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公开(公告)号:US06492392B1
公开(公告)日:2002-12-10
申请号:US09481542
申请日:2000-01-12
申请人: Yutaka Kanda , Rieko Tanaka , Mitsunobu Hara , Jun Eishima , Shiro Akinaga , Tadashi Ashizawa
发明人: Yutaka Kanda , Rieko Tanaka , Mitsunobu Hara , Jun Eishima , Shiro Akinaga , Tadashi Ashizawa
IPC分类号: A61K31445
CPC分类号: C07D401/14 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/06 , C07D405/14 , C07D409/14
摘要: The present invention provides 2-piperidone compounds or pharmaceutically acceptable salts thereof, which have a potent activity of inhibiting the proliferation of tumor cells and thus are useful as medicaments, as well as antitumor agents containing these compounds. The 2-piperidone compound is represented by the following formula (I): wherein R1 represents —(CH2)nR1a {wherein n is an integer of from 0 to 5, and R1a represents amino, lower alkylamino, di(lower alkyl)amino, substituted or unsubstituted aryl, or a substituted or unsubstituted heterocyclic group}, and R2 and R3 independently represent lower alkyl which may be substituted by lower alkoxycarboyl; lower alkenyl, aralkyl or lower alkynyl which may be substituted by substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; substituted or unsubstituted aryl; or a substituted or unsubstituted heterocyclic group.
摘要翻译: 本发明提供了具有抑制肿瘤细胞增殖的有效活性的2-哌啶酮化合物或其药学上可接受的盐,因此可用作药物,以及含有这些化合物的抗肿瘤剂。 2-哌啶酮化合物由下式(I)表示:其中R1表示 - (CH2)nR1a {其中n为0-5的整数,R1a表示氨基,低级烷基氨基,二(低级烷基)氨基,取代的 或未取代的芳基,或取代或未取代的杂环基},R2和R3独立地表示可以被低级烷氧基羰基取代的低级烷基; 可被取代或未取代的芳基或取代或未取代的杂环基取代的低级烯基,芳烷基或低级炔基; 取代或未取代的芳基; 或取代或未取代的杂环基。
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公开(公告)号:US5256685A
公开(公告)日:1993-10-26
申请号:US857427
申请日:1992-03-26
申请人: Hitoshi Arai , Yutaka Kanda , Motomichi Kono , Masaji Kasai , Tadashi Ashizawa , Katsushige Gomi
发明人: Hitoshi Arai , Yutaka Kanda , Motomichi Kono , Masaji Kasai , Tadashi Ashizawa , Katsushige Gomi
IPC分类号: C07D487/14 , C07D491/22 , A61K31/33 , A61K31/40
CPC分类号: C07D487/14
摘要: Novel mitomycin derivatives represented by the formula (I) are obtained by introducing a substituent at the 6-position. The mitomycin derivatives of the present invention have an antitumor activity.
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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.
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公开(公告)号:US6080771A
公开(公告)日:2000-06-27
申请号:US133363
申请日:1998-08-13
申请人: Yutaka Kanda , Hitoshi Arai , Hiroyuki Yamaguchi , Tadashi Ashizawa , Shun-ichi Ikeda , Chikara Murakata , Tatsuya Tamaoki
发明人: Yutaka Kanda , Hitoshi Arai , Hiroyuki Yamaguchi , Tadashi Ashizawa , Shun-ichi Ikeda , Chikara Murakata , Tatsuya Tamaoki
IPC分类号: C07D513/08 , C07D513/18 , C07D513/20 , C07H15/26 , C07H17/02 , A61K31/425 , A61K31/70 , C07D519/00
CPC分类号: C07D513/08 , C07H15/26 , C07H17/02
摘要: DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents CO(CR.sup.4A R.sup.4B).sub.n1 (O(CH.sub.2).sub.p1).sub.n2 OR.sup.5 {wherein n1 represents an integer of 1 or 2; R.sup.4A and R.sup.4B are the same or different, and each represents hydrogen or lower alkyl; p1 and n2 each represents an integer of 1 to 10; and R.sup.5 represents hydrogen, lower alkyl, or the like), or ##STR2##
摘要翻译: 提供了具有抗微生物活性和抗肿瘤活性的由式(I)表示的DC107衍生物或其药学上可接受的盐,其中R1表示CO(CR4AR4B)n1(O(CH2)p1)n2OR5 {其中n1表示1或2的整数; R4A和R4B相同或不同,各自表示氢或低级烷基; p1和n2各自表示1〜10的整数, 和R 5表示氢,低级烷基等)
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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.
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公开(公告)号:US5981558A
公开(公告)日:1999-11-09
申请号:US133614
申请日:1998-08-13
申请人: Hitoshi Arai , Yutaka Kanda , Hiroyuki Yamaguchi , Tadashi Ashizawa , Chikara Murakata , Shun-ichi Ikeda , Tatsuya Tamaoki
发明人: Hitoshi Arai , Yutaka Kanda , Hiroyuki Yamaguchi , Tadashi Ashizawa , Chikara Murakata , Shun-ichi Ikeda , Tatsuya Tamaoki
IPC分类号: C07D513/18 , C07H15/26 , C07D513/08 , A61K31/425
CPC分类号: C07D513/18 , C07H15/26
摘要: DC107 derivatives represented by formula (I) or pharmaceutically acceptable salts thereof which have antimicrobial activity and antitumor activity are provided: ##STR1## wherein R.sup.1 represents hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4, or the like; R.sup.2 represents hydrogen or COR.sup.6 ; R.sup.3 represents --CH.sub.2 OCOR.sup.7, phthalimidomethyl, or the like; and W represents oxygen or NR.sup.8 (wherein R.sup.8 represents hydroxy, lower alkoxy, lower alkenyloxy, aralkyloxy, substituted or unsubstituted arylsulfonylamino, or lower alkoxycarbonylamino).
