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 37. Отображено 36.
18-02-2016 дата публикации

BICYCLIC SULFONAMIDE COMPOUNDS AS SODIUM CHANNEL INHIBITORS

Номер: US20160046626A1
Принадлежит:

The present invention provides compounds of Formula I, 132-. (canceled)34. The compound in accordance with claim 33 , or a pharmaceutically acceptable salt thereof claim 33 , wherein each Ris independently H claim 33 , F or Cl.35. The compound in accordance with claim 33 , or a pharmaceutically acceptable salt thereof claim 33 , wherein Ris a 6 membered aryl or heteroaryl group claim 33 , where the heteroaryl group can have from 1 to 3 heteroatoms independently selected from O claim 33 , N or S claim 33 , and the aryl or heteroaryl group can be unsubstituted or substituted with from 1 to 4 substituents independently selected from halo claim 33 , —Calkyl claim 33 , —OCalkyl claim 33 , hydroxyCalkyl claim 33 , —CF claim 33 , —CHF claim 33 , —CHF claim 33 , —OCF claim 33 , —OCHF claim 33 , —OCHF claim 33 , CN claim 33 , —C(═O)NRR claim 33 , —C(═O)OR claim 33 , —OA or A; and{'sub': 1-6', '1-6', '1-6', '3', '2', '2', '3', '2', '2, 'sup': b', 'b, 'A is a 5 to 6 membered aryl or heteroaryl group, wherein the heteroaryl group can have from 1 to 3 heteroatoms independently selected from O, N or S, and the aryl or heteroaryl group can be unsubstituted or substituted with from 1 to 4 substituents independently selected from halo, —Calkyl, —OCalkyl, hydroxyCalkyl —CF, —CHF, —CHF, —OCF, —OCHF, —OCHF, —CN, or —C(═O)NRR.'}36. The compound in accordance with claim 33 , or a pharmaceutically acceptable salt thereof claim 33 , wherein Ris a phenyl ring or pyridyl ring claim 33 , wherein the ring can be unsubstituted or substituted with from 1 to 4 substituents independently selected from halo claim 33 , —Calkyl claim 33 , —OCalkyl claim 33 , hydroxyCalkyl claim 33 , —CF claim 33 , —CHF claim 33 , —CHF claim 33 , —OCF claim 33 , —OCHF claim 33 , —OCHF claim 33 , CN claim 33 , —C(═O)NRR claim 33 , —C(═O)OR claim 33 , —OA or A.37. The compound in accordance with claim 33 , or a pharmaceutically acceptable salt thereof claim 33 , wherein A is a ring selected from cyclopropyl claim 33 , ...

Подробнее
06-06-2019 дата публикации

Pyridine sulfonamides

Номер: US20190167682A1
Принадлежит: AMGEN INC

The present invention provides compounds of Formula (I), as defined in the specification, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders, cough, or itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

Подробнее
06-08-2020 дата публикации

COUPON AND CONTEST BUSINESS METHODS

Номер: US20200250695A1
Автор: BUTLER John R.
Принадлежит:

A coupon and/or contest business method is described. Users can be given the opportunity to obtain and use a coupon that provides benefits such as discounts at a multitude of different stores. The users can also be entered into one or more contests. For instance, in one embodiment, the user is automatically entered into a first contest via use of the coupon, and can enter a second contest for a nominal fee, such as a fee of $0.25 /month. Periodic prizes, such as monthly giveaways, can be included. 1. A business method for providing discounts , comprising providing a user with a digital coupon usable at a plurality of stores to provide the user with a discount , further comprising entering the user into a contest after the user downloads or uses the digital coupon.2. The business method of claim 1 , wherein the digital coupon is provided via text message.3. The business method of claim 1 , wherein the digital coupon is provided via download of an app.4. The business method of claim 3 , wherein the app permits a user to become a character in a movie or show using facial recognition technology.5. The business method of claim 1 , further comprising asking the user one or more questions.6. The business method of claim 5 , wherein the user is provided a benefit if they answer one of said questions correctly.7. The business method of claim 1 , wherein the digital coupon provides at least a 10% discount.8. The business method of claim 1 , where the digital coupon provides at least a 25% discount online.9. A business method claim 1 , comprising:providing a website;contacting at least one user to provide the address of said website; providing said user with a coupon for use at a plurality of stores; and', 'entering said user into a first contest with a first prize., 'upon said user visiting said website and entering information10. The business method of claim 9 , wherein said contacting comprises contacting said user via ringless voicemail.11. The business method of claim 10 ...

