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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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Применить Всего найдено 15. Отображено 14.
14-11-2013 дата публикации

INHIBITOR COMPOUNDS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1

Номер: US20130303522A1
Автор: ANTOLIN HERNANDEZ Albert, CATENA RUIZ Juan Lorenzo, MONLLEO MAS Esther, REY PUIGGROS Oscar, SERRA COMAS Carme
Принадлежит: LABORATORIOS SALVAT, S.A.

The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration. 2. The method according to claim 1 , wherein in the compound Y is CO or SO.3. The method according to claim 1 , wherein in the compound W1 and W2 is each independently selected from the group consisting of a bond claim 1 , S and NR1.4. The method according to claim 3 , wherein in the compound R1 is H5. The method according to claim 1 , wherein in the compound V is —CO-T claim 1 , —CS-T or —SO-T.7. The method according to claim 1 , wherein in the compound T is NR2R3 claim 1 , R2 claim 1 , OR2 or SR2.8. The method according to claim 1 , wherein in the compound R2 and R3 is each independently selected from the group consisting of H claim 1 , COR4 claim 1 , SOR4 claim 1 , Calkyl claim 1 , phenyl claim 1 , naphthyl claim 1 , benzyl claim 1 , phenethyl claim 1 , Calkenyl claim 1 , Ccycloalkyl claim 1 , and heterocycle claim 1 , particularly claim 1 , 2-furanyl claim 1 , 2-thiophenyl claim 1 , 2-(1-methylindole) claim 1 , quinoline claim 1 , isoquinoline and 2-benzofuranyl.9. The method according to claim 8 , wherein in the compound R2 and R3 is each independently selected from the groups consisting of Calkyl and Calkenyl.10. The method according to claim 9 , wherein in the compound R2 or R3 are optionally substituted with one or several substituents independently selected from the groups consisting of F claim 9 , OR4 claim 9 , NR4R5 claim 9 , COOR4 claim 9 , CONR4R5 claim 9 , phenyl claim 9 , Ccycloalkyl claim 9 , hexenyl claim 9 , ...

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Номер записи: 1
08-05-2014 дата публикации

Process for obtaining rivaroxaban and intermediate thereof

Номер: US20140128601A1
Автор: Amadeo Llebaria Soldevilla, Carme Serra Comas, Francisco Marquillas Olondriz, Xavier BERZOSA RODRÍGUEZ
Принадлежит: Interquim SA

This invention relates to a procedure for obtaining a thiophene-2-carboxamide compound, specifically rivaroxaban, which comprises the (i) fragmentation of the N═C bond of a compound of formula 23 where R1 is selected among hydrogen, halogen, and (C1-C6)alkyl; and (ii) acylation of the resulting intermediate with 5-chloro-tiofen-2-carbonyl chloride in a solvent medium, in the presence of a base. The invention also relates to the compounds of formula 23 and their use in the obtention of rivaroxaban.

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Номер записи: 2
08-06-2017 дата публикации

ADDITION SALTS OF (S)-2-(1-(6-AMINO-5-CYANOPYRIMIDIN-4-YLAMINO)ETHYL)-4-OXO-3-PHENYL-3,4-DIHYDROPYRROLO[1,2-F][1,2,4]TRIAZINE-5-CARBONITRILE

Номер: US20170158699A1
Автор: Carrera Carrera Francesc, Pérez Garcia Juan Bautista, SANCHEZ IZQUIEROD Francisco, SERRA COMA Maria Carme, VIDAL JUAN Bernat
Принадлежит:

