ПОЛИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Изобретение относится к способу получения соединения формулы (IVa):или его фармацевтически приемлемой соли или стереоизомера. Способ включает обработку гидроксиалкилтиофена формулы (i):(i),аминоальдегид ацеталем и кислотой с получением соединения формулы (IVa), где m равно 0, n равно 1, Rи Rявляются, каждый независимо, водородом или Салкилом, Rи Rявляются, каждый независимо, водородом или Салкилом, Rпредставляет собой водород, и Rи Rявляются, каждый независимо, водородом, галогеном или Салкилом. Также предложены способы получения конкретных соединений формулы (IVa). Изобретение позволяет получить соединения, которые применятся для предотвращения и/или проведения лечения неврологических нарушений. 3 н. и 25 з.п. ф-лы, 2 табл.

ПОЛИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

... 1. Соединение формулы (I):или его фармацевтически приемлемая соль или стереоизомер, гдеодин из Х и Y является O, а другой является CH; или оба, и Х, и Y, являются CH;один из Z, Zи Zявляется S; и (i) два из Z, Zи Zявляются C; или (ii) один из Z, Zи Zявляется C, и один из Z, Zи Zявляется N;Rи Rявляются, каждый независимо, (i) водородом, алкилом, алкоксилом, аминоалкилом, алкенилом, алкинилом, циклоалкилом, циклоалкилалкилом, арилом или аралкилом, каждый из которых является необязательно замещенным; или (ii) -(CH)-R, где Rявляется SOалкилом или SOарилом, каждый из которых является необязательно замещенным; или (iii) Rи Rвместе с атомом азота, к которому они присоединены, образуют необязательно замещенный гетероциклил или гетероарил;Rи Rявляются, каждый независимо, (i) водородом, алкилом, алкоксилом, аминоалкилом, алкенилом, алкинилом, циклоалкилом, циклоалкилалкилом, арилом или аралкилом, каждый из которых является необязательно замещенным; или (ii) -(CH)-R, где Rявляется CF, CN, нитро, амино ...

Thieno [2,3-B] pyridine derivatives as viral replication inhibitors

Spirothienopyran- piperidine derivatives as ORL-1 receptor antagonists for their use in the treatment of alcohol dependence and abuse

Spiropiperidine derivatives for controlling pests.

Thieno [2,3-B] pyridine derivatives as viral replication inhibitors.

Spirothienopyran- piperidine derivatives as ORL-1 receptor antagonists for their use in the treatment of alcohol dependence and abuse

Spiropiperidine derivatives for controlling pests

Spirothienopyran- piperidine derivatives as ORL-1 receptor antagonists for their use in the treatment of alcohol dependence and abuse

Thieno [2,3-B] pyridine derivatives as viral replication inhibitors.

Spiropiperidine derivatives for controlling pests

Spiropiperidine derivatives for controlling pests

Spirothienopyran- piperidine derivatives as ORL-1 receptor antagonists for their use in the treatment of alcohol dependence and abuse

Thieno [2,3-B] pyridine derivatives as viral replication inhibitors.

QUINOLYLHYDANTOINS AND ALDOSE REDUCTASE INHIBITION

COMPOUNDS WHICH INHIBIT THE RELEASE OF INFLAMMATORY CYTOKINES

The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula (I): wherein R comprises ethers or amines; R1 is:a) substituted or unsubstituted aryl; orb) substituted or unsubstituted heteroaryl; R2a and R2b units are each independently hydrogen, ethers, amines, amides, carboxylates, or said units can form a double bond, a carbonyl, or R2a and R2b can be taken together to form a substituted or unsubstituted ring comprising from 4 to 8 atoms, said ring selected from the group consisting of: i) carbocyclic; ii) heterocyclic; iii) aryl; iv) heteroaryl; v) bicyclic; and vi) heterobicyclic ...

MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF

Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

PYRAZOLOPYRIMIDINE DERIVATIVE

... [PROBLEMS] To provide a novel compound capable of inhibiting the activity of HSP90, particularly a novel compound capable of inhibiting the chaperon protein function of HSP90 and having an anti-tumor activity. [MEANS FOR SOLV ING PROBLEMS] A pyrazolopyrimidine compound represented by the formula (1) h aving various substituents, which is capable of inhibiting the ATPase activi ty of HSP90 and has an anti-tumor activity; an HSP90 inhibitor comprising th e compound represented by the formula (1); a pharmaceutical agent comprising the compound represented by the formula (1); an anti-cancer agent comprisin g the compound represented by the formula (1); a pharmaceutical composition comprising the compound represented by the formula (1); a method for the tre atment of cancer by using the compound represented by the formula (1); and o thers. (1) ...

GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention provides gonadotropin releasing hormone receptor antagonists and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.

GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention provides gonadotropin releasing hormone receptor antagonists of Formula (I) and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.

Compounds, useful for inhibiting RoR deployment-gamma-t of

СПИРОПИПЕРИДИНОВЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ АНТАГОНИСТОВ РЕЦЕПТОРА ORL-1

Предложены антагонист рецептора ORL-1 формулы его применение для лечения ожирения, мигрени и депрессии.

ПРОИЗВОДНЫЕ СПИРОПИПЕРИДИНА, СПОСОБ БОРЬБЫ С НАСЕКОМЫМИ И ПРОМЕЖУТОЧНОЕ СОЕДИНЕНИЕ

Производные спиропиперидина формулы І, где Y означает простая связь, С=O, C=S или S(O)m, где m равняется 0, 1 или 2; кольцо, обозначенное с помощью Т, представляет собой 5- или 6-членное гетероароматическое кольцо, и R1, R2, R3, R8 и Ra являются заданными органическими группами, и р равняется 0, 1, 2, 3, 4, 5 или 6; q равняется 0, 1, 2, 3, 4, 5 или 6; p+q равняется 1, 2, 3, 4, 5 или 6; или их соли или N-оксиды или композиции, которые их содержат, для борьбы с насекомыми; также описаны новые соединения. (I) ...

ПРОИЗВОДНЫЕ ТИЕНО[2,3-b]ПИРИДИНА КАК ИНГИБИТОРЫ РЕПЛИКАЦИИ ВИРУСА

Представленное изобретение касается ряда новых соединений, которые имеют противовирусную активность, более особенно способность ингибировать репликацию ВИЧ (вирус иммунодефицита человека). Изобретение также касается способов получения таких соединений, также как и новых промежуточных соединений, полезных на одной или более стадиях таких синтезов. Изобретение также касается фармацевтических композиций, содержащих эффективное количество таких соединений в качестве активных ингредиентов. Это изобретение также касается применения таких соединений как медикаментов или при приготовлении медикамента, полезного для лечения животных, страдающих вирусными инфекциями, в частности ВИЧ. Это изобретение также касается способов лечения вирусных инфекций у животных путем назначения терапевтического количества таких соединений, необязательно объединенных с одним или большим количеством других лекарственных средств, которые имеют противовирусную активность.

DERIVATIVES OF SPIROPIPERIDINE, INTENDED FOR DEALING WITH THE WRECKERS

SPIROTHIENOPYRAN- PIPERIDINE DERIVATIVES AS ORL-1 RECEPTOR ANTAGONISTS FOR THEIR USE IN THE TREATMENT OF ALCOHOL DEPENDENCE AND ABUSE

COMPOUNDS USEFUL FOR INHIBITING ROR-GAMMA-T

MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF

... 본 발명은 다환형 화합물, 이의 합성 방법, 상기 화합물을 포함하는 약학 조성물, 및 이들의 사용 방법에 관한 것이다. 본원에 제공되는 화합물은, 정신병 및 정신분열증을 포함하지만 이로 한정되지는 않는 다양한 신경학적 장애의 치료, 예방 및/또는 관리에 유용하다.

COMPOUNDS AND THEIR USE OR NUMBER TWO IT OXINDOLE AS THERAPEUTIC AGENTS

COMPOSED OF 6,7-DIHIDRO-5H-PIRAZOLO [1,2A] PIRAZOL-1-ONA ESPIROCICLICO AND THEIR USE TO MAKE a PHARMACEUTICAL COMPOSITION

Un compuesto de 6,7-dihidro-5H-pirazolo[1,2a]pirazol-1-ona espirocíclico incluyendo todas las formas enantioméricas y diastereoméricas, y sales farmacéuticamente aceptables de éstas, el compuesto antes mencionado tiene la fórmula (1), en donde R es: a) -O[CH2]kR3; o b) -NR4aR4b, R3 es alquilo C1-4 sustituido o no sustituido, hidrocarbilo sustituido o no sustituido, heterociclilo sustituido o no sustituido, arilo, alquilenarilo sustituido o no sustituido, heteroarilo o alquilenheteroarilo sustituido o no sustituido; el índice k es de 0 a 5; R4a y R4b independientemente son cada uno: a) hidrógeno; o b) -[C(R5aR5b)]mR6; cada R5a y R5b independientemente son hidrógeno, o alquilo C1-4 lineal, ramificado, o cíclico, y mezclas de éstos; R6 es -OR7, -N(R7)2, -CO2R7, -CON(R7)2; alquilo C1-4 sustituido o no sustituido, arilo sustituido o no sustituido, o heteroarilo sustituido o no sustituido; R7 es hidrógeno, un catión soluble en agua, o alquilo C1-4; el índice m es de 0 a 5; R1 es: a) arilo sustituido ...

Gonadotropin releasing hormone receptor antagonists, method for the preparation thereof and pharmaceutical composition comprising the same

Disclosed are a gonadotropin releasing hormone receptor antagonist and a pharmaceutical composition including the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.

ピリドモルフィナン類、チエノモルフィナン類及びそれらの使用

... 定式(I)及び(II): 【化1】 そして 【化2】 式中、各々のY、XおよびRは、独立して、水素、水酸基、ハロ基、CF3、NO2、CN、NH2、COR1及びCO2R2から群より選択されるものであり;式中のY、XおよびRの少なくとも1つは、水素以外のものである場合:R1はアルキル、アリル基、アラルキル基及びNH2から群より選択されるものであり、R2はアルキル、アリル基及びアラルキル基から群より選択されるものである;によって表わされる化合物、並びに、それの薬学的許容できる塩類を提供する。式の化合物は、免疫調製剤として痛みの処置の為の鎮痛剤として有用である。 ...

ПРОИЗВОДНОЕ ПИРАЗОЛОПИРИМИДИНА

Изобретение относится к соединению, представленному формулой (1), к его соли или гидрату, где в формуле (1) R1 представляет собой метиленовую группу, R2 представляет собой фенильную группу, которая может содержать заместитель(и), или гетероциклическую группу, которая может содержать заместитель(и), цикл А представляет собой 6- или 7-членный цикл (где составляющие цикл атомы цикла А, отличные от атома серы в положении 6, являются атомами углерода), и R3 представляет собой атом водорода, или 1-3 одинаковых или разных заместителя, которыми замещен цикл А, где возможные заместители указаны в п.1 формулы изобретения. Изобретение также относится к фармацевтической композиции, обладающей противоопухолевой активностью, на основе соединения, представленного формулой (1). Технический результат - получены новые соединения и фармацевтическая композиция на их основе, которые могут найти применение в медицине для лечения рака. 6 н. и 11 з.п. ф-лы, 2 табл.

6,7-ДИГИДРО-5H-ПИРАЗОЛО[1,2-a]ПИРАЗОЛ-1-ОНЫ (ВАРИАНТЫ), ИНГИБИРУЮЩИЕ ВЫСВОБОЖДЕНИЕ ВОСПАЛИТЕЛЬНЫХ ЦИТОКИНОВ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ И СПОСОБ ИНГИБИРОВАНИЯ

Изобретение относится к новым соединениям формулы (I), обладающим свойствами ингибитора высвобождения воспалительных цитокинов из клеток. В формуле (I): R выбран из: а) фрагмента, имеющего формулу -OR3, где R3 выбирается из группы, состоящей из фенила, 2-фторфенила, 3-фторфенила, 4-фторфенила, 2,6-дифторфенила, 2-цианофенила, 3-цианофенила, 2-трифторметилфенила, 4-трифторметилфенила, 2-метилфенила, 4-метилфенила, 2,4-диметилфенила, 3-N-ацетиламинофенила, 2-метоксифенила, 4-метоксифенила и 3-бензо[1,3]диоксол-5-ила; в) фрагмента, имеющего формулу: где R6 выбирается из группы, состоящей из водорода, метила, этила, винила, циклопропила, циклогексила, метоксиметила, метоксиэтила, 1-гидрокси-1-метилэтила, карбоксифенила, 4-фторфенила, 2-аминофенила, 2-метилфенила, 4-метилфенила, 4-метоксифенила, 4-(пропансульфонил)фенила, 3-бензо[1,3]диоксол-5-ила, пиридин-2-ила, пиридин-3-ила; или с) фрагмента, имеющего формулу: где R6 выбирается из группы, состоящей из водорода, метила, этила, винила, циклопропила ...

СПИРООКСИНДОЛЬНЫЕ СОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ТЕРАПЕВТИЧЕКИХ СРЕДСТВ

... 1. Соединение формулы (I):где n является 1 или 2;один из J и K является -CH-, а другой является -O-;или оба, и J, и K, являются, каждый, -CH-;Rявляется водородом, метилом, циклопропилом, карбоксиметилом, (3-карбокси)бензилом, (3-метилсульфониламино)бензилом, [(3-метилсульфониламино)пиридин-2-ил]метилом, [(3-карбокси)пиридин-2-ил]метилом, [(этокси)карбонил]метилом, 2-циклопропилэтилом, 1,3-тиазол-5-илметилом, 3-метоксипропилом, (6-метилпиридин-2-ил)метилом, пиридин-3-илметилом, [3-(циано)пиридин-2-ил]метилом, [3-(дифторметил)пиридин-2-ил]метилом, 3-(5-метил-1,2,4-оксадиазол-3-ил)бензилом, 4-(5-метил-1,2,4-оксадиазол-3-ил)бензилом, [5-(трифторметил)-1,2,4-оксадиазол-3-ил]метилом, [5-(трифторметил)-1,3,4-оксадиазол-2-ил]метилом, [4-(трифторметил)пиридин-2-ил]метилом, (4-метил-1,2,5-оксадиазол-3-ил)метилом, пиразин-2-илметилом, пиримидин-2-илметилом, (1-метил-1H-бензотриазол-5-ил)метилом, [2-(трет-бутоксикарбониламино)пиридин-5-ил]метилом, [6-(диметиламино)пиридин-3-ил]метилом, [6-(диметиламино ...

