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18 条记录 (耗时 0.023 秒)

    Use of catecholamines and related compounds as anti-angiogenic agents
    1.
    发明授权
    Use of catecholamines and related compounds as anti-angiogenic agents 有权
    使用儿茶酚胺和相关化合物作为抗血管生成剂

    公开(公告)号：US09351947B2

    公开(公告)日：2016-05-31

    申请号：US12448981

    申请日：2008-01-29

    申请人： Yasuo Konishi ,  Joanne Magoon ,  Suwatchai Jarussophon

    发明人： Yasuo Konishi ,  Joanne Magoon ,  Suwatchai Jarussophon

    IPC分类号： A61K31/137 ,  A61K31/216 ,  A61K31/222 ,  A61K31/36 ,  A61K31/445 ,  A61K31/495 ,  A61K31/522

    CPC分类号： A61K31/137 ,  A61K9/0048 ,  A61K31/216 ,  A61K31/222 ,  A61K31/36 ,  A61K31/445 ,  A61K31/495 ,  A61K31/522

    摘要： A catecholamine or related compound having (S)-configuration at β-carbon, a physiologically tolerated salt thereof, a prodrug thereof, a physiologically functional derivative thereof or any mixture thereof and having a lipophilicity greater than (S)-noradrenaline has use as an anti-angiogenic agent. A catecholamine or related compound in which a β-hydroxy group has been modified are also anti-angiogenic. The anti-angiogenic agent is preferably a compound of formula (I) or (II) a physiologically tolerated salt thereof, a prodrug thereof, a physiologically functional derivative thereof or any mixture thereof.

    摘要翻译： 具有（S）构型的碳原子数为1〜8的碳原子数为1〜4的烷氧基苯基或其相应的化合物，其生理学上可接受的盐，其前体药物，其生理功能衍生物或其任何混合物的亲油性大于（S） - 非 - 抗血管生成剂。 已经修饰了＆bgr-羟基的儿茶酚胺或相关化合物也是抗血管生成的。 抗血管生成剂优选为式（I）或（II）的化合物，其生理学上耐受的盐，其前药，其生理功能衍生物或其任何混合物。

    Brake control device for a vehicle
    3.
    发明授权
    Brake control device for a vehicle 失效

    公开(公告)号：US06585332B2

    公开(公告)日：2003-07-01

    申请号：US09986736

    申请日：2001-11-09

    申请人： Akihito Kusano ,  Yasuo Konishi ,  Junji Ishimura

    发明人： Akihito Kusano ,  Yasuo Konishi ,  Junji Ishimura

    IPC分类号： B60T834

    CPC分类号： B60T8/4081 ,  B60T7/042 ,  B60T13/686

    摘要： A brake control device for a vehicle includes a master cylinder generating a master cylinder hydraulic pressure in response to a brake pedal depressing force, a wheel cylinder connected with the master cylinder via a hydraulic conduit, a stroke simulator connected to a branch hydraulic conduit branching from the hydraulic conduit, a first solenoid valve connecting or disconnecting the master cylinder with the wheel cylinder and disposed at the hydraulic conduit between a branch portion where the branch hydraulic conduit branches from the hydraulic conduit and the wheel cylinder, a second solenoid valve connecting or disconnecting the master cylinder with the stroke simulator, a pressure controlling mechanism having a pressure source and connected at a portion of the hydraulic circuit between the first solenoid valve and the wheel cylinder, and a controller for controlling the pressure controlling mechanism, the first solenoid valve and the second solenoid valve.

