ЗАМЕЩЕННЫЕ АМИДЫ ФЕНИЛЦИКЛОГЕКСАНКАРБОНОВОЙ КИСЛОТЫ, ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ И ЛЕКАРСТВЕННОЕ СРЕДСТВО НА ИХ ОСНОВЕ

Изобретение относится к замещённым амидам фенилциклогексанкарбоновой кислоты формулы (I) в которой A, D, Е и G одинаковы или различны и означают группу СН или атом азота, R1 означает группу СН2-ОН или остаток формулы CO-NH2, R2 означает алкил, содержащий 1-8 атомов углерода, который может быть прерван атомом кислорода, или пиперизин, содержащий остаток формулы NR4, где R4 означает водород, алкил, содержащий 1-6 атомов углерода, или циклоалкил, содержащий 3-7 атомов углерода, причем алкил, содержащий 1-8 атомов углерода, который может быть прерван атомом кислорода, замещен 1-3 гидроксильными группами или остатком формулы –NR5R6, где R5 и R6 означают водород, или вместе с атомом азота образуют кольцо морфолина, R3 означает фенильное кольцо, и их соли. Изобретение также относится к лекарственному средству, обладающему ингибирующим поглощением аденозина, на основе этих соединений. Технический результат – получение новых соединений и лекарственного средства на их основе в целях лечения ишемических ...

СОЕДИНЕНИЯ С КОНДЕНСИРОВАННЫМ КОЛЬЦОМ И ИХ ИСПОЛЬЗОВАНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Изобретение относится к области медицины и органической химии и касается терапевтического средства против гепатита С, содержащего соединения формулы I, фармкомпозиции, содержащей указанные соединения, и ингибитора полимеразы вируса гепатита С. Соединения обладают существенно более высокой активностью, чем известные. 9 с. и 24 з.п.ф-лы, 218 табл.

АМИДНЫЕ ПРОИЗВОДНЫЕ И ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ, СПОСОБ ИХ ПОЛУЧЕНИЯ И МЕДИЦИНСКОЕ ПРИМЕНЕНИЕ

Настоящее изобретение относится к cоединению общей формулы (I), или его энантиомеру, или их смеси, или его фармацевтически приемлемым солям:В формуле (I) кольцо Р выбрано из пятичленного гетероарила, имеющего от одного до двух гетероатомов, выбранных из группы, состоящей из N, О и S, в качестве атома кольца, и пятичленного гетероциклила, имеющего один гетероатом N в качестве атома кольца; кольцо Q выбрано из фенила и пиридила; А, В или Y выбран из -СН- и N; Rвыбран из алкила, содержащего от 1 до 6 атомов углерода, и циклоалкила, содержащего от 3 до 6 атомов углерода, где указанный алкил, содержащий от 1 до 6 атомов углерода, или циклоалкил, содержащий от 3 до 6 атомов углерода, необязательно дополнительно замещен одной или более чем одной группой, выбранной из группы, состоящей из алкила, содержащего от 1 до 6 атомов углерода, галогена и галогеналкила, содержащего от 1 до 6 атомов углерода; Rвыбран из галогена и галогеналкила, содержащего от 1 до 6 атомов углерода; Rявляются одинаковыми ...

НОВЫЕ ПРОИЗВОДНЫЕ БЕНЗИМИДАЗОЛА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Настоящее изобретение относится к новым производным бензимидазола, имеющих общую формулу (I), где А обозначает -CH2-, -C(O), -C(O)-C(Ra)(Rb)-, Х обозначает -CH-радикал; Ra и Rb обозначают, независимо, атом водорода или (C1-C6)алкильный радикал; ! R1 обозначает атом водорода или (C1-C8)алкильный радикал; R2 обозначает ! (C1-С8)алкильный радикал; R3 обозначает -(CH2)p-Z3, -C(O)-Z'3 или -C(O)-NH-Z''3; Z3 обозначает (C1-C6)алкильный, (C2-C6)алкенильный, (C1-C6)алкокси, (C1-C6)алкилкарбонильный, (C1-C6)алкоксикарбонильный, ! (C1-C6)алкил-N(RN)карбонильный, (C3-C7)циклоалкильный, арильный, арилтио или гетероарильный радикал, Z3 присоединен к радикалу -(CH2)р- через атом углерода, гетероарильный радикал, представляющий собой 5-10-членный гетероарил, включающий 1-2 одинаковых или разных гетероатомов, выбранных из серы, азота или кислорода, и необязательно замещен одним или несколькими одинаковыми или разными заместителями, выбранными из галогена, нитрогруппы или -(CH2)p'-V30-Y3; арильный радикал ...

СОЕДИНЕНИЯ И КОМПОЗИЦИИ В КАЧЕСТВЕ МИМЕТИКОВ ТРО

... 1. Изобретение относится к новым соединениям формулы I ! ! где: n означает 0 или 1; Z означает N, CR8, где R8 означает Н, С1-С6алкил; R1, R2, R4 и R5 независимо означают Н, галоген, ОН, -XNR9R10, где X означает химическую связь, a R9 и R10 означают Н; R3 означает -NR11S(O)2R12, -NR11C(O)R12, -C(O)OR11, -NR11R12, S(O)2NR11R12 и -C(O)NR11R12, где R11 и R12 независимо означают H, С1-С6алкил; R6 означает галоген, С1-С6алкил; R7 означает фенил, замещенный 1 или 2 группами, независимо выбранными из фтора и С1-С6алкила, и его фармацевтически приемлемым солям. Соединения проявляют активность миметика ТРО, что позволяет получать из них лекарственные средства для повышения уровня тромбоцитов в крови животного. 4 н. и 4 з.п. ф-лы.

КОНДЕНСИРОВАННЫЕ 5-ЧЛЕННЫЕ ГЕТЕРОЦИКЛЫ ИЛИ ИХ СОЛИ, ПРОЯВЛЯЮЩИЕ АКТИВНОСТЬ ПО ТОРМОЖЕНИЮ АГРЕГАЦИИ

Использование: в качестве препаратов, проявляющих активность по торможению агрегации. Сущность изобретения: конденсированные 5-членные гетероциклы ф лы (1) с определенными буквенными значениями, проявляющие активность по торможению агрегации. 1 табл. (I).

2,5- ИЛИ 2,6-ДИЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ ГИДРОХИНОНА, СОДЕРЖАЩИЕ ПО КРАЙНЕЙ МЕРЕ ОДНУ КАРБОКСИ-, СУЛЬФО- ИЛИ АМИДОГРУППУ, ПРИМЕНЯЕМЫЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Изобретение относится к новым производным гидрохинона формулы (I), где Ra, Rb, R1-R3 определены в формуле изобретения, промежуточным соединениям для получения производных гидрохинона формулы (I), а также фармацевтическим композициям для применения в лечении и/или предотвращения, например, аутоиммунных, иммунологических, ревматологических, сосудистых, офтальмологических, фиброзных, метаболических и желудочно-кишечных расстройств, нейровоспалительных и нейродегенеративных заболеваний, новообразований и связанных с раком заболеваний, гормональных заболеваний и иммунологических нарушений, возникающих в результате вирусных и бактериальных инфекционных заболеваний и их осложнений. 4 н. и 15 з.п. ф-лы, 11 ил., 59 табл., 5 пр.

ГЕТЕРОЦИКЛИЛ-БЕНЗОИЛ-ГУАНИДИНЫ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Гетероциклил-бензоил-гуанидины формулы I, где R1-А, CF3, CH2F, CHF2, C2F5, Hal , Х-R4; R2 - SO2-А; R3 = Н, R4 -Н или А; Het- насыщенный или ненасыщенный ароматический одно- или двухъядерный ароматический гетероцикл с 1 - 2 атомами азота или с атомом кислорода, связанный через азот или углерод, возможно замещенный алкилом, аминогруппой или гидроксильной группой; А - алкил; Х = О, Hal - F, Cl, Br, I, а также их физиологически приемлемые соли являются ингибиторами Na+/Н+ - насоса антипорта и, таким образом, представляют собой хорошие антиаритмические средства. 4 с. и 2 з.п. ф-лы.

АЗОТСОДЕРЖАЩИЕ ПРОИЗВОДНЫЕ ГЕТЕРОАРИЛА

... 1. Соединение формулы (I) где R1 выбирают из группы, включающей -OR7 и -NR8R9; где R7 выбирают из группы, включающей водород, алкил, замещенный алкил, циклоалкил, замещенный циклоалкил, алкенил, замещенный алкенил, алкинил, замещенный алкинил, арил, замещенный арил, гетероарил, замещенный гетероарил, гетероцикл и замещенный гетероцикл; R8 и R9 независимо выбирают из группы, включающей водород, алкил, замещенный алкил, циклоалкил, замещенный циклоалкил, алкенил, замещенный алкенил, алкинил, замещенный алкинил, арил, замещенный арил, гетероарил, замещенный гетероарил, гетероцикл и замещенный гетероцикл, или, альтернативно, R8 и R9 вместе с атомом азота, к которому они присоединены, образуют гетероциклическую или замещенную гетероциклическую кольцевую группу; R2 и R12 независимо выбирают из группы, включающей водород, алкил, замещенный алкил, циклоалкил, замещенный циклоалкил, алкенил, замещенный алкенил, алкинил, замещенный алкинил, арил, замещенный арил, гетероарил, замещенный гетероарил ...

НОВОЕ СУЛЬФОНАМИДНОЕ ПРОИЗВОДНОЕ МАЛОНОВОЙ КИСЛОТЫ И ЕГО ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ

... 1. Производное сульфонилмалонамида, представленное следующей формулой (I) ! ! где R1 представляет собой необязательно замещенный C1-8 алкил, необязательно замещенный C2-6 алкенил, необязательно замещенный C2-6 алкинил, необязательно замещенный C3-10 циклоалкил, необязательно замещенный C3-10 циклоалкил C1-6 алкил, необязательно замещенный гетероцикл, необязательно замещенный арил, необязательно замещенный арил C1-6 алкил, необязательно замещенный арилокси C1-6 алкил, необязательно замещенный арил C2-6 алкенил, необязательно замещенный гетероарил, необязательно замещенный гетероарил C1-6 алкил, необязательно замещенный гетероарилокси C1-6 алкил или необязательно замещенный гетероарил C2-6 алкенил; ! один из R2 и R3 представляет собой атом водорода или атом галогена, а другой представляет собой атом галогена, необязательно замещенный C1-6 алкил, необязательно замещенный C1-6 алкокси, необязательно замещенный C2-6 алкенил, необязательно замещенный C2-6 алкинил, -(CH2)n-С(O)-NR5R6 (где n представляет ...

НОВЫЕ ПРОИЗВОДНЫЕ БЕНЗИМИДАЗОЛА И ИМИДАЗОПИРИДИНАИ ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ЛЕКАРСТВЕННЫХ СРЕДСТВ

Соединение общей формулы (I) в рацемической, энантиомерной форме или в виде любых сочетаний указанных форм, где А обозначает -CH2-, -C(O)-, -C(O)-C(Ra)(Rb)-; X обозначает -CH-радикал или атом азота; Ra и Rb обозначают, независимо, атом водорода или (C1-C6)алкильный радикал; R1 обозначает атом водорода или (C1-C8)алкильный радикал; R2 обозначает (C1-C8)алкильный радикал; или R1 и R2 вместе с атомом азота, к которому они присоединяются, образуют гетеробициклоалкил или гетероциклоалкил, необязательно замещенный одним или несколькими идентичными или разными (C1-C6)алкильными заместителями; R3 обозначает -(CH2)p-Z3, -C(O)-Z'3, -CH(OH)-Z'3 или -C(O)-NH-Z"3; Z3 обозначает (С1-C6)алкильный, (С2-C6)алкенильный, (С1-C6)алкокси, (С1-C6)алкилкарбонильный, (С1-C6)алкоксикарбонильный, (С1-C6)алкил-N(RN)карбонильный, (С3-C7 )циклоалкильный, гетероциклоалкильный, арильный, арилтио или гетероарильный радикал, Z3 присоединен к радикалу -(CH2)p- через атом углерода, (C3-C7)циклоалкильный и гетероциклоалкильный ...

ЗАМЕЩЕННЫЕ 2-ФЕНИЛБЕНЗИМИДАЗОЛЫ И 2-ФЕНИЛИНДОЛЫ, ИХ ПОЛУЧЕНИЕ И ПРИМЕНЕНИЕ

... 1. Производные 2-фенилбензимидазола или -индола общей формулы I где А принимает значения N или СН; R1 означает водород, разветвленный или неразветвленный C1-С6-алкил, причем один атом углерода алкильного остатка может иметь еще OR11, где R11 означает водород или C1-С4алкил; R2 означает водород, хлор, фтор, бром, йод, разветвленный или неразветвленный C1-C6-алкил, нитро, CF3, CN, NR21R22, NH-CO-R23, OR21, где R21 и R22 независимо друг от друга означают водород или С1-С4-алкил и R23 означает водород, С1-С4-алкил или фенил; R3 означает -NR31R32, (CH2)q-NR33R34, где q может принимать значения 1, 2 или 3, R31 означает водород, C1-C6-алкил, (CH2)rNR33R34, где R32 означает (CH2)rNR33R34, где для R31 и R32 независимо друг от друга r означает 2, 3, 4, 5 или 6, R33 и R34 независимо друг от друга могут означать водород, C1-С6-алкил, образующий вместе с азотом кольцо с 3 до 8 атомами, которое может иметь дополнительный гетероатом, выбранный из группы, включающей О, N-C1-C4-алкил N-(C)n-фенил, где n ...

СОЕДИНЕНИЯ ДЛЯ АФФИННОЙ ХРОМАТОГРАФИИ И ДЛЯ ПРОДЛЕНИЯ ВРЕМЕНИ ПОЛУЖИЗНИ ТЕРАПЕВТИЧЕСКОГО СРЕДСТВА

2-(ФЕНИЛ ИЛИ ГЕТЕРОЦИКЛО)-1H-ФЕНАНТРО[9.10-D]ИМИДАЗОЛЫ В КАЧЕСТВЕ ИНГИБИТОРОВ MPGES-1

... 1. Соединение по п.1 формулы B: ! ! или его пролекарство, или фармацевтически приемлемая соль указанного соединения или пролекарства, где ! R3 представляет собой и ! R6 выбран из группы, состоящей из (1) H; (2) F; (3) Cl; (4) Br; (5) I; (6) -CN; (7) С1-10алкила или C2-10алкенила, где один или несколько атомов водорода, связанных с указанным С1-10алкилом или C2-10алкенилом, могут быть замещены атомом фтора, или два атома водорода на смежных атомах углерода могут быть объединены вместе и замещены группой -CH2- с образованием циклопропильной группы, или два атома водорода по одному и тому же атому углерода могут быть замещены и объединены вместе с образованием спиро C3-6циклоалкильной группы, и где указанный С1-10алкил или C2-10алкенил необязательно может быть замещен одним-тремя заместителями, независимо выбранными из группы, состоящей из -OH, ацетила, метокси, этенила, Rl1-O-C(O)-, R35-N(R36)-; R37-N(R38)-C(O)-, циклопропила, пирролила, имидазолила, пиридила и фенила, при этом указанный ...

АЦИЛАМИНОЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ КОНДЕНСИРОВАННЫХ ЦИКЛОПЕНТАНКАРБОНОВЫХ КИСЛОТ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ФАРМАЦЕВТИЧЕСКИХ СРЕДСТВ

... 1. Соединение формулы I в любой из его стереоизомерных форм или сочетании стереоизомерных форм в любом соотношении, или его физиологически приемлемая соль, или физиологически приемлемый сольват любого из них ! ! где кольцо A является циклоалкановым кольцом с числом членов от 3 до 7, бензольным кольцом или моноциклическим 5-членным или 6-членным ароматическим гетероциклическим кольцом, содержащим 1 или 2 одинаковых или разных гетерочленов кольца, выбранных из группы, содержащей N, N(R0), O и S, причем циклоалкановое кольцо может необязательно иметь один или более одинаковых или разных заместителей, выбранных из группы, содержащей фтор и (C1-C4)-алкил, а бензольное и гетероциклическое кольца могут необязательно иметь один или более одинаковых или разных заместителей, выбранных из группы, содержащей галоген, R1, HO-, R1-O-, R1-C(O)-O-, R1-S(O)2-O-, R1-S(O)m-, H2N-, R1-NH-, R1-N(R1)-, R1-C(O)-NH-, R1-C(O)-N(R71)-, R1-S(O)2-NH-, R1-S(O)2-N(R71)-, R1-C(O)-, HO-C(O)-, R1-O-C(O)-, H2N-C(O)-, R1 ...

ПРОИЗВОДНЫЕ БЕНЗИМИДАЗОЛА, СМЕСЬ ИХ ИЗОМЕРОВ ИЛИ ОТДЕЛЬНЫЕ ИЗОМЕРЫ И ИХ СОЛИ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ С АНТАГОНИСТИЧЕСКОЙ В ОТНОШЕНИИ АНГИОТЕНЗИНА АКТИВНОСТЬЮ НА ИХ ОСНОВЕ

Предлагаются производные бензимидазола общей формулы I, приведенной в описании. Указанные в описании производные, смесь их изомеров или отдельные изомеры и их соли могут представлять собой активное вещество фармацевтической композиции с антагонистической в отношении ангиотензина активностью.

КОНДЕНСИРОВАННОЕ ГЕТЕРОЦИКЛИЧЕСКОЕ СОЕДИНЕНИЕ И ЕГО ИСПОЛЬЗОВАНИЕ ДЛЯ БОРЬБЫ С ВРЕДИТЕЛЯМИ

... 1. Конденсированное гетероциклическое соединение формулы (1):,где Aпредставляет собой -NR-, атом кислорода или атом серы;Aпредставляет собой атом азота или =CR-;Aпредставляет собой атом азота или =CR-;Rпредставляет собой углеводородную группу с С-Cцепью, необязательно содержащую один или несколько атомов или групп, выбранных из Группы X, или C-Cалициклическую углеводородную группу, необязательно содержащую один или несколько атомов или групп, выбранных из Группы Y;R, R, Rи Rявляются одинаковыми или разными и независимо представляют собой углеводородную группу с C-Cцепью, необязательно содержащую один или несколько атомов галогена, фенильную группу, необязательно содержащую один или несколько атомов или групп, выбранных из Группы Z, 5-членную гетероциклическую группу, необязательно содержащую один или несколько атомов или групп, выбранных из Группы Z, 6-членную гетероциклическую группу, необязательно содержащую один или несколько атомов или групп, выбранных из Группы Z, -OR, -S(O)R, -NRR ...

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 ...

Способ получения производных пиперазина или пиперидина или их солей

Способ получения 2-замещенных производных 1-циннамилбензимидазола

HETEROZYKLISCH SUBSTITUIERTE BENZIMIDAZOLE, DEREN HERSTELLUNG UND ANWENDUNG

VERFAHREN ZUR HERSTELLUNG UND REINIGUNG VON 1,7'-DIMETHYL-2'-PROPYL-2,5'-BI-1H-BENZIMIDAZOL

Schaedlingsbekaempfungs- und Desinfektionsmittel

VERFAHREN ZUR SYNTHESE DER BISBENZIMIDAZOLEN UND IHREN DERIVATEN.

Benzimidazol-Derivate und Verfahren zu deren Herstellung

VERFAHREN ZUR HERSTELLUNG VON IMIDAZOLDERIVATEN

Heterocyclyl-benzoylguanidine

POLYAMINE UND IHRE THERAPEUTISCHE VERWENDUNG

VERFAHREN ZUM OPTISCHEN AUFHELLEN VON ORGANISCHEN MATERIALIEN

Insektizides und akarizides Mittel

Electrophotographic materials

Photoconductive compositions as in Specification 964,873 use as photoconductive compounds pyrroles, pyrrolines, pyrrolidines, indoles, indolenines, indolines and naphthopyrrolines, including substituted derivatives and cyanine and merocyanine dyes derived from such. Many typical compounds are mentioned. The sensitizing dyestuffs, resins and auxiliary materials mentioned in Specification 964,873 may be used. Specified resins are polyvinyl formal and butyral, polyvinyl-carbazole and a terpolymer of vinyl chloride, vinyl acetate and maleic anhydride. Specifications 856,770, 883,312, 916,660 and 964,871 also are referred to.ALSO:A cyanine dye of the formula is made by reacting 3-ethyl-2-methyl-benzthiazolium iodide with N-methylisatin-a -anil. Specifications 344,409, 354,898, 428,222, 428,359, 428,360, 633,824, 856,770, 883,312, 916,660, 964,871 and 964,875 are referred to.

BENZIMIDAZOLYL SULPHIDES AND SULPHONES

... 1388041 Benzimidazoles E R SQUIBB & SONS Inc 29 Feb 1972 [4 March 1971] 9328/72 Heading C2C Novel compounds (I) (including salts thereof) where R is H, OH, alkoxy, NH 2 , alkylamino, NHCO 2 R5, alkyl, NO 2 , -SCN, halo, aralkyl, SH, aryl or alkylaryl, R1, R2, R21, R3 and R4 are H, alkyl, aralkyl or optionally substituted aryl, R5 is alkyl, aryl or cycloalkyl, m is 1 or 2, n is 0 or 1, n1 is 0 to 4, n + n1 is 4 or less and n2 is 0 or 1, are made by standard methods. Pharmaceutical preparations having anthelmintic action contain (I) as active ingredient. Administration is, e.g. orally.

PROCESS FOR PREPARING QUATERNARY SALTS, NOVEL QUATERNARY SALTS AND PHOTOGRAPHIC EMULSIONS CONTAINING THEM

... 1283835 Heterocyclic quaternary salts EASTMAN KODAK CO 23 April 1970 [28 April 1969 (2)] 19547/70 Heading C2C [Also in Division G2] Novel heterocyclic quaternary salts of the formula in which Z represents the atoms required to complete a mono- or poly-nuclear heterocyclic ring system containing a 5- or 6-membered ring including the quaternary nitrogen atom, the atoms being selected from C, N, O, S and Se, n is 0 or 1, m is 0 or 1-4, X is an acid anion, R1 is hydrogen or an alkyl, aralkyl, aryl or alkylthio group, and R2 is a 1-hydrazono-C 1-5 -alkyl group, are prepared by reacting a salt of the formula with a compound of the formula where R6 is formyl, acetyl, propionyl, butyryl or pentanoyl, and condensing the intermediate carbonyl compound with a hydrazine having two hydrogen atoms attached to the same nitrogen atom. Specified hydrazine reactants include heterocyclic hydrazines, phenylhydrazines, in which the phenyl group may be substituted by alkyl, sulpho, ...

