Claims for Patent: 8,207,158

Summary for Patent: 8,207,158

Title:	5HT2c 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)
Application Number:	13/118,126
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,207,158
Patent Claims:	1. A method of decreasing food intake of a subject comprising identifying a subject in need of decreasing food intake; and 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. 2. The method of claim 1, wherein identifying a subject in need of decreasing food intake comprises determining the body mass index (BMI) of said subject. 3. The method of claim 2, wherein said subject has a BMI greater than 30 kg/m.sup.2. 4. The method of claim 2, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 5. The method of claim 1, wherein identifying a subject in need of decreasing food intake comprises determining the body fat content of the subject. 6. The method of claim 5, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 7. The method of claim 1, wherein identifying a subject in need of decreasing food intake comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 8. The method of claim 1, further comprising advising said subject to increase physical activity. 9. The method of claim 1, further comprising advising said subject to reduce dietary fat content. 10. The method of claim 1, further comprising advising said subject to consume fewer calories. 11. A method of decreasing food intake of a subject comprising identifying a subject in need of decreasing food intake; and administering to said subject a pharmaceutically effective amount of a hydrate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 12. The method of claim 11, wherein identifying a subject in need of decreasing food intake comprises determining the body mass index (BMI) of said subject. 13. The method of claim 12, wherein said subject has a BMI greater than 30 kg/m.sup.2. 14. The method of claim 12, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 15. The method of claim 11, wherein identifying a subject in need of decreasing food intake comprises determining the body fat content of the subject. 16. The method of claim 15, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 17. The method of claim 11, wherein identifying a subject in need of decreasing food intake comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 18. The method of claim 11, further comprising advising said subject to increase physical activity. 19. The method of claim 11, further comprising advising said subject to reduce dietary fat content. 20. The method of claim 11, further comprising advising said subject to consume fewer calories. 21. A method of decreasing food intake of a subject comprising identifying a subject in need of decreasing food intake; and administering to said subject a pharmaceutically effective amount of a solvate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 22. The method of claim 21, wherein identifying a subject in need of decreasing food intake comprises determining the body mass index (BMI) of said subject. 23. The method of claim 22, wherein said subject has a BMI greater than 30 kg/m.sup.2. 24. The method of claim 22, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 25. The method of claim 21, wherein identifying a subject in need of decreasing food intake comprises determining the body fat content of the subject. 26. The method of claim 25, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 27. The method of claim 21, wherein identifying a subject in need of decreasing food intake comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 28. The method of claim 21, further comprising advising said subject to increase physical activity. 29. The method of claim 21, further comprising advising said subject to reduce dietary fat content. 30. The method of claim 21, further comprising advising said subject to consume fewer calories. 31. A method of method of controlling weight gain of a subject comprising identifying a subject in need of weight gain control; and 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. 32. The method of claim 31, wherein identifying a subject in need of weight gain control comprises determining the body mass index (BMI) of said subject. 33. The method of claim 32, wherein said subject has a BMI greater than 30 kg/m.sup.2. 34. The method of claim 33, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 35. The method of claim 31, wherein identifying a subject in need of weight gain control comprises determining the body fat content of the subject. 36. 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. 37. The method of claim 31, wherein identifying a subject in need of weight gain control comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 38. The method of claim 31, further comprising advising said subject to increase physical activity. 39. The method of claim 31, further comprising advising said subject to reduce dietary fat content. 40. The method of claim 31, further comprising advising said subject to consume fewer calories. 41. A method of controlling weight gain of a subject comprising identifying a subject in need of weight gain control; and administering to said subject a pharmaceutically effective amount of a hydrate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 42. The method of claim 41, wherein identifying a subject in need of weight gain control comprises determining the body mass index (BMI) of said subject. 43. The method of claim 42, wherein said subject has a BMI greater than 30 kg/m.sup.2. 44. The method of claim 42, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 45. The method of claim 41, wherein identifying a subject in need of weight gain control comprises determining the body fat content of the subject. 46. The method of claim 45, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 47. The method of claim 41, wherein identifying a subject in need of weight gain control comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 48. The method of claim 41, further comprising advising said subject to increase physical activity. 49. The method of claim 41, further comprising advising said subject to reduce dietary fat content. 50. The method of claim 41, further comprising advising said subject to consume fewer calories. 51. A method of controlling weight gain of a subject comprising identifying a subject in need of weight gain control; and administering to said subject a pharmaceutically effective amount of a solvate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 52. The method of claim 51, wherein identifying a subject in need of weight gain control comprises determining the body mass index (BMI) of said subject. 53. The method of claim 52, wherein said subject has a BMI greater than 30 kg/m.sup.2. 54. The method of claim 52, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 55. The method of claim 51, wherein identifying a subject in need of weight gain control comprises determining the body fat content of the subject. 56. The method of claim 55, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 57. The method of claim 51, wherein identifying a subject in need of weight gain control comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 58. The method of claim 51, further comprising advising said subject to increase physical activity. 59. The method of claim 51, further comprising advising said subject to reduce dietary fat content. 60. The method of claim 51, further comprising advising said subject to consume fewer calories. 