Tanaproget derivatives, metabolites, and uses thereof

Abstract

A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.

What is claimed is: 
     
         1 . A method for detecting metabolites of tanaproget in a sample, said method comprising:
 (a) isolating said metabolite of tanaproget in said sample;   (b) characterizing said metabolite of tanaproget to determine the structure of said metabolite of tanaproget; and   (c) comparing said structure to the structures of synthetic N- and S-glucuronide derivatives of tanaproget.   
     
     
         2 . The method according to  claim 1 , wherein said synthetic glucuronide derivative of tanaproget is an S-glucuronide derivative. 
     
     
         3 . The method according to  claim 1 , wherein said synthetic glucuronide derivative of tanaproget is an N-glucuronide derivative. 
     
     
         4 . An antibody generated using a synthetic glucuronide derivative of tanaproget, said antibody being specific for tanaproget or a derivative thereof. 
     
     
         5 . The antibody according to  claim 4 , wherein said synthetic glucuronide derivative of tanaproget is an S-glucuronide derivative. 
     
     
         6 . The antibody according to  claim 4 , wherein said synthetic glucuronide derivative of tanaproget is an N-glucuronide derivative. 
     
     
         7 . A kit for monitoring therapy with tanaproget, said kit comprising an antibody according to  claim 6 . 
     
     
         8 . A method for detecting metabolites of tanaproget, said method comprising detecting binding to an antibody according to  claim 6 . 
     
     
         9 . A method for detecting metabolites of tanaproget, said method comprising comparison of a sample to a tanaproget derivative selected from the group consisting of:
 (a) an enzymatically derived tanaproget glucuronide derivative;   (b) tanaproget having a sulfate moiety located on the thiocarbonyl group;   (c) tanaproget having a hydroxy group located on the pyrrole ring;   (d) tanaproget having a hydroxy group located on the phenylpyrrole ring; and   (e) tanaproget having a carbamate located on the thiocarbonyl group.   
     
     
         10 . An antibody generated using a tanaproget derivative selected from the group consisting of:
 (a) an enzymatically derived tanaproget glucuronide derivative;   (b) tanaproget having a sulfate moiety located on the thiocarbonyl group;   (c) tanaproget having a hydroxy group located on the pyrrole ring;   (d) tanaproget having a hydroxy group located on the phenylpyrrole ring; and   (e) tanaproget having a carbamate located on the thiocarbonyl group.   
     
     
         11 . A kit for monitoring therapy with tanaproget, said kit comprising an antibody according to  claim 10 . 
     
     
         12 . A method for detecting metabolites of tanaproget, said method comprising detecting binding to an antibody according to  claim 10 . 
     
     
         13 . A composition comprising a pharmaceutically acceptable carrier and a synthetic glucuronide derivative of tanaproget. 
     
     
         14 . The composition according to  claim 13 , wherein said synthetic glucuronide derivative of tanaproget is an S-glucuronide derivative. 
     
     
         15 . The composition according to  claim 13 , wherein said synthetic glucuronide derivative of tanaproget is an N-glucuronide derivative.