US2021205222A1PendingUtilityA1

Dexamethasone prodrug compositions and uses thereof

Assignee: RIPPLE THERAPEUTICS CORPPriority: Feb 2, 2018Filed: Jan 8, 2021Published: Jul 8, 2021
Est. expiryFeb 2, 2038(~11.5 yrs left)· nominal 20-yr term from priority
C07J 9/005A61K 47/55A61K 47/6921A61K 47/554C07J 5/00A61K 9/50A61K 31/573A61K 9/0024A61K 9/7007A61K 47/6953A61P 29/00A61L 27/54A61K 9/0051A61K 9/0092A61K 9/5089A61K 9/1682A61K 9/0048A61K 9/5192A61K 9/167A61K 9/51A61K 47/54A61P 27/02C07J 7/0055
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Claims

Abstract

The disclosure features dexamethasone prodrug dimers of dexamethasone and pharmaceutical compositions thereof useful for, e.g., the extended release of a drug and for the treatment of a disease or condition.

Claims

exact text as granted — not AI-modified
1 - 30 . (canceled) 
     
     
         31 . A coating comprising a compound having a structure represented by formula (I): 
       
         
           
           
               
               
           
         
         wherein:
 n is an integer from 1 to 6, 
 
         or a pharmaceutically salt or solvate thereof. 
       
     
     
         32 . The coating of  claim 31 , wherein at least 70% (w/w) of the coating is the compound. 
     
     
         33 . The coating of  claim 32 , wherein at least 90% (w/w) of the coating is the compound. 
     
     
         34 . The coating of  claim 31 , wherein n is an integer from 3-5. 
     
     
         35 . The coating of  claim 34 , wherein the compound has a structure represented by: 
       
         
           
           
               
               
           
         
       
     
     
         36 . The coating of  claim 31 , wherein the compound or dexamethasone in its free form is released from the coating through surface erosion. 
     
     
         37 . The coating of  claim 31 , wherein less than or equal to 10% of dexamethasone, as a percentage of the total dexamethasone present in the coating, is released from the coating at 37° C. in 100% bovine serum over a period of at least 5 days. 
     
     
         38 . The coating of  claim 31 , wherein less than or equal to 2% of dexamethasone, as a percentage of the total dexamethasone present in the coating, is released from the coating at 37° C. in PBS over a period of at least 5 days. 
     
     
         39 . The coating of  claim 31 , wherein more than or equal to 20% of dexamethasone, as a percentage of the total dexamethasone present in the coating, is released from the coating at 37° C. in 100% bovine serum over a period of at least 6 days. 
     
     
         40 . The coating of  claim 31 , wherein dexamethasone is released from the coating at 37° C. in 100% bovine serum or at 37° C. in phosphate buffered saline (PBS) at a rate such that t 10  is greater than or equal to 1/10 of t 50 . 
     
     
         41 . The coating of  claim 31 , wherein the coating resides on the surface of an implantable device. 
     
     
         42 . The coating of  claim 31 , wherein the coating resides on the surface of a minimally invasive glaucoma surgery (MIGS) device. 
     
     
         43 . A method of treating inflammation in a subject, the method comprising administering to the subject an implantable device comprising a coating in an amount sufficient to treat inflammation in the subject, wherein the coating comprises a compound having a structure represented by formula (I): 
       
         
           
           
               
               
           
         
         wherein:
 n is an integer from 1 to 6, 
 
         or a pharmaceutically salt or solvate thereof. 
       
     
     
         44 . The method of  claim 43 , wherein the inflammation is post-surgical inflammation. 
     
     
         45 . The method of  claim 43 , wherein at least 70% (w/w) of the coating is the compound. 
     
     
         46 . The method of  claim 45 , wherein at least 90% (w/w) of the coating is the compound. 
     
     
         47 . The method of  claim 43 , wherein the compound has a structure represented by: 
       
         
           
           
               
               
           
         
       
     
     
         48 . The method of  claim 43 , wherein the implantable device is administered locally to the subject. 
     
     
         49 . The method of  claim 48 , wherein the implantable device is administered in the eye of the subject. 
     
     
         50 . The method of  claim 48 , wherein the implantable device is administered into a joint space of the subject.

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