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    NORVALINE DERIVATIVE AND METHOD FOR PREPARATION THEREOF
    2.
    发明申请
    NORVALINE DERIVATIVE AND METHOD FOR PREPARATION THEREOF 审中-公开
    NORVALINE DERIVATIVE AND METHOD FOR COMPEPARTING THEREOF

    公开(公告)号：WO2006080477A1

    公开(公告)日：2006-08-03

    申请号：PCT/JP2006/301394

    申请日：2006-01-24

    Applicant: TANABE SEIYAKU CO., LTD. ,  HARADA, Naoyuki ,  HIKOTA, Masataka

    Inventor： HARADA, Naoyuki ,  HIKOTA, Masataka

    IPC: C07C237/22 ,  C07D295/12 ,  C07D295/14 ,  C07C323/62 ,  C07C323/63 ,  C07D211/14 ,  C07D211/58 ,  A61K31/165 ,  A61K31/44 ,  A61P25/00 ,  A61P13/00

    CPC classification number: C07D295/13 ,  C07C237/22 ,  C07C323/60 ,  C07C323/62 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07D207/09 ,  C07D211/58 ,  C07D295/155

    Abstract: Norvaline derivative of the formula [I] or pharmaceutically acceptable salt thereof, method for preparing the same, pharmaceutical composition containing the same, and use of said compound for inhibiting transporting activity of glycine transporter type 2 (GlyT2). [wherein X is -CH 2 -, -O-, -S- or single bond; Ar is optionally substituted aryl or lower cycloalkyl; n is 0 to 2; R 1 and R 2 are (i) each is hydrogen or lower alkyl; (ii) R 1 and R 2 are combined to form lower alkylene; or (iii) R 1 is hydrogen or lower alkyl and R 2 is combined with R 4 or R 6 to form lower alkylene; R 3 and R 4 are (i) each is hydrogen or lower alkyl; (ii) R 3 and R 4 are combined to form lower alkylene; or (iii) R 3 is hydrogen or lower alkyl and R 4 is combined with R 2 or R 6 to form lower alkylene; R is or -OR 7 ; R 5 and R 6 are (i) each is optionally substituted lower alkyl, or hydrogen; (ii) R 5 and R 6 are combined to form aliphatic 5- to 6-membered heterocyclic group; or (iii) R 5 is optionally substituted lower alkyl or hydrogen and R 6 is combined with R 2 or R 4 to form lower alkylene; R 7 is lower alkyl.

    Abstract translation: 式[I]的诺瓦宁衍生物或其药学上可接受的盐，其制备方法，含有该化合物的药物组合物和所述化合物用于抑制甘氨酸转运蛋白2型（GlyT2）的转运活性的用途。 [其中X是-CH 2 - ， - O - ， - S-或单键; Ar是任选取代的芳基或低级环烷基; n为0〜2; R 1和R 2均为（i）各自为氢或低级烷基; （ii）R 1和R 2结合形成低级亚烷基; 或（iii）R 1是氢或低级烷基，R 2与R 4或R 6相结合， 形成低级亚烷基; R 3和R 4是（i）各自为氢或低级烷基; （ii）R 3和R 4结合形成低级亚烷基; 或（iii）R 3是氢或低级烷基，R 4与R 2或R 6相结合， 形成低级亚烷基; R是或-OR 7; R 5和R 6是（i）各自为任选取代的低级烷基或氢; （ii）R 5和R 6结合形成脂族5至6元杂环基; 或（iii）R 5是任选取代的低级烷基或氢，R 6与R 2或R 4相结合， SUP>以形成低级亚烷基; R 7是低级烷基。

    IMIDAZOLE COMPOUND
    7.
    发明申请
    IMIDAZOLE COMPOUND 审中-公开
    咪唑化合物

    公开(公告)号：WO2006030977A2

    公开(公告)日：2006-03-23

    申请号：PCT/JP2005/017540

    申请日：2005-09-16

    Applicant: TANABE SEIYAKU CO., LTD. ,  KUSAMA, Mari ,  WATANABE, Tatsuya ,  HOSAKA, Toshihiro ,  KUBOTA, Yuko

    Inventor： KUSAMA, Mari ,  WATANABE, Tatsuya ,  HOSAKA, Toshihiro ,  KUBOTA, Yuko

    CPC classification number: C07D233/64 ,  C07D401/04 ,  C07D403/10 ,  C07D409/04 ,  C07D487/04

