RU2003130093A - 4-(2-бутиламино)-2,7-диметил-8-(2-метил-6-метоксипирид-3-ил) пиразоло-[1,5-а]-1,3,5-триазин, его энантиомеры и фармацевтически приемлемые соли в качестве лигандов рецепторов рилизинг- фактора кортикотропина - Google Patents
4-(2-бутиламино)-2,7-диметил-8-(2-метил-6-метоксипирид-3-ил) пиразоло-[1,5-а]-1,3,5-триазин, его энантиомеры и фармацевтически приемлемые соли в качестве лигандов рецепторов рилизинг- фактора кортикотропина Download PDFInfo
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Claims (17)
2. Соединение по п.1, его фармацевтически приемлемые пролекарства или фармацевтически приемлемые солевые формы, где указанное соединение представляет собой 4-((R)-2-бутиламино)-2,7-диметил-8-(2-метил-6-метоксипирид-3-ил)[1,5-a]пиразоло-1,3,5-триазин.
3. Соединение по п.1, его фармацевтически приемлемые пролекарства или фармацевтически приемлемые солевые формы, где указанное соединение по существу не содержит его (S) стереоизомер.
4. Соединение по п.1, где указанное соединение представляет собой 4-(2-бутиламино)-2,7-диметил-8-(2-метил-6-метоксипирид-3-ил)[1,5-a]пиразоло-1,3,5-триазин.
5. Соединение по п.1, где указанное соединение представляет собой 4-((R)-2-бутиламино)-2,7-диметил-8-(2-метил-6-метоксипирид-3-ил)[1,5-a]пиразоло-1,3,5-триазин.
6. Фармацевтическая композиция, включающая фармацевтически приемлемый носитель и терапевтически эффективное количество соединения по п.1.
7. Фармацевтическая композиция, включающая фармацевтически приемлемый носитель и терапевтически эффективное количество соединения по п.5.
8. Способ антагонистического воздействия на рецептор CRF у млекопитающего, включающий введение млекопитающему терапевтически эффективного количества соединения по п.1.
9. Способ лечения расстройства, проявляющегося гиперсекрецией CRF у теплокровного животного, включающий введение животному терапевтически эффективного количества соединения по п.1.
10. Способ лечения расстройства, лечение которого можно осуществить или облегчить антагонистическим воздействием на CRF, включающий введение млекопитающему терапевтически эффективного количества соединения по п.1.
11. Способ антагонистического воздействия на рецептор CRF у млекопитающего, включающий введение млекопитающему терапевтически эффективного количества соединения по п.5.
12. Способ лечения тревоги или депрессии у млекопитающих, включающий введение млекопитающему терапевтически эффективного количества соединения по п.1.
13. Способ лечения тревоги или депрессии у млекопитающих, включающий введение млекопитающему терапевтически эффективного количества соединения по п. 5.
14. Способ скрининга для выявления лигандов рецепторов CRF, причем способ включает: а) проведение анализа конкурентного связывания с рецептором CRF количества соединения по п.1, которое мечено выявляемой меткой, и потенциального лиганда; и b) определение способности указанного потенциального лиганда заместить указанное меченое соединение.
15. Способ выявления рецепторов CRF в ткани, включающий: а) обеспечение контакта соединения по п.1, которое мечено выявляемой меткой, с тканью при условиях, которые обеспечивают возможность связывания соединения с тканью; и b) выявление меченого соединения, связанного с тканью.
16. Способ ингибирования связывания CRF с рецептором CRF-1, включающий обеспечение контакта соединения по п.1 с раствором, включающим клетки, экспрессирующие рецептор CRF1, причем соединение присутствует в растворе в концентрации, достаточной для ингибирования связывания CRF с рецептором CRF-1.
17. Изделие, включающее: а) упаковочный материал; b) соединение по п.1; и с) этикетку или вкладыш упаковки, содержащийся внутри указанного упаковочного материала и указывающий, что указанное соединение эффективно для лечения тревоги или депрессии.
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RU2003130093/04A RU2292347C2 (ru) | 2001-03-13 | 2002-03-06 | 4-(2-БУТИЛАМИНО)-2,7-ДИМЕТИЛ-8-(2-МЕТИЛ-6-МЕТОКСИПИРИД-3-ИЛ)ПИРАЗОЛО-[1,5-а]-1,3,5-ТРИАЗИН, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЕГО СОДЕРЖАЩАЯ, И ЕГО ПРИМЕНЕНИЕ |
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US7094782B1 (en) * | 1996-07-24 | 2006-08-22 | Bristol-Myers Squibb Company | Azolo triazines and pyrimidines |
US20030125330A1 (en) * | 2001-03-13 | 2003-07-03 | Gilligan Paul J. | 4 - (2-butylamino) - 2, 7-dimethyl-8- (2-methyl-6-methoxypyrid-3-yl) pyrazolo- [1,5-A] - 1,3,5-triazine, its enantiomers and pharmaceutically acceptable salts as corticotropin releasing factor receptor ligands |
FR2842809A1 (fr) * | 2002-07-26 | 2004-01-30 | Greenpharma Sas | NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION |
AR041470A1 (es) * | 2002-10-17 | 2005-05-18 | Upjohn Co | Compuestos de pirrolo (1,2 - b) piridazina y sus usos |
US7329658B2 (en) * | 2003-02-06 | 2008-02-12 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
US7176210B2 (en) * | 2003-02-10 | 2007-02-13 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
US7041671B2 (en) | 2003-04-02 | 2006-05-09 | Pfizer Inc | Pyrrolo[1,2-b]pyridazine compounds and their uses |
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