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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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Применить Всего найдено 3976. Отображено 198.
20-01-2016 дата публикации

ПРОИЗВОДНЫЕ ФЕНИЛОКСАДИАЗОЛА В КАЧЕСТВЕ ИНГИБИТОРОВ PGDS

Номер: RU2572608C2
Принадлежит: САНОФИ (FR)

Изобретение относится к соединениям формулы (I), где R1 представляет собой водород или C-Cалкил; R2 представляет собой водород и R3 представляет собой гидрокси(C-C)алкил; или их фармацевтически приемлемым солям. Также изобретение относится к способам получения соединений формулы (I), промежуточным соединениям, указанным в пп.14-19 формулы изобретения, и способу получения промежуточного соединения по п.17 формулы изобретения. Технический результат - соединения формулы (I) в качестве ингибиторов PGD2-синтазы и промежуточные соединения для их получения. 9 н. и 11 з.п. ф-лы, 3 пр.

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20-06-2001 дата публикации

БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, СПОСОБ ПОДАВЛЕНИЯ СЛИПАНИЯ ТРОМБОЦИТОВ И КОМПОЗИЦИЯ ДЛЯ ЕГО ОСУЩЕСТВЛЕНИЯ

Номер: RU2169146C2

Описываются новые бициклические соединения, имеющие ядро, сформированное из двух конденсированных шестичленных колец, А и В, представленное формулой I, либо фармацевтически приемлемая соль, сольват или пролекарственная производная этого соединения, в котором бициклическое ядро из колец А и В выбирается из группы, состоящей из формул (17)-(21), R3 является кислотной группой, содержащей кислотный радикал, выбранный из формул группы (С), n = 0-6; R0 является одинаковым или разным и выбирается независимо из водорода, алкила, связующая группа -(L)- является связью или выбирается из формул -C(=O)-N(H)- и -С(Н2)-O-, Q является основной группой и выбирается из амидиногруппы и пиперидина. Новые бициклические соединения полезны в качестве препаратов, нейтрализующих действие гликопротеина IIв/IIIа, для предотвращения тромбоза. Описывается также способ подавления слипания тромбоцитов и композиция для его осуществления. 13 с. и 12 з.п. ф-лы, 1 табл.

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27-04-2010 дата публикации

ПРОИЗВОДНЫЕ НАФТАЛИНА, ПРИГОДНЫЕ В КАЧЕСТВЕ ЛИГАНДОВ РЕЦЕПТОРОВ 3 ГИСТАМИНА

Номер: RU2387638C2
Принадлежит: Ф.ХОФМАНН-ЛЯ РОШ АГ (CH)

Изобретение относится к новым производным нафталина формулы I , а также к их фармацевтически приемлемым солям, которые могут найти применение для лечения и/или профилактики заболеваний, связанных с модулированием Н-3 рецепторов. В формуле I R1 выбран из водорода, низшего алкила, фенила, фенила-низшего алкила и низшего алкоксиалкила; R2 выбран из водорода, низшего алкила, С3-С7-циклоалкила, низшего алкоксиалкила или низшего алкилсульфанилалкила (все значения R1 и R2 приведены в формуле изобретения); или R1 и R2 вместе с атомом азота, к которому они присоединены, образуют 4-7-членное насыщенное или частично ненасыщенное гетероциклическое кольцо, которое может содержать еще один гетероатом, выбранный из атомов азота, кислорода и серы, где указанное гетероциклическое кольцо может быть незамещенным или замещенным 1-2 группами, либо оно может быть конденсировано с незамещенным фенильным кольцом; ! А выбран из ! или ! (значения R3-R7, R9, R10, X, m, n, t, p, q и s приведены в формуле изобретения ...

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10-01-2008 дата публикации

БЕНЗИЛЭФИРАМИНЫ, ПОЛЕЗНЫЕ КАК АНТАГОНИСТЫ CCR-5

Номер: RU2006120084A
Принадлежит:

... 1. Соединение общей формулы I его энантиомеры, диастереомеры, соли и сольваты, в которой Х представляет собой связь или кислород; m представляет собой 0, 1, 2, 3 или 4; n представляет собой 0, 1 или 2; R1 представляет собой необязательный заместитель, независимо выбираемый в каждом случае из галогена, алкила, галоалкила, нитро или -NR5R6; R2 представляет собой a) водород; или b) алкил, циклоалкил, алкенил, арил или гетероарил, любой из которых может быть, необязательно, замещен группой Y; Y представляет собой a) арил или гетероарил, каждый из которых может быть, необязательно, замещен одним или несколькими Z1, Z2, Z3; b) циклоалкил или гетероцикло, каждый из которых может быть, необязательно, замещен одним или несколькими Z1, Z2, Z3; c) -COOR7; d) -NR8R9; e) CHR10(OR11); f) -C(=O)-NR8R9; g) -NR12-(C=O)-NR8 R9; h) -CN; i) -C(=N-OR13); j) алкокси; R3 и R4 независимо выбирают из a)водорода; b) алкила, циклоалкила, (циклоалкил)алкила, арила, (арил)алкила, гетероцикло, (гетероцикло)алкила, гетероарила ...

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27-07-2011 дата публикации

НОВОЕ СУЛЬФОНАМИДНОЕ ПРОИЗВОДНОЕ МАЛОНОВОЙ КИСЛОТЫ И ЕГО ФАРМАЦЕВТИЧЕСКОЕ ПРИМЕНЕНИЕ

Номер: RU2010101633A
Принадлежит:

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

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27-04-2010 дата публикации

АГЕНТЫ, НАРУШАЮЩИЕ КЛЕТОЧНУЮ РЕПЛИКАЦИЮ, И ИХ ПРИМЕНЕНИЕ ДЛЯ ИНГИБИРОВАНИЯ ПАТОЛОГИЧЕСКИХ СОСТОЯНИЙ

Номер: RU2008141686A
Принадлежит:

... 1. Применение соединения, соответствующего формуле (LXVII) ! ! в которой ! R21 означает аралкил или гетероаралкил, необязательно замещенный; ! R22 означает арил или гетероаралкил, необязательно замещенный; и ! Х представляет собой О или S; ! и их фармацевтически приемлемые соли, ! для получения лекарственного средства, снижающего клеточную репликацию, для лечения, улучшения или предупреждения заболеваний, состояний и/или нарушений. ! 2. Применение по п.1, при котором R21 означает бензил, необязательно замещенный, и R22 является арилом, необязательно замещенным. ! 3. Применение по п.1 или 2, при котором R21 имеет структуру, соответствующую формуле (LXVIII) ! ! R23, R24, R25, R26 и R27 независимо друг от друга означает Н, галоген, CN; NO2; NR′R′′; алкил, алкенил, алкинил; алкокси, алкоксиалкил; -OOC-R′′′; -COO-R′′′′′; арил, гетероарил, необязательно замещенные; ! где R′ и R′′ независимо друг от друга означают атом водорода, алкил, алкенил или алкинил, арил или гетероарил; необязательно замещенные ...

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30-08-1989 дата публикации

Способ снижения гербицидного поражения кукурузы 2-хлор-N-(этоксиметил)-6-этил-о-ацетотолуидидом

Номер: SU1505425A3

Изобретение относится к химическим средствам защиты растений и может найти применение в растениеводстве , в частности, при выращивании кукурузы. Цель изобретения - повышение эффективности защиты кукурузы от повреждающего действия гербицида ацетохлора. Способ состоит в использовании в качестве средства, защищающего кукурузу от повреждающего действия ацетохлора, 2-(дихлорацетил)-1-метил-1,2,3,4-тетрагидроизохинолина в дозе 0,11-0,67 кг/га при соотношении гербицид - антидот (10-20):1. Использование указанного антидота в рекомендуемых дозах обеспечивает подавление сорняков на 85-100% при снижении повреждения кукурузы до экономически приемлемой степени - 12-15% в сравнении с 20-30%, обеспечиваемыми известным антидотом. 6 табл.

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07-07-1989 дата публикации

Способ получения (2-оксо-1,2,3,5-тетрагидроимидазо[2,1- @ ]хиназолинил)оксиалкиламидов или их фармацевтически приемлемых солей с кислотами

Номер: SU1493109A3

Изобретение относится к гетероциклическим соединениям ,в частности, к получению (2-оксо-1,2,3,5-тетрагидроимидазо [2,1-B] хиназолинил)оксиалкиламидов формулы @ , где N-1-6 A - группа-NR1R2, где R1-H или C3-C8- циклоалкил и R2-H или C1-C6-алкил, или их фармацевтически приемлемых солей с кислотами, которые обладают ингибирующими фосфодиэстеразу свойствами. Цель - разработка способа получения новых более активных соединений. Получение их ведут взаимодействием соответствующих эфиров или кислот (2-оксо-1,2,3,5-тетрагидроимидазо[2,1-B]хиназолинилов) с амином формулы HNR1R2, где R1-H или C3-C8-циклоалкил и R2-H или C1-C6-алкил. Целевой продукт выделяют в виде свободного основания или в виде фармацевтически приемлемой соли. 5 табл.

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10-05-1995 дата публикации

Pharmaceutically active isoquinolines

Номер: GB2283488A
Принадлежит:

Compounds of formula I wherein R is ethyl or n-propyl, and their physiologically-hydrolysable and -acceptable esters, and acid addition salts thereof are of useful as pharmaceuticals, e.g. for asthma therapy.

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03-12-1997 дата публикации

Isoquinolines

Номер: GB0002283488B
Автор: NAEF RETO, RETO * NAEF
Принадлежит: SANDOZ LTD, * SANDOZ LTD

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14-07-1965 дата публикации

Amines and the corresponding cyclic ureas thereof

Номер: GB0000998352A
Автор:
Принадлежит:

Compounds of the formula where R is hydrogen or an unsubstituted or substituted alkyl, aryl, aralkyl, alkaryl, cycloalkyl, alkenyl, aralkenyl or heterocyclic radical and n is 1-10, at least one of the unspecified valencies being other than hydrogen, are obtained by saponification of the bis-urethanes claimed in Specification 998,351. Compounds of the formulae where each R is aryl or heterocyclic, and also each compound of the first two formulae above which are specified, are claimed as novel. In examples (1), (2) benzaldehyde and carbamic acid ethyl ester are condensed together and the products reacted with styrene to give 1,3-diphenylpropane - 1,3 - bis - carbamic acid ethyl ester, which is hydrolysed to 1,3-diphenyl-1,3-diaminopropane and 4,6-diphenyl-2-oxohexahydropyrimidine. Similar reactions produce (3), (4) 1-phenyl-1,3-diaminopropane and 4-phenyl - 2 - oxohexahydropyrimidine: (5), (6) 1-phenyl - 3 - p ...

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09-06-1982 дата публикации

ISOQUINOLINE DERIVATIVES

Номер: GB0002007660B
Автор:
Принадлежит: RHONE POULENC IND, RHONE-POULENC INDUSTRIES

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30-09-2001 дата публикации

Oxamic acids and derivatives as thyroid receptor ligands

Номер: AP0200102259A0
Автор:
Принадлежит:

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31-05-2015 дата публикации

Anthelminitic compounds and compositions and method of using thereof

Номер: AP0201508449D0
Принадлежит:

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23-07-1997 дата публикации

HIV Protease inhibitors.

Номер: AP0000000600A
Принадлежит:

Hiv protease inhibitors, obtainable by chemical systhesis, inhibit or block the biologocal activity of the hiv protease enzyme, causing the replication of the hiv virus to terminate. These compounds as well as pharmaceutical compositions that contain these compounds and optionally other anti-viral agents as active ingrediants, are suitable for treating patients or hosts infected with the hiv virus, which is known to cause aids.

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13-09-1999 дата публикации

Biphenyl-2-carboxylic acid-tetrahydro-isoquiolin-6-yl amide derivatives.

Номер: AP0000000760A
Принадлежит:

Compounds of formula wherein X, Y, and Z are as defined in the specification. The compounds are useful in decreasing apoB secretion and are useful in the treatment of conditions such as atherosclerosis.

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30-06-2000 дата публикации

Substituted isoquinoline derivatives and their use as anticonvulsants.

Номер: AP2000001832A0
Принадлежит:

Compounds of formula (i)or pharmaceutically acceptable salts or solvates thereof, where q is a monocyclic or bicyclic aryl or heteroaryl ring, r1 is hydrogen, c1-6alkyl (optionally substituted by hydroxy or c1-4alkoxy), c1-6alkenyl, c1-6alkynyl, c1-6alkylco-, formyl, cf3co- or c1-6alkylso2-, r2 is hydrogen or up to three substituents selected from halogen, no2, cn, n3, cf3o-,cf3s-, cf3co-, trifluoromethyldiazirinyl, c1-6alkyl, c1-6alkenyl, c1-6alkynyl, c1-6perfluoroalkyl, c3-6cycloalkyl, c3-6cycloalkyl-c1-4alkyl-,c1-6alkylo-, c1-6alkylco-, c3-6cycloalkylo-, c3-6cycloalkylco-, c3-6cycloalkyl-c1-4alkylo-, c3-6cycloalkyl-c1-4alkylco-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-c1-4alkyl-, c1-6alkylso2-, (c1-4alkyl)2nso2-, (c1-4alkyl)nhso2-, (c1-4alkyl)2nco-, (c1-4alkyl)nhco, conh2, cf3so2, c1-6alkenyl, c1-6alkynyl or c1-6hydroxyalkyl; or -nr3r4 where r3 is hydrogen or c1-4alkyl, and r4 is hydrogen, c1-4alkyl, formyl, -co2c1-4alkyl or -coc1-4alkyl; or two r2 groups together form a carbocyclic ...

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30-09-2001 дата публикации

Oxamic acids and derivatives as thyroid receptor ligands.

Номер: AP2001002259A0
Принадлежит:

The present invention provides novel compounds of formula ((i)and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein r1-r8 and w are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts threof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and disease such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesterremia, depression and osteoporosis are also provided.

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31-10-1996 дата публикации

Ther peuti amid s

Номер: AP0009600848A0
Автор:
Принадлежит:

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31-07-1996 дата публикации

Therapeutic amides

Номер: AP0009600804A0
Автор:
Принадлежит:

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30-06-2006 дата публикации

Sulfonamide derivatives for the treatment of diseases

Номер: AP2006003669A0
Принадлежит:

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31-07-1996 дата публикации

HIV protease inhibitors

Номер: AP0009600844A0
Автор:
Принадлежит:

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31-05-2015 дата публикации

Anthelminitic compounds and compositions and method of using thereof

Номер: AP2015008449A0
Принадлежит:

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15-11-2001 дата публикации

Therapeutic amides

Номер: OA0000010363A
Принадлежит:

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14-01-1970 дата публикации

Process for the preparation of heterocyclic compounds.

Номер: OA0000001814A
Автор:
Принадлежит:

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09-02-2004 дата публикации

Substituted isoquinoline derivatives and their useas anticonvulsants.

Номер: OA0000011526A
Принадлежит:

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30-06-1981 дата публикации

New derivatives of the isoquinoline and their method of preparation.

Номер: OA0000006082A
Автор:
Принадлежит:

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23-08-2005 дата публикации

Oxamic acids and derivatives as thyroid receptor ligands.

