Nippon Shinyaku Company, Ltd.

Toshio Fujiwara

Joanna Bis

Senthil Kumar Kusalakumari Sukumar

A main object of the present invention is to provide a novel crystal of 2-{4-[N-{5, 6-diphenylpyrazin-2-yl}-N-isopropylamino]butyloxy}acetic acid (hereinafter referred to as 'Compound B').

Crystalline substituted pyrazines as PGI2 receptor agonists

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

A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}acetic acid (hereinafter referred to as 'Compound B'). A form-I crystal of Compound B, which shows peaks at diffraction angles (2&#x3b8;) of 6.4&#xb0;, 8.1&#xb0;, 9.5&#xb0;, 10.9&#xb0;, 13.2&#xb0;, 15.7&#xb0;, 17.0&#xb0;, 19.5&#xb0;, 20.3&#xb0;, 21.0&#xb0;, and 22.8&#xb0; in a powder X-ray diffraction spectrum obtained using a Cu-K&#x3b1; radiation (&#x3bb;=1.54 &#x212b;). A form-II crystal of Compound B, which shows peaks at diffraction angles (2&#x3b8;) of 9.6&#xb0;, 11.4&#xb0;, 11.7&#xb0;, 16.3&#xb0;, 17.5&#xb0;, 18.5&#xb0;, 18.7&#xb0;, 19.9&#xb0;, 20.1&#xb0;, 21.0&#xb0;, and 24.6&#xb0; in a powder X-ray diffraction spectrum obtained using a Cu-K&#x3b1; radiation (&#x3bb;=1.54 &#x212b;).

A main object of the present invention is to provide a novel crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}acetic acid (hereinafter referred to as 'Compound B'). A form-I crystal of Compound B, which shows peaks at diffraction angles (2&#x3b8;) of 6.4&#xb0;, 8.1&#xb0;, 9.5&#xb0;, 10.9&#xb0;, 13.2&#xb0;, 15.7&#xb0;, 17.0&#xb0;, 19.5&#xb0;, 20.3&#xb0;, 21.0&#xb0;, and 22.8&#xb0; in a powder X-ray diffraction spectrum obtained using a Cu-K&#x3b1; radiation (&#x3bb;=1.54 &#x212b;). A form-III crystal of Compound B, which shows peaks at diffraction angles (2&#x3b8;) of 9.6&#xb0;, 11.4&#xb0;, 11.7&#xb0;, 16.3&#xb0;, 17.5&#xb0;, 18.5&#xb0;, 18.7&#xb0;, 19.9&#xb0;, 20.1&#xb0;, 21.0&#xb0;, and 24.6&#xb0; in a powder X-ray diffraction spectrum obtained using a Cu-K&#x3b1; radiation (&#x3bb;=1.54 &#x212b;).

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Paramus, NJ, United States of America

Toshio Fujiwara