Agustin Casimiro-Garcia

Summary

Affiliation: Pfizer Global Research and Development
Country: USA

Publications

  1. ncbi request reprint The discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an orally efficacious factor Xa inhibitor
    Jeffrey T Kohrt
    Michigan Laboratories, Ann Arbor Campus, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Chem Biol Drug Des 70:100-12. 2007
  2. doi request reprint Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies
    Agustin Casimiro-Garcia
    Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Bioorg Med Chem 16:4883-907. 2008
  3. doi request reprint Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ
    Agustin Casimiro-Garcia
    Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, 200 CambridgePark Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 23:767-72. 2013
  4. doi request reprint Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists
    Agustin Casimiro-Garcia
    Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Rd, Ann Arbor, MI 48105, USA
    Bioorg Med Chem 17:7113-25. 2009
  5. doi request reprint Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ
    Agustin Casimiro-Garcia
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Rd, Groton, Connecticut 06340, United States
    J Med Chem 54:4219-33. 2011
  6. doi request reprint Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action
    Chad A Van Huis
    Michigan Laboratories, Ann Arbor Campus, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Bioorg Med Chem 17:2501-11. 2009
  7. ncbi request reprint Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors
    Chad A Van Huis
    Chem Biol Drug Des 69:444-50. 2007

Collaborators

Detail Information

Publications7

  1. ncbi request reprint The discovery of (2R,4R)-N-(4-chlorophenyl)-N- (2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl)-4-methoxypyrrolidine-1,2-dicarboxamide (PD 0348292), an orally efficacious factor Xa inhibitor
    Jeffrey T Kohrt
    Michigan Laboratories, Ann Arbor Campus, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Chem Biol Drug Des 70:100-12. 2007
    ..This compound is a selective, orally bioavailable, efficacious FXa inhibitor that is currently in phase II clinical trials for the treatment and prevention of thrombotic disorders...
  2. doi request reprint Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies
    Agustin Casimiro-Garcia
    Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Bioorg Med Chem 16:4883-907. 2008
    ..An X-ray crystal structure of the complex of 53 with the PPARgamma-ligand-binding domain was obtained and discussed in this report...
  3. doi request reprint Design, synthesis, and evaluation of imidazo[4,5-c]pyridin-4-one derivatives with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ
    Agustin Casimiro-Garcia
    Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, 200 CambridgePark Drive, Cambridge, MA 02140, USA
    Bioorg Med Chem Lett 23:767-72. 2013
    ..Among them, 21b was identified possessing potent dual pharmacology (AT1 IC(50) = 7 nM; PPARγ EC(50) = 295 nM, 27% max) and good ADME properties...
  4. doi request reprint Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists
    Agustin Casimiro-Garcia
    Department of Chemistry, Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Rd, Ann Arbor, MI 48105, USA
    Bioorg Med Chem 17:7113-25. 2009
    ..The increased potency for binding and activation of both PPAR subtypes observed with 17j when compared to previous analogs in this series was explained based on results derived from crystallographic and modeling studies...
  5. doi request reprint Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-γ
    Agustin Casimiro-Garcia
    Pfizer Global Research and Development, Groton Laboratories, Eastern Point Rd, Groton, Connecticut 06340, United States
    J Med Chem 54:4219-33. 2011
    ..In the SHR, 2l was highly efficacious in lowering blood pressure, while robust lowering of glucose and triglycerides was observed in the male ZDF rat...
  6. doi request reprint Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action
    Chad A Van Huis
    Michigan Laboratories, Ann Arbor Campus, Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA
    Bioorg Med Chem 17:2501-11. 2009
    ....
  7. ncbi request reprint Structure-based drug design of pyrrolidine-1, 2-dicarboxamides as a novel series of orally bioavailable factor Xa inhibitors
    Chad A Van Huis
    Chem Biol Drug Des 69:444-50. 2007
    ..Optimization of the initial hit resulted in an orally bioavailable, subnanomolar inhibitor of factor Xa (13, IC(50) = 0.38 nM), which was shown to be efficacious in a canine electrolytic model of thrombosis with minimal bleeding...