IP Library Granted Patent US 9,765,090
Granted Patent B2
US 9,765,090 · App. 14/286,929 · Granted Sep 19, 2017

Epidithiodioxopiperazine compound or its derivatives, and the use thereof

Inventors: Sang Won Kang (Seoul, KR); Dong Hoon Kang (Gyeonggi-do, KR); Doo Jae Lee (Seoul, KR)
Assignee: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
C07D513/08A61K31/00C12Q1/26G01N2333/90212G01N2500/02
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Quick Facts
Patent No.
US 9,765,090
App. No.
14/286,929
Granted
Sep 19, 2017
Kind
B2
Abstract

The present invention relates to an epidithiodioxopiperazine derivative represented by the following Chemical Formula 1 or its reduced derivative; a method for preparing a compound represented by Chemical Formula 1 having improved intracellular permeability and mimicking the activity of 2-Cys-Prx in its reduced form in the cells; a pharmaceutical composition for preventing or treating vascular diseases comprising an epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient; a drug delivery device for local administration including the pharmaceutical composition; and a pharmaceutical composition for inhibiting melanoma metastasis comprising the epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient.

Claims (11)

1. An epidithiodioxopiperazine derivative represented by the following Chemical Formula 1, or a pharmaceutically acceptable salt thereof:

wherein, in Chemical Formula 1,

R 1 and R 3 are hydrogen,

R 2 and R 4 are each independently linear or branched C2 to C6 alkenyl or alkynyl, substituted or unsubstituted benzyl, alkoxyalkyl, one or more aryl-substituted C1 to C6 alkyl, linear or branched C1 to C6 alkylaryl, or a substituted or unsubstituted aryl group, provided that the compound of chemical formula 1 is not the following compound of Chemical Formula 9:

2. The derivative, or the pharmaceutically acceptable salt thereof of claim 1 , wherein R 1 and R 3 are hydrogen;

R 2 and R 4 are each independently linear or branched C2 to C6 alkenyl, C1 to C6 alkoxybenzyl, linear or branched C1 to C6 alkoxy C1 to C6 alkyl or benzhydryl.

3. The derivative, or the pharmaceutically acceptable salt thereof of claim 1 , wherein R 1 and R 3 are hydrogen;

R 2 and R 4 are each independently allyl, 4-methoxybenzyl, 3-methoxypropyl or benzhydryl.

4. The derivative, or the pharmaceutically acceptable salt thereof of claim 1 , wherein the derivative is any one of compounds represented by the following Chemical Formulae 10 to 12, and 14:

5. A composition comprising:

the epidithiodioxopiperazine derivative represented by the Chemical Formula 1 or the pharmaceutically acceptable salt thereof of claim 1 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 13, 2018
From: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
To: VASTHERA CO. LTD.
Reel/Frame 047486/0169 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 6, 2014
From: KANG, SANG WON; KANG, DONG HOON; LEE, DOO JAE
To: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
Reel/Frame 033480/0903 →
Priority Claims (2)
KR 10-2011-0124603 · Nov 25, 2011 · national
KR 10-2013-0059351 · May 24, 2013 · national
Continuity (2)
Continuation In Part PCTKR2012010073 · Nov 26, 2012
Related Publication 20160222031A1 · Aug 4, 2016