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Publikationer i urvalet

8 träffar

Bibliografisk träff 2019-12-16

An amide-based sulfenamide prodrug of gamma secretase inhibitor BMS-708163 delivers parent drug from an oral conventional solid dosage form in male beagle dog.

Guarino VR, Olson RE, Everlof JG, Wang N, McDonald I, Haskell R, Clarke W, Lentz KA.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2019.126856

Bibliografisk träff 2018-02-15

Secretase inhibitors for the treatment of Alzheimer's disease: Long road ahead.

Kumar D, Ganeshpurkar A, Kumar D, Modi G, Gupta SK, Singh SK.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2018.02.035

Bibliografisk träff 2013-06-20

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.

J Med Chem · journal article · DOI 10.1021/jm301741t

Bibliografisk träff 2012-12-21

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.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2012.12.039

Bibliografisk träff 2012-09-24

2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors.

Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Dee MF, Gai Y, Guss VL, Higgins MA, Keavy DJ, Loo A, Mate RA, Marcin LR, McElhone KE, Polson CT, Roberts SB, Macor JE.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2012.09.057

Bibliografisk träff 2012-03-29

Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.

Stepan AF, Subramanyam C, Efremov IV, Dutra JK, O'Sullivan TJ, DiRico KJ, McDonald WS, Won A, Dorff PH, Nolan CE, Becker SL, Pustilnik LR, Riddell DR, Kauffman GW, Kormos BL, Zhang L, Lu Y, Capetta SH, Green ME, Karki K, Sibley E, Atchison KP, Hallgren AJ, Oborski CE, Robshaw AE, Sneed B, O'Donnell CJ.

J Med Chem · journal article · DOI 10.1021/jm300094u

Bibliografisk träff 2011-10-26

Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.

Stepan AF, Karki K, McDonald WS, Dorff PH, Dutra JK, Dirico KJ, Won A, Subramanyam C, Efremov IV, O'Donnell CJ, Nolan CE, Becker SL, Pustilnik LR, Sneed B, Sun H, Lu Y, Robshaw AE, Riddell D, O'Sullivan TJ, Sibley E, Capetta S, Atchison K, Hallgren AJ, Miller E, Wood A, Obach RS.

J Med Chem · journal article · DOI 10.1021/jm200893p

Bibliografisk träff 2009-10-01

Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.

Kreft AF, Martone R, Porte A.

J Med Chem · review; journal article · DOI 10.1021/jm900188z