IP Library Granted Patent US 10,961,195
Granted Patent B2
US 10,961,195 · App. 16/863,038 · Granted Mar 30, 2021

Crystalline forms of an NK-1 antagonist

Inventors: Christian Bacilieri (Breganzona, CH); Gionata Frasca (Minusio, CH)
Assignee: Helsinn Healthcare SA
C07D213/75
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Quick Facts
Patent No.
US 10,961,195
App. No.
16/863,038
Granted
Mar 30, 2021
Kind
B2
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.

Claims (7)

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 2θ at 11.5°±0.2°.

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 2θ at 11.5°±0.2°.

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 2θ at 13.1°±0.2°.

4. The crystalline form of claim 1 , having an X-ray powder diffraction pattern further comprising the following characteristic peak, in terms of 2θ: 11.5°±0.2°.

5. The crystalline form of claim 1 , having an X-ray powder diffraction pattern further comprising the following characteristic peak, in terms of 2θ: 13.1°±0.2°.

6. The crystalline form of claim 1 , having an X-ray powder diffraction pattern further comprising the following characteristic peaks, in terms of 2θ: 11.5°±0.2°; and 13.1°±0.2°.

7. The crystalline form of claim 2 , having an X-ray powder diffraction pattern further comprising the following characteristic peaks, in terms of 2θ: 13.1°±0.2°.

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 27, 2024
From: BACILIERI, CHRISTIAN; FRASCA, GIONATA
To: HELSINN HEALTHCARE SA
Reel/Frame 068418/0844 →
SECURITY INTEREST Recorded Aug 27, 2024
From: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
To: HAMIL TON SA LLC
Reel/Frame 068418/0861 →
RELEASE OF SECURITY INTEREST Recorded Aug 27, 2024
From: HAMIL TON SA LLC
To: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; 08830 HELSINN BIREX PHARMACEUTICALS LIMITED
Reel/Frame 068418/0889 →
RELEASE OF SECURITY INTEREST Recorded Sep 20, 2023
From: HAMILTON SA LLC
To: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
Reel/Frame 064961/0567 →
SECURITY INTEREST Recorded Dec 30, 2022
From: HELSINN HEALTHCARE SA; HELSINN THERAPEUTICS (U.S.), INC.; HELSINN BIREX PHARMACEUTICALS LIMITED
To: HAMILTON SA LLC
Reel/Frame 062254/0888 →
Continuity (5)
Continuation 16259913 · Jan 28, 2019
Continuation 15918868 · Mar 12, 2018
Continuation 14865370 · Sep 25, 2015
Provisional Application 62055836 · Sep 26, 2014
Related Publication 20200255381A1 · Aug 13, 2020
Cited By (1)
US 12,606,527