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1. 发明申请

WO2007104944A1 PYRROLOPYRIMIDINE DERIVATIVES USED AS HSP90 INHIBITORS 审中-公开
标题翻译：用作HSP90抑制剂的吡咯烷酮衍生物
公开(公告)号：WO2007104944A1
公开(公告)日：2007-09-20
申请号：PCT/GB2007/000831
申请日：2007-03-09
申请人： VERNALIS (R & D) LTD. , BROUGH, Paul, Andrew , DRYSDALE, Martin, James , DAVIES, Nicholas, Gareth, Morse , FOLOPPE, Nicolas, Noel , STOKES, Stephan
发明人： BROUGH, Paul, Andrew , DRYSDALE, Martin, James , DAVIES, Nicholas, Gareth, Morse , FOLOPPE, Nicolas, Noel , STOKES, Stephan
IPC分类号： C07D487/04 , A61K31/517 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) have HSP90 inhibitory activity and are therefore useful in the treatment of, inter alia, cancer: Formula (I) wherein R i is hydrogen, fluoro, chloro, bromo, or a radical of formula -X-Alk 1 -(Z) m -(Alk 2 )n-Q wherein X is -O-, -S- -S(O)-, -SO 2 -, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO 2 -, -NR A -, or, in either orientation -C(=O)O-, -C(=O)NR A - , -C(=S)NR A -, -SO 2 NR A -, -NR A C(=O)-, or -NR A SO 2 - wherein R A is hydrogen or C 1 -C 6 alkyl AIk 1 and AIk 2 are optionally substituted divalent C 1 -C 3 alkylene or C 2 -C 3 alkenylene radicals, m, n and p are independently 0 or 1 , and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R 2 is a radical of formula -(Ar 1 ) p -(Alk 1 ) q -(Z) r -(Alk 2 ) s -Q wherein Ar 1 is an optionally substituted aryl or heteroaryl radical, Alk 1 , Alk 2 , Z, and Q are as defined above, and p, q, r and s are independently 0 or 1 ; and R 3 is cyano (-CN), fluoro, chloro, bromo, methyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, ethyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, cyclopropyl, -OH, -CH 2 OH, -C(O)NH 2 , -C(O)CH 3 , Or -NH 2 .
摘要翻译：式（I）化合物具有HSP90抑制活性，因此可用于治疗尤其是癌症：式（I）其中R 1是氢，氟，氯，溴或基团式（X-Alk）其中X是-O-，-S- - （Z）m - （Z）） - （Alk 2） S（O） - ， - SO 2 - 或-NH-，Z是-O - ， - S - ， - （C = O） - ， - （C = S）或者取代-C（= O）O - ， - C（= O） - ， - SO（O） - ， - SO 2 - -C（= S）NR A - ， - SO 2 - ， - NR 2 - ， - C（= O） - 或-NR A SO 2 - ，其中R A A是氢或 C 1 -C 6烷基，Alk 1和Alk 2是任选取代的二价C 1〜亚烷基或C 1 -C 3亚烷基，m，n和p独立地为0或1，并且Q为氢或任选取代的碳环或杂环基; R 2是下式的基团 - （Ar 1） - （Al 1）q（q） - （Z） - 其中Ar 1是（A 1）任选取代的芳基或杂芳基，Alk 1，Alk 2，Z和Q如上所定义，p，q，r和s独立地为0或1; 和R 3是氰基（-CN），氟，氯，溴，其中一个或多个氢原子任选被氟原子取代的甲基，其中一个或多个氢原子 -OH，-CH 2 OH，-C（O）NH 2，-C（O）CH 3，或-N 2 H 2。