Номер: OA0000011839A
Принадлежит:

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31-10-1996 дата публикации

Ther peuti amid s

Номер: AP0009600848D0
Автор:
Принадлежит:

Подробнее
30-06-2006 дата публикации

Sulfonamide derivatives for the treatment of diseases

Номер: AP0200603669D0
Принадлежит:

Подробнее
30-09-2001 дата публикации

Oxamic acids and derivatives as thyroid receptor ligands

Номер: AP0200102259D0
Автор:
Принадлежит:

Подробнее
31-07-1996 дата публикации

HIV protease inhibitors

Номер: AP0009600844D0
Автор:
Принадлежит:

Подробнее
31-05-2015 дата публикации

Anthelminitic compounds and compositions and method of using thereof

Номер: AP0201508449A0
Принадлежит:

Подробнее
30-06-2006 дата публикации

Sulfonamide derivatives for the treatment of diseases

Номер: AP0200603669A0
Принадлежит:

Подробнее
30-06-2000 дата публикации

Substituted isoquinoline derivatives and their use as anticonvulsants

Номер: AP0200001832A0
Автор:
Принадлежит:

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15-07-2007 дата публикации

TYROSINDERIVATE

Номер: AT0000364592T
Принадлежит:

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10-02-1982 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW DERIVATIVES OF 4

Номер: AT0000365601B
Автор:
Принадлежит:

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11-08-1980 дата публикации

PROCEDURE FOR the PRODUCTION OF 4-OXOHEXAHYDRO - PYRAZINOISOCHINOLINDERIVATEN AND THEIR PHYSIOLOGICALLY HARMLESS ONE SALTS

Номер: AT0000358043B
Автор:
Принадлежит:

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15-02-1977 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN CHINOLINDERIVATEN

Номер: ATA575274A
Автор:
Принадлежит:

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15-08-1998 дата публикации

ISOCHINOLINE

Номер: ATA204894A
Автор:
Принадлежит:

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15-04-2012 дата публикации

MODULATORS OF THE CELLULAR ADHESION

Номер: AT0000551339T
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15-08-1975 дата публикации

PROCEDURE FOR the PRODUCTION OF NEW ONE 3,4-DIHYDRO-2 (1H) - ISOCHINOLIN CARBOXAMIDDERIVATEN AND THEIR SALTS

Номер: AT0000602874A
Автор:
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15-02-1977 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW CHINOLINDERIVATEN

Номер: AT0000575274A
Автор:
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15-01-1978 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW ISOCHINOLIN DERIVATIVES AND YOUR SALTS

Номер: AT0000869575A
Автор:
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11-09-1978 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW ISOCHINOLIN DERIVATIVES AND YOUR SALTS

Номер: AT0000345294B
Автор:
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15-01-1980 дата публикации

PROCEDURES FOR the PRODUCTION OF 4-OXOHEXAHYDRO PYRAZINOISOCHINOLINDERIVATEN AND THEIR PHYSIOLOGICALLY HARMLESS ONE SALTS

Номер: AT0000147576A
Автор:
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11-03-1974 дата публикации

Procedure for the production of new sulphonyl urea and their salts

Номер: AT0000313914B
Автор:
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25-09-1974 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW SULPHONYL UREA AND YOUR SALTS

Номер: AT0000317912B
Автор:
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25-09-1974 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW SULPHONYL UREA AND YOUR SALTS

Номер: AT0000317914B
Автор:
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25-09-1974 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW SULPHONYL UREA AND YOUR SALTS

Номер: AT0000317916B
Автор:
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15-08-2006 дата публикации

USE OF NITRILE CONNECTIONS AS ARZTNEIMITTEL

Номер: AT0000333451T
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15-03-2004 дата публикации

SUBSTITUTED ISOCHINOLINE DERIVATIVES AND YOUR USE AS ANTICONVULSIVA

Номер: AT0000260258T
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09-02-2012 дата публикации

Modulators of Cellular Adhesion

Номер: US20120035154A1
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 4 , n, p, A, B, D, E, L and AR 1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

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23-02-2012 дата публикации

Diacylethylenediamine compound

Номер: US20120046292A1
Принадлежит: Astellas Pharma Inc

[Problem] A compound which is useful as an anti-obesity agent is provided. [Means for Solution] The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases, and as a result, they have found that the diacylethylenediamine compound of the present invention has an excellent DGAT1 inhibitory action, thereby completing the present invention. That is, the diacylethylenediamine compound of the present invention has a DGAT1 inhibitory action, and can be therefore used as an agent for preventing and/or treating obesity, type II diabetes mellitus, fatty liver, and diseases associated with these diseases.

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23-08-2012 дата публикации

New compounds, pharmaceutical compositions and uses thereof

Номер: US20120214785A1
Принадлежит: BOEHRINGER INGELHEIM INTERNATIONAL GMBH

The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.

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13-09-2012 дата публикации

Compositions and Methods for Treatment of Eye Disorders

Номер: US20120232019A1
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

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06-06-2013 дата публикации

Novel hydroxamates as therapeutic agents

Номер: US20130142758A1
Принадлежит: Pharmacyclics LLC

The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

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06-06-2013 дата публикации

Guanidine compound

Номер: US20130143860A1
Принадлежит: Astellas Pharma Inc

[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

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19-09-2013 дата публикации

Synthesis of Tripodal Catechol Derivatives Having an Adamantyl Basic Framework for Functionalizing Surfaces

Номер: US20130245269A1
Принадлежит: Justus Liebig Universitaet Giessen

The present invention describes tripodal catechol derivatives with an adamantyl basic framework for the functionalisation of surfaces, methods for their production and use. The remaining fourth bridgehead position is easily suitable to be further functionalised via so-called click reactions, by way of example with biomolecules, dyes, radiomarkers, polyethylene glycol or active agents. The compounds according to the present invention have the general formula X-Ad[(CH 2 ) n —YZ] 3 , wherein A stands for the adamantyl skeleton, X stands for a group —(CH 2 ) p —R 5 , wherein p=0 to 10 and R 5 is selected from —H, —NH 2 , —NO 2 , —OH, —SH, —O—NH 2 , —NH—NH 2 , —N═C═S—, —N═C═O—, —CH═CH 2 , —C≡CH, —COOH, —(C═O)H, —(C═O)R 6 Y stands for —CH 2 —, —CH═CH—, —O—, —S—, —S—S—, —NH—, —O—NH—, —NH—O—, —HC═N—O—, —O—N═CH—, —NR 1 —, -aryl-, -heteroaryl-, —(C═O)—, —O—(C═O)—, —(C═O)—O—, —NH—(C═O)—, —(C═O)—NH—, —NR 1 —(C═O)—, —(C═O)—NR 1 —, —NH—(C═O)—NH—, —NH—(C═S)—NH—, R 1 stands for an alkyl group, R 6 for an alkyl, alkenyl, alkynyl, aryl or heteroaryl group, and Z stands for a catechol derivative. The production of the compounds occurs by reacting a compound X-Ad[(CH 2 ) n —Y′] 3 with a reagent Y″Z to the corresponding compound X-Ad[(CH 2 ) n —YZ] 3 and subsequently purifying the reaction product. Y′ and Y″ are hereby precursors of Y. The compounds according to formula (I) according to the present invention are suitable to be used in a method to functionalise surfaces. The X group of the compounds according to the present invention is suitable to be optionally coupled to an effector, for example, by means of click chemistry.

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28-11-2013 дата публикации

TETRAHYDROISOQUINOLINE DERIVATIVE

Номер: US20130317010A1
Принадлежит: Astellas Pharma Inc

To provide an excellent agent for preventing or treating dementia and schizophrenia based on serotonin 5-HTreceptor regulating action, it was found that a tetrahydroisoquinoline derivative characterized by a structure in which an acylguanidino group binds to a N atom of a tetrahydroisoquinoline ring or the like, and a cyclic group binds to an unsaturated ring has a potent 5-HTreceptor regulating action and an excellent pharmacological action based on the regulating action and also discovered that the tetrahydroisoquinoline derivative is useful as an agent for treating or preventing dementia, schizophrenia, and the like, whereby the present invention has been completed. 2. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '1', '2', '3', '4, 'wherein Rrepresents phenyl, pyridyl, or cycloalkyl which may be respectively substituted with group(s) selected from G, Rrepresents halogen, m represent 1, n represents 1, and both Rand Rrepresent H.'}3. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2', '3', '4, 'wherein Rrepresents phenyl which may be substituted with halogen or —O-(lower alkyl), Rrepresents H, F, Cl, or methyl, m represents 1, n represents 1, and both Rand Rrepresent H.'}4. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2', '3', '4, 'wherein Rrepresents pyridyl which may be substituted with halogen or —O-(lower alkyl), Rrepresents H, F, Cl, or methyl, m represents 1, n represents 1, and both Rand Rrepresent H.'}5. The compound according to or a pharmaceutically acceptable salt thereof claim 1 ,{'sup': 1', '2', '3', '4, 'wherein Rrepresents phenyl which may be substituted with halogen or —O-(lower alkyl), Rrepresents H, F, Cl, or methyl, m represents 1, n represents 1, and Rand Rform cyclopropane-1,1-diyl or cyclobutane-1,1-diyl together with the carbon atom binding thereto, as ethylene or trimethylene.'}6. A compound selected ...

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20-02-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140051724A1
Принадлежит: Vertex Pharmaceuticals Inc

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.

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27-03-2014 дата публикации

FLUORINATED ARYLALKYLAMINOCARBOXAMIDE DERIVATIVES

Номер: US20140088074A1
Автор: Pevarello Paolo
Принадлежит: NEWRON PHARMACEUTICALS S.P.A.

Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R, R, R, R, Rand Rhave the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role. 2. A compound of claim 1 , wherein:{'sub': 2', 'm', '1', '4', '3', '6, 'W is a group A-[(CH)—O]— wherein: m is zero, 1, 2 or 3; A is (C-C)alkyl optionally substituted by one to three fluorine atoms; (C-C)cycloalkyl; phenyl optionally substituted with a halo group; or thiazolyl'}{'sub': 1', '4, 'J independently is hydrogen; C-Calkyl; chloro; or fluoro;'} [{'sup': '1', 'sub': 1', '4', '1', '4', '3', '6, 'Ris hydrogen; (C-C)alkyl optionally substituted with a hydroxy group or a (C-C)alkoxy group; or (C-C)cycloalkyl;'}, {'sup': '2', 'sub': 1', '4, 'Ris hydrogen; or (C-C)alkyl;'}, {'sup': '2′', 'sub': 1', '4', '1', '4', '1', '4, 'R is hydrogen or (C-C)alkyl optionally substituted with a (C-C)alkoxy or a phenyl group, the phenyl group being optionally substituted with a (C-C)alkoxy group;'}, {'sup': '3', 'sub': 1', '4, 'Ris hydrogen; or (C-C)alkyl;'}, {'sup': '4', 'sub': 1', '4, 'Ris hydrogen; (C-C)alkyl; phenyl; or cyclohexyl; or'}], 'n is 1 or 2;'}{'sup': 3', '4, 'sub': 1', '2', '1', '4, 'claim-text': [{'sup': '5', 'Ris hydrogen or fluoro; and'}, {'sup': '6', 'Ris fluoro;'}], 'Rand R, taken together with the adjacent nitrogen atom, form an azetidinyl, pyrrolidinyl, morpholinyl, piperidinyl or piperazinyl, the piperydinyl ring being optionally substituted with one or two (C-C)alkyl group(s) and the piperazinyl ring being optionally substituted on the other N-atom with a (C-C)alkyl, ...

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10-04-2014 дата публикации

Guanidine compound

Номер: US20140100210A1
Принадлежит: Astellas Pharma Inc

[Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.

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03-01-2019 дата публикации

PHENYLOXADIAZOLE DERIVATIVES AS PGDS INHIBITORS

Номер: US20190000845A1
Принадлежит:

This invention is directed to a compound of formula (I): 224-. (canceled) The present invention is directed to phenyloxadiazole compounds, their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in the treatment of disease states capable of being modulated by the inhibition of the prostaglandin D synthase.Allergic rhinitis, the most common atopic disease, has an estimated prevalence ranging from about 5 to about 22 percent of the general human population and is characterized by the symptoms of sneezing, nasal discharge, and nasal congestion. These symptoms are believed to be triggered by multiple mediators released from mast cells and other inflammatory cells. Current therapies, such as antihistamines, deal effectively with the sneezing and nasal discharge, but have little effect on congestion, which is a key symptom affecting the quality of life of patients.Local allergen challenge in patients with allergic rhinitis, bronchial asthma, allergic conjunctivitis and atopic dermatitis has been shown to result in rapid elevation of prostaglandin D2 “(PGD2)” levels in nasal and bronchial lavage fluids, tears and skin chamber fluids. PGD2 has many inflammatory actions, such as increasing vascular permeability in the conjunctiva and skin, increasing nasal airway resistance, airway narrowing and cosinophil infiltration into the conjunctiva and trachea. PGD2 is the major cyclooxygenase product of arachidonic acid produced from mast cells on immunological challenge [Lewis, R A, Soter N A, Diamond P T, Austen K F, Oates J A, Roberts L J II, Prostaglandin D2 generation after activation of rat and human mast cells with anti-IgE, 129, 1627-1631, 1982]. Activated mast cells, a major source of PGD2, are one of the key players in driving the allergic response in conditions such as asthma, allergic rhinitis, allergic conjunctivitis, allergic dermatitis and other diseases [Brightling C E, Bradding P, Pavord I D, Wardlaw A J, New Insights ...

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17-01-2019 дата публикации

METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF

Номер: US20190016715A1
Принадлежит:

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions. 162.-. (canceled)65. The compound of claim 63 , or a pharmaceutically acceptable salt thereof claim 63 , wherein X is —O—.66. The compound of claim 63 , or a pharmaceutically acceptable salt thereof claim 63 , wherein Ris substituted or unsubstituted heteroaryl.67. The compound of claim 63 , or a pharmaceutically acceptable salt thereof claim 63 , wherein n is 1 and Ris halogen or —CH.68. The compound of claim 63 , or a pharmaceutically acceptable salt thereof claim 63 , wherein Ris —CF.69. The compound of claim 63 , or a pharmaceutically acceptable salt thereof claim 63 , wherein m is 0.71. A pharmaceutical composition comprising a compound of claim 63 , or a pharmaceutically acceptable salt claim 63 , and at least one pharmaceutically acceptable excipient.72. A method of treating a central nervous disorder (CNS) claim 63 , the method comprising the step of administering to a subject in need thereof claim 63 , an effective amount of a compound of claim 63 , thereby treating the disorder.75. The compound of claim 73 , or a pharmaceutically acceptable salt thereof claim 73 , wherein X is —O—.76. The compound of claim 73 , or a pharmaceutically acceptable salt thereof claim 73 , wherein Ris substituted or unsubstituted heteroaryl.77. The compound of claim 73 , or a pharmaceutically acceptable salt thereof claim 73 , wherein n is 1 and Ris halogen or —CH.78. The compound of claim 73 , or a pharmaceutically acceptable salt thereof claim 73 , wherein Ris —CF.79. The compound of claim 73 , or a pharmaceutically acceptable salt thereof claim 73 , wherein m is 0.81. A pharmaceutical composition comprising a compound of claim 73 , or a pharmaceutically acceptable salt claim 73 , and at least one pharmaceutically acceptable excipient.82. A method of treating ...

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23-01-2020 дата публикации

CAPSAZEPINE ANALOGS FOR THE TREATMENT OF CANCER AND OTHER PROLIFERATIVE DISEASES

Номер: US20200024276A1

The present disclosure relates generally to derivatives of capsazepine and methods of use thereof. In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. 2. The method of claim 1 , wherein Xis O.3. The method of claim 1 , wherein Xis S.4. The method according to claim 1 , wherein Ris —NRR claim 1 , wherein: Ris hydrogen claim 1 , alkyl claim 1 , substituted alkyl; and Ris aralkylor substituted aralkyl.512-. (canceled)1443-. (canceled)44. The method according to claim 1 , wherein Ris substituted aralkyl.4546-. (canceled)48. The method according to claim 1 , wherein the cancer is a carcinoma claim 1 , sarcoma claim 1 , lymphoma claim 1 , leukemia claim 1 , melanoma claim 1 , mesothelioma claim 1 , multiple myeloma claim 1 , or seminoma.49. The method according to claim 1 , wherein the cancer is of the bladder claim 1 , blood claim 1 , bone claim 1 , brain claim 1 , breast claim 1 , central nervous system claim 1 , cervix claim 1 , colon claim 1 , endometrium claim 1 , esophagus claim 1 , gall bladder claim 1 , gastrointestinal tract claim 1 , genitalia claim 1 , genitourinary tract claim 1 , head claim 1 , kidney claim 1 , larynx claim 1 , liver claim 1 , lung claim 1 , muscle tissue claim 1 , neck claim 1 , oral or nasal mucosa claim 1 , ovary claim 1 , pancreas claim 1 , prostate claim 1 , skin claim 1 , spleen claim 1 , small intestine claim 1 , large intestine claim 1 , stomach claim 1 , testicle claim 1 , or thyroid.5055-. (canceled)56. The method according to claim 1 , wherein the cancer is a solid tumor.57. The method according to claim 1 , wherein the method comprises injecting the compound directly into the tumor.58. (canceled)59. The method according to claim 1 , wherein the method comprises administering the compound systemically.60. (canceled)61. The method according to claim 1 , wherein the method further comprises alleviating pain.62. The method according to claim 1 , wherein ...

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02-02-2017 дата публикации

Substituted Aromatic Sulfur Compounds and Methods of Their Use

Номер: US20170029367A1
Принадлежит:

Compounds of formula II are described: 2. The compound of claim 1 , wherein A is at the 4-position of the phenyl ring.4. The compound of claim 1 , wherein Rand Rare each —CH.5. The compound of claim 3 , wherein Ris —OH.6. The compound of claim 3 , wherein Ris substituted or unsubstituted heterocycloalkyl.7. The compound of claim 3 , wherein Ris —NRR.8. The compound of claim 7 , wherein Ris H.9. The compound of claim 8 , wherein Ris substituted or unsubstituted alkyl.10. The compound of claim 8 , wherein Ris substituted or unsubstituted aryl.11. The compound of claim 8 , wherein Ris substituted or unsubstituted aralkyl.12. The compound of claim 8 , wherein Ris substituted or unsubstituted heteroaryl.13. The compound of claim 8 , wherein Ris substituted or unsubstituted heteroaralkyl.14. The compound of claim 8 , wherein Ris substituted or unsubstituted cycloalkyl.15. The compound of claim 8 , wherein Ris substituted or unsubstituted heterocycloalkyl.16. The compound of claim 8 , wherein Ris substituted or unsubstituted alkyene oxide.17. The compound of claim 8 , wherein Ris —NHCOcycloalkyl.18. The compound of claim 8 , wherein Rand R claim 8 , together with the atoms through which they are attached claim 8 , form a substituted or unsubstituted heterocycloalkyl ring.19. The compound of claim 3 , wherein Ris —CH.20. The compound of claim 19 , wherein Ris substituted or unsubstituted alkyl.21. The compound of claim 19 , wherein Ris substituted or unsubstituted aryl.22. The compound of claim 19 , wherein Ris substituted or unsubstituted aralkyl.23. The compound of claim 19 , wherein Ris substituted or unsubstituted heteroaryl.24. The compound of claim 19 , wherein Ris substituted or unsubstituted heteroaralkyl.25. The compound of claim 19 , wherein Ris substituted or unsubstituted cycloalkyl.26. The compound of claim 19 , wherein Ris substituted or unsubstituted heterocycloalkyl.27. The compound of claim 19 , wherein Ris substituted or unsubstituted alkyene oxide.28. The ...

