公开(公告)号：US20060089332A1

公开(公告)日：2006-04-27

申请号：US11232252

申请日：2005-09-21

Applicant: Xu Lin ,  Ivan King ,  Michael Belcourt ,  Terrence Doyle

Inventor： Xu Lin ,  Ivan King ,  Michael Belcourt ,  Terrence Doyle

IPC: A61K31/675 ,  C07F9/58 ,  C07F9/28

CPC classification number: C07F9/12 ,  C07F9/6518

Abstract: 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=C1-10 alkyl, or C1-10 haloalkyl (preferably containing no more than 5 halogen groups, preferably 2-chloroethyl); R′ and R″ are independently C1-10 alkyl, or C5-20 aryl or heteroaryl (preferably methyl); R1 is H, C1-10 alkyl, C1-10 alkoxyl, C5-20 aryl or heteroaryl or C5-20 aroxyl or heteroaroxyl (preferably methyl and ethyl); X is O, NH, or NR (preferably O); Y is (CH2)n, O(CH2)n, NH(CH2)n, NR(CH2)n, OCOO(CH2)n, NHCOO(CH2)n; n is 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.

Abstract translation: 磺酰肼的新型含磷酸酯前药具有式I，II，III和IV。 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（CH 2）n，O（CH 2）n，NH（CH 2） NR（CH 2）n，OCOO（CH 2）2，N（CH 2）n， nCO 2，NHCOO（CH 2 CH 2）n N; n为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）; 和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。

公开(公告)号：US06855695B2

公开(公告)日：2005-02-15

申请号：US10461282

申请日：2003-06-13

Applicant: Xu Lin ,  Terrence W. Doyle ,  Ivan King

Inventor： Xu Lin ,  Terrence W. Doyle ,  Ivan King

IPC: A61K38/04 ,  A61K38/16 ,  C07C311/55 ,  C07F9/12 ,  A61K38/00

CPC classification number: C07C311/55 ,  A61K38/04 ,  A61K38/16 ,  C07F9/12

Abstract: The present invention relates to compounds according to the structure (I): Where R is —CH3 or —CH2CH2Cl; R′ is C1-C7 alkyl or —CH2CH2Cl; R2 or R4 is OPO3H2, NO2, OCO(Glu-OH), NHCO(Glu-OH), NHR7 and unassigned groups of R2, R3, R4, R5 and R6 are, independently H, F, Cl, Br, I, OH, OPO3H2, OCH3, CF3, OCF3, NO2, CN, SO2CH3, SO2CF3, COCH3, COOCH3, SCH3, SF5, NH2, NHR7, N(CH3)2, OPO3H2, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R2, R3, R4, R5 or R6 are other than H, the other two of unassigned groups of R2, R3, R4, R5 or R6 are H. R7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

Abstract translation: 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，I，OH ，OPO3H2，OCH3，CF3，OCF3，NO2，CN，SO2CH3，SO2CF3，COCH3，COOCH3，SCH3，SF5，NH2，NHR7，N（CH3）2，OPO3H2或C1-C7烷基，条件是当任何 R2，R3，R4，R5或R6中的两个未分配的基团不是H，R2，R3，R4，R5或R6的其他两个未分配的基团是H.R 7是H或如所述的聚谷氨酰基。 磷酸和谷氨酸可以是游离酸或其药学上可接受的盐。

公开(公告)号：US20090075945A1

公开(公告)日：2009-03-19

申请号：US12080357

申请日：2008-04-02

Applicant: Xu Lin ,  Ivan King ,  Michael F. Belcourt ,  Terrence W. Doyle

Inventor： Xu Lin ,  Ivan King ,  Michael F. Belcourt ,  Terrence W. Doyle

IPC: A61K31/662 ,  A61P35/00

CPC classification number: C07F9/12 ,  C07F9/6518

Abstract: Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Methods of 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 is C1-C10 alkyl or haloalkyl; R′ and R″ are each independently C1-C10 alkyl; and R1 is C1-C10 alkyl, or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.

Abstract translation: 磺酰肼的新型含磷前体药物具有以下公式。 要求治疗癌症的方法。 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是C 1 -C 10烷基或卤代烷基; R'和R“各自独立地为C 1 -C 10烷基; 并且R 1是C 1 -C 10烷基，或其药学上可接受的盐，溶剂合物，多晶型物或代谢物。

公开(公告)号：US07405317B2

公开(公告)日：2008-07-29

申请号：US11232252

申请日：2005-09-21

Applicant: Xu Lin ,  Ivan King ,  Michael F. Belcourt ,  Terrence W. Doyle

Inventor： Xu Lin ,  Ivan King ,  Michael F. Belcourt ,  Terrence W. Doyle

IPC: C07F9/22 ,  C07C313/04 ,  C07C313/06

CPC classification number: C07F9/12 ,  C07F9/6518

Abstract: Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. 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 is C1-C10 alkyl or haloalkyl; R′ and R″ are each independently C1-C10 alkyl; R1 is CH3; and X is O; or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.

