КОНДЕНСИРОВАННЫЕ ПРОИЗВОДНЫЕ АЗОЛПИРИМИДИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (PI3K)

Изобретение относится к новым конденсированным производным азолпиримидина формулы (I), их таутомерной или стереоизомерной форме и их физиологически приемлемым солям. Соединения настоящего изобретения обладают повышенной активностью при ингибировании фосфатидилинозитол-3-киназы (PI3K), в особенности при ингибировании РI3К-γ, и могут использоваться для приготовления лекарственных средств для профилактики и лечения заболеваний, связанных с активностью PI3K и в особенности - РI3К-γ. Такими заболеваниями могут быть, например, воспалительные и иммунорегуляторные заболевания, такие как астма и др. В соединениях формулы (I) Х означает CR5R6 или NH; Y1 означает CR3 или N; химическая связь между означает одинарную связь или двойную связь при условии, что если означает двойную связь, то Y2 и Y3 означают СН, и если означает одинарную связь, то Y2 и Y3 независимо означают CR3R4; Z1, Z2, Z3 и Z4 независимо означают СН, CR2 или N; R1 означает фенил, необязательно содержащий от 1 до 3 заместителей, выбранных ...

ДИАЗЕПИНОИНДОЛЫ - ИНГИБИТОРЫ ФОСФОДИЭСТЕРАЗ-IV

Использование в медицине описываемых производных диазепиноиндола общей формулы I, где R и A имеют указанные в формуле изобретения значения, их рацемические формы, их изомерные конфигурации, определяемые углеродом в положении 3 диазепиноиндол-4-онового ядра, и их фармакологически приемлемые соли, являющиеся ингибиторами фосфодиэстераз-IV, фармацевтические композиции на их основе, обладающие повышенной в отношении ингибирования фосфодиэстераз-IV активностью. 3 с. и 8 з. п. ф-лы, 1 табл.

ГЕТЕРОЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, ПРИГОДНЫЕ ДЛЯ ИСПОЛЬЗОВАНИЯ В КАЧЕСТВЕ АНАБОЛИЧЕСКИХ АГЕНТОВ СКОТА

Настоящее изобретение относится к соединению формулы (I) или его фармацевтически или ветеринарно приемлемым солям, где: А представляет собой -CH2-; и В представляет собой -СН2-, -С(СН3)2-; или -А-В- представляет собой -СН=СН-; один из R1 и R2 представляет собой СН3 и другой представляет собой Н; R3, R4, R5, R6 и R7, каждый независимо выбран из Н, R8 и R9; или R4 и R5 вместе представляют собой -O-СН2-СН2-, -СН2-СН2-O- или -O-СН2-O-, и R3, R6 и R7, каждый представляет собой Н; R8 представляет собой галоген, -CN, C1-C4 алкил, C1-C4 галогеналкил, -СН2OН, -O-(C1-C4 алкил), -O-СН2-(С3-С5)циклоалкил, -СO2Н, -CO2(C1-C4 алкил), -CONH2, -CONH(C1-C4 алкил), -CONH(C1-C4 галогеналкил), -CONH(C3-C6 циклоалкил) или NH2; и R9 представляет собой -ОН, -NHSO2(C1-C3 алкил), -NHCO(C1-C4 алкил), -NHCO(C1-C4 галогеналкил), -NHSO2(С1-С3 галогеналкил) или -NНSO2(фенил). Также изобретение относится к фармацевтической композиции на основе соединения формулы (I), которая обладает агонистической активностью в отношении ...

ТРИЦИКЛИЧЕСКИЕ ОКСАЗОЛИДИНОНОВЫЕ АНТИБИОТИЧЕСКИЕ СОЕДИНЕНИЯ

Настоящее изобретение относится к соединению формулы (I), где ″-----″ обозначает связь, V представляет собой СН и U представляет собой СН или N, или ″-----″ обозначает связь, V представляет собой CRи U представляет собой СН, или также ″-----″ обозначает связь, V представляет собой N и U представляет собой СН, или ″-----″ отсутствует, V представляет собой СН и U представляет собой СН, NH или NR; Rпредставляет собой Н или, в случае когда ″-----″ обозначает связь, может также представлять собой Cалкоксигруппу; Rпредставляет собой Н, галоген, цианогруппу, Салкил или этинил; Rпредставляет собой Н, ацетил или группу формулы -CH-R; Rпредставляет собой Н, Cалкил или Cгидроксиалкил; Rпредставляет собой Н или, в случае когда n не равно 0 и Rобозначает Н, может также представлять собой ОН; Rпредставляет собой Н, Салкил, Сгидроксиалкил, Саминоалкил, СалкоксиСалкил, карбоксильную группу или Салкоксикарбонил; Rпредставляет собой Cгидроксиалкил, карбоксильную группу, Cалкоксикарбонил или группу -(CH)- ...

CПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ 1,2,3,6-ТЕТРАГИДРОПИРРОЛО[1,2-d][1,4]ДИАЗОЦИНОВ

Описывается способ получения нового класса соединений - производных 1,2,3,6-тетрагидропирроло[1,2-d][1,4]диазоцина общей формулы I-VI ! ! где: ! I R1=Me; R2-Me; R3=CHO; X=CO2Me; ! II R1=Et; R2=Me; R3=CHO; X=CO2Me; ! III R1=Et; R2=Me; R3=CF3CO; a) X=CO2Me, b) X=COMe; ! IV R1=Bn; R2=Me; R3=CHO; X=CO2Me; ! V R1=Me; R2=Ph; R3=CHO; a) X=CO2Me, b) X=COMe; ! VI R1=Me; R2=Ph; R3=CF3CO; a) X=CO2Me, b) X=COMe, ! которые могут представлять интерес в качестве ноотропных средств. Способ заключается в том, что соответствующее производное 1,2,3,4-тетрагидропирроло[1,2-а]пиразина растворяют в ацетонитриле и подвергают взаимодействию с двумя молями соединения Н-С=С-Х при кипячении не менее 7 часов, остаток, полученный по окончании реакции и удаления растворителя, очищают с помощью колоночной хроматографии на оксиде алюминия.

СПОСОБ ПОЛУЧЕНИЯ ТЕТРАГИДРО [1,4]-БЕНЗОДИАЗЕПИН-2-ТИОНОВ ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫХ КИСЛЫХ АДДИТИВНЫХ СОЛЕЙ ИЛИ СТЕРЕОХИМИЧЕСКИХ ИЗОМЕРОВ

Сущность изобретения: продукт- ф-лы 1, где R1 - C3 -C6 -алкил, замещенный C3-C6 -циклоалкилом; R2 и R3 -независимо означают водород или C1-C6 -алкил; R4 и R5 - независимо означают водород, C1-C6 -алкил, галоид, циано, нитро или трифторметил; или фармацевтически приемлемые соли. Реагент 1: соответствующее 4, 5, 6, 7-тетрагидроимидазо-[4, 5-ik][1,4]-бензодиазепин-2-он. Реагент 2: галоид. Реагент 3: тиомочевина. Условия реакции: в среде инертного органического растворителя. Структура соединения 1 . 3 табл.

ТРИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ИЛИ ИХ ФАРМАЦЕВТИЧЕСКИ ПРИЕМЛЕМЫЕ СОЛИ

Использование: в качестве терапевтических агентов при желудочно-кишечных заболеваниях: рвоте, панкреатите. Сущность изобретения: продукт - производные бензодиазепина ф-лы 1, где R1-фенил, возможно замещенный фтором, X- -CH2 - или =CHR3, где R3-C1-C4-алкил, R2-2-индолилкарбонил, фенил(низший)алкеноил, который может быть замещен аминогруппой; или R2-фенилкарбамоил, который может быть замещен галогеном или низшей алкоксигруппой, или их фармацевтически приемлемые соли. Предпочтительный продукт: (3S)-1-(2-фторфенил)-3, 4, 6, 7-тетрагидро-3-(2-индолилкарбониламино)-4-оксопирроло(3, 2, 1 - jk)(1,4)-бензодиазепин. Структура ф-лы 1. 1 з. п. ф-лы, 1 табл.

1,7-АНЕЛЛИРОВАННЫЕ ПРОИЗВОДНЫЕ 3-(ПИПЕРАЗИНОАЛКИЛ)-ИНДОЛА, СПОСОБ ИХ ПОЛУЧЕНИЯ (ВАРИАНТЫ), СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И ПРОМЕЖУТОЧНЫЙ ПРОДУКТ ДЛЯ ИХ ПОЛУЧЕНИЯ

Использование: в медицине в качестве лекарственных средств. Сущность изобретения: продукт-1,7-анеллированные производные 3-(гиперазиноалкил)-индола формулы I: где R1 - водород, низший алкоксил, низший алкилтио, гидроксил, галоген, нитро и другие; R2 - водород, галоген, низший алкил и другие; R3 - водород, низший алкил и другие; R4 - водород, C1-C7-алкил; C3-C7-алкенил, C3-C6-циклоалкил и другие; A - сера; кислород, алкиленовая цепь с 2-4-C атомами; R - азот или CH-группа; R5 - пиридинил, фенил, в случае необходимости, замещенный низшим алкилом, алкоксилом, галогеном; D - связь, а также промежуточный продукт - соединения формулы IV, где A - -CH2-, B - -CH2-, R5 - низший алкил; R III 1 - водород, низший алкил, нитрогруппа; R6 - низший алкилкарбонил; R2 - водород, низший алкил; R7 - водород, C1-C7 -алкил; Q - Q'-CO-цепь, где Q' - алкиленовая цепь с 1-3-C-атомами. Соединения формулы I получают взаимодействием соединения формулы II с соединением формулы III или восстановлением соединения формулы ...

ПРОИЗВОДНЫЕ ЦИТОТОКСИЧНЫХ АЛКАЛОИДОВ, ВКЛЮЧАЮЩИХ АСМАРИНЫ A И B, ВЫДЕЛЕННЫЕ ИЗ ГУБКИ

... 1. Соединение, имеющее структурную формулу (I) либо формулу (II): в которых R1 представляет либо водород, либо низкомолекулярный алкил, либо низкомолекулярный алканоил; R2 представляет водород либо низкомолекулярный алкил; R3 является либо алкилом, либо циклоалкиловой группой, содержащей одну или несколько остатков изопрена, либо монотерпеном, либо гексотерпеном, либо гексотерпеновой или дитерпеновой группой; R4 или R5 представляют собой водород либо низкомолекулярный алкил; R6 является низкомолекулярным алкилом; Х представляет собой F, Cl, Вr, или I; а также, в которых низкомолекулярный алкил и низкотяолекулярный-алкильный остаток низкомолекулярного алканоила представляют собой неразветвленную или разветвленную алкильную группу, содержащую от одного до шести атомов углерода, такую как метил, этил, пропил, изопропил, бутил, изобутил, sec-бутил, трет-бутил, пентил, неопентил и гексил. 2. Соединение, Асмарин А, по п. 1, имеющее следующую формулу: 3. Соединение, Асмарин В, по п. 1, имеющее ...

ТРИЦИКЛИЧЕСКИЕ ИНДОЛОВЫЕ ПРОИЗВОДНЫЕ И ИХ ПРИМЕНЕНИЕ В ЛЕЧЕНИИ БОЛЕЗНИ АЛЬЦГЕЙМЕРА

... 1. Соединение формулы (I) где R1 и R2 независимо представляют собой С1-3алкил, С2-4алкенил, галоген, С1-3алкокси, амино, циано или гидрокси; m и n независимо равны 0, 1 или 2; р равно 1 или 2; А-В представляет собой -NR5-SO2- или -NR5-СО-; R5 представляет собой водород, С1-6алкил, С3-6алкенил, С3-6алкинил, С3-8циклоалкил, арил, гетероарил, арил-С1-6алкил, гетероарил-С1-6алкил, арил-С3-8циклоалкил или гетероарил-С3-8циклоалкил; Х-Y-Z представляет собой -N-CR8=CR9-; R8 представляет собой водород, С1-6алкил или С3-8циклоалкил; R9 представляет собой водород, С1-6алкил, С3-8циклоалкил, арил, гетероарил, арил-С1-6алкил, гетероарил-С1-6алкил, арил-С3-8циклоалкил, гетероарил-С3-8циклоалкил, -COOR10, -OR10, -CONR10R11, -SO2NR10R11, -СОС1-6алкил или -SO2 С1-6алкил (где R10 и R11 независимо представляют собой водород, С1-6алкил или С3-8циклоалкил); R3 представляет собой необязательно замещенный С1-6алкил, С2-6алкенил, С2-6алкинил, С1-6алкил-С3-8циклоалкил, С1-6алкиларил, С1-6алкилгетероарил или С1 ...

КОНДЕНСИРОВАННЫЕ ПРОИЗВОДНЫЕ АЗОЛПИРИМИДИНА

... 1. Конденсированное производное азолпиримидина формулы (I), его таутомерная или стереоизомерная форма или его соль где Х означает CR5 R6 или NH; Y1 означает CR3 или N; химическая связь между означает ординарную связь или двойную связь, при условии, что если означает двойную связь, то Y2 и Y3 независимо означают CR4 или N, и если означает ординарную связь, то Y2 и Y3 независимо означают CR3R4 или NR4; Z1, Z2, Z3 и Z4 независимо означают СН, CR2 или N; R1 означает арил, необязательно содержащий от 1 до 3 заместителей, выбранных из группы, включающей R11, С3-8циклоалкил, необязательно содержащий от 1 до 3 заместителей, выбранных из группы, включающей R11, C1-6алкил, необязательно содержащий в качестве заместителей арил, гетероарил, C1-6 алкоксиарил, арилоксил, гетероарилоксил или один или большее количество атомов галогенов, C1-6алкоксил, необязательно содержащий в качестве заместителей карбоксил, арил, гетероарил, C1-6алкоксиарил, арилоксил, гетероарилоксил или один или большее количество ...

Способ получения 4,5-дигидроимидазо- @ 4,5,1-J-к @ /1/-бензазепин-2,7-/1Н,6Н/-диона

Изобретение относится к гетероциклическим соединениям, в частности к получению 4,5-дигидроимидазо- 4,5, l-j-kjri 1 -бензазепин-2, В, 6Н -дио- на (1), обладающего высокой антиги- пертензивной, гипотензивной и сосудорасширяющей активностями. Цель - раз- работка способа получения новых промежуточных продуктов для синтеза соединений , обладающих фармакологи чески- ми свойствами. Получение соединения ...

Способ получения производных бензазепина или их солей

Способ получения циклических соединений или их солей

Verfahren zur Herstelung von Pirlindolehydrochlorid

CYCLOPENTA[B][1,4] DIAZEPINO[6,7,1-HI]INDOLE ALS 5HT2C ANTAGONISTEN

Verfahren zur Herstellung von Farbstoffen der Phthaloperinonreihe

PHARMACEUTICAL COMPOUNDS

Novel dibromodecafluoro-pentamethylene or hexamethylene-tetramine

Novel dibromodecafluoro-pentamethylene or hexamethylene-tetramine is capable in the presence of emulsifying agents of forming blood substitutes stable at room temperature and possessing enhanced oxygen carrying capacity.

Use of rnai inhibiting parp activity for the manufacture of a medicament for the treatment of cancer

Perinone dyes

... 1,132,646. Perinone dyes. SANDOZ Ltd. 14 Feb., 1966 [25 Feb., 1965; 5 Aug., 1965], No. 6346/66. Heading C4P. The invention comprises compounds of the formula where one of X and Y is a 1,8-naphthalene radical and the other is a 1,2-phenylene or 1,8- naphthalene radical, R 1 is a phenyl, naphthyl or cyclohexyl radical which may be substituted other than by carboxylic or sulphonic acid groups, n is 1 or 2 and X and Y may bear further monovalent substituents other than carboxylic or sulphonic acid groups. The compounds are prepared by acylating compounds of the formula with suitable carboxylic acids or functional derivatives thereof.

METHOD OF PRODUCING AN INDOLE DERIVATIVE

... 1340529 Process for 1,10-trimethylene-8- methyl - 1,2,3,4 - tetrahydropyrazino[1,2- a] indole and its hydrochloride VSESOJUZNY NAUCHNO-ISSLEDOVATESKY KHIMIKOFAKMATSEVTICHESKY INSTITUT IMENI SERGO ORDZHONIKIDZE 27 March 1971 11461/73 Divided out of 1340528 Heading C2C The invention comprises a method of producing 1,10 - trimethylene - 8 - methyl - 1,2,3,4- tetrahydropyrazino - [1,2 - a] - indole hydrochloride by reacting 1-keto-1,2,3,4-tetrahydro- 6-methylcarbazole with a base to form a derivative of 1-keto-1,2,3,4-tetrahydro-6-methylcarbazole, alkylating the derivative with chloroacetonitrile in the presence of an organic solvent to form 1-keto-1,2,3,4-tetrahydro-6-methyl-9- cyanmethyl-carbazole, effecting a reductive cyclization of the cyanmethylcarbazole with hydrogen in the presence of a hydrogenation catalyst and an organic solvent and at a pressure of 30 to 70 atmospheres and a temperature within the range from 30‹ to 60‹ C., and treating 'the resultant cyclized compound with hydrogen ...

ELECTROPHOTOGRAPHIC PHOTOCONDUCTORS

Serotoninergic abeo-ergoline derivatives

1-Alkoxy-polyalkyl-piperidine derivatives and their use as polymerization regulators

TRICYCLIC ALKYLAMINE DERIVATIVES AND PREPARATION THEREOF

... 1480679 Amines derived from carbazole, cyclopent[b]indole and cycloehpt[b]indole AYERST MCKENNA & HARRISON Ltd 13 June 1975 [18 June 1974] 25315/75 Heading C2C The invention comprises compounds of formula and their pharmaceutically acceptable acid addition salts, wherein R1 is C 1-6 alkyl; R2 is H or C 1-6 alkyl; R3 is H, halogen, C 1-6 alkyl, C 1-4 alkoxy, C 2-6 alkanoyloxy, OH, CF 3 , CCl 3 or CBr 3 ; R4 is H or C 1-6 alkyl; R5 and R6 are each H or C 1-6 alkyl; m is 2-4; p is 0-2; and "C 1-6 alkyl" excludes C 5-6 branched-chain alkyl. In examples, these compounds are prepared by reducing an amide in which the terminal group is CONR5R6 or CH 2 NR5CHO, or by hydrolysing the latter or the corresponding isocyanate (which is itself made from the azide). The amides are prepared by reacting the corresponding carboxylic compound, in the form of a mixed anhydride with EtOCO 2 H, with R5R6NH. Starting ...

Tricyclic inhibitors of ply (adp-robose) polymerases

Tricyclic inhibitors of poly(adp-ribose)polymerases.

NOVEL ANTIVIRAL TETRAHYDROIMIDAZO(1,4)BENZODIAZEPIN-2-(THI)ONES

Tricyclic inhibitors of poly (adp-ribose) polymerases.

Diazepinoindole derivatives as kinase inhibitors.

Novel antiviral tetrahydroimidazo (1,4) benzodiazepin-2-(thi) ones.

Novel tetrahydroimidazo{1,4}benzodiazepin-2-(thi)ones fo formulathe pharmaceutically acceptable acid addition salts and the stereochemically isomeric thereof wherein ...

Antiviral tetrahydroimidazo (1,4) benzodiazepines.

Novel tetrahydroimidazole (1,4) ...

Tricydic inhibitors of poly (ADP-Ribose) polymerases.

Antiviral tetrahydroimidazo[1,4]benzodiazepin-2-thiones.

Novel tetrahydroimidazo[1,4]benzodiazepen-2-thiones possessing antiviral activity. Compositions containing these compounds as active ingredient and methods of treating subjects suffering from viral infections by administering said compounds.

Diazepinoindole derivatives as kinase inhibitors

ANTIVIRAL TETRAHYDROIMIDAZOL(1.4)BENZODIAZEPIN-2-THIONES

ANTIVIRAL TETRAHYDROIMIDAZO(1,4)BENZODIA-ZEPINES

Tricyclic inhibitors of ply (adp-robose) polymerases

NOVEL ANTIVIRAL TETRAHYDROIMIDAZO(1,4)BENZODIAZEPIN-2-(THI)ONES

Diazepinoindole derivatives as kinase inhibitors.

METHOD FOR PREPARING SUBSTITUTED [1,4]DIAZEPINO[6,7,1-hi]INDOL-4-ONES.

The invention concerns a method for preparing enantiopure diazepino-indolone of formula (1) which consists in the intramolecular cyclisation of a product of formula (II) wherein A, B, X1, X2, Z, Z1, Z2 and R are as defined in the description, in the presence of a weak Lewis acid catalyst.

6-(5-HYDROXY-1H-PYRAZOL-1-YL) NICOTINAMIDA DERIVATIVES AND THEIR USE AS PHD INHIBITORS

Method for preparing substituted (1,4)diazepino (6,7,1 HI) indol 4 ones

Tetrahydro-imidazo [1,4] antiviral benzodiazepines

Method of preparation of Ä1,4ÜdiazépinoÄ6,7,1-hiÜindol-4-ones substituted.

Tricyclic inhibitors of poly(adp-ribose)polymerases.

"Tétrahydroimidazo (1,4) benzodiazépin-2-thiones antivirales".

News tétrahydroimidazo [1,4] benzodiazepine-2 (thi) ones antiviral.

Diazepinoindole derivatives as kinase inhibitors.

Tricyclic inhibitors of poly(adp-ribose)polymerases.

Saturated tricyclic-nitrogen-containing diones as cognition activators.

ANTIVIRAL TETRAHYDROIMIDAZO(1,4)BENZODIA-ZEPINES

ANTIVIRAL TETRAHYDROIMIDAZOL(1.4)BENZODIAZEPIN-2-THIONES

Diazepinoindole derivatives as kinase inhibitors.

6-(5-HYDROXY-1H-PYRAZOL-1-YL) NICOTINAMIDA DERIVATIVES AND THEIR USE AS PHD INHIBITORS

Tricyclic inhibitors of ply (adp-robose) polymerases

Method for preparing substituted (1,4)diazepino (6,7,1 HI) indol 4 ones

6-(5-HYDROXY-1H-PYRAZOL-1-YL) NICOTINAMIDA DERIVATIVES AND THEIR USE AS PHD INHIBITORS

PROCEDURE FOR THE PRODUCTION OF NEW PYRROLOCHINOXALINONEN AND PYRROLOBENZDIA ZEPINONEN

AS ANABOLE MEANS FOR CATTLE APTITUDE HETERO-CYCLIC CONNECTIONS

NEW INDAZOLVERBINDUNGEN WITH CONDENSED RING

IMPROVED CONNECTIONS FUR THE PRODUCTION OF CHEMILUMINESZENZ WITH A PEROXIDASE

TRICYCLI PARP HEMMER

PYRIDO(3,2,1-IJ)-1,3,4-BENZOXADIAZINDERIVATE UND DIESE ENTHALTENDE PHARMAZEUTISCHE PRAEPARATE

PROCEDURE FOR THE PRODUCTION OF PERYLEN-3,4: 9,10TETRACARBONSÄUREDIIMIDEN AND PERYLEN-3,4: 9,10TETRACARBONSÄUREDIANHYDRID AS WELL AS OF NAPHTHALIN-1,8-DICARBONSÄUREIMIDEN

ZOO-TECHNICAL COMPOSITIONS WITH CONTENT OF AN ADRENERGIC BETA RECEPTOR BLOCKER.

1-ALKOXYPOLYALKYLPIPERIDINDERIVATE UND IHRE VERWENDUNG ALS POLYMERISATIONSREGLER

TETRACYCLI INDOLDERIVATE.

USE OF PYRROL (3,2,1-HI>INDOL-DERIVATEN FOR the PRODUCTION of a DRUG FOR the TREATMENT OF DIABETES.

TRICYCLI INDOLDERIVATE, PRODUCTION AND APPLICATION AS DRUGS.

ANTIVIRAL ONE TETRAHYDROIMIDAZO (1,4>BENZODIAZEPIN-2 THIONE.

