US2005124810A1PendingUtilityA1

Crystalline pharmaceutical

65
Priority: Mar 30, 2000Filed: Nov 9, 2004Published: Jun 9, 2005
Est. expiryMar 30, 2020(expired)· nominal 20-yr term from priority
Inventors:Daniel A. DickmanSanjay R. ChemburkarJames J. FortRodger F. HenryDavid Lechuga-BallesterosYuping NiuWilliam Porter
A61K 9/4866C07D 239/10A61K 47/44A61P 31/18A61K 31/513A61K 31/00A61K 47/10
65
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Claims

Abstract

New crystalline forms of lopinavir are disclosed.

Claims

exact text as granted — not AI-modified
1 . A crystalline hydrated form of lopinavir.  
     
     
         2 . The crystalline form of lopinavir of  claim 1  with a peak in the solid state infrared spectrum at a position within the range 1652-1666 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1606-1615 cm −1 .  
     
     
         3 . A substantially pure crystalline hydrated form of lopinavir.  
     
     
         4 . The crystalline form of lopinavir of  claim 3  with a peak in the solid state infrared spectrum at a position within the range 1652-1666 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1606-1615 cm −1 .  
     
     
         5 . A solvated crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1661-1673 cm −1 , a peak in the solid state infrared spectrum at a position within the range 1645-1653 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1619-1629 cm −1 .  
     
     
         6 . A substantially pure solvated crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1645-1673 cm −1 , a peak in the solid infrared spectrum at a position within the range 1645-1653 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1619-1629 cm −1 .  
     
     
         7 . A crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1 .  
     
     
         8 . A crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1636-1647 cm −1 .  
     
     
         9 . A substantially pure crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1 .  
     
     
         10 . A substantially pure crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1636-1647 cm −1 .  
     
     
         11 . A solvated crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1 .  
     
     
         12 . A solvated crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1636-1647 cm −1 .  
     
     
         13 . A substantially pure solvated crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1 .  
     
     
         14 . A substantially pure solvated crystalline form of lopinavir with a peak in the solid state infrared spectrum at a position within the range 1655-1662 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1636-1647 cm −1 .  
     
     
         15 . A non-solvated crystalline form of lopinavir.  
     
     
         16 . The crystalline form of lopinavir of  claim 15  with a peak in the solid state infrared spectrum at a position within the range 1680-1685 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1625-1630 cm −1 .  
     
     
         17 . The crystalline form of lopinavir of  claim 15  with characteristic peaks in the ponder X-ray diffraction pattern at values of two theta of 6.85°±0.1°, 9.14°±0.1°, 12.88°±0.1°, 15.09°±0.1°, 17.74°±0.1°, 18.01°±0.1° and 18.53°±0.1°.  
     
     
         18 . The crystalline form of lopinavir of  claim 15  with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 6.85°±0.1°, 9.14°±0.1°, 10.80°±0.1°, 12.04°±0.1°, 12.88°±0.1°, 15.09°±0.1°, 17.74°±0.1°, 18.01°±0.1°, 18.26°±0.1°, 18.53°±0.1°, 20.47°±0.1° and 25.35°±0.1°.  
     
     
         19 . A substantially pure non-solvated crystalline form of lopinavir.  
     
     
         20 . The crystalline form of lopinavir of  claim 19  with a peak in the solid state infrared spectrum at a position within the range 1680-1685 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1625-1630 cm −1 .  
     
     
         21 . The crystalline form of lopinavir of  claim 19  with a peak in the solid state infrared spectrum at a position within the range 1680-1685 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1668-1674 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1656-1662 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1642-1648 cm −1  and a peak in the solid state infrared spectrum at a position within the range 1625-1630 cm −1 .  
     
     
         22 . The crystalline form of lopinavir of  claim 19  with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 6.85°±0.1°, 9.14°±0.1°, 12.88°±0.1°, 15.09°±0.1°, 17.74°±0.1°, 18.01°±0.1° and 18.53°±0.1°.  
     
     
         23 . The crystalline form of lopinavir of  claim 19  with characteristic peaks in the powder X-ray diffraction pattern at values of two theta of 6.85°±0.1°, 9.14°±0.1°, 10.80°±0.1°, 12.04°±0.1°, 12.88°±0.1°, 15.09°±0.1°, 17.74°±0.1°, 18.01°±0.1°, 18.26°±0.1°, 18.53°±0.1°, 20.47°±0.1° and 25.35°±0.1°.

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