Benzoic acid derivatives useful as intermediates

Aromatic heterocyclic derivatives have the formula wherein R1 represents wherein R3 represents hydrogen, -OR4 wherein R4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R3 represents wherein r' and r'' represent hydrogen, lower alkyl or together form a heterocycle, R2 represents hydrogen or -CH3 and Ar represents (A) (B) wherein Z is O or S, (C) wherein R5 is lower alkyl or (D) wherein R6 is hydrogen or alkyl having 1-10 carbon atoms and R7 represents alkyl having 4-12 carbon atoms or cycloalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or -N-R8 when R8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R6 is alkyl having 1-4 carbon atoms and R7 is branched alkyl having 4-12 atoms useful in veterinary or human therapy and in cosmetic formulations.

Improved die attach methods and apparatus for micro-fluid ejection device

Manufacture of substituted phenylaminobenzimidazoles

Process for the manufacture of substituted phenylaminobenzimidazoles which comprises reacting a 4- nitro, 4-sulpho or 4-amino 1,2- diaminobenzene, optionally carrying an alkyl group or alkoxy group having 1 to 4 carbon atoms, or a chlorine or bromine atom, with an optionally substituted aminobenzoic acid in the presence of polyphosphoric acid at a temperature in the range of 50 to 150 DEG C.

A method for incorporating color formers in emulsions

... 975,363. Photographic colour couplers. GENERAL ANILINE & FILM CORPORATION. May 30, 1961 [June 9, 1960], No. 19538/61. Heading G2C. Colour couplers containing a benzimidazole nucleus are incorporated in gelatine silver halide emulsions by disolving in an alkyl lactate in which the alkyl group contains 1-3 carbon atoms, diluting this solution with an aqueous solution which may contain a surface active agent and adding the dispersion thus formed to the emulsion. Specified colour couplers are those of formulae: wherein R is a reactive methylene, ethenol or phenolic hydroxy group, R1 is hydroxy aryl which may be substituted, R2 is alkyl with at least ten carbon-atoms, R3 is a water-solubilising group e.g. sulphur or carboxy, R4 is -NH-COCH2A in which A is acyl, R5 is hydrogen, carboxyalkyl, allyl or alkyl with 1 to 4 carbon atoms, R6 is allyl, alkyl with 1 to 4 carbon atoms, aryl or heterocyclic, X is halogen and n is 1 or 2 and the contour coupler of formula ...

New Benzimidazoles, their production and use

... 1,191,112. Insecticides/acaricides containing benzimidazoles. AGRIPAT S.A. 5 May, 1967 [6 May, 1166], No. 20959/67. Heading A5E. [Also in Division C2] Insecticidal and acaricidal compositions comprise, as active agent, a benzimidazole derivative of formula: where R represents H or a metal cation, each of X and X, represents fluorine, chlorine, bromine, trifluoromethyl, alkyl, alkoxy, nitro, hydroxyl, amino, alkanoylamino, optionally substituted phenoxy or phenylsulphonyl or the radical of a sulphonic acid or its ester or amide, m is 1-5, n is 1-4, providing that, in all, at least 3 of the X and X, groups are halogen atoms and/or trifluoromethyl groups of which none is in the position ortho to the linking position of the radical, and that there are at most 2 trifluoromethyl groups present in each of the two benzene nuclei. The compositions may be formulated as dusts, sprinkling agents, aqueous dispersions, wettable powders, pastes, emulsion concentrates, solutions and aerosols, and may contain ...

BIS-IMIDAZOLYL-BISPHENYLMETHANES AND THEIR SALTS

... 1,268,690. Bis-imidazole or -benzimidazolebis-phenyl-methanes. FARBENFABRIKEN BAYER A.G. 27 Oct., 1969 [5 Nov., 1968], No. 52502/69. Heading C2C. Novel compounds I (including salts thereof) where R1 is H, alkyl or optionally substituted aryl, R2 and R3 are H, alkyl, optionally substituted aryl or comprise a fused benzo-ring, X and Y are alkyl, 5-alkyl, O-alkyl or an electronegative substituent, m is 0, 1 or 2 and n is 0, 1 or 2, are made by interacting appropriate diphenyl-dihalo-methanes and (benz)imidazoles. Pharmaceutical preparations showing antimycotic and hypocholesterinaemic activity, activity against pathogenic protozoa, viruses and bacteria, and activating the granulation in wound healing contain I as active ingredient. Administration is orally, parenterally or topically.

PRODUCTION OF 1,3-DIAZA-HETEROCYCLES

A process and products for the improvement of the optical properties of organic material

Compounds of general formula in which A is an aromatic nucleus which may be substituted and in which 2 adjacent carbons are linked directly to B and the group B is sulphur or the group in which R1 is H or an organic substituent, R is an organic substituent, R2 is an organic substituent having at least 3 conjugated double bonds which are also in conjugation with the >C=N bond of the heterocyclic ring, and X is an acid residue, may be used in conjunction with washing agents for the treatment of organic materials. Suitable washing agents are, for example, soaps; salts of sulphonate washing agents, such as sulphonated benzimidazoles substituted on the 2-carbon atom by high alkyl radicals; salts of monocarboxylic acid esters of 4-sulphophthalic acid with high fatty alcohols; salts of fatty alcohol sulphonates; alkylaryl sulphonic acids; or condensation products of high fatty acids with aliphatic hydroxy or amino sulphonic acids.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

Method of preparation of new anthelminthic compositions.

Composition and sythesis of new reagents for inhibition of HIV replication

Benzimidazole compounds.

A range is disclosed of benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DMA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents.

This invention provides a compound of the formula (i); or the pharmaceutically acceptable salts thereof, wherein y1, y2, y3, and y4 are independently selected from n, ch, etc., r1 is h, c1-8 alkyl, etc., q1 is 5-12 membered monocyclic or bicyclic aromatic ring optonally containing up to 4 heteroatoms selected from o,n and s,etc., a is a 5-6 membered monocyclic aromatic ring optionally containing up to 3 heteroatoms selected from o,n and s,etc.;B is c1-6 alkylene optionally substituted with an oxo group, etc.; w is nh, o, etc.; r2 is h,c1-4 alkyl, etc.; z is a 5-12 membered monocyclic or bicyclic aromatic ring optionally containing up to 3 heteroatoms selected from o,n and s, etc.; l is halo, c1-4 alkyl,,etc.; m is0, 1 or 2; r3 and r4 are independently selected from o,n and s, etc.; l is halo, c1-4 alkyl ; r5 is h, c1-4 alkyl, etc.; q2 is a 5-12 membered monocyclic or bicyclic aromatic ring ortricyclic ring optionally containing up to 3 heteroatoms selected from o, n and s, etc. These compounds ...

Compounds that modulate PPAR activity and methods for their preparation.

This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia, hypercholesteremia, obesity, eating disorders, hyperglycemia, atherosclerosis, hypertriglyceridemia, hyperinsulinemia and diabetes in a mammal as well as methods of suppressing appetite.and modulating leptin levels in a mammal. The present invention also discloses methods for making the disclosed compounds.

Benzimidazole compounds

Composition and sythesis of new reagents for inhibition of HIV replication

Compounds that modulate PPAR activity and methods for their preparation

EP4 receptor inhibitors to treat rheumatoid arthritis.

The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin ep4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents

Benzimidazole compounds

Ep-4 receptor inhibitors to treat rheumatoid arthritis.

Heterocyclially substituted benzoylureas, method for their production and their use as medicaments.

Compounds that modulate PPAR activity and methods for their preparation.

Aryl or heteroaryl fused imidazole compounds as anti-inflammatory and analgesic agents.

Method of preparation of isothiocyano-benzazoles.

3Ep4 receptor inhibitors to treat rheumatoid arthritis

Composition and sythesis of new reagents for inhibition of HIV replication

Benzimidazole compounds

3Ep4 receptor inhibitors to treat rheumatoid arthritis

Compounds that modulate PPAR activity and methods for their preparation

Compounds that modulate PPAR activity and methods for their preparation

VERFAHREN ZUR HERSTELLUNG VON NEUEN IMIDAZOLYL- (2) -CARBINOLEN UND IHREN SALZEN

C-LINKING CYCLIC ANTAGONISTS OF THE P2Y1REZEPTORS WITH SUITABILITY WITH THE TREATMENT THROMBOTI SUFFERING

SUBSTITUTED ONES 1H-BENZIMIDAZOL-4-CARBONSÄUREAMIDE ARE EFFECTIVE PARP INHIBITORS

PRODUCTION OF 1,7 (- DIMETHYL-2 (- PROPYL-2,5 (- BI-1H-BENZIMIDAZOL

PROCEDURE FOR the PRODUCTION AND CLEANING OF 1,7 ' - DIMETHYL-2' PROPYL-2,5' BI-1H-BENZIMIDAZOL

CHROMOPHORBESCHICHTETE METALLIC OXIDE PARTICLE

VERFAHREN ZUR HERSTELLUNG VON NEUEN AROMATISCHEN HETEROCYCLISCHEN VERBINDUNGEN

VERFAHREN ZUM HERSTELLEN VON NEUEN BENZIMIDAZOLDERIVATEN UND VON ESTERN UND SALZEN HIEVON

MONOUND BICYCLI AZOLDERIVATE THE INTERACTION OF LIGANDS WITH RISES UP RESTRAINING

REGIOSELEKTIVE, COPPER-CATALYZED SYNTHESIS OF BENZIMIDAZOLEN AND AZABENZIMIDAZOLEN

AZOLOARIN DERIVATIVES, PROCEDURES FOR THEIR PRODUCTION, THESE CONNECTIONS CONTAINING DRUGS AND THEIR USE

SUBSTITUTED 1H-BENZIMIDAZOL-4-CARBOXAMIDE AS POTENT PARP HEMMER

VERRAHREN FOR MANUFACTURING NEW PHENYLAETHYLAMINDERIVATE

PROCEDURE FOR MANUFACTURING NEW BENZIMIDAZOLDERIVATEN AND ESTERS AND SALTS HIEVON

ORGANIC COMPOUND WITH DOUBLE SPIROKONFIGURATION AND ELEKTROLUMINESCENTE DEVICES

ENZYMATIC ANALYSIS USING A SUBSTRATE THAT NIERDERSCHLAG RESULTS IN A FLUORESCENT ONE

BENZIMIDAZOLE, THESE CONNECTIONS CONTAINING DRUGS AND PROCEDURES FOR YOUR PRODUCTION

N-SUBSTITUTING HETEROCYCLEN, PROCEDURE FOR YOUR PRODUCTION, AND IT CONTAINING DRUGS.

2-PHENYLBENZIMIDAZOLE AND 2-PHENYLINDOLE, THEIR PRODUCTION AND APPLICATION

CHINONVERBINDUNGEN FOR THE TREATMENT OF DISEASES

BENZIMIDAZOLDERIVATE

ESTER OF 3-HYDROXY-PIPERIDINMETHANOL-DERIVATEN

PROCEDURE FOR THE PRODUCTION OF 2 - ARYLBENZIMIDAZOLSULFONSÄUREN

OLIGOBENZIMIDAZOLDERIVATE AND YOUR USE AS DNA TRANSFEKTIONSMITTEL

Rocker switch with announcement of the switching positions

Procedure for the production of new Benzimidazoliumverbindungen

ANTITHROMBOTI MEANS

Zweikomponentendiazotypiematerial

BENZOIC ACID DERIVATIVES

PROCESS OF MAKING CHALCOME DERIVATIVES

TRANSCRIPTION FACTOR MODULATING COMPOUNDS AND METHODS OF USE THEREOF

Inhibitors of histone deacetylase

Benzimidazole derivatives, method for the production thereof, their use as FXR agonists and pharmaceutical preparations containing the same

Substituted heterocyclic compounds

Nitrogen-containing heteroaryl derivatives for the treatment of HCV-infection

Nitrogen-containing organic compound, chemically amplified positive resist composition, and patterning process

An aralkylcarbamate of imidazole base is effective as the quencher. In a chemically amplified positive resist composition comprising the carbamate, deprotection reaction of carbamate takes place by reacting with the acid generated upon exposure to high-energy radiation, whereby the composition changes its basicity before and after exposure, resulting in a pattern profile with advantages including high resolution, rectangular shape, and minimized dark-bright difference.

Azole derivatives and fused bicyclic azole derivatives as therapeutic agents

This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, β-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Triarylamine Compound, Light-Emitting Element, Light-Emitting Device, Electronic Device, and Lighting Device

A novel triarylamine compound having a bipolar property is provided. The triarylamine compound can be used for a hole-injection layer, a hole-transport layer, a light-emitting layer, or an electron-transport layer in a light-emitting element. The triarylamine compound can also be used as a host material with a light-emitting material which emits relatively short-wavelength light, in a structure where the host material and the guest material constitute a light-emitting layer. The triarylamine compound of the present invention is a fluorescent compound and therefore can also be used as a light-emitting substance of a light-emitting layer. A light-emitting element having high emission efficiency is provided. A light-emitting device, an electronic device, or a lighting device having low power consumption is provided.

Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use

The invention relates to cyclopentanecarboxamide derivatives of formula 1, to their use as Fatty Acid Synthase inhibitors, to methods for their therapeutic use and to pharmaceutical compositions containing them, wherein R 1 , R 2 , R 3 , LO, W, AR 1 , n are as defined in claim 1 .

Organic light-emitting device, method of manufacturing the same, and flat panel display device including the same

An organic light-emitting device including: a substrate; a first electrode; a second electrode; an emission layer between the first electrode and the second electrode; and an electron transport layer between the emission layer and the second electrode, wherein the emission layer includes a blue emission layer, the electron transport layer includes a unit that includes a first single layer including a first material, a first mixed layer on the first single layer and including the first material and a second material, a second single layer on the first mixed layer and including the second material, a second mixed layer on the second single layer and including the first and second materials, and a third single layer on the second mixed layer and including the first material, wherein the first mixed layer has a thickness that is larger than that of the second mixed layer.

Heterocyclic Compound and Light-Emitting Element, Light-Emitting Device, Lighting Device, and Electronic Device Using the Same

To provide a novel heterocyclic compound having a bipolar property. To improve element characteristics of a light-emitting element by application of the novel heterocyclic compound to the light-emitting element. A heterocyclic compound represented by a general formula (G1) and a light-emitting element formed using the heterocyclic compound represented by the general formula (G1) are provided. When the heterocyclic compound represented by the general formula (G1) is used for the light-emitting element, the characteristics of the light-emitting element can be improved.

2-(2-Hydroxybiphenyl-3-yl)-1H-Benzoimidazole-5-Carboxamidine Derivatives as Factor VIIA Inhibitors

The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.

MANUFACTURE, COMPOSITIONS AND USES OF COAGULATION FACTOR VIIa MODULATOR

Treatment of cancer and thromboembolic disorders using inhibitors of Factor VIIa are disclosed herein using a compound of Formula I:

Mediators of Hedgehog Signaling Pathways, Compositions and Uses Related Thereto

The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. 136.-. (canceled)38. The compound of claim 37 , wherein X—Y—Z includes an amide claim 37 , urea claim 37 , or sulfonamide.39. The compound of claim 37 , wherein Ris optionally substituted with from 1-5 substituents.40. The compound of claim 37 , wherein the substituents on Rare selected from nitro claim 37 , halogen claim 37 , cyano claim 37 , lower alkyl claim 37 , acylamino claim 37 , alkoxy claim 37 , alkylamino claim 37 , a substituted or unsubstituted cycloalkyl claim 37 , heterocyclyl claim 37 , aryl claim 37 , and heteroaryl fused to the aryl or heteroaryl ring.41. The compound of claim 37 , wherein Rrepresents from 1-4 substituents as defined.42. The compound of claim 41 , wherein Rrepresents from 1-4 substituents selected from halogen claim 41 , cyano claim 41 , nitro claim 41 , alkoxy claim 41 , amino claim 41 , acylamino claim 41 , a substituted or unsubstituted cycloalkyl claim 41 , heterocyclyl claim 41 , aryl claim 41 , or heteroaryl fused to G claim 41 , and substituted or unsubstituted lower alkyl.43. The compound of claim 37 , wherein Rrepresents a substituted or unsubstituted benzene ring claim 37 , cyclopentyl ring claim 37 , cyclohexyl ring claim 37 , thiophene ring claim 37 , furan ring claim 37 , isobenzofuran ring claim 37 , pyridine ring claim 37 , benzodioxane ring claim 37 , or benzodioxole ring.44. The compound of claim 37 , wherein Rrepresents a substituted or unsubstituted benzene ring or pyridine ring.46. A pharmaceutical composition comprising one or more compounds according to formulated together with one or more pharmaceutically ...

PROCESS FOR PREPARING BENZOIC ACID ESTERS

There is provided a more industrially advantageous process for preparing novel pyridine derivatives expected to be used as medicines. A process for preparing 3-[(6-hydroxy-1-methyl-1H-benzimidazol-2-yl)methoxy]benzoic acid esters as intermediates with high quality, in short steps and in a high yield, as well as novel benzoic acid esters as their precursors and a process for preparing the same. 2. The preparation process according to claim 1 , wherein A is a methyl group.3. The preparation process according to claim 1 , wherein B is a phenyl group.4. The preparation process according to claim 1 , wherein the solvent is a halogenated hydrocarbon claim 1 , a nitrile claim 1 , an ether or a mixed solvent thereof.5. The preparation process according to claim 1 , wherein the solvent is tetrahydrofuran.6. The preparation process according to claim 1 , wherein the solvent is a halogenated hydrocarbon claim 1 , a nitrile claim 1 , an ether claim 1 , an amide claim 1 , a carboxylate or a mixed solvent thereof.7. The preparation process according to claim 1 , wherein the solvent is N claim 1 ,N-dimethylacetamide.8. The preparation process according to claim 1 , wherein the preparation process proceeds in the presence of a halogenating agent.9. The preparation process according to claim 8 , wherein the halogenating agent is thionyl chloride claim 8 , oxalyl chloride or phosphorus pentachloride.10. The preparation process according to claim 8 , wherein the halogenating agent is thionyl chloride.11. The preparation process according to claim 8 , wherein the compound represented by the general formula (1) and the compound represented by the general formula (2) are previously mixed and the halogenating agent is added thereto.12. The preparation process according to claim 1 , wherein the preparation process proceeds in the presence of a base.13. The preparation process according to claim 12 , wherein the base is an alkali metal hydride.14. The preparation process according to claim ...

NOVEL METHOD OF PREPARING BENZOIMIDAZOLE DERIVATIVES

This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method of preparing a benzoimidazole derivative at high purity and high yield, wherein the benzoimidazole derivative is synthesized using a novel intermediate, namely, benzaldehyde, and thereby the preparation process is simple so that it can be applied to production. 3. The method of or , wherein said palladium catalyst is any one selected from the group consisting of Pd(PPh) , Pd(dba) , PdCl(PPh)and Pd(PtBu).4. The method of or , wherein the step in 1) of or the step 1) of is further performed in the presence of a base.5. The method of claim 4 , wherein the base is an inorganic base or an organic base.6. The method of claim 5 , wherein the inorganic base is any one selected from the group consisting of calcium carbonate claim 5 , sodium carbonate claim 5 , potassium hydroxide claim 5 , sodium hydroxide claim 5 , cesium carbonate claim 5 , potassium tert-butoxide (t-BuOK) and lithium hydroxide.7. The method of claim 5 , wherein the organic base is any one selected from the group consisting of triethylamine claim 5 , tert-butylamine claim 5 , and diisopropylethylamine.8. The method of or claim 5 , wherein the step 1) of or the step 1) of is performed using any one solvent selected from the group consisting of ethanol claim 5 , toluene claim 5 , 1 claim 5 ,2-dimethoxyethane claim 5 , a mixture of water and ethanol claim 5 , a mixture of water and toluene claim 5 , or a mixture of water and 1 claim 5 ,2-dimethoxyethane.9. The method of claim 8 , wherein in the mixture of water and ethanol claim 8 , the mixture of water and toluene claim 8 , and the mixture of water and 1 claim 8 ,2-dimethoxyethane claim 8 , a ratio of water and ethanol claim 8 , water and toluene claim 8 , and water and 1 claim 8 ,2-dimethoxyethane is 100:1 ...

NOVEL NEUROTRYPSIN INHIBITORS

The invention relates to novel acylamino-hydroxy-benzamides of formula (I), wherein Ris phenyl substituted by phenyl, phenoxy, phenylamino or heteroaryl, all optionally further substituted; bicyclic aryl, monocyclic heteroaryl substituted by optionally substituted phenyl, or bicyclic heteroaryl, Ris hydrogen or methyl, and Rand Rhave the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers. 2. The compound according to of formula (I) wherein{'sup': '1', 'sub': 5', '6, 'Ris optionally substituted biphenylyl, phenoxyphenyl or phenylaminophenyl, optionally substituted 1H-benzimidazol-2-yl-phenyl, optionally substituted benzo-C- or C-cycloalkyl or -cycloalkenyl, optionally substituted phenyl-thiophenyl or benzothiophenyl, optionally substituted 1H-benz[d]imidazol-2-yl, optionally substituted indolyl, optionally substituted quinolinyl, or optionally substituted phenyl-1,3-thiazol-2-yl or benzo-1,3-thiazol-2-yl;'}{'sup': '2', 'Ris hydrogen or methyl;'}{'sup': '3', 'Ris alkyl, optionally substituted benzyl, optionally substituted phenylethyl, optionally substituted phenyl; and'}{'sup': '4', 'Ris hydrogen or lower alkyl; or'}{'sup': 3', '4, 'Rand Rtogether with the nitrogen atom, to which they are bound, are optionally substituted pyrrolidino, optionally substituted piperidino, 1,2,3,4-tetrahydro-quinol-1-yl or 1,2,3,4-tetrahydro-isoquinol-2-yl, morpholino, or optionally substituted piperazino.'}3. The compound according to of formula (I) wherein{'sup': '1', 'Ris optionally substituted biphenylyl, phenoxyphenyl or phenylaminophenyl with one to three substituents, wherein the substituents are selected from the group consisting of lower alkyl, hydroxy, lower alkoxy, halo or cyano; 1H-benzimidazol-2-yl-phenyl optionally substituted at nitrogen by methyl or carboxymethyl and at the benzo residue by carboxy, chloro or dichloro; 2-indanyl ...

Nitrogenated heterocyclic derivative, electron-transporting material for organic electroluminescent elements, and organic electroluminescent element using same

A specific nitrogen-containing heterocyclic compound having a urea structure, an electron transporting material containing the nitrogen-containing heterocyclic compound, and an organic electroluminescence device including a light emitting layer and an electron transporting layer between a cathode and an anode in which the electron transporting layer includes the electron transporting material or the nitrogen-containing heterocyclic derivative. An organic EL device exhibiting high emission efficiency even at low voltage and a material for organic EL devices are described.