2. 发明授权

EP2007767B1 PYRROLOPYRIMIDINE DERIVATIVES USED AS HSP90 INHIBITORS 有权
标题翻译： AS HSP90抑制剂一起使用PYRROLOPYRIMIDINDERIVATE
公开(公告)号：EP2007767B1
公开(公告)日：2011-11-02
申请号：EP07712872.6
申请日：2007-03-09
申请人： VERNALIS (R&D) LTD
发明人： BROUGH, Paul, Andrew , DRYSDALE, Martin, James , DAVIES, Nicholas, Gareth, Morse , FOLOPPE, Nicolas, Noel , STOKES, Stephan
IPC分类号： C07D487/04 , A61K31/517 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) have HSP90 inhibitory activity and are therefore useful in the treatment of, inter alia, cancer: Formula (I) wherein Ri is hydrogen, fluoro, chloro, bromo, or a radical of formula -X-Alk1-(Z)m-(Alk2)n-Q wherein X is -O-, -S- -S(O)-, -SO2-, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO2-, -NRA-, or, in either orientation -C(=O)O-, -C(=O)NRA- , -C(=S)NRA-, -SO2NRA-, -NRAC(=O)-, or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, n and p are independently 0 or 1 , and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is a radical of formula -(Ar1)p-(Alk1)q-(Z)r-(Alk2)s-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1, Alk2, Z, and Q are as defined above, and p, q, r and s are independently 0 or 1 ; and R3 is cyano (-CN), fluoro, chloro, bromo, methyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, ethyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, cyclopropyl, -OH, -CH2OH, -C(O)NH2, -C(O)CH3, Or -NH2.

3. 发明公开

EP2007767A1 PYRROLOPYRIMIDINE DERIVATIVES USED AS HSP90 INHIBITORS 有权
标题翻译：用作HSP90抑制剂的吡咯并嘧啶衍生物
公开(公告)号：EP2007767A1
公开(公告)日：2008-12-31
申请号：EP07712872.6
申请日：2007-03-09
申请人： VERNALIS (R&D) LTD
发明人： BROUGH, Paul, Andrew , DRYSDALE, Martin, James , DAVIES, Nicholas, Gareth, Morse , FOLOPPE, Nicolas, Noel , STOKES, Stephan
IPC分类号： C07D487/04 , A61K31/517 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) have HSP90 inhibitory activity and are therefore useful in the treatment of, inter alia, cancer: Formula (I) wherein Ri is hydrogen, fluoro, chloro, bromo, or a radical of formula -X-Alk1-(Z)m-(Alk2)n-Q wherein X is -O-, -S- -S(O)-, -SO2-, or -NH-, Z is -O-, -S-, -(C=O)-, -(C=S)-, -S(O)-, -SO2-, -NRA-, or, in either orientation -C(=O)O-, -C(=O)NRA- , -C(=S)NRA-, -SO2NRA-, -NRAC(=O)-, or -NRASO2- wherein RA is hydrogen or C1-C6 alkyl AIk1 and AIk2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, n and p are independently 0 or 1 , and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R2 is a radical of formula -(Ar1)p-(Alk1)q-(Z)r-(Alk2)s-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1, Alk2, Z, and Q are as defined above, and p, q, r and s are independently 0 or 1 ; and R3 is cyano (-CN), fluoro, chloro, bromo, methyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, ethyl in which in which one or more hydrogen atoms are optionally replaced by fluorine atoms, cyclopropyl, -OH, -CH2OH, -C(O)NH2, -C(O)CH3, Or -NH2.
摘要翻译：式（I）化合物具有HSP90抑制活性，因此可用于治疗癌症：其中R 1为氢，氟，氯，溴或式-X-Alk1-（ Z）m-（Alk2）nQ其中X是-O - ， - S-S（O） - ， - SO2-或-NH-，Z是-O-，-S - ， - （C = O）（= O）N - ， - C（= O）N RA - ， - C （= S）N RA - ， - SO 2 NR A - ， - NR C（= O） - 或-NR A SO 2 - ，其中RA是氢或C 1 -C 6烷基，Alk 1和Alk 2是任选取代的二价C 1 -C 3亚烷基或C 2 -C 3亚烯基， m，n和p独立地为0或1，Q为氢或任选取代的碳环或杂环基; R2是式 - （Ar1）p-（Alk1）q-（Z）r-（Alk2）sQ的基团，其中Ar1是任选取代的芳基或杂芳基，Alk1，Alk2，Z和Q如上所定义，并且p，q，r和s独立地为0或1; 和R 3是氰基（-CN），氟，氯，溴，其中一个或多个氢原子任选被氟原子取代的甲基，其中一个或多个氢原子任选被氟原子取代的乙基，，-OH，-CH 2 OH，-C（O）NH 2，-C（O）CH 3或-NH 2。

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