NEW PATENT........WO 2015021902, Novel apixaban crystal form and preparation method thereof

 APIXABAN

NEW PATENT       WO-2015021902

	Novel apixaban crystal form and preparation method thereof
	2y-Chem Ltd Apixaban (BMS-562247-01, tradename Eliquis) is an anticoagulant for the treatment of venous thromboembolic events. It is a direct factor Xa inhibitor. Apixaban has been available in Europe since May 2012. An FDA decision on apixaban which was expected on June 28, 2012 was delayed. On August 21, 2014, Pfizer announced that Apixaban was now FDA approved for treatment and secondary prophylaxis of DVT and PE. It is being developed in a joint venture by Pfizer and Bristol-Myers Squibb.
	Novel crystalline polymorphic form A of apixaban, useful for treating venous thromboembolism. Appears to be the first filing by the assignees on this API, which was originally developed and launched by Bristol-Myers Squibb and Pfizer.  Apixaban is protected by two patent families, that from WO0039131 (where it is first disclosed generically as part of the Markush formula) and that from WO03026652 (claimed specifically). Family members of WO03026652 have SPC protection until May 2026 and expire in the US in 2023 with US154 extension.  Disclosed are an apixaban A-type crystal form and a preparation method thereof. A diffraction characteristic peak and a differential scanning calorimetry characteristic peak of X-ray powder thereof are respectively shown in FIG. 1 and FIG. 2. The A-type crystal form in the present invention is stable and nonhygroscopic, has a simple preparation method, and has excellent repetition. The drug also has NCE exclusivity till 2017.
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