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Page 1
Synthesis of novel potent dipeptidyl peptidase IV inhibitors with enhanced chemical stability: interplay between the N-terminal amino acid alkyl side chain and the cyclopropyl group of alpha-aminoacyl-l-cis-4,5-methanoprolinenitrile-based inhibitors.
Magnin DR, Robl JA, Sulsky RB, Augeri DJ, Huang Y, Simpkins LM, Taunk PC, Betebenner DA, Robertson JG, Abboa-Offei BE, Wang A, Cap M, Xin L, Tao L, Sitkoff DF, Malley MF, Gougoutas JZ, Khanna A, Huang Q, Han SP, Parker RA, Hamann LG. Magnin DR, et al. Among authors: hamann lg. J Med Chem. 2004 May 6;47(10):2587-98. doi: 10.1021/jm049924d. J Med Chem. 2004. PMID: 15115400
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Augeri DJ, Robl JA, Betebenner DA, Magnin DR, Khanna A, Robertson JG, Wang A, Simpkins LM, Taunk P, Huang Q, Han SP, Abboa-Offei B, Cap M, Xin L, Tao L, Tozzo E, Welzel GE, Egan DM, Marcinkeviciene J, Chang SY, Biller SA, Kirby MS, Parker RA, Hamann LG. Augeri DJ, et al. Among authors: hamann lg. J Med Chem. 2005 Jul 28;48(15):5025-37. doi: 10.1021/jm050261p. J Med Chem. 2005. PMID: 16033281
Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors.
Zhao G, Taunk PC, Magnin DR, Simpkins LM, Robl JA, Wang A, Robertson JG, Marcinkeviciene J, Sitkoff DF, Parker RA, Kirby MS, Hamann LG. Zhao G, et al. Among authors: hamann lg. Bioorg Med Chem Lett. 2005 Sep 15;15(18):3992-5. doi: 10.1016/j.bmcl.2005.06.043. Bioorg Med Chem Lett. 2005. PMID: 16046120
Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.
Ostrowski J, Kuhns JE, Lupisella JA, Manfredi MC, Beehler BC, Krystek SR Jr, Bi Y, Sun C, Seethala R, Golla R, Sleph PG, Fura A, An Y, Kish KF, Sack JS, Mookhtiar KA, Grover GJ, Hamann LG. Ostrowski J, et al. Among authors: hamann lg. Endocrinology. 2007 Jan;148(1):4-12. doi: 10.1210/en.2006-0843. Epub 2006 Sep 28. Endocrinology. 2007. PMID: 17008401
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.
Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR Jr, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG. Sun C, et al. Among authors: hamann lg. J Med Chem. 2006 Dec 28;49(26):7596-9. doi: 10.1021/jm061101w. J Med Chem. 2006. PMID: 17181141
Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.
Hamann LG, Manfredi MC, Sun C, Krystek SR Jr, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J. Hamann LG, et al. Bioorg Med Chem Lett. 2007 Apr 1;17(7):1860-4. doi: 10.1016/j.bmcl.2007.01.076. Epub 2007 Jan 27. Bioorg Med Chem Lett. 2007. PMID: 17292608
Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.
Li JJ, Sutton JC, Nirschl A, Zou Y, Wang H, Sun C, Pi Z, Johnson R, Krystek SR Jr, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Fura A, Vyas VP, Li CY, Gougoutas JZ, Galella MA, Zahler R, Ostrowski J, Hamann LG. Li JJ, et al. Among authors: hamann lg. J Med Chem. 2007 Jun 28;50(13):3015-25. doi: 10.1021/jm070312d. Epub 2007 Jun 7. J Med Chem. 2007. PMID: 17552509
82 results