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Небесная энциклопедия

Космические корабли и станции, автоматические КА и методы их проектирования, бортовые комплексы управления, системы и средства жизнеобеспечения, особенности технологии производства ракетно-космических систем

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Мониторинг СМИ

Мониторинг СМИ и социальных сетей. Сканирование интернета, новостных сайтов, специализированных контентных площадок на базе мессенджеров. Гибкие настройки фильтров и первоначальных источников.

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Применить Всего найдено 5513. Отображено 189.
30-07-1990 дата публикации

Способ получения бензоконденсированных циклоалкантранс-1,2-диаминовых производных в виде энантиомеров или рацематов, или их фармацевтически приемлемых солей

Номер: SU1582984A3

Изобретение относится к амидам, в частности к получению бензоконденсированных циклоалкантранс-1,2-диаминовых производных ф-лы I R-N-COCH 2 @ в виде энантиомеров или рацематов, где B-H, OH, OCOC 25, OCOC 6H 5, OR 1, CH* 2OR 1 C-H, OR 1, OH R - C 1-C 3-алкил X и Y - CL или вместе с бензольным кольцом образуют группу CH=CH-CH=CH-C=CH-S - CH=CH R 1 - C 1-C 3-алкил, или их фармацевтически приемлемых солей, которые обладают обезболивающими и мочегонным действием и могут найти применение в медицине. Цель - получение новых соединений, обладающих высокой обезболивающией активностью. Получение ведут ацилированием соединения ф-лы I, где B и C - указаны, соответствующей карбоновой кислотой в присутствии циклогексилкарбодиимида или хлорангидридом карбоновой кислоты в присутствии триэтиламина, или водного бикарбоната натрия, или ацилимидазолом (полученным из карбоновой кислоты с карбонилдиимидазолом). 3 табл.

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29-12-2004 дата публикации

METHODS AND COMPOSITIONS FOR TREATING AMYLOID-RELATED DISEASES

Номер: CA0002529257A1
Принадлежит:

Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.

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20-01-2000 дата публикации

LIGANDS FOR METALS AND METAL-CATALYZED PROCESSES

Номер: CA0002336691A1
Принадлежит:

One aspect of the present invention relates to novel ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in transition metal-catalyzed carbon- heteroatom and carbon-carbon bond-forming reactions. The subject processes provide improvements in many features of the transition metal-catalyzed reactions, including the range of suitable substrates, reaction conditions, and efficiency.

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13-01-2005 дата публикации

4-(METHYL SULFONYL AMINO) PHENYL ANALOGUES AS VANILLOID ANTAGONIST SHOWING EXCELLENT ANALGESIC ACTIVITY AND THE PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME

Номер: CA0002533547A1
Принадлежит:

The present invention relates to novel 4-(methylsulfonylamino) phenyl analogue as a potent vanilloid receptor antagonist and the pharmaceutical compositions comprising the same. The inventive compound can be useful for analgesics to prevent, alleviate or treat pain diseases or inflammatory disease comprising pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflammatory bowel disease, inflammatory disease and urgent urinary incontinence.

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09-12-1999 дата публикации

METHOD FOR TREATING NEURODEGENERATIVE DISORDERS

Номер: CA0002333951A1
Принадлежит:

The invention is directed to a method of treating a neurodegenerative disorder in a subject in need thereof which comprises administering to the subject an amount of a compound effective to inhibit the interaction of amyloid-beta with alpha-7 nicotinic acetylcholine receptors.

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02-07-2013 дата публикации

NOVEL LIGANDS THAT ARE ACTIVATORS OF THE RAR RECEPTORS, USE IN HUMAN MEDICINE AND IN COSMETICS

Номер: CA0002545112C
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

... ²The present invention relates to novel compounds corresponding to the general ²formula (l) below, to compositions containing them, and to their use in ²pharmaceutical compositions intended for use in human or veterinary medicine, ²or ²alternatively in cosmetic compositions.²(see formula I)² ...

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22-01-2013 дата публикации

CONDENSED RING COMPOUND

Номер: CA0002527691C
Принадлежит: TAKEDA PHARMACEUTICAL COMPANY LIMITED

... ²²² The present invention aims at providing a novel fused ring ²compound having a GPR40 receptor function modulating action and ²being useful as an insulin secretagogue or a pharmaceutical²²agent for the prophylaxis or treatment of diabetes, more ²particularly, a compound represented by the formula: ²(see formula I)²²wherein Ar is an optionally substituted cyclic group,²²ring A is a ring optionally further substituted (provided that ²the ring is not thiazole, oxazole, imidazole and pyrazole),² Xa and Xb are each independently a bond or a spacer having a ²main chain of 1 to 5 atom(s),²² Xc is O, S, SO or SO2, ²(see formula II) is²²(see formula III), (see formula IV), (see formula V) or (see formula VI),²ring B is a 5- to 7-membered ring, ²Xd is a bond, CH or CH2,²² ~ is a single bond when Xd is a bond or CH2, or a double bond ²when Xd is CH, and²² R1 is an optionally substituted hydroxy group, and a salt thereof.² ...

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02-02-2010 дата публикации

SUBSTITUTED N-SULFONYLAMINOBENZYL-2-PHENOXYACETAMIDE COMPOUNDS

Номер: CA0002587149C
Принадлежит: PFIZER INC.

This invention provides a compound of the formula (I): wherein R1 represents a (C1,-C6)alkyl group; R2 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1-C6) alkyl group or a (C1-C6) alkoxy group; R3, R4, R5 and R6 each independently represents a hydrogen atom, a (C1-C6) alkyl, or a halogen atom; R7 represents a hydrogen atom, a halogen atom, a hydroxy group, a (C1-C6) alkyl group optionally substituted with a piperidino group, a (C1-C6)alkoxy group optionally substituted with a 3-7 membered cycloalkyl ring, a hydroxy(C1- C6)alkoxy group, a (C1-C8)alkoxy- (C1-C8)alkyl group, a (C1-C6)alkoxy-(C1- C6)alkoxy group, a halo (C1-C6)alkyl group, a (C1-C6)alkylthio group, a (C1- C6)alkylsulfinyl group or a (C1-C6)alkylsulfonyl group; R8 represents a (C1- C6)alkyl group, a halo(C1-C6,)aIkyl group, a (C1-C6)alkoxy group, a hydroxy(C1- C6)alkoxy group, a (C1-C6)alkoxy-(C1-C6)alkyl group or a (C1-C6)alkoxy-(C1- C6)alkoxy group; or R7 and R8, when adjacent to each other, taken together ...

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07-12-2010 дата публикации

ALKYL UREA RETINOID AGONISTS I

Номер: CA0002460693C
Принадлежит: F. HOFFMANN-LA ROCHE AG

The current invention provides compounds of the general formula (I), methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and termatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cance and dermatological disorders.

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03-11-2009 дата публикации

ORTHO SUBSTITUTED CHIRAL PHOSPHINES AND PHOSPHINITES AND THEIR USE IN ASYMMETRIC CATALYTIC REACTIONS

Номер: CA0002427579C
Автор: ZHANG, XUMU
Принадлежит: THE PENN STATE RESEARCH FOUNDATION

... 3,3'-Substituted chiral biaryl phosphine and phosphinite ligands and metal complexes based on such chiral ligands useful in asymmetric catalysis are disclosed. Provided, for example, are ligands of the formula: (see above formula) The metal complexes are useful as catalysts in asymmetric reactions, such as, hydrogenation, hydride transfer, allylic alkylation, hydrosilylation, hydroboration, hydrovinylation, hydroformylation, olefin metathesis, hydrocarboxylation, isomerization, cyclopropanation, Diels-Alder reaction, Heck reaction, isomerization, Aldol reaction, Michael addition. epoxidation, kinetic resolution and [m+n] cycloaddition. The metal complexes are particularly effective in Ru-catalyzed asymmetric hydrogenation of beta-ketoesters to beta- hydroxyesters and Ru-catalyzed asymmetric hydrogenation of enamides to beta amino acids.

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24-06-2004 дата публикации

TETRAHYDRO-NAPHTHALENE DERIVATIVES

Номер: CA0002508618A1
Принадлежит:

This invention relates to tetrahydro-naphthalene derivatives and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have an excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.

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12-08-1999 дата публикации

HYDROXYLATION ACTIVATED PRODRUGS

Номер: CA0002319836A1
Принадлежит:

The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

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10-02-2005 дата публикации

ALKYNYL ARYL CARBOXAMIDES

Номер: CA0002527861A1
Принадлежит:

The present invention is related to alkynyl aryl carboxamides of Formula (I~) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance. insulin resistance, hyperlipidemia, hypertriglyceridemia- hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I~) to modulate, notably to inhibit the activity of PTPs. (I~) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy' is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1and R2 are independently from each other is selected from the group consisting of hydrogen or (CI-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting ...

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28-03-2002 дата публикации

N-ACYLSULFONAMIDE APOPTOSIS PROMOTERS

Номер: CA0002423103A1
Принадлежит:

N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.

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11-04-2002 дата публикации

RETINOIDS FOR THE TREATMENT OF EMPHYSEMA

Номер: CA0002422805A1
Принадлежит:

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

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10-02-2000 дата публикации

PROPENAMIDES AS CCR5 MODULATORS

Номер: CA0002338804A1
Принадлежит:

This invention relates to substituted anilides which are modulators, agonists or antagonists, of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5.

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05-12-2002 дата публикации

CARBOXAMIDE-SUBSTITUTED PHENYLUREA DERIVATIVES AND METHOD FOR PRODUCTION THEREOF AS MEDICAMENTS

Номер: CA0002448023A1
Принадлежит:

The invention relates to carboxamide-substituted phenylurea derivatives and method for production thereof as medicaments, physiologically-acceptable salts and physiologically-functional derivatives thereof. Compounds of formula (I), in which the groups have the given meanings, the physiologically-acceptable salts and methods for production thereof are disclosed. Said compounds are suitable, for example, for the treatment of type II diabetes.

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23-10-2003 дата публикации

BICYCLIC AMIDES

Номер: CA0002481313A1
Принадлежит:

Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

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24-11-1994 дата публикации

BICYCLIC AMIDE DERIVATIVES AND THEIR USE AS MUSCLE RELAXANTS

Номер: CA0002355987A1
Принадлежит:

Novel compounds of formula (I): (See formula I) wherein R1, R2, R3 and R4 are each selected from hydrogen and fluoro and at least one and not more than two is fluoro; R5 is selected from hydrogen and C1-C4 alkyl; R6 is selected from hydrogen, C1-C4 alkyl and hydroxy; R7 is selected from hydrogen and hydroxy; R8 and R9 are each selected from hydrogen, C1,-C4 alkyl and cyclo (C3 or C4) alkyl or together with the nitrogen form a morpholino group; and X is selected from methylene and -O- and is always -O- when any of R5, R6 and R7 is other than hydrogen; and a salt or solvate thereof; have a number of uses in medicine in particular as central muscle relaxants.

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13-11-2003 дата публикации

PROCESS FOR PREPARATION OF POLYMORPHIC FORM II OF SERTRALINE HYDROCHLORIDE, PHARMACEUTICAL FORMULATIONS AND METHODS OF ADMINISTRATION THEREOF

Номер: CA0002483569A1
Принадлежит:

Provided are processes for preparation of crystalline sertraline hydrochloride form II substantilly free of other polymorphic forms of sertraline hydrochloride, preferably on an industrial scale.

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08-05-2007 дата публикации

NOVEL SUBSTITUTED CYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Номер: CA0002331870C
Принадлежит: LES LABORATOIRES SERVIER

L'invention concerne les composés de formule (I) : R-A-R' (I) dans laquelle : .cndot. A est tel que défini dans la description .cndot. R représente un groupement (voir formule), ou -NR'a R"a où R'a et R"a sont tels que définis dans la description, .cndot. R' représente un groupement -(CH2)T-R2 dans lequel t et R2 sont tels que définis dans la description. Les composés de la présente invention présentent des caractéristiques pharmacologiques très intéressantes concernant les récepteurs mélatoninergiques et peuvent être utilisés pour le traitement de pathologies liées au système mélatoninergique.

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28-02-2006 дата публикации

NOVEL SUBSTITUTED CYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

Номер: CA0002331877C
Принадлежит: LES LABORATOIRES SERVIER

L'invention concerne les composés de formule (I): R-A-R' (I) dans laquelle: .cndot. A est tel que défini dans la description .cndot. R représente un groupement (voir formule I, II, III ou IV) où E, Q, R1, R2, R3, v et R4 sont tels que définis dans la description .cndot. R' représente un groupement -(CH2)t-R5 dans lequel t et R5 sont tels que définis dans la description. Les composés de la présente invention présentent des caractéristiques pharmacologiques très intéressantes concernant les récepteurs mélatoninergiques et peuvent être utilisés pour le traitement de pathologies liées au système mélatoninergique.

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29-01-2008 дата публикации

INTERMEDIATES FOR PREPARING ARYLSULPHONAMIDES AND ANALOGUES

Номер: CA0002470183C
Принадлежит: BAYER AKTIENGESELLSCHAFT

Intermediates of formula (XV), (XVI) and (XVII): Cl-SO2-(CH2)h-U-(CH2)i-CR49R50-CF2-R51 (XV) Cl-SO2-CH2-CH2-CH2-CF3 (XVI) Cl-SO2-CH2-CH2-CH2-CF2-CF3 (XVII) for preparing aryl ether sulphonamides and analogues which have medicinal uses, wherein U represents O or a single bond, R49 and R50 independently represent H, F, Cl or CF3, R51 represents H, F, Cl or Br, h represents 1 or 2, and i represents 0 or 1.

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08-02-2011 дата публикации

LIGANDS THAT ARE INHIBITORS OF THE RAR RECEPTORS

Номер: CA0002484450C
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

Novel ligands that are inhibitors of the RAR receptors, process for preparing them and use thereof in human medicine and in cosmetics. The invention relates to novel bicyclic compounds corresponding to the general formula (I) below: R4 R5 X-R6 Q R2 R2 \ X-R1 R3 R3 t~~ and to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, or alternatively in cosmetic compositions.

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30-10-2014 дата публикации

ЗАМЕЩЕННОЕ ПРОИЗВОДНОЕ ЭТИЛЕНДИАМИНА ДЛЯ ЛЕЧЕНИЯ МИКОБАКТЕРИАЛЬНЫХ ЗАБОЛЕВАНИЙ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕГО ОСНОВЕ

Номер: EA0000020307B1

Изобретение относится к замещенным производным этилендиамина формулы где значения радикалов раскрыты в формуле изобретения, к фармацевтическим композициям, содержащим упомянутые выше соединения для лечения микобактериальных инфекций, и к медикаментам для лечения инфекционных заболеваний, включающим эффективное количество упомянутых соединений необязательно в комбинации с фармацевтически приемлемым носителем.

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30-12-2008 дата публикации

НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА IV АГОМЕЛАТИНА, СПОСОБ ЕЁ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, КОТОРЫЕ ЕЁ СОДЕРЖАТ

Номер: EA0000010867B1

Кристаллическая форма IV соединения формулы (I) которая характеризуется ее рентгеновской дифракционной порошкограммой. Лекарственные средства.

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30-10-2000 дата публикации

НОВЫЕ ЗАМЕЩЕННЫЕ ДИМЕРНЫЕ СОЕДИНЕНИЯ, СПОСОБ ИХ ПОЛУЧЕНИЯ И СОДЕРЖАЩАЯ ИХ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ

Номер: EA0200000261A2
Принадлежит:

Изобретение относится к соединениям формулы (I) A-G1-Cy-G2-Cy-G3-B (I) где A представляет собой группу NR1C(Q)R2, NR1C(Q)NR2R3 или C(Q)NR2R3, B представляет собой группу NR1C(Q)R2, C(Q)NR2R3, NR1C(Q)NR2R3, C(Q)OR1, NR1C(Q)OR2 и NR2R3, G1 и C3 являются необязательно замещенной алкиленовой цепью, Cy представляет собой циклическую структуру G2 представляет собой цепь Лекарственные препараты.

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30-10-2009 дата публикации

СПОСОБЫ И КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ АМИЛОИДНЫХ ЗАБОЛЕВАНИЙ

Номер: EA0000012429B1

Описаны способы, соединения, фармацевтические композиции и наборы для лечения или предупреждения амилоидных заболеваний.

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28-12-2012 дата публикации

ПРОИЗВОДНЫЕ ТЕТРАГИДРОНАФТАЛИН-1-КАРБОНОВОЙ КИСЛОТЫ, ИНГИБИРУЮЩИЕ МТР

Номер: EA0000017376B1

Настоящее изобретение относится к новым производным тетрагидронафталин-1-карбоновой кислоты, обладающим апоВ секрецией/МТР ингибирующей активностью и сопутствующей гиполипидемической активностью. Изобретение, кроме того, относится к способам получения таких соединений, фармацевтических композиций, включающих указанные соединения, а также к применению указанных соединений в качестве лекарственных средств для лечения атеросклероза, панкреатита, ожирения, гипертриглицеридемии, гиперхолестеролемии, гиперлипидемии, диабета и диабета II типа.

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29-11-2013 дата публикации

МОДУЛЯТОРЫ γ-СЕКРЕТАЗЫ

Номер: EA0000018862B1

Изобретение относится к соединениям с общей формулой I, как показано ниже; определения А, X, Y, R1 R2, R3 R4, R5, R6, R7, R8 и R9 приведены в спецификации. Соединения формулы I могут применяться для лечения заболеваний, связанных с активностью γ-секретазы, включая болезнь Альцгеймера.

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27-02-2007 дата публикации

НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА V АГОМЕЛАТИНА, СПОСОБ ЕЁ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, КОТОРЫЕ ЕЁ СОДЕРЖАТ

Номер: EA200601273A1
Принадлежит:

Кристаллическая форма V соединения формулы (I) которая характеризуется ее рентгеновской дифракционной порошкограммой. Лекарственные средства.

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27-02-2007 дата публикации

НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА III АГОМЕЛАТИНА, СПОСОБ ЕЁ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, КОТОРЫЕ ЕЁ СОДЕРЖАТ

Номер: EA200601274A1
Принадлежит:

Кристаллическая форма III соединения формулы (I) которая характеризуется ее рентгеновской дифракционной порошкограммой. Лекарственные средства.

