Compositions, Synthesis, And Methods Of Using Piperazine Based Antipsychotic Agents

• US 20090298819A1
• Filed: 05/27/2009
• Published: 12/03/2009
• Est. Priority Date: 05/27/2008
• Status: Active Grant

• Current Assignee: Reviva Pharmaceuticals, Inc.
• Original Assignee: Reviva Pharmaceuticals, Inc.
• Inventors: Bhat, Laxminarayan, Mohapatra, Prabhu Prasad, Adiey, Kouacou
• Granted Patent: US 8,207,163 B2
• Time in Patent Office: Days
• US Class Current: 514/230.5
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/24 Antidepressants
• CPC Class Codes: C07D 239/96 Two oxygen atoms
• CPC Class Codes: C07D 265/36 condensed with one six-membered ring

Abstract

The present invention provides novel piperazine derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder and depression.

Claims

1. A compound comprising structural Formula (I):

2. The compound of claim 1, wherein the soft-moiety is an amide, an ester, a carbonate, a phosphate, a sulfate, or a carbamate.

3. The compound of claim 2, wherein the soft-moiety further comprises a spacer.

4. The compound of claim 3, wherein the spacer is O, S, alkyl, substituted alkyl, acyl, acylamino, alkoxy, alkylamino, alkylthio, amino, carboxy, or alkoxycarbonyl.

5. The compound of claim 4, wherein the spacer is alky or substituted alkyl.

6. A compound comprising structural Formula (II):

7. The compound of claim 6, wherein the spacer is O, S, alkyl, substituted alkyl, acyl, acylamino, alkoxy, alkylamino, alkylthio, amino, carboxy, or alkoxycarbonyl.

8. The compound of claim 7, wherein the spacer is alky or substituted alkyl.

9. A compound comprising structural Formula (III):

10. A compound comprising structural Formula (IV):

11. A compound comprising structural Formula (V):

12. A compound comprising structural Formula (VI):

13. A compound comprising structural Formula (VII):

14. A compound comprising structural Formula (VIII):

15. A compound comprising structural Formula (IX):

16. A compound comprising structural Formula (X):

17. A compound comprising structural Formula (XI):

18. A method of treating a patient, the method comprising:

administering to the patient a pharmaceutical composition comprising a compound of Formula (I);

19. The method of claim 18, wherein the spacer is O, S, alkyl, substituted alkyl, acyl, acylamino, alkoxy, alkylamino, alkylthio, amino, carboxy, or alkoxycarbonyl.

20. The method of claim 18, wherein R¹ and R² form a 5- or 6-membered substituted or unsubstituted ring.

21. The method of claim 18, wherein the composition is for oral, mucosal, rectal, parenteral, transdermal, or subcutaneous administration.

22. The method of claim 18, wherein the patient is suffering from psychoses, schizophrenia, acute manic, bipolar disorder, autistic disorder, or depression.

23. The method of claim 22, wherein the patient is suffering from schizophrenia.

24. The method of claim 22, wherein the patient is suffering from bipolar disorder.