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1. 发明授权

US06465522B1 Anthraquinone anticancer drugs 失效
标题翻译：蒽醌类抗癌药
公开(公告)号：US06465522B1
公开(公告)日：2002-10-15
申请号：US09868956
申请日：2001-11-07
申请人： Gerard Andrew Potter , Laurence Hylton Patterson , Paul Teesdale-Spittle , Zennia Paniwynk
发明人： Gerard Andrew Potter , Laurence Hylton Patterson , Paul Teesdale-Spittle , Zennia Paniwynk
IPC分类号： A61K31135
CPC分类号： A61K47/55 , A61K47/54
摘要： A molecule of formula (I); wherein: X is a halogen, or a substituted sulfonate group; m=1-5; n=1-5; R1, R2=H, C1-4 lower alkyl or C1-4 lower alkyl chain having additional functionality; and the amino group −NR1R2 linked to the anthraquinone is primary, secondary or tertiary or is a tertiary group in the N-oxide form having the formula —N(O)R1R2.
摘要翻译：式（I）的分子;其中：X是卤素或取代的磺酸酯基; m = 1-5; n = 1-5; R 1，R 2 = H，C 1-4低级烷基或C 1-4低级烷基链具有附加功能; 与蒽醌连接的氨基-NR1R2是伯，仲或叔或是具有式-N（O）R 1 R 2的N-氧化物形式的叔基。

2. 发明授权

US06468753B1 Anthraquinone and its derivatives 有权
标题翻译：蒽醌及其衍生物
公开(公告)号：US06468753B1
公开(公告)日：2002-10-22
申请号：US09719863
申请日：2001-02-20
申请人： Paul James Smith , Laurence Hylton Patterson
发明人： Paul James Smith , Laurence Hylton Patterson
IPC分类号： C12Q168
CPC分类号： G01N33/52 , C07C225/36 , C09B1/5155
摘要： There is disclosed a compound of formula (I) wherein each of X1 and X2 are independently NH—A—NR1R2, and wherein A is A C2-8 alkylene group and R1 and R2 are independently selected from hydrogen, C1-4 alkyl, C2-4 hydroxy-alkyl and C2-4 aminoalkyl, or R1 and R2 together form a C2-6 alkylene group which with the nitrogen atom to which R1 and R2 are attached forms a heterocyclic ring, or an N-oxide derivative thereof, and wherein the compound (I) or its N-oxide derivative is optionally in the form of an acid salt derived from an organic or inorganic acid. Also disclosed is a method of its production and its uses, including its use in analyzing a cell or biological material and detecting the emitted fluorescence signal.
摘要翻译：公开了式（I）化合物，其中X1和X2各自独立地为NH-A-NR1R2，其中A为A C2-8亚烷基，R1和R2独立地选自氢，C1-4烷基，C2 -4-羟基 - 烷基和C 2-4氨基烷基，或者R 1和R 2一起形成与R 1和R 2所连接的氮原子一起形成杂环的C 2-6亚烷基或其N-氧化物衍生物，其中化合物（I）或其N-氧化物衍生物任选为衍生自有机或无机酸的酸盐形式。还公开了其生产方法及其用途，包括其用于分析细胞或生物材料并检测发出的荧光信号。

3. 发明授权

US08017640B2 Benz-indole and benzo-quinoline derivatives as prodrugs for tumor treatment 有权
标题翻译：苯并吲哚和苯并喹啉衍生物作为肿瘤治疗的前药
公开(公告)号：US08017640B2
公开(公告)日：2011-09-13
申请号：US11710899
申请日：2007-02-27
申请人： Mark Searcey , Laurence Hylton Patterson
发明人： Mark Searcey , Laurence Hylton Patterson
IPC分类号： A61K31/4035 , A61K31/4185 , A61K31/4188
CPC分类号： A61K31/47 , A61K31/403 , C07D209/60
摘要： Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which C is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors. The prodrug is expected to be activated preferentially in tumor cells, which it will act as a DNA alkylating agent preventing cell division.
摘要翻译：其中X为H，Y为离去基团的通式（I）或（IA）化合物，R1优选为芳族DNA结合亚基，为杜卡霉素的前药类似物。化合物预期在C连接的碳原子上被细胞色素P450特别是CYP1B1羟化，在肿瘤中以高水平表达。预期前体药物在肿瘤细胞中优先被活化，其将用作防止细胞分裂的DNA烷基化剂。

