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    • 8. 发明授权
    • Pyrrolidines
    • 吡咯烷
    • US4342692A
    • 1982-08-03
    • US198671
    • 1980-10-20
    • John T. SuhRack H. ChungNai-Yi WangJeffrey N. Barton
    • John T. SuhRack H. ChungNai-Yi WangJeffrey N. Barton
    • C07C69/738A61K31/40A61P9/12A61P37/08C07C43/225C07C45/59C07C67/00C07C201/00C07C205/32C07C205/45C07D207/06C07D207/08C07D207/20C07D211/22C07D317/22C07D317/24C07D317/28C07D317/30C07D317/72
    • C07D207/08C07C205/32C07C205/45C07C43/225C07C45/59C07D207/20C07D211/22C07D317/22C07D317/24C07D317/28C07D317/30
    • Compounds of the formulae: ##STR1## wherein, Z and Y are each alkylene containing one to about five carbon atoms in the principal chain or said alkylene substituted with OH, alkanoyloxy, alkoxy, mercapto or alkylmercapto;each of R.sub.1, R.sub.2 and R.sub.3 is independently H, alkyl, aryl, halo, alkoxy, alkenyloxy, alkylsulfinyl, alkylsulfonyl, alkylmercapto, cyano, carboxy, carbalkoxy, carboxamido, sulfamoyl, trifluoromethyl, hydroxy, hydroxyalkyl, acyloxy, alkylamino, sulfonylamino, or acylamino; and R.sub.1 and R.sub.2, when taken together, form a methylenedioxy or --O--CO--O--;Ar is heteroaryl, cycloalkyl or ##STR2## wherein, R.sub.1, R.sub.2 and R.sub.3 are as hereindescribed; andR is H, alkyl, cycloalkyl, aryl, aralkyl, alkenyl, alkynyl, carboalkoxy, or CONR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is H or alkyl; wherein the total number of carbon atoms in each hydrocarbyl group is up to 10;and ##STR3## wherein, each of R.sub.1 and R.sub.2 is independently H, alkyl, aryl, halo, alkoxy, alkenyloxy, alkylsulfinyl, alkylsulfonyl, alkylmercapto, cyano, carboxy, carbalkoxy, carboxamido, sulfamoyl, trifluoromethyl, hydroxy, hydroxyalkyl, acyloxy, alkylamino, sulfonylamino, or acylamino; and R.sub.1 and R.sub.2, when taken together, form a methylenedioxy, or --O--CO--O--; R.sub.6 is H, alkyl, aryl, halo, alkoxy, alkenyloxy, alkylsulfonyl, alkylmercapto, cyano, carboxy, carbalkoxy, carboxamido, sulfamoyl, trifluoromethyl, hydroxy, hydroxyalkyl, acyloxy, alkylamino, sulfonylamino or acylamino; wherein the total number of carbon atoms in each hydrocarbyl group is up to 10; and acid addition salts thereof have selective cardiotonic, antihypertensive and antiallergic activity.
    • 下式的化合物:其中Z和Y分别是在主链中含有1至约5个碳原子的亚烷基或被OH,烷酰氧基,烷氧基,巯基或烷基巯基取代的所述亚烷基; R 1,R 2和R 3各自独立地是H,烷基,芳基,卤素,烷氧基,烯氧基,烷基亚磺酰基,烷基磺酰基,烷基巯基,氰基,羧基,烷氧基,甲酰胺基,氨磺酰基,三氟甲基,羟基,羟基烷基,酰氧基,烷基氨基,磺酰基氨基或 酰氨基; 当R 1和R 2一起形成亚甲二氧基或-O-CO-O-时; Ar是杂芳基,环烷基或者其中R 1,R 2和R 3如以下所示: 并且R为H,烷基,环烷基,芳基,芳烷基,烯基,炔基,烷氧羰基或CONR4R5,其中R4和R5各自为H或烷基; 其中每个烃基中的碳原子总数最多为10; 其中,R1和R2各自独立地为H,烷基,芳基,卤素,烷氧基,烯氧基,烷基亚磺酰基,烷基磺酰基,烷基巯基,氰基,羧基,烷氧基,甲酰氨基,氨磺酰基,三氟甲基,羟基, ,酰氧基,烷基氨基,磺酰基氨基或酰基氨基; 当R 1和R 2一起形成亚甲二氧基或-O-CO-O-时; R 6是H,烷基,芳基,卤素,烷氧基,烯氧基,烷基磺酰基,烷基巯基,氰基,羧基,烷氧基,甲酰胺基,氨磺酰基,三氟甲基,羟基,羟基烷基,酰氧基,烷基氨基,磺酰基氨基或酰基氨基; 其中每个烃基中的碳原子总数最多为10; 其酸加成盐具有选择性强心药,抗高血压药和抗过敏活性。