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US 12,753,180 B2Granted
Sirt6 activators
AssigneeBoard of Regents, The University of Texas System
InventorsJia Zhou, Wenbo Zhang, Hua Liu
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel small molecule activators of Sirt6, for example, compounds of the general Formula (I), their methods and use for the treatment of various human diseases such as cancer, inflammatory diseases, neurodegenerative diseases, and infectious diseases:
Claims10
A compound according to Formula (I):
- or a pharmaceutically acceptable salt, tautomer, or isotopologue thereof,
- wherein:
- represents a single or double bond;
- X is NR5 or N or O or C;
- R5 is chosen from hydrogen, alkyl, cycloalkyl, alkoxyalkyl, alkylcarbonyl, or alkylsulfonyl;
- A is a five to ten membered ring chosen from heteroaryl, or fused heteroaryl;
- R1, R2, R4 are independently chosen from hydrogen, alkyl, cycloalkyl, haloalkyl, haloalkoxy, alkoxy, halo, cyano, carboxy, alkoxycarbonyl-R8, alkylcarbonyl-R8, aminocarbonyl, alkylaminocarbonyl-R8, alkoxyalkyl, aminoalkyl, aminoalkoxy, hydroxyl, and hydroxyalkyl;
- R3 is a four to eight membered heterocycle, substituted with one or more R6 substituents;
- R6 is chosen from hydrogen, hydroxyl, halo, alkyl-R7, alkoxy, cycloalkyl, carbonyl-R7, alkylcarbonyl-R7, alkylsulfonyl, heteroaryl, or heterocyclyl;
- wherein R7 is chosen from hydrogen, hydroxyl, halo, alkoxy, amino, cyano, alkylamino, dialkylamino, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, heterocyclyl, or heteroaryl;
- wherein R7 is chosen from hydrogen, halo, hydroxyl, cycloalkyl, alkoxy, or alklysulfonyl.
8 more elements
A compound chosen from any of the following structures:
- Cpd
- No.
- Structure
- 21
- 30
- 22
- 23
- 24
- 25
- 18
- 28
- 29
- 16
- 19
- 26
- 20
- 27
- 17
- 35
- 38
- 36
- 65
- 37
- 39
- 48
- 44
- 40
- 41
- 42
- 43
- 45
- 46
- 50
- 47
- 49
- 64
- 60
- 62
- 61
- 66
- 68
- 70
- 69
- 73
- 71
- 72
- 74
- 76
- 75
46 more elements
Dependencies are inferred from the claim text.