N-benzenesulfonyl L-proline compounds as bradykinin antagonists

   
   

This invention provides a compound of the formula (I): ##STR1## or the pharmaceutically acceptable salts thereof wherein X.sup.1 and X.sup.2 are halo; R.sup.1 and R.sup.2 are independently hydrogen or C.sub.1-4 alkyl; R.sup.3 and R.sup.4 are each hydrogen or halo; and R.sup.5 is (a) --C.sub.3-9 diazacycloalkyl optionally substituted with C.sub.5-11 azabicycloalkyl; (b) --C.sub.3-9 azacycloalkyl-NH--(C.sub.5-11 azabicycloalkyl optionally substituted with C.sub.1-4 alkyl); (c) --NH--C.sub.1-3 alkyl-C(O)--C.sub.5-11 diazabicycloalkyl; (d) --NH--C.sub.1-3 alkyl-C(O)--NH--C.sub.5-11 azabicycloalkyl, the C.sub.5-11 azabicycloalkyl being optionally substituted with C.sub.1-4 alkyl; (e) --C.sub.3-9 azacycloalkyl optionally substituted with C.sub.3-9 azacycloalkyl; or (f) --NH--C.sub.1-5 alkyl-NH--C(O)--C.sub.4-9 cycloalkyl-NH.sub.2. These compounds are useful for the treatment of medical conditions mediated by bradykinin such as inflammation, allergic rhinitis, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.

Questa invenzione fornisce un residuo della formula (i): ## del ## STR1 o i sali farmaceuticamente accettabili di ciò in cui X.sup.1 e X.sup.2 sono guidacarta; R.sup.1 e R.sup.2 sono indipendentemente idrogeno o alchile C.sub.1-4; R.sup.3 e R.sup.4 sono ogni idrogeno o guidacarta; e R.sup.5 è (a) -- il diazacycloalkyl C.sub.3-9 facoltativamente sostituito con il azabicycloalkyl C.sub.5-11; (b) -- C.sub.3-9 azacycloalkyl-NH -- il azabicycloalkyl (C.sub.5-11 facoltativamente ha sostituito con alchile C.sub.1-4); (c) -- NH -- C.sub.1-3 alchile-C(O) -- diazabicycloalkyl C.sub.5-11; (d) -- NH -- C.sub.1-3 alchile-C(O) -- NH -- C.sub.5-11 azabicycloalkyl, il azabicycloalkyl C.sub.5-11 facoltativamente che si è sostituito con l'alchile C.sub.1-4; (e) -- Il azacycloalkyl C.sub.3-9 facoltativamente ha sostituito con il azacycloalkyl C.sub.3-9; o (f) -- NH -- C.sub.1-5 alchile-NH -- C(O) -- C.sub.4-9 cycloalkyl-NH.sub.2. Questi residui sono utili per il trattamento delle circostanze mediche mediate da bradykinin quali infiammazione, rhinitis allergico, dolore, ecc. Questa invenzione inoltre fornisce una composizione farmaceutica che contiene il suddetto residuo.

 
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