US2023310402A1PendingUtilityA1

Corneal endothelium ecm therapeutic medicaments

Assignee: KYOTO PREFECTURAL PUBLIC UNIV CORPPriority: Jul 30, 2013Filed: Jun 7, 2023Published: Oct 5, 2023
Est. expiryJul 30, 2033(~7 yrs left)· nominal 20-yr term from priority
A61K 31/4439A61K 39/395A61K 31/519A61K 31/4725A61K 31/4745A61K 31/4709A61K 31/4402A61K 45/06A61K 9/0048C12N 15/1136C12N 2310/14C12N 2320/30A61P 27/02A61P 43/00
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Claims

Abstract

The present invention provides medicaments for treating or preventing a disease, disorder, or condition associated with extracellular matrix (ECM) abnormality in a corneal endothelium, wherein the medicaments comprise a TGF-beta signal inhibiting agent. More specifically, this disease, disorder, or condition is a disorder associated with Fuchs' endothelial corneal dystrophy. Such a disorder includes photophobia, blurred vision, vision disorder, eye pain, lacrimation, hyperemia, pain, bullous keratopathy, ophthalmic unpleasantness, a decrease in contrast, glare, edema in corneal stroma, bullous keratopathy, corneal opacity, and the like. A preferable TGF-beta signal inhibiting agent includes 4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide.

Claims

exact text as granted — not AI-modified
1 . A medicament for treating or preventing a disease, disorder, or condition associated with extracellular matrix (ECM) abnormality in a corneal endothelium, wherein the medicament comprises an effective amount of a TGF-beta signal inhibiting agent. 
     
     
         2 . The medicament for treating or preventing according to  claim 1 , wherein the disease, disorder, or condition is a disorder related to Fuchs' endothelial corneal dystrophy. 
     
     
         3 . The medicament for treating or preventing according to  claim 1 , wherein the disease, disorder, or condition comprises at least one selected from the group consisting of photophobia, blurred vision, vision disorder, eye pain, lacrimation, hyperemia, pain, bullous keratopathy, ophthalmic unpleasantness, a decrease in contrast, glare, edema in corneal stroma, bullous keratopathy, and corneal opacity in Fuchs' endothelial corneal dystrophy. 
     
     
         4 . The medicament for treating or preventing according to  claim 1 , wherein the TGF-beta signal inhibiting agent comprises at least one of 4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide, BMP-7, anti-TGF-beta antibody, anti-TGF-beta receptor antibody, siRNA of TGF-beta, siRNA of a TGF-beta receptor, shRNA of TGF-beta, shRNA of a TGF-beta receptor, an aptamer of TGF-beta, an aptamer of a TGF-beta receptor, an antisense oligonucleotide of TGF-beta, 6,7-dimethoxy-2-((2E)-3-(1-methyl-2-phenyl-1H-pyrrolo[2,3-b]pyridine-3-yl-prop-2-enoyl))-1,2,3,4-tetrahydroisoquinolone, 3-(6-methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, 2-(3-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl)-1,5-naphthyridine, 6-(4-(piperidin-1-yl)ethoxy)phenyl)-3-(pyridin-4-yl)pyrazolo[1,5-a]pyrimidine, 2-(5-chloro-2-fluorophenyl)-4-[(4-pyridinyl)amino]pteridine, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-quinoline, pharmaceutically acceptable salts or solvates thereof, or solvates of the pharmaceutically acceptable salts. 
     
     
         5 . The medicament for treating or preventing according to  claim 1 , wherein the TGF-beta signal inhibiting agent comprises 4-[4-(1,3-benzodioxol-5-yl)-5-(2-pyridinyl)-1H-imidazol-2-yl]benzamide or a pharmaceutically acceptable salt thereof. 
     
     
         6 . The medicament for treating or preventing according to  claim 1 , wherein the corneal endothelium is of a primate. 
     
     
         7 . The medicament for treating or preventing according to  claim 1 , wherein the corneal endothelium is of a human. 
     
     
         8 . The medicament for treating or preventing according to  claim 1 , comprising an additional medicinal component. 
     
     
         9 . The medicament for treating or preventing according to  claim 1 , being eye-drops.

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