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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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Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Применить Всего найдено 4139. Отображено 199.
18-03-2024 дата публикации

АНИЛИДЫ АМИНОКИСЛОТ В КАЧЕСТВЕ НИЗКОМОЛЕКУЛЯРНЫХ МОДУЛЯТОРОВ IL-17

Номер: RU2815505C2
Принадлежит: ЛЕО ФАРМА А/С (DK)

Изобретение относится к соединению формулы (I) или его фармацевтически приемлемым солям, которые обладают ингибирующей активностью в отношении IL-17. В формуле (I) R1 выбирают из группы, состоящей из 5-членного гетероарила, который содержит от 2 до 3 гетероатомов, выбранных из N, O и S, 9- или 10-членного бициклического гетероарила, который содержит от 2 до 3 гетероатомов, выбранных из N, O и S, фенила, (C1-C6)алкокси, (C3-C7)циклоалкокси, (C1-C6)алкила, фенил-(C1-C4)алкила, (C3-C7)циклоалкила и -NRcRd, где указанный 5-членный гетероарил, 9- или 10-членный бициклический гетероарил, фенил, (C1-C6)алкокси, (C3-C7)циклоалкокси, (C1-C6)алкил, фенил-(C1-C4)алкил и (C3-C7)циклоалкил необязательно замещен одним или более заместителями, независимо выбранными из Ra; Ra представляет собой галоген, гидрокси, -NRcRd, (C1-C6)алкил, (C3-C7)циклоалкил, фенил, 5- или 6-членный гетероарил, который содержит от 1 до 3 гетероатомов, выбранных из N, O и S, или 4-6-членный гетероциклоалкил, который содержит ...

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10-08-2007 дата публикации

ИНГИБИТОРЫ ПРОДУЦИРОВАНИЯ / СЕКРЕЦИИ β-АМИЛОИДНОГО БЕЛКА

Номер: RU2304140C2

Описывается соединение общей формулы (3): где R15 представляет гетероциклическую группу, выбранную из 3-7-членной насыщенной или 4-7-членной ненасыщенной моноциклической гетероциклической группы, имеющей 1-4 атома, выбранных из атома азота, атома кислорода и атома серы, или 7-14-членной полициклической гетероциклической группы, имеющей 1-4 атома, выбранных из атома азота, атома кислорода и атома серы, которая может иметь заместитель; R16представляет циклоалкильную группу, имеющую 3-7 атомов углерода, моноциклическую ароматическую углеводородную группу, имеющую 6-14 атомов углерода, или гетероциклическую группу, выбранную из 3-7-членной насыщенной или 4-7-членной ненасыщенной моноциклической гетероциклической группы, имеющей 1-4 атома, выбранных из атома азота, атома кислорода и атома серы, которая может иметь заместитель; R17представляет моноциклическую ароматическую углеводородную группу, имеющую 6-14 атомов углерода, или гетероциклическую группу, выбранную из 4-7-членной ненасыщенной ...

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20-11-1999 дата публикации

ПРИМЕНЕНИЕ ПРОИЗВОДНЫХ ИМИДАЗОЛА ДЛЯ ПРИГОТОВЛЕНИЯ ФАРМКОМПОЗИЦИЙ, АКТИВНЫХ К РЕЦЕПТОРАМ АТ1 И АТ2 АНГИОТЕНЗИНА, НЕКОТОРЫЕ ИЗ ЭТИХ СОЕДИНЕНИЙ, СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ИМИДАЗОЛА И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ НА ИХ ОСНОВЕ

Номер: RU2141321C1
Принадлежит: Руссель Юклаф (FR)

Изобретение касается химии и медицины. Предложено новое средство, фармацевтические композиции на его основе для лечения заболеваний, связанных с аномальной стимуляцией рецепторов АТ1 и АТ2, - соединение формулы I Значения радикалов приведены в формуле. Предложены новые соединения с вышеуказанной активностью и способы их получения. 6 с. и 9 з.п.ф-лы, 4 табл.

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20-03-1996 дата публикации

ИМИДАЗОЛИЛЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ ЦИКЛОГЕКСАНА И ИХ СОЛИ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ИСХОДНЫЕ СОЕДИНЕНИЯ И СПОСОБ ИХ ПОЛУЧЕНИЯ, ЛЕКАРСТВЕННОЕ СРЕДСТВО И СПОСОБ ЕГО ПОЛУЧЕНИЯ

Номер: RU93046254A
Принадлежит:

Объектом изобретения являются имидазолилзамещенные производные циклогексана общей формулы где A означает линейный или разветвленный алкил или алкенил с 1 - 8 атомами углерода каждый или циклоалкил с 3 - 8 атомами углерода; B означает водород, галоген или перфторалкил с 1 - 5 атомами углерода; D означает группу формулы -CH2 OR3 или -CO-R4, где R3 означает водород или линейный или разветвленный алкил с 1 - 8 атомами углерода; R4 означает водород, гидроксигруппу или линейный или разветвленный алкоксил с 1 - 8 атомами углерода; R1 означает водород, галоген, нитрогруппу, гидроксигруппу, трифторметильную группу, трифторметоксигруппу, линейный или разветвленный алкил, алкокси или алкоксикарбонил с 1 - 6 атомами углерода каждый, цианогруппу или карбоксил, R2 означает остаток формул -CO-R5, -CO-NR6R7 или где R5 означает гидроксил или линейный или разветвленный алкоксил с 1 - 8 атомами углерода; R6 означает водород, линейный или разветвленный алкил с 1 - 6 атомами углерода; R7 означает остаток формул ...

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10-11-2013 дата публикации

СПОСОБ ПОЛУЧЕНИЯ СОЕДИНЕНИЙ БИФЕНИЛИМИДАЗОЛА

Номер: RU2012117812A
Принадлежит:

... 1. Способ получения соединения формулы I:где Rозначает -Салкил, и P представляет защитную группу карбоновой кислоты, включающей стадию взаимодействия соединения формулы 1:с соединением формулы 2:в органическом разбавителе и водном разбавителе основного характера в присутствии межфазного катализатора, где разбавители являются по существу несмешивающимися, с образованием соединения формулы I.2. Способ по п.1, где органическим разбавителем является толуол.3. Способ по п.1, где водным разбавителем основного характера является NaOH.4. Способ по п.1, где межфазным катализатором является тетрабутиламмонийбромид.5. Способ по п.1, дополнительно включающий стадию получения кристаллической формы соединения формулы I.6. Способ получения соединения формулы II:или его соли; где Rпредставляет -Салкил, Rпредставляет -Салкил, и P представляет защитную группу карбоновой кислоты; включающий стадии:(a) взаимодействия соединения формулы I:с реагентом калий-Салкилтрифторборатом в присутствии палладий-фосфинового ...

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10-10-1996 дата публикации

СПОСОБ ПОЛУЧЕНИЯ 2-ЗАМЕЩЕННЫХ 5-ХЛОРИМИДАЗОЛ-4-КАРБАЛЬДЕГИДОВ

Номер: RU94040184A
Принадлежит:

Описывается новый способ получения 2-замещенных 5-хлоримидазол-4-карбальдегидов. При этом гидрогалогенид глицинового эфира с помощью эфира имидокислоты циклизуют до 2-замещенного 3,5-дигидроимидазол-4-она, переводят его с помощью N,N-замещенного формамидацеталя в N,N-замещенный аминометиленимидазолинон и затем хлорируют. 5-хлоримидазол-4-карбальдегиды представляют собой важные промежуточные продукты для изготовления фармацевтических препаратов, снижающих кровяное давление.

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10-04-2001 дата публикации

ПРОИЗВОДНЫЕ N-(ИМИДАЗОЛИЛБУТИЛ)БЕНЗОЛСУЛЬФАМИДА, ИХ ПОЛУЧЕНИЕ И ИХ ТЕРАПЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ

Номер: RU99113043A
Принадлежит:

... 1. Соединения формулы (I) в которой каждый из R1 и R'1, независимо друг от друга, представляет собой либо атом водорода, либо атом галогена, либо (С1-С4)алкильную группу; R2 представляет собой либо пиперидин-1-ильную группу, возможно замещенную в положении 4 одной или более чем одной группой, выбранной из гидроксильной, (С1-С4)алкильной, причем последняя является нормальной или разветвленной, гидрокси(С1-С4)алкильной, (С1-С4)алкокси(С1-С4)алкильной, (С1-С4)алкокси, (С1-С4)алкилтио, нитрильной, монофторметильной, дифторметильной, трифторметильной, 2-фторэтокси, 2,2,2-трифторэтокси, (С3-С6)цикпоалкильной, -COOR' и -CONR'R'' групп (причем R' представляет собой (С1-С4)алкильную группу, а R'' представляет собой атом водорода или (C1-С4)алкильную группу), или группой =CYZ [причем Y и Z выбраны, независимо друг от друга, из атомов водорода и галогена и (С1-С4)алкильной (возможно замещенной одним или более чем одним атомом галогена), циано и -COOR' групп, a R1 является таким, как определено выше ...

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10-10-1996 дата публикации

СПОСОБ ПОЛУЧЕНИЯ 2-ЗАМЕЩЕННЫХ 5-ХЛОРИМИДАЗОЛ-4-КАРБАЛЬДЕГИДОВ

Номер: RU94040184A1
Принадлежит:

Описывается новый способ получения 2-замещенных 5-хлоримидазол-4-карбальдегидов. При этом гидрогалогенид глицинового эфира с помощью эфира имидокислоты циклизуют до 2-замещенного 3,5-дигидроимидазол-4-она, переводят его с помощью N,N-замещенного формамидацеталя в N,N-замещенный аминометиленимидазолинон и затем хлорируют. 5-хлоримидазол-4-карбальдегиды представляют собой важные промежуточные продукты для изготовления фармацевтических препаратов, снижающих кровяное давление.

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01-01-1969 дата публикации

СПОСОБ ПОЛУЧЕНИЯ 2-АЛКИЛ-4,5-ДИХЛОРИМИДАЗОЛОВ

Номер: SU232270A1
Автор:
Принадлежит:

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15-11-1983 дата публикации

Гербицидное средство

Номер: SU1055311A3
Принадлежит: БАСФ АГ (ФИРМА)

ГЕРБИЦИДНОЕ СРЕДСТВО, содержащее активное вещество - замещенный анилид карбоновой кислоты, растворитель и поверхностно-активное вещество, отличающее|с я тем, что, с целью снижения фйтотоксичности , оно содержит в замещенного анилида карбогде R и R одинаковые или различные и означают метил или этил, ; R - метоксиметил, метоксиизопропил , 1-пйразрлилметил, 1-имидаЗОЛИЛМ8ТЙЛ , ,4-триазолил-1-метил , R - 1,2,4-триазолил-1-, имидазолил-1-4 ,5-дихлоримидазолил-1, пиразолил-1 I 6 качестве растворителя - ксилол, а в качестве поверхностно активного вещества - оксиэтилированный N-моноэтаноламид олеиновой кислоты , кальциевую соль додецилбензолсульфокислоты и оксизтилированное касторовое масло при массовом соот :н шении 20:64t8:4:4 соответственно. :л :п :о ...

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25-03-1999 дата публикации

New 1-benzyl-imidazole and known tetrazole derivatives

Номер: DE0019741636A1
Принадлежит:

... 1-Benzylimidazole derivatives of formula (I) and their salts are new. R1 = H, 1-8C alkyl, -CaH2a-Ar or -CaH2a-(3-7C)cycloalkyl; a = 0-2; Ar = phenyl or 1-9C heteroaryl (both optionally substituted by 1-3 F, Cl, Br, I, CF3, Me, OMe, OH or NR8R9); R8, R9 = H or 1-4C alkyl; R2, R3 = H, F, Cl, Br, I, CF3, CN, NO2, CH2OR17, COR6 or OR7, 1-8C alkyl, 3-7C cycloalkyl, -CaH2a-Ar or -SOa-R22; R17= H or 1-8C alkyl; R6 = H, 1-8C alkyl, OR30 or phenyl (optionally substituted as in Ar); R7 = H, 1-8C alkyl or Ar; R22 = 1-8C alkyl, 3-7C cycloalkyl or -CaH2a-Ph; R4, R5 = H, 1-8C alkyl, F, Cl, Br, I, CF3, CN, NO2, SOa-R16, COR23 or OR24; R16 = 1-8C alkyl or phenyl (optionally substituted as in Ar); R23 = H, 1-8C alkyl or OR25; R24 = H, 1-8C alkyl or phenyl (optionally substituted as in Ar); and R25 = H or 1-8C alkyl. Also claimed is the treatment or prophylaxis of ischaemia-mediated conditions or the treatment of respiratory disorders using a tetrazole derivative.

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12-07-1984 дата публикации

Substituted diphenyl ethers

Номер: DE0003248779A1
Принадлежит:

Novel substituted diphenyl ethers of the formula in which R<1>, R<2>, R<3>, R<4>, R<5>, Y, m and n have the meaning given in the description, a plurality of processes for the preparation of the novel substances, and their use as herbicides. Novel intermediates and processes for their preparation.

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17-12-1970 дата публикации

Verfahren zur Herstellung von Imidazolderivaten

Номер: DE0001695139A1
Автор: HOFFER MAX, HOFFER,MAX
Принадлежит:

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05-06-1974 дата публикации

THIOPHOSPHATE ESTERS HAVING PESTICIDAL ACTIVITY

Номер: GB0001354729A
Автор:
Принадлежит:

... 1354729 Pesticidal application of thiophosphate esters CIBA-GEIGY AG 4 Aug 1971 [5 Aug 1970] 36660/71 Heading A5E [Also in Division C2] Compounds of formula I where R 1 and R 2 are C 1-4 alkyl, Z and X are oxygen or sulphur, n is 0 or 1, R 3 is hydrogen or methyl and Y 1 , Y 2 and Y 3 are chlorine or bromine are used as the active ingredients in conventional pesticidal compositions, optionally together with other pesticides such as those specified in German Offenlegungsschrift 2133571.

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14-09-1983 дата публикации

ALKYNYLAMINO ETHYLENES

Номер: GB0002102791B
Принадлежит: BRISTOL MYERS CO, * BRISTOL-MYERS COMPANY

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01-06-1994 дата публикации

Angiotensin-11 receptor blocking cycloalkylbenzylimidazoles

Номер: GB0002272899A
Принадлежит:

Novel cycloalkylbenzylimidazoles of Formula (I), where X is a cycloalkenyl group substitutes at the alpha position by a carboxyl or tetrazolyl group. These compounds are useful angiotensin II antagonists.

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17-01-1968 дата публикации

A novel imidazole derivative and a process for the preparation thereof

Номер: GB0001099789A
Автор:
Принадлежит:

... 2 - Iodo - 4 (or 5) - nitroimidazole is prepared by nitrating 2,4 (or 5)-diiodo-imidazole.

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02-04-1969 дата публикации

A novel halo-cyano-imidazole and its use as a herbicide

Номер: GB0001147555A
Принадлежит:

... 1,147,555. 1 - Cyano - 2,4,5 - trichloro- and 1,2,4,5 - tetrachloro - imidazole. SHELL INTERNATIONALE RESEARCH MAATSCHAPPIJ N.V. 6 Feb., 1967 [8 Feb., 1966; 12 Oct., 1966], No. 5534/67. Heading C2C. [Also in Division A5] The invention comprises 1-cyano-2,4,5-trichloroimidazole. The compound is prepared by reacting 1,2,4,5-tetrachloroimidazole with anhydrous cuprous cyanide at a temperature of at least 110‹ C., or by reacting 2,4,5-trichloroimidazole with an alkali metal alcoholate. in the presence of an inert polar solvent and in the absence of moisture and then reacting the resulting 2,4,5-trichloroimidazole salt solution with cyanogen chloride or bromide at 0-30‹ C. The 1,2,4,5-tetrachloroimidazole starting material may be obtained by chlorination of an imidazole salt (e.g. the hydrochloride) in the presence of a chlorinated hydrocarbon solvent and under anhydrous conditions.

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08-10-1980 дата публикации

1 - ACYLOXYMETHYL - 4,5 - DICHLORO - IMIDAZOLE - 2-CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PLANT PROTECTION AGENTS

Номер: GB0001576509A
Автор:
Принадлежит:

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31-08-2006 дата публикации

Substituted heteroaryl and phenylsulfamoyl compounds

Номер: AP0200603714D0
Принадлежит:

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31-07-2013 дата публикации

Glucagon receptor modulator

Номер: AP0201307012D0
Принадлежит:

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31-07-1991 дата публикации

CYCLOPROPYLACETIC ACID DERIVATIVES

Номер: AP0009100295D0
Автор:
Принадлежит:

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21-10-1993 дата публикации

Cyclopropylacetic acid derivatives.

Номер: AP0000000288A
Принадлежит:

Novel 2-(2,2-difluorocyclopropyl)-acetic acid derivatives of formula i wherein a is oxygen or -nr1- b is c2-c6alkylene, d id oxygen, sulfur or -o-ch2-, e is phenyl;phenyl substituted by from one to three substituents selected from the group halogen, c1-c4alkyl, c1-c3haloalkyl and c1-c4alkoxy; a five-membered aromatic heterocycle having from one tothree hetero atoms selected from the group nitrogen,oxygen and sulfur, a five-membered aromatic heterocycle having from one to three hetero atoms selected from the group nitrogen, oxygen and sulfur that is substituted by one or two substituents selected from the group halogen, c1-c4alkyl and c1-c3-haloalkyl; a six-membered aromatic heterocycle having from one to three nitrogen atoms; or a six-membered aromatic heterocycle having from one to three nitrogen atoms that is substituted by one or two substituted by one ot two substituents selected from the group halogen, c1-c4alkyl and c1-c3 haloalkyl, l is halogen or methyl, n is 0, 1 or 2 and r1 is ...

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31-08-2007 дата публикации

Compounds that modulate PPAR activity and methods for their preparation

Номер: AP0000001772A
Принадлежит:

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31-07-1992 дата публикации

Retroviral protease inhibitors.

Номер: AP0009200410A0
Принадлежит:

The present invention provides compounds, more particularly depeptide analogs, which bind to retroviral proteases. These compounds are inhibitors of retroviral proteases and are sueful for treating diseases relating to infection by retroviruses.

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31-07-1991 дата публикации

CYCLOPROPYLACETIC ACID DERIVATIVES

Номер: AP0009100295A0
Автор:
Принадлежит:

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30-09-2004 дата публикации

Compounds that modulate PPAR activity and methods for their preparation

Номер: AP2004003135A0
Автор:
Принадлежит:

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31-08-2006 дата публикации

Substituted heteroaryl and phenylsulfamoyl compounds

Номер: AP2006003714A0
Принадлежит:

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31-07-2015 дата публикации

Glucagon receptor modulator

Номер: AP0000003338A
Принадлежит:

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31-07-2013 дата публикации

Glucagon receptor modulator

Номер: AP2013007012A0
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30-06-1992 дата публикации

Pesticidal 1-arylimidazoles.

Номер: OA0000009207A
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31-03-1989 дата публикации

Pesticidal method using 2-phenylimidazole derivatives.

Номер: OA0000008721A
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30-06-1981 дата публикации

New useful acetanilides like weedkillers.

Номер: OA0000006061A
Автор:
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31-10-1980 дата публикации

Method of preparation of a compound antihistamine.

Номер: OA0000004814A
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30-04-1981 дата публикации

New derivatives of carboxylic acid 4,5-dichlorimidazole-2-, their method of preparation and their application like pesticides.

Номер: OA0000005593A
Автор:
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15-09-1994 дата публикации

1-Arylimidazoles pesticides.