4. 发明授权

US07557215B2 Anthraquinone compounds as anti cancer compounds 失效
标题翻译：蒽醌化合物作为抗癌化合物
公开(公告)号：US07557215B2
公开(公告)日：2009-07-07
申请号：US10596783
申请日：2004-12-22
申请人： Laurence Hylton Patterson , Klaus Pors , Paul Henry Teesdale-Spittle
发明人： Laurence Hylton Patterson , Klaus Pors , Paul Henry Teesdale-Spittle
IPC分类号： C07D211/00 , C07D207/04
CPC分类号： C07D207/08 , C07D207/06 , C07D207/10 , C07D207/12 , C07D207/46 , C07D211/18 , C07D211/22 , C07D211/38 , C07D211/46 , C07D211/94
摘要： Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (R5)2 in which R0 is a C1-12 alkanediyl and each R5 is H or optionally substituted C1-4 alkyl, and a group of formula (II) in which at least one of R6, R7 and R8 is selected from X2, and X2 substituted C1-4 alkyl and any others are H or C1-4 alkyl; R9 is selected from H, C1-4 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C1-6 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives. The amine compounds are cytotoxic and may be used as alkylating agents having topoisomerase II inhibiting activities in cancer therapy.
摘要翻译：通式（I）的蒽醌化合物或其盐（式I）其中R 1至R 4各自选自H，C 1-4烷基，X 1，-NHRO N（R 5）2，其中R 0为 C 1-12烷二基，每个R 5为H或任选取代的C 1-4烷基，以及其中R 6，R 7和R 8中的至少一个选自X 2，以及X 2取代的C 1-4烷基和任何其余为H或C 1-4烷基; R 9选自H，C 1-4烷基，X 2和X 2取代的C 1-4烷基; m为0或1; n为1或2; X1是卤素原子，羟基，C1-6烷氧基，芳氧基或酰氧基; X2是卤素原子，羟基，C1-6烷氧基，芳氧基或酰氧基; 条件是R 1至R 4中的至少一个为式（II）的基团。 N-氧化物是有用的前药，其在缺氧肿瘤中选择性地生物还原成相应的环胺衍生物。胺化合物是细胞毒性的，并且可以用作在癌症治疗中具有拓扑异构酶II抑制活性的烷化剂。

5. 发明授权

US09051467B2 Method of analysing a cell or other biological material containing a nucleic acid 有权
标题翻译：分析含有核酸的细胞或其他生物材料的方法
公开(公告)号：US09051467B2
公开(公告)日：2015-06-09
申请号：US13639872
申请日：2011-04-08
申请人： Paul James Smith , Rachel J. Errington , Laurence Hylton Patterson
发明人： Paul James Smith , Rachel J. Errington , Laurence Hylton Patterson
IPC分类号： C12Q1/68 , C09B1/16 , C09K11/06 , G01N1/30 , C09B1/20
CPC分类号： G01N1/30 , C09B1/16 , C09B1/207 , C09K11/06 , C09K2211/1011 , C12Q1/68 , G01N33/582 , G01N2001/302
摘要： According to the invention there is provided a compound of Formula (I) in which: A is a C2-8 alkylene group; R1, R2, R3, and R4 are independently selected from hydrogen, C1-4 alkyl, C2-4 dihydroxyalkyl in which the carbon atom attached to the nitrogen atom does not carry a hydroxyl group and no carbon atom is substituted by two hydroxyl groups, or R2 and R3 together form a C2-6 alkylene group which with the nitrogen atom to which R2 and R3 are attached forms a heterocyclic ring; X1, X2 and X3 are independently selected from hydrogen, hydroxyl, NR1-A-NR2R3R4+(Zm−)1/m, halogeno amino, C1-4 alkoxy or C2-8 alkanoyloxy; and (Zm−)1/m is an anion of charge m; or a derivative in which the group NR1 is quaternarised.
摘要翻译：根据本发明，提供式（I）的化合物，其中：A是C 2-8亚烷基; R 1，R 2，R 3和R 4独立地选自氢，C1-4烷基，C2-4二羟基烷基，其中与氮原子连接的碳原子不携带羟基，没有碳原子被两个羟基取代，或者R 2和R 3一起形成与R2和R3所连接的氮原子一起形成杂环的C 2-6亚烷基; X1，X2和X3独立地选自氢，羟基，NR1-A-NR2R3R4 +（Zm-）1 / m，卤代氨基，C1-4烷氧基或C2-8烷酰氧基; 和（Zm-）1 / m是电荷m的阴离子; 或NR1为季铵化的衍生物。

