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    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。

    Tracheal smooth muscle relaxant
    5.
    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]。

    Glutamic acid receptor agonist
    6.
    发明授权
    Glutamic acid receptor agonist 失效
    谷氨酸受体激动剂

    公开(公告)号：US5955505A

    公开(公告)日：1999-09-21

    申请号：US894433

    申请日：1997-08-20

    申请人： Jiro Takeo ,  Shinya Yamashita ,  Keiji Wada ,  Yoshiyuki Chiba

    发明人： Jiro Takeo ,  Shinya Yamashita ,  Keiji Wada ,  Yoshiyuki Chiba

    IPC分类号： A61K31/00 ,  A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/216 ,  A61K31/4035 ,  A61K31/4406 ,  C07C317/28 ,  C07C323/49 ,  C07C323/56 ,  C07C323/62 ,  A61K31/44

    CPC分类号： C07C323/62 ,  A61K31/00 ,  A61K31/18 ,  A61K31/192 ,  A61K31/195 ,  A61K31/216 ,  A61K31/4035 ,  A61K31/4406 ,  C07C317/28 ,  C07C323/49 ,  C07C323/56

    摘要： A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.2 is a hydrogen atom, a hydroxyl group, an alkyl group having 1 to 3 carbon atoms, a carboxymethyl group or an alkoxycarbonylmethyl group having 3 to 6 carbon atoms; m is an integer from 0 to 2; and n is an integer from 0 to 3, or an pharmaceutically acceptable salt thereof, as an effective ingredient. The agonist is efficacious in the medical treatment of nerve degenerative disorders.

    摘要翻译： PCT No.PCT / JP96 / 00379 Sec。 371日期1997年8月20日 102（e）日期1997年8月20日PCT提交1996年2月20日PCT公布。 公开号WO96 / 25926 日期：1996年8月29日一种方法，包括向需要谷氨酸受体活化的患者施用磺酰胺衍生物，其中A为萘基，吡啶基，苯基，被1〜 5个选自卤素原子，具有1至40个碳原子的烷基，具有1至4个碳原子的烷氧基，硝基和乙酰氨基，或具有1至20个碳的烷基的基团 原子 B是具有1至3个碳原子的亚烷基，-OCH 2 - 或-CH = CH-的基团; X和Y相同或不同，分别为氢原子或氟原子; R为羧基，碳原子数2〜5的烷氧基羰基，羟甲基或其中R1为氢原子或碳原子数1〜3的烷基的基团。 R2为氢原子，羟基，碳原子数为1〜3的烷基，羧甲基或碳原子数为3〜6的烷氧基羰基甲基。 m为0〜2的整数; n为0〜3的整数，或其药学上可接受的盐作为有效成分。 激动剂在神经退行性疾病的治疗中是有效的。

    Tricyclic fused heterocycle compounds, process for preparing the same and use thereof
    7.
    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。

    Prodrug, medicinal utilization thereof and process for producing the same
    8.
    发明申请
    Prodrug, medicinal utilization thereof and process for producing the same 审中-公开
    前药，药用及其制备方法

    公开(公告)号：US20050203061A1

    公开(公告)日：2005-09-15

    申请号：US10505961

    申请日：2003-06-20

    申请人： Shinya Yamashita ,  Jiro Takeo ,  Takaaki Okita

    发明人： Shinya Yamashita ,  Jiro Takeo ,  Takaaki Okita

    IPC分类号： A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P43/00 ,  C07H15/18 ,  C07H15/203 ,  A61K31/715 ,  C07H5/04

    CPC分类号： C07H15/203 ,  C07H15/18

    摘要： A prodrug utilizes an enzyme whose enzymatic activity is different in between the target site of the drug and the site to express side effects, the prodrug having a substituent cleavable with the enzyme and being activated by cleaving the substituent with the enzyme. As the target site of the drug, for example, a respiratory organ can be mentioned and as the site to express side effects, for example, the heart can be mentioned. As the example of the drug, a bronchodilator can be mentioned and as the example of the enzyme, a glycosidase (for example, β-glucuronidase) can be mentioned. Furthermore, the substituent is, for example, a glycosyl group composed of a monosaccharide or an oligosaccharide. Use of the enzyme enables reducing the side effects of a drug of the type whose target site is different from the site to express side effects.

    摘要翻译： 前体药物利用酶的活性在药物的靶位点和表达副作用的位点之间的酶活性不同的酶，前药具有可与酶切割的取代基并通过用酶切割取代基来活化。 作为药物的靶位，例如可以提及呼吸器官，作为表达副作用的部位，例如可以提及心脏。 作为药物的实例，可以提及支气管扩张剂，作为酶的实例，可以提及糖苷酶（例如β-葡糖苷酸酶）。 此外，取代基是例如由单糖或寡糖构成的糖基。 使用该酶能够减少目标部位不同于该部位的药物的副作用，以表现副作用。