ПРОИЗВОДНЫЕ ИМИДАЗОЛА И ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМАЯ КОМПОЗИЦИЯ

Изобретение относится к производным имидазола общей формулы I, где n=0 или 1, R1 - водород, алкил, R2 - водород или R2 и R3 образуют двойную связь, R3 - водород, алкил, R4 - водород, алкил, гидроксигруппа, алкокси, R5 - водород или алкил, или R4 и R5 образуют карбоксильную группу, R6, R7, R8 - водород, алкил, гидроксигруппа, алкокси, гидроксиалкил, галоген, Х - -CHR9-(CHR10)m-, m = 0 или 1, R9 и R10 - водород или алкил. Соединения формулы I обладают α2 -агонистической активностью и благодаря этому свойству могут использоваться в качестве активного ингредиента в фармацевтической композиции. 2 с. и 13 з.п.ф-лы, 2 табл.

СИНТЕЗ КИСЛОРОДЗАМЕЩЕННЫХ БЕНЗОЦИКЛОГЕПТЕНОВ В КАЧЕСТВЕ ЦЕННЫХ ПРОМЕЖУТОЧНЫХ ПРОДУКТОВ ДЛЯ ПОЛУЧЕНИЯ ТКАНЕСЕЛЕКТИВНЫХ ЭСТРОГЕНОВ

Изобретение относится к новым промежуточным продуктам и усовершенствованному способу получения соединения С: Предлагаемый в изобретении способ получения основан на использовании недорогих исходных материалов, позволяет получать промежуточные продукты с высоким выходом и высокой степенью чистоты без необходимости проводить операции по хроматографической очистке и может быть реализован в условиях крупномасштабного промышленного производства. Изобретение относится к усовершенствованным способам получения соединения формулы I: соединения формулы II: соединения формулы III: соединения формулы VIII: соединения формулы IX: а также к реагенту, состоящему из трибромида бора и 2,6-диметилпиридина, для щадящего и селективного отщепления метильной группы в ароматических простых метиловых эфирах. 11 н. и 1 з.п. ф-лы.

ПРОИЗВОДНЫЕ 1-N-ФЕНИЛАМИНО-1Н-ИМИДАЗОЛА И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Изобретение относится к новым производным имидазола формулы (I): ! ! и к его солям с кислотой, где R1 и R2 обозначают водород; Q обозначает(СН2)m-Х-(СН2)n-А; А обозначает прямую связь. О, SO2, NR5; Х обозначает прямую связь, О, SO2, C(O) или NR5; Z обозначает группу, выбранную из: ! ! m и n обозначают, каждый независимо, 0, 1, 2, 3 или 4; р обозначает 1, 2, 3 или 4; q обозначает 0, 1 или 2; пунктирная линия означает, что R8 и/или R9 могут находиться в любом положении бензотиофенового кольца; R3 и R8 обозначают, каждый независимо, водород или гидрокси, циано, галоген, нитро, ! (С1-С6)алкил, (С1-С6)алкокси, трифторметил, (С1-C6)алкилтио, (С1-С6)алкилсульфонил, ацил, (С1-С6)алкоксикарбонил, карбоксамидо, ! NR10R11, SO2NR10R11, OSO2NR10R11 или NR12SO2NR10R11, OSO2NR12SO2NR10R11, CO2R10; когда Q-Z обозначает ! ! n обозначает 0, 1 или 2 и р обозначает 1, один из R3 и R8 обозначает гидрокси, нитро, ! NR10R11, OSO2NR10R11, NR12SO2NR10R11, ! OSO2NR12SO2NR10R11, CO2R10, CONR10R11, a другой обозначает ...

ПРОИЗВОДНЫЕ ИНДЕНА В КАЧЕСТВЕ ФАРМАЦЕВТИЧЕСКИХ СРЕДСТВ

Настоящее изобретение относится к соединениям формулы (I) в виде отдельного стереоизомера, смеси стереоизомеров или рацемической смеси стереоизомеров и их фармацевтически приемлемым солям. Соединения настоящего изобретения обладают противовоспалительной активностью. В формуле (I) ! ! кольцо А, С или D независимо является полностью или частично насыщенным; каждый из С1, С4, С11, С12, С15 и С16 независимо замещен двумя атомами водорода; каждый из С9 и С14 независимо замещен атомом водорода; R1 означает -OR7 или -N(R7)2. Значения остальных радикалов указаны в формуле изобретения. Изобретение также относится к фармацевтической композиции, обладающей противовоспалительной активностью и содержащей эффективное количество соединения изобретения, и к применению соединений для получения лекарственного средства, обладающего противовоспалительной активностью. 3 н. и 20 з.п. ф-лы.

СПОСОБ ПОЛУЧЕНИЯ АЗОТСОДЕРЖАЩИХ ГЕТЕРОЦИКЛИЧЕСКИХ СОЕДИНЕНИЙ

Использование: в качестве препаратов, обладающих противогрибковым действием. Сущноть изобретения: продукт общей формулы; , где Ar - фенил, замещенный одним или более галогенами, (C1-C3) - галоалкилами или (C1-C4) - галоалкоксигруппами; K, X1, Z обозначают независимо друг от друга О, B1 и B2 , которые могуб быть одинаковыми или различными и обозначают линейные или разветвленные (C1-C6) - алкилидены, Rh обозначает (C1-C6) - галоалкил, содержащий от 1 до 9 атомов галогена, (C3-C8) - галоалкоксиалкил, где галогеном является фтор или хлор, А обозначает азотную гетероциклическую группу, выбранную из имидазолов, замещенных C1-C6 - алкилами или пиридина. Реагент 1: соединение формулы: Ar-X1-B1-Y , где Ar, X1 и B1 имеют приведенные значения, Y - галоген. Реагент II: амин формулы: NA2-B2, -ZH , где B2 и Z имеют вышеприведенные значения. Среда - органический растворитель, в присутствии основания при комнатной температуре. Реагент III: Ar-X1-B1-NH-B2-ZH , где Ar, X1 , B1 , B2 , Z имеют вышеприведенные ...

ЗАМЕЩЕННЫЕ 2-ГИДРОКСИ-3-[1-(1H-ИМИДАЗОЛ-4-ИЛ)-АЛКИЛ] - БЕНЗОЛКАРБОКСИМИДАМИДЫ, ИХ ОПТИЧЕСКИЕ ИЗОМЕРЫ, ИХ РАЦЕМИЧЕСКИЕ СМЕСИ ИЛИ ИХ НЕТОКСИЧНЫЕ, ОФТАЛЬМОЛОГИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ ПРИСОЕДИНЕНИЯ КИСЛОТ.

Предложены указанные соединения общей формулы I ,где R1 - атом водорода или алкильный радикал с 1 - 4 C-атомами; R2 - атом водорода, гидроксильная группа, аминогруппа или алкильный радикал с 1 - 4 C-атомами; R3 - атом водорода, или R1 и R2 вместе образуют группу -CH2-CH2-, и их нетоксичные, офтальмологически приемлемые соли присоединения кислот. Предложен также способ получения соединений формулы I, который заключается во взаимодействии соединения формулы II, где R1 имеет указанное выше значение, с алканолом с 1 - 4 C-атомами, в присутствии газообразного хлороводорода; полученный при этом продукт формулы III, где значение R1 указано выше и alk обозначает алкильный радикал с 1 - 4 C-атомами, вводят во взаимодействие с одним из энантиомеров α-метилбензиламина; таким образом полученный 2-гидрокси-3-[1-(1H-имидазол-4-ил)-алкил]-N-α-метилбензил-бензол-карбоксимидамид формулы IV, где R1 имеет указанное значение, вводят во взаимодействие с азотсодержащим соединением формулы R2NH2(Y), в которой ...

СПОСОБ ПОЛУЧЕНИЯ 1,2,3,9-ТЕТРАГИДРО-9-МЕТИЛ-3-[(2-МЕТИЛ-1Н-ИМИДАЗОЛ-1-ИЛ)-МЕТИЛ]-4Н-КАРБАЗОЛ-4-ОНА

Способ получения 1,2,3, 9-тетрагидро-9-метил-3- [(2-метил-1Н-имидазол-1-ил)метил] -4Н-карбазол-4-она формулы I, который заключается в циклизации соединения формулы II при условиях ацилирования по Фриделю-Крафтсу через активацию карбоксильной группы кислотным катализатором в среде подходящего растворителя и конечным выделением требуемого продукта общепринятыми способами. 4 з.п. ф-лы.

ПРИМЕНЕНИЕ АТИПАМЕЗОЛА ДЛЯ ЛЕЧЕНИЯ МУЖСКОЙ СЕКСУАЛЬНОЙ ИМПОТЕНЦИИ

Изобретение относится к медицине. Предложен способ лечения мужской сексуальной импотенции путем введения атипамизола определенными способами в определенных дозах. Технический результат: новый способ лечения мужской импотенции. 1 ил.

СПОСОБ ПОЛУЧЕНИЯ ИНГИБИТОРОВ 5-ЛИПОКСИГЕНАЗЫ, ИМЕЮЩИХ РАЗЛИЧАЮЩИЕСЯ ГЕТЕРОЦИКЛИЧЕСКИЕ СИСТЕМЫ

Описан способ получения соединения формулы (1.3.0), где является группой, выбранной из формул (1.3.2), (1.3.3), (1.3.4) или (1.3.5), включающий образование реакционной смеси, состоящей из карбоксамида формулы (2.0.0) и соответствующего бициклического N-гетероцикла в апротонном растворителе в присутствии сильного основания в твердой форме, выбранного из группы, включающей гидроксид натрия и гидроксид калия, и (необязательно) в присутствии каталитического количества карбоната цезия, Cs2СО3 или катализатора межфазного переноса с последующим нагреванием указанной реакционной смеси в атмосфере азота, в результате чего образуется целевое соединение. Также раскрыты способ получения одного из конкретных соединений и способ получения мезилатной соли соединения. Изобретение представляет собой улучшенный способ получения известных и новых ингибиторов 5-липоксигеназы, полезных при лечении воспалительных заболеваний и аллергии. 4 с. и 4 з.п. ф-лы, 3 табл.

УЛУЧШЕННЫЙ СПОСОБ ПОЛУЧЕНИЯ МЕДЕТОМИДИНА ИЛИ ЕГО НЕТОКСИЧНЫХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫХ СОЛЕЙ

Настоящее изобретение относится к области органической химии, а именно к способу получения 4-[1-(2,3-диметилфенил)этил]-1Н-имидазола, известного также под названием медетомидин, соответствующего структурной формуле I !! который заключается в том, что проводят алкилирование N-триметилсилилимидазола 2,3-триметилбензилхлоридом в присутствии четыреххлористого титана в среде хлорсодержащих органических растворителей при мольном соотношении 2,3-триметилбензилхлорид : триметилсилилимидазол : TiCl4 1,0:4,0-5,0:3,6-4,5. Технический результат: разработан улучшенный способ получения медетомидина, отличающийся высоким выходом целевого продукта. 1 з.п. ф-лы, 1 табл., 1 пр.

ТРИЦИКЛИЧЕСКИЕ ДИКАРБОНИЛЬНЫЕ ПРОИЗВОДНЫЕ И ЛЕКАРСТВЕННЫЙ ПРЕПАРАТ НА ИХ ОСНОВЕ

Использование: в медицине в качестве защитных веществ для нервной системы. Раскрыты трициклические дикарбонильные производные формул Ia, Ib, II, где R1 и R2 каждый независимо друг от друга обозначают водород, (низший)алкил, (низший)алкокси, нитро, трифторметил, амино, галоген и R2 может дополнительно обозначать морфолино, 5- или 6-членный гетероцикл с 1 - 3 атомами азота, необязательно замещенный (низшим)алкилом, гидроксигруппой, или группу -NR5R6, где R5 и R6 могут быть идентичными или различными и обозначают водород, (низший)алкил, и Х в формуле II обозначает -CH=CH-, -CH=N-, -NH-, -CO- или -О-, а также фармацевтически приемлемые соли соединений общих формул Ia, Ib и II, за исключением 2,3,5,6-тетрагидро[1,2,4]триазол[1,5-с] хиназолин-2,5-диона, а также лекарственный препарат на их основе. 2 с. и 9 з.п. ф-лы, 3 табл.

АМИДО- ИЛИ КАРБАМИДО- ПРОИЗВОДНЫЕ, ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИЕ СОЛИ И КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ИНГИБИРУЮЩЕЙ АКТИВНОСТЬЮ В ОТНОШЕНИИ АЦИЛ-СОА:ХОЛЕСТЕРИН АЦИЛТРАНСФЕРАЗЫ

Предложены соединения формулы (I): где R1 означает алкильную группу; или группу формулы (II), (III), (IY) или (Y): и где R2, R3, R4 и R5 являются водородом или различными оорганическими группами; и их фармацевтически приемлемые соли; а также способы их получения и их использование при лечении и профилактике гиперхолестеремии и атеросклероза. 3 с. и 29 з.п. ф-лы, 32 ил., 12 табл.

