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    Seco precursors of cyclopropylindolines and their use as prodrugs
    2.
    发明授权
    Seco precursors of cyclopropylindolines and their use as prodrugs 失效
    环丙基吲哚啉的山梨醇前体及其作为前药的用途

    公开(公告)号：US06251933B1

    公开(公告)日：2001-06-26

    申请号：US09319771

    申请日：1999-06-11

    Applicant: William Alexander Denny ,  Moana Tercel ,  Graham John Atwell ,  Jared Milbank

    Inventor： William Alexander Denny ,  Moana Tercel ,  Graham John Atwell ,  Jared Milbank

    IPC: A61K31404

    CPC classification number: C07D403/12 ,  C07D209/10 ,  C07D209/12

    Abstract: A compound which is a 6-substituted seco indoline of the formula (I): wherein: X is halogen or OSO2R where R represents H or C1-5 alkyl optionally substituted with from 1 to 4 hydroxyl, acid (COOH) or amino groups which amino may be optionally substituted by one or two C1-5 alkyl groups; Y is N02, N3, NHOH, NHR, NRR, N═NR, N(O)RR, SR or SSR, where R is defined as above, but that in the case where Y is SSR or N═NR, then R can also be another moiety of formula (I); or Y is a group of formula:

    Abstract translation: 化合物，其为式（I）的6-取代的仲二氢吲哚：其中：X为卤素或OSO2R，其中R为H或任选被1至4个羟基，酸（COOH）或氨基取代的C 1-5烷基， 氨基可以任选地被一个或两个C 1-5烷基取代; Y是N 2，N 3，NHOH，NHR，NRR，N = NR，N（O）RR，SR或SSR，其中R如上所定义， 在Y是SSR或N = NR的情况下，R也可以是式（I）的另一部分;或Y是下式的基团：

    Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents
    4.
    发明授权
    Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents 失效
    硝基苄基芥末季盐及其作为缺氧选择性细胞毒性剂的用途

    公开(公告)号：US5872129A

    公开(公告)日：1999-02-16

    申请号：US903937

    申请日：1997-07-31

    Applicant: William Alexander Denny ,  William Robert Wilson ,  Moana Tercel

    Inventor： William Alexander Denny ,  William Robert Wilson ,  Moana Tercel

    IPC: A61K31/14 ,  A61K31/415 ,  A61K47/48 ,  A61P35/00 ,  A61P43/00 ,  C07C209/12 ,  C07C211/63 ,  C07C211/64 ,  C07C217/58 ,  C07C237/30 ,  C07C309/69 ,  C07C317/32 ,  C07C323/32 ,  C07D233/95 ,  A61K31/38 ,  A61K31/40

    CPC classification number: A61K47/48338 ,  C07C211/63 ,  C07C217/58 ,  C07C317/32 ,  C07D233/95

    Abstract: ##STR1## Nitrobenzyl mustard quaternary salts of formula (I), and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR
    1 R
    3 -- or CR
    1 ═CR
    2 -- (where R
    1 and R
    2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO
    2 R; Q is lower alkyl (optionally substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or ether groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO
    2 , SO
    2 R, CONHR, R, OR, SR, CF
    3 and aza (ring --CH-- replared by --N═); with the proviso that when Y=Cl or Br, Q=Me, and X=--CH
    2 -- then Ar≠2-nitrophanyl or 4-nitrophenyl.

    Abstract translation: （I）式（I）的硝基苄基芥末季盐及其药学上可接受的盐，其制备方法及其作为缺氧选择性细胞毒性剂的化学治疗用途。 其中X表示连接基-CR1R3-或CR1 = CR2-（其中R1和R2分别为H，低级烷基，苯基或硝基苯基; Y为卤素或OSO2R; Q为低级烷基（任选被烷基和/或醚取代） 基团并含有最多6个碳原子）或硝基苯基; Ar表示单环或双环芳族单元，R是任选被烷基和/或醚基取代的低级烷基，并且可以含有至多8个碳原子，Z表示一个或多个 NO 2，SO 2 R，CONHR，R，OR，SR，CF 3和氮杂（环-CH-被-N =取代）;条件是当Y = Cl或Br时，Q = Me，X = 然后是Ar NOTEQUAL 2-硝基苯甲酰基或4-硝基苯基。

    Condensed N-aclyindoles as antitumor agents
    6.
    发明授权
    Condensed N-aclyindoles as antitumor agents 失效
    浓缩的N-亚氨基吲哚作为抗肿瘤剂

