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    Aryloxy-substituted benzimidazole derivatives
    5.
    发明授权
    Aryloxy-substituted benzimidazole derivatives 有权
    芳氧基取代的苯并咪唑衍生物

    公开(公告)号：US07932394B2

    公开(公告)日：2011-04-26

    申请号：US11666555

    申请日：2005-11-01

    申请人： Noriaki Hashimoto ,  Keiji Takahashi ,  Chisato Nakama ,  Yoshio Ogino ,  Fumiko Sakai ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    发明人： Noriaki Hashimoto ,  Keiji Takahashi ,  Chisato Nakama ,  Yoshio Ogino ,  Fumiko Sakai ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    IPC分类号： C07D401/00 ,  A61K31/445

    CPC分类号： A61K38/31 ,  A61K31/155 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K38/28 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/06 ,  C07D413/14 ,  A61K2300/00

    摘要： A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.

    摘要翻译： 提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防，或治疗和/或预防糖尿病如视网膜病，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的治疗和/或预防肥胖症。 本发明涉及式（I）化合物：其中R 1和R 2表示氢等; R3表示氢原子，卤原子等; R4各自独立地表示氢原子，低级烷基等; Q表示碳原子，氮原子或硫原子（硫原子可以被氧代基单取代或二取代）。 R5和R6各自表示氢原子，低级烷基等; X1，X2，X3和X4各自独立地表示碳原子或氮原子; Z表示氧原子，硫原子或氮原子; Ar表示任选被选自取代基组中的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数， n表示0〜3的整数， p表示0〜2的整数（X1〜X4中的至少2个为碳原子）。 q表示0或1]或其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用作糖尿病的治疗。

    Aryloxy-Substituted Benzimidazole Derivatives
    6.
    发明申请
    Aryloxy-Substituted Benzimidazole Derivatives 有权
    芳氧基取代的苯并咪唑衍生物

    公开(公告)号：US20080125429A1

    公开(公告)日：2008-05-29

    申请号：US11666555

    申请日：2005-11-01

    申请人： Noriaki Hashimoto ,  Keiji Takahashi ,  Chisato Nakama ,  Yoshio Ogino ,  Fumiko Sakai ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    发明人： Noriaki Hashimoto ,  Keiji Takahashi ,  Chisato Nakama ,  Yoshio Ogino ,  Fumiko Sakai ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    IPC分类号： A61K31/5377 ,  C07D213/02 ,  C07D221/00 ,  C07D239/06 ,  C07D241/10 ,  C07D295/00 ,  A61P3/10 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/506 ,  A61K31/497

    CPC分类号： A61K38/31 ,  A61K31/155 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K38/28 ,  A61K45/06 ,  C07D401/04 ,  C07D401/14 ,  C07D413/06 ,  C07D413/14 ,  A61K2300/00

    摘要： A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.

    摘要翻译： 提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防，或治疗和/或预防糖尿病如视网膜病，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的治疗和/或预防肥胖症。 本发明涉及式（I）的化合物：其中R 1和R 2代表氢等; R 3表示氢原子，卤素原子等; R 4各自独立地表示氢原子，低级烷基等; Q表示碳原子，氮原子或硫原子（硫原子可以被氧代基单取代或二取代）。 R 5和R 6各自表示氢原子，低级烷基等; X 1，X 2，X 3和X 4各自独立地表示碳原子或氮原子; Z表示氧原子，硫原子或氮原子; Ar表示任选被选自取代基组β的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数， n表示0〜3的整数， p表示0〜2的整数（条件是X 1〜X 4中的至少2个为碳原子）; q表示0或1]或其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用作糖尿病的治疗。

    Aminobenzamide derivative
    7.
    发明授权
    Aminobenzamide derivative 失效
    氨基苯甲酰胺衍生物

    公开(公告)号：US07253188B2

    公开(公告)日：2007-08-07

    申请号：US10952471

    申请日：2004-09-27

    申请人： Teruyuki Nishimura ,  Tomoharu Iino ,  Yasufumi Nagata ,  Jun-ichi Eiki

    发明人： Teruyuki Nishimura ,  Tomoharu Iino ,  Yasufumi Nagata ,  Jun-ichi Eiki

    IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/4427 ,  A61K31/506 ,  A61K31/5377 ,  A61P3/04 ,  A61P3/10 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  A61K31/47 ,  A61K31/497 ,  A61K31/501

