149352-64-7Relevant academic research and scientific papers
SUBSTITUTED QUINOLINYL AND NAPHTHALENYLBENZAMIDES OR BENZYLAMINES AND RELATED COMPOUNDS USEFUL AS ANALGESICS
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, (2008/06/13)
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 1 ; Y is C(R 1)(R 2)O, OC(R. sup.1)(R 2), C(R 1)(R 2)N(R 3), N(R. sup.3)C(R 1)(R. sup.2) or C(R 1)=C(R 2); wherein R 1, R 2, and R 3 are independently hydrogen or lower alkyl containing 1 to 10 carbon atoms; Z is oxygen or (R 1)(R 2); R 4 is R 1, benzyl, benzyl ring substituted with R 5, benzyl alpha monosubstituted with R. sup.1, benzyl ring substituted with R 5 and alpha monosubstituted with R 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 1, lower alkoxy containing 1 to 10 carbon atoms, halogen, trihalomethyl, NO 2, N(R 1)(R 2) or C(O)N(R 1)(R 2); R 6 is R 1 or R. sup.6 is C(O)(R 7) with the proviso that Z is not oxygen; and wherein R 7 is R 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 2 O of the above structure.
