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Небесная энциклопедия

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

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Мониторинг СМИ

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

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Форма поиска

Поддерживает ввод нескольких поисковых фраз (по одной на строку). При поиске обеспечивает поддержку морфологии русского и английского языка
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Применить Всего найдено 99. Отображено 99.
28-02-2002 дата публикации

ТРИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ, ОБЛАДАЮЩИЕ АКТИВНОСТЬЮ В ОТНОШЕНИИ ИНТЕГРИНОВ, В ЧАСТНОСТИ В ОТНОШЕНИИ ИНТЕГРИНА АЛЬФАvБЕТА 3, СПОСОБ ИХ ПОЛУЧЕНИЯ И ПРОМЕЖУТОЧНЫЕ СОЕДИНЕНИЯ, ИСПОЛЬЗУЕМЫЕ В ЭТОМ СПОСОБЕ, ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МЕДИКАМЕНТОВ И СОДЕРЖАЩИЕ ИХ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ

Номер: EA0000002271B1

... 1. Соединения общей формулы (I) в которой R1обозначает группу -О-[А]-[В]-COR6, в которой R6обозначает -ОН, C1-С6алкокси, -О-СН2-СН(ОН)-СН2OН, [A] обозначает группу C1-С6алкилен, возможно замещенный оксогруппой, [B] обозначает радикал -CH(Z)- или простую связь, Z обозначает группу -NHCO2Rc, или -NHSO2Rc, где Rcобозначает радикал фенил(C1-С4)алкил-, хинолинил или пиридинилимидазолил(C1-С4)алкил-, R2и R3, одинаковые или разные, обозначают атом водорода, радикал гидроксил, радикал C1-С6алкокси или R2и R3образуют вместе группу -O-(C1-С3-алкилен)-O- или -O-C(Ph)2-O, G обозначает радикал -NH-C-(=X)-NH2, в котором Х обозначает S, О или NH, или радикал -NH-Het', где Het' обозначает имидазол, возможно замещенный группой оксо, пиримидин, диазепин или бензимидазол формул где р равно 2, 3 или 4, пунктирные линии представляют собой возможную вторую связь, а также соли присоединения с кислотами и основаниями и сложные эфиры, R1, R2и R3могут находиться в положении 8, 9 или 10 трицикла. 2. Соединения общей ...

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17-04-2007 дата публикации

NOVEL TRICYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Номер: CA0002318381C
Принадлежит: LES LABORATOIRES SERVIER

L'invention concerne de nouveaux composés répondant à la formule (I) (See formula I) dans laquelle A forme avec le groupement auquel il est lié un système tricyclique choisi parmi A1, A2, A3 et A4: (See formula A1, A2, A3, A4) 137 R1 représente un atome d'hydrogène ou d'halogène, ou un groupement alkyle, alkoxy, hydroxy ou oxo; R2 et R3, identiques ou différents, représentent un atome d'halogène ou un groupement R a, OR a, COR a, OCOR a ou COOR a dans lequel R a représente un atome d'hydrogène ou un groupement alkyle, trihalogénoalkyle, alcényle, alcynyle, cycloalkyle, cycloalkyle ou aryle, les représentations (R2)m et (R3)m' signifiant que le cycle concerné est éventuellement substitué par 1 à 3 groupements identiques ou différents appartenant aux définitions de R2 et R3; X représente, lorsque A représente un système tricyclique A1, A2, A3 ou A4, un atome de soufre, un groupement (CH2)q où q vaut 1 ou 2, un groupement -CH=CH- ou un groupement NR4 dans lequel R4 représente un atome d'hydrogène ...

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30-12-1996 дата публикации

НОВЫЕ ТРИЦИКЛИЧЕСКИЕ ПРОИЗВОДНЫЕ, СПОСОБ ИХ ПОЛУЧЕНИЯ, СПОСОБЫ ПОЛУЧЕНИЯ ОПТИЧЕСКИ АКТИВНЫХ ИЛИ РАЦЕМИЧЕСКИХ КОЛХИЦИНА И ТИОКОЛХИЦИНА, ИХ АНАЛОГОВ ИЛИ ПРОИЗВОДНЫХ С ИСПОЛЬЗОВАНИЕМ ТРИЦИКЛИЧЕСКИХ СОЕДИНЕНИЙ И ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ СИНТЕЗА

Номер: EA199600007A3
Принадлежит:

Изобретение относится к трициклическим производным общей формулы I, где R1 и R2 - алкил, R3 - водород или A-SO2, при этом А - алкил или фенил с возможностью замещения, или R1 и R3 - водород или алкил, a R1 - А-SO2, или R1, R2 и R3 - водород или алкил, или R1 - A-SO2 или водород, a R2 и R3 образуют защитную группу, или R3 - А-SO2, a R1 и R3 образуют защитную группу, или R1 - водород, a R2 и R3 - алкил или образуют защитную группу, которые могут быть использованы для получения рацемических и оптически активных колхицина и тиоколхицина, их аналогов или производных. Изобретение относится также к способам получения трициклических производных формулы I, к способу получения колхицина и тиоколхицина с использованием соединений формулы I и к промежуточным соединениям синтеза.

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01-10-1996 дата публикации

НОВЫЕ ТРИЦИКЛИЧЕСКИЕ ПРОИЗВОДНЫЕ, СПОСОБ ИХ ПОЛУЧЕНИЯ, СПОСОБЫ ПОЛУЧЕНИЯ ОПТИЧЕСКИ АКТИВНЫХ ИЛИ РАЦЕМИЧЕСКИХ КОЛХИЦИНА И ТИОКОЛХИЦИНА, ИХ АНАЛОГОВ ИЛИ ПРОИЗВОДНЫХ С ИСПОЛЬЗОВАНИЕМ ТРИЦИКЛИЧЕСКИХ СОЕДИНЕНИЙ И ПРОМЕЖУТОЧНЫЕ ПРОДУКТЫ СИНТЕЗА

Номер: EA199600007A2
Принадлежит:

Изобретение относится к трициклическим производным общей формулы I где R1 и R2 - алкил, R3 - водород или A-SO2, при этом А - алкил или фенил с возможностью замещения, или R2 и R3 - водород или алкил, a R1 - A-SO2, или R1, R2 и R3 - водород или алкил, или R1 - A-SO2 или водород, a R2 и R3 образуют защитную группу, или R3 - A-SO2, a R1 и R2 образуют защитную группу, или R1 - водород, a R2 и R3 - алкил или образуют защитную группу, которые могут быть использованы для получения рацемических и оптически активных колхицина и тиоколхицина, их аналогов или производных. Изобретение относится также к способам получения трициклических производных формулы I, к способу получения колхицина и тиоколхицина с использованием соединений формулы I и к промежуточным соединениям синтеза.

