IP Library Granted Patent US 10,370,342
Granted Patent B2
US 10,370,342 · App. 15/692,093 · Granted Aug 6, 2019

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 10,370,342
App. No.
15/692,093
Granted
Aug 6, 2019
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 (26)

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 phenyl

optionally substituted with 1 to 3 R 5 ;

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

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

2. The compound of claim 1 , wherein R 1 is —H or C 1-4 alkyl.

3. The compound of claim 1 , wherein R 1 is methyl.

4. The compound of claim 1 , wherein R 2 is C 3-6 alkyl.

5. The compound of claim 1 , wherein R 3 and R 4 are taken together to form phenyl optionally substituted with 1 to 3 chloro, fluoro, bromo, —CN, C 1-2 alkyl optionally substituted with —OH, C 1-2 alkoxy, —C(O)C 1-2 alkyl, —C(O)OC 1-2 alkyl, pyrazolyl optionally substituted with 1 to 3 C 1-2 alkyl; or imidazolyl optionally substituted with 1 to 3 C 1-2 alkyl.

6. The compound of claim 1 , wherein:

R 1 is —H or C 1-4 alkyl;

R 2 is C 3-6 alkyl;

R 3 and R 4 are taken together to form phenyl optionally substituted with 1 to 3 halogen.

7. The compound of claim 1 , wherein Formula I is represented by Formula II

8. The compound of claim 1 , wherein Formula I is represented by Formula III

9. The compound of claim 6 , wherein R 3 and R 4 are taken together to form phenyl optionally substituted with 1 to 3 fluoro.

10. The compound of claim 1 , selected from

or a pharmaceutically acceptable salt thereof.

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

12. The pharmaceutical composition of claim 11 , further comprising one or more additional therapeutic agents.

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

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2017
From: CHIN, GREGORY; MACKMAN, RICHARD L.; MISH, MICHAEL R.; ZABLOCKI, JEFF
To: GILEAD SCIENCES, INC.
Reel/Frame 043471/0208 →
Continuity (2)
Provisional Application 62383162 · Sep 2, 2016
Related Publication 20180065938A1 · Mar 8, 2018
Cited By (9)
US 12,187,753 US 12,318,403 US 12,377,100 US 12,404,262 US 12,492,189 US 12,522,570 US 12,590,089 US 12,594,267 US 12,636,279