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    Carboxilic acid derivatives
    2.
    发明授权
    Carboxilic acid derivatives 失效
    羧酸衍生物

    公开(公告)号：US08044236B2

    公开(公告)日：2011-10-25

    申请号：US11870718

    申请日：2007-10-11

    申请人： Youichi Yamaguchi ,  Takeshi Yanase ,  Susumu Muto ,  Akiko Itai

    发明人： Youichi Yamaguchi ,  Takeshi Yanase ,  Susumu Muto ,  Akiko Itai

    IPC分类号： C07C65/00 ,  C07C59/40

    CPC分类号： C07C51/00 ,  C07C59/64 ,  C07C65/24 ,  C07C65/28 ,  C07C205/06 ,  C07C205/34 ,  C07C217/86 ,  C07C235/80 ,  C07C255/37

    摘要： A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein R1 represents a C6-10 aryl group; or a substituted C6-10 aryl group, R2 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a phenyl group and carboxy group, X represents —CH2—, —CH2CH2—, —CH═CH— or —N(R3)—C(═O)—, Y represents carboxy group or a bioisostere of carboxy group, R3 represents hydrogen atom, a C1-4 alkyl group or a C7-12 aralkyl group, m represents 0 or 1.

    摘要翻译： 具有对纤维蛋白溶酶原激活物抑制剂-1（PAI-1）具有抑制作用的由以下通式（I）表示的化合物或其盐，或其水合物或其溶剂化物：其中R1表示C6-10芳基; 或取代的C6-10芳基，R2表示C6-10芳基; 或被选自卤素原子，硝基，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基，卤代 C 1-6烷氧基，苯基和羧基，X表示-CH 2 - ， - CH 2 CH 2 - ， - CH = CH-或-N（R 3）-C（= O） - ，Y表示羧基或生物电子 羧基，R 3表示氢原子，C 1-4烷基或C 7-12芳烷基，m表示0或1。

    N-phenyloxamide derivatives
    4.
    发明授权
    N-phenyloxamide derivatives 有权
    N-苯基酰胺衍生物

    公开(公告)号：US07884234B2

    公开(公告)日：2011-02-08

    申请号：US11870741

    申请日：2007-10-11

    申请人： Youichi Yamaguchi ,  Takeshi Yanase ,  Susumu Muto ,  Akiko Itai

    发明人： Youichi Yamaguchi ,  Takeshi Yanase ,  Susumu Muto ,  Akiko Itai

    IPC分类号： C07C229/00

    CPC分类号： C07D307/91 ,  C07C233/56 ,  C07C255/60 ,  C07C323/41

    摘要： A compound represented by the following general formula (I) or a salt thereof, or a hydrate thereof or a solvate thereof having an inhibitory action against plasminogen activator inhibitor-1 (PAI-1): wherein R1 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, cyano group, nitro group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group and a C1-6 alkylsulfanyl group, R2 represents a C6-10 aryl group; or a C6-10 aryl group substituted with a group or groups selected from the group consisting of a halogen atom, hydroxy group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxy group, a halogenated C1-6 alkoxy group, a C1-6 alkylsulfanyl group and phenyl group, X represents a single bond or oxygen atom, Z represents a phenylene group or a substituted phenylene group, m represents 0 or 1.

    摘要翻译： 具有对纤维蛋白溶酶原激活物抑制剂-1（PAI-1）具有抑制作用的由以下通式（I）表示的化合物或其盐，或其水合物或其溶剂化物：其中R1表示C6-10芳基; 或被选自卤素原子，氰基，硝基，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基中的一个或多个基团取代的C 6-10芳基 卤代C 1-6烷氧基和C 1-6烷硫基，R 2表示C 6-10芳基; 或被选自卤素原子，羟基，C 1-6烷基，卤代C 1-6烷基，C 1-6烷氧基，卤代的基团取代的C 6-10芳基 C 1-6烷氧基，C 1-6烷硫基和苯基，X表示单键或氧原子，Z表示亚苯基或取代亚苯基，m表示0或1。

    HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 DATA-HYDROXYSTEROID DEHYDROGENASE
    5.
    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
    10.
    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。