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Page 1
Azepanone-based inhibitors of human and rat cathepsin K.
Marquis RW, Ru Y, LoCastro SM, Zeng J, Yamashita DS, Oh HJ, Erhard KF, Davis LD, Tomaszek TA, Tew D, Salyers K, Proksch J, Ward K, Smith B, Levy M, Cummings MD, Haltiwanger RC, Trescher G, Wang B, Hemling ME, Quinn CJ, Cheng HY, Lin F, Smith WW, Janson CA, Zhao B, McQueney MS, D'Alessio K, Lee CP, Marzulli A, Dodds RA, Blake S, Hwang SM, James IE, Gress CJ, Bradley BR, Lark MW, Gowen M, Veber DF. Marquis RW, et al. Among authors: haltiwanger rc. J Med Chem. 2001 Apr 26;44(9):1380-95. doi: 10.1021/jm000481x. J Med Chem. 2001. PMID: 11311061
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF. Yamashita DS, et al. Among authors: haltiwanger rc. J Med Chem. 2006 Mar 9;49(5):1597-612. doi: 10.1021/jm050915u. J Med Chem. 2006. PMID: 16509577
Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.
Miller WH, Alberts DP, Bhatnagar PK, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Erhard KF, Heerding DA, Keenan RM, Kwon C, Manley PJ, Newlander KA, Ross ST, Samanen JM, Uzinskas IN, Venslavsky JW, Yuan CC, Haltiwanger RC, Gowen M, Hwang SM, James IE, Lark MW, Rieman DJ, Stroup GB, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF. Miller WH, et al. Among authors: haltiwanger rc. J Med Chem. 2000 Jan 13;43(1):22-6. doi: 10.1021/jm990446u. J Med Chem. 2000. PMID: 10633035 No abstract available.
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.
Miller WH, Manley PJ, Cousins RD, Erhard KF, Heerding DA, Kwon C, Ross ST, Samanen JM, Takata DT, Uzinskas IN, Yuan CC, Haltiwanger RC, Gress CJ, Lark MW, Hwang SM, James IE, Rieman DJ, Willette RN, Yue TL, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF. Miller WH, et al. Among authors: haltiwanger rc. Bioorg Med Chem Lett. 2003 Apr 17;13(8):1483-6. doi: 10.1016/s0960-894x(03)00102-1. Bioorg Med Chem Lett. 2003. PMID: 12668017
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.
Miller WH, Bondinell WE, Cousins RD, Erhard KF, Jakas DR, Keenan RM, Ku TW, Newlander KA, Ross ST, Haltiwanger RC, Bradbeer J, Drake FH, Gowen M, Hoffman SJ, Hwang SM, James IE, Lark MW, Lechowska B, Rieman DJ, Stroup GB, Vasko-Moser JA, Zembryki DL, Azzarano LM, Adams PC, Huffman WF, et al. Miller WH, et al. Among authors: haltiwanger rc. Bioorg Med Chem Lett. 1999 Jul 5;9(13):1807-12. doi: 10.1016/s0960-894x(99)00283-8. Bioorg Med Chem Lett. 1999. PMID: 10406646
Potent and selective nonpeptide inhibitors of caspases 3 and 7 inhibit apoptosis and maintain cell functionality.
Lee D, Long SA, Adams JL, Chan G, Vaidya KS, Francis TA, Kikly K, Winkler JD, Sung CM, Debouck C, Richardson S, Levy MA, DeWolf WE Jr, Keller PM, Tomaszek T, Head MS, Ryan MD, Haltiwanger RC, Liang PH, Janson CA, McDevitt PJ, Johanson K, Concha NO, Chan W, Abdel-Meguid SS, Badger AM, Lark MW, Nadeau DP, Suva LJ, Gowen M, Nuttall ME. Lee D, et al. Among authors: haltiwanger rc. J Biol Chem. 2000 May 26;275(21):16007-14. doi: 10.1074/jbc.275.21.16007. J Biol Chem. 2000. PMID: 10821855 Free article.
ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo.
Gribble AD, Ife RJ, Shaw A, McNair D, Novelli CE, Bakewell S, Shah VP, Dolle RE, Groot PH, Pearce N, Yates J, Tew D, Boyd H, Ashman S, Eggleston DS, Haltiwanger RC, Okafo G. Gribble AD, et al. Among authors: haltiwanger rc. J Med Chem. 1998 Sep 10;41(19):3582-95. doi: 10.1021/jm980091z. J Med Chem. 1998. PMID: 9733484
Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.
Keenan RM, Callahan JF, Samanen JM, Bondinell WE, Calvo RR, Chen L, DeBrosse C, Eggleston DS, Haltiwanger RC, Hwang SM, Jakas DR, Ku TW, Miller WH, Newlander KA, Nichols A, Parker MF, Southhall LS, Uzinskas I, Vasko-Moser JA, Venslavsky JW, Wong AS, Huffman WF. Keenan RM, et al. Among authors: haltiwanger rc. J Med Chem. 1999 Feb 25;42(4):545-59. doi: 10.1021/jm980166z. J Med Chem. 1999. PMID: 10052962
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
Christensen SB, Guider A, Forster CJ, Gleason JG, Bender PE, Karpinski JM, DeWolf WE Jr, Barnette MS, Underwood DC, Griswold DE, Cieslinski LB, Burman M, Bochnowicz S, Osborn RR, Manning CD, Grous M, Hillegas LM, Bartus JO, Ryan MD, Eggleston DS, Haltiwanger RC, Torphy TJ. Christensen SB, et al. Among authors: haltiwanger rc. J Med Chem. 1998 Mar 12;41(6):821-35. doi: 10.1021/jm970090r. J Med Chem. 1998. PMID: 9526558
29 results