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Generated: October 15, 2018

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Details for Patent: 9,440,931

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Title:Form-III crystal of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide and use thereof
Abstract: Form-III 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-III 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: 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees, and 23.5 degrees. The Form-III crystal can be produced by crystallizing the subject compound from an ester solvent or an aromatic hydrocarbon solvent. 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): Nakamichi; Koji (Kashihara, JP), Tosaka; Takashi (Kyoto, JP)
Assignee: NIPPON SHINYAKU CO., LTD. (Kyoto, JP)
Filing Date:Jun 09, 2015
Application Number:14/734,012
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.: 9.3 degrees, 9.7 degrees, 16.8 degrees, 20.6 degrees, and 23.5 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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Merck
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Queensland Health
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Julphar

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