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17 条记录 (耗时 0.025 秒)

    Piperidine derivative
    5.
    发明授权
    Piperidine derivative 有权
    哌啶衍生物

    公开(公告)号：US08377967B2

    公开(公告)日：2013-02-19

    申请号：US12864878

    申请日：2008-11-20

    申请人： Kunihiko Higashiura ,  Takashi Ogino ,  Taizo Ito ,  Hiroyuki Iwatsuki

    发明人： Kunihiko Higashiura ,  Takashi Ogino ,  Taizo Ito ,  Hiroyuki Iwatsuki

    IPC分类号： A61K31/4535 ,  C07D409/02 ,  A61P37/08

    CPC分类号： C07D495/04 ,  C07D409/04 ,  C07D497/04

    摘要： The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.

    摘要翻译： 本发明提供了具有优异的组胺受体拮抗作用的化合物哌啶衍生物，其可用作药物组合物，特别是抗组胺药的活性成分。 本发明的哌啶衍生物具有有效的组胺受体拮抗作用。 此外，本发明的化合物即使在小鼠口服给药化合物的脑受体结合试验中也显示低脑转移，因此该化合物具有减轻中枢神经系统中的副作用的优选性质，例如嗜睡。 本发明的哌啶衍生物作为在中枢神经系统中具有较小副作用的新型抗组胺药例如嗜睡是非常有用的。

    Oxepin derivative
    6.
    发明申请
    Oxepin derivative 有权
    奥克辛衍生物

    公开(公告)号：US20100004456A1

    公开(公告)日：2010-01-07

    申请号：US12311215

    申请日：2007-09-27

    申请人： Kunihiko Higashiura ,  Takashi Ogino ,  Kazuhito Furukawa ,  Yuriko Yamazaki

    发明人： Kunihiko Higashiura ,  Takashi Ogino ,  Kazuhito Furukawa ,  Yuriko Yamazaki

    IPC分类号： C07D405/04

    CPC分类号： C07D405/04

    摘要： The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low intracerebral migration even when a mouse that is orally administered with the compound is subjected to an intracerebral receptor binding test, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The oxepin derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.

    摘要翻译： 本发明提供一种化合物，具有优异的组胺受体拮抗作用的氧杂环丁衍生物，其可用作抗组胺药。 本发明的oxepin衍生物具有有效的组胺受体拮抗作用。 此外，本发明的化合物即使经口给予该化合物的小鼠进行脑内受体结合试验，也显示低脑内迁移，使得该化合物具有优选的减轻中枢神经系统副作用的性质，例如 作为嗜睡 本发明的oxepin衍生物作为在中枢神经系统中具有较小副作用的新型抗组胺药如睡意觉是非常有用的。

    Three-dimensional structural activity correlation method
    7.
    发明申请
    Three-dimensional structural activity correlation method 审中-公开
    三维结构活动相关法

    公开(公告)号：US20060080073A1

    公开(公告)日：2006-04-13

    申请号：US10530550

    申请日：2003-10-07

    申请人： Takayuki Kotani ,  Kunihiko Higashiura

    发明人： Takayuki Kotani ,  Kunihiko Higashiura

    IPC分类号： G06G7/58

    CPC分类号： G16C20/30 ,  G16C20/50 ,  G16C20/70

    摘要： A three-dimensional quantitative structure-activity relationship method has process B1 of calculating the coordinates of the respective atoms contained in the plural molecules thus superposed in the virtual space, process B2 of calculating interatomic distances between each atom and other atoms and identifying the shortest interatomic distance among thus calculated interatomic distances and two atoms constituting the shortest interatomic distance; process B3 of deleting the two atoms having the shortest interatomic distance from the three-dimensional space and generating an atom which represents the two atoms in the weighted average coordinates of the two atoms to delete, when the shortest interatomic distance thus calculated is equal to or smaller than a predetermined threshold value; process B4 of returning to the second process B2 after the third process B3 and executing the second process B2 including the atoms formed during the third process B3; and process B5 of terminating the process B when the shortest interatomic distance thus calculated is exceeds the predetermined threshold. This method enables strikingly reducing the memory zone and amount of computation required for 3D QSAR analysis.

    摘要翻译： 三维定量结构 - 活动关系方法具有计算包含在虚拟空间中的多个分子中包含的各个原子的坐标的处理B1，计算每个原子与其它原子之间的原子间距离的处理B2，并且识别最短的原子间 由此计算的原子间距离和构成最短原子间距离的两个原子之间的距离; 从三维空间中删除具有最短原子间距离的两个原子的过程B3，并产生一个表示两个原子的加权平均坐标中要删除的两个原子的原子，当这样计算的最短原子间距离等于或 小于预定阈值; 在第三处理B3之后返回到第二处理B2并且执行包括在第三处理B3期间形成的原子的第二处理B2的处理B4; 以及当这样计算的最短原子间距离超过预定阈值时终止处理B的处理B5。 该方法可显着减少3D QSAR分析所需的存储区和计算量。

    PROCESS FOR PRODUCING THIABENZOAZULENE-PROPIONIC ACID DERIVATIVE
    8.
    发明申请
    PROCESS FOR PRODUCING THIABENZOAZULENE-PROPIONIC ACID DERIVATIVE 失效
    生产噻唑烷 - 丙酸衍生物的方法

    公开(公告)号：US20120123127A1

    公开(公告)日：2012-05-17

    申请号：US13383441

    申请日：2010-07-26

    申请人： Kunihiko Higashiura ,  Taizo Ito ,  Takashi Ogino ,  Taisuke Hasegawa

    发明人： Kunihiko Higashiura ,  Taizo Ito ,  Takashi Ogino ,  Taisuke Hasegawa

    IPC分类号： C07D409/08

    CPC分类号： C07D409/04

    摘要： Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.

