A series of retro-binding inhibitors of human a-thrombin was prepared to elucidate structure-acti... more A series of retro-binding inhibitors of human a-thrombin was prepared to elucidate structure-activity relationships (SAR) and optimize in vivo performance. Compounds 9 and 11, orally active inhibitors of thrombin catalytic activity, were identified to be efficacious in a thrombin-induced lethality model in mice.
Bioorganic & Medicinal Chemistry Letters, 2002
A series of structurally novel small molecule inhibitors of human alpha-thrombin was prepared to ... more A series of structurally novel small molecule inhibitors of human alpha-thrombin was prepared to elucidate their structure-activity relationships (SARs), selectivity and activity in vivo. BMS-189664 (3) is identified as a potent, selective, and orally active reversible inhibitor of human alpha-thrombin which is efficacious in vivo in a mouse lethality model, and at inhibiting both arterial and venous thrombosis in cynomolgus monkey models.
Chars were made from four Australian coals of varying vitrinite content at pressures of 5, 10, an... more Chars were made from four Australian coals of varying vitrinite content at pressures of 5, 10, and 15 atm. The morphology of the chars was correlated with the petrography of the parent coal. The intrinsic reaction rates of the chars at high pressures were measured, and no ...
A series of retro-binding inhibitors of human a-thrombin was prepared to elucidate structure-acti... more A series of retro-binding inhibitors of human a-thrombin was prepared to elucidate structure-activity relationships (SAR) and optimize in vivo performance. Compounds 9 and 11, orally active inhibitors of thrombin catalytic activity, were identified to be efficacious in a thrombin-induced lethality model in mice.
Bioorganic & Medicinal Chemistry Letters, 2002
A series of structurally novel small molecule inhibitors of human alpha-thrombin was prepared to ... more A series of structurally novel small molecule inhibitors of human alpha-thrombin was prepared to elucidate their structure-activity relationships (SARs), selectivity and activity in vivo. BMS-189664 (3) is identified as a potent, selective, and orally active reversible inhibitor of human alpha-thrombin which is efficacious in vivo in a mouse lethality model, and at inhibiting both arterial and venous thrombosis in cynomolgus monkey models.
Chars were made from four Australian coals of varying vitrinite content at pressures of 5, 10, an... more Chars were made from four Australian coals of varying vitrinite content at pressures of 5, 10, and 15 atm. The morphology of the chars was correlated with the petrography of the parent coal. The intrinsic reaction rates of the chars at high pressures were measured, and no ...
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