Benzimidazole derivatives: preparation and pharmaceutical applications

The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).

Hedgehog antagonists having zinc binding moieties

The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.

Novel compound having skin-whitening, anti-oxidizing and ppar activities and medical use therefor

Provided are a novel compound having skin-whitening, anti-oxidizing and PPAR activities and a medical use thereof, and the compound has skin-whitening activities for the suppression of tyrosinase, and accordingly, is useful for use in skin-whitening pharmaceutical composition or cosmetic products; has anti-oxidant activities, and accordingly, is useful for the prevention and treatment of skin-aging; and has PPAR activities, and in particular, PPARα and PPARγ activities, and accordingly, is useful for use in pharmaceutical compositions or health foods which are effective for the prevention and treatment of obesity, metabolic disease, or cardiovascular disease.

MANUFACTURE, COMPOSITIONS AND USES OF COAGULATION FACTOR VIIA MODULATOR

Treatment of cancer and thromboembolic disorders using inhibitors of Factor VIIa are disclosed herein using a compound of Formula I: This application is a continuation of U.S. patent application Ser. No. 13/954,088 filed on Jul. 30, 2013, which is a continuation of U.S. patent application Ser. No. 12/738,372 filed on Jul. 27, 2010, now U.S. Pat. No. 8,552,046 issued on Oct. 8, 2013, which is a National Phase Application of International Application No. PCT/US2008/080221, filed on Oct. 16, 2008, which claims the benefit of U.S. Provisional Application No. 60/980,386, filed Oct. 16, 2007, all of which are incorporated herein by reference.Described herein are compositions and methods for the treatment of proliferative disorders, including cancer, and thromboembolic disorders by inhibiting coagulation Factor VIIa and/or the TF:Factor VIIa complex.The main role of factor VII (FVII) is to initiate the process of coagulation in conjunction with tissue factor (TF). Once bound to TF, FVII is activated to FVIIa.In cancer, the TF-FVIIa complex is found in abundance in pancreatic, gastric, breast, lung, prostate, ovarian, and colon tumors, and triggers a host of physiologic processes that facilitate angiogenesis, tumor growth, and invasion. Inhibitors of Factor VIIa block tumor growth and metastasis, as has been shown in animal models.Described herein are compositions of a compound of Formula I dissolved in water (other pharmaceutically-acceptable organic solvents are optional), in which the compositions have a pH between about 8.0 and 9.5. The pH is optionally obtained by addition of a base and/or a buffer. Additional optional components in the composition are anti-crystallizing agents. Such compositions are in the form of a non-viscous aqueous solution within 15° C. of ambient (or room) temperature, including within 10° C. of room temperature, and including within 5° C. of room temperature. Thus, at or around room temperature, such compositions are readily administrable ...

Process for the preparation of aromatic azole compounds

Aromatic azole compounds such as 2-(4-aminophenyl)-5-amino-benzimidazole are prepared in an organic sulfonic acid solvent instead of polyphosphoric acid. This allows recovery and recycle of the solvent and avoids the handling and environmental concerns resulting from the use of polyphosphoric acid. The resulting compounds find use in the pharmaceutical industry, as anticorrosion agents, and as precursors for high-performance fibers having high strength, stiffness, and flame resistance.

CONDENSED-CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DIODE INCLUDING THE CONDENSED-CYCLIC COMPOUND

A condensed-cyclic compound and an organic light-emitting diode including the condensed-cyclic compound. 2. The compound of claim 1 , wherein A1 is a substituted or unsubstituted pyrrolyl group claim 1 , a substituted or unsubstituted pyrazolyl group claim 1 , a substituted or unsubstituted imidazolyl group claim 1 , a substituted or unsubstituted imidazolinyl group claim 1 , a substituted or unsubstituted imidazopyridinyl group claim 1 , a substituted or unsubstituted imidazopyrimidinyl group claim 1 , a substituted or unsubstituted pyridinyl group claim 1 , a substituted or unsubstituted pyrazinyl group claim 1 , a substituted or unsubstituted pyrimidinyl group claim 1 , a substituted or unsubstituted benzoimidazolyl group claim 1 , a substituted or unsubstituted indolyl group claim 1 , a substituted or unsubstituted purinyl group claim 1 , a substituted or unsubstituted quinolinyl group claim 1 , a substituted or unsubstituted phthalazinyl group claim 1 , a substituted or unsubstituted indolizinyl group claim 1 , a substituted or unsubstituted naphthyridinyl group claim 1 , a substituted or unsubstituted quinazolinyl group claim 1 , a substituted or unsubstituted cinnolinyl group claim 1 , a substituted or unsubstituted indazolyl group claim 1 , a substituted or unsubstituted carbazolyl group claim 1 , a substituted or unsubstituted phenazinyl group claim 1 , a substituted or unsubstituted phenanthridinyl group claim 1 , a substituted or unsubstituted pyranyl group claim 1 , a substituted or unsubstituted chromenyl group claim 1 , a substituted or unsubstituted furanyl group claim 1 , a substituted or unsubstituted benzofuranyl group claim 1 , a substituted or unsubstituted thiophenyl group claim 1 , a substituted or unsubstituted benzothiophenyl group claim 1 , a substituted or unsubstituted isothiazolyl group claim 1 , a substituted or unsubstituted benzoimidazolyl group claim 1 , a substituted or unsubstituted isoxazolyl group claim 1 , a substituted or ...

Prodrugs of dhodh inhibitors and their uses

The invention generally relates to Pro-Drugs of dihydroorotate dehydrogenase (DHODH) inhibitors and methods of use thereof. In certain embodiments, the invention provides a DHODH inhibitor compound including a cleavable functional group that increases bioavailability as compared to a form of the DHODH inhibitor without the functional group, rendering the former more suitable for therapeutic use.

SPIRO-TYPE COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT COMPRISING SAME

The present specification provides a compound having a spiro structure, and an organic light emitting device including the same. 3. The compound of claim 1 , wherein HAr is a substituted or unsubstituted pyridyl group; a substituted or unsubstituted pyrimidyl group; a substituted or unsubstituted triazinyl group; a substituted or unsubstituted furan group; a substituted or unsubstituted thiophene group; a substituted or unsubstituted oxadiazole group; a substituted or unsubstituted thiadiazole group; a substituted or unsubstituted phenanthroline group; a substituted or unsubstituted quinolinyl group; a substituted or unsubstituted isoquinolinyl group; a substituted or unsubstituted quinazoline group; a substituted or unsubstituted benzoxazole group; a substituted or unsubstituted benzothiazole group; a substituted or unsubstituted benzimidazole group; a substituted or unsubstituted phenoxazine group; a substituted or unsubstituted phenothiazine group; a substituted or unsubstituted dibenzofuran group; a substituted or unsubstituted dibenzothiophene group; a substituted or unsubstituted carbazole group; or a substituted or unsubstituted diarylphosphine oxide group.7. An organic light emitting device comprising:a first electrode;a second electrode provided opposite to the first electrode; andone or more organic material layers provided between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein one or more layers of the organic material layers include the compound of .'}8. The organic light emitting device of claim 7 , wherein the organic material layer includes a light emitting layer claim 7 , and the light emitting layer includes the compound.9. The organic light emitting device of claim 8 , wherein the light emitting layer further includes a light emitting dopant.10. The organic light emitting device of claim 7 , wherein the organic material layer includes an electron injection layer claim 7 , an electron transfer ...

PESTICIDALLY ACTIVE SEMI-CARBAZONES AND THIOSEMICARBAZONES DERIVATIVES

Compounds of formula (I), wherein the substituents are as defined in claim 1, and agrochemically acceptable salts and enantiomers thereof, can be used as insecticides. 10. A pesticidal composition claim 1 , which comprises at least one compound of formula I according to claim 1 , where appropriate claim 1 , a tautomer thereof claim 1 , in each case in free form or in agrochemically utilizable salt form claim 1 , as active ingredient and at least one auxiliary.11. A method for controlling pests claim 1 , which comprises applying a compound according to claim 1 , optionally with at least on auxiliary claim 1 , to the pests or their environment with the exception of a method for treatment of the human or animal body by surgery or therapy and diagnostic methods practised on the human or animal body.12. A method for the protection of plant propagation material from the attack by pests claim 10 , which comprises treating the propagation material or the site claim 10 , where the propagation material is planted claim 10 , with a composition according to .13. The pesticidal composition of claim 10 , further including a propagation material claim 10 , wherein the composition is coating the propagation material. The present invention relates to compounds of formula (I) below, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests.Heterocyclic compounds with pesticidal activity are known and described, for example, in WO09/102736, WO11/017505, WO12/109125, WO13/116052, WO13/116053 and WO14/011429. There have now been found novel pesticidal active semi-carbazones and thiosemicarbazones with bicyclic rings substituents.The present invention accordingly relates to compounds of formula I,wherein,wherein indicates that the ring is aromatic or non-aromatic;In one embodiment, the present ...

Amine derivative and an organic electroluminescent device thereof

The present disclosure discloses an amine derivative and an organic electroluminescent device thereof, and relates to a technical field of organic photoelectric materials. The technical problem to be solved by the present disclosure is that the current light extraction material has poor thermal stability and the organic electroluminescent device has short service life. The amine derivative of the present disclosure is a diamine with a bridging group containing a fluorenyl group or a spirofluorenyl group, and the substituent group on N contains at least one benzoxazolyl group, benzothiazolyl group or benzimidazolyl group. The organic electroluminescent device of the present disclosure comprises an anode, an organic layer, a cathode and a light extraction layer, the organic layer is located between the anode and the cathode, and the light extraction layer comprises the amine derivative of Formula I according to the present disclosure. 4. The amine derivative according to claim 3 , wherein Arand Arare the same.10. An organic electroluminescent device claim 1 , comprising an anode claim 1 , an organic layer claim 1 , a cathode and a light extraction layer claim 1 , the organic layer is located between the anode and the cathode claim 1 , the organic layer comprises a hole transport layer claim 1 , a light emitting layer claim 1 , and an electron transport layer claim 1 , with the hole transport layer being located between the anode and the light emitting layer claim 1 , and the electron transport layer being located between the light emitting layer and the cathode claim 1 , the light extraction layer being located on a side of the cathode away from the anode claim 1 , and the light extraction layer contains the amine derivative according to . The application claims the benefit of the earlier filing date of Chinese Patent Application No. 201910631205.2 filed on Jul. 12, 2019 to the China National Intellectual Property Administration, the contents of which are incorporated ...

BLUE FLUORESCENT EMITTERS

The present invention relates to compounds of the formula (I) 8. Use of at least one compound according to in an optoelectronic component from the group comprising: an organic electroluminescent device (OLED) claim 1 , an organic integrated circuit (O-IC) claim 1 , an organic field-effect transistor (O-FET) claim 1 , an organic thin-film transistor (O-TFT) claim 1 , an organic light-emitting transistor (O-LET) claim 1 , an organic solar cell (O-SC) claim 1 , an organic optical detector claim 1 , an organic photoreceptor claim 1 , an organic field-quench device (O-FQD) claim 1 , a light-emitting electrochemical cell (LEC) claim 1 , or an organic laser diode (O-laser).9. An optoelectronic component comprising at least one compound according to . The present application is a national stage entry according to 35 U.S.C. §371 of PCT Application No. PCT/EP2016/052413 filed on Feb. 4, 2016, which claims priority to German Patent Application No. 10 2015 101 767.9, filed on Feb. 6, 2015; both of which are herein incorporated by reference in their entirety.The subject matter herein generally provides compounds of formula (I) as defined herein, as well as their use as emitter or carrier material in an optoelectronic component.The development of novel functional compounds for use in electronic devices is currently the subject of intensive research. The aim here is the development and study of compounds which have not been used to date in electronic devices, and the development of compounds which enable an improved profile of properties of the devices.According to a non-limiting embodiment, the term “optoelectronic component” is understood to mean inter alia organic integrated circuits (OICs), organic field-effect transistors (OFETs), organic thin-film transistors (OTFTs), organic light-emitting transistors (OLETs), organic solar cells (OSCs), organic optical detectors, organic photoreceptors, organic field-quench devices (OFQDs), organic light-emitting electrochemical cells ( ...

POLY(PHENYLENE) AND M-TERPHENYL AS PROTECTING GROUPS FOR BENZIMIDAZOLIUM HYDROXIDES

The present disclosure provides alkaline-stable m-terphenyl benzimidazolium hydroxide compounds, in which the C2-position is attached to a phenyl group having various substituents at the ortho positions. Polymers incorporating m-terphenylene repeating groups derived from these alkaline-stable benzimidazolium hydroxide compounds are also presented, along with their inclusion in ionic membranes and in electrochemical devices. 2. The compound of claim 1 , wherein Rand Rare each independently selected from alkyl claim 1 , perfluoroalkyl claim 1 , and heteroalkyl.35-. (canceled)6. The compound of claim 1 , wherein Rand Rare each methyl.711-. (canceled)12. The compound of claim 1 , wherein Rand Rare each independently selected from methyl and phenyl claim 1 , wherein said phenyl is optionally substituted with 1 claim 1 , 2 claim 1 , 3 claim 1 , or 4 halo.13. The compound of claim 1 , wherein Ris selected from hydrogen claim 1 , alkyl claim 1 , perfluoroalkyl claim 1 , heteroalkyl claim 1 , aryl claim 1 , and heteroaryl.14. (canceled)15. (canceled)16. The compound of claim 1 , wherein Ris selected from hydrogen and methyl.17. (canceled)18. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each hydrogen.19. The compound of claim 1 , further comprising an anion X selected from iodide claim 1 , bromide claim 1 , chloride claim 1 , fluoride claim 1 , triiodide claim 1 , hydroxide claim 1 , carbonate claim 1 , bicarbonate claim 1 , cyanide claim 1 , acetate claim 1 , nitrate claim 1 , sulfate claim 1 , phosphate claim 1 , triflate claim 1 , tosylate claim 1 , tetrakis(3 claim 1 ,5-bis(trifluoromethyl)phenyl)borate claim 1 , bis(trifluoromethane)sulfonamide claim 1 , and any combination thereof claim 1 , wherein the anion X counterbalances the positive charge in the compound.21. A polymer comprising a repeating unit derived from a compound of .23. The polymer of claim 22 , wherein R claim 22 , R claim 22 , and Rare each independently selected from ...

MULTI-TIERED, HIGH THROUGH-PUT SCREEN FOR COMPOUNDS EFFECTIVE AGAINST BACTERIAL BIOFILM COMPOUNDS EFFECTIVE FOR INHIBITING AND ERADICATING BACTERIAL BIOFILM

A high through-put screening method for identifying agents effective for inhibiting biofilm formation and/or killing established biofilm are disclosed. The method includes three tiers, and each tier includes three specific biological process assays. The tier levels are a primary screen, a confirmation screen, and a dose-response screen, and the biological process assays include as says for total bacterial growth, bacterial metabolic activity, and biofilm formation. 1. A high through-put screening method for identifying agents from a library of compounds , said agents effective for inhibiting biofilm formation and/or killing established biofilm , the method comprising: (A) primary screen,', '(B) confirmation screen,', '(C) dose-response screen;, 'conducting three tiers of three assays; the tiers comprising'} (a) total bacterial growth assay', '(b) bacterial metabolic activity assay', '(c) biofilm formation assay,, 'the assays comprising'}wherein the library of compounds is subject to tier A and only compounds meeting a primary parameter advance to tier B, and only tier B compounds meeting a confirmation parameter advance to tier C, and only tier C compounds meeting a dose-response parameter are identified as putative agents effective for inhibiting and/or eradicating a biofilm, further wherein the assays are conducted for each compound subject to the respective tier.2. The high through-put screening method according to claim 1 , wherein the total bacterial growth assay according to (a) comprises optical density measurement claim 1 , the bacterial metabolic activity assay according to (b) comprises resazurin indicator claim 1 , and the biofilm formation assay according to (c) comprises crystal violet staining claim 1 , each assay being conducted in the presence of a concentration of a compound subject to a tier.3. The high through-put screening method according to claim 2 , wherein the primary parameter is one of ≧80% inhibition in (a) claim 2 , ≧80% inhibition in (b) ...

AMINE-BASED COMPOUND AND ORGANIC LIGHT-EMITTING DIODE INCLUDING THE SAME

An amine-based compound and an organic light-emitting diode including the amine-based compound. 2. The amine-based compound of claim 1 , wherein the at least one electron withdrawing group is selected from the group consisting of: —F; —CN; —NO; a C-Calkyl group substituted with at least one —F; a C-Cheteroaryl group including a ring-forming N atom; and a C-Cheteroaryl group that includes a ring-forming N atom and is substituted with at least one of a deuterium atom claim 1 , —F claim 1 , —Cl claim 1 , —Br claim 1 , —I claim 1 , —CN claim 1 , a hydroxyl group claim 1 , —NO claim 1 , an amino group claim 1 , an amidino group claim 1 , hydrazine claim 1 , hydrazone claim 1 , a carboxyl group or a salt thereof claim 1 , a sulfonic acid group or a salt thereof claim 1 , phosphoric acid or a salt thereof claim 1 , a C-Calkyl group claim 1 , a C-Calkyl group substituted with at least one —F claim 1 , a C-Calkoxy group claim 1 , a C-Caryl group claim 1 , and a C-Cheteroaryl group.3. The amine-based compound of claim 1 , wherein the at least one electron withdrawing group is selected from the group consisting of —F; —CN; a C-Calkyl group substituted with at least one —F; a pyrrolyl group claim 1 , a pyrazolyl group claim 1 , an imidazolyl group claim 1 , an imidazolinyl group claim 1 , an imidazopyridinyl group claim 1 , an imidazopyrimidinyl group claim 1 , a pyridinyl group claim 1 , a pyrazinyl group claim 1 , a pyrimidinyl group claim 1 , a benzoimidazolyl group claim 1 , an indolyl group claim 1 , a purinyl group claim 1 , a quinolinyl group claim 1 , an isoquinolinyl group claim 1 , a phthalazinyl group claim 1 , an indolizinyl group claim 1 , a quinazolinyl group claim 1 , a cinnolinyl group claim 1 , an indazolyl group claim 1 , a carbazolyl group claim 1 , a phenazinyl group claim 1 , a phenanthridinyl group claim 1 , a triazinyl group claim 1 , a pyridazinyl group claim 1 , a triazoly group claim 1 , and a tetrazoly; and a pyrrolyl group claim 1 , a pyrazolyl group ...

BINDING FUNCTION 3 (BF3) SITE COMPOUNDS AS THERAPEUTICS AND METHODS FOR THEIR USE

This invention provides compound having a structure of Formulas: 120-. (canceled)281. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to claim and a pharmaceutically acceptable excipient.29. A pharmaceutical composition comprising a compound or pharmaceutically acceptable salt thereof according to and a pharmaceutically acceptable excipient.301. A method of modulating AR activity claim 27 , the method comprising (a) administering a compound of claim to a subject in need thereof.31. The method of claim 30 , wherein the modulating AR activity is for the treatment of at least one indication selected from the group consisting of: AR-mediated cancer claim 30 , prostate cancer claim 30 , breast cancer claim 30 , ovarian cancer claim 30 , endometrial cancer claim 30 , bladder cancer claim 30 , Taxene resistant triple negative breast cancer claim 30 , hair loss claim 30 , acne claim 30 , hirsutism claim 30 , ovarian cysts claim 30 , polycystic ovary disease claim 30 , precocious puberty claim 30 , and age-related macular degeneration.32. The method of claim 31 , wherein the modulating AR activity is for the treatment of prostate cancer.33. The method of claim 31 , wherein the modulating AR activity is for the treatment of Taxene resistant triple negative breast cancer.34. The method of claim 31 , wherein the modulating AR activity is for the treatment of ovarian cancer.35. The method of claim 31 , wherein the modulating AR activity is for the treatment of endometrial cancer. This application is a continuation of U.S. application Ser. No. 16/426,406, filed May 30, 2019, which is a divisional application of U.S. application Ser. No. 15/302,363, filed Oct. 6, 2016, now U.S. Pat. No. 10,351,527, which is a National Stage Application of International Patent Application No. PCT/CA2015/000239, filed Apr. 9, 2015; which claims the benefit of U.S. Provisional Patent Application Ser. No. 61/977,445, filed Apr. 9, 2014 and U.S. ...

ANTHRACENE DERIVATIVES CONTAINING BENZIMIDAZOLE OR BORATE AND ORGANOELECTROLUMINESCENT DEVICE INCLUDING THE SAME

An organic light-emitting diode comprises a first electrode layer, a second electrode layer, and an organic luminescent unit disposed between the first electrode layer and the second electrode layer. The organic luminescent unit has an organic electroluminescent material containing anthracene group as shown in General Formula (1): 2. The organic light-emitting diode according to claim 1 , wherein the alkyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 alkyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 alkyl group claim 1 , the cycloalkyl group is a substituted or unsubstituted C3˜C6 cycloalkyl group claim 1 , the alkoxy group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 alkoxy group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 alkoxy group claim 1 , the haloalkyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 haloalkyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 haloalkyl group claim 1 , the thioalkyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 thioalkyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 thioalkyl group claim 1 , the silyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C1˜C6 silyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 silyl group claim 1 , and the alkenyl group is selected from the group consisting of a substituted or unsubstituted straight-chain C2˜C6 alkenyl group claim 1 , and a substituted or unsubstituted branched-chain C3˜C6 alkenyl group.4. The organic light-emitting diode of claim 1 , wherein the organic luminescent unit comprises an organic luminescent layer.5. The organic light-emitting diode of claim 4 , wherein the organic luminescent unit further comprises a ...