    Bivalent thrombin inhibitors
    4.
    发明授权
    Bivalent thrombin inhibitors 失效
    二价凝血酶抑制剂

    公开(公告)号：US6127337A

    公开(公告)日：2000-10-03

    申请号：US636698

    申请日：1996-06-28

    申请人： Yasuo Konishi ,  Zbigniew Szewczuk ,  Yuko Tsuda

    发明人： Yasuo Konishi ,  Zbigniew Szewczuk ,  Yuko Tsuda

    IPC分类号： A61K38/00 ,  C07K14/815 ,  A61K38/03 ,  C07K7/00

    CPC分类号： C07K14/815 ,  A61K38/00

    摘要： Hirudin is the most potent and specific thrombin inhibitor and is derived from the medicinal leech. It is reported to inhibit thrombin with an equilibrium dissociation constant (K.sub.i) value of 2.2.times.10.sup.-14 M. synthetic thrombin inhibitors have been designed based on the hirudin sequence but with a dramatically reduced size. The bulky active site inhibitor segment, hirudin.sup.1-48, has been substituted by small non-substrate type active site inhibitors of thrombin, e.g., dansyl-Arg-(D-pipecolic acid). The linker segment has also been modified using a combination of .omega.-amino acids to reduce the molecular weight but retaining sufficient length to span the two principal binding domains. Among the inhibitors designed, dansyl-Arg-(D-pipecolic acid)-(12-aminododecanoic acid)-4-aminobutyric acid)-Asp-Tyr-Glu-Pro-Ile-Pro-Glu-Glu-Ala-(L-.beta.-cyclohexylalamine)-(D-Glu)-OH (SEQ ID NO:45) showed the highest affinity and displays a competitive-type inhibition. The incorporation of the non-substrate type active site inhibitor segment and the linker of .omega.-amino acids into the bivalent thrombin inhibitors not only improved in vitro thrombin inhibitory activity to the pM level, overcame proteolytic susceptibility at the level of the "normal" scissile bond and confered high in vivo activity.

    摘要翻译： PCT No.PCT / CA94 / 00585 Sec。 371日期：1996年6月28日 102（e）日期1996年6月28日PCT 1994年10月25日PCT PCT。 第WO95 / 11921号公报 日期1995年5月4日水蛭素是最有效和特异性的凝血酶抑制剂，来源于药用水蛭。 据报道，以平均解离常数（Ki）值为2.2×10-14 M抑制凝血酶。已经基于水蛭素序列设计合成的凝血酶抑制剂，但其显着减小的大小。 大体积的活性位点抑制物片段，水蛭素1-48已经被小的非底物型的凝血酶活性位点抑制剂例如丹磺酰-Arg-（D-哌啶酸）所取代。 接头片段也已经使用ω-氨基酸的组合进行了修饰，以降低分子量，但保留足够的长度来跨越两个主要的结合结构域。 在设计的抑制剂中，丹磺酰-Arg-（D-哌啶酸） - （12-氨基十二烷酸）-4-氨基丁酸）-Asp-Tyr-Glu-Pro-Ile-Pro-Glu-Glu-Ala-（L- β-环己胺） - （D-Glu）-OH（SEQ ID NO：45）显示出最高的亲和力并显示出竞争性抑制。 将非底物型活性位点抑制物区段和ω-氨基酸接头加入到二价凝血酶抑制剂中不仅提高了对pM水平的体外凝血酶抑制活性，克服了在“正常”剪切水平下的蛋白水解敏感性 结合并提出高体内活性。

    Brake control device for a vehicle
    7.
    发明授权
    Brake control device for a vehicle 有权
    车辆制动控制装置

    公开(公告)号：US06685278B2

    公开(公告)日：2004-02-03

    申请号：US09842849

    申请日：2001-04-27

    申请人： Akihito Kusano ,  Yasuo Konishi ,  Junji Ishimura

    发明人： Akihito Kusano ,  Yasuo Konishi ,  Junji Ishimura

    IPC分类号： B60T834

    CPC分类号： B60T8/4081 ,  B60T7/042 ,  B60T13/662 ,  B60T13/686

    摘要： A brake control device for a vehicle includes a master cylinder, a wheel cylinder, a brake pedal behavior simulator, a normally-open type electromagnetic valve, a normally-closed type electromagnetic valve, and a brake pressure control device. The brake pressure control device includes a pump, a reservoir, and two electromagnetic valves to increase and decrease wheel cylinder hydraulic pressure. When the brake pressure control device is normally operated, a hydraulic pressure in the wheel cylinder is controlled by the brake pressure control device. On the other hand, when the brake pressure control device malfunctions or is abnormally operating, the wheel cylinder hydraulic pressure is controlled by hydraulic pressure generated from the master cylinder. At least the normally-closed type electromagnetic valve is opened when the brake pedal is in the non-operational state.

