申请人:Kyowa Hakko Kogyo Co., Ltd.
公开号:US06492392B1
公开(公告)日:2002-12-10
The present invention provides 2-piperidone compounds or pharmaceutically acceptable salts thereof, which have a potent activity of inhibiting the proliferation of tumor cells and thus are useful as medicaments, as well as antitumor agents containing these compounds. The 2-piperidone compound is represented by the following formula (I):
wherein
R1 represents —(CH2)nR1a {wherein n is an integer of from 0 to 5, and R1a represents amino, lower alkylamino, di(lower alkyl)amino, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group}, and
R2 and R3 independently represent lower alkyl which may be substituted by lower alkoxycarboyl; lower alkenyl, aralkyl or lower alkynyl which may be substituted by substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; substituted or unsubstituted aryl; or a substituted or unsubstituted heterocyclic group.
本发明提供2-哌啶酮化合物或其药学上可接受的盐,具有抑制肿瘤细胞增殖的强效活性,因此可用作药物,以及含有这些化合物的抗肿瘤剂。2-哌啶酮化合物由以下公式(I)表示:
其中,
R1表示—(CH2)nR1a(其中n为0至5的整数,R1a表示氨基,较低的烷基氨基,二(较低的烷基)氨基,取代或未取代芳基,或取代或未取代的杂环基);
R2和R3独立地表示较低的烷基,可以被较低的烷氧羰基取代;较低的烯基,芳基烷基或较低的炔基,可以被取代或未取代的芳基或取代或未取代的杂环基取代;取代或未取代的芳基;或取代或未取代的杂环基。