BINDING FUNCTION 3 (BF3) SITE COMPOUNDS AS THERAPEUTICS AND METHODS FOR THEIR USE

This invention provides compound having a structure of Formulas: Uses of such compounds for treatment of various indications, including prostate cancer as well as methods of treatment involving such compounds are also provide. 2. The compound of claim 1 , wherein the compound is selected from one or more of the compounds in TABLE 2.7. The compound of any one of - claim 1 , for use in the treatment of at least one indication selected from the group consisting of: cancer claim 1 , hair loss claim 1 , acne claim 1 , hirsutism claim 1 , ovarian cysts claim 1 , polycystic ovary disease claim 1 , precocious puberty claim 1 , and age related macular degeneration.8. A pharmaceutical composition for modulating AR activity claim 1 , the composition comprising a compound of any one of - claim 1 , and a pharmaceutically acceptable carrier.9. The compound of any one of - claim 1 , for the treatment of at least one indication selected from the group consisting of: AR-mediated cancer claim 1 , prostate cancer claim 1 , breast cancer claim 1 , ovarian cancer claim 1 , endometrial cancer claim 1 , bladder cancer claim 1 , Taxene resistant triple negative breast cancer claim 1 , hair loss claim 1 , acne claim 1 , hirsutism claim 1 , ovarian cysts claim 1 , polycystic ovary disease claim 1 , precocious puberty claim 1 , and age-related macular degeneration.10. A method of modulating AR activity claim 1 , the method comprising (a) administering a compound of any one of - or a pharmaceutical composition of to a subject in need thereof.11. The method of claim 10 , wherein the modulating AR activity is for the treatment of at least one indication selected from the group consisting of: AR-mediated cancer claim 10 , prostate cancer claim 10 , breast cancer claim 10 , ovarian cancer claim 10 , endometrial cancer claim 10 , bladder cancer claim 10 , Taxene resistant triple negative breast cancer claim 10 , hair loss claim 10 , acne claim 10 , hirsutism claim 10 , ovarian cysts claim 10 , ...

2-(Het)aryl-substituted fused heterocycle derivatives as pesticides

The invention relates to novel compounds of the formula (I) 4. The compound of formula (I) according to wherein{'sup': 1', '4, 'Arepresents nitrogen or ═C—R,'}{'sup': '1', 'Rrepresents methyl, ethyl, n-propyl, isopropyl, cyclopropyl, n-butyl, isobutyl, tert-butyl, cyclobutyl, fluoromethyl, difluoromethyl, trifluoromethyl, fluoroethyl, difluoroethyl, trifluoroethyl, tetrafluoroethyl or pentafluoroethyl,'}{'sup': '2', 'Rrepresents a group selected from G1, G2, G3, G4 G10, G11, G12, G13, G14, G15, G18 or G19,'}{'sup': '3', 'sub': 1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'Rrepresents hydrogen, cyano, halogen, (C-C)alkyl, (C-C)haloalkyl, (C-C)haloalkoxy, (C-C)alkylthio, (C-C)alkylsulphinyl, (C-C)alkylsulphonyl, (C-C)haloalkylthio, (C-C)haloalkylsulphinyl, (C-C)haloalkylsulphonyl or NHCO—(C-C)alkyl ((C-C)alkylcarbonylamino),'}{'sup': '4', 'Rrepresents hydrogen, fluorine, chlorine, bromine or cyano,'}X represents a heteroaromatic 9-membered or 12-membered fused bicyclic or tricyclic ring system from the series H1, H2, H3, H4, H5, H7, H8, H10, H11, H12, H13, H15, H16, H17, H18, H19, or H20,{'sup': '5', 'sub': 1', '4', '1', '4', '2', '4', '2', '4', '2', '4', '2', '4', '3', '6', '3', '6', '3', '6', '1', '4', '3', '6', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4', '1', '4, 'Rrepresents hydrogen, cyano, halogen, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkenyl, (C-C)haloalkenyl, (C-C)alkynyl, (C-C)haloalkynyl, (C-C)cycloalkyl, (C-C)cycloalkyl-(C-C)cycloalkyl, (C-C)alkyl-(C-C)cycloalkyl, (C-C)alkoxy, (C-C)haloalkoxy, (C-C)alkoxyimino, (C-C)alkylthio, (C-C)haloalkylthio, (C-C)alkylsulphinyl, (C-C)haloalkylsulphinyl, (C-C)alkylsulphonyl, (C-C)haloalkylsulphonyl, (C-C)alkylcarbonyl, (C-C)haloalkylcarbonyl, (C-C)alkylaminocarbonyl, di-(C-C)alkylaminocarbonyl, (C-C)alkylsulphonylamino (C-C)alkylaminosulphonyl or di-(C-C) ...

BENZIMIDAZOLE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS

The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor, more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders. 12. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of or .13. A pharmaceutical composition made by mixing a compound of or and a pharmaceutically acceptable carrier.14. A process for making a pharmaceutical composition comprising mixing a compound of or and a pharmaceutically acceptable carrier.15. A method of treating a disorder mediated by the CB-1 receptor , comprising administering to a subject in need thereof a therapeutically effective amount of the compound of or .16. The method of claim 15 , wherein the disorder mediated by the CB-1 receptor is selected from the group consisting of obesity claim 15 , Type I diabetes claim 15 , Type II diabetes claim 15 , gestational diabetes claim 15 , latent autoimmune diabetes of adults (LADA) claim 15 , pre-diabetes claim 15 , insulin resistance claim 15 , inadequate glucose tolerance claim 15 , dyslipidemias (including claim 15 , but not limited to elevated triglycerides and LDL claim 15 , and low HDL) claim 15 , nonalcoholic steatohepatitis (NASH) claim 15 , cirrhosis claim 15 , fatty liver disease claim 15 , atherosclerosis claim 15 , hypertension claim 15 , inflammatory bowel disease claim 15 , Alzheimer's disease claim 15 , osteoporosis claim 15 , multiple sclerosis claim 15 , traumatic brain injury claim 15 , arthritis claim 15 , and neuropathic pain.17. A method of treating a disorder selected from the group consisting of obesity claim 12 , Type I diabetes claim 12 , Type II diabetes claim 12 , gestational diabetes claim 12 , latent autoimmune ...

Heterocyclic compound and organic light-emitting device including the same

A heterocyclic compound of Formula 1 below and an organic light-emitting device including the same are provided. X 1 to X 4 , L 1 , L 2 , n, m, and Ar 1 to, Ar 4 in Formula 1 are defined as in the specification.

NOVEL FUSED POLYCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING ELEMENT INCLUDING THE SAME

The present invention provides a novel fused polycyclic compound suitably used for a blue light emitting element and an organic light emitting element including the fused polycyclic compound. 2. The fused polycyclic compound according to claim 1 ,{'sub': 1', '10', '11', '20, 'wherein at least two of R, R, R, and Rare independently selected from the group consisting of a cyano group, a substituted or an unsubstituted alkyl group, a substituted or an unsubstituted aryl group, and a substituted or an unsubstituted heterocyclic group.'}3. The fused polycyclic compound according to claim 1 ,{'sub': 1', '10', '11', '20, 'wherein at least two of R, R, R, and Reach represent an electron withdrawing substituent.'}4. The fused polycyclic compound according to claim 3 ,wherein the electron withdrawing substituent is a phenyl group, a pyridyl group, a quinolinyl group, or an isoquinolinyl group, andthe phenyl group has a halogen atom, a halogenated alkyl group, a cyano group, or a benzimidazole group.5. The fused polycyclic compound according to claim 2 ,{'sub': 1', '10', '11', '20, 'wherein two of R, R, R, and Reach represent a hydrogen atom.'}6. The fused polycyclic compound according to claim 2 ,{'sub': 1', '10', '11', '20, 'wherein Rand Ror Rand Reach represent a hydrogen atom.'}7. The fused polycyclic compound according to claim 1 ,wherein the fused polycyclic compound emits blue light.8. An organic light emitting element comprising:a pair of electrodes; andan organic compound layer provided between the electrodes,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the organic compound layer contain the fused polycyclic compound according to .'}9. The organic light emitting element according to claim 8 ,wherein the organic compound layer includes a light emitting layer containing a host and a guest, andthe guest includes the fused polycyclic compound.10. The organic light emitting element according to claim 8 ,wherein the organic light emitting element emits blue ...

AMIDE DERIVATIVES AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, PREPARATION METHOD THEREOF AND MEDICINAL APPLICATION THEREOF

Amide derivatives and pharmaceutically acceptable salts thereof, preparation method thereof and medicinal application thereof are provided. Specifically, amide derivatives represented by general formula (I) are provided. The amide derivatives represented by general formula (I) can be used as a therapeutic agent, particularly as an inhibitor for microsomal prostaglandin E synthase-1 (mPGES-1), and also to treat and/or prevent diseases or illnesses such as inflammation and/or pain etc. The definition of each substituent group in general formula (I) is the same as the definition in the description. 6. The compound of formula (I) claim 1 , or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or pharmaceutically acceptable salt thereof according to claim 1 , wherein A claim 1 , B and Y are —CH—.7. The compound of formula (I) claim 1 , or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or pharmaceutically acceptable salt thereof according to claim 1 , wherein one of A claim 1 , B and Y is N claim 1 , the other two are —CH—.9. The compound of formula (I) claim 1 , or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris selected from the group consisting of alkyl and haloalkyl.15. A pharmaceutical composition comprising a therapeutically effective amount of the compound of formula (I) claim 1 , or the tautomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or pharmaceutically acceptable salt thereof according to claim 1 , and a pharmaceutically acceptable carrier claim 1 , diluent or excipient.1618.-. (canceled)19. The compound of formula (I) claim 1 , or the tautomer claim 1 , ...

FUSED AZOLE DERIVATIVE

The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia. Specifically, the invention provides fused azole derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof that have an antagonistic action against the arginine-vasopressin 1b receptor: 3. The fused azole derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein in Formula (I) claim 1 ,{'sup': '1', 'sub': '1-5', 'Ris Calkyl;'}{'sup': '2', 'sub': '1-5', 'Rrepresents aryl or heteroaryl (the aryl and heteroaryl are optionally substituted by one or two groups selected from the group consisting of Calkoxy and halogen atoms);'}{'sup': 4', '5, 'sub': '1-5', 'Rand Rwhich may be the same or different are each Calkyl; or'}{'sup': 4', '5, 'sub': 1-5', '1-5, 'Rand R, together with the adjoining nitrogen atom, may form a 4- to 8-membered saturated heterocycle optionally containing one or more oxygen atoms in the ring in addition to the adjoining nitrogen atom (the 4- to 8-membered saturated heterocycle is optionally substituted by one or two groups selected from the group consisting of hydroxy and Calkyl, and the 4- to 8-membered saturated heterocycle optionally has a Calkylene group crosslinking two different carbon atoms in the ring), 2-oxa-6-azaspiro[3.3]hept-6-yl, or 2-oxa-7-azaspiro[3.5]non-7-yl;'}{'sup': '6', 'sub': '3-7', 'Ris Ccycloalkyl.'}4. The fused azole derivative or a pharmaceutically acceptable salt thereof according to claim 1 , wherein in Formula (I) claim 1 ,{'sup': '2', 'sub': '1-5', 'Ris phenyl or pyridyl (the phenyl and pyridyl are optionally substituted by one or two groups selected from the group consisting ...

SYNTHETIC BUILDING BLOCKS FOR THE PRODUCTION OF MATERIALS FOR ORGANIC ELECTROLUMINESCENCE DEVICES

The present invention relates to compounds which are suitable as synthesis precursors for the production of electronically active materials for use in organic electroluminescence devices. 113.-. (canceled)15. The compound according to claim 14 , wherein n=0 claim 14 , 1 claim 14 , 2 or 3.16. The compound according to claim 14 , wherein n=0 claim 14 , 1 or 2.17. The compound according to claim 14 , wherein L stands for a single bond claim 14 , NR claim 14 , BR claim 14 , P(═O)R claim 14 , a straight-chain alkylene or alkylidene group having 1 to 10 C atoms or a branched or cyclic alkylene or alkylidene group having 3 to 10 C atoms claim 14 , which may be substituted by in each case substituted by one or more radicals R claim 14 , where one or more non-adjacent CHgroups may be replaced by —RC═CR— claim 14 , —C≡C— claim 14 , Si(R) claim 14 , C═O claim 14 , —O— claim 14 , —S— or —CONR— and where one or more H atoms may be replaced by D or F claim 14 , or an aromatic or heteroaromatic ring system having 5 to 24 aromatic ring atoms claim 14 , which may be substituted by one or more radicals R.20. The compound according to claim 14 , wherein R is selected on each occurrence claim 14 , identically or differently claim 14 , from the group consisting of H claim 14 , NAr claim 14 , C(═O)Ar claim 14 , C(═O)R claim 14 , P(═O)Ar claim 14 , PAr claim 14 , Si(R) claim 14 , a straight-chain alkyl group having 1 to 10 C atoms or a branched or cyclic alkyl group having 3 to 10 C atoms or an alkenyl group having 2 to 10 C atoms claim 14 , each of which may be substituted by one or more radicals R claim 14 , where in each case one or more non-adjacent CHgroups may be replaced by RC═CRor O and where one or more H atoms may be replaced by F claim 14 , an aromatic or heteroaromatic ring system having 5 to 40 aromatic ring atoms claim 14 , which may in each case be substituted by one or more radicals R; two or more adjacent substituents R here may optionally form a monocyclic or polycyclic ...

LIGHT-EMITTING DEVICE AND METHOD FOR PRODUCING SAME

Provided is a light-emitting device including an anode, a light-emitting layer, an electron-transporting layer and a cathode. The electron-transporting layer contains at least one electron-transporting material whose LUMO level is −3.0 eV or more and at least one dopant material selected from the group consisting of a heterocyclic compound whose SOMO level is −2.2 to −1.5 eV and a derivative thereof. The LUMO level of the electron-transporting material is smaller than the SOMO level of the heterocyclic compound. 1. A light-emitting device comprising an anode , a light-emitting layer , an electron-transporting layer and a cathode ,the electron-transporting layer containing at least one electron-transporting material whose LUMO level is −3.0 eV or more and at least one dopant material selected from the group consisting of a heterocyclic compound whose SOMO level is −2.2 to −1.5 eV and a derivative thereof, whereinthe LUMO level of the electron-transporting material is smaller than the SOMO level of the heterocyclic compound.2. The light-emitting device according to claim 1 , wherein the electron-transporting layer and the cathode are adjacent.3. The light-emitting device according to or claim 1 , wherein a content of the dopant material in the electron-transporting layer is 1 to 50 parts by mass with respect to 100 parts by mass of the electron-transporting material.4. The light-emitting device according to any one of to claim 1 , wherein the light-emitting layer comprises a phosphorescent material.9. A method for producing an electron-transporting layer claim 1 , comprisinga step of doping an electron-transporting material whose LUMO level is −3.0 eV or more with a heterocyclic compound whose SOMO level is −2.2 to −1.5 eV, whereinthe LUMO level of the electron-transporting material is smaller than the SOMO level of the heterocyclic compound.10. A method for producing a light-emitting device having an anode claim 1 , a light-emitting layer claim 1 , an electron- ...

FULLERENE DERIVATIVE, ORGANIC SOLAR CELL USING SAME, AND MANUFACTURING METHOD THEREOF

The present specification relates to a fullerene derivative, an organic solar cell including the same, and a fabricating method thereof. 3. The fullerene derivative of claim 1 , wherein m is 0.4. The fullerene derivative of claim 1 , wherein m is 1.5. The fullerene derivative of claim 1 , wherein at least one of the substituents of the hydrocarbon ring formed by the adjacent substituents of R1 to R10; and R5 to R8 is -(L)a-(M)b.6. The fullerene derivative of claim 1 , wherein a is an integer of 0 or 1; andL is a substituted or unsubstituted alkylene group having 1 to 4 carbon atoms; or a substituted or unsubstituted phenylene group.7. The fullerene derivative of claim 1 , wherein R is a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms; a substituted or unsubstituted alkoxy group having 1 to 20 carbon atoms; a substituted or unsubstituted cycloalkyl group having 3 to 60 carbon atoms; a substituted or unsubstituted cycloalkoxy group having 3 to 60 carbon atoms; a substituted or unsubstituted arylalkoxy group having 7 to 50 carbon atoms; a substituted or unsubstituted aryl group having 6 to 60 carbon atoms; a substituted or unsubstituted aryloxy group having 6 to 60 carbon atoms; a substituted or unsubstituted heteroaryl group having 2 to 60 carbon atoms claim 1 , which includes one or more of N claim 1 , O and S atoms; or a substituted or unsubstituted heteroaryloxy group having 2 to 60 carbon atoms claim 1 , which includes one or more of N claim 1 , O and S atoms.8. The fullerene derivative of claim 1 , wherein R is a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms; a substituted or unsubstituted alkoxy group having 1 to 20 carbon atoms; a substituted or unsubstituted arylalkoxy group having 7 to 50 carbon atoms; a substituted or unsubstituted aryl group having 6 to 60 carbon atoms; or a substituted or unsubstituted heteroaryloxy group having 2 to 60 carbon atoms claim 1 , which includes one or more of N claim 1 , O and S ...

METHOD FOR PREVENTING AND/OR TREATING AGING-ASSOCIATED COGNITIVE IMPAIRMENT AND NEUROINFLAMMATION

The present invention is directed to a method for preventing and/or treating aging-related cognitive impairment in the central nervous system. The method comprises administering to a subject in need thereof a Ppargc1a activator 2-(4-tert-butylphenyl)-1H-benzimidazole, 2-[4-(1,1-dimethylethyl)phenyl]-1H-benzimidazole, in an effective amount. A preferred route of administration is oral administration. 1. A method of suppressing neuroinflammation or systemic inflammation and metabolic abnormalities of microglia in the brain comprising the step of:administering to a subject in need thereof an effective mount of a compound 2-[4-(1,1-dimethylethyl)phenyl]-1H-benzimidazole, or a pharmaceutically acceptable salt thereof.2. The method according to claim 1 , wherein said method reverses or alleviates cognitive behavioral dysfunction of the subject.3. The method according to claim 1 , wherein said method suppresses neuroinflammation and/or systemic inflammation of the subject.4. The method according to claim 1 , wherein said method suppresses metabolic abnormalities of microglia in the brain of the subject.5. The method according to claim 1 , wherein said compound is administered by systemic administration.6. The method according to claim 1 , wherein said compound is administered by oral administration. The present invention relates to methods for preventing and/or treating aging-associated cognitive impairment and neuroinflammation by administering to a subject a Ppargc1a activator 2-(4-tert-butylphenyl)-1H-benzimidazole, 2-[4-(1,1-dimethylethyl)phenyl]-1H-benzimidazole.Microglia are immune cells that are located only in the CNS. Microglia originate from a yolk-sac hematopoietic progenitor, which populates the brain during embryogenesis (Ginhoux et al Science 2009). During homeostatic conditions, microglia carry out reparative processes such as debris clearance. They also produce an arsenal of inflammatory mediators, which could be released upon receiving pathological stimuli ...

BENZIMIDAZOLE DERIVATIVES USEFUL AS CB-1 INVERSE AGONISTS

The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders. 12. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of or .13. A pharmaceutical composition made by mixing a compound of or and a pharmaceutically acceptable carrier.14. A process for making a pharmaceutical composition comprising mixing a compound of or and a pharmaceutically acceptable carrier.15. A method of treating a disorder mediated by the CB-1 receptor , comprising administering to a subject in need thereof a therapeutically effective amount of the compound of or .16. The method of claim 15 , wherein the disorder mediated by the CB-1 receptor is selected from the group consisting of obesity claim 15 , Type I diabetes claim 15 , Type II diabetes claim 15 , gestational diabetes claim 15 , latent autoimmune diabetes of adults (LADA) claim 15 , pre-diabetes claim 15 , insulin resistance claim 15 , inadequate glucose tolerance claim 15 , dyslipidemias (including claim 15 , but not limited to elevated triglycerides and LDL claim 15 , and low HDL) claim 15 , nonalcoholic steatohepatitis (NASH) claim 15 , cirrhosis claim 15 , fatty liver disease claim 15 , atherosclerosis claim 15 , hypertension claim 15 , inflammatory bowel disease claim 15 , Alzheimer's disease claim 15 , osteoporosis claim 15 , multiple sclerosis claim 15 , traumatic brain injury claim 15 , arthritis claim 15 , and neuropathic pain.17. A method of treating a disorder selected from the group consisting of obesity claim 12 , Type I diabetes claim 12 , Type II diabetes claim 12 , gestational diabetes claim 12 , latent autoimmune ...

COMPOUNDS FOR TREATMENT OF CANCER

The present invention relates to colchicine-binding site compounds having anti-cancer activity, compositions comprising the same, and their use for treating various forms of cancer. 4. The compound of claim 1 , wherein Z is CH.5. The compound of claim 1 , wherein Z is N.6. The compound of claim 1 , wherein Ris OCH claim 1 , n is 3 and Ris hydrogen.9. A pharmaceutical composition comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and at least one pharmaceutically acceptable carrier.10. The pharmaceutical composition of claim 9 , further comprising at least one pharmaceutically active compound useful in the treatment of cancer.11. A method of treating claim 1 , suppressing claim 1 , reducing the severity claim 1 , reducing the risk claim 1 , or inhibiting cancer comprising administering a compound of to a subject having cancer under conditions effective to treat the cancer.12. The method of claim 11 , wherein said cancer is selected from the group consisting of prostate cancer claim 11 , drug-resistant prostate cancer claim 11 , breast cancer claim 11 , drug-resistant breast cancer claim 11 , ovarian cancer claim 11 , drug-resistant ovarian cancer claim 11 , skin cancer claim 11 , melanoma claim 11 , drug-resistant melanoma claim 11 , lung cancer claim 11 , colon cancer claim 11 , glioma claim 11 , leukemia claim 11 , lymphoma claim 11 , renal cancer claim 11 , CNS cancer claim 11 , uterine cancer claim 11 , drug-resistant uterine cancer claim 11 , and combinations thereof.13. The method of claim 11 , wherein said cancer is melanoma.14. The method of claim 11 , wherein said cancer is metastatic melanoma.15. The method of claim 11 , wherein said cancer is prostate cancer.16. The method of claim 15 , wherein said prostate cancer is drug-resistant prostate cancer.17. The method of claim 11 , wherein said administering is carried out in combination with another cancer therapy.18. A method of treating a drug resistant tumor ...

Chemical modulators of immune checkpoints and therapeutic use

Compounds and pharmaceutical compositions that down-regulate immune checkpoints such as PD-1, PD-L1 and CTLA-4 are provided. Also provided are methods of treating a disease by down-regulating immune checkpoints such as PD-1, PD-L1 and CTLA-4. The methods are useful for treating cancer and viral infection in a subject.