Подробнее
18-12-2014 дата публикации

BICYCLIC SULFONAMIDE COMPOUNDS AS SODIUM CHANNEL INHIBITORS

Номер: US20140371201A1
Принадлежит:

The present invention provides compounds of Formula I, 2. A compound in accordance with claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each of Aand Ais claim 1 , independently claim 1 , CR.3. A compound in accordance with claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein each Ris independently H or F.4. A compound in accordance with claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein{'sup': 1', 'b', 'b', 'b', '1, 'sub': 1-6', '1-6', '1-6', '3', '2', '2', '3', '2', '2, 'Ris a ring selected from phenyl, pyridinyl or pyrimidinyl, wherein the ring is substituted with from 1 to 4 substituents independently selected from halo, —Calkyl, —OCalkyl, hydroxyCalkyl, —CF, —CHF, —CHF, —OCF, —OCHF, —OCHF, CN, —C(═O)NRR, —C(═O)OR, —OA or A, provided at least one substituent on Ris A or —OA; and'}{'sub': 1-6', '1-6', '1-6', '3', '2', '2', '3', '2', '2, 'sup': b', 'b, 'A is a 5 to 6 membered aryl or heteroaryl group, or a 4 to 6 membered N-linked heterocycloalkyl group, or a 3 to 6 membered cycloalkyl group, where the heteroaryl can have from 1 to 3 heteroatoms independently selected from O, N or S, the N-linked heterocycloalkyl can have 1 additional heteroatom independently selected from O, N or S, and the aryl, heteroaryl, heterocyclic and cycloalkyl group can be unsubstituted or substituted with from 1 to 4 substituents independently selected from halo, —Calkyl, —OCalkyl, hydroxyCalkyl —CF, —CHF, —CHF, —OCF, —OCHF, —OCHF, —CN, or —C(═O)NRR.'}5. A compound in accordance with claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a phenyl ring or pyridyl ring claim 1 , wherein the ring is substituted with from 1 to 4 substituents independently selected from halo claim 1 , —Calkyl claim 1 , —OCalkyl claim 1 , hydroxyCalkyl claim 1 , —CF claim 1 , —CHF claim 1 , —CHF claim 1 , —OCF claim 1 , —OCHF claim 1 , —OCHF claim 1 , CN claim 1 , —C(═O)NRR—C(═O)OR claim 1 , —OA or A claim 1 , provided ...

Подробнее
02-06-2022 дата публикации

Novel prmt5 inhibitors

Номер: CA3202141A1
Принадлежит: AMGEN INC

Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formule (I).

Подробнее
19-08-2021 дата публикации

Novel prmt5 inhibitors

Номер: WO2021163344A1
Принадлежит: Amgen Inc.

Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure: (I)

Подробнее
28-03-2024 дата публикации

Tricyclic carboxamide derivatives as prmt5 inhibitors

Номер: US20240101570A1
Принадлежит: AMGEN INC

Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formula (I).

Подробнее
24-08-2023 дата публикации

Inhibidores de prmt5 novedosos

Номер: CR20230286A
Принадлежит: AMGEN INC

Se describen en el presente documento compuestos de Fórmula I y sales farmacéuticamente aceptables de los mismos, así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, tales como cáncer, trastornos metabólicos y sanguíneos. Los compuestos de Fórmula I tienen la siguiente estructura:

Подробнее
01-12-2023 дата публикации

Inhibidores de prmt5 novedosos

Номер: CL2023001461A1
Принадлежит: AMGEN INC

Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formule (I).

Подробнее
08-09-2023 дата публикации

Derivados de carboxamida tricíclica como inhibidores de prmt5

Номер: CO2023007504A2
Принадлежит: AMGEN INC

Se describen en el presente documento compuestos de Fórmula I y sales farmacéuticamente aceptables de los mismos, así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, tales como cáncer, trastornos metabólicos y sanguíneos. Los compuestos de Fórmula I tienen la siguiente estructura:

Подробнее
17-11-2023 дата публикации

Inhibidores de prmt5

Номер: CL2023001738A1
Принадлежит: AMGEN INC

Se describen en el presente documento inhibidores novedosos de PRMT5 de Fórmula I y sales farmacéuticamente aceptables de los mismos, así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, metabólicos y sanguíneos. Los compuestos de Fórmula I tienen la siguiente estructura:

Подробнее
01-09-2023 дата публикации

Inhibidores de prmt5

Номер: CR20230310A
Принадлежит: AMGEN INC

Se describen en el presente documento inhibidores novedosos de PRMT5 de Fórmula I y sales farmacéuticamente aceptables de los mismos, así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, metabólicos y sanguíneos. Los compuestos de Fórmula I tienen la siguiente estructura:

Подробнее
19-12-2023 дата публикации

PRMT5 inhibitors

Номер: US11845760B2
Принадлежит: AMGEN INC

Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

Подробнее
18-10-2022 дата публикации

Inhibidores de prmt5 novedosos.