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30-10-2009 дата публикации

ПРОИЗВОДНЫЕ ТЕТРАГИДРОНАФТАЛИН-1-КАРБОНОВОЙ КИСЛОТЫ, ИНГИБИРУЮЩИЕ МТР

Номер: EA200970399A1
Принадлежит:

Настоящее изобретение относится к новым производным тетрагидронафталин-1-карбоновой кислоты, обладающим apoB секрецией/MTP ингибирующей активностью и сопутствующей гиполипидемической активностью. Изобретение, кроме того, относится к способам получения таких соединений, фармацевтических композиций, включающих указанные соединения, а также к применению указанных соединений в качестве лекарственных средств для лечения атеросклероза, панкреатита, ожирения, гипертриглицеридемии, гиперхолестеролемии, гиперлипидемии, диабета и диабета II типа.

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10-08-2010 дата публикации

СУЛЬФОНИЛИРОВАННЫЙ ДИАМИН, СПОСОБ ЕГО ПОЛУЧЕНИЯ И ПРИМЕНЕНИЕ В КАТАЛИЗЕ ГИДРИРОВАНИЯ С ПЕРЕНЕСЕНИЕМ ВОДОРОДА

Номер: UA0000091527C2

Сульфонилированный диамин формулы (I), в которой А представляет собой водород или насыщенную или ненасыщенную С1-С20 алкильную группу или арильную группу; В представляет собой замещенную или незамещенную С1-С20 алкильную, циклоалкильную, алкиларильную, арилалкильную или арильную группу или алкиламиногруппу и по меньшей мере один из X1, X2, Y1, Y2 и Z является С1-С10 алкильным, циклоалкильным, алкиларильным, арилалкильным или алкокси заместителем, и в случае, когда X1, X2, Y1, Y2 и Z не является С1-С10 алкильным, циклоалкильным, алкиларильньим, арилалкильным или алкокси заместителем, тогда X1, X2, Y1, Y2 и Z представляют собой водород. Хиральный диамин применяют для приготовления катализаторов, пригодных для использования в реакциях гидрирования с перенесением водорода. (I) ...

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27-04-2007 дата публикации

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ЗАМЕЩЕННОГО ТЕТРАЛИНА И ЗАМЕЩЕННОГО ИНДАНА

Номер: EA200601927A1
Принадлежит:

Настоящее изобретение относится к новым способам получения производных замещенного тетралина и замещенного индана. Настоящее изобретение относится далее к новым способам получения промежуточных соединений при получении производных замещенного тетралина и замещенного индана.

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30-04-2010 дата публикации

СПОСОБЫ И КОМПОЗИЦИИ ДЛЯ ЛЕЧЕНИЯ АМИЛОИДНЫХ ЗАБОЛЕВАНИЙ

Номер: EA200900802A1
Принадлежит:

Описаны способы, соединения, фармацевтические композиции и наборы для лечения или предупреждения амилоидных заболеваний.

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30-12-2009 дата публикации

1,4-ДИАМИНОБИЦИКЛИЧЕСКИЕ АНАЛОГИ РЕТИГАБИНА КАК МОДУЛЯТОРЫ КАЛИЕВЫХ КАНАЛОВ

Номер: EA0200900749A1
Принадлежит:

Данное изобретение касается соединений формулы I, где G означает -О-, -S-, -C(g1)(g2)- или -NH-, a n=1, 2 или 3. Такие соединения модулируют калиевые каналы. Эти соединения применимы для лечения и профилактики таких заболеваний, на которые влияет модулирование калиевых ионных каналов. Одними из таких заболеваний являются эпилептические заболевания.

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25-12-2013 дата публикации

СПОСОБ СИНТЕЗА АГОМЕЛАТИНА

Номер: UA0000104123C2

Способ промышленного синтеза соединения формулы (I) (I).

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28-02-2008 дата публикации

АМИДНЫЕ ПРОИЗВОДНЫЕ В КАЧЕСТВЕ ЛИГАНДОВ ИОННЫХ КАНАЛОВ, ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ И СПОСОБЫ ИХ ПРИМЕНЕНИЯ

Номер: EA200701835A1
Принадлежит:

Описаны соединения, которые имеют формулу, представленную в описании. Соединения могут быть приготовлены в виде фармацевтических композиций и могут быть использованы для предупреждения и лечения целого ряда состояний у млекопитающих, в том числе у человека, и эти состояния включают, но без ограничения, боль, воспаление, травму и др.

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30-08-2010 дата публикации

ЗАМЕЩЕННОЕ ПРОИЗВОДНОЕ ЭТИЛЕНДИАМИНА ДЛЯ ЛЕЧЕНИЯ МИКОБАКТЕРИАЛЬНЫХ ЗАБОЛЕВАНИЙ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ЕГО ОСНОВЕ

Номер: EA201000643A1
Принадлежит:

Изобретение относится к замещенным производным этилендиамина формулы где значения радикалов раскрыты в формуле изобретения, к фармацевтическим композициям, содержащим упомянутые выше соединения, для лечения микобактериальных инфекций и к медикаментам для лечения инфекционных заболеваний, включающии эффективное количество упомянутых соединений необязательно в комбинации с фармацевтически приемлемым носителем.

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29-10-2010 дата публикации

РЕТИНОИДНОЕ ПРОЛЕКАРСТВЕННОЕ СОЕДИНЕНИЕ

Номер: EA0201070536A1
Принадлежит:

Предложено соединение общей формулы (I) где R1-R5 представляют собой атом водорода, алкильную группу или триалкилсилильную группу; Х представляет собой -NH-СО-, -CO-NH-, -N(COR6)-CO-, -CO-N(COR7)- (R6 и R7 представляют собой низшую алкоксигруппу или карбоксизамещенную фенильную группу) и т.д.; Z представляет собой -Y-CH(R12)-COOH, -СНО, -СН=СН-СООН или -COOR13 (Y представляет собой одинарную связь, -CH2-, -СН(ОН)-, -СО-, -CO-NH- или -CO-NH-CH2-CO-NH-, R12 представляет собой атом водорода или низшую алкильную группу и R13 представляет собой атом водорода, -СН(R14)-COOH (R14 представляет собой атом водорода, низшую алкильную группу или гидроксильную группу), -[СН2СН2-O]n-СН2-СН2-ОН, -СН2-O-[СН2СН2-O]m-СН2-ОН или -[СН(СН3)-СО-O]р-СН(СН3)-COOH (m, n и p представляют собой целое число от 1 до 100)), его соль или сложный эфир, которое обладает способностью превращаться в ретиноид после абсорбции in vivo.

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10-02-2009 дата публикации

СПОСОБ ПОЛУЧЕНИЯ ПРОИЗВОДНЫХ ЗАМЕЩЕННЫХ ТЕТРАЛИНОВ И ЗАМЕЩЕННЫХ ИНДАНОВ

Номер: UA0000085589C2

Изобретение относится к новым способам получения производных замещенных тетралинов и замещенных инданов. Изобретение, кроме того, относится к новым способам получения промежуточных соединений при получении производных замещенных тетралинов и замещенных инданов.

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27-02-2007 дата публикации

НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА IV АГОМЕЛАТИНА, СПОСОБ ЕЁ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, КОТОРЫЕ ЕЁ СОДЕРЖАТ

Номер: EA0200601271A1
Принадлежит:

Кристаллическая форма IV соединения формулы (I) которая характеризуется ее рентгеновской дифракционной порошкограммой. Лекарственные средства.

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27-10-2008 дата публикации

АЦЕТИЛ 2-ГІДРОКСИ-1,3 ДІАМІНОАЛКАНИ

Номер: UA0000084407C2

Розкрито сполуки формули: , де змінні Z, X, R15, R2, R3 та Rc відповідають визначенням, поданим в описі. Сполуки, розкриті в описі, є інгібіторами ферменту бета-секретази і тому є корисними для лікування хвороби Альцгеймера та інших захворювань, які характеризуються відкладенням пептиду А-бета в організмі ссавців.

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30-06-2005 дата публикации

ЗАМЕЩЕННЫЕ СОЕДИНЕНИЯ БИФЕНИЛА, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, СОДЕРЖАЩИЕ ИХ

Номер: EA0000005766B1

Изобретение относится к соединениям формулы (I) в которой В обозначает атом водорода, COOR группу, CONRR' группу или (С1-С6)алкильную группу, замещенную COOR, CONRR' или OR группой, G1 обозначает -X'-(CH2)n-X-(CH2)m-X"-цепь, в которой X, X", X", n и m принимают значения, указанные в описании, Су обозначает группу формулы (II) или (III) G2 обозначает алкиленовую цепь, такую, как указано в описании, и А обозначает NRCOR', NRCSR', CONRR', CSNRR', NRCONR'R" или NRCSNR'R" группу. Медикаменты.

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27-02-2007 дата публикации

НОВЫЙ СПОСОБ СИНТЕЗА (7-МЕТОКСИ-1-НАФТИЛ)АЦЕТОНИТРИЛА И ЕГО ПРИМЕНЕНИЕ ПРИ СИНТЕЗЕ АГОМЕЛАТИНА

Номер: EA0000007787B1

Способ промышленного синтеза соединения формулы (I) Применение при синтезе агомелатина.

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27-02-2007 дата публикации

НОВЫЙ СПОСОБ СИНТЕЗА (7- МЕТОКСИ-1-НАФТИЛ)АЦЕТОНИТРИЛА И ЕГО ПРИМЕНЕНИЕ ПРИ СИНТЕЗЕ АГОМЕЛАТИНА

Номер: EA0000007789B1

Способ промышленного синтеза соединения формулы (I) Применение при синтезе агомелатина.

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28-12-2007 дата публикации

АЦЕТИЛ 2-ГИДРОКСИ-1,3-ДИАМИНОАЛКАНЫ

Номер: EA0000009196B1

Раскрываются соединения формулы I, где переменные Z, X, R15, R2, R3 и Rc имеют определенное выше значение. Раскрываемые соединения являются ингибиторами фермента бета-секретазы и поэтому полезны при лечении болезни Альцгеймера и других заболеваний, характеризующихся отложениями А бета-пептида в организме млекопитающих.

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28-02-2008 дата публикации

ЗАМЕЩЁННЫЕ ТЕТРАЛИНЫ И ИНДАНЫ И ИХ ПРИМЕНЕНИЕ

Номер: EA0000009554B1

Настоящее изобретение относится к производным тетралинов и инданов, композициям, содержащим их, и способам их применения в качестве модуляторов PPAR альфа для лечения или ингибирования развития, например, диабета.

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28-02-2008 дата публикации

ЗАМЕЩЁННЫЕ ТЕТРАЛИНЫ И ИНДАНЫ

Номер: EA0000009553B1

Данное изобретение относится к соединениям тетралина и индана, содержащим их композициям и способам применения их в качестве АППР альфа модуляторов для лечения или ингибирования развития, например, дислипидемии.

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30-12-2008 дата публикации

НОВАЯ КРИСТАЛЛИЧЕСКАЯ ФОРМА V АГОМЕЛАТИНА, СПОСОБ ЕЁ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ, КОТОРЫЕ ЕЁ СОДЕРЖАТ

Номер: EA0000011030B1

Кристаллическая форма V соединения формулы (I) которая характеризуется ее рентгеновской дифракционной порошкограммой. Лекарственные средства.

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30-09-2014 дата публикации

ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ АГОМЕЛАТИНА И СПОСОБ ИХ ПОЛУЧЕНИЯ

Номер: EA0000020271B1

Настоящее изобретение относится к промежуточным соединениям для получения агомелатина, так же, как и к способам их получения. Промежуточное соединение настоящего изобретения для получения агомелатина представляет собой соединение А в соответствии с следующей формулой. Также обеспечены два новых промежуточных соединения. Когда применяются эти новые промежуточные соединения для получения агомелатина, способ является простым для управления, хорошо контролируемым и дает продукт с высокой чистотой, без сложных операций, таких как ректификация и разделение хроматографией на колонке, и является подходящим для промышленного производства. При этом способы получения самих двух новых промежуточных соединений являются простыми и с высоким выходом, только когда применяют наиболее широкоиспользуемый 7-метокситетралон в качестве исходного стартового материала и проводят одну стадию реакции для получения промежуточных соединений, с последующей еще одной стадией преобразования промежуточного соединения ...

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15-09-2010 дата публикации

Compounds for use in imaging, diagnosing, and/or treatment of diseases of the central nervous system or of tumors

Номер: CN0101835728A
Принадлежит:

This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).

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10-07-2013 дата публикации

Drug derivatives

Номер: CN103201260A
Принадлежит:

The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state.; In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention ...

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03-07-2002 дата публикации

Process for preparing tetrahydronaphthalene derivative

Номер: CN0001356303A
Принадлежит:

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30-07-2003 дата публикации

Method of producing 2-substituted-3,4-fused heterocycle benzoic acid

Номер: CN0001116271C
Принадлежит:

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13-05-2009 дата публикации

Process for producing amine derivatives

Номер: CN0100486957C
Принадлежит:

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09-11-1979 дата публикации

DERIVES DU STILBENE, LEUR PREPARATION ET LEUR APPLICATION EN TANT QUE MEDICAMENTS

Номер: FR0002422620A
Автор: PETER LOELIGER
Принадлежит:

Dérivés du stilbène, leur préparation et leur application en tant que médicaments. Les composés selon l'invention ont pour fomule : ...

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31-03-1989 дата публикации

Derives d'alcadienes, leurs preparations, les medicaments les contenant et produits intermediaires

Номер: FR0002621038A
Принадлежит:

Composes de formule :dans laquelle R1 = hydroxy ou acetoxy, R2 = hydrogene, carboxy, alcoxycarbonyle ou phenyle et - soit R3 = alkylthio ou alcoxy et R4 = naphtoyle ou benzoyle eventuellement substitue, - soit R3 = alcoxycarbonyle, cycloalkyloxycarbonyle ou cyano et R4 = alkyle, phenyle eventuellement substitue, benzylthio, eventuellement substitue, phenylthio eventuellement substitue, naphtylthio, phenethylthio ou allylthio, - soit R3 et R4 forment avec l'atome de carbone auquel ils sont rattaches un cycle : dans lesquelles R5 = hydrogene ou alcoxy et X = methylene ou S. Procedes de preparation de ces composes, produits intermediaires pour leur preparation et medicaments les contenant.

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29-09-2000 дата публикации

NEW DERIVATIVES DIMERIQUES SUBSTITUTE, THEIR METHOD OF PREPARATION AND THE COMPOSITIONS PHARMACEUTICAL WHICH CONTAIN THEM

Номер: FR0002791344A1
Принадлежит:

L'invention concerne les composés de formule (I). A-G1-Cy-G2-Cy-G3-B dans laquelle : - A, B, représentent un groupement NR1C (Q) R2 , C (Q) NR1R2 ou NR1C (Q) NR2R3, - G1 , G3 représentent une chaîne alkylène éventuellement substituée, - Cy représente une structure cyclique - G2 représente une chaîne Médicaments.

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03-05-1991 дата публикации

Procédé pour la préparation énantiosélective de 2-aminotétralines.

Номер: FR0002653765A
Принадлежит:

L'invention concerne un procédé pour la préparation énantiosélective de 2-aminotétralines de formule (I) (CF DESSIN DANS BOPI) dans laquelle R représente l'hydrogène ou un groupe alkyle inférieur et l'astérisque dénote que l'atome de carbone ainsi marqué a une configuration absolue détérminée, et de leurs sels d'addition d'acides, en partant d'un éther de phénol de formule (CF DESSIN DANS BOPI) dans laquelle Rdegré est un groupe alkyle inférieur et de l'anhydride de l'acide N-trifluoroacétyl-aspartique optiquement actif de formule (CF DESSIN DANS BOPI) par les nouveaux intermédiaires de formule (CF DESSIN DANS BOPI) dans laquelle Rdegré et l'astérisque ont la signication donnée ci-dessus et X représente un atome d'oxygène ou deux atomes d'hydrogène.

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27-11-1987 дата публикации

DERIVES DE TETRAHYDRONAPHTALENE ET D'INDANE, UTILISATION POUR LA FABRICATION DE PREPARATIONS PHARMACEUTIQUES ET PROCEDE D'OBTENTION.

Номер: FR0002599027A
Принадлежит:

COMPOSES DE FORMULE GENERALE: (CF DESSIN DANS BOPI) DANS LAQUELLE X ET Y SONT -CH- OU C(CH); Z EST UN RESTE -CHR-, CO, CROR, -CHR-CHR-, -CHOR-CH, -CO-CHOR OU -CHOR-CHOR-; R EST LE FLUOR, CHLORE, IODE, O- OU M-BROME, UN ALCOXY INFERIEUR, ACYLOXY, NITRO, HYDROXY, AMINO, ALKYLAMINO INFERIEUR, DI-ALKYL (INFERIEUR) AMINO OU PHENYLE; OU UN ALKYLE INFERIEUR EN POSITION O- OU M-; R ET R SONT L'HYDROGENE, TRIFLUOROMETHYLE OU HALOGENE ET L'UN DES RESTES R ET R EST L'HYDROGENE, LE TRIFLUOROMETHYLE OU UN ALKYLE INFERIEUR, R ET R SONT L'HYDROGENE, UN ALKYLE, ALCOXY OU HALOGENE; R EST L'HYDROGENE, UN HALOGENE, UN ALKYLE INFERIEUR OU UN RESTE -OR; R EST L'HYDROGENE, UN ALKYLE INFERIEUR OU ACYLE; R EST L'HYDROGENE OU UN ALKYLE INFERIEUR; M EST UN NOMBRE ENTIER DE 0 A 5; PLUSIEURS RESTES PRESENTS R, R OU R PEUVENT ETRE DIFFERENTS L'UN PAR RAPPORT A L'AUTRE; R EST L'HYDROGENE QUAND SIMULTANEMENT Z -CH-CH- ET M 0; AVEC L'EXCEPTION DU 1, 2, 3, 4-TETRAHYDRO-1, 1, -4,4-TETRAMETHYL-6-(A-METHYLSTYRYL) NAPHTALENE ...

