COMPOUNDS AND COMPOSITIONS AS TLR ACTIVITY MODULATORS

摘要

The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 7. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.

主权项

1. A compound of Formula (I), or pharmaceutically acceptable salt thereof:wherein:
R1 is C1-C4alkyl, —C(R5)2OH, -L1R5 or -L1R6; L1 is —C(O)— or —O—; L2 is C1-C6alkylene, C2-C6alkenylene, arylene, heteroarylene or —((CR4R4)pO)q(CH2)p—, wherein the C1-C6alkylene and C2-C6alkenylene of L2 are optionally substituted with 1 to 4 fluoro groups; each L3 is independently selected from C1-C6alkylene and —((CR4R4)pO)q(CH2)p—, wherein the C1-C6alkylene of L3 is optionally substituted with 1 to 4 fluoro groups; L4 is arylene or heteroarylene; R2 is C1-C4alkyl; R3 is selected from -L3R5, -L1R5, -L3R7, -L3L4L3R7, -L3L4R5, -L3L4L3R5, —OL3R7, —OL3L4R7, —OL3L4L3R7, —OR8, —OL3L4R5 and —OL3L4L3R5; each R4 is independently selected from H and fluoro; R5 is —P(O)(OH)2, R6 is —CF2P(O)(OH)2 or —C(O)OH; R7 is —CF2P(O)(OH)2 or —C(O)OH; R8 is H or C1-C4alkyl; each p is independently selected from 1, 2, 3, 4, 5 and 6, and q is 1, 2, 3 or 4.