Discovery of INCB10820/PF-4178903, a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist.
Bioorg Med Chem Lett
; 21(5): 1442-6, 2011 Mar 01.
Article
em En
| MEDLINE
| ID: mdl-21295478
ABSTRACT
We report the discovery of a potent, selective, and orally bioavailable dual CCR2 and CCR5 antagonist (3S,4S)-N-[(1R,3S)-3-isopropyl-3-({4-[4-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl}carbonyl)cyclopentyl]-3-methoxytetrahydro-2H-pyran-4-amine (19). After evaluation in 28-day toxicology studies, compound 19 (INCB10820/PF-4178903) was selected as a clinical candidate.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperazinas
/
Piranos
/
Receptores CCR2
/
Descoberta de Drogas
/
Antagonistas dos Receptores CCR5
Limite:
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos