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Items: 1 to 20 of 98

1.

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

Duan JJ, Lu Z, Jiang B, Stachura S, Weigelt CA, Sack JS, Khan J, Ruzanov M, Galella MA, Wu DR, Yarde M, Shen DR, Shuster DJ, Borowski V, Xie JH, Zhang L, Vanteru S, Gupta AK, Mathur A, Zhao Q, Foster W, Salter-Cid LM, Carter PH, Dhar TGM.

ACS Med Chem Lett. 2019 Feb 26;10(3):367-373. doi: 10.1021/acsmedchemlett.9b00010. eCollection 2019 Mar 14.

PMID:
30891142
2.

Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.

Shirai J, Tomata Y, Kono M, Ochida A, Fukase Y, Sato A, Masada S, Kawamoto T, Yonemori K, Koyama R, Nakagawa H, Nakayama M, Uga K, Shibata A, Koga K, Okui T, Shirasaki M, Skene R, Sang B, Hoffman I, Lane W, Fujitani Y, Yamasaki M, Yamamoto S.

Bioorg Med Chem. 2018 Jan 15;26(2):483-500. doi: 10.1016/j.bmc.2017.12.006. Epub 2017 Dec 9.

PMID:
29262987
3.

Discovery of orally efficacious RORγt inverse agonists. Part 2: Design, synthesis, and biological evaluation of novel tetrahydroisoquinoline derivatives.

Kono M, Oda T, Tawada M, Imada T, Banno Y, Taya N, Kawamoto T, Tokuhara H, Tomata Y, Ishii N, Ochida A, Fukase Y, Yukawa T, Fukumoto S, Watanabe H, Uga K, Shibata A, Nakagawa H, Shirasaki M, Fujitani Y, Yamasaki M, Shirai J, Yamamoto S.

Bioorg Med Chem. 2018 Jan 15;26(2):470-482. doi: 10.1016/j.bmc.2017.12.008. Epub 2017 Dec 11.

PMID:
29258712
4.

Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.

Fauber BP, René O, Deng Y, DeVoss J, Eidenschenk C, Everett C, Ganguli A, Gobbi A, Hawkins J, Johnson AR, La H, Lesch J, Lockey P, Norman M, Ouyang W, Summerhill S, Wong H.

J Med Chem. 2015 Jul 9;58(13):5308-22. doi: 10.1021/acs.jmedchem.5b00597. Epub 2015 Jun 23.

PMID:
26061388
5.

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.

Gong H, Weinstein DS, Lu Z, Duan JJ, Stachura S, Haque L, Karmakar A, Hemagiri H, Raut DK, Gupta AK, Khan J, Camac D, Sack JS, Pudzianowski A, Wu DR, Yarde M, Shen DR, Borowski V, Xie JH, Sun H, D'Arienzo C, Dabros M, Galella MA, Wang F, Weigelt CA, Zhao Q, Foster W, Somerville JE, Salter-Cid LM, Barrish JC, Carter PH, Dhar TGM.

Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93. doi: 10.1016/j.bmcl.2017.12.006. Epub 2017 Dec 5.

PMID:
29233651
6.

Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists.

Wang Y, Yang T, Liu Q, Ma Y, Yang L, Zhou L, Xiang Z, Cheng Z, Lu S, Orband-Miller LA, Zhang W, Wu Q, Zhang K, Li Y, Xiang JN, Elliott JD, Leung S, Ren F, Lin X.

Bioorg Med Chem. 2015 Sep 1;23(17):5293-302. doi: 10.1016/j.bmc.2015.07.068. Epub 2015 Aug 1.

PMID:
26277758
7.

Design and synthesis of a novel series of histamine H3 receptor antagonists through a scaffold hopping strategy.

Gao Z, Hurst WJ, Hall D, Hartung R, Reynolds W, Kang J, Nagorny R, Hendrix JA, George PG.

Bioorg Med Chem. 2015 Feb 1;23(3):429-38. doi: 10.1016/j.bmc.2014.12.036. Epub 2014 Dec 23.

PMID:
25577710
8.

Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists.

Hintermann S, Guntermann C, Mattes H, Carcache DA, Wagner J, Vulpetti A, Billich A, Dawson J, Kaupmann K, Kallen J, Stringer R, Orain D.

ChemMedChem. 2016 Dec 16;11(24):2640-2648. doi: 10.1002/cmdc.201600500. Epub 2016 Nov 30.

PMID:
27902884
9.

Discovery of carbazole carboxamides as novel RORγt inverse agonists.

Huang Y, Yu M, Sun N, Tang T, Yu F, Song X, Xie Q, Fu W, Shao L, Wang Y.

Eur J Med Chem. 2018 Mar 25;148:465-476. doi: 10.1016/j.ejmech.2018.02.050. Epub 2018 Feb 16.

PMID:
29477887
10.

Discovery of a factor Xa inhibitor (3R,4R)-1-(2,2-difluoro-ethyl)-pyrrolidine-3,4-dicarboxylic acid 3-[(5-chloro-pyridin-2-yl)-amide] 4-[[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenyl]-amide] as a clinical candidate.