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26-09-1997 дата публикации

NEW COMPOSE TRICYCLIC, THEIR METHOD OF PREPARATION, AND THEM INTERMEDIARIES OF THIS PROCESS, THEIR APPLICATION AS DRUGS AND THE COMPOSITIONS PHARMACEUTICAL CONTAINING THEM

Номер: FR0002746394A1
Принадлежит:

L'invention a pour objet les produits de formule (I): (CF DESSIN DANS BOPI) dans laquelle R1 , R2 , R3 , R4 , R5 et G sont tels que définis dans la description, les traits en pointillés représentent une éventuelle seconde liaison, ainsi que les sels d'addition avec les acides et les bases, leur procédé de préparation et les intermédiaires de ce procédé, leur application à titre de médicaments et les compositions pharmaceutiques les renfermant.

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04-12-2014 дата публикации

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR MODULATORS AND USES THEREOF IN REGULATING BLOOD GLUCOSE LEVELS

Номер: WO2014193832A2
Принадлежит:

The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor.

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25-09-1997 дата публикации

TRICYCLIC COMPOUNDS HAVING ACTIVITY SPECIFIC FOR INTEGRINS, PARTICULARLY 'alpha'v'beta'3 INTEGRINS, METHOD FOR PREPARING SAME, INTERMEDIATES THEREFOR, USE OF SAID COMPOUNDS AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Номер: WO1997034865A1
Принадлежит:

Compounds of formula (I), wherein R1, R2, R3, R4, R5 and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.

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22-07-1999 дата публикации

NOVEL TRICYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Номер: WO1999036392A1
Принадлежит:

The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m' are such as defined in the description; n represents an integer such that 0≤n≤3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.

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30-06-2005 дата публикации

CYCLOPROPANE COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Номер: CA0002549660A1
Принадлежит:

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is - (CH2) m-X- (CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, -(CH2)p-X1- (CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is -C02R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, - (CH2)m12-X12-(CH2)m12-R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug ...

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06-09-1996 дата публикации

NOVEL TRICYCLIC DERIVATIVES, THEIR PREPARATION, THEIR USE FOR THE PREPARATION OF COLCHICINE AND THIOCOLCHICINE OPTICALLY ACTIVE OR RACEMIC AND ANALOGS OR DERIVATIVES AND INTERMEDIATES

Номер: FR0002731217A1
Принадлежит:

L'invention concerne les composés (I): (CF DESSIN DANS BOPI) où R1 et R2 = alkyle et R3 = hydrogène ou ASO2 , A étant notamment alkyle ou phényle éventuellement substitué, ou R2 et R3 = hydrogène ou alkyle et R1 = ASO2 , ou R1 , R2 et R3 = hydrogène ou alkyle, ou R1 = ASO2 ou hydrogène et R2 et R3 forment un groupement protecteur, ou R3 = ASO2 et R1 et R2 forment un groupement protecteur, leur préparation, leur application à la préparation de la colchicine et de la thiocolchicine racémiques et optiquement actives et d'analogues ou dérivés, intermédiaires. ainsi que des intermédiaires ...

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22-06-2000 дата публикации

TUBULIN-BINDING AGENTS

Номер: WO2000035865A2
Принадлежит:

La présente invention concerne des dérivés de composés de liaison de tubuline comprenant un groupe caractéristique de (poly)fluorobenzène, de fluoropyridine, ou de fluoronitrobenzène incorporé ou ajouté à la structure. Ces dérivés peuvent être utilisés comme agents antimitotiques et peuvent être considérés comme des modificateurs covalents de tubuline. La stratégie mise au point pour chacun des composés consiste: i) à ajouter un électrophile fluoré(par exemple pentafluorophénylsulfonamido, 2-fluoropyridyle, or 3,5-dinitro-4-fluorophényle) à un groupe fonctionnel existant dans un produit naturel; ii) à remplacer un noyau aromatique dans un produit naturel par un électrophile fluoré; ou iii) à attacher un électrophile fluoré à une valence ouverte dans une partie de la molécule n'empêchant pas la reconnaissance et la liaison à un site de tubuline. L'invention concerne également des dérivés à base de colchicine, stéganacine, podophyllotoxine, nocodazole, combretastatine, curacine A, vinblastine ...

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25-04-2013 дата публикации

INGENANE-TYPE DITERPENE COMPOUND, AND PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING VIRAL INFECTIOUS DISEASES CONTAINING SAME

Номер: WO2013058484A3
Принадлежит:

The present invention relates to an ingenane-type diterpene compound derived from Euphorbia kansui, and a pharmaceutical composition for treating or preventing viral infectious diseases, a dietary supplement for preventing or improving viral infectious diseases and a composition for enhancing the production of interferon-γ, containing the same. Furthermore, the present invention relates to a method for preventing or treating viral infectious diseases, comprising the step of administering a therapeutically effective amount of the composition to an individual with a viral infectious disease or a risk thereof.

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29-09-1994 дата публикации

N-ACYL-DEMETHYLCOLCHICINE DERIVATIVES AND THEIR USE AS MAMMALIAN DNA TOPOISOMERASE II INHIBITORS

Номер: WO1994021598A1
Принадлежит:

A novel antiproliferative drug and methods are disclosed. The drug has general structural formula (I) or (II) where R1=OR1', SR1', or NR1'R1", where R1' and R1" are the same or different and are H or lower alkyl groups, and R2 is an aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells.

