公开(公告)号：US4923986A

公开(公告)日：1990-05-08

申请号：US273519

申请日：1988-11-08

申请人： Chikara Murakata ,  Akira Sato ,  Mitsuru Takahashi ,  Eiji Kobayashi ,  Makoto Morimoto ,  Shiro Akinaga ,  Tadashi Hirata ,  Kenichi Mochida ,  Hiroshi Kase ,  Koji Yamada ,  Kazuyuki Iwashashi

发明人： Chikara Murakata ,  Akira Sato ,  Mitsuru Takahashi ,  Eiji Kobayashi ,  Makoto Morimoto ,  Shiro Akinaga ,  Tadashi Hirata ,  Kenichi Mochida ,  Hiroshi Kase ,  Koji Yamada ,  Kazuyuki Iwashashi

IPC分类号： A61K31/55 ,  C07D20060101 ,  C07D498/22

CPC分类号： C07D498/22

摘要： The present invention relates to novel derivatives of K-252, (8R*, 9S*, 11S*)-(-)-9-hydroxy-9-methoxycarbonyl-8-methyl-2,3,9,10-tetrahydro-8,11-epoxy-1H,8H, 11H-2,7b,11a-triazadibenzo[a,g]cycloocta-[c,d,e,]trinden-1-one, and the compounds are represented by formula (I): ##STR1## wherein W.sub.1, W.sub.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and Y represent various substituents. The compounds are physiologically active substances that inhibit protein kinase C and exhibit an antitumor activity, and are useful as medicines.

公开(公告)号：US4877776A

公开(公告)日：1989-10-31

申请号：US288787

申请日：1988-12-22

申请人： Chikara Murakata ,  Akira Sato ,  Masaji Kasai ,  Eiji Kobayashi ,  Makoto Morimoto ,  Shiro Akinaga

发明人： Chikara Murakata ,  Akira Sato ,  Masaji Kasai ,  Eiji Kobayashi ,  Makoto Morimoto ,  Shiro Akinaga

IPC分类号： C07D498/22 ,  A61K31/55 ,  A61P35/00 ,  C07H19/23

CPC分类号： C07H19/23

摘要： A K-252 compound represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently H or OH; X represents COOH, COOR or CH.sub.2 OH; Y represents H, R or COR; and Z represents OH, OR or SR, wherein R represents lower alkyl has C-kinase inhibitory activity and is expected to be useful as an active ingredient of anti-tumor agents, etc.

公开(公告)号：US4946957A

公开(公告)日：1990-08-07

申请号：US400883

申请日：1989-08-30

申请人： Hiromitsu Saito ,  Yoichi Uosaki ,  Akira Sato ,  Tadashi Hirata ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Hiromitsu Saito ,  Yoichi Uosaki ,  Akira Sato ,  Tadashi Hirata ,  Makoto Morimoto ,  Tadashi Ashizawa

IPC分类号： A61K31/495 ,  A61P31/04 ,  C07D471/18 ,  C07D498/22

CPC分类号： C07D471/18 ,  C07D498/22

摘要： The present invention relates to novel derivatives of DC-52 represented by the following formula (I): ##STR1## [wherein X is chlorine, bromine, iodine, hydroxyl, formyl, hydroxyiminomethyl, cyano, nitro, amino or lower alkanoylamino; and Y is hydroxyl and Z is cyano, or Y and Z represent --O-- in the form of --Y--Z--]. These compounds and pharmacologically acceptable salts thereof have high anti-tumor activity.

公开(公告)号：US4822882A

公开(公告)日：1989-04-18

申请号：US102359

申请日：1987-09-29

申请人： Hiromitsu Saito ,  Yoichi Uosaki ,  Akira Sato ,  Tadashi Hirata ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Hiromitsu Saito ,  Yoichi Uosaki ,  Akira Sato ,  Tadashi Hirata ,  Makoto Morimoto ,  Tadashi Ashizawa

IPC分类号： C07D471/18 ,  C07D498/22 ,  A61K31/495 ,  C07D487/18

CPC分类号： C07D471/18 ,  C07D498/22

摘要： Compounds represented by the following formula or by the corresponding hydroquinone type formula: ##STR1## in which R.sup.1 and R.sup.2 are independently hydrogen, lower alkoxy, azido, amino, lower alkylamino, di-lower alkylamino, cyclic amino, lower alkylthio or unsubstituted or substituted arylthio; and X represents hydroxyl and Y represents cyano or X and Y together represents --O-- in the form of --X--Y--, have an excellent antitumor activity.

公开(公告)号：US4879386A

公开(公告)日：1989-11-07

申请号：US207639

申请日：1988-05-25

申请人： Hiromitsu Saito ,  Yoichi Uosaki ,  Akira Sato ,  Tadashi Hirata ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Hiromitsu Saito ,  Yoichi Uosaki ,  Akira Sato ,  Tadashi Hirata ,  Makoto Morimoto ,  Tadashi Ashizawa

IPC分类号： A61K31/495 ,  A61P31/04 ,  C07D471/18 ,  C07D498/22

CPC分类号： C07D471/18 ,  C07D498/22

摘要： The present invention relates to novel derivatives of DC-52 represented by the following formula (I): ##STR1## ps [wherein X is chlorine, bromine, iodine, hydroxyl, formyl, hydroxyiminomethyl, cyano, nitro, amino or lower alkanoylamino; and Y is hydroxyl and Z is cyano, or Y and Z represent --O-- in the form of --Y--Z--]. These compounds and pharmacologically acceptable salts thereof have high anti-tumor activity.

