Pyrrolo Pyrimidines as Agents for the Inhibition of Cystein Proteases
申请人:Betschart Claudia
公开号:US20090054467A1
公开(公告)日:2009-02-26
The invention provides compounds of Formula I or a pharmaceutically acceptable salt or ester thereof wherein the symbols have meaning as defined, which are inhibitors of cathepsin K and find use pharmaceutically for treatment of diseases and medical conditions in which cathepsin K is implicated, e.g. various disorders including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis and tumors.
The synthesis of eight rigid analogs of L-N-iminoethylornithine (L-NIO) is described. The compounds have been evaluated for their inhibition of inducible nitric oxide synthase. Preliminary structure-activity relationships are discussed. (C) 1998 Elsevier Science Ltd. All rights reserved.
SYNTHESIS OF BICYCLIC COMPOUNDS AND METHOD FOR THEIR USE AS THERAPEUTIC AGENTS
申请人:Wulff Jeremy E.
公开号:US20130210904A1
公开(公告)日:2013-08-15
Disclosed embodiments concern the synthesis and use of therapeutic compounds that for treating emerging flu strains and minimizing resistance to such strains. Methods for making the disclosed compounds concern using a base-mediated addition/cyclization sequence followed by functional group manipulation to develop functionalized compounds that can target neuraminidase, which makes them ideal candidates for treating influenza. Pharmaceutical compositions comprising the therapeutic compounds and biologically-acceptable materials are also described. Methods of inhibiting neuraminidase in subjects that are suspected of containing neuraminidase are also described. The use of metabolites of the disclosed compounds can also be used in diagnostic assays for therapeutic dosing of the disclosed compounds.