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    • 3. 发明授权
    • Water soluble camptothecin derivatives
    • 水溶性喜树碱衍生物
    • US5559235A
    • 1996-09-24
    • US258136
    • 1994-06-10
    • Michael J. LuzzioJeffrey M. BestermanMichael G. EvansPeter L. Myers
    • Michael J. LuzzioJeffrey M. BestermanMichael G. EvansPeter L. Myers
    • C07D317/66C07D319/18C07D491/22A61K31/47
    • C07D319/18C07D317/66
    • The present invention relates to water soluble, camptothecin derivatives of formula (I), ##STR1## wherein: 1) R.sup.1 and R.sup.2 represent independently, hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy lower alkyl;ii) R.sup.1 represents hydrogen, lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl or lower alkoxy lower alkyl, and R.sup.2 represents --COR.sup.3,wherein:R.sup.3 represents hydrogen, lower alkyl, perhalo-lower alkyl, C.sub.3-7)cycloalkyl, C.sub.3-7)cycloalkyl lower alkyl, lower alkenyl, hydroxy lower alkyl, lower alkoxy or lower alkoxy lower alkyl; oriii) R.sup.1 and R.sup.2 taken together with the linking nitrogen form a saturated 3 to 7 atom heterocyclic group of formula (IA) ##STR2## wherein: Y represents O, S, SO, SO.sub.2, CH.sub.2 or NR.sup.4wherein:R.sup.4 represents hydrogen, lower alkyl, perhalo lower alkyl, aryl, aryl substituted with one or more lower alkyl, lower alkoxy, halogen, nitro, amino, lower alkyl amino, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or;--COR.sup.5,wherein:R.sup.5 represents hydrogen, lower alkyl, perhalo-lower alkyl, lower alkoxy, aryl, aryl substituted with one or more lower alkyl, perhalo-lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl groups or;the pharmaceutically acceptable salts thereof; their use in the treatment of tumors and methods of their preparation.
    • 本发明涉及式(I)的水溶性喜树碱衍生物,其中:1)R1和R2独立地表示氢,低级烷基,C3-7)环烷基,C3-7)环烷基低级烷基 低级烯基,羟基低级烷基,低级烷氧基低级烷基; ii)R1表示氢,低级烷基,C3-7)环烷基,C3-7)环烷基低级烷基,低级烯基,羟基低级烷基或低级烷氧基低级烷基,R2表示-COR3,其中:R3表示氢,低级烷基, 全卤代低级烷基,C3-7)环烷基,C3-7)环烷基低级烷基,低级烯基,羟基低级烷基,低级烷氧基或低级烷氧基低级烷基; 或(iii)R 1和R 2与连接氮一起形成式(IA)的饱和3至7个原子的杂环基(IA)其中:Y表示O,S,SO,SO 2,CH 2或NR 4,其中:R 4 代表氢,低级烷基,全卤代低级烷基,芳基,被一个或多个低级烷基,低级烷氧基,卤素,硝基,氨基,低级烷基氨基,全卤代低级烷基,羟基低级烷基,低级烷氧基低级烷基取代的芳基。 -COR 5,其中:R 5表示氢,低级烷基,全卤代低级烷基,低级烷氧基,芳基,被一个或多个低级烷基,全卤代低级烷基,羟基低级烷基,低级烷氧基低级烷基取代的芳基。 其药学上可接受的盐; 其用于治疗肿瘤及其制备方法。
    • 6. 发明申请
    • Knife having superior functionality and appeal
    • 刀具具有优越的功能和吸引力
    • US20090293289A1
    • 2009-12-03
    • US12455322
    • 2009-06-01
    • William A. GallopMichael G. EvansAshish K. Mithal
    • William A. GallopMichael G. EvansAshish K. Mithal
    • B26B27/00
    • B26B3/02
    • A plastic knife adapted for resting on a table surface with the blade disposed in a vertical orientation. The knife includes a blade connected to a handle, a top wall, a middle wall and a bottom wall. The middle wall is connected to the blade and is orthogonal to the top and bottom walls. The blade includes a narrow blade tip and a cutting edge. The top wall features a tapering profile with a wide handle end, a narrow blade end, and a transition area of intermediate widths. The transition area is disposed between the wide handle end and the narrow blade end. The bottom wall includes a flat section for resting on a flat table surface. The knife features superior functionality and strength and may include a thin metallic coating deposited on at least a portion of one of its surfaces.
    • 一种塑料刀,适于搁置在桌面上,刀片以垂直方向设置。 刀包括连接到手柄,顶壁,中间壁和底壁的刀片。 中间壁与叶片连接并且与顶壁和底壁垂直。 刀片包括窄刀片尖端和切削刃。 顶壁具有锥形轮廓,具有宽的手柄端,窄的刀片端部和中间宽度的过渡区域。 过渡区域设置在宽手柄端和窄刀片端之间。 底壁包括用于搁置在平台表面上的平坦部分。 刀具有优异的功能和强度,并且可以包括沉积在其表面之一的至少一部分上的薄金属涂层。