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33 条记录 (耗时 0.024 秒)

    Amidine compound
    12.
    发明授权
    Amidine compound 失效
    脒化合物

    公开(公告)号：US4454338A

    公开(公告)日：1984-06-12

    申请号：US300534

    申请日：1981-09-09

    申请人： Setsuro Fujii ,  Toshiyuki Okutome ,  Toyoo Nakayama ,  Takashi Yaegashi ,  Masateru Kurumi

    发明人： Setsuro Fujii ,  Toshiyuki Okutome ,  Toyoo Nakayama ,  Takashi Yaegashi ,  Masateru Kurumi

    IPC分类号： C07C249/02 ,  A61K31/155 ,  C07C257/18 ,  C07C279/18 ,  C07D317/68 ,  C07C101/00 ,  C07C101/48

    CPC分类号： C07D317/68 ,  C07C279/18

    摘要： Amidino compounds represented by the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful antitrypsine, antiplasmin, antikallikrein and antithrombin agents. Having strong anti-C1 (C1r, C1s) activities and an anticomplement activity, they are also useful as anticomplement agents. These amidino compounds are prepared by usual esterification of carboxylic acid compounds represented by the formula ##STR2## with 6-amidino-2-naphthol and, if necessary, can be transformed into pharmaceuticlly acceptable acid addition salts thereof.

    摘要翻译： 由式＆lt; IMAGE＆gt;表示的脒基化合物及其药学上可接受的酸加成盐是新的化合物，可用作强效的抗胰蛋白胨，抗血浆素，抗激肽释放酶和抗凝血酶剂。 具有强大的抗C1（C1＆upbar＆r，C1＆upbar＆s）活性和抗补体活性，它们也可用作抗补体剂。 这些脒基化合物通过将式（ⅩⅧ）代表的羧酸化合物与6-脒基-2-萘酚进行常规的酯化反应来制备，如果需要，可以将其转化成其药学上可接受的酸加成盐。

    Process for producing camptothecin
    13.
    发明授权
    Process for producing camptothecin 失效
    喜树碱的制备方法

    公开(公告)号：US06743918B2

    公开(公告)日：2004-06-01

    申请号：US10239113

    申请日：2002-11-25

    申请人： Takashi Yaegashi ,  Takanori Ogawa ,  Seigo Sawada

    发明人： Takashi Yaegashi ,  Takanori Ogawa ,  Seigo Sawada

    IPC分类号： C07D49112

    CPC分类号： C07D491/22 ,  A61K31/475

    摘要： Problem: A large scale production of camptothecin, which is a starting compound of irinotecan hydrochloride and various camptothecin derivatives, at a low cost and with ease. Solution: A process for preparing camptothecin, characterized in that it comprises the following steps (a) and (b); (a) the step to hydrolyze 9-methoxycamptothecin or a natural material containing 9-methoxycamptothecin; (b) the step to convert 9-hydroxycamptothecin obtained in the step (a) into camptothecin by 9-O—perfluoro-lower-alkylsulfonylation or 9-O—phenyltetrazolylation, followed by hydrogenolysis.

    摘要翻译： 问题：大量生产喜树碱，它是伊立替康盐酸盐和各种喜树碱衍生物的起始化合物，成本低，易于使用。溶液：一种制备喜树碱的方法，其特征在于它包括以下步骤（a）和 （b）;（a）水解9-甲氧基喜树碱或含有9-甲氧基喜树碱的天然物质的步骤;（b）将步骤（a）中得到的9-羟基喜树碱通过9-O-全氟低级 - 烷基磺酰化或9-O-苯基四唑化，然后氢解。

    Phenanthroindolizidine compound and NFκB inhibitor containing same as active ingredient
    14.
    发明授权
    Phenanthroindolizidine compound and NFκB inhibitor containing same as active ingredient 有权
    菲并吲哚哩啶化合物和含有与活性成分相同的NF＆kgr B抑制剂

    公开(公告)号：US09174979B2

    公开(公告)日：2015-11-03

    申请号：US13125698

    申请日：2009-10-23

    申请人： Takashi Ikeda ,  Seigo Sawada ,  Takashi Yaegashi ,  Takeshi Matsuzaki ,  Shusuke Hashimoto ,  Ryuta Yamazaki

    发明人： Takashi Ikeda ,  Seigo Sawada ,  Takashi Yaegashi ,  Takeshi Matsuzaki ,  Shusuke Hashimoto ,  Ryuta Yamazaki

