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1. 发明授权

US06277880B1 Chemical compounds 有权
标题翻译：化合物
公开(公告)号：US06277880B1
公开(公告)日：2001-08-21
申请号：US09314894
申请日：1999-05-19
申请人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
发明人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
IPC分类号： A61K3127
CPC分类号： C07D257/04 , A61K47/6899 , B82Y5/00 , C07C237/20 , C07C271/54 , C07C275/24 , C07C275/40 , C07C309/66 , C07C311/51
摘要： Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.
摘要翻译：通用型I的前药被公开用于抗体定向酶前药治疗（ADEPT）。前药是羧肽酶G2（CPG2）的底物，并且比已知的CPG2催化反应产物产生更多的活性细胞毒性药物。

2. 发明授权

US5958971A Chemical compounds 失效
公开(公告)号：US5958971A
公开(公告)日：1999-09-28
申请号：US956008
申请日：1997-10-22
申请人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
发明人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
IPC分类号： A61K31/17 , A61K31/195 , A61K31/27 , A61K31/41 , A61K39/395 , A61K45/00 , A61K47/48 , A61P35/00 , A61P43/00 , C07C237/20 , C07C237/40 , C07C269/04 , C07C271/54 , C07C275/24 , C07C275/40 , C07C275/42 , C07C309/66 , C07C309/69 , C07C309/72 , C07C311/51 , C07C317/50 , C07C323/58 , C07D257/04 , A01N47/10
CPC分类号： C07D257/04 , A61K47/48761 , B82Y5/00 , C07C237/20 , C07C271/54 , C07C275/24 , C07C275/40 , C07C309/66 , C07C311/51
摘要： Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.

3. 发明授权

US5714148A Chemical compounds 失效
标题翻译：化合物
公开(公告)号：US5714148A
公开(公告)日：1998-02-03
申请号：US722669
申请日：1996-09-30
申请人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
发明人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
IPC分类号： A61K31/17 , A61K31/195 , A61K31/27 , A61K31/41 , A61K39/395 , A61K45/00 , A61K47/48 , A61P35/00 , A61P43/00 , C07C237/20 , C07C237/40 , C07C269/04 , C07C271/54 , C07C275/24 , C07C275/40 , C07C275/42 , C07C309/66 , C07C309/69 , C07C309/72 , C07C311/51 , C07C317/50 , C07C323/58 , C07D257/04 , C07C261/00 , C07F9/02 , C07K16/00
CPC分类号： C07D257/04 , A61K47/48761 , B82Y5/00 , C07C237/20 , C07C271/54 , C07C275/24 , C07C275/40 , C07C309/66 , C07C311/51
摘要： Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.
摘要翻译：通用型I的前药被公开用于抗体定向酶前药治疗（ADEPT）。前药是羧肽酶G2（CPG2）的底物，并且比CPG2催化反应的已知产物产生更多的活性细胞毒性药物。

4. 发明授权

US5660829A Process for antibody directed enzyme prodrug therapy 失效
标题翻译：抗体定向酶前药治疗方法
公开(公告)号：US5660829A
公开(公告)日：1997-08-26
申请号：US442348
申请日：1995-05-16
申请人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger
发明人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger
IPC分类号： A61K31/17 , A61K31/195 , A61K31/27 , A61K31/41 , A61K39/395 , A61K45/00 , A61K47/48 , A61P35/00 , A61P43/00 , C07C237/20 , C07C237/40 , C07C269/04 , C07C271/54 , C07C275/24 , C07C275/40 , C07C275/42 , C07C309/66 , C07C309/69 , C07C309/72 , C07C311/51 , C07C317/50 , C07C323/58 , C07D257/04 , C07C261/00 , C07F9/02 , C07K16/00
CPC分类号： C07D257/04 , A61K47/48761 , B82Y5/00 , C07C237/20 , C07C271/54 , C07C275/24 , C07C275/40 , C07C309/66 , C07C311/51
摘要： Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalysed reactions.
摘要翻译：通用型I的前药被公开用于抗体定向酶前药治疗（ADEPT）。前药是羧肽酶G2（CPG2）的底物，并且比已知的CPG2催化反应产物产生更多的活性细胞毒性药物。

5. 发明授权

US08415334B2 Method of combating infection 失效
标题翻译：抗感染方法
公开(公告)号：US08415334B2
公开(公告)日：2013-04-09
申请号：US11991080
申请日：2006-09-04
申请人： Philip John Burke , Roger Melton , Richard John Knox
发明人： Philip John Burke , Roger Melton , Richard John Knox
IPC分类号： A61K31/33
CPC分类号： A61K31/396 , Y02A50/409 , Y02A50/414 , Y02A50/488
摘要： Method of combating a parasitic protozoal infection of a host organism, wherein the parasite causing the infection is associated with an enzyme system capable of activating tretazicar into a cytotoxic form. The method is carried out by administering tretazicar to the host organism.
摘要翻译：抵抗宿主生物体的寄生性原虫感染的方法，其中引起感染的寄生虫与能够将赖氨酸转化为细胞毒性形式的酶系统相关联。该方法通过对宿主生物体施用噻托他汀来进行。

