ОССОВСКАЯ Валерия С. (US),БРЭДЛИ Чарльз (US),ШЕРМАН Барри М. (US)
申请号：
RU2010128107/15
公开号：
RU2010128107A
申请日:
2008.12.05
申请国别(地区):
RU
年份:
2012
代理人:
摘要：
1. A method of treating cancer, comprising administering to the patient an effective amount of a topoisomerase inhibitor in combination with one PARP inhibitor of formula (Ia):! ! where R1, R2, R3, R4 and R5 are independently selected from the group consisting of hydrogen, hydroxy, amino, nitro, iodine, bromine, fluorine, chlorine, (C1-C6) alkyl, (C1-C6) alkoxy, (C3-C7 ) cycloalkyl and phenyl, wherein at least two of the five substituents R1, R2, R3, R4 and R5 are always hydrogen, at least one of the five substituents is always nitro and at least one substituent next to nitro is always iodine, as well as pharmaceutically acceptable salts, solvates, isomers, tautomers, metabolites, analogs or their prodrugs! where the cancer does not include breast cancer, uterine cancer or ovarian cancer. ! 2. The method according to claim 1, in which the PARP inhibitor has the formula:! ! 3. The method according to claim 1, wherein a 4-iodo-3-nitrobenzamide metabolite selected from the group consisting of:! ! ! R6 is selected from the group consisting of hydrogen, (C1-C8) alkyl, (C1-C8) alkoxy, isoquinolines, indoles, thiazole, oxazole, oxadiazole, thiophene or phenyl. ! ! ! ! and! ! 4. The method according to claim 1, in which the topoismerase inhibitor is topotecan, irinotecan, lurtotecan, exatecan or its pharmaceutically acceptable salt or metabolite. ! 5. The method according to claim 1, wherein the topoismerase inhibitor is topotecan or a pharmaceutically acceptable salt or metabolite thereof. ! 6. The method according to claim 1, in which the cancer is selected from the group consisting of cancer of the adrenal cortex, cancer of the anal canal, aplastic anemia, cancer of the bile ducts, cancer of the bladder, bone cancer, bone metastases, CNS tumors, peripheral CNS cancer Castle disease1. Способ лечения рака, предусматривающий введение пациенту эффективного количества ингибитора топоизомеразы в комбинации с одним ингибитором PARP формулы (Ia): ! ! где R1, R2, R3, R4 и R5
