Настройки

Укажите год
-

Небесная энциклопедия

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

Подробнее
-

Мониторинг СМИ

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

Подробнее

Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Ведите корректный номера.
Укажите год
Укажите год

Применить Всего найдено 1498. Отображено 196.
27-04-2014 дата публикации

ПОЛИМОРФНЫЕ ФОРМЫ СОЕДИНЕНИЯ ST-246 И СПОСОБЫ ПОЛУЧЕНИЯ

Номер: RU2012144818A
Принадлежит: Сига Текнолоджиз, Инк

1. Полиморф формы I 4-трифторметил-N-(3,3а,4,4а,5,5а,6,6а-октагидро-1,3-диоксо-4,6-этеноциклопроп[f]изоиндол-2(1Н)-ил)бензамида (соединение ST-246), который демонстрирует картину рентгеновской порошковой дифракции, имеющую характеристические пики при угле отражения 2θ приблизительно 7,63, 10,04, 11,47, 14,73, 15,21, 15,47, 16,06, 16,67, 16,98, 18,93, 19,96, 20,52, 20,79, 22,80, 25,16, 26,53, 27,20, 27,60, 29,60, 30,23, 30,49, 30,68, 31,14, 33,65, 34,33, 35,29, 35,56, 36,30, 37,36, 38,42, 38,66 градусов.2. Полиморф по п.1, который представляет собой изолированный полиморф, и который является по меньшей мере приблизительно на 70% свободным от других форм, предпочтительно является по меньшей мере приблизительно на 80% свободным от других форм, более предпочтительно является по меньшей мере приблизительно на 90% свободным от других форм, еще более предпочтительно является по меньшей мере приблизительно на 95% свободным от других форм, в частности является по меньшей мере приблизительно на 99% свободным от других форм.3. Полиморф формы II 4-трифторметил-N-(3,3а,4,4а,5,5а,6,6а-октагидро-1,3-диоксо-4,6-этеноциклопроп[f]изоиндол-2(1Н)-ил)бензамида (соединение ST-246), который демонстрирует картину рентгеновской порошковой дифракции, имеющую характеристические пики при угле отражения 2θ в соответствии с фиг.2.4. Полиморф по п.3, который представляет собой изолированный полиморф, и который является по меньшей мере приблизительно на 70% свободным от других форм, предпочтительно является по меньшей мере приблизительно на 80% свободным от других форм, более предпочтительно является по меньшей мере приблизительно на 90% свободным от других форм, еще более предпочтительно является по меньшей мере приблизительно на 95% свободным от других форм, в частности является � РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (51) МПК A61K 31/44 (13) 2012 144 818 A (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2012144818/04, 23.03.2011 (71) ...

Подробнее
20-02-1992 дата публикации

INDENOINDOLVERBINDUNGEN

Номер: DD0000298388A5
Принадлежит: UNIV BATH, UNIVERSITY OF BATH,GB

Подробнее
24-07-1997 дата публикации

CARBAMATE DES INDAN-PYRROLIDINS

Номер: DE0069126612D1
Принадлежит: PFIZER, PFIZER INC., NEW YORK, N.Y., US

Подробнее
15-11-1995 дата публикации

Compounds

Номер: GB0009518572D0
Автор:
Принадлежит:

Подробнее
30-04-2015 дата публикации

Polymorphic forms ST-246 and methods of preparation

Номер: AP0000003221A
Принадлежит:

Подробнее
31-10-2012 дата публикации

Polymorphic forms ST-246 and methods of preparation

Номер: AP2012006514A0
Принадлежит:

Подробнее
31-03-1987 дата публикации

Process of production of derived from 2-oxindole-1-carboxamide.

Номер: OA0000008098A
Автор: KADIN SAUL BERNARD
Принадлежит:

Подробнее
28-02-1981 дата публикации

Derived from 1 (Omega, Omega, Omega-triarylalkyl) -4 - phényl-4- piperidin methanols, and their method of preparation.

Номер: OA0000005304A
Автор:
Принадлежит:

Подробнее
30-03-1971 дата публикации

Process for the preparation of compounds pentacyclic.

Номер: OA0000003608A
Автор:
Принадлежит:

Подробнее
31-10-2012 дата публикации

Polymorphic forms ST-246 and methods of preparation

Номер: AP0201206514A0
Принадлежит:

Подробнее
31-10-2012 дата публикации

Polymorphic forms ST-246 and methods of preparation

Номер: AP0201206514D0
Принадлежит:

Подробнее
15-04-2007 дата публикации

OXADIAZOLE WITH ANTIPROLIFERATIVER EFFECT

Номер: AT0000358676T
Принадлежит:

Подробнее
15-04-1978 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN STICKSTOFFHALTIGEN POLYCYCLISCHEN VERBINDUNGEN UND IHREN SAUREADDITIONSSALZEN

Номер: ATA170275A
Автор:
Принадлежит:

Подробнее
27-12-1978 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW ONES 1.1.1 - TRI ARYL ALKYL AMINES AND OF THEM SAEUREADDITIONS SALTS

Номер: AT0000347463B
Автор:
Принадлежит:

Подробнее
15-01-1990 дата публикации

THREE-CYCLIC OXINDOLE AS ANTI-INFLAMMATION MEANS.

Номер: AT0000049211T
Принадлежит:

Подробнее
15-05-1978 дата публикации

PROCEDURE FOR the PRODUCTION OF NEW ONE 1,1,1-TRIARYLALKYLAMINEN AND THEIR ACID ADDITION SALTS

Номер: AT0000278976A
Автор:
Принадлежит:

Подробнее
10-10-1973 дата публикации

Procedure for the production of new Indenopyrrolderivaten and their salts

Номер: AT0000310731B
Автор: NORMAN FRANK HAYES
Принадлежит:

Подробнее
25-01-1976 дата публикации

INSECTICIDES MEANS

Номер: AT0000334685B
Автор:
Принадлежит:

Подробнее
27-11-1978 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW NITROGENOUS ONES POLYCYCLI CONNECTIONS AND YOUR SAEUREADDITONSSALZEN

Номер: AT0000346839B
Автор:
Принадлежит:

Подробнее
26-02-1979 дата публикации

PROCEDURE FOR the PRODUCTION OF NEW ONE 1 - (TRI ARYL ALKYL) - 4-PHENYLPIPERIDINDERIVATEN AND THEIR SAEUREADDITIONSSALZEN

Номер: AT0000348525B
Автор:
Принадлежит:

Подробнее
15-05-1975 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN INDOLCARBONSAUREN, IHREN ESTERN UND SALZEN

Номер: ATA62074A
Автор:
Принадлежит:

Подробнее
15-06-1978 дата публикации

VERFAHREN ZUR HERSTELLUNG VON NEUEN 1,1,1-TRIARYLALKYLAMINEN UND DEREN SALZEN

Номер: ATA32178A
Автор:
Принадлежит:

Подробнее
15-03-2003 дата публикации

CONDENSED ISOINDOLONE AS PROTEIN KINASE C INHIBITORS

Номер: AT0000234284T
Принадлежит:

Подробнее
12-07-1971 дата публикации

Procedure for the production of new benzene sulphonyl urea and their salts

Номер: AT0000291274B
Автор:
Принадлежит:

Подробнее
30-07-2020 дата публикации

Novel metal complex, method for producing same, and method for producing gamma-lactam compound using same

Номер: AU2019205881A1
Принадлежит: Phillips Ormonde Fitzpatrick

The present invention relates to a novel metal complex, a method for producing same, and a method for producing a gamma-lactam compound using same, and the metal complex according to the present invention is used as a catalyst for producing a gamma-lactam compound and can efficiently produce a gamma-lactam compound with an excellent yield and excellent selectivity.

Подробнее
13-06-1989 дата публикации

N, 3-DISUBSTITUTED 2-OXINDOLE-1-CARBOXAMIDES AS ANALGESIC AND ANTIINFLAMMATORY AGENTS

Номер: CA1255658A
Принадлежит: PFIZER, PFIZER INC.

N,3-DISUBSTITUTED 2-OXINDOLE-1-CARBOXAMIDES AS ANALGESIC AND ANTIINFLAMMATORY AGENTS Certain 2-oxindole-1-carboxamide compounds having an acyl substituent at the 3-position, and also further suhstituted on the carboxamide nitrogen by an alkyl, cycloalkyl, phenyl or substituted phenyl group, are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and antiinflammatory agents in mammalian subjects. These 2-oxindole-1-carboxamide compounds are of particular value for ameliorating pain in human patients recovering from surgery or trauma, and alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects. Certain 2-oxindole-1-carboxamide compounds unsubstituted at C-3, but having a substituent on the carboxamide nitrogen, are useful as intermediates to the analgesic and antiinflammatory agents of the invention.

Подробнее
04-05-1982 дата публикации

TETRACYCLIC COMPOUNDS

Номер: CA1122976A
Принадлежит: AKZONA INC, AKZONA INCORPORATED

Biologically active tetracyclic compounds are disclosed of the formula or a pharmaceutically acceptable non-toxic acid addi.tion or quaternary ammonium nitrogen oxide. R1, R2, R3, and R4 are hydrogen, hydroxy, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, and trifluoromethyl; R5 is hy rogen C1-C6 alkyl or aralkyl having 7 to 10 carbon atoms; X is oxygen, sulfur,-CH2-, or -N?6 where R6 is hydrogen or C1-C4 alkyl and m is 1 or 2. These compounds are of interest because of their CNS-depressant activity and excellent antihistamine and antiserotonin activities.

Подробнее
08-11-1988 дата публикации

TRICYCLIC OXINDOLE ANTIINFLAMMATORY AGENTS

Номер: CA1244427A
Принадлежит: PFIZER, PFIZER INC.

TRICYCLIC OXINDOLE ANTIINFLAMMATORY AGENTS Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.

Подробнее
08-07-1975 дата публикации

PROCESS FOR PREPARING NOVEL INDOLYLACETIC ACID DERIVATIVES

Номер: CA970775A
Автор:
Принадлежит:

Подробнее
31-01-1978 дата публикации

N-PHENYLPYRROLES AND PROCESS FOR THEIR MANUFACTURE

Номер: CA1025455A
Автор:
Принадлежит:

Подробнее
10-02-1976 дата публикации

INDOLE-2-CARBOXYLIC ACID DERIVATIVES AND PROCESS FOR THEIR PREPARATION

Номер: CA983511A
Автор:
Принадлежит:

Подробнее
22-11-1977 дата публикации

9, 12-BRIDGED ETHENOANTHRACENES AND COMPOUNDS DERIVED THEREFROM

Номер: CA1021331A
Автор:
Принадлежит:

Подробнее
20-12-1988 дата публикации

2-OXOINDOLE 3-CARBOXAMIDE DERIVATIVE ANTIINFLAMMATORY AGENTS

Номер: CA0001247099A1
Автор: MELVIN LAWRENCE S JR
Принадлежит:

Подробнее
11-07-2019 дата публикации

NOVEL METAL COMPLEX, METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING GAMMA-LACTAM COMPOUND USING SAME

Номер: CA0003087522A1
Принадлежит: CASSAN MACLEAN IP AGENCY INC.

The present invention relates to a novel metal complex, a method for producing same, and a method for producing a gamma-lactam compound using same, and the metal complex according to the present invention is used as a catalyst for producing a gamma-lactam compound and can efficiently produce a gamma-lactam compound with an excellent yield and excellent selectivity.

Подробнее
20-03-2012 дата публикации

ISOINDOLINE DERIVATIVES

Номер: CA0002505029C
Принадлежит: MARUISHI PHARMACEUTICAL CO., LTD.

Provided is a novel isoindoline compound of the formula (I): (see formula I) The compound is useful for anesthesia by inducing sedation in a mammal.

Подробнее
20-05-2014 дата публикации

TETRAHYDROCYCLOPENTA[B]INDOLE COMPOUNDS AS ANDROGEN RECEPTOR MODULATORS

Номер: CA0002670340C
Принадлежит: ELI LILLY AND COMPANY, LILLY CO ELI

The present invention provides a compound of the formula: Formula (I) or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising aa compound of Formula (I) in combination with a suitable carrier, diluent, or excipient; and methods for treating physiological disorders, particularly reduced bones mass, osteoporosis, osteopenia, or reduced muscle mass or strength, comprising administering a compound of Formula (I), or a pharmaceutically acceptable salt thereof. X-17142.

Подробнее
12-09-1997 дата публикации

MCBI ANALOGS OF CC-1065 AND THE DUOCARMYCINS

Номер: CA0002246783A1
Принадлежит:

MCBI (7-methoxy-1,2,9,9a-tetra-hydrocyclopropa¢c!benz¢e!indol-4-one) is employable as a DNA alkylating agent and can be incorporated into analogs of CC-1065 and the duocarmycins for constructing regioselective DNA alkylating agents.

Подробнее
25-08-2009 дата публикации

SUBSTITUTED TRICYCLICS

Номер: CA0002269246C
Принадлежит: ELI LILLY AND COMPANY, LILLY CO ELI

Novel tricyclics of formula I (see formula I) wherein all variables are as described herein, are disclosed together with t he use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.

Подробнее
15-07-1976 дата публикации

Номер: CH0000577471A5
Автор:
Принадлежит: ALLEN & HANBURYS LTD, ALLEN & HANBURYS LTD.

Подробнее
30-06-1976 дата публикации

N-substd phenyl dicarboximides - insecticides useful against lepidoptera larvae, prepd. from an anhydride and an aniline

Номер: CH0000576744A5
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Title cpds. are of formula (I) (where R = phenyl which is monosubstituted by a methylene dioxy group or has 1-3 substituents selected from F, Cl, Br, I, CF3, NO2, CN, alkyl (1-4C) methoxy or methylthio, and Z1 & Z2 = H or together form a bond.).

Подробнее
28-06-1974 дата публикации

Tetrahydro dibenzo (3,4:6,7)cyclohepta(1,2-c)pyrroles - with CNS depressant, adrenolytic and histamine antagonist activity

Номер: CH0000550788A
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Cpds. of formula (I; R=H): (where X is H, Cl, CH3 or OCH3) are prepd. by hydrolysing (I; R= acyl or CN).

Подробнее
15-07-1974 дата публикации

VERFAHREN ZUR HERSTELLUNG VON 4B,8B,8C,8D-TETRAHYDRO-DIBENZO (A,F)CYCLOPROPA (CD)PENTALENVERBINDUNGEN.

Номер: CH0000551366A
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Подробнее
15-07-1974 дата публикации

VERFAHREN ZUR HERSTELLUNG VON 4B,8B,8C,8D-TETRAHYDRO-DIBENZO (A,F)CYCLOPROPA (CD)PENTALENVERBINDUNGEN.

Номер: CH0000551370A
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Подробнее
15-07-1974 дата публикации

VERFAHREN ZUR HERSTELLUNG VON 4B,8B,8C,8D-TETRAHYDRO-DIBENZO (A,F)CYCLOPROPA (CD)PENTALENVERBINDUNGEN.

Номер: CH0000551367A
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Подробнее
15-07-1974 дата публикации

VERFAHREN ZUR HERSTELLUNG VON 4B,8B,8C,8D-TETRAHYDRO-DIBENZO (A,F)CYCLOPROPA (CD)PENTALENVERBINDUNGEN.

Номер: CH0000551368A
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Подробнее
15-07-1974 дата публикации

Tetrahydro-dibenzo-cylopropapentalene antidepressants

Номер: CH0000551364A
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Pentalene anti-depressants. 4b, 8b, 8c, 8d-tetrahydro-dibenzo a.f -cyclopropa c.d -pentalene derivs. of formula I (where Ph1 and Ph2 = opt. substd. 1,2-phenylene; Alk = alkylene, Am = an opt. substd. amino gp., R1 = H, an ether or ester residue, an aliphatic, araliphatic or aromatic residue, or an alkylene bridge joined to Am; and R2 and R3 = H, OH, an ether, ester or an aliphatic residue) and their acyl derivs., N-oxides, quat. ammonium salts, and acid addn. salts, are new cmpds. of use as anti-depressants at 0.0001-0.75g/kg.

Подробнее
31-12-1975 дата публикации

Номер: CH0000570980A5
Автор: HAYES N F
Принадлежит: ALLEN & HANBURYS LTD, ALLEN & HANBURYS LTD.

Подробнее
30-09-1972 дата публикации

Bis-imide enthaltendes flammfestes Gemisch

Номер: CH0000528574A
Принадлежит: RAYCHEM CORP, RAYCHEM CORPORATION

Подробнее
15-07-1975 дата публикации

Номер: CH0000563978A5
Автор:

Подробнее
15-12-1981 дата публикации

Process for the preparation of 1-(triarylalkyl)-4-phenylpiperidine derivatives

Номер: CH0000626879A5
Принадлежит: SEARLE & CO, SEARLE, G.D., & CO.

Compounds of the formula III in which the substituents are defined in Claim 1, and their acid addition salts, are obtained by reacting a carbonyl compound of the formula II in the presence of an organic solvent with a suitable reducing agent, and converting resulting compounds of the formula III where appropriate into their acid addition salts. Corresponding alkanoyl esters can be obtained from compounds of the formula III by esterification. The compounds of the formula III and their alkanoyl esters generally have valuable pharmacological properties. They are, for example, effective antidiarrhoeal agents with only a very low or absolutely no analgesic effect. ...

Подробнее
15-06-1979 дата публикации

Номер: CH0000611605A5
Принадлежит: HOECHST AG

Подробнее
15-04-1977 дата публикации

Номер: CH0000586678A5
Автор:

Подробнее
15-04-1977 дата публикации

Номер: CH0000586677A5
Автор:
Принадлежит: BOEHRINGER MANNHEIM GMBH

Подробнее
13-05-1977 дата публикации

Номер: CH0000587816A5
Автор:
Принадлежит: BOEHRINGER MANNHEIM GMBH

Подробнее
15-09-1977 дата публикации

N-substd phenyl dicarboximides - insecticides useful against lepidoptera larvae, prepd. from an anhydride and an aniline

Номер: CH0000591207A5
Автор:
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Title cpds. are of formula (I) (where R = phenyl which is monosubstituted by a methylene dioxy group or has 1-3 substituents selected from F, Cl, Br, I, CF3, NO2, CN, alkyl (1-4C) methoxy or methylthio, and Z1 & Z2 = H or together form a bond.).

