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Items: 11

1.

A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

Chrovian CC, Soyode-Johnson A, Peterson AA, Gelin CF, Deng X, Dvorak CA, Carruthers NI, Lord B, Fraser I, Aluisio L, Coe KJ, Scott B, Koudriakova T, Schoetens F, Sepassi K, Gallacher DJ, Bhattacharya A, Letavic MA.

J Med Chem. 2018 Jan 11;61(1):207-223. doi: 10.1021/acs.jmedchem.7b01279. Epub 2017 Dec 20.

PMID:
29211470
2.

Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.

Swanson DM, Savall BM, Coe KJ, Schoetens F, Koudriakova T, Skaptason J, Wall J, Rech J, Deng X, De Angelis M, Everson A, Lord B, Wang Q, Ao H, Scott B, Sepassi K, Lovenberg TW, Carruthers NI, Bhattacharya A, Letavic MA.

J Med Chem. 2016 Sep 22;59(18):8535-48. doi: 10.1021/acs.jmedchem.6b00989. Epub 2016 Sep 8.

PMID:
27548392
3.

Characterization of 2-(2,6-dichloro-benzyl)-thiazolo[5,4-d]pyrimidin-7-yl]-(4-trifluoromethyl-phenyl)-amine (JNJ-39729209) as a novel TRPV1 antagonist.

Maher MP, Bhattacharya A, Ao H, Swanson N, Wu NT, Freedman J, Kansagara M, Scott B, Li DH, Eckert WA 3rd, Liu Y, Sepassi K, Rizzolio M, Fitzgerald A, Liu J, Branstetter BJ, Rech JC, Lebsack AD, Breitenbucher JG, Wickenden AD, Chaplan SR.

Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50. doi: 10.1016/j.ejphar.2011.05.001. Epub 2011 May 10.

PMID:
21575625
4.

Pharmacological characterization of 1-(5-chloro-6-(trifluoromethoxy)-1H-benzoimidazol-2-yl)-1H-pyrazole-4-carboxylic acid (JNJ-42041935), a potent and selective hypoxia-inducible factor prolyl hydroxylase inhibitor.

Barrett TD, Palomino HL, Brondstetter TI, Kanelakis KC, Wu X, Haug PV, Yan W, Young A, Hua H, Hart JC, Tran DT, Venkatesan H, Rosen MD, Peltier HM, Sepassi K, Rizzolio MC, Bembenek SD, Mirzadegan T, Rabinowitz MH, Shankley NP.

Mol Pharmacol. 2011 Jun;79(6):910-20. doi: 10.1124/mol.110.070508. Epub 2011 Mar 3.

PMID:
21372172
5.

Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development.

Letavic MA, Aluisio L, Atack JR, Bonaventure P, Carruthers NI, Dugovic C, Everson A, Feinstein MA, Fraser IC, Hoey K, Jiang X, Keith JM, Koudriakova T, Leung P, Lord B, Lovenberg TW, Ly KS, Morton KL, Motley ST, Nepomuceno D, Rizzolio M, Rynberg R, Sepassi K, Shelton J.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4210-4. doi: 10.1016/j.bmcl.2010.05.041. Epub 2010 May 16.

PMID:
20561786
6.

Accounting for the effects of moderately increased pressure on the energetics of melting and solubility in metered dose inhalers.

Mogalian E, Sepassi K, Myrdal PB.

Drug Dev Ind Pharm. 2008 Sep;34(9):930-5. doi: 10.1080/03639040802154871 .

PMID:
18800253
7.

Comparison of aqueous solubility estimation from AQUAFAC and the GSE.

Jain P, Sepassi K, Yalkowsky SH.

Int J Pharm. 2008 Aug 6;360(1-2):122-47. doi: 10.1016/j.ijpharm.2008.04.028. Epub 2008 Apr 23.

PMID:
18514447
8.

Formulation and in vivo evaluation of chlorpropham (CIPC) oral formulations.

Kuehl PJ, Brenner T, Jain PK, Karlage K, Sepassi K, Yang G, Mayersohn M, Yalkowsky SH, Myrdal PB.

J Pharm Sci. 2008 Dec;97(12):5222-8. doi: 10.1002/jps.21384.

PMID:
18383335
9.

Solubility prediction in octanol: a technical note.

Sepassi K, Yalkowsky SH.

AAPS PharmSciTech. 2006 Mar 24;7(1):E26.

10.

Solubility prediction in octanol: A technical note.

Sepassi K, Yalkowsky SH.

AAPS PharmSciTech. 2006 Mar;7(1):E184-E191. doi: 10.1208/pt070126. Epub 2017 Mar 8.

PMID:
28290041
11.

Freeze-drying above room temperature.

Tesconi MS, Sepassi K, Yalkowsky SH.

J Pharm Sci. 1999 May;88(5):501-6.

PMID:
10229639

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