IP Library Granted Patent US 12,522,570
Granted Patent B2
US 12,522,570 · App. 18/476,141 · Granted Jan 13, 2026

Toll like receptor modulator compounds

Inventors: Gregory Chin (San Francisco, CA); Richard L. Mackman (Millbrae, CA); Michael R. Mish (Foster City, CA); Jeff Zablocki (Los Altos, CA)
Assignee: Gilead Sciences, Inc.
C07D239/95A61K31/517A61K31/519A61K45/06A61P31/18A61P35/00C07D471/04C07D487/04C07D495/04
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Quick Facts
Patent No.
US 12,522,570
App. No.
18/476,141
Granted
Jan 13, 2026
Kind
B2
Abstract

This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.

Claims (22)

1 . A compound of Formula I

or a pharmaceutically acceptable salt thereof, wherein:

R 1 is —H, C 1-4 alkyl, or C 1-4 haloalkyl;

R 2 is C 1-6 alkyl or C 1-6 haloalkyl;

Q is CR 4 ;

R 3 and R 4 are taken together to form:

each R 6 is optionally present and is independently halogen, —OH, —NH 2 , —CN, C 1-4 alkyl optionally substituted with 1 phenyl optionally substituted with 1 to 3 RZ, C 1-4 haloalkyl, C 1-4 alkoxy, —S(O) 2 C 1-4 alkyl, 5 to 6 membered heterocyclyl having 1 to 3 heteroatoms selected from oxygen, nitrogen, and sulfur optionally substituted with 1 to 3 R 2 , phenyl optionally substituted with 1 to 3 R2, or 5 to 6 membered heteroaryl having 1 to 3 heteroatoms selected from oxygen, nitrogen, and sulfur optionally substituted with 1 to 3 RZ; and

each R 2 is independently-NH 2 , C 1-4 alkyl, halogen, —CN, —OC 1-4 alkyl, C 1-4 haloalkyl, or —C(O) NH 2 ;

with the proviso that Formula I is not

2 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is —H or C 1-4 alkyl.

3 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is methyl.

4 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 2 is C 3-6 alkyl.

5 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein R 1 is —H or C 1-4 alkyl;

R 2 is C 3-6 alkyl; and

each R 6 is independently halogen, —OH, C 1-4 alkyl, or C 1-4 alkoxy.

6 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Formula I is represented by Formula II

7 . The compound of claim 1 , or a pharmaceutically acceptable salt thereof, wherein Formula I is represented by Formula III

8 . The compound of claim 1 selected from

or a pharmaceutically acceptable salt thereof.

9 . A pharmaceutical composition comprises a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

10 . The pharmaceutical composition of claim 9 , further comprising one or more additional therapeutic agents.

11 . A kit comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 8, 2023
From: CHIN, GREGORY; MACKMAN, RICHARD L.; MISH, MICHAEL R.; ZABLOCKI, JEFF
To: GILEAD SCIENCES, INC.
Reel/Frame 065501/0856 →
Continuity (5)
Continuation 17399984 · Aug 11, 2021
Division 16441339 · Jun 14, 2019
Division 15692093 · Aug 31, 2017
Provisional Application 62383162 · Sep 2, 2016
Related Publication 20240254091A1 · Aug 1, 2024
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