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    Remedy for eye diseases accompanied by optic nerve injuries
    1.
    发明申请
    Remedy for eye diseases accompanied by optic nerve injuries 审中-公开
    补救眼病伴伴视神经损伤

    公开(公告)号：US20060287246A1

    公开(公告)日：2006-12-21

    申请号：US10572075

    申请日：2004-09-24

    申请人： Shinji Yoneda ,  Rie Yamamoto ,  Hideaki Hara

    发明人： Shinji Yoneda ,  Rie Yamamoto ,  Hideaki Hara

    IPC分类号： A61K38/08 ,  A61K38/06

    CPC分类号： A61K38/55 ,  A61K38/06 ,  A61K38/07

    摘要： An object of the present invention is to search for a novel medicinal use of a compound having a secretase inhibitory activity. Because the compound having a secretase inhibitory activity has a remarkable inhibitory effect on retinal neuronal cell death, it is useful as a therapeutic agent for a retinal disease typified by retinal vessel occlusion, diabetic retinopathy, ischemic optic neuropathy, macular degeneration, retinitis pigmentosa and Leber's disease or an eye disease accompanied by an optic neuropathy such as glaucoma.

    摘要翻译： 本发明的目的是寻找具有分泌酶抑制活性的化合物的新型药物用途。 由于具有分泌酶抑制活性的化合物对视网膜神经元细胞死亡具有显着的抑制作用，因此可用作视网膜病变治疗剂，以视网膜血管闭塞，糖尿病性视网膜病变，缺血性视神经病变，黄斑变性，色素性视网膜炎和Leber's 伴有视神经病如青光眼的疾病或眼病。

    NOVEL THIOPHENEDIAMINE DERIVATIVE HAVING UREA STRUCTURE
    4.
    发明申请
    NOVEL THIOPHENEDIAMINE DERIVATIVE HAVING UREA STRUCTURE 有权
    具有尿素结构的新型噻吩二胺衍生物

    公开(公告)号：US20120202808A1

    公开(公告)日：2012-08-09

    申请号：US13448674

    申请日：2012-04-17

    申请人： Hiroyuki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe ,  Junko Fujikawa ,  Minoru Yamamoto

    发明人： Hiroyuki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe ,  Junko Fujikawa ,  Minoru Yamamoto

    IPC分类号： A61K31/4436 ,  A61P27/06 ,  A61K31/5377 ,  A61P27/02 ,  C07D409/14 ,  C07D413/14

    CPC分类号： C07D333/36 ,  C07D409/12

    摘要： A compound of formula (1): wherein R1 and R2 represent hydrogen, lower alkyl, lower alkenyl, lower alkynyl or R3 represents hydroxyl, lower alkoxy, lower cycloalkyloxy, aryloxy, carboxy, lower alkoxycarbonyl, or NRaRb of the formula R4 and R5 represent halogen, lower alkyl, hydroxyl, or lower alkoxy; R6 represents halogen, lower alkyl, aryl, heterocyclic, hydroxy, lower alkoxy, mercapto, lower alkylthio, lower alkylcarbonyl, amino, nitro or cyano; R7 represents lower alkyl, hydroxyl or lower alkoxy; Ra and Rb represent hydrogen or lower alkyl; ring A represents a cyclic hydrocarbon or a heterocyclic ring; ring B represents a heterocyclic ring; X represents lower alkylene; Z represents a single bond or lower alkylene; Y represents lower alkylene and W1-W2 represents CH—CH, or represents a single bond and W1-W2 represents N—CH, CH—N or CH—CH; and 1, m, n and o represent 0, 1, 2, or 3.

