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1. 发明授权

US5571914A 4-desoxy-4-epipodophyllotoxin derivative or pharmaceutically acceptable salt thereof 失效
标题翻译： 4-脱氧-4-表鬼臼毒素衍生物或其药学上可接受的盐
公开(公告)号：US5571914A
公开(公告)日：1996-11-05
申请号：US466733
申请日：1995-06-06
申请人： Tadafumi Terada , Katsuhiko Fujimoto , Makoto Nomura , Junichi Yamashita , Setsuo Takeda , Takashi Kobunai , Hideo Yamaguchi , Konstanty Wierzba
发明人： Tadafumi Terada , Katsuhiko Fujimoto , Makoto Nomura , Junichi Yamashita , Setsuo Takeda , Takashi Kobunai , Hideo Yamaguchi , Konstanty Wierzba
IPC分类号： A61K31/34 , A61K31/357 , A61K31/365 , A61P35/00 , C07D493/04 , C07D413/00 , C07D407/00
CPC分类号： C07D493/04
摘要： A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.
摘要翻译：下式（R）的4-脱氧-4-表鬼臼毒素衍生物，其中R和R 1如本说明书中所定义，或其药学上可接受的盐，以及包含该衍生物或盐作为活性成分的抗肿瘤组合物。

2. 发明授权

US5536847A 4-desoxy-4-epipodophyllotoxin derivative or pharmaceutically acceptable salt thereof 失效
公开(公告)号：US5536847A
公开(公告)日：1996-07-16
申请号：US471524
申请日：1995-06-06
申请人： Tadafumi Terada , Katsuhiko Fujimoto , Makoto Nomura , Junichi Yamashita , Setsuo Takeda , Takashi Kobunai , Hideo Yamaguchi , Konstanty Wierzba
发明人： Tadafumi Terada , Katsuhiko Fujimoto , Makoto Nomura , Junichi Yamashita , Setsuo Takeda , Takashi Kobunai , Hideo Yamaguchi , Konstanty Wierzba
IPC分类号： A61K31/34 , A61K31/357 , A61K31/365 , A61P35/00 , C07D493/04 , C07D407/00 , C07D307/77
CPC分类号： C07D493/04
摘要： A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.

3. 发明授权

US5489698A 4-Desoxy-4-epipodophyllotoxin derivative or pharmaceutically acceptable salt thereof 失效
标题翻译： 4-脱氧-4-表鬼臼毒素衍生物或其药学上可接受的盐
公开(公告)号：US5489698A
公开(公告)日：1996-02-06
申请号：US375565
申请日：1995-01-13
申请人： Tadafumi Terada , Katsuhiko Fujimoto , Makoto Nomura , Junichi Yamashita , Setsuo Takeda , Takashi Kobunai , Hideo Yamaguchi , Konstanty Wierzba
发明人： Tadafumi Terada , Katsuhiko Fujimoto , Makoto Nomura , Junichi Yamashita , Setsuo Takeda , Takashi Kobunai , Hideo Yamaguchi , Konstanty Wierzba
IPC分类号： A61K31/34 , A61K31/357 , A61K31/365 , A61P35/00 , C07D493/04
CPC分类号： C07D493/04
摘要： A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.
摘要翻译：下式（R）的4-脱氧-4-表鬼臼毒素衍生物，其中R和R 1如本说明书中所定义，或其药学上可接受的盐，以及包含该衍生物或盐作为活性成分的抗肿瘤组合物。

