Isarna Therapeutics Gmbh

Michel Janicot

Eugen Uhlmann

Frank Jaschinski

Eugen Leo

Petra Fettes

Katja Wosikowski-Buters

The present invention is directed to an oligonucleotide comprising a nucleic acid sequence of SEQ ID No. 1 or parts thereof, wherein 1 to 4 nucleotides at the 3'-end and/or at the 5&#x2032;-end of the oligonucleotide are modified at a base, a sugar and/or a phosphate for use in a method of reducing or inhibiting of scarring, of fibrotic closure of the trabeculectomy canal, of epithelial-to-mesenchymal transition of the trabecular meshwork and/or providing of protecting activity of the optic nerve optionally the optic nerve head. Further, the present invention refers to a pharmaceutical composition comprising such oligonucleotide and a pharmaceutically acceptable carrier.

TGF-beta oligonucleotide for use in treatment of ophthalmic diseases

The invention refers to an oligonucleotide consisting of 10 to 20 nucleotides of selected regions of the TGF-beta1, TGF-beta2 or TGF-beta3 nucleic acid sequence, which comprises modified nucleotides such as LNA, ENA, polyalkylene oxide-, 2'-fluoro, 2&#x2032;-O-methoxy and/or 2&#x2032;-O-methyl modified nucleotides. The selected regions are preferably the region of nucleic acid no. 1380 to 1510, no. 1660 to 1680, no. 2390 to 2410, or no. 2740 to 2810 of the TGF-beta2 nucleic acid sequence of SEQ ID NO. 1, specific regions of the TGF-beta1 nucleic acid sequence of SEQ ID NO. 149, or specific regions of the TGF-beta3 nucleic acid sequence of SEQ ID No. 267. The invention further relates to pharmaceutical compositions comprising such oligonucleotide, wherein the composition or the oligonucleotide is used in the prevention and/or treatment of a malignant and/or benign tumor, an immunologic disease, fibrosis, glaucoma, etc.

Modified TGF-beta oligonucleotides

The invention refers to an oligonucleotide consisting of 10 to 20 nucleotides of selected regions of the TGF-beta1, TGF-beta2 or TGF-beta3 nucleic acid sequence, which comprises modified nucleotides such as LNA, ENA, polyalkylene oxide-, 2'-fluoro, 2&#x2032;-O-methoxy and/or 2&#x2032;-O-methyl modified nucleotides. The invention further relates to pharmaceutical compositions comprising such oligonucleotide, wherein the composition or the oligonucleotide is used in a method for the prevention and/or treatment of glaucoma, posterior capsular opacification, dry eye, Marfan or Loeys-Dietz syndrome, riboblastoma, choroidcarcinoma, macular degeneration, such as age-related macular degeneration, diabetic macular endma, or cataract.

Modified TGF-beta oligonucleotide for use in a method of preventing and/or treating an ophthalmic disease

The invention refers to an oligonucleotide consisting of 10 to 18 nucleotides of selected regions of the TGF-beta2 nucleic acid sequence, which comprises modified nucleotides such as LNA, ENA, polyalkylene oxide-, 2'-fluoro, 2&#x2032;-O-methoxy and/or 2&#x2032;-O-methyl modified nucleotides. The invention further relates to pharmaceutical compositions comprising such oligonucleotide, wherein the composition or the oligonucleotide is used in the prevention and/or treatment of a malignant and/or benign tumor, an immunologic disease, fibrosis, or an ophthalmic disease such as dry eye, glaucoma or posterior capsular opacification (PCO).

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Brussels, Belgium

Michel Janicot