Back to results
US 10,947,214 B2Granted
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
The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as TLR7/8 antagonists.
Claims8
A compound of formula I-e,
- or a pharmaceutically acceptable salt thereof, wherein:
- R1 is —CF3 or —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;
- R4 is C1-6 aliphatic, —C(O)R, —C(O)N(R)2, —C(NH)NR2, —NRC(O)R, —N(R)2;
- or 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- each R5 is independently 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, 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 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;
- n is 0, 1, or 2;
- p is 0;
- r is 0;
- and
- t is 1 or 2.
17 more elements
A compound wherein the compound is selected from the group consisting of compounds shown in the following Table or a pharmaceutically acceptable salt thereof
- Compound 1
- Compound 2
- Compound 3
- Compound 4
- Compound 5
- Compound 6
- Compound 7
- Compound 8
- Compound 9
- Compound 10
- Compound 11
- Compound 12
- Compound 13
- Compound 14
- Compound 15
- Compound 16
- Compound 17
- Compound 18
- Compound 19
- Compound 20
- Compound 21
- Compound 23
- Compound 24
- Compound 25
- Compound 26
- Compound 27
- Compound 28
- Compound 29
- Compound 30
- Compound 31
- Compound 32
- Compound 33
- Compound 34
- Compound 35
- Compound 36
- Compound 37
- Compound 38
- Compound 39
- Compound 40
- Compound 41
- Compound 42
- Compound 43
- Compound 44
- Compound 45
- Compound 46
- Compound 47
- Compound 48
- Compound 49
- Compound 50
- Compound 51
- Compound 52
- Compound 53
- Compound 54
- Compound 55
- Compound 56
- Compound 57
- Compound 58
- Compound 59
- Compound 60
- Compound 61
- Compound 62
- Compound 63
- Compound 64
- Compound 65
- Compound 66
- Compound 67
- Compound 68
- Compound 69
- Compound 70
- Compound 71
- Compound 72
- Compound 73
- Compound 74
- Compound 75
- Compound 76
- Compound 77
- Compound 78
- Compound 79
- Compound 85
- Compound 91
- Compound 92
- Compound 93
- Compound 96
- Compound 97
- Compound 98
- Compound 99
- Compound 100
- Compound 106
- Compound 107
- Compound 108
- Compound 109
- Compound 110
- Compound 113
- Compound 116
- Compound 117
- Compound 118,
- and
- Compound 119.
95 more elements
Dependencies are inferred from the claim text.