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16-11-2004 дата публикации

Preparation of Aromatic Nitriles

Номер: KR0100452077B1
Автор:
Принадлежит:

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23-02-2006 дата публикации

Estrogen receptor modulators

Номер: US20060041003A1
Принадлежит:

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

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23-07-1999 дата публикации

Tricyclic compounds having affinity for melatonin receptors for treatment of melatoninergic system disorders - such as insomnia, fatigue, schizophrenia, senile dementia, etc.

Номер: FR0002773798A1
Принадлежит:

L'invention concerne les composé de formule (I) : dans laquelle : . A forme un système tricyclique de formule A1, A2, A3 ou A4, . R1 représente un atome d'hydrogène, un groupement alkyle, hydroxy, alkoxy ou oxo, . (R2) m et (R3) m sont tels que définis dans la description, . n représente un entier tel que 0 ≤ n ≤ 3 . p représente un entier tel que 0 ≤ p ≤ 4 . B est tel que défini dans la description. Médicaments.

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04-12-2014 дата публикации

SYNTHESIS OF GALANAL COMPOUNDS AND ANALOGUES THEREOF

Номер: WO2014193837A8
Принадлежит:

The present disclosure provides methods of preparing glucagon-like peptide-1 (GLP-1) receptor modulators, such as compounds of Formula (II) or (VI), or intermediates thereof. The compounds that may be prepared by the described methods are useful for regulating blood glucose levels and/or treating a disease mediated by a GLP-1 receptor (e.g.diabetes).

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19-12-1996 дата публикации

PROTEIN KINASE C MODULATORS .X.

Номер: WO1996040614A1
Принадлежит:

Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from diterpene and benzolactan phorboids.

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26-08-2014 дата публикации

Prostratin analogs, bryostatin analogs, prodrugs, synthetic methods, and methods of use

Номер: US0008816122B2

Embodiments of the present disclosure provide for prostratin analogs, bryostatin analogs, prodrugs of prostratin and prostratin analogs, methods of making prostratin analogs, and methods of making prodrugs of prostratin and prostratin analogs, methods of use of prostratin analogs, bryostatin analogs, and prodrugs thereof, and the like.

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01-02-2007 дата публикации

SYNTHESIS OF SCABRONINES AND ANALOGUES THEREOF

Номер: CA0002616028A1
Принадлежит:

A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.

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01-07-2004 дата публикации

Process for preparing brevifoliol

Номер: US20040127741A1

The present invention provides a process for production of an anticancer taxoid brevifoliol of the formula 1 from plants belonging to the genus Taxus by first extracting the dried and pulverized leaves of the plant with an alcohol preferably at a temperature in the range of 20-40° C. and then concentrating the solvent to obtain an alcoholic extract. The alcoholic extract obtained is then adsorbed with an adsorbent and the resulting adsorbed material is then dried at a temperature ranging from 20-50° C. for 4-48 hours. The dried adsorbed material is then extracted with a combination of an aliphatic solvent and a chlorinated solvent successively and concentrated to obtain a residue. The residue is subjected to gross fractionation using column chromatography such as silica gel, florosil and silicic acid followed by chromatography with a suitable adsorbent to get brevifoliol.

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21-12-2006 дата публикации

CYCLOPROPANE COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Номер: KR1020060132615A
Принадлежит:

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is - (CH2) m-X- (CH 2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, - (CH2)p-X1-(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X 1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is - C02R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, - (CH2)m12-X12-(CH2)m12-R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12is a single bond, etc. and R30 is a hydrogen atom, etc.; or a ...

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22-06-2000 дата публикации

TUBULIN-BINDING AGENTS

Номер: WO0000035865A3
Принадлежит:

La présente invention concerne des dérivés de composés de liaison de tubuline comprenant un groupe caractéristique de (poly)fluorobenzène, de fluoropyridine, ou de fluoronitrobenzène incorporé ou ajouté à la structure. Ces dérivés peuvent être utilisés comme agents antimitotiques et peuvent être considérés comme des modificateurs covalents de tubuline. La stratégie mise au point pour chacun des composés consiste: i) à ajouter un électrophile fluoré(par exemple pentafluorophénylsulfonamido, 2-fluoropyridyle, or 3,5-dinitro-4-fluorophényle) à un groupe fonctionnel existant dans un produit naturel; ii) à remplacer un noyau aromatique dans un produit naturel par un électrophile fluoré; ou iii) à attacher un électrophile fluoré à une valence ouverte dans une partie de la molécule n'empêchant pas la reconnaissance et la liaison à un site de tubuline. L'invention concerne également des dérivés à base de colchicine, stéganacine, podophyllotoxine, nocodazole, combretastatine, curacine A, vinblastine ...

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04-01-1994 дата публикации

Polycyclic amines useful as cerebrovascular agents

Номер: US0005276053A1
Автор: Johnson; Graham
Принадлежит: Warner-Lambert Company

A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

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01-02-2007 дата публикации

SYNTHESIS OF SCABRONINES AND ANALOGUES THEREOF

Номер: WO000002007013965A3
Принадлежит:

A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.

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09-11-1995 дата публикации

BENZOFURAN DERIVATIVES USEFUL AS INHIBITORS OF BONE RESORPTION

Номер: WO1995029907A1
Принадлежит:

This invention relates to a novel heterocyclic compound represented by formula (I), wherein X is O or S, Y is vinylene, or a group of formula: -NHCO-, -NHSO2-, -OCO-, -OCH2-, -NHCOCO-, -NHCOCH=CH-, -NHCOCH2-, -NHCONH- or (a) (wherein R6 is lower alkyl), Z is heterocyclic group which may have one or more suitable substituent(s), or aryl which may have one or more suitable substituent(s), 1 = 0, 1 and the other symbols are as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.

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28-09-1999 дата публикации

Tricyclic compounds

Номер: US0005959146A1
Принадлежит: Hoechst Marion Roussel

Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.

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25-04-2013 дата публикации

INGENANE-TYPE DITERPENE COMPOUND, AND PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING VIRAL INFECTIOUS DISEASES CONTAINING SAME

Номер: WO2013058484A2
Принадлежит:

The present invention relates to an ingenane-type diterpene compound derived from Euphorbia kansui, and a pharmaceutical composition for treating or preventing viral infectious diseases, a dietary supplement for preventing or improving viral infectious diseases and a composition for enhancing the production of interferon-γ, containing the same. Furthermore, the present invention relates to a method for preventing or treating viral infectious diseases, comprising the step of administering a therapeutically effective amount of the composition to an individual with a viral infectious disease or a risk thereof.

