| abstract |
Cyclic anthranilic acid derivatives of general formula (I) and acid addition salts and alkali salts thereof, useful for treating rheumatism, autoimmune diseases and metabolic bone diseases, wherein R?1, R?2 and R?3 may be the same of different from one another and each represents hydrogen, halogen, lower (C1? to C3?) alkyl, lower (C1? to C3?) alkoxy, amino, nitro, hydroxy, sulfonamide, trifluoromethyl, cyano, carboxyl, carbamoyl, acetyl, optionally substituted benzoylmethyl, methylthio, optionally substituted phenylethynyl, optionally substituted ethynyl, lower (C1? to C3?) alkanoylamino, optionally substituted benzoylamino, lower (C1? to C3?) alkylsulfonylamino, or optionally substituted phenylsulfonylamino; R?4 and R?5 may be the same or different from each other and each represents hydrogen, lower (C1? to C3?) alkyl, cyano, carboxyl, hydroxylmethyl, optionally substituted phenyl, or benzyl; R?6 represents hydrogen, lower (C1? to C3?) alkyl or benzyl; X represents a single bond, -CHR?7-CHR?8-(CHR?9)m?-, -O-CHR?8-(CHR?9)m?-, -S(O)n?-CHR?8-(CHR?9)m?- or -CO(CHR?8)p?-(CHR?8)m?-; R?7, R?8 and R?9 may be the same or different from one another and each represents hydrogen, lower (C1? to C3?) alkyl, cyano, carboxyl, hydroxymethyl, or optionally substituted phenyl; m and p are each 0 or 1; and n is an integer of 0 to 2; provided that R?2 represents neither chlorine nor hydrogen when both of R?7 and R?8 are hydrogen atoms and m is 0. |