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    1,2,4-BENZOTRIAZINE OXIDES AS RADIOSENSITIZERS AND SELECTIVE CYTOTOXIC AGENTS
    6.
    发明专利
    1,2,4-BENZOTRIAZINE OXIDES AS RADIOSENSITIZERS AND SELECTIVE CYTOTOXIC AGENTS 未知

    公开(公告)号：CA2001903A1

    公开(公告)日：1991-04-30

    申请号：CA2001903

    申请日：1989-10-31

    Applicant: STANFORD RES INST INT

    Inventor： LEE WILLIAM W ,  BROWN MARTIN J ,  GRANGE EDWARD W ,  MARTINEZ ABELARDO P ,  TRACY MICHAEL ,  POLLART DANIEL J

    IPC: A61K31/53 ,  C07D253/10 ,  C07D403/02

    Abstract: A method of using 1,2,4-benzotriazine oxides, some of which are novel compounds, as radiosensitizers and selective cytotoxic agents is disclosed. These compounds are shown to specifically radiosensitize hypoxic tumor cells. Some are additionally disclosed to be useful as specific cytotoxic agents for these cells. They also show an unexpected ability to radiosensitize aerobic cells following or preceding a hypoxic incubation of the cells with the drug. This provides a basis for selective radiosensitization of tumors compared to normal cells. Novel compounds of a novel method for preparing the 1,2,4- benzotriazine oxides is also disclosed. Novel compounds of the formula wherein X is OH, alkoxy (1-4C), NHR or NRR where each R is independently an alkyl of 1-4 carbon atoms, or aryl of 1-4 carbon atoms, or where the two R groups are alkyls linked together to form a pyrrolidino or piperidino ring or linked through an oxygen to form a morpholino ring, and the R groups may be further substituted with OH, NH2, alkyl (1-4C) secondary amino, dialkyl (1-4C) tertiary amino, pyrrolidino, piperidino, alkoxy (1-4C), or halogen substitutents; n is 1; and Y1 is H and Y2 is nitro; or a pharmacologically acceptable salt thereof are also disclosed. A novel method for preparing the 1,2,4-benzotriazine oxides is also disclosed.

    1,2,4-Benzotriazine oxide derivs. - used for radio-sensitising hypoxic tumour cells and selectively killing hypoxic tumour cells
    9.
    发明专利
    1,2,4-Benzotriazine oxide derivs. - used for radio-sensitising hypoxic tumour cells and selectively killing hypoxic tumour cells 未知

    公开(公告)号：DE3745196B4

    公开(公告)日：2005-12-08

    申请号：DE3745196

    申请日：1987-06-16

    Applicant: STANFORD RES INST INT

    Inventor： LEE WILLIAM W ,  BROWN J MARTIN ,  GRANGE EDWARD W ,  MARTINEZ ABELARDO P

    IPC: A61K31/04 ,  A61K31/53 ,  C07D253/08 ,  C07D405/12

    Abstract: Method of radiosensitising hypoxic tumour cells comprises administering a 1,2,4-benzotriazine oide deriv. of formula (I) where X = OH, OR, NH2, NR or NR2; each R = 1-4C alkyl or morpholino and may further be substd. with OH, alkoxy, amino or halogeno; n = 0 or 1; Y1, Y2 = halogeno, hydrocarbyl (1-14C) including cyclic and unsatd. hydrocarbyl, opt. substd. with 1 or 2 substits. selected from halogeno, OH, epoxy, alkoxy, alkylthio, amino (including morpholino), acyloxy, acylamido and their thio analogues, carboxy, alkoxycarbonyl, carbamoyl or alkylcarbamyl and where the hydrocarbyl can opt. be interrupted by a single ether (-O-) linkage or Y1 and Y2 are NHR1, O(CO)R1, NH(CO)R1, O(SO)R1 or O(POR1)R1; R1 = a hydrocarbyl opt. substd. as before. Also claimed is a method of selectively killing hypoxic tumour cells comprising administering directly to the cells (I), where X = NH2, NHR or NR2 and n is 1 and R may also be amide, and Y1, Y2 may also be H. (C) Also claimed are cpds. (I) where (a) X is OH, OR or NR2 and n is 0 or 1, Y1, Y2 may also be H; (b) X is NH2 or NHR and n is 0, Y1, Y2 may also be H. (c) X is NH2, n is 1 and Y1 and Y2 are H, satd. or unsatd. hydrocarbyl or 7-14C or unsatd. hydrocarbyl of 1-6C either hydrocarbyl being unsubstd. or substd. with halogen, OH, epoxy, alkoxy, alkylthio, amino, morpholino, acyloxy, acylamido and their thio analogues and where the hydrocarbyl can be opt. interrupted by a single ether linkage or Y1 and Y2 are NHR1, O(CO)R1, NH(CO)R1, O(SO)R1 or O(POR1)R1.

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