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    PYRIDINYLPYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE 7 INHIBITORS
    3.
    发明授权
    PYRIDINYLPYRAZOLOPYRIMIDINONE DERIVATIVES AS PDE 7 INHIBITORS 有权
    作为PDE 7抑制剂的吡啶基吡唑并嘧啶酮衍生物

    公开(公告)号：EP1636235B1

    公开(公告)日：2009-10-14

    申请号：EP04736704.0

    申请日：2004-06-11

    申请人： Asubio Pharma Co., Ltd.

    发明人： INOUE, Hidekazu ,  MURAFUJI, Hidenobu ,  HAYASHI, Yasuhiro

    IPC分类号： C07D487/04 ,  C07D519/00 ,  A61K31/519 ,  A61P29/00 ,  A61P37/00

    CPC分类号： C07D487/04

    摘要： To provide the compounds inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic disease, inflammatory disease or immunologic disease. The compound is pyridinylpyrazolopyrimidinone compound represented by the following formula (IA) or (IB): especially, R1 is cyclohexyl or cycloheptyl group, R2 is methyl; R3 is a group: -NR5R6 or -S(O)0-2R8; hydrogen atom; nitro group; cyano group; a halogen atom; heteroaryl group; and R4 is methoxy or ethoxy group.

    摘要翻译： 为了提供选择性抑制PDE7的化合物，并因此提高细胞cAMP水平。 因此，该化合物可用于治疗各种疾病，如过敏性疾病，炎性疾病或免疫性疾病。 该化合物为由下式（IA）或（IB）表示的吡啶基吡唑并嘧啶酮化合物：特别地，R 1为环己基或环庚基，R 2为甲基; R3是基团：-NR5R6或-S（O）0-2R8; 氢原子; 硝基; 氰基; 卤素原子; 杂芳基; 和R4是甲氧基或乙氧基。

    THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY
    4.
    发明公开
    THIENOPYRAZOLE DERIVATIVE HAVING PDE7 INHIBITORY ACTIVITY 有权
    THIENOPYRAZOLDERIVAT MIT PDE7-HEMMENDER WIRKUNG

    公开(公告)号：EP1775298A4

    公开(公告)日：2009-07-01

    申请号：EP05765241

    申请日：2005-07-01

    申请人： ASUBIO PHARMA CO LTD

    发明人： INOUE H ,  MURAFUJI H ,  HAYASHI Y

    IPC分类号： C07D495/04 ,  A61K31/4162 ,  A61P37/00 ,  C07D519/00

    CPC分类号： C07D231/18 ,  C07D495/04

    摘要： A thienopyrazole derivative represented by the following formula (I): [wherein preferably, R1 is cyclohexyl, cycloheptyl, or tetrahydropyranyl; R2 is methyl; R3 is hydrogen; and R4 is -CONR5R6 (wherein either of R5 and R6 is hydrogen)]. It has selective inhibitory activity against PDE7 and thus heightens the intracellular cAMP level to inhibit the activation of T cells. The derivative is hence useful in the prevention and treatment of various allergic diseases and inflammatory/immunologic diseases.

    摘要翻译： 由下式（I）表示的噻吩并吡唑衍生物：[其中优选R1为环己基，环庚基或四氢吡喃基; R2是甲基; R3是氢; 并且R 4是-CONR 5 R 6（其中R 5和R 6中的任一个是氢）]。 它对PDE7具有选择性抑制活性，因此增加了细胞内cAMP水平以抑制T细胞的活化。 因此该衍生物可用于预防和治疗各种过敏性疾病和炎性/免疫性疾病。

    GLYCOLIPID DERIVATIVE AND THERAPEUTIC AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT
    7.
    发明公开
    GLYCOLIPID DERIVATIVE AND THERAPEUTIC AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT 审中-公开
    GLYKOLIPIDDERIVAT UND THERAPEUTISCHES MITTEL，DAS DIESES ALS WIRKSTOFFENTHÄLT

    公开(公告)号：EP1905766A1

    公开(公告)日：2008-04-02

    申请号：EP06780844.4

    申请日：2006-06-30

    申请人： Japan as represented by President of National Center of Neurology and Psychiatry ,  Asubio Pharma Co., Ltd.

    发明人： MIYAKE, Sachiko ,  YAMAMURA, Takashi ,  TOBA, Tetsuya

    IPC分类号： C07D309/10

    CPC分类号： C07D319/06 ,  C07D317/20 ,  C07D317/26 ,  C07D317/28

    摘要： Glycolipid derivatives having the formula (I):

    wherein R 1 indicates an aldopyranose residue, R 2 indicates a hydrogen atom or hydroxyl group, A indicates -CH 2 -, - CH(OH)-CH 2 - or -CH=CHCH 2 -, Z indicates -O- or -CH 2 -, when Z is -O- and x is an integer of 4 to 16, y indicates an integer of 26 to 35, when Z is -O- and x indicates an integer of 17 to 25, y indicates an integer of 0 to 35, when Z is -CH 2 - and x indicates an integer of 4 to 15, y indicates an integer of 26 to 35, and when Z is -CH 2 - and x indicates an integer of 16 to 25, y indicates an integer of 0 to 35 and a drug containing the glycolipid derivative for treatment of autoimmune arthritis and other autoimmune disease, bronchial asthma and other allergic diseases or diseases in which NKT cells or stimulation of NKT cells is known to be participating in the deterioration of conditions.