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04-12-2014 дата публикации

SYNTHESIS OF GALANAL COMPOUNDS AND ANALOGUES THEREOF

Номер: WO2014193837A1
Принадлежит:

The present disclosure provides methods of preparing glucagon-like peptide-1 (GLP-1) receptor modulators, such as compounds of Formula (II) or (VI), or intermediates thereof. The compounds that may be prepared by the described methods are useful for regulating blood glucose levels and/or treating a disease mediated by a GLP-1 receptor (e.g.diabetes).

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14-11-2013 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF FIBROMYALGIA PAIN

Номер: WO2013168004A3
Автор: KANDULA, Mahesh
Принадлежит:

The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of fibromyalgia pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, post herpetic neuralgia, diabetic neuropathy, bipolar depression, stress, cancer pain, and lower back pain.

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29-04-2013 дата публикации

INGENANE TYPE DITERPENE COMPOUND SEPARATED FROM AN EUPHORBIA KANSUI ROOT PARTS AND A PHARMACEUTICAL COMPOSITION FOR TREATMENT AND PREVENTION OF VIRUS INFECTION COMPRISING THE SAME

Номер: KR1020130042990A
Принадлежит:

PURPOSE: An ingenane type diterpene compound is provided to have activity deriving IFN-γ generation from NK cells, thereby treating and preventing virus infection. CONSTITUTION: A compound is represented by chemical formula 1. A pharmaceutical composition for treatment and prevention of virus infection comprising the same comprises a compound represented by chemical formula 2 as an active ingredient. In chemical formula 2, R1 is H, R2 is H, R3 is OCO-(CH2)10-CH3, and R4 is CO-CH(CH3)-CH(CH3)2; R1 is CO-CH(CH3)-CH(CH3)2, R2 is H, R3 is OCO-(CH2)10-CH3, and R4 is H; R1 is H, R2 is OCO-(CH2)8-CH3, R3 is H, and R4 is H; R1 is CO(CH=CH)-(CH2)4-CH3, R2 is OAc, R3 is H, and R4 is H; R1 is CO-CH(CH3)-CH(CH3)2, R2 is OCO-(CH2)14-CH3, R3 is OCO-(CH2)10-CH3, and R4 is H; or R1 is CO-CH(CH3)-CH(CH3)2, R2 is OH, R3 is OCO-(CH2)10-CH3, and R4 is H. COPYRIGHT KIPO 2013 ...

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20-05-1999 дата публикации

BENZOCYCLOHEPTENE DERIVATIVES

Номер: WO1999024397A1
Принадлежит:

A compound of formula (I) wherein R1 is a carboxy group or a protected carboxy group, R2 is a hydrogen atom, a hydroxy group or a protected hydroxy group, R3 is a hydrogen atom, a hydroxy group or a protected hydroxy group, in addition to the above definitions, R2 and R3 are combined together to form an oxo group or a lower alkylene group, R4 is a hydrogen atom, a hydroxy group or a protected hydroxy group, R5 and R6 are each optionally a substituted aryl group, A1 and A2 are each a lower alkylene group, and A and two adjacent carbon atoms of the benzene ring to be bonded with A form a seven-membered ring optionally containing an oxygen atom and optionally substituted with an epoxy group and its salt, process for preparing it, a pharmaceutical composition including it, and a use thereof.

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30-06-2005 дата публикации

CYCLOPROPANE COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Номер: WO2005058884A3
Принадлежит:

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is - (CH2)m-X- (CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, -(CH2)p-X1-(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is -C02R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, - (CH2)m12-X12-(CH2)m12-R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug ...

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12-06-2014 дата публикации

Ingenane type diterpene compound and a pharmaceutical composition for treatment and prevention of virus infection comprising the same

Номер: KR0101406201B1
Автор:
Принадлежит:

Подробнее
26-05-2005 дата публикации

Process for preparation of (6S,9R)-11-OXO-5,6,7,8,9,10-hexahydro-6,9-methanobenzocyclooctene

Номер: US20050112738A1
Принадлежит:

The present invention is directed to processes for the preparation of (6S,9R)-11-oxo-5,6,7,8,9,10-hexahydro-6,9-methanobenzocyclooctene. Racemic 11-oxo-5,6,7,8,9, 10-hexahydro-6,9-methanobenzocyclooctene has the Chemical Abstracts registry number 82799-14-2 and is useful in the preparation of compounds with pharmacological activity.

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14-11-2013 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF FIBROMYALGIA PAIN

Номер: WO2013168004A2
Автор: KANDULA, Mahesh
Принадлежит:

The invention relates to the compounds of formula (I) or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula (I), and methods for the treatment of fibromyalgia pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, post herpetic neuralgia, diabetic neuropathy, bipolar depression, stress, cancer pain, and lower back pain.

Подробнее
04-09-1996 дата публикации

Tricyclic derivatives, their preparation, their use in the preparation of optically active or racemic colchicine, thiocolchicine and analogues or derivatives, and intermediates

Номер: EP0000729933A1
Принадлежит:

New tri:cyclic derivs. useful in prepn. of colchicine and thiocolchicine Tricyclic cpds. of formula (I) are new. (a) R1, R2 = alkyl and R3 = H or A-SO2; (b) R2, R3 = both H or both alkyl and R1 = A-SO2-; (c) R1-R3 = all H or all alkyl; (d) R1 = A-SO2- or H and OR2+OR3 = -O-X-O-; (e) R3 = A-SO2-; OR2+OR3 = -O-X-O-; (f) R1 = H and R2, R3 = both alkyl or OR2+OR3 = -O-X-O-; A = alkyl, phenyl (opt. substd. by 1-3 alkyl) or naphthyl (opt. substd. by 1-5 alkyl); alkyl and alkyloxy = 1-6C; X = -B(OR4)-, alkyl, -C(O)- or -CR5R6-; R4 = H; R5, R6 = H, alkyl or phenyl (opt. substd. by 1-3 alkyl, hydroxy or alkoxy); or CR5R6 = 5 or 6 membered carbocycle.

