Enantiomers of selected fused heterocyclics and uses thereof

Abstract

This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.

1 . A method for treating cancer comprising administering to an animal in need thereof a therapeutically effective amount of (R) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide, or a pharmaceutically acceptable salt thereof, which is substantially free of (S) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide. 
   
   
       2 . The method of  claim 1 , wherein the cancer is selected from the group consisting of a carcinomas of the brain, breast, ovary, lung, colon and prostate, multiple myeloma leukemias, lymphomas, tumors of the central and peripheral nervous system, melanoma, fibrosarcoma, Ewing's sarcoma, and osteosarcoma. 
   
   
       3 . The method of  claim 1 , wherein the cancer is lymphoma. 
   
   
       4 . The method of  claim 1 ,  2 , or  3 , wherein the animal is a human. 
   
   
       5 . The method of  claim 1 , wherein (S) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide is present in an amount of no more than 2% w/w. 
   
   
       6 . The method of  claim 1 , wherein (S) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide is present in an amount of no more than 1% w/w. 
   
   
       7 . A method for the prophylaxis treatment of cancer, comprising administering to an animal in need thereof a therapeutically effective amount of (R) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide, or a pharmaceutically acceptable salt thereof, which is substantially free of (S) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide. 
   
   
       8 . The method of  claim 7 , wherein the animal is human. 
   
   
       9 . The method of  claim 7 , wherein (S) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide is present in an amount of no more than 2% w/w. 
   
   
       10 . The method of  claim 7 , wherein (S) N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-4,5-dihydroisothiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide is present in an amount of no more than 1% w/w.