PYRROLO (3,2,1-HI) INDOLDERIVATE, ITS PRODUCTION AND YOUR THERAPEUTIC APPLICATION.

RESOLVENTS

BENZOKONDENSIERTE LACTAMS

PROCEDURE FOR the PRODUCTION OF ENANTIOMER PURE IMIDAZO (4,5,1-JK) (1,4) - BENZODIAZEPIN-2 (1H) - THIONEN

CYCLOPENTA (B) (1,4) DIAZEPINO (6,7,1-HI) INDOLE AS 5HT2C ANTAGONIST

Procedure for the production of new 1,2,8,9-Tetraazaphenalenen and their salts

BENZODIAZEPIN DERIVATIVES, THEIR PRODUCTION AND APPLICATION

NAPHTHALENEHYDRAZAMIMIDE AND PERYLENHYDRAZAMIMIDE

PROCEDURE FOR THE PRODUCTION OF ENANTIOMERISCH PURE IMIDAZOL CONNECTIONS

PROCEDURE FOR HERSTELUNG OF PIRLINDOLEHYDROCHLORID

ISOINDOLOINDOLON DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND THE CONTAINING PHARMACEUTICAL COMPOSITIONS

NEW TRICYCLI CONNECTIONS WITH ICE/CED-3 PROTEASE FAMILY-RESTRAINING CHARACTERISTICS

EXTENDED RHODAMINVERBINDUNGEN USABLE AS FLUORESCENT ONE MARKING MEANS

Procedure for the production of new 1,2,8,9-Tetraazaphenalenen and their physiologically acceptable acid addition salts

Procedure for the production of new 1-substituierter 1H-1,2,8,9-Tetraazaphenalene and their acid addition salts

PROCEDURE FOR the PRODUCTION OF SUBSTITUTING (1, 4) DIAZEPINO (6,7,1-HI) INDOL-4-ONE

AMINO-SUBSTITUTED BRIDGED AZABICYCLIC QUINOLONE CARBOXYLIC ACIDS AND ESTERS

ANTIVIRAL TETRAHYDROIMIDAZO(1,4)BENZODIAZEPIN-2-THIONES

TRICYCLIC NITROGEN-CONTAINING DIONES

TERT. ALKYLPHENOXY SUBSTITUTED POLYCYCLIC COMPOUNDS

Cyclopenta(b)(1,4) diazepino(6,7,1-hi)indoles as 5ht2c antagonists

Enantioselective synthesis of 6-amino-7-hydroxy-4, 5, 6, 7-tetrahydro-imidazo [4, 5, 1-jk] -benzazepin-2 -one and zilpaterol

Novel benzenesulfonamides as calcium channel blockers

The present application relates to calcium channel inhibitors comprising compounds of formula (I), formula (II), formula (III), or formula (IV), wherein L1, R1, R2, R3, R4, R5, R6, R7 and Rc are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.

METHOD FOR THE PRODUCTION OF PERYLEN-3,4:9,10-TETRACARBOXYLIC ACID DIIMIDES AND PERYLEN-3,4:9,10-TETRACARBOXYLIC ACID DIANHYDRIDE AND NAPHTALENE-1,8-DICARBOXYLIMIDES

PROCESSES FOR MAKING ZILPATEROL AND SALTS THEREOF

This invention generally relates to processes for making zilpaterol and salts thereof, as well as processes for making intermediates that, inter alia, may be used to make zilpaterol and salts thereof. This invention also relates to methods of treatment using zilpaterol and salts prepared in accordance with this invention to increase the rate of weight gain, improve feed efficiency, and/or increase carcass leanness in livestock, poultry, and fish. 115-. (canceled)16. A method of increasing the rate of weight gain in a bovine animal comprising administering a single oral daily dose of zilpaterol or a salt thereof in the bovine animal's feed wherein the concentration of the zilpaterol or salt thereof in the feed is between 0.01 ppm and 75 ppm.17. The method of claim 16 , wherein the zilpaterol salt is zilpaterol hydrochloride.18. The method of claim 16 , wherein the concentration of the zilpaterol or salt thereof in the feed is between 0.01 ppm and 38 ppm.19. The method of claim 16 , wherein the concentration of the zilpaterol or salt thereof in the feed is between 0.5 ppm and 20 ppm.20. The method of claim 16 , wherein the concentration of the zilpaterol or salt thereof in the feed is between 3 ppm and 8 ppm.21. The method of claim 16 , wherein the concentration of the zilpaterol or salt thereof in the feed is between 3.7 ppm and 7.5 ppm.22. The method of claim 16 , wherein the zilpaterol or salt thereof is administered in a daily dose of 0.01 mg/kg body weight to 50 mg/kg body weight.23. The method of claim 16 , wherein the zilpaterol or salt thereof is administered in a daily dose of 0.01 mg/kg body weight to 10 mg/kg body weight.24. The method of claim 16 , wherein the zilpaterol or salt thereof is administered in a daily dose of 0.05 mg/kg body weight to 2 mg/kg body weight.25. The method of claim 16 , wherein the zilpaterol or salt thereof is administered in a daily dose of 0.1 mg/kg body weight to 1 mg/kg body weight.26. The method of claim 16 , wherein the ...

Compositions and Methods for Treatment of Cancer

The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent. 115-. (canceled)1716. The pharmaceutical composition of , wherein said second chemotherapeutic agent is selected from the group consisting of tamoxifen , raloxifene , anastrozole , exemestane , letrozole , trastuzumab , imatinib , paclitaxel , cyclophosphamide , lovastatin , mimosine , gemcitabine , araC , 5-fluorouracil , methotrexate , docetaxel , goserelin , vinctristine , vinblastine , nocodazole , teniposide , etoposide , gemcitabine , epothilone , navelbine , camptothecin , daunorubicin , dactinomycin , mitoxantrone , amsacrine , doxorubicin , epirubicin or idarubicin.1826-. (canceled)28. The method of claim 27 , wherein said second chemotherapeutic agent is selected from the group consisting of tamoxifen claim 27 , raloxifene claim 27 , anastrozole claim 27 , exemestane claim 27 , letrozole claim 27 , trastuzumab claim 27 , imatinib claim 27 , paclitaxel claim 27 , cyclophosphamide claim 27 , lovastatin claim 27 , mimosine claim 27 , gemcitabine claim 27 , araC claim 27 , 5-fluorouracil claim 27 , methotrexate claim 27 , docetaxel claim 27 , goserelin claim 27 , vinctristine claim 27 , vinblastine claim 27 , nocodazole claim 27 , teniposide claim 27 , etoposide claim 27 , gemcitabine claim 27 , epothilone claim 27 , navelbine claim 27 , camptothecin claim 27 , daunorubicin claim 27 , dactinomycin claim 27 , mitoxantrone claim 27 , amsacrine claim 27 , doxorubicin claim 27 , epirubicin or idarubicin.29. The method of wherein said treating said cell proliferative ...

Novel pharmaceutical intermediates and methods for preparing the same

A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.

DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)

A compound having the structure set forth in Formula (I) and Formula (II): 3. The compound of wherein Y is an aryl group which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 R; or a single isomer claim 1 , stereoisomer claim 1 , or enantiomer claim 1 , or mixture thereof claim 1 , optionally as a salt thereof.4. The compound of wherein the aryl group is a phenyl group which is optionally substituted with 1 claim 3 , 2 claim 3 , or 3 R; or a single isomer claim 3 , stereoisomer claim 3 , or enantiomer claim 3 , or mixture thereof claim 3 , optionally as a salt thereof.5. The compound of wherein the phenyl group is substituted with 1 claim 4 , 2 claim 4 , or 3 Rselected from the group consisting of Br claim 4 , Cl claim 4 , F claim 4 , and I; or a single isomer claim 4 , stereoisomer claim 4 , or enantiomer claim 4 , or mixture thereof claim 4 , optionally as a salt thereof.6. The compound of wherein the phenyl group is substituted with 1 claim 4 , 2 claim 4 , or 3 Rselected from the group consisting of (NRR)C-Calkylene claim 4 , (NRR)carbonyl claim 4 , (NRR)carbonylalkylene claim 4 , (NRR)sulfonyl claim 4 , and (NRR)sulfonylalkylene; or a single isomer claim 4 , stereoisomer claim 4 , or enantiomer claim 4 , or mixture thereof claim 4 , optionally as a salt thereof.7. The compound of wherein Ris (NRR)C-Calkylene; or a single isomer claim 6 , stereoisomer claim 6 , or enantiomer claim 6 , or mixture thereof claim 6 , optionally as a salt thereof.8. The compound of wherein Rand Rare each independently hydrogen claim 7 , C-Calkyl claim 7 , or C-Ccycloalkyl; or a single isomer claim 7 , stereoisomer claim 7 , or enantiomer claim 7 , or mixture thereof claim 7 , optionally as a salt thereof.9. The compound of wherein (NRR) is azetidine claim 7 , pyrrolidine claim 7 , piperidine or morpholine; or a single isomer claim 7 , stereoisomer claim 7 , or enantiomer claim 7 , or mixture thereof claim 7 , optionally as a salt thereof.10. The compound of wherein Ris ...

Flindersia Alkaloids, Derivatives and Analogs: Compositions and Methods for Producing the Same

The present invention provides methods for chemically synthesizing naturally-occurring alkaloids, for example, alkaloids, and their analogs and derivatives. Generally, the precursor borrerine is synthesized from tryptamine in the presence of an alkylating agent, an acylating agent and a reducing agent and dimerized in the presence of an acid, for example, tetrafluoroacetic acid, hydrochloric acid or acetic acid to yield the products. Analog and derivative compounds are produced by derivatizing one or more of the tryptamine, alkylating agent or acylating agent. Also provided are the synthetic alkaloids and derivatives and analogs thereof produced by the synthetic methods. 1. A method for chemically synthesizing a naturally occurring alkaloid compound , comprising the steps of:synthesizing a precursor of the alkaloid compound; anddimerizing the synthesized precursor in the presence of an acid to yield the synthetic alkaloid compound.2. The method of claim 1 , wherein the precursor is borrerine claim 1 , said synthesizing step comprising:adding an alkylating agent to tryptamine or to a derivative thereof;adding an acylating agent in the presence of a base to form a substituted piperidinyl-N-carbamate intermediate; andadding a strong reducing agent to the intermediate to produce borrerine.3. The method of claim 2 , wherein the tryptamine is derivatized independently at one or more of C4 claim 2 , C5 claim 2 , C6 claim 2 , and C7 with hydroxy claim 2 , methoxy claim 2 , acetoxy claim 2 , benzyloxy claim 2 , sulfomethyl claim 2 , amino claim 2 , acetate claim 2 , methyl claim 2 , ethyl claim 2 , iso-propyl claim 2 , t-butyl claim 2 , trifluoromethyl claim 2 , cyano claim 2 , methylformate claim 2 , nitrate claim 2 , or halide.4. The method of claim 2 , wherein the alkylating agent is 3-methyl 2-butenal claim 2 , the acylating agent is methyl chloroformate and the strong reducing agent is lithium aluminum hydride.5. The method of claim 2 , wherein the alkylating agent is ...

SUBSTITUTED INDOLES, ANTIVIRAL ACTIVE COMPONENT, METHOD FOR PREPARATION AND USE THEREOF

The invention relates to novel antiviral active components of the general formula 1, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatisis C viruses (HCV). In the general formula 1 58-. (canceled)9. A medicament in the form of a tablet claim 1 , a sheath or an injection placed in a pharmaceutically acceptable package for prophylaxis or treating a viral disease caused by hepatitis C virus (HCV) comprising a pharmaceutical composition of .10. (canceled)11. A method for treating a viral disease caused by hepatisis C viruses (HCV) claim 1 , comprising administering a pharmaceutical composition of in an effective amount to a subject in need thereof. The present invention relates to novel antiviral component, pharmaceutical composition, antiviral medicament, method for prophylaxis and treatment of viral diseases, particularly caused by hepatitis C virus (HCV).Virus infections may cause a great number of diseases that create a serious threat for health and existence of mankind For the last 20 years no less than 30 essentially new infectious agents have been discovered such as: HIV, viral hepatitises, acute and long-lasting diarrhea, hemorrhagic fever (Ebola, Venezuelan, Brazilian, Rift valleys) [a) Lednicky J. A., Rayner J. O. Uncommon respiratory pathogens. 2006, 12(3), 235-239. b) Hayden F. G. Respiratory viral threats. 2006, 19(2), 169-178]. In particular, special anxiety is caused by the risk of infection by so named avian influenza. [a) Liu J. P. Avian influenza—a pandemic waiting to happen? 2006, 39(1), 4-10. b) Henter J. I.; Chow C. B.; Leung C. W, Lau Y. L. Cytotoxic therapy for severe avian influenza A (H5N1) infection. 2006 367(9513), 870-873. Review]. According to statistical data 60-65% of epidemic infections have viral ethiology. Because of the complexity of interaction in triad “virus—host's organism—drug”, most of modern antiviral drugs display side effects in the course of ...

SELECTIVE BROMINATION OF PERYLENE DIIMIDES AND DERIVATIVES THEREOF UNDER MILD CONDITIONS

The present invention is directed to novel process for the preparation of regioselective perylenediimides derivatives, specifically mono and dibrominated derivatives. 2. The compound of claim 1 , wherein said metal or metal ion comprises Pd claim 1 , Pt claim 1 , Fe claim 1 , Cu claim 1 , Ag claim 1 , Rh claim 1 , Ir claim 1 , Ru or Os.3. The compound of claim 1 , wherein said metal or metal ion is coordinated to a chelating group. This application is a Divisional application from United-States application Serial No. 12/599,292 filed Jun. 22, 2010, which is a National Phase application from International Application Number PCT/IL2008/000621 filed May 6, 2008 which claims the benefit of U.S. Ser. No. 60/924,327 filed May 9, 2007, each of which is hereby incorporated by reference in its entirety.The present invention is directed to novel processes for the regioselective preparation of perylenediimides derivatives, specifically mono and dibrominated derivatives.Perylene-diimides (PDIs) are outstanding versatile organic chromophores. They demonstrate exceptional thermal and photochemical stability, strongly absorb visible light, and show high fluorescence quantum yields. PDIs have been utilized as industrial dyes, electronic materials, sensors, photovoltaics, and building blocks for light-harvesting and artificial photosynthetic systems Importantly, photophysical and redox properties of PDIs can be conveniently modified through substitution in the aromatic core at the positions 1, 6, 7, and 12 (bay region). Substitutions at bay positions and expansion of the PDI core are usually carried out starting from the halogenated derivatives, particularly brominated PDIs. These are almost exclusively synthesized through bromination of perylene dianhydride (PDA) in concentrated HSOupon heating, followed by imidation with amines. Usually this bromination procedure affords a mixture of di-, tri- and tetrabrominated PDIs. The dibromoperylene diimides contain 1,7 (major) and 1,6 ( ...

Macrocyclic Indoles as Hepatitis C Virus Inhibitors

The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, 7. A compound according to claim 1 , wherein each of c claim 1 , d claim 1 , e claim 1 , f claim 1 , g claim 1 , and h claim 1 , is claim 1 , independently claim 1 , 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3 claim 1 , with the proviso that the macrocycle formed by the bivalent chain R claim 1 , the —C(═O)—NH— moiety to which Ris attached and the nitrogen and carbon atoms N1 claim 1 , C6 claim 1 , C7 claim 1 , and C7′ of the indole ring claim 1 , has from 14 to 16 member atoms.8. A compound according to claim 1 , wherein Ris hydrogen or Calkyl.9. A pharmaceutical composition comprising an anti-virally effective amount of a compound as claimed in and a pharmaceutically acceptable carrier.1015.-. (canceled) The present invention is concerned with macrocyclic indoles having inhibitory activity on the replication of the hepatitis C virus (HCV). It further concerns compositions comprising these compounds as active ingredients as well as processes for preparing these compounds and compositions.Hepatitis C virus is the leading cause of chronic liver disease worldwide and has become a focus of considerable medical research. HCV is a member of the Flaviviridae family of viruses in the hepacivirus genus, and is closely related to the genus, which includes a number of viruses implicated in human disease, such as dengue virus and yellow fever virus, and to the animal pestivirus family, which includes bovine viral diarrhoea virus (BVDV). HCV is a positive-sense, single-stranded RNA virus, with a genome of around 9,600 bases. The genome comprises both 5′ and 3′ untranslated regions which adopt RNA secondary structures, and a central open reading frame that encodes a single polyprotein of around 3,010-3,030 amino acids. The polyprotein encodes ten gene products which ...

Highly Pure Pyrroloquinolinyl-Pyrrole-2,5-Dione and Pyrroloquinolinyl-Pyrrolidine-2,5-Dione and Methods of Preparing Same

The present invention relates to highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin--yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. The present invention also relates to methods for preparing highly-pure pyrroloquinolinyl-pyrrole-2,5-dione and pyrroloquinolinyl-pyrrolidine-2,5-dione, for example, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione, 3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, and pharmaceutically acceptable salts, solvates, and diastereomers thereof. 2. The method of claim 1 , wherein the organic solvent is an ether claim 1 , a hydrocarbon claim 1 , or an amide.3. The method of claim 1 , wherein the organic solvent is an ether.4. The method of claim 1 , wherein the organic solvent is dimethyl ether claim 1 , diethyl ether claim 1 , tetrahydrofuran claim 1 , toluene claim 1 , hexane claim 1 , dimethylformamide claim 1 , or dimethylacetamide.5. The method of claim 1 , wherein the organic solvent is tetrahydrofuran.6. The method of claim 1 , wherein the base is an inorganic base or a metal base.7. The method of claim 1 , wherein the base is a metal hydroxide or a metal alkoxide.8. The method of claim 1 , wherein the base is an metal alkoxide.9. The method of claim 1 , wherein the base is sodium hydroxide claim 1 , potassium hydroxide claim 1 , potassium tert-butoxide claim 1 , sodium tert-butoxide claim 1 , lithium hexamethyldisilazide claim 1 , sodium hexamethyldisilazide claim 1 , or lithium diisopropylamide.10. The method of claim 1 , wherein the base is potassium tert-butoxide.11. The method of claim 1 , wherein the base is dissolved or suspended in an organic solvent.12. The method of claim 11 , wherein the ...

Tetraazaperopyrene compounds and their use as n-type semiconductors

A tetraazaperopyrene compound of formula (I): wherein: R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 at each occurrence, independently are selected from H, Cl and Br, with the proviso that at least one of R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , Wand R 8 is Cl or Br, R 9 , R 10 , at each occurrence, independently are selected from H, a C 1-30 alkyl group, a C 1-30 haloalkyl group, a C 6-14 aryl group, a heteroaryl group having 5 to 14 ringatoms, and a C 7-20 arylalkyl group, wherein aryl, heteroaryl and arylalkyl can be optionally substituted with one or more halogen, C 1-4 haloalkyl, —CN, —NO 2 , —CHO, —COOH, —CONH 2 , —CO(C 1-14 alkyl), —COO(C 1-14 alkyl), —CONHC(C 1-14 alkyl) and —CON(C 1-14 alkyl) 2 groups.

ASYMMETRICALLY SUBSTITUTED ANTHRAPYRIDAZONE DERIVATIVES AS CYTOSTATICS

The invention relates to the new, asymmetrically substituted derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione and their use as cytostatics exhibiting activity against tumor cells, especially against cells with multidrug resistance (MDR). In particular, the invention concerns derivatives of 2,7-dihydro-3H-dibenzo[de,h]cinnoline-3,7-dione represented by the general formula (I). 6. Anthrapyridazone derivatives according to selected from the group comprising:2-[2-(Dimethylamino)ethyl]-6-{[2-(methylamino)ethyl]amino}-2,7-dihydro-3H-dibenzo[de,h]cynnoline-3,7-dione,2-[2-(Dimethylamino)ethyl]-6-[2-(aminoethypamino)-2,7-dihydro-3H-dibenzo [de,h]cynnoline-3,7-dione,2-[2-(Dimethylamino)ethyl]-6-(N-methylamino)-2,7-dihydro-3H-dibenzo[de,h]cynnoline-3,7-dione,2-[2-(Dimethylamino)ethyl]-6-{[2-(ethylamino)ethyl]amino}2,7-dihydro-3H-dibenzo [de,h]cynnoline-3,7-dione,2-[2-(Dimethylamino)ethyl]-6-[(3-aminopropyl)amino]-2,7-dihydro-3H-dibenzo[de,h]cynnoline-3,7-dione,2-[2-(Dimetyloamino)etyl]-6-[(3-acetyloaminopropyl)amino]-2,7-dihydro 3H-dibenzo [de,h]cynnolino-3,7-dione,2-[2-(dimethylamino)ethyl]-6-(acetylamino)-2,7-dihydro-3H-dibenzo[de,h]cynnoline 3,7-dione,2-[2-(Dimethylamino)ethyl]-6-{[(2-diethylamino)ethyl]amino}2,7-dihydro 3H -dibenzo[de,h]cynnoline-3,7-dione,2-[2-(Dimethylamino)ethyl]-6-(N-benzylamino)-2,7-dihydro-3H-dibenzo[de,h]cynnoline-3,7-dione,2-[2-(Dimethylamino)ethyl]-6-[2-(2-aminoethylamino)etanolo]-2,7-dihydro 3H -dibenzo [de,h]cynnoline-3,7-dione,2-[2-(Dimethylamino)ethyl]-6-[(N,N-dimethyloacetamido)amino]-2,7-dihydro-3H-dibenzo [de,h]cynnolin-3,7-dione,2-[2-(Dimethylamino)propyl]-6-{[2-(dimethylamino)propyl]amino}-2,7dihydro-3H-dibenzo[de,h]cynnoline-3,7-dione,2-(2-Morpholinethyl)-6-amino-2,7-dihydro-3H-dibenzo[de,h]cynnoline 3,7-dione,2-[3-(Dimethylamino)propyl]-6-amino-2,7-dihydro-3H-dibenzo[de,h]cynnoline-3,7-dione,2-[2-(Piperidinamino)ethylo]-6-amino-2,7-dihydro-3H-dibenzo[de,h]cynnoline-3,7-dione,{'b': '0', '2-(2-Hydroxyethyl)-6-(2- ...

Purified Pyrroloquinolinyl-Pyrrolidine-2,5-Dione Compositions and Methods for Preparing and Using Same

The present invention relates to a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. The present invention also relates to (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds having a chiral purity greater than 99%, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising these (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a composition comprising (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione having a chiral purity greater than 99% or a form 1 and form 2 polymorph of (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione. 1. A method for preparing (−)-trans-3-(5 ,6-dihydro-4H-pyrrolo[3 ,2 ,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2 ,5-dione , comprising:a. mixing (±)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione with (1S,2S)-(+)-pseudoephedrine in a first solvent to form solid (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.(1S,2S)-(+)-pseudoephedrine;b. washing the (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.(1S,2S)-(+)-pseudoephedrine solid formed in step (a) with an aqueous mixture of the first solvent;c. reacting the (−)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione.(1S,2S)-(+)-pseudoephedrine from step (b) with an acid in an organic solvent and isolating the organic layer of the resultant solution;d. washing the ...

