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    NOVEL GAMMA-SECRETASE INHIBITOR
    1.
    发明申请
    NOVEL GAMMA-SECRETASE INHIBITOR 失效
    新型GAMMA-SECRETASE抑制剂

    公开(公告)号：US20110071224A1

    公开(公告)日：2011-03-24

    申请号：US12672326

    申请日：2008-07-01

    申请人： Atsuhiro Abe ,  Hideaki Shimizu ,  Seigo Sawada ,  Hiroshi Kodaira

    发明人： Atsuhiro Abe ,  Hideaki Shimizu ,  Seigo Sawada ,  Hiroshi Kodaira

    IPC分类号： A61K31/198 ,  C07C229/28 ,  A61P25/28

    CPC分类号： C07K5/0207 ,  A61K38/00

    摘要： It is intended to provide a novel compound that has an excellent γ-secretase inhibitory effect and specifically inhibits Aβ production.The present invention provides a compound of the following formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a linear or branched alkyl group having 1 to 4 carbon atoms or a phenyl group; R2 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more phenyl or halogenophenyl groups; R3 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more hydroxyl groups; R4 represents a linear or branched alkyl group having 1 to 4 carbon atoms; and the symbol “*” represents a chiral center.

    摘要翻译： 本发明提供具有优异的γ-分泌酶抑制效果并特异性抑制A＆bgr的新型化合物。 生产。 本发明提供下式（1）的化合物或其药学上可接受的盐：其中R1表示具有1-4个碳原子的直链或支链烷基或苯基; R2表示可被一个或多个苯基或卤代苯基取代的具有1至4个碳原子的直链或支链烷基; R3表示可以被一个或多个羟基取代的具有1至4个碳原子的直链或支链烷基; R4代表具有1-4个碳原子的直链或支链烷基; 符号“*”表示手性中心。

    γ-secretase inhibitor
    2.
    发明授权
    γ-secretase inhibitor 失效
    γ-分泌酶抑制剂

    公开(公告)号：US08501813B2

    公开(公告)日：2013-08-06

    申请号：US12672326

    申请日：2008-07-01

    申请人： Atsuhiro Abe ,  Hideaki Shimizu ,  Seigo Sawada ,  Hiroshi Kodaira

    发明人： Atsuhiro Abe ,  Hideaki Shimizu ,  Seigo Sawada ,  Hiroshi Kodaira

    IPC分类号： A01N37/18 ,  A61K31/16 ,  C07C233/00 ,  C07C235/00 ,  C07C237/00 ,  C07C239/00

    CPC分类号： C07K5/0207 ,  A61K38/00

    摘要： It is intended to provide a novel compound that has an excellent γ-secretase inhibitory effect and specifically inhibits Aβ production.The present invention provides a compound of the following formula (1) or a pharmaceutically acceptable salt thereof: wherein R1 represents a linear or branched alkyl group having 1 to 4 carbon atoms or a phenyl group; R2 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more phenyl or halogenophenyl groups; R3 represents a linear or branched alkyl group having 1 to 4 carbon atoms which may be substituted by one or more hydroxyl groups; R4 represents a linear or branched alkyl group having 1 to 4 carbon atoms; and the symbol “*” represents a chiral center.

    摘要翻译： 旨在提供具有优异的γ-分泌酶抑制作用并特异性抑制Abeta产生的新型化合物。 本发明提供下式（1）的化合物或其药学上可接受的盐：其中R1表示具有1-4个碳原子的直链或支链烷基或苯基; R2表示可被一个或多个苯基或卤代苯基取代的具有1至4个碳原子的直链或支链烷基; R3表示可以被一个或多个羟基取代的具有1至4个碳原子的直链或支链烷基; R4代表具有1-4个碳原子的直链或支链烷基; 符号“*”表示手性中心。

    Taxane derivatives and drugs containing the same
    5.
    发明授权
    Taxane derivatives and drugs containing the same 失效
    紫杉烷衍生物和含有相同的药物

    公开(公告)号：US6025385A

    公开(公告)日：2000-02-15

    申请号：US147521

    申请日：1999-01-14

    申请人： Hideaki Shimizu ,  Atsuhiro Abe ,  Takashi Yaegashi ,  Seigo Sawada ,  Hiroshi Nagata

    发明人： Hideaki Shimizu ,  Atsuhiro Abe ,  Takashi Yaegashi ,  Seigo Sawada ,  Hiroshi Nagata

    IPC分类号： C07D305/14 ,  C07D405/12 ,  C07D413/12 ,  C07D413/14 ,  A61K31/335

    CPC分类号： C07D405/12 ,  C07D305/14 ,  C07D413/12 ,  C07D413/14

    摘要： This invention relates to a taxane derivative represented by the following formula (1): wherein at least one of X and Y represents a group --CO--A--B in which A represents a single bond, an alkylenecarbonyl group or the like and B represents a substituted or unsubstituted piperidino group or the like, the other represents a tert-butoxycarbonyl group or the like, and Z represents a hydrogen atom or a triethylenesilyl group, and also to a drug containing the same.This compound has high solubility in water and also has excellent antitumor activities.