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03-03-2006 дата публикации

ABCA-1 ELEVATING COMPOUNDS

Номер: KR0100555192B1
Автор:
Принадлежит:

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07-03-2006 дата публикации

NEW GAMMA SELECTIVE RETINOIDS

Номер: KR1020060021416A
Принадлежит:

New RAR selective retinoid agonists of formula (I) wherein the symbols are as defined in the specification, and pharmaceutically active salts of carboxylic acids of formula (I), further the invention relates to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor γ(RARγ) selective agonists for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumours and precancerous changes of the mucous membrane in the mouth, tongue, larynx, oesophagus, bladder, cervix and colon. © KIPO & WIPO 2007 ...

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07-10-2005 дата публикации

ARYL SULFONAMIDES AND ANALOGUES THEREOF AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES

Номер: KR1020050097554A
Принадлежит:

The present invention relates to novel aryl sulfonamides and analogues thereof, methods for producing same and their use in the treatment of neurodegenerative diseases, in particular the prophylaxis and treatment of neurodegenerative diseases, and notably for the treatment of cerebral stroke and craniocerebral trauma. © KIPO & WIPO 2007 ...

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12-01-2005 дата публикации

4-(METHYLSULFONYLAMINO)PHENYL ANALOGUE AS VANILLOID RECEPTOR ANTAGONIST SHOWING EXCELLENT ANALGESIC ACTIVITY AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME

Номер: KR1020050004006A
Принадлежит:

PURPOSE: A 4-(methylsulfonylamino)phenyl analogue and a pharmaceutical composition containing the same are provided to function as potent vanilloid receptor antagonists and analgesics and thus to alleviate or relieve acute, chronic or inflammatory pains, to suppress inflammation, and to prevent or treat urinary diseases. CONSTITUTION: The 4-(methylsulfonylamino)phenyl analogue is represented by the formula I, wherein A is CONH, NHCO, NHC(=S)NH, NHC(=O)NH, each of R1 to R4 is independently hydrogen, halogen, cyano, nitro, a lower alkylamine, C1-C3-alkoxy, carboxylic acid, hydroxamic acid, C1-C6-alkylester, C1-C6-alkylamide, benzylamide, a 5- or 6-membered heterocyclic group, each of R5 and R6 is independently at least one hydrogen, hydroxy, amine, a linear or branched C1-C6-alkyl, a cycloalkyl, a substituted or non-substituted phenyl and benzyl, provided that both of R5 and R6 are not hydrogen, B is selected from (I-1), (I-2) and (I-3), and the asterisk mark * indicates a chiral carbon atom ...

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07-06-2007 дата публикации

NEW PROCESS FOR THE SYNTHESIS OF ENEAMIDE DERIVATIVES

Номер: KR1020070057693A
Принадлежит:

A process for the production of ene- amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, -CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or -COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is ...

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02-06-2003 дата публикации

NAPHTHALENE DERIVATIVES

Номер: KR20030043994A
Принадлежит:

The present invention relates to naphthalene derivatives of formula (I), wherein X is S, S(O), S(O) 2, S(O)2NH, P(O)OCH3, P(O)OH, NH, N(CH3), NHC(O)NH, C(O), C(O)O, NHC(O), CH(OH), CH=N, CH=CH, CH2NH, C(=NH) ; R1 is aryl or heteroaryl; R2 is hydrogen, OR4 or NR5R6 and the other variables are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals in treating or preventing a disease or condition in which cannobinoid receptor activation plays a role or is implicated. © KIPO & WIPO 2007 ...

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03-06-2008 дата публикации

ORGANIC COMPOUNDS

Номер: KR1020080049027A
Принадлежит:

The invention relates to novel diamines of the formula (I) in which all variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them. © KIPO & WIPO 2008 ...

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16-03-2006 дата публикации

MERCAPTOAMIDES AS HISTONE DEACETYLASE INHIBITORS

Номер: WO2006028972A2
Принадлежит:

Mercaptoamide compounds, represented by Formulas (IA), (IB), (IIA), and (IIB): or a pharmaceutically acceptable salt thereof, inhibit histone deacetylase enzyme and are useful for the treatment and/or prevention of various infections, cancerous diseases, and conditions.

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10-01-2013 дата публикации

DEUTERATED PHENYLPROPIONIC ACID DERIVATIVE

Номер: WO2013005753A1
Принадлежит:

A compound, in which some or all of the hydrogen atoms of the ethylene group constituting propionic acid in 3-[4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]phenyl]propionic acid have been substituted with deuterium, or a salt thereof, or an ester thereof, and a prodrug for releasing Am80 as an active medicament after absorption in the body, which comprises the compound or a salt thereof, or an ester thereof as an active ingredient.

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13-11-2014 дата публикации

PRO-FRAGRANCE COMPOUNDS

Номер: WO2014180782A1
Принадлежит:

A compound of Formula (I) wherein R1 represents a C3 to C20 hydrocarbon group derived from a fragrant alcohol of formula R1OH or from a fragrant aryl aldehyde or ketone of Formula (II), wherein: R2 is, independently, hydrogen atom, hydroxyl group, acetoxy group, -O(C=O)CH(CH3), optionally substituted C1-C6 alkyl group or C1-C6 alkoxy group, wherein any two of R2 may form an optionally substituted 5 or 6 membered ring, and R1 represents a radical derived from a fragrant alcohol of formula R1OH or from a fragrant aldehyde or from a fragrant aryl aldehyde or ketone of formula (II). The compounds are useful for example as a precursor for the prolonged delivery or release of fragrant compounds such as fragrant alcohols or aldehydes.

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07-06-2007 дата публикации

NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING SAME, AND USES OF THOSE

Номер: WO000002007063789A1
Принадлежит:

Disclosed are a compound having a strong COMT inhibitory effect and represented by the general formula (I) below, a pharmacologically acceptable salt thereof, a pharmaceutical composition containing either of them, and uses of them. (I) (In the formula, R1 and R2 independently represent a hydrogen, a lower acyl, a lower alkoxycarbonyl or the like; R3 represents a nitro or cyano; R4 and R5 independently represent a hydrogen, a lower alkyl or the like; and R6, R7, R8, R9 and R10 independently represent a hydrogen, a halogen, a lower alkyl, a halogenated lower alkyl, a lower alkenyl, a lower alkoxy, a halogenated lower alkoxy, a carboxy, a lower alkoxycarbonyl, a lower acyl, a lower alkylsulfonyl, a cyano or the like.) ...

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28-08-2014 дата публикации

BICYCLIC COMPOUNDS

Номер: WO2014130752A3
Принадлежит:

Disclosed are compounds of Formula (I) and/or a salt thereof; wherein R is -OH or -OP(O)(OH)2. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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12-06-1997 дата публикации

PROCESS FOR PREPARATING OPTICALLY ACTIVE COMPOUNDS

Номер: WO1997020789A1
Принадлежит:

A novel and practically excellent process for preparing optically active compounds, such as optically active alcohols or amines, useful for various applications of, for example, synthetic intermediates of pharmaceuticals, liquid crystalline materials, and reagents for optical resolution, wherein a hydrogen transfer type asymmetric reduction is carried out in the presence of both a transition metal complex and an optically active nitrogen compound or a transition metal complex having an optically active nitrogen compound as an asymmetric ligand, and a hydrogen-donating organic or inorganic compound. Further, optically active secondary alcohols are prepared from racemic secondary alcohols or meso-diols by a hydrogen transfer oxidation.

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06-01-2005 дата публикации

NOVEL THERAPEAUTIC AGENTS FOR THE TREATMENT OF CANCER, METABOLIC DISEASES AND SKIN DISORDERS

Номер: WO2005000233A2
Принадлежит:

The present invention is directed to compounds having the structure (I) wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

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13-12-2001 дата публикации

FACTOR VIIA INHIBITORY (THIO)UREA DERIVATIVES, THEIR PREPARATION AND THEIR USE

Номер: WO0000194301A3
Принадлежит:

The present invention relates to compounds of formula (I), in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula (I) are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula (I), their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.

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12-02-2009 дата публикации

PYRROLIDINES AS CATALYST COMPOUNDS

Номер: WO000002009019469A9
Принадлежит:

The present invention relates to compounds for use as catalysts, methods for producing said compounds and the use of said compounds as catalysts in catalytic processes including, but not limited to, the asymmetric reduction of imine and enamine compounds and/or the reductive animation of ketone compounds. A compound for use as a catalyst has the formula (I) wherein: R1, R2, R3, R4 and R5 are each separately selected from the group consisting of hydrogen, alkyl and aryl; X is oxygen or sulfur; and Z has the formula (II) wherein: R6 and R7 are each separately selected from the group consisting of hydrogen, alkoxy, nitro, halogen, alkyl and aryl, or R6 and R7 are linked to form a cyclic group; and Y is oxygen, sulfur or NR10 in which R10 is selected from the group consisting of hydrogen, alkyl and aryl.

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30-08-2007 дата публикации

DIARYL COMPOUNDS AS NON-STEROIDAL INHIBITORS OF 17-BETA HYDROXYSTEROID DEHYDROGENASE AND/OR STEROID SULPHATASE FOR THE TREATMENT OF OESTROGEN-RELATED DISEASES SUCH AS HORMONE DEPENDENT BREAST CANCER

Номер: WO000002007096647A3
Принадлежит:

There is provided a compound of Formula (I): wherein R3, R4, R5, R6, R7, R9, and R10, are independently selected from -H, -OH, hydrocarbyl groups, oxyhydrocarbyl groups, cyano (-CN), nitro (-NO2), and halogens; wherein ring A is optionally further substituted wherein X is a bond or a linker group wherein (A) (i) R9 is selected from alkyl and halogen groups; and (ii) R10 is selected from -OH, oxyhydrocarbyl and -OSO2NR1R2; wherein R1 and R2 are independently selected from H and hydrocarbyl or (B) at least one of R3, R4, R5, R6 and R7 is the group -C(=0)-CR11 R12-R8 wherein R8 is a selected from (i) an alkyloxyalkyl group (ii) a nitrile group, (iii) alkylaryl group, wherein the aryl group is substituted by other than a C1-10 group (iv) alkenylaryl group wherein the aryl group is substituted (v) alkylheteroaryl group, wherein when heteroaryl group comprises only C and N in the ring, the aryl group is substituted by other than a methyl group (vi) alkenylheteroaryl group (vii) =N-O-alkyl or ...

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06-10-2011 дата публикации

OCTAHYDROBINAPHTHOL DERIVATIVE FOR L/D OPTICAL CONVERSION AND OPTICAL RESOLUTION

Номер: WO2011122917A3
Автор: KIM, Kwan-Mook
Принадлежит:

The present invention relates to an octahydrobinaphthol derivative which recognizes an amino acid and amino alcohol in a chiral-selective manner, converts L-amino acid into D-amino acid, and performs optical resolution on an amino acid and amino alcohol with high efficiency.

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26-04-2012 дата публикации

CHEMOSENSORY RECEPTOR LIGAND-BASED THERAPIES

Номер: WO2012054526A3
Принадлежит:

Provided herein are methods for treating conditions associated with a chemosensory receptor, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administering a composition comprising a chemosensory receptor ligand. Also provided herein are chemosensory receptor ligand compositions and methods for the preparation thereof for use in the methods of the present invention.

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24-08-1995 дата публикации

SUBSTITUTED BIPHENYL DERIVATIVES AS PHOSPHODIESTERASE INHIBITORS

Номер: WO1995022520A1
Принадлежит:

L'invention concerne un composé ayant la formule (I). Dans cette fomule, lorsque R8 = H, R1 = alkyle, cycloalkyle, arylalkyle, aryle; R2 = cycloalkyle, aryle, C3-C10 alkyle; X, Y = O, S(O)n, NH; Z = CH2OH, NHSO2R3, CHO, CO2R3, CONHR4R5, CN, COR6, H, halo, NHCN, NHCONR4R5, CONR4OR5, CONR4NR5R6, 1-tétrazole, S(O)nOH, S(O)nNR3R4, C=NOH, C(=N(OH)NH2, OCONR7R6, P(O)(OR4)2, NH2, SH, OH, OS(O)2R3, C(O)CO2R3, C(O)CONR3R4, CH(OH)CO2R3, CHFCO2R3, CF2CO2R3, CH(OH)CONR3R4, CF2CONR3R4, C=NNH2, C(=NOC(=O)R3)R4, C(=NNHC(=O)R3)R4, C(=NOH)R3, C(=NNR3)R4, NHC(=O)R6 or C(O)CONH2; R3, R4, R5, R6, R7 = hydrogène, alkyle, aryle, aryalkyle, cycloalkyle, ou fluoroalkyle; ou un composé de la formule (I), où R1 = alkyle, cycloalkyle, aryalkyle, or aryle; R2 = cycloalkyle, aryle, ou alkyle; X, Y = CH2, O, S(O)n), ou NH; R3, R4, R5, R6, R7 sont chacun d'une manière indépendante un hydrogène, alkyle, aryle, aryalkyle, cycloalkyle, ou fluoroalkyle; R8 = CO2R3, CONR3, ou R8 et Z sont reliés pour que R8Z = C(O)NHNHC(O ...

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11-07-1996 дата публикации

Номер: WO1996020930A1
Автор:
Принадлежит:

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11-12-2003 дата публикации

LIGANDS THAT ARE INHIBITORS OF THE RAR RECEPTORS

Номер: WO2003101945A1
Принадлежит:

Novel ligands that are inhibitors of the RAR receptors, process for preparing them and use thereof in human medicine and in cosmetics. The invention relates to novel bicyclic compounds corresponding to the general formula (I) and to the method for preparing them, and to their use in pharmaceutical compositions intended for use in human or veterinary medicine, or alternatively in cosmetic compositions.

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03-01-2008 дата публикации

CXCR2 INHIBITORS

Номер: WO000002008000410A1
Принадлежит:

The invention relates to compounds of the formula (I), in which R1, R2, A, B, X and Y have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.

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25-07-1996 дата публикации

Номер: WO1996022288A1
Автор:
Принадлежит:

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23-10-1997 дата публикации

PHENYLETHANOLAMINOTETRALINCARBOXAMIDE DERIVATIVES

Номер: WO1997038970A1
Принадлежит:

Phenylethanolaminotetralincarboxamide derivative represented by general formula (I) and pharmacologically acceptable salts thereof, wherein A represents lower alkylene; B represents amino, di(lower alkyl)amino or 3- to 7-membered alicyclic amino which may bear oxygen on the ring; the asterisked carbon atom represents a carbon atom with an R- or S-configuration or a mixture of such atoms; and the carbon atom labeled with (S) represents a carbon atom with an S-configuration. These compounds have selective 'beta'2-adrenergic receptor stimulating effects while reducing the burden on the heart, such as tachycardia, and are useful as preventives for threatened abortion and premature birth, bronchodilator, and agents for remission and lithagogue for urinary calculus.

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25-05-2001 дата публикации

HYDRAZONE COMPOUNDS AND PESTICIDES

Номер: WO0000136381A1
Принадлежит:

Cette invention concerne des composés hydrazone représentés par la formule (1) ou des sels de ces composés ainsi que de nouveaux produits chimiques destinés à l'agriculture (en particulier des pesticides et des miticides renfermant cet ingrédient actif). Dans la formule (I), A représente -CH¿2-, -CH¿2CH¿2-, -OCH¿2-, etc; B représente une liaison unique, oxygène, soufre, etc. ; G représente un groupe de formule G-1, G-2 ou G-3 ; Q1¿ et Q¿2 représentent chacun indépendamment hydrogène, alkyle en C¿1-12, haloalkyle en C¿1-12, etc.; W1¿, W2¿ et W3¿ représentent chacun indépendamment oxygène, soufre, etc. ; X représente hydrogène, halogéno, cyano, etc.; R1¿, R2¿, R5¿, R7¿ et R8¿ représentent chacun indépendamment hydrogène, alkyle en C¿1-6, haloalkyle en C¿1-6, etc.; R6¿ et R9¿ représente chacun indépendamment alkyle en C¿1-6, haloalkyle en C¿1-6, etc.; et m est un entier compris entre 1 et 4.

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31-12-2003 дата публикации

AMINOALKYLPHENOLS, METHODS OF USING AND MAKING THE SAME

Номер: WO2004000783A1
Принадлежит:

The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.

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08-09-2005 дата публикации

Compounds and methods for treatment of cancer and modulation of programmed cell death for melanoma and other cancer cells

Номер: US20050197511A1
Принадлежит:

Compounds and related methods for synthesis, and the use of compounds and combination therapies for the treatment of cancer and modulation of apoptosis in cells are disclosed. The generation of synthetic combinatorial libraries and the evaluation of library member compounds regarding induction of apoptosis selectively in cancer cells are disclosed. Compounds, methods of making the compounds, and therapeutic methods with application against breast cancer cells, melanoma cancer cells, colon cancer cells, and other cancer cells are described.

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20-10-2005 дата публикации

Anthracene derivatives and organic electroluminescent devices made by using the same

Номер: US20050233165A1
Принадлежит:

An anthracene derivative represented by the following general formula (1) which enables an organic electroluminescence device to exhibit a great efficiency of light emission and uniform light emission even at high temperatures since crystallization is suppressed and no thermal decomposition takes place during vapor deposition and an organic electroluminescence device utilizing the derivative, are provided. [Ar represents a group represented by the following general formula (2): (L1 and L2 each represent a substituted or unsubstituted methylene group, ethylene group or the like, and at least one of them is present), Ar′ represents a substituted or unsubstituted aryl group having 6 to 50 nuclear carbon atoms, X represent an alkyl group or the like, a and b each represent an integer of 0 to 4, and n represents an integer of 1 to 3.] ...

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25-10-2007 дата публикации

Biaromatic compounds and cosmetic/pharmaceutical applications thereof

Номер: US20070249710A1
Принадлежит: GALDERMA RESEARCH & DEVELOPMENT

Novel biaromatic compounds having the structural formula (I): have a selective agonist activity with respect to the RAR-gamma receptor and are useful for combating skin aging and for treating, e.g., cell differentiation or proliferation disorders, pathologies related to keratinization disorders, acne and psoriasis.

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18-01-2007 дата публикации

NPY Y5 antagonist

Номер: US20070015762A1
Принадлежит:

The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof ...

