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Page 1
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
Zhao G, Souers AJ, Voorbach M, Falls HD, Droz B, Brodjian S, Lau YY, Iyengar RR, Gao J, Judd AS, Wagaw SH, Ravn MM, Engstrom KM, Lynch JK, Mulhern MM, Freeman J, Dayton BD, Wang X, Grihalde N, Fry D, Beno DW, Marsh KC, Su Z, Diaz GJ, Collins CA, Sham H, Reilly RM, Brune ME, Kym PR. Zhao G, et al. Among authors: mulhern mm. J Med Chem. 2008 Feb 14;51(3):380-3. doi: 10.1021/jm7013887. Epub 2008 Jan 10. J Med Chem. 2008. PMID: 18183944
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: mulhern mm. 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
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. Among authors: mulhern mm. 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
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: mulhern mm. 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
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Iyengar RR, Lynch JK, Mulhern MM, Judd AS, Freeman JC, Gao J, Souers AJ, Zhao G, Wodka D, Doug Falls H, Brodjian S, Dayton BD, Reilly RM, Swanson S, Su Z, Martin RL, Leitza ST, Houseman KA, Diaz G, Collins CA, Sham HL, Kym PR. Iyengar RR, et al. Among authors: mulhern mm. Bioorg Med Chem Lett. 2007 Feb 15;17(4):874-8. doi: 10.1016/j.bmcl.2006.11.065. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17234405
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Judd AS, Souers AJ, Wodka D, Zhao G, Mulhern MM, Iyengar RR, Gao J, Lynch JK, Freeman JC, Falls HD, Brodjian S, Dayton BD, Reilly RM, Gintant G, Limberis JT, Mikhail A, Leitza ST, Houseman KA, Diaz G, Bush EN, Shapiro R, Knourek-Segel V, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR. Judd AS, et al. Among authors: mulhern mm. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2365-71. doi: 10.1016/j.bmcl.2006.11.068. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17350253
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
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
Screening for cardiovascular safety: a structure-activity approach for guiding lead selection of melanin concentrating hormone receptor 1 antagonists.
Kym PR, Souers AJ, Campbell TJ, Lynch JK, Judd AS, Iyengar R, Vasudevan A, Gao J, Freeman JC, Wodka D, Mulhern M, Zhao G, Wagaw SH, Napier JJ, Brodjian S, Dayton BD, Reilly RM, Segreti JA, Fryer RM, Preusser LC, Reinhart GA, Hernandez L, Marsh KC, Sham HL, Collins CA, Polakowski JS. Kym PR, et al. J Med Chem. 2006 Apr 6;49(7):2339-52. doi: 10.1021/jm0512286. J Med Chem. 2006. PMID: 16570930
Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM. Pei Z, et al. J Med Chem. 2006 Nov 2;49(22):6439-42. doi: 10.1021/jm060955d. J Med Chem. 2006. PMID: 17064063
14 results