Pharmaceutical Compositions for the Treatment of Capillary Arteriopathy

The present invention relates to the use of ergot derivatives or ergolines, and in particular of lisuride and terguride for the prophylaxis and treatment of constrictive capillary arteriopathy. Constrictive capillary arteriopathy refers to the diseases pulmonary arterial hypertension, endogenously induced or exogenously induced glomeruloscleroses as well as secondary Raynaud's syndrome. 2. Use according to claim 1 , wherein the constrictive capillary arteriopathy refers to the following diseases: pulmonary arterial hypertension claim 1 , endogenously induced or exogenously induced glomeruloscleroses as well as secondary Raynaud's syndrome.3. Use according to claim 2 , wherein the compounds having the general formula (I) are lisuride or terguride.4. Pharmaceutical compositions claim 2 , comprising at least one compound having the general formula (I) in a concentration of active substances of 0.1 to 10 mg per single dose together with pharmacologically compatible carriers claim 2 , auxiliary substances and/or solvents.5. Pharmaceutical composition according to claim 4 , wherein the pharmaceutical composition is suitable for oral claim 4 , sublingual claim 4 , parenteral claim 4 , cutaneous claim 4 , buccal claim 4 , percutaneous claim 4 , subcutaneous claim 4 , inhalative or nasal administration.6. Pharmaceutical composition according to or provided as tablets claim 4 , layered tablets claim 4 , capsules claim 4 , retard-oral medicines claim 4 , transdermal systems claim 4 , suppositories claim 4 , micro-formulations claim 4 , nano-formulations claim 4 , liposomal formulations claim 4 , drops claim 4 , nose drops claim 4 , nose sprays claim 4 , aerosols claim 4 , ampoules claim 4 , solutions claim 4 , emulsions claim 4 , dispersions claim 4 , powders claim 4 , inhalation powders claim 4 , micro-crystalline formulations claim 4 , inhalation sprays claim 4 , transdermal systems or subcutaneous formulations. The present invention relates to the use of ergot derivatives ...

DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) FOR USE IN TREATMENT OF DISEASES ASSOCIATED WITH A PTEN DEFICIENCY

A compound having the structure set forth in Formula (I) and Formula (II): 3. The method of wherein Y is a heteroaryl group optionally substituted with 1 claim 1 , 2 claim 1 , or 3 R.4. The method of wherein the heteroaryl group is selected from the group consisting of furan claim 3 , pyridine claim 3 , pyrimidine claim 3 , pyrazine claim 3 , imidazole claim 3 , thiazole claim 3 , isothiazole claim 3 , pyrazole claim 3 , triazole claim 3 , pyrrole claim 3 , thiophene claim 3 , oxazole claim 3 , isoxazole claim 3 , 1 claim 3 ,2 claim 3 ,4-oxadiazole claim 3 , 1 claim 3 ,3 claim 3 ,4-oxadiazole claim 3 , 1 claim 3 ,2 claim 3 ,4-triazine claim 3 , indole claim 3 , benzothiophene claim 3 , benzoimidazole claim 3 , benzofuran claim 3 , pyridazine claim 3 , 1 claim 3 ,3 claim 3 ,5-triazine claim 3 , thienothiophene claim 3 , quinoxaline claim 3 , quinoline claim 3 , and isoquinoline; each of which is optionally substituted with 1 claim 3 , 2 claim 3 , or 3 R.5. The method of wherein the heteroaryl group is substituted with C-Calkyl selected from the group consisting of methyl claim 4 , ethyl claim 4 , n-propyl claim 4 , iso-propyl claim 4 , n-butyl claim 4 , iso-butyl claim 4 , and tert-butyl.6. The method of wherein C-Calkyl is methyl.7. The method of wherein Z is an aryl group which is optionally substituted with 1 claim 1 , 2 claim 1 , or 3 R.8. The method of wherein the aryl group is a phenyl group which is optionally substituted with 1 claim 7 , 2 claim 7 , or 3 R.9. The method of any of wherein the phenyl group is substituted with 1 claim 8 , 2 claim 8 , or 3 Rselected from the group consisting of Br claim 8 , Cl claim 8 , F claim 8 , and I.10. The method of wherein Ris F.11. The method of wherein Ris selected from the group consisting of F claim 1 , Cl claim 1 , Br claim 1 , and I.12. The method of wherein Ris F.13. The method of where the compound is selected from the group consisting of:8,9-diphenyl-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one;8,9-bis(4- ...

TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES

The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor. 2. The compound as claimed in claim 1 , wherein at least one hydrogen atom has been replaced by a deuterium atom.3. The compound as claimed in any of the preceding claims claim 1 , where Ris selected from hydrogen and C-C-alkyl and is preferably hydrogen.4. The compound as claimed in any of the preceding claims claim 1 , where Ris selected from cyano claim 1 , nitro claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy and fluorinated C-C-alkoxy claim 1 , and preferably from C-C-alkyl.5. The compound as claimed in any of the preceding claims claim 1 , where Rand R claim 1 , independently of each other claim 1 , are selected from hydrogen claim 1 , cyano claim 1 , nitro claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy and fluorinated C-C-alkoxy.6. The compound as claimed in claim 5 , where Ris selected from hydrogen claim 5 , cyano claim 5 , nitro claim 5 , C-C-alkyl claim 5 , fluorinated C-C-alkyl claim 5 , C-C-alkoxy and fluorinated C-C-alkoxy claim 5 , and Ris hydrogen.7. The compound as claimed in claim 6 , where Ris selected from hydrogen and methyl claim 6 , and Ris hydrogen.8. The compound as claimed in claim 7 , where Rand Rare hydrogen.9. The compound as claimed in any of the preceding claims claim 7 , where Rand R claim 7 , independently of each other claim 7 , are selected from hydrogen claim 7 , C-C-alkyl and fluorinated C-C-alkyl or form together a group ═O claim 7 , and are preferably hydrogen or form together a group ═O claim ...

TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES

The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor. 2. The compound as claimed in claim 1 , wherein at least one hydrogen atom has been replaced by a deuterium atom.3. The compound as claimed in any of the preceding claims claim 1 , where Ris selected from hydrogen and C-C-alkyl and is preferably hydrogen.4. The compound as claimed in any of the preceding claims claim 1 , where Ris selected from cyano claim 1 , nitro claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy and fluorinated C-C-alkoxy claim 1 , and preferably from C-C-alkyl.5. The compound as claimed in any of the preceding claims claim 1 , where Rand R claim 1 , independently of each other claim 1 , are selected from hydrogen claim 1 , cyano claim 1 , nitro claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy and fluorinated C-C-alkoxy.6. The compound as claimed in claim 5 , where Ris selected from hydrogen claim 5 , cyano claim 5 , nitro claim 5 , C-C-alkyl claim 5 , fluorinated C-C-alkyl claim 5 , C-C-alkoxy and fluorinated C-C-alkoxy claim 5 , and Ris hydrogen.7. The compound as claimed in claim 6 , where Ris selected from hydrogen and methyl claim 6 , and Ris hydrogen.8. The compound as claimed in claim 7 , where Rand Rare hydrogen.9. The compound as claimed in any of the preceding claims claim 7 , where Rand R claim 7 , independently of each other claim 7 , are selected from hydrogen claim 7 , C-C-alkyl and fluorinated C-C-alkyl or form together a group ═O claim 7 , and are preferably hydrogen or form together a group ═O claim ...

TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES

The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor. 2. The compound as claimed in claim 1 , wherein at least one hydrogen atom has been replaced by a deuterium atom.3. The compound as claimed in any of the preceding claims claim 1 , where Ris selected from hydrogen and C-C-alkyl and is preferably hydrogen.4. The compound as claimed in any of the preceding claims claim 1 , where Ris selected from cyano claim 1 , nitro claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy and fluorinated C-C-alkoxy claim 1 , in particular from C-C-alkyl and especially from methyl.5. The compound as claimed in any of the preceding claims claim 1 , where Rand R claim 1 , independently of each other claim 1 , are selected from hydrogen claim 1 , cyano claim 1 , nitro claim 1 , C-C-alkyl claim 1 , fluorinated C-C-alkyl claim 1 , C-C-alkoxy and fluorinated C-C-alkoxy.6. The compound as claimed in claim 5 , where Ris selected from hydrogen claim 5 , cyano claim 5 , nitro claim 5 , C-C-alkyl claim 5 , fluorinated C-C-alkyl claim 5 , C-C-alkoxy and fluorinated C-C-alkoxy claim 5 , and Ris hydrogen.7. The compound as claimed in claim 6 , where Ris selected from hydrogen and methyl claim 6 , and Ris hydrogen.8. The compound as claimed in claim 7 , where Rand Rare hydrogen.9. The compound as claimed in any of the preceding claims claim 7 , where Rand R claim 7 , independently of each other claim 7 , are selected from hydrogen claim 7 , C-C-alkyl and fluorinated C-C-alkyl or form together a group ═O claim 7 , and are in particular hydrogen or ...

Dihydro-6-Azaphenalene Derivatives for the Treatment of CNS, Oncological Diseases and Related Disorders

In one embodiment, the present application discloses 2-aza-, 2-oxa- and 2-thia-2,3-dihydro-6-azaphenalene compounds and compositions, and methods for treating a neurological disease in a patient in need thereof using the compounds and compositions as disclosed herein. 2. The compound of claim 1 , wherein Xis —OH.3. The compound of claim 1 , wherein Xis —NR claim 1 , wherein Ris substituted or unsubstituted Calkyl or a substituted or unsubstituted —Calkyl-Caryl.4. The compound of claim 3 , wherein Ris Calkyl-X claim 3 , wherein X is selected from the group consisting of I claim 3 , I claim 3 , I claim 3 , H claim 3 , I claim 3 , F claim 3 , F claim 3 , Br and Br.5. The compound of claim 4 , wherein X is F.6. The compound of claim 1 , wherein Aand Aare each independently —C(O)— or —CH—.7. The compound of claim 1 , wherein R claim 1 , R claim 1 , Rand Rare hydrogen.8. The compound of claim 1 , wherein Ris H or selected from the group consisting of methyl claim 1 , ethyl claim 1 , propyl claim 1 , allyl claim 1 , propargyl and N-benzyl.10. The compound of claim 9 , wherein Xis OH and R claim 9 , R claim 9 , Rand Rare hydrogen.11. The compound of claim 10 , wherein Ris selected from the group consisting of Calkyl and substituted or unsubstituted —Calkyl-Caryl.12. The compound of claim 9 , wherein:{'sup': '1', 'Xis —OH;'}{'sup': 10', '11', '12, 'R, Rand Rare hydrogen;'}{'sup': '3', 'sub': 1-6', '6-10', '1-6', '6-10, 'Ris —Calkyl-Caryl or —Calkyl-Caryl-X; and'}{'sup': '13', 'sub': 2', '3', '1-6', '1-6', '1-6', '1-6', '2', 'n', '2', 'm', '1-6', '1-6', '2', 'n', '1-6', '1-6', '3-10', '3-10, 'Ris H or is selected from the group consisting of —OR′, —SR′, —NR′R″, —COR′, —SOR′, —Calkyl-SH, substituted or unsubstituted Calkoxy-, substituted or unsubstituted CalkylC(O)—, substituted or unsubstituted CalkylC(S)—,—(CH)—NH—(CH)—NR′R″, CalkylC(NR′)—, CalkylC(NOH)—,—(CH)—C(NOH)—Calkyl, —Calkyl-Cheteroaryl and —Cheteroaryl.'}13. The compound of claim 9 , wherein Ris Calkyl-X claim 9 , ...

Use of RNAI Inhibiting PARP Activity for the Manufacture of a Medicament for the Treatment of Cancer

The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination. 132-. (canceled)33. A method of treatment of cancer cells defective in homologous recombination (HR) in a human patient , the method comprising;administering to the patient a therapeutically effective amount of a compound which inhibits PARP-1.34. The method of wherein the PARP inhibitor is selected from the group consisting of benzimidazole-carboxamides claim 33 , quinazolin-4-[3H]-ones and isoquinolone derivatives.35. The method of wherein the PARP inhibitor is selected from the group consisting of 2-(4-hydroxyphenyl)benzimidazole-4-carboxamide claim 34 , 8-hydroxy-2-methylquinazolin-4-[3H]one claim 34 , 6(5H)phenanthridinone claim 34 , 3-aminobenzamide claim 34 , benzimidazole-4-carboxamides and tricyclic lactam indoles.36. The method of wherein the cancer cells have defect in a gene encoding a protein involved in HR.37. The method of wherein the human patient has one functional allele of said gene claim 36 , said functional allele being lost in the cancer cells.38. The method of wherein the gene encoding a protein involved in HR is selected from the group consisting of XRCC1 claim 33 , CTPS claim 33 , RPA claim 33 , RPA1 claim 33 , RPA2 claim 33 , RPA3 claim 33 , XPD claim 33 , ERCC1 claim 33 , XPF claim 33 , MMS19 claim 33 , RAD51 claim 33 , RAD51B claim 33 , RAD51C claim 33 , RAD51D claim 33 , DMC1 claim 33 , XRCC2 claim 33 , XRCC3 claim 33 , BRCA1 claim 33 , BRCA2 claim 33 , RAD52 claim 33 , RAD54 claim 33 , RAD50 claim 33 , MRE11 claim 33 , NBS1 claim 33 , WRN claim 33 , BLM claim 33 , Ku70 claim 33 , Ku80 claim 33 , ATM claim 33 , ATR claim 33 , chkl claim 33 , chk2 claim 33 , FANCA claim 33 , FANCB claim 33 , FANCC claim 33 , FANCD1 claim 33 , FANCD2 claim 33 , FANCE claim 33 , FANCF claim ...

SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO)METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE

The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer. 17-. (canceled)8. A process for preparing a solid dosage form containing a camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1 ,3 ,4 ,5-tetrahydro-6H-azepino[5 ,4 ,3-cd]indol-6-one , comprisingi) preparing a first vessel comprising 8-fluoro-2-{4-[(methylamino)methyl] phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one and a first solvent comprising one or more of water, an alcohol, and an ether;ii) preparing a second vessel comprising camphor sulfonic acid and a second solvent comprising one or more of water, an alcohol, and an ether;iii) combining the contents of the first vessel and the second vessel to form a camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one; andiv) isolating the camsylate salt formed in step iii);v) combining the isolated camsylate salt with one or more of a pharmaceutically acceptable carrier, a pharmaceutically acceptable diluent, a pharmaceutically acceptable vehicle, or a pharmaceutically acceptable excipient; andvi) preparing the solid dosage form by one or more processes selected from mixing, granulating, and compressing.9. The process of wherein the camphor sulfonic acid is S-camphor sulfonic acid.10. The process of wherein the camphor sulfonic acid is R-camphor sulfonic acid.11. The process of wherein the camphor sulfonic acid comprises a ratio of R-camphor sulfonic acid and S-camphor sulfonic acid.12. The process of wherein the camphor sulfonic acid is selected from 1R:1S-camphor sulfonic acid claim 11 , 1R:9S-camphor sulfonic acid claim 11 , 1R ...

ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE

An organic electroluminescence device comprising a cathode, an anode and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a fluorescent emitting layer and the fluorescent emitting layer comprises at least one first compound selected from the compounds represented by formulae (19), (21), (22), and (23), a second compound selected from the compounds represented by formula (3a), and a dopant material selected from the compounds represented by formulae (D1) and (D2) is excellent in its performance. 2. The organic electroluminescence device according to claim 1 , wherein the content of the second compound in the fluorescent emitting layer is less than that of the first compound in the fluorescent emitting layer.3. The organic electroluminescence device according to claim 1 , wherein the content of the second compound in the fluorescent emitting layer is 30% by mass or less based on a total amount of the first compound claim 1 , the second compound claim 1 , and the dopant material.4. The organic electroluminescence device according to claim 1 , wherein the content of the dopant material in the fluorescent emitting layer is 10% by mass or less based on a total amount of the first compound claim 1 , the second compound claim 1 , and the dopant material.10. The organic electroluminescence device according to claim 7 , wherein at least one of R claim 7 , R claim 7 , R claim 7 , R claim 7 , and Rof formula (1) does not form a substituted or unsubstituted ring structure having 3 or more ring atoms.20. The organic electroluminescence device according to claim 7 , wherein Rand Rof formula (1) are bonded to each other to form at least two substituted or unsubstituted ring structures each having 3 or more ring atoms.21. The organic electroluminescence device according to claim 7 , wherein{'sub': 1', '2', '2', '3, 'a pair of Rand Rand a pair of Rand R;'}{'sub': 4', '5', '5', '6, 'a pair of Rand Rand a pair of Rand R;'}{'sub': 5', '6', ...

Organic electroluminescence element and electronic apparatus

An organic electroluminescence device comprising a cathode, an anode and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a fluorescent emitting layer and the fluorescent emitting layer comprises a first compound, a second compound having a hole mobility larger than that of the first compound, and a dopant material showing a fluorescent spectrum with a half width of 30 nm or less; and an organic electroluminescence device comprising a cathode, an anode and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a fluorescent emitting layer and the fluorescent emitting layer comprises a first compound, a third compound having an affinity larger than that of the first compound, and a dopant material showing a fluorescent spectrum with a half width of 30 nm or less and the content of the third compound in the fluorescent emitting layer is less than that of the first compound in the fluorescent emitting layer are excellent in their performance.

FUSED CYCLIC COMPOUND, AND PREPARATION METHOD AND USE THEREOF

The invention relates to a fused cyclic compound having a structure of Formula compound by controlling conjugation of aromatic and heterocyclic rings. The electron transport performance balances while hole performance of the fused cyclic compound improves. The compound has high triplet energy level and glass transition temperature. The material molecule isn't prone to crystallization. The compound ensures transfer of energy to a guest material. Adjusting substituents improves electron and hole transport performances, reducing the difference between energy levels, broadening the recombination region of carriers, and preventing triplet-triplet exciton annihilation. The invention also relates to an organic light-emitting device having at least one functional layer containing the fused cyclic compound used as a host material in a light emitting layer. The energy level of the light emitting layer becomes matched with that of the carrier transport layers, reducing the driving voltage of the device while increasing luminescence efficiency of the device. 2. The fused cyclic compound according to claim 1 , wherein{'sub': 1', '2', '1', '30', '2', '30', '2', '30', '3', '30', '1', '30', '1', '30', '6', '60', '3', '30, 'Rand Rare each independently selected from hydrogen, halo, cyano, a C-Csubstituted or unsubstituted alkyl group, a C-Csubstituted or unsubstituted alkenyl group, a C-Csubstituted or unsubstituted alkynyl group, a C-Csubstituted or unsubstituted cycloalkyl group, a C-Csubstituted or unsubstituted alkoxy group, a C-Csubstituted or unsubstituted silyl group, a C-Csubstituted or unsubstituted aryl group, or a C-Csubstituted or unsubstituted heteroaryl group;'}{'sub': 1', '1', '30', '2', '30', '2', '30', '3', '30', '1', '30', '1', '30', '6', '60', '3', '30, 'Aris selected from hydrogen, halo, cyano, a C-Csubstituted or unsubstituted alkyl group, a C-Csubstituted or unsubstituted alkenyl group, a C-Csubstituted or unsubstituted alkynyl group, a C-Csubstituted or ...

CRYSTALLINE (8S,9R)-5-FLUORO-8-(4-FLUOROPHENYL)-9-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-8,9-DIHYDRO-2H-PYRIDO[4,3,2-DE]PHTHALAZIN-3(7H)-ONE TOSYLATE SALT

Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, arid methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer. 134-. (canceled)35. A crystalline tosylate salt of (8S ,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1 ,2 ,4-triazol-5-yl)-8 ,9-dihydro-2H-pyrido[4 ,3 ,2-de]phthalazin-3(7H)-one having an X-ray powder diffraction pattern comprising peaks at 2θ angle degrees ±0.2 of 7.5 , 20.1 , and 24.1.36. The crystalline tosylate salt of claim 35 , having an X-ray powder diffraction pattern comprising peaks at 2θ angle degrees ±0.2 of 7.5 claim 35 , 15.1 claim 35 , 18.1 claim 35 , 20.1 claim 35 , 20.5 claim 35 , 22.6 claim 35 , and 24.1.37. A crystalline tosylate salt of (8S claim 35 ,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1 claim 35 ,2 claim 35 ,4-triazol-5-yl)-8 claim 35 ,9-dihydro-2H-pyrido[4 claim 35 ,3 claim 35 ,2-de]phthalazin-3(7H)-one exhibiting a solid state C NMR spectrum with peaks at 143.2 claim 35 , 136.0 claim 35 , 131.8 claim 35 , 123.9 claim 35 , 112.2 claim 35 , 105.2 claim 35 , and 100.3 ppm ±0.2 ppm.38. A pharmaceutical composition comprising the crystalline tosylate salt of and a pharmaceutically acceptable excipient.39. A pharmaceutical composition comprising the crystalline tosylate salt of and a pharmaceutically acceptable excipient.40. A method of treating a cancer claim 35 , comprising administering a therapeutically effective amount of the crystalline tosylate salt of to a subject with cancer.41. The method of claim 40 , ...

Fused Acridine Derivative and Pharmaceutical Composition, Preparation Method and Use Thereof

Provided is a fused acridine derivative as formula (I), which has good antitumor activity. In addition, also provided are a process for preparing the derivative, a pharmaceutical composition containing the derivative, and the use thereof. 2. A fused acridine derivative of claim 1 , or pharmaceutically acceptable acid addition salt or solvate thereof claim 1 , wherein claim 1 , n is 1 claim 1 , 2 or 3.3. A fused acridine derivative of claim 1 , or pharmaceutically acceptable acid addition salt or solvate thereof claim 1 , wherein claim 1 , Xis hydroxy or —NRR claim 1 , Rand Rtogether with the N to which they are attached form a nitrogen-containing 4 to 6 membered heterocyclic ring claim 1 , and the nitrogen-containing 4 to 6 membered heterocyclic rings is selected from 4 claim 1 , 5 or 6 membered Nitrogen heterocyclic which can optionally be substituted by one or more of the following substituents selected from hydroxyl claim 1 , amido claim 1 , sulfamido claim 1 , Calkyl claim 1 , Calkoxy claim 1 , halogen claim 1 , nitro or cyano.4. A fused acridine derivative of claim 3 , or pharmaceutically acceptable acid addition salt or solvate thereof claim 3 , wherein claim 3 , Rand Rtogether with the N to which they are attached form nitrogen-containing 4 to 6 membered heterocyclic rings which are selected from azetidine claim 3 , pyrrolidine claim 3 , pyrrole claim 3 , imidazole claim 3 , piperidine claim 3 , piperazine or morpholine.5. A fused acridine derivative of claim 1 , or pharmaceutically acceptable acid addition salt or solvate thereof claim 1 , wherein claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare each independently hydrogen claim 1 , hydroxy claim 1 , methyl claim 1 , methoxy claim 1 , fluorine claim 1 , chlorine claim 1 , bromine claim 1 , iodine claim 1 , nitro or cyano claim 1 , preferably claim 1 , R claim 1 , Rand Rare each independently hydrogen claim 1 , hydroxy claim 1 , methyl claim 1 , methoxy claim 1 , fluorine claim ...

TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES

The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor.

COMPOSITIONS AND METHODS FOR TREATING MITOCHONDRIAL DISEASES

The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof. 1. A method for treating a mitochondrial disease in a patient , the method comprising the step of administering a therapeutically effective amount of one or more tetracyclic pyrazinoindoles , pharmaceutically acceptable salts thereof , or a combination thereof to the patient.2. The method of wherein the mitochondrial disease is selected from the group consisting of FRDA claim 1 , LHON claim 1 , DAD claim 1 , Leigh's disease claim 1 , NARP claim 1 , MNGIE claim 1 , MERRF claim 1 , and MELAS.3. The method of wherein the mitochondrial disease is FRDA.4. The method of wherein the mitochondrial disease is LHON.9. The method of wherein Ris alkyl.10. The method of wherein Ris methyl.11. The method of wherein Ris cycloalkyl.12. The method of wherein Ris cyclohexyl.13. The method of wherein Ris alkoxy.14. The method of wherein Ris methoxy.15. The method of wherein Ris16. The method of wherein Ris hydrogen.17. The method of wherein Ris hydrogen.18. The method of wherein Ris alkyl.19. The method of wherein Ris methyl.20. The method of wherein Ris cycloalkyl.2126-. (canceled) This application claims priority under 35 U.S.C. §119(e) to U.S. Provisional Application Ser. No. 61/603,763 filed on Feb. 27, 2012, the entire disclosure of which is incorporated herein by reference.The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof.Mitochondrial diseases are a group of disorders caused by dysfunctional mitochondria, ...