(1R,4R) 7-ОКСО-2-АЗАБИЦИКЛО[2.2.2]ОКТ-5-ЕН И ЕГО ПРОИЗВОДНЫЕ

1. Соединение Формулы (I) или (Ia):или соль указанного соединения, гдеRвыбран из группы, состоящей из водорода, -COR, -COR, -C(R)и защитной группы для амина;Rвыбран из группы, состоящей из C-Cалкила, возможно замещенного 1-3 заместителями, выбранными из C-Cарила, C-Cциклоалкила, C-Cгетероарила, C-Cгетероциклила, галогена, амино, -N, гидрокси, C-Cалкокси, силила, нитро, циано и группы COH или ее сложноэфирной группы, C-Cалкенила, C-Cалкинила, C-Cарила, C-Cгетероарила, C-Cциклоалкила и C-Cгетероциклила,Rи Rнезависимо выбраны из группы, состоящей из водорода, C-Cалкила, возможно замещенного 1-3 заместителями, выбранными из C-Cарила, C-Cциклоалкила, C-Cгетероарила, C-Cгетероциклила, галогена, амино, -N, гидрокси, C-Cалкокси, силила, нитро, циано и группы COH или ее сложноэфирной группы, C-Cалкенила, C-Cалкинила, C-Cарила, C-Cгетероарила, C-Cциклоалкила и C-Cгетероциклила,Rи Rнезависимо представляют собой водород, гидрокси, C-Cалкил, C-Cалкенил и C-Cалкинил, -SRили -OR, причем указанная алкильная, алкенильная или алкинильная группа возможно замещена 1-3 заместителями, выбранными из группы, состоящей из кето, галогена, C-Cалкокси, амино, гидрокси, циано, нитро, -NHCOCH, -Nи группы -COH или ее сложноэфирной группы, при условии что по меньшей мере один из Rи R, предпочтительно R, является заместителем, отличным от водорода, илиRи Rсовместно с атомом углерода, к которому они присоединены, образуют кетоновую (C=O) группу, основание Шиффа (=NR), винилиденовый фрагмент формулы =CRR, или образуют 5-6-членный циклический кеталь или тиокеталь, причем циклический кеталь или тиокеталь имеет формулу:каждый Rнезависимо выбран из группы, состоящей из C-Cалкила, возможно замещенного 1-3 заместителями, выбранными из C-Cарила, C-Cциклоалкила, C-Cгетероарила, C-Cгетероциклила, галогена, амино, -N, гидрокси, C-Cалкокси, силила, нитро, циано и группы COH или е РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК C07D 451/04 (13) 2014 124 531 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ ...

Novel viral replication inhibitors

CONNECTIONS, WHICH THE RELEASE OF CYTOKINEN INHIBIEREN

PROCEDURE FOR THE PRODUCTION OF NEW SPIROPYRIDOCHROMAN-4',5-HYDANTOINEN

Spiropiperidine compounds as ORL-1 receptor antagonists

An ORL-1 receptor antagonist of the formula: its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also demonstrated through animal models that the compounds of the present invention are useful for the treatment of migraines.

Gonadotropin releasing hormone receptor antagonists, method for the preparation thereof and pharmaceutical composition comprising the same

The present invention provides gonadotropin releasing hormone receptor antagonists and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.

SPIROCYCLIC-6,7-DIHYDRO-5H-PYRAZOLO[1,2-A]PYRAZOL-1-ONES WHICH CONTROL INFLAMMATORY CYTOKINES

The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines;R1 is:a) substituted or unsubstituted aryl; orb) substituted or unsubstituted heteroaryl;two R2 units on the same carbon atom are taken together to form a spirocyclic ring having from 4 to 7 atoms, the balance of the R2 units are independently selected from the group consisting of:a) hydrogen;b) - O(CH2)jR8;c) -(CH2)jNR9aR9b;d) -(CH2)jCO2R10;e) OCO2R10f) -(CH2)jCON(R10)2; andg) two R2 units can be taken together to form a carbonyl unit;R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ...

COMPOUNDS USEFUL FOR INHIBITING ROR-GAMMA-T

The present invention provides novel ROR gamma-t inhibitors and pharmaceutical compositions thereof: ...

ALDOSE REDUCTASE INHIBITING QUINOLYLHYDANTIONS

BENZOPYRAN AND PYRANOPYRIDINE DERIVATIVES AS POTASSIUM CHANNEL OPENERS

The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.

NOVEL BENZOPYRAN DERIVATIVES AS POTASSIUM CHANNEL OPENERS

The present invention is directed to novel benzopyran derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.

MNK INHIBITORS AND METHODS RELATED THERETO

The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4a, R4b, R5, R6, R7, R8, W1, W2, Y and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula (I) compounds as well as methods for utilizing the compounds of Formula (I) and the pharmaceutically acceptable compositions of Formula (I) compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

INHIBITORS OF MNK AND RELATED METHODS

ПРОИЗВОДНЫЕ СПИРОПИПЕРИДИНА, ПРЕДНАЗНАЧЕННЫЕ ДЛЯ БОРЬБЫ С ВРЕДИТЕЛЯМИ

В изобретении описано применение соединения формулы I Y обозначает ординарную связь, С=O, C=S или S(O)m, где m равно 0, 1 или 2; кольцо, обозначенное с помощью Т, представляет собой 5- или 6-членное гетероароматическое кольцо и R1, R2, R3, R8 и Ra являются заданными органическими группами и р равно 0, 1, 2, 3, 4, 5 или 6; q равно 0, 1, 2, 3, 4, 5 или 6; p+q равно 1, 2, 3, 4, 5 или 6; или его солей, или N-оксидов, или содержащих его композиций для борьбы с насекомыми, клещами, нематодами или моллюсками; также описаны новые соединения.

COMPOUNDS OF SPIROPIPERIDINES AS ANTAGONISTS OF THE ORL-1 RECEPTORS

RSV ANTIVIRAL COMPOUNDS

ПРОИЗВОДНЫЕ ТИЕНО[2,3-B]ПИРИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ РЕПЛИКАЦИИ ВИРУСА

Представленное изобретение касается ряда новых соединений, которые имеют противовирусную активность, особенно способность ингибировать репликацию ВИЧ (вирус иммунодефицита человека). Изобретение также касается способов получения таких соединений, также как и новых промежуточных соединений, полезных на одной или большем количестве стадии таких синтезов. Изобретение также касается фармацевтических композиций, которые содержат эффективное количество соединений в качестве активных ингредиентов. Это изобретение также касается применения соединений как медикаментов или при изготовлении медикамента, полезного для лечения животных, которые страдают вирусными инфекциями, в частности ВИЧ. Это изобретение также касается способов лечения вирусных инфекций у животных путем назначения терапевтического количества таких соединений, необязательно, объединенных с одним или большим количеством других лекарственных средств, имеющих противовирусную активность.

DERIVATIVES OF SPIROTIENOPIRANPIPERIDINA AS ANTAGONISTS OF RECEPTOR ORL-1 FOR USE FOR TREATING ALCOHOL DEPENDENCE AND ALCOHOL ABUSE

spiropiperidinovye compounds as orl-1 receptor antagonists

spiropiperidinovye compounds as orl-1 receptor antagonists

ANTIVIRAL COMPOUNDS AGAINST RSV

Nonrepresentative protein kinase C of thienopyrimidines inhibitors

다환형 화합물 및 이의 사용 방법

... 본 발명은 다환형 화합물, 이의 합성 방법, 상기 화합물을 포함하는 약학 조성물, 및 이들의 사용 방법에 관한 것이다. 본원에 제공되는 화합물은, 정신병 및 정신분열증을 포함하지만 이로 한정되지는 않는 다양한 신경학적 장애의 치료, 예방 및/또는 관리에 유용하다.

Compound having spiro structure and organic light emitting device comprising the same

COMPOUNDS USEFUL FOR INHIBITING ROR-GAMMA-T

SPIROTHIENOPYRAN- PIPERIDINE DERIVATIVES AS ORL-1 RECEPTOR ANTAGONISTS FOR THEIR USE IN THE TREATMENT OF ALCOHOL DEPENDENCE AND ABUSE

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 skin or mucous membrane.

NOVEL BENZOPYRAN DERIVATIVES AS POTASSIUM CHANNEL OPENERS

The present invention is directed to novel benzopyran derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.

Thienopyrimidine inhibitors of atypical protein kinase C

... or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.

Thienopyrimidine inhibitors of atypical protein kinase C

The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.

SPIROCYCLIC HETERCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS

The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R 1 , R 2 and R 11 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.

ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ АСПАРТИЛЬНОЙ ПРОТЕАЗЫ

1. Соединение, имеющее структурную формулу I ! ! или его стереоизомер, таутомер или фармацевтически приемлемая соль или сольват, где W представляет собой связь, -C(=S)-, -S(O)-, -S(O)2-, -С(=O)-, -O-, -C(R6)(R7)-, -N(R5)- или -C(=N(R5))-; ! X представляет собой -O-, -N(R5)- или -C(R6)(R7)-; ! U представляет собой связь или -(C(R3)(R4))b-, где b равен 1 или 2; ! R1, R2 и R5 независимо выбраны из группы, состоящей из атома водорода (Н), алкила, арилалкила, гетероарилалкила, циклоалкилалкила, гетероциклоалкилалкила, арилциклоалкилалкила, гетероарилциклоалкилалкила, арилгетероциклоалкилалкила, гетероарилгетероциклоалкилалкила, циклоалкила, арилциклоалкила, гетероарилциклоалкила, гетероциклоалкила, арилгетероциклоалкила, гетероарилгетероциклоалкила, алкенила, арилалкенила, циклоалкенила, арилциклоалкенила, гетероарилциклоалкенила, гетероциклоалкенила, арилгетероциклоалкенила, гетероарилгетероциклоалкенила, алкинила, арилалкинила, арила, циклоалкиларила, гетероциклоалкиларила, циклоалкениларила, гетероциклоалкениларила, гетероарила, циклоалкилгетероарила, гетероциклоалкилгетероарила, циклоалкенилгетероарила, гетероциклоалкенилгетероарила, -OR15, -CN, -C(=NR11)R8, -C(O)R8, -C(O)OR9, -S(O)R10, -S(O)2R10, -C(O)N(R11)(R12), -S(O)N(R11)(R12), -S(O)2N(R11)(R12), -NO2, -N=C(R8)2 и -N(R11)(R12), при условии, что R1 и R5 не выбраны оба одновременно из -NO2, -N(R8)2 и -N(R11)(R12); ! R3, R4 и R6 независимо выбраны из группы, состоящей из Н, алкила, арилалкила, гетероарилалкила, циклоалкилалкила, гетероциклоалкилалкила, арилциклоалкилалкила, гетероарилциклоалкилалкила, арилгетероциклоалкилалкила, гетероарилгетероциклоалкилалкила, циклоалкила, арилциклоалкила, гетероарилциклоалкила, гетероциклоалкила, арилгетероциклоалкила, гетероарилгетероц РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2009 100 074 (13) A (51) МПК C07D 239/20 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21), (22) Заявка: 2009100074/04, 07.06.2007 (71) ...

ПОЛИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

МОДУЛИРОВАНИЕ ХЕМОСЕНСОРНЫХ РЕЦЕПТОРОВ И СВЯЗАННЫХ С НИМИ ЛИГАНДОВ

... 1. Проглатываемая композиция, содержащая соединение структурной формулы (IIс) в количестве, обеспечивающем улучшение сладкого вкуса:или его таутомер, соль, сольват и/или его сложный эфир, где:А является водородом, алкилом, замещенным алкилом, гетероалкилом, замещенным гетероалкилом, -CN, -OR, -NHOR, NRCOR, -NRR, -NRCOR, -NRCONRR, -NRCSNRRили -NRC(=NH)NRR;Rявляется водородом, алкилом, замещенным алкилом, арилалкилом, замещенным арилалкилом, гетероалкилом, замещенным гетероалкилом, гетероарилалкилом или замещенным гетероарилалкилом;R, Rили Rнезависимо являются водородом, алкилом, замещенным алкилом, арилом, замещенным арилом, арилалкилом, замещенным арилалкилом, ацилом, замещенным ацилом, гетероалкилом, замещенным гетероалкилом, гетероарилом, замещенным гетероарилом, гетероарилалкилом или замещенным гетероарилалкилом; или альтернативно Rи Rили Rи R, вместе с атомами, к которым они присоединены, образуют циклогетероалкильное или замещенное циклогетероалкильное кольцо;W является -S-;Y является ...

6,7-DIHYDRO-5H-PYRAZOLO-1,2-AÖ PYRAZOL-1-ONE AS a CHECK OF INFLAMMATION-PROMOTING CYTOKINEN

HETERO-CYCLIC CONDENSED MORPHINE DERIVATIVES

PROCEDURE FOR THE PRODUCTION OF NEW SPIROPYRIDOCHROMAN-4',5-HYDANTOINEN

SPIROPIPERIDINDERIVATE FOR THE FIGHT AGAINST PARASITS

NEW BENZOPYRANDERIVATE AS POTASSIUM CHANNEL OPENERS

VERFAHREN ZUR HERSTELLUNG VON NEUEN SPIROPYRIDOCHROMAN-4',5-HYDANTOINEN

Pyrazolopyrimidine derivative

Spiropiperidine compounds as ORL-1 receptor antagonists

As ORL-1 receptor antagonist of the formula I, its uses, and methods for its preparation are described. ORL-1 antagonists are deemed to be useful; in the treatment of depression and/or the treatment of overweight, obesity, and/or weight maintenance post treatment for overweight or obesity. Certain compounds have also demonstrated through animal models that the compounds of the present invention are useful for the treatment of migraine.

Gonadotropin releasing hormone receptor antagonists, method for the preparation thereof and pharmaceutical composition comprising the same

The present invention provides gonadotropin releasing hormone receptor antagonists and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.

PYRIDOMORPHINANS, THIENOMORPHINANS AND USE THEREOF

Compounds represented by formulae (I) and (II) wherein each of Y, X and R individually is selected from the group consisting of hydrogen, hydroxy, halo, CF3, NO2, CN, NH2, COR1 and CO2R2 wherein R1 is selected from the group consisting of alkyl, aryl, alkaryl, and NH2, and R2 is selected from the group consisting of alkyl, aryl and aralkyl, and provided that at least one of Y, X, and R is other than H; and pharmaceutically acceptable salts thereof are provided. Compounds of the formula are useful as analgesics for treating pain, as immunomodulators and for treating drug abuse.

THIENOPYRIMIDINE INHIBITORS OF ATYPICAL PROTEIN KINASE C

The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.

THIENOPYRIMIDINE INHIBITORS OF ATYPICAL PROTEIN KINASE C

The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.

DETECTION AND USE OF LOW MOLECULAR-WEIGHT MODULATORS OF THE COLD-MENTHOL RECEPTOR TRPM8

The invention relates to novel modulators of the cold-menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to the objects and means produced using said modulators.

10-AMINO-1,2,3,4-TETRAHYDROPYRIDO[2,1-A]ISOINDOL-6(10BH)-ONE DERIVATIVES, METHOD FOR PREPARING SAME, AND THERAPEUTIC USES THEREOF

La présente invention concerne des composés de formule générale (I) suivante dans laquelle : - A représente un groupe SO2 ou CX, X représentant O ou S; - R1, R2, R", R4 représentent notamment H, - R représente notamment un groupe alkyle ou un groupe aryle, ainsi que ses sels pharmaceutiquement acceptables, ledit composé de formule (I) étant sous forme de stéréoisomère pur ou sous forme de mélange d'énantiomères et/ou de diastéréoisomères, y compris de mélanges racémiques.

(1R,4R) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene and derivatives thereof

This invention provides novel (1R,4R) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene and derivatives thereof, preferably in substantially enantiomerically enriched forms, intermediates thereto, and processes of their synthesis.

POLYHETEROAROMATIC COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

Tricyclic benzazepine derivs - as inters for theno benzazepine antidepressants

MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF

... 본 발명은 다환형 화합물, 이의 합성 방법, 상기 화합물을 포함하는 약학 조성물, 및 이들의 사용 방법에 관한 것이다. 본원에 제공되는 화합물은, 정신병 및 정신분열증을 포함하지만 이로 한정되지는 않는 다양한 신경학적 장애의 치료, 예방 및/또는 관리에 유용하다.

다환형 화합물 및 이의 사용 방법

... 본 발명은 다환형 화합물, 이의 합성 방법, 상기 화합물을 포함하는 약학 조성물, 및 이들의 사용 방법에 관한 것이다. 본원에 제공되는 화합물은, 정신병 및 정신분열증을 포함하지만 이로 한정되지는 않는 다양한 신경학적 장애의 치료, 예방 및/또는 관리에 유용하다.