ПРОИЗВОДНЫЕ БОРО-ПЕПТИДОВ, ИХ ПОЛУЧЕНИЕ И СОДЕРЖАЩИЕ ИХ МЕДИКАМЕНТ И ФАРМАЦЕВТИЧЕСКИЙ СОСТАВ

Соединения, отвечающие формуле I, приведенной в описании, в форме оптических или геометрических изомеров, представленных в чистой форме или в форме смесей, а также солей, образующихся при добавлении к ним фармацевтически приемлемых кислот и оснований. Терапевтическое применение.

ПРОИЗВОДНЫЕ 1-N-ФЕНИЛАМИНО-1Н-ИМИДАЗОЛА И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

... 1. Производное имидазола формулы (I) и его соли с кислотой и стереоизомерные формы, в которой R1 и R2 обозначают, каждый независимо, водород, (C1-C6)алкил или (C3-C8)циклоалкил; или R1 и R2 вместе образуют насыщенное или ненасыщенное 5-, 6-или 7-членное карбоциклическое кольцо; Q обозначает(CH2 )m-X-(CH2)n-A; A обозначает прямую связь, O, S, SO, SO2, NR5; X обозначает прямую связь, CF2, O, S, SO, SO2, C(O), NR5 или CR6R7; Z обозначает группу, выбранную из m и n обозначают, каждый независимо, 0, 1, 2, 3 или 4; p обозначает 1, 2, 3 или 4; q обозначает 0, 1 или 2; пунктирная линия означает, что R8 и/или R9 могут находиться в любом положении бензотиофенового кольца; R3 и R8 обозначают, каждый независимо, водород или гидрокси, циано, галоген, нитро, (C1-C6)алкил, (C1-C6)алкокси, трифторметил, (C1-C6)алкилтио, (C1-C6 )алкилсульфонил, ацил, (C1-C6)алкоксикарбонил, карбоксамидо, OPO(OR10)2, NR10R11, SO2NR10R11, OSO2NR10R11, OSO2OR10, SO2OR10, SSO2NR10R11, CF2SO2OR10, CF2SO2NR10R11, CF2-тетразолил ...

ПРОИЗВОДНЫЕ ФЕНИЛ-ИМИДАЗОЛИДИНОНА, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Изобретение относится к новым производным 1-имидазолил-алкил-З-фенил-имидазoлидин-2-онов общей формулы I, где n = 1,2 или 3, каждый из R , Rи R, которые могут быть одинаковыми или различными, представляет собой водород, галоген, гидрокси, циано, C- C-алкил, CF, C- C-алкокси, C-C-алкилтио, формил, C- C-алканоил, карбокси, C- C-алкоксикарбонил, нитро, - N(RR), где каждый из Rи Rнезависимо представляет собой водород, C- C-алкил, формил или C- C-алканоил; или группу (RR)N - SO, где каждый из Rи Rнезависимо представляет собой водород или C- C-алкил; Rпредставляет собой имидазольную группу формулы (а) или (b), где каждый из Rи R, которые могут быть одинаковыми или различными, представляет собой водород или C- C-алкил, R- водород, C- C-алкил или азотозащитная группа, или к их фармацевтически приемлемым солям, указанные производные полезны в применении в качестве средства для лечения расстройств центральной нервной системы, таких как, например, тревога и психоз, и для лечения расстройств подвижности ...

АРАЛКИЛБЕНЗИЛОВЫЕ ПРОСТЫЕ ЭФИРЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, ПРИМЕНЕНИЕ ТАКИХ СОЕДИНЕНИЙ, СПОСОБЫ ЛЕЧЕНИЯ И/ИЛИ ПРОФИЛАКТИКИ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ЛЕКАРСТВЕННЫЙ ПРЕПАРАТ, СОДЕРЖАЩИЕ ЭТИ СОЕДИНЕНИЯ

... 1. Бензиларалкиловые простые эфиры, характеризующиеся Формулой (1):их соли, сольваты, пролекарства, сложные эфиры, энантиомеры и/или фармацевтически приемлемые диастереоизомеры, гдеAr представляет собой, арил, имидазолил, 1,2,4-триазолил и бензимидазолил;R, R, Rи Rнезависимо представляют собой водород, галоген, Cалкил;Rявляется заместителем, который представляет собой галоген, Cалкил или О-R′, в котором R′ представляет собой водород или низший алкил;Rпредставляет арил или замещенный арил, трифторметил, трихлорметил или О-R′, в котором R′ представляет собой водород или низший алкил; при этом заместителем арила являются галоген или радикал тетразолил;n и m независимо представляют целое число от 0 до 5;при условии, что когда Ar представляет собой имидазолил, Rпредставляет собой хлор, Rпредставляет собой n-фенил, и R, R, Rn Rпредставляют водород, n должно быть отлично от 2, и/или когда n и m отличны от 0 и 1, Rили Rмогут быть представлены заместителями, которые необязательно равны, и/или когда ...

ЗАМЕЩЕННЫЕ 2-ГИДРОКСИ-3[1-(1Н-ИМИДАЗОЛ-4-ИЛ)АЛКИЛ]-БЕНЗОЛКАРБОКСИМИДАМИДЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ

Изобретение относится к новым замещенным 2-гидрокси-3-[1-( 1H-имидазол-4-ил)-алкил]-бензолкарбоксимидамидам и их солям, к способам их получения и содержащим их глазным композициям. Эти новые соединения отвечают обшей формуле I: в которой R1 - водород или С1-C4-алкил; R< Mv>2 - водород, гидроксил, амино-группа или C1-C4- алкил; R3 - водород; R2 и R3 - -CH2-CH2. Эти соединения способны снижать внутриглазное давление и могут использоваться при лечении и профилактике глаукомы.

ПРОИЗВОДНЫЕ 1-(АРИЛАЛКИЛАМИНОАЛКИЛ)ИМИДАЗОЛА, СПОСОБ ИХ ПОЛУЧЕНИЯ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ЛЕЧЕНИЯ

Изобретение касается соединений формулы и фармацевтически приемлемых солей этих соединений, где R1, R2 и R3 - независимые друг от друга водород, галоген, алкокси, фенокси, фенил, алкоксикарбонил, - NR13 R14, галоидированный алкокси, галоидированный алкил, бензилокси, гидрокси, гидроксиалкил, (C2-6-алкоксикарбонил)винил, -S(O)nR7, карбамоилалкил, алкоксикарбонилалкил, -CONR11R12, или R1 и R2 вместе с фенильным кольцом - нафтилогруппа, R4 и R5 - независимые друг от друга водород, алкил, фенил или вместе с атомом углерода представляют собой C3-6-циклоалкил, R6 - водород, алкил или ω -гидроксиалкил, А - C2-9-алкилен, R8 - водород, алкил, галоген, алкокси, гидроксиалкил, бензил или фенил, R9 и R10 - независимые друг от друга водород, алкил, галоген, алкокси, фенил, гидроксиалкил, алкоксикарбонил, нитро, -NR30R31, аллканоилоксиалкил или аминометил, которые являются противовоспалительными и антиаллергическими средствами. Описаны также составы, содержащие эти соединения и способы их получения.

Способ получения 2-ундецилимидазола

Изобретение касается производного имидазола, в частности получения 2-унде- цилимидазола. который находит применение в качестве стабилизатора полимеров. отвердителя эпоксидных смол, ингибитора коррозии металлов. Цель - упрощение процесса . Реакцию взаимодействия этилендиа- мина с 40-45%-ным бензольным раствором лауриновой кислоты ведут в аппарате непрерывного действия в токе водорода на алюмоплатиновом катализаторе при 350- 400°С,.при молярном соотношении лауриновой к-ты и этилендиамина 1:(1.15-1,60) с выделением целевого продукта охлаждением реакционной смеси в холодильнике-сепараторе барботажного типа, содержащем в качестве растворителя воду, этанол, изо- пропанол или их смесь. Эти условия обеспечивают проведение процесса в одну стадию без выделения промежуточного 2-ундецили- мидазолина с выходом 88%. 1 ил. ё ...

Гидробромид 2-(пара-хлорфенил)-5Н-имидазо(2,1-а)изоиндола, обладающий свойствами ингибитора кислотной коррозии

Использование: в качестве ингибитора кислотной коррозии. Сущность изобретения: Продукт гидробромид 2-пара-хлорфе- нил-5Н-имидазо-(2,1-а) изоиндола, БФ CieHi2N 2BrCI выход 60,5%, т.пл. 301- 302°С. Реагент 1 а-бром-п-хлорацетофе- нон. Реагент 2 З-амино-1 Н-изоиндол Условия реакции: в среде хлороформа. 1 табл.

Способ получения цинковой соли 5-метилимидазола

СПОСОБ ПОЛУЧЕНИЯ ЦИНКОВОЙ СОЛИ 5-МЕТИЛИМИДАЗОЛА путем взаимодействия карбонильного соединения с аммиаком, формальдегидом и гидроокисью цинка, отличающийся тем, что, с целью повьппения чистоты целевого продукта и упрощения процесса , в качестве карбонильного соединения используется dt-этоксиакролеин , водный раствор которого последовательно обрабатывают каталитическим количеством соляной кислоты при 3540 С , избытком аммиака, зквимолярным количеством формальдегида при 4550с и гидроокисью цинка.

Способ получения производных имидазола или их солей

Способ получения нафталин-,бензофуран-или бензо-/ @ /-тиофенкарбоновых кислот или их фармацевтически допустимых солей

Способ ползгчения нафталин-, бензофуран- или бензо- Ь -тиофенкарбоновых кислот общей формулы где у присоединен к кольцу А, и означает -СООН, -СОО(С -С -алкил), X-0,S или , R .присоединен к атом углерода кольца В, означает водород. где R и X имеют указанные -значения;. Q - галоид, С -С -алкилсульфонилокси или ArSOjO, где Аг - фенил, возможно g замещенный 1 или 2 заместителями, выбранными из группы С -С -алкила, СП С -С -алкокси и галоида, а группы (С -С -алкш1)-0-С , и CHjQ присоединены соответственно к атому углерода колец А и В, подвергают взаимодейS ствию либо с имидазолом в присутствии дополнительного основания, либо с металлсодержащей солью имидазола, ;О 4 после чего при необходимости полученный продукт переводят в соединение формулы I, где Y- группа -СОСИ, ьо м путем кислотного или щелочного гидролиза или соединение формулы I пере00 водят в фармацевтически допустимую соль.

Способ получения азоловых соединений или их кислотно-аддитивных солей,их простых или сложных эфиров

Изобретение касается азоловых соединений (АС) .в частности соединений общей формулыHC N-CH Y-N-CH,.-c(ОН-) (CRi -t )L, где К - -СНг-СН -СНг JL Н, - С,-С5.-алкил или циклопропил; RZ. - водород или С -Су-алкил; R, и Rg вместе - (СН) 5 RB галоген; R - водород или галоген; Y N, или их кислотно-аддитивных солей, их простых или сложных эфиров, которые обладают антимикотическит ми свойствами. Для повьппения фун- гицидной -активности были получены новые АС. Их синтез ведут из соответствующего незамещенного азола.и замещенного оксирана в среде оргаИИ- ческого инертного растворителя (дн- метилформа1 д) при температуре от комнатной до температуры кипеМия реакционной массы в присутствии KjCOs с выделением АС в свободном виде или в виде простого или Сложного эфира. Испытания АС показывают, что их активность выше активности стандарта - 1-циклогексилметил-вг.- (п-метилфенил)-1Н-1, 2,4-триазол-1- этанола против мучнистой росы вийо- града и хлебных злаков. 3 табл. О) ...

Способ борьбы с нежелательной растительностью

Способ получения имидазолпроизводных или их фармацевтически приемлемых солей с кислотами

Изобретение относится к гетероциклическим соединениям, в частности к получению имидазолпроизводных ф-лы Н3С NYN-N-CH-C Rs «ч Кэ v -см3 он -СН-, Н3с ч. где R и RC каждый - низший ал кил, R-y-H и или RJ + 4 дополнительная связь между С и N, Rg-- H, низшие : алкил или алкилтио, или их фармацевтически приемлемых солей с кислотами , которые могут найти применение для лечения и предупреждения воспалении и отеков. Цель - разработка способа получения соединений, обладающих активностью, не характерной для данного ряда соединений. Получение ведут конденсацией соединения ф-лы (NH(2), где Rs - указано выше, с соответствующим альдегидом . Полученное соединение выделяют или восстанавливают. В случае, когда низшая алкилтиогруппа, процесс ведут с отщеплением низшей .;. алкнлтиогруппы или дегидрированием с получением целевых продуктов в свободном виде или в виде фармацевтически приемлемой соли. 2 табл. Ё ...

Способ получения производных имидазола

Фунгицид

Способ получения производных имидазола

Гербицидное средство

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 ...

