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    PROCESS FOR PRODUCING PYRROLIDINE DERIVATIVE
    2.
    发明公开
    PROCESS FOR PRODUCING PYRROLIDINE DERIVATIVE 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES PYRROLIDINDERIVATS

    公开(公告)号：EP1623975A4

    公开(公告)日：2008-07-02

    申请号：EP04731729

    申请日：2004-05-07

    申请人： DAIICHI SEIYAKU CO

    发明人： NAKAYAMA A ,  MACHINAGA N ,  YONEDA Y ,  SETOGUCHI M

    IPC分类号： C07D207/04 ,  C07D207/12 ,  C07D403/12

    CPC分类号： C07D207/12

    摘要： A process for industrially advantageously producing a 1,4-trans-cyclohexanecarboxylic acid derivative (1) which has excellent VLA-4 inhibitory activity and is safe; and an intermediate advantageous for the production process. The process comprises converting a compound represented by the formula (I) into a compound represented by the formula (VI) according to the following scheme.

    摘要翻译： 在工业上有利地制备具有良好VLA-4抑制活性且安全的1,4-反式 - 环己烷羧酸衍生物（1）的方法; 以及对生产过程有利的中间产品。 该方法包括根据以下方案将由式（I）表示的化合物转化为由式（VI）表示的化合物。

    PROCESS FOR PRODUCING 1,2-CIS-2-FLUOROCYCLOPROPANE-1­CARBOXYLIC ESTER COMPOUND
    3.
    发明公开
    PROCESS FOR PRODUCING 1,2-CIS-2-FLUOROCYCLOPROPANE-1­CARBOXYLIC ESTER COMPOUND 有权
    VERFAHREN ZUR HERSTELLUNG EINER 1,2-CIS-2-FLUORCYCLOPROPAN-1-CARBONSÄUREESTERVERBINDUNG

    公开(公告)号：EP1731499A4

    公开(公告)日：2008-04-02

    申请号：EP05727931

    申请日：2005-03-31

    申请人： DAIICHI SEIYAKU CO

    发明人： SATO KOJI ,  IMAI MAKOTO

    IPC分类号： C07C67/317 ,  C07B61/00 ,  C07C69/74

    CPC分类号： C07C67/317 ,  C07C2601/02 ,  C07C69/74

    摘要： An industrially usable process for producing a 1,2-cis-2-fluorocyclopropane-1-carboxylic ester. The process, which is for producing a compound represented by the following general formula (3): [Chemical formula 2] (wherein R1 represents C1-8 alkyl, etc.), comprises reacting a compound represented by the following general formula (1): [Chemical formula 1] [wherein X1 represents hydrogen, chlorine, bromine, or iodine and X2 represents hydrogen, chlorine, bromine, or iodine, provided that not both of X1 and X2 are hydrogen; and R1 is the same as defined above] with a reducing agent represented by the formula (2): M1BHmR2n (2-1) or M2(BHmR2n)2 (2-2) (wherein M1 represents an alkali metal; M2 represents an alkaline earth metal or zinc; R2 represents hydrogen, etc.; and m is an integer of 1-4 and n is an integer of 0-3, provided that the sum of m and n is 4) in the presence of an aprotic polar solvent and a Lewis acid such as, e.g., a halide of an element selected among boron, magnesium, aluminum, etc.

    摘要翻译： 提供了用于生产1,2-顺式-2-氟环丙烷-1-羧酸酯的工业上适用的方法。 制备由式（3）表示的化合物的方法：[其中R 1表示例如C 1 -C 8烷基]，该方法包括使式（1）表示的化合物：[其中X 1表示氢 原子，氯原子，溴原子或碘原子; X 2表示氢原子，氯原子，溴原子或碘原子; X 1和X 2不同时为氢原子; 和R 1具有与式（3）中所定义的含义相同的含义）与式（2）表示的还原剂：ƒ€ƒ€ƒ€ƒ€ƒ€ƒM1 BH m R 2 n -1）或M 2（BH m R 2 n）2€ƒ€ƒ€ƒ（2-2）[其中M 1表示碱金属原子; M 2表示碱土金属原子或锌原子; R 2表示例如氢原子; m表示1〜4的整数， n表示0〜3的整数， 并且在非质子极性溶剂的存在下，m和n的和为4]，以及路易斯酸如选自例如硼，镁和铝的原子的卤化物。

    METHOD OF SCREENING DRUG ACTING ON CELL WALL
    4.
    发明公开
    METHOD OF SCREENING DRUG ACTING ON CELL WALL 有权
    一种筛选对细胞壁活性药物物质

    公开(公告)号：EP1283261A4

    公开(公告)日：2006-09-06

    申请号：EP01925961

    申请日：2001-04-26

    申请人： DAIICHI SEIYAKU CO

    发明人： KITAMURA AKIHIRO ,  SOMEYA KAZUHIKO ,  NAKAJIMA RYOHEI

    IPC分类号： C12N1/19 ,  C12Q1/02 ,  C12Q1/18 ,  C12N15/09

    CPC分类号： C12Q1/18 ,  C12Q1/025 ,  G01N2500/00

    摘要： A method of screening a drug acting on cell wall which involves: (1) the step of incubating microorganisms, in which a reporter protein is fixed as GPI anchor protein respectively to the cell wall and the cell membrane, in the presence of a test substance; (2) the step of assaying the reporter protein released in the cultures of the above microorganisms; and (3) the step of judging the test substance as a drug having a selective inhibitory action on the cell wall, in case where the reporter protein is released into the culture of the microorganism having the reporter protein fixed to the cell wall but not substantially released into the culture of the other microorganism having the reporter protein fixed to the cell membrane.

