Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.

@article{Kaila2014DiscoveryOI,
  title={Discovery of isoquinolinone indole acetic acids as antagonists of chemoattractant receptor homologous molecule expressed on Th2 cells (CRTH2) for the treatment of allergic inflammatory diseases.},
  author={Neelu Kaila and Bruce C. Follows and Louis Leung and Jennifer Thomason and Adrian Huang and Alessandro Moretto and Kristin Janz and Michael D Lowe and Tarek S. Mansour and Cedric Hubeau and Karen Page and Paul R Morgan and Susan Fish and Xin Xu and Cara Penry Williams and Eddine Saiah},
  journal={Journal of medicinal chemistry},
  year={2014},
  volume={57 4},
  pages={1299-322}
}
Previously we reported the discovery of CRA-898 (1), a diazine indole acetic acid containing CRTH2 antagonist. This compound had good in vitro and in vivo potency, low rates of metabolism, moderate permeability, and good oral bioavailability in rodents. However, it showed low oral exposure in nonrodent safety species (dogs and monkeys). In the current paper… CONTINUE READING