221142-27-4Relevant articles and documents
SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS
-
Page/Page column 32, (2013/06/27)
The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula(I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives
Costanzo, Michael J.,Yabut, Stephen C.,Zhang, Han-Cheng,White, Kimberley B.,de Garavilla, Lawrence,Wang, Yuanping,Minor, Lisa K.,Tounge, Brett A.,Barnakov, Alexander N.,Lewandowski, Frank,Milligan, Cynthia,Spurlino, John C.,Abraham, William M.,Boswell-Smith, Victoria,Page, Clive P.,Maryanoff, Bruce E.
, p. 2114 - 2121 (2008/12/21)
We have explored a series of spirocyclic piperidine amide derivatives (5) as tryptase inhibitors. Thus, 4 (JNJ-27390467) was identified as a potent, selective tryptase inhibitor with oral efficacy in two animal models of airway inflammation (sheep and guinea pig asthma models). An X-ray co-crystal structure of 4 · tryptase revealed a hydrophobic pocket in the enzyme's active site, which is induced by the phenylethynyl group and is comprised of amino acid residues from two different monomers of the tetrameric protein.
