ХАРТ Чарльз (US),МАТТЕУЧЧИ Марк (US),КУРД Джон (US)
申请号：
RU2013146659/15
公开号：
RU2013146659A
申请日:
2012.03.30
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
1. A method of treating cancer comprising administering a therapeutically effective amount of a compound of formula I: wherein Y2 represents O, S, NR, NCORili NSORRpredstavlyaet a CC-alkyl, CC-heteroalkyl, aryl or heteroaryl r and are independently selected from the group consisting of 2- haloalkyl, alkilsulfoniloksialkila-2, 2-geteroalkilsulfoniloksialkila, 2-arilsulfoniloksialkila and 2- geteroalkilsulfoniloksialkila formula R d LZ L represents C (Z) Znezavisimo each represents hydrogen, halogen, CC-alkyl, CC-heteroalkyl, aryl, heteroaryl, C-Ctsikloalkil, heterocyclyl, CC-acyl, C-Cgeteroatsil, aroyl or heteroaroyl or L is: ,,,,,,, or, Zpredstavlyaet a bioreductive group having a formula selected from the group consisting of:, and Xnezavisimo each represents N or CR X b is NR, S or O each independently represents a CC-alkyl, CC-heteroalkyl, C-Ctsikloalkil, heterocyclyl, aryl or heteroaryl, and independently represents hydrogen, halogen, cyano, CHF, CF, COH, amino , CC-alkyl, CC-heteroalkyl, C-Ctsikloalkil, CC-alkoxy, C-Calkilaminogruppu, C-Cdialkilaminogruppu, aryl, CON (R), CC-acyl, C-Cgeteroa yl, aroyl or heteroaroyl, or a pharmaceutically acceptable salt thereof in combination with a therapeutically effective amount of a pharmacological agent which reduces or inhibits homologous directed DNA repair (HDR) in a patient in need etom.2. A method according to Claim. 1, wherein a pharmacological agent which reduces or inhibits homologous directed DNA repair is represented bortezomib, vorinostat, imatinib, gefitinib or erlotinib.3. A method according to Claim. 1 or 2, wherein the compound of formula I is a TH-302.4. The method claim1. Способ лечения рака, включающий введение терапевтически эффективного количества соединения формулы I:где Y2 представляет собой O, S, NR6, NCOR6 или NSO2R6R6 представляет собой C1-C6-алкил, C1-C6-гетероалкил, арил или гетероарилR3 и R4 независимо выбраны из группы, состоящей из 2-галогеналкила, 2-алкилсульфонилоксиалкила, 2-гетероалкилсуль
