Back to results
US 12,473,296 B2Granted
Perk inhibiting compounds
AssigneeHiberCell, Inc.
InventorsMark J. Mulvihill, An-Hu Li, Matthew David Surman
Life of this patent
Estimating the term…
Abstract
Provided herein are compounds, compositions, and methods useful for inhibiting PERK and for treating related conditions, diseases, and disorders. PERK-inhibiting compounds of Formula (I) having the following structure: are described herein. Also described herein are pharmaceutical compositions containing a compound of Formula (I) in one or more pharmaceutically acceptable carriers, diluents, or excipients, as well as methods for inhibiting a PERK enzyme in a patient or treating cancer in a patient.
Claims28
A compound of the formula (I):
- wherein:
- Ar1 is aryl, heteroaryl, or cycloalkyl, optionally substituted by one or more independent R1 substituents;
- Ar2 is aryl or heteroaryl, optionally substituted by one or more independent R2 substituents;
- Y is C(R3a)(R3b)C0-6alkyl, NR3a, —O—, C(O), CF2, CNOR3bb, or a direct bond to Ar1;
- R3a is H, alkyl, or cycloalkyl;
- R3b is H, alkyl, OR3c, or NR3dR3e;
- R3bb is H or alkyl;
- R4 is H, alkyl, or OH;
- X is CR7 or N;
- R1 is one or more independent H, deuterium, halo, CN, NO2, alkyl, cycloalkyl, C0-6alkyl-O—C1-12alkyl, C0-6alkyl-OH, C0-6alkyl-O—C3-12cycloalkyl, or C0-6alkyl-O—C3-12heterocycloalkyl, optionally substituted by one or more independent G1 substituents;
- R2 is one or more independent H, deuterium, halo, CN, NO2, alkyl, C0-6alkylcycloalkyl, C0-6alkyl-O—C1-12alkyl, C0-6alkyl-OH, or C0-6alkyl-O—C3-12cycloalkyl, optionally substituted by one or more independent G2 substituents;
- R3c, R3d and R3e are each independently H, alkyl, or cycloalkyl, optionally substituted by one or more independent G3 substituents;
- R5 is H, CH3, NHR9, or OR9;
- R6 is selected from the group consisting of:
- R7 is H, CN, or alkyl, optionally substituted by one or more independent deuterium or halo;
- R8a and R8b are each independently H, C1-12alkyl, C0-12alkyl-C3-12cycloalkyl, or C0-12alkyl-C3-12heterocycloalkyl, optionally substituted by one or more independent G4 substituents;
- or
- R8a and R8b taken together with the nitrogen to which they are attached form 5-10 membered heterocyclyl;
- R9 is H, alkyl, cycloalkyl, or heterocycloalkyl;
- G1, G2, G3, or G4 are each independently H, deuterium, halo, CN, NO2, C1-12alkyl, C0-12alkyl-C3-12cycloalkyl, C0-12alkyl-C3-12heterocycloalkyl, OR10, NR10R11, C(O)R10, C(O)OR10, C(O)NR10R11, OC(O)R10, OC(O)OR10, OC(O)NR10R11, N(R12)C(O)R10, N(R12)C(O)OR10, N(R12)C(O)NR10R11, S(O)nR10, S(O)nOR10, S(O)nNR10R11, N(R12)S(O)nR10, N(R12)S(O)nOR10, or N(R12)S(O)nNR10R11, optionally substituted by one or more independent H, deuterium, halo, OH, CN, or NO2;
- R10, R11, or R12 are each independently selected from H, deuterium, halo, CN, NO2, alkyl, cycloalkyl or heterocycloalkyl, optionally substituted by one or more independent H, deuterium, halo, OH, CN, or NO2;
- n is 0, 1, or 2;
- or a pharmaceutically acceptable salt thereof.
20 more elements
Dependencies are inferred from the claim text.