Process for controlling crystal structure of risedronate

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S277000

Reexamination Certificate

active

07002014

ABSTRACT:
The present invention relates to a process for controlling the crystal form of 3-pyridyl-1-hydroxy-ethylidene-1,1-bisphosphonic acid salt (Risedronate). The process employs a pH adjustment step to induce the proper hydrate form and thereby avoiding inadvertent nucleation of undesired hydrate forms.

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patent: WO01/56983 (2001-08-01), None
Gossman, W.L. et al., “Three Hydrates of the Bisphosphonate Risedronate, Consisting of One Molecular and Two Ionic Structures”,Acta Crystallographica Section C. Crystal Structure Communication, 2003, pp. M33-M36, vol. 50, No. 2.
Nicbolbon et al., “A General Method of Preparation of Tetramethyl Alkyl-1-hydroy-1, 1-diphosphonates”,J. of Organic Chemistry, 1971, vol. 36, No. 24, pp. 3844-3845.
Ebetino et al, “Elucidation of Pharmacophore for the Bisphosphonate Mechanism of Bone Antiresorptive Activity”,Phosphorus, Sulfur, and Silicon, 1996, vols. 109-110, pp. 217-220.
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