    摘要翻译： 式（1）的化合物：其中R 1和R 2表示氢，低级烷基，低级烯基，低级炔基或R 3表示羟基，低级烷氧基，低级环烷氧基，芳氧基，羧基，低级烷氧基羰基或NR 4 R b R 5表示 卤素，低级烷基，羟基或低级烷氧基; R6表示卤素，低级烷基，芳基，杂环，羟基，低级烷氧基，巯基，低级烷硫基，低级烷基羰基，氨基，硝基或氰基; R7表示低级烷基，羟基或低级烷氧基; Ra和Rb代表氢或低级烷基; 环A表示环状烃或杂环; 环B表示杂环; X表示低级亚烷基; Z表示单键或低级亚烷基; Y表示低级亚烷基，W1-W2表示CH-CH，或表示单键，W1-W2表示N-CH，CH-N或CH-CH; 和1，m，n和o表示0,1,2或3。

    NOVEL THIOPHENEDIAMINE DERIVATIVE HAVING UREA STRUCTURE
    5.
    发明申请
    NOVEL THIOPHENEDIAMINE DERIVATIVE HAVING UREA STRUCTURE 有权
    具有尿素结构的新型噻吩二胺衍生物

    公开(公告)号：US20110077244A1

    公开(公告)日：2011-03-31

    申请号：US12993452

    申请日：2009-05-25

    申请人： Hiroyaki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe

    发明人： Hiroyaki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe

    IPC分类号： A61K31/5377 ,  C07D409/14 ,  A61K31/4436 ,  C07D409/12 ,  A61K31/381 ,  C07D413/12 ,  A61K31/496 ,  A61K31/4439 ,  A61K31/444 ,  C07D333/36 ,  C07D417/14 ,  A61P27/02 ,  A61P27/06

    CPC分类号： C07D333/36 ,  C07D409/12

    摘要： The present invention relates to synthetic studies of a novel thiophenediamine derivative having a urea structure and to finding pharmaceutical actions thereof. The present invention provides a compound represented by the following general formula (1) or a salt thereof. In the formula (1), R1 and R2 are the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, etc. R3 represents a hydroxy group, a lower alkoxy group which may have a substituent, a lower cycloalkyloxy group which may have a substituent, etc. R4 and R5 are the same or different and represent a halogen atom, a lower alkyl group, a hydroxy group, etc. X represents a lower alkylene group which may have a substituent, etc. Y represents a single bond or a lower alkylene group which may have a substituent, etc. W1-W2 represents N—CH, CH—N, etc. and l and m are the same or different and represent 0, 1, etc.

    摘要翻译： 本发明涉及具有尿素结构的新型噻吩并二胺衍生物的合成研究以及其药物作用。 本发明提供由下述通式（1）表示的化合物或其盐。 式（1）中，R 1和R 2相同或不同，表示氢原子，可以具有取代基的低级烷基等。R3表示羟基，可以具有取代基的低级烷氧基，可以具有取代基的低级烷氧基 可以具有取代基的低级环烷氧基等。R4和R5相同或不同，表示卤素原子，低级烷基，羟基等.X表示可以具有取代基的低级亚烷基等。 Y表示可以具有取代基的单键或低级亚烷基等。W1-W2表示N-CH，CH-N等，l和m相同或不同，表示0,1等。

    Thiophenediamine derivative having urea structure
    6.
    发明授权
    Thiophenediamine derivative having urea structure 有权
    具有尿素结构的噻吩并二胺衍生物

    公开(公告)号：US08198271B2

    公开(公告)日：2012-06-12

    申请号：US12993452

    申请日：2009-05-25

    申请人： Hiroyuki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe ,  Junko Fujikawa ,  Minoru Yamamoto

    发明人： Hiroyuki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe ,  Junko Fujikawa ,  Minoru Yamamoto

    IPC分类号： A61K31/444 ,  A61K31/5377 ,  A61K31/4436 ,  A61K31/381 ,  A61K31/496 ,  A61K31/4439 ,  C07D409/14 ,  C07D409/12 ,  C07D413/12 ,  C07D333/36 ,  C07D417/14

    CPC分类号： C07D333/36 ,  C07D409/12

    摘要： A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—  (2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—  (3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkylene; Z represents a single bond or a lower alkylene; W1-W2 represents N—CH or C—N and l, m, n and o represent 0, 1, 2, or 3.