TREATMENT OF ACANTHAMOEBA OR BALAMUTHIA TROPHOZOITES AND/OR CYSTS

Compounds, compositions, and methods for the treatment of infections caused by or trophozoites and/or cysts and for the disinfection of solids and/or liquids, such as medical and personal care items, for example contact lenses, that may harbor trophozoites and/or cysts are provided. 2. The compound of claim 1 , wherein one of Rand Ris a halogen.3. The compound of claim 1 , wherein two of Rand R claim 1 , R claim 1 , Rand Rare selected from a halogen.4. The compound of claim 1 , wherein two of R claim 1 , R claim 1 , R claim 1 , Rand Rare selected from a halogen.5. The compound claim 1 , wherein one of R claim 1 , R claim 1 , R claim 1 , and Ris selected from C-Calkoxy.6. The compound of claim 1 , wherein Rand Rare isopropyl.14. The compound of claim 13 , wherein Ris independently at each occurrence selected from hydrogen claim 13 , C-Calkyl claim 13 , and C-Ccycloalkyl.17. A pharmaceutical composition comprising a compound of or a pharmaceutically acceptable salt thereof claim 1 , optionally in a pharmaceutically acceptable carrier.18Acanthamoeba. A method for the treatment of an eye infection caused by one gr more species in a host in need thereof comprising administering an effective amount of a compound of claim 1 , optionally in a pharmaceutically acceptable carrier.19Acanthamoeba. A method for the disinfection of one or more species from a solid claim 1 , liquid or gel object comprising administering an effective amount of a compound of claim 1 , optionally in a pharmaceutically acceptable carrier.20. The method of claim 19 , wherein the object is selected from an application claim 19 , a dressing claim 19 , contact lens claim 19 , an optical implant claim 19 , a contact lens solution claim 19 , an ocular solution and rewetting eye drops.21Acanthamoeba. The method of wherein the eye infection is keratitis.22. The method of claim 18 , further comprising administering an effective amount of an additional therapeutic agent selected from alexidine claim 18 , ...

Novel Therapeutic Agents

The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases. 2. The compound according to or an N-oxide thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , polymorph or tautomer thereof claim 1 , wherein p is 1 and q is 2; or p is 2 and q is 1; or p is 0 and q is 3; or p is 3 and q is 0; or p and q are both 2.3. The compound according to or an N-oxide thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , polymorph or tautomer thereof claim 1 , wherein Z is (CH)NH(CH).4. The compound according to or an N-oxide thereof claim 3 , or a pharmaceutically acceptable salt claim 3 , solvate claim 3 , polymorph or tautomer thereof claim 3 , wherein Z is (CH)NH(CH).5. The compound according to or an N-oxide thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , polymorph or tautomer thereof claim 1 , wherein Xand Xare each independently selected from chloro claim 1 , bromo and iodo.6. The compound according to or an N-oxide thereof claim 5 , or a pharmaceutically acceptable salt claim 5 , solvate claim 5 , polymorph or tautomer thereof claim 5 , wherein Xand Xare both chloro.7. The compound according to or an N-oxide thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , polymorph or tautomer thereof claim 1 , wherein Q is an optionally substituted benzimidazolyl.8. The compound according to or an N-oxide thereof claim 7 , or a pharmaceutically acceptable salt claim 7 , solvate claim 7 , polymorph or tautomer thereof claim 7 , wherein Q is benzimidazolyl substituted by one or more alkyl groups.12. The compound according to claim 11 , which is the hydrochloride salt or a solvate or polymorph thereof.13. A pharmaceutical composition comprising a compound of formula (I) or an N-oxide ...

Phototherapy Devices and Methods Comprising Optionally Substituted Quinquiesphenyl Compounds

Methods and devices related to the treatment of diseases using phototherapy are described. Some embodiments provide an organic light-emitting diode device, such as a light-emitting device for phototherapy, comprising Ring System 1, Ring System 2, Ring System 3, Ring System 4 or Ring System 5. Methods of treating disease with phototherapy are also described.

Space-Through Charge Transfer Compound, and Organic Light Emitting Diode and Display Device Using the Same

Discussed is a space-through charge transfer compound including a naphthalene core; an electron donor moiety selected from carbazole and phenylcarbazole; and an electron acceptor moiety selected from pyridine, diazine, triazole, and phenyl benzodiazole, wherein the electron donor moiety and the electron acceptor moiety are combined to first and eighth positions of the naphthalene core with a benzene linker, respectively. 1. A delayed fluorescence compound , comprising:a naphthalene core;an electron donor moiety; andan electron acceptor moiety selected from the group consisting of pyridine, diazine, triazole, and phenyl benzodiazole,wherein the electron donor moiety and the electron acceptor moiety are combined to first and eighth positions of the naphthalene core with a benzene linker, respectively.2. The delayed fluorescence compound according to claim 1 , wherein the electron donor moiety is selected from the group consisting of carbazole claim 1 , phenylcarbazole and biphenylamine.4. The delayed fluorescence compound according to claim 1 , wherein a difference between a singlet energy of the delayed fluorescence compound and a triplet energy of the delayed fluorescence compound is less than 0.3 eV.5. The delayed fluorescence compound according to claim 1 , wherein a charge transfer is directly generated through a space between the electron donor moiety and the electron acceptor moiety.7. An organic light emitting diode claim 1 , comprising:a first electrode;a second electrode facing the first electrode; andan organic emitting layer between the first electrode and the second electrode, the organic emitting layer including a delayed fluorescence compound,wherein the delayed fluorescence compound includes a naphthalene core, an electron donor moiety, and an electron acceptor moiety selected from the group consisting of pyridine, diazine, triazole, and phenyl benzodiazole, andwherein the electron donor moiety and the electron acceptor moiety are combined to first and ...

Fluoroallylamine Derivative And Use Thereof

The present invention relates to a fluoroallylamine derivative and use thereof. In particular, the present invention relates to a compound as shown in Formula I, a prodrug, an isomer, an isotope-labeled compound, a solvate or a pharmaceutically acceptable salt thereof, which has VAP-1/SSAO inhibitory activity, and can be used for treating a disease associated with VAP-1/SSAO overactivity. 8. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , an ester claim 1 , a solvate claim 1 , a hydrate claim 1 , an isomer claim 1 , or an isotope-labeled compound thereof; any crystal form or racemate thereof; a metabolite thereof; or a mixture thereof claim 1 , wherein the pharmaceutically acceptable salt is a hydrochloride or a trifluoroacetate claim 1 , and preferably claim 1 , the pharmaceutically acceptable salt is a hydrochloride.11. A pharmaceutical composition claim 1 , comprising a compound of claim 1 , a pharmaceutically acceptable salt claim 1 , an ester claim 1 , a solvate claim 1 , a hydrate claim 1 , an isomer claim 1 , or an isotope-labeled compound thereof; any crystal form or racemate thereof; a metabolite thereof; or a mixture thereof claim 1 , and one or more pharmaceutical excipients.1314.-. (canceled)15. A method for treating a disease or disorder associated with the overactivity of VAP-1/SSAO claim 1 , comprising a step of administrating a patient in need of such treatment with an effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , an ester claim 1 , a hydrate claim 1 , a solvate claim 1 , an isomer claim 1 , or an isotope-labeled compound thereof; any crystal form or racemate thereof; a metabolite thereof; or a mixture thereof.16. The compound of claim 4 , or a pharmaceutically acceptable salt claim 4 , an ester claim 4 , a solvate claim 4 , a hydrate claim 4 , an isomer claim 4 , or an isotope-labeled compound thereof; any crystal form or racemate thereof; a metabolite thereof; or a mixture ...

INHIBITORS OF INV(16) LEUKEMIA

This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. 7. The method of claim 6 , wherein said inv(16) leukemia cell is an acute myeloid leukemia cell.8. The method of claim 6 , wherein said compound inhibits CBFβ-SMMHC activity.9. The method of claim 8 , wherein said compound inhibits CBFβ-SMMHC from interacting with Runt.10. The method of claim 6 , wherein said compound binds to the CBFβ portion of CBFβ-SMMHC.9. The method of claim 8 , wherein said compound increases apoptosis.13. A method of inhibiting inv(16) leukemia cell proliferation claim 1 , said method comprising contacting an inv(16) leukemia cell with a pharmaceutical composition comprising an effective amount of at least one compound of claim 1 , and a pharmaceutically-acceptable carrier.14. The method of claim 13 , wherein said inv(16) leukemia cell is an acute myeloid leukemia cell.15. The method of claim 13 , wherein said compound inhibits CBFβ-SMMHC activity.16. The ...

PESTICIDALLY ACTIVE CARBAMOYLATED AND THIOCARBAMOYLATED OXIME DERIVATIVES

Compounds of formula (I), wherein the substituents are as defined in claim , and agrochemically acceptable salts thereof, can be used as insecticides. 13. A pesticidal composition claim 1 , which comprises at least one compound of formula (I) according to or claim 1 , where appropriate claim 1 , a tautomer thereof claim 1 , in each case in free form or in an agrochemically utilizable salt form claim 1 , as active ingredient and at least one auxiliary.14. A method for controlling pests claim 13 , which comprises applying a composition according to to the pests or their environment with the exception of a method for treatment of the human or animal body by surgery or therapy and diagnostic methods practiced on the human or animal body.15. A method for the protection of plant propagation material from the attack by pests claim 13 , which comprises treating the propagation material or the site claim 13 , where the propagation material is planted claim 13 , with a composition according to . The present invention relates to compounds of formula (I) below, to processes for preparing them, to pesticidal, in particular insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control pests such as insect, acarine, mollusc and nematode pests.Heterocyclic compounds with pesticidal activity are known and described, for example, in WO09/102736, WO11/017505, WO12/109125, WO13/116052, WO13/116053 and WO14/011429. There have now been found novel pesticidal active carbamoylated and thiocarbamoylated oximes. The present invention accordingly relates to compounds of formula (I),wherein, Arand Arare independently of each other phenyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl, wherein said phenyl, thienyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, furanyl can be substituted by one to three substituents independently selected from the group consisting of hydrogen, C-Calkyl, C-Calkenyl, C- ...

COMPOSITIONS AND METHODS OF MODULATING SHORT-CHAIN DEHYDROGENASE

Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors described herein. 196-. (canceled)102: The method of claim 97 , the compound being administered to a tissue of a subject at an amount effective to increase prostaglandin levels in the tissue.103: The method of claim 97 , the compound being administered to a subject to promote wound healing claim 97 , tissue repair claim 97 , and/or tissue regeneration.104: The method of claim 97 , the compound being administered to a subject to treat at least one of oral ulcers claim 97 , gum disease claim 97 , colitis claim 97 , ulcerative colitis claim 97 , gastrointestinal ulcers claim 97 , inflammatory bowel disease claim 97 , vascular insufficiency claim 97 , Raynaud's disease claim 97 , Buerger's disease claim 97 , diabetic neuropathy claim 97 , pulmonary artery hypertension claim 97 , cardiovascular disease claim 97 , and renal disease.105: The method of claim 97 , the compound being administered to tissue of the subject to increase tissue stem cells.106: The method of claim 97 , the compound being administered to a tissue graft donor claim 97 , bone marrow graft donor claim 97 , and/or a hematopoietic stem cell donor to increase the fitness of a donor tissue graft claim 97 , a donor bone marrow graft claim 97 , and/or a donor hematopoietic stem cell graft.107: The method of claim 97 , the compound being administered to bone marrow of a subject to increase stem cells in the subject or to increase the fitness of the marrow as a donor graft.108: The method of claim 97 , the compound being administered to a preparation of hematopoietic stem cells of a subject to increase the fitness of the stem cell preparation as a donor graft or to increase the fitness of the stem cell preparation as a donor graft.109: The method of claim 97 , ...

SPACE-THROUGH CHARGE TRANSFER COMPOUND, AND ORGANIC LIGHT EMITTING DIODE AND DISPLAY DEVICE USING THE SAME

Discussed is a space-through charge transfer compound including a naphthalene core; an electron donor moiety selected from carbazole and phenylcarbazole; and an electron acceptor moiety selected from pyridine, diazine, triazole, and phenyl benzodiazole, wherein the electron donor moiety and the electron acceptor moiety are combined to first and eighth positions of the naphthalene core with a benzene linker, respectively. 1. A space-through charge transfer compound , comprising:a naphthalene core;an electron donor moiety selected from the group consisting of carbazole and phenylcarbazole; andan electron acceptor moiety selected from the group consisting of pyridine, diazine, triazole, and phenyl benzodiazole,wherein the electron donor moiety and the electron acceptor moiety are combined to first and eighth positions of the naphthalene core with a benzene linker, respectively.3. The space-through charge transfer compound according to claim 2 , wherein a difference between a singlet energy of the space-through charge transfer compound and a triplet energy of the space-through charge transfer compound is less than 0.3 eV.4. An organic light emitting diode claim 2 , comprising:a first electrode;a second electrode facing the first electrode; andan organic emitting layer between the first electrode and the second electrode, the organic emitting layer including a space-through charge transfer compound,wherein the space-through charge transfer compound includes a naphthalene core, an electron donor moiety selected from the group consisting of carbazole and phenylcarbazole, and an electron acceptor moiety selected from the groupo consisting of pyridine, diazine, triazole, and phenyl benzodiazole, andwherein the electron donor moiety and the electron acceptor moiety are combined to first and eighth positions of the naphthalene core with a benzene linker, respectively.5. The organic light emitting diode according to claim 4 , wherein the organic emitting layer includes a hole ...

HETEROCYCLIC DERIVATIVE AND ORGANIC ELECTROLUMINESCENT DEVICE THEREOF

Provided are a heterocyclic derivative and an organic electroluminescent device thereof, which relates to the field of organic photoelectric materials. The heterocyclic derivative of Formula I has high electron mobility and great hole blocking performance, and thus the organic electroluminescent device prepared by using the heterocyclic derivative as the electron transport region material, especially the hole blocking material, has low drive voltage and high luminous efficiency. The organic electroluminescent device can also include a hole transport region, and the hole transport region, especially the emissive auxiliary layer, contains the triarylamine compound of Formula II. Since the electron transport region and the hole transport region of the device can effectively balance carriers, which reduces the quenching of excitons and improves the recombination probability of carriers, the device shows low drive voltage and high luminous efficiency. 6. An organic electroluminescent device claim 1 , comprising an anode claim 1 , an organic layer claim 1 , and a cathode claim 1 , wherein the organic layer is disposed between the anode and the cathode claim 1 , and the organic layer comprises an electron transport region containing the heterocyclic derivative according to .9. The organic electroluminescent device according to claim 7 , wherein Ris independently selected from one of hydrogen claim 7 , deuterium claim 7 , methyl claim 7 , ethyl claim 7 , propyl claim 7 , butyl claim 7 , adamantyl claim 7 , camphanyl claim 7 , norbornyl claim 7 , phenyl claim 7 , tolyl claim 7 , biphenyl claim 7 , triphenyl claim 7 , naphthyl claim 7 , anthryl claim 7 , phenanthryl claim 7 , triphenylenyl claim 7 , acridinyl claim 7 , spirodifluorenyl claim 7 , 9 claim 7 ,9-dimethylfluorenyl claim 7 , 9 claim 7 ,9-diphenylfluorenyl claim 7 , 9-phenylcarbazolyl claim 7 , pyrenyl claim 7 , indolyl claim 7 , benzothiophenyl claim 7 , benzofuranyl claim 7 , dibenzothiophenyl or dibenzofuranyl ...

BENZIMIDAZOLE DERIVATES USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY

A compound of formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compound. The compound is useful in therapy, for the treatment of disorders mediated by HDAC6, such as autoimmune disorders, neurodegenerative disorders and hyperproliferative disorders, such as cancer. 3. The compound of claim 2 , wherein each Ris independently selected from halogen claim 2 , C1-C10 alkyl claim 2 , RO claim 2 , RRNX claim 2 , CN claim 2 , 5- or 6-membered heteroaryl claim 2 , and phenyl claim 2 , and when n is at least 2 claim 2 , two Rattached to adjacent atoms of ring A may form together a biradical selected from —YCHY— and —Y(CH)Y—; wherein Yand Yare independently selected from O and CH.4. The compound of claim 3 , wherein each Ris independently selected from halogen claim 3 , C1-C10 alkyl claim 3 , RO claim 3 , and phenyl claim 3 , said phenyl optionally being substituted with one or more R.5. The compound of claim 2 , wherein n is an integer of from 1 to 3.6. The compound claim 5 , wherein one Ris phenyl claim 5 , said phenyl optionally being substituted with one or more R.7. The compound of claim 5 , wherein ring A is phenyl.9. The compound of claim 2 , wherein ring A is 5- to 10-membered mono- or bicyclic heteroaryl.10. The compound of claim 2 , wherein ring A is 5- or 6-membered monocyclic heteroaryl.11. The compound of claim 1 , wherein W is a direct bond claim 1 , CH claim 1 , CH(CH) claim 1 , CHCH claim 1 , or CH═CH.12. The compound of claim 11 , wherein W is a direct bond.13. The compound of claim 1 , wherein Ris H.14. The compound of claim 1 , wherein Ris H.15. A compound according to claim 1 , selected from2-(3-chlorophenyl)-N-hydroxy-1H-benzimidazole-6-carboxamide,N-hydroxy-2-(2-methoxyphenyl)-1H-benzimidazole-6-carboxamide,2-(4-bromophenyl)-N-hydroxy-1H-benzimidazole-6-carboxamide,N-hydroxy-2-(4-methylphenyl)-1H-benzimidazole-6-carboxamide,N-hydroxy-2-[4-(trifluoromethyl)phenyl]-1H-benzimidazole-6-carboxamide,2- ...

SUBSTITUTED BENZOFURAN DERIVATIVES AS NOVEL ANTIMYCOBACTERIAL AGENTS

Novel bacterial inhibitors comprising benzofuran derivatives, and methods of bacterial inhibition using the inhibitors are disclosed. The inhibitors may inhibit, for example, mycobacteria, including , by inhibition of the Pks13 enzyme. The inhibitors cmat exhibit potent whole cell and in vivo efficacy against 3. The composition of claim 1 , wherein the Rsubstituent of the at least one benzofuran derivative is a hydroxyl moiety.4. The composition of claim 1 , wherein the Rsubstituent of the at least one benzofuran derivative is a CONHMe moiety.5. The composition of claim 1 , wherein the at least one benzofuran derivative has a half-maximal inhibitory concentration against wild-type Pks13 thioesterase of 0.25 μM or less.6Mycobacterium tuberculosis. The composition of claim 1 , wherein the at least one benzofuran derivative has a minimum inhibitory concentration against bacilli of 2 μM or less.7. The composition of claim 1 , wherein the at least one benzofuran derivative is selected from the group consisting of Inhibitor 31 and Inhibitor 32.9Mycobacterium.. The method of claim 8 , wherein the bacterium is a10MycobacteriumMycobacterium tuberculosis.. The method of claim 9 , wherein the is11. The method of claim 8 , further comprising administering to the patient at least one additional antibiotic drug.12. The method of claim 11 , wherein the at least one additional antibiotic drug is selected from the group consisting of with one or more drugs selected from the group consisting of isoniazid claim 11 , rifampicin claim 11 , pyrazinamide claim 11 , ethambutol claim 11 , rifapentine claim 11 , rifabutin claim 11 , streptomycin claim 11 , kanamycin claim 11 , and amikacin claim 11 , capreomycin claim 11 , viomycin claim 11 , ciprofloxacin claim 11 , levofloxacin claim 11 , moxifloxacin claim 11 , ofloxacin claim 11 , gatifloxacin claim 11 , para-aminosalicylic acid claim 11 , cycloserine claim 11 , terizidone claim 11 , ethionamide claim 11 , prothionamide claim 11 , ...

(hetero)aryl sulfonamide compound and formulation for controlling harmful organisms

In formula (I), Ar1 is a benzene ring or a 5- to 6-membered heteroaryl ring, R1 is a C1 to C6 alkyl group, a halogeno group, or the like, n represents the number of R1 and is 0, 1, 2, or 3, and in the case of n being 2 or more, two or more R1 may be the same as or different from one another, R2 is a C1 to C6 alkyl group, a C1 to C6 haloalkyl group, or the like, R3 is a hydrogen atom, a C1 to C6 alkyl group, a C1 to C6 alkylcarbonyl group, or the like, and AR2 represents a substituted or unsubstituted heteroaryl group.

COMPOUNDS FOR TREATMENT OF CANCER

The present invention relates to colchicine-binding site compounds having anti-cancer activity, compositions comprising the same, and their use for treating various forms of cancer. 2. The method according to claim 1 , wherein Ris OCH claim 1 , n is 3 and Ris hydrogen.4. The method according to claim 1 , wherein the cancer is prostate cancer claim 1 , drug-resistant prostate cancer claim 1 , breast cancer claim 1 , drug-resistant breast cancer claim 1 , ovarian cancer claim 1 , drug-resistant ovarian cancer claim 1 , skin cancer claim 1 , melanoma claim 1 , drug-resistant melanoma claim 1 , lung cancer claim 1 , colon cancer claim 1 , glioma claim 1 , leukemia claim 1 , lymphoma claim 1 , renal cancer claim 1 , CNS cancer claim 1 , uterine cancer claim 1 , drug-resistant uterine cancer claim 1 , or a combination thereof.5. The method according to claim 1 , wherein cancer is melanoma claim 1 , metastatic melanoma claim 1 , or prostate cancer.7. The method according to claim 7 , wherein Ris OCH claim 7 , n is 3 and Ris hydrogen.10. The method according to claim 7 , wherein the tumor is prostate cancer tumor claim 7 , breast cancer tumor claim 7 , glioma tumor claim 7 , ovarian cancer tumor claim 7 , skin cancer tumor claim 7 , lung cancer tumor claim 7 , colon cancer tumor claim 7 , leukemia tumor claim 7 , lymphoma tumor claim 7 , renal cancer tumor claim 7 , CNS cancer tumor claim 7 , uterine cancer tumor claim 7 , or a combination thereof.11. The method according to claim 7 , wherein the tumor is drug-resistant prostate cancer tumor claim 7 , drug-resistant breast cancer tumor claim 7 , drug-resistant ovarian cancer tumor claim 7 , drug-resistant melanoma tumor claim 7 , drug-resistant uterine cancer tumor claim 7 , or a combination thereof.12. The method according to claim 7 , wherein cancer is melanoma tumor claim 7 , metastatic melanoma tumor claim 7 , or prostate cancer tumor.13. The method according to further comprising a second cancer therapy. This ...

