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Items: 12

1.

Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.

Pero JE, Matthews JM, Behm DJ, Brnardic EJ, Brooks C, Budzik BW, Costell MH, Donatelli CA, Eisennagel SH, Erhard K, Fischer MC, Holt DA, Jolivette LJ, Li H, Li P, McAtee JJ, McCleland BW, Pendrak I, Posobiec LM, Rivera KLK, Rivero RA, Roethke TJ, Sender MR, Shu A, Terrell LR, Vaidya K, Xu X, Lawhorn BG.

J Med Chem. 2018 Dec 27;61(24):11209-11220. doi: 10.1021/acs.jmedchem.8b01344. Epub 2018 Dec 12.

PMID:
30500190
2.

Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.

Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS.

ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11.

3.

Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema.

Hilfiker MA, Hoang TH, Cornil J, Eidam HS, Matasic DS, Roethke TJ, Klein M, Thorneloe KS, Cheung M.

ACS Med Chem Lett. 2013 Jan 27;4(2):293-6. doi: 10.1021/ml300449k. eCollection 2013 Feb 14.

4.

An orally active TRPV4 channel blocker prevents and resolves pulmonary edema induced by heart failure.

Thorneloe KS, Cheung M, Bao W, Alsaid H, Lenhard S, Jian MY, Costell M, Maniscalco-Hauk K, Krawiec JA, Olzinski A, Gordon E, Lozinskaya I, Elefante L, Qin P, Matasic DS, James C, Tunstead J, Donovan B, Kallal L, Waszkiewicz A, Vaidya K, Davenport EA, Larkin J, Burgert M, Casillas LN, Marquis RW, Ye G, Eidam HS, Goodman KB, Toomey JR, Roethke TJ, Jucker BM, Schnackenberg CG, Townsley MI, Lepore JJ, Willette RN.

Sci Transl Med. 2012 Nov 7;4(159):159ra148. doi: 10.1126/scitranslmed.3004276.

5.

The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.

Watson NS, Adams C, Belton D, Brown D, Burns-Kurtis CL, Chaudry L, Chan C, Convery MA, Davies DE, Exall AM, Harling JD, Irvine S, Irving WR, Kleanthous S, McLay IM, Pateman AJ, Patikis AN, Roethke TJ, Senger S, Stelman GJ, Toomey JR, West RI, Whittaker C, Zhou P, Young RJ.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1588-92. doi: 10.1016/j.bmcl.2011.01.129. Epub 2011 Feb 2.

PMID:
21349711
6.

Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.

McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20.

PMID:
18524591
7.

Development of potent and selective small-molecule human Urotensin-II antagonists.

McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10.

PMID:
18502123
8.

Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.

McCleland BW, Davis RS, Palovich MR, Widdowson KL, Werner ML, Burman M, Foley JJ, Schmidt DB, Sarau HM, Rogers M, Salyers KL, Gorycki PD, Roethke TJ, Stelman GJ, Azzarano LM, Ward KW, Busch-Petersen J.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1713-7. Epub 2006 Dec 23.

PMID:
17236763
9.

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.

J Med Chem. 2006 Mar 9;49(5):1597-612.

PMID:
16509577
10.

SB-242235, a selective inhibitor of p38 mitogen-activated protein kinase. I: preclinical pharmacokinetics.

Ward KW, Proksch JW, Salyers KL, Azzarano LM, Morgan JA, Roethke TJ, McSurdy-Freed JE, Levy MA, Smith BR.

Xenobiotica. 2002 Mar;32(3):221-33.

PMID:
11958561
11.

Preclinical pharmacokinetics of SB-203580, a potent inhibitor of p38 mitogen-activated protein kinase.

Ward KW, Prokscht JW, Azzaranot LM, Mumawa JA, Roethke TJ, Stelman GJ, Walsh MJ, Zeigler KS, McSurdy-Freed JE, Kehlert JR, Chokshi J, Levy MA, Smith BR.

Xenobiotica. 2001 Nov;31(11):783-97.

PMID:
11765141
12.

Preclinical pharmacokinetics and interspecies scaling of a novel vitronectin receptor antagonist.

Ward KW, Azzarano LM, Bondinell WE, Cousins RD, Huffman WF, Jakas DR, Keenan RM, Ku TW, Lundberg D, Miller WH, Mumaw JA, Newlander KA, Pirhalla JL, Roethke TJ, Salyers KL, Souder PR, Stelman GJ, Smith BR.

Drug Metab Dispos. 1999 Nov;27(11):1232-41.

PMID:
10534306

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