US 12,570,685 B2Granted

2-methoxyestradiol derivatives and medical uses thereof

AssigneesInstitut Pasteur Korea, Korea Institute of Radiological & Medical Sciences

InventorsHaeng Ran Seo, Inhee Choi, Junghwan Choi, Young Mi Kim, Yeonhwa Song, A-Ram Kim, Yoon Jin Lee, Hae-June Lee, Jae-Kyung Nam, Jihee Kim, Su-Yeon Lee

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Abstract

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.

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.

11 more elements

Facts

Application

17/768,936Filed 14 Oct 2020

Priority

KR 10-2019-012795115 Oct 2019

Published

US 2023/0295217 A121 Sep 2023

Granted

10 Mar 2026

Term ends

Not estimatedThe source records don’t support an estimate.

Classification12 codes

C07J 1/0074
The substituent being an OH group free esterified or etherified: esters
A61K 31/566
Not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol: having an oxo group in position 17, e.g. estrone
A61P 1/16
Drugs for disorders of the alimentary tract or the digestive system: for liver or gallbladder disorders, e.g. hepatoprotective agents,…
A61P 11/00
Drugs for disorders of the respiratory system

Abstract

Claims6