I) или его фармацевтически приемлемой соли или сольвата где Ph представляет фенильную группу, включающий взаимодействие соединения формулы (II) или его соли с соединением формулы (III) в присутствии растворителя и, необязательно, третичного аминного основания и, при необходимости, превращение соединения формулы (I) в его фармацевтически приемлемую соль или сольват. 2. Способ по п.1, в котором третичным аминным основанием является алифатический амин. 3. Способ по п.1 или 2, в котором растворителем является спирт. 4. Способ по любому из пп.1-3, в котором фармацевтически приемлемой солью является кислотно-аддитивная соль, полученная из хлористоводородной, бромистоводородной, борной, фосфорной, серной, уксусной, винной, малеиновой, лимонной, янтарной, аскорбиновой, бензойной, 4-метоксибензойной, 2- или 4-гидроксибензойной, 4-хлорбензойной, бензолсульфоновой, пара-толуолсульфоновой, нафталинсульфоновой, метансульфоновой, сульфаминовой, салициловой, дифенилуксусной ...

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20-10-2011 дата публикации

СПОСОБ ПОЛУЧЕНИЯ 2(3Н)-БЕНЗОТИАЗОЛОНА И НЕКОТОРЫХ ПРОИЗВОДНЫХ НА ЕГО ОСНОВЕ

Номер: RU2010114142A
Принадлежит:

... 1. Способ получения 2(3H)-бензотиазолона (II), заключающийся в кипячении исходного бис-(2,2'-диметоксикарбоксамидо)фенилдисульфида (I) с цинковой пылью в течение 7,5 ч в ледяной уксусной кислоте, отделении солей цинка, разбавлении фильтрата ледяной водой, фильтровании кристаллического продукта и его промывании разбавленной НСl (1:1), водой и последующей сушке на воздухе и перекристаллизации из этанола. ! ! 2. Способ получения 3-2-[2-оксо-1,3-бензотиазол-3(2Д)-ил]этил-1,3-бензотиазол-2(3Д)-она (III), заключающийся в кипячении 2(3Н)-бензотиазолона (II) с 1,2 дибромэтаном в ацетоне в присутствии К2СО3, добавлении воды, обработке смеси диэтиловым эфиром, промывании органической фазы 10%-ным водным раствором NaOH, водой, сушке безводным карбонатом калия, удалении растворителя и перекристаллизации из метанола. ! ! 3. Способ получения 3-(2-хлорацетил)-1,3-бензотиазол-2(3H)-она (IV), заключающийся в кипячении 2(3H)-бензотиазолона (II) в безводном бензоле с хлорацетилхлоридом в течение 10 ч, промывании ...

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10-05-2001 дата публикации

TESTSATZ UND VERFAHREN ZUR BESTIMMUNG VON PESTIZIDEN

Номер: DE0069330077D1
Принадлежит: CHARM SCIENCES INC, CHARM SCIENCES, INC.

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25-11-1976 дата публикации

VERWENDUNG VON 3-SUBSTITUIERTEN BENZOTHIAZOLINEN ALS PFLANZENWUCHSREGULIERENDE MITTEL

Номер: DE0002620789A1
Принадлежит:

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01-06-1989 дата публикации

VERFAHREN ZUR HERSTELLUNG VON 1-THIOCYANATOMETHYLETHERN

Номер: DE0003740285A1
Принадлежит:

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07-05-1975 дата публикации

Fungicidal seed dressings - contg. substd benzazole derivs

Номер: DE0002355092A1
Принадлежит:

Fungicidal agents for use as seed dressings contain substd. benzazole derivs. of formula (I):- (where X is NH, NR2, S or O; Y is NH, S or -SCOO-; R1 is alkyl, alkenyl, alkynyl a dienyl residue, furfuryl, thienyl, CH2SCH3 or CH2OCH3; R2 is 1-4C alkylcarbamoyl; and R3 is H or one or more substituents selected from 1-4C aliphaticyl, F, Cl, Br, pseudohalogen (CNS, CN) and NO2), opt. in admixture with known fungicides and/or insecticides. Examples of cpds. (I) are 2-propylthio-benzimidazole, 2-propylthio-benzthiozole and 2-allylthio-benzoxazole.

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19-09-1985 дата публикации

Process for the preparation of benzoxazolyl- and benzothiazolyloxyphenoxypropionic acid derivatives

Номер: DE0003409201A1
Принадлежит:

A process for the preparation of benzoxazolyl- and benzothiazolyloxyphenoxypropionic acid derivatives of the formula I in which X denotes oxygen or sulphur or a group of the formula =N-alkyl, R denotes halogen or CF3, n denotes the figures 0 to 3 and R<1> denotes optionally substituted alkyl or cycloalkyl, by reaction of compounds of the formula II in which X, R, n and R<1> have the abovementioned meanings, with compounds of the formula III in which Y is chlorine and R<1> has the abovementioned meaning, in the presence of catalytic amounts of metal iodides and/or 2-iodopropionic acid esters of the formula III where Y = I.

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11-02-1971 дата публикации

Номер: DE0002037999A1
Автор:
Принадлежит:

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03-06-1971 дата публикации

Номер: DE0002056224A1
Автор:
Принадлежит:

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29-05-1975 дата публикации

SENSITIVE SILVER HALIDE PHOTOGRAPHIC MATERIALS AND COMPOUNDS FOR USE THEREIN

Номер: GB0001395767A
Автор:
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... 1395767 Silver halide materials EASTMAN KODAK CO 3 May 1972 [3 May 1971] 20600/72 Heading G2C [Also in Division C2] A sensitive photographic material comprises in a silver halide layer or a layer adjacent thereto a compound of general Formula:- in which A is a cation, X is S or Se, R1 to R5 each represent H, optionally substituted alkyl, or a sulphonic acid or sulphonate group provided that at least one of R1 to R5 represent a sulphonic acid or sulphonate group, m and n are each 0 or an integer, the sum of m and n being from 1 to 8, or a compound of general Formula:- in which A is a cation, X is S or Se, R6 is aryl or optionally substituted alkyl, R7 is aryl or optionally substituted alkyl, and # each represent H, optionally substituted alkyl or an aryl group or alternatively they are electrons which form a second bond between the carbon atoms carrying Y and L; Y and Z each represent H, optionally substituted alkyl or an aryl group, ...

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26-11-1975 дата публикации

SILVER HALIDE LIGHT-SENSITIVE PHOTOGRAPHIC MATERIALS

Номер: GB0001415010A
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27-11-1991 дата публикации

FUNGICIDES

Номер: GB0009122098D0
Автор:
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11-08-1982 дата публикации

Process for producing N-(halomethyl) acylamides

Номер: GB0002092148A
Автор: Chupp, John Paul
Принадлежит:

The disclosure herein relates to a new process for the preparation of N-(halomethyl)acylamides by reacting the corresponding N-(alkoxymethyl)acylamide with thionyl chloride or thionyl bromide in the presence of a Lewis Acid catalyst.

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28-02-1996 дата публикации

Pharmaceutically active compounds

Номер: GB0009526511D0
Автор:
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31-12-2006 дата публикации

Substituted aryl acylthioureas and related compounds; inhibitors of viral replication

Номер: AP0200603808D0
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05-04-2002 дата публикации

Novel hexanoic acid derivatives.

Номер: AP0000001056A
Принадлежит:

... bstract: Compounds of the formula Which are potent and selective inhibitors of MIP-l(a) binding to its receptor CCR1 found on inflammatory and immunomodulatory cells (preferably leukocytes and lymphocytes). The compounds are useful in the treatment of inflammation particularly in autoimmune disease.

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31-12-2002 дата публикации

Biciclic cyclohexylamines and their use as NMDA receptor antagonists.

Номер: AP2002002697A0
Принадлежит:

Described are bicycle-substituted cyclohexylamines of Formula (1) and their pharmaceutically acceptable salts thereof. The (I) compounds are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, cerebral ischemia, cardiac arrest, stroke, and Parkinson's disease. The substituents are defined in the specification.

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31-12-2006 дата публикации

Substituted aryl acylthioureas and related compounds; inhibitors of viral replication

Номер: AP2006003808A0
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30-06-2004 дата публикации

N,N' -substituted-1,3-diamino -2-hydroxypropane derivatives.

Номер: AP2004003049A0
Принадлежит:

Disclosed are compounds of the formula (0, wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of betasec-retase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.

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30-06-2005 дата публикации

Substituted aryl thioureas and related compounds; inhibitors of viral replication

Номер: AP2005003319A0
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30-06-2011 дата публикации

Therapeutic antiviral poptides.

Номер: AP2011005695A0
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30-06-1981 дата публикации

Derived from aryloxy-propionic acids optically active, usable like weedkillers.

Номер: OA0000006138A
Автор:
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11-12-2003 дата публикации

Bicyclic cyclohexylamines and their use as NMDA receptor antagonists.

Номер: OA0000012275A
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31-05-1981 дата публикации

Heterocyclic and produced phenylic ethers weedkillers which contain some.

Номер: OA0000005766A
Автор:
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30-06-2005 дата публикации

Substituted aryl thioureas and related compounds; inhibitors of viral replication

Номер: AP0200503319A0
Принадлежит:

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30-06-2011 дата публикации

Therapeutic antiviral poptides.

Номер: AP0201105695D0
Принадлежит:

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30-06-2005 дата публикации

Substituted aryl thioureas and related compounds; inhibitors of viral replication

Номер: AP0200503319D0
Принадлежит:

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31-12-2002 дата публикации

Bicyclic cyclohexylamines and their use as nmd

Номер: AP0200202697D0
Автор:
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31-12-2006 дата публикации

Substituted aryl acylthioureas and related compounds; inhibitors of viral replication

Номер: AP0200603808A0
Принадлежит:

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31-12-2002 дата публикации

Bicyclic cyclohexylamines and their use as nmd

Номер: AP0200202697A0
Автор:
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30-06-2011 дата публикации

Therapeutic antiviral poptides.

Номер: AP0201105695A0
Принадлежит:

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10-02-1987 дата публикации

HERBICIDES MEANS

Номер: AT0000382295B
Автор:
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11-10-1982 дата публикации

HERBICIDES MEANS

Номер: AT0000368357B
Автор:
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15-02-2010 дата публикации

N-ALKYNYL-2-HETEROARYLOXYALKYLAMIDE FOR USE AS FUNGICIDES

Номер: AT0000455770T
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15-07-1981 дата публикации

HERBIZIDE MITTEL

Номер: ATA642377A
Автор:
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15-02-2007 дата публикации

ACETYLENE DERIVATIVES AS INHIBITORS OF HISTONDEACETYLASE

Номер: AT0000353319T
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15-01-1997 дата публикации

FUNGICIDES

Номер: AT0000147374T
Принадлежит:

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15-03-1996 дата публикации

CHEMILIMINESZENTE 1,2-DIOXETAN-VERBINDUNGEN

Номер: AT0000135353T
Принадлежит:

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15-09-1995 дата публикации

ARYL FLUORINE ALKENE AMIDES AND YOUR USE AS PESTICIDES.

Номер: AT0000127790T
Принадлежит:

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15-11-1983 дата публикации

PROCEDURE FOR the PRODUCTION OF 2CHLORBENZOTHIAZOL.

Номер: AT0000005192T
Принадлежит:

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15-12-1984 дата публикации

USE OF 2-PROPARGYLOXY-BENZAZOLEN AS SYNERGISTEN.

Номер: AT0000010630T
Принадлежит:

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15-04-1984 дата публикации

PROCEDURE FOR THE PRODUCTION OF N (HALO METHYL) ECYL AMIDES.

Номер: AT0000006774T
Автор: CHUPP, JOHN PAUL
Принадлежит:

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15-05-1995 дата публикации

PESTICIDES HETERO-CYCLIC CONNECTIONS.

Номер: AT0000122040T
Принадлежит:

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15-11-1997 дата публикации

PRODUCTION AND USE OF FLUORESCENT BENZOTHIAZOLDERIVATEN

Номер: AT0000159760T
Принадлежит:

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15-05-1989 дата публикации

2-PHENOXYPROPIONS of URE CYANAMIDES.

Номер: AT0000042741T
Принадлежит:

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15-03-2006 дата публикации

2-BROM/CHLOR-THIAZOLIUMSALZE AND YOUR USE AS CONDENSATION REAGENTS

Номер: AT0000317843T
Принадлежит:

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10-08-1976 дата публикации

PROCEDURE FOR the PRODUCTION OF 4-CHLOR-2-HYDROXYBENZOTHIAZOL

Номер: AT0000331240B
Автор:
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15-06-2004 дата публикации

BENZAZOL CONNECTIONS AND YOUR USE

Номер: AT0000268327T
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15-01-2000 дата публикации

FIBRINOGENREZEPTOR ANTAGONIST

Номер: AT0000188379T
Принадлежит:

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04-04-2013 дата публикации

CARBOXYLATION CATALYSTS

Номер: US20130085276A1
Принадлежит:

The use of a complex of the form Z—M—OR in the carboxylation of a substrate is described. The group Z is a two-electron donor ligand, M is a metal and OR is selected from the group consisting of OH, alkoxy and aryloxy. The substrate may be carboxylated at a C—H or N—H bond. The metal M may be copper, silver or gold. The two-electron donor ligand may be a phosphine, a carbene or a phosphite ligand. Also described are methods of manufacture of the complexes and methods for preparing isotopically labelled caboxylic acids and carboxylic acid derivatives. 134-. (canceled)25. A method of carboxylation of a substrate , the method comprising;{'sub': '2', 'contacting a complex of the form Z—M—OR ,wherein the group Z is a two-electron donor ligand, M is a metal, and OR is selected from the group consisting of OH, alkoxy and aryloxy; with a substrate and a source of CO.'}26. The method according to claim 25 , wherein the metal M is selected from the group consisting of copper claim 25 , silver and gold.27. The method according to claim 25 , wherein the carboxylation is carried out in the presence of a base.28. The method according to claim 27 , wherein the base is an alkali metal hydroxide or alkoxide.29. The method according to claim 25 , wherein the two-electron donor ligand Z is selected from the group consisting of phosphines claim 25 , carbenes claim 25 , or phosphites.30. The method according to claim 29 , wherein the two-electron donor ligand Z is a nitrogen containing heterocyclic carbene ligand.33. The method according to claim 26 , wherein the complex is selected from the group consisting of: [M(OH)(IMes)] claim 26 , [M(OH)(SIMes)] claim 26 , [M(OH)(IPr)] claim 26 , [M(OH)(ItBu)] claim 26 , and [M(OH)(SIPr)] claim 26 , where M is Au claim 26 , Ag or Cu.34. The method according to claim 25 , wherein the substrate is carboxylated at a C—H or N—H bond.35. The method according to claim 25 , wherein the substrate is a substituted or unsubstituted aromatic compound.36. The ...