    摘要翻译： 具有式（I）的糖脂衍生物：其中R 1表示吡喃葡萄糖残基，R 2表示氢原子或羟基，A表示-CH 2 - ， - CH（OH）-CH 2 - 或-CH = CHCH 2 - ，Z表示-O-或-CH 2 - ，当Z为-O-，x为4〜16的整数时，y为26〜35的整数，Z为-O-，x为17的整数时 至25，y表示0〜35的整数，当Z为-CH 2 - ，x表示4〜15的整数时，y表示26〜35的整数，Z表示-CH 2 - ，x表示 16〜25的整数，y表示0〜35的整数，含有用于治疗自身免疫性关节炎和其他自身免疫性疾病，其他自身免疫性疾病或其他过敏性疾病或其中已知NKT细胞或NKT细胞刺激的过敏性疾病或疾病的药物 参与条件的恶化。

    AGENT FOR IMPROVEMENT OF INSULIN RESISTANCE
    8.
    发明公开
    AGENT FOR IMPROVEMENT OF INSULIN RESISTANCE 审中-公开
    促进胰岛素抵抗的代理商

    公开(公告)号：EP1886692A1

    公开(公告)日：2008-02-13

    申请号：EP06746919.7

    申请日：2006-05-26

    申请人： Asubio Pharma Co., Ltd.

    发明人： WAKABAYASHI, Naomi BioPharma Center, ASUBIO PHARMA CO., ltd. ,  HARADA, Yuriko ,  MASUDA, Yutaka BioPharma Center, ASUBIO PHARMA CO., ltd.

    IPC分类号： A61K45/00 ,  A61K38/04 ,  A61K38/22 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12

    CPC分类号： A61K9/0043 ,  A61K9/0019 ,  A61K9/0073 ,  A61K38/26

    摘要： A novel dosage regimen of GLP-1 receptor agonists causes little or no side effects or drug interactions and is suitable for improving insulin resistance. Also provided is an insulin resistance improver for use in the dosage regimen. The dosage regimen comprises repeatedly administering, preferably in a non-invasive manner, a GLP-1 receptor agonist at least before eating for a predetermined period of time to create a condition similar to what is observed with postprandial temporary secretion of the endogenous GLP-1 receptor agonist, rather than administering it continuously. This creates a similar or enhanced variation in the plasma levels of GLP-1 receptor agonist as compared to the circadian variation of the endogenous GLP-1 receptor agonist in a healthy individual. A pharmaceutical composition for use in the dosage regimen containing GLP-1 receptor agonist as an active ingredient is also provided.

    摘要翻译： GLP-1受体激动剂的新剂量方案几乎不引起副作用或药物相互作用，并且适用于改善胰岛素抵抗。 还提供了用于剂量方案中的胰岛素抵抗改善剂。 给药方案包括至少在进食预定时间段之前，优选以非侵入方式重复施用GLP-1受体激动剂，以产生与用餐后暂时分泌内源性GLP-1所观察到的相似的状况 受体激动剂，而不是连续给药。 与健康个体中内源性GLP-1受体激动剂的昼夜节律变化相比，这会在GLP-1受体激动剂的血浆水平上产生相似或增强的变化。 还提供了用于含有GLP-1受体激动剂作为活性成分的剂量方案中的药物组合物。

    PROCESS FOR PRODUCING PEPTIDE WITH THE USE OF ACCESSORY PEPTIDE
    10.
    发明授权
    PROCESS FOR PRODUCING PEPTIDE WITH THE USE OF ACCESSORY PEPTIDE 有权
    用于生产救济肽肽借助于

    公开(公告)号：EP0978565B1

    公开(公告)日：2007-10-10

    申请号：EP99901926.8

    申请日：1999-01-29

    申请人： Asubio Pharma Co., Ltd.

    发明人： OHSUYE, Kazuhiro ,  YABUTA, Masayuki ,  SUZUKI, Yuji

    IPC分类号： C12N15/62 ,  C12P21/02 ,  C12P21/06 ,  A61K38/28 ,  C12N1/21 ,  C12N5/10 ,  C07K14/605

    CPC分类号： C12N15/62 ,  C07K14/605 ,  C07K2319/50 ,  C07K2319/75

    摘要： A process for producing a peptide having a desired biological activity via gene recombination characterized in that an accessory peptide is added to the target peptide followed by the expression thereof. Use of this process makes it possible to prevent agglutination in the recovery and purification steps with the regulation of isoelectric points, to achieve an elevated yield in ion exchange chromatography, to improve the solubility of a fused protein in an enzymatic reaction wherein the target peptide is expressed as the fused protein with another protein and then liberated by enzymatic cleavage, to improve the solubility of the target peptide in an enzymatic reaction wherein the peptide should be enzymatically modified, etc., thus elevating the purification efficiency and yield of the target protein.