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    Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents
    3.
    发明申请
    Phosphate-bearing prodrugs of sulfonyl hydrazines as hypoxia-selective antineoplastic agents 有权
    含磺酸肼的含磷前体作为缺氧选择性抗肿瘤药

    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。

    Magnetic resonance imaging scanner with molded fixed shims
    4.
    发明申请
    Magnetic resonance imaging scanner with molded fixed shims 有权
    具有模制固定垫片的磁共振成像扫描仪

    公开(公告)号：US20070030004A1

    公开(公告)日：2007-02-08

    申请号：US10558768

    申请日：2004-05-19

    Applicant: William Amor ,  Dennis Everett ,  Jerome Alden ,  Robert Henderson ,  Terrence Doyle ,  Ronald Sharpless ,  Gerardus Mulder ,  Gerardus Peeren

    Inventor： William Amor ,  Dennis Everett ,  Jerome Alden ,  Robert Henderson ,  Terrence Doyle ,  Ronald Sharpless ,  Gerardus Mulder ,  Gerardus Peeren

    IPC: G01V3/00

    CPC classification number: G01R33/3873

    Abstract: A magnetic resonance imaging scanner includes a generally cylindrical main magnet assembly (10) that defines a cylinder axis (16). A first set of shims (60) are rigidly positioned inside the magnet assembly (10) at about a first distance (d1) relative to the cylinder axis (16). A second set of shims (62) are rigidly positioned inside the main magnet assembly (10) at about a second distance (d2) relative to the cylinder axis (16). The second distance (d2) is different from the first distance (d1). A generally cylindrical radio frequency coil (26) is arranged inside the main magnet assembly (10) at about a third distance (d3) relative to the cylinder axis (16). A plurality of gradient coils (20) are arranged inside the main magnet assembly (10) at about a fourth distance (d4) relative to the cylinder axis (16).

    Abstract translation: 磁共振成像扫描仪包括限定气缸轴线（16）的大致圆柱形的主磁体组件（10）。 第一组垫片（60）相对于气缸轴线（16）以大约第一距离（d 1）刚性地定位在磁体组件（10）的内部。 第二组垫片（62）相对于气缸轴线（16）以大约第二距离（d 2）刚性地定位在主磁体组件（10）的内部。 第二距离（d 2）与第一距离（d 1）不同。 大致圆柱形的射频线圈（26）相对于气缸轴线（16）以大约第三距离（d 3）布置在主磁体组件（10）的内部。 多个梯度线圈（20）相对于气缸轴线（16）以大约第四距离（d 4）布置在主磁体组件（10）的内部。

    Water-soluble SHPs as novel alkylating agents
    6.
    发明申请
    Water-soluble SHPs as novel alkylating agents 审中-公开
    水溶性SHP作为新型烷基化剂

    公开(公告)号：US20050043244A1

    公开(公告)日：2005-02-24

    申请号：US10950890

    申请日：2004-09-27

    Applicant: Xu Lin ,  Terrence Doyle ,  Ivan King

    Inventor： Xu Lin ,  Terrence Doyle ,  Ivan King

    IPC: A61K38/04 ,  A61K38/16 ,  C07C311/55 ,  C07F9/12 ,  A61K31/175 ,  A61K31/195 ,  A61K31/277 ,  A61K38/05 ,  A61K38/06 ,  A61K38/08 ,  A61K38/10

    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 OP03H2, N02, 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, OP03H2, OCH3, CF3, OCF3, NO2, CN, SO2CH3, SO2CF3, COCH3, COOCH3, SCH3, SFs, 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OP03H2，N02，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，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，SCH 3，SF，NH 2，NHR 7，N（CH 3）2，OPO 3 H 2或C 1 -C 7烷基， 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。

    Benzoate derivatives of taxol
    7.
    依法登记的发明
    Benzoate derivatives of taxol 失效
    紫杉醇的苯甲酸衍生物

    公开(公告)号：USH1487H

    公开(公告)日：1995-09-05

    申请号：US128949

    申请日：1993-09-29

    Applicant: Henry Wong ,  Terrence Doyle

    Inventor： Henry Wong ,  Terrence Doyle

    IPC: A61K31/335 ,  A61K31/337 ,  A61P35/00 ,  C07D305/14 ,  C07F9/655 ,  C07F9/6558 ,  C07D413/00

    CPC classification number: C07D305/14 ,  C07F9/65512 ,  C07F9/65586

    Abstract: This invention relates to a compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.2 is a radical of the formula ##STR2## in which R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl, said C.sub.1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C.sub.1-6 alkyl) amino; or NR.sup.a R.sup.b together represents a radical of the formula ##STR3## in which y is one to three, and R.sup.a is as defined above; R.sup.p and R.sup.r are independently same or different C.sub.1-6 alkyl;R.sup.1 is hydrogen or a radical Z of the formula ##STR4## in which Q is --(CH.sub.2).sub.f --, optionally substituted with one to six same or different C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, or a carbon atom of said --(CH.sub.2).sub.f -- radical may also be a part of C.sub.3-6 cycloalkylidene;R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl, or R.sup.3 and R.sup.4 taken together with the carbon atom to which they are attached form C.sub.3-6 cycloalkylidene;R.sup.5 is --OC(.dbd.O)R, --OP.dbd.O(OH).sub.2 or --CH.sub.2 OP.dbd.O(OH).sub.2, in which R is C.sub.1-6 alkyl;R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or hydrogen, but when R.sup.5 is --OC(.dbd.O)R, one of R.sup.6, R.sup.7, R.sup.8 or R.sup.9 is --OP.dbd.O(OH).sub.2 ;f is 2 to 6;n is O, and m is 1 or 0 when R.sup.5 is --CH.sub.2 OP.dbd.O(OH).sub.2 ;and n is 1 or 0, and m is 1 when R.sup.5 is --OC(.dbd.O)R or --OP.dbd.O(OH).sub.2.Also provided by this invention are pharmaceutical formulations and a method for treating mammalian tumors with a compound of formula I.

    Abstract translation: 本发明涉及式Ⅰ的化合物其中R 2是下式的基团，其中R a和R b独立地是氢或C 1-6烷基，所述C 1-6烷基任选被取代 与羟基，膦酰基，膦酰氧基，羧基或二（C 1-6烷基）氨基; 或NRaRb一起表​​示如上所定义的式 的基团; Rp和Rr独立地相同或不同的C1-6烷基; R1是氢或具有一至六个相同或不同的C 1-6烷基或C 3-6环烷基或所述 - （CH 2）f - 基团的碳原子的式“IMAGE”或“IMAGE”的基团Z也可以是 部分C3-6亚环烷基; R 3和R 4独立地为氢或C 1-6烷基，或者R 3和R 4与它们所连接的碳原子一起形成C 3-6亚环烷基; R5是-OC（= O）R，-OP = O（OH）2或-CH2OP = O（OH）2，其中R是C1-6烷基; R6，R7，R8和R9独立地是卤素，C1-6烷基，C1-6烷氧基或氢，但当R5是-OC（= O）R时，R6，R7，R8或R9之一是-OP = O（ OH）2; f为2〜6; 当R 5为-CH 2 OP = O（OH）2时，n为O，m为1或0; 当R 5为-OC（= O）R或-OP = O（OH）2时，n为1或0，m为1。 本发明还提供药物制剂和用式I化合物治疗哺乳动物肿瘤的方法。

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