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US 11,629,134 B2Granted
TLR7/8 antagonists and uses thereof
AssigneeMerck Patent GmbH
InventorsBrian A. Sherer, Nadia Brugger
Life of this patent
Estimating the term…
Abstract
Compounds of Formula 1 and pharmaceutically acceptable compositions thereof are useful as TLR7/8 antagonists.
Claims14
A compound of formula I,
- or a pharmaceutically acceptable salt thereof, wherein:
- Ring A is pyridyl;
- Ring B is pyridyl or pyrazinyl;
- R1 is —CHF2, —CH3, —F, —CF3, —OMe, or —CN;
- each R2 is independently —H, —C1-8 alkyl, C1-6 aliphatic, C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, 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, alkyl, -haloalkyl, and —CN;
- X is CH2 or O;
- each R4 is independently selected from the group consisting of
- each R5 is independently alkyl or -haloalkyl;
- 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, with the exception of H;
- 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 0 or 1;
- n is 0, 1, or 2;
- p is 0, 1, or 2;
- r is 1 or 2;
- and
- t is 1 or 2.
17 more elements
A compound selected from the group consisting of one of the compounds of the following Table, or a pharmaceutically acceptable salt thereof:
- Compound
- Example
- Number
- Number
- Chemical Structure
- 10
- 9
- 15
- 10
- 17
- 11
- 18
- 12
- 22
- 10
- 23
- 10
- 26
- 13
- 27
- 13
- 29
- 13
- 30
- 13
- 33
- 10
- 34
- 13
- 37
- 10
- 39
- 12
- 41
- 10
- 42
- 14
- 47
- 18
- 48
- 19
- 52
- 22
- 53
- 22
- 54
- 22
- 55
- 22
- 56
- 22
- 58
- 22
- 60
- 22
- 61
- 23
- 62
- 24
- 63
- 25
- 64
- 25
- 65
- 25
- 80
- 37
- 84
- 39
- 86
- 40
- 89
- 41
- 90
- 41
- 93
- 42
- 94
- 42
- 96
- 42
- 100
- 43
- 101
- 43
- 104
- 13
- 105
- 13
- 107
- 13
- 110
- 10
- 114
- 44
- 115
- 44
- 118
- 13
- 120
- 10
- 121
- 12
- 126
- 12
- 127
- 45
- 128
- 13
- 131
- 10
- 133
- 10
- 139
- 42
- 141
- 10
- 143
- 10
- 145
- 10
- 148
- 41
- 149
- 41
- 152
- 41
- 153
- 41
- 156
- 41
- 157
- 41
- 160
- 41
- 161
- 41
- 164
- 10
- 168
- 10
- 170
- 10
- 172
- 10
- 459
- 32
- 460
- 114
- 553
- 30
- 554
- 122
- 555
- 122
- 556
- 122
- 557
- 122
- 558
- 122
- 559
- 122
- 560
- 122
- 561
- 123
- 562
- 123
- 563
- 123
- 564
- 124
- 565
- 124
- 566
- 124
- 567
- 138
176 more elements
Dependencies are inferred from the claim text.