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    Substituted 1,3-thiazole compounds, their production and use
    2.
    发明授权
    Substituted 1,3-thiazole compounds, their production and use 失效
    取代的1,3-噻唑化合物，其生产和使用

    公开(公告)号：US07495018B2

    公开(公告)日：2009-02-24

    申请号：US10239692

    申请日：2001-03-29

    申请人： Shigenori Ohkawa ,  Ken-ichi Naruo ,  Seiji Miwatashi ,  Hiroyuki Kimura

    发明人： Shigenori Ohkawa ,  Ken-ichi Naruo ,  Seiji Miwatashi ,  Hiroyuki Kimura

    IPC分类号： A61K31/4436 ,  C07D417/04

    CPC分类号： C07D417/04

    摘要： (1) A 1,3-thiazole compound of which the 5-position is substituted with a 4-pyridyl group having a substituent including no aromatic group or (2) a 1,3-thiazole compound of which the 5-position is substituted with a pyridyl group having at the position adjacent to a nitrogen atom of the pyridyl group a substituent including no aromatic group has an excellent p38 MAP kinase inhibitory activity.

    摘要翻译： （1）5-取代的不具有芳香族基团的取代基的4-吡啶基的1,3-噻唑化合物或（2）取代有5位的1,3-噻唑化合物 在与吡啶基的氮原子相邻的位置具有吡啶基的情况下，不含芳香族基团的取代基具有优异的p38MAP激酶抑制活性。

    5-pyridyl-1, 3-azole compounds, process for producing the same and use there of
    3.
    发明申请
    5-pyridyl-1, 3-azole compounds, process for producing the same and use there of 审中-公开
    5-吡啶基-1,3-唑化合物，其制备方法和用途

    公开(公告)号：US20090048307A1

    公开(公告)日：2009-02-19

    申请号：US11896072

    申请日：2007-08-29

    申请人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    发明人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    IPC分类号： A61K31/4439 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D417/14 ,  C07D417/04

    摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

    摘要翻译： 由下式表示的任选的N-氧化化合物：其中R1表示氢，烃，杂环，氨基，酰基，R2表示芳族基团，R3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示 键，氧，任选氧化的硫，由式NR4表示的基团（R4表示氢，烃或酰基），Z表示键或二价无环烃或其盐具有优异的腺苷A3受体拮抗活性，并且为 用作预防或治疗与腺苷A3受体有关的疾病的药剂。 此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof
    5.
    发明授权
    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效
    5-吡啶基-1,3-唑化合物，其制备方法及其用途

    公开(公告)号：US07276527B2

    公开(公告)日：2007-10-02

    申请号：US11354897

    申请日：2006-02-16

    申请人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    发明人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    IPC分类号： A61K31/4436 ,  C07D417/04

    CPC分类号： C07D417/14 ,  C07D417/04

    摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

    摘要翻译： 由下式表示的任选的N-氧化化合物：其中R 1表示氢，烃，杂环，氨基，酰基，R 2表示芳族基团， 3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR 4表示的基团（R 4代表氢，烃或酰基），Z表示键或二价无环烃，或其盐具有优异的腺苷A 3受体拮抗活性，并用作 用于预防或治疗与腺苷A 3受体相关的疾病的药剂。 此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof
    6.
    发明申请
    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效
    5-吡啶基-1,3-唑化合物，其制备方法及其用途

    公开(公告)号：US20060135566A1

    公开(公告)日：2006-06-22

    申请号：US11354897

    申请日：2006-02-16

    申请人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    发明人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    IPC分类号： A61K31/4439 ,  C07D417/04 ,  C07D413/04

    CPC分类号： C07D417/14 ,  C07D417/04

    摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

    摘要翻译： 由下式表示的任选的N-氧化化合物：其中R 1表示氢，烃，杂环，氨基，酰基，R 2表示芳族基团， 3表示氢，吡啶基，芳香烃，X表示氧，任选氧化的硫，Y表示键，氧，任选氧化的硫，由式NR 4表示的基团（R 4代表氢，烃或酰基），Z表示键或二价无环烃，或其盐具有优异的腺苷A 3受体拮抗活性，并用作 用于预防或治疗与腺苷A 3受体相关的疾病的药剂。 此外，化合物（I）或其盐具有p38 MAP激酶抑制活性和TNF-α抑制活性，并且用作预防或治疗与p38 MAP激酶相关的疾病和与TNF-α相关的疾病的药剂。

    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof
    8.
    发明授权
    5-pyridyl-1,3-azole compounds, process for producing the same and use thereof 失效

    公开(公告)号：US07101899B1

    公开(公告)日：2006-09-05

    申请号：US09959356

    申请日：2000-04-20

    申请人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    发明人： Shigenori Ohkawa ,  Naoyuki Kanzaki ,  Seiji Miwatashi

    IPC分类号： A61K31/445 ,  C07D417/04

    CPC分类号： C07D417/14 ,  C07D417/04

    摘要： An optionally N-oxidized compound represented by the formula: wherein R1 represents hydrogen, hydrocarbon, heterocycle, amino, acyl, R2 represents an aromatic group, R3 represents hydrogen, pyridyl, aromatic hydrocarbon, X represents oxygen, optionally oxidized sulfur, Y represents a bond, an oxygen, optionally oxidized sulfur, a group represented by the formula NR4 (R4 represents hydrogen, hydrocarbon or acyl) and Z represents a bond or a divalent acyclic hydrocarbon, or a salt thereof has an excellent adenosine A3 receptor antagonistic activity and is used as an agent for preventing or treating diseases related to an adenosine A3 receptor. Furthermore, the compound (I) or a salt thereof has p38 MAP kinase inhibitory activity and TNF-α inhibitory activity and is used as an agent for preventing or treating diseases related to p38 MAP kinase and diseases related to TNF-α.

    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。