Подробнее
13-10-1978 дата публикации

Номер: CH0000605750A5
Принадлежит: DU PONT, DU PONT DE NEMOURS (E.I.) & CO.

Подробнее
31-10-1978 дата публикации

Номер: CH0000606222A5
Принадлежит: CIBA GEIGY AG, CIBA-GEIGY AG

Подробнее
15-04-1982 дата публикации

Process for the preparation of 1-(triarylalkyl)-4-phenylpiperidine derivatives

Номер: CH0000629190A5
Принадлежит: SEARLE & CO, SEARLE, G.D., & CO.

Compounds of the general formula I in which the substituents are defined in Claim 1, as well as their acid addition salts, are obtained by reacting a compound of the general formula II in which the substituents are defined in Claim 1, in the presence of an organic solvent with a suitable reducing agent to give compounds of the general formula III in which the substituents are defined in Claim 1, and subsequently treating resulting compounds of the general formula III in a suitable solvent with sodium hydride and then treating with an appropriate alkyl halide to form the required ether of the formula I, and converting resulting compounds of the general formula I where appropriate into their acid addition salts. The alkyl ethers of the formula I and their acid addition salts are effective antidiarrhoeal agents which have only a slight or even no analgesic effect.

Подробнее
15-04-1982 дата публикации

Process for the preparation of 1-(triarylalkyl)-4-phenylpiperidine derivatives

Номер: CH0000629191A5
Принадлежит: SEARLE & CO, SEARLE, G.D., & CO.

Compounds of the general formula I in which the substituents are defined in Claim 1, and their acid addition salts, are obtained by reacting a halide of the general formula A in which the substituents are defined in Claim 1, in a suitable inert solvent and in the presence of an acid acceptor, with an amine of the general formula B in which the substituents are defined in Claim 1, and converting resulting compounds of the general formula I where appropriate into their acid addition salts. The compounds of the formula I and their acid addition salts are effective antidiarrhoeal agents which have only a very small or even no analgesic effect.

Подробнее
29-07-1983 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW OF TETRACYCLI PYRIDIN OR PYRROLDERIVATE.

Номер: CH0000637382A5
Принадлежит: AKZO NV

Подробнее
15-12-1982 дата публикации

PROCEDURE FOR THE PRODUCTION OF NEW TETRACYCLI PIPERIDIN- ONES OR PYRROLIDINDERIVATE.

Номер: CH0000633536A5
Принадлежит: AKZO NV

Подробнее
30-11-1979 дата публикации

Process for the preparation of novel tertiary amines and their acid addition salts, and compounds thus prepared

Номер: CH0000614448A5
Принадлежит: SEARLE & CO, SEARLE, G.D., & CO.

Novel tertiary amines and their acid addition salts of the formula I in which the substituents have the meaning given in Claim 1, are prepared by reaction of an alkali metal-organic compound of the formula wherein M is the alkali metal atom, with the appropriate chloroalkyl or bromoalkyl compound of the formula in which Z is the halogen atom in question. The novel compounds of the formula I are valuable anti-diarrhoea agents, having only very slight, if any, analgesic side-effects.

Подробнее
28-11-2014 дата публикации

strigolaktonovye derivatives as compounds, regulating plant growth

Номер: EA0201400714A1
Автор:
Принадлежит:

Подробнее
30-04-2018 дата публикации

Tricyclic sulfones as modulators of γ-RoR deployment

Номер: EA0201792258A1
Автор:
Принадлежит:

Подробнее
27-04-2007 дата публикации

АМИДОСОЕДИНЕНИЯ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ФАРМАЦЕВТИЧЕСКИХ СРЕДСТВ

Номер: EA0200602062A1
Принадлежит:

Настоящее изобретение относится к ингибиторам 11-β-гидроксилстероиддегидрогеназы типа 1, антагонистам рецептора минералокортикоида (MR) и их фармацевтическим композициям. Соединения изобретения могут быть применимыми при лечении различных заболеваний, ассоциированных с экспрессией или активностью 11-β-гидроксилстероиддегидрогеназы типа 1 и/или заболеваний, ассоциированных с избытком альдостерона.

Подробнее
24-04-2003 дата публикации

ПРОИЗВОДНЫЕ БЕНЗО[3,4] ЦИКЛОБУТА [1,2-c] ПИРРОЛА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ ОБРАТНОГО ЗАХВАТА СЕРОТОНИНА

Номер: EA0000003302B1

... 1. Соединение формулы (I), имеющее цис-соединение колец в которой R1, R2и R3 , которые могут быть одинаковыми или различными, каждый независимо от других, представляет группу, выбранную из атома водорода, атома галогена, линейной или разветвленной (C1-C6 )алкоксигруппы, линейной или разветвленной (C1-C6)тригалогеналкильной группы, или два из R1, R2и R3в смежных положениях представляют (C1-C2)алкилендиоксигруппу; R4представляет группу, выбранную из атома водорода, линейной или разветвленной (C1-C6)алкильной группы, арил-(C1-C6 )алкильной группы, в которой алкильная часть является линейной или разветвленной; R5 представляет арильную группу, необязательно замещенную арильную группу, гетероарильную группу или необязательно замещенную гетероарильную группу; n представляет целое число от 1 до 2 включительно; его изомеры и аддитивные соли с фармацевтически приемлемой кислотой или основанием, причем имеется в виду, что циклоалкильная группа означает (C3-C8 )моноциклическую насыщенную кольцевую ...

Подробнее
14-12-2016 дата публикации

Heterocyclic compounds and organic light emitting diode

Номер: CN0102924364B
Автор:
Принадлежит:

Подробнее
16-03-1973 дата публикации

DIBENZOCYCLOPROPAPENTALENE COMPOUNDS, PROCESS FOR THEIR MANUFACTURE AND COMPOSITIONS CONTAINING THEM

Номер: FR0002024263B1
Автор: [UNK]
Принадлежит: Ciba Geigy AG

Подробнее
15-11-1974 дата публикации

CYCLOHEPTENE DERIVATIVES THEIR PREPARATION AND COMPOSITIONS CONTAINING SAME

Номер: FR0002126967B1
Автор:
Принадлежит:

Подробнее
18-10-1974 дата публикации

FUSED RING INDOLE DERIVATIVES AND A PROCESS FOR THE MANUFACTURE THEREOF

Номер: FR0002100677B1
Автор:
Принадлежит:

Подробнее
12-04-1974 дата публикации

Benzoindole and indanopyrrole derivs - analgesics and antiinflammator

Номер: FR0002096914B1
Автор:
Принадлежит:

Подробнее
12-06-1981 дата публикации

PRODUITS D'ADDITION DIENIQUES DE L'HEXACHLOROCYCLOPENTADIENE SUR DES IMIDES N-SUBSTITUES D'ACIDES DICARBOXYLIQUES INSATURES ET LEUR PROCEDE DE PREPARATION

Номер: FR0002470766A
Принадлежит:

LA PRESENTE INVENTION CONCERNE DE NOUVEAUX COMPOSES QUI SONT DES PRODUITS D'ADDITION DE L'HEXACHLOROCYCLOPENTADIENE SUR DES IMIDES N-SUBSTITUES D'ACIDES INSATURES DICARBOXYLIQUES REPONDANT A LA FORMULE GENERALE SUIVANTE: (CF DESSIN DANS BOPI) DANS LAQUELLE R EST H OU CH; R EST 2-CHN, 4-CHN OU CHY; Y EST OH, CL OU COOH; ET N EST EGAL A 0 OU 1, ET LEUR PROCEDE DE PREPARATION.

Подробнее
19-11-1965 дата публикации

Method of preparation of imides of acids polyhalopolyhydroalcanonaphtalenedicarboxylic, produced while resulting and their applications

Номер: FR0001418511A
Автор:
Принадлежит:

Подробнее
12-11-1976 дата публикации

DERIVED FROM (1 - (O, O, O-TRIARYLALKYL) - 4-PHENYL-4-PIPERIDIN) METHANOLS, THEIR PREPARATION AND THEIR THERAPEUTIC USE

Номер: FR0002307535A1
Автор:
Принадлежит:

Подробнее
16-09-2012 дата публикации

Plant growth regulating compounds

Номер: TW0201237038A
Принадлежит:

The present invention relates to novel strigolactam derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.

Подробнее
08-09-2006 дата публикации

PHOTOSENSITIZERS FOR TARGETED PHOTODYNAMIC THERAPY

Номер: WO2006093891A2
Принадлежит:

The present invention relates to photosensitizer compounds based on functionalized fullerenes useful in targeted photodynamic therapy (PDT), and methods of use thereof.

Подробнее
13-03-1986 дата публикации

TRICYCLIC OXINDOLE ANTIINFLAMMATORY AGENTS

Номер: WO1986001510A1
Принадлежит:

Tricyclic oxindole carboxamides, prepared by (a) reaction of an isocyanate with the basic ring system or (b) ammonolysis of a corresponding alkyl ester, are non-steroidal antiinflammatory agents useful in the treatment of rheumatoid arthritis.

Подробнее
07-02-1978 дата публикации

1-(3,3,3-Triarylalkyl)-4-phenyl-piperidinealkanols

Номер: US0004072686A1
Принадлежит: G. D. Searle & Co.

The present invention encompasses compounds of the formula см. иллюстрацию в PDF-документе and pharmaceutically acceptable acid addition salts thereof wherein the Alk is straight or branched chain alkylene containing 2-4 carbon atoms; M is alkylene having 1-4 carbon atoms; Ar and Ar' are phenyl, alkyl substituted phenyl wherein the alkyl contains from 1-4 carbon atoms or halo substituted phenyl; Ar" is phenyl, alkyl substituted phenyl wherein the alkyl contains 1-4 carbon atoms, halo substituted phenyl or pyridyl; X is hydrogen, halogen, trifluoromethyl or alkyl having from 1-4 carbon atoms; R is hydrogen alkyl having from 1-7 carbon atoms or an alkanoyl having from 2-5 carbon atoms. These compounds are potent antidiarrheal agents characterized by little, if any, central nervous system activity.

Подробнее
27-06-1972 дата публикации

FLAME RETARDANT COMPOSITIONS OF MATTER

Номер: US0003673149A1
Автор:
Принадлежит: UOP

Подробнее
31-08-1999 дата публикации

Antiparasitic agents

Номер: US0005945317A
Автор:
Принадлежит:

Novel compounds isolated from the fermentation of producing cultures of Nodulisporium sp. are antiparasitic and insecticidal agents.

Подробнее
23-10-2014 дата публикации

COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT AND PREVENTION OF ORTHOPOXVIRUS INFECTIONS AND ASSOCIATED DISEASES

Номер: US20140316145A1
Принадлежит: SIGA TECHNOLOGIES, INC.,

Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. 119-. (canceled)21. The process of claim 20 , wherein the ratio of compound 1(b) to 4-trifluoromethylbenzhydrazide is 0.89 to 1.22. The process of claim 20 , wherein the solvent is ethanol.23. The process of claim 20 , wherein the reaction occurs at above room temperature.24. The process of claim 20 , wherein the reaction occurs under argon.25. The process of claim 20 , wherein the solvent is removed by evaporation.26. The process of claim 20 , wherein N-[(3aR claim 20 ,4S claim 20 ,4aS claim 20 ,5aR claim 20 ,6R claim 20 ,6aS)-3 claim 20 ,3a claim 20 ,4 claim 20 ,4a claim 20 ,5 claim 20 ,5a claim 20 ,6 claim 20 ,6a-octahydro-1 claim 20 ,3-dioxo-4 claim 20 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide is further purified by chromatography.28. The method of claim 27 , wherein said first solvent comprises xylenes.29. The method of claim 27 , wherein said second solvent is ethanol. This application is a continuation-in-part of U.S. application Ser. No. 11/785,998 filed Apr. 23, 2007, which is a continuation-in-part of U.S. application Ser. No. 10/561,153 filed Apr. 5, 2006, now U.S. Pat. No. 7,737,168, which is a national stage filing of corresponding international application number PCT/US04/19552, filed on Jun. 18, 2004, which claims priority of U.S. Provisional Application No. 60/480,182, filed Jun. 20, 2003, all of which are hereby incorporated by reference in their entirety.This invention was made with U.S. government support under Grant No. 7R43AI056409 and Contract HHSN266200600014C awarded by the National Institute of Health (NIH). The U.S. Government has certain rights in the invention.The present invention relates to the ...

Подробнее
03-09-2019 дата публикации

Indomethacin analogs for the treatment of castrate-resistant prostate cancer

Номер: US0010398678B2

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Подробнее
19-03-2014 дата публикации

Номер: JP0005449351B2
Автор:
Принадлежит:

Подробнее
23-03-1989 дата публикации

Способ получения 2-оксиндол-1-карбоксамидов или их фармацевтически приемлемых солей

Номер: SU1468413A3
Принадлежит: ПФАЙЗЕР ИНК. (ФИРМА)

Изобретение касается гетероциклических соединений, в частности способа получения 2-оксиндол-1-карбок- саюадов общей формулы : M-C(0)R,, где И - группа формулы: 0 C- JH-R2 при X H,F,C1, 5- или б-СР,; R, - С -С -алкил, CF, , ,феноксиметил, С,- -С -циклоалкил, С,-С -фенилалкил, фтор- или хлорбенэил, фенил, хлорфе- НИЛ, пиридил, фурил, фурилметил. тиенил или тиенилметил; R - С.-С,-апкил , циклогексил, бензил, фенил, 2,4-дифторфенил, хлор- или метокси- или фторфенил, при условии, что когда X - Н, то при R, - СН,, или 4-хлорфенилу(, при R, CF , R, ,4-дифторфенилу, при R, - пиридил, RJ, it 4-хлорфенилу, при R, - фенил; R : фенилу или 4-хлорфенилу когда X - 5-хлор, то при R, - СН,, или циклогексилу, или их фармацевтически приемлемых солей, обладающих аиальгетической и противовоспалительной активностью, что может быть использовано в медицине. Цель - создание новых высокоактивных и малотоксичных соединений указанного класса. Синтез целевых веществ ведут реакцией .соединений общей формулы (II); М-Н ...

Подробнее
08-03-2012 дата публикации

Novel Indicator Platform

Номер: US20120058503A1
Принадлежит: Biosynth AG

A novel indicator platform comprises a plurality of 1H-lndol-3-yl indicator compounds that are capable of converting to a signalophore compound in response to an external stimulus. In one class of indicator compounds, the resulting signalophores are 2-benzylideneindoline compounds that are formed by an intermolecular Aldol-type process; in a further class of indicator compounds, the resulting signalophores are 10H-indolo[1,2-a]indole compounds that are formed by an intramolecular Aldol-type process. The indicators can be used in a wide array of applications relating, for example, to biological systems or optical data storage.

Подробнее
04-01-2018 дата публикации

TRICYCLIC SULFONES AS ROR GAMMA MODULATORS

Номер: US20180002358A1
Принадлежит:

There are described RORγ modulators of the formula (I), 10. The compound according to wherein{'sup': 1', '1a', '1a, 'sub': '1-6', 'Ris halo, phenyl substituted with 0-3 R, or Calkyl substituted with 0-3 R;'}{'sup': 1a', 'a', '2e', '2f', 'b', '2e', '2f', 'a, 'sub': 3', '1-6, 'Ris, independently at each occurrence, hydrogen, CF, halo, Calkyl substituted with 0-3 R, —(CRR)r-OR, and —(CRR)r-phenyl substituted with 0-3 R,'}{'sup': '1b', 'sub': 3', '3', '1', '4, 'Ris, independently at each occurrence, hydrogen, CD, halo, CF, and C-Calkyl;'}{'sup': 2', '2c', '2a', '2b', '2d', '11', '11', 'a, 'sub': 2', '1-6', '2', 'p, 'Ris hydrogen, SOR, Calkyl substituted with 0-3 R, COR, —C(O)R, —C(O)NRR; or a 5-7 membered heterocycle comprising carbon atoms, and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R,'}{'sup': 2a', 'a, 'sub': '1-6', 'Ris hydrogen or Calkyl substituted with 0-3 R;'}{'sup': 2b', 'a', 'a', '2e', '2f', 'a', '2e', '2f', 'a, 'sub': 1-6', '3-6', 'p, 'Ris hydrogen, Calkyl substituted with 0-2 R, Ccycloalkyl substituted with 0-3 R, —(CRR)r-5-7 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R, or —(CRR)r-phenyl substituted with 0-3 R;'}{'sup': 2c', 'a', 'a', 'a', 'a', '2e', '2f', 'a, 'sub': 1-6', '2-6', '3-10', '6-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Calkenyl substituted with 0-3 R, Ccycloalkyl substituted with 0-3 R, Caryl substituted with 0-3 R, or —(CRR)r-5-10-membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), substituted with 0-4 R;'}{'sup': 2d', 'd', '11', '11', 'd', '2e', '2f', 'a', 'a, 'sub': 1-6', '1-6', '3-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Chaloalkyl, C(O)NRR, Ccycloalkyl substituted with 0-2 R, (CRR)r-phenyl substituted with 0-2 R, or a 4-10 membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), ...

