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Page 1
Discovery and pharmacological evaluation of growth hormone secretagogue receptor antagonists.
Xin Z, Serby MD, Zhao H, Kosogof C, Szczepankiewicz BG, Liu M, Liu B, Hutchins CW, Sarris KA, Hoff ED, Falls HD, Lin CW, Ogiela CA, Collins CA, Brune ME, Bush EN, Droz BA, Fey TA, Knourek-Segel VE, Shapiro R, Jacobson PB, Beno DW, Turner TM, Sham HL, Liu G. Xin Z, et al. Among authors: bush en. J Med Chem. 2006 Jul 27;49(15):4459-69. doi: 10.1021/jm060461g. J Med Chem. 2006. PMID: 16854051
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.
Souers AJ, Gao J, Brune M, Bush E, Wodka D, Vasudevan A, Judd AS, Mulhern M, Brodjian S, Dayton B, Shapiro R, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR. Souers AJ, et al. J Med Chem. 2005 Mar 10;48(5):1318-21. doi: 10.1021/jm0490890. J Med Chem. 2005. PMID: 15743174
Identification of ortho-amino benzamides and nicotinamides as MCHr1 antagonists.
Vasudevan A, LaMarche MJ, Blackburn C, Che JL, Luchaco-Cullis CA, Lai S, Marsilje TH, Patane MA, Souers AJ, Wodka D, Geddes B, Chen S, Brodjian S, Falls DH, Dayton BD, Bush E, Brune M, Shapiro RD, Marsh KC, Hernandez LE, Sham HL, Collins CA, Kym PR. Vasudevan A, et al. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4174-9. doi: 10.1016/j.bmcl.2005.06.089. Bioorg Med Chem Lett. 2005. PMID: 16085414
Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists.
Kym PR, Iyengar R, Souers AJ, Lynch JK, Judd AS, Gao J, Freeman J, Mulhern M, Zhao G, Vasudevan A, Wodka D, Blackburn C, Brown J, Che JL, Cullis C, Lai SJ, LaMarche MJ, Marsilje T, Roses J, Sells T, Geddes B, Govek E, Patane M, Fry D, Dayton BD, Brodjian S, Falls D, Brune M, Bush E, Shapiro R, Knourek-Segel V, Fey T, McDowell C, Reinhart GA, Preusser LC, Marsh K, Hernandez L, Sham HL, Collins CA. Kym PR, et al. J Med Chem. 2005 Sep 22;48(19):5888-91. doi: 10.1021/jm050598r. J Med Chem. 2005. PMID: 16161992
Aminopiperidine indazoles as orally efficacious melanin concentrating hormone receptor-1 antagonists.
Vasudevan A, Souers AJ, Freeman JC, Verzal MK, Gao J, Mulhern MM, Wodka D, Lynch JK, Engstrom KM, Wagaw SH, Brodjian S, Dayton B, Falls DH, Bush E, Brune M, Shapiro RD, Marsh KC, Hernandez LE, Collins CA, Kym PR. Vasudevan A, et al. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5293-7. doi: 10.1016/j.bmcl.2005.08.049. Epub 2005 Oct 3. Bioorg Med Chem Lett. 2005. PMID: 16203136
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
Yeh VS, Kurukulasuriya R, Fung S, Monzon K, Chiou W, Wang J, Stolarik D, Imade H, Shapiro R, Knourek-Segel V, Bush E, Wilcox D, Nguyen PT, Brune M, Jacobson P, Link JT. Yeh VS, et al. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5555-60. doi: 10.1016/j.bmcl.2006.08.034. Epub 2006 Aug 23. Bioorg Med Chem Lett. 2006. PMID: 16931002
Optimization of chromone-2-carboxamide melanin concentrating hormone receptor 1 antagonists: assessment of potency, efficacy, and cardiovascular safety.
Lynch JK, Freeman JC, Judd AS, Iyengar R, Mulhern M, Zhao G, Napier JJ, Wodka D, Brodjian S, Dayton BD, Falls D, Ogiela C, Reilly RM, Campbell TJ, Polakowski JS, Hernandez L, Marsh KC, Shapiro R, Knourek-Segel V, Droz B, Bush E, Brune M, Preusser LC, Fryer RM, Reinhart GA, Houseman K, Diaz G, Mikhail A, Limberis JT, Sham HL, Collins CA, Kym PR. Lynch JK, et al. J Med Chem. 2006 Nov 2;49(22):6569-84. doi: 10.1021/jm060683e. J Med Chem. 2006. PMID: 17064075
Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.
Souers AJ, Gao J, Wodka D, Judd AS, Mulhern MM, Napier JJ, Brune ME, Bush EN, Brodjian SJ, Dayton BD, Shapiro R, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR. Souers AJ, et al. Among authors: bush en. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2752-7. doi: 10.1016/j.bmcl.2005.03.114. Bioorg Med Chem Lett. 2005. PMID: 15911251
2,4-diaminopyrimidine derivatives as potent growth hormone secretagogue receptor antagonists.
Serby MD, Zhao H, Szczepankiewicz BG, Kosogof C, Xin Z, Liu B, Liu M, Nelson LT, Kaszubska W, Falls HD, Schaefer V, Bush EN, Shapiro R, Droz BA, Knourek-Segel VE, Fey TA, Brune ME, Beno DW, Turner TM, Collins CA, Jacobson PB, Sham HL, Liu G. Serby MD, et al. Among authors: bush en. J Med Chem. 2006 Apr 20;49(8):2568-78. doi: 10.1021/jm0510934. J Med Chem. 2006. PMID: 16610800
Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: the effects of chirality on substituted indan-1-ylamines.
Souers AJ, Iyengar RR, Judd AS, Beno DW, Gao J, Zhao G, Brune ME, Napier JJ, Mulhern MM, Lynch JK, Freeman JC, Wodka D, Chen CJ, Falls HD, Brodjian S, Dayton BD, Diaz GJ, Bush EN, Shapiro R, Droz BA, Knourek-Segel V, Hernandez LE, Marsh KC, Reilly RM, Sham HL, Collins CA, Kym PR. Souers AJ, et al. Among authors: bush en. Bioorg Med Chem Lett. 2007 Feb 15;17(4):884-9. doi: 10.1016/j.bmcl.2006.11.061. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17188866
66 results