COMPOSED OF ESPIRO-OXINDOL AND ITS USE LIKE THERAPEUTIC AGENTS.

Compuestos de espiro-oxindol, como estereoisomeros, enantiomeros, tautomeros de los mismos o mezclas de los mismos; o sales, solvatos o prodrogas farmacéuticamente aceptables de los mismos, para el tratamiento y/o la prevencion de enfermedades o condiciones mediadas por canales de sodio, tal como el dolor. Reivindicacion 1: Un compuesto caracterizado porque es de formula (1) en donde n es 1 o 2; uno de J y K es -CH2- y el otro es -O-; o ambos J y K son cada uno -CH2-; R1 es hidrogeno, metilo, ciclopropilo, carboximetilo, (3-carboxi)bencilo, (3-metilsulfonilamino)bencilo, [(3-metilsulfonilamino)piridin-2-il]metilo, [(3-carboxi)piridin-2-il]metilo, [(etoxi)carbonil]metilo, 2-ciclopropiletilo, 1,3-tiazol-5-ilmetiIo, 3-metoxipropilo, (6-metilpiridin-2-il)metilo, piridin-3-ilmetilo, [3-(ciano)piridini-2-il]metilo, [3-(difluorometil)piridin-2-il]metilo, 3-(5-metil-1,2,4-oxadiazoI-3-il)bencilo, 4-(5-metil-1,2,4-oxadiazol-3-il)bencilo, [5-(trifluorometil)-1,2,4-oxadiazoI-3-il]metilo, [5-(trifluorometil ...

NOVEL BENZOPYRAN DERIVATIVES AS POTASSIUM CHANNEL OPENERS

The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.

SPIRO COMPOUND AND MEDICAL USES THEREOF

The present invention relates to a spiro compound and medical uses thereof. Specifically, the present invention relates to a spiro compound represented by the general formula (I), a preparation method thereof, a pharmaceutical composition containing the same, and is used as an acetyl-Coenzyme A carboxylase (ACC) inhibitor and is used for treating diseases associated with ACC activity. Each substituent in the general formula (I) is as defined in description. 2. The compound of formula (I) according to claim 1 ,wherein X is —S—.4. The compound of formula (I) according to claim 1 ,wherein,{'sup': '3', 'sub': 1', '6, 'Ris selected from alkyl, preferably C-Calkyl, said alkyl is further substituted by one or more Q groups;'}{'sup': a', 'a, 'each Q is independently selected from the group consisting of aryl, heteroaryl, ORand SR; wherein said aryl and heteroaryl are optionally further substituted with one or more groups selected from the group consisting of halogen, amino, nitro, cyano, hydroxyl, thiol, carboxyl, ester, oxo, alkyl, alkoxyl, haloalkyl, haloalkoxyl, cycloalkyl, heterocyclyl, aryl and heteroaryl;'}{'sup': 'a', 'Ris selected from the group consisting of alkyl, cycloalkyl and heterocyclyl, wherein said alkyl, cycloalkyl and heterocyclic are optionally further substituted with one or more groups selected from the group consisting of halogen, amino, nitro, cyano, hydroxyl, thiol, carboxyl, ester, oxo, alkyl, alkoxyl, cycloalkyl, heterocyclyl, aryl and heteroaryl.'}7. The compound of formula (I) according to claim 1 ,wherein,{'sub': 3', '7, 'ring A is a C-Ccycloalkyl group or a 5- to 7-membered heterocyclic group;'}{'sup': '1', 'sub': 1', '3, 'Lis selected from a single bond and a C-Calkylene, preferably a single bond;'}{'sup': 4', 'a', 'a', 'a', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'b', 'a', 'a', 'a', 'a', 'b, 'sub': n', 'n', 'n', 'n', '2, 'Ris selected from the group consisting of hydrogen, halogen, cyano, —R, ...

Method for synthesis of nitroxyl radical

The problem to be solved by the present invention is to provide a highly-versatile method for producing a nitroxyl radical derivative, in which position-2 and position-6 in a TEMPO-based compound can be easily substituted, and further, a method for producing a nitroxyl radical derivative, in which a nitrogen nucleus is labeled with 15N. The above-described problem can be solved by reacting a triacetoneamine derivative with ketone or aldehyde in the presence of ammonium salt or a 15N-labeled compound thereof to obtain a 2,6-substituted-4-piperidone derivative.

ПОЛИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Изобретение относится к соединению структурной формулы (Iva), которое может быть использовано для лечения, предотвращения или проведения лечения неврологического нарушения. В формуле (Iva) m равно 0; n равно 1; Rи Rявляются, каждый независимо, водородом, C-Cалкилом или С-Сциклоалкилом; Rи Rявляются, каждый независимо, водородом или C-Cалкилом; Rявляется водородом и Rи Rявляются, каждый независимо, водородом, галогеном, С-Салкилом, С-Сарилом, 5-10-членным гетероарилом, содержащим один атом О, один атом S и/или 1-4 атома N, 3-8-членным гетероциклилом, содержащим 1-2 гетероатома, выбранных из О, S и N, C-Cалкоксилом или аминоC-Cалкилом. Изобретение также относится к фармацевтической композиции, содержащей указанное соединение, и к способу лечения, предотвращения или проведения лечения неврологического нарушения, такого как психоз или шизофрения. 3 н. и 51 з.п. ф-лы, 2 табл.

МОДУЛИРОВАНИЕ ХЕМОСЕНСОРНЫХ РЕЦЕПТОРОВ И СВЯЗАННЫХ С НИМИ ЛИГАНДОВ

FIELD: chemistry. SUBSTANCE: group of inventions discloses edible compositions containing modifiers of chemosensory receptors and ligands thereof. Group of inventions particularly includes oral compositions containing a compound of structural formula EFFECT: possibility of obtaining and improving sweet taste. 27 cl, 13 dwg, 39 tbl, 284 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК G01N 33/15 (13) 2 586 282 C2 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2013153359/15, 03.06.2008 (24) Дата начала отсчета срока действия патента: 03.06.2008 Приоритет(ы): (30) Конвенционный приоритет: 2 5 8 6 2 8 2 R U (56) Список документов, цитированных в отчете о поиске: US2007104709 A1, 10.05.2007. US4196207 A, 01.04.1980. US3957783 A, 18.05.1976. LEISTNER et al. "Polycyclic azines with heteroatoms in the 1- and 3-positions. Part 22. A facile synthesis of 2-(alkylthio)-4aminothieno[2,3-d]pyrimidi nes" Archiv der Pharmazie (Weinheim, Germany), 322(4), PP. 227-230. БЕЛИКОВ В.Г., Фармацевтическая химия, М., Высшая школа, 1993, стр. 43-47. (73) Патентообладатель(и): СИНОМИКС, ИНК. (US) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) МОДУЛИРОВАНИЕ ХЕМОСЕНСОРНЫХ РЕЦЕПТОРОВ И СВЯЗАННЫХ С НИМИ ЛИГАНДОВ (57) Реферат: Группа изобретений раскрывает съедобные композиции, содержащие модификаторы хемосенсорных рецепторов и их лигандов. Конкретнее группа изобретений включает проглатываемые композиции, содержащие соединение структурной формулы (IIc) Композиции заявленной группы изобретений обеспечивают возможность получения и улучшения сладкого вкуса. 2 н. и 25 з.п. ф-лы, 13 Стр.: 1 C 2 C 2 (45) Опубликовано: 10.06.2016 Бюл. № 16 2 5 8 6 2 8 2 (43) Дата публикации заявки: 10.06.2015 Бюл. № 16 R U 08.06.2007 US 11/760,592; 08.08.2007 US 11/836,074; 08.02.2008 US 61/027,410 Номер и дата приоритета первоначальной заявки, из которой данная заявка выделена: ...

МОДУЛИРОВАНИЕ ХЕМОСЕНСОРНЫХ РЕЦЕПТОРОВ И СВЯЗАННЫХ С НИМИ ЛИГАНДОВ

Группа изобретений относится к соединениям - модификаторам хемосенсорных рецепторов и их лигандов, имеющим структурную формулу (IIIb), их подвидам и конкретным соединениям, съедобным композициям, содержащим модификаторы хемосенсорных рецепторов и их лигандов, имеющие структурную формулу (IIIb), их подвиды и конкретные соединения, а также к способам применения вышеуказанных соединений для улучшения сладкого вкуса съедобных композиций. Соединения данной группы изобретений обеспечивают возможность получения и улучшения сладкого вкуса. 6 н. и 18 з.п. ф-лы, 19 ил., 44 табл., 813 пр.

SPIROCYCLI 6,7-DIHYDRO-5H-PYRAZOLOC1,2 A) PYRAZOL-1-ONE, the INFLAMMATORI CYTOKINE TAXES

MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF

Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia. 24-. (canceled)6. The compound of claim 5 , wherein m is 0; n is 1; Rand Rare each independently hydrogen claim 5 , optionally substituted C-Calkyl claim 5 , or optionally substituted C-Calkyl; Rand Rare each independently hydrogen or optionally substituted C-Calkyl; Ris hydrogen; and Rand Rare each independently hydrogen claim 5 , halo claim 5 , C-Calkyl claim 5 , aryl claim 5 , heteroaryl claim 5 , heterocyclyl claim 5 , alkoxyl claim 5 , or aminoalkyl claim 5 , each of which is optionally substituted.7. (canceled)8. The compound of claim 5 , wherein Rand Rtogether with the nitrogen atom to which they are attached form a heteroaryl or heterocyclyl claim 5 , each of which is optionally substituted.9. (canceled)10. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an optionally substituted heterocyclyl ring.11. (canceled)12. The compound of claim 5 , wherein Rand Rtogether with the atom to which they are attached form a cycloalkyl or heterocyclyl ring claim 5 , each of which is optionally substituted.13. (canceled)14. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an aryl or cycloalkyl ring claim 5 , each of which is optionally substituted.15. (canceled)16. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an optionally substituted heterocyclyl.17. (canceled)18. The compound of claim 5 , wherein Rand Rtogether with the atoms to which they are attached form an optionally substituted heterocyclyl and Rand Rtogether with the nitrogen atom to which they are attached form an optionally substituted aryl. ...

Dihydrothienopyrimidines

The present invention relates to dihydrothienopyrimidines, their use as modulators of γ-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with γ-secretase and/or its substrate and therefore modulate the formation of Aβ peptides.

LOW MOLECULAR WEIGHT MODULATORS OF THE COLD MENTHOL RECEPTOR TRPM8 AND USE THEREOF

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators. 123.-. (canceled)27. The method according to claim 27 , where claim 27 , in the compound of the formula (II) claim 27 , X is not a methylene or linear 1 claim 27 ,4-butylene bridge.28. The method according to claim 27 , in which claim 27 , in the compounds of the formula II claim 27 , R claim 27 , Rand Rare H and{'sub': 22', '23, 'Rand R, together with the carbon atoms to which they are bonded, form a methylenedioxy group.'}29. The method according to claim 27 , in which claim 27 , in the compounds of the formula II claim 27 , the radicals Rand R claim 27 , independently of one another claim 27 , are an in each case mononuclear aryl or heteroaryl radical or a C-C-cycloalkyl radical.31. The method according to claim 25 , where the receptor is brought into contact with at least one compound which claim 25 , in a cellular activity test using cells which recombinantly express the human TRPM8 receptor claim 25 , modulates the permeability of these cells for Ca ions.32. The method according to claim 25 , where the modulating compound has an agonistic or antagonistic effect on the cellular Ca ion permeability.33. The method according to claim 25 , where the modulating compound is a TRPM8 receptor agonist.34. The use of a compound according to the definition in for inducing a sensation of coldness in humans and/or animals claim 25 , in particular for non-therapeutic purposes.35. The use of a compound according to the definition in as active constituent of a pharmaceutical composition.36. The use of a compound according to the definition in for the treatment of prostate carcinomas claim 25 , for the treatment of bladder weakness or in pain therapy.37. The use of a compound ...

SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. 13.-. (canceled)5. The compound of selected from:1′-(pyridin-2-ylmethyl)spiro[furo[2,3-g]quinoxaline-8,3′-indol]-2′(1′H)-one;1-(diphenylmethyl)spiro[indole-3,3′-thieno[2,3-f][1]benzofuran]-2(1′H)-one;1-(diphenylmethyl)spiro[indole-3,3′-thieno[2,3-f][1]benzofuran]-2(1′H)-one 5,5′-dioxide;spiro[indole-3,3′-thieno[2,3-f][1]benzofuran]-2(1′H)-one 5,5′-dioxide; or1-(pyridin-2-ylmethyl)spiro[indole-3,3′-thieno[2,3-f][1]benzofuran]-2(1′H)-one 5,5′-dioxide.1′-(4-methoxybenzyl)-3-methylspiro[furo[2,3-f][1,2]benzisoxazole-7,3′-indol]-2′(1′H)-one;5-(benzyloxy)-1′-[(5-chloro-2-thienyl)methyl]spiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;1′-(diphenylmethyl)-6-methoxy-5-methylspiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;6-bromo-1′-(diphenylmethyl)spiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;1′-(diphenylmethyl)-5,6-dimethylspiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;6-(benzyloxy)-1′-(diphenylmethyl)spiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;1′-(diphenylmethyl)-5-fluoro-6-methoxyspiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;1′-(diphenylmethyl)-5-fluorospiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;1′-(diphenylmethyl)-6-methoxyspiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;6-(benzyloxy)-1′-(3-methylbutyl)spiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;6-bromo-1′-{[5-(trifluoromethyl)furan-2-yl]methyl}spiro[1-benzofuran-3,3′-indol]-2′(1H)-one;5-bromo-1-{[5-(trifluoromethyl)furan-2-yl]methyl}spiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;6-methoxy-5-methylspiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;6-bromospiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;5,6-dimethylspiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;5-fluoro-6-methoxyspiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;5-fluoro-spiro[1-benzofuran-3,3′-indol]-2′(1′H)-one;6- ...

(1R,4R) 7-OXO-2-AZABICYCLO[2.2.2]OCT-5-ENE AND DERIVATIVES THEREOF

This invention provides novel (1R,4R) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene and derivatives thereof, preferably in substantially enantiomerically enriched forms, intermediates thereto, and processes of their synthesis. 3. The compound of claim 2 , wherein Ris hydrogen or CORand Ris C-Calkyl.4. The compound of wherein{'sup': 1', '11', '12', '13', '11', '12, 'sub': 2', '3, 'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'Ris —COR, —COR, —C(R), or another amine protecting group, wherein Rand Rdefined as in above,'}{'sup': '2', 'sub': 1', '6', '2', '6', '2', '6', '1', '6', '3', '3', '2, 'Ris C-Calkyl, C-Calkenyl, or C-Calkynyl, wherein the alkyl, alkenyl, or the alkynyl group is optionally substituted with 1-3 substituents selected from the group consisting of keto, halo, C-Calkoxy, amino, hydroxy, cyano, nitro, —NHCOCH, —N, and —COH or an ester thereof, and'}{'sup': '3', 'Zis hydroxy or hydrogen.'}7. The compound of claim 5 , which is an R claim 5 ,R enantiomer.8. An isolated R claim 7 ,R enantiomer of the compound of claim 7 , which is in substantial enantiomeric excess (ee). This application claims the benefit under 35 U.S.C. 119(e) of U.S. Provisional Application Ser. No. 61/741,798 filed Jan. 25, 2012, which is hereby incorporated by reference into this application in its entirety.This invention provides (1R,4R) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene as well as derivatives thereof. Such compounds are readily converted into pharmaceutically important compounds containing the isoquinuclidene moiety. In one embodiment, the 7-oxo-2-azabicyclo[2.2.2]oct-5-ene compounds of this invention are in substantially enantiomerically enriched forms. This invention also provides for processes for preparing such 7-oxo-2-azabicyclo[2.2.2]oct-5-ene compounds as well as for preparing novel intermediates used therein.Many pharmaceutical compounds mirror the structures of natural products. In particular, certain aspects of the natural product are modified in order to enhance beneficial ...

