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    Acylamide compounds having secretagogue or inducer activity of adiponectin
    1.
    发明授权
    Acylamide compounds having secretagogue or inducer activity of adiponectin 失效
    具有促分泌素或脂联素诱导活性的酰胺化合物

    公开(公告)号：US07732637B2

    公开(公告)日：2010-06-08

    申请号：US11835029

    申请日：2007-08-07

    申请人： Katsumi Maezono ,  Toshihiko Yoshimura ,  Nozomu Ishida ,  Naoyuki Fukuchi ,  Toshihiro Hatanaka ,  Osamu Ikehara ,  Yayoi Kawato ,  Hideyuki Tanaka

    发明人： Katsumi Maezono ,  Toshihiko Yoshimura ,  Nozomu Ishida ,  Naoyuki Fukuchi ,  Toshihiro Hatanaka ,  Osamu Ikehara ,  Yayoi Kawato ,  Hideyuki Tanaka

    IPC分类号： C07C229/06 ,  A61K31/20

    CPC分类号： C07C233/47 ,  A23L33/10 ,  C07C323/59

    摘要： The present invention provides an acylamide compound of the following formula (1), prodrugs thereof, or pharmaceutically acceptable salts thereof; and an adiponectin inducer or secretagogue, therapeutic agent of metabolic syndromes, therapeutic agent of hypoadiponectinemia, therapeutic agent of hyperlipemia, preventive/therapeutic agent of diabetes, improving agent of impaired glucose tolerance, improving agent of insulin resistance, enhancing agent of insulin sensitivity, therapeutic agent of hypertension, preventive/therapeutic agent of vascular disorders, an anti-inflammatory agent, therapeutic agent of hepatic inflammation, therapeutic agent of fatty liver, therapeutic agent of hepatic fibrosis, therapeutic agent of liver cirrhosis, preventive/therapeutic agent of non-alcoholic/nonviral steatohepatitis (NASH) or non-alcoholic/nonviral fatty liver disease (NAFLD), or therapeutic agent of obesity, each of which has the above compounds as an active ingredient.

    摘要翻译： 本发明提供下式（1）的酰胺化合物，其前体药物或其药学上可接受的盐; 和脂联素诱导剂或促分泌素，代谢综合征的治疗剂，低脂联素血症的治疗剂，高脂血症的治疗剂，糖尿病的预防/治疗剂，葡萄糖耐量降低的改善剂，胰岛素抵抗的改善剂，胰岛素敏感性的增强剂，治疗 高血压药物，血管疾病的预防/治疗剂，抗炎剂，肝脏炎症治疗剂，脂肪肝治疗剂，肝纤维化治疗剂，肝硬化治疗剂，非酒精性预防/治疗剂 /非病毒性脂肪性肝炎（NASH）或非酒精性/非病毒性脂肪性肝病（NAFLD）或肥胖症治疗剂，其各自具有上述化合物作为活性成分。

    ACYLAMIDE COMPOUNDS HAVING SECRETAGOGUE OR INDUCER ACTIVITY OF ADIPONECTIN
    2.
    发明申请
    ACYLAMIDE COMPOUNDS HAVING SECRETAGOGUE OR INDUCER ACTIVITY OF ADIPONECTIN 失效
    具有ADIPONECTIN的秘密活性或诱导活性的酰亚胺化合物

    公开(公告)号：US20070282002A1

    公开(公告)日：2007-12-06

    申请号：US11835029

    申请日：2007-08-07

    申请人： Katsumi MAEZONO ,  Toshihiko Yoshimura ,  Nozomu Ishida ,  Naoyuki Fukuchi ,  Toshihiro Hatanaka ,  Osamu Ikehara ,  Yayoi Kawato ,  Hideyuki Tanaka

    发明人： Katsumi MAEZONO ,  Toshihiko Yoshimura ,  Nozomu Ishida ,  Naoyuki Fukuchi ,  Toshihiro Hatanaka ,  Osamu Ikehara ,  Yayoi Kawato ,  Hideyuki Tanaka

    IPC分类号： A61K31/198 ,  C07C235/12

    CPC分类号： C07C233/47 ,  A23L33/10 ,  C07C323/59

    摘要： The present invention provides an acylamide compound of the following formula (1), prodrugs thereof, or pharmaceutically acceptable salts thereof; and an adiponectin inducer or secretagogue, therapeutic agent of metabolic syndromes, therapeutic agent of hypoadiponectinemia, therapeutic agent of hyperlipemia, preventive/therapeutic agent of diabetes, improving agent of impaired glucose tolerance, improving agent of insulin resistance, enhancing agent of insulin sensitivity, therapeutic agent of hypertension, preventive/therapeutic agent of vascular disorders, an anti-inflammatory agent, therapeutic agent of hepatic inflammation, therapeutic agent of fatty liver, therapeutic agent of hepatic fibrosis, therapeutic agent of liver cirrhosis, preventive/therapeutic agent of non-alcoholic/nonviral steatohepatitis (NASH) or non-alcoholic/nonviral fatty liver disease (NAFLD), or therapeutic agent of obesity, each of which has the above compounds as an active ingredient.