摘要翻译: 提供了具有抗微生物活性和抗肿瘤活性的由式(I)表示的DC107衍生物或其药学上可接受的盐,其中R1表示氢,低级烷氧基烷基,芳烷氧基烷基,低级烷氧基烷氧基烷基,低级烷氧基烷氧基烷氧基烷基,芳烷基,四氢吡喃基,COR4等; R2表示氢或COR6; R3表示-CH2OCOR7,苯二甲酰亚氨基甲基等; W表示氧或NR8(其中R8表示羟基,低级烷氧基,低级烯氧基,芳烷氧基,取代或未取代的芳基磺酰基氨基或低级烷氧基羰基氨基)。
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公开(公告)号:US5334611A
公开(公告)日:1994-08-02
申请号:US101029
申请日:1993-08-03
申请人: Hitoshi Arai , Yutaka Kanda , Motomichi Kono , Masaji Kasai , Tadashi Ashizawa , Katsushige Gomi
发明人: Hitoshi Arai , Yutaka Kanda , Motomichi Kono , Masaji Kasai , Tadashi Ashizawa , Katsushige Gomi
IPC分类号: C07D487/14 , C07D491/22 , C07D487/22 , A61K31/40
CPC分类号: C07D487/14
摘要: Novel mitomycin derivatives represented by the formula (I) are obtained by introducing a substituent at the 6-position. The mitomycin derivatives of the present invention have an antitumor activity.
摘要翻译: 通过在6-位上引入取代基而获得由式(I)表示的新型丝裂霉素衍生物。 本发明的丝裂霉素衍生物具有抗肿瘤活性。
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公开(公告)号:US5733924A
公开(公告)日:1998-03-31
申请号:US776938
申请日:1997-04-17
申请人: Yutaka Kanda , Yutaka Saitoh , Hiromitsu Saito , Tadashi Ashizawa , Kazuyo Sugiyama , Katsushige Gomi , Shingo Kakita , Yuichi Takahashi , Chikara Murakata
发明人: Yutaka Kanda , Yutaka Saitoh , Hiromitsu Saito , Tadashi Ashizawa , Kazuyo Sugiyama , Katsushige Gomi , Shingo Kakita , Yuichi Takahashi , Chikara Murakata
IPC分类号: C07D513/08 , A61K37/00
CPC分类号: C07D513/08
摘要: DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, �wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.!
摘要翻译: PCT No.PCT / JP96 / 01646 Sec。 371日期1997年04月17日 102(e)1997年4月17日PCT PCT 1996年6月14日PCT公布。 出版物WO97 / 00260 PCT 日本1997年3月1日由式(I)代表的DC107衍生物:其中R1为氢,低级烷氧基烷基,芳烷氧基烷基,低级烷氧基烷氧基烷基,低级烷氧基烷氧基烷氧基烷基,芳烷基,四氢吡喃基,COR4或 类似; R2表示氢或COR5; R3代表低级烷基,低级烯基,可被取代或未取代的芳基取代的芳烷基,低级烷氧基烷基,芳烷氧基烷基,取代或未取代的芳氧基烷基,低级烷氧基羰基烷基,低级烷酰氧基烷基,脂环族烷酰氧基烷基等,或与Y键合以表示单键 ; Y键合到R3表示单键,或键合到Z表示单键; Z表示氢或与Y键合以表示单键; W表示氧或NR 6,条件是其中R1,R2和Z各自表示氢,R3与Y键合以表示单键,W表示氧(DC107)的化合物。
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公开(公告)号:US5972997A
公开(公告)日:1999-10-26
申请号:US930852
申请日:1997-10-03
申请人: Tamio Mizukami , Akira Asai , Katsuhiko Ando , Shingo Kakita , Akira Mihara , Katsunori Kita , Yasuhiro Suzuki , Tadashi Ashizawa
发明人: Tamio Mizukami , Akira Asai , Katsuhiko Ando , Shingo Kakita , Akira Mihara , Katsunori Kita , Yasuhiro Suzuki , Tadashi Ashizawa
IPC分类号: C07D307/77 , C07D493/04 , C12P17/04 , A01N43/08
CPC分类号: C07D307/77 , C07D493/04 , C12P17/04
摘要: The present invention relates to UCT1072 compounds represented by formula (I): wherein R.sup.1 and R.sup.2 together represent --CH(OH)CH.sub.2 O-- or --CH.sub.2 CH.sub.2 CH(OH)CH.sub.2 --.
摘要翻译: PCT No.PCT / JP97 / 00282 Sec。 371日期1997年10月3日第 102(e)日期1997年10月3日PCT 1997年2月6日提交PCT公布。 第WO97 / 29099号公报 日期:1997年8月14日本发明涉及由式(I)表示的UCT1072化合物:其中R 1和R 2一起表示-CH(OH)CH 2 O-或-CH 2 CH 2 CH(OH)CH 2 - 。
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10.
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。
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