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US 2026/0234151 A1Published application
SUBSTITUTED IMIDAZO[1,2-a]QUINAZOLINES AND IMIDAZO[1,2-a]PYRIDO[4,3-e]PYRIMIDINES AS INHIBITORS OF PARG
Assignee858 Therapeutics, Inc.
InventorsJames M. VEAL, Jeffrey A. STAFFORD, Donald S. KARANEWSKY, Shyama HERATH
Life of this patent
Estimating the term…
Abstract
Provided herein are inhibitors of PARG, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the PARG inhibitory compounds for the treatment of disease.
Claims21
-70. (canceled)
A compound, having the structure of Formula 1.7:
- or a salt or stereoisomer thereof, wherein:
- Y is CH, CF, or N;
- R1 is alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), aralkyl, alkyl(heteroaryl), alkenyl, and alkynyl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), the alkyl portion of the aralkyl, the alkyl portion of the alkyl(heteroaryl), alkenyl, or alkynyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the aryl portion of the aralkyl, the heteroaryl portion of the alkyl(heteroaryl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R2 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R3 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R4 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORaC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R5 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- optionally, R2 and R3, taken together with the carbon atom to which they are attached, form an optionally substituted carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORaC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- optionally, R3 and R4, taken together with the carbon atom to which they are attached, form an optionally substituted carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- optionally, R4 and R5, taken together with the carbon atom to which they are attached, form an optionally substituted carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R7 is alkyl, cycloalkyl, or 1,1′-bi(cyclopropan)-1-yl;
- wherein the alkyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- and
- wherein the cycloalkyl or 1,1′-bi(cyclopropan)-1-yl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- each Ra is independently H, D, alkyl, alkyl(cycloalkyl), alkyl(heterocycloalkyl), aralkyl, alkyl(heteroaryl), cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;
- each Rc is independently alkylene or alkenylene;
- and
- each t is independently 1 or 2.
25 more elements
A compound, having the structure of Formula 2.7:
- or a salt or stereoisomer thereof, wherein:
- Y is CH, CF, or N;
- R1 is alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), aralkyl, alkyl(heteroaryl), alkenyl, and alkynyl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), the alkyl portion of the aralkyl, the alkyl portion of the alkyl(heteroaryl), alkenyl, or alkynyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the aryl portion of the aralkyl, the heteroaryl portion of the alkyl(heteroaryl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R2 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R3 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R4 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- R5 is H, halo, CN, alkyl, alkyl(cycloalkyl), alkyl(heterocyclyl), alkenyl, alkynyl, alkynyl(cycloalkyl), OH, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- wherein the alkyl, alkyl portion of the alkyl(cycloalkyl), the alkyl portion of the alkyl(heterocyclyl), alkenyl, alkynyl, or alkynyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- wherein the cycloalkyl portion of the alkyl(cycloalkyl), the heterocyclyl portion of the alkyl(heterocyclyl), the cycloalkyl portion of the alkynyl(cycloalkyl) is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- optionally, R2 and R3, taken together with the carbon atom to which they are attached, form an optionally substituted carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- optionally, R3 and R4, taken together with the carbon atom to which they are attached, form an optionally substituted carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- optionally, R4 and R5, taken together with the carbon atom to which they are attached, form an optionally substituted carbocyclyl or heterocyclyl, wherein the carbocyclyl or heterocyclyl is optionally substituted with one or more substituents independently selected from the group consisting of D, halo, CN, NO2, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, C(O)Ra, C(O)N(Ra)2, C(O)ORa, N(Ra)2, NRaC(O)Ra, NRaC(O)ORa, NRaS(O)tRa, ORa, OC(O)Ra, OC(O)N(Ra)2, OC(O)ORa, ORcC(O)N(Ra)2, ═O, S(O)tRa, S(O)tN(Ra)2, S(O)tORa, ═S, cycloalkyl, heterocycloalkyl, aryl, and heteroaryl;
- each Ra is independently H, D, alkyl, alkyl(cycloalkyl), alkyl(heterocycloalkyl), aralkyl, alkyl(heteroaryl), cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;
- each Rc is independently alkylene or alkenylene;
- and
- each t is independently 1 or 2.
21 more elements
A compound, or a salt or stereoisomer thereof, selected from the group consisting of:
Dependencies are inferred from the claim text.