INHIBITORS OF cGAS ACTIVITY AS THERAPEUTIC AGENTS

A compound according to Formula (I):

• or a pharmaceutically acceptable salt, N-oxide, and/ or solvate or hydrate thereof, wherein:
• m is an integer of 1, 2, or 3;
• n is an integer of 0. 1, 2, 3, or 4;
• ring A represents a 4 to 8 membered heterocyclyl ring;
• each R7 is independently selected from halogen, —NO2, —CN, C1-C6 alkyl, C1-C6 haloalkyl. —OH, 1-C6 alkoxy, and C1-C6 haloalkoxy:
• R2 is hydrogen, 1-C6 alkyl, or 1-C6 haloalkyl;
• R3 is —CO2R5, —COR5, —C(O)NR5R6, —CONH—OH, —S(O)0-2—R5, SO2OR5, or —SO2NR5R6;
• and
• RA is —C(O)NR6R7, —CO2R7, —SO2OR7, or —SONR6R7,
• wherein
• R5 is hydrogen or C1-C6 alkyl;
• R6 is hydrogen, C1-C6 alkyl, or C1-C6 haloalkyl;
• R7 is selected from the group consisting of aryl(C0-C4 alkyl) optionally substituted with one or more R8, heteroaryl(C0-C4 alkyl) optionally substituted with one or more R9, heterocyclyl(C0-C4 alkyl) optionally substituted with one or more R8, and cycloalkyl(C0-C4 alkyl) optionally substituted with one or more R8;
• each R3 is independently selected from the group consisting of halogen, —NO2, —CN, C1-C6 alkyl, C1-C6 haloalkyl, —N3, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)2, —OH, C1-C6 alkoxy, C1-C6 haloalkoxy, —C(O)R6, —C(O)OR6, and —C(O)NR5R6, or two R6 form an oxo;
• each R9 is independently selected from the group consisting of halogen, —NO2, —CN, C1-C6 alkyl, C1-C6 haloalkyl, —Na, —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)2, —OH, C1-C6 alkoxy, C1-C6 haloalkoxy, aryl(C0-C1 alkyl) optionally substituted with one or more R10. heteroaryl(C0-C1 alkyl) optionally substituted with one or more R10, heterocyclyl(C0-C1 alkyl) optionally substituted with one or more R10, and cycloalkyl(C0-C1 alkyl) optionally substituted with one or more R10, and
• each R10 is independently selected from the group consisting of halogen, —NO2, —CN, C1-C6 alkyl, C1-C6 haloalkyl, —N3, —NH2, —NH(1-C6 alkyl), —N(C1-C6 alkyl)2, —OH, C1-C6 alkoxy, C1-C6 haloalkoxy, and -methyl-OH;
• provided the compound is not (2S,4R)-1-(2-methylbenzofuro[3,2-d]pyrimidin-4-yl)-4-(2-oxo-2-(pyridin-4-ylamino)ethyl)pyrrolidine-2-carboxylic acid, (2S,4R)-4-(2-((1H-pyrazol-4-yl)amino)-2-oxoethyl)-1-(2-methylbenzofuro[3,2-d]pyrimidin-4-yl)pyrrolidine-2-carboxylic acid, (2S,4R)-1-(2-methylbenzofuro[3,2-d]pyrimidin-4-yl)-4-(2-oxo-2-(pyridin-2-ylamino)ethyl)pyrrolidine-2-carboxylic acid, (2S,4R)-4-(2- (cyclopentylamino)-2-oxoethyl)-1-(2-methylbenzofuro[3,2-d]pyrimidin-4-yl)pyrrolidine-2-carboxylic acid;
• or (2S,4R)-1-(2-methylbenzofuro[3,2-d]pyrimidin-4-yl)-4-(2-oxo-2-(phenylamino)ethyl)pyrrolidine-2-carboxylic acid.