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Generated: September 19, 2017

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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 Brunswisk, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Application Number:10/786,886
Patent Claims: 1. A crystalline polymorph Form I of the compound represented by the formula I ##STR4##

and characterized by at least one of the following properties: a melting point range of about 164 to about 165.degree. C. wherein the melting point range is determined using USP Class Ia procedure; a specific rotation equal to [a].sup.25.sub.D =-29.4.degree. wherein the specific rotation is determined using a concentration of 10 mg/ml in methanol; an X-ray powder diffraction pattern substantially similar to that presented in FIG. 1; a differential scanning calorimetry thermogram substantially similar to that presented in FIG. 7; or the proton NMR spectrum substantially similar to that presented in FIG. 10.

2. A pharmaceutical composition comprising an anti-fungally effective amount of the crystalline polymorph form I of claim 1 and a pharmaceutically acceptable carrier.

3. 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 I of claim 1.

4. A crystalline polymorph Form III of the compound represented by the formula I ##STR5##

and characterized by an X-ray powder diffraction pattern displaying d spacing peaks at 28.69, 14.45, 10.59, 7.27, 6.59, 4.14, 3.58, and 3.53 +/-0.04.

5. The crystalline polymorph Form III of claim 4 further characterized by an X-ray powder diffraction pattern substantially similar to that presented in FIG. 3.

6. A pharmaceutical composition comprising an anti-fungally effective amount of the crystalline polymorph Form III of claim 4 and a pharmaceutically acceptable carrier.

7. 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 III of claim 4.
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