Crystalline forms of therapeutic compounds and uses thereof

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.

What is claimed is: 
     
         1 . A method of inhibiting aberrant signaling of a growth factor comprising administering to a subject a therapeutically effective amount of a crystalline form of Compound 1: 
       
         
           
           
               
               
           
         
       
       wherein the crystalline form has an XRPD pattern comprising peaks at 7-8 degrees 2θ, 12.5-13.5 degrees 2θ, 14.5-15.5 degrees 2θ, 17-18 degrees 2θ, and 26-27 degrees 2θ, or
 a pharmaceutical composition comprising the crystalline form. 
 
     
     
         2 . The method of  claim 1 , wherein the growth factor is vascular endothelial growth factor. 
     
     
         3 . The method of  claim 2 , wherein aberrant signaling of a growth factor is associated with a disease selected from cancer, a benign neoplasm, atherosclerosis, hypertension, an inflammatory disease, rheumatoid arthritis, and an ocular disease. 
     
     
         4 . The method of  claim 1 , wherein the crystalline form is a hydrate. 
     
     
         5 . The method of  claim 1 , wherein the pharmaceutical composition is suitable for topical administration. 
     
     
         6 . The method of  claim 3 , wherein the ocular disease is macular edema. 
     
     
         7 . The method of  claim 6 , wherein the ocular disease is a diabetic macular edema or cystoid macular edema. 
     
     
         8 . The method of  claim 7 , wherein the ocular disease is a macular degeneration. 
     
     
         9 . The method of  claim 3 , wherein the ocular disease is a retinal vein occlusion. 
     
     
         10 . The method of  claim 3 , wherein the ocular disease is retinopathy. 
     
     
         11 . The method of  claim 8 , wherein the ocular disease is age-related macular degeneration (AMD). 
     
     
         12 . The method of  claim 3 , wherein the ocular disease is corneal neovascularization. 
     
     
         13 . The method of  claim 3 , wherein the ocular disease is glaucoma. 
     
     
         14 . The method of  claim 3 , wherein the ocular disease is inflammatory meibomian gland disease. 
     
     
         15 . The method of  claim 3 , wherein the ocular disease is dry eye syndrome. 
     
     
         16 . The method of  claim 3 , wherein the ocular disease is blepharitis. 
     
     
         17 . The method of  claim 3 , wherein the ocular disease is uveitis. 
     
     
         18 . The method of  claim 3 , wherein the ocular disease is allergic conjunctivitis. 
     
     
         19 . The method of  claim 3 , wherein the ocular disease is rosacea of the eye. 
     
     
         20 . A kit comprising a crystalline form of Compound 1: 
       
         
           
           
               
               
           
         
       
       wherein the crystalline form has an X-ray powder diffraction (XRPD) pattern comprising peaks at 7-8 degrees 2θ, 12.5-13.5 degrees 2θ, 14.5-15.5 degrees 2θ, 17-18 degrees 2θ, and 26-27 degrees 2θ, or
 a pharmaceutical composition comprising the crystalline form.