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    HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 DATA-HYDROXYSTEROID DEHYDROGENASE
    3.
    发明申请
    HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 DATA-HYDROXYSTEROID DEHYDROGENASE 审中-公开
    具有I型11数据羟基脱氢酶抑制活性的杂环衍生物

    公开(公告)号：US20100234363A1

    公开(公告)日：2010-09-16

    申请号：US12679159

    申请日：2008-09-17

    申请人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

    发明人： Akiko Itai ,  Susumu Muto ,  Ryuko Tokuyama ,  Hiroshi Fukasawa ,  Takeshi Yanase

    IPC分类号： A61K31/5415 ,  C07D279/08 ,  A61P3/10 ,  C07D265/24 ,  A61K31/536

    CPC分类号： C07D279/06 ,  C07D265/24 ,  C07D279/08 ,  C07D417/04 ,  C07D417/12

    摘要： Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.

    摘要翻译： 公开了可用作11-羟基类固醇脱氢酶1型抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中X为O或S，虚线和波浪线表示存在或不存在键，（i）当虚线表示 键的存在，波浪线表示不存在键，R2和R3各自独立地为氢，卤素，氰基，羟基，羧基，任选取代的烷基，任选取代的烯基，任选取代的炔基等，（ii）当 虚线表示不存在键，波浪线表示键的存在，R 1和R 4各自独立地为氢，卤素等，R 2和R 3各自独立地为氢，卤素，氰基，羟基，羧基，任选地 取代的烷基，任选取代的烯基，任选取代的炔基等，R 5和R 6各自独立地为氢，任选取代的烷基，任选取代的烯基，任选取代的炔基等。

    Antiallergic agents
    5.
    发明授权
    Antiallergic agents 失效
    抗过敏剂

    公开(公告)号：US07700655B2

    公开(公告)日：2010-04-20

    申请号：US11783324

    申请日：2007-04-09

    申请人： Susumu Muto ,  Akiko Itai

    发明人： Susumu Muto ,  Akiko Itai

    IPC分类号： A61K31/165

    CPC分类号： C07D295/192 ,  A61K31/055 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/167 ,  A61K31/18 ,  A61K31/357 ,  A61K31/381 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/455 ,  A61K31/47 ,  A61K31/498 ,  A61K31/5375 ,  A61K31/606 ,  A61K31/609 ,  A61K31/616 ,  A61K31/63 ,  C07C235/64

    摘要： A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

    摘要翻译： 一种用于预防和/或治疗过敏性疾病和/或子宫内膜异位症和/或子宫肌瘤的药物，其包含作为活性成分的选自以下通式（I）表示的化合物和药理学上可接受的物质 其盐及其水合物及其溶剂化物：其中X表示主链中的原子数为2〜5的连接基（所述连接基可以被取代），A表示氢原子或乙酰基，E表示 可以被取代的芳基或可以被取代的杂芳基，环Z表示可以具有一个或多个取代基的芳族，除了由式-OA表示的基团之外，其中A具有与上述相同的含义， 由式-XE表示的基团，其中X和E各自具有与上述定义相同的含义，或可以具有一个或多个取代基的杂芳烃 与式-O-A表示的基团的离子，其中A具有与上述相同的含义和由式-X-E表示的基团，其中X和E各自具有与上述相同的含义。

    Coumarin derivative
    6.
    发明授权
    Coumarin derivative 失效
    香豆素衍生物

    公开(公告)号：US07411076B2

    公开(公告)日：2008-08-12

    申请号：US10488254

    申请日：2002-09-12

    申请人： Susumu Muto ,  Masayuki Komukai ,  Akiko Itai

    发明人： Susumu Muto ,  Masayuki Komukai ,  Akiko Itai

    IPC分类号： C07D311/16 ,  C07D409/12 ,  C07D405/12 ,  C07C407/12

    CPC分类号： C07D405/12 ,  A61K31/282 ,  A61K31/37 ,  A61K31/381 ,  A61K31/382 ,  A61K31/385 ,  A61K31/407 ,  A61K31/4433 ,  A61K31/675 ,  A61K31/704 ,  A61K31/7064 ,  A61K33/24 ,  A61K45/06 ,  C07D311/16 ,  C07D407/12 ,  C07D409/12

    摘要： A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I): wherein X represents a single bond or a C1 to C6 alkylene group which may be substituted; A represents a C1 to C6 alkyl group which may be substituted, a C6 to C10 aryl group which may be substituted, or a 4 to 10-membered monocyclic or bicyclic and unsaturated, partly saturated, or completely saturated heterocyclic group which may be substituted, wherein said heterocyclic group comprises as ring-constituting atoms 1 to 4 hetero atoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

