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US 2018/0002277 A1Published application
Antioxidant inflammation modulators: oleanolic acid derivatives with amino and other modifications at c-17
AssigneeReata Pharmaceuticals, Inc.
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.
Claims23
1-257. (canceled)
A method of making a first compound defined as:
- wherein:
- R1 is:
- hydrogen or hydroxy;
- 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), alkoxy(C≦12), alkenyloxy(C≦12), alkynyloxy(C≦12), aryloxy(C≦12), aralkoxy(C≦12), heteroaryloxy(C≦12), heteroaralkoxy(C≦12), thioacyl(C≦12), alkylsulfonyl(C≦12), alkenylsulfonyl(C≦12), alkynylsulfonyl(C≦12), arylsulfonyl(C≦12), aralkylsulfonyl(C≦12), heteroarylsulfonyl(C≦12), or heteroaralkylsulfonyl(C≦12), or a substituted version of any of these groups;
- R2 is:
- hydroxy;
- 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), alkoxy(C≦12), alkenyloxy(C≦12), alkynyloxy(C≦12), aryloxy(C≦12), aralkoxy(C≦12), heteroaryloxy(C≦12), heteroaralkoxy(C≦12), thioacyl(C≦12), alkylsulfonyl(C≦12), alkenylsulfonyl(C≦12), alkynylsulfonyl(C≦12), arylsulfonyl(C≦12), aralkylsulfonyl(C≦12), heteroarylsulfonyl(C≦12), or heteroaralkylsulfonyl(C≦12), or a substituted version of any of these groups;
- wherein the first step of the synthesis comprises modification of the C-17 amino group of the following compound:
7 more elements
259-264. (canceled)
Dependencies are inferred from the claim text.