US2005131008A1PendingUtilityA1

42-O-alkoxyalkyl rapamycin derivatives and compositions comprising same

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Assignee: SUN BIOMEDICAL LTDPriority: Nov 12, 2003Filed: Nov 12, 2004Published: Jun 16, 2005
Est. expiryNov 12, 2023(expired)· nominal 20-yr term from priority
Inventors:Ronald E. BettsDouglas R. SavageJohn E. Shulze
A61P 37/00A61P 37/06C07D 498/18
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Claims

Abstract

42-O-alkoxyalkyl derivatives of rapamycin having biological activity are described. Compositions and delivery devices comprising the 42-O-alkoxyalkyl rapamycin derivatives are also disclosed.

Claims

exact text as granted — not AI-modified
1 . A compound of the form:  
       
         
           
           
               
               
           
         
       
       wherein R is R a —O—R b , where R a  is C 2-6  alkylene and R b  is C 1-5  alkyl, and where the number of carbon atoms in the sum of R a  and R b  is 7 or fewer.  
     
     
         2 . The compound according to  claim 1 , wherein R is of the form —(CH 2 ) n —O—(CH 2 ) m H, where n is from 2 to 6 and m is from 1 to 5.  
     
     
         3 . The compound according to  claim 2 , wherein n is 2-5 and m is 1-4.  
     
     
         4 . The compound according to  claim 2 , wherein n is 2 and m is 1 or 2.  
     
     
         5 . The compound according to  claim 2 , wherein n is 2 and m is 1.  
     
     
         6 . The compound according to  claim 2 , wherein n is 2 and m is 2.  
     
     
         7 . The compound according to  claim 1 , wherein the number of carbon atoms in the sum of R a  and R b  is 6 or fewer.  
     
     
         8 . The compound according to  claim 1 , wherein the number of carbon atoms in the sum of R a  and R b  is 5 or fewer.  
     
     
         9 . The compound according to  claim 1 , wherein the number of carbon atoms in the sum of R a  and R b  is 4 or fewer.  
     
     
         10 . A composition comprising a compound according to  claim 1  together with a carrier.  
     
     
         11 . The composition according to  claim 10 , wherein said carrier is a pharmaceutical preparation having the form of an ointment or a gel.  
     
     
         12 . The composition according to  claim 10 , wherein said carrier is comprised of polymer microparticles.  
     
     
         13 . The composition according to  claim 10 , wherein said carrier is a pharmaceutical preparation having the form of a liquid, tablet, or suppository.  
     
     
         14 . The composition according to  claim 10  wherein said carrier is a stent.  
     
     
         15 . The composition according to  claim 14  wherein said stent is formed of metal or polymer.  
     
     
         16 . The composition according to  claim 15  wherein said stent is formed of a biodegradable polymer.  
     
     
         17 . The composition according to  claim 15 , wherein said stent is metal and said compound is carried directly on the surface of the stent.  
     
     
         18 . The composition according to  claim 15 , where said compound is carried in a polymer layer in contact with said stent.  
     
     
         19 . The composition according to  claim 16 , where said compound is carried in a polymer layer in contact with said stent.  
     
     
         20 . A stent for use in treating restenosis, comprising 
 an expandable stent body; and    carried on said stent body for release therefrom at a controlled rate, a compound of the form                          wherein R is R a —O—R b , where R a  is C 2-6  alkylene and R b  is C 1-5  alkyl, and where the number of carbon atoms in the sum of R a  and R b  is 7 or fewer.    
     
     
         21 . The stent according to  claim 20 , wherein R is of the form —(CH 2 ) n —O—(CH 2 ) m H, where n is from 2 to 6 and m is from 1 to 5.  
     
     
         22 . The stent according to  claim 21 , wherein n is 2-5 and m is 1-4.  
     
     
         23 . The stent according to  claim 21 , wherein n is 2 and m is 1 or 2.  
     
     
         24 . The stent according to  claim 21 , wherein n is 2 and m is 1.  
     
     
         25 . The stent according to  claim 20 , wherein the number of carbon atoms in the sum of R a  and R b  is 6 or fewer.  
     
     
         26 . The stent according to  claim 20 , wherein the number of carbon atoms in the sum of R a  and R b  is 5 or fewer.  
     
     
         27 . The stent according to  claim 20 , wherein the number of carbon atoms in the sum of R a  and R b  is 4 or fewer.  
     
     
         28 . The stent according to  claim 20 , wherein said stent body is comprised of metal or polymer.  
     
     
         29 . The stent according to  claim 28 , wherein said stent body is comprised of a biodegradable polymer.  
     
     
         30 . The stent according to  claim 20 , wherein said stent further includes a polymer layer in contact with said stent body and said compound incorporated into said polymer layer.  
     
     
         31 . The stent according to  claim 30 , wherein said polymer layer is comprised of a biodegradable polymer.  
     
     
         32 . The stent according to  claim 30 , further comprising a polymer underlayer disposed between the stent body and the polymer layer.  
     
     
         33 . The stent according to  claim 20 , wherein said stent body has a surface, and wherein said surface is treated to enhance adhesion of said compound relative to a stent surface with no treatment.  
     
     
         34 . The stent according to  claim 33 , wherein said stent surface is treated with a nitric acid solution.  
     
     
         35 . The stent according to  claim 33 , wherein said stent surface is treated by a process selected from sand blasting, laser etching, and chemical etching.  
     
     
         36 . The stent according to  claim 20 , wherein said compound is applied to the stent from a solution of the compound in an organic solvent.  
     
     
         37 . The stent according to  claim 36 , where a membrane is applied over the compound to control bioavailability of the compound.  
     
     
         38 . The stent according to  claim 36 , where a polymer underlayer is in contact with the stent, and the compound/polymer film is in contact with the polymer underlayer.  
     
     
         39 . The stent according to  claim 38 , where the polymer underlayer is polytetrafluoroethylene (Teflon) or poly(dichloro-para-xylylene) (Parylene).  
     
     
         40 . The stent of  claim 37 , where the membrane is a polymer membrane.  
     
     
         41 . The stent according to  claim 36 , wherein said solution is applied to the stent by a technique selected from the group consisting of brushing, spraying, dipping, and flowing.  
     
     
         42 . The stent according to  claim 36 , wherein said compound forms a glassy layer on the stent.  
     
     
         43 . The stent according to  claim 36 , wherein said solution is comprised of between about 2 and 60% by weight compound, remainder solvent.  
     
     
         44 . The stent according to  claim 43 , wherein said solvent is ethyl acetate.  
     
     
         45 . A method of treating a condition responsive to treatment by rapamycin, comprising 
 administering a compound according to  claim 1 .    
     
     
         46 . A method of treating restenosis, comprising 
 providing a stent according to  claim 20.

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