US2016151381A1PendingUtilityA1
Salts of lorcaserin with optically active acids
Est. expirySep 1, 2030(~4.1 yrs left)· nominal 20-yr term from priority
Inventors:Anthony C. BlackburnWilliam L. Betts, IiiJaimie Karyn RueterYun ShanAnna ShifrinaScott Stirn
A61P 43/00A61K 31/155C07D 223/16A61P 3/04A61K 31/55A61K 45/06
41
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Claims
Abstract
Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.
Claims
exact text as granted — not AI-modified1 - 50 . (canceled)
51 . A method for weight management, comprising administering to an individual in need thereof a therapeutically effective amount of a salt selected from:
(R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (1S)-(+)-10-camsylate salt; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hemi-L-malate salt; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine L-glutamate salt; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine L-aspartate salt; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hemimucate salt; (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine pyroglutamate salt; and (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine glucuronate salt; and pharmaceutically acceptable solvates and hydrates thereof.
52 . The method of claim 51 , wherein the weight management comprises one or more of: weight loss, maintenance of weight loss, decreased food consumption, increasing meal-related satiety, reducing pre-meal hunger, and reducing intra-meal food intake.
53 . The method of claim 51 , wherein the method for weight management is a method of decreasing food intake.
54 . The method of claim 51 , wherein the method for weight management is a method of inducing satiety.
55 . The method of claim 51 , wherein the method for weight management is a method of controlling weight gain.
56 . The method of claim 51 , wherein the method for weight management is a method of treating obesity.
57 . The method of claim 51 , as an adjunct to a reduced-calorie diet.
58 . The method of claim 51 , wherein the individual in need of weight management is selected from:
an obese patient with an initial body mass index ≧30 kg/m 2 ; and an overweight patient with an initial body mass index ≧27 kg/m 2 in the presence of at least one weight-related comorbid condition.
59 . The method of claim 58 , wherein the weight-related comorbid condition is selected from: hypertension, dyslipidemia, and type 2 diabetes.
60 . The method of claim 51 , further comprising administering a second anti-obesity agent to the individual.
61 . The method of claim 60 , wherein the second anti-obesity agent is selected from: chlorphentermine, clortermine, phenpentermine, and phentermine, and pharmaceutically acceptable salts, solvates, and hydrates thereof.
62 . The method of claim 51 , further comprising administering an anti-diabetes agent to the individual.
63 . The method of claim 62 , wherein the anti-diabetes agent is metformin.
64 . The method of claim 51 , wherein the salt is (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine (1S)-(+)-10-camsylate salt.
65 . The method of claim 51 , wherein the salt is(R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hemi-L-malate salt.
66 . The method of claim 51 , wherein the salt is (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine L-glutamate salt.
67 . The method of claim 51 , wherein the salt is (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine L-aspartate salt.
68 . The method of claim 51 , wherein the salt is (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hemimucate salt.
69 . The method of claim 51 , wherein the salt is (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine pyroglutamate salt.
70 . The method of claim 51 , wherein the salt is(R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine glucuronate salt.
71 . (canceled)Cited by (0)
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