公开(公告)号：US5138059A

公开(公告)日：1992-08-11

申请号：US380379

申请日：1989-07-17

申请人： Keiichi Takahashi ,  Michio Ichimura ,  Shigeo Katsumata ,  Tatsuhiro Ogawa ,  Makoto Morimoto ,  Tadashi Ashizawa ,  Masaji Kasai ,  Kenichi Muroi ,  Hiromitsu Saito ,  Hiroshi Sano ,  Toru Yasuzawa

发明人： Keiichi Takahashi ,  Michio Ichimura ,  Shigeo Katsumata ,  Tatsuhiro Ogawa ,  Makoto Morimoto ,  Tadashi Ashizawa ,  Masaji Kasai ,  Kenichi Muroi ,  Hiromitsu Saito ,  Hiroshi Sano ,  Toru Yasuzawa

IPC分类号： C12P17/18 ,  A61K31/40 ,  A61K31/435 ,  A61P31/04 ,  A61P35/00 ,  C07D471/04 ,  C07D487/04 ,  C12N1/20 ,  C12R1/465

CPC分类号： C07D471/04 ,  C07D487/04

摘要： Novel DC-89 compounds represented by the general formula: ##STR1## wherein X represents a single bond or --CH.sub.2 --; and when X represents a single bond, Y represents --CH.sub.2 Br or --CH.sub.2 Cl and when X represents --CH.sub.2 --, Y represents Br, are obtained by the present invention. The compounds have antibacterial and anti-tumor activity.

公开(公告)号：US5071984A

公开(公告)日：1991-12-10

申请号：US612487

申请日：1990-11-14

申请人： Hiromitsu Saito ,  Akira Sato ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Hiromitsu Saito ,  Akira Sato ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

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

CPC分类号： C07D471/18 ,  C07D498/22

摘要： Disclosed are DC-52 derivatives represented by the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or hydroxyl, X represents hydroxyl and Y represents cyano and Z represents carboxyl or hydroxymethyl, or pharmacologically acceptable salts thereof. The DC-52 derivatives are useful as antitumor agents.

公开(公告)号：US4992551A

公开(公告)日：1991-02-12

申请号：US435246

申请日：1989-11-13

申请人： Hiromitsu Saito ,  Akira Sato ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Hiromitsu Saito ,  Akira Sato ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

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

CPC分类号： C07D471/18 ,  C07D498/22

摘要： Disclosed are DC-52 derivatives represented by the formula: ##STR1## wherein each of R.sup.1 and R.sup.2 independently represents hydrogen or hydroxyl, X represents hydroxyl and Y represents cyano and Z represents carboxyl or hydroxymethyl, or pharmacologically acceptable salts thereof. The DC-52 derivatives are useful as antitumor agents.

公开(公告)号：US4771068A

公开(公告)日：1988-09-13

申请号：US850200

申请日：1986-04-10

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

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

IPC分类号： A61K31/40 ,  A61P35/00 ,  C07D487/14

CPC分类号： C07D487/14

摘要： Mitomycin derivatives of the formula: ##STR1## wherein X is ##STR2## [wherein R.sub.3 is alkyl, cycloalkyl or optionally substituted phenyl; and R.sub.4 is alkyl or cycloalkyl]; n is an integer of 2 to 8; one of R.sub.1 and R.sub.2 is a hydrogen atom and the other is a carbamoyloxymethyl group, or alternatively R.sub.1 and R.sub.2 may be combined together to form a methylene group (.dbd.CH.sub.2); and Y and Z independently represent hydrogen or methyl;exhibit anti-bacterial and anti-tumor activities.

摘要翻译： 下式的丝裂霉素衍生物：其中X为<其中R 3为烷基，环烷基或任选取代的苯基; 和R4是烷基或环烷基]; n为2〜8的整数， R1和R2之一是氢原子，另一个是氨基甲酰氧基甲基，或者R1和R2可以组合在一起形成亚甲基（= CH 2）; Y和Z独立地表示氢或甲基; 表现出抗菌和抗肿瘤活性。

公开(公告)号：US5084468A

公开(公告)日：1992-01-28

申请号：US392271

申请日：1989-08-10

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

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：US5952355A

公开(公告)日：1999-09-14

申请号：US757080

申请日：1996-11-26

申请人： Shun-Ichi Ikeda ,  Uichiro Kimura ,  Tadashi Ashizawa ,  Katsushige Gomi ,  Hiromitsu Saito ,  Masaji Kasai ,  Junji Kanazawa ,  Kimihito Sasaki ,  Etsuko Nukui ,  Masami Okabe ,  Soichiro Sato

发明人： Shun-Ichi Ikeda ,  Uichiro Kimura ,  Tadashi Ashizawa ,  Katsushige Gomi ,  Hiromitsu Saito ,  Masaji Kasai ,  Junji Kanazawa ,  Kimihito Sasaki ,  Etsuko Nukui ,  Masami Okabe ,  Soichiro Sato

IPC分类号： C07D209/12 ,  C07D209/30 ,  C07D401/06 ,  C07D405/06 ,  C07F7/08 ,  C07H15/24 ,  A61K31/40 ,  A61K31/44 ,  C07D209/32 ,  C07D209/40