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05-01-2017 дата публикации

N-SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF

Номер: US20170002017A1
Принадлежит:

The invention provides novel compounds having the general formula: 3. The compound of wherein B is N and Ris absent.4. The compound of wherein B is C.5. The compound of wherein R claim 1 , Rand Rare each independently selected from H claim 1 , F claim 1 , or Cl.6. The compound of wherein Ris H claim 1 , F or Cl; Rand Rare each H; and Ris an optionally substituted group selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —CN claim 1 , Calkyl claim 1 , Chaloalkyl claim 1 , Ccycloalkyl claim 1 , and Calkoxy.7. The compound of wherein Ris Calkyl claim 1 , Chaloalkyl claim 1 , Ccycloalkyl or —NRR.8. The compound of claim 7 , wherein Ris selected from the group consisting of methyl claim 7 , ethyl claim 7 , propyl claim 7 , trifluoromethyl claim 7 , difluoromethyl claim 7 , monofluoromethyl claim 7 , isopropyl and cyclopropyl.11. The compound of wherein Ris selected from the group consisting of: methyl claim 1 , ethyl claim 1 , tert-butyl claim 1 , dimethylamino claim 1 , methylamino claim 1 , amino claim 1 , morpholino claim 1 , azetidino claim 1 , imidazolyl claim 1 , 3-hydroxyazetidino claim 1 , 3-fluoroazetidino claim 1 , cyclopropyl claim 1 , pyrrolidinyl claim 1 , 3 claim 1 ,3-difluoroazetidino claim 1 , tert-butyl claim 1 , ethyl claim 1 , 2-methoxyethyl claim 1 , 3-methoxyazetidino claim 1 , 2-hydroxyethyl claim 1 , 3-hydroxypyrrolidinyl claim 1 , and N-methylimidazolyl.12. The compound of wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)- is an optionally substituted group selected from the group consisting of Calkylene claim 1 , Calkenylene or Calkynylene.13. The compound of claim 1 , wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)- is selected from the group consisting of —CH— claim 1 , —C(═O)— claim 1 , —C(H)(CH)— claim 1 , —CH—CH— claim 1 , —CH—C(H)(CH)— claim 1 , —C(H)(CH)—C(H)— claim 1 , —CHCHCH— claim 1 , —CH—C(H)(CH)—CH— or —CHCHCHCH—.14. The compound of claim 13 , ...

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12-01-2017 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20170008859A1

The invention provides compounds and compositions that are useful for treating conditions including Alzheimer's disease, Parkinson's disease, diabetes, cancer, and psychotic disorders such as schizophrenia. 5. The compound of which is a compound of formula IV claim 1 , wherein Ris ethyl or isopropyl; or a salt thereof.11. A pharmaceutical composition comprising a compound as described in or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier.12. A method for treating Alzheimer's disease claim 1 , Parkinson's disease claim 1 , diabetes claim 1 , cancer claim 1 , or a psychotic disorder in an animal comprising administering a compound as described in or a pharmaceutically acceptable salt thereof claim 1 , to the animal.1314-. (canceled) This invention was made with government support under R15 CA139364 awarded by the National Institutes of Health. The government has certain rights in the invention.The human retinoid X receptors (hRXRs) consist of three identified isoforms (α, β, γ) that function as transcription promoters often in partnership with other members of a larger nuclear receptor (NR) family of transcription regulators including the thyroid receptor (TR), the vitamin D receptor (VDR), the liver X receptor (LXR), the peroxisome proliferator-activated receptor (PPAR), and the retinoic acid receptor (RAR). While 9-cis-retinoic acid (9-cis-RA) and docosahexaenoic acid (DHA) have been shown to bind to hRXRs and promote RXR element (RXRE) regulated transcription (i.e. function as RXR agonists), it is still unclear if RXR has a bona fide endogenous molecular ligand. RXR has been described as the central NR regulator, because it often plays a critical role, either as a permissive or non-permissive partner, in heterodimer complexes that must be formed with the other NRs to regulate their respective response elements.Recent studies have identified several RXR-selective-binding molecular ligands (rexinoids) that can modulate ...

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21-01-2016 дата публикации

RESINS FOR UNDERLAYERS

Номер: US20160016872A1
Принадлежит:

Polymeric reaction products of certain substituted tetraarylmethane monomers are useful as underlayers in semiconductor manufacturing processes. 2. The polymeric reaction product of wherein AG is OR.5. The polymeric reaction product of wherein Ar claim 1 , Ar claim 1 , Arand Arare independently chosen from phenyl claim 1 , biphenyl claim 1 , naphthalenyl claim 1 , anthracenyl claim 1 , phenanthrenyl claim 1 , pyrenyl claim 1 , tetracenyl claim 1 , triphenylenyl claim 1 , tetraphenyl claim 1 , benzo[f]tetraphenyl claim 1 , benzo[m]tetraphenyl claim 1 , benzo[k]tetraphenyl claim 1 , pentacenyl claim 1 , perylenyl claim 1 , benzo[a]pyrenyl claim 1 , benzo[e]pyrenyl claim 1 , benzo[ghi]perylenyl claim 1 , coronenyl claim 1 , quinolonyl claim 1 , 7 claim 1 ,8-benzoquinolinyl claim 1 , fluorenyl claim 1 , chrysenyl claim 1 , triphenylenyl claim 1 , and 12H-dibenzo[b claim 1 ,h]fluorenyl.6. A composition comprising the polymeric reaction product of claim 1 , an organic solvent claim 1 , and optionally one or more additives chosen from curing agents and surfactants.7. The composition of wherein the curing agent is an acid or a thermal acid generator.8. A method of forming a patterned layer comprising disposing a layer of the composition of on a substrate; removing organic solvent to form a polymeric underlayer; disposing a layer of a photoresist on the polymeric underlayer; exposing the photoresist layer to actinic radiation through a mask; developing the exposed photoresist layer to form a resist pattern; and transferring the pattern to the polymeric underlayer to expose portions of the substrate. The present invention relates generally to field of manufacturing electronic devices, and more specifically to the field of materials for use in semiconductor manufacture.It is well-known in lithographic processes that a resist pattern can collapse due to surface tension from the developer used if the resist pattern is too tall (high aspect ratio). Multilayer resist processes ( ...

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21-01-2016 дата публикации

PREPARATION OF CHIRAL AMIDES AND AMINES

Номер: US20160016891A1
Принадлежит:

This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.

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04-02-2016 дата публикации

Cycloalkyl-dione derivatives and methods of their use

Номер: US20160031805A1
Принадлежит: University of Pennsylvania Penn

The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R 1 is H or C 1-6 alkyl and R 2 is H, C 1-6 alkyl, C 1-6 alkaryl, aryl, or heteroaryl; and X is O or NH. Tautomers, enantiomers, and diastereomers, as well as pharmaceutically acceptable salt forms, of compounds of formula I are also within the scope of the invention. Methods of preparing and using the compounds of formula I are also described. wherein A is

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04-02-2016 дата публикации

GUANIDINOBENZOIC ACID ESTER COMPOUND

Номер: US20160031847A1
Принадлежит: Astellas Pharma Inc.

[Problem]To provide a compound which is useful as an agent for preventing and/or treating kidney diseases. 2. The compound or a salt thereof according to claim 1 , wherein{'sup': '1', 'sub': '1-3', 'Lis a bond or Calkylene,'}{'sup': '2', 'Lis lower alkylene optionally substituted with a substituent D1, and'}{'sup': 1', '1', '2, 'sub': 2', '2', '2, 'Ris H or lower alkyl optionally substituted with at least one substituent selected from the group consisting of (i) aryl optionally substituted with a substituent D2, (ii) an aromatic heterocyclic group optionally substituted with a substituent D2, and (iii) —COH, or Rwith the nitrogen atom bonded thereto and the HOC-Lgroup on the nitrogen atom form 1,2,3,4-tetrahydroisoquinolin-2-yl substituted with at least one —COH group,'} halogen,', '—OH,', '—O-lower alkyl,', '—SH,', '—S-lower alkyl,', '—S(O)-lower alkyl,', {'sub': '2', '—S(O)-lower alkyl,'}, '—CN,', {'sub': '2', '—NO,'}, {'sub': '2', '—NH,'}, '—NH-(lower alkyl),', {'sub': '2', '—N(lower alkyl),'}, '—C(O)-lower alkyl,', {'sub': 2', '2', '2, 'aryl substituted with at least one substituent selected from the group consisting of —O-(lower alkyl optionally substituted with at least one —COH group), halogen, —COH, and lower alkyl which is optionally substituted with at least one substituent selected from the group consisting of halogen and —COH,'}, '—C(O)—O-lower alkyl,', {'sub': '2', '—COH, or'}, 'a biological equivalent thereof,, 'the substituent D1 is'}and halogen,', '—OH,', '—O-lower alkyl,', '—SH,', '—S-lower alkyl,', '—S(O)-lower alkyl,', {'sub': '2', '—S(O)-lower alkyl,'}, '—CN,', {'sub': '2', '—NO,'}, {'sub': '2', '—NH,'}, '—NH-(lower alkyl),', {'sub': '2', '—N(lower alkyl),'}, '—C(O)-lower alkyl,', {'sub': '2', '—C(O)—NH,'}, '—C(O)—NH-(lower alkyl),', {'sub': '2', '—C(O)—N(lower alkyl),'}, '—C(O)—O-lower alkyl,', {'sub': '2', '—COH, or'}, 'a biological equivalent thereof,', {'sub': 2', '2', '2', '2', '2', '2, 'lower alkyl optionally substituted with halogen, —OH, ...

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11-02-2016 дата публикации

LIQUID CRYSTAL COMPOUND HAVING BUTENE-BONDING GROUP, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20160040067A1
Автор: KOBAYASHI Masahide
Принадлежит:

To provide a liquid crystal compound satisfying at least one of high stability to heat, light and so forth, a high clearing point, low minimum temperature of a liquid-crystal phase, small viscosity, suitable optical anisotropy, large dielectric anisotropy, a suitable elastic constant and excellent compatibility with other liquid-crystal compounds, a liquid crystal composition containing the compound and a liquid crystal display device including the composition. 5. Use of at least one of the compounds according to any one of to as a component of a liquid crystal composition.6. A liquid crystal composition , containing at least one of the compounds according to any one of to .11. The liquid crystal composition according to claim 6 , further containing at least one optically active compound and/or at least one polymerizable compound.12. The liquid crystal composition according to claim 6 , further containing at least one antioxidant and/or at least one ultraviolet light absorbent.13. A liquid crystal display device claim 6 , including the liquid crystal composition according to . The invention relates to a liquid crystal compound, a liquid crystal composition and a liquid crystal display device. More specifically, the invention relates to a 2,3-difluorobenzene derivative having a butene-bonding group, a liquid crystal composition that contains the compound and has a nematic phase, and a liquid crystal display device including the composition.A liquid crystal display device has been widely used for a display of a personal computer, a television or the like. The device utilizes optical anisotropy, dielectric anisotropy and so forth of a liquid crystal compound. As an operating mode of the liquid crystal display device, such a mode is known as a phase change (PC) mode, a twisted nematic (TN) mode, a super twisted nematic (STN) mode, a bistable twisted nematic (BTN) mode, an electrically controlled birefringence (ECB) mode, an optically compensated bend (OCB) mode, an in- ...

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18-02-2016 дата публикации

Synthetic building blocks for the production of materials for organic electroluminescence devices

Номер: US20160046563A1
Принадлежит: Merck Patent GmBH

The present invention relates to compounds which are suitable as synthesis precursors for the production of electronically active materials for use in organic electroluminescence devices.

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25-02-2016 дата публикации

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

Номер: US20160056383A1
Принадлежит:

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

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02-03-2017 дата публикации

SYSTEM AND METHOD FOR HYDROGENATING AROMATIC COMPOUND

Номер: US20170057890A1
Принадлежит:

In a system for hydrogenation of an aromatic compound, an excessive temperature rise in the hydrogenation reaction unit is prevented, and the amount of the dilution gas to be circulated is minimized. The hydrogenation system () comprises a hydrogenation reaction unit () for producing a hydrogenated aromatic compound by adding hydrogen to an aromatic compound via a hydrogenation reaction, a separation unit () for separating the hydrogenated aromatic compound from a product of the hydrogenation reaction unit, and a transportation unit () for circulating at least a part of a residual component remaining in the separation unit after separating the hydrogenated aromatic compound therefrom to the hydrogenation reaction unit. The hydrogen supplied to the hydrogenation reaction unit consists of diluted hydrogen (L) diluted by a dilution compound having a higher molar specific heat than nitrogen, and the dilution compound includes a component circulated to the hydrogenation reaction unit as the residual component. 1. A system for hydrogenating an aromatic compound , comprising:a hydrogenation reaction unit for producing a hydrogenated aromatic compound by adding hydrogen to an aromatic compound via a hydrogenation reaction;a separation unit for separating the hydrogenated aromatic compound from a product of the hydrogenation reaction unit; anda transportation unit for circulating at least a part of a residual component remaining in the separation unit after separating the hydrogenated aromatic compound therefrom to the hydrogenation reaction unit;wherein the hydrogen supplied to the hydrogenation reaction unit consists of diluted hydrogen diluted by a dilution compound having a higher molar specific heat than nitrogen, and the dilution compound includes a component circulated to the hydrogenation reaction unit as the residual component.2. The system for hydrogenating an aromatic compound according to claim 1 , wherein the dilution compound in the diluted hydrogen is in a ...

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10-03-2016 дата публикации

FULVIC ACID AND DERIVATIVES AND METHODS OF PREPARATION AND USE

Номер: US20160066603A1
Принадлежит:

Disclosed are antioxidative, natural compounds, their salts, chelates and cleavage derivatives that exhibit a superior combination of properties. The compounds can be used for a variety of purposes, including stabilizing foods, cosmetics, beverages and nutritional supplements. The compounds can be prepared by hydrolyzing a fulvic acid of formula I or VIII to provide at least one antioxidant compounds of formula II, formula III, formula IV, formula V, formula VI, formula VII, salts, or chelates thereof. 2. The antioxidant compound of claim 1 , wherein at least one compound is formula II-VII claim 1 , a salt claim 1 , or chelate thereof.3. The antioxidant compound of claim 1 , wherein the compound is formula II claim 1 , a salt claim 1 , or chelate thereof.4. The antioxidant compound of claim 1 , wherein the compound is formula III claim 1 , a salt claim 1 , or chelate thereof.5. The antioxidant compound of claim 1 , wherein the compound is formula IV claim 1 , a salt claim 1 , or chelate thereof.6. The antioxidant compound of claim 1 , wherein the compound is formula V claim 1 , a salt claim 1 , or chelate thereof.7. The antioxidant compound of claim 1 , wherein the compound is formula VI claim 1 , a salt claim 1 , or chelate thereof.8. The antioxidant compound of claim 1 , wherein the compound is formula VII claim 1 , a salt claim 1 , or chelate thereof.9. The antioxidant compound of claim 1 , wherein the compound is formula VIII claim 1 , a salt claim 1 , or chelate thereof.10. The antioxidant compound of claim 1 , wherein the salt is selected from the group consisting of a lithium salt claim 1 , a sodium salt claim 1 , an ammonium salt claim 1 , a potassium salt claim 1 , a calcium salt claim 1 , a barium salt claim 1 , a magnesium salt claim 1 , a manganese salt claim 1 , a zinc salt claim 1 , an aluminum salt claim 1 , and an iron salt.11. The antioxidant compound of claim 1 , wherein the salt comprises sodium salt claim 1 , potassium salt claim 1 , calcium salt ...

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17-03-2016 дата публикации

ARYLALKYLAMINE COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS

Номер: US20160075655A1
Принадлежит:

The present invention provides arylalkylamine compounds as calcium sensing receptor modulators (CaSR). In particular, the compounds described herein are useful for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of calcium sensing receptors (CaSR). The invention also provides herein the pharmaceutical compositions thereof, and methods for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of CaSR. The invention also relates to process for the preparation of the compounds of the invention. (Formula I) 6. The compound of wherein Ris substituted or unsubstituted phenyl or substituted or unsubstituted naphthyl; wherein the substituents are selected from halogen claim 1 , hydroxy claim 1 , substituted or unsubstituted alkyl claim 1 , substituted or unsubstituted haloalkyl claim 1 , and substituted or unsubstituted alkoxy.7. The compound of claim 1 , wherein X is bond claim 1 , —(CRR)— claim 1 , —O— claim 1 , —O(CRR) claim 1 , —C(O)NR— claim 1 , —C(O)NR(CRR) claim 1 , —(CRR)cycloalkylene- claim 1 , cycloalkylene claim 1 , cycloalkylene-(CRR) claim 1 , and —O-cycloalkylene; wherein Rand Rare independently a hydrogen or substituted or unsubstituted alkyl; Ris a hydrogen or substituted or unsubstituted alkyl; and ‘r’ is 1 or 2.8. The compound of claim 1 , wherein Z is —ORwhere Ris hydrogen or substituted or unsubstituted alkyl.10. The compound of claim 1 , which is selected from:3-(3-((((R)-1-(Naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)benzoic acid hydrochloride,2-Fluoro-5-(3-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydro naphthalen-1-yl)benzoic acid hydrochloride,2-Methyl-5-(3-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydro naphthalen-1-yl)benzoic acid hydrochloride,3-Methyl-5-(3-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydro ...

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16-03-2017 дата публикации

GUANIDINE COMPOUNDS AND USE THEREOF

Номер: US20170073331A1
Принадлежит: IMMUNOMET THERAPEUTICS INC.

