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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。
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公开(公告)号:US5539112A
公开(公告)日:1996-07-23
申请号:US464093
申请日:1995-06-05
申请人: Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
发明人: Tsutomu Akama , Shun-ichi Ikeda , Yasushi Shida , Masaji Kasai , Hiroyuki Ishida , Uichiro Kimura , Katsushige Gomi , Hiromitsu Saito , Kimihisa Ueno
IPC分类号: C07D311/30 , C07D413/12
CPC分类号: C07D311/30
摘要: 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.6 are taken together to form a heterocyclic group containing the nitrogen atom in the ring), lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, carboxy, lower alkoxycarbonyl, lower alkanoyl, adizo, cyano, substituted or unsubstituted carbamoyl or lower alkylthiothiocarbonyl: or pharmaceutically acceptable salts thereof.
摘要翻译: 由式(I)表示的5-氨基黄酮衍生物:其中R 1,R 2,R 3和R 4相同或不同,表示氢,取代或未取代的低级烷基,低级烯基,卤素取代或未取代的低级 烷酰基或低级烷氧基羰基,X 1,X 2,Y 1和Y 2相同或不同,表示氢,卤素或低级烷基,X 1和X 2中的至少一个表示卤素或低级烷基,X 3表示氢,取代或未取代的低级烷基,低级 烯基,低级炔基,卤素,羟基,取代或未取代的低级烷氧基,NR5R6(其中R5和R6相同或不同,代表氢,或取代或未取代的低级烷基,或R5和R6一起形成含有 环中的氮原子),低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,羧基,低级烷氧基羰基,低级烷酰基,二唑基,氰基,取代或未取代的氨基甲酰基或低级烷硫基硫代 辛基或其药学上可接受的盐。
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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: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.
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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.
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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.
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公开(公告)号:US5248692A
公开(公告)日:1993-09-28
申请号:US24472
申请日:1993-03-01
IPC分类号: C07D487/04
CPC分类号: C07D487/04
摘要: Novel DC-89 derivatives as shown below have an excellent anti-tumor activity, and thus are useful as anti-tumor agent ##STR1## wherein L represents chlorine or bromine; R represents ##STR2## (wherein n represents an integer of 4 to 7) or ##STR3## (wherein Y represents oxygen or N--M).
摘要翻译: 如下所示的新型DC-89衍生物具有优异的抗肿瘤活性,因此可用作抗肿瘤剂(IMAGE),其中L代表氯或溴; R表示
(其中n表示4至7的整数)或 (其中Y表示氧或N-M)。 -
公开(公告)号:US5641780A
公开(公告)日:1997-06-24
申请号:US564178
申请日:1995-12-15
申请人: Nobuyoshi Amishiro , Satoru Nagamura , Hiromitsu Saito , Eiji Kobayashi , Akihiko Okamoto , Katsushige Gomi
发明人: Nobuyoshi Amishiro , Satoru Nagamura , Hiromitsu Saito , Eiji Kobayashi , Akihiko Okamoto , Katsushige Gomi
IPC分类号: C07D487/04 , A61K31/495
CPC分类号: C07D487/04
摘要: DC-89 derivatives represented by the formula ##STR1## wherein X represents CL or Br; R represents substituted or unsubstituted alkyl, substituted or unsubstituted aralkyl, COR.sup.1 or S.sub.2 OR.sup.7 ; and Y represents ##STR2## and pharmaceutically acceptable salts thereof. The compounds of the present invention exhibit excellent anti-tumor activity and are useful as anti-tumor agents.
摘要翻译: PCT No.PCT / JP95 / 00779 371 1995年12月15日第 102(e)1995年12月15日PCT PCT 1995年4月20日提交PCT公布。 公开号WO95 / 29179 日期为1995年11月2日,由式表示的取代或未取代的烷基,取代或未取代的芳烷基,COR1或S2OR7的DC-89衍生物; Y表示“IMAGE”或“IMAGE”及其药学上可接受的盐。 本发明的化合物表现出优异的抗肿瘤活性,可用作抗肿瘤剂。
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公开(公告)号:US5332740A
公开(公告)日:1994-07-26
申请号:US46365
申请日:1993-04-13
IPC分类号: C07D471/04 , A61K31/435 , A61K31/495 , C07D487/04
CPC分类号: C07D471/04
摘要: Novel DC-89 derivatives represented by general formula (I): ##STR1## wherein X represents Cl or Br; R.sup.1 represents hydrogen, CONR.sup.2 R.sup.3 (in which R.sup.2 and R.sup.3 independently represent hydrogen, a straight-chain or branched alkyl group having 1 to 4 carbon atoms or phenyl group), ##STR2## (in which n represents an integer of 4 to 7), ##STR3## (in which R.sup.4 represents oxygen, N--CH.sub.3 or N--CH.sub.2 CH.sub.2 NH.sub.2), ##STR4## (in which R.sup.5 R.sup.6 and R.sup.7 independently represent a straight-chain or branched alkyl group having 1 to 4 carbon atoms); and ##STR5## (in which Y represents hydrogen or CO.sub.2 CH.sub.3); provided that when R.sup.1 is hydrogen, CONR.sup.2 R.sup.3 or SiR.sup.5 R.sup.6 R.sup.7, ##STR6## and pharmaceutically acceptable salts thereof have an excellent anti-tumor activity and are expected to be useful as anti-tumor compositions.
摘要翻译: 由通式(I)表示的新型DC-89衍生物:其中X表示Cl或Br; R1表示氢,CONR2R3(其中R2和R3独立地表示氢,具有1至4个碳原子的直链或支链烷基或苯基),其中n表示4至7的整数, (其中R 4表示氧,N-CH 3或N-CH 2 CH 2 NH 2),其中R 5和R 7独立地表示碳原子数1〜4的直链或支链烷基。 和其中Y表示氢或CO 2 CH 3)。 条件是当R 1是氢时,CONR 2 R 3或SiR 5 R 6 R 7,其药学上可接受的盐具有优异的抗肿瘤活性,并且预期可用作抗肿瘤组合物。
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公开(公告)号:US5670492A
公开(公告)日:1997-09-23
申请号:US557055
申请日:1995-11-28
申请人: Nobuyoshi Amishiro , Satoru Nagamura , Hiromitsu Saito , Eiji Kobayashi , Akihiko Okamoto , Katsushige Gomi
发明人: Nobuyoshi Amishiro , Satoru Nagamura , Hiromitsu Saito , Eiji Kobayashi , Akihiko Okamoto , Katsushige Gomi
IPC分类号: C07D487/04 , C07D487/10 , A61K31/40 , A61K31/405 , A61K31/495
CPC分类号: C07D487/04 , C07D487/10
摘要: Provided are DC-89 derivatives represented by the formula: ##STR1## wherein X represents Cl or Br, R represents hydrogen or COR.sup.1, and W represents ##STR2## and pharmaceutically acceptable salts thereof. The compounds of the present invention have excellent anti-tumor activity and are useful as anti-tumor agents.
摘要翻译: PCT No.PCT / JP95 / 00626 Sec。 371日期:1995年11月28日 102(e)日期1995年11月28日PCT 1995年3月31日PCT PCT。 WO95 / 26964 PCT公开号 日期1995年10月12日提供了由下式表示的DC-89衍生物:其中X表示Cl或Br,R表示氢或COR1,W表示其药学上可接受的盐。 本发明的化合物具有优异的抗肿瘤活性,可用作抗肿瘤剂。
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