VERWENDUNG VON HETEROCYCLISCH OMEGA, OMEGA'-DISUBSTITUIERTEN P-OLIGOPHENYLENEN ALS STRAHLENUMWANDLER

BIOCIDE N-THIOCYANATOMETHOXI-AZAHETEROCYCLEN

VERFAHREN ZUR HERSTELLUNG VON IMIDAZOLYL-METHAN-DERIVATEN

1-[N-(4-Chlor-2-trifluormethylphenyl)-phenylacetimidoyl]-imidazol und seine Metallkomplexe,Verfahren zur Herstellung dieser Verbindungen sowie deren Verwendung in Fungiziden

SUBSTITUTED ALKANYL-AZOLYL CARBAMATES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS INSECTICIDES, ACARICIDES AND NEMATOCIDES

CYCLOALKYLENAZOLE, VERFAHREN ZU DEREN HERSTELLUNG, PHARMAZEUTISCHE PRAEPARATE, DIE DIESE ENTHALTEN SOWIE IHRE VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN

VERFAHREN ZUR HERSTELLUNG VON 4-METHYLIMIDAZOL

FUNGIZIDE MITTEL

VERFAHREN ZUR HERSTELLUNG VON N-(OMEGA-(1H-IMIDAZOL-1-YL)-ALKYL)-ARYLAMIDEN

(HETERO)ARYLOXYNAPHTHALINE MIT UEBER SCHWEFEL GEBUNDENEN SUBSTITUENTEN.

NEUE POLYZYKLISCHE INDANYLIMIDAZOLE MIT ALPHA2 ADRENERGIK AKTIVITÄT

VITRONEKTINREZEPTORANTAGONISTEN

VERFAHREN ZUM OPTISCHEN AUFHELLEN VON ORGANISCHEN MATERIALIEN

PREPARATION OF TERTIARY ALKYL ESTERS OF ALPHA-ISOTHIOCYANATE CARBOXYLIC ACID

... 1309994 - Isothiocyanate carboxylic acid esters; N,N - thiocarbonyldi - imidazole STAMICARBON NV 19 April 1971 [18 Feb 1970] 23566/71 Heading C2C Novel t-alkyl esters of -isothiocyanate carboxylic acids of the formula wherein R 3 is a C 4-7 t-alkyl group, R 1 is a hydrogen atom or a residue of an amino acid and R 2 is a hydrogen atom or an optionally substituted C 1-3 alkyl group, are prepared by reacting the corresponding amino acid esters with phosgene or with heterocyclic thiocarbonyl compounds. N,N - Thiocarbonyldi - imidazole may be obtained by reacting thiophosgene with imidazole.

USE OF OLEFINIC COMPOUNDS

N-TRITYLIMIDAZOLES

... 1,261,500. Imidazole derivatives. FARBENFABRIKEN BAYER A.G. 29 Jan., 1969 [29 Jan., 1968], No. 43215/71. Divided out of 1,260,588. Heading C2C. Novel imidazole derivatives of the formula wherein R is C 1-3 alkyl are prepared by reacting the appropriate trilyl halides with imidazole in inert polar organic solvents at temperatures of from 0‹ to 100‹ C., in the presence of acidbinding agents. Fungicidal compositions contain the above novel compounds in admixture with solid diluents or carriers or in admixture with liquid diluents or carriers.

Chemical process for the preparation of Medetomidine

USE OF ATIPAMEZOLE

1 5-DISUBSTITUTED IMIDAZOLE DERIVATIVES & PROCESS FOR THEIR PREPARATION

TRIAZOLES AND IMIDAZOLES

... 1468129 Triazole and imidazole derivatives UPJOHN CO 24 April 1975 [3 June 1974] 16945/75 Heading C2C Novel compounds of formulae I and II in which R and R 1 are each H or taken together represent =N-NR 2 R 3 , in which R 2 is H or C 1-3 alkyl and R 3 is C 1-3 alkyl, R 4 , R 5 , R 6 and R 7 are each H, halogen, NO 2 or CF 3 , R 8 is C 1-3 alkyl, cyclopropyl, CH 2 OH or -(CH 2 ) n -NR 9 R 10 , in which R 9 and R 10 are C 1-3 alkyl and n is 1 to 3, R 11 is H, C 1-3 alkyl, CH 2 OH or and R 12 is H, cyclopropyl, C 1-3 alkyl, CH 2 OH or (CH 2 ) n -NR 9 R 10 , and pharmacologically acceptable acid addition salts thereof, are prepared by reacting a compound of formulae III or IV with a compound of formula H 2 N-NR 2 R 3 , and, if desired, converting a resulting compound into a pharmacologically acceptable salt thereof. Pharmaceutical compositions having sedative, hypnotic, anticonvulsant, tranquillizing and muscle relaxing activity, for oral, parenteral or rectal administration, comprise a compound ...

IMIDAZOLYLOXIME ETHERS HAVING ANTIMYCOTIC AND BACTERICIDAL ACTIVITY

... 1514870 Imidazolyl-oxime SIEGFRIED AG 23 Dec 1976 [24 Dec 1975] 52951/76 Heading C2C Novel compounds of Formula I in the form of either of their possible geometric isomers or a mixture thereof in free base form or salt form as a result of reaction with an acid, in which general formula: "alk" denotes an alkylene chain containing from 1 to 4 carbon atoms, A denotes an aromatic or heteroaromatic ring system containing from 1 to 3 rings and which is optionally substituted by one or more radicals which is/are halogen, nitro, alkyl or alkoxy containing from 1 to 6 carbon atoms, cycloalkyl, phenyl or phenoxy, said cycloalkyl, phenyl or phenoxy radicals optionally being substituted in their turn by one or more radicals which is/are halogen, nitro or alkyl or alkoxy containing from 1 to 6 carbon atoms, and B denotes either a group of formula wherein R is a saturated or unsaturated aliphatic group containing up to 8 carbon atoms, A has the aforesaid meaning, Z is a direct chemical linkage or an ...

METHOD FOR PREPARATION OF 4-SUBSTITUTED-3-ANILINO-5-PYRAZOLONES

... 1455967 4 - Substituted - 3 - arylamine- 5-pyrazolones FUJI PHOTO FILM CO Ltd 14 Jan 1975 [14 Jan 1974] 1636/75 Heading C2C [Also in Division G2] 4 - Substituted - 3 - arylamino - 5 - pyrazolone represented by the general Formula (I) wherein R1 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted aralkyl group or an optionally substituted aryl group; R2 represents one or two substituents selected from a hydrogen or halogen atom, and alkyl, alkoxy, alkylthio, alkylsulphonic acid, carbamido, acylamino, cyano, alkoxycarbonyl, sulphonamino, sulphamoyl, diacylamino, carbamoyl, carboxy, sulpho and nitro groups; and Y represents an alkylamino, dialkylamino, sulphonamino, acylamino, diacylamino, arylamino or diarylamino group, or a nitrogen-containing heterocyclic group bonded via the nitrogen atom in the heterocyclic ring or a releasable group bonded via an oxygen atom, some of which are novel, are prepared by conducting a ring-closing ...

IMIDAZOLE COMPOUNDS

IMIDAZOLE DERIVATIVES AND SALTS THEREOF THEIR SYNTHESIS AND INTERMEDIATES AND PHARMACEUTICAL FORMULATIONS

Inhibiting hydrocarbon hydrate agglomeration

A process for inhibiting the formation of gas hydrates in a hydrocarbon fluid comprising adding to the hydrocarbon fluid, a gas hydrate anti-agglomerate which is a biodegradable anti-agglomerant derived from a naturally occurring substance.

Fungicidal Azolylméthylcyclopentane benzylidene. Benzolidene azolylméthylcycloalcane and use as fungicide.

Manufactoring process of derived from imidazol and products obtained.

Apoptosis signal-regulating kinase inhibitor

Heteroaryl succinamides and their use as metalloprotein ase inhibitors

Endothelin receptor antagonistis.

Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Heteroaryl succinamides and their use as metalloproteinase inhibitors.

The present invention is directed to compound of formula (i), wherein r1, r2, r3, r4, r5, x, y and (1a)are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.

Substituted N-[(Aminoiminomethyl or aminomethyl) Phenyl] Propyl amides.

This invention relates to compounds of formula (I) which inhibit Factor Xa, to pharmaceutical compositions containing the compounds, and to the use of the compounds for the treatment of patients suffering from conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.

ENDOTHELIN RECEPTOR ANTAGONISTS

Proatease inhibitors.

The present invention provides compounds which inhibit proteases, including cathepsin k, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Heteroaryl succinamides and their use as metalloprotein ase inhibitors

Vitronectin receptor antagonists.

Substituted n-[(aminoiminomethyl or aminomethyl) phenyl]propyl amides

Vitronectin receptor antagonists

Apoptosis signal-regulating kinase inhibitor

Apoptosis signal-regulating kinase inhibitor

Substituted n-Ä(aminoiminomethyl or aminomethyl)p henylÜpropyl amides

Method of preparation of N (Tertiary sector-Aminoalkyl) - Dioxybenzamides Methylene.

Heteroaryl succinamides and their use as metalloproteinase inhibitors

New useful acetanilides like weedkillers.

ENDOTHELIN RECEPTOR ANTAGONISTS

Fungicidal compounds and compositions.

New derivatives of imidazol, proceeded for their preparation and application as fungicidal agents.

Protease inhibitors

Imidazole derivatives and their use as cytokine inhibitors

NOVEL COMPOUNDS

Substituted n-[(aminoiminomethyl or aminomethyl) phenyl]propyl amides

Vitronectin receptor antagonists

ENDOTHELIN RECEPTOR ANTAGONISTS

NOVEL COMPOUNDS

PROCEDURES FOR THE PRODUCTION OF NEW N-SUBSTI TUIERTEN HALOGENACETANILIDEN

PROCEDURE FOR THE PRODUCTION OF NEW IMIDAZOL DERIVATIVES AND THEIR METAL COMPLEXES

FUNGICIDES COMPOSITION

PROCEDURE FOR THE PRODUCTION OF NEW ARALI PHA TABLES MORPHOLINOVERBINDUNGEN, THEIR SAEUREADDITIONSSALZEN AND OPTICAL ACTIVE EN CONNECTIONS

PROCEDURE FOR the PRODUCTION OF NEW ONE 1-ARYL-2 (1 - IMIDAZOLYL) - ALKYL SULFIDES, OF THEIR SAEURE ADDITION SALTS AND OPTICAL ACTIVE EN CONNECTIONS

PROCEDURE FOR MANUFACTURING NEW ONE 1-ARYL-ALKYL-IMIDAZOLDERIVATEN AND THEIR SALTS

PROCEDURE FOR the PRODUCTION of NEW ALPHA ARYL ALPHA (CYCLOPROPYLMETHYL) - 1H-AZOL-1-ETHANOLE

PROCEDURE FOR THE PRODUCTION OF NEW IMIDAZOLDERIVATEN AND THEIR SALTS

ORGANIC SULFATES AS IONI LIQUIDS

2-HALOGENACETAMID-HERBIZIDE

PROCEDURES FOR the PRODUCTION OF NEW ONE 1-SUBSTITUIERTEN IMIDAZOLDERIVATEN AND THEIR SALTS

PROCEDURE FOR THE TREATMENT OF GLAUKOM

HERBIZID

VERFAHREN ZUR HERSTELLUNG VON NEUEN AZOLYL-9,10 -DIHYDROANTHRACEN-DERIVATEN UND DEREN SALZEN

Volatile Imidazoles and Group 2 Imidazole Based Metal Precursors

Sterically hindered imidazole ligands are described, along with their synthesis, which are capable of coordinating to Group 2 metals, such as: calcium, magnesium, strontium, in an eta-5 coordination mode which permits the formation of monomeric or dimeric volatile complexes. A compound comprising one or more polysubstituted imidazolate anions coordinated to a metal selected from the group consisting of barium, strontium, magnesium, radium or calcium or mixtures thereof. Alternatively, one anion can be substituted with and a second non-imidazolate anion. Synthesis of the novel compounds and their use to form BST films is also contemplated

Photoredox-Catalyzed Direct C-H Functionalization of Arenes

The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron donating group is selected from —OH claim 1 , —SH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 thioalkoxy claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , —OC(═O)R claim 1 , —NHC(═O)R claim 1 , and Ar;{'sup': 6', '7, 'wherein each of Rand Ris independently selected from C1-C8 alkyl; and'}{'sup': '2', 'wherein Aris selected from aryl and heteroaryl and substituted with 0, 1, 2, or 3 groups independently selected from halogen and C1-C8 alkyl.'}3. The method of claim 1 , wherein Z is F.48-. (canceled)12. (canceled)13. The method of claim 1 , wherein the fluoride is selected from ammonium fluoride claim 1 , cesium fluoride claim 1 , and triethylamine hydrofluoride.1415-. (canceled)16. The method of claim 1 , wherein the oxidant is molecular oxygen.17. The method of claim 1 , wherein the oxidant is 2 claim 1 ,2 claim 1 ,6 claim 1 ,6-tetramethyl-1-piperidinyloxy radical (TEMPO).1820-. (canceled)21. The method of claim 1 , wherein Z is —CN.29. The method of claim 1 , wherein the compound is isotopically-labeled.30. The method of claim 25 , wherein the compound contains a radioactive isotope.31. The method of claim 1 , wherein the compound is not isotopically-labeled. This application is a continuation of U.S. application Ser. No. 15/826,092, filed Nov. 29, 2017, which is a continuation of International Application No. PCT/US2016/035549 with an international filing date of Jun. 2, 2016, which claims priority to U.S. Provisional Application No. 62/170,632 filed on Jun. 3, 2015, the contents of which are incorporated ...

