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    Fused thiophene derivatives, their production and use
    1.
    发明授权
    Fused thiophene derivatives, their production and use 失效
    稠合噻吩衍生物，其生产和使用

    公开(公告)号：US5284661A

    公开(公告)日：1994-02-08

    申请号：US47368

    申请日：1993-04-19

    申请人： Akira Morimoto ,  Kohei Nishikawa ,  Takehiko Naka

    发明人： Akira Morimoto ,  Kohei Nishikawa ,  Takehiko Naka

    IPC分类号： C07D495/04 ,  A61K9/20

    CPC分类号： C07D495/04

    摘要： Novel fused thiophene derivatives of the formula (I): ##STR1## wherein W is ##STR2## R.sup.1 and R.sup.2 which may be same or different, are each independently hydrogen, halogen, cyano, nitro, acylamino, or a hydrocarbon residue which may be substituted; R.sup.3 is hydrogen, optionally substituted alkyl or alkenyl, or --COD wherein D is hydrogen, alkoxy, hydroxy, halogen, or optionally substituted amino; R.sup.4 is hydrogen, halogen or nitro; R.sup.5 is a residue capable of forming an anion or a residue convertible into an anion; R.sup.6 is hydrogen or optionally substituted alkyl or alkenyl; A is a direct bond or a spacer having atomic length of two or less between the phenylene group and the phenyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof have potent angiotensin II antagonist activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases, strokes, etc.

    摘要翻译： 式（I）的新型稠合噻吩衍生物：其中W为R 1和R 2可以相同或不同，各自独立地为氢，卤素，氰基，硝基，酰氨基或烃残基 可以替代; R3是氢，任选取代的烷基或烯基或-COD，其中D是氢，烷氧基，羟基，卤素或任选取代的氨基; R4是氢，卤素或硝基; R5是能够形成阴离子或可转化为阴离子的残基的残基; R6是氢或任选取代的烷基或链烯基; A是亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; n为1或2的整数; 其药学上可接受的盐具有有效的血管紧张素II拮抗剂活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏病，中风等的治疗剂。

    Benzimidazole derivatives and use thereof
    2.
    发明授权
    Benzimidazole derivatives and use thereof 失效
    苯并咪唑衍生物及其用途

    公开(公告)号：US5705517A

    公开(公告)日：1998-01-06

    申请号：US131667

    申请日：1993-10-05

    申请人： Takehiko Naka ,  Kohei Nishikawa

    发明人： Takehiko Naka ,  Kohei Nishikawa

    IPC分类号： A61K31/415 ,  C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  C07D405/14 ,  A61K31/41 ,  C07D235/06

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  C07D405/14

    摘要： Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R' is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

    摘要翻译： 式（I）的苯并咪唑衍生物：其中环A是可以任选地含有取代基的R'基团的苯环; R'是氢或任选取代的烃残基; R2是能够形成阴离子或可转换的基团的基团; X是亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; R'是羧基，其酯，其酰胺或能够形成阴离子或可转化成阴离子的基团; Y是-O - ， - S（O）m - 或-N（R4） - ，其中m是0,1或2的整数，R4是氢或任选取代的烷基; n为1或2的整数; 和其药学上可接受的盐具有有效的血管紧张素II拮抗活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏病（例如高血压，心力衰竭，心肌梗塞等），中风 ，脑中风，肾炎等

    Benzimidazole derivatives, their production and use
    3.
    发明申请
    Benzimidazole derivatives, their production and use 失效
    苯并咪唑衍生物，其生产和使用

    公开(公告)号：US20070259932A1

    公开(公告)日：2007-11-08

    申请号：US11594982

    申请日：2006-11-09

    申请人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    发明人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    IPC分类号： A61K31/4184 ,  A61K31/41 ,  A61P13/12 ,  A61P9/04 ,  A61P9/12 ,  C07D257/04 ,  C07D403/10

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14

    摘要： Benzimidazole derivatives of the formula (I): wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

