| 摘要 |
Disclosed are compounds of Formula (I) and/or salts thereof:;;wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer; or as prodrugs of such compounds. |
| 主权项 |
1. A compound of Formula (I): and/or at least one salt thereof, wherein: R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Rx is: —CH2OC(O)CH(CH3)NH2, —CH2OC(O)CH(NH2)CH(CH3)2, —CH2OC(O)CH((CH(CH3)2)NHC(O)CH(NH2)CH(CH3)2, Ry is: —SCH2CH(NH2)C(O)OH, —SCH2CH(NH2)C(O)OCH3, or —SCH2CH(NH2)C(O)OC(CH3)3; Ring A is phenyl or pyridinyl; each Ra is independently Cl, C1-3 alkyl, —CH2OH, —CF3, cyclopropyl, —OCH3, and/or —O(cyclopropyl); y is zero, 1, or 2; and z is zero, 1, r 2; provided that if Ring A is phenyl, then y is 1 or 2 and at least one Ra is C1-3 alkyl, —CH2OH, —CF3, cyclopropyl, or —O(cyclopropyl); provided that if R3 is Rx then R4 is H; and provided that if R4 is Ry then R3 is H or —CH3. |
