Patent ID: 11926612
Assignee: RESEARCH TRIANGLE INSTITUTE
Field: Pharmaceuticals (Chemistry)
Classification: CPC C  A | IPC C

Claim 0:
1. A compound represented by the Formula I:, or a pharmaceutically acceptable salt, a prodrug, or a salt of a prodrug thereof,
wherein ring A is a 5-member heteroaryl ring; each G1 is independently selected from C or N;
each G2 is independently selected from CH or N; the bond between each two instances of G1 or G2 is either a single or a double bond so as to make the ring A an aromatic heterocycle, wherein at least one G1 or G2 is N and a maximum number of three instances of either G1 or G2 in the ring are simultaneously N; provided that if there are two N in ring A and G1 connected to R2 or R1 is N, the adjacent G2 is not N;
R1 is represented by the formula:, wherein, is a monocyclic aryl or heteroaryl group;

each A is independently C1-8 alkyl, C1-8 alkyl(aryl), C1-8 alkoxy, C1-8 alkoxy aryl, C2-8 alkenyl, C3-8 alkynyl, C3-8 cycloalkyl, —CF3, —(CH2)xNR7R8, —CN, —CONR7R8, —COR7, —CO2(CH2)xNR7R8, —CO2R7, halogen, hydroxyl, —N3, —NHCOR7, —NHSO2C1-8 alkyl, —NHCO2C1-8 alkyl, —NO2, —NR7R8, —O(CH2)xNR7R8, —O(CH2)xCO2R7, —OCOC1-8 alkyl, —OCO(CH2)xNR7R8, —SO2NR7R8, —SO(1-3)R7, or —SR7;
R7 and R8 are independently C1-8 alkoxy, aryl, C1-8 alkyl, C1-8 alkyl alcohol, C1-8 alkyl amino, C1-8 alkyl amido, C1-8 alkyl(aryl), C1-8 alkyl (C3-8 cycloalkyl), C1-8 alkyl guanidinyl, C1-8 alkyl heteroaryl, C1-8 alkyl thioether, C1-8 alkyl thiol, C2-8 alkenyl, C3-8 alkynyl, C3-8 cycloalkyl, —(CH2)xCONHR9, —(CH2)xCOR9, —(CH2)xCO2R9, H, or heteroaryl; or R7 and R8 together make a 3-9 member ring which may contain one or more heteroatoms; or R7 and R8 together make a 5-8 nitrogen containing member ring with one or more carbonyl groups;
n is 1, 2, 3, 4 or 5;
R2 is optionally substituted C3-8 alkyl or optionally substituted C0-8 alkyl-R10, wherein R10 is a 3- to 8-membered ring, optionally containing one or more heteroatom selected from N, O, or S, optionally containing one or more degrees of unsaturation;
R3 is H;
R4 is adamantanyl, C1-8 alkyl amido, C2-8 alkyl(aryl), C1-8 alkyl (C3-8 cycloalkyl), C1-8 alkyl (C3-8 cycloalkyl)-CO2R7, C1-8 alkyl guanidinyl, C1-8 alkyl heteroaryl, C2-4 alkyl heterocycloalkyl, C1-8 alkyl thioether, C1-8 alkyl thiol, C2-8 alkenyl, C2-8 alkenyl(aryl), C2-8 alkenyl(heteroaryl), C3-8 alkynyl, C3-8 cycloalkyl-CO2R7, —(CH2)xNR7R8, —(CH2)xOR7,

—(CH2)xNR9COR7, —(CH2)xNR9SO2R7, —(CH2)xNR9CO2R7, —(CH2)xNHCOR7,
—(CH2)xNHSO2R7, —(CH2)xNHCO2R7, —(CH2)xxCONR7R8,
—(CH2)xCONR7(CH2)yCO2R9, —(CH2)xCONR7(CH2)yCONR7R8,
—(CH2)xCONR7(CH2)yR9, —(CH2)xCOR7, —(CH2)xxCO2R7,
—(CH2)xSO2NR7(CH2)yR9, —CHR7COR9, —CHR7CONHCHR8COR9,
—CONR7(CH2)xCO2R8, —CONR7CHR8CO2R9, —NHCO2R7, or —(CH2)x SO2NR7R8;
R5 is adamantanyl, C1-8 alkyl amido, C2-8 alkyl(aryl), C1-8 alkyl (C3-8 cycloalkyl), C1-s alkyl (C3-8 cycloalkyl)-CO2R7, C1-8 alkyl guanidinyl, C1-8 alkyl heteroaryl, C2-4 alkyl heterocycloalkyl, C1-8 alkyl thioether, C1-8 alkyl thiol, C2-8 alkenyl, C2-8 alkenyl(aryl), C2-8 alkenyl(heteroaryl), C3-8 alkynyl, C5-8 cycloalkyl, C3-8 cycloalkyl-CO2R7, —(CH2)xNR7R8, where at least one of R7 or R8 is not H, —(CH2)xOR7, —(CH2)xNR9COR7,

—(CH2)xNR9SO2R7, —(CH2)xNR9CO2R7, —(CH2)xNHCOR7, —(CH2)xNHSO2R7,
—(CH2)xNHCO2R7, —(CH2)xxCONR7R8, —(CH2)xCONR7(CH2)yCO2R9,
—(CH2)xCONR7(CH2)yCONR7R8, —(CH2)xCONR7(CH2)yR9, —(CH2)xCOR7,
—(CH2)xxCO2R7, —(CH2)xSO2NR7(CH2)yR9, —CHR7COR9, —CHR7CONHCHR8COR9,
—CONR7(CH2)xCO2R8, —CONR7CHR8CO2R9, —NHCO2R7, or —(CH2)x SO2NR7R8;
R9 is aryl, C1-8 alkoxy, C1-8 alkyl, C1-8 alkyl(aryl), C3-8 cycloalkyl, H, heteroaryl, or hydroxyl;
each x is independently 0-8;
each xx is independently 1-8; and
each y is independently 1-8.