    摘要翻译： 公开了可用作抗组胺剂等的有效成分的噻哆烷 - 丙酸衍生物的制造方法。 根据本发明的制造方法，可以制备噻吩并薁类骨架的2位用丙酸取代的噻吩并薁 - 丙酸衍生物。 由此合成的硫代苯并薁丙酸衍生物对组胺H1受体和低脑内转移具有优异的拮抗作用，因此可用作药物组合物如抗组胺剂的活性成分。

    Aminopropylidene derivative
    9.
    发明授权
    Aminopropylidene derivative 有权
    氨基亚丙基衍生物

    公开(公告)号：US08653285B2

    公开(公告)日：2014-02-18

    申请号：US13055780

    申请日：2009-07-31

    申请人： Kunihiko Higashiura ,  Takashi Ogino ,  Taizo Ito ,  Koji Kunimasu ,  Kazuhito Furukawa

    发明人： Kunihiko Higashiura ,  Takashi Ogino ,  Taizo Ito ,  Koji Kunimasu ,  Kazuhito Furukawa

    IPC分类号： C07D313/08 ,  C07D333/50 ,  A61K31/38 ,  A61K31/335

    CPC分类号： C07D495/04 ,  C07D333/78

    摘要： An aminopropylidene derivative having excellent histamine receptor antagonistic action, a compound which is useful as a pharmaceutical composition, especially as an active ingredient, having alleviated side effects in the central nervous system is described. In the aminopropylidene derivative, R1 and R2, which may be identical or different, stand for a hydrogen, a substituted carbonyl, a substituted carbonylalkyl, and acrylic acid, excluding a case where both are hydrogen; R3 and R4, which may be identical or different, stand for hydrogen, an alkyl which may be substituted with phenyl, or the like; A stands for unsubstituted or an oxo; B stands for a carbon or an oxygen; one of X and Y stands for a carbon and the other stands for a sulfur, a broken line part stands for a single bond or a double bond, and a wavy line stands for cis-form and/or trans-form.

    摘要翻译： 描述了具有优异的组胺受体拮抗作用的氨基亚丙基衍生物，可用作药物组合物的化合物，特别是作为活性成分，在中枢神经系统中具有缓解的副作用。 在氨基亚丙基衍生物中，R 1和R 2可以相同或不同，代表氢，取代的羰基，取代的羰基烷基和丙烯酸，不包括两者均为氢的情况; R3和R4可以相同或不同，代表氢，可被苯基取代的烷基等; A代表未取代或氧代; B代表碳或氧; X和Y中的一个代表碳，另一个代表硫，虚线部分代表单键或双键，波浪线代表顺式和/或反式。

    Histidine derivatives
    10.
    发明授权
    Histidine derivatives 有权
    组氨酸衍生物

    公开(公告)号：US08236844B2

    公开(公告)日：2012-08-07

    申请号：US12087591

    申请日：2007-01-23

    申请人： Ko Nakamura ,  Yoshitaka Nakazawa ,  Minoru Kawamura ,  Kunihiko Higashiura ,  Tomoshi Miura

    发明人： Ko Nakamura ,  Yoshitaka Nakazawa ,  Minoru Kawamura ,  Kunihiko Higashiura ,  Tomoshi Miura

    IPC分类号： C07D233/64 ,  A61K31/4172

    CPC分类号： C07D233/64 ,  A61K31/4172

    摘要： A novel histidine derivative represented by the following formula (I), and a pharmaceutically acceptable salt and hydrate thereof, useful as a pharmaceutical agent such as analgesics for the treatment of various kinds of acute or chronic pain diseases and of neuropathic pain diseases: wherein, R1 is hydrogen, alkyl having 1 to 6 carbon(s) or benzyl which may be substituted with alkyl having 1 to 4 carbon(s) or halogen; R2 is hydrogen or alkyl having 1 to 4 carbon(s); R3 and R4 are same or different and each is hydrogen, alkyl having 1 to 4 carbon(s) or phenyl which may be substituted with any one or two of alkyl having 1 to 6 carbon(s), alkoxy having 1 to 6 carbon(s), halogen, trifluoromethyl, nitro and cyano; and R5 is hydrogen or an alkyl group having 1 to 4 carbon(s).

    摘要翻译： 由下式（I）表示的新型组氨酸衍生物及其药学上可接受的盐和水合物，可用作治疗各种急性或慢性疼痛疾病和神经性疼痛疾病的止​​痛药等药剂，其中， R1是氢，具有1至6个碳原子的烷基或可被具有1至4个碳原子的烷基或卤素取代的苄基; R2是氢或具有1至4个碳的烷基; R3和R4相同或不同，各自为氢，可具有1至4个碳的烷基或可被具有1至6个碳的烷基的任何一个或两个的烷基取代的苯基，具有1至6个碳的烷氧基（ s），卤素，三氟甲基，硝基和氰基; 并且R 5是氢或具有1至4个碳的烷基。