IP Library › Granted Patent US 8,461,154
Granted Patent B2
US 8,461,154 · App. 13/465,549 · Granted Jun 11, 2013

Methods of utilizing arylpiperazine derivatives

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Quick Facts
Patent No.
US 8,461,154
App. No.
13/465,549
Granted
Jun 11, 2013
Kind
B2
Abstract

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

Claims (23)

1. A compound of Formula 1:

or a pharmaceutically acceptable salt, isomer, racemate, diastereomeric mixture thereof, wherein:

A is —(CH 2 ) 4 — or —O—(CH 2 ) 4 —;

B is S;

R 1 and R 2 are independently alkyl, alkoxy, or halogen; and

R 3 , R 4 , R 6 , R 7 , and R 8 are independently hydrogen, alkyl, alkoxy, or halogen, wherein R 1 , R 2 , R 3 , R 4 , R 6 , R 7 and R 8 and A are optionally substituted with isotopes selected from the group consising of 2 H (deuterium), 3 H (tritium), 13 C, 36 Cl, 18 F, 17 O, and 18 O.

2. The compound of claim 1 , wherein the compound has Formula 1a:

3. The compound of claim 1 , wherein A is —O—(CH 2 ) 4 .

4. The compound of claim 1 , wherein A is —(CH 2 ) 4 —.

5. The compound of claim 1 , wherein R 1 and R 2 are independently halogen or alkoxy.

6. The compound of claim 5 , wherein R 2 is methoxy.

7. The compound of claim 1 , wherein R 1 and R 2 are chloro.

8. The compound of claim 1 , wherein A is —(CH 2 ) 4 —; and R 3 , R 4 , R 6 , R 7 , and R 8 are independently hydrogen or alkyl.

9. The compound of claim 1 , wherein R 3 , R 4 , R 6 , R 7 , and R 8 are hydrogen.

10. The compound of claim 1 , wherein R 3 , R 4 , R 6 , R 7 , and R 8 and A are optionally substituted with 2 H (deuterium).

11. The compound of claim 1 , wherein the compound is in the form of a hydrochloride salt.

12. The compound of claim 1 , wherein the compound is enantiomerically pure and/or diastereomerically pure.

13. A pharmaceutical composition comprising the compound of claim 1 , and a pharmaceutically acceptable carrier, excipient, or diluent.

14. A method of treating psychosis, schizophrenia, acute mania, bipolar disorder, autistic disorder or depression, the method comprising administering to a patient in need thereof the pharmaceutical formulation claim 13 .

15. The method of claim 14 , wherein said method treats depression.

16. The method of claim 14 , wherein said method treats schizophrenia.

17. The method of claim 14 , wherein said method treats psychosis.

18. The method of claim 14 , wherein said method treats autistic disorder.