公开(公告)号：EP1173253A1

公开(公告)日：2002-01-23

申请号：EP00935851.6

申请日：2000-05-01

申请人： American Home Products Corporation ,  LIGAND PHARMACEUTICALS INCORPORATED

发明人： GRUBB, Gary, S. ,  ZHI, Lin ,  JONES, Todd, K. ,  SANTILLI, Arthur, A. ,  TEGLEY, Christopher, M. ,  VIET, Andrew Q, ,  ZHANG, Puwen, ,  FENSOME, Andrew, ,  WROBEL, Jay, E. ,  EDWARDS, James P.

IPC分类号： A61P15/18 ,  A61K45/06 ,  A61K31/57 ,  A61K31/565

CPC分类号： A61K31/56 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61K31/565 ,  A61K45/06 ,  A61K2300/00

摘要： This invention relates to cyclic combination therapies and regimens utilizing, in combination with progestins, substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure:where A and B are independent substituents selected from S, CH or N; provided that when A is S, B is CH or N; and when B is S, A is CH or N; and A and B cannot both be CH; and when A and B both equal N, one N may be optionally substituted with an C1 to C6 alkyl group; R1 and R2 are independent substituents selected from the group of H, C1 to C6 alkyl, substituted C1 to C6 alkyl, C2 to C6 alkenyl, substituted C2 to C6 alkenyl, C2 to C6 alkynyl, substituted C2 to C6 alkynyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heterocyclic, substituted heterocyclic, CORA, or NRBCORA; or R1 and R2 are fused to form optionally substituted 3 to 8 membered spirocyclic alkyl, alkenyl or heterocyclic ring, the heterocyclic ring containing one to three heteroatoms selected from the group of O, S and N; or pharmaceutically useful salts thereof. These methods of treatment may be used for contraception.