Details for Patent: 6,713,481
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Title: | Crystalline antifungal polymorph |
Abstract: | The crystalline polymorph Form I of (-)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-tri azol-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 ##STR1## pharmaceutical compositions containing such a polymorph and methods of using such a polymorph to treat fungal infections in mammals are disclosed. |
Inventor(s): | Andrews; David R. (Maplewood, NJ), Leong; William (Westfield, NJ), Sudhakar; Anantha (East Brunswick, NJ) |
Assignee: | |
Filing Date: | Oct 05, 1998 |
Application Number: | 09/166,445 |
Claims: | 1. A crystalline polymorph form I of(-)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-t riazol-1-ylmethyl)furan-3-yl]-methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihy dro-2-[(S)-1-ethyl-2(S)-hydroxylpropyl]-3H-1,2,4-triazol-3-one represented by formula I ##STR4## and characterized by the following x-ray powder diffraction pattern expressed in terms of "d" spacing and relative intensities("RI"): 2. A crystalline polymorph form I of(-)-4-[4-[4-[4-[[(2R-cis)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-t riazol-1-ylmethyl)furan-3-yl]-methoxy]phenyl]-1-piperazinyl]phenyl-2,4-dihy dro-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) 3. The crystalline polymorph of the compound of claim 1 further characterized by an infrared spectrum generated on a potassium bromide pellet of said crystalline of polymorph showing the following peaks: 4. A pharmaceutical composition comprising an anti-fungally effective amount of the crystalline polymorph form 1 of claim 1 and a pharmaceutically acceptable carrier. 5. A method of treating and/or preventing fungal infections in a mammal which comprises administering to said mammal an anti-fungally effective amount of the crystalline polymorph form 1 of claim 1. |