BROMODOMAIN INHIBITORS AND USES THEREOF

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders. 2. The compound according to claim 1 , wherein Ring A is benzo claim 1 , pyrido claim 1 , pyrimidino claim 1 , pyrazino claim 1 , pyridazino claim 1 , thieno claim 1 , or isothiazolo.39-. (canceled)10. The compound according to claim 1 , wherein Ring B is phenyl.11. (canceled)12. The compound according to claim 1 , wherein Lis a covalent bond.13. The compound according to claim 1 , wherein Ris halogen or optionally substituted Caliphatic.1418-. (canceled)19. The compound according to claim 1 , wherein Rand Rof formula are taken together with their intervening atoms to form an optionally substituted 3-7 membered saturated or partially unsaturated spiro-fused ring having 0-2 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , or sulfur.20. (canceled)21. The compound according to claim 1 , wherein Rand X are taken together with their intervening atoms to form an optionally substituted 5-membered heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen claim 1 , oxygen claim 1 , or sulfur.22. The compound according to claim 1 , wherein Rand X are taken together with their intervening atoms to form an optionally substituted triazolyl ring.25. The compound according to claim 24 , wherein Ring A is pyrimidino claim 24 , pyrazino claim 24 , isothiazolo claim 24 , or pyridazino.26. (canceled)27. (canceled)28. The compound according to claim 24 , wherein Ring B is phenyl.29. (canceled)30. The compound according to claim 24 , wherein Lis a covalent bond.31. The compound according to claim 24 , wherein Ris hydrogen claim 24 , halogen claim 24 , or optionally substituted Caliphatic.3238-. (canceled)39. The compound according to claim 24 , wherein ...

Tetracarboxylic Acid Dianhydride and Method for Preparing the Same

Provided are a novel tetracarboxylic acid dianhydride and a method for preparing the same. According to an exemplary embodiment of the present invention, a novel tetracarboxylic acid dianhydride appropriate for providing a polyimide film having high transparency and thermal resistance and having excellent thermal dimensional stability due to a substrate of which the stress is not increased even with a heat treatment at a high temperature and a method for preparing the same may be provided. 4. The tetracarboxylic acid dianhydride of claim 1 , wherein in Chemical Formula 1 claim 1 , Rand Rare independently of each other a halogen claim 1 , hydroxy claim 1 , thiol claim 1 , nitro claim 1 , cyano claim 1 , C1-C10 alkyl claim 1 , C1-C10 alkoxy claim 1 , C6-C20 aryl claim 1 , C1-C10 haloalkyl claim 1 , or C1-C10 haloalkoxy claim 1 , and n and m are independently of each other an integer selected from 0 to 2.5. The tetracarboxylic acid dianhydride of claim 1 , wherein in Chemical Formula 1 claim 1 , Rand Rare independently of each other a halogen claim 1 , hydroxy claim 1 , thiol claim 1 , nitro claim 1 , cyano claim 1 , C1-C4 alkyl claim 1 , C1-C4 alkoxy claim 1 , C6-C18 aryl claim 1 , C1-C4 haloalkyl claim 1 , or C1-C4 haloalkoxy claim 1 , and n and m are independently of each other an integer selected from 0 to 2.6. The tetracarboxylic acid dianhydride of claim 1 , wherein in Chemical Formula 1 claim 1 , Rand Rare independently of each other a halogen claim 1 , nitro claim 1 , cyano claim 1 , C1-C4 alkyl claim 1 , C1-C4 alkoxy claim 1 , C6-C12 aryl claim 1 , C1-C4 haloalkyl claim 1 , or C1-C4 haloalkoxy claim 1 , and n and m are independently of each other an integer selected from 0 to 2 and satisfy 0≤n+m≤2.9. The method for preparing a tetracarboxylic acid dianhydride of claim 8 , wherein the dehydrating agent is an acid anhydride.10. A composition comprising the tetracarboxylic acid dianhydride of .11. The composition of claim 10 , further comprising: an organic ...

Polyimide Precursor, Polyimide Precursor Composition, Polyimide Film, Method for Preparing the Same, and Use Thereof

Provided are a polyimide precursor, a polyimide precursor solution, a polyimide film, a method for preparing the same, and a use thereof. According to an exemplary embodiment of the present invention, a polyimide film having excellent thermal resistance and satisfying transparency and a low coefficient of linear thermal expansion may be provided, and thus, may be usefully applied in a flexible display field requiring high dimensional stability and the like. 3. The polyimide precursor solution of claim 1 , wherein the polyimide precursor solution includes: a polymerization component including the tetracarboxylic acid dianhydride represented by Chemical Formula 1 and a diamine; and an organic solvent.5. The polyimide precursor solution of claim 3 , wherein the organic solvent is selected from amides.6. The polyimide precursor solution of claim 5 , wherein the organic solvent is N claim 5 ,N-diethylacetamide claim 5 , N claim 5 ,N-diethylformamide claim 5 , N-ethylpyrrolidone claim 5 , N claim 5 ,N-dimethylpropionamide claim 5 , N claim 5 ,N-diethylpropionamide claim 5 , or a combination thereof.10. The polyimide precursor of claim 9 , wherein the polyimide precursor includes 10 to 100 mol % of the repeating unit represented by Chemical Formula a claim 9 , based on total repeating units.13. The polyimide film of claim 11 , wherein the polyimide film has a coefficient of thermal expansion (CTE) of 50 ppm/° C. or less at 100 to 450° C.14. The polyimide film of claim 11 , wherein the polyimide film hasYI in accordance with ASTM E313 of 15 or less;a haze in accordance with ASTM D1003 of 2 or less; anda total light transmittance in a region of 380 to 780 nm in accordance with ASTM D1746 of 80% or more.15. The polyimide film of claim 11 , wherein the polyimide film has a modulus in accordance with ASTM D882 of 5.0 or more and an elongation of 15% or more.16. The polyimide film of claim 11 , wherein the polyimide film hasa coefficient of thermal expansion of 50 ppm/° C. or ...

Compounds useful for inhibiting ror-gamma-t

The present invention provides novel ROR gamma-t inhibitors and pharmaceutical compositions thereof. Formula (I).

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.

Organic compound, organic light emitting diode and organic light emitting device including the organic compound

The present disclosure relates to an organic compound having the following structure, and an organic light emitting diode (OLED) and an organic light emitting device including the organic compound. The organic compound is a bipolar compound having a p-type moiety and an n-type moiety and has high energy level and proper energy bandgap for an emissive layer of the OLED. As the organic compound is applied into the emissive layer, the OLED can maximize its luminous properties as holes and electrons are recombined uniformly over the whole area in an emitting material layer (EML).

COMPOUNDS USEFUL FOR INHIBITING ROR-GAMMA-T

The present invention provides novel ROR gamma-t inhibitors and pharmaceutical compositions thereof, formula (A). 6. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients7. The pharmaceutical composition according to comprising one or more other therapeutic agents.8. A method of treating psoriasis comprising administering a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to a patient in need thereof.9. A method of treating seronegative spondylarthropathies comprising administering a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to a patient in need thereof.10. The method according to for treating axial spondyloarthritis claim 9 , ankylosing spondylitis claim 9 , or psoriatic arthritis.11. (canceled)12. (canceled)13. (canceled)14. (canceled)15. (canceled)16. (canceled)17. (canceled)18. The compound according to wherein Ris ethyl.19. The compound according to wherein Ris methyl.20. The compound according to wherein Ris —CH.21. The compound according to wherein Ris —CH.22. The compound according to wherein Rand Rare —H and —H.23. The compound according to wherein Rand Rare —H and —CH. The present invention relates to compounds useful for inhibiting retinoic acid receptor-related orphan receptor gamma-t (RORγt), pharmaceutical compositions, and methods for treating diseases related to RORγ activity.The retinoic acid receptor-related orphan receptors (RORs) are members of the nuclear receptor (NR) superfamily identified as important pathological regulators in many diseases. The ROR subfamily consists of RORα, RORβ, and RORγ. The mouse and human RORγ gene generates two isoforms, yl and y2, the latter most commonly referred to as γt. RORγt signaling, often in response to IL-23/IL-23 receptor signaling, is required for the differentiation ...

COMPOUNDS USEFUL FOR INHIBITING ROR-GAMMA-T

The present invention provides novel ROR gamma-t inhibitors and pharmaceutical compositions thereof: 4. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , in combination with one or more pharmaceutically acceptable carriers claim 1 , diluents claim 1 , or excipients5. The pharmaceutical composition according to comprising one or more other therapeutic agents.6. A method of treating psoriasis comprising administering a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to a patient in need thereof.7. A method of treating seronegative spondylarthropathies comprising administering a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to a patient in need thereof.8. The method according to for treating axial spondyloarthritis claim 7 , ankylosing spondylitis claim 7 , or psoriatic arthritis. The present invention relates to compounds useful for inhibiting retinoic acid receptor-related orphan receptor gamma-t (RORγt), pharmaceutical compositions, and methods for treating diseases related to RORγ activity.The retinoic acid receptor-related orphan receptors (RORs) are members of the nuclear receptor (NR) superfamily identified as important pathological regulators in many diseases. The ROR subfamily consists of RORα, RORβ, and RORγ. The mouse and human RORγ gene generates two isoforms, γ1 and γ2, the latter most commonly referred to as γt. RORγt signaling, often in response to IL-23/IL-23 receptor signaling, is required for the differentiation of naive CD4+ T-cells into a subset of T-cells designated Th17, which are distinct from the classical Th1 and Th2 cells, and supports their maintenance. Th17 cells produce interleukin-17A (IL-17) and IL-17F. In addition, Th17 cells produce a range of other factors known to drive inflammatory responses, including tumor necrosis factor-alpha (TNF-α), interleukin-6 (IL-6), GM-CSF, CXCL1 and CCL20. NK cells and innate ...

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 ...

SPIRO COMPOUND AND ORGANIC LIGHT-EMITTING ELEMENT COMPRISING SAME

The present specification provides a compound having a spiro structure and an organic light emitting device including the same. 5. The compound of claim 1 , wherein X is NAr and Ar is represented by —(L)n-Ar claim 1 ,{'sub': 1', '1, "Lis a direct bond; a substituted or unsubstituted arylene group; or a substituted or unsubstituted heteroarylene, n is an integer from 0 to 2, and when n is 2, L's are the same as or different from each other, and"}{'sub': '1', 'Aris hydrogen; deuterium; a halogen group; a nitrile group; a nitro group; a hydroxy group; a carbonyl group; an ester group; an imide group; an amino group; a substituted or unsubstituted silyl group; a substituted or unsubstituted boron group; a substituted or unsubstituted alkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted alkoxy group; a substituted or unsubstituted aryloxy group; a substituted or unsubstituted alkylthioxy group; a substituted or unsubstituted arylthioxy group; a substituted or unsubstituted alkylsulfoxy group; a substituted or unsubstituted arylsulfoxy group; a substituted or unsubstituted alkenyl group; a substituted or unsubstituted aralkyl group; a substituted or unsubstituted aralkenyl group; a substituted or unsubstituted alkylaryl group; a substituted or unsubstituted alkylamino group; a substituted or unsubstituted aralkylamino group; a substituted or unsubstituted heteroarylamino group; a substituted or unsubstituted arylamino group; a substituted or unsubstituted arylheteroarylamino group; a substituted or unsubstituted arylphosphine group; a substituted or unsubstituted phosphine oxide group; a substituted or unsubstituted aryl group; or a substituted or unsubstituted heterocyclic group.'}6. The compound of claim 5 , wherein Aris a substituted or unsubstituted aryl group; a substituted or unsubstituted heterocyclic group; a substituted or unsubstituted arylamino group; or a substituted or unsubstituted arylphosphine group.7. The compound ...

MNK INHIBITORS AND METHODS RELATED THERETO

The present invention relates to compounds according to Formula (I): 1. A method for treating a disease or condition in a mammal in need thereof , the method comprising administering to the mammal a therapeutically effective amount of at least one MAP kinase interacting kinase (Mnk) inhibitor and at least one other therapeutic agent , wherein the at least one other therapeutic agent is other than the at least one Mnk inhibitor.2. The method of claim 1 , wherein the mammal is a human.3. The method of claim 1 , wherein the at least one other therapeutic agent is an anti-cancer agent.4. The method of claim 3 , wherein the anti-cancer agent is a chemo-therapeutic drug.5. The method of claim 3 , wherein the anti-cancer agent is selected from folate antagonists claim 3 , antiproliferative agents claim 3 , antimitotic agents claim 3 , microtubule inhibiting agents claim 3 , DNA damaging agents claim 3 , DNA synthesis inhibitors claim 3 , DNA interactive agents claim 3 , DNA repair inhibitors claim 3 , antiplatelet agents claim 3 , antimetabolites claim 3 , hormones claim 3 , hormone analogs claim 3 , aromatase inhibitors claim 3 , fibrinolytic agents claim 3 , antimigratory agents claim 3 , antisecretory agents claim 3 , immunosuppressives claim 3 , anti-angiogenic compounds claim 3 , growth factor inhibitors claim 3 , angiotensin receptor blocker claim 3 , nitric oxide donors claim 3 , anti-sense oligonucleotides claim 3 , antibodies claim 3 , chimeric antigen receptors claim 3 , cell cycle inhibitors claim 3 , differentiation inducers claim 3 , mTOR inhibitors claim 3 , topoisomerase inhibitors claim 3 , corticosteroids claim 3 , growth factor signal transduction kinase inhibitors claim 3 , mitochondrial dysfunction inducers claim 3 , caspase activators claim 3 , and inhibitors of chromatin function.7. The method of claim 6 , wherein n is 1.8. The method of claim 6 , wherein Rand Rtaken together with the carbon atom to which they are attached form a cycloalkyl or ...

PHOTOACTIVE COMPOUNDS FOR VAPOR DEPOSITED ORGANIC PHOTOVOLTAIC DEVICES

Photoactive compounds are disclosed. The disclosed compounds can exhibit molecular structural elements tending to increase the evaporability of the compounds, such as by including geometric core disruption by use of conformationally restricted side groups instead of freely rotatable side groups or use of indandione moieties instead of dicyanomethyleneindanone moieties. The disclosed photoactive compounds include those with an imine-bridging linking moiety, which can shift the optical properties to a more red-shifted absorbance as compared to compounds with an alkene-bridging linking moiety. The disclosed photoactive compounds can be used in organic photovoltaic devices, such as visibly transparent or opaque photovoltaic devices.

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.

