НОВЫЕ ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ И СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ КАМПТОТЕЦИНА (СРТ-11) И РОДСТВЕННЫХ СОЕДИНЕНИЙ

Описываются новые промежуточные продукты камптотецина общей формулы (I), где Ra представляет собой атом хлора, низшую алкоксигруппу, Rb представляет собой атом водорода, С1-8алкил, гидроксиС1-8алкил, группу -С(O)Н или группу (a), Rc представляет собой группу, выбранную из ряда формул (II-IХ) или Rb и Rc вместе образуют остаток формулы -СН2-O-С(O)-С(ОН)(R6)- или -СН2-О-СН(ОН)-С(ОН)(R6)-, Rd представляет собой атом хлора или группу C(O)OR4, R3 представляет собой атом водорода или бензил, R4 представляет собой С1-8алкил, R5 представляет собой атом водорода, R6 представляет собой С1-8алкил, R7 представляет собой атом водорода. Соединения являются эффективными противораковыми лекарственными средствами. Описывается также способ получения производных камптотецина (СРТ-11) и родственных соединений. 6 с. и 50 з.п. ф-лы.

СПОСОБЫ ИНГИБИРОВАНИЯ ТИРОЗИНКИНАЗЫ РЕЦЕПТОРА ЭПИДЕРМАЛЬНОГО ФАКТОРА РОСТА, БИЦИКЛИЧЕСКИЕ ПРОИЗВОДНЫЕ ПИРИМИДИНА, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ ИНГИБИРУЮЩЕЙ ТИРОЗИНКИНАЗУ РЕЦЕПТОРА ЭПИДЕРМАЛЬНОГО ФАКТОРА РОСТА АКТИВНОСТЬЮ, И КОМПОЗИЦИЯ, ОБЛАДАЮЩАЯ КОНТРАЦЕПТИВНЫМ ДЕЙСТВИЕМ

Изобретение относится к новым бициклическим производным пиримидина или их фармацевтически приемлемым солям, способу ингибирования тирозинкиназы рецептора эпидермального фактора роста, в частности при лечении раковых заболеваний, фармацевтической композиции, обладающей ингибирующей тирозинкиназу рецептора фактора эпидермального роста активностью, а также композиции, обладающей контрацептивным действием. Предлагаемые соединения соответствуют общей формуле I, где 1 - 2 из радикалов А - Е означает азот, а остальные радикалы - углерод или два смежных радикала А - Е вместе представляют гетероатом из группы азот, сера, при этом А - Е вместе с прилегающими атомами углерода означают пиридиновое, пиримидиновое, тиенильное, пиррольное, имидазольное кольцо; Х - группы NH, NHR5, где R5 означает низший алкил с 1 - 4 атомами углерода; n = 0, 1 или 2; R отсутствует или означает водород, алкил с 1 - 4 атомами углерода, алкоксил с 1 - 4 атомами углерода, нитрогруппу, галоген, перфторалкил с 1 - 4 атомами ...

КУМАРИНХИНОЛОНКАРБОНОВЫЕ КИСЛОТЫ И СПОСОБ ИХ ПОЛУЧЕНИЯ

Изобретение относится к новым кумаринхинолонкарбоновым кислотам, в которых система пиридона конденсирована в 3,4-, 6,7- и 7,8-положениях кумариновой системы, общей формулы I где R1R2 = NHCH=C(CO2R6)CO, R3 = NO2 или NH2, R4 = R5 = H, R6 = H или C2H5; R1R2 = NHCH=C(CO2R6)CO, R3 = R4 = H, R5 = F, R6 = H или С2Н5; R1R2 = СО(СО2R6)С = СНNH, R3 = R4 = R5 = H, R6 = H или С2Н5; R1R2 = R3R4 = NHCH= C(CO2R6)CO, R5 = H, R6 = H или С2Н5; R1 = Н или ОН, R2 = R5 = Н, R3R4 = -NHCH=C(CO2R6)CO,R6 = H или С2Н5; R1 = ОН, R2 = R3 = Н, R4 R5 = -СО(СО2R6)С = СНNH, R6 = H или С2Н5; R1 = R5 = Н, R2 - СН3 или CF3, R3R4 = CO(CO2 R6)C = CHNH, R6 = H или С2Н5, а также к их фармацевтически приемлемым солям. Новые соединения являются ингибиторами испытанных штаммов бактерий, ингибируют рост клеток рака молочной железы, рака поджелудочной железы и рака гортани. Описываются также способы получения новых соединений. 3 с. и 18 з.п.ф-лы, 10 табл.

СПОСОБ ПОЛУЧЕНИЯ КОНДЕНСИРОВАННЫХ ПОЛИЦИКЛИЧЕСКИХ АЛКАЛОИДОВ, СОЕДИНЕНИЯ, СПОСОБ ИНДУЦИРОВАНИЯ АПОПТОЗА

Изобретение относится к способу получения конденсированных полициклических алкалоидов общей формулы I, в том числе и новых, включающему стадию циклизации азометинилида общей формулы II, где А - необязательно замещенный арил, Z - кислород, n = 1, Y -необязательно замещенный арил, W и Х вместе с атомами азота и углерода, к которым они присоединены, образуют насыщенную или ненасыщенную азотсодержащую гетероциклическую группу, возможно замещенную и возможно конденсированную с арильной, карбоциклической или гетероциклической группой. Соединения I индуцируют апоптоз в клетках с множественной лекарственной устойчивостью, что усиливает противоопухолевое терапевтическое действие лекарственных средств. 5 с. и 50 з.п. ф-лы, 2 табл.

ГЕТЕРОАРИЛЬНЫЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Изобретение относится к соединению формулы (I):в которой n равен 1 или 2; каждый X независимо представляет собой N или CR; каждый Z независимо представляет собой N или С; каждый Y независимо представляет собой N или CR; при условии, чтосодержит 2 или 4 атомов азота в кольце; Rпредставляет собой водород или C-Салкил; каждый Rнезависимо представляет собой (i) водород, галоген, C-Салкил; или (ii) два смежных Rсовместно с атомами углерода, к которым они присоединены, образуют 5-10-членное гетероарильное кольцо, содержащее один атом N; В представляет собой,или; (i) Rи Rсовместно с атомами, к которым они присоединены, образуют моноциклическое 6-10-членное арильное кольцо, моноциклическое 5-10-членное гетероарильное кольцо, содержащее один атом N, замещенное C-Салкилом, С-Сциклоалкилом, галогеном, галоген C-Салкокси C-Салкилом; или бициклическое 5-10-членное гетероарильное кольцо, содержащее один атом N, замещенное галогеном, или бициклическое 5-10-членное гетероарильное кольцо, содержащее 3 гетероатома ...

ВЕЩЕСТВО С ПРОТИВОВИРУСНОЙ И АНТИБАКТЕРИАЛЬНОЙ АКТИВНОСТЬЮ НА ОСНОВЕ ПРОИЗВОДНЫХ 2,8-ДИТИОКСО-1H-ПИРАНО[2,3-D, 6,5-D`] ДИПИРИМИДИНА И ИХ 10-АЗА-АНАЛОГОВ

Изобретение относится к новому веществу, обладающему антивирусной и антибактериальной активностью на основе производных 2, 8-дитиоксо-1Н-пирано[2,3-d; 6,5-d']дипиримидина и их 10-аза-аналогов, отличающееся тем, что включает производное указанной группы общей формулы А1 * М: где Х выбран из группы: О, NH, N-Alkyl; R1 выбран из группы: Н, ОН, Cl, O-Alkyl, NH2, NH-Alkyl, NH-Ar, N(Alkyl)2, SH, S-Alkyl; R2 выбран из группы: фенилнезамещенный или замещенный, нафтил,тиенил; R3 выбран из группы: Н, Cl, O-Alkyl, NH2, NH-Alkyl, S- дигидроксипиримидинил; М либо отсутствует, либо выбран из группы: катион Na, К, Li, аммония, или любой другой фармакологически приемлемый катион; либо комплекс фармакологически приемлемого катиона (см. выше) с анионом одного из производных А1 (варианты R1-R3 заданы выше). Технический результат - получение новых соединений, обладающих противовирусной и антибактериальной активностью. 1 н. и 16 з.п. ф-лы, 7 табл.

НОВЫЕ ПРОИЗВОДНЫЕ ПИРИДО[3, 2: 4, 5]ФУРО[3, 2-D]ПИРИМИДИНА

... 1. Производное пиридофуропиримидина формулы (I): ! ! где G1 представляет собой группу, выбранную из -CR6R7 - и -О-, где R6 и R7 независимо представляют собой атомы водорода или С1-4 алкильные группы; ! R1 и R2 независимо выбраны из атомов водорода и С1-4 алкильных групп; ! R3 представляет собой группу, выбранную из С1-4алкила, С1-4алкокси, амино, гидрокси, моно-С1-4алкиламино, ди-С1-4алкиламино, С3-8циклоалкиламино, арила, гетероарила и насыщенных N-содержащих гетероциклильных групп, которые связаны с пиридиновым циклом через их атом азота, причем каждая из которых необязательно замещена одним или несколькими заместителями, выбранными из группы, состоящей из атомов галогена и гидрокси, С1-4алкила, С1-4алкокси-С1-4алкила, арил-С1-4алкила, -O(CO)O R8, С1-4алкокси, -(CO)NR8R9, -CN, -CF3, -NR8R9, -SR8 и -SO2NH2 групп, где R8 и R9 каждый независимо представляет собой атом водорода или С1-4алкильную группу; ! R4 и R5 независимо выбраны из группы, состоящей из атомов водорода, С1-4алкильных групп ...

СПИРОЦИКЛИЧЕСКИЕ АЗАИНДОЛЬНЫЕ ПРОИЗВОДНЫЕ

... 1. Спироциклические азаиндольные производные общей формулы I ! ! в которой А означает N или CR7-10, причем А по меньшей мере один раз и самое большее ! дважды означает N ! W означает NR4 ! Х означает NR17, О или S ! R1 и R2, независимо друг от друга означают Н; C1-5-алкил каждый раз насыщенный или ненасыщенный, разветвленный или неразветвленный, монозамещенный или полизамещенный или незамещенный; С3-8-циклоалкил, каждый раз монозамещенный или полизамещенный или незамещенный; или связанный C1-3-алкилом арил, С3-8-циклоалкил или гетероарил, каждый раз монозамещенный или полизамещенный или незамещенный; ! или остатки R1 и R2 вместе означают CH2CH2OCH2CH2, CH2CH2NR10CH2CH2 или (СН2)3-6, ! причем R10 означает Н; C1-5-алкил, каждый раз насыщенный или ненасыщенный, разветвленный или неразветвленный, монозамещенный или полизамещенный или незамещенный, С3-8-циклоалкил, каждый раз монозамещенный или полизамещенный или незамещенный; арил-, или гетероарил, каждый раз монозамещенный или полизамещенный ...

АНТИБАКТЕРИАЛЬНЫЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

... 1. Соединение формулы (I), формулы (II) или формулы (III):или его форма, гдеX представляет собой связь, N(R), S, O, -CH(R)-, -CH(R)-CH(R)-, -CH(R)-CH(R)-CH(R)-, -C(R)=C(R)-, -C(R)=C(R)-CH(R)-, -CH(R)-C(R)=C(R)-, -O-CH(R)-, -CH(R)-O-, -N(R)-CH(R)-, -CH(R)-N(R)-, -S-CH(R)-, -CH(R)-S-, -O-CH(R)-CH(R)-, -CH(R)-O-CH(R)-, -CH(R)-CH(R)-O-, -N(R)-CH(R)-CH(R)-, -CH(R)-N(R)-CH(R)-, -CH(R)-CH(R)-N(R)-, -S-CH(R)-CH(R)-, -CH(R)-S-CH(R)-, -CH(R)-CH(R)-S-; -O-C(O)-CH(R)-, -C(O)-O-CH(R)-, -CH(R)-O-C(O)-, -CH(R)-C(O)-O-, -N(R)-C(O)-CH(R)-, -C(O)-N(R)-CH(R)-, -CH(R)-N(R)-C(O)-, -CH(R)-C(O)-N(R)-, -S-C(O)-CH(R)-, -C(O)-S-CH(R)-, -CH(R)-S-C(O)- или -CH(R)-C(O)-S-;Yпредставляет собой -N(R)- или -O-;Yпредставляет собой -C(R)-, -N(R)- или -O-; где пунктирная линия представляет собой двойную связь, которая присутствует, если Yпредставляет собой -C(R)- и отсутствует, если Yпредставляет собой -N(R)- или -O-;Z представляет собой N(R), S, O, C(O) или -CH(R)-;Rпредставляет собой водород, галоген, гидроксил, оксо, циано ...

АЗАГЕТЕРОЦИКЛЫ, КОМБИНАТОРНАЯ БИБЛИОТЕКА, ФОКУСИРОВАННАЯ БИБЛИОТЕКА, ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ ПОЛУЧЕНИЯ

... 1. Азагетероциклы общей формулы 1 где R1a представляет собой заместитель аминогруппы; Rb и Rc вместе с атомом углерода, с которым они связаны, образуют карбонильную группу, атом углерода которой находится в цикле; R1d и R2d вместе с атомом углерода, с которым они связаны, образуют карбонильную группу, атом углерода которой находится в цикле; Х представляет собой группу NR2a, атом азота которой находится в цикле, a R2aпредставляет собой заместитель аминогруппы; W, Y и Z вместе образуют метиленовую группу CR3dR4d, в которой R3d и R4d, независимо друг от друга, представляют собой заместитель циклической системы или R3d и R4d вместе с атомом углерода, с которым они связаны, образуют через R3d и R4d циклоалкил или гетероциклил; или R2a, вместе с атомом азота с которым он связан, и R3d, вместе с атомом углерода, с которым он связан, замыкают через R2aи R3d азагетероцикл; или где R1a представляет собой заместитель аминогруппы; Rb представляют собой карбамоильную группу; Rc представляют собой заместитель ...

ЗАМЕЩЕННЫЕ ПИРАЗОЛОАЗЕПИН-4-ОНЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ФОСФОДИЭСТЕРАЗЫ

PROCESS FOR PREPARING 4-AMINOPYRIDINE DERIVATIVES

Способ получения производных бензимидазола

Beta-carbolinderivate, Ligande für Benzodiazepinrezeptoren mit agonistischer Inverse und Benzodiazepinantasonistische Wirkungen und diese enthaltende Arzneimittel

PYRANO-PYRAZOL-DERIVATE

SUBSTITUTED HEXAHYDRO ARYLQUINOLIZINES

New 2-alkoxy-4-halo-6-alkylphenyl-substituted (hetero)cyclic ketoenols, useful as total or selective herbicides and pesticides, e.g. insecticides, acaricides and nematocides for plant protection

... 2-Alkoxy-4-halo-6-alkylphenyl-substituted cyclic keto-enol compounds (I), derived from pyrrole, furan, thiophene, pyran, 1,3-thiazine, cyclopentane, cyclohexane or pyrazole, are new. Also new are 19 classes of intermediates, e.g. 2-alkoxy-4-halo-6-alkylphenylacetic acids (XXVII) and various ester or amide derivatives. Cyclic keto-enol derivatives of formula R-Ar (I) are new. Ar : 2-alkoxy-4-halo-6-alkylphenyl; R : cyclic keto-enol residue of formula (a) - (c); T 1N(D), O or S; T 2-C(A)=C(D)-O-, -C(A)(B)-C(Q 1>)(Q 2>)-, -C(A)(B)-C(Q 3>)(Q 4>)-C(Q 5>)(Q 6>)- or -N(A)-N(D)-; A : H; alkyl, alkenyl, alkoxyalkyl or alkylthioalkyl (all optionally substituted (os) by halo); os, optionally unsaturated cycloalkyl (optionally having at least one ring atom replaced by a heteroatom); or aryl, aralkyl or heteroaryl (all os by halo, alkyl, haloalkyl, alkoxy, haloalkoxy, CN or NO 2); B : H, alkyl or alkoxyalkyl; or C(A)(B) : os, (un)saturated ring (optionally containing heteroatom(s)); D : H; or alkyl, ...

PYRANOÄ2,3-cÜIMIDAZOÄ1,2-aÜPYRIDIN-DERIVATE ZUR BEHANDLUNG VON GASTROINTESTINALEN ERKRANKUNGEN

IMIDAZOPYRROLOPYRIDINE UND KONDENSIERTE DERIVATE DAVON ALS ZWISCHENPRODUKTE FUER DIE HERSTELLUNG VON HERBIZIDEN VERBINDUNGEN.

IMIDAZOPYRROLOPYRIDINE UND KONDENSIERTE DERIVATE DAVON ALS ZWISCHENPRODUKTE FUER DIE HERSTELLUNG VON HERBIZIDEN VERBINDUNGEN.

Verfahren zur Herstellung neuer heterocyclischer Verbindungen

Polynuclear heterocyclic compounds

The invention comprises compounds of the general formula or (wherein X represents oxygen or sulphur, and R1 and R2 represent alkyl or aryl groups or members of a further aromatic or cycloaliphatic ring), and the preparation thereof by the following processes: (a) reacting 5- or 6-hydrazine derivatives of the dihydrofurano- or dihydrothiophene-quinaldine series with carbonyl compounds; (b) treating 4-hydroxy-5:6-pyrrole- or indolequinaldines according to process (a) of Specification 703,277; (c) treating primary 5- or 6-aminoindoles or 2- or 3-aminocarbazoles according to process (b) of Specification 703,277. The products possess amoebicidal activity and form water-soluble salts with mineral acids, e.g. halogen hydracids, sulphuric, phosphoric and nitric acids. In examples: (1) the 6-hydrazine compound obtained from the amino compound of example (2) of Specification 703,277 by diazotization and reduction of the diazo compound with stannous chloride ...

BENZ[5,6]ISOINDOLO[2,1-B]ISOQUINOLINES

A process for the manufacture of 2-oxo-benzoquinolizine derivatives

... 2-Oxo-benzoquinolizines of general formula wherein R1 represents an alkyl group of 1-6 carbon atoms, R2 and R3 each represent an alkyl group of 1-4 carbon atoms, R4, R5 and R6 each represent an alkoxy group of 1-4 carbon atoms and R4 and R5 may together form a methylenedioxy or ethylenedioxy group, the broken lines indicating optional substituents, are manufactured by reacting a 3,4-dihydroisoquinoline of formula in a basic medium with an alkyl vinyl ketone of formula The products are characterized by their oximes and/or acid addition salts. 3,4-Dihydro-isoquinolines of the second general formula above are prepared by converting the corresponding b -phenyl-ethylamine to its formamide and cyclising this by the Bischler-Napieralski reaction. Hydrochlorides may be obtained. Alkyl vinyl ketones of the third general formula above may be obtained by condensing saturated ketones with aldehydes, or by dehydrating carbinols, ...

Functionalized heterocycles as chemokine receptor modulators.

The present invention is a novel series functionalized heterocycles as chemokine receptor modulators of Formula (I) useful as modulators of chemokine receptor activity. The compounds are useful in the treatment and prevention of the AIDS virus. Intermediates useful in the preparation of the final products, pharmaceutical compositions containing the final products are also taught.

Nodulisporic acid derivative spot-on formulations for combating parasites

Inhibitors of HIV integrase enzyme

Nodulisporic acid derivative spot-on formulations for combating parasites

Naphtyridinones-1,8 substituted, proceeded for their obtaining and pharmaceutical compositions the container.

Functionalized heterocycles as chemokine receptor modulators.

Polycylic quinoline, naphthyridine and pyrazinopyridine derivatives.

Nodulisporic acid derivative spot-on formulations for combating parasites

Nodulisporic acid derivative spot-on formulations for combating parasites

Inhibitors of HIV integrase enzyme

Functionalized heterocycles as chemokine receptor modulators

CYCLOPENTA (D) PYRAZOLO (1,5-A) PYRIMIDIN VERBINDUN AS CRF RECEPTOR ANTAGONIST

PYRANO, PIPERIDINO, AND THIOPYRANO DERIVATIVES AND METHOD FOR USE

TRICYCLI CONDENSED HETERO-CYCLIC CONNECTIONS AS CRF ANTAGONIST

VERFARHREN FOR PRODUCTION NEW 2,3,5,8-TETRAHYDROFURO AND/OR 5,8-DIHYDROFURO-1,8-NAPHTHYRIDINE-VERBINDUNG

VERFAHREN ZUR HERSTELLUNG VON NEUEN SALZEN VON ALKALOIDDERIVATEN VON THIOPHOSPHORSAEURE

VERFAHREN ZUR HERSTELLUNG VON BENZO (A) CHINOLIZIDIN-DERIVATEN UND DEREN SALZEN

VERFAHREN ZUR HERSTELLUNG VON NEUEN PYRIMIDO (1,2-A)BENZIMIDAZOLDERIVATEN

MULTICYCLI CONNECTIONS AND THEIR USE AS INHIBITORS OF THE PARP, VEGFR2 AND MLK3 OF ENZYMES

SUBSTITUTED PYRIDOÄ3',2':4,5ÜTHIENOÄ3,2 DÜPYRIMIDINE AND PYRIDOÄ3',2':4,5ÜFUROÄ3,2-DÜ PYRIMIDINE FOR USE AS INHIBITORS OF THE PDA-4 AND/OR TNF ALPHA RELEASE

TRICYCLI CONNECTIONS AND THEIR USE AS MGLUR1-ANTAGONISTEN

BENZOPYRAN FARBMITTEL, PRODUCTION AND USE

NEW CHELIDONIN DERIVATIVES, PROCEDURES FOR YOUR PRODUCTION AND YOUR USE FOR THE PRODUCTION OF PHARMACEUTICAL ACTIVE SUBSTANCES

REGIOSELEKTIVE, METAL-CATALYZED SYNTHESIS OF ANNELIERTER BENZIMIDAZOLE AND AZABENZIMIDAZOLE

SULFONE ACID DERIVATIVES OF POLYCYCLI COLORING MATERIALS FOR ANALYTIC APPLICATIONS

PROCEDURE FOR THE PRODUCTION OF NEW CONDENSED PYRIMIDINEN AND THEIR SALTS

PROCEDURE FOR the PRODUCTION OF NEW PYRIMIDO (6.1-A) ISOCHINOLIN-4-ON-DERIVATEN AND YOUR SALTS

BETA CARBOLINDERIVATE ONE, LIGANDE FOR BENZODIAZEPINREZEPTOREN WITH AGONISTI INVERSE ONE AND BENZODIAZEPINANTASONISTI EFFECTS AND THESE CONTAINING DRUGS

CONDENSED IMIDAZOPYRIDINDERIVATE WITH PSYCHOTROPI EFFECT

TETRAHYDROPYRANOCHINOLINDERIVATE

2, 4, 6-PHENYLSUBSTITUIERTE CYCLI KETOENOLE

BENZIMIDAZOLDERIVATE AS SELECTIVE ONES SÄUREPUMPENHEMMER

PROCEDURE FOR THE PRODUCTION OF NEW SALTS OF ALKALOID DERIVATIVES OF THIOPHOSPHORSAEURE

4-AMINOPYRIDINDERIVATE.

SUBSTITUTED HEXAHYDROARYLCHINOLIZINE.

IMIDAZOPYRROLOPYRIDINE AND CONDENSED DERIVATIVES OF IT AS INTERMEDIATE PRODUCTS FOR THE PRODUCTION OF HERBICIDES CONNECTIONS.