Compounds and Methods for Treating Cancer and Diseases of the Central Nervous System

Disclosed are compounds of the general formula (I): 132-. (canceled)3436-. (canceled)37. The method of claim 33 , wherein D is 1 claim 33 ,3-imidazolyl.38. The method of claim 33 , wherein n is 3 to 4.39. The method of claim 33 , wherein n is 4.40. The method of claim 33 , wherein T is substituted with perfluoroalkyl.41. The method of claim 33 , wherein T is selected from the group consisting of: 4-chlorophenyl claim 33 , 3-methoxyphenyl claim 33 , 2-amino-4-chlorophenyl claim 33 , 4-methoxyphenyl claim 33 , phenyl claim 33 , 4 fluorophenyl claim 33 , 4-bromophenyl claim 33 , 4-iodophenyl claim 33 , 2-hydroxyphenyl claim 33 , 4-nitrophenyl claim 33 , biphenyl-4-yl claim 33 , 3 claim 33 ,4-dichlorophenyl claim 33 , 4-isopropylphenyl claim 33 , 4-tert-butylphenyl claim 33 , 4-hydroxyphenyl claim 33 , 4-(trifluoromethyl)phenyl) claim 33 , and 4-benzoylphenyl.42. (canceled)43. The method of claim 33 , wherein said compound is selected from the group consisting of: 4-(4-chlorophenyl)-1-(1H-imidazol-1-yl)butane hydrochloride (QC-105); 1-(3-Phenyl-propyl)-1H-imidazole hydrochloride (QC-172); 1-[4-(4-Bromo-phenyl)-butyl]1H-imidazole hydrochloride (QC-199); 1-[4-(4-(Trifluoromethyl)phenyl)butyl]-1H-imidazole hydrochloride (QC-234); and pharmaceutically acceptable salts thereof.44. The method of claim 33 , wherein said compound is 1-[4-(4 Bromo-phenyl)-butyl]-1H-imidazole hydrochloride (QC-199); or pharmaceutically acceptable salts thereof.45. The method according to claim 33 , wherein the disease is Alzheimer's disease.4689-. (canceled)90. The method according to claim 33 , wherein the disease is Parkinson's disease.91. The method of claim 40 , wherein T is substituted with Br.92. The method of claim 40 , wherein T is substituted with Cl. This invention is in the field of pharmaceuticals, and relates to compounds and compositions for treating/mitigating cancer and for suppressing tumor growth. The invention also relates to compounds, compositions and methods for the ...

PHOTOREDOX-CATALYZED DIRECT C-H FUNCTIONALIZATION OF ARENES

The invention generally relates to methods of making substituted arenes via direct C—H amination. More specifically, methods of making para- and ortho-substituted arenes via direct C—H amination are disclosed. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 2. The method of claim 1 , wherein the electron donating group is selected from —OH claim 1 , —SH claim 1 , —NH claim 1 , C1-C8 alkyl claim 1 , C1-C8 alkoxy claim 1 , C1-C8 thioalkoxy claim 1 , C1-C8 alkylamino claim 1 , (C1-C8)(C1-C8) dialkylamino claim 1 , —OC(═O)R claim 1 , —NHC(═O)R claim 1 , and Ar;{'sup': 6', '7, 'wherein each of Rand Ris independently selected from C1-C8 alkyl; and'}{'sup': '2', 'wherein Aris selected from aryl and heteroaryl and substituted with 0, 1, 2, or 3 groups independently selected from halogen and C1-C8 alkyl.'}3. The method of claim 1 , wherein Z is a halogen.4. The method of claim 3 , wherein the halogen is selected from fluorine and chlorine.5. The method of claim 1 , wherein Z is selected from C1-C4 alkylamino claim 1 , C1-C4 dialkylamino claim 1 , arylamino claim 1 , diarylamino claim 1 , and C1-C4 alkarylamino.6. The method of claim 1 , wherein Z is —NH.7. The method of claim 1 , wherein Z is Ar.8. The method of claim 7 , wherein Aris selected from pyrazole claim 7 , 1 claim 7 ,2 claim 7 ,3-triazole claim 7 , 1 claim 7 , 2 claim 7 , 4-triazole claim 7 , benzotriazole claim 7 , imidazole claim 7 , and benzimidazole.12. The method of claim 1 , wherein the nucleophile is a halide.13. The method of claim 12 , wherein the halide is selected from ammonium fluoride claim 12 , cesium fluoride claim 12 , lithium chloride claim 12 , triethylamine hydrochloride claim 12 , and triethylamine hydrofluoride.14. The method of claim 1 , wherein the nucleophile is an amine.15. The method of claim 14 , wherein the amine is ammonium bicarbonate.16. The method of claim 1 , wherein the ...

Process for Preparing Asymmetrical Imidazolium Salts

The invention relates to a process for preparing an asymmetrical imidazolium salt of formula (1A), in which R1 is an aromatic group, R2 is chosen from a cyclic secondary aliphatic alkyl group and a heteroalkyl group, R3 and R4 are chosen, independently of one another, from the group consisting of hydrogen, a halide and an alkyl group, and A″ is an anion. The process comprises a fast substep of forming a reaction mixture by bringing one equivalent of an aniline into contact with one equivalent of a compound bearing an amine group, in the presence of at least four point five equivalents of a Brønsted acid. The process also comprises a second substep of forming a solution comprising one equivalent of a dicarbonyl, one equivalent of formaldehyde, and at least four point five equivalents of the Brønsted acid, and adding thereto the reaction mixture formed in the first substep. The mixture is left to stir for a predetermined time at a predetermined temperature. The intermediate asymmetrical imidazolium salt 1A is then isolated.

METHOD OF PREPARING A HIGH PURITY IMIDAZOLIUM SALT

The present invention encompasses a novel method for synthesizing highly pure salts of the general formula QA, wherein Q is: 2. The process of claim 1 , wherein R=R=R=hydrogen and wherein each of R claim 1 , R claim 1 , R claim 1 , Rare independently methyl or ethyl.3. The process of claim 2 , wherein R=R=R=hydrogen claim 2 , R=methyl and wherein each of R claim 2 , R claim 2 , Rare independently methyl or ethyl.4. The process of claim 1 , wherein step a) is carried out in the absence of a solvent.5. The process of claim 1 , wherein step a) is carried out in the presence of a solvent.6. The process of claim 5 , wherein the solvent is at least partially removed between steps a) and b).7. The process of claim 1 , wherein claim 1 , in step b) claim 1 , water is added in an amount of at least 1 weight-% based on the amount of compounds (II) and (III) used in step a).8. The process of claim 1 , wherein “partial removal” in step c) means removal of at least 50% of the water added in step b).9. The process of claim 1 , wherein pressure pis lower than the saturated vapour pressure of compound (III) at the temperature Tand higher than the saturated vapour pressure of (I) at the temperature T.10. The process of claim 1 , wherein steps b) and c) are carried out at least twice claim 1 , and wherein step b) is carried out with the high purity compound of formula (I) obtained in directly antecedent step c).11. The process of claim 2 , wherein said process is carried out in the absence of an organic solvent.12. The process of claim 11 , wherein in step b) water is added in an amount of at least 1 weight-% based on the amount of compounds (II) and (III) used in step a).13. The process of claim 12 , wherein “partial removal” in step c) means removal of at least 50% of the water added in step b).14. The process of claim 13 , wherein pressure pis lower than the saturated vapour pressure of compound (III) at the temperature Tand higher than the saturated vapour pressure of (I) at the ...

ELUXADOLINE CRYSTALLINE FORMS AND PROCESSES FOR THEIR PREPARATION

Novel crystalline forms of Eluxadoline, having the formula (I), are described. Also described are the processes for the preparation of said crystalline forms. 1. A polymorphically and chemically stable crystalline form α′ of 5-({[(2S)-2-amino-3-(4-carbamoyl-2 ,6-dimethylphenyl)propanoyl][(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]-amino}methyl)-2-methoxybenzoic acid having an X-ray powder diffraction pattern that , when collected with Kα radiation of copper (λ=1.5418 Å) comprises main peaks at 7.98° , 13.94° , 14.28° , 14.66° , and 19.04° 2θ±0.1° 2θ.3. A solvate form of 5-({[(2S)-2-amino-3-(4-carbamoyl-2 ,6-dimethylphenyl)propanoyl][(1S)-1-(4-phenyl-1H-imidazol-2-yl)ethyl]amino}methyl)-2-methoxybenzoic acid with a ketone selected from the group consisting of acetone , 2-butanone , 3-pentanone and mixtures thereof.4. The solvate form according to claim 3 , wherein the solvate form is an acetone solvate having unit cell parameters equal to the following cell dimensions: a=24.18 ű0.01 Å; b=17.10 ű0.01 Å claim 3 , c=9.62 ű0.01 Å; α=90 degrees claim 3 , β=90 degrees; γ=90 degrees.5. The solvate form according to claim 4 , wherein the solvate form in an X-ray powder diffraction pattern collected with Kα radiation of copper (λ=1.5418 Å) comprises main peaks at 6.33° claim 4 , 8.92° claim 4 , 9.86° claim 4 , 12.80° claim 4 , and 18.04°+0.1° 2θ.6. The solvate form according to claim 5 , wherein the X-ray powder diffraction pattern further comprises peaks at 7.280 claim 5 , 8.92° claim 5 , 13.82° claim 5 , and 15.06°+0.1° 2θ.7. The solvate form according to claim 4 , wherein the solvate form in a DSC thermogram performed with a heating ramp of 10° C./min comprises a first feature with maximum at 122.9° C.±4.0° C. claim 4 , an event with maximum at 173.7° C.±4.0° C. claim 4 , and a second feature with maximum at 196.6° C.±4.0° C.8. The solvate form according to claim 4 , wherein the solvate form in a TGA thermogram shows a weight loss step between 25° C. and 120° C. of up to ...

Derivatives of N-alkyl imidazoles

Compounds of the formula ##STR1## wherein R is lower alkyl; R 1 is substituted or unsubstituted phenyl or phenyl straight chain lower alkyl; R 2 is substituted or unsubstituted phenyl, phenyl straight chain lower alkyl or phenyl straight chain lower alkenyl; and wherein said substitution, solely in the phenyl ring of the aforesaid groups, comprises one or more substituents independently selected from the group consisting of lower alkyl, lower alkoxy, halo and trifluoromethyl; X is oxygen or sulfur; n is an integer of from 1 to 4 with the proviso that n cannot be 1 when X is oxygen and R 1 is phenyl or substituted phenyl; and the antimicrobial acid addition salts thereof are useful as antifungal antibacterial and antiprotozoal agents.

GROUP 8-10 TRANSITION METAL CATALYST FOR THE POLYMERIZATION OF OLEFINS

Organic sulfates as ionic liquids

The invention relates to novel ionic liquids of general formula [cation] [R'-SO4], wherein R' represents a branched or linear, saturated or unsaturated, aliphatic or alicyclic, functionalised or unfunctionalised hydrocarbon chain having between 3 and 36 carbon atoms. Said novel ionic liquids can, for example, be used as solvents or solvent additives in chemical reactions, as extracting agents or as heat transfer media.

