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    • 6. 发明授权
    • Substituted quinolinyl- and naphthalenylbenzamides or benzylamines and
related compounds useful as analgesics
    • 取代的喹啉基 - 和萘基苯甲酰胺或苄胺和相关化合物可用作镇痛药
    • US5212182A
    • 1993-05-18
    • US592160
    • 1990-10-03
    • John H. MusserAlbert J. MolinariDominick Mobilio
    • John H. MusserAlbert J. MolinariDominick Mobilio
    • C07D211/58C07D401/12
    • C07D401/12C07D211/58
    • This invention relates to novel quinolinyl- and naphthalenylbenzamides or benylamines and related disclosed compounds of the formula ##STR1## wherein X is nitrogen, NO or CR.sup.1 ; Y is C(R.sup.1)(R.sup.2)O, OC(R.sup.1)(R.sup.2), C(R.sup.1)(R.sup.2)N(R.sup.3), N(R.sup.3)C(R.sup.1)(R.sup.2) or C(R.sup.1).dbd.C(R.sup.2); wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen or lower alkyl containing 1 to 10 carbon atoms; Z is oxygen or (R.sup.1)(R.sup.2); R.sup.4 is R.sup.1, benzyl, benzyl ring substituted with R.sup.5, benzyl alpha monosubstituted with R.sup.1, benzyl ring substituted with R.sup.5 and alpha monosubstituted with R.sup.1, phenyl, phenylalkyl containing 2 to 10 carbon atoms in the alkyl group or phenylalkyl ring substituted with R.sup.5 and containing 2 to 10 carbon atoms in the alkyl group; wherein R.sup.5 is R.sup.1, lower alkoxy containing 1 to 10 carbon atoms, halogen, trihalomethyl, NO.sub.2, N(R.sup.1)(R.sup.2) or C(O)N(R.sup.1)(R.sup.2); R.sup.6 is R.sup.1 or R.sup.6 is C(O)(R.sup.7) with the proviso that Z is not oxygen; and wherein R.sup.7 is R.sup.1, phenyl, perfluoroalkyl containing 1 to 10 carbon atoms, phenylalkyl containing 1 to 10 carbon atoms in the alkyl group; or a pharmaceutically acceptable acid addition salt thereof, and their use in the treatment of pain mediated by the biological peptide, bradykinin. In particular, the preferred compounds are where X is nitrogen, and Y is CH.sub.2 O of the above structure.
    • 本发明涉及新颖的喹啉基和萘基苯甲酰胺或联苯胺及其相关公开的式(I)的化合物,其中X是氮,NO或CR 1; Y是C(R1)(R2)O,OC(R1)(R2),C(R1)(R2)N(R3),N(R3)C(R1)(R2)或C(R1) R2); 其中R1,R2和R3独立地是氢或含有1-10个碳原子的低级烷基; Z是氧或(R1)(R2); R4是R1,苄基,被R5取代的苄基环,被R1单取代的苄基,被R5取代的苄基环和被R1单取代的α,苯基,在烷基中含有2-10个碳原子的苯基烷基或被R5取代的苯基烷基, 烷基中的2至10个碳原子; 其中R 5为R 1,含有1至10个碳原子的低级烷氧基,卤素,三卤代甲基,NO 2,N(R 1)(R 2)或C(O)N(R 1)(R 2) R6是R1或R6是C(O)(R7),条件是Z不是氧; 并且其中R 7为R 1,苯基,含有1至10个碳原子的全氟烷基,烷基中含有1至10个碳原子的苯基烷基; 或其药学上可接受的酸加成盐,以及它们在治疗由生物肽缓激肽介导的疼痛的用途。 特别优选的化合物是其中X是氮,Y是上述结构的CH 2 O.