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Last Updated: April 25, 2024

Details for Patent: 8,546,379


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Title:5HT.sub.2C receptor modulators
Abstract: The present invention relates to novel compounds of Formula (I): ##STR00001## which act as 5HT.sub.2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
Inventor(s): Smith; Brian (San Diego, CA), Smith; Jeffrey (San Diego, CA)
Assignee: Arena Pharmaceuticals, Inc. (San Diego, CA)
Filing Date:Sep 14, 2012
Application Number:13/617,072
Claims:1. A compound of Formula (I): ##STR00060## wherein R.sub.1 is H or Me, R.sub.2 is Me, R.sub.2a is H, R.sub.3 is halogen, R.sub.4 is H, and R.sub.6 is H.

2. The compound according to claim 1, wherein R.sub.3 is Cl.

3. The compound according to claim 1, wherein the compound of Formula (I) is an R enantiomer.

4. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier or excipient.

5. A method of decreasing food intake of a mammal comprising administering to said mammal a pharmaceutically effective amount of a compound according to claim 1.

6. A method of inducing satiety in a mammal comprising administering to said mammal a pharmaceutically effective amount of a compound according to claim 1.

7. A method of controlling weight gain of a mammal comprising administering to said mammal a pharmaceutically effective amount of a compound according to claim 1.

8. A method of treatment of obesity comprising administering to a patient in need of such treatment a pharmaceutically effective amount of a compound according to claim 1.

9. The method of claim 8 further comprising the step of identifying a subject, said subject being in need of treatment for obesity, wherein said identifying step is performed prior to administering to said subject said pharmaceutically effective amount of said compound.

10. A pharmaceutically acceptable salt of a compound of Formula (I): ##STR00061## wherein R.sub.1 is H or Me, R.sub.2 is Me, R.sub.2a is H, R.sub.3 is halogen, R.sub.4 is H, and R.sub.6 is H.

11. The pharmaceutically acceptable salt according to claim 10, wherein R.sub.3 is Cl.

12. The pharmaceutically acceptable salt according to claim 10, wherein the compound of Formula (I) is an R enantiomer.

13. A pharmaceutical composition comprising a pharmaceutically acceptable salt of claim 10 and a pharmaceutically acceptable carrier or excipient.

14. A method of decreasing food intake of a mammal comprising administering to said mammal a pharmaceutically effective amount of a pharmaceutically acceptable salt of claim 10.

15. A method of inducing satiety in a mammal comprising administering to said mammal a pharmaceutically effective amount of a pharmaceutically acceptable salt of claim 10.

16. A method of controlling weight gain of a mammal comprising administering to said mammal a pharmaceutically effective amount of a pharmaceutically acceptable salt of claim 10.

17. A method of treatment of obesity comprising administering to a patient in need of such treatment a pharmaceutically effective amount of a pharmaceutically acceptable salt of claim 10.

18. The method of claim 17 further comprising the step of identifying a subject, said subject being in need of treatment for obesity, wherein said identifying step is performed prior to administering to said subject said pharmaceutically effective amount of said pharmaceutically acceptable salt.

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