616202-49-4Relevant academic research and scientific papers
Discovery and structure-activity relationship of (1R)-8-chloro-2,3,4,5- tetrahydro-1-methyl-1H-3-benzazepine (Lorcaserin), a selective serotonin 5-HT2C receptor agonist for the treatment of obesity
Smith, Brian M.,Smith, Jeffrey M.,Tsai, James H.,Schultz, Jeffrey A.,Gilson, Charles A.,Estrada, Scott A.,Chen, Rita R.,Park, Douglas M.,Prieto, Emily B.,Gallardo, Charlemagne S.,Sengupta, Dipanjan,Dosa, Peter I.,Covel, Jon A.,Ren, Albert,Webb, Robert R.,Beeley, Nigel R. A.,Martin, Michael,Morgan, Michael,Espitia, Stephen,Saldana, Hazel R.,Bjenning, Christina,Whelan, Kevin T.,Grottick, Andrew J.,Menzaghi, Frederique,Thomsen, William J.
, p. 305 - 313 (2008/09/19)
The synthesis and SAR of a novel 3-benzazepine series of 5-HT2C agonists is described. Compound 7d (lorcaserin, APD356) was identified as one of the more potent and selective compounds in vitro (pEC50 values in functional assays measuring [3H]phosphoinositol turnover: 5-HT 2C = 8.1; 5-HT2A = 6.8; 5-HT2B = 6.1) and was potent in an acute in vivo rat food intake model upon oral administration (ED50 at 6 h = 18 mg/kg). Lorcaserin was further characterized in a single-dose pharmacokinetic study in rat (t1/2 = 3.7 h; F = 86%) and a 28-day model of weight gain in growing Sprague-Dawley rat (8.5% decrease in weight gain observed at 36 mg/kg b.i.d.). Lorcaserin was selected for further evaluation in clinical trials for the treatment of obesity.
BENZAZEPINE DERIVATIVES AND METHODS OF PROPHYLAXIS OR TREATMENT OF 5HT2C RECEPTOR ASSOCIATED DISEASES
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Page/Page column 42, (2008/06/13)
The present invention relates to substituted-2,3,4,5-tetrahydro-3-benzazepine derivatives that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the prophylaxis or treatment of 5HT2C receptor associated diseases, conditions or disorders, such as, obesity and related disorders.
BENZAZEPINE DERIVATIVES AND METHODS OF PROPHYLAXIS OR TREATMENT OF 5HT2C RECEPTOR ASSOCIATED DISEASES
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Page/Page column 33, (2008/06/13)
The present invention relates to substituted-2,3,4,5-tetrahydro-3-benzazepine derivatives that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the prophylaxis treatment of 5HT2C receptor associated diseases, conditions or disorders, such as, obesity and related disorders.
5HT2c receptor modulators
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Page 21, (2010/02/05)
The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
