公开(公告)号：US4229448A

公开(公告)日：1980-10-21

申请号：US23504

申请日：1979-03-23

申请人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

发明人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

IPC分类号： C07D213/65 ,  C07D213/79 ,  C07D213/81 ,  A61K31/455

CPC分类号： C07D213/79 ,  C07D213/65 ,  C07D213/81

摘要： 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.

摘要翻译： 由式（I）表示的5-取代的吡啶甲酸衍生物：其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基： 其中可以相同或不同的R 3和R 4各自表示氢原子，卤素原子，低级烷基，低级烷氧基，硝基，氨基，N-烷基取代的氨基， 酰氨基，乙酰基，酰氧基，羟基或卤素取代的烷基，或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基，其中M表示氢，钠，钾，钙，铝或镁原子，具有1至6个碳原子的直链或支链或环状烷氧基，氨基烷氧基，苯氧基，取代的 苯氧基，5-茚满氧基，具有式“IMAGE”的酰氧基烷氧基，其中R5表示氢原子或甲基，R6表示碳原子数1〜6的低级烷基，苯基或取代苯基 或由式“IMAGE”表示的氨基，其中R7和R8可以相同或不同，表示可用作抗高血压剂的氢原子，低级烷基或苯基， 制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。