Halogenide-free preparation of ionic fluids

Preparation of ionic liquids (I) involves alkylating an amine, phosphine, imidazole, pyridine, triazole or pyrazole corresponding to the cation of (I) with a sulfate diester (II), then replacing the sulfate anion by the anion of (I). Preparation of ionic liquids of formula (I) involves alkylating the amine, phosphine, imidazole, pyridine, triazole or pyrazole, corresponding to the cation A<+>, with a sulfate diester of formula (II), then replacing the sulfate anion R4SO4<-> or R5SO4<-> by the anion Yn-. (An)<+>.(Yn-) (I) R4SO2R5 (II) n = 1 or 2; Yn- = BF4<->, BCl4<->, PF6<->, SbF6<->, AsF6<->, AlCl4<->, ZnCl3<->, CuCl2<->, SO4<2->, CO3<2->, R'COO<->, R'SO3<-> or (R'SO2)2N<->; R' = 1-12C linear, branched or cyclic alkyl, 5-18C aryl, (5-18C) aryl-(1-6C) alkyl or (1-6C) alkyl-(5-18C) aryl (all optionally halo-substituted); A<-> = N<+>R1R2R3R or P<+>R1R2R3R; or 1-(R)-3-(R1)-imidazolium, (R1)-substituted 1-(R)-pyridinium, 1-(R)-2-(R1)-pyrazolium or 1-(R)-1,3,5-triazolium (all optionally ring-substituted by one or more of 1-6C alkyl, 1-6C alkoxy, 1-6C aminoalkyl, 5-12C aryl or (5-12C) aryl-(1-6C) alkyl); R1-R3 = H; 1-20C linear, branched or cyclic alkyl; Het or Het-(1-6C) alkyl; or Ar or Ar-(1-6C) alkyl; R, R4, R5 = 1-24C linear, branched or cyclic alkyl; Het-(1-6C) alkyl; or Ar'-(1-6C) alkyl; Het = heteroaryl containing 3-8C and at least one of N, O and S (optionally substituted by one or more of 1-6C alkyl and halo); Ar = 5-12C aryl (optionally substituted by one or more of 1-6C alkyl and halo); and Ar' = 5-24C aryl (optionally substituted by one or more of 1-6C alkyl and halo).

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins. Suitable complexes include those of the following structure: wherein M represents the transition metal, and Q, T, L, W, Z, R 1 ,R 2 and R 10 represent functional groups.

Catalyst compositions for the polymerization of olefins

The present invention provides catalyst systems useful in the polymerization of olefins comprising a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond from two imine groups. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. In a preferred embodiment, the catalyst system of the present invention further comprises a Lewis or Bronsted acid complexed with the ligand component of the transition metal-ligand complex.

Catalyst compositions for the polymerization of olefins

The present invention includes novel ligands which may be utilized as part of a catalyst system. A catalyst system of the present invention is a transition metal-ligand complex. In particular, the catalyst system includes a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. A catalyst system of the present invention may further comprise a Lewis or Bronsted acid. The Lewis or Bronsted acid may be complexed with the ligand component of the transition metal-ligand complex.,

Group 8-10 transition metal olefin polymerization catalysts

A composition comprising a boron or aluminum containing neutral Lewis acid and a compound of formula I or Ia: wherein R 1 and R 2 are each independently hydrocarbyl, substituted hydrocarbyl, or silyl; Q is (i) C—R 4 , where R 4 is hydrocarbyl, substituted hydrocarbyl, heteroatom connected hydrocarbyl, or heteroatom connected substituted hydrocarbyl, (ii) P(NH 2 ) 2 , or (iii) S(NH)(NH 2 ) or S(O)(OH); L is a monoolefin or a neutral Lewis base that can be displaced by a monoolefin; T is hydrogen, hydrocarbyl or substituted hydrocarbyl, or with L forms a π-allyl group; and M is Ni(II), Pd(II), Co(II) or Fe(II). The composition is useful as an olefin polymerization catalyst. Also described is a process for preparing a supported catalyst.

Microbicide

Novel 1-phenoxyphenyl-2-triazolylethanol ethers of the formula I <IMAGE> in which R1 is halogen, R2 is halogen or methyl and R3 is C1-C4-alkyl, C1-C4-haloalkyl, C2-C6-alkoxyalkyl, C3-C6-alkenyl, C3-C6-alkynyl or cyclopropyl and their phytophysiologically acceptable acid addition salts have outstanding microbicidal, in particular phytofungicidal, properties. They can be used for the control and/or preventive protection of crop plants against infections by microorganisms. The preparation of these active substances and compositions containing them are described.

CARBAMOILOXIALQUILAZOLES SUBSTITUTED BY N.

Un compuesto de la fórmula (III); (III), en donde, R1, es hidrógeno o alquilo, R2, es hidrógeno, alquilo, alquilcarboniloxialquilo, acoxicarbonilo, alquilcarbonilo, mono- ó dialquilminoalquil- carboniloxialquilo; R4 y R6, se seleccionan, de una forma independiente, de entre el grupo consistente en hidrógeno, halógeno, alquilo, alcoxi, alquiltio, alquilsulfinilo, alquilsulfonilo, carboxi, alcoxicarbonilo, ciano, trifluorometilo, trifluorometoxi, nitro, aminosulfonilo, o sulfo; R6, es hidroxi, alcoxicarbonilalquilamino, alcoxi- carbonilamino, amino, alquilamino, alquilcarboniloxi, alcoxicarbonilalquilamino-alquilcarboniloxi, alcoxicarbonil- amino-alquilcarboniloxi, alquilaminoalquilcarboniloxi, amino- alquilcarboniloxi, alquilcarbonilamino, alquilcarbonilalquil- amino, aciloxi, acilamino, acilalquilamino; el grupo es fenilo o piridini-2-ílo; X- es X- y, X-, es un anión farmacéutcimente aceptable, en donde, ¿acilo¿, se refiere a un residuo representado por la fórmula R7CO- ó (R8O)2PO-, en donde, R7, es hidrógeno, alcoxi, alquilo, el cual puede estar opcionalmente sustituido por carboxi, amino, alquilamino, dialquilamino, o fenilo, y R8, es hidrógeno o alquilo, ¿alquilo¿, se refiere a un radical hidrocarburo, saturado o insaturado, que tiene de 1 a 6 átomos de carbono, ¿alcoxi¿, se refiere a una cadena de -O-alquilo, lineal o ramificada, que tiene de 1 a 5 átomos de carbono, ¿halógeno¿, significa flúor, cloro o bromo y, ¿alquiltio¿, se refiere a un cadena de -S-alquilo, lineal o ramificada, que tiene de 1 a 4 átomos de carbono, así como sales, hidratos o solvatos, farmacéuticamente aceptables, de la fórmula (III). A compound of the formula (III); (III), wherein R1 is hydrogen or alkyl, R2 is hydrogen, alkyl, alkylcarbonyloxyalkyl, acoxycarbonyl, alkylcarbonyl, mono- or dialkyl aminoalkylcarbonyloxyalkyl; R4 and R6 are independently selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, carboxy, alkoxycarbonyl, ...

Imidazolylalkylamine derivative and pharmaceutical composition thereof

An imidazolylalkylamine derivative represented by general formula (I) useful as a steroid 17-20 lyase, a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing the same as the active ingredient, wherein R1 represents hydrogen or lower alkyl; A1 represents optionally branched lower alkylene; A2 represents optionally bonded or branched lower alkylene; R2 represents (un)substituted phenyl, (un)substituted bi- or tricyclic hydrocarbon ring having fused benzene ring(s); or (un)substituted bi- or tricyclic fused hetero ring having fused benzene ring(s) and a hetero ring containing oxygen and/or sulfur and/or nitrogen as the hetero atom(s); R3 represents alkyl, lower alkenyl, lower alkynyl, cycloalkyl, -A3-R4, halogen-substituted lower alkyl, cyano-substituted lower alkyl, or (un)substituted hetero ring containing nitrogen as the hetero atom(s); A3 represents optionally branched lower alkylene or carbonyl; and R4 represents (un)substituted cycloalkyl, (un)substituted phenyl, or (un)substituted hetero ring containing nitrogen as the hetero atom(s); provided (1) -A?2-R2 and -R3¿ may be combined with the adjacent nitrogen atom to form (un)substituted tri- or tetracyclic fused hetero ring, and (2) when -A2-R2 represent (un)substituted phenyl or benzyl, (a) is bonded to the 4- or 5- position of the imidazole ring.

Isocyanates blocked with 1-amino-alkyl imidazoles as epoxy curing agents

Novel curing agents for heat-curable single package epoxy resins, the agents being adducts of aminoalkyl imidazoles with isocyanates. Cures are effected on heating the epoxy resin for times as short as 5 seconds.

Catalyst compositions for the polymerization of olefins

The present invention includes novel ligands which may be utilized as part of a catalyst system. A catalyst system of the present invention is a transition metal-ligand complex. In particular, the catalyst system includes a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. A catalyst system of the present invention may further comprise a Lewis or Bronsted acid. The Lewis or Bronsted acid may be complexed with the ligand component of the transition metal-ligand complex.

Catalyst compositions for the polymerization of olefins

The present invention provides catalyst systems useful in the polymerization of olefins comprising a transition metal component and a ligand component comprising a Nitrogen atom and/or functional groups comprising a Nitrogen atom, generally in the form of an imine functional group. In certain embodiments, the ligand component may further comprise a phosphorous atom. Preferred ligand components are bidentate (bind to the transition metal at two or more sites) and include a nitrogen-transition metal bond. The transition metal-ligand complex is generally cationic and associated with a weakly coordinating anion. In a preferred embodiment, the catalyst system of the present invention further comprises a Lewis or Bronsted acid complexed with the ligand component of the transition metal-ligand complex.

Processo para preparação de 2,4-oxazolidinadionas e intermediário

CATALYST COMPOSITIONS FOR THE POLYMERIZATION OF OLEFINS

Indan- und tetralinderivate

Compound process for preparing same composition containing same and method of inhibiting mould

Derivatives of thienyl- and furyl-substituted N-butyl and N-phenyl imidazoles

The compounds of the present invention are represented by the formula ##STR1## wherein R 1 and R 2 are the same or different and are optionally substituted furyl or thienyl the substituents independently selected from the group halo, C 1 to C 6 alkyl and C 1 to C 6 alkoxy or optionally substituted phenyl the substituents independently selected from the group halo, C 1 to C 4 alkyl, C 1 to C 4 alkoxy and trifluoromethyl; X is oxygen or sulfur; m is the integer 0; and n is the integer 2 or 3; and the antimicrobial acid addition salts thereof, with the proviso that when either R 1 or R 2 is said optionally substituted phenyl the other R 1 or R 2 is said optionally substituted furyl or thienyl. The compounds are useful for combatting fungi, bacteria and protozoa. They also have spermatocidal and spermatostatic activity.

Microbicidal triazolyl-ethyl-ethers

Novel substituted azolyl-ethyl ethers of the general formula I <IMAGE> wherein R1 is phenyl, phenyl mono- to trisubstituted by halogen, C1-C3- haloalkyl, nitro, C1-C3-alkoxy, C1-C8-alkyl and/or cyano, or phenyl substituted by phenyl or phenoxy, naphthyl, or naphthyl mono- or -disubstituted by halogen, nitro and/or C1-C3-alkyl, benzyl, or benzyl mono- or disubstituted by halogen, nitro and/or C1-C3-alkyl; R2 is phenyl, phenyl mono- to trisubstituted by halogen, C1-C3-haloalkyl, nitro, C1-C3-alkoxy, C1-C8-alkyl and/or cyano, or phenyl substituted by phenyl or phenoxy, or it is C1-C10-alkyl, C3-C8-cycloalkyl or C3-C8- cycloalkyl-(C1-C4-alkyl); R3 is C1-C12-alkyl, C2-C4-alkenyl, C3-C4-alkynyl, benzyl, or benzyl mono- or disubstituted by halogen, nitro and/or C1-C3-alkyl; and R4 is an azolyl group; including acid addition salts thereof, quaternary azolium salts and metal complexes, are used in agrochemical compositions for the preventive and curative combating of harmful microorganisms.

Ether derivatives from substituted 1-hydroxyalkyl azoles, process for their preparation as well as their use as fungicides and plant-growth regulators

Die Erfindung betrifft neue Ether-Derivate von substituierten 1-Hydroxyalkyl-azolen, ein Verfahren zu ihrer Herstellung sowie ihre Verwendung als Fungizide und Pflanzenwachstumsregulatoren. Die Verbindungen der allgemeinen Formel <IMAGE> in welcher A, B, R¹, R², Z und m die in der Beschreibung angegebene Bedeutung besitzen, werden erhalten, wenn man Alkoholate von 1-Hydroxylalkyl-azolen mit einem Halogenid R² - Hal in Gegenwart eines Verdünnungsmittels umsetzt, und gegebenenfalls anschließend an die so erhaltenen Verbindungen der Formel (I) eine Säure oder ein Metallsalz addiert. Die Wirkstoffe sind für den Gebrauch als Pflanzenschutzmittel geeignet und können mit besonders gutem Erfolg zur Bekämpfung solcher Pilze eingesetzt werden, die echte Mehltauerkrankungen hervorrufen. Die Wirkstoffe greifen ferner in den Metabolismus der Pflanzen ein und können deshalb als Wachstumsregulatoren eingesetzt werden. The invention relates to new ether derivatives of substituted 1-hydroxyalkyl-azoles, a process for their preparation and their use as fungicides and plant growth regulators. The compounds of the general formula <IMAGE> in which A, B, R¹, R², Z and m have the meaning given in the description are obtained if alcoholates of 1-hydroxylalkyl-azoles with a halide R² - Hal in the presence of a Reacts diluent, and then optionally adds an acid or a metal salt to the compounds of formula (I) thus obtained. The active ingredients are suitable for use as crop protection agents and can be used with particularly good success to combat those fungi which cause real mildew diseases. The active substances also interfere with the metabolism of the plants and can therefore be used as growth regulators.

