HNF4-α antagonist and use thereof

US9795586B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-9795586-B2
Application numberUS-201715464178-A
CountryUS
Kind codeB2
Filing dateMar 20, 2017
Priority dateJan 5, 2015
Publication dateOct 24, 2017
Grant dateOct 24, 2017

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  6. CPC / IPC classifications

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  7. Citations and related patents

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Abstract

Official abstract text for this publication.

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.

First claim

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:

Assignees

Inventors

Classifications

  • A61K31/343Primary

    condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone · CPC title

  • 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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What does patent US9795586B2 cover?
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…
Who is the assignee on this patent?
Nat Cancer Ct
What technology area does this patent fall under?
Primary CPC classification A61K31/343. Mapped technology areas include Human Necessities.
When was this patent published?
Publication date Tue Oct 24 2017 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).