公开(公告)号：US5079358A

公开(公告)日：1992-01-07

申请号：US365736

申请日：1989-06-14

申请人： Toru Sugaya ,  Yukiteru Mimura ,  Yasushi Shida ,  Yutaka Osawa ,  Ikuo Matsukuma ,  Shiro Akinaga ,  Makoto Morimoto

发明人： Toru Sugaya ,  Yukiteru Mimura ,  Yasushi Shida ,  Yutaka Osawa ,  Ikuo Matsukuma ,  Shiro Akinaga ,  Makoto Morimoto

IPC分类号： A61K31/47 ,  A61P35/00 ,  C07D471/06

CPC分类号： C07D471/06

摘要： Novel pyrazoloacridone compounds represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof have an excellent anti-tumor activity.

公开(公告)号：US4650869A

公开(公告)日：1987-03-17

申请号：US606902

申请日：1984-05-04

申请人： Tadashi Hirata ,  Shigeru Kobayashi ,  Keiichi Takahashi ,  Makoto Morimoto ,  Yuko Arai

发明人： Tadashi Hirata ,  Shigeru Kobayashi ,  Keiichi Takahashi ,  Makoto Morimoto ,  Yuko Arai

IPC分类号： A61K31/495 ,  A61P31/04 ,  A61P35/00 ,  C07D471/18 ,  C07D498/08 ,  C07D498/22 ,  C07D487/18

CPC分类号： C07D471/18 ,  C07D498/22

摘要： A compound represented by the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl group, X is a hydroxymethyl group and Y is a cyano group, and when R is a lower alkyl group, X and Y may combine to form --CH.sub.2 --O--, and salts thereof, process for preparing the same, and an anti-tumor composition containing the same, which is improved in stability in comparison with a starting compound DC-52.

摘要翻译： 由下式表示的化合物：其中r是氢原子或低级烷基，X是羟甲基，Y是氰基，当R是低级烷基时，X和Y可以组合形成 -CH 2 -O-及其盐，其制备方法和含有该组合物的抗肿瘤组合物，与起始化合物DC-52相比，其稳定性提高。

公开(公告)号：US4618687A

公开(公告)日：1986-10-21

申请号：US724549

申请日：1985-04-18

申请人： Tadashi Hirata ,  Hiromitsu Saito ,  Makoto Morimoto

发明人： Tadashi Hirata ,  Hiromitsu Saito ,  Makoto Morimoto

IPC分类号： A61K31/35 ,  A61K31/352 ,  A61P35/00 ,  C07D311/94

CPC分类号： C07D311/94

摘要： A cyclopentenone compound represented by the following formula: ##STR1## has an antitumor effect and can be produced from the antibiotic XK-213.

摘要翻译： 由下式表示的环戊烯酮化合物：具有抗肿瘤作用，可由抗生素XK-213生产。

公开(公告)号：US5117006A

公开(公告)日：1992-05-26

申请号：US700507

申请日：1991-05-15

申请人： Hiromitsu Saito ,  Masaji Kasai ,  Makoto Morimoto ,  Eiji Kobayashi ,  Yoichi Uosaki ,  Yutaka Kanda ,  Hiroshi Sano

发明人： Hiromitsu Saito ,  Masaji Kasai ,  Makoto Morimoto ,  Eiji Kobayashi ,  Yoichi Uosaki ,  Yutaka Kanda ,  Hiroshi Sano

IPC分类号： C07D487/04 ,  C07D487/10

CPC分类号： C07D487/04 ,  C07D487/10

摘要： A DC-88A derivative represented by general formula: ##STR1## wherein ##STR2## represents ##STR3## has an excellent antitumor activity and is useful as an anti-tumor agent.

公开(公告)号：US5187186A

公开(公告)日：1993-02-16

申请号：US755760

申请日：1991-09-06

申请人： Yutaka Kanda ,  Youichi Uosaki ,  Hiromitsu Saito ,  Hiroshi Sano ,  Eiji Kobayashi ,  Makoto Morimoto ,  Satoru Nagamura

发明人： Yutaka Kanda ,  Youichi Uosaki ,  Hiromitsu Saito ,  Hiroshi Sano ,  Eiji Kobayashi ,  Makoto Morimoto ,  Satoru Nagamura

IPC分类号： C07D487/04 ,  C07D487/10

CPC分类号： C07D487/04 ,  C07D487/10

摘要： DC-88A derivatives represented by the general formula: ##STR1## wherein X represents hydrogen or CO.sub.2 R.sup.1 (in which R.sup.1 represents hydrogen, a straight-chain or branched alkyl having 1 to 4 carbon atoms, allyl, or benzyl); and ##STR2## have an excellent anti-tumor activity and are useful as anti-tumor agents.

摘要翻译： 其中X表示氢或CO 2 R 1（其中R 1表示氢，具有1至4个碳原子的直链或支链烷基，烯丙基或苄基）表示的DC-88A衍生物。 和 具有优异的抗肿瘤活性，可用作抗肿瘤剂。