Novel Potent Selective Orally Active S1P5 Receptor Antagonists.
Ma B, Guckian KM, Liu XG, Yang C, Li B, Scannevin R, Mingueneau M, Drouillard A, Walzer T.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/acsmedchemlett.0c00631 PUBLIKATIONSREGISTRET
Gå till forskningen.
Publikationsdata från Europe PMC och PubMed. Följ källhänvisningar från ämnesregistret till originalpublikationerna.
Publikationer som ChEBI hänvisar till för fty720-p. Visa hela publikationsregistret
En publikationsträff är inte en slutsats. Publikationslistan visar bibliografiska uppgifter. Eventuella forskningsutdrag visas separat med originalunderlag. En källhänvisning visar inte i sig effekt, dosering eller säkerhet.
Publikationer i urvalet
19 träffarIdentification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P<sub>1</sub>) Modulator Advanced into Clinical Trials.
Gilmore JL, Xiao HY, Dhar TGM, Yang MG, Xiao Z, Xie J, Lehman-McKeeman LD, Gong L, Sun H, Lecureux L, Chen C, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Borowski V, Warrack BM, Li Y, Shi H, Levesque PC, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Rampulla R, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Salter-Cid LM, Carter PH, Dyckman AJ.
J Med Chem · journal article · DOI 10.1021/acs.jmedchem.8b01695Kinase-independent phosphoramidate S1P<sub>1</sub> receptor agonist benzyl ether derivatives.
James E, Pertusati F, Brancale A, McGuigan C.
Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2017.02.011Potent and Selective Agonists of Sphingosine 1-Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series.
Watterson SH, Guo J, Spergel SH, Langevine CM, Moquin RV, Shen DR, Yarde M, Cvijic ME, Banas D, Liu R, Suchard SJ, Gillooly K, Taylor T, Rex-Rabe S, Shuster DJ, McIntyre KW, Cornelius G, D'Arienzo C, Marino A, Balimane P, Warrack B, Salter-Cid L, McKinnon M, Barrish JC, Carter PH, Pitts WJ, Xie J, Dyckman AJ.
J Med Chem · journal article · DOI 10.1021/acs.jmedchem.6b00089Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Demont EH, Bailey JM, Bit RA, Brown JA, Campbell CA, Deeks N, Dowell SJ, Eldred C, Gaskin P, Gray JR, Haynes A, Hirst DJ, Holmes DS, Kumar U, Morse MA, Osborne GJ, Renaux JF, Seal GA, Smethurst CA, Taylor S, Watson R, Willis R, Witherington J.
J Med Chem · journal article · DOI 10.1021/acs.jmedchem.5b01512Late-stage optimization of a tercyclic class of S1P3-sparing, S1P1 receptor agonists.
Horan JC, Kuzmich D, Liu P, DiSalvo D, Lord J, Mao C, Hopkins TD, Yu H, Harcken C, Betageri R, Hill-Drzewi M, Patenaude L, Patel M, Fletcher K, Terenzzio D, Linehan B, Xia H, Patel M, Studwell D, Miller C, Hickey E, Levin JI, Smith D, Kemper RA, Modis LK, Bannen LC, Chan DS, Mac MB, Ng S, Wang Y, Xu W, Lemieux RM.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2015.11.090Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Buzard DJ, Kim SH, Lopez L, Kawasaki A, Zhu X, Moody J, Thoresen L, Calderon I, Ullman B, Han S, Lehmann J, Gharbaoui T, Sengupta D, Calvano L, Montalban AG, Ma YA, Sage C, Gao Y, Semple G, Edwards J, Barden J, Morgan M, Chen W, Usmani K, Chen C, Sadeque A, Christopher RJ, Thatte J, Fu L, Solomon M, Mills D, Whelan K, Al-Shamma H, Gatlin J, Le M, Gaidarov I, Anthony T, Unett DJ, Blackburn A, Rueter J, Stirn S, Behan DP, Jones RM.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml500389mSynthesis and SAR studies of benzyl ether derivatives as potent orally active S1P₁ agonists.
