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    Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof
    7.
    发明授权
    Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof 失效
    苯并稠合的5元杂环化合物，其制备方法及其用途

    公开(公告)号：US07208495B2

    公开(公告)日：2007-04-24

    申请号：US10481367

    申请日：2002-07-04

    申请人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

    发明人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

    IPC分类号： A61K31/497 ,  A61K31/445 ,  C07D405/00 ,  C07D401/00

    CPC分类号： A61K31/4525 ,  A61K31/496 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D307/82 ,  C07D307/83 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/14

    摘要： A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3–8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5–8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and— represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.

    摘要翻译： 由下式表示的化合物（其中，R 1和R 2相同或不同，各自表示氢原子，烃基或杂环基， 可以与相邻的碳原子一起形成3-8元的异或杂环基，R 3表示环状 基团，羟基，可具有氧代基的巯基或氨基，R 4表示氢原子，烃基，羟基，可具有氧代基的巯基，或 氨基或R 2和R 4可以连接在一起形成双键，X表示键或直链烃基，W表示氧原子或 硫原子，环B表示5-8元含氮杂环基，环C表示苯环，代表单键或双键）或其盐或前药具有优异的神经变性抑制活性， 脑穿透性 并且可用作预防/治疗神经变性疾病的药剂。

    Benzo-fused 5-membered heterocyclic compounds, their production and use
    8.
    发明申请
    Benzo-fused 5-membered heterocyclic compounds, their production and use 审中-公开
    苯并稠合的5元杂环化合物，其生产和使用

    公开(公告)号：US20070149558A1

    公开(公告)日：2007-06-28

    申请号：US11679257

    申请日：2007-02-27

    申请人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

    发明人： Shigenori Ohkawa ,  Masaomi Miyamoto ,  Masahiro Okura ,  Tetsuya Tsukamoto

    IPC分类号： A61K31/4747 ,  A61K31/407

    CPC分类号： A61K31/4525 ,  A61K31/496 ,  C07D307/79 ,  C07D307/80 ,  C07D307/81 ,  C07D307/82 ,  C07D307/83 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D407/04 ,  C07D409/04 ,  C07D409/14

    摘要： A compound represented by the formula: (wherein, R1 and R2 are the same or different and each represents a hydrogen atom, hydrocarbon group or heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3-8 membered iso- or heterocyclic group, R3 represents a cyclic group, a hydroxy group, a mercapto group that may have oxo, or an amino group, R4 represents a hydrogen atom, a hydrocarbon group, a hydroxy group, a mercapto group which may have oxo, or an amino group, or R2 and R4 may link together to form a double bond, X represents a bond or a linear hydrocarbon group, W represents an oxygen atom or a sulfur atom, ring B represents a 5-8 membered nitrogen-containing heterocyclic group, ring C represents a benzene ring, and represents a single bond or a double bond), or a salt or a prodrug thereof that has excellent neurodegenerative inhibitory activity and brain penetrability, and is useful as an agent for preventing/treating neurodegenerative diseases.

    摘要翻译： 由下式表示的化合物（其中，R 1和R 2相同或不同，各自表示氢原子，烃基或杂环基， 可以与相邻的碳原子一起形成3-8元的异或杂环基，R 3表示环状 基团，羟基，可具有氧代基的巯基或氨基，R 4表示氢原子，烃基，羟基，可具有氧代基的巯基，或 氨基或R 2和R 4可以连接在一起形成双键，X表示键或直链烃基，W表示氧原子或 硫原子，环B表示5-8元含氮杂环基，环C表示苯环，并且表示单键或双键）或其具有优异的神经变性抑制活性和脑渗透性的盐或其前药，并且可用作预防/治疗神经变性疾病的药剂。

    Dihydrobenzofuran derivatives, process for the preparing thereof and agents
    9.
    发明授权
    Dihydrobenzofuran derivatives, process for the preparing thereof and agents 失效
    二氢苯并呋喃衍生物，其制备方法和试剂

    公开(公告)号：US07008940B1

    公开(公告)日：2006-03-07

    申请号：US10069314

    申请日：2000-08-18

    申请人： Shigenori Ohkawa ,  Tadatoshi Hashimoto ,  Tetsuya Tsukamoto

    发明人： Shigenori Ohkawa ,  Tadatoshi Hashimoto ,  Tetsuya Tsukamoto

    IPC分类号： A61P9/00 ,  A61P25/00 ,  A61K31/407 ,  A61K31/55 ,  C07D491/48

    CPC分类号： C07D491/04

    摘要： A compound represented by the formula (I): or a salt thereof exhibits excellent inhibitory activity of lipid peroxidation and is useful as an agent for inhibiting lipoperoxide production, wherein ring A denotes a non-aromatic 5- to 7-membered nitrogen-containing heterocyclic ring which may be further substituted, B ring denotes a benzene ring which may be further substituted, C ring denotes a dihydrofuran ring which may be further substituted, and R denotes hydrogen atom or an acyl group.

    摘要翻译： 由式（I）表示的化合物或其盐表现出优异的脂质过氧化抑制活性，可用作抑制脂肪过氧化物产生的试剂，其中环A表示非芳香族5至7元含氮杂环 环可以进一步被取代，B环表示可以被进一步取代的苯环，C环表示可以被进一步取代的二氢呋喃环，R表示氢原子或酰基。

    Antidepressant
    10.
    发明授权
    Antidepressant 失效
    抗抑郁药

    公开(公告)号：US07750037B2

    公开(公告)日：2010-07-06

    申请号：US11475539

    申请日：2006-06-27

    申请人： Shigenori Ohkawa ,  Masaomi Miyamoto

    发明人： Shigenori Ohkawa ,  Masaomi Miyamoto

    IPC分类号： A61K31/4035 ,  C07D405/02

    CPC分类号： C07D405/04 ,  C07D307/79 ,  C07D405/12 ,  C07D409/12 ,  C07D491/04 ,  C07D491/10

    摘要： A PKB (Akt) activating agent comprising a compound represented by the formula (I): wherein R1 and R2: H, a hydrocarbon group or a heterocyclic group or R1 and R2 form a ring in cooperation with the adjacent carbon atom; R3: H, a hydrocarbon group or a heterocyclic group; W: represents a group represented by the formulas: wherein ring A: an optionally substituted benzene ring; ring B: an optionally substituted 5- to 7-membered nitrogen-containing heterocycle; R4: an aliphatic hydrocarbon group substituted with an aromatic group and further optionally substituted, or an acyl group containing an aromatic group; R5: H, C1-6 alkyl or acyl; R4c: an aromatic group, an aliphatic hydrocarbon group or acyl; and X: O or S; Y: O, S or NH; and ring C: an optionally substituted benzene ring, or a salt or a prodrug thereof, and use of the activating agent in prevention or treatment of depression, anxiety, manic-depressive psychosis or PTSD are provided.

    摘要翻译： 一种PKB（Akt）活化剂，其包含由式（I）表示的化合物：其中R1和R2：H，烃基或杂环基或R1和R2与相邻碳原子一起形成环; R3：H，烃基或杂环基; W：表示由下式表示的基团：其中环A：任选取代的苯环; 环B：任选取代的5-至7-元含氮杂环; R4：被芳基取代并进一步任选取代的脂族烃基或含芳基的酰基; R5：H，C1-6烷基或酰基; R4c：芳基，脂族烃基或酰基; 和X：O或S; Y：O，S或NH; 和环C：任选取代的苯环，或其盐或前药，并且提供了用于预防或治疗抑郁，焦虑，躁狂抑郁性精神病或PTSD的活化剂。