CONDENSED-CYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

A condensed cyclic compound is represented by Formula 1 below:

MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (I): 2. The compound of claim 1 , wherein:{'sub': 1-4', 'p, 'ring A is independently a 6-membered carbocycle, a 9- to 10-membered carbocycle, or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-3 heteroatoms selected from N, NH, N(Calkyl), O, and S(O);'}ring B is independently selected from the group consisting of: imidazole, oxazole, oxadiazole, triazole, pyridine, pyridazine, pyrimidine, and benzene; andring C is independently selected from the group consisting of: benzene, pyridine, indazole, indole, benzimidazole, quinoline, isoquinoline, tetrahydroquinoline, tetrahydroisoquinoline, and quinazoline.8. The compound of claim 1 , wherein:{'sub': 1', '2', '2', '2, 'Lis independently selected from the group consisting of: a bond, —CHCH—, —CH═CH—, —C(Me)=CH—, —C≡C—, and —CHNH— in Formula (I), (II), (IIa), (IIb), (IIe) or (IIf);'}{'sub': 3-7', '3-7', '1-4', '1-4, 'sup': '7', 'L is independently selected from the group consisting of: Calkylene and Calkenylene; wherein said alkylene and alkenylene are substituted with 0-2 Rand optionally one or two of the carbon atoms of said alkylene and alkenylene may be replaced by O, CO, NH, N(Calkyl), CONH, NHCO, or CON(Calkyl);'}{'sub': 2', '1-4', '1-4', '2', '1-4', '2', '1-4', '1-4', '2', '2', '1-4', '2', '2', '2', '1-4', '2', '2', '1-4', '2', '2, 'Y is independently selected from the group consisting of: CH, CO, CH(Calkyl), C(Calkyl), O, S, NH, N(Calkyl), N(CO(Calkyl)), —N(Calkyl)CH—, —N(CO(Calkyl))CH—, —N(CHCO(Calkyl))CH—, —CONH—, —NHCO—, —CONHCH—, —CON(Calkyl)CH—, —OCONH—, —NHCONH—, and —SONH—;'}{'sub': 2', '3-6, 'alternatively, L-Y is —(CH)—CH═N—;'}{'sup': '1', 'sub': 2', '2', '3', '1-4', '1-4', '1-4', '1-4', '2', '1-4', '1-4', '2', '2', '2', '2', '2', '2', '2, 'Ris, independently at each occurrence, selected from: halogen, CN, OH, OCHF, OCHF, OCF, Chaloalkyl, Calkyl, Calkoxy, CO(Calkyl), NH, NH(Calkyl), N(Calkyl), —C(═NH)NH, —C(O)NH, —CHNH, and —SONH;'}{'sup': ...

A PLURALITY OF HOST MATERIALS AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME

The present disclosure relates to a plurality of host materials and organic electroluminescent device comprising the same. By comprising a specific combination of a plurality of host materials, the organic electroluminescent device of the present disclosure can show long lifespan while maintaining high luminous efficiency. 4. The organic electroluminescent device according to claim 1 , wherein the substituents of the substituted alkyl group claim 1 , the substituted cycloalkyl group claim 1 , the substituted cycloalkenyl group claim 1 , the substituted heterocycloalkyl group claim 1 , the substituted aryl(ene) group claim 1 , the substituted heteroaryl group claim 1 , and the substituted mono- or polycyclic claim 1 , alicyclic or aromatic ring in A claim 1 , L claim 1 , L claim 1 , Xto Xand Rto R claim 1 , each independently claim 1 , are at least one selected from the group consisting of deuterium; a halogen; a cyano; a carboxyl; a nitro; a hydroxyl; a (C1-C30)alkyl; a halo(C1-C30)alkyl; a (C2-C30)alkenyl; a (C2-C30)alkynyl; a (C1-C30)alkoxy; a (C1-C30)alkylthio; a (C3-C30)cycloalkyl; a (C3-C30)cycloalkenyl; a (3- to 7-membered)heterocycloalkyl; a (C6-C30)aryloxy; a (C6-C30)arylthio; a (3- to 30-membered)heteroaryl unsubstituted or substituted with a (C6-C30)aryl; a (C6-C30)aryl unsubstituted or substituted with a cyano claim 1 , a (3- to 30-membered)heteroaryl or tri(C6-C30)arylsilyl; a tri(C1-C30)alkylsilyl; a tri(C6-C30)arylsilyl; a di(C1-C30)alkyl(C6-C30)arylsilyl; a (C1-C30)alkyldi(C6-C30)arylsilyl; an amino; a mono- or di-(C1-C30)alkylamino; a mono- or di-(C6-C30)arylamino; a (C1-C30)alkyl(C6-C30)arylamino; a (C1-C30)alkylcarbonyl; a (C1-C30)alkoxycarbonyl; a (C6-C30)arylcarbonyl; a di(C6-C30)arylboronyl; a di(C1-C30)alkylboronyl; a (C1-C30)alkyl(C6-C30)arylboronyl; a (C6-C30)aryl(C1-C30)alkyl; and a mono- or di-(C1-C30)alkyl(C6-C30)aryl. The present disclosure relates to a plurality of host materials and organic electroluminescent device comprising the same. ...

NOVEL METHYSERGIDE DERIVATIVES

Provided herein are novel methysergide derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders or symptoms thereof, such as, migraine and Parkinson's disease using the compounds and compositions disclosed herein. In still other embodiments, provided herein, such as, for example, are methods for antagonizing the 5-HTreceptor without agonizing the 5-HTreceptor using the compounds and compositions disclosed herein. In still other embodiments, provided herein such as, for example, are methods of agonizing the 5-HTreceptor using the compounds and compositions disclosed herein. 3. A composition comprising the compound of and a vehicle.4. The compound of claim 2 , wherein Ris a (C-C) alkyl substituted with one or more fluorine atoms.5. The compound of claim 2 , wherein Ris a (C-C) alkyl.6. The compound of claim 4 , wherein Ris a (C-C) alkyl.7. A composition comprising the compound of and a vehicle.8. The composition of claim 7 , wherein the composition is formulated as an oral dosage form.9. The composition of claim 8 , wherein the oral dosage form is in the form of a tablet claim 8 , pill claim 8 , capsule or troche. This application is a continuation of U.S. patent application Ser. No. 14/134,114, filed Dec. 19, 2013, which claims priority under 35 U.S.C. §119(e) from U.S. Provisional Application Ser. No. 61/745,131, filed on Dec. 21, 2012 and U.S. Provisional Application Ser. No. 61/753,328, filed on Jan. 16, 2013, each of which is hereby incorporated by reference in their entirety.Provided herein are novel methysergide derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine and Parkinson's disease using the compounds and compositions disclosed herein. In still other embodiments, provided herein, such as, for example, are ...

TRICYCLIC COMPOUNDS AS STING AGONISTS, AND PREPARATION METHODS AND MEDICINAL USES THEREOF

Compounds of formula (I) useful as agonists of stimulator of interferon genes (STING), the preparation method therefor, pharmaceutical compositions comprising the compounds, and the pharmaceutical uses for the treatment of STING-mediated diseases or disorders are disclosed. 3. The compound of , or a tautomer , cis- or trans-isomer , mesomer , racemate , enantiomer , diastereomer , or mixture thereof , or a pharmaceutically acceptable salt , solvate , or prodrug thereof , wherein G , G , Gand Gare identical or different , and each is independently CR; wherein Rat each occurrence is independently as defined in .4. The compound according to claim 1 , or a tautomer claim 1 , cis- or trans-isomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Rand Rare identical or different claim 1 , and each is independently aryl or heteroaryl; wherein the aryl or heteroaryl is unsubstituted or substituted with one or more substituents independently selected from the group consisting of halogen claim 1 , alkyl claim 1 , alkoxy claim 1 , haloalkyl claim 1 , amino claim 1 , nitro claim 1 , cyano claim 1 , hydroxy claim 1 , hydroxyalkyl claim 1 , cycloalkyl claim 1 , heterocyclyl claim 1 , aryl claim 1 , and heteroaryl.5. The compound according to claim 1 , or a tautomer claim 1 , cis- or trans-isomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or prodrug thereof claim 1 , wherein Rand Rare each hydrogen.7. The compound according to claim 1 , or a tautomer claim 1 , cis- or trans-isomer claim 1 , mesomer claim 1 , racemate claim 1 , enantiomer claim 1 , diastereomer claim 1 , or mixture thereof claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , or ...

TRICYCLIC COMPOUND

The present invention provides a compound having a superior serotonin 5-HTreceptor activating action. 3. The compound or salt of claim 1 , wherein n is 0.4. The compound or salt of claim 2 , wherein n is 0 claim 2 , and Y claim 2 , Yand Yare all carbon atoms.5. The compound or salt of claim 2 , wherein Ris a halogen atom or an alkyl group optionally having substituent(s).6. The compound or salt of claim 1 , wherein X is —N(R)—.7. (2aS)-9-Chloro-1-isopropyl-2 claim 1 ,2a claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-hexahydro-1H-azepino[3 claim 1 ,4 claim 1 ,5-cd]indole claim 1 , or a salt thereof.8. 9-Chloro-2 claim 1 ,2a claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-hexahydro-1H-azepino[3 claim 1 ,4 claim 1 ,5-cd]indole claim 1 , or a salt thereof.9. 9-Isopropyl-1-methyl-2 claim 1 ,2a claim 1 ,3 claim 1 ,4 claim 1 ,5 claim 1 ,6-hexahydro-1H-azepino[3 claim 1 ,4 claim 1 ,5-cd]indole claim 1 , or a salt thereof.10. A medicament comprising the compound or salt of .11. The medicament of claim 10 , which is a serotonin 5-HTreceptor activator.12. The medicament of claim 10 , which is an agent for the prophylaxis or treatment of lower urinary tract symptom claim 10 , obesity and/or organ prolapse.13. A method of activating serotonin 5-HTreceptor claim 1 , which comprises administering an effective amount of the compound or salt of to a mammal.14. A method for the prophylaxis or treatment of lower urinary tract symptom claim 1 , obesity and/or organ prolapse claim 1 , which comprises administering an effective amount of the compound or salt of to a mammal.1516-. (canceled) The present invention relates to a tricyclic compound having a superior serotonin 5-HTreceptor activating action and useful as an agent for treatment or the prophylaxis of a lower urinary tract symptom, obesity and/or organ prolapse etc., and the like.Serotonin 5-HTreceptor is one of the receptors of the biological transmitter serotonin, which is distributed mainly in the central nervous system and controls ...

USE OF RNAI INHIBITING PARP ACTIVITY FOR THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT OF CANCER

The present invention relates to the use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination. 1. Use of an agent that inhibits the activity of an enzyme that mediates repair of a DNA strand break in the manufacture of a medicament for the treatment of diseases caused by a defect in a gene that mediates homologous recombination.2. The use as claimed m wherein the enzyme is poly(ADP-ribose) polymerase (PARP).3. The use as claimed in wherein the agent is a PARP inhibitor.4. The use as claimed in wherein the PARP inhibitor is selected from the group consisting of PARP-1 claim 3 , PARP-2 claim 3 , PARP-3 claim 3 , PARP-4 claim 3 , tankyrase 1 and tankyrase 2.5. The use as claimed in wherein the PARP is PARP-1.6. The use as claimed in or wherein the agent is an RNAi molecule specific to a PARP gene.7. The use as claimed in wherein the RNAi molecule is derived from a nucleic acid molecule comprising a nucleic acid sequence selected from the group consisting of:{'figref': {'@idref': 'DRAWINGS', 'FIG. 9, 10, 11, 12, 13 or 14'}, 'a) a nucleic acid sequence as represented by the sequence in , or a fragment thereof;'}{'figref': {'@idref': 'DRAWINGS', 'FIG. 9, 10, 11, 12, 13 or 14'}, 'b) a nucleic acid sequence which hybridises to the nucleic acid sequences of , and encodes a gene for PARP; or'}c) a nucleic acid sequence which comprises sequences which are degenerate as a result of the genetic code to the nucleic acid sequences defined in (a) and (b).8. The use as claimed in or wherein the RNAi molecule comprises the nucleic acid sequence aaa agc cau ggu gga gua uga.9. The use as claimed in or wherein the RNAi molecule consists of the nucleic acid sequence aag acc aau cuc ucc agu uca ac.10. The use as claimed in or wherein the RNAi molecule consists of the nucleic acid sequence aag acc aac auc gag aac aac. ...

PROCESS FOR THE PREPARATION OF TETRACARBOXYNAPHTHALENEDIIMIDE COMPOUNDS DISUBSTITUTED WITH HETEROARYL GROUPS

A process for the preparation of a tetracarboxynaphthalenediimide compound disubstituted with heteroaryl groups having general formula (I), comprising the reaction of at least one disubstituted N,Ndialkyl-1,4,5,8-tetracarboxynaphthalenediimide with at least one heteroaryl compound. Said tetracarboxynaphthalenediimide compound disubstituted with heteroaryl groups can be advantageously used as monomer in the synthesis of semiconductor polymers which can be advantageously used in the construction of organic field effect transistors (OFET) or of organic thin film transistors (OTFT). 2. The process according to claim 1 , wherein said process relates to the preparation of 2 claim 1 ,6-di-(2 claim 1 ,2′-thienyl)-N claim 1 ,N′-dialkyl-1 claim 1 ,4 claim 1 ,5 claim 1 ,8-tetracarboxynaphthal-enediimide corresponding to a tetracarboxynaphthalenediimide compound disubstituted claim 1 , in positions 2 and 6 claim 1 , with heteroaryl groups having general the formula (I) where{'sup': '1', 'Rrepresents an ethyl-hexyl group or a n-heptyl group,'}Y represents a sulfur atom,{'sup': 2', '2, 'Z represents a CRgroup where Rrepresents a hydrogen atom, and'}{'sup': 3', '4, 'Rand Rrepresent a hydrogen atom.'}3. The process according to claim 1 , wherein a molar ratio of said disubstituted N claim 1 ,N′-dialkyl-1 claim 1 ,4 claim 1 ,5 claim 1 ,8-tetracarboxy-naphthalenediimide of formula (II) to said heteroaryl compound of formula (III) is from 1:2 to 1:20.4. The process according to claim 1 , wherein said process is carried out in the presence of at least one weak organic base.5. The process according to claim 4 , wherein said weak organic base is selected from the group consisting of a carbonate of an alkaline metal claim 4 , a carbonate of an alkaline-earth metal claim 4 , and any mixture thereof.6. The process according to claim 4 , wherein a molar ratio of said disubstituted N claim 4 ,N′-dialkyl-1 claim 4 ,4 claim 4 ,5 claim 4 ,8-tetracarboxynaphthalenediimide of formula (II) to said ...

TRICYCLIC QUINOLINE AND QUINOXALINE DERIVATIVES

The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor. 150.-. (canceled)51. A compound selected from the group consisting oftrans-12a-methyl-4,5,6,7,10,11,12,12a-octahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinolin-9(9aH)-one;cis-12a-methyl-4,5,6,7,10,11,12,12a-octahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinolin-9(9aH)-one;cis-12a-methyl-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline;trans-12a-methyl-4,5,6,7,9,9a,10,11,12,12a-decahydrocyclopenta[c][1,4]diazepino[6,7,1-ij]quinoline;(R)-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline;(S)-5,6,7,9,9a,10,11,12-octahydro-4H-[1,4]diazepino[1,7,6-de]pyrrolo[1,2-a]quinoxaline; and3-benzyl-2′,3′,7′,8′,9′,10′-hexahydro-1H-3′,8′,10a′-triaza-cyclohepta[de]naphthalene;or a pharmaceutically acceptable salt thereof.52. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound as claimed in claim 51 , or a stereoisomer thereof claim 51 , or a pharmaceutically acceptable salt thereof in combination with at least one pharmaceutically acceptable carrier and/or auxiliary substance. This application claims the benefit of U.S. Patent Application No. 61/701,514 filed on Sep. 14, 2012 and U.S. Patent Application No. 61/701,531 filed on Sep. 14, 2012, the contents of each of which are herein incorporated by reference.The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially ...

CRYSTAL FORM OF MONOMETHANESULFONATE OF DEUTERATED 3-(4,5-SUBSTITUTED AMINOPYRIMIDINE)PHENYL COMPOUND AND PREPARATION METHOD THEREFOR

Disclosed in the present invention are a crystal form of monomethanesulfonate of a deuterated 3-(4,5-substituted aminopyrimidine)phenyl compound as represented by formula I, and a preparation method therefor. The crystal form is highly stable, can be used for treatment or prevention of diseases or conditions by means of epidermal growth factor receptors (EGFRs) in some mutation forms, can effectively inhibit the growth of a variety of tumor cells, and have an inhibiting effect on other proteases of EGFR and Her families, and thus can be used for preparing antitumor drugs. 2. The crystal form A according to claim 1 , wherein in the X-ray powder diffraction claim 1 , the 2θ diffraction angle also has characteristic peaks at 6.34±0.2° claim 1 , 10.24±0.2° claim 1 , 10.72±0.2° claim 1 , 14.94±0.2° claim 1 , 15.42±0.2° claim 1 , 16.88±0.2° claim 1 , 17.86±0.2° claim 1 , 20.58±0.2° claim 1 , 21.58±0.2° claim 1 , 23.86±0.2° claim 1 , 24.96±0.2° claim 1 , 26.28±0.2° claim 1 , and 27.58±0.2°.3. The crystal form A according to claim 1 , having an X-ray powder diffraction pattern basically as shown in .4. The crystal form A according to claim 1 , having a thermogravimetric analysis graph basically as shown in and a differential scanning calorimetry curve basically as shown in .5. The crystal form A according to claim 1 , having infrared spectra with the following characteristic absorption peaks: 3249 cm claim 1 , 3019 cm claim 1 , 1942 cm claim 1 , 1906 cm claim 1 , 1672 cm claim 1 , 1575 cm claim 1 , 1552 cm claim 1 , 1411 cm claim 1 , 1368 cm claim 1 , 727 cm claim 1 , 558 cm claim 1 , and 522 cm.7. The crystal B according to claim 6 , wherein in the X-ray powder diffraction of the crystal form B claim 6 , the 20 diffraction angle also has characteristic peaks at 7.20±0.2° claim 6 , 8.00±0.2° claim 6 , 8.50±0.2° claim 6 , 10.38±0.2° claim 6 , 14.9±0.2° claim 6 , 16.06±0.2° claim 6 , 18.1±0.2° claim 6 , 19.28±0.2° claim 6 , 20.88±0.2° claim 6 , 21.96±0.2° claim 6 , 22.68±0.2° ...

COMPOUND, ORGANIC OPTOELECTRONIC ELEMENT COMPRISING SAME, AND DISPLAY DEVICE

A compound represented by Chemical Formula 1, an organic optoelectronic device including the same and a display device including the organic optoelectronic device are disclosed. A structure of the compound represented by Chemical Formula 1 is described in the specification. 2. The compound of claim 1 , wherein:{'sup': '1', 'Ris hydrogen, deuterium, a substituted or unsubstituted C1 to C20 alkyl group, or a substituted or unsubstituted C3 to C40 silyl group, and'}Ar is a substituted or unsubstituted C6 to C30 aryl group, or a substituted or unsubstituted C2 to C30 heteroaryl group having electron characteristics.6. The compound of claim 1 , wherein X is NR′ or CR′R″ claim 1 , in which R′ and R″ are each independently hydrogen claim 1 , deuterium claim 1 , a substituted or unsubstituted C1 to C20 alkyl group claim 1 , a substituted or unsubstituted C6 to C30 aryl group claim 1 , or a substituted or unsubstituted C2 to C30 heteroaryl group.9. The compound of claim 1 , wherein:{'sup': '1', 'Ris hydrogen, deuterium, a substituted or unsubstituted C1 to C10 alkyl group, or a substituted or unsubstituted silyl group, and'}{'sup': '2', 'Ris hydrogen, deuterium, a substituted or unsubstituted C1 to C20 alkyl group, a substituted or unsubstituted C6 to C30 aryl group, or a substituted or unsubstituted C2 to C30 heteroaryl group.'}10. The compound of claim 9 , wherein:{'sup': '2', 'Ris the substituted or unsubstituted C6 to C30 aryl group, and'}the substituted or unsubstituted C6 to C30 aryl group is a substituted or unsubstituted phenyl group, a substituted or unsubstituted naphthyl group, a substituted or unsubstituted biphenyl group, a substituted or unsubstituted anthracenyl group, a substituted or unsubstituted phenanthryl group, or a substituted or unsubstituted triphenylenyl group.14. The compound of claim 1 , wherein the compound has a triplet exciton energy (T1) of 2.0 eV or greater.15. An organic optoelectronic device claim 1 , comprising:an anode and a cathode ...

AMINE COMPOUND AND ORGANIC LIGHT EMITTING DIODE COMPRISING SAME

Provided is a compound of Chemical Formula 1: 4. The compound of claim 1 , wherein Ar11 to Ar14 are the same as or different from each other claim 1 , and each independently is an aryl group which is unsubstituted or substituted with one substituent selected from the group consisting of deuterium claim 1 , a halogen group claim 1 , a nitrile group claim 1 , an alkyl group claim 1 , a haloalkyl group claim 1 , an alkoxy group claim 1 , a haloalkoxy group claim 1 , a silyl group claim 1 , and a cycloalkyl group claim 1 , or a substituent to which two or more substituents selected from the group are linked; or a heteroaryl group which is unsubstituted or substituted with one substituent selected from the group consisting of deuterium claim 1 , a halogen group claim 1 , a nitrile group claim 1 , an alkyl group claim 1 , a haloalkyl group claim 1 , an alkoxy group claim 1 , a haloalkoxy group claim 1 , a silyl group claim 1 , and a cycloalkyl group claim 1 , or a substituent to which two or more substituents selected from the group are linked.5. The compound of claim 1 , wherein -(L)n-Ar15 in Formula 1 is a phenyl group which is unsubstituted or substituted with deuterium claim 1 , a halogen group claim 1 , a nitrile group claim 1 , an alkyl group which is unsubstituted or substituted with deuterium claim 1 , an alkoxy group claim 1 , or a silyl group; or a biphenyl group which is unsubstituted or substituted with deuterium claim 1 , a halogen group claim 1 , a nitrile group claim 1 , an alkyl group which is unsubstituted or substituted with deuterium claim 1 , an alkoxy group claim 1 , or a silyl group.6. The compound of claim 1 , wherein Ar15 is bonded to adjacent R1 to form a benzene ring which is unsubstituted or substituted with deuterium claim 1 , a halogen group claim 1 , a nitrile group claim 1 , a methyl group claim 1 , an isopropyl group claim 1 , a t-butyl group claim 1 , a methoxy group claim 1 , CD claim 1 , a phenyl group claim 1 , a phenyl group which is ...

Organic electroluminescent element and electronic device

An organic electroluminescence device having a further improved lifetime, which comprising a cathode, an anode and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises a fluorescent emitting layer and the fluorescent emitting layer comprises at least one dopant material selected from the compounds represented by formulae (D1) and (D2), at least one first compound selected from the compounds represented by formulae (19), (21), (22), and (23), and at least one second compound selected from the compounds represented by formulae (2a), (2b), and (2c) and an electronic device comprising the organic electroluminescence device are described.