Подробнее
03-03-2016 дата публикации

STRIGOLACTAM DERIVATIVES AS PLANT GROWTH REGULATING COMPOUNDS

Номер: US20160060218A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel strigolactam derivatives, to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds. 1. A compound of Formula (II).whereinW is O or S;{'sub': 1', '3, 'R2 and R3 are independently hydrogen, or C-Calkyl;'}{'sub': 1', '3', '1', '3', '1', '3', '1', '3', '1', '3, 'R4 and R5 are independently hydrogen, halogen, nitro, cyano, C-Calkyl, C-Chaloalkyl, C-Calkoxy, hydroxyl, —OC(O)R9, amine, N—C-Calkyl amine, or N,N-di-C-Calkyl amine;'}{'sub': 1', '6', '1', '6', '1', '6, 'R9 is hydrogen, C-Calkyl, C-Calkoxy, or C-Chaloalkyl;'}{'sub': 1', '6', '1', '6', '1', '8', '1', '8', '1', '8', '1', '6', '1', '6', '1', '8', '1', '8', '1', '8, 'R8 is hydrogen, nitro, cyano, C-Calkyl, C-Chaloalkyl, halogen, C-Calkylthio, C-Chaloalkylthio, C-Calkylsulfinyl, N—C-Calkyl amine, N,N-di-C-Calkyl amine, C-Chaloalkylsulfinyl, C-Calkylsulfonyl, or C-Chaloalkylsulfonyl;'}{'sub': 1', '6', '1', '6', '1', '6', '1', '6', '1', '8', '1', '8, 'R1 is hydrogen, C-Calkoxy, hydroxyl, amine, N—C-Calkyl amine, N,N-di-C-Calkyl amine, C-Calkyl optionally substituted by one to five R10, C-Calkylcarbonyl, C-Calkoxycarbonyl, aryl optionally substituted by one to five R10, heteroaryl optionally substituted by one to five R10, or benzyl optionally substituted by one to five R10;'}{'sub': 1', '6', '1', '6', '1', '6', '2', '6', '2', '6, 'R10 is hydrogen, cyano, nitro, halogen, C-Calkyl, C-Calkoxy, C-Chaloalkyl, C-Calkenyl, or C-Calkynyl;'}{'sub': 1', '2', '3', '4', '1', '2', '3', '4', '1', '2', '3', '4, 'A, A, Aand Aare each independently C—X, C—Y or nitrogen, wherein each X or Y may be the same or different, and provided that no more than two of A, A, Aand Aare nitrogen and that at least one of A, A, Aand Ais C—X;'}{'sub': 1', '6', '1', '6', '1', '6', '1', '3', '1', '6', '1', '6, 'Y is hydrogen, halogen, cyano, hydroxyl, —OC(O)R9, ...

Подробнее
29-03-2018 дата публикации

FULLERENE DERIVATIVE AND LUBRICANT

Номер: US20180086771A1
Принадлежит:

A fullerene derivative, used as a lubricant, includes, in a molecule: a fullerene backbone; and n pyrrolidine rings each being condensed to the fullerene backbone, each of the pyrrolidine rings including one aryl group including a group including m perfluoropolyether chains, “m” being an integer from 2 to 5 and “n” being an integer from 1 to 5. 1. A fullerene derivative comprising , in a molecule:a fullerene backbone; andn pyrrolidine rings each being condensed to the fullerene backbone,each of the pyrrolidine rings including one aryl group including a group including m perfluoropolyether chains, “m” being an integer from 2 to 5 and “n” being an integer from 1 to 5.3. The fullerene derivative according to claim 2 , wherein the “R” is an alkyl group or an aryl group whose carbon number is less than or equal to 24.4. The fullerene derivative according to claim 1 , wherein the fullerene backbone is C.5. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains includes at least a partial structure selected from —(CF)O— in which “x” is an integer from 1 to 5.6. The fullerene derivative according to claim 5 , wherein the group including perfluoropolyether chains includes a partial structure expressed by —(CFCFO)(CFO)— in which each of “y” and “z” is an integer from 1 to 50.7. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains is configured only by a perfluoropolyether structure.8. The fullerene derivative according to claim 1 , wherein the group including perfluoropolyether chains is a straight-chain.9. A lubricant comprising the fullerene derivative according to .10. The lubricant according to claim 9 , further comprising a perfluoropolyether chemical compound that does not include a fullerene backbone. This application is a continuation-in-part application filed under 35 U.S.C. 111(a) claiming the benefit under 35 U.S.C. 120 and 365(c) of PCT International Application No. PCT ...

Подробнее
31-03-2016 дата публикации

FULLERENE DERIVATIVE AND N-TYPE SEMICONDUCTOR MATERIAL

Номер: US20160093807A1
Принадлежит:

The present invention is a material that exhibits excellent properties as an n-type semiconductor, in particular for use in organic thin-film solar cells. The present invention relates to a fullerene derivative represented by formula (1): 3. The fullerene derivative according to claim 2 , wherein Rand Rare the same or different claim 2 , and each represents a hydrogen atom or a fluorine atom;{'sup': 1a', '1b, 'at least one of Rand Ris a fluorine atom;'}{'sup': 1c', '1d, 'Rand Rare the same or different, and each represents a hydrogen atom or a fluorine atom;'}{'sup': 2', '2, 'i': a', 'b, 'Rand Rare the same or different, and each represents a hydrogen atom, a fluorine atom, alkyl, or alkoxy; and'}{'sup': 2', '2, 'i': c', 'd, 'Rand Reach represents a hydrogen atom.'}4. The fullerene derivative according to claim 1 , wherein the ring A is Cfullerene or Cfullerene.5. An n-type semiconductor material consisting of the fullerene derivative according to .6. The n-type semiconductor material according to claim 5 , which is for use in an organic thin-film solar cell.7. An organic power-generating layer comprising the n-type semiconductor material according to .8. A photoelectric conversion element comprising the organic power-generating layer according to .9. The photoelectric conversion element according to claim 8 , which is an organic thin-film solar cell. The present invention relates to a fullerene derivative, an n-type semiconductor material, and the like.Organic thin-film solar cells are formed by a coating technique with a solution of an organic compound, which is a photoelectric conversion material. The cells have various advantages: for example, 1) device production cost is low; 2) area expansion is easy; 3) the cells are more flexible than inorganic materials, such as silicon, thus enabling a wider range of applications; and 4) resource depletion is less likely. As such, organic thin-film solar cells have been developed, and the use of the bulk heterojunction ...

Подробнее
02-06-2022 дата публикации

NOVEL METAL COMPLEX, METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING GAMMA-LACTAM COMPOUND USING SAME

Номер: US20220168717A1
Принадлежит:

The present invention relates to a novel metal complex, a method for producing same, and a method for producing a gamma-lactam compound using same, and the metal complex according to the present invention is used as a catalyst for producing a gamma-lactam compound and can efficiently produce a gamma-lactam compound with an excellent yield and excellent selectivity. 3. The method of preparing a gamma-lactam compound of claim 1 , wherein the metal complex is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol-one compound.4. The method of preparing a gamma-lactam compound of claim 1 , wherein the base is one or two or more selected from NaBAr(sodium tetrakis [3 claim 1 ,5-bis (trifluoromethyl)phenyl]borate) claim 1 , AgSbF(silver hexafluoroantimonate(V)) claim 1 , AgNTf(silver bis(trifluoromethanesulfonyl)imide) claim 1 , AgBF(silver tetrafluoroborate) claim 1 , AgPF(silver hexafluorophosphate) claim 1 , AgOTf (silver trifluoromethanesulfonate) claim 1 , and AgOAc (silver acetate).5. The method of preparing a gamma-lactam compound of claim 1 , wherein the base is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol-one compound.6. The method of preparing a gamma-lactam compound of claim 1 , wherein the amidating is performed at 20 to 60° C.8. The method of preparing a gamma-lactam compound of claim 2 , wherein{'sub': a1', 'a5, 'Rto Rare independently of each other hydrogen, (C1-C20)alkyl, or (C3-C20)heterocycloalkyl;'}{'sub': a6', 'a5', 'a6, 'Ris independently of each other hydrogen, (C1-C20)alkyl, (C3-C20)cycloalkyl, (C2-C20)alkenyl, (C2-C20)alkynyl, (C6-C20)aryl, or (C3-C20)heteroaryl, or Rand Rmay be connected to form a (C5-C8)spiro ring,'}{'sub': a2', 'a3', 'a1', 'a2, 'Rand Rmay be connected by (C2-C10)alkenylene to form a (C6-C12)aromatic ring, and in this case, Rand Rare not present,'}{'sub': a3', 'a6, 'Rand Rmay be connected to each other to form a (C3-C20)alicyclic ring with or without an aromatic ring,'}{'sub': a3', 'a4', 'a6, 'Rand Rand ...

Подробнее
21-04-2016 дата публикации

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Номер: US20160107993A1
Принадлежит: Siga Technologies, Inc.

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 110.-. (canceled)11. A polymorph Form II of ST-246 which shows a X-ray powder diffraction pattern having characteristic peaks at a reflection angle 20 according to .12. An isolated polymorph according to that is at least about 70% free of other forms.13. An isolated polymorph according to that is at least about 80%% free of other forms.14. An isolated polymorph according to that is at least about 90% % free of other forms.15. An isolated polymorph according that is at least about 95% % free of other forms.16. An isolated polymorph according that is at least about 99% free of other forms.17. A pharmaceutical composition comprising the polymorph of and further comprising one or more pharmaceutically acceptable ingredients selected from the group consisting of carriers claim 11 , excipients claim 11 , diluents claim 11 , additives claim 11 , fillers claim 11 , lubricants and binders.18. The pharmaceutical composition of claim 17 , wherein the composition is formulated for oral administration.19. A method of treating Orthopoxvirus infections comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of .2021. A method of treating eczema vaccinatum comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of claim .2163.-. (canceled)64. A method of producing crystal polymorphic Form II of ST-246 claim 11 , comprising the steps of:a) dissolving ST-246 in at least one solvent to make a solution;b) cooling said solution to a temperature that causes the preferential crystallization of said ST-246 polymorphic Form II; andc) optionally drying the formed crystals of ST-246,wherein said solvent is selected from the group consisting of ethyl acetate, chloroform and 1- ...

Подробнее
13-05-2021 дата публикации

INHIBITORS OF METALLO-BETA-LACTAMASES

Номер: US20210137884A1
Принадлежит:

The present invention relates to compounds of Formula (I) that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection. (Formula (I)) 2. A compound of Formula I according to claim 1 , or a pharmaceutically acceptable salt or solvate thereof claim 1 , for use in the treatment of a bacterial infection in combination with a beta-lactam antibiotic.3. A compound according to any one of or claim 1 , wherein Ris selected from hydrogen or (1-4C)alkyl which is optionally substituted by one or more substituent groups selected from oxo claim 1 , halo claim 1 , or (1-2C)alkoxy.4. A compound according to any one of to claim 1 , wherein Ris hydrogen.5. A compound according to any one of to claim 1 , wherein Ris selected from:(i) —C(O)OH;{'sub': 2B', '2C', '2B', '2C, 'sup': 'A', '(ii) —C(O)NRR; wherein Rand Rare each independently selected from hydrogen, (1-6C)alkyl, (3-8C)cycloalkyl, aryl or heteroaryl, each of which is optionally substituted by one or more substituent groups R;'}{'sub': 2D', '2B', '2C', '2D', '2B', '2C, '(iii) —C(O)NRNRR; wherein Ris selected from hydrogen or (1-2C)alkyl and Rand Rare as defined above;'}(iv) tetrazolyl;{'sub': 2F', '2G', '2F', '2G', '2F', '2G, '(v) —B(OR)(OR), wherein Rand Rare each independently selected from hydrogen, (1-4C)alkyl or Rand Rare linked such that, together with the B and O atoms, they form a 5 or 6-membered heterocyclic ring, which is optionally substituted by (1-2C)alkyl; or'}(vi) cyano:{'sup': 'A', 'claim-text': {'br': None, 'sup': 2', '2, '—X—Z'}, 'and wherein Ris selected from halo, cyano, or a group of the formula [{'sup': '2', 'sub': '2', 'Xis absent or —C(O)—, —SO—; and'}, {'sup': '2', 'Zis hydrogen, (1-6C)alkyl, aryl, or heteroaryl;'}, {'sup': 2', 'A4', 'A5', 'A4', 'A5, 'and wherein Zis optionally further substituted by one or ...

Подробнее
13-05-2021 дата публикации

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Номер: US20210137885A1
Принадлежит: Siga Technologies, Inc.

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 1116.-. (canceled)117. A method of treating Orthopoxvirus infections comprising administering to a subject in need thereof a therapeutically effective amount of a polymorph Form I of 4-trifluoromethyl-N-(3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of about 7.63 , 10.04 , 11.47 , 14.73 , 15.21 , 15.47 , 16.06 , 16.67 , 16.98 , 18.93 , 19.96 , 20.52 , 20.79 , 22.80 , 25.16 , 26.5 3 , 27.20 , 27.60 , 29.60 , 30.23 , 30.49 , 30.68 , 31.14 , 33.65 , 34.33 , 35.29 , 35.56 , 36.30 , 37.36 , 38.42 , 38.66 degrees.118. The method of claim 117 , wherein the polymorph Form I is at least about 70% free of other forms.119. The method of claim 117 , wherein the polymorph Form I is at least about 80% free of other forms.120. The method of claim 117 , wherein the polymorph Form I is at least about 90% free of other forms.121. The method of claim 117 , wherein the polymorph Form I is at least about 95% free of other forms.122. The method of claim 117 , wherein the polymorph Form I is at least about 99% free of other forms.123. The method of claim 117 , wherein the polymorph Form I is administered orally.124. A method of treating eczema vaccinatum comprising administering to a patient in need thereof a therapeutically effective amount of a polymorph Form I of 4-trifluoromethyl-N-(3 claim 117 ,3a claim 117 ,4 claim 117 ,4a claim 117 ,5 claim 117 ,5a claim 117 ,6 claim 117 ,6a-octahydro-1 claim 117 ,3-dioxo-4 claim 117 ,6-ethenocycloprop[f]isoindol-2(1H)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of about 7.63 claim 117 , 10.04 claim 117 , ...

Подробнее
05-05-2016 дата публикации

FULLERENE DERIVATIVE AND N-TYPE SEMICONDUCTOR MATERIAL

Номер: US20160126462A1
Принадлежит:

The present invention is a material having excellent performance as an n-type semiconductor material, in particular for organic thin-film solar cells. 2. The n-type semiconductor material according to claim 1 , which is for use in an organic thin-film solar cell.3. An organic power-generating layer comprising the n-type semiconductor material according to and a p-type semiconductor material.4. The organic power-generating layer according to claim 3 , wherein the p-type semiconductor material consists of a donor-acceptor type π-conjugated polymer claim 3 , the donor-acceptor type π-conjugated polymer including as a donor unit benzodithiophene claim 3 , dithienosilole claim 3 , or N-alkyl carbazole and as an acceptor unit benzothiadiazole claim 3 , thienothiophene claim 3 , or thiophene pyrrole dione.5. The organic power-generating layer according to claim 4 , wherein the donor-acceptor type π-conjugated polymer is poly(thieno[3 claim 4 ,4-b]thiophene-co-benzo[1 claim 4 ,2-b:4 claim 4 ,5-b′]thiophene) claim 4 , or poly(dithieno[1 claim 4 ,2-b:4 claim 4 ,5-b′][3 claim 4 ,2-b:2′ claim 4 ,3′-d]silole-alt-(2 claim 4 ,1 claim 4 ,3-benzothiadiazole).6. The organic power-generating layer according to claim 4 , wherein the donor-acceptor type π-conjugated polymer is poly(thieno[3 claim 4 ,4-b]thiophene-co-benzo[1 claim 4 ,2-b:4 claim 4 ,5-b′]thiophene).7. The organic power-generating layer according to claim 3 , wherein the p-type semiconductor material is poly-3-hexylthiophene claim 3 , or poly[[4 claim 3 ,8-bis[(2-ethylhexyl)oxy]benzo[1 claim 3 ,2-b:4 claim 3 ,5-b′]dithiophene-2 claim 3 ,6-diyl][3-fluoro-2-[(2-ethylhexyl)carbonyl]thieno[3 claim 3 ,4-b]thiophenediyl]].8. The organic power-generating layer according to claim 3 , further comprising diiodooctane.9. A photoelectric conversion element comprising the organic power-generating layer according to .10. The photoelectric conversion element according to claim 9 , which is an organic thin-film solar cell. The present ...

Подробнее
10-05-2018 дата публикации

AMORPHOUS TECOVIRIMAT PREPARATION

Номер: US20180125819A1
Принадлежит: Siga Technologies, Inc.

Disclosed are methods for the preparation of amorphous N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide. 122-. (canceled)23. A method for producing amorphous solid dispersion of N-[(3aR ,4R ,4aR ,5aS ,6S ,6aS)-3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide , said method comprising:(a) heating a solid form of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide in the presence of at least one polymer at a temperature sufficient to cause melting and produce a liquid solution; and(b) cooling the solution of step (a) and thus producing said amorphous dispersion.24. The method of claim 23 , wherein said polymer is selected from the group consisting of: Polyethylene glycol claim 23 , Gelucire claim 23 , Glycerol mono and di stearate claim 23 , methacrylic acid copolymer claim 23 , Hydroxypropyl methyl cellulose (HPMC) claim 23 , HPMCP-H55 claim 23 , CAP claim 23 , PVAP claim 23 , HPMCAS-L claim 23 , HPMCAS-M claim 23 , HPMCAS-H claim 23 , Hypromellose claim 23 , HPC claim 23 , Poloxamer claim 23 , PVP-VA claim 23 , PVP (neutral) claim 23 , hydroxypropyl cellulose claim 23 , methyl cellulose claim 23 , ethyl cellulose claim 23 , and mixtures thereof.25. The method of claim 24 , wherein said polymer is Polyethylene glycol.26. The method of claim 23 , wherein said liquid solution comprises a surfactant.27. The method of claim 26 , wherein said ...

Подробнее
21-05-2015 дата публикации

Method Of Preparing Fused Ring Indeno Compounds

Номер: US20150141662A1
Принадлежит: TRANSITIONS OPTICAL, INC.

