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    VLA-4 inhibitory drug
    2.
    发明授权
    VLA-4 inhibitory drug 失效
    VLA-4抑制药

    公开(公告)号：US08129366B2

    公开(公告)日：2012-03-06

    申请号：US12097269

    申请日：2006-12-13

    申请人： Nobuo Machinaga ,  Shin Iimura ,  Yoshiyuki Yoneda ,  Jun Chiba ,  Fumihito Muro ,  Hideko Hoh ,  Atsushi Nakayama

    发明人： Nobuo Machinaga ,  Shin Iimura ,  Yoshiyuki Yoneda ,  Jun Chiba ,  Fumihito Muro ,  Hideko Hoh ,  Atsushi Nakayama

    IPC分类号： A61K31/553 ,  C07D243/08

    CPC分类号： C07D409/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  C07D491/048 ,  C07D491/056 ,  C07D491/08 ,  C07D495/04

    摘要： There is provided a VLA-4 inhibitory drug having good oral absorbability and exhibiting sufficient anti-inflammatory effects when administered orally.A compound represented by the following formula (I): wherein R1 represents a hydrogen atom or a C1-8 alkyl group; R2 represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group, or a benzyloxy group which may be substituted; Q represents a monocyclic or bicyclic nitrogen-containing heterocyclic group which may be substituted, and has a nitrogen atom as the bonding site; Y represents an oxygen atom or CH2; W represents a bicyclic aromatic hydrocarbon ring group which may be substituted, or a bicyclic aromatic heterocyclic group which may be substituted; R3a, R3b and R3c each independently represent a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group; and A1 represents a nitrogen atom or C—R3d (wherein R3d represents a hydrogen atom, a halogen atom, a C1-8 alkoxy group or a C1-8 alkyl group), or a salt thereof, or a VLA-4 inhibitory drug comprising the compound or the salt as an active ingredient.

    摘要翻译： 提供口服吸收性良好的VLA-4抑制药物，口服给药时具有足够的抗炎作用。 由下式（I）表示的化合物：其中R1表示氢原子或C1-8烷基; R2表示氢原子，卤素原子，C1-8烷氧基或可被取代的苄氧基; Q表示可以被取代的单环或双环含氮杂环基，并且具有氮原子作为键合位点; Y表示氧原子或CH2; W表示可被取代的双环芳香族烃环基或可被取代的双环芳香族杂环基; R3a，R3b和R3c各自独立地表示氢原子，卤素原子，C1-8烷氧基或C1-8烷基; A1表示氮原子或C-R3d（其中R3d表示氢原子，卤原子，C1-8烷氧基或C1-8烷基）或其盐或VLA-4抑制药，其包含 化合物或盐作为活性成分。

    Vla-4 Inhibitor
    5.
    发明申请
    Vla-4 Inhibitor 审中-公开
    Vla-4抑制剂

    公开(公告)号：US20070232601A1

    公开(公告)日：2007-10-04

    申请号：US11629354

    申请日：2005-06-14

    申请人： Yoshiyuki Yoneda ,  Atsushi Nakayama ,  Nobuo Machinaga ,  Jun Chiba ,  Fumihito Muro

    发明人： Yoshiyuki Yoneda ,  Atsushi Nakayama ,  Nobuo Machinaga ,  Jun Chiba ,  Fumihito Muro

    IPC分类号： A61K31/535 ,  A61K31/40 ,  A61K31/425 ,  C07D207/00 ,  C07D263/00 ,  C07D277/62 ,  C07D265/28 ,  C07D241/00 ,  A61K31/445 ,  A61K31/497

    CPC分类号： C07D417/14 ,  C07D413/14

    摘要： An object of the present invention is to provide a compound which selectively inhibits binding of a ligand and α4β1 integrin (VLA-4), a process for producing the compound, and a medicament containing the compound. A compound represented by the formula (I) etc. or a salt thereof, a process for producing the compound or a salt thereof, a medicament containing the compound or a salt thereof, as well as a preventive and/or a therapeutic agent for a disease caused by cell adhesion, for example, inflammatory reaction, autoimmune disease, cancer metastasis, bronchial asthma, nasal obstruction, diabetes, arthritis, psoriasis, multiple sclerosis, inflammatory bowel disease and rejection reaction at transplantation, containing the compound or a salt thereof as a primary component. [wherein Y1 represents a divalent aryl group etc., V1 represents an aryl group etc., and R11 to R14 represent H, OH or a halogen atom etc.]