Номер: OA0000009901A
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31-07-1992 дата публикации

RETROVIRAL PROTEASE INHIBITORS

Номер: AP0009200410D0
Автор:
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31-07-2013 дата публикации

Glucagon receptor modulator

Номер: AP0201307012A0
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Substituted heteroaryl and phenylsulfamoyl compounds

Номер: AP0200603714A0
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30-09-2004 дата публикации

Compounds that modulate PPAR activity and methods for their preparation

Номер: AP0200403135D0
Автор:
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30-09-2004 дата публикации

Compounds that modulate PPAR activity and methods for their preparation

Номер: AP0200403135A0
Автор:
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15-09-2008 дата публикации

NPYY5-ANTAGONISTEN

Номер: AT0000405257T
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25-06-1980 дата публикации

PROCEDURES FOR THE PRODUCTION OF NEW N-SUBSTI TUIERTEN HALOGENACETANILIDEN

Номер: AT0000357153B
Автор:
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26-04-1982 дата публикации

HERBICIDE

Номер: AT0000366550B
Автор:
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15-09-1980 дата публикации

HERBIZID

Номер: ATA709078A
Автор:
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15-10-1979 дата публикации

HERBIZID

Номер: ATA755477A
Автор:
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15-09-1980 дата публикации

HERBICIDE

Номер: AT0000709078A
Автор:
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15-10-1976 дата публикации

HERBICIDE MEANS

Номер: AT0000349774A
Автор:
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15-09-1988 дата публикации

NEW DOPAMINE BETA HYDROXYLASEINHIBITOREN

Номер: AT0000269087A
Автор:
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15-09-1995 дата публикации

INHIBITORS OF THE CALCIUM ADMISSION.

Номер: AT0000127455T
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15-12-1986 дата публикации

4-CHLOR-2-PHENYLIMIDAZOL-5-ESSIGSAEUREABKOEMMLING.

Номер: AT0000023997T
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15-02-1984 дата публикации

IMIDAZOL-5-ESSIGSAEUREDERIVATE, YOUR PRODUCTION AND USE.

Номер: AT0000005880T
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15-11-1994 дата публикации

ANGIOTENSIN II-RECEPTOR-BLOCKING IMIDAZOLE.

Номер: AT0000113276T
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10-01-1974 дата публикации

Procedure for the production of a new Oxazins

Номер: AT0000312625B
Автор:
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15-10-2006 дата публикации

CELL ADHESION INHIBITORS

Номер: AT0000339196T
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11-07-1977 дата публикации

HERBICIDE MEANS

Номер: AT0000337493B
Автор:
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15-09-2004 дата публикации

NEW IMIDAZOLE WITH ENTZÜNDUNGSHEMMENDER EFFECT

Номер: AT0000275549T
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28-05-1987 дата публикации

2,21-B1-1H-IMIDAZOLES

Номер: AU0006556586A
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27-02-1975 дата публикации

PEST CONTROL AGENTS

Номер: AU0000458520B2
Автор:
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21-02-2013 дата публикации

Fungicidal imidazoles

Номер: AU2011307289A1
Принадлежит:

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, Formula 1 wherein Q ...

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15-03-2012 дата публикации

Process for preparing biphenyl imidazole compounds

Номер: AU2010300788A1
Принадлежит:

The invention provides processes for preparing intermediates useful for preparing compounds of the formula (IV), or a salt thereof, where R are as defined in the specification.

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13-03-1980 дата публикации

PRODUCTION OF 2-AMINO-2-ALKYLTHIO-NITROETHYLENES

Номер: AU0000508238B2
Автор: WHITE G R, DYER N D, G.R. WHITE
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11-04-2013 дата публикации

NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS

Номер: US20130090478A1
Принадлежит:

The present invention is directed to novel opioid receptor modulators of Formula (I). 1. A compound , wherein said compound is 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.3. A hydrobromic , hydriodic , perchloric , sulfuric , nitric , phosphoric , acetic , propionic , glycolic , lactic , succinic , maleic , fumaric , malic , tartaric , citric , benzoic , mandelic , methanesulfonic , hydroxyethanesulfonic , benzenesulfonic , oxalic , pamoic , 2-naphthalenesulfonic , p-toluenesulfonic , cyclohexanesulfamic , salicylic , saccharinic or trifluoroacetic acid salt of 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.4. A benzathine , chloroprocaine , choline , diethanolamine , ethylenediamine , meglumine , procaine , aluminum , calcium , lithium , magnesium , potassium , sodium , or zinc salt of 5-({[2-Amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-4 ,5-dihydro-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. The present application is a divisional of U.S. Ser. No. 12/838,825, filed Jul. 19, 2010, which is a divisional of U.S. Ser. No. 11/877,747, filed Oct. 24, 2007 (now U.S. Pat. No. 7,786,158), which is a continuation of U.S. Ser. No. 11/079,647, filed Mar. 14, 2005 (now U.S. Pat. No. 7,741,356), which claims the benefit of U.S. Provisional App. No. 60/553,342, filed Mar. 14, 2004, the entire contents of each of which are hereby incorporated by reference.The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of opioid modulated disorders.The opioid receptors were identified in the mid-1970's, and were quickly categorized into three sub-sets of receptors (mu, ...

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18-04-2013 дата публикации

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS AND METHODS

Номер: US20130096315A1
Принадлежит:

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed. 146.-. (canceled)48. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris lower alkyl substituted with hydroxy.49. The compound of claim 48 , or a pharmaceutically acceptable salt thereof claim 48 , wherein Ris 2-hydroxyethyl.50. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris lower alkyl substituted with optionally substituted amino.51. The compound of claim 50 , or a pharmaceutically acceptable salt thereof claim 50 , wherein Ris lower alkyl substituted 2-dimethylamino-acetylamino.52. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris halo.53. The compound of claim 52 , or a pharmaceutically acceptable salt thereof claim 52 , wherein Ris chloro.54. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris optionally substituted isopropoxy.55. The compound of claim 54 , or a pharmaceutically acceptable salt thereof claim 54 , wherein Ris 2 claim 54 ,2 claim 54 ,2-trifluoro-1-methyl-ethoxy.56. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris chloro and Ris 2 claim 47 ,2 claim 47 ,2-trifluoro-1-methyl-ethoxy.57. The compound of claim 47 , or a pharmaceutically acceptable salt thereof claim 47 , wherein Ris selected from 1-methyl-1H-imidazol-4-yl and 1-ethyl-1H-imidazol-4-yl claim 47 , each optionally substituted with optionally substituted lower alkyl.58. The compound of claim 57 , or a pharmaceutically acceptable salt thereof claim 57 , wherein Ris selected from 1-methyl-1H-imidazol-4-yl and 1-ethyl-1H-imidazol-4-yl claim 57 , each optionally substituted with 1-hydroxy-1-methyl-ethyl.59. The compound of claim 57 , or a pharmaceutically acceptable salt thereof claim 57 , wherein Ris selected from 1- ...

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25-04-2013 дата публикации

HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS

Номер: US20130102789A1
Принадлежит: Dow Global Technologies LLC

Hafnium complexes of heterocyclic organic ligands having improved solubility in aliphatic hydrocarbon solvents and their use as components of olefin polymerization catalysts as well as novel syntheses of component parts thereof are disclosed. 2. The process of wherein Ris methyl claim 1 , Ris bromo claim 1 , and the reaction is conducted in an organic solvent comprising an aliphatic ether at −80° C. This application is a divisional application of the U.S. patent application Ser. No. 12/299,519, filed on Nov. 4, 2008, entitled “HAFNIUM COMPLEXES OF HETEROCYCLIC ORGANIC LIGANDS,” and which is a 371 national phase of PCT application number PCT/US07/07882, filed on Mar. 29, 2007, which claims the benefit of U.S. Provisional Patent Application No. 60/798,108, filed on May 5, 2006, the teachings of which are incorporated by reference herein, as if reproduced in full hereinbelow.This invention is directed to certain hafnium complexes, to catalyst compositions comprising the same, and to addition polymerization processes, especially olefin polymerization processes, using such hafnium complexes as one component of a coordination polymerization catalyst composition.Advances in polymerization and catalysis have resulted in the capability to produce many new polymers having improved physical and chemical properties useful in a wide variety of superior products and applications. With the development of new catalysts the choice of polymerization-type (solution, slurry, high pressure or gas phase) for producing a particular polymer has been greatly expanded. Also, advances in polymerization technology have provided more efficient, highly productive and economically enhanced processes. Recently, several new disclosures related to metal complexes based on polyvalent metal-centered, heteroaryl donor ligands have published. Among these are U.S. Pat. No. 6,103,657, U.S. Pat. No. 6,320,005, U.S. Pat. No. 6,653,417, U.S. Pat. No. 6,637,660, U.S. Pat. No. 6,906,160, U.S. Pat. No. 6,919, ...

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02-05-2013 дата публикации

METHODS OF PREPARING 1-(4-((1R,2S,3R)-1,2,3,4-TETRAHYDROXYBUTYL)-1H-IMIDAZOL-2-YL)ETHANONE

Номер: US20130109865A1
Автор: Wu Wenxue
Принадлежит:

Methods of preparing 1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone and derivatives thereof are disclosed. 1. A method of preparing 1-(4-((1R ,2S ,3R)-1 ,2 ,3 ,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone , which comprises:contacting 2-ethoxyacrylimidate with a weak acid salt of D-glucosamine to provide a first mixture;contacting the first mixture with a base to provide a second mixture;adding an aqueous acid to the second mixture to provide a third mixture;maintaining the third mixture at a temperature of greater than 30° C. for at least 0.5 hours; andisolating 1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone from the third mixture.2. The method of claim 1 , wherein the weak acid salt of D-glucosamine is D-glucosamine acetate.3. The method of claim 2 , wherein the base is an alkaline or alkaline earth metal alkoxide claim 2 , hydroxide claim 2 , carbonate claim 2 , phosphate claim 2 , or trialkylamine.4. The method of claim 3 , wherein the base is methoxide.5. The method of claim 1 , wherein the first mixture is maintained at a temperature of greater than 10° C. for at least 0.5 hours.6. The method of claim 1 , wherein the second mixture is maintained at a temperature of greater than 5° C. for at least 1 hour.7. The method of claim 1 , wherein the third mixture is maintained at a temperature of greater than 50° C. claim 1 , for at least 0.5 hours.8. The method of claim 1 , wherein the aqueous acid has a pKof from 0 to 10.9. The method of claim 8 , wherein the aqueous acid is formic claim 8 , acetic claim 8 , or trichloroacetic acid.10. The method of claim 9 , wherein the aqueous acid is acetic acid.11. The method of claim 1 , wherein the 1-(4-((1R claim 1 ,2S claim 1 ,3R)-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone is isolated by filtering a slurry prepared by concentrating claim 1 , cooling and/or diluting the third mixture with water.12. (canceled)13. The method of claim 1 , wherein ...

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06-06-2013 дата публикации

FUNGICIDAL IMIDAZOLES

Номер: US20130143929A1
Принадлежит: EI DU PONT DE NEMOURS AND COMPANY

Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, 2. A compound of wherein:{'sup': 1', '5a', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R; or a pyridinyl or pyrimidinyl ring optionally substituted with up to 3 substituents independently selected from R;'}{'sup': 2', '5a', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R; or a pyrazolyl, pyridinyl or pyrimidinyl ring optionally substituted with up to 3 substituents independently selected from Ron carbon atom ring members and methyl on the nitrogen atom ring member;'}{'sup': 1', '2, 'sub': 1', '3, 'Rand Rare each independently H, halogen, cyano, C-Calkyl or cyclopropyl;'}{'sup': 3', '6, 'Ris Br, Cl, F, —ORor —SC≡N;'}{'sup': '4', 'Ris H or methyl;'}{'sup': '5a', 'sub': 1', '2', '1', '2', '1', '2', '1', '2, 'each Ris independently halogen, cyano, C-Calkyl, C-Chaloalkyl, cyclopropyl, C-Calkoxy, C-Calkylthio or -T-U—V;'}{'sup': '6', 'sub': 1', '3', '1', '2', '2', '3', '2', '4', '2', '4', '2', '4', '2', '4', '2', '4, 'Ris H, —CH(═O), C-Calkyl, C-Chaloalkyl, C-Calkoxyalkyl, C-Ccyanoalkyl, C-Calkylcarbonyl, C-Calkoxycarbonyl, C-C(alkylthio)carbonyl or C-Calkoxy(thiocarbonyl);'}each T is independently O, NH or a direct bond;{'sub': 1', '3, 'each U is independently C-Calkylene, wherein up to 1 carbon atom is selected from C(═O);'}{'sup': 8a', '8b', '9, 'each V is independently N(R)(R) or OR;'}{'sup': 8a', '8b, 'each Rand Ris independently H or methyl; and'}{'sup': '9', 'each Ris independently H, methyl or halomethyl.'}3. A compound of wherein{'sup': 1', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R;'}{'sup': 2', '5a, 'Qis a phenyl ring substituted with 1 to 3 substituents independently selected from R;'}{'sup': 1', '2, 'sub': 1', '2, 'Rand Rare each independently H, Cl, Br, I or C-Calkyl; and'}{'sup': '5a', 'each Ris independently halogen, cyano, ...

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01-08-2013 дата публикации

COMPOUNDS FOR TREATMENT OF CANCER

Номер: US20130197049A1
Принадлежит:

The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer. 4. The compound of claim 1 , wherein said compound is(4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70a);(4-(4-fluorophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70b);(4-(4-chlorophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70c);(4-(4-bromophenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70d);(4-(4-(trifluoromethyl)phenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70e);(4-p-tolyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70f);(4-(4-methoxyphenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70g);(4-(4-(dimethylamino)phenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70h);(4-(4-hydroxyphenyl)-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70i);(5-methyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70j);(5-ethyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70k);(4-phenyl-5-propyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70l);(1-methyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70m);(1-ethyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70n);(1-benzyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70o); or(1-cyclopentyl-4-phenyl-1H-imidazol-2-yl)(3,4,5-trimethoxyphenyl)methanone (70p).5. A pharmaceutical composition comprising a compound according to and a pharmaceutically acceptable carrier.6. A method of treating claim 1 , suppressing claim 1 , reducing the severity claim 1 , reducing the risk claim 1 , inhibiting cancer comprising administering a compound according to to a subject having cancer under conditions effective to treat the cancer.7. The method of claim 6 , wherein said cancer is selected ...

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19-09-2013 дата публикации

DUAL-ACTING IMIDAZOLE ANTIHYPERTENSIVE AGENTS

Номер: US20130245087A1
Принадлежит:

The invention is directed to compounds having the formula: 125-. (canceled)26. A pharmaceutical composition comprising the compound of and a pharmaceutically acceptable carrier.27. The pharmaceutical composition of further comprising a second therapeutic agent selected from the group consisting of diuretics claim 26 , βadrenergic receptor blockers claim 26 , calcium channel blockers claim 26 , angiotensin-converting enzyme inhibitors claim 26 , ATreceptor antagonists claim 26 , neprilysin inhibitors claim 26 , non-steroidal anti-inflammatory agents claim 26 , prostaglandins claim 26 , anti-lipid agents claim 26 , anti-diabetic agents claim 26 , anti-thrombotic agents claim 26 , renin inhibitors claim 26 , endothelin receptor antagonists claim 26 , endothelin converting enzyme inhibitors claim 26 , aldosterone antagonists claim 26 , angiotensin-converting enzyme/neprilysin inhibitors claim 26 , vasopressin receptor antagonists claim 26 , and combinations thereof.2830-. (canceled)31. A method for causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of hypertension claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .32. A method for causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of heart failure claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .33. A method of causing regression of claim 39 , suppressing claim 39 , or alleviating the symptoms of chronic kidney disease claim 39 , comprising administering to a patient a therapeutically effective amount of a compound of .3438-. (canceled)39. 4′-{4-Cyclopropyl-2-ethoxy-5-[((S)-2-mercapto-4-methylpentanoylamino)-methyl]imidazol-1-ylmethyl}-3′-fluorobiphenyl-2-carboxylic acid claim 39 , or a pharmaceutically acceptable salt thereof. This application claims the benefit of U.S. Provisional Application No. 60/925,931, filed on Apr. 24, 2007; the entire ...

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19-09-2013 дата публикации

AMINE COMPOUND AND USE FOR SAME

Номер: US20130245280A1
Принадлежит: KUREHA CORPORATION

Provided is an ester of 3-[(4-dipropylamino-butyl)(4-{[(1H-imidazole-2-ylmethyl)(1-methyl-1H-imidazole-2-ylmethyl)amino]methyl}benzyl)amino]propionic acid which is easily hydrolyzed in serum. The amine compound of the present invention is an ester compound represented by general formula (1). (In general formula (1), n is 1-4, and Rand Rrepresent an alkyl group having 1-3 carbon atoms.) 2. An amine compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein n in the general formula (1) is 2 or 3.3. An amine compound or a pharmacologically acceptable salt thereof according to claim 2 , wherein n in the general formula (1) is 2 claim 2 , and Rand Rin the general formula (1) represent a methyl group or an ethyl group.4. An amine compound or a pharmacologically acceptable salt thereof according to claim 1 , wherein the amine compound represented by the general formula (1) is 2-dimethylaminoethyl 3-[(4-dipropylaminobutyl)(4-{[(1H-imidazol-2-ylmethyl)(1-methyl-1H-imidazol-2-ylmethyl)amino]methyl}benzyl)amino]propionate.5. An amine compound or a pharmacologically acceptable salt thereof according to claim 4 , wherein the pharmacologically acceptable salt is a citrate of 2-dimethylaminoethyl 3-[(4-dipropylaminobutyl)(4-{[(1H-imidazol-2-ylmethyl)(1-methyl-1H-imidazol-2-ylmethyl)amino]methyl}benzyl)amino]propionate.6. A pharmaceutical composition comprising as an active ingredient the amine compound or the pharmacologically acceptable salt thereof according to .7. A pharmaceutical composition according to claim 1 , comprising as a prodrug the amine compound or the pharmacologically acceptable salt thereof according to .8. A CXCR4 antagonist comprising as an active ingredient the amine compound or the pharmacologically acceptable salt thereof according to .9. An antiviral drug comprising as an active ingredient the amine compound or the pharmacologically acceptable salt thereof according to .10. An anti-rheumatic disease agent based on CXCR4 ...

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31-10-2013 дата публикации

ESTER PRO-DRUGS OF [3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL] METHANOL FOR LOWERING INTRAOCULAR PRESSURE

Номер: US20130289088A1
Принадлежит:

The present invention relates to method of lowering intraocular pressure in a subject in need of such treatment, which comprises administering a therapeutically effective amount of a composition comprising a ester pro-drugs of [3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, of enantiomers thereof, of tautomers thereof, pharmaceutical compositions containing them and their use as pharmaceuticals. 2. The pharmaceutical composition according to claim 1 , wherein the compound having a structure of Formula II is selected from:iso-Butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester;2,2-Dimethyl-propionic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;Acetic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;Benzoic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;3-Methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;3-Phenyl-propionic acid 3-[(S)-1-(1H-imidazol-4-yl)ethyl]-2-methyl-benzyl ester;2-Amino-3-methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester;2-(2-Amino-3-methyl-butyrylamino)-3-methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester;2-(2-Amino-acetylamino)-3-methyl-butyric acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester; and2-Amino-3-phenyl-propionic acid 3-[(S)-1-(1H-imidazol-4-yl)-ethyl]-2-methyl-benzyl ester.3. The pharmaceutical composition according to claim 1 , wherein the buffering agents include: sodium chloride claim 1 , potassium chloride claim 1 , calcium chloride dihydrate claim 1 , magnesium chloride hexahydrate claim 1 , boric acid and sodium borate decahydrate.4. The pharmaceutical composition according to claim 1 , wherein the viscosity building agents include: polyvinyl alcohol claim 1 , polyvinyl pyrrolidone claim 1 , methyl cellulose claim 1 , hydroxypropyl methylcellulose claim 1 , hydroxyethyl cellulose claim 1 , carboxymethyl cellulose and hydroxypropyl cellulose.5. The pharmaceutical ...