NEW HERBICIDES

ANTIALLERGI IMIDAZOAZEPINE

EXTENDED RHODAMINVERBINDUNGEN USABLE AS FLUORESCENT ONE MARKING MEANS

ANNELIERTE HETEROCYCLEN, A PROCEDURE FOR THE PRODUCTION OF THE CONNECTIONS AND MEDICINES, THIS CONTAINING

(3,4-A: 3,4-C) CARBAZOLDERIVATE, PROCEDURE FOR YOUR PRODUCTION AND THESE CONTAINING PHARMACEUTICAL PREPARATIONS

PYRROLOINDOLE, PYRIDOINDOLE AND AZEPINOINDOLE AS 5-HT2C AGONISTEN

PROCEDURE FOR the PRODUCTION OF IMIDAZO (1,2-C) (2, 3) BENZODIAZEPINEN AND INTERMEDIATE PRODUCTS WHEN THEIR PRODUCTION

Procedure for the production of new N-hetero-cyclic connections

4-AMINOPYRIDINE DERIVATIVES

ANTIHYPERTENSIVE PYRANO(3,2-C) PYRIDINES

Heterocyclic cyclopamine analogs and methods of use thereof

The present invention relates to steroidal alkaloid-like compounds that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.

Heterocyclic cyclopamine analogs and methods of use thereof

2-(hetero)-aryl-substituted tetrahydroquinoline derivatives

Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative, and inflammatory disorders

The present invention provides compounds of the following structure, wherein R, R, R, R, R, R, and R are defined above: These compounds are useful in treating neurological disorders or complications due to stroke or head injury; benign or malignant neoplastic disease, carcinomas and adenocarcinomas; proliferative disorders; and inflammatory disorders. The compounds are therefore useful as neuroprotective and neurogenerative, anti-proliferative, and anti-inflammatory agents.

7H-8,9-dihydro-pyrano (2,3-C) imidazo (1,2a) pyridine derivatives and their use as gastric acid secretio inhibitors

TRICYCLIC CARBAPENEM COMPOUNDS

PURIFICATION OF BENZOPHENANTHRIDINE ALKALOIDS FROM ALKALOID EXTRACTS

POLYCYCLIC COMPOUNDS AS POTENT ALPHA2-ADRENOCEPTOR ANTAGONISTS

Azepino(4,5-b)pyrano(3,2-e)indoles

Polycyclic-Carbamoylpyridone compounds and their pharmaceutical use

Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): (Ia) including stereoisomers and pharmaceutically acceptable salts thereof, wherein A, A', R and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family

Condensed 2,3-benzodiazepine derivatives and their use as ampa-receptor inhibitors

4-AMINOPYRIDINE DERIVATIVES

Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family

PYRAZOPYRIDINE COMPOUNDS

PYRIOD 3,4-C ,PSORALENS

New substituted 7,12-dioxabenz(a)anthracene compounds, process for preparing them and pharmaceutical compositions containing them

IMIDAZOLIDINONES, AND IMIDAZOLIDINE-THIONES, PROCESS AND INTERMEDIATES FOR THE PREPARATION THEREOF, AND USE OF SAID COMPOUNDS AS HERBICIDAL AGENTS

TRICYCLIC EPOXIDES

The invention relates to compounds of Formula (1), in which the substituents and symbols have the meanings indicated in the description. The compounds are valuable intermediates for the preparation of pharmaceutical active compounds.

PYRANO-PYRAZOLE DERIVATIVES

NEW DIHYDROFURO-[3,4-B]QUINOLEIN-1-ONES DERIVATIVES, THE PROCEDURE FOR PREPARING THEM AND THE PHARMACEUTICAL COMPOSITIONS THAT CONTAIN THEM

L'invention concerne de nouveaux composés répondant à la formule (I): (voir formule I) dans laquelle: (voir formule II) représente une liaison simple ou double; R0 représente un atome d'hydrogène ou un groupement hydroxy ou alkoxy; R1 et R2, identiques ou différents, représentent un atome d'hydrogène ou d'halogène, un groupement alkyle, alkoxy, hydroxy, polyhalogénoalkyle, nitro, ou amino, ou un groupement de formule (voir formule III) dans laquelle m représente un entier tel que 1 ~ m ~ 4, ou bien R1 et R2 forment ensemble avec les atomes de carbone qui les portent un groupement mono- ou bicyclique de 5 à 12 chaînons; R3 représente un atome d'hydrogène ou un groupement aryle, hétéroaryle, cycloalkyle, alkyle, ou un groupement de formule COR7 dans laquelle R7 représente un groupement aryle, alkyle, ou amino, ou un groupement de formule OR10 dans laquelle R10 représente un atome d'hydrogène ou un groupement aryle ou alkyle; X représente un atome d'oxygène, de soufre ou un groupement -CH2 ...

2,4,6-PHENYL SUBSTITUTED CYCLIC KETOENOLS

The present invention relates to novel 2,4,6-phenyl-substituted cyclic ketoenols of the formula (I) (see formula I) in which W, X, Y and CKE have the abovementioned meanings, to a plurality of processes for their preparation and to their use as pesticides and/or herbicides. Moreover, the invention relates to selectively herbicidal compositions containing firstly 2,4,6-phenyl-substituted cyclic ketoenols and secondly a compound which improves crop plant tolerance.

INDOLE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF MALIGNANT AND OTHER DISEASES BASED ON PATHOLOGICAL CELL PROLIFERATION

The invention relates to tyrosine kinase in-hibitors of bis-indolyl compounds of formula (I), to the medicaments containing said inhibitors and to their use in treating malignant and other diseases caused by pathological cell proliferation.

CONDENSED PYRADIZINDIONE DERIVATIVES AS PDE INHIBITORS

The present invention provides compounds of general structural formula (I) and use of the compounds, salts, and solvate thereof, as PDE inhibitors.

HETEROCYCLIC TETRACYCLIC TETRAHYDROFURAN DERIVATIVES AS 5HT2 INHIBITORS IN THE TREATMENT OF CNS DISORDERS

... ²²²This invention concerns novel substituted heterocyclic tetracyclic ²tetrahydrofuran derivat ives with binding affinities towards serotonin ²receptors, in particular 5-HT2A and 5- HT2C receptors, and towards dopamine ²receptors, in particular dopamine D2 receptors and with norepinephrine ²reuptake inhibition properties, pharmaceutical compositions comprising the ²compounds according to the invention, the use thereof as a medicine, in ²particular for the prevention and/or treatment of a range of psychiatric and ²neurological disorders, in particular certain psychotic, cardiovascular and ²gastrokinetic disorders and processes for their production. The compounds ²according to the invention can be represented by general Formula (I) , and ²comprises also the pharmaceutically acceptable acid or base addition salts ²thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof ²and prodrugs thereof, wherein all substituents are defined as in Claim 1.² ...

A REGIOSELECTIVE METAL CATALYZED SYNTHESIS OF ANNELATED BENZIMIDAZOLES AND AZABENZIMIDAZOLES

A regioselective metal catalyzed synthesis of benzimidazoles and azabenzimidazoles The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N--substituted benzimidazoles or azabenzimidazoles of formula (I) starting from 2-halo- nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, ...

SUBSTITUTED 1,8-NAPHTHYRIDINONES, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Substituted 1,8-naphthyridinones of formulae V, VI or VII VI V VII wherein n is 1 or 2; R1 and R2 may be combined to form a bond, or R1 is hydrogen and R2 is OR, halogen or NR3R4; R is hydrogen, carboxylic acyl or carbamyl; R3 and R4 are independently hydrogen or alkyl having from 1 to 6 carbon atoms, or R3 and R4 may be combined with the nitrogen to which they are attached to form a pyrrolidino, piperidino, morpholino or piperazino ring; R5 is hydrogen or carboxylic acyl; and Y is CH or N. The compounds possess anti-allergic, antiinflammatory and cytoprotective activity.

IMIDAZOLIDINONES, AND IMIDAZOLIDINE-THIONES, PROCESS AND INTERMEDIATES FOR THE PREPARATION THEREOF, AND USE OF SAID COMPOUNDS AS HERBICIDAL AGENTS

IMIDAZOLIDINONES, AND IMIDAZOLIDINETHIONES, PROCESS AND INTERMEDIATES FOR THE PREPARATION THEREOF, AND USE OF SAID COMPOUNDS AS HERBICIDAL AGENTS This invention relates to novel imidazolidinone and imidazolidinethione compounds, a process and intermediates for the preparation of said compounds and a method for controlling undesirable plant species therewith.

PYRIMIDOQUINOXALINE DERIVATIVES, PROCESS FOR PRODUCING THE SAME, AND MEDICINE COMPRISING THE SAME FOR ALLERGIC ASTHMA

Substituted pyrimido¢5,6-b!quinoxaline-4(3H)-one-2-carboxylic acid compounds represented by the formula (I) wherein: R designates a member selected from the group consisting of hydrogen, alkyl groups having 1 to 4 carbon atoms, benzyl group, and phenyl group; and each of R1, R2, R3 and R4 independently designates a member selected from the group consisting of hydrogen, alkyl group having 1 to 4 carbon atoms, alkoxy groups having 1 to 4 carbon atoms, halogens, benzyloxy group, hydroxyl group, alkyl-thio groups having 1 to 4 carbon atoms, and alkylenedioxy groups having 1 to 4 carbon atoms and formed by the bonding of two of R1, R2, R3 and R4, or pharmacologically acceptable salts of said compounds. The compounds of the invention are suitable for oral administration in the treatment of allergic asthma.

Lactam compounds useful as protein kinase inhibitors

The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Pyrimidine derivatives and analogs, preparation method and use thereof

This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X 1 , X 2 , X 3 , X 4 are, independently at each occurrence, C, O, S, Se, N and P elements; R 1 , R 2 , R 3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.

Fluorescent dyes

Provided are various compounds comprising the formula Also provided are fluorescent dyes comprising the above compound. Additionally, a fluorescence energy transfer system is provided that comprises the above-described fluorescent dye and a second dye, wherein the second dye is capable of energy transfer with the fluorescent dye. Further provided is a kit for labeling a target molecule, where the kit comprises the above-described fluorescent dye with additional reagents useful for labeling the target molecule. Additionally provided is a target molecule labeled with the above-described fluorescent dye. A method of labeling a target molecule is also provided. The method comprises contacting reactive group Z of the above-described fluorescent dye with the target molecule such that reactive group Z reacts with the target molecule to form a covalent bond between reactive group Z and the target molecule. Also, another method of labeling a target molecule is provided. The method comprises contacting the above-described fluorescent dye, which further comprises a member of a binding pair, with the target molecule, where the target molecule comprises a second member of the binding pair.

LONG WAVELENGTH FLUOROGENIC INTRACELLULAR ION INDICATORS THAT ARE WELL RETAINED IN THE CYTOSOL

Cell permeable metal ion indicator compounds and methods of their use and synthesis are described. The compound comprises a metal chelating moiety (M), a reporter molecule and two or more lipophilic groups (G) covalently bonded through a linker to the reporter molecule, wherein the lipophilic groups, when present in a live cell, are cleaved resulting in two or more negatively charged groups. 1. An intracellular ion indicator compound , wherein the compound comprises a metal chelating moiety (M) , a reporter molecule and two or more lipophilic groups (G) covalently bonded through a linker to the reporter molecule , wherein the lipophilic groups , when present in a live cell , are cleaved resulting in two or more negatively charged groups.245-. (canceled) The present invention provides intracellular ion indicator compounds capable of chelating and detecting metal ions in cells. The compounds generally comprise a metal chelating moiety (M), a reporter molecule and one or more lipophilic groups (G) covalently bonded to the reporter molecule, wherein the lipophilic groups, when present in a live cell, are cleaved resulting in one or more negatively charged groups.Metal ions such as calcium are involved in many cellular processes including signal transduction. Small variances in intracellular ion levels can have a major impact on cellular processes. Measurement of ion levels provides a very sensitive method for identifying various cellular activities.Several fluorescent calcium indicators known in art are employed in biological research and high throughput screening. Generally, long wavelength indicators, such as rhodamine-based compounds bear a positive charge. Positively charged molecules compartmentalize in cell mitochondria. Because calcium ion release in activated cells happens in the cytosol, positively charged indicators show a weak response to calcium ion influx. Alternatively, fluorescein-based indicators have also been described that avoid accumulation in the ...

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.

4-AZA-2, 3-DIDEHYDROPODOPHYLLOTOXIN COMPOUNDS AND PROCESS FOR THE PREPARATION THEREOF

The present invention provides 4-Aza-2,3-didehydropodophyllotoxin compound of general formula A (4a-4z and 4aa-4ae) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4-Aza-2,3-didehydropodophyllotoxin compounds (4a-4z and 4aa-4ae). 2. The compound as claimed in claim 1 , are selected from;2,4-dimethoxy-5-(3,4,5-trimethoxyphenyl)-5,6,8,9-tetrahydrofuro[3′,4′:5,6]pyrido[2,3-d]pyrimidin-6-one (4a);5-(4-hydroxy-3-methoxyphenyl)-2,4-dimethoxy-5,6,8,9-tetrahydrofuro[3′,4′:5,6]pyrido[2,3-d]pyrimidin-6-one (4b);5-(3-hydroxy-4-methoxyphenyl)-2,4-dimethoxy-5,6,8,9-tetrahydrofuro[3′,4′:5,6]pyrido[2,3-d]pyrimidin-6-one (4e);5-(4-fluoro-3-methoxyphenyl)-2,4-dimethoxy-5,6,8,9-tetrahydrofuro[3′,4′:5,6]pyrido[2,3-d]pyrimidin-6-one (4d);3-(4-methoxyphenyl)-4-(3,4,5-trimethoxyphenyl)-4,5,7,8 tetrahydrofuro[3′,4′:5,6]pyrido[3,2-d]isoxazol-5-one (4aa);4-(3-hydroxy-4-methoxyphenyl)-3-(4-methoxyphenyl)-4,5,7,8-tetrahydrofuro[3′,4′:5,6]pyrido[3,2-d]isoxazol-5-one (4ab);3-(4-chlorophenyl)-4-(3,4,5-trimethoxyphenyl)-4,5,7,8-tetrahydrofuro[3′,4′:5,6]pyrido[3,2-d]isoxazol-5-one (4ae);3-(4-chlorophenyl)-4-(3-hydroxy-4-methoxyphenyl)-4,5,7,8-tetrahydrofuro[3′,4′:5,6]pyrido[3,2-d]isoxazol-5-one (4ad),4. The compound as claimed in claim 1 , wherein said compounds exhibit in vitro anticancer activity against human cancer cell lines selected from the group consisting of colon (Colo205) claim 1 , lung (Hop-62 claim 1 , A549) claim 1 , cervix (SiHa) claim 1 , prostate (PC3) claim 1 , oral (KB claim 1 , DWD claim 1 , Gurav) claim 1 , Ovarian (A-2780) and breast (MCF7 claim 1 , Zr-75-1).5. The compounds as claimed in claim 2 , wherein the concentration of the compound used for in vitro activity against breast cancer cell lines for GIis in the range of 0.1 to 2.9 μm at an exposure period of at least 48 hrs.6. The compounds as claimed in claim 2 , wherein the concentration of the compound used for in vitro activity ...

NICOTINIC ACETYLCHOLINE RECEPTOR AGONISTS

The invention provides novel nicotinic acetylcholine receptor agonists, for example, phantasmidine and derivatives thereof, for example a compound of formula (I). Also disclosed are methods of treating disorders responsive to nicotinic acetylcholine receptor agonists such as Alzheimer's disease, schizophrenia, Myasthenia Gravis, Tourette's syndrome, Parkinson's disease, epilepsy, pain, and cognitive dysfunction by treatment with the nicotinic acetylcholine for agonists. 1. Phantasmidine , or phantasmidine in isolated or purified form , an enantiomer thereof , stereoisomer thereof , racemic mixtures thereof , or a pharmaceutically acceptable salt thereof.3. The compound claim 2 , enantiomer thereof claim 2 , stereoisomer thereof claim 2 , racemic mixtures thereof claim 2 , or salt of claim 2 , wherein the compound has Formula I.4. The compound claim 3 , enantiomer thereof claim 3 , stereoisomer thereof claim 3 , racemic mixtures thereof claim 3 , or salt of claim 3 , wherein m is 1 claim 3 , n is 0 claim 3 , p is 2 claim 3 , W is a bond claim 3 , and Z is 0.5. The compound claim 4 , enantiomer thereof claim 4 , stereoisomer thereof claim 4 , racemic mixtures thereof claim 4 , or salt of claim 4 , wherein Ris selected from the group consisting of hydrogen claim 4 , C-Calkyl claim 4 , C-Calkenyl claim 4 , C-Calkynyl claim 4 , C-Ccycloalkyl claim 4 , C-Ccycloalkenyl claim 4 , C-Carylalkyl claim 4 , C-Caryl claim 4 , heterocyclyl claim 4 , heteroaryl claim 4 , and RCO.6. The compound claim 4 , enantiomer thereof claim 4 , stereoisomer thereof claim 4 , racemic mixtures thereof claim 4 , or salt of claim 4 , wherein Ris selected from the group consisting of hydrogen claim 4 , C-Calkyl claim 4 , C-Calkenyl claim 4 , C-Calkynyl claim 4 , and RCO.7. The compound claim 6 , enantiomer thereof claim 6 , stereoisomer thereof claim 6 , racemic mixtures thereof claim 6 , or salt of claim 6 , wherein Ris hydrogen or C-Calkyl.8. The compound claim 7 , enantiomer thereof claim 7 , ...

IAP BINDING COMPOUNDS

IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kof less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed. 5. The compound of or a pharmaceutically acceptable salt thereof where Ais H claim 1 , methyl claim 1 , or ethyl and where Ris H; Ris methyl or ethyl.6. The compound of or a pharmaceutically acceptable salt thereof where Y is an alkyl group of 1 to 10 carbon atoms claim 1 , a branched alkyl group of 1 to 10 carbon atoms claim 1 , an alkynyl group claim 1 , a cycloalkyl group of 3 to 7 carbon atoms claim 1 , or optionally substituted versions of these groups.7. The compound of or a pharmaceutically acceptable salt thereof where Zand Zare independently an H claim 1 , hydroxy claim 1 , amino claim 1 , alkylamino claim 1 , dialkylamino claim 1 , alkoxy claim 1 , aryloxy claim 1 , or heteroaryloxy.8. The compound of or a pharmaceutically acceptable salt thereof where M is an alkyl or an alkylene of 1 to 5 carbon atoms.13. A method of treating cancerous cells comprising administering to the cells an IAP binding compound of .14. A method of treating cells comprising:{'claim-ref': {'@idref': 'CLM-00011', 'claim 11'}, 'administering to cells that have a proliferation disorder, wherein the disorder is selected from the group consisting of a cancer or an autoimmune disorder, an amount of the IAP binding compound of or a pharmaceutically acceptable salt thereof that reduces the cellular proliferation disorder in the sample of cells.'}15. A method of treating cells comprising:{'claim-ref': {'@idref': 'CLM-00012', 'claim 12'}, 'administering to cells that have a proliferation disorder, wherein the disorder is selected from the group consisting of a cancer or an autoimmune ...

Inhibitors of Hepatitis C Virus

A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV. 2. The compound of claim 1 , having an inhibitory activity with respect to HCV claim 1 , as measured by the concentration of the compound effective to produce a half-maximal inhibition of HCV1b replication (EC) in a 1b_Huh-Luc/Neo-ET cell line in culture claim 1 , of 1 mM or less.7. The compound of claim 6 , selected from the group consisting of compounds identified by ID NOS: B89 claim 6 , B96 claim 6 , B97 claim 6 , B125 claim 6 , B126 claim 6 , and B129.9. The compound of claim 5 , wherein Ris phenyl substituted with one or more Rsubstituents.10. The compound of claim 5 , where Ris 4-phenoxyphenyl and the phenoxy group is substituted with one or more Rsubstituents.15. The compound of claim 14 , having an inhibitory activity with respect to HCV claim 14 , as measured by the concentration of the compound effective to produce a half-maximal inhibition of HCV1b replication (EC) in a 1b_Huh-Luc/Neo-ET cell line in culture claim 14 , of 100 nM or less.17. The compound of claim 16 , selected from the group consisting of compounds identified by ID NOS: B5 claim 16 , B15 claim 16 , B20 claim 16 , B33 claim 16 , B35 claim 16 , B45 claim 16 , B67 claim 16 , B85 claim 16 , B92 claim 16 , B94 claim 16 , B107 claim 16 , B118 claim 16 , B120 claim 16 , B121 claim 16 , B127 claim 16 , B128 claim 16 , B130 claim 16 , B131 claim 16 , B132 claim 16 , B138 claim 16 , B139 claim 16 , B145 claim 16 , B148 claim 16 , B158 claim 16 , B163 claim 16 , B168 claim 16 , B169 claim 16 , B171 claim 16 , B187 claim 16 , B190 claim 16 , B191 claim 16 , B192 claim 16 , B196 claim 16 , B197 claim 16 , B198 claim 16 , B201 claim 16 , B207 claim 16 , B208 claim 16 , B212 claim 16 , B214 claim 16 , B218 claim 16 , B221 claim 16 , B226 claim 16 , B232 claim 16 , B233 claim 16 , B236 claim 16 , B237 ...

CARBOXY X RHODAMINE ANALOGS

The present invention provides novel fluorescent dyes and kits containing the same, which are useful for labeling a wide variety of biomolecules, cells and microorganisms. The present invention also provides various methods of using the fluorescent dyes for research and development, forensic identification, environmental studies, diagnosis, prognosis and/or treatment of disease conditions. 24.-. (canceled)5. A compound according to wherein at least one of R claim 8 , Ror Ris H.67.-. (canceled)9. A compound according to wherein X is CH.1011.-. (canceled)12. A compound according to wherein Rand Rform a 5-7 membered carbocyclic ring.1315.-. (canceled)16. A compound according to wherein Ris H claim 8 , Cl or OMe.17. A compound according to wherein Rand Rform a 5-7 membered carbocyclic ring.18. (canceled)19. A compound according to wherein at least one of R claim 8 , R claim 8 , Rand Ris H.2024.-. (canceled)25. A compound according to wherein Ris H claim 8 , Cl or OMe.26. A compound according to wherein Ris Calkyl.27. A compound according to wherein Ris methyl or ethyl.28227. A compound according to any one of claims - wherein Ris Calkyl.29. A compound according to wherein Ris methyl or ethyl.30. A compound according to wherein Ris part of a heterocycle.31. (canceled)32. A compound according to wherein Ris part of a heterocycle.3344.-. (canceled)45. A compound according to wherein Ris H.46. A compound according to wherein Ris H.47. A compound according to wherein Ris H or halogen.48. A compound according to wherein Ris H or halogen.49. A compound according to wherein Ris H claim 8 , F claim 8 , Cl COH or SOH.50. A compound according to wherein one of Rand Ris -L-R claim 8 , -L-COH or -L-Cand the other is H claim 8 , Cl claim 8 , or F.51. A compound according to wherein L is —CO— claim 8 , —SCHCO— claim 8 , or —SO—.52. A compound according to is a self-immolative linker.54. A compound according to wherein Cis NHCHCH(OCHCH)(CH)Cl claim 8 , wherein n is 2-6.55. A compound ...