    摘要翻译： 本发明提供下式（1）的酰胺化合物，其前体药物或其药学上可接受的盐; 和脂联素诱导剂或促分泌素，代谢综合征的治疗剂，低脂联素血症的治疗剂，高脂血症的治疗剂，糖尿病的预防/治疗剂，葡萄糖耐量降低的改善剂，胰岛素抵抗的改善剂，胰岛素敏感性的增强剂，治疗 高血压药物，血管疾病的预防/治疗剂，抗炎剂，肝脏炎症治疗剂，脂肪肝治疗剂，肝纤维化治疗剂，肝硬化治疗剂，非酒精性预防/治疗剂 /非病毒性脂肪性肝炎（NASH）或非酒精性/非病毒性脂肪性肝病（NAFLD）或肥胖症治疗剂，其各自具有上述化合物作为活性成分。

    PPAR ACTIVITY REGULATORS
    3.
    发明申请
    PPAR ACTIVITY REGULATORS 失效
    PPAR活性调节剂

    公开(公告)号：US20070276041A1

    公开(公告)日：2007-11-29

    申请号：US11753967

    申请日：2007-05-25

    申请人： Akiko Oonuki ,  Toshihiko Yoshimura ,  Katsumi Maezono ,  Yayoi Kawato ,  Hideyuki Tanaka ,  Naoyuki Fukuchi ,  Nozomu Ishida

    发明人： Akiko Oonuki ,  Toshihiko Yoshimura ,  Katsumi Maezono ,  Yayoi Kawato ,  Hideyuki Tanaka ,  Naoyuki Fukuchi ,  Nozomu Ishida

    IPC分类号： A61K31/198 ,  C07C235/04

    CPC分类号： C07C233/47 ,  C07C233/49 ,  C07C233/52 ,  C07C2601/14

    摘要： The object of the present invention is to provide PPAR (peroxisome proliferator-activated receptor) activity regulators, which can be widely used for improving insulin resistance and preventing/treating various diseases such as diabetes, metabolic syndromes, hyperlipemia, high-blood pressure, vascular disorders, inflammation, hepatitis, fatty liver, liver fibrosis, NASH (non-alcoholic steatohepatitis) and obesity.The present invention provides PPAR activity regulators which comprise an acylamide compound having the specific structure, prodrugs thereof, or pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明的目的是提供PPAR（过氧化物酶体增殖物激活受体）活性调节剂，其可广泛用于改善胰岛素抵抗和预防/治疗各种疾病如糖尿病，代谢综合征，高脂血症，高血压，血管 疾病，炎症，肝炎，脂肪肝，肝纤维化，NASH（非酒精性脂肪性肝炎）和肥胖症。 本发明提供了包含具有特定结构的酰基酰胺化合物，其前药或其药学上可接受的盐的PPAR活性调节剂。

    PPAR activity regulators
    4.
    发明授权
    PPAR activity regulators 失效
    PPAR活性调节剂

    公开(公告)号：US07728158B2

    公开(公告)日：2010-06-01

    申请号：US11753967

    申请日：2007-05-25

    申请人： Akiko Oonuki ,  Toshihiko Yoshimura ,  Katsumi Maezono ,  Yayoi Kawato ,  Hideyuki Tanaka ,  Naoyuki Fukuchi ,  Nozomu Ishida

    发明人： Akiko Oonuki ,  Toshihiko Yoshimura ,  Katsumi Maezono ,  Yayoi Kawato ,  Hideyuki Tanaka ,  Naoyuki Fukuchi ,  Nozomu Ishida

