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US 12,509,436 B2Granted
Benzamide derivatives as cGAS-sting pathway agonists
AssigneeBaruch S. Blumberg Institute
InventorsJinhong Chang, Yanming Du, Ju-Tao Guo
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Abstract
Pharmaceutical compositions of the invention comprise functionalized benzamide derivatives useful as cyclic GMP-AMP synthase-Stimulator of interferon gene (cGAS-STING) pathway agonists, and useful for treating viral diseases and boost antitumor immunity.
Claims10
A compound having formula (II):
- or a hydrate, solvate, pharmaceutically acceptable salt, prodrug or complex thereof, wherein:
- R1 is selected from a group consisting of hydrogen, halogen, optionally substituted C1-6 haloalkyl, optionally substituted C1-6 alkenyl, CO2R7, CONHR8, NHR9, NR9R10, OR10, cyano, N3, SO2R11, optionally substituted phenyl, optionally substituted heteroaryl, and N-containing monocyclic heterocycloalkyl;
- R3 is selected from a group consisting of hydrogen, halogen, optionally substituted C1-6 haloalkyl, optionally substituted C1-6 alkenyl, CO2R7, CONHR8, NHR9, NR9R10, OR10, cyano, N3, SO2R11, optionally substituted phenyl, optionally substituted heteroaryl, and N-containing monocyclic heterocycloalkyl;
- n is 1;
- R4 and R5 are taken together with the atom to which they are bound to form an optionally substituted cycloalkane ring having 5 ring atoms;
- R7 is selected from a group consisting of hydrogen, optionally substituted C1-4 alkyl, optionally substituted C3-C7 cycloalkyl, and optionally substituted phenyl;
- R8 is selected from a group consisting of hydrogen, optionally substituted C1-4 alkyl, optionally substituted C3-C7 cycloalkyl, and optionally substituted phenyl;
- R9 is selected from a group consisting of hydrogen, optionally substituted C1-4 alkyl, optionally substituted C3-C7 cycloalkyl, and optionally substituted phenyl, optionally substituted heteroaryl, COR10, SO2R10;
- R10 is selected from a group consisting of hydrogen, optionally substituted C1-4 alkyl, optionally substituted C3-C7 cycloalkyl, and optionally substituted phenyl, or two R10 units are taken together with the atoms to which they are bound to form a ring having 5-8 ring atoms, or R9 and R10 units are taken together with the atoms to which they are bound to form a ring having 5-8 ring atoms;
- R11 is selected from a group consisting of hydrogen, optionally substituted C1-4 alkyl, optionally substituted C3-C7 cycloalkyl, and optionally substituted phenyl.
7 more elements
Dependencies are inferred from the claim text.