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29-01-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150031722A1
Принадлежит: Vertex Pharmaceuticals Inc

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.

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04-02-2016 дата публикации

SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF

Номер: US20160031820A1
Принадлежит:

This invention provides compounds of formula (I): 3. The compound of claim 2 , wherein:{'sub': 1', '2, 'Vis —C(O)—, —C(O)—NH—, or —S(O)—;'}{'sub': '2', 'Vis —NH— or —O—;'}{'sup': '1', 'Ris chloro, fluoro, cyano, hydroxy, methoxy, ethoxy, trifluoromethoxy, trifluoromethyl, methyl, or ethyl;'}{'sup': '2', 'each occurrence of Ris independently fluoro, methyl, or trifluoromethyl;'}m is 0-1; andn is 0-2.5. The compound of claim 2 , wherein:{'sup': 3', '5', '5', '5a', '5d', '5d', '5d, 'sub': 3', '3', '3, 'Rwhen substituted is substituted with 1-4 independent occurrences of —R, wherein Ris —R, —R, -L-R, or —V-L-R;'}{'sup': 5a', '5b', '5b', '5c', '5c', '5c', '5b', '5b', '5b', '5b', '5b', '5e', '5b', '5e', '5c', '5e', '5b', '5e', '5b', '5e', '5b', '5dd', '5b', '5b', '5c', '5c', '5c', '5b', '5b', '5b', '5b', '5b', '5e', '5b', '5e', '5c', '5e', '5b', '5e', '5b', '5e', '5b, 'sub': 1-3', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '1-4', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2', '2, 'each occurrence of Ris independently halogen, Caliphatic, —CN, —NO, —N(R), —OR, —SR, —S(O)R, —S(O)R—C(O)R, —C(O)OR, —C(O)N(R), —S(O)N(R), —OC(O)N(R), —N(R)C(O)R, —N(R)SOR, —N(R)C(O)OR, —N(R)C(O)N(R), or —N(R)SON(R), or a Caliphatic substituted with R, halogen, —CN, —NO, —N(R), —OR, —SR, —S(O)R, —S(O)R—C(O)R, —C(O)OR, —C(O)N(R), —S(O)N(R), —OC(O)N(R), —N(R)C(O)R, —N(R)SOR, —N(R)C(O)OR, —N(R)C(O)N(R), or —N(R)SON(R);'}{'sup': 5b', '5b, 'sub': '1-6', 'each occurrence of Ris independently hydrogen or an optionally substituted group selected from Caliphatic, 3-10-membered cycloaliphatic, 4-10-membered heterocyclyl having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur, 6-10-membered aryl, or 5-10-membered heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur; or two occurrences of Ron the same nitrogen atom can be taken together with the nitrogen atom to which they are bound to form an optionally substituted 4-7-membered ...

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11-02-2016 дата публикации

INHIBITORS OF MICROSOMAL TRIGLYCERIDE TRANSFER PROTEIN AND APO-B SECRETION

Номер: US20160039765A1
Принадлежит:

The present invention relates to compounds which are inhibitors of microsomal triglyceride transfer protein and/or apolipoprotein B (Apo B) secretion. These compounds can be useful for the prevention and treatment of various diseases, particularly atherosclerosis and its clinical sequelae, for lowering serum lipids, and related ailments. The invention further relates to pharmaceutical compositions comprising the compounds and to methods of treating diseases, such as hypertriglyceridemia, hyperchylomicronemia, atherosclerosis, obesity, and related conditions using the compounds. A method for decreasing apolipoprotein B (apo B) secretion is also provided. 2. The compound of claim 1 , wherein Xis O.3. The compound of claim 1 , wherein Ris alkyl.4. The compound of claim 3 , wherein Ris methyl.6. The compound of claim 1 , wherein Rand Xtaken together form CH—O—.7. The compound of claim 11 , wherein Ris unsubstituted or substituted phenyl.10. The compound of claim 9 , wherein Ris —OCH.11. The compound of claim 9 , wherein Ris not H.12. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.13. The pharmaceutical composition of further comprising an additional lipid-lowering agent.14. A method of treating or preventing a condition selected from the group consisting of atherosclerosis claim 1 , pancreatitis claim 1 , obesity claim 1 , hypercholesteremia claim 1 , hypertriglyceridemia claim 1 , hyperlipidemia claim 1 , and diabetes claim 1 , comprising administering to a mammal in need of such treatment an effective amount of a compound of claim 1 , such that the condition is treated or prevented.15. The method of claim 14 , wherein said condition is selected from atherosclerosis claim 14 , pancreatitis claim 14 , obesity claim 14 , and diabetes.16. The method as defined in claim 14 , wherein said condition is atherosclerosis.17. A method of decreasing apo-B secretion in a mammal claim 1 , comprising administering to said mammal an ...

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12-02-2015 дата публикации

Hydroxybenzamide Derivatives And Their Use As Inhibitors Of HSP90

Номер: US20150045362A1
Принадлежит: ASTEX THERAPEUTICS LTD

The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; optionally substituted C 1-5 hydrocarbyl and optionally substituted C 1-5 hydrocarbyloxy; R 4 is selected from hydrogen; a group —(O) n —R 7 where n is 0 or 1 and R 7 is an optionally substituted acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C 1-5 hydrocarbyl-amino; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR 5 R 6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.

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16-02-2017 дата публикации

Compounds for preparing pyrrole six-membered heteroaryl ring derivative

Номер: US20170044171A1

Intermediate compounds used in the preparation of pyrrole six-membered heteroaryl ring derivatives are disclosed. In particular, compounds of formula (IB) are disclosed. The compounds of formula (IB) are used in the synthesis of Janus kinase (JAK) inhibitors. Substituents in formula (IB) have the same definitions as in the description.

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25-02-2016 дата публикации

3-AMIDOBENZAMIDES AND USES THEREOF FOR INCREASING CELLULAR LEVELS OF A3G AND OTHER A3 FAMILY MEMBERS

Номер: US20160052870A1
Принадлежит: Northwestern University

Disclosed are novel benzamide compounds and the uses thereof for treating diseases and disorders in a patient in need thereof by increasing cellular levels of A3G and/or other members of the A3 family of proteins in the patient. The disclosed compounds include -benzamide compounds that may be administered to treat an HIV-1 infection or cancer in a patient. 2. The compound of claim 1 , wherein n is 0.3. The compound of claim 1 , wherein X is C.4. The compound of claim 1 , wherein Ris methoxy.6. The compound of claim 5 , wherein Ris C1-C6-alkoxy.7. The compound of claim 5 , wherein Ris H claim 5 , C1-C6-alkyl optionally substituted with C1-C6-alkoxy claim 5 , hydroxyl claim 5 , C1-C6-alkylamino claim 5 , C1-C6 dialkylamino claim 5 , phenyl claim 5 , benzyl claim 5 , benzo[1 claim 5 ,3]diox8yl claim 5 , pyridin-2-yl claim 5 , pyridin-3-yl claim 5 , pyridin-4-yl claim 5 , C3-C6-cycloalkyl optionally substituted with methyl claim 5 , C1-C6-alkoxy claim 5 , N-piperidinyl claim 5 , and tetrahydrofuran-2-yl.8. The compound of claim 5 , wherein R claim 5 , R claim 5 , R claim 5 , R claim 5 , and Rare independently selected from H claim 5 , C1-C6-alkoxy claim 5 , and halo.9. The compound of claim 5 , wherein one or more of R claim 5 , R claim 5 , are Rare methoxy.10. The compound of claim 9 , wherein one or more of Rand Rare chloro.12. A pharmaceutical composition comprising the compound of and a pharmaceutical carrier.13. The pharmaceutical composition of comprising an effective amount of the compound for increasing levels of A3G and/or other members of the A3 family of proteins after the composition is administereing to a patient in need thereof.14. A method for treating HIV-1 infection in a patient in need thereof claim 13 , the method comprising administering the pharmaceutical composition of to the patient.15. A method for treating cancer in a patient in need thereof claim 13 , the method comprising administering the pharmaceutical composition of to the patient. The ...

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13-02-2020 дата публикации

T1r hetero-oligomeric taste receptors, cell lines that express said receptors, and taste compounds

Номер: US20200049699A1
Принадлежит: Firmenich Inc

The invention relates to compounds that specifically bind a T1R1/T1R3 or T1R2/T1R3 receptor or fragments or sub-units thereof. The present invention also relates to the use of hetero-oligomeric and chimeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions. The use of these cells lines in cell-based assays to identify umami and sweet taste modulatory compounds is also provided, particularly high throughput screening assays that detect receptor activity by use of fluorometric imaging.

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05-03-2015 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20150065487A1
Принадлежит: Vertex Pharmaceuticals Inc

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.

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05-06-2014 дата публикации

Modulators of atp-binding cassette transporters

Номер: US20140155431A1
Принадлежит: Vertex Pharmaceuticals Inc

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.

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21-04-2016 дата публикации

CXCR7 RECEPTOR MODULATORS

Номер: US20160107997A1
Принадлежит:

The present invention relates to derivatives of formula (I) 5. The compound of formula (I) according to claim 1 , wherein (R)represents one optional substituent independently selected from (C)alkyl claim 1 , (C)alkoxy claim 1 , halogen claim 1 , (C)fluoroalkyl claim 1 , (C)fluoroalkoxy claim 1 , or cyano;or a pharmaceutically acceptable salt thereof.6. The compound of formula (I) according to claim 1 , wherein Lrepresents a two-membered linker group selected from —NH—CH—* claim 1 , —O—CH—* claim 1 , —CHCH— claim 1 , or —CH═CH—; wherein the asterisks indicate the bond with which the group Lis attached to the carbonyl group;or a pharmaceutically acceptable salt thereof.7. The compound of formula (I) according to claim 1 , wherein Lrepresents —CH—; or a pharmaceutically acceptable salt thereof.9. The compound of formula (I) according to claim 1 , wherein Rrepresents{'sub': '2-5', '(C)alkyl which is mono-substituted with hydroxy; or disubstituted wherein the substituents are independently methoxy or hydroxy;'}{'sub': 2-4', '1-4', '1-4', '2-3', '3-6', '3-6', '1-3', '3-6', '1-3, 'sup': 6', '7', '6', '7, '—(C)alkylene-NRR, wherein Rrepresents hydrogen or (C)alkyl; and Rrepresents (C)alkyl; (C)fluoroalkyl; (C)cycloalkyl; or (C)cycloalkyl-(C)alkyl; (C)cycloalkyl-(C)alkyl, wherein the cycloalkyl group is optionally mono-substituted with hydroxy;'}{'sub': 4-7', '4-7', '1-3', '4-7', '4-7, 'claim-text': one oxo substituent attached to a ring carbon atom in alpha position to a ring nitrogen; and/or', {'sub': '1-4', '(C)alkyl attached to a ring nitrogen atom having a free valency; or'}, 'two fluoro substituents attached to a ring carbon atom;, '(C)heterocyclyl or (C)heterocyclyl-(C)alkyl, wherein in the above groups the (C)heterocyclyl independently has one or two ring heteroatoms independently selected from nitrogen or oxygen; wherein in the above groups said (C)heterocyclyl independently is unsubstituted, or mono-, or di-substituted wherein the substituents are independently ...

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29-04-2021 дата публикации

GPR183 ANTAGONISTS FOR THE TREATMENT OF PAIN

Номер: US20210122750A1
Принадлежит:

Disclosed herein are compositions and methods for treating neuropathic pain in a subject in need thereof. Compositions disclosed herein are GPR183 antagonists. The methods include administering to a subject in need thereof a therapeutically effective amount of a GPR183 antagonist. 2. The compound of claim 1 , wherein L is a substituted or unsubstituted nitrogen containing ring system comprising one or two optionally aromatic rings and one or more carbonyl groups.5. The compound of claim 4 , wherein p is 1 and ring B is aryl or heteroaryl.6. The compound of claim 4 , wherein Rand Rtogether with the atoms they are attached to form a carbonyl group.8. The compound of claim 1 , wherein L is a substituted or unsubstituted nitrogen containing ring system comprising one or two optionally aromatic rings and one or more alkoxy substituents.10. The compound of claim 9 , wherein p is 1 such that ring C is a 6 membered ring.11. The compound of claim 9 , wherein at least one of R claim 9 , R claim 9 , R claim 9 , and Ris alkoxy or —OH.13. The compound of claim 12 , wherein at least one of R claim 12 , R claim 12 , R claim 12 , R claim 12 , and Ris halo.15. A method for treating pain in a subject in need thereof claim 12 , the method comprising: administering to the subject in need thereof a therapeutically effective amount of a GPR183 antagonist.16. The method of claim 15 , wherein the GPR183 antagonist comprises a compound Formula (XVII) and pharmaceutically acceptable salts thereof.18. The method of claim 15 , wherein the pain is at least one of chemotherapy-induced neuropathy claim 15 , diabetic neuropathy claim 15 , cancer pain claim 15 , autoimmune neuropathy claim 15 , and traumatic neuropathy.19. The method of claim 17 , wherein the GPR183 antagonist is administered orally claim 17 , intravenously claim 17 , intrathecalyl claim 17 , sublingually claim 17 , transdermally claim 17 , subcutaneously claim 17 , topically claim 17 , intranasally claim 17 , intraarterially claim ...

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09-06-2022 дата публикации

SUMO INHIBITOR COMPOUNDS AND USES THEREOF

Номер: US20220177488A1
Принадлежит:

The present invention relates to compounds and compositions capable of acting as inhibitors of small ubiquitin-like modifier (SUMO) family of proteins. The compounds and compositions may be used in the treatment of cancer. There are disclosed, inter alia, methods of inhibiting an E1 enzyme, and compounds useful for inhibiting an E1 enzyme. 2. The compound of wherein ring A is selected from dihydropyran claim 1 , dihydrothienyl claim 1 , dihydrofuryl claim 1 , oxo-dihydrofuryl claim 1 , pyrrolinyl claim 1 , dihydrothiazolyl claim 1 , dihydro-oxazolyl claim 1 , dihydro-isothiazolyl claim 1 , dihydro-isoxazolyl claim 1 , midazolinyl and pyrazolinyl claim 1 , wherein ring A is optionally substituted with one or more substituent groups.3. The compound of wherein ring A is selected from thienyl claim 1 , furanyl claim 1 , pyrrolyl claim 1 , thiazolyl claim 1 , oxazolyl claim 1 , midazolyl claim 1 , pyrazolyl claim 1 , isoxazolyl claim 1 , triazolyl and isothiazolyl claim 1 , wherein ring A is optionally substituted with one or more substituent groups.6. The compound of wherein ring A is selected from phenyl claim 1 , pyridyl claim 1 , pyrazinyl claim 1 , pyrimidinyl claim 1 , pyridazinyl claim 1 , and triazinyl claim 1 , wherein ring A is optionally substituted with one or more substituent groups.8. The compound of wherein ring A is selected from phenyl or thienyl claim 1 , wherein ring A is optionally substituted with one or more substituent groups.9. The compound of any one of - wherein Ris selected from substituted or unsubstituted phenyl claim 1 , substituted or unsubstituted cycloalkyl and substituted or unsubstituted 5- or 6-membered heteroaryl.10. The compound of any one of - wherein Ris selected from substituted or unsubstituted phenyl claim 1 , substituted or unsubstituted cyclopentyl claim 1 , substituted or unsubstituted cyclohexyl and substituted or unsubstituted pyridyl.11. The compound of any one of - wherein E is selected from —C(═O)CH═CH claim 1 , —C(═O)- ...

