Abstract: The present invention relates to a novel method for synthesizing a decursin derivative, enabling high-yield mass synthesis of a decursin derivative (PRG-A-04) represented by compound I through a reaction between decursinol and an intermediate compound in which a Boc protecting group is introduced to an OH group of 3-(3-methoxy-4-nitrophenyl)prop-2-en-1-ol in the presence of a palladium catalyst and xantphos.
Abstract: The present invention relates to a composition for prevention or treatment of neurofibromatosis type 2 syndrome, wherein in contrast to the conventional T?R1 kinase inhibitor TEW7197, the compound represented by chemical formula 1, a pharmaceutically acceptable salt thereof, a solvate thereof, a stereoisomer thereof, or a combination thereof according to the present invention suppresses TGF-? receptor 1 (T?R1)-mediated RKIP reduction while not inhibiting normal TGF-? signaling and thus, can be used as a novel form of a therapeutic agent for neurofibromatosis type 2 syndrome, which can solve the side effect problem caused by the inhibition of normal TGF-? signaling.
Abstract: The present invention relates to a novel method for synthesizing a decursin derivative, the method comprising: a step (I) for preparing a solution by mixing cinnamyl bromide and an N-Methyl-2-pyrrolidone [N-Methyl-2-pyrrolidone (NMP)] solvent; a step (II) for preparing a solution by mixing decursinol, a tetrahydrofuran (THF) solvent, and sodium hydride (NaH); and a step (III) for obtaining a decursin derivative by mixing the solutions prepared in step (I) and step (II). The method can increase the yield of the obtained decursin derivative compound and enables mass production.
Abstract: The present invention relates to a use of a novel compound, for preventing, improving or treating amyotrophic lateral sclerosis (ALS). The present inventors have found that SOD1 aggregation is one of the important causes of ALS, and have proposed the possibility that WT-SOD1 aggregation, caused by suppressing the regulation of intracellular stress or TDP-43, may be a cause of sALS. In addition, the present inventors have discovered the novel compound PRG-A-01(SLC-B036) as a SOD1 aggregation and misfolding inhibitor. The compound exhibited a protective effect against muscle weakness and movement disorder in an ALS mouse model. According to the result of a histological analysis, intraspinal nerves were maintained by means of a treatment using PRG-A-01(SLC-B036). In addition, the present inventors have obtained a candidate compound (PRG-A-04) which can be a more optimized drug. Consequently, the compound of the present invention may be usefully employed in developing a therapeutic agent for ALS.
Abstract: A composition for preventing or treating an aging-related disease includes a novel decursin derivative as an active ingredient, wherein the novel decursin derivative has exhibited an excellent effect of inhibiting progerin expression and excellent effect of inhibiting binding between progerin and lamin A, and it has been confirmed that the novel decursin derivative prolongs the survival period of animal models in which progerin was induced.
Type:
Grant
Filed:
April 25, 2018
Date of Patent:
May 18, 2021
Assignee:
PRG S&TECH INC
Inventors:
Bum Joon Park, Gyu Yong Song, Yu Seok O, Jee Hyun Lee, Eun Ju Yun
Abstract: A composition for preventing or treating an aging-related disease includes a novel decursin derivative as an active ingredient, wherein the novel decursin derivative has exhibited an excellent effect of inhibiting progerin expression and excellent effect of inhibiting binding between progerin and lamin A, and it has been confirmed that the novel decursin derivative prolongs the survival period of animal models in which progerin was induced.
Type:
Application
Filed:
April 25, 2018
Publication date:
February 13, 2020
Applicant:
PRG S&TECH INC.
Inventors:
Bum Joon PARK, Gyu Yong SONG, Yu Seok O, Jee Hyun LEE, Eun Ju YUN