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02-01-2014 дата публикации

FAMILY OF POLYAMINE ARYLETHYLAMIDE COMPOUNDS, AND THEIR COSMETIC OR DERMOCOSMETIC USE

Номер: US20140005244A1
Принадлежит: EXSYMOL

The invention relates to a family of stable polyamine arylethylamide compounds, and to the use of these compounds as agents inhibiting DNA damages induced by by-products of the non-enzymatic glycosylation of skin tissues. 2. The compound according to claim 1 , which is selected from the group consisting of N-((4-imidazolyl)ethyl)-α claim 1 ,γ-diaminobutanamide claim 1 , N-((4-imidazolyl)ethyl)-α claim 1 ,β-diamino-propanamide and pharmaceutically acceptable salts of these compounds.3. The compound according to claim 2 , which is N--((4-imidazolyl)ethyl)-α claim 2 ,β-diaminopropanamide or a pharmaceutically acceptable salt thereof.4. A cosmetic or dermocosmetic composition claim 1 , which comprises as main active ingredient a compound as defined in claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with an additive which is physiologically acceptable with skin.5. The composition according to claim 4 , wherein said compound is selected from the group consisting of N-((4-imidazolyl)ethyl)-α claim 4 ,γ-diaminobutanamide claim 4 , N-((4-imidazolyl)-ethyl)-α claim 4 ,β-diaminopropanamide claim 4 , and pharmaceutically acceptable salts of these compounds.6. The composition according to claim 5 , wherein said compound is N-((4-imidazolyl)ethyl)-α claim 5 ,β-diaminopropanamide or a pharmaceutically acceptable salt thereof.7. The composition according to claim 4 , wherein the amount of said compound is comprised between 0.01% and 1% in weight based on the total weight of the composition.8. The composition according to claim 4 , which further comprises one or several additional active ingredients selected from the group consisting of deglycation agents claim 4 , agents that increase the synthesis of collagen or elastin or prevent their degradation claim 4 , agents that increase the synthesis of glycosaminoglycans or proteoglycans or prevent their degradation claim 4 , agents that increase the cell proliferation claim 4 , depigmenting or pro- ...

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09-01-2014 дата публикации

Novel crystals and process of making 5-(-METHYL)-2-METHOXY-BENZOIC ACID

Номер: US20140011851A1
Принадлежит:

The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. 17-. (canceled)8. Form α crystal of 5-({[2-amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.9. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 14.0 claim 8 , 14.3 claim 8 , and 14.7 degrees 2-theta.10. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2 claim 8 , 11.3 claim 8 , 14.0 claim 8 , 14.3 claim 8 , and 14.7 degrees 2-theta.11. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2 claim 8 , 11.3 claim 8 , 11.8 claim 8 , 14.0 claim 8 , 14.3 claim 8 , 14.7 claim 8 , 16.1 claim 8 , and 18.3 degrees 2-theta.12. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 1.13. The α crystal of claim 8 , wherein said crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially similar to the powder X-ray diffraction peaks of .14. The α crystal of claim 8 , wherein said crystal is characterized by a thermal gravimetric analysis (TGA) substantially similar to the TGA in .15. The α crystal of claim 8 , wherein said crystal is characterized by a differential scanning calorimetry (DSC) measurement substantially similar to the DSC in .16. A method of treating a mammal ...

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09-01-2014 дата публикации

POLYETHER COMPOUND AND ELECTROLYTE COMPOSITION

Номер: US20140012012A1
Принадлежит: ZEON CORPORATION

A polyether compound containing oxirane monomer units in an average number per molecule of to , wherein the polyether compound contains repeating units which are represented by the general formula () as at least part of the oxirane monomer units is provided. According to the present invention, it is possible to provide a polymer material which has suitable fluidity and is excellent in ion conductivity. 2. The polyether compound as set forth in wherein claim 1 , in the general formula (2) claim 1 , the anion which is represented by X and is comprised of 2 to 25 atoms is any of OH claim 1 , SCN claim 1 , BF claim 1 , PF claim 1 , ClO claim 1 , (FSO)N claim 1 , (CFSO)N claim 1 , (CFCFSO)N claim 1 , CHSO claim 1 , CFSO claim 1 , CFCOO claim 1 , and PhCOO.3. The polyether compound as set forth in claim 1 , wherein claim 1 , in the repeating units which are expressed by the general formula (1) claim 1 , the ratio of the repeating units which are represented by the general formula (2) is 2 mol % or more.4. The polyether compound as set forth in claim 1 , wherein claim 1 , in the repeating units which are represented by the general formula (1) claim 1 , the units other than the repeating units which are represented by the general formula (2) include at least one unit selected from units where the monovalent group which is represented by A in the general formula (1) is a hydrogen atom claim 1 , units where it is an alkyl group claim 1 , and units where it is a haloalkyl group claim 1 , and units which have the same structure as the repeating units which are represented by the general formula (2) except anions where X is comprised of a single atom.5. An electrolyte composition which contains the polyether compound as set forth in .6. A method of production of the polyether compound as set forth in comprising claim 1 ,a step of ring opening polymerizing a monomer composition which contains epichlorohydrin in the presence of an onium salt of a compound which contains atoms of ...

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23-01-2014 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20140024835A1
Принадлежит: THERAVANCE, INC.

The invention is directed to compounds having the formula: 14-. (canceled)5. The process of claim 33 , wherein Ris selected from —COOH claim 33 , —SONHR claim 33 , and tetrazol-5-yl.6. (canceled)7. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —N— claim 33 , Q is —N— and W is a bond.8. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —CH— claim 33 , Q is —C(R)— and W is —C(O)—.9. The process of claim 33 , wherein Y represents —N— claim 33 , Z is —C(R)— claim 33 , Q is —C(R)— and W is a bond.10. The process of claim 33 , wherein Y represents —C(R)— claim 33 , Z is —CH— claim 33 , Q is —N— and W is a bond.11. The process of claim 33 , wherein Ris selected from H claim 33 , halo claim 33 , —Calkyl claim 33 , —Ccycloalkyl claim 33 , and —Calkylene-OR.12. The process of claim 33 , wherein Ris selected from —Calkyl and —Calkylene-O—Calkylene-R claim 33 , where Ris —Calkyl.1314-. (canceled)15. The process of claim 33 , wherein X is selected from: —C(O)NH—; —CH—NHC(O)—; —C(O)NH—CH—; —C(O)NH—NHC(O)—; —CH═C(—CH-2-thiophene)-C(O)NH—; —(CH)—NHC(O)—; —C(O)NH—CH—CH(COOH)—CH—; —C(O)NH—CH(benzyl)-CH—NHC(O)—; —C(O)NH—CH(benzyl)-CH—C(O)NH—; —CH—NHC(O)—CH—NHC(O)—; —CH—NHC(O)-cyclohexylene-NHC(O)—; —CH—N(OH)C(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—CH—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—C(O)N(OH)—CH—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; and —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—.16. The process of claim 15 , wherein X is selected from ...

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06-02-2014 дата публикации

NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS

Номер: US20140039024A1
Принадлежит:

The present invention is directed to novel opioid receptor modulators of Formula (I). 6. The method according to claim 1 , comprising administering to the subject a therapeutically effective amount of a pharmaceutically acceptable salt of said compound.7. The method according to claim 6 , wherein the salt is a hydrochloric claim 6 , hydrobromic claim 6 , hydriodic claim 6 , perchloric claim 6 , sulfuric claim 6 , nitric claim 6 , phosphoric claim 6 , acetic claim 6 , propionic claim 6 , glycolic claim 6 , lactic claim 6 , succinic claim 6 , maleic claim 6 , fumaric claim 6 , malic claim 6 , tartaric claim 6 , citric claim 6 , benzoic claim 6 , mandelic claim 6 , methanesulfonic claim 6 , hydroxyethanesulfonic claim 6 , benzenesulfonic claim 6 , oxalic claim 6 , pamoic claim 6 , 2-naphthalenesulfonic claim 6 , p-toluenesulfonic claim 6 , cyclohexanesulfamic claim 6 , salicylic claim 6 , saccharinic claim 6 , or trifluoroacetic acid salt.8. The method according to claim 6 , wherein the salt is a benzathine claim 6 , chloroprocaine claim 6 , choline claim 6 , diethanolamine claim 6 , ethylenediamine claim 6 , meglumine claim 6 , procaine claim 6 , aluminum claim 6 , calcium claim 6 , lithium claim 6 , magnesium claim 6 , potassium claim 6 , sodium claim 6 , or zinc salt.9. The method according to claim 1 , wherein the chronic pain is selected from the group consisting of neuropathic pain conditions claim 1 , diabetic peripheral neuropathy claim 1 , post-herpetic neuralgia claim 1 , trigeminal neuralgia claim 1 , post-stroke pain syndromes and cluster or migraine headaches.10. The method of claim 1 , wherein the method is for treating centrally mediated pain.11. The method according to claim 1 , wherein the method is for treating peripherally mediated pain.12. The method according to claim 1 , wherein the method is for treating structural or soft tissue injury related pain.13. The method according to claim 1 , wherein the method is for treating pain related to ...

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06-02-2014 дата публикации

Substituted Imidazole Derivatives and Methods of Use Thereof

Номер: US20140039025A1
Принадлежит: TransTech Pharma, Inc.

The present invention provides imidazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof. 2. The method of claim 1 , wherein the compound is (R)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.3. The method of claim 1 , wherein the compound is (R)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.4. The method of claim 1 , wherein the compound is (S)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.5. The method of claim 1 , wherein the compound is (S)-1-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.6. The method of claim 1 , wherein the compound is (R)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.7. The method of claim 1 , wherein the compound is (S)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-dimethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.8. The method of claim 1 , wherein the compound is (R)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.9. The method of claim 1 , wherein the compound is (S)-1-(4-{1-[4-(4-chloro-phenoxy)-phenyl]-2-ethoxymethyl-1H-imidazol-4-yl}-phenoxy)-3-diethylamino-propan-2-ol or a pharmaceutically acceptable salt thereof.10. The method of claim 1 , wherein the disease or condition is Alzheimer's Disease.11. The method of claim 1 , wherein the disease or condition is sepsis.12. The method of claim 1 , wherein the disease or condition is diabetes.13. The method of ...

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05-01-2017 дата публикации

Processes for the Synthesis of Substituted Urea Compounds

Номер: US20170001962A1
Принадлежит: Bial-Portela & CA, S.A.

The present invention concerns a process for preparing a compound having the Formula A: 2. The process according to claim 1 , wherein the oxidation of the derivative of R5 and R6 employs an inorganic acid.3. The process according to claim 2 , wherein the inorganic acid is HX claim 2 , where X is a halogen atom.4. The process according to claim 3 , wherein the inorganic acid is HCl or HBr.5. The process according to any preceding claim claim 3 , wherein DMSO is used as a solvent and oxidising agent in the oxidation of the derivative of R5 and R6.6. The process according to any preceding claim claim 3 , wherein R1 is selected from H and Calkyl.7. The process according to claim 6 , wherein R1 is selected from H claim 6 , methyl and ethyl.8. The process according to any preceding claim claim 6 , wherein R2 is selected from aryl claim 6 , heteroaryl claim 6 , heterocyclyl claim 6 , Ccycloalkyl claim 6 , aryl Calkyl claim 6 , heteroaryl Calkyl claim 6 , heterocyclyl Calkyl and Ccycloalkyl Calkyl claim 6 , each of which may be substituted or unsubstituted.9. The process according to claim 8 , wherein R2 is selected from aryl claim 8 , heteroaryl claim 8 , heterocyclyl claim 8 , and Ccycloalkyl each of which may be substituted or unsubstituted.10. The process according to or claim 8 , wherein R2 is selected from fully saturated heterocyclyl claim 8 , and Ccycloalkyl each of which are monocyclic and may be substituted or unsubstituted.11. The process according to claim 10 , wherein R2 is an unsubstituted cyclopentyl or unsubstituted cyclohexyl.12. The process according to claim 10 , wherein R2 is a fully saturated heterocyclyl claim 10 , and wherein the heterocyclyl ring contains a single heteroatom claim 10 , such as nitrogen or oxygen.13. The process according to claim 12 , wherein the heterocyclyl is six membered and the heteroatom in the said heterocyclyl group is at the 4-position relative to the position of attachment of the heterocyclyl group R2 to the urea nitrogen. ...

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25-01-2018 дата публикации

PRODUCTION METHOD FOR INCLUSION COMPOUND

Номер: US20180022675A1
Автор: HOSHI Eiji, Ono Kazuo
Принадлежит: NIPPON SODA CO., LTD.

A method for producing a thermodynamically more stable clathrate compound including at least one compound selected from the group consisting of 1,1,2,2-tetrakis(4-hydroxyphenyl)ethane, 5-hydroxyisophthalic acid, and 5-nitroisophthalic acid as a host compound and an imidazole compound as a guest compound. The method for producing a clathrate compound includes: a mixing step of mixing a mixed solvent including a protic solvent, at least one compound selected from the group consisting of 1,1,2,2-tetrakis(4-hydroxyphenyl)ethane, 5-hydroxyisophthalic acid and 5-nitroisophthalic acid, and an imidazole compound; and a heating step. 3. The method for producing a clathrate compound according to claim 1 , wherein the mixed solvent comprises a first solvent which is at least one solvent selected from the group consisting of water and methanol and a second solvent which is at least one solvent selected from the group consisting of an alcoholic solvent claim 1 , an ester-based solvent claim 1 , a ketone-based solvent claim 1 , an aliphatic hydrocarbon-based solvent claim 1 , and an aromatic hydrocarbon-based solvent claim 1 , the second solvent being a solvent different from the first solvent.4. The method for producing a clathrate compound according to claim 1 , wherein the imidazole compound represented by formula (I) is 2-phenyl-4-methyl-5-hydroxymethylimidazole or 2-ethyl-4-methylimidazole.5. The method for producing a clathrate compound according to claim 2 , wherein the mixed solvent comprises a first solvent which is at least one solvent selected from the group consisting of water and methanol and a second solvent which is at least one solvent selected from the group consisting of an alcoholic solvent claim 2 , an ester-based solvent claim 2 , a ketone-based solvent claim 2 , an aliphatic hydrocarbon-based solvent claim 2 , and an aromatic hydrocarbon-based solvent claim 2 , the second solvent being a solvent different from the first solvent.6. The method for producing a ...

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25-01-2018 дата публикации

PROCESSES FOR PREPARING ASK1 INHIBITORS

Номер: US20180022708A1
Принадлежит:

The present disclosure provides processes for the preparation of a compound of formula: 2. The method of claim 1 , wherein the reaction conditions of step (a) comprise a base.3. The method of claim 1 , wherein the reaction conditions of step (a) comprise a solvent selected from the group consisting of tetrahydrofuran claim 1 , 2-methyltetrahydrofuran claim 1 , methyl-tert-butyl ether claim 1 , and diethyl ether.4. The method of claim 1 , wherein the reaction conditions of step (a) comprise a first temperature of about −20° C. to about 40° C. and a second temperature of about −10° C. to about 50° C.5. The method of claim 1 , wherein the reaction conditions of step (b) comprise a chlorinating reagent.6. The method of claim 1 , wherein the reaction conditions of step (b) comprise a solvent selected from the group consisting of dichloromethane claim 1 , acetonitrile claim 1 , tetrahydrofuran claim 1 , methyl-tert-butyl ether claim 1 , and chloroform.7. The method of claim 1 , wherein the reaction conditions of step (b) comprise a temperature of about −20° C. to about 40° C.8. The method of claim 1 , wherein the reaction conditions of step (c) comprise an organic base.9. The method of claim 1 , wherein the reaction conditions of step (c) comprise a solvent selected from the group consisting of dichloromethane claim 1 , dichloroethane claim 1 , acetonitrile claim 1 , tetrahydrofuran claim 1 , 2-methyltetrahydrofuran claim 1 , toluene claim 1 , methyl-tert-butyl ether claim 1 , and chloroform.10. The method of claim 1 , wherein the reaction conditions of step (c) comprise a temperature of about 0° C. to about 40° C.11152.-. (canceled) This Application is a Division of application Ser. No. 15/413,154 filed on Jan. 23, 2017. Application Ser. No. 15/413,154 is a Division of application Ser. No. 14/757,663 filed on Dec. 22, 2015. Application Ser. No. 14/757,663 claims the benefit of U.S. Provisional Application 62/269,064 filed on Dec. 17, 2015. Application Ser. No. 14/757,663 ...

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01-02-2018 дата публикации

Process for the preparation of intermediates useful in the synthesis of eluxadoline

Номер: US20180029994A1
Принадлежит: Allergan Holdings ULC

The invention relates to an improved process for preparing [(S)-1-(4-phenyl-1-H-imidazol-2-yl)-ethyl]-amine. The process involves formation of the novel intermediate crystalline compound [(S)-1-(4-phenyl-1-H-imidazol-2-yl)-ethyl]-carbamic acid tert-butyl ester oxalate.

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30-01-2020 дата публикации

NOVEL 5-SUBSTITUTED IMIDAZOLYLMETHYL DERIVATIVES

Номер: US20200031778A1
Принадлежит:

The present invention relates to novel 5-substituted imidazolylmethyl derivatives, to processes for preparing these compounds, to compositions and mixtures comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. 4. Imidazole derivative of formula (I) according to claim 1 , wherein{'sup': 2', '2a', '2a, 'sub': 1', '3', '1', '3', '1', '3', '1', '3', '3', '8', '3', '8', '1', '8', '1', '8', '1', '8, 'Rrepresents —OR, wherein Rrepresents H, C-C-alkyl, C-C-cyanoalkyl, C-C-alkoxy-C-C-alkyl, C-C-alkenyl, C-C-alkynyl, —C(O)N-di-C-C-alkyl, or halogen- or C-C-alkoxy-substituted or non-substituted —C(O)—C-C-alkyl;'}And/or a salt and/or N-oxide thereof,5. Imidazole derivative of formula (I) according to claim 1 , wherein{'sup': '3', 'sub': 2', '4', '1', '4', '1', '4', '1-4', '1', '4', '3', '7', '3', '7', '2', '2', '1-4', '1-4', '1', '4', '1-4', '1-4', '1-4', '1', '8', '1', '8', '1', '8', '1', '8, 'Rrepresents halogen, cyano, carboxaldehyde, hydroxycarbonyl, C-C-alkyl, C-C-haloalkyl, C-C-cyanoalkyl, C-alkyloxy, C-C-haloalkyloxy, C-C-cycloalkyl, C-C-halocycloalkyl, C-05-alkenyl, C-05-alkynyl, C-alkylsulfanyl, C-haloalkylsulfanyl, C-C-alkylcarbonyl, C-haloalkylcarbonyl, carbamoyl, aminothiocarbonyl, C-alkoxycarbonyl, C-haloalkoxycarbonyl, benzyl, phenyl, furyl, pyrrolyl, thienyl, pyridyl, benzyloxy, or phenyloxy, wherein the benzyl, phenyl, 5-membered heteroaryl, 6-membered heteroaryl, benzyloxy or phenyloxy may be optionally substituted by one or more group(s) selected from halogen, C-C-alkyl, C-C-haloalkyl, C-C-alkyloxy, C-C-haloalkyloxy; optionally represents fluorine, chlorine, bromine, iodine, cyano, hydroxycarbonyl, carboxaldehyde, trifluoromethyl, cyanomethyl, methoxy, methylsulfanyl, cyclopropyl, ethinyl, methylcarbonyl (acetyl), carboxyl, aminothiocarbonyl, methoxycarbonyl, ethoxycarbonyl, phenyl, or 2-thienyl, ...

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02-03-2017 дата публикации

ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF

Номер: US20170057926A1
Принадлежит: EPIZYME, INC.

Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. 1174-. (canceled)176. A pharmaceutical composition comprising a compound of claim 175 , or a pharmaceutically acceptable salt thereof claim 175 , and a pharmaceutically acceptable excipient.177. A kit or packaged pharmaceutical comprising a compound of claim 175 , or a pharmaceutically acceptable salt thereof claim 175 , and instructions for use thereof.178. A method of inhibiting an arginine methyltransferase (RMT) comprising contacting a cell with an effective amount of a compound of claim 175 , or a pharmaceutically acceptable salt thereof.179. A method of modulating gene expression comprising contacting a cell with an effective amount of a compound of claim 175 , or a pharmaceutically acceptable salt thereof.180. A method of modulating transcription comprising contacting a cell with an effective amount of a compound of claim 175 , or a pharmaceutically acceptable salt thereof.181. A method of treating an RMT-mediated disorder claim 175 , comprising administering to a subject in need thereof a therapeutically effective amount of a compound of claim 175 , or a pharmaceutically acceptable salt thereof.182. The method of claim 181 , wherein the disorder is a proliferative disorder claim 181 , a neurological disorder claim 181 , a muscular dystrophy claim 181 , an autoimmune disorder claim 181 , or a vascular disorder.183. The method of claim 182 , wherein the proliferative disorder is cancer.184. The method of claim 182 , wherein the neurological disorder is amyotrophic lateral sclerosis. The present application claims priority under 35 U.S.C §119(e) to U.S. Provisional Patent Application Ser. No. 61/781,054, filed Mar. 14, 2013, the entire ...