    CPC分类号： C07D401/12 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  C07D277/46 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    摘要： This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, —S—(O)q-B or —O-D, wherein p and q, which are the same or different, each represent an integer from 0 to 2, A is a straight chain C1-C10 alkyl group which may be substituted by R10, and B and D each independently represent R12 which may be substituted by R10; R2 is a hydrogen atom, a halogen atom, or a straight chain or branched C1-C6 alkyl group which may be substituted by R10; X1 and X2 each independently represent N or CH, but cannot both be N; the formula (II): shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R10; R10 is R11, or a hydrocarbon group which may be substituted by R11; R11 is, for example, a hydrogen atom or amino; and R12 is, for example, phenyl, thiazolyl, pyridyl or methylene dioxyphenyl. The compound according to this invention has a glucokinase activation effect, and for example, is useful in the treatment and prevention of diabetes mellitus, and in the prevention of its complications such as diabetic nephropathy, diabetic retinopathy, diabetic neuropathy and diabetic arteriosclerosis.

    摘要翻译： 本发明涉及由式（I）表示的新化合物或其药学上可接受的盐，其中R 1是-S（O）p A，-S-（O）qB或-OD 其中相同或不同的p和q各自表示0至2的整数，A是可以被R 10取代的直链C 1 -C 10烷基，B和 D各自独立地表示可被R 10取代的R 12， R 2是氢原子，卤素原子或可被R 10取代的直链或支链C 1 -C 6烷基; X 1和X 2各自独立地表示N或CH，但不能都是N; 式（II）表示具有与结合到酰胺基上的碳原子相邻的氮原子的单环或双环杂芳基，杂芳基可以被R 10取代; R 10是R 11，或可被R 11取代的烃基; R 11是例如氢原子或氨基; R 12是例如苯基，噻唑基，吡啶基或亚甲基二氧苯基。 根据本发明的化合物具有葡糖激酶活化作用，例如可用于治疗和预防糖尿病，并且可用于预防其并发症如糖尿病性肾病，糖尿病性视网膜病，糖尿病性神经病和糖尿病性动脉硬化。

    Isoindole derivatives
    8.
    发明授权
    Isoindole derivatives 失效
    异吲哚衍生物

    公开(公告)号：US06608098B1

    公开(公告)日：2003-08-19

    申请号：US10069376

    申请日：2002-02-25

    申请人： Toshio Nagase ,  Tomoharu Iino ,  Yoshiyuki Sato ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    发明人： Toshio Nagase ,  Tomoharu Iino ,  Yoshiyuki Sato ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    IPC分类号： A61K31403

    CPC分类号： C07D498/04

    摘要： This invention relates to compounds represented by the general formula [I]   wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及由通式[I]表示的化合物，其中R表示叠氮基等，R 1和R 2相同或不同，表示氢原子等，R 3和R 4相同或不同，表示 氢原子等，X1表示氧原子等，X2表示氧原子等，Y表示氧原子等，Z表示缩合芳基等，或其药学上可接受的盐 ，其制备方法和糖尿病治疗剂，用于糖尿病慢性并发症的预防剂或抗肥胖药物，含有作为有效成分的化合物或其药学上可接受的盐。

    Isoindole derivatives
    9.
    发明授权
    Isoindole derivatives 失效
    异吲哚衍生物

    公开(公告)号：US06777410B2

    公开(公告)日：2004-08-17

    申请号：US10408220

    申请日：2003-04-08

    申请人： Toshio Nagase ,  Tomoharu Iino ,  Yoshiyuki Sato ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    发明人： Toshio Nagase ,  Tomoharu Iino ,  Yoshiyuki Sato ,  Teruyuki Nishimura ,  Jun-ichi Eiki