Antimycosic agent

1. Antimycotic agent, characterised in that it contains at least one ether derivative of a substituted 1-hydroxyalkyl-azolyl derivative of the general formula : see diagramm : EP0085843,P11,F1 in which B represents oxygen, sulphur or the CH2 group ; R**1 represents the groupings : see diagramm : EP0085843,P11,F2 and see diagramm : EP0085843,P11,F3 or represents cycloalkyl which has 3 to 7 carbon atoms and is optionally substituted by alkyl with 1 to 2 carbon atoms, and optionally substituted phenyl, the following being mentioned as substituents : halogen, alkyl with 1 to 4 carbon atoms and halogenoalkyl with 1 to 2 carbon atoms and 1 to 5 identical or different halogen atoms ; X**1 represents hydrogen or halogen, X**2 represents halogen ; Y represents alkyl, alkoxy, alkylthio, halogeno-alkoxy, halogenoalkylthio, alkenyl with up to 6 carbon atoms, alkoxycarbonyl with 1 to 4 carbon atoms in the alkyl part, cyano and optionally substituted phenyl, phenoxy, phenylthio, phenylalkoxy with 1 to 4 carbon atoms in the alkyl part and phenylalkylthio with 1 to 4 carbon atoms in the alkyl part, the following being mentioned as phenyl substituents in each case : halogen, alkyl with 1 to 4 carbon atoms ; alkoxy and alkylthio with in each case 1 to 2 carbon atoms ; halogenoalkyl, halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon atoms and 1 to 5 identical or different halogen atoms, cyclohexyl, dialkylamino with 1 to 4 carbon atoms in each alkyl part, nitro, cyano and alkoxycarbonyl with 1 to 4 carbon atoms in the alkyl part ; n represents the numbers 0, 1 or 2 ; Z represents halogen, alkyl with 1 to 4 carbon atoms, cycloalkyl with 5 to 7 carbon atoms, alkoxy and alkylthio with in each case 1 to 4 carbon atoms, halogenoalkyl and halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon atoms and 1 to 5 identical or different halogen atoms, and phenyl, phenoxy and phenylalkyl and phenylalkoxy with 1 to 2 carbon atoms in the alkyl part or in the alkoxy ...

Fungicidally active 3-substituted 1-azolyl-3-methyl-1-phenoxy-butan-2-ones and -ols

New 3-substituted 1-azolyl-3-methyl-1-phenoxy-butan-2-ones and -ols of the general formula ##STR1## in which Az represents 1,2,4-triazol-1-yl, 1,2,4-triazol-4-yl or imidazol-1-yl, B represents the keto group or the CH(OH) group, Y represents oxygen or sulphur, R represents halogenoalkyl, optionally substituted phenyl or optionally substituted benzyl, or provided Y represents sulphur, may represent alkyl and X 1 , X 2 and X 3 are selected independently and each represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio, alkylsulphonyl, nitro, cyano, alkoxycarbonyl or optionally substituted phenyl, are obtained if halogenoether ketones are reacted with 1,2,4-triazole or imidazole in the presence of a diluent and of an acid-binding agent, and, if appropriate, the keto derivatives thus obtained are reduced. The compounds, as such or as their acid-addition salts or metal-salt complexes, have fungicidal activity, for example against those fungi which cause powdery mildew diseases or cause rice diseases.

1-(beta-aryl-beta-(r-oxy)-ethyl)-imidazoles

THE COMPOUNDS ARE OF THE CLASS OF 1(B-ARYL-B-(R-OXY)ETHYL)-IMIDAZOLES, WHEREIN R IS ALKYL, ALKENYL, PHENYLALKENYL, HALOPHENYL ALKENYL OR ALKYNYL, USEFUL FOR THEIR ANTI-FUNGAL AND ANTI-BACTERIAL ACTIVITY.

1-{8 {62 -(1-adamantyloxy)halophenethyl{9 {0 imidazoles and congeners

Preparation of 1-( (3-(1-adamantyloxy)phenethyl)imidazoles and congeners- for example, 1-( Beta -(1-adamantyloxy)-4chlorophenethyl)imidazole oxalate- and 3-(1-adamantyl)-1-( ( Beta -hydroxyl)halophenethyl) imidazolium bromide by-products, together with biological properties thereof including antibacterial, antiprotozoal, anthelmintic, antifungal, and antialgal activities, are disclosed.

1-(beta-aryl)ethyl-imidazole derivatives

THE COMPOUNDS ARE OF THE CLASS OF 1-(B-ARYL)ETHYLIMIDAZOLE ETHERS AND AMINES USEFUL FOR THEIR ANTI-FUNGAL AND ANTI-BACTERIAL ACTIVITY.

Phenyl-imidazolylalkanyl derivatives

PHENYL-IMIDAZOLYLALKANYL DERIVATIVES ARE ANTIMYCOTIC AGENTS. THEY ARE PREPARED BY A NUMBER OF PROCESSES INCLUDING ACYLATION OR SULFONYLATION OF A PHENYL-IMIDAZOLYLALKANOL, TREATMENT OF A PHENYL-ALKANYL-CARBINOL WITH A DIIMIDAZOLLYL SULFONE, OXIDATION OF A PHENYL-IMIDAZOLYLALKYLMERCAPTAN OR REDUCTION OF A PHENYL-IMIDAZOLYLALKYLANOTE OR ALKANONITRILE. A TYPICAL EMBODIMENT IS 1-(1,1-DIPHENYL-2-ACETOXYETHYL) IMIDAZOLE.

Suebstitueye azolil-etil-eter ve bunlarin asit ilavesi tuzlari,kuaterner azolium tuz lari ve metal kompleksleri bun larin hazirlanisini ve mikrobisid madde olarak kullanilmasi

Ether derivatives of substituted 1-hydroxyalkyl- azoles as fungicides and plant growth regulators

Compounds which are ether derivatives of substituted 1-hydroxyalkyl-azoles, of the general formula ##STR1## in which A represents a nitrogen atom or a CH group, B represents oxygen, sulphur or a CH 2 group, R 1 represents a substituted alkyl, optionally substituted cycloalkyl or optionally substituted phenyl radical or, if either A represents a nitrogen atom, or if A represents the CH group and at the same B represents oxygen or sulphur, R 1 also represents an unsubstituted alkyl radical, R 2 represents an alkyl, alkenyl, alkinyl, optionally substituted phenyl or optionally substituted benzyl radical, Z represents a halogen atom or an alkyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, optionally substituted phenoxy, optionally substituted phenylalkyl or optionally substituted phenylalkoxy radical and m is 0, 1, 2 or 3, and acid addition salts and metal salt complexes thereof, are novel, are prepared as described, and find use as fungicides and as agents for regulating plant growth.

Ether derivatives from substituted 1-hydroxyalkyl azoles, process for their preparation as well as their use as fungicides and plant-growth regulators

Ether derivatives of substituted 1-hydroxyalkyl-azoles as fungicides and plant growth regulators

Compounds which are ether derivatives of substituted 1-hydroxyalkyl-azoles, of the general formula ##STR1## in which A represents a nitrogen atom or a CH group, B represents oxygen, sulphur or a CH 2 group, R 1 represents a substituted alkyl, optionally substituted cycloalkyl or optionally substituted phenyl radical or, if either A represents a nitrogen atom, or if A represents the CH group and at the same B represents oxygen or sulphur, R 1 also represents an unsubstituted alkyl radical, R 2 represents an alkyl, alkenyl, alkinyl, optionally substituted phenyl or optionally substituted benzyl radical, Z represents a halogen atom or an alkyl, cycloalkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, optionally substituted phenoxy, optionally substituted phenylalkyl or optionally substituted phenylalkoxy radical and m is 0, 1, 2 or 3, and acid addition salts and metal salt complexes thereof, are novel, are prepared as described, and fine use as fungicides and as agents for regulating plant growth.

Substituted diazolylalkyl or triazolylalkyl carbinols, process for their preparation and their use as antimycotic compounds

1. Substituted di- or triazolylalkyl-carbinols of the general formula see diagramm : EP0120276,P20,F1 in which A represents a nitrogen atom or the CH group ; B represents a nitrogen atom or the CH group ; X represents hydrogen and straight-chain or branched alkyl with 1 to 6 carbon atoms ; Y represents straight-chain or branched alkyl with 1 to 6 carbon atoms ; and, if X represents hydrogen, also straight-chain or branched alkenyl and alkinyl with in each case 3 to 6 carbon atoms and benzyl which is optionally mono- to trisubstituted in the phenyl part by identical or different substituents, substituents which may mentioned being : halogen, alkyl with 1 to 4 carbon atoms, alkoxy and alkylthio with in each case 1 to 4 carbon atoms, halogenoalkyl, halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon and 1 to 5 identical or different halogen atoms, such as preferably fluorine and chlorine atoms, nitro and cyano ; R represents phenyl which is optionally mono- to tri-substituted by identical or different substituents, preferred substituents which may be mentioned being : halogen, alkyl with 1 to 4 carbon atoms, alkoxy and alkylthio with in each case 1 to 4 carbon atoms, halogenoalkyl, halogenoalkoxy and halogenoalkylthio with in each case 1 to 2 carbon and 1 to 5 identical or different halogen atoms, such as preferably fluorine and chlorine atoms, nitro, cyano, hydroxyl, hydroxycarbonyl with 1 to 4 carbon atoms in the alkyl part, hydroximinoalkyl with 1 to 4 carbon atoms, alkoximinoalkyl with 1 to 4 carbon atoms in each alkyl part, and phenyl, phenoxy, benzyl and benzyloxy, each of which is optionally substituted by halogen and/or alkyl with 1 to 2 carbon atoms ; R furthermore preferably represents the grouping see diagramm : EP0120276,P20,F2 wherein Alk**1 represents straight-chain or branched alkyl with 1 to 4 carbon atoms ; Alk**2 represents straight-chain or branched alkyl with 1 to 4 carbon atoms ; Alk**1 and Alk**2, together with the carbon atom to ...

Imidazolyl vinyl ethers having fungicidal and bactericidal activity

Aryl-imidazol-1-yl vinyl ethers and their acid addition salts are disclosed, wherein the imidazolyl vinyl ether has the formula: <IMAGE> Ar in the formula represents a substituted or unsubstituted aryl or heterocyclic radical; R represents hydrogen or a C1-C12 alkyl or cycloalkyl (saturated or unsaturated) or Ar as above; Im represents a 1-H-imidazol-1-yl group (unsubstituted or substituted); and Y represents a saturated or unsaturated, acyclic or cyclic C1-C12 alkyl, or aryl or aralkyl, or an alkyl or alkylene residue directly bound to the ether oxygen and having a chain once or twice interrupted by -O-, -S-, -SO- or -SO2- bridges. These compounds are effective wide spectrum fungicides and bactericides. [US4210657A]

Patent DE2633492C2

FUNGICIDAL AGENTS

Cyclopropyl-substituted azolyl methyl carbinoles, process for their preparation and their use as therapeutic agents

The present invention relates to 1-cyanocyclopropyl- and 1-carboxamido-cyclopropyl-azolylmethylcarbinol derivatives, process for the preparation thereof and the use thereof in medicaments, especially for mycoses.

1-phenethylimidazole derivatives

ABSTRACT 1-Phenethylimidazole compounds of the formula: wherein R4 and R5 are independently hydrogen or halogen, and Z is a mono or disubstituted phenyl moiety of the formula:

1-(2,2-bis-thioethyl)1-h-imidozole compounds

Abstract of the Disclosure Novel imidazole mercaptals of the formula I wherein each m is independently zero or one; and R1 and R2 each are independently selected from (lower)alkyl, cyclo-alkyl, cycloalkyl(lower)alkyl, phenyl, phenyl(lower)alkyl, thienyl, thienyl(lower)alkyl, pyridyl and pyridyl(lower)-alkyl, in which the phenyl and heterocyclic rings optionally may contain from 1 to 3 substituents, and acid addition salts thereof, are useful antimicrobial agents.

Thioketal substituted n-alkyl imidazoles and pharmaceutical compositions containing them

Derivatives of substituted n-alkyl imidazoles, their preparation and these compounds for pharmaceutical use

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

Olefin polymerization catalysts containing group 8-10 transition metals, bidentate ligands, processes employing such catalysts and polymers obtained therefrom

Methods for preparing olefin polymers, or oligomers catalysts for preparing olefin polymers and bidentate ligand used for preparing these catalysts are disclosed. The polymers can be prepared containing the corresponding monomers with a Group 8-10 transition metal catalyst. The polymers are suitable for processing in conventional extrusion processes, and can be formed into high barrier sheets or films, or low molecular weight resins for use in synthetic waxes in wax coatings or as emulsions.

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

[UNK]

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

第８〜１０族遷移金属オレフィン重合触媒

(57)【要約】 オレフィンモノマーの重合で触媒として有用な、ある種の遷移金属錯体が供給される。詳しくは、本発明は、Ni，Pd，Co又はFeに結合したある種の二座配位子及び任意的な１種又はそれ以上の中性ルイス酸の錯体並びにオレフィンの重合に於けるその使用を提供する。

Group 8-10 transition metal olefin polymerization catalysts

Provided are certain transition metal complexes which are useful as catalysts in the polymerization of olefinic monomers. In particular, the invention provides complexes of certain bidentate ligands bonded to Ni, Pd, Co, or Fe, and optionally, one or more neutral Lewis acids, and their use in the polymerization of olefins.

The method of obtaining derivatives of phenylimidazolyl

Process for preparation of 1-benzylimidazole compound, and novel compound

내용없음. None.

一种咪唑类不饱和离子液体及其制备方法

本发明涉及一种咪唑类不饱和离子液体及其制备方法，将卤代试剂单体和烯基咪唑分别加入到溶剂中，在10～70℃下反应得到目标离子液体。所合成离子液体的咪唑两端侧链分别带有双键，丰富了可聚离子液体的种类，为离子液体作为可聚合单体、交联剂及在催化和分离等领域中的应用提供了更多的选择。本发明所合成的离子液体具有良好的水溶性，在生物领域具有潜在的应用价值。

Способ получения энантиомерно чистого 6-[(4-хлорфенил)-(1h-1,2,4-триазол-1-ил)метил]-1-метил-1н-бензотриазола, промежуточные соединения для их получения и способ их получения

Предлагается способ получения (+)-6-[(4-хлорфенил) (1-1,2,4 -триазол-1-ил)метил] -1-метил-1H-бензотриазола, включающий расщепление (±)-6-[(4-хлорфенил)гидразинометил]-1-метил-1H-бензотриазола и превращение проходящего энантиомерно чистого промежуточного гидразина в (+)-6-[(4-хлорфенил)(1H-1,2,4-триазол-1-ил)метил] -1-метил-1H-бензотриазол. Предложены также новые промежуточные соединения для получения целевых соединений и способы их получения.

Optically active hydroxybenzylamine derivative, optically active

내용 없음. No content.

Method for preparing 1,2,4-triazole derivatives

1-Alkoxy-1-azolylmethyloxirane, process for their preparation and their use as crop protection agents.

Patent SU408476A3

Use of polyacids to treat mineral fertilizers containing a nitrification inhibitor

THE USE OF INORGANIC OR ORGANIC POLYACIDS FOR THE TREATMENT OF INORGANIC FERTILIZERS, IN PARTICULAR THE USE OF THE POLYACIDS AS A MIXTURE WITH AT LEAST ONE NITRIFICATION INHIBITOR FOR THE TREATMENT OF INORGANIC FERTILIZERS; THE USE OF SELECTED PYRAZOLE DERIVATIVES AS NITRIFICATION INHIBITOR IN INORGANIC FERTILIZERS AND ALSO AS STABILIZERS OF LIQUID MANURE OR LIQUID FERTILIZER FORMULATIONS, AS WELL AS THE CORRESPONDING TREATED INORGANIC FERTILIZERS PER SE; AND NOVEL PYRAZOLE DERIVATIVES WHICH CAN BE USED AS NITRIFICATION INHIBITORS IN INORGANIC FERTILIZERS AND ALSO AS STABILIZERS OF LIQUID MANURE OR LIQUID FERTILIZER FORMULATIONS ARE DESCRIBED.

Process for preparing 2,4-oxazolidinediones

一种环丙基酰肼和甲氧苯类gpr119激动剂、制备方法及其用途

本发明涉及与II型糖尿病相关的药物领域。具体而言，本发明涉及一种含环丙基酰肼和甲氧基苯类结构的GPR119激动剂、其制备方法以及在制备2型糖尿病药物中的应用。

3-cyclyl-5-(nitrogen-containing 5-membered ring) methyl-oxazolidinone derivatives and their use as antibacterial agents

Disclosed are compounds of formula (I), wherein: -N-HET is (Id) or (If), R1 is an alkyl group, Q is Q1 or Q2, and the remaining substituents are defined herein. The compounds are used in the manufacture of medicaments for use as antibiotics.

METHOD OF OBTAINING DERIVATIVE PHENYLIMIDAZOZYLALKANES

Гербицидное средство

１，２，４−トリアゾ−ル誘導体および農園芸用殺菌剤

(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。

ヒドロキシベンズアルドキシムｏ−エ−テルの製造法

(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。

Processes for the preparation of fluorazolyl propan derivatives

A process for prepg. fluoroazolylpropane of formula (I) and its acid addn. salts, quaternary azollynium salts and metal complex salts comprise (i) reacting fluoroazolyl methyl oxirane with alcohol or thioalcohol of formula H-X-R5 in the presence of base in an inert solvent and (ii) etherification or esterification of the product. In the formula, Az is imidazol-1-yl or 1,2,4triazol-1-yl; R1 is H, Me, Et or mono-substd. benzyl by F or Cl; R2 is t-Bu; R3 is H, me or acetyl; R5 is n-Bu, Ph or mono- or di-substd. Ph; X is O or S; Y is halogen or org. or inorg. acid radical.

The way to fight fungi

1-아릴-2-플루오로-2-아졸릴 알카논 및 알칸올의 제조방법

내용 없음.

Itraconazole and saperconazole stereoisomers

본 발명은 일반식 (시스-(Ⅰ))로 표시될 수 있는 이트라코나졸(X=Cl) 및 사퍼코나졸(X=F)의 입체이성체, 및 그의 약제학적으로 허용되는 산 부가염, 이들 입체이성체의 제조방법, 이들 입체이성체와 사이클로덱스트린의 복합체, 이 복합체를 함유하는 약제학적 조성물, 및 이들 복합체 및 약제학적 조성물을 제조하는 방법에 관한 것이다. The present invention relates to stereoisomers of itraconazole (X = Cl) and saperconazole (X = F), which can be represented by the general formula (cis- (I)), and pharmaceutically acceptable acid addition salts thereof, these stereoisomers It relates to a process for the preparation of these compounds, complexes of these stereoisomers and cyclodextrins, pharmaceutical compositions containing these complexes, and methods of preparing these complexes and pharmaceutical compositions. 상기식에서, 세 개의 *는 세개의 키랄 중심(chiral center)을 나타내며, '시스'는 (1H-1,2,4-트리아졸-1-일메틸) 부위를 의미하고, Wherein three * represent three chiral centers, 'cis' means (1H-1,2,4-triazol-1-ylmethyl) moiety, 치환된 페녹시 부위는 1,3-디옥솔란 환에 의해 규정되는 평면상의 동일한 면에 위치한다. The substituted phenoxy moiety is located on the same side of the plane defined by the 1,3-dioxolane ring.

Ｎ−〔１−トリアゾ−ル−（１）−イル−２，２，２−トリクロロエチル〕−置換アミド誘導体及び該誘導体を含有するうどんこ病防除剤

(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。

Tetrahydrofuran antifungals

A compound represented by the formula I ##STR1## wherein X is independently both F or both Cl or one X is independently F and the other is independently Cl; R 1 is a straight or branched chain (C 3 to C 8 ) alkyl group substituted by one or two phosphate ester groups (e.g., a phosphate ester convertible in vivo into a hydroxy group) thereof or a pharmaceutically acceptable salt thereof and pharmaceutical compositions thereof useful for treating and/or preventing fungal infections are disclosed.

Производные 3-циклического-5-(азотсодержащего 5-членного кольцевого) метил-оксазолидинона и их применение в качестве антибактериальных средств

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (51) ÌÏÊ 7 (11) 2004 129 276 (13) A C 07 D 413/14 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2004129276/04, 25.02.2003 (71) Çà âèòåëü(è): ÀÑÒÐÀÇÅÍÅÊÀ ÀÁ (SE) (30) Ïðèîðèòåò: 28.02.2002 US 60/360,957 (43) Äàòà ïóáëèêàöèè çà âêè: 10.06.2005 Áþë. ¹ 16 (86) Çà âêà PCT: GB 03/00785 (25.02.2003) (74) Ïàòåíòíûé ïîâåðåííûé: Âåñåëèöêà Èðèíà Àëåêñàíäðîâíà Àäðåñ äë ïåðåïèñêè: 101000, Ìîñêâà, Ì.Çëàòîóñòèíñêèé ïåð., ä.10, êâ.15, "ÅÂÐÎÌÀÐÊÏÀÒ", È.À.Âåñåëèöêîé (54) ÏÐÎÈÇÂÎÄÍÛÅ 3-ÖÈÊËÈ×ÅÑÊÎÃÎ-5-(ÀÇÎÒÑÎÄÅÐÆÀÙÅÃÎ 5-×ËÅÍÍÎÃÎ ÊÎËÜÖÅÂÎÃÎ) Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ôîðìóëû (I), èëè åãî ôàðìàöåâòè÷åñêè ïðèåìëåìà ñîëü, èëè ñëîæíûé ýôèð, êîòîðûé ñïîñîáåí ê ãèäðîëèçó â óñëîâè õ in vivo A ãäå -N-HET âûáðàí èç íèæåïðèâåäåííûõ ñòðóêòóð (la)-(If): R U 2 0 0 4 1 2 9 2 7 6 A ÌÅÒÈË-ÎÊÑÀÇÎËÈÄÈÍÎÍÀ È ÈÕ ÏÐÈÌÅÍÅÍÈÅ Â ÊÀ×ÅÑÒÂÅ ÀÍÒÈÁÀÊÒÅÐÈÀËÜÍÛÕ ÑÐÅÄÑÒ Ñòðàíèöà: 1 RU 2 0 0 4 1 2 9 2 7 6 (87) Ïóáëèêàöè PCT: WO 03/072575 (04.09.2003) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.09.2004 (72) Àâòîð(û): Ìàéêë Áàððè ÃÐÅÉÂÑÒÎÊÊ (US), Íèë Äæåéìñ ÕÅÉËÑ (US), Ôîëüêåðò ÐÅÊÊ (US), Ôåé ÄÆÎÓ (US), Ïîë Ðîáåðò ÔËÅÌÈÍà (US), Äàíèåë Ðîáåðò ÊÀÐÊÀÍÀÃÜÞ (US), Ìàðê Ìèøåëü ÆÈÐÀÐÄÎ (US) ãäå u è v íåçàâèñèìî ïðåäñòàâë þò ñîáîé 0 èëè 1; R1 ïðåäñòàâë åò ñîáîé Ñ1-Ñ4-àëêèëüíóþ ãðóïïó; Q âûáðàí èç Q1-Q6: 2 0 0 4 1 2 9 2 7 6 R U A Ñòðàíèöà: 2 2 0 0 4 1 2 9 2 7 6 A R U ãäå R 2 è R 3 íåçàâèñèìî âûáðàíû èç Í, F, Cl, CF3, ÎÌå, SMe, Me è Et; B1 ïðåäñòàâë åò ñîáîé Î èëè S; Ò âûáðàí èç ãðóïï â (ÒÀ) - (ÒÅ), óêàçàííûõ íèæå (ãäå AR1, AR2, AR2a, AR2b, AR3, AR3a, AR3b, AR4, AR4a, CY1 è CY2 èìåþò çíà÷åíè , óêàçàííûå íèæå); (ÒÀ) Ò âûáðàí èç ñëåäóþùèõ ãðóïï: (ÒÀà) AR1 èëè AR3; èëè (TAb) ãðóïïà ôîðìóëû (TAb1) - (TAb6): A 2 0 0 4 1 2 9 2 7 6 R U A Ñòðàíèöà: 3 2 0 0 4 1 2 9 2 7 6 R 4 è R 5 íåçàâèñèìî âûáðàíû èç âîäîðîäà, ãàëîãåíà, òðèôòîðìåòèëà, öèàíî, àçèäî, íèòðî, Ñ1-Ñ4-àëêîêñè, Ñ1-Ñ4-àëêèëS(O)q- (q ïðåäñòàâë åò ...

旋光吡咯化合物及其制法和用途

式(I)旋光性的吡咯化合物或其盐，可用作杀菌 剂。式中R 1 和R 2 独立地为氢、卤素、卤代烷基、卤 代烷氧基或必要时被取代的含氮杂环基；R 3 是氢或 酰基；Q是CH或N； 是至少有两个可被取代 的相邻氮原子作为成环原子的含氮芳族五元杂环基 或有两个或更多可被取代的氮原子作为成环原子的 芳族稠合杂环基；标有(R)的碳原子表示R-构型；条 件是R 1 和R 2 之一当 是1H-1，2，4-三唑-1- 基时应为必要时被取代的含氮杂环基。

Method of fighting true mildew

There are desclosed compounds of formula: wherein R = H, an alkyl, an alkenyl, an alkynyl, an alkoxyl, a phenyl, a phenoxy, an alkoxycarbonyl, an alkylcarbonyl, a benzoyl or a cyano group; R' and R 2 = an alkyl, an alkenyl, an alkynyl, a phenyl, an alkoxycarbonyl, an alkylcarbonyl or a cyano group; or R and R 2 together form an orthocondensed benzene ring; X = CH or N. The compounds of formula I are endowed with fungicide activity against phytopathogenous fungi.

