Design, synthesis and structure–activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors
摘要:
The structure-activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate beta-amyloid peptide synthesis via gamma-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficacious in reducing the cortical A beta x-40 levels in FVB mice via a single PO dose, as well as sulfonamide-pyrazoles that exhibit selectivity for inhibition of APP versus Notch processing by gamma-secretase, are highlighted. (C) 2011 Elsevier Ltd. All rights reserved.
Design, synthesis and structure–activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent γ-secretase inhibitors
摘要:
The structure-activity relationship (SAR) of a novel, potent and metabolically stable series of sulfonamide-pyrazoles that attenuate beta-amyloid peptide synthesis via gamma-secretase inhibition is detailed herein. Sulfonamide-pyrazoles that are efficacious in reducing the cortical A beta x-40 levels in FVB mice via a single PO dose, as well as sulfonamide-pyrazoles that exhibit selectivity for inhibition of APP versus Notch processing by gamma-secretase, are highlighted. (C) 2011 Elsevier Ltd. All rights reserved.
Matrix stabilized enzyme crystals and methods of use
申请人:——
公开号:US20020182201A1
公开(公告)日:2002-12-05
The invention relates to the stabilization of enzymes through the formation of matrix stabilized enzyme crystals. A matrix stabilized enzyme crystal is formed through cross-linking a polymer having one or more reactive moieties with an enzyme crystal using a low concentration of a multi-functional cross-linking reagent. The invention includes matrix stabilized enzyme crystals of phenylalanine ammonia lyase and a method of using to treat hyperphenylalaninemia.
MATRIX STABILIZED ENZYME CRYSTALS AND METHODS OF USE
申请人:IBEX TECHNOLOGIES
公开号:EP1372703A2
公开(公告)日:2004-01-02
N-SULFONAMIDO POLYCYCLIC PYRAZOLYL COMPOUNDS
申请人:Elan Pharmaceuticals Inc.
公开号:EP2346863A2
公开(公告)日:2011-07-27
US4742068A
申请人:——
公开号:US4742068A
公开(公告)日:1988-05-03
[EN] MATRIX STABILIZED ENZYME CRYSTALS AND METHODS OF USE<br/>[FR] CRISTAUX D'ENZYMES À STABILISATION MATRICIELLE ET MODALITÉS D'UTILISATION
申请人:IBEX TECHNOLOGIES
公开号:WO2002070646A2
公开(公告)日:2002-09-12
The invention relates to the stabilization of enzymes through the formation of matrix stabilized enzyme crystals. A matrix stabilized enzyme crystal is formed through cross-linking a polymer having one or more reactive moieties with an enzyme crystal using a low concentration of a multi-functional cross-linking reagent. The invention includes matrix stabilized enzyme crystals of phenylalanine ammonia lyase and a method of using to treat hyperphenylalaninemia.