ORGANIC COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT

The present disclosure provides an organic compound that has a mother skeleton with a fused-ring structure, an electron-withdrawing group bonded to the mother skeleton, and an electron-donating group bonded to the mother skeleton, wherein the electron-withdrawing group is bonded at a position satisfying the following relationship in the mother skeleton. 1. An organic compound comprising: a mother skeleton with a fused-ring structure; an electron-withdrawing group bonded to the mother skeleton; and an electron-donating group bonded to the mother skeleton , wherein the electron-withdrawing group is bonded at a position satisfying the following relationship in the mother skeleton.{'br': None, 'i': C', '|>Σ|C, 'sub': H', 'L, 'Σ||\u2003\u2003(1)'}{'sub': 'H', '(C: 2PZ atomic orbital coefficient of a carbon at a substitution site in HOMO of the mother skeleton)'}{'sub': 'L', '(C: 2PZ atomic orbital coefficient of the carbon at the substitution site in LUMO of the mother skeleton)'}2. The organic compound according to claim 1 , wherein the electron-withdrawing group satisfies the following formula (2) claim 1 , the electron-donating group is provided on a first carbon atom in the mother skeleton such that a substituent can be introduced into at least one of second and third carbon atoms on both sides of the first carbon atom claim 1 , and an electric charge value of a natural bond orbital of the first carbon atom having the electron-donating group in the mother skeleton is equal to or lower than an electric charge value of a natural bond orbital of the second carbon atom adjacent to the first carbon atom and equal to or lower than an electric charge value of a natural bond orbital of the third carbon atom adjacent to the first carbon atom.{'br': None, 'i': 'E−Eb', '≤−1.51 (eV)\u2003\u2003(2)'}(E: a LUMO level of a substituent in the mother skeleton, Eb: a LUMO level of a structure in which the electron-withdrawing group is removed from the substituent)3. The organic ...

SSAO INHIBITOR

The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof. 5. The compound or the pharmaceutically acceptable salt thereof according to any one of claim 1 , wherein the ring A is selected from the group consisting of 1 claim 1 ,3 claim 1 ,4-oxadiazolyl claim 1 , 1 claim 1 ,2 claim 1 ,4-oxadiazolyl claim 1 , 1H-1 claim 1 ,2 claim 1 ,4-triazolyl claim 1 , thiazolyl claim 1 , isothiazolyl claim 1 , 1 claim 1 ,2 claim 1 ,4-thiadiazolyl claim 1 , oxazolyl claim 1 , isoxazolyl claim 1 , 1H-tetrazyl claim 1 , pyridyl claim 1 , pyrimidinyl claim 1 , pyridazinyl claim 1 , indolyl claim 1 , benzoxazolyl claim 1 , benzisoxazolyl claim 1 , 4 claim 1 ,5 claim 1 ,6 claim 1 ,7-tetrahydro-1H-benzimidazolyl claim 1 , 2H-1 claim 1 ,2 claim 1 ,3-triazolyl claim 1 , benzo[d]thiazolyl claim 1 , 2H-benzo[d]imidazolyl claim 1 , indoline-2 claim 1 ,3-diketo claim 1 , 4 claim 1 ,5-dihydro-1H-imidazolyl and 1 claim 1 ,3-dihydro-1H-pyrrole claim 1 , wherein each is optionally substituted by a R group.10. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , halogen claim 1 , OH claim 1 , NH claim 1 , CN claim 1 , COOH claim 1 , and —C(═O)NH; or is selected from the group consisting of Calkyl claim 1 , Cheteroalkyl claim 1 , phenyl claim 1 , cyclopropyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , morpholinyl claim 1 , cyclobutyl and tetrahydro-2H-pyranyl claim 1 , wherein each is optionally substituted by one claim 1 , two or three R groups.19. A method for the treatment of a disease related to SSAO claim 1 , comprising a step of administering the compound or the pharmaceutically acceptable salt thereof according to or a tautomer thereof to a subject in need.20. The method according to claim 19 ...

1,3-DIAMINOCYCLOPENTANE CARBOXAMIDE DERIVATIVES

Compounds of the formula I 2. Compounds according to in which{'sup': '4', 'Rdenotes H, OA′, Hal or A′,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.3. Compounds according to claim 1 , in which{'sub': '2', 'sup': '5', 'A denotes unbranched or branched alkyl with 1-10 C-atoms, wherein one or two non-adjacent CH- and/or CH-groups may be replaced by N- and/or O-atoms and wherein 1-7 H-atoms may be replaced by R,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.4. Compounds according to claim 1 , in which{'sup': 3', '3', '3', '3, 'sub': 2', '2', 'p', '2', 'p', '2, 'Ar denotes phenyl, which is unsubstituted or mono-, di-, tri-, tetra- or pentasubstituted by Hal, CN, CON(R), [C(R)]OA, [C(R)]COOR, A, Cyc and/or OCHCyc,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.5. Compounds according to claim 1 , in which{'sup': '1', 'Ardenotes phenyl or naphthyl,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.6. Compounds according to claim 1 , in which{'sup': 3', '3', '3', '3', '1', '3, 'sub': 2', 'p', '2', 'n', '2', '2', '2', 'n, 'Het denotes a mono- or bicyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which is unsubstituted or mono-, di- or trisubstituted by Hal, [C(R)]OA′, [C(R)]N(R), CON(R), Het, A, [C(R)]CN and/or ═O,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.7. Compounds according to claim 1 , in which{'sup': '1', 'Hetdenotes a monocyclic saturated, unsaturated or aromatic heterocycle having 1 to 4 N, O and/or S atoms, which is unsubstituted or mono- or disubstituted by Hal, A and/or ═O,'}and pharmaceutically acceptable salts, tautomers and stereoisomers thereof, including mixtures ...

MULTI-TIERED HIGH THROUGH-PUT SCREEN FOR COMPOUNDS EFFECTIVE AGAINST BACTERIAL BIOFILM AND COMPOUNDS EFFECTIVE FOR INHIBITING AND ERADICATING BACTERIAL BIOFILM

A high through-put screening method for identifying agents effective for inhibiting biofilm formation and/or killing established biofilm are disclosed. The method includes three tiers, and each tier includes three specific biological process assays. The tier levels are a primary screen, a confirmation screen, and a dose-response screen, and the biological process assays include assays for total bacterial growth, bacterial metabolic activity, and biofilm formation. The series of assays may be run once or more than once at each tier. A library of compounds is subject to tier A and only compounds meeting a primary parameter advance to tier B, and only tier B compounds meeting a confirmation parameter advance to tier C, and only tier C compounds meeting a dose-response parameter are identified as putative agents effective for inhibiting and/or eradicating a biofilm, further wherein the assays are conducted for each compound subject to the respective tier. The method is effective and validated for identifying agents which inhibit and/or kill , and biofilms. Agents identified according to the high through-put screen and validated in follow-up experiments as effective for inhibiting and/or killing bacterial biofilms are also disclosed. 1S. epidermidis, P. aeruginosaA. baumannii. A compound effective for inhibiting bacterial biofilm formation and/or killing established bacterial biofilm , wherein the bacteria is one or more of , and , and the compound is selected from the compounds set forth in Table 1.2A. baumannii. The compound according to effective for killing established biofilm claim 1 , wherein the compound is selected from 1 claim 1 , 2 claim 1 , 12 claim 1 , 17 claim 1 , 18 claim 1 , 31 claim 1 , and 34.3A. baumannii. The compound according to effective for inhibiting formation of an biofilm claim 1 , wherein the compound is selected from 1 claim 1 , 2 claim 1 , 12 claim 1 , 17 and 18.4P. aeruginosa. The compound according to effective for inhibiting formation of a ...

ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE

The compound represented by formula (1): 2. The compound according to claim 1 , wherein the compound is represented by any of formulae (2-1) to (2-6);{'sup': 11', '16', '21', '26', 'a, 'sub': 101', '102', '103, 'each of Rto Rand Rto Ris independently a hydrogen atom, a fluorine atom, a cyano group, a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms, a substituted or unsubstituted cycloalkyl group having 3 to 20 ring carbon atoms, a substituted or unsubstituted alkoxy group having 1 to 20 carbon atoms, a substituted or unsubstituted fluoroalkyl group having 1 to 20 carbon atoms, a substituted or unsubstituted fluoroalkoxy group having 1 to 20 carbon atoms, a substituted or unsubstituted aryloxy group having 6 to 30 ring carbon atoms, a substituted or unsubstituted alkylthio group having 1 to 20 carbon atoms, a substituted or unsubstituted arylthio group having 6 to 30 ring carbon atoms, a group represented by —Si(R)(R)(R), or a group represented by —Z—R;'}{'sup': 11', '16', '21', '26', 'a, 'provided that at least one of Rto Rand Rto Rof each of formulae (2-1), (2-2), (2-3), (2-4), (2-5), and (2-6) is a group represented by —Z—R;'}{'sup': 1', '2', '1', '2, "R's and R's, if present, may be the same or different, and R's and R's may be bonded to each other to form a ring structure, respectively; and"}{'sup': 11', '16', '21', '26, 'adjacent two selected from Rto Rand Rto Rmay be bonded to each other to form a ring structure.'}3. A material for organic electroluminescence devices comprising the compound according to .4. An organic electroluminescence device comprising an organic thin film layer which comprises one or more layers and is disposed between a cathode and an anode claim 1 , wherein the organic thin film layer comprises a light emitting layer and at least one layer of the organic thin film layer comprises the compound according to .5. The organic electroluminescence device according to claim 4 , wherein the light emitting layer comprises the ...

METABOTROPHIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS OF USE THEREOF

Compounds that modulate GluR5 activity and methods of using the same are disclosed. 2. The compound of claim 1 , wherein at least one of Y claim 1 , Y claim 1 , and Yis nitrogen.3. The compound of claim 1 , wherein Y claim 1 , Y claim 1 , and Yare all CR.4. The compound of claim 1 , wherein L is —C≡C—.5. The compound of claim 1 , wherein Rand Rare hydrogen.6. The compound of claim 1 , wherein Ris aryl or heteroaryl.7. The compound of claim 1 , wherein Ris heteroaryl.8. The compound of claim 7 , wherein Ris an oxadiazolyl or triazolyl moiety.10. The compound of claim 9 , wherein at least one of Y claim 9 , Y claim 9 , and Yis nitrogen.11. The compound of claim 9 , wherein Y claim 9 , Y claim 9 , and Yare CR.12. The compound of claim 9 , wherein Ris hydrogen.13. The compound of claim 9 , wherein Ris aryl or heteroaryl.15. The compound of claim 9 , wherein Ris heterocycloalkyl or heteroaryl.17. The compound of claim 15 , wherein Ris heteroaryl.21. (canceled)22. A pharmaceutical composition comprising a therapeutically effective amount of a compound or and a pharmaceutically acceptable carrier.23. A method for treating a disorder or disease mediated by mGluR5 claim 15 , comprising administering to a subject in need thereof a therapeutically effective amount of a compound of or .24. The method of claim 23 , wherein the disorder or disease mediated by mGluR5 is a neurological disorder.25. The method of claim 24 , wherein the neurological disorder is a neurodegenerative disease claim 24 , a neuropsychiatric disease claim 24 , an affective disorder claim 24 , a loss of cognitive function or a learning and memory disorder.26. A methods for treating psychosis claim 24 , comprising administering to a subject in need thereof a therapeutically effective amount of a compound of or .27. A method for treating schizophrenia claim 24 , comprising administering to a subject in need thereof a therapeutically effective amount of a compound of or .28. A method for treating cognitive ...

FACTOR VIIA INHIBITOR

The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed. This application is a continuation of U.S. application Ser. No. 13/623,578, filed Sep. 20, 2012, which is a continuation of U.S. application Ser. No. 13/100,058, filed May 3, 2011, now issued as U.S. Pat. No. 8,415,328 on Apr. 9, 2013, which is a continuation of U.S. application Ser. No. 11/597,335, filed Jul. 14, 2008, which is the National Phase entry of International Application No. PCT/US2005/019394, filed June, 2005, which claims the benefit of U.S. Provisional Application No. 60/576,382, filed Jun. 2, 2004, all of which are hereby incorporated by reference in their entireties.1. Field of InventionThe present invention relates to novel inhibitors of Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing disorders mediated by Factor VIIa. Processes for preparing these inhibitors are also disclosed.2. State of the ArtThrombosis results from a complex sequence of biochemical events, known as the coagulation cascade. A triggering event in coagulation is the binding of the serine protease Factor VIIa (FVIIa), found in the circulation, to tissue factor (TF), a receptor, which is found on the surface of blood vessels after damage or inflammation. Once bound to TF, Factor VIIa catalyzes the formation of the serine protease Factor Xa, which subsequently forms the final protease in the cascade, thrombin.The clinical manifestations of thrombosis range from acute myocardial infarction (AMI or heart attack) and unstable angina (UA), which occur in the key blood vessels of the heart (coronary vasculature) to deep vein thrombosis (DVT), which is the ...

Aryl hydrocarbon receptor activators

Small molecule AhR ligands are disclosed. The ligands can induce the differentiation of Tr1 cells to suppress pathogenic immune responses without inducing nonspecific immune suppression. Methods of treatment of autoimmune diseases using the AhR ligands are also disclosed.

BENZIMIDAZOLE SUBSTITUTION-BASED PHENYL N-BUTYRAMIDE COMPOUND AND PREPARATION METHOD THEREFOR

The present disclosure relates to a benzimidazole-substituted phenyl-n-butyramide-based compound and the preparation method thereof. The method of the present disclosure avoids nitration reaction and polyphosphoric acid cyclization reaction, and avoids the generation of a large amount of waste acid reaction solution from the source. The synthesis method embodied in the invention has the advantages of simplicity and high efficiency, mild conditions and few pollutants, etc., and is suitable to be developed as a green and sustainable production process. 4. The method according to claim 2 , wherein the method Five is conducted according to one of the following three methods:{'sub': '3', 'Method (a), when Ris chlorine, or bromine, or n-butyryloxy, reacting the compound of formula VI with n-butyryl chloride, or n-butyryl bromide, or n-butyric anhydride to prepare the compound of formula III,'}In particular, method (a) is conducted in presence of a basic reagent, the basic reagent is one selected from the group consisting of lithium carbonate, sodium carbonate, potassium carbonate, cesium carbonate, sodium bicarbonate, potassium bicarbonate, sodium phosphate, potassium phosphate, sodium monohydrogen phosphate, potassium monohydrogen phosphate, lithium hydroxide, sodium hydroxide, potassium hydroxide, magnesium carbonate, magnesium hydroxide, calcium carbonate, calcium hydroxide, calcium oxide, magnesium oxide, lithium methoxide, sodium methoxide, potassium methoxide, sodium ethoxide, potassium ethoxide, lithium isopropoxide, sodium isopropoxide, potassium isopropoxide, lithium tert-butoxide, sodium tert-butoxide, potassium tert-butoxide, magnesium methoxide, magnesium ethoxide, magnesium tert-butoxide, ammonia water, triethylamine, diisopropylamine, diisopropyl ethyl amine, tri-n-butyl amine, pyridine, 2-methylpyridine, 2,6-dimethylpyridine, 4-dimethylaminopyridine, tetrahydropyrrole, morpholine, piperidine and 2,2,6,6-tetramethylpiperidine; or a mixture thereof;In ...

NOVEL COMPOUND AND METHOD FOR PRODUCING SAME

A compound represented by the formula (1) is provided: 2. The compound according to claim 1 , wherein both of two Aare —NR—.4. The compound according to claim 1 , wherein Ris a hydrogen atom.5. A composition comprising the compound according to and an electron-transporting material.6. A composition comprising the compound according to claim 5 , further comprising a solvent.8. The method according to claim 7 , wherein{'sup': '4', 'Ris a hydrogen atom, and'}{'sup': '2', 'Mis an aluminum atom.'} The present invention relates to a novel compound and a method for producing the same.In recent years, research on various electronic devices such as organic light-emitting diodes (OLED), polymer light-emitting diodes (PLED), organic photovoltaics (OPV), and organic thin film transistors (OTFT) using ultrathin films of organic materials has been actively made. For these electronic devices, methods using doping materials are known as methods for improving conductivity.For example, an organic thin film transistor using N-DMBI as an n-type doping material is disclosed in Non Patent Literature 1; an organic light-emitting diode using N-DMBI as an n-type doping material is disclosed in Patent Literature 1; and an n-type dopant precursor for doping an organic semiconductor material is disclosed in Patent Literature 2.However, sufficient findings on stable n-type doping materials that permit film formation by a coating method have not yet been obtained. For example, compounds described as n-type doping materials in the cited literatures mentioned above did not always have sufficient electron-donating ability.Accordingly, an object of the present invention is to provide a novel compound that can be suitably used as a strong n-type doping material, and a method for producing the same.The present invention provides the following [1] to [9]:[1] A compound represented by the formula (1):whereinArepresents an oxygen atom, a sulfur atom, —NR— or —PR—; two Aare the same as or different from ...

Crystals containing unsaturated carboxylic acid amide compound and method for producing same

Provided is a crystal of an unsaturated carboxylic acid amide. The crystal is useful as or for fine chemicals such as pharmaceuticals, agricultural chemicals, polymeric materials, functional materials, and intermediates of them, has a high purity, still is not bulky, and can be handled excellently. The crystal includes an unsaturated carboxylic acid amide represented by Formula (1) in an amount of 95 percent by area or more and has a bulk density of 0.2 to 0.7 g/mL. In the formula, R 1 to R 5 are independently selected from hydrogen, alkyl, hydroxyl, alkoxy, and nitro. At least two of R 1 to R 5 may be linked to form a ring together with carbon atoms constituting the specified aromatic ring. R 6 , R 7 , and R 8 are independently selected from hydrogen, alkyl, and aryl. R 7 and R 8 may be linked to form a ring together with carbon atoms constituting the specified imidazole ring.

Pyrene-based compound and organic light-emitting diode comprising the same

A pyrene-based compound, and an organic light-emitting diode including the pyrene-based compound are provided.

TOLL-LIKE RECEPTOR ANTAGONIST COMPOUNDS AND METHODS OF USE

The invention relates to compounds of formula (I): 2. The method of claim 1 , wherein at least one applies:{'sup': 1', '2', '2', '3, '(a) Ais N, Ais CRand Ais N;'}{'sup': 1', '2', '2', '2a', '3, '(b) Ais C, Ais CRor NRand Ais NH;'}{'sup': 4', '5, '(c) Ais N and Ais N;'}{'sup': 4', '5', '5, '(d) Ais N and Ais CR;'}{'sup': 4', '4', '5', '5, '(e) Ais CRand Ais CR.'}3. The method of claim 1 , wherein at least one applies:{'sup': '2a', 'sub': 1', '6, '(a) Ris C-Calkyl;'}{'sup': '4', '(b) Ris hydrogen;'}{'sup': '5', '(c) Ris hydrogen.'}5. The method of claim 1 , wherein i is 2 and j is 1 or 2; or wherein i is 1 and j is 2; or wherein i is 1 and j is 1; or wherein i is 1 and j is 0; or wherein i is 0 and j is 0.6. The method of claim 1 , wherein at least one applied:(a) U is a bond;(b) Visa bond;{'sub': 2', '2, '(c) V is ethylene (—CHCH—).'}7. The method of claim 1 , wherein: n is 0; or n is 1 or 2 and each Ris independently C-Calkyl optionally substituted by R.8. The method of claim 1 , wherein Ris phenyl optionally substituted by R.9. The method of claim 1 , wherein at least one applies:{'sup': '2', 'sub': 1', '6, '(a) Ris C-Calkyl;'}{'sup': '3', 'sub': 1', '6, '(b) Ris C-Calkyl;'}{'sup': '7', 'sub': 1', '6, '(c) Ris hydrogen or C-Calkyl;'}(d) W is a bond;{'sub': 1', '4, 'sup': W1', 'W2, '(e) W is C-Calkylene optionally substituted by one or both of Rand R;'}{'sup': X1', 'X2, 'sub': 1', '6, 'each of Rand Ris independently hydrogen or C-Calkyl;'}{'sup': Y1', 'Y2, 'sub': 1', '6, '(g) each of Rand Ris independently hydrogen or C-Calkyl;'}{'sup': '8', 'sub': 1', '6, '(h) Ris hydrogen or C-Calkyl;'}{'sup': 9', '10, 'sub': 1', '6, 'Ris hydrogen or C-Calkyl optionally substituted by R;'}{'sup': 8', '9', '10', '10, 'Rand Rare taken together with the nitrogen atom to which they are attached to form a 3-12-membered heterocyclyl optionally substituted by Ror a 5-10-membered heteroaryl optionally substituted by R;'}{'sup': Y1', 'Y2', '8', '9', '10, '(k) R, R, Rand Rare taken ...

BICYCLIC COMPOUND

The present invention provides a compound represented by the formula (I): 2. The compound or salt of claim 1 , wherein Ris a group represented by —CORwherein Ris a Calkyl group claim 1 , a Calkoxy group claim 1 , or an amino group optionally mono- or di-substituted by Calkyl group(s).3. The compound or salt of claim 1 , wherein Ris a Calkyl group optionally substituted by 1 to 3 halogen atoms.4. The compound or salt of claim 1 , wherein Rand Rare both hydrogen atoms.5. The compound or salt of claim 1 , wherein X is C claim 1 , CO or CH.6. The compound or salt of t claim 1 , wherein ring A is a 5- or 6-membered aromatic ring optionally further substituted by 1 to 4 substituents selected from(1) a halogen atom,{'sub': '1-6', '(2) a Calkyl group, and'}{'sub': '1-6', '(3) a Calkoxy group.'}8. The compound or salt of claim 1 , wherein Ris a Calkyl group optionally substituted by 1 to 3 substituents selected from{'sub': '3-6', '(a) a Ccycloalkyl group optionally substituted by 1 to 5 halogen atoms,'}(b) a halogen atom,(c) a hydroxy group, and{'sub': '6-14', '(d) a Caryl group.'}10. N-((2S)-1-((2-(4-(Cyclopropylmethoxy)-2 claim 1 ,5-difluorophenyl)[1 claim 1 ,3]oxazolo[4 claim 1 ,5-c]pyridin-6-yl)oxy)propan-2-yl)acetamide or a salt thereof.11. N-((2S)-1-((2-(4-(((1R)-2 claim 1 ,2-Difluorocyclopropyl)methoxy)phenyl)[1 claim 1 ,3]oxazolo[4 claim 1 ,5-c]pyridin-6-yl)oxy)propan-2-yl)acetamide or a salt thereof.12. N-((2S)-1-((2-(4-(((1R)-2 claim 1 ,2-Difluorocyclopropyl)methoxy)-3-fluorophenyl) [1 claim 1 ,3]oxazolo[4 claim 1 ,5-c]pyridin-6-yl)oxy)propan-2-yl)acetamide or a salt thereof.13. A medicament comprising the compound or salt of .14. The medicament of claim 13 , which is an acetyl-CoA carboxylase inhibitor.15. The medicament of claim 13 , which is an agent for the prophylaxis or treatment of obesity or diabetes.16. A method of inhibiting acetyl-CoA carboxylase in a mammal claim 1 , which comprises administering an effective amount of the compound or salt of to the ...