DELAYED FLUORESCENCE COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE USING THE SAME

The present invention discloses a delayed fluorescence compound and the organic electroluminescent device employing the delayed fluorescence compound as the delayed fluorescence dopant material, the delayed fluorescence host material, or the phosphorescent host material in the light emitting layer, and/or used in the hole blocking layer and/or the electron transporting layer of the organic EL device, which thereby displays good performance. 5. The delayed fluorescence compound of claim 1 , wherein a difference between a singlet energy of the delayed fluorescence compound and a triplet energy of the delayed fluorescence compound is less than 0.3 eV.6. The delayed fluorescence compound of claim 1 , wherein the delayed fluorescence compound is used as a light-emitting material.7. An organic electroluminescent device claim 1 , comprising a pair of electrodes composed of a cathode and an anode claim 1 , and a light emitting layer and one or more organic thin film layers between the pair of electrodes claim 1 , wherein at least one of the light emitting layer and the organic thin film layer comprises the delayed fluorescence compound of .8. The organic electroluminescent device of claim 7 , wherein the light emitting layer comprising the delayed fluorescence compound is a delayed fluorescence host material.9. The organic electroluminescent device of claim 8 , wherein the light emitting layer further comprises a second fluorescence host material.10. The organic electroluminescent device of claim 9 , wherein the second fluorescence host material is H1.11. The organic electroluminescent device of claim 7 , wherein the light emitting layer comprising the delayed fluorescence compound is a phosphorescent host material.12. The organic electroluminescent device of claim 7 , wherein the light emitting layer further includes a host material claim 7 , and the delayed fluorescence compound is used as a dopant material.13. The organic electroluminescent device of claim 12 , wherein ...

PHOTOACTIVE COMPOUNDS FOR VAPOR DEPOSITED ORGANIC PHOTOVOLTAIC DEVICES

Photoactive compounds are disclosed. The disclosed compounds can exhibit molecular structural elements tending to increase the evaporability of the compounds, such as by including geometric core disruption by use of conformationally restricted side groups instead of freely rotatable side groups or use of indandione moieties instead of dicyanomethyleneindanone moieties. The disclosed photoactive compounds include those with an imine-bridging linking moiety, which can shift the optical properties to a more red-shifted absorbance as compared to compounds with an alkene-bridging linking moiety. The disclosed photoactive compounds can be used in organic photovoltaic devices, such as visibly transparent or opaque photovoltaic devices. 2. The photoactive compound of claim 1 , having a molecular weight of from 250 atomic mass units to 1200 atomic mass units.3. The photoactive compound of claim 1 , characterized by or exhibiting a sublimation purification yield by mass of 20% or greater.4. The photoactive compound of claim 1 , having a thermal decomposition temperature of from 200° C. to 500° C.5. The photoactive compound of claim 1 , exhibiting a bandgap of 0.5 eV to 4.0 eV.6. The photoactive compound of claim 1 , exhibiting a sublimation temperature of from 150° C. to 450° C. at pressures of from 0.2 Torr to 10Torr.7. The photoactive compound of claim 1 , wherein the central core comprises an aromatic claim 1 , heteroaromatic claim 1 , polycyclic aromatic claim 1 , or polycyclic heteroaromatic moiety including one or more 5-membered rings claim 1 , one or more 6-membered rings claim 1 , or a combination of one or more 5-membered rings and one or more 6-membered rings.8. The photoactive compound of claim 1 , wherein the central core comprises one or more quaternary carbons.12. The photoactive compound of claim 1 ,wherein each Z is independently an unsubstituted or methyl, ethyl, fluoro, or trifluoromethyl substituted cycloalkyl group, an unsubstituted or methyl, ethyl, ...

Thienopyrimidine inhibitors of atypical protein kinase c

or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have a PKC inhibitory activity, and may be used to treat proliferative disorders.

DETECTION AND USE OF LOW MOLECULAR-WEIGHT MODULATORS OF THE COLD-MENTHOL RECEPTOR TRPM8

The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators. 1. A method for the in-vitro or in-vivo modulation of the cold menthol receptor TRMP8 , comprising contacting the receptor with at least one compound which is selected from polynuclear organic compounds which , in a cellular activity test using cells which recombinantly express the human TRPM8 receptor , modulate the permeability of these cells for Caions.2. The method according to claim 1 , where the compound has at least two 4- to 7-membered rings which claim 1 , independently of one another claim 1 , are carbo- or heterocyclic claim 1 , mono- or polycyclic claim 1 , and wherein at least two of these rings can optionally be condensed.3. The method according to claim 1 , wherein the modulator has an agonistic or antagonistic effect on the cellular Caion permeability.5. A modulator for the TRPM8 receptor which is selected from polynuclear organic compounds which claim 1 , in a cellular activity test using a cell which recombinantly expresses the human TRPM8 receptor claim 1 , modulates the permeability of the cell for Caions.6. The use of a modulator for the TRPM8 receptor according to for inducing a sensation of coldness in humans and/or animals.7. The use of a modulator for the TRPM8 receptor according to as an active constituent of a pharmaceutical composition.8. The use of a modulator for the TRPM8 receptor according to for the treatment of prostate carcinomas claim 5 , for the treatment of bladder weakness or in pain therapy.9. The use of a modulator for the TRPM8 receptor according to as insect repellent or insecticide.10. The use of a modulator for the TRPM8 receptor according to for inducing a sensation of coldness in a packaging.11. The use of a modulator for the TRPM8 receptor according to for ...

SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. 12.-. (canceled)411.-. (canceled)12. The compound of wherein Z is —O— or —N(H)— and Ris hydrogen or methyl.13. The compound of selected from:1′-[2-(trifluoromethyl)benzyl]-1H-spiro[furo[3,2-f]indazole-5,3′-indol]-2′(1′H)-one;1′-(pyridin-2-ylmethyl)-1H-spiro[furo[3,2-f]indazole-5,3′-indol]-2′(1′H)-one;1′-((3-(trifluoromethyl)pyridin-2-yl)methyl)-1,6-dihydrospiro[furo[3,2-f]indazole-5,3′-indolin]-2′-one;1′-(4-methoxybenzyl)-3-methylspiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methylspiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-{[5-(trifluoromethyl)furan-2-yl]methyl}spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-(pyridin-2-ylmethyl)spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-(pyridin-3-ylmethyl)spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-[(2R)-tetrahydrofuran-2-ylmethyl]spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;1′-(4-isoxazol-5-ylbenzyl)-3-methylspiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-[2-(trifluoromethyl)benzyl]spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-{[3-(trifluoromethyl)pyridin-2-yl]methyl}spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;1′-[2-(2-methoxyethoxy)ethyl]-3-methylspiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-(3-methylbutyl)spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;3-methyl-1′-(pyrazin-2-ylmethyl)spiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;1′-[(3-fluoropyridin-2-yl)methyl]-3-methylspiro[furo[3,2-f][1,2]benzisoxazole-5,3′-indol]-2′(1′H)-one;methyl 2-[(3-methyl-2′-oxospiro[furo[3,2-f][1,2] ...

POLYHETEROAROMATIC COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

The present invention discloses a novel polyheteroaromatic compound derived from 7′,7′-dimethyl-5′,7′-dihydrospiro[cyclopenta[1,2-b:5,4-b′-dithiophene-4,13′-indeno[1,2-b]acridine] core structures. The polyheteroaromatic compound can be used as organic electroluminescence materials for use in an organic electroluminescence device and electronic equipment. 4. The polyheteroaromatic compound according to claim 3 , wherein Ror Rrepresents one of the following substituents:6. An organic electroluminescence device claim 1 , comprising a pair of electrodes composed of a cathode and an anode claim 1 , and a light emitting layer and one or more organic thin film layers between the pair of electrodes claim 1 , wherein at least one of the light emitting layer and the organic thin film layer comprises the polyheteroaromatic compound according to .7. The organic electroluminescence device according to claim 6 , wherein the light emitting layer comprising the polyheteroaromatic compound of formula (1) is a host material.8. The organic electroluminescence device according to claim 6 , wherein the light emitting layer comprising the polyheteroaromatic compound of formula (1) is a fluorescent dopant material.9. The organic electroluminescence device according to claim 6 , wherein the light emitting layer comprising the polyheteroaromatic compound of formula (1) is a thermally activated delayed fluorescence host material.10. The organic electroluminescence device according to claim 6 , wherein the light emitting layer comprising the polyheteroaromatic compound of formula (1) is a thermally activated delayed fluorescence dopant material.11. The organic electroluminescence device according to claim 6 , wherein the organic thin film layer comprising the polyheteroaromatic compound of formula (1) is an electron transporting layer.12. The organic electroluminescence device according to claim 6 , wherein the organic electroluminescence device is a lighting panel.13. The organic ...

MULTICYCLIC COMPOUNDS AND METHODS OF USE THEREOF

Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia. 139-. (canceled)44. A pharmaceutical composition comprising a compound of claim 40 , or a pharmaceutically acceptable salt or stereoisomer thereof claim 40 , and a pharmaceutically acceptable excipient or carrier.45. The pharmaceutical composition of claim 44 , which further comprises one or more additional active agents.46. A method of treating claim 40 , preventing claim 40 , or managing a neurological disorder claim 40 , comprising administering to a subject a therapeutically or prophylactically effective amount of a compound of claim 40 , or a pharmaceutically acceptable salt or stereoisomer thereof.47. The method of claim 46 , wherein said subject is a human.48. The method of claim 46 , wherein the disorder is schizophrenia claim 46 , schizophrenia spectrum disorder claim 46 , acute schizophrenia claim 46 , chronic schizophrenia claim 46 , NOS schizophrenia claim 46 , schizoid personality disorder claim 46 , schizotypal personality disorder claim 46 , delusional disorder claim 46 , psychosis claim 46 , psychotic disorder claim 46 , brief psychotic disorder claim 46 , shared psychotic disorder claim 46 , psychotic disorder due to a general medical condition claim 46 , drug-induced psychosis claim 46 , psychoaffective disorder claim 46 , aggression claim 46 , delirium claim 46 , Parkinson's psychosis claim 46 , excitative psychosis claim 46 , Tourette's syndrome claim 46 , organic or NOS psychosis claim 46 , seizure claim 46 , agitation claim 46 , post-traumatic stress disorder claim 46 , behavior disorder claim 46 , neurodegenerative disease claim 46 , Alzheimer's disease claim 46 , Parkinson's disease claim 46 , dyskinesias claim 46 ...

MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES

The invention relates to compounds which are suitable for use in electronic devices, and to electronic devices, in particular organic electroluminescent devices, containing said compounds. 114.-. (canceled)17. The compound as claimed in claim 15 , wherein p is the same or different at each instance and is 0 or 1.20. The compound as claimed in claim 15 , wherein A is oxygen.22. The compound as claimed in claim 15 , wherein Ar is selected from the group consisting of phenyl claim 15 , biphenyl claim 15 , terphenyl claim 15 , quaterphenyl claim 15 , fluorene claim 15 , spirobifluorene claim 15 , naphthalene claim 15 , indole claim 15 , benzofuran claim 15 , benzothiophene claim 15 , carbazole claim 15 , dibenzofuran claim 15 , dibenzothiophene claim 15 , indenocarbazole claim 15 , indolocarbazole claim 15 , pyridine claim 15 , pyrimidine claim 15 , pyrazine claim 15 , pyridazine claim 15 , triazine claim 15 , phenanthrene claim 15 , triphenylene and combinations of two or three of these groups claim 15 , where these groups may each be substituted by one or more R radicals.23. The compound as claimed in claim 15 , wherein R is the same or different at each instance and is selected from the group consisting of H claim 15 , D claim 15 , F claim 15 , CN claim 15 , N(Ar) claim 15 , C(═O)Ar claim 15 , P(═O)(Ar) claim 15 , a straight-chain alkyl or alkoxy group having 1 to 10 carbon atoms or a branched or cyclic alkyl or alkoxy group having 3 to 10 carbon atoms or an alkenyl group having 2 to 10 carbon atoms claim 15 , each of which may be substituted by one or more Rradicals claim 15 , where one or more nonadjacent CHgroups may be replaced by O and where one or more hydrogen atoms may be replaced by D or F claim 15 , or an aromatic or heteroaromatic ring system which has 5 to 30 aromatic ring atoms and may be substituted in each case by one or more Rradicals.24. A process for preparing the compound as claimed in claim 15 , comprising the reaction steps of:a) synthesizing the ...

METHODS AND COMPOSITIONS FOR CELLULAR IMMUNOTHERAPY

The present disclosure relates to genetically modified T cells comprising a transgene encoding an engineered antigen specific receptor, wherein expression of an endogenous gene selected from MNK1, MNK2, or both are inhibited in the genetically modified T cell in order to enhance central memory T cell subsets in cellular immunotherapy compositions. 1. A modified T cell , comprising a chromosomal MNK gene knock out , wherein the MNK gene comprises the MNK1 gene , the MNK2 gene , or both; optionally further comprising a transgene encoding an engineered antigen specific receptor.26-. (canceled)7. The modified T cell of claim 1 , wherein the encoded engineered antigen specific receptor is a chimeric antigen receptor (CAR) claim 1 , a T cell receptor (TCR) claim 1 , a TCR-CAR claim 1 , or any combination thereof.8. The modified T cell of claim 7 , wherein the encoded CAR comprises a binding domain comprising an scFv that specifically binds to the antigen.9. The modified T cell of claim 7 , wherein the encoded CAR comprises at least one signaling domain.10. The modified T cell of claim 7 , wherein the encoded T cell receptor is an enhanced affinity TCR.11. The modified T cell of claim 7 , wherein the encoded TCR is an αβ TCR or a γδ TCR.12. The modified T cell of claim 1 , wherein both MNK1 and MNK2 are knocked out.13. The modified T cell of claim 1 , wherein the antigen is a tumor antigen claim 1 , a pathogenic microorganism antigen claim 1 , or an autoimmune disease antigen.14. The modified T cell of claim 13 , wherein the tumor antigen is selected from the group consisting of human immunodeficiency virus (HIV) antigens claim 13 , hepatitis C virus (HCV) antigens claim 13 , hepatitis B virus (HBV) antigens claim 13 , cytomegalovirus (CMV) antigens claim 13 , Epstein Barr virus (EBV) antigens claim 13 , parasitic antigens claim 13 , and tumor antigens claim 13 , such as ROR1 claim 13 , EGFR claim 13 , EGFRvIII claim 13 , HPV E6 claim 13 , HPV E7 claim 13 , L1-CAM claim 13 ...

Substituted thienopyrimidines and pharmaceutical use thereof

The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.

THIENOPYRIMIDINE INHIBITORS OF ATYPICAL PROTEIN KINASE C

The present application provides a compound of formula (I) 2. The compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein Rand Rare H.3. The compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein Ris H.4. The compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein R claim 1 , Rand Rare H.5. The compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein Ris selected from Calkyl optionally substituted by 1-13 Rand Carylalkyl optionally substituted by 1-9 R.6. The compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein Ris H.7. The compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein Ris selected from Calkyl claim 1 , phenyl claim 1 , Ccycloalkyl claim 1 , halogen and —OR.8. The compound claim 1 , or pharmaceutically acceptable salt thereof claim 1 , according to wherein R claim 1 , R claim 1 , R claim 1 , and Rare independently chosen from H and halogen.13. The method according to wherein the cancer is selected from squamous cell carcinoma claim 12 , leukemia claim 12 , prostate cancer claim 12 , non-Hodgkin's lymphoma claim 12 , endometrial cancer claim 12 , lung cancer and breast cancer.14. The method according to wherein the lung cancer is non-small cell lung cancer.15. The method according to wherein the squamous cell carcinoma is esophageal squamous cell carcinoma.16. The method according to wherein the non-Hodgkin's lymphoma is follicular lymphoma. This application is a continuation of U.S. application Ser. No. 14/285,007, filed May 22, 2014, which is a U.S. National Phase application under 35 U.S.C. §371 of International Patent Application No. PCT/US2012/065831, filed Nov. 19, 2012, which claims the benefit of U.S. Provisional Application No. 61/563,310, filed Nov. 23, 2011, the content of each of which is incorporated herein by ...