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11-04-2013 дата публикации

Benzoxazole Derivatives Having Inhibitory Activity Against Interleukin-6, Preparation Method Thereof, and Pharmaceutical Composition Containing the Same

Номер: US20130090480A1
Принадлежит:

The present invention relates to benzoxazole derivatives represented by the Formula 1, which has an inhibitory activity against interleukin-6 (IL-6), a method for preparation thereof, and a pharmaceutical composition containing the same. The compound represented by the Formula 1 according to the present invention has a superior inhibitory activity against interleukin-6, and therefore, can be practically applied for prevention and treatment of diseases caused by abnormal interleukin-6 activity. 3. The compound according to characterized in that said Ris phenyl substituted with two identical or different substitutents each independently selected from the group consisting of halogen claim 1 , nitro claim 1 , Chaloalkyl claim 1 , and Calkoxy.4. The compound according to characterized in that said Ris phenyl substituted with halogen and nitro claim 3 , phenyl substituted with halogen and Chaloalkyl claim 3 , phenyl substituted with two halogens claim 3 , or phenyl substituted with two Calkoxy.5. The compound according to characterized in that said Ris phenyl substituted with three Calkoxy.7. The compound according to characterized in that said Ris trifluoromethyl.8. The compound according to characterized in that the compound is selected from the group consisting of:N-(2-(4-ethylphenyl)benzo[d]oxazole-2,5-diamine,N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-2-phenylacetamide,N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide,4-chloro-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide,2-chloro-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-4-nitrobenzamide,2-chloro-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-5-nitrobenzamide,3,4-dichlorobenzamide-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide,3-(chloromethyl)-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide,4-ethyl-N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)benzamide,N-(2-(4-ethylphenylamino)benzo[d]oxazol-5-yl)-3-fluoro-5-(trifluoromethyl)benzamide,2-ethoxy-N-(2-(4-ethylphenylamino)benzo[d] ...

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23-05-2013 дата публикации

COMPOUNDS AND METHODS FOR ASSAYING REDOX STATE OF METABOLICALLY ACTIVE CELLS AND METHODS FOR MEASURING NAD(P)/NAD(P)H

Номер: US20130130289A1
Принадлежит: PROMEGA CORPORATION

The present invention provides compounds and methods for assaying redox state of metabolically active cells and methods for assaying enzyme activity and/or metabolite level by coupling to redox defining co-factor NAD(P)/NAD(P)H measurement. 146.-. (canceled)51. A method for analyzing the redox state of a metabolically active cellular sample:{'claim-ref': {'@idref': 'CLM-00047', 'claim 47'}, 'a. contacting the metabolically active cellular sample with a compound according to to form a first mixture;'}b. contacting the first mixture with a luciferase reaction mixture; andc. detecting bioluminescence.52. The method of claim 51 , wherein the metabolically active cellular sample comprises a cell claim 51 , a physiological fluid claim 51 , isolated organelles claim 51 , mitochondria or a mitochondrial complex or enzyme.53. The method of claim 51 , wherein the bioluminescence is indicative of cell viability.54. The method of claim 51 , wherein the metabolically active cellular sample is in an animal.55. A method for detecting cellular metabolites in a sample comprising claim 51 ,{'claim-ref': {'@idref': 'CLM-00047', 'claim 47'}, 'a. contacting the sample with a compound according to , an amplification enzyme system, NAD or NADP, diaphorase, and a luciferase reaction mixture; and'}b. detecting bioluminescence.56. The method of claim 55 , wherein the compound claim 55 , amplification enzyme claim 55 , diaphorase claim 55 , NAD or NADP and luciferase reaction mixture are in a single composition.57. A method of screening for a compound that affects cell toxicity claim 55 , cell viability or the redox state of a cell comprising:a. contacting a cell with a test compound to form a first mixture;{'claim-ref': {'@idref': 'CLM-00047', 'claim 47'}, 'b. contacting the first mixture a compound according to ;'}c. contacting the mixture of b) with a luciferase reaction mixture; andd. detecting a bioluminescent signal, wherein the signal is indicative of the test compound's effect on the ...

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19-09-2013 дата публикации

NITROBENZOTHIAZOLE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC APPLICATIONS THEREOF

Номер: US20130245008A1
Автор: Pellet Alain
Принадлежит: SANOFI

The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis. 2. The compound of formula (I) as claimed in claim 1 , characterized in that Rrepresents:{'sub': 1', '4, 'claim-text': one or more fluorine atoms;', 'a phenyl optionally substituted with one or more groups chosen, independently of one another, from an OH, methoxy, morpholine or trifluoromethoxy group and a chlorine or fluorine atom;', 'a pyridinyl, isoxazolyl, pyrazolyl, thienyl, benzoxazolyl, tetrahydroisoquinolinyl, quinolinyl and thiazolyl group optionally substituted with one or more groups chosen, independently of one another, from a methyl or ethyl group or a chlorine atom;', 'an unsubstituted pyridinyl-NH group;', 'an unsubstituted cyclohexyl group;', 'a tetrahydropyranyl group, a morpholinyl group, a pyrrolidinyl group and a thiomorpholinyl group optionally substituted with one or more groups chosen, independently of one another, from a methyl, phenyl and benzyl group;, 'a (C-C)alkyl radical substituted withor{'sub': 1', '4, 'claim-text': 'an unsubstituted phenyl;', 'a (C-C)alkyl radical disubstituted with 'an unsubstituted morpholinyl group;', 'and'}in the form of a base or of an addition salt with an acid or with a base.3. The compound of formula (I) as claimed in claim 1 , characterized in that it corresponds to the following compounds:N-[2-(4-chlorophenyl)ethyl]-7-nitro-5-(trifluoromethyl)-1,3-benzothiazole-2-carboxamide;7-nitro-N-[2-(tetrahydro-2H-pyran-4-yl)ethyl]-5-(trifluoromethyl)-1,3-benzothiazole-2-carboxamide;7-nitro-N-(2-pyridin-2-ylethyl)-5-(trifluoromethyl)-1,3-benzothiazole-2-carboxamide;7-nitro-5-(trifluoromethyl)-N-(3,3,3-trifluoropropyl)-2-benzothiazolecarboxamide;7-nitro-N-(pyridin-2-ylmethyl)-5-(trifluoromethyl)-1,3-benzothiazole-2-carboxamide;N-[3-(4-morpholinyl)propyl]-7-nitro-5-(trifluoromethyl)-2-benzothiazolecarboxamide;N-[2-(4-methoxyphenyl)ethyl]-7-nitro-5-(trifluoromethyl)-1,3-benzothiazole-2- ...

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13-02-2014 дата публикации

SUBSTITUTED 1,3-BENZOTHIAZOL-2(3H)-ONES AND [1,3]THIAZOLO[5,4-B]PYRIDIN-2(1H)-ONES AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2

Номер: US20140045829A1
Принадлежит: Merck Sharp & Dohme Corp.

The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved. 2. The compound according to wherein Ris (CHR)pCcycloalkyl claim 1 , —(CH)piperidinyl claim 1 , (CH)phenyl claim 1 , and Calkyl claim 1 , said cycloalkyl claim 1 , piperidinyl claim 1 , phenyl and alkyl optionally substituted with 1 to 3 groups of R.3. The compound according to wherein Ris optionally substituted (CHR)pCcycloalkyl.4. The compound according to wherein Ris —(CH)pcyclopropyl claim 3 , said cyclopropyl optionally substituted with 0-2 groups of halo.5. The compound according to wherein Ris optionally substituted Calkyl.6. The compound according to wherein Ris selected from the group consisting of: halo claim 1 , Calkyl claim 1 , Ccycloalkyl claim 1 , —OCheterocyclyl claim 1 , Calkoxy claim 1 , Ccycloalkoxy claim 1 , —CN claim 1 , —OH claim 1 , —C(O)—Calkyl claim 1 , —(CH)pCaryl claim 1 , —(CH)pCheterocyclyl claim 1 , CF claim 1 , —C(O)-aryl claim 1 , and —(CH)pNHC(O)OCalkyl claim 1 , said alkyl claim 1 , aryl and heterocyclyl optionally substituted with 1 to 3 groups of OH claim 1 , CN claim 1 , halo claim 1 , carboxy claim 1 , —C(O)—O—Calkyl claim 1 , Calkyl claim 1 , Calkoxy claim 1 , Calkylamino claim 1 , phenyl and Cheterocycle.7. The compound according to wherein Ris Caryl claim 1 , Cheterocyclyl claim 1 , OCaryl or OCheterocyclyl optionally substituted with 1 to 3 substituents R.8. The compound according to wherein Ris selected from ...

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21-01-2016 дата публикации

Luciferin derivatives from bicyclic reactants and aminothiol derivatives and methods of use thereof

Номер: US20160015835A1
Принадлежит: UNIVERSITY OF CALIFORNIA

The present disclosure features a condensation reaction and a luciferin-unmasking reaction that can be carried out under physiological conditions. In general, the condensation reaction involves reacting a bicyclic reactant with an aminothiol derivative, generating a luciferin or luciferin derivative. A luciferin can provide detectable luminescence. A luciferin derivative can be unmasked to provide detectable luminescence in a luciferin-unmasking reaction. The present disclosure provides bicyclic reactants and aminothiol derivatives suitable for use in the condensation reaction. The condensation and luciferin-unmasking reactions find use in a variety of applications, which are also provided.

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15-01-2015 дата публикации

HIGHLY SELECTIVE SIGMA RECEPTOR LIGANDS

Номер: US20150018339A1
Принадлежит:

Compounds having the general formula II, III, or IV 6. The compounds of claim 1 , wherein Y=O and Z=O.7. The compounds of claim 1 , wherein Y=S and Z=S.8. The compounds of claim 1 , where Y=CHor Y=CH.10. The compounds of claim 1 , wherein X is fluoro.11. The compounds of claim 1 , wherein X is trifluoromethyl.12. The compounds of claim 1 , wherein the alkylene bridging moiety is substituted by methyl or trifluoromethyl.13. A method of treating a subject for alleviation of affects in the subject resulting from drug intake or drug abuse by the subject comprising administering to the subject a therapeutically effective amount of at least one compound according to .14. A method according to wherein the drug abuse or drug intake results from methamphetamine intake or methamphetamine abuse by the subject.15. A method according to wherein the drug intake or drug intake results from cocaine abuse or cocaine intake by the subject.16. A method of treating a subject having a need for therapy involving sigma receptors comprising administering to the subject an effective amount of at least one compound of .17. A method of treating a subject to prevent neurotoxic effects resulting from drug abuse or drug intake by the subject comprising administering to the subject a therapeutically effective amount of at least one compound according to .18. A radioligand composition comprising at least one compound according to wherein at least one compound contains a radioactive element.19. A pharmaceutical composition comprising at least one compound according to and an acceptable carrier or excipient.22. A method of treating a subject for alleviation of affects in the subject resulting from drug intake or drug abuse by the subject comprising administering to the subject a therapeutically effective amount of the compound according to .23. A method according to wherein the drug abuse or drug intake results from methamphetamine intake or methamphetamine abuse by the subject.24. A method ...

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26-01-2017 дата публикации

PROCESS FOR THE SYNTHESIS OF CHLORZOXAZONE

Номер: US20170022172A1
Принадлежит:

Disclosed is a process for the synthesis of chlorzoxazone (1) from 4-chloro-2-aminophenol and ethyl chloroformate in the presence of a base. 2. A process according to wherein the solvent is selected from acetonitrile claim 1 , N claim 1 ,N-dimethylformamide claim 1 , dichloromethane claim 1 , toluene claim 1 , acetone claim 1 , ethyl acetate or water.3. A process according to wherein the base is selected from potassium carbonate claim 1 , potassium bicarbonate claim 1 , sodium carbonate and sodium bicarbonate.4. A process according to wherein the molar ratio of 4-chloro-2-aminophenol to ethyl chloroformate ranges from 0.9 to 1.55. A process according to wherein the reaction is carried out at a temperature ranging from 0° C. to 80° C. or the reflux temperature in the case of low-boiling solvents.6. A process according to claim 1 , wherein the solvent is selected from ethyl acetate claim 1 , acetonitrile claim 1 , N claim 1 ,N-dimethylformamide or water.7. A process according to claim 1 , wherein the base is potassium carbonate.8. A process according to claim 1 , wherein the molar ratio of 4-chloro-2-aminophenol to ethyl chloroformate ranges from 1.2 to 1.4.9. A process according to claim 1 , wherein the reaction is carried out at a temperature of 55-60° C. This application claims priority to and the benefit of Italian Patent Application No. 102015000037594 filed on Jul. 23, 2015, incorporated herein by reference in its entirety.Chlorzoxazone, 5-chlorobenzo[d]oxazol-2(3H)-one, is a muscle relaxant which acts at central level and is used in the treatment of muscle spasms and the resulting pain. Chlorzoxazone acts on the spinal cord, by depressing/suppressing the reflexes.A number of examples of synthesis of chlorzoxazone (1) from 4-chloro-2-aminophenol, into which an acyl group, usually from urea or phosgene, is inserted, are described in the literature. Cases in which the carbonyl group inserted is directly gaseous CO are also reported.A representative example of the ...

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02-02-2017 дата публикации

MIF INHIBITORS

Номер: US20170029387A1
Принадлежит:

Compounds of Formula (I′), and the use of the compounds of Formula (I′) as inhibitors of macrophage migration inhibitory factor (MIF). The use of compounds of Formula (I′) or pharmaceutical compositions thereof and method of using them, for treating disorders, diseases or conditions related to MIF. 111-. (canceled)15. The compound according to claim 12 , wherein Rrepresents H.16. The compound according to claim 12 , selected from:3-(2-methoxybenzyl)benzo[d]oxazole-2(3H)-thione;3-(4-bromobenzyl)benzo[d]oxazole-2(3H)-thione;3-(4-chlorobenzyl)benzo[d]oxazole-2(3H)-thione;3-(3-hydroxy-4-methoxybenzyl)benzo[d]oxazole-2(3H)-thione;3-(2,6-dichlorobenzyl)benzo[d]oxazole-2(3H)-thione;3-(4-nitrobenzyl)benzo[d]oxazole-2(3H)-thione;3-(2,4,6-trimethoxybenzyl)benzo[d]oxazole-2(3H)-thione;3-(naphthalen-2-ylmethyl)benzo[d]oxazole-2(3H)-thione;3-(pyridin-2-ylmethyl)benzo[d]oxazole-2(3H)-thione;3-(3-methoxybenzyl)benzo[d]oxazole-2(3H)-thione;3-(4-fluorobenzyl)benzo[d]oxazole-2(3H)-thione;3-(4-(trifluoromethyl)benzyl)benzo[d]oxazole-2(3H)-thione;3-(2-fluorobenzyl)benzo[d]oxazole-2(3H)-thione;3-(3-fluorobenzyl)benzo[d]oxazole-2(3H)-thione;3-(3-nitrobenzyl)benzo[d]oxazole-2(3H)-thione;3-(2-nitrobenzyl)benzo[d]oxazole-2(3H)-thione;3-(pyridin-3-ylmethyl)benzo[d]oxazole-2(3H)-thione;3-(4-methoxybenzyl)benzo[d]oxazole-2(3H)-thione;3-(2-hydroxybenzyl)benzo[d]oxazole-2(3H)-thione;3-(3-chlorobenzyl)benzo[d]oxazole-2(3H)-thione;3-(2-chlorobenzyl)benzo[d]oxazole-2(3H)-thione;3-(3-hydroxybenzyl)benzo[d]oxazole-2(3H)-thione;3-((1H-indol-2-yl)methyl)benzo[d]oxazole-2(3H)-thione;3-((1H-pyrrol-2-yl)methyl)benzo[d]oxazole-2(3H)-thione;3-((1H-indol-4-yl)methyl)benzo[d]oxazole-2(3H)-thione;3-((1H-indazol-4-yl)methyl)benzo[d]oxazole-2(3H)-thione;3-((1H-indazol-5-yl)methyl)benzo[d]oxazole-2(3H)-thione;3-((1H-indol-6-yl)methyl)benzo[d]oxazole-2(3H)-thione;3-(quinolin-4-ylmethyl)benzo[d]oxazole-2(3H)-thione;1-(2-hydroxybenzyl)-1H-benzo[d]imidazole-2(3H)-thione;1-(4-hydroxybenzyl)-1H-benzo[d]imidazole-2(3H)- ...