    摘要翻译： 车辆的制动控制装置包括主缸，轮缸，制动踏板行为模拟器，常开型电磁阀，常闭型电磁阀和制动压力控制装置。 制动压力控制装置包括泵，储存器和两个电磁阀，以增加和减少轮缸液压。 当制动压力控制装置正常工作时，通过制动压力控制装置控制轮缸中的液压。 另一方面，当制动压力控制装置发生故障或异常动作时，通过从主缸产生的液压来控制轮缸液压。 当制动踏板处于非操作状态时，至少常闭型电磁阀打开。

    Spool valve device
    9.
    发明授权
    Spool valve device 失效
    阀芯阀装置

    公开(公告)号：US06776191B2

    公开(公告)日：2004-08-17

    申请号：US10124299

    申请日：2002-04-18

    申请人： Norihiro Nakamura ,  Yasuo Konishi ,  Hitoshi Ikeuchi

    发明人： Norihiro Nakamura ,  Yasuo Konishi ,  Hitoshi Ikeuchi

    IPC分类号： F15B1304

    CPC分类号： F16K11/0716 ,  F16K11/0708 ,  Y10T137/8671

    摘要： A spool valve includes a sleeve and a spool. The sleeve has a first communicating hole opening into the cylinder bore and a second communicating hole opening into the cylinder bore and separated from the first communicating hole in the axial direction of the cylinder bore. The spool is fluidtightly accommodated in the cylinder bore to slide and has one end portion which opens and closes the first communicating hole upon sliding operation thereof and the another end portion which opens and closes the second communicating hole upon sliding operation thereof. At least one of the end portions has an end surface extending from the outer circumference approximately at a right angle to the spool axis and an inclined surface which progressively decreases a diameter of the spool from the end surface.

    摘要翻译： 滑阀包括套筒和阀芯。 所述套筒具有通向所述气缸孔的第一连通孔和通向所述气缸孔的第二连通孔，并且在所述气缸孔的轴向方向上与所述第一连通孔分离。 阀芯流体密封地容纳在气缸孔中以滑动，并且具有在滑动操作时打开和关闭第一连通孔的一个端部和在滑动操作时打开和关闭第二连通孔的另一端部。 至少一个端部具有从外周大致与卷轴轴线成直角延伸的端面和从端面逐渐减小卷轴直径的倾斜面。

    Method of folding somatotropins
    10.
    发明授权
    Method of folding somatotropins 失效
    生长激素的折叠方法

    公开(公告)号：US4975529A

    公开(公告)日：1990-12-04

    申请号：US395830

    申请日：1989-08-18

    申请人： Ronald B. Frazier ,  Yasuo Konishi

    发明人： Ronald B. Frazier ,  Yasuo Konishi

    IPC分类号： C07K1/113 ,  C07K14/61 ,  C12N15/18

    CPC分类号： C07K1/1136 ,  C07K14/61

    摘要： A method of recovering biologically active somatotropins which are produced as insoluble refractile bodies in transformed microorganisms which comprises dissolving refractile bodies in a denaturant and 2-amino-2-methyl-1-propanol, homogenizing, and diluting to fold.

    摘要翻译： 回收在转化的微生物中作为不溶性折射体产生的生物活性生长激素的方法，其包括将折射体溶解在变性剂和2-氨基-2-甲基-1-丙醇中，均化和稀释至折叠。