Pyrimidin-4-yl)oxy)-1h-indole-1-carboxamide derivatives and use thereof

Abstract

This invention relates to certain metabolites of N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide In particular, the present invention relates to pharmaceutical compositions comprising these metabolites, as well as processes for their preparation and their use in the treatment of diseases.

What is claimed: 
     
         1 . A metabolite, or salt thereof, of N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino)methyl)pyrimidin-4-yl)oxy-1H-indole-1-carboxamide selected from 
       
         
           
           
               
               
           
         
       
     
     
         2 . The metabolite, or salt thereof, of  claim 1  wherein the metabolite is: 
       
         
           
           
               
               
           
         
       
     
     
         3 . A pharmaceutical formulation comprising, the metabolite according to  claim 1 , or a salt thereof, and at least one pharmaceutically acceptable excipient. 
     
     
         4 . A method of treating an ocular neovascular disease in a patient, the method comprising the step of administering the metabolite according to  claim 1 , or a salt thereof to the patient in need of therapy. 
     
     
         5 . A use of a metabolite of  claim 1 , or a salt thereof, for the treatment of a disease or disorder in a subject mediated by a protein kinase, especially protein tyrosine kinase, more especially VEGF-R receptor dependent diseases. 
     
     
         6 . Use of a metabolite according  claim 1 , for the treatment of a disorder or disease in a subject characterized by an abnormal activity of a protein kinase, especially protein tyrosine kinase, more especially VEGF-R receptor. 
     
     
         7 . A method of inhibiting VEGF-R activity in a subject, wherein the method comprises administering to the subject a therapeutically effective amount of the metabolite according to  claim 1 . 
     
     
         8 . A method of treating a disorder or a disease in a subject mediated by VEGF-R, wherein the method comprises administering to the subject a therapeutically effective amount of the metabolite according to  claim 1 . 
     
     
         9 . The method of  claim 8 , wherein the disease is AMD or Diabetic Retinopathy.