Discovery and optimization of CRTH2 and DP dual antagonists.
Bioorg Med Chem Lett
; 19(22): 6419-23, 2009 Nov 15.
Article
en En
| MEDLINE
| ID: mdl-19804971
ABSTRACT
A series of phenylacetic acid derivatives was discovered as CRTH2 antagonists. Modification of the series led to compounds that are also antagonists of DP. Since activation of CRTH2 and DP are believed to play key roles in mediating responses of asthma and other immune diseases, this series was optimized to increase the dual antagonistic activities and improve pharmacokinetic properties. These efforts led to selection of AMG 009 as a clinical candidate.
Texto completo:
1
Bases de datos:
MEDLINE
Asunto principal:
Asma
/
Receptores de Prostaglandina
Límite:
Animals
/
Humans
Idioma:
En
Revista:
Bioorg Med Chem Lett
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2009
Tipo del documento:
Article
País de afiliación:
Estados Unidos