ПРОИЗВОДНЫЕ ПИРИМИДИНИЛОКСИАЛКАНАМИДОВ И ФУНГИЦИДЫ ДЛЯ СЕЛЬСКОГО ХОЗЯЙСТВА ИЛИ САДОВОДСТВА

Изобретение относится к новым производным пиримидинилоксиалканамидов общей формулы I и фунгицидам для сельского хозяйства или садоводства на их основе. В соединениях общей формулы I А означает кислород или серу, Q представляет цианогруппу или группу COR7, где R7 означает С1-С6-алкильную группу, С3-С6-циклоалкильную группу, которая может быть замещена атомом галогена или С1-С6-алкильной группой, С1-С6-галогеналкильную группу, С1-С6-алкоксигруппу, С2-С6-алкенилоксигруппу, С2-С6-алкинилоксигруппу или С3-С6-циклоалкилоксигруппу; R4 представляет атом водорода, С1 -С6-алкильную группу, С3-С6-циклоалкильную группу или С1-С6-галогеналкильную гpyппy; R1, R2, RЗ, R5, R6 означают водород, С1-С6-алкильную группу и другие группы, указанные в формуле изобретения, или R2 и R3 вместе с атомом углерода, с которым они связаны, образуют ненасыщенное 5-6-членное кольцо, или R5 и R6 вместе с атомом углерода, с которым они связаны, образуют 5-7-членную циклоалкильную группу, которая может быть замещена С1-С6 ...

АМИНОПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗ

Изобретение относится к соединению формулы I или его таутомеру или их фармацевтически приемлемым солям, где R2 представляет собой С1-3-алкил или циклопропил; R9 представляет собой галоген, С1-3-алкил, -O-(C1-3-алкил), -S-(С1-3-алкил) или CF3 и р равно 1-2. Предлагаемые соединения являются ингибиторами Аврора-протеинкиназ. Они могут использоваться в способе ингибирования активности Аврора-протеинкиназы. Изобретение также предоставляет фармацевтически приемлемые композиции, включающие такие соединения; и способ лечения пролиферативного расстройства у пациента с применением указанного соединения. 4 н. и 7 з.п. ф-лы, 7 табл.

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

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

ИНГИБИТОРЫ ПРОДУЦИРОВАНИЯ / СЕКРЕЦИИ β-АМИЛОИДНОГО БЕЛКА

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 ...

ПРОИЗВОДНЫЕ 2(О-[ПИРИМИДИН-4-ИЛ]МЕТИЛЕНОКСИ)ФЕНИЛУКСУСНОЙ КИСЛОТЫ, СРЕДСТВА БОРЬБЫ С ВРЕДОНОСНЫМИ ГРИБАМИ И ВРЕДИТЕЛЯМИ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СПОСОБ БОРЬБЫ С ВРЕДОНОСНЫМИ ГРИБАМИ И ВРЕДИТЕЛЯМИ

Изобретение относится к новым производным 2-(О-[пиримидин-4-ил]метиленокси)фенилуксусной кислоты, их солям и N-оксидам общей формулы I, средствам для борьбы с вредоносными грибами и вредителями, способу их получения и способу борьбы с вредоносными грибами и вредителями с использованием соединений общей формулы I. В соединениях формулы I R1 означает водород, C1-2-алкил, R2 означает галоген, C1-2-алкил, R3 означает амино, гидрокси, меркапто, галоген, C1-8-алкил, причем алкильные группы могут быть замещены фенильной группой, которая в свою очередь может быть замещена одним или независимо друг от друга двумя заместителями из числа следующих: галоген, циано, нитро, C1-4-алкил, C1-4-галогеналкил и C1-4-алкокси; C1-8-галогеналкил, С1-8-алкокси-С1-4-алкил, C1-8-алкокси, С1-8 -моноалкиламино, ди-C1-8-алкиламино, C1-8 -алкилтио, C1-8-алкилсульфоксил, C1-8-алкилсульфонил, С3-6-циклоалкил, три-С1-8 -алкилсилилокси или необязательно замещенный в ароматическом кольце: фенил, фенокси, феноксиметил, бензилокси ...

ИНГИБИТОРЫ КИНУРЕНИН-3-МОНООКСИГЕНАЗЫ

Изобретение относится к области органической химии и медицины и касается новых соединений формулы (I), соответствующей фармацевтической композиции, содержащей эти соединения, и способа лечения состояния или расстройства, опосредованного активностью Кинуренин-3-моноксигеназы. Изобретение расширяет ассортимент средств, активных в отношении Кинуренин-3-моноксигеназы. 4 н. и 13 з.п. ф-лы, 2 табл., 15 пр. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 239/24 A61K 31/505 A61K 31/506 A61P 25/28 (13) 2 523 448 C2 (2006.01) (2006.01) (2006.01) (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2011107437/15, 04.08.2009 (24) Дата начала отсчета срока действия патента: 04.08.2009 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 10.09.2012 Бюл. № 25 (45) Опубликовано: 20.07.2014 Бюл. № 20 2242480, C2, 20.12.2004. WO 2004/112690, 29.12.2004 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 04.03.2011 (86) Заявка PCT: 2 5 2 3 4 4 8 (56) Список документов, цитированных в отчете о поиске: US 2005/028830 A1, 29.12.2005. RU (73) Патентообладатель(и): СиЭйчДиАй ФАУНДЕЙШН, Инк, (US) R U 04.08.2008 US 61/086,090 (72) Автор(ы): ВИТЯК Джон (US), ТОЛЕДО-ШЕРМАН Летисиа М. (US), ДОМИНГЕЗ Селия (US), КУРТНЕЙ Стивен Мартин (GB), ЯРНОЛЬД Кристофер Джон (GB), ДЕ АГУЯР ПЕНА Паула Кристина (GB), ШИЛЛ Андреас (DE), ВИНКЛЕР Дирк (DE) 2 5 2 3 4 4 8 R U (87) Публикация заявки PCT: WO 2010/017179 (11.02.2010) Адрес для переписки: 119019, Москва, Гоголевский бульвар, д. 11, 3й этаж, "Гоулингз Интернэшнл Инк." (54) ИНГИБИТОРЫ КИНУРЕНИН-3-МОНООКСИГЕНАЗЫ (57) Реферат: Изобретение относится к области органической химии и медицины и касается новых соединений формулы (I), соответствующей фармацевтической композиции, содержащей эти соединения, и способа лечения состояния или расстройства, опосредованного активностью Кинуренин-3-моноксигеназы. Изобретение расширяет ассортимент средств, активных в отношении ...

СПОСОБ ПОЛУЧЕНИЯ Е-ИЗОМЕРОВ ПРОИЗВОДНЫХ АКРИЛОВОЙ КИСЛОТЫ

Использование: в качестве фунгицидов в сельском хозяйстве. Сущность изобретения: продукт: Е - изомеры производных акриловой кислоты общей формулы , где W - пиридинил- или пиримидинилгруппа, замещенная галогеном, C1-C4 -алкилом, который, в свою очередь, может быть замещен гомогеном, фенилом; C1-C4 -алкоксилом, феноксигруппой, которая может быть замещена 1-метоксикарбонил-2-метоксиэтенилом, галогеном, циано- или нитрогруппой, амино-, формамидо-, нитро-, циано- или N-оксидной группой, или W-хинолинил- или хиназолинилгруппа, возможно замещенная галогеном, и связанные с А одним из атомов углерода цинка, А - кислород или группа S(O)n , где n=0, или 1, или 2 при условии, что когда W - 5-трифторметилпиридинил-2, то А не является кислородом. Реагент 1: соединение общей формулы . Реагент 2: W - L, где L - галоген. Условия процесса: в присутствии основания в органическом растворителе, возможно в присутствии катализатора из числа переходного металла или его соли. 9 табл.

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 2-АНИЛИНОПИРИМИДИНА ИЛИ ИХ КИСЛОТНО-АДДИТИВНЫХ СОЛЕЙ

Использование: в химической промышленности как способ получения производных 2-анилинопиримидина, соединений, обладающих фунгицидной активностью. Сущность изобретения - способ получения производных 2-анилинопиримидина общей формулы 1 где R1 - Н, галоид; R2 - Н, галоид, метил; R3 - алкил- C1-C4 , замещенный галоидом, алкил- (C1-C4), циклопропил; R4 - циклопропил, незамещенный или замещенный галоидом или метилом, или их кислотно-аддитивных солей, заключающийся в том, что тиомочевину формулы II S=C(NH2)2 или соль изотиурония формулы III где A⊖ - анион кислоты, причем R5- C1-C8-алкил или незамещенный или замещенный галогеном и/или C1-C4-алкилом, бензил вводят во взаимодействие с дикетоном IV R3-C(O)CH2O(O)-R4 процесс ведут в инертном растворителе в присутствии кислоты при 20 - 140С, с получением соединений общей формулы V где y - Н или R5, R5 - C1-C8-алкил или незамещенный, или замещенный галогеном и/или (C1-C4)-алкилом бензил, соединение V, где y - Н в виде щелочной или щелочноземельной соли ...

АРИЛАНИЛИНОВЫЕ АГОНИСТЫ БЕТА2 АДРЕНЕРГИЧЕСКИХ РЕЦЕПТОРОВ

... 1. Соединение формулы (I) где каждый из R1-R5 независимо выбран из группы, включающей водород, алкил, алкенил, алкинил, арил, гетероарил, циклоалкил, гетероциклил и Ra; или R1 и R2, R2 и R3, R3 и R4 или R4 и R5 объединены вместе с образованием группы, выбранной из группы, включающей -С(Rd)=C(Rd)С(=O)NRd-, -CRdRd-CRdRd-C(=O)NRd-, -NRdC(=O)C(Rd)=C(Rd)-, -NRdC(=O)CRdRd-CRdRd-, -NRdC(=O)S-, -SC(=O)NRd-, -(CRdRd)p-, -S(CRdRd)q-, -(CRdRd)qS-, -S(CRdRd)rO-, -O(CRdRd)rS- и -NHC(Rj)=C(Rk)-; R6 представляет собой водород, алкил или алкокси; R7 представляет собой водород или алкил; R8 представляет собой водород или алкил; или R8 вместе с R9представляет собой -CH2- или -СН2СН2-; R9 независимо выбран из группы, включающей алкил, алкенил, алкинил, арил, гетероарил, циклоалкил, гетероциклил и Ra, или R9вместе с R8 представляет собой -CH2 - или -СН2СН2-; R10 представляет собой водород или алкил; R11, R12 и R13 независимо выбраны из группы, включающей водород, алкил, циклоалкил, алкенил, алкинил, арил, ...

ТИОЭФИРНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ НИТРИФИКАЦИИ

СОЕДИНЕНИЕ ПИРИМИДИНА

... 1. Соединение формулы (I) или его сольгде Rнизший алкил, Сциклоалкил, -О-низший алкил, галоген-низший алкил, низший алкилен-Сциклоалкил или низший алкилен-О-низший алкил;R-С(О)R, -С(О)NRR, низший алкилен-R, низший алкилен-NRR, низший алкилен-NRC(О)R, низший алкилен-OR, -NRC(О)R, -NRC(О)OR, -NRC(О)NRR, -NRS(О)Rили -NRS(О)NRR;W -СН-, -NR-, -О- или -S(O)-;RСалкил; Салкенил; Салкинил; галоген-Салкил; Салкил, замещенный 1-5 группами, выбранными из группы G; R; -Салкилен-R; -Салкилен-О-R; -Салкилен-О-низший алкилен-R; -Салкилен-S(О)-R; -Х-С(R)(фенил)или -СН(фенил)-СН(ОН)-фенил;где Салкилен может содержать от 1 до 5 заместителей, выбранных из группы G;или W и R, объединенные друг с другом, представляют собойилиRодинаковые или отличаются друг от друга, при этом каждый представляет собой Н или низший алкил;Rазотсодержащая насыщенная гетероциклическая группа, которая может содержать от 1 до 5 заместителей, выбранных из группы G;Rнизший алкил, галоген-низший алкил, низший алкилен-OR, низший алкилен-О-низший ...

ФАРМАЦЕВТИЧЕСКИЕ СОЕДИНЕНИЯ

... 1. Соединение формулы (1):или соль, N-оксид, таутомер или стереоизомер указанного соединения, где:А представляет собой СН или азот;Е представляет собой СН или азот;Rвыбран из следующего:- ациклическая Cуглеводородная группа, возможно содержащая один или два заместителя R, причем один атом углерода в ациклической Cуглеводородной группе может быть необязательно заменен гетероатомом или группой, выбранными из О, S, NR, S(O) и SO, или два соседних атома углерода в ациклической d.углеводородной группе могут быть необязательно заменены группой, выбранной из CONR, NRCO, NRSOи SONR, при условии, что в каждом случае в ациклической Cуглеводородной группе сохраняется по меньшей мере один атом углерода; и- моноциклическая карбоциклическая или гетероциклическая группа, содержащая от 3 до 7 членов кольца, из которых 0, 1, 2, 3 или 4 членов кольца являются гетероатомами, выбранными из О, N и S, причем указанная карбоциклическая или гетероциклическая группа возможно содержит один или два заместителя R; ...

ИНГИБИТОРЫ ГИСТОНДЕАЦЕТИЛАЗЫ

... 1. Соединение формулы (I) !! и его N-оксиды, гидраты, сольваты, фармацевтически приемлемые соли, пролекарства и комплексы указанного соединения, и рацемические и скалемические смеси, таутомеры, диастереомеры и энантиомеры, где ! выбирают из группы, включающей арил, гетероарил, циклоалкил и гетероциклил, где каждый арил, гетероарил, циклоалкил и гетероциклил является необязательно замещенным; ! W выбирают из группы, включающей N, -C= и -C(R1)-, причем если представляет собой циклоалкил или гетероциклил, тогда W представляет собой -C(R1)-; ! M выбирают из группы, включающей -C(O)N(R1)OR2, -C(O)NR1R2, -C(O)OH, -C(O)OR1, -C(O)C1-C3алкил-SR1, -NHC(O)C1-C3алкил-SR1, -NHC(O)C1-C3алкил-OR1, -C(O)CH2-S(ацетил), -C(O)-гетероарил, -C(O)-гетероциклил, -C(NOH)NR1R2, -C(O)C1-C3алкил-OR1, -C(O)C1-C3алкил-NR1R2, -C(O)CF3, -C(O)C(O)OR1, -C(O)C(O)NR1R2, -C(O)C1-C4алкил, -N(OH)C(O)H, -N(OR1)C(O)R2, -NR1SO2NR1R2, -SO2NR1OH, -N(OH)C(O)NR1R2, -NR1C(O)N(OH)R2, -OC(O)N(OH)R2, -C(NOH)NR1R2 и группу, хелатирующую ...

Фунгицидное средство

Использование: сельское хозяйство, химическое средство защиты растенш Сущность изобретения фунгицидное средство, включающее производныетеримидинаформулы , i ДР R1 - водород фтор, хлор, бром, метил, трифторметид меток- сид мохсип; R - водород фтор. R -С -С алкид, гидроксиметид циклопролид фтором или бромом замещенный метид R - незамещенный или замещенный фтором, хпороч бромом или метилом цик- попролик. в количестве 2-95 мас%, целевые добавки - остальное. 3 таба ...

GEMINALE DIMETHYLALKYL-VERBINDUNGEN, VERFAHREN ZU IHRER HERSTELLUNG UND IHRE VERWENDUNG IN FLUESSIGKRISTALLINEN MISCHUNGEN

Geminate dimethylalkyl compounds with general formula (I) can be used to good advantage in liquid crystalline mixtures. In the formula, R<1> is, for example, a straight or branched chain (with or without asymmetric C-atom) alkyl or alkenyl with 2 to 16 C-atoms; A<1>, A<2>, A<3> are the same or different and represent, for example, 1.4-phenylene, 1.4-cyclohexylene or pyrimidin-2.5-diyl; M<1>, M<2> are the same or different and represent CO-O, O-CO; G is, for example, the same or different straight or branched chain alkylene with 1 to 16 C-atoms; k, l, m, n are zero or 1; and R<6> is straight-chain alkyl with 1 to 10 C-atoms. The compounds described offer a lower point of fusion in liquid crystalline mixtures, a shift in the thermal limit of the Sc-phase in ferroelectric mixtures, and other improvements in important electro-optical characteristics.

ANILID-DERIVATE ALS FUNGIZIDE

ANILID-DERIVATE ALS FUNGIZIDE

VERFAHREN ZUR HERSTELLUNG VON FLUORALKENYLTHIO HETEROZYCLISCHE DERIVATE

N-Phenylcarbamate, Verfahren zu ihrer Herstellung und biozide Zusammensetzungen zur Bekämpfung von Schädlingen

Pyrimidinderivate als HMG-CoA reduktase Hemmer

DIAMID-DERIVATE VON HETEROCYCLISCHEN DICARBONSÄUREN, INSEKTIZIDE FÜR ACKER- UND GARTENBAU UND EIN VERFAHREN ZU IHRER VERWENDUNG

2-SUBSTITUIERTE-2-CYCLOPENTENONE UND DIESE ALS AKTIVE SUBSTANZEN ENTHALTENDE CARCINOSTATIKA UND OSTEOGENESIS-PROMOTER

HEMMUNG DER RAF-KINASE UNTER VERWENDUNG VON SYMMETRISCH UND UNSYMMETRISCH SUBSTITUIERTEN HARNSTOFFEN

Neue Pyrimidin-Derivate,Verfahren zu ihrer Herstellung und diese enthaltende fungizide Mittel

1,3-DIAZA-9-THIA-ANTHRACENE-2,4-DIONES AND PHOTOPOLYMERIZABLE MIXTURE CONTAINING THESE COMPOUNDS

FUNGICIDES

NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS

CHEMICAL COMPOUNDS

THERAPEUTIC AMIDES

Pesticidal heterocyclic and phenyl compounds

A compound of formula (I), R-S(O)nCH2CH2C(CH3) =CF2 or a salt thereof, wherein n is 0, 1 or 2; and R is a heterocyclic or phenyl group, has nematicidal, insecticidal and acaricidal activity.