USE OF HEMATOPOIETIC GROWTH FACTOR MIMETICS

The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. A method of treating a disorder associated with erythropoiesis in a patient in need of such treatment , said method comprising:administering an initial effective amount of a non-peptidyl small molecule mimetic of EPO to the patient; andadministering a second effective amount of the mimetic of EPO to the patient,wherein the initial and the second effective amounts are substantially the same.25. The method of claim 24 , further comprising administering a third effective amount of the mimetic of EPO to the patient that is substantially the same as the initial and second effective amounts.26. The method of claim 25 , further comprising administering one or more subsequent effective amounts of the mimetic of EPO to the patient that is substantially the same as the initial claim 25 , second claim 25 , and third effective amounts.27. The method of claim 24 , wherein the initial and the second effective amounts are the same.28. The method of claim 24 , comprising administering a series of effective amounts that are substantially the same to the patient at least daily claim 24 , at least weekly claim 24 , or at least monthly.29. A method of treating a disorder associated with erythropoiesis to a patient in need of such treatment claim 24 , said method comprising:administering an effective amount of a non-peptidyl small molecule mimetic of EPO to the patient, wherein the amount administered to the patient is not titrated over the period of time for administration.30. The ...

INHIBITORS OF INV(16) LEUKEMIA

This invention describes the development of targeted small molecule inhibitors of the inv(16) fusion, the causative agent in ˜12% of acute myeloid leukemia (AML). The inv(16) fusion results in expression of the CBFβ-SMMHC fusion protein in the blood cells of afflicted patients. The present invention provides compounds which inhibit the function of both CBFβ and the CBFβ-SMMHC fusion. These compounds block the growth of an inv(16) leukemia cell line as well as increase its apoptosis, while showing minimal effects against non inv(16) cell lines. As a mechanism to develop inhibitors with selectivity for the CBFβ-SMMHC fusion protein, the present invention further provides dimeric derivatives of these compounds which show both increased potency as well as selectivity for CBFβ-SMMHC. These compounds show potent inhibition of an inv(16) leukemia cell line with minimal effects on non inv(16) cell lines. Analysis of the pharmacokinetics of the developed compounds has made it possible to improve the lifetime of the compound in the plasma of mice to a level commensurate with long-term treatment. 5. The method of claim 3 , wherein inv(16) leukemia is acute myeloid leukemia.6. The method of claim 3 , wherein said compound inhibits CBFβ-SMMHC activity.7. The method of claim 3 , wherein said compound inhibits CBFβ-SMMHC from interacting with Runt.8. The method of claim 3 , wherein said compound binds to the CBFβ portion of CBFβ-SMMHC.9. The method of claim 3 , wherein said compound increases apoptosis.12. The method of claim 10 , wherein inv(16) leukemia is acute myeloid leukemia.13. The method of claim 10 , wherein said compound inhibits CBFβ-SMMHC activity.14. The method of claim 10 , wherein said compound inhibits CBFβ-SMMHC from interacting with Runt.15. The method of claim 10 , wherein said compound binds to the CBFβ portion of CBFβ-SMMHC.16. The method of claim 10 , wherein said compound increases apoptosis. This application is a continuation application of U.S. application ...

TRANSCRIPTOME-WIDE DESIGN OF SELECTIVE, BIOACTIVE SMALL MOLECULES TARGETING RNA

Methods and computer systems are described herein for identifying small molecules that bind to selected RNA structural features (e.g., to RNA secondary structures). Also described are compounds and compositions that modulate RNA function and/or activity. 3. A method of modulating microRNA function or activity comprising claim 1 , contacting the microRNA with the compound of .4. The method of claim 3 , wherein the microRNA is a pre-microRNA-96 claim 3 , a pre-microRNA-210 claim 3 , or a pre-microRNA-182.5. A method of treating cancer in a subject claim 3 , comprising administering to the subject a compound of or a composition of claim 3 , to thereby treat cancer in the subject.7. The method of claim 6 , wherein the microRNA is pre-microRNA-96.9. The method of claim 8 , wherein the microRNA is pre-microRNA-210.11. The method of claim 10 , wherein the microRNA is microRNA-182.12. A method for identifying a compound that binds to an RNA claim 10 , comprising:(a) comparing a query dataset of RNA secondary structures from the RNA, with a dataset of identified bound RNA motif-small molecule pairs, to generate an output listing of pairs of identified RNA secondary structures and the identified small molecule that bind thereto;(b) obtaining an RNA with an identified RNA secondary structure and the identified small molecule that binds thereto;(c) determining a binding affinity of the identified RNA secondary structure with the identified small molecule that binds thereto by mixing an RNA having the RNA secondary structure with the identified small molecule and measuring the binding affinity, and/or determining whether the identified small molecule reduces or increases amounts of an RNA having the RNA secondary structure in a mammalian cell;to thereby identify a compound that binds to the RNA.13. The method of claim 12 , wherein the output listing of pairs of identified RNA secondary structures and the identified small molecule that binds thereto comprises one or more RNA ...

AGONISTS OF ROR GAMMAt

The present invention is directed to compounds of the formula (I) wherein all substituents are defined herein, as well as pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders. 14. A compound which is2,4-dichloro-3-(3-isopropyl-4-methoxyphenoxy)benzonitrile,4,6-dichloro-5-(3-isopropyl-4-methoxyphenoxy)-2-phenyl-1H-benzo[d]imidazole,N-({2,4-dichloro-3-[4-methoxy-3-(propan-2-yl)phenoxy]phenyl}methyl)-2-[(1-methanesulfonylpiperidin-4-yl)oxy]acetamide,N-({2,4-dichloro-3-[4-methoxy-3-(propan-2-yl)phenoxy]phenyl}methyl)-2-{[1-(ethanesulfonyl)piperidin-4-yl]oxy}acetamide,2-benzyl-4,6-dichloro-5-[4-methoxy-3-(propan-2-yl)phenoxy]-1H-1,3-benzodiazole,4,6-dichloro-5-[4-methoxy-3-(propan-2-yl)phenoxy]-2-[(pyridin-3-yl)methyl]-1H-1,3-benzodiazole,3,5-dichloro-4-[4-methoxy-3-(propan-2-yl)phenoxy]aniline, or{3,5-dichloro-4-[4-methoxy-3-(propan-2-yl)phenoxy]phenyl}methanolor a pharmaceutically acceptable salt thereof.15. A pharmaceutical composition comprising one or more compounds according to or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable carriers claim 1 , diluents or excipients. This application claims the benefit of U.S. Provisional Application No. 62/883,171, filed Aug. 6, 2019, the disclosure of which is incorporated herein by reference in its entirety.The invention provides novel compounds, pharmaceutical compositions comprising the compounds, and methods of using them, for example, for the treatment or prophylaxis of certain cancers and to their use in therapy.RORgt is a key lineage-defining transcription factor involved in the differentiation of naïve T cells to Th17 and Tc17 cells. IL-17 is a signature cytokine of RORgt transactivation (Ivanov et al; 2006, 126, 1121).High IL-17 levels have been associated with various autoimmune diseases. Consequently, several groups have identified RORgt inverse agonists to decrease IL-17 ...

SSAO INHIBITOR

The present invention provides an SSAO inhibitor and an application thereof in preparing a drug for treating a disease related to SSAO. In particular, the present invention provides a compound shown in formula (IV) and a pharmaceutically acceptable salt thereof. 4. The compound or the pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris selected from the group consisting of H claim 1 , halogen claim 1 , OH claim 1 , NH claim 1 , CN claim 1 , COOH claim 1 , and —C(═O)NH; or is selected from the group consisting of Calkyl claim 1 , Cheteroalkyl claim 1 , phenyl claim 1 , cyclopropyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , morpholinyl claim 1 , cyclobutyl and tetrahydro-2H-pyranyl claim 1 , wherein each is optionally substituted by one claim 1 , two or three R groups.8. A method for the treatment of a disease related to SSAO claim 1 , comprising a step of administering the compound or the pharmaceutically acceptable salt thereof according to or a tautomer thereof to a subject in need.9. The method according to claim 8 , wherein the disease related to SSAO is nonalcoholic steatohepatitis. This application is a divisional application of U.S. utility application Ser. No. 16/714,690, filed Dec. 14, 2019, now pending, which is a continuation application of International Patent Application No. PCT/CN2018/092003 with an international filing date of Jun. 20, 2018, designating the United States, now expired, and further claims priority benefits to Chinese Patent Application No. CN201710470167.8, filed on Jun. 20, 2017; Chinese Patent Application No. CN201710661017.5, filed on Aug. 4, 2017; Chinese Patent Application No. CN201711229457. X, filed on Nov. 29, 2017; and Chinese Patent Application No. CN201810582595.4, filed on Jun. 7, 2018. The contents of all of the aforementioned applications are incorporated herein by reference.The present disclosure relates to an SSAO inhibitor and use thereof in the preparation of a medicament for the ...

METHOD FOR TREATING NEURODEGENERATIVE DISEASES

The present invention is directed to a method for treating a neurodegenerative disease such as amyotrophic lateral sclerosis (ALS), Alzheimer disease, Parkinson's disease, Huntington's disease, frontotemporal degeneration, dementia with Lewy bodies, a motor neuron disease, or a demyelinating disease. The method comprises administering to a subject in need thereof a Ppargca activator 2-(4-tert-butylphenyl)-1H-benzimidazole, 2-[4-(1,1-dimethylethyl)phenyl]-1H-benzimidazole, in an effective amount. A preferred route of administration is oral administration. 1. A method of suppressing myeloid-mediated inflammation in a subject diagnosed with a neurodegenerative disease , comprising the step of administering to a subject suffering from a neurodegenerative disease an effective amount of 2-(4-tert-butylphenyl)-1H-benzimidazole , or a solvate or pharmaceutically acceptable salt thereof.2. The method of claim 1 , wherein the neurodegenerative disease is selected from the group consisting of: amyotrophic lateral sclerosis (ALS) claim 1 , Alzheimer disease claim 1 , Parkinson's disease claim 1 , Huntington's disease claim 1 , frontotemporal degeneration claim 1 , dementia with Lewy bodies claim 1 , a motor neuron disease claim 1 , and a demyelinating disease.3. The method according to claim 1 , wherein said compound is administered by systemic administration.4. The method according to claim 1 , wherein said compound is administered by oral administration.5. The method according to claim 2 , wherein the neurodegenerative disease is ALS.6. The method according to claim 2 , wherein the neurodegenerative disease is Alzheimer disease.7. The method according to claim 2 , wherein the neurodegenerative disease is Parkinson's disease.8. The method according to claim 2 , wherein the neurodegenerative disease is Huntington's disease.9. The method according to claim 2 , wherein the neurodegenerative disease is frontotemporal degeneration.10. The method according to claim 2 , wherein the ...

Anthracene derivative and organic electroluminescent element using same

An anthracene derivative is represented by the following formula (1). In the formula (1), one of R 11 to R 20 is used to bond to L 1 , and is a single bond. The remainder of R 11 to R 20 that are not used to bond to L 1 are independently a hydrogen atom, a halogen atom, a cyano group, a substituted or unsubstituted alkyl group including 1 to 20 carbon atoms, or the like. L 1 is a single bond, a substituted or unsubstituted divalent aromatic hydrocarbon group including 6 to 50 ring carbon atoms, or the like. Z has a structure represented by the following formula (2). In the formula (2), one of R 1 , R 3 , and R 4 is used to bond to L 1 , and is a single bond. The remainder of R 1 , R 3 , and R 4 that are not used to bond to L 1 , R 2 , and R 5 to R 10 are independently a hydrogen atom, a halogen atom, a cyano group, a substituted or unsubstituted alkyl group including 1 to 20 carbon atoms, or the like. At least one pair of groups among R 5 to R 8 that are adjacent to each other are bonded to each other to form a saturated or unsaturated hydrocarbon ring.

COMPOUNDS FOR ELECTRONIC DEVICES

The present invention relates to a compound of the formula (I), to the use of this compound in an electronic device, and to an electronic device comprising one or more compounds of the formula (I). The invention furthermore relates to the preparation of the compound of the formula (I) and to a formulation comprising one or more compounds of the formula (I). 115.-. (canceled)17. The compound of claim 16 , wherein the groups Arof group A of formula (II) are identically or differently on each occurrence claim 16 , an aryl group having 6 to 10 aromatic ring atoms.18. The compound of claim 16 , wherein the group A is identically or differently on each occurrence claim 16 , of the formula (II) claim 16 , and each of the groups Arare connected via the group Y.21. The compound of claim 16 , wherein Y is selected from a single bond claim 16 , C(R) claim 16 , NR claim 16 , O claim 16 , or S.22. The compound of claim 18 , wherein Y is selected from a single bond claim 18 , C(R) claim 18 , NR claim 18 , O claim 18 , or S.23. The compound of claim 16 , wherein the group Ris claim 16 , identically or differently on each occurrence claim 16 , F or CN.24. The compound of claim 16 , wherein the radicals Rin formula (I) are selected identically.25. The compound of claim 23 , wherein the radicals Rin formula (I) are selected identically.27. An oligomer claim 16 , polymer claim 16 , or dendrimer claim 16 , comprising one or more compounds of claim 16 , wherein bonds to the oligomer claim 16 , polymer claim 16 , or dendrimer claim 16 , are connected at any position of the formula (I) by R claim 16 , R claim 16 , R.28. A formulation comprising at least one compound of and at least one solvent.29. A formulation comprising at least one oligomer claim 25 , polymer claim 25 , or dendrimer claim 25 , of and at least one solvent.30. An electronic device comprising at least one compound of claim 16 , wherein the the electronic device is selected from an organic integrated circuit (O-IC) claim ...

TRANSCRIPTOME-WIDE DESIGN OF SELECTIVE, BIOACTIVE SMALL MOLECULES TARGETING RNA

Methods and computer systems are described herein for identifying small molecules that bind to selected RNA structural features (e.g., to RNA secondary structures). Also described are compounds and compositions that modulate RNA function and/or activity. 3. A method of modulating microRNA function or activity comprising claim 1 , contacting the microRNA with the compound of .4. The method of claim 3 , wherein the microRNA is a pre-microRNA-96 claim 3 , a pre-microRNA-210 claim 3 , or a pre-microRNA-182.5. A method of treating cancer in a subject claim 2 , comprising administering to the subject the composition of claim 2 , to thereby treat cancer in the subject.7. The method of claim 6 , wherein the microRNA is pre-microRNA-96.9. The method of claim 8 , wherein the microRNA is pre-microRNA-210.11. The method of claim 10 , wherein the microRNA is microRNA-182.12. A method for identifying a compound that binds to an RNA claim 10 , comprising:(a) comparing a query dataset of RNA secondary structures from the RNA, with a dataset of identified bound RNA motif-small molecule pairs, to generate an output listing of pairs of identified RNA secondary structures and the identified small molecule that bind thereto;(b) obtaining an RNA with an identified RNA secondary structure and the identified small molecule that binds thereto;(c) determining a binding affinity of the identified RNA secondary structure with the identified small molecule that binds thereto by mixing an RNA having the RNA secondary structure with the identified small molecule and measuring the binding affinity, and/or determining whether the identified small molecule reduces or increases amounts of an RNA having the RNA secondary structure in a mammalian cell;to thereby identify a compound that binds to the RNA.13. The method of claim 12 , wherein the output listing of pairs of identified RNA secondary structures and the identified small molecule that binds thereto comprises one or more RNA sequence for each ...

N-(3-heteroarylaryl)-4-arylarylcarboxamides and Analogs as Hedgehog Pathway Inhibitors and Use Thereof

Disclosed are novel N-(3-heteroarylaryl)-4-arylarylcarboxamides and analogs thereof, represented by the Formula I: wherein C cyclic group, D-D, Q, Q, Rare defined herein. Compounds having Formula (I) are hedgehog pathway inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of hedgehog activity, such as cancer. 2. (canceled)4. The compound of claim 3 , wherein Qis an optionally substituted phenyl claim 3 , pyridyl claim 3 , morpholinyl claim 3 , piperazinyl or piperidyl.7. (canceled)8. The compound of claim 1 , wherein said compound is selected from the group consisting of:N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methylbiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-4′-methoxybiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-4′-fluorobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-4′-(methylsulfonyl)biphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-4′-cyanobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-4′-nitrobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-4′-chlorobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-4′-acetylbiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-3′-fluorobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methyl-3′-cyanobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-4′-fluorobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3′-fluorobiphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-2-methyl-4′-(trifluoromethyl)biphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-methoxy-4′-(trifluoromethyl)biphenyl-4-carboxamide;N-(3-(1H-benzo[d]imidazol-2-yl)-4-chlorophenyl)-3-hydroxy-4′-(trifluoromethyl)biphenyl-4- ...

COMPOUND HAVING AGONISTIC ACTIVITY ON SOMATOSTATIN RECEPTOR, AND USE THEREOF FOR MEDICAL PURPOSES

Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): 2. The compound according to claim 1 , wherein Ring G represents benzene.8. The compound according to claim 1 , wherein the Ring A represents benzene claim 1 , benzimidazole claim 1 , indazole claim 1 , indole claim 1 , imidazole claim 1 , triazole claim 1 , pyrazole claim 1 , pyridine claim 1 , pyrimidine claim 1 , thiophene claim 1 , oxazole claim 1 , thiazole claim 1 , or oxadiazole.9. The compound according to claim 4 , wherein the compound is (1) 1-{3-(3 claim 4 ,5-dimethylphenyl)-5-[4-(trifluoromethyl)phenyl]-4-pyridinyl}-4-piperidinamine claim 4 , (2) 1-{3-(3-fluoro-5-methylphenyl)-5-[4-(trifluoromethyl)phenyl]-4-pyridinyl}-4-piperidinamine claim 4 , (3) 3-{(E)-2-[4-(4-amino-1-piperidinyl)-5-(3-fluoro-5-methylphenyl)-3-pyridinyl]vinyl}benzonitrile claim 4 , (4) 4-(4-amino-1-piperidinyl)-N claim 4 ,5-bis(3 claim 4 ,5-dimethyphenyl)pyridine-3-carboxamide claim 4 , (5) 1-[3-(4 claim 4 ,6-dimethyl-1H-benzimidazol-2-yl)-5-(3 claim 4 ,5-dimethyphenyl)-4-pyridyl]piperidin-4-amine claim 4 , (6) 1-[3-(4 claim 4 ,6-dimethyl-1H-benzimidazol-2-yl)-5-(3 claim 4 ,5-dimethyphenyl)-4-pyridinyl]-N-(3-oxetanyl)-4-piperidinamine claim 4 , (7) 1-[3-(3 claim 4 ,5-dimethoxyphenyl)-5-(5 claim 4 ,7-dimethyl-1H-benzimidazol-2-yl)-4-pyridinyl]-N-(2-fluoroethyl)-4-piperidinamine claim 4 , (8) 1-[3-(3-fluoro-5-methoxyphenyl)-5-(1H-indazol-6-yl)-4-pyridinyl]-4-piperidinamine claim 4 , (9) 5-[4-(4-amino-1-piperidinyl)-5-(3-fluoro-5-methylphenyl)-3-pyridinyl]-2-methylphenol claim 4 , (10) 1-[3-(5-chloro-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)-4-pyridinyl]-N-(3-oxetanyl)-4-piperidinamine claim 4 , (11) (3-{4-(4-amino-1-piperidinyl)-5-[4-(trifluoromethyl)phenyl]-3-pyridinyl}-5-fluorophenyl)methanol claim 4 , or (12) {4-[4-(4-amino-1-piperidinyl)-5-(3-fluoro-5-methylphenyl)-3-pyridinyl]phenyl}acetonitrile.10. The compound according to claim ...

CYTOSINE DEAMINASE MODULATORS FOR ENHANCEMENT OF DNA TRANSFECTION

Compounds and methods are provided for enhancing or boosting the transfection rate or efficiency of mammalian cells by foreign DNA, such as bacterial plasmid DNA. Compounds, including natural products and inventive synthetic compounds can increase the effectiveness of uptake and incorporation of foreign DNA by mammalian cells, such as human cells, by suppression of DNA cytosine deamination, which is believed to be a mechanism by which these cells eliminate foreign DNA. Inhibition of the cytosine deaminase enzymes by compounds as described herein serves to provide more effective transfection of eukaryotic cells by plasmids including engineered gene sequences. Transfection can be used to study cellular processes, or to cure genetic diseases in human patients. The inventive materials and methods increase the efficiency and effectiveness of such transfection techniques. 410.-. (canceled)12. (canceled)14. (canceled)17. (canceled)18. The method of wherein the cytosine deaminase is any or all of APOBEC3A (A3A) claim 16 , APOBEC3B (A3B) claim 16 , APOBEC3C (A3C) claim 16 , APOBEC3D (A3D; also known as A3DE) claim 16 , APOBEC3F (A3F) claim 16 , APOBEC3G (A3G) claim 16 , APOBEC3H (A3H) claim 16 , AID claim 16 , APOBEC1 claim 16 , APOBEC2 claim 16 , APOBEC4 claim 16 , or any of Z1 claim 16 , Z2 claim 16 , and/or Z3 type APOBEC3.20. (canceled)21. The method of wherein the foreign DNA comprises a single-stranded or double-stranded DNA fragment claim 19 , a plasmid claim 19 , a cosmid claim 19 , a synthetic chromosome claim 19 , or engineered viral DNA.22. The method of wherein the foreign DNA is contacted with the target cell in the presence of the compound and further in the presence of a transfection adjuvant claim 19 , or with electroporation claim 19 , or with nucleofection claim 19 , or any combination thereof.23. The method of wherein the transfection adjuvant comprises a cationic lipid claim 22 , a cationic polymer claim 22 , a cationic peptide claim 22 , a pegylated ...

Chemical modulators of immune checkpoints and therapeutic use

Compounds and pharmaceutical compositions that down-regulate immune checkpoints such as PD-1, PD-L1 and CTLA-4 are provided. Also provided are methods of treating a disease by down-regulating immune checkpoints such as PD-1, PD-L1 and CTLA-4. The methods are useful for treating cancer and viral infection in a subject.

