US2022073500A1PendingUtilityA1

Crystalline pharmaceutical and methods of preparation and use thereof

76
Assignee: NOVARTIS PHARMACEUTICALS CORPPriority: Apr 15, 2008Filed: May 18, 2021Published: Mar 10, 2022
Est. expiryApr 15, 2028(~1.8 yrs left)· nominal 20-yr term from priority
C07D 217/02A61K 9/06A61K 9/08A61K 47/10A61P 27/14A61K 45/06A61P 29/00C07D 217/26C07D 405/10A61K 31/4709A61K 31/4725C07D 217/04A61K 47/22A61K 47/38A61K 47/183A61K 47/02A61P 17/14A61K 47/14C07C 317/48A61P 11/06A61P 17/02C07D 405/06A61P 17/00A61K 47/06A61P 17/06A61P 11/02A61P 27/02A61P 17/08A61P 27/04
76
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Claims

Abstract

Novel crystalline polymorphic forms, Forms A, B, C, D, and E of a compound of Formula I, which has been found to be a potent inhibitor of LFA-1, are disclosed. Methods of preparation and uses thereof in the treatment of LFA-1 mediated diseases are also disclosed in this invention.

Claims

exact text as granted — not AI-modified
1 - 67 . (canceled) 
     
     
         68 . A method of treating diabetic retinopathy or diabetic macular edema in a subject in need thereof, comprising administering to the subject an effective amount of a composition comprising an isolated compound of Formula I: 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof, wherein said compound comprises a purity of greater than about 90 percent. 
     
     
         69 . The method of  claim 68 , wherein said compound has a purity of greater than about 98 percent. 
     
     
         70 . The method of  claim 68 , wherein said compound comprises at least about 95 percent of an S-enantiomer. 
     
     
         71 . The method of  claim 68 , wherein said compound is a sodium salt. 
     
     
         72 . The method of  claim 68 , wherein the subject suffers from diabetic retinopathy. 
     
     
         73 . The method of  claim 68 , wherein the subject suffers from diabetic macular edema.

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