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 PDF

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RU2003130093A
RU2003130093A RU2003130093/04A RU2003130093A RU2003130093A RU 2003130093 A RU2003130093 A RU 2003130093A RU 2003130093/04 A RU2003130093/04 A RU 2003130093/04A RU 2003130093 A RU2003130093 A RU 2003130093A RU 2003130093 A RU2003130093 A RU 2003130093A
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Пол Дж ДЖИЛЛИГАН (US)
Пол Дж ДЖИЛЛИГАН
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Бристоль-Мейерз Сквибб Фарма Компани (Us)
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Claims (17)

1. Соединение формулы (I):
Figure 00000001
(I)
его изомеры, стереоизомерные формы или смеси его стереоизомерных форм, его фармацевтически приемлемые пролекарства или фармацевтически приемлемые солевые формы.
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.
RU2003130093/04A 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 RU2292347C2 (ru)

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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
US7056920B2 (en) 2003-04-04 2006-06-06 Pfizer Inc Pyrrolo[1,2-B]pyridazine compounds and their uses
US7034023B2 (en) * 2003-04-04 2006-04-25 Pfizer Inc Pyrrolo[1,2-B]pyridazine compounds and their uses
JP2006523675A (ja) * 2003-04-15 2006-10-19 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー ピロロ[1,2−b]ピリダジン化合物及びそれらの使用
US7153961B2 (en) 2003-11-25 2006-12-26 Bristol-Myers Squibb Pharma Co. Salt and crystalline form thereof of a corticotropin releasing factor receptor antagonist
US7208596B2 (en) * 2003-11-25 2007-04-24 Bristol-Myers Squibb Pharma Company Processes for the preparation of pyrazolo[1,5-a]-1,3,5-triazines and intermediates thereof
US8030304B2 (en) 2006-09-20 2011-10-04 Eli Lilly And Company Thiazole pyrazolopyrimidines CRF1 receptor antagonists
EP2841068B8 (en) * 2012-04-23 2019-03-06 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Crhr1 antagonists for use in the treatment of patients having crh overactivity
GB201210686D0 (en) 2012-06-15 2012-08-01 Holsboermaschmeyer Neurochemie Gmbh V1B receptor antagonist for use in the treatment of patients having an elevated AVP level and/or an elevated copeptin level
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神分裂病を処置するための方法および組成物
GB201310782D0 (en) 2013-06-17 2013-07-31 Max Planck Innovation Gmbh Method for predicting a treatment response to a CRHR1 antagonist and/or V1B antagonist in a patient with depressive and/or anxiety symptoms
KR102079844B1 (ko) * 2016-09-20 2020-02-20 가톨릭대학교 산학협력단 담석 용해제를 포함하는 담낭 질환 치료용 약학 조성물
BR112023002497A2 (pt) 2020-08-12 2023-05-02 Spruce Biosciences Inc Métodos e composições para tratamento da síndrome dos ovários policísticos
US11708372B2 (en) 2021-11-19 2023-07-25 Spruce Biosciences, Inc. Crystalline composition of tildacerfont and methods of use and preparation thereof

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW370529B (en) 1992-12-17 1999-09-21 Pfizer Pyrazolopyrimidines
JP3398152B2 (ja) 1993-10-12 2003-04-21 ブリストル‐マイヤーズ・スクイブ・ファーマ・カンパニー 1n−アルキル−n−アリールピリミジンアミンおよびその誘導体
TW530047B (en) 1994-06-08 2003-05-01 Pfizer Corticotropin releasing factor antagonists
JP2000507552A (ja) 1996-03-26 2000-06-20 デュポン ファーマシューティカルズ カンパニー アリールオキシおよびアリールチオ縮合ピリジン、アリールオキシおよびアリールチオ縮合ピリミジン、およびそれらの誘導体
US6107300A (en) 1996-03-27 2000-08-22 Dupont Pharmaceuticals Arylamino fused pyrimidines
WO1997044308A1 (en) 1996-05-24 1997-11-27 The Dow Chemical Company Process for preparing aliphatic ester compounds and alkanols
PL195762B1 (pl) * 1996-07-24 2007-10-31 Bristol Myers Squibb Pharma Co Związki [1,5-a]pirazolo-1,3,5-triazynowe, środek farmaceutyczny i zastosowanie związków [1,5-a]pirazolo-1,3,5-triazynowych do wytwarzania leku
US6191131B1 (en) * 1997-07-23 2001-02-20 Dupont Pharmaceuticals Company Azolo triazines and pyrimidines
EP0915880B1 (en) 1996-07-24 2007-10-10 Bristol-Myers Squibb Pharma Company Azolo triazines and pyrimidines
AU735401B2 (en) * 1996-08-28 2001-07-05 Pfizer Inc. Substituted 6,5-hetero-bicyclic derivatives
UA62972C2 (en) 1997-07-03 2004-01-15 Application of imidazopyrimidins and imidazopyridins for the treatment of neural disorders
AU746706B2 (en) 1997-07-03 2002-05-02 Du Pont Pharmaceuticals Company Imidazopyrimidines and imidazopyridines for the treatment of neurological disorders
CA2296014A1 (en) 1997-07-03 1999-01-14 Frank W. Hobbs Aryl-and arylamino-substituted heterocycles as corticotropin releasing hormone antagonists
IL134748A0 (en) 1997-09-02 2001-04-30 Du Pont Pharm Co Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone (crh) antagonists, useful for treating cns and stress-related disorders
SI1049699T1 (en) * 1998-01-28 2004-10-31 Bristol-Myers Squibb Pharma Company Pyrazolotriazines as crf antagonists
US6194410B1 (en) * 1998-03-11 2001-02-27 Hoffman-La Roche Inc. Pyrazolopyrimidine and pyrazolines and process for preparation thereof
JP2002510695A (ja) 1998-04-03 2002-04-09 デュポン ファーマシューティカルズ カンパニー 副腎皮質刺激ホルモン放出因子(CRF)拮抗剤としてのチアゾロ[4,5−d]ピリミジンおよびピリジン
US6124463A (en) 1998-07-02 2000-09-26 Dupont Pharmaceuticals Benzimidazoles as corticotropin release factor antagonists
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

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