COMPOSITIONS AND METHODS FOR TREATING OR PREVENTING PNEUMOVIRUS INFECTION AND ASSOCIATED DISEASES

摘要

The present invention provides novel crystalline polymorphic forms of MDT-637, in particular, crystalline polymorphic forms with physicochemical properties specifically suited for drug production, amorphous formation, composite form, and methods of preparation thereof. The novel polymorphs described herein are useful for the treatment of respiratory disease, such as disease caused by respiratory syncytial virus.

主权项

1. A composition comprising at least one polymorph of MDT-637 selected from the group consisting of:
P-2 hydrate crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 4.83°, 8.42°, 9.61°, 11.83°, 14.60°, 16.94°, 19.25°, 20.46°, 24.09°, 24.85°, 27.76° and 28.56°; P-3 monohydrate crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 8.25°, 9.55°, 11.66°, 14.30°, 18.03°, 19.70°, 20.29°, 24.55°, 25.29°, 26.31° and 27.26°; P-3 dihydrate crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 7.03°, 8.16°, double peak at 9.47° and 9.75°, 11.60°, 14.24°, 17.95°, 19.64°, 20.26°, 24.52°, 26.24° and 27.25°; P-3 ethanolate crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 8.25, 9.54, 9.85, 11.69, 14.32, 15.99, 18.06, 19.73, 20.33, 24.54, and 26.27; P-3 monohydrate crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 8.25°, 9.55, 11.66, 14.30, 18.03, 19.70, 20.29, 24.55, 25.29, 26.31 and 27.26; P-3 anhydrous crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 8.27°, 9.54°, 11.68°, 14.29°, 18.07°, 19.79°, 20.30°, 24.54°, 25.27°, 26.36°, and 27.25°; P-2 anhydrous crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 8.58°, 10.64°, 12.58°, 14.51°, 15.89°, 17.20°, 21.06°, 21.41°, 22.37°, 25.43° and 27.62°; P-4 crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 4.31°, 7.99°, 9.37°, 11.02°, 13.04°, 13.43°, 14.18°, 16.13°, 16.70°, 17.08°, 17.42° and 17.92°; P-6 crystal form having characteristic powder X-ray diffraction peaks at 2θ values of double peak at 3.43° and 3.89°, 6.89°, double peak at 7.87° and 8.25°, 10.88°, 13.06°, 13.81°, 16.12°, 17.38° and 18.51°; P-7 crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 5.18°, 6.59°, 7.70°, double peak at 10.02° and 10.62°, double peak at 12.18° and 12.50°, 15.16°, double peak at 15.88° and 16.4°, double peak at 17.20° and 17.42°, and double peak at 18.07° and 18.25°; P-8 crystal form having characteristic powder X-ray diffraction peaks at 2θ values of 4.15°, 7.85°, 9.33°, 14.29°, triple peak at 15.84°, 16.68° and 17.14°, 18.53°, 20.27°, 23.90°, 24.80° and 27.39°; and combinations thereof.