US2016151381A1PendingUtilityA1

Salts of lorcaserin with optically active acids

41
Assignee: ARENA PHARM INCPriority: Sep 1, 2010Filed: Jul 29, 2015Published: Jun 2, 2016
Est. expirySep 1, 2030(~4.1 yrs left)· nominal 20-yr term from priority
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-modified
1 - 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)

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