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19-01-1993 дата публикации

Polycyclic amines useful as cerebrovascular agents

Номер: US0005180736A1
Автор: Johnson; Graham
Принадлежит: Warner-Lambert Company

A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

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01-02-2007 дата публикации

SYNTHESIS OF SCABRONINES AND ANALOGUES THEREOF

Номер: WO2007013965A2
Принадлежит:

A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.

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01-07-2004 дата публикации

PROCESS FOR ISOLATING BREVIFOLIOL

Номер: WO2004054959A1
Принадлежит:

The present invention provides a process for production of an anticancer taxoid brevifoliol of the formula (I), from plants belonging to the genus Taxus by first extracting the dried and pulverized leaves of the plant with an alcohol preferably at a temperature in the range of 20-40°C and then concentrating the solvent to obtain an alcoholic extract. The alcoholic extract obtained is then adsorbed with an adsorbent and the resulting adsorbed material is then dried at a temperature ranging from 20-50°C for 4-48 hours. The dried adsorbed material is then extracted with a combination of an aliphatic solvent and a chlorinated solvent successively and concentrated to obtain a residue. The residue is subjected to gross fractionation using column chromatography such as silica gel, florosil and silicic acid followed by chromatography with a suitable adsorbent to get brevifoliol.

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20-08-1997 дата публикации

Process for the preparation of aromatic nitriles

Номер: EP0000790234A1
Автор: Breitschuh, Richard
Принадлежит:

Benzo-, naphtho-, pyridine- or quinoline- nitrile (compound) preparation Preparation of a nitrile of formula Ar-CN (I) comprises reacting an aldehyde of formula Ar-CHO (II) with hydroxylamine sulphate, followed by dehydration. The reaction is carried out in the presence of a tertiary amine base (B) at 100-160, preferably 120-150 degrees C, with simultaneous removal of the water of reaction by distillation at 0.02-1.5 bar, preferably 0.1 bar to atmospheric pressure; then the ammonium salt is removed and (I) is isolated by usual methods. (B) is pyridine or quinoline (both optionally mono- or di- substituted, by Me and/or Et) or NR5R6R7; Ar = a group of formula (a); X = CH or N; R1, R2 = H, Cl, Br, 1-6 C alkyl, 1-6 C alkoxy, 1-6 C alkylamino, CN, phenyl, phenoxy, dimethylamino, piperidyl, morpholinyl or pyrrolidyl; or R1+R2 = a condensed benzene ring; R5 = branched 3-5 C alkyl or phenyl; R6, R7 = methyl or ethyl.

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01-04-2004 дата публикации

ESTROGEN RECEPTOR MODULATORS

Номер: WO2004026887A3
Принадлежит:

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget s disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Подробнее
30-06-2005 дата публикации

CYCLOPROPANE COMPOUNDS AND PHARMACEUTICAL USE THEREOF

Номер: WO2005058884A2
Принадлежит:

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is - (CH2)m-X- (CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, -(CH2)p-X1-(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is -C02R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, - (CH2)m12-X12-(CH2)m12-R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug ...

Подробнее
13-07-2005 дата публикации

ESTROGEN RECEPTOR MODULATORS

Номер: EP0001551820A2
Принадлежит:

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget s disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Подробнее
07-01-1999 дата публикации

TRICYCLIC COMPOUNDS HAVING ACTIVITY SPECIFIC FOR INTEGRINS, PARTICULARLY $g(a)v$g(b)3 INTEGRINS, METHOD FOR PREPARING SAME, INTERMEDIATES THEREFOR, USE OF SAID COMPOUNDS AS DRUGS, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Номер: EP0000888292A1
Принадлежит:

Compounds of formula (I), wherein R1, R2, R3, R4, R5 and G are as defined in the description and the dotted lines indicate an optional second bond, as well as the acid, base and ester addition salts thereof, a method for preparing said compounds, intermediates therefor, the use of said compounds as drugs, and pharmaceutical compositions containing same, are disclosed.

Подробнее
04-12-2014 дата публикации

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR MODULATORS AND USES THEREOF IN REGULATING BLOOD GLUCOSE LEVELS

Номер: WO2014193832A3
Принадлежит:

The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor.

Подробнее
01-04-2004 дата публикации

ESTROGEN RECEPTOR MODULATORS

Номер: WO2004026887A2
Принадлежит:

The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Paget s disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Подробнее
14-02-2008 дата публикации

PROCESS FOR PREPARING BREVIFOLIOL

Номер: US20080039641A1

The present invention provides a process for production of an anticancer taxoid brevifoliol of the formula I from plants belonging to the genus Taxus by first extracting the dried and pulverized leaves of the plant with an alcohol preferably at a temperature in the range of 20-40° C. and then. concentrating the solvent to obtain an alcoholic extract. The alcoholic extract obtained is then adsorbed with an adsorbent and the resulting adsorbed material is then dried at a temperature ranging from 20-50° C. for 4-48 hours. The dried adsorbed material is then extracted with a combination of an aliphatic solvent and a chlorinated solvent successively and concentrated to obtain a residue. The residue is subjected to gross fractionation using column chromatography such as silica gel, florosil and silicic acid followed by chromatography with a suitable adsorbent to get brevifoliol.

Подробнее
27-08-2014 дата публикации

INGENANE-TYPE DITERPENE COMPOUND, AND PHARMACEUTICAL COMPOSITION FOR TREATING OR PREVENTING VIRAL INFECTIOUS DISEASES CONTAINING SAME

Номер: EP2769973A2
Принадлежит:

The present invention relates to an injenane-type diterpene compound derived from Euphorbia kansui Liou, and a pharmaceutical composition for treating or preventing viral infectious diseases, a health functional food for preventing or ameliorating viral infectious diseases and a composition for enhancing the production of interferon-gamma, which comprise the injenane-type diterpene compound. Furthermore, the present invention relates to a method for preventing or treating viral infectious diseases including administering the composition to a subject having a viral infectious disease occurrence or a risk thereof with a therapeutically effective dose.

