# US 11,433,090 B2 · mTOR-inhibitor-containing medicine for treating or preventing ophthalmic symptoms, disorders, or diseases, and application thereof > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,433,090 B2 - Document ID: US11433090B2 - Status: Granted - Kind: B2 - Application number: 16/621,881 - Filed: 2018-06-15 - Published: 2020-04-16 - Granted: 2022-09-06 - Earliest claimed: 2017-06-16 - Assignees: The Doshisha - Applicants: The Doshisha - Inventors: Noriko Koizumi; Naoki Okumura - Web page: https://patentgrep.com/patent/US11433090B2 ## CPC - A61K 31/711: Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links - A61K 31/436: the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin - A61K 31/7088: Compounds having three or more nucleosides or nucleotides - A61K 31/7105: Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links - A61K 45/00: Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00 - A61P 27/02: Ophthalmic agents - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention provides a medicine and a method for preventing or treating ophthalmic symptoms, disorders, or diseases. The present invention provides an mTOR-inhibitor-containing composition for preventing or treating ophthalmic symptoms, disorders, or diseases. In some of the embodiments of the present invention, this composition is capable of treating or preventing corneal endothelial symptoms, disorders, or diseases; in particular, corneal endothelial symptoms, disorders, or diseases that are attributed to overexpression of the transforming growth factor-β (TGF-β) signal and/or extracellular matrix (ECM). ## Claims ### Claim 1 A method for preventing or treating an eye condition, disorder, or disease in a subject, wherein the method comprises administering an effective amount of an mTOR inhibitor to the subject, wherein the eye condition, disorder, or disease is a corneal endothelial condition, disorder, or disease due to a transforming growth factor-β (TGF-β). ### Claim 2 (depends on 1) The method of claim 1, wherein the corneal endothelial condition, disorder, or disease is selected from the group consisting of Fuchs' endothelial corneal dystrophy, post-corneal transplant disorder, corneal endotheliitis, trauma, ophthalmic surgery, post-ophthalmic laser surgery disorder, aging, posterior polymorphous dystrophy (PPD), congenital hereditary endothelial dystrophy (CHED), idiopathic corneal endothelial disorder, and cytomegalovirus corneal endotheliitis. ### Claim 3 (depends on 1) The method of claim 1, wherein the corneal endothelial condition, disorder, or disease is due to overexpression of extracellular matrix (ECM). ### Claim 4 (depends on 3) The method of claim 3, wherein the corneal endothelial condition, disorder, or disease is selected from the group consisting of Fuchs' endothelial corneal dystrophy, guttae formation, hypertrophy of a Descemet's membrane, hypertrophy of a cornea, turbidity, scar, corneal nebula, corneal macula, leucoma, photophobia, and blurred vision. ### Claim 5 (depends on 1) The method of claim 1, wherein the condition, disorder, or disease comprises Fuchs' endothelial corneal dystrophy. ### Claim 6 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is selected from the group consisting of rapamycin, temsirolimus, everolimus, PI-103, CC-223, INK128, AZD8055, KU 0063794, Voxtalisib, Ridaforolimus, NVP-BEZ235, CZ415, Torkinib, Torin 1, Omipalisib, OSI-027, PF-04691502, Apitolisib, WYE-354, Vistusertib, Torin 2, Tacrolimus, GSK1059615, Gedatolisib, WYE-125132, BGT226, Palomid 529, PP121, WYE-687, CH5132799, WAY-600, ETP-46464, GDC-0349, XL388, Zotarolimus, and Chrysophanic Acid. ### Claim 7 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is selected from the group consisting of rapamycin, temsirolimus, and everolimus. ### Claim 8 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is administered as an eye drop. ### Claim 9 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is rapamycin and is administered as an eye drop at least about 0.1 nM. ### Claim 10 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is administered as an eye drop, wherein the mTOR inhibitor is rapamycin and is present in the eye drop at least about 0.1 mM. ### Claim 11 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is temsirolimus and is administered as an eye drop at least about 0.01 nM. ### Claim 12 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is administered as an eye drop, wherein the mTOR inhibitor is temsirolimus and is present in the eye drop at least about 0.01 mM. ### Claim 13 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is everolimus and is administered as an eye drop at least about 0.1 nM. ### Claim 14 (depends on 1) The method of claim 1, wherein the mTOR inhibitor is administered as an eye drop, wherein the mTOR inhibitor is everolimus and is present in the eye drop at least about 0.1 mM. ### Claim 15 A method for preventing or treating an eye condition, disorder, or disease in a subject, wherein the method consists essentially of administering an effective amount of an mTOR inhibitor to the subject, wherein the eye condition, disorder, or disease is a corneal endothelial condition, disorder, or disease due to a transforming growth factor-β (TGF-β). ### Claim 16 (depends on 15) The method of claim 15, wherein the mTOR inhibitor is rapamycin.