The present invention relates to methods of preparing fused ring indeno compounds that involves reacting together a dienophile and a lactone compound, in the presence of a catalyst, and a carboxylic acid anhydride. With some embodiments, the fused ring indeno compound is represented by the following Formula (I-A), the dienophile is represented by the following Formula (II-A), and the lactone compound is represented by the following Formula (III-A): 3. The method of wherein claim 2 , the metal M of Formula (V) and Formula (VI) is independently selected from Bi claim 2 , B claim 2 , Al claim 2 , Hf claim 2 , Sc claim 2 , Cu claim 2 , Yb claim 2 , Ti claim 2 , Sn claim 2 , Fe claim 2 , Zn claim 2 , Ag claim 2 , Y claim 2 , In claim 2 , Nb and Mg claim 2 , Ris selected from C-Clinear or branched alkyl claim 2 , and C-Clinear or branched perfluoroalkyl claim 2 , and X is selected from F claim 2 , Cl claim 2 , I claim 2 , and Br.4. The method of wherein said method is conducted in the presence of a solvent claim 1 , said solvent being selected from benzene claim 1 , toluene claim 1 , xylene claim 1 , methylene chloride claim 1 , 1 claim 1 ,2-dichloroethane claim 1 , C-Clinear or branched perhaloalkyl claim 1 , acetonitrile claim 1 , nitromethane claim 1 , and combinations thereof.6. The method of wherein for Formula (I-B) and Formula (II-B) Zis N—R claim 5 , and Ris claim 5 , or is converted to claim 5 , a group L represented by the following Formula (VII) claim 5 , and{'sup': '1', 'claim-text': {'br': None, 'sub': 1', 'c', '1', '2', 'd', 'd′', '2', '3', 'e', 'e′', '3', '4', 'f', 'f′', '5, '—[S]-[Q-[S]]-[Q-[S]]-[Q-[S]]—S—P\u2003\u2003Formula (VII)'}, 'optionally for Formula (I-B) at least one Rindependently for each n, is selected from said group L represented by the following Formula (VII),'}wherein:{'sub': 1', '2', '3, '(a) Q, Q, and Qfor each occurrence, are independently selected from a divalent group selected from optionally substituted aryl, optionally substituted ...

Подробнее
09-05-2019 дата публикации

SUBSTITUTED (1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS

Номер: US20190135752A1
Принадлежит:

The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. 158-. (canceled)60. The process according to claim 59 , wherein n is 1.61. The process according to claim 59 , wherein Y is CR.62. The process according to claim 61 , wherein Ris H or C-Chaloalkyl.63. The process according to claim 61 , wherein Ris H or trifluoromethyl.64. The process according to claim 59 , wherein Ris selected from the group consisting of H claim 59 , cyano claim 59 , C-Chaloalkoxy and C-Chaloalkyl.65. The process according to claim 59 , wherein Ris selected from the group consisting of H claim 59 , cyano claim 59 , trifluoromethoxy and trifluoromethyl.66. The process according to claim 59 , wherein Ris selected from the group consisting of cyclobutyl claim 59 , cyclohexyl claim 59 , cyclopentyl claim 59 , and cyclopropyl.67. The process according to claim 59 , wherein Z is CR.68. The process according to claim 67 , wherein Ris selected from the group consisting of H claim 67 , cyano claim 67 , C-Chaloalkoxy and C-Chaloalkyl.69. The process according to claim 67 , wherein Ris selected from the group consisting of H claim 67 , cyano claim 67 , trifluoromethoxy and trifluoromethyl. The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple ...

Подробнее
02-06-2016 дата публикации

AMORPHOUS TECOVIRIMAT PREPARATION

Номер: US20160152565A1
Принадлежит: Siga Technologies, Inc.

Disclosed are methods for the preparation of amorphous N-[(aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus. Also disclosed are methods for the preparation of amorphous solid dispersion of N-[(aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1 H)-yl]-4-(trifluoromethyl)-benzamide. 1. A method for producing amorphous N-[(3aR ,4R ,4aR ,5aS ,6S ,6aS)-3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide , said method comprising:(a) heating a solid form of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide at a temperature sufficient to cause melting; and(b) cooling the melted form of N-[(3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide and thus producing amorphous N-[( 3aR,4R,4aR,5aS,6S,6aS)-3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl]-4-(trifluoromethyl)-benzamide.2. The method of claim 1 , wherein said heating is carried out at a temperature of at least about 196° C.3. The method of claim 1 , wherein said heating is carried out at a temperature of up to about 230° C.4. The method of claim 1 , wherein said heating is carried out at a temperature from about 196° C. to about 230° C.5. The method of claim 1 , wherein said cooling step is carried out at a temperature below about 0° C.6. The method of claim 1 , wherein said cooling step is carried out at a temperature of less than about −50 ° C.7. The method of claim 1 , wherein said cooling step is carried out in liquid nitrogen.8. The method of claim 1 ...

Подробнее
02-06-2016 дата публикации

TRICYCLIC PYRROLE COMPOUNDS, THEIR PREPARATION AND USE IN MEDICAMENTS

Номер: US20160152566A1
Принадлежит:

The invention refers to compounds of general formula (I) 2. The compound according to claim 1 , wherein Ris selected from —COOR claim 1 , —CONHR claim 1 , —CONRR claim 1 , more preferably it is —COOR.3. The compound according to of claim 2 , wherein Ris —COOH or a salt thereof.4. The compound according to claim 1 , wherein Ris hydrogen.5. The compound according to claim 1 , wherein Ris substituted or unsubstituted alkenyl claim 1 , preferably unsubstituted alkenyl.6. The A compound according to claim 5 , wherein Ris 1-propenyl.7. The compound according to claim 1 , Ris substituted or unsubstituted alkenyl claim 1 , preferably unsubstituted alkenyl.8. The compound according to claim 7 , wherein Ris 1-propenyl.10. A process for the preparation of a compound of formula general (I) as defined in claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , or solvate thereof claim 1 , wherein the process comprises the step of isolating a compound of formula (I) above from a culture broth of a microorganism.11Paraconiothyrium. The process according to claim 10 , wherein the microorganism is a fungal strain claim 10 , more preferably a sp.12Paraconiothyrium. The process according to claim 11 , wherein the fungal strain is sp. HL-78-gCHSP3-B005 which has been deposited in the Colección Española de Cultivos Tipo at the Universidad de Valencia claim 11 , Spain under the accession number CECT 20841.13. A pharmaceutical composition comprising at least one compound of general formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , or solvate thereof and a pharmaceutically acceptable excipient.14. A method for inhibiting angiogenesis in a subject comprising administering to the subject a compound of general formula (I) as defined in claim 1 , or a pharmaceutically acceptable salt claim 1 , stereoisomer claim 1 , or solvate thereof.15. The method according to claim 14 , for the treatment and/or prophylaxis of ...

Подробнее
12-07-2018 дата публикации

Polymorphic forms of st-246 and methods of preparation

Номер: US20180193308A1
Принадлежит: Siga Technologies Inc

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.

Подробнее
19-08-2021 дата публикации

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Номер: US20210251960A1
Принадлежит:

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects. 3. The method of claim 1 , wherein the AKR1C3 polypeptide is present within a subject.4. The method of claim 3 , wherein the subject is a mammal.5. The method of claim 3 , wherein the subject is a male and the AKR1C3 polypeptide is present in the prostate of the subject.6. The method of claim 5 , wherein the prostate of the subject comprises a tumor claim 5 , optionally a castrate-resistant tumor.9. The method of claim 7 , wherein the subject is a mammal.10. The method of claim 9 , wherein the subject is a male and the undesirable AKR1C3 biological activity is present in a tumor claim 9 , optionally a castrate-resistant tumor claim 9 , present in the prostate of the subject.13. The method of claim 11 , wherein the prostate tumor is a castrate-resistant prostate tumor.14. The method of claim 11 , wherein the administering is via a route selected from the group consisting of peroral claim 11 , intravenous claim 11 , intraperitoneal claim 11 , inhalation claim 11 , intraprostatic claim 11 , and intratumoral. This application is a divisional of U.S. patent application Ser. No. 16/530,907, filed Aug. 2, 2019 (pending), which itself is a divisional of U.S. patent application Ser. No. 15/899,171, filed Feb. 19, 2018 (now U.S. Pat. No. 10,398,678), which itself is a U.S. patent application Ser. No. 15/132,937, filed Apr. 19, 2016 (now U.S. Pat. No. 9,895,351), which itself is a continuation of U.S. patent application Ser. No. 14/352,421, filed Apr. 17, ...

Подробнее
16-08-2018 дата публикации

COMPOUNDS FOR THE INHIBITION OF CYCLOPHILINS AND USES THEREOF

Номер: US20180230162A1
Принадлежит:

The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of cyclophilins, and for the treatment of cyclophilin-related disorders. 117-. (canceled)19. The method of claim 18 , wherein the disease or disorder is selected from viral infections claim 18 , inflammation claim 18 , neurologic disorders claim 18 , cardiac failure and cancer.20. The method of claim 18 , wherein the disease or disorder is selected from Alzheimer's disease claim 18 , Parkinson's disease claim 18 , Amyotrophic Lateral Sclerosis (ALS) claim 18 , Dementia claim 18 , Multiple Sclerosis claim 18 , and Huntington's disease.21. The method of claim 18 , wherein each R′ is independently —R claim 18 , —OR claim 18 , or —N(R).22. The method of claim 21 , wherein each R′ is independently H claim 21 , -Me claim 21 , -Et claim 21 , —OH claim 21 , or —NH.23. The method of claim 18 , wherein X is CH.24. The method of claim 18 , wherein X claim 18 , and the bonds attached to X claim 18 , are absent.25. The method of claim 18 , wherein each Ris independently H claim 18 , Me claim 18 , or -Et.26. The method of claim 25 , wherein each Ris independently —H or -Me.27. The method of claim 18 , wherein Rand Rtaken together with the atom to which they are attached form a cyclopropyl claim 18 , cyclobutyl claim 18 , cyclopentyl claim 18 , or cyclohexyl claim 18 , each of which is optionally substituted. This application claims the benefit of U.S. Provisional application No. 62/315,890, filed on Mar. 31, 2016, the content of which is incorporated in its entirety by reference.The present invention relates to dioxo-hexahydroisoindolyl compounds useful as inhibitors of Cyclophilins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.Cyclophilins or peptidyl-prolyl isomereases (PPAses) are widely expressed enzymes which ...

Подробнее
13-11-2014 дата публикации

Strigolactam derivatives as plant growth regulating compounds

Номер: US20140336052A1
Принадлежит: SYNGENTA PARTICIPATIONS AG

The present invention relates to novel strigolactam derivatives of formula (I), to processes and intermediates for preparing them, to plant growth regulator compositions comprising them and to methods of using them for controlling the growth of plants and/or promoting the germination of seeds.

Подробнее
08-08-2019 дата публикации

Tricyclic sulfones as ror gamma modulators

Номер: US20190241588A1
Принадлежит: Bristol Myers Squibb Co

There are described RORγ modulators of the formula (I), and formula (II) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.

Подробнее
27-09-2018 дата публикации

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Номер: US20180271835A1
Принадлежит:

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects. 519-. (canceled)20. A method for inhibiting a biological activity of an aldo-keto reductase family 1 claim 1 , member C3 (AKR1C3) polypeptide claim 1 , the method comprising contacting the AKR1C3 polypeptide with an effective amount of a compound of .22. The method of claim 20 , wherein the AKR1C3 polypeptide is present within a subject.23. The method of claim 22 , wherein the subject is a mammal.24. The method of claim 22 , wherein the subject is a male and the AKR1C3 polypeptide is present in the prostate of the subject.25. The method of claim 24 , wherein the prostate of the subject comprises a tumor claim 24 , optionally a castrate-resistant tumor.26. A method for inhibiting undesirable aldo-keto reductase family 1 claim 1 , member C3 (AKR1C3) biological activity in a subject claim 1 , the method comprising administering to the subject an effective amount of a compound of .28. The method of claim 26 , wherein the subject is a mammal.29. The method of claim 28 , wherein the subject is a male and the undesirable AKR1C3 biological activity is present in a tumor claim 28 , optionally a castrate-resistant tumor claim 28 , present in the prostate of the subject.30. A method for treating a prostate tumor in a subject claim 1 , the method comprising administering the subject a therapeutically effective amount of a compound of .32. The method of claim 30 , wherein the prostate tumor is a castrate-resistant prostate tumor.33. The method of claim 30 , ...

Подробнее
18-12-2014 дата публикации

Indomethacin analogs for the treatment of castrate-resistant prostate cancer

Номер: US20140371261A1

Provided are compositions for inhibiting a biological activity of an aldoketo reductase family 1, member C3 (AKR1 C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1 C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Подробнее
25-12-2014 дата публикации

Aromatic amine derivative and organic electroluminescence element using same

Номер: US20140374720A1
Принадлежит: Idemitsu Kosan Co Ltd

An aromatic amine derivative represented by formula (1): wherein L 1 , L 2 , Ar 1 , Ar 2 , R 1 , R 2 , a, b, and Q are as defined in the specification. An organic electroluminescence device having at least one organic thin film layer which includes the aromatic amine derivative has high emission efficiency and long lifetime.

Подробнее
05-10-2017 дата публикации

COMPOUNDS FOR THE INHIBITION OF CYCLOPHILINS AND USES THEREOF

Номер: US20170283427A1
Принадлежит:

The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of cyclophilins, and for the treatment of cyclophilin-related disorders. 2. The compound of claim 1 , wherein Ring A is phenyl.3. The compound of claim 2 , wherein Ring A is phenyl which is fused with a 7-9 membered saturated or partially unsaturated heterocyclic mono- or bicyclic ring having 1-3 heteroatoms independently selected from nitrogen claim 2 , oxygen claim 2 , or sulfur; which is optionally substituted.4. The compound of claim 1 , wherein each R′ is independently —R claim 1 , —OR claim 1 , or —N(R).5. The compound of claim 4 , wherein each R′ is independently H claim 4 , -Me claim 4 , -Et claim 4 , —OH claim 4 , or —NH.7. The compound of claim 1 , wherein X is CH.8. The compound of claim 1 , wherein X is O.9. The compound of claim 1 , wherein X claim 1 , and the bonds attached to X claim 1 , are absent.10. The compound of claim 1 , wherein each Ris independently —H or -Me.11. The compound of claim 1 , wherein Rand Rtaken together with the atom to which they are attached form a cyclopropyl claim 1 , cyclobutyl claim 1 , cyclopentyl claim 1 , or cyclohexyl claim 1 , each of which is optionally substituted.16. The compound of claim 1 , selected from Table 1.17. A pharmaceutical composition comprising a compound of claim 1 , and a pharmaceutically acceptable adjuvant claim 1 , carrier claim 1 , or vehicle.18. A method for treating a cyclophilin-mediated disease or disorder in a subject in need thereof claim 1 , comprising the step of administering to said subject a compound of .19. The method of claim 18 , wherein the disease or disorder is selected from viral infections claim 18 , inflammation claim 18 , neurologic disorders claim 18 , cardiac failure and cancer.20. The method of claim 18 , wherein the disease or disorder is selected from Alzheimer's disease claim 18 , Parkinson's disease claim 18 , Amyotrophic Lateral Sclerosis (ALS) claim ...

Подробнее
20-10-2016 дата публикации

Indomethacin analogs for the treatment of castrate-resistant prostate cancer

Номер: US20160303082A1

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects.

Подробнее
05-11-2015 дата публикации

MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES

Номер: US20150318478A1
Принадлежит:

The present invention describes indenocarbazole derivatives having electron- and hole-transporting properties, in particular for use in the emission and/or charge-transport layer of electroluminescent devices or as matrix material. The invention furthermore relates to a process for the preparation of the compounds according to the invention and to electronic devices comprising same. 116-. (canceled)19. The compound according to claim 17 , wherein R is selected from H claim 17 , D claim 17 , N(Ar) claim 17 , a substituted or unsubstituted arylamine claim 17 , a straight-chain alkyl group having 1 to 20 C atoms claim 17 , a branched alkyl group having 3 to 20 C atoms claim 17 , or an aromatic or heteroaromatic ring system having 5 to 40 ring atoms.20. The compound according to claim 19 , wherein the aromatic or heteroaromatic ring system here is selected from substituted or unsubstituted phenyl claim 19 , naphthyl claim 19 , pyridine claim 19 , triazine claim 19 , pyrimidine claim 19 , benzimidazole claim 19 , thiophene claim 19 , triphenylamine or combinations of these groups.21. The compound according to claim 17 , wherein Ris selected on each occurrence claim 17 , independently of one another claim 17 , from alkyl claim 17 , substituted or unsubstituted triazine claim 17 , pyridine claim 17 , pyrimidine claim 17 , pyrazine claim 17 , phenyl claim 17 , biphenyl claim 17 , terphenyl claim 17 , naphthyl claim 17 , anthracenyl and carbazole claim 17 , and two radicals Rwhich are bonded to the same C atom together with the atom(s) to which they are bonded may also form an aliphatic claim 17 , aromatic or heteroaromatic ring.22. An electronic device comprising at least one compound according to .23. An organic electroluminescent device which comprises the compound according claim 17 , to is employed in an emitting layer and/or as electron-transport material and/or as hole-transport material and/or as hole-injection material and/or as hole-blocking material.24. An ...

Подробнее
01-11-2018 дата публикации

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Номер: US20180311213A1
Принадлежит: Siga Technologies, Inc.

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 1138-. (canceled)139. A polymorph Form IV of 4-trifluoromethyl-N-(3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of 6.97 , 9.75 , 11.21 , 12.13 , 13.54 , 16.82 , 18.17 , 18.79 , 19.69 , 20.51 , 23.31 , 24.78 , 27.24 , 30.20 , and 33.52 degrees.140. An isolated polymorph according to that is at least about 70% free of other forms.141. An isolated polymorph according to that is at least about 80% free of other forms.142. An isolated polymorph according to that is at least about 90% free of other forms.143. An isolated polymorph according that is at least about 95% free of other forms.144. An isolated polymorph according that is at least about 99% free of other forms.145. A pharmaceutical composition comprising the polymorph of and further comprising one or more pharmaceutically acceptable ingredients selected from the group consisting of carriers claim 139 , excipients claim 139 , diluents claim 139 , additives claim 139 , fillers claim 139 , lubricants and binders.146. The pharmaceutical composition of claim 145 , wherein the composition is formulated for oral administration.147. Use of the polymorph of in the preparation of a medicament for treating Orthopoxvirus infections.148. Use of the polymorph of in the preparation of a medicament for treating eczema vaccinatum.149. A method of producing crystal polymorphic Form IV of ST-246 claim 139 , comprising the steps of: 'dissolving 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide (ST-246) in at least one solvent to make a solution wherein said solvent is selected from the group ...

