公开(公告)号：US20060205027A1

公开(公告)日：2006-09-14

申请号：US11373623

申请日：2006-03-09

Applicant: Ivan King ,  Xu Lin

Inventor： Ivan King ,  Xu Lin

IPC: C12Q1/48 ,  C07H19/16

CPC classification number: C12Q1/48 ,  G01N2333/91245

Abstract: This invention provides a method to determine alkylguanyltransferase activity in a sample, comprising steps of placing the sample in an appropriate condition so that the AGT is functional; contacting the sample with an AGT Detector under conditions permitting the binding of AGT and AGTD to produce a signal; and measuring the signal, thereby determining the AGT activity in said sample. This invention provides different uses of this method.

Abstract translation: 本发明提供了一种测定样品中烷基泛酰基转移酶活性的方法，包括以下步骤：将样品置于适当的条件下，使得AGT具有功能; 在允许AGT和AGTD结合产生信号的条件下将样品与AGT检测器接触; 并测量信号，从而确定所述样品中的AGT活性。 本发明提供了该方法的不同用途。

公开(公告)号：US06458816B1

公开(公告)日：2002-10-01

申请号：US09977659

申请日：2001-10-15

Applicant: Terrence W. Doyle ,  Srinivasa Karra ,  Zujin Li ,  Xu Lin ,  John Mao ,  Qi Qiao ,  Yang Xu

Inventor： Terrence W. Doyle ,  Srinivasa Karra ,  Zujin Li ,  Xu Lin ,  John Mao ,  Qi Qiao ,  Yang Xu

IPC: C07D21302

CPC classification number: C07D213/75 ,  A61K31/407 ,  A61K31/44 ,  A61K31/47 ,  A61K31/675 ,  A61K31/70 ,  A61K31/704 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  A61K47/52 ,  C07F9/58 ,  A61K31/195 ,  A61K2300/00

Abstract: The present invention relates to compounds according to the structure: Where R is H or CH3; R2 is phosphate which can be free acid or salt; R3 is H, F, Cl, Br, I, OCH3, OCF3 , CF3 or a C1-C3 alkyl group; R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3; and R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3, with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H which may be used to treat neoplasia, including cancer.

Abstract translation: 本发明涉及以下结构的化合物：其中R是H或CH 3; R 2是可以是游离酸或盐的磷酸酯; R 3是H，F，Cl，Br，I，OCH 3，OCF 3，CF 3或C 1 -C 3 烷基; R 4是H，F，Cl，Br，I，OCH 3，OCF 3或CF 3; R 5和R 6各自独立地为H，F，Cl，Br，I，OCH 3，OCF 3或CF 3，条件是当R 3，R 4，R 5或R 6中的任何两个不同于H时， R5或R6是H，其可以用于治疗包括癌症在内的肿瘤。

公开(公告)号：US20080076132A1

公开(公告)日：2008-03-27

申请号：US11856909

申请日：2007-09-18

Applicant: Ivan King ,  Xu Lin

Inventor： Ivan King ,  Xu Lin

IPC: C12Q1/68 ,  C07D473/30 ,  G01N33/53 ,  C07D473/34

CPC classification number: C12Q1/48 ,  G01N2333/91245

Abstract: This invention provides a method to determine alkylguanyltransferase activity in a sample, comprising steps of placing the sample in an appropriate condition so that the AGT is functional; contacting the sample with an AGT Detector under conditions permitting the binding of AGT and AGTD to produce a signal; and measuring the signal, thereby determining the AGT activity in said sample. This invention provides different uses of this method.

Abstract translation: 本发明提供了一种测定样品中烷基泛酰基转移酶活性的方法，包括以下步骤：将样品置于适当的条件下，使得AGT具有功能; 在允许AGT和AGTD结合产生信号的条件下将样品与AGT检测器接触; 并测量信号，从而确定所述样品中的AGT活性。 本发明提供了该方法的不同用途。

公开(公告)号：US07273714B2

公开(公告)日：2007-09-25

申请号：US11373623

申请日：2006-03-09

Applicant: Ivan C. King ,  Xu Lin

Inventor： Ivan C. King ,  Xu Lin

IPC: C12Q1/48 ,  G01N33/53

CPC classification number: C12Q1/48 ,  G01N2333/91245

Abstract: This invention provides a method to determine alkylguanyltransferase activity in a sample, comprising steps of placing the sample in an appropriate condition so that the AGT is functional; contacting the sample with an AGT Detector under conditions permitting the binding of AGT and AGTD to produce a signal; and measuring the signal, thereby determining the AGT activity in said sample. This invention provides different uses of this method.