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18-04-2019 дата публикации

2-PHENETHENYLTETRAHYDRO ISOQUINOLINES USEFUL AS ANTI-HIV COMPOUNDS

Номер: US20190111044A1
Принадлежит:

This invention provides, among other things, tetrahydroisoquinolines useful for treating viral infections, pharmaceutical formulations containing such compounds, as well as methods of inhibiting the replication of a virus, such as HIV, or treating a disease, such as AIDS. 6. A pharmaceutical formulation comprising:a) a compound of a preceding claim, or a pharmaceutically acceptable salt thereof; andb) a pharmaceutically acceptable excipient.7. A method of inhibiting the replication of a virus in an animal , comprising:a) administering a compound or a pharmaceutical formulation of a preceding claim to the animal, wherein the animal is in need of treatment thereof thereby inhibiting the replication of the virus in an animal.8. The method of claim 7 , wherein the virus is a member of the Orthoretroviridae family.9. The method of claim 7 , wherein the virus is HIV.10. A method of treating a disease in an animal claim 7 , comprising:a) administering a compound or a pharmaceutical formulation of a preceding claim to the animal, wherein the animal is in need of treatment thereof thereby treating the disease in the animal.11. The method of claim 10 , wherein the disease is AIDS.12. The method of claim 7 , wherein the animal is a human.13. A method of treating an HIV infection in a human claim 1 , the method comprising administering to said human a therapeutically effective amount of a compound according to . This application is a continuation of U.S. patent application Ser. No. 15/536,104 filed Jun. 14, 2017, which claims National Stage of International Patent Application No. PCT/US2015/065893 filed Dec. 15, 2015 and published as WO 2016/100391 A1, which claims priority to U.S. Provisional Application No. 62/092,115 filed Dec. 15, 2014, the entire contents of which applications is incorporated herein for all purposes by this reference.There is a need in the art to discover new compounds useful as antivirals.It has now been discovered that certain tetrahydroisoquinolines are ...

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21-05-2015 дата публикации

COMPOSITIONS AND METHODS FOR TREATMENT

Номер: US20150140076A1
Автор: Burnier John, Gadek Thomas
Принадлежит: SARcode Bioscience Inc.

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists. 1101.-. (canceled)103. A method as defined in wherein said integrin comprises LFA-1 and said intercellular adhesion molecule is selected from the group consisting of ICAM-1 claim 102 , ICAM-2 claim 102 , ICAM-3 claim 102 , ICAM-4 or any combination of any of the foregoing.104. A method as defined in claim 102 , wherein the patient does not have Sjogren's syndrome.105. A method as defined in claim 102 , wherein the patient has Sjogren's syndrome.106. A method as defined in claim 102 , wherein said administration comprises topical administration of said compound via a carrier vehicle selected from a group consisting of liquid drops claim 102 , liquid wash claim 102 , gel claim 102 , ointment claim 102 , spray claim 102 , liposome claim 102 , and any combination of any of the foregoing.107. A method as defined in claim 106 , wherein said topical administration comprises infusion of said compound or salt to an eye of said patient via a device selected from the group consisting of a pump-catheter system claim 106 , a continuous or selective release device claim 106 , a contact lens claim 106 , or any combination of any of the foregoing.108. A method as defined in claim 102 , wherein said administration comprises systemically administering a liquid or liquid suspension of said compound or salt via nose drops claim 102 , nasal spray claim 102 , nebulized liquid claim 102 , or any combination of any of ...

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03-06-2021 дата публикации

OPIOID RECEPTOR MODULATORS AND PRODUCTS AND METHODS RELATED THERETO

Номер: US20210163402A1
Принадлежит:

Compounds are provided having the structure of Formula (I): 1100-. (canceled)102. The compound of claim 101 , or a pharmaceutically acceptable isomer claim 101 , racemate claim 101 , hydrate claim 101 , solvate claim 101 , isotope claim 101 , or salt thereof claim 101 , wherein:ring A is phenyl, pyridinyl, or pyrazinyl;{'sub': 3', '7, 'sup': '7', 'ring C is a C-Ccycloalkyl or 3-7 membered heterocycloalkyl, substituted with 0-5 R;'}{'sup': 1', '2, 'Rand Rare each, independently, H, methyl, ethyl, isopropyl or cyclopropyl, substituted with 0-3 halo;'}{'sup': 3', '4, 'sub': 1', '6', '1', '6, 'Rand Rare each, independently, H, (C-C)alkyl, (C-C)haloalkyl, or cyclopropylmethyl;'}{'sup': 5', '1', '2', '3', '5, 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently —C(O)NRR, —OH, halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle; or Rand one R, together with the atoms to which they are connected, form a 5-7 membered heterocycle;'}{'sup': '6', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '7', 'sub': 1', '6', '1', '6', '1', '6, 'each Ris independently halo, (C-C)alkyl, (C-C)haloalkyl, (C-C)alkoxy, or carbocycle;'}{'sup': '8', 'Ris H;'}m is 1-3; andn is 0-3.103. The compound of claim 102 , or a pharmaceutically acceptable isomer claim 102 , racemate claim 102 , hydrate claim 102 , solvate claim 102 , isotope claim 102 , or salt thereof claim 102 , wherein ring A is phenyl.104. The compound of claim 103 , or a pharmaceutically acceptable isomer claim 103 , racemate claim 103 , hydrate claim 103 , solvate claim 103 , isotope claim 103 , or salt thereof claim 103 , wherein ring B is phenyl claim 103 , indazolyl claim 103 , 2 claim 103 ,3-dihydrobenzoxazolyl claim 103 , benzoxazolonyl claim 103 , or pyrazolopyridinyl.105. The compound of claim 104 , or a pharmaceutically acceptable isomer claim 104 , racemate claim 104 , hydrate claim 104 , solvate claim 104 , isotope claim 104 , or ...

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09-05-2019 дата публикации

MODULATORS OF CELLULAR ADHESION

Номер: US20190134022A1
Принадлежит: SARcode Bioscience Inc.

The present invention provides compounds having formula (I): 175-. (canceled)79. The method of claim 76 , wherein the compound is present in an amount effective to modulate adhesion between intracellular adhesion molecules and the leukocyte integrin family of receptors.80. The method of claim 76 , wherein the compound is present in an amount effective to antagonize CD11/CD18 receptors associated with leukocytes.81. The method of claim 76 , wherein the LFA-1 antagonist is a sodium claim 76 , potassium claim 76 , lithium claim 76 , magnesium claim 76 , or calcium salt.82. The method of claim 76 , wherein the formulation is in the form of an ointment claim 76 , paste claim 76 , cream claim 76 , lotion claim 76 , gel claim 76 , powder claim 76 , solution claim 76 , spray claim 76 , inhalant claim 76 , patch claim 76 , suspension claim 76 , emulsion claim 76 , crystalline form claim 76 , oil claim 76 , plaster claim 76 , liposome claim 76 , microemulsion claim 76 , or buffered solution.83. The method of claim 76 , wherein the excipient is selected from the group consisting of alcohols claim 76 , quaternary amines claim 76 , organic acids claim 76 , parabens claim 76 , phenols claim 76 , ascorbic acid claim 76 , ascorbic acid esters claim 76 , sodium bisulfite claim 76 , butylated hydroxytoluene claim 76 , butylated hydroxyanisole claim 76 , tocopherols claim 76 , chelating agents claim 76 , glycerine claim 76 , sorbitol claim 76 , polyethylene glycols claim 76 , urea claim 76 , propylene glycol claim 76 , citric buffer claim 76 , hydrochloric buffer claim 76 , lactic acid buffer claim 76 , quaternary ammonium chlorides claim 76 , cyclodextrins claim 76 , benzyl benzoate claim 76 , lecithin claim 76 , polysorbates claim 76 , vitamin E oil claim 76 , allatoin claim 76 , dimethicone claim 76 , glycerin claim 76 , petrolatum claim 76 , zinc oxide claim 76 , and combinations thereof.84. The method of claim 76 , further comprising a topical penetration enhancer.85. The method ...

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25-05-2017 дата публикации

Compositions and methods for treatment

Номер: US20170143692A1
Автор: John Burnier, Thomas Gadek
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

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25-05-2017 дата публикации

Compositions and methods for treatment

Номер: US20170143693A1
Автор: John Burnier, Thomas Gadek
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

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16-05-2019 дата публикации

PROCESS FOR PRODUCING ORGANIC COMPOUND

Номер: US20190144404A1
Принадлежит: KANEKA CORPORATION

The present disclosure provides a reaction of a chlorine-containing compound using a flow reactor which is less restricted by a solvent to be used. In the present disclosure, an organic compound is produced by supplying a reaction substrate having at least one functional group which can react with chlorine and is selected from the group consisting of hydroxy group, a thiol group, an amino group, a carboxyl group, a thiocarboxyl group, and an acid amide group, and a chlorine-containing compound to a flow reactor together with a trialkyl amine having 9 to 40 carbon atoms and an organic solvent, and allowing the reaction substrate and the chlorine-containing compound to react with each other. 2: The process according to claim 1 , whereinthe flow reactor has two or more raw material feeding ports, a mixing unit configured to mix a raw material fed from the feeding ports, and a reactor unit configured to flow a mixed solution therein, anda first organic solvent solution comprising the reaction substrate and the trialkyl amine dissolved therein, and a second organic solvent solution comprising the chlorine-containing compound dissolved therein, are fed to the reactor unit from different raw material feeding ports.3: The process according to claim 1 , wherein the organic solvent is at least one selected from the group consisting of an aliphatic hydrocarbon solvent claim 1 , an aromatic hydrocarbon solvent claim 1 , an ether solvent claim 1 , an ester solvent claim 1 , a ketone solvent claim 1 , a nitrile solvent claim 1 , and an amide solvent.4: The process according to claim 1 , wherein the trialkyl amine and the organic solvent are supplied to the flow reactor such that an amount of the trialkyl amine is 3 parts by weight or more with respect to 100 parts by weight of the organic solvent.5: The process according to claim 1 , wherein the trialkyl amine is tripropylamine claim 1 , tributylamine claim 1 , trihexylamine claim 1 , or trioctylamine.7: The process according to ...

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16-05-2019 дата публикации

MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS

Номер: US20190144450A1
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.

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13-08-2015 дата публикации

PROCESS FOR PREPARING (1S)-1-PHENYL-3,4-DIHYDRO-2(1H)-ISOQUINOLINE-CARBOXYLATE

Номер: US20150225348A1
Автор: Huang Yue, Zheng Fei
Принадлежит:

A process for preparation of (1S)-1-phenyl-3,4-dihydro-2(1H)-isoquinoline-carboxylate (Formula I), comprising reacting (1S)-1-phenyl-3,4-dihydro-2(1H)isoquinoline (Formula II) with carbon dioxide and an alkylating agent R-LG in the presence of a base to obtain the compound of Formula I in an organic solvent. 2. The process according to claim 1 , wherein R is an alkyl or a substituted alkyl claim 1 , LG is a leaving group.3. The process according to claim 1 , wherein R is a C-Calkyl group.4. The process according to claim 1 , wherein LG is a chloro- claim 1 , bromo- claim 1 , or Iodo-leaving group.5. The process according to claim 1 , wherein a ratio of the alkylating agent R-LG to the compound of formula II is (1.0-5.0):1.6. The process according to claim 2 , wherein a ratio of the alkylating agent R-LG to the compound of formula II is (1.0-5.0):1.7. The process according to claim 1 , wherein the carbon dioxide is in gas or solid phase claim 1 , and a pressure of the carbon dioxide is equal to or less than 1.0 Mpa.8. The process according to claim 1 , wherein the base is an inorganic carboxylate claim 1 , 1 claim 1 ,8-Diazabicyclo[5.4.0]undec-7-ene (DBU) claim 1 , or a mixture thereof.9. The process according to claim 1 , wherein the base is lithium carbonate claim 1 , sodium carbonate claim 1 , potassium carbonate claim 1 , cesium carbonate claim 1 , or a mixture thereof.10. The process according to claim 1 , wherein a ratio of the base to the compound of formula II is (1.0-10.0):1.11. The process according to claim 10 , wherein the ratio of the base to the compound of formula II is (2.0-7.0):1.12. The process according to claim 1 , wherein the organic solvent is an aprotic polar solvent.13. The process according to claim 1 , wherein the organic solvent is N claim 1 ,N dimethyl formamide claim 1 , acetonitrile claim 1 , tetrahedronfuran claim 1 , dioxane claim 1 , or a mixture thereof.14. The process according to claim 1 , wherein reaction temperature is 0-50° C.15 ...

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11-07-2019 дата публикации

Azadecalin derivatives as inhibitors of human immunodeficiency virus replication

Номер: US20190209550A1

Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, azadecaline derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: These compounds are useful for the treatment of HIV and AIDS.

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02-07-2020 дата публикации

PROCESS FOR PRODUCING ORGANIC COMPOUND

Номер: US20200207717A1
Принадлежит: KANEKA CORPORATION

A process for producing an organic compound using a flow reactor for a first reaction in which a raw material liquid A and a raw material liquid B are mixed, and reacted in a reactor unit, and a flow reactor for a second reaction in which a first reaction solution discharged from the flow reactor for the first reaction and a raw material liquid C are mixed, and reacted in a reactor unit, wherein the raw material liquid A is a solution in which triphosgene and/or diphosgene is dissolved, wherein the raw material liquid B is a nitrogen-containing organic compound or a solution thereof, wherein the raw material liquid C is a reaction substrate having a functional group capable of reacting with phosgene, or a solution containing the reaction substrate, and wherein a product of the first reaction is phosgene. 1. A process for producing an organic compound using an apparatus comprising:a first flow reactor for a first reaction in which a raw material liquid A and a raw material liquid B are introduced from separate feeding channels, mixed in a first mixing unit, and then reacted in a first reactor unit, anda second flow reactor for a second reaction in which a first reaction solution discharged from the first flow reactor for the first reaction and a raw material liquid C are introduced from separate feeding channels, mixed in a second mixing unit, and then reacted in a second reactor unit,wherein the raw material liquid A is a solution in which triphosgene and/or diphosgene is dissolved,wherein the raw material liquid B is a nitrogen-containing organic compound not including an amino group, an amino group comprising one substituent on N, an amido group, an amido group comprising one substituent on N, a —C(═O )NH2, and a —OC(═O)NH2 comprising one substituent on N, or a solution of the nitrogen-containing organic compound,wherein the raw material liquid C is a reaction substrate having at least one functional group capable of reacting with phosgene, the functional group ...

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09-08-2018 дата публикации

PYRROLE HETEROARYL RING DERIVATIVE AND METHOD OF USE THEREOF

Номер: US20180222912A1
Принадлежит:

A pyrrole six-membered heteroaryl ring derivative, and the medicinal uses thereof are described. Specifically, the pyrrole six-membered heteroaryl ring derivative is a compound of formula (I), wherein the variable groups are as described in the specification. 3. A method for the treatment of a disease or disorder claim 2 , comprising administering to a subject in need thereof the pharmaceutical composition according to claim 2 , wherein the disease or disorder is selected form the group consisting of allograft rejection; graft versus host disease; atopic dermatitis; rheumatoid arthritis; psoriasis; lymphoma; leukemia; pancreatic cancer; breast cancer; cutaneous T-cell lymphoma; and cutaneous B-cell lymphoma.7. The process according to claim 5 , wherein the alkaline condition of step (i) is provided by an organic base or an inorganic base.8. The process according to claim 7 , wherein the organic base is selected from the group consisting of triethylamine claim 7 , N claim 7 , N-diisopropylethylamine claim 7 , n-butyllithium claim 7 , tert-butyl potassium alkoxide claim 7 , and tetrabutylammonium bromide; and the inorganic base is selected from the group consisting of sodium hydride claim 7 , sodium carbonate claim 7 , sodium bicarbonate claim 7 , potassium carbonate claim 7 , potassium bicarbonate and cesium carbonate.9. The process according to claim 8 , wherein the alkaline condition of step (i) is provided by the organic base of triethylamine.10. The process according to claim 5 , wherein the t-butoxycarbonyl group of compound 5 is removed in step (ii) in the presence of hydrogen chloride.14. The process according to claim 12 , wherein the alkaline condition is provided by an organic base or an inorganic base.15. The process according to claim 14 , wherein the organic base is selected from the group consisting of triethylamine claim 14 , N claim 14 , N-diisopropylethylamine claim 14 , n-butyllithium claim 14 , tert-butyl potassium alkoxide claim 14 , and ...

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26-08-2021 дата публикации

Fgfr inhibitor, preparation method therefor and application thereof

Номер: US20210261544A1
Принадлежит: Abbisko Therapeutics Co Ltd

A compound having a structure of formula (I) and a preparation method therefor, and a use of the compound serving as an FGFR inhibitor for treating tumors, cancers, myeloproliferative diseases, bone or chondrocyte disorders, and hypophosphatemia.

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16-07-2020 дата публикации

NOVEL FLAVORS, FLAVOR MODIFIERS, TASTANTS, TASTE ENHANCERS, UMAMI OR SWEET TASTANTS, AND/OR ENHANCERS AND USE THEREOF

Номер: US20200225217A1
Принадлежит:

The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions. 1322-. (canceled)324. The method of claim 323 , wherein Ris a phenyl group claim 323 , which comprises a substituent selected independently from the group consisting of hydroxy claim 323 , fluoro claim 323 , chloro claim 323 , NH claim 323 , NHCH claim 323 , N(CH) claim 323 , COCH claim 323 , SCH claim 323 , SCHCH claim 323 , methyl claim 323 , ethyl claim 323 , isopropyl claim 323 , vinyl claim 323 , trifluoromethyl claim 323 , methoxy claim 323 , ethoxy claim 323 , isopropoxy claim 323 , and trifluoromethoxy.325. The method of claim 324 , wherein Ris a phenyl group claim 324 , which comprises two substituents selected independently from the group consisting of hydroxy claim 324 , fluoro claim 324 , chloro claim 324 , NH claim 324 , NHCH claim 324 , N(CH) claim 324 , COCH claim 324 , SCH claim 324 , SCHCH claim 324 , methyl claim 324 , ethyl claim 324 , isopropyl claim 324 , vinyl claim 324 , trifluoromethyl claim 324 , methoxy claim 324 , ethoxy claim 324 , isopropoxy claim 324 , and trifluoromethoxy.326. The method of claim 325 , wherein Ris a phenyl group claim 325 , which comprises three substituents selected independently from the group consisting of hydroxy claim 325 , fluoro claim 325 , chloro claim 325 , NH claim 325 , NHCH claim 325 , N(CH) claim 325 , COCH claim 325 , SCH claim 325 , SCHCH claim 325 , methyl claim 325 , ethyl claim 325 , isopropyl claim 325 , vinyl claim 325 , trifluoromethyl claim 325 , ...

