公开(公告)号：EP0863878A1

公开(公告)日：1998-09-16

申请号：EP96928900.0

申请日：1996-08-15

申请人： HOECHST MARION ROUSSEL, INC.

发明人： THOMAS, Craig, E. ,  FEVIG, Thomas, L. ,  BOWEN, Stephen, M. ,  FARR, Robert, A. ,  CARR, Albert, A. ,  JANOWICK, David, A.

IPC分类号： A61K31 ,  A61P39 ,  C07D209 ,  C07D217 ,  C07D221 ,  C07D223 ,  C07D491 ,  C07D495

CPC分类号： C07D221/20 ,  C07D209/44 ,  C07D217/08 ,  C07D217/24 ,  C07D221/10 ,  C07D223/14 ,  C07D223/16 ,  C07D491/04 ,  C07D491/10 ,  C07D495/04

摘要： The present invention is directed to novel cyclic nitrones of the formula (I) in which R1 and R2 are each independently represented by a C1-3 alkyl or R1 and R2 together form a C5-6 alkylene ring or a ring of structure (a), Z represents (CHx)n, wherein x and n are independently 0 or an integer from 1-2; R3 is represented by a substituent selected from the group consisting of hydrogen, C1-4 alkyl, OH, OAc or (b); and the ring represented by X is a substituent selected from the group consisting of (c), (d), (e) or (f) wherein the area of dark shading represents the side of attachment to the nitrone ring, R4, R5, R6 and R7 are independently selected from the group consisting of hydrogen, C1-3 alkyl, OH or C1-3 alkoxy and the pharmaceutically acceptable salts thereof, with the proviso that when R1 and R2 together form a C5-6 alkylene ring and n is 1, then R3 cannot be hydrogen and their use in the prevention of oxidation tissue damage by free radicals, their use in the treatment of a number of disease states in which radicals either damage or destroy tissues via oxidation, and pharmaceutical compositions containing these cyclic nitrones.