Номер: MX2022010011A
Принадлежит: AMGEN INC

Se describen en el presente documento compuestos de fórmula I y sales farmacéuticamente aceptables de los mismos, estereoisómeros, tautómeros así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, metabólicos y sanguíneos. Los compuestos de fórmula I tienen la siguiente estructura: (I) (Ver Fórmula I).

Подробнее
03-07-2023 дата публикации

Inhibidores de prmt5.

Номер: MX2023007192A
Принадлежит: AMGEN INC

Se describen en el presente documento inhibidores novedosos de PRMT5 de Fórmula I y sales farmacéuticamente aceptables de los mismos, así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, metabólicos y sanguíneos. Los compuestos de Fórmula I tienen la siguiente estructura: (ver Fórmula).

Подробнее
04-10-2023 дата публикации

Tricyclic carboxamide derivatives as prmt5 inhibitors

Номер: EP4251624A1
Принадлежит: AMGEN INC

Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formule (I).

Подробнее
25-08-2022 дата публикации

Novel PRMT5 inhibitors

Номер: AU2021219730A1
Принадлежит: AMGEN INC

Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure: (I)

Подробнее
21-12-2022 дата публикации

Novel prmt5 inhibitors

Номер: EP4103558A1
Принадлежит: AMGEN INC

Described herein are compounds of Formula I and pharmaceutically acceptable salt thereof, stereoisomers, tautomers as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure: (I)

Подробнее
24-08-2023 дата публикации

Derivados triciclicos de carboxamida como inhibidores de la prmt5

Номер: PE20231312A1
Принадлежит: AMGEN INC

Referido a un compuesto de Formula I, un tautomero del mismo, un esteroisomero del mismo o una sal farmaceuticamente aceptable de cualquiera de los anteriores, en donde: R es un triciclo independientemente seleccionado de las formulas IA y IB, en donde la linea punteada es un enlace sencillo o doble; X1, X2, X6 y X7 son en cada caso N o C, en donde tanto X1 como X2 no pueden ser N al mismo tiempo, y en donde si X1 es C, puede estar opcionalmente sustituido con halo; X3, X4 y X5 se seleccionan en cada caso independientemente de un C, O, N y S opcionalmente sustituidos; R3 en cada caso se selecciona independientemente de H o alquilo C1-3; Ar1 es un arilo o heteroarilo opcionalmente sustituido de seis miembros; R1 en cada caso se selecciona independientemente de H, halo, alquilo C1-3 opcionalmente sustituido; entre otros; R2 en cada caso se selecciona independientemente de un alquilo C1-8 opcionalmente sustituido, ciclo o heterociclo de 5 o 6 miembros opcionalmente sustituido con hidroxi, amino, entre otros. Un compuesto seleccionado es 4-amino-N-(ciclopropilmetil)-N-((5-(trifluorometil)-2-piridinil)metil)-1,3-dihidrofuro[3,4-c]quinolin-8-carboxamida. Estos compuestos son derivados triciclicos de carboxamida, y son inhibidores de la PRMT5. Tambien se refiere a metodos de sintesis de dichos compuestos, productos intermedios, composiciones farmaceuticas que comprenden dichos compuestos, y su uso en el tratamiento de trastornos proliferativos, tales como cancer, trastornos metabolicos y sanguineos.

Подробнее
06-06-2023 дата публикации

Inhibidores de prmt5 novedosos.

Номер: MX2023006145A
Принадлежит: AMGEN INC

Se describen en el presente documento compuestos de Fórmula I y sales farmacéuticamente aceptables de los mismos, así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, tales como cáncer, trastornos metabólicos y sanguíneos. Los compuestos de Fórmula I tienen la siguiente estructura: (ver Fórmula).