Подробнее
10-11-2016 дата публикации

TRICYCLIC SULFONES AS RORy MODULATORS

Номер: US20160326195A1
Принадлежит:

There are described RORγ modulators of the formula (I), 10. A compound according to wherein{'sup': 1', '1a', '1a, 'sub': '1-6', 'Ris halo, phenyl substituted with 0-3 R, or Calkyl substituted with 0-3 R;'}{'sup': 1a', 'a', '2e', '2f', 'b', '2e', '2f', 'a, 'sub': 3', '1-6, 'Ris, independently at each occurrence, hydrogen, CF, halo, Calkyl substituted with 0-3 R, —(CRR)r-OR, and —(CRR)r-phenyl substituted with 0-3 R,'}{'sup': '1b', 'sub': 3', '3', '1', '4, 'Ris, independently at each occurrence, hydrogen, CD, halo, CF, and C-Calkyl;'}{'sup': 2', '2c', '2a', '2b', '2d', '11', '11', 'a, 'sub': 2', '1-6', '2', 'p, 'Ris hydrogen, SOR, Calkyl substituted with 0-3 R, COR, —C(O)R, —C(O)NRR; or a 5-7 membered heterocycle comprising carbon atoms, and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R,'}{'sup': 2a', 'a, 'sub': '1-6', 'Ris hydrogen or Calkyl substituted with 0-3 R;'}{'sup': 2b', 'a', 'a', '2e', '2f', 'a', '2e', '2f', 'a, 'sub': 1-6', '3-6', 'p, 'Ris hydrogen, Calkyl substituted with 0-2 R, Ccycloalkyl substituted with 0-3 R, —(CRR)r-5-7 membered heterocycle comprising carbon atoms and 1-4 heteroatoms selected from N, O, P(═O) and S(O)substituted with 0-4 R, or —(CRR)r-phenyl substituted with 0-3 R;'}{'sup': 2c', 'a', 'a', 'a', 'a', '2e', '2f', 'a, 'sub': 1-6', '2-6', '3-10', '6-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Calkenyl substituted with 0-3 R, Ccycloalkyl substituted with 0-3 R, Caryl substituted with 0-3 R, or —(CRR)r-5-10-membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), substituted with 0-4 R;'}{'sup': 2d', 'd', '11', '11', 'd', '2e', '2f', 'a', 'a, 'sub': 1-6', '1-6', '3-10', 'p, 'Ris, independently at each occurrence, hydrogen, Calkyl substituted with 0-3 R, Chaloalkyl, C(O)NRR, Ccycloalkyl substituted with 0-2 R, (CRR)r-phenyl substituted with 0-2 R, or a 4-10 membered heterocycle containing 1-4 heteroatoms selected from N, O, P(═O) and S(O), ...

Подробнее
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. ...

Подробнее
15-10-2020 дата публикации

THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION

Номер: US20200325124A1
Принадлежит:

Disclosed herein are compounds of formula (I), or a salt thereof and compositions comprising compounds of formula I that exhibit antibacterial activities, when tested alone and/or in combination with a bacterial efflux pump inhibitor. Also disclosed are methods of treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I alone or in combination with the administration of a bacterial efflux pump inhibitor. 2. The compound of claim 1 , wherein Ris (C-C)alkyl substituted with one NRRand wherein the (C-C)alkyl is optionally substituted with one or more halo claim 1 , hydroxyl or phenyl wherein the phenyl is optionally substituted independently with one or more halo claim 1 , cyano claim 1 , (C-C)alkyl claim 1 , or (C-C)haloalkyl claim 1 , and Ris hydrogen or (C-C)alkyl claim 1 , or Rand Rtogether with the atoms to which they are attached form a 5 or 7-membered carbocycle wherein the carbocycle is substituted with one NRRand wherein the carbocycle is optionally substituted with one or more halo claim 1 , hydroxyl claim 1 , or (C-C)alkyl.3. The compound of claim 1 , wherein Ris (C-C)alkyl substituted with one NRRand Ris hydrogen claim 1 , or Rand Rtogether with the atoms to which they are attached form a 5 or 7-membered carbocycle wherein the carbocycle is substituted with one NRR.4. The compound of claim 1 , wherein Ris (C-C)alkyl substituted with one NRRand Ris hydrogen.6. The compound of claim 5 , wherein Ris hydrogen or (C-C)alkyl optionally substituted with one or more halo claim 5 , hydroxyl claim 5 , NRRor phenyl wherein the phenyl is optionally substituted independently with one or more halo claim 5 , cyano claim 5 , (C-C)alkyl claim 5 , or (C-C)haloalkyl and Ris hydrogen or (C-C)alkyl optionally substituted with one or more halo claim 5 , hydroxyl claim 5 , oxo claim 5 , or NRR.7. The compound of claim 5 , wherein Ris hydrogen or (C-C)alkyl optionally substituted with one or more halo claim 5 , ...

Подробнее
22-10-2020 дата публикации

NOVEL METAL COMPLEX, METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING GAMMA-LACTAM COMPOUND USING SAME

Номер: US20200330969A1
Принадлежит:

The present invention relates to a novel metal complex, a method for producing same, and a method for producing a gamma-lactam compound using same, and the metal complex according to the present invention is used as a catalyst for producing a gamma-lactam compound and can efficiently produce a gamma-lactam compound with an excellent yield and excellent selectivity. 4. The metal complex of claim 3 , wherein A is —CO— claim 3 , Rand Rare independently of each other (C1-C20)alkoxy claim 3 , and n is an integer of 1.5. The metal complex of claim 1 , wherein the metal complex is used as a catalyst for preparing a gamma-lactam compound from a dioxazol-one compound.7. The method of preparing a metal complex of claim 6 , wherein the base is any one or two or more selected from NaOAc claim 6 , NaCO claim 6 , NaHNO claim 6 , Cu(OAc) claim 6 , Cu(OAc).HO claim 6 , and NEt.8. The method of preparing a metal complex of claim 6 , wherein the base is used at 2 to 10 mol with respect to 1 mol of the metal precursor compound of Chemical Formula 3A claim 6 , and the quinoline-based compound of Chemical Formula 3B is used at 1.5 to 2.5 mol with respect to 1 mol of the metal precursor compound of Chemical Formula 3A.11. The method of preparing a gamma-lactam compound of claim 9 , wherein the metal complex is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol-one compound.12. The method of preparing a gamma-lactam compound of claim 9 , wherein the base is one or two or more selected from NaBAr(sodium tetrakis[3 claim 9 ,5-bis(trifluoromethyl)phenyl]borate) claim 9 , AgSbF(silver hexafluoroantimonate(V)) claim 9 , AgNTf(silver bis(trifluoromethanesulfonyl)imide) claim 9 , AgBF(silver tetrafluoroborate) claim 9 , AgPF(silver hexafluorophosphate) claim 9 , AgOTf (silver trifluoromethanesulfonate) claim 9 , and AgOAc (silver acetate).13. The method of preparing a gamma-lactam compound of claim 9 , wherein the base is used at 0.01 to 0.1 mol with respect to 1 mol of the dioxazol- ...

Подробнее
15-12-2016 дата публикации

Novel tricyclic compounds and preparation thereof

Номер: US20160362371A1

The present invention provides novel tricyclic compound of Formula I or its stereoisomer or ester or pharmaceutically acceptable salts and preparation thereof useful for treatment of cancer.

Подробнее
14-11-2019 дата публикации

POLYMORPHIC FORMS OF ST-246 AND METHODS OF PREPARATION

Номер: US20190343799A1
Принадлежит: Siga Technologies, Inc.

Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions. 140.-. (canceled)41. A polymorph Form VI of 4-trifluoromethyl-N-(3 ,3a ,4 ,4a ,5 ,5a ,6 ,6a-octahydro-1 ,3-dioxo-4 ,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide (ST-246) which shows an X-ray powder diffraction pattern having characteristic peaks at a reflection angle 2θ of 6.43 , 7.10 , 8.23 , 10.46 , 12.62 , 13.72 , 15.71 , 17.84 , 19.34 , 21.52 , 23.73 , 24.17 , 24.71 , 26.71 , 27.26 , 30.11 and 31.00 degrees.42. An isolated polymorph according to that is at least about 70% free of other forms.43. An isolated polymorph according to that is at least about 80% free of other forms.44. An isolated polymorph according to that is at least about 90% free of other forms.45. An isolated polymorph according to that is at least about 95% free of other forms.46. An isolated polymorph according to that is at least about 99% free of other forms.47. A pharmaceutical composition comprising the polymorph of claim and further comprising one or more pharmaceutically acceptable ingredients selected from the group consisting of carriers claim 41 , excipients claim 41 , diluents claim 41 , additives claim 41 , fillers claim 41 , lubricants and binders.48. The pharmaceutical composition of claim 47 , wherein the composition is formulated for oral administration.49. A method of treating Orthopoxvirus infections comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of .50. A method of treating eczema vaccinatum comprising administering to a patient in need thereof a therapeutically effective amount of the polymorph of .5183.-. (canceled)84. A method of producing crystal polymorphic Form VI of ST-246 claim 41 , comprising the steps of:a) dissolving ST-246 in at least one solvent to make a solution;b) cooling said solution ...

Подробнее
21-11-2019 дата публикации

INDOMETHACIN ANALOGS FOR THE TREATMENT OF CASTRATE-RESISTANT PROSTATE CANCER

Номер: US20190350903A1
Принадлежит:

Provided are compositions for inhibiting a biological activity of an aldo-keto reductase family 1, member C3 (AKR1C3) polypeptide. In some embodiments, the compositions are indomethacin derivatives that are AKR1C3-specific inhibitors. Also provided are methods for producing disclosed indomethacin derivatives that substantially lack cyclooxygenase inhibitory activity but that have AKR1C3 inhibitory activity, methods for inhibiting AKR1C3 polypeptide biological activities, and methods for treating prostate tumors in subjects. 5. A method for producing an indomethacin derivative that substantially lacks cyclooxygenase inhibitory activity but that has aldo-keto reductase family 1 , member C3 (AKR1C3) inhibitory activity , the method comprising performing a microwave-assisted reaction between (a) a Cto Calkoxy- or halo-substituted phenylhydrazine or salt thereof and (b) a cyclic or acyclic aliphatic ketoacid or alkyl ester thereof thereby providing an indole alkyl carboxylic acid or ester thereof , wherein the indole alkyl carboxylic acid or ester is a synthetic precursor of the indomethacin derivative.6. The method of claim 5 , wherein the microwave-assisted reaction is performed in the presence of sulfuric acid.7. The method of claim 5 , wherein the microwave-assisted reaction is performed in an alcoholic solvent claim 5 , preferably methanol.10. The method of claim 9 , wherein the cyclic or acyclic aliphatic ketoacid or alkyl ester thereof is selected from the group consisting of 3-oxopentanoic acid claim 9 , 4-oxobutanoic acid claim 9 , 4-oxopentanoic acid claim 9 , 5-oxohexanoic acid claim 9 , 4-oxohexanoic acid claim 9 , 4-oxoheptanoic acid claim 9 , 4-oxocyclohexanecarboxylic acid claim 9 , 3-oxocyclohexanecarboxylic acid or a methyl or ethyl ester thereof.12. The method of claim 5 , further comprising reacting the indole alkyl carboxylic acid or ester thereof with an aliphatic or aromatic acid halide to introduce an acyl substituent at the indole nitrogen atom ...

Подробнее
31-12-2020 дата публикации

PURIFICATION METHOD

Номер: US20200406166A1
Принадлежит: DAIKIN INDUSTRIES, LTD.

An object of the present disclosure is to provide a method for purifying the following fullerene derivative represented by formula (1) that is advantageous in production costs. The object is achieved by the method for purifying the fullerene derivative represented by formula (1) 2. The purification method according to claim 1 , wherein Ris an aryl group that is substituted with at least one substituent or unsubstituted.3. The purification method according to claim 1 , wherein ring A is a Cfullerene;{'sup': '1', 'Ris an alkyl group that is substituted with at least one substituent or unsubstituted, or an aryl group that is substituted with at least one substituent or unsubstituted; and'}{'sup': '2', 'Ris an aryl group that is substituted with at least one alkyl group or substituted.'}4. The purification method according to claim 1 , wherein n is 1.5. The purification method according to claim 1 , wherein the aluminum-containing inorganic porous adsorbent is activated clay.6. The purification method according to claim 1 , wherein the aluminum-containing inorganic porous adsorbent has a median size of 50 to 500 μm.7. The purification method according to claim 1 , wherein step 1 is a step of introducing the composition containing the fullerene derivative represented by formula (1) claim 1 , which is a target product for purification claim 1 , and the one or more impure fullerene compounds into a column containing activated clay claim 1 , which is a solid phase; and the method further comprises step 2 of allowing a solvent claim 1 , which is a liquid phase claim 1 , to flow through the column having the composition introduced to elute the fullerene derivative represented by formula (1) from the column.8. The purification method according to claim 1 , wherein the flow rate of the fullerene derivative represented by formula (1) per column cross-section area of 0.002 mis 0.001 to 50 g/min.9. The purification method according to claim 1 , wherein the flow rate of the solvent ...

Подробнее
31-12-2020 дата публикации

SUBSTITUTED (1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS

Номер: US20200407316A1
Принадлежит: Arena Pharmaceuticals Inc

Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.

Подробнее
28-10-1999 дата публикации

MCBI analogs of CC-1065 and the duocarmycins

Номер: AU711974B2
Автор: Dale L. Boger
Принадлежит: Scripps Research Institute

Подробнее
12-09-1997 дата публикации

Mcbi analogs of cc-1065 and the duocarmycins

Номер: WO1997032850A1
Автор: Dale L. Boger
Принадлежит: The Scripps Research Institute

MCBI (7-methoxy-1,2,9,9a-tetra-hydrocyclopropa[c]benz[e]indol-4-one) is employable as a DNA alkylating agent and can be incorporated into analogs of CC-1065 and the duocarmycins for constructing regioselective DNA alkylating agents.

Подробнее
16-12-1999 дата публикации

Metalosen dan katalis untuk polimerisasi olefin

Номер: ID22914A
Принадлежит: Montell Technology Company Bv

Подробнее
09-07-1999 дата публикации

Metallocenes and catalysts for olefin polymerization

Номер: NO993398D0
Принадлежит: Montell Technology Company Bv

Подробнее
20-05-1999 дата публикации

Metallocenes and catalysts for olefin-polymerisation

Номер: WO1999024446A1
Принадлежит: Montell Technology Company B.V.

A class of metallocenes of formula (I): (ZR1m)n(Cp)(A)rMLpL'q (I) wherein (ZR1m)n is a divalent group bridging Cp and A, Cp is a heterocyclic cyclopentadienyl group of formula (II) or (II'), wherein one of X or Y is a single bond, the other being an heteroatom; R?2 and R3¿ are hydrogen, halogen or a hydrocarbon radical, optionally containing heteroatoms; R4 is halogen or an hydrocarbon radical, optionally containing heteroatoms; the group A is a cyclopentadienyl derivative or is equal to Cp; M is Ti, Zr or Hf; m is 1 or 2; n ranges from 0 to 4; r is 0 or 1; p and q range from 0 to 3; and a ranges from 0 to 4. Moreover, are disclosed catalyst systems containing these metallocenes, useful in the polymerization of olefins.

Подробнее
17-09-2002 дата публикации

Metallocenes and catalysts for olefin-polymerisation

Номер: US6451724B1
Принадлежит: Basell Technology Co BV

A class of metallocenes of formula (I): (ZR 1 m ) n (Cp)(A) r ML p L′ q (I) wherein (ZR 1 m ) n , is a divalent group bridging Cp and A, Cp is a heterocyclic cyclopentadienyl group of formula (II) or (II′), wherein one of X or Y is a single bond, the other being an heteroatom; R 2 and R 3 are hydrogen, halogen or a hydrocarbon radical, optionally containing heteroatoms; R 4 is halogen or an hydrocarbon radical, optionally containing heteroatoms; the group A is a cyclopentadienyl derivative or is equal to Cp; M is Ti, Zr or Hf; m is 1 or 2; n ranges from 0 to 4; r is 0 or 1; p and q range from 0 to 3; and a ranges from 0 to 4. Moreover, are disclosed catalyst systems containing these metallocenes, useful in the polymerization of olefins.

Подробнее
13-11-2003 дата публикации

METALLOCENES AND CATALYSTS FOR OLEFIN POLYMERIZATION

Номер: DE69810894T2
Принадлежит: BASELL POLYOLEFINE GMBH

Подробнее
07-08-2003 дата публикации

Metallocenes and catalysts for olefin-polymerisation

Номер: US20030148877A1
Принадлежит: Individual

A class of metallocenes of formula (I): (ZR 1 m ) n (Cp)(A) r ML p L′ q (I) wherein ZR 1 m ) is a divalent group bridging Cp and A, Cp is a heterocyclic cyclopentadienyl group of formula (II) or (II′), wherein one of X or Y is a single bond, the other being an heteroatom; R 2 and R 3 are hydrogen, halogen or a hydrocarbon radical, optionally containing heteroatoms; R 4 is a halogen or an hydrocarbon radical, optionally containing heteroatoms; the group A is a cyclopentadienyl derivative or is equal to Cp; M is Ti, Zr or Hf; m is 1 or 2; n ranges from 0 to 4; r is 0 or 1; p and q range from 0 to 3; and a ranges from 0 to 4. Moreover, are disclosed catalyst systems containing these metallocenes, useful in the polymerization of olefins.