Abstract translation: 磺酰肼的新型含磷前体药物具有以下公式。 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是C 1 -C 10烷基或卤代烷基; R'和R“各自独立地为C 1 -C 10烷基; R 1是CH 3 3; X为O; 或其药学上可接受的盐，溶剂化物，多晶型物或代谢物。

公开(公告)号：US20050198680A1

公开(公告)日：2005-09-08

申请号：US11098787

申请日：2005-04-05

Applicant: Paul Baran ,  Xu Lin ,  John Pickens ,  Michael Field

Inventor： Paul Baran ,  Xu Lin ,  John Pickens ,  Michael Field

IPC: H04L29/06 ,  H04N7/173 ,  H05K1/02 ,  H05K1/14 ,  H05K1/18 ,  H04N7/20

CPC classification number: H04L63/068 ,  H04L29/06027 ,  H04L63/10 ,  H04L65/4084 ,  H04N7/17318 ,  H04N21/2318 ,  H04N21/2326 ,  H04N21/23406 ,  H04N21/2347 ,  H04N21/2362 ,  H04N21/2365 ,  H04N21/26606 ,  H04N21/4347 ,  H04N21/47202 ,  H04N21/6405 ,  H04N21/6587 ,  H05K1/0275 ,  H05K1/144 ,  H05K1/185 ,  H05K2201/10151

Abstract: A conditional access method and apparatus for use with a system for controlling of digital TV program start time. Subscriber access is authorized to digital program streams. Content are divided into a plurality of working periods. Each working period of the plurality of working periods is scrambled with a different working key. A working key of a given period is delivered ahead of the given period. The working key is synchronized with scrambling control bits in an header working keys are inserted into an entitlement control message (ECM) packet, and the ECM packet is encrypted using a service key. A time period is inserted into the ECM packet during which the service key is valid. A service key is inserted in an entitlement.

Abstract translation: 一种用于控制数字电视节目开始时间的系统的条件访问方法和装置。 用户接入被授权给数字节目流。 内容分为多个工作时段。 多个工作周期的每个工作周期用不同的工作密钥加扰。 给定期间的工作密钥在给定期限之前交付。 工作密钥与报头中的加扰控制位同步工作密钥插入到授权控制消息（ECM）分组中，并且使用服务密钥对ECM分组进行加密。 一个时间段被插入ECM包中，其中服务密钥是有效的。 一个服务密钥插入一个权利。

公开(公告)号：US20050039212A1

公开(公告)日：2005-02-17

申请号：US10911736

申请日：2004-08-04

Applicant: Paul Baran ,  Xu Lin ,  John Pickens ,  Michael Field

Inventor： Paul Baran ,  Xu Lin ,  John Pickens ,  Michael Field

IPC: H04L29/06 ,  H04N7/173 ,  H05K1/02 ,  H05K1/14 ,  H05K1/18 ,  H04N7/18

CPC classification number: H04L63/068 ,  H04L29/06027 ,  H04L63/10 ,  H04L65/4084 ,  H04N7/17318 ,  H04N21/2318 ,  H04N21/2326 ,  H04N21/23406 ,  H04N21/2347 ,  H04N21/2362 ,  H04N21/2365 ,  H04N21/26606 ,  H04N21/4347 ,  H04N21/47202 ,  H04N21/6405 ,  H04N21/6587 ,  H05K1/0275 ,  H05K1/144 ,  H05K1/185 ,  H05K2201/10151

Abstract: A construction arrangement for a small set-top box to protect cryptographic capabilities and prevent a digital program in clear from being able to be tapped as required by Digital Rights Management protocols. A first layer of sheet metal capable of blocking X-rays, is formed as a shallow pan to hold a set of printed circuit boards. A second layer has a thin epoxy based printed circuit material. A third layer has a printed circuit board with integrated components placed on top of the second layer. A fourth layer has a three layer thin printed circuit board with a first and second metallic layer and holes for large components, such as electrolytic capacitors. A black liquid thermosetting epoxy fills the interstices between the sheet metal layer and the second layer, and between the second layer and the third layer, and between the third layer and the fourth layer, thereby preventing access to exposed circuit trace carrying digital signals in the clear. A connection from the first metallic layer of the fourth printed circuit material layer to a sending circuit and a connection from the second metallic layer so that a short between these two layers sets off an indicator circuit that an attempt is made to enter the protected area.

Abstract translation: 一种小型机顶盒的构造安排，用于保护加密功能，并防止数字程序清楚地被数字版权管理协议所要求的。 能够阻挡X射线的第一层金属片被形成为浅盘以保持一组印刷电路板。 第二层具有薄的环氧基印刷电路材料。 第三层具有布置在第二层顶部的集成元件的印刷电路板。 第四层具有三层薄印刷电路板，其具有第一和第二金属层以及诸如电解电容器的大部件的孔。 黑色液体热固性环氧树脂填充金属片层与第二层之间的间隙，以及第二层与第三层之间以及第三层与第四层之间的间隙，从而防止在载体中承载数字信号的裸露电路迹线 明确。 从第四印刷电路材料层的第一金属层到发送电路的连接以及来自第二金属层的连接，使得这两层之间的短路使得指示电路成为尝试进入保护区域的指示电路。