The present invention relates to guanidine compounds for inhibiting mitochondrial oxidative phosphorylation (OXPHOS) and use thereof. More specifically, the present invention relates to a pharmaceutical composition for preventing or treating a OXPHOS-related disease, particularly cancer, by inhibiting mitochondrial oxidative phosphorylation and reprogramming cellular metabolism. 120-. (canceled)23. The compound of claim 22 , wherein each of R claim 22 , Rand Ris hydrogen in chemical formula 2.25. The compound of claim 24 , wherein each of R claim 24 , Rand Ris hydrogen in chemical formula 3.27. The compound of claim 25 , wherein each of R claim 25 , Rand Ris hydrogen in chemical formula 4.29. The compound of claim 28 , wherein each of R claim 28 , Rand Ris hydrogen in chemical formula 5.30. The compound of claim 21 , wherein each of Rand Ris hydrogen in chemical formula 6.31. A compound selected from the group consisting of the following compounds claim 21 , and pharmaceutically acceptable salts claim 21 , pharmaceutically acceptable solvates claim 21 , prodrug forms of claim 21 , and derivatives of claim 21 , such compounds:N-1-(3,4-dichloro)phenethylbiguanide,N-1-(2,5-dichloro)phenethylbiguanide,N-1-(2-chloro)phenethylbiguanide,N-1-(2,4-dichloro)phenethylbiguanide,N-1-(3-fluoro)phenethylbiguanide,N-1-(4-trifluoromethoxy)phenethylbiguanide,N-1-(4-trifluoromethyl)phenethylbiguanide,N-1-(3-methoxy)phenethylbiguanide,N-1-(2-fluoro)phenethylbiguanide,N-1-(4-methyl)phenethylbiguanide,N-1-(4-methanesulphoneamine)phenethylbiguanide,N-1-(4-(N,N-dimethyl)phenethylbiguanide,N-1-(4-phenoxy)phenethylbiguanide,N-1-(4-isopropyl)phenethylbiguanide,N-1-(3,4-dimethyl)phenethylbiguanide,N-1-(2,4-dimethyl)phenethylbiguanide,N-1-(4-fluoro-2-methyl)phenethylbiguanide,N-1-(2,4-dimethyl)benzylbiguanide,N-1-(4-fluoro-3-methoxy)phenethylbiguanide,N-1-(3,4-difluoro)phenethylbiguanide,N-1-(2-morpholinoethyl)biguanide,N-1-(2-methyl)phenethylbiguanide,N-1-(3-bromo-4-fluoro)benzylbiguanide,N-1 ...

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23-03-2017 дата публикации

Serotonin Receptor-Targeting Compounds and Methods

Номер: US20170081273A1
Автор: Booth Raymond G.
Принадлежит:

This invention relates to, in part, compositions and methods that are useful for, inter alia, the treatment of various diseases, including those linked to binding at a serotonin receptor. The compositions include chiral tetrahydronaphthalen-2-amine derivatives. Accordingly, the present invention provides for compositions and methods that agonize or antagonize one or more serotonin receptors and which find Use in the treatment of various neuropsychiatric diseases or disorders including, without limitation, autism spectrum disorder (ASD) or associated symptoms. 2. The pharmaceutical composition of claim 1 , wherein:{'sup': 1', '2', '1', '2, 'each of Rand Ris independently hydrogen or alkyl, or Rand Rcome together to form an optionally substituted heterocyclic ring;'}{'sup': 3', '4', '5', '6', '7', '8', '9', '10, 'each of R, R, R, R, R, R, R, and Ris independently hydrogen, hydroxy, acyl, acyloxy, alkyl, heteroalkyl, alkenyl, heteroalkenyl, alkynyl, heteroalkynyl, alkoxycarbonyl, cyano, trifluoromethyl, trifluoromethoxy, nitro, amino, and amido, and wherein any two adjacent R groups may optionally come together to form a carbocyclic or heterocyclic ring system;'}and a pharmaceutically acceptable excipient or carrier.3. The pharmaceutical composition of claim 1 , wherein the composition comprises at least about 70% claim 1 , or at least about 80% claim 1 , or at least about 85% claim 1 , or at least about 90% claim 1 , or at least about 95% claim 1 , or at least about 97% claim 1 , or at least about 99% of a single enantiomer.4. The pharmaceutical composition of any of the above claims claim 1 , wherein the dual partial agonist binds to serotonin 5-HTreceptor and/or the 5-HTreceptor with a binding affinity (K) of less than about 100 nM claim 1 , or less than about 50 nM claim 1 , or less than about 25 nM claim 1 , or less than about 20 nM claim 1 , or less than about 10 nM claim 1 , or less than about 5 nM claim 1 , or less than about 2 nM claim 1 , or less than about 1 ...

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27-04-2017 дата публикации

18-20 MEMBER BI-POLYCYCLIC COMPOUNDS

Номер: US20170114019A1
Принадлежит:

The invention relates to 18-20 member bi-polycyclic compounds, methods of making these compounds, and methods of using them in treating hyperproliferative disorders (e.g., cancer) and non-malignant tumors; promoting muscle formation; inhibiting muscle degeneration or the loss of muscle mass or muscle function; and myofibers ex vivo. 2. The compound of claim 1 , wherein W is an indolinylene linked to A at any one of positions 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 or 7 of the indolinylene; a quinolinene linked to A at any one of positions 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , or 8; or an isoquinolinene linked to A at any one of positions 1 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 claim 1 , or 8.3. The compound of claim 1 , wherein W is -propylene-phenylene-.4. The compound of claim 1 , wherein Z is —C(O)NRRor —C(O)OR claim 1 , wherein Rand Rare each independently hydrogen (H) claim 1 , hydroxyl (OH) claim 1 , Calkyl claim 1 , hydroxyCalkyl claim 1 , aminoCalkyl claim 1 , or aminoaryl; and Ris H or Calkyl.5. The compound of claim 2 , wherein Z is linked to the indolinylene claim 2 , quinolinene claim 2 , or isoquinolinene at any one of the positions that is not linked to A.7. The compound of claim 1 , wherein W is an indolinylene linked to A at any one of positions 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 or 7 of the indolinylene; Z is —C(O)NRRor —C(O)OR claim 1 , wherein Rand Rare each independently hydrogen claim 1 , hydroxyl claim 1 , Calkyl claim 1 , hydroxyCalkyl claim 1 , aminoCalkyl claim 1 , or aminoaryl; and Ris H or Calkyl claim 1 , and wherein Z is linked to the indolinylene at any one of positions 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 or 7 of the indolinylene not linked to A.8. The compound of claim 1 , wherein W is a quinolinene linked to A at any one of positions 2 claim 1 , 3 claim 1 , 4 claim 1 , 5 claim 1 , 6 claim 1 , 7 or 8 of the quinolinene; Z is —C(O)NRRor —C(O) ...

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18-05-2017 дата публикации

ARYLALKYLAMINE COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS

Номер: US20170137371A1
Принадлежит:

The present invention provides arylalkylamine compounds as calcium sensing receptor modulators (CaSR). In particular, the compounds described herein are useful for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of calcium sensing receptors (CaSR). The invention also provides herein the pharmaceutical compositions thereof, and methods for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of CaSR. The invention also relates to process for the preparation of the compounds of the invention. (Formula I) 6. The compound of wherein Ris substituted or unsubstituted phenyl or substituted or unsubstituted naphthyl; wherein the substituents are selected from halogen claim 1 , hydroxy claim 1 , substituted or unsubstituted alkyl claim 1 , substituted or unsubstituted haloalkyl claim 1 , and substituted or unsubstituted alkoxy.7. The compound of claim 1 , wherein X is bond claim 1 , —(CRR)— claim 1 , —O— claim 1 , —O(CRR)— claim 1 , —C(O)NR— claim 1 , —C(O)NR(CRR)— claim 1 , —(CRR)cycloalkylene- claim 1 , cycloalkylene claim 1 , cycloalkylene-(CRR)— claim 1 , and —O-cycloalkylene; wherein Rand Rare independently a hydrogen or substituted or unsubstituted alkyl; Ris a hydrogen or substituted or unsubstituted alkyl; and ‘r’ is 1 or 2.8. The compound of claim 1 , wherein Z is —ORwhere Ris hydrogen or substituted or unsubstituted alkyl.10. The compound of claim 1 , which is selected from:3-(3-((((R)-1-(Naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydronaphthalen-1-yl)benzoic acid hydrochloride,2-Fluoro-5-(3-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydro naphthalen-1-yl)benzoic acid hydrochloride,2-Methyl-5-(3-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydro naphthalen-1-yl)benzoic acid hydrochloride,3-Methyl-5-(3-((((R)-1-(naphthalen-1-yl)ethyl)amino)methyl)-1,2,3,4-tetrahydro ...

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26-05-2016 дата публикации

Quinone based nitric oxide donating compounds for ophthalmic use

Номер: US20160145192A1
Принадлежит: Nicox Science Ireland Ltd

The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment and/or prophylaxis of glaucoma and ocular hypertension.

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25-05-2017 дата публикации

Unique dual-action therapeutics

Номер: US20170143836A1
Принадлежит: Rutgers State University of New Jersey

A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; X═C, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.

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02-06-2016 дата публикации

NOVEL INTERMEDIATE FOR SYNTHESIZING TREPROSTINIL DIETHANOLAMINE AND METHOD FOR PREPARING THE SAME

Номер: US20160152548A1
Принадлежит:

The present invention relates to a method for treprostinil diethanolamine synthesis. The present invention also relates to a novel intermediate used in the method for treprostinil diethanolamine synthesis. The novel intermediate is shown in the following formula (II): 2. The compound as claimed in claim 1 , wherein R1 is a methyl group.3. The compound as claimed in claim 1 , wherein R2 is a methyl group.6. The method as claimed in claim 5 , wherein R2 is a methyl group.8. The method as claimed in claim 7 , wherein R2 is a methyl group.9. The method as claimed in claim 7 , wherein in step (A) claim 7 , the hydroxyl-protecting group is selected from the group consisting of methyl group claim 7 , ethyl group claim 7 , tert-butyl group claim 7 , acetyl group claim 7 , pivaloyl group (Piv) claim 7 , benzyl group (Bn) claim 7 , p-methoxy benzyl group (PMB) claim 7 , 9-fluorenylmethyl group (Fm) claim 7 , diphenylmethyl group (DPM) claim 7 , trimethylsilyl group (TMS) claim 7 , tert-butyldimethylsilyl group (TBS) claim 7 , triisopropylsilyl group (TIPS) claim 7 , 2-methoxylethoxymethyl group (MEM) claim 7 , methylthiomethy group (MTM) claim 7 , methoxymethyl group (MOM) claim 7 , and tetrahydropyranyl group (THP).10. The method as claimed in claim 7 , wherein in step (H) claim 7 , R4 is a methyl group.12. The compound as claimed in claim 11 , wherein R2 is a methyl group. This application claims the benefits of the Taiwan Patent Application Serial Number 103141569, filed on Dec. 1, 2014, the subject matter of which is incorporated herein by reference.1. Field of the InventionThe present invention relates to a method for treprostinil diethanolamine preparation. In addition, the present invention also relates to a novel intermediate for treprostinil diethanolamine preparation.2. Description of Related ArtTreprostinil and derivatives thereof are beneficial for vasodilation stimulation, platelet aggregation and thrombus formation inhibition, thrombolysis stimulation, cell ...

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18-06-2015 дата публикации

METHOD FOR PRODUCING RUTHENIUM CATALYST AND METHOD FOR PRODUCING ALKYL GROUP- OR ALKENYL GROUP-SUBSTITUTED COMPOUND USING RUTHENIUM CATALYST

Номер: US20150165433A1
Принадлежит:

This invention relates to a method for producing a ruthenium catalyst in which ruthenium supported on at least one metal oxide is pretreated with an aldehyde compound, a phosphorus compound, and a lower alcohol compound, and a method for producing alkyl- or alkenyl-substituted compound using the ruthenium catalyst. 2. The method for producing a ruthenium catalyst according to claim 1 , wherein the aldehyde compound is at least one member selected from the group consisting of formaldehyde claim 1 , 1 claim 1 ,3 claim 1 ,5-trioxane claim 1 , paraformaldehyde claim 1 , glyoxal claim 1 , methylglyoxal claim 1 , malonaldehyde claim 1 , acetaldehyde claim 1 , and propionaldehyde.3. The method for producing a ruthenium catalyst according to claim 1 , wherein the aldehyde compound is formaldehyde.4. The method for producing a ruthenium catalyst according to claim 1 , wherein the phosphorus compound is at least one member selected from the group consisting of phosphines claim 1 , phosphites claim 1 , and phosphine oxides.5. The method for producing a ruthenium catalyst according to claim 1 , wherein the phosphorus compound is triphenylphosphine.6. The method for producing a ruthenium catalyst according to claim 1 , wherein the lower alcohol compound is at least one member selected from the group consisting of lower alcohols claim 1 , lower alkylene glycols claim 1 , and lower alkoxy-lower alcohols.7. The method for producing a ruthenium catalyst according to claim 1 , wherein the lower alcohol compound is 2-methoxyethanol.8. The method for producing a ruthenium catalyst according to claim 1 , wherein the heating temperature is 40 to 200° C. The present invention relates to a method for producing a ruthenium catalyst supported on at least one metal oxide, and a method for producing an alkyl- or alkenyl-substituted compound using a heterogeneous catalyst that is a ruthenium catalyst supported on at least one metal oxide.A method for producing an alkyl- or alkenyl-substituted ...

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16-06-2016 дата публикации

Oxone-Aceton Mediated Metal Free Preparation of Syn-Diols

Номер: US20160168114A1
Принадлежит:

The present invention disclose a simple and high yielding process of Oxone-acetone mediated metal free syn-dihydroxylation of benzo fused olefins of formula (II) to obtain library of dioxolo compounds of formula (I). The invention further disclose a simple and high yielding process of Oxone-acetone mediated metal free syn-dihydroxylation of stilbene and its derivatives of formula (III) thereof. Also disclosed herein is Wacker-type oxidation of benzo-fused olefins of formula (X). The invention further disclose compounds of formula (I) which can be useful for the treatment of HIV, cancer or malaria. 2. The process as claimed in claim 1 , wherein the mixture of acetone claim 1 , ethyl acetate claim 1 , and water is in the ratio of 5:1:1.4. The process as claimed in claim 1 , wherein the compound of Formula I is selected from the group consisting of:(i) 2,2-dimethyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2a);(ii) 2,2-dimethyl-3a-propyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2b);(iii) 3a-(3-chloropropyl)-2,2-dimethyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2c);(iv) 8-(4-bromobutyl)-2,2-dimethyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2d);(v) 8-benzyl-2,2-dimethyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2e);(vi) 3a-benzyl-2,2-dimethyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2f);(vii) 3a-isopropyl-2,2-dimethyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2g);(viii) 3a-cyclohexyl-2,2-dimethyl-8,8a-dihydro-3aH-indeno[2,1-d][1,3]dioxole (2h);(ix) 2,2-dimethyl-3a-phenyl-8,8a-dihydro-3aH-indeno[1,2-d][1,3]dioxole (2i);(x) 7-(2,2-dimethyl-8,8a-dihydro-3aH-indeno[2,1-d][1,3]dioxol-3a-yl)heptan-2-one (2j);(xi) 2′,2′-dimethyl-3a′,8a′-dihydrospiro[cyclopentane-1,8′-indeno[2,1-d][1,3]dioxole](2k);(xii) 3a-(but-3-enyl)-2,2-dimethyl-8,8a-dihydro-3aH-indeno[2,1-d][1,3]dioxole (2m);(xiii) 2,2,9b-Trimethyl-3a,4,5,9b-tetrahydronaphtho[2,1-d][1,3]dioxole (2o);(xiv) 7-Methoxy-2,2,9b-trimethyl-3a,4,5,9b-tetrahydronaphtho[1,2-d][1,3]dioxole (2p);(xv) 2,2-Dimethyl-9b- ...

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16-06-2016 дата публикации

MONOMER, LIQUID CRYSTAL COMPOSITION, LIQUID CRYSTAL DISPLAY DEVICE, AND PRODUCTION METHOD FOR LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20160168465A1
Принадлежит:

An aspect of the present invention provides a monomer from which a polymer layer capable of keeping high display quality even in high temperature and high humidity environments can be formed. The monomer in an aspect of the present invention is a compound represented by P-Sp-Z-A-(Z-A)-Z-Sp-P: in the formula, P denotes the same or different radical polymerizable group; and at least one of Z, Z, and Zdenotes —NRCO— or —CONR— group. 3. A liquid crystal composition comprising: the monomer according to ; and a liquid crystal material.4. The liquid crystal composition according to further comprising a monomer having a structure for producing a radical by hydrogen abstraction reaction by light irradiation or a structure for producing a radical by self-cleavage reaction by light irradiation.9. The liquid crystal display device according to claim 7 , wherein the monomer further comprises a monomer having a structure for forming a radical by hydrogen abstraction reaction by light irradiation or a structure for producing a radical by self-cleavage reaction by light irradiation.14. The production method for a liquid crystal display device according to or claim 7 , wherein the liquid crystal composition further comprises a monomer having a structure for producing a radical by hydrogen abstraction reaction by light irradiation or a structure for producing a radical by self-cleavage reaction by light irradiation. An aspect of the present invention relates to a liquid crystal composition, a liquid crystal display device, and a production method for a liquid crystal display device. More particularly, an aspect of the present invention relates to a liquid crystal composition for forming a polymer layer by which orientation of liquid crystal molecules can be controlled, a liquid crystal display device having a polymer layer which can control orientation of liquid crystal molecules and which is formed by polymerizing a monomer contained in a liquid crystal composition (hereinafter, ...

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22-06-2017 дата публикации

Fused (hetero)cyclic compounds as s1p modulators

Номер: US20170174672A1
Принадлежит: AbbVie Deutschland GmbH and Co KG

The invention relates to (hetero)cyclic compounds as S1P modulators, pharmaceutical compositions comprising such compounds, and uses thereof in the treatment, alleviation or prevention of diseases or disorders mediated by an S1P receptor.

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22-06-2017 дата публикации

Compounds that are s1p modulating agents and/or atx modulating agents

Номер: US20170174710A1
Принадлежит: Biogen MA Inc

Compounds of formula (I) can modulate the activity of one or more S1P receptors and/or the activity of autotaxin (ATX).

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14-07-2016 дата публикации

NOVEL AND SPECIFIC INHIBITORS OF CYTOCHROME P450 26 RETINOIC ACID HYDROXYLASE

Номер: US20160200703A1
Принадлежит: UNIVERSITY OF MONTANA

The present disclosure is generally directed to compositions and methods for treating diseases that are ameliorated by the inhibition of CYP26 mediated retinoic acid metabolism. The compositions comprise compounds of formula (I). A repreid50000060307390 IB/345 nullsents aryl optionally substituted with one, two, three, or four groups that are each independently halogen, cyano, nitro, Calkyl, Chaloalkyl, —NH, —NH(C-Calkyl), —N(C-Calkyl), —OH, C-Calkoxy, and C-Chaloalkoxy; X is a bond, —CH—, —CHR—, —C═CHR—, —NR—, —N═O—R—, —O—, —S—, —SO—, —SO—, —C(O)—, or —C(NR)—, or X is of formula (a), (b) or (c), wherein each n is independently 1, 2, or 3; each Ris independently hydrogen or Calkyl; Ris independently hydrogen, Calkyl, or —OR, where Ris selected from the group consisting of hydrogen, Calkyl, Calkenyl, CalkynyL Ccycloalkyl, heterocyclyl, aryl, arylCalkyl, heteroaryl, or heteroarylCalkyl; Y is Calkylene, Calkenylene, or Calkylylene moiety.