    公开(公告)号：US6130237A

    公开(公告)日：2000-10-10

    申请号：US266966

    申请日：1999-03-12

    Applicant: William A. Denny ,  Moana Tercel ,  Graham J. Atwell

    Inventor： William A. Denny ,  Moana Tercel ,  Graham J. Atwell

    IPC: C07D209/60 ,  C07D487/04 ,  C07D209/10

    CPC classification number: C07D487/04 ,  C07D209/60

    Abstract: The invention provides compounds of general formula (I), wherein: X is halogen or OSO.sub.2 R, where R represents H or is unsubstituted or hydroxy-or amino-substituted lower alkyl; Y is a nitro or amine group or a substituted derivative thereof; W is selected from the structures of formulae (Ia, Ib or Ic), where E is --N.dbd. or --CH.dbd., G is O, S, or NH, and Q is either up to three of R, OR, NRR, NO.sub.2, CONHR, NHCOR or NHCONHR, or is an additional group of formulae (Ia, Ib or Ic) and HET represents a 5- or 6-membered carbocycle or heterocycle; and A and B collectively represent a fused benzene or 2-CO.sub.2 R pyrrole ring. In one embodiment, the group Y is an amine derivative substituted by a group which is a substrate for a nitroreductase or carboxypeptidase enzyme such that one of said enzymes is able to bring about removal of that group. ##STR1##

    Abstract translation: 本发明提供通式（I）的化合物，其中：X为卤素或OSO 2 R，其中R为H或未取代的或羟基或氨基取代的低级烷基; Y是硝基或胺基或其取代的衍生物; W选自式（Ia，Ib或Ic）的结构，其中E为-N =或-CH =，G为O，S或NH，Q为R，OR，NRR， NO2，CONHR，NHCOR或NHCONHR，或另外一组式（Ia，Ib或Ic），HET表示5-或6-元碳环或杂环; A和B统称为稠合苯或2-CO 2 R吡咯环。 在一个实施方案中，基团Y是被作为硝基还原酶或羧肽酶的底物的基团取代的胺衍生物，使得所述酶之一能够导致该基团的去除。

    Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents
    8.
    发明授权
    Nitrobenzyl mustard quaternary salts and their use as hypoxia-selective cytotoxic agents 失效
    硝基苄基芥末季盐及其作为缺氧选择性细胞毒性剂的用途

    公开(公告)号：US5691371A

    公开(公告)日：1997-11-25

    申请号：US525785

    申请日：1995-09-27

    Applicant: William Alexander Denny ,  William Robert Wilson ,  Moana Tercel

    Inventor： William Alexander Denny ,  William Robert Wilson ,  Moana Tercel

    IPC: A61K31/14 ,  A61K31/415 ,  A61K47/48 ,  A61P35/00 ,  A61P43/00 ,  C07C209/12 ,  C07C211/63 ,  C07C211/64 ,  C07C217/58 ,  C07C237/30 ,  C07C309/69 ,  C07C317/32 ,  C07C323/32 ,  C07D233/95

    CPC classification number: A61K47/48338 ,  C07C211/63 ,  C07C217/58 ,  C07C317/32 ,  C07D233/95

    Abstract: Nitrobenzyl mustard quaternary salts of formula (I), ##STR1## and the pharmaceutically acceptable salts thereof, process for their manufacture and their chemotherapeutic use as hypoxia selective cytotoxic agents. Wherein, X represents a linker chain --CR.sub.1 R.sub.2 -- or CR.sub.1 .dbd.CR.sub.2-- (where R.sub.1 and R.sub.2 are separately H, lower alkyl, phenyl or nitrophenyl; Y is halogen or OSO.sub.2 R; Q is lower alkyl (optionaly substituted with alkyl and/or ether groups and containing up to 6 carbons) or nitrophenyl; Ar represents a mono- or bicyclic aromatic unit, R is lower alkyl optionally substituted with alkyl and/or other groups, and may contain up to eight carbon atoms. Z represents one or more of the groups NO.sub.2, SO.sub.2 R, CONHR, R, OR, SR, CF.sub.3 and aza (ring --CH.dbd.replaced by --N.dbd.); with the proviso that when H-Cl or Br, Q=Me, and X=CH.sub.2 -- then Ar.noteq.2-nitrophenyl or 4-nitrophenyl.

    Abstract translation: PCT No.PCT / NZ94 / 00046 Sec。 371 1995年9月27日第 102（e）1995年9月27日PCT PCT 1994年5月24日PCT公布。 第WO94 / 27954号公报 日期1994年12月8日公式（I）的硝基苄基芥末季盐及其药学上可接受的盐，其制备方法及其作为缺氧选择性细胞毒性剂的化学治疗用途。 其中X表示连接基-CR1R2-或CR1 = CR2-（其中R1和R2分别为H，低级烷基，苯基或硝基苯基; Y为卤素或OSO2R; Q为低级烷基（任选被烷基和/或醚取代） 基团并含有最多6个碳原子）或硝基苯基; Ar表示单环或双环芳族单元，R是任选被烷基和/或其它基团取代的低级烷基，并且可含有至多8个碳原子，Z表示一个或多个 NO 2，SO 2 R，CONHR，R，OR，SR，CF 3和氮杂（环-CH =被-N =取代）;条件是当H-Cl或Br，Q = Me和X = CH 2 Ar注释2-硝基苯基或4-硝基苯基。

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