Claims for Patent: 10,676,440
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Summary for Patent: 10,676,440
| 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 (Lugano/Pazzallo, CH) |
| Application Number: | 16/259,913 |
| Patent Claims: |
1. A non-solvated 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 having an X-ray powder diffraction pattern comprising the following peak, in terms of 2.theta.: 11.5.degree..+-.0.2.degree..
2. The crystalline form of claim 1, having an X-ray powder diffraction pattern further comprising the following peak, in terms of 2.theta.: 13.1.degree..+-.0.2.degree.. 3. A pharmaceutical composition comprising a non-solvated 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)pyri din-3-yl)propanamide, having an X-ray powder diffraction pattern comprising the following peak, in terms of 2.theta.: 11.5.degree..+-.0.2.degree. and one or more pharmaceutically acceptable excipients. 4. The pharmaceutical composition of claim 3, wherein the crystalline form further has an X-ray powder diffraction pattern comprising the following peak, in terms of 2.theta.: 13.1.degree..+-.0.2.degree.. 5. The compound of claim 1 wherein said compound comprises less than 0.5% impurities. 6. The pharmaceutical composition of claim 3, wherein the compound is in the form of particles wherein at least 90% of the particles are greater than 0.01 microns and less than 500 microns. 7. The pharmaceutical composition of claim 3, wherein the compound is in the form of particles wherein at least 90% of the particles are greater than 0.1 microns and less than 100 microns. 8. The pharmaceutical composition of claim 3 wherein said compound comprises less than 0.5% impurities. 9. 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 one of the following peak, in terms of 2.theta.: 11.5.degree..+-.0.2.degree., wherein the compound is in the form of particles wherein at least 90% of the particles are greater than 0.01 microns and less than 500 microns. 10. The crystalline form of claim 9, having an X-ray powder diffraction pattern further comprising a peak, in terms of 20 at 4.5.degree..+-.0.2.degree.. 11. The crystalline form of claim 9, having an X-ray powder diffraction pattern further comprising the following peak, in terms of 2.theta.: 13.1.degree..+-.0.2.degree.. 12. The crystalline form of claim 9, wherein the compound is in the form of particles wherein at least 90% of the particles are greater than 0.1 microns and less than 100 microns. 13. The crystalline form of claim 9, wherein said compound comprises less than 0.5% impurities. |
