Amino-caprolactam derivatives as gamma-secretase inhibitors. 2007

Michael F Parker, and Joanne J Bronson, and Donna M Barten, and Jason A Corsa, and Wengsheng Du, and Kevin M Felsenstein, and Valerie L Guss, and Darcy Izzarelli, and Alice Loo, and Kate E McElhone, and Larry R Marcin, and Ramesh Padmanabha, and Roger Pak, and Craig T Polson, and Jeremy H Toyn, and Sam Varma, and Jian Wang, and Victoria Wong, and Ming Zheng, and Susan B Roberts
Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, 5 Research Parkway, Wallingford, CT 06492, USA. parkerm@BMS.com

A series of amino-caprolactam sulfonamides were developed from a screening hit. Compounds with good in vitro and in vivo gamma-secretase activity are reported.

UI MeSH Term Description Entries
D002209 Caprolactam Cyclic amide of caproic acid used in manufacture of synthetic fibers of the polyamide type. Can cause local irritation. Aminocaproic Lactam,Hexahydro-2H-Azepin-2-One,Hexahydro 2H Azepin 2 One,Lactam, Aminocaproic
D004791 Enzyme Inhibitors Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction. Enzyme Inhibitor,Inhibitor, Enzyme,Inhibitors, Enzyme
D053829 Amyloid Precursor Protein Secretases Endopeptidases that are specific for AMYLOID PROTEIN PRECURSOR. Three secretase subtypes referred to as alpha, beta, and gamma have been identified based upon the region of amyloid protein precursor they cleave. APP Secretase,Amyloid Precursor Protein Secretase,Secretase,Secretases,alpha-Secretase,beta-Secretase,gamma-Secretase,Secretase, APP,alpha Secretase,beta Secretase,gamma Secretase

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