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05-03-2015 дата публикации

DUAL-ACTING ANTIHYPERTENSIVE AGENTS

Номер: US20150065543A1
Принадлежит: THERAVANCE BIOPHARMA R&D IP, LLC

The invention is directed to compounds having the formula: 12-. (canceled)5. The method of claim 4 , wherein Ris selected from —COOH claim 4 , —SONHR claim 4 , and tetrazol-5-yl.7. The method of claim 36 , wherein Y represents —C(R)— claim 36 , Z is —N— claim 36 , Q is —N— and W is a bond.8. The method of claim 36 , wherein Y represents —C(R)— claim 36 , Z is —CH— claim 36 , Q is —C(R)— and W is —C(O)—.9. The method of claim 36 , wherein Y represents —N— claim 36 , Z is —C(R)— claim 36 , Q is —C(R)— and W is a bond.10. The method of claim 36 , wherein Y represents —C(R)— claim 36 , Z is —CH— claim 36 , Q is —N— and W is a bond.11. The method of claim 36 , wherein Ris selected from H claim 36 , halo claim 36 , —Calkyl claim 36 , —Ccycloalkyl claim 36 , and —Calkylene-OR.12. The method of claim 36 , wherein Ris selected from —Calkyl and —Calkylene-O—Calkylene-R claim 36 , where Ris —Calkyl.13. The method of claim 12 , wherein Ris selected from —Calkyl and —O—Calkyl.14. The method of claim 36 , wherein X is —Calkylene- claim 36 , 1 to 4 —CH— moieties in the alkylene are replaced with a —NR—C(O)— or —C(O)—NR— moiety claim 36 , and Ris selected from H and —OH.15. The method of wherein X is selected from: —C(O)NH—; —CH—NHC(O)—; —C(O)NH—CH—; —C(O)NH—NHC(O)—; —CH═C(—CH-2-thiophene)-C(O)NH—; —(CH)—NHC(O)—; —C(O)NH—CH—CH(COOH)—CH—; —C(O)NH—CH(benzyl)-CH—NHC(O)—; —C(O)NH—CH(benzyl)-CH—C(O)NH—; —CH—NHC(O)—CH—NHC(O)—; —CH—NHC(O)-cyclohexylene-NHC(O)—; —CH—N(OH)C(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—CH—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—C(O)N(OH)—CH—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—; —CH—NHC(O)—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)—; —C(O)NH—(CH)—CH(COOH)—NHC(O)—; —CH—NHC(O)—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —CH—C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; —C(O)NH—(CH)—NHC(O)—CH—NHC(O)—; —C(O)NH—(CH)—NHC(O)-cyclohexylene-NHC(O)—; ...

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19-03-2015 дата публикации

PHARMACEUTICAL COMPOSITIONS COMPRISING (3-(1-(1H-IMIDAZOL-4-YL)ETHYL)-2-METHYLPHENYL)METHANOL

Номер: US20150080445A1
Автор: Gil Daniel W.
Принадлежит:

Disclosed herein is a pharmaceutical composition comprising (3-(1-(1H-imidazol-4-yl)ethyl)-2-methylphenyl)methanol and methods of using the composition to treat chronic pain. 412-. (canceled)13. The pharmaceutical composition of claim 1 , wherein the ester is an alkyl ester.14. The pharmaceutical composition of claim 2 , wherein the ester is an alkyl ester.15. The pharmaceutical composition of claim 3 , wherein the ester is an alkyl ester.16. The pharmaceutical composition of claim 1 , wherein the ester is a Calkyl ester.17. The pharmaceutical composition of claim 2 , wherein the ester is a Calkyl ester.18. The pharmaceutical composition of claim 3 , wherein the ester is a Calkyl ester.19. The pharmaceutical composition of claim 16 , wherein the alkyl part of the ester is selected from the group consisting of methyl claim 16 , ethyl claim 16 , propyl claim 16 , isopropyl claim 16 , n-butyl claim 16 , sec-butyl claim 16 , iso-butyl claim 16 , t-butyl claim 16 , pentyl isomers claim 16 , hexyl isomers claim 16 , cyclopropyl claim 16 , cyclobutyl claim 16 , cyclopentyl and cyclohexyl.20. The pharmaceutical composition of claim 17 , wherein the alkyl part of the ester is selected from the group consisting of methyl claim 17 , ethyl claim 17 , propyl claim 17 , isopropyl claim 17 , n-butyl claim 17 , sec-butyl claim 17 , iso-butyl claim 17 , t-butyl claim 17 , pentyl isomers claim 17 , hexyl isomers claim 17 , cyclopropyl claim 17 , cyclobutyl claim 17 , cyclopentyl and cyclohexyl.21. The pharmaceutical composition of claim 18 , wherein the alkyl part of the ester is selected from the group consisting of methyl claim 18 , ethyl claim 18 , propyl claim 18 , isopropyl claim 18 , n-butyl claim 18 , sec-butyl claim 18 , iso-butyl claim 18 , t-butyl claim 18 , pentyl isomers claim 18 , hexyl isomers claim 18 , cyclopropyl claim 18 , cyclobutyl claim 18 , cyclopentyl and cyclohexyl. This application is a continuation of, and claims priority to, U.S. patent application Ser. No. ...

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12-06-2014 дата публикации

LXR MODULATORS

Номер: US20140163081A1
Принадлежит:

Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 1. A compound , isotope , or pharmaceutically acceptable salt thereof , which is 2-(1-(3′-fluoro-4′-(hydroxymethyl)-5′-(methylsulfonyl)biphenyl-4-yl)-2-(2-(2-fluorophenyl)propan-2-yl)-1H-imidazol-4-yl)propan-2-ol.2. A pharmaceutical composition comprising a compound claim 1 , or pharmaceutically acceptable salt thereof of claim 1 , and one or more pharmaceutically acceptable carriers.3. A method of treating a disease or disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound claim 1 , or pharmaceutically acceptable salt thereof of claim 1 , wherein the disease or disorder is atherosclerosis claim 1 , insulin resistance claim 1 , osteoarthritis claim 1 , stroke claim 1 , hyperglycemia claim 1 , dyslipidemia claim 1 , psoriasis claim 1 , age and UV exposure-related skin wrinkling claim 1 , diabetes claim 1 , cancer claim 1 , Alzheimer's disease claim 1 , inflammation claim 1 , immunological disorders claim 1 , lipid disorders claim 1 , obesity claim 1 , macular degeneration claim 1 , conditions characterized by a perturbed epidermal barrier function claim 1 , conditions of disturbed differentiation or excess proliferation of the epidermis or mucous membrane claim 1 , or cardiovascular disorders.4. The method of wherein the disease or disorder is atherosclerosis claim 3 , diabetes claim 3 , Alzheimer's disease or dyslipidemia.5. The method of wherein the disease or disorder is atherosclerosis.6. The method of wherein the disease or disorder is diabetes.7. The method of wherein the disease or disorder is Alzheimer's disease. This application is a Continuation of U.S. patent application Ser. No. 13/319,937 filed Nov. 30, 2011, ...

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12-03-2020 дата публикации

Crystalline Form of Eluxadoline

Номер: US20200079740A1
Принадлежит:

The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D). 1. A solid pharmaceutical composition comprising a crystalline form of Eluxadoline that is a co-crystal of Eluxadoline and methyl nicotinate characterized by a PXRD diffractogram comprising peaks , expressed in degrees 2θ (±0.2°) , at 6.4° , 6.9° , and 11.4° , and one or more pharmaceutically acceptable excipients.2. The pharmaceutical composition of claim 1 , wherein the crystalline form of Eluxadoline further comprises at least three peaks claim 1 , expressed in degrees 2θ (±0.2°) claim 1 , selected from the group consisting of: 8.7° claim 1 , 9.9° claim 1 , 12.7° claim 1 , 14.8° claim 1 , 15.8° claim 1 , 17.5° claim 1 , 18.9° claim 1 , 19.8° claim 1 , and 23.8°.3. The pharmaceutical composition of claim 1 , wherein the crystalline form of Eluxadoline further comprises peaks claim 1 , expressed in degrees 2θ (±0.2°) claim 1 , at 8.7° claim 1 , 9.9° claim 1 , 12.7° claim 1 , 14.8° claim 1 , 15.8° claim 1 , 17.5° claim 1 , 18.9° claim 1 , 19.8° claim 1 , and 23.8°.4. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is in the form of a solid dosage form.5. The pharmaceutical composition of claim 4 , wherein the pharmaceutical composition is a tablet.6. The pharmaceutical composition of claim 1 , wherein a molar ratio of Eluxadoline to methyl nicotinate in the crystalline form is between approximately 1:0.5 and approximately 1:1.5.7. The pharmaceutical composition of claim 1 , wherein a molar ratio of Eluxadoline to methyl nicotinate in the crystalline form is approximately 1:1.8. The pharmaceutical composition of claim 5 , wherein the co-crystal of ...

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29-03-2018 дата публикации

Novel 5-substituted imidazole derivatives

Номер: US20180084780A1
Принадлежит:

The present invention relates to novel 5-substituted imidazolylmethyl derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. 5. Method for controlling harmful microorganisms in crop protection and in the protection of one or more materials claim 1 , comprising applying a compound of the formula (I) and/or a salt and/or N-oxide thereof according to to the harmful microorganisms and/or a habitat thereof.6. Method for controlling phytopathogenic harmful fungi in crop protection and in the protection of one or more materials claim 1 , comprising applying a compound of the formula (I) and/or a salt and/or N-oxide thereof according to to the phytopathogenic harmful fungi and/or a habitat thereof.7. Composition for controlling harmful microorganisms claim 1 , optionally for controlling phytopathogenic harmful fungi claim 1 , comprising a content of at least one compound of the formula (I) and/or a salt and/or N-oxide thereof according to claim 1 , in addition to one or more extenders and/or surfactants.8. Composition according to comprising at least one further active ingredient selected from the group consisting of insecticides claim 7 , attractants claim 7 , sterilants claim 7 , bactericides claim 7 , acaricides claim 7 , nematicides claim 7 , fungicides claim 7 , growth regulators claim 7 , herbicides claim 7 , fertilizers claim 7 , safeners and semiochemicals.9. A product comprising a compound of the formula (I) and/or a salt and/or N-oxide thereof according to for control of harmful microorganisms claim 1 , optionally phytopathogenic harmful fungi claim 1 , in crop protection and/or for protection of one or more materials.10. Process for producing a composition for controlling harmful microorganisms claim 1 , optionally for ...

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21-03-2019 дата публикации

NOVEL 5-SUBSTITUTED IMIDAZOLE DERIVATIVES

Номер: US20190082691A1
Принадлежит:

The present invention relates to novel 5-substituted imidazolylmethyl derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. 2. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'sub': 1', '8', '1', '8', '2', '7', '2', '7', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '7, 'Rrepresents in each case optionally branched C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-haloalkenyl, or optionally halogen-, cyano-, C-C-alkyl-, C-C-haloalkyl-, C-C-alkoxy-, C-C-haloalkoxy-, C-C-alkylthio- or C-C-haloalkylthio-substituted C-C-cycloalkyl.'}3. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'sub': 1', '4', '1', '4', '2', '5', '2', '5', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '6, 'Rrepresents in each case optionally branched C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-haloalkenyl, or optionally halogen-, cyano-, C-C-alkyl-, C-C-haloalkyl-, C-C-haloalkoxy-, C-C-alkoxy-, C-C-alkylthio- or C-C-haloalkylthio-substituted C-C-cycloalkyl.'}4. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'sub': 1', '4', '1', '4', '1', '4, 'Rrepresents tert-butyl, isopropyl, 1-halocyclopropyl, 1-(C-C-alkyl)cyclopropyl, 1-(C-C-alkoxy)cyclopropyl or 1-(C-C-alkylthio)cyclopropyl.'}5. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'Rrepresents tert-butyl, isopropyl, 1-chlorocyclopropyl, 1-fluorocyclopropyl or 1-methylcyclopropyl.'}6. A compound of formula (XVII) and/or a salt and/or N-oxide thereof according to claim 1 , wherein{'sup': '1', 'Rrepresents 1-chlorocyclopropyl or 1-fluorocyclopropyl ...

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29-03-2018 дата публикации

THERAPEUTIC COMPOUNDS AND FORMULATIONS FOR INTRANASAL DELIVERY

Номер: US20180085306A1
Принадлежит: Regents of the University of Minnesota

Certain embodiments of the invention provide a formulation suitable for nasal administration comprising water, a prodrug of a therapeutic agent, and an enzyme that is suitable for intranasal conversion of the prodrug to the therapeutic agent, as well as methods of use thereof. 1. A formulation suitable for nasal administration comprising: water , a prodrug of a therapeutic agent , and an enzyme that is suitable for intranasal conversion of the prodrug to the therapeutic agent , wherein the therapeutic agent is midazolam or a precursor of midazolam.2. The formulation of claim 1 , wherein the formulation is significantly free of surfactants or organic solubilizing agents.3. The formulation of claim 1 , wherein the prodrug comprises a prodrug moiety that increases the water solubility of the therapeutic agent.4. The formulation of claim 3 , wherein the prodrug comprises a lysine moiety.7. The formulation of claim 1 , wherein the enzyme is selected from an esterase claim 1 , an amidase claim 1 , a protease claim 1 , a proteinase claim 1 , and an aminopeptidase.8. The formulation of claim 1 , wherein the enzyme is a fungal protease.9Aspergillus Orizae. The formulation of claim 8 , wherein the fungal protease is from (O.A.) (e.g. claim 8 , EC 3.4.21.63).10. The formulation of claim 1 , wherein the enzyme is a human aminopeptidase.11. The formulation of wherein the enzyme is EC 3.4.11.6.12. The formulation of claim 1 , wherein the ratio of the prodrug to the enzyme ranges between about 0.1 mM (prodrug)/1 U/ml (enzyme) to about 10 mM (prodrug)/1 U/ml (enzyme).13. A kit comprising a) a prodrug of a therapeutic agent in an aqueous solution; b) an enzyme; and c) instructions for concurrent intranasal administration of the prodrug and the enzyme claim 1 , wherein the therapeutic agent is midazolam or a precursor of midazolam.14. A method of delivering midazolam to an animal claim 1 , comprising intranasally administering to the animal a formulation as described in .15. ( ...

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09-04-2015 дата публикации

Novel crystals and process of making 5-(-methyl)-2-methoxy-benzoic acid

Номер: US20150099724A1
Принадлежит:

The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. 1. (canceled)2. A pharmaceutical composition comprising a Form α crystal of 5-({[2-amino-3-(4-carbamoyl-2 ,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.3. The pharmaceutical composition of claim 2 , wherein said Form α crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 14.0 claim 2 , 14.3 claim 2 , and 14.7 degrees 2-theta.4. The pharmaceutical composition of claim 2 , wherein said Form α crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2 claim 2 , 11.3 claim 2 , 14.0 claim 2 , 14.3 claim 2 , and 14.7 degrees 2-theta.5. The pharmaceutical composition of claim 2 , wherein said Form α crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks at about 10.2 claim 2 , 11.3 claim 2 , 11.8 claim 2 , 14.0 claim 2 , 14.3 claim 2 , 14.7 claim 2 , 16.1 claim 2 , and 18.3 degrees 2-theta.6. The pharmaceutical composition of claim 2 , wherein said Form α crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially as shown in Table 1.7. The pharmaceutical composition of claim 2 , wherein said Form α crystal is characterized by a powder X-ray diffraction pattern having powder X-ray diffraction peaks substantially similar to the powder X ray diffraction peaks of .8. The pharmaceutical composition of claim 2 , wherein said Form α crystal is characterized by a thermal gravimetric analysis (TGA) substantially similar to the TGA in .9. The ...

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28-03-2019 дата публикации

Crystalline Form of Eluxadoline

Номер: US20190092734A1
Принадлежит:

The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D). 1. A crystalline form of Eluxadoline that is a co-crystal of Eluxadoline and methyl nicotinate.2. The co-crystal of claim 1 , wherein the molar ratio of Eluxadoline to methyl nicotinate is between approximately 1:0.5 and approximately 1:1.5.3. The co-crystal of claim 1 , wherein the molar ratio of Eluxadoline to methyl nicotinate is approximately 1:1.4. A crystalline form of Eluxadoline that is a co-crystal of Eluxadoline and methyl nicotinate characterized by a PXRD diffractogram comprising peaks claim 1 , expressed in degrees 2θ (±0.2°) claim 1 , at 6.4° claim 1 , 6.9° and 11.4°.5. The co-crystal of claim 4 , further comprising at least three peaks claim 4 , expressed in degrees 2θ (±0.2°) claim 4 , selected from the group consisting of: 8.7° claim 4 , 9.9° claim 4 , 12.7° claim 4 , 14.8° claim 4 , 15.8° claim 4 , 17.5° claim 4 , 18.9° claim 4 , 19.8° and 23.8°.6. The co-crystal of claim 4 , further comprising peaks claim 4 , expressed in degrees 2θ (±0.2°) claim 4 , at 8.7° claim 4 , 9.9° claim 4 , 12.7° claim 4 , 14.8° claim 4 , 15.8° claim 4 , 17.5° claim 4 , 18.9° claim 4 , 19.8° and 23.8°.7. The co-crystal of claim 4 , providing a PXRD diffractogram substantially the same in appearance as the PXRD diffractogram provided in .8. The co-crystal of claim 4 , wherein the molar ratio of Eluxadoline to methyl nicotinate is approximately 1:1.9. A pharmaceutical composition comprising a crystalline form of Eluxadoline that is a co-crystal of Eluxadoline and methyl nicotinate characterized by a PXRD diffractogram comprising peaks claim 4 , expressed in degrees 2θ (±0.2°) claim 4 , at ...

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06-04-2017 дата публикации

IMIDAZOLE DERIVATIVES AS FORMYL PEPTIDE RECEPTOR MODULATORS

Номер: US20170096401A1
Принадлежит:

The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor. 4. The compound of claim 3 , wherein Ris H claim 3 , ORor NRR.5. The compound of claim 1 , wherein:m is 0;n is 0; and{'sup': '8', 'Ris H.'}6. The compound of claim 1 , wherein:m is 1;n is 1;{'sup': 8', '9', '9, 'sub': '1-8', 'Ris OR, wherein Ris H or unsubstituted Calkyl;'}{'sup': '18', 'sub': '1-8', 'Ris H or unsubstituted Calkyl; and'}{'sup': '19', 'Ris H.'}7. The compound of claim 1 , wherein:m is 1;n is 2;{'sup': 8', '10', '11', '10', '11, 'sub': 1-8', '1-8, 'Ris NRR, wherein Ris H or unsubstituted Calkyl, and Ris H or optionally substituted Calkyl;'}{'sup': '18', 'each Ris H; and'}{'sup': '19', 'each Ris H.'}8. The compound of claim 1 , wherein:m is 1;n is 2;{'sup': 8', '9', '9, 'sub': '1-8', 'Ris OR, wherein Ris H or unsubstituted Calkyl;'}{'sup': '18', 'each Ris H; and'}{'sup': '19', 'each Ris H.'}9. The compound of claim 1 , wherein:m is 0;n is 2;{'sup': 8', '9', '9, 'Ris OR, wherein Ris H;'}{'sup': '18', 'each Ris H; and'}{'sup': '19', 'each Ris H.'}11. A pharmaceutical composition comprising as active ingredient a therapeutically effective amount of a compound according to and a pharmaceutically acceptable adjuvant claim 1 , diluent or carrier.12. The pharmaceutical composition of claim 1 , comprising as active ingredient a therapeutically effective amount of a compound of .13. A method of treating a disease or condition associated with modulation of FPR2 in a subject in need thereof claim 1 , the method comprising administering a therapeutically effective amount of a compound of or a pharmaceutical composition of or to the subject claim 1 , thereby treating the disease or condition.14. The method of claim 13 , wherein the disease or condition is dry eye.15. The method of claim 13 , wherein the disease or condition is post-surgical inflammation.16. ...

