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
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- 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 |
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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 (29)
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) |
HK (1) | HK1174614A1 (es) |
HR (1) | HRP20140072T1 (es) |
IL (2) | IL219121A0 (es) |
MX (1) | MX2012003720A (es) |
NZ (2) | NZ613580A (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 (9)
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 |
US20170202845A1 (en) * | 2014-07-17 | 2017-07-20 | Santen Pharmaceutical Co., Ltd. | Prophylactic or therapeutic agent for a posterior ocular disease |
US11052069B2 (en) | 2016-09-14 | 2021-07-06 | Novartis Ag | Regimes of FXR agonists |
JOP20190040A1 (ar) | 2016-09-14 | 2019-03-10 | Novartis Ag | توليفة من ناهضات fxr |
CA3070423A1 (en) * | 2017-07-20 | 2019-01-24 | 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-oxopyrrolidin-1-yl)cyclohexyl)acetamide |
EP3743076A1 (en) | 2018-01-22 | 2020-12-02 | Bristol-Myers Squibb Company | Compositions and methods of treating cancer |
CA3158521A1 (en) * | 2019-11-13 | 2021-05-20 | 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 |
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