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    Novel compounds having 4-pyridylalkylthio group as substituent
    1.
    发明申请
    Novel compounds having 4-pyridylalkylthio group as substituent 有权
    具有4-吡啶基烷硫基作为取代基的新型化合物

    公开(公告)号：US20060194836A1

    公开(公告)日：2006-08-31

    申请号：US10548283

    申请日：2004-03-05

    申请人： Takahiro Honda ,  Hisashi Tajima ,  Yoshimosa Sasabuchi ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto

    发明人： Takahiro Honda ,  Hisashi Tajima ,  Yoshimosa Sasabuchi ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto

    IPC分类号： A61K31/4709 ,  A61K31/444 ,  C07D401/14

    CPC分类号： C07D401/12 ,  C07D213/32 ,  C07D401/14

    摘要： A subject of the present invention is to provide a novel aromatic five- or six-memberd heterocyclic derivative having 4-pyridylalkylthio as a substituent or a salt thereof which is useful as a pharmaceutical. Compound represented by the following general formula [I] or salts thereof are useful as therapeutic agents for diseases in which angiogenesis or augmentation of vascular permeability is involved. In the formula, ring “A” is a benzene ring or an aromatic five- or six-memberd heterocycle which can be fused with a cycloalkane ring, “B” is alkylene, R1 and R2, the same or different, are H, OH, substituted or unsubstituted alkoxy and the like, X and Y, the same or different, are group(s) selected from H, halogen, OH, substituted or unsubstituted alkoxy and the like respectively, p is 0, 1 or 2, and q is 0 or 1.

    摘要翻译： 本发明的目的是提供一种新颖的具有4-吡啶基烷硫基作为取代基的五元或六元杂环衍生物或其盐，其可用作药物。 由以下通式[I]表示的化合物或其盐可用作涉及血管生成或增加血管通透性的疾病的治疗剂。 在该式中，环“A”是可以与环烷烃环稠合的苯环或芳族五元或六元杂环，“B”是亚烷基，R 1和R 2 相同或不同的是H，OH，取代或未取代的烷氧基等，X和Y相同或不同，为选自H，卤素，OH，取代或未取代的 烷氧基等，p为0,1或2，q为0或1。

    Cyclic compound having pyrimidinylalkylthio group
    2.
    发明授权
    Cyclic compound having pyrimidinylalkylthio group 有权
    具有嘧啶基烷硫基的环状化合物

    公开(公告)号：US08507485B2

    公开(公告)日：2013-08-13

    申请号：US12931072

    申请日：2011-01-24

    申请人： Hisashi Tajima ,  Takahiro Honda ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto

    发明人： Hisashi Tajima ,  Takahiro Honda ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto

    IPC分类号： A61K31/5377 ,  A61K31/506

    CPC分类号： C07D401/14 ,  C07D239/42 ,  C07D401/12 ,  C07D409/12

    摘要： A method of treating a disease associated with angiogenesis by administering a therapeutically effective amount of a compound represented by the formula (1) or a salt thereof wherein the ring X represents R1 and R2 independently represent a hydrogen atom, an alkyl, an aryl or an aromatic heterocyclic; R3 represents a hydrogen atom, a halogen atom, a hydroxy, an alkoxy, an aryloxy, an alkyl, an aryl, an amino, an alkylamino, a cycloalkylamino, an arylamino, an alkylcarbonylamino, an arylcarbonylamino, a mercapto, an alkylthio, an arylthio, an alkylsulfinyl or a nonaromatic heterocyclic; A1 represents a sulfur atom, a sulfinyl or a sulfonyl; and A2 represents an alkylene.

    摘要翻译： 通过施用治疗有效量的由式（1）表示的化合物或其盐来治疗与血管生成相关的疾病的方法，其中环X表示R 1和R 2独立地表示氢原子，烷基，芳基或 芳香杂环; R 3表示氢原子，卤素原子，羟基，烷氧基，芳氧基，烷基，芳基，氨基，烷基氨基，环烷基氨基，芳基氨基，烷基羰基氨基，芳基羰基氨基，巯基，烷硫基 芳硫基，烷基亚磺酰基或非芳族杂环; A1表示硫原子，亚磺酰基或磺酰基; A2表示亚烷基。

    Novel cyclic compound having 4-pyridylalkylthio group having substituted or unsubstituted amino group introduced therein
    4.
    发明申请
    Novel cyclic compound having 4-pyridylalkylthio group having substituted or unsubstituted amino group introduced therein 有权
    具有引入其中具有取代或未取代的氨基的4-吡啶基烷硫基的新型环状化合物

    公开(公告)号：US20070149574A1

    公开(公告)日：2007-06-28

    申请号：US10587410

    申请日：2005-02-17

    申请人： Takahiro Honda ,  Hisashi Tajima ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Takaaki Inaba ,  Yuriko Takeno

