Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
J Med Chem
; 56(18): 7343-57, 2013 Sep 26.
Article
em En
| MEDLINE
| ID: mdl-23964740
ABSTRACT
Optimization of a 5-oxopyrrolopyridine series based upon structure-activity relationships (SARs) developed from our previous efforts on a number of related bicyclic series yielded compound 2s (BMS-767778) with an overall activity, selectivity, efficacy, PK, and developability profile suitable for progression into the clinic. SAR in the series and characterization of 2s are described.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Desenho de Fármacos
/
Dipeptidil Peptidase 4
/
Compostos Bicíclicos Heterocíclicos com Pontes
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Inibidores da Dipeptidil Peptidase IV
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Acetamidas
Limite:
Animals
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Humans
/
Male
Idioma:
En
Revista:
J Med Chem
Ano de publicação:
2013
Tipo de documento:
Article