    摘要翻译： 本发明的目的是提供选择性抑制配体和α4β1整联蛋白（VLA-4）结合的化合物，该化合物的制备方法和含有该化合物的药物。 由式（I）等表示的化合物或其盐，化合物或其盐的制备方法，含有该化合物或其盐的药物以及用于治疗和/ 包含其化合物或其盐的细胞粘附引起的疾病，例如炎性反应，自身免疫性疾病，癌症转移，支气管哮喘，鼻塞，糖尿病，关节炎，银屑病，多发性硬化，炎症性肠病和移植排斥反应 主要组成部分。 [其中Y 1表示二价芳基等，V 1表示芳基等，R 11至R 11， 14表示H，OH或卤素原子等]

    Vla-4 inhibitors
    9.
    发明授权
    Vla-4 inhibitors 失效
    Vla-4抑制剂

    公开(公告)号：US07157487B2

    公开(公告)日：2007-01-02

    申请号：US10451159

    申请日：2001-12-28

    申请人： Atsushi Nakayama ,  Nobuo Machinaga ,  Yoshiyuki Yoneda ,  Yuichi Sugimoto ,  Jun Chiba ,  Toshiyuki Watanabe ,  Shin Iimura

    发明人： Atsushi Nakayama ,  Nobuo Machinaga ,  Yoshiyuki Yoneda ,  Yuichi Sugimoto ,  Jun Chiba ,  Toshiyuki Watanabe ,  Shin Iimura

    IPC分类号： A61K31/405 ,  C07D209/04

    CPC分类号： C07D263/58 ,  C07C275/42 ,  C07D209/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D491/04

    摘要： The present invention relates to a compound represented by the following formula (I): (wherein, W represents WA-A1-WB- (in which, WA is substituted or unsubstituted aryl, etc., A1 is —NR1—, single bond, —C(O)—, etc., and WB is substituted or unsubstituted arylene, etc.), R is single bond, —NH—, —OCH2—, alkenylene, etc., X is —C(O)—, —CH2—, etc., and M is, for example, the following formula: (in which, R11, R12 and R13 each independently represents hydrogen, hydroxyl, amino, halogen, etc., R14 is hydrogen or lower alkyl, Y represents —CH2—O—, etc., Z is substituted or unsubstituted arylene, etc., A2 is single bond, etc, and R10 is hydroxyl or lower alkoxy)), or salt thereof; and a medicament containing the same. This compound or salt thereof selectively inhibits binding of cell adhesion molecules to VLA-4 and exhibits high bioavailability so that it is useful as a preventive and/or remedy for inflammatory diseases, autoimmune diseases, metastasis, bronchial asthma, rhinostenosis, diabetes, and the like.

    摘要翻译： 本发明涉及由下式（I）表示的化合物：（其中，W表示W A，A，B， - （其中，W A是取代或未取代的芳基等，A 1是-NR 1 - 单键，-C （O） - 等，W B是取代或未取代的亚芳基等），R是单键，-NH-，-OCH 2 - ，亚烯基 等等，X是-C（O） - ， - CH 2 - 等，M是例如下式：（其中R 11， R 12，R 12和R 13各自独立地表示氢，羟基，氨基，卤素等，R 14是氢或低级烷基 ，Y表示-CH 2 -O-O-等，Z是取代或未取代的亚芳基等，A 2是单键等，R“ 10是羟基或低级烷氧基））或其盐; 和含有该药物的药物。 该化合物或其盐选择性地抑制细胞粘附分子与VLA-4的结合并且表现出高的生物利用度，使得其可用作炎性疾病，自身免疫性疾病，转移，支气管哮喘，鼻窦炎，糖尿病的预防和/或补救。 喜欢。

    Process for producing pyrrolidine derivative
    10.
    发明申请
    Process for producing pyrrolidine derivative 失效
    制备吡咯烷衍生物的方法

    公开(公告)号：US20070105935A1

    公开(公告)日：2007-05-10

    申请号：US10556043

    申请日：2004-05-07

    申请人： Atsushi Nakayama ,  Nobuo Machinaga ,  Yoshiyuki Yoneda ,  Masaki Setoguchi

    发明人： Atsushi Nakayama ,  Nobuo Machinaga ,  Yoshiyuki Yoneda ,  Masaki Setoguchi

    IPC分类号： A61K31/405 ,  C07D403/02

    CPC分类号： C07D207/12

    摘要： This invention provides an industrially useful process for producing 1,4-transcyclohexanecarboxylic acid derivative (1) which has excellent VLA-4 inhibitory action and safety, and an intermediate which is useful in such method. More particularly, this invention relates to a process for converting a compound of formula (I) into a compound of formula (VI) by the reaction scheme:

    摘要翻译： 本发明提供了具有优异的VLA-4抑制作用和安全性的1,4-反式环己烷羧酸衍生物（1）的工业上有用的方法和可用于该方法的中间体。 更具体地，本发明涉及通过反应方案将式（I）化合物转化为式（VI）的化合物的方法：