ORGANIC ELECTROLUMINESCENCE ELEMENT AND ELECTRONIC DEVICE

Organic EL devices having excellent performance and electronic devices comprising the organic EL devices are provided. The organic EL device comprises a cathode, an anode, and an organic layer disposed between the cathode and the anode, wherein the organic layer comprises one or more layers that comprise a fluorescent emitting layer and the fluorescent emitting layer comprises a first compound represented by formula (P) and a second compound that is not the same as the first compound. The electronic device comprises the organic EL device. 7. The organic electroluminescence device according to claim 3 ,{'sub': 2', '4', '5', '10', '11', '101', '102', '103', '104', '105', '101', '105, 'claim-ref': {'@idref': 'CLM-00003', 'claim 3'}, 'wherein at least one selected from R, R, R, R, and Rof formula (1) is a group not forming the ring structure having 3 or more atoms and is a halogen atom, a cyano group, a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms, a substituted or unsubstituted alkenyl group having 1 to 20 carbon atoms, a substituted or unsubstituted alkynyl group having 1 to 20 carbon atoms, a substituted or unsubstituted cycloalkyl group having 3 to 20 ring carbon atoms, an amino group, 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 50 ring carbon atoms, a substituted or unsubstituted alkylthio group having 1 to 20 carbon atoms, a substituted or unsubstituted arylthio group having 6 to 50 ring carbon atoms, a group of —Si(R)(R)(R), a group of —N(R)(R) wherein Rto Rare as defined in , a substituted or unsubstituted aryl group having 6 to 50 ring carbon atoms, or a substituted or unsubstituted heteroaryl group having 5 to 50 ring atoms.'}8. The organic electroluminescence device according to claim 7 ,{'sub': 2 ...

NITROGEN-CONTAINING TRICYCLIC DERIVATIVES HAVING HIV REPLICATION INHIBITORY ACTIVITY

The present invention provides a novel compound having antiviral activity, especially HIV replication inhibitory activity and a medicament containing the same. The compound represented by the formula: 3: The compound or pharmaceutically acceptable salt according to claim 1 , wherein Ris alkyl.5: A pharmaceutical composition claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'the compound or pharmaceutically acceptable salt according to in an effective amount; and'}a pharmaceutically acceptable carrier.6: The pharmaceutical composition according to claim 5 , wherein the effective amount of the compound or pharmaceutically acceptable salt is an effective amount having anti-virus activity.7: The pharmaceutical composition according to claim 5 , wherein the effective amount of the compound or pharmaceutically acceptable salt is an effective amount having anti-HIV activity.8: A method of treating or preventing a HIV infectious disease claim 5 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'administering the compound or pharmaceutically acceptable salt according to to a patient in need thereof.'}10: The compound or pharmaceutically acceptable salt according to claim 9 , wherein the Substituent Group E includes alkyl claim 9 , halogen claim 9 , alkyloxy claim 9 , dialkylamino alkyloxy claim 9 , and alkylamino alkyloxy.13: The compound or pharmaceutically acceptable salt according to claim 9 , wherein Ris alkyl.14: A pharmaceutical composition claim 9 , comprising:{'claim-ref': {'@idref': 'CLM-00009', 'claim 9'}, 'the compound or pharmaceutically acceptable salt according to in an effective amount; and'}a pharmaceutically acceptable carrier.15: The pharmaceutical composition according to claim 14 , wherein the effective amount of the compound or pharmaceutically acceptable salt is an effective amount having anti-virus activity.16: The pharmaceutical composition according to claim 14 , wherein the effective amount of the compound or ...

TRICYCLIC OXAZOLIDINONE ANTIBIOTIC COMPOUNDS

The present invention relates to antibacterial compounds of formula (I) wherein “----” is a bond or is absent, V is CH, CRor N; Ris H or, if “----” is a bond, may also be alkoxy; Ris cyano, alkyl, or ethynyl; U is CH or N when “----” is a bond, or, if “----” is absent, U is CH, NH or NH; Ris H, alkylcarbonyl or CH—R; Ris H, alkyl or hydroxyalkyl; Ris H or, if n is not 0 and Ris H, may also be OH; Ris H, alkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, carboxy or alkoxycarbonyl; Ris hydroxyalkyl, carboxy, alkoxycarbonyl or —(CH)—NRR, q being 1, 2 or 3 and each of Rand Rindependently being H or alkyl or Rand Rforming with the N atom bearing them a ring; Ris alkyl or hydroxyalkyl; A is —(CH)—, —CHCHCH(OH)— or —COCHCH(OH)—; G is substituted phenyl or Gor G, wherein Q is O or S and X is CH or N; and Y, Yand Ymay each be CH or N; and n is 0 when A is —CHCHCH(OH)— or —COCHCH(OH)—, and n is 0, 1 or 2 when A is —(CH)—, p being 1, 2, 3 or 4, with the proviso that the sum of n and p is then 2, 3 or 4; and to salts of such compounds. 2. The compound according to claim 1 ,wherein{'sup': '1', 'sub': 1', '3, 'Rrepresents cyano or (C-C)alkyl;'}{'sub': '2', 'U represents CH or N when “-----” is a bond, or, in case “----” is absent, U represents CHor NH;'}{'sup': '5', 'sub': 1', '3', '1', '3', '1', '3', '1', '3', '1', '3, 'Rrepresents H, (C-C)alkyl, (C-C)hydroxyalkyl, (C-C)alkoxy(C-C)alkyl or (C-C)alkoxycarbonyl;'}or a salt thereof of such a compound.34-. (canceled)5. The compound according to claim 1 ,wherein V represents CH and U represents CH or N, or', {'sup': '6', 'V represents CRand U represents CH, or'}, 'V represents N and U represents CH; or, '“-----” is a bond,'} {'sub': '2', 'sup': '9', 'V represents CH and U represents CH, NH or NR;'}, '“-----” is absent,'}{'sup': 2', '3, 'sub': '2', 'Rrepresents H, acetyl or a group of the formula —CH—R;'}{'sup': 6', '7', '8', '7', '8', '7', '8, 'sub': 1', '3', '1', '3', '2', 'q', '1', '3, 'Rrepresents (C-C)hydroxyalkyl, carboxy, (C-C) ...

NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (Ia): 10. A pharmaceutical composition comprising one or more compounds according to and a pharmaceutically acceptable carrier or diluent.11. A method for the treatment and/or prophylaxis of a thromboembolic disorder claim 1 , comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a stereoisomer claim 1 , a tautomer claim 1 , or a pharmaceutically acceptable salt thereof.12. A method according to claim 11 , wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders claim 11 , venous cardiovascular thromboembolic disorders claim 11 , and thromboembolic disorders in the chambers of the heart or in the peripheral circulation.13. A method according to claim 12 , wherein the thromboembolic disorder is selected from unstable angina claim 12 , an acute coronary syndrome claim 12 , atrial fibrillation claim 12 , myocardial infarction claim 12 , transient ischemic attack claim 12 , stroke claim 12 , atherosclerosis claim 12 , peripheral occlusive arterial disease claim 12 , venous thrombosis claim 12 , deep vein thrombosis claim 12 , thrombophlebitis claim 12 , arterial embolism claim 12 , coronary arterial thrombosis claim 12 , cerebral arterial thrombosis claim 12 , cerebral embolism claim 12 , kidney embolism claim 12 , pulmonary embolism claim 12 , and thrombosis resulting from medical implants claim 12 , devices claim 12 , or procedures in which blood is exposed to an artificial surface that promotes thrombosis.14. A compound of claim 1 , or a stereoisomer claim 1 , a tautomer claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , for use in therapy. This application is a divisional application of U.S. patent application Ser. No. 14/236,973, filed Feb. 4, 2014, which is a national phase of International Patent Application No. PCT/US2012/049706, filed Aug. 6, 2012, which claims ...

Pesticidally active heterocyclic derivatives with sulfur containing substituents

Compounds of formula (I), wherein the substituents are as defined in claim 1 , and the agrochemically acceptable salts, stereoisomers, enantiomers, tautomers and N-oxides of those compounds, can be used as insecticides and can be prepared in a manner known per se.

DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) FOR USE IN TREATMENT OF DISEASES ASSOCIATED WITH A PTEN DEFICIENCY

A compound having the structure set forth in Formula (I) and Formula (II): 122-. (canceled)24. The method of claim 23 , wherein said administration is in combination with ionizing radiation claim 23 , one or more chemotherapeutic agents claim 23 , or a combination thereof.26. The method of claim 25 , wherein said administration is in combination with ionizing radiation claim 25 , one or more chemotherapeutic agents claim 25 , or a combination thereof. This application is a continuation of U.S. patent application Ser. No. 14/671,944, filed Mar. 27, 2015, now abandoned, which is a continuation of U.S. patent application Ser. No. 13/972,166, filed Aug. 21, 2013, now U.S. Pat. No. 9,018,201, issued on Apr. 28, 2015, which is a continuation of U.S. patent application Ser. No. 13/020,619, filed Feb. 3, 2011, now U.S. Pat. No. 8,541,403, issued on Sep. 24, 2013, which claims the benefit of priority of U.S. Provisional Patent Application No. 61/301,174, filed Feb. 3, 2010, each of which is hereby incorporated by reference in its entirety into this application.Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to modulate the activity of PARP to treat or prevent diseases or conditions associated with a deficiency in the enzyme phosphatase and tensin homolog deleted on chromosome 10 (PTEN).The family of poly(ADP-ribose)polymerases (PARP) includes approximately 18 proteins, which all display a certain level of homology in their catalytic domain but differ in their cellular functions (Ame et al., 26(8), 882-893 (2004)). PARP-1 and PARP-2 are unique members of the family, in that their catalytic activities are stimulated by the occurrence of DNA strand breaks.PARP has been implicated in the signaling of DNA damage through its ability to recognize and rapidly bind to DNA single or double strand breaks (D'Amours, et at, 342, 249-268 (1999)). It participates in ...

AMINO ACID-, PEPTIDE- AND POLYPEPTIDE-LIPIDS, ISOMERS, COMPOSITIONS, AND USES THEREOF

Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: 185-. (canceled)87. The method of claim 86 , wherein each instance of Ris a group of formula (iv).92. The method of claim 86 , wherein X is NR claim 86 , wherein Ris hydrogen or a nitrogen protecting group.93. The method of claim 86 , wherein X is O.94. The method of claim 86 , wherein the composition is a pharmaceutical composition.95. The method of claim 86 , wherein the agent is an organic molecule claim 86 , inorganic molecule claim 86 , nucleic acid claim 86 , protein claim 86 , peptide claim 86 , polynucleotide claim 86 , targeting agent claim 86 , an isotopically labeled chemical compound claim 86 , vaccine claim 86 , an immunological agent claim 86 , or an agent useful in bioprocessing.96. The method of claim 86 , wherein the agent is a polynucleotide.97. The method of claim 96 , wherein the polynucleotide is RNA.98. The method of claim 97 , wherein the RNA carries out RNA interference.99. The method of claim 97 , wherein the RNA is RNAi claim 97 , dsRNA claim 97 , siRNA claim 97 , shRNA claim 97 , miRNA claim 97 , or antisense RNA.100. The method of claim 97 , wherein upon delivery of the RNA into the cell claim 97 , the RNA is able to interfere with the expression of a specific gene in a biological cell.101. The method of claim 96 , wherein the polynucleotide is DNA.102. The method of claim 96 , wherein the polynucleotide encodes a ...

SYNTHESIS OF POLYCYCLIC ALKALOIDS

Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use. 6. The compound according to wherein the V bearing Ris carbon; Rand Rare joined claim 5 , together with the atom to which each is attached claim 5 , to form an aromatic ring; and any remaining V is selected from oxygen claim 5 , sulfur claim 5 , and nitrogen.7. The compound according to wherein the V bearing Ris carbon claim 5 , Rand Rare joined claim 5 , together with the atom to which each is attached claim 5 , to form an aromatic ring; and any remaining V is selected from oxygen claim 5 , sulfur claim 5 , and nitrogen.8. The compound according to wherein Ris selected from nitromethyl claim 5 , —CH—NH claim 5 , carboxyl claim 5 , and amide claim 5 , and Ris selected from methyl and hydrogen.9. The compound according to wherein W is oxygen.16. The method according to wherein the one or more activating reagents are selected from N-ethyl-N′-(3-dimethylaminopropyl)carbodiimide claim 13 , 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride claim 13 , dicyclohexylcarbodiimide claim 13 , carbonyl diimidazole claim 13 , 1-hydroxybenzotriazole claim 13 , 1-hydroxy-7-aza-benzotriazole claim 13 , and o-(7-azabenzotriazol-1-yl)-N claim 13 ,N claim 13 ,N′ claim 13 ,N′-tetramethyluronium hexafluorophosphate claim 13 , and any combination thereof claim 13 , the base is selected from triethylamine claim 13 , 1 claim 13 ,8-diazabicycloundec-7-ene claim 13 , 1 claim 13 ,4-diazabicyclo[2.2.2]octane claim 13 , and diisopropylethylamine claim 13 , and the solvent is ...

TRAPPING-FREE PARP INHIBITORS

The disclosure provides PARP PROTAC molecules comprising a PARP inhibitor linked to an E3 ligase binder, and their use in treating diseases caused by aberrant PARP activation. Such PROTAC molecules produce selective degradation of one or a specific set of PARP proteins with limited effects on the protein level of other PARPs. 2. The composition of claim 1 , wherein the PARP protein is PARP1.3. The composition of claim 1 , wherein the PARP protein is PARP2.4. The composition of claim 1 , wherein the PARP protein is PARP3.5. The composition of claim 1 , wherein the PARP protein is PARP5A.6. The composition of claim 1 , wherein the PARP protein is PARP5B.7. The composition of claim 1 , wherein the E3 ligase is protein cereblon (CRBN).8. The composition of claim 1 , wherein the E3 ligase is von Hippel Lindau disease tumor suppressor (pVHL).9. The composition of claim 1 , wherein the E3 ligase is mouse double minute 2 homolog (MDM2).10. The composition of claim 1 , wherein the E3 ligase is cellular inhibitor of apoptosis protein-1 (cIAP1).11. The composition of claim 1 , wherein the E3 ligase is beta-transducin repeat containing protein (β-TrCP).12. The composition of claim 1 , wherein A makes one or more interactions with human PARP1 at one or more sites selected from the group consisting of Glu763 claim 1 , Asp766 claim 1 , His862 claim 1 , Gly863 claim 1 , Arg878 claim 1 , Ala880 claim 1 , Gly888 claim 1 , Tyr889 claim 1 , Tyr896 claim 1 , Ser904 claim 1 , and Glu988.13. The composition of claim 1 , wherein A makes one or more interactions with human PARP2 at one or more sites selected from the group consisting of Gly429 claim 1 , Arg444 claim 1 , Tyr462 claim 1 , Ser470 claim 1 , and Tyr473.14. The composition of claim 1 , wherein A makes one or more interactions with human PARP3 at one or more sites selected from the group consisting of Leu287 claim 1 , Asp291 claim 1 , His384 claim 1 , Gly385 claim 1 , Thr386 claim 1 , Arg400 claim 1 , Tyr414 claim 1 , and Ser422. ...

CYCLIC P1 LINKERS AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. 4. The compound of claim 2 , wherein:ring A is selected from the group consisting of phenyl, imidazole, pyridine, pyridazine, pyrimidine, pyridone, and pyridazinone.9. A pharmaceutical composition comprising one or more compounds according to and a pharmaceutically acceptable carrier or diluent.10. A method for the treatment and/or prophylaxis of a thromboembolic disorder claim 1 , comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a stereoisomer claim 1 , a tautomer claim 1 , or a pharmaceutically acceptable salt thereof.11. A method according to claim 10 , wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders claim 10 , venous cardiovascular thromboembolic disorders claim 10 , and thromboembolic disorders in the chambers of the heart or in the peripheral circulation.12. A method according to claim 11 , wherein the thromboembolic disorder is selected from unstable angina claim 11 , an acute coronary syndrome claim 11 , atrial fibrillation claim 11 , myocardial infarction claim 11 , transient ischemic attack claim 11 , stroke claim 11 , atherosclerosis claim 11 , peripheral occlusive arterial disease claim 11 , venous thrombosis claim 11 , deep vein thrombosis claim 11 , thrombophlebitis claim 11 , arterial embolism claim 11 , coronary arterial thrombosis claim 11 , cerebral arterial thrombosis claim 11 , cerebral embolism claim 11 , kidney embolism claim 11 , pulmonary embolism ...

AMINOINDOLO[3,2,1-jk]CARBAZOLE COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

The present invention provides a novel aminoindolo[3,2,1-jk]carbazole compound having a good film-forming property and provides an organic light-emitting device including the compound. Provided is the aminoindolo[3,2,1-jk]carbazole compound represented by Formula [1] according to Claim 1 . In Formula [1], l represents an integer of 1 to 3; n and m each independently represent an integer of 0 to 2; and R 1 to R 32 represent hydrogen atom, alkyl groups having 1 to 8 carbon atoms or fluorine atoms, wherein the alkyl groups may contain fluorine atoms.

GRANZYME B DIRECTED IMAGING AND THERAPY

Provided herein are compounds of Formula (I) below that are useful for imaging Granzyme B. Methods of imaging Granzyme B and treating an immunoregulatory abnormality, pharmaceutical compositions, and kits comprising the Granzyme B imaging agents are also provided.

MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (I): 2. The compound of claim 1 , wherein:{'sub': 1-4', 'p, 'ring A is independently a 6-membered carbocycle, a 9- to 10-membered carbocycle, or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-3 heteroatoms selected from N, NH, N(Calkyl), O, and S(O);'}ring B is independently selected from the group consisting of: imidazole, oxazole, oxadiazole, triazole, pyridine, pyridazine, pyrimidine, and benzene; andring C is independently selected from the group consisting of: benzene, pyridine, indazole, indole, benzimidazole, quinoline, isoquinoline, tetrahydroquinoline, tetrahydroisoquinoline, and quinazoline.8. The compound of claim 1 , wherein:{'sub': 1', '2', '2', '2, 'Lis independently selected from the group consisting of: a bond, —CHCH—, —CH═CH—, —C(Me)=CH—, —C≡C—, and —CHNH— in Formula (I), (II), (IIa), (IIb), (IIe) or (IIf);'}{'sub': 3-7', '3-7', '1-4', '1-4, 'sup': '7', 'L is independently selected from the group consisting of: Calkylene and Calkenylene; wherein said alkylene and alkenylene are substituted with 0-2 Rand optionally one or two of the carbon atoms of said alkylene and alkenylene may be replaced by O, CO, NH, N(Calkyl), CONH, NHCO, or CON(Calkyl);'}{'sub': 2', '1-4', '1-4', '2', '1-4', '2', '1-4', '1-4', '2', '2', '1-4', '2', '2', '2', '1-4', '2', '2', '1-4', '2', '2, 'Y is independently selected from the group consisting of: CH, CO, CH(Calkyl), C(Calkyl), O, S, NH, N(Calkyl), N(CO(Calkyl)), —N(Calkyl)CH—, —N(CO(Calkyl))CH—, —N(CHCO(Calkyl))CH—, —CONH—, —NHCO—, —CONHCH—, —CON(Calkyl)CH—, —OCONH—, —NHCONH—, and —SONH—;'}{'sub': 2', '3-6, 'alternatively, L-Y is —(CH)—CH═N—;'}{'sup': '1', 'sub': 2', '2', '3', '1-4', '1-4', '1-4', '1-4', '2', '1-4', '1-4', '2', '2', '2', '2', '2', '2', '2, 'Ris, independently at each occurrence, selected from: halogen, CN, OH, OCHF, OCHF, OCF, Chaloalkyl, Calkyl, Calkoxy, CO(Calkyl), NH, NH(Calkyl), N(Calkyl), —C(═NH)NH, —C(O)NH, —CHNH, and —SONH;'}{'sup': ...

SALTS AND POLYMORPHS OF 8-FLUORO-2-{4-[(METHYLAMINO)METHYL]PHENYL}-1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE

The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer. 1. A crystalline camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1 ,3 ,4 ,5-tetrahydro-6H-azepino[5 ,4 ,3-cd]indol-6-one , wherein the salt has a powder X-ray diffraction pattern comprising two or more peaks at diffraction angle (2θ) selected from the group consisting of 12.2±0.2 , 13.8±0.2 , 18.3±0.2 , 22.5±0.2 , and 25.4±0.2 , wherein said powder x-ray diffraction pattern is obtained using copper k-alphax-rays at a wave length of 1.5406 Ångstroms.2. The salt of claim 1 , wherein the salt has a solid state NMR spectrum comprising 2 or more C chemical shifts selected from the group consisting of 213.4±0.2 claim 1 , 171.8±0.2 claim 1 , and 17.3±0.2 ppm.3. The salt of claim 1 , wherein the salt has a solid state NMR spectrum comprising F chemical shifts at −118.9±0.2 and −119.7±0.2 ppm.4. The salt of claim 1 , wherein the DSC thermogram of the salt comprises an endotherm onset at 303.2° C.5. The salt of claim 1 , wherein the camsylate comprises S-camsylate.6. The salt of claim 1 , wherein the camsylate comprises R-camsylate.7. A pharmaceutical composition comprising the salt of and a pharmaceutically acceptable carrier. This application is a continuation of U.S. application Ser. No. 14/698,463, filed Apr. 28, 2015, entitled “Salts and Polymorphs of 8-Fluoro-2-{4-[(Methylamino)Methyl]Phenyl}-1,3,4,5-Tetrahydro-6H-Azepino[5,4,3-cd]Indol-6-One”. U.S. application Ser. No. 14/698,463 is a continuation of U.S. application Ser. No. 14/272,589, filed May 8, 2014, now U.S. Pat. No. 9,045,487. U.S. application Ser. No. 14/272,589 is a continuation of U ...

SOLID STATE FORMS OF RUCAPARIB AND OF RUCAPARIB SALTS

Disclosed are solid state forms of Rucaparib and of Rucaparib salts, and pharmaceutical compositions thereof. 134-. (canceled)35. A crystalline form of Rucaparib Hemi-Edisylate designated as Form III , characterized by data selected from one or more of the following:{'figref': {'@idref': 'DRAWINGS', 'FIG. 25'}, 'a. an X-ray powder diffraction pattern substantially as depicted in ;'}b. an X-ray powder diffraction pattern having peaks at 7.1, 17.2, 21.3, 21.8 and 23.5 degrees 2-theta±0.2 degrees 2-theta; andc. combinations of these data.36. The crystalline form of Rucaparib Hemi-Edisylate according to claim 35 , characterized by an X-ray powder diffraction pattern having peaks at 7.1 claim 35 , 17.2 claim 35 , 21.3 claim 35 , 21.8 and 23.5 degrees 2-theta±0.2 degrees 2-theta and also having any one claim 35 , two claim 35 , three claim 35 , four or five additional peaks selected from 11.2 claim 35 , 11.4 claim 35 , 15.7 claim 35 , 21.6 claim 35 , and 25.4 degrees 2-theta±0.2 degrees 2-theta.37. A process for preparing Rucaparib salt or a solid state form thereof comprising preparing the crystalline form of Rucaparib according to claim 35 , and converting it to Rucaparib salt or a solid state form thereof.38. A pharmaceutical formulation comprising the crystalline form according to and at least one pharmaceutically acceptable excipient.39. A process for preparing the pharmaceutical formulation according to claim 38 , comprising combining the crystalline form with the at least one pharmaceutically acceptable excipient.40. A medicament comprising the crystalline form according to .41. The crystalline form according to for use in the treatment of cancer.42. The crystalline form according to for the manufacture of a medicament for treating cancer.43. A process for preparing Rucaparib salt or a solid state form thereof comprising preparing the crystalline form of Rucaparib according to claim 35 , and converting it to Rucaparib salt or a solid state form thereof.44. A ...

Indolo heptamyl oxime analogue as parp inhibitor

Disclosed is a type of indolo heptamyl oxime compounds as a PARP inhibitor. Specifically disclosed are a compound as represented by formula (II) and a pharmaceutically acceptable salt thereof.