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31-01-2019 дата публикации

LUMINOGENIC AND FLUOROGENIC COMPOUNDS AND METHODS TO DETECT MOLECULES OR CONDITIONS

Номер: US20190031629A1
Принадлежит:

A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided. 19-. (canceled)11. The method of claim 10 , wherein R is H or methyl.12. The method of claim 11 , wherein Ris (C) alkyl substituted by R.13. The method of claim 12 , wherein Ris amino.14. The method of claim 10 , wherein Ris selected from the group consisting of —SO(C)aryl and —S(O)(C)aryl claim 10 , wherein the aryl in —SO(C)aryl and —S(O)(C)aryl is optionally substituted.15. The method of claim 14 , wherein the aryl in —SO(C)aryl and —S(O)(C)aryl is substituted with one or more substituents.16. The method of claim 15 , wherein the one or more substituents are selected from the group consisting of nitro claim 15 , phenyl and (C)alkyl.19. The method of claim 10 , wherein Ris (C)aryl claim 10 , heteroaryl claim 10 , piperidinyl (C)alkylthio claim 10 , (C)alkyl-S(O)— claim 10 , (C)alkyl-SO— claim 10 , (C)alkyl-SO— claim 10 , (C)alkylphosphate claim 10 , (C)alkylphosphonate claim 10 , (C)arylthio claim 10 , (C)aryl-S(O)— claim 10 , (C)aryl-SO— claim 10 , (C)aryl-SO— claim 10 , (C)arylphosphate claim 10 , or (C)arylphosphonate.20. The method of claim 12 , wherein Ris (C)cycloalkyl claim 12 , (C)alkoxyl claim 12 , (C)alkylcarbonyl claim 12 , (C)alkylcarboxyl claim 12 , hydroxyl claim 12 , —COOR claim 12 , —SOR claim 12 , (C)alkylthio claim 12 , (C)arylthio claim 12 , (C)alkyl-S(O)— claim 12 , (C)alkyl-S(O)— claim 12 , nitro claim 12 , NH(C)alkynyl claim 12 , N((C)alkynyl) claim 12 , mercapto claim 12 , saccharide claim 12 , or trifluoromethyl.21. The method of claim 10 , wherein the molecule is an enzyme claim 10 , a cofactor for an enzymatic reaction claim 10 , an enzyme substrate claim 10 , an enzyme inhibitor claim 10 , an enzyme activator claim 10 , or an OH radical.23. The method of claim 22 , or a salt thereof ...

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03-03-2022 дата публикации

LEUKOTRIENE SYNTHESIS INHIBITORS

Номер: US20220064132A1
Принадлежит: Naegis Pharmaceuticals Inc.

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

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14-02-2019 дата публикации

ENDOPARASITE CONTROL AGENT

Номер: US20190046511A1
Принадлежит:

The present invention is intended to provide a novel parasiticide, antiprotozoal or other endoparasite control agents which are effective for controlling animal endoparasites that have been impossible to control by conventional ones. Provided is an endoparasite control agent comprising, as an active ingredient, a carboxamide derivative represented by the general formula (I): 111-. (canceled)13. The method according to claim 12 , wherein the endoparasite control agent is orally or parenterally administered to a non-human mammal.14. The method according to claim 13 , wherein the non-human mammal is a domestic animal.15. The method according to claim 12 , wherein the mammal is a human.16. The method according to claim 12 , wherein the mammal is a non-human mammal. The present invention relates an endoparasite control agent comprising a carboxamide derivative or a salt thereof as an active ingredient, and a method for controlling endoparasites, comprising orally or parenterally administering the endoparasite control agent.Certain kinds of carboxamide derivatives have been known to have microbicidal activity (see Patent Literature 1 to 12). However, the literature does not describe that these compounds are effective for the disinfection or control of endoparasites in animals such as mammals and birds. It is also known that certain kinds of carboxamide derivatives are effective against nematodes that may damage agricultural products (see Patent Literature 4 or 5), but there is no specific disclosure as to whether these compounds are effective against endoparasites in animals. Furthermore, there is a report that compounds that inhibit succinate-ubiquinone reductase (mitochondrial complex II), which is one of the respiratory enzymes of endoparasites, can serve as an endoparasite control agent (see Non Patent Literature 1).In addition, Patent Literature 13 discloses certain kinds of carboxamide derivatives which are effective against endoparasites. However, there is no ...

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05-03-2015 дата публикации

ORGANIC COMPOUNDS

Номер: US20150065490A1
Принадлежит: NOVARTIS AG

Compounds of formula I 2. A compound according to claim 1 , in which{'sup': 1', '2', 'a, 'X is —R—Ar—Ror —R—Y;'}{'sub': 1', '10', '1', '10', '1', '10, 'Ar denotes a phenylene group optionally substituted by halo, C-C-alkyl, C-C-alkoxy or by C-C-alkoxy substituted by phenyl;'}{'sup': 1', '2, 'Rand Rare attached to adjacent carbon atoms in Ar, and'}{'sup': 1', '2, 'sub': 1', '10, 'either Ris C-C-alkylene and Ris hydrogen,'}{'sup': 1', '2, 'or Rand Rtogether with the carbon atoms in Ar to which they are attached denote a 5-, 6- or 7-membered cycloaliphatic ring;'}{'sup': 'a', 'sub': 1', '10', '6', '10', '7', '14, 'Ris a bond or C-C-alkylene optionally substituted by hydroxy, C-C-aryl or C-C-aralkyl; and'}{'sub': 1', '10', '1', '10', '2', '10', '3', '10', '1', '10', '3', '10', '7', '14', '7', '14', '6', '10', '1', '10', '1', '10', '6', '10', '1', '10', '3', '10', '6', '10', '1', '10', '1', '10', '1', '10', '6', '10', '7', '14', '1', '10', '1', '10', '1', '10', 'e', '1', '10', '6', '10', '1', '10', '6', '10', '7', '14', '1', '10', '3', '10', '6', '10, 'sup': b', 'c', 'b', 'c', 'b', 'd', 'e', 'd', 'e', 'e', 'f', 'f', 'g', 'g, 'Y is C-C-alkyl, C-C-alkoxy or C-C-alkynyl; C-C-cycloalkyl optionally fused to one or more benzene rings and optionally substituted by C-C-alkyl, C-C-cycloalkyl, C-C-aralkyl, C-C-aralkyloxy optionally substituted by halo, or by C-C-aryl optionally substituted by C-C-alkyl or C-C-alkoxy C-C-aryl optionally substituted by halo, hydroxy, C-C-alkyl, phenoxy, C-C-alkylthio, C-C-aryl, a 4- to 10-membered heterocyclic ring having at least one ring nitrogen atom, or by NRRwhere Rand Rare each independently C-C-alkyl optionally substituted by hydroxy or phenyl or Rmay additionally be hydrogen; phenoxy optionally substituted by C-C-alkoxy; a 4- to 10-membered heterocyclic ring having at least one ring nitrogen or oxygen atom, said heterocyclic ring being optionally substituted by C-C-alkyl, C-C-aryl, C-C-aralkyl, C-C-alkoxycarbonyl or by a 4- to 10-membered ...

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27-02-2020 дата публикации

Method For The Manufacture of Efavirenz

Номер: US20200062722A1
Принадлежит: NELSON MANDELA METROPOLITAN UNIVERSITY

This invention relates to a method for the manufacture of optically pure (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. Specifically, this invention relates to a flow synthesis method for the manufacture of (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. 2. The method according to claim 1 , wherein in step (b) or step (c) the butyllithium is n-butyllithium.3. The method according to claim 1 , wherein in step (b) the reaction is performed in the presence of tetramethylethylenediamine.4. The method according to claim 1 , wherein the reactions of steps (a)-(d) are each independently performed in a solvent or solvent mixture selected from the group consisting of tetrahyroduran claim 1 , dichloromethane claim 1 , acetonitrile claim 1 , acetone claim 1 , water claim 1 , and mixtures thereof.5. The method according to claim 1 , further comprising recrystallization from a solution of ethyl acetate in heptane.7. The method according to claim 6 , wherein in step (b) the butyllithium is n-butyllithium.8. The method according to claim 6 , wherein the reactions of steps (a)-(c) are each independently performed in a solvent or solvent mixture selected from the group consisting of tetrahyroduran claim 6 , dichloromethane claim 6 , acetonitrile claim 6 , acetone claim 6 , water claim 6 , and mixtures thereof.9. The method according to claim 6 , further comprising recrystallization from a solution of ethyl acetate in heptane.10. The method of claim 6 , wherein the reaction of step (a) has a residence time of between about 5 minutes and about 12 minutes.11. The method of claim 6 , wherein in step (a) the molar ratio of 4-chloroaniline to di-tert-butyl dicarbamate is in the range of about 1:1 to 1:1.2.12. The method of claim 6 , wherein the reaction of step (a) is performed at a temperature of about 30° C. to about 60° C.13. The method of claim 1 , wherein the reaction of step (b) is performed at a ...

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11-03-2021 дата публикации

Luminescent compounds

Номер: US20210070720A1
Принадлежит: UNIVERSITY OF BIRMINGHAM

Polycyclic aromatic hydrocarbons represented by the following general formula (I) wherein X is one of nitrogen, phosphorus, arsenic, antimony, bismuth, sulphur, selenium, tellurium; R independently represents an aromatic group and/or an aliphatic group; Q is one of a cyclic aliphatic hydrocarbon, a cyclic aromatic hydrocarbon, a polycyclic hydrocarbon, a polycyclic aromatic hydrocarbon, and/or a fused polycyclic aromatic hydrocarbon; wherein the substituents independently comprise one or more of a hydrogen atom, a deuterium atom, a fluorine atom, a chlorine atom, a bromine atom, a carbon atom, an oxygen atom (e.g. an alkylated oxygen atom), a nitrogen atom (e.g. an alkylated nitrogen atom), a cyano group, a nitro group, an alkyl group and/or anaryl group; p is an integer of 1 to 2; q is an integer of 1 to 4; Y 1 and Y 2 independently represent one or more of a hydrogen atom, a deuterium atom, a fluorine atom, a chlorine atom, a bromine atom, a carbon atom, an oxygen atom (e.g. an alkylated oxygen atom), a nitrogen atom (e.g. an alkylated nitrogen 20 atom), a cyano group, a nitro group, an alkyl group and/oranaryl group; and x is an integer of 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 or more.

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05-06-2014 дата публикации

LUMINOGENIC AND FLUOROGENIC COMPOUNDS AND METHODS TO DETECT MOLECULES OR CONDITIONS

Номер: US20140154716A1
Принадлежит:

A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided. 2. The compound or salt thereof of claim 1 , wherein the —COH substituent on the thiazole ring of formula (X) is in the (S) stereochemical configuration.3. The compound or salt thereof of claim 2 , wherein Ris H and Ris unsubstituted phenylCalkyl.4. The compound or salt thereof of claim 2 , wherein Ris H and Ris phenylCalkyl claim 2 , and phenyl is substituted with amino claim 2 , optionally substituted Calkylamino claim 2 , or optionally substituted di-Calkylamino.5. The compound or salt thereof of claim 2 , wherein Ris H and Ris phenylCalkyl claim 2 , wherein phenyl is substituted with amino claim 2 , and the amino group is substituted with optionally substituted Calkylcarbonyl or Calkoxycarbonyl.6. A luciferase substrate comprising a compound of .7. The compound of claim 1 , wherein Ris H and Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , or hexyl.8. The compound of claim 1 , wherein Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , or hexyl claim 1 , and Ris methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl claim 1 , pentyl claim 1 , or hexyl.9. The compound of claim 1 , wherein Ris H and Ris benzyl claim 1 , phenethyl claim 1 , phenylpropyl claim 1 , phenylbutyl claim 1 , phenylpentyl claim 1 , or phenylhexyl.10. The compound of claim 1 , wherein Ris H and Ris benzyl claim 1 , phenethyl claim 1 , phenylpropyl claim 1 , phenylbutyl claim 1 , phenylpentyl claim 1 , or phenylhexyl wherein the benzene ring of Ris substituted with an amino group.13. The compound or a salt thereof according to claim 12 , wherein either one of Rand Ris hydrogen claim 12 , and the other is a group represented by the formula (A) claim 12 , and in the ...

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31-03-2022 дата публикации

SMALL MOLECULE PYRIN-DOMAIN TARGETED NLRP3 INFLAMMASOME INHIBITORS

Номер: US20220098188A1
Автор: Ji Haitao, LIST Alan
Принадлежит:

Disclosed herein are small molecule pyrin-domain targeted NLRP3 inflammasome inhibitors. 2. (canceled)4. (canceled)6. The compound of claim 1 , wherein Ais NH.7. The compound of claim 1 , wherein Ais selected from C or N.8. (canceled)9. (canceled)10. (canceled)11. The compound of claim 1 , wherein R′ and R″ are independently selected from hydrogen; unsubstituted C-Calkyl claim 1 , unsubstituted C-Chaloalkyl claim 1 , unsubstituted alkoxy claim 1 , or both R′ and R″ combine to form a substituted or unsubstituted C-Ccycloalkyl claim 1 , a substituted or unsubstituted C-Ccycloalkenyl claim 1 , a substituted or unsubstituted C-Cheterocycloalkyl claim 1 , or a substituted or unsubstituted C-Cheterocycloalkenyl together with the atom to which they are attached.12. (canceled)13. (canceled)14. (canceled)15. The compound of claim 1 , wherein R′″ is hydrogen and Ris independently selected from hydrogen; substituted or unsubstituted C-Calkyl claim 1 , substituted or unsubstituted aminoalkyl claim 1 , substituted or unsubstituted C-Chaloalkyl claim 1 , substituted or unsubstituted alkoxy claim 1 , substituted or unsubstituted cycloalkyl claim 1 , substituted or unsubstituted cycloheteroalkyl claim 1 , substituted or unsubstituted aryl claim 1 , substituted or unsubstituted heteroaryl claim 1 , or{'sup': 'iv', 'sub': ['3', '8', '3', '8', '2', '7', '2', '7'], '#text': 'both R′″ and Rcombine to form a substituted or unsubstituted C-Ccycloalkyl, a substituted or unsubstituted C-Ccycloalkenyl, a substituted or unsubstituted C-Cheterocycloalkyl, or a substituted or unsubstituted C-Cheterocycloalkenyl together with the atom to which they are attached.'}16. (canceled)17. (canceled)18. (canceled)19. The compound of claim 1 , wherein Ris selected from hydrogen; hydroxyl claim 1 , halide claim 1 , unsubstituted nitrile claim 1 , unsubstituted nitro claim 1 , unsubstituted amine claim 1 , unsubstituted alkyl halide claim 1 , unsubstituted carboxyl claim 1 , unsubstituted amide claim 1 , ...