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10-09-2015 дата публикации

Heterocyclyl Derivatives and their use as Prostaglandin D2 Receptor Modulators

Номер: US20150252036A1
Принадлежит:

The present invention relates to phenyl-substituted heterocyclyl derivatives of the formula (I), 2. The compound according to claim 1 , wherein{'sup': '1', 'Rrepresents hydrogen or halogen;'}{'sup': '2', 'Rrepresents hydrogen or halogen;'}{'sup': 3', '4', '5, 'sub': 1', '3', '1', '3, 'one of R, Rand Rrepresents carboxy-(C-C)alkyl or carboxy-(C-C)alkoxy and the other two represent hydrogen;'}{'sup': '6', 'Rrepresents hydrogen, methoxy or halogen;'}{'sup': '7', 'sub': 1', '4, 'Rrepresents hydrogen, (C-C)alkoxy, trifluoromethyl, trifluoromethoxy, halogen or methylsulfonyl;'}{'sup': '8', 'claim-text': [{'sub': 1', '4', '1', '2, '(C-C)alkyl which is mono-substituted with optionally substituted aryl, optionally substituted heteroaryl or optionally substituted aryl-(C-C)alkoxy; or'}, 'cyclopropyl which is mono-substituted with optionally substituted aryl;, 'Rrepresents'}n represents 1 or 2;m represents 1 or 2; andZ represents —NH—, —O— or a bond;or a salt thereof.3. The compound according to claim 1 , wherein{'sup': '1', 'Rrepresents fluoro;'}{'sup': 2', '3', '4', '6, 'R, R, Rand Rrepresent hydrogen;'}{'sup': '5', 'Rrepresents carboxy-methyl or 1-carboxy-ethyl;'}{'sup': '7', 'Rrepresents methoxy, ethoxy, isopropoxy or 2,2,2-trifluoroethoxy;'}{'sup': '8', 'claim-text': phenyl, wherein the phenyl is unsubstituted, mono-substituted with fluoro, chloro, methyl or methoxy, di-substituted with fluoro, or di-substituted with fluoro and chloro; or', 'pyridin-2-yl, wherein the pyridin-2-yl is unsubstituted, mono-substituted with methyl, or di-substituted with methyl and fluoro;, 'Rrepresents a methyl, ethyl or n-propyl group, which groups are independently mono-substituted with'}n represents 1;m represents 2; andZ represents —O— or a bond;or a salt thereof.4. The compound according to claim 1 , wherein{'sup': '1', 'Rrepresents fluoro, chloro or cyano;'}{'sup': 2', '3', '5', '6, 'R, R, Rand Rrepresent hydrogen;'}{'sup': '4', 'Rrepresents carboxy-methyl or 1-carboxy-ethyl;'}{'sup': ' ...

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24-09-2015 дата публикации

Compositions and methods for the treatment of disease associated with trp-p8 expression

Номер: US20150266810A1
Принадлежит: Dendreon Pharmaceuticals Llc

Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Tip-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Tip-p8 expression.

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07-10-2021 дата публикации

Compounds affecting pigment production and methods for treatment of bacterial diseases

Номер: US20210309622A1
Принадлежит: Versitech Ltd

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II):The present methods include administering to a subject an effective amount of one or more compounds of Formula (II). In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.

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28-10-2021 дата публикации

PHENYLOXADIAZOLE DERIVATIVES AS PGDS INHIBITORS

Номер: US20210330671A1
Принадлежит:

This invention is directed to a compound of formula (1): 2. The compound of wherein R1 is hydrogen claim 1 , R2 is hydrogen and R3 is hydroxy alkyl.3. The compound of which is 2-Pyridin-2-yl-pyrimidine-5-carboxylic acid 3-5-(1-hydroxy-1 methyl-ethyl)[1 claim 2 ,2 claim 2 ,4]oxadiazol-3-yl]benzyl amide;4. The compound of where R1 is C-Calkyl claim 1 , R2 is hydrogen and R3 is hydroxyalkyl.5. The compound of selected from the group consisting of 2-pyridin-2-yl-pyrimidine-5-carboxylic acid ((S)-1-{3-[5-(1-hydroxy-1-methyl-ethyl)-1 claim 4 ,2 claim 4 ,4-oxadiazol-3-yl]-phenyl}-ethyl)-amide and 2-pyridin-2-yl-pyrimidine-5-carboxylic acid ((R)-1-{3-[5-(1-hydroxy-1-methyl-ethyl)-1 claim 4 ,2 claim 4 ,4-oxadiazol-3-yl]-phenyl}-ethyl)-amide.6. A pharmaceutical composition comprising the compound according to and a pharmaceutically acceptable carrier.7. A method for treating an allergic or inflammatory disorder in a patient in need thereof claim 1 , comprising administering to the patient a pharmaceutically effective amount of the compound according to .8. The method according to claim 7 , wherein the allergic or inflammatory disorder is selected from the group consisting of allergic rhinitis claim 7 , asthma claim 7 , chronic obstructive pulmonary disease and age-related macular degeneration.11. The process of wherein the suitable coupling reagent is selected from the consisting of DMTMM claim 10 , CDI claim 10 , and TBTU.14. The process of wherein R4 of the ester compound is CH.1824.-. (canceled) The present invention is directed to phenyloxadiazole compounds, their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in the treatment of disease states capable of being modulated by the inhibition of the prostaglandin D synthase.Allergic rhinitis, the most common atopic disease, has an estimated prevalence ranging from about 5 to about 22 percent of the general human population and is characterized by the symptoms of sneezing, ...

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28-09-2017 дата публикации

TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2

Номер: US20170273965A1
Принадлежит: Merck Sharp & Dohme Corp.

The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula (I) are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions. 2. The compound of or a pharmaceutically acceptable salt thereof wherein Ris aryl.3. The compound of claim 2 , or a pharmaceutically acceptable salt thereof wherein ring A is phenyl or fused phenyl.4. The compound of claim 3 , or a pharmaceutically acceptable salt thereof wherein X is —CONH—* claim 3 , wherein * indicates the position of attachment to R.5. The compound of claim 2 , or a pharmaceutically acceptable salt thereof wherein ring A is 5- or 6-membered heteroaryl containing 1-4 heteroatoms selected from the group consisting of N claim 2 , O claim 2 , and S or fused 8- to 10-membered heteroaryl containing 1-4 heteroatoms selected from the group consisting of N claim 2 , O claim 2 , and S.6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof wherein X is —CONH—* claim 5 , wherein * indicates the position of attachment to R.7. The compound of or a pharmaceutically acceptable salt thereof wherein Ris hydrogen.8. The compound of or a pharmaceutically acceptable salt thereof wherein Ris 5- or 6-membered heteroaryl containing 1-4 heteroatoms selected from the group consisting of N claim 1 , O claim 1 , and S claim 1 , wherein the heteroaryl is unsubstituted or substituted with (C)alkyl or halo(C)alkyl.9. The compound of claim 8 , or a pharmaceutically acceptable salt thereof wherein ring A is phenyl or fused phenyl.10. The compound of claim 9 , or a pharmaceutically ...

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28-09-2017 дата публикации

TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2

Номер: US20170273966A1
Принадлежит: Merck Sharp & Dohme Corp.

The present invention relates to a compound represented by formula I:and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions. 2. The compound of or a pharmaceutically acceptable salt thereof wherein L is —CH—.3. The compound of or a pharmaceutically acceptable salt thereof wherein M is *—N(R)—C(O)— claim 2 , or *—N(R)—C(O)-heterocyclyl- claim 2 , wherein the heterocyclyl is a 5- to 6-membered monocyclic ring containing 1-2 heteroatoms selected from the group consisting of N claim 2 , O claim 2 , and S; wherein * indicates the point of attachment to group L.4. The compound of or a pharmaceutically acceptable salt thereof wherein X is —NH—.5. The compound of or a pharmaceutically acceptable salt thereof wherein L is —C(O)—.7. The compound of or a pharmaceutically acceptable salt thereof wherein X is —NH—.8. The compound of or a pharmaceutically acceptable salt thereof wherein ring A is ring A is 5- or 6-membered heteroaryl containing 1-4 heteroatoms selected from the group consisting of N claim 1 , O claim 1 , and S or fused 8- to 10-membered heteroaryl containing 1-4 heteroatoms selected from the group consisting of N claim 1 , O claim 1 , and S.9. The compound of or a pharmaceutically acceptable salt thereof wherein ring A is pyrazolyl claim 1 , isoquinolinyl claim 1 , quinolinyl claim 1 , imidazolyl claim 1 , 1H-benzo[d]imidazolyl claim 1 , imidazo[1 claim 1 ,2-a]pyrimidinyl claim 1 , imidazo[1 claim 1 ,2-a]pyridinyl claim 1 , benzo[c][1 claim 1 ,2 claim 1 ,5]oxadiazolyl claim 1 , imidazo[2 claim 1 ,1-b]thiazolyl ...

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29-08-2019 дата публикации

PHENYLOXADIAZOLE DERIVATIVES AS PGDS INHIBITORS

Номер: US20190262338A1
Принадлежит:

This invention is directed to a compound of formula (I): 224-. (canceled) The present invention is directed to phenyloxadiazole compounds, their preparation, pharmaceutical compositions containing these compounds, and their pharmaceutical use in the treatment of disease states capable of being modulated by the inhibition of the prostaglandin D synthase.Allergic rhinitis, the most common atopic disease, has an estimated prevalence ranging from about 5 to about 22 percent of the general human population and is characterized by the symptoms of sneezing, nasal discharge, and nasal congestion. These symptoms are believed to be triggered by multiple mediators released from mast cells and other inflammatory cells. Current therapies, such as antihistamines, deal effectively with the sneezing and nasal discharge, but have little effect on congestion, which is a key symptom affecting the quality of life of patients.Local allergen challenge in patients with allergic rhinitis, bronchial asthma, allergic conjunctivitis and atopic dermatitis has been shown to result in rapid elevation of prostaglandin D2 “(PGD2)” levels in nasal and bronchial lavage fluids, tears and skin chamber fluids. PGD2 has many inflammatory actions, such as increasing vascular permeability in the conjunctiva and skin, increasing nasal airway resistance, airway narrowing and cosinophil infiltration into the conjunctiva and trachea. PGD2 is the major cyclooxygenase product of arachidonic acid produced from mast cells on immunological challenge [Lewis, R A, Soter N A, Diamond P T, Austen K F, Oates J A, Roberts L J II, Prostaglandin D2 generation after activation of rat and human mast cells with anti-IgE, . Immunol. 129, 1627-1631, 1982]. Activated mast cells, a major source of PGD2, are one of the key players in driving the allergic response in conditions such as asthma, allergic rhinitis, allergic conjunctivitis, allergic dermatitis and other diseases [Brightling C E, Bradding P, Pavord I D, Wardlaw A J, ...

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28-09-2017 дата публикации

NOVEL CAPSAZEPINE ANALOGS FOR THE TREATMENT OF CANCER AND OTHER PROLIFERATIVE DISEASES

Номер: US20170275280A1

The present disclosure relates generally to derivatives of capsazepine and methods of use thereof In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. In some aspects of the present disclosure, the disclosure provides capsazepine derivatives which may be useful in the treatment of cancer. Such cancers that the compounds may be used to treating include but are not limited to breast, cervical, oral, head, neck, or prostate cancer. In some aspects, the compounds may be useful in treating a tumor by direct injection of the compound into the tumor, particularly an oral tumor. In other aspects, the compounds are administered systemically. The compounds of the present disclosure may also be used to treat the pain associated with a tumor for which it is being administered. 2. The method of claim 1 , wherein Xis O.3. The method of claim 1 , wherein Xis S.4. The method according to any one of - claim 1 , wherein Ris —NRR claim 1 , wherein: Ris hydrogen claim 1 , alkyl claim 1 , substituted alkyl; and Ris aralkylor substituted aralkyl.5. The method of claim 4 , wherein Ris hydrogen.6. The method of claim 4 , wherein Ris alkyl.7. The method of claim 6 , wherein Ris alkyl.8. The method of claim 7 , wherein Ris methyl.9. The method according to any one of - claim 7 , wherein Ris aralkyl.10. The method of claim 9 , wherein Ris benzyl or 2-phenylethyl.11. The method according to any one of - claim 9 , wherein Ris substituted aralkyl.12. The method of claim 11 , wherein Ris 3 claim 11 ,4-dihydroxybenzyl claim 11 , 4-chlorobenzyl claim 11 , 4-fluorobenzyl claim 11 , 2 claim 11 ,4-dichlorobenzyl claim 11 , 3 claim 11 ,4-dimethoxybenzyl claim 11 , 2-(3 claim 11 ,4-dihydroxyphenyl)ethyl claim 11 , 2-(4-chlorophenyl)ethyl claim 11 , 2-(4-fluorophenyl)ethyl claim 11 , 2-(2 claim 11 ,4-dichlorophenyl)ethyl claim 11 , or 2-(dimethoxyphenyl)ethyl.14. The method of claim 13 , wherein Ris hydrogen.15. The method ...

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29-08-2019 дата публикации

Compounds and method of use

Номер: US20190263802A1
Принадлежит: Individual

This present disclosure relates to compounds with ferroptosis inducing activity, a method of treating a subject with cancer with the compounds, and combination treatments with a second therapeutic agent.

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18-12-2014 дата публикации

COMPOSITIONS AND METHODS FOR TREATMENT

Номер: US20140371265A1
Принадлежит: SARcode Bioscience Inc.

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists. 1. A method of treating dry eye disease in a subject in need thereof comprising administering to said subject an effective amount of a lymphocyte function associated antigen-1 (LFA-1) antagonist or a pharmaceutically acceptable salt or ester thereof , wherein the LFA-1 antagonist is a peptide , a small organic molecule , or a combination thereof.2. The method of wherein said LFA-1 antagonist is directly competitive with the binding of ICAM-1 at the αL subunit of LFA-1.13. The method according to claim 1 , wherein said administration involves topical administration of said compound via a carrier vehicle selected from a group consisting of liquid drops claim 1 , liquid wash claim 1 , gel claim 1 , ointment claim 1 , spray claim 1 , and liposome.14. The method according to claim 13 , wherein said topical administration comprises infusion of said compound to said eyes via a device selected from the group consisting of a pump-catheter system claim 13 , a continuous or selective release device claim 13 , and a contact lens.15. The method according to claim 1 , wherein said administration involves systemically administering a liquid or liquid suspension of said compound via nose drops or nasal spray or nebulized liquid to oral or nasopharyngeal airways of said subject claim 1 , such that a therapeutically effective amount of said compound contacts the eyes of said subject via systemic absorption and ...

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26-10-2017 дата публикации

Tetrahydroisoquinoline Derivatives

Номер: US20170304292A1
Принадлежит:

The present invention relates to tetrahydroisoquinoline derivatives according to formula (I), which are Positive Allosteric Modulators of D1 and accordingly of benefit as pharmaceutical agents for the treatment of diseases in which D1 receptors play a role. 4. The compound or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen claim 1 , halogen claim 1 , hydroxy claim 1 , C-alkyl hydroxy claim 1 , Calkoxy claim 1 , Calkylsulfanyl claim 1 , Calkylsulfinyl claim 1 , Calkylsulfonyl or (C-alkylsulfonyl)amino.5. The compound or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris hydrogen claim 1 , halogen claim 1 , Calkyl unsubstituted or substituted by one or more halogens claim 1 , C-alkyl hydroxy claim 1 , Calkoxy claim 1 , Calkylsulfanyl claim 1 , Calkylsulfinyl claim 1 , Calkylsulfonyl claim 1 , cyano claim 1 , Calkylamido claim 1 , pyrazolyl claim 1 , or a group of formula —CHR claim 1 , —NHRor —CHNHRwherein Ris selected from Calkylacyl or Calkylsulfonyl.6. The compound or a pharmaceutically acceptable salt thereof wherein Ris halogen claim 1 , Calkyl or Calkoxy.7. The compound or a pharmaceutically acceptable salt thereof wherein{'sup': 5', '6', '5', '5', '5', '5, 'sub': 1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6-', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '1-6', '3-8', '1-6', '1-6', '3-8, 'Ris hydrogen, cyano, hydroxy, amino, carbamoyl, sulfamoyl, Calkylsulfinyl, Calkylaminosulfinyl, Calkylsulfonyl optionally substituted by Calkoxy or heterocycle, N-cyano-S—(C-alkyl)sulfonimidoyl, N,S-(di-C-alkyl)sulfonimidoyl, (di-C-alkyl)(oxido)-λ-sulfanylidene-amino, (C-alkylsulfonyl)amino; or Ris Calkyl mono- or polysubstituted by hydroxy, halogen, Calkylsulfanyl, Calkylsulfonyl, (Calkyl sulfonyl)amino, (C-alkylacyl)amino, Calkylureido, Calkylcarbamate, Calkoxycarbonyloxy; or Ris an heterocycle optionally mono- or polysubstituted by Calkyl or Calkylsulfonyl; or Ris an amido group selected from ...

