Estrogen receptor modulators
US-10400006-B2 · Sep 3, 2019 · US
2-methoxyestradiol derivatives and medical uses thereof
US12570685B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-12570685-B2 |
| Application number | US-202017768936-A |
| Country | US |
| Kind code | B2 |
| Filing date | Oct 14, 2020 |
| Priority date | Oct 15, 2019 |
| Publication date | Mar 10, 2026 |
| Grant date | Mar 10, 2026 |
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- Title
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- Abstract
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- Assignees and inventors
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- First independent claim
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Abstract
Official abstract text for this publication.
The present invention relates to novel 2-Methoxyestradiol derivatives and their medical use. In particular, the novel derivatives of the present invention are useful for the treatment or prevention of liver or lung fibrosis. Accordingly, the present invention also provides medical uses of the 2-Methoxyestradiol derivatives of the present invention. The present invention also provides a method of treating or preventing liver or lung fibrosis comprising administering an effective amount of the 2-Methoxyestradiol derivatives of the present invention.
First claim
Opening claim text (preview).
The invention claimed is: 1 . A compound or pharmaceutically acceptable salt thereof, wherein the compound is (13S, 17S)-17-hydroxy-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl benzenesulfonate, (13S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyldibenzenesulfonate, (13S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl bis(4-fluorobenzenesulfonate), (13S,17S)-2-methoxy-13-methyl-3-((phenylsulfonyl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl acetate, (13S,17S)-2-methoxy-13-methyl-17-((methylsulfonyl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl benzenesulfonate, (13S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl bis(3,4-difluorobenzenesulfonate), (13S,17S)-17-hydroxy-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl4-nitrobenzenesulfonate, (13S,17S)-17-hydroxy-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl4-methoxybenzenesulfonate, (13S,17S)-17-hydroxy-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl naphthalene-2-sulfonate, (13S,17S)-17-hydroxy-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl naphthalene-1-sulfonate, (13S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl bis(naphthalene-2-sulfonate), (13S,17S)-2-methoxy-13-methyl-3-((naphthalen-2-ylsulfonyl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl acetate, (13S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl bis(4-fluorobenzenesulfonate), (13S,17S)-2-methoxy-13-methyl-3-(((4-nitrophenyl)sulfonyl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl acetate, or (13S,17S)-2-methoxy-3-(((4-methoxyphenyl)sulfonyl)oxy)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl acetate. 2 . The compound or pharmaceutically acceptable salt of claim 1 , wherein the compound is (13S, 17S)-17-hydroxy-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl benzenesulfonate, (13S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyldibenzenesulfonate, (13S, 17S)-2-methoxy-13-methyl-17-((methylsulfonyl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl benzenesulfonate, or (13S,17S)-2-methoxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl bis(naphthalene-2-sulfonate). 3 . A composition comprising a compound or pharmaceutically acceptable salt of claim 1 and a pharmaceutically acceptable carrier. 4 . A method for treating or preventing fibrosis, comprising: administering to a subject in need of treatment or prevention of fibrosis a compound or pharmaceutically acceptable salt of claim 1 . 5 . The method of claim 4 , wherein the fibrosis is liver fibrosis or pulmonary fibrosis. 6 . The method of claim 5 , wherein the liver fibrosis is a fibrosis caused by chronic hepatitis virus infection, alcohol abuse, drug-induced liver injury (DILI), cholestasis, or NASH (Non-Alcoholic Steath Hepatitis).
Assignees
Inventors
Classifications
the A ring of the steroid being aromatic · CPC title
not covered by C07J31/003 · CPC title
- C07J1/007Primary
the substituent being an OH group free esterified or etherified · CPC title
Drugs for disorders of the respiratory system · CPC title
- A61P1/16Primary
for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title
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Frequently asked questions
Answers are generated from the same data shown on this page.
- What does patent US12570685B2 cover?
- The present invention relates to novel 2-Methoxyestradiol derivatives and their medical use. In particular, the novel derivatives of the present invention are useful for the treatment or prevention of liver or lung fibrosis. Accordingly, the present invention also provides medical uses of the 2-Methoxyestradiol derivatives of the present invention. The present invention also provides a method o…
- Who is the assignee on this patent?
- Pasteur Institut Korea, Korea Inst Radiological & Medical Sciences
- What technology area does this patent fall under?
- Primary CPC classification C07J1/007. Mapped technology areas include Chemistry & Metallurgy.
- When was this patent published?
- Publication date Tue Mar 10 2026 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
- What related patents are in patentsdb?
- We list 8 related publications on this page (citations in our corpus or others sharing the same primary CPC).