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Last Updated: November 22, 2024

Claims for Patent: 10,961,195

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Summary for Patent: 10,961,195

Title:	Crystalline forms of an NK-1 antagonist
Abstract:	The present invention is related to crystalline forms of 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridin-3-yl)propanamide which is an NK-1 antagonist useful in the treatment of induced vomiting and other disorders.
Inventor(s):	Bacilieri; Christian (Breganzona, CH), Frasca; Gionata (Minusio, CH)
Assignee:	Helsinn Healthcare SA (Pazzallo, CH)
Application Number:	16/863,038
Patent Claims:	1. A crystalline micronized free-base form of the compound 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridin-3-yl)propenamide comprising less than 2.5% impurities, having an X-ray powder diffraction pattern comprising a characteristic peak in terms of 2.theta. at 11.5.degree..+-.0.2.degree.. 2. A crystalline micronized free-base form of the compound 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridin-3-yl)propanamide comprising less than 2.5% impurities, having an X-ray powder diffraction pattern comprising a characteristic peak in terms of 2.theta. at 11.5.degree..+-.0.2.degree.. 3. A crystalline micronized free-base form of the compound 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridin-3-yl)propenamide comprising less than 2.5% impurities, having an X-ray powder diffraction pattern comprising a characteristic peak in terms of 2.theta. at 13.1.degree..+-.0.2.degree.. 4. The crystalline form of claim 1, having an X-ray powder diffraction pattern further comprising the following characteristic peak, in terms of 2.theta.: 11.5.degree..+-.0.2.degree.. 5. The crystalline form of claim 1, having an X-ray powder diffraction pattern further comprising the following characteristic peak, in terms of 2.theta.: 13.1.degree..+-.0.2.degree.. 6. The crystalline form of claim 1, having an X-ray powder diffraction pattern further comprising the following characteristic peaks, in terms of 2.theta.: 11.5.degree..+-.0.2.degree.; and 13.1.degree..+-.0.2.degree.. 7. The crystalline form of claim 2, having an X-ray powder diffraction pattern further comprising the following characteristic peaks, in terms of 2.theta.: 13.1.degree..+-.0.2.degree..

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