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An orally active small molecule MCHr1 antagonist in an acute feeding model was reported in the following: Takekawa, S, Asami, A, Ishihara, Y, Terauchi, J, Kato, K, Shimomura, Y, Mori M, Murakoshi, H, Kato, K, Suzuki, N, Nishimura, O, Fujino, M. T-226296: A novel, orally active and selective melanin-concentrating hormone receptor antagonist. Eur. J Pharmacol. 2002, 4383, 129-135
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(b) An orally active small molecule MCHr1 antagonist in an acute feeding model was reported in the following: Takekawa, S.; Asami, A.; Ishihara, Y.; Terauchi, J.; Kato, K.; Shimomura, Y.; Mori M.; Murakoshi, H.; Kato, K.; Suzuki, N.; Nishimura, O.; Fujino, M. T-226296: A novel, orally active and selective melanin-concentrating hormone receptor antagonist. Eur. J Pharmacol. 2002, 438(3), 129-135.
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Identification of 2- (4-benzyloxyphenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1H indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity
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(c) Souers, A.J.; Gao, J.; Brune, M.; Bush, E.; Wodka, D.; Vasudevan, A.; Judd, A.S.; Mulhem, M.; Brodjian, S.; Dayton, B.; Shapiro, R.; Hernandez, L.; Collins, C.A.; Kym, P.R. Identification of 2- (4-benzyloxyphenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1H indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity. J. Med. Chem. 2005, 48, 1318-1321.
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(d) Souers, A.J.; Gao, J.; Wodka D.; Judd, A.S.; Mulhern, M.M.; Napier, J.J.; Brune, M.E.; Bush, E.N., Brodjian, S.J.; Dayton, B.D.; Shapiro, R.; Hernandez, L.E.; Marsh, K.C.; Sham, H.L.; Collins, C.A.; Kym, P.R. Synthesis and evaluation of urea-based indazoles as melanin concentrating hormone receptor 1 antagonists for the treatment of obesity. Bioorg. Med. Chem. Lett. 2005, 15(11), 2752-2757.
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Kym, P. R.; Iyengar, R. R.; Souers, A. J.; Lynch, L K.; Judd, A. S.; Gao, J.; Freeman, J. C.; Mulhern, M. M.; Zhao, G.; Vasudevan, A.; Wodka, D.; Blackburn, C.; Brown, J.; Che, J. L.; Cullis, C.; Lai, S. J.; LaMarche, M.; Marsilje, T.; Roses, J.; Sells, T.; Geddes, B.; Govek, E.; Patane, M.; Fry, D.; Dayton, B. D.; Brodjian, S.; Falls, H. D.; Brune, M.; Bush, E.; Shapiro, R.; Knourek-Segel, V.; Fey, T.; McDowell, C.; Reinhart, G. A.; Preusser, L. C.; Marsh, K.; Hernandez, L.; Sham, H. L.; Collins, C. A. Discovery and characterization of aminopiperidinecoumarin melan concentrating hormone receptor 1 antagonists. J. Med. Chem. 2005, 48, 5888-5891.
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(e) Kym, P. R.; Iyengar, R. R.; Souers, A. J.; Lynch, L K.; Judd, A. S.; Gao, J.; Freeman, J. C.; Mulhern, M. M.; Zhao, G.; Vasudevan, A.; Wodka, D.; Blackburn, C.; Brown, J.; Che, J. L.; Cullis, C.; Lai, S. J.; LaMarche, M.; Marsilje, T.; Roses, J.; Sells, T.; Geddes, B.; Govek, E.; Patane, M.; Fry, D.; Dayton, B. D.; Brodjian, S.; Falls, H. D.; Brune, M.; Bush, E.; Shapiro, R.; Knourek-Segel, V.; Fey, T.; McDowell, C.; Reinhart, G. A.; Preusser, L. C.; Marsh, K.; Hernandez, L.; Sham, H. L.; Collins, C. A. Discovery and characterization of aminopiperidinecoumarin melan concentrating hormone receptor 1 antagonists. J. Med. Chem. 2005, 48, 5888-5891.
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McBriar, M.D.; Guzik, H.; Shapiro, S.; Paruchova, J.; Xu, R.; Palami, A.; Clader, J.W.; Cox, K.; Greenlee, W.J.; Hawes, B.E.; Kowalski, T.J.; O'neill, K.; Spar, B.D.; Weig, B.; Weston, D.J.; Farley, C.; Cook, J. Discovery of orally efficacious melanin concentrating hormone receptof 1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas. J. Med. Chem. 2006, 49(6), 2294-2310.
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(f) McBriar, M.D.; Guzik, H.; Shapiro, S.; Paruchova, J.; Xu, R.; Palami, A.; Clader, J.W.; Cox, K.; Greenlee, W.J.; Hawes, B.E.; Kowalski, T.J.; O'neill, K.; Spar, B.D.; Weig, B.; Weston, D.J.; Farley, C.; Cook, J. Discovery of orally efficacious melanin concentrating hormone receptof 1 antagonists as antiobesity agents. Synthesis, SAR, and biological evaluation of bicyclo[3.1.0]hexyl ureas. J. Med. Chem. 2006, 49(6), 2294-2310.
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(g) Lynch, J. K.; Freeman, J. C.; Judd, A. S.; Iyengar, R.; Mulhern, M.; Zhao, G.; Napier, J. J.; Wodka, D.; Brodjian, S.; Dayton, B. D.; Falls, D.; Ogiela, C.; Reilly, R. M.; Campbell, T. J.; Polakowski, J. S.; Hernandez, L.; Marsh, K. C.; Shapiro, R.; Knourek-Segel, V.; Droz, B.; Bush, E.; Brune, M.; Preusser, L. C.; Fryer, R. M.; Reinhart, G. A.; Houseman, K.; Diaz, G.; Mikhail, A.; Limberis, J. T.; Sham, H. L., Collins, A. A.; Kym P. R. Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: Assessment of potency, efficacy, and cardiovascular safety. J. Med. Chem. 2006, 49(22), 6569-6584.
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