N-benzenesulfonyl l-proline compounds as bradykinin antagonists

Details N-benzenesulfonyl l-proline compounds as bradykinin antagonists N-benzenesulfonyl l-proline compounds as bradykinin antagonists

C - Chemistry, Metallurgy

07

D

C07D 401/14 (2006.01) A61K 31/4709 (2006.01) A61K 31/496 (2006.01) A61P 9/00 (2006.01) A61P 25/28 (2006.01) A61P 29/00 (2006.01) C07D 401/12 (2006.01) C07D 451/02 (2006.01) C07D 451/04 (2006.01) C07D 453/02 (2006.01) C07D 487/08 (2006.01)

Patent

CA 2364178

This invention provides a compound of the formula (I): Image or the pharmaceutically acceptable salts thereof wherein X1 and X2 are halo; R1 and R2 are independently hydrogen or C1-4 alkyl; R3 and R4 are each hydrogen or halo; and R5 is ~(a) -C3-9 diazacycloalkyl optionally substituted with C5-11 azabicycloalkyl; (b) -C3-9 azacycloalkyl-NH-(C5-11 azabicycloalkyl optionally substituted with C1-4 alkyl); (c) -NH-C1-3 alkyl-C(O)-C5-11 diazabicycloalkyl; (d) -NH-C1-3 alkyl-C(O)-NH-C5-11 azabicycloalkyl, the C5-11 azabicycloalkyl being optionally substituted with C1-4 alkyl; (e) -C3-9 azacycloalkyl optionally substituted with C3-9 azacycloalkyl; or (f) -NH-C1-5 alkyl-NH-C(O)-C4-9 cycloalkyl-NH2. 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.

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