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P29/00 ,  A61P35/00 ,  C07D491/147

    CPC分类号： C07D471/04 ,  C07D491/147

    摘要： A novel compound having an excellent NFκB inhibitory effect is provided and specifically disclosed is a compound represented by the following formula (1) or a salt thereof:wherein, R1 represents a hydrogen atom, a lower alkyl group, a lower alkyloxy group, or a halogen atom;R2 represents a hydroxyl group, or a lower alkyloxy group;R3 represents a hydrogen atom, a lower alkyl group, or a halogen atom;R4 represents a hydrogen atom or a lower alkyloxy group;R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6;R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5;R7 represents a hydrogen atom or a lower alkyl group; andR8 represents a hydrogen atom, a hydroxyl group, an amino group, or a lower alkylcarbonyloxy group (excluding the case where R1, R3, R4 and R7 are hydrogen atoms, R2 and R8 are hydroxyl groups, and R5 and R6 are methoxy groups).

    摘要翻译： 提供了具有优异的NF＆Kgr B抑制效果的新化合物，具体公开了下式（1）表示的化合物或其盐：其中，R1表示氢原子，低级烷基，低级烷氧基， 或卤素原子; R2表示羟基或低级烷氧基; R3表示氢原子，低级烷基或卤素原子; R4表示氢原子或低级烷氧基; R5表示与R6一起形成的与R6或异丙烯二氧基一起形成的氢原子，低级烷氧基，卤素原子，羟基或亚甲二氧基; R6表示与R5一起形成的氢原子，低级烷氧基或亚甲二氧基，或与R5形成的异丙烯二氧基; R7表示氢原子或低级烷基; 并且R 8表示氢原子，羟基，氨基或低级烷基羰基氧基（R 1，R 3，R 4和R 7为氢原子的情况除外，R 2和R 8为羟基，R 5和R 6为甲氧基 ）。

    Taxane derivatives and drugs containing the same
    16.
    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。

    Bicycle wheel rim structure
    18.
    发明授权
    Bicycle wheel rim structure 有权
    自行车轮辋结构

    公开(公告)号：US08978725B2

    公开(公告)日：2015-03-17

    申请号：US13277698

    申请日：2011-10-20

    申请人： Kazuki Koshiyama ,  Hiroshi Fujita ,  Takashi Yaegashi

    发明人： Kazuki Koshiyama ,  Hiroshi Fujita ,  Takashi Yaegashi

    IPC分类号： B60B21/12 ,  B60B21/02 ,  B60B21/06 ,  B60B1/04

    CPC分类号： B60B21/025 ,  B60B1/041 ,  B60B1/044 ,  B60B21/026 ,  B60B21/062 ,  B60B21/12 ,  B60B21/125 ,  B60B2900/112 ,  B60B2900/115 ,  Y10S152/16

    摘要： A bicycle wheel rim structure is provided with a rim, a cap and a tape. The rim includes a first annular side portion, a second annular side portion and an annular bridge portion extending between the first and second annular side portions. The bridge portion has at least one opening. The cap includes a base plate and a projection. The base plate overlies an outer rim surface of the annular bridge portion. The projection extends from the base plate into the at least one opening. The tape is attached to the outer rim surface of the annular bridge portion and overlying the base plate of the cap. The tape is dimensioned to cover an interface between a peripheral edge of the base plate of the cap and the outer rim surface of the annular bridge portion.

    摘要翻译： 自行车轮辋结构设置有轮辋，帽和带。 轮缘包括第一环形侧部，第二环形侧部和在第一和第二环形侧部之间延伸的环形桥部。 桥接部分具有至少一个开口。 盖包括底板和突起。 基板覆盖环形桥部分的外缘表面。 突起从基板延伸到至少一个开口中。 带子附接到环形桥接部分的外缘表面并且覆盖在盖的基板上。 胶带的尺寸设计成覆盖盖的基板的周边边缘和环形桥接部分的外边缘表面之间的界面。

    Phenanthroindolizidine derivative and NFκB inhibitor containing same as active ingredient
    19.
    发明授权
    Phenanthroindolizidine derivative and NFκB inhibitor containing same as active ingredient 有权
    菲咯啉二氮茚衍生物和含有与活性成分相同的NFkappaB抑制剂

