CO6460737A2 - N-((1r,2s,5r)-5-(tert -butilamino)-2-((s)-3-(7-tert-butilpirazolo[1.5-a][1.3.5]traizin -4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)acetamida, 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]traizin -4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)acetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos

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Publication number
CO6460737A2
CO6460737A2 CO12060326A CO12060326A CO6460737A2 CO 6460737 A2 CO6460737 A2 CO 6460737A2 CO 12060326 A CO12060326 A CO 12060326A CO 12060326 A CO12060326 A CO 12060326A CO 6460737 A2 CO6460737 A2 CO 6460737A2
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Colombia
Prior art keywords
tert
acetamide
processes
activity
oxopirrolidin
Prior art date
Application number
CO12060326A
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English (en)
Inventor
Percy H Carter
Robert J Cherney
Jun Li
Victor W Rosso
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Bristol Myers Squibb Co
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Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CO6460737A2 publication Critical patent/CO6460737A2/es

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    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
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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)acetamida: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-butilpirazolo[1,5-a][1,3,5]triazin-4-ilamino)-2- oxopirrolidin-1-il)ciclohexil)acetamida. También se proporcionan en la presente compuestos que son intermediarios útiles del proceso.
CO12060326A 2009-10-13 2012-04-12 N-((1r,2s,5r)-5-(tert -butilamino)-2-((s)-3-(7-tert-butilpirazolo[1.5-a][1.3.5]traizin -4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)acetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos CO6460737A2 (es)

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US25097809P 2009-10-13 2009-10-13

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CO6460737A2 true CO6460737A2 (es) 2012-06-15

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CO12060326A CO6460737A2 (es) 2009-10-13 2012-04-12 N-((1r,2s,5r)-5-(tert -butilamino)-2-((s)-3-(7-tert-butilpirazolo[1.5-a][1.3.5]traizin -4-ilamino)-2-oxopirrolidin-1-il)ciclohexil)acetamida, un modulador dual de la actividad del receptor de quimiocinas, formas cristalinas y procesos

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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)
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NZ (2) NZ613580A (es)
PE (1) PE20121349A1 (es)
PL (1) PL2488523T3 (es)
PT (1) PT2488523E (es)
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SI (1) SI2488523T1 (es)
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TN (1) TN2012000132A1 (es)
TW (1) TW201120042A (es)
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