Substituted 2-phenyl-3-methoxypropenoate fungicides

Ferroelctric liquid crystals

Antiinflammatory heterocyclic sulphones

Compounds of the formula are useful in the treatment of inflammatory processes, where
Het represents a C-bound heterocycle, and A represents an optional substituent on the heterocycle, m being from 0 to 3. D represents an optionally substituted (C 1 -C 4 )-alkandiyl, E represents CH=CH, CH=N or N=CH, and G represents a group of the formula wherein R2 represents H or (C 1 -C 6 )-alkyl,
R1, R3 and R4 are groups selected from hydrogen, halogen, hydroxy, nitro, trifluoromethyl, trifluoromethoxy, hydroxymethyl, (C 1 -C 6 )-alkoxy, (C 1 -C 6 )-alkoxycarbonyl, (C 6 -C 10 )-aryloxy or (C 1 -C 6 )-alkyl, and R5 is optionally substituted (C 6 -C 10 )-aryl, (C 5 -C 10 )-heteroaryl, (C 3 -C 8 )-cycloalkyl or (C 1 -C 7 )-alkyl.

NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS, AND THEIR PRODUCTION AND USE

OLEFINE DERIVATIVES

Diazacycloalkenes and the preparation thereof

The invention comprises compounds of the general formula: the acid addition and quaternary ammonium salts thereof (the latter having an alkyl group containing up to four carbon atoms) wherein R is an alkyl or alkenyl group containing up to eighteen carbon atoms; X is oxygen or sulphur; n is an integer from three to five; R1 is a hydrogen atom or an alkyl or alkenyl group containing up to six carbon atoms, the total number of carbon atoms in R and R1 being six to twenty-four; and further compounds wherein is two or three and adjacent carbon atoms in the heterocyclic ring form a conjugated system, and the preparation thereof (1) where X is sulphur and the heterocyclic residue is imidazole or pyrimidine, by reacting an alkyl or alkenyl halide with the sodium salt of a 2-mercaptoimidazole or 2-mercaptopyrimidine in an ether solvent at between 35 to 140 DEG C. for from about one to five hours; or (2) where X is sulphur and the heterocyclic residue is tetrahydropyrimidine ...

Photographic silver halide emulsions containing fog inhibiting or stabilizing agents

The following heterocyclic mercapto compounds are heated in aqueous solution with sodium chloroacetate to give the corresponding carboxymethylmercapto-derivatives; 1-phenyl-2-imidazole-thione, 2-mercaptopyrimidine and its 4, 6-diamino-, 4, 5, 6-triamino, 4-amino-6-hydroxy or 4-hydroxy-6-methylderivatives, 2-mercaptobenzoxazole, 2-mercaptobenzthiazole, 3-phenyl (or amino)-4-amino-5-mercapto- 1, 2, 4-triazole, 3-mercapto-5-hydroxy (or phenyl) 6-methyl-1, 2, 4-triazine and 2-mercapto-imidazoline and its 4-methyl-derivative. 2-Carboxymethylmercapto- 4, 6-diamino-S-triazine is prepared by adding chloroacetic acid to a solution of 4, 6-diamino-2-mercapto-s-triazine in aqueous sodium hydroxide. 2-(1-Carboxyoctylmercapto)-4, 6-diamino-S-triazine is prepared by stirring a solution of a -bromopelargonic acid and 4, 6-diamino-2-mercapto-s-triazine in aqueous sodium hydroxide. 2-Carboxymethylmercapto-imidazoline chloroacetate is prepared by p boiling 2-mercapto-imidazoline and chloroacetic acid in ...

PYRIMIDINYL -THIONO- THIOL-PHOSPHORIC-PHOSPHONIC ACID ESTERS AND THEIR USE AS INSECTICIDES ACARICIDES AND NEMATO CIDES

... 1477936 Pyrimidyl esters of phosphorus acids; pyrimidines BAYER AG 17 Oct 1975 [17 Jan 1975] 42636/75 Headings C2P and C2C The invention comprises compounds of formula (wherein R is C 1-9 alkyl; R 1 is C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkylthio or phenyl; R 2 is C 1-6 alkyl; R 3 is H or halo; R 4 is halo, SCN, C 1-4 alkoxy, C 1-4 alkylthio or C 2-4 -(alkoxycarbonyl); and X is O or S); and their preparation from the corresponding pyrimidin-2-ols (which may be in the form of hydrochloride, alkali metal, alkaline earth metal or ammonium salts) by reaction with (RO)(R 1 )P(X)-halogen, and an acid acceptor where necessary. Intermediates of formula (R5 = Me, Et, i-Pr) are prepared by reacting (CO 2 R5) 2 with (CH 3 ) 3 CCOCH 3 . 2 - Hydroxy - 4 - tert - butyl - 6 - (CO 2 R5)- pyrimidine hydrochloride is prepared from IV by reaction with urea and HC1. 2 - Hydroxy - 4 - methyl - 6 - chloropyrimidine sodium salt (V) is prepared from 2-methylthio- 4 - methyl - 6 - chloropyrimidine ...

5-(Trifluoromethyl) Pyrimidine derivative and production method therefor

FUNGICIDES

Azabicyclic carbamoyloxy mutilin derivatives for antibacterial use.

Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof: in which: R.1 is vinyl or ethyl; and R2 is a group R3, R4CH2~, or R5R6C=CH-; wherein each of R3 and R4 is an azabicyclic ring system or R5 and R^ together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

Certain 1, 4, 5-Tri-substituted imidazole compounds useful as cytokine.

This invention relates to certain 5-(optionally substituted aryl or heteroaryl)-4-(optionally substituted heteroaryl)-1-(optionally substituted heterocyclyl or heterocyclylalkyl)or -1- optionally substituted alkyl or alkenyl - imidazoles and derivatives thereof. Synthetic processes for the preparation of said tri-substituted imidazoles is described. The aforementioned imidazoles are useful for treating cytokine mediated diseases. The compounds of the invention are incorporated into pharmaceutical compositions for use in treating cytokine related diseases.

Aryl substituted pyrisines pyrimidines pyrazines and triazines and the use thereof

Fungicides

Compounds useful as fungicides ...

Aryl substituted pyridines, pyrimidines, pyrazines and triazines and the use thereof.

This invention relates aryl substituted pyridines, pyrimides, pyrazines and triazines of formula (i): or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein a1,a2,a3,r1-r4, x and y are set in the specification. The invention is also directed to the use of compounds of formula i for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegerative conditions such as amyotrophic lateral sclerosis (als), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus, agents, as anticonvulsants, and as antimaniac depressants,as local anesthetics, as antiarrhymics and for the treatment of prevention of diabetic neuropathy ...

Carbamoyloxy derivatives of mutiline and their use as antibacterials.

Derivatives of mutiline of formula (1a)and pharmaceutically acceptable salts and derivatives thereof, in which r1 is ethyl or vinyl, y is a carbamoyloxy group, which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Novel compounds

Novel compounds

FUNGICIDES

Novel compounds.

Compounds of formula (1a)and pharmaceutically acceptable salts and derivativews thereof in which y is a carbamoyloxy group, in which the n-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Novel herbicides

Novel herbicides

Anilides of acids thioglicolic carrying heterocyclic substances, which have fungicidal properties usable in phytiatrie.

Carbamoyloxy derivatives of mutiline and their useas antibacterials.

Acetyl 2-hydroxy-1,3 diaminoalkanes.

Acids (pyrimidyloxy) phenoxy-alkanecarboxylic, process for their preparation and their use as herbicides.

Nitrogenized heterocyclic compounds, just as their production and their use.

Aminoalkoxyphenyl derivatives process of preparation and compositions containing the same

Nematocide pyrimidine derivatives.

Nematocide pyrimidine derivatives.

Aryl substituted pyridines, pyrimidines, pyrazinesand triazines and the use thereof.

Synthesis of the isopropylamino-2 pyrimidin.

Certain 1, 4, 5-tri-substituted imidazole compounds useful as cytokine

New derivatives of the dithiole-1,2 and their method of preparation.

Fungicides.

Novel compounds

Carb moylo y der vativ s of utiline and their use as antibacterials

Novel compounds

Novel compounds

FUNGICIDES

FUNGICIDES

Aryl substituted pyrisines pyrimidines pyrazines and triazines and the use thereof

RETINOIDE FOR THE TREATMENT OF EMPHYSEM

NEUE VERBINDUNGEN, IHRE HERSTELLUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE ZUBEREITUNGEN

Compounds of formula I and salts thereof and their use for prevention and treatment of tumors. r ...

MALONONITRILVERBINDUNGEN AS PESTICIDES

PROCEDURE FOR the PRODUCTION OF 2-ISOPROPYLAMINOPYRIMIDIN

PROCEDURE FOR the PRODUCTION OF NEW ONES 2-AMINOUND/ODER 4-AMINO-5-ALKYLTHIOPYRIMIDINEN AND THEIR SALTS

ARYL ANILINE PRAY-PRAYING A2 ADRENERGIC RECEPTOR AGONISTE

4-PHENYL-6-SUBSTITUIERTE PYRIMIDIN-2 CARBONITRILDERIVATE

NEUE VERBINDUNGEN, IHRE HERSTELLUNG UND DIESE ENTHALTENDE PHARMAZEUTISCHE ZUBEREITUNGEN

SUBSTITUTED ANILIDDERIVATE, THEIR INTERMEDIATE PRODUCTS, CHEMICALS FOR THE AGRICULTURE AND THE HORTICULTURE AND THEIR USE

ARYL SUBSTITUTED PYRIDINEN, PYRIMIDINEN, PYRAZINEN AND TRIAZINEN AND THEIR USE

PROCEDURE FOR the PRODUCTION OF 2-ISOPROPYLAMINOPYRIMIDIN

PROCEDURE FOR THE PRODUCTION OF NEW SUBSTITUTED ONE PYRIMIDINYL (THIONO) - (THIOL) - PHOSPHORUS (PHOSPHON) - SOUR ESTERS

PROCEDURE FOR THE PRODUCTION OF NEW ONE 1.2 - DITHIOLDERIVATEN

4-PYRIMIDIN SULFENAMIDE AND YOUR USE IN INDIA RUBBER

RETROVIRALE PROTEASE INHIBITORS

THERAPEUTIC AMIDES

VERFAHREN ZUR HERSTELLUNG VON NEUEN 1,2-DITHIOLDERIVATEN

PROCEDURE FOR THE PRODUCTION OF PYRIMIDINDERIVATEN.

THIOFORMAMIDINE, PROCEDURE FOR THEIR PRODUCTION AND THEIR APPLICATION AS DRUGS.

LIQUIDCRYSTALLINE CYCLOPROPYL ALKYL OR - ALKENYL HETEROCYCLEN, PROCEDURE FOR YOUR PRODUCTION AND YOUR USE IN LIQUID CRYSTALLINE MIXTURES.

PRECDRUG OF MERCAPTOGRUPPEN ABSTENTION, BIOLOGICAL ACTIVE ONE MEANS, PROCEDURE FOR YOUR PRODUCTION AND THESE CONTAINING THERAPEUTIC ACTIVE MIXTURES.

SUBSTITUTED PYRIMIDIN-2-ONE AND THEIR SALTS.

AMIDE DERIVATIVES.

ANILID DERIVATIVES AS FUNGICIDES

NEW AMINO DICARBOXYLIC ACID DERIVATIVES WITH PHARMACEUTICAL CHARACTERISTICS

PHENETHYL-5-BROMOPYRIDYLTHIOHARNSTOFF (PBT) DERIVATIVES WITH SPERMIZIDER EFFECT

Novel Dihydropyrimidin-2(1H)-one Compounds as S-Nitrosoglutathione Reductase Inhibitors

The present invention is directed to novel dihydropyrimidin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

Viral polymerase inhibitors

Compounds of formula I: wherein X, R 2 , R 3 , R 3a , R 3b , R 5 and R 6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.

New compounds, pharmaceutical compositions and uses thereof

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

NOVEL IODO PYRIMIDINE DERIVATIVES USEFUL FOR THE TREATMENT OF MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS

Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound. 2. The compound of selected from the group set forth in Table 1.3. The compound of claim 1 , wherein X and Y are both N.4. The compound of claim 3 , wherein B is H.5. The compound of claim 1 , wherein A is halo claim 1 , B is A claim 1 , and X and Y are both N.6. The compound of claim 1 , wherein X is N claim 1 , and Y is CH.7. The compound of claim 6 , wherein B is H.8. The compound of claim 1 , wherein X is CH claim 1 , and Y is N.9. The compound of claim 8 , wherein B is H.10. The compound of claim 1 , wherein A is selected from the group consisting of indole claim 1 , quinoline claim 1 , and naphthalene.11. The compound of claim 1 , wherein the compound is 4-Iodo-6-(2-fluorophenyl)pyrimidine or 4-Iodo-6-(3-aminocarbonylphenyl)pyrimidine.13. The pharmaceutical composition of claim 12 , wherein the compound is selected from the group set forth in Table 1.15. The method of claim 14 , wherein the MIF-implicated disease is selected from the group consisting of inflammatory disease and cancer.16. The method of claim 15 , wherein the inflammatory disease is selected from the group consisting of dermatitis claim 15 , arthritis claim 15 , rheumatoid arthritis claim 15 , insulin-dependent diabetes claim 15 , proliferative vascular disease claim 15 , acute respiratory distress syndrome claim 15 , sepsis claim 15 , septic shock claim 15 , psoriasis claim 15 , asthma ...

THIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. 2. A compound of claim 1 , wherein one of X claim 1 , X claim 1 , Xor Xis N.4. A compound of claim 1 , wherein two of X claim 1 , X claim 1 , Xor Xare N.7. A compound of claim 1 , wherein{'sup': '3', 'sub': 3', '3', '3, 'Ris H, CH, OCH, CF, F or Cl; and'}{'sup': '4', 'sub': 3', '3', '3, 'Ris H, CH, OCH, CF, F or Cl.'}8. A compound of claim 7 , wherein Rand Rare both H.9. A compound of claim 1 , wherein Rand Rtogether with the carbon atoms to which they are attached form an optionally substituted 5- or 6-membered ring claim 1 , optionally containing one or two heteroatoms selected from O claim 1 , N and S claim 1 , wherein said 5- or 6-membered ring maybe a saturated claim 1 , an unsaturated or an aromatic ring.10. A compound of claim 1 , wherein Rand Rtogether with the carbon atoms to which they are attached form an optionally substituted claim 1 , 6-membered aromatic ring.12. A compound of claim 1 , wherein{'sup': 'a', 'sub': '3', 'Ris H or CH; and'}{'sup': 'b', 'sub': '3', 'Ris H or CH.'}13. A compound of claim 12 , wherein Rand Rare both CH.15. A compound of claim 14 , wherein{'sup': '1', 'Xis CH;'}{'sup': '2', 'Xis N;'}{'sup': '3', 'Xis CH; and'}{'sup': '4', 'Xis CH.'}16. A compound of claim 15 , wherein{'sup': 1', '1, 'Yis CR; and'}{'sup': 2', '2, 'Yis CR.'}17. (canceled)19. A compound of claim 18 , wherein R claim 18 , Rand Rare all H.20. A compound of claim 1 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- claim 1 , 4- claim 1 , 5- or 6-membered ring claim 1 , optionally containing one or two heteroatoms selected from O claim 1 , N and S.21. A compound of claim 20 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- ...

Thioacetate compounds, compositions and methods of use

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.

Compounds And Methods For Treating Candidiasis And Aspergillus Infections

The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a or species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an infection. 2. The method of wherein each X is S.3. The method of wherein each Ris claim 1 , independently claim 1 , —CH claim 1 , —(CH)—NH claim 1 , —(CH)—NH—C(═NH)NH claim 1 , or —(CH)—NH—C(═O)—R claim 1 , where each n is claim 1 , independently claim 1 , 1 or 2 claim 1 , and each Ris claim 1 , independently claim 1 , H or methyl.49-. (canceled)10. The method of wherein each Ris CF.11. The method of wherein each Vis H and each Vis claim 1 , independently claim 1 , —N—C(═O)—R claim 1 , where each Ris claim 1 , independently claim 1 , —(CH)—NHor —(CH)—NH—C(═NH)NH claim 1 , where each n is claim 1 , independently claim 1 , 1 to 4.1218-. (canceled)19. The method of wherein each Vis H and each Vis —S—R claim 1 , where each Ris —(CH)—NHwhere each n is 2.20. The method of wherein each Ris H claim 1 , —S—(CH)—NH claim 1 , or —S—(CH)—NH—C(═NH)NH claim 1 , where each m is claim 1 , independently claim 1 , 1 to 4.2123-. (canceled)24. The method of wherein:each X is S;{'sup': '1', 'sub': 2', 'n', '2', '2', 'n', '2, 'each Ris, independently, —(CH)—NHor —(CH)—NH—C(═NH)NH, where each n is, independently, 1 to 4;'}{'sup': '2', 'sub': 3', '3', '3, 'each Ris, independently, halo, CF, or C(CH); and'}{'sup': 1', '2', '5', '5, 'sub': 2', 'n', '2, 'each Vis H and each Vis, independently, —S—R, where each Ris, independently, —(CH)—NH, where each n is, independently, 1 to 4.'}2532-. (canceled)3553-. (canceled)5576-. (canceled)7880-. (canceled)82122-. (canceled)124159-. (canceled)161179-. (canceled)181198-. (canceled)200218-. (canceled)220237-. (canceled)239243-. (canceled)245252-. (canceled) The present disclosure was supported by funds from the U.S. Government (NIH/NIDCR Grant No. 2R44DE018371-02) and the U.S. Government may therefore have certain rights in the ...

Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof

Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.

Iminopropene compound and use thereof

The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.