The present invention is directed to novel pharmaceutically acceptable, addition salts of (S)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3,4-dihydropyrrolo[1,2-f][1,2,4]triazine-5-carbonitrile with sulfonic acid derivatives, in particular with methanesulfonic acid, naphthalene-2-sulfonic acid and para-toluenesulfonic acid, and pharmaceutically acceptable solvates thereof, and their use as Phosphoinositide 3-Kinase (PI3K) inhibitors. 1. A pharmaceutically acceptable crystalline addition salt of (S)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3 ,4-dihydropyrrolo[1 ,2-f][1 ,2 ,4]triazine-5-carbonitrile with sulfonic acid derivatives chosen from methanesulfonic acid , naphthalene-2-sulfonic acid and para-toluenesulfonic acid , or a pharmaceutically acceptable solvate thereof.2. The salt according to claim 1 , chosen from (S)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3 claim 1 ,4-dihydropyrrolo[1 claim 1 ,2-f][1 claim 1 ,2 claim 1 ,4]triazine-5-carbonitrile methanesulfonate claim 1 , or a pharmaceutically acceptable solvate thereof.3. The salt according to claim 1 , chosen from (S)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3 claim 1 ,4-dihydropyrrolo[1 claim 1 ,2-f][1 claim 1 ,2 claim 1 ,4]triazine-5-carbonitrile naphthalene-2-sulfonate claim 1 , or a pharmaceutically acceptable solvate thereof.4. The salt according to claim 1 , chosen from (S)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3 claim 1 ,4-dihydropyrrolo[1 claim 1 ,2-f][1 claim 1 ,2 claim 1 ,4]triazine-5-carbonitrile para-toluenesulfonate claim 1 , or a pharmaceutically acceptable solvate thereof.5. A pharmaceutical composition comprising a therapeutically effective amount of the salt according to and a pharmaceutically acceptable carrier.6. The pharmaceutical composition according to further comprising a therapeutically effective amount of at least one additional therapeutic agent.7. The pharmaceutical ...

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Номер записи: 3
10-02-2017 дата публикации

Addition salts of (s) -2- (1- (6-amino-5-cyanopyrimidin-4-ylamino) ethyl) -4-oxo-3-phenyl-3,4-dihydropyrrolo [1,2-f] [ 1,2,4] triazine-5-carbonitrile.

Номер: CL2016002970A1
Автор: Carrera Francesc Carrera, Coma Maria Carme Serra, Garcia Juan Bautista Perez, Izquierdo Francisco Sanchez, Juan Bernat Vidal
Принадлежит: Almirall SA

<p>UNA SAL DE ADICION CRISTALINA DE (S)-2-(1-(6-AMINO-5-CIANOPIRIMIDIN-4-ILAMINO)ETIL)-4-OXO-3-FENIL-3,4-DIHIDROPIRROLO[1,2-F][1,2,4]TRIAZINA-5-CARBONITRILO; COMPOSICION FARMACEUTICA QUE LA COMPRENDE; Y SU USO PARA EL TRATAMIENTO DE UNA AFECCION O ENFERMEDAD SUSCEPTIBLE DE MEJORAR POR INHIBICION DE FOSFOINOSITIDO 3-QUINASA.</p> <p> A CRYSTALLINE ADDITION SALT OF (S) -2- (1- (6-AMINO-5-CYANOPIRIMIDIN-4-ILAMINO) ETIL) -4-OXO-3-PHENYL-3,4-DIHYDROPIRROLO [1, 2-F] [1,2,4] TRIAZINE-5-CARBONITRILE; PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS IT; AND ITS USE FOR THE TREATMENT OF AN AFFECTION OR SUSCEPTIBLE DISEASE TO IMPROVE BY INHIBITION OF 3-QUINASE PHOSFOINOSITIDE. </p>

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Номер записи: 4
03-12-2015 дата публикации

Addition salts of (s)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3,4-dihydropyrrolo[1,2-f][1,2,4]triazine-5-carbonitrile

Номер: CA2944611A1
Автор: Bernat Vidal Juan, Francesc Carrera Carrera, Francisco Sanchez Izquierdo, Juan Bautista Perez Garcia, Maria Carme SERRA COMA
Принадлежит: Almirall SA

The present invention is directed to novel pharmaceutically acceptable, addition salts of (S)-2-(1-(6-amino-5-cyanopyrimidin-4-ylamino)ethyl)-4-oxo-3-phenyl-3,4- dihydropyrrolo[1,2-f][1,2,4]triazine-5-carbonitrile with sulfonic acid derivatives, in particular with methanesulfonic acid, naphthalene-2-sulfonic acid and para-toluenesulfonic acid, and pharmaceutically acceptable solvates thereof, and their use as Phosphoinositide 3-Kinase (PI3K) inhibitors.

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Номер записи: 5
09-12-2010 дата публикации

Inhibitor compounds of 11-beta-hydroxysteroid dehydrogenase type 1

Номер: CA2764214A1
Автор: Albert Antolin Hernandez, Carme Serra Comas, Ester MONLLEÓ MAS, Juan Lorenzo Catena Ruiz, Oscar Rey Puiggros
Принадлежит: Laboratorios Salvat SA

The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type 1 (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.