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23-07-2015 дата публикации

Compounds that are s1p modulating agents and/or atx modulating agents

Номер: US20150203515A1
Принадлежит: Biogen MA Inc

Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

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20-07-2017 дата публикации

CHIRAL DIAMINE COMPOUNDS FOR THE PREPARATION OF CHIRAL ALCOHOLS AND CHIRAL AMINES

Номер: US20170204036A1
Принадлежит:

A process for the stereoselective preparation of a chiral alcohol or a chiral amine, the process comprising reacting a first prochiral reactant selected from the group consisting of a ketone, an aldehyde, and an imine, with a second reactant comprising a Grignard reagent, in the presence of a chiral trans-diamine of formula (1) as defined herein: 2. The process according to claim 1 , wherein the ketone claim 1 , aldehyde or imine is formed in-situ.3. The process according to claim 1 , wherein Ra and Rb together define a C-Ccycloalkyl group.4. The process according to claim 3 , wherein the cycloalkyl group is cyclohexane or cyclopentane.5. The process according to claim 1 , wherein Ra and Rb are each independently an alkyl or an aryl group.6. The process according to claim 5 , wherein Ra and Rb are each independently phenyl claim 5 , methyl or tert-butyl.7. The process according to claim 1 , wherein Rc is a Calkyl group.8. The process according to claim 1 , wherein Rd is a Calkyl group.9. The process according to claim 1 , wherein Rd and Re together define an imidazolidine ring with the two N atoms.10. The process according to claim 1 , wherein Re is a Calkyl group.11. The process according to claim 1 , wherein n is 1.12. The process according to claim 1 , wherein Rf is an alkyl or aryl group.13. The process according to claim 12 , wherein Rf is a tert-butyl group.14. The process according to claim 12 , wherein Rf is an aryl group which is substituted by at least one substituent selected from hydroxy claim 12 , alkoxy claim 12 , amino claim 12 , aminoalkyl claim 12 , thiol claim 12 , halo claim 12 , haloalkyl claim 12 , haloalkoxy claim 12 , alkyl claim 12 , cycloalkyl claim 12 , alkenyl claim 12 , cycloalkenyl claim 12 , alkynyl claim 12 , aryl claim 12 , heterocyclyl claim 12 , cyano claim 12 , nitro claim 12 , silyl claim 12 , sulfanyl claim 12 , phosphanyl and CF.16. The process according to claim 15 , wherein Rii and Riv are both hydrogen.17. The process ...

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03-09-2015 дата публикации

Method for producing diisocyanates by phosgenating diamine suspensions

Номер: US20150246873A1
Принадлежит: BAYER MATERIALSCIENCE AG

The invention relates to a method for producing organic diisocyanates by reacting the corresponding diamines with phosgene in inert solvents. High-melting diamines from the series of 1,5-naphthalenediamine, tetralindiamine, 1,4-phenylenediamine, durenediamine, and o-tolidinediamine are used as diamines. According to the invention, a suspension of the diamines in inert solvents is produced, wherein dynamic mixing units, selected from dispersion disks and rotor-stator systems, are used, and the obtained suspension is phosgenated.

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10-09-2015 дата публикации

Use of a Compound for Inducing Differentiation of Mesenchymal Stem Cells into Cartilage Cells

Номер: US20150252003A1

Use of a compound of Formula 1 for inducing differentiation of mesenchymal stem cells to chondrocytes, and a pharmaceutical composition for treating a cartilage disease, which includes chondrocytes in which differentiation from mesenchymal stem cells is induced by the compound of Formula 1, are provided. Differentiation of the mesenchymal stem cells treated with the compound of Formula 1 to chondrocytes is specifically induced, and thus the compound can be used to effectively treat a cartilage disease such as arthritis, cartilage damage, and a cartilage defect.

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01-09-2016 дата публикации

BICYCLIC COMPOUNDS

Номер: US20160251309A1
Принадлежит:

Disclosed are compounds of Formula (I) 112-. (canceled) This application is a continuation of U.S. application Ser. No. 14/798,498, filed Jul. 14, 2015, which claims priority to U.S. application Ser. No. 14/185,164, filed Feb. 20, 2014, which claims priority to U.S. Provisional Application No. 61/767,531 filed on Feb. 21, 2013, whose contents are hereby incorporated by reference.The present invention generally relates to bicyclic compounds useful as S1Pagonists. Provided herein are bicyclic compounds, compositions comprising such compounds, and methods of their use. The invention further pertains to pharmaceutical compositions comprising at least one compound according to the invention that are useful for the treatment of conditions related to S1Pmodulation, such as autoimmune diseases and vascular disease.Sphingosine-1-phosphate (S1P) is a zwitterionic lysophospholipid metabolite of sphingosine (Sph), which in turn is derived from enzymatic cleavage of ceramides. Enzymatic phosphorylation of Sph by two kinases (SphK1 and SphK2) leads to the production of S1P largely from erythrocytes, but also from a radiation resistant source, possibly the lymphatic endothelium (Pappu, R. et al., 316:295-298 (2007)). Originally thought to operate solely as an intracellular signaling molecule, S1P was subsequently identified as a high affinity ligand for five members of the endothelial differentiation gene (EDG) class of G-protein coupled receptors (GPCRs) named S1Por S1P1, S1Por S1P2, S1Por S1P3, S1Por S1P4, and S1Por S1P5 (formerly called EDG-1, EDG-5, EDG-3, EDG-6, and EDG-8, respectively) (Chun, J. et al., 62:579-587 (2010)). The interaction of S1P with the S1P receptors plays a fundamental physiological role in a large number of processes including cell proliferation, cell morphology, tumor cell invasion, angiogenesis, tumorigenesis, cytoskeletal rearrangement, vascular development, and lymphocyte trafficking (Olivera, A. et al., 716:123-142 (2011)). S1P receptors are ...

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20-11-2014 дата публикации

THERAPEUTIC COMPOUNDS

Номер: US20140343079A1
Принадлежит:

The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease. 4. The compound of wherein ring A is a phenyl ring substituted with one or more groups independently selected from halo claim 1 , cyano claim 1 , nitro claim 1 , (C-C)alkyl claim 1 , (C-C)cycloalkyl claim 1 , (C-C)alkenyl claim 1 , (C-C)alkynyl claim 1 , (C-C)alkoxy claim 1 , (C-C)alkoxycarbonyl claim 1 , or (C-C)alkanoyloxy claim 1 , wherein each (C-C)alkyl claim 1 , (C-C)cycloalkyl claim 1 , (C-C)alkenyl claim 1 , (C-C)alkynyl claim 1 , (C-C)alkoxy claim 1 , (C-C)alkoxycarbonyl claim 1 , and (C-C)alkanoyloxy claim 1 , is optionally substituted with one or more groups independently selected from halo claim 1 , hydroxy claim 1 , nitro claim 1 , cyano claim 1 , and oxo (═O).5. The compound of wherein ring A is a 6-membered heteroaryl ring claim 1 , which is optionally substituted with one or more groups independently selected from halo claim 1 , hydroxy claim 1 , cyano claim 1 , nitro claim 1 , (C-C)alkyl claim 1 , (C-C)cycloalkyl claim 1 , (C-C)alkenyl claim 1 , (C-C)alkynyl claim 1 , (C-C)alkoxy claim 1 , (C-C)alkoxycarbonyl claim 1 , or (C-C)alkanoyloxy claim 1 , wherein each (C-C)alkyl claim 1 , (C-C)cycloalkyl claim 1 , (C-C)alkenyl claim 1 , (C-C)alkynyl claim 1 , (C-C)alkoxy claim 1 , (C-C)alkoxycarbonyl claim 1 , and (C-C)alkanoyloxy claim 1 , is optionally substituted with one or more groups independently selected from halo claim 1 , hydroxy claim 1 , nitro claim 1 , cyano claim 1 , and oxo (═O).7. The compound of wherein Ris H claim 6 , halo claim 6 , hydroxy claim 6 , cyano claim 6 , nitro claim 6 , (C-C)cycloalkyl claim 6 , (C-C)alkenyl claim 6 , (C-C)alkynyl claim 6 , (C-C)alkoxy claim 6 , (C-C)alkoxycarbonyl claim 6 , or (C-C)alkanoyloxy claim 6 , wherein each (C-C)alkyl claim 6 , (C-C)cycloalkyl claim 6 , (C-C)alkenyl claim 6 , ...

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24-09-2015 дата публикации

INTEGRATED PROCESS FOR PRODUCTION OF HIGH OCTANE GASOLINE, HIGH AROMATIC NAPHTHA AND HIGH CETANE DIESEL FROM HIGH AROMATIC MIDDLE DISTILLATE RANGE STREAMS

Номер: US20150267130A1
Принадлежит:

An integrated process for production of ultra low sulfur products of high octane gasoline, high aromatic naphtha and high Cetane Diesel from high aromatic middle distillate range streams from any cracker units such as Light Cycle Oil (LCO) stream of Fluid catalytic cracking (FCC) units and comprising of subjecting the feed boiling between 200 to 400° C. and having at least 30 wt % multi-ring aromatics content subjected to hydrotreating for removal of heteroatoms like sulfur and nitrogen and at a pressure sufficient only for saturation of one ring of multi-ring aromatics. The effluent from hydrotreating is subjected to hydrocracking at same pressure of hydrotreating step above for selective opening of saturated ring of multi-ring aromatics. The effluent from hydrocracking is separated in CUT-1 boiling between 35 to 70° C., CUT-2 boiling between 70 to 200° C. in which the monoaromatics and alkylated monoaromatics are concentrated and CUT-3 boiling above 200° C. in which concentration of saturates i.e. paraffins and naphthenes significantly increased. The CUT-3 is selectively oxidized in selective oxidation step in presence of catalyst, an oxidizing agent and operating conditions such that it results in diesel product with more enhanced Cetane. 1. An integrated process for production of High Octane Gasoline , High Aromatic Naphtha and High Cetane Diesel , the process comprising:a. subjecting a feed to hydrotreating step at a predetermined pressure to obtain a first effluent having a substantially reduced quantity of hetero-atoms compared to the feed, the feed comprising at least 30 wt % multi-ring aromatics and having boiling point between 200 to 400° C., wherein the predetermined pressure is capable to saturate one or more rings of multi-ring aromatics and to remains unsaturated one or more rings of the multi-ring aromatics;b. subjecting the first effluent to a hydrocracking step at the predetermined pressure to obtain a second effluent, the hydrocracking step ...

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01-10-2015 дата публикации

METHOD OF TREATING CANCER USING SELECTIVE ESTROGEN RECEPTOR MODULATORS

Номер: US20150274640A1
Принадлежит:

Disclosed herein are methods of treating subjects suffering from estrogen receptor positive cancer of the brain by administering a selective estrogen receptor degrader (SERM). Also disclosed are methods of treating a cancer that is resistant to an estrogen receptor modulator by administering a SERM. 1. A method of treating breast cancer brain metastasis in a subject , the method comprising administering a compound of (R)-6-{2-{ethyl[4-(2-ethylaminoethyl)benzyl]amino}-4-methoxyphenyl}-5 ,6 ,7 ,8-tetrahydronaphthalen-2-ol , wherein the breast cancer brain metastasis is resistant to an estrogen receptor modulator.2. The method of claim 1 , wherein an effective amount of the compound is administered.3. The method of claim 2 , wherein the effective amount comprises a high dosage.4. The method of claim 3 , wherein the high dosage is more than about 20 mg/kg.5. The method of claim 3 , wherein the high dosage is about 20 mg/kg to about 100 mg/kg.6. The method of claim 1 , wherein the compound is administered by oral administration claim 1 , intravenous administration claim 1 , intradermal injection claim 1 , intramuscular injection or subcutaneous injection.7. The method of claim 1 , further comprising administering an effective amount of at least one compound selected from the group consisting of a cyclin-dependent kinase 4 and 6 inhibitor (CDK4/6 inhibitor) claim 1 , an antiestrogen claim 1 , a ligand of retinoic acid or retinoxic X receptor claim 1 , an antiprogestin claim 1 , an antiandrogen claim 1 , vitamin D or metabolite thereof claim 1 , a farnesyl transferase inhibitor claim 1 , a PPARα or gamma agonist and a MAP kinase inhibitor.8. The method of claim 1 , wherein the breast cancer brain metastasis is de novo resistant to the estrogen receptor modulator.9. The method of claim 1 , wherein the resistance to the estrogen receptor modulator is acquired.10. The method of claim 1 , wherein the estrogen receptor modulator is a selective estrogen receptor modulator (SERM ...

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29-09-2016 дата публикации

Asymmetric catalytic decarboxylative alkyl alkylation using low catalyst concentrations and a robust precatalyst

Номер: US20160280623A1

This invention provides efficient and scalable enantioselective methods that yield 2-alkyl-2-allylcycloalkyanone compounds with quaternary stereogenic centers. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II) or (III): with a palladium (II) catalyst under alkylation conditions.

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29-09-2016 дата публикации

CROSS-COUPLING OF UNACTIVATED SECONDARY BORONIC ACIDS

Номер: US20160280721A1
Принадлежит:

Provided are methods for site- and stereo-retentive cross-couplings with unactivated secondary boronic acids, which methods are particularly useful in building block-based approach for small molecule synthesis. Also provided is a method of forming an air-stable chiral secondary boronic acid. 23-. (canceled)4. The method of claim 1 , wherein ligand is P(o-tol).58-. (canceled)9. The method of claim 1 , wherein the secondary boronic acid is chiral and has an enantiomeric excess of at least 80 percent.1012-. (canceled)13. The method of claim 1 , wherein the product represented by RRCH-Ar is chiral and has an enantiomeric excess of at least 80 percent.1419-. (canceled)20. The method of claim 1 , wherein X is Br.21. The method of claim 1 , wherein X is I.2324-. (canceled)25. The method of claim 22 , wherein the hydrolyzing is with aqueous hydroxide.26. (canceled)27. The method of claim 22 , wherein the chiral iminodiacetic acid has an enantiomeric excess of at least 80 percent.2829-. (canceled)30. The method of claim 22 , wherein the chiral iminodiacetic acid is benzylcyclopentyl iminodiacetic acid (BIDA).31. The method of claim 22 , wherein the weak acid catalyst is pyridinium p-toluenesulfonate (PPTS).3234-. (canceled)35. The method of claim 22 , wherein the air-stable chiral secondary boronic acid has an enantiomeric excess of at least 80 percent.3637-. (canceled)39. The method of claim 38 , further comprising combining the air-stable trihydroxyborate salt of a primary or secondary boronic acid claim 38 , a Lewis acid claim 38 , and a second polar aprotic solvent claim 38 , thereby re-forming the primary or secondary boronic acid represented by formula (I).4041-. (canceled)4348-. (canceled)5070-. (canceled)7275-. (canceled)7778-. (canceled)79. The method of claim 76 , wherein the chiral organic group has an enantiomeric excess of at least 80 percent.8081-. (canceled)82. The method of claim 76 , wherein the chiral boronic acid has an enantiomeric excess of at least 80 ...

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25-12-2014 дата публикации

Synthetic Epigallocatechin Gallate (EGCG) Analogs

Номер: US20140378541A1
Принадлежит:

Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for treating cancer and for treating metabolic disorders is also provided. 1121.-. (canceled)124. The compound of claim 123 , wherein X and Z are the same.125. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.127. The method of claim 126 , wherein said contacting occurs in vivo.128. The method of claim 127 , wherein said contacting comprises administering the at least one compound to a subject by a route selected from the group consisting of oral claim 127 , parenteral claim 127 , subcutaneous claim 127 , intravenous claim 127 , intramuscular claim 127 , intraperitoneal claim 127 , intraarterial claim 127 , transdermal claim 127 , and mucosal administration.129. A method for inhibiting tumor cell growth and/or treating cancer in a subject claim 126 , comprising administering to the subject a therapeutically effective amount of at least one compound of claim 126 , or an analog or pharmaceutically acceptable salt thereof claim 126 , such that tumor cell growth is inhibited and/or cancer is treated in the subject.130. The method claim 129 , wherein cancer stem cell population claim 129 , activity of epidermal growth factor receptor (EGFR) claim 129 , or NF-kB claim 129 , PI3K/Akt and/or mTOR signaling pathways are decreased or inhibited.131. The method of claim 129 , wherein the CD44/CD24cell population is reduced.132. The method of claim 129 , wherein the compound or composition is administered orally claim 129 , parenterally claim 129 , subcutaneously claim 129 , intravenously claim 129 , intramuscularly claim 129 , intraperitoneally claim 129 , intraarterially claim 129 , transdermally claim 129 , or through the mucosa.133. The method of claim 129 , wherein the subject is a human.134. The method of claim 129 , wherein the compound ...

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22-10-2015 дата публикации

UV CURED BENZOPHENONE TERMINATED QUARTERNARY AMMONIUM ANTIMICROBIALS FOR SURFACES

Номер: US20150299475A1
Принадлежит:

The invention relates to benzophenone-terminated quaternary ammonium compounds of formula (I), processes for preparing benzophenone-terminated quaternary ammonium compounds of formula (I), environmentally friendly antimicrobial formulations of said quaternary ammonium compounds and their use as durable antimicrobial surface coatings for surfaces. 2. The compound of wherein Rand Rare methyl.3. The compound of wherein X is bromo or iodo.4. The compound of wherein Rand Rare independently methyl claim 1 , ethyl claim 1 , n-propyl or isopropyl and Ris hydrogen.6. The compound of wherein m is 13 claim 5 , 15 or 17 except when n is 1 claim 5 , X is bromo and Rand Rare methyl.9. The process of wherein R claim 8 , and Rare methyl.10. The process of wherein X is selected from the group consisting of bromo and iodo.11. The process of wherein Rand Rare independently methyl claim 8 , ethyl claim 8 , n-propyl or isopropyl and Ris hydrogen.13. The process of wherein m is 17.15. The process of wherein the alkali metal carbonate is potassium carbonate.17. The composition of wherein Rand Rare methyl.18. The composition of wherein X is bromo or iodo.19. The composition of wherein Rand Rare independently methyl claim 16 , ethyl claim 16 , n-propyl or isopropyl and Ris hydrogen.21. The composition of wherein m is 17.23. The composition of wherein the carrier is a mixture of water and an alcohol.24. The composition of wherein the alcohol is methanol.25. A process for coating a surface with an antimicrobial coating claim 23 , said process comprising the steps of:{'claim-ref': {'@idref': 'CLM-00015', 'claim 15'}, 'i) contacting the surface with a composition of ; and'}ii) irradiating the coated surface.26. The process of wherein the surface comprises a polymer or a fibre.27. The process of further comprising iii) a washing step wherein the washing step comprises the use of a water and isopropanol mixture.28. The process of wherein the irradiating step comprises irradiating the coated ...

