IP Library Granted Patent US 8,796,269
Granted Patent B2
US 8,796,269 · App. 13/389,525 · Granted Aug 5, 2014

Crystalline 2-(3,5-Bis(trifluoromethyl)phenyl)-

Inventors: Andrew Simon Craig (Stevenage, GB); Salima Zarah Ismail (Stevenage, GB); Ronnie Maxwell Lawrence (Stevenage, GB)
Assignee: Nerre Therapeutics Limited
C07D498/04
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Quick Facts
Patent No.
US 8,796,269
App. No.
13/389,525
Granted
Aug 5, 2014
Kind
B2
Abstract

The invention relates to the compound of formula (I) in a crystalline anhydrate form, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.

Claims (11)

1. A compound of formula (I):

in a crystalline anhydrate form and having an X-ray powder diffraction pattern comprising 2 theta angle peaks at 7.9°±0.1, 9.8°±0.1, and 10.8°±0.1 which correspond respectively to d-spacing at 11.1, 9.0, and 8.2 Å.

2. The compound according to claim 1 , having substantially the same X-ray powder diffraction pattern as in FIG. 1 .

3. The compound according to claim 1 , having an X-ray powder diffraction pattern comprising 2 theta angle peaks at the following positions: 4.3°±0.1, 7.9°±0.1, 9.8°±0.1, 10.7°±0.1, 10.8°±0.1, 13.3°±0.1, 14.0°±0.1, 15.1±0.1° degrees, which correspond respectively to d-spacing at 20.4, 11.1, 9.0, 8.3, 8.2, 6.6, 6.3 and 5.9 Å.

4. The compound according to claim 1 , having an X-ray powder diffraction pattern comprising 2 theta angle peaks at the following positions: 4.3°±0.1, 7.9°±0.1, 9.8°±0.1, 10.7°±0.1, 10.8°±0.1, 13.1°±0.1, 13.2°±0.1, 13.3°±0.1, 14.0°±0.1, 14.4°±0.1, 15.0°±0.1, 15.1°±0.1, 15.7°±0.1, 15.9°±0.1, 16.3°±0.1, 16.5°±0.1, 16.8°±0.1, 17.0°±0.1, 17.4°±0.1, 17.5°±0.1, 18.1°±0.1, 18.2°±0.1, 18.7°±0.1, 19.4°±0.1, 19.7°±0.1, 20.0°±0.1, 20.1°±0.1, 20.2°±0.1, 20.5°±0.1, 20.7°±0.1, 21.5°±0.1, and 21.8±0.1° degrees, which correspond respectively to d-spacings at 20.4, 11.1, 9.0, 8.3, 8.2, 6.8, 6.7, 6.6, 6.3, 6.1, 5.9, 5.9, 5.6, 5.6, 5.4, 5.4, 5.3, 5.2, 5.1, 5.1, 4.9, 4.9, 4.7, 4.6, 4.5, 4.4, 4.4, 4.4, 4.3, 4.3, 4.1 and 4.1 Å.

5. The compound according to claim 1 , having a 13 C solid state nuclear magnetic resonance spectrum comprising chemical shifts at 175.03±0.2, 163.30±0.2, 158.66±0.2, 156.50±0.2, 149.79±0.2, 148.17±0.2, 146.96±0.2, 139.56±0.2, 133.19±0.2, 132.32±0.2, 129.76±0.2, 126.5±0.2, 124.15±0.2, 120.37±0.2, 119.20±0.2, 118.16±0.2, 112.83±0.2, 70.62±0.2, 67.61±0.2, 64.96±0.2, 59.89±0.2, 57.08±0.2, 55.50±0.2, 52.41±0.2, 48.35±0.2, 40.79±0.2, 32.75 and 21.12±0.2 ppm.

6. A pharmaceutical composition comprising the compound according to claim 1 and a pharmaceutically acceptable carrier and/or diluent.

7. A pharmaceutical composition according to claim 6 further comprising one or more additional pharmaceutically acceptable carriers or diluents.

8. A method for the treatment or prophylaxis of psychotic disorders, depression, mood disorders, anxiety, sleep disorders and alcohol dependence comprising administering to the mammal, an effective amount of the compound according to claim 1 .

9. A compound of formula (I):

in crystalline anhydrate form, having the same 13 C solid state nuclear magnetic resonance spectrum as in FIG. 3 .

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2020
From: NERRE THERAPEUTICS LIMITED
To: KANDY THERAPEUTICS LIMITED
Reel/Frame 054687/0378 →
CHANGE OF ADDRESS Recorded Dec 9, 2020
From: NERRE THERAPEUTICS LIMITED
To: NERRE THERAPEUTICS LIMITED
Reel/Frame 054663/0915 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 12, 2013
From: GLAXOSMITHKLINE LLC
To: NERRE THERAPEUTICS LIMITED
Reel/Frame 029794/0242 →
Continuity (2)
Provisional Application 61237435 · Aug 27, 2009
Related Publication 20120157450A1 · Jun 21, 2012