Novel Salts of Raltegravir
AssigneeLupin Limited
InventorsPurna Chandra Ray, Ashok Sopanrao Yadav, Dnyaneshwar Tukaram Singare, Surinder Kumar Arora, Girij Pal Singh
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Abstract
The present invention provides novel salts of raltegravir, viz., meglumine salt, erbumine salt, ammonium salt, tris salt and L-arginine salt of raltegravir and processes for their preparation.
Claims34
Meglumine salt of raltegravir.
A crystalline meglumine salt of raltegravir, represented by formula I,
- which is characterized by XRPD (X-ray powder diffractogram) comprising of peaks expressed as 2θ at 7.9, 8.2, 8.9, 12.4, 13.4, 14.9, 15.9, 17.2, 19.4, 21.5, 21.9, 22.4, 22.8, 25.0, 26.3 and 27.1±0.2 degrees.
Erbumine salt of raltegravir.
A crystalline erbumine salt of raltegravir, represented by formula II,
- which is characterized by XRPD (X-ray powder diffractogram) comprising of peaks expressed as 2θ at 4.2, 8.4, 9.1, 11.7, 12.6, 13.8, 15.2, 16.9, 18.0, 18.4, 18.8, 19.0, 20.8, 21.2, 22.0, 22.4 and 22.7±0.2 degrees.
Ammonium salt of raltegravir.
A crystalline ammonium salt of raltegravir, represented by formula III,
- which is characterized by XRPD (X-ray powder diffractogram) comprising of peaks expressed as 2θ at 6.0, 8.8, 9.9, 11.3, 12.4, 16.2, 17.2, 17.7, 18.7, 19.4, 20.0, 20.8, 21.6, 24.6, 25.4, 26.4±0.2 degrees.
Tris salt of raltegravir.
A crystalline tris salt of raltegravir, represented by formula IV,
- which is characterized by XRPD (X-ray powder diffractogram) which comprises of peaks expressed as 2θ at 7.6, 7.9, 8.1, 11.3, 11.6, 13.4, 14.9, 15.4, 15.8, 15.9, 16.2, 20.0, 22.4, 22.8, 23.3, 23.8, 25.0, 25.3, 26.5, 27.0, 29.2, 29.9, 32.3±0.2 degrees.
L-arginine salt of raltegravir.
An amorphous L-arginine salt of raltegravir, represented by formula V,
- which is characterized by XRPD (X-ray powder diffractogram) which comprises of a single broad peak expressed as 2θ at about 20.2±0.2 degrees.
Dependencies are inferred from the claim text.