Anselm L, Banner DW, Benz J, Zbinden KG, Himber J, Hilpert H, Huber W, Kuhn B, Mary JL, Otteneder MB, Panday N, Ricklin F, Stahl M, Thomi S, Haap W.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5313-9. doi: 10.1016/j.bmcl.2010.06.126. Epub 2010 Jul 1.

PMID:
20650636
11.

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G.

J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9.

PMID:
30130103
12.

Structural States of RORγt: X-ray Elucidation of Molecular Mechanisms and Binding Interactions for Natural and Synthetic Compounds.

Kallen J, Izaac A, Be C, Arista L, Orain D, Kaupmann K, Guntermann C, Hoegenauer K, Hintermann S.

ChemMedChem. 2017 Jul 6;12(13):1014-1021. doi: 10.1002/cmdc.201700278. Epub 2017 Jun 20.

PMID:
28590087
13.

Identification and biological evaluation of thiazole-based inverse agonists of RORγt.

Gege C, Cummings MD, Albers M, Kinzel O, Kleymann G, Schlüter T, Steeneck C, Nelen MI, Milligan C, Spurlino J, Xue X, Leonard K, Edwards JP, Fourie A, Goldberg SD, Hoffmann T.

Bioorg Med Chem Lett. 2018 May 15;28(9):1446-1455. doi: 10.1016/j.bmcl.2018.03.093. Epub 2018 Apr 3.

PMID:
29631962
14.

Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.

Yu M, Lizarzaburu M, Motani A, Fu Z, Du X, Liu JJ, Jiao X, Lai S, Fan P, Fu A, Liu Q, Murakoshi M, Nara F, Oda K, Okuyama R, Reagan JD, Watanabe N, Yamazaki M, Xiong Y, Zhang Y, Zhuang R, Lin DC, Houze JB, Medina JC, Li L.

ACS Med Chem Lett. 2013 May 1;4(9):829-34. doi: 10.1021/ml4000854. eCollection 2013 Sep 12.

15.

Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors.

Wang Y, Cai W, Zhang G, Yang T, Liu Q, Cheng Y, Zhou L, Ma Y, Cheng Z, Lu S, Zhao YG, Zhang W, Xiang Z, Wang S, Yang L, Wu Q, Orband-Miller LA, Xu Y, Zhang J, Gao R, Huxdorf M, Xiang JN, Zhong Z, Elliott JD, Leung S, Lin X.

Bioorg Med Chem. 2014 Jan 15;22(2):692-702. doi: 10.1016/j.bmc.2013.12.021. Epub 2013 Dec 21.

PMID:
24388993
16.

Pharmacological inhibitory profile of TAK-828F, a potent and selective orally available RORγt inverse agonist.

Shibata A, Uga K, Sato T, Sagara M, Igaki K, Nakamura Y, Ochida A, Kono M, Shirai J, Yamamoto S, Yamasaki M, Tsuchimori N.

Biochem Pharmacol. 2018 Apr;150:35-45. doi: 10.1016/j.bcp.2018.01.023. Epub 2018 Jan 31.

PMID:
29369782
17.

1,2-Diarylcyclopentenes as selective cyclooxygenase-2 inhibitors and orally active anti-inflammatory agents.

Li JJ, Anderson GD, Burton EG, Cogburn JN, Collins JT, Garland DJ, Gregory SA, Huang HC, Isakson PC, Koboldt CM, et al.

J Med Chem. 1995 Oct 27;38(22):4570-8.

PMID:
7473585
18.

Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.

Lavey BJ, Kozlowski JA, Shankar BB, Spitler JM, Zhou G, Yang DY, Shu Y, Wong MK, Wong SC, Shih NY, Wu J, McCombie SW, Rizvi R, Wolin RL, Lunn CA.

Bioorg Med Chem Lett. 2007 Jul 1;17(13):3760-4. Epub 2007 Apr 10.

PMID:
17466519
19.

Novel derivatives of 2-pyridinemethylamine as selective, potent, and orally active agonists at 5-HT1A receptors.

Vacher B, Bonnaud B, Funes P, Jubault N, Koek W, Assié MB, Cosi C, Kleven M.

J Med Chem. 1999 May 6;42(9):1648-60.

PMID:
10229633
20.

Discovery of Highly Potent Liver X Receptor β Agonists.

Kick EK, Busch BB, Martin R, Stevens WC, Bollu V, Xie Y, Boren BC, Nyman MC, Nanao MH, Nguyen L, Plonowski A, Schulman IG, Yan G, Zhang H, Hou X, Valente MN, Narayanan R, Behnia K, Rodrigues AD, Brock B, Smalley J, Cantor GH, Lupisella J, Sleph P, Grimm D, Ostrowski J, Wexler RR, Kirchgessner T, Mohan R.

ACS Med Chem Lett. 2016 Oct 23;7(12):1207-1212. eCollection 2016 Dec 8.

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