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    • 2. 发明申请
    • SULFONYL HYDRAZINES AS HYPOXIA-SELECTIVE ANTINEOPLASTIC AGENTS
    • SULFONYL HYDRAZINES作为HYPOXIA-选择性抗生素
    • WO2006034266A3
    • 2007-03-01
    • PCT/US2005033641
    • 2005-09-21
    • VION PHARMACEUTICALS INCLIN XUKING IVANBELCOURT MICHAEL FDOYLE TERRENCE W
    • LIN XUKING IVANBELCOURT MICHAEL FDOYLE TERRENCE W
    • A61K31/4196C07D249/08
    • C07F9/65181C07F9/12
    • Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formulas (I), (II), (III) and (IV). Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. Where R = C 1-10 alkyl, or C 1-10 haloalkyl (preferably containing no more than 5 halogen groups, preferably 2-chloroethyl); R' and R" are independently C 1-10 alkyl, or C 5-20 aryl or heteroaryl (preferably methyl); R 1 is H, C 1-10 alkyl, C 1-10 alkoxyl, C 5-20 aryl or heteroaryl or C 5-20 aroxyl or heteroaroxyl (preferably methyl and ethyl); X is O, NH, or NR (preferably O); Y is (CH 2 ) n , where n = 1, 2, 3, 4 or 5 (preferably n = 2 and 3); or Y = aryl or heteroaryl (preferably para-phenyl); A = CH, or N (preferably CH); and B = CH=CH, O, S, NH, or NR (preferably CH=CH); or pharmaceutically acceptable salts, solvates, polymorphs or metabolites, thereof.
    • 具有式(I),(II),(III)和(IV)的磺酰肼的新型含磷前体药物。 要求保护药物组合物及其在治疗癌症中的用途。 前述药物包括对映异构体,立体异构体和互变异构体,以及来自所有阶段的药学上可接受的盐或溶剂合物和代谢物。 上述前药优先在缺氧性肿瘤中活化,并且可以单独给予,也可以与其它抗癌剂或光疗法或放疗相结合。 其中R = C 1-10烷基或C 1-10 1-10卤代烷基(优选含有不超过5个卤素基团,优选2-氯乙基); R'和R“独立地为C 1-10烷基,或C 5-20-20芳基或杂芳基(优选甲基); R 1是 H,C 1-10烷基,C 1-10烷氧基,C 5-20-20芳基或杂芳基或C 5-20 芳基或杂芳基(优选甲基和乙基); X是O,NH或NR(优选O); Y是(CH 2 CH 2)n,其中 n = 1,2,3,4或5(优选n = 2和3);或Y =芳基或杂芳基(优选对苯基); A = CH或N(优选CH);且B = CH = CH ,O,S,NH或NR(优选CH = CH);或其药学上可接受的盐,溶剂合物,多晶型物或代谢物。
    • 3. 发明申请
    • PHOSPHATE-BEARING PRODRUGS OF SULFONYL HYDRAZINES AS HYPOXIA-SELECTIVE ANTINEOPLASTIC AGENTS
    • 磺酸盐酸盐的磷酸盐 - 载体作为羟基选择性抗生素
    • WO2006034266A2
    • 2006-03-30
    • PCT/US2005/033641
    • 2005-09-21
    • VION PHARMACEUTICALS, INC.LIN, XuKING, IvanBELCOURT, Michael, F.DOYLE, Terrence, W.
    • LIN, XuKING, IvanBELCOURT, Michael, F.DOYLE, Terrence, W.
    • A61K31/675C07F9/58C07F9/28
    • C07F9/65181C07F9/12
    • Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formulas (I), (II), (III) and (IV). Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. Where R = C 1-10 alkyl, or C 1-10 haloalkyl (preferably containing no more than 5 halogen groups, preferably 2-chloroethyl); R' and R" are independently C 1-10 alkyl, or C 5-20 aryl or heteroaryl (preferably methyl); R 1 is H, C 1-10 alkyl, C 1-10 alkoxyl, C 5-20 aryl or heteroaryl or C 5-20 aroxyl or heteroaroxyl (preferably methyl and ethyl); X is O, NH, or NR (preferably O); Y is (CH 2 ) n , where n = 1, 2, 3, 4 or 5 (preferably n = 2 and 3); or Y = aryl or heteroaryl (preferably para-phenyl); A = CH, or N (preferably CH); and B = CH=CH, O, S, NH, or NR (preferably CH=CH); or pharmaceutically acceptable salts, solvates, polymorphs or metabolites, thereof.