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02-11-2017 дата публикации

AMINOINDANE-, AMINOTETRAHYDRONAPHTHALENE- AND AMINOBENZOCYCLOBUTANE-DERIVED PRMT5-INHIBITORS

Номер: US20170313713A1
Принадлежит:

A compound of formula (1a), (1b) or (1c) wherein: n is 1 or 2; Ris H or Me; Ris optionally one or more halo or methyl groups; Rand Rare independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand R(if present) are independently selected from the group consisting of: (i) F; (ii) H; (iii) Me; and (iv) CHOH; Rand Rare independently selected from H and Me; Ris selected from OH, —NH, —C(═O)NH, and —CHOH; Ris either H or Me; Ris either H or Me; A is either (i) optionally substituted phenyl; (ii) optionally substituted naphthyl; or (iii) optionally substituted Cheteroaryl. 26-. (canceled)7. A compound according to claim 1 , wherein Rrepresents one to four Me or halo groups.8. A compound according to claim 1 , wherein:{'sup': 2a', '2b', '2c', '2d, '(a) R, R, Rand R(if present) are all H; or'}{'sup': 2a', '2b', '2c', '2d, 'sub': '2', '(b) of formula Ia or Ib, wherein R, R, Rand Rare comprised of three H and one Me or CHOH group; or'}{'sup': 2a', '2b', '2c', '2d, '(c) of formula Ia or Ib, wherein R, R, Rand Rare comprised of two H and two Me groups; or'}{'sup': 2a', '2b, 'sub': '2', '(d) of formula Ic, wherein Ris H and Ris a Me or CHOH group; or'}{'sup': 2a', '2b, 'sub': '2', '(e) of formula Ic, wherein Rand Rare each a Me or CHOH group.'}917-. (canceled)18. A compound according to claim 1 , wherein:{'sup': 3a', '3b, '(a) Ris H and Ris Me, or'}{'sup': 3a', '3b, '(b) Rand Rare both H, or'}{'sup': 3a', '3b, '(c) Rand Rare both Me.'}1925.-. (canceled)28. A compound according to claim 1 , wherein the compound is a racemate at the carbon atom to which Rand Rare attached.29. A compound according to claim 1 , wherein the compound is a single enantiomer at the carbon atom to which Rand Rare attached.3031-. (canceled)32. A compound according to claim 1 , wherein the optional substituents on A are independently selected from the group consisting of: Calkyl claim 1 , Cfluoroalkyl claim 1 , Ccycloalkyl claim 1 , Cheteroaryl claim 1 , Cheteroaryl ...

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01-10-2020 дата публикации

LXR INVERSE AGONISTS FOR TREATMENT OF CANCER

Номер: US20200308135A1
Принадлежит: SAINT LOUIS UNIVERSITY

In some aspects, the present disclosure provides compounds of the formula: (I) or (II) wherein the variables are as defined herein. In some embodiments, these compounds may be used to treat cancer or other hyperproliferative diseases, as well as atherosclerosis and coronary artery disease. 7. The compound according to claim 2 , wherein Ris —S(O)R.812-. (canceled)13. The compound according to claim 2 , wherein Ris hydrogen.14. The compound according to claim 2 , wherein Ris —C(O)OR.15. (canceled)16. The compound according to claim 2 , wherein Ris —(CH)C(O)NRR.1729-. (canceled)30. The compound according to claim 2 , wherein Ris hydrogen.31. The compound according to claim 2 , wherein Ris halo.32. The compound according to claim 2 , wherein Ris arylor substituted aryl.3334-. (canceled)35. The compound according to claim 2 , wherein Ris heteroarylor substituted heteroaryl.3637-. (canceled)38. The compound according to claim 2 , wherein R′ is hydrogen.39. The compound according to claim 2 , wherein R′ is alkyl.40. (canceled)41. The compound according to claim 2 , wherein R″ is hydrogen.42. The compound according to claim 2 , wherein R″ is alkyl.4345-. (canceled)46. The compound according to claim 2 , wherein Ris —C(O)R.4750-. (canceled)51. The compound according to claim 2 , wherein Ris —S(O)R.5256-. (canceled)57. The compound according to claim 2 , wherein Ris hydrogen.58. The compound according to claim 2 , wherein Ris alkylor substituted alkyl.59. The compound according to claim 2 , wherein Ris hydrogen.60. The compound according to claim 2 , wherein Ris halo.61. (canceled)62. The compound according to claim 2 , wherein Ris arylor substituted aryl.63. (canceled)64. The compound according to claim 2 , wherein p is 1 or 2.6569-. (canceled)70. A pharmaceutical composition comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, '(A) a compound according to ; and'}(B) an excipient.71. The pharmaceutical composition of claim 70 , wherein the pharmaceutical composition ...

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17-11-2016 дата публикации

FLUORINATED ARYLALKYLAMINOCARBOXAMIDE DERIVATIVES

Номер: US20160332959A1
Автор: Pevarello Paolo
Принадлежит:

Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R, R, R, R, R, Rand Rhave the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urolological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role. 2. A compound of claim 1 , wherein:{'sub': 2', 'm', '1', '4', '3', '6, 'W is a group A-[(CH)—O]— wherein: m is zero, 1, 2 or 3; A is (C-C)alkyl optionally substituted by one to three fluorine atoms; (C-C)cycloalkyl; phenyl optionally substituted with a halo group; or thiazolyl'}{'sub': 1', '4, 'J independently is hydrogen; C-Calkyl; chloro; or fluoro;'} [{'sup': '1', 'sub': 1', '4', '1', '4', '3', '6, 'Ris hydrogen; (C-C)alkyl optionally substituted with a hydroxy group or a (C-C)alkoxy group; or (C-C)cycloalkyl;'}, {'sup': '2', 'sub': 1', '4, 'Ris hydrogen; or (C-C)alkyl;'}, {'sup': '2′', 'sub': 1', '4', '1', '4', '1', '4, 'R is hydrogen or (C-C)alkyl optionally substituted with a (C-C)alkoxy or a phenyl group, the phenyl group being optionally substituted with a (C-C)alkoxy group;'}, {'sup': '3', 'sub': 1', '4, 'Ris hydrogen; or (C-C)alkyl;'}, {'sup': '4', 'sub': 1', '4, 'Ris hydrogen; (C-C)alkyl; phenyl; or cyclohexyl; or'}, {'sup': 3', '4, 'sub': 1', '2', '1', '4, 'Rand R, taken together with the adjacent nitrogen atom, form an azetidinyl, pyrrolidinyl, morpholinyl, piperidinyl or piperazinyl, the piperydinyl ring being optionally substituted with one or two (C-C)alkyl group(s) and the piperazinyl ring being optionally substituted on the other N-atom with a (C-C)alkyl, benzyl, or phenylsulfonyl group; or a pirrolidinyl, piperidinyl, morpholinyl or piperazinyl ring fused ...

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16-11-2017 дата публикации

Ire-1alpha inhibitors

Номер: US20170326104A1

Compounds which directly inhibit IRE-1α activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) and can be used as single agents or in combination therapies.

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26-11-2015 дата публикации

ACTINIC-RAY- OR RADIATION-SENSITIVE RESIN COMPOSITION, ACTINIC-RAY- OR RADIATION-SENSITIVE FILM AND METHOD OF FORMING PATTERN

Номер: US20150338736A1
Принадлежит: FUJIFILM Corporation

Provided is an actinic-ray- or radiation-sensitive resin composition including a resin (A) and any of compounds (B) of general formula (I) below. (In general formula (I), Rf represents a fluorine atom or a monovalent organic group containing at least one fluorine atom; Rrepresents a hydrogen atom or a monovalent substituent containing no fluorine atom; Xrepresents a monovalent organic group having at least two carbon atoms, or a methyl group in which a substituent other than a fluorine atom is optionally introduced, provided that Xmay be bonded to Rto thereby form a ring; and Z represents a moiety that when exposed to actinic rays or radiation, is converted to a sulfonic acid group, an imidic acid group or a methide acid group.) 2. The actinic-ray- or radiation-sensitive resin composition according to claim 1 , wherein Xin general formula (I) above is any of organic groups of general formula (Ia) below claim 1 ,{'br': None, 'sub': 11', '11, '-L-X\u2003\u2003(Ia)'}in which{'sub': 11', '2', '11, 'Lrepresents a connecting group selected from among —COO—, —OCO—, —CO—, —O—, —S—, —SO—, —SO—, —NH—, —C(═S)—, —CONR— (R is a hydrogen atom, an alkyl group or a cycloalkyl group), an alkylene group, a cycloalkylene group, an alkenylene group, an alkynylene group, an arylene group and a group comprised of a combination of two or more of these, provided that the connecting group represented by Lcontains no fluorine atom, and'}{'sub': '11', 'Xrepresents a substituent,'}provided that the any of organic groups of general formula (Ia) as a whole contains at least two carbon atoms.3. The actinic-ray- or radiation-sensitive resin composition according to claim 1 , wherein Rf in general formula (I) above is a fluorine atom or a perfluoroalkyl group having 1 to 4 carbon atoms.5. The actinic-ray- or radiation-sensitive resin composition according to claim 4 , wherein Xin general formula (II) above is either *—ORor *—NRR claim 4 , in which * represents a position of bonding to the carbonyl ...

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23-11-2017 дата публикации

Amido Compounds And Their Use As Pharmaceuticals

Номер: US20170334847A1
Принадлежит:

The present invention relates to inhibitors of 11-β hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-β hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess. 138-. (canceled)39. A compound , which is N-methyl-5-[4-(1-{[3-oxo-1′H ,3H-spiro[2-benzofuran-1 ,3′-pyrrolidin]-1′-yl]carbonyl}cyclopropyl)phenyl]pyridine-2-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium; or a pharmaceutically acceptable salt thereof.40. A compound , which is N-methyl-5-[4-(1-{[(1R)-3-oxo-1′H ,3H-spiro[2-benzofuran-1 ,3′-pyrrolidin]-1′-yl]carbonyl}cyclopropyl)phenyl]pyridine-2-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium; or a pharmaceutically acceptable salt thereof.41. A compound , which is N-methyl-5-[4-(1-{[(1R)-3-oxo-1′H ,3H-spiro[2-benzofuran-1 ,3′-pyrrolidin]-1′-yl]carbonyl}cyclopropyl)phenyl]pyridine-2-carboxamide , wherein one or more hydrogen atoms are replaced by deuterium.42. A pharmaceutical composition comprising the compound of claim 39 , or a pharmaceutically acceptable salt thereof claim 39 , and a pharmaceutically acceptable carrier.43. A pharmaceutical composition comprising the compound of claim 40 , or a pharmaceutically acceptable salt thereof claim 40 , and a pharmaceutically acceptable carrier.44. A pharmaceutical composition comprising the compound of claim 41 , and a pharmaceutically acceptable carrier. This application is a continuation of U.S. Ser. No. 14/808,337, filed Jul. 24, 2015, which is a continuation of U.S. Ser. No. 13/243,565, filed Sep. 23, 2011, now issued as U.S. Pat. No. 9,126,927 on Sep. 8, 2005, which is a continuation of U.S. Ser. No. 12/817,887 filed Jun. 17, 2010, now issued as U.S. Pat. No. 8,058,288 on Nov. 15, 2011, which is a continuation of U.S. ...

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22-11-2018 дата публикации

TETRAHYDROISOQUINOLINE DERIVATIVES

Номер: US20180334436A1
Принадлежит:

Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds. 2. A compound or salt according to wherein Ris Calkyl.3. A compound or salt according to wherein W is a bond.4. A compound or salt according to wherein each Ris H.5. A compound or salt according to wherein Ris optionally substituted phenyl.6. A compound or salt according to wherein Ris phenyl substituted by one to four substituents selected from fluorine claim 5 , methyl claim 5 , —CHCHCHO— wherein said —CHCHCHO— is bonded to adjacent carbon atoms on said phenyl to form a bicyclic ring claim 5 , or —NHCHCHO— wherein said —NHCHCHO— is bonded to adjacent carbon atoms on said phenyl to form a bicyclic ring.7. A compound or salt according to wherein each Ris independently Calkyl claim 1 , phenyl claim 1 , naphthyl claim 1 , cyclopentyl claim 1 , cyclohexyl claim 1 , pyridyl claim 1 , or tetrahydropyranyl claim 1 , each of which is optionally substituted by 1-3 substituents selected from halogen claim 1 , Calkyl claim 1 , —OCalky claim 1 , Cfluoroalkyl claim 1 , or phenyl.8. A compound or salt according to wherein each Ris methyl.9. A compound or salt according to wherein X is O.10. A compound or salt according to wherein one Y group is N-L-R.12. (canceled)13. A pharmaceutical composition comprising a compound or salt according to .14. A method for treating a viral infection in a patient mediated at least in part by a virus in the retrovirus family of viruses claim 13 , comprising administering to said patient a composition according to .15. The method of wherein said viral infection is mediated by the HIV virus.1618-. (canceled) The present invention relates to substituted tetrahydroisoquinoline compounds, pharmaceutical compositions, and methods of use thereof for (i) inhibiting HIV replication in a subject infected with HIV, or (ii) treating a subject infected with HIV, by administering such compounds.Human immunodeficiency virus type 1 (HIV-1) ...

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30-11-2017 дата публикации

ANTIMICROBIAL COMPOUNDS, COMPOSITIONS AND METHODS

Номер: US20170342025A1
Принадлежит:

The invention discloses compounds of the formula wherein A, B, X, Y and Z are defined. The compounds of the invention show activity against a range of bacteria, and are useful in the treatment or prophylaxis of a bacterial infection in an animal. 2. The compound of claim 1 , wherein A is an aryl group selected from a group consisting of phenyl claim 1 , thiazolyl claim 1 , pyridyl claim 1 , imidazolyl claim 1 , and benzothiazole.3. The compound of wherein A is a phenyl group claim 1 , optionally substituted with from one to three groups independently selected from a group consisting of halo claim 1 , C1-C6 alkyl claim 1 , C1-C6 haloalkyl claim 1 , C1-C6 alkoxy claim 1 , C1-C6 haloalkoxy claim 1 , nitro claim 1 , cyano and C1-C6 thioalkyl.5. The compound of claim 1 , wherein B is an aryl group selected from a group consisting of phenyl claim 1 , thiazolyl claim 1 , pyridyl claim 1 , and benzothiazole.6. The compound of claim 5 , wherein B is a phenyl group claim 5 , optionally substituted with from one to three groups independently selected from a group consisting of halo claim 5 , C1-C6 alkyl claim 5 , C1-C6 haloalkyl claim 5 , C1-C6 alkoxy claim 5 , C1-C6 haloalkoxy claim 5 , nitro claim 5 , cyano and C1-C6 thioalkyl.7. The compound of claim 1 , wherein Y is CH═N.8. The compound of claim 1 , wherein Ris NR claim 1 , with Ras defined in .9. The compound of claim 8 , wherein Ris H.10. The compound of claim 1 , wherein R claim 1 , Rand Rare all H.11. The compound of which is one of 1-[({3-[(2 claim 1 ,3-dichlorophenyl)methoxy]phenyl}methylidene)amino]guanidine; 1-{[(3-{[2-chloro-3-(trifluoromethyl)phenyl]methoxy}phenyl)methylidene]amino} guanidine; 7-[(2 claim 1 ,3-dichlorophenyl)methoxy]-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroisoquinoline-2-carboximidamide; 5-[(2 claim 1 ,3-dichlorophenyl)methoxy]-1 claim 1 ,2 claim 1 ,3 claim 1 ,4-tetrahydroisoquinoline-2-carboximidamide; 1-({3-[(2 claim 1 ,3-dichlorophenyl)methoxy]phenyl}methyl)-1-methylguanidine; 1-({3-[(2 ...