COMPOUND, ORGANIC ELECTROLUMINESCENCE DEVICE AND ELECTRONIC DEVICE

A novel compound capable of producing an organic electroluminescence (EL) device with excellent properties, an organic EL device comprising the compound, and an electronic device comprising the organic EL device are provided. 2. The compound according to claim 1 , wherein in two or more pairs selected from Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , and Rand R claim 1 , Rand R claim 1 , wherein n is an integer selected from 4 to 6 and 8 to 10 claim 1 , are bonded to each other to form a ring structure together with two ring atoms to which Rand Rare bonded claim 1 , wherein the ring structure has 3 or more atoms composed of a carbon atom claim 1 , an oxygen atom claim 1 , a sulfur atom claim 1 , and a nitrogen atom.3. The compound according to claim 1 , wherein Rto Ris a hydrogen atom or a substituent claim 1 , and the substituent represented by Rto Ris independently a halogen atom claim 1 , a cyano group claim 1 , a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted alkenyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted alkynyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted cycloalky group having 3 to 20 ring carbon atoms claim 1 , an amino group claim 1 , a substituted or unsubstituted alkoxy group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted fluoroalkyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted fluoroalkoxy group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted aryloxy group having 6 to 50 ring carbon atoms claim 1 , a substituted or unsubstituted alkylthio group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted arylthio group having 6 to 50 ring carbon atoms claim 1 , a group represented by —Si(R)(R)(R) claim 1 , a group represented by —N(R)(R) claim 1 , a substituted or unsubstituted aryl group having 6 to 50 ring ...

MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (I): 2. The compound of claim 1 , wherein:{'sub': 1-4', 'p, 'ring A is independently a 6-membered carbocycle, a 9- to 10-membered carbocycle, or a 5- to 10-membered heterocycle comprising: carbon atoms and 1-3 heteroatoms selected from N, NH, N(Calkyl), O, and S(O);'}ring B is independently selected from the group consisting of: imidazole, oxazole, oxadiazole, triazole, pyridine, pyridazine, pyrimidine, and benzene; andring C is independently selected from the group consisting of: benzene, pyridine, indazole, indole, benzimidazole, quinoline, isoquinoline, tetrahydroquinoline, tetrahydroisoquinoline, and quinazoline. This Divisional application claims the benefit of U.S. Ser. No. 13/024,544 filed Feb. 10, 2011 which in turn claims the benefit of U.S. Provisional Application Ser. No. 61/303,423 filed Feb. 11, 2010 and U.S. Provisional Application Ser. No. 61/405,338 filed Oct. 21, 2010, hereby incorporated by reference in their entireties.The present invention relates generally to novel macrocyclic compounds, and their analogues thereof, which are inhibitors of Factor XIa and/or plasma kallikrein, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of thromboembolic disorders.Thromboembolic diseases remain the leading cause of death in developed countries despite the availability of anticoagulants such as warfarin (COUMADIN®), heparin, low molecular weight heparins (LMWH), and synthetic pentasaccharides and antiplatelet agents such as aspirin and clopidogrel (PLAVIX®). The oral anticoagulant warfarin, inhibits the post-translational maturation of coagulation Factors VII, IX, X and prothrombin, and has proven effective in both venous and arterial thrombosis. However, its usage is limited due to its narrow therapeutic index, slow onset of therapeutic effect, numerous dietary and drug interactions, and a need for monitoring and dose adjustment. Thus, discovering and ...

TRICYCLIC HETEROCYCLE DERIVATIVES HAVING HIV REPLICATION INHIBITORY EFFECT

The present invention provides the following compound having anti-HIV activity of formula: 3: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein at least one of conditions 1) to 3) is fulfilled:{'sup': 3', '3C, 'sub': '2', '1) Ais N, NR, O, S, SO, or SO;'}{'sup': 4', '4, 'sub': '2', '2) Ais N, NRC, O, S, SO, or SO; and'}{'sup': '5', '3) Ais N.'}4: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ais R; Ais R; and Ais N.5: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ais or NR; Ais R; and Ais C.6: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ais N or NR; Ais CR; and Ais C or N.7: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ais O or S; Ais CRor N; and Ais C.20: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris alkyl.21: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein n is 1 claim 1 , and Ris alkyloxy.22: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris hydrogen.23: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris substituted or unsubstituted aromatic carbocyclyl claim 1 , substituted or unsubstituted non-aromatic carbocyclyl claim 1 , substituted or unsubstituted aromatic heterocyclyl claim 1 , or substituted or unsubstituted non-aromatic heterocyclyl.24: The compound or pharmaceutically acceptable salt thereof according to claim 1 , wherein Ris alkyl; n is 1 claim 1 , Ris alkyloxy; Ris hydrogen; and Ris substituted or unsubstituted aromatic carbocyclyl claim 1 , substituted or unsubstituted non-aromatic carbocyclyl claim 1 , substituted or unsubstituted aromatic heterocyclyl claim 1 , or substituted or unsubstituted non-aromatic heterocyclyl.25: The compound or pharmaceutically acceptable salt ...

DELAYED FLUORESCENCE COMPOUND, AND ORGANIC LIGHT EMITTING DIODE AND DISPLAY DEVICE USING THE SAME

Discussed is a delayed fluorescence compound of Formula 1: 2. 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.4. The organic light emitting diode according to claim 3 , wherein the organic emitting layer includes a hole injection layer (HIL) claim 3 , a hole transporting layer (HTL) claim 3 , an emitting material layer (EML) claim 3 , an electron transporting layer (ETL) claim 3 , and an electron injection layer (EIL) claim 3 , andwherein at least one from selected from the group consisting of the HIL, the HTL, the EML, the ETL and the EIL includes the delayed fluorescence compound.5. The organic light emitting diode according to claim 3 , 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.6. The organic light emitting diode according to claim 3 , wherein the organic emitting layer further includes a host claim 3 , and the delayed fluorescence compound is used as a dopant.7. The organic light emitting diode according to claim 6 , wherein a difference between a HOMO of the host and a highest occupied molecular orbital (HOMO) of the dopant or a difference between a lowest unoccupied molecular orbital (LUMO) of the host and a LUMO of the dopant is less than 0.5 eV.8. The organic light emitting diode according to claim 3 , wherein the organic emitting layer further includes a dopant claim 3 , and the delayed fluorescence compound is used as a host.9. The organic light emitting diode according to claim 3 , wherein the organic emitting layer further includes a host and a first dopant claim 3 , and the delayed fluorescence compound is used as a second dopant claim 3 , andwherein a triplet energy of the second dopant is smaller than a triplet energy of the host and larger than a triplet energy of ...

DELAYED FLUORESCENCE COMPOUND, AND ORGANIC LIGHT EMITTING DIODE AND DISPLAY DEVICE USING THE SAME

Discussed is a delayed fluorescence compound including a first electron donor moiety of indolo-[3,2,1-j,k]carbazole; a second electron donor moiety selected from indolo-[3,2,1-j,k]carbazole, carbazole, or triphenylamine; and an electron acceptor moiety selected from dibenzothiophene sulfone or diphenyl sulfone, wherein the first and second electron donor moieties are combined to the electron acceptor moiety, and the electron acceptor moiety is combined to a third position or a sixth position of the first electron donor moiety. 1. A delayed fluorescence compound , comprising:a first electron donor moiety of indolo-[3,2,1-j,k]carbazole;a second electron donor moiety selected from the group consisting of indolo-[3,2,1-j,k]carbazole, carbazole, and triphenylamine; andan electron acceptor moiety selected from the group consisting of dibenzothiophene sulfone and diphenyl sulfone,wherein the first electron donor moiety and the second electron donor moiety are combined to the electron acceptor moiety, and the electron acceptor moiety is combined to a third position or a sixth position of the first electron donor moiety.3. The delayed fluorescence compound according to claim 2 , 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.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 delayed fluorescence compound,wherein the delayed fluorescence compound includes a first electron donor moiety of indolo-[3,2,1-j,k]carbazole, a second electron donor moiety selected from the group consisting of indolo-[3,2,1-j,k]carbazole, carbazole, and triphenylamine, and an electron acceptor moiety selected from the group consisting of dibenzothiophene sulfone and diphenyl sulfone,wherein the first ...

ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME

The present disclosure relates to an organic electroluminescent compound represented by formula 1 and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound of the present disclosure, it is possible to provide an organic electroluminescent device having improved operating voltage, luminous efficiency, lifetime, and/or power efficiency. 2. The organic electroluminescent compound according to claim 1 , wherein Bto B claim 1 , each independently claim 1 , are not present or represent a substituted or unsubstituted benzene ring claim 1 , a substituted or unsubstituted naphthalene ring claim 1 , a substituted or unsubstituted pyrrole ring claim 1 , a substituted or unsubstituted furan ring claim 1 , a substituted or unsubstituted thiophene ring claim 1 , a substituted or unsubstituted cyclopentadiene ring claim 1 , a substituted or unsubstituted fluorene ring claim 1 , a substituted or unsubstituted pyridine ring claim 1 , or a substituted or unsubstituted dibenzofuran ring; with the proviso that at least five of Bto Bare present claim 1 , and the adjacent rings of Bto Bare fused with each other.5. The organic electroluminescent compound according to claim 3 , wherein the substituents of the substituted (C1-C30)alkyl(ene) claim 3 , the substituted (C6-C30)aryl(ene) claim 3 , the substituted (3- to 30-membered)heteroaryl(ene) claim 3 , and the substituted (C3-C30)cycloalkyl(ene) in Ar claim 3 , L claim 3 , Rto R claim 3 , and R claim 3 , each independently claim 3 , are at least one selected from the group consisting of deuterium; a halogen; a cyano; a carboxyl; a nitro; a hydroxyl; a (C1-C30)alkyl; a halo(C1-C30)alkyl; a (C2-C30)alkenyl; a (C2-C30)alkynyl; a (C1-C30)alkoxy; a (C1-C30)alkylthio; a (C3-C30)cycloalkyl; a (C3-C30)cycloalkenyl; a (3- to 7-membered)heterocycloalkyl; a (C6-C30)aryloxy; a (C6-C30)arylthio; a (C6-C30)aryl unsubstituted or substituted with at least one selected from the group consisting of ...

COMPOSITIONS AND METHODS FOR TREATING MITOCHONDRIAL DISEASES

The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof. 1. A method for treating a mitochondrial disease in a patient , the method comprising the step of administering a therapeutically effective amount of a compound selected from the group consisting of pirlindole and salts thereof , to the patient.2. The method of wherein the mitochondrial disease is selected from the group consisting of FRDA claim 1 , LHON claim 1 , DAD claim 1 , Leigh's disease claim 1 , NARP claim 1 , MNGIE claim 1 , MERRF claim 1 , MELAS.3. The method of wherein the mitochondrial disease is FRDA.4. The method of wherein the mitochondrial disease is LHON.526.-. (canceled)27. The method of wherein the compound is a pirlindole salt.28. The method of wherein the compound is pirlindole hydrochloride.29. The method of wherein the compound is a pirlindole salt.30. The method of wherein the compound is pirlindole hydrochloride.31. The method of wherein the compound is a pirlindole salt.32. The method of wherein the compound is pirlindole hydrochloride.33. The method of wherein the compound is a pirlindole salt.34. The method of wherein the compound is pirlindole hydrochloride. This application claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application Ser. No. 61/603,763 filed on Feb. 27, 2012, the entire disclosure of which is incorporated herein by reference.The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof.Mitochondrial diseases are a group of disorders caused by ...

DELAYED FLUORESCENCE MATERIAL AND ORGANIC LIGHT EMITTING DEVICE HAVING THE DELAYED FLUORESCENCE MATERIAL

A delayed fluorescence material is disclosed. The delayed fluorescence material has a molecular structure that includes an electron donor unit that donates electrons; and an electron acceptor unit that is coupled to the electron donor unit and accepts electrons, wherein the electron acceptor unit includes an indolocarbazole group having at least one acceptor functional-group bound to the indolocarbazole group. Thus, the delayed fluorescence material exhibits high structural and thermal stability as well as high quantum efficiency. 1. A delayed fluorescence material having a molecular structure , wherein the molecular structure includes an electron donor unit and an electron acceptor unit coupled to the electron donor unit , wherein the electron acceptor unit includes an indolocarbazole group having at least one acceptor functional-group bound to the indolocarbazole group.5. An organic light-emitting device including a light emission layer claim 1 , wherein the layer contains the delayed fluorescence material of .6. An organic light-emitting device including a light emission layer claim 2 , wherein the layer contains the delayed fluorescence material of .7. An organic light-emitting device including a light emission layer claim 3 , wherein the layer contains the delayed fluorescence material of .8. An organic light-emitting device including a light emission layer claim 4 , wherein the layer contains the delayed fluorescence material of .9. An organic light-emitting device including a light emission layer claim 5 , wherein the layer contains the delayed fluorescence material of . The present disclosure relates to a delayed fluorescence material emitting over a long period of time, and an organic electroluminescent device comprising the same.In order to commercialize an organic light emitting device, it is necessary to improve the efficiency of a light emitting material. For this purpose, studies on phosphorescent and delayed fluorescent materials have been actively ...

N-FLUOROALKYL-SUBSTITUTED DIBROMONAPHTHALENE DIIMIDES AND THEIR USE AS SEMICONDUCTOR

The present invention relates to compounds of the formula (I) where Rand Rindependently of each other, are selected from 1H,1H—C-C-perfluoroalkyl and 1H,1H,2H,2H—C-C-perfluoroalkyl, except for the compound of formula (I), where Rand Rare both 1H,1H-perfluorobutyl, and to their use, especially as an n-type semiconductor. 2. The compound according to claim 1 , wherein Rand Rare the same.3. The compound according to claim 1 , is2,6-dibromo-N,N-bis(2,2,2-trifluoroethyl)-naphthalene[1,8:4,5]bis(dicarboximide); or2,6-dibromo-N,N′-bis(1H,1H-perfluoropropyl)-naphthalene[1,8:4,5]bis(dicarboximide).4. A semiconductor claim 1 , comprising the compound according to .5. A thin film semiconductor claim 1 , comprising the compound according to .6. An organic field effect transistor claim 1 , comprisinga substrate comprising at least one gate structure,a source electrode and a drain electrode, and{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'at least one compound according to as a semiconductor material.'}7. The organic field effect transistor according to claim 6 , having a top-gate bottom-contact configuration.8. The organic field effect transistor according to claim 6 , having a bottom-gate bottom-contact configuration.9. A substrate claim 6 , comprisinga plurality of organic field-effect transistors,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein at least some of the field-effect transistors comprising at least one compound according to .'}10. A semiconductor unit claim 9 , comprising at least one substrate according to .11. An organic solar cell claim 1 , comprising at least one compound according to . The present invention relates to N-fluoroalkyl-substituted dibromonaphthalene diimides and their use as semiconductor, in particular as semiconductor in organic electronics.Recent developments in organic-based light-emitting diodes (OLEDs), photovoltaics (OPVs), and field-effect transistors (OFETs) have opened up many opportunities in the field of organic ...

Compositions and Methods for Treatment of Cancer

The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent. 2. The compound of claim 1 , wherein Q is an indolyl group or an indolyl group substituted with one or more substituents independently selected from the group consisting of F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —(C-C) alkyl claim 1 , —(C-C) fluoro-substituted alkyl claim 1 , —(C-C) cycloalkyl claim 1 , —(C-C) fluoro-substituted cycloalkyl claim 1 , —O—(C-C) alkyl claim 1 , —O—(C-C) fluoro-substituted alkyl claim 1 , —O—(C-C) cycloalkyl claim 1 , and —O—(C-C) fluoro-substituted cycloalkyl claim 1 , -aryl claim 1 , —O-aryl claim 1 , —O—(C-C) alkyl-aryl claim 1 , —O—(C-C) alkyl-heterocycle claim 1 , and —S(═O)—(C-C) alkyl.3. The compound of claim 1 , wherein R4 is —CHR7 claim 1 , and R7 is —O—P(═O)(OH) claim 1 , —O—P(═O)(—OH)(—O—(C-C) alkyl) claim 1 , —O—P(═O)(—O—(C-C) alkyl) claim 1 , a carboxylic acid group claim 1 , an amino carboxylic acid group claim 1 , or a peptide.4. The compound of claim 3 , wherein R7 is —O—P(═O)(OH) claim 3 , —O—P(═O)(—OH)(—O—(C-C) alkyl) claim 3 , or —O—P(═O)(—O—C-C)alkyl).5. The compound of claim 3 , wherein R7 is a carboxylic acid group claim 3 , an amino carboxylic acid group claim 3 , or a peptide.6. The compound of claim 5 , wherein R7 is alanine claim 5 , arginine claim 5 , asparagine claim 5 , aspartic acid claim 5 , cysteine claim 5 , glutamine claim 5 , glutamic acid claim 5 , glycine claim 5 , histidine claim 5 , isoleucine claim 5 , leucine claim 5 , lysine claim 5 , methionine claim 5 , phenylalanine claim 5 , proline ...

REDOX ACTIVE TRIANGULAR ORGANIC MATERIALS

A redox-active triangular prism is provided. The redox-active triangular prism includes a plurality of pure enantiomers selected from a group consisting of (−)-NDI-Δ and (+)-NDI-Δ. Methods for their preparation as solvent-templated supramolecular structures and a characterization of their redox-active behavior are provided. 1. A redox-active triangular prism , comprising:a plurality of pure enantiomers selected from a group consisting of (−)-NDI-Δ and (+)-NDI-Δ.2. The redox-active triangular prism of claim 1 , wherein the plurality of pure enantiomers form a structure having a central cavity.3. The redox-active triangular prism of claim 1 , wherein the central cavity comprises sufficient dimensions to accommodate a guest anion.4. The redox-active triangular prism of claim 1 , wherein structure is stabilized through π-π interactions among adjacent members of the plurality of pure enantiomers upon binding a guest anion.5. The redox-active triangular prism of claim 1 , wherein the structure comprises a redox activity of greater than two reversible one-electron cathodic waves.6. The redox-active triangular prism of claim 1 , wherein the plurality of pure enantiomers consist of (−)-NDI-Δ.7. The redox-active triangular prism of claim of claim 6 , wherein the plurality of pure enantiomers form a structure having a central cavity claim 6 , wherein the structure is selected from a group consisting of a right-handed claim 6 , supramolecular (P)-helix claim 6 , an organogel claim 6 , a non-helical supramolecular nanotube and a (P)-helical supramolecular nanotube.8. The redox-active triangular prism of claim of claim 6 , wherein the structure is an organogel comprising a plurality of intertwining supramolecular nanotubes.9. The redox-active triangular prism of claim 1 , wherein the plurality of pure enantiomers consist of (+)-NDI-Δ.10. The redox-active triangular prism of claim 9 , wherein the plurality of pure enantiomers form a structure having a central cavity claim 9 , ...

CYCLIC TRIPEPTIDE MIMETICS AS PLASMIN INHIBITORS

The invention relates to peptide mimetics comprising the residues P4-P3-P2-P1, which were cyclized between the side chains of P3 and P2 amino acid and are, as inhibitors of the serine protease plasmin, suitable to be used to inhibit fibrinolysis and thus to reduce blood loss in hyperfibrinolytic conditions, for example during surgery. 2. Compound according to claim 1 , characterized in that Ris H.3. Compound according to claim 1 , characterized in that Ris H.6. Compound according to claim 1 , characterized in that m equals 0 or 1.8. Medicament claim 1 , comprising at least one compound according to .9. Medicament according to claim 8 , characterized in that it is used in the form of a tablet claim 8 , a dragee claim 8 , a capsule claim 8 , a pellet claim 8 , a suppository claim 8 , a solution claim 8 , in particular an injection or infusion solution claim 8 , of eye claim 8 , nose or ear drops claim 8 , a juice claim 8 , of an emulsion or suspension claim 8 , of a globule claim 8 , a styli claim 8 , an aerosol claim 8 , an aerosol spray claim 8 , a powder claim 8 , a paste claim 8 , a cream or an ointment claim 8 , preferably it is used as injection or infusion solution.10. Utilization of the compounds according to and a medicament comprising at least one of said compounds to reduce blood loss in the case of hyperfibrinolytic conditions.11. Utilization of the compounds according to and a medicament comprising at least one of said compounds to prevent blood loss during surgical procedures claim 1 , in particular during heart surgery and organ transplants claim 1 , but also for the alleviation of severe menstrual bleeding claim 1 , the prevention or alleviation of bleeding during tooth extraction or bleeding gums claim 1 , particularly in patients with hemophilia claim 1 , but also for the therapy of mild forms of hemophilia.12. Utilization of the compounds according to and a medicament comprising at least one of said compounds as agent for the preparation of fibrin ...

Novel Pharmaceutical Intermediates and Methods for Preparing the Same

A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same.

Novel Pharmaceutical Intermediates and Methods for Preparing the Same

A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same. 117-. (canceled)18. A pharmaceutical intermediate , comprising: a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety , an optionally carboxylated azonane moiety , or a second , optionally carboxylated indole moiety , having at least one of an alkyl , allyl , phenylallyl , cinnamyl , alkenyl , and alkyl-alkenyl substituent pendant from a nitrogen atom of the same. This application is a divisional of U.S. application Ser. No. 13/346,815, filed Jan. 10, 2012, entitled “Novel Pharmaceutical Intermediates and Methods for Preparing the Same” which is hereby incorporated herein by reference in its entirety, including all references cited therein.1. Field of the InventionThe present invention relates in general to novel pharmaceutical intermediates and, more particularly, to novel indole derived pharmaceutical intermediates and methods for preparing the same. The novel compounds of the present invention are preferably suitable for participation in direct or multi-step convergent syntheses with other compounds including, but not limited to, aldehyde derived pharmaceutical intermediates, etcetera.2. Background ArtThe commercial development of novel pharmaceutical compounds is, often times, replete with arduous problems relative to transitioning from research and development scale to plant scale synthesis. A plurality of complex issues, including reagent cost, reaction yield, reaction time, competitive side reactions, product isolation and/or purification, disposal of toxic waste and/or byproducts remain largely problematic for the scale-up of most pharmaceutical endeavors. ...

Novel Pharmaceutical Intermediates and Methods for Preparing the Same

A pharmaceutical intermediate including a first indole moiety which is associated with an optionally carboxylated hexahydroazepino moiety, an optionally carboxylated azonane moiety, or a second, optionally carboxylated indole moiety, having an alkyl, allyl, phenylallyl, cinnamyl, alkenyl, and/or alkyl-alkenyl substituent pendant from a nitrogen atom of the same. 18-. (canceled)1318-. (canceled) This application is a divisional of U.S. application Ser. No. 13/346,815, filed Jan. 10, 2012, entitled “Novel Pharmaceutical Intermediates and Methods for Preparing the Same” which is hereby incorporated herein by reference in its entirety, including all references cited therein.1. Field of the InventionThe present invention relates in general to novel pharmaceutical intermediates and, more particularly, to novel indole derived pharmaceutical intermediates and methods for preparing the same. The novel compounds of the present invention are preferably suitable for participation in direct or multi-step convergent syntheses with other compounds including, but not limited to, aldehyde derived pharmaceutical intermediates, etcetera.2. Background ArtThe commercial development of novel pharmaceutical compounds is, often times, replete with arduous problems relative to transitioning from research and development scale to plant scale synthesis. A plurality of complex issues, including reagent cost, reaction yield, reaction time, competitive side reactions, product isolation and/or purification, disposal of toxic waste and/or byproducts remain largely problematic for the scale-up of most pharmaceutical endeavors.Problems associated with preparing novel pharmaceutical compounds can become exponentially difficult when, for example, intermediates comprise delicate compounds where one or more atoms, functional groups, and/or moieties need to be associated with a protecting group during one or more steps of a synthesis. For example, hexahydroazepinoindole-carboxylate intermediates comprise ...

NOVEL MACROCYCLES AS FACTOR XIA INHIBITORS

The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. 17. A pharmaceutical composition comprising one or more compounds according to and a pharmaceutically acceptable carrier or diluent.18. A method for the treatment and/or prophylaxis of a thromboembolic disorder claim 1 , comprising: administering to a patient in need thereof a therapeutically effective amount of a compound of claim 1 , or a stereoisomer claim 1 , a tautomer claim 1 , or a pharmaceutically acceptable salt thereof.19. A method according to claim 18 , wherein the thromboembolic disorder is selected from the group consisting of arterial cardiovascular thromboembolic disorders claim 18 , venous cardiovascular thromboembolic disorders claim 18 , and thromboembolic disorders in the chambers of the heart or in the peripheral circulation.20. A method according to claim 19 , wherein the thromboembolic disorder is selected from unstable angina claim 19 , an acute coronary syndrome claim 19 , atrial fibrillation claim 19 , myocardial infarction claim 19 , transient ischemic attack claim 19 , stroke claim 19 , atherosclerosis claim 19 , peripheral occlusive arterial disease claim 19 , venous thrombosis claim 19 , deep vein thrombosis claim 19 , thrombophlebitis claim 19 , arterial embolism claim 19 , coronary arterial thrombosis claim 19 , cerebral arterial thrombosis claim 19 , cerebral embolism claim 19 , kidney embolism claim 19 , pulmonary embolism claim 19 , and thrombosis resulting from medical implants claim 19 , devices claim 19 , or procedures in which blood is exposed to an artificial surface that ...

