Polymorphic forms of 3-amino-1-propanesulfonic acid

• US 20070049638A1
• Filed: 07/14/2006
• Published: 03/01/2007
• Est. Priority Date: 07/21/2005
• Status: Abandoned Application

• Current Assignee: Neurochem (International) Limited
• Original Assignee: Neurochem (International) Limited
• Inventors: Guay, France
• Application Number:
  US11/487,161
• Publication Number:
  US 20070049638A1
• Time in Patent Office: Days
• US Class Current: 514/553
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: C07C 309/14 containing amino groups bound to the carbon skeleton

Abstract

Polymorphic forms of 3-amino-1-propanesulfonic acid are described.

Claims

1. Crystalline 3-amino-1-propanesulfonic acid in polymorphic Form A.

11. The crystalline 3-amino-1-propanesulfonic acid of claim 1, wherein said crystalline 3-amino-1-propanesulfonic acid is characterized by XRPD peaks at one or more of the following °

2θ

values;

17.1, 21.3, and 24.7.

12. The crystalline 3-amino-1-propanesulfonic acid of claim 1, wherein said crystalline 3-amino-1-propanesulfonic acid is characterized by FT-IR peaks at one or more of the following wavelengths:

789 cm<sup>−

1</sup> and 833 cm<sup>−

1</sup>.

13. The crystalline 3-amino-1-propanesulfonic acid of claim 1, wherein said crystalline 3-amino-1-propanesulfonic acid is characterized by an FT-Raman peak at 790 cm⁻

1.

17. A pharmaceutical composition comprising crystalline 3-amino-1-propanesulfonic acid of claim 1.

18. The pharmaceutical composition of claim 17, wherein said composition further comprises a pharmaceutically acceptable carrier.

19. The pharmaceutical composition of claim 18, wherein said composition comprises the ingredients described in Example 12, Example 13, Example 14, Example 15, Example 16, Example 17 or Example 18.

25. The pharmaceutical composition of claim 17, wherein said pharmaceutical composition comprises an effective amount of crystalline 3-amino-1-propanesulfonic acid to treat an Aβ

-amyloid related disease.

26. The pharmaceutical composition of claim 25, wherein said Aβ

-amyloid related disease is Alzheimer'"'"'s disease or CAA.

28. A method for treating an Aβ

-amyloid related disease in a subject, comprising administering to said subject, in need thereof, an effective amount of a crystalline 3-amino-1-propanesulfonic acid of claim 1, such that said Aβ

-amyloid related disease is treated in said subject.

29. The method of claim 28, wherein said subject is a human.

30. The method of claim 28, wherein said Aβ

-amyloid related disease is Alzheimer'"'"'s disease or CAA.

2. Crystalline 3-amino-1-propanesulfonic acid in a mixture of Form A and Form B.

3. Substantially pure crystalline 3-amino-1-propanesulfonic acid in polymorphic Form A.

4. The substantially pure crystalline 3-amino-1-propanesulfonic acid of claim 3, wherein said substantially pure crystalline 3-amino-1-propanesulfonic acid is comprised of 90% or greater polymorph Form A.

5. The substantially pure crystalline 3-amino-1-propanesulfonic acid of claim 4, wherein said substantially pure crystalline 3-amino-1-propanesulfonic acid is comprised of 95% or greater polymorph Form A.

6. The substantially pure crystalline 3-amino-1-propanesulfonic acid of claim 5, wherein said substantially pure crystalline 3-amino-1-propanesulfonic acid is comprised of 97% or greater polymorph Form A.

7. Substantially pure crystalline 3-amino-1-propanesulfonic acid in polymorphic Form B.

8. The substantially pure crystalline 3-amino-1-propanesulfonic acid of claim 7, wherein said substantially pure crystalline 3-amino-1-propanesulfonic acid is comprised of 90% or greater polymorph Form B.

9. The substantially pure crystalline 3-amino-1-propanesulfonic acid of claim 8, wherein said substantially pure crystalline 3-amino-1-propanesulfonic acid is comprised of 95% or greater polymorph Form B.

10. The substantially pure crystalline 3-amino-1-propanesulfonic acid of claim 9, wherein said substantially pure crystalline 3-amino-1-propanesulfonic acid is comprised of 97% or greater polymorph Form B.

14. The crystalline 3-amino-1-propanesulfonic acid of claim 7, wherein said crystalline 3-amino-1-propanesulfonic acid is characterized by XRPD peaks at one or more of the following °

2θ

values;

17.3 and 25.3.

15. The crystalline 3-amino-1-propanesulfonic acid of claim 7, wherein said crystalline 3-amino-1-propanesulfonic acid is characterized by FT-IR peaks at one or more of the following wavelengths:

803 cm<sup>−

1</sup> and 843 cm<sup>−

1</sup>.

16. The crystalline 3-amino-1-propanesulfonic acid of claims 7, wherein said crystalline 3-amino-1-propanesulfonic acid is characterized by an FT-Raman peak at 802 cm⁻

1.

20-24. -24. (canceled)

27. (canceled)

31. (canceled)