Multicyclic Compounds and Methods of Use Thereof

Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

Spiro compound and organic light-emitting element comprising same

The present specification provides a compound having a spiro structure and an organic light emitting device including the same.

Novel compound or pharmaceutically acceptable salt thereof

Provided are 2-(piperidin-1-yl)pyrimidin-4(3H)-ones or pharmaceutically acceptable salts thereof, each characterized by having a 1,8-diazaspiro[4.5]deca-3-ene, 1-oxa-8-azaspiro[4.5]deca-3-ene, 2,8-diazaspiro[4.5]deca-3-ene, 2-oxa-8-azaspiro[4.5]deca-3-ene, 2,9-diazaspiro[5.5]undeca-3-ene, 1-oxa-9-azaspiro[5.5]undeca-3-ene, 1,9-diazaspiro[5.5]undeca-4-ene, or 3,9-diazaspiro[5.5]undeca-1-ene structure represented by the following general formula (1):

THIENO [2, 3-B] PYRIDINE DERIVATIVES AS VIRAL REPLICATION INHIBITORS

The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity. 3. The compound according to claim 1 , wherein Ris —COOH.4. The compound according to claim 1 , wherein Ris selected from aryl or heteroaryl claim 1 , wherein said aryl or heteroaryl can be unsubstituted or substituted with one or more Z.5. The compound according to claim 1 , wherein one of Rand Ris hydrogen claim 1 , and the other of Rand Ris selected from cyano; alkyl; alkenyl; alkynyl; arylalkyl; arylalkenyl; arylalkynyl; heterocycle-alkyl; heterocycle-alkenyl; or heterocycle-alkynyl;wherein said alkyl, alkenyl, alkynyl, arylalkyl; arylalkenyl; arylalkynyl; heterocycle-alkyl; heterocycle-alkenyl; or heterocycle-alkynyl optionally includes one or more heteroatoms, said heteroatoms in the alkyl, alkenyl or alkynyl moiety being selected from the atoms O, S and N;{'sup': '1', 'wherein said alkyl, alkenyl, alkynyl, arylalkyl; arylalkenyl; arylalkynyl; heterocycle-alkyl; heterocycle-alkenyl; or heterocycle-alkynyl vinyl or vinylalkyl, can be unsubstituted or substituted with one or more Z;'}{'sub': '2', 'and wherein optionally a carbon atom or heteroatom of said alkyl, alkenyl, alkynyl, ...

ORGANIC ELECTROLUMINESCENT COMPOUNDS AND ORGANIC ELECTROLUMINESCENT DEVICES COMPRISING THE SAME

The present invention relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. By using the organic electroluminescent compound of the present invention, it is possible to produce an organic electroluminescent device having low driving voltage and excellent luminous efficiency such as current efficiency and power efficiency, emitting color of high purity, and having improved lifespan. 2. The organic electroluminescent compound according to claim 1 , wherein the substituents of the substituted alkyl group claim 1 , the substituted aryl group claim 1 , the substituted heteroaryl group claim 1 , the substituted cycloalkyl group claim 1 , the substituted alkoxy group claim 1 , the substituted trialkylsilyl group claim 1 , the substituted dialkylarylsilyl group claim 1 , the substituted alkyldiarylsilyl group claim 1 , the substituted triarylsilyl group claim 1 , the substituted mono- or di-alkylamino group claim 1 , the substituted mono- or di-arylamino group claim 1 , the substituted alkylarylamino group claim 1 , and the substituted mono- or polycyclic claim 1 , alicyclic or aromatic ring in Rto Reach independently are at least one selected from the group consisting of deuterium claim 1 , a halogen claim 1 , a cyano claim 1 , a carboxyl claim 1 , a nitro claim 1 , a hydroxyl claim 1 , a (C1-C30)alkyl claim 1 , a halo(C1-C30)alkyl claim 1 , a (C1-C30)alkoxy claim 1 , a (C1-C30)alkylthio claim 1 , a (C3-C30)cycloalkyl claim 1 , a 3- to 7-membered heterocycloalkyl claim 1 , a (C6-C30)aryloxy claim 1 , a (C6-C30)arylthio claim 1 , a 3- to 30-membered heteroaryl unsubstituted or substituted with a (C6-C30)aryl claim 1 , a (C6-C30)aryl unsubstituted or substituted with a 3- to 30-membered heteroaryl claim 1 , a tri(C1-C30)alkylsilyl claim 1 , a tri(C6-C30)arylsilyl claim 1 , a di(C1-C30)alkyl(C6-C30)arylsilyl claim 1 , a (C1-C30)alkyldi(C6-C30)arylsilyl claim 1 , an amino claim 1 , a mono- or di-(C1-C30)alkylamino claim ...

Spirothienopyran-piperidine derivatives as orl-1 receptor antagonists for their use in the treatment of alcohol dependence and abuse

The use of ORL-1 receptor antagonists of the formula: for the treatment of alcohol use disorders is described.

MNK INHIBITORS AND METHODS RELATED THERETO

The present invention relates to compounds according to Formula (I): 119-. (canceled)21. The method of wherein the pharmaceutically acceptable salt is an organic or inorganic acid salt selected from the group consisting of acetate claim 20 , mesylate claim 20 , sulfate claim 20 , citrate claim 20 , oxalate claim 20 , hydrochloride claim 20 , dihydrochloride claim 20 , isothionate claim 20 , lactate claim 20 , and laurate.22. The method of wherein the pharmaceutically acceptable salt is hydrochloride.23. The method of wherein the mammal is a human.25. The process according to claim 24 , wherein Ris alkyl.26. The process according to claim 24 , wherein X is halogen.27. The process according to claim 26 , wherein the halogen is bromine.28. The process according to claim 24 , wherein Y is alkyl.29. The process according to claim 24 , wherein in step (a) the acid is hydrochloric claim 24 , sulfuric claim 24 , or p-toluenesulfonic.30. The process according to claim 24 , wherein in step (d) the conditions suitable to amidate an ester comprise contact with ammonia.32. The process according to claim 31 , wherein in step (b) the metal catalyst is a palladium catalyst claim 31 , the inorganic base is CsCO claim 31 , and the phosphine ligand is xantphos.33. The process according to claim 32 , wherein the palladium catalyst is Pd(dba)or Pd(OAc).34. The process according to claim 32 , wherein the non-polar aprotic solvent is 1 claim 32 ,4-dioxane.35. The process according to claim 32 , wherein the reaction temperature is between 90° C. and 105° C.36. The process according to claim 31 , wherein X is halogen.37. The process according to claim 36 , wherein the halogen is chlorine.38. The process according to claim 31 , wherein R′ is cycloalkyl.39. The process according to claim 38 , where the cycloalkyl is cyclopropyl. The present application is a continuation of U.S. patent application Ser. No. 15/809,011, filed Nov. 10, 2017, which is a continuation of U.S. patent application Ser. ...

Thienopyrimidine Inhibitors of Atypical Protein Kinase C

The present application provides a compound of formula (I) 2. A compound as defined in claim 1 , wherein A is NR.5. A compound as defined in claim 1 , wherein R claim 1 , R claim 1 , and Rare independently chosen from H and Calkyl optionally substituted by 1-3 R; R claim 1 , R claim 1 , R claim 1 , and Rare independently chosen from H claim 1 , Calkyl optionally substituted by 1-3 R claim 1 , halogen claim 1 , —CN claim 1 , —C(═O)R claim 1 , —C(═O)OR claim 1 , —C(═O)NRR claim 1 , —NO claim 1 , —NRR claim 1 , —NRC(O)R claim 1 , —NRS(═O)R claim 1 , OR claim 1 , OC(O)R claim 1 , S(O)R claim 1 , and S(═O)NRR; alternatively claim 1 , Rand Rcan claim 1 , together with the atoms linking them claim 1 , form a Caryl optionally substituted by 1-3 R claim 1 , Ccycloalkyl optionally substituted by 1-3 R claim 1 , 3-10 membered heterocycloalkyl optionally substituted by 1-3 Ror a 5-10 membered heteroaryl optionally substituted by 1-3 R; alternatively Rand Ror Rand Rcan together form a double bond; and alternatively any of Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , Rand R claim 1 , and Rand Rcan claim 1 , together with the atoms linking them claim 1 , form a 5-15 membered heterocycloalkyl optionally substituted by 1-3 Ror a 5-15 membered heteroaryl optionally substituted by 1-3 R.6. A compound as defined in claim 1 , wherein R claim 1 , R claim 1 , R claim 1 , R claim 1 , and Rare independently chosen from H and Calkyl optionally substituted by 1-3 R; Ris chosen from H claim 1 , Calkyl optionally substituted by 1-3 R claim 1 , Carylalkyl optionally substituted by 1-3 R claim 1 , and 6-10 membered heteroarylalkyl optionally substituted by 1-3 R; Ris chosen from H claim 1 , Calkyl optionally substituted by 1-3 R claim 1 , Carylalkyl optionally substituted by 1-9 R claim 1 , Ccycloalkylalkyl optionally substituted by 1-6 R claim 1 , and 6-11 membered heteroarylalkyl optionally substituted by 1-7 R; and alternatively any of Rand R claim 1 , Rand R claim 1 , ...

ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

The present invention discloses an organic compound represented by the following formula (1) and an organic electroluminescence device using the organic compound as the phosphorescent host material, the fluorescent host material, or the fluorescent dopant material. The organic compound may increase a current efficiency or half-life of the organic electroluminescence device. 2. The organic compound according to claim 1 , wherein A is a naphthyl group claim 1 , a phenanthrenyl group claim 1 , a dibenzothiophenyl group claim 1 , a dibenzofuranyl group claim 1 , a pyridinyl group claim 1 , a fluorenyl group claim 1 , a benzothiophenyl group claim 1 , a benzofuranyl group claim 1 , a phenanthrolinyl group claim 1 , a quinolinyl group or a indolyl group.3. The organic compound according to claim 1 , wherein L is independently a direct bond claim 1 , a divalent phenylene group claim 1 , a divalent biphenyl group claim 1 , a divalent naphthalene group claim 1 , a divalent anthrance group claim 1 , and a divalent fluorene group.6. An organic electroluminescence device claim 1 , comprising a pair of electrodes having a cathode and an anode claim 1 , and between the pairs of electrodes comprising at least a light emitting layer and one or more layers of organic thin film layers claim 1 , wherein the light emitting layer and/or the one or more thin film layers comprise the organic compound according to .7. The organic electroluminescence device of claim 7 , wherein the light emitting layer comprising the organic compound of formula (1) is a host material.8. The organic electroluminescence device of claim 7 , wherein the organic electroluminescence device is a backlight panel.9. The organic electroluminescence device of claim 7 , wherein the organic electroluminescence device is a light panel. The present invention relates to a novel organic compound and, more particularly, to an organic electroluminescence device using the organic compound.An organic electroluminescence ( ...

COMPOUNDS OF CHIRAL AROMATIC SPIROKETAL DIPHOSPHINE LIGANDS, PREPARATION METHODS AND USES THEREOF

Disclosed are aromatic spiroketal diphosphine ligands, preparation methods and uses thereof. The ligands have the structure of formula (I), in which R, R, R, R, R, R, R, R, X and n are defined as such described in the specification. The aromatic spiroketal diphosphine ligands are prepared from aromatic spiroketal compounds. Also disclosed are the preparation methods of aromatic spiroketal compounds. The preparation methods are simple and can produce racemic or chiral aromatic spiroketal diphosphine ligands. The ligands can be used as catalysts of asymmetrical catalytic reactions having economical practicability and industry application prospect. 3. The preparation method of claim 2 , wherein claim 2 , in step (a2) claim 2 , the mole ratio of the base to the compound of formula II is 2:1-10:1; and the mole ratio of RPCl or RPBr to the compound of formula II is 2:1-10:1; or{'sup': '4', 'sub': '2', 'in step (a3), the mole ratio of the metal catalyst to the compound of formula II is 0.001-0.5:1; and the mole ratio of RPH to the compound of formula II is 2-10:1.'}4. The preparation method of claim 2 , wherein said metal catalyst is at least one selected from Pd(OAc) claim 2 , PdCl claim 2 , Pd(dba) claim 2 , Pd(dba) claim 2 , [Pd(CH)Cl] claim 2 , Pd(PPh) claim 2 , Pd(PPh)Cl claim 2 , Pd(CHCN)Cl claim 2 , dpppNiCl claim 2 , Ni(PPh)Cl claim 2 , CuI or a combination thereof.5. The preparation method of claim 2 , wherein claim 2 , in step (a1) claim 2 , the mole ratio of the metal catalyst to the compound of formula II is 0.001-0.5:1; and the mole ratio of RPOH to the compound of formula II is 2-10:1; and/or in step (b1) claim 2 , the reducing agent is one selected from HSiCl claim 2 , (MeSiH)O claim 2 , LiAlH claim 2 , (EtO)SiH or a combination thereof.7. The preparation method of claim 6 , wherein the mole ratio of KPRor LiPRto the compound of formula II is 2:1-10:1.9. The preparation method of claim 8 , wherein claim 8 , in step (i1) claim 8 , the mole ratio of the base ...

Thioxanthone Derivatives, Composition Comprising the Same and Pattern Forming Method Comprising Said Composition

Latent photoinitiator compounds are described, as well as compositions containing such compounds and their uses in photoinitiated methods for producing photoresist structures. 2. (canceled)3. A compound according to claim 1 , wherein one of the aromatic rings is substituted with at least one substituent independently selected from hydroxy claim 1 , alkoxy claim 1 , benzyloxy claim 1 , alkylcarbonate claim 1 , hydroxyalkyl claim 1 , acetal claim 1 , ester claim 1 , oxyacetic acid and esters thereof claim 1 , aryloxy or arylthio claim 1 , and the other aromatic ring is unsubstituted.4. A compound according to claim 1 , wherein one aromatic ring is substituted with a single substituent selected from hydroxy claim 1 , alkoxy claim 1 , benzyloxy claim 1 , alkylcarbonate claim 1 , hydroxyalkyl claim 1 , acetal claim 1 , ester claim 1 , oxyacetic acid and esters thereof claim 1 , aryloxy or arylthio.5. A compound according to claim 1 , wherein one aromatic ring is substituted with two substituents independently selected from hydroxy claim 1 , alkoxy claim 1 , benzyloxy claim 1 , alkylcarbonate claim 1 , hydroxyalkyl claim 1 , acetal claim 1 , ester claim 1 , oxyacetic acid and esters thereof claim 1 , aryloxy or arylthio.6. A compound according to claim 1 , wherein one aromatic is substituted with three substituents independently selected from hydroxy claim 1 , alkoxy claim 1 , benzyloxy claim 1 , alkylcarbonate claim 1 , hydroxyalkyl claim 1 , acetal claim 1 , ester claim 1 , oxyacetic acid and esters thereof claim 1 , aryloxy or arylthio.7. A compound according to claim 1 , wherein the one aromatic substituted with four substituents independently selected from hydroxy claim 1 , alkoxy claim 1 , benzyloxy claim 1 , alkylcarbonate claim 1 , hydroxyalkyl claim 1 , acetal claim 1 , ester claim 1 , oxyacetic acid and esters thereof claim 1 , aryloxy or arylthio.8. A compound according to claim 1 , wherein each of the aromatic rings is substituted with at least one substituent ...

