➤ Get the DrugPatentWatch Daily Briefing

Get Daily Updates on Generic Entry, Litigation, Biosimilars, and more …

Serving leading biopharmaceutical companies globally:

Colorcon
Johnson and Johnson
Harvard Business School
Medtronic
AstraZeneca
Express Scripts

Last Updated: September 21, 2021

DrugPatentWatch Database Preview

Claims for Patent: 9,951,016


Email this page to a colleague

« Back to Dashboard

Summary for Patent: 9,951,016
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:14/865,370
Patent Claims: 1. A micronized non-solvated crystalline 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 which comprises less than 1% impurities and exhibits an XRPD pattern substantially as shown in FIG. 28.

2. The crystalline form of claim 1 which is substantially isolated and micronized.

3. A micronized pharmaceutical composition comprising a non-solvated crystalline free-base form of the compound 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridine-3-yl)propanamide which comprises less than 1% impurities and exhibits an XRPD pattern substantially as shown in FIG. 28, and one or more pharmaceutically acceptable excipients.

4. A crystalline form of a trifluoroethanol solvate of the compound 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridine-3-yl)propanamide which is Form II.

5. A crystalline form of a formate salt of the compound 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridine-3-yl)propanamide which is Form III.

6. The pharmaceutical composition of claim 3, in the form of a tablet, pill, powder, lozenge, sachet, cachet, elixir, suspension, emulsion, solution, syrup, aerosol, ointment, soft or hard gelatin capsule, suppository, sterile injectable solution, or sterile packaged powder.

7. The pharmaceutical composition of claim 3, in the form of a tablet or capsule.

8. The compound of claim 1, 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.

9. The compound of claim 1, 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.

10. The 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.

11. The 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.

12. The compound of claim 1 wherein said non-solvated crystalline free-base form of 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridine-3-yl)propanamide comprises less than 0.5% impurities.

13. The composition of claim 3 wherein said non-solvated crystalline free-base form of 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1- -yl)-4-(o-tolyl)pyridine-3-yl)propanamide comprises less than 0.5% impurities.

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

Baxter
McKesson
Mallinckrodt
McKinsey
Colorcon
Harvard Business School

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.