ARYL HYDROCARBON RECEPTOR ANTAGONISTS AND METHODS OF USE

The disclosure relates to aryl hydrocarbon receptor antagonists as well as methods of modulating aryl hydrocarbon receptor activity and expanding hematopoietic stem cells by culturing hematopoietic stem or progenitor cells in the presence of these agents. Additionally, the disclosure provides methods of treating various pathologies, such as cancer, by administration of these aryl hydrocarbon receptor antagonists. Additionally, the disclosure provides methods of treating various pathologies in a patient by administration of expanded hematopoietic stem cells. The disclosure further provides kits containing aryl hydrocarbon receptor antagonists that can be used for the expansion of hematopoietic stem cells. The disclosure further relates to pharmaceutical compositions comprising the compounds and methods of treating or preventing a disease in which aryl hydrocarbon receptor plays a role. 2. The compound of claim 1 , wherein b is 1 and c is 0.3. The compound of any one of the preceding claims claim 1 , wherein A is an optionally substituted monocyclic ring selected from the group consisting of benzene claim 1 , pyridine claim 1 , thiazole claim 1 , piperazine claim 1 , pyrimidine claim 1 , 1 claim 1 ,2 claim 1 ,3-triazole claim 1 , pyrazole claim 1 , furan claim 1 , isoxazole claim 1 , 4H-pyridazine claim 1 , thiophene claim 1 , oxazole claim 1 , and 2H-pyridine.4. The compound of any one of the preceding claims claim 1 , wherein A is an optionally substituted bicyclic ring selected from the group consisting of benzo[d][1 claim 1 ,2 claim 1 ,3]triazole claim 1 , thieno[2 claim 1 ,3-b]pyridine claim 1 , imidazo[1 claim 1 ,2-a]pyridine claim 1 , quinolone claim 1 , pyrido[1 claim 1 ,2-a]pyrimidine claim 1 , 6 claim 1 ,7-dihydro-5H-thiazolo[4 claim 1 ,5-b]pyridine claim 1 , benzo[d]imidazole claim 1 , isoindoline claim 1 , benzo[d]isothiazole claim 1 , benzo[d]thiazole claim 1 , benzo[b]thiophene claim 1 , indoline claim 1 , and [1 claim 1 ,2 claim 1 ,4]triazolo[1 claim 1 ...

COMPOUND HAVING AGONISTIC ACTIVITY ON SOMATOSTATIN RECEPTOR, AND USE THEREOF FOR MEDICAL PURPOSES

Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): 2. (canceled)3. (canceled)8. (canceled)9. (canceled)10. The compound according to claim 1 , wherein the compound is (1) 5-[(E)-2-{5-(3-fluoro-5-methylphenyl)-4-[rac-(4aR claim 1 ,8aR)-octahydro-6H-pyrido[3 claim 1 ,4-b][1 claim 1 ,4]oxazin-6-yl]-3-pyridinyl}vinyl]nicotinonitrile claim 1 , or (2) rac-(4aR claim 1 ,8aR)-6-[3-(6-chloro-1H-benzimidazol-2-yl)-5-(3-fluoro-5-methylphenyl)-4-pyridinyl]octahydro-1H-pyrido[3 claim 1 ,4-b][1 claim 1 ,4]oxazine.11. A pharmaceutical composition which comprises the compound of the formula (I) according to claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , a solvate thereof claim 1 , and a pharmaceutically acceptable excipients.12. (canceled)13. (canceled)14. A medicine comprising the compound according to claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , or a solvate thereof and at least one drug selected from the group consisting of pegvisomant claim 1 , bromocriptine claim 1 , and cabergoline.15. A medicine comprising the compound according to claim 1 , a salt thereof claim 1 , an N-oxide thereof claim 1 , or a solvate thereof and at least one drug selected from the group consisting of prochlorperazine claim 1 , levomepromazine claim 1 , risperidone claim 1 , metoclopramide claim 1 , domperidone claim 1 , diphenhydramine claim 1 , chlorpheniramine claim 1 , dimenhydrinate claim 1 , promethazine claim 1 , diprophylline claim 1 , famotidine claim 1 , cimetidine claim 1 , scopolamine claim 1 , tropisetron claim 1 , granisetron claim 1 , ondansetron claim 1 , azasetron claim 1 , ramosetron claim 1 , indisetron claim 1 , palonosetron claim 1 , cisapride claim 1 , mosapride claim 1 , dexamethasone claim 1 , betamethasone claim 1 , prednisolone claim 1 , aprepitant claim 1 , olanzapine claim 1 , quetiapine claim 1 , perospirone claim 1 , methylnaltrexone and morphine ...

NOVEL FUSED POLYCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE, DISPLAY APPARATUS, IMAGE INFORMATION PROCESSING APPARATUS, LIGHTING SYSTEM, AND IMAGE FORMING APPARATUS HAVING THE COMPOUND

A novel organic compound suitable for blue-light-emitting devices and an organic light-emitting device including the compound are provided. 2. The fused polycyclic compound according to claim 1 , wherein{'sub': 2', '4', '8', '12', '13, 'at least two of R, R, R, R, and Rare electron-withdrawing substituents.'}3. An organic light-emitting device comprising:a pair of electrodes; andan organic compound layer disposed between the pair of electrodes, wherein{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the organic compound layer includes a fused polycyclic compound according to .'}4. The organic light-emitting device according to claim 3 , whereinthe organic compound layer is a light-emitting layer including a host material and a guest material; andthe guest material is the fused polycyclic compound.5. The organic light-emitting device according to claim 3 , whereinthe organic compound layer is a light-emitting layer including a plurality of guest materials;at least one of the plurality of guest materials is the fused polycyclic compound; andthe device emits white light.6. A display apparatus comprising:a plurality of pixels, wherein{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'at least one of the plurality of pixels includes an organic light-emitting device according to and an active device connected to the organic light-emitting device.'}7. An image information processing apparatus comprising:an image input section for inputting image information; anda display section for displaying an image, wherein{'claim-ref': {'@idref': 'CLM-00006', 'claim 6'}, 'the display section is a display apparatus according to .'}8. A lighting system comprising:{'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'an organic light-emitting device according to ; and'}an AC/DC converter circuit connected to the organic light-emitting device.9. An image forming apparatus comprising:a photosensitive member;a charging unit for charging a surface of the photosensitive member;an exposure unit ...

1h-benzimidazole-4-carboxamides substituted with phenyl at the 2-position are potent parp inhibitors

Compounds having formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds having formula (I), methods of treatment comprising compounds having formula (I), and methods of inhibiting the PARP enzyme comprising compounds having formula (I).

USE OF SUBSTITUTED 2-AMIDOBENZIMIDAZOLES, 2-AMIDOBENZOXAZOLES AND 2-AMIDOBENZOTHIAZOLES OR SALTS THEREOF AS ACTIVE SUBSTANCES AGAINST ABIOTIC PLANT STRESS

The use of substituted 2-amidobenzimidazoles, 2-amidobenzoxazoles and 2-amidobenzothiazoles of the general formula (I) or salts thereof 2. The compound as claimed in claim 1 , where claim 1 , in formula (I) claim 1 ,{'sup': 1', '2', '3, 'sub': 1', '8', '3', '8', '4', '8', '3', '8', '2', '8', '2', '8', '1', '8', '2', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '3', '8', '3', '8', '1', '8', '1', '8', '1', '8', '2', '8', '1', '8', '2', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '1', '8', '2', '8', '2', '8', '2', '8', '1', '8', '2', '8', '3', '8', '2', '8', '1', '8', '2', '8', '1', '8', '1', '8', '1', '8', '1', '8', '3', '8', '1', '8', '1', '8', '3', '8', '1', '8', '2', '8', '2', '8', '2', '8', '3', '8', '2', '8', '1', '8', '1', '8', '1', '8', '1', '8', '3', '8', '3', '8', '1', '8', '2', '8, 'R, R, Rindependently of one another represent hydrogen, halogen, (C-C)-alkyl, (C-C)-cycloalkyl, (C-C)-cycloalkenyl, (C-C)-halocycloalkyl, (C-C)-alkenyl, (C-C)-alkynyl, optionally substituted phenyl, aryl-(C-C)-alkyl, aryl-(C-C)-alkenyl, heteroaryl, heteroaryl-(C-C)-alkyl, heterocyclyl, heterocyclyl-(C-C)-alkyl, (C-C)-alkoxy-(C-C)-alkyl, (C-C)-alkylthio, (C-C)-haloalkylthio, (C-C)-haloalkyl, (C-C)-alkoxy, (C-C)-haloalkoxy, (C-C)-cycloalkoxy, (C-C)-cycloalkyl-(C-C)-alkoxy, aryloxy, heteroaryloxy, (C-C)-alkoxy-(C-C)-alkoxy, (C-C)-alkynyl-(C-C)-alkoxy, (C-C)-alkenyloxy, bis[(C-C)-alkyl]amino-(C-C)-alkoxy, tris[(C-C)-alkyl]silyl, bis[(C-C)-alkyl]arylsilyl, bis[(C-C)-alkyl]-(C-C)-alkylsilyl, tris[(C-C)-alkyl]silyl-(C-C)-alkynyl, aryl-(C-C)-alkynyl, heteroaryl-(C-C)-alkynyl, (C-C)-alkyl-(C-C)-alkynyl, (C-C)-cycloalkyl-(C-C)-alkynyl, (C-C)-haloalkyl-(C-C)-alkynyl, heterocyclyl-N—(C-C)-alkoxy, nitro, cyano, amino, (C-C)-alkylamino, bis[(C-C)-alkyl]amino, (C-C)-alkylcarbonylamino, (C-C)-cycloalkylcarbonylamino, arylcarbonylamino, (C-C)-alkoxycarbonylamino, heterocyclyl-(C-C)-alkoxy, (C-C)-cycloalkyl-(C-C)-alkyl, (C-C)- ...

Benzimidazole Compounds, Use As Inhibitors of WNT Signaling Pathway in Cancers, and Methods for Preparation Thereof

The present disclosure is concerned with benzimidazole compounds that are capable of inhibiting Wnt signaling and methods of treating disease states such as, for example, cancer, using these compounds. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. 7. A method of treating a disorder associated with Wnt dysfunction in a subject claim 1 , the method comprising administering to the subject an effective amount of at least one compound of claim 1 , or a pharmaceutically acceptable salt thereof.8. The method of claim 7 , wherein the disorder is cancer.9. The method of claim 7 , wherein the compound is selected to have activity of less than about 5 μM against a pancreatic cancer stem cell line.10. The method of claim 9 , wherein the pancreatic cancer stem cell line is selected from PANC-1 claim 9 , Suit-2 claim 9 , S2VP10 claim 9 , and L3.6p1.15. A method of treating a disorder associated with Wnt dysfunction in a subject claim 12 , the method comprising administering to the subject an effective amount of at least one compound of claim 12 , or a pharmaceutically acceptable salt thereof.16. The method of claim 15 , wherein the disorder is cancer.17. The method of claim 15 , wherein the compound is selected to have activity of less than about 5 μM against a pancreatic cancer stem cell line.18. The method of claim 17 , wherein the pancreatic cancer stem cell line is selected from PANC-1 claim 17 , Suit-2 claim 17 , S2VP10 claim 17 , and L3.6p1.21. A method of treating a disorder associated with Wnt dysfunction in a subject claim 20 , the method comprising administering to the subject an effective amount of at least one compound of claim 20 , or a pharmaceutically acceptable salt thereof.22. The method of claim 21 , wherein the disorder is cancer.23. The method of claim 21 , wherein the compound is selected to have activity of less than about 5 μM against a pancreatic ...

Amine derivatives, material for organic electroluminescent device comprising the same, and organic electroluminescent device using the same

A novel amine derivative, a material for an organic electroluminescent (EL) device capable of lowering the driving voltage and enhancing the emission efficiency of the organic EL device, and an organic EL device using the same. According to an embodiment of the present disclosure, an amine derivative is represented by following Formula 1:

VASCULAR ADHESION PROTEIN-1 (VAP-1) MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule Vascular Adhesion Protein-1 (VAP-1) modulator compositions, pharmaceutical compositions, the use and preparation thereof. 3. The compound of claim 2 , wherein Ais selected from the group consisting of —O— claim 2 , —NH— claim 2 , and —S—.4. The compound of claim 2 , wherein Ris selected from the group consisting of —NHCONHPr claim 2 , —NHCONEt claim 2 , —N(Me)CONHEt claim 2 , —NHCOOEt claim 2 , —NHCOEt claim 2 , and —NHCONHEt.7. The compound of claim 6 , wherein X is ═N— and Y is —NH—.8. The compound of claim 6 , wherein X is ═N— and Y is —S—.10. The compound of claim 9 , wherein Z is selected from the group consisting of —O— claim 9 , —NH claim 9 , —NCOCH claim 9 , and —OC(O)NH—.13. The compound of claim 12 , wherein Ais selected from the group consisting of —NHSOMe claim 12 , and —NHSOPh.16. The compound of claim 15 , wherein Ris selected from the group consisting of H claim 15 , —C(O)NRR claim 15 , —NRCOOR claim 15 , —NRCONRR claim 15 , and —O(CO)NRR claim 15 , and —SONRR.18. The compound of claim 17 , wherein Ris selected from the group consisting of H claim 17 , —COMe claim 17 , —COPh claim 17 , —CHPh claim 17 , phenyl claim 17 , and cyclohexyl.19. The compound of claim 17 , wherein Ris —CONHBu.20. The compound of claim 1 , wherein Ais selected from the group consisting of —S— claim 1 , —S(═O)— claim 1 , —SO— claim 1 , —O— claim 1 , —C(═S)— claim 1 , —C(═O)— claim 1 , —NR— claim 1 , —C(O)NR— claim 1 , —S(CH)— claim 1 , —O(CH)— claim 1 , —NR(CH)— claim 1 , —OC(O)NR— claim 1 , —NHC(O)NH— —NHC(S)NH— claim 1 , —NHC(S)O— claim 1 , —NHC(S)— claim 1 , and —NRSO—.22. A pharmaceutical composition comprising a therapeutically effective amount of a compound of any one of - and a pharmaceutically acceptable excipient.23. A method of treating fibrotic disease or a secondary disease state or condition thereof claim 1 , comprising administering to a subject in need thereof claim 1 , a compound according to any one of -.24. The method of ...

Novel compound and organic electronic device comprising the same

A novel compound is disclosed, which is represented by the following Formula (I): wherein Ar 1 , Ar 2 , Ar 3 , Ar 4 , L, Q, G, n1, n2, m1, m2 and q represent the same as defined in the specification. In addition, an organic electronic device is also disclosed, and an organic layer therein comprises the novel compound of the present invention.

COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME

Provided are a novel compound and an organic electronic device using the same. The novel compound is represented by the following Formula (I): 2. The compound as claimed in claim 1 , wherein h claim 1 , i claim 1 , j claim 1 , k claim 1 , l are each independently an integral of 1 to 2 claim 1 , and the total of h claim 1 , i claim 1 , j claim 1 , k claim 1 , and l is not more than 6.6. The compound as claimed in claim 5 , wherein Rand Rare each selected from the group consisting of: the pyridine group claim 5 , the pyrimidine group claim 5 , the pyrazine group claim 5 , the pyridazine group claim 5 , the cyano group claim 5 , the nitro group claim 5 , the trifluoromethyl group claim 5 , the fluoro group claim 5 , the phenylpyridine group claim 5 , the phenylpyrimidine group claim 5 , the phenylpyrazine group claim 5 , the phenylpyridazine group claim 5 , the cyanophenyl group claim 5 , the nitrophenyl group claim 5 , and the trifluoromethylphenyl group.9. The compound as claimed in claim 1 , wherein Gto Gare each independently selected from the group consisting of: a hydrogen atom claim 1 , a deuterium atom claim 1 , a halogen group claim 1 , a nonsubstituted alkyl group having 1 to 12 carbon atoms claim 1 , a nonsubstituted alkenyl group having 2 to 12 carbon atoms claim 1 , and a nonsubstituted alkynyl group having 2 to 12 carbon atoms.10. The compound as claimed in claim 1 , wherein Gand Gare the same.11. The compound as claimed in claim 1 , wherein Gand Ware the same.13. An organic electronic device claim 1 , comprising a first electrode claim 1 , a second electrode claim 1 , and an organic layer disposed between the first electrode and the second electrode claim 1 , wherein the organic layer comprises the compound as claimed in .14. The organic electronic device as claimed in claim 13 , wherein the organic electronic device is an organic light emitting device.15. The organic electronic device as claimed in claim 14 , wherein the organic light emitting device ...

Compound and electronic device including same

A compound is disclosed. The compound has a formula of MA x L y , wherein: A is L is one of M is a metal having six valence electrons, x is an integer from 1-3, y is an integer from 0-2, x+y=3, any of R a -R b and R 1 -R 3 is independently selected from a group consisting of hydrogen, deuterium, fluorine, chlorine, bromine, iodine, N(R 1 ) 2 , N(Ar 1 ) 2 , C(═O)Ar 2 , P(═O)Ar 3 2 , S(═O)Ar 4 , S(═O) 2 Ar 5 , CR 2 ═CR 3 Ar 6 , CN, NO 2 , Si(R 4 ) 3 , B(OR 5 ) 2 , OSO 2 R 6 , a linear alkyl having 1 to 40 carbon atoms, a C 1 -C 40 alkoxyl, a C 1 -C 40 alkylthiol, a C 3 -C 40 branched alkyl, a C 3 -C 40 cycloalkyl, a C 3 -C 40 branched alkoxyl, a C 3 -C 40 cyclic alkoxyl, a C 3 -C 40 branched alkylthiol and a C 3 -C 40 cyclic alkylthiol, any of R 1 -R 6 is one of a hydrogen and an alkyl, any of Ar 1 -Ar 6 is one of a hydrogen and an aryl, and any of R 4 ˜R 11 and R 13 ˜R 15 is independently selected from a group consisting of a hydrogen, a deuterium, a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted cycloalkyl and a substituted or unsubstituted aryl.

Compounds for affinity chromatography and for extending the half-life of a therapeutic agent

Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which, upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent.

Formulations and electronic devices

A formulation comprising at least one solvent and at least two different functional compounds of formula (I) AB] k   (I) wherein A is a functional structural element, the structural element serving as host material, as a unit that has hole-injection and/or hole-transport properties, as a unit t at has electron-injection and/or electron-transport properties, as a unit which has light-emitting properties, or as a unit which improves the transfer from the singlet state to the triplet state of light-emitting compounds; B is a solubility-promoting structural element; and k is an integer in the range from 1 to 20; the molecular weight of the functional compound is at least 550 g/mol, and the solubility-promoting structural element B conforms to the general formula (L-I)

POTENT AND SELECTIVE INHIBITORS OF CYTOCHROME P450

Inhibitors of the enzyme cytochrome P450 (CYP), including 1B1 (CYP1B1), 1A1 (CYP1A1) and 19A1 (CYP19A1) are provided, and are useful in medical applications. Disclosed are highly potent and selective compounds that can be used in chemoprevention to ameliorate malignant changes induced by CYP, or to aid in treatment, including restoration of chemotherapeutic efficacy. 2. The compound of claim 1 , selected from the compounds set forth in Table 2.3. The compound of claim 1 , selected from the compounds set forth in Table 3.4. The compound of claim 1 , selected from the compounds set forth in Table 4.5. The compound of claim 1 , wherein at least one of R1-R6 is a substituted moiety claim 1 , wherein the substitution is a metal complex.6. The compound of claim 3 , selected from the compounds set forth in Table 5.7. A method for inhibiting CYP by administering to cells the compound of .8. A method for inhibiting CYP in a subject comprising administering to the subject a therapeutically effective amount of the compound of .9. A method of restoring the chemotherapeutic efficacy of a chemotherapeutic agent comprising administering to a patient the compound of together with the chemotherapeutic agent. This application claims priority from U.S. Provisional Application Ser. No. 62/975,107 filed Feb. 11, 2020, the entire disclosure of which is incorporated herein by this reference.This invention was made with government support under grant number 5R01GM107586 awarded by the National Institutes of Health. The government has certain rights in the invention.The present invention relates to relates to small molecule inhibitors of the enzyme cytochrome P450 (CYP), including 1B1 (CYP1B1), 1A1 (CYP1A1) and 19A1 (CYP19A1) for use in medical applications. In particular, the invention provides highly potent and selective compounds that may be used in chemoprevention to ameliorate malignant changes induced by CYP, or to aid in treatment, including restoration of chemotherapeutic efficacy. ...

POLYMER-FIXED DERIVATIVES OF DITHIOLANE OR DITHIANE

Derivatives of 1,3-dithianes and 1,3-dithiolanes of the general formula 1a 110.-. (canceled)12. The derivative of claim 11 , wherein Z is selected from:{'sub': 2', '2', 'n', '2', '2', '2', 'n, '—CH—Y—(CH)—CH—, —CH—Y—(CH)—CH═,'}{'sub': 2', '2', 'n', '2', '2', '2', 'n, '—CH—Y—CO—(CH)—CH—, —CH—Y—CO—(CH)—CH═,'}{'sub': 2', '6', '4', '2', 'n', '2', '2', '6', '4', '2', 'n, '—CH—NH—CH—Y—(CH)—CH— or —CH—NH—CH—Y—(CH)—CH═,'}whereY═NH or O, andn=0 to 10.13. The derivative of claim 11 , wherein Z is selected from:{'sub': 2', '2', 'n', '2', '2', '2', 'n, '—CH—Y—(CH)—CH—, —CH—Y—(CH)—CH═,'}{'sub': 2', '2', 'n', '2', '2', '2', 'n, '—CH—Y—CO—(CH)—CH—, —CH—Y—CO—(CH)—CH═,'}whereY═NH or O, andn=0 to 10.14. The derivative of claim 12 , wherein n=1 or 2.15. The derivative of claim 13 , wherein n=1 or 2.16. The derivative of claim 11 , wherein X is selected from Br claim 11 , Cl claim 11 , Br claim 11 , ClO claim 11 , HCl claim 11 , BF claim 11 , CFSO.17. The derivative of claim 11 , wherein X is selected from BF and CFSO.18. The derivative of claim 11 , wherein P is selected from one or more of polystyrene claim 11 , polypropylene claim 11 , polyethylene claim 11 , polyethylene terephthalate claim 11 , silica claim 11 , cellulose.19. The derivative of claim 11 , wherein P represents polystyrene.20. The derivative of claim 15 , wherein P represents polystyrene and X is selected from BF and CFSO.22. A process for preparing a derivative of claim 11 , wherein the process comprises or consists of(a) providing a polymeric support with pendant functional groups,(b) reacting the functional groups in the polymeric support with a chain extender,(c) optionally, modifying the functional groups of the chain-extended product resulting from (b),(d) reacting the product resulting from (b) or (c) with optionally substituted aliphatic or aromatic dithio compounds having one or two carbon atoms between the sulfur atoms, and (e1) to afford a corresponding dithiolanylium salt/dithianylium salt (1b),', 'or', ...

Prodrugs of non-steroid anti-inflammatory agents (nsaids)

The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.