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：US4853385A

公开(公告)日：1989-08-01

申请号：US174897

申请日：1988-03-29

申请人： Yutaka Saito ,  Masaji Kasai ,  Kunikatsu Shirahata ,  Motomichi Kono ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Yutaka Saito ,  Masaji Kasai ,  Kunikatsu Shirahata ,  Motomichi Kono ,  Makoto Morimoto ,  Tadashi Ashizawa

IPC分类号： C07D487/14 ,  A61K31/495 ,  A61P35/00 ,  C07D487/22

CPC分类号： C07D487/22

摘要： 7-N,8-N-Ethylenemitomycin 8-imines represented by the formula ##STR1## wherein one of the R.sub.1 and R.sub.2 represents carbamoyloxymethyl and another represents hydrogen or both are combined together to form methylene; R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each independently represent hydrogen or C.sub.1-4 alkyl, or R.sub.3 and R.sub.4 may be combined together to represent --(CH.sub.2).sub.n --, wherein n is 3 or 4; and Y and Z represent hydrogen or methyl, provided that when R.sub.1 represents carbamoyloxymethyl and Y represents methyl, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and Z are not hydrogen simultaneously, has an excellent antitumor activity.

公开(公告)号：US4847387A

公开(公告)日：1989-07-11

申请号：US199043

申请日：1988-03-17

申请人： Hirofumi Nakano ,  Isami Takahashi ,  Fusao Tomita ,  Kozo Asano ,  Toru Yasuzawa ,  Tadashi Ashizawa ,  Keiichi Takahashi

发明人： Hirofumi Nakano ,  Isami Takahashi ,  Fusao Tomita ,  Kozo Asano ,  Toru Yasuzawa ,  Tadashi Ashizawa ,  Keiichi Takahashi

IPC分类号： C07H7/06 ,  C07H15/12 ,  C07H17/04 ,  C12P19/26 ,  C12P19/44

CPC分类号： C07H15/12 ,  C07H17/04 ,  C12P19/26 ,  C12P19/44

摘要： The present invention relates to novel compounds DC-92B and DC-92D having anthraquinone moiety and represented by the following planar structural formula (I) and to a process for producing the same. These compounds can be produced by culture of a microorganism belonging to the genus Actinomadura, and are useful as medicaments because of their antibacterial and anti-tumor activities. ##STR1## wherein R is a group represented by formula (II) or formula (III): ##STR2##

公开(公告)号：US4791113A

公开(公告)日：1988-12-13

申请号：US57889

申请日：1987-05-12

申请人： Tokuyuki Kuroda ,  Koji Hisamura ,  Tohru Sugaya ,  Yutaka Ohsawa ,  Hideo Ueno ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Tokuyuki Kuroda ,  Koji Hisamura ,  Tohru Sugaya ,  Yutaka Ohsawa ,  Hideo Ueno ,  Makoto Morimoto ,  Tadashi Ashizawa

IPC分类号： C07D487/14 ,  A61K31/505 ,  A61K31/40 ,  C07D487/04

CPC分类号： C07D487/14

摘要： Mitomycin derivatives having potent antitumor activity having the formula: ##STR1## wherein A is ON--or R.sub.4 N.dbd.N--[wherein R.sub.4 is selected from ##STR2## and optionally substituted heterocyclic groups (wherein R.sub.5 and R.sub.8 are each independently selected from hydrogen, lower alkyl and lower cycloalkyl; R.sub.6 is selected from hydrogen, halogen, hydroxy, lower alkoxy, amino and nitro; R.sub.7 is selected from lower alkyl and lower cycloalkyl; and X is selected from oxygen, sulphur and imino)];R.sub.1 and R.sub.2 are each independently selected from hydrogen, lower alkyl, lower cycloalkyl, optionally substituted aralkyl, optionally substituted alkanoyl, optionally substituted arylcarbonyl, optionally substituted alkanesulfonyl, arylsulfonyl and aralkylsulfonyl;R.sub.3 is hydrogen or carbamoyl;Y is hydrogen or methyl;Z is selected from hydrogen, methyl and acetyl;and is an .alpha. or .beta. bond.

摘要翻译： 丝裂霉素衍生物具有有效的抗肿瘤活性，具有下式：其中A为ON-或R 4 N = N- [其中R 4为选自下列任意取代的杂环基团（其中R5和R8 各自独立地选自氢，低级烷基和低级环烷基; R6选自氢，卤素，羟基，低级烷氧基，氨基和硝基; R7选自低级烷基和低级环烷基; X选自氧，硫和亚氨基 ）]; R 1和R 2各自独立地选自氢，低级烷基，低级环烷基，任选取代的芳烷基，任选取代的烷酰基，任选取代的芳基羰基，任选取代的烷基磺酰基，芳基磺酰基和芳烷基磺酰基; R3是氢或氨基甲酰基; Y是氢或甲基; Z选自氢，甲基和乙酰基; 并且是α或β键。

公开(公告)号：US4593097A

公开(公告)日：1986-06-03

申请号：US575294

申请日：1984-01-30

申请人： Fusao Tomita ,  Keiichi Takahashi ,  Isao Kawamoto ,  Kozo Asano ,  Makoto Morimoto ,  Tadashi Ashizawa ,  Kazuhisa Fujimoto

发明人： Fusao Tomita ,  Keiichi Takahashi ,  Isao Kawamoto ,  Kozo Asano ,  Makoto Morimoto ,  Tadashi Ashizawa ,  Kazuhisa Fujimoto

IPC分类号： A61K31/495 ,  A61P1/04 ,  A61P31/04 ,  A61P35/00 ,  C07D241/46 ,  C12P17/12 ,  C12R1/465

CPC分类号： C12P17/12 ,  C07D241/46

摘要： Phenazine compounds represented by the formula: ##STR1## wherein R is a hydrogen atom, an unsubstituted or substituted lower alkanoyl group, or an unsubstituted or substituted arylcarbonyl group have antibacterial and anti-tumor activities.Some of these compounds are produced by incubation of a microorganism.

摘要翻译： 由下式表示的吩嗪化合物：其中R为氢原子，未取代或取代的低级烷酰基或未取代或取代的芳基羰基具有抗菌和抗肿瘤活性。 这些化合物中的一些通过温育微生物产生。

公开(公告)号：US4563462A

公开(公告)日：1986-01-07

申请号：US546142

申请日：1983-10-27

申请人： Shinzo Ishii ,  Shigeo Katsumata ,  Yuko Arai ,  Tadashi Ashizawa ,  Makoto Morimoto ,  Kunikatsu Shirahata ,  Yutaka Saito ,  Motomichi Kono

发明人： Shinzo Ishii ,  Shigeo Katsumata ,  Yuko Arai ,  Tadashi Ashizawa ,  Makoto Morimoto ,  Kunikatsu Shirahata ,  Yutaka Saito ,  Motomichi Kono

IPC分类号： A61K31/47 ,  A61P35/00 ,  A61P35/02 ,  C07D471/16 ,  C12P17/18 ,  C12R1/465

CPC分类号： C07D471/16 ,  C12P17/182 ,  C12R1/465

摘要： A substance designated by us as AX-2 and represented by the formula: ##STR1## This substance is produced by culturing a microorganism of the genus Streptomyces and capable of producing AX-2 in a medium to accumulate AX-2 in the cultured broth and isolating AX-2 therefrom.An anti-tumor composition comprising an effective amount of AX-2 in association with a physiologically acceptable carrier or excipient, which is active against Sarcoma 180.

摘要翻译： 由我们指定为AX-2并由下式表示的物质：该物质通过培养链霉菌属的微生物并能够在培养基中产生AX-2并在培养的肉汤中积累AX-2而产生AX-2， 从其中分离AX-2。 一种抗肿瘤组合物，其包含与生理上可接受的载体或赋形剂相关联的有效量的AX-2，其对肉瘤180有活性。