| 摘要 |
Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II).; |
| 主权项 |
1. A method of treating a cancer or an anemia responsive to activation of human pyruvate kinase M2 (PK-M2) comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula II: wherein: R11 is selected from the group consisting of H, C1-C10 alkyl, OR17, SR17, SOR17, SO2R17, NR17R18, NCOR17, SCOR17, COR17, OCOR17, B(OH)2, NO2, NHCOR17, CN, CHO, hydroxy C1-C10 alkyl, and halogen, R12 is selected from the group consisting of H, methyl, NCOR14, and SO2R14, R13 to R16 are selected from the group consisting of H, C1-C10 alkyl, OR17, SR17, NR17R18, NCOR17, OCOR17, SCOR17, SOR17, SO2R17, SO2NR17R18, CF3, and halogen, and R17 and R18 are independently selected from the group consisting of H and C1-C10 alkyl, or a pharmaceutically acceptable salt thereof, wherein the cancer is selected from the group consisting of renal cancer, ovarian cancer, breast cancer, CNS cancer, leukemia, prostate cancer, non-small cell lung cancer, colon cancer, and melanoma. |
