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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
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.
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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。
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