Back to results
US 2021/0002256 A1Published application
Tlr7/8 antagonists and uses thereof
AssigneeMerck Patent GmbH
InventorsBrian A. Sherer, Xiaoling Chen, Esther Cleary, Nadia Brugger
Life of this patent
Estimating the term…
Abstract
A compound of Formula I or pharmaceutically acceptable compositions thereof, is useful to as a TLR7/8 antagonist.
Claims19
A compound of formula I,
- Ring A is aryl or heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- Ring B is heteroaryl having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- R1 is —H, —CH3—, —CF3—, —CN, —F, —Cl, —OCH3, or —OCF3;
- each R2 is independently —H, —R, halogen, -haloalkyl, —OR, —SR, —CN, —NO2, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2;
- each R3 is independently —H, —R, halogen, -haloalkyl, —OR, —SR, —CN, —NO2, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2;
- X is C(R4)2;
- Y is C(R)2;
- each R4 is independently —H, —R, halogen, -haloalkyl, —OR, —SR, —CN, —NO2, —SO2R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —C(NH)R, —C(NH)NR2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2;
- each R5 is independently —H, —R, halogen, -haloalkyl, —OR, —SR, —CN, —NO2, —SO R, —SOR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRSO2R, or —N(R)2;
- each R is independently hydrogen, C1-6 aliphatic, C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- or
- two R groups on the same atom are taken together with the atom to which they are attached to form a C3-10 aryl a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- k is 1 or 2;
- n is 0, 1, or 2;
- p is 0, 1, or 2;
- r is 0, 1, or 2;
- and
- t is 0, 1, or 2.
19 more elements
7-8. (canceled)
Dependencies are inferred from the claim text.