公开(公告)号：US06716831B1

公开(公告)日：2004-04-06

申请号：US09914788

申请日：2001-11-15

申请人： Gloria A. Breault ,  Stewart R. James ,  Janet E. Pease

发明人： Gloria A. Breault ,  Stewart R. James ,  Janet E. Pease

IPC分类号： A61K3133

CPC分类号： C07D403/04

摘要： A pyrimidine derivative of formula (I) or (I′): wherein: Rx is a substituent as defined within; Q1 is optionally substituted phenyl, and Q1 bears a substituent of formula (Ia) wherein: X, Y1, Y2, Z, n, and m are as defined within; —NQ2 is an optionally substituted heterocyclic moiety containing one hydrogen heteroatom and optionally containing a further heteroatom; or a pharmaceutically acceptable salt in vivo hydrolysable ester thereof; are useful as anti-cancer agents. Processes for their manufacture and pharmaceutical compositions containing them are described.

摘要翻译： 式（I）或（I'）的嘧啶衍生物：其中：R x是如下定义的取代基; Q1是任选取代的苯基，并且Q1具有式（Ia）的取代基，其中：X，Y 1，Y 2，Z，n和m如在其中所定义; -NQ2是含有一个氢原子并任选地含有另外的杂原子的任选取代的杂环部分; 或其药学上可接受的盐的体内可水解的酯; 可用作抗癌剂。 描述了其制备方法和含有它们的药物组合物。

公开(公告)号：US06670368B1

公开(公告)日：2003-12-30

申请号：US09958077

申请日：2001-10-04

申请人： Gloria A. Breault ,  Stewart R. James ,  Janet E. Pease

发明人： Gloria A. Breault ,  Stewart R. James ,  Janet E. Pease

IPC分类号： C07D23946

CPC分类号： C07D239/47

摘要： A pyrimidine derivative of formula (I) wherein V is O or S, Q1 and Q2 are independently selected from phenyl, naphthyl, a 5- or 6-membered monocyclic moiety and a 9- or 10-membered bicyclic heterocyclic moiety; and Q1 is substituted by one substituent of formula (Ia), and Q2 may optionally bear further substituents of formula (Ia) wherein X is CH2—, O—, NH—, NRy— or —S—[wherein Ry is as defined within]; Y1 is H, C1-4alkyl or as defined for Z; Y2 is H or C1-4alkyl; Z is RaO—, RbRcN—, RdS—, ReRfNNRg—, a nitrogen linked heteroaryl or a nitrogen linked heterocycle, wherein Ra, Rb, Rc, Rd, Re, Rf and Rg are as defined within; n is 1, 2 or 3; m is 1, 2 or 3; and Q1 and Q2 may optionally be further substituted; or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof; are useful as anti-cancer agents; and processes for their manufacture and pharmaceutical compositions containing them are described.

摘要翻译： 其中V是O或S，Q 1和Q 2的式（I）的嘧啶衍生物独立地选自苯基，萘基，5-或6-元单环部分和9-或10-元双环杂环部分; 并且Q 1被式（Ia）的一个取代基取代，并且Q 2可以任选地具有式（Ia）的其它取代基，其中X是CH 2 - ，O-，NH-，NR' - 或-S- [ y>如] Y 1是H，C 1-4烷基或如对Z所定义; Y 2是H或C 1-4烷基; Z是R a，R，R c，N，R d，R e R f N NN R g，氮连接的杂芳基或氮连接的杂环 其中R a，R b，R c，R d，R e，R f和R g如上所定义; n为1,2或3; m为1,2或3; 并且Q1和Q2可以任选地进一步被取代; 或其药学上可接受的盐或体内可水解的酯; 可用作抗癌剂; 并描述了其制造方法和含有它们的药物组合物。

公开(公告)号：US5554606A

公开(公告)日：1996-09-10

申请号：US329614

申请日：1994-10-26

申请人： Michael J. Betts ,  Gloria A. Breault

发明人： Michael J. Betts ,  Gloria A. Breault

IPC分类号： C07D477/20 ,  C07D487/04 ,  A61K31/40

CPC分类号： C07D477/20

摘要： The present invention provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are ortho with respect to one another wherein R.sup.3 and R.sup.4 are independently hydroxy or in vivo hydrolyzable esters thereof; the benzene ring being optionally further substituted; or a pharmaceutically acceptable salt or in vivo hydrolyzable ester thereof.

摘要翻译： 本发明提供式（I）化合物其中：R1是1-羟乙基，1-氟乙基或羟甲基; R2是氢或C1-4烷基; R3和R4相对于彼此是邻位的，其中R3和R4独立地是羟基或其体内可水解的酯; 苯环任选被进一步取代; 或其药学上可接受的盐或体内可水解的酯。

公开(公告)号：US5447925A

公开(公告)日：1995-09-05

申请号：US129148

申请日：1993-10-06

申请人： Michael J. Betts ,  Gloria A. Breault

发明人： Michael J. Betts ,  Gloria A. Breault

IPC分类号： C07D477/00 ,  A61K31/397 ,  A61K31/44 ,  A61P31/04 ,  C07D207/12 ,  C07D403/12 ,  C07D477/20 ,  C07F9/568 ,  C07D487/00 ,  A01N43/00 ,  A61K31/395

CPC分类号： C07D477/20 ,  C07D207/12 ,  C07D403/12 ,  C07F9/5683

摘要： The present invention provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;n is zero or an integer 1 to 4; andP is a benzene ring substituted by groups R.sup.3 and R.sup.4 which are ortho with respect to one another wherein R.sup.3 and R.sup.4 are independently hydroxy or in vivo hydrolysable esters thereof;or P is a group of the formula (II) or (III) ##STR2## wherein M is oxygen or a group NR.sup.5 wherein R.sup.5 is hydrogen or C.sub.1-4 alkyl;ring P being optionally further substituted;or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof.

摘要翻译： 本发明提供式（I）化合物其中：R1是1-羟乙基，1-氟乙基或羟甲基; R2是氢或C1-4烷基; n为0或整数1〜4; 并且P是被相对于彼此邻接的基团R3和R4取代的苯环，其中R3和R4独立地是羟基或其体内可水解的酯; 或者P是式（II）或（III）的基团，其中M是氧或基团NR5，其中R5是氢或C1-4烷基; 环P任选被进一步取代; 或其药学上可接受的盐或体内可水解的酯。