SUBSTITUTED HETEROCYCLIC COMPOUNDS

The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): 2. The compound of claim 1 , wherein R4 is optionally substituted cycloalkyl claim 1 , optionally substituted heterocyclyl claim 1 , optionally substituted aryl claim 1 , or optionally substituted heteroaryl.3. The compound of claim 1 , wherein R4 is aryl substituted with one or more groups selected from aryl claim 1 , lower alkyl claim 1 , heteroaryl claim 1 , halo claim 1 , heterocyclyl claim 1 , amino claim 1 , and carboxyl claim 1 , wherein said one or more groups are optionally substituted with alkyl claim 1 , aryl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , halo claim 1 , or carboxyl.4. The compound of claim 1 , wherein R5 is —NR52R53 claim 1 , where R52 and R53 are each independently selected from hydrogen claim 1 , lower alkyl claim 1 , optionally substituted cycloalkyl claim 1 , optionally substituted aryl claim 1 , or optionally substituted benzyl; or where R52 and R53 taken together with the nitrogen to which they are both directly attached form a 5 or 6 membered heterocyclyl or heteroaryl moiety claim 1 , said 5 or 6 membered heterocyclyl or heteroaryl moiety optionally substituted by a group selected from halo claim 1 , alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , alkoxy claim 1 , aryl claim 1 , and cycloalkyl and combinations thereof claim 1 , wherein said alkyl claim 1 , alkenyl claim 1 , alkynyl claim 1 , alkoxy claim 1 , aryl claim 1 , or cycloalkyl is each optionally substituted.5. The compound of claim 1 , wherein R5 and R6 taken together with the carbons to which R5 and R6 are directly attached and the carbon directly attached to both of the carbons to which R5 and R6 are directly attached form a 5 or 6 membered heterocyclyl claim 1 , heteroaryl claim 1 , cycloalkyl claim 1 , or a ...

THERAPEUTIC THIOPHENE-, FURAN-, AND PYRIDINE-FUSED AZOLOPYRIMIDIN-5-(6H)-ONES

Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. 2. The compound of claim 1 , wherein M=1.3. The compound of claim 1 , wherein M=2.4. The compound of claim 1 , wherein one or more of R claim 1 , R claim 1 , R claim 1 , and Ris halomethyl.5. The compound of claim 1 , wherein{'sup': 1', '2, 'sub': 1', '6', '3, 'Ris H, and Ris C-Calkoxy, more specifically —OCH.'}6. The compound of claim 1 , whereinA is sulfur, and X is N.7. The compound of claim 1 , wherein{'sup': 1', '2, 'sub': 1', '6', '3', '2, 'Ris halo, more specifically F, Cl, or Br, and Ris C-Calkoxy, more specifically, —CFor —CHF.'}8. The compound of claim 1 , wherein{'sup': 3', '4, 'sub': 1', '6, 'Ris C-Calkyl, more specifically methyl, and Ris H; or'}{'sup': 3', '4', '10', '11', '12', '13, 'sub': 1', '6', '1', '3', '0-3, 'Ris C-Calkyl, more specifically C-Calkyl, and Ris —(CRR)NRR; or'}{'sup': 3', '4, 'Rand Rtaken together with the carbons to which they are attached form a six member monocyclic ring system, wherein D is a nitrogen atom.'}9. The compound ofor a pharmaceutically acceptable salt thereof, wherein{'sup': 1', '2, 'sub': 1', '3', '1', '3', '1', '3', '2', '2', '1', '3', '2', '1', '3', '2', '1', '3', '1', '3', '2, 'each occurrence of Rand Ris independently selected from —H, halo, —CN, —C-Calkyl, —C-Chaloalkyl, —OH, —C-Chaloalkoxy, —NO, —SOC-Calkyl, —SON(C-Calkyl), —CONH(C-Calkyl), and —CON(C-Calkyl);'}{'sup': 1', '2, 'or Rand Rare on adjacent carbons and taken together with the carbons to which they are attached form a 5-6 member monocylic ring system comprising one or more oxygen atoms, wherein the ring system is optionally substituted with one or more F;'}{'sup': 3', '4', '10', '11', '12', '13, 'sub': 1', '3', '1', '6', '3', '2', '1', '3', '3', '2', '2', '1', '3', '2 ...

INHIBITORS OF SERINE PROTEASES, PARTICULARLY HCV NS3-NS4A PROTEASE

The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. 1. (canceled)3. (canceled)5. The compound according to claim 4 , wherein V is —NH—.6. The compound according to claim 4 , wherein V is —C(O)—.7. The compound according to claim 4 , wherein T is a —(C5-C10)heteroaryl.9. The compound according to claim 4 , wherein T contains at least one hydrogen bond donor moiety selected from —NH claim 4 , —NH— claim 4 , —OH claim 4 , and —SH.15. The compound according to claim 14 , wherein Ris —CH—C(CH) claim 14 , —C(CH) claim 14 , —CH(CH) claim 14 , —CH(CH)—CH—CH claim 14 , or cyclohexyl.16. The compound according to claim 15 , wherein Ris cyclohexyl.18. The compound according to claim 17 , wherein Ris —C(CH) claim 17 , —CH(CH) claim 17 , —CH(CH)—CH—CH claim 17 , or cyclohexyl.19. The compound according to claim 18 , wherein Ris —C(CH)or —CH(CH).21. The compound according to claim 20 , wherein Ris —CHCHCH claim 20 , —CHCHCHCH claim 20 , —CHCHCHF claim 20 , —CHCHCHF claim 20 , or —CHCHCF.22. The compound according to claim 21 , wherein Ris —CHCHCHCHor —CHCHCHF.23. The compound according to claim 22 , wherein Ris —CHCHCHCH.24. The compound according to claim 4 , wherein Rand Rare each independently H claim 4 , methyl claim 4 , ethyl claim 4 , or propyl.25. The compound according to claim 4 , wherein W is C(O)—C(O)—NH(R).26. The compound according to claim 25 , wherein in the W claim 25 , the —NH(R) is —NH—(C-Ccycloalkyl) claim 25 , —NH—CH(CH)-aryl ...

TRI - AND TETRACYCLIC PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS AS ANTINEOPLASTIC AGENT

The present invention relates to compounds of following general formula (I): and to the pharmaceutically acceptable salts of same, the tautomers of same, the stereoisomers or mixture of stereoisomers in any proportions of same, such as a mixture of enantiomers, notably a racemic mixture, as well as to methods for preparing same and uses of same, notably as an antineoplastic agent. 119.-. (canceled)22. The compound according to claim 20 , wherein Rand Rtogether form claim 20 , with the carbon atoms that carry them claim 20 , a ring selected from an aryl claim 20 , a heteroaryl claim 20 , a carbocycle and a heterocycle claim 20 ,{'sub': 2', '26', '27', '28', '29', 'N', '2', '31', '2', '32', '33', '34', '35', '36', '37', '2', '38', '2', '39', '40', '2', '41', '42', '1', '6', '1', '6', '43', '44', '45', '1', '6', '1', '6, 'said ring being optionally substituted by one or more groups selected from a halogen atom, a CN, NO, OR, SR, NRR, COR, COR, OCOR, CONRR, NRCOR, NRSOR, SONRR, SOR, SOR, (C-C)alkyl, aryl, heteroaryl, carbocycle and heterocycle group, the (C-C)alkyl chains as well as the rings of the whole being optionally substituted by one or more groups selected from OR, NRR, —C(O)O—(C-C)-alkyl, heterocycle and (C-C)-alkyl.'}23. The compound according to claim 20 , wherein Rand Reach represent claim 20 , independently of each other claim 20 , a hydrogen atom claim 20 , a halogen atom claim 20 , or a (C-C)alkenyl claim 20 , (C-C)alkynyl claim 20 , aralkyl claim 20 , (C-C)alkyl claim 20 , aryl claim 20 , heteroaryl claim 20 , carbocycle or heterocycle group claim 20 , the (C-C)alkenyl and (C-C)alkynyl chains as well as the aromatic or non-aromatic rings of the whole being optionally substituted by one or more groups selected from a halogen atom claim 20 , a CN claim 20 , NO claim 20 , OR claim 20 , SR claim 20 , NRR claim 20 , COR claim 20 , COR claim 20 , OCOR claim 20 , CONRR claim 20 , NRCOR claim 20 , NRSOR claim 20 , SONRR claim 20 , SOR claim 20 , SOR claim 20 , ( ...

Protein kinase d inhibitors

Compounds according to Formula (I), are potent inhibitors of protein kinase D (pan-PKD) activity. PKD controls key signaling cascades in cells, affecting cell proliferation, gene transcription, and protein trafficking. Accordingly, pharmaceutically acceptable compositions of the inventive compounds are candidate therapeutics for pathological conditions conditioned by changes in PKD activity.

Protein Kinase Inhibitors

The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families. 8. The compound according to claim 7 , wherein the compound is selected from the group consisting of compounds 1 claim 7 , 20 claim 7 , 21 claim 7 , 23 claim 7 , 24 claim 7 , 28 claim 7 , 29 claim 7 , 31 claim 7 , 32 claim 7 , 33 claim 7 , 34 claim 7 , 35 claim 7 , 37 claim 7 , 39 claim 7 , 40 claim 7 , and 45.9. The compound according to claim 7 , wherein the compound is selected from the group consisting of compounds 25 claim 7 , 41 claim 7 , 43 claim 7 , 44 claim 7 , 46 claim 7 , 49 claim 7 , 50 claim 7 , 53 claim 7 , 54 claim 7 , 56 claim 7 , 57 claim 7 , 58 claim 7 , 59 claim 7 , 61 claim 7 , 62 claim 7 , 64 claim 7 , 67 claim 7 , 68 claim 7 , 75 claim 7 , 77 claim 7 , 78 claim 7 , 85 claim 7 , 86 claim 7 , 87 claim 7 , 89 claim 7 , 93 claim 7 , 94 claim 7 , 95 claim 7 , 96 claim 7 , 97 claim 7 , 99 claim 7 , 100 claim 7 , 102 claim 7 , 103 claim 7 , 104 claim 7 , 105 claim 7 , 106 claim 7 , 107 claim 7 , 108 claim 7 , 109 claim 7 , 115 claim 7 , 112 claim 7 , 123 claim 7 , 124 claim 7 , 128 claim 7 , 129 claim 7 , 130 claim 7 , 131 claim 7 , 132 claim 7 , 133 claim 7 , 134 claim 7 , 135 claim 7 , 136 claim 7 , 137 claim 7 , 138 claim 7 , 140 claim 7 , 141 claim 7 , 142 claim 7 , 143 claim 7 , and 144.10. The compound according to claim 7 , wherein the compound is selected from the group consisting of compounds 47 claim 7 , 66 claim 7 , 69 claim 7 , 70 claim 7 , 76 claim 7 , 80 claim 7 , 81 claim 7 , 82 claim 7 , 84 claim 7 , 111 claim 7 , 112 claim 7 , 114 claim 7 , 118 claim 7 , 119 claim 7 , 120 claim 7 , 121 claim 7 , 125 claim 7 , 126 claim 7 , and 127.11. A pharmaceutical composition comprising a compound of and a ...

Compounds and methods for inhibiting mitotic progression

This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.

HEXAHYDRODIBENZO[A,G]QUINOLIZINE COMPOUND, PREPARATION METHOD THEREOF, PHARMACEUTICAL COMPOSITION AND USE THEREOF

The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on. 2. The hexahydrodibenzo[a claim 1 ,g]quinoline compound claim 1 , the enantiomer claim 1 , diastereoisomer claim 1 , racemate claim 1 , pharmaceutically acceptable organic salt or inorganic salt claim 1 , crystalline hydrate or solvate thereof claim 1 , or mixture thereof according to claim 1 ,{'sub': 1', '2', '3', '4', '5', '6', '7', '8, 'wherein Ris H, a halogen-substituted or unsubstituted C1-C6 alkyl, a halogen-substituted or unsubstituted C1-C6 alkoxy, a hydroxy, a hydroxy-substituted C1-C6 alkyl or a halogen-substituted or unsubstituted benzyloxy; Ris a hydroxy, a hydroxy-substituted C1-C6 alkyl, a halogen substituted or unsubstituted C1-C6 alkyl, a halogen substituted or unsubstituted C1-C6 alkoxy, or a halogen; Ris H, or a halogen substituted or unsubstituted C1-C6 alkyl; Ris H, a halogen substituted or unsubstituted C1-C6 alkyl, or a halogen substituted or unsubstituted C1-C6 alkoxy; Ris H, a halogen substituted or unsubstituted C1-C6 alkyl, a halogen substituted or unsubstituted C1-C6 alkoxy or a halogen; Ris H, a halogen-substituted or unsubstituted C1-C6 alkyl, a halogen-substituted or unsubstituted C1-C6 alkoxy, a hydroxy, or a hydroxy-substituted C1-C6 alkyl; Ris H, a ...

FGFR4 INHIBITOR AND USE THEREOF

Disclosed is a compound as a fibroblast growth factor receptor 4 (FGFR4) inhibitor (as shown in formula (I)), and a pharmaceutical composition thereof and a preparation method therefor, as well as the use of same in the treatment of FGFR4-mediated diseases. The above-mentioned compounds act by participating in a number of processes, such as regulating cell proliferation, apoptosis, migration, neovascularization. 2. The compound or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , chelate claim 1 , non-covalent complex claim 1 , or prodrug thereof of claim 1 , wherein L claim 1 , Q and T is selected from the following groups:{'sub': '2', '(i) L is C, Q is N, T is CH;'}(ii) L is C, Q is N, T is C;(iii) L is C, Q is C, T is N;(iv) L is C, Q is N, T is CH;{'sub': '2', '(v) L is N, Q is N, T is CH; or'}(vi) L is C, Q is CH, T is O.4. The compound or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , chelate claim 1 , non-covalent complex claim 1 , or prodrug thereof of claim 1 , wherein ring A is phenyl claim 1 , Cheteroaryl or Cheterocyclyl claim 1 , wherein the Cheteroaryl optionally containing 1 claim 1 , 2 or 3 heteroatoms selected from N and S claim 1 , the Cheterocyclyl is a fused bicyclic which has two N atoms and one O atom in the ring.5. The compound or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , chelate claim 1 , non-covalent complex claim 1 , or prodrug thereof of claim 1 , wherein ring A is Cheteroaryl.6. The compound or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , chelate claim 1 , non-covalent complex claim 1 , or prodrug thereof of claim 1 , wherein Ris selected from the group consisting of H claim 1 , halogen claim 1 , cyano claim 1 , Calkyl claim 1 , halogen substituted Calkyl claim 1 , —(CH)NRRsubstituted amino claim 1 , Calkoxy which substituted with substituted Cheterocyclyl claim 1 , wherein Rand Rare each optionally selected from Calkyl.8. The compound or a pharmaceutically acceptable ...

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

A condensed cyclic compound represented by Formula 1: 2. The condensed cyclic compound of claim 1 , wherein{'sub': 11', '12, 'Rand Rare each independently selected froma phenyl group, a biphenyl group, a terphenyl group, a naphthyl group, a phenanthrenyl group, an anthracenyl group, a triphenylenyl group, a pyrenyl group, and a chrysenyl group; and{'sub': 1', '20', '1', '20, 'a phenyl group, a biphenyl group, a terphenyl group, a naphthyl group, a phenanthrenyl group, an anthracenyl group, a triphenylenyl group, a pyrenyl group, and a chrysenyl group, each substituted with at least one selected from deuterium, —F, —Cl, —Br, —I, a cyano group, a C-Calkyl group, a C-Calkoxy group, and a phenyl group.'}3. The condensed cyclic compound of claim 1 , wherein{'sub': '12', 'and Rare each independently selected froma phenyl group, a biphenyl group, a terphenyl group, and a naphthyl group; anda phenyl group, a biphenyl group, a terphenyl group, and a naphthyl group, each substituted with at least one selected from deuterium, a methyl group, an ethyl group, an n-propyl group, an isopropyl group, an n-butyl group, an iso-butyl group, a sec-butyl group, a tert-butyl group, an n-pentyl group, an iso-pentyl group, a sec-pentyl group, a tert-pentyl group, an n-hexyl group, an iso-hexyl group, a sec-hexyl group, a tert-hexyl group, a methoxy group, an ethoxy group, a propoxy group, a butoxy group, a pentoxy group, and a phenyl group.4. The condensed cyclic compound of claim 1 , wherein{'sub': '21', 'Ais a benzene group, and'}{'sub': '22', 'Ais selected from a benzene group, a fluorene group, a carbazole group, a dibenzofuran group, a dibenzothiophene group, an indolofluorene group, an indolocarbazole group, an indolodibenzofuran group, an indolodibenzothiophene group, an indenofluorene group, an indenocarbazole group, an indenodibenzofuran group, an indenodibenzothiophene group, a benzofuranofluorene group, a benzofuranocarbazole group, a benzofuranodibenzofuran group, a ...

BENZOPYRYLIUM COMPOUNDS

Compounds used as labels with properties comparable to known fluorescent compounds. The compounds are conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided. 2. The compound of wherein{'sup': 2', '3', '5', '6', '11', '13', '14', '1', '4', '7', '8', '9', '12, 'when the compound is according to general formula Ia or IIa each of Rand Ris independently selected from sulfoalkyl or a PEG group P-L-Z; Ris alkyl; Ris t-butyl or an unsubstituted or substituted phenyl; Ris sulfonic acid, carboxylic acid, or an amino group; each of Rand Ris independently selected from alkyl, sulfoalkyl, or a PEG group P-L-Z; and each of R, R, R, R, R, and Ris H;'}{'sup': 2', '3', '5', '6', '11', '13', '14', '1', '4', '7', '8', '9', '12, 'when the compound is according to general formula Ib or IIb each of Rand Ris independently selected from sulfoalkyl or a PEG croup P-L-Z; Ris alkyl; Ris t-butyl or an unsubstituted or substituted phenyl; Ris sulfonic acid, carboxylic acid, or an amino group; each of Rand Ris independently selected from alkyl, sulfoalkyl, or a PEG group P-L-Z; and each of R, R, R, R, R, and Ris H;'}{'sup': 2', '3', '5', '6', '11', '13', '14', '1', '4', '7', '8', '9', '12, 'when the compound is according to general formula Ic or IIc each of Rand Ris independently selected from sulfoalkyl or a PEG group P-L-Z; Ris alkyl; Ris t-butyl or an unsubstituted or substituted phenyl; Ris sulfonic acid, carboxylic acid, or an amino group; each of Rand Ris independently selected from alkyl, sulfoalkyl, or a PEG group P-L-Z; and each of R, R, R, R, R, and Ris H; and'}{'sup': 2', '3', '5', '6', '11', '13', '14', '1', '4', '7', '8', '9', '12, 'when the compound is according to general formula Id or IId each of Rand Ris independently selected from sulfoalkyl or a PEG group P-L-Z; Ris alkyl; Ris t-butyl or an unsubstituted or substituted phenyl ...

AZOLOBENZAZINE COMPOUNDS, COMPOSITIONS COMPRISING THESE COMPOUNDS AND THEIR USE FOR CONTROLLING INVERTEBRATE PESTS

Azolobenzazine compounds of the formula I and N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof are disclosed, as well as are methods for controlling invertebrate pests using the disclosed compounds. Further disclosed are plant propagation materials, agricultural compositions, and veterinary compositions that include the disclosed compounds. 3. The compound of claim 2 , selected from compounds of the formulae (I) claim 2 , (Ia) claim 2 , (Ib) claim 2 , (Ic) and (Id) claim 2 , wherein{'sup': 4', '5', '6, 'Ais N, while Ais CH and Ais CH; or'}{'sup': 5', '4', '6, 'Ais N, while Ais CH and Ais CH; or'}{'sup': 6', '4', '5, 'Ais N, while Ais CH and Ais CH; or'}{'sup': 4', '5', '6, 'Ais N, Ais N and Ais CH; or'}{'sup': 4', '6', '5, 'Ais N, Ais N and Ais CH; or'}{'sup': 5', '6', '4, 'Ais N, Ais N and Ais CH.'}4. The compound of claim 1 , wherein Q is selected from the group consisting of O claim 1 , S claim 1 , —CH— claim 1 ,{'sup': Q1', 'Q2', 'Q2', 'Q2', 'Q2', 'Q1', 'Q2, 'sub': 2', '2', '2', '2', '2', '2', '2', '2', '2, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '—N(R)—, —CH═CH—, —CHCH—, —N═CH—, O—CH, —S—CH, —S(═O)—CH—, —S(═O)—CH—, —N(R)—C(═O)—, —N(R)—C(═S)—, —N(R)—S(═O)—, and —N(R)—CH—, wherein Rand Rare as defined in .'}5. The compound of claim 1 , wherein Ar is phenyl claim 1 , pyridyl claim 1 , pyrimidinyl or pyridazinyl claim 1 , which are unsubstituted or carry 1 claim 1 , 2 or 3 radicals R.6. The compound of claim 1 , wherein Ris selected from the group consisting of halogen claim 1 , C-C-alkyl claim 1 , C-C-haloalkyl claim 1 , C-C-alkoxy claim 1 , C-C-haloalkoxy and S—R claim 1 , wherein Ris C-C-alkyl or C-C-haloalkyl.7. The compound of claim 1 , wherein Ris a moiety -T-X—Y—Z—R.8. The compound of claim 1 , wherein Ris aryl claim 1 , aryl-C-C-alkyl claim 1 , hetaryl claim 1 , or hetaryl-C-C-alkyl claim 1 , wherein the aryl and hetaryl rings in the last 4 radicals are unsubstituted or carry 1 claim 1 , 2 claim 1 , 3 ...

Compounds for electronic devices

The present invention relates to compounds of formula (I), to processes for producing the compounds, and to electronic devices containing at least one compound of formula (I).

HETEROCYCLIC COMPOUND, MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENTS USING SAME, ORGANIC ELECTROLUMINESCENT ELEMENT USING SAME, AND ELECTRONIC DEVICE

A heterocyclic compound in which three 5-membered rings are fused to a benzene ring and a saturated or unsaturated ring is further fused to each of the 5-membered rings is a novel material, which is useful as a material for organic electroluminescence devices for the production of organic electroluminescence devices and electronic equipment. 2. The heterocyclic compound according to claim 1 , wherein each of Ato Aindependently represents a substituted or unsubstituted 5- claim 1 , 6- or 7-membered ring.4. The heterocyclic compound according to claim 1 , wherein the substituent 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 3 to 50 ring carbon atoms; a substituted or unsubstituted aryl group having 6 to 50 ring carbon atoms; a substituted or unsubstituted aralkyl group having 7 to 51 carbon atoms; an amino group; a mono- or disubstituted 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; a substituted or unsubstituted alkoxy group having 1 to 50 carbon atoms; a substituted or unsubstituted aryloxy group having 6 to 50 ring carbon atoms; a mono- claim 1 , di- claim 1 , or trisubstituted 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 heteroaryl 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 ring carbon atoms; a ...

COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, COMPOSITION FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE

A compound for an organic optoelectronic device, a composition for an organic optoelectronic device including the same, an organic optoelectronic device, and a display device, the compound being represented by Chemical Formula 1: 2. The compound as claimed in claim 1 , wherein Lis a single bond or a substituted or unsubstituted phenylene group.3. The compound as claimed in claim 1 , wherein Rand Rare each independently a substituted or unsubstituted phenyl group or a substituted or unsubstituted biphenyl group.5. The compound as claimed in claim 1 , wherein Aris a substituted or unsubstituted phenyl group claim 1 , a substituted or unsubstituted biphenyl group claim 1 , or a substituted or unsubstituted naphthyl group.10. An organic optoelectronic device claim 1 , comprising:an anode and a cathode facing each other, andat least one organic layer between the anode and the cathode,{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'wherein the at least one organic layer includes the compound for an organic optoelectronic device as claimed in .'}11. The organic optoelectronic device as claimed in claim 10 , wherein:the at least one organic layer includes a light emitting layer, andthe light emitting layer includes the compound for an organic optoelectronic device.12. A display device comprising the organic optoelectronic device as claimed in .13. An organic optoelectronic device claim 10 , comprising:an anode and a cathode facing each other, andat least one organic layer between the anode and the cathode,{'claim-ref': {'@idref': 'CLM-00007', 'claim 7'}, 'wherein the at least one organic layer includes the composition for an organic optoelectronic device as claimed in .'}14. The organic optoelectronic device as claimed in claim 13 , wherein:the at least one organic layer includes a light emitting layer, andthe light emitting layer includes the composition for an organic optoelectronic device.15. A display device comprising the organic optoelectronic device as claimed in ...