Подробнее
14-12-2005 дата публикации

金属茂和烯烃聚合催化剂

Номер: CN1231487C
Принадлежит: Spherilene SRL

本发明涉及一类式(I)的金属茂:(ZR 1 m ) n (Cp)(A) r ML p L’ q (I),其中(ZR 1 m ) n 是一个桥连Cp和A的二价基团,Cp是一个式(II)或(II’)的杂环环戊二烯基基团,其中X或Y之一是一个单键,另一个是杂原子;R 2 和R 3 是氢、卤素或一个烃基,任选含有杂原子;R 4 是卤素或一个烃基,任选含有杂原子;基团A是一个环戊二烯基衍生物或等于Cp;M是Ti、Zr或Hf;m是1或2;n范围为0-4;r是0或1;p和q范围为0-3和0-4。此外,这里公开了可用于烯烃聚合的含这些金属茂的催化剂体系。

Подробнее
28-02-2000 дата публикации

Metalocenes and olefins polymerisation catalysts

Номер: PL334470A1
Принадлежит: Montell Technology Company Bv

Подробнее
17-03-2014 дата публикации

유기 전계 발광 소자

Номер: KR20140032823A

본 발명은 특정 조합의 도판트 화합물 및 호스트 화합물을 함유하는 유기 전계 발광 소자에 관한 것이다. 본 발명에 따른 유기 전계 발광 소자는 황록색 발광을 나타내고, 소자의 전류특성을 개선시킴으로써 소자의 구동전압을 저하시키고 동시에 전력효율과 작동수명을 향상시킨다.

Подробнее
23-12-2011 дата публикации

Organic light emitting device

Номер: KR101097312B1

본 발명은 하기 화학식 1로 표시되는 헤테로 고리 화합물 및 이를 포함한 유기막을 구비한 유기 발광 소자에 관한 것이다: The present invention relates to an organic light emitting device having a heterocyclic compound represented by Chemical Formula 1 and an organic film including the same: <화학식 1> <Formula 1> 상기 화학식에 대한 설명은 발명의 상세한 설명을 참조한다. For the description of the above formula, see the detailed description of the invention.

Подробнее
17-02-1987 дата публикации

Flame retardants and compositions containing them

Номер: US4644066A
Автор: Joseph Sonnenberg
Принадлежит: Raychem Corp

Flame retardants having good stability at the processing temperatures of high melting polymers are described. The flame retardants are halogen-containing bis-imides, for example, those of the formula ##STR1## R being defined in the specification.

Подробнее
10-10-2017 дата публикации

Patterning method, chemically-amplified resist composition, and resist film

Номер: KR101783729B1
Автор: 카오루 이와토
Принадлежит: 후지필름 가부시키가이샤

고감도, 고해상성, 우수한 러프니스 성능, 및 우수한 드라이 에칭 내성을 동시에 만족함과 아울러 또한 현상 시간 의존성이 우수한 패턴 형성 방법으로서 (가) (A) 산 분해성기를 갖는 풀러렌 유도체와, (B) 활성광선 또는 방사선의 조사에 의해 산을 발생하는 화합물과, (C) 용제를 함유하는 화학증폭형 레지스트 조성물에 의해 막을 형성하는 공정, (나) 상기 막을 노광하는 공정, 및 (다) 유기 용제를 포함하는 현상액을 사용하여 현상하는 공정을 포함하는 네거티브형 패턴 형성 방법을 제공한다. (A) a fullerene derivative having an acid-decomposable group, (B) an actinic ray-curable resin composition comprising (A) a fullerene derivative having an acid-decomposable group, and (C) a step of forming a film by a chemically amplified resist composition containing a solvent, (B) a step of exposing the film, and (C) a step of exposing the film to a developing solution containing an organic solvent And a step of developing the light-emitting layer by using the light-emitting layer.

Подробнее
31-05-1999 дата публикации

Metallocenes and catalysts for olefin-polymerisation

Номер: AU1870999A
Принадлежит: Montell Technology Co BV

Подробнее
31-08-2011 дата публикации

取代的四环四氢吡喃、吡咯烷和四氢噻吩衍生物

Номер: CN101115719B
Принадлежит: Janssen Pharmaceutica NV

本发明涉及新的取代的四环四氢吡喃、吡咯烷和四氢噻吩衍生物,其对于血清素受体、尤其是5-HT 2A 和5-HT 2C 受体具有结合亲合性,对于多巴胺受体、尤其是多巴胺D2受体具有结合亲合性,具有去甲肾上腺素再摄取抑制性能,涉及包含按照本发明化合物的药物组合物,其作为药物的用途,尤其是用于预防和/或治疗精神病学和神经病学疾病范围内的疾病,特别是某些精神病、心血管和胃动力学病症,和它们的制备方法。按照本发明的化合物可以由通式(I)代表也包括其药学可接受的酸或碱加成盐,其立体化学异构形式,其N-氧化物形式和其前体药物,其中所有的取代基如权利要求1所定义。

Подробнее
20-01-2009 дата публикации

Новые замещенные тетрациклические производные тетрагидрофурана, пирролидина и тетрагидротиофена

Номер: RU2007125693A

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2007 125 693 (13) A (51) ÌÏÊ C07D 209/70 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007125693/04, 06.12.2005 (71) Çà âèòåëü(è): ßÍÑÑÅÍ ÔÀÐÌÀÖÅÂÒÈÊÀ Í.Â. (BE) (30) Êîíâåíöèîííûé ïðèîðèòåò: 07.12.2004 EP 04106373.6 (43) Äàòà ïóáëèêàöèè çà âêè: 20.01.2009 Áþë. ¹ 2 (87) Ïóáëèêàöè PCT: WO 2006/061392 (15.06.2006) A Àäðåñ äë ïåðåïèñêè: 129010, Ìîñêâà, óë. Á.Ñïàññêà , 25, ñòð.3, ÎÎÎ "Þðèäè÷åñêà ôèðìà Ãîðîäèññêèé è Ïàðòíåðû", ïàò.ïîâ. À.Â.Ìèö (54) ÍÎÂÛÅ ÇÀÌÅÙÅÍÍÛÅ ÒÅÒÐÀÖÈÊËÈ×ÅÑÊÈÅ ÏÐÎÈÇÂÎÄÍÛÅ ÒÅÒÐÀÃÈÄÐÎÔÓÐÀÍÀ, ÏÈÐÐÎËÈÄÈÍÀ È ÒÅÒÐÀÃÈÄÐÎÒÈÎÔÅÍÀ R U 1. Ñîåäèíåíèå ôîðìóëÛ (I) A 2 0 0 7 1 2 5 6 9 3 (57) Ôîðìóëà èçîáðåòåíè åãî N-îêñèäíà ôîðìà, ôàðìàöåâòè÷åñêè ïðèåìëåìà àääèòèâíà ñîëü èëè ñòåðåîõèìè÷åñêè èçîìåðíà ôîðìà, ãäå ïóíêòèðíà ëèíè îçíà÷àåò íåîá çàòåëüíóþ ñâ çü; i è j îçíà÷àþò öåëûå ÷èñëà, íåçàâèñèìî äðóã îò äðóãà ðàâíûå íóëþ, 1, 2, 3 èëè 4; A è B êàæäûé íåçàâèñèìî äðóã îò äðóãà îçíà÷àþò áåíçî-, íàôòîãðóïïó èëè ðàäèêàë, âûáðàííûé èç ãðóïïû, ñîñòî ùåé èç ôóðî-; òèåíî-; ïèððîëî-; îêñàçîëî-; òèàçîëî-; èìèäàçîëî-; èçîêñàçîëî-; èçîòèàçîëî-; îêñàäèàçîëî-; òðèàçîëî-; ïèðèäèíî-; ïèðèäàçèíî-; ïèðèìèäèíî-; ïèðàçèíî-; èíäîëî-; èíäîëèçèíî-; èçîèíäîëî-; áåíçîôóðî-; èçîáåíçîôóðî-; áåíçîòèåíî-; èíäàçîëî-; áåíçèìèäàçîëî-; áåíçòèàçîëî-; õèíîëèçèíî-; õèíîëèíî-; èçîõèíîëèíî-; ôòàëàçèíî-; õèíàçîëèíî-; õèíîêñàëèíî-; õðîìåíî- è íàôòèðèäèíîãðóïïû; êàæäûé R 9 íåçàâèñèìî äðóã îò äðóãà âûáðàí èç ãðóïïû, ñîñòî ùåé èç âîäîðîäà; ãàëîãåíà; öèàíîãðóïïû; ãèäðîêñèãðóïïû; êàðáîêñèëà; íèòðîãðóïïû; àìèíîãðóïïû; ìîíîÑòðàíèöà: 1 RU 2 0 0 7 1 2 5 6 9 3 (86) Çà âêà PCT: EP 2005/056544 (06.12.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 09.07.2007 (72) Àâòîð(û): ÑÈÄ-ÍÓÍÜÅÑ Õîñå Ìàðè (ES), ÌÅÃÅÍÑ Àíòîíèóñ Àäðèàíóñ Õåíäðèêóñ Ïåòðóñ (BE), ÒÐÀÁÀÍÊÎ-ÑÓÀÐÅÑ Àíäðåñ Àâåëèíî (ES), ÊÎÓÊÍÈ Ìîõàìåä (BE), ÕÎÐÍÀÐÒ Äæîðæ Æîçåô Êîðíåëèóñ (BE), ÊÎÌÏÅÐÍÎËËÅ Ôðàíñ Éîçåô Êîðíåëèóñ (BE), ...

Подробнее
27-02-2010 дата публикации

Derivatives of tetrahydrocarbazoles, method of obtaining them and pharmaceutical compositions containing them

Номер: RU2382770C2
Принадлежит: Ф.Хоффманн-Ля Рош Аг

FIELD: medicine. SUBSTANCE: invention relates to compounds of general formula (I) and their pharmaceutically acceptable salts and pharmaceutically acceptable asters, possessing activity with respect to LXRα and/or LXRβ receptors. Compounds can be applied for treatment and prevention of diseases mediated by LXRα and/or LXRβ receptors, namely: increased level of lipids and cholesterol level, atherosclerotic diseases, diabetes, metabolic syndrome, dyslipidermia, sepsis, inflammatory diseases, pancreatitis, liver cholestasis/fibrosis, and diseases which include inflammatory component, such as Alzheimer's disease and reduced/improvable cognitive function. In general formula n represents integer number from 0 to 3; R 1 is independently selected from group consisting of halogen, -CN, -NO 2 , -SO 2 Me, lower alkyl, -OR 11 , pyperidinyl and -N(R 11 )(R 11 ), where R 11 is independently selected from lower alkyl and H, X 1 , X 2 , X 3 and X 4 are independently selected from nitrogen and carbon, on condition that, not more than two of X 1 , X 2 , X 3 and X 4 can simultaneously represent nitrogen, and in case when two of X 1 , X 2 , X 3 and X 4 represent nitrogen, n represents 0,1 or 2; k represents integer number 0 or 1; R2 represents H; R 3 represents H, lower alkyl or halogen; R 4 represents aryl, heteroaryl, lower alkylaryl or lower alkylheteroaryl, each of which is optionally substituted with substituents in amount from one to five, which are independently selected from group consisting of halogen, lower alkyl, -OR 41 , lower alkinyl and NR 42 R 43 , where R 41 represents lower alkyl, R 42 and R 43 independently on each other represent hydrogen or lower alkyl, or NR 42 R 43 represents pyrrolidinyl, or R 4 represents lower alkyl; R 5 is selected from group, heteroaryl, consisting of and , said aryl and heteroaryl being optionally substituted in one or more positions with one or more substituents, independently selected from group consisting of H, halogen, lower alkyl ...

Подробнее
02-06-2022 дата публикации

Pyromethene metal complex, pyromethene compound, light emitting device material, light emitting device, display device and lighting device

Номер: KR102404529B1
Принадлежит: 도레이 카부시키가이샤

본 발명의 목적은 발광 효율이 높고, 색순도가 우수한 적색 발광 재료 및 적색 발광 소자를 제공하는 것이다. 본 발명은 특정한 일반식으로 표시되는 피로메텐 금속 착체이다.

Подробнее
02-03-1976 дата публикации

Containing hindered phenolic norbornane-2,3-dicarboximides stabilized compositions

Номер: US3941746A
Автор: John F. Stephen
Принадлежит: Ciba Geigy Corp

Compounds having the formula ##SPC1## Wherein R 1 and R 2 are lower alkyl, X and Y are hydrogen or, when taken together, they form a bond or an ether linkage, m is 0 to 3, and n is 0 to 2, are good ultraviolet light stabilizers for synthetic polymers.

Подробнее
27-03-2016 дата публикации

Polymorphic forms of st-246 compound and methods for producing

Номер: RU2578606C2
Принадлежит: Сига Текнолоджиз, Инк

FIELD: medicine, pharmaceutics. SUBSTANCE: invention refers to a polymorphic form of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)benzamide (ST-246 compound), a method for producing the polymorphic form, and a pharmaceutical composition containing said polymorphic form. EFFECT: producing new compounds. 13 cl, 24 dwg, 18 tbl, 11 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 578 606 C2 (51) МПК C07D 209/76 (2006.01) A61K 31/403 (2006.01) A61P 31/20 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ (21)(22) Заявка: ИЗОБРЕТЕНИЯ К ПАТЕНТУ 2012144818/04, 23.03.2011 (24) Дата начала отсчета срока действия патента: 23.03.2011 Приоритет(ы): (30) Конвенционный приоритет: (43) Дата публикации заявки: 27.04.2014 Бюл. № 12 (56) Список документов, цитированных в отчете о поиске: CN 101445478 A, 03.06.2009. US 20080004452 A1, 03.01.2008. RU 2412160 C1, 20.02.2011. (73) Патентообладатель(и): СИГА ТЕКНОЛОДЖИЗ, ИНК (US) (85) Дата начала рассмотрения заявки PCT на национальной фазе: 23.10.2012 2 5 7 8 6 0 6 (45) Опубликовано: 27.03.2016 Бюл. № 9 R U 23.03.2010 US 61/316,747; 12.08.2010 US 61/373,031 (72) Автор(ы): ТЯВАНАГИМАТТ Шантхакумар Р. (US), СТОУН Мелиалани А.К.Л. (US), УЭЙМЕРС Уилльям К. (US), НЕЛЬСОН Дилан (US), БОЛКЕН Тоув К. (US), ХРУБИ Деннис Э. (US), О'НЕЙЛЛ Майкл Х. (US), СВИТЭППЛ Гари (US), МакКЛУН Келли А. (US) (86) Заявка PCT: (87) Публикация заявки PCT: WO 2011/119698 (29.09.2011) Адрес для переписки: 129090, Москва, ул. Б. Спасская, 25, строение 3, ООО "Юридическая фирма Городисский и Партнеры" (54) ПОЛИМОРФНЫЕ ФОРМЫ СОЕДИНЕНИЯ ST-246 И СПОСОБЫ ПОЛУЧЕНИЯ (57) Реферат: Изобретение относится к полиморфной форме получения полиморфной формы и 4-трифторметил-N-(3,3a,4,4a,5,5a,6,6a-октагидрофармацевтической композиции, содержащей 1,3-диоксо-4,6-этеноциклопроп[f]изоиндол-2(1H) указанную полиморфную форму. 7 н. и 6 з.п. ф-ил)бензамида (соединение ST-246), к способу лы, 24 ил., 18 табл., 11 пр. R ...

Подробнее
21-03-2017 дата публикации

Method for synthesizing cycloalkanyl[b]indoles, cycloalkanyl[b]benzofurans, cycloalkanyl[b]benzothiophenes, compounds and methods of use

Номер: US9598365B2
Автор: Jimmy Wu
Принадлежит: Dartmouth College

A method of synthesizing cycloalkanyl[b]indoles, as well as related cycloalkanyl[b]benzofurans and cycloalkanyl[b]benzothiophenes is provided. The method is a single, multicomponent reaction that combines (1) an indole, benzofuran, or benzothiopene, (2) an aldehyde, ketone, or ketal, and (3) a diene in the presence of an acid, in particular a Ga(III) or In(III) salt. Compositions and methods of using these compounds to stimulate secretion and/or production of glucagon-like peptide-1 or inhibit the activity of Calcitonin Gene-Related Peptide receptor are also provided.

Подробнее
16-10-1996 дата публикации

Indenoindole compounds II

Номер: CN1033029C

具有如下结构式的化合物及其对映体和盐 式中R是氢或低级烷基或COR 15 R 1 、R 2 、R 11 、和R 12 、是氢或低级烷基, R 3 、R 4 、R 5 、和R 6 是氢、羟基、卤素、低级烷基、低级烷氧基或者一或二-低级烷基氨基、NH 2 或NR 13 COR 14 , R 7 、R 8 、R 9 和R 10 是氢、羟基、低级烷基、低级烷氧基、一或二-低级烷基氨基、或NR 13 COR 14 ,其中R 13 、R 14 和R 15 是氢或低级烷基,但须:当R是COR 15 时,R 3 -R 10 中至少有一个羟基或一或二-低级烷基氨基,该化合物在医药和非医药领域内作为抗氧化剂是有效的。结构式为IA和IB的化合物有许多是新的,并且叙述了制备它们的各种方法。

Подробнее
10-09-2008 дата публикации

Tricyclic derivatives of indenopyrrole as modulators of serotinin receptors, a pharmaceutical composition based on them, and a method for treating diseases, and / or non-trivial necrosis.

