Inhibitor of protein modification products formation
    1.
    发明授权
    Inhibitor of protein modification products formation 失效
    抑制蛋白质改性产物的形成

    公开(公告)号:US07645882B2

    公开(公告)日:2010-01-12

    申请号:US10581255

    申请日:2004-12-03

    摘要: To provide a inhibitor of protein modification products formation capable of inhibiting of vitamin B6 deficiency disease as a side effect, especially a renal protective agent.There is provided a use, as an active ingredient, of any of free or salt-form compounds of either of the formulae: (I) (II) [wherein R1 is substituted or unsubstituted aromatic ring; and each of R2, R3 and R4 is a hydrogen atom or monovalent organic group, or alternatively R2 and R3 cooperate to form a condensed ring or R3 and R4 cooperate to represent a divalent organic group, provided that R3 and R4 are not simultaneously hydrogen atoms].

    摘要翻译: 提供能够抑制维生素B6缺乏症作为副作用的蛋白质修饰产物形成抑制剂,特别是肾保护剂。 提供以下任一式的任何游离或盐形式的化合物作为活性成分的用途:(I)(II)[其中R 1是取代或未取代的芳环; R 2,R 3和R 4各自为氢原子或一价有机基团,或者R 2和R 3相互配位以形成稠合环,或者R 3和R 4相互配位以表示二价有机基团,条件是R 3和R 4不同时为氢原子 ]。

    Modified-protein formation inhibitor
    2.
    发明申请
    Modified-protein formation inhibitor 审中-公开
    修饰蛋白形成抑制剂

    公开(公告)号:US20070161691A1

    公开(公告)日:2007-07-12

    申请号:US10580465

    申请日:2004-11-19

    IPC分类号: A61K31/41 C07D257/04

    CPC分类号: C07D257/04 A61M1/287

    摘要: [PROBLEMS] To provide a inhibitor of protein modification products formation that exibits intense and excellent protein modification products formation inhibiting effects without causing any blood pressure drop. [MEANS FOR SOLVING PROBLEMS] There is provided a inhibitor of protein modification products formation comprising as an active ingredient a compound consisting of a tetrazole ring having, via methylene, various substituents, especially compound (I) or (II) of the following formula: (wherein R1 and R2 represent monovalent organic groups identical with or different from each other). This inhibitor of protein modification products formation is useful in the prevention and treatment of diseases associated with AGEs and ALEs, for example, used as a renal tissue protectant alone or in mixture in a peritoneal dialyzing solution or hemodialysate.

    摘要翻译: [问题]提供蛋白质修饰产物形成的抑制剂,其在不引起任何血压降低的情况下发挥强烈和优异的蛋白质改性产物形成抑制作用。 提供了一种蛋白质修饰产物形成抑制剂,其包含具有通过亚甲基,各种取代基,特别是下式的化合物(I)或(II)的四唑环作为活性成分的化合物: (其中R1和R2表示彼此相同或不同的一价有机基团)。 这种蛋白质修饰产物形成抑制剂可用于预防和治疗与AGEs和ALE相关的疾病,例如单独用作肾组织保护剂或在腹膜透析溶液或血液透析液中混合使用。

    Inhibitor of protein modification products formation
    4.
    发明申请
    Inhibitor of protein modification products formation 失效
    抑制蛋白质改性产物的形成

    公开(公告)号:US20070123577A1

    公开(公告)日:2007-05-31

    申请号:US10581255

    申请日:2004-12-03

    IPC分类号: A61K31/4152

    摘要: [PROBLEMS] To provide a inhibitor of protein modification products formation capable of inhibiting of vitamin B6 deficiency disease as a side effect, especially a renal protective agent. [MEANS FOR SOLVING PROBLEMS] There is provided a use, as an active ingredient, of any of free or salt-form compounds of either of the formulae: (I) (II) [wherein R1 is substituted or unsubstituted aromatic ring; and each of R2, R3 and R4 is a hydrogen atom or monovalent organic group, or alternatively R2 and R3 cooperate to form a condensed ring or R3 and R4 cooperate to represent a divalent organic group, provided that R3 and R4 are not simulataneously hydrogen atoms].

    摘要翻译: [问题]提供能够抑制维生素B6缺乏症作为副作用的蛋白质修饰产物形成抑制剂,特别是肾保护剂。 解决问题的手段作为活性成分,可提供以下任一式的任意一种游离盐或盐形式的化合物:(I)(II)[其中R 1为取代或未取代的芳环; R 2,R 3和R 4各自为氢原子或一价有机基团,或者R 2和R 3相互配位以形成稠合环,或者R 3和R 4合作表示二价有机基团,条件是R 3和R 4不是同时氢原子 ]。

    Megsin/Rage/Inos-Overexpressing Renal Disease Model Animals and Methods for Evaluating Compounds Using the Model Animals
    6.
    发明申请
    Megsin/Rage/Inos-Overexpressing Renal Disease Model Animals and Methods for Evaluating Compounds Using the Model Animals 审中-公开
    Megsin / Rage / Inos过表达肾脏疾病模型动物和使用模型动物评价化合物的方法

    公开(公告)号:US20080263683A1

    公开(公告)日:2008-10-23

    申请号:US10582655

    申请日:2004-12-09

    IPC分类号: A01K67/027

    摘要: Triple Tg (megsin/RAGE/iNOS-Tg) was created by crossing megsin-Tg with RAGE/iNOS-Tg. The megsin/RAGE/iNOS-Tg develops marked pathologies of diabetic nephropathy unfound in conventional models at early stages, and various pathological conditions such as glomerular hypertrophy were observed uniformly in the megsin/RAGE/iNOS-Tg mice. In addition, it was also found that animals exhibiting these symptoms were useful as a disease model animal for diabetic nephropathy. Specifically, the disease model animals of the present invention overexpress the megsin gene, a gene encoding the receptor for advanced glycation end-products, and an inducible nitric oxide synthase gene. As a result, accompanying kidney function disorders of glomerular failure develop at early stages.

