利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

6 条记录 (耗时 0.035 秒)

    Tracheal smooth muscle relaxant
    1.
    发明授权
    Tracheal smooth muscle relaxant 失效
    气管平滑肌松弛剂

    公开(公告)号：US06180659B2

    公开(公告)日：2001-01-30

    申请号：US09101842

    申请日：1998-08-31

    申请人： Shinya Yamashita ,  Jiro Takeo ,  Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita ,  Junichiro Hata ,  Yasuhiro Fukuda ,  Naomi Ohtsuka

    发明人： Shinya Yamashita ,  Jiro Takeo ,  Shuji Jinno ,  Yasuyo Kogure ,  Hiroyuki Onuki ,  Takaaki Okita ,  Junichiro Hata ,  Yasuhiro Fukuda ,  Naomi Ohtsuka

    IPC分类号： A61K3138

    CPC分类号： C07D337/14 ,  A61K31/352 ,  A61K31/382 ,  C07D313/14 ,  Y10S514/826

    摘要： The present invention offers a tracheal smooth muscle relaxant containing the compound represented by the following formula (1) or pharmacologically acceptable salt thereof as an effective ingredient. [In the formula, X and Y each is any group selected from a group consisting of CH2, CHW1 (where W1 is halogen atom, hydroxyl group or lower alkoxy group) and C═O when the bond of X and Y is a single bond while, when it is a double bond, X and Y each is any group selected from a group consisting of CH and COW2 (where W2 is lower alkyl group or lower alkylcarbonyl group); Z is O, S, S═O or SO2; and R1˜R8 each is selected from a group consisting of hydrogen atom, VR9 (where V is O, S, S═O or SO2; and R9 is hydrogen atom, lower alkyl group, hydroxy lower alkyl group, lower acyl group, trihalomethyl group or carboxyl lower alkyl group), carboxyl lower alkyl group, hydroxy lower alkyl group, hydroxy lower alkenyl group, hydroxy lower alkynyl group, halogen atom, lower alkyl group, lower alkyl ketone, trihalomethyl group, trimethylsilylethynyl, nitro group, amino group, N-carbonyl lower alkyl group, lower alkylphenyl group and phenyl group].

    摘要翻译： 本发明提供含有下述式（1）表示的化合物或其药理学上可接受的盐作为有效成分的气管平滑肌松弛剂。[式中，X和Y各自为选自CH 2， CHW1（其中W1为卤原子，羟基或低级烷氧基），当X和Y的键为单键时为C = O，而当为双键时，X和Y各自为选自 由CH和COW 2组成（其中W2是低级烷基或低级烷基羰基）; Z是O，S，S = O或SO 2; R1〜R8各自选自氢原子，VR9（其中V为O，S，S = O或SO2; R9为氢原子，低级烷基，羟基低级烷基，低级酰基，三卤甲基 羧基低级烷基，羟基低级烷基，羟基低级烯基，羟基低级炔基，卤素原子，低级烷基，低级烷基酮，三卤代甲基，三甲基甲硅烷基乙炔基，硝基，氨基， N-羰基低级烷基，低级烷基苯基和苯基]。

    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    2.
    发明授权
    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
    三环稠合杂环化合物，其制备方法及其应用

    公开(公告)号：US06700013B2

    公开(公告)日：2004-03-02

    申请号：US10291429

    申请日：2002-11-12

    申请人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    IPC分类号： C07C53134

    CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

    摘要： Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S═O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

    摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述定义相同 Y）为例如CH，CH 2或C = O; Z为例如O，S，S = O或SO 2; U为C或N; R 1至R 4各自独立地为例如 氢原子，OR，SR（其中R与上述定义相同）或芳环，取代的芳环或杂环; R 5和R 8中的至少一个是例如OH，剩余的R 5和R 8 各自独立地，例如，氢原子或OH，其旋光异构体，其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    3.
    发明授权
    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
    三环稠合杂环化合物，其制备方法及其应用

    公开(公告)号：US06602898B1

    公开(公告)日：2003-08-05

    申请号：US09980581

    申请日：2002-02-26

    申请人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    IPC分类号： A61K3138

    CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

    摘要： Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S=O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

    摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2，CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和R'与上述定义相同 Y）为例如CH，CH 2或C = O; Z为例如O，S，S = O或SO 2; U为C或N; R 1至R 4各自独立地为例如 氢原子，OR，SR（其中R与上述定义相同）或芳环，取代的芳环或杂环; R 5和R 8中的至少一个是例如OH，剩余的R 5和R 8 各自独立地，例如，氢原子或OH，其旋光异构体，其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    5.
    发明授权
    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof 失效
    三环稠合杂环化合物，其制备方法及其应用

