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公开(公告)号：US5223506A
公开(公告)日：1993-06-29
申请号：US710230
申请日：1991-06-04
申请人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , M. Ross Johnson , Milana Dezube , Salvatore Profeta, Jr.
发明人： Michael J. Luzzio , Jeffrey M. Besterman , Michael G. Evans , M. Ross Johnson , Milana Dezube , Salvatore Profeta, Jr.
IPC分类号： C07D221/18 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/056 , C07D491/14 , C07D491/147 , C07D491/153
CPC分类号： C07D221/18 , C07D471/04 , C07D491/04 , C07D491/14
摘要： The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen;ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.3 is hydrogen or methoxy and R.sup.4 is hydrogen;iii) when R.sup.2 is hydroxy, methoxy or amino, R.sup.3 is hydrogen, hydroxy or methoxy, and R.sup.4 is hydrogen;iv) when R.sup.4 is hydroxy or amino, R.sup.1 and R.sup.3 are hydrogen and R.sup.2 is hydroxy or amino; and.v) when R.sup.1 is fluoro, chloro, iodo or amino, R.sup.2 is hydrogen, hydroxy or methoxy, R.sup.3 is hydrogen, hydroxy or methoxy and R.sup.4 is hydrogenand the use of these compounds as topoisomerase inhibitors and antitumor agents.
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公开(公告)号：US5318976A
公开(公告)日：1994-06-07
申请号：US931611
申请日：1992-08-18
申请人： Michael J. Luzzi , Jeffrey Besterman , Michael G. Evans , M. Ross Johnson , Milana Dezube , Salvatore Profeta, Jr.
发明人： Michael J. Luzzi , Jeffrey Besterman , Michael G. Evans , M. Ross Johnson , Milana Dezube , Salvatore Profeta, Jr.
IPC分类号： C07D221/18 , C07D471/04 , C07D491/04 , C07D491/048 , C07D491/056 , C07D491/14 , C07D491/147 , C07D491/153 , A61K31/435 , C07D471/14
CPC分类号： C07D221/18 , C07D471/04 , C07D491/04 , C07D491/14
摘要： The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen;X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; andX.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen.
摘要翻译： 本发明涉及式（I）的某些取代的四环稠合喹啉衍生物：其中：R 1是氢，羟基，氟，氯，溴，碘，甲氧基或氨基; R2是氢，羟基，甲氧基或氨基; R3是氢，羟基，甲氧基，甲氧基甲氧基，氨基，-OCONH2，[2（5H）-3,4-二氢-3-呋喃酮]，2-羟基乙氧基，2-氨基乙氧基，3-羟基丙氧基或3-氨基丙氧基; 或与R2或R4一起亚甲二氧基或亚乙二氧基取代; R4是氢，羟基或氨基; Z是-CH 2 - ， - O-或-NH-; 和a）X1是氢; X2是氢，羟基，氟，氯，溴，碘或甲氧基; X3为氢或羟基; 或b）X 2与X 3一起为亚甲二氧基或亚乙二氧基，并且X 1为氢或其药学上可接受的盐，条件是：i）R 1至R 4中的至少一个不是氢。
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公开(公告)号：US5126351A
公开(公告)日：1992-06-30
申请号：US645373
申请日：1991-01-24
IPC分类号： C07D491/04 , C07D491/056
CPC分类号： C07D491/04
摘要： The present invention relates to the compounds of formula (I), ##STR1## wherein: R.sup.1 is hydrogen, hydroxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or methoxymethoxy;R.sup.3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R.sup.2, methylenedioxy (also known as 1,3-dioxolo);R.sup.4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C.sub.1-4)alkylaminomethyl or, taken together with R.sup.3, methylenedioxy;R.sup.5 is hydrogen or hydroxy; provided that at least one of R.sup.1 through R.sup.5 is other than hydrogen; andi) X.sup.2 is hydroxy or methoxy with X.sup.1, X.sup.3 and X.sup.4 being hydrogen; orii) X.sup.1 taken together with X.sup.2,X.sup.2 taken together with X.sup.3 or X.sup.3 taken together with X.sup.4, is methylenedioxy, provided that each of the remaining respective X.sup.1, X.sup.2, X.sup.3 and X.sup.4 substituents are hydrogen,intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.