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13-04-2017 дата публикации

UREA COMPOUNDS AND THEIR USE AS ENZYME INHIBITORS

Номер: US20170101381A1
Принадлежит:

A compound having the following structure: 2. A pharmaceutical composition comprising a compound according to claim 1 , together with one or more pharmaceutically acceptable excipients.3. The pharmaceutical composition of claim 2 , further comprising one or more additional active pharmaceutical ingredients claim 2 , such as anandamide claim 2 , oleoyl ethanolamide or palmitoyl ethanolamide.4. A method of treatment or prevention of a condition whose development or symptoms are linked to a substrate of the FAAH enzyme claim 1 , the method comprising the administration claim 1 , to a subject in need of such treatment or prevention claim 1 , of a therapeutically effective amount of a compound according to .5. A method according to claim 4 , wherein the condition is a disorder associated with the endocannabinoid system.6. A method according to claim 5 , wherein the disorder is selected from appetite regulation claim 5 , obesity claim 5 , metabolic disorders claim 5 , cachexia claim 5 , anorexia claim 5 , pain claim 5 , inflammation claim 5 , neurotoxicity claim 5 , neurotrauma claim 5 , stroke claim 5 , multiple sclerosis claim 5 , spinal cord injury claim 5 , Parkinson's disease claim 5 , levodopa-induced dyskinesia claim 5 , Huntington's disease claim 5 , Gilles de la Tourette's syndrome claim 5 , tardive dyskinesia claim 5 , dystonia claim 5 , amyotrophic lateral sclerosis claim 5 , Alzheimer's disease claim 5 , epilepsy claim 5 , schizophrenia claim 5 , anxiety claim 5 , depression claim 5 , insomnia claim 5 , nausea claim 5 , emesis claim 5 , alcohol disorders claim 5 , drug addictions such as opiates claim 5 , nicotine claim 5 , cocaine claim 5 , alcohol and psychostimulants claim 5 , hypertension claim 5 , circulatory shock claim 5 , myocardial reperfusion injury claim 5 , atherosclerosis claim 5 , asthma claim 5 , glaucoma claim 5 , retinopathy claim 5 , cancer claim 5 , inflammatory bowel disease claim 5 , acute and chronic liver disease such as hepatitis and ...

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30-04-2015 дата публикации

CORROSION INHIBITION COMPOSITION FOR PIPELINES, PROCESS OF ELABORATION AND SYNTHESIS

Номер: US20150118104A1
Принадлежит:

Compounds and compositions are used as corrosion inhibitors for pipelines for crude oil containing water with high salt concentrations. The inhibitors are ionic liquids, imidazoles, benzotriazoles, and mixtures thereof. The composition includes two or more members of the inhibitors with a solvent. The inhibitors reduce corrosion of metallic surfaces of the pipelines containing crude oil having 0.2 and 40 wt % water, 10,000 to 70,000 ppm salt, and 9 to 600 ppm hydrogen sulfide. A synergic effect is provided by two or more different inhibitors. This synergy is derived from interactions with the metallic surface, among themselves or with the corrosive medium depending on the chain length, to inhibit the corrosion with decrease of the formulation dose. The composition can be a ternary formulation of the three families or two components of one family and a third component of a different family. 1. A corrosion inhibition composition for pipelines , process of elaboration and synthesis , wherein the procedure for obtaining each formulation comprises the following stages: a stage of synthesis of structures used as an active component; a step of addition of one , two or three active components of the same family or of different chemical structure family; a step of incorporating a solvent and a stirring stage until full integration of the formulation is achieved.2. A corrosion inhibition composition according to claim 1 , wherein the inhibitors are basically constituted by compounds of molecular structure families claim 1 , selected from the group consisting of imidazoles claim 1 , benzotriazoles and ionic liquids; the formulations including two or more components of each family and use as alcohol solvents claim 1 , xylene claim 1 , toluene claim 1 , or combinations thereof.3. A corrosion inhibition composition according to claim 1 , wherein it controls the corrosion of metallic surfaces of the pipelines containing congenital water concentrations from 0.2 to 40% by weight; ...

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16-04-2020 дата публикации

IMIDAZOLE DERIVATIVES AS FORMYL PEPTIDE RECEPTOR MODULATORS

Номер: US20200115346A1
Принадлежит:

The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor. 120.-. (canceled)22. The method of claim 21 , wherein in the compound of Formula I claim 21 , or pharmaceutically acceptable salt thereof:{'sup': 1', '2', '4', '5', '20, 'sub': '1-8', 'each R, R, Rand Ris independently H, optionally substituted Calkyl or halogen; wherein each said optional alkyl substituent is independently selected from one or more R;'}{'sup': 3', '17', '20, 'sub': '1-8', 'Ris optionally substituted Calkyl, halogen or —OR; wherein said optional alkyl sub stituent is selected from one or more R;'}{'sup': 6', '25, 'sub': '1-8', 'Ris H or optionally substituted Calkyl, wherein said optional alkyl substituent is selected from one or more R;'}{'sup': 7', '25, 'sub': '1-8', 'Ris H or optionally substituted Calkyl, wherein said optional alkyl substituent is selected from one or more R;'}{'sup': 8', '9', '10', '11, 'sub': '1-8', 'Ris selected from the group consisting of H, OR, NRR; sulfonate, sulfonic acid, phosphonate, phosphonic acid, phosphoric acid and optionally substituted heterocycle, wherein said heterocycle is selected from the group consisting of tetrazole, imidazole, thiazole, oxazole, triazole, thiophene, pyrazole and pyrrole; and wherein said optional heterocycle substituent an optionally substituted Calkyl, wherein said optional alkyl substituent is OH or halogen;'}{'sup': '9', 'sub': 1-8', '1-8', '1-3', 'q', '1-3, 'Ris H or optionally substituted Calkyl, wherein said optional alkyl substituent is OH, halogen, —OCalkyl or —(OCalkylene)—OCalkyl;'}{'sup': 10', '11, 'sub': 1-8', '1-8, 'Ris H or unsubstituted Calkyl; Ris H or unsubstituted Calkyl;'}{'sup': '17', 'sub': '1-8', 'Ris H or unsubstituted Calkyl;'}{'sup': '18', 'sub': '1-8', 'each Ris H or unsubstituted Calkyl;'}{'sup': '19', 'sub': '1-8', 'each Ris H or unsubstituted Calkyl ...

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02-05-2019 дата публикации

FLEXIBLE PIEZOELECTRIC AND FERROELECTRIC HALOIMIDAZOLE CRYSTALS

Номер: US20190127331A1
Принадлежит:

Provided herein are substituted haloimidazole crystals, the substituted haloimidazole crystal comprising a substituted haloimidazole compound wherein the substituents are selected from the group consisting of hydrogen, an alkyl, and a halogen. The substituted haloimidazole crystals may further comprise second substituted haloimidazole. The substituted haloimidazole crystals may be piezoelectric, ferroelectric, flexible, or any combination thereof. Also provided herein are methods for preparing substituted haloimidazole crystals. 2. The crystal of claim 1 , wherein the haloimidazole is a dihaloimidazole.3. The crystal of claim 2 , wherein the dihaloimidazole comprises two different halogens.4. The crystal of claim 2 , wherein the dihaloimidazole comprises two of the same halogen.5. The crystal of claim 2 , wherein one of R claim 2 , R claim 2 , and Ris an alkyl group.6. The crystal of claim 3 , wherein the alkyl group is selected from methyl and ethyl7. The crystal of claim 1 , wherein the haloimidazole is a trihaloimidazole.8. The crystal of claim 7 , wherein the trihaloimidazole comprises at least two different halogens.9. The crystal of claim 7 , wherein the trihaloimidazole comprises three of the same halogen.10. The crystal of any of - claim 7 , wherein the halogen is selected from the group consisting of chlorine claim 7 , bromine claim 7 , and iodine.11. The crystal of claims 1 , wherein the haloimidazole is selected from the group consisting of 4 claims 1 ,5-dichloro-2-methylimidazole claims 1 , 4 claims 1 ,5-dibromo-2-methylimidazole claims 1 , 4 claims 1 ,5-diiodo-2-methylimidazole claims 1 , 2 claims 1 ,4 claims 1 ,5-trichloroimidazole claims 1 , 2 claims 1 ,4 claims 1 ,5-tribromoimidazole claims 1 , 2-bromo-4 claims 1 ,5-dichloroimidazole claims 1 , 2 claims 1 ,4-dibromo-5-chloroimidazole claims 1 , 2 claims 1 ,4-dibromo-5-methylimidazole claims 1 , 4 claims 1 ,5-dichloro-2-ethylimidazole claims 1 , 4 claims 1 ,5-dibromo-2-ethylimidazole claims 1 , 2 ...

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07-08-2014 дата публикации

Novel crystals and process of making 5-(-methyl)-2-methoxy-benzoic acid

Номер: US20140221444A1
Принадлежит: FURIEX PHARMACEUTICALS, INC.

The present invention relates to a novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. 1. A method of treating a mammal suffering from irritable bowel syndrome, pain or another opioid receptor disorder comprising administering to said mammal an effective amount of a Form β crystal of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1H-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid. This Application is a continuation of U.S. application Ser. No. 13/987,009, filed on Jun. 24, 2013; which is a continuation of U.S. application Ser. No. 13/175,342, filed on Jul. 1, 2011, which issued as U.S. Pat. No. 8,609,865 on Dec. 17, 2013; which is a divisional of U.S. application Ser. No. 12/168,331, filed on Jul. 7, 2008, which issued as U.S. Pat. No. 7,994,206 on Aug. 9, 2011; which claims the benefit of priority to U.S. Application No. 60/948,584, filed on Jul. 9, 2007; all of which are incorporated herein by reference in their entireties.The present invention relates to novel crystals of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl] -amino}-methyl)-2-methoxy-benzoic acid and methods of making the zwitterion of 5-({[2-amino-3-(4-carbamoyl-2,6-dimethyl-phenyl)-propionyl]-[1-(4-phenyl-1h-imidazol-2-yl)-ethyl]-amino}-methyl)-2-methoxy-benzoic acid.Delivering an API to a patient requires more than just identifying a molecule and its use. An API must be formulated for delivery to a patient and this formulation (in addition to the API activity) is evaluated by regulatory agencies such as the US Food and Drug Administration (FDA) and the European Medicines Agency (EMEA). The FDA evaluates the formulation for, among other ...

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30-04-2020 дата публикации

CONTINUOUS PROCESS FOR THE PREPARATION OF 2-(1H-IMIDAZOL-4-YL) ETHANAMINE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF

Номер: US20200131137A1
Принадлежит: Jubilant Generics Limited

The invention relates to a commercially viable, cost effective and energy efficient process for the preparation of 2-(1H-Imidazol-4-yl)ethanamine or pharmaceutically acceptable salts thereof in high purity and yield via application of continuous flow technology. 2. The process according to claim 1 , wherein the catalyst used in step (a) is selected from the group comprising of acetophenone claim 1 , 4-methylacetophenone claim 1 , 4-nitroacetophenone claim 1 , 4-bromoacetophenone claim 1 , benzoyl peroxide claim 1 , 2 claim 1 ,2′-azobisisobutyronitrile and cyclohexanone.3. The process according to claim 1 , wherein the solvent used in step (a) is selected from the group comprising of alcohols claim 1 , aromatic hydrocarbon claim 1 , aprotic polar solvent claim 1 , water and mixtures thereof.4. (canceled)5. The process according to claim 1 , wherein the continuous reactor is a plug flow reactor.6. The process according to claim 1 , wherein the continuous reaction has a residence time of about 30 seconds to about 10 minutes.7. (canceled)8. The process according to claim 1 , wherein the pharmaceutically acceptable salt of histamine formed is dihydrochloride.9. The process according to claim 1 , wherein the histamine dihydrochloride is prepared with a purity of not less than 99.9%.10. The process according to claim 1 , wherein the particle size distribution of L-histidine used to prepare the solution of step (a) has a dof less than 300 μ.11. The process according to claim 1 , wherein the particle size distribution of L-histidine used to prepare the solution of step (a) has a dvalue of between about 50 μ and about 300 μ.13. The process according to claim 12 , wherein the particle size distribution of L-histidine has a dless than 200 μ.14. The process according to claim 12 , wherein the particle size distribution of L-histidine has a dless than 100 μ.15. The process according to claim 12 , wherein the particle size distribution of L-histidine has a dless than 50 μ.16. The ...

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25-05-2017 дата публикации

TRIPHENYLETHYLENE COMPOUNDS AND USES THEREOF

Номер: US20170144975A1
Принадлежит:

Triphenylethylene compounds as dual aromatase inhibitors and selective estrogen receptors modulators are described. Also described are methods for treating patients of breast cancers, and patients of breast cancer comorbid with osteoporosis, using the described triphenylethylence compounds or pharmaceutical formulations thereof. 8. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , hydrate claim 1 , or solvate thereof claim 1 , and one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , and excipients.9. A method for treating a patient with cancer claim 8 , the method comprising the step of administering a therapeutically effective amount of the pharmaceutical composition of to the patient in need of relief from said cancer.10. The method of claim 9 , wherein the cancer patient is a patient of breast cancer.11. The method of claim 9 , wherein the cancer patient is a patient of breast cancer comorbid with osteoporosis.12. A method for treating a patient with cancer claim 1 , the method comprising the step of administering a therapeutically effective amount of a compound of claim 1 , together with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , and excipients claim 1 , to the patient in need of relief from said cancer.13. The method of claim 12 , wherein the cancer patient is a patient of breast cancer.14. The method of claim 12 , wherein the cancer patient is a patient of breast cancer comorbid with osteoporosis15. A method for treating a patient with cancer claim 1 , the method comprising the step of administering a therapeutically effective amount of a compound of claim 1 , together with a therapeutically effective amount of one or more other compounds of the same or different mode of action and one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , and excipients claim 1 , to the patient in need of relief from said cancer.16. The ...

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24-06-2021 дата публикации

HYBRID ZEOLITIC IMIDAZOLATE FRAMEWORK AND A METHOD OF CAPTURING CARBON DIOXIDE

Номер: US20210187475A1

A hybrid zeolitic imidazolate framework having an isolated purity of at least 95 wt. %, which is a coordination product formed between zinc(II) ions, a linker of formula (I), and a linker of formula (II); 2. The hybrid zeolitic imidazolate framework of claim 1 , wherein a relative mol % of the linker of formula (II) is 10 to 75 mol % claim 1 , based on a total molar amount of the linkers of formulae (I) and (II).3. The hybrid zeolitic imidazolate framework of claim 1 , wherein claim 1 , each based on a total molar amount of the linkers of formulae (I) and (II):a relative mol % of the linker of formula (II) is 10 mol %,a relative mol % of the linker of formula (II) is 25 mol %,a relative mol % of the linker of formula (II) is 50 mol %, ora relative mol % of the linker of formula (II) is 75 mol %.4. The hybrid zeolitic imidazolate framework of claim 1 , wherein Rand Rare each hydrogen.5. The hybrid zeolitic imidazolate framework of claim 1 , wherein Rand Rare each hydrogen.7. The hybrid zeolitic imidazolate framework of claim 1 , which is isoreticular with ZIF-90.8. The hybrid zeolitic imidazolate framework of claim 1 , which has a BET surface area of 3 to 850 m/g.9. The hybrid zeolitic imidazolate framework of claim 1 , which has a micropore volume of 0.05 to 0.25 cm/g.10. The hybrid zeolitic imidazolate framework of claim 1 , which has a COuptake capacity of 20 to 95 cm/g at 273 K and 15 to 47 cm/g at 298 K claim 1 , each at 760 Torr.11. The hybrid zeolitic imidazolate framework of claim 1 , which has an ideal selectivity of CO/Nof 25 to 80 claim 1 , and an ideal selectivity of CO/CHof 5 to 65.13. The method of claim 12 , wherein the parent zeolitic imidazolate framework is post-synthetically modified with a molar ratio of the amino alcohol of formula (III) to the parent zeolitic imidazolate framework of 0.2:1 to 1.6:1 claim 12 , which provides a relative mol % of the linker of formula (II) of 10 to 75 mol % claim 12 , based on a total molar amount of the linkers of ...

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25-06-2015 дата публикации

STABILIZED MULTI-FUNCTIONAL ANTIOXIDANT COMPOUNDS AND METHODS OF USE

Номер: US20150175552A1
Принадлежит:

Disclosed are novel stable compounds having anti-oxidant properties and methods of using the compounds for the treatment of diseases or injuries associated with oxidative stress. 2. The compound according to claim 1 , wherein the compound is a compound of Formula I wherein:{'sub': 1-6', '1-6, 'R is H, Calkyl or Calkoxy;'}{'sup': 1', '2', '3, 'sub': '1-6', 'Rand Rare each independently H, Calkyl, or —C(═O)R;'}{'sup': '3', 'sub': 1-6', '1-6, 'Ris Calkyl or Calkoxy;'}{'sub': 2', 'm, 'L is —(CH)—;'}{'sup': 1', '5, 'Lis —CH(R)— or —C(═O)—;'}{'sup': '2', 'Lis —O— or —NH—;'}{'sup': '4', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': 5', '2', '7, 'Ris H, —C(O)OH, or —C(═O)LR;'}{'sup': 6', '8, 'sub': 2', 'n, 'Ris H, —(CH)C(═O)R;'}{'sup': '7', 'sub': 1-6', '2', 'p, 'Ris H, Calkyl, or —(CH)C(═O)OH;'}{'sup': '8', 'sub': 3', '2', '2', 'w', '2, 'Ris —OH, —CH, —CHC(═O)OH, or —(CH)—CH(NH)—C(═O)OH;'}m is 1, 2, 3, or 4; andn, p, and w, are each independently 0, 1, 2, 3, or 4.3. (canceled)4. The compound according to claim 2 , wherein R is H claim 2 , methyl or propyl claim 2 , or tert-butoxycarbonyl.5. (canceled)6. (canceled)7. The compound according to claim 2 , wherein Ris H and Ris —C(═O)R.8. (canceled)9. The compound according to claim 2 , wherein Rand Rare H.10. (canceled)11. The compound according to claim 2 , wherein m is 2 or 3.12. The compound according to claim 2 , wherein Ris H or methyl.14. (canceled)15. (canceled)16. The compound according to claim 2 , wherein Lis —CH(R)— and Ris —C(═O)LR.17. The compound according to claim 16 , wherein Lis —O— claim 16 , and Ris H or Calkyl.18. (canceled)19. The compound according to claim 16 , wherein Lis —NH— claim 16 , and Ris H claim 16 , Calkyl claim 16 , or —(CH)C(═O)OH.21. The compound according to claim 1 , wherein the compound is a compound of Formula II claim 1 , wherein L is —(CH)—;{'sup': 1', '5, 'Lis —CH(R)— or —C(═O)—;'}{'sup': '2', 'Lis —O— or —NH—;'}{'sup': '4', 'sub': '1-6', 'Ris H or Calkyl;'}{'sup': 5', '2', '7, 'Ris H, —C( ...

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11-09-2014 дата публикации

NOVEL COMPOUNDS AS OPIOID RECEPTOR MODULATORS

Номер: US20140256779A1
Принадлежит: Jannsen Pharmaceutica, N.V.

The present invention is directed to novel opioid receptor modulators of Formula (I).

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13-06-2019 дата публикации

PROCESS FOR THE PREPARATION OF 5-[[[(2S)-2-AMINO-3-[4-(AMINOCARBONYL)-2,6-DIMETHYLPHENYL]-1-OXOPROPYL] [(1S)-1-(4-PHENYL-1H-IMIDAZOL-2-YL)ETHYL]AMINO] METHYL-2-METHOXYBENZOIC ACID AND ITS POLYMORPHS THEREOF

Номер: US20190177281A1
Принадлежит:

The present invention relates to an improved process for the preparation of 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]amino]methyl]-2-methoxybenzoic acid compound of formula-1, and polymorphs thereof, the compound of formula-1 is further represented by the following structural formula: 21. The process according to claim- , wherein , in step-a) the suitable coupling agent is selected from N ,N′-dicyclohexyl carbodiimide (DCC) , N ,N′-diisopropylcarbodiimide (DIC) , 1-ethyl-3-(3-dimethylamino propyl)carbodiimide HCl (EDC.HCl) , alkyl or aryl chloroformates such as ethylchloro formate , benzylchloroformate , diphenylphosphoro azidate (DPPA) , thionyl chloride , oxalyl chloride , phosphorousoxychloride , phosphorous pentachloride , 4-methyl-2-oxopentanoyl chloride (i-BuCOCOCl) , (Benzotriazol-1-yloxy) tripyrrolidinophosphoniumhexafluoro phosphate (PyBOP) , methane sulfonyl chloride and the like optionally in combination with 1-hydroxy-7-azatriazole (HOAt) , 1-hydroxy benzotriazole (HOBt) , 1-Hydroxy-1H-1 ,2 ,3-triazole-4-carboxylate (HOCt) , N-hydroxy succinamide (HOSu) , N-hydroxysulfosuccinimide (Sulfo-NHS) , 4-dimethylamino pyridine and the like and suitable base is selected from organic or inorganic base;in step-d) the suitable hydrochloric acid source is selected from hydrochloric acid, aqueous hydrochloric acid, methanolic-HCl, ethanolic-HCl, IPA-HCl, hydrochloric acid gas and the suitable base is selected from organic base;in step-a) to step-e) the suitable solvent is selected from alcohol solvents, ketone solvents, ester solvents, hydrocarbon solvents, polar aprotic solvents, ether solvents, nitrile solvents, chloro solvents and polar solvents like water or mixture thereof.3. An improved process for the preparation of amorphous form of 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2 ,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(4-phenyl-1H-imidazol-2yl) ethyl]amino]methyl]-2-methoxy benzoic acid compound ...

