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50 条记录 (耗时 0.039 秒)

    Benzofuran derivatives, their production and use
    22.
    发明授权
    Benzofuran derivatives, their production and use 失效
    苯并呋喃衍生物，其生产和使用

    公开(公告)号：US07456162B2

    公开(公告)日：2008-11-25

    申请号：US11081615

    申请日：2005-03-17

    申请人： Shigenori Ohkawa ,  Yasuyoshi Arikawa ,  Kouki Kato ,  Masahiro Okura ,  Masaki Setoh

    发明人： Shigenori Ohkawa ,  Yasuyoshi Arikawa ,  Kouki Kato ,  Masahiro Okura ,  Masaki Setoh

    IPC分类号： A61K31/33 ,  C07D405/00 ,  C07D411/00 ,  C07D209/00

    CPC分类号： C07D307/79 ,  C07D405/04 ,  C07D407/06 ,  C07D407/12 ,  C07D409/06

    摘要： Compounds represented by the formula: wherein R1 and R2 are hydrogen atom, a hydrocarbon group or a heterocyclic group, or R1 and R2 may form, together with the adjacent carbon atom, a 3- to 8-membered homocyclic or heterocyclic ring, W indicates a group represented by the formula: wherein R4 indicates (1) an aliphatic hydrocarbon group, which may be substituted with an aromatic group, or (2) an acyl group containing an aromatic group, R5 is hydrogen atom, a C1-6 alkyl, or an acyl group, R3 indicates a C6-14 aryl group, or salts thereof. The compounds have an excellent action to inhibit neurodegeneration as well as an excellent brain penetrability and are low in the toxicity, thereby being useful as drugs for nerve degenerative diseases.

    摘要翻译： 由下式表示的化合物：其中R 1和R 2是氢原子，烃基或杂环基，或R 1和R 2 可以与相邻的碳原子一起形成3-至8-元的杂环或杂环，W表示由下式表示的基团：其中R 4表示 （1）可以被芳族基团取代的脂族烃基，或（2）含有芳基的酰基，R 5是氢原子，C 1-6 烷基或酰基，R 3表示C 6-14芳基或其盐。 该化合物具有抑制神经变性以及优异的脑渗透性的优异作用，毒性低，因此可用作神经退行性疾病的药物。

    Benzo-fused 5-membered hetrocycle compounds, process for preparation of the same, and use thereof
    23.
    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。

    Tricyclic compounds, their production and use
    24.
    发明授权
    Tricyclic compounds, their production and use 有权
    三环化合物，其生产和使用

    公开(公告)号：US06218429B1

    公开(公告)日：2001-04-17

    申请号：US09309519

    申请日：1999-05-10

    申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    IPC分类号： A01N34308

    CPC分类号： C07D263/52 ,  C07D265/34 ,  C07D307/93 ,  C07D311/94 ,  C07D317/70 ,  C07D319/14 ,  C07D491/04 ,  Y10S514/923

    摘要： A compound of the formula: wherein R1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R2 is H or an optionally substituted hydrocarbon group; R3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR4, NR4, O or S in which R4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

    摘要翻译： 下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

    Tricyclic compounds, their production and use
    25.
    发明授权
    Tricyclic compounds, their production and use 失效
    三环化合物，其生产和使用

    公开(公告)号：US6034239A

    公开(公告)日：2000-03-07

    申请号：US812168

    申请日：1997-03-06

    申请人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    发明人： Shigenori Ohkawa ,  Osamu Uchikawa ,  Kohji Fukatsu ,  Masaomi Miyamoto

    IPC分类号： C07C233/00 ,  C07D307/92 ,  C07D413/00 ,  C07D493/00

    CPC分类号： C07D307/77 ,  C07D263/62 ,  C07D311/94 ,  C07D317/70 ,  C07D319/14 ,  C07D491/04

    摘要： A compound of the formula: ##STR1## wherein R.sup.1 is an optionally substituted hydrocarbon, amino or heterocyclic group; R.sup.2 is H or an optionally substituted hydrocarbon group; R.sup.3 is H or an optionally substituted hydrocarbon or heterocyclic group; X is CHR.sup.4, NR.sup.4, O or S in which R.sup.4 is H or an optionally substituted hydrocarbon group; Y is C, CH or N; ring A is optionally substituted 5- to 7-membered ring; ring B is an optionally substituted benzene ring; and m is 1 to 4, or a salt thereof, a process for producing it, an intermediate for the production and a pharmaceutical composition comprising it are provided.

    摘要翻译： 下式的化合物：其中R 1是任选取代的烃，氨基或杂环基; R2是H或任选取代的烃基; R3是H或任选取代的烃或杂环基; X是CHR 4，NR 4，O或S，其中R 4是H或任选取代的烃基; Y为C，CH或N; 环A为任选取代的5-至7-元环; 环B是任选取代的苯环; 和m为1至4，或其盐，其制备方法，制备中间体和包含其的药物组合物。

    Benzo-fused 5-membered heterocyclic compounds, their production and use
    28.
    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。

    Antidepressant
    30.
    发明申请
    Antidepressant 失效
    抗抑郁药

    公开(公告)号：US20060241168A1

    公开(公告)日：2006-10-26

    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R 1和R 2：H，烃基或杂环基或R 与相邻的碳原子一起形成环;和<！ - SIPO