US 12,410,174 B1
Small molecular inhibitors of sting signaling compositions and methods of use
Glen N Barber, Miami, FL (US)
Assigned to TYERELL IMMUNOTHERAPEUTICS INC, Columbus, OH (US)
Filed by Glen N Barber, Miami, FL (US)
Filed on Dec. 4, 2023, as Appl. No. 18/528,433.
Application 18/528,433 is a continuation of application No. 17/246,480, filed on Apr. 30, 2021, granted, now 11,897,888.
Claims priority of provisional application 63/017,984, filed on Apr. 30, 2020.
This patent is subject to a terminal disclaimer.
Int. Cl. C07D 487/04 (2006.01); A61P 37/06 (2006.01)
CPC C07D 487/04 (2013.01) [A61P 37/06 (2018.01)] 20 Claims
 
1. A method of inhibiting a functional activity of a STING protein (STimulator of INterferon Genes protein) in a human subject suffering from a disease and in need thereof, comprising:
(a) determining whether the human subject has an upregulated functional activity of STING protein, comprising:
isolating a biological sample from the human subject having the disease;
performing an assay on the biological sample to determine the functional activity of the STING protein;
(b) if the human subject has an upregulated functional activity of the STING protein;
then selecting a compound to inhibit the functional activity of the STING protein, where the compound has formula I:

OG Complex Work Unit Chemistry
or a pharmaceutically acceptable salt, hydrate, ester, solvate, stereoisomer, or tautomer thereof, where R1 is —(C2-C6) alkyl-(C3-C6) cycloalkenyl, —(C1-C6) alkyl-(C3-C6) cycloalkyl, —(C1-C6) alkyl-(C3-C6) substituted cycloalkenyl, —(C1-C6) alkoxy-(C3-C6) cycloalkenyl, —(C2-C6) alkenyl-(C3-C6) cycloalkenyl, where R2, R3, R4, R5 and R6 are independently selected from the group consisting of —H, -halogen, —(C1-C6) alkyl, —(C3-C6) cycloalkyl, —(C1-C6) haloalkyl, —(C1-C6) alkoxy, —(C1-C6) haloalkoxy, —(C2-C6) alkenyl, —(C2-C6) alkynyl, -nitro, —CN, —OH, —COOH, —SH, —NH2, —NH(C1-C4) alkyl, and —N((C1-C4) alkyl)2, where R7 is an atom selected from the group consisting of selenium and oxygen; and
administering the compound to the human subject suffering from the disease to inhibit the functional activity of the STING protein in the human subject.