| 摘要 |
The present invention relates to new sulfonamide derivatives of formula (I)wherein Ris hydrogen atom or C-Calkyl group; Ris selected from (1) hydrogen atom; (2) C-Cstraight or branched alkyl group; (3) -(CH)-NH; (4) -(CH)-OH; (5) -(CH)-CO-NH; (6) benzyl optionally substituted with hydroxy group or halogen atom; or R, Rand the carbon atom to which they are both attached together form a 3-7 membered cycloalkyl ring; Ris (1) hydrogen atom, (2) C-Cstraight or branched alkyl group, optionally substituted with one or more substituents independently selected from amino, hydroxy, 1H-imidazol-4-yl, -NRR, -COOR, -NH-C(=NH)-NH, -CO-NHgroup; Ris (1) hydrogen atom, (2) -(CH)-NRRgroup; (3) -(CH)-X-P group; R, Rand Rare independently of each other hydrogen atom, halogen atom, cyano, nitro, amino, or amino substituted with one or more C-Calkyl group; trifluoromethyl; C-Calkoxy or trifluoromethoxy; Ris hydrogen atom or C-Calkyl group; Z is selected from (1) single bond; (2) oxygen atom; (3) CHgroup; (4) CO group; (5) NRgroup; n is an integer from 0 to 6; m is an integer from 0 to 6; X is selected from (1) single bond; or CO; P is selected from (1) phenyl group, optionally substituted with -(CH)-CN, -O-CO-NRR, -NH-CO-R, [l,4']bipiperidinyl'-yl or -(CH)-NH-C(=NH)-NHgroup; (2) a saturated, partially unsaturated or aromatic 4-7 membered ring containing 1-3 heteroatom selected from O, S and N; wherein said ring is optionally substituted with one or more halogen atom, trifluoromethyl, -NH-CO-R, -C(=NH)-NH, C-Calkyl, pyridin-4-yl, piperidin-1-yl; (3) a system consisting of saturated or aromatic 9 membered bicyclic ring containing 1-2 heteroatom selected from O, S and N; wherein said ring system is optionally substituted with one or more halogen atom, (4) C-Ccycloalkyl group, optionally substituted with -(CH)-NRRgroup; Rand Rare (1) hydrogen atom; (2) straight or branched C-Calkyl group; (3) R, Rand the nitrogen atom to which they are both attached together form a saturated, partially unsaturated or aromatic 5-6-membered ring containing 0-1 heteroatom (in addition to the nitrogen atom to which Rand Rattached) selected from O, S and N; wherein said ring is optionally substituted with C-Calkyl group; Ris hydrogen atom or C-Calkyl group, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to a process for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions. |
