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Details for Patent: 9,340,516

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Details for Patent: 9,340,516

Title:Form-II crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl) acetamide, method for producing the same, and use thereof
Abstract: Form-II crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide and a method of producing the crystal are provided. The Form-II crystal exhibits diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2.theta. when the spectrum is obtained by using Cu K.alpha. radiation: 9.0 degrees, 12.9 degrees, 20.7 degrees, and 22.6 degrees. The Form-II crystal can be produced by crystallizing the subject compound from an alcoholic solvent, a ketone solvent, a saturated hydrocarbon solvent, an ether solvent, water, or a mixture of these solvents. The crystal may be administered as an active ingredient to a subject for the purpose of treating or preventing certain diseases, disorders, and symptoms, or for promoting angiogenesis or gene therapy. The targeted diseases and disorders include transient ischemic attack, diabetic neuropathy, diabetic gangrene, peripheral circulatory disturbance, connective tissue disease, reocclusion/restenosis after percutaneous transluminal coronary angioplasty, arteriosclerosis, thrombosis, hypertension, pulmonary hypertension, and diabetic nephropathy.
Inventor(s): Itou; Hideyuki (Kyoto, JP)
Assignee: NIPPON SHINYAKU COMPANY, LTD. (Kyoto, JP)
Filing Date:Jan 22, 2014
Application Number:14/160,699
Claims:1. A crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide, showing diffraction peaks in its X-ray powder diffraction spectrum at least at the following angles of diffraction 2.theta.: 9.0 degrees, 12.9 degrees, 20.7 degrees and 22.6 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 treating diabetic neuropathy, diabetic gangrene, peripheral circulatory disturbance, chronic arterial occlusion, intermittent claudication, scleroderma, thrombosis, pulmonary hypertension, myocardial infarction, angina, glomerulonephritis, diabetic nephropathy, chronic renal failure, bronchial asthma, interstitial pneumonia (pulmonary fibrosis), chronic obstructive pulmonary disease, inflammatory bowel disease, or symptoms associated with spinal canal stenosis, comprising the step of administering the crystal of claim 1 as an active ingredient to a subject.

4. The method according to claim 3, wherein the method is for treating peripheral circulatory disturbance.

5. The method according to claim 3, wherein the method is for treating chronic arterial occlusion.

6. The method according to claim 3, wherein the method is for treating intermittent claudication.

7. The method according to claim 3, wherein the method is for treating scleroderma.

8. The method according to claim 3, wherein the method is for treating pulmonary hypertension.

9. The method according to claim 3, wherein the method is for treating pulmonary fibrosis.

10. The method according to claim 3, wherein the method is for treating symptoms associated with spinal canal stenosis.

11. The method according to claim 3, wherein the method is for treating chronic renal failure.
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