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1. 发明授权

US5977065A Bacterial nitroreductase for the reduction of CB1954 and analogues thereof to a cytotoxic form 失效
标题翻译：用于将CB1954及其类似物还原成细胞毒性形式的细菌硝基还原酶
公开(公告)号：US5977065A
公开(公告)日：1999-11-02
申请号：US87855
申请日：1998-06-01
申请人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
发明人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
IPC分类号： C12N9/12 , A61K38/00 , C07C219/34 , C07C271/18 , C07D203/14 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/02 , C12N15/00 , C12N15/09 , C12N15/53 , C12P17/10 , C12P21/08 , C12R1/01 , C12R1/07 , C12R1/19 , G01N33/53 , G01N33/573 , A61K38/12 , C07K5/00 , C07K7/00
CPC分类号： C07D203/14 , C07C219/34 , C07C271/18 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/0036 , C12P17/10 , C12Y101/01284 , A61K38/00 , Y02E50/16
摘要： A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R.sup.1 NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.2 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
摘要翻译：式（I）的前药：其中R1是使化合物R1NH2表示放线菌素D，多柔比星，丝裂霉素C或式（IV）的氮芥的基团：式（II）的前药：其中R 2 是化合物R 2 OH是酚氮芥的基团; 以及其中制备前述前药的方法，其中前药前体化合物与无水条件下的氯甲酸4-硝基苄酯反应。

2. 发明授权

US5958682A Bacterial nitroreductase gene-prodrug system 失效
标题翻译：细菌硝基还原酶基因前体药物系统
公开(公告)号：US5958682A
公开(公告)日：1999-09-28
申请号：US640808
申请日：1996-07-01
申请人： Thomas Connors , Richard Knox , Roger Sherwood
发明人： Thomas Connors , Richard Knox , Roger Sherwood
IPC分类号： C12N15/00 , A61K31/265 , A61K31/27 , A61K31/40 , A61K35/76 , A61K38/00 , A61K38/44 , A61K45/00 , A61K48/00 , A61P35/00 , A61P43/00 , C07H21/04 , C07K14/195 , C12N9/02 , C12N15/53 , C12N5/00
CPC分类号： C12N9/0036 , A61K38/44 , A01K2217/05 , A61K48/00
摘要： A system is disclosed which comprises: (i) a viral vector comprising a nucleotide sequence encoding a nitroreductase, which nitroreductase is capable of converting a prodrug into a cytotoxic drug; and (ii) a prodrug capable of being converted into a cytotoxic drug by the nitroreductase encoded by the vector. The disclosed invention also includes methods for killing cancerous and/or non-cancerous cells using the system described above. Included in the invention are methods for killing cells in vitro by introducing a vector encoding a nitroreductase into the cells, and then by providing a prodrug to the cells growing in vitro. Also included are methods in which cancerous and/or non-cancerous cells are killed in vivo in an animal or human by administering the vector and prodrug directly to cells of the animal or human. The invention further includes methods in which cancerous and/or non-cancerous cells are killed in vivo in an animal or human, by introducing a viral vector encoding a nitroreductase into animal or human cells growing in vitro so that the nitroreductase is produced in the cells, administering the cells to an animal or human subject, and then administering a prodrug to the animal or human, where it is converted into a cytotoxic agent in nitroreductase-containing cells of the animal or human.
摘要翻译： PCT No.PCT / GB94 / 02423 Sec。 371日期：1996年7月1日 102（e）日期1996年7月1日PCT 1994年11月4日PCT PCT。 WO95 / 12678 PCT出版物日期1995年5月11日公开了一种系统，其包括：（i）包含编码硝基还原酶的核苷酸序列的病毒载体，所述硝基还原酶能够将前药转化为细胞毒性药物; 和（ii）能够通过载体编码的硝基还原酶转化成细胞毒性药物的前药。所公开的发明还包括使用上述系统杀死癌和/或非癌细胞的方法。本发明包括通过将编码硝基还原酶的载体引入细胞，然后通过向体外生长的细胞提供前体来在体外杀死细胞的方法。还包括通过将该载体和前药直接施用于动物或人的细胞，在动物或人体内将癌和/或非癌细胞体内杀死的方法。本发明还包括通过将编码硝基还原酶的病毒载体引入体外生长的动物或人类细胞中，使动物或人体内杀死癌细胞和/或非癌细胞的方法，使得在细胞中产生硝基还原酶给动物或人类受试者施用细胞，然后向动物或人施用前体药物，在动物或人类的硝酸还原酶细胞中转化成细胞毒性剂。