Подробнее
03-09-2014 дата публикации

Ingenane-Type Diterpene Compound, And Pharmaceutical Composition For Treating Or Preventing Viral Infectious Diseases Containing Same

Номер: CN104024212A
Принадлежит:

The present invention relates to an ingenane-type diterpene compound derived from Euphorbia kansui, and a pharmaceutical composition for treating or preventing viral infectious diseases, a dietary supplement for preventing or improving viral infectious diseases and a composition for enhancing the production of interferon-gamma, containing the same. Furthermore, the present invention relates to a method for preventing or treating viral infectious diseases, comprising the step of administering a therapeutically effective amount of the composition to an individual with a viral infectious disease or a risk thereof.

Подробнее
12-08-1991 дата публикации

POLYCYCLIC AMINES USEFUL AS CEREBROVASCULAR AGENTS

Номер: JP0003184943A
Принадлежит:

PURPOSE: To provide a cerebrovascular agent for treatment of neurodegenerative disorders including cerebrovascular diseases, comprising a polycyclic amine such as aminomethylhexahydrophenanthrene. CONSTITUTION: A compound of the formula [R1 and R2 are each H, an alkyl, alkenyl, arylalkyl or a pharmaceutically acceptable labile group, or R1 and R2 together form a heterocyclic ring; R3 and R4 are each H, an alkyl, OH, alkoxy, halogen, NH2, mono or dialkylamino, etc.; ring A may be thiophene; R5 and R6 are each H, an alkyl, alkenyl, OH, aldehyde, alkylcarbonyl, etc.; X' is CH2, O, S, etc.; X is CR7R8, CR7R8CH2, CR7=CR8, CHR7S, etc. (R7 and R8 are each H, an alkyl, OH, methoxy, etc.); n is 0 to 2], e.g. 1,3,4,10a- tetrahydro-N-2-propenyl-4a(2H)-phenanthreneamine, is incorporated as an active ingredient. COPYRIGHT: (C)1991,JPO ...

Подробнее
26-09-1990 дата публикации

Polycyclic amines useful as cerebrovascular agents

Номер: EP0000388977A3
Принадлежит:

Подробнее
11-10-2006 дата публикации

Номер: JP0003831445B2
Автор:
Принадлежит:

Подробнее
30-08-2000 дата публикации

BENZOCYCLOHEPTENE DERIVATIVES

Номер: EP0001030834A1
Принадлежит:

A compound of formula (I) wherein R1 is a carboxy group or a protected carboxy group, R2 is a hydrogen atom, a hydroxy group or a protected hydroxy group, R3 is a hydrogen atom, a hydroxy group or a protected hydroxy group, in addition to the above definitions, R2 and R3 are combined together to form an oxo group or a lower alkylene group, R4 is a hydrogen atom, a hydroxy group or a protected hydroxy group, R5 and R6 are each optionally a substituted aryl group, A1 and A2 are each a lower alkylene group, and A and two adjacent carbon atoms of the benzene ring to be bonded with A form a seven-membered ring optionally containing an oxygen atom and optionally substituted with an epoxy group and its salt, process for preparing it, a pharmaceutical composition including it, and a use thereof.

Подробнее
20-06-1995 дата публикации

Mammalian DNA topoisomerase II inhibitor and method

Номер: US0005426224A1

A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: см. иллюстрацию в PDF-документе where R1=OR1 ', SR1 ', or N(R1 'R1 ")2, where R1 ' and R1 " are H or lower alkyl groups, and R2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.

Подробнее
26-09-1990 дата публикации

Polycyclic amines useful as cerebrovascular agents

Номер: EP0000388977A2
Принадлежит:

A novel series of polycyclic amine derivatives, of formula I methods of making the compounds, novel intermediates, compositions containing them, and pharmaceutical compositions useful in the treatment and prevention of cerebrovascular disorders and useful as anesthetics or analgesics.

Подробнее
03-02-1998 дата публикации

PRODUCTION OF AROMATIC NITRILE

Номер: JP0010029967A
Автор: BREITSCHUH RICHARD
Принадлежит:

PROBLEM TO BE SOLVED: To obtain an aromatic nitrile by reacting an aldehyde with hydroxylamine sulfate under specific condition. SOLUTION: The objective nitrile of the formula II is produced by reacting an aldehyde of the formula I (X is CH or N; R1 and R2 are each H, Cl, Br, a 1-6C alkyl, a 1-6C alkoxy, a 1-6C alkyl-amino, CN, phenyl, phenoxy or dimethylamino or R1 and R2 together form a condensed benzene ring, etc.) with hydroxylamine sulfate and dehydrating the reaction product. The reaction is carried out in an organic solvent immiscible with water (e.g. toluene) in the presence of a t-amine base of the formula III (R3 and R4 are each H, methyl or ethyl), etc., at 100-160°C while distilling out water isolated by the reaction under a pressure of 0.02-1.5bar and removing the ammonium salt. The compound of the formula II is useful as a synthetic intermediate for a diketopyrrolopyrrole pigment. COPYRIGHT: (C)1998,JPO ...

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12-03-2003 дата публикации

Intermediate for preparing tricyclic compound and preparing method thereof

Номер: CN0001401621A
Принадлежит:

Подробнее
07-09-2006 дата публикации

Cyclopropane compounds and pharmaceutical use thereof

Номер: US20060199826A1
Принадлежит:

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X1 is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1-(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.; or a prodrug ...

Подробнее
02-11-2000 дата публикации

NOVEL TRICYCLIC COMPOUNDS, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME

Номер: EP0001047664A1
Принадлежит:

The invention concerns compounds of formula (I) in which: A forms a tricyclic system of formula A1, A2, A3 or A4; R1 represents a hydrogen atom, an alkyl, hydroxy, alkoxy or oxo group; (R2)m and (R3)m' are such as defined in the description; n represents an integer such that 0¿n¿3; p represents an integer such as defined in the description; B represents a group (a) or (b). The invention is useful for preparing medicines.

Подробнее
27-06-2000 дата публикации

Protein kinase C modulators N

Номер: US0006080784A1
Принадлежит: PROCYON PHARMACEUTICALS, INC.

Compositions with protein kinase C-modulatory, anti-inflammatory and other activities are disclosed.

