| 摘要 |
This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazole boronic acid compounds for treating cancer. |
| 主权项 |
1. A compound of formula (I): wherein R2 is selected from H, —NHRa, alkoxy, halogen, —CF3, —CHF2, and C1-6alkyl; R3 is selected from aryl and heteroaryl, wherein said aryl or heteroaryl may be substituted by one to three Rc; R4 is selected from H or Ra; each R5 is independently selected from C1-6alkyl; each Ra is independently selected from C1-3alkyl; each Rc is independently selected from C1-3alkyl, halogen, —CF3, and hydroxy; and n is 0-2, or a pharmaceutically acceptable salt thereof. |