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Номер записи: 6
29-11-2012 дата публикации

Process for obtaining rivaroxaban and intermediate thereof

Номер: WO2012159992A1
Автор: Amadeo Llebaria Soldevilla, Carme Serra Comas, Francisco Marquillas Olondriz, Xavier BERZOSA RODRÍGUEZ
Принадлежит: INTERQUIM, S.A.

This invention relates to a procedure for obtaining a thiophene-2-carboxamide compound, specifically rivaroxaban, which comprises the (i) fragmentation of the N=C bond of a compound of formula 23 where R1 is selected among hydrogen, halogen, and (C1-C6)alkyl; and (ii) acylation of the resulting intermediate with 5-chloro-tiofen-2-carbonyl chloride in a solvent medium, in the presence of a base. The invention also relates to the compounds of formula 23 and their use in the obtention of rivaroxaban.

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Номер записи: 7
01-02-2024 дата публикации

Ip5 substituted compounds

Номер: WO2024023360A1
Автор: Amadeu Llebaria Soldevila, Carme Serra Comas, Carolina Salcedo Roca, Joan Perello Bestard, Juan Lorenzo Catena Ruiz, María Del Mar PÉREZ FERRER, Miquel David Ferrer Reynes, Mohamad Firas BASSISSI
Принадлежит: SANIFIT THERAPEUTICS, S.A.

The present invention provides IP5 substituted compounds of general formula I, their methods of synthesis and their uses. The IP5 substituted compounds of the invention are characterized for having -O(alkyl)nX, and -O(alkyl)yCy(alkyl)y'-Z chains in positions R1, R2, R4, and R5. Also provided are methods, pharmaceutical compositions and formulations, methods of use, articles of manufacture, and kits for the treatment of diseases and conditions such as pathological crystallization-related diseases and conditions.

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Номер записи: 8
11-02-2013 дата публикации

Procedimiento de obtención de una tiofen-2-carboxamida.

Номер: ES2395304A1
Автор: Amadeo Llebaria Soldevilla, Carme Serra Comas, Francisco Marquillas Olondriz, Xavier BERZOSA RODRÍGUEZ
Принадлежит: Interquim SA

Procedimiento de obtención de una tiofen-2-carboxamida.La invención se refiere a un procedimiento de obtención de una tiofen-2-carboxamida, específicamente el rivaroxaban, que comprende la hidrólisis de una 4-(4-{5-[(benciliden-amino)-metil]-2-oxo-oxazolidin-3-il}-fenil)-morfolin-3-ona y subsiguiente acilación de la 4-[4-(5-aminometil-2-oxo-oxazolidin-3-il)-fenil]-morfolin-3-ona resultante con cloruro de 5-cloro-tiofen-2-carbonilo. La invención contempla también las 4-(4-{5-[(benciliden-amino)-metil]-2-oxo-oxazolidin-3-il}-fenil)-morfolin-3-onas y su uso en la obtención del rivaroxaban.

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Номер записи: 9
26-07-2023 дата публикации

Compuestos de derivados sustituidos en 4,6 de ip4.

Номер: MX2023008250A
Автор: Bestard Joan Perello, Castro Joaquín Ortega, Comas Carme Serra, Ferrer María Del Mar Pérez, Mohamad Firas BASSISSI, Reynés Miquel David Ferrer, Roca Carolina Salcedo, Ruiz Juan Lorenzo Catena, Soldevila Amadeu Llebaria
Принадлежит: Sanifit Therapeutics S A

La presente invención proporciona derivados sustituidos en 4,6 de IP4, sus métodos de síntesis y sus usos. En algunos aspectos, el derivado 4,6-IP4 es un compuesto de fórmula I, en donde R1, R3, R7 y R11 son OPO32-, y R5 y R9 se seleccionan del grupo que consiste en -O(Alquil)nX, -O(Alquil)yCy(Alquil2)y-Z, -O(Alquil)yA(Alquil)y-Z', y sus análogos de tiofosfato. También se proporcionan métodos, composiciones farmacéuticas y formulaciones, métodos de uso, artículos de fabricación y kits para el tratamiento de enfermedades y afecciones tales como enfermedades y afecciones relacionadas con la cristalización patológica.