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13-06-2019 дата публикации

A PROCESS FOR THE PREPARATION OF ELUXADOLINE

Номер: US20190177282A1
Принадлежит:

The present invention relates to an improved process for the preparation of eluxadoline and its intermediates and that includes the use of an aqueous surfactant solution in the preparation of N-[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide, an intermediate in the preparation of eluxadoline. 1. (canceled)4. (canceled)5. The process according to the claim 2 , wherein the coupling is carried out in the presence of a coupling agent selected from the group consisting of N claim 2 ,N′-dicyclohexylcarbodiimide (DCC) claim 2 , 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDCI) claim 2 , 1 claim 2 ,1′-carbonyldiimidazole (CDI) claim 2 , N claim 2 ,N claim 2 ,N′ claim 2 ,N′-tetramethyl-O-(benzotriazol-1-yl)uronium tetrafluoroborate (TBTU) claim 2 , N claim 2 ,N claim 2 ,N′ claim 2 ,N′-tetramethyl-O-(1H-benzotriazol-1-yl)uronium hexafluorophosphate (HBTU) claim 2 , and (1-cyano-2-ethoxy-2-oxoethylidenaminooxy) dimethylamino-morpholino-carbenium hexafluorophosphate (COMU).7. The process according to the claim 2 , wherein the coupling is carried out in the presence of a base selected from the group consisting of triethylamine claim 2 , N-methylmorpholine claim 2 , 4-(N claim 2 ,N-dimethylamino)pyridine claim 2 , 2 claim 2 ,6-lutidine claim 2 , 1-methylpiperidine claim 2 , N-ethyldiisopropylamine claim 2 , N claim 2 ,N-diisopropylethylamine claim 2 , 2 claim 2 ,4 claim 2 ,6-trimethylpyridine claim 2 , and 2 claim 2 ,4 claim 2 ,6-collidine.8. The process according to claim 2 , wherein the coupling is carried out in the presence of an aqueous surfactant solution prepared by contacting an anionic surfactant claim 2 , a cationic surfactant claim 2 , or a nonionic surfactant with water.9. (canceled)10. (canceled)11. (canceled)12. (canceled) The present invention relates to an improved process for the preparation of eluxadoline and its intermediates.Eluxadoline chemically is 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(4-phenyl-1H- ...

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15-07-2021 дата публикации

METABOLITES OF [3-(4-{2-BUTYL-1-[4-(4-CHLORO-PHENOXY)-PHENYL]-1H-IMIDAZOL-4 YL}-PHENOXY)-PROPYL]-DIETHYL-AMINE

Номер: US20210214314A1
Принадлежит:

The present invention relates to metabolites of [3-(4-{2-butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-diethyl-amine. These metabolites may act as RAGE antagonists. These metabolites may also be useful in assays to measure the presence or amount of one or more metabolites of the parent compound in a sample. 1. A compound selected from the group consisting of:3-(4-{2-Butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl)-phenoxy)-propionic acid;[3-(4-(2-Butyl-1-[4-(4-chloro-phenoxy)-benzyl]-1H-imidazol-4-yl}-phenoxy)-propyl]-ethyl-amine;2-[4-[2-butyl-4-[4-[3-(diethylamino)propoxy]phenyl]imidazol-1-yl]phenoxy]-5-chloro-phenol;5-[4-[2-butyl-4-[4-[3-(diethylamino)propoxy]phenyl]imidazol-1-yl]phenoxy]-2-chloro-phenol; and3-(4-{2-Butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl)-phenoxy)-propan-1-ol;or a pharmaceutically acceptable salt thereof.2. The compound of claim 1 , wherein the compound is 3-(4-(2-Butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propionic acid or a pharmaceutically acceptable salt thereof.3. The compound of claim 1 , wherein the compound is [3-(4-{2-Butyl-1-[4-(4-chloro-phenoxy)-benzyl]-1H-imidazol-4-yl)-phenoxy)-propyl]-ethyl-amine or a pharmaceutically acceptable salt thereof.4. The compound of claim 1 , wherein the compound is 2-[4-[2-butyl-4-[4-[3-(diethylamino)propoxy]phenyl]imidazol-1-yl]phenoxy]-5-chloro-phenol or a pharmaceutically acceptable salt thereof.5. The compound of claim 1 , wherein the compound is 5-[4-[2-butyl-4-[4-[3-(diethylamino)propoxy]phenyl]imidazol-1-yl]phenoxy]-2-chloro-phenol or a pharmaceutically acceptable salt thereof.6. The compound of claim 1 , wherein the compound is 3-(4-(2-Butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl}-phenoxy)-propan-1-ol or a pharmaceutically acceptable salt thereof.7. A pharmaceutical composition comprising a compound selected from the group consisting of:3-(4-(2-Butyl-1-[4-(4-chloro-phenoxy)-phenyl]-1H-imidazol-4-yl)-phenoxy)- ...

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13-07-2017 дата публикации

4,5-DIARYLIMIDAZOLE DERIVATIVES AS HDAC INHIBITORS

Номер: US20170197992A1
Принадлежит:

The present invention relates to a 4,5-diarylimidazole derivative of formulae (I), (II) or (III): or a pharmaceutically acceptable salt thereof, wherein the 4,5-diarylimidazole derivative has a hydroxamic acid residue at a first aryl ring and a residue R1 at a second aryl ring; and wherein R1 is hydrogen, a halogen atom or an unsubstituted or substituted alkoxy group; R2 is independently selected from an unsubstituted or substituted alkyl, alkoxy or alkene group; M is a metal atom; L is a halogen atom, an unsubstituted or substituted phosphane, sulfane, arene or alkene group or a 4,5-diarylimidazole-derivative of formula (I); and n is an integer of from 1 to 5. 2. The 4 claim 1 ,5-diarylimidazole derivative according to claim 1 , wherein R1 is a hydrogen claim 1 , a halogen atom or a Calkoxy group; preferably R1 is a hydrogen claim 1 , a halogen atom or a methoxy or ethoxy group; more preferably R1 is a hydrogen claim 1 , a fluorine atom or a methoxy group; most preferably R1 is a hydrogen or a methoxy group.3. The 4 claim 1 ,5-diarylimidazole derivative according to claim 1 ,{'sub': '1-4', 'wherein R2 is a Calkyl group, preferably R2 is a methyl or ethyl group.'}4. The 4 claim 1 ,5-diarylimidazole derivative according to claim 1 ,wherein M is a transition metal atom, preferably M is Cu, Ag, Au, Rh, Ir, Pt or Ru, more preferably M is Au.5. The 4 claim 1 ,5-diarylimidazole derivative according to claim 1 , wherein L is a Pphosphane claim 1 , sulfane claim 1 , arene or alkene group or the 4 claim 1 ,5-diarylimidazole derivative according to formula (I); preferably L is the 4 claim 1 ,5-diarylimidazole derivative according to formula (I).6. The 4 claim 1 ,5-diarylimidazole derivative according to claim 1 , wherein n is an integer of from 1 to 3 claim 1 , preferably n is an integer of from 1 to 2 claim 1 , more preferably n is 1.7. The 4 claim 1 ,5-diarylimidazole derivative according to claim 1 , wherein the hydroxamic acid is at position 3 or 4 of the first aryl ring. ...

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04-07-2019 дата публикации

PROCESSES FOR THE PREPARATION OF ELUXADOLINE

Номер: US20190202793A1
Принадлежит:

The present invention relates to processes for the preparation of eluxadoline and its intermediates. 2. (canceled)3. The process according to claim 1 , wherein the cyclization of N-[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III to obtain the compound of Formula II is carried out in the presence of acetic acid.4. (canceled)5. The process of claim 3 , wherein the cyclization of N-[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III is carried out in the presence of acetic acid and the toluene are in a ratio of about 1:3 to about 1:8 (vol/vol).6. (canceled)7. The process according to claim 3 , wherein the cyclization of N-[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III is conducted at a temperature of about 80° C. to about 140° C.8. (canceled)9. The process according to claim 3 , wherein the cyclization of N-[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula III proceeds for 2 to 8 hours.10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. The compound of Formula II obtained by the process of having greater than 90% chromatographic purity claim 1 , without the use of column chromatography.16. (canceled)17. (canceled)18. (canceled) The present invention relates to processes for the preparation of eluxadoline and its intermediates.Eluxadoline, chemically 5-[[[(2S)-2-amino-3-[4-(aminocarbonyl)-2,6-dimethylphenyl]-1-oxopropyl][(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]amino]methyl]-2-methoxybenzoic acid, is represented by Formula I.Eluxadoline is a mu-opioid receptor agonist, indicated in adults for the treatment of irritable bowel syndrome with diarrhea (IBS-D).U.S. Pat. No. 7,741,356 describes a process for the preparation of eluxadoline comprising cyclizing N-[(benzyloxy)carbonyl]-N-(2-oxo-2-phenylethyl)-L-alaninamide of Formula IIIwith ammonium acetate in xylene to obtain benzyl [(1S)-1-(5-phenyl-1H-imidazol-2-yl)ethyl]carbamate of Formula II, which is ...

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30-10-2014 дата публикации

IDO Inhibitors

Номер: US20140323740A1
Принадлежит:

Presently provided are compounds according to the formula (I) or (II), and pharmaceutical compositions comprising the compounds, wherein R, R, and Rare defined herein. Such compounds and compositions are useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine -2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease. 1. (canceled)4. The pharmaceutical composition of claim 1 , wherein Ris —OR or —SR.5. The pharmaceutical composition of claim 1 , wherein Ris —OH claim 1 , —OCH claim 1 , or —SH.6. The pharmaceutical composition of claim 1 , wherein{'sup': 12', '14', '15, 'sub': 1', '6', '1', '6', '2', '2', '2, 'R, R, and Rare each independently hydrogen, halogen, cyano, C-Calkyl, C-Chaloalkyl, —OR, —SR, —NR, —C(O)OR, —C(O)NR, or —N(R)S(O)R; and'}{'sup': '13', 'Ris hydrogen or —SH.'}7. The pharmaceutical composition of claim 1 , wherein{'sup': 12', '14', '15, 'sub': 1', '6', '1', '6', '2', '2', '2, 'R, R, and Rare each independently hydrogen, halogen, cyano, nitro, C-Calkyl, C-Chaloalkyl, —OR, —SR, —NR, —C(O)OR, —C(O)NR, or —N(R)S(O)R;'}{'sup': '13', 'Ris hydrogen or —SH; and'}{'sup': '11', 'Ris —OR or —SR.'}8. The pharmaceutical composition of claim 1 , wherein{'sup': 11', '12', '14', '15, 'sub': 1', '6', '1', '6', '2', '2', '2, 'R, R, R, and Rare independently hydrogen, halogen, cyano, C-Calkyl, C-Chaloalkyl, —OR, —SR, —NR, —C(O)OR, —C(O)NR, or —N(R)S(O)R; and'}{'sup': '13', 'Ris hydrogen or —SH,'}9. The pharmaceutical composition of claim 1 , wherein{'sup': 11', '12', '14', '15, 'sub': 1', '6', '1', '6', '2', '2', '2, 'R, R, R, and Rare independently hydrogen, halogen, cyano, C-Calkyl, C- ...

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17-08-2017 дата публикации

PROCESSES FOR PREPARING ASK1 INHIBITORS

Номер: US20170233350A1
Принадлежит:

The present disclosure provides processes for the preparation of a compound of formula: 1131-. (canceled)132. Crystalline 5-(4-cyclopropyl-1H-imidazol-1-1-2-fluoro-4-methylbenzoic acid hydrochloride (Compound of formula (D-a) Form II) characterized by an X-ray powder diffractogram comprising the following peaks: 8.7 , 12.1 , 25.7 , and 26.3 °2θ±0.2 °2θ , as determined on a diffractometer using Cu-K□ radiation at a wavelength of 1.5406 Å.133. Compound of formula (D-a) Form II according to claim 132 , wherein the diffractogram comprises additional peaks at 17.3 claim 132 , 19.0 claim 132 , 22.4 claim 132 , 28.6 claim 132 , and 29.7 °2θ±0.2 °2θ.134. Compound of formula (D-a) Form II according to claim 132 , wherein the diffractogram is substantially as shown in .135. Compound of formula (D-a) Form II according to claim 132 , characterized by a differential scanning calorimetry (DSC) curve that comprises an endotherm at about 217° C.136. Compound of formula (D-a) Form II according to claim 132 , wherein the DSC curve is substantially as shown in .137152-. (canceled) This application claims the benefit under of 35 U.S.C. §119(e) of U.S. Provisional Application 62/096,391, filed on Dec. 23, 2014, and U.S. Provisional Application 62/269,064, filed on Dec. 17, 2015, both of which are hereby incorporated by reference.The present disclosure relates generally to the field of organic synthetic methodology for the preparation of compounds for the treatment of apoptosis signal-regulating kinase 1 (“ASK1”) mediated diseases and the synthetic intermediates prepared thereby.Therapeutic agents that function as inhibitors of ASK1 signaling have the potential to remedy or improve the lives of patients in need of treatment for diseases or conditions such as neurodegenerative, cardiovascular, inflammatory, autoimmune, and metabolic disorders. In particular, ASK1 inhibitors have the potential to treat cardio-renal diseases, including kidney disease, diabetic kidney disease, chronic kidney ...

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13-11-2014 дата публикации

2-IODO IMIDAZOLE-DERIVATIVES

Номер: US20140336232A1
Принадлежит:

The present invention relates to novel 2-iodoimidazole derivatives, to processes for preparing these compounds, to compositions comprising these compounds and to their use as biologically active compounds, in particular for controlling harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators. 2. 2-Iodoimidazole derivative of the formula (I) and/or salt according to claim 1 , in which{'sup': '1', 'X represents OR,'}{'sub': 2', '2, 'Y represents O, S, SO, —CH— or a direct bond,'}m represents 0 or 1,n represents 0 or 1,{'sub': 3', '7', '1', '8', '2', '7', '2', '7', '2', '7', '2', '7', '1', '4', '1', '3', '1', '4', '1', '3', '1', '3', '1', '3', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '3', '7', '3', '7', '1', '3', '1', '4, 'R represents in each case optionally branched C-C-alkyl, C-C-haloalkyl, C-C-alkenyl, C-C-haloalkenyl, C-C-alkynyl, C-C-haloalkynyl, C-C-alkoxy-C-C-alkyl, C-C-haloalkoxy-C-C-alkyl, tri(C-C-alkyl)silyl-C-C-alkyl, in each case optionally halogen-, C-C-alkyl-, C-C-haloalkyl-, C-C-alkoxy-, C-C-haloalkoxy-, C-C-haloalkylthio-, C-C-alkylthio- or phenoxy-substituted (where phenoxy may in turn be substituted by halogen or C-C-alkyl) C-C-cycloalkyl or C-C-cycloalkyl-C-C-alkyl where any substitution is on the cycloalkyl moiety, and optionally mono- to tri-halogen- or —C-C-alkyl-substituted phenyl,'}{'sup': '1', 'sub': 1', '3', '1', '3', '1', '3, 'Rrepresents hydrogen, (C-C-alkyl)carbonyl, (C-C-haloalkyl)carbonyl or tri(C-C-alkyl)silyl,'}{'sup': '2', 'sub': 1', '4', '1', '4, 'Rrepresents hydrogen, fluorine, chlorine, bromine, iodine, C-C-alkyl or C-C-haloalkyl,'}{'sup': '3', 'sub': 1', '4', '1', '4, 'Rrepresents hydrogen, fluorine, chlorine, bromine, iodine, C-C-alkyl or C-C-haloalkyl,'}{'sup': 2', '3, 'sub': 2', '5, 'Rand Rtogether furthermore represent straight-chain or branched and optionally halogen-, in particular fluorine-, chlorine- or bromine-, substituted C-C-alkylene,'}{' ...

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15-08-2019 дата публикации

PROCESSES FOR THE PREPARATION OF ELUXADOLINE

Номер: US20190248748A1
Принадлежит:

The present invention relates to processes for the preparation of eluxadoline. The present invention also provides a compound of Formula V, a process for its preparation, and its use for the preparation of eluxadoline. 1. (canceled)314-. (canceled)16. (canceled)1832-. (canceled)33. The process according to claim 2 , wherein the acid is selected from the group consisting of citric acid claim 2 , acetic acid claim 2 , fumaric acid claim 2 , lactic acid claim 2 , maleic acid claim 2 , malic acid claim 2 , tartaric acid claim 2 , benzoic acid claim 2 , methanesulfonic acid claim 2 , oxalic acid claim 2 , p-toluenesulfonic acid claim 2 , and succinic acid.34. The process according to claim 2 , wherein the reductive amination is carried out in the presence of a reducing agent in a solvent.35. The process according to claim 34 , wherein the reducing agent is selected from the group consisting of sodium borohydride claim 34 , sodium cyanoborohydride claim 34 , sodium triacetoxyborohydride claim 34 , lithium borohydride claim 34 , potassium borohydride claim 34 , Raney Nickel claim 34 , and Palladium on carbon (Pd/C).36. The process according to claim 33 , wherein the solvent is selected from the group consisting of alcohols claim 33 , nitriles claim 33 , halogenated hydrocarbons claim 33 , ethers claim 33 , water claim 33 , and mixtures thereof.38. The process according to claim 36 , wherein the base is selected from the group consisting of sodium hydroxide claim 36 , potassium hydroxide claim 36 , lithium hydroxide claim 36 , calcium hydroxide claim 36 , sodium bicarbonate claim 36 , potassium bicarbonate claim 36 , and cesium hydroxide.39. The process according to claim 36 , wherein the solvent is selected from the group consisting of alcohols claim 36 , nitriles claim 36 , halogenated hydrocarbons claim 36 , ethers claim 36 , water claim 36 , and mixtures thereof. The present invention relates to processes for the preparation of eluxadoline. The present invention also ...

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13-09-2018 дата публикации

METHOD AND APPARATUS FOR SYNTHESIZING A WATER-SOLUBLE HEXAARYL BIIMIDAZOLE

Номер: US20180258051A1
Автор: Finson Stephen L
Принадлежит:

A method for forming a water-soluble hexaaryl biimidazole, comprising the steps of reacting benzil with a carboxy benzaldehyde and ammonium acetate to yield a carboxy triaryl imidazole, and dimerizing the carboxy triaryl imidazole in an alkaline aqueous solution of potassium ferricyanide to yield a water-soluble salt of a bicarboxy hexaaryl biimidazole. 1. (canceled)2. (canceled)3. (canceled)4. A method for forming a water-soluble hexaaryl biimidazole , comprising the steps of:a) reacting benzil with a carboxy benzaldehyde and ammonium acetate to yield a carboxy triaryl imidazole; and 'wherein said water-soluble salt of a carboxy hexaaryl biimidazole is the disodium salt of 2,2′-bicarboxy hexaaryl biimidazole.', 'b) dimerizing said carboxy triaryl imidazole in an alkaline aqueous solution of potassium ferricyanide to yield a water-soluble salt of a bicarboxy hexaaryl biimidazole,'}6. (canceled)8. (canceled)9. A water-soluble hexaaryl biimidazole compound resulting from dimerization of two carboxy triaryl imidazole compounds wherein each of said carboxy triaryl imidazole compounds is the 2-carboxy isomer. The present invention relates to synthesis of organic compounds; more particularly, to synthesis of photo-initiators; and most particularly to a method and apparatus for synthesizing a water-soluble hexaaryl biimidazole (also referred to herein as “HABI”).Various derivatives of hexaaryl biimidazole are well known in the prior art as radical polymerization photoinitiators. All such photoinitiators are insoluble in water.For example, U.S. Pat. No. 6,524,770 B1, “Hexaaryl biimidazole compounds as photoinitiators, photo sensitive composition and method of manufacturing patterns using the compounds”, issued Feb. 25, 2003 to Hidaka et al. and incorporated herein by reference in its entirety discloses a hexaaryl biimidazole compound useful as a photoinitiator, represented by Formula (I) shown in , wherein each R group represents an alkyl group which may be the same or ...