6. 发明申请

US20100273762A1 Method of combating infection 失效
标题翻译：抗感染方法
公开(公告)号：US20100273762A1
公开(公告)日：2010-10-28
申请号：US11991080
申请日：2006-09-04
申请人： Philip John Burke , Roger Melton , Richard John Knox
发明人： Philip John Burke , Roger Melton , Richard John Knox
IPC分类号： A61K31/396 , C07D203/04 , A61P33/02
CPC分类号： A61K31/396 , Y02A50/409 , Y02A50/414 , Y02A50/488
摘要： A method of combating a parasitic protozoal infection of a host organism, the method comprising administering tretazicar to the host organism. Tretazicar is the compound 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB 1954), and the parasitic infection is preferably an infection of Trypanosoma cruzi, T. b. brucei, Leishmania spp. particularly L. infantum, Cryptosporidium or Giardia spp.
摘要翻译：一种抵抗宿主生物体的寄生原虫感染的方法，所述方法包括向所述宿主生物体施用噻托他汀。 Tretazicar是5-（吖啶啶-1-基）-2,4-二硝基苯甲酰胺（CB 1954）的化合物，寄生虫感染优选为克氏锥虫感染T. 布鲁斯，利什曼原虫属特别是婴幼儿，隐孢子虫或贾第虫属。

7. 发明授权

US07138122B2 Therapeutic systems 失效
公开(公告)号：US07138122B2
公开(公告)日：2006-11-21
申请号：US10099830
申请日：2002-03-13
申请人： Philip John Burke , Richard John Knox
发明人： Philip John Burke , Richard John Knox
IPC分类号： A01N43/00 , A61K31/33
CPC分类号： C12N9/0036 , A61K31/455 , A61K38/00 , A61K47/6815 , A61K47/6899 , A61K48/005 , B82Y5/00 , C07K2319/74
摘要： A compound comprising a target cell-specific portion and human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug, or a polynucleotide encoding said NQO2 or said variant or fragment or fusion or derivative. A recombinant polynucleotide comprising a target cell-specific promoter operably linked to a polynucleotide encoding human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug. The compounds and polynucleotides are useful in a method of treating a patient in conjunction with a suitable prodrug. A method of treating a human patient with a target cell to be destroyed wherein the target cell expresses NQO2 the method comprising administering to the patient a prodrug which is converted to a substantially cytotoxic drug by the action of NQO2 and nicotinamide riboside (reduced) (NRH) or an analogue thereof which can pass reducing equivalents to NQO2.

8. 发明授权

US06867231B1 Therapeutic systems 失效
标题翻译：治疗系统
公开(公告)号：US06867231B1
公开(公告)日：2005-03-15
申请号：US09445865
申请日：1998-06-15
申请人： Philip John Burke , Richard John Knox
发明人： Philip John Burke , Richard John Knox
IPC分类号： C12N15/09 , A61K31/455 , A61K31/711 , A61K45/00 , A61K47/22 , A61K47/48 , A61K48/00 , A61P35/00 , A01N47/10 , A01N43/00 , A61K31/785
CPC分类号： C12N9/0036 , A61K31/455 , A61K38/00 , A61K47/6815 , A61K47/6899 , A61K48/005 , B82Y5/00 , C07K2319/74
摘要： A compound comprising a target cell-specific portion and human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug, or a polynucleotide encoding said NQO2 or said variant or fragment or fusion or derivative. A recombinant polynucleotide comprising a target cell-specific promoter operably linked to a polynucleotide encoding human NAD(P)H:quinone reductase 2 (NQO2) or a variant or fragment or fusion or derivative thereof which has substantially the same activity as NQO2 towards a given prodrug. The compounds and polynucleotides are useful in a method of treating a patient in conjunction with a suitable prodrug. A method of treating a human patient with a target cell to be destroyed wherein the target cell expresses NQO2 the method comprising administering to the patient a prodrug which is converted to a substantially cytotoxic drug by the action of NQO2 and nicotinamide riboside (reduced) (NRH) or an analogue thereof which can pass reducing equivalents to NQO2.
摘要翻译：包含目标细胞特异性部分和人NAD（P）H：醌还原酶2（NQO2）或其与NQO2具有与给定前药基本相同的活性的变体或片段或融合物或衍生物的化合物或编码所述NQO2或所述变体或片段或融合物或衍生物。一种重组多核苷酸，其包含与编码人NAD（P）H：醌还原酶2（NQO2）的多核苷酸或其变体或片段或融合物或衍生物可操作地连接的靶细胞特异性启动子，其与NQO2具有基本相同的活性前药。化合物和多核苷酸可用于与合适的前药联合治疗患者的方法。一种用待破坏的靶细胞治疗人类患者的方法，其中靶细胞表达NQO2，该方法包括向患者施用通过NQO2和烟酰胺核苷（还原）（NRH）的作用将其转化为基本上细胞毒性药物的前药）或其类似物，其可以通过还原当量到NQO 2。

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