    发明人： Takahiro Honda ,  Hisashi Tajima ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Takaaki Inaba ,  Yuriko Takeno

    IPC分类号： A61K31/4439 ,  A61K31/44 ,  C07D403/02 ,  C07D213/72

    CPC分类号： C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14

    摘要： A novel cyclic compound having a 4-pyridylalkylthio group having an (un)substituted amino group introduced therein or a salt thereof. They are useful as a medicine. The cyclic compound is a compound represented by the following formula (1), which is useful for the treatment of diseases in which angiogenesis participates. In the following formula (1), ring A represents a benzene ring or a 5- or 6-membered aromatic heterocycle optionally fused with a cycloalkane ring; B represents alkylene; R1 and R2 each represents H, (substituted) aryl, (substituted) heterocyclic group, etc.; R3 and R4 each represents H, (substituted) alkyl, (substituted) cycloalkyl, -Z-R5, etc.; R5 represents (substituted) alkyl, (substituted) aryl, (substituted) heterocyclic group, etc.; X and Y each represents H, etc.; Z represents —CO—, —COO—, —CONR6—, —SO2—, etc.; R6 represents H, etc.; p is 0, 1, or 2; and q is 0 or 1.

    摘要翻译： 具有引入其中具有（未）取代的氨基的4-吡啶基烷硫基的新型环状化合物或其盐。 它们作为一种药物是有用的。 环状化合物是由下式（1）表示的化合物，其可用于治疗血管发生参与的疾病。 在下式（1）中，环A表示任选与环烷烃环稠合的苯环或5-或6-元芳族杂环; B表示亚烷基; R 1和R 2各自表示H，（取代的）芳基，（取代的）杂环基等; R 3和R 4各自表示H，（取代的）烷基，（取代的）环烷基，-Z-R 5等; R 5表示（取代的）烷基，（取代的）芳基，（取代的）杂环基等; X和Y各自表示H等; Z表示-CO-，-COO - ， - CONR 6 - ， - SO 2 - 等; R 6表示H等; p为0,1或2; q为0或1。

    Compounds having a 4-pyridylalkylthio group as a substituent
    5.
    发明授权
    Compounds having a 4-pyridylalkylthio group as a substituent 有权
    具有4-吡啶基烷硫基作为取代基的化合物

    公开(公告)号：US08207194B2

    公开(公告)日：2012-06-26

    申请号：US12381290

    申请日：2009-03-10

    申请人： Takahiro Honda ,  Hisashi Tajima ,  Yoshimasa Sasabuchi ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Masakazu Ban

    发明人： Takahiro Honda ,  Hisashi Tajima ,  Yoshimasa Sasabuchi ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Masakazu Ban

    IPC分类号： A61K31/47 ,  C07D401/02 ,  C07D213/02

    CPC分类号： C07D401/12 ,  C07D213/32 ,  C07D401/14

    摘要： A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is benzene or an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxy, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.

    摘要翻译： 具有下式[I]的化合物或其药学上可接受的盐：其中A是任选与环烷烃环稠合的苯或芳族五元杂环; B是亚烷基; R 1和R 2是氢，羟基，烷氧基，芳氧基，烷基，环烷基，芳基，杂环，氨基，烷基氨基，芳基氨基或酰基，或R 1和R 2连接在一起形成杂环; X和Y是氢，卤素，羟基，烷氧基，芳氧基，烷基，环烷基，芳基，巯基，烷硫基，芳硫基，羧基，羧基的酯，羧基的酰胺，氰基或硝基; p为0,1或2; q为0或1.该化合物可用于治疗涉及血管生成或增加血管通透性的疾病。

    Cyclic compound having 4-pyridylalkylthio group having substituted or unsubstituted amino group introduced therein
    8.
    发明授权
    Cyclic compound having 4-pyridylalkylthio group having substituted or unsubstituted amino group introduced therein 有权
    具有引入其中具有取代或未取代氨基的4-吡啶基烷硫基的环状化合物

    公开(公告)号：US07544703B2

    公开(公告)日：2009-06-09

    申请号：US10587410

    申请日：2005-02-17

    申请人： Takahiro Honda ,  Hisashi Tajima ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Takaaki Inaba ,  Yuriko Takeno

    发明人： Takahiro Honda ,  Hisashi Tajima ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Takaaki Inaba ,  Yuriko Takeno

    IPC分类号： A61K31/4436 ,  C07D213/89

    CPC分类号： C07D213/73 ,  C07D213/74 ,  C07D213/75 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/14

    摘要： A novel cyclic compound having a 4-pyridylalkylthio group having an (un)substituted amino group introduced therein or a salt thereof. They are useful as a medicine. The cyclic compound is a compound represented by the following formula (1), which is useful for the treatment of diseases in which angiogenesis participates. In the following formula (1), ring A represents a benzene ring or a 5- or 6-membered aromatic heterocycle optionally fused with a cycloalkane ring; B represents alkylene; R1 and R2 each represents H, (substituted) aryl, (substituted) heterocyclic group, etc.; R3 and R4 each represents H, (substituted) alkyl, (substituted) cycloalkyl, -Z-R5, etc.; R5 represents (substituted) alkyl, (substituted) aryl, (substituted) heterocyclic group, etc.; X and Y each represents H, etc.; Z represents —CO—, —COO—, —CONR6—, —SO2—, etc.; R6 represents H, etc.; p is 0, 1, or 2; and q is 0 or 1.

