US2011009459A1PendingUtilityA1

Epothilone derivatives

Assignee: NOVARTIS AGPriority: Mar 16, 2004Filed: Sep 21, 2010Published: Jan 13, 2011
Est. expiryMar 16, 2024(expired)· nominal 20-yr term from priority
C07D 493/04A61P 35/00C07D 405/04C07D 417/06
51
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Claims

Abstract

Epothilone derivatives of Formula (I) and their use as a pharmaceutical.

Claims

exact text as granted — not AI-modified
1 . A compound of formula I 
       
         
           
           
               
               
           
         
         wherein 
       
       
         
           
           
               
               
           
         
         R 1  is 
         R 2  is methyl or hydrogen; 
         R 3  is hydrogen; 
         Z is O; 
            is a single or double bond between C2 and C3; 
       
       or salts thereof. 
     
     
         2 - 3 . (canceled) 
     
     
         4 . The compound of formula I according to  claim 1  selected from the group consisting of,
 3-(1,2-Dimethyl-1H-benzoimidazol-5-yl)-11-hydroxy-8,8,10,12-tetramethyl-4,17-dioxa-bicyclo[14.1.0]heptadecane-5,9-dione; 
 (1S,3S,10R,11S,12S,16S)-3-(1,2-Dimethyl-1H-benzoimidazol-5-yl)-11-hydroxy-8,8,10,12-tetramethyl-4,17-dioxa-bicyclo[14.1.0]heptadecane-5,9-dione; 
 3-(1,2-Dimethyl-1H-benzoimidazol-5-yl)-7,11-dihydroxy-8,8,10,12-tetramethyl-4,17-dioxa-bicyclo[14.1.0]heptadecane-5,9-dione; 
 (1S,3S,7S,10R,11S,12S,16S)-3-(1,2-Dimethyl-1H-benzoimidazol-5-yl)-7,11-dihydroxy-8,8,10,12-tetramethyl-4,17-dioxa-bicyclo[14.1.0]heptadecane-5,9-dione; and 
 (E)-(1S,3S,10R,11S,12S,16S)-3-(1,2-Dimethyl-1H-benzoimidazol-5-yl)-11-hydroxy-8,8,10,12-tetramethyl-4,17-dioxa-bicyclo[14.1.0]heptadec-6-ene-5,9-dione. 
 
     
     
         5 . A pharmaceutical composition, comprising a compound of  claim 1 , or a salt thereof, provided that salt-forming groups are present, and one or more pharmaceutically acceptable carriers. 
     
     
         6 - 9 . (canceled)

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