Crystalline antifungal polymorph
OwnerDavid R. Andrews, William Leong +1inventors
InventorsDavid R. Andrews, William Leong, Anantha Sudhakar
Life of this patent
Estimating the term…
Abstract
The crystalline polymorph Form I of (−)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by the formula I pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed.
Claims5
A crystalline polymorph form I of(−)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]-methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by formula I
- and characterized by the following x-ray powder diffraction pattern expressed in terms of “d” spacing and relative intensities(“RI”):
- d spacing (±0.04) RI 6.10 Medium 4.63 Medium 4.10 Wide 3.69 Wide 3.05 Wide
A crystalline polymorph form I of(−)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)furan-3-yl]-methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihydro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one characterized by the following x-ray powder diffraction pattern expressed(Table 1) in terms of “d” spacing and relative intensities(“RI”) (S=strong, M=medium, W=weak, V=very and D=diffuse)
- TABLE 1 relative d spacing intensity 22.14 VWD 12.27 VWD 11.37 M 10.35 VWD 8.85 M 7.90 VWD 7.52 W 6.77 W 6.10 M 5.82 M 5.63 M 5.52 M 5.41 M 5.17 W 4.95 VS 4.84 M 4.63 M 4.54 M 4.42 S 4.29 VWD 4.23 WD 4.10 W 4.02 WD 3.98 M 3.86 W 3.82 W 3.76 W 3.69 W 3.63 W 3.47 M 3.45 WD 3.36 W 3.30 VW 3.24 VWD 3.21 WD 3.17 VWD 3.14 VWD 3.05 W 2.99 VWD 2.95 VWD 2.90 VWD 2.87 VWD 2.84 VWD 2.77 VWD 2.72 WD 2.67 VWD 2.65 VWD 2.61 VWD 2.58 VWD 2.52 VWD 2.48 VWD 2.44 VWD 2.41 VWD 2.35 VWD 2.34 VWD 2.28 VWD 2.26 VWD
Dependencies are inferred from the claim text.