Griseofulvin compound and pharmaceutical use thereof
US-11993593-B2 · May 28, 2024 · US
US9795586B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9795586-B2 |
| Application number | US-201715464178-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 20, 2017 |
| Priority date | Jan 5, 2015 |
| Publication date | Oct 24, 2017 |
| Grant date | Oct 24, 2017 |
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Provided is a hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist and a use thereof. The HNF4-α antagonist selected in the present invention was confirmed to specifically bind to the ligand binding domain of HNF4-α, thereby inhibiting the activity of HNF4-α. The HNF4-α antagonist of the present invention can significantly reduce the expression of Wnt5a in a specific manner compared to that of the conventional known HNF4-α antagonists, and can also inhibit the growth of gastric cancer cells. Therefore, the HNF4-α antagonist of the present invention can not only be used as a pharmaceutical composition or a health functional food for preventing and treating cancer but can also be applied to a composition for treating or preventing diseases occurring due to the overexpression of HNF4-α.
Opening claim text (preview).
What is claimed is: 1. A method for inhibiting activity of hepatocyte nuclear factor 4 alpha (HNF4-α) comprising administering an effective amount of a HNF4-α antagonist comprising a compound of the following Formula 1 or salts thereof to a subject in need of inhibition of HNF4-α activity: wherein R 1 to R 5 are each independently a hydrogen atom (H), a nitro group (NO 2 ), a halogen atom, a C 1-6 alkyl group substituted with one to six identical or different halogen atoms, or a C 1-6 alkyl group. 2. The method of claim 1 , wherein the compound of the Formula 1 is defined by the following Formula 3: 3. A method for treating gastric cancer comprising administering an effective amount of a hepatocyte nuclear factor 4 alpha (HNF4-α) antagonist comprising a compound of the following Formula 3 or salts thereof to a subject in need of gastric cancer treatment:
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having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole · CPC title
having five-membered rings · CPC title
Antineoplastic agents · CPC title
Coumarins, e.g. psoralen · CPC title
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