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12-06-2014 дата публикации

DIPHOSPHATE MIMETICS AND USES THEREOF

Номер: US20140163079A1

The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions. 35-. (canceled)6. The compound of claim 1 , wherein R claim 1 , R claim 1 , or the ring formed therefrom claim 1 , is substituted with at least substituent selected from the group consisting of —C(═O)R claim 1 , —C(═O)OR claim 1 , —C(═O)SR claim 1 , —C(═O)N(R) claim 1 , —OC(═O)R claim 1 , —OC(═O)OR claim 1 , —OC(═O)SR claim 1 , —OC(═O)N(R) claim 1 , —NRC(═O)R claim 1 , —NRC(═O)OR claim 1 , —NRC(═O)SR claim 1 , —NRC(═O)N(R) claim 1 , —SC(═O)R claim 1 , —SC(═O)OR claim 1 , —SC(═O)SR claim 1 , —SC(═O)N(R) claim 1 , —C(═NR)R claim 1 , —C(═NR)OR claim 1 , —C(═NR)SR claim 1 , —C(═NR)N(R) claim 1 , —OC(═NR)R claim 1 , —OC(═NR)OR claim 1 , —OC(═NR)SR claim 1 , —OC(═NR)N(R) claim 1 , —NRC(═NR)R claim 1 , —NRC(═NR)OR claim 1 , —NRC(═NR)SR claim 1 , —NRC(═NR)N(R) claim 1 , —SC(═NR)R claim 1 , —SC(═NR)OR claim 1 , —SC(═NR)SR claim 1 , —SC(═NR)N(R) claim 1 , —C(═S)R claim 1 , —C(═S)OR claim 1 , —C(═S)SR claim 1 , —C(═S)N(R) claim 1 , —OC(═S)R claim 1 , —OC(═S)OR claim 1 , —OC(═S)SR claim 1 , —OC(═S)N(R) claim 1 , —NRC(═S)R claim 1 , —NRC(═S)OR claim 1 , —NRC(═S)SR claim 1 , —NRC(═S)N(R) claim 1 , —SC(═S)R claim 1 , —SC(═S)OR claim 1 , —SC(═S)SR claim 1 , —SC(═S)N(R) claim 1 , —S(═O)R claim 1 , —SOR claim 1 , —NRSOR claim 1 , —SON(R) claim 1 , ...

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02-04-2015 дата публикации

BENZOTHIAZOLONE COMPOUND

Номер: US20150094346A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form 2. A compound according to which is (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one in free form.3. A compound according to which is (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one in acetate salt form.4. A compound according to which is (R)-7-(2-(1-(4-butoxyphenyl)-2-methylpropan-2-ylamino)-1-hydroxyethyl)-5-hydroxybenzo[d]thiazol-2(3H)-one in glycolate salt form.5. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to and one or more pharmaceutically acceptable carriers.6. A pharmaceutical composition according to wherein one of the pharmaceutically acceptable carriers is benzyl alcohol.7. A combination comprising a therapeutically effective amount of a compound according to and one or more therapeutically active co-agents.11. A process according to wherein the LG is chloro. The present invention relates to a benzothiazolone compound, to its preparation, to its medical use as a beta-2 adrenoceptor agonist and to medicaments, pharmaceutical compositions and combinations comprising it.Benzothiazolone compounds which are beta-2-adrenoceptor agonists are described in WO2004/16601 and WO2006/056471. WO2005/110990 also describes benzo-condensed heterocycles as beta-2 agonists.While beta-2 agonists have long been known for their bronchodilating properties, they are also known for their capability to produce skeletal muscle hypertrophy.Numerous studies have focused on therapeutic applications of the anabolic properties of beta-2 agonists for ameliorating muscle wasting and improving muscle function. However, this class of compounds has also been associated with undesirable side-effects, including increased risk of adverse cardiovascular-related events. Thus, the use of beta-2 agonists in muscle ...

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28-03-2019 дата публикации

BENZIMIDAZOLONE AND BENZOTHIAZOLONE COMPOUNDS AND THEIR USE AS AMPA RECEPTOR MODULATORS

Номер: US20190092735A1
Принадлежит: Janssen Pharmaceutica NV

Provided herein are compounds of Formula (I), and pharmaceutically acceptable salts, N-oxides, or solvates thereof, 2. The compound of claim 1 , wherein X is NH.3. The compound of claim 1 , wherein X is S.4. The compound of claim 1 , wherein Rand Rare H.5. The compound of claim 1 , wherein Ris H claim 1 , —Cl claim 1 , —CH claim 1 , —CHCH claim 1 , —CF claim 1 , —OCF claim 1 , or —CN.6. The compound of claim 1 , wherein Ris H claim 1 , H or —F.7. The compound of claim 1 , wherein Ris —OCF claim 1 , —OCHF claim 1 , —OCHCF claim 1 , —OCHCHF claim 1 , —OCH claim 1 , —OCH(CH) claim 1 , —OC(CH) claim 1 , or —OCHC(CH).9. The compound of claim 1 , wherein Ris —Br claim 1 , —Cl claim 1 , —F claim 1 , —OCF claim 1 , —OCHF claim 1 , —OCHCF claim 1 , or —OCHCHF.11. The compound of claim 1 , wherein Ris —CN or oxadiazolyl optionally substituted with Calkyl or Chaloalkyl.12. The compound of claim 1 , wherein Ris H claim 1 , —Cl claim 1 , —F claim 1 , or —OCF.13. The compound of claim 1 , wherein Ris H.14. The compound of claim 1 , wherein Ris H claim 1 , —Cl claim 1 , —CH claim 1 , —CF claim 1 , —CN claim 1 , —COCH claim 1 , —(C═O)NH-phenyl claim 1 , —(C═O)pyrrolidine claim 1 , or —(C═O)piperidine.15. The compound of claim 1 , wherein Ris H or halo.16. The compound of claim 1 , wherein Ris H claim 1 , halo claim 1 , Calkyl claim 1 , —CHCN claim 1 , Calkoxy claim 1 , Chaloalkyl claim 1 , or Chaloalkoxy claim 1 , and Ris H or halo.17. The compound of claim 1 , wherein Ris H claim 1 , halo claim 1 , Calkyl claim 1 , or —CHCN.20. The compound of claim 18 , wherein Ris halo claim 18 , Calkyl claim 18 , Chaloalkyl claim 18 , —CN claim 18 , or —CH—CN.22. The compound of claim 21 , wherein Ris Calkoxy or Chaloalkoxy claim 21 , and Ris selected from: H claim 21 , —Cl claim 21 , and —COCH.23. The compound of claim 22 , wherein Ris —OCF claim 22 , —OCH claim 22 , or —OCH(CH).25. A compound of wherein Ris 01-5 alkoxy claim 24 , or Chaloalkoxy; and{'sup': '5', 'sub': '1-5', 'Ris H, halo, or ...

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02-06-2016 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20160152582A1
Принадлежит:

Compounds of formula I′: 2. The compound of wherein A is phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.3. The compound of wherein A is phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle wherein any phenyl claim 1 , monocyclic N-heteroaryl or monocyclic heterocycle of A is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.4. The compound of wherein A is monocyclic N-heteroaryl claim 1 , wherein monocyclic N-heteroaryl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.5. The compound of wherein A is pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl claim 1 , wherein pyridinyl claim 1 , pyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl-2-one claim 1 , tetrahydropyrimidinyl-2-one claim 1 , imidazolidinyl-2-one claim 1 , pyrrolidinyl-2-one or pyrrolidinyl is optionally substituted with one or more Zgroups claim 1 , and B is aryl claim 1 , heteroaryl or hetereocycle wherein any aryl claim 1 , heteroaryl or hetereocycle of B is optionally substituted with one or more Zgroups.6. The compound of wherein B is phenyl claim 1 , pyridinyl claim 1 , pyrazolyl claim 1 , pyrimidinyl claim 1 , indazolyl claim 1 , pyrazolopyridine or benzimidazolyl claim 1 , wherein any ...

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29-06-2017 дата публикации

SUBSTITUTED BENZOXAZOLONE DERIVATIVES AS ACID CERAMIDASE INHIBITORS, AND THEIR USE AS MEDICAMENTS

Номер: US20170182009A1
Принадлежит:

The present invention relates to substituted benzoxazolone derivatives as acid ceramidase inhibitors, pharmaceutical compositions containing these inhibitors and methods of inhibiting acid ceramidase for the treatment of disorders in which modulation of the levels of ceramide is clinically relevant. The invention also provides substituted benzoxazolone derivatives for use in the treatment of cancer, inflammation, pain, inflammatory pain or pulmonary diseases. 4. A compound according to having Formula (Ia) wherein:X is a bond, CO, CH(OH); X can be attached to any position of the ring to which it is connected;R is hydrogen;{'sub': 1', '2, 'Rand Rare independently hydrogen or methyl;'}n is an integer from 2 to 4;m is an integer from 2 to 4;{'sub': '3-7', 'G is phenyl, thiophenyl, pyridyl, naphthyl or Ccycloalkyl;'}{'sub': 3', '3, 'Ris hydrogen, chlorine; Rcan be attached to any position of the ring to which it is connected;'}{'sub': '4', 'Ris hydrogen;'}{'sub': 5', '2', '3, 'Ris independently selected from the group consisting of halogen, Me, Et, MeO, EtO, OH, CN, NO, CF;'}{'sub': 6', '7', '2', '3, 'Rand Rare independently selected from the group consisting of hydrogen, halogen, Me, Et, MeO, EtO, OH, CN, NO, CF;'}{'sub': 4', '5', '6', '7, 'R, R, Rand Rcan be attached to any position of the ring to which they are connected.'}6. A compound of Formula (Ib) according to claim 5 , whereinX is a bond, CO, CH(OH); X can be attached to any position of the ring to which it is connected;R is hydrogen;{'sub': 1', '2, 'Rand Rare independently hydrogen or Me;'}n is an integer from 1 to 4;m is 0 or an integer from 1 to 4;{'sub': '3-7', 'G is phenyl, thiophenyl, pyridyl, naphthyl or Ccycloalkyl;'}{'sub': 3', '3, 'Ris hydrogen, chlorine; Rcan be attached to any position of the ring to which it is connected;'}{'sub': '4', 'Ris hydrogen;'}{'sub': 5', '2', '3, 'Ris independently selected from the group consisting of halogen, Me, Et, MeO, EtO, OH, CN, NO, CF;'}{'sub': 6', '7', '2', '3, ' ...

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11-06-2020 дата публикации

PHOTOSENSITIVE RESIN COMPOSITION, RESIST FILM, PATTERN FORMING METHOD, AND METHOD FOR MANUFACTURING ELECTRONIC DEVICE

Номер: US20200183279A1
Принадлежит: FUJI FILM Corporation

A photosensitive resin composition includes a resin having a constitutional unit having an acid-decomposable group, a photoacid generator, a solvent, and a compound represented by Formula D. In Formula D, Xrepresents an O atom or an S atom, Rrepresents a hydrogen atom, a hydrocarbon group, an acyl group, an acyloxy group, or an alkoxycarbonyl group, Rrepresents a substituent, nD represents an integer from 0 to 4, and two or more of R's may be bonded to each other to form a ring. 2. The photosensitive resin composition according to claim 1 ,wherein a pKa of a conjugate acid of the compound represented by Formula D is 0.0 to 3.0.11. The photosensitive resin composition according to claim 1 ,wherein the solvent includes γ-hutyrolactone.12. The photosensitive resin composition according to claim 1 , further comprising a low-molecular-weight ester compound having alkali decomposability and having a molecular weight of less than 1 claim 1 ,500.13. A resist film which is a solidified product of the photosensitive resin composition according to .14. A pattern forming method comprising:{'claim-ref': {'@idref': 'CLM-00013', 'claim 13'}, 'exposing the resist film according to ; and'}developing the exposed resist film.15. A method for manufacturing an electronic device claim 4 , comprising the pattern forming method according to . This application is a Continuation of PCT International Application No. PCT/JP2018/030050 filed on Aug. 10, 2018, which claims priority under 35 U.S.C § 119(a) to Japanese Patent Application No. 2017-190835 filed on Sep. 29, 2017. Each of the above application(s) is hereby expressly incorporated by reference, in its entirety, into the present application.The present disclosure relates to a photosensitive resin composition, a resist film, a pattern forming method, and a method for manufacturing an electronic device.In processes for manufacturing semiconductor devices such as an integrated circuit (IC) in the related art microfabrication by lithography ...

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30-10-2014 дата публикации

THERAPEUTIC COMPOUNDS AND COMPOSITIONS

Номер: US20140323467A1
Принадлежит: AGIOS PHARMACEUTICALS, INC

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer. 2. The compound of claim 1 , wherein W claim 1 , X claim 1 , Y and Z are CH.3. The compound of claim 2 , wherein D is NRand Dis a bond.4. The compound of claim 3 , wherein Ris H claim 3 , methyl or ethyl.5. The compound of claim 1 , wherein L is a bond claim 1 , —(CRR)— claim 1 , —NRC(O)— claim 1 , —(CRR)—C(O)— claim 1 , —C(O)— claim 1 , or —O(CO)—.6. The compound of claim 5 , wherein L is a bond.7. The compound of claim 6 , wherein Ris alkyl claim 6 , aryl or heteroaryl substituted with 0-5 occurrences of R.8. The compound of claim 7 , wherein L is —(CRR)—.9. The compound of claim 8 , wherein Ris cycloalkyl claim 8 , aryl claim 8 , heteroaryl or heterocyclyl substituted with 0-5 occurrences of R.10. The compound of claim 5 , wherein L is —NRC(O)— and Ris hydrogen.11. The compound of claim 10 , wherein Ris aryl substituted with 0-5 occurrences of R.12. The compound of claim 5 , wherein L is —(CRR)—C(O)—.13. The compound of claim 12 , wherein Ris cycloalkyl claim 12 , aryl or heteroaryl substituted with 0-5 occurrencs of R.14. The compound of claim 5 , wherein L is —C(O)—.15. The compound of claim 14 , wherein Ris aryl claim 14 , alkyl claim 14 , or heteroaryl substituted with 0-5 occurrencs of R.16. The compound of claim 5 , wherein L is —OC(O)—.17. The compound of claim 16 , wherein Ris alkyl claim 16 , aryl or heterocyclyl substituted with 0-5 occurrences of R.18. The compound of claim 5 , wherein L is —(CRR)—OC(O)—.19. The compound of claim 18 , wherein Ris heterocyclyl or cycloalkyl substituted with 0-5 occurrences of R.20. The compound of claim 5 , wherein n is 0.21. The compound of claim 5 , wherein n is 1 and Ris CH claim 5 , CHCH claim 5 , OCH claim 5 , OCHCH claim 5 , OH claim 5 , F claim 5 , Cl claim 5 , or CF.22. A pharmaceutical composition ...

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06-11-2014 дата публикации

NOVEL DOPAMINE D3 RECEPTOR LIGANDS AND PREPARATION AND MEDICAL USES OF THE SAME

Номер: US20140329831A1
Принадлежит:

The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction. 3. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein L is —CHCHCHCH— , or cis- or trans —CHCH═CHCH—.4. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein R , R , and Reach are independently H , F , Cl , Br , I , C-Calkyl , or C-Calkyloxy; preferably , wherein R , R , and Reach are independently H , F , Cl , methyl , ethyl , methyloxy , or ethyloxy.5. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein X is O.6. The compound of formula I according to or , or tautomers , racemates , optical isomers , pharmaceutically acceptable salts or solvates thereof , wherein both Y and Z are C.76. The compound of formula I according to any one of - claims 1 , which is selected from:N-{4-[4-(5-chloro-2-methylphenyl)piperazinyl]butyl}-benzoxazolin-2-one-5-carboxamide;N-{4-[4-(5-chloro-2-methylphenyl)piperazinyl]butyl}-benzoxazolin-2-one-6-carboxamide;N-{4-[4-(2-methyloxyphenyl)piperazinyl]butyl}-benzoxazolin-2-one-5-carboxamide;N-{4-[4-(2-methyloxyphenyl)piperazinyl]butyl}-benzoxazolin-2-one-6-carboxamide;N-{4-[4-(5-chloro-2-methylphenyl)piperazinyl]-trans-2-buten-1 ...

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08-09-2016 дата публикации

NOVEL ONIUM SALT COMPOUND, RESIST COMPOSITION, AND PATTERN FORMING PROCESS

Номер: US20160259242A1
Принадлежит: SHIN-ETSU CHEMICAL CO., LTD.

