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US 11,957,693 B2Granted
Combination MCL-1 inhibitors with anti-cancer agents
AssigneeGilead Sciences, Inc.
InventorsThomas F. Kenney, Clinton K. Matson, Chandrasekar Venkataramani
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Abstract
The present disclosure generally relates to methods of treating cancer by administering an MCL-1 inhibitor and an anticancer agent.
Claims19
A method of treating a TROP-2 expressing cancer comprising:
- administering to a human patient in need a therapeutically effective amount of gemcitabine, and a therapeutically effective amount of an MCL-1 inhibitor;
- wherein the MCL-1 inhibitor is of formula (I):
- or a pharmaceutically acceptable salt thereof;
- wherein R1 is 5-10 membered heteroaryl containing 1-2 heteroatoms;
- wherein each heteroatom is independently selected from nitrogen, sulfur, and oxygen;
- the 5-10 membered heteroaryl of R1 is optionally substituted with 1-3 substituents independently selected from halo, hydroxyl, —CN, C1-6alkyl, C1-6haloalkyl, —ORa, and C3-6cycloalkyl;
- and
- each R2, R3, R4, and R5 is independently hydrogen or C1-6alkyl;
- R6 is hydrogen or halo;
- and
- Ra is independently hydrogen, C1-6alkyl, C2-6alkenyl, and C3-10cycloalkyl.
8 more elements
A method of treating a TROP-2 expressing cancer comprising:
- administering to a human patient in need a therapeutically effective amount of gemcitabine, and a therapeutically effective amount of an MCL-1 inhibitor, wherein the MCL-1 inhibitor is selected from AMG-397, AMG-176, PRT-1419, and S64315.
Dependencies are inferred from the claim text.