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13-10-2016 дата публикации

N-SUBSTITUTED BENZAMIDES AND METHODS OF USE THEREOF

Номер: US20160297754A1
Принадлежит:

The invention provides novel compounds having the general formula: 2. (canceled)4. The compound of wherein B is N and Ris absent.5. The compound of wherein B is C.6. The compound of wherein R claim 1 , Rand Rare each independently selected from H claim 1 , F claim 1 , or Cl.7. The compound of wherein Ris H claim 1 , F or Cl; Rand Rare each H; and Ris an optionally substituted group selected from the group consisting of H claim 1 , F claim 1 , Cl claim 1 , Br claim 1 , I claim 1 , —CN claim 1 , Calkyl claim 1 , Chaloalkyl and Calkoxy.8. The compound of wherein Ris Calkyl claim 1 , Chaloalkyl claim 1 , Ccycloalkyl or —NRR.9. The compound of claim 8 , wherein Ris selected from the group consisting of methyl claim 8 , ethyl claim 8 , propyl claim 8 , trifluoromethyl claim 8 , difluoromethyl claim 8 , monofluoromethyl claim 8 , isopropyl and cyclopropyl.10. (canceled)11. The compound of wherein Ris selected from the group consisting of: methyl claim 1 , ethyl claim 1 , tert-butyl claim 1 , dimethylamino claim 1 , methylamino claim 1 , amino claim 1 , morpholino claim 1 , azetidino claim 1 , imidazolyl claim 1 , 3-hydroxyazetidino claim 1 , 3-fluoroazetidino claim 1 , cyclopropyl claim 1 , pyrrolidinyl claim 1 , 3 claim 1 ,3-difluoroazetidino claim 1 , tert-butyl claim 1 , ethyl claim 1 , 2-methoxyethyl claim 1 , 3-methoxyazetidino claim 1 , 2-hydroxyethyl claim 1 , 3-hydroxypyrrolidinyl claim 1 , and N-methylimidazolyl.12. The compound of wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)-is an optionally substituted group selected from the group consisting of Calkylene claim 1 , Calkenylene or Calkynylene.13. The compound of claim 1 , wherein Xis —O— or —N(H)—; Xis absent; the subscript m is 1; and -(L)-is selected from the group consisting of —CH— claim 1 , —C(═O)— claim 1 , —C(H)(CH)— claim 1 , —CH—CH— claim 1 , —CH—C(H)(CH)— claim 1 , —C(H)(CH)—C(H)— claim 1 , —CHCHCH— claim 1 , —CH—C(H)(CH)—CH— or —CHCHCHCH—.14. The compound of claim 13 , wherein ...

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05-11-2015 дата публикации

Therapeutic compounds

Номер: US20150315127A1
Автор: Raymond G. Booth

The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C and/or RSK disorders, including diseases and disorders mediated by GPCRs and/or RSKs.

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05-11-2015 дата публикации

BICYCLIC COMPOUNDS

Номер: US20150315128A1
Автор: Xiao Hai-Yun
Принадлежит:

Disclosed are compounds of Formula (I) 112-. (canceled)14. The compound according to claim 13 , wherein said crystalline Form N-1 is substantially pure.15. A pharmaceutical composition comprising the compound in crystalline Form N-1 according to ; and at least one pharmaceutically acceptable carrier and/or diluent. This application is a continuation of U.S. application Ser. No. 14/185,164, filed Feb. 20, 2014, which claims priority to U.S. Provisional Application No. 61/767,531 filed on Feb. 21, 2013, whose contents are hereby incorporated by reference.The present invention generally relates to bicyclic compounds useful as S1Pagonists. Provided herein are bicyclic compounds, compositions comprising such compounds, and methods of their use. The invention further pertains to pharmaceutical compositions comprising at least one compound according to the invention that are useful for the treatment of conditions related to S1Pmodulation, such as autoimmune diseases and vascular disease.Sphingosine-1-phosphate (SIP) is a zwitterionic lysophospholipid metabolite of sphingosine (Sph), which in turn is derived from enzymatic cleavage of ceramides. Enzymatic phosphorylation of Sph by two kinases (SphK1 and SphK2) leads to the production of S1P largely from erythrocytes, but also from a radiation resistant source, possibly the lymphatic endothelium (Pappu, R. et al., 316:295-298 (2007)). Originally thought to operate solely as an intracellular signaling molecule, S1P was subsequently identified as a high affinity ligand for five members of the endothelial differentiation gene (EDG) class of G-protein coupled receptors (GPCRs) named S1Por S1P1, S1Por S1P2, S1Por S1P3, S1Por S1P4, and S1Por S1P5 (formerly called EDG-1, EDG-5, EDG-3, EDG-6, and EDG-8, respectively) (Chun, J. et al., 62:579-587 (2010)). The interaction of S1P with the SIP receptors plays a fundamental physiological role in a large number of processes including cell proliferation, cell morphology, tumor cell ...

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05-11-2015 дата публикации

SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS

Номер: US20150315211A1
Принадлежит:

This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients. 25.-. (canceled)6. A pharmaceutical composition comprising a compound according to or a physiologically acceptable salt claim 1 , solvate claim 1 , hydrate or stereoisomer thereof and a pharmaceutically acceptable diluent or carrier.710.-. (canceled)11. A method of selectively modulating MCL-1 in cells comprising contacting a cell with one or more compounds of claim 1 , thereby regulating MCL-1 in said cell.12. A method for modulating apoptotic cell death in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating apoptotic cell death in said cell.13. A method for modulating autophagy in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating autophagy in said cell.14. A method for modulating necrotic cell death in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating necrotic cell death in said cell.15. A method for modulating metabolism in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating energy production and consumption to effect cell viability in said cell.16. A method for modulating cell division in a cell comprising contacting a cell with one or more compounds of claim 1 , thereby regulating proliferation in said cell.17. A method for modulating transcription in a cell comprising contacting a cell with one or more compounds of claim 1 , ...

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03-11-2016 дата публикации

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Номер: US20160318931A1
Принадлежит: VERTEX PHARMACEUTICALS INCORPORATED

The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators. 313-. (canceled)1618-. (canceled)20. (canceled)2231-. (canceled)3739-. (canceled)4142-. (canceled)4445-. (canceled)49. (canceled)5155-. (canceled)5762-. (canceled)6467-. (canceled)68. A pharmaceutical composition comprising a compound of formula I according to and a pharmaceutically acceptable carrier or adjuvant.69. The composition according to claim 68 , wherein said composition comprises an additional agent selected from a mucolytic agent claim 68 , bronchodialator claim 68 , an anti-biotic claim 68 , an anti-infective agent claim 68 , an anti-inflammatory agent claim 68 , CFTR modulator claim 68 , or a nutritional agent.70. A method of modulating ABC transporter activity comprising the step of contacting said ABC transporter with a compound of formula I according to .7172-. (canceled)73. A kit for use in measuring the activity of a ABC transporter or a fragment thereof in a biological sample in vitro or in vivo claim 1 , comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(i) a composition comprising a compound of formula I according to ;'} a) contacting the composition with the biological sample;', 'b) measuring activity of said ABC transporter or a fragment thereof., '(ii) instructions for7475-. (canceled) The present application claims priority under 35 U.S.C. §119 to U.S. Provisional Application No. 60/582,676, filed Jun. 24, 2004 and entitled “MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS”, U.S. Provisional Application No. 60/630,127, filed Nov. 22, 2004 and entitled “MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS”, U.S. Provisional Application No. 60/635,674, filed Dec. 13, 2004 and entitled “MODULATORS OF ATP- ...

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17-11-2016 дата публикации

Photobase generators and photoresist compositions comprising same

Номер: US20160334703A1

New photobase generators suitable for use in photoresists are provided that correspond to Formula (I): X 1 —R 1 —O—C(═O)N(R 2 )R 3   (I) wherein X 1 is an optionally substituted aromatic group; R 1 is a linker; and R 2 and R 3 are the same or different optionally substituted linear, branched or cyclic aliphatic group or an optionally substituted aromatic group, wherein at least one of R 2 and R 3 is an optionally substituted branched alkyl group having 4 or more carbon atoms.

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01-12-2016 дата публикации

COMPOUNDS FOR USE AS GPR120 AGONISTS

Номер: US20160347768A1
Принадлежит: Piramal Enterprises Limited

The present invention relates to a compound of formula (I), or a tautomer, stereoisomer, geometrical isomer, prodrug, carboxylic acid isostere, solvate, polymorph, N-oxide, S-oxide or pharmaceutically acceptable salt thereof, which are GPR120 agonists. The present invention also relates to a pharmaceutical composition of a compound of formula (I) for the treatment of metabolic disorders, particularly Type 2 diabetes and associated diseases. 3. A compound according to claim 1 , wherein{'sup': 1', '2, 'Rand Rare combined together with one or two atoms of Ring A to formi) a 3- to 8-membered, partly saturated or saturated carbocycle; orii) a 3- to 8-membered, saturated heterocycle which contains 1, 2 or 3 heteroatoms independently selected from the group consisting of N, O and S;{'sub': 1', '6', '1', '6', '1', '6', '6', '10, 'wherein the carbocycle or heterocycle is unsubstituted or substituted with the one or more groups independently selected from the group consisting of (C-C)alkyl, halo(C-C)alkyl, (C-C)alkoxy, hydroxy, halogen, cyano, (C-C)aryl, heteroaryl and heterocyclyl.'}5. A compound according to claim 1 , wherein Ring A is 6- to 10-membered aromatic carbocycle claim 1 , wherein aromatic carbocycle is unsubstituted or substituted with one or more groups independently selected from the group consisting of (C-C)alkyl claim 1 , halo(C-C)alkyl claim 1 , hydroxy claim 1 , halogen claim 1 , (C-C)alkoxy claim 1 , halo(C-C)alkoxy claim 1 , (C-C)aryl claim 1 , (C-C)cycloalkyl claim 1 , heteroaryl claim 1 , heterocyclyl claim 1 , amino claim 1 , cyano claim 1 , nitro claim 1 , —C(O)O(C-C)alkyl claim 1 , —C(O)NRRand —S(O)R; wherein R claim 1 , R claim 1 , Rand t are as defined above.6. A compound according to claim 1 , wherein Ring A is phenyl; wherein phenyl is unsubstituted or substituted with one or more groups independently selected from the group consisting of (C-C)alkyl claim 1 , halo(C-C)alkyl claim 1 , hydroxy claim 1 , halogen claim 1 , (C-C)alkoxy claim 1 , halo( ...

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01-12-2016 дата публикации

Alkenes as alkyne equivalents in radical cascades terminated by fragmentations

Номер: US20160347778A1

Disclosed are methods for rerouting radical cascade cyclizations by using alkenes as alkyne equivalents. The reaction sequence is initiated by a novel 1,2 stannyl shift which achieves chemo- and regioselectivity in the process. The radical “hopping” leads to the formation of the radical center necessary for the sequence of selective cyclizations and fragmentations to follow. In the last step of the cascade, the elimination of a rationally designed radical leaving group via β-C—C bond scission aromatizes the product without the need for external oxidant. The Bu 3 Sn moiety, which is installed during the reaction sequence, allows further functionalization of the product via facile reactions with electrophiles as well as Stille and Suzuki cross-coupling reactions. This selective radical transformation opens a new approach for the controlled transformation of enynes into extended polycyclic structures of tunable dimensions.

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10-12-2015 дата публикации

COLORING MATERIAL AND METHOD FOR PRODUCING THE SAME

Номер: US20150353472A1
Принадлежит:

The present invention is to provide a color material with excellent dyeing property and excellent heat resistance, and a method for producing the color material, which is able to obtain the color material with high purity and at high yield. Disclosed is a color material represented by the following general formula (I): 2. The color material according to claim 1 , wherein the anion (B) in the general formula (I) is an organic anion having a sulfonato group (—SO— group).3. The color material according to claim 1 , wherein the organic anion is an anion represented by the following general formula (II):{'br': None, 'sup': 2', '−, 'sub': '3', 'Ar\ue8a0SO]\u2003\u2003General Formula (II)'}{'sup': '2', 'wherein Aris a monovalent aromatic group which can have a substituent group.'} The present invention relates to a novel color material with excellent heat resistance and dyeing property, and a method for producing the same.Today, many dyes are known and they are broadly classified into natural dyes and synthetic dyes. Examples of the synthetic dyes include aniline blue, fuchsine and methyl orange. Most of the synthetic dyes have an aromatic or heterocyclic ring, and they are each classified as either an ionic compound (e.g., all water-soluble dye) or a nonionic compound (e.g., disperse dye). In addition, in the case of ionic dyes, they are classified into anionic dyes and cationic dyes.The cationic dyes are made of an organic cation, which has a positive charge delocalized over a covalent bond, and an anion, which is generally inorganic. Also, they are generally dyes in which an amino group, which can have a substituent group, is involved in resonance. Therefore, the selection of cationic dyes depends on the number and type of anions, which are counter ions. Examples of counter anions include chloride ion, bromide ion, iodide ion, perchlorate ion, tetrafluoroborate ion, hexafluorophosphate ion, alkyl or aryl sulfate ion, tosylate ion, acetate or oxalate ion, etc.In general, ...

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17-12-2015 дата публикации

COMPOSITION FOR TREATMENT OF PATHOGENS THAT ARE RESISTANT TO TETRACYCLINES

Номер: US20150359791A1
Принадлежит:

The invention relates to compounds and pharmaceutical compositions useful in combination with tetracyclines in the treatment of bacterial infections caused by Gram-positive and Gram-negative pathogens, with particular efficacy in tetracycline resistant strains. These compounds specifically bind to TetR and therefore prevent the transcriptional activation of tet resistance genes. The compounds have a potentiating effect on the activity of members of the tetracycline family, in particular of tetracycline, minocycline, doxycycline and tigecycline, in the treatment of tetracycline susceptible, intermediate and tetracycline resistant pathogens. 1. A pharmaceutical composition comprising(a) one or more tetracyclines;(b) a TetR binding compound preventing TetR from dissociation of the tetO operator sequence in the presence of the inducing antibiotic tetracycline.3. A pharmaceutical composition according to or , wherein the tetracycline (a) is selected from the group consisting of tetracycline , oxytetracycline , chlorotetracycline , demeclocycline , meclocycline , rolitetracycline , 6-thiatetracycline , 4-epi-anhydrochlortetracycline , aminomethylcycline , azatetracycline , fluorocycline , pentacycline , minocycline , doxycycline and tigecycline.4. A pharmaceutical composition according to or , wherein the TetR binding compound (b) is a compound of formula (1) , (2) , (3) and (4) , wherein{'sup': '1', 'Ris hydrogen or methyl;'}{'sup': '2', 'Ris hydrogen or methyl;'}{'sup': 3', '4, 'Rand Rare, independently of each other, hydrogen, lower alkyl, halo-lower alkyl, halogen, cyano, lower alkoxy, optionally substituted lower alkylcarbonylamino, or phenyl;'}{'sup': '5', 'Ris hydrogen, methyl, trifluoromethyl, fluorine, chlorine or cyano;'}{'sup': '6', 'Ris hydrogen, phenoxy or phenyl;'}{'sup': '7', 'Ris lower alkyl, cyclohexyl-lower alkyl, phenyl, unsubstituted or substituted by one, two or three substituents selected from lower alkyl, halo-lower alkyl, halogen, cyano, hydroxy, ...

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24-12-2015 дата публикации

Lysine specific demethylase-1 inhibitors and their use

Номер: US20150368186A1
Принадлежит: Oryzon Genomics SA

The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH 2 C(=0)NH 2 , heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH 2 —, —CH 2 CH 2 —, —CH 2 CH 2 CH 2 —, and —CH 2 CH 2 CH 2 CH 2 —; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH 2 , —NH(C 1 -C 6 alkyl), —N(C 1 -C 6 alkyl)(C 1 -C 6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)-(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.

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24-12-2015 дата публикации

CYCLOALKENYL HYDROXAMIC ACID DERIVATIVES AND THEIR USE AS HISTONE DEACETYLASE INHIBITORS

Номер: US20150368221A1
Принадлежит:

The present invention provides compounds of formula (I) or a pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein W, X, n, s, t, and Ra are as described herein. The present invention relates generally to selective inhibitors of histone deacetylase and to methods of making and using them. 2. The compound of claim 1 , wherein n is 0 claim 1 , 1 claim 1 , or 2 claim 1 , and t is 0 claim 1 , 1 claim 1 , 2 claim 1 , or 3.315-. (canceled)1718-. (canceled)2031-. (canceled)3341-. (canceled)4347-. (canceled)49. The compound of claim 42 , wherein:{'sup': b', 'c', 'cc, 'one of Ror Ris attached to Rto form a fused ring; or'}{'sup': cc', 'e, 'Ris attached to Rto form a fused ring.'}50. The compound of claim 48 , wherein:{'sup': b', 'c', 'cc, 'one of Ror Ris attached to Rto form a fused ring; or'}{'sup': cc', 'e, 'Ris attached to Rto form a fused ring.'}5175-. (canceled)76. The compound of claim 48 , wherein Rand Rtaken together with the carbon atom to which they are attached form a spirocyclic ring.77151-. (canceled)153175-. (canceled)177187-. (canceled)189. A pharmaceutical composition comprising an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , tautomer claim 1 , or prodrug thereof; and a pharmaceutical carrier claim 1 , diluent claim 1 , or excipient.190. A method of treating or preventing a disease claim 1 , disorder claim 1 , or condition in a subject comprising administering to the subject in need thereof an effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , solvate claim 1 , tautomer claim 1 , or prodrug thereof.191. The method of claim 190 , wherein the disease claim 190 , disorder claim 190 , or condition is selected from neurological disorder claim 190 , infectious disease claim 190 , inflammatory disease claim 190 , neoplastic disease claim 190 , autoimmune disease claim 190 , heteroimmune disease claim 190 , metabolic disease claim 190 , and a ...

