申请人:Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
公开号:US04218404A1
公开(公告)日:1980-08-19
The invention relates to novel .omega.-aminocarboxylic acid amides having the formula (I) ##STR1## wherein A is --SO.sub.2 OH or --OPO(OH).sub.2, R.sup.1 is hydrogen, an acyl group, such as benzoyl, arylsulfonyl, alkoxycarbonyl, cycloalkoxycarbonyl or aralkoxycarbonyl group or an aralkoxycarbonyl group having a halogen, alkoxy, nitro, phenylazo or alkoxyphenylazo substituent, alkyl-substituted aryloxycarbonyl or carbonyl, R.sup.2 is hydrogen or a carbonyl group, with the proviso that when R.sup.1 and R.sup.2 each stand for carbonyl, the two carbonyl groups form a ring through an intervening o-phenylene, alkylene or vinylene group when A is --SO.sub.2 OH and R.sup.1 is an acyl group such as benzoyl, aryl sulfonyl, alkoxy-carbonyl, cycloalkoxycarbonyl or aryloxycarbonyl group or an aralkoxy carbonyl group having a halogen, alkoxy, nitro, phenylozo or alkoxyphenylazo substituent or an alkyl-substituted aryloxycarbonyl group or carbonyl group, R.sup.2 is hydrogen or a carbonyl group, with the proviso that when R.sup.1 and R.sup.2 each stand for carbonyl, the two carbonyl groups form a ring through an intervening o-phenylene, alkylene or vinylene group when A is --O--P--O(OH).sub.2 and n is equal to 2 or 3, and salts of the above compounds, furthermore to a process for the preparation thereof. The novel compounds according to the invention possess valuable pharmacological effects in reducing blood sugar levels or can be applied as intermediate in the synthesis of biologically active compounds.
本发明涉及具有以下式子(I)的新型ω-氨基羧酸酰胺:其中A为--SO2OH或--OPO(OH)2,R1为氢、酰基、如苯甲酰基、芳烷磺酰基、烷氧羰基、环烷氧羰基或芳基烷氧羰基或具有卤素、烷氧基、硝基、苯偶氮或烷氧基苯偶氮取代基的芳基烷氧羰基或羰基、R2为氢或羰基,但当R1和R2均为羰基时,当A为--SO2OH且R1为酰基,如苯甲酰基、芳烷磺酰基、烷氧羰基、环烷氧羰基或芳基烷氧羰基或具有卤素、烷氧基、硝基、苯偶氮或烷氧基苯偶氮取代基的芳基烷氧羰基或羰基时,两个羰基通过介于o-苯撑、烷基或乙烯基的环形结构形成;但当A为--O--P--O(OH)2且n等于2或3时,R1为苯甲酰基、芳烷磺酰基、烷氧羰基、环烷氧羰基或芳基烷氧羰基或具有卤素、烷氧基、硝基、苯偶氮或烷氧基苯偶氮取代基的芳基烷氧羰基或羰基,R2为氢或羰基,但当R1和R2均为羰基时,两个羰基通过介于o-苯撑、烷基或乙烯基的环形结构形成。本发明还涉及上述化合物的盐,并提供了一种制备它们的方法。根据本发明的新型化合物具有降低血糖水平的有价值的药理作用,或可用作生物活性化合物合成中间体。