Compounds as nlrp3 inflammasome inhibitors and compositions and uses thereof
AssigneeVirginia Commonwealth University
InventorShijun ZHANG
Life of this patent
Estimating the term…
Abstract
Scaffold compounds are used to design small molecule compounds and structure-activity relationship studies identify inhibitors of inflammation. Methods include pharmaceutical compositions of the small molecule compounds to inhibit, prevent and treat diseases and conditions associated with inflammation, including multiple sclerosis, Alzheimer's disease, acute myocardial infarction, traumatic brain injury and autoinflammatory diseases.
Claims11
A compound or a pharmaceutically acceptable salt, solvate or hydrate thereof having the general chemical structure
- wherein
- R1 is unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted C1-C8 alkyl or is unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted C1-C8 alkoxyl, or nitro, or cyano;
- R4 is H, halogen, amino, nitro or cyano;
- R2, R3 and R5 may be the same or different and are independently selected from H, C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkyl, C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkoxyl, C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkylcarbonyl, halogen, hydroxyl, amino, nitro and cyano;
- W is absent or is unbranched, branched, saturated, unsaturated, substituted or unsubstituted C1-C4 alkyl;
- R6 is unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted C1-C8 alkylcarbonyl;
- substituted or unsubstituted aryl or heteroarylcarbonyl;
- C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkyl, or H;
- Y is C1-C5 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkyl;
- V is i) NR1R2 where R11 and R2 are H or C1-C8 alkyl and may be the same or different;
- or ii) a saturated heterocycle comprising N bonded directly to S.
A compound having a chemical structure selected from the group consisting of
- and pharmaceutically acceptable salts, solvates or hydrates thereof.
A method of inhibiting, preventing or treating NRLP3 inflammasome-associated disease in a subject in need thereof, comprising a step of
- administering to said subject a therapeutically effective amount of a pharmaceutical composition comprising at least one compound or pharmaceutically acceptable salt, solvate or hydrate thereof having the general chemical structure of:
- wherein
- R1 is unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted C1-C8 alkyl or is unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted C1-C8 alkoxyl, or nitro, or cyano;
- R4 is H, halogen, amino, nitro or cyano;
- R2, R3 and R5 may be the same or different and are independently selected from H, C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkyl, C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkoxyl, C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkylcarbonyl, halogen, hydroxyl, amino, nitro and cyano;
- W is unbranched, branched, saturated, unsaturated, substituted or unsubstituted
- C1-C4 alkyl and may be present or absent;
- R6 is unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted C1-C8 alkylcarbonyl;
- substituted or unsubstituted aryl or heteroarylcarbonyl;
- C1-C8 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkyl or H;
- Y is C1-C5 unbranched, branched, saturated, unsaturated, cyclic or acyclic, substituted or unsubstituted alkyl;
- V is i) NR1R2 where R1 and R2 are H or C1-C8 alkyl and may be the same or different;
- or ii) a saturated heterocycle comprising N bonded directly to S;
- and
- a physiologically acceptable carrier.
Dependencies are inferred from the claim text.