Abstract translation: 本发明提供了一种测定样品中烷基泛酰基转移酶活性的方法，包括以下步骤：将样品置于适当的条件下，使得AGT具有功能; 在允许AGT和AGTD结合产生信号的条件下将样品与AGT检测器接触; 并测量信号，从而确定所述样品中的AGT活性。 本发明提供了该方法的不同用途。

公开(公告)号：US20060089332A1

公开(公告)日：2006-04-27

申请号：US11232252

申请日：2005-09-21

Applicant: Xu Lin ,  Ivan King ,  Michael Belcourt ,  Terrence Doyle

Inventor： Xu Lin ,  Ivan King ,  Michael Belcourt ,  Terrence Doyle

IPC: A61K31/675 ,  C07F9/58 ,  C07F9/28

CPC classification number: C07F9/12 ,  C07F9/6518

Abstract: Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formulas I, II, III and IV. Pharmaceutical compositions and uses thereof in the treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. Where R=C1-10 alkyl, or C1-10 haloalkyl (preferably containing no more than 5 halogen groups, preferably 2-chloroethyl); R′ and R″ are independently C1-10 alkyl, or C5-20 aryl or heteroaryl (preferably methyl); R1 is H, C1-10 alkyl, C1-10 alkoxyl, C5-20 aryl or heteroaryl or C5-20 aroxyl or heteroaroxyl (preferably methyl and ethyl); X is O, NH, or NR (preferably O); Y is (CH2)n, O(CH2)n, NH(CH2)n, NR(CH2)n, OCOO(CH2)n, NHCOO(CH2)n; n is 1, 2, 3, 4 or 5 (preferably n=2 and 3); or Y=aryl or heteroaryl (preferably para-phenyl); A=CH, or N (preferably CH); and B=CH═CH, O, S, NH, or NR (preferably CH═CH); or pharmaceutically acceptable salts, solvates, polymorphs or metabolites, thereof.

Abstract translation: 磺酰肼的新型含磷酸酯前药具有式I，II，III和IV。 要求保护药物组合物及其在治疗癌症中的用途。 前述药物包括对映异构体，立体异构体和互变异构体，以及来自所有阶段的药学上可接受的盐或溶剂合物和代谢物。 上述前药优先在缺氧性肿瘤中活化，并且可以单独给予，也可以与其它抗癌剂或光疗法或放疗相结合。 其中R = C 1-10烷基或C 1-10 1-10卤代烷基（优选含有不超过5个卤素基团，优选2-氯乙基）; R'和R“独立地为C 1-10烷基或C 5-20-20芳基或杂芳基（优选甲基）; R 1是H，C 1-10烷基，C 1-10烷氧基，C 5-20-20芳基 或杂芳基或C 5-20芳基或杂芳基（优选甲基和乙基）; X是O，NH或NR（优选O）; Y（CH 2）n，O（CH 2）n，NH（CH 2） NR（CH 2）n，OCOO（CH 2）2，N（CH 2）n， nCO 2，NHCOO（CH 2 CH 2）n N; n为1,2,3,4或5（优选n = 2和3）; 或Y =芳基或杂芳基（优选对苯基）; A = CH或N（优选CH）; 和B = CH-CH，O，S，NH或NR（优选CH-CH）; 或其药学上可接受的盐，溶剂合物，多晶型物或代谢物。

公开(公告)号：US06855695B2

公开(公告)日：2005-02-15

申请号：US10461282

申请日：2003-06-13

Applicant: Xu Lin ,  Terrence W. Doyle ,  Ivan King

Inventor： Xu Lin ,  Terrence W. Doyle ,  Ivan King

IPC: A61K38/04 ,  A61K38/16 ,  C07C311/55 ,  C07F9/12 ,  A61K38/00

CPC classification number: C07C311/55 ,  A61K38/04 ,  A61K38/16 ,  C07F9/12

Abstract: The present invention relates to compounds according to the structure (I): Where R is —CH3 or —CH2CH2Cl; R′ is C1-C7 alkyl or —CH2CH2Cl; R2 or R4 is OPO3H2, NO2, OCO(Glu-OH), NHCO(Glu-OH), NHR7 and unassigned groups of R2, R3, R4, R5 and R6 are, independently H, F, Cl, Br, I, OH, OPO3H2, OCH3, CF3, OCF3, NO2, CN, SO2CH3, SO2CF3, COCH3, COOCH3, SCH3, SF5, NH2, NHR7, N(CH3)2, OPO3H2, or a C1-C7 alkyl group with the proviso that when any two of unassigned groups of R2, R3, R4, R5 or R6 are other than H, the other two of unassigned groups of R2, R3, R4, R5 or R6 are H. R7 is H or polyglutamyl as described. Phosphoric acid and glutamic acid can be a free acid or pharmaceutically acceptable salt thereof.

Abstract translation: 本发明涉及根据结构（I）的化合物：其中R是-CH 3或-CH 2 CH 2 Cl; R'是C 1 -C 7烷基或-CH 2 CH 2 Cl; R2或R4是OPO3H2，NO2，OCO（Glu-OH），NHCO（Glu-OH），NHR7，R2，R3，R4，R5和R6的未分配基团独立地是H，F，Cl，Br，I，OH ，OPO3H2，OCH3，CF3，OCF3，NO2，CN，SO2CH3，SO2CF3，COCH3，COOCH3，SCH3，SF5，NH2，NHR7，N（CH3）2，OPO3H2或C1-C7烷基，条件是当任何 R2，R3，R4，R5或R6中的两个未分配的基团不是H，R2，R3，R4，R5或R6的其他两个未分配的基团是H.R 7是H或如所述的聚谷氨酰基。 磷酸和谷氨酸可以是游离酸或其药学上可接受的盐。