US2021380588A1PendingUtilityA1

Novel Compounds and Uses Thereof

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Assignee: KALA PHARMACEUTICALS INCPriority: May 30, 2013Filed: Feb 2, 2021Published: Dec 9, 2021
Est. expiryMay 30, 2033(~6.9 yrs left)· nominal 20-yr term from priority
A61P 29/00A61P 37/06A61P 7/10A61P 35/00C07D 487/04A61P 3/10A61P 9/10A61P 27/02C07D 519/00
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Claims

Abstract

The present invention provides novel compounds of any one of Formulae (I)-(IV), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of any one of Formulae (I)-(IV) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor signaling pathway (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.

Claims

exact text as granted — not AI-modified
1 - 195 . (canceled) 
     
     
         196 . A compound having the formula: 
       
         
           
           
               
               
           
         
         or a pharmaceutically acceptable salt thereof. 
       
     
     
         197 - 216 . (canceled) 
     
     
         217 . A method of treating an ocular disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the compound of  claim 196 . 
     
     
         218 . A method of inhibiting signaling of a growth factor in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the compound of  claim 196 . 
     
     
         219 . The method of  claim 218 , wherein the growth factor is a vascular endothelial growth factor. 
     
     
         220 . A method of treating a disease associated with abnormal angiogenesis in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the compound of  claim 196 . 
     
     
         221 . A pharmaceutical composition, comprising the compound of  claim 196  and a pharmaceutically acceptable excipient. 
     
     
         222 . A method of treating an ocular disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of  claim 221 . 
     
     
         223 . A method of inhibiting signaling of a growth factor in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of  claim 221 . 
     
     
         224 . The method of  claim 223 , wherein the growth factor is a vascular endothelial growth factor. 
     
     
         225 . A method of treating a disease associated with abnormal angiogenesis in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of  claim 221 . 
     
     
         226 . A composition, comprising the compound of claim  1 . 
     
     
         227 . A method of treating an ocular disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the composition of  claim 226 . 
     
     
         228 . A method of inhibiting signaling of a growth factor in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the composition of  claim 226 . 
     
     
         229 . The method of  claim 228 , wherein the growth factor is a vascular endothelial growth factor. 
     
     
         230 . A method of treating a disease associated with abnormal angiogenesis in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the composition of  claim 226 . 
     
     
         231 . A pharmaceutical composition, comprising the compound of  claim 196  and a pharmaceutically acceptable excipient,
 wherein the pharmaceutical composition is formulated for enteral, parenteral, intravenous, intramuscular, intra-arterial, intramedullary, intrathecal, subcutaneous, intraventricular, transdermal, interdermal, rectal, intravaginal, intraperitoneal, topical, mucosal, nasal, bucal, sublingual, intratracheal, or bronchial administration. 
 
     
     
         232 . A method of treating an ocular disease in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of  claim 231 . 
     
     
         233 . A method of inhibiting signaling of a growth factor in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of  claim 231 . 
     
     
         234 . The method of  claim 233 , wherein the growth factor is a vascular endothelial growth factor. 
     
     
         235 . A method of treating a disease associated with abnormal angiogenesis in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition of  claim 231 .

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