Подробнее
12-02-1997 дата публикации

BENZOFURAN DERIVATIVES USEFUL AS INHIBITORS OF BONE RESORPTION

Номер: EP0000757682A1
Принадлежит:

This invention relates to a novel heterocyclic compound represented by formula (I), wherein X is O or S, Y is vinylene, or a group of formula: -NHCO-, -NHSO2-, -OCO-, -OCH2-, -NHCOCO-, -NHCOCH=CH-, -NHCOCH2-, -NHCONH- or (a) (wherein R6 is lower alkyl), Z is heterocyclic group which may have one or more suitable substituent(s), or aryl which may have one or more suitable substituent(s), 1 = 0, 1 and the other symbols are as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.

Подробнее
04-09-2002 дата публикации

Preparation of aromatic nitriles

Номер: CN0001090177C
Принадлежит:

Подробнее
06-04-1999 дата публикации

Protein kinase C modulators Q

Номер: US0005891870A1
Принадлежит: Procyon Pharmaceuticals, Inc.

Compositions with anti-inflammatory and other activitites are disclosed. The compositions are derived from phorboids of the diterpene- and benzolactam-classes.

Подробнее
16-07-2015 дата публикации

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR MODULATORS AND USES THEREOF IN REGULATING BLOOD GLUCOSE LEVELS

Номер: US20150197480A9
Автор: Klim King, Rong-Jie Chein
Принадлежит: Academia Sinica, Chi-Ming Liang

The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein:{'sub': 'A', 'Gis hydrogen, ═O, ═S, —OR″, —SR″, —NR″H, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, a thiocarbamate group, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms, wherein each instance of R″ is independently hydrogen, a cyclic or acyclic, saturated or unsaturated, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 16 carbon atoms;'}{'sub': A1', 'A2', 'A3', 'A4', 'A5', 'A6', 'A7', 'A8', 'A9', 'A10, 'R, R, R, R, R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbons;'}{'sub': A11', 'A12', 'A13', 'A15', 'A16', 'A17, 'R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms;'}{'sub': 'A14', 'Ris halogen, —NR″H, —SR″, —OR″, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, or a thiocarbamate group;'}{'sub': 'A20', 'Ris hydrogen, halogen, or a cyclic or acyclic, substituted ...

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17-06-1997 дата публикации

Mammalian DNA topoisomerase II inhibitor and method

Номер: US0005639793A1

A novel antiproliferative drug and methods are disclosed. The drug has the general structural formula: см. иллюстрацию в PDF-документе where R1=OR1 ', SR1 ', or N(R1 'R1 ")2, where R1 ' and R1 " are H or lower alkyl groups, and R2 is an acylamino, or aroylamino group. The compound is useful for inhibiting cell proliferation in drug-resistant tumor cells. Also disclosed is a method of chemical converting a colchicine derivative to form an active inhibitor of DNA topisomerase II.

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21-09-1999 дата публикации

Protein kinase C modulators O

Номер: US0005955501A1
Принадлежит: Procyon Pharmaceuticals, Inc.

Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.

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09-06-1998 дата публикации

Preparation of aromatic nitriles

Номер: US0005763638A1
Автор: Breitschuh; Richard
Принадлежит: Ciba Specialty Chemicals Corporation

A process for the preparation of nitriles of formula см. иллюстрацию в PDF-документе wherein X is CH or N, and R1 and R2 are each independently of the other hydrogen, chloro, bromo, C1 -C6 alkyl, C1 -C6 alkoxy, C1 -C6 alkylamino, CN, phenyl, phenoxy, dimethylamino, piperidyl, morpholinyl or pyrrolidyl, or R1 and R2 together form a fused benzene ring, by reacting an aldehyde of formula см. иллюстрацию в PDF-документе with hydroxylaminosulfate in the presence of a tertiary amine base of formula см. иллюстрацию в PDF-документе wherein R3 and R4 are each independently of the other hydrogen, methyl or ethyl, R5 is branched C3 -C5 alkyl or phenyl, and R6 and R7 are methyl or ethyl, in the temperature range from 100° to 160° C., while distilling the released water of reaction off concomittantly at a pressure in the range of 0.02 to 1.5 bar, with subsequent removal of the ammonium salts, and isolating the nitrile so obtained by customary methods.

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12-01-1999 дата публикации

Benzofuran derivatives useful as inhibitors of bone resorption

Номер: US0005858995A1
Принадлежит: Fujisawa Pharmaceutical Co., Ltd.

This invention relates to a novel heterocyclic compound represented by formula (I), wherein each symbol is as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.

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28-05-2008 дата публикации

Номер: JP0004091983B2
Автор:
Принадлежит:

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11-03-1997 дата публикации

NEW TRICYCLIC DERIVATIVES, THEIR PRODUCTION, OPTICALLY ACTIVE OR RACEMIC COLCHICINE AND THIOCOLCHICINE AND THEIR USE FOR PRODUCING ANALOGUES OR DERIVATIVES AND INTERMEDIATE

Номер: JP0009067326A
Принадлежит:

PROBLEM TO BE SOLVED: To obtain the subject new derivative represented by a specific formula, and useful for producing a kind of alkaloid, colchicine, and their related derivatives. SOLUTION: This compound of formula I {R1, R2 are each an alkyl, etc.; R3 is H, A-SO3- [A is an alkyl, a (substituted) naphthyl], etc.,}, e.g. 2,3,5,6- tetrahydro-8,9,10-trihydroxybenzo[e]azulen-4(1H)-one. This derivative is preferably obtained by reacting a compound of formula II (R1'-R3' are the same as R1 to R3, respectively) with a halogenating agent (preferably thionyl chloride), reacting the obtained corresponding acyl halide with a reacting agent of formula III (Ra, Rb are each an alkyl, or are combined with the nitrogen atom bound to the groups to form a five or six-membered heterocyclic ring) [preferably 1-(N-morpholinyl)cyclopentene], and further passing through a compound of formula IV. COPYRIGHT: (C)1997,JPO ...

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10-12-1991 дата публикации

Polycyclic amines useful as cerebrovascular agents

Номер: US0005071853A1
Принадлежит:

A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.