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28-10-2021 дата публикации

SUBSTITUTED 4-AMINO-1H-IMIDAZO[4,5-c]QUINOLINE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION

Номер: US20210332040A1
Принадлежит:

Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators. 4. The method according to for making a compound of Formula (I) claim 3 , or a tautomer claim 3 , a stereoisomer or a salt thereof;{'sup': 'rd', 'comprising (1) contacting a compound of Formula (II) as defined in the 3aspect, or a tautomer, a stereoisomer, or a salt thereof, with a mixture of Reagent 1 selected from dichloroacetic acid, acetic acid, p-toluenesulfonic acid, HCl, citric acid, diphenylphosphinic acid, oxalic acid, methyl phosphonic acid, phenylphosphonic acid, salicylic acid and hydrido(dimethylphosphinous acid-kP)[hydrogen bis(dimethylphosphinito-kP)]platinum (II) or a combination thereof, with or without Base 1 selected from NaOAc, KOAc, NaOPiv, KOPiv, NaOMe, KOMe and N,N-diisopropylethylamine, with an additive selected from pyrrole, N-methylpyrrole, (carboxymethyl)trimethylammonium chloride hydrazide, 2,4-dimethylpyrrole, 2,5-dimethylpyrrole, 4-methoxy-2-methylindole, 2-methylfuran, 1,2-dimethylindole, 2-methylthiophene, and N-methylindole, in Solvent 1 selected from MeOH, MeTHF, BuOH, EtOH, THF, DMF, NMP, DMF, dioxane, toluene, DME, and DMAc or a combination thereof;'}for a time from 1 to 96 hours and at a temperature ranging from 20° C. and 80° C. sufficient for cyclization and to produce a compound of Formula (III), or a tautomer, a stereoisomer, or a salt thereof;{'sup': 'rd', 'sub': 2', '4', '3', '4', '4, 'and (2) contacting the compound of Formula (III) as defined in the 3aspect, or a tautomer, a stereoisomer, or a salt thereof, with Reagent 2 selected from HCl, HBr, HSO, HPO, HBF, 1,5-naphthalenedisulfonic acid, benzenesulfonic acid, methanesulfonic acid, p-toluenesulfonic acid, camphorsulfonic acid, and ethanesulfonic acid or a combination thereof, in Solvent 2 selected from MTBE, MeOH, MIBK, iPrOAc, toluene, 2-Me-THF, MeCN, CPME, IPA or a combination thereof, with or ...

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29-09-2016 дата публикации

LXR MODULATORS

Номер: US20160280661A1
Автор: Busch Brett B.
Принадлежит: EXELIXIS PATENT COMPANY LLC

Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 2. A pharmaceutical composition comprising the compound of claim 1 , or an isotopically-labeled compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and one or more pharmaceutically acceptable carriers.3. A method of treating a disease or disorder comprising administering to a subject in need thereof a therapeutically effective amount of the compound of claim 1 , or an isotopically-labeled compound claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the disease or disorder is insulin resistance claim 1 , osteoarthritis claim 1 , stroke claim 1 , hyperglycemia claim 1 , psoriasis claim 1 , age and UV exposure-related skin wrinkling claim 1 , diabetes claim 1 , cancer claim 1 , Alzheimer's disease claim 1 , inflammation claim 1 , immunological disorders claim 1 , lipid disorders claim 1 , obesity claim 1 , macular degeneration claim 1 , conditions characterized by a perturbed epidermal barrier function claim 1 , conditions of disturbed differentiation or excess proliferation of the epidermis or mucous membrane claim 1 , or cardiovascular disorders.4. The method of claim 3 , wherein the disease or disorder is a cardiovascular disorder claim 3 , a lipid disorder claim 3 , diabetes claim 3 , or Alzheimer's disease.5. The method of claim 4 , wherein the disease or disorder is a cardiovascular disorder.6. The method of claim 5 , wherein said cardiovascular disorder is atherosclerosis.7. The method of claim 4 , wherein the disease or disorder is a lipid disorder.8. The method of claim 7 , wherein said lipid disorder is dyslipidemia.9. The method of wherein the disease or disorder is diabetes.10. The method of wherein the disease or disorder is ...

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27-09-2018 дата публикации

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

Номер: US20180273487A1

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject. 10. The SARD compound of claim 1 , wherein Q claim 1 , Q claim 1 , Qor Qis hydrogen claim 1 , CN claim 1 , NO claim 1 , CF claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , NHCOOR claim 1 , N(R) claim 1 , NHCOR claim 1 , COR claim 1 , or substituted or unsubstituted phenyl.12. The compound according to claim 1 , wherein the compound exhibits at least one of AR-splice variant (AR-SV) degradation activity claim 1 , full length (AR-FL) degradation activity claim 1 , AR-SV inhibitory claim 1 , or AR-FL inhibitory activity.13. A pharmaceutical composition comprising a SARD compound according to claim 1 , or its isomer claim 1 , pharmaceutically acceptable salt claim 1 , pharmaceutical product claim 1 , hydrate or any combination thereof claim 1 , and a pharmaceutically acceptable carrier.14. The pharmaceutical composition according to claim 13 , wherein the composition is formulated for topical use.15. The pharmaceutical composition according to claim 14 , wherein the composition is in the form of a solution claim 14 , lotion claim 14 , salve claim 14 , cream claim 14 , ointment ...

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05-10-2017 дата публикации

METHOD FOR PRODUCING PURE L-HERCYNINE

Номер: US20170283382A1
Автор: Erdelmeier Irene
Принадлежит:

The invention relates to a method for the purification of L-hercynine. Said method for the purification of L-hercynine, from a reaction mixture resulting from the reaction of L-histidine, in controlled pH conditions, with a methylating agent Me X in a polar solvent or a mixture of polar solvents, at room temperature, is characterised in that it comprises at least one step of separating the organic products from the inorganic salts formed during the reaction by electrodialysis. This method allows the L-hercynine losses to be limited during the purification. 1. A method for purifying L-hercynine , or its enantiomer , D-hercynine , or its racemic mixture , or one of its isotopically marked derivatives from a reaction mixture resulting from the reaction of L-histidine , or its enantiomer D-histidine or its racemic mixture , or one of its isotopically marked derivatives or one of its a-N-methylated derivatives , under controlled pH conditions , with a methylation agent MeX in a polar solvent or a mixture of polar solvents , at room temperature , characterized in that it comprises at least one step for separating the organic products from the inorganic salts formed during the reaction by electrodialysis; and in that the electrodialysis is conducted on a reaction medium adjusted to a pH comprised between 8.5 and 9.5 , at the beginning of the electrodialysis.2. The purification method according to claim 1 , characterized in that it comprises an additional step for recrystallization of the L-hercynine claim 1 , or its enantiomer claim 1 , D-hercynine claim 1 , or its racemic mixture claim 1 , or one of its isotopically marked derivatives or one of its methylated derivatives claim 1 , to eliminate the organic impurities.3. A method for the industrial-scale production of L-hercynine claim 1 , or its enantiomer claim 1 , D-hercynine claim 1 , or its racemic mixture claim 1 , or one of its isotopically marked derivatives claim 1 , or one of its a-N-methylated derivatives claim 1 ...

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22-10-2015 дата публикации

LXR MODULATORS

Номер: US20150299136A1
Принадлежит:

Compounds, pharmaceutically acceptable salts, isomers, or prodrugs thereof, of the invention are disclosed, which are useful as modulators of the activity of liver X receptors (LXR). Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed. 1. A compound selected from the group consisting of 2-(1-(3-chloro-3′-fluoro-4′-(hydroxymethyl)-5′-(methylsulfonyl)biphenyl-4-yl)-2-(2-(2-fluorophenyl)propan-2-yl)-1H-imidazol-4-yl)propan-2-ol and 2-(2-(2-(2-chloro-6-fluorophenyl)propan-2-yl)-1-(3′-fluoro-4′-(hydroxymethyl)-3-methyl-5′-(methylsulfonyl)biphenyl-4-yl)-1H-imidazol-4-yl)propan-2-ol , or isotope , or a pharmaceutically acceptable salt thereof.2. The compound of claim 1 , which is 2-(1-(3-chloro-3′-fluoro-4′-(hydroxymethyl)-5′-(methylsulfonyl)biphenyl-4-yl)-2-(2-(2-fluorophenyl)propan-2-yl)-1H-imidazol-4-yl)propan-2-ol claim 1 , or isotope claim 1 , or a pharmaceutically acceptable salt thereof.3. The compound of claim 1 , which is 2-(2-(2-(2-chloro-6-fluorophenyl)propan-2-yl)-1-(3′-fluoro-4′-(hydroxymethyl)-3-methyl-5′-(methylsulfonyl)biphenyl-4-yl)-1H-imidazol-4-yl)propan-2-ol claim 1 , or isotope claim 1 , or a pharmaceutically acceptable salt thereof.4. A pharmaceutical composition comprising a compound of claim 1 , or isotope claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and one or more pharmaceutically acceptable carriers.5. A method of treating a disease or disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of claim 1 , or isotope claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein the disease or disorder is insulin resistance claim 1 , osteoarthritis claim 1 , stroke claim 1 , hyperglycemia claim 1 , psoriasis claim 1 , age and UV exposure-related skin wrinkling claim 1 , diabetes claim 1 , cancer claim 1 , Alzheimer's disease claim 1 , inflammation claim 1 , immunological disorders claim 1 , lipid disorders ...

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24-09-2020 дата публикации

SELECTIVE ANDROGEN RECEPTOR DEGRADER (SARD) LIGANDS AND METHODS OF USE THEREOF

Номер: US20200299243A1

This invention is directed to pyrrole, pyrazole, imidazole, triazole, and morpholine based selective androgen receptor degrader (SARD) compounds including heterocyclic anilide rings and their synthetic precursors, R-isomers, and non-hydroxylated and/or non-chiral propanamides, and pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, triple negative breast cancer, other cancers expressing the androgen receptor, androgenic alopecia or other hyperandrogenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), abdominal aortic aneurysm (AAA), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject. 10. The method of claim 1 , wherein Q claim 1 , Q claim 1 , Qor Qis hydrogen claim 1 , CN claim 1 , NO claim 1 , CF claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , NHCOOR claim 1 , N(R) claim 1 , NHCOR claim 1 , COR claim 1 , or substituted or unsubstituted phenyl.12. The method of claim 1 , wherein the compound exhibits at least one of AR-splice variant (AR-SV) degradation activity claim 1 , full length (AR-FL) degradation activity claim 1 , AR-SV inhibitory claim 1 , or AR-FL inhibitory activity.13. The method of claim 1 , wherein the SARD compound is formulated for topical use.14. The method of claim 13 , wherein the compound is formulated in the form of a solution claim 13 , lotion claim 13 , salve claim 13 , cream claim 13 , ointment claim 13 , liposome claim 13 , spray claim 13 , gel claim 13 , foam claim 13 , roller stick claim 13 , cleansing soap or bar claim 13 , emulsion claim 13 , mousse claim 13 , aerosol claim 13 , or shampoo.15. The method of claim 1 , wherein said disease or condition is triple negative breast cancer claim 1 , Kennedy's disease claim 1 , acne ...

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09-11-2017 дата публикации

USE OF HALOGEN DERIVATIVES OF HISTIDINE AS ELECTROLYTIC SALT IN A PHOTOVOLTAIC DYE CELL

Номер: US20170323732A1
Принадлежит:

The invention relates to the use of halogenated histidine derivatives as electrolyte salts in the preparation of an electrolyte composition in a photoelectrochemical cell based on the sensitization to light of photoactive molecules, and also to a photoelectrochemical cell based on the sensitization to light of photoactive molecules comprising an electrolyte composition comprising at least one halogenated histidine derivative as electrolyte salt.

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10-12-2015 дата публикации

Substituted [1,2,4]triazole and imidazole compounds

Номер: US20150351401A1
Принадлежит: BASF SE

The present invention relates to compounds of the formula I wherein the substituents are defined in the description and claims, their preparation and uses of the compounds I.

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31-10-2019 дата публикации

PYRROLOMYCINS AND METHODS OF USING THE SAME

Номер: US20190330147A1
Принадлежит:

Provided herein are pyrrolomycin derivatives, which can be used to modulate Mcl-1, inhibit proliferation of bacteria and pathogens, as well as to treat infectious diseases and cancers.

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05-11-2020 дата публикации

PPAR AGONISTS, COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE THEREOF

Номер: US20200347037A1
Принадлежит: Mitobridge, Inc.

Provided herein are compounds and compositions useful in increasing PPARδ activity. The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases). 4. The compound of claim 1 , wherein Ris halomethyl claim 1 , CN or halogen.5. The compound of claim 1 , wherein Ris CF claim 1 , Cl or CN.6. The compound of claim 5 , wherein Ris hydrogen claim 5 , halogen claim 5 , CN claim 5 , C-C-alkyl claim 5 , C-Calkoxy claim 5 , C-C-haloalkyl claim 5 , C-C-haloalkoxy claim 5 , S(C-C-alkyl) claim 5 , or furanyl claim 5 , wherein the furanyl can be optionally substituted with C-C-alkyl; and x is 0 or 1.7. The compound of claim 6 , wherein Ris H claim 6 , halogen claim 6 , CN claim 6 , CH claim 6 , halomethyl claim 6 , halomethoxy claim 6 , methoxy or furanyl claim 6 , wherein the furanyl can be optionally substituted with CH; and Ris methyl or halogen.8. The compound of claim 7 , wherein Ris H claim 7 , F claim 7 , Cl claim 7 , CN claim 7 , CF claim 7 , OCFor furanyl; and x is 0.9. The compound of claim 8 , wherein Ris hydrogen.10. The compound of claim 8 , wherein Ris hydrogen or fluoro.11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier or excipient and the compound of claim 1 , or a pharmaceutically acceptable salt thereof.12. A method of treating a PPARδ related disease or condition in a subject claim 1 , comprising administering to the subject in need thereof a therapeutically effective amount of one or more compounds of claim 1 , or a pharmaceutically acceptable salt thereof.13. The method of claim 12 , wherein the PPARδ related disease is a muscle structure disorder claim 12 , a neuronal activation disorder claim 12 , a muscle fatigue disorder claim 12 , a muscle mass disorder claim 12 , a mitochondrial disease claim 12 , a beta oxidation disease claim 12 , a metabolic disease claim 12 , a cancer claim 12 , a vascular ...

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20-12-2018 дата публикации

CHIRAL SYNTHESIS METHOD FOR PRODUCING CIS-IMIDAZOLINE COMPOUNDS FOR PHARMACEUTICAL USE

Номер: US20180362510A1
Принадлежит:

This invention provides a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized according to the invention with an enantiomeric excess as high as 99%. Cis-imidazolines such as Nutlin-3a prepared according to this invention may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions. 130.-. (canceled)351. The method of claim , wherein Ris phenyl.361. The method of claim , wherein Xand Xare both chloride.371. The method of claim , wherein the chiral aromatic acid is D-mandelic acid or L-mandelic acid.381. The method of claim , wherein the separating includes crystallizing molecules of the precursor with the chiral aromatic acid , and recovering the first stereoisomer from crystals formed thereby.391. The method of claim , further comprising separating and recovering the second stereoisomer not associated with the chiral aromatic acid; andderivatizing and cyclizing the second stereoisomer to form a second batch of the same cis-imidazoline.401. The method of claim , wherein the ring-closing reaction performed by combining the first stereoisomer with either triphenylphosphine oxide (PhPO) or 2-fluoropyridine , and with either trifluoromethanesulfonic anhydride (TfO) or trifluoroacetic anhydride (TFAA).411. The method of claim , wherein the cis-imidazoline synthesized thereby is 4-[[(4S ,5R)-4 ,5-bis(4-chlorophenyl)-4 ,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone (UBXO101).4211. The method of claim , wherein the cis-imidazoline prepared from molecules separated in step (b) have an enantiomeric excess (ee) of at least 98%.4413. The method of claim , wherein the chiral aromatic ...

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19-11-2020 дата публикации

PEPTIDE DERIVATIVES AND THERAPEUTIC ACTIVITY THEREOF

Номер: US20200361875A1
Принадлежит: FLAMMA S.P.A.

Disclosed are peptide or pseudopeptide derivatives containing a nitrogenous heterocyclic residue with blocking activity against the by-products of lipid oxidative stress, and in particular of unsaturated aldehydes such as malondialdehyde and 4-hydroxy-trans-2-nonenal (HNE). 2. The compound according to wherein:{'sub': '1', 'Ris a heterocyclic ring selected from imidazole, pyrrole, pyrazole, triazole, indole, isoindole, indazole, benzimidazole and benzotriazole, preferably imidazole or imidazole substituted at the nitrogen atom at the 1-position or at the 3-position with methyl, ethyl or propyl;'}{'sub': 2', '3, 'Rand Rare as defined above.'}3. The compound according to wherein:{'sub': '1', 'Ris imidazole optionally substituted at the nitrogen atom at the 1-position or at the 3-position with methyl, ethyl or propyl;'}{'sub': 2', '2', '8', '8, 'Ris CH—OH or a COORgroup wherein Ris selected from hydrogen, methyl and ethyl;'}{'sub': 3', '4', '5', '6', '7', '6', '7', '1', '10', '3', '7, 'Ris a group of formula II wherein Rand Rare both methyl or halogen, Rand Rare both hydrogen or one of Rand Ris hydrogen and the other is a straight or branched C-Calkoxycarbonyl or C-Ccyclic group, and n and q are as defined above.'}4. The compound according to wherein:{'sub': '1', 'Ris imidazole optionally substituted at the nitrogen atom at the 1-position or at the 3-position with methyl, ethyl or propyl;'}{'sub': 2', '2', '8', '8, 'Ris CH—OH or a COORgroup wherein Ris selected from hydrogen, methyl and ethyl;'}{'sub': 3', '4', '5', '6', '7', '6', '7', '1', '10', '3', '7, 'Ris a group of formula IV wherein Rand Rare joined to form, together with the carbon atom to which they are bonded, a C3-C6 cycloaliphatic ring selected from cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; Rand Rare both hydrogen or one of Rand Ris hydrogen and the other is a straight or branched C-Calkoxycarbonyl or a C-Ccyclic group, and m, n and q are as defined above.'}5. The compound according to wherein:{' ...

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07-02-2008 дата публикации

Surfactants and polymerizable surfactants based on room-temperature ionic liquids that form lyotropic liquid crystal phases with water and room-temperature ionic liquids

Номер: US20080029735A1
Принадлежит: University of Colorado

A modular surfactant architecture based on room temperature ionic liquids (RTILs) has been developed that affords non-polymerizable and polymerizable amphiphiles that form lamellar (L), hexagonal (H) or bicontinuous cubic (Q) LLC phases when mixed with water or RTILs serving as the polar solvent. The amphiphiles are imidazolium salts having two or more imidazolium head groups joined by one or more spacers. Polymerization of the LLC assembly can produce polymeric materials having ordered nanopores, with the ordering of the pores determined by the LLC phase.

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16-06-2005 дата публикации

Zwitterionic compounds and photovoltaic cells containing same

Номер: WO2005055286A2
Принадлежит: Konarka Technologies, Inc.

Zwitterionic compounds, photovoltaic cell charge carrier layers (140) containing such compounds, photovoltaic cells (100) including such charge carrier layers (140), and related methods are disclosed.

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22-05-2007 дата публикации

Zwitterionic compounds and photovoltaic cells containing same

Номер: US7220914B2
Принадлежит: Konarka Technologies Inc

Zwitterionic compounds, photovoltaic cell charge carrier layers containing such compounds, photovoltaic cells including such charge carrier layers, and related methods are disclosed.

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29-09-2005 дата публикации

Zwitterionic compounds and photovoltaic cells containing same

Номер: US20050211292A1
Принадлежит: Konarka Technologies Inc

Zwitterionic compounds, photovoltaic cell charge carrier layers containing such compounds, photovoltaic cells including such charge carrier layers, and related methods are disclosed.