    摘要翻译： PCT No.PCT / JP97 / 02431 Sec。 371日期1999年1月14日第 102（e）1999年1月14日PCT PCT 1997年7月14日PCT公布。 出版物WO98 / 02426 日本特开2003-12-04本发明涉及下述式（1）表示的紫杉烷衍生物：其中X和Y中的至少一个表示A表示单键的-CO-AB基团，亚烷基羰基等 B表示取代或未取代的哌啶子基等，另一方表示叔丁氧基羰基等，Z表示氢原子或三亚甲基甲硅烷基，也可以是含有该取代基的药物。 该化合物在水中的溶解度高，抗肿瘤活性也优异。

    Method for preparing polymorphism of irinotecan hydrochloride
    6.
    发明授权
    Method for preparing polymorphism of irinotecan hydrochloride 失效
    盐酸伊立替康多态性的制备方法

    公开(公告)号：US07488825B2

    公开(公告)日：2009-02-10

    申请号：US10546687

    申请日：2004-02-24

    申请人： Hideaki Shimizu ,  Atsuhiro Abe ,  Takashi Yaegashi ,  Seigo Sawada

    发明人： Hideaki Shimizu ,  Atsuhiro Abe ,  Takashi Yaegashi ,  Seigo Sawada

    IPC分类号： C07D491/22

    CPC分类号： C07D491/22

    摘要： A method for preparing a novel crystalline polymorphic irinotecan hydrochloride which is excellent in the solubility in water and reduced in the content of impurities is provided. A method for preparing c-type crystals of irinotecan hydrochloride having diffraction peaks (2θ) at 9.15°, 10.00°, 11.80°, 12.20°, 13.00° and 13.40° in the powder X-ray diffractometry characterized by mixing irinotecan with one or more solvents selected from the group consisting of acetone, acetonitrile and tetrahydrofuran, adding hydrochloric acid, and collecting the formed crystals.

    摘要翻译： 提供了一种制备在水中的溶解性优异且杂质含量降低的新型结晶多晶异氟酸盐酸伊立替康的方法。 在粉末X射线衍射法中，制备在9.15°，10.00°，11.80°，12.20°，13.00°和13.40°具有衍射峰（2θ）的伊立替康盐酸盐的c型晶体的方法，其特征在于将伊立替康与一种或多种 选自丙酮，乙腈和四氢呋喃的溶剂，加入盐酸，收集形成的晶体。

    Taxane derivatives
    7.
    发明授权
    Taxane derivatives 失效
    紫杉烷衍生物

    公开(公告)号：US06268381B1

    公开(公告)日：2001-07-31

    申请号：US09581908

    申请日：2000-06-19

    申请人： Hideaki Shimizu ,  Atsuhiro Abe ,  Takanori Ogawa ,  Hiroshi Nagata ,  Seigo Sawada

    发明人： Hideaki Shimizu ,  Atsuhiro Abe ,  Takanori Ogawa ,  Hiroshi Nagata ,  Seigo Sawada

    IPC分类号： A61K31445

    CPC分类号： C07D405/12 ,  C07D305/14 ,  C07D405/14 ,  C07D407/12

    摘要： The present invention relates to taxane derivatives each represented by the following formula (1): [wherein, A1 represents a group (in which R1 represents H or a (substituted) alkyl group) or a group (in which R2 represents an amino group, a mono- or di-alkylamino group, a piperidino group, a pyrrolidino group or a morpholino group), X represents H, an alkoxycarbonyl group or a benzoyl group, Y represents H or a trialkylsilyl group, A2 represents a furyl group, an alkylfuryl group, an alkyl group or a fluorophenyl group, Ac represents an acetyl group, and Bz represents a benzoyl group] or salts thereof; and drugs containing the same as an active ingredient. These compounds have excellent water solubility and antitumor activity.

