MX2012003720A - N-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo[ 1,5-a][1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos. - Google Patents
N-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo[ 1,5-a][1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos.Info
- Publication number
- MX2012003720A MX2012003720A MX2012003720A MX2012003720A MX2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A MX 2012003720 A MX2012003720 A MX 2012003720A
- Authority
- MX
- Mexico
- Prior art keywords
- tert
- oxopyrrolidin
- triazin
- ylamino
- butylamino
- Prior art date
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Abstract
La presente invención proporciona un antagonista novedoso: N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-3-(7-tert-butilpirazolo[ 1,5-a] [1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida: (ver fórmula) o su sal, solvato o profármaco, farmacéuticamente aceptable, que tiene una actividad del receptor dual de CCR-2 y CCR-5 inesperada. También se describen formas cristalinas, metabolitos, composiciones farmacéuticas que contienen los mismos y procesos de uso de los mismos como agentes para el tratamiento de enfermedades inflamatorias, alérgicas, autoinmunes, metabólicas, cáncer y/o cardiovasculares. La presente invención también proporciona procesos de preparación de compuestos de Fórmula (I) como los provistos en la presente, incluyendo N-((1R,2S,5R)-5-(tert-butilamino)-2-((S)-3-(7-tert-buti lpirazolo[1,5-a] [1,3,S]triazin-4-ilamino)-2-oxopirrolidin-1-il)ci clohexil)acetamida. También se proporcionan en la presente compuestos que son intermediarios útiles del proceso.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US25097809P | 2009-10-13 | 2009-10-13 | |
| PCT/US2010/052288 WO2011046916A1 (en) | 2009-10-13 | 2010-10-12 | N-((1r,2s,5r)-5-(tert-butylamino)-2-((s)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2012003720A true MX2012003720A (es) | 2012-04-30 |
Family
ID=43063940
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2012003720A MX2012003720A (es) | 2009-10-13 | 2010-10-12 | N-((1r,2s,5r)-5-(tert-butilamino)-2-((s)-3-(7-tert-butilpirazolo[ 1,5-a][1,3,5]triazin-4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)a cetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos. |
Country Status (28)
| Country | Link |
|---|---|
| US (3) | US8383812B2 (es) |
| EP (2) | EP2664620A3 (es) |
| JP (1) | JP5759999B2 (es) |
| KR (1) | KR20120102052A (es) |
| CN (1) | CN102648201B (es) |
| AR (1) | AR078627A1 (es) |
| AU (1) | AU2010306968B2 (es) |
| BR (1) | BR112012008650B1 (es) |
| CA (1) | CA2777563A1 (es) |
| CL (1) | CL2014000753A1 (es) |
| CO (1) | CO6460737A2 (es) |
| DK (1) | DK2488523T3 (es) |
| EA (2) | EA020486B1 (es) |
| ES (1) | ES2442897T3 (es) |
| HR (1) | HRP20140072T1 (es) |
| IL (2) | IL219121A0 (es) |
| MX (1) | MX2012003720A (es) |
| NZ (2) | NZ599311A (es) |
| PE (1) | PE20121349A1 (es) |
| PL (1) | PL2488523T3 (es) |
| PT (1) | PT2488523E (es) |
| RS (1) | RS53131B (es) |
| SI (1) | SI2488523T1 (es) |
| SM (1) | SMT201400020B (es) |
| TN (1) | TN2012000132A1 (es) |
| TW (1) | TW201120042A (es) |
| WO (1) | WO2011046916A1 (es) |
| ZA (1) | ZA201305994B (es) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8383812B2 (en) * | 2009-10-13 | 2013-02-26 | Bristol-Myers Squibb Company | N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-A][1,3,5]triazin-4-ylamino)-2-oxopyrrolidin-1-yl)cyclohexyl)acetamide, a dual modulator of chemokine receptor activity, crystalline forms and processes |
| BR112017000991A2 (pt) * | 2014-07-17 | 2018-07-24 | Santen Pharmaceutical Co Ltd | agente profilático ou terapêutico para uma doença ocular posterior |
| WO2018051229A1 (en) | 2016-09-14 | 2018-03-22 | Novartis Ag | Novel regimes of fxr agonists |
| JOP20190040A1 (ar) | 2016-09-14 | 2019-03-10 | Novartis Ag | توليفة من ناهضات fxr |
| US11254679B2 (en) * | 2017-07-20 | 2022-02-22 | Bristol-Myers Squibb Company | Process for the preparation of N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-3-(7-tert-butylpyrazolo[1,5-a][1,3,5]triazin-4-ylamino)-2-oxopyrroldin-1-yl)cyclohexyl)acetamide |
| EA202091751A1 (ru) * | 2018-01-22 | 2020-11-06 | Бристол-Маерс Сквибб Компани | Композиции и способы лечения рака |
| US12006318B2 (en) * | 2019-11-13 | 2024-06-11 | Rapt Therapeutics, Inc. | Crystalline forms of C-C chemokine receptor type 4 antagonist and uses thereof |
| JP2023538533A (ja) | 2020-08-07 | 2023-09-08 | ブリストル-マイヤーズ スクイブ カンパニー | 線維症の処置のための、ccr2/5拮抗剤と組み合わせたfgf21 |
| WO2023092049A1 (en) * | 2021-11-19 | 2023-05-25 | Bristol-Myers Squibb Company | Azirine pharmaceutical compositions |
| CN118987211B (zh) * | 2023-05-22 | 2025-09-19 | 无锡瓴方生物医药科技有限公司 | 一种联合用药物组合物及其应用 |
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| DE812551C (de) | 1949-05-13 | 1951-09-03 | Basf Ag | Verfahren zur Herstellung von Pyrrolidon-Derivaten |
| JPS6383082A (ja) | 1986-09-26 | 1988-04-13 | Takeda Chem Ind Ltd | テトラヒドロフランカルボン酸誘導体の製造法 |
| CA2084800A1 (en) | 1991-12-16 | 1993-06-17 | Joseph P. Vacca | Hiv protease inhibitors with an internal lactam ring |
| GB9515411D0 (en) | 1995-07-27 | 1995-09-27 | Pharmacia Spa | N-(4-substituted-benzyl)-2-aminolactam derivatives |
| US5827875A (en) | 1996-05-10 | 1998-10-27 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
| UA51716C2 (uk) | 1996-07-08 | 2002-12-16 | Авентіс Фармасьютікалз Продактс Інк. | Сполуки, що мають гіпотензивну, кардіопротекторну, анти-ішемічну та антиліполітичну властивості, фармацевтична композиція та способи лікування |
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| US6620823B2 (en) | 2000-07-11 | 2003-09-16 | Bristol-Myers Squibb Pharme Company | Lactam metalloprotease inhibitors |
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| JP2005506949A (ja) * | 2000-12-20 | 2005-03-10 | ブリストル−マイヤーズ・スクイブ・ファーマ・カンパニー | ケモカイン受容体の調節剤としてのジアミン |
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