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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.
J Med Chem. 2013 Jul 11;56(13):5261-74. doi: 10.1021/jm301741t. Epub 2013 Jun 20.
J Med Chem. 2013.
PMID: 23713656
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: kwong gt.
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
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Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.
Garofalo AW, Adler M, Aubele DL, Brigham EF, Chian D, Franzini M, Goldbach E, Kwong GT, Motter R, Probst GD, Quinn KP, Ruslim L, Sham HL, Tam D, Tanaka P, Truong AP, Ye XM, Ren Z.
Garofalo AW, et al. Among authors: kwong gt.
Bioorg Med Chem Lett. 2013 Apr 1;23(7):1974-7. doi: 10.1016/j.bmcl.2013.02.041. Epub 2013 Feb 15.
Bioorg Med Chem Lett. 2013.
PMID: 23453068
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Development of ALZET® osmotic pump compatible solvent compositions to solubilize poorly soluble compounds for preclinical studies.
Gullapalli R, Wong A, Brigham E, Kwong G, Wadsworth A, Willits C, Quinn K, Goldbach E, Samant B.
Gullapalli R, et al.
Drug Deliv. 2012 Jun-Jul;19(5):239-46. doi: 10.3109/10717544.2012.691121. Epub 2012 Jun 1.
Drug Deliv. 2012.
PMID: 22656673
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