6. 发明申请

US20080027107A1 Antharquinone Compounds as Anti Cancer Compounds 失效
标题翻译：蒽醌化合物作为抗癌化合物
公开(公告)号：US20080027107A1
公开(公告)日：2008-01-31
申请号：US10596783
申请日：2004-12-22
申请人： Laurence Hylton Patterson , Klaus Pors , Paul Henry Teesdale-Spittle
发明人： Laurence Hylton Patterson , Klaus Pors , Paul Henry Teesdale-Spittle
IPC分类号： A61K31/445 , A61K31/40 , A61P35/00 , C07D207/08 , C07D207/10 , C07D211/18 , C07D211/22 , C07D211/38 , C07D211/94
CPC分类号： C07D207/08 , C07D207/06 , C07D207/10 , C07D207/12 , C07D207/46 , C07D211/18 , C07D211/22 , C07D211/38 , C07D211/46 , C07D211/94
摘要： Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (Rs)2 in which R° is a C1l12 alkanediyl and each R5 is H or optionally substituted C14 alkyl, and a group of formula (11) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C14 alkyl; R9 is selected from H, C14 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1.6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C16 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives. The amine compounds are cytotoxic and may be used as alkylating agents having topoisomerase II inhibiting activities in cancer therapy.
摘要翻译：通式（I）的蒽醌化合物或其盐（式I）其中R 1至R 4各自分别选自H，C < 其中R 1是C 1 ，其中R 1是C 1 H 2，烷二基和每个R 5是H或任选取代的C 14-14烷基，和式（11）的基团，其中至少 R 6，R 7和R 8中的一个选自X 2，X 2，取代的C 1-4烷基，任何其它的是H或C 14烷基; R 9选自H，C 1-4烷基，X 2和X 2取代的C 1 -C 4烷基， 1-4烷基; m为0或1; n为1或2; X 1是卤素原子，羟基，C 1 -C 6烷氧基，芳氧基或酰氧基; X 2是卤素原子，羟基，C 1〜6烷氧基，芳氧基或酰氧基; 条件是R 1至R 4中的至少一个为式（II）的基团。 N-氧化物是有用的前药，其在缺氧肿瘤中选择性地生物还原成相应的环胺衍生物。胺化合物是细胞毒性的，并且可以用作在癌症治疗中具有拓扑异构酶II抑制活性的烷化剂。

7. 发明授权

US07074835B2 Formulations of anthraquinone derivatives 失效
标题翻译：蒽醌衍生物的配方
公开(公告)号：US07074835B2
公开(公告)日：2006-07-11
申请号：US10507483
申请日：2003-03-17
申请人： William Alexander Denny , Laurence Hylton Patterson , Gavin William Halbert , Steven John Ford
发明人： William Alexander Denny , Laurence Hylton Patterson , Gavin William Halbert , Steven John Ford
IPC分类号： C07C291/04 , A61K47/02 , A61K47/12 , A61P35/00
CPC分类号： C07C225/36 , A61K9/0019 , A61K47/02 , A61K47/12 , C07C291/04 , C07C2603/24
摘要： A compound of formula (I): in which A is a C alkylene group with a chain length between NH and N(O)R′R″ of at least 2 carbon atoms and R′ and R″ are each separately selected from C1-4 alkyl groups and C2-4 hydroxyalkyl and C2-4 dihydroxyalkyl groups, or R′ and R″ together are a C2-6 alkylene group, is formulated so that upon dissolution in aqueous solution the pH of the solution is in the range of 5 to 9. The compound may be in the form of salt with a physiologically acceptable acid having a pKa in the range of −3.0 (minus 3.0) to 9.0
摘要翻译：式（I）化合物：其中A是具有NH和至少2个碳原子的N（O）R'R“之间的链长的C亚烷基，R'和R”分别选自 C 1-4烷基和C 2-4 2-4羟基烷基和C 2-4 2-4羟基烷基，或者R'和R“一起是配制C 2-6亚烷基，使得当溶解在水溶液中时，溶液的pH在5至9的范围内。该化合物可以是与生理学上的盐的形式具有-3.0（减3.0）至9.0范围内的pK 的可接受的酸

8. 发明授权

US07626026B2 Pyrrolo-indole and pyrrolo-quinoline derivatives as prodrugs for tumour treatment 有权
标题翻译：吡咯并吲哚和吡咯并喹啉衍生物作为肿瘤治疗的前药
公开(公告)号：US07626026B2
公开(公告)日：2009-12-01
申请号：US10468741
申请日：2002-02-22
申请人： Mark Searcey , Laurence Hylton Patterson
发明人： Mark Searcey , Laurence Hylton Patterson
IPC分类号： C07D487/06 , C07D487/02 , A61K31/407
CPC分类号： A61K31/407 , C07D471/04 , C07D487/04
摘要： Compounds of the general formula (I) or (IA) in which X is H, Y is a leaving group, R1 and optionally also R3 preferably being an aromatic DNA binding subunit are prodrug analogues of duocarmycin. The compounds are expected to be hydroxylated at the carbon atom to which X is joined, by cytochrome P450, in particular by CYP1B1, expressed at high levels in tumors. The prodrug is expected to be activated preferentially in tumor cells, where it will act as a DNA alkylating agent preventing cell division.
摘要翻译：其中X是H，Y是离去基团的通式（I）或（IA）的化合物，R 1和任选地也可以是R3优选是芳族DNA结合亚基的化合物是杜卡霉素的前药类似物。化合物预期在X连接的碳原子上被细胞色素P450特别是CYP1B1羟化，在肿瘤中以高水平表达。预期前体药物优先在肿瘤细胞中活化，其中它将用作防止细胞分裂的DNA烷基化剂。