Sulfonium and iodonium salts of nitrogen-containing carboxylic acids are novel. The onium salt functions as an acid diffusion controlling agent in a resist composition, enabling to form a pattern of good profile with high resolution, improved MEF, LWR and DOF. 6. The resist composition of claim 3 , further comprising a nonionic nitrogen-containing compound.7. The resist composition of claim 3 , further comprising a surfactant which is insoluble or substantially insoluble in water and soluble in alkaline developer and/or a surfactant which is insoluble or substantially insoluble in water and alkaline developer.8. A pattern forming process comprising the steps of applying the resist composition of onto a substrate claim 3 , prebaking to form a resist film claim 3 , exposing the resist film to KrF excimer laser claim 3 , ArF excimer laser claim 3 , EB or EUV through a photomask claim 3 , baking claim 3 , and developing the exposed resist film in a developer.9. The pattern forming process of wherein the exposing step is by immersion lithography wherein a liquid having a retractive index of at least 1.0 is interposed between the resist film and a protection lens.10. The pattern forming process of claim 9 , further comprising the step of forming a protective film on the resist film claim 9 , and in the immersion lithography claim 9 , the liquid is interposed between the protective film and the projection lens. This non-provisional application claims priority under 35 U.S.C. §119(a) on Patent Application No. 2014-168155 filed in Japan on Aug. 21, 2014, the entire contents of which are hereby incorporated by reference.This invention relates to an onium salt compound of specific structure, a resist composition, typically chemically amplified resist composition comprising the salt, and a pattern forming process using the resist composition.While a number of recent efforts are being made to achieve a finer pattern rule in the drive for higher integration densities and ...

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06-09-2018 дата публикации

ANTIBACTERIAL HETEROCYCLIC DERIVATIVES

Номер: US20180251434A1
Принадлежит:

The invention relates to antibacterial compounds of formula I 2. A compound according to claim 1 , wherein V represents O;or a pharmaceutically acceptable salt thereof.3. A compound according to wherein Rand Rboth represent hydrogen;or a pharmaceutically acceptable salt thereof.4. A compound according to claim 1 , wherein Rrepresents hydrogen claim 1 , or Rrepresents —POH claim 1 , —SOH claim 1 , phosphonooxymethyl claim 1 , or dimethylaminomethylcarbonyl;or a pharmaceutically acceptable salt thereof.5. A compound according to claim 1 , wherein Rrepresents hydrogen;or a pharmaceutically acceptable salt thereof.8. A compound according to claim 1 , wherein M is the group M;or a pharmaceutically acceptable salt thereof.9. A compound of formula I according to claim 1 , which is selected from the following:(R)-4-(6-(2-fluoro-4-methoxyphenyl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-hydroxy-2-methyl-2-(methylsulfonyl)butanamide;(R)—N-hydroxy-4-(6-((3-hydroxyoxetan-3-yl)buta-1,3-diyn-1-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-2-methyl-2-(methylsulfonyl)butanamide;(R)—N-hydroxy-4-(6-((4-(hydroxymethyl)phenypethynyl)-2-oxobenzo[d]oxazol-3(2H)-yl)-2-methyl-2-(methylsulfonyl)butanamide;(R)—N-hydroxy-4-(6-((1-(hydroxymethyl)cyclopropyl)buta-1,3-diyn-1-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-2-methyl-2-(methylsulfonyl)butanamide;(R)—N-hydroxy-2-methyl-2-(methylsulfonyl)-4-(6-((4-(morpholinomethyl)phenyl)ethynyl)-2-oxobenzo[d]oxazol-3(2H)-yl)butanamide;(R)—N-hydroxy-2-methyl-4-(6-((1-(methylamino)cyclopropyl)buta-1,3-diyn-1-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-2-(methylsulfonyl)butanamide;(R)—N-hydroxy-4-(6-(((1S,2S)-2-(hydroxymethyl)cyclopropyl)buta-1,3-diyn-1-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-2-methyl-2-(methylsulfonyl)butanamide;(R)-4-(6-(((1R,2R)-2-fluoro-2-(hydroxymethyl)cyclopropyl)buta-1,3-diyn-1-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-hydroxy-2-methyl-2-(methylsulfonyl)butanamide;(R)-5-(3-(4-(hydroxyamino)-3-methyl-3-(methylsulfonyl)-4-oxobutyl)-2-oxo-2,3-dihydrobenzo[d]oxazol-6-yl)penta-2,4-diyn-1- ...

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22-09-2016 дата публикации

DIAMINE DERIVATIVES AS INHIBITORS OF LEUKOTRIENE A4 HYDROLASE

Номер: US20160272649A1
Принадлежит:

This invention is directed to compounds of formula (I): 3. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, cyano, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted heteroarylalkyl, optionally substituted heterocyclyl, or optionally substituted heterocyclylalkyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each independently hydrogen or halo.'}4. A compound according to wherein{'sup': 1a', '13', '10', '13', '10, 'Ris hydrogen, —R—C(O)OR, —R—C(O)R, alkyl, halo, haloalkyl, optionally substituted phenyl, furanyl, thienyl, thiazolyl, or optionally substituted oxazolyl; and'}{'sup': 1b', '1c', '1d', '1e, 'R, R, Rand Rare each hydrogen.'}6. A compound according to wherein R is an optionally substituted heteroaryl.7. A compound according to wherein R is furanyl claim 6 , oxazolyl claim 6 , pyrazol claim 6 , pyridinyl claim 6 , triazolyl claim 6 , thiazolyl claim 6 , or benzothiazolyl claim 6 , each of which is optionally substituted.8. A compound according to wherein:{'sup': 2', '7', '5a', '5b', '5c, 'Rand R, together with the nitrogens to which they are attached and one of R, Rand R, form an optionally substituted 6- to 10-membered bridged N-heterocyclyl.'}10. A compound according to wherein:{'sup': 3', '12', '12', '12, 'Ris a direct bond, —O—, —R—O—, —O—R—, —O—R—O—, or an optionally substituted straight or branched alkylene chain;'}{'sup': 4', '12a, 'Ris a direct bond, —O—R—, or an optionally substituted straight or branched alkylene chain;'}{'sup': 8', '13', '10', '13', '10', '13', '10', '13', '10', '11, 'Ris aralkyl optionally substituted with one or more substituents selected from the group consisting of —R—OR, —R—C(═O)R, —R—C(═O)ORand —R—C(═O)N(R)R;'}{'sup': 9', '10, 'each Ris independently alkyl, halo or —O—R;'}{'sup': '12', 'Ris an ...

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11-12-2014 дата публикации

PROCESS

Номер: US20140364601A1
Принадлежит: AstraZeneca AB

Processes for the preparation of the compound of formula (II) and intermediate compounds for use in the processes. 8. A novel intermediate compound as set out in Table 1 hereinbefore. The present invention relates to processes for the preparation of chemical compounds that have MABA activity and intermediates for use in such preparations.The first-line treatment for a variety of pulmonary disorders including chronic obstructive pulmonary disease (COPD) and asthma is through the use of bronchodilators. Muscarinic-receptor antagonists (anti-cholinergics) are bronchodilators that exert their efficacy by reducing vagal cholinergic tone, the main reversible component of airway constriction in COPD. β-adrenoceptor agonists are also bronchodilators due to their ability to functionally antagonise the bronchoconstrictor responses to a range of mediators, including acetylcholine.In addition to improving lung function, these agents improve dyspnoea (breathlessness), quality of life, exercise tolerance and they reduce exacerbations. A number of clinical studies have demonstrated that combined administration of an anti-cholinergic and a β-receptor agonist is more efficacious than either of the individual components (van Noord, J. A., Aumann, J-L., Janssens, E., Smeets, J. J., Verhaert, J., Disse, B., Mueller, A. & Cornelissen, P. J. G., 2005. “Comparison of tiotropium once daily, formoterol twice daily and both combined once daily in patients with COPD”, 26, pp 214-222.). A single molecule possessing activities at muscarinic and β-receptors (MABA) may provide additional benefits to COPD patients in terms of efficacy and side-effect profile over either single agent. Moreover, a molecule possessing dual activity may also offer benefits in terms of ease-of-use and patient compliance over co-administration of the single therapies. A single agent may also be beneficial from the perspective of formulation compared to two separate compounds, also offering the potential, if combined ...

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29-09-2016 дата публикации

COMPOSITIONS FOR THE TREATMENT OF HYPERTENSION AND/OR FIBROSIS

Номер: US20160280671A1
Автор: Duggan Karen Annette
Принадлежит:

The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of hypertension and/or fibrosis. 2. The compound claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof claim 1 , according to wherein Q is halo selected from the group consisting of F claim 1 , Cl claim 1 , Br and I.3. The compound claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Q is substituted amino of the formula —NHW and wherein:{'sub': 2', 'a', 'a, 'W is selected from —CN, —SO(X)Y and —CO(X)Y,'}a is 0 or 1,X is selected from —NH— and —O—, and{'sub': 3', '2', '3', '2', '2', '2, 'Y is selected from —H, —CH, —CHCH, —CHOH and —CHCHOH.'}4. The compound claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof claim 1 , according to claim 1 , wherein Q is substituted amino selected from the group consisting of —NHSOCH claim 1 , —NHCOH claim 1 , —NHCONHCH claim 1 , —NHCONHCHCH—NHSONHCH claim 1 , —NHSONHCHCH claim 1 , —NHCOCH claim 1 , —NHCOOCH claim 1 , —NHCOOCHCHOH claim 1 , —NHCONHand —NHCN.5. The compound claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof claim 1 , according to wherein Q is alkyl selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , butyl and pentyl.8. A pharmaceutical composition comprising a compound claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof claim 1 , according to and a pharmaceutically-acceptable excipient.9. A method for the therapeutic treatment of hypertension or prehypertension in a subject comprising administering to the subject a compound claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof claim 1 , according to .10. A method for the prophylactic treatment of fibrosis in a subject comprising administering to the subject a compound claim 1 , or a stereoisomer or pharmaceutically acceptable salt thereof claim 1 , according to .11. A ...

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15-10-2015 дата публикации

METHOD FOR PROMOTING PLANT GROWTH

Номер: US20150289512A1
Принадлежит: Sumitomo Chemical Company, Limited

The present invention provides a method for promoting plant growth, which comprises treating a plant with at least one compound represented by the following Formula (1) 2. The method according to claim 1 , wherein the compound represented by Formula (1) is a compound in which{'sup': 2', '12', '1, 'Arepresents a —N(R)—, an oxygen atom, or a sulfur atom, when Ais a nitrogen atom,'}{'sup': 2', '1', '5', '3', '4, 'Arepresents an oxygen atom, when Ais —C(R)═ and Ais ═C(R)—,'}{'sup': 2', '12', '1', '5', '3, 'Arepresents —N(R)— or an oxygen atom, when Ais —C(R)═ and Ais a nitrogen atom,'}{'sup': 1', '2', '3', '4', '11', '12', '7', '11', '11', '11', '2', '12', '1', '3', '2, 'sub': 2', 'm', '5, 'R, R, R, and Rare the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a nitro group, a C1-C6 alkyl group optionally having one or more groups selected from the group X, a C2-C6 alkenyl group optionally having one or more groups selected from the group X, a C2-C6 alkynyl group optionally having one or more groups selected from the group X, a phenyl group optionally having one or more groups selected from the group Y, a 5-membered aromatic heterocyclic group optionally having one or more groups selected from the group Y, a carboxy group, a C2-C6 alkylcarbonyl group optionally having one or more halogen atoms, a benzoyl group optionally having one or more groups selected from the group Y, a C2-C6 alkoxycarbonyl group, an aminocarbonyl group, —NRR, —S(O)NRR, —OR, —S(O)R, or —SF, when Ais —N(R)— or a sulfur atom, or when at least one or more of Aand Aare a nitrogen atom and Ais an oxygen atom, and'}{'sup': 1', '2', '3', '4', '12', '15', '7', '11', '15', '11', '1', '5', '2', '3', '4, 'sub': 2', 'm', '5, 'R, R, R, and Rare the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a nitro group, a C1-C6 alkyl group optionally having one or more groups selected from the group X, a C2-C6 alkenyl group optionally having one ...

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09-12-2021 дата публикации

SOLID STATE FORMS OF PEMAFIBRATE

Номер: US20210380543A1
Принадлежит: Teva Pharmaceuticals International GmbH

The present disclosure relates to solid state forms of Pemafibrate processes for preparation thereof and pharmaceutical compositions thereof. 1. Crystalline Form A of Pemafibrate , which is characterized by data selected from one or more of the following:i. an XRPD pattern having peaks at 7.7, 8.2, 11.1, 11.6 and 18.6 degrees 2-theta±0.2 degrees 2-theta;{'figref': {'@idref': 'DRAWINGS', 'FIG. 1'}, 'ii. an XRPD pattern as depicted in ;'}{'sup': '13', 'iii. a solid state C-NMR spectrum with peaks at 171.2, 158.0, 147.9, 141.1 and 137.7 ppm±0.2 ppm;'}{'sup': '13', 'iv. a solid state C-NMR spectrum having the following chemical shift absolute differences from a peak at 127.8 ppm±1 ppm: 43.4, 30.2, 20.1, 13.3 and 9.9 ppm±0.1 ppm;'}{'sup': '13', 'figref': {'@idref': 'DRAWINGS', 'i': 'a', 'FIG. 7'}, 'v. a solid state C-NMR spectrum substantially as depicted in ; or combinations of (i)-(v).'}2. A crystalline form of Pemafibrate according to claim 1 , which is characterized by an XRPD pattern having peaks at 7.7 claim 1 , 8.2 claim 1 , 11.1 claim 1 , 11.6 and 18.6 degrees 2-theta±0.2 degrees 2-theta claim 1 , and also having one claim 1 , two claim 1 , three claim 1 , four or five additional peaks selected from 9.8 claim 1 , 14.1 claim 1 , 16.4 claim 1 , 17.4 and 20.1 degrees 2-theta±0.2 degrees 2-theta.3. Crystalline Form B of Pemafibrate claim 1 , which is characterized by data selected from one or more of the following:i. an XRPD pattern having peaks at 8.7, 13.1, 17.0, 18.2 and 22.9 degrees 2-theta±0.2 degrees 2-theta;{'figref': {'@idref': 'DRAWINGS', 'FIG. 2 or 5'}, 'ii. an XRPD pattern as depicted in ;'}{'sup': '13', 'iii. a solid state C-NMR spectrum with peaks at 173.3, 146.7, 130.8, 119.6 and 115.5 ppm±0.2 ppm;'}{'sup': '13', 'iv. a solid state C-NMR spectrum having the following chemical shift absolute differences from a peak at 107.4 ppm±1 ppm: 65.9, 39.3, 23.4, 12.2 and 8.1 ppm±0.1 ppm;'}{'sup': '13', 'figref': {'@idref': 'DRAWINGS', 'i': 'a', 'FIG. 8'}, 'v. a ...

