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Last Updated: March 19, 2024

Details for Patent: 8,273,734


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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:Jun 14, 2012
Application Number:13/523,805
Claims:1. A method for weight loss in a subject comprising administering to said subject a pharmaceutically effective amount of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, wherein said subject has at least one weight related condition chosen from sleep apnea, hypertension, cardiovascular disease, and diabetes.

2. The method of claim 1, wherein said subject has sleep apnea.

3. The method of claim 1, wherein said subject has hypertension.

4. The method of claim 1, wherein said subject has cardiovascular disease.

5. The method of claim 1, wherein said subject has diabetes.

6. The method of claim 1, wherein said subject has a BMI greater than 30 kg/m.sup.2.

7. The method of claim 1, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2.

8. The method of claim 1, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female.

9. The method of claim 1, further comprising advising said subject to increase physical activity.

10. The method of claim 1, further comprising advising said subject to reduce dietary fat content.

11. The method of claim 1, further comprising advising said subject to consume fewer calories.

12. A method of controlling weight gain of a subject comprising administering to said subject a pharmaceutically effective amount of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, wherein said subject has at least one weight related condition chosen from sleep apnea, hypertension, cardiovascular disease, and diabetes.

13. The method of claim 12, wherein said subject has sleep apnea.

14. The method of claim 12, wherein said subject has hypertension.

15. The method of claim 12, wherein said subject has cardiovascular disease.

16. The method of claim 12, wherein said subject has diabetes.

17. The method of claim 12, wherein said subject has a BMI greater than 30 kg/m.sup.2.

18. The method of claim 12, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2.

19. The method of claim 12, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female.

20. The method of claim 12, further comprising advising said subject to increase physical activity.

21. The method of claim 12, further comprising advising said subject to reduce dietary fat content.

22. The method of claim 12, further comprising advising said subject to consume fewer calories.

23. A method for maintaining weight in a subject comprising administering to said subject a pharmaceutically effective amount of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, wherein said subject has at least one weight related condition chosen from sleep apnea, hypertension, cardiovascular disease, and diabetes.

24. The method of claim 23, wherein said maintaining weight comprises maintaining weight after weight loss.

25. The method of claim 23, wherein said subject has sleep apnea.

26. The method of claim 23, wherein said subject has hypertension.

27. The method of claim 23, wherein said subject has cardiovascular disease.

28. The method of claim 23, wherein said subject has diabetes.

29. The method of claim 23, wherein said subject has a BMI greater than 30 kg/m.sup.2.

30. The method of claim 23, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2.

31. The method of claim 23, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female.

32. The method of claim 23, further comprising advising said subject to increase physical activity.

33. The method of claim 23, further comprising advising said subject to reduce dietary fat content.

34. The method of claim 23, further comprising advising said subject to consume fewer calories.

35. A method for treatment of obesity of a subject comprising administering to said subject a pharmaceutically effective amount of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, wherein said subject has at least one weight related condition chosen from sleep apnea, hypertension, cardiovascular disease, and diabetes.

36. The method of claim 35, wherein said subject has sleep apnea.

37. The method of claim 35, wherein said subject has hypertension.

38. The method of claim 35, wherein said subject has cardiovascular disease.

39. The method of claim 35, wherein said subject has diabetes.

40. The method of claim 35, wherein said subject has a BMI greater than 30 kg/m.sup.2.

41. The method of claim 35, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2.

42. The method of claim 35, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female.

43. The method of claim 35, further comprising advising said subject to increase physical activity.

44. The method of claim 35, further comprising advising said subject to reduce dietary fat content.

45. The method of claim 35, further comprising advising said subject to consume fewer calories.

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