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05-11-2020 дата публикации

METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF

Номер: US20200347021A1
Принадлежит:

Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions. 6. The compound of claim 5 , or a pharmaceutically acceptable salt thereof claim 5 , wherein Ris unsubstituted phenyl.10. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein p is 1 and Ris halogen claim 1 , —CF claim 1 , or —OCH.11. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein p is 0.12. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 1 and Ris halogen claim 1 , —CF claim 1 , or —OCH.13. The compound of claim 12 , or a pharmaceutically acceptable salt thereof claim 12 , wherein Ris F.14. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein n is 0.15. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris —COH.17. (canceled)18. (canceled)19. (canceled)20. (canceled)21. (canceled)22. (canceled)23. (canceled)24. (canceled)25. (canceled)26. (canceled)27. (canceled)28. (canceled)29. (canceled)30. (canceled)31. (canceled)32. (canceled)33. (canceled)34. (canceled)35. (canceled)36. (canceled)37. (canceled)38. (canceled)39. (canceled)40. (canceled)41. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt claim 1 , and at least one pharmaceutically acceptable excipient.42. (canceled)43. (canceled)44. A method of treating a central nervous disorder (CNS) the method comprising the step of administering to a subject in need thereof claim 1 , an effective amount of the compound of claim 1 , thereby treating the disorder.45. (canceled)46. (canceled)47. (canceled)48. (canceled)49. (canceled)50. (canceled)51. (canceled)52. (canceled)53. (canceled)54. (canceled)55. (canceled)56. (canceled)57. (canceled)58. (canceled) ...

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28-12-2017 дата публикации

2-PHENETHENYLTETRAHYDRO ISOQUINOLINES USEFUL AS ANTI-HIV COMPOUNDS

Номер: US20170368051A1
Принадлежит:

This invention provides, among other things, tetrahydroisoquinolines useful for treating viral infections, pharmaceutical formulations containing such compounds, as well as methods of inhibiting the replication of a virus, such as HIV, or treating a disease, such as AIDS. 6. A pharmaceutical formulation comprising:{'claim-ref': {'@idref': 'CLM-00001', 'claim 1'}, 'a) a compound of , or a pharmaceutically acceptable salt thereof; and'}b) a pharmaceutically acceptable excipient.8. The method of claim 7 , wherein the virus is a member of the Orthoretroviridae family.9. The method of claim 7 , wherein the virus is HIV.11. The method of claim 10 , wherein the disease is AIDS.12. The method of claim 10 , wherein the animal is a human.13. A method of treating an HIV infection in a human claim 1 , the method comprising administering to said human a therapeutically effective amount of a compound according to . This application claims the benefit of U.S. Provisional Patent Application No. 62/092,115, filed Dec. 15, 2014, which is incorporated by reference in its entirety for all purpose.There is a need in the art to discover new compounds useful as antivirals.It has now been discovered that certain tetrahydroisoquinolines are surprisingly effective antivirals. This, and other uses of these compounds are described herein.This invention provides, among other things, novel compounds useful for treating viral infections, pharmaceutical formulations containing such compounds, as well as methods of inhibiting the replication of a virus or treating a disease.In an exemplary embodiment, the invention provides a compound of the formula which is:in whichIn an exemplary embodiment, there is provided a pharmaceutical formulation comprising a compound of the invention and a pharmaceutically acceptable diluent or carrier.Also provided is a method of treating a subject infected with a lentivirus, e.g., human immunodeficiency virus (HIV). The method comprises, administering to the subject a ...

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26-11-2020 дата публикации

COMPOSITIONS OF SPHINGOSINE-1-PHOSPHATE RECEPTOR 2 (S1PR2) BINDING AGENTS AND USES THEREOF

Номер: US20200369626A1
Принадлежит: WASHINGTON UNIVERSITY

Described are compounds for the binding of S1PR2, and imaging agents and pharmaceutical compositions including said compounds. Also described are methods employing the compounds, imaging agents, and pharmaceutical compositions. These methods include imaging and/or treatment of diseases associated with S1PR2. 166.-. (canceled)7266. The compound of claim , wherein Y is —O— , —S— , —C(O)— , —C(OH)— , —N(H)— or —N(BOC)—.7366. The compound of claim , wherein Ris —CON(R) , F , —SOCH , alkoxy , haloalkoxy , or —COOH.7466. The compound of claim , wherein Ris —C(O)NH , —C(O)NHCH , —C(O)N(CH) , F , —SOCH , —OCH , or —OCHCHF.7566. The compound of claim , wherein Rand Rare each independently hydrogen , substituted or unsubstituted C1 to C6 alkyl , hydroxyl , or alkoxy.7666. The compound of claim , wherein Rand Rare each independently hydrogen , —OH , 2-(ethyl)butyl , isobutyl , isopropyl , methyl , ethyl , propyl , butyl , 4-methylpentan-2-onyl , or C1 to C6 hydroxyalkyl.8066. An imaging agent comprising a compound of claim and a reporting group.8166. A pharmaceutical composition comprising a compound of claim and at least one pharmaceutically acceptable excipient.8266. A method of treating anaphylaxis , cancer , central nervous system diseases , fibrosis diseases , diabetes , diabetic pulmonary fibrosis , diabetic nephropathy , inflammation , inflammation diseases , inflammatory response in multiple sclerosis , multiple sclerosis , liver fibrosis , and/or lung fibrosis in a subject in need thereof , the method comprising administering to the subject a therapeutically effective amount of a compound of claim .83. A method of imaging a target in a subject , the method comprising:{'claim-ref': {'@idref': 'CLM-00080', 'claim 80'}, 'administering the imaging agent of and'}detecting the imaging agent in the subject, wherein detecting the imaging agent comprises imaging with positron emission tomography (PET) imaging, single photon emission computed tomography (SPECT) imaging, mass ...

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26-11-2020 дата публикации

A PROCESS TO OBTAIN A TETRAHYDROISOQUINOLINE DERIVATIVE

Номер: US20200369651A1
Принадлежит:

The present invention relates to a process for preparing lifitegrast or a salt thereof, wherein the process comprises hydrogenation of compound II in a mixture comprising at least one solvent selected from the group consisting of acetonitrile, a ketone solvent, an ester solvent and a mixture thereof, preferably acetonitrile. 2. The process according to claim 1 , wherein the hydrogenation is a transfer hydrogenolysis catalyzed by palladium and in the presence of formic acid or a salt thereof as a hydrogen donor.3. The process according to claim 2 , wherein the hydrogen donor is triethylammonium formate.4. The process according to claim 1 , wherein the ketone solvent is selected from the group consisting of acetone claim 1 , methyl butyl ketone claim 1 , methyl ethyl ketone claim 1 , methyl isobutyl ketone claim 1 , methyl isopropyl ketone and a mixture thereof claim 1 , and the ester solvent is selected from the group consisting of butyl acetate claim 1 , ethyl acetate claim 1 , ethyl formate claim 1 , isobutyl acetate claim 1 , isopropyl acetate claim 1 , methyl acetate claim 1 , methyl formate claim 1 , propyl acetate and a mixture thereof.5. The process according to claim 1 , wherein the hydrogenation is performed in the presence of a chloride salt.6. The process according to claim 5 , wherein the chloride salt is an ammonium chloride salt claim 5 , preferably tetrabutylammonium chloride.8. The process according to claim 7 , wherein the reaction to obtain compound II is performed in a solvent selected from the group consisting of butyl acetate claim 7 , ethyl acetate claim 7 , ethyl formate claim 7 , isobutyl acetate claim 7 , isopropyl acetate claim 7 , methyl acetate claim 7 , methyl formate claim 7 , propyl acetate claim 7 , dimethylsulfoxide claim 7 , N claim 7 ,N-dimethylformamide claim 7 , N claim 7 ,N-dimethylacetamide and a mixture thereof claim 7 , preferably in a mixture comprising ethyl acetate and dimethylsulfoxide.10. The process according to claim 9 ...

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05-12-2019 дата публикации

Organic Electroluminescence Device

Номер: US20190372030A1
Принадлежит:

The present invention relates to an electroluminescence device having high luminous efficiency (for example, external quantum efficiency) and high durability and causing little chromaticity shift after device deterioration. The present invention also relates to an organic electroluminescence device material comprising a substrate having thereon a pair of electrode and at least one organic layer between the electrodes, the organic layer containing a light emitting layer, wherein the light emitting layer contains a metal complex having a group represented by formula (I). 127.-. (canceled)29. The metal complex as claimed in claim 28 , wherein in formula (I) claim 28 , nrepresents an integer of 1 to 3.30. The metal complex as claimed in wherein in formula (I) claim 28 , nis 1.31. The metal complex as claimed in claim 28 , wherein in formula (I) claim 28 , each of Rand Rrepresents a hydrogen atom.32. The metal complex as claimed in claim 28 , wherein in formula (I) claim 28 , Z represents a cyclopentyl group or a cyclohexyl group.43. The metal complex as claimed in claim 28 , wherein the one layer of the layer containing a metal complex represented by formula (2) claim 28 , a metal complex represented by formula (14) claim 28 , or a phosphorescent metal complex containing a monoanionic bidentate ligand represented by the formulae (A1) to (A4) a metal having an atomic weight of 40 or more claim 28 , having a group represented by formula (I) is the light-emitting layer.45. A light emission apparatus comprising the organic electroluminescence device as claimed in .46. A display apparatus comprising the organic electroluminescence device as claimed in .47. An illumination apparatus comprising the organic electroluminescence device as claimed in . The present invention relates to a luminescence device capable of converting an electric energy into light and thereby producing luminescence. More specifically, the present invention relates to an organic electroluminescence device ...

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10-12-2020 дата публикации

Phenyloxadiazole derivatives as pgds inhibitors

Номер: US20200383982A1
Принадлежит: SANOFI SA

wherein R1, R2 and R3 are as defined herein, a pharmaceutical composition comprising the compound, intermediates and processes for making said compounds, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma, chronic obstructive pulmonary disease (COPD) and age-related macular degeneration (AMD).

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17-12-2020 дата публикации

COMPOUNDS AFFECTING PIGMENT PRODUCTION AND METHODS FOR TREATMENT OF BACTERIAL DISEASES

Номер: US20200392095A1
Принадлежит:

Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives, and methods for prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (II): 21. The composition of claim , wherein the composition is administered to reduce a virulence of bacteria causing the microbial infections and/or related disease or conditions in said subject.31. The composition of claim , wherein the composition further comprises one or more pharmaceutical acceptable carrier , salt , ester , excipient , vehicle , solvent , diluent , or any combination thereof.41. The composition of claim , wherein the one or more compounds and/or prodrugs thereof are anti-virulent agents for bacteria.61. The composition of claim , wherein the microbial infections and/or related diseases or conditions comprise infections of the skin and soft tissue , bone and joint , surgical wound , indwelling devices , lung and heart valves.71. The composition of claim , wherein the microbial infections are bacterial infections.8Staphylococcus. The composition of claim 7 , wherein the bacterial infections comprise sp. Infections.9StaphylococcusStaphylococcus aureusStaphylococcus aureus.. The composition of claim 8 , wherein the sp. Comprises or methicillin-resistant101Staphylococcus aureus.. The composition of claim claim 8 , wherein the composition inhibits biosynthesis of staphyloxanthin in the111Staphylococcus aureus.. The composition of claim claim 8 , wherein the composition blocks pigments production in121. The composition of claim claim 8 , wherein said subject is a mammal.131. The composition of claim claim 8 , wherein said subject is human.141. The composition of claim claim 8 , wherein the composition is administered to the subject in need thereof through oral pathways in one or more forms comprising capsule claim 8 , tablet claim 8 , granule ...

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28-11-1978 дата публикации

Medically useful 3*4*55trimethoxybfnzene derivative

Номер: JPS53135945A
Принадлежит: METABIO JOULLIE SA

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04-07-2001 дата публикации

Tetrahydroisoquinoline compounds as estrogen agonists/antagonists

Номер: EP1113007A1
Принадлежит: PFIZER INC

This invention relates to compounds useful for treating or preventing obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease, prostatic disease, and the like, and to pharmaceutical composition, methods, and kits comprising such compounds.

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06-05-2005 дата публикации

Tao kinase modulators and methods of use

Номер: WO2005040355A2
Принадлежит: Exelixis, Inc.

The invention provides compounds and methods for inhibition of kinases, such as those of the TAO family, more specifically KIAA1361, TAO, and JIK kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions.

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16-04-2012 дата публикации

Azadecalin glucocorticoid receptor modulators

Номер: KR101135885B1
Принадлежит: 코어셉트 쎄라퓨틱스, 잉크.

본 발명은 신규한 아자데칼린 화합물 부류 및 글루코코르티코이드 수용체 조절제로서 당해 화합물을 사용하는 방법을 제공한다. The present invention provides a new class of azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. 아자데칼린, 글루코코르티코이드, 글루코코르티코이드 수용체 조절제, 길항제, 작용제 Azadecalin, glucocorticoids, glucocorticoid receptor modulators, antagonists, agonists

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15-01-1981 дата публикации

Method of preparing isoquinoline derivatives, their salts, racemates or optical isomers

Номер: SU797580A3

Isoquinoline derivatives of the formula: <IMAGE> wherein A represents pyrid-3-yl, isoquinol-5-yl or a 3-alkylisoquinol-5-yl radical in which the alkyl moiety contains 1 to 10 carbon atoms, are new compounds, possessing useful pharmacological properties. They are particularly valuable as analgesic, anti-inflammatory and antipyretic agents.

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06-02-2008 дата публикации

氮杂萘烷糖皮质激素受体调节剂

Номер: CN101119970A
Принадлежит: Corcept Therapeutics Inc

本发明提供新的一类式(1)氮杂萘烷化合物和将这些化合物用作糖皮质激素受体调节剂的方法。

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15-01-2021 дата публикации

一种不对称硫脲类化合物的制备方法

Номер: CN110330450B
Принадлежит: Wenzhou Medical University

本发明公开了一种不对称硫脲类化合物的制备方法,包括:在DMSO或DMF溶剂中,以胺类化合物与二硫化碳为底物,合成不对称硫脲类化合物。本发明方法通过三组份串联反应一步合成不对称硫脲类化合物。本发明反应原料廉价易得,制备方法简单。反应仅需要溶剂,不需要其它添加剂,产率高,操作简单,适用于不同类型的不对称硫脲类化合物的合成。本发明方法可用于合成一系列的不对称硫脲类化合物,合成的产物不仅可作为中间化合物,用于进一步构筑复杂的活性化合物;同时该类化合物具有极大的药物活性潜力。

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27-05-2015 дата публикации

胍化合物

Номер: CN103459369B
Принадлежит: Yamanouchi Pharmaceutical Co Ltd

本发明提供作为药物组合物、特别是作为VAP-1相关疾病的预防和/或治疗用药物组合物的有效成分有用的化合物。本发明人对于具有VAP-1抑制活性的化合物进行了广泛深入的研究,结果发现,本发明化合物或其盐显示优异的VAP-1抑制活性,对于VAP-1相关疾病、特别是糖尿病性肾病或糖尿病性黄斑水肿的预防和/或治疗有用,并完成了本发明。另外,本发明涉及含有本发明化合物或其盐和赋形剂的药物组合物,特别是VAP-1相关疾病的预防和/或治疗用药物组合物。

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10-01-2000 дата публикации

Isoquinolines, method of their synthesis and pharmaceutical composition based on thereof

Номер: RU2144027C1
Автор: Рето Наэф
Принадлежит: НОВАРТИС АГ

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to isoquinolines of the formula (I) ДСОУТУГСсС ПЧ Го (19) 13) ВО” 2 144 027 ^С1 57 МК’ © 070 217/20, А 61 К 31/47 РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 94040170/04, 04.11.1994 (71) Заявитель: Новартис АГ (СН) (24) Дата начала действия патента: 04.11.1994 (72) Изобретатель: Наэф Рето (СН) (30) Приоритет: 05.11.1993 СВ 9322828.6 (73) Патентообладатель: (46) Дата публикации: 10.01.2000 Новартис АГ (СН) == (56) Ссылки: ЗЦ 1097621 А, 15.06.84. СВ 1407685, о 24.09.75. СВ 1400425, 16.07.75. (98) Адрес для переписки: 101000, Москва, Малый Златоустинский пер., ^ д.10, кв.15, "Евромаркпат", патентному поверенному Веселицкой И.А. сч © (54) ИЗОХИНОЛИНЫ, СПОСОБ ИХ ПОЛУЧЕНИЯ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ < (57) Реферат: где К - этильная или н-пропильная группа, < Изохинолины формулы | или их физиологически гидролизуемые и приемлемые сложные эфиры или = но-<сн,>.-© к кислотноаддитивные соли таких соединений ых или сложных эфиров, обладают с' противовоспалительными, снижающими сн © гиперреактивность дыхательных путей, а 3 также бронхорасширяющими свойствами. 3 с. —) и 3 з.п. ф-лы. О «1-С Н_>-0о 0—1-С Н_› 3? 3? ДСОУТУГСсС ПЧ Го (19) КУЗЗАМ АСЕМСУ ГОК РАТЕМТ$ АМО ТКАОЕМАКК$ 12) АВЗТКАСТ ОЕ 1МУЕМТОМ ВИ” 2144 027‘ (51) 1пЁ. С1.7 13) СЛ С 070 217/20, А 61 К 31/47 (21), (22) АррИсаНоп: 94040170/04, 04.11.1994 (24) ЕНесНуе дае Гог ргорейу па: 04.11.1994 (30) Рпогйу: 05.11.1993 СВ 9322828.6 (46) Рае оГ рибИсаНоп: 10.01.2000 (98) Май адагез$: 101000, Мозкуа, Мау| ЛаюизИпт$к| рег., .10, Ку.15, "ЕуготагКра{!", раеппоти роуегеппоти МезеШ$Ко] |.А. (71) АррИсапе: Моуаг!$ АС (СН) (72) пуетщог. — Мае!!Вею (СН) (73) Ргорпеюг: Моуа5$ Ас (СН) (54) ЗОСЧМОНМЕ$, МЕТНОО ОЕ ТНЕК ЗУМТНЕ$!$ АМО РНАКМАСЕОЧТ!'САЕ СОМРОЗПОМ ВАЗЕО ОМ ТНЕКЕОР (57) АБзГасЕ: НЕГО: огдапс спетгу, — рПагтасу. ЗУВЗТАМСЕ: пуепНоп геаез |(® зодитпопе$ ог Ше огти[а (1) Но < ...