    摘要翻译： 具有引入其中具有（未）取代的氨基的4-吡啶基烷硫基的新型环状化合物或其盐。 它们作为一种药物是有用的。 环状化合物是由下式（1）表示的化合物，其可用于治疗血管发生参与的疾病。 在下式（1）中，环A表示任选与环烷烃环稠合的苯环或5-或6-元芳族杂环; B表示亚烷基; R1和R2各自表示H，（取代的）芳基，（取代的）杂环基等; R 3和R 4各自表示H，（取代的）烷基，（取代的）环烷基，-Z-R 5等; R5代表（取代）烷基，（取代）芳基，（取代）杂环基等; X和Y各自表示H等; Z表示-CO - ， - COO - ， - CONR 6 - ， - SO 2 - 等; R6表示H等; p为0,1或2; q为0或1。

    Compounds having 4-pyridylalkylthio group as a substituent
    9.
    发明授权
    Compounds having 4-pyridylalkylthio group as a substituent 有权
    具有4-吡啶基烷硫基作为取代基的化合物

    公开(公告)号：US08518973B2

    公开(公告)日：2013-08-27

    申请号：US13449921

    申请日：2012-04-18

    申请人： Takahiro Honda ,  Hisashi Tajima ,  Yoshimasa Sasabuchi ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Masakazu Ban

    发明人： Takahiro Honda ,  Hisashi Tajima ,  Yoshimasa Sasabuchi ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto ,  Masakazu Ban

    IPC分类号： C07D401/12 ,  A61K31/44

    CPC分类号： C07D401/12 ,  C07D213/32 ,  C07D401/14

    摘要： A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.

    摘要翻译： 具有下式[I]的化合物或其药学上可接受的盐：其中A是任选与环烷烃环稠合的芳族五元杂环; B是亚烷基; R 1和R 2是氢，羟基，烷氧基，芳氧基，烷基，环烷基，芳基，杂环，氨基，烷基氨基，芳基氨基或酰基，或R 1和R 2连接在一起形成杂环; X和Y是氢，卤素，羟基，烷氧基，芳氧基，烷基，环烷基，芳基，巯基，烷硫基，芳硫基，羧基，羧基的酯，羧基的酰胺，氰基或硝基; p为0,1或2; q为0或1.该化合物可用于治疗涉及血管生成或增加血管通透性的疾病。

    Cyclic compound having pyrimidinylalkylthio group
    10.
    发明授权
    Cyclic compound having pyrimidinylalkylthio group 有权
    具有嘧啶基烷硫基的环状化合物

    公开(公告)号：US07906511B2

    公开(公告)日：2011-03-15

    申请号：US11887308

    申请日：2006-03-31

    申请人： Hisashi Tajima ,  Takahiro Honda ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto

    发明人： Hisashi Tajima ,  Takahiro Honda ,  Kenji Kawashima ,  Kazuyoshi Okamoto ,  Minoru Yamamoto

    IPC分类号： C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  A61K31/506 ,  A61K31/5377

    CPC分类号： C07D401/14 ,  C07D239/42 ,  C07D401/12 ,  C07D409/12

    摘要： The present invention has its object to study synthesis of novel cyclic compounds having a pyrimidinylalkylthio group and to find pharmacological actions of the compounds. According to the present invention, a compound represented by the formula (1) or a salt thereof is provided. In the formula, the ring X represents: R1 and R2 independently represent a hydrogen atom, an alkyl group, an aryl group, an aromatic heterocyclic group or the like; R3 represents a hydrogen atom, a halogen atom, a hydroxy group, an alkoxy group, an aryloxy group, an alkyl group, an aryl group, an amino group, an alkylamino group or the like; A1 represents a sulfur atom or the like; and A2 represents an alkylene group.

    摘要翻译： 本发明的目的是研究具有嘧啶基烷硫基的新型环状化合物的合成，并找到化合物的药理作用。 根据本发明，提供由式（1）表示的化合物或其盐。 在该式中，环X表示：R 1和R 2分别表示氢原子，烷基，芳基，芳香族杂环基等， R 3表示氢原子，卤素原子，羟基，烷氧基，芳氧基，烷基，芳基，氨基，烷基氨基等; A1表示硫原子等; A2表示亚烷基。