9. 发明申请

US20130101994A1 Method of Analysing a Cell or Other Biological Material Containing a Nucleic Acid 有权
标题翻译：分析含有核酸的细胞或其他生物材料的方法
公开(公告)号：US20130101994A1
公开(公告)日：2013-04-25
申请号：US13639872
申请日：2011-04-08
申请人： Paul James Smith , Rachel J. Errington , Laurence Hylton Patterson
发明人： Paul James Smith , Rachel J. Errington , Laurence Hylton Patterson
IPC分类号： C09B1/16 , C09B1/20 , C12Q1/68
CPC分类号： G01N1/30 , C09B1/16 , C09B1/207 , C09K11/06 , C09K2211/1011 , C12Q1/68 , G01N33/582 , G01N2001/302
摘要： According to the invention there is provided a compound of Formula (I) in which: A is a C2-8 alkylene group; R1, R2, R3, and R4 are independently selected from hydrogen, C1-4 alkyl, C2-4 dihydroxyalkyl in which the carbon atom attached to the nitrogen atom does not carry a hydroxyl group and no carbon atom is substituted by two hydroxyl groups, or R2 and R3 together form a C2-6 alkylene group which with the nitrogen atom to which R2 and R3 are attached forms a heterocyclic ring; X1, X2 and X3 are independently selected from hydrogen, hydroxyl, NR1-A-NR2R3R4+(Zm−)1/m, halogeno amino, C1-4 alkoxy or C2-8 alkanoyloxy; and (Zm−)1/m is an anion of charge m; or a derivative in which the group NR1 is quaternarised.
摘要翻译：根据本发明，提供式（I）的化合物，其中：A是C 2-8亚烷基; R 1，R 2，R 3和R 4独立地选自氢，C1-4烷基，C2-4二羟基烷基，其中与氮原子连接的碳原子不携带羟基，没有碳原子被两个羟基取代，或者R 2和R 3一起形成与R2和R3所连接的氮原子一起形成杂环的C 2-6亚烷基; X1，X2和X3独立地选自氢，羟基，NR1-A-NR2R3R4 +（Zm-）1 / m，卤代氨基，C1-4烷氧基或C2-8烷酰氧基; 和（Zm-）1 / m是电荷m的阴离子; 或NR1为季铵化的衍生物。

10. 发明授权

US07605280B2 Anthraquinone and its derivatives 有权
标题翻译：蒽醌及其衍生物
公开(公告)号：US07605280B2
公开(公告)日：2009-10-20
申请号：US11367328
申请日：2006-03-06
申请人： Paul James Smith , Laurence Hylton Patterson
发明人： Paul James Smith , Laurence Hylton Patterson
IPC分类号： C09B1/16 , C12Q1/00 , C12Q1/68 , A01N33/24
CPC分类号： G01N33/52 , C07C225/36 , C09B1/5155
摘要： There is disclosed a compound of formula (I) wherein each of X1 and X2 are independently NH-A-NR1R2, and wherein A is A C2-8 alkylene and R1 and R2 are independently selected from hydrogen, C1-4 alkyl, C2-4 hydroxy-alkyl and C2-4 aminoalkyl, or R1 and R2 together form a C2-6 alkylene group which with the nitrogen atom to which R1 and R2 are attached forms a heterocyclic ring, or an N-oxide derivative thereof, and wherein the compound (I) or its N-oxide derivative is optionally in the form of an acid salt derived from an organic or inorganic acid. Also disclosed is a method of its production and its uses, including its use in analyzing a cell or biological material and detecting the emitted fluorescence signal.
摘要翻译：公开了式（I）的化合物，其中X1和X2各自独立地为NH-A-NR1R2，其中A为A C2-8亚烷基，R1和R2独立地选自氢，C1-4烷基，C2- 4个羟基 - 烷基和C 2-4氨基烷基，或者R 1和R 2一起形成与R 1和R 2所连接的氮原子一起形成杂环的C 2-6亚烷基或其N-氧化物衍生物，其中化合物（I）或其N-氧化物衍生物任选为衍生自有机或无机酸的酸盐形式。还公开了其生产方法及其用途，包括其用于分析细胞或生物材料并检测发出的荧光信号。

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