THIOPYRIMIDINE-BASED COMPOUNDS AND USES THEREOF

The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases. 2. The compound according to claim 1 , wherein W is absent claim 1 , CO or Calkylene.3. The compound according to claim 1 , wherein Ris aryl; heterocyclyl; Calkyl; or aryl substituted with 1 to 3 substituents selected from NRR claim 1 , NRCOR claim 1 , CN claim 1 , OCalkyl claim 1 , OH claim 1 , COR claim 1 , CONRR claim 1 , CONRR claim 1 , NRCOR claim 1 , substituted or unsubstituted Calkyl claim 1 , SR claim 1 , CHO and substituted or unsubstituted heterocyclyl.4. The compound according to claim 1 , wherein Ris aryl claim 1 , imidazolyl; (methylenedioxy)phenyl; or aryl substituted with 1 to 4 substituents selected from an N-containing 5 or 6 membered heterocyclyl; substituted or unsubstituted OCalkyl; NRCOR claim 1 , wherein in this instance only Ris H claim 1 , and Ris Calkyl claim 1 , Calkenyl claim 1 , Calkynyl or CN; NH; halo; COR; SONRR; NO; NHSOMe; CHOHCFCH; CHNHSOMe; OH; and SH.5. The compound according to claim 1 , wherein Ris H; Calkyl; halogen; Calkenyl; substituted or unsubstituted amino; cyano; nitro; methoxy; aryl; or 5 or 6 membered heterocyclyl containing 1 or 2 N atoms.8. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.9. An implant comprising a compound of .10. A method for the treatment of a kinase associated disease which comprises administering a therapeutically effective amount of a compound of or a pharmaceutical composition comprising a compound of to a human in ...

THIOPYRIMIDINE-BASED COMPOUNDS AND USES THEREOF

The present invention relates to thiopyrimidine-based compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2 or JAK3 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases and vascular diseases. 5. The method of claim 1 , wherein W is absent claim 1 , CO or Calkylene.6. The method of claim 1 , wherein Ris H; Calkyl; halo; Calkenyl; amino which may be substituted with Calkenyl; cyano; nitro; methoxy; aryl; or 5 or 6 membered heterocyclyl containing 1 or 2 N atoms which may be substituted with trimethylcarboxy.7. The method of claim 1 , wherein the therapeutically effective amount of said compound is administered using an implant claim 1 , wherein said implant comprises a compound of or a pharmaceutical composition comprising a compound of .8. The method of claim 1 , wherein the kinase associated disease is an immunological disease claim 1 , an inflammatory disease claim 1 , a hyperproliferative disease claim 1 , a viral disease claim 1 , a metabolic disease or a vascular disease.9. A method for suppressing the immune system of a human in need thereof claim 1 , wherein said method comprises administering a therapeutically effective amount of a compound of or a pharmaceutical composition comprising a compound of .10. A method of inhibiting a kinase in a cell claim 1 , wherein said method comprises contacting the cell with a compound of . This application is a continuation of, and claims priority to, U.S. patent application Ser. No. 12/524,849, filed Nov. 20, 2009, which is the national phase of PCT Appln. No. PCT/AU2008/000103, filed Jan. 31, 2008, which in turn claims priority to U.S. Provisional Appln. No. 60/898,898, filed ...

Benzamide derivatives as p2x7 receptor antagonists

The invention relates to benzamide derivatives of formula (I), wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.

METHOD FOR TREATING MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS WITH IODO PYRIMIDINE DERIVATIVES

Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula I: 2. The method of claim 1 , wherein the MIF-implicated disease is selected from the group consisting of inflammatory disease and cancer.3. The method of claim 2 , wherein the inflammatory disease is selected from the group consisting of dermatitis claim 2 , arthritis claim 2 , rheumatoid arthritis claim 2 , insulin-dependent diabetes claim 2 , proliferative vascular disease claim 2 , acute respiratory distress syndrome claim 2 , sepsis claim 2 , septic shock claim 2 , psoriasis claim 2 , asthma claim 2 , cytokine related toxicity claim 2 , lupus claim 2 , multiple sclerosis claim 2 , transplant-host response claim 2 , and autoimmune disorders.4. The method of claim 1 , wherein the MIF-implicated condition is caused by a MIF-producing pathogen.5. The method of claim 4 , wherein the MIF-producing pathogen is selected from the group consisting of parasitic helminths claim 4 , spirochetes claim 4 , and plasmodium.6. The method of claim 1 , wherein:A is a substituted or unsubstituted 5- or 6-membered aromatic ring having 0 or 1 heteroatoms selected from the group consisting of N and S;B is H;X and Y are both N,and further wherein the MIF inhibitory compound interacts with a MIF polypeptide present in the patient in need thereof to inhibit an enzymatic activity of the MIF polypeptide.7. The method of claim 1 , wherein the MIF inhibitory compound is selected from the group consisting of:4-Iodo-6-(2,3-difluoro-4-methoxyphenyl)pyrimidine;4-Iodo-6-(2-fluorophenyl)pyrimidine;4-Iodo-6-(pyridin-3-yl)pyrimidine;4-Iodo-6-(3-fluorophenyl)pyrimidine;4-Iodo-6-(2-fluoropyridin-3-yl)pyrimidine;4-Iodo-6-(3-fluoro-4-methoxyphenyl)pyrimidine;4-Iodo-6-(2,4-difluorophenyl)pyrimidine;4-Iodo-6-(2-chlorophenyl)pyrimidine;4-Iodo-6-(2,4,5-trifluorophenyl)pyrimidine;4-Iodo-6-(2,4-difluoropyridin-3-yl)pyrimidine;4-Iodo-6-(thiophen-2-yl)pyrimidine; and4-Iodo-6-(3,4- ...

BICYCLO [2.2.1] ACID GPR120 MODULATORS

The present invention provides compounds of Formula (I): (I) or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR120 G protein-coupled receptor modulators which may be used as medicaments.

COMPOUNDS AND COMPOSITIONS FOR USE IN AUGMENTATION OF GLUCOSE

The present invention is directed to compounds such as: formula wherein linker is independently selected from the group consisting of —S—, —S—S—, —S—(CH2)n—, —NH—, —NH—(CH2)n—, —O—, —S02-, arylene, heteroarylene; R1 is selected from the group consisting of straight or branched C4-C20 alkyl, straight or branched C4-C20 alkenyl, straight or branched C4-C20 alkynyl, each optionally interrupted with at least one NH, C5-C7 saturated cycloalkyl or heteroalkyl ring, C5-C12 aromatic or heteroaromatic ring, each optionally substituted with at least one group selected from —COOH, —NH2, C1-C8 alkoxy, C1-C5 amidyle, C1-C5 carboxyl, halogen; and R2 is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, CN, C1-C8 alkoxy, C1-C5 carboxylic acid, straight or branched C1-C8 alkyl, straight or branched C2-C10 alkenyl, straight or branched C2-C12 alkynyl each optionally substituted by at least one substituent selected from the group consisting of C1-C5 alkoxy, C1-C5 carboxylic acid, OH, SH, NH2, halogen; and compositions for use in the treatment of diabetes and related disorders. 132-. (canceled)34. A compound of claim 33 , wherein at least one of Xto Xis O.35. A compound of claim 33 , wherein at least two of Xto Xare O.36. A compound of claim 33 , wherein least one of Xto Xis CHR.37. A compound of claim 33 , wherein Ris aryl or heretroaryl.38. A compound of claim 33 , wherein Y and Z are identical.39. A compound of claim 33 , wherein Y and Z are S.41. A compound of claim 33 , being used as a medicament.42. A composition comprising a compound according to .43. A method of treating or preventing a condition claim 33 , symptom or disease associate with elevated blood glucose levels in a subject in need thereof claim 33 , said method comprising administering to said subject a compound of .44. A method for the treatment or prevention of at least one condition selected from hyperglycemia claim 33 , diabetes claim 33 , altered insulin secretion claim 33 , ...

BUMETANIDE DERIVATIVES FOR THE THERAPY OF HYPERHIDROSIS

The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions comprising these compounds for use in the treatment or prevention of diseases/disorders involving Na—K2Cl-cotransporters (NKCCs), and particularly for use in the treatment or prevention of hyperhidrosis. 3. The compound for use according to claim 2 , wherein Ris —COO—(Calkyl) claim 2 , wherein the alkyl moiety of said —COO—(Calkyl) is optionally substituted with one or more groups independently selected from halogen claim 2 , —CF claim 2 , —CN claim 2 , —NO claim 2 , —NH claim 2 , —NH(Calkyl) claim 2 , —N(Calkyl)(Calkyl) claim 2 , —OH claim 2 , —O(Calkyl) claim 2 , —SH and —S(Calkyl) claim 2 , and further wherein one or two —CH— units comprised in the alkyl moiety of said —COO—(Calkyl) are each optionally replaced by a group independently selected from —O— claim 2 , —CO— claim 2 , —COO— claim 2 , —O—CO— claim 2 , —NH— claim 2 , —N(Calkyl)- claim 2 , —NH—CO— claim 2 , —N(Calkyl)-CO— claim 2 , —CO—NH— claim 2 , —CO—N(Calkyl)- claim 2 , —S— claim 2 , —SO— claim 2 , —SO— claim 2 , —SO—NH— claim 2 , —SO—N(Calkyl)- claim 2 , —NH—SO— and —N(Calkyl)-SO—.4. The compound for use according to or claim 2 , wherein Ris —COO—CH.5. The compound for use according to claim 2 , wherein Ris —COOH.6. The compound for use according to claim 2 , wherein Ris selected from —(Calkylene)-NH—(Calkylene)-R claim 2 , —COO—(Calkylene)-R claim 2 , —O—CO—(Calkylene)-R claim 2 , —CO—(Calkylene)-R claim 2 , —CO—NH—(Calkylene)-R claim 2 , —CO—N(Calkyl)-(Calkylene)-R claim 2 , —NH—CO—(Calkylene)-Rand —N(Calkyl)-CO—(Calkylene)-R claim 2 , wherein Ris independently selected from —CF claim 2 , —CN and halogen.7. The compound for use according to or claim 2 , wherein Ris —(Calkylene)-NH—(Calkylene)-CF.8. The compound for use according to any one of to claim 2 , wherein Ris hydrogen.9. The compound for use according to any one of to claim 2 , wherein Ris selected from —SO—NH claim 2 , —SO—NH(Calkyl ...

HEAT SHOCK PROTEIN BINDING COMPOUNDS, COMPOSITIONS, AND METHODS FOR MAKING AND USING SAME

The present subject matter relates to a compound represented by the general formula (I) or (I′) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70). 142-. (canceled)44. The pharmaceutical composition according to claim 43 , wherein:{'sub': '2', 'Y is S, SO, or SO;'}Z is alkenyl, alkynyl, saturated or unsaturated cycloalkyl, saturated or unsaturated heterocycle, halogen, hydroxyl, alkoxy, dialkylamino, cycloalkylamino, arylamino, or diarylamino;{'sub': 1', '2, 'Wand Ware independently hydrogen, alkyl, alkenyl, alkynyl, aryl, alkoxy, amino, alkylamino, dialkylamino, cycloalkylamino, arylamino, or diarylamino; and'}{'sub': 3', '4', '2', '2, 'Wand Ware independently hydrogen, halogen, hydroxyl, cyano, aryloxy, alkoxy, halogenated alkoxy, alkenyloxy, hydroxyalkyl, amino, alkylamino, dialkylamino, cycloalkylamino, arylamino, diarylamino, acylamino, carbamyl, substituted and unsubstituted amido, alkylamido, alkylsulfonamido, sulfonamido, —NHSOalkenyl, —NHCOalkenyl, —NHCOalkynyl, —COalkenyl, —COalkynyl, trihalocarbon, thioalkyl, —SO-alkyl, —COO-alkyl, —COalkyl, or alkyl-CN.'}46. The pharmaceutical composition according to claim 43 , wherein Y is S claim 43 , SO claim 43 , or SO.47. The pharmaceutical composition according to claim 43 , wherein Z is alkenyl claim 43 , alkynyl claim 43 , ...

Ror gamma (rory) modulators

Treatment methods including administering a compound according to Formula (I) Meta or para or a pharmaceutically acceptable salt thereof wherein: A 11 -A 14 are N or CR 11 , CR 12 , CR 13 , CR 14 , respectively, with the proviso that no more than two of the four positions A in A 11 -A 14 are simultaneously N; A 6 , A 7 , A 8 , A 9 , A 10 are N or CR 6 , CR 7 , CR 8 , CR 9 , CR 10 , respectively, with the proviso that at least one but no more than two of the five positions A in A 6 , A 7 , A 8 , A 9 , A 10 is N; R 1 is C(2-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1-3)alkyl)amino; R 5 is H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5) heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl; —SO 2 R 1 is represented by one of R 7 , R 8 or R 9 ; R 15 is H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl; R 16 is C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl.

NOVEL VIRAL REPLICATION INHIBITORS

The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity. 2. The compound according to claim 1 , wherein Ris —C(O)OH.3. The compound according to claim 1 , wherein Ris selected from aryl or heteroaryl claim 1 , wherein said aryl or heteroaryl can be unsubstituted or substituted with one or more Z.4. The compound according to claim 3 , wherein Ris selected from benzothiazolyl claim 3 , quinolinyl claim 3 , piperidinyl claim 3 , 1-H-azepinyl claim 3 , 4-methyl-piperazinyl claim 3 , naphtyl claim 3 , benzothiophenyl claim 3 , benzofuranyl claim 3 , indazolyl claim 3 , N-methyl-indazolyl claim 3 , chromanyl claim 3 , 4H-isoquinolinyl claim 3 , isochromanyl claim 3 , 5-F-8-Me-isochromanyl claim 3 , 5 Cl-isochromanyl claim 3 , t-butyl claim 3 , ethyl claim 3 , phenyl claim 3 , and phenyl substituted with 1 claim 3 , 2 or 3 substituents independently selected from the group consisting of C-C-alkyl claim 3 , chloro claim 3 , fluoro claim 3 , hydroxy claim 3 , methoxy claim 3 , trifluoromethyl.5. The compound according to claim 1 , wherein one of Rand Ris hydrogen claim 1 , and the other of Rand Ris selected from hydrogen; cyano; alkyl; ...

KETONE INHIBITORS OF LYSINE GINGIPAIN

The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium . Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with infection, including brain disorders such as Alzheimer's disease. 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of Ccycloalkyl claim 1 , Calkyl claim 1 , Caryl claim 1 , and 5- to 12-membered heteroaryl each of which is optionally substituted with one or more Rsubstituents claim 1 , and each Ris independently selected from the group consisting of halogen claim 1 , —N claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Calkoxy claim 1 , Chaloalkoxy claim 1 , —N(R) claim 1 , —N(R) claim 1 , and —NRC(O)R.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris Calkyl substituted with Calkoxy.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen.67-. (canceled)8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris Chaloalkyl.9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —CHR claim 1 , Ris —O—R claim 1 , and Ris 5- to 12-membered heteroaryl claim 1 , which is optionally substituted with one or more members independently selected from the group consisting of halogen and Calkyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of —N(R) claim 1 , 5- to 12-membered heteroaryl claim 1 , and 3- to 12-membered heterocyclyl claim 1 , wherein:{'sub': 1-3', '1-3, '5- to 12-membered heteroaryl is optionally substituted with one or more members ...

Inhibitors of alpha-amino-beta-carboxymuconic acid semialdehyde decarboxylase

The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD + biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament.

METHOD OF PRODUCING PENTAFLUOROSULFANYL AROMATIC COMPOUND

A method of producing a pentafluorosulfanyl aromatic compound is provided. A method of producing a pentafluorosulfanyl aromatic compound represented by general formula (3): 1. A method of producing a pentafluorosulfanyl aromatic compound represented by general formula (3):{'br': None, 'sub': 5', 'k, 'Ar—(SF)\u2003\u2003(3)'}wherein Ar is a substituted or an unsubstituted aryl group or heteroaryl group andk is an integer of 1 to 3;{'sub': '5', 'claim-text': {'br': None, 'sub': 4', 'k, 'Ar—(SFHal)\u2003\u2003(2)'}, 'the method comprising reacting IFwith a halotetrafluorosulfanyl aromatic compound represented by general formula (2)wherein Ar and k are defined as above; andHal is a Cl group, a Br group, or an I group.2. The method according to claim 1 , wherein the aryl group or heteroaryl group has a substituent selected from the group consisting of a halogen group claim 1 , an electron-withdrawing group excluding halogen groups claim 1 , and an electron-donating group excluding halogen groups.4. The method according to claim 1 , wherein the substituent is an electron-withdrawing group excluding halogen groups claim 1 , and the reaction is performed at 50° C. or higher.5. The method according to claim 1 , wherein the substituent is an electron-withdrawing group excluding halogen groups claim 1 , and 1 equivalent or more of IFis used for the SFHal group claim 1 , that is the halotetrafluorosulfanyl aromatic compound represented by general formula (2).6. The method according to claim 3 , wherein:at least one of X and Y is N; andat least one of R is an electron-withdrawing group excluding halogen groups, the electron-withdrawing group being present at the 3-position of the ring. The present invention relates to a method of producing a pentafluorosulfanyl aromatic compound.A pentafluorosulfanyl group (hereinafter, referred to as SFgroup) has been drawing attention as a very promising material. For the unique physicochemical characteristics, the SFgroup is attracting ...

SPECIFIC CARBOXAMIDES AS KCNQ2/3 MODULATORS

The invention relates to specific carboxamides, to processes for their preparation, to medicaments comprising these compounds and to the use of these compounds in the preparation of medicaments. 3. The compound according to claim 1 , wherein{'sup': '1', 'Arepresents S; and'}{'sup': 2', '12', '13, 'sub': '2', 'claim-text': {'sup': 12', '13, 'wherein Rand Rboth represent H or both represent F.'}, 'Arepresents S, S(═O)or CRR,'}4. The compound according to claim 1 ,wherein{'sup': 3', '7', '4', '7', '5', '7', '6', '7, 'n denotes 1 and Arepresents CR, Arepresents CR, Arepresents CRand Arepresents CR; or'}{'sup': 3', '4', '7', '5', '7', '6', '7, 'n denotes 1 and Arepresents N, Arepresents CR, Arepresents CRand Arepresents CR; or'}{'sup': 3', '7', '4', '5', '7', '6', '7, 'n denotes 1 and Arepresents CR, Arepresents N, Arepresents CRand Arepresents CR; or'}{'sup': 3', '7', '4', '7', '5', '6', '7, 'n denotes 1 and Arepresents CR, Arepresents CR, Arepresents N and Arepresents CR; or'}{'sup': 3', '4', '5', '7', '6', '7, 'n denotes 1 and Arepresents N, Arepresents N, Arepresents CRand Arepresents CR; or'}{'sup': 3', '4', '7', '5', '6', '7, 'n denotes 1 and Arepresents N, Arepresents CR, Arepresents N and Arepresents CR; or'}{'sup': 3', '4', '7', '5', '7', '6, 'n denotes 1 and Arepresents N, Arepresents CR, Arepresents CRand Arepresents N; or'}{'sup': 3', '7', '4', '5', '7', '6, 'n denotes 1 and Arepresents CR, Arepresents N, Arepresents CRand Arepresents N; or'}{'sup': 3', '7', '4', '5', '6', '7, 'n denotes 1 and Arepresents CR, Arepresents N, Arepresents N and Arepresents CR; or'}{'sup': 3', '7', '4', '7', '5', '6, 'n denotes 1 and Arepresents CR, Arepresents CR, Arepresents N and Arepresents N; or'}{'sup': 3', '4', '7', '5', '7, 'n denotes 0 and Arepresents S, Arepresents CRand Arepresents CR;'}or{'sup': 3', '4', '7', '5, 'n denotes 0 and Arepresents S, Arepresents CRand Arepresents N;'}or{'sup': 3', '4', '7', '5', '7, 'n denotes 0 and Arepresents O, Arepresents CRand ...

