公开(公告)号：USRE35321E

公开(公告)日：1996-08-27

申请号：US951720

申请日：1992-09-25

申请人： Sinji Inukai ,  Mitsuzi Agata ,  Manami Umezawa ,  Yoshihiro Horio ,  Yasuhiro Ootake ,  Shohei Sawaki ,  Masayoshi Goto

发明人： Sinji Inukai ,  Mitsuzi Agata ,  Manami Umezawa ,  Yoshihiro Horio ,  Yasuhiro Ootake ,  Shohei Sawaki ,  Masayoshi Goto

IPC分类号： A61K31/41 ,  A61P3/08 ,  A61P3/10 ,  A61P13/02 ,  A61P15/00 ,  A61P25/02 ,  A61P27/02 ,  A61P27/12 ,  C07D257/04 ,  C07D405/04 ,  C07D409/04

CPC分类号： C07D405/04 ,  C07D409/04

摘要： A tetrazoleacetic acid derivative represented by the following general formula (I): ##STR1## .[.[in Formula (I),.]. .Iadd.wherein .Iaddend.R.sub.1 represents a hydrogen atom or an alkyl group; R.sub.2 represents a hydrogen atom, an alkyl group, an aralkyl group, a halogen atom, a haloalkyl group, a hydroxyl group, an alkoxy group, an alkoxyalkyl group, an amino group, an aryl group, an alkyl or aryl thio group, an alkyl or aryl carbonylamino group, an alkyl or aryl sulfonylamino group, an alkyl or aryl aminosulfonyl group, an alkyl or aryl sulfonyl group or an alkyl or aryl sulfinyl group; and X represents --O-- or --S--.[.].]. except for [5-(2-thienyl)tetrazol-1-yl] acetic acid, [5-(2-furyl)tetrazol-1-yl) acetic acid.Iadd., (5-(5-bromo-2-furyl)tetrazol-1-yl)acetic acid, (5-(5-phenylthio-2-furyl)tetrazol-1-yl)acetic acid, (5-(5-phenylsulfonyl-2-furyl)tetrazol-1-yl)acetic acid .Iaddend.and ethyl esters thereof, or a salt thereof shows excellent aldose reductase inhibitory activity, has low toxicity to organisms and is quite effective as an essential component of a preventative medicine and/or remedy for diabetic complications.

摘要翻译： 由下列通式（I）表示的四唑乙酸衍生物：其中R1表示氢原子或烷基;（I） R 2表示氢原子，烷基，芳烷基，卤素原子，卤代烷基，羟基，烷氧基，烷氧基烷基，氨基，芳基，烷基或芳基硫基， 烷基或芳基羰基氨基，烷基或芳基磺酰基氨基，烷基或芳基氨基磺酰基，烷基或芳基磺酰基或烷基或芳基亚磺酰基; 和[5-（2-噻吩基）四唑-1-基]乙酸，[5-（2-呋喃基）四唑-1-基）乙酸]（其中X表示-O-或-S- [ （5-（5-溴-2-呋喃基）四唑-1-基）乙酸，（5-（5-苯基硫代-2-呋喃基）四唑-1-基）乙酸（5-（5-苯基磺酰基-2 - 呋喃基）四唑-1-基）乙酸及其乙酯或其盐显示出优异的醛糖还原酶抑制活性，对生物体具有低毒性，并且作为预防药物和/或糖尿病治疗的必需成分是非常有效的 并发症。

公开(公告)号：US5068239A

公开(公告)日：1991-11-26

申请号：US588057

申请日：1990-09-24

申请人： Sinji Inukai ,  Mitsuzi Agata ,  Manami Umezawa ,  Yoshihiro Horio ,  Yasuhiro Ootake ,  Shohei Sawaki ,  Masayoshi Goto

发明人： Sinji Inukai ,  Mitsuzi Agata ,  Manami Umezawa ,  Yoshihiro Horio ,  Yasuhiro Ootake ,  Shohei Sawaki ,  Masayoshi Goto

IPC分类号： A61K31/41 ,  A61P3/08 ,  A61P3/10 ,  A61P13/02 ,  A61P15/00 ,  A61P25/02 ,  A61P27/02 ,  A61P27/12 ,  C07D257/04 ,  C07D405/04 ,  C07D409/04

CPC分类号： C07D405/04 ,  C07D409/04

摘要： A tetrazoleacetic acid derivative represented by the following general formula (I): ##STR1## [in Formula (I), R.sub.1 represents a hydrogen atom or an alkyl group; R.sub.2 represents a hydrogen atom, an alkyl group, an aralkyl group, a halogen atom, a haloalkyl group, a hydroxyl group, an alkoxy group, an alkoxyalkyl group, an amino group, an aryl group, an alkyl or aryl thio group, an alkyl or aryl carbonylamino group, an alkyl or aryl sulfonylamino group, an alkyl or aryl aminosulfonyl group, an alkyl or aryl sulfonyl group or an alkyl or aryl sulfinyl group; and X represents --O-- or --S--] except for [5-(2-thienyl)tetrazol-1-yl] acetic acid, [5-(2-furyl)tetrazol-1-yl] acetic acid and ethyl esters thereof, or a salt thereof shows excellent aldose reductase inhibitory activity, has low toxicity to organisms and is quite effective as an essential component of a preventive medicine and/or remedy for diabetic complications.

公开(公告)号：US5262433A

公开(公告)日：1993-11-16

申请号：US924453

申请日：1992-08-04

申请人： Yoshihiro Horio ,  Yasuhiro Ootake ,  Shohei Sawaki ,  Sinji Inukai ,  Mitsuji Agata ,  Manami Umezawa ,  Masayoshi Goto

发明人： Yoshihiro Horio ,  Yasuhiro Ootake ,  Shohei Sawaki ,  Sinji Inukai ,  Mitsuji Agata ,  Manami Umezawa ,  Masayoshi Goto

IPC分类号： C07D257/04 ,  C07D405/04 ,  C07D409/04 ,  A61K31/41 ,  C07D407/04

CPC分类号： C07D257/04 ,  C07D405/04 ,  C07D409/04

摘要： A tetrazoleacetic acid derivative represented by the following general formula I: ##STR1## wherein in the formula I, R represents a hydrogen atom or a lower alkyl group; A is an alkylene group having 2 to 5 carbon atoms; Ar is selected from the group consisting of a phenyl group, a naphthyl group, a furyl group, a thienyl group, a benzofuryl group, and a benzothienyl group; wherein the Ar may be substituted with a lower alkyl group, a lower alkoxy group, a halogen atom, a lower haloalkyl group, an alkylthio group and an alkylsulfonylamino group shows excellent aldose reductase inhibitory activity, and is quite effective as an essential component of a preventive medicine and/or remedy for diabetic complications.