| 摘要 |
NEW MATERIAL:The compound of formula I [R1 is H or 1-4C alkyl; R2 is H, halogen, 1-4C alkyl or 1-4C alkoxy; R3 is H or NHCOR4; R4 is group of formula II, formula III, or COOR5 (R5 is H or lower alkyl); X is CH or N; Y is carbonyl or methylene; n is 0-3] and its salt. EXAMPLE:N,N'-(2-Methoxy-5-picolinoyl)-m-phenylene dioxamidic acid. USE:The compound exhibits the activities to suppress the passive skin anaphlactic reaction and to suppress the isolation of histamine from mastocyte, and is useful for the remedy and prevention of allergic symptom. It can be administered orally. PREPARATION:The compound of formula I can be produced by (1) nitrating and reducing the compound of formula IV, (2) reacting the resultant compound of formula V (B is H or NH2) with the compound of formula R4'-COZ [R4' is group of formula III or COOR5' (R5' is lower alkyl); Z is halogen], and if necessary, (3) hydrolyzing the reaction product. |