Номер: RU2007107494A

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2007 107 494 (13) A (51) ÌÏÊ C07D 209/80 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2007107494/04, 26.07.2005 (71) Çà âèòåëü(è): Ýñåðñèñ, Èíê. (US) (30) Êîíâåíöèîííûé ïðèîðèòåò: 29.07.2004 US 60/592047 (43) Äàòà ïóáëèêàöèè çà âêè: 10.09.2008 Áþë. ¹ 25 Àäðåñ äë ïåðåïèñêè: 127055, Ìîñêâà, à/ 11, ïàò.ïîâ. Í.Ê.Ïîïåëåíñêîìó, ðåã. N 31 (54) ÒÐÈÖÈÊËÈ×ÅÑÊÈÅ ÏÐÎÈÇÂÎÄÍÛÅ ÈÍÄÅÍÎÏÈÐÐÎËÀ ÊÀÊ ÌÎÄÓËßÒÎÐÛ R U (57) Ôîðìóëà èçîáðåòåíè 1. Òðèöèêëè÷åñêèå ïðîèçâîäíûå èíäåíîïèððîëà, îõâàòûâàåìûå îáùåé ñòðóêòóðíîé ôîðìóëîé A 2 0 0 7 1 0 7 4 9 4 A ÑÅÐÎÒÈÍÈÍÎÂÛÕ ÐÅÖÅÏÒÎÐÎÂ, ÔÀÐÌÀÖÅÂÒÈ×ÅÑÊÀß ÊÎÌÏÎÇÈÖÈß ÍÀ ÈÕ ÎÑÍÎÂÅ È ÑÏÎÑÎÁ ËÅ×ÅÍÈß ÇÀÁÎËÅÂÀÍÈÉ, ÐÀÑÒÐÎÉÑÒ È/ÈËÈ ÏÀÒÎËÎÃÈ×ÅÑÊÈÕ ÑÎÑÒÎßÍÈÉ, ÑÂßÇÀÍÍÛÕ Ñ ÍÅÎÁÕÎÄÈÌÎÑÒÜÞ ÌÎÄÓËßÖÈÈ ÔÓÍÊÖÈÈ 5-ÍÒ2Ñ ÐÅÖÅÏÒÎÐΠâ êîòîðîé R1 âûáðàí èç ãðóïïû, ñîñòî ùåé èç Í, ãàëîãåíà, Ñ1-10-àëêèëà, Ñ2-àëêåíèëà, Ñ2-10-àëêèíèëà, ïåðãàëîãåíàëêèëà, CN, N(R6)2, SR6, CON(R6)2, NR6COR7, 10 NR6CO2R7, SO2N(R6)2, NR6SO2R7, àðèëà, ãåòåðîàðèëà, Ñ1-10-àëêèëàðèëà è Ñ1-10àëêèëãåòåðîàðèëà; è åñëè m+n=1, òî R1 ìîæåò òàêæå áûòü OR6 èëè OCOR7; R2, R3 è R4 íåçàâèñèìî âûáðàíû èç ãðóïïû, ñîñòî ùåé èç Í, ãàëîãåíà, Ñ1-10-àëêèëà, Ñ2-àëêåíèëà, Ñ2-10-àëêèíèëà, ïåðãàëîãåíàëêèëà, CN, OR6, N(R6)2, SR6, OCOR7, CON(R6)2, 10 NR6COR7, NR6CO2R7, SO2N(R6)2, NR6SO2R7, àðèëà, ãåòåðîàðèëà, Ñ1-10-àëêèëàðèëà è Ñ1-àëêèëãåòåðîàðèëà, èëè R2 è R3 ñîâìåñòíî ñ öèêëîì, ê êîòîðîìó îíè ïðèñîåäèíåíû, 10 îáðàçóþò 5-7-÷ëåííûé êàðáî- èëè ãåòåðîöèêë; R5 âûáðàí èç ãðóïïû, ñîñòî ùåé èç Í, Ñ1-10-àëêèëà, Ñ2-10-àëêåíèëà, Ñ2-10-àëêèíèëà, Ñòðàíèöà: 1 RU 2 0 0 7 1 0 7 4 9 4 (86) Çà âêà PCT: US 2005/026415 (26.07.2005) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 28.02.2007 (72) Àâòîð(û): ÕÀÊ Áåéàðä (US), ÁÅÍÍÀÍÈ Þññåô Ë. (US), ÐÎÁÀÐÄÆ Ìàéêë Äæ. (US) A 2 0 0 7 1 0 7 4 9 4 A R U 2 0 0 7 1 0 7 4 9 4 Ñòðàíèöà: 2 R U ïåðãàëîãåíàëêèëà, CN, OR6, N(R6)2, SR6, OCOR7, CON(R6)2, NR6COR7, NR6CO2R7, NR6SO2R7, ...

Подробнее
13-11-2018 дата публикации

Compound having indenocarbazole ring structure and organic electroluminescent element

Номер: KR101918304B1

고효율, 고내구성의 유기 일렉트로루미네센스 소자용의 재료로서, 정공의 주입·수송성능이 우수하고, 전자 저지능력을 가지며, 박막 상태에서의 안정성이 높고, 발광 효율이 높은 우수한 특성을 가지는 유기 화합물을 제공하고, 이 화합물을 더 이용하여, 고효율, 고내구성의 유기 일렉트로루미네센스 소자를 제공하는 것. 하기 일반식(1)로 표시되는 인데노카바졸 환 구조를 가지는 화합물이고, 한 쌍의 전극과 그 사이에 끼워진 적어도 1층의 유기층을 가지는 유기 일렉트로루미네센스 소자에 있어서, 상기 화합물이, 적어도 1개의 유기층의 구성 재료로서 이용되고 있는 것을 특징으로 하는 유기 일렉트로루미네센스 소자이다. An organic electroluminescence device having high efficiency and high durability and having excellent characteristics of injecting and transporting holes, having electron blocking ability, high stability in a thin film state, And further using this compound to provide an organic electroluminescent device with high efficiency and high durability. An organic electroluminescence device having an indenocarbazole ring structure represented by the following general formula (1), wherein the compound has at least a pair of electrodes and at least one organic layer sandwiched therebetween, Is an organic electroluminescent device characterized by being used as a constituent material of one organic layer.

Подробнее
02-12-2010 дата публикации

Materials for organic electroluminescent devices

Номер: DE102009023155A1
Принадлежит: Merck Patent GmBH

Die vorliegende Erfindung beschreibt Indenocarbazol-Derivate mit elektronen- und lochtransportierenden Eigenschaften, insbesondere zur Verwendung in der Emissions- und/oder Ladungstransportschicht von Elektrolumineszenzvorrichtungen oder als Matrixmaterial. Die Erfindung betrifft ferner ein Verfahren zur Herstellung der erfindungsgemäßen Verbindungen sowie elektronische Vorrichtungen, enthaltend diese. The present invention describes indenocarbazole derivatives having electron and hole transporting properties, in particular for use in the emission and / or charge transport layer of electroluminescent devices or as matrix material. The invention further relates to a process for the preparation of the compounds according to the invention and to electronic devices containing them.

Подробнее
21-11-2017 дата публикации

Organic light-emitting device

Номер: US9822133B2
Принадлежит: Samsung Display Co Ltd

Provided is an organic light-emitting device including a first electrode, a second electrode, an emission layer between the first electrode and the second electrode, and a hole transport region between the first electrode and the emission layer, wherein the hole transport region includes an auxiliary layer, the auxiliary layer including at least one amine-based compound represented by Formula 1: where R 11 , R 12 , R 13 , R 14 , R 15 , R 16 , X 11 , L 11 , L 12 , L 13 , a11, a12, a13, b15, and b16 are as defined in the specification.

Подробнее
22-03-2021 дата публикации

Organic light-emitting device

Номер: KR102230191B1
Принадлежит: 삼성디스플레이 주식회사

유기 발광 소자가 개시된다. An organic light emitting device is disclosed.

Подробнее
15-06-2006 дата публикации

Substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives

Номер: WO2006061392A2
Принадлежит: Janssen Pharmaceutica N.V.

This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Подробнее
09-04-2013 дата публикации

Substituted tetracyclic tetahydrofuran, pyrrolidine and tetrahydrothiophene derivatives

Номер: US8415347B2
Принадлежит: Janssen Pharmaceutica NV

This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT 2A and 5-HT 2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Подробнее
04-09-2020 дата публикации

2-aldehyde indole compound and preparation method thereof

Номер: CN111620808A
Автор: 汪思敏, 胡益民, 韦强, 鲍丽
Принадлежит: Anhui Normal University

本发明提供了一种2‑醛基吲哚类化合物及其制备方法,以四炔类化合物和2‑苯基‑2‑恶唑啉为原料,在甲苯溶剂反应,得到了一种2‑醛基吲哚类化合物。与现有技术相比,本发明提供了一种全新的2‑醛基吲哚的合成方法,生成一种新的2‑醛基吲哚类化合物。合成的2‑醛基吲哚类化合物具有较高原子经济性,结构更加复杂多样,具有一定的运用前景。

Подробнее
10-01-2009 дата публикации

Isoindoline derivatives

Номер: RU2343145C2

FIELD: chemistry. SUBSTANCE: in general formula (I) , R 1 represents similar or different 2 groups, each of which is selected from group consisting of C 1-3 alkyl, or when R 1 are two adjacent groups, two groups R 1 , taken together, can form saturated or unsaturated 5- or 6-member cyclic group, which can have 1 or 2 oxygens as heteroatom; X represents oxygen or sulphur; values of other radicals are given in invention formula. EFFECT: increase of composition efficiency. 16 cl, 11 tbl, 31 ex ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß RU (19) (11) 2 343 145 (13) C2 (51) ÌÏÊ C07D 209/46 C07D 401/04 C07D 401/06 C07D 401/12 C07D 401/14 ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ C07D 403/04 ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ,C07D 403/12 ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ C07D 405/14 C07D 491/048 C07D 491/056 (12) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) (2006.01) A61K A61K A61K A61K A61K 31/4035 (2006.01) 31/4439 (2006.01) 31/4545 (2006.01) 31/496 (2006.01) 31/551 (2006.01) ÎÏÈÑÀÍÈÅ ÈÇÎÁÐÅÒÅÍÈß Ê ÏÀÒÅÍÒÓ (21), (22) Çà âêà: 2005120003/04, 25.11.2003 (24) Äàòà íà÷àëà îòñ÷åòà ñðîêà äåéñòâè ïàòåíòà: 25.11.2003 (30) Êîíâåíöèîííûé ïðèîðèòåò: 26.11.2002 JP 2002-342399 2 3 4 3 1 4 5 R U (56) Ñïèñîê äîêóìåíòîâ, öèòèðîâàííûõ â îò÷åòå î ïîèñêå: Jan Epsztajn et al. Application of organolithium and related reagents in synthesis. Part 23: synthesis strategies based on ortho-aromatic metallation. Synthesis of 4b-arylisoindolo[2,1-a]quinoline derivatives. Tetrahedron, 2000, vol.56, no.27, p.4837-4844. SU 1376941 A3, 23.02.1988. WO 9842666 A1, 01.10.1998. GB 1307205 A (RHONE-POULENC S.A.), 14.02.1973. C 2 C 2 (45) Îïóáëèêîâàíî: 10.01.2009 Áþë. ¹ 1 (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 27.06.2005 (86) Çà âêà PCT: JP 03/014986 (25.11.2003) (87) Ïóáëèêàöè PCT: WO 2004/048332 (10.06.2004) Àäðåñ äë ïåðåïèñêè: 103735, Ìîñêâà, óë. Èëüèíêà, 5/2, ÎÎÎ "Ñîþçïàòåíò", ïàò.ïîâ. À.Ï.Àãóðååâó (54) ÏÐÎÈÇÂÎÄÍÛÅ ÈÇÎÈÍÄÎËÈÍÀ (57) Ðåôåðàò: Èçîáðåòåíèå îòíîñèòñ ê íîâûì ñîåäèíåíè ì ôîðìóëû (I) è èõ ...

Подробнее
16-03-2015 дата публикации

Novel anthracene derivatives and organic electroluminescent device using the same

Номер: KR101502811B1
Автор: 권순기, 김윤희, 이윤지
Принадлежит: 경상대학교산학협력단

본 발명은 신규한 비대칭 안트라센 유도체 및 이를 발광층에 포함하는 유기 발광 소자에 관한 것으로, 보다 상세하게 본 발명에 따른 안트라센 유도체는 하기 화학식1로 표시되며, 비대칭의 고도로 뒤틀린 안트라센 화합물인 것을 특징으로 한다. [화학식 1] [상기 화학식 1에서, R 1 내지 R 4 , X 및 Y는 각각 발명의 상세한 설명에서 정의한 바와 같다.] The present invention relates to a novel asymmetric anthracene derivative and an organic light emitting device including the same in a light emitting layer. More specifically, the anthracene derivative according to the present invention is represented by the following general formula (1) and is an asymmetric highly twisted anthracene compound. [Chemical Formula 1] [Wherein R 1 to R 4 , X and Y are each as defined in the description of the invention].

Подробнее
11-06-1987 дата публикации

Process for preparing tricyclic oxindole carboxamide derivatives

Номер: KR870001144B1

Tricyclic oxindole carbox-amide derivs., useful as an antiinflammatory agent, are prepd. Thus, a mixt. contg. 1.0g ethyl2- methyl-5-ethyl-6-oxo-6, 7-dihydrofuro [2,3-f indol-7-carboxylate and 793 mg 2-amino-5-methyl thiazole in 35ml benzene is refluxed for 45min, treated with 145ml dichloro-methane, and added into 150ml cold IN-HCl to give 1.06g N-(5-methylthiazo-2-yl)-2-methyl5-ethyl-6-oxo-6, 7-dihydro-furo [2,3-f indol-7-carboxamide.

Подробнее
01-03-2006 дата публикации

Isoindoline derivative

Номер: CN1741995A
Принадлежит: Maruishi Pharmaceutical Co Ltd

一种新的式(I)表示的异吲哚啉化合物。该式(I)化合物具有镇静活性。该化合物导致哺乳动物镇静并因此用作麻醉药物。

Подробнее
07-05-2014 дата публикации

Aromatic amine derivative and organic electroluminescence element using same

Номер: CN103781782A
Автор: 加藤朋希, 藤山高广
Принадлежит: Idemitsu Kosan Co Ltd

下述式(1)所示的芳香族胺衍生物。(式(1)中,L 1 、L 2 、Ar 1 、Ar 2 、R 1 、R 2 、a、b、和Q如说明书中所定义。)具有1层以上含有上述芳香族胺衍生物的有机薄膜层的有机电致发光元件的发光效率高且为长寿命。

Подробнее
26-09-2017 дата публикации

Tricyclic compounds and preparation thereof

Номер: US9771325B2

The present invention provides novel tricyclic compound of Formula I or its stereoisomer or ester or pharmaceutically acceptable salts and preparation thereof useful for treatment of cancer.

Подробнее
01-08-2022 дата публикации

Compounds for Electronic Devices

Номер: KR20220107000A
Принадлежит: 메르크 파텐트 게엠베하

본 출원은 식 (I) 또는 (II) 의 화합물, 전자 디바이스에서의 그의 용도, 그 화합물의 제조 방법, 및 그 화합물을 포함하는 전자 디바이스에 관한 것이다.

Подробнее
03-02-2011 дата публикации

Fullerene derivatives

Номер: WO2011013597A1
Автор: 上谷保則, 藤原淳
Принадлежит: 住友化学株式会社

Fullerene derivatives which each have a partial structure represented by general formula (1), in particular, fullerene derivatives which each have one to four partial structures represented by general formula (1) are applicable to organic photoelectric conversion elements with high open-circuit voltage, and are therefore suitable for use in organic thin-film solar cells or organic photo-sensors, thus being extremely useful. In general formula (1), R is a monovalent group; and r is an integer of 0 to 4.

Подробнее
18-03-2014 дата публикации

Fullerene derivatives

Номер: US8673958B2
Принадлежит: Sumitomo Chemical Co Ltd

A fullerene derivative having a partial structure represented by formula (1): wherein R represents a monovalent group, and r represents an integer of 0 to 4, in particular, a fullerene derivative, which has one to four structures represented by formula (1), can be applied to an organic photoelectric conversion element having a high open-circuit voltage and is therefore suitable for an organic thin-film solar cell or an organic photosensor, and thus it is extremely useful.

Подробнее
24-12-2015 дата публикации

Organic compound anthracene derivative and light emitting element light emitting device and electronic appliance using anthracene derivative

Номер: KR101579918B1

신규한 안트라센 유도체 및 신규한 유기 화합물을 제공하는 것을 과제로 한다. 또한, 발광 효율이 높은 발광소자를 제공하는 것을 과제로 한다. 또한, 색 순도가 좋은 청색 발광을 얻을 수 있는 발광소자를 제공하는 것을 과제로 한다. 또한, 소비전력이 저감된 발광장치 및 전자 기기를 제공하는 것을 과제로 한다. 하기 일반식 (1)로 나타내어지는 안트라센 유도체 및 하기 일반식 (8)로 나타내어지는 유기 화합물을 제공한다. 또한, 하기 일반식 (1)로 나타내어지는 안트라센 유도체를 사용함으로써, 발광 효율이 높은 발광소자를 얻을 수 있다. 또한, 하기 일반식 (1)로 나타내어지는 안트라센 유도체를 사용함으로써, 색 순도가 높은 청색 발광을 얻을 수 있는 발광소자를 얻을 수 있다. And to provide a novel anthracene derivative and a novel organic compound. Another object of the present invention is to provide a light emitting device having high light emitting efficiency. It is another object of the present invention to provide a light emitting element which can obtain blue light emission with good color purity. It is another object of the present invention to provide a light emitting device and an electronic device with reduced power consumption. An anthracene derivative represented by the following general formula (1) and an organic compound represented by the following general formula (8) are provided. Further, by using the anthracene derivative represented by the following general formula (1), a light emitting device having high light emitting efficiency can be obtained. Further, by using the anthracene derivative represented by the following general formula (1), it is possible to obtain a light emitting device capable of emitting blue light with high color purity. 안트라센 유도체, 유기 화합물, 발광소자, 발광장치, Anthracene derivatives, organic compounds, light emitting devices, light emitting devices,

Подробнее
04-10-2000 дата публикации

Tricyclic 1-aminoethylpyrrol derivative

Номер: CN1057083C
Принадлежит: F Hoffmann La Roche AG

本发明涉及式I所示三环的吡咯衍生物及其可药用酸加成盐,式中各基团定义详见说明书,这些新颖化合物具有有价值的药理性能,可用于治疗和预防各种疾病。

Подробнее
01-02-2017 дата публикации

Functional norbornanyl ester derivatives, polymers and process for preparing same

Номер: CN104379553B
Автор: 余蕙
Принадлежит: Individual

本发明涉及一种新的功能性降冰片酯衍生物和/或聚合物组成,该功能性降冰片酯衍生物和/或聚合物可以方便地通过由相应的二烯烃和二烯亲和物所得到的狄尔斯‑阿尔德反应加成物与羧酸进行反应来制备。本发明主要涉及一种生产环状化工原料的新方法,这种环状化工原料可用于制造涂料,油墨,粘合剂,增塑剂,热塑性或热固性塑料和功能性聚合物。

Подробнее
10-10-2010 дата публикации

Novel substituted tetracyclic derivatives of tetrahydropyran, pyrrolidine and tetrahydrothiophene

Номер: RU2401257C2

FIELD: chemistry. SUBSTANCE: invention relates to novel substituted tetracyclic derivatives of tetrahydropyran, pyrrolidine and tetrahydrothiophene of general formula (I), their pharmaceutically acceptable addition salts, their stereochemically isomeric forms, their N-oxide forms, in which all substitutes are defined in claim 1 of the formula of invention. These compounds have binding affinity to serotonin receptors, particularly 5-HT 2A and 5-HT 2C receptors, and to dopamine receptors particularly D2 dopamine receptors, and have norepiniphrine reuptake inhibition properties. The invention also relates to a pharmaceutical composition containing said compounds, method of preparing said composition and use of said compounds as medicinal agents, particularly for preventing and/or treating several psychiatric and neurological disorders. EFFECT: new compounds have useful biological properties. 12 cl, 3 tbl, 49 ex РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) 2 401 257 (51) МПК C07D C07D C07D C07D C07D C07D ФЕДЕРАЛЬНАЯ СЛУЖБА C07D ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ, C07D ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ A61K A61K (12) ОПИСАНИЕ 209/70 487/04 491/044 333/80 311/94 413/06 211/18 307/93 31/343 31/352 (24) Дата начала отсчета срока действия патента: 06.12.2005 (43) Дата публикации заявки: 20.01.2009 (73) Патентообладатель(и): ЯНССЕН ФАРМАЦЕВТИКА Н.В. (BE) (85) Дата перевода заявки PCT на национальную фазу: 09.07.2007 C 2 C 2 (56) Список документов, цитированных в отчете о поиске: Ueda K., et al, Chem. and Pharm. Bull. Pharm. Soc. Of Japan, 1978, v.26, no.10, p.3058-3070. Мао H. et al, Tetrahedron Letters, 2002, v.43, no.48, 25, p.8697-8700. WO 9919317 A1, 22.04.1999. WO 9738991 A1, 23.10.1997. RU 2197490 C2, 27.04.2003. RU 2104279 C1, 10.02.1998. RU 2001110075 A, 10.02.2003. (72) Автор(ы): СИД-НУНЬЕС Хосе Мария (ES), МЕГЕНС Антониус Адрианус Хендрикус Петрус (BE), ТРАБАНКО-СУАРЕС Андрес Авелино (ES), КОУКНИ Мохамед (BE), ХОРНАРТ Джорж Жозеф Корнелиус (BE), КОМПЕРНОЛЛЕ Франс Йозеф Корнелиус (BE), ...

