Details for Patent: 9,061,019

Title:	Pharmaceutical salts and polymorphs of a factor Xa inhibitor
Abstract:	The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I. ##STR00001##
Inventor(s):	Grant; Craig (Burwell, GB), Kanter; James P. (San Ramon, CA), Langlands; Graeme (Soham, GB)
Assignee:	Millennium Pharmaceuticals, Inc. (Cambridge, MA)
Filing Date:	Feb 17, 2014
Application Number:	14/182,209
Claims:	1. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a salt represented by Formula II: ##STR00014## and aspirin, wherein the salt is a crystalline polymorph comprising a powder X-ray diffraction pattern having at least four characteristic peak locations selected from 4.9.+-.0.2, 9.7.+-.0.2, 13.8.+-.0.2, 14.1.+-.0.2, 15.2.+-.0.2, 17.6.+-.0.2, 18.5.+-.0.2, 20.8.+-.0.2, 21.6.+-.0.2, 22.7.+-.0.2, 24.1.+-.0.2, 26.3.+-.0.2, 26.8.+-.0.2 degrees 2.theta.. 2. The pharmaceutical composition of claim 1 in tablet form. 3. The pharmaceutical composition of claim 1 in capsule form. 4. The pharmaceutical composition of claim 1 in lozenge form. 5. The pharmaceutical composition of claim 1, wherein the salt has a powder X-ray diffraction pattern having at least eight characteristic peak locations selected from 4.9.+-.0.2, 9.7.+-.0.2, 11.8.+-.0.2, 13.8.+-.0.2, 14.1.+-.0.2, 15.2.+-.0.2, 17.6.+-.0.2, 18.5.+-.0.2, 19.9.+-.0.2, 20.8.+-.0.2, 21.6.+-.0.2, 22.7.+-.0.2, 24.1.+-.0.2, 25.0.+-.0.2, 26.3.+-.0.2, 26.8.+-.0.2 degrees 2.theta.. 6. The pharmaceutical composition of claim 1, wherein the salt has a powder X-ray diffraction pattern as shown in FIG. 1A or 1B.