ADMINISTRATION OF AURORA KINASE INHIBITORS FOR ANTI-MALARIAL THERAPY

Novel compositions and methods for the treatment and prevention of malaria are disclosed herein. 1. A composition comprising one or more of compounds 1 , 2 , 3 , 4 , 5 , 6 , or 7 or a derivative thereof , or pharmaceutically acceptable salt of the foregoing.2. The composition of claim 1 , further comprising one or more of compounds 101 claim 1 , 102 claim 1 , 103 claim 1 , 104 claim 1 , 105 claim 1 , 106 claim 1 , DC-5156 claim 1 , DC-5154 or DC-5146 or a derivative thereof claim 1 , or pharmaceutically acceptable salt of the foregoing.3. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'an effective amount of the composition of ; and'}a pharmaceutically acceptable carrier.4. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00002', 'claim 2'}, 'an effective amount of the composition of ; and'}a pharmaceutically acceptable carrier.5. (canceled)6. (canceled)7. (canceled)8. A method for treating a condition in a subject in need claim 1 , the method comprising administering to the subject an effective amount of a composition comprising one or more of compounds 1 claim 1 , 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , 101 claim 1 , 102 claim 1 , 103 claim 1 , 104 claim 1 , 105 claim 1 , 106 claim 1 , DC-5156 claim 1 , DC-5154 or DC-5146 wherein the condition comprises of a symptom of malaria.9. The method of claim 8 , wherein composition further comprises a pharmaceutically acceptable carrier.10. The method of claim 8 , further comprising co-administering a conjunctive anti-malarial agent to the subject.11F. Plasmodium. The method of claim 1 , wherein treating malaria comprises killing or arresting the growth of in a subject in need thereof.12. (canceled)14. The compound of claim 13 , wherein Ris 3 carbon straight alkyl chain.15. The compound of claim 14 , wherein when Ris 3 carbon straight alkyl chain claim 14 , R′ is A claim 14 , B claim 14 , or C.16. The compound of claim 13 , ...

HETROARYLAMINE COMPOUNDS FOR MODULATING THE HEDGEHOG PATHWAY AND PREPARING METHOD AND USES THEREOF

The present invention provides a compound of formula (I) wherein X, Y, Z, Z, R, R, A, B, p and q are as disclosed in the specification. A pharmaceutical composition and a method for modulating the Hedgehog pathway are also provided. The present invention further provides a process for preparing the compound. 2. The compound according to claim 1 , wherein at least one of X and Y is N; both Zand Zare CH claim 1 , or one of Zand Zis N and the other is CH; Ris NH claim 1 , OR claim 1 , NHR claim 1 , SRor SOR; Ris optionally substituted alkyl; Ris aryl claim 1 , heteroaryl claim 1 , or heterocycloalkyl claim 1 , which are optionally substituted with 1 claim 1 , 2 claim 1 , or 3 R; Ris halo claim 1 , hydroxy claim 1 , mercapto claim 1 , cyano claim 1 , nitro claim 1 , amino claim 1 , alkyl claim 1 , alkoxy claim 1 , alkylamino claim 1 , dialkylamino claim 1 , cycloalkyl claim 1 , haloalkyl claim 1 , or haloalkoxy; A is hydrogen claim 1 , halo claim 1 , cyano claim 1 , amino claim 1 , alkyl claim 1 , haloalkyl claim 1 , alkoxy claim 1 , or haloalkoxy claim 1 , wherein the alkyl and alkoxy are optionally substituted; B is hydrogen claim 1 , halo claim 1 , cyano claim 1 , amino claim 1 , alkyl claim 1 , haloalkyl claim 1 , alkoxy claim 1 , haloalkoxy claim 1 , alkylaminoalkyl claim 1 , alkylaminodialkyl claim 1 , or alkyl-heterocycloalkyl claim 1 , wherein the alkyl and alkoxy are optionally substituted; p is 0 claim 1 , 1 claim 1 , or 2; and q is 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3.3. The compound according to claim 2 , wherein both X and Y are N claim 2 , or claim 2 , X is CH and Y is N; both Zand Zare CH claim 2 , or Zis N and Zis CH; Ris NH claim 2 , OR claim 2 , NHR claim 2 , SRor SOR; Ris optionally substituted alkyl; Ris aryl or heteroaryl claim 2 , which is optionally substituted with 1 claim 2 , 2 claim 2 , or 3 R; Ris halo claim 2 , cyano claim 2 , alkyl claim 2 , or haloalkoxy; A is hydrogen or halogen; B is cyano claim 2 , halo claim 2 , alkyl claim 2 , ...

TREATMENT OF PULMONARY AND OTHER CONDITIONS

Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: 5. The method of claim 1 , wherein Xand Xare each optionally-substituted pyrazinyl or optionally-substituted pyrimidinyl.6. The method of claim 1 , wherein Xand Xare each the same.7. The method of claim 1 , wherein Xand Xare each different.8. The method of claim 1 , wherein —S—Ris a N-acetylcysteine moiety claim 1 , a 2-mercaptoethane sulfonate moiety claim 1 , or glutathione moiety.11. The method of claim 1 , wherein the compound is administered to the subject via inhalation.12. The method of claim 1 , wherein the compound is administered via direct pulmonary delivery.13. The method of claim 1 , wherein the pulmonary disease is pulmonary fibrosis claim 1 , chronic obstructive pulmonary disease (COPD) claim 1 , asthma claim 1 , cystic fibrosis claim 1 , acute lung injury (ALI) claim 1 , acute respiratory distress syndrome claim 1 , pulmonary hypertension claim 1 , lung cancer claim 1 , or pulmonary manifestations of cystic fibrosis.14. The method of claim 4 , wherein the pulmonary disease is pulmonary fibrosis claim 4 , chronic obstructive pulmonary disease (COPD) claim 4 , asthma claim 4 , cystic fibrosis claim 4 , acute lung injury (ALI) claim 4 , acute respiratory distress syndrome claim 4 , pulmonary hypertension claim 4 , lung cancer claim 4 , or pulmonary manifestations of cystic fibrosis.15. The method of claim 9 , wherein the compound is administered to the subject via inhalation.17. The method of claim 16 , wherein the ischemia and reperfusion is consequent to transplanting of an organ in the subject.18. The method of claim 16 , wherein the compound is administered to a donor prior to removal of the organ.19. The method of claim 16 , wherein the compound is provided to the transplanted organ between the time of removal from a donor and placement in a recipient.20. The method of claim 16 , wherein the organ is a lung. This application is a divisional of U. ...

TREATMENT OF PULMONARY AND OTHER CONDITIONS

Disclosed is a compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: 18-. (canceled)9. A compound , or a pharmaceutically acceptable salt or ester thereof , comprising an adduct of a hydrophilic thiol and an enone that comprises at least two N-heterocycles.1415-. (canceled)16. The compound of claim 12 , wherein Xand Xare each optionally-substituted pyrazinyl or optionally-substituted pyrimidinyl.17. The compound of claim 16 , wherein Xand Xare each the same.18. The compound of claim 16 , wherein Xand Xare each different.19. The compound of claim 12 , wherein Ris an acylamino-substituted carboxylalkyl claim 12 , a sulfonate-substituted alkyl claim 12 , or an acylamino-substituted amido.20. The compound of claim 12 , wherein —S—Ris a derivative of N-acetylcysteine claim 12 , 2-mercaptoethane sulfonate claim 12 , or glutathione.21. A pharmaceutical composition comprising a compound of claim 10 , and at least one pharmaceutically acceptable excipient.22. The pharmaceutical composition of claim 21 , wherein the composition is in the form of an aerosol.23. The pharmaceutical composition of claim 21 , wherein the composition is in the form of a dry powder.24. A method for treating a pulmonary disease in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a compound claim 21 , or a pharmaceutically acceptable salt or ester thereof claim 21 , {'br': None, 'sup': 1', '2, 'X-L-X'}, 'having a structure ofwherein L is a linking moiety comprising an enone; and{'sup': 1', '2, 'Xand Xare each independently an optionally-substituted N-heterocycle.'}25. The method of claim 24 , wherein the compound is administered to the subject via inhalation.26. The method of claim 24 , wherein the compound is administered via direct pulmonary delivery.27. A method for treating a pulmonary disease in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a ...

Aryloxyurea compound and pest control agent

The present invention provides an aryloxyurea compound or salt thereof, and a pest control agent including the aryloxyurea compound or salt thereof as an active ingredient. The aryloxyurea compound has a superior acaricidal and/or insecticidal activity, superior safety, and can be synthesized advantageously and industrially. The compound of the present invention includes aryloxyurea compounds represented by the following formula or salts thereof: in the formula, Cy represents an unsubstituted or X-substituted phenyl group or the like, X represents a halogen atom or the like, R 1 represents an ethyl group or the like, R 2 represents a hydrogen atom or the like, R 3 and R 4 represents a methyl group or the like, X 1 represents a methylthio group or the like, m1 represents an integer of 1 to 4, X 2 represents a methyl group or the like, m2 is an integer of 0 to 3.

USE OF SMALL MOLECULE INHIBITORS TO KLF10 FOR MODULATION OF T REGULATORY CELLS AND CANCER IMMUNOTHERAPY

The invention relates to compositions and methods for inhibiting Krüppel-like Factor 10 (KLF10) for modulation of T regulatory cells and cancer immunotherapy. 6. A method of modulating an immune response claim 1 , comprising: administering to a subject an effective amount of an inhibitor of KLF10 claim 1 , wherein the inhibitor of KLF10 is a compound of .7. A method of modulating an immune response claim 2 , comprising: administering to a subject an effective amount of an inhibitor of KLF10 claim 2 , wherein the inhibitor of KLF10 is a compound of .8. A method of modulating an immune response claim 3 , comprising: administering to a subject an effective amount of an inhibitor of KLF10 claim 3 , wherein the inhibitor of KLF10 is a compound of .9. A composition claim 1 , comprising: an effective amount of an inhibitor of KLF10 to decrease T regulatory (T reg) cells at a tumor site or a pathogen infected area of a subject claim 1 , wherein the inhibitor of KLF10 is a compound of .10. A composition claim 2 , comprising: an effective amount of an inhibitor of KLF10 to decrease T regulatory (T reg) cells at a tumor site or a pathogen infected area of a subject claim 2 , wherein the inhibitor of KLF10 is a compound of .11. A composition claim 3 , comprising: an effective amount of an inhibitor of KLF10 to decrease T regulatory (T reg) cells at a tumor site or a pathogen infected area of a subject claim 3 , wherein the inhibitor of KLF10 is a compound of .12. A composition claim 1 , comprising: an effective amount of an inhibitor of KLF10 to decrease T regulatory (T reg) cells at a tumor site or a pathogen infected area of a subject in combination with one or more disease antigens claim 1 , wherein the inhibitor of KLF10 is a compound of .13. A composition claim 2 , comprising: an effective amount of an inhibitor of KLF10 to decrease T regulatory (T reg) cells at a tumor site or a pathogen infected area of a subject in combination with one or more disease antigens claim 2 , ...

Compounds having multimodal activity against pain

wherein the meanings for the various substituents are as disclosed in the description, having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the NET receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

THIOETHER COMPOUNDS AS NITRIFICATION INHIBITORS

Provided herein are a use of thioether compounds of formula I as nitrification inhibitors, and agricultural mixtures and compositions including the thioether compounds. 2. The thioether compound of claim 1 , wherein in the compound of formula I{'sup': 1', '2, 'Rand Rare H; and'}p is 1 or 2.6. A composition for use in reducing nitrification comprising at least one compound of formula I as defined in and at least one carrier.7. An agrochemical mixture comprising (i) at least one fertilizer; and (ii) at least one compound of formula I as defined in .8. (canceled)9. (canceled)10. A method for reducing nitrification claim 1 , the method comprising treating a plant growing on at least one of soil claim 1 , soil substituents claim 1 , and a locus claim 1 , soil claim 1 , and soil substituents where the plant is growing or is intended to grow with at least one compound of formula I as defined in .11. The method of claim 10 , further comprising providing the at least one of the plant and the locus claim 10 , soil claim 10 , and soil substituents where the plant is growing or is intended to grow with a fertilizer.12. The method of claim 11 , wherein the treating with the compound of formula I and the providing of the fertilizer are carried out simultaneously.13. A method for treating at least one of a fertilizer and a fertilizer composition claim 1 , comprising applying a nitrification inhibitor as defined in to the at least one of the fertilizer and the fertilizer composition.14. The agrochemical mixture of claim 7 , wherein the fertilizer is selected from the group consisting of a solid ammonium-containing inorganic fertilizer claim 7 , a liquid ammonium-containing inorganic fertilizer claim 7 , a solid organic fertilizer claim 7 , a liquid organic fertilizer claim 7 , and a urea-containing fertilizer.15. The method of claim 10 , wherein the plant is an agricultural plant claim 10 , a vegetable claim 10 , sorghum; a silvicultural plant; an ornamental plant; and a ...

THIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. 26.-. (canceled)7. A compound of claim 1 , wherein{'sup': '3', 'sub': 3', '3', '3, 'Ris H, CH, OCH, CF, F or Cl; and'}{'sup': '4', 'sub': 3', '3', '3, 'Ris H, CH, OCH, CF, F or Cl.'}8. (canceled)9. A compound of claim 1 , wherein Rand Rtogether with the carbon atoms to which they are attached form an optionally substituted 5- or 6-membered ring claim 1 , optionally containing one or two heteroatoms selected from O claim 1 , N and S claim 1 , wherein said 5- or 6-membered ring maybe a saturated claim 1 , an unsaturated or an aromatic ring.10. (canceled)12. A compound of claim 1 , wherein{'sup': 'a', 'sub': '3', 'Ris H or CH; and'}{'sup': 'b', 'sub': '3', 'Ris H or CH.'}13. A compound of claim 12 , wherein Rand Rare both CH.14. (canceled)15. A compound of claim 13 , wherein{'sup': '1', 'Xis CH;'}{'sup': '2', 'Xis N;'}{'sup': '3', 'Xis CH; and'}{'sup': '4', 'Xis CH.'}16. A compound of claim 15 , wherein{'sup': 1', '1, 'Yis CR; and'}{'sup': 2', '2, 'Yis CR.'}18. (canceled)19. A compound of claim 16 , wherein R claim 16 , Rand Rare all H.20. A compound of claim 1 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3- claim 1 , 4- claim 1 , 5- or 6-membered ring claim 1 , optionally containing one or two heteroatoms selected from O claim 1 , N and S.21. (canceled)22. A compound of claim 20 , wherein Rand Rtogether with the carbon atom to which they are attached form a 3-membered ring.23. A compound of claim 1 , wherein M is H.24. A compound of claim 1 , wherein M is C-Calkyl.25. A compound of claim 1 , wherein M is a pharmaceutically acceptable cation.26. A compound of claim 25 , wherein the pharmaceutically acceptable cation is Na claim 25 , Li claim 25 , K claim ...

ROR GAMMA (RORY) MODULATORS

Novel compounds according to Formula I 2. The compound according to wherein:{'sub': 11', '14', '11', '12', '13', '14', '1', '14, 'A-Aare N or CR, CR, CR, CR, respectively, with the proviso that no more than two of the four positions A in A-Acan be simultaneously N;'}{'sub': 6', '7', '9', '10', '6', '7', '9', '10', '6', '7', '9', '10, 'A, A, A, Aare N or CR, CR, CR, CR, respectively, with the proviso that at least one but no more than two of the four positions A in A, A, A, Ais N;'}{'sub': 8', '8, 'Ais CR;'}{'sub': '1', 'Ris C(3-6)cycloalkylC(1-3)alkyl or (di)C(3-6)cycloalkylamino with all carbon atoms of alkyl groups optionally substituted with one or more F and all carbon atoms of cycloalkyl groups optionally substituted with one or more F or methyl;'}{'sub': 2', '3, 'Rand Rare independently H;'}{'sub': '4', 'Ris H;'}{'sub': '5', 'Ris H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl, all groups optionally substituted with one or more F, C(1-2)alkoxy or cyano;'}{'sub': 1', '8, 'the sulfonyl group with Ris represented by R;'}{'sub': 6', '14, 'the remaining R-Rare independently H, halogen, C(1-3)alkoxy or C(1-6)alkyl, all of the alkyl groups optionally being substituted with one or more F or hydroxy; and'}{'sub': '15', 'Ris C(1-6)alkyl or C(3-6)cycloalkyl, all groups optionally substituted with one or more F, C(1-2)alkoxy or cyano;'}{'sub': '16', 'and Ris C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkyl-C(1-3)alkyl, all groups optionally substituted with one or more F, C(1-2)alkyl, C(1-2)alkoxy or cyano.'}3. The compound according to wherein:{'sub': 11', '14', '11', '12', '13', '14, 'A-Aare respectively CR, CR, CR, CR;'}{'sub': 6', '7', '9', '10', '6', '7', '9', '10', '6', '7', '9', '10, 'A, A, A, Aare N or CR, CR, CR, CR, respectively, with the proviso that at least one but no more than two of the four positions A in A, A, A, Ais N;'}{'sub': ...