    IPC分类号： A61K31423

    CPC分类号： C07D498/04

    摘要： This invention relates to compounds represented by the general formula [I] wherein, R represents an azido group, etc., R1 and R2 are the same or different and represent hydrogen atoms, etc., R3 and R4 are the same or different and represent hydrogen atoms, etc., X1 represents an oxygen atom, etc., X2 represents an oxygen atom, etc., Y represents an oxygen atom, etc., and Z represents a condensed aryl group, etc., or a pharmaceutically acceptable salt thereof, preparation processes thereof, and an agent for treating diabetes, a prophylactic agent for chronic complications of diabetes or a drug against obesity, containing, as an effective ingredient, the compound or the pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及由通式[I]表示的化合物，其中R表示叠氮基等，R 1和R 2相同或不同，表示氢原子等，R 3， 和R 4相同或不同，表示氢原子等，X 1表示氧原子等，X 2表示氧原子等，Y表示氧原子等，Z表示缩合 芳基等，或其药学上可接受的盐，其制备方法和用于治疗糖尿病的药物，用于糖尿病慢性并发症的预防剂或抗肥胖药物，其含有作为有效成分的化合物或药学上可接受的盐 其可接受的盐。

    Novel aminobenzamide derivative
    10.
    发明申请
    Novel aminobenzamide derivative 失效
    新型氨基苯甲酰胺衍生物

    公开(公告)号：US20050282815A1

    公开(公告)日：2005-12-22

    申请号：US10952471

    申请日：2004-09-27

    申请人： Teruyuki Nishimura ,  Tomoharu Iino ,  Yasufumi Nagata ,  Jun-ichi Eiki

    发明人： Teruyuki Nishimura ,  Tomoharu Iino ,  Yasufumi Nagata ,  Jun-ichi Eiki

    IPC分类号： A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  A61P3/04 ,  A61P3/10 ,  A61P43/00 ,  C07D277/46 ,  C07D277/56 ,  C07D401/12 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04 ,  A61K31/497 ,  A61K31/501 ,  C07D413/02 ,  C07D417/02 ,  C07D43/02

    CPC分类号： C07D401/12 ,  A61K31/426 ,  A61K31/427 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/506 ,  C07D277/46 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D513/04

    摘要： This invention relates to a novel compound represented by the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is —S(O)p-A, —S—(O)q-B or —O-D, wherein p and q, which are the same or different, each represent an integer from 0 to 2, A is a straight chain C1-C10 alkyl group which may be substituted by R10, and B and D each independently represent R12 which may be substituted by R10; R2 is a hydrogen atom, a halogen atom, or a straight chain or branched C1-C6 alkyl group which may be substituted by R10; X1 and X2 each independently represent N or CH, but cannot both be N; the formula (II): shows a monocyclic or bicyclic heteroaryl group which has a nitrogen atom adjacent to the carbon atom bonded to the amide group, and the heteroaryl group may be substituted by R10; R10 is R11, or a hydrocarbon group which may be substituted by R11; R11 is, for example, a hydrogen atom or amino; and R12 is, for example, phenyl, thiazolyl, pyridyl or methylene dioxyphenyl. The compound according to this invention has a glucokinase activation effect, and for example, is useful in the treatment and prevention of diabetes mellitus, and in the prevention of its complications such as diabetic nephropathy, diabetic retinopathy, diabetic neuropathy and diabetic arteriosclerosis.

    摘要翻译： 本发明涉及由式（I）表示的新化合物或其药学上可接受的盐，其中R 1是-S（O）p A，-S-（O）qB或-OD 其中相同或不同的p和q各自表示0至2的整数，A是可以被R 10取代的直链C 1 -C 10烷基，B和 D各自独立地表示可被R 10取代的R 12， R 2是氢原子，卤素原子或可被R 10取代的直链或支链C 1 -C 6烷基; X 1和X 2各自独立地表示N或CH，但不能都是N; 式（II）表示具有与结合到酰胺基上的碳原子相邻的氮原子的单环或双环杂芳基，杂芳基可以被R 10取代; R 10是R 11，或可被R 11取代的烃基; R 11是例如氢原子或氨基; R 12是例如苯基，噻唑基，吡啶基或亚甲基二氧苯基。 根据本发明的化合物具有葡糖激酶活化作用，例如可用于治疗和预防糖尿病，并且可用于预防其并发症如糖尿病性肾病，糖尿病性视网膜病，糖尿病性神经病和糖尿病性动脉硬化。