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公开(公告)号：US5559235A
公开(公告)日：1996-09-24
申请号：US258136
申请日：1994-06-10
IPC分类号： C07D317/66 , C07D319/18 , C07D491/22 , A61K31/47
CPC分类号： C07D319/18 , C07D317/66
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US20100133272A1
公开(公告)日：2010-06-03
申请号：US12639649
申请日：2009-12-16
申请人： Craig S. Whitaker , Ashish K. Mithal , Matthew J. Wichmann , Michael G. Evans , Van T. Walworth
发明人： Craig S. Whitaker , Ashish K. Mithal , Matthew J. Wichmann , Michael G. Evans , Van T. Walworth
IPC分类号： B65D47/00
CPC分类号： B65D43/0212 , B65D2205/02 , B65D2231/025 , B65D2543/00046 , B65D2543/00092 , B65D2543/00296 , B65D2543/00537 , B65D2543/00638 , B65D2543/00685 , B65D2543/00731 , B65D2543/00796
摘要： A one-piece disposable cup lid enables drinking while inhibiting splashing and spilling by blocking straight-line paths through the lid and dispensing beverage through a well. A drinking spout can include a well having a sidewall, a bottom and a penetration into the cup, or a sloping lid section can intersect a raised rim to create a well therebetween, with a penetration in the sloping section or the rim configured to block straight-line paths, for example by upwardly hinging of a flap or depressing half of a split, convex bubble. Embodiments include baffles that force a beverage to flow through a convoluted path and/or through chambers before being consumed. Baffles can be formed in place, or by hinged movement of flaps after forming. Textures and/or protruding structures can intercept, direct, and/or influence surface tension as beverage flows across surfaces. Vent hole sizes and locations can further limit flow and spilling.
摘要翻译： 一体式一次性杯盖可以通过阻挡直线路径通过盖子并通过井分配饮料来抑制飞溅和溢出而饮用。 饮用水口可以包括具有侧壁，底部和穿入杯子的井，或者倾斜的盖部分可以与凸起边缘相交以在其间形成井，其中倾斜区域或边缘中的穿透被构造成阻挡直线 线路径，例如通过向上铰接翼片或压下分开的凸起气泡的一半。 实施例包括在饮用之前迫使饮料流过回旋路径和/或通过室的挡板。 挡板可以形成在适当的位置，也可以在成形后通过铰链运动。 当饮料流过表面时，纹理和/或突出结构可以拦截，引导和/或影响表面张力。 排气孔尺寸和位置可进一步限制流量和溢出。
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公开(公告)号：US20090293289A1
公开(公告)日：2009-12-03
申请号：US12455322
申请日：2009-06-01
IPC分类号： B26B27/00
CPC分类号： B26B3/02
摘要： 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.
摘要翻译： 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。
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公开(公告)号：US4265597A
公开(公告)日：1981-05-05
申请号：US933639
申请日：1978-08-11
申请人： Harris F. Payne , Michael G. Evans
发明人： Harris F. Payne , Michael G. Evans
CPC分类号： B60H1/00471 , B60H1/00978 , H01H37/76 , H01H85/0241
摘要： A circuit interrupting apparatus and method for a blower having a resistance heater in the air stream of the blower for cooling of the resistance heater and a fuse surrounded by the resistance heater to cause the fuse to blow through heat of the resistance heater when the air stream stops flowing and the amperage of the circuit is not sufficient to blow the main fuse of the system.
摘要翻译： 一种用于鼓风机的电路中断装置和方法，该鼓风机具有用于冷却电阻加热器的鼓风机气流中的电阻加热器和由电阻加热器包围的保险丝，以在空气流中引起熔丝吹过电阻加热器的热量 停止流动，电路的安培数不足以吹动系统的主保险丝。
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公开(公告)号：USD249070S
公开(公告)日：1978-08-22
申请号：US759511
申请日：1977-01-14
申请人： Michael G. Evans
设计人： Michael G. Evans
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公开(公告)号：US6047852A
公开(公告)日：2000-04-11
申请号：US183755
申请日：1998-10-30
CPC分类号： A47G23/0216 , B65D43/0212 , B65D43/169 , B65D51/24 , B65D2543/00046 , B65D2543/00092 , B65D2543/00296 , B65D2543/00351 , B65D2543/00527 , B65D2543/00537 , B65D2543/00685 , B65D2543/00731 , B65D2543/00796
摘要： A hot beverage lid having thermal protective flex-guards or flaps extending from opposite sides of a cover portion of the lid for protecting a consumer's fingers from heat emanating from the side of a cup. A first flap extends a first distance from under a drinking opening having sufficient area for a thumb. A second flap extends a second distance which is greater than the first flap from the opposite side of the lid and has sufficient area for at least two fingers. Each flap is contoured to conform to the curvature or the sidewall of the cup and each flap comprises swirled rib embossing for improved retention against fingers holding the cup. The top of the cover portion is concave with a hole in the center to allow liquid spillage to reenter the cup. Also, a channel surrounding the base of a circular plateau on top of the cover of the lid is provided for collecting fluid spillage.
摘要翻译： 一种热饮料盖，其具有从盖的盖部分的相对侧延伸的热保护性柔性护罩或翼片，用于保护消费者的手指免受从杯侧发散的热量。 第一翼片从具有足够面积的用于拇指的饮水口下方延伸第一距离。 第二挡板从盖的相对侧延伸大于第一翼片的第二距离，并且对于至少两个手指具有足够的面积。 每个翼片的轮廓是符合杯子的曲率或侧壁，每个翼片包括旋转肋压花，以改善保持杯状物的手指。 盖部分的顶部是凹形的，在中心有一个孔，以允许液体溢出重新进入杯子。 此外，围绕盖的盖顶部的圆形平台的底部的通道被设置用于收集流体溢出物。
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