3. 发明授权

US5633158A Bacterial nitroreductase for the reduction of CB 1954 and analogues thereof to a cytotoxic form 失效
标题翻译：用于将CB 1954及其类似物还原成细胞毒性形式的细菌硝基还原酶
公开(公告)号：US5633158A
公开(公告)日：1997-05-27
申请号：US232018
申请日：1994-07-27
申请人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger
发明人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger
IPC分类号： C12N9/12 , A61K38/00 , C07C219/34 , C07C271/18 , C07D203/14 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/02 , C12N15/00 , C12N15/09 , C12N15/53 , C12P17/10 , C12P21/08 , C12R1/01 , C12R1/07 , C12R1/19 , G01N33/53 , G01N33/573 , C07H21/04 , C12N1/20
CPC分类号： C07D203/14 , C07C219/34 , C07C271/18 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/0036 , C12P17/10 , C12Y101/01284 , A61K38/00 , Y02E50/16
摘要： The invention provides a nitroreductase, obtainable from a bacterium having the following characteristics as exemplified by examples isolated from Escherichia coli B and Bacillus amyloliquifaciens: 1) it is flavoprotein having a molecular weight in the range of 20-60 Kilodaltons; 2) it requires either NADH or NAD(P)H or analogues thereof as a cofactor; 3) it has a Km for NADH or NAD(P)H in the range of 1-100 .mu.M; and 4) it is capable of reducing either or both nitro groups of CB1954 and analogues thereof to a cytotoxic form e.g. the hydroxylamine. The sequence of one such nitroreductase is shown in Seq. ID No. 1. The nitroreductase may be conjugated to a tumor targeting agent such as a monoclonal antibody and used to convert prodrugs into active antitumor agents. Such prodrugs and drugs are also provided.
摘要翻译： PCT No.PCT / GB92 / 01947。 371日期：1994年7月27日 102（e）日期1994年7月27日PCT提交1992年10月23日PCT公布。公开号WO93 / 08288 日期：1993年04月29日本发明提供了可从具有以下特征的细菌获得的硝基还原酶，其特征如分离自大肠杆菌B和Bacillus amylolquifaciens的实施例所示：1）它是分子量在20-60千道尔顿范围内的黄素蛋白; 2）它需要NADH或NAD（P）H或其类似物作为辅因子; 3）其NADH或NAD（P）H的Km为1-100μM; 和4）它能够将CB1954的硝基和其类似物的一个或两个还原成细胞毒性形式，例如羟胺。一种这样的硝基还原酶的顺序示于Seq。硝基还原酶可以与肿瘤靶向剂如单克隆抗体缀合，并用于将前药转化为活性抗肿瘤剂。还提供了这些前药和药物。

4. 发明授权

US5780585A Bacterial nitroreductase for the reduction of CB 1954 and analogues thereof to a cytotoxic form 失效
标题翻译：用于将CB 1954及其类似物还原成细胞毒性形式的细菌硝基还原酶
公开(公告)号：US5780585A
公开(公告)日：1998-07-14
申请号：US504047
申请日：1995-06-07
申请人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
发明人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
IPC分类号： C12N9/12 , A61K38/00 , C07C219/34 , C07C271/18 , C07D203/14 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/02 , C12N15/00 , C12N15/09 , C12N15/53 , C12P17/10 , C12P21/08 , C12R1/01 , C12R1/07 , C12R1/19 , G01N33/53 , G01N33/573 , C07K7/56 , C07C68/00 , C07C69/96 , C07C269/04 , C07C271/28 , C07H15/24
CPC分类号： C07D203/14 , C07C219/34 , C07C271/18 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/0036 , C12P17/10 , C12Y101/01284 , A61K38/00 , Y02E50/16
摘要： A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R--NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.1 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
摘要翻译：式（I）的前药：其中R 1是使得化合物R-NH 2表示放线菌素D，多柔比星，丝裂霉素C或式（IV）的氮芥的基团：式（II）的前药：其中R 1是使化合物R 2 OH是酚氮芥的基团; 以及其中制备前述前药的方法，其中前药前体化合物与无水条件下的氯甲酸4-硝基苄酯反应。

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