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    Camptothecin derivatives, preparations thereof and antitumor agents
    21.
    发明授权
    Camptothecin derivatives, preparations thereof and antitumor agents 失效
    喜树碱衍生物，其制剂和抗肿瘤剂

    公开(公告)号：US5843954A

    公开(公告)日：1998-12-01

    申请号：US976398

    申请日：1997-11-21

    申请人： Takashi Yaegashi ,  Seigo Sawada ,  Tomio Furuta ,  Teruo Yokokura

    发明人： Takashi Yaegashi ,  Seigo Sawada ,  Tomio Furuta ,  Teruo Yokokura

    IPC分类号： A61K31/47 ,  A61K31/4745 ,  A61P35/00 ,  C07D209/00 ,  C07D221/00 ,  C07D471/14 ,  C07D487/02

    CPC分类号： C07D471/14

    摘要： New camptothecin derivatives of the general formula (1): ##STR1## wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.2 represents a hydrogen or a C.sub.1 -C.sub.6 alkoxy group, R.sup.3 represents a hydrogen or halogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, C.sub.2 -C.sub.6 acyloxy or methoxyethoxymethoxy group, R.sup.4 represents a hydrogen or halogen atom, and R.sup.5 represents a C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 unsaturated alkyl, alkylthioalkyl, alkoxyalkyl, pyridyl or substituted phenyl group, with the proviso that all of the R.sup.2, R.sup.3 and R.sup.4 substituents should not be a hydrogen atom, and a process for preparing the new camptothecin derivatives by subjecting the camptothecin derivatives of the general formula (2): ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 have the same meanings as given above, to the reaction with N,N-dimethylethylenediamine without solvent to open the E-lactone ring followed by acylation of 17-hydroxyl group with corresponding acylating agents and an antitumor agent containing the same as an active ingredient.

    摘要翻译： （1）的新喜树碱衍生物：其中R1表示氢原子或C1-C6烷基，R2表示氢或C1-C6烷氧基，R3表示氢或卤素原子 或C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，C 2 -C 6酰氧基或甲氧基乙氧基甲氧基，R 4表示氢或卤素原子，R 5表示C 1 -C 6烷基，C 3 -C 6不饱和烷基，烷硫基烷基，烷氧基烷基，吡啶基 或取代的苯基，条件是所有的R 2，R 3和R 4取代基不应该是氢原子，以及通过使通式（2）的喜树碱衍生物进行制备来制备新的喜树碱衍生物的方法： （2）其中R 1，R 2，R 3和R 4具有与上述相同的含义，与没有溶剂的N，N-二甲基乙二胺反应以打开E-内酯环，随后用相应的酰化剂酰化17-羟基， 含有与活性物质相同的抗肿瘤剂 e成分。

    Camptothecin derivatives
    22.
    发明授权
    Camptothecin derivatives 失效
    喜树碱衍生物

    公开(公告)号：US4914205A

    公开(公告)日：1990-04-03

    申请号：US210918

    申请日：1988-06-24

    申请人： Seigo Sawada ,  Kenichiro Nokata ,  Satoru Okajima ,  Hisako Nagai ,  Takashi Yaegashi ,  Kenichi Tezuka ,  Tadashi Miyasaka

    发明人： Seigo Sawada ,  Kenichiro Nokata ,  Satoru Okajima ,  Hisako Nagai ,  Takashi Yaegashi ,  Kenichi Tezuka ,  Tadashi Miyasaka

    IPC分类号： C07D471/14

    CPC分类号： C07D471/14

    摘要： New camptothecin derivatives, useful as antitumor agents or intermediates therefor, of the general formula (I) ##STR1## wherein X is a lower alkyl group, and R is a hydrogen atom or the grouping -COY where Y is a linear or branched unsubstituted C.sub.1 -C.sub.18 alkyl group; a lower alkyl group substituted by a halogen atom or a lower alkylthio, amino, acylamino, hydroxyl, lower alkoxy, aryloxy or lower alkoxycarbonyl group; a C.sub.3 -C.sub.19 alkenyl, C.sub.3 -C.sub.19 alkynyl or C.sub.3 -C.sub.8 cycloalkyl group; a C.sub.3 -C.sub.8 cycloalkyl group substituted by an acylamino-lower alkyl group; an N-acylpyrrolidyl group; a phenyl group; a phenyl group substituted by a halogen atom or a trifluoromethyl, nitro, amino, lower alkoxycarbonyl, lower alkyl, phenyl or lower alkoxy; a cinnamyl group; a benzyl group; a naphthyl group; a pyridyl group; a furyl group; or a thienyl group, as well as acid addition salts and quaternary ammonium salts thereof,and a process for preparing the new camptothecin derivatives by subjecting 7-ethylcamptothecin to the treatment with an N-di-X-ethylenediamine followed by acylation.

