Process for preparation of pyrroles having hypolipidemic hypocholesteremic activities

Abstract

The present invention provides pyrroles having hypolipidemic hypocholesteremic activities. The invention provides saroglitazar and its pharmaceutically acceptable salts, hydrates, solvates, polymorphs or intermediates thereof. The invention also provides a process for the preparation of saroglitazar. The invention further provides intermediates as well process for preparation thereof.

1 - 23 . (canceled) 
     
     
         24 . A substantially amorphous form of saroglitazar magnesium having a purity of at least about 98% by area percentage of HPLC and less than about 0.5% of residual solvents by GC analysis, wherein the residual solvents comprise one or more of cyclohexane, tetrahydrofuran, ethanol, n-butyl acetate, methylene dichloride, and n-heptane. 
     
     
         25 . A substantially amorphous form of saroglitazar magnesium having a purity of at least about 98% by area percentage of HPLC and one or more of the following:
 (i) a chiral purity of at least 99% by area percentage of HPLC; or   (ii) less than about 0.5% of residual solvents by GC analysis.   
     
     
         26 . A pharmaceutical composition comprising a substantially amorphous form of saroglitazar magnesium having a purity of at least about 98% by area percentage of HPLC and one or more of the following:
 (i) a chiral purity of at least 99% by area percentage of HPLC;   (ii) less than about 0.5% of residual solvents by GC analysis.   
     
     
         27 . A pharmaceutical composition comprising a substantially amorphous form of saroglitazar magnesium comprising less than about 25% of crystalline saroglitazar magnesium. 
     
     
         28 . The pharmaceutical composition according to  claim 27 , wherein the substantially amorphous form of saroglitazar magnesium is characterized by an x-ray powder diffraction pattern substantially the same as that shown in  FIG. 1 . 
     
     
         29 . The pharmaceutical composition according to  claim 27 , wherein the composition comprises the substantially amorphous form of saroglitazar magnesium together with one or more pharmaceutically acceptable carriers, excipients, or diluents. 
     
     
         30 . The pharmaceutical composition according to  claim 27 , wherein the composition is in the form of a tablet, a capsule, a pill, a liquid, a suspension, an emulsion, a granule, a suppository, or an injection preparation. 
     
     
         31 . A substantially amorphous form of saroglitazar magnesium having less than about 25% of crystalline saroglitazar magnesium. 
     
     
         32 . A substantially amorphous form of saroglitazar magnesium having a particle size distribution of one or more of the following:
 (a) D(10) of about 10 μm or less;   (b) D(50) of about 25 μm or less; and   (c) D(90) of about 100 μm or less.