Loxapine analogs and methods of use thereof

• US 20060063928A1
• Filed: 09/21/2005
• Published: 03/23/2006
• Est. Priority Date: 09/21/2004
• Status: Active Grant

• Current Assignee: Hypnion, Inc.
• Original Assignee: Hypnion, Inc.
• Inventors: White, James F., Hangauer, David G., Solomon, Michael, Edgar, Dale M., Shiosaki, Kazumi
• Granted Patent: US 7,592,333 B2
• Time in Patent Office: Days
• US Class Current: 540/551
• CPC Class Codes: A61K 31/553 having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: C07D 267/20 [b, f]-condensed
• CPC Class Codes: C07D 413/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The invention relates to novel compounds and methods of using them for modulating sleep.

Claims

1. A compound having the formula of Compound 1:

2. The compound of claim 1, wherein Compound 1 is a solvate.

3. The compound of claim 1, wherein Compound 1 is a hydrate.

4. The compound of claim 1, wherein the Compound I is a pharmaceutically acceptable salt.

5. The compound of claim 4, wherein the salt is an acid addition salt.

6. The compound of claim 4, wherein the salt is a hydrochloride salt.

7. The compound of claim 6, wherein the compound is:

8. The compound of claim 6, wherein the compound is:

9. The compound of claim 1, wherein the compound is a prodrug.

10. A composition comprising Compound 1:

11. The composition of claim 10, wherein the compound is a solvate.

12. The composition of claim 10, wherein the compound is a hydrate.

13. The composition of claim 10, wherein the compound is a pharmaceutically acceptable salt.

14. The composition of claim 13, wherein the salt is an acid addition salt.

15. The composition of claim 14, wherein the salt is a hydrochloride salt.

16. The composition of claim 15, wherein the composition is:

17. The pharmaceutical composition of claim 15, wherein the composition is:

18. A method of modulating sleep in a subject, comprising administering to a subject in need thereof a therapeutically effective amount of Compound 1:

19. The method of claim 18, wherein the sleep modulation is selected from decreasing the time to sleep onset, increasing the average sleep bout length, and increasing the maximum sleep bout length.

20. The method of claim 19, wherein the sleep modulation treats a sleep disorder.

21. The method of claim 20, wherein the sleep disorder is selected from circadian rhythm abnormality, insomnia, parasomnia, sleep apnea syndrome, narcolepsy and hypersomnia.

22. The method of claim 18, wherein the compound or pharmaceutically acceptable salt, solvate, hydrate, or prodrug, is administered as a pharmaceutical composition comprising at least one pharmaceutically acceptable excipient.

23. The method of claim 18, wherein the compound or pharmaceutically acceptable salt, solvate, hydrate, or prodrug is co-administered with one or more additional therapies.

24. The method of claim 18, wherein the subject is a human.