Modulators of toll-like receptor 7

Patent metadata

Field	Value
Publication number	US-9611268-B2
Application number	US-201514626738-A
Country	US
Kind code	B2
Filing date	Feb 19, 2015
Priority date	Jun 29, 2007
Publication date	Apr 4, 2017
Grant date	Apr 4, 2017

Abstract

The present application includes a compound of Formula I or II:

or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.

First claim

What is claimed:

1. A compound represented by Formula IIa:

or a pharmaceutically acceptable salt thereof, wherein:
R 1 is —NR 4 R 5 ;
R 2 is alkyl, alkenyl, carbocyclyl, carbocyclylalkyl, arylalkyl, or substituted arylalkyl;
-L 3 -R 3 is —O-alkyl or —O-alkylene-O-alkyl;
R 4 and R 5 are each independently H, or carbocyclylalkyl; or
R 4 and R 5 , taken together with the nitrogen to which they are both attached, form an unsubstituted heterocycle, wherein the heterocycle is a 4- to 6-membered monocyclic fully saturated ring containing one hetero atom selected from N; and
n is 0.

2. A pharmaceutical composition comprising: at least one compound of claim 1 , or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier or excipient.

3. The compound of claim 1 , wherein R 2 is methyl, ethyl, n-propyl, isopropyl, n-butyl, allyl, cyclopropyl, methylcyclopropyl, cyclopropylmethylene, benzyl or methoxybenzyl.

4. The compound of claim 1 , wherein -L 3 -R 3 is —OCH 2 CH 2 OCH 3 or —OCH 2 CH 2 CH 2 CH 3 .

5. The compound of claim 1 selected from the group consisting of:

or pharmaceutically acceptable salts thereof.

6. The compound of claim 1 wherein -L 3 -R 3 is —OCH 2 CH 2 CH 2 CH 3 .

7. The compound of claim 1 wherein R 4 and R 5 , taken together with the nitrogen to which they are both attached form a heterocycle having the structure:

Assignees

• Gilead Sciences Inc

Inventors

• Graupe Michael
• Halcomb Randall L

Classifications

• A61P31/14

  for RNA viruses · CPC title

• A61P31/12

  Antivirals · CPC title

• A61P31/00

  Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P31/20

  for DNA viruses · CPC title