912846-31-2Relevant academic research and scientific papers
The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs
Watson, Nigel S.,Adams, Carl,Belton, David,Brown, David,Burns-Kurtis, Cynthia L.,Chaudry, Laiq,Chan, Chuen,Convery, Máire A.,Davies, David E.,Exall, Anne M.,Harling, John D.,Irvine, Stephanie,Irving, Wendy R.,Kleanthous, Savvas,McLay, Iain M.,Pateman, Anthony J.,Patikis, Angela N.,Roethke, Theresa J.,Senger, Stefan,Stelman, Gary J.,Toomey, John R.,West, Robert I.,Whittaker, Caroline,Zhou, Ping,Young, Robert J.
scheme or table, p. 1588 - 1592 (2011/05/05)
The discovery and evaluation of potent and long-acting oral sulfonamidopyrrolidin-2-one factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs are described. Unexpected selectivity issues versus tissue plasminogen activator in the form
3-SULFONYLAMINO-PYRROLIDINE-2-ONE DERIVATIVES AS FACTOR XA INHIBITORS
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, (2008/06/13)
The present invention provides at least one chemical entity chosen from compounds of formula (I) wherein: R1 represents a group selected from formula (II), (III), (IV), (V), (VI), (VII), each ring of which optionally contains a further heteroatom N, Z represents an optional substituent halogen, -C1-3alkyl or -NRaRb, alk represents alkylene or alkenylene, T represents S, O or NH; Ra and Rb independently represent hydrogen or -C1-3alkyl; R2 represents a group selected from formula (VIII), (IX), W, X and Y independently represent CH, C-R5 or N; R5 represents halogen or C1-3alkyl; V represents NR3, S or O; R3 represents hydrogen or C1-3alkyl; one of A1 and A2 represents N and the other represents CH; Each R4, R6, R7, R8, R9 independently represents hydrogen or C1-3alkyl; R10 represents hydrogen, -C1-6alkyl, -C1-3alkylCONRaRb, -C1-3alkylCO2C1-4alkyl, -CO2C1-4alkyl or -C1-3alkylCO2H; and pharmaceutically acceptable derivative(s) thereof. The invention also relates to processes for the preparation of compound(s) of formula (I), pharmaceutical compositions containing compound(s) of formula (I) and to the use of compound(s) of formula (I) in medicine, particularly in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.
