IP Library Granted Patent US 7,829,723
Granted Patent B2
US 7,829,723 · App. 12/365,424 · Granted Nov 9, 2010

Polymorphic forms of (S)-1-cyanobutan-2-yl (S)-1-(3-3-(3-methoxy-4-(oxazol-5-yl)phenyl)uriedo)phenyl)ethylcarbamate

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Quick Facts
Patent No.
US 7,829,723
App. No.
12/365,424
Granted
Nov 9, 2010
Kind
B2
Abstract

The present invention relates to polymorphic forms of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, pharmaceutical compositions thereof, processes to prepare therein, and uses therewith.

Claims (10)

1. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate.

2. The polymorphic Form B2 according to claim 1 , wherein the polymorph has a peak position at about 4.1 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

3. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 is characterized by peak positions at about 4.1, 12.6, 14.4, 16.4, 22.1, or 27.1 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

4. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 has a peak position at about 4.1 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

5. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 has a peak position at about 12.6 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

6. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 has a peak position at about 14.4 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

7. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 has a peak position at about 16.4 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

8. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 has a peak position at about 22.1 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

9. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 has a peak position at about 27.1 degrees 2-theta in an x-ray powder diffraction pattern obtained using Cu K alpha radiation.

10. A polymorphic Form B2 of (S)-1-cyanobutan-2-yl (S)-1-(3-(3-(3-methoxy-4-(oxazol-5-yl)phenyl)ureido)phenyl)ethylcarbamate, wherein said polymorphic Form B2 is characterized by an x-ray powder diffraction pattern as shown in FIG. 2 .

Assignments (2)
RELEASE OF SECURITY INTEREST Recorded Oct 14, 2016
From: MACQUARIE US TRADING LLC
To: VERTEX PHARMACEUTICALS INCORPORATED; VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
Reel/Frame 040357/0001 →
SECURITY INTEREST Recorded Jul 10, 2014
From: VERTEX PHARMACEUTICALS INCORPORATED; VERTEX PHARMACEUTICALS (SAN DIEGO) LLC
To: MACQUARIE US TRADING LLC
Reel/Frame 033292/0311 →