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    Bisarylamines
    3.
    发明授权
    Bisarylamines 失效
    二芳基胺

    公开(公告)号：US4795757A

    公开(公告)日：1989-01-03

    申请号：US932557

    申请日：1986-11-20

    申请人： John R. Regan ,  Jeffrey N. Barton ,  John T. Suh ,  Jerry W. Skiles

    发明人： John R. Regan ,  Jeffrey N. Barton ,  John T. Suh ,  Jerry W. Skiles

    IPC分类号： C07C255/46 ,  C07D209/08 ,  C07D215/06 ,  C07D217/02 ,  A61K31/40 ,  C07D209/04

    CPC分类号： C07C255/46 ,  C07D209/08 ,  C07D215/06 ,  C07D217/02

    摘要： Compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein: Ar is phenyl, naphthyl, heteroaryl, indole, or fused arylcycloalkyl optionally substituted with hydroxy, halo, CF.sub.3, NO.sub.2, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or aryloxy;A and A' are each hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy or aryloxy;X is cyano, nitro, COOR, SR, SOR or SOOR;R is H, C.sub.1-6 alkyl or aryl;n n' and n" are each 0 to 4; andm, m' and m" are each 1 to 4, have calcium channel blocking activity.

    摘要翻译： 其中：Ar为任选被羟基取代的苯基，萘基，杂芳基，吲哚或稠合的芳基环烷基，其中R 1，R 2，R 3，R 4， ，CF 3，NO 2，C 1-6烷基，C 1-6烷氧基或芳氧基; A和A'各自为氢，C 1-6烷基，C 1-6烷氧基，羟基或芳氧基; X是氰基，硝基，COOR，SR，SOR或SOOR; R为H，C 1-6烷基或芳基; n n和n“分别为0〜4; m，m'和m“各自为1〜4，具有钙通道阻断活性。

    Method of using phenyl-alkylene-2-pyridyl derivatives to increase cardiac contractility in a mammal
    4.
    发明授权
    Method of using phenyl-alkylene-2-pyridyl derivatives to increase cardiac contractility in a mammal 失效
    使用苯基 - 亚烷基-2-吡啶基衍生物增加哺乳动物心脏收缩力的方法

    公开(公告)号：US4569941A

    公开(公告)日：1986-02-11

    申请号：US692602

    申请日：1985-01-17

    申请人： John T. Suh ,  Rack H. Chung, deceased ,  Nai-Yi Wang ,  Jeffrey N. Barton

    发明人： John T. Suh ,  Rack H. Chung, deceased ,  Nai-Yi Wang ,  Jeffrey N. Barton

    IPC分类号： C07D207/08 ,  C07D211/22 ,  A61K31/445

    CPC分类号： C07D207/08 ,  C07D211/22

    摘要： Compounds of the formulae: ##STR1## wherein, Z and Y are each alkylene or oxy-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; or 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; or 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.

    摘要翻译： 下式的化合物：其中Z和Y分别是在主链中含有一至五个碳原子的亚烷基或氧代 - 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。

    Pyrrolidines
    9.
    发明授权
    Pyrrolidines 失效
    吡咯烷

    公开(公告)号：US4342692A

    公开(公告)日：1982-08-03

    申请号：US198671

    申请日：1980-10-20

    申请人： John T. Suh ,  Rack H. Chung ,  Nai-Yi Wang ,  Jeffrey N. Barton

    发明人： John T. Suh ,  Rack H. Chung ,  Nai-Yi Wang ,  Jeffrey N. Barton

    IPC分类号： C07C69/738 ,  A61K31/40 ,  A61P9/12 ,  A61P37/08 ,  C07C43/225 ,  C07C45/59 ,  C07C67/00 ,  C07C201/00 ,  C07C205/32 ,  C07C205/45 ,  C07D207/06 ,  C07D207/08 ,  C07D207/20 ,  C07D211/22 ,  C07D317/22 ,  C07D317/24 ,  C07D317/28 ,  C07D317/30 ,  C07D317/72

    CPC分类号： C07D207/08 ,  C07C205/32 ,  C07C205/45 ,  C07C43/225 ,  C07C45/59 ,  C07D207/20 ,  C07D211/22 ,  C07D317/22 ,  C07D317/24 ,  C07D317/28 ,  C07D317/30

    摘要： 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.

    摘要翻译： 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。