2-piperidone compounds
    1.
    发明授权
    2-piperidone compounds 失效
    2-哌啶酮化合物

    公开(公告)号:US06492392B1

    公开(公告)日:2002-12-10

    申请号:US09481542

    申请日:2000-01-12

    IPC分类号: A61K31445

    摘要: 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.

    摘要翻译: 本发明提供了具有抑制肿瘤细胞增殖的有效活性的2-哌啶酮化合物或其药学上可接受的盐,因此可用作药物,以及含有这些化合物的抗肿瘤剂。 2-哌啶酮化合物由下式(I)表示:其中R1表示 - (CH2)nR1a {其中n为0-5的整数,R1a表示氨基,低级烷基氨基,二(低级烷基)氨基,取代的 或未取代的芳基,或取代或未取代的杂环基},R2和R3独立地表示可以被低级烷氧基羰基取代的低级烷基; 可被取代或未取代的芳基或取代或未取代的杂环基取代的低级烯基,芳烷基或低级炔基; 取代或未取代的芳基; 或取代或未取代的杂环基。

    DC107 derivatives
    6.
    发明授权
    DC107 derivatives 失效
    DC107衍生品

    公开(公告)号:US5981558A

    公开(公告)日:1999-11-09

    申请号:US133614

    申请日:1998-08-13

    CPC分类号: C07D513/18 C07H15/26

    摘要: DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4, or the like; R.sup.2 represents hydrogen or COR.sup.6 ; R.sup.3 represents --CH.sub.2 OCOR.sup.7, phthalimidomethyl, or the like; and W represents oxygen or NR.sup.8 (wherein R.sup.8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).

    摘要翻译: 提供了具有抗微生物活性和抗肿瘤活性的由式​​(I)表示的DC107衍生物或其药学上可接受的盐,其中R1表示氢,低级烷氧基烷基,芳烷氧基烷基,低级烷氧基烷氧基烷基,低级烷氧基烷氧基烷氧基烷基,芳烷基,四氢吡喃基,COR4等; R2表示氢或COR6; R3表示-CH2OCOR7,苯二甲酰亚氨基甲基等; W表示氧或NR8(其中R8表示羟基,低级烷氧基,低级烯氧基,芳烷氧基,取代或未取代的芳基磺酰基氨基或低级烷氧基羰基氨基)。

    DC 107 derivatives and treatment methods
    8.
    发明授权
    DC 107 derivatives and treatment methods 失效
    DC 107衍生物和处理方法

    公开(公告)号:US5733924A

    公开(公告)日:1998-03-31

    申请号:US776938

    申请日:1997-04-17

    IPC分类号: C07D513/08 A61K37/00

    CPC分类号: C07D513/08

    摘要: DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, �wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.!

    摘要翻译: PCT No.PCT / JP96 / 01646 Sec。 371日期1997年04月17日 102(e)1997年4月17日PCT PCT 1996年6月14日PCT公布。 出版物WO97 / 00260 PCT 日本1997年3月1日由式(I)代表的DC107衍生物:其中R1为氢,低级烷氧基烷基,芳烷氧基烷基,低级烷氧基烷氧基烷基,低级烷氧基烷氧基烷氧基烷基,芳烷基,四氢吡喃基,COR4或 类似; R2表示氢或COR5; R3代表低级烷基,低级烯基,可被取代或未取代的芳基取代的芳烷基,低级烷氧基烷基,芳烷氧基烷基,取代或未取代的芳氧基烷基,低级烷氧基羰基烷基,低级烷酰氧基烷基,脂环族烷酰氧基烷基等,或与Y键合以表示单键 ; Y键合到R3表示单键,或键合到Z表示单键; Z表示氢或与Y键合以表示单键; W表示氧或NR 6,条件是其中R1,R2和Z各自表示氢,R3与Y键合以表示单键,W表示氧(DC107)的化合物。