US2020345734A1PendingUtilityA1

Methods of treating ocular conditions

Assignee: OYSTER POINT PHARMA INCPriority: Apr 7, 2016Filed: Apr 17, 2020Published: Nov 5, 2020
Est. expiryApr 7, 2036(~9.7 yrs left)· nominal 20-yr term from priority
A61P 27/04A61P 27/02A61K 31/506A61K 9/0043A61K 31/436A61K 45/06A61K 38/13
62
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Claims

Abstract

Described herein are methods and pharmaceutical formulations for treating ocular conditions.

Claims

exact text as granted — not AI-modified
1 - 61 . (canceled) 
     
     
         62 . A method for increasing the amount or concentration of one or more lacrimal proteins produced by an individual in need thereof, comprising local administration of a therapeutically effective amount of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, in alternating nostrils of an individual in need thereof,
 wherein the therapeutically effective amount per dose is between 1 microgram and 5 milligrams of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, per dose.   
     
     
         63 . The method of  claim 62 , wherein the one or more lacrimal proteins are selected from the group consisting of epithelial growth factor, lactoferin, lacritin, prolactin, adrenocorticotropic, leucine enkephalin, ALS2CL, ARHGEF19, KIAA1109, PLXNA1, POLG, WIPI1, ZMIZ2, or other proteins of the tear proteome. 
     
     
         64 . The method of  claim 62 , wherein the pharmaceutically acceptable salt is a citrate salt or a galactarate salt. 
     
     
         65 . The method of  claim 64 , wherein the pharmaceutically acceptable salt is (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine mono-citrate or (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine hemigalactarate. 
     
     
         66 . The method of  claim 64 , wherein the pharmaceutically acceptable salt is (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine hemigalactarate dihydrate or (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine hemigalactarate monohydrate. 
     
     
         67 . The method of  claim 62 , wherein the therapeutically effective amount is between 500 micrograms and 5 milligrams of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, per dose. 
     
     
         68 . The method of  claim 62 , wherein the therapeutically effective amount is between 500 micrograms and 3 milligrams of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, per dose. 
     
     
         69 . The method of  claim 62 , wherein the therapeutically effective amount is between 1 microgram and 2 milligrams of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, per dose. 
     
     
         70 . The method of  claim 62 , wherein the therapeutically effective amount is between 100 micrograms and 1000 micrograms of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, per dose. 
     
     
         71 . The method of  claim 62 , wherein (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered at least once daily. 
     
     
         72 . The method of  claim 62 , wherein (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered at least twice daily. 
     
     
         73 . The method of  claim 62 , wherein (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered as a liquid, suspension, aerosol, gel, ointment, dry powder, cream, paste, lotion, or balm. 
     
     
         74 . The method of  claim 62 , wherein (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered by a syringe, dropper, bottle nebulizer, atomization pump, inhaler, powder spray device, vaporizer, patch, medicated stick, pipette, or jet of liquid. 
     
     
         75 . The method according to  claim 62 , wherein (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered with a medical device. 
     
     
         76 . The method of  claim 62 , wherein the (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered in a pharmaceutical formulation for nasal administration comprising between 10 mg/mL and 25 mg/mL of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof. 
     
     
         77 . The method of  claim 62 , wherein the (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered in a pharmaceutical formulation for nasal administration comprising between 5 mg/mL and 50 mg/mL of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof. 
     
     
         78 . The method of  claim 62 , wherein the (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered in a pharmaceutical formulation for nasal administration comprising about 1 mg/mL, about 5 mg/mL, about 6 mg/mL, or about 10 mg/mL of (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof. 
     
     
         79 . The method of  claim 62 , wherein the (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered prior to or after LASIK eye surgery. 
     
     
         80 . The method according to  claim 62 , wherein the (R)-5-((E)-2-pyrrolidin-3-ylvinyl)pyrimidine, or a pharmaceutically acceptable salt thereof, is administered prior to or after an ophthalmologic surgical procedure.

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