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26-09-2019 дата публикации

LUCIFERIN DERIVATIVES FROM BICYCLIC REACTANTS AND AMINOTHIOL DERIVATIVES AND METHODS OF USE THEREOF

Номер: US20190290784A1
Принадлежит:

The present disclosure features a condensation reaction and a luciferin-unmasking reaction that can be carried out under physiological conditions. In general, the condensation reaction involves reacting a bicyclic reactant with an aminothiol derivative, generating a luciferin or luciferin derivative. A luciferin can provide detectable luminescence. A luciferin derivative can be unmasked to provide detectable luminescence in a luciferin-unmasking reaction. The present disclosure provides bicyclic reactants and aminothiol derivatives suitable for use in the condensation reaction. The condensation and luciferin-unmasking reactions find use in a variety of applications, which are also provided. 7. The compound of any of and - , wherein at least one of PGand PGis a protecting group.8. The compound of any of and - , wherein—PGis a protecting group.9. The compound of any of and - , wherein—PGis a protecting group.12. The compound of any of - , wherein PGis hydrogen.13. The compound of any of - , wherein PGis a protecting group.14. The compound of any of - , wherein PGis hydrogen.15. The compound of any of - , wherein PGis a protecting group.16. The compound of claim 15 , wherein PGforms a masked amino group in which the masked amino group is a carbamate or an amide.17. The compound of claim 15 , wherein PGforms a masked amino group in which the masked amino group is an amino group that is connected to an amino acid claim 15 , peptide claim 15 , or protein.19. The compound of any of - claim 15 , wherein PGis hydrogen.20. The compound of any of - claim 15 , wherein PGis a protecting group.26. A method for detection of a biological process or biomolecule in a test subject claim 15 , the method comprising contacting test subject with a compound of any of Formula I-V and a compound of Formula VI.27. The method of claim 15 , wherein the test subject is contacted with the compound of and .28. The method of claim 26 , further comprising monitoring the test subject for luminescence ...

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26-11-2015 дата публикации

BENZOTHIAZOLONE COMPOUND

Номер: US20150336914A1
Принадлежит: NOVARTIS AG

The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form 4. A process according to wherein the LG is chloro. The present invention relates to a benzothiazolone compound, to its preparation, to its medical use as a beta-2 adrenoceptor agonist and to medicaments, pharmaceutical compositions and combinations comprising it.Benzothiazolone compounds which are beta-2-adrenoceptor agonists are described in WO2004/16601 and WO2006/056471. WO2005/110990 also describes benzo-condensed heterocycles as beta-2 agonists.While beta-2 agonists have long been known for their bronchodilating properties, they are also known for their capability to produce skeletal muscle hypertrophy.Numerous studies have focused on therapeutic applications of the anabolic properties of beta-2 agonists for ameliorating muscle wasting and improving muscle function. However, this class of compounds has also been associated with undesirable side-effects, including increased risk of adverse cardiovascular-related events. Thus, the use of beta-2 agonists in muscle wasting diseases has hitherto been limited by cardiac hypertrophy and potentially deleterious effects on cardiovascular function.There is a need to provide new beta-2 agonists that are good drug candidates. In particular, a new beta-2 agonist should bind potently to the beta-2 adrenoceptor whilst showing little affinity for other receptors, such as e.g. the beta-1 adrenoceptor, the alpha-1A adrenoceptor, or the 5HTreceptor, and show functional activity as an agonist. It should be metabolically stable and possess favourable pharmacokinetic properties. It should be non-toxic and demonstrate few side-effects, in particular fewer cardiac side-effects than known marketed beta-2 agonists, such as e.g. formoterol. Furthermore, the ideal drug candidate will exist in a physical form that is stable, non-hygroscopic and easily formulated.The compound of the invention is a selective beta-2 agonist. In ...

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22-10-2020 дата публикации

DERIVATIVES OF LUCIFERIN AND METHODS FOR THEIR SYNTHESIS

Номер: US20200331902A1
Принадлежит:

6-Thio derivatives of D-luciferin, also referred to as D-thioluciferins, having the general structure of Formula (I) are provided. Methods for synthesising D-luciferin, its derivatives, and their related 2-cyanobenzothiazole precursors are also provided. These compounds are commercially valuable due to their application in optical imaging, particularly in bioluminescence imaging. 2. A compound as claimed in claim 1 , wherein Ris H.3. A compound as claimed in claim 1 , wherein Ris H claim 1 , halogen claim 1 , —SR claim 1 , or optionally substituted alkyl.7. A probe for a luminescence assay claim 1 , the probe comprising a compound as claimed in .9. A luciferase substrate comprising a compound as claimed in .10. A kit for a luminescence assay claim 1 , the kit comprising a compound as claimed in and optionally one or more components selected from the group consisting of a luciferase enzyme having an amino acid sequence that has at least 80% sequence identity with SEQ ID NO: 1 or with any subsequence thereof claim 1 , ATP claim 1 , coenzyme A and Mg.11. A method of biological imaging claim 1 , the method comprising contacting claim 1 , or causing to be contacted claim 1 , a compound as claimed in with a luciferase enzyme having an amino acid sequence that has at least 80% sequence identity with SEQ ID NO: 1 or with any subsequence thereof in a subject or biological sample claim 1 , and detecting a fluorescence or luminescence signal resulting from the contact.13. A method as claimed in claim 12 , wherein Y is —SR.15. A method as claimed in claim 12 , wherein the base is 1 claim 12 ,8-diazabicyclo[5.4.0]undec-7-ene (DBU) or 1 claim 12 ,5-diazabicyclo[4.3.0]non-5-ene (DBN). This application claims priority to United Kingdom patent application no. 1711983.5 which is incorporated by reference herein.The invention relates to derivatives of the molecule, D-luciferin, and methods for their synthesis.Luciferins are light emitting compounds which are oxidised by luciferase ...

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02-09-2014 дата публикации

Pesticidal carboxamides

Номер: US8822691B2
Принадлежит: Bayer CropScience AG

To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent: wherein each substituent is as defined in the specification.

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15-01-2019 дата публикации

一种[2-[(5-氯-苯并噁唑-2-基)(3-氧代丁基)氨基]乙基]氨基甲酸叔丁酯的制备方法

Номер: CN106478537B
Принадлежит: SHANGHAI ZAIQI BIO-TECHNOLOGY CO LTD

本发明公开了一种[2‑[(5‑氯‑苯并恶唑‑2‑基)(3‑氧代丁基)氨基]乙基]氨基甲酸叔丁酯的制备方法,以乙二胺、丁烯酮、2‑氨基‑4‑氯苯酚等为原料,经过五步反应得到目的产物[2‑[(5‑氯‑苯并恶唑‑2‑基)(3‑氧代丁基)氨基]乙基]氨基甲酸叔丁酯。本发明操作简便、环境友好,综合收率为52%以上,较现有35.6%的收率,具有显著的提升,大幅降低了现有药物生产成本,适合工业化规模生产。

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24-08-2017 дата публикации

2-(phenylamino)benzo[d]oxazol-5-ol derivatives, preparation method thereof, and pharmaceutical composition for use in preventing or treating inflammatory diseases containing the same as an active ingredient

Номер: KR101770310B1
Принадлежит: 이화여자대학교 산학협력단

본 발명은 2-(페닐아미노)벤조[ d ]옥사졸-5-올 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 염증성 질환의 예방 또는 치료용 약학적 조성물에 관한 것으로, 본 발명에 따른 2-(페닐아미노)벤조[ d ]옥사졸-5-올 유도체, 이의 광학 이성질체, 또는 이의 약학적으로 허용 가능한 염은 T 세포가 T 세포의 증식 촉진인자로 알려진 인터루킨-2(Interleukin-2, IL-2)에 의하여 염증성 사이토카인인 IFNγ(Interferon gamma) 생성과 5-리폭시게나아제(5-Lipoxygenase, 5-LO)의 발현이 주로 나타나는 Th1(T helper cells 1) 세포로의 분화를 방지하고, 인터루킨-6(Interleukin-6, IL-6)의 발현을 효과적으로 억제하는 활성이 우수하므로, 이와 관련한 염증성 질환의 예방 또는 치료용 약학적 조성물로 유용하게 사용될 수 있다. The present invention relates to a 2- (phenylamino) benzo [ d ] oxazol-5-ol derivative, a process for preparing the same, and a pharmaceutical composition for the prevention or treatment of inflammatory diseases containing the same as an active ingredient. (Phenylamino) benzo [ d ] oxazol-5-ol derivative, an optical isomer thereof, or a pharmaceutically acceptable salt thereof is useful as a medicament for the treatment and / or prevention of interleukin-2 (T helper cells 1) cells, which mainly express IFN gamma (interferon gamma) and 5-Lipoxygenase (5-LO), which are inflammatory cytokines, (IL-6), and thus can be effectively used as a pharmaceutical composition for the prophylaxis or treatment of inflammatory diseases associated therewith.

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18-05-2017 дата публикации

Curable compound with high refractive index, adhesive composition for optical member comprising the same and composition for optical sheet comprising the same

Номер: KR101737196B1
Принадлежит: 삼성에스디아이 주식회사

화학식 1의 화합물, 화학식 4의 화합물, 이를 포함하는 광학부재용 점착제 조성물 및 이를 포함하는 광학시트용 조성물이 제공된다. A compound of the formula (1), a compound of the formula (4), a pressure-sensitive adhesive composition for an optical member containing the same, and a composition for an optical sheet containing the same.

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12-04-2022 дата публикации

Beta adrenergic agonists and methods of use thereof

Номер: CN114340740A
Принадлежит: Kulassen Therapy

本公开涉及化合物和此类化合物在治疗与肾上腺素能受体相关的疾病中的用途。

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30-09-1982 дата публикации

Process for producing heterocyclic phenyl esters (modifications)

Номер: SU963465A3
Принадлежит: Хехст Аг (Фирма)

Compounds of formula <IMAGE> (I) wherein R is halogen, CF3, NO2, CN, (C1-C4)alkyl or (C1-C4)-alkoxy, n is zero or 1, X is O, S, NH, or N-(C1-C4)alkyl, Y is O or S, R1 is H or (C1-C4)alkyl and Z is, among others, a cyanalkyl, (subst.) carbalkoxyalkyl, (subst.) carbalkoxyphenyl, sulfoxyalkyl or oxime group, are selective herbicides active especially against weed grasses.

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16-06-1985 дата публикации

A PROCEDURE FOR PREPARING IMIDAZO-HETEROCICLICO COMPOUNDS

Номер: ES530011A0
Автор: [UNK]
Принадлежит: Fujisawa Pharmaceutical Co Ltd

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27-01-2011 дата публикации

Pesticidal carboxamides

Номер: WO2011009540A2
Принадлежит: Bayer CropScience AG

To provide novel carboxamides which exhibit an excellent pesticidal activity as pesticides. Carboxamides represented by the following Formula (I) and use thereof as pesticides and an animal parasite control agent wherein each substituent is as defined in the specification.

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24-04-2018 дата публикации

The method that the thio formyl chloride of N under a kind of microwave radiation, N- dimethylamino catalyzes and synthesizes 2- An base benzoxazole derivatives

Номер: CN107954944A
Автор: 施孙洁, 林晨, 柯方, 许建华
Принадлежит: Fujian Medical University

本发明公开一种微波辐射下N,N‑二甲基氨基硫代甲酰氯催化合成2‑氨基苯并噁唑衍生物的方法。在反应容器中加入催化剂量催化剂CuI、辅助催化剂NaOH、吡啶以及取代邻氨基苯酚和N,N‑二甲基氨基硫代甲酰氯为底物,置于微波反应仪中在一定温度和功率下反应,一定时间后,减压浓缩,产品经过柱层析纯化。本发明是一种环境友好,操作简便,高效的制备苯并噁唑化合物的方法。与现有技术相比,此方法反应速度较常规加热下明显加快,反应条件温和、操作简单、产率高,安全,成本低廉,环保; 其中R 1 为H或选自4位取代的含C 1‑4 烷基、F、Cl、Br、硝基、腈基、甲氧基、乙氧基;R 1 可在酚羟基的邻位、间位和对位。R 2 为甲基或乙基。

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02-04-2019 дата публикации

The synthetic method of 2- sulfydryl -6- chlorobenzene diozaiole

Номер: CN107033096B
Принадлежит: JIANGSU YONGKAI CHEMISTRY CO Ltd

本发明涉及化工领域,公开了一种2‑巯基‑6‑氯苯并恶唑的合成方法,包括以下步骤:(1)碱解:将6‑氯苯并恶唑酮与碱液混合均匀,升温至95℃~100℃保温反应生成2‑羟基钠‑4‑氯苯氨基酸钠,降温至75~80℃,得A液;(2)巯基合成:向所述A液中滴加二硫化碳,滴加结束后75~80℃保温反应生成2‑巯基钠‑6‑氯苯并恶唑,得B液;(3)酸化:将所述B液滴加到盐酸中反应生成2‑巯基‑6‑氯苯并恶唑,反应后体系PH为4~5,经压滤、干燥得2‑巯基‑6‑氯苯并恶唑精品。与现有技术相比,本合成方法不会在短时间内产生大量气体,不会发生冲料现象,避免了安全环保事故的发生。

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10-04-2020 дата публикации

Synthesis method of benzoxazolone

Номер: CN110698421B
Принадлежит: Hunan Subo Biotechnology Co ltd

本发明涉及有机合成技术领域,尤其涉及一种卧式双螺旋反应器中熔融状态下连续化合成苯并噁唑酮的方法。本发明相较于传统的无溶剂法,反应装置为卧式双螺旋反应器,具有连续化、受热均匀、搅拌效果好、反应时间短等优点,使得产品的原子利用度高,收率为97.3%~98.5%(以2‑氨基苯酚计),含量为98.3%~99.1%(液相色谱,外标),三废量少,且易于处理,操作简单,便于自动化生产。

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11-08-2017 дата публикации

The synthetic method of the chlorobenzene diozaiole of 2 sulfydryl 6

Номер: CN107033096A
Принадлежит: JIANGSU YONGKAI CHEMISTRY CO Ltd

本发明涉及化工领域,公开了一种2‑巯基‑6‑氯苯并恶唑的合成方法,包括以下步骤:(1)碱解:将6‑氯苯并恶唑酮与碱液混合均匀,升温至95℃~100℃保温反应生成2‑羟基钠‑4‑氯苯氨基酸钠,降温至75~80℃,得A液;(2)巯基合成:向所述A液中滴加二硫化碳,滴加结束后75~80℃保温反应生成2‑巯基钠‑6‑氯苯并恶唑,得B液;(3)酸化:将所述B液滴加到盐酸中反应生成2‑巯基‑6‑氯苯并恶唑,反应后体系PH为4~5,经压滤、干燥得2‑巯基‑6‑氯苯并恶唑精品。与现有技术相比,本合成方法不会在短时间内产生大量气体,不会发生冲料现象,避免了安全环保事故的发生。

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28-02-1993 дата публикации

Process for preparing of piperazinyl-heterocyclic compounds

Номер: EG18398A
Автор:
Принадлежит: Pfizer

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19-04-2017 дата публикации

Preparation method of benzothiazole-2-carboxylic acid

Номер: CN104860901B
Принадлежит: BEIJING UNIVERSITY OF TECHNOLOGY

一种苯并噻唑‑2‑羧酸的制备方法,属于苯并噻唑‑2‑羧酸技术领域。该方法是以2‑甲基苯并噻唑为原料,水、乙醇为溶剂,两者含量分别为0~80%,20%~100%,选用10~200ppm具有式(Ⅰ)或式(Ⅱ)结构的单核金属卟啉为催化剂,以浓度为0.5~2mol/L氢氧化钠为助剂,0.5~2.0MPa的氧气、30%过氧化氢为氧化剂,于40~140℃下反应2~12小时,得到苯并噻唑‑2‑羧酸。本方法采用金属卟啉作为催化剂,用量小,无污染;乙醇或乙醇与水混合体系的碱溶液作溶剂,绿色、无毒、环保;氧气、过氧化氢为氧化剂,大大降低了高锰酸钾以及浓硫酸对反应设备的腐蚀,提高了实验操作的安全性和环保性。

