Genistein phosphate derivatives
Patent Information
- Application Number
- HK62026127088
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2023-11-28
- Filing Date
- 2026-08-05
- Publication Date
- 2026-10-09
- Estimated Expiration
- 2044-11-20
Abstract
Description
Abstract Novel genistein phosphate derivatives, pharmaceutical compositions comprising them, and their medical uses.
Claims
Claims:
1. A compound of formula 1 or II:or a pharmaceutically acceptable salt thereof, where: in formula I: each of R1, R2, and R3independently is selected from the group consisting of H, Ci-6 alkyl, and (R4O)2P(O)CH2-, provided that at least one of R1, R2, and R3is (R4O)2P(O)CH2-; and each R4independently is selected from the group consisting of H and Ci-6 alkyl; and in formula II: each of R5and R6independently is selected from the group consisting of H, Ci-6 alkyl, and (R7O)2P(O)CH2-, and each R7independently is selected from the group consisting of H and Ci-6 alkyl.
2. The compound of claim 1 that is a compound of formula I or a pharmaceutically acceptable salt thereof.
3. The compound of claim 2 where R1is H, or a pharmaceutically acceptable salt thereof.
4. The compound of claim 2 or 3 where each R4is H, or a pharmaceutically acceptable salt thereof.
5. The compound of claim 2 that is (4-(5,7-dihydroxy-4-oxo-477-chromen-3-yl)phenoxy)methyl dihydrogen phosphate, ((5-hydroxy-3-(4-hydroxyphenyl)-4-oxo- 47 -chromen -7-y 1 )oxy )methyl dihydrogen phosphate, or ((5-hydroxy-4-oxo- 3-(4-((phosphonooxy)methoxy)phenyl)-4H-chromen-7-yl)oxy)methyl dihydrogen phosphate, or a pharmaceutically acceptable salt thereof.
6. The compound of claim 5 that is ((5 -hydroxy-3 -(4-hydroxypheny l)-4-oxo-4H-chromen- 7-yl)oxy)methyl dihydrogen phosphate or a pharmaceutically acceptable salt thereof.
7. The compound of claim 6 that is ((5 -hydroxy-3 -(4-hydroxypheny l)-4-oxo-4H-chromen- 7-yl)oxy)methyl dihydrogen phosphate.
8. The compound of claim 1 that is a compound of formula II or a pharmaceutically acceptable salt thereof.
9. The compound of claim 8 where R5and R6are H, or a pharmaceutically acceptable salt thereof.
10. The compound of claim 8 or 9 where each R7is H, or a pharmaceutically acceptable salt thereof.
11. The compound of claim 8 that is 4-(5,7-dihydroxy-4-oxo-4H-chromen-3-yl)phenyl 2,2-dimethyl-5-(phosphonooxy)pentanoate or a pharmaceutically acceptable salt thereof.
12. A pharmaceutical formulation comprising a compound of any one of claims 1 to 11.
13. The pharmaceutical formulation of claim 12 that is an oral formulation.
14. The pharmaceutical formulation of claim 13 that is a tablet, a capsule, an oral solution, or an oral suspension.
15. The pharmaceutical formulation of any one of claims 12 to 14 where the compound is a compound of claim 6 or 7.
16. A compound of any one of claims 1 to 11 for use as a medicament.
17. The compound for use of claim 16 where the compound is a compound of claim 6 or 7.
18. A compound of any one of claims 1 to 11 for use in the treatment of a condition treatable by genistein or a genistein derivative.
19. A compound of any one of claims 1 to 1 1 for use in the treatment of a condition selected from dilated cardiomyopathy, Duchenne muscular dystrophy, heart failure, inflammatory bowel disease / ulcerative colitis / Crohn’s disease, obesity and obesity-induced diabetes, osteoarthritis, pancreatitis, pancreatic ductal adenocarcinoma, rheumatoid arthritis, systemic vasculitis, and transthyretin amyloid cardiomyopathy, or Down syndrome.
20. The compound for use of claim 18 or 19 where the compound is a compound of claim 6 or 7.
21. The compound for use of any one of claims 16 to 20 where the dose of the compound is 0.1 - 100, 0.2 - 80, 0.3 - 60, 0.4 - 40, or 0.5 - 20 mg / Kg / day.
22. The compound for use of any one of claims 16 to 20 where the dose of the compound is1 - 2,500, 2 - 2,000, 5 - 1,500, 10 - 1,000, 15 - 750, or 20 - 500 mg twice / day.