478644-12-1Relevant academic research and scientific papers
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl} sulfonamides
Chan, Chuen,Borthwick, Alan D.,Brown, David,Burns-Kurtis, Cynthia L.,Campbell, Matthew,Chaudry, Laiq,Chung, Chun-Wa,Convery, Máire A.,Hamblin, J. Nicole,Johnstone, Lisa,Kelly, Henry A.,Kleanthous, Savvas,Patikis, Angela,Patel, Champa,Pateman, Anthony J.,Senger, Stefan,Shah, Gita P.,Toomey, John R.,Watson, Nigel S.,Weston, Helen E.,Whitworth, Caroline,Young, Robert J.,Zhou, Ping
, p. 1546 - 1557 (2008/02/01)
Factor Xa inhibitory activities for a series of N-{(3S)-1-[(1S)-1-methyl-2- morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides with different P1 groups are described. These data provide insight into binding interactions within the S1 primary spe
Selective and dual action orally active inhibitors of thrombin and factor Xa
Young, Robert J.,Brown, David,Burns-Kurtis, Cynthia L.,Chan, Chuen,Convery, Maire A.,Hubbard, Julia A.,Kelly, Henry A.,Pateman, Anthony J.,Patikis, Angela,Senger, Stefan,Shah, Gita P.,Toomey, John R.,Watson, Nigel S.,Zhou, Ping
, p. 2927 - 2930 (2008/02/04)
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.
CRYSTALLINE FORM
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Page 17-19, (2010/02/07)
(E)-2-(5-Chlorothien-2-yl)-N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide in substantially crystalline form, pharmaceutical formulations thereof, processes for preparing it, and its use inmedicine, particularl
PYRROLYDIN-2-ONE DERIVATIVES AS INHIBITORS OF THROMBIN AND FACTOR XA
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Page 54, (2010/02/07)
The invention relates to compounds of formula (I), wherein : R1 represents hydrogen, C1-4 alkyl, -CH2CO2H, -CH2CO2C1-2alkyl, or -CH2CONR7R8; Rsu
