公开(公告)号：US20080145372A1

公开(公告)日：2008-06-19

申请号：US11663469

申请日：2005-09-26

申请人： Peter David Davis ,  Matthew Alexander Naylor ,  Peter Thomson ,  Steven Albert Everett ,  Michael Richard Lacey Stratford ,  Peter Wardman

发明人： Peter David Davis ,  Matthew Alexander Naylor ,  Peter Thomson ,  Steven Albert Everett ,  Michael Richard Lacey Stratford ,  Peter Wardman

IPC分类号： A61K39/395 ,  C07H19/09 ,  A61K31/7068 ,  A61P35/00 ,  A61K31/7052 ,  A61P19/02 ,  A61K38/44

CPC分类号： C07H19/20 ,  C07H19/06 ,  C07H19/10 ,  C07H19/16

摘要： The present invention relates to a compound of formula (1), or a pharmaceutically acceptable salt thereof, Formula: (1); wherein: R1 is a substituted aryl or heteroaryl group bearing at least one nitro or azido group or is an optionally substituted benzoquinone, optionally substituted naphthoquinone or optionally substituted fused heterocycloquinone: R2 is H, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, aryl or heteroaryl; and R3 is selected such that R3NH2 represents a cytotoxic nucleoside analogue or an ester or phosphate ester prodrug of a cytotoxic nucleoside analogue, with the proviso that if R1 is an aryl group then R2 is not H.

摘要翻译： 本发明涉及式（1）化合物或其药学上可接受的盐，式（1）; 其中：R1是带有至少一个硝基或叠氮基的取代的芳基或杂芳基，或任选被取代的苯醌，任选取代的萘醌或任选取代的稠合的杂环醌：R2是H，任选取代的烷基，任选取代的烯基，任选取代的炔基， 任选取代的环烷基，任选取代的杂环烷基，芳基或杂芳基; 并且选择R3，使得R3NH2表示细胞毒性核苷类似物或细胞毒性核苷类似物的酯或磷酸酯前药，条件是如果R 1是芳基，则R 2不是H.

公开(公告)号：US5659048A

公开(公告)日：1997-08-19

申请号：US447463

申请日：1995-05-23

申请人： Vladimir Genukh Beylin ,  Anthony Denver Sercel ,  Howard Daniel Hollis Showalter ,  Gerald Edward Adams ,  Edward Martin Fielden ,  Matthew Alexander Naylor ,  Ian James Stratford

发明人： Vladimir Genukh Beylin ,  Anthony Denver Sercel ,  Howard Daniel Hollis Showalter ,  Gerald Edward Adams ,  Edward Martin Fielden ,  Matthew Alexander Naylor ,  Ian James Stratford

IPC分类号： A61K31/415 ,  A61P43/00 ,  C07D233/91 ,  C07D403/06 ,  C07D413/06 ,  C07F7/18 ,  C07D233/54

CPC分类号： C07D403/06 ,  C07D233/91 ,  C07D413/06

摘要： Chiral compounds useful as radiosensitizers or chemosensitizers having the formula ##STR1## wherein X is halogen or ##STR2## intermediates used to prepare these compounds, and a novel process to prepare these compounds are described.

摘要翻译： 描述了用作放射增敏剂或具有式（IMAGE）的化学敏化剂的手性化合物，其中X是用于制备这些化合物的卤素或中间体，以及制备这些化合物的新方法。

公开(公告)号：US20090202571A1

公开(公告)日：2009-08-13

申请号：US11663495

申请日：2005-09-26

申请人： Peter David Davis ,  Matthew Alexander Naylor ,  Peter Thomson ,  Steven Albert Everett ,  Michael Richard Lacey Stratford ,  Peter Wardman

发明人： Peter David Davis ,  Matthew Alexander Naylor ,  Peter Thomson ,  Steven Albert Everett ,  Michael Richard Lacey Stratford ,  Peter Wardman

IPC分类号： A61K39/395 ,  C07H17/04 ,  A61K31/7028 ,  A61K38/44 ,  A61K31/7052 ,  A61P35/00

CPC分类号： C07D493/04 ,  A61K31/381 ,  A61K45/06 ,  A61K2300/00

摘要： A compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: —Ar is a substituted heteroaryl group bearing at least one nitro or azido group or is a benzoquinone, naphthoquinone or fused heterocyloquinone; -R1 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; -R2 is a glycoside, OH, optionally substituted alkyl, optionally substituted alkoxy, C2-C8 alkenyl, C1-C8 hydroxyalkyl, optionally substituted arylamino, optionally substituted aryl C1-C4 alkylamino or hydroxyalkylamino; and -R3 and R4 are each independently H or halo.

摘要翻译： 式（1）化合物或其药学上可接受的盐，其中：-Ar为带有至少一个硝基或叠氮基的取代杂芳基，或为苯醌，萘醌或稠合异喹啉醌; -R1是氢，任选取代的烷基，任选取代的烯基，任选取代的炔基，任选取代的环烷基，任选取代的杂环烷基，任选取代的芳基或任选取代的杂芳基; -R2是糖苷，OH，任选取代的烷基，任选取代的烷氧基，C 2 -C 8烯基，C 1 -C 8羟烷基，任选取代的芳基氨基，任选取代的芳基C 1 -C 4烷基氨基或羟烷基氨基; 且R 3和R 4各自独立地为H或卤素。