    公开(公告)号：US08569327B2

    公开(公告)日：2013-10-29

    申请号：US13124554

    申请日：2009-10-23

    申请人： Takashi Ikeda ,  Seigo Sawada ,  Takashi Yaegashi ,  Takeshi Matsuzaki ,  Shusuke Hashimoto ,  Ryuta Yamazaki

    发明人： Takashi Ikeda ,  Seigo Sawada ,  Takashi Yaegashi ,  Takeshi Matsuzaki ,  Shusuke Hashimoto ,  Ryuta Yamazaki

    IPC分类号： A61K31/403 ,  C07D221/18

    CPC分类号： C07D471/04

    摘要： A novel compound having an excellent NFκB inhibitory effect is provided. Specifically disclosed is a compound represented by the following formula (1) or a salt thereof: wherein, R1 represents a hydrogen atom, a lower alkyl group, or the like; R2 represents a hydrogen atom, a lower alkyl group, a halogen atom, or the like; R3 represents a hydrogen atom, a lower alkyl group, a hydroxyl group, or a halogen atom; R4 represents a hydrogen atom or a lower alkyloxy group; R5 represents a hydrogen atom, a lower alkyloxy group, a halogen atom, a hydroxyl group, or a methylenedioxy group formed together with R6 or an isopropylidenedioxy group formed together with R6; R6 represents a hydrogen atom, a lower alkyloxy group, or a methylenedioxy group formed together with R5 or an isopropylidenedioxy group formed together with R5; R7 represents a hydrogen atom or a lower alkyl group; and R8 represents a hydrogen atom, a hydroxyl group, an amino group, a lower alkylcarbonyloxy group, or a halogen atom.

    摘要翻译： 提供了具有优异NFκB抑制作用的新型化合物。 具体公开的是由下式（1）表示的化合物或其盐：其中，R1表示氢原子，低级烷基等; R2表示氢原子，低级烷基，卤素原子等; R3表示氢原子，低级烷基，羟基或卤素原子; R4表示氢原子或低级烷氧基; R5表示与R6一起形成的与R6或异丙烯二氧基一起形成的氢原子，低级烷氧基，卤素原子，羟基或亚甲二氧基; R6表示与R5一起形成的氢原子，低级烷氧基或亚甲二氧基，或与R5形成的异丙烯二氧基; R7表示氢原子或低级烷基; R8表示氢原子，羟基，氨基，低级烷基羰基氧基或卤素原子。

    Reinforced bicycle rim
    20.
    发明授权
    Reinforced bicycle rim 有权
    强化自行车轮圈

    公开(公告)号：US07578563B2

    公开(公告)日：2009-08-25

    申请号：US11739748

    申请日：2007-04-25

    申请人： Tsutomu Muraoka ,  Takashi Yaegashi ,  Shinpei Okajima

    发明人： Tsutomu Muraoka ,  Takashi Yaegashi ,  Shinpei Okajima

    IPC分类号： B60B21/06 ,  B60B25/00

    CPC分类号： B60B21/062 ,  B60B1/041 ,  B60B1/044 ,  B60B21/023 ,  B60B21/025 ,  B60B21/04 ,  B60B21/08 ,  B60B21/12

    摘要： A bicycle rim is basically provided with an annular metallic rim member and a reinforcing member. The annular metallic rim member includes a plurality of spoke attachment areas with at least one spoke attachment opening in each of the spoke attachment areas. The reinforcing member overlies an exterior surface of the annular metallic rim member. The reinforcing member includes a plurality of spoke attachment sections individually arranged in a circumferential direction to overlie the spoke attachment openings. The spoke attachment sections include a plurality of discrete first reinforcing parts and a plurality of discrete second reinforcing parts. The first reinforcing parts are attached to the spoke attachment areas around the spoke attachment openings. The second reinforcing parts are attached to the spoke attachment areas to overlie the first reinforcing parts, with the second reinforcing parts being larger than the first reinforcing parts.

    摘要翻译： 自行车边缘基本上设置有环形金属边缘构件和加强构件。 环形金属边缘构件包括在每个辐条连接区域中具有至少一个辐条连接开口的多个辐条连接区域。 加强构件覆盖在环形金属边缘构件的外表面上。 加强构件包括沿圆周方向单独布置以覆盖轮辐附接开口的多个轮辐连接部。 轮辐连接部分包括多个离散的第一加强部分和多个离散的第二加强部分。 第一增强部分附接到轮辐附接开口周围的轮辐连接区域。 第二加强部分附接到轮辐附接区域以覆盖第一加强部分，第二加强部分大于第一加强部分。