Подробнее
16-10-2018 дата публикации

1',2',5'-trisubstituted fulleropyrrolidines, methods for production and use thereof in photovoltaic cell

Номер: RU2669782C2

FIELD: chemistry.SUBSTANCE: invention relates to 1',2',5'-trisubstituted fulleropyrrolidines of formula (1), where Cis the carbon skeleton of fullerene C, in which R and R' are the same or mutually different and represent a substituent in the form of a C-Calkyl group with a normal or branched structure, Ris hydrogen, Rrepresents a substituent in the form of a C-Calkoxy group with a normal or branched structure, -O-(CH)-O-(CH)-CHgroup, while n and m represent the number of substituents Rand Rin the corresponding phenyl rings which are attached to the pyrrolidine moiety and are an integer from 1 to 3, a method for the preparation of fulleropyrrolidines of formula (1) and their use in photovoltaic cells, preferably in organic solar cells with volumetric heterojunction and photodetectors to improve open-circuit voltage and energy conversion efficiency in solar cells..EFFECT: in the invention 1',2',5'-trisubstituted fulleropyrrolidines, a method for their preparation and use in a photovoltaic cell are proposed.11 cl, 3 tbl, 2 ex, 4 dwg РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2 669 782 C2 (51) МПК C07D 209/70 (2006.01) H01L 51/42 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ (52) СПК C07D 209/70 (2006.01); H01L 51/42 (2006.01); H01L 51/0047 (2006.01) (21)(22) Заявка: 2016121444, 06.02.2015 (24) Дата начала отсчета срока действия патента: Дата регистрации: 16.10.2018 07.02.2014 EP 14154323.1 (43) Дата публикации заявки: 13.03.2018 Бюл. № 8 (56) Список документов, цитированных в отчете о поиске: WO 2009063785 A1, 22.05.2009. US (45) Опубликовано: 16.10.2018 Бюл. № 29 2011193072 A1, 11.08.2011. US 2011001093 A1, 06.01.2011. WO 2009035017 A1, 19.03.2009. RU 2005110567 A, 20.10.2006. (85) Дата начала рассмотрения заявки PCT на национальной фазе: 07.09.2016 (86) Заявка PCT: C 2 C 2 (73) Патентообладатель(и): Федеральное государственное бюджетное учреждение науки Институт проблем химической физики ...

Подробнее
20-01-2006 дата публикации

ISOINDOLINE DERIVATIVES

Номер: RU2005120003A

ÐÎÑÑÈÉÑÊÀß ÔÅÄÅÐÀÖÈß (19) RU (11) 2005 120 003 (13) A (51) ÌÏÊ C07D 209/46 (2006.01) ÔÅÄÅÐÀËÜÍÀß ÑËÓÆÁÀ ÏÎ ÈÍÒÅËËÅÊÒÓÀËÜÍÎÉ ÑÎÁÑÒÂÅÍÍÎÑÒÈ, ÏÀÒÅÍÒÀÌ È ÒÎÂÀÐÍÛÌ ÇÍÀÊÀÌ (12) ÇÀßÂÊÀ ÍÀ ÈÇÎÁÐÅÒÅÍÈÅ (21), (22) Çà âêà: 2005120003/04, 25.11.2003 (71) Çà âèòåëü(è): ÌÀÐÓÈÑÈ ÔÀÐÌÀÑÜÞÒÈÊÀË ÊÎ., ËÒÄ. (JP) (30) Ïðèîðèòåò: 26.11.2002 JP 2002-342399 (43) Äàòà ïóáëèêàöèè çà âêè: 20.01.2006 Áþë. ¹ 02 (86) Çà âêà PCT: JP 03/14986 (25.11.2003) Àäðåñ äë ïåðåïèñêè: 103735, Ìîñêâà, óë. Èëüèíêà, 5/2, ÎÎÎ "Ñîþçïàòåíò", ïàò.ïîâ. À.Ï.Àãóðååâó (54) ÏÐÎÈÇÂÎÄÍÛÅ ÈÇÎÈÍÄÎËÈÍÀ R U A 2 0 0 5 1 2 0 0 0 3 A Ôîðìóëà èçîáðåòåíè 1. Ñîåäèíåíèå ôîðìóëû (I) ãäå R1 ïðåäñòàâë þò ñîáîé îäèíàêîâûå èëè ðàçëè÷íûå 1-3 ãðóïïû, êàæäà èç êîòîðûõ âûáðàíà èç ãðóïïû, ñîñòî ùåé èç C1-3 àëêèëà è C1-3 àëêîêñè, èëè êîãäà R1 âë þòñ äâóì ñìåæíûìè ãðóïïàìè, äâå ãðóïïû R1, âç òûå, âìåñòå ìîãóò îáðàçîâûâàòü íàñûùåííóþ èëè íåíàñûùåííóþ 5- èëè 6-÷ëåííóþ öèêëè÷åñêóþ ãðóïïó, êîòîðà ìîæåò èìåòü 1 èëè 2 ãåòåðîàòîìà, âûáðàííûõ èç ãðóïïû, ñîñòî ùåé èç ñåðû, àçîòà è êèñëîðîäà: Õ ïðåäñòàâë åò ñîáîé êèñëîðîä èëè ñåðó: R2 âûáðàí èç ãðóïïû, ñîñòî ùåé èç ôåíèëà, áåíçèëà, ïèðèäèëà, ïèðèäèëìåòèëà, ïèðèìèäèíèëà, öèêëîãåêñèëà, ìåòèëïèïåðàçèíèëà, èíäàíèëà è íàôòèëà, êàæäûé èç êîòîðûõ ìîæåò íåîá çàòåëüíî áûòü çàìåùåí; ïðè óñëîâèè, ÷òî êîãäà R2 ïðåäñòàâë åò ñîáîé ôåíèë, 3- è 4-ïîëîæåíè ôåíèëüíîãî îñòàòêà íå âë þòñ çàìåùåííüìè ñ ïîìîùüþ àëêîêñèãðóïï îäíîâðåìåííî: îáîçíà÷àåò ïðîñòóþ èëè äâîéíóþ ñâ çü: è L ïðåäñòàâë åò ñîáîé Ñòðàíèöà: 1 RU 2 0 0 5 1 2 0 0 0 3 (74) Ïàòåíòíûé ïîâåðåííûé: Àãóðååâ Àëåêñàíäð Ïàâëîâè÷ (87) Ïóáëèêàöè PCT: WO 2004/048332 (10.06.2004) R U (85) Äàòà ïåðåâîäà çà âêè PCT íà íàöèîíàëüíóþ ôàçó: 27.06.2005 (72) Àâòîð(û): ÒÎÅÎÊÀ Êîóõåé (JP), ÊÀÍÀÌÈÒÑÓ Íîðèìàñà (JP), ÅÑÈÌÓÐÀ Ìàñàêàçó (JP), ÊÓÐÈßÌÀ Õàðóî (JP), ÒÀÌÓÐÀ Òàêàñè (JP) ãäå n âë åòñ öåëûì ÷èñëîì îò 1 äî 8; ãäå R3 âûáðàí èç ãðóïïû, ñîñòî ùåé èç âîäîðîäà, ëèíåéíîãî èëè ðàçâåòâëåííîãî C1-8 àëêèëà, C1-3 àëêèëà, çàìåùåííîãî, ïî êðàéíåé ìåðå, îäíèì èç àòîìîâ ôòîðà, öèêëîïåíòèëüíîé, ...

Подробнее
10-04-1999 дата публикации

Pyrrole tricyclic derivatives, a pharmaceutical preparation

Номер: RU2128649C1
Принадлежит: Ф.Хоффман-Ля Рош Аг

FIELD: organic chemistry, medicine, pharmacy. SUBSTANCE: invention relates to tricyclic derivatives of pyrrole of the general formula (I) where R 1 -R 4 mean hydrogen, halogen atom, lower alkyl, phenyl, cycloalkyl or lower alkoxy-group and R 2 means additionally lower alkoxycarbonyl, acyloxy or mesyloxy-group; R 5 means lower alkyl; R 6 , R 7 mean hydrogen atom or lower alkyl; X means CH 2 CH(C 6 H 5 )-, -CH=C(C 6 H 5 )-, -YCH 2 -,, -CH=CH- or C(R 11 R 12 ) n ;; R 11 and R 12 mean hydrogen atom, phenyl and lower alkyl, respectively; n = 1-3 and Y means O or S, and to pharmaceutically acceptable acid-additive salts also. Invention relates to also a pharmaceutical preparation showing capability to bind with serotonine receptors. Synthesized compounds are effective in prophylaxis and treatment of patients with central nervous system disorders, for example, depression, bipolar disorders, fear state, dream and sexual disorders, psychosis, migraines, schizophrenia and other morbid states associated with headache, disorders associated with personal senses or obsession, social phobia or panic attacks, psychic organic disorders, psychic disorders in children, memory disorders associated with age, disorders of contacts with other humans, morbid passion, obesity, bulimia and so on; disorders of nervous system functions caused by traumas, brain hemorrhage, nervous-degenerative sicknesses and so on; cardiovascular disorders, high blood pressure, thrombosis, insult and so on; gastroenteric disorders, dysfunction of gastroenteric tract motor activity. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 12 cl, 77 ex БбУ9зЗсЬс ПЧ Го (19) РОССИЙСКОЕ АГЕНТСТВО ПО ПАТЕНТАМ И ТОВАРНЫМ ЗНАКАМ (51) МПК 13) ВИ "” 2 128 649 ^^ Сл С 070 209/58, 209/60, 491/052, 513/04, А 61 К 31/40 12) ОПИСАНИЕ ИЗОБРЕТЕНИЯ К ПАТЕНТУ РОССИЙСКОЙ ФЕДЕРАЦИИ (21), (22) Заявка: 94037968/04, 20.10.1994 (30) Приоритет: 22.10.1993 СН 3202/93 17.08.1994 СН 2529/94 (46) Дата публикации: 10.04. ...

Подробнее
13-03-2018 дата публикации

Patent RU2016121444A3

Номер: RU2016121444A3
Автор:
Принадлежит:

РОССИЙСКАЯ ФЕДЕРАЦИЯ (19) RU (11) (13) 2016 121 444 A (51) МПК C07D 209/70 (2006.01) ФЕДЕРАЛЬНАЯ СЛУЖБА ПО ИНТЕЛЛЕКТУАЛЬНОЙ СОБСТВЕННОСТИ (12) ЗАЯВКА НА ИЗОБРЕТЕНИЕ (21)(22) Заявка: 2016121444, 06.02.2015 (71) Заявитель(и): Федеральное государственное бюджетное учреждение науки Институт проблем химической физики Российской Академии наук (ИПХФ РАН) (RU) Приоритет(ы): (30) Конвенционный приоритет: 07.02.2014 RU EP14154323.1 (85) Дата начала рассмотрения заявки PCT на национальной фазе: 07.09.2016 (86) Заявка PCT: (87) Публикация заявки PCT: Адрес для переписки: 142432, Московская обл., г. Черноголовка, пр-кт Академика Семенова, 1, Федеральное государственное бюджетное учреждение науки Институт проблем химической физики Российской Академии наук (ИПХФ РАН), директору ИПХФ РАН, академику С.М. Алдошину (54) 1',2',5'-тризамещенные фуллеропирролидины, способ их получения и применение в фотовольтаической ячейке R U (57) Формула изобретения 1. Фуллеропирролидины с общей формулой (1) где C2n - углеродный каркас фуллерена С60 или С70, в которых R и R' - одинаковые или взаимно различающиеся и представляют собой заместитель Стр.: 1 A 2 0 1 6 1 2 1 4 4 4 A WO 2016/003316 (07.01.2016) 2 0 1 6 1 2 1 4 4 4 RU 2015/000076 (06.02.2015) (72) Автор(ы): Трошин Павел Анатольевич (RU), Новиков Дмитрий Викторович (RU), Мухачева Ольга Андреевна (RU), Мумятов Александр Валерьевич (RU), Пруднов Федор Анатольевич (RU) R U (43) Дата публикации заявки: 13.03.2018 Бюл. № 08 A 2 0 1 6 1 2 1 4 4 4 A R U 2 0 1 6 1 2 1 4 4 4 Стр.: 2 R U в виде произвольным образом замещенной алкильной группы С1-С20, галоидалкильной группы С1-С20, предпочтительно фторалкильной группы С1-С20, алкилэфирной группы C1-С20, арил-С1-С20 алкильной группы или гетероарил-С1-С20 алкильной группы, R1 и R2 - одинаковые или не зависят друг от друга и представляют собой заместитель в виде атома водорода, произвольным образом замещенной алкильной группы С1-С20 , галоидалкильной группы С1-С20, предпочтительно фторалкильной группы С1- ...

Подробнее
12-07-2019 дата публикации

Fullerene chemistry amino benzenes derivates and its preparation method and application

Номер: CN110003087A

本发明公开了式(Ⅰ)所示的富勒烯吡咯烷苯胺类衍生物及其制备方法,氨基酸与对胺基苯甲醛反应生成甲亚胺叶立德,再与富勒烯进行[1,3]环加成反应得到富勒烯吡咯烷苯胺类衍生物。该富勒烯衍生物作为一种光稳定剂用于聚苯乙烯制品时,其光稳定效果明显优于富勒烯C 60 。 式中:R 1 =‑CH 3 ,‑C 2 H 5 ,R 2 =‑H,‑CH 2 ‑C 6 H 5 ,‑CH 2 ‑C 6 H 5 ‑OCH 3 。

Подробнее
27-03-2017 дата публикации

Aromatic amine derivative and organic electroluminescence element using same

Номер: KR101720395B1

하기 화학식 1로 표시되는 방향족 아민 유도체. [화학식 1] (화학식 1 중, L 1 , L 2 , Ar 1 , Ar 2 , R 1 , R 2 , a, b 및 Q는 명세서에서 정의한 바와 같다.) 상기 방향족 아민 유도체를 함유하는 유기 박막층을 1층 이상 갖는 유기 전기발광 소자는 발광 효율이 높고 장수명이다. An aromatic amine derivative represented by the following formula (1). [Chemical Formula 1] (Wherein L 1 , L 2 , Ar 1 , Ar 2 , R 1 , R 2 , a, b and Q are as defined in the specification) Organic electroluminescent devices having one or more organic thin film layers containing the aromatic amine derivatives have high luminous efficiency and long life.

Подробнее
30-07-2019 дата публикации

Fullerene phenylate class pyrrolidines phenylate analog derivative and its preparation method and application

Номер: CN110066238A

本发明公开了式(Ⅰ)所示的富勒烯吡咯烷苯醚类衍生物的制备方法及应用。首先以氨基酸、对烷氧基苯甲醛为原料生成甲亚胺叶立德,再与富勒烯进行[1,3]环加成反应得到富勒烯吡咯烷苯醚类衍生物。该富勒烯吡咯烷苯醚类衍生物作为一种光稳定剂单独作用于聚苯乙烯时,其光稳定性明显优于富勒烯。 式中:R 1 =‑CH 3 ,‑C 2 H 5 ,R 2 =‑H,‑CH 2 ‑C 6 H 5 ,‑CH 2 ‑C 6 H 5 ‑OCH 3 。

Подробнее
12-11-1976 дата публикации

TRIARYL-1,1,1 ALKYLAMINES AND THEIR PREPARATION PROCESS

Номер: FR2307530A1
Автор: [UNK]
Принадлежит: GD Searle LLC

Подробнее
07-09-1973 дата публикации

Patent FR2169181A1

Номер: FR2169181A1
Автор: [UNK]
Принадлежит: Boehringer Mannheim GmbH

Подробнее