Method of preparing imidazole derivatives or thir salts

Imidazole derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof are provided: <IMAGE> I In the formula, R4 1- or 2-naphthyl, optionally substituted with Cl, Br, or I; 1,2,3,4-tetrahydro-6-naphthyl; 3-duryl, optionally 6-substituted by Cl, Br, I, NO2, CH3 or benzyl; mesityl, phenyl 2-, 3- or 4-substituted by OH, NH2, NO2, CH3CONH, phenyl, phenoxy, cyclohexyl, phenylthio, benzylthio, C1-C6 alkyl or C1C6 alkylthio; 4-bibenzylyl; 3,4-dihydroxyphenyl, n=0, 1 or 2 and (a) R=H, alkyl having 1 to 6 carbon atoms or phenyl R1=H, alkyl having 1 to 6 carbon atoms or phenyl one of R2 and R3=H the other of R2 and R3=H, OH, benzoyloxy, C2-C7 alkanoyloxy, N-(C1-C6 alkyl)-carbamoyloxy, N,N-[di-(C1C6)alkyl]-carbamoyloxy, but if R2=R3=H then R=R1=H, or (b) R=H, C1-C6 alkyl, phenyl R1=H, C1-C6 alkyl, phenyl R2+R3=O, or <IMAGE> (c) The compounds of formula I are anti-convulsivants.

Method of producing derivatives of 3-(1-triazolyl)-furan

There are desclosed compounds of formula: wherein R = H, an alkyl, an alkenyl, an alkynyl, an alkoxyl, a phenyl, a phenoxy, an alkoxycarbonyl, an alkylcarbonyl, a benzoyl or a cyano group; R' and R 2 = an alkyl, an alkenyl, an alkynyl, a phenyl, an alkoxycarbonyl, an alkylcarbonyl or a cyano group; or R and R 2 together form an orthocondensed benzene ring; X = CH or N. The compounds of formula I are endowed with fungicide activity against phytopathogenous fungi.

Azolylmethyl-cyclopropylcarbinol derivative

METHOD OF OBTAINING N-TRIPHENYLMETHILIMIDAZOLES

SUBSTITUTED [1,2,4] TRIAZOL AND IMIDAZOL COMPOUNDS AS FUNGICIDES

Изобретение относится к соединениям формулы Iи к их применению в качестве фунгицидов, где переменные определены, как описано в формуле изобретения и в описании. The invention relates to compounds of the formula I and to their use as fungicides, where the variables are defined as described in the claims and in the description.

Fungicidal (trihalophenoxy or trihalophenthio) alkylaminoalkyl pyridines and pyrroles

Compounds of the Formula: ##STR1## wherein X is sulfur or oxygen; R is phenyl or phenyl substituted with 1 to 3 substituents independently selected from fluoro, chloro, bromo, iodo, lower alkyl or trihalomethyl; R 1 is lower alkyl or lower alkoxyalkyl; and R 2 is 5- or 6-member heterocyclic ring having 1 to 3 ring nitrogens and the remainder of the ring atoms carbon atoms, optionally substituted with 1 to 2 independent lower alkyl groups, provided that a nitrogen of the 5- or 6-member heterocyclic ring is not bonded to the adjacent --CH 2 -- group; or the group --CH 2 --R 3 wherein R 3 is a 5- or 6-member heterocyclic ring having 1 to 3 ring nitrogens and the remainder of the ring atoms carbon atoms, are fungicidal.

Method of fighting fungi

Method of controlling weeds (its versions)

1. Способ борьбы с сорными растени ми в посевах культурных растений путем обработки их или почвы, на которой они пр)оизрастают, гербицидом производным хлорацетанилида общей формулы (Г) 1 .X СН2--Б снз о где R R метил, этил J водород, метил; X - водород, метил, метокси, хлор, отличающийс  тем, что, с целью повышени  избирательности действи , обработку провод т смесью про-, изводного хлорацетанилида общей формулы

Fungicide

Process for the preparation of microbicidal compounds

Substd. azolyl-ethylethers of formula (I), their acid addn. salts, quat. azolium salts and metal complexes are new. In (I), R1 is phenyl (opt. mono- or tri-substd. by halo, C1-3 haloalkyl, nitro, C1-3 alkoxy, C1-8 alkyl or cyano, or substd. by phenyl or phenoxy), naphthyl (opt. mono- or di-substd. by halo, nitro or C1-3 alkyl or benzyl (opt. substd. as naphthyl); R2 is phenyl (opt. substd. as above), C1-10 alkyl, C3-8 cycloalkyl or C3-8 cycloalkyl-(C1-4 alkyl); R3 is C1-12 alkyl, C2-4 alkenyl, C3-4 alkynyl or benzyl (opt. substd. as above); R4 is an azolyl gp.. (I) are useful in plant protection as microbicides, esp. systemic fungicides.

Method of obtaining 1,2,4-triazole derivatives or salts thereof

A PROCEDURE FOR OBTAINING SUBSTITUTED DIAZOLYLALKYL-CARBINOLS

Ionic liquids ii

An ionic liquid of the general formula: K+A- (I), in which: K+ is a cation which is: (see formula II), (see formula III), (see formula IV), (see formula V), (see formula VI), (see formula VII), (see formula VIII), (see formula IX), where R1 to R6 are identical or different, are optionally bonded directly to one another by a single or double bond and each, individually or together, have the following meaning: - H, - halogen, a C1 to C8 alkyl radical, which may be partially or fully substituted by F, Cl, N(C n F(2n+1-x)H x)2, O(C n F(2n+1-x)H x), SO2(C n F(2n+1-x)H x) or C n F(2n+1- x)H x, where 1 < n < 6 and 0 < x <= 2n+1; and A- is tris(pentafluoroethyl)trifluorophosphate or tris(nonafluorobutyl)trifluorophosphate.

Process for preparing 2-guanidino-4-heteroarylthiazoles

The title compds. I [X = S, NH; Y = CH, C CH3, N; R = H, hydroxymethyl, alkyl containing 1-6 carbons, -(CH2)nAr, -NH2, -NHR', -NHCOR' (R' = alkyl containing 1-6 carbons, -(CH2)mAr; n = integer 2-4; m = integer 0-4; Ar = phenyl) were prepd. Thus, 2-guanidino-4- thiazolecarboxylic acid 2-propion imidohydrazide was refluxed 2hr. and then cooled and precipitated, via recrystn., to give 2-guanidino- 4-(3-ethyl-5-1,2,4-triazolyl) thiazole. The compds. I activate stomach secretions and inhibit histamine H2 activity and are useful ad a medicine for excese stomach acid and ulcers.

Process for preparation azloes

1-Phenyl-2-azole-ethylaminocarbonyl derivs. of formula (I) and their acid addn. salts are prepd. by acylation of a compd. of formula (II). In the formulas, R1 and R2 are each opt. substd. aliphatic heteroaryl or aryl, or R1 is also H; R3 and R4 are opt. aliphatic gp. attached via S, O, SO or SO2, or opt. substd. phenyl or phenoxy; X is N or CH. (I) are useful as anti-mycotics.

Method of fungus control

1418430 Triazolyl-O,N-acetals BAYER AG 10 May 1974 [12 May 1973] 20763/74 Heading C2C The invention comprises compounds of the formula R<SP>1</SP>-O-C(R<SP>2</SP>)(Az)-C(OH)(R<SP>3</SP>)(R<SP>4</SP>) (I), where R<SP>1</SP> is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, optionally substituted aryl or aralkyl optionally substituted in the aryl part; R<SP>2</SP>, R<SP>3</SP> and R<SP>4</SP> are the same as R<SP>1</SP> or may also be hydrogen but R<SP>3</SP> andR<SP>4</SP> are not simultaneously hydrogen; and Az is optionally substituted 1,2,4-triazolyl-(1), 1,2,4-triazolyl-(4) or 1,2,3-triazolyl(1); and their salts, and their preparation by reducing a compound of the formula R<SP>1</SP>-O-C(R<SP>2</SP>)(Az)-CO-R<SP>4</SP> (II) or by reacting the said compound II with a compound M-R<SP>3</SP> where M is an alkali metal or a X-Mg-radical, where X is Cl, Br or I. # - [4<SP>1</SP> - Chlorophenoxy] - # - [1,2,4 - triazolyl- (1<SP>1</SP>)]acetophenone is made by condensing 4- chlorophenol with #-chloroacetophenone, brominating the resulting #-(4<SP>1</SP>-chlorophenoxy). acetophenone and reacting the formed #- bromo - # - [4<SP>1</SP> - chlorophenoxy]acetophenone with 1,2,4-triazole. Fungicidal compositions for preventing the growth of fungi on plants, comprise compounds (I) with a suitable carrier and the invention includes these compositions and methods of combating fungi at a locus by treating the locus with said compounds alone or together with suitable diluents or carriers.

Tricyclic compounds useful as angiotensin ? agonists

하기 화학식 1의 화합물이 제공된다. 여기서, 본 명세서에서 설명된 X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Z 1 , Z 2 , R 4 및 R 5 와 그들의 약학적으로 허용가능한 염은 AT2 수용체의 선택적인 작용제로, 예를 들면 특히, 소화불량, IBS 및 MOF과 같은, 위장 용태(gastrointestinal conditions)와, 그리고 심장혈관질환의 치료에 유용하다. There is provided a compound of formula 1 Wherein X 1 , X 2 , X 3 , X 4 , Y 1 , Y 2 , Y 3 , Y 4 , Z 1 , Z 2 , R 4 and R 5 and their pharmaceutically acceptable salts described herein Is a selective agent of the AT2 receptor, and is particularly useful, for example, in indigestion, gastrointestinal conditions, such as IBS and MOF, and in the treatment of cardiovascular diseases. [화학식 1] [Formula 1]

Method of producing derivatives of azole or phytopharmaceutically acceptable acid-additive salts thereof

Novel 1-(2-aryl-1,3-dioxan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles wherein the 1,3-dioxane ring is optionally substituted with 1 to 3 substituents.

Fungicide

Quinoline derivatives, method of their synthesis and anti-inflammatory agent

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to derivatives of quinoline of the general formula (I) where Y means group C-G where G - carboxy- or alkoxycarbonyl-group; - imidazole, benzimidazole, pyrazole, triazole, 1,2-dihydropyridine, indolyl optionally substituted with alkyl, amino-, hydroxy-, oxo- or formyl-group; each of A and B rings can be substituted with 1-3 substituents taken from halogen atom, hydroxy-, oxo-, alkyl-, alxoxy-group and -O(CH 2 ) l -group; l - the whole number 1-3; n - the whole number 1-4; k = 0 or 1, or their pharmaceutically acceptable salts showing an anti-inflammatory effect. EFFECT: improved method of synthesis, an anti-inflammatory activity of compounds. 21 cl, 10 tbl, 63 ex ОС с ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) (51) МПК ВИ "” 2 132 330. С 070 401/06, 403/06, 239/74, 13) СЛ А 61 К 31/47, 31/495, 31/505 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 94002335/04, 21.01.1994 (30) Приоритет: 28.01.1993 УР 012628/1993 20.08.1993 УР 206128/1993 (46) Дата публикации: 27.06.1999 (56) Ссылки: ЗЦ 1780536 АЗ, 1992. ЗЦ 1471243 А, 1987. ЕР 125756 АД, 1983. ЕР 371564 А2, 1990. 4$ 5084462 А, 1992. 5Ц 1318148 АЗ, 1983. (98) Адрес для переписки: 129010, Москва, ул.Б.Спасская, д.25, стр.3, ООО "СОЮЗПАТЕНТ" (71) Заявитель: Такеда Кемикал Индастриз Лтд. (4Р) (72) Изобретатель: Такеси Сохда (/Р}, Харухико Макино (/Р), Ацуо Баба (.Р) (73) Патентообладатель: Такеда Кемикал Индастриз Лтд. (ФР) (54) ПРОИЗВОДНЫЕ ХИНОЛИНА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРОТИВОВОСПАЛИТЕЛЬНОЕ СРЕДСТВО (57) Реферат: Производные хинолина общей формулы 1, в которой У - группа С-С; С - карбокси или алкоксикарбонил:; =) _ имидазол, бензимидазол, пиразол, триазол, 1,2-дигидропиридин, индолил, необязательно замещенный алкилом, амино-, гидрокси-, оксо- или формильной группой; каждое из колец А и В возможно замещено 1 - 3 заместителями, выбранными из галогена, гидрокси, оксо, алкила, алкокси и группы -О(СН>)4; | - целое ...