Fatty liver disease treatment using glucocorticoid and mineralocorticoid receptor antagonists
Patent Information
- Application Number
- HK42026128045
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2014-12-15
- Filing Date
- 2026-08-26
- Publication Date
- 2026-10-09
- Estimated Expiration
- 2035-10-13
Smart Images
Figure 00000000_0000_ABST
Abstract
Description
Abstract This invention provides a treatment for fatty liver disease using a class of pyrimidine dione cyclohexyl compounds. In one embodiment, the invention provides a method for treating fatty liver disease. The method comprises administering a therapeutically effective amount of a compound of formula I to a subject in need, thereby treating the fatty liver disease, wherein the compound of formula I has structure (I).
Claims
1. A pharmaceutical composition for oral administration comprising a compound of Formula Id and a pharmaceutically acceptable excipient, for use in a method of treating fatty liver disease, the method comprising orally administering to a subject in need thereof a therapeutically effective amount of the pharmaceutical composition , thereby treating the fatty liver disease, wherein the compound of Formula Id has the structure: wherein each R1a is independently H, C1-6 alkyl, halogen, or C1-6 haloalkyl; R2 is H, or C1-6 alkyl; and each R4 is H, C1-6 alkyl, halogen, or C1-6 haloalkyl; or is a salt thereof.
2. The pharmaceutical composition for oral administration for use according to claim 1, wherein the fatty liver disease is alcohol related liver disease (ARLD) or nonalcoholic fatty liver disease (NAFLD).
3. The pharmaceutical composition for oral administration for use according to claim 2, wherein the alcohol related liver disease is alcohol fatty liver disease (AFL), alcoholic steatohepatitis (ASH) or alcoholic cirrhosis.
4. The pharmaceutical composition for oral administration for use according to claim 2, wherein the nonalcoholic fatty liver disease is nonalcoholic steatohepatitis (NASH) or nonalcoholic cirrhosis.
5. The pharmaceutical composition for oral administration for use according to claim 1, wherein each R1a is C1-6 haloalkyl.
6. The pharmaceutical composition for oral administration for use according to claim 1, wherein each R1a is independently selected from the group consisting of H, Me, Et, F, Cl, or -CF3.
7. The pharmaceutical composition for oral administration for use according to claim 1, wherein each R1a is -CF3.
8. The pharmaceutical composition for oral administration for use according to claim 1, wherein R2 is H.
9. The pharmaceutical composition for oral administration for use according to claim 1, wherein the compound of Formula Id is selected from the group consisting of: and salts thereof.
10. The pharmaceutical composition for oral administration for use according to claim 1, wherein the compound of Formula Id has the formula: or a salt thereof.
11. The pharmaceutical composition for oral administration for use according to claim 1, wherein said compound of Formula Id is an antagonist of glucocorticoid receptor and mineralocorticoid receptor activity.
12. The pharmaceutical composition for oral administration for use according to claim 1, wherein said compound of Formula Id is a mineralocorticoid receptor antagonist and has an inhibition constant (Ki) against the human glucocorticoid receptor of between 0.0001 nanomolar (nM) and 1000 nM.
13. The pharmaceutical composition for oral administration for use according to claim 1, wherein the fatty liver disease is nonalcoholic fatty liver disease.
14. The pharmaceutical composition for oral administration for use according to claim 13, wherein the fatty liver disease is nonalcoholic steatohepatitis (NASH).
15. The pharmaceutical composition for oral administration for use according to claim 13, wherein the fatty liver disease is nonalcoholic cirrhosis.