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-Reference-Cited by-同舟云学术

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

Published:2013-06-20 Issue:13 Volume:56 Page:5261-5274
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Probst Gary¹,Aubele Danielle L.¹,Bowers Simeon¹,Dressen Darren¹,Garofalo Albert W.¹,Hom Roy K.¹,Konradi Andrei W.¹,Marugg Jennifer L.¹,Mattson Matthew N.¹,Neitzel Martin L.¹,Semko Chris M.¹,Sham Hing L.¹²,Smith Jenifer¹,Sun Minghua¹,Truong Anh P.¹,Ye Xiaocong M.¹,Xu Ying-zi¹,Dappen Michael S.²,Jagodzinski Jacek J.²,Keim Pamela S.²,Peterson Brian²,Latimer Lee H.²,Quincy David²,Wu Jing²,Goldbach Erich³,Ness Daniel K.³,Quinn Kevin P.³,Sauer John-Michael³,Wong Karina³,Zhang Hongbin³,Zmolek Wes³,Brigham Elizabeth F.⁴,Kholodenko Dora⁴,Hu Kang⁴,Kwong Grace T.⁴,Lee Michael⁴,Liao Anna⁴,Motter Ruth N.⁴,Sacayon Patricia⁴,Santiago Pamela⁴,Willits Christopher⁴,Bard Frédérique⁵,Bova Michael P.⁵,Hemphill Susanna S.⁵,Nguyen Lam⁵,Ruslim Lany⁵,Tanaka Kevin⁵,Tanaka Pearl⁵,Wallace William⁵,Yednock Ted A.¹²³⁴⁵,Basi Guriqbal S.⁵

Affiliation:

1. Department of Medicinal Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, California 94080, United States

2. Department of Process and Analytical Chemistry, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, California 94080, United States

3. Department of Lead Finding, Drug Disposition, and Safety Evaluation, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, California 94080, United States

4. Department of In Vivo Pharmacology, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, California 94080, United States

5. Department of Biology, Elan Pharmaceuticals, 180 Oyster Point Boulevard, South San Francisco, California 94080, United States

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/jm301741t

Reference56 articles.

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