[EN] SUBSTITUTED 1-AMINOALKYL-LACTAMS AND THEIR USE AS MUSCARINIC RECEPTOR ANTAGONISTS<br/>[FR] 1-AMINOALKYLE-LACTAMES SUBSTITUES ET LEUR UTILISATION EN TANT QU'ANTAGONISTES DE RECEPTEUR MUSCARINIQUE
申请人:HOFFMANN LA ROCHE
公开号:WO2001090081A1
公开(公告)日:2001-11-29
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula (I) wherein one of X, Y or Z is independently -S-,-0- CH2- or ⊃N-R6, the others are -CH¿2?-; m is an integer from 0 to 3 inclusive; n is an integer from 1 to 6 inclusive; R?4¿ is (C¿1-6?)-alkyl; R?5¿ is independently in each occurrence (C¿1-6?)-alkyl, (C1-6)-alkenyl, (C1-6)- alkynyl or cycloalkyl; and R?1, R2, and R3¿ are hydrogen or specified substituents. These compounds are useful for treating diseases associated with smooth muscle disorders.
Heterocyclylalkylamines as muscarinic receptor antagonists
申请人:——
公开号:US20040087581A1
公开(公告)日:2004-05-06
This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I:
1
wherein X, Y, and Z are O, S or NR
5
, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
N,N'-(2,6-pyrazinediyl)bis(2-oxoglycine) derivatives are useful as antiallergic agents. The compounds are prepared by starting with an appropriate 2,6-diaminopyrazine and reacting that with an alkyl oxalyl halide.