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US 12,747,230 B2Granted
Inhibitors of cysteine proteases and methods of use thereof
AssigneePardes Biosciences, Inc.
InventorsLee D. Arnold, Uri Lopatin, Walter Keung
Life of this patent
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Abstract
The disclosure provides compounds with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.
Claims14
A compound represented by Formula I:
- or a pharmaceutically acceptable salt or stereoisomer thereof, wherein:
- R25 is —C(O)R1,
- R1 is 4-7 membered heterocyclyl, wherein R1 is optionally substituted by one, two or three substituents each selected from Ra,
- R2 is C6-C14aryl, wherein R2 is optionally substituted by one, two or three substituents each selected from R5;
- wherein C6-C14aryl may optionally be fused with one or more carbocyclyl or heterocyclyl groups, and wherein C6-C14aryl designates the number of carbon atoms in the aryl ring system;
- R3 is 5-6 membered monocyclic heteroaryl, wherein the 5-6 membered monocyclic heteroaryl contains at least one ring nitrogen and may have one, two or three optional substituents each selected from Ra;
- R3a is selected from the group consisting of hydrogen and C1-C6alkyl;
- R4 is selected from the group consisting of C3-C10cycloalkyl and C1-C6alkyl-(C6-C14aryl), wherein the C3-C10cycloalkyl is optionally substituted by one, two or three substituents each selected from Ra;
- R4a is hydrogen;
- R5 is independently selected, for each occurrence, from the group consisting of halogen, SF5, C1-C6alkyl, C3-C10cycloalkyl, and C6-C14aryl;
- Ra is independently selected, for each occurrence, from the group consisting of halogen, hydroxyl, cyano, —ORaa, C1-C6alkyl, C1-C6haloalkyl, and C1-C6alkoxy;
- and
- Raa is C1-C6haloalkyl.
10 more elements
A protease inhibitor compound selected from the group consisting of:
- or a pharmaceutically acceptable salt or stereoisomer thereof.
A protease inhibitor compound selected from the group consisting of:
Dependencies are inferred from the claim text.