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US 2022/0064185 A1Published application
Rapamycin derivatives
AssigneeNovartis AG
InventorsSimone Bonazzi, Michael Connolly, David Jonathan Glass, Manuel Mihalic, Andrew W. Patterson, Silvio Roggo, Tea Shavlakadze, Patrik Zueger
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Abstract
The disclosure provides 32-deoxo-rapamycin derivatives of Formula (I), or a pharmaceutically acceptable salt thereof, pharmaceutical compositions and pharmaceutical combinations comprising a compound of Formula (I), and methods of making same. Also provided herein are methods of using a compound of Formula (I) or a pharmaceutically acceptable salt thereof for treating the diseases and disorders described herein.
Claims61
A compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein:
- R1 is selected from the group consisting of —ORa and a 5-6 membered heteroaryl;
- R2 and R3 are each independently selected from the group consisting of H, C1-6alkyl, —ORb, —C0-6alkylene-SO2R4, and —C(O)OR5;
- R4 is —OR5, C1-6alkyl, C1-6haloalkyl, heteroC1-6alkyl, C1-6hydroxyalkyl, C3-8cycloalkylC0-6alkyl;
- R5 is H or C1-6alkyl;
- Ra is selected from the group consisting of H, —P(O)(Rb)2, —C(O)Rc, —C(O)ORc, C1-6alkyl, and C1-6hydroxyalkyl;
- each Rb is independently selected from the group consisting of H and C1-6alkyl;
- and
- each Rc is independently selected from the group consisting of H, C1-6alkyl, and C1-6hydroxyalkyl.
5 more elements
Dependencies are inferred from the claim text.