| 摘要 |
Disclosed herein are radiosensitizer compounds useful in combination with radiation therapy, e.g., a synergistic combination therapy for the treatment of cancer and other disorders. The radiosensitizer compounds have the general formula I: wherein A represents an aromatic core; at least one of Ra and Rb is an electron transfer promoter as defined herein, e.g., NH2; and at least one of Rc is a leaving group as defined herein, e.g., halogen; and the remainder of the molecule is as defined herein. Pharmaceutical compositions, methods, uses, kits and commercial packages comprising the radiosensitizer compounds are also disclosed.; |
| 主权项 |
1. A method of treating cancer in a patient comprising administering to said patient a biocompatible radiosensitizer compound in combination with ionizing radiation, the compound having the general formula I: wherein A is a 5- or 6-membered aryl or heteroaryl ring containing 0-2 ring heteroatoms selected from the group consisting of N, O and S, the remaining ring atoms being carbon, Ra and Rb are, independently, H, OH, alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heterocyclyl, heteroaryl or an electron transfer promoter, wherein at least one of Ra and Rb is an electron transfer promoter; Rc is, independently for each occurrence, H, OH, alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heterocyclyl, heteroaryl, a leaving group, or two adjacent Rc groups taken together with the ring atoms to which they are attached form a 5- or 6-membered saturated, partially saturated or unsaturated ring which contains 0-2 ring heteroatoms selected from N, O and S and which can be optionally substituted with 1-4 Rd; wherein at least one Rc is a leaving group; Rd is independently OH, alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heterocyclyl or heteroaryl; and n=1-4, wherein each of the alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heterocyclyl and heteroaryl moieties is optionally substituted; or a pharmaceutically acceptable salt thereof. |