Cyclohexanone compounds and herbicides comprising the same

The present invention provides a compound having an excellent efficacy for controlling weeds. A cyclohexanone compound of the formula (I): wherein m is an integer of 1, 2 or 3; n is an integer of any one of 1 to 5; X represents CH 2 , O, S, S(O) or S(O) 2 ; R 1 represents a hydrogen atom or a methyl group; R 2 and R 3 represents a hydrogen atom, a C 1-6 alkyl group and the like; R 4 represents a C 6-10 aryl group or a five- to six-membered heteroaryl group; G represents a hydrogen atom and the like; Z represents a halogen atom, a cyano group, a nitro group, a phenyl group, a C 1-6 alkyl group and the like; is useful as an active ingredient for herbicides.

Apoptosis Inhibitors

The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition. 2. The method of wherein:R1 is an optionally substituted, optionally hetero-, optionally cyclic C1-C18 alkyl, or an optionally substituted, optionally hetero-, optionally cyclic C2-C18 alkenyl or alkynyl, or an optionally substituted, optionally hetero-, optionally cyclic C2-C18 aryl.3. The method of wherein:R1 is an optionally substituted C1-C4 alky.4. The method of wherein:R2 is an optionally substituted, optionally hetero-, optionally cyclic C1-C18 alkyl, or an optionally substituted, optionally hetero-, optionally cyclic C2-C18 alkenyl or alkynyl, or an optionally substituted, optionally hetero-, optionally cyclic C2-C18 aryl.5. The method of wherein:R2 is F, CH2F, CHF2, or CF3.6. The method of wherein:R3 is an optionally substituted, heterocyclic C3-C18 hydrocarbyl.7. The method of wherein:R3 is an optionally substituted 5-pyridin-2(1H)-one.8. The method of wherein:R4 is H or an optionally substituted, optionally hetero-, optionally cyclic C1-C18 alkyl, or an optionally substituted, optionally hetero-, optionally cyclic C2-C18 alkenyl or alkynyl, or an optionally substituted, optionally hetero-, optionally cyclic C2-C18 aryl.9. The method of wherein:R4 is H.10. The method of wherein:R1 is an optionally substituted C1-C4 alky;R2 is F, CH2F, CHF2, or CF3;R3 is an optionally substituted 5-pyridin-2(1H)-one; andR4 is H.13. The method wherein:R1 is an optionally substituted, optionally hetero-, optionally cyclic C1-C18 alkyl, or an optionally substituted, optionally hetero-, optionally cyclic C2-C18 alkenyl or alkynyl, or an optionally substituted, ...

METHODS OF TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES AND DISORDERS

The present invention provides compostions and methods useful for treating and preventing neurodenerative disease and neurologically related disorders by inhibition of Lp-PLA2. The compositions and methods are useful for treating and preventing diseases and disorders with abnormal blood brain barrier (BBB) function, for example neurodegenerative diseases with a permeable BBB, such as but not limited to, Alzhiemer's Disease, Huntington's Disease, Parkinson's Disease and Vascular Dementia. 1. (canceled)2. A method for reducing blood brain barrier (BBB) permeability in a subject , comprising administering to the subject a pharmaceutical composition comprising 1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)-aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5 ,6-trimethylenepyrimidin-4-one.3. The method of claim 2 , wherein the subject has been identified with mild cognitive impairment.4. The method of claim 2 , wherein the subject is identified to have Alzheimer's disease or is at risk of developing Alzheimer's disease.5. The method of claim 2 , wherein prior to the administration of the pharmaceutical composition to the subject claim 2 , the subject is selected for treatment with the pharmaceutical composition.6. The method of claim 4 , the subject is selected for treatment with the pharmaceutical composition based on the subject exhibiting at least one symptom of mild cognitive impairment or Alzheimer's disease.7. A method for reducing blood brain barrier (BBB) permeability in a subject with any one of mild cognitive impairment claim 4 , Alzheimer's disease claim 4 , vascular dementia claim 4 , Huntington's Disease or Parkinson's disease claim 4 , comprising administering to the subject a pharmaceutical composition comprising 1-(N-(2-(diethylamino)ethyl)-N-(4-(4-trifluoromethylphenyl)benzyl)-aminocarbonylmethyl)-2-(4-fluorobenzyl)thio-5 claim 4 ,6-trimethylenepyrimidin-4-one.8. A method for reducing blood brain barrier (BBB) permeability in a subject with ...

THIOACETATE COMPOUNDS, COMPOSITIONS AND METHODS OF USE

Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid. 136-. (canceled)39. The method of claim 37 , further comprising administering a xanthine oxidase inhibitor.40. The method of claim 39 , wherein the xanthine oxidase inhibitor is febuxostat.41. The method of claim 39 , wherein the xanthine oxidase inhibitor is allopurinol.42. The method of claim 37 , wherein the human has type 2 diabetes.45. The method of claim 43 , further comprising administering a xanthine oxidase inhibitor.46. The method of claim 45 , wherein the xanthine oxidase inhibitor is febuxostat.47. The method of claim 45 , wherein the xanthine oxidase inhibitor is allopurinol.48. The method of claim 43 , wherein the human has diabetes.49. The method of claim 48 , wherein the human has type 2 diabetes. Uric acid is the result of the oxidation of xanthine. Disorders of uric acid metabolism include, but are not limited to, polycythemia, myeloid metaplasia, gout, a recurrent gout attack, gouty arthritis, hyperuricaemia, hypertension, a cardiovascular disease, coronary heart disease, Lesch-Nyhan syndrome, Kelley-Seegmiller syndrome, kidney disease, kidney stones, kidney failure, joint inflammation, arthritis, urolithiasis, plumbism, hyperparathyroidism, psoriasis or sarcoidosis.In certain embodiments, provided herein are compounds, methods and compositions, e.g., for the modulation of serum uric acid levels (sUA) or the treatment of gout or hyperuricemia in individuals in need thereof. In some embodiments, such compositions comprise and such methods comprise the administration to an individual in need thereof an effective amount of a compound of formula I:In specific instances:Provided in certain embodiments, is a compound of formula (I), wherein one of X, X, Xor Xis N. Certain ...

NOVEL COMPOSITIONS USEFUL FOR INHIBITING HIV-1 INFECTION AND METHODS USING SAME

The present invention includes novel compounds, and compositions comprising same, useful for preventing or treating an HIV-1 infection in a subject in need thereof. The present invention further includes a novel method of preventing or treating an HIV-1 infection in a subject in need thereof, comprising administering to the subject an effective amount of a compound and/or composition of the invention. In certain embodiments, the subject is further administered at least one additional therapeutic agent. 6. The compound of claim 1 , wherein the compound is selected from the group consisting of:2-(thieno[2,3-d]pyrimidin-4-ylthio)-1-(4-(thiophene-2-carbonyl)piperazin-1-yl)ethan-1-one (DC04);1-(4-(furan-2-carbonyl)piperazin-1-yl)-2-(naphthalen-1-yl)ethan-1-one (DC08);1-(4-benzoylpiperazin-1-yl)-2-((4,6-dimethylpyrimidin-2-yl)thio)ethan-1-one (DC10);1-(4-benzoylpiperazin-1-yl)-2-(naphthalen-1-yloxy)ethan-1-one (DC18);(5-benzoylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(1,2-dihydroacenaphthylen-5-yl)methanone (SC04);4-benzoyl-1-(1,2-dihydroacenaphthylene-5-carbonyl)-2-methylpiperazine (SC06);1-(5-benzoylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-2-(7-chloro-4-methoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (SC07);1-(5-benzoylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (SC08);1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-(4-phenyl hexahydrocyclopenta[c]pyrrol-2(1H)-yl)ethane-1,2-dione (SC10);1-(4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-(1-phenyl-3a,4,6,6a-tetrahydropyrrolo[3,4-c]pyrazol-5 (1H)-yl)ethane-1,2-dione (SC12);N-((1-benzoylazetidin-3-yl)methyl)-2-(4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoacetamide (SC14);1-(4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-(3-(3-oxo-3-phenylpropyl)azetidin-1-yl)ethane-1,2-dione (SC15);S-((1-(2-(4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3 ...

INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE

The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NADbiosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. 1. (canceled)3. (canceled)4. The compound of claim 2 ,wherein:{'sup': a', 'b', 'x', 'x, 'sub': 2', '2', '2, 'one of Rand Ris hydrogen and the other is COR, CHCOR, tetrazole, or oxadiazolone;'}{'sup': c', 'x, 'sub': 1', '6, 'Ris halogen, —CN, —OR, or C-Calkyl;'}{'sup': 'd', 'Ris methyl, optionally substituted 5- to 10-membered aryl, optionally substituted 5- or 6-membered heteroaryl, or optionally substituted 5- or 6-membered carbocycle; and'}{'sup': 'x', 'sub': 1', '6, 'Ris hydrogen or C-Calkyl;'}{'sup': e', 'y', 'z, 'sub': 1', '6', '2', '6', '2', '6', '1', '6, 'each Ris independently C-Calkyl, C-Calkenyl, C-Calkynyl, halogen, —OR, C-Chaloalkyl, —NHR, —OH, or —CN;'}{'sup': y', 'z, 'sub': 1', '6', '1', '6, 'each Rand Ris independently hydrogen, C-Calkyl, or C-Chaloalkyl;'}{'sup': c', 'd', 'c', 'd, 'with the proviso that Ris not hydrogen or —CN when Ris optionally substituted phenyl and that Ris not —CN when Ris 2-furyl.'}56-. (canceled)7. The compound of claim 2 , wherein Ris —CN or halogen.8. The compound of claim 2 , wherein Ris methyl claim 2 , cyclohexyl claim 2 , pyridinyl claim 2 , thiazolyl claim 2 , phenyl claim 2 , or thienyl.9. The compound of claim 2 , wherein Ris methyl claim 2 , cyclohexyl claim 2 , pyridinyl claim 2 , thiazolyl claim 2 , thienyl claim 2 , or optionally substituted phenyl.10. The compound of claim 2 , wherein Ris hydrogen claim 2 , CHCOH claim 2 , tetrazole claim 2 , or oxadiazolone (1 claim 2 ...

SecA INHIBITORS AND METHODS OF MAKING AND USING THEREOF

Inhibitors of SecA, and methods of making and using thereof, are described herein. The compounds described herein can be used to treat or prevent microbial infections, such as bacterial infections. 211-. (canceled)12. The compound of claim 1 , wherein the compound is a compound of Formula VI claim 1 , wherein R-Rare independently absent or selected from the group consisting of hydrogen; halogen; hydroxyl; ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n- claim 1 , sec- claim 1 , iso- claim 1 , or t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , heptyl; substituted or unsubstituted cyclopentanyl; substituted or unsubstituted alkoxy; substituted or unsubstituted alkenyl claim 1 , cycloalkenyl claim 1 , heterocycloalkyl claim 1 , and heteroaryl; wherein R-Rare optionally substituted with one or more substituents independently selected from the group consisting of hydrogen; halogen; hydroxyl; ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 , n- claim 1 , sec- claim 1 , iso- claim 1 , or t-butyl claim 1 , pentyl claim 1 , hexyl claim 1 , or heptyl; substituted or unsubstituted cyclopentanyl; substituted or unsubstituted alkoxy; substituted or unsubstituted alkenyl claim 1 , cycloalkenyl claim 1 , heterocycloalkyl claim 1 , heteroaryl; or R-Rtaken together is O claim 1 , S claim 1 , SO claim 1 , SO claim 1 , NR claim 1 , or CRR;{'sub': 3', '13', '2', '2', '2, 'sup': 14', '14', '14', '14', '14', '14', '14', '14', '14', '14', '14', '14', '14', '14', '14, 'wherein R-Rare independently absent or selected from the group consisting of hydrogen; halogen; hydroxyl; substituted or unsubstituted alkoxy; substituted or unsubstituted alkyl; of —OR; cycloalkyl; cycloalkenyl; primary amine; secondary amine; tertiary amine; —C(O)R, —C(O)OR, —C(O)NRR, —NRR, —NRS(O)R, —NRC(O)R, —S(O)R, —SR, and —S(O)NRR; and'}{'sub': '14', 'sup': '14', 'Ris independently selected from the group consisting of hydrogen, halogen, cyano, —OR, alkyl, alkenyl, cycloalkyl, cycloalkenyl, aryl, ...

Apoptosis Inhibitors

The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition. 2. The method wherein:R1 is substituted or unsubstituted C1-C18 alkyl or substituted or unsubstituted C1-C18 heteroalkyl.3. The method of wherein:R1 is substituted or unsubstituted C1-C4 alkyl.4. The method of wherein:R1 is Me.5. The method of wherein:{'sub': 3', '2', '2', '3, 'R2 is CH, F, CHF, CHF, or CF.'}6. The method of wherein:R3 is N-substituted with substituted or unsubstituted benzyl.7. The method of wherein:R3 is N-substituted with 3,4-disubstituted benzyl.8. The method of wherein:R3 is 3-substituted with F.9. The method of wherein:R3 is 3-substituted with F, and N-substituted with substituted or unsubstituted benzyl.10. The method of wherein:R4 is H.11. The method wherein:R1 is substituted or unsubstituted C1-C18 alkyl or substituted or unsubstituted C1-C18 heteroalkyl;{'sub': 3', '2', '2', '3, 'R2 is CH, F, CHF, CHF, or CF;'}R3 is N-substituted with substituted or unsubstituted benzyl, andR4 is H.12. The method of wherein:R1 is substituted or unsubstituted C1-C4 alkyl;{'sub': 3', '2', '2', '3, 'R2 is CH, F, CHF, CHF, or CF,'}R3 is N-substituted with substituted or unsubstituted benzyl, andR4 is H.13. The method of wherein:R1 is Me;{'sub': 3', '2', '2', '3, 'R2 is CH, F, CHF, CHF, or CF,'}R3 is N-substituted with substituted or unsubstituted benzyl, andR4 is H.14. The method of wherein:{'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'wherein substituents for alkyl and heteroalkyl radicals, as well as those groups referred to as alkylene, alkenyl, heteroalkylene, heteroalkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl and ...

HERBICIDE COMPOSITION

There is provided a herbicidal composition containing a cyclohexanone compound represented by Formula (I) and at least one compound selected from Group A. 3. The herbicidal composition according to claim 2 ,{'sup': 2', '3', '2', '3', '2', '3, "wherein Rand Reach independently are hydrogen, a methyl group, an ethyl group, or Rand Rare bonded to form an ethylene chain, and two R's may be the same or different, and two R's may be the same or different,"}{'sup': '4', 'Ris a phenyl group, a 2-pyridyl group, a 3-pyridyl group, a 4-pyridyl group, a 2-pyrimidinyl group, a 2-pyrazinyl group, a 3-pyridazinyl group, a 3-furyl group, a 2-thienyl group, a 2-thiazolyl group, a 1,2,3-triazolyl group, or a 1-pyrazolyl group,'}wherein the phenyl group, the 2-pyridyl group, the 3-pyridyl group, the 4-pyridyl group, the 2-pyrimidinyl group, the 2-pyrazinyl group, the 3-pyridazinyl group, the 3-furyl group, the 2-thienyl group, and 2-thiazolyl group have one or more substituents selected from the group consisting of chlorine, bromine, iodine, fluorine, a methyl group, an ethyl group, an isopropyl group, a t-butyl group, a methoxy group, a nitro group, an amino group, a cyano group, a hydroxyl group, an acetyl group, a methoxycarbonyl group, a pentafluorothio group, a pentafluoroethyl group, a difluoroethyl group, a heptafluoroisopropyl group, a trifluoromethylthio group, a benzoylamino group, a trifluoromethoxy group, and a trifluoromethyl group, andwherein the 1,2,3-triazolyl group and 1-pyrazolyl group optionally have one or more substituents selected from the group consisting of a methyl group and a phenyl group, andwherein the phenyl group optionally has one or more substituents selected from the group consisting of chlorine, bromine, iodine, fluorine, and a trifluoromethyl group,G is hydrogen, an acetyl group, a propionyl group, a butylcarbonyl group, a benzoyl group, a methylsulfonyl group, a methoxycarbonyl group, an ethoxycarbonyl group, an allyloxycarbonyl group, a ...

Compounds and methods for treating candidiasis and aspergillus infections

The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for killing or inhibiting the growth of a Candida or Aspergillus species or preventing or treating a mammal having candidiasis (oral and/or disseminated) or an Aspergillus infection.

SULFONYLUREAS AND SULFONYLTHIOUREAS AS NLRP3 INHIBITORS

The present invention relates to compounds of formula (I): 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein Ris a 6-membered heteroaryl group containing at least two nitrogen atoms in the 6-membered ring structure claim 1 , wherein Rmay optionally be substituted claim 1 , and wherein optionally:(i) at least one of the two nitrogen atoms is located at the 3, 4 or 5-position of the 6-membered ring structure; or(ii) a first nitrogen atom is located at the 2-position and a second nitrogen atom is located at the 6-position of the 6-membered ring structure, and wherein the 6-membered heteroaryl group is substituted with one or more monovalent groups at the 3- and/or 5-positions of the 6-membered ring structure.34-. (canceled)5. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein the 6-membered heteroaryl group of Ris substituted with at least one monovalent group X claim 1 , wherein X is at each occurrence any group that can mesomerically donate a lone pair of electrons from a nitrogen claim 1 , oxygen or sulphur atom onto at least one nitrogen atom in the 6-membered ring structure claim 1 , and wherein the 6-membered heteroaryl group may optionally be further substituted.6. The compound or a pharmaceutically acceptable salt claim 1 , solvate or prodrug thereof claim 1 , as claimed in claim 1 , wherein:{'sup': '1', 'the 6-membered heteroaryl group of Ris substituted with at least one monovalent group X′ at a position ortho- or para- to at least one nitrogen atom in the 6-membered ring structure;'}{'sup': '1', 'the 6-membered heteroaryl group of Rmay optionally be further substituted;'}{'sup': '1', 'Xis at each occurrence independently selected from a'}{'sup': 3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3', '3, 'sub': 2', '2', '2', '2, '—OR, —SR, —N(R), —O-L-OR, —O-L-SR, —O-L-N(R), —S-L-OR, —S ...