    摘要翻译: 通过将megsin-Tg与RAGE / iNOS-Tg交叉产生三重Tg(megsin / RAGE / iNOS-Tg)。 megsin / RAGE / iNOS-Tg在早期常规模型中未发现糖尿病肾病的明显病理,并且在megsin / RAGE / iNOS-Tg小鼠中均匀地观察到各种病理状况如肾小球肥大。 此外,还发现表现出这些症状的动物可用作糖尿病性肾病的疾病模型动物。 具体地,本发明的疾病模型动物过表达megsin基因,编码晚期糖基化终产物的受体的基因和诱导型一氧化氮合酶基因。 结果伴随肾功能障碍的肾小球衰竭发展在早期阶段。

    Impact sensor and manufacturing method therefor
    7.
    发明授权
    Impact sensor and manufacturing method therefor 失效
    冲击传感器及其制造方法

    公开(公告)号:US5773720A

    公开(公告)日:1998-06-30

    申请号:US790283

    申请日:1997-01-28

    申请人: Toshio Miyata

    发明人: Toshio Miyata

    摘要: An impact sensor 10 has mounting pins which are strongly fixed to a housing body 11 without having to increase the outside dimensions of the housing body. The impact sensor includes the housing body 11, which has a hollow space 12 for accommodating a sensing mechanism, and a mounting arrangement 17 for fixing the housing body 11 to a wiring board 13. The mounting arrangement 17 includes a first pin portion 17a, a second pin portion 17b extending from the first pin portion at right angles with the longitudinal direction thereof, and a third pin portion 17c extending from the first pin portion 17a in the opposite direction from the extending direction of the second pin portion. On each side of the housing body 11, a press-fit recess 16 is formed into which the first and second pin portions 17a and 17b are press-fitted. The housing body 11 is fixed to the wiring board 13 by those portions of the third pin portions 17c of the mounting arrangement 17 which protrude from the housing body 11.

    摘要翻译: 撞击传感器10具有牢固地固定到壳体主体11的安装销,而不必增加壳体的外部尺寸。 冲击传感器包括壳体11,其具有用于容纳感测机构的中空空间12,以及用于将壳体11固定到布线板13的安装装置17.安装装置17包括第一销部分17a, 第二销部分17b从第一销部分与其纵向成直角延伸;以及第三销部分17c,其从第一销部分17a沿与第二销部分的延伸方向相反的方向延伸。 在壳体11的每一侧上,形成有压配合凹部16,第一和第二销部分17a和17b被压入其中。 壳体11通过从壳体11突出的安装装置17的第三销部17c的那些部分固定到布线板13。

    ORAL MEDICINAL COMPOSITION FOR PATIENTS UNDERGOING PERITONEAL DIALYSIS AND METHOD FOR USING SAME
    9.
    发明申请
    ORAL MEDICINAL COMPOSITION FOR PATIENTS UNDERGOING PERITONEAL DIALYSIS AND METHOD FOR USING SAME 审中-公开
    腹膜透析患者的口服药物组合物及其使用方法

    公开(公告)号:US20130338574A1

    公开(公告)日:2013-12-19

    申请号:US13811763

    申请日:2011-07-22

    IPC分类号: A61K9/00 A61K31/4412

    摘要: The present invention provides an oral medicinal composition for peritoneal dialysis patients to suppress an increase of carbonyl compounds and/or advanced glycation/lipoxidation end products (AGEs) in the peritoneal cavity and peritoneal tissue after intraperitoneal administration of a glucose-containing peritoneal dialysis fluid, the oral medicinal composition comprising a pharmaceutically acceptable salt of pyridoxamine as an active ingredient.

    摘要翻译: 本发明提供一种腹膜透析患者的口服药物组合物,其用于抑制腹膜内给予含葡萄糖的腹膜透析液后腹膜腔和腹膜组织中羰基化合物和/或晚期糖化/脂氧化终产物(AGEs)的增加, 所述口服药物组合物含有药学上可接受的吡哆胺盐作为活性成分。

    Plasminogen activator inhibitor-1 inhibitor
    10.
    发明授权
    Plasminogen activator inhibitor-1 inhibitor 失效
    纤溶酶原激活物抑制剂-1抑制剂

    公开(公告)号:US07951806B2

    公开(公告)日:2011-05-31

    申请号:US12046547

    申请日:2008-03-12

    摘要: The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof. Each symbol is defined as those in the specification.

    摘要翻译: 本发明涉及纤溶酶原激活物抑制剂-1抑制剂。 本发明还涉及对PAI-1活性具有抑制作用的药物组合物,其可用于预防和治疗与PAI-1活性相关的各种疾病。 此外,本发明涉及由以下通式(I)表示的具有PAI-1抑制活性的新型化合物及其盐。 每个符号被定义为说明书中的符号。