4. 发明授权

US5420117A 5-substituted uridine derivatives 失效
标题翻译： 5-取代的尿苷衍生物
公开(公告)号：US5420117A
公开(公告)日：1995-05-30
申请号：US963250
申请日：1992-10-19
申请人： Tadafumi Terada , Katsuhiko Fujimoto , Junichi Yamashita , Mitsugi Yasumoto , Setsuo Takeda , Junji Uchida , Konstanty Wierzba , Yuji Yamada
发明人： Tadafumi Terada , Katsuhiko Fujimoto , Junichi Yamashita , Mitsugi Yasumoto , Setsuo Takeda , Junji Uchida , Konstanty Wierzba , Yuji Yamada
IPC分类号： C07H19/06 , C07H23/00 , A61K31/505
CPC分类号： C07H23/00 , C07H19/06
摘要： This invention provides a 5-substituted uridine derivative of the formula ##STR1## wherein X is F or CF.sub.3, R.sub.1 and R.sub.2 each represent a group --OSi--(R.sub.4)(R.sub.5)(R.sub.6) (wherein R.sub.4, R.sub.5 and R.sub.6 represent C.sub.1 -C.sub.10 alkyl or the like), OH, aminoacyloxy group wherein the amino group may be substituted with lower alkyl group or carboxylalkylcarbonyloxy group, R.sub.3 is a group --OSi(R.sub.4)(R.sub.5)(R.sub.6), H, OH, aminoacyloxy group wherein the amino group may be substituted with lower alkyl group, or carboxylalkylcarbonyloxy group, and at least one of R.sub.1, R.sub.2 and R.sub.3 is a group --OSi--(R.sub.4)(R.sub.5)(R.sub.6), with the proviso that when X is fluorine atom, R.sub.3 is not hydrogen, and an intermediate for the preparation thereof, preparation processes of the derivative and anti-tumor agent containing the derivative as an active ingredient.
摘要翻译：本发明提供了下式的5-取代的尿苷衍生物，其中X是F或CF 3，R 1和R 2各自表示-OSi-（R 4）（R 5）（R 6）（其中R 4，R 5和R 6表示C1 -C 10烷基等），OH，其中氨基可被低级烷基或羧基烷基羰基氧基取代的氨基酰氧基，R3是基团-OSi（R4）（R5）（R6），H，OH，氨基酰氧基，其中氨基可以被低级烷基或羧基烷基羰基氧基取代，R 1，R 2和R 3中的至少一个是-OSi-（R 4）（R 5）（R 6）基团，条件是当X是氟原子时， R3不是氢，其制备中间体，衍生物的制备方法和含有该衍生物的抗肿瘤剂作为活性成分。

5. 发明授权

US5750515A Cancer metastasis inhibitor 失效
标题翻译：癌转移抑制剂
公开(公告)号：US5750515A
公开(公告)日：1998-05-12
申请号：US737799
申请日：1996-11-26
申请人： Jiro Shibata , Konstanty Wierzba , Koji Murakami , Yuji Yamada , Koichi Shudo
发明人： Jiro Shibata , Konstanty Wierzba , Koji Murakami , Yuji Yamada , Koichi Shudo
IPC分类号： A61K31/192 , A61K31/196 , A61K31/695 , A61P35/04 , A61K31/19 , A61K31/20
CPC分类号： A61K31/695 , A61K31/192 , A61K31/196
摘要： The present invention relates to a cancer metastasis inhibitor comprising a benzoic acid derivative as an active ingredient represented by the formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each represents hydrogen atom, hydroxyl group or trimethylsilyl group, or R.sub.3 and R.sub.4 are bonded to each other to form a tetramethylene group substituted with lower alkyl group, and X represents group --COCH.dbd.C(OH)--, group --NHCO-- or group --CONH--, provided that when R.sub.3 and R.sub.4 are bonded to each other to form a tetramethylene group substituted with lower alkyl group, X is group --COCH.dbd.C(OH)-- or group --CONH--, use of the benzoic acid derivative for preparing the cancer metastasis inhibitor and method of inhibiting cancer metastasis, characterized in that an effective amount of the benzoic acid derivative is administered to a mammalian animal for inhibiting metastasis of cancer. The benzoic acid derivative represented by the above formula (I) has extremely good metastasis inhibiting properties.
摘要翻译： PCT No.PCT / JP96 / 00980 Sec。 371日期1996年11月26日 102（e）1996年11月26日PCT PCT 1996年4月10日PCT公布。第WO96 / 32101号公报日期：1996年10月17日本发明涉及包含苯甲酸衍生物作为由式（I）表示的活性成分的癌症转移抑制剂，其中R1，R2，R3和R4相同或不同，各自表示氢原子，羟基或三甲基甲硅烷基，或者R 3和R 4相互键合形成被低级烷基取代的四亚甲基，X表示-COCH = C（OH） - 基团，-NHCO-或基团 -CONH-，条件是当R 3和R 4彼此键合以形成被低级烷基取代的四亚甲基时，X是基团-COCH = C（OH） - 或基团-CONH-，使用苯甲酸衍生物制备癌转移抑制剂和抑制癌转移的方法，其特征在于向哺乳动物施用有效量的苯甲酸衍生物以抑制癌转移。上述式（I）表示的苯甲酸衍生物具有极好的转移抑制性质。

