会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 7. 发明授权
    • Heregulin antagonists and methods for their use
    • 促胰岛素拮抗剂及其使用方法
    • US6143740A
    • 2000-11-07
    • US308396
    • 1999-08-16
    • Dajun YangShaomeng WangAlan P. KozikowskiMarc E. Lippman
    • Dajun YangShaomeng WangAlan P. KozikowskiMarc E. Lippman
    • C07D498/18A61K31/34A61K31/395A61K31/495A61K31/496A61K31/551A61K31/655A61P35/00A61P43/00C07D498/08A61K31/33C07K1/00C07K16/00
    • A61K31/708A61K31/395A61K31/495A61K31/496A61K31/551A61K31/655A61K31/704A61K31/7076C07D498/08
    • The invention provides a method of inhibiting cancer cell growth, and thereby of treating cancer comprising administering to a mammal afflicted with cancer an effective amount of the compound of formula (I), wherein the variables of R.sub.1, and R.sub.2 have the meanings defined in the specification. The present invention also provides novel compounds of formula (I) as well as novel pharmaceutical compositions and intermediates useful for preparing compounds of formula (I). The figure illustrates the structure and binding activity of compounds of the invention and some of the rifamycin analogs.______________________________________ ##STR1## ______________________________________ Compounds R.sub.1 = ______________________________________ A1 --OH A2 --OH A3 --OH A4 --OH A5 --OH A6 --OH A7 --OH - A8 ##STR2## ______________________________________ Compounds R.sub.2 = ______________________________________ A1 #STR3## - A2 #STR4## - A3 #STR5## - A4 #STR6## - A5 #STR7## - A6 #STR8## - A7 #STR9## - A8 --H ______________________________________ Compounds IC.sub.50 (1) IC.sub.50 (2) ______________________________________ A1 10 uM 1 uM A2 10 uM 3 uM A3 10 uM 3 uM A4 50 uM 5 uM A5 >500 uM >50 uM A6 >500 uM >50 uM A7 >200 uM >50 uM A8 >500 M >50 uM ______________________________________
    • PCT No.PCT / US97 / 21474 Sec。 371日期1999年8月16日 102(e)1999年8月16日PCT 1997年11月19日PCT公布。 第WO98 / 21956号公报 日期1998年5月28日本发明提供抑制癌细胞生长,从而治疗癌症的方法,包括向患有癌症的哺乳动物施用有效量的式(I)化合物,其中R1和R2的变量具有 在本说明书中定义的含义。 本发明还提供新的式(I)化合物以及可用于制备式(I)化合物的新型药物组合物和中间体。 该图示出了本发明化合物和一些利福霉素类似物的结构和结合活性。 - 化合物R1 = -Al-OH-A2-OH-A3-OH-A4-OH-A5-OH-A6-OH-A7 -OH - - A8化合物R2 = 图像 - - A2 - - A3 - - A4 GE> - - A7 - - A8 -H - 化合物IC50(1)IC50(2) - A1 10 uM 1 uM - A2 10 uM 3 uM - A3 10 uM 3 uM - A4 50 uM 5 uM - A5> 500 uM> 50 uM - A6> 500 uM> 50 uM - A7> 200 uM> 50 uM - A8> 500 M> 50 uM -