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US 12,599,672 B2Granted
KRAS proteolysis targeting chimeras
AssigneePAQ Therapeutics Inc.
InventorsNan Ji, Hui Qiu, Ruoxi Lan
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Abstract
Provided herein are KRAS proteolysis targeting chimeras (PROTACs), compositions comprising the KRAS PROTACs, and methods of making and using the KRAS PROTACs, e.g., to promote degradation of KRAS and/or treat KRAS-associated cancers. In an embodiment, the KRAS PROTAC has the following structural formula: or a pharmaceutically acceptable salt thereof, wherein values for the variables are as described herein.
Claims25
A compound of the following formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is
- X1 is N or C(R10);
- R10 is hydrogen, halogen, (C1-C6)alkyl, (C1-C6)haloalkyl, (C1-C6)haloalkoxy, (C2-C6)alkenyl, (C2-C6)alkynyl, —CN, (C1-C6)alkoxy, —S—(C1-C6)alkyl or —S—(C1-C6)haloalkyl;
- R3 is
- R4 is hydrogen or fluoro;
- L′ is
- wherein * indicates point of attachment of L′ to Degron;
- and
- Degron is
- wherein one or more of the hydrogen atoms on the benzene ring of the Degron is optionally replaced with a fluorine atom,
- provided the compound is not
- or a salt thereof.
10 more elements
A compound of the following structure:
- or a pharmaceutically acceptable salt thereof.
A compound selected from:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.