61. A method of method of inducing satiety of a subject comprising identifying a subject in need of inducing satiety; and 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. 62. The method of claim 61, wherein identifying a subject in need of inducing satiety comprises determining the body mass index (BMI) of said subject. 63. The method of claim 62, wherein said subject has a BMI greater than 30 kg/m.sup.2. 64. The method of claim 62, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 65. The method of claim 61, wherein identifying a subject in need of inducing satiety comprises determining the body fat content of the subject. 66. The method of claim 65, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 67. The method of claim 61, wherein identifying a subject in need of inducing satiety comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 68. The method of claim 61, further comprising advising said subject to increase physical activity. 69. The method of claim 61, further comprising advising said subject to reduce dietary fat content. 70. The method of claim 61, further comprising advising said subject to consume fewer calories. 71. A method of inducing satiety of a subject comprising identifying a subject in need of inducing satiety; and administering to said subject a pharmaceutically effective amount of a hydrate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 72. The method of claim 71, wherein identifying a subject in need of inducing satiety comprises determining the body mass index (BMI) of said subject. 73. The method of claim 72, wherein said subject has a BMI greater than 30 kg/m.sup.2. 74. The method of claim 72, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 75. The method of claim 71, wherein identifying a subject in need of inducing satiety comprises determining the body fat content of the subject. 76. The method of claim 75, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 77. The method of claim 71, wherein identifying a subject in need of inducing satiety comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 78. The method of claim 71, further comprising advising said subject to increase physical activity. 79. The method of claim 71, further comprising advising said subject to reduce dietary fat content. 80. The method of claim 71, further comprising advising said subject to consume fewer calories. 81. A method of inducing satiety of a subject comprising identifying a subject in need of inducing satiety; and administering to said subject a pharmaceutically effective amount of a solvate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 82. The method of claim 81, wherein identifying a subject in need of inducing satiety comprises determining the body mass index (BMI) of said subject. 83. The method of claim 82, wherein said subject has a BMI greater than 30 kg/m.sup.2. 84. The method of claim 82, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 85. The method of claim 81, wherein identifying a subject in need of inducing satiety comprises determining the body fat content of the subject. 86. The method of claim 85, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 87. The method of claim 81, wherein identifying a subject in need of inducing satiety comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 88. The method of claim 81, further comprising advising said subject to increase physical activity. 89. The method of claim 81, further comprising advising said subject to reduce dietary fat content. 90. The method of claim 81, further comprising advising said subject to consume fewer calories. 91. A method for treatment of obesity of a subject comprising identifying a subject in need of obesity treatment; and 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. 92. The method of claim 91, wherein identifying a subject in need of obesity treatment comprises determining the body mass index (BMI) of said subject. 93. The method of claim 92, wherein said subject has a BMI greater than 30 kg/m.sup.2. 94. The method of claim 92, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 95. The method of claim 91, wherein identifying a subject in need of obesity treatment comprises determining the body fat content of the subject. 96. The method of claim 95, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 97. The method of claim 91, wherein identifying a subject in need of obesity treatment comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 98. The method of claim 91, further comprising advising said subject to increase physical activity. 99. The method of claim 91, further comprising advising said subject to reduce dietary fat content. 100. The method of claim 91, further comprising advising said subject to consume fewer calories. 101. A method for treatment of obesity of a subject comprising identifying a subject in need of obesity treatment; and administering to said subject a pharmaceutically effective amount of a hydrate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 102. The method of claim 101, wherein identifying a subject in need of obesity treatment comprises determining the body mass index (BMI) of said subject. 103. The method of claim 102, wherein said subject has a BMI greater than 30 kg/m.sup.2. 104. The method of claim 102, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 105. The method of claim 101, wherein identifying a subject in need of obesity treatment comprises determining the body fat content of the subject. 106. The method of claim 105, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 107. The method of claim 101, wherein identifying a subject in need of obesity treatment comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 108. The method of claim 101, further comprising advising said subject to increase physical activity. 109. The method of claim 101, further comprising advising said subject to reduce dietary fat content. 110. The method of claim 101, further comprising advising said subject to consume fewer calories. 111. A method for treatment of obesity of a subject comprising identifying a subject in need of obesity treatment; and administering to said subject a pharmaceutically effective amount of a solvate of a pharmaceutically acceptable salt of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine. 112. The method of claim 111, wherein identifying a subject in need of obesity treatment comprises determining the body mass index (BMI) of said subject. 113. The method of claim 112, wherein said subject has a BMI greater than 30 kg/m.sup.2. 114. The method of claim 112, wherein said subject has a BMI ranging from 25.0 to 29.9 kg/m.sup.2. 115. The method of claim 111, wherein identifying a subject in need of obesity treatment comprises determining the body fat content of the subject. 116. The method of claim 115, wherein the subject has greater than 25% body fat content if male and greater than 30% body fat content if female. 117. The method of claim 111, wherein identifying a subject in need of obesity treatment comprises determining whether the subject suffers from coronary insufficiency, atheromatous disease, cardiac insufficiency, and/or diabetes. 118. The method of claim 111, further comprising advising said subject to increase physical activity. 119. The method of claim 111, further comprising advising said subject to reduce dietary fat content. 120. The method of claim 111, further comprising advising said subject to consume fewer calories.