US 12,281,125 B2
Rapamycin derivatives
Simone Bonazzi, Cambridge, MA (US); Michael Connolly, Salem, MA (US); David Jonathan Glass, Cortland Manor, NY (US); Manuel Mihalic, Grenzach-Wyhle (DE); Andrew W. Patterson, Somerville, MA (US); Silvio Roggo, Muttenz (CH); Tea Shavlakadze, Hawthorne, NY (US); and Patrik Zueger, Basel (CH)
Assigned to NOVARTIS AG, Basel (CH)
Appl. No. 17/414,696
Filed by NOVARTIS AG, Basel (CH)
PCT Filed Dec. 17, 2019, PCT No. PCT/IB2019/060957
§ 371(c)(1), (2) Date Jun. 16, 2021,
PCT Pub. No. WO2020/128861, PCT Pub. Date Jun. 25, 2020.
Claims priority of provisional application 62/781,242, filed on Dec. 18, 2018.
Prior Publication US 2022/0064185 A1, Mar. 3, 2022
Int. Cl. C07D 498/18 (2006.01); A61K 31/436 (2006.01); A61K 45/06 (2006.01)
CPC C07D 498/18 (2013.01) [A61K 31/436 (2013.01); A61K 45/06 (2013.01)] 14 Claims
 
1. A compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein:

OG Complex Work Unit Chemistry
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, C3-8 gscycloalkyl C0-6alkyl;
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.