LOW MOLECULAR WEIGHT MODULATORS OF THE COLD MENTHOL RECEPTOR TRPM8 AND USE THEREOF

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

MNK INHIBITORS AND METHODS RELATED THERETO

The present invention relates to compounds according to Formula (I):

Spiro-oxindole compounds and their use as therapeutic agents

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

SULFONE-CONTAINING FUSED HETEROCYCLIC COMPOUND AND APPLICATION THEREOF

A sulfone-containing fused heterocyclic compound and application thereof. The sulfone-containing fused heterocyclic compound is represented by formula (1) 7. The sulfone-containing fused heterocyclic compound according to claim 1 , wherein the sulfone-containing fused heterocyclic compound has a triplet energy level T≥2.2 eV.8. The sulfone-containing fused heterocyclic compound according to claim 1 , wherein the sulfone-containing fused heterocyclic compound has a glass transition temperature T≥100° C.9. The sulfone-containing fused heterocyclic compound according to claim 1 , wherein the sulfone-containing fused heterocyclic compound has a difference between the singlet and triplet energy levels Δ(S−T)≤0.25 eV.10. A formulation comprising at least one sulfone-containing fused heterocyclic compound according to and at least one organic solvent.11. The formulation according to claim 10 , wherein the organic solvent is selected from aliphatic chain/ring substituted aromatic solvents claim 10 , or aromatic ketone solvents claim 10 , or aromatic ether solvents.12. The formulation according to claim 10 , wherein the organic solvent is selected from one of the group consisting of p-diisopropylbenzene claim 10 , pentylbenzene claim 10 , tetrahydronaphthalene claim 10 , cyclohexyl benzene claim 10 , chloronaphthalene claim 10 , 1 claim 10 ,4-dimethylnaphthalene claim 10 , 3-isopropylbiphenyl claim 10 , p-cymene claim 10 , dipentylbenzene claim 10 , tripentylbenzene claim 10 , pentyltoluene claim 10 , o-xylene claim 10 , m-xylene claim 10 , p-xylene claim 10 , o-diethylbenzene claim 10 , m-diethylbenzene claim 10 , p-diethylbenzene claim 10 , 1 claim 10 ,2 claim 10 ,3 claim 10 ,4-tetramethylbenzene claim 10 , 1 claim 10 ,2 claim 10 ,3 claim 10 ,5-tetramethylbenzene claim 10 , 1 claim 10 ,2 claim 10 ,4 claim 10 ,5-tetramethylbenzene claim 10 , butylbenzene claim 10 , dodecylbenzene claim 10 , dihexylbenzene claim 10 , dibutylbenzene claim 10 , p-diisopropylbenzene claim 10 , ...

(1r,4r) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene and derivatives thereof

This invention provides novel (1R,4R) 7-oxo-2-azabicyclo[2.2.2]oct-5-ene and derivatives thereof, preferably in substantially enantiomerically enriched forms, intermediates thereto, and processes of their synthesis.

Multicyclic compounds and methods of use thereof

Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

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. 117.-. (canceled)19. The compound as claimed in claim 18 , wherein Aand Aare single bonds.20. The compound as claimed in comprising exactly one or two groups of the formula (2).23. The compound as claimed in claim 18 , wherein in the group of the formula (2) claim 18 , Z is the same or different and is C═O or C═S claim 18 , and in that E is a single bond claim 18 , CR claim 18 , C═O or NR.28. The compound as claimed in claim 18 , wherein all R radicals are H or in that one or two R radicals are an aromatic or heteroaromatic ring system which has 6 to 24 aromatic ring atoms and may be substituted in each case by one or more Rradicals claim 18 , and the other R radicals are H.29. An oligomer claim 18 , polymer or dendrimer containing one or more of the compounds as claimed in claim 18 , wherein one or more bonds of the compound to the polymer claim 18 , oligomer or dendrimer are present in place of one or more R radicals.30. A formulation comprising at least one compound as claimed in and at least one further compound claim 18 , especially a solvent or a mixture of two or more solvents.31. A method comprising incorporating the compound as claimed in in an electronic device.32. An electronic device comprising at least one compound as claimed in .33. The electronic device as claimed in claim 18 , wherein the device is an organic electroluminescent device and the compound as claimed in is used in an emitting layer as matrix material for fluorescent or phosphorescent emitters and/or in a hole blocker layer and/or in an electron transport layer. The present invention relates to materials for use in electronic devices, especially as host material for phosphorescent emitters in organic electroluminescent devices, and to electronic devices, especially organic electroluminescent devices, ...

MNK INHIBITORS AND METHODS RELATED THERETO

The present invention relates to compounds according to Formula (I): 2. The compound of wherein n is 1 and Y is —N(R)—.3. The compound of wherein Wand Ware O.4. The compound of wherein Rand Rare each independently hydrogen claim 1 , methyl claim 1 , ethenylene claim 1 , propynylene claim 1 , 2-methyl-1-propenylene claim 1 , benzyl claim 1 , fluorobenzyl claim 1 , chlorobenzyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , difluorocyclohexyl claim 1 , iso-propyl claim 1 , trifluoromethyl claim 1 , 1 claim 1 ,1 claim 1 ,1-trifluoroethylene claim 1 , thiophene claim 1 , thiazole claim 1 , methylenenitrile claim 1 , chlorophenyl claim 1 , fluorophenyl claim 1 , fluorochlorophenyl claim 1 , difluorophenyl claim 1 , pyridine claim 1 , methylpyridine claim 1 , chloropyridine claim 1 , N-methylaminomethylene claim 1 , aminomethylene claim 1 , 1-aminoethylene claim 1 , t-butyl claim 1 , methylaminomethylene claim 1 , propyl claim 1 , 1-hydroxyethylene claim 1 , or 1 claim 1 ,1-difluoroethylene.5. The compound of wherein Rand Rare each independently methyl claim 4 , trifluoromethyl claim 4 , 1 claim 4 ,1 claim 4 ,1-trifluoroethylene claim 4 , cyclopentyl claim 4 , cyclohexyl claim 4 , difluorocyclohexyl claim 4 , chlorophenyl claim 4 , or fluorophenyl.6. The compound of wherein n is 1 and Rand Rtogether with the carbon atom to which they are attached forms a cycloalkyl or a heterocyclyl ring that is optionally substituted with 1 claim 1 , 2 or 3 J groups.7. The compound of wherein Rand Rtogether with the carbon atom to which they are attached forms a cycloalkyl ring selected from the group consisting of cyclobutyl claim 6 , cyclopentyl and cyclohexyl and wherein any cyclobutyl claim 6 , cyclopentyl or cyclohexyl is optionally substituted with halogen claim 6 , hydroxy claim 6 , or trifluoromethylene groups.8. The compound of wherein Rand Rtogether with the carbon atom to which they are attached forms a heterocyclyl ring that is optionally substituted with 1 claim 6 , 2 ...

HETEROAROMATIC COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE USING THE SAME

A heteroaromatic compound which can be used as the fluorescent guest material in the light emitting layer of the organic electroluminescence device is disclosed. The organic electroluminescence device employing the heteroaromatic compound of the present invention shows lower power consumption, higher efficiency, and longer half-life time than the existed organic electroluminescence devices. 5. An organic electroluminescence device claim 1 , comprising a pair of electrodes composed of a cathode and an anode claim 1 , and a light emitting layer between the pair of electrodes claim 1 , wherein the light emitting layer comprises the heteroaromatic compound according to .6. The organic electroluminescence device according to claim 5 , wherein the light emitting layer comprising the heteroaromatic compound of formula (1) is a fluorescent dopant material.7. The organic electroluminescence device according to claim 5 , wherein the light emitting layer emits blue fluorescence.8. The organic electroluminescence device according to claim 5 , wherein the organic electroluminescence device is a lighting panel.9. The organic electroluminescence device according to claim 5 , wherein the organic electroluminescence device is a backlight panel. The present invention relates to a heteroaromatic compound and, more particularly, to an organic electroluminescence device using the heteroaromatic compound.An organic electroluminescence (organic EL) device is an organic light-emitting diode (OLED) in which the light emitting layer is a film made from organic compounds, which emits light in response to the electric current. The light emitting layer containing the organic compound is sandwiched between two electrodes. The organic EL device is applied to flat panel displays due to its high illumination, low weight, ultra-thin profile, self-illumination without back light, low power consumption, wide viewing angle, high contrast, simple fabrication methods and rapid response time.Typically, ...

SPIRO-CONDENSED LACTAM COMPOUNDS FOR ORGANIC ELECTROLUMINESCENT DEVICES

The invention relates to polycondensed lactam compounds as materials for use in electronic devices, and electronic devices, in particular organic electroluminescent devices, containing said materials. 114.-. (canceled)16. The compound as claimed in claim 15 , wherein X is CR or N claim 15 , where not more than one X group per cycle is N.18. The compound as claimed in claim 17 , wherein the symbols used are as follows:X is the same or different at each instance and is CR or N, where not more than one X group per cycle is N;{'sub': '2', 'E is the same or different at each instance and is NR where R is not H or D, or CR, O, S or C═O;'}{'sup': '1', 'claim-ref': {'@idref': 'CLM-00017', 'claim 17'}, 'Aris selected from the groups of the formulae (2), (3), (4), (5) and (6) according to ,'}{'sup': '2', 'claim-ref': {'@idref': 'CLM-00017', 'claim 17'}, 'Aris selected from the groups of the formulae (9), (10) and (11) according to ;'}{'sup': '3', 'claim-ref': {'@idref': 'CLM-00017', 'claim 17'}, 'Aris selected from the groups of the formulae (12), (13), (14) and (15) according to .'}22. The compound as claimed in claim 15 , wherein E is NR and R is selected from aromatic and heteroaromatic ring systems which have 5 to 40 aromatic ring atoms and is optionally substituted by one or more Rradicals claim 15 , especially phenyl claim 15 , ortho- claim 15 , meta- or para-biphenyl claim 15 , ortho- claim 15 , meta- claim 15 , para- or branched terphenyl claim 15 , ortho- claim 15 , meta- claim 15 , para- or branched quaterphenyl claim 15 , 1- claim 15 , 2- claim 15 , 3- or 4-fluorenyl claim 15 , 1- claim 15 , 2- claim 15 , 3- or 4-spirobifluorenyl claim 15 , triazine claim 15 , 1- claim 15 , 2- claim 15 , 3- or 4-dibenzofuranyl claim 15 , 1- claim 15 , 2- claim 15 , 3- or 4-dibenzothienyl or 1- claim 15 , 2- claim 15 , 3- or 4-carbazolyl claim 15 , each of which is optionally substituted by one or more Rradicals.23. A formulation comprising at least one compound as claimed in and at ...

LOW MOLECULAR WEIGHT MODULATORS OF THE COLD MENTHOL RECEPTOR TRPM8 AND USE THEREOF

The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators. 123.-. (canceled)25. A composition comprising the substance according to .2641. The composition according to claim claim 24 , wherein the composition is selected from the group consisting ofa. pharmaceutical compositions;b. foods,c. mouthcare compositions,d. bodycare compositions, ande. foams and gels.27. The composition according to claim 26 , comprisinga) one or more further substances with a physiological cooling effect, where the further substance or one, several or all of the further substances (i) cause a gustatory effect or (ii) do not cause a gustatory effect,and/orb) one or more aroma substances without a physiological cooling effect and/orc) one or more trigeminally or mouth-washing effective substances without a physiological cooling effectand/ord) (iii) one or (iv) several compounds which, in the case of (iv), independently of one another or together, additionally cause a taste-modulating effect and/or a trigeminal and/or mouth-washing stimulus.29. The substance according to claim 28 , wherein the substance is selected from compounds P1 to P7.30. A method for the in-vitro or in-vivo modulation of the cold menthol receptor TRMP8 claim 24 , where the receptor is brought into contact with the substance according to .31. A method for the in-vitro or in-vivo modulation of the cold menthol receptor TRMP8 claim 25 , where the receptor is brought into contact with the composition according to .32. A method for the in-vitro or in-vivo modulation of the cold menthol receptor TRMP8 claim 28 , where the receptor is brought into contact with the substance according to .35. The composition according to for preventing claim 25 , controlling or alleviating symptoms of ...

Spiropyrazine derivatives as inhibitors of non-apoptotic regulated cell-death

The present invention relates to spiropyrazine compounds which are inhibitors of non-apoptotic regulated cell death, and to pharmaceutical compositions containing such compounds. Furthermore, the present invention relates to the use of such compounds and pharmaceutical compositions in therapy, in particular in the treatment of a condition, disorder or disease that is characterised by non-apoptotic regulated cell-death or where non-apoptotic regulated cell-death is likely to play or plays a substantial role. The compounds and pharmaceutical compositions described herein are also useful in the treatment of a condition, disorder or disease that is characterised by oxidative stress or where oxidative stress is likely to play or plays a substantial role; and/or a condition, disorder or disease that is characterised by activation of (1) one or more components of the necrosome; (2) death domain receptors; and/or (3) Toll-like receptors; and/or (4) players in ferroptotic/ferroptosis signalling, or where activation of any one of (1) to (3) and/or (4) is likely to play or plays a substantial role.

ORGANIC POLYSPIROGRID NANO POLYMER MATERIAL AND PREPARATION METHOD THEREFOR

The invention relates to an organic polyspiralgrid nanopolymer material and a preparation method thereof, and belongs to the field of nanotechnology and organic electronics. The structure of the organic polyspiralgrid nanopolymer material is composed of grids containing a spiro ring that serves as a repeat unit to form a special nano polymer, and the structure shares the spiro ring structure. A synthetic method thereof relates to a synthon containing the spiro ring, and by means of a Friedel-Crafts reaction, an organic spirogrid and a nano polymer thereof are built. By means of reasonable molecular design and the Friedel-Crafts reaction with the advantages of being mild in reaction condition, high in yield, high in selectivity, simple in posttreatment, green, free of toxicity and the like, the problems that a traditional polymer molecule is complex in synthesis step, toxic in posttreatment, large in pollution and the like are solved. 4. The method for preparing the organic polyspiralgrid nanopolymer material of claim 3 , wherein the acid includes Lewis acids and protonic acids claim 3 , and an amount of acid catalyst added is 2-5 times that of A2B2-type synthon according to reactivity of different substrates; and a reaction concentration of A2B2-type synthon is between 1 mmol/L-10 mmol/L according to the reactivity of different substrates.5. The method for preparing the organic polyspiralgrid nanopolymer material of claim 4 , wherein the Lewis acids and protonic acids are one or a combination of several of the following acids: acetic acid claim 4 , hydroiodic acid claim 4 , hydrobromic acid claim 4 , hydrochloric acid claim 4 , methanesulfonic acid claim 4 , fluoromethylsulfonic acid claim 4 , trifluoromethanesulfonic acid claim 4 , concentrated sulfuric acid claim 4 , trifluoroacetic acid and hydrofluoric acid-antimony pentafluoride.6. The method for preparing the organic polyspiralgrid nanopolymer material of claim 3 , wherein the dry organic solvent is one of the ...

Organic electroluminescence device and monoamine compound for organic electroluminescence device

An organic electroluminescence device of an embodiment includes a first electrode, a second electrode provided on the first electrode, and a plurality of organic material layers provided between the first electrode and the second electrode, wherein at least one organic material layer among the plurality of organic material layers include a monoamine compound, and the monoamine compound includes a core structure including two condensed rings which are combined to form a spiro structure, where each condensed ring has a condensed structure of three or more pentagonal or hexagonal rings. High emission efficiency may be achieved.

Materials for organic electroluminescent devices

The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which comprise these compounds.