    • 具有式(I),(II),(III)和(IV)的磺酰肼的新型含磷前体药物。 要求保护药物组合物及其在治疗癌症中的用途。 前述药物包括对映异构体,立体异构体和互变异构体,以及来自所有阶段的药学上可接受的盐或溶剂合物和代谢物。 上述前药优先在缺氧性肿瘤中活化,并且可以单独给予,也可以与其它抗癌剂或光疗法或放疗相结合。 其中R = C
    • 4. 发明申请
    • WATER-SOLUBLE SHPS AS NOVEL ALKYLATING AGENTS
    • 水溶胶作为新型碱性剂
    • WO2005004897A1
    • 2005-01-20
    • PCT/US2004/015547
    • 2004-05-18
    • VION PHARMACEUTICALS, INC.LIN, XuDOYLE, Terrence, W.KING, Ivan
    • LIN, XuDOYLE, Terrence, W.KING, Ivan
    • A61K38/16
    • C07C311/55A61K38/04A61K38/16C07F9/12
    • The present invention relates to compounds according to the structure (I): Where R is -CH 3 or -CH 2 CH 2 CI; R' is C 1 -C 7 alkyl or -CH 2 CH 2 C1; R 2 or R 4 is OPO 3 H 2 , NO 2 , OCO(Glu-OH), NHCO(Glu-OH), NHR 7 and unassigned groups of R 2 , R 3 , R 4 , R 5 and R 6 are, independently, H, F, Cl, Br, I, OH, OPO 3 H 2 , OCH 3 , CF 3 , OCF 3 , NO 2 , CN, SO 2 CH 3 , SO 2 CF 3 , COCH 3 , COOCH 3 , SCH3, SF 5 , NH 2 , NHR 7 , N(CH 3 ) 2 , OP0 3 H 2 , or a C 1 -C 7 alkyl group with the proviso that when any two of unassigned groups of R 2 , R 3 , R 4 , R 5 or R 6 are other than H, the other two of unassigned groups of R 2 , R 3 , R 4 , R 5 or R 6 are H. R 7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.
    • 本发明涉及根据结构(I)的化合物:其中R是-CH 3或-CH 2 CH 2 Cl; R'是C 1 -C 7烷基或-CH 2 CH 2 Cl; R2或R4是OPO3H2,NO2,OCO(Glu-OH),NHCO(Glu-OH),NHR7,R2,R3,R4,R5和R6的未分配基团独立地是H,F,Cl,Br, OH,OPO3H2,OCH3,CF3,OCF3,NO2,CN,SO2CH3,SO2CF3,COCH3,COOCH3,SCH3,SF5,NH2,NHR7,N(CH3)2,OP03H2或C1-C7烷基,条件是当 R2,R3,R4,R5或R6的任何两个未分配的基团不是H,R2,R3,R4,R5或R6的另外两个未分配的基团是H.R 7是H或所述的聚谷氨酰基。 磷酸和谷氨酸可以是游离酸或其药学上可接受的盐。
    • 8. 发明申请
    • REMOTE MONITORING SYSTEM AND METHOD
    • 远程监控系统和方法
    • US20130165074A1
    • 2013-06-27
    • US13434868
    • 2012-03-30
    • ZHONG-LIN XUXIN LUYAO-HUA LIU
    • ZHONG-LIN XUXIN LUYAO-HUA LIU
    • H04W12/08
    • H04L67/08H04L67/025
    • A remote monitoring system includes a network server for communicating with a portable terminal, which sends a request or a remote operation command in response to an user's input. The network server includes a display device, an analyzing unit, a control unit, and a streaming media unit. The analyzing unit receives and analyzes the request to determine a request event. The streaming media unit captures an images of the real time screen of the display device in response to a command generated by the control unit, encodes the captured image, and sends the encoded image to the portable terminal The portable terminal decodes the captured image and displays the decoded image thereon. A related method is also provided.