    PARTICULATE PRODUCT COMPRISING PANTETHINE
    7.
    发明公开
    PARTICULATE PRODUCT COMPRISING PANTETHINE 有权
    PANTETHIN坚持TEILCHENF RMIGES PRODUKT

    公开(公告)号：EP1547584A4

    公开(公告)日：2005-12-14

    申请号：EP03798538

    申请日：2003-09-29

    申请人： DAIICHI SEIYAKU CO

    发明人： KIDOKORO M ,  TSUTSUMI Y ,  NADA MITSUMASA

    IPC分类号： A61K9/16 ,  A61K9/20 ,  A61K31/145 ,  A61K31/16 ,  A61K47/04 ,  A61P3/00 ,  A61P43/00

    CPC分类号： A61K31/145 ,  A61K9/1611 ,  A61K9/1652 ,  A61K9/2009 ,  A61K9/2054 ,  A61K31/16

    摘要： A particulate product which contains pantethine, a light silicic anhydride and a crystalline cellulose, wherein it contains the light silicic anhydride and the crystalline cellulose in a total amount such that provides an adsorptive capability of 0.6 or more. The particulate product comprising pantethine is excellent in fluidity, is free from problems such as blocking or the like, has particle diameters suitable for handling and exhibits good storage stability.

    摘要翻译： 含有泛胺，轻质无水硅酸和微晶纤维素的微粒，其中微晶纤维素的轻质无水硅酸的总含量达到0.6或更高的吸附性的量。 本发明的含有甜胺的颗粒具有良好的流动性和足够的颗粒尺寸，提供优异的操作性能。 它没有障碍物，如堵塞，并具有良好的储存稳定性。

    CRYSTALS OF TAXANE DERIVATIVE AND PROCESS FOR THEIR PRODUCTION
    8.
    发明公开
    CRYSTALS OF TAXANE DERIVATIVE AND PROCESS FOR THEIR PRODUCTION 有权
    紫杉烷和方法及其晶体

    公开(公告)号：EP1457492A4

    公开(公告)日：2005-03-23

    申请号：EP02785977

    申请日：2002-11-29

    申请人： DAIICHI SEIYAKU CO

    发明人： UCHIDA S ,  TAKAYANAGI Y ,  ONO MAKOTO

    IPC分类号： A61K31/443 ,  A61P35/00 ,  C07D493/04 ,  C07D493/08

    CPC分类号： A61K31/443 ,  C07D493/04

    摘要： Crystals of (1S,2S,3R,4S,5R,8R,9S,10R,13S)-4-acetoxy-2 -benzoyloxy-9,10-[(1S)-2-(dimethylamino)ethylidenedioxy]-5,20-epoxy-1-hydroxytax-11-en-13-yl (2R,3S)-3-(tert-butoxy- carbonylamino)-3-(3-fluoro-2-pyridyl)-2-hydroxypropionate, which exhibit in the powder X-ray diffraction pattern characteristic peaks at diffraction angles (2θ) of 6.2°, 10.3°, 10.7°, 11.4°, and 12.0°; and a process for production of the crystals which comprises the step of conducting crystallization by the use of an organic solvent selected from among ketones, nitriles and mixtures of both or a mixture of the organic solvent with water.

    REMEDIES FOR DISEASES CAUSED BY INSULIN RESISTANCE
    10.
    发明公开
    REMEDIES FOR DISEASES CAUSED BY INSULIN RESISTANCE 审中-公开
    由胰岛素抵抗补救措施引起的疾病

    公开(公告)号：EP1010433A4

    公开(公告)日：2004-09-22

    申请号：EP98944230

    申请日：1998-09-25

    申请人： DAIICHI SEIYAKU CO

    发明人： YAZAKI YOSHIO ,  ASANO TOMOICHIRO ,  KUBO HIDEO ,  KANDA AKIRA

    IPC分类号： A61K38/17 ,  G01N33/15

    CPC分类号： A61K38/17

    摘要： Remedies for diseases caused by insulin resistance which contain as the active ingredient a substance having an activity of inhibiting the binding of the whole insulin receptor substrate-1 (IRS) or insulin receptor substrate-2 (IRS-2) or a part of the same to the whole 14-3-3 protein or a part of the same; and a method of screening remedies for diseases caused by insulin resistance which comprises assaying the above-mentioned binding inhibitory activity. Use of this screening method makes it possible to obtain remedies for various diseases induced by insulin resistance, such as diabetes, diabetic microangiopathies (diabetic nephropathy, diabetic neuropathy and diabetic retinopathy), impaired glucose tolerance, hyperinsulinemia, hyperlipemia, arteriosclerosis, hypertension, obesity, ischemic heart diseases, ischemic brain disorders, peripheral embolism, etc.