6. 发明授权

US06255314B1 Cancerous metastasis inhibitors containing uracil derivatives 失效
标题翻译：含有尿嘧啶衍生物的癌转移抑制剂
公开(公告)号：US06255314B1
公开(公告)日：2001-07-03
申请号：US09077209
申请日：1998-05-26
申请人： Kazutaka Miyadera , Tomohiro Emura , Konstanty Wierzba , Yuji Yamada
发明人： Kazutaka Miyadera , Tomohiro Emura , Konstanty Wierzba , Yuji Yamada
IPC分类号： A61K31513
CPC分类号： A61K31/505 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K31/55 , C07D239/553
摘要： This invention provides a drug which has inhibitory activities against thymidine phosphorylase and inhibits metastasis of a cancer. Specifically, this invention relates to a cancerous metastasis inhibitor comprising, as an active ingredient, a uracil derivative represented by the following formula (1): wherein R1 represents a chlorine, bromine or iodine atom or a cyano or lower alkyl group and R2 represents a substituted or unsubstituted 4-8 membered hetero-cyclic group having nitrogen atoms or a substituted or unsubstituted amidinothio, guanidino, (lower alkyl)amidino, amino or like group, or a salt thereof.
摘要翻译：本发明提供了对胸苷磷酸化酶具有抑制活性并抑制癌转移的药物。具体而言，本发明涉及含有作为活性成分的下述式（1）所示的尿嘧啶衍生物的癌性转移抑制剂，其中R1表示氯，溴或碘原子或氰基或低级烷基，R2表示取代或未取代的具有氮原子的4-8元杂环基或取代或未取代的脒基硫代，胍基，（低级烷基）脒基，氨基或类似基团或其盐。

7. 发明授权

US07192763B2 Streptomyces anulatus microorganism and a process for producing the substance GM-95 失效
标题翻译：链霉菌属微生物和生产物质GM-95的方法
公开(公告)号：US07192763B2
公开(公告)日：2007-03-20
申请号：US10401589
申请日：2003-03-31
申请人： Haruo Seto , Kazuo Shin-Ya , Konstanty Wierzba
发明人： Haruo Seto , Kazuo Shin-Ya , Konstanty Wierzba
IPC分类号： C12N1/20 , C12P17/18
CPC分类号： C12P17/185 , C07D513/00 , C07D513/22
摘要： A compound which has the following formula (1), a process for its production, a pharmaceutical composition comprising the compound as an active ingredient, a method of treating tumor which comprises administering the compound, use of the compound as a medicine, and a microorganism capable of producing the compound. The compound of the present invention is a novel compound which has antitumor action and is useful as a medicine.
摘要翻译：具有下式（1）的化合物，其制备方法，包含该化合物作为活性成分的药物组合物，治疗肿瘤的方法，其包括给予化合物，使用该化合物作为药物和微生物能够生产化合物。本发明化合物是具有抗肿瘤作用的新化合物，可用作药物。

8. 发明授权

US06613759B1 Substance GM-95, process for producing the same and utilization thereof 失效
标题翻译：物质GM-95，其制备方法及其应用
公开(公告)号：US06613759B1
公开(公告)日：2003-09-02
申请号：US09806475
申请日：2001-04-09
申请人： Haruo Seto , Kazuo Shin-Ya , Konstanty Wierzba
发明人： Haruo Seto , Kazuo Shin-Ya , Konstanty Wierzba
IPC分类号： A61K3133
CPC分类号： C12P17/185 , C07D513/00 , C07D513/22
摘要： A compound which has the following formula (1), a process for its production, a pharmaceutical composition comprising the compound as an active ingredient, a method of treating tumor which comprises administering the compound, use of the compound as a medicine, and a microorganism capable of producing the compound. The compound of the present invention is a novel compound which has antitumor action and is useful as a medicine.
摘要翻译：具有下式（1）的化合物，其制备方法，包含该化合物作为活性成分的药物组合物，治疗肿瘤的方法，其包括给予化合物，使用该化合物作为药物和微生物能够生产化合物。本发明化合物是具有抗肿瘤作用的新化合物，可用作药物。

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