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27-08-2013 дата публикации

PESTICIDE CARBOXAMIDES

Номер: RU2012106433A
Принадлежит: Байер Кропсайенс Аг

1. Карбоксамид, описываемый следующей формулой (I)в которой D означает 6-членное ароматическое углеродное кольцо, которое может быть замещенным, или 5- - 6-членный ароматической гетероцикл, который может быть замещенным;А, А, Аи Авсе независимо означают азот, С-Хили следующую формулу (Е)при условии что, по меньшей мере, один из А, А, Аи Аявляется формулой (Е);G означает кислород или серу;Q означает водород, C-алкил, C-галогеналкил, (C-алкил)карбонил, (С-галогеналкил)карбонил, (C-алкокси)карбонил или (C-галогеналкокси)карбонил,В, В, В, Ви Вкаждый независимо означает азот, С-Хили C-J, при условии что 5 групп В, В, В, Ви Водновременно не являются азотом и, по меньшей мере, один из В, В, В, Ви Вявляется C-J, X, Xи Xкаждый независимо означает водород, цианогруппу, галоген, нитрогруппу, кислород, гидроксигруппу, меркаптогруппу, аминогруппу, формил, оксид, C-алкил, C-галогеналкил, арил-(C)алкил, гетероциклил-(C)алкил, C-алкил-О-, C-алкил-NH-, C-алкил-3-, C-алкил-S(O)-, C-алкил-S(O)-, С-алкил-S(O)О-, C-галогеналкил-O-, C-галогеналкил-NH-, C-галогеналкил-S-, C-галогеналкил-S(О)-, C-галогеналкил-S(O)-, C-галогеналкил-S(O)O-, арил-O-, арил-NH-, арил-S-, арил-S(О)-, арил-S(O)-, арил-S(O)O-, гетероциклил-O-, гетероциклил-NH-, гетероциклил-8-, гетероциклил-S(О)-, гетероциклил-S(O)-, гетероциклил-S(O)0-, C-алкил-O-(C)алкил, C-алкил-NH-(C)алкил, C-алкил-S-(C)алкил, C-алкил-S(O)-(C)алкил, C-алкил-S(O)-(C)алкил, C-галогеналкил-O-(C)алкил, C-галогеналкил-NH-(C)алкил, C-галогеналкил-S-(C)алкил, C-галогеналкил-S(O)-(C)алкил, C-галогеналкил-S(O)-(C)алкил, арил-O-(C)алкил, арил-NH-(C)алкил, арил-S-(C)алкил, арил-S(O)-(C)алкил, арил-S(O)-(C)алкил, гетероциклил-O-(C)алкил, гетероциклил-NH-(C)алкил, гетероциклил-8-(C)алкил, гетероциклил-S(O)-(C)алкил, гетероциклил-S(O)-(C)алкил, С-циклоалкил, С-циклоалкил- РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 215/48 (13) 2012 106 433 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: ...

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17-01-2020 дата публикации

Synthesis method of benzoxazolone

Номер: CN110698421A
Принадлежит: Hunan Suobo Biotechnology Co Ltd

本发明涉及有机合成技术领域,尤其涉及一种卧式双螺旋反应器中熔融状态下连续化合成苯并噁唑酮的方法。本发明相较于传统的无溶剂法,反应装置为卧式双螺旋反应器,具有连续化、受热均匀、搅拌效果好、反应时间短等优点,使得产品的原子利用度高,收率为97.3%~98.5%(以2‑氨基苯酚计),含量为98.3%~99.1%(液相色谱,外标),三废量少,且易于处理,操作简单,便于自动化生产。

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10-08-1995 дата публикации

Bioluminescent indicator based upon the expression of a gene for a modified green-fluorescent protein

Номер: WO1995021191A1
Принадлежит: Martin Chalfie, William Ward

A pre-coelenterazine peptide comprising a modified A. victoria GFP having an amino acid sequence in which Ser65 is replaced with Tyr. There are further provided a polynucleotide encoding the pre-coelenterazine peptide, allowing synthesis of large, pure amounts of coelenterazine, as by culturing organisms transformed with the polynucleotide; methods for synthesizing coelenterazine; and improved assays employing the polynucleotide or transformed organisms, e.g., to detect mutagenesis.

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30-01-1980 дата публикации

Fungicidic composition

Номер: SU713523A3

3,4-Disubstituted benzoxa(thia)zole-2-one derivatives of the formula; <IMAGE> wherein R1 is a halogen atom or methyl group, R2 is a methyl or ethyl group and X and Y are individually an oxygen or sulfur atom, and their preparation and use as a fungicide.

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15-01-1989 дата публикации

Method of controlling undesirable vegetation

Номер: SU1452454A3
Принадлежит: Хехст Аг (Фирма)

The compounds of the formula I <IMAGE> where Ar is the group <IMAGE> or <IMAGE>, R<1> is H or alkyl, R<2> is H, alkyl or phenyl, R<3> is H, halogen, nitro, alkyl, alkoxy or CF3; X and T are O, S or N-R<1>, m is 1 or 2, n is 1, 2, 3 or 4, Y is an alkylene, alkenylene or alkynylene chain, and Z is CH or N, have advantageous selective herbicidal effects against annual and perennial grass weeds. The compounds of the formula I also have plant-growth-regulating effects.

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15-09-1985 дата публикации

Method of producing 2-benzoxazolone or derivatives thereof

Номер: SU1179928A3
Принадлежит: Ugine Kuhlmann

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10-02-2005 дата публикации

Method for preparing chlorobenzoxazoles

Номер: RU2245880C2

FIELD: organic chemistry, chemical technology, agriculture, pharmacy. SUBSTANCE: invention relates to a method for preparing chlorobenzoxazoles of the formula (I): wherein R 1 , R 2 and R 3 are determined as in cl. 1; in the case (a) R 3 means hydrogen, halogen atom, cyano-, nitro-group, halogenalkyl with 1-5 carbon atoms, halogenalkoxy-group with 1-5 carbon atoms, alkyl with 1-5 carbon atoms, alkoxy-group with 1-5 carbon atoms, phenyl or phenoxy-group; or in the case (b) R 3 means chlorine atom. Method involves interaction of benzoxazoles of the formula (II) given in the invention description with chlorinating agent in the presence of acid catalyst to form the monochlorinated product (I), or in the case (b) with excess of chlorinating agent to form dichlorinated product (I) wherein R 3 means chlorine atom. Chlorobenzoxazoles are used as intermediate substances for synthesis of biologically active compounds, agents for protection of plants and pharmaceuticals preparations. Invention provides selective synthesis of chlorobenzoxazoles with high yields. EFFECT: improved preparing method. 10 cl, 7 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) (13) 2 245 880 C2 C 07 D 263/58 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2000118803/04, 08.12.1998 (24) Äàòà íà÷àëà äåéñòâè ïàòåíòà: 08.12.1998 (30) Ïðèîðèòåò: 16.12.1997 (ïï.1-10) DE 19755904.2 (73) Ïàòåíòîîáëàäàòåëü(ëè): ÀÂÅÍÒÈÑ ÊÐÎÏÑÀÉÅÍÑ ÃÌÁÕ (DE) 2 2 4 5 8 8 0 (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: DE 2059725 À, 08.06.1972. US 4433153 À, 21.02.1984. US 4658034 À, 14.04.1987. US 4764621 À, 16.08.1988. ÅÐ 0141053 À, 15.05.1985. RU 2007397 Ñ1, 15.02.1994. (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 17.07.2000 (86) Çà âêà PCT: EP 98/07969 (08.12.1998) 2 2 4 5 8 8 0 R U Àäðåñ äë ïåðåïèñêè: 103064, Ìîñêâà, óë. Êàçàêîâà,16, ÍÈÈÐ Êàíöåë ðè "Ïàòåíòíûå ïîâåðåííûå Êâàøíèí, Ñàïåëüíèêîâ è ïàðòíåðû", Êâàøíèíó Â.Ï. C 2 C ...

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08-12-1988 дата публикации

Piperazinyl-heterocyclic compound

Номер: JPS63301861A
Принадлежит: PFIZER INC

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

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16-05-1989 дата публикации

Aryl piperazinyl-(C2 or C4) alkylene heterocyclic compounds having neuroleptic activity

Номер: US4831031A
Принадлежит: PFIZER INC

Arylpiperazinyl-ethyl(or butyl)-heterocyclic compounds and their pharmaceutically acceptable acid addition salts are neuroleptic agents. They are useful in the treatment of psychotic disorders.

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26-05-1998 дата публикации

New heterocyclic aminomethyl compound, production thereof and medicinal composition containing the same

Номер: JPH10139780A
Принадлежит: ADIR SARL

(57)【要約】 【課題】 精神行動障害の治療に有用である、新規な複 素環式アミノメチル化合物を提供する。 【解決手段】 一般式(I): 【化44】 (式中、R 1 はH又はアルキルなど;nは0又は1;A はO又はS;XはCH 2 又は単結合;YはCH又はN; Arはハロゲンなどで置換されていてもよいフェニル、 3−(ベンゾ〔d〕1,2−チアゾリルなどである)で 示される化合物である。

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17-02-1981 дата публикации

Manufacture of luciferines

Номер: JPS5616480A
Принадлежит: Boehringer Mannheim GmbH

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10-06-1980 дата публикации

Plant growth regulant

Номер: JPS5576805A
Автор: Jiyosefu Damiko Jiyon
Принадлежит: Monsanto Co

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30-05-1984 дата публикации

Process for preparing benzoaxazoline-2

Номер: SU1095877A3
Автор: Руи Ноэль

1. СПОСОБ ПОЛУЧЕНИЯ БЕНЗОКСАЗОЛОНА-2 взаимодействием салициламида с типохлоритом натри  в водной среде в присутствии щелочи о т л ич а ющи йс   тем что, с цепью упрощени  технологии процесса и повышени  выхода целевого продукта, в качестве щелочи берут едкое кали и процесс ведут в присутствии хлорида натри  при отношении концентрации ионов натри  к ионам кали  1:10 3:1 . 2.Способ по п. 1, отличающийс  тем, что гипохлорит натри  берут в количестве, при котором концентраци  ионов гипохлорита в реакционной смеси составл ет 1,5 0 ,05 г-ион/л. 3.Способ по п. 1, отличающийс  тем, что едкое кали берут в количестве, при котором 5 концентраци  ионов гидроксила в реакционной смеси составл ет 6 2 ,5 г-ион/л. 4.Способ по п. 1, отличающийс  тем, что салициламид берут в количестве, при котором его концентраци  в реакционной смеси составл ет 3-0,2 моль/л. О ;О :л X) а 1. METHOD FOR OBTAINING BENZOXAZOLONA-2 by the interaction of salicylamide with sodium tipochlorite in an aqueous medium in the presence of alkali, which is causative in potassium, and the process is carried out in the presence of alkali sodium chloride at a ratio of sodium ions to potassium ions 1:10 3: 1. 2. A method according to claim 1, characterized in that the sodium hypochlorite is taken in an amount at which the concentration of the hypochlorite ions in the reaction mixture is 1.5-0.05 g-ion / l. 3. A method according to claim 1, characterized in that caustic potash is taken in an amount in which 5 the concentration of hydroxyl ions in the reaction mixture is 6: 2 g-ion / l. 4. A method according to claim 1, characterized in that the salicylamide is taken in an amount in which its concentration in the reaction mixture is 3-0.2 mol / L. O; O: l X) a

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25-10-1984 дата публикации

Process for preparing benzothiazole imide amide derivatives

Номер: KR840001933B1
Принадлежит: 몬산토 캄파니, 존 엘머 마우어

내용 없음.

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15-11-1983 дата публикации

Process for preparing 2-cyano-6-hydroxybenzthiazole

Номер: SU1055332A3

1 .Способ .тюлучени  2-циано-6-оксибензтиазола с использованием 2-хлор-6-мётоксибензтиазола, цианист того кали  и органического растворител , отличающийс  тем, что, с целью увеличени  выхода цепе Ього продукта, 2-хлор-6-метоксибензтиазол подвергают взаимодействию с йодтриметилсипаном, полученное три нетилсилильное производное гидролизуют и образующуюс  смесь 2-хлор-6-оксибензтиазбла и 2-йод-6-оксибензтиазола обрабатывают цианистым калием в среде органического растворител , предпочтительно димеТилсульфоксида . 2. Способ получени  2-цйано-6 -оксибензтиазола с использованием 2-хлор-6-метоксибензтиазопа, циаиис .того кали  и органического растворител , отличающий с   тем, что, с целью увеличени  выхода целевого продукта, 2-хлор-6-метоксибензтиазол подвергают взаимодействию С иодтриметилсиланом, полученное трИ метилсилильное производное обрабатывают цианистым калием в среде-органи ческого растворител , предпочтительно диметилсуэтьфоксида,и oбpaзyk)щийс  продукт гидролизуют. 3« Способ полумени  2-циано-6 (Л -оксибензтиазола с использованием 2-хлор-6-метоксибензтиазо1па, цианистого кали  и органического раствори тел , отличающийс  тем, что, с целью увеличени  выхода целевого продукта, 2-хлор-6-метоксибензтиазол подвергают взаимодействию с цианистым калием в среде органического растворител , предпочтительно ди- . метилсульфоксида, полученный продукт подвергают взаимодействию с иодтри; метилсиланом и образующеес  триметилсилильное производное подвергают iгидролизу 1. Method of 2-cyano-6-hydroxybenzthiazole irradiation using 2-chloro-6-methoxybenzthiazole, potassium cyanide and an organic solvent, characterized in that in order to increase the chain yield of the product, 2-chloro-6-methoxybenzthiazole interaction with iodotrimethylsipane, the obtained three non-silyl derivative is hydrolyzed and the resulting mixture of 2-chloro-6-hydroxybenzethiazbl and 2-iodo-6-hydroxybenzthiazole is treated with potassium cyanide in an organic solvent, preferably dimethylsulfoxide. 2. A ...

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01-04-1981 дата публикации

Ving an herbicidal effect process for the preparation of substituted acetanilides ha

Номер: PT72769A
Автор:
Принадлежит: Nihon Tokushu Noyaku Seizo KK

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17-02-2022 дата публикации

Beta adrenergic agonist and methods of using the same

Номер: AU2020300999A1
Принадлежит: Curasen Therapeutics Inc

The present disclosure is directed to chemical compounds and to the use of such compounds in the treatment of diseases associated with an adrenergic receptor.