Подробнее
18-04-2024 дата публикации

Tricyclic-amido-bicyclic prmt5 inhibitors

Номер: US20240124442A1
Принадлежит: AMGEN INC

Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

Подробнее
11-07-2024 дата публикации

Tricyclic-amido-bicyclic prmt5 inhibitors

Номер: AU2022217791A9
Принадлежит: AMGEN INC

Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

Подробнее
13-12-2023 дата публикации

Tricyclic-amido-bicyclic prmt5 inhibitors

Номер: EP4288435A1
Принадлежит: AMGEN INC

Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

Подробнее
11-04-2024 дата публикации

Heterocyclic inhibitors of kras g12c mutant proteins and uses thereof

Номер: WO2024076674A1
Принадлежит: Amgen Inc.

The present disclosure provides compounds having activity as inhibitors of the G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic, and colorectal cancer. In particular, the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein the substituents are as described.

Подробнее
11-09-2023 дата публикации

Inhibidores tricíclicos-amido-bicíclicos de prmt5.

Номер: MX2023009222A
Принадлежит: AMGEN INC

Se describen en el presente documento inhibidores novedosos de PRMT5 de Fórmula I y sales farmacéuticamente aceptables de los mismos, así como las composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, metabólicos y sanguíneos. Los compuestos de fórmula I tienen la siguiente estructura (ver fórmula).

Подробнее
11-04-2024 дата публикации

Heterocyclic inhibitors of kras g12c mutant proteins and uses thereof

Номер: WO2024076672A1
Принадлежит: Amgen Inc.

The present disclosure provides compounds having activity as inhibitors of the G12C mutant KRAS protein, pharmaceutical compositions comprising the compounds, and methods of treating certain disorders, such as cancer, including but not limited to lung, pancreatic, and colorectal cancer. In particular, the disclosure provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein the substituents are as described.

Подробнее
21-03-2024 дата публикации

Novel prmt5 inhibitors

Номер: US20240092794A1
Принадлежит: AMGEN INC

Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well as the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

Подробнее
22-08-2023 дата публикации

Inhibidores de prmt5

Номер: PE20231295A1
Принадлежит: AMGEN INC

Un compuesto de Formula I, en donde R1 , R2 y el atomo de nitrogeno al que estan unidos forman un anillo de cinco, seis o siete miembros que puede estar saturado o parcialmente saturado, y comprende 0, 1 o 2 heteroatomos adicionales, iguales o diferentes seleccionados de O, N o S, en donde el atomo de S esta opcionalmente sustituido con uno o dos grupos oxo; en donde el anillo formado por R1 , R2 y el atomo de nitrogeno al que estan unidos puede estar sustituido con 0, 1, 2 o 3 R3 ; en donde R3 se selecciona en cada caso de alquilo C1-6 , halo, haloalquilo C1-6 , -O-alquilo C1-6 , -O-haloalquilo C1-6 , -C(O)-alquilo C1-6 , -C(O)-haloalquilo C1-6 , -C(O)O-alquilo C1-6 , -C(O)Ohaloalquilo C1-6 y ciclo de cinco o seis miembros que puede estar saturado, parcialmente saturado o ser aromatico, y comprende 0, 1 o 2 heteroatomos, iguales o diferentes, seleccionados de O, N y S, en donde el ciclo puede estar opcionalmente sustituido con uno o mas Ra , en donde Ra se selecciona en cada caso de halo, CN, alquilo C1-6 , haloalquilo C1-6 , pentafluorosulfanilo, -O-alquilo C1-3 y -O-haloalquilo C1-3; en donde R es un triciclo seleccionado de las formulas IA y IB; X1 , X2 , X6 , X7 y X8 se seleccionan en cada caso de N y C opcionalmente sustituidos, en donde los sustituyentes se seleccionan de alquilo C1-3; en donde tanto X1 como X2 no pueden ser N al mismo tiempo, y X6 y X7 , y X7 y X8 no pueden ser N al mismo tiempo; ademas en donde si X1 es C, puede estar opcionalmente sustituido con halo; X3 , X4 y X5 se seleccionan en cada caso de C, O, N y S opcionalmente sustituidos, en donde los sustituyentes se seleccionan de alquilo C1-3 y alquil C1-3 (OH), en donde el alquilo puede estar opcionalmente sustituido con halo. Son compuestos preferidos: (4-amino-1-metil-1H-pirazolo[4,3-c][1,7]naftiridin-8-il)((3S)-3-(4-(trifluorometil)fenil)-4- morfolinil)metanona; (4-amino-1,3-dihidrofuro[3,4-c][1,7]naftiridin-8-il)((3S,5R)-3-(6-(ciclopropiloxi)-3- piridazinil)-5-metil-4-morfolinil)metanona ...

