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Page 1
Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.
Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Mathvink RJ, et al. Among authors: hom gj. J Med Chem. 2000 Oct 19;43(21):3832-6. doi: 10.1021/jm000286i. J Med Chem. 2000. PMID: 11052788
Design and pharmacology of N-[(3R)-1,2,3,4-tetrahydroisoquinolinium- 3-ylcarbonyl]-(1R)-1-(4-chlorobenzyl)- 2-[4-cyclohexyl-4-(1H-1,2,4-triazol- 1-ylmethyl)piperidin-1-yl]-2-oxoethylamine (1), a potent, selective, melanocortin subtype-4 receptor agonist.
Sebhat IK, Martin WJ, Ye Z, Barakat K, Mosley RT, Johnston DB, Bakshi R, Palucki B, Weinberg DH, MacNeil T, Kalyani RN, Tang R, Stearns RA, Miller RR, Tamvakopoulos C, Strack AM, McGowan E, Cashen DE, Drisko JE, Hom GJ, Howard AD, MacIntyre DE, van der Ploeg LH, Patchett AA, Nargund RP. Sebhat IK, et al. Among authors: hom gj. J Med Chem. 2002 Oct 10;45(21):4589-93. doi: 10.1021/jm025539h. J Med Chem. 2002. PMID: 12361385
L-750355, a human beta3-adrenoceptor agonist; in vitro pharmacology and profile of activity in vivo in the rhesus monkey.
Forrest MJ, Hom G, Bach T, Candelore MR, Cascieri MA, Strader C, Tota L, Fisher MH, Szumiloski J, Ok HO, Weber AE, Wyvratt M, Vicario P, Marko O, Deng L, Cioffe C, Hegarty-Friscino B, MacIntyre E. Forrest MJ, et al. Eur J Pharmacol. 2000 Oct 27;407(1-2):175-81. doi: 10.1016/s0014-2999(00)00724-x. Eur J Pharmacol. 2000. PMID: 11050305
A selective human beta3 adrenergic receptor agonist increases metabolic rate in rhesus monkeys.
Fisher MH, Amend AM, Bach TJ, Barker JM, Brady EJ, Candelore MR, Carroll D, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hegarty-Friscino B, Guan XM, Hom GJ, Hutchins JE, Kelly LJ, Mathvink RJ, Metzger JM, Miller RR, Ok HO, Parmee ER, Saperstein R, Strader CD, Stearns RA, MacIntyre DE, et al. Fisher MH, et al. Among authors: hom gj. J Clin Invest. 1998 Jun 1;101(11):2387-93. doi: 10.1172/JCI2496. J Clin Invest. 1998. PMID: 9616210 Free PMC article.
3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Weber AE, Ok HO, Alvaro RF, Candelore MR, Cascieri MA, Chiu SH, Deng L, Forrest MJ, Hom GJ, Hutchins JE, Kao J, MacIntyre DE, Mathvink RJ, McLoughlin D, Miller RR, Newbold RC, Olah TV, Parmee ER, Perkins L, Stearns RA, Strader CD, Szumiloski J, Tang YS, Tota L, Fisher MH, et al. Weber AE, et al. Among authors: hom gj. Bioorg Med Chem Lett. 1998 Aug 18;8(16):2111-6. doi: 10.1016/s0960-894x(98)00381-3. Bioorg Med Chem Lett. 1998. PMID: 9873496
3-Pyridylethanolamines: potent and selective human beta 3 adrenergic receptor agonists.
Naylor EM, Colandrea VJ, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE. Naylor EM, et al. Among authors: hom gj. Bioorg Med Chem Lett. 1998 Nov 3;8(21):3087-92. doi: 10.1016/s0960-894x(98)00571-x. Bioorg Med Chem Lett. 1998. PMID: 9873681
Human beta3 adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides.
Parmee ER, Naylor EM, Perkins L, Colandrea VJ, Ok HO, Candelore MR, Cascieri MA, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Parmee ER, et al. Among authors: hom gj. Bioorg Med Chem Lett. 1999 Mar 8;9(5):749-54. doi: 10.1016/s0960-894x(99)00073-6. Bioorg Med Chem Lett. 1999. PMID: 10201841
Human beta3 adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides.
Naylor EM, Parmee ER, Colandrea VJ, Perkins L, Brockunier L, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Strader CD, Tota L, Wang PR, Wyvratt MJ, Fisher MH, Weber AE. Naylor EM, et al. Among authors: hom gj. Bioorg Med Chem Lett. 1999 Mar 8;9(5):755-8. doi: 10.1016/s0960-894x(99)00072-4. Bioorg Med Chem Lett. 1999. PMID: 10201842
L-770,644: a potent and selective human beta3 adrenergic receptor agonist with improved oral bioavailability.
Shih TL, Candelore MR, Cascieri MA, Chiu SH, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Shih TL, et al. Among authors: hom gj. Bioorg Med Chem Lett. 1999 May 3;9(9):1251-4. doi: 10.1016/s0960-894x(99)00182-1. Bioorg Med Chem Lett. 1999. PMID: 10340609
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
Feng DD, Biftu T, Candelore MR, Cascieri MA, Colwell LF Jr, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Strader CD, Tota L, Wyvratt MJ, Fisher MH, Weber AE. Feng DD, et al. Among authors: hom gj. Bioorg Med Chem Lett. 2000 Jul 3;10(13):1427-9. doi: 10.1016/s0960-894x(00)00267-5. Bioorg Med Chem Lett. 2000. PMID: 10888324
30 results