Dihydropyridine derivatives as bradykinin antagonists

Details Dihydropyridine derivatives as bradykinin antagonists Dihydropyridine derivatives as bradykinin antagonists

C - Chemistry, Metallurgy

07

D

C07D 211/90 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/54 (2006.01) C07D 401/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 405/00 (2006.01) C07D 405/06 (2006.01) C07D 409/00 (2006.01) C07D 409/06 (2006.01) C07D 413/00 (2006.01) C07D 417/00 (2006.01) C07D 451/04 (2006.01) C07D 453/02 (2006.01)

Patent

CA 2198231

A compound of formula (I) and its pharmaceutically acceptable salts, wherein A1 and A2 are each halo; X is direct bond, CH2, CO, O, S, S(O) or S(O)2; R1 is selected from a variety of groups such as hydrogen; substituted or unsubstituted C1-4 alkyl; substituted or unsubstituted piperidinyl; substituted or unsubstituted C5-14 cycloalkyl, bicycloalkyl or tricycloalkyl; substituted or unsubstituted C7-14 azacyclo-, azabicyclo- or azatricyclo- alkyl; bicyclo C7-10 alkenyl; benzocyclo C5-7 alkyl; and heterocyclic; R2 is hydrogen, C1-4 alkyl, substituted or unsubstituted phenyl or heterocyclic; and R3 and R4 are each C1-5 alkyl. The novel dihydropyridine compounds of this invention have excellent bradykinin antagonistic activity and are thus useful for the treatment of inflammation, cardiovascular disease, pain, common cold, allergies, asthma, pancreatitis, burns, virus infection, head injury, multiple trauma or the like in mammalian, especially humans.

Composé de la formule (I), ainsi que ses sels acceptables sur le plan pharmaceutique, dans laquelle A?1¿ et A?2¿ représentent chacun halo; X représente une liaison directe, CH¿2?, CO, O, S, S(O) ou S(O)¿2?; R?1¿ est choisi parmi plusieurs groupes tels qu'hydrogène; alkyle C¿1-4? substitué ou non, pipéridinyle substitué ou non; cycloalkyle, bicycloalkyle ou tricycloalkyle C¿5-14? substitués ou non; azacyclo-, azabicyclo- ou azatricycloalkyle C¿7-14?, substitués ou non; bicyclo-alcényle C¿7-10?; benzocyclo-alkyle C¿5-7?; et hétérocyclique; R?2¿ représente hydrogène, alkyle C¿1-4?, phényle substitué ou non, ou hétérocyclique; et R?3¿ et R?4¿ représentent chacun alkyle C¿1-5?. Les nouveaux composés dihydropyridine de cette invention possèdent une excellente activité antagoniste des bradykinines et sont par conséquent utiles dans le traitement, chez les mammifères et notamment chez l'homme, de l'inflammation, des maladies cardio-vasculaires, de la douleur, du rhume banal, des allergies, de l'asthme, de la pancréatite, des brûlures, des infections à virus, des traumatismes crâniens, des traumatismes multiples ou analogues.

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