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Номер записи: 10
04-04-2024 дата публикации

Ip4-4,6 substituted derivative compounds

Номер: US20240109924A1
Автор: Amadeu Llebaria Soldevila, Carme Serra Comas, Carolina Salcedo Roca, Joan Perello Bestard, Joaquín ORTEGA CASTRO, Juan Lorenzo Catena Ruiz, María Del Mar PÉREZ FERRER, Miquel David Ferrer Reynes, Mohamad Firas BASSISSI
Принадлежит: Sanifit Therapeutics SA

The present invention provides IP4-4,6 substituted derivatives, their methods of synthesis and their uses. In some aspects, the IP4-4,6 derivative is a compound of formula I wherein R1, R3, R7, and R11 are OPO32−, and R5 and R9 are selected from the group consisting of —O(Alkyl)nX, —O(Alkyl)yCy(Alkyl2)y-Z, —O(Alkyl)yA(Alkyl)y-Z′, and their thiophosphate analogs. Also provided are methods, pharmaceutical compositions and formulations, methods of use, articles of manufacture, and kits for the treatment of diseases and conditions such as pathological crystallization-related diseases and conditions.

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Номер записи: 11
10-10-2023 дата публикации

Compostos derivados substituídos com ip4-4,6

Номер: BR112023014549A2
Автор: Bestard Joan Perello, Castro Joaquín Ortega, Comas Carme Serra, Ferrer María Del Mar Pérez, Mohamad Firas BASSISSI, Reynés Miquel David Ferrer, Roca Carolina Salcedo, Ruiz Juan Lorenzo Catena, Soldevila Amadeu Llebaria
Принадлежит: Sanifit Therapeutics S A

compostos derivados substituídos com ip4-4,6. provê derivados substituídos com ip4-4,6, seus métodos de síntese e seus usos. em alguns aspectos, o derivado de ip4-4,6 é um composto de fórmula i em que r1, r3, r7, e r11 são opo32-, e r5 e r9 são selecionados do grupo que consiste em -o(alquil)nx, -o(alquil)ycy(alquil2)y-z, -o(alquil)ya(alquil)y-z', e seus análogos de tiofosfato. são também são providos métodos, composições farmacêuticas e formulações, métodos de uso, artigos de fabricação, e kits para o tratamento de doenças e condições tais como doenças e condições relacionadas a cristalização patológica.

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Номер записи: 12
06-12-2023 дата публикации

Ip4-4,6 substituted derivative compounds

Номер: EP4284809A1
Автор: Amadeu Llebaria Soldevila, Carme Serra Comas, Carolina Salcedo Roca, Joan Perello Bestard, Joaquín ORTEGA CASTRO, Juan Lorenzo Catena Ruiz, María Del Mar PÉREZ FERRER, Miquel David Ferrer Reynes, Mohamad Firas BASSISSI
Принадлежит: Sanifit Therapeutics SA

The present invention provides IP4-4,6 substituted derivatives, their methods of synthesis and their uses. In some aspects, the IP4-4,6 derivative is a compound of formula I wherein R1, R3, R7, and R11 are OPO3 2-, and R5 and R9 are selected from the group consisting of -O(Alkyl)nX, -O(Alkyl)yCy(Alkyl2)y-Z, -O(Alkyl)yA(Alkyl)y-Z', and their thiophosphate analogs. Also provided are methods, pharmaceutical compositions and formulations, methods of use, articles of manufacture, and kits for the treatment of diseases and conditions such as pathological crystallization-related diseases and conditions.

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Номер записи: 13
31-05-2019 дата публикации

Análogos no glicosídicos de alfa-galactosilceramida como activadores de células nkt

Номер: WO2019102054A1
Автор: Amadeu Llebaria Soldevila, Anna Alcaide Lopez, Carme Serra Comas, Roser BORRAS TUDURÍ
Принадлежит: CONSEJO SUPERIOR DE INVESTIGACIONES CIENTIFICAS (CSIC)

Análogos no glicosídicos de alfa-galactosilceramida de fórmula (I) donde A, Z, Ra, Rb Rc tienen el significado indicado en la descripción como activadores de células NKT. (I)

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Номер записи: 14