Gonadotropin releasing hormone receptor antagonists, method for the preparation thereof and pharmaceutical composition comprising the same

본 발명은 고나도트로핀 방출 호르몬 수용체 길항제 및 이를 포함하는 약학 조성물에 관한 것으로, 본 발명에 따른 화합물은 성호르몬과 관련된 다양한 증상, 예를 들면, 자궁내막증, 무월경, 월경불순, 자궁근종, 자궁 유섬유종, 다낭성 난소질환, 홍반성 루푸스, 다모증, 성조발증, 단신증, 여드름, 탈모증, 생식선 스테로이드-의존성 신생물, 성선자극 뇌하수체선종, 수면 무호흡증, 과민성 대장증후군, 월경전 증후군, 양성 전립선 비대증, 피임 및 불임 및 알츠하이머 등의 예방 또는 치료에 유용하게 사용될 수 있다. The present invention relates to a gonadotropin releasing hormone receptor antagonist and a pharmaceutical composition comprising the same. The compounds according to the present invention are useful for the treatment of various symptoms associated with sex hormones such as endometriosis, amenorrhea, menstrual irregularities, Gonadal steroid-dependent neoplasia, gonadotrophic pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception And in the prevention or treatment of infertility and Alzheimer's disease.

- novel adduct compound methods for purification and preparation of fused polycyclic aromatic compound solution for formation of organic semiconductor film and novel -diketone compound

증착법보다 일반적으로 용이한 용액법을 이용하여, 축합 다고리 방향족 화합물로 이루어지는 유기 반도체층의 형성을 가능하게 하는 신규한 부가 화합물 및 α-디케톤 화합물을 제공한다. 또, 이 부가 화합물의 정제 방법, 및 이 부가 화합물을 함유하는 유기 반도체막 형성용 용액을 제공한다. 본 발명의 부가 화합물은 디나프토티에노티오펜 등의, 식 (Ⅰ) 의 축합 다고리 방향족 화합물에, 헥사클로로시클로펜타디엔 등의 이중 결합을 갖는 화합물이 탈리 가능하게 부가되어 이루어지는 구조를 갖는다. 또, 본 발명의 α-디케톤 화합물은 디나프토티에노티오펜 등의 축합 다고리 방향족 화합물에, 헥사클로로시클로펜타디엔 등의 이중 결합을 갖는 화합물이 탈리 가능하게 부가되어 이루어지는 구조를 갖는다. Ar 1 Ar 2 Ar 3 (Ⅰ) (식 중, Ar 1 , Ar 2 , Ar 3 은 명세서에서 정의된 바와 같다) A novel adduct compound and an? -Diketone compound which enables the formation of an organic semiconductor layer composed of a condensed polycyclic aromatic compound by using a solution method generally easier than a vapor deposition method. Further, a method for purifying the addition compound and a solution for forming an organic semiconductor film containing the addition compound are provided. The addition compound of the present invention has a structure in which a compound having a double bond such as hexachlorocyclopentadiene is removably added to a condensed polycyclic aromatic compound of formula (I) such as dinaphthothienothiophene. The? -Diketone compound of the present invention has a structure in which a compound having a double bond such as hexachlorocyclopentadiene is removably added to a condensed polycyclic aromatic compound such as dinaphthothienothiophene. Ar 1 Ar 2 Ar 3 (I) (Wherein Ar 1 , Ar 2 , Ar 3 are as defined in the specification)

作为病毒复制抑制剂的噻吩并[2,3-b]吡啶衍生物

本发明涉及一系列具有抗病毒活性、更具体地说具有HIV(人免疫缺陷病毒)复制抑制特性的式(A)的化合物。本发明还涉及这种化合物的制备方法，以及涉及可用于此合成的一个或多个步骤中的新型中间体。本发明还涉及包括治疗有效量的作为活性成分的此化合物的药物组合物。本发明进一步涉及此化合物作为药物的应用或者此化合物在制备可用于治疗患有病毒感染、特别是HIV感染的动物的药物中的应用。本发明进一步涉及通过施用任选地与一种或多种具有抗-病毒活性的其它药物组合的治疗有效量的此化合物来治疗动物的病毒感染的方法。

Materials for organic electroluminescent devices

본 발명은 전자 소자에서 사용하기에 적합한 화합물, 및 상기 화합물을 함유하는 전자 소자, 특히 유기 전계발광 소자에 관한 것이다. The present invention relates to compounds suitable for use in electronic devices, and to electronic devices containing said compounds, in particular organic electroluminescent devices.

Ühendid

Condensed fluorene derivative comprising heterocyclic ring

본 발명은 헤테로고리를 포함하는 축합 플루오렌 유도체에 관한 것으로서, 보다 상세하게는 유기발광 재료로 사용되는 경우에 휘도와 발광 효율이 우수하며, 장수명의 우수한 소자특성을 보여줄 수 있는 헤테로고리 화합물을 제조하기 위한 중간체에 관한 것이다. The present invention relates to a condensed fluorene derivative including a heterocycle, and more particularly, when used as an organic light emitting material, excellent in brightness and luminous efficiency, and manufacturing a heterocyclic compound that can show excellent long-term device characteristics It relates to an intermediate for.

Heterocyclic aspartyl protease inhibitors

Disclosed are compounds of formula (I) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, U, W, X, R1, R2, R6, R7, R30 and R31 are as described above in the specification. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors

The present invention provides compounds including substituted thienopyrimidinone derivatives of Formula (IIc) as ligands for modulating chemosensory receptors: These compounds are useful as sweet taste enhancers in comestible or medicinal compositions. The present invention also provides screening methods for identifying modifiers of chemosensory receptors and their ligands, e.g., by determining whether a test entity is suitable to interact with one or more interacting sites within the Venus flytrap domains of the chemosensory receptors as well as modifiers capable of modulating chemosensory receptors and their ligands.

Compounds for Electronic Devices

본 출원은 식 (I) 의 화합물, 전자 디바이스에서의 이의 용도, 상기 화합물의 제조 방법, 및 화합물을 포함하는 전자 디바이스에 관한 것이다.

Organic electroluminescent compound, organic electroluminescent device and application thereof

本发明提供了有机电致发光化合物、有机电致发光器件及其应用。本发明有机电致发光化合物结构如下：

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

【課題】皮膚又は粘膜上で冷却効果を得るための新規ＴＲＰＭ８モジュレーターの提供。【解決手段】例えば式（Ｉ）で表される様な特定の基本骨格を持つ化合物及びその誘導体を調製したＴＲＰＭ８作動薬。【選択図】図３

Organic electroluminescent materials and device

A compound including a first ligand L A of Formula I, useful as an emitter in OLEDs is disclosed.

Materials for organic electroluminescent devices

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

Materials for organic electroluminescent devices

The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which comprise these compounds.

Heterocyclic compound for use in electronic devices

The present invention relates to heterocyclic compounds, particularly for use in electronic devices. The invention further relates to a method for producing the compounds according to the invention and to electronic devices comprising the same.

Heteroaromatics and the organic EL component for using it

本发明提供了一种杂芳族化合物，其可用作有机电激发光组件发光层的荧光掺杂材料。使用该杂芳族化合物的有机电激发光组件，可具有更低的功耗、更高的发光电流效率、或更长的半衰期。

Gonadotropin releasing hormone receptor antagonists, method for the preparation thereof and pharmaceutical composition comprising the same

本发明提供了促性腺激素释放激素受体拮抗剂和包含该促性腺激素释放激素受体拮抗剂的药物组合物，其可用于预防或治疗性激素相关疾病，如子宫内膜异位症、闭经、月经不调、子宫肌瘤、子宫纤维瘤、多囊卵巢病、红斑狼疮、多毛症、性早熟、矮小症、痤疮、脱发、性腺激素依赖性肿瘤、产生促性腺激素的垂体腺瘤、睡眠呼吸暂停、肠易激综合征、经前期综合征、良性前列腺增生、避孕和不育，以及阿尔茨海默病。

One kind including 4,5- diaza spiro formula thioxanthene structure electroluminescent organic materials and its application and device

本发明属于有机电致发光材料领域，具体涉及一种包含4,5‑二氮杂螺式硫杂蒽结构有机电致发光材料及其应用和器件，可用于有机发光二极管，并且具有很好地双极性传输性质，可作为主体材料使用。结构式如下： 其中，Ar 1 、Ar 2 独立的选自氢原子、C 3 ～C 30 的取代或者非取代的咔唑基团、C 3 ～C 30 取代或者非取代的芳胺基团、C 3 ～C 30 取代或者非取代的吩噻嗪基团、C 3 ～C 30 取代或者非取代的吩噁嗪基团、C 3 ～C 30 取代或者非取代的吩嗪基团、C 3 ～C 30 取代或者非取代的吖啶基团，Ar 1 、Ar 2 不同时为氢。本发明还涉及一种包括至少一层所述双极性化合物作为主体材料的器件和制造所述器件的方法。

Bipolarity organic electroluminescent compounds and its application and organic electroluminescence device

本发明涉及有机电致发光器件领域，公开了双极性有机电致发光化合物及其应用和有机电致发光器件，该化合物具有式(I)所示的结构，其中，在式(I)中，X 1 为Si或C；X 2 为S或O。本发明提供的前述双极性有机电致发光化合物在用作有机电致发光器件中时能够显著提高发光效率以及延长材料的使用寿命。

Spiro-oxindole compounds and their use as therapeutic agents

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Spiro-oxindole compounds and their use as therapeutic agents

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Spiro-oxindole compounds and their uses as therapeutic agents

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Spiro-oxindole compounds and their use as therapeutic agents

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Spiro-oxindole compounds and their use as therapeutic agents

This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.

Materials for organic light-emitting devices

본 발명은 전자 소자, 특히 유기 전계발광 소자에서 인광 방사체용 호스트 재료로서의 사용을 위한 재료, 및 이러한 재료를 포함하는 전자 소자, 특히 유기 전계발광 소자에 관한 것이다. The present invention relates to materials for use as host materials for phosphorescent emitters in electronic devices, in particular organic electroluminescent devices, and to electronic devices comprising such materials, in particular organic electroluminescent devices.

Materials for organic electroluminescent devices

本發明關於適合用於電子裝置(特別是有機電致發光裝置)的式(1)化合物，及包含此等化合物之電子裝置。

SPIRO-6,7-DIHYDRO-5H-PYRAZOLO[1,2-a]PYRAZOLE-1-ONES THAT REGULATE INFLAMMATORY CYTOKINES, PHARMACEUTICAL COMPOSITION AND METHOD FOR INHIBITION

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to new compounds able to prevent the extracellular release of inflammatory cytokines. Proposed compounds including their diastereomeric forms and their pharmaceutically acceptable salts correspond to the formula: wherein R means: (a) -O[CH 2 ] k R 3 or (b) -NR 4a R 4b ; R 3 means a substituted or unsubstituted (C 1 -C 4 )-alkyl, a substituted or unsubstituted phenyl wherein substitutes are taken among halogen atom, cyano-group, trihalidemethyl, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkylsulfonyl, -NR 4a R 4b , -O[CH 2 ] k R 3 wherein R 3 means hydrogen atom each among R 4a and R 4b means independently hydrogen atom or (C 1 -C 4 )-alkyl-CO- or benzo(1,3)dioxol; index k has a value from 0 to 5; each among R 4a and R 4b means independently: (a) hydrogen atom or (b) -[C(R 5a R 5b ) 2 ] m R 6 wherein each R a means hydrogen atom, and R 5b means hydrogen atom, linear or branched (C 1 -C)-alkyl; R 6 means vinyl, the group -OR 7 , -CO 2 R 7 , cyclic (C 3 -C)-alkyl, unsubstituted phenyl or phenyl substituted with (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkylsulfonyl, -NR 4a R 4b , -O[CH 2 ] k R 3 wherein each among R 3 , R 4a and R 4b means independently hydrogen atom, or unsubstituted 6-membered nitrogen-containing heteroaryl; R 7 means hydrogen atom, water-soluble cation or (C 1 -C 4 )-alkyl; index m has a value from 0 to 5. Also, invention relates to a pharmaceutical composition comprising the effective dose of compounds corresponding to abovementioned formula, and to a method for inhibition of extracellular release of inflammatory cytokines. EFFECT: valuable medicinal properties of compounds and composition. 14 cl, 1 sch, 6 tbl, 3 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 272 040 (13) C2 (51) ÌÏÊ C07D 491/20 (2006.01) C07D 495/20 (2006.01) A61K 31/4162 (2006.01) A61P 29/00 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: ...

Compound containing imidazole spiro ring and application thereof

本发明涉及一种含咪唑螺环的化合物及其应用，该化合物具有如化学式(1)所示的结构通式。该化合物稳定性好、发光效率高、寿命长、合成简单。

The conjugated compound of the formula carboline thioxanthene of spiral shell containing 9,9- and preparation and application

本发明属于电致发光材料技术领域，公开了一种含9,9‑螺式二氮芴噻吨的共轭化合物及制备与应用。所述含9,9‑螺式二氮芴噻吨的共轭化合物具有式1或式2所示的结构通式，其中R 1 和R 2 为相同或者不相同的具有给电子性的乙烯撑基、乙炔撑基、碳氢原子构成的芳香环、碳氮氢原子构成的芳香杂环、碳氮氧氢原子构成的芳香杂环、碳硫氢原子构成的芳香杂环、碳硅氢原子构成的芳香杂环、C1～C24的烷基、烷基取代的共轭单元、烷氧基取代的共轭单元或烷基和烷氧基同时取代的共轭单元。本发明所得化合物具有荧光性，作为有机电致发光二极管的发光层可显著提升器件的外量子效率。

P-doped organic small molecule and preparation method and application thereof

本发明公开了两种p掺杂有机小分子及其制备方法和应用。本发明分别采用Suzuki偶联反应和Buchward–Hartwig反应制备了Spiro‑DTP‑TPA和Spiro‑DTP‑DPA。这两种有机材料具有高的空穴流动性和与Pb具有强的相互作用。应用于钙钛矿太阳能电池的反溶剂工程中，优化了钙钛矿的结晶，钝化了钙钛矿薄膜表面与晶界处的缺陷，同时p掺杂钙钛矿实现能带弯曲，最终大大的提高了电池的性能和稳定性，将钙钛矿太阳能电池的光电转化效率从原有的17.22%提升至20.21%，同时，在相对湿度为30~40%，温度为20~35 o C的条件下储存1080 h后，p掺杂的电池仍可维持94%的初始效率，而原始器件的效率已降低至初始效率的49%。

Detection and use of low molecular-weight modulators of the cold-menthol receptor TRPM8

The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.

Detection and use of low molecular-weight modulators of the cold-menthol receptor TRPM8

The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.

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.

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.

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.

Detection and use of low molecular-weight modulators of the cold-menthol receptor trpm8

The invention relates to novel modulators of the cold-menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to the objects and means produced using said modulators.

The detection of cold menthol receptor TRPM8 low molecule amount conditioning agent and purposes

本发明涉及冷薄荷醇受体TRPM8的低分子量调节剂的检测和用途。具体而言，本发明涉及冷薄荷醇受体TRPM8的新调节剂，使用这些调节剂调节TRPM8受体的方法；所述调节剂用于诱导冷感觉的用途；以及使用这些调节剂制备的物品和工具。

Detection and use of low molecular weight modulators of the cold menthol receptor TRPM8

本发明涉及冷薄荷醇受体TRPM8的低分子量调节剂的检测和用途。具体而言，本发明涉及冷薄荷醇受体TRPM8的新调节剂，使用这些调节剂调节TRPM8受体的方法；所述调节剂用于诱导冷感觉的用途；以及使用这些调节剂制备的物品和工具。