Polymorphic forms of (1-{3-[3-(4-cyano-3-methoxy-phenyl) ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester
AssigneeVertex Pharmaceuticals Incorporated
InventorsTodd Blythe, Philip Nyce, Yong Cui
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Abstract
The present invention relates to polymorphic forms of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, processes therein, pharmaceutical compositions thereof, and uses therewith.
Claims26
A polymorphic Form A of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, characterized by one or more peaks at about 5.76, 7.82, 8.10, 10.08, and 15.73 degrees 2θ in an X-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form B of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, characterized by one or more peaks at about 11.72, 14.57, 18.25, 22.40, and 27.72 degrees 2θ in a X-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form C of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, characterized by one or more peaks at about 3.82, 8.5, 10.74, 15.22, 17.02 degrees 2θ in a X-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form D of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester, characterized by one or more peaks at about 6.06, 9.53, and 23.86 degrees 2θ in an X-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form E of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester characterized by one or more peaks at about 5.15, 14.76, 20.86, 24.28, 24.94 degrees 2θ in an X-ray powder diffraction pattern obtained using Cu K alpha radiation.
A polymorphic Form F of (1-{3-[3-(4-cyano-3-methoxy-phenyl)ureido]-phenyl}-ethyl)-carbamic acid-2-cyano-1-ethyl-ethyl ester characterized by one or more peaks at about 7.82, 8.16, 12.93, 19.01, 23.83 degrees 2θ in an X-ray powder diffraction pattern obtained using Cu K alpha radiation.
A method of producing a pharmaceutical composition comprising an amorphous form of Compound 1, comprising the step of:
- (i) converting any one of polymorphic Form A, Form B, Form C, Form D, Form E, or From F to said amorphous form;
- and
- (ii) combining said amorphous form with one or more suitable pharmaceutical carriers or adjuvants.
Dependencies are inferred from the claim text.