AZETIDINE AMIDE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS
The present invention relates to azetidine amide derivatives derivatives of formula (I) wherein rings A1 A2 and A3 are as described in the description, to pharmaceutically acceptable salts thereof, to their preparation, to
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Page/Page column 50
(2014/09/29)
Heteroalicyclic carboxamidines as inhibitors of inducible nitric oxide synthase; The identification of (2R)-2-pyrrolidinecarboxamidine as a potent and selective haem-co-ordinating inhibitor
Heteroalicyclic carboxamidines were synthesised and evaluated as inhibitors of nitric oxide synthases. (2R)-2-Pyrrolidinecarboxamidine, in particular, was shown to be a highly potent in vitro (IC50 = 0.12 μM) and selective iNOS inhibitor (>100-fold vs both eNOS and nNOS), with probable binding to the key anchoring glutamate residue and co-ordination to the haem iron.
Young, Robert J.,Alderton, Wendy,Angell, Anthony D.R.,Beswick, Paul J.,Brown, David,Chambers, C. Lynn,Crowe, Miriam C.,Dawson, John,Hamlett, Christopher C.F.,Hodgson, Simon T.,Kleanthous, Savvas,Knowles, Richard G.,Russell, Linda J.,Stocker, Richard,Woolven, James M.
scheme or table
p. 3037 - 3040
(2011/06/26)
AZETIDINE COMPOUNDS AS OREXIN RECEPTOR ANTAGONISTS
The invention relates to novel azetidine compounds of formula (I), wherein R1, R2, and X are as described in the description and their use as orexin receptor antagonists.