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

Autor: Cheung M; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Bao W; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Behm DJ; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Brooks CA; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Bury MJ; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Dowdell SE; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Eidam HS; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Fox RM; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Goodman KB; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Holt DA; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Lee D; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Roethke TJ; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Willette RN; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Xu X; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Ye G; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States., Thorneloe KS; GlaxoSmithKline, Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapeutic Area, King of Prussia, Pennsylvania 19406, United States.

Publikováno v: ACS medicinal chemistry letters [ACS Med Chem Lett] 2017 Mar 20; Vol. 8 (5), pp. 549-554. Date of Electronic Publication: 2017 Mar 20 (Print Publication: 2017).

Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors.

Autor: Goodman KB; Department of Chemistry, Cardiovascular and Urogenital Center of Excellence in Drug Discovery, GlaxoSmithKline, UW2430, King of Prussia, PA 19406, USA. krista.b.goodman@gsk.com, Bury MJ, Cheung M, Cichy-Knight MA, Dowdell SE, Dunn AK, Lee D, Lieby JA, Moore ML, Scherzer DA, Sha D, Suarez DP, Murphy DJ, Harpel MR, Manas ES, McNulty DE, Annan RS, Matico RE, Schwartz BK, Trill JJ, Sweitzer TD, Wang DY, Keller PM, Krawiec JA, Jaye MC

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2009 Jan 01; Vol. 19 (1), pp. 27-30. Date of Electronic Publication: 2008 Nov 14.

Aminomethylpiperazines as selective urotensin antagonists.

Autor: Hilfiker MA; Department of Medicinal Chemistry, Cardiovascular and Urogenital Center of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, PO Box 1539, King of Prussia, PA 19406, USA. mark.a.hilfiker@gsk.com, Zhang D, Dowdell SE, Goodman KB, McAtee JJ, Dodson JW, Viet AQ, Wang GZ, Sehon CA, Behm DJ, Wu Z, Carballo LH, Douglas SA, Neeb MJ

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Aug 15; Vol. 18 (16), pp. 4470-3. Date of Electronic Publication: 2008 Jul 20.

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

Autor: McAtee JJ; Department of Medicinal Chemistry, Cardiovascular and Urogenital Center of Excellence for Drug Discovery, GlaxoSmithKline Pharmaceuticals, 709 Swedeland Road, King of Prussia, PA 19406, USA. jeff.j.mcatee@gsk.com, 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

Publikováno v: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jun 15; Vol. 18 (12), pp. 3500-3. Date of Electronic Publication: 2008 May 10.

Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.

Autor: Stavenger RA; Department of Medicinal Chemistry, GlaxoSmithKline, King of Prussia, Pennsylvania 19406, USA. robert.a.stavenger@gsk.com, Cui H, Dowdell SE, Franz RG, Gaitanopoulos DE, Goodman KB, Hilfiker MA, Ivy RL, Leber JD, Marino JP Jr, Oh HJ, Viet AQ, Xu W, Ye G, Zhang D, Zhao Y, Jolivette LJ, Head MS, Semus SF, Elkins PA, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Doe CP, Bentley R, Chen ZX, Hu E, Lee D

Publikováno v: Journal of medicinal chemistry [J Med Chem] 2007 Jan 11; Vol. 50 (1), pp. 2-5.