SUBSTITUTED HETEROCYCLES AS ANTIVIRAL AGENTS

The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts thereof: 2. A compound of claim 1 , wherein A is optionally substituted 5- to 7-membered unsaturated heterocyclic claim 1 , or optionally substituted 5- to 6-membered heteroaryl.9. A pharmaceutical composition claim 1 , comprising a compound according to and a pharmaceutically acceptable carrier or excipient.10. A method of treating or preventing an HBV infection in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of a compound or a combination of compounds according to .11. The method of claim 10 , further comprising administering to the subject an additional therapeutic agent selected from the group consisting of a HBV polymerase inhibitor claim 10 , interferon claim 10 , viral entry inhibitor claim 10 , viral maturation inhibitor claim 10 , literature-described capsid assembly modulator claim 10 , reverse transcriptase inhibitor claim 10 , TLR-agonist claim 10 , inducer of cellular viral RNA sensor claim 10 , therapeutic vaccine claim 10 , and agents of distinct or unknown mechanism claim 10 , and a combination thereof.12. The method of claim 11 , wherein the compound and the additional therapeutic agent are co-formulated.13. The method of claim 11 , wherein the compound and the additional therapeutic agent are co-administered.14. The method of claim 11 , wherein the additional therapeutic agent is administered at a lower dose or frequency compared to the dose or frequency of the additional therapeutic agent that is required to treat an HBV infection when administered alone.15. The method of claim 11 , wherein the subject is refractory to at least one compound selected from the group consisting of a HBV polymerase inhibitor claim 11 , interferon claim 11 , viral entry inhibitor claim 11 , viral maturation inhibitor claim 11 , distinct capsid assembly modulator claim 11 , inducer of cellular viral RNA sensor ...

HETEROCYCLIC COMPOUNDS

Provided herein are compounds of formula I and compositions containing the compounds. The compounds and compositions are useful in the methods of inhibiting the action of ERK5, a BET family protein or both. In certain embodiments, the compounds and compositions are useful in the prevention, amelioration or treatment of a ERK5-mediated disease, a BET protein-mediated disease or both. 2. The compound of claim 1 , wherein{'sup': 7', '7', '8, 'Y is CRor CRR;'}{'sup': 9', '9', '10', '7', '9', '8', '10, 'Z is CRor CRR; wherein Rand Rtogether with the atoms on which they are substituted form a 3 to 6-membered cycloalkyl, aryl, heterocyclyl or heteroaryl ring; and Rand R, when present, are each independently selected from hydrogen, alkyl and cycloalkyl.'}3. The compound of claim 1 , wherein Ris phenyl claim 1 , pyridinyl claim 1 , cyclohexyl claim 1 , tetrahydropyranyl or pyrazolyl claim 1 , where Ris optionally substituted with 1 or 2 substituents Q.6. The compound of claim 4 , wherein Qis alkoxy.7. The compound of claim 4 , wherein Qis ethoxy.9. The compound of claim 8 , wherein{'sup': '3', 'sub': '0-2', 'X is NR, O or S(O);'}{'sup': '2', 'Ris alkyl or deuteroalkyl;'}{'sup': 3', '19, 'sub': '2', 'Ris alkyl, deuteroalkyl, cycloalkyl or SOR;'}{'sup': '4', 'Rhydrogen or alkyl;'}{'sup': '19', 'Ris alkyl;'}{'sub': '2', 'E is CO or SO;'}{'sup': '1', 'Ris aryl, heteroaryl, heterocyclyl or cycloalkyl;'}{'sup': 1', '3', '3', 'u', 'x', 'u', 'y', 'z', 'u', 'y', 'z', 'u', 'y', 'z', 'u', 'x', 'w', '4', '4, 'sub': t', 't, 'claim-text': [{'sup': 'u', 'each Ris independently alkylene or a direct bond;'}, {'sup': 'w', 'Ris alkyl or amino;'}, {'sup': 'x', 'each Ris independently hydrogen, alkyl or hydroxyalkyl;'}, {'sup': y', 'z, 'Rand Rare each independently selected from (i) or (ii) below, {'sup': y', 'z', 'y', 'z', '5, '(i) Ris hydrogen or alkyl; and Ris hydrogen, alkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, ...

BERBERINE-URSODEOXYCHOLIC ACID CONJUGATE FOR TREATING THE LIVER

The present invention is a method and compound for treating liver cancer. The invention treats liver cancer by directing a cancer-fighting drug into the liver hepatoportal circuit. The cancer-fighting drug is attached to a natural produced molecule which functions primarily in the hepatoportal circuit and has organotropism for the hepatoportal circuit. 2. The compound of claim 1 , wherein said R is a hydrogen atom.3. The compound of claim 1 , wherein said R is a functional group.4. The compound of claim 1 , wherein said R is an ethyl group.6. The method of synthesizing a molecule of claim 5 , further comprising the steps:cooling said first synthesized compound; andrecrystallizing said first synthesized compound to create a crystalized solid.7. The method of synthesizing a molecule of claim 6 , further comprising the steps:mixing said crystallized solid with a first solvent and adding 1,6-dibromohexane to create a first mixture;heating said first mixture;diluting with a first precipitation solvent to create a first precipitate; andfiltering said first precipitate and washing said first precipitate with a first washing solvent to create a first crude compound.8. The method of synthesizing a molecule of claim 7 , further comprising the steps:purifying said first crude compound to create a first purified compound.9. The method of synthesizing a molecule of claim 8 , further comprising the steps:dissolving said first purified compound in a second solvent;adding aqueous ammonia and ammonium chloride; andstirring to create a second mixture.10. The method of synthesizing a molecule of claim 9 , further comprising the steps:evaporating said second mixture to create a second crude compound.11. The method of synthesizing a molecule of claim 10 , further comprising the steps:purifying said second crude compound to create a second purified compound.12. The method of synthesizing a molecule of claim 11 , further comprising the steps:mixing said second purified compound and ...

COMPOUNDS TARGETING MUTANT CALRETICULIN

The present invention relates to compounds binding to calreticulin which selectively inhibit growth of CALR mutant cells and/or exhibit selective cytotoxicity towards CALR mutant cells, to pharmaceutical compositions comprising such compounds as well as to their use in treating diseases or conditions caused by or associated with a mutation of CALR, in particular myeloid malignancies, such as myeloproliferative neoplasms or myelodysplasia syndrome. The present invention also relates to screening assays allowing the identification of such compounds. 5. The compound for use of any one of to , wherein each of rings A and B is independently selected from benzo , pyridino , pyrimidino , and hydrated forms thereof , wherein the sum of m1 and m2 is 1 to 7 , preferably the sum of m1 and m2 is 1 , 2 , 3 , 4 , 5 , or 6.7. The compound for use of any one of to , wherein each of Rand Ris independently selected from the group consisting of Calkyl , Calkenyl , Calkynyl , Ccycloalkyl , Caryl , 3- to 7-membered heterocyclyl , 3- to 7-membered heteroaryl , halogen , —CN , —NO , —OH , —O(Calkyl) , —CF , —OCF , —O(CH)(Ccycloalkyl) , —O(CH)(Caryl) , —O(CH)(3- to 7-membered heteroaryl) , —O(CH)(3- to 7-membered heterocyclyl) , —NH , —NH(Calkyl) , —N(Calkyl) , —NHS(O)(Calkyl) , —S(O)NH(Calkyl) , —C(═O)(Calkyl) , —C(═O)OH , —OC(═O)R , —C(═O)O(Calkyl) , —C(═O)NH(Calkyl) , —NHC(═O)H , —NHC(═O)(Calkyl) , —NHC(═NH)NH(Calkyl) , —N(Calkyl)C(═NH)NH(Calkyl) , and —(Calkylene)OH , wherein z is 0 , 1 , or 2; and Ris selected from the group consisting of Calkyl , Ccycloalkyl , Caryl , 3- to 7-membered heterocyclyl , and 3- to 7-membered heteroaryl , and is optionally substituted with one or two independently selected R; and/or any two Rwhich are bound to the same carbon atom of ring A may join together to form ═O and/or any two Rwhich are bound to the same carbon atom of ring B may join together to form ═O and/or any two Ron adjacent ring atoms of ring A may join together with the adjacent ring atoms ...

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C-Calkyl) or S; each X is independently CH or N; Ris a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; Ris (LQ)Y; and each Ris independently H, C-Calkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy. 111.-. (canceled)13. The method of claim 12 , wherein the cancer is a lymphoma.14. The method of claim 12 , wherein Y is H. The present invention relates to novel compounds which act as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, for the treatment of cancer, immune and inflammatory diseases.The phosphoinositide 3-kinases (PI3Ks) constitute a family of lipid kinases involved in the regulation of a network of signal transduction pathways that control a range of cellular processes. PI3Ks are classified into three distinct subfamilies, named class I, II, and Ill based upon their substrate specificities. Class IA PI3Ks possess a p110α, p110β, or p110δ catalytic subunit complexed with one of three regulatory subunits, p85α, p85β or p55δ. Class IA PI3Ks are activated by receptor tyrosine kinases, antigen receptors, G-protein coupled receptors (GPCRs), and cytokine receptors. The class IA PI3Ks primarily generate phosphatidylinositol-3,4,5-triphosphate (PI(3,4,5)P), a second messenger that activates the downstream target AKT. The consequences of biological activation of AKT include tumour cell progression, proliferation, survival and growth, and there is significant evidence suggesting that the PI3K/AKT pathway is dysregulated in many human cancers. Additionally, PI3K activity has been implicated in endocrinology, cardiovascular disease, immune disorders and inflammation. It has been established that PI3K-p110δ plays a critical role in the recruitment and activation of immune and inflammatory cells. PI3K- ...

INHIBITORS OF HIV REPLICATION

Compounds of formula (I) and pharmaceutical compositions thereof: wherein AAand Aare each independently selected from the group consisting of N and CR, wherein Ris an optionally substituted heterocyclyl or an optionally substituted —(C)alkyl-heterocyclyl, Ris an optionally substituted aryl or an optionally subsisted heteroaryl, Ris an optionally substituted aryl, an optionally substituted heterocyclyl or an optionally substituted heteroaryl, useful as an inhibitor of HIV replication. 2. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein A claim 1 , Aand Aare each independently selected from CR.3. The compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein one of A claim 1 , Aand Ais N and the remaining two of A claim 1 , Aand Aare each independently selected from CR.4. The compound according to claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , wherein Ris heterocyclyl or —(C)alkyl-heterocyclyl claim 3 , wherein each said heterocyclyl and —(C)alkyl-heterocyclyl is optionally substituted with 1 to 2 substituents each independently selected from —(C)alkyl; and wherein said heterocyclyl is a 5- claim 3 , 6- or 7-membered heterocycle containing one oxygen atom.6. The compound according to claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris a 5- or 6-membered heteroaryl optionally substituted with 1 to 2 substituents each independently selected from the group consisting of —(C)alkyl claim 5 , halo claim 5 , —(C)haloalkyl claim 5 , —N(R)(R) and —O(C)alkyl;{'sup': '21', 'sub': '1-3', 'Ris H or —(C)alkyl; and'}{'sup': '22', 'sub': 1-3', '2-4, 'Ris H, —(C)alkyl or —(C)alkenyl.'}8. The compound according to claim 7 , or a pharmaceutically acceptable salt thereof claim 7 , wherein Ris independently in each instance selected from the group consisting of H claim 7 , halo claim 7 , —CN claim 7 , —O(C)alkyl and —(C)alkyl optionally substituted with —O(C ...

PEPTIDE CONJUGATES OF CYTOTOXINS AS THERAPEUTICS

The present invention relates to peptide conjugates of cytotoxins such as topoisomerase I inhibitors which are useful for the treatment of diseases such as cancer. 3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a peptide capable of selectively delivering RQ- across a cell membrane having an acidic or hypoxic mantle having a pH less than about 6.0.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a peptide comprising at least one of the following sequences:ADDQNPWRAYLDLLFPTDTLLLDLLWCG (SEQ ID NO: 1; Pv1);AEQNPIYWARYADWLFTTPLLLLDLALLVDADECG (SEQ ID NO: 2; Pv2);ADDQNPWRAYLDLLFPTDTLLLDLLWDADECG (SEQ ID NO: 3; Pv3);Ac-AAEQNPIYWARYADWLFTTPLLLLDLALLVDADEGTKCG (SEQ ID NO: 4; Pv4); and{'sup': 7', '7, 'AAEQNPIYWARYADWLFTTPLLLLDLALLVDADEGTC (SEQ ID No. 5; Pv5); and wherein Ris attached to Q through a cysteine residue of R.'}5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a peptide comprising at least one of the following sequences:ADDQNPWRAYLDLLFPTDTLLLDLLWCG (SEQ ID NO: 1; Pv1),AEQNPIYWARYADWLFTTPLLLLDLALLVDADECG (SEQ ID NO: 2; Pv2), and{'sup': 7', '7, 'ADDQNPWRAYLDLLFPTDTLLLDLLWDADECG (SEQ ID NO: 3; Pv3), and wherein Ris attached to Q through a cysteine residue of R.'}6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a peptide comprising the sequence: ADDQNPWRAYLDLLFPTDTLLLDLLWCG (SEQ ID NO: 1; Pv1).7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a peptide comprising the sequence: AEQNPIYWARYADWLFTTPLLLLDLALLVDADECG (SEQ ID NO: 2; Pv2).9. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , and Rare each independently selected from H claim 1 , Calkyl claim 1 , Calkenyl claim 1 , Caryl claim 1 , 5-10 membered heteroaryl claim 1 , halo claim 1 , CN claim 1 , NO claim ...

Materials for organic light-emitting devices

The invention relates to compounds which are suitable for use in electronic devices, and electronic devices, in particular organic electroluminescent devices, containing said compounds.

AMINE COMPOUND HAVING HETERO-FUSED RING AND ORGANIC ELECTROLUMINESCENT ELEMENT USING AMINE COMPOUND

A compound represented by the following formula (1). 2. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , at least one of a and d is 1.3. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , a is 0 claim 1 , and b+c+d+c is 1 to 4.4. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , e is 0 and a+b+c+d is 1 to 4.5. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , a and d are 0 and b+c+e is 1 to 4.6. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , a and e are 0 and b+c+d is 1 to 4.7. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , a claim 1 , d and e are 0 and b+c is 1 or 2.8. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , a claim 1 , b and c are 0 and d is 1.9. The compound according to claim 1 , wherein claim 1 , in the formula (1) claim 1 , a claim 1 , b claim 1 , c and e are 0 and d is 1.10. The compound according to claim 1 , wherein Arand Arin the formula (1) are independently a substituted or unsubstituted phenylene group claim 1 , a substituted or unsubstituted naphthalenediyl group claim 1 , a substituted or unsubstituted anthracenediyl group claim 1 , a substituted or unsubstituted triphenylenediyl group claim 1 , a substituted or unsubstituted fluorenediyl group claim 1 , a substituted or unsubstituted benzofluorenediyl group claim 1 , a substituted or unsubstituted biphenyldiyl group claim 1 , a substituted or unsubstituted terphenyldiyl group claim 1 , a substituted or unsubstituted phenanthrenediyl group claim 1 , a substituted or unsubstituted fluoranthenediyl group claim 1 , a substituted or unsubstituted pyridinediyl group claim 1 , a substituted or unsubstituted pyrimidinediyl group claim 1 , a substituted or unsubstituted triazinediyl group claim 1 , a substituted or unsubstituted dibenzofuranediyl group claim 1 , a ...

POLYCYCLIC-CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): 172-. (canceled)74. The method of claim 73 , wherein the first additional therapeutic agent is tenofovir alafenamide.75. The method of claim 73 , wherein the first additional therapeutic agent is tenofovir alafenamide hemifumarate.76. The method of claim 73 , wherein the first additional therapeutic agent is tenofovir alafenamide fumarate.78. The method of claim 77 , wherein the first additional therapeutic agent is tenofovir alafenamide.79. The method of claim 77 , wherein the first additional therapeutic agent is tenofovir alafenamide hemifumarate.80. The method of claim 77 , wherein the first additional therapeutic agent is tenofovir alafenamide fumarate. This application is a continuation of U.S. application Ser. No. 15/349,353, filed Nov. 11, 2016, which is a continuation of U.S. application Ser. No. 14/977,347, filed Dec. 21, 2015, now U.S. Pat. No. 9,522,912, which claim the benefit of U.S. Provisional App. No. 62/096,291, filed Dec. 23, 2014, the disclosures of which are incorporated herein by reference in their entireties.Compounds, compositions, and methods which may be used for the treatment of human immunodeficiency virus (HIV) infection are disclosed. In particular, novel polycyclic carbamoylpyridone compounds and methods for their preparation and use as therapeutic or prophylactic agents are disclosed.Human immunodeficiency virus infection and related diseases are a major public health problem worldwide. Human immunodeficiency virus type 1 (HIV-1) encodes three enzymes which are required for viral replication: reverse transcriptase, protease, and integrase. Although drugs targeting reverse transcriptase and protease are in wide use and have shown effectiveness, particularly when employed in combination, toxicity and development of resistant strains have limited their usefulness (Palella, et al. . (1998) 338: ...

PYRIDIN-3-YL ACETIC ACID DERIVATIVES AS INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION

Disclosed are compounds of Formula I, including pharmaceutically acceptable salts, pharmaceutical compositions comprising the compounds, methods for making the compounds and their use in inhibiting HIV integrase and treating those infected with HIV or AIDS. 2. A compound or salt according to wherein Ris hydrogen claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , —Calkyl-OH claim 1 , —N(R)(R) claim 1 , or (R)(R)NCalkyl-.3. A compound or salt according to wherein Ris hydrogen or (R)(R)NCalkyl-.4. A compound or salt according to wherein Ris Ar—Calkyl- wherein Aris as defined above; or Arwherein Aris selected from benzofuropyrimidinyl claim 1 , pyrazinyl claim 1 , pyridinyl claim 1 , pyridofuropyrimidinyl claim 1 , or pyrimidinyl claim 1 , and is substituted with 0-3 substituents selected from R claim 1 , Calkyl claim 1 , —O—Calkyl claim 1 , —COH claim 1 , cyano claim 1 , halo claim 1 , Chaloalkyl claim 1 , or hydroxy wherein Ris as defined above.5. A compound or salt according to wherein Ris Ar—Calkyl- wherein Aris as defined above; or Arwherein Aris selected from benzofuropyrimidinyl claim 4 , pyridinyl claim 4 , or pyridofuropyrimidinyl claim 4 , and is substituted with 0-3 substituents selected from R claim 4 , Calkyl claim 4 , —O—Calkyl claim 4 , —COH claim 4 , cyano claim 4 , halo claim 4 , Chaloalkyl claim 4 , or hydroxy.6. A pharmaceutical composition comprising a compound or salt according to .7. The composition of further comprising at least one other agent used for treatment of AIDS or HIV infection selected from nucleoside HIV reverse transcriptase inhibitors claim 6 , non-nucleoside HIV reverse transcriptase inhibitors claim 6 , HIV protease inhibitors claim 6 , HIV fusion inhibitors claim 6 , HIV attachment inhibitors claim 6 , CCR5 inhibitors claim 6 , CXCR4 inhibitors claim 6 , HIV budding or maturation inhibitors claim 6 , and HIV integrase inhibitors claim 6 , and a pharmaceutically acceptable carrier.8. A method for treating HIV infection comprising ...

HETEROCYCLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME

A heterocyclic compound is represented by Formula 1: 2. The heterocyclic compound as claimed in claim 1 , wherein:{'sub': 1', '10', '60', '6', '60, 'ring Ais a C-Ccarbocyclic group with two or more rings condensed with each other, or a C-Cheterocyclic group with two or more rings condensed with each other.'}3. The heterocyclic compound as claimed in claim 1 , wherein:{'sub': '1', 'ring Ais a naphthalene, a fluorene, a benzofluorene, a phenanthrene, an anthracene, a quinoline, an isoquinoline, a benzoquinoline, a carbazole, a dibenzofuran, a dibenzothiophene, or a benzocarbazole.'}5. The heterocyclic compound as claimed in claim 1 , wherein:{'sub': '1', 'Lis selected froma benzene group, a fluorene group, an anthracene group, a pyridine group, a triazine group, and a carbazole group;{'sub': 1', '20', '1', '20', '31', '32', '33', '31', '32', '31', '32, 'a benzene group, a fluorene group, an anthracene group, a pyridine group, a triazine group, and a carbazole group, each substituted with at least one selected from deuterium, —F, —Cl, —Br, —I, a hydroxyl group, a cyano group, a C-Calkyl group, a C-Calkoxy group, a phenyl group, a biphenyl group, a terphenyl group, a naphthyl group, —Si(Q)(Q)(Q), —N(Q)(Q), and —B(Q)(Q); and'}{'sub': 2', '4', '4, '*—S(═O)—*′, *—S(═O)—*′, *—P(═O)(Q)—*′, and *—P(═S)(Q)—*′,'}{'sub': 4', '31', '33', '1', '20', '1', '20, 'Qand Qto Qare each independently selected from a C-Calkyl group, a C-Calkoxy group, a phenyl group, a biphenyl group, a terphenyl group, and a naphthyl group, and'}* and *′ each indicate a binding site to a neighboring atom.6. The heterocyclic compound as claimed in claim 1 , wherein:a1 is an integer selected from 0 to 3.8. The heterocyclic compound as claimed in claim 1 , wherein:{'sub': '1', 'Aris selected froma phenyl group, a biphenyl group, a terphenyl group, a naphthyl group, a fluorenyl group, a phenanthrenyl group, a pyridinyl group, a dinaphthofuranyl group, and a benzoimidazonaphthoimidazolyl group;{'sub': 1', '20 ...

Dyes and Labeled Molecules

Dimeric and trimeric nucleic acid dyes, and associated systems and methods are provided. Such a dye may form a hairpin-like structure that enables it to stain nucleic acids via a release-on-demand mechanism, for example. Such a dye may have low background fluorescence in the absence of nucleic acids and high fluorescence in the presence of nucleic acids, upon binding therewith, for example. A dye provided herein may be useful in a variety of applications, such as in DNA quantitation in real-time PCR, for example.

ORGANIC ELECTROLUMINESCENCE ELEMENT AND MATERIAL FOR ORGANIC ELECTROLUMINESCENCE

An organic electroluminescence element including an anode, a plurality of organic functional layers including a light-emitting layer, and a cathode in that order wherein the organic functional layer containing a compound having a structure represented by the following general formula (1) is arranged between the light-emitting layer and the cathode, wherein X, Xto X, R, and Lare as defined in the specification. 4. The organic electroluminescence element according to claim 1 , wherein Xand Xrepresent a nitrogen atom.5. The organic electroluminescence element according to claim 1 , wherein Xand Xrepresent a nitrogen atom.6. The organic electroluminescence element according to claim 1 , wherein Xand Xrepresent a nitrogen atom.7. The organic electroluminescence element according to claim 1 , wherein Xand Xrepresent a nitrogen atom.8. The organic electroluminescence element according to claim 1 , wherein Xto Xrepresent CR.9. The organic electroluminescence element according to claim 1 , wherein at least one of Xto Xrepresents a nitrogen atom.10. The organic electroluminescence element according to claim 1 , wherein Rrepresents a substituent including a pyridine ring claim 1 , a pyrazine ring claim 1 , a triazine ring claim 1 , a pyrimidine ring claim 1 , an azadibenzofuran ring claim 1 , an azadibenzothiophene ring claim 1 , an azacarbazole ring claim 1 , a quinazoline ring claim 1 , a quinoxaline ring claim 1 , a quinoline ring claim 1 , an isoquinoline ring claim 1 , a benzoquinoline ring claim 1 , a benzisoquinoline ring claim 1 , an indole ring claim 1 , an imidazole ring claim 1 , a benzimidazole ring claim 1 , a pyrazole ring claim 1 , a triazole ring claim 1 , an oxazole ring claim 1 , a triazole ring claim 1 , or a carbazole ring.11. The organic electroluminescence element according to claim 2 , wherein in the general formula (1) claim 2 , Xand Xrepresent a nitrogen atom and Xto Xrepresent CR claim 2 , or Xand Xrepresent a nitrogen atom and X claim 2 , X claim 2 , ...