CARBOCYCLIC SULFONE ROR GAMMA MODULATORS

Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders. 2. A compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein B is a phenyl ring.3. The compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein:{'sup': '1′', 'sub': 3', '1-6, 'R is halo, CF, or Calkyl; and'}{'sup': 1', '1a', '1b', '1a, 'sub': 2', '3', '1-6', '2', 'r', '2', 'r, 'Ris hydrogen, NH, CF, halo, Calkyl substituted with 0-3 R, —(CH)OR, or (CH)-phenyl substituted with 0-3 R.'}4. The compound according to claim 1 , or a stereoisomer or pharmaceutically-acceptable salt thereof claim 1 , wherein{'sup': 3', '3b', '3a', '3a, 'sub': 3', '2', '1-6', '1-6', '2', '1-6', '3-10, 'Ris hydrogen, halo, N, CN, OR, —NH, NH(Calkyl), N(Calkyl), Calkyl substituted with 0-3 Ror Ccycloalkyl substituted with 0-3 R;'}{'sup': 3a', 'b', 'b', 'b', 'b', '11', '11', '11', '11', 'b', 'c', 'b', 'c', 'b', '11', '11', '11', '11', 'b', 'c', 'a', 'a', 'a', 'a', 'a', 'a, 'sub': 3', '2', '3', '2', '2', '2', 'r', '2', 'r', 'p', '2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', '2', 'r', 'p', 'p', '1-6', '2-6', '2-6', '1-6', '2', 'r', '2', 'r', '2', 'r', 'p, 'Ris, independently at each occurrence, hydrogen, ═O, halo, OCF, OCHF, CF, CHF, CN, NO, —(CH)OR, —(CH)S(O)Rb, —(CH)C(O)R, —(CH)C(O)OR, —(CH)OC(O)R, —(CH)NRR, —(CH)C(O)NRR, —(CH)NRC(O)R, —(CH)NRC(O)OR, —NRC(O)NRR, —S(O)NRR, —NRS(O)RCalkyl substituted with 0-3 R, Calkenyl ...

NOVEL SYNTHETIC ANTIOXIDANTS AND THEIR USES

The present invention relates to synthetic organic antioxidants of small molecules. The novel dithiol-containing compounds in this invention possess strongest possible capability as both scavenger for free radicals and antioxidant. This invention is directed to novel molecules as prodrugs of the novel dithiol-containing compounds, their rational design, their feasible preparation route by means of synthetic organic chemistry, and their potential uses in application to treatment and/or prevention of major diseases associated with oxidative stress, such as Alzheimer's disease, Parkinson's disease, cancer, diabetes, HIV, acne, cardiovascular disease, renal disease, hypertension, hypercholesterolemia, hyperlipidemia, rheumatoid arthritis, inflammation, pain, aging, stroke, cataract, glaucoma, age-related macular degeneration, etc. 1. A compound comprising at least one pair of functional groups that consist of one functional group as thiol (—SH) groups and another one as either carbodithioic acid (—CSSH) or carbothioic acid (—COSH) , which when oxidized can form an intramolecular 5 or 6-membered ring via a disulfide bond , wherein said one pair functional groups are each optionally protected by an independently selected protecting group that is removable under physiological conditions for the purpose of drug delivery.2. (canceled)3. The compound of claim 1 , wherein each of the pair of functional groups is covalently single-bonded with a carbon atom located on an aromatic ring that is selected from the group consisting of benzene claim 1 , diphenylene claim 1 , naphthalene claim 1 , phenanthrene claim 1 , anthracene claim 1 , aromatic heterocyclic rings and combinations thereof.4. (canceled)5. The compound of claim 1 , wherein each of the pair of functional groups is optionally protected by forming a covalent bond with another functional group or molecular moiety independently selected from the group consisting of acetyl (—Ac) claim 1 , succinic acid claim 1 , amino acid ...

THIOETHER COMPOUNDS AS NITRIFICATION INHIBITORS

Provided herein are a use of thioether compounds of formula I as nitrification inhibitors, and agricultural mixtures and compositions including the thioether compounds. 2. The thioether compound of claim 1 , wherein in the compound of formula I{'sup': 1', '2, 'Rand Rare H; and'}p is 1 or 2.6. A composition for use in reducing nitrification comprising at least one compound of formula I as defined in and at least one carrier.7. An agrochemical mixture comprising (i) at least one fertilizer; and (ii) at least one compound of formula I as defined in .8. (canceled)9. (canceled)10. A method for reducing nitrification claim 1 , the method comprising treating a plant growing on at least one of soil claim 1 , soil substituents claim 1 , and a locus claim 1 , soil claim 1 , and soil substituents where the plant is growing or is intended to grow with at least one compound of formula I as defined in .11. The method of claim 10 , further comprising providing the at least one of the plant and the locus claim 10 , soil claim 10 , and soil substituents where the plant is growing or is intended to grow with a fertilizer.12. The method of claim 11 , wherein the treating with the compound of formula I and the providing of the fertilizer are carried out simultaneously.13. A method for treating at least one of a fertilizer and a fertilizer composition claim 1 , comprising applying a nitrification inhibitor as defined in to the at least one of the fertilizer and the fertilizer composition.14. The agrochemical mixture of claim 7 , wherein the fertilizer is selected from the group consisting of a solid ammonium-containing inorganic fertilizer claim 7 , a liquid ammonium-containing inorganic fertilizer claim 7 , a solid organic fertilizer claim 7 , a liquid organic fertilizer claim 7 , and a urea-containing fertilizer.15. The method of claim 10 , wherein the plant is an agricultural plant claim 10 , a vegetable claim 10 , sorghum; a silvicultural plant; an ornamental plant; and a ...

METHOD FOR TREATING MACROPHAGE MIGRATION INHIBITORY FACTOR (MIF)-IMPLICATED DISEASES AND CONDITIONS WITH IODO PYRIMIDINE DERIVATIVES

Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula I: 2. The method of claim 1 , wherein the MIF-implicated disease is selected from the group consisting of inflammatory disease and cancer.3. The method of claim 2 , wherein the inflammatory disease is selected from the group consisting of dermatitis claim 2 , arthritis claim 2 , rheumatoid arthritis claim 2 , insulin-dependent diabetes claim 2 , proliferative vascular disease claim 2 , acute respiratory distress syndrome claim 2 , sepsis claim 2 , septic shock claim 2 , psoriasis claim 2 , asthma claim 2 , cytokine related toxicity claim 2 , lupus claim 2 , multiple sclerosis claim 2 , transplant-host response claim 2 , and autoimmune disorders.4. The method of claim 1 , wherein the MIF-implicated condition is caused by a MIF-producing pathogen.5. The method of claim 4 , wherein the MIF-producing pathogen is selected from the group consisting of parasitic helminths claim 4 , spirochetes claim 4 , and plasmodium.6. The method of claim 1 , wherein the MIF inhibitory compound is selected from the group consisting of:4-Iodo-6-(2,3-difluoro-4-methoxyphenyl)pyrimidine;4-Iodo-6-(2-fluoro-4-methoxyphenyl)pyrimidine;4-Iodo-6-(2-fluorophenyl)pyrimidine;4-Iodo-6-(4-fluorophenyl)pyrimidine;4-Iodo-6-(furan-3-yl)pyrimidine;4-Iodo-6-(pyridin-3-yl)pyrimidine;4-Iodo-6-(3-fluorophenyl)pyrimidine;4-Iodo-6-(4-tert-butyloxymethylphenyl)pyrimidine;4-Iodo-6-(2-fluoropyridin-3-yl)pyrimidine;4-Iodo-6-(furan-2-yl)pyrimidine;4-Iodo-6-(4-fluoropyrimidin-3-yl)pyrimidine;4-Iodo-6-(3-fluoro-4-methoxyphenyl)pyrimidine;4-Iodo-6-(2-chloropyridin-5-yl)pyrimidine;4-Iodo-6-(2-hydroxyphenyl)pyrimidine;4-Iodo-6-(2,4-difluorophenyl)pyrimidine;4-Iodo-6-(2-fluoro-6-methoxyphenyl)pyrimidine;4-Iodo-6-(2-chlorophenyl)pyrimidine;4-Iodo-6-(3-acetylaminophenyl)pyrimidine;4-Iodo-6-(thiophen-3-yl)pyrimidine;4-Iodo-6-(3-hydroxymethylphenyl)pyrimidine;4-Iodo-6-(isoquinolin-4-yl)pyrimidine;4-Iodo ...

INHIBITORS OF ALPHA-AMINO-BETA-CARBOXYMUCONIC ACID SEMIALDEHYDE DECARBOXYLASE

The present disclosure discloses compounds capable of modulating the activity of α-amino-β-carboxymuconic acid semialdehyde decarboxylase (ACMSD), which are useful for the prevention and/or the treatment of diseases and disorders associated with defects in NAD biosynthesis, e.g., metabolic disorders, neurodegenerative diseases, chronic inflammatory diseases, kidney diseases, and diseases associated with ageing. The present application also discloses pharmaceutical compositions comprising said compounds and the use of such compounds as a medicament. 117-. (canceled)1920-. (canceled)2223-. (canceled)25. The method of claim 24 , wherein said disorder associated with mitochondrial dysfunction is an inherited mitochondrial disease claim 24 , a metabolic disorder claim 24 , a neurodegenerative disease claim 24 , a chronic inflammatory disease claim 24 , a fatty liver disease claim 24 , a kidney disease claim 24 , or an aging related disorder.26. (canceled)2840-. (canceled)4244-. (canceled)45. The method of claim 18 , wherein said disease or disorder associated with α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) dysfunction is a metabolic disorder claim 18 , a neurodegenerative disease claim 18 , a chronic inflammatory disease claim 18 , a fatty liver disease claim 18 , a kidney disorder claim 18 , or an aging related disorder.46. The method of claim 21 , wherein said disease or disorder associated with reduced nicotinamide adenine dinucleotide (NAD) levels is a metabolic disorder claim 21 , a neurodegenerative disease claim 21 , a chronic inflammatory disease claim 21 , a fatty liver disease claim 21 , a kidney disorder claim 21 , or an aging related disorder.47. The method of claim 27 , wherein promoting oxidative metabolism is associated with treating claim 27 , preventing claim 27 , or reducing the risk of a disease or disorder selected from the group consisting of a metabolic disorder claim 27 , a neurodegenerative disease claim 27 , a chronic ...

5-(trifluoromethyl)pyrimidine derivatives and method for producing same

Provided are 5-(trifluoromethyl)pyrimidine derivatives useful as intermediates for pharmaceuticals and agrochemicals and as intermediates for electronic materials and methods for producing the same. 2,4-dichloro-5-(trifluoromethyl)pyrimidine is reacted with 2,2,2-trifluoroethanol, benzyl alcohol, or benzenethiol to obtain the intended 2-(2,2,2-trifluoroethoxy)-4-chloro-5-(trifluoromethyl)pyrimidine, 2-benzyloxy-4-chloro-5-(trifluoromethyl)pyrimidine, 2,4-bis(2,2,2-trifluoroethoxy)-5-(trifluoromethyl)pyrimidine, or 2-chloro-4-phenylthio-5-(trifluoromethyl)pyrimidine.

PHOTOCATALYST-FREE, LIGHT-INDUCED CARBON-SULFUR CROSS-COUPLING METHODS

In one aspect, the invention provides a method of promoting a carbon-sulfur bond forming reaction. In certain embodiments, the reaction comprises cross-coupling of a(n) (hetero)aryl halide with a thiol to form the carbon-sulfur bond, wherein the method is promoted by light irradiation in the absence of a photocatalyst. In other embodiments, the cross-coupling reaction can be promoted through visible light irradiation, including sunlight. 1. A method of generating a(n) (hetero)aryl thioether , the method comprising irradiating a system comprising a(n) (hetero)aryl halide , a thiol , and at least one base with at least one light wavelength , whereby a carbon-sulfur bond is formed between the (hetero)aryl halide and the thiol , wherein the system is essentially free of at least one catalyst selected from the group consisting of a transition metal and an organic photocatalyst.2. The method of claim 1 , wherein the system is essentially free of a transition metal and an organic photocatalyst.3. The method of claim 1 , wherein the system is free of the at least one catalyst.4. The method of claim 1 , wherein the system is free of a transition metal and an organic photocatalyst5. The method of claim 1 , wherein claim 1 , if the at least one catalyst is present in the system claim 1 , the at least one catalyst is present at levels that do not promote significant carbon-sulfur bond formation between the (hetero)aryl halide and the thiol.6. The method of claim 1 , wherein the at least one base is selected from the group consisting of an amine claim 1 , a phosphine claim 1 , a carbonate salt claim 1 , a hydroxide salt claim 1 , an alkoxide salt claim 1 , a phosphate salt claim 1 , a metal hydride and a carboxylate salt.7. The method of claim 6 , wherein the at least one base is selected from the group consisting of NaCO claim 6 , KCO claim 6 , RbCOand CsCO.8. The method of claim 1 , wherein the (hetero)aryl halide and the thiol are irradiated with a radiation selected from the ...

NONAQUEOUS ELECTROLYTE, NONAQUEOUS ELECTROLYTE ENERGY STORAGE DEVICE, AND METHOD FOR PRODUCING NONAQUEOUS ELECTROLYTE ENERGY STORAGE DEVICE

Provided are a nonaqueous electrolyte capable of providing a nonaqueous electrolyte energy storage device with reduced direct current resistance and an increased capacity retention ratio after charge-discharge cycles, a nonaqueous electrolyte energy storage device including such a nonaqueous electrolyte, and a method for producing such a nonaqueous electrolyte energy storage device. One mode of the present invention is a nonaqueous electrolyte for an energy storage device, containing an additive represented by the following Formula (1) or Formula (2). In Formula (1), Rto Rare each independently a hydrogen atom or a group represented by —NR¾, —ORa, —SRa, etc., with the proviso that at least one of Rto Ris a group represented by —ORa, —SRa, —COORa, —CORa, —SO2Ra, or —SO3Ra. In Formula (2), Rto Rare each independently a hydrogen atom or a group represented by —NRb, —OR, or —SR, with the proviso that at least one of Rto Ris a group represented by —SRb. 2. The nonaqueous electrolyte according to claim 1 , whereinthe additive is represented by Formula (1), and{'sup': 1', '4', 'a', 'a', 'a', 'a', 'a', 'a, 'sub': 2', '3, 'the Rto Rare each independently a hydrogen atom or a group represented by —OR, —SR, —COOR, —COR, —SOR, or —SOR.'}3. The nonaqueous electrolyte according to claim 1 , whereinthe additive is represented by Formula (1), and{'sup': 1', '4', 'a', 'a', 'a, 'sub': 2', '3, 'at least one of the Rto Ris a group represented by —SR, —SOR, or —SOR.'}4. The nonaqueous electrolyte according to claim 1 , whereinthe additive is represented by Formula (2), and{'sup': 5', '7', 'b', 'b, 'the Rto Rare each independently a group represented by —ORor —SR.'}5. A nonaqueous electrolyte energy storage device claim 1 , comprising the nonaqueous electrolyte according to .6. A method for producing a nonaqueous electrolyte energy storage device claim 1 , using the nonaqueous electrolyte according to . The present invention relates to a nonaqueous electrolyte, a nonaqueous electrolyte ...

HETEROCYCLES CAPABLE OF MODULATING T-CELL RESPONSES, AND METHODS OF USING SAME

The present disclosure is directed in part to heterocycles, and their use in treating medical disorders, such as immune inflammatory disorders such as Crohn's disease, ulcerative colitis, rheumatic disorders, psoriasis, and allergies. The compounds are contemplated to modulate T-Cell responses. 139-. (canceled)48. A method of treating an immune inflammatory disease or disorder in a subject in need thereof claim 40 , the method comprising administering to the subject a pharmaceutically effective amount of the heterocyclic compound of claim 40 , wherein the immune inflammatory disease or disorder is selected from the group consisting of Crohn's disease claim 40 , ulcerative colitis claim 40 , a rheumatic disorder claim 40 , psoriasis claim 40 , and an allergy.49. The method of claim 48 , wherein the allergy is contact dermatitis.50. The method of claim 48 , wherein the allergy is atopic dermatitis.51. A method of treating an immune inflammatory disease or disorder in a subject in need thereof claim 44 , the method comprising administering to the subject a pharmaceutically effective amount of the pharmaceutical composition of claim 44 , wherein the immune inflammatory disease or disorder is selected from the group consisting of Crohn's disease claim 44 , ulcerative colitis claim 44 , a rheumatic disorder claim 44 , psoriasis claim 44 , and an allergy.52. The method of claim 51 , wherein the allergy is contact dermatitis.53. The method of claim 51 , wherein the allergy is atopic dermatitis. This application is a continuation patent application of U.S. patent application Ser. No. 14/404,839, filed on Dec. 1, 2014, which application is a U.S. national stage application of International Application No. PCT/EP2013/061330, filed on May 31, 2013, which application claims priority to and the benefit of U.S. Provisional Patent Application No. 61/654,385, filed on Jun. 1, 2012; the contents of each of which are incorporated by reference herein in their entirety.T lymphocytes (i. ...

Propanamine derivatives for treating pain and pain related conditions

The present invention relates to new compounds of formula (I) that show great affinity and activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels or dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments.

Novel herbicides

Bicyclic dione compounds, and derivatives thereof, which are suitable for use as herbicides. formula (I)

Retinoids for the treatment of emphysema

The current invention provides novel retinoid compounds and methods for their synthesis, the use of such compounds for the preparation of medicaments for treating or preventing emphysema, cancer and dermatological disorders, methods for such deseases and pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders.

Substituted n-phenyl-phenoxy nicotinic acid-(thio)amides and their use as herbicides

The present invention relates to a substituted anilide derivative represented by general formula (I): (wherein R 1 is a hydrogen atom, a (C 1 -C 6 )alkyl group, a halo(C 1 -C 6 )alkyl group or the like; R 2 is a hydrogen atom, a halogen atom or a halo(C 1 -C 6 )alkyl group; R 3 is a hydrogen atom, a halogen atom, a (C 1 -C 6 )alkyl group or the like; t is 0 or 1; m is an integer of 0 to 6; each of Xs is a (C 2 -C 8 )alkyl group, a (C 1 -C 8 )alkoxy group or the like in the case of t being 0, and is a halogen atom, a cyano group or the like in the case of t being 1; n is an integer of 1 to 4; Z is O or S; and Q is any of Q1 to Q25), an intermediate thereof, an agricultural and horticultural chemical, and a usage of the same.

