IP Library › Patent Application 12563788
Patent Application
App. No. 12/563,788

CRYSTALLINE FORMS OF A BIPHENYL COMPOUND

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Quick Facts
Patent No.
US None
App. No.
12/563,788
Abstract

The invention provides crystalline forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester, and pharmaceutically acceptable solvates thereof. The crystalline form can be a freebase, or a salt such as a diphosphate, monosulfate or dioxalate salt. The invention also provides pharmaceutical compositions comprising these crystalline compounds or prepared using these compounds; processes and intermediates for preparing the crystalline compounds; and methods of using these compounds to treat a pulmonary disorder.

Claims (6)

1 - 54 . (canceled)

55 . A composition comprising a crystalline salt of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester and phosphoric acid in a 1:2 molar ratio characterized by a powder x-ray diffraction pattern comprising diffraction peaks at 2θ values of 15.0±0.2, 19.4±0.2, 21.6±0.2, and 23.7±0.2, and water.

56 . The composition of claim 55 , wherein the powder x-ray diffraction pattern further comprises diffraction peaks at 2θ values selected from 6.4±0.2, 7.6±0.2, 8.6±0.2, 13.7±0.2, 22.1±0.2, and 22.9±0.2.

57 . The composition of claim 55 , wherein the crystalline salt is further characterized by a differential scanning calorimetry trace which shows a maximum endothermic heat flow at about 154.5° C.

58 . The composition of claim 55 , wherein the composition comprises about 6.2 weight percent of water.

59 . The composition of claim 55 , wherein the composition comprises about 6.5 weight percent of water.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 3, 2014
From: THERAVANCE, INC.
To: THERAVANCE BIOPHARMA R&D IP, LLC
Reel/Frame 033127/0174 →