COMPOUNDS AND METHODS FOR INHIBITING MITOTIC PROGRESSION

This invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides compounds that inhibit Aurora kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer. 2. The compound of claim 1 , wherein:{'sup': x', 'y', '3', 'x', 'y, 'sub': '1-6', 'each of Rand Rindependently is hydrogen, fluoro, or a Caliphatic optionally substituted with one or two R; or Rand R, taken together with the carbon atom to which they are attached, form an optionally substituted 3- to 6-membered cycloaliphatic ring;'}{'sup': e', '4', '3', '7, 'sub': '1-3', 'Ris hydrogen, —OH, —NHR, —SH, or a Caliphatic optionally substituted with Ror R;'}{'sup': f1', 'f2, 'Rand Rtogether form a bond;'}{'sub': 2', '1-3', '1-3', '1-3', '2', '1-3', '1-3', '1-3, 'sup': 1', '7', '1', '7', '1', '7, 'G is —H, —OH, —NH, —O(Calkyl), —NH(Calkyl), —N(Calkyl), Calkyl, Cfluoroalkyl, —O-L-R, —N(Calkyl)-L-R, or -L-R; and'}{'sup': '1', 'sub': '1-3', 'Lis a covalent bond or Calkylene.'}5. The compound of claim 3 , wherein each of Rand Rindependently is hydrogen claim 3 , fluoro claim 3 , or a Caliphatic optionally substituted with one or two R; or Rand R claim 3 , taken together with the carbon atom to which they are attached claim 3 , form an optionally substituted 3- to 6-membered cycloaliphatic ring.6. The compound of claim 5 , wherein Ring A is a substituted or unsubstituted ring selected from the group consisting of furano claim 5 , dihydrofurano claim 5 , thieno claim 5 , dihydrothieno claim 5 , cyclopenteno claim 5 , cyclohexeno claim 5 , 2H-pyrrolo claim 5 , pyrrolo claim 5 , pyrrolino claim 5 , pyrrolidino claim 5 , oxazolo claim 5 , thiazolo claim 5 , imidazolo claim 5 , imidazolino claim 5 , imidazolidino claim 5 , pyrazolo claim 5 , pyrazolino claim 5 , pyrazolidino claim 5 , isoxazolo claim 5 , isothiazolo claim 5 , oxadiazolo claim 5 , triazolo claim 5 , thiadiazolo claim 5 , 2H-pyrano claim 5 , 4H- ...

FUSED TETRACYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE

A fused tetracyclic compound and application thereof in medicine, especially as a medicament for the treatment and/or prevention of hepatitis B. A compound having Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, in medicine, especially as a medicament for the treatment and/or prevention of hepatitis B, wherein each variable is as defined in the specification. 3. The compound of claim 1 , wherein Ris hydrogen claim 1 , deuterium claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , hydroxy claim 1 , cyano claim 1 , Calkyl claim 1 , Calkynyl claim 1 , Ccycloalkyl claim 1 , heterocyclyl consisting of 3 to 6 ring atoms claim 1 , phenyl claim 1 , heteroaryl consisting of 5 ring atoms claim 1 , heteroaryl consisting of 6 ring atoms or R—Calkylene-O— claim 1 , wherein each of Calkyl claim 1 , Calkynyl claim 1 , Ccycloalkyl claim 1 , heterocyclyl consisting of 3 to 6 ring atoms claim 1 , phenyl claim 1 , heteroaryl consisting of 5 ring atoms claim 1 , heteroaryl consisting of 6 ring atoms and —Calkylene- of R—Calkylene-O— is independently unsubstituted or substituted by 1 claim 1 , 2 claim 1 , 3 or 4 R;{'sup': 10', 'n', 'j, 'sub': 1-4', '3-6', '1-4', '3-6, 'Ris deuterium, RO—, Calkyl, Ccycloalkyl, heterocyclyl consisting of 3 to 6 ring atoms, phenyl, heteroaryl consisting of 5 ring atoms or heteroaryl consisting of 6 ring atoms, wherein each of Calkyl, Ccycloalkyl, heterocyclyl consisting of 3 to 6 ring atoms, phenyl, heteroaryl consisting of 5 ring atoms and heteroaryl consisting of 6 ring atoms is independently unsubstituted or substituted by 1, 2, 3, or 4 R.'}4. The compound of claim 1 ,{'sup': 1', '10', '10', '10', '10', '10', '10', '10', 'g, 'sub': 2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2', '2', '3', '2', '3, 'wherein Ris hydrogen, deuterium, F, Cl, Br, hydroxy, cyano, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, ethynyl, propargyl, propynyl, ...

Tricyclic heterocyclic compounds as phosphoinositide 3-kinase inhibitors

A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C 1 -C 10 alkyl) or S; each X is independently CH or N; R 1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R 2 is LY; each L is a direct bond, C 1 -C 10 alkylene, C 2 -C 10 alkenylene or C 2 -C 10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R 3 is independently H, C 1 -C 10 alkyl, halogen, fluoro C 1 -C 10 alkyl, O— C 1 -C 10 alkyl, NH—C 1 -C 10 alkyl, S—C 1 -C 10 alkyl, O-fluoro C 1 -C 10 alkyl, NH-acyl, NH—C(O)—NH—C 1 -C 10 alkyl, C(O)—NH—C 1 -C 10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.

SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS

The present invention relates to Substituted Quinolizine Derivatives of Formula (I): 115.-. (canceled)17. A pharmaceutical composition comprising an effective amount of a compound according to claim 16 , or a pharmaceutically acceptable salt thereof claim 16 , and a pharmaceutically acceptable carrier.18. A method for the inhibition of HIV integrase in a subject in need thereof which comprises administering to the subject an effective amount of the compound according claim 16 , or a pharmaceutically acceptable salt thereof.19. A method for the treatment of infection by HIV or for the treatment of AIDS in a subject in need thereof claim 16 , which comprises administering to the subject an effective amount of the compound according to claim 16 , or a pharmaceutically acceptable salt thereof.20. (canceled)21. The pharmaceutical composition of claim 17 , further comprising one or more additional therapeutic agents selected from claim 17 , lamivudine claim 17 , abacavir claim 17 , ritonavir claim 17 , darunavir claim 17 , atazanavir claim 17 , emtricitabine claim 17 , tenofovir claim 17 , rilpivirine and lopinavir.22. The method of claim 17 , further comprising administering to the subject one or more additional therapeutic agents selected from claim 17 , abacavir claim 17 , lamivudine claim 17 , ritonavir and lopinavir claim 17 , wherein the amounts administered of the compound of . The present invention relates to Substituted Quinolizine Derivatives, compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.A retrovirus designated human immunodeficiency virus (HIV), particularly the strains known as HIV type-1 (HIV-1) virus and type-2 (HIV-2) virus, is the etiological agent of the complex disease that includes progressive destruction of the immune system (acquired immune deficiency syndrome; AIDS) and degeneration of the central and ...

Derivatives Of Protoberberine Biological Alkaloids And Use Of Same Inhibiting Ulcerative Colitis

Disclosed are derivatives of protoberberine biological alkaloids or physiologically acceptable salts thereof produced by means of a derivative reaction of a source material of biological alkaline quaternary ammonium salts of protoberberine alkaloids, a preparation method for same and pharmaceutical uses thereof. The derivatives of protoberberine biological alkaloids or the physiologically acceptable salts thereof show activity inhibiting ulcerative colitis and can be used in the preparation of drugs for same. 10. A pharmaceutical composition , characterized in comprising effective amount of the compound according to any one of to and common pharmaceutically acceptable carriers.11. Use of the compound according to any one of to in the preparation of drugs for the treatment of ulcerative colitis. The present invention relates to novel protoberberine alkaloid derivatives obtained from various protoberberine alkaloids quaternium as substrate through various derivatization reactions or their physiologically acceptable salts, their preparation method and the use of them as a drug for inhibition of ulcerative colitis. The use as anti-ulcerative colitis (UC) drugs of some known protoberberine alkaloid derivatives obtained from various protoberberine alkaloids quaternium as substrate through various derivatization reactions is also involved. The specific protoberberine alkaloid derivatives or their physiologically acceptable salts are as follows: dihydrocoptisine, dihydropseudocoptisine, dihydroberberine, dihydropalmatine, 3-methyldihydrocoptisine, (±)-8-cyanodihydrocoptisine, (±)-8-cyanodihydropseudocoptisine, 8-oxodihydrocoptisine, 8-oxodihydropseudocoptisine, (±)-8-acylmethyldihydrocoptisine, 8-(1-acyl-2-alkyl-ethenyl)-13-alkylcoptisine quaternium, and 8-(1-acyl-2-alkyl-ethenyl)-13-alkylberberine quaternium. The present invention belongs to innovative drug research field.Inflammatory bowel disease (IBD) is a kind of chronic inflammatory disease with its etiology and ...

TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE

The present invention relates to novel tricyclic compounds which can bind to FXR and act as modulators of the FXR, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the uses of the compounds for the treatment of diseases and/or conditions mediated by FXR. The invention further provides a pharmaceutical composition containing the compound disclosed herein and a method of treatment of diseases and/or conditions mediated by FXR comprising administering the compound or the pharmaceutical composition. 2. (canceled)3. The compound of claim 1 , wherein{'sup': '1', 'sub': 1-6', '1-6', '1-6', '3-6', '2-6', '2-6', '2-6', '1-6', '1-6', '6-10', '1-9, 'each Ris independently H, deuterium, F, Cl, Br, I, hydroxy, amino, nitro, cyano, Calkyl, Chaloalkyl, Chaloalkoxy, Ccycloalkyl, Cheterocyclyl, Calkenyl, Calkynyl, Calkylamino, Calkoxy, Caryl or Cheteroaryl;'}{'sup': '2', 'sub': 1-6', '1-6', '1-6', 'C1-6', '1-6', '3-6', '1-6', '2-6', '1-6', '1-6, 'Ris H, deuterium, F, Cl, Br, I, hydroxy, amino, nitro, cyano, Calkyl, Chaloalkyl, Chaloalkoxy, alkoxy—C-alkyl, Ccycloalkyl, Chydroxyalkyl, Cheterocyclyl, Calkylamino or Calkoxy; and'}{'sub': 1-6', '2-6', '2-6', '3-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '2-9', '6-10', '1-9, 'sup': I', '2', '9, 'Wherein each of said hydroxy, amino, Calkyl, Calkenyl, Calkynyl, Ccycloalkyl, Chaloalkyl, Calkylamino, Calkoxy, Chaloalkoxy, Chydroxyalkyl, Calkoxy—C-alkyl, Cheterocyclyl, Caryl and Cheteroaryl of Rand Ris independently and optionally substituted with one or more R; or'}{'sup': '1', 'sub': 1-3', '1-3', 'h3', 'C3-6', '2-9', '2-4', '2-4', '1-3', '1-3', '6-10', '1-9, 'wherein each Ris independently H, deuterium, F, Cl, Br, I, hydroxy, amino, nitro, cyano, Calkyl, Chaloalkyl, Chaloalkoxy, cycloalkyl, Cheterocyclyl, Calkenyl, Calkynyl, Calkylamino, Calkoxy, Caryl or Cheteroaryl;'}{'sup': '2', 'sub': 1-3', '1-3', '1-3', '1-3', '1-3', ...

TETRACYCLIC PYRIDONE COMPOUNDS AS ANTIVIRALS

The invention provides compounds of Formula (I) 5. A pharmaceutical composition claim 1 , comprising a compound of admixed with at least one pharmaceutically acceptable carrier.6. A method to treat a hepatitis B infection claim 1 , which comprises administering to a patient having a hepatitis B infection a compound of .7. The method of claim 1 , wherein the compound of is used in combination with an additional therapeutic agent selected from an interferon or peginterferon claim 1 , an HBV polymerase inhibitor claim 1 , a viral entry inhibitor claim 1 , a viral maturation inhibitor claim 1 , a capsid assembly inhibitor claim 1 , an HBV core modulator claim 1 , a reverse transcriptase inhibitor claim 1 , a TLR-agonist claim 1 , or an immunomodulator.8. A pharmaceutical composition claim 2 , comprising a compound of admixed with at least one pharmaceutically acceptable carrier.9. A method to treat a hepatitis B infection claim 2 , which comprises administering to a patient having a hepatitis B infection a compound of .1018. The method of claim 9 , wherein the compound of claim is used in combination with an additional therapeutic agent selected from an interferon or peginterferon claim 9 , an HBV polymerase inhibitor claim 9 , a viral entry inhibitor claim 9 , a viral maturation inhibitor claim 9 , a capsid assembly inhibitor claim 9 , an HBV core modulator claim 9 , a reverse transcriptase inhibitor claim 9 , a TLR-agonist claim 9 , or an immunomodulator.11. A pharmaceutical composition claim 3 , comprising a compound of admixed with at least one pharmaceutically acceptable carrier.12. A method to treat a hepatitis B infection claim 3 , which comprises administering to a patient having a hepatitis B infection a compound of .13. The method of claim 3 , wherein the compound of is used in combination with an additional therapeutic agent selected from an interferon or peginterferon claim 3 , an HBV polymerase inhibitor claim 3 , a viral entry inhibitor claim 3 , a viral ...

ENZYME INHIBITORS

The present invention provides compounds of formula (I): 1. A compound that is:N-({6-[4-(difluoromethyl)-1,2,3-triazol-1-yl]-2-fluoro-3-methoxyphenyl}methyl)-3-(methoxymethyl)-1-[(2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]pyrazole-4-carboxamide;N-{[2-fluoro-3-methoxy-6-(4-methyl-1,2,3-triazol-1-yl)phenyl]methyl}-3-(methoxymethyl)-1-[(2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]pyrazole-4-carboxamide;N-{[2-fluoro-3-methoxy-6-(3-methyl-1,2,4-triazol-1-yl)phenyl]methyl}-3-(methoxymethyl)-1-[(2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]pyrazole-4-carboxamide;N-{[6-(3-cyanopyrazol-1-yl)-2-fluoro-3-methoxyphenyl]methyl}-3-(methoxymethyl)-1-[(2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]pyrazole-4-carboxamide;N-({2-fluoro-3-methoxy-6-[3-(trifluoromethyl)-1,2,4-triazol-1-yl]phenyl}methyl)-3-(methoxymethyl)-1-[(2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]pyrazole-4-carboxamide;N-({6-[3-(difluoromethyl)-1,2,4-triazol-1-yl]-2-fluoro-3-methoxyphenyl}methyl)-3-(methoxymethyl)-1-[(2-methyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]pyrazole-4-carboxamide;N-({2-fluoro-3-methoxy-6-[3-(trifluoromethyl)-1,2,4-triazol-1-yl]phenyl}methyl)-1-[(2-isopropyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]-3-(methoxymethyl)pyrazole-4-carboxamide;N-({6-[3-(difluoromethyl)-1,2,4-triazol-1-yl]-2-fluoro-3-methoxyphenyl}methyl)-1-[(2-isopropyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]-3-(methoxymethyl)pyrazole-4-carboxamide;N-{[6-(3-cyanopyrazol-1-yl)-2-fluoro-3-methoxyphenyl]methyl}-1-[(2-isopropyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]-3-(methoxymethyl)pyrazole-4-carboxamide;1-[(2-ethyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]-N-({2-fluoro-3-methoxy-6-[3-(trifluoromethyl)-1,2,4-triazol-1-yl]phenyl}methyl)-3-(methoxymethyl)pyrazole-4-carboxamide;N-({6-[3-(difluoromethyl)-1,2,4-triazol-1-yl]-2-fluoro-3-methoxyphenyl}methyl)-1-[(2-ethyl-3,4-dihydro-1H-isoquinolin-7-yl)methyl]-3-(methoxymethyl)pyrazole-4-carboxamide;N-{[6-(3-cyanopyrazol-1-yl)-2-fluoro-3-methoxyphenyl]methyl}-1-[(2-ethyl-3, ...

Compounds for the Treatment of Kinase-Dependent Disorders

Disclosed herein are compounds of Formula I′. Compounds of Formula I′ inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.

HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DIODE COMPRISING SAME

The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same. 2. The heterocyclic compound of claim 1 , wherein the “substituted or unsubstituted” means being substituted with one or more substituents selected from the group consisting of C1 to C60 linear or branched alkyl; C2 to C60 linear or branched alkenyl; C2 to C60 linear or branched alkynyl; C3 to C60 monocyclic or polycyclic cycloalkyl; C2 to C60 monocyclic or polycyclic heterocycloalkyl; C6 to C60 monocyclic or polycyclic aryl; C2 to C60 monocyclic or polycyclic heteroaryl; —SiRR′R″; —P(═O)RR′; C1 to C20 alkylamine; C6 to C60 monocyclic or polycyclic arylamine; and C2 to C60 monocyclic or polycyclic heteroarylamine claim 1 , or being unsubstituted claim 1 , or being substituted with a substituent linking two or more substituents selected from among the substituents illustrated above claim 1 , or being unsubstituted; andR, R′ and R″ have the same definitions as in Chemical Formula 1.4. The heterocyclic compound of claim 1 , wherein Rand Rare hydrogen.5. The heterocyclic compound of claim 1 , wherein L is a substituted or unsubstituted C6 to C60 arylene group; or a substituted or unsubstituted C2 to C60 heteroarylene group.6. The heterocyclic compound of claim 1 , wherein Z is selected from the group consisting of hydrogen; a substituted or unsubstituted C6 to C60 aryl group; and a substituted or unsubstituted C2 to C60 heteroaryl group.8. An organic light emitting device comprising:a first electrode;a second electrode provided opposite to the first electrode; andone or more organic material layers provided between the first electrode and the second electrode,{'claim-ref': {'@idref': 'CLM-00001', '#text': 'claim 1'}, '#text': 'wherein one or more layers of the organic material layers comprise the heterocyclic compound of .'}9. The organic light emitting device of claim 8 , wherein the organic material layer comprises a ...

METABOTROPHIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS USE THEREOF

Compounds that modulate GluR5 activity and methods of using the same are disclosed. 3. (canceled)67-. (canceled)9. (canceled)10. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to and a pharmaceutically acceptable carrier.11. A method for treating a disorder or disease mediated by mGluR5 claim 1 , comprising administering to a subject in need thereof a therapeutically effective amount of a compound according to .12. The method of claim 11 , wherein the disorder or disease mediated by mGluR5 is a neurological disorder.13. The method of claim 12 , wherein the neurological disorder is a neurodegenerative disease claim 12 , a neuropsychiatric disease claim 12 , an affective disorder claim 12 , a loss of cognitive function or a learning and memory disorder.14. The method according to claim 11 , wherein the disease or disorder is psychosis.15. The method according to claim 11 , wherein the disease or disorder is schizophrenia.16. The method according to claim 11 , wherein the disease or disorder is cognitive impairment associated with schizophrenia.17. The method according to claim 11 , wherein the disease or disorder is Alzheimer's disease.18. The method according to claim 11 , wherein the disease or disorder is cognitive disorder.1920-. (canceled) This application claims priority to U.S. Provisional Patent Application No. 61/494,731, filed Jun. 8, 2011. The entire contents of the foregoing application are hereby incorporated by reference.The amino acid L-glutamate (which herein is referred to simply as glutamate) is the principal excitatory neurotransmitter in the brain and other elements of the central nervous system of mammals. Glutamate binds to neurons and activates cell surface receptors. Glutamate has significant roles in motor control, cognitive function, sensory perception, and acts as a mediator of persistent changes in the strength of synaptic signaling (synaptic plasticity), thereby modulating long term ...

COMPOUND HAVING AZAINDENO[1,2-c]PHENANTHRENE RING STRUCTURE, AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

A compound has an azaindeno phenanthrene ring structure, the compound being represented by the following general formula (A-1).

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C-Calkyl) or S; each X is independently CH or N; Ris a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; Ris (LQ)Y; and each Ris independently H, C-Calkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy. 111.-. (canceled)13. The composition of claim 12 , wherein both of the Rgroups that are attached to the 6 claim 12 ,5-ring system in formula I are H.14. The composition of claim 12 , wherein Y is H.15. The composition of claim 12 , wherein Q is selected from —NR— and —NRR—.16. The composition of claim 12 , wherein Q is —NRRwherein Rand Rtogether with the nitrogen to which they are attached form a 5 to 7-membered heterocycle linker having an additional heteroatom O; and Y is H.18. The method of claim 17 , wherein Y is H. The present invention relates to novel compounds which act as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, for the treatment of cancer, immune and inflammatory diseases.The phosphoinositide 3-kinases (PI3Ks) constitute a family of lipid kinases involved in the regulation of a network of signal transduction pathways that control a range of cellular processes. PI3Ks are classified into three distinct subfamilies, named class I, II, and III based upon their substrate specificities. Class IA PI3Ks possess a p110α, p110β, or p110δ catalytic subunit complexed with one of three regulatory subunits, p85α, p85β or p55δ. Class IA PI3Ks are activated by receptor tyrosine kinases, antigen receptors, G-protein coupled receptors (GPCRs), and cytokine receptors. The class IA PI3Ks primarily generate phosphatidylinositol-3,4,5-triphosphate (PI(3,4,5)P), a second messenger that activates the downstream target AKT. The consequences of biological activation of AKT include tumour cell progression, ...

PYRIDYLAMINO SUBSTITUTED HETEROTRICYCLIC COMPOUNDS, AND PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF

The present disclosure relates to pyridinamine-substituted heterotricyclo compounds, a preparation method thereof, and a use thereof in medicines. Specifically, a compound of formula (I), or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, a preparation method and a use thereof are disclosed, wherein the groups in the formula (I) are as defined in the Description and claims. 2. The compound of , or a pharmaceutically acceptable salt , stereoisomer , solvate or prodrug thereof , wherein Y is Ccycloalkyl , 4 to 6 membered saturated single heterocycle , 5 to 6 membered monocyclic heteroaryl ring , spiro , spiroheterocycle , bridged ring or bridged heterocycle , wherein the cycloalkyl , 4 to 6 membered saturated single heterocycle , 5 to 6 membered monocyclic heteroaryl ring , spiro , spiroheterocycle , bridged ring or bridged heterocycle is unsubstituted or substituted with —(CH)-L; wherein Lis CN , acetyl , hydroxy , hydroxymethyl , hydroxyethyl , carboxyl , —C(O)OCalkyl , Calkyl , Ccycloalkyl , halogenated Calkyl , NRR , Calkoxy , azetidine , oxetane , tetrahydrothiophene , pyrrolidine , tetrahydrofuran , piperidine , oxazolidine , piperazine , dioxolane , dioxane , morpholine , thiomorpholine , thiomorpholine-1 , 1-dioxide or tetrahydropyrane; m is 0 , 1 or 2; R , Rare as defined in .3. The compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , solvate or prodrug thereof claim 1 , wherein Y is a group selected from: cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , azetidine claim 1 , pyrrolidine claim 1 , tetrahydrofuran claim 1 , piperidine claim 1 , piperazine claim 1 , morpholine or tetrahydropyrane claim 1 , wherein the Y group is unsubstituted or substituted with Lor —CH-L; Lis CN claim 1 , acetyl claim 1 , hydroxy claim 1 , hydroxymethyl claim 1 , hydroxyethyl claim 1 , carboxyl claim 1 , —C(O)OCH claim 1 , —C(O)OCHCH claim 1 , —C(O)OC(CH) claim 1 , —C(O)OCH(CH) claim 1 , methyl ...