    IPC分类号： C07C233/00 ,  A61K31/195

    CPC分类号： C07C233/47 ,  C07C233/49 ,  C07C233/52 ,  C07C2601/14

    摘要： The object of the present invention is to provide PPAR (peroxisome proliferator-activated receptor) activity regulators, which can be widely used for improving insulin resistance and preventing/treating various diseases such as diabetes, metabolic syndromes, hyperlipemia, high-blood pressure, vascular disorders, inflammation, hepatitis, fatty liver, liver fibrosis, NASH (non-alcoholic steatohepatitis) and obesity.The present invention provides PPAR activity regulators which comprise an acylamide compound having the specific structure, prodrugs thereof, or pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明的目的是提供PPAR（过氧化物酶体增殖物激活受体）活性调节剂，其可广泛用于改善胰岛素抵抗和预防/治疗各种疾病如糖尿病，代谢综合征，高脂血症，高血压，血管 疾病，炎症，肝炎，脂肪肝，肝纤维化，NASH（非酒精性脂肪性肝炎）和肥胖症。 本发明提供了包含具有特定结构的酰基酰胺化合物，其前药或其药学上可接受的盐的PPAR活性调节剂。

    Inhibitors of the GPIb—vWF interaction, their preparation and use
    9.
    发明授权
    Inhibitors of the GPIb—vWF interaction, their preparation and use 有权
    GPIb-vWF相互作用的抑制剂，其制备和使用

    公开(公告)号：US07235558B2

    公开(公告)日：2007-06-26

    申请号：US10454939

    申请日：2003-06-04

    申请人： Otmar Klingler ,  Melitta Just ,  Kuniya Sakurai ,  Naoyuki Fukuchi

    发明人： Otmar Klingler ,  Melitta Just ,  Kuniya Sakurai ,  Naoyuki Fukuchi

    IPC分类号： C07D215/46

    CPC分类号： C07D401/12 ,  C07D215/48 ,  C07D401/14 ,  C07D417/12

    摘要： The present invention relates to compounds of the formula I, in which R1, R2, A, B, D, F, n, m and o have the meanings indicated herein. The compounds of the formula I are valuable pharmacologically active compounds. They are reversible inhibitors of the interaction between the plasma protein von Willebrand factor (vWF) and the blood platelet receptor glycoprotein Ib-IX-V complex (GPIb). They exhibit an antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of atherothrombotic diseases

    摘要翻译： 本发明涉及式Ⅰ化合物，其中R1，R2，A，B，D，F，n，m和o具有本文所述的含义。 式I的化合物是有价值的药理活性化合物。 它们是血浆蛋白血管性血友病因子（vWF）和血小板受体糖蛋白Ib-IX-V复合物（GPIb）之间相互作用的可逆抑制剂。 它们表现出抗血栓形成的作用，例如适用于治疗和预防动脉粥样硬化血栓形成疾病

    Protein having antithrombotic activity and method for producing the same
    10.
    发明授权
    Protein having antithrombotic activity and method for producing the same 失效
    具有抗血栓形成活性的蛋白质及其制造方法

    公开(公告)号：US06710031B2

    公开(公告)日：2004-03-23

    申请号：US09969763

    申请日：2001-10-04

    申请人： Naoyuki Fukuchi ,  Morikazu Kito ,  Takashi Kayahara ,  Fumie Futaki ,  Kohki Ishikawa ,  Eiichiro Suzuki ,  Keiko Gondoh ,  Nobuhisa Shimba ,  Naoyuki Yamada

    发明人： Naoyuki Fukuchi ,  Morikazu Kito ,  Takashi Kayahara ,  Fumie Futaki ,  Kohki Ishikawa ,  Eiichiro Suzuki ,  Keiko Gondoh ,  Nobuhisa Shimba ,  Naoyuki Yamada

    IPC分类号： A61K3846

    CPC分类号： C07K14/46 ,  C07K14/745

    摘要： A method for producing a protein having an antithrombotic activity, which comprises replacing, in a protein that has an amino acid sequence having a homology of not less than 30% to the amino acid sequence of SEQ ID NO: 1 and forms a higher order structure composed of a first &bgr; strand (&bgr;1), a first &agr; helix (&agr;1), a second &agr; helix (&agr;2), a second &bgr; strand (&bgr;2), a loop, a third &bgr; strand (&bgr;3), a fourth &bgr; strand (&bgr;4) and a fifth &bgr; strand (&bgr;5) in this order from the amino terminus, at least one amino acid residue in a region from &agr;2 to &bgr;2 and/or a region from &bgr;3 to &bgr;4 so that electric charge of the amino acid residue is changed towards positive direction.

    摘要翻译： 一种具有抗血栓形成活性的蛋白质的制造方法，其特征在于，具有与SEQ ID NO：1的氨基酸序列具有不小于30％的同源性的氨基酸序列的蛋白质，并形成高级结构 由第一β链（β1），第一α螺旋（alpha1），第二α螺旋（α2），第二β链（β2），环，第三β链（β3），第四条β链 β4）和第五个β链（β5），从氨基末端起始，α2至β2区域和/或β3至β4区域中的至少一个氨基酸残基，使得氨基酸残基的电荷为 转向正向。