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29-08-2001 дата публикации

New tricyclic derivate and their producing process

Номер: CN0001310171A
Принадлежит:

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06-01-1998 дата публикации

Tricyclic compounds

Номер: US0005705704A1
Принадлежит: Roussel Uclaf

Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.

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02-11-1965 дата публикации

Номер: US0003215739A1
Автор:
Принадлежит:

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02-05-1972 дата публикации

POLYCYCLIC COMPOUNDS AND COPOLYMERS DERIVED THEREFROM

Номер: US0003660508A1
Автор:
Принадлежит: IMPERIAL CHEMICAL INDUSTRIES PLC

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19-10-1989 дата публикации

Номер: JP0001503063A
Автор:
Принадлежит:

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28-01-1998 дата публикации

Preparation of aromatic nitriles

Номер: CN0001171395A
Принадлежит:

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22-12-1997 дата публикации

Номер: JP0009512795A
Автор:
Принадлежит:

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23-04-2015 дата публикации

COMPOSITIONS AND METHODS FOR THE TREATMENT OF FIBROMYALGIA PAIN

Номер: US20150111966A1
Автор: Kandula Mahesh
Принадлежит:

The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of fibromyalgia pain may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of injury, post-operative pain, osteoarthritis, rheumatoid arthritis, multiple sclerosis, spinal cord injury, migraine, HIV related neuropathic pain, post herpetic neuralgia, diabetic neuropathy, bipolar depression, stress, cancer pain, and lower back pain. 2. A pharmaceutical composition comprising a compound of and a pharmaceutically acceptable carrier.3. The pharmaceutical composition of claim 2 , wherein said pharmaceutical composition is formulated to treat the underlying etiology with an effective amount administering the patient in need by oral administration claim 2 , delayed release or sustained release claim 2 , transmucosal claim 2 , syrup claim 2 , topical claim 2 , parenteral administration claim 2 , injection claim 2 , subdermal claim 2 , oral solution claim 2 , rectal administration claim 2 , buccal administration or transdermal administration.4. A method of treating fibromyalgia pain and pain as the underlying etiology claim 3 , the method comprising administering to a patient in need thereof an effective amount of .5. The method of claim 4 , wherein the fibromyalgia pain and pain as the underlying etiology is selected from injury claim 4 , post-operative pain claim 4 , osteoarthritis claim 4 , rheumatoid arthritis claim 4 , multiple sclerosis claim 4 , spinal cord injury claim 4 , migraine claim 4 , depression claim 4 , HIV related neuropathic pain claim 4 , post herpetic neuralgia claim 4 , diabetic neuropathy claim 4 , bipolar depression claim 4 , stress ...

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27-11-2014 дата публикации

GLUCAGON-LIKE PEPTIDE 1 (GLP-1) RECEPTOR MODULATORS AND USES THEREOF IN REGULATING BLOOD GLUCOSE LEVELS

Номер: US20140350100A1
Автор: Chein Rong-Jie, KING Klim
Принадлежит:

The present disclosure provides novel glucagon-like peptide-1 (GLP-1) receptor modulators such as compounds of Formula (I) or (II), and pharmaceutically acceptable salts thereof. The present disclosure also provides pharmaceutical compositions, kits, and uses that involve the GLP-1 receptor modulators for regulating blood glucose levels and/or treating diabetes via, e.g., modulating the endogenous signaling pathways mediated by the GLP-1 receptor. 2. The compound or pharmaceutically acceptable salt of claim 1 , wherein:{'sub': 'A', 'Gis hydrogen, ═O, ═S, —OR″, —SR″, —NR″H, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, a thiocarbamate group, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms, wherein each instance of R″ is independently hydrogen, a cyclic or acyclic, saturated or unsaturated, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 16 carbon atoms;'}{'sub': A1', 'A2', 'A3', 'A4', 'A5', 'A6', 'A7', 'A8', 'A9', 'A10, 'R, R, R, R, R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbons;'}{'sub': A11', 'A12', 'A13', 'A15', 'A16', 'A17, 'R, R, R, R, R, and Rare each independently hydrogen, halogen, or a cyclic or acyclic, substituted or unsubstituted, branched or unbranched, (hetero)aliphatic group having 1 to 6 carbon atoms;'}{'sub': 'A14', 'Ris halogen, —NR″H, —SR″, —OR″, alkenyl, alkynyl, an amide group, an ester group, an aldehyde group, a nitrile group, an imino group, a ketone group, a thione group, an isonitrile group, an isothiocyanide group, a carbamate group, or a thiocarbamate group;'}{'sub': 'A20', 'Ris hydrogen, halogen, or a cyclic or acyclic, substituted ...

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05-09-2017 дата публикации

Spirally configured cis-stilbene/fluorene hybrid materials for organic light-emitting diode

Номер: US09755154B2
Принадлежит: Nichem Fine Technology Co Ltd

The present invention provides a series of spirally configured cis-stilbene/fluorene hybrid materials, which are spirally-configured cis-stilbene/fluorene derivatives having glass transition temperatures ranged from 105° C. to 130° C., decomposition temperatures ranged from 385° C. to 415° C., reversible electron transport property, and balanced charges motilities. Moreover, a variety of experimental data have proved that the yellow fluorescent, the green phosphorescent, the yellow phosphorescent, and the red phosphorescent OLEDs using this spirally configured cis-stilbene/fluorene derivatives as the electron transport layers having hole blocking functions can indeed show excellent EQE, current efficiency, power efficiency, maximum luminance, and device lifetime performances much better than the conventional or commercial yellow fluorescent, green phosphorescent, yellow phosphorescent, and red phosphorescent OLEDs.

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01-11-2016 дата публикации

Ingenane-type diterpene compound, and pharmaceutical composition for treating or preventing viral infectious diseases containing same

Номер: US09481630B2

The present invention relates to an injenane-type diterpene compound derived from Euphorbia kansui Liou, and a pharmaceutical composition for treating or preventing viral infectious diseases, a health functional food for preventing or ameliorating viral infectious diseases and a composition for enhancing the production of interferon-gamma, which comprise the injenane-type diterpene compound. Furthermore, the present invention relates to a method for preventing or treating viral infectious diseases including administering the composition to a subject having a viral infectious disease occurrence or a risk thereof with a therapeutically effective dose.

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