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19-10-1984 дата публикации

Patent FR2521994B1

Номер: FR2521994B1
Автор: [UNK]

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04-08-1967 дата публикации

Process for the preparation of sulfonated polynuclear amines and new products thus obtained

Номер: FR1490508A
Автор: Gerard Thirot, Rene Roe
Принадлежит: Kuhlmann SA

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16-11-1984 дата публикации

Patent FR2447366B1

Номер: FR2447366B1
Автор: [UNK]
Принадлежит: Hoechst AG

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15-06-1960 дата публикации

Process for the production of thioacylhydrazones

Номер: FR1223207A
Автор:
Принадлежит: Bayer AG

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07-11-1980 дата публикации

PHENOXY-ALKANOIC ACID DERIVATIVES CARRYING A HETEROCYCLIC SUBSTITUTE AND HERBICIDE PRODUCTS CONTAINING SAME

Номер: FR2453858A1
Автор: [UNK]
Принадлежит: Hoechst AG

L'INVENTION CONCERNE DES DERIVES D'ACIDES (HYDROXY-PHENOXY)-ALCANOIQUES PORTANT, A LA PLACE DE L'HYDROGENE PHENOLIQUE, UN RADICAL BENZOXAZOLYLE OU BENZOTHIAZOLYLE. CEUX QUE L'ON CONSIDERE COMME LES MEILLEURS REPONDENT A LA FORMULE: (CF DESSIN DANS BOPI) DANS LAQUELLE R REPRESENTE UN HALOGENE OU UN GROUPE TRIFLUOROMETHYLE, NITRO OU CYANO, N EST EGAL A 0 OU A 1 ET Z DESIGNE UN RADICAL CYANETHYLE OU UN RADICAL -CH(R)-COOR DANS LEQUEL R REPRESENTE UN ALKYLE ET R UN ATOME D'HYDROGENE OU UN ALKYLE. APPLICATION EN TANT QUE MATIERES ACTIVES DE PRODUITS HERBICIDES SELECTIFS ET A LARGE CHAMP D'ACTIVITE, CAPABLES DE DETRUIRE NOTAMMENT DE NOMBREUSES PLANTES ADVENTICES MONOCOTYLEDONES, ANNUELLES OU PERENNES. THE INVENTION CONCERNS (HYDROXY-PHENOXY) -ALKANOIC ACID DERIVATIVES CARRYING, IN THE PLACE OF PHENOLIC HYDROGEN, A BENZOXAZOLYL OR BENZOTHIAZOLYL RADICAL. THOSE CONSIDERED TO BE THE BEST RESPOND TO THE FORMULA: (CF DRAWING IN BOPI) IN WHICH R REPRESENTS A HALOGEN OR A TRIFLUOROMETHYL, NITRO OR CYANO GROUP, N IS EQUAL TO 0 OR 1 AND Z DESIGNATES A RADICAL CYANETHYL OR A RADICAL -CH (R) -COOR IN WHICH R REPRESENTS AN ALKYL AND R A HYDROGEN ATOM OR AN ALKYL. APPLICATION AS ACTIVE MATERIALS OF SELECTIVE HERBICIDE PRODUCTS AND A WIDE FIELD OF ACTIVITY, CAPABLE OF DESTROYING IN PARTICULAR MANY SINGLE-LIGHT, ANNUAL OR PERENNIAL ADVENTICAL PLANTS.

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18-04-1975 дата публикации

Chalcones and analogues - analgesics having low toxicity

Номер: FR2244507A1
Автор: [UNK]

Novel cpds. of formula (I) are new: (where R1 is phenyl, opt substd. by e.g. halogen, methoxy, carboxyl, or nitro, styryl or thienyl; R2 is H or 1-6C alkyl; Y and Z are H or together form a double bond between the corresp. C atoms), are analgesics, with LD50 >2500 mg./kg.

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02-11-1990 дата публикации

NOVEL BENZOTHIAZOLINONIC DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Номер: FR2646350A1
Принадлежит: ADIR SARL

Composés de formule générale I : (CF DESSIN DANS BOPI) dans laquelle : R1 représente un atome d'hydrogène ou un groupement alkyle inférieur; R2 représente un alkyle substitué ou non, un aryle substitué ou non, une alkényle substitué ou non, un groupement thiényle, furyle, pyrrolyle ou pyridinyle substitué ou non; X représente un atome d'hydrogène; Y représente un groupement hydroxyle; ou bien X et Y représentent ensemble un atome d'oxygène, leurs énantiomères, diastéréoisomères et épimères. Médicaments. (CF DESSIN DANS BOPI) cas particulier des dérivés de formule I dans laquelle : R1 et R2 ont la même signification que dans la formule I; X représente un atome d'hydrogène; Y représente un groupement hydroxyle, dont on sépare, si on le souhaite, les isomères, par une technique classique de séparation et que l'on purifie éventuellement par une technique classique de purification. Compositions pharmaceutiques. Compounds of general formula I: (CF DRAWING IN BOPI) in which: R1 represents a hydrogen atom or a lower alkyl group; R2 represents a substituted or unsubstituted alkyl, a substituted or unsubstituted aryl, a substituted or unsubstituted alkenyl, a thienyl, furyl, pyrrolyl or pyridinyl group, substituted or not; X represents a hydrogen atom; Y represents a hydroxyl group; or else X and Y together represent an oxygen atom, their enantiomers, diastereomers and epimers. Medicines. (CF DRAWING IN BOPI) particular case of derivatives of formula I in which: R1 and R2 have the same meaning as in formula I; X represents a hydrogen atom; Y represents a hydroxyl group, the isomers of which are separated, if desired, by a conventional separation technique and which are optionally purified by a conventional purification technique. Pharmaceutical compositions.

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09-01-1981 дата публикации

PROCESS FOR THE PREPARATION OF BENZOXAZOLONE

Номер: FR2459238A1
Автор: Noel Rouy
Принадлежит: Rhone Poulenc Agrochimie SA

L'INVENTION CONCERNE UN PROCEDE DE PREPARATION DE BENZOXAZOLONE A PARTIR DE SALICYLAMIDE ET D'IONS HYPOCHLORITE. ELLE SE CARACTERISE PAR L'USAGE D'UN RAPPORT NAK PARTICULIER. ELLE S'APPLIQUE A LA REALISATION D'INTERMEDIAIRES POUR INSECTICIDES. THE INVENTION RELATES TO A PROCESS FOR PREPARING BENZOXAZOLONE FROM SALICYLAMIDE AND HYPOCHLORITE IONS. IT IS CHARACTERIZED BY THE USE OF A PARTICULAR NAK REPORT. IT APPLIES TO THE REALIZATION OF INTERMEDIARIES FOR INSECTICIDES.

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19-01-1973 дата публикации

Substd benzthiazolones - acaricides, insecticides ovicides and fungicides

Номер: FR2141002A5
Автор: [UNK]
Принадлежит: Bayer AG

Benzthiazolones of formula (I): where R1 = an electronegative gp. R2 = H, alkyl or an electronegative gp. R3 = H, OH, O-alkyl, or an aliphatic or cycloaliphatic residue R4 = H, COR5, CO2R6, CONR7R8, or SO2R9, R5 = H, alkyl alkenyl or Ph, R6 = alkyl or Ph, R7 = H, alkoxyalkyl, alkenyl, pehnylalkyl or Ph, R8 = H, alkyl or alkenyl, or NR7R8 = a heterocyclic residue, R9 = alkyl, Ph, or NMe2, and n = 1 or 2, are acaricides and insecticides with ovicidal, fungicidal and antibacterial activity. (I) are prepd. e.g. by reacting N- unsubstd. 2-carbamylbenzthiazole-3-N-oxides with POCL3 giving I (R4 = H) and then condensing with ClCOR5, ClCO2R6 or ClSO2R9.

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29-09-1995 дата публикации

New amino-alkyl benzo-thiazoline-ones bind to sigma receptors

Номер: FR2717807A1
Принадлежит: ADIR SARL

Composés de formule générale (I): (CF DESSIN DANS BOPI) où n, R1 , R2 , sont tels que définis dans la description, Médicaments.

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07-04-1978 дата публикации

HETEROCYCLIC PHENYL ETHERS AND HERBICIDAL PRODUCTS CONTAINING THEM

Номер: FR2364210A1
Автор:
Принадлежит: Hoechst AG

Dérivés d'acides phénoxy-alcanoïques contenant un radical. benzoxazolique, benzothiazolique ou benzimidazolique. Ils répondent à la formule :

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29-09-1995 дата публикации

New amino-alkyl benzo-thiazoline-ones bind to sigma receptors

Номер: FR2717806A1
Принадлежит: ADIR SARL

Aminoalkyl benzothiazolinones of formula (I), their optical isomers, and their acid and base addn. salts, are new. R1 = H or opt. substd. alkyl; R2 = -(CH2)3-N(R3)R4 (gp.R21), or a gp. of formula (R22); R3, R4 = H, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or -(CH2)m-aryl (opt. substd. on aryl by one or more halo, hydroxy, alkyl (opt. substd. by one or more halo) or lower alkoxy); m = 0-4; or NR3R4 = a 5-9 atom heterocyclic gp., opt. contg. further heteroatoms (O or S) (opt. substd. by one or more alkyl), or form a 4-(methoxyphenyl)-piperazin-1-yl gp.; n = 2-4; R5, R6 = H or halo; alkyl and alkoxy are 1-6C; alkenyl and alkynyl are 2-6C; aryl = phenyl or naphthyl; cycloalkyl is 3-8C.

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02-10-1981 дата публикации

PROCESS FOR PREPARING HETEROCYCLYLMETHYL RADICAL 2-HALOACETAMIDES, NOVEL PRODUCTS THUS OBTAINED AND THEIR USE AS HERBICIDES

Номер: FR2479221A1
Автор: John Paul Chupp
Принадлежит: Monsanto Co

DES 2-HALOACETAMIDES AYANT LA FORMULE: (CF DESSIN DANS BOPI) OU R EST UN RADICAL PHENYLE OU CYCLOALKENYLE EN C OU CE RADICAL R INDEPENDAMMENT A SUBSTITUTION ALKYLE, THIOALKYLE, ALCOXY, ALCOXYALKYLE, POLYALCOXY, CES DIFFERENTS RADICAUX ETANT EN C, ALKENYLE OU ALKYNYLE, CES DEUX RADICAUX ETANT EN C, ARYLE EN C, HALOGENE, NO, CF OU A SUBSTITUTION PAR UN NOYAU HETEROCYCLIQUE EN C CONTENANT O OU S COMME HETEROATOMES, Y ET O, S OU NR, R ETANT L'HYDROGENE OU UN GROUPE ALKYLE EN C, R EST L'HYDROGENE OU LES RADICAUX TELS QU'ILS PEUVENT ETRE SUBSTITUES SUR R ET N EST UN NOMBRE ENTIER DE 0 A 4, INCLUSIVEMENT, SONT UTILES COMME HERBICIDES. 2-HALOACETAMIDES HAVING THE FORMULA: (CF DRAWING IN BOPI) OR R IS A PHENYL OR CYCLOALKENYL RADICAL IN C OR THIS RADICAL R INDEPENDENTLY A SUBSTITUTION ALKYL, THIOALKYL, ALCOXY, ALCOXYALKYL, THESE AND C DIFFERENT RADICAL DIFFUSED ALKYL, THIOALKYL, ALCOXY, ALCOXYALKYL, THESE AND POLYALCOXENT ALKYNYL, THESE TWO RADICALS BEING IN C, ARYL IN C, HALOGEN, NO, CF OR SUBSTITUTED BY A HETEROCYCLIC NUCLEUS IN C CONTAINING O OR S AS HETEROATOMES, Y AND O, S OR NR, R BEING HYDROGEN OR A GROUP ALKYL IN C, R IS HYDROGEN OR RADICALS AS SUBSTITUTED FOR R AND N IS A WHOLE NUMBER FROM 0 TO 4, INCLUSIVELY, ARE USEFUL AS HERBICIDES.

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10-12-1982 дата публикации

Patent FR2377389B1

Номер: FR2377389B1
Автор: [UNK]
Принадлежит: Sumitomo Chemical Co Ltd

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04-11-1977 дата публикации

Patent FR2261756B1

Номер: FR2261756B1
Автор: [UNK]
Принадлежит: Roussel Uclaf SA

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10-02-1967 дата публикации

New pesticide chemicals

Номер: FR1469297A
Автор:
Принадлежит: Ciba AG, Ciba Geigy AG

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16-02-1935 дата публикации

Process for the preparation of 3.4.5.6-tetrahologene-2-amino-1-oxybenzol

Номер: FR777350A
Автор: Dr Max Raeck
Принадлежит: IG Farbenindustrie AG

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11-08-1961 дата публикации

Process for the preparation of benzoxazolone

Номер: FR1269067A
Автор:
Принадлежит: PROFATEC SOC

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24-08-1984 дата публикации

NOVEL HYDROXYLAMINE DERIVATIVES, PROCESS FOR PREPARING THEM AND THEIR APPLICATION AS PLANT GROWTH FACTORS

Номер: FR2541282A1
Принадлежит: Roussel Uclaf SA

L'INVENTION A POUR OBJET LES COMPOSES DE FORMULE (I): (CF DESSIN DANS BOPI) DANS LAQUELLE AR REPRESENTE UN RADICAL AROMATIQUE OU HETERO-AROMATIQUE MONO OU POLYCYCLIQUE EVENTUELLEMENT SUBSTITUE ET R REPRESENTE UN ATOME D'HYDROGENE, UN RADICAL CO R OU CO R, R ET R REPRESENTANT UN RADICAL ALKYLE OU UN RADICAL AROMATIQUE MONO OU POLYCYCLIQUE EVENTUELLEMENT SUBSTITUE, AINSI QUE LEURS SELS D'ADDITION AVEC LES ACIDES.

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07-06-1983 дата публикации

Soya plant growth control method

Номер: SU1022648A3

Compounds having the formula <IMAGE> are found to be effective plant growth regulants.

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24-12-1970 дата публикации

N-Substd. and N,N-Disubstd. aminocarbonylalkyl cpds. - having anti-inflammatory and/or anti-arrhythmic activity

Номер: FR2035788A2
Автор: [UNK]
Принадлежит: Fujisawa Pharmaceutical Co Ltd

N-substd. - and N, N-disubstd.-aminocarbonyl-alkyl compounds of general formula (I): Z =-S or lower alkylimino; A = lower alkylene; R1 = H, halogen, lower alkyl, lower alkoxy or trifluoromethyl; R2 = H, alkyl or hydroxy-alkyl R3 = H, alkyl, halo alkyl, hydroxy-alkyl, alkanoyloxy-alkyl, alkoxy-alkyl, hydroxy-alkoxy-alkyl, hydroxycarbonyl-alkyl, alkoxycarbonyl-alkyl, phenyl opt. substd. by one or more alkyl, halogen, hydroxy, alkoxy and/or alkanoyl; phenyl-alkyl opt. nuclearly substd. by one or more halogen, hydroxy, lower alkoxy and/or alkanoyl; or a group -A1 - NR4R5; or NR2R3 may form a 3-7 membered heterocyclic ring. A1 = lower alkylene; R4 and R5 = alkyl or phenyl or form together with N a 5-7 membered heterocyclic ring; R1 cannot be H when R2 and R3 are lower alkyl or form together with N a alkylene group or form together an oxa-alkylene group. R1 cannot be Cl when R2 and R3 are both H. (I) Have anti-inflammatory and/or antiarrhythmic activity and may be used in the treatment of inflammations and certain cases of arrhythmia e.g. conversion of atric fibrillation, abolition of paroxysmal atric tachycardia and control of ventricular ectopic beats.

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27-10-1978 дата публикации

PROCESS FOR THE PREPARATION OF 2-HYDROXYBENZOTHIAZOLE COMPOUNDS AND NEW PRODUCTS THUS OBTAINED

Номер: FR2385706A1
Автор: [UNK]
Принадлежит: Monsanto Co

Procédé de préparation de composés de 2-hydroxybenzothiazole et nouveaux produits ainsi obtenus. Ce procédé consiste à faire réagir de l'o-aminobenzènethiol et du sulfure de carbonyle en présence d'une amine tertiaire et d'un solvant approprié, le mélange réactionnel étant chauffé à une température comprise entre la température ambiante et la température de reflux du solvant. La présente invention est particulièrement utile pour la préparation de composés de 2-hydroxybenzothiazole qui sont des intermédiaires pour la formation de 2-oxo-3-benzothiazolines employés comme produits de régulation de la croissance des plantes. Process for the preparation of 2-hydroxybenzothiazole compounds and new products thus obtained. This process consists of reacting o-aminobenzenethiol and carbonyl sulphide in the presence of a tertiary amine and a suitable solvent, the reaction mixture being heated to a temperature between room temperature and the reflux temperature of the gas. solvent. The present invention is particularly useful for the preparation of 2-hydroxybenzothiazole compounds which are intermediates for the formation of 2-oxo-3-benzothiazolines used as products of plant growth regulation.

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