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    • 1. 发明授权
    • Piperidine derivative
    • 哌啶衍生物
    • US08377967B2
    • 2013-02-19
    • US12864878
    • 2008-11-20
    • Kunihiko HigashiuraTakashi OginoTaizo ItoHiroyuki Iwatsuki
    • Kunihiko HigashiuraTakashi OginoTaizo ItoHiroyuki Iwatsuki
    • A61K31/4535C07D409/02A61P37/08
    • C07D495/04C07D409/04C07D497/04
    • 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.
    • 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。
    • 2. 发明申请
    • PIPERIDINE DERIVATIVE
    • 哌啶衍生物
    • US20100331365A1
    • 2010-12-30
    • US12864878
    • 2008-11-20
    • Kunihiko HigashiuraTakashi OginoTaizo ItoHiroyuki Iwatsuki
    • Kunihiko HigashiuraTakashi OginoTaizo ItoHiroyuki Iwatsuki
    • A61K31/4535C07D409/02A61P37/08
    • C07D495/04C07D409/04C07D497/04
    • 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.
    • 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。
    • 3. 发明授权
    • Aminopropylidene derivative
    • 氨基亚丙基衍生物
    • US08653285B2
    • 2014-02-18
    • US13055780
    • 2009-07-31
    • Kunihiko HigashiuraTakashi OginoTaizo ItoKoji KunimasuKazuhito Furukawa
    • Kunihiko HigashiuraTakashi OginoTaizo ItoKoji KunimasuKazuhito Furukawa
    • C07D313/08C07D333/50A61K31/38A61K31/335
    • C07D495/04C07D333/78
    • 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.
    • 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。
    • 8. 发明授权
    • Vulcanizing machine with segmented mold
    • 具有分段模具的硫化机
    • US06292993B1
    • 2001-09-25
    • US09294049
    • 1999-04-19
    • Taizo ItoTomotaka GotoMasami Nagata
    • Taizo ItoTomotaka GotoMasami Nagata
    • B29C3502
    • B29D30/0662B29D30/0629B29D2030/0653Y10T29/49815Y10T29/49826
    • A vulcanizing machine for producing pneumatic tires includes an exchangeable segmented mold comprised of tread mold pieces for defining the outer contour of a tire tread portion, and upper and lower side mold members engaged with the tread mold pieces, for defining the outer contours of the sidewall portions. The tread mold pieces are detachably connected to connector segments which are slidably engaged with a container ring so that vertical movement of the container ring causes radial movement of the connector segments relative to the tread mold pieces. After production of tires of a predetermined size has been completed, the mold is removed from the machine by moving the container ring upwards to disconnect the connector segments from the tread mold pieces, and disconnecting the upper side mold member from a top plate of the machine. Another segmented mold for tires of a different size is incorporated into the machine, by placing and centering the mold relative to the machine, moving the container ring downwards to connect the connector segments to the tread mold pieces, and connecting the top plate to the upper side mold member. The mold can be efficiently exchanged with respect to the machine under a high temperature condition, thereby improving the manufacturing productivity of tires.
    • 一种用于生产充气轮胎的硫化机包括一个可更换的分段模具,其包括用于限定轮胎胎面部分的外轮廓的胎面模具件,以及与胎面模具件接合的上下侧模具构件,用于限定侧壁的外轮廓 部分。 胎面模具可拆卸地连接到与容器环可滑动地接合的连接器部分,使得容器环的垂直运动导致连接器部分相对于胎面模具件的径向移动。 在已经完成了预定尺寸的轮胎的生产之后,通过向上移动容器环从模具中取出模具以将连接器段与胎面模具件断开,并将上侧模具构件与机器的顶板断开 。 通过将模具相对于机器放置和对中而将不同尺寸的轮胎的另一个分段模具并入机器中,向下移动容器环以将连接器部分连接到胎面模具件,并将顶板连接到上部 侧模构件。 可以在高温条件下相对于机器有效地更换模具,从而提高轮胎的制造生产率。