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24-12-2015 дата публикации

LIQUID CRYSTAL COMPOUND, LIQUID CRYSTAL COMPOSITION AND LIQUID CRYSTAL DISPLAY DEVICE

Номер: US20150368272A1
Принадлежит:

To provide a liquid crystal compound satisfying at least one physical property such as high stability to light, a high clearing point, low minimum temperature of a liquid-crystal phase, small viscosity, suitable optical anisotropy, large dielectric anisotropy, a large dielectric constant in a minor axis direction, a suitable elastic constant, excellent compatibility with other liquid crystal compounds. The compound is represented by formula (1-1): 11. Use of at least one compound according to as a component of a liquid crystal composition.12. A liquid crystal composition containing at least one liquid crystal compound according to .17. The liquid crystal composition according to claim 12 , further containing at least one optically active compound and/or polymerizable compound.18. The liquid crystal composition according to claim 12 , further containing at least one antioxidant and/or ultraviolet light absorber.19. A liquid crystal display device claim 12 , including the liquid crystal composition according to . This application claims the benefit of priority to Japanese Application No. 2014-129217, filed Jun. 24, 2014, and Japanese Application No. 2014-158794, filed Aug. 4, 2014 in the Japanese Patent Office. All disclosures of the documents named above are incorporated herein by reference.The invention relates to a liquid crystal compound, a liquid crystal composition and a liquid crystal display device. More specifically, the invention relates to a compound having a difluoromethyleneoxy group, a liquid crystal composition containing the compound and having a nematic phase, and a liquid crystal display device including the composition.The liquid crystal display device is widely utilized for a display of a personal computer, a television and so forth. The device utilizes optical anisotropy, dielectric anisotropy and so forth of the liquid crystal compound. As an operating mode of the liquid crystal display device, a phase change (PC) mode, a twisted nematic (TN) ...

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29-12-2016 дата публикации

1,2-NAPHTHOQUINONE BASED DERIVATIVE AND METHOD OF PREPARING THE SAME

Номер: US20160376243A1
Принадлежит: KT&G LIFE SCIENCES CORPORATION

Disclosed are a compound represented by Formula (1), or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, tautomer, enantiomer, or pharmaceutically acceptable diastereomer thereof, a method of preparing the same, and a pharmaceutical composition, which have effects for treatment or prevention of metabolic syndromes, comprising the same: 2. The compound or the pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , prodrug claim 1 , tautomer claim 1 , enantiomer claim 1 , or pharmaceutically acceptable diastereomer thereof according to claim 1 ,{'sub': 1', '2', '3', '3, 'wherein X, and Xare each independently C(H), CO, or N(R″), where R″ is hydrogen or C1-C3 alkyl; and'}{'sub': 3', '4, 'Xand Xare each independently C(H) or N.'}3. The compound or the pharmaceutically acceptable salt claim 2 , hydrate claim 2 , solvate claim 2 , prodrug claim 2 , tautomer claim 2 , enantiomer claim 2 , or pharmaceutically acceptable diastereomer thereof according to claim 2 , wherein Xis C(H) claim 2 , N claim 2 , NH claim 2 , or NCH;{'sub': '2', 'Xis C(H) or CO; and'}{'sub': 3', '4, 'Xand Xare each independently C(H) or N.'}4. The compound or the pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , prodrug claim 1 , tautomer claim 1 , enantiomer claim 1 , or pharmaceutically acceptable diastereomer thereof according to claim 1 , wherein Rand Rare each independently hydrogen claim 1 , F claim 1 , C1 claim 1 , —OCH claim 1 , —OCHCH claim 1 , —O(CH)CH claim 1 , —CH claim 1 , —NO claim 1 , —N(CH) claim 1 , —NHCOCH claim 1 , —NHCOCH claim 1 , —NHCOCH claim 1 , —CN or —OH.5. The compound or the pharmaceutically acceptable salt claim 1 , hydrate claim 1 , solvate claim 1 , prodrug claim 1 , tautomer claim 1 , enantiomer claim 1 , or pharmaceutically acceptable diastereomer thereof according to claim 1 , wherein Ris hydrogen claim 1 , substituted or unsubstituted methyl claim 1 , ethyl claim 1 , n-propyl claim 1 , isopropyl claim 1 ...

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16-06-2015 дата публикации

Alpha, beta-unsaturated imines

Номер: US9055743B2
Принадлежит: Bayer Intellectual Property GmbH

The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors.

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29-09-2015 дата публикации

Method of preparing (S)-2-amino-5-methoxytetralin hydrochloride

Номер: US9145353B2

A method of preparing (S)-2-amino-5-methoxytetralin hydrochloride[(S)-2-amino-5-methoxyl-1,2,3,4-tetrahydronaphthalene hydrochloride], comprising the steps of: (1) producing a compound (I) by addition-elimination reaction of 5-methoxy-2-tetralone and R-(+)-a-phenylethylamine; (2) producing a compound (II) by reduction reaction of the compound (I) with a reducing agent; and (3) producing a compound (II) hydrochloride by reacting the compound (II) with a salt-forming agent, then carrying out reduction reaction with a palladium-carbon catalyst to produce (S)-2-amino-5-methoxytetralin hydrochloride. The method can significantly increase the yield of (S)-2-amino-5-methoxytetralin hydrochloride with short synthetic path, low preparation cost and less pollution, which is environmentally friendly and is suitable for medical industrialized production. The structural formulae of the compound (I) and the compound (II) are: respectively.

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27-10-2015 дата публикации

Antagonists of the glucagon receptor

Номер: US9169201B2
Принадлежит: Metabasis Therapeutics Inc

The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

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25-08-2015 дата публикации

Tetrahydronaphthalenyl compounds useful as sipi agonists

Номер: US9115054B2
Принадлежит: Bristol Myers Squibb Co

Disclosed are compounds of Formula (I) and/or a salt thereof; wherein R is —OH or —OP(O)(OH) 2 . Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P 1 , and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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09-05-2017 дата публикации

Cycloalkyl-dione derivatives and methods of their use

Номер: US9643919B2
Принадлежит: University of Pennsylvania Penn

The present invention is directed to compounds of formula I: wherein A is n is 0, 1, or 2; m is 0 or 1; R 1 is H or C 1-6 alkyl and R 2 is H, C 1-6 alkyl, C 1-6 alkaryl, aryl, or heteroaryl; and X is O or NH. Tautomers, enantiomers, and diastereomers, as well as pharmaceutically acceptable salt forms, of compounds of formula I are also within the scope of the invention. Methods of preparing and using the compounds of formula I are also described. wherein A is

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20-12-2016 дата публикации

Substituted bicyclic compounds

Номер: US9522888B2
Принадлежит: Bristol Myers Squibb Co

Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): and/or a salt thereof, wherein R 1 is —OH or —OP(O)(OH) 2 , and X 1 , X 2 , X 3 , R 2 , R 2a , R a , R b , and R c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P 1 , and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

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04-08-2015 дата публикации

Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy

Номер: US9096619B2

The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.

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23-08-2016 дата публикации

Substituted naphthalenes as feedstock for plasticizer production

Номер: US9422227B2
Принадлежит: ExxonMobil Research and Engineering Co

Provided are compounds and processes of making compounds of the formula: wherein x=4 to 8, R is H, C 1 to C 4 alkyl, —C(O)OR 1 or —OC(O)R 1 , y=4 to 8, R′ is H, C 1 to C 4 alkyl, and at least one R′ is —C(O)OR 1 or —OC(O)R 1 , wherein R 1 is a branched C 4 to C 14 alkyl, and their use in polymer compositions.

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16-05-2017 дата публикации

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

Номер: US9653689B2
Принадлежит: Samsung Display Co Ltd, SFC Co Ltd

A condensed-cyclic compound represented by Formula 1 below, and an organic light-emitting diode including the condensed-cyclic compound. wherein R 1 through R 6 , Ar 5 and Ar 6 , and X 1 through X 10 are defined as in the specification.

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10-02-2015 дата публикации

N-substituted benzamides and methods of use thereof

Номер: US8952169B2
Принадлежит: Genentech Inc, Xenon Pharmaceuticals Inc

The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables R A , subscript n, ring A, X 2 , L, subscript m, X 1 , B, R 1 , R 2 , R 3 , R 4 , R 5 and R N have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.

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12-04-2016 дата публикации

Pesticidal diaryl—heterocyclyl derivatives

Номер: US9307764B2
Принадлежит: Bayer Intellectual Property GmbH

To provide pesticidal allylAryl heterocycle derivatives that are useful as a pesticidal compound. Pesticidal allylAryl heterocycle derivatives that are expressed by the Formula (I), and pesticides and an agent for controlling animal parasites which include the allylAryl heterocycle derivatives as an effective component.

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06-10-2015 дата публикации

Neuro-protective compounds and their use

Номер: US9150608B2
Принадлежит: Biotechnology Research Corp Ltd

Isolated compounds from Adelostemma gracillimum refined fractions and compositions containing the compounds are provided by the present invention. Adelostemma gracillimum refined fractions and the extraction process thereof are also provided by the present invention. The uses of the compounds and the Adelostemma gracillimum refined fractions for inhibiting the activities of NMDA receptor or amyloid-beta peptide, for improving memory, and for treating neurodegenerative diseases, neuropathological conditions or epilepsy are further provided by the present invention.

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01-09-2015 дата публикации

Radiation-sensitive resin composition, compound and producing method of compound

Номер: US9120726B2
Автор: Ken Maruyama
Принадлежит: JSR Corp

A radiation-sensitive resin composition includes a compound shown by a following general formula (A), a solvent and a resin having an acid-labile group. Each of R 1 and R 2 independently represents a substituted or unsubstituted monovalent hydrocarbon group having 1 to 25 carbon atoms. Each of X and Z independently represents a substituted or unsubstituted divalent hydrocarbon group having 1 to 25 carbon atoms. Y represents a single bond or the like. n represents an integer from 0 to 5.

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17-04-2018 дата публикации

Compounds that are S1P modulating agents and/or ATX modulating agents

Номер: US09944666B2
Принадлежит: Biogen MA Inc

Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

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23-01-2018 дата публикации

Compounds useful as immunomodulators

Номер: US09872852B2
Принадлежит: Bristol Myers Squibb Co

Disclosed are compounds of Formula (I): (I). Also disclosed are methods of using such compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of virological diseases or disorders and cancer.

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19-09-2017 дата публикации

IDO inhibitors

Номер: US09765018B2

There are disclosed compounds of formula (I) that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

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08-08-2017 дата публикации

Fluorinated benzenesulfonamides as inhibitors of carbonic anhydrase

Номер: US09725467B2
Принадлежит: VILNIAUS UNIVERSITETAS

Novel fluorinated benzenesulfonamides compounds of general formula (I) can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit enzymes which participate in disease progression.

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01-08-2017 дата публикации

Synthetic building blocks for the production of materials for organic electroluminescence devices

Номер: US09718764B2
Принадлежит: Merck Patent GmBH

The present invention relates to compounds which are suitable as synthesis precursors for the production of electronically active materials for use in organic electroluminescence devices.

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11-07-2017 дата публикации

Antagonists of the glucagon receptor

Номер: US09701626B2
Принадлежит: Metabasis Therapeutics Inc

The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.

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11-07-2017 дата публикации

Pesticidal compositions and processes related thereto

Номер: US09701620B2
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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20-06-2017 дата публикации

Compounds for use in imaging, diagnosing and/or treatment of diseases of the central nervous system or of tumors

Номер: US09682944B2
Принадлежит: PIRAMAL IMAGING SA

This invention relates to novel compounds suitable for labelling or already labelled by 18 F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).

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20-06-2017 дата публикации

Composition for treatment of pathogens that are resistant to tetracyclines

Номер: US09682079B2
Принадлежит: BioVersys AG

The invention relates to compounds and pharmaceutical compositions useful in combination with tetracyclines in the treatment of bacterial infections caused by Gram-positive and Gram-negative pathogens, with particular efficacy in tetracycline resistant strains. These compounds specifically bind to TetR and therefore prevent the transcriptional activation of tet resistance genes. The compounds have a potentiating effect on the activity of members of the tetracycline family, in particular of tetracycline, minocycline, doxycycline and tigecycline, in the treatment of tetracycline susceptible, intermediate and tetracycline resistant pathogens.

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06-06-2017 дата публикации

Tetralin and indane derivatives and uses thereof

Номер: US09670151B2
Принадлежит: Roche Palo Alto LLC

Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, p, q, Ar, R 1 and R 2 are as defined herein. Also provided are methods for preparing, compositions comprising, and methods for using compounds of formula I.

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09-05-2017 дата публикации

Integrated process for production of high octane gasoline, high aromatic naphtha and high cetane diesel from high aromatic middle distillate range streams

Номер: US09644155B2
Принадлежит: Indian Oil Corp Ltd

An integrated process for production of ultra low sulfur products of high octane gasoline, high aromatic naphtha and high Cetane Diesel from high aromatic middle distillate range streams from any cracker units such as Light Cycle Oil (LCO) stream of Fluid catalytic cracking (FCC) units and subjected to hydrotreating for removal of heteroatoms like sulfur and nitrogen. The effluent from hydrotreating is subjected to hydrocracking at same pressure of hydrotreating step above for selective opening of saturated ring of multi-ring aromatics. The effluent from hydrocracking is separated in CUT-1, CUT 2 in which the monoaromatics and alkylated monoaromatics are concentrated and CUT-3 in which concentration of saturates significantly increased. The CUT-3 is selectively oxidized in selective oxidation step in presence of catalyst, an oxidizing agent and operating conditions such that it results in diesel product with more enhanced Cetane.

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25-04-2017 дата публикации

Pesticidal compositions and processes related thereto

Номер: US09630910B2
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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18-04-2017 дата публикации

Pesticidal compositions and processes related thereto

Номер: US09622477B2
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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11-04-2017 дата публикации

Method for producing novel organometallic complex and amine compound

Номер: US09617292B2
Принадлежит: Kanto Chemical Co Inc

The purpose of the invention is to provide a novel organometallic compound that can be utilized as a catalyst having high generality, high activity, and excellent functional group selectivity. The invention pertains to a novel organometallic compound represented by general formula (1) that catalyzes a reductive amination reaction.

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11-04-2017 дата публикации

Pesticidal compositions and processes related thereto

Номер: US09615576B2
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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21-03-2017 дата публикации

Arylalkylamine compounds as calcium sensing receptor modulators

Номер: US09598371B2
Принадлежит: LUPIN ATLANTIS HOLDINGS SA

The present invention provides arylalkylamine compounds as calcium sensing receptor modulators (CaSR). In particular, the compounds described herein are useful for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of calcium sensing receptors (CaSR). The invention also provides herein the pharmaceutical compositions thereof, and methods for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of CaSR. The invention also relates to process for the preparation of the compounds of the invention. (Formula I)

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21-03-2017 дата публикации

Quinone based nitric oxide donating compounds for ophthalmic use

Номер: US09598349B2
Принадлежит: Nicox Science Ireland Ltd

The present invention relates to nitric oxide donor compounds having a quinone based structure, to processes for their preparation and to their use in the treatment and/or prophylaxis of glaucoma and ocular hypertension.

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28-02-2017 дата публикации

Aromatic acylation with cyclic anhydride for plasticizer production

Номер: US09580571B2
Принадлежит: ExxonMobil Research and Engineering Co

Provided is a process for making non-phthalate plasticizers, by acylating an aromatic compound with a succinic anhydride to form a keto-acid, and then esterifying the keto-acid with C 4 -C 13 OXO-alcohols to form a plasticizer compound. The aromatic rings of the aromatic compound may also be optionally hydrogenated.

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28-02-2017 дата публикации

Aryloxyurea compound and pest control agent

Номер: US09580384B2
Принадлежит: Nippon Soda Co Ltd

The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein R 1 to R 5 each independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof.

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21-02-2017 дата публикации

Therapeutic compounds

Номер: US09573906B2
Принадлежит: Arizona State University ASU

The invention provides compounds of formulae (I), (II), (III), and (IV): and salts thereof, as well as pharmaceutical compositions comprising such compounds. The compounds are useful for treating cancers and Alzheimer's disease.

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14-02-2017 дата публикации

N-(4-(bis(4-(dimethylamino)phenyl)methylene)-8-(dimethylamino)

Номер: US09567291B2
Автор: Jack Arbiser
Принадлежит: EMORY UNIVERSITY

This disclosure relates to N-(4-(bis(4-(dimethylamino)phenyl)methylene)-8 -(dimethylamino)naphthalen-1(4H)-ylidene)-N-methylmethanaminium, derivatives, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I. In certain embodiments, the disclosure relates to methods of treating or preventing Nox related diseases and conditions comprising administering an effective amount of compounds disclosed herein to a subject in need thereof. In certain embodiments, the Nox related disease or condition is cancer.

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24-01-2017 дата публикации

Compounds that are S1P modulating agents and/or ATX modulating agents

Номер: US09550798B2
Принадлежит: Biogen MA Inc

Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX).

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10-01-2017 дата публикации

Pesticidal compositions and processes related thereto

Номер: US09538756B2
Принадлежит: DOW AGROSCIENCES LLC

This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.

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06-12-2016 дата публикации

Aromatic acylation with cyclic anhydride for plasticizer production

Номер: US09512296B2
Принадлежит: ExxonMobil Research and Engineering Co

Provided is a process for making non-phthalate plasticizers, by acylating an aromatic compound with a succinic anhydride to form a keto-acid, and then esterifying the keto-acid with C 4 -C 13 OXO-alcohols to form a plasticizer compound. The aromatic rings of the aromatic compound may also be optionally hydrogenated.

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29-11-2016 дата публикации

Intermediate for synthesizing treprostinil diethanolamine and method for preparing the same

Номер: US09505704B2
Принадлежит: Everlight Chemical Industrial Corp

The present invention relates to a method for treprostinil diethanolamine synthesis. The present invention also relates to a novel intermediate used in the method for treprostinil diethanolamine synthesis. The novel intermediate is shown in the following formula (II): wherein R1 and R2 are described in the description.

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