    • 远程监视系统包括用于与便携式终端通信的网络服务器,其响应于用户的输入发送请求或远程操作命令。 网络服务器包括显示设备,分析单元,控制单元和流媒体单元。 分析单元接收并分析用于确定请求事件的请求。 流媒体单元响应于由控制单元产生的命令捕获显示设备的实时屏幕的图像,对所捕获的图像进行编码,并将编码的图像发送到便携式终端。便携式终端解码所捕获的图像并显示 其上的解码图像。 还提供了相关的方法。
    • 9. 发明授权
    • Process for the manufacture of bridged monobactam intermediates
    • 桥联单体中间体的制备方法
    • US08450477B2
    • 2013-05-28
    • US12676580
    • 2008-09-15
    • Marc MullerXiaoping WuLin Xu
    • Marc MullerXiaoping WuLin Xu
    • C07D487/04C07C271/22C07C269/04
    • C07C271/54C07C271/22C07D487/04
    • A process for manufacturing a compound of Formula (I) which has cis-conformation and wherein R1 represents a 1-phenyl-C1-C4alkyl or 1-naphthyl-C1-C4alkyl group, wherein the phenyl or naphthyl moiety of R1 is unsubstituted or substituted with one or more C1-C4alkoxy groups and the carbon atoms in 2-, 3-, and/or 4-position of the alkyl part of R1 are, independently of the phenyl or naphthyl moiety of R1 and independently of one another, unsubstituted or substituted with C1-C4alkoxy and/or silyloxy or, preferably, are unsubstituted or substituted with one C1-C4alkoxy group and/or silyloxy group per carbon atom, and R2 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, in which process a compound of Formula (II) wherein R3 represents a C1-C6alkyl group or an unsubstituted or substituted benzyl group, and R1 and R2 have the same meaning as in formula (I); is treated with a base at a temperature of 0° C. or less in a liquid aprotic solvent for a time period sufficient to obtain the compound of formula (I).
    • 制备具有顺式构型的式(I)化合物的方法,其中R 1表示1-苯基-C 1 -C 4烷基或1-萘基-C 1 -C 4烷基,其中R 1的苯基或萘基部分是未取代或取代的 与一个或多个C 1 -C 4烷氧基和R 1的烷基部分的2-,3-和/或4-位上的碳原子独立地为R 1的苯基或萘基部分且彼此独立地是未取代的或未取代的 被C1-C4烷氧基和/或甲硅烷氧基取代,或优选未被取代或被每个碳原子一个C 1 -C 4烷氧基和/或甲硅烷氧基取代,并且R 2表示C 1 -C 6烷基或未取代或取代的苄基,其中 处理其中R 3表示C 1 -C 6烷基或未取代或取代的苄基的式(II)化合物,并且R 1和R 2具有与式(I)中相同的含义。 在液体非质子溶剂中在0℃或更低的温度下用碱处理足以获得式(I)化合物的时间段。
    • 10. 发明授权
    • Magnetic stimulation apparatus for central nervous system, circuit and use thereof, and method of using the apparatus
    • 用于中枢神经系统的磁刺激装置,电路及其应用,以及使用该装置的方法
    • US08172742B2
    • 2012-05-08
    • US11917732
    • 2006-06-12
    • Yunfeng ZhengJiang WangLin Xu
    • Yunfeng ZhengJiang WangLin Xu
    • A61N1/00
    • A61N2/006A61N2/02
    • A magnetic stimulation apparatus for central nervous system and circuit thereof, and use of the apparatus and method of using the apparatus are shown. Controlling circuit design and outputting wave form signal to a drive power supply circuit enables the drive power supply circuit to output current of corresponding wave form to coils, and by means of the design of the shape, number of turns, size, interval of the coils, generates within a certain region inside the coils a desired time-variant magnetic field which is then applied to the brain of an animal or a human being so that the central nervous system can receive a wide area synergy magnetic stimulation with a precise wave form, high frequency or a combination of a plurality of frequency components, thus achieving the treatment of nervous and psychiatric diseases or brain function improvement in combination with behavior guidance, thought guidance, or psychological guidance.
    • 示出了用于中枢神经系统的磁刺激装置及其电路,以及使用该装置和使用该装置的方法。 控制电路设计并将波形信号输出到驱动电源电路,使得驱动电源电路能够将相应波形的电流输出到线圈,并且通过形状,匝数,尺寸,线圈间隔的设计 在线圈内的某个区域内产生期望的时变磁场,然后将其施加到动物或人的大脑,使得中枢神经系统可以以精确的波形形式接收广泛的协同磁刺激, 高频率或多个频率分量的组合,从而实现与行为指导,思维指导或心理指导相结合的神经和精神疾病或脑功能改善的治疗。