    摘要翻译： 本发明涉及各种由下式（1）表示的紫杉烷衍生物：[其中，A1表示基团（其中R1表示H或（取代的（alkyl））烷基）或基团（其中R2表示氨基， 一或二烷基氨基，哌啶子基，吡咯烷子基或吗啉代基），X表示H，烷氧基羰基或苯甲酰基，Y表示H或三烷基甲硅烷基，A2表示呋喃基，烷基 基团，烷基或氟苯基，Ac表示乙酰基，Bz表示苯甲酰基]或其盐; 和含有相同活性成分的药物。这些化合物具有优异的水溶性和抗肿瘤活性。

    Acid addition salt of irinotecan
    8.
    发明授权
    Acid addition salt of irinotecan 有权
    伊立替康的酸加成盐

    公开(公告)号：US07897772B2

    公开(公告)日：2011-03-01

    申请号：US11576356

    申请日：2005-09-29

    申请人： Hideaki Shimizu ,  Miyuki Uchida ,  Seigo Sawada ,  Norimasa Kaneda ,  Tsuneo Matsumoto

    发明人： Hideaki Shimizu ,  Miyuki Uchida ,  Seigo Sawada ,  Norimasa Kaneda ,  Tsuneo Matsumoto

    IPC分类号： C07D401/02

    CPC分类号： C07D491/22

    摘要： The present invention is directed to an irinotecan acid addition salt which is formed through addition of an acid selected from the group consisting of sulfuric acid, nitric acid, phosphoric acid, methanesulfonic acid, citric acid, maleic acid, and succinic acid to irinotecan, to a method for producing the salt, and to a pharmaceutical composition containing the salt. The addition salt requires no heating process during drug preparation and provides an aqueous drug product in which the salt is stably dissolved.

    摘要翻译： 本发明涉及通过向伊立替康中加入选自硫酸，硝酸，磷酸，甲磺酸，柠檬酸，马来酸和琥珀酸的酸形成的伊立替康酸加成盐， 盐的制造方法和含有该盐的药物组合物。 加成盐在药物制备过程中不需要加热过程，并提供其中盐稳定溶解的水性药物产品。

    Acid Addition Salt of Irinotecan
    9.
    发明申请
    Acid Addition Salt of Irinotecan 有权
    伊立替康的酸加成盐

    公开(公告)号：US20070299099A1

    公开(公告)日：2007-12-27

    申请号：US11576356

    申请日：2005-09-29

    申请人： Hideaki Shimizu ,  Miyuki Uchida ,  Seigo Sawada ,  Norimasa Kaneda ,  Tsuneo Matsumoto

    发明人： Hideaki Shimizu ,  Miyuki Uchida ,  Seigo Sawada ,  Norimasa Kaneda ,  Tsuneo Matsumoto

    IPC分类号： A61K31/437 ,  A61P35/00 ,  C07D491/22

    CPC分类号： C07D491/22

    摘要： The present invention is directed to an irinotecan acid addition salt which is formed through addition of an acid selected from the group consisting of sulfuric acid, nitric acid phosphoric acid, methanesulfonic acid, citric acid maleic acid and succinic acid to Irinotecan, to a method for producing the salt, and to a pharmaceutical composition containing the salt. The addition salt requires no heating process during drug preparation and provides an aqueous drug product in which the salt is stably dissolved.

    摘要翻译： 本发明涉及通过向伊立替康中加入选自硫酸，硝酸磷酸，甲磺酸，柠檬酸马来酸和琥珀酸的酸形成的伊立替康酸加成盐， 产生盐，以及含有该盐的药物组合物。 加成盐在药物制备过程中不需要加热过程，并提供其中盐稳定溶解的水性药物产品。

    Storage medium having image processing program stored thereon and image processing apparatus
    10.
    发明授权
    Storage medium having image processing program stored thereon and image processing apparatus 有权
    存储有图像处理程序的存储介质和图像处理装置

    公开(公告)号：US09561442B2

    公开(公告)日：2017-02-07

    申请号：US11898109

    申请日：2007-09-10

    申请人： Hideaki Shimizu

    发明人： Hideaki Shimizu

    IPC分类号： A63F13/00 ,  A63F13/42 ,  A63F13/5258 ,  A63F13/40

    CPC分类号： A63F13/42 ,  A63F13/10 ,  A63F13/5258 ,  A63F2300/6045 ,  A63F2300/646 ,  A63F2300/6684

    摘要： An operation target object in a virtual game space as seen from a virtual camera is displayed on a display device. A moving direction of the operation target object in a virtual space in accordance with a direction represented by direction data based on a direction input by the user is determined based on an exactly upward vector representing a direction of a virtual gravity acting on the position of the operation target object in the virtual space and a direction of the normal in the virtual field at the position. The operation target object is moved in the determined moving direction.

    摘要翻译： 从虚拟摄像机观察的虚拟游戏空间中的操作对象物体被显示在显示装置上。 根据由用户输入的方向根据由方向数据表示的方向的虚拟空间中的操作目标对象的移动方向，基于表示作用在该位置上的虚拟重力的方向的精确向上的向量来确定 虚拟空间中的操作目标对象和该位置的虚拟场中的法线方向。 操作对象物体在确定的移动方向上移动。