摘要 |
Provided are methods for treating cancer in a patient, comprising administering to a patient in need thereof a therapeutically effective regimen, the regimen comprising administering a gamma-secretase inhibitor, wherein the regimen results in a reduction in the cancer cell population in the patient. In some embodiments of the methods, the therapeutically effective regimen stabilizes, reduces or eliminates the cancer stem cell population.;Also provided are compounds of the formula I;;or a pharmaceutically acceptable salt thereof, wherein R1, R2, and X are as herein described. |
主权项 |
1. A method of treating cancer in a human patient, comprising administering to a human patient in need thereof a therapeutically effective amount of a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein:
X is halo;R1 is hydrogen, halogen, hydroxy, C1-6alkyl, or C1-4alkoxy;R2 is a radical of the following structure: wherein:
E is CH2 or NH;D is (CH2)m, O(CH2)m, HN(CH2)n, or CH═CH;
wherein m is 0, 1 or 2;A and Q are independently N, NCH3 or C;M is C or C═O;n is 1 or 2;Z1 and Z2 are independently H, halo, halo(C1-4)alkyl, phenyl, or
Z1 and Z2, when attached to carbon atoms, form a 6-membered aryl ring with the carbon atoms to which they are attached; andZ3 is H, halo, halo(C1-4)alkyl, or phenyl. |