4-bromo-5-(2-chloro-benzoylamino)-1h-pyrazole-3-carboxylic...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 231/40 (2006.01) A61K 31/415 (2006.01) A61K 31/4155 (2006.01) A61P 29/00 (2006.01)

Patent

CA 2524318

Disclosed are compounds that are bradykinin B1 receptor antagonists of formulae (I) and (II) and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action. Formula (I) and (II) wherein Z~ is selected from O, S and NH; R1 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heteroaryl, substituted heteroaryl, heterocyclic and substituted heterocyclic; R2 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl; R3 is selected from the group consisting of hydrogen, alkyl, and substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, cycloalkyl, substituted cycloalkyl, heteroaryl, substituted heteroaryl, heterocyclic and substituted heterocyclic; R4 is selected from the group consisting of aryl, substituted aryl, heteroaryl, and substituted heteroaryl; R5 is selected from the group consisting of hydrogen, alkyl and substituted alkyl; X is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aryl, substituted aryl, carboxyl, carboxyl esters, cyano, halo, heteroaryl, substituted heteroaryl, hydroxy, nitro, amino, substituted amino, acylamino, and aminoacyl.

L'invention a trait à des composés, qui sont des antagonistes du récepteur B¿1? à la bradykinine et sont utiles pour traiter des maladies ou soulager des symptômes indésirables associés à des états pathologiques chez des mammifères, lesdits maladies et états pathologiques étant induits par le récepteur B¿1? à la bradykinine. Certains desdits composés présentent une puissance améliorée, et sont considérés comme ayant en outre une action de plus longue durée.

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