CPC分类号： C07D401/06 ,  C07D209/12 ,  C07D209/30 ,  C07D405/06 ,  C07F7/0812 ,  C07H15/24

摘要： The present invention relates to propenone derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, or YR.sup.5 (wherein Y represents S or O; and R.sup.5 represents substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a substituted or unsubstituted cyclic ether residue); R.sup.2 and R.sup.3 independently represent hydrogen, lower alkyl, or substituted or unsubstituted aralkyl, or alternatively R.sup.2 and R.sup.3 are combined to form substituted or unsubstituted methylene or ethylene; R.sup.4 represents hydrogen, hydroxy, lower alkyl, substituted or unsubstituted aralkyl, lower alkoxy, substituted or unsubstituted aralkyloxy, or halogen; and X represents substituted or unsubstituted indolyl; or pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及由下式（I）表示的丙烯酮衍生物：其中R1表示氢，取代或未取代的低级烷基，取代或未取代的芳基或YR5（其中Y表示S或O; R5表示取代或未取代的低级烷基 取代或未取代的芳基，取代或未取代的杂芳基，或取代或未取代的环醚残基）; R2和R3独立地表示氢，低级烷基或取代或未取代的芳烷基，或者R2和R3组合形成取代或未取代的亚甲基或亚乙基; R4表示氢，羟基，低级烷基，取代或未取代的芳烷基，低级烷氧基，取代或未取代的芳烷氧基或卤素; X表示取代或未取代的吲哚基; 或其药学上可接受的盐。

公开(公告)号：US4880825A

公开(公告)日：1989-11-14

申请号：US173219

申请日：1988-03-25

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

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

IPC分类号： C07D491/22

CPC分类号： C07D491/22

摘要： Mitomycin derivatives having potent anti-tumor activity having the formula: ##STR1## wherein one of R.sub.1 and R.sub.2 represents carbamoyloxymethyl and the other represents hydrogen or R.sub.1 and R.sub.2 are bonded together to form methylene;X is hydrogen or halogen;Y is hydrogen or methyl;Z is hydrogen, methyl or acyl; andn is an integer of 2 or 3.

公开(公告)号：US5068349A

公开(公告)日：1991-11-26

申请号：US404353

申请日：1989-09-07

申请人： Yutaka Kanda ,  Masaji Kasai ,  Hitoshi Arai ,  Makoto Morimoto ,  Tadashi Ashizawa

发明人： Yutaka Kanda ,  Masaji Kasai ,  Hitoshi Arai ,  Makoto Morimoto ,  Tadashi Ashizawa

IPC分类号： A61K31/40 ,  A61P31/04 ,  A61P35/00 ,  C07D487/14 ,  C07D513/14

CPC分类号： C07D487/14

摘要： Novel mitomycin derivatives are characterized by a substituent on the C.sub.6 -methyl group. The mitomycin derivatives exhibit anti-tumor and antibacterial activity and have low toxicity.

公开(公告)号：US4691024A

公开(公告)日：1987-09-01

申请号：US915949

申请日：1986-10-03

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

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

IPC分类号： A61K31/40 ,  A61K38/00 ,  A61P31/04 ,  A61P35/00 ,  C07D487/14 ,  C07K5/02 ,  C07K5/06

CPC分类号： C07D487/14 ,  C07K5/0215 ,  C07K5/06026 ,  A61K38/00

摘要： The present invention provides new mitomycin derivatives of general formula (I) ##STR1## [wherein Y and Z, which may be the same or different, each represents a hydrogen atom or a methyl group; represents .alpha. or .beta. bonding and X represents a group of formula (II) ##STR2## (wherein R.sub.1 to R.sub.5 are each selected from hydrogen, halogen, hydroxyl, nitro, amino, lower alkyl, lower alkoxy, lower alkylamino or lower alkanoylamino);or an S-yl group of an amino acid having a thiol group, the carboxyl group optionally being protected e.g. in the form of a lower alkyl ester group and the amino group optionally being protected e.g. in the form of a lower alkanoylamino group;or an S-yl group of a di- or tripeptide containing an amino acid residue with a thiol group, the carboxyl group optionally being protected e.g. in the form of a lower alkyl ester and the amino group optionally being protected e.g. in the form of a lower alkanoylamino group]; and salts thereof.Such mitomycin derivatives have improved anti-bacterial and anti-tumor activities and low toxicity.

摘要翻译： 本发明提供新的通式（I）的丝裂霉素衍生物：其中Y和Z可以相同或不同，各自表示氢原子或甲基; 表示α或β键，X表示式（II）的基团（II）（其中R 1至R 5各自选自氢，卤素，羟基，硝基，氨基，低级烷基，低级烷氧基，低级烷基氨基或低级 烷酰氨基）; 或具有硫醇基的氨基酸的S-基团，所述羧基任选被保护，例如。 以低级烷基酯基团的形式，并且任选地被保护的氨基，例如。 为低级烷酰氨基的形式; 或含有具有硫醇基的氨基酸残基的二肽或三肽的S-基团，所述羧基任选被保护，例如。 以低级烷基酯的形式，并且任选地被保护的氨基，例如。 以低级烷酰氨基的形式]; 及其盐。 这种丝裂霉素衍生物具有改善的抗细菌和抗肿瘤活性和低毒性。