C7 carbamoyloxy substituted taxane compositions

Abstract

Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.

1 - 164 . (Canceled)  
     
     
         165 . A method of inhibiting tumor growth in a mammal, said method comprising administering a therapeutically effective amount of a pharmaceutical composition comprising at least one pharmaceutically acceptable carrier and a taxane having the formula  
       
         
           
           
               
               
           
         
       
       wherein 
 R 7  is carbamoyloxy;  
 R 10  is hydroxy;  
 X 3  is heterocyclo;  
 X 5  is —COOX 10 ;  
 X 10  is C 1-8  alkyl;  
 Ac is acetyl; and  
 Bz is benzoyl.  
 
     
     
         166 . The method of  claim 165  wherein X 10  is substituted or unsubstitued methyl, ethyl or straight or cyclic propyl, butyl, pentyl or hexyl.  
     
     
         167 . The method of  claim 165  wherein X 10  is branched propyl, pentyl or hexyl.  
     
     
         168 . The method of any of claims  165 - 167  wherein X 3  is furyl, thienyl, pyridyl, oxazolyl, pyrrolyl, indolyl, quinolinyl, or isoquinolinyl.  
     
     
         169 . The method of any of claims  165 - 167  wherein X 3  is oxazolyl, pyrrolyl, indolyl, quinolinyl, isoquinolinyl, thiazolyl or isoxazolyl.  
     
     
         170 . The method of  claim 168  wherein X 3  is 2-furyl, 3-furyl, 2-thienyl, 3-thienyl, 2-pyridyl, 3-pyridyl, or 4-pyridyl.  
     
     
         171 . A taxane having the formula  
       
         
           
           
               
               
           
         
       
       wherein R 7  is R 7 aNHCOO— and R 7a  is ethyl; X 3  is 2-furyl; and X 5  is —COOX 10  and X 10  is t-butoxy.