IP Library Granted Patent US 9,770,436
Granted Patent B2
US 9,770,436 · App. 14/860,427 · Granted Sep 26, 2017

Polymorphs of azabicyclohexane

Inventors: Eric J. Hagen (Lafayette, IN); Kevin Halloran (Somerset, NJ)
Assignee: EUTHYMICS BIOSCIENCE, INC.
A61K31/403C07D209/52C07D209/94
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Quick Facts
Patent No.
US 9,770,436
App. No.
14/860,427
Granted
Sep 26, 2017
Kind
B2
Abstract

The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.

Claims (16)

1. A pharmaceutical composition comprising polymorph form A of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo [3.1.0] hexane hydrochloride substantially free of other geometric and optical isomers and polymorphic forms thereof and an inert pharmaceutically acceptable carrier or diluent.

2. The pharmaceutical composition of claim 1 in oral unit dosage form.

3. The oral unit dosage form of claim 2 wherein said polymorph form A in crystalline form is present in said oral unit dosage form in the amount of about 25 mg to about 300 mg.

4. The oral unit dosage form of claim 3 wherein said oral unit dosage form is a tablet or capsule.

5. A pharmaceutical composition comprising polymorph form B of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo [3.1.0] hexane hydrochloride substantially free of other geometric and optical isomers and polymorphic forms thereof and an inert pharmaceutically acceptable carrier or diluent.

6. The pharmaceutical composition of claim 5 in oral unit dosage form.

7. The oral unit dosage form of claim 6 wherein said polymorph form B in crystalline form is present in said oral unit dosage form in the amount of about 25 mg to about 300 mg.

8. The oral unit dosage form of claim 7 wherein said oral unit dosage form is a tablet or capsule.

9. A pharmaceutical composition comprising polymorph form C of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo [3.1.0] hexane hydrochloride substantially free of other geometric and optical isomers and polymorphic forms thereof and an inert pharmaceutically acceptable carrier or diluent.

10. The pharmaceutical composition of claim 9 in oral unit dosage form.

11. The oral unit dosage form of claim 10 wherein said polymorph form C in crystalline form is present in said oral unit dosage form in the amount of about 25 mg to about 300 mg.

12. The oral unit dosage form of claim 11 wherein said oral unit dosage form is a tablet or capsule.

13. A pharmaceutical composition comprising a mixture of polymorph form A and either or both polymorph form B and polymorph form C of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo [3.1.0]hexane hydrochloride wherein the amount of polymorph form A ranges from about 85% to about 95% (by weight).

14. A pharmaceutical composition comprising a mixture of polymorph form A and either or both polymorph form B and polymorph form C (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo [3.1.0]hexane hydrochloride wherein the amount of polymorph form A ranges from about 95% to about 99% (by weight).

15. A pharmaceutical composition comprising a mixture of polymorph form C and either or both polymorph form A and polymorph form B of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo [3.1.0] hexane hydrochloride.

16. The pharmaceutical composition of claim 1 wherein said pharmaceutical composition comprises about 50 mg to about 1000 mg of said polymorph.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 5, 2018
From: EUTHYMICS BIOSCIENCE, INC.
To: ETHISMOS RESEARCH, INC.
Reel/Frame 045252/0870 →
Continuity (8)
Continuation 13907809 · May 31, 2013
Continuation 13366209 · Feb 3, 2012
Continuation 13207144 · Aug 10, 2011
Continuation 12428399 · Apr 22, 2009
Continuation 12208284 · Sep 10, 2008
Continuation 11205956 · Aug 16, 2005
Provisional Application 60651505 · Aug 18, 2004
Related Publication 20160008324A1 · Jan 14, 2016