LATE SV40 (LSF) INHIBITORS

The present invention is directed to compositions, methods and kits for treatment of cancer, e.g. hepatocellular carcinoma (HCC). In some embodiments, the present invention discloses the use of a small-molecule compounds of Formula (I)-(V) to inhibit tubulin methylation or to modulate chromatin or cytoskeleton modification in a cell. 2. The compound of claim 1 , wherein Rand Rare independently an aryl substituted with at least one ORand optionally further substituted with halogen claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Cheteroalkyl claim 1 , C-Calkoxy claim 1 , C-Calkenyl claim 1 , amino (NH) claim 1 , mono(C-Calkyl)amino or di(C-Calkyl)amino.3. The compound of claim 2 , wherein Rand Rare independently an aryl substituted with at least one C-Calkoxy and at least one halogen claim 2 , amino (NH) claim 2 , mono(C-Calkyl)amino or di(C-Calkyl)amino.4. The compound of claim 1 , wherein Rand Rare independently a phenyl substituted with at least one ORand optionally further substituted with halogen claim 1 , C-Calkyl claim 1 , C-Chaloalkyl claim 1 , C-Cheteroalkyl claim 1 , C-Calkoxy claim 1 , amino (NH) claim 1 , mono(C-Calkyl)amino or di(C-Calkyl)amino.5. The compound of claim 4 , wherein Rand Rare independently a phenyl substituted with at least one C-Calkoxy and at least one halogen claim 4 , C-Calkyl claim 4 , C-Chaloalkyl claim 4 , C-Cheteroalkyl claim 4 , C-Calkoxy claim 4 , amino (NH) claim 4 , mono(C-Calkyl)amino or di(C-Calkyl)amino.6. The compound of claim 5 , wherein Rand Rare independently a phenyl substituted with at least one C-Calkoxy and at least one halogen claim 5 , amino (NH) claim 5 , mono(C-Calkyl)amino or di(C-Calkyl)amino.7. The compound of claim 6 , wherein Rand Rare independently phenyl substituted with at least one C-Calkoxy and at least one halogen or di(C-Calkyl)amino.9. The compound of claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , R claim 1 , Rand Rare independently selected from the group consisting of H ...

AMINE-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS EHMT2 INHIBITORS AND METHODS OF USE THEREOF

The present disclosure relates to amine-substituted heterocyclic compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., cancer) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted heterocyclic compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes. 3. The compound of claim 1 , wherein the compound is of Formula (I0) or a tautomer thereof claim 1 , or a pharmaceutically acceptable salt of the compound or the tautomer.6. The compound any one of the preceding claims claim 1 , wherein ring B is C-Caryl or 5- to 10-membered heteroaryl.9. The compound any one of the preceding claims claim 1 , wherein ring B is C-Caryl or 5- to 10-membered heteroaryl substituted with one R.12. The compound of claim 2 , being of Formula (I) or a tautomer thereof claim 2 , or a pharmaceutically acceptable salt of the compound or the tautomer.17. The compound of any one of the preceding claims claim 2 , wherein at least one of X claim 2 , X claim 2 , Xand Xis N.18. The compound of any one of the preceding claims claim 2 , wherein Xand Xare N.19. The compound of any one of the preceding claims claim 2 , wherein Xand Xare N claim 2 , Xis CRand Xis CR.20. The compound of any one of the preceding claims claim 2 , wherein Ris C-Calkyl.21. The compound of any one of the preceding claims claim 2 , wherein Ris H.22. The compound of any one of the preceding claims claim 2 , wherein at most one of Rand Ris not H.23. The compound of any one of the preceding claims claim 2 , wherein Ris H or halo.24. The compound of any one of the preceding claims claim 2 , wherein Ris H.25. The compound of any one of the preceding claims claim 2 , wherein Ris C-Calkyl.26. The compound of any one of the preceding claims ...

LIGANDS SELECTIVE TO ALPHA 6 SUBUNIT-CONTAINING GABAA RECEPTORS AND THEIR METHODS OF USE

Provided herein are novel pyrazoloquinolinone compounds and method of using such compounds to treat disorders such as neuropsychiatric disorders with sensorimotor gating deficits, such as schizophrenia, tic disorders, attention deficit hyperactivity disorder, obsessive compulsive disorder, panic disorder, Huntington's disease and nocturnal enuresis; depression; temporomandibular myofascial pain; disorders of trigeminal nerve, such as trigeminal neuralgia and trigeminal neuropathy; migraine; and tinnitus. 3. A compound according to or , wherein at least one of R′ , R′ , R′ , R , R , R , R , R , Rand Ris a haloalkyl.4. The compound according to claim 3 , wherein the haloalkyl is CF.5. A compound according to any of the preceding claims wherein at least one of R′ claim 3 , R′ claim 3 , R′ claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , R claim 3 , Rand Ris Calkoxy.6. A compound according to claim 5 , wherein the Calkoxy is a methoxy.7. A compound according to claim 6 , wherein the Calkoxy is —OCD.8. A compound according to any of the preceding claims wherein at least one of R′ claim 6 , R′ claim 6 , R′ claim 6 , R claim 6 , R claim 6 , R claim 6 , and Ris a halogen.9. A compound according to wherein the halogen is bromine or chlorine.10. A compound according to any of the preceding claims wherein each X is C.11. A compound according to any of - wherein at least one X is N.12. A compound according to any of the preceding claims wherein R′is selected from H claim 8 , —OCHand —OCD.13. A compound according to any of the preceding claims wherein R′is selected from H claim 8 , —OCHand —OCD.14. A compound according to any of the preceding claims wherein Ris selected from H claim 8 , —OCHand —OCD.15. A compound according to any of the preceding claims wherein Ris selected from H claim 8 , halogen claim 8 , —OCHand —OCD.16. A compound according to any of the preceding claims wherein Ris selected from H or halogen.17. A compound according to any of the preceding claims ...

Pyrimidine-based antiproliferative agents

This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

Pyranopyridone inhibitors of tankyrase

There are provided compounds of the formula or a pharmaceutically acceptable salt thereof wherein X, M, Y, R 1 and R 2 are as defined herein. The compounds have activity as anticancer agents.

SUBSTITUTED METHYLFORMYL REAGENTS AND METHOD OF USING SAME TO MODIFY PHYSICOCHEMICAL AND/OR PHARMACOKINETIC PROPERTIES OF COMPOUNDS

The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent. 127.-. (canceled)29. A method according to claim 28 , wherein Y═R; or alternatively Y═Rand compound 1 claim 28 , is selected from the group comprising:i. chloromethyl isopropyl carbonate;ii. benzyl chloromethyl carbonate;iii. chloromethyl morpholinomethyl carbonate;iv. chloromethyl isobutyl carbonate;v. chloromethylmethyl carbonate;vi. (S)-sec-butyl chloromethyl carbonate;vii. (R)-sec-butyl chloromethyl carbonate;viii. chloromethyl((3S,5R)-3,5-dimethylmorpholino)methyl carbonate;ix. chloromethyl 2-methylcyclopropyl carbonate;x. chloromethyl2-methoxyethyl carbonate;xi. chloromethyl propyl carbonate;xii. chloromethyl cyclobutyl carbonate;xiii. chloromethyl cyclopropyl carbonate;xiv. chloromethyl 2,2-dimethylcyclobutyl carbonate;xv. chloromethyl cyclopentyl carbonate;xvi. chloromethyl oxetan-3-yl carbonate;xvii. (S)-chloromethyl tetrahydrofuran-3-yl carbonate;xviii. chloromethyl cyclohexylmethyl carbonate;xix. chloromethyl 3-methoxycyclohexyl carbonate;xx. (R)-chloromethyl tetrahydrofuran-3-yl carbonate;xxi. chloromethyl ethoxymethyl carbonate;xxii. chloromethyl oxepan-4-yl carbonate;xxiii. (1R,2S,4S)-bicyclo[2.2.1]heptan-2-yl chloromethyl carbonate;xxiv. chloromethyl 2,3-dihydro-1H-inden-1-yl carbonate;xxv. benzyl chloromethyl carbonate;xxvi. (S)-chloromethyl 1-phenylethyl carbonate;xxvii. chloromethyl cyclohexyl carbonate;xxviii. chloromethyl isobutyl carbonate;xxix. chloromethyl 4-methylcyclohexyl carbonate;xxx. chloromethyl 2-(methylthio)ethyl carbonate;xxxi. chloromethyl 3-methylcyclohexyl carbonate;xxxii. chloromethylpentan-2-yl carbonate;xxxiii. chloromethyl neopentyl carbonate;xxxiv. methyl 1-((chloromethoxy)carbonyloxy) ...

THERAPEUTIC THIOPHENE-, FURAN-, AND PYRIDINE-FUSED AZOLOPYRIMIDIN-5-(6H)-ONES

Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. Any and all priority claims identified in the Application Data Sheet, or any correction thereto, are hereby incorporated by reference under 37 CFR 1.57. For example, this application is a continuation of U.S. patent application Ser. No. 15/394,058, filed Dec. 29, 2016, which is a continuation of U.S. patent application Ser. No. 14/853,856, filed Sep. 14, 2015, which is a divisional of U.S. patent application Ser. No. 13/920,974, filed Jun. 18, 2013, which claims priority under 35 U.S.C. § 119(e) to U.S. Provisional Application No. 61/661,091, filed on Jun. 18, 2012; the disclosures of which are incorporated herein by reference in their entireties.The present invention relates to novel compounds, e.g., thiophene-, furan-, and pyridine-fused azolopyrimidin-5-(6 h)-one compounds, useful, e.g., as PDE1 inhibitors; methods of preparing such compounds; pharmaceutical compositions comprising such compounds; and the use of these compounds and compositions to treat one or more disorders, including neurological disorders, cardiovascular disorders, renal disorders, and other conditions and diseases involving PDE1 or cyclic nucleotide signaling.The cyclic nucleotides 5′-3′ cyclic adenosine monophosphate (cAMP) and 5′-3′ cyclic guanosine monophosphate (cGMP) are second messenger molecules, relaying signals from receptors on the cell surface to target molecules inside the cell. The cyclic nucleotide phosphodiesterases (PDEs) are a group of enzymes (which can be localized to different cellular compartments) that hydrolyze the phosphodiester bond of cyclic nucleotides and thereby inactivate their function. PDEs can therefore play important roles in signal transduction by modulating the localization, ...

TETRANDRINE FAMILY PHARMACEUTICAL FORMULATIONS AND METHOD

Drug formulations, methods and their use in treatment of diseases using formulations of pure di-acid salts of tetrandrine family members, especially d-tetrandrine di-hydrochloride, combined with a pharmaceutical diluent or carrier. 1. (canceled)2. (canceled)3. (canceled)4. (canceled)5. (canceled)6. (canceled)7. (canceled)8. (canceled)9. (canceled)10. (canceled)11. (canceled)12. (canceled)13. (canceled)15. The method of claim 14 , wherein the tetrandrine family member has the “S” isomeric configuration at the C-1′ chiral carbon location.16. The method of wherein the tetrandrine family member is the pure di-acid salt of d-tetrandrine.17. A method of treating ailments of claim 14 , in which said pharmaceutical composition is administered in conjunction with a principle drug used to treat such ailments.19. (canceled)20. (canceled)21. The method of in which said spray drier is set with a wall temperature of 240-400 C. claim 18 , and an atomizer set to feed the di-acid salt solution at a rate of 1-2 liters/minute.22. The method of in which said dilute acid solution is 5-20% molar hydrochloric acid.23. The method of in which said solution is filtered prior to spray drying to remove any residual solids. The present application claims the benefit of U.S. Provisional Patent Application No. 61/792,849, entitled TETRANDRINE FAMILY PHARMACEUTICAL FORMULATIONS AND METHOD, filed on Mar. 15, 2013, the entire contents of which are incorporated by reference.The present invention relates to pharmaceutical formulations of a family of bisbenzylisoquinoline alkaloids. The specific family is referred to herein as the “tetrandrine family.”The tetrandrine family bisbenzylisoquinolines have two nitrogen locations and hence can exist in the free base form or as a mono or di-acid salt. Because of the enhanced solubility of the salt form of pharmaceutical ingredients, the salt forms are used in formulating pharmaceutical compositions. The active ingredient thus solubilizes more quickly and ...

TETRANDRINE FAMILY PHARMACEUTICAL FORMULATIONS AND METHOD

Drug formulations, methods and their use in treatment of diseases using formulations of pure di-acid salts of tetrandrine family members, especially d-tetrandrine di-hydrochloride, combined with a pharmaceutical diluent or carrier. 2. The pharmaceutical formulation of claim 1 , wherein the tetrandrine family member has the “S” isomeric configuration at the C-1′ chiral carbon location.3. The pharmaceutical formulation of comprising: the pure di-acid salt of d-tetrandrine.4. The pharmaceutical formulation of wherein the pharmaceutical carrier comprises: a solution containing 0.20-0.30% carboxymethylcellulose.5. The pharmaceutical formulation of wherein the pharmaceutical carrier comprises: a pregelatinized starch carrier.6. The pharmaceutical formulation of also comprising: colloidal silicone dioxide claim 5 , sodium lauryl sulfate and magnesium stearate.7. (canceled)8. (canceled)9. (canceled)10. The pharmaceutical composition of wherein the di-acid salt of the tetrandrine family member is made by dissolving a purified member of the tetrandrine family in 2 molar equivalent solution of dilute acid claim 1 , and fed through a spray drier set with a wall temperature of 240-400 C claim 1 , and an atomizer set to feed the di-acid salt solution at a rate of 1-2 liters/minute.11. The pharmaceutical composition of wherein the dilute acid used is 5-20% molar hydrochloric acid.12. The pharmaceutical formulation of wherein the tetrandrine family member has the “S” isomeric configuration at the C-1′ chiral carbon location.13. The pharmaceutical formulation of wherein the tetrandrine family member comprises d-tetrandrine.14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. (canceled)21. The di-acid salt of in which said spray drier is set with a wall temperature of 240-400 C claim 20 , and an atomizer set to feed the di-acid salt solution at a rate of 1-2 liters/minute.22. The di-acid salt of in which said dilute acid solution is 5-20% molar hydrochloric acid.23. The di- ...

Organic electroluminescent materials and devices

The present invention includes a novel series of host materials for OLEDs based on substituted fused 1,2,4-triazines. The compounds of the invention may improve the device EQE and lifetime.

BLUE THERMALLY ACTIVATED DELAYED FLUORESCENT EMITTERS AND HOSTS BASED ON FUNCTIONALIZED IMIDAZOLYL GROUPS

Compounds of General Formula I may act as thermally activated delayed fluorescent emitters in organic electroluminescent devices. Compounds of General Formula I have donor and acceptor groups part of the same conjugated system. Devices incorporating compounds of General Formula I may have higher EQE and longer material lifetimes. 13. An organic light emitting diode comprising the compound of .14. An organic light emitting diode comprising the compound of .15. An organic light emitting diode comprising the compound of .16. An organic light emitting diode comprising the compound of .17. A light emitting device comprising the light emitting diode of .18. A light emitting device comprising the light emitting diode of .19. A light emitting device comprising the light emitting diode of .20. A light emitting device comprising the light emitting diode of . The present application claims priority to U.S. Provisional Application No. 63/075,924, filed: Sep. 9, 2020, which is incorporated by reference herein in its entirety.This invention was made with government support under DE-EE0008721 awarded by the Department of Energy. The government has certain rights in the invention.Opto-electronic devices that make use of organic materials are becoming increasingly desirable for a number of reasons. Many of the materials used to make such devices are relatively inexpensive, so organic opto-electronic devices have the potential for cost advantages over inorganic devices. In addition, the inherent properties of organic materials, such as their flexibility, may make them well suited for particular applications such as fabrication on a flexible substrate. Examples of organic opto-electronic devices include organic light emitting diodes (OLEDs), organic phototransistors, organic photovoltaic cells, and organic photodetectors. For OLEDs, the organic materials may have performance advantages over conventional materials. For example, the wavelength at which an organic emissive layer emits ...

4-PYRIDONE DERIVATIVE COMPOUNDS AND USES THEREOF AS HIV INTEGRASE INHIBITORS

The present invention relates to 4-Pyridone Compounds of Formula (I); and pharmaceutically acceptable salts and prodrugs thereof, wherein A, R, R, and Rare as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridone Compound, and methods of using the 4-Pyridone Compounds for treating or preventing HIV infection in a subject or the clinical manifestations thereof. 3. The compound of claim 2 , wherein up to 2 of R claim 2 , R claim 2 , R claim 2 , R claim 2 , and Rare independently selected from H and halo.5. The compound of claim 4 , wherein the definitions of R claim 4 , R claim 4 , and Rare selected from the group consisting of sets (a) to (c) as follows:{'sup': 5B', '5C', '5D, '(a) Ris H, Ris F, and Ris Cl;'}{'sup': 5B', '5C', '5D, '(b) Ris Cl, Ris F, and Ris H; and'}{'sup': 5B', '5C', '5D, '(c) Ris H, Ris F, and Ris H.'}6. The compound of claim 5 , wherein:{'sup': '2', 'sub': 2', '2', '3', '2', '2', '2, 'Ris selected from —C(O)NHCHCHOCHand —CHOH, —CHNH; and'}{'sup': '3', 'sub': 3', '2', '3', '2', '3, 'Ris selected from cyclopentenyl, cyclohexenyl, cyclopentyl, isopropyl, —C(CH)═CH, —CFand —CHCF.'}7. The compound of claim 5 , wherein Rand R claim 5 , together with the carbon atoms to which they are attached claim 5 , join to form a cyclic group Y.8. The compound of claim 5 , wherein Y is a 4- to 8-membered monocyclic heterocycloalkyl group that can be optionally substituted as set forth in .9. The compound of claim 5 , wherein Y is an 8- to 11-membered bicyclic heterocycloalkyl group that can be optionally substituted as set forth in .10. The compound of claim 5 , wherein Y is a 4- to 8-membered monocyclic heterocycloalkenyl group that can be optionally substituted as set forth in .11. The compound of claim 5 , wherein Y is or an 8- to 11-membered bicyclic heterocycloalkenyl group claim 5 , that can be optionally substituted as set forth in .14. A pharmaceutical composition comprising an effective amount of a compound ...

NOVEL TARGETING AGENTS FOR DIAGNOSTIC AND THERAPEUTIC INDICATIONS

The invention relates to compounds and use thereof in the diagnosis and/or in treatment of medical disorders. In some embodiments, the compounds may be used for detecting a cancer. The compound may include a di-acid moiety. In some embodiments the di-acid moiety comprises a di-carboxylic acid and in some embodiments the di-acid moiety comprises a di-tetrazole. 160-. (canceled)62. The compound according to claim 61 , wherein the leaving group is selected from halide claim 61 , sulfonate claim 61 , mesylate claim 61 , tosylate claim 61 , triflate claim 61 , nosylate claim 61 , brosylate or a phenyl substituted by a nitro or halogen.63. The compound according to claim 61 , which is further radiolabeled.64. The compound according to claim 63 , for use in X-ray claim 63 , CT scan claim 63 , magnetic resonance imaging (MRI) claim 63 , single photon emission tomography (SPECT) and positron emission tomography (PET).65. The compound according to claim 61 , radiolabeled with F.68. A compound represented by the structure in formula (VIII):{'br': None, 'R—O—X\u2003\u2003(VIII)'}{'claim-ref': {'@idref': 'CLM-00061', 'claim 61'}, 'wherein R stands for any of the compounds according to ; and'}X is a leaving group.69. The compound according to claim 68 , wherein X is a halide or a sulfonate.7170. The compound according to claim 68 , wherein X is a halogen or a sulfonate.72. A method for the selective detection of cells undergoing perturbations and alterations of their normal plasma membrane organization among a population of cells claim 61 , wherein the method comprises contacting the cell population with a compound according claim 61 , said method comprising the detection of the signal obtained from said cells by a suitable detector.73. A method for selective detection of cells undergoing cell death in the living body of a multi-cellular organism claim 61 , said method comprising administration to said organism adequate amounts of a compound according claim 61 , wherein said ...

Process for preparation of 2-amino-5-hydroxy propiophenone

The present invention relates to a process for preparation of 2-Amino-5-hydroxy propiophenone, a key intermediate for the synthesis of camptothecin analogs including 7-Ethyl-10-hydroxycamptothecin (SN-38).

TRICYCLIC ANTIBIOTICS

The present invention relates to antibacterial compounds of formula I: 142-. (canceled)44. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , whereinX1 represents a nitrogen atom andX2 represents a group CR2.45. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , whereinA1 represents —O— or —S—.46. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , wherein{'sub': '2', 'A2 represents —CH—.'}47. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , whereinA3 is a cyclohexylene group or saturated and unsaturated 4 to 6-membered heterocyclodiyl with 1 or 2 nitrogen atoms as heteroatoms.50. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , whereinn is 0.51. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , wherein{'sub': 1', '4, 'A4 is C-Calkylene or >C═O.'}52. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , wherein{'sub': r', '6, 'R1 is selected from the group consisting of halogen and C—Calkoxy.'}54. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , wherein{'sub': 1', '4', '2', '4, 'A4 represents C-Calkylene, —C(═O)— or a group —CHS— being linked to the adjacent NR5-group via the carbon atom;'}{'sub': 1', '6', '1', '6, 'R1 and R2 independently of one another, represent hydrogen or a substituent selected from hydroxy, halogen, cyano, C-Calkyl, or C-Calkoxy, in which substituents the alkyl moieties are unsubstituted; and'}n is 0 or 1.55. A compound according to or a pharmaceutically acceptable salt claim 43 , hydrate or solvate thereof claim 43 , whereinX1 represents a nitrogen atom and X2 ...

Methods and compositions for inhibiting human copper trafficking proteins atox1 and ccs

Compositions and methods concern organic molecules that bind to human Atox1 and CCS at the copper trafficking interface of these proteins. This binding suppresses copper trafficking, which leads to inhibition of cancer cell proliferation and tumor growth. In addition to serving as an effective treatment of cancer, these organic molecules inhibit cellular copper uptake and can be used as treatment of disorders of copper metabolism such as Wilson's disease, which is characterized by copper overload, as well as wound healing.

THERAPEUTIC THIOPHENE-, FURAN-, AND PYRIDINE-FUSED AZOLOPYRIMIDIN-5-(6H)-ONES

Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders. 2. (canceled)3. The compound of claim 1 , wherein one or more of R claim 1 , R claim 1 , R claim 1 , and Ris halomethyl.4. The compound of claim 1 , wherein Ris H claim 1 , and Ris C-Calkoxy; or Ris F claim 1 , Cl claim 1 , or Br claim 1 , and Ris —CFor —CHF.5. The compound of claim 1 , wherein A is S (sulfur); and X is N (nitrogen).6. (canceled)7. The compound of claim 1 , wherein Ris C-Calkyl; and Ris H claim 1 , or Ris C-Calkyl; and Ris —(CRR)NRR.9. (canceled)10. The compound of claim 8 , wherein one or more of R claim 8 , R claim 8 , R claim 8 , and Ris halomethyl.11. The compound of claim 8 , wherein Ris H claim 8 , and Ris —C-Calkoxy; or Ris F claim 8 , Cl claim 8 , or Br claim 8 , and Ris —CFor —CHF.12. The compound of claim 8 , wherein A is S (sulfur); X is N (nitrogen); Ris F claim 8 , Cl claim 8 , or Br; and Ris —C-Calkoxy.13. (canceled)14. The compound of claim 8 , wherein{'sup': 3', '4, 'sub': 1', '3, 'Ris —C-Calkyl; and Ris H, or'}{'sup': 3', '4', '10', '11', '12', '13, 'sub': 1', '3', '0-3, 'Ris —C-Calkyl; and Ris —(CRR)NRR.'}16. The compound of claim 15 , wherein Ris H claim 15 , and Ris C-Calkoxy; or Ris F claim 15 , Cl claim 15 , or Br claim 15 , and Ris —CFor —CHF.17. The compound of claim 16 , wherein A is S (sulfur); and X is N (nitrogen).18. (canceled)19. The compound of claim 16 , wherein Ris —C-Calkyl; and Ris —(CRR)NRR.21. (canceled)22. The compound of claim 20 , wherein Ris H claim 20 , and Ris C-Calkoxy; or Ris F claim 20 , Cl claim 20 , or Br claim 20 , and Ris —CFor —CHF.23. The compound of claim 22 , wherein A is S (sulfur); and X is N (nitrogen).24. (canceled)25. The compound of claim 22 , wherein Ris C-Calkyl; and Ris —(CRR)NRR.26. A compound selected ...

