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Selective and dual action orally active inhibitors of thrombin and factor Xa. 2007
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Rob.J.Young@gsk.com
The synthetic entry to new classes of dual fXa/thrombin and selective thrombin inhibitors with significant oral bioavailability is described. This was achieved through minor modifications to the sulfonamide group in our potent and selective fXa inhibitor (E)-2-(5-chlorothien-2-yl)-N-{(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide and these observed activity changes have been rationalised using structural studies.
Related Publications
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
June 2007,
Bioorganic & medicinal chemistry letters,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
December 2011,
Bioorganic & medicinal chemistry letters,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
November 2004,
Hamostaseologie,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
May 2003,
Seminars in vascular medicine,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
June 2004,
Bioorganic & medicinal chemistry letters,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
March 2008,
Bioorganic & medicinal chemistry,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
October 2010,
Bioorganic & medicinal chemistry letters,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
May 2001,
Medizinische Monatsschrift fur Pharmazeuten,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
April 2006,
Bioorganic & medicinal chemistry letters,
Robert J Young, and
David Brown, and
Cynthia L Burns-Kurtis, and
Chuen Chan, and
Máire A Convery, and
Julia A Hubbard, and
Henry A Kelly, and
Anthony J Pateman, and
Angela Patikis, and
Stefan Senger, and
Gita P Shah, and
John R Toomey, and
Nigel S Watson, and
Ping Zhou
March 2009,
Bioorganic & medicinal chemistry,
