Nippon Shinyaku Company, Ltd.

Achillion Pharmaceuticals, Inc.

Senthil Kumar Kusalakumari Sukumar

Avinash S Phadke

Akihiro Hashimoto

Pingyun Chen

Joanna Bis

Toshio Fujiwara

A main object of the present invention is to provide new crystals of (S)-N-[1-(4-fluorophenyl)ethyl]-4-(1-methyl-1H-pyrazol-4-yl)-N-(pyrazin-2-yl)pyridine-2,6-diamine maleate (hereinafter, referred to as 'compound A'). A Form-I crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2&#x3b8;: 6.9 degrees, 9.4 degrees, 12.5 degrees, 15.1 degrees, 16.4 degrees, 18.3 degrees, 19.0 degrees, 24.9 degrees, 25.4 degrees, 27.3 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu K&#x3b1; radiation (&#x3bb;=1.54 &#x212b;). A Form-II crystal of the compound A, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2&#x3b8;: 6.9 degrees, 9.2 degrees, 12.4 degrees, 14.8 degrees, 16.5 degrees, 18.1 degrees, 18.5 degrees, 19.8 degrees, 23.6 degrees, 24.9 degrees, and 27.7 degrees, wherein X-ray powder diffraction spectrum is obtained by using Cu K&#x3b1; radiation (&#x3bb;=1.54 &#x212b;).

Crystals

The disclosure provides a crystalline sodium salt of ACH-0142684 comprising a Form A polymorph, a Form B polymorph, a Form C polymorph, a Form D polymorph, a Form E polymorph, a Form F polymorph, a Form G polymorph, a Form H polymorph, a Form I polymorph, or a combination thereof, wherein the Form A, B, C, D, E, F, G, H, and I polymorph exhibits an X-ray powder diffraction pattern having peak locations in accordance with FIGS., and, respectively.

ACH-0142684 sodium salt polymorph, composition including the same, and method of manufacture thereof

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Raleigh, NC, United States of America

Senthil Kumar Kusalakumari Sukumar