US2006020024A1PendingUtilityA1

TNP-470 species, polymer conjugates and use thereof

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Assignee: CHILDRENS MEDICAL CENTERPriority: Apr 11, 2002Filed: Jul 20, 2005Published: Jan 26, 2006
Est. expiryApr 11, 2022(expired)· nominal 20-yr term from priority
Inventors:Ronit Satchi-FainaroJudah Folkman
A61K 47/58A61P 35/04C07D 303/22A61P 35/00A61P 9/00C08L 53/00C08F 220/56C08F 220/58
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Claims

Abstract

The present invention relates to conjugates of water-soluble polymers and o-(chloracetyl-carbamoyl) fumagillol (TNP-470) and use of those conjugates as specific intracellular carriers of the TNP-470 into tumor vessels. The present invention further relates to use of those conjugates to lower the neurotoxicity of TNP-470. Preferably, the polymer has a molecular weight in the range of 100 Da to 800 kDa. More preferably, the polymer has a molecular weight no greater than 60 kDa. Most preferably, the polymer has a molecular weight in the range of 15 kDa to 40 kDa.

Claims

exact text as granted — not AI-modified
1 . A composition of the formula  
       
         
           
           
               
               
           
         
       
       , wherein R is (CH 2 ) n R′, where n is 1 to 3, R′ is NH 2 , O or S, and its pharmaceutically acceptable salts thereof.  
     
     
         2 . The composition of  claim 1 , wherein R′ is (CH 2 ) 2 NH 2 .  
     
     
         3 . A method of inhibiting angiogenesis in a mammal having undesired angiogenesis comprising administering an effective amount of the composition of  claim 1.

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