    摘要翻译： 一种用于增强基于DNA损伤作用模式的癌症治疗效果的药物，其包含作为活性成分的由以下通式（I）表示的化合物：其中X表示单键或C < 1可以被取代的C 6亚烷基; A表示可被取代的C 6〜C 6烷基，C 6〜C 10芳基的C 1〜 可以被取代的基团，或可以被取代的4元至10元单环或双环和不饱和的，部分饱和的或完全饱和的杂环基，其中所述杂环基包含1-4个选自以下的杂原子： 由氮原子，氧原子和硫原子组成的组。

    Antiallergic agents
    7.
    发明申请
    Antiallergic agents 失效
    抗过敏剂

    公开(公告)号：US20070185110A1

    公开(公告)日：2007-08-09

    申请号：US11783324

    申请日：2007-04-09

    申请人： Susumu Muto ,  Akiko Itai

    发明人： Susumu Muto ,  Akiko Itai

    IPC分类号： A61K31/5375 ,  A61K31/445 ,  A61K31/40 ,  A61K31/165

    CPC分类号： C07D295/192 ,  A61K31/055 ,  A61K31/137 ,  A61K31/15 ,  A61K31/165 ,  A61K31/167 ,  A61K31/18 ,  A61K31/357 ,  A61K31/381 ,  A61K31/40 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/421 ,  A61K31/422 ,  A61K31/427 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/455 ,  A61K31/47 ,  A61K31/498 ,  A61K31/5375 ,  A61K31/606 ,  A61K31/609 ,  A61K31/616 ,  A61K31/63 ,  C07C235/64

    摘要： A medicament for the preventive and/or therapeutic treatment of allergic diseases and/or endometriosis and/or hysteromyoma which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substitutents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

    摘要翻译： 一种用于预防和/或治疗过敏性疾病和/或子宫内膜异位症和/或子宫肌瘤的药物，其包含作为活性成分的选自以下通式（I）表示的化合物和药理学上可接受的物质 其盐及其水合物及其溶剂化物：其中X表示主链中的原子数为2〜5的连接基（所述连接基可以被取代），A表示氢原子或乙酰基，E表示 可以被取代的芳基或可以被取代的杂芳基，环Z表示可以具有一个或多个取代基的芳族，除了由式-OA表示的基团之外，其中A具有与上述相同的含义， 由式-XE表示的基团，其中X和E各自具有与上述相同的含义，或另外可以具有一个或多个取代基的杂芳烃 与由式-O-A表示的基团，其中A具有与上述相同的含义和由式-X-E表示的基团，其中X和E各自具有与上述相同的含义。

    Inhibitors against the activation of ap-1 and nfat
    10.
    发明申请
    Inhibitors against the activation of ap-1 and nfat 审中-公开
    抑制剂对ap-1和nfat的激活

    公开(公告)号：US20060100257A1

    公开(公告)日：2006-05-11

    申请号：US10515342

    申请日：2003-06-05

    申请人： Susumu Muto ,  Akiko Itai

    发明人： Susumu Muto ,  Akiko Itai

    IPC分类号： A61K31/427 ,  A61K31/403

    CPC分类号： A61K31/222 ,  A61K31/00 ,  A61K31/055 ,  A61K31/121 ,  A61K31/15 ,  A61K31/166 ,  A61K31/167 ,  A61K31/17 ,  A61K31/18 ,  A61K31/185 ,  A61K31/192 ,  A61K31/216 ,  A61K31/275 ,  A61K31/357 ,  A61K31/381 ,  A61K31/402 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/404 ,  A61K31/4164 ,  A61K31/421 ,  A61K31/426 ,  A61K31/433 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4418 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/47 ,  A61K31/496

    摘要： A medicament inhibiting the activation of AP-1 which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in the main chain is 2 to 5 (said connecting group may be substituted), A represents hydrogen atom or acetyl group, E represents an aryl group which may be substituted or a hetero aryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above, or a heteroarene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group represented by formula —X-E wherein each of X and E has the same meaning as that defined above.

    摘要翻译： 一种抑制AP-1活化的药物，其包含选自下述通式（I）表示的化合物及其药理学可接受的盐及其水合物及其溶剂合物作为活性成分的物质： 其中X表示主链中的原子数为2〜5的连接基团（所述连接基团可以被取代），A表示氢原子或乙酰基，E表示可被取代的芳基或杂芳基， 可以被取代，环Z表示除了由式-OA表示的基团之外还可以具有一个或多个取代基的芳烃，其中A具有与上述相同的含义和由式-XE表示的基团，其中X和E各自 具有与上述相同的含义，或除了由式-OA表示的基团之外还可以具有一个或多个取代基的杂芳烃，其中A具有与tha相同的含义 t和由式-X-E表示的基团，其中X和E各自具有与上述相同的含义。