    摘要翻译： 具有下式（1）的化合物或其盐：其中R1和R2表示氢，低级烷基，低级烯基，低级炔基或具有下式（2）的基团：（R6）n- {圆 （A）} - Z-（2），R3表示羟基，低级烷氧基，低级环烷氧基，芳氧基，羧基，低级烷氧基羰基或具有下式（3）的-NR aRb：（R 7） （B）} - （3），R4和R5代表卤素，低级烷基，羟基或低级烷氧基; R6表示卤素，低级烷基，芳基，杂环，羟基，低级烷氧基，巯基，低级烷硫基，低级烷基羰基，氨基，硝基或氰基; R7表示低级烷基，羟基或低级烷氧基; Ra和Rb代表氢或低级烷基; 环A表示环状烃或杂环; 环B表示具有一个或多个选自氮和氧的杂原子的杂环; X表示低级亚烷基; Y表示低级亚烷基; Z表示单键或低级亚烷基; W1-W2表示N-CH或C-N，且l，m，n和o表示0,1,2或3。

    Pyridinecarboxylic acid (2-aminophenyl) amide derivative having urea structure
    9.
    发明授权
    Pyridinecarboxylic acid (2-aminophenyl) amide derivative having urea structure 有权
    具有尿素结构的吡啶羧酸（2-氨基苯基）酰胺衍生物

    公开(公告)号：US08012972B2

    公开(公告)日：2011-09-06

    申请号：US12450387

    申请日：2008-03-28

    申请人： Hiroyuki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe ,  Junko Fujikawa ,  Minoru Yamamoto

    发明人： Hiroyuki Mogi ,  Hisashi Tajima ,  Noriko Mishina ,  Yusuke Yamazaki ,  Shinji Yoneda ,  Katsuhiko Watanabe ,  Junko Fujikawa ,  Minoru Yamamoto

    IPC分类号： A61K31/5377 ,  A61K31/44 ,  C07D413/12 ,  C07D213/81

    CPC分类号： C07D213/81 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12

    摘要： Objects of the present invention are to study the synthesis of a novel pyridinecarboxylic acid (2-aminophenyl)amide derivative having a novel urea structure and to find a pharmacological effect of the derivative. The invention provides a compound represented by the formula (1) or a salt thereof. In the formula, R1 and R2 represent a hydrogen atom, a lower alkyl group or the like; R3 represents a hydroxy group, a lower alkoxy group, a lower cycloalkyloxy group, an aryloxy group, a carboxy group, a lower alkoxycarbonyl group, —OCONRaRb, —NRcRd or the like; R4 and R5 represent a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or the like; Ra and Rb represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group, a heterocyclic group or the like; Rc and Rd represent a hydrogen atom, a lower alkyl group, a lower cycloalkyl group, an aryl group or the like; X represents a lower alkylene group; Y represents a single bond, a lower alkylene group; W1-W2 represents N—C or C—N; and l and m represent 0, 1, 2 or 3.

    摘要翻译： 本发明的目的是研究具有新型尿素结构的新型吡啶羧酸（2-氨基苯基）酰胺衍生物的合成，并找到该衍生物的药理作用。 本发明提供由式（1）表示的化合物或其盐。 在该式中，R 1和R 2表示氢原子，低级烷基等; R3表示羟基，低级烷氧基，低级环烷氧基，芳氧基，羧基，低级烷氧基羰基，-OCONRaRb，-NRcRd等; R4和R5代表卤原子，低级烷基，羟基，低级烷氧基等; Ra和Rb表示氢原子，低级烷基，低级环烷基，芳基，杂环基等; Rc和R d表示氢原子，低级烷基，低级环烷基，芳基等; X表示低级亚烷基; Y表示单键，低级亚烷基; W1-W2表示N-C或C-N; l和m表示0,1,2或3。