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Page 1
Discovery of a novel [3.2.1] benzo fused bicyclic sulfonamide-pyrazoles as potent, selective and efficacious γ-secretase inhibitors.
Ye XM, Konradi AW, Sun M, Yuan S, Aubele DL, Dappen M, Dressen D, Garofalo AW, Jagodzinski JJ, Latimer L, Probst GD, Sham HL, Wone D, Xu YZ, Ness D, Brigham E, Kwong GT, Willtis C, Tonn G, Goldbach E, Quinn KP, Zhang HH, Sauer JM, Bova M, Basi GS. Ye XM, et al. Among authors: ness d. Bioorg Med Chem Lett. 2013 Feb 15;23(4):996-1000. doi: 10.1016/j.bmcl.2012.12.039. Epub 2012 Dec 21. Bioorg Med Chem Lett. 2013. PMID: 23312944
Discovery of (R)-4-cyclopropyl-7,8-difluoro-5-(4-(trifluoromethyl)phenylsulfonyl)-4,5-dihydro-1H-pyrazolo[4,3-c]quinoline (ELND006) and (R)-4-cyclopropyl-8-fluoro-5-(6-(trifluoromethyl)pyridin-3-ylsulfonyl)-4,5-dihydro-2H-pyrazolo[4,3-c]quinoline (ELND007): metabolically stable γ-secretase Inhibitors that selectively inhibit the production of amyloid-β over Notch.
Probst G, Aubele DL, Bowers S, Dressen D, Garofalo AW, Hom RK, Konradi AW, Marugg JL, Mattson MN, Neitzel ML, Semko CM, Sham HL, Smith J, Sun M, Truong AP, Ye XM, Xu YZ, Dappen MS, Jagodzinski JJ, Keim PS, Peterson B, Latimer LH, Quincy D, Wu J, Goldbach E, Ness DK, Quinn KP, Sauer JM, Wong K, Zhang H, Zmolek W, Brigham EF, Kholodenko D, Hu K, Kwong GT, Lee M, Liao A, Motter RN, Sacayon P, Santiago P, Willits C, Bard F, Bova MP, Hemphill SS, Nguyen L, Ruslim L, Tanaka K, Tanaka P, Wallace W, Yednock TA, Basi GS. Probst G, et al. Among authors: ness dk. J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20. J Med Chem. 2013. PMID: 23713656
Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimer's disease.
Basi GS, Hemphill S, Brigham EF, Liao A, Aubele DL, Baker J, Barbour R, Bova M, Chen XH, Dappen MS, Eichenbaum T, Goldbach E, Hawkinson J, Lawler-Herbold R, Hu K, Hui T, Jagodzinski JJ, Keim PS, Kholodenko D, Latimer LH, Lee M, Marugg J, Mattson MN, McCauley S, Miller JL, Motter R, Mutter L, Neitzel ML, Ni H, Nguyen L, Quinn K, Ruslim L, Semko CM, Shapiro P, Smith J, Soriano F, Szoke B, Tanaka K, Tang P, Tucker JA, Ye XM, Yu M, Wu J, Xu YZ, Garofalo AW, Sauer JM, Konradi AW, Ness D, Shopp G, Pleiss MA, Freedman SB, Schenk D. Basi GS, et al. Among authors: ness d. Alzheimers Res Ther. 2010 Dec 29;2(6):36. doi: 10.1186/alzrt60. Alzheimers Res Ther. 2010. PMID: 21190552 Free PMC article.
Safety and Tolerability of Multiple Ascending Doses of PRX002/RG7935, an Anti-α-Synuclein Monoclonal Antibody, in Patients With Parkinson Disease: A Randomized Clinical Trial.
Jankovic J, Goodman I, Safirstein B, Marmon TK, Schenk DB, Koller M, Zago W, Ness DK, Griffith SG, Grundman M, Soto J, Ostrowitzki S, Boess FG, Martin-Facklam M, Quinn JF, Isaacson SH, Omidvar O, Ellenbogen A, Kinney GG. Jankovic J, et al. JAMA Neurol. 2018 Oct 1;75(10):1206-1214. doi: 10.1001/jamaneurol.2018.1487. JAMA Neurol. 2018. PMID: 29913017 Free PMC article. Clinical Trial.
A Phase II Study to Evaluate the Safety and Efficacy of Prasinezumab in Early Parkinson's Disease (PASADENA): Rationale, Design, and Baseline Data.
Pagano G, Boess FG, Taylor KI, Ricci B, Mollenhauer B, Poewe W, Boulay A, Anzures-Cabrera J, Vogt A, Marchesi M, Post A, Nikolcheva T, Kinney GG, Zago WM, Ness DK, Svoboda H, Britschgi M, Ostrowitzki S, Simuni T, Marek K, Koller M, Sevigny J, Doody R, Fontoura P, Umbricht D, Bonni A; PASADENA Investigators; Prasinezumab Study Group. Pagano G, et al. Among authors: ness dk. Front Neurol. 2021 Oct 1;12:705407. doi: 10.3389/fneur.2021.705407. eCollection 2021. Front Neurol. 2021. PMID: 34659081 Free PMC article.
Exacerbation of cerebral amyloid angiopathy-associated microhemorrhage in amyloid precursor protein transgenic mice by immunotherapy is dependent on antibody recognition of deposited forms of amyloid beta.
Racke MM, Boone LI, Hepburn DL, Parsadainian M, Bryan MT, Ness DK, Piroozi KS, Jordan WH, Brown DD, Hoffman WP, Holtzman DM, Bales KR, Gitter BD, May PC, Paul SM, DeMattos RB. Racke MM, et al. Among authors: ness dk. J Neurosci. 2005 Jan 19;25(3):629-36. doi: 10.1523/JNEUROSCI.4337-04.2005. J Neurosci. 2005. PMID: 15659599 Free PMC article.
130 results