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US 2020/0369648 A1Published application
Tlr7/8 antagonists and uses thereof
AssigneeMerck Patent GmbH
InventorsBrian A. Sherer, Nadia Brugger, Ruoxi Lan, Xiaoling Chen
Life of this patent
Estimating the term…
Abstract
Compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists, are described herein.
Claims20
A compound of formula I,
- or a pharmaceutically acceptable salt thereof, wherein,
- Ring A is an aryl having 6 atoms;
- Ring B is a heteroaryl having 2 nitrogen atoms, each nitrogen having a double bond to an adjacent carbon;
- R1 is —CN;
- 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;
- each R4 is independently —C(O)N(R)2, —NRC(O)R, —NRC(O)N(R)2, —NRC(O)OR, —NRSO2R, or —N(R)2;
- each R5 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 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 0, 1 or 2;
- n is 0, 1, or 2;
- p is 0, 1, or 2;
- r is 1,2, or 3;
- and
- t is 1, 2, or 3;
- wherein k is 0 when attached to nitrogen;
- and k is 1 or 2 when attached to carbon.
18 more elements
(canceled)
(canceled)
Dependencies are inferred from the claim text.