PYRI (MI) DYL-OXY AND THIO-BENZOESIC ACID DERIVATIVES

BUMETHANIDE DERIVATIVES FOR THE TREATMENT OF HYPERHYDROSIS

Настоящее изобретение относится к производным буметанида формулы (I), а также к фармацевтическим композициям, содержащим эти соединения, для применения для лечения или предупреждения заболеваний/нарушений, в которых участвуют сопереносчики Na+-K+-2Cl- (NKCC), и особенно для применения для лечения или предупреждения гипергидроза. The present invention relates to bumetanide derivatives of formula (I) as well as pharmaceutical compositions containing these compounds for use in the treatment or prevention of diseases / disorders in which Na + -K + -2Cl- (NKCC) co-carriers are involved, and especially for use for treatment or prevention of hyperhidrosis.

Substituted pyrimidine compounds and their use

The invention relates to pyrimidine compounds with the formula wherein the meanings of the substituents are shown in the description. The compounds have affinity to the dopamine D3-receptors and can be applied for the treatment of diseases which react to dopamine D3-receptor antagonists, or agonists, respectively. 20 claims

Замещенные циклопентилазины в качестве casr-активных соединений

1. Соединение общей формулы I:[I]гдеAr представляет собой Cарил, Cгетероарил или Cгетероциклоалкиларил, где указанный Cарил, Cгетероарил или Cгетероциклоалкиларил необязательно замещен одним или более одинаковыми или различными заместителями, независимо выбранными из галогена, гидрокси, Cалкила, трифторметила или Cалкокси;X представляет собой -CH- или атом азота;Rпредставляет собой Cалкил, Cалкенил, Cалкинил, гидроксиСалкил, галогенСалкил или Cциклоалкил;Rпредставляет собой водород или выбран из группы, состоящей из аминоСалкила, Cалкила, Cалкенила, гидроксиСалкила, CалкиламиноСалкила, гидроксиСалкиламиноСалкила, CалкилсульфониламиноСалкила, Cалкилкарбонила, Cалкиламинокарбонила, CалкилсульфонилСгетероциклоалкила, аминосульфонилСалкила, Cгегетероциклоалкила, Cгетероциклоалкилкарбонила, где указанный Cалкил, Cалкенил, гидроксиСалкил, CалкиламиноСалкил, гидроксиСалкиламиноСалкил, Cалкилкарбонил, Cалкиламинокарбонил, Cгетероциклоалкил или Cгетероциклоалкилкарбонил необязательно дополнительно замещен одним или более заместителями, выбранными из галогена, гидрокси, трифторметила, -S(O)NH, -S(O)CHили -NH;Rпредставляет собой водород или выбран из группы, состоящей из Cалкила, Cалкенила, Cалкокси, аминоСалкила, Cциклоалкила или Cгетероциклоалкила;или Rи Rвместе с соседним атомом, к которому они присоединены, образуют 4-, 5-, 6- или 7-членный Cгетероциклоалкил, содержащий один или более гетероатомов, выбранных из группы, состоящей из O, S и N, причем указанный Cгетероциклоалкил необязательно замещен оксо, гидрокси, атомом галогена, трифторметилом, Cалкилом, -NH, -S(O)NH, -S(O)CH, Cалкилкарбонилом, гидроксиСалкилом, Cалкокси, аминоСалкилом, Cалкил� РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 213/61 (13) 2013 128 950 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2013128950/04, 21.11.2011 (71) Заявитель(и): ЛЕО ФАРМА А/С (DK) Приоритет(ы): (30) Конвенционный приоритет: 26.11.2010 US 61/417,369 (85) Дата начала ...

ARYLANILINE AGONISTS OF β2-ADRENERGIC RECEPTORS, THEIR USING, PHARMACEUTICAL COMPOSITION BASED ON THEREOF AND METHOD FOR MODULATION OF β2-ADRENERGIC RECEPTORS

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel compounds of the formula (I): their pharmaceutically acceptable salts or solvates, or stereoisomers possessing properties of agonists of β 2 -adrenoreceptors, to pharmaceutical composition based on thereof, using the claimed compounds in manufacturing a medicinal agent, and to a method for modulation of β 2 -adrenergic receptors. In the formula (I) each among R 1 -R 5 is chosen independently from group comprising hydrogen atom, (C 1 -C 4 )-alkyl and R a wherein alkyl is substituted optionally with substituted chosen from R b ; or R 4 and R 5 are combined to form group of the formula: -NR d C(=O)C(R d )=C(R d )-; R 6 , R 7 and R 8 represent hydrogen atom; R 9 represents (C 1 -C 4 )-alkyl; R 10 represents hydrogen atom or (C 1 -C 4 )-alkyl; each among R 11 , R 12 and R 13 is chosen independently from group including hydrogen atom, (C 1 -C 4 )-alkyl, vinyl, cyclohexyl, phenyl, halogen atom, -CO 2 R d , -OR d , -S(O) m R d , -N(NR d R e )R d or -S(O) 2 NR d R e , 5-6-membered monocyclic heteroaryl comprising 1 or 2 heteroatoms chosen from nitrogen (N), sulfur (S) atoms, 9-membered bicyclic heteroaryl comprising N as a heteroatom and 5-membered heterocycle comprising N as a heteroatom; or R 11 and R 12 in common with atoms to which they are bound form 6- or 7-membered heterocyclic ring comprising oxygen (O) atom as a heteroatom and wherein for R 11 -R 13 each phenyl or heteroaryl is substituted optionally with 1 or 2 substitutes chosen independently from R c , and each heterocyclyl is substituted optionally with 1 or 2 substitutes chosen from R b and R c ; alkyl is substituted optionally with substitute chosen from R b , and vinyl is substituted optionally with substitute chosen from R m ; w = 0, 1, 2, 3 or 4. Values R a , R b , R c , R d , R m and m are given in the invention claim. EFFECT: improved method for modulation, valuable medicinal properties of compounds and pharmaceutical composition. ...

Method for obtaining e-isomers of acrylic acid derivatives

Compounds of formula: <CHEM> and stereoisomers thereof, wherein the substituents have the meaning given in claim 1; and metal complexes thereof. The compounds are useful mainly as fungicides but also as plant growth regulators and insecticides/nematocides.

一类sirt2蛋白抑制剂及其在制药中的用途

本发明公开了式Ⅰ所示的化合物或其药学上可接受的盐、晶型、溶剂合物：其中，X选自 等；R 1 选自芳基、杂芳基、取代芳基、取代杂芳基或 R 2 选自 R 3 选自卤素、C 1 ～C 4 烷基或C 1 ～C 4 烷氧基。本发明式Ⅰ所示的新化合物，不仅对SIRT2具有良好的抑制活性，而且对肿瘤具有很好的抑制作用，具有很好的药用潜力，为临床用药提供了一种新的潜在选择。

Замещенное анилидное производное, его промежуточное соединение, химикаты для борьбы с вредителями сельскохозяйственных и плодовых культур и их использование

Изобретение относится к замещенному анилидному производному формулы (I) где R 1 представляет атом водорода, (С 1 -С 6 )алкильную группу; R 2 представляет атом водорода, атом галогена или галоген(С 1 -С 6 )алкильную группу; R 3 представляет атом водорода, атом галогена, (С 1 -С 6 )алкильную группу, гидроксильную группу или (С 1 -С 6 )алкоксигруппу; t равно 1, m равно целому числу 0; каждый из X, которые могут быть одинаковыми или различными, представляет (С 2 -С 8 )алкильную группу, гидрокси(С 1 -С 6 )алкильную группу или (С 3 -С 6 )циклоалкил(С 1 -С 6 )алкильную группу; и n равно 1 или 2; Z представляет атом кислорода; и Q означает заместитель, представленный любой из формул: Q1-Q3, Q6, Q8-Q12, Q14-Q19, Q21 и Q23 (где каждый из Y 1 , которые могут быть одинаковыми или различными, представляет атом галогена, (С 1 -С 6 )алкильную группу, и т.д.); Y 2 представляет (С 1 -С 6 )алкильную группу или галоген(С 1 -С 6 )алкильную группу; Y 3 представляет (С 1 -С 6 )алкильную группу, галоген(С 1 -С 6 )алкильную группу или замещенную фенильную группу; р представляет целое число от 1 до 2, q представляет целое число от 0 или 2, а r представляет целое число от 0 до 2. Предложен химикат для борьбы с вредителями сельскохозяйственных и плодовых культур. Химикат включает замещенное анилидное производное формулы (I) в качестве активного ингредиента и представляет собой инсектицид, фунгицид или акарицид. Предложен способ внесения химиката для борьбы с вредителями сельскохозяйственных и плодовых культур. Также предложено анилиновое производное, представленное общей формулой (II) где R 1 представляет атом водорода, (С 1 -С 6 )алкильную группу; R 2 представляет атом водорода, атом галогена или галоген(С 1 -С 6 )алкильную группу; R 3 представляет атом водорода, атом галогена, (С 1 -С 6 )алкильную группу, гидроксильную группу или (С 1 -С 6 )алкоксигруппу; t равно 1, m равно целому числу 0; каждый из X, которые могут быть одинаковыми или различными, представляет (С 2 -С 8 )алкильную группу, ...

Aryl aniline β2 adrenergic receptor agonists

본 발명은 신규한 β 2 아드레날린 수용체 작용제인 화학식 1의 화합물을 제공한다: 여기에서, R1-R13 및 w는 본 명세서에 기재되어 있는 임의의 값이다. 본 발명은 또한 그러한 화합물을 포함하는 약제학적 조성물, β 2 아드레날린 수용체 활성과 관련이 있는 질병을 치료하기 위해 그러한 화합물을 사용하는 방법, 및 그러한 화합물을 제조하는 방법 및 그러한 제조에 유용한 중간체를 제공한다. The present invention provides compounds of formula 1 which are novel β 2 adrenergic receptor agonists: wherein R 1 -R 13 and w are any of the values described herein. The present invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with β 2 adrenergic receptor activity, methods of making such compounds, and intermediates useful in such preparations. .

药物化合物

本发明提供用于治疗丙型肝炎病毒(HCV)感染的化合物。所述化合物具有所述式(1)：或其盐、N-氧化物、互变异构体或立体异构体，其中A是CH或N；E是CH或N；R 1 选自：任选地取代的非环状C 1-8 烃基团，其中所述非环状C 1-8 烃基团的一个碳原子可任选地被O、S、NRC、S(O)或SO 2 替代，或者所述非环状d-β烃基团的两个相邻的碳原子可任选地被CONR c 、NR c CO、NR c SO 2 或SO 2 NR c 替代，前提是在每种情况下保留所述非环状C 1-8 烃基团的至少一个碳原子；和任选地取代的3至7个环成员的单环碳环或杂环基团，其中0、1、2、3或4个环成员是选自O、N和S的杂原子环成员；R 2 是氢或X-R 8 ；X是C 1-8 烷二基，其中所述C 1-8 烷二基的一个碳原子可任选地与-CH 2 -CH 2 -部分键合以形成环丙烷-1,1-二基或者所述C 1-8 烷二基的两个相邻碳原子可任选地与–(CH 2 ) n 部分键合，其中n是1至5，以形成C 3-7 -环烷-1,2-二基；R 3 是任选地取代的3-至10-元单环或双环碳环或杂环环，其含有选自N、O和S的0至3个杂原子环成员；R 4 是氢或R 43 ，其中R 43 是卤素；氰基；C 1-4 烷基；氟-1.4烷基；C 1-4 烷氧基；氟-C 1-4 烷氧基；羟基-C 1-4 烷基；或C 1-2 烷氧基-C 1-4 烷基；R 5 是氢或R 53 ，其中R 53 选自任选地被氟取代的C 1-2 烷基；任选地被氟；卤素；环丙基；和氰基取代的C 1-3 烷氧基；R 8 是羟基或C(＝O)NR 10 R 11 ；前提是当R8是羟基时，所述羟基和连接X的所述氮原子之间有至少两个碳原子成一直线；R 10 是氢或C 1-4 烷基；或者R 11 是氢；氨基-C 2-4 烷基或羟基-C 2-4 烷基；但不包括所述化合物1-(3-苯甲酰基苯基)-乙基胺和1-(3-呋喃-2-酰基羰基苯基)-乙基胺。

Method of preparing derivatives of 2-amino- or 4-amino-5-alkthiopyrimidines

Pyrimidine derivs. of formula (I), their salts with mineral or organic acids, and mixts. of their isomers, are new: (where R1 is 1-5C alkyl; X1, X2 or X3 is Cl or Br, and the other 2 are NR2R3 and NR4R5; R2-5 are each H, 1-5C alkyl, cycloalkyl, opt. substd aryl or -CO-R (where R is H or 1-5C alky), or NR2R3 and/or NR4R5 is/are heterocyclic other than opt. substd. piperazino, at least one of NR2R3 and NR4R5 being NH2 or -NH-CO-R). (I) are herbicides with pre- and post-emergence activity against mono- and dicotyledon weeds at 150-2500 g/ha and at these rates are generally inactive towards winter and spring cereals, e.g. maize, wheat, rye and rice.

硫代乙酸盐化合物、组合物及其使用方法

本文描述适用于调节血液尿酸水平的化合物、含有该化合物的制剂及其使用方法。在一些实施方案中，本文所述的化合物用于治疗或预防与尿酸水平异常相关的病症。

丹皮酚二氢嘧啶酮类衍生物及其制备方法和应用

本发明公开了一种丹皮酚二氢嘧啶酮类衍生物及其制备方法和应用，制备方法包括如下步骤：将丹皮酚与端基二溴烷烃化合物，在有机溶剂和缚酸剂下进行经亲核取代反应，生成溴代丹皮酚；将芳香醛、氰乙酸乙酯与硫脲，在有机溶剂和催化剂下通过环合反应，合成6‑取代苯基‑5‑氰基‑2‑硫代脲嘧啶；最后将溴代丹皮酚与合成的6‑取代苯基‑5‑氰基‑2‑硫代脲嘧啶，在有机溶剂和缚酸剂下通过亲核取代，合成丹皮酚二氢嘧啶酮类衍生物。本发明提供了一类新的丹皮酚二氢嘧啶酮类衍生物，其制备周期短，操作简单，成本低，且得到的衍生物纯度高，质量稳定；申请人还发现，通过在丹皮酚骨架上引入功能性基团二氢嘧啶酮可以改善化合物的抗肿瘤活性，有进一步的研究意义。

Производные 4-(сульфанилпиримидин-4-илметил)морфолина в качестве лигандов gaba-рецептора, для лечения тревожности, депрессии и эпилепсии

1. Соединение формулыв которой Х представляет собой -S- или -NH-;Rпредставляет собой алкил, алкенил, арилалкил, арилалкенил или арил-O-алкил, и где указанные арильные группы являются необязательно замещенными одним или более заместителями, выбранными из группы, состоящей из низшего алкила, низшего алкокси, галогена и низшего галогеналкила;Rпредставляет собой водород, низший алкил или циклоалкил;R/Rвместе с N-атомом, к которому они присоединены, образуют неароматическую 5-, 6- или 7-членную кольцевую систему, которая необязательно содержит в дополнение к N-атому один дополнительный гетероатом, выбранный из группы, состоящей из О, S и N, и где кольцевая система является необязательно замещенной группой: низший алкил, низший алкокси, -NR, -CONR, -СО-низший алкил или бензил; илиR/Rвместе с N-атомом, к которому они присоединены, могут образовывать гетероциклическую кольцевую систему, которая содержит по меньшей мере два кольца и которая необязательно содержит один или два дополнительных гетероатома, выбранных из группы, состоящей из N и О;R представляет собой водород или низший алкил;Rпредставляет собой водород или низший алкил;или аддитивные соли с кислотой этих соединений.2. Соединение по п.1, где Х представляет собой -S-.3. Соединение по п.2, где Rпредставляет собой алкил, и Rи Rобразуют вместе с N-атомом пяти- или шестичленную кольцевую систему, которая может содержать дополнительный О-гетероатом, и которая является незамещенной или замещенной низшим алкилом.4. Соединение по п.3, где Rи Rобразуют вместе с N-атомом морфолиновое кольцо.5. Соединения по п.4, где указанные соединения представляют собой 4-(2-гексилсульфанил-6-метилпиримидин-4-илмети� ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2006 134 632 (13) A (51) ÌÏÊ C07D 239/00 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2006134632/04, 22.02.2005 (71) Çà âèòåëü(è): Ô.ÕÎÔÔÌÀÍÍ-Ëß ÐÎØ Àà (CH) (30) Êîíâåíöèîííûé ïðèîðèòåò: 02.03.2004 EP ...

Pyrimidin-z-ones

Compounds of the general formula: <IMAGE> I wherein X represents halogen or trifluoromethyl; R1 and R2, independently represent hydrogen or lower alkyl; R3, R4 and R5, which may be the same or different, each represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkanoyl, lower alkenoyl, C7-16 aralkyl or C6-10 aryl or a 5-9 membered unsaturated or aromatic heterocyclic ring; one or both of R4 and R5 may also represent aroyl groups; Z represents an oxygen atom or a sulfur atom or oxide thereof or a group NR6 (wherein R6 is as defined for R hereinafter or represents the group COR7 in which R7 represents hydrogen or optionally substituted aryl, heterocyclic, aralkyl, lower alkyl or lower alkoxy group; and R represents a C6-10 carbocyclic aromatic group or a heterocyclic group containing a 5-9 membered unsaturated or aromatic heterocyclic ring which ring contains one or more heteroatoms selected from O, N and S and optionally carries a fused ring which carbocyclic or heterocyclic group may carry one or more C1-4 alkyl or phenyl groups said groups being optionally substituted; and where acid or basic groups are present, the salts thereof are useful in combating abnormal cell proliferation. The compounds of the invention are prepared by inter alia alkylation, ring closure and oxidation.