    摘要翻译： 式（I）的苯并咪唑衍生物：其中环A是可以任选地除R'基团之外的取代基的苯环; R 1是氢或任选取代的烃残基; R 2是能够形成阴离子或可转换的基团的基团; X是亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; R'是羧基，其酯，其酰胺或能够形成阴离子或可转化成阴离子的基团; Y是-O - ， - S（O）m - 或-N（R 4） - ，其中m是0,1或2的整数，R 0 > 4是氢或任选取代的烷基; n为1或2的整数; 和其药学上可接受的盐具有有效的血管紧张素II拮抗活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏病（例如高血压，心力衰竭，心肌梗塞等），中风 ，脑中风，肾炎等

    Benzimidazole derivatives, their production and use
    4.
    发明授权
    Benzimidazole derivatives, their production and use 失效
    苯并咪唑衍生物，其生产和使用

    公开(公告)号：US06844443B2

    公开(公告)日：2005-01-18

    申请号：US10612984

    申请日：2003-07-07

    申请人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    发明人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    IPC分类号： A61P9/12 ,  C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  C07D257/04

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14

    摘要： A method for producing a compound represented by the formula: wherein the ring A is a benzene ring which may be substituted in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is —O—, —S(O)m- or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.

    摘要翻译： 一种制备由下式表示的化合物的方法：其中环A是除R'基之外可被取代的苯环; R 1是氢或任选取代的烃残基; X是在亚苯基和苯基之间具有原子长度或者两个或更少的直接键或间隔子; Y是-O - ， - S（O）m - 或-N（R 4） - ，其中m是0,1或2的整数，R 4是氢或任选取代的烷基; R'是羧基，其酯，其酰胺或能够形成阴离子的基团或可转化的基团; n为1或2的整数; 其包括使由下式表示的化合物脱保护：其中R是三苯甲基，2-四氢吡喃基，甲氧基甲基或乙氧基甲基，其它符号如上定义; 或其盐。

    Benzimidazole derivatives, their production and use
    5.
    发明授权
    Benzimidazole derivatives, their production and use 失效
    苯并咪唑衍生物，其生产和使用

    公开(公告)号：US5703110A

    公开(公告)日：1997-12-30

    申请号：US715100

    申请日：1996-09-17

    申请人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    发明人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    IPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  A01N43/50 ,  A61K31/41 ,  C07D235/12

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10

    摘要： Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

    摘要翻译： 式（I）的苯并咪唑衍生物：其中环A是可以任选地含有取代基的R'基团的苯环; R1是氢或任选取代的烃残基; R2是能够形成阴离子或可转换的基团的基团; X是亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; R'是羧基，其酯，其酰胺或能够形成阴离子或可转化成阴离子的基团; Y是-O - ， - S（O）m - 或-N（R4） - ，其中m是0,1或2的整数，R4是氢或任选取代的烷基; n为1或2的整数; 和其药学上可接受的盐具有有效的血管紧张素II拮抗活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏病（例如高血压，心力衰竭，心肌梗塞等），中风 ，脑中风，肾炎等

    Benzimidazole derivatives, their production and use
    7.
    发明授权
    Benzimidazole derivatives, their production and use 失效
    苯并咪唑衍生物，其生产和使用

    公开(公告)号：US07538133B2

    公开(公告)日：2009-05-26

    申请号：US11594982

    申请日：2006-11-09

    申请人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    发明人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    IPC分类号： A61K31/41 ,  C07D257/04

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14

    摘要： Benzimidazole derivatives of the formula (I): wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; R2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.