SELECTIVE BROMINATION OF PERYLENE DIIMIDES AND DERIVATIVES THEREOF UNDER MILD CONDITIONS

The present invention is directed to novel process for the preparation of regioselective perylenediimides derivatives, specifically mono and dibrominated derivatives. 2. The compound of claim 1 , wherein said metal or metal ion comprises Pd claim 1 , Pt claim 1 , Fe claim 1 , Cu claim 1 , Ag claim 1 , Rh claim 1 , Ir claim 1 , Ru or Os. This application is a Divisional application from U.S. application Ser. No. 13/771,498 filed Feb. 20, 2013, which is a Divisional application from U.S. application Ser. No. 12/599,292 filed Jun. 22, 2010, which is a National Phase application from International Application Number PCT/IL2008/000621 filed May 6, 2008 which claims the benefit of U.S. Ser. No. 60/924,327 filed May 9, 2007, each of which is hereby incorporated by reference in its entirety.The present invention is directed to novel processes for the regioselective preparation of perylenediimides derivatives, specifically mono and dibrominated derivatives.Perylene-diimides (PDIs) are outstanding versatile organic chromophores. They demonstrate exceptional thermal and photochemical stability, strongly absorb visible light, and show high fluorescence quantum yields. PDIs have been utilized as industrial dyes, electronic materials, sensors, photovoltaics, and building blocks for light-harvesting and artificial photosynthetic systems. Importantly, photophysical and redox properties of PDIs can be conveniently modified through substitution in the aromatic core at the positions 1,6, 7, and 12 (bay region). Substitutions at bay positions and expansion of the PDI core are usually carried out starting from the halogenated derivatives, particularly brominated PDIs. These are almost exclusively synthesized through bromination of perylene dianhydride (PDA) in concentrated HSOupon heating, followed by imidation with amines. Usually this bromination procedure affords a mixture of di-, tri- and tetrabrominated PDIs. The dibromoperylene diimides contain 1,7 (major) and 1,6 (minor) ...

Process for obtaining optically active pirlindole enantiomers and salts thereof

The present invention provides a new process for obtaining optically active pirlindole enantiomers, in the form of a free base or in the form of pharmaceutically acceptable salts. The products obtained according to the present invention are enantiomerically pure and are useful in medicine.

CRYSTALLINE (8S,9R)-5-FLUORO-8-(4-FLUOROPHENYL)-9-(1-METHYL-1H-1,2,4-TRIAZOL-5-YL)-8,9-DIHYDRO-2H-PYRIDO[4,3,2-DE]PHTHALAZIN-3(7H)-ONE TOSYLATE SALT

Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer. 1. A (8S ,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1 ,2 ,4-triazol-5-yl)-8 ,9-dihydro-2H-pyrido[4 ,3 ,2-de]phthalazin-3(7H)-one tosylate salt.2. The (8S claim 1 ,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1 claim 1 ,2 claim 1 ,4-triazol-5-yl)-8 claim 1 ,9-dihydro-2H-pyrido[4 claim 1 ,3 claim 1 ,2-de]phthalazin-3(7H)-one tosylate salt of claim 1 , where the salt is in a substantially pure crystalline form.3. The (8S claim 1 ,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1 claim 1 ,2 claim 1 ,4-triazol-5-yl)-8 claim 1 ,9-dihydro-2H-pyrido[4 claim 1 ,3 claim 1 ,2-de]phthalazin-3(7H)-one tosylate salt of claim 1 , where the salt is a crystalline form exhibiting at least one of{'sup': '13', 'a solid state C NMR spectrum with peaks at 143.2, 136.0, 131.8, 123.9, 112.2, 105.2, and 100.3 ppm±0.2 ppm;'}a differential scanning calorimetry thermogram having an endotherm with a maximum at between about 320° C. and about 335° C.;a thermogravimetric analysis thermogram indicative of an unsolvated material;a dynamic vapor sorption isotherm plot which does not exhibit a significant weight change from 0 to 95% relative humidity;an X-ray powder diffraction pattern comprising characteristic peaks expressed in d-values (Å) of about 11.9, 5.9, 4.9, 4.4, 4.3, 3.9, and 3.7; andan X-ray powder diffraction pattern comprising peaks at 2θ angle degrees±0.2 2 ...

Organic Electroluminescent Device; A Charge Transporting Material For The Organic Electroluminescent Device; And A Luminescent Device, A Display Device And A Lighting System Using The Organic Electroluminescent Device

An organic electroluminescent element comprising a substrate; a pair of electrodes including an anode and a cathode, disposed on the substrate; and at least one organic layer including a light emitting layer, disposed between the electrodes, wherein the light emitting layer includes a compound represented by the following general formula: 1. A compound having Formula I:{'br': None, 'sup': 1', '2, 'sub': 'n', 'G\ue8a0L-G),\u2003\u2003Formula I;'}{'sup': '1', 'wherein Gis a monocyclic or polycyclic ring formed by a single bond between atoms selected from the group consisting of trivalent boron, trivalent nitrogen, divalent oxygen, divalent sulfur, and divalent selenium;'}{'sup': '1', 'wherein Ghas at least one trivalent boron;'}{'sup': 1', '1', '9', '1, 'wherein an unused valence on boron and nitrogen after forming a ring in Gmay be attached to L or to a substituent selected from R-R, or may form an additional ring fused to G;'}wherein n is an integer from 1 to 20;wherein L is a direct bond or an organic linker;{'sup': 1', '9', '2, 'wherein R-Rand Gare each independently selected from the group consisting of hydrogen, deuterium, halide, alkyl, cycloalkyl, heteroalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carbonyl, carboxylic acids, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, a boron containing group, and combinations thereof;'}wherein any two adjacent substituents can optionally join or fuse to form a ring;{'sup': '2', 'wherein at least one of Gis selected from the group consisting of dibenzofuran, dibenzothiophene, dibenzoselenphene, triphenylene, azadibenzofuran, azadibenzothiophene, azadibenzoselenphene, azatriphenylene, triazine, pyrimidine, pyridine, and quinazoline;'}provided that the triphenylene group is not fused to any additional rings.2. The compound of claim 1 , wherein Gis a monocyclic ring.3. The compound of claim 1 , wherein Gis a polycyclic ring.4. The ...

NOVEL TRICYCLIC COMPOUNDS AND PROCESS FOR PREPARATION THEREOF

The present invention relates to novel tricyclic compounds of formula (I) and (II) More particularly, the present invention relates to novel tricyclic compounds of formula (I) and (II) and process of preparation of these compounds from 4,5-di-methyl-o-phenylinediamine. Further, the present invention relates to a process for preparation of tricyclic compound hunanamycin A. 3. The tricyclic compounds of formula (I) and formula (II) according to for use as an antibacterial agent.4Salmonella enterica.. The tricyclic compounds of formula (I) and formula (II) according to claim 3 , wherein the antibacterial activity is against5. The tricyclic compounds of formula (I) and formula (II) according to claim 1 , wherein the compound is 7 claim 1 ,7 claim 1 ,8 claim 1 ,9-tetramethyl-2-((2 claim 1 ,3 claim 1 ,4 claim 1 ,5-tetrahydroxypentyl)oxy)-6 claim 1 ,7-dihydro-3H claim 1 ,5H-pyrido[1 claim 1 ,2 claim 1 ,3-de]quinoxalin-3-one.6. A process for the preparation 7 claim 5 ,7 claim 5 ,8 claim 5 ,9-tetramethyl-2-((2 claim 5 ,3 claim 5 ,4 claim 5 ,5-tetrahydroxypentyl)oxy)-6 claim 5 ,7-dihydro-3H claim 5 ,5H-pyrido[1 claim 5 ,2 claim 5 ,3-de]quinoxalin-3-one according to claim 5 , comprising the following steps:a) refluxing the mixture of 4,5-dimethyl-o-phenylinediamine dissolved in 4N HCL and oxalic acid for overnight to obtain 6,7-dimethyl-1,4-dihydroquinoxaline-2,3-dione,{'sub': 2', '3, 'b) adding cesium carbonate (CsCO), 3,3-dimethylallyl bromide to a solution of compound of step (a) in dry DMF followed by stirring to obtain mono alkylated and dialkylated 6,7-dimethyl-1-(3-methylbut-2-en-1-yl)-1,4-dihydro-quinoxaline-2,3-dione,'}{'sub': '3', 'c) heating the reaction mixture of compound of step (b) and AlClin chlorobenzene up to 120° C. for 12 hrs to obtain 7,7,8,9-tetramethyl-6,7-dihydro-1H,5H-pyrido[1,2,3-de]quinoxaline-2,3-dione,'}d) adding triphenylphosphine, protected sugar, diisopropyl azodicarboxylate to a solution compound of step (c) in dry THF followed by stirring to ...

FULLERENE DERIVATIVE, AND METHOD OF PREPARING THE SAME

A fullerene derivative having 60 or more carbon atoms, includes at least one specific structure. This patent application is based on and claims priority pursuant to 35 U.S.C. §119 to Japanese Patent Application No. 2013-255722, filed on Dec. 11, 2013, in the Japan Patent Office, the entire disclosure of which is hereby incorporated by reference herein.1. Technical FieldThe present invention relates to a new fullerene derivative useful as an organic semiconductive material and a method of preparing the same.2. Description of the Related ArtOrganic semiconductive materials are well studied in an organic electronics field such as organic transistors and organic ELs. Further, an organic solar battery using a fullerene derivative as an organic photoelectric conversion element is strenuously studied. As the most famous fullerene derivative in this field, [6,6]-phenylC61-butyric methyl ester (PCBM) which is soluble in an organic solvent is disclosed in J. Org. Chem. 1995, 60, 532-538. A functional group having a suitable size is introduced to the fullerene and solubility in an organic solvent is adjusted to increase an area of a pn bonded interface which is a charge generation area and photoelectric conversion efficiency. However, the photoelectric conversion efficiency is still insufficient, and a better fullerene derivative is required.Japanese published unexamined applications Nos. JP-2011-26235-A, JP-2011-35116-A, JP-2011-77486-A, JP-2011-93848-A, JP-2011-98906-A and JP-2011-121886-A disclose fullerene derivatives various functional groups are introduced to for the purpose of improving an open end voltage and expanding absorption wavelength area. Bulky functional groups are introduced to the fullerenes to improve solubility in an organic solvent, and further, compatibility with a p-type semiconductive material is increased to improve photoelectric conversion efficiency. However, being short of solubility in an organic solvent, these are unable to construct a close bulk ...

FUSED TETRA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARP INHIBITORS

Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof. 5. The at least one compound of any one of - , having a PARP-inhibiting activity corresponding to a ICof 10 μM or less in a PARP enzyme assay.6. The at least one compound of any one of - , having a PARP-Pyralation activity corresponding to a ECof 10 uM or less in a PARP cellular assay.7. A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier and as an active ingredient a therapeutically effective amount of the at least one compound of any one of -.8. A method of treating cancer responsive to inhibition of PARP comprising administering to a subject in recognized need thereof at least one compound of any one of - in an amount effective to inhibit said PARP.9. Use of at least one compound of any one of - in the manufacture of medicaments for the treatment of at least one disease responsive to inhibition of PARP. This application is a continuation of U.S. patent application Ser. No. 14/369,374 filed on Mar. 6, 2015, now U.S. Pat. No. 9,260,440, with the title “FUSED TETRA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARP INHIBITORS” which is a U.S. national stage application of International Application No. PCT/CN2011/085148, which was filed on Dec. 31, 2011 with the title “FUSED TETRA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARP INHIBITORS”, the content of each of which are hereby incorporated by reference in its entirety for all purposes.Disclosed herein are fused tetra or penta-cyclic compounds which can inhibit the activity of poly (ADP-ribose)polymerases (PARPs), pharmaceutical compositions comprising at least one of the compounds, and the use thereof in treating certain diseases.Poly(ADP-ribose) polymerases (PARPs), previously known as poly(ADP-ribose) synthases or poly(ADP-ribose) transferases, are a family of proteins that contain PARP catalytic domain (2005 Oct. 4; 6: 139). Approximately 17 ...

HEXAHYDRODIAZEPINOQUINOLINES CARRYING A CYCLIC RADICAL

The present invention relates to tricyclic hexahydrodiazepinoquinolines carrying a cyclic substituent, to a method for producing them, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HTreceptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HTreceptor, to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HTreceptor, and processes for preparing such compounds and compositions. 2. The compound as claimed in claim 1 , where Ris selected from hydrogen and C-C-alkyl.3. The compound as claimed in claim 2 , where Ris hydrogen.4. The compound as claimed in any of the preceding claims claim 2 , where Ris selected from C-C-alkyl claim 2 , fluorinated C-C-alkyl claim 2 , C-C-alkoxy-C-C-alkyl and fluorinated C-C-alkoxy-C-C-alkyl.5. The compound as claimed in claim 4 , where Ris selected from C-C-alkyl and fluorinated C-C-alkyl.6. The compound as claimed in claim 5 , where Ris selected from methyl and CF.7. The compound as claimed in any of the preceding claims claim 5 , where Rand R claim 5 , independently of each other claim 5 , are selected from hydrogen claim 5 , cyano claim 5 , nitro claim 5 , C-C-alkyl and fluorinated C-C-alkyl.8. The compound as claimed in claim 7 , where Ris selected from hydrogen claim 7 , cyano claim 7 , nitro claim 7 , C-C-alkyl and fluorinated C-C-alkyl; and Ris hydrogen.9. The compound as claimed in claim 8 , where Ris selected from hydrogen and methyl; and Ris hydrogen.10. The compound as claimed in claim 9 , where Rand Rare hydrogen.11. The compound as claimed in any of the preceding claims claim 9 , where Rand R claim 9 , independently of each other claim 9 , are selected from hydrogen claim 9 , C-C-alkyl claim 9 , fluorinated C-C-alkyl claim 9 , C-C-alkoxy-C-C-alkyl and fluorinated C-C-alkoxy-C-C-alkyl claim 9 , or form ...

ORGANIC ELECTROLUMINESCENCE

A nitrogen-containing heterocyclic compound wherein a pyrrole ring, an aromatic ring and a 7-membered ring are fused one another, a material for organic electroluminescence device including the compound, and an organic electroluminescence device including the material. 4. The material for organic electroluminescence device according to claim 1 , wherein each of the groups referred to in formulae (1) to (3) is independently selected from a substituted or unsubstituted alkyl group having 1 to 50 carbon atoms; a substituted or unsubstituted cycloalkyl group having 5 to 50 ring carbon atoms; a substituted or unsubstituted aryl group having 6 to 50 ring carbon atoms; an aralkyl group having 7 to 51 total carbon atoms having a substituted or unsubstituted aryl group having 6 to 50; an amino group; a mono- or di-substituted amino group having a substituent selected from a substituted or unsubstituted alkyl group having 1 to 50 carbon atoms and a substituted or unsubstituted aryl group having 6 to 50 ring carbon atoms; an alkoxy group having a substituted or unsubstituted alkyl group having 1 to 50 carbon atoms; an aryloxy group having a substituted or unsubstituted aryl group having 6 to 50 ring carbon atoms; a mono- claim 1 , di- or tri-substituted silyl group having a substituent selected from a substituted or unsubstituted alkyl group having 1 to 50 carbon atoms and a substituted or unsubstituted aryl group having 6 to 50 ring carbon atoms; a substituted or unsubstituted heterocyclic group having 5 to 50 ring atoms; a substituted or unsubstituted haloalkyl group having 1 to 50 carbon atoms; a halogen atom; a cyano group; a nitro group; a sulfonyl group having a substituent selected from a substituted or unsubstituted alkyl group having 1 to 50 carbon atoms and a substituted or unsubstituted aryl group having 6 to 50 carbon atoms; and a di-substituted phosphoryl group having a substituent selected from a substituted or unsubstituted alkyl group having 1 to 50 carbon ...

INHIBITORS OF HCV NS5A

The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection. 2. The compound of claim 1 , wherein X is H claim 1 , each Ris H claim 1 , and each Ris C(═O)OCH.3. The compound of claim 2 , A is biphenyl.4. The compound of claim 3 , wherein Ris isopropyl.5. The compound of claim 4 , wherein Yis H.6. The compound of claim 5 , wherein Yis H.7. The compound of claim 4 , wherein Yis F.8. The compound of claim 7 , wherein Yis H9. The compound of claim 4 , wherein Yis F.10. The compound of claim 9 , wherein Yis F.11. A compound selected from the group consisting of:{(2S,5S)-2-[(S)-2-(4′-{2-[(S)-1-((S)-2-Methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl]-3H-imidazol-4-yl}-biphenyl-4-ylcarbamoyl)-pyrrolidine-1-carbonyl]-4-oxo-1,2,4,5,6,7-hexahydro-azepino[3,2,1-hi]indol-5-yl}-carbamic acid methyl ester;{(4S,7S)-4-[(S)-2-(4′-{2-[(S)-1-((S)-2-Methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl]-3H-imidazol-4-yl}-biphenyl-4-ylcarbamoyl)-pyrrolidine-1-carbonyl]-6,10-dioxo-octahydro-pyridazino[1,2-a][1,2]diazepin-7-yl}-carbamic acid methyl ester;{(2S,5S)-2-[(S)-2-(4′-{2-[(S)-1-((S)-2-Methoxycarbonylamino-3-methyl-butyryl)-4,4-difluoropyrrolidin-2-yl]-3H-imidazol-4-yl}-biphenyl-4-ylcarbamoyl)-pyrrolidine-1-carbonyl]-4-oxo-1,2,4,5,6,7-hexahydro-azepino[3,2,1-hi]indol-5-yl}-carbamic acid methyl ester; and{(2S,5S)-2-[(S)-2-(4′-{5-Chloro-2-[(S)-1-((S)-2-methoxycarbonylamino-3-methyl-butyryl)-pyrrolidin-2-yl]-3H-imidazol-4-yl}-biphenyl-4-ylcarbamoyl)-pyrrolidine-1-carbonyl]-4-oxo-1,2,4,5,6,7-hexahydro-azepino[3,2,1-hi]indol-5-yl}-carbamic acid methyl ester.1217-. (canceled)18. A method for treating a Hepatitis C Virus (HCV) infection comprising administering to a patient in need thereof a therapeutically effective amount of a compound of .19. A method of treating a Hepatitis ...

SALTS AND POLYMORPHS OF 8-FLUORO-2--1,3,4,5-TETRAHYDRO-6H-AZEPINO[5,4,3-CD]INDOL-6-ONE

The present invention relates to novel polymorphic forms of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer. 1. A camsylate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1 ,3 ,4 ,5-tetrahydro-6H-azepino[5 ,4 ,3-cd]indol-6-one.2. The salt of claim 1 , wherein the salt is amorphous.3. The salt of claim 1 , wherein the camsylate is S-camsylate.4. The salt of claim 1 , wherein the camsylate is R-camsylate.5. The salt of claim 1 , wherein the salt has a solid state NMR spectrum comprising one or more 13C chemical shifts selected from the group consisting of 213.4±0.2 claim 1 , 171.8±0.2 claim 1 , and 17.3±0.2 ppm.6. The salt of claim 1 , wherein the salt has a solid state NMR spectrum comprising one or more 19F chemical shifts selected from the group consisting of −118.9±0.2 and −119.7 ppm±0.2.7. A maleate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1 claim 1 ,3 claim 1 ,4 claim 1 ,5-tetrahydro-6H-azepino[5 claim 1 ,4 claim 1 ,3-cd]indol-6-one.8. The salt of claim 7 , wherein the salt is amorphous.9. The salt of claim 7 , wherein the salt has a solid state NMR spectrum comprising one or more 13C chemical shifts selected from the group consisting of 171.3±0.2 claim 7 , 112.4±0.2 claim 7 , and 43.8±0.2 ppm.10. The salt of claim 7 , wherein the salt has a solid state NMR spectrum comprising a 19F chemical shift at −123.1 ppm±0.2.11. A pharmaceutical composition comprising the salt of and a pharmaceutically acceptable carrier.12. A pharmaceutical composition comprising the salt of and a pharmaceutically acceptable carrier. This application is a continuation of U.S. application Ser. No. 13/522,549, filed Jul. 17, 2012, entitled “Salts and Polymorphs of 8- ...

NOVEL COMPOUND HAVING PARP INHIBITORY ACTIVITY

A compound represented by the following general formula (1) or a salt thereof. Rrepresents a halogen atom and so on; Rand Reach represent a hydrogen atom and so on; Rand Reach represent a hydrogen atom and so on, or Rand Rmay form an oxo group; Rand Reach represent a lower alkyl group optionally having a substituent and so on, or they may bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural R; Rrepresents an aryl group optionally having a substituent and so on; ring A represents a benzene ring and so on; and m represents 0, 1 or 2. 2. The compound according to or a salt thereof claim 1 , wherein in the general formula (1) claim 1 ,{'sup': '1', 'Rrepresents a halogen atom or a lower alkyl group;'}{'sup': 2', '3, 'Rand Rmay be the same or different and each represent a hydrogen atom, a halogen atom or a lower alkyl group;'}{'sup': 4', '5', '4', '5, 'Rand Rmay be the same or different and each represent a hydrogen atom, a deuterium atom or a lower alkyl group, or Rand Rmay form an oxo group;'}{'sup': a', 'b, 'Rand Rmay be the same or different and each represent a hydrogen atom, a lower alkyl group or an aryl group, and the lower alkyl group or the aryl group may be substituted by a deuterium atom, an aryl group, a heterocyclic group, an amino group or a lower alkylamino group;'}{'sup': a', 'b', 'c, 'Rand Rmay bind to each other to form a nitrogen-containing heterocyclic ring which may be substituted by one or plural R;'}{'sup': 'c', 'Rrepresents a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclic group, a hydroxy group, a lower alkoxy group, a lower alkylcarbonyl group, a lower cycloalkylcarbonyl group, a lower alkylaminocarbonyl group, a lower cycloalkylaminocarbonyl group, a lower alkoxycarbonyl group, an amino group, a lower alkylamino group or a carboxyl group, and the lower alkyl group, the lower cycloalkyl group, the aryl group, the heterocyclic group, the lower alkoxy group, the ...

Superstructures of diketopyrrolopyrrole donors and perylenediimide acceptors formed by hydrogen-bonding and pi...pi stacking

A quantitative model that describes the assembly of diketopyrrolopyrrole-based donors and a perylenediimide acceptor into chiral superstructures, as a result of both hydrogen bonding and π•••π stacking. This model provides thermodynamic parameters (ΔH° and ΔS°) for all noncovalent interactions involved in the assembly and explains the subtle supramolecular cues that convert disordered aggregates into well-defined helical assemblies.