    Process for Production of Camptothecin Derivative
    26.
    发明申请
    Process for Production of Camptothecin Derivative 失效
    喜树碱衍生物的制备方法

    公开(公告)号：US20120142926A1

    公开(公告)日：2012-06-07

    申请号：US12226506

    申请日：2007-04-27

    申请人： Seigo Sawada ,  Takashi Yaegashi

    发明人： Seigo Sawada ,  Takashi Yaegashi

    IPC分类号： C07D491/22

    CPC分类号： C07B53/00 ,  C07D491/22

    摘要： Disclosed is a process for production of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]-carbonyloxycamptothecin from a camptothecin composition containing 18,19-dehydrocamptothecin without producing any vinyl form of the compound. The process is characterized by catalytically reducing at least one compound selected from a compound (1) and others in the process of producing a compound (5) from a composition containing the compound (1).

    摘要翻译： 公开了一种从不含任何乙烯基形式的化合物生产含有18,19-脱氢喜树碱的喜树碱组合物的7-乙基-10- [4-（1-哌啶子基）-1-哌啶子基]羰氧基喜树碱的方法。 该方法的特征在于在含有化合物（1）的组合物的制备方法中催化还原至少一种选自化合物（1）和其它化合物的化合物。

    PHENANTHROINDOLIZIDINE COMPOUND AND NFkB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT
    27.
    发明申请
    PHENANTHROINDOLIZIDINE COMPOUND AND NFkB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT 有权
    苯并噻唑类化合物和含有其作为活性成分的NFkB抑制剂

    公开(公告)号：US20110201638A1

    公开(公告)日：2011-08-18

    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： A61K31/437 ,  C07D471/04 ,  A61P29/00 ,  A61P35/00

    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; and R8 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 ）。

    PHENANTHROINDOLIZIDINE DERIVATIVE AND NFKB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT
    28.
    发明申请
    PHENANTHROINDOLIZIDINE DERIVATIVE AND NFKB INHIBITOR CONTAINING SAME AS ACTIVE INGREDIENT 有权
    苯并呋喃衍生物和含有其作为活性成分的NFκB抑制剂

    公开(公告)号：US20110201637A1

    公开(公告)日：2011-08-18

    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： A61K31/437 ,  C07D221/18 ,  A61P35/00

    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NF＆Kgr B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。

    Camptothecin derivatives
    30.
    发明授权
    Camptothecin derivatives 有权
    喜树碱衍生物

    公开(公告)号：US06310210B1

    公开(公告)日：2001-10-30

    申请号：US09530828

    申请日：2000-05-03

    申请人： Takanori Ogawa ,  Takashi Yaegashi ,  Seigo Sawada ,  Tomio Furuta

    发明人： Takanori Ogawa ,  Takashi Yaegashi ,  Seigo Sawada ,  Tomio Furuta

    IPC分类号： C07D47104

    CPC分类号： C07D471/14

    摘要： The present invention relates to new camptothecin derivatives shown by the below formula, which are water-soluble and excellent in an anti-tumor activity, and to salts thereof. In the formula, R1 represents a hydrogen atom or an alkyl group with 1-6 carbon atoms, R2 represents identically or differently 0-4 alkyl groups with 1-6 carbon atoms, a halogen atom, an alkoxyl or hydroxyl group, R3 represents a lower alkylamino, di-lower alkylamino, arylamino, cyclicamino or lower alkoxyl group, and salts thereof.

    摘要翻译： 本发明涉及由下式表示的新的喜树碱衍生物，它是水溶性的，抗肿瘤活性优异的盐及其盐。式中R1表示氢原子或1-6位烷基 碳原子，R2表示相同或不同的具有1-6个碳原子的0-4个烷基，卤素原子，烷氧基或羟基，R3表示低级烷基氨基，二低级烷基氨基，芳基氨基，环氨基或低级烷氧基， 的盐。