    摘要翻译： 式（I）的苯并咪唑衍生物：其中环A是可以任选地除R'基团之外的取代基的苯环; R1是氢或任选取代的烃残基; R2是能够形成阴离子或可转换的基团的基团; X是亚苯基和苯基之间的原子长度为2以下的直接键或间隔物; R'是羧基，其酯，其酰胺或能够形成阴离子或可转化成阴离子的基团; Y是-O - ， - S（O）m - 或-N（R4） - ，其中m是0,1或2的整数，R4是氢或任选取代的烷基; n为1或2的整数; 和其药学上可接受的盐具有有效的血管紧张素II拮抗活性和抗高血压活性，因此可用作治疗循环系统疾病如高血压疾病，心脏病（例如高血压，心力衰竭，心肌梗塞等），中风 ，脑中风，肾炎等

    Benzimidazole derivatives, their production and use
    8.
    发明授权
    Benzimidazole derivatives, their production and use 失效
    苯并咪唑衍生物，其生产和使用

    公开(公告)号：US06608210B2

    公开(公告)日：2003-08-19

    申请号：US10046189

    申请日：2002-01-16

    申请人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    发明人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    IPC分类号： C07D25702

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14

    摘要： A method for producing a compound represented by the formula: wherein the ring A is a benzene ring which may be substituted in addition to the R′ group; R1 is hydrogen or an optionally substituted hydrocarbon residue; X is a direct bond or a spacer having an atomic length or two or less between the phenylene group and the phenyl group; Y is —O—, —S(O)m— or —N(R4)— wherein m is an integer of 0, 1 or 2 and R4 is hydrogen or an optionally substituted alkyl group; R′ is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or a group convertible thereinto; n is an integer of 1 or 2; or a salt thereof, which comprises deprotecting a compound represented by the formula: wherein R is triphenylmethyl, 2-tetrahydropyranyl, methoxymethyl or ethoxy methyl, the other symbols as defined above; or a salt thereof.

    摘要翻译： 一种制备由下式表示的化合物的方法：其中环A是除R'基之外可被取代的苯环; R1是氢或任选取代的烃残基; X是在亚苯基和苯基之间具有原子长度或者两个或更少的直接键或间隔子; Y是-O - ， - S（O）m - 或-N（R4） - ，其中m是0,1或2的整数，R4是氢或任选取代的烷基; R'是羧基，其酯，其酰胺或能够形成阴离子的基团或可转化的基团; n为1或2的整数; 其包括使由下式表示的化合物脱保护：其中R是三苯甲基，2-四氢吡喃基，甲氧基甲基或乙氧基甲基，其它符号如上定义; 或其盐。

    Benzimidazole derivatives, their production and use
    9.
    发明授权
    Benzimidazole derivatives, their production and use 失效

    公开(公告)号：US6004989A

    公开(公告)日：1999-12-21

    申请号：US280094

    申请日：1999-03-29

    申请人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    发明人： Takehiko Naka ,  Kohei Nishikawa ,  Takeshi Kato

    IPC分类号： A61P9/12 ,  C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/10 ,  A61K31/41 ,  C07D235/12 ,  C07D257/04

    CPC分类号： C07D235/02 ,  C07D235/26 ,  C07D235/28 ,  C07D235/30 ,  C07D403/04 ,  C07D403/10 ,  C07D405/14

    摘要： Benzimidazole derivatives of the formula (I): ##STR1## wherein the ring A is a benzene ring which may optionally contain substitution in addition to the R' group; R.sup.1 is hydrogen or an optionally substituted hydrocarbon residue; R.sup.2 is a group capable of forming an anion or a group convertible thereinto; X is a direct bond or a spacer having an atomic length of two or less between the phenylene group and the phenyl group; R' is carboxyl, an ester thereof, an amide thereof or a group capable of forming an anion or convertible to an anion; Y is --O--, --S(O).sub.m -- or --N(R.sup.4)-- wherein m is an integer of 0, 1 or 2 and R.sup.4 is hydrogen or an optionally substituted alkyl group; and n is an integer of 1 or 2; and the pharmaceutically acceptable salts thereof, have potent angiotensin II antagonistic activity and antihypertensive activity, thus being useful as therapeutic agents for treating circulatory system diseases such as hypertensive diseases, heart diseases (e.g. hypercardia, heart failure, cardiac infarction, etc.), strokes, cerebral apoplexy, nephritis, etc.