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Last Updated: December 15, 2024

Claims for Patent: 8,791,122

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Summary for Patent: 8,791,122

Title:	Form-I crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide and method for producing the same
Abstract:	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}-N-(methylsu- lfonyl)acetamide (hereinafter referred to as "compound A"). A Form-I crystal of compound A shows diffraction peaks at 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees in the powder X-ray diffraction spectrum thereof. A Form-II crystal of compound A shows diffraction peaks at 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 degrees in the powder X-ray diffraction spectrum thereof. A Form-III crystal of compound A shows diffraction peaks at 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees and 23.5 degrees in the powder X-ray diffraction spectrum thereof.
Inventor(s):	Itou; Hideyuki (Kyoto, JP)
Assignee:	Nippon Shinyaku Co., Ltd. (Kyoto, JP)
Application Number:	13/379,531
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,791,122
Patent Claims:	1. A crystal of 2-{-4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methyls- ulfonyl)acetamide, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2.theta.: 9.4 degrees, 9.8 degrees, 17.2 degrees and 19.4 degrees, wherein the X-ray powder diffraction diagram is obtained by using Cu K.alpha. radiation. 2. A pharmaceutical composition comprising the crystal of claim 1 as an active ingredient. 3. A method for producing the crystal of claim 1, comprising the steps of dissolving 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide in an alcoholic solvent or a mixed solvent of an alcoholic solvent and a ketone solvent while heating, and subsequently crystallizing 2-{-4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methyls- ulfonyl)acetamide by cooling the solution gradually.

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