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1. 发明授权

US5539112A 5-aminoflavone derivatives 失效
标题翻译： 5-氨基黄酮衍生物
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。

2. 发明授权

US5952355A Propenone derivatives 失效
标题翻译：丙烯醌衍生物
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。

3. 发明授权

US5220026A Pyrazoloacridone derivatives 失效
标题翻译：吡咯烷酮衍生物
公开(公告)号：US5220026A
公开(公告)日：1993-06-15
申请号：US793522
申请日：1991-11-18
申请人： Yukiteru Mimura , Yasushi Shida , Masaji Kasai , Tadashi Ashizawa , Katsushige Gomi
发明人： Yukiteru Mimura , Yasushi Shida , Masaji Kasai , Tadashi Ashizawa , Katsushige Gomi
IPC分类号： A61K31/47 , A61P35/00 , C07D471/06
CPC分类号： C07D471/06
摘要： Disclosed is pyrazoloacridone derivatives represented by formula (I): ##STR1## wherein: each of R.sup.1a, R.sup.1b, R.sup.1c and R.sup.1d independently represents hydrogen, lower alkyl, --(CH.sub.2).sub.p --Xwherein p represents an integer of 1 to 6, and X represents hydroxy, lower alkoxy or --NR.sup.2a R.sup.2bwherein each of R.sup.2a and R.sup.2b independently represents hydrogen, lower alkyl, or --(CH.sub.2).sub.m --Ywherein m represents an integer of 1 to 6, and Y represents hydroxy, lower alkoxy or --NR.sup.3a R.sup.3bwherein each of R.sup.3a and R.sup.3b independently represents hydrogen or lower alkylor --CH[(CH.sub.2).sub.n OH].sub.2wherein n represents an integer of 1 to 5; or a pharmaceutically acceptable salt thereof.

4. 发明授权

US5256685A Mitomycin derivatives 失效
标题翻译：丝裂霉素衍生物
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.

5. 发明授权

US5334611A 6-ethyl mitomycin derivatives 失效
标题翻译： 6-乙基丝裂霉素衍生物
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。

6. 发明授权

US5218126A Halogen substituted mitomycin derivatives 失效
标题翻译：卤素取代的咪唑啉衍生物
公开(公告)号：US5218126A
公开(公告)日：1993-06-08
申请号：US755528
申请日：1991-09-05
申请人： Hitoshi Arai , Masaji Kasai , Katsushige Gomi , Tadashi Ashizawa
发明人： Hitoshi Arai , Masaji Kasai , Katsushige Gomi , Tadashi Ashizawa
IPC分类号： C07D487/14
CPC分类号： C07D487/14
摘要： Disclosed are mitomycin derivatives of formula (I): ##STR1## where W represents halogen; X represents methoxy, amino or ethylenimino; Y represents hydrogen or methyl; Z represents hydrogen or methyl; and one of R.sup.1 and R.sup.2 represents carbamoyloxymethyl, and the other represents hydrogen. The derivatives are usable as an antitumor and antibacterial agent.

7. 发明授权

US5180825A Mitomycin derivatives 失效
标题翻译：麻醉药衍生物
公开(公告)号：US5180825A
公开(公告)日：1993-01-19
申请号：US791188
申请日：1991-11-13
申请人： Hitoshi Arai , Motomichi Kono , Masaji Kasai , Katsushige Gomi , Tadashi Ashizawa
发明人： Hitoshi Arai , Motomichi Kono , Masaji Kasai , Katsushige Gomi , Tadashi Ashizawa
IPC分类号： C07D487/14 , C07H15/26
CPC分类号： C07D487/14 , C07H15/26
摘要： Disclosed in a mitomycin derivative represented by the formula (I): ##STR1## wherein W is a heterocyclic group.

8. 发明授权

US5641780A Pyrrolo-indole derivatives 失效
标题翻译：吡咯 - 吲哚衍生物
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。

9. 发明授权

US5332740A DC-89 derivatives 失效
标题翻译： DC-89衍生物
公开(公告)号：US5332740A
公开(公告)日：1994-07-26
申请号：US46365
申请日：1993-04-13
申请人： Hiromitsu Saito , Satoru Nagamura , Akira Asai , Eiji Kobayashi , Katsushige Gomi
发明人： Hiromitsu Saito , Satoru Nagamura , Akira Asai , Eiji Kobayashi , Katsushige Gomi
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。

10. 发明授权

US5248692A DC-89 derivatives as anti-tumor agents 失效
标题翻译： DC-89衍生物作为抗肿瘤剂
公开(公告)号：US5248692A
公开(公告)日：1993-09-28
申请号：US24472
申请日：1993-03-01
申请人： Hiromitsu Saito , Akira Asai , Satoru Nagamura , Eiji Kobayashi , Katsushige Gomi
发明人： Hiromitsu Saito , Akira Asai , Satoru Nagamura , Eiji Kobayashi , Katsushige Gomi
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）。

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