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Page 1
Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.
Gingrich DE, Lisko JG, Curry MA, Cheng M, Quail M, Lu L, Wan W, Albom MS, Angeles TS, Aimone LD, Haltiwanger RC, Wells-Knecht K, Ott GR, Ghose AK, Ator MA, Ruggeri B, Dorsey BD. Gingrich DE, et al. Among authors: haltiwanger rc. J Med Chem. 2012 May 24;55(10):4580-93. doi: 10.1021/jm201550q. Epub 2012 May 7. J Med Chem. 2012. PMID: 22564207
Design, synthesis, and anaplastic lymphoma kinase (ALK) inhibitory activity for a novel series of 2,4,8,22-tetraazatetracyclo[14.3.1.1³,⁷.1⁹,¹³]docosa-1(20),3(22),4,6,9(21),10,12,16,18-nonaene macrocycles.
Breslin HJ, Lane BM, Ott GR, Ghose AK, Angeles TS, Albom MS, Cheng M, Wan W, Haltiwanger RC, Wells-Knecht KJ, Dorsey BD. Breslin HJ, et al. Among authors: haltiwanger rc. J Med Chem. 2012 Jan 12;55(1):449-64. doi: 10.1021/jm201333e. Epub 2011 Dec 15. J Med Chem. 2012. PMID: 22172029
Piperidine-3,4-diol and piperidine-3-ol derivatives of pyrrolo[2,1-f][1,2,4]triazine as inhibitors of anaplastic lymphoma kinase.
Mesaros EF, Angeles TS, Albom MS, Wagner JC, Aimone LD, Wan W, Lu L, Huang Z, Olsen M, Kordwitz E, Haltiwanger RC, Landis AJ, Cheng M, Ruggeri BA, Ator MA, Dorsey BD, Ott GR. Mesaros EF, et al. Among authors: haltiwanger rc. Bioorg Med Chem Lett. 2015 Mar 1;25(5):1047-52. doi: 10.1016/j.bmcl.2015.01.019. Epub 2015 Jan 17. Bioorg Med Chem Lett. 2015. PMID: 25655723
3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity.
Hudkins RL, Becknell NC, Lyons JA, Aimone LD, Olsen M, Haltiwanger RC, Mathiasen JR, Raddatz R, Gruner JA. Hudkins RL, et al. Among authors: haltiwanger rc. Eur J Med Chem. 2015 May 5;95:349-56. doi: 10.1016/j.ejmech.2015.03.054. Epub 2015 Mar 24. Eur J Med Chem. 2015. PMID: 25827402
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
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
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
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
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.
29 results