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27-02-2010 дата публикации

Atp-binding casette transporter modulators

Номер: RU2382779C2

FIELD: chemistry. SUBSTANCE: novel compound is N-(5-hydroxy-2,4-di-tert-butylphenyl)-4-oxo-1H-quinoline-3-carboxamide or its pharmaceutically acceptable salts. The invention also relates to a pharmaceutical composition. EFFECT: obtaining a novel biologically active compound with CFTR activity modulation properties. 2 cl, 485 ex, 3 tbl (19) РОССИЙСКАЯ ФЕДЕРАЦИЯ RU (11) (51) МПК C07D C07D C07D C07D C07D C07D ФЕДЕРАЛЬНАЯ СЛУЖБА C07D ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, C07D ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ C07D A61K (12) ОПИСАНИЕ 2 382 779 401/12 (2006.01) 215/56 (2006.01) 209/12 (2006.01) 209/14 (2006.01) 209/18 (2006.01) 405/12 (2006.01) 409/12 (2006.01) 413/12 (2006.01) 417/12 (2006.01) 31/47 (2006.01) (13) C2 A61K 31/4709 (2006.01) A61P 25/00 (2006.01) A61P 31/00 (2006.01) ИЗОБРЕТЕНИЯ К ПАТЕНТУ (21), (22) Заявка: 2007102578/04, 24.06.2005 (24) Дата начала отсчета срока действия патента: 24.06.2005 (43) Дата публикации заявки: 27.07.2008 2 3 8 2 7 7 9 R U (56) Список документов, цитированных в отчете о поиске: WO 01/34570 А, 17.05.2001. US 4786644 А, 22.11.1988. Т.VAN ES ET AL, SOUTH AFRICAN JOURNAL OF CHEMISTRY, vol.54, 2001, pages 102-117. I.M.HEILBRONN ET AL, JOURNAL OF THE CHEMICAL SOCIETY, 1928, pages 934-941. K.GROHE ET AL, LIEBIGS ANNALEN DER CHEMIE, 1987, pages 871-879. Y.ITO ET AL, NEUROPHARMACOLOGY, vol.35, no.9/10, 1996, pages 1263-1269. (см. прод.) C 2 C 2 (45) Опубликовано: 27.02.2010 Бюл. № 6 (85) Дата перевода заявки PCT на национальную фазу: 24.01.2007 (86) Заявка PCT: US 2005/022768 (24.06.2005) (87) Публикация PCT: WO 2006/002421 (05.01.2006) Адрес для переписки: 129090, Москва, ул. Б.Спасская, 25, стр.3, ООО "Юридическая фирма Городисский и Партнеры", пат.пов. Е.Е.Назиной (54) МОДУЛЯТОРЫ ТРАНСПОРТЕРОВ АТФ-СВЯЗЫВАЮЩЕЙ КАССЕТЫ (57) Реферат: Изобретение соединению, относится к представляющего N-(5-гидрокси-2,4-ди-трет-бутилфенил)4-оксо-1Н-хинолин-3-карбоксамид, или к его фармацевтически приемлемым солям. новому собой Ñòð.: 1 ru 2 3 8 2 7 7 9 (73) ...

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25-07-2007 дата публикации

Atp-结合弹夹转运蛋白的调控剂

Номер: CN101006076A
Принадлежит: Vertex Pharmaceuticals Inc

本发明涉及ATP-结合弹夹(“ABC”)转运蛋白或其片段的调控剂、包括囊性纤维化跨膜电导调节剂、其组合物和与之有关的方法。本发明也涉及使用这类调控剂治疗ABC转运蛋白介导的疾病的方法。

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05-05-2022 дата публикации

Fgfr inhibitor, method for production and application thereof

Номер: RU2771526C1

FIELD: pharmaceuticals.SUBSTANCE: proposed is a compound by the formula (II), a stereoisomer, prodrug or pharmacologically acceptable salt thereof, wherein X constitutes CH; R1is selected from the group consisting of a C1-3alkyl, a C5cycloalkyl and a 4-6-membered heterocyclyl, optionally substituted with one or multiple additional substituents, R2constitutes phenyl, pyridyl or pyrazolyl, optionally substituted with one or multiple additional substituents; R3constitutes a methoxy; R4is independently selected from the group consisting of H, F and Cl; R10constitutes a C1alkyl; R13and R14each independently constitute a C1alkyl; r is 2; wherein, unless otherwise indicated, the heteroatom of heterocyclyl in the above substituents is selected from 1-2 nitrogen or oxygen atoms. Also proposed are a method for production and an application of a compound acting as an FGFR inhibitor for treating tumours, malignant neoplasms, myeloproliferative diseases, diseases of cells of bone and cartilaginous tissue, and hypophosphatemia.EFFECT: production of heteroaromatic compounds applicable as an FGFR inhibitor.9 cl, 10 ex, 2 tbl РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 771 526 C1 (51) МПК C07D 239/42 (2006.01) C07D 239/84 (2006.01) C07D 217/06 (2006.01) C07D 403/04 (2006.01) C07D 471/04 (2006.01) A61K 31/437 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА A61K 31/505 (2006.01) ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ A61K 31/506 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 239/42 (2022.02); C07D 239/84 (2022.02); C07D 217/06 (2022.02); C07D 403/04 (2022.02); C07D 471/04 (2022.02); A61K 31/437 (2022.02); A61K 31/505 (2022.02); A61K 31/506 (2022.02); A61K 31/519 (2022.02); A61P 35/00 (2022.02) 2020143515, 23.07.2019 (24) Дата начала отсчета срока действия патента: 23.07.2019 05.05.2022 (73) Патентообладатель(и): АББИСКО ТЕРАПЕУТИКС КО., ЛТД. (CN) Приоритет(ы): (30) Конвенционный приоритет: 14.09.2018 CN 201811073492.1 C 1 (85) Дата начала рассмотрения ...

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10-10-1999 дата публикации

Compound, pharmaceutical composition and method of inhibition of hiv-protease activity

Номер: RU2139280C1

FIELD: organic chemistry, biochemistry, pharmacy. SUBSTANCE: invention relates to compounds of the formula (I) where Q 3 - aryl or S-aryl possibly substituted with halogen atom, aryl - a carbocyclic aromatic 5-14-membered monocyclic or polycyclic residue; A - a carbocyclic aromatic 5-14-membered monocyclic or polycyclic residue, pyridine, pyridine-N-oxidyl, quinoline, isoquinoline, indole, indoline, thiazole-1,1-dioxide, thiophene or thiophene-1,1-dioxide; B - a carbocyclic aromatic 5-14-membered monocyclic or polycyclic residue involving nitrogen heteroatom, pyridylmethylpiperazine, octahydrothieno[3,2-c]pyridine or octahydrothieno[3,2-c] pyridine-1,1-dioxide; Q 1 ,Q 2 mean independently hydrogen atom or alkyl; Q 4-8 mean independently hydrogen atom, hydroxyl, halogen atom, nitro-, amino-, sulfonylamino-, alkylamino-group, alkyl possibly substituted with halogen atom, alkoxyl, the group -O-J (where J is a hydrolyzable group) or the group L 6 C(O)L 4 (where L 6 - a single bond or -O and L 4 - alkyl or alkoxyl); Y and G - oxygen atom; D - carbon or nitrogen atom being D atom is bound by a single bond with each of adjacent atoms of ring; E - carbon atom; Q 9 - hydrogen atom, or its pharmaceutically acceptable salt or a pharmaceutical composition based on said that inhibits activity of HIV-protease. EFFECT: compounds as inhibitors of HIV-protease. 63 cl, 3 tbl, 73 ex ОзЗсбз гс ПЧ Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ ВИ "” 2 139 280 ' С 070 217/06, 401/06, 495/04, С 07К 5/00, А 61 К 31/47, 38/02, (51) МПК 13) СЛ 38/07 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 96109378/04, 07.10.1994 (24) Дата начала действия патента: 07.10.1994 (30) Приоритет: 07.10.1993 1$ 08/133.543 07.10.1993 1$ 08/133.696 02.02.1994 ЦЗ 08/190.764 (46) Дата публикации: 10.10.1999 (56) Ссылки: ЗИ 1676454 АЗ, 1991. ЗЦ 1287532 А, 1990. ЕР 0346847 АЛ, 1989. ЕР 0361341 АЛ, 1990. ЕР 0490667 А2, 1992. \М!О 91108221 АЛ, 1991. (85) Дата перевода заявки ...

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13-06-1986 дата публикации

Substituted phenoxyurea, its preparation, herbicide containing same as an active intredient

Номер: JPS61126065A

(57)【要約】本公報は電子出願前の出願データであるた め要約のデータは記録されません。

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22-12-2020 дата публикации

FGFR inhibitor, preparation method and application thereof

Номер: CN112119064A
Принадлежит: Abbisko Therapeutics Co Ltd

一种具有式(I)结构的化合物和其制备方法,及其作为FGFR抑制剂,在治疗肿瘤、癌症、骨髓增生性疾病、骨骼或软骨细胞紊乱、低磷血症中的用途。

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28-09-2021 дата публикации

有机化合物的制造方法

Номер: CN109689611B
Принадлежит: Kaneka Corp

本公开提供一种不易受到使用溶剂的限制的使用了流动式反应器的含氯化合物的反应。在本公开中,将具有至少1个能与氯反应的官能团的反应底物和含氯化合物与碳原子数9~40的三烷基胺和有机溶剂一起供给至流动式反应器,使上述反应底物与含氯化合物反应,从而制造有机化合物,其中,上述能与氯反应的官能团选自羟基、硫醇基、氨基、羧基、及硫代羧基、酸酰胺基。

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16-07-2018 дата публикации

Guanidine compound

Номер: KR101879011B1

본 발명은, 의약 조성물, 특히, VAP-1 관련 질환의 예방 및/또는 치료용 의약 조성물의 유효 성분으로서 유용한 화합물을 제공한다. 본 발명자들은, VAP-1 저해 활성을 갖는 화합물에 대해서 예의 검토한 결과, 본 발명 화합물 또는 그의 염이, 우수한 VAP-1 저해 활성을 나타내어, VAP-1 관련 질환, 특히 당뇨병성 신증 혹은 당뇨병성 황반 부종의 예방 및/또는 치료에 유용한 것을 발견하여, 본 발명을 완성하였다. 또한, 본 발명은, 본 발명 화합물 또는 그의 염, 및 부형제를 함유하는 의약 조성물, 특히, VAP-1 관련 질환의 예방 및/또는 치료용 의약 조성물에 관한 것이다. The present invention provides a compound useful as an active ingredient of a pharmaceutical composition, particularly, a pharmaceutical composition for the prevention and / or treatment of VAP-1 related diseases. The present inventors have intensively studied a compound having VAP-1 inhibitory activity and found that the compound of the present invention or a salt thereof exhibits excellent VAP-1 inhibitory activity and is useful as a therapeutic agent for VAP-1 related diseases, particularly diabetic nephropathy or diabetic macular Which is useful for prevention and / or treatment of edema, thereby completing the present invention. The present invention also relates to a pharmaceutical composition containing the compound of the present invention or a salt thereof and an excipient, and particularly to a pharmaceutical composition for the prevention and / or treatment of VAP-1 related diseases.

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15-10-2019 дата публикации

A kind of preparation method of asymmetry thiourea

Номер: CN110330450A
Принадлежит: Wenzhou Medical University

本发明公开了一种不对称硫脲类化合物的制备方法,包括:在DMSO或DMF溶剂中,以胺类化合物与二硫化碳为底物,合成不对称硫脲类化合物。本发明方法通过三组份串联反应一步合成不对称硫脲类化合物。本发明反应原料廉价易得,制备方法简单。反应仅需要溶剂,不需要其它添加剂,产率高,操作简单,适用于不同类型的不对称硫脲类化合物的合成。本发明方法可用于合成一系列的不对称硫脲类化合物,合成的产物不仅可作为中间化合物,用于进一步构筑复杂的活性化合物;同时该类化合物具有极大的药物活性潜力。

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10-05-2017 дата публикации

Derivatives of pyrrolopyrimidine useful as jak-kinases inhibitors

Номер: RU2618673C2

FIELD: chemistry. SUBSTANCE: invention relates to a heterocyclic compound of the formula (I) or to its enantiomer, a diastereomer and a mixture thereof and a pharmaceutically acceptable salt thereof, wherein A: CH or N; L: bond or C 1-2 alkyl; R 1 is selected from hydrogen, C 1-4 alkyl, heteroaryl, - (CH 2 ) n C(O)OR 15 , -C(O)R 15 , -C(O)NR 16 R 17 , and -S(O) m R 15 , where each of alkyl or heteroaryl is possible is substituted with 1-3 groups selected from halogen, hydroxy, cyano, C 1-2 alkyl, C 1-2 alkoxy, C 3 cycloalkyl, C 6 aryl, pyridine and - (CH 2 ) n C(O)OR 15 ; R 2 or R 4 is independently selected from hydrogen and C 1-2 alkyl; R or R 3 is independently selected from hydrogen and halogen; R 5 or R 6 is independently selected from hydrogen and C 1-2 alkyl; R 7 , R 8 , R 9 or R 10 is independently selected from hydrogen, C 1-2 alkyl and hydroxyC 1-2 alkyl; R 11 , R 12 , R 13 or R 14 is independently selected from hydrogen or R 11 and R 12 or R 13 and R 14 taken together form an oxo group; R 15 is selected from C 1-4 alkyl, C 3 cycloalkyl, C 2 alkenyl, C 6 aryl and pyridine, wherein each of alkyl, cycloalkyl or heteroaryl is optionally substituted with 1 to 4 groups selected from halogen, hydroxy, cyano, C 1-4 alkoxy, C 6 aryl, tetrazole, -NR 19 R 20 , -S(O) m R 18 , -NHC(O)OR 18 and -NHS(O) m R 18 ; R 16 or R 17 is independently selected from hydrogen, C 1-3 alkyl and heteroaryl, wherein heteroaryl is optionally substituted by one selected from C 1-2 alkyl, hydroxy, C 1-2 alkoxy, C 3 cycloalkyl, hydroxyC 1 alkyl and-OR 18 ; R 18 is selected from C 1-4 alkyl and hydroxyC 1-4 alkyl; R 19 or R 20 is independently selected from the group consisting of hydrogen; M is 0, 1 or 2; N is 0 or 1; P is 0, 1 or 2; Q is 0 or 1; S is 1 or 2; And t is 1 or 2. The invention also relates to particular intermediates, a process for the preparation of a compound of formula (I), a pharmaceutical composition based on it, the use of a compound of formula (I), a method for ...

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13-01-2009 дата публикации

Flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof

Номер: US7476399B2
Принадлежит: Senomyx Inc

The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

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Flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof

Номер: US11268952B2
Принадлежит: Firmenich Inc

The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

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11-02-2020 дата публикации

Flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof

Номер: US10557845B2
Принадлежит: Firmenich Inc

The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

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28-02-2012 дата публикации

Flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof

Номер: US8124121B2
Принадлежит: Senomyx Inc

The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

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25-11-2014 дата публикации

Flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof

Номер: US8895050B2
Принадлежит: Senomyx Inc

The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

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28-08-2018 дата публикации

Flavors, flavor modifiers, tastants, taste enhancers, umami or sweet tastants, and/or enhancers and use thereof

Номер: US10060909B2
Принадлежит: Senomyx Inc

The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers,—savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

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05-01-2011 дата публикации

Modulators of ATP-binding cassette transporters

Номер: CN101935301A
Принадлежит: Vertex Pharmaceuticals Inc

本发明涉及ATP-结合弹夹(“ABC”)转运蛋白或其片段的调控剂、包括囊性纤维化跨膜电导调节剂、其组合物和与之有关的方法。本发明也涉及使用这类调控剂治疗ABC转运蛋白介导的疾病的方法。

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Автор: John Burnier, Thomas Gadek
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.

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22-12-2015 дата публикации

Modulators of cellular adhesion

Номер: US9216174B2
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 4 , n, p, A, B, D, E, L and AR 1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

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02-02-2016 дата публикации

Modulators of cellular adhesion

Номер: US9248126B2
Принадлежит: Sarcode Bioscience Inc

The present invention provides compounds having formula (I): and pharmaceutically acceptable derivatives thereof, wherein R 1 -R 4 , n, p, A, B, D, E, L and AR 1 are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of disorders mediated by the CD11/CD18 family of cellular adhesion molecules (e.g., LFA-1).

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