IP Library › Granted Patent US 10,500,174
Granted Patent B2
US 10,500,174 · App. 16/361,129 · Granted Dec 10, 2019

Pharmaceutical composition for preventing or treating degenerative brain disease

Inventors: Jungkyun Im (Asan-si, KR); Goutam Biswas (Delhi, IN)
Assignee: SOONCHUNHYANG UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
A61K31/165A23L33/10A61K31/155A61K31/16A61K31/352A61K49/0041A61P25/16A61P25/28A61P29/00C07D311/86A23V2002/00A23V2200/322
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Quick Facts
Patent No.
US 10,500,174
App. No.
16/361,129
Granted
Dec 10, 2019
Kind
B2
Abstract

The present invention relates to an ibuprofen conjugate in which ibuprofen (S-(+)-ibuprofen) is covalently linked to a guanidine-terminal-group-bound sugar alcohol derivative and to a pharmaceutical composition containing the same. The ibuprofen conjugate in which ibuprofen is covalently linked to a guanidine-terminal-group-bound sugar alcohol derivative can more effectively penetrate into the brain by passing through the blood-brain barrier (BBB), thus enabling efficient drug delivery to the brain, whereby administration of the ibuprofen conjugate in an optimal dose can minimize side effects of nonsteroidal anti-inflammatory drugs (NSAIDs) and can prevent or treat degenerative brain disease.

Claims (12)

1. A pharmaceutical composition for treating a brain disease, containing, as an active ingredient, a compound represented by Chemical Formula 1 below:

wherein X is represented by Chemical Formula 2 below:

wherein the R groups are selected from the group consisting of hydrogen, deuterium or Chemical Formula 3 below:

wherein at least one R is Chemical Formula 3, and FITC represents a fluorescein group.

2. The pharmaceutical composition of claim 1 , wherein all of the R groups are represented by Chemical Formula 3.

3. The pharmaceutical composition of claim 1 , wherein the brain disease is selected from the group consisting of stroke, palsy, dementia, Alzheimer's disease, Parkinson's disease, Lou Gehrig's disease, Huntington's disease, Pick's disease, Creutzfeldt-Jakob disease, thrombosis, embolism, transient ischemic attack, lacune, multiple sclerosis, proximal lateral sclerosis, palsy, stroke, mild cognitive impairment, cerebral hemorrhage, cerebral infarction, head trauma, cerebral circulation metabolic disorder, and brain coma.

4. A compound represented by Chemical Formula 1 below:

wherein X is represented by Chemical Formula 2 below:

wherein the R groups are selected from the group consisting of hydrogen, deuterium or Chemical Formula 3 below:

wherein at least one R is chemical formula 3, and FITC represents a fluorescein group.

5. The compound of claim 4 , wherein all of the R groups are represented by Chemical Formula 3.

6. A health functional food composition for treating a degenerative brain disease, comprising the compound of claim 4 .

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 21, 2019
From: IM, JUNGKYUN; BISWAS, GOUTAM
To: SOONCHUNHYANG UNIVERSITY INDUSTRY ACADEMY COOPERATION FOUNDATION
Reel/Frame 048666/0648 →
Priority Claims (1)
KR 10-2016-0121577 · Sep 22, 2016 · national
Continuity (2)
Continuation PCTKR2017000915 · Jan 25, 2017
Related Publication 20190216752A1 · Jul 18, 2019