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29-09-2005 дата публикации

Zwitterionic compounds and photovoltaic cells containing same

Номер: WO2005055286A3

Zwitterionic compounds, photovoltaic cell charge carrier layers (140) containing such compounds, photovoltaic cells (100) including such charge carrier layers (140), and related methods are disclosed.

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01-09-1983 дата публикации

VALPROIC ACID SALTS, THEIR PREPARATION AND THEIR USE

Номер: LU83729A1
Автор: Arthur Marie Deboeck
Принадлежит: Galephar

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19-12-2002 дата публикации

Solvent extraction mixture comprising substituted imidazole or benzimidazole for the purification of base metals

Номер: WO2002101101A2
Принадлежит: Billiton Sa Limited

This invention provides an organic solvent extraction mixture for the purification of base metals which includes: a) a first extractant, which is a substituted imidazole (Diagram 1) or benzimidazole (Diagram 2) and wherein the substituents are: R1 = an organic group which has between 2 and 20 carbon atoms, preferably between 6 and 15 carbon atoms; R3 = a hydrogen atom or a short chain organic group with 1 or 2 carbon atoms, preferably hydrogen or a methyl group; R4 = a hydrogen atom or a short chain organic group with 1 or 2 carbon atoms, preferably hydrogen or a methyl group; R2 = a -2-pyridine group in which the pyridine group can be substituted or unsubstituted; or = a -methylene-1-pyrazole group in which the pyrazole group can be substituted or unsubstituted; or = an imidazole based group, which may be a mirror image of the compound shown in Diagram 1 or 2; or = a methylene-amino group as shown in Diagram 3; b) a non selective strongly acidic cation second extractant, such as a sulphonic acid (R-SO2H), to facilitate phase transfer of base metal ions from aqueous weakly acidic sulphate solution into the organic phase, and wherein R is an aliphatic group, either saturated or unsaturated and branched or unbranched, an aromatic organic group or a mixed group consisting of aliphatic and aromatic parts, with between 3 and 40 carbon atoms, preferably with between 8 and 30 carbon atoms; c) a modifier to improve the characteristics of the organic phase with respect to metal complex solubility to avoid third phase formation, completeness and ease of stripping, viscosity and phase disengagement; and d) a diluent, which is selected from a non-specific aliphatic or aromatic or partly aliphatic, partly aromatic mixture of unspecified composition with moderate boiling point range and a suitable flash point, such as Kerosene, Shellsol (various grades), Escaid (various grades), Solvesso and similar products.

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25-06-1998 дата публикации

Relatively stable (1,3-disubstitutedimidazol-2-ylidene)-type carbenes

Номер: WO1998027064A1

This invention concerns a compound of formula (I) wherein: R?1 and R2¿ are each independently hydrocarbyl or substituted hydrocarbyl; X1 is an element or substituted element more electronegative than carbon; and X2 is an element more electronegative than carbon, a substituted element more electronegative than carbon, hydrogen, hydrocarbyl, substituted hydrocarbyl or an inert functional group. A process for making these carbenes is also disclosed. The carbenes are useful in various catalysts and as ligands in transition metal compounds.

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07-01-2015 дата публикации

氨基酸席夫碱配体银配合物及其制备方法与抗菌应用

Номер: CN104262366A
Принадлежит: Suihua University

本发明提供了水杨醛缩 L -组氨酸席夫碱配体及其还原型配体与银形成的两种配合物以及制备方法和抗菌应用。所述的两种银配合物可用通式{Ag(L 1 )} n 和Ag 2 (L 2 ) 2 ·3H 2 O表示,其中L 1 与L 2 结构式如图所示。制备方法:首先用NaBH 4 将水杨醛缩 L -组氨酸席夫碱配体(HL 1 )中C=N双键还原为C-N单键后,得到还原型配体(HL 2 ),然后两种配体分别与AgNO 3 作用得到两种银配合物。本发明所提供的氨基酸席夫碱银配合物结构全新,制备方法简单,且具有显著的抗菌活性,有望在抗菌材料以及抗菌药物中得到应用。

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24-10-2006 дата публикации

Process for the preparation of formylimidazoles

Номер: KR100587187B1
Принадлежит: 론자 아게

본 발명은 할로겐화 히드록시메틸이미다졸의 할로겐화 포르밀이미다졸로의 촉매 전환을 위한 신규 방법에 관한 것이다. 촉매반응은 과산화물의 존재하에 수행된다. 할로겐화 포르밀이미다졸은 약제학적 유효 성분의 중요한 중간물질이다. The present invention relates to a novel process for catalytic conversion of halogenated hydroxymethylimidazoles to halogenated formylimidazoles. Catalysis is carried out in the presence of peroxides. Halogenated formylimidazoles are important intermediates of pharmaceutically active ingredients.

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14-09-2010 дата публикации

Synthesis of histamine dihydrochloride

Номер: CA2356871C
Принадлежит: Maxim Pharmaceuticals Inc

The invention disclosed herein relates to the preparation of pharmaceutical grades of histamine dihydrochloride using a two step non-enzymatic synthetic method. The invention disclosed herein describes the synthesis of histamine dihydrochloride by the non-enzymatic decarboxylation of histidine and the step-wise conversion of the decarboxylated product to the dihydrochloride salt form. The invention disclosed herein considers a final product of histamine dihydrochloride containing less than each of the following: 0.8% L- histidine HCI monohydrate, 0.1% individual chromatographic impurities, and 2% total impurities, to be acceptable for pharmaceutical use.

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09-11-2001 дата публикации

히스타민 디하이드로클로라이드의 합성 방법

Номер: KR20010099867A

본 발명은 2단계의 비효소적 합성 방법을 사용하여 약학 등급의(pharmaceutical grade) 히스타민 디하이드로클로라이드를 제조하는 방법에 관한 것이다. 본 발명은 히스티딘을 비효소적으로 탈카복실화시킨후 상기 탈카복실화된 생성물을 디하이드로클로라이드 염의 형태로 변환시켜 히스타민 디하이드로클로라이드를 합성하는 방법을 개시하고 있다. 본 발명에서는 L-히스티딘 HCl 일수화물을 0.8% 이하, 각각의 크로마토그래피의 불순물을 0.1% 이하, 및 전체 불순물을 2% 미만으로 함유하는 히스타민 디하이드로클로라이드의 최종 생성물이 약학적 용도로서 허용 가능하다고 보고 있다.

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20-03-1999 дата публикации

Histidine derivatives and process for the preparation thereof

Номер: KR0178086B1
Принадлежит: 손경식, 제일제당주식회사

1. 청구범위에 기재된 발명이 속한 기술분야 1. TECHNICAL FIELD OF THE INVENTION 유기화합물 및 약학. Organic compounds and pharmaceuticals. 2. 발명이 해결하려고 하는 기술적 과제 2. The technical problem to be solved by the invention 개선된 안지오텐신 II 길항제의 개발. Development of Improved Angiotensin II Antagonists. 3. 발명의 해결방법의 요지 3. Summary of Solution to Invention 하기 일반식(I)로 표시되는 화합물(여기서 R 1 은 C 1-6 알킬, C 2-6 알케닐 또는 C 3-7 사이클로알킬이고, R 2 는 -COOH, -SO 2 NHR 4 , 또는 C결합형 테트라졸이며, R 3 은 수소, 또는 C 1-6 알킬이고, R 4 는 R 1 으로 치환된 벤질이며, X는 수소, 산소, 또는 황이고, Y는 하이드록시, C 1-6 알콕시, C 1-6 카르복실, 또는 피리딘카르복실이다.): A compound represented by the following general formula (I), wherein R 1 is C 1-6 alkyl, C 2-6 alkenyl or C 3-7 cycloalkyl, and R 2 is —COOH, —SO 2 NHR 4 , or C A bound tetrazole, R 3 is hydrogen, or C 1-6 alkyl, R 4 is benzyl substituted with R 1 , X is hydrogen, oxygen, or sulfur, Y is hydroxy, C 1-6 alkoxy, C 1-6 carboxyl, or pyridinecarboxyl): 4. 발명의 중요한 용도 4. Important uses of the invention 중추신경계 질환 및 심장혈관계 질환의 치료제. Treatment of central nervous system diseases and cardiovascular diseases.

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30-10-1984 дата публикации

Method of obtaining cymetidine

Номер: SU1122222A3

I. СПОСОБ ПОЛУЧЕНИЯ ЩШЕТИД11НА путем взаимодействи  производных 5-метил-1Н-имидазола и N-циано N-метил-гуанидина, вз тых в эквимол рных количествах, в водной среде в присутствии щелочи, отлич ающ и и с   тем, .что, с целью упрощени  процесса, в качестве производных 5-метил-1Н-имидазола и N-циано-Мметил-гуанидина используют 4-галоидметил-5-метил-1Н-имидазол и N-циано-М-метил-М - I. THE METHOD OF OBTAINING SCHSHETID11HA by the interaction of 5-methyl-1H-imidazole and N-cyano N-methyl-guanidine derivatives, taken in equimolar amounts, in an aqueous medium in the presence of alkali, is characterized by to simplify the process, 4-halomethyl-5-methyl-1H-imidazole and N-cyano-M-methyl-M are used as derivatives of 5-methyl-1H-imidazole and N-cyano-Mmethyl-guanidine

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25-06-2014 дата публикации

Substituted [1,2,4]triazole and imidazole compounds

Номер: EP2746260A1
Принадлежит: BASF SE

The present invention relates to compounds of the formula I wherein the variables are defined in the description and claims, their preparation and uses thereof.

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25-06-2014 дата публикации

Substituted [1,2,4]triazole and imidazole compounds

Номер: EP2746255A1
Принадлежит: BASF SE

The present invention relates to compounds of the formula I wherein the substituents are as defined in the description and claims, their preparation and their uses.

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25-06-2014 дата публикации

Substituted [1,2,4]triazole and imidazole compounds

Номер: EP2746258A1
Принадлежит: BASF SE

The present invention relates to compounds of the formula I wherein the variables are defined in the description and claims, their preparation methods and uses of the compounds.

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25-06-2014 дата публикации

Substituted [1,2,4]triazole and imidazole compounds

Номер: EP2746259A1
Принадлежит: BASF SE

The present invention relates to compounds of the formula I Wherein the variables are defined in the description and claims, their preparation and uses of compounds I.

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25-06-2014 дата публикации

Fungicidal imidazolyl and triazolyl compounds

Номер: EP2746256A1
Принадлежит: BASF SE

The present invention relates to fungicidal imidazolyl and triazolyl compounds I, agrochemical compositions comprising them, to their use and to methods for combating phytopathogenic fungi. The present invention also relates to seeds treated with at least one such compound. Furthermore the invention relates to processes for preparing compounds of formula I as well as to specific intermediates that are obtained during the reaction sequence.

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25-06-2014 дата публикации

Substituted [1,2,4]triazole and imidazole compounds

Номер: EP2746257A1
Принадлежит: BASF SE

The present invention relates to compounds of the formula I wherein, the variables are defined in the description and the claims, their preparation processes and uses.

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26-06-2014 дата публикации

Fungicidal imidazolyl and triazolyl compounds

Номер: WO2014095381A1
Принадлежит: BASF SE

The present invention relates to fungicidal imidazolyl and triazolyl compounds (I), agrochemical compositions comprising them, to their use and to methods for combating phytopathogenic fungi. The present invention also relates to seeds treated with at least one such compound. Furthermore the invention relates to processes for preparing compounds of formula I as well as to specific intermediates that are obtained during the reaction sequence.

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27-12-2007 дата публикации

N1-((Pyrazol-1-Ymethyl)-2-Methylphenyl)-Phatalamide Derivatives And Related Compounds Insecticides

Номер: US20070299085A1
Принадлежит: Bayer CropScience AG

Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfinyl, C 1-6 alkylsulfenyl or C 1-6 alkylsulfonyl, R 1 represents C 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, or C 1-6 alkyl, m represents 0 or 1, A represents O, S, SO, SO 2 , CH 2 or CH(CH 3 ), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

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09-03-2010 дата публикации

Heterocycle-substituted n-phenyl-phthalamide derivatives, related compounds and their use as insecticides

Номер: US7674807B2
Принадлежит: Bayer CropScience AG

Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfinyl, C 1-6 alkylsulfenyl or C 1-6 alkylsulfonyl, R 1 represents C 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, or C 1-6 alkyl, m represents 0 or 1, A represents O, S, SO, SO 2 , CH 2 or CH(CH 3 ), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

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27-05-2010 дата публикации

Heterocycle-substituted, n-phenyl-phthalamide derivatives, related compounds and their use as insecticides

Номер: US20100130743A1
Принадлежит: Bayer CropScience AG

Novel benzenedicarboxamides of the formula (I) wherein X represents hydrogen, halogen atom, nitro, C 1-6 alkylsulfonyloxy, C 1-6 alkylsulfinyl, C 1-6 alkylsulfenyl or C 1-6 alkylsulfonyl, R 1 represents C 1-6 alkyl, C 1-6 alkylthio-C 1-6 alkyl, C 1-6 alkylsulfinyl-C 1-6 alkyl or C 1-6 alkylsulfonyl-C 1-6 alkyl, Y represents halogen or C 1-6 alkyl, m represents 0 or 1, A represents O, S, SO, SO 2 , CH 2 or CH(CH 3 ), and Q represents a 5- or 6-membered heterocyclic group that contains at least one hetero atom selected from the group consisting of N, O and S and can be optionally substituted; processes for their preparation, their intermediates and their use as insecticides.

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08-02-1984 дата публикации

Novel process for preparing n-cyano-n-methyl-n"(2-((methyl-5-imidazolyl)methylthio)ethyl

Номер: KR840000071B1

Cimetidine (VII) was prepd. by treating 4-methyl-5-hydroxymethyl imidazol-HCl with 2-aminoethanthiol-H2SO4 to give 86.2% 4-methy1-5[(2-aminoethyl) thiomethy1 imidazole, which was treated with NCN:C(OEt)SMe to give 78.3% N-cyano-N'=[2-((4-methyl-5 -imidazolyl) methylthio)ethyl -o-ethyl-isourea. Aminolysis of the latter compd. with MeNH2 gave 80.3% cimetidine.

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04-08-1982 дата публикации

Process for preparation of 5-methyl-4(2-aminoethyl) thio ethyl imidazol

Номер: KR820001386B1
Автор: 심영기
Принадлежит: 대한중외제약 주식회사, 이종호

Substituted imidazoles I useful as a synthetic intermediate of cure of a gastric ulcer, were prepd. Thus, 50g 5-methyl-4-imidazole carboxylic acid methyl ester reacted with 16.5g sodium bis aluminium hydride and 16.5 g toluene to give 39.48g 4-hydroxymethyl-5-methyl-1H-imidazole(yield 98.7%).

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18-04-1986 дата публикации

4-methyl-5-thioformamidinomethylimidazole dihydrochloride

Номер: JPS6176465A
Принадлежит: KANTO ISHI PHARMA CO Ltd

(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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26-04-2011 дата публикации

Surfactants and polymerizable surfactants based on room-temperature ionic liquids that form lyotropic liquid crystal phases with water and room-temperature ionic liquids

Номер: US7931824B2
Принадлежит: University of Colorado

A modular surfactant architecture based on room temperature ionic liquids (RTILs) has been developed that affords non-polymerizable and polymerizable amphiphiles that form lamellar (L), hexagonal (H) or bicontinuous cubic (Q) LLC phases when mixed with water or RTILs serving as the polar solvent. The amphiphiles are imidazolium salts having two or more imidazolium head groups joined by one or more spacers. Polymerization of the LLC assembly can produce polymeric materials having ordered nanopores, with the ordering of the pores determined by the LLC phase.

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25-02-1975 дата публикации

Method for preparing imidazole derivatives

Номер: SU461100A1

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02-06-2021 дата публикации

Amino-acid derivative of the decahydro-closo-decaborate anion and its antiviral activity against influenza a virus

Номер: RU2749006C1

FIELD: virology; medicine.SUBSTANCE: invention relates to virology and medicine, namely to the amino-acid derivative of the decahydro-closo-decaborate anion (Na2[B10H9OCH2CH2CH2CH2CO-His-OMe]), where the anion part is represented by the formula (I).EFFECT: compound Na2[B10H9-O(CH2)4CO-His-OMe] inhibits the reproduction of the influenza A virus, including strains resistant to adamantane-type drugs.2 cl, 3 dwg, 3 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 749 006 C1 (51) МПК C07D 233/64 (2006.01) C07F 5/02 (2006.01) C01B 35/18 (2006.01) A61K 31/4172 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 233/64 (2021.02); C07F 5/02 (2021.02); A61K 31/4172 (2021.02) (21)(22) Заявка: 2020138978, 27.11.2020 (24) Дата начала отсчета срока действия патента: Дата регистрации: 02.06.2021 (45) Опубликовано: 02.06.2021 Бюл. № 16 2 7 4 9 0 0 6 R U (73) Патентообладатель(и): федеральное государственное бюджетное учреждение "Национальный исследовательский центр эпидемиологии и микробиологии имени почетного академика Н.Ф. Гамалеи" Министерства здравоохранения Российской Федерации (RU) (56) Список документов, цитированных в отчете о поиске: RU 2676699 C1, 10.01.2019. RU 2624906 C2, 10.07.2017. WO 2020180390 А1, 10.09.2020. WO 2017216816 А1, 21.12.2017. Genady, A. R., & Nakamura, H.: " Undecahydrocloso-dodecaborates as good leaving groups in organic synthesis: generation of substituted styrenes via elimination of arylethyl dodecaborates", Organic & Biomolecular Chemistry, 2010, (см. прод.) (54) Аминокислотное производное декагидро-клозо-декаборатного аниона и его противовирусная активность в отношении вируса гриппа А (57) Реферат: Изобретение относится к вирусологии и адамантанового ряда. 1 з.п. ф-лы, 3 ил., 3 пр. медицине, а именно к аминокислотному производному декагидро-клозо-декаборатного аниона (Na2[B10H9OCH2CH2CH2CH2CO-His-ОМе] ), где анионная часть представлена формулой (I). Cоединение: Na2[B10H9-O(CH2)4CO-His-OMe] ...

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10-06-2022 дата публикации

Synthesis method of high-purity histamine dihydrochloride

Номер: CN112266360B
Принадлежит: Wuhan Jason Biotech Co ltd

本发明公开了一种高纯度组胺二盐酸盐的合成方法,属于有机合成技术领域。该方法包括:在溶剂A中,L‑组氨酸在复合脱羧催化剂的作用下于110‑150℃条件下进行脱羧反应,反应完成后过滤,复合脱羧催化剂由主催化剂和辅助催化剂构成,主催化剂选自氢氧化钠、氢氧化钾、碳酸钠、碳酸钾、吡啶、4‑甲基吡啶、苯胺、4‑甲基苯胺、N,N‑二甲基苯胺和N,N‑二甲基甲酰胺中的一种,辅助催化剂选自苯甲酮、苯乙酮、二苯甲酮和对甲基苯乙酮中的一种;对滤液进行减压蒸馏,在残留物中加入水并使用盐酸调整pH值至5‑6得到水溶液;水溶液采用萃取剂萃取至少一次以进行除杂;蒸除水溶液中的水,再用溶剂B进行打浆,过滤和干燥得到产品。

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21-10-2022 дата публикации

Preparation method of 4-halogenated-1- (difluoromethyl) -1H-imidazole

Номер: CN115215803A

本发明公开了一种4‑卤代‑1‑(二氟甲基)‑1H‑咪唑的制备方法。该方法包括将2,4,5‑三卤代‑1‑(二氟甲基)‑1H‑咪唑与脱卤试剂在有机溶剂中,惰性气体氛围下发生高区域选择性交换生成中间态,再加入水反应得到4‑卤代‑1‑(二氟甲基)‑1H‑咪唑,所述脱卤试剂选自格氏试剂或有机锂试剂,所述格氏试剂为R‑Mg‑Br,所述有机锂试剂为R‑Li,其中R为C1‑6烷基或苯基,所述脱卤试剂与2,4,5‑三卤代‑1‑(二氟甲基)‑1H‑咪唑的摩尔比为2~4:1。本发明的制备方法可以高选择性高收率地得到目标化合物,且不会产生目标化合物的同分异构体,后续分离简单,利于工业化生产。

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