Подробнее
22-03-2023 дата публикации

Inhibidores de prmt5 novedosos

Номер: AR124369A1
Принадлежит: AMGEN INC

Se describen en el presente documento compuestos de fórmula (1) y sales farmacéuticamente aceptables de los mismos, así como composiciones farmacéuticas de los mismos. Los compuestos de la presente invención son útiles para inhibir la actividad de PRMT5 y pueden tener uso en el tratamiento de trastornos proliferativos, metabólicos y sanguíneos. Los compuestos de fórmula (1) tienen la siguiente estructura. Reivindicación 1: Un compuesto de fórmula (1), un tautómero del mismo, un esteroisómero del mismo o una sal farmacéuticamente aceptable de cualquiera de los anteriores: en donde R¹, R² y el átomo de nitrógeno al que están unidos forman un anillo de cinco, seis o siete miembros que puede estar saturado o parcialmente saturado, y comprende 0, 1 ó 2 heteroátomos adicionales, iguales o diferentes, seleccionados de O, N o S, en donde el átomo de S está opcionalmente sustituido con uno o dos grupos oxo; en donde el anillo formado por R¹, R² y el átomo de nitrógeno al que están unidos puede estar sustituido con 0, 1, 2 o R³; en donde R³ se selecciona en cada caso de alquilo C₁₋₆, halo, haloalquilo C₁₋₆, -O-alquilo C₁₋₆, -O-haloalquilo C₁₋₆, -C(O)-alquilo C₁₋₆, -C(O)-haloalquilo C₁₋₆, -C(O)O-alquilo C₁₋₆, -C(O)O-haloalquilo C₁₋₆ y ciclo de cinco o seis miembros que puede estar saturado, parcialmente saturado o ser aromático, y comprende 0, 1 ó 2 heteroátomos, iguales o diferentes, seleccionados de O, N y S, en donde el ciclo puede estar opcionalmente sustituido con uno o más Rᵃ, en donde Rᵃ se selecciona en cada caso de halo, CN, alquilo C₁₋₆, haloalquilo C₁₋₆, pentafluorosulfanilo, -O-alquilo C₁₋₃ y -O-haloalquilo C₁₋₃; en donde R es un triciclo seleccionado de las fórmulas (2) y (3), en donde ⁻ ⁻ ⁻ ⁻ ⁻ es un enlace sencillo o doble, X¹, X², X⁶, X⁷ y X⁸ se seleccionan en cada caso de N y C opcionalmente sustituidos, en donde los sustituyentes se seleccionan de alquilo C₁₋₃; en donde tanto X¹ como X² no pueden ser N al mismo tiempo, y X⁶ y X⁷ y X⁷ y X⁸ no pueden ser N al ...

Подробнее
25-10-2023 дата публикации

Prmts inhibitors

Номер: EP4263545A1
Принадлежит: AMGEN INC

Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

Подробнее
08-08-2024 дата публикации

Tricyclic carboxamide derivatives as prmt5 inhibitors

Номер: AU2021386149A9
Принадлежит: AMGEN INC

Described herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, such as cancer, metabolic and blood disorders. Compounds of Formula (I) have the following structure of Formule (I).

Подробнее
26-05-1931 дата публикации

Universal connection for piston rods

Номер: US1807382A
Автор: John R Butler
Принадлежит: Individual

Подробнее
10-10-2024 дата публикации

Biaryl derivatives and related uses

Номер: WO2024211834A1
Принадлежит: Moma Therapeutics, Inc.

The present disclosure relates to compounds of Formula (I), and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating DNA polymerase Q activity and may be used in the treatment of disorders in which DNA polymerase Q activity is implicated, such as cancer.

Подробнее
24-10-2024 дата публикации

PRMT5 inhibitors

Номер: AU2021400942A9
Принадлежит: AMGEN INC

Described herein are novel PRMT5 inhibitors of Formula I and pharmaceutically acceptable salts thereof, as well the pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity and may have use in treating proliferative, metabolic and blood disorders. Compounds of Formula I have the following structure:

Подробнее
10-10-2024 дата публикации

Semi-saturated bicyclic derivatives and related uses

Номер: WO2024211836A2
Принадлежит: Moma Therapeutics, Inc.

The present disclosure relates to compounds of Formula (I): and to their prodrugs, pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for modulating DNA polymerase Θ activity and may be used in the treatment of disorders in which DNA polymerase Θ activity is implicated, such as cancer.

Подробнее
04-10-2016 дата публикации

Bicyclic sulfonamide compounds as sodium channel inhibitors

Номер: US09458152B2
Принадлежит: AMGEN INC

The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

Подробнее