CHEMICAL SELF-DOPING OF ONE-DIMENSIONAL ORGANIC NANOMATERIALS FOR HIGH CONDUCTIVITY APPLICATION IN CHEMIRSISTIVE SENSING GAS OR VAPOR

A chemiresistive vapor sensor compound for detecting target vapors can comprise a perylene-tetracarboxylic diimide (PTCDI) core according to structure (I): 2. The chemiresistive sensor compound of claim 1 , wherein R is a straight C-Calkyl chain or a branched C-Calkyl group.3. The chemiresistive sensor compound of claim 1 , wherein A claim 1 , A′ claim 1 , or both are a carbon-based linking group.4. The chemiresistive sensor compound of claim 1 , wherein A claim 1 , A′ claim 1 , or both comprise at least one of a C-Calkylene group claim 1 , a C-Ccycloalkylene group claim 1 , and a phenylene group.5. The chemiresistive sensor compound of claim 1 , wherein A claim 1 , A′ claim 1 , or both are 0.8 nm to 2 nm or alternatively 5 carbons to 12 carbons in length measured by carbon-carbon single bond length.6. The chemiresistive vapor sensor compound of claim 1 , wherein D claim 1 , D′ claim 1 , or both create a ΔG<0 for formation of the anionic PTCDI radical.10. The chemiresistive vapor sensor compound of claim 1 , wherein R—Rare independently hydrogen claim 1 , C-Calkyl groups claim 1 , or a combination thereof.11. The chemiresistive vapor sensor compound of claim 1 , wherein the electron transfer occurs from the electron donor portion of one chemiresistive vapor sensor compound to the PTCDI portion of another chemiresistive vapor sensor compound claim 1 , generating an anionic radical of PTCDI without photo-excitation.12. A chemiresistive vapor sensor for detection of a target compound claim 1 , the sensor comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a. an assembly of nanofibers formed of the chemiresistive sensor compound of ; and'}b. a pair of electrodes operatively oriented about the assembly of nanofibers to allow electrical current to pass from a first electrode in the pair of electrodes through the assembly of nanofibers and to a second electrode in the pair of electrodes.13. The chemiresistive vapor sensor of claim 12 , wherein the nanofibers are ...

HETEROARYL COMPOUNDS FOR KINASE INHIBITION

Compounds and pharmaceutical compositions that modulate kinase activity, including mutant EGFR and mutant HER2 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mutant EGFR and mutant HER2 activity, are described herein. 14. The compound according to claim 1 , wherein Xis CR.15. The compound according to or claim 1 , wherein Xis CH.16. The compound according to or claim 1 , wherein Xis N.17. The compound of any one of or - claim 1 , wherein Xis CR.18. The compound according to claim 1 , wherein Xis N.19. The compound of any one of or - claim 1 , wherein Xis CR.20. The compound of any one of or - claim 1 , wherein Xis N.21. The compound according to claim 1 , wherein Z claim 1 , Z claim 1 , and Zare each independently selected from CRR claim 1 , NRand O.22. The compound according to claim 21 , wherein Z claim 21 , Z claim 21 , and Zare each independently selected from CRR.23. The compound according to claim 22 , wherein Rand Rare each H.24. The compound according to claim 1 , wherein Zis CRR.25. The compound according to claim 24 , wherein Zis selected from CRR claim 24 , NR claim 24 , and O.26. The compound according to claim 25 , wherein Zis selected from CRR claim 25 , NR claim 25 , and O.27. The compound according to claim 1 , wherein Zis CH claim 1 , Zis CRR claim 1 , and Zis O.28. The compound according to claim 1 , wherein Zis CH claim 1 , Zis CH claim 1 , and Zis NR.29. The compound according to claim 1 , wherein Zis CH claim 1 , Zis CRRwhere Rand Rare taken together with the carbon atom to which they are attached to form an oxo group claim 1 , and Zis O or NR.30. The compound according to or wherein Zis NMe.31. The compound according to claim 1 , wherein Zis CRRwhere Rand Rare taken together with the carbon atom to which they are attached to form an oxo group claim 1 , Zis CH claim 1 , and Zis selected from CRR claim 1 , O and NR.32. The compound ...

FUSED TETRA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARP INHIBITORS

Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof. 5. The at least one compound of claim 1 , having a PARP-inhibiting activity corresponding to a ICof 10 μM or less in a PARP enzyme assay.6. The at least one compound of claim 1 , having a PARP-Pyralation activity corresponding to a ECof 10 uM or less in a PARP cellular assay.7. A pharmaceutical composition comprising at least one pharmaceutically acceptable carrier and as an active ingredient a therapeutically effective amount of the at least one compound of .8. A method of treating cancer responsive to inhibition of PARP comprising administering to a subject in recognized need thereof at least one compound of in an amount effective to inhibit said PARP.9. (canceled) Disclosed herein are fused tetra or penta-cyclic compounds which can inhibit the activity of poly (ADP-ribose)polymerases (PARPs), pharmaceutical compositions comprising at least one of the compounds, and the use thereof in treating certain diseases.Poly(ADP-ribose) polymerases (PARPs), previously known as poly(ADP-ribose) synthases or poly(ADP-ribose) transferases, are a family of proteins that contain PARP catalytic domain (2005 Oct. 4; 6: 139.). Approximately 17 members of PARPs have been discovered so far, including PARP-1, PARP-2, PARP-3, PARP-4(Vault-PARP), PARP-5a (Tankyrase-1), PARP5b (Tankyrase-2), PARP-6, PARP-7 (tiPARP), PARP-8, PARP-9 (BALI), PARP-10, PARP-11, PARP-12, PARP-13 (ZAP), PARP-14 (CoaSt6), PARP-15, and PARP-16. The catalytic activity of PARPs can be to transfer the ADP-ribose moiety from nicotinamide adenine dinucleotide (NAD) to glutamic acid residues of a number of target proteins, and to form long branches of ADP-ribose polymers. However, some of the PARP families have been reported to catalyze only mono-ADP-ribosylation of targets while activities of others have yet to be reported (2008 Oct. 10; 32(1): 57-69.). A number of the PARP enzymes have been ...

SUBSTITUTED TERRYLENE AND QUATERRYLENE DERIVATES AND USE AS SEMICONDUCTORS THEREOF

Disclosed are terrylene and quaterrylene derivates of general formula (I) and the use thereof as organic semiconductor materials. 4: The compound according to claim 1 , wherein Rand Rare the same.5: The compound according to claim 1 , wherein X claim 1 , X claim 1 , Xand Xare the same.6: The compound according to claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rand claim 1 , if present claim 1 , R claim 1 , R claim 1 , Rand Rare all hydrogen.8: An organic field-effect transistor claim 1 , comprising a substrate comprising a gate structure claim 1 , a source electrode and a drain electrode and a compound of the formula I as defined in as a semiconductor material.9: A substrate comprising a plurality of organic field-effect transistors claim 1 , wherein one or more of the field-effect transistors comprise the compound of the formula I as defined in .10: A semiconductor unit comprising the substrate as defined in .11: An electroluminescent arrangement comprising an upper electrode claim 1 , a lower electrode claim 1 , wherein at least one electrode is transparent claim 1 , an electroluminescent layer and optionally an auxiliary layer claim 1 , wherein the electroluminescent arrangement comprises the compound of the formula I as defined in .12: The electroluminescent arrangement as claimed in further comprising a hole-injecting layer claim 11 , wherein the hole-injecting layer or the transparent electrode comprises the compound of the formula I.13: The electroluminescent arrangement as claimed in in the form of an organic light-emitting diode (OLED).14: An organic solar cell comprising the compound of the formula (I) as defined in .15: A semiconductor material claim 1 , comprising the compound of the general formula I as defined in .16: The semiconductor material of claim 15 , which is present in an organic field-effect transistor. It is expected that, in the future, not only the classical inorganic semiconductors but ...

MATERIAL FOR ORGANIC ELECTROLUMINESCENCE DEVICE AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

A material for an organic electroluminescence (EL) device and an organic EL device, the material being represented by the following Formula 1: 2. The material for an organic EL device as claimed in claim 1 , wherein:{'sup': 1', '2, 'at least one of Arand Aris a substituted or unsubstituted heteroaryl group, and'}{'sup': 1', '2', '3, 'L, L, and Lare each independently a single bond or a substituted or unsubstituted arylene group having 6 to 18 ring carbon atoms.'}3. The material for an organic EL device as claimed in claim 1 , wherein Arand Arare each independently a substituted or unsubstituted aryl group having 6 to 24 ring carbon atoms for forming a ring claim 1 , a substituted or unsubstituted carbazolyl group claim 1 , a substituted or unsubstituted dibenzofuryl group claim 1 , or a substituted or unsubstituted dibenzothienyl group.5. The organic EL device as claimed in claim 4 , wherein the material is a hole transport material.6. The organic EL device as claimed in claim 4 , wherein:the organic EL device includes an emission layer and an anode, andthe material is included in a layer that is between the emission layer and the anode.9. The organic EL device as claimed in claim 4 , wherein the material is one of the following Compounds 37 to 52:18. The organic EL device as claimed in claim 4 , wherein:{'sup': 1', '2, 'at least one of Arand Aris a substituted or unsubstituted heteroaryl group, and'}{'sup': 1', '2', '3, 'L, L, and Lare each independently a single bond or a substituted or unsubstituted arylene group having 6 to 18 ring carbon atoms.'}19. The organic EL device as claimed in claim 4 , wherein Arand Arare each independently a substituted or unsubstituted aryl group having 6 to 24 ring carbon atoms for forming a ring claim 4 , a substituted or unsubstituted carbazolyl group claim 4 , a substituted or unsubstituted dibenzofuryl group claim 4 , or a substituted or unsubstituted dibenzothienyl group. Japanese Patent Application No. 2013-264433, filed on ...

ERGOLINE COMPOUNDS AND USES THEREOF

Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT, 5-HTand 5-HTreceptors without agonizing the 5-HTreceptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HTadrenergic alphaand/or the alphareceptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein. 123-. (canceled)25. The compound of claim 24 , wherein Ris hydrogen or methyl.26. The compound of claim 25 , wherein Ris independently selected from hydrogen claim 25 , —CF claim 25 , cyclopropyl or cyclopentyl.27. The compound of claim 26 , wherein Rand R claim 26 , together with the atoms to which they are joined claim 26 , form a double bond.28. The compound of claim 26 , wherein Ris independently selected from fluorine or OR.29. The compound of claim 28 , wherein Ris independently selected from hydrogen or methyl.30. The compound of claim 27 , wherein Ris a (C-C)alkyl substituted with an —OH group and one or more fluorine atoms.31. The compound of claim 27 , wherein Ris a (C-C)alkyl substituted with an —OH group32. The compound of claim 29 , wherein Ris a (C-C)alkyl substituted with an —OH group.33. The compound of claim 27 , wherein Ris a (C-C)alkyl substituted with an —OCHgroup.34. The compound of claim 30 , wherein Ris cyclopropyl.35. The compound of claim 31 , wherein Ris cyclopropyl.36. The compound of claim 32 , wherein Ris cyclopropyl.37. The compound of claim 33 , ...

ERGOLINE COMPOUNDS AND USES THEREOF

Provided herein are ergoline compounds and pharmaceutical compositions thereof. In some embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT, 5-HTand 5-HTreceptors without agonizing the 5-HTreceptor using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the 5-HTadrenergic alphaand/or the alphareceptors using the compounds and pharmaceutical compositions disclosed herein. In still other embodiments, provided herein are methods of antagonizing the D2 and D3 receptor using the compounds and pharmaceutical compositions disclosed herein. 123-. (canceled)25. The compound of claim 24 , wherein Rand R claim 24 , together with the atoms to which they are joined claim 24 , form a 5 membered ring;26. The compound of claim 24 , wherein Ris hydrogen27. The compound of claim 26 , wherein Ris cyclopropyl.28. The compound of claim 26 , wherein Ris hydrogen.29. The compound of claim 26 , wherein Ris CF.30. The compound of or claim 26 , wherein Rand Rare ethyl.31. The compound of claim 28 , wherein Rand Rare CF.32. The compound of or claim 28 , wherein Rand Rare CHCF.33. The compound of claim 28 , wherein Ris ethyl and Ris CF.34. The compound of claim 28 , wherein Ris ethyl and Ris CHCF.37. The compound of claim 36 , wherein Ris methyl.38. The compound of claim 37 , wherein Ris hydrogen.39. The compound of claim 37 , wherein Ris independently selected from cyclopropyl or cyclopentyl.40. The compound of claim 37 , wherein Rand Ralong with the atoms to which they are attached form a 5 membered ring.41. The compound of or claim 37 , wherein Ris ORand Ris independently selected from hydrogen or methyl.42. The compound of claim 39 , ...

CRYSTALLINE OF CAMPHORSULFONIC ACID SALT OF RUCAPARIB AND METHOD OF PREPARING OF TRICYCLIC COMPOUNDS, RUCAPARIB AND CRYSTALLINE OF CAMPHORSULFONIC ACID SALT OF RUCAPARIB

A method of preparing a tricyclic compound of formula (I), comprising the step of converting a compound of formula (II) into a compound of formula (III); and hydrogenating the compound of formula (III) in the presence of hydrogenation catalyst and hydrogen to form the tricyclic compound of formula (I); wherein Ris H or a Calkyl group; and Ris H, a halogen element or a Calkyl group. 2. The method of claim 1 , wherein the step of converting the compound of formula (II) into the compound of formula (III) comprises reacting the compound of formula (II) with methylamine to form the compound of formula (III).3. The method of claim 1 , wherein the hydrogenation catalyst is at least one selected from the group consisting of Pd catalyst claim 1 , Ni catalyst claim 1 , Pt catalyst and Rh catalyst.4. The method of claim 1 , wherein the step of converting the compound of formula (II) and the step of hydrogenating the compound of formula (III) are performed in succession without isolating the compound of formula (III).9. The method of claim 8 , wherein the pharmaceutically acceptable acid is camphorsulfonic acid.12. The crystalline (S)-camphorsulfonate salt of Rucaparib of claim 11 , wherein the X-ray powder diffraction pattern further comprises characteristic peaks at two theta values of 12.0°±0.2° and 25.7°±0.2°.13. The crystalline (S)-camphorsulfonate salt of Rucaparib of claim 11 , wherein the X-ray powder diffraction pattern is substantially the same as that shown in .14. The crystalline (S)-camphorsulfonate salt of Rucaparib of claim 11 , wherein the melting point thereof is about 304±2° C. This application claims priority to CN application No. 201811423037.X filed on Nov. 27, 2018, which is herein incorporated by reference in its entirety.The present invention is related to a method of preparing of tricyclic compounds. More particularly, the present invention is related to a method of preparing of tricyclic compounds for PARP inhibitor. The present invention is further ...

1,9-DIAZAPHENALENE DERIVATIVE AND PROCESS FOR MANUFACTURING THE SAME

A 1,9-diazaphenalene derivative is represented by 3. The 1 claim 1 ,9-diazaphenalene derivative according to claim 1 , wherein each R is independently selected from the group consisting of phenyl claim 1 , 4-methylphenyl claim 1 , 4-methoxyphenyl claim 1 , 4-bromophenyl claim 1 , 4-trifluoromethylphenyl and 2-thienyl.5. The process according to claim 4 , wherein a molar ratio of the benzamidine derivative to the alkyne compound ranges from 1:2 to 1:3.5.6. The process according to claim 5 , wherein the molar ratio of the benzamidine derivative to the alkyne compound ranges from 1:3 to 1:3.5.7. The process according to claim 4 , wherein the oxidant is selected from the group consisting of copper (II) acetate claim 4 , copper (II) acetate monohydrate claim 4 , and copper trifluoromethanesulfonate.8. The process according to claim 4 , wherein the rhodium-containing complex is selected from the group consisting of [Cp*Rh(CHCN)](SbF)and [RhCp*Cl] claim 4 , wherein Cp* represents pentamethylcyclopentadienyl.9. The process according to claim 4 , wherein the ruthenium-containing complex is [RuCl(p-cymene)] claim 4 , wherein Cp* represents pentamethylcyclopentadienyl.10. The process according to claim 4 , wherein the catalystic reaction is conducted in the presence of an organic solvent.11. The process according to claim 10 , wherein the organic solvent is selected from the group consisting of 2-methyl-2-butanol claim 10 , dimethylformamide claim 10 , o-xylene claim 10 , dichloroethane claim 10 , acetonitrile and acetic acid.12. The process according to claim 4 , wherein X represents hydroxyl.14. The process according to claim 13 , wherein a molar ratio of the benzonitrile compound to the alkyne compound ranges from 1:2 to 1:3.5. This application claims priority of Taiwanese Application No. 103145258, filed on Dec. 24, 2014.The disclosure relates to a 1,9-diazaphenalene derivative, and more particularly to a 1,9-diazaphenalene derivative which is highly substituted. The ...

DIIMIDE COMPOUNDS

The invention relates to novel compounds which are naphthalene diimides of general formula (I): 2. A compound according to claim 1 , wherein Xand Xare N-methyl piperazine.3. A compound according to claim 1 , wherein two of groups X claim 1 , X claim 1 , Yand Yare morpholino.4. A compound according to claim 3 , wherein Yand Yare morpholino.5. A compound according to claim 4 , wherein p and q are both 2.6. A compound according to claim 1 , wherein Xand Xare N-methyl piperazine; wherein Yand Yare morpholino; and wherein p and q are both 2.8. A method for the treatment or prophylaxis of cancer comprising administering to a subject a compound according to claim 1 , or a salt claim 1 , solvate or prodrug thereof.9. A method according to claim 8 , wherein the cancer is prostate cancer claim 8 , lung cancer claim 8 , renal cancer claim 8 , pancreatic cancer claim 8 , breast cancer claim 8 , or melanoma.10. A method according to claim 8 , wherein Xand Xare N-methyl piperazine.11. A method according to claim 8 , wherein two of groups X claim 8 , X claim 8 , Yand Yare morpholino.12. A method according to claim 11 , wherein Yand Yare morpholino.13. A method of preparation of a pharmaceutical composition claim 11 , the method comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'obtaining a compound according to , and'}combining the compound with a pharmaceutically acceptable carrier.14. A method according to claim 13 , wherein Xand Xare N-methyl piperazine.15. A method according to claim 13 , wherein two of groups X claim 13 , X claim 13 , Yand Yare morpholino.16. A method according to claim 13 , wherein Yand Yare morpholino.17. A pharmaceutical composition comprising a compound according to .18. A pharmaceutical composition according to claim 17 , wherein Xand Xare N-methyl piperazine.19. A pharmaceutical composition according to claim 17 , wherein two of groups X claim 17 , X claim 17 , Yand Yare morpholino.20. A pharmaceutical composition according to claim 19 , ...

ORGANIC SEMICONDUCTING COMPOUNDS COMPRISING A TETRAAZAPYRENE CORE

The present invention relates to organic semiconducting compounds of formula (I) wherein Xis C, Si or Ge; Xis , S or Se; and Xis N or P as well as to organic electronic devices comprising such organic semiconducting compounds. (I) 3. Compound according to claim 1 , wherein Xis C.4. Compound according to claim 1 , wherein Xis S.5. Compound according to claim 1 , wherein Xis N.6. Compound according to claim 1 , wherein at least one of Rand R—if present—are independently of each other an electron withdrawing group R.7. Compound according to claim 1 , wherein at least one of Rand R—if present—are independently of each other an electron withdrawing group R.9. Compound according to claim 1 , wherein said compound is an oligomer or a polymer.10. A mixture or a blend comprising one or more compounds of and one or more compounds or polymers selected from the group consisting of binders and compounds or polymers having semiconducting claim 1 , charge transport claim 1 , hole transport claim 1 , electron transport claim 1 , hole blocking claim 1 , electron blocking claim 1 , electrically conducting claim 1 , photoconducting or light emitting properties.11. Formulation comprising the compound of and an organic solvent.12. The use of the compound of as charge transport claim 1 , semiconducting claim 1 , electrically conducting claim 1 , photoconducting or light emitting material claim 1 , preferably as n-type semiconducting material claim 1 , in optical claim 1 , electrooptical claim 1 , electronic claim 1 , electroluminescent or photoluminescent components or devices.13. Charge transport claim 1 , semiconducting claim 1 , electrically conducting claim 1 , photoconducting or light emitting material comprising the compound of .14. A component or device comprising the compound of claim 1 , said component or device being selected from the group consisting of organic field effect transistors (OFET) claim 1 , thin film transistors (TFT) claim 1 , integrated circuits (IC) claim 1 , ...

COMPOUND, ORGANIC ELECTROLUMINESCENCE DEVICE AND ELECTRONIC DEVICE

A novel compound capable of producing an organic electroluminescence (EL) device with excellent properties, an organic EL device comprising the compound, and an electronic device comprising the organic EL device are provided. 2. The compound according to claim 1 , wherein in two or more pairs selected from Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , and Rand R claim 1 , Rand R claim 1 , wherein n is an integer selected from 4 to 6 and 8 to 10 claim 1 , are bonded to each other to form a ring structure together with two ring atoms to which Rand Rare bonded claim 1 , wherein the ring structure has 3 or more atoms composed of a carbon atom claim 1 , an oxygen atom claim 1 , a sulfur atom claim 1 , and a nitrogen atom.3. The compound according to claim 1 , wherein Rto Ris a hydrogen atom or a substituent claim 1 , and the substituent represented by Rto Ris independently a halogen atom claim 1 , a cyano group claim 1 , a substituted or unsubstituted alkyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted alkenyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted alkynyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted cycloalky group having 3 to 20 ring carbon atoms claim 1 , an amino group claim 1 , a substituted or unsubstituted alkoxy group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted fluoroalkyl group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted fluoroalkoxy group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted aryloxy group having 6 to 50 ring carbon atoms claim 1 , a substituted or unsubstituted alkylthio group having 1 to 20 carbon atoms claim 1 , a substituted or unsubstituted arylthio group having 6 to 50 ring carbon atoms claim 1 , a group represented by —Si(R)(R)(R) claim 1 , a group represented by —N(R)(R) claim 1 , a substituted or unsubstituted aryl group having 6 to 50 ring ...

GENES AND PROCESSES FOR THE PRODUCTION OF CLAVINE-TYPE ALKALOIDS

Microorganisms and processes for the recombinant manufacture of clavine-type alkaloids such as cycloclavine, festuclavine, agroclavine, chanoclavine and chanoclavine aldehyde, as well as polypeptides, polynucleotides and vectors comprising such polynucleotides which can be applied in a method for the manufacture of clavine-type alkaloids are provided. 1. A recombinant microorganism comprising:a) at least one EasH activity, orb) at least one EasH and EasD activity, orc) at least one EasH and EasA reductase activity, ord) at least one EasH, EasD and EasA activity, ore) at least one EasH and EasD, EasA reductase and EasG activity, orf) at least one DmaW, EasF, EasE, EasC, EasD, EasH, EasA and EasG activity, org) at least one EasD, EasA and EasG activity, orh) at least one DmaW, EasF, EasE, EasC, EasD, EasA reductase and EasG activity, ori) at least one DmaW, EasF, EasE, EasC, EasD, EasA isomerase and EasG activity, orj) at least one DmaW, EasF, EasE and EasC activity, or 'wherein the recombinant microorganism is not a natural ergot alkaloid producer organism.', 'k) a combination of at least two of a) to j).'}2. A recombinant natural ergot alkaloid producer organism having at least one up-regulated activity selected from the group of activities consisting of: DmaW , EasF , EasE , EasC , EasD , EasH , EasA and EasG activity , wherein the EasA activity is an EasA reductase , an EasA isomerase or an EasA reductase and EasA isomerase activity.3. A recombinant natural ergot alkaloid producer organism as claimed in claim 2 , wherein the at least one up-regulated activity is selected from the activities of one or more of the groups of:a) at least one EasH activity, orb) at least one EasH and EasD, orc) at least one EasH and EasA reductase activity, ord) at least one EasH, EasD and EasA activity, ore) at least one EasH and EasD, EasA reductase and EasG activity, orf) at least one DmaW, EasF, EasE, EasC, EasD, EasH, EasA and EasG activity, org) at least one EasD, EasA and EasG ...

Process for the preparation of pirlindole enantiomers and its salts

The present invention relates to an improved process for the preparation of Pirlindole enantiomers, or a pharmaceutically acceptable salt thereof.

Use of substituted benzodiazepinones and benzazepinones or the salts thereof as active substances against abiotic plant stress

The use of substituted benzodiazepinones and benzazepinones of the general formula (I) or salts thereof where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and to selected processes for preparing the compounds mentioned above.