Thioacetate compounds, compositions and methods of use

본원은 혈액 요산 농도 조정에 유용한 화합물, 이를 포함하는 제제 및 이를 사용하는 방법을 기술한다. 일부 구체예에서, 본원에 기술된 화합물은 비정상적인 요산 농도와 관련된 질환의 치료 또는 예방에 사용된다. The present application describes compounds useful for the adjustment of blood uric acid concentration, formulations containing the same, and methods of using the same. In some embodiments, the compounds described herein are used in the treatment or prevention of diseases associated with abnormal uric acid levels.

Novel retinoids for emphysema treatment

FIELD: organic chemistry, medicine. SUBSTANCE: invention relates to novel retinoid compounds of the structural formula (I) or their pharmaceutically acceptable salts and pharmaceutical compositions possessing agonistic activity with respect to retinoid receptors and comprising indicated compounds wherein n = 1; d = 0 or 1; B means -CR 7 =CR 8 -, -CH 2 O- wherein R 7 and R 8 each means independently hydrogen atom; X means phenyl optionally substituted with halogen atom, or 5-membered heteroaryl comprising sulfur atom (S) as a heteroatom; R 1 means -C(=O)-R 9 wherein R 9 means alkyl, hydroxyl, amino-, heteroaryloxy-group comprising oxygen atom (O) or 6-membered heterocyclyl comprising nitrogen atom (N) as a heteroatom; R 2 means: (a) -(CR 10 R 11 ) m -Y p -R 12 ; m means a whole number from 1 to 10; p means 0 or 1; R 10 and R 11 mean hydrogen atom; Y means -O-, -S- or -NR 13 -; R 13 means hydrogen atom; R 12 means hydrogen atom, alkyl, cycloalkyl, phenyl, 5- or 6-membered heteroaryl comprising atoms N, S, O as a heteroatom, 5- or 6-membered heteroarylalkyl comprising atoms N, S, O as a heteroatom, heteroalkyl comprising atoms N, S, O as a heteroatom, 5- or 6-membered heterocyclyl comprising atoms N, S, O as a heteroatom, or 5- or 6-membered heterocyclylalkyl comprising atoms N, S, O as a heteroatom under condition that when p means 0 then R 12 doesn't mean hydrogen atom or alkyl; (b) 5- or 6-membered heteroaryl comprising atoms N, S, O as a heteroatom; (c) -Z-L wherein Z means -CR 14 =CR 15 -, -C≡C-, -C(=O) or -S-; R 14 and R 15 mean hydrogen atom; L means 5- or 6-membered heteroaryl comprising atoms N, S, O as a heteroatom; (d) -CR 14 =CR 15 -L 1 wherein L 1 means -S(O) 2 R 17 or -SO 2 NR 18 R 19 wherein R 17 means alkyl; R 18 and R 19 mean hydrogen atom; each R 3 means independently hydrogen atom, hydroxyl or oxo-group; t means 1 or 2. EFFECT: valuable medicinal properties of compounds and compositions. 59 cl, 10 tbl, 54 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 ...

Method of synthesis of 2-anilinopyrimidine derivatives

FIELD: organic chemistry. SUBSTANCE: product: derivatives of 2-anilinopyrimidine of the general formula , where R 1 and R 2 are independently each of other mean hydrogen, halogen, C 1 -C 3 -alkyl, C 1 -C 2 -halogenalkyl, C 1 -C 3 -alkoxy or C 1 -C 3 -halogenalkoxy; R 3 - hydrogen, C 1 -C 4 -alkyl, or C 1 -C 4 -alkyl substituted with hydroxy-group, cyclopropyl or cyclopropyl substituted with methyl; R 4 -C 3 -C 6 -cyclopropyl or substituted similarly or differently with methyl and/or halogen up to triple, (C 3 -C 6 )-cycloalkyl. Reagent 1: phenylguanidine salt of the general formula , where A ⊖ - anion of mineral acid, or guanidine of the general formula . Reagent 2: diketone: R 3 C(O)CH 2 C(O)R 4 . Cyclization is carried out at 60-160 C. Synthesized compounds are used in agriculture as fungicides and insecticides. EFFECT: improved method of synthesis.

Novel aromatic compound

本发明涉及关于式(A)所示的新型化合物，其中各符号的含义在说明书中给出，它们的合成，在控制害虫方面的应用以及含有此新化合物的害虫控制配方。

液晶环丙基烷基杂环化合物制备方法

通式(I)的液晶环丙基烷基或烯基杂环化合物可由式(II)的内生单官能活性化合物与式(III)的单官能活性环丙基烷基化合物反应而制得。通式(I)的液晶环丙基烷基或烯基杂环化合物具有化学，光化学热稳定性以及良好的混合相容性，光学各向异性值Δn较低，呈混合物状态时熔点较低，可用来与其它许多成分结合形成各种LC混合物。式(I)，(II)和(III)中各符号意义如说明书所述。

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Apoptosis promoters

Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.

Substituted pryimidine compounds and their use

本发明涉及如下通式的嘧啶化合物的用途其中R 1 ，R 2 ，R 3 ，A，B和Ar具有在说明书中指明的意义。根据本发明的化合物对多巴胺D 3 受体具有高的亲和性，因而可被用于治疗响应多巴胺D 3 配体的病症。

Specific kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions and methods of their use

N-alkynyl-2-chloroacetanilide derivative and herbicide containing the same

내용 없음. No content.

Process for preparing phenylamino-pyrimidine derivatves

制备通式I的化合物的方法，其中R 1 和R 2 各自为氢，卤素，C 1-3 烷基，C 1-2 卤代烷基，C 1-3 烷氧基或C 1-3 卤代烷氧基；R 3 是氢，C 1-4 烷基或被卤素、羟基或氰基取代的C 1-4 烷基，环丙基或被1-3个甲基和/或卤素取代的环丙基；R 4 是C 3-6 环烷基或被1-3个甲基和/或卤素取代的C 3-6 环烷基，这些化合物具有有价值的杀菌和杀虫性能。这些新的活性组分可用于预防致植物病微生物或有害昆虫对栽培植物的危害，并控制这些害虫。

Thioether compounds as nitrification inhibitors

Provided herein are a use of thioether compounds of formula I as nitrification inhibitors, and agricultural mixtures and compositions including the thioether compounds.

4-phenyl-pyrimidine derivatives

The invention provides compounds of the formula wherein R 1 is hydrogen or halogen; R 2 is hydrogen, halogen, lower alkyl or lower alkoxy; R 1 and R 2 may together be —CH═CH—CH═CH—, wherein R1 and R 2 together with the two carbon ring atoms to which they are attached form a fused ring; R 3 is halogen, trifluoromethyl, lower alkyl or lower alkoxy; R 4 /R 4′ are each independently hydrogen or lower alkyl; R 5 is lower alkyl, lower alkoxy, amino, phenyl, hydroxy-lower alkyl, cyano-lower alkyl, carbamoyl-lower alkyl, pyridyl, pyrimidyl, —(CH 2 ) n -piperazinyl, which is optionally substituted by one or two lower alkyl groups or by hydroxy-lower alkyl, —(CH 2 ) n -morpholinyl, —(CH 2 ) n -piperidinyl, —(CH 2 ) n+1 -imidazolyl, lower alkyl-sulfanyl, lower alkyl-sulfonyl, benzylamino, —NH—(CH 2 ) n+1 N(R 4″ ) 2 , —(CH 2 ) n+1 N(R 4″ ) 2 , —O—(CH 2 ) n+1 -morpholinyl, —O—(CH 2 ) n+1 -piperidinyl or —O—(CH 2 ) n+1 N(R 4″ ) 2 , wherein R 4″ is hydrogen or lower alkyl; and n is 0-2; X is —C(O)N(R 4″ )— or —N(R 4″ )C(O)—; and to pharmaceutically acceptable acid addition salts thereof. It has been shown that the compounds have a good affinity to the NK-1 receptor and may therefore used for the treatment of diseases related to this receptor.

Pyrimidine derivatives

Method for producing derivatives of thiouracial or their pharmaceutically-acceptable acid-additive salts

2-anilinopyrimidine derivatives or their salts showing fungicide activity

FIELD: organic chemistry. SUBSTANCE: products: derivatives of 2-anilinopyrimidine of the formula (I) where R 1 and R 2 independently each of other mean hydrogen, halogen, C 1 -C 3 -alkyl, C 1 -C 2 -halogenalkyl, C 1 -C 3 -alkoxy or C 1 -C 3 -halogenalkoxy; R 3 hydrogen, C 1 -C 4 -alkyl or C 1 -C 4 -alkyl substituted with halogen, hydroxy- and/or cyano-group; cyclopropyl which can be substituted up to three-fold with methyl and/or halogen being similar or differently; R 4 -C 3 -C 6 -C 3 -C 6 -cycloalkyl or C 3 -C 6 -cycloalkyl which can be substituted up to three-fold with methyl and/or halogen being similar or differently. Synthesized compounds were used in agriculture. EFFECT: improved method of synthesis. 9 cl, 5 tbl ОСУУЗУОС ПЧ Го РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (19) ВИ “” 2045 520‘ 13) СЛ 57 МК С 070 239/42, А 01 М 43/54 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 5011341/04, 14.04.1992 (30) Приоритет: 28.03.1987 СН 3750/87 11.04.1988 СН 1333/88 (46) Дата публикации: 10.10.1995 (56) Ссылки: Патент США М 4600428, кл. А 01М 43/54, 1986. (71) Заявитель: Циба-Гейги АГ (СН) (72) Изобретатель: Адольф Хубеле[ОЕ] (73) Патентообладатель: Циба-Гейги АГ (СН) (54) ПРОИЗВОДНЫЕ 2-АНИЛИНО-ПИРИМИДИНА ИЛИ ИХ СОЛИ, ПРОЯВЛЯЮЩИЕ ФУНГИЦИДНУЮ АКТИВНОСТЬ (57) Реферат: Использование: сельское хозяйство. Сущность — изобретения: — производные 2-анилино-пиримидина Фф-лы |1 где К и К2 независимо друг от друга означают водород, галоген, С1-Сз алкил, С 1-С2 галогеналкил, С41-Сз алкокси или С 1-Сз галогеналкокси, Кз водород, С 1-С4 алкил, или замещенный галогеном, гидрокси- и/или циано-группой С.-Сд алкил; циклопропил или замещенный до трех раз одинаково или различно метилом и/или галогеном циклопропил; КВ.-Сз-Сь циклоалкил или замещенный до трех раз одинаково или различно метилом иили галогеном С 3-Св циклоалкил. Структура ф-лы 1: 2сибзЗ. п. ф-лы, 5 табл. 2045520 С1 КО ОСУУЗУОС ПЧ Го КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ (19) 13) ВО’ 2045 ...

Substituted cyclopentyl - azines as casr- active compounds

Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

Substituted diaminocarboxamides and diaminocarbonitrile pyrimidines, compositions thereof and methods of treatment therewith

Substituted pyrimidine compounds and their uses (Substituted Pyrimidine Compounds and Their Use)

하기 화학식의 피리미딘 화합물의 용도가 제공된다. 이 화합물은 도파민 D 3 수용체에 대한 친화성이 높아서, 도파민 D 3 리간드에 대해 반응하는 질환의 치료에 사용된다. (식 중, R 1 , R 2 , R 3 , A, B 및 Ar은 명세서에 기재한 정의를 갖는다.)

Acrylic acid ester derivative, manufacture and agricultural drug composition

(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。

Aryl amine alkyl sulfide class compound of class Ruzadolane structure and preparation method thereof

一种类卢扎朵仑结构的芳胺基烷基硫类化合物及其制备方法，该化合物是将Ar 1 ‑X 1 、通式Ⅲ所表示的化合物、Ar 2 ‑X 2 及硫源加入到溶剂中，按反应式(1)加热反应完全后得到；或者是将Ar 1 ‑X 1 、通式Ⅲ所表示的化合物及Ar 2 ‑S ‑ M + 加入到溶剂中，按反应式(2)加热反应完全后得到。本方法操作简单高效，反应条件温和，所用到的试剂廉价易得，安全性强，适于工业化大生产。

Thioacetate compounds, compositions and methods of use

本文描述适用于调节血液尿酸水平的化合物、含有该化合物的制剂及其使用方法。在一些实施方案中，本文所述的化合物用于治疗或预防与尿酸水平异常相关的病症。

ROR GAMMA MODULATORS (RORγ)

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2017 145 928 A (51) МПК C07D 213/71 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2017145928, 03.06.2016 (71) Заявитель(и): ЛИД ФАРМА ХОЛДИНГ Б.В. (NL), САНОФИ (FR) Приоритет(ы): (30) Конвенционный приоритет: 05.06.2015 EP 15170768.4 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 09.01.2018 (86) Заявка PCT: (87) Публикация заявки PCT: WO 2016/193468 (08.12.2016) A Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, стр. 3, ООО "Юридическая фирма Городисский и Партнеры" (57) Формула изобретения 1. Соединение формулы I A (Формула I) R U 2 0 1 7 1 4 5 9 2 8 (54) МОДУЛЯТОРЫ ROR ГАММА (RORγ) 2 0 1 7 1 4 5 9 2 8 EP 2016/062708 (03.06.2016) R U (43) Дата публикации заявки: 10.07.2019 Бюл. № 19 (72) Автор(ы): КАЛС, Йосеф Мария Герардус Барбара (NL), МАШНИК, Давид (FR), НАБЮЮРС, Сандер Бернардус (NL), САБЮКО, Жан-Франсуа (FR), ШИО, Лоран (FR) Стр.: 1 A 2 0 1 7 1 4 5 9 2 8 A R U 2 0 1 7 1 4 5 9 2 8 Стр.: 2 R U Мета или пара или его фармацевтически приемлемая соль, где: - A11-A14 являются N или CR11, CR12, CR13, CR14, соответственно, при условии, что не более двух из четырех положений A в A11-A14 одновременно могут быть N; - A6, A7, A8, A9,A10 являются N or CR6, CR7, CR8, CR9, CR10, соответственно, при условии, что, по крайней мере, одно, но не более двух из пяти положений A в A6, A7, A8, A9, A10 является N; - R1 является C(2-6)алкилом, C(3-6)циклоалкилом, C(3-6)циклоалкилC(1-3)алкилом, (ди)C(3-6)циклоалкиламино или (ди)(C(3-6)циклоалкилC(1-3)алкил)амино, где все атомы углерода алкильных групп необязательно замещены одним или более F и где все атомы углерода циклоалкильных групп необязательно замещены одним или более F или метилом; - R2 и R3 независимо являются H, F, метилом, этилом, гидрокси, метокси, или R2 и R3 вместе являются карбонилом, все алкильные группы, если присутствуют, необязательно замещены одним или более F; - R4 является H или C(1-6)алкилом ...

Arylaniline β2 adrenergic receptor agonist

Weed control method

FIELD: agriculture; plant protection chemicals. SUBSTANCE: fields to be protected are treated with a derivative of pyrimidine described by the following formula , where R is hydrogen, lower alkyl, C 1 -C 2 , alkoxymethyl, benzyloxymethyl, ethoxycarbonyl ethyl, methyl cyanide or a group , where R 1 is hydrogen, methyl; R 2 is methyl, phenyl substituted or not substituted with a nitro group; X - halogen, methyl methyl phenoxy or its salt, 0.16-10 g/ar. EFFECT: more efficient weed control. 13 tbl

Aminopyrimidines as kinase inhibitors

Настоящее изобретение относится к новым соединениям общей формулы ii-d и их фармацевтически приемлемым солям, которые обладают свойствами ингибитора активности Aurora-протеинкиназы и могут быть использованы при лечении пролиферативных расстройств. В формуле ii-d: R 2 представляет собой C 1-3 -алкил или циклопропил; R 5 представляет собой CH 2 CH 3 , CH 2 CF 3 , CH 2 CH 2 CF 3 , или R y представляет собой или J 1 представляет собой атом водорода или СН 3 , J 2 представляет собой C 1-4 -алкил; и Су представляет собой С 3-5 -циклоалкил. 5 н. и 7 з.п. ф-лы, 8 табл. РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 423 361 (13) C2 (51) МПК C07D 405/14 (2006.01) A61K 31/506 (2006.01) A61P 35/00 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (72) Автор(ы): БИНЧ Хэйли (US), (24) Дата начала отсчета срока действия патента: МОРТИМОР Майкл (GB), 03.11.2006 ФРАЙСС Дамьен (GB), ДЭВИС Крис (GB), Приоритет(ы): О'ДОННЕЛЛ Майкл (GB), (30) Конвенционный приоритет: ЭВЕРИТТ Саймон (GB), 03.11.2005 US 60/732,951 РОБИНСОН Дэниел (GB), 04.11.2005 US 60/733,557 ПИНДЕР Джоанн (GB), (43) Дата публикации заявки: 10.12.2009 Бюл. № 34 МИЛЛЕР Эндрю (GB) (21)(22) Заявка: 2008122046/04, 03.11.2006 2 4 2 3 3 6 1 R U (86) Заявка PCT: US 2006/042994 (03.11.2006) C 2 C 2 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 03.06.2008 (87) Публикация заявки РСТ: WO 2007/056164 (18.05.2007) Адрес для переписки: 129090, Москва, ул.Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е. Назиной (54) АМИНОПИРИМИДИНЫ В КАЧЕСТВЕ ИНГИБИТОРОВ КИНАЗ (57) Реферат: Настоящее изобретение относится к новым соединениям общей формулы ii-d и их фармацевтически приемлемым солям, которые обладают свойствами ингибитора активности Aurora-протеинкиназы и могут быть использованы при лечении пролиферативных расстройств. В формуле ii-d: R 2 представляет собой C1 ‐ 3-алкил или циклопропил; R 5 представляет собой CH2CH3, ...

Herbicidal phenylpyrimidines.

Uso de fenilpirimidinas de fórmula (I) (ver Fórmula) o sus sales o derivados aceptables para uso agrícola como herbicidas, en donde las variables se definen de acuerdo con la descripción, fenilpirimidinas específicas de fórmula (I), procesos e intermediarios para preparar las fenilpirimidinas de fórmula (I), composiciones que las comprenden, y su uso como herbicidas, es decir, para controlar plantas dañinas, y también un método para controlar la vegetación no deseada que comprende permitir que una cantidad efectiva de herbicida de al menos una fenilpirimidina de la fórmula (I) actúe sobre las plantas, su semilla y/o su hábitat.