US2021355136A1PendingUtilityA1

Crystalline forms of therapeutic compounds and uses thereof

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Assignee: KALA PHARMACEUTICALS INCPriority: Sep 8, 2016Filed: Jul 29, 2021Published: Nov 18, 2021
Est. expirySep 8, 2036(~10.2 yrs left)· nominal 20-yr term from priority
C07D 491/107A61P 35/00A61K 31/506C07D 519/00A61P 27/02C07B 2200/13A61P 43/00
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Claims

Abstract

Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
         1 . A crystalline form of Compound 1: 
       
         
           
           
               
               
           
         
         wherein the crystalline form has an X-ray powder diffraction (XRPD) pattern with a largest peak at about 8-9 degrees 2θ. 
       
     
     
         2 . The compound of  claim 1  wherein the crystalline form is an anhydrate. 
     
     
         3 . A process for preparing a crystalline form of either of  claim 1  or  claim 2 , comprising mixing Compound 1 and ethyl acetate. 
     
     
         4 . A pharmaceutical composition comprising the crystalline form of either of  claim 1  or  claim 2  and a pharmaceutically acceptable carrier. 
     
     
         5 . The pharmaceutical composition of  claim 4 , wherein the pharmaceutical composition is suitable for topical administration. 
     
     
         6 . The pharmaceutical composition of  claim 4 , wherein the pharmaceutical composition is suitable for injection. 
     
     
         7 . The pharmaceutical composition of any one of  claims 4 ,  5  or  6 , wherein the pharmaceutical composition is suitable for delivery to the eye. 
     
     
         8 . A kit comprising the crystalline form of any one of  claims 1 ,  2 , or  3 , or the pharmaceutical composition of any one of  claims 4 ,  5 ,  6 , or  7 . 
     
     
         9 . A method of treating a disease comprising administering to a subject in need thereof a therapeutically effective amount of the crystalline form of any one of  claims 1  or  2  or the pharmaceutical composition of any one of  claims 4 ,  5 ,  6 , or  7 . 
     
     
         10 . The method of  claim 9 , wherein the disease is a proliferative disease. 
     
     
         11 . The method of  claim 8 , wherein the disease is cancer. 
     
     
         12 . The method of  claim 9 , wherein the disease is an ocular disease. 
     
     
         13 . The method of  claim 9 , wherein the disease is retinopathy. 
     
     
         14 . The method of  claim 9 , wherein the disease is age-related macular degeneration (AMD). 
     
     
         15 . The method of  claim 9 , wherein the disease is corneal neovascularization. 
     
     
         16 . A method of inhibiting growth factor signaling comprising administering to a subject a therapeutically effective amount of the crystalline form of any one of  claims 1  or  2  or the pharmaceutical composition of any one of  claims 4 ,  5 ,  6 , or  7 .

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