TRICYCLIC P13K INHIBITOR COMPOUNDS AND METHODS OF USE

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. 5. The compound of wherein Ris phenyl substituted with one or more groups selected from F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —CH claim 1 , —CHCH claim 1 , —CH(CH) claim 1 , —CN claim 1 , —CF claim 1 , —CHOH claim 1 , —COH claim 1 , —CONH claim 1 , —CONH(CH) claim 1 , —CON(CH) claim 1 , —NO claim 1 , —NH claim 1 , —NHCH claim 1 , —NHCOCH claim 1 , —OH claim 1 , —OCH claim 1 , —OCHCH claim 1 , —OCH(CH) claim 1 , —SH claim 1 , —NHC(═O)NHCH claim 1 , —NHC(═O)NHCHCH claim 1 , —NHS(O)CH claim 1 , —N(CH)C(═O)OC(CH) claim 1 , and —S(O)CH.6. The compound of wherein Ris an optionally substituted bicyclic heteroaryl group selected from 1H-indazole claim 1 , 1H-indole claim 1 , indolin-2-one claim 1 , 1-(indolin-1-yl)ethanone claim 1 , 1H-benzo[d][1 claim 1 ,2 claim 1 ,3]triazole claim 1 , 1H-pyrazolo[3 claim 1 ,4-b]pyridine claim 1 , 1H-pyrazolo[3 claim 1 ,4-d]pyrimidine claim 1 , 1H-benzo[d]imidazole claim 1 , 1H-benzo[d]imidazol-2(3H)-one claim 1 , 1H-pyrazolo[3 claim 1 ,4-c]pyridine claim 1 , 1H-pyrrolo[2 claim 1 ,3-c]pyridine claim 1 , 3H-imidazo[4 claim 1 ,5-c]pyridine claim 1 , 7H-pyrrolo[2 claim 1 ,3-d]pyrimidine claim 1 , 7H-purine claim 1 , 1H-pyrazolo[4 claim 1 ,3-d]pyrimidine claim 1 , 5H-pyrrolo[3 claim 1 ,2-d]pyrimidine claim 1 , 2-amino-1H-purin-6(9H)-one claim 1 , quinoline claim 1 , quinazoline claim 1 , quinoxaline claim 1 , isoquinoline claim 1 , isoquinolin-1(2H)-one claim 1 , 3 claim 1 ,4-dihydroisoquinolin-1(2H)-one claim 1 , 3 claim 1 ,4-dihydroquinolin-2(1H)-one claim 1 , quinazolin-2(1H)-one claim 1 , quinoxalin-2( ...

Berbamine derivatives

The invention provides novel berbamine derivatives, and compositions or pharmaceutical compositions thereof. These berbamine derivatives have shown higher potency in killing cancer/tumor cells comparing to berbamine, and can be used in cancer/tumor treatments.

Benzimidazoles and Methods of Using Same

The present disclosure is concerned with benzimidazole compounds and methods of using these compounds for the treatment of hepatitis (e.g., hepatitis C), RNA virus infections (e.g., Zika virus, dengue virus, Powassan virus, Chikungunya virus, Enterovirus, respiratory syntactical virus (RSV), Rift Valley fever, Influenza virus, Tacaribe virus, Mayaro virus, West Nile virus, yellow fever virus, and coronavirus), and disorders of uncontrolled cellular proliferation (e.g., cancer). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

FUNCTIONALIZED HETEROCYCLES AS ANTIVIRAL AGENTS

The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: 2. The compound of claim 1 , wherein A is optionally substituted 5- to 7-membered unsaturated heterocyclic claim 1 , or optionally substituted 5- to 6-membered heteroaryl.7. A pharmaceutical composition claim 1 , comprising a compound according to claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with a pharmaceutically acceptable carrier or excipient.8. A method of treating or preventing an HBV infection in a subject in need thereof claim 1 , comprising administering to the subject a therapeutically effective amount of a compound or a combination of compounds according to .9. The method of claim 8 , further comprising administering to the subject an additional therapeutic agent selected from the group consisting of a HBV polymerase inhibitor claim 8 , interferon claim 8 , viral entry inhibitor claim 8 , viral maturation inhibitor claim 8 , literature-described capsid assembly modulator claim 8 , reverse transcriptase inhibitor claim 8 , TLR-agonist claim 8 , inducer of cellular viral RNA sensor claim 8 , therapeutic vaccine claim 8 , and agents of distinct or unknown mechanism.10. The method of claim 9 , wherein the compound and the additional therapeutic agent are co-formulated.11. The method of claim 9 , wherein the compound and the additional therapeutic agent are co-administered.12. The method of claim 9 , wherein the additional therapeutic agent is administered at a lower dose or frequency compared to the dose or frequency of the additional therapeutic agent that is required to treat an HBV infection when administered alone.13. The method of claim 9 , wherein the subject is refractory to at least one compound selected from the group consisting of a HBV polymerase inhibitor claim 9 , interferon claim 9 , viral entry inhibitor claim 9 , viral maturation inhibitor claim 9 , distinct capsid assembly modulator claim 9 , inducer of ...

4-AZAPODOPHYLOTOXINS COMPOUNDS

The present disclosure relates to 4-azapodophylotoxins compounds, pharmaceutical compositions comprising such compounds, kits, and methods for using such compounds or pharmaceutical compositions. 2. (canceled)4. (canceled)5. The compound of claim 1 , wherein Ris (C-C)alkyl claim 1 , wherein the alkyl is unsubstituted or substituted with a substituent selected from OR claim 1 , NRR claim 1 , (5- or 6-membered)heterocyclic ring comprising one or two heteroatoms selected from N claim 1 , O and S claim 1 , (C-C)cycloalkyl claim 1 , (C-C)aryl claim 1 , (5- or 6-membered)heteroaryl comprising one claim 1 , two or three heteroatoms selected from N claim 1 , O and S claim 1 , or a Linker Unit.611.-. (canceled)12. The compound of claim 1 , wherein Ris selected from H or (C-C)alkoxy.1316.-. (canceled)17. The compound of claim 1 , wherein Ris selected from H claim 1 , (C-C)alkoxy and hydroxyl.1821.-. (canceled)22. The compound of claim 1 , wherein Ris selected from (C-C)alkoxy claim 1 , halo claim 1 , hydroxyl claim 1 , O-Protecting Group claim 1 , and O-Linker Unit.2327.-. (canceled)28. The compound of claim 1 , wherein Ris H.29. The compound of claim 1 , wherein Rand Rare taken together with the carbons to which they are attached to form a 1 claim 1 ,3-dioxolo ring.30. The compound of claim 1 , wherein Ris H or (C-C)alkoxy.3133.-. (canceled)34. The compound of claim 1 , wherein Ris (C-C)alkoxy.35. (canceled)36. The compound of claim 1 , wherein Ris (C-C)alkoxy.37. (canceled)38. The compound of claim 1 , wherein Rand Rare taken together with the carbons to which they are attached to form a 1 claim 1 ,3-dioxolo ring.40. The compound of claim 39 , wherein Ris (C-C)alkoxy.4142.-. (canceled)43. The compound of claim 39 , wherein Ris (C-C)alkoxy.4445.-. (canceled)46. The compound of claim 39 , wherein Ris (C-C)alkoxy.4750.-. (canceled)51. The compound of claim 39 , wherein Rand Rare taken together with the carbons to which they are attached to form a 1 claim 39 ,3-dioxolo ring.52. ...

USE OF PHYSIOLOGICAL COOLING ACTIVE INGREDIENTS, AND AGENTS CONTAINING SUCH ACTIVE INGREDIENTS

The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane. 2. The method according to claim 1 , wherein the receptor is brought into contact with one or more compounds of formula (I).3. The method according to claim 1 , wherein the receptor is brought into contact with one or more compounds of formula (II).4. The method according to claim 1 , wherein the receptor is brought into contact with at least one compound which claim 1 , in an in vitro cellular activity test using cells which recombinantly express the human TRPM8 receptor claim 1 , modulate the permeability of these cells for Ca ions.5. The method according to claim 1 , wherein the modulating compound has an agonistic or antagonistic effect on the cellular Ca2+ ion permeability.6. The method according to claim 1 , wherein the modulating compound is a TRPM8 receptor agonist.7. A method for inducing a sensation of coldness in a human and/or an animal comprising contacting a human and/or animal with one or more compounds of formula (I) or formula (II) as defined in .8. A pharmaceutical composition comprising one or more compounds of formula (I) or formula (II) as defined in .9. A method for treating prostate carcinomas claim 1 , bladder weakness claim 1 , or pain comprising contacting a patient with one or more compounds of formula (I) or formula (II) as defined in .10. A method for inducing a sensation of coldness to packaging comprising adding one or more compounds of formula (I) or formula (II) as defined in to the packaging.11. A method for inducing a sensation of coldness to a textile comprising adding one or more compounds of formula (I) or formula (II) as defined in to the textile.13. An agent comprising one or more compounds of formula (I) or formula (II) as defined in .14. The agent according to selected from the group consisting of:a) pharmaceutical compositions;b) foods;c) mouth care compositions;d) body care compositions; ande) foams or gels.16. An ...

PYRIDO-/AZEPINO-BENZOFURAN AND PYRIDO-/AZEPINO-BENZOTHIOPHENE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USE THEREOF

Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described. 2. The compound according to claim 1 , wherein G is —NR—CRR—.3. The compound according to claim 1 , wherein G is —CRR—NR—.4. The compound according to claim 1 , wherein G is —NR—CRR—CRR—.5. The compound according to claim 1 , wherein G is —CRR—NR—CRR—.6. The compound according to claim 1 , wherein G is —CRR—CRR—NR—.7. The compound according to claim 1 , wherein Rto Rare each independently selected from the group consisting of H and optionally substituted C-Calkyl.8. The compound according to claim 1 , wherein Ris H claim 1 , halogen claim 1 , or optionally substituted C-Calkyl.9. The compound according to claim 1 , wherein Ris H claim 1 , halogen claim 1 , or optionally substituted C-Calkyl.10. The compound according to claim 1 , wherein Ris H or C-Calkyl and R-Rare H.11. The compound according to claim 1 , wherein Rand one of R claim 1 , R claim 1 , R claim 1 , and Rcombine to form a 3- to 7-membered heterocycle.12. The compound according to claim 1 , wherein any one of R claim 1 , R claim 1 , R claim 1 , or Rcombine with any one of R claim 1 , R claim 1 , R claim 1 , or Rto form —(CH)— and r is from 1 to 4.13. The compound according to claim 1 , wherein Ris H or C-Calkyl.14. The compound according to claim 1 , wherein Ris —C(O)R.15. The compound according to claim 1 , wherein Z is O.16. The compound according to claim 1 , wherein Z is S.17. The compound according to claim 1 , wherein X is N claim 1 , CH claim 1 , or CH.18. The compound according to claim 1 , wherein Y is N or C.19. The compound according to claim 1 , wherein L is a bond.20. The compound according to claim 1 , wherein L is —CH—O—.21. The compound according to claim 1 , wherein L is —CH—CH—.22. The compound according to claim 1 , ...

METABOTROPHIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS USE THEREOF

Compounds that modulate GluR5 activity and methods of using the same are disclosed. 120-. (canceled) This application claims priority to U.S. Provisional Patent Application No. 61/494,731, filed Jun. 8, 2011. The entire contents of the foregoing application are hereby incorporated by reference.The amino acid L-glutamate (which herein is referred to simply as glutamate) is the principal excitatory neurotransmitter in the brain and other elements of the central nervous system of mammals. Glutamate binds to neurons and activates cell surface receptors. Glutamate has significant roles in motor control, cognitive function, sensory perception, and acts as a mediator of persistent changes in the strength of synaptic signaling (synaptic plasticity), thereby modulating long term potentiation (LTP) and long term depression (LTD), which form the basis of learning and memory. Many neurological and neuropsychiatric disorders, including, but not limited to, psychosis spectrum disorders, schizophrenia and other cognitive deficits, are associated with aberrations in the function of (or the regulation by, or the regulation of) glutamate signaling systems.Glutamate mediates its effect via two distinct types of receptors, the ionotropic receptors and the metabotropic receptors. The family of the metabotropic receptors (mGlu or mGluR) consists of eight different subtypes, which are further classified into three subgroups based on sequence homology, effector coupling and pharmacology. In particular, group I mGlu receptors (mGluR1 and mGluR5) are positively coupled to phospholipase C, while group II mGlu receptors (mGluR2 and mGluR3) and group III receptors (mGluR4, mGluR6, mGluR7, and mGluR8) are negatively coupled to adenylate cyclase (Conn et al. 1997; 37:205-37).mGluR5, which is widely expressed in the central nervous system, has at least two discrete allosteric binding sites, in addition to the orthosteric site, and has been implicated in a range of physiological functions, ...

CEPHALOTAXUS ESTERS, METHODS OF SYNTHESIS, AND USES THEREOF

The present invention provides novel esters, syntheses thereof, and intermediates thereto. The invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of using said compounds or compositions in the treatment of proliferative diseases (e.g., benign neoplasm, cancer, inflammatory disease, autoimmune disease, diabetic retinopathy) and infectious disease. The invention further provides methods of using said compounds or compositions in the treatment of multidrug resistant cancer. 269-. (canceled)70. The compound of claim 1 , wherein neither Rnor Ris hydrogen.71. The compound of claim 1 , wherein Ris taken together with Rto form an optionally substituted claim 1 , saturated or unsaturated 3-7-membered ring having 0-2 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , or sulfur.72. The compound of wherein Ris —(CH)COR.73. The compound of claim 72 , wherein n is 1 claim 72 , and Ris methyl.74. The compound of claim 72 , wherein Ris —CHF.76. The compound of claim 1 , wherein Ris —OR.77. The compound of claim 76 , wherein R is H.78. The compound of claim 1 , wherein Ris -T-R claim 1 , wherein:{'sub': '1-12', 'T is a covalent bond or a bivalent Csaturated or unsaturated, straight or branched, hydrocarbon chain, wherein one or two methylene units of T are optionally and independently replaced by —O—, —S—, or —N(R)—; and'}{'sup': 'z', 'sub': 2', '3', '1-6, 'Ris hydrogen, halogen, a monosaccharide, a disaccharide, —OR, —SR, —NR, —N, or an optionally substituted group selected from acyl, arylalkyl, heteroarylalkyl, Caliphatic, 6-10-membered aryl, 5-10-membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, 4-7-membered heterocyclyl having 1-2 heteroatoms independently selected from nitrogen, oxygen or sulfur.'}81. The compound of claim 1 , wherein both Rand Rare hydrogen.82. The compound of claim 1 , wherein Ris hydrogen or —OCOR.84. A pharmaceutical ...

Use of physiological cooling active ingredients, and agents containing such active ingredients

The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.

Indole ahr inhibitors and uses thereof

The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.

TRICYCLIC AND TETRACYCLIC SYSTEMS ACTING UPON THE VASCULAR AND CENTRAL NERVOUS SYSTEMS

Tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine, and pyrimidodiazepine fused with 1,4-dihydropyridine derivatives are disclosed. The present derivatives can be obtained from derivatives containing a dihydropyrldine ring reacting with compounds of the ortho-phenyldiamine, ortho-diaminopyridine, and ortho-diaminopyrimidine type, as well as some subsequent transformations and, tricyclic and tetracyclic derivatives can be obtained with a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, having a substituted or unsubstituted ring of benzene, pyridine or pyrimidine. The present derivatives exhibit vascular and central nervous system therapeutic activity. 117-. (canceled)19. The pharmaceutical composition according to wherein R is an unsubstituted or substituted phenyl group.20. The pharmaceutical composition according to wherein Ris —OR.21. The pharmaceutical composition according to wherein R′ is a straight or branched alkyl group having 1 to 24 carbon atoms.22. The pharmaceutical composition according to wherein Rrepresents an alkyl.23. The pharmaceutical composition according to wherein A is a benezene substituted with NO. This application is a continuation-in-part of U.S. 371 National Phase Patent Application Ser. No. 13/500,983, Filed Apr. 9, 2012, and claims priority to PCT Application No. PCT/CU2010/000004; Filed, Oct. 8, 2010; PCT Publication No. WO2011/041,989, Published Apr. 14, 2011; PCT Application No. PCT/CU2009/000172, Filed Oct. 9, 2009, which applications and publication are incorporated herein in their entireties by reference thereto.The invention relates to tricyclic and tetracyclic derivatives of a diazepine or diazepinone. The invention also relates to compounds having vascular and central nervous system therapeutic activity, and more specifically, calcium channel blocking activity.EP1593683 and EP1157992 describe the process of obtaining molecules derived from dihydro-2,3-benzodiazepine as potential ...

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

A compound of formula I: 3. The method according to claim 1 , wherein Ris morpholine.4. The method according to claim 1 , wherein W is O or S.5. The method according to claim 1 , wherein W is O.6. The method compound according to claim 1 , wherein X is CH.7. The method according to claim 1 , wherein Ris H.8. The method compound according to claim 1 , wherein L is C-Calkylene.9. The method according to claim 1 , wherein Y contains one or two heteroatoms.10. (canceled)11. The method according to claim 1 , wherein A is O or C-Calkylene.12. The method compound according to claim 1 , wherein W at Y is O or CH.1421.-. (canceled)22. The method of claim 1 , wherein L is methylene.23. The method of claim 1 , wherein Y contains two heteroatoms.24. The method of claim 1 , wherein A is methylene.25. The method of claim 1 , wherein W at Y is O.26. The method of claim 1 , wherein the leukemia is chronic myelogenous leukemia or acute myeloid leukemia.27. The method of claim 1 , wherein the PTEN-negative tumor is selected from the group consisting of PTEN-negative haematological claim 1 , breast claim 1 , lung claim 1 , endometrial claim 1 , skin claim 1 , brain and prostate cancer This application is a national stage filing under 35 U.S.C. § 371 of PCT/GB2015/050396, filed Feb. 12, 2015, which claims priority to Patent Application No. GB1402431.9, filed Feb. 12, 2014, the entire disclosure of each of which is incorporated by reference herein.The present invention relates to novel compounds which act as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, for the treatment of cancer, immune and inflammatory diseases.The phosphoinositide 3-kinases (PI3Ks) constitute a family of lipid kinases involved in the regulation of a network of signal transduction pathways that control a range of cellular processes. PI3Ks are classified into three distinct subfamilies, named class I, II, and III based upon their substrate specificities. Class IA PI3Ks possess a p110α, p110 ...

Condensed cyclic compound and organic light-emitting device including the same

A condensed cyclic compound and an organic light-emitting device including the same are provided. The organic light-emitting device includes a first electrode, a second electrode, and an organic layer disposed between the first electrode and the second electrode. The organic layer includes the condensed cyclic compound represented by Formula 1: in Formula 1, A 11 is a C 1 -C 60 heterocyclic group, A 12 is a C 5 -C 60 carbocyclic group or a C 1 -C 60 heterocyclic group, X 11 is O or S, X 12 is C, X 13 is selected from N, C, and C(R 13 ), X 14 is selected from N, C, and C(R 14 ), and X 13 and X 14 are linked via a single bond or a double bond.

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable sail thereof, wherein: W is O, N—H, N—(C-Calkyl) or S; each X is independently CH or N; Ris a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; Ris (LQ)Y; and each Ris independently H, C-Calkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy. 2. The compound of claim 1 , wherein both of the Rgroups that are attached to the 6 claim 1 ,5-ring system in formula I are H.3. The compound of claim 1 , wherein Q is a heterocyclic linker and Y is selected from the group consisting of H claim 1 , C-Calkyl claim 1 , and —OC-Calkyl.4. The compound of claim 1 , wherein Q is NR claim 1 , and Y is heterocycle.5. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient.7. The compound of claim 6 , wherein L is Calkylene.8. The compound of claim 7 , wherein m is 1.9. The compound of claim 6 , wherein Y is selected from the group consisting of H claim 6 , Calkyl claim 6 , Ccycloalkyl claim 6 , and —OR.10. The compound of claim 9 , wherein Q is selected from —NR— and —NRR—.11. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable excipient. The present invention relates to novel compounds which act as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, for the treatment of cancer, immune and inflammatory diseases.The phosphoinositide 3-kinases (PI3Ks) constitute a family of lipid kinases involved in the regulation of a network of signal transduction pathways that control a range of cellular processes. PI3Ks are classified into three distinct subfamilies, named class I, II, and III based upon their substrate specificities. Class IA PI3Ks possess a p110α, p110β, or p110δ catalytic subunit complexed with one of three regulatory subunits, p85α, p85β or p55δ. Class IA PI3Ks are activated by ...

FOURTH-GENERATION EGFR TYROSINE KINASE INHIBITOR

Provided is a compound having a tyrosine kinase inhibitory activity specific to C797S resistant mutant EGFR (particularly C797S tertiary-resistant mutant EGFR) and is useful as a C797S resistant mutant EGFR (particularly C797S mutant tertiary-resistant EGFR) specific tyrosine kinase inhibitor, an agent for preventing and/or treating non-small cell lung cancer with resistance mutant EGFR and the like, and the like. 4. The method of claim 3 , wherein the non-small cell lung cancer is associated with C797S resistant mutant EGFR. The present invention relates to a compound having an EGFR tyrosine kinase inhibitory activity and an EGFR tyrosine kinase inhibitor containing the compound.80% of lung cancer is non-small cell lung cancer, and gene mutation of epidermal growth factor receptor (EGFR) is observed in 20-30% of the non-small cell lung cancer. The major mutation is the L858R mutation or exon 19 deletion in the EGFR kinase domain. This mutation constantly activates transmission of cell proliferation signal from EGFR to the nucleus and causes canceration of the cells. Tyrosine kinase inhibitors (first-generation EGFR-TKI) such as Gefitinib (1) and Erlotinib (2) show remarkable antitumor effects for non-small cell lung cancer having such activating mutation EGFR (L858R or exon 19 deletion). On the other hand, if these drugs are continuously used, secondary-resistant mutation (T790M) occurs in EGFR in about one year in many cases and cancer relapses (non-patent document 1). To deal with this resistant mutation, an irreversible inhibitor Afatinib (3) (second-generation EGFR-TKI) in which Michael receptor is incorporated into the skeleton of Gefitinib (1) was developed (non-patent document 2). However, this drug strongly inhibits not only T790M secondary-resistant mutant EGFR but also wild-type EGFR (WT) which is present in normal cells. Therefore, the blood concentration of the drug cannot be sufficiently increased, and a sufficient therapeutic effect has not been shown ...

POLYCYCLICCARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): 29-. (canceled)10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen or CHF.1159-. (canceled)60. A pharmaceutical composition comprising a compound of or claim 1 , or pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable excipient.61. The pharmaceutical composition of further comprising one or more additional therapeutic agents.62. The pharmaceutical composition of wherein the one or more additional therapeutic agents is an anti-HIV agent.63. The pharmaceutical composition of wherein the one or more additional therapeutic agents is selected from the group consisting of HIV protease inhibitors claim 62 , HIV non-nucleoside inhibitors of reverse transcriptase claim 62 , HIV nucleoside or nucleotide inhibitors of reverse transcriptase claim 62 , and combinations thereof.64. The pharmaceutical composition of claim 60 , further comprising a first additional therapeutic agent selected from the group consisting of: abacavir sulfate claim 60 , tenofovir claim 60 , tenofovir disoproxil fumarate claim 60 , tenofovir alafenamide claim 60 , and tenofovir alafenamide hemifumarate and a second additional therapeutic agent selected from the group consisting of emtricitabine and lamivudine.65. A method of treating an HIV infection in a human having or at risk of having the infection by administering to the human a therapeutically effective amount of a compound of any one of or .66. The method of further comprising administering to the human a therapeutically effective amount of one or more additional therapeutic agents.67. The method of wherein the one or more additional therapeutic agents is an anti-HIV agent.68. The method of wherein the one or more additional therapeutic agents is selected from the group consisting of HIV protease inhibitors claim 67 , ...

Organic electroluminescence device and compound for organic electroluminescence device

An organic electroluminescence device including a first electrode, a second electrode, and an emission layer between the first electrode and the second electrode, wherein the emission layer includes a compound represented by Formula 1 to achieve high efficiency and an improved efficiency drop in a deep blue emission wavelength region:

TRICYCLIC HETEROCYCLIC COMPOUNDS USEFUL AS INHIBITORS OF TNF

Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: —(CR3R3)2-5-, —(CR3R3)x-Y—(CR3R3)y-, —Y—(CR3R3)2-3-Y—, —CR3R3-Y—(CR3R3)2-Y—, —Y—(CR3R3)2-Y—CR3R3-; and Y, R1, R2, R3, R5, R6, R8, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases. 2. The compound according to or a salt thereof claim 1 , wherein:{'sub': 3', '3', '2', '3', '3', '3', '3, 'W is —(CRR)—, —Y—CRR—, or —CRR—Y—.'}3. The compound according to or a salt thereof claim 1 , wherein:{'sub': 3', '3', '3', '3', '3', '2', '3', '3', '3', '3', '3', '3', '2, 'W is —(CRR)—, —Y—(CRR)—, —CRR—Y—CRR—, or —(CRR)—Y—.'}4. The compound according to or a salt thereof claim 1 , wherein:{'sub': 3', '3', '4', '3', '3', '3', '3', '3', '3', '3', '2', '3', '3', '2', '3', '3', '3', '3', '3', '3', '3', '2, 'W is —(CRR)—, —Y—(CRR)—, —CRR—Y—(CRR)—, —(CRR)—Y—CRR—, —(CRR)—Y—, or —Y—(CRR)—Y—.'}5. The compound according to or a salt thereof claim 1 , wherein:{'sub': 3', '3', '5', '3', '3', '4', '3', '3', '3', '3', '3', '3', '3', '2', '3', '3', '2', '3', '3', '3', '3', '3', '3', '3', '4', '3', '3', '3', '3', '3', '3', '3', '2', '3', '3', '2', '3', '3, 'W is —(CRR)—, —Y—(CRR)—, —CRR—Y—(CRR)—, —(CRR)—Y—(CRR)—, —(CRR)—Y—CRR—, —(CRR)—Y—, —Y—(CRR)—Y—, —CRR—Y—(CRR)—Y—, or —Y—(CRR)—Y—CRR—.'}6. The compound according to or a salt thereof claim 1 , wherein each Ris independently H claim 1 , F claim 1 , —OH claim 1 , —CH claim 1 , —CF claim 1 , or pyridinyl.7. The compound according to or a salt thereof claim 1 , wherein:{'sub': 2', '2', '2', '2', '2', '3', '2', '2', '2', '2', '2', '2, 'W is —CHCH—, —CHCHO—, —CH(OH)CHO—, —C(CH)(OH)CHO—, —C(OH)(pyridinyl)CHO—, —CHCHNH—, —CHFCHNH—, or —CH(OH)CHNH—;'}{'sub': 1', '3', '3', '2', '2', '3', '2', '3', '2', '3', '3', '2', '3', '3', '2', '3', '2', '2', '3', '3', '2', '2', '3', '3', '2', '3', '2', '2 ...

NOVEL SUBSTITUTED PYRAZOLO-PIPERAZINES AS CASEIN KINASE 1 D/E INHIBITORS

The invention provides compounds of Formula (I): 3. The compound according to claim 2 , wherein:{'sub': 1', '4', '5, 'Ris independently selected from aryl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, furyl, thienyl, imidazolyl, thiazolyl, indolyl, oxazolyl, isoxazolyl, pyrazolyl, triazolyl, tetrazolyl, indazolyl, 1,2,4-thiadiazolyl, isothiazolyl, quinolinyl, isoquinolinyl, each substituted with 1-4 Rand R;'}{'sub': 4', '1-4', 'e, 'R, at each occurrence, is independently selected from H and Calkyl substituted with 0-3 R;'}{'sub': 5', '1-4', 'e, 'claim-text': [{'sub': 2', 'b', 'p', 'c', 'b', '2', 'r', 'b', '2', 'r', 'a', 'a', '2', 'r', 'a', 'a', '2', 'r', 'b', '2', 'r', 'b', '2', 'r', 'a', 'a', '2', 'r', 'a', 'a', '2', 'r', 'b', '2', 'r', '2', 'a', 'a', '2', 'r', '2', 'a', 'a', '2', 'r', '2', 'c', '2', 'r', 'e, 'NO, —OR, —S(O)R, —CN, —OR, —(CH)C(═O)R, —(CH)NRR, —(CH)C(═O)NRR, —(CH)NHC(═O)R, —(CH)NHC(═O)OR, —(CH)OC(═O)NRR, —(CH)NHC(═O)NRR, —(CH)C(═O)OR, —(CH)S(O)NRR, —(CH)NHS(O)NRR, —(CH)NHS(O)R, (CH)-carbocyclyl substituted with 0-3 R,'}, {'sub': 2', 'r', 'e, 'and —(CH)-heterocyclyl substituted with 0-3 R;'}], 'R, at each occurrence, is independently selected from H, Calkyl substituted with 0-3 R, F, Cl, Br, ═O, CN,'}{'sub': a', '1-6', 'e', '2-6', 'e', '2-6', 'e', '2', 'r', '3-10', 'e', '2', 'r', 'e', 'a', 'a', 'e, 'R, at each occurrence, is independently selected from H, CN, Calkyl substituted with 0-5 R, Calkenyl substituted with 0-5 R, Calkynyl substituted with 0-5 R, —(CH)—Ccarbocyclyl substituted with 0-5 R, and —(CH)-heterocyclyl substituted with 0-5 R; or Rand Rtogether with the nitrogen atom to which they are both attached form a heterocyclic ring substituted with 0-5 R;'}{'sub': b', '1-6', 'e', '2-6', 'e', '2-6', 'e', '2', 'r', '3-10', 'e', '2', 'r', 'e, 'R, at each occurrence, is independently selected from H, Calkyl substituted with 0-5 R, Calkenyl substituted with 0-5 R, Calkynyl substituted with 0-5 R, —(CH)—Ccarbocyclyl substituted with 0-5 ...

POLYCYCLICCARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE

Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (Ia): 142-. (canceled)46. (canceled)47. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris selected from the group consisting of H , Calkyl , Chaloalkyl , and Ccycloalkyl.48. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris selected from the group consisting of hydrogen , methyl , ethyl , propyl , isopropyl , CHCF , CHCHFand cyclopropyl.49. The compound of any one of - , or a pharmaceutically acceptable salt thereof , wherein Ris ethyl.50. The compound of any of - , or a pharmaceutically acceptable salt thereof , wherein Ris selected from the group consisting of Chaloalkyl and Ccycloalkyl.51. The compound of claim 50 , or a pharmaceutically acceptable salt thereof claim 50 , wherein Ris selected from the group consisting of CHCF claim 50 , CHCHFand cyclopropyl.5259-. (canceled)60. A pharmaceutical composition comprising a compound of any one of - claim 50 , or pharmaceutically acceptable salt thereof claim 50 , and a pharmaceutically acceptable excipient.61. The pharmaceutical composition of further comprising one or more additional therapeutic agents.62. The pharmaceutical composition of wherein the one or more additional therapeutic agents is an anti-HIV agent.63. The pharmaceutical composition of wherein the one or more additional therapeutic agents is selected from the group consisting of HIV protease inhibitors claim 61 , HIV non-nucleoside inhibitors of reverse transcriptase claim 61 , HIV nucleoside or nucleotide inhibitors of reverse transcriptase claim 61 , and combinations thereof.64. The pharmaceutical composition of claim 60 , further comprising a first additional therapeutic agent selected from the group consisting of: abacavir sulfate claim 60 , tenofovir claim 60 , tenofovir disoproxil fumarate claim 60 , tenofovir alafenamide claim ...

COMPOUND, ORGANIC ELECTROLUMINESCENT DEVICE, AND DISPLAY DEVICE

Disclosed is a compound applicable to an electron transport layer, an electron transport assisting layer, a light emitting layer (n-type) of an organic electroluminescent device, an organic electroluminescent device in which said compound is used, and an organic EL display device including the organic electroluminescent device. The organic electroluminescent device includes: a first electrode; a second electrode facing the first electrode; and an organic material layer interposed between the first electrode and the second electrode and includes the compound. 25-. (canceled)7. An organic electroluminescent device comprising:a first electrode;a second electrode facing the first electrode; andan organic material layer interposed between the first electrode and the second electrode, wherein the organic material layer comprises the compound of chemical formula 1.8. The organic electroluminescent device of claim 7 , wherein the first electrode is an anode claim 7 , the second electrode is a cathode claim 7 , andwherein the organic material layer comprises i) a light emitting layer, ii) a hole transport region interposed between the first electrode and the light emitting layer and including at least one of a hole injection layer, a hole transport layer, and a hole transport assisting layer, and iii) an electron transport region interposed between the light emitting layer and the second electrode and including at least one of an electron transport assisting layer, an electron transport layer and an electron injection layer.9. The organic electroluminescent device of claim 8 , wherein claim 8 , the electron transport region comprises the compound of chemical formula 1.10. The organic electroluminescent device of claim 9 , wherein the electron transport layer or the electron transport assisting layer of the organic electroluminescent device comprises the compound of chemical formula 1.11. A display device including the organic electroluminescent device of claim 7 , wherein ...

Acid-Labile Lipophilic Prodrugs of Cancer Chemotherapeutic Agents

The present application discloses an acid labile lipophilic molecular conjugate of cancer chemotherapeutic agents and methods for reducing or substantially eliminating the side effects of chemotherapy associated with the administration of a cancer chemotherapeutic agent to a patient in need thereof. 117-. (canceled)19. The pharmaceutical composition of claim 18 , wherein the liquid formulation is a lipid emulsion (INTRALIPID®) for intravenous injection.20. The pharmaceutical composition of claim 18 , wherein the liquid formulation is a buffered claim 18 , isotonic claim 18 , aqueous solution.21. The composition of claim 18 , wherein the liquid formulation further comprise suitable diluents selected from the group consisting of normal isotonic saline solution claim 18 , 5% dextrose in water or buffered sodium or ammonium acetate solution.32. A method for the treatment of cancer in a patient comprising administering to the patient a therapeutically effective amount of a compound or composition of claim 18 , to a patient in need of such treatment.33. The method of claim 32 , wherein the cancer is selected from the group consisting of leukemia claim 32 , neuroblastoma claim 32 , glioblastoma claim 32 , cervical claim 32 , colorectal claim 32 , pancreatic claim 32 , renal and melanoma.34. The method of claim 32 , wherein the cancer is selected from the group consisting of lung claim 32 , breast claim 32 , prostate claim 32 , ovarian and head and neck.36. The method of claim 35 , wherein the method provides a higher concentration of the cancer chemotherapeutic agent in a cancer cell of the patient. This application claims the benefit of U.S. Non-Provisional application Ser. No. 13/856,216, filed Apr. 3, 2013, which claims the benefit of U.S. Non-Provisional application Ser. No. 13/489,247, filed Jun. 5, 2012, which claims the benefit of U.S. Provisional Application No. 61/493,827 filed Jun. 6, 2011 and U.S. Provisional Application No. 61/496,367 filed Jun. 13, 2011, the ...

Polycyclic compound and organic electroluminescence device including the same

Disclosed are a polycyclic compound and an organic electroluminescence device including the same. The polycyclic compound according to an embodiment is represented by the following Formula 1,

COUMARIN COMPOUNDS AND THEIR USES AS FLUORESCENT LABELS

The present application relates to new coumarin compounds and their uses as fluorescent labels. The compounds may be used as fluorescent labels for nucleotides in nucleic acid sequencing applications. 3. The compound of claim 2 , wherein X is O.4. The compound of claim 2 , wherein X is S.7. The compound of or claim 2 , wherein each Rand Ris a substituted alkyl.8. The compound of any one of to claim 2 , wherein each Rand Ris alkyl substituted with carboxyl claim 2 , carboxylate claim 2 , sulfo or sulfonate.9. The compound of any one of to claim 2 , wherein Ris substituted with one or more substituents selected from the group consisting of alkyl claim 2 , halo claim 2 , and C-carboxy.10. The compound of any one of to claim 2 , wherein the bond represented by a solid and dashed line is a double bond.11. The compound of claim 10 , wherein Ris alkyl.12. The compound of claim 11 , wherein Ris methyl.13. The compound of any one of to claim 11 , wherein each Rand Ris H.14. The compound of any one of to claim 11 , wherein at least one of Rand Ris alkyl.15. The compound of claim 14 , wherein each Rand Ris alkyl.16. The compound of claim 15 , wherein each Rand Ris methyl.17. The compound of any one of to claim 15 , wherein the bond represented by a solid and dashed line is a single bond.18. The compound of claim 17 , wherein at least one of Rand Ris alkyl.19. The compound of claim 18 , wherein each of Rand Ris alkyl.20. The compound of claim 17 , wherein at least one of Rand Ris H.21. The compound of claim 20 , wherein each of Rand Ris H.22. The compound of any one of to claim 20 , wherein at least one of Rand Ris H.23. The compound of any one of to claim 20 , wherein at least one of Rand Ris alkyl.24. The compound of any one of to claim 20 , wherein Ris a substituted alkyl.25. The compound of claim 24 , wherein Ris alkyl substituted with carboxyl.26. The compound of claim 24 , wherein Ris alkyl substituted with —C(O)OR claim 24 , and wherein Ris selected from the group ...

COMPOUND, MATERIAL FOR ORGANIC ELECTROLUMINESCENT ELEMENTS, ORGANIC ELECTROLUMINESCENT ELEMENT, AND ELECTRONIC DEVICE

A compound is represented by a formula (1) below, in which k is an integer of 0 or more, m is an integer of 1 or more, n is an integer of 2 or more. L is a substituted or unsubstituted aromatic hydrocarbon ring having 6 to 30 ring carbon atoms, CN is a cyano group, and Dand Dare each independently represented by one of a formula (2), a formula (3) and formula (3x) below, Dand Dbeing optionally mutually the same or different. 2. The compound according to claim 1 , wherein{'sub': 1', '2, 'the Dis the same as the D.'}3. The compound according to claim 1 , wherein{'sub': 1', '2, 'the Dis different from the D.'}4. The compound according to claim 1 , whereinthe L is a substituted or unsubstituted aromatic hydrocarbon ring having 6 to 10 ring carbon atoms.15. The compound according to claim 14 , wherein{'sub': '50', 'the Ris each independently a group selected from the group consisting of a substituted or unsubstituted 1-carbazolyl group, a substituted or unsubstituted 2-carbazolyl group, a substituted or unsubstituted 3-carbazolyl group, a substituted or unsubstituted 4-carbazolyl group, and a substituted or unsubstituted 9-carbazolyl group.'}16. The compound according to claim 1 , whereinp is 2 in the formula (3).17. The compound according to claim 16 , whereinamong two cyclic structures A, a first cyclic structure A is represented by the formula (31) and a second cyclic structure A is represented by the formula (32).19. The compound according to claim 18 , wherein{'sub': 1', '2, 'at least one of Dand Drepresented by the formula (3) is represented by one of the formulae (33) to (36).'}20. The compound according to claim 1 , wherein{'sub': 1', '8', '11', '18', '111', '118, 'the Rto R, the Rto R, and the Rto Rare each independently a hydrogen atom, a substituted or unsubstituted aryl group having 6 to 30 ring carbon atoms, a substituted or unsubstituted heterocyclic group having 5 to 30 ring atoms, a substituted or unsubstituted alkyl group having 1 to 30 carbon atoms, a ...

NOVEL SUBSTITUTED PYRAZOLO-PIPERAZINES AS CASEIN KINASE 1 D/E INHIBITORS

The invention provides compounds of Formula (I): 3. The compound according to claim 2 , wherein:{'sub': 1', '4', '5, 'Ris independently selected from aryl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazinyl, furyl, thienyl, imidazolyl, thiazolyl, indolyl, oxazolyl, isoxazolyl, pyrazolyl, triazolyl, tetrazolyl, indazolyl, 1,2,4-thiadiazolyl, isothiazolyl, quinolinyl, isoquinolinyl, each substituted with 1-4 Rand R;'}{'sub': 4', '1-4', 'e, 'R, at each occurrence, is independently selected from H and Calkyl substituted with 0-3 R;'}{'sub': 5', '1-4', 'e', '2', 'b', 'p', 'c', 'b', '2', 'r', 'b', '2', 'r', 'a', 'a', '2', 'r', 'a', 'a', '2', 'r', 'b', '2', 'r', 'b', '2', 'r', 'a', 'a', '2', 'r', 'a', 'a', '2', 'r', 'b', '2', 'r', '2', 'a', 'a', '2', 'r', '2', 'a', 'a', '2', 'r', '2', 'c', '2', 'r', 'e', '2', 'r', 'e, 'R, at each occurrence, is independently selected from H, Calkyl substituted with 0-3 R, F, Cl, Br, ═O, CN, NO, —OR, —S(O)R, —CN, —OR, —(CH)C(═O)R, —(CH)NRR, —(CH)C(═O)NRR, —(CH)NHC(═O)R, —(CH)NHC(═O)OR, —(CH)OC(═O)NRR, —(CH)NHC(═O)NRR, —(CH)C(═O)OR, —(CH)S(O)NRR, —(CH)NHS(O)NRR, —(CH)NHS(O)R, (CH)-carbocyclyl substituted with 0-3 R, and —(CH)-heterocyclyl substituted with 0-3 R;'}{'sub': a', '1-6', 'e', '2-6', 'e', '2-6', 'e', '2', 'r', '3-10', 'e', '2', 'r', 'c', 'a', 'a', 'e, 'R, at each occurrence, is independently selected from H, CN, Calkyl substituted with 0-5 R, Calkenyl substituted with 0-5 R, Calkynyl substituted with 0-5 R, —(CH)—Ccarbocyclyl substituted with 0-5 R, and —(CH)-heterocyclyl substituted with 0-5 R; or Rand Rtogether with the nitrogen atom to which they are both attached form a heterocyclic ring substituted with 0-5 R;'}{'sub': b', '1-6', 'e', '2-6', 'e', '2-6', 'e', '2', 'r', '3-10', 'e', '2', 'r', 'e, 'R, at each occurrence, is independently selected from H, Calkyl substituted with 0-5 R, Calkenyl substituted with 0-5 R, Calkynyl substituted with 0-5 R, —(CH)—Ccarbocyclyl substituted with 0-5 R, and —(CH)-heterocyclyl ...

NOVEL TETRACYCLIC 4-OXO-PYRIDINE-3-CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

The invention provides novel compounds having the general formula: 2. The compound of formula I according to claim 1 , wherein{'sup': '1', 'Ris hydrogen;'}{'sup': '2', 'sub': '1-6', 'Ris halogen or Calkoxy;'}{'sup': 3', '7, 'sub': '1-6', 'Ris selected from Calkyl, pyrrolidinyl or OR, wherein'}{'sup': '7', 'sub': 1-6', '1-6', '3-7', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6, 'Ris hydrogen, Calkyl, haloCalkyl, CcycloalkylCalkyl, phenylCalkyl, cyanoCalkyl, hydroxyCalkyl, CalkoxyCalkyl, carboxyCalkyl, CalkoxycarbonylCalkyl, CalkylsulfanylCalkyl, CalkylsulfonylCalkyl, aminoCalkyl, CalkylcarbonylaminoCalkyl, CalkylsulfonylaminoCalkyl, CalkoxycarbonylaminoCalkyl, morpholinylCalkyl, pyrrolidinylCalkyl or (2-oxo-pyrrolidinyl)Calkyl;'}{'sup': '4', 'Ris hydrogen;'}{'sup': '5', 'sub': '1-6', 'Ris hydrogen or Calkyl;'}{'sup': '6', 'sub': '1-6', 'Ris hydrogen or Calkyl;'}{'sub': '2', 'V and Y are CH;'}{'sub': 2', '2', '1-6, 'X is selected from a bond, CH, O, S, SOand phenylCalkoxycarbonylamino when W is a bond; or'}{'sub': 2', '2, 'X is CHwhen W is CH;'}or a pharmaceutically acceptable salt, or an enantiomer, or a diastereomer thereof.3. The compound of formula I according to claim 2 , wherein{'sup': '1', 'Ris hydrogen;'}{'sup': '2', 'Ris chloro or methoxy;'}{'sup': '3', 'Ris selected from methyl, ethyl, propyl, pyrrolidinyl, hydroxy, methoxy, difluoroethoxy, trifluoroethoxy, cyclopropylmethoxy, benzyloxy, cyanopropoxy, hydroxypropoxy, hydroxyhexyloxy, hydroxydimethylpropoxy, methoxyethoxy, methoxypropoxy, carboxypropoxy, ethoxycarbonylpropoxy, methylsulfanylpropoxy, methylsulfonylpropoxy, aminohexyloxy, methylcarbonylaminohexyloxy, methylsulfonylaminohexyloxy, tert-butoxycarbonylaminohexyloxy, morpholinylpropoxy, pyrrolidinylpropoxy and (2-oxo-pyrrolidinyl)propoxy;'}{'sup': '4', 'Ris hydrogen;'}{'sup': '5', 'Ris hydrogen or methyl;'}{'sup': '6', 'Ris hydrogen or ...

PYRIDINO[1,2-A]PYRIMIDONE ANALOGUE USED AS MTOR/P13K INHIBITOR

Disclosed is a pyridino[1,2-a]pyrimidone analogue used as an mTOR/PI3K inhibitor. The present invention particularly relates to a compound represented by formula (I) or a pharmaceutically acceptable salt thereof. 5. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1 , wherein one of L and Q is selected from the group consisting of —S(═O)NH— claim 1 , —S(═O)— claim 1 , —NH— claim 1 , —NHC(═O)NH— claim 1 , and the other is selected from the group consisting of a single bond and —CH—.6. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1 , wherein zero or one of X claim 1 , Y claim 1 , and Z is selected from N claim 1 , and the others are selected from the group consisting of CH claim 1 , C(CH) claim 1 , C(CF) claim 1 , CCl claim 1 , CF.71. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1 , wherein A and T are independently selected from the group consisting of N claim 1 , CH claim 1 , C(CH) claim 1 , C(CF) claim 1 , CC claim 1 , CF; or B is selected from the group consisting of NH claim 1 , N(CH) and N(CF).8. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the ring formed between any two R claim 1 , Rand Rin the same D claim 1 , two D claim 1 , or Rand one Dis selected from the group consisting of cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , oxetanyl claim 1 , 1 claim 1 ,3-dioxolanyl.10. The compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1 , wherein the compound is selected from the group consisting of compound 1-compound 284. The present invention relates to a class of pyridino[1,2-a]pyrimidinone analogs as mTOR/PI3K inhibitor, and particularly, the present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof.PI3K pathway is a site in human cancer cells where ...

Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases

The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.