Tsuji T, Suzuki K, Nakamura T, Goto T, Sekiguchi Y, Ikeda T, Fukuda T, Takemoto T, Mizuno Y, Kimura T, Kawase Y, Nara F, Kagari T, Shimozato T, Yahara C, Inaba S, Honda T, Izumi T, Tamura M, Nishi T.
Bioorg Med Chem · journal article · DOI 10.1016/j.bmc.2014.05.035Identification of benzoxazole analogs as novel, S1P(3) sparing S1P(1) agonists.
Deng G, Meng Q, Liu Q, Xu X, Xu Q, Ren F, Guo TB, Lu H, Xiang JN, Elliott JD, Lin X.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2012.04.095Synthesis and evaluation of CS-2100, a potent, orally active and S1P(3)- sparing S1P(1) agonist.
Nakamura T, Asano M, Sekiguchi Y, Mizuno Y, Tamaki K, Nara F, Kawase Y, Yabe Y, Nakai D, Kamiyama E, Urasaki-Kaneno Y, Shimozato T, Doi-Komuro H, Kagari T, Tomisato W, Inoue R, Nagasaki M, Yuita H, Oguchi-Oshima K, Kaneko R, Nishi T.
Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2012.02.022Novel immunomodulators based on an oxazolin-2-one-4-carboxamide scaffold.
He X, Wang L, Zheng Z, Xiao J, Zhong W, Li S.
Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2011.10.088Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Pennington LD, Croghan MD, Sham KK, Pickrell AJ, Harrington PE, Frohn MJ, Lanman BA, Reed AB, Lee MR, Xu H, McElvain M, Xu Y, Zhang X, Fiorino M, Horner M, Morrison HG, Arnett HA, Fotsch C, Tasker AS, Wong M, Cee VJ.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2011.10.085Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J.
J Med Chem · journal article · DOI 10.1021/jm200609tFingolimod (FTY720): a recently approved multiple sclerosis drug based on a fungal secondary metabolite.
Strader CR, Pearce CJ, Oberlies NH.
J Nat Prod · review; journal article · DOI 10.1021/np2000528Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
Nishi T, Miyazaki S, Takemoto T, Suzuki K, Iio Y, Nakajima K, Ohnuki T, Kawase Y, Nara F, Inaba S, Izumi T, Yuita H, Oshima K, Doi H, Inoue R, Tomisato W, Kagari T, Shimozato T.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml100301kBenzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.
Saha AK, Yu X, Lin J, Lobera M, Sharadendu A, Chereku S, Schutz N, Segal D, Marantz Y, McCauley D, Middleton S, Siu J, Bürli RW, Buys J, Horner M, Salyers K, Schrag M, Vargas HM, Xu Y, McElvain M, Xu H.
ACS Med Chem Lett · rapid-communication; journal article · DOI 10.1021/ml100227qStereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Ma B, Guckian KM, Lin EY, Lee WC, Scott D, Kumaravel G, Macdonald TL, Lynch KR, Black C, Chollate S, Hahm K, Hetu G, Jin P, Luo Y, Rohde E, Rossomando A, Scannevin R, Wang J, Yang C.
Bioorg Med Chem Lett · research-article; journal article; research support, n.i.h., extramural · DOI 10.1016/j.bmcl.2010.02.006Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
Evindar G, Bernier SG, Kavarana MJ, Doyle E, Lorusso J, Kelley MS, Halley K, Hutchings A, Wright AD, Saha AK, Hannig G, Morgan BA, Westlin WF.
Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.11.072Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.
Albert R, Hinterding K, Brinkmann V, Guerini D, Müller-Hartwieg C, Knecht H, Simeon C, Streiff M, Wagner T, Welzenbach K, Zécri F, Zollinger M, Cooke N, Francotte E.
J Med Chem · journal article · DOI 10.1021/jm050242f