    公开(公告)号：US07410997B2

    公开(公告)日：2008-08-12

    申请号：US10727644

    申请日：2003-12-05

    申请人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    发明人： Shuji Jinno ,  Takaaki Okita ,  Naomi Ohtsuka ,  Shinya Yamashita ,  Junichiro Hata ,  Jiro Takeo

    IPC分类号： A61K31/335 ,  C07D313/08

    CPC分类号： C07D405/04 ,  A61K31/31 ,  A61K31/335 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61K31/4353 ,  A61K31/4427 ,  C07D313/14 ,  C07D337/14 ,  C07D407/04 ,  C07D409/04 ,  C07D491/04

    摘要： Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S═O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.

    摘要翻译： 由式（1）表示的化合物，其中X为例如CH，CH 2 CHR（其中R为低级烷基或取代的低级烷基）或CRR'（其中R和 R'与上述定义的R相同）; Y是例如CH，CH 2或C-O; Z是例如O，S，S-O或SO 2; U是C或N; R 1至R 4各自独立地为例如氢原子，OR，SR（其中R与上述定义相同），或芳环， 取代的芳环或杂环; R 5和R 8中的至少一个是例如OH，R 5和R 8的剩余部分， SUB>各自独立地为例如氢原子或OH，其光学异构体，其结合物或其药学上可接受的盐。 这些化合物的特征在于具有广泛的药理作用，例如气管平滑肌的优异的缓解作用，气道超敏反应的抑制和抑制炎症细胞浸润到气道中，另外还具有高安全性。

    Process for producing dibenzo[b,f]thiepine derivatives
    6.
    发明授权
    Process for producing dibenzo[b,f]thiepine derivatives 失效
    二苯并[b，f]硫杂衍生物的制备方法

    公开(公告)号：US06207837B1

    公开(公告)日：2001-03-27

    申请号：US09462903

    申请日：2000-01-18

    申请人： Naomi Ohtsuka ,  Shuji Jinno ,  Takaaki Okita

    发明人： Naomi Ohtsuka ,  Shuji Jinno ,  Takaaki Okita

    IPC分类号： C07D33712

    CPC分类号： C07D337/14 ,  C07C319/14 ,  C07C323/62

    摘要： Efficient synthesis of diaryl sulfide derivatives useful as intermediates for pharmaceutical compounds. Provision of a convenient process for producing large quantities of dibenzo[b,f]thiepine derivatives using such intermediates. Halogen-substituted phenyl derivatives of the general formula (1): (where X is a halogen atom and R1-R5 is any substituent selected from among hydrogen, a lower alkyl group, a lower cycloalkyl group, an aryl group, a halogen atom, a lower alkoxyl group, an amino group, an N-lower acylamino group, a nitro group, a lower alkylthio group and a carboxyl group) are reacted with disulfide derivatives of the general formula (2): (where R6-R10 is any substituent selected from among hydrogen, a lower alkyl group, a lower cycloalkyl group, an aryl group, a halogen atom, a lower alkoxyl group, an amino group, an N-lower acylamino group, a nitro group, a lower alkylthio group and a carboxyl group) in the presence of metal catalysts to form a sulfide bond, thereby producing diaryl sulfide derivatives of the general formula (3): (where R1-R10 are the same as defined above) or salts thereof. Pharmaceutical compounds such as dibenzo[b,f]thiepine derivatives are produced from the diaryl sulfide derivatives or salts thereof by known techniques.

    摘要翻译： 用作药物化合物中间体的二芳基硫醚衍生物的高效合成。 提供使用这种中间体生产大量二苯并[b，f]硫杂衍生物的方便方法。通式（1）的原位取代的苯基衍生物:(其中X是卤素原子，R 1 -R 5是任选的取代基 从氢，低级烷基，低级环烷基，芳基，卤原子，低级烷氧基，氨基，N-低级酰氨基，硝基，低级烷硫基和羧基 ）与通式（2）的二硫化物衍生物反应:(其中R 6 -R 10是选自氢，低级烷基，低级环烷基，芳基，卤素原子，低级烷氧基， 氨基，N-低级酰氨基，硝基，低级烷硫基和羧基），形成硫化物键，由此制造通式（3）的二芳基硫醚衍生物:( 其中R1-R10与上述相同）或sa 其中。 药物化合物如二苯并[b，f]硫嘌呤衍生物由二芳基硫醚衍生物或其盐通过已知技术制备。