    Abstract: An imidazole compound of the formula (1): wherein Ring A is benzene or a heterocyclic ring; G is alkylthio, alkylsulfonyl, optionally substituted phenyl, or optionally substituted heterocyclic ring group, etc.; Ring C is imidazole; R 1 is carbamoyl, etc.; R 2 is cyano, nitro, hydroxyl, an alkoxy, a halogen, carboxy, an alkoxycarbonyl, carbamoyl, amino, an alkyl, etc.; m is 0 to 2; and R 4 is hydrogen, an alkyl, etc., or a pharmaceutically acceptable salt thereof, is a large conductance calcium-activated K channel opener useful for treatment of pollakiuria, urinary incontinence, etc.

    Abstract translation: 式（1）的咪唑化合物：其中环A是苯或杂环; G是烷硫基，烷基磺酰基，任选取代的苯基或任选取代的杂环基团等; 环C是咪唑; R 1是氨基甲酰基等; R 2是氰基，硝基，羟基，烷氧基，卤素，羧基，烷氧基羰基，氨基甲酰基，氨基，烷基等; m为0〜2; R 4是氢，烷基等或其药学上可接受的盐，是用于治疗尿频，尿失禁等的大电导钙激活K通道开放剂。

    SUBSTITUTED BENZIMIDAZOLE-, BENZTRIAZOLE-, AND BENZIMIDAZOLONE-O-GLUCOSIDES
    9.
    发明申请
    SUBSTITUTED BENZIMIDAZOLE-, BENZTRIAZOLE-, AND BENZIMIDAZOLONE-O-GLUCOSIDES 审中-公开
    取代的苯并咪唑，苯并唑和 - 苯并咪唑酮-O-葡萄糖苷

    公开(公告)号：WO2005012242A2

    公开(公告)日：2005-02-10

    申请号：PCT/US2004/024673

    申请日：2004-07-30

    Applicant: JANSSEN PHARMACEUTICA NV ,  TANABE SEIYAKU CO., LTD ,  URBANSKI, Maud

    Inventor： URBANSKI, Maud

    IPC: C07D

    CPC classification number: C07H15/26

    Abstract: This invention relates to to substituted benzimidazole-O-glucosides, benztriazole-O-glucosides, and benzimidazolone-O-glucosides, compositions containing them, and methods of using them, for example, for the treatment or prophylaxis of diabetes and Syndrome X.

    Abstract translation: 本发明涉及取代的苯并咪唑-O-葡萄糖苷，苯并三唑-O-葡糖苷和苯并咪唑酮-O-葡糖苷，含有它们的组合物，以及使用它们的方法，例如用于治疗或预防糖尿病和综合征X.

    A PROCESS FOR PREPARING A PHENYLALANINE DERIVATIVE AND INTERMEDIATES THEREOF
    10.
    发明申请
    A PROCESS FOR PREPARING A PHENYLALANINE DERIVATIVE AND INTERMEDIATES THEREOF 审中-公开
    一种制备苯丙氨酸衍生物及其中间体的方法

    公开(公告)号：WO2003072536A1

    公开(公告)日：2003-09-04

    申请号：PCT/JP2003/002181

    申请日：2003-02-27

    Applicant: TANABE SEIYAKU CO., LTD. ,  INOUE, Isao ,  KURODA, Toru ,  YOSHIOKA, Ryuzo

    Inventor： INOUE, Isao ,  KURODA, Toru ,  YOSHIOKA, Ryuzo

    IPC: C07C233/87

    CPC classification number: C07C233/87 ,  C07C231/02 ,  C07F5/025

    Abstract: The present invention provides a process for preparing a novel phenylalanine derivative of the formula (I): wherein X1 is a halogen atom, X2 is a halogen atom, Q is a group of the formula -CH2- or -(CH2)2- and Y is a lower alkyl group, or a pharmaceutically acceptable salt thereof, which has excellent inhibitory effects on α4 integrin-mediated cell adhesion, and an intermediate useful in the process.

    Abstract translation: 本发明提供了制备式（I）的新型苯丙氨酸衍生物的方法：其中X1是卤素原子，X2是卤素原子，Q是式-CH2-或 - （CH2）2-的基团，和 Y是对α4整联蛋白介导的细胞粘附具有优异抑制作用的低级烷基或其药学上可接受的盐，以及在该方法中有用的中间体。

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