Antioxidant inflammation modulators: oleanolic acid derivatives with amino and other modifications at C-17
AssigneeReata Pharmaceuticals Holdings, LLC
InventorsEric Anderson, Xin Jiang, Melean Visnick
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Abstract
This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
Claims30
A method of suppressing the demyelination of neurons in a patient's brain or spinal cord, comprising administering to the patient an effective amount of a compound of the formula:
- wherein:
- R1 and R2 are independently:
- hydrogen;
- or
- alkyl(C≤12), alkenyl(C≤12), alkynyl(C≤12), aryl(C≤12), aralkyl(C≤12), heteroaryl(C≤12), heteroaralkyl(C≤12), acyl(C≤12), alkylsulphonyl, alkenylsulphonyl(C≤12), alkynylsulphonyl(C≤12), arylsulphonyl(C≤12), aralkylsulphonyl(C≤12), heteroarylsulphonyl(C≤12), heteroaralkyl-sulphonyl(C≤12), or a substituted version of any of these groups;
- or pharmaceutically acceptable salts, tautomers, or optical isomers thereof.
A method of suppressing neuronal apoptosis in a patient's brain or spinal cord, comprising administering to the patient an effective amount of a compound of the formula:
- wherein:
- Rand R2 are independently:
- hydrogen;
- or
- alkyl(C≤12), alkenyl(C≤12), alkynyl(C≤12), aryl(C≤12), aralkyl(C≤12), heteroaryl(C≤12), heteroaralkyl(C≤12), acyl(C≤12), alkylsulphonyl, alkenylsulphonyl(C≤12), alkynylsulphonyl(C≤12), arylsulphonyl(C≤12), aralkylsulphonyl(C≤12), heteroarylsulphonyl(C≤12), heteroaralkyl-sulphonyl(C≤12), or a substituted version of any of these groups;
- or pharmaceutically acceptable salts, tautomers, or optical isomers thereof.
A method of stimulating the remyelination of neuron axons in a patient's brain or spinal cord, comprising administering to the patient an effective amount of a compound of the formula:
- wherein:
- R1 and R2 are independently:
- hydrogen;
- or
- alkyl(C≤12), alkenyl(C≤12), alkynyl(C≤12), aryl(C≤12), aralkyl(C≤12), heteroaryl(C≤12), heteroaralkyl(C≤12), acyl(C≤12), alkylsulphonyl, alkenylsulphonyl(C≤12), alkynylsulphonyl(C≤12), arylsulphonyl(C≤12), aralkylsulphonyl(C≤12), heteroarylsulphonyl(C≤12), heteroaralkyl-sulphonyl(C≤12), or a substituted version of any of these groups;
- or pharmaceutically acceptable salts, tautomers, or optical isomers thereof.
Dependencies are inferred from the claim text.