US2021206764A1PendingUtilityA1

2-azabicyclo hexane jak inhibitor compound

Assignee: THERAVANCE BIOPHARMA R&D IP LLCPriority: Oct 29, 2018Filed: Mar 1, 2021Published: Jul 8, 2021
Est. expiryOct 29, 2038(~12.2 yrs left)· nominal 20-yr term from priority
C07D 471/04A61P 27/02A61K 9/0019A61K 9/0048A61K 31/437
64
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Claims

Abstract

The invention provides a compound of formula 1or a pharmaceutically-acceptable salt thereof, that is useful as a JAK inhibitor. The invention also provides pharmaceutical compositions comprising the compound, methods of using the compound to treat diseases amenable to a JAK inhibitor, and processes useful for preparing the compound.

Claims

exact text as granted — not AI-modified
1 - 16 . (canceled) 
     
     
         17 . A method of treating an ocular disease in a mammal, the method comprising administering a pharmaceutical composition comprising a compound of the formula 1: 
       
         
           
           
               
               
           
         
         or a pharmaceutically-acceptable salt thereof, and a pharmaceutically-acceptable carrier, to the eye of the mammal. 
       
     
     
         18 . The method of  claim 17 , wherein the ocular disease is selected from the group consisting of uveitis, diabetic retinopathy, diabetic macular edema, dry eye disease, age-related macular degeneration, retinal vein occlusion, and atopic keratoconjunctivitis. 
     
     
         19 . The method of  claim 18 , wherein the ocular disease is diabetic macular edema. 
     
     
         20 . The method of  claim 18 , wherein the ocular disease is uveitis. 
     
     
         21 . The method of  claim 18 , wherein the ocular disease is diabetic retinopathy. 
     
     
         22 . The method of  claim 18 , wherein the ocular disease is dry eye disease. 
     
     
         23 . The method of  claim 18 , wherein the ocular disease is age-related macular degeneration 
     
     
         24 . The method of  claim 18 , wherein the ocular disease is retinal vein occlusion. 
     
     
         25 . The method of  claim 18 , wherein the ocular disease is atopic keratoconjunctivitis. 
     
     
         26 . The method of  claim 18 , wherein the pharmaceutical composition is administered by injection. 
     
     
         27 . The method of  claim 18 , wherein the pharmaceutical composition is administered by intravitreal injection. 
     
     
         28 . The method of  claim 18 , wherein the pharmaceutical composition is a suspension. 
     
     
         29 . The method of  claim 18 , wherein the pharmaceutical composition is a crystalline suspension. 
     
     
         30 . The method of  claim 18 , wherein the mammal is a human. 
     
     
         31 . The method of  claim 18 , wherein the compound of formula 1 is administered as a free base. 
     
     
         32 . The method of  claim 18 , wherein the compound of formula 1 is administered as a pharmaceutically-acceptable salt. 
     
     
         33 . The method of  claim 18 , wherein the pharmaceutical composition contains from 0.01 to 95% by weight of the compound of formula 1, or a pharmaceutically-acceptable salt thereof. 
     
     
         34 . The method of  claim 18 , wherein the pharmaceutical composition contains from 0.05 to 30% by weight of the compound of formula 1, or a pharmaceutically-acceptable salt thereof. 
     
     
         35 . The method of  claim 18 , wherein the pharmaceutical composition contains from 0.1% to 10% by weight of the compound of formula 1, or a pharmaceutically-acceptable salt thereof.

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