Ingenol-derived compounds that can be used for treating cancer

Abstract

The present invention relates to new ingenol derivative compounds for treating cancer. In other aspects, the invention relates to a pharmaceutical composition, medicament, method for treating cancer and dosage form.

1 . An ingenol derivative compound of formula I: 
       
         
           
           
               
               
           
         
         wherein A is phenyl, CH3- or CH 2 ═CH—, and B is —CH═CH—, 
         [CH 2 —] or [—CH 2 —] y    
         where x is an integer ranging between 1 and 10, 
         where y is an integer ranging between 1 and 10, 
         provided that: 
         when A is phenyl, B is —CH═CH—; 
         when A is CH 3 —, B is [—CH 2 —]; 
         when A is CH 2 ═CH—, B is [—CH 2 —] y    
         for treating cancer. 
       
     
     
         2 . The compound according to  claim 1 , wherein the cancer is selected from the group consisting of breast cancer, colorectal cancer, head and neck cancer, brain cancer, prostate cancer, choriocarcinoma, cervical cancer, leukemia, skin cancer, lung cancer, esophageal cancer, pancreatic cancer, bladder cancer, and ovarian cancer. 
     
     
         3 - 15 . (canceled) 
     
     
         16 . The compound according to  claim 1 , wherein x varies between 2 and 6 and y varies between 8 and 10. 
     
     
         17 . The compound according to  claim 1  wherein the compound is selected from the group consisting of 3-cinnamyl-ingenol, 3-hexanoyl-ingenol, 3-dodecanoyl-ingenol, 3-dodeca-11-enoyl-ingenol, and combinations thereof. 
     
     
         18 . The compound according to  claim 1 , wherein the compound is selected from the group consisting of isomers, metabolites, crystals, hydrates, solvates and pharmaceutically acceptable salts of the compound of formula I. 
     
     
         19 . The compound according to  claim 1 , comprising one of the following structures: 
       
         
           
           
               
               
           
         
       
     
     
         20 . A pharmaceutical composition, comprising a compound of formula I and one or more pharmaceutically acceptable excipients. 
     
     
         21 . The pharmaceutical composition, according to  claim 20 , further comprising at least one second active principle other than the compound of formula I. 
     
     
         22 . The pharmaceutical composition, according to  claim 21 , wherein the second active principle is selected from the group consisting of an anti-tumor agent, an anti-retroviral agent, an antibiotic, an anti-cachexia agent, a neurological active principle, an anti-diabetic agent, an antihypertensive agent and proton pump inhibitors. 
     
     
         23 . (canceled) 
     
     
         24 . A medicament comprising at least one compound of formula I, as defined in  claim 1 . 
     
     
         25 - 26 . (canceled) 
     
     
         27 . A method for treating cancer, comprising administering to a patient in need an ingenol derivative according to  claim 1 . 
     
     
         28 . A method for treating cancer, comprising administering to a patient in need thereof the composition according to  claim 20 . 
     
     
         29 . (canceled) 
     
     
         30 . A dosage form for treating cancer, comprising between 0.01 and 5000 mg of an ingenol derivative according to  claim 1 . 
     
     
         31 . A method for treating cancer, comprising administering to a patient in need thereof a medicament according to  claim 24 . 
     
     
         32 . The method for treating cancer according to  claim 27 , wherein the cancer is selected from the group consisting of breast cancer, colorectal cancer, head and neck cancer, brain cancer, prostate cancer, choriocarcinoma, cervical cancer, leukemia, skin cancer, lung cancer, esophageal cancer, pancreatic cancer, bladder cancer, and ovarian cancer.