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1. 发明授权

US08716287B2 Pharmaceutical compounds 有权
标题翻译：药物化合物
公开(公告)号：US08716287B2
公开(公告)日：2014-05-06
申请号：US13697743
申请日：2011-05-12
申请人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
发明人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
IPC分类号： A61K31/535 , C07D241/00
CPC分类号： C07D241/26 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61N5/10 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12
摘要： A compound of the formula (I):
摘要翻译：式（I）的化合物：

2. 发明申请

US20090247538A1 Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors 有权
标题翻译：正电子缩合吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：US20090247538A1
公开(公告)日：2009-10-01
申请号：US11577963
申请日：2005-10-25
申请人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
IPC分类号： A61K31/52 , C07D473/34 , C07D487/04 , A61K31/519 , C12N9/99 , C12Q1/48
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR5; J1-J2 is N═C(R6), (R7)C═N, (R8)N—C(O), (R8)2C—C(O), N═N or (R7)C═C(R6); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q1 is a bond or a saturated C1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRq or NRqCO where Rq is hydrogen or methyl, or Rq is a C1-4 alkylene chain linked to R1 or a carbon atom of Q1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q2 is other than a bond; G is hydrogen, NR2R, OH or SH provided that when E is aryl or heteroaryl and Q2 is a bond, then G is hydrogen; R1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R1 is hydrogen and G is NR2R3, then Q2 is a bond; and R2, R3, R4, R6 and R8 are as defined in the claims.
摘要翻译：本发明提供用作蛋白激酶B抑制剂的化合物，该化合物为式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或CR 5; J1-J2是N-C（R6），（R7）C-N，（R8）N-C（O），（R8）2C-C（O），N-N或（R7）C-C（R6） E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q1是键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选被氧或氮原子代替，或者相邻的一对碳原子可被CONRq或NRqCO代替，其中Rq 是氢或甲基，或Rq是与R1或Q1的碳原子连接的C 1-4亚烷基链，形成环状部分; 并且其中所述连接基团Q1的碳原子可任选地具有一个或多个选自氟和羟基的取代基; Q2是含有1至3个碳原子的键或饱和烃连接基团，其中连接基团中的一个碳原子可任选被氧或氮原子取代; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q2不是键; G为氢，NR2R，OH或SH，条件是当E为芳基或杂芳基且Q2为键时，则G为氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢且G是NR 2 R 3时，则Q2是一个键; 并且R 2，R 3，R 4，R 6和R 8如权利要求中所定义。

3. 发明申请

US20080275029A1 Compounds for Treating Protein-Kinase Mediated Disorders 审中-公开
公开(公告)号：US20080275029A1
公开(公告)日：2008-11-06
申请号：US11718943
申请日：2005-11-09
申请人： Valerio Berdini , Robert George Boyle , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Hannah Fiona Sore , David Winter Walker , John Caldwell , Ian Collins
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Hannah Fiona Sore , David Winter Walker , John Caldwell , Ian Collins
IPC分类号： A61K31/517 , C07D239/88 , C07D401/12 , C07D401/04 , A61K31/496 , A61K31/551 , A61P35/00 , C12N5/06 , A61K31/5377 , C07D401/06 , C07D403/12 , C07D413/14
CPC分类号： C07D403/12 , A61K31/505 , C07D239/88 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B; wherein the ring Q is a benzene ring; J2-J1 is N═CR7 or R1aN—CO; G is OH or NR5R6; E is CONR7, NR7CO, C(R8)═C(R8) or (X)m(CR8R8a)n where X is O, S or NR7; provided that when J2-J1 is R1aN—CO, E is other than NR7CO; m and n are each 0 or 1, where m+n=1 or 2; A is a bond and R4 and R4a are absent or A is a saturated optionally substituted C1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N; R1, R1a, R2, and R3 are each H; halogen; C1-6 hydrocarbyl optionally substituted by halogen, OH or C1-2 alkoxy; CN; CONHR8; NH2; NHCOR10 or NHCONHR10; R4 is H or C1-4 alkyl; R4a is H, C1-4 alkyl or a group R9; R5 and R6 are each selected from H, R9 and C1-4 hydrocarbyl optionally substituted by halogen, C1-2 alkoxy or R9; or NR5R6 forms a saturated 4-7 membered monocyclic heterocyclic group; R7 is H or C1-4 alkyl; R8 and R8a each H or saturated C1-4 hydrocarbyl optionally substituted by fluorine; R9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R4, R4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR5R6, R4 and A form a saturated 4-7 membered monocyclic heterocycle; or R4, together with R7 or R8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR5R6 and R7 or R8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R10 is optionally substituted phenyl or benzyl.

4. 发明申请

US20130005702A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 失效
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：US20130005702A1
公开(公告)日：2013-01-03
申请号：US13536174
申请日：2012-06-28
申请人： Valerio BERDINI , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio BERDINI , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/415 , C07D401/10 , A61K31/451 , A61K31/4439 , C12N5/09 , A61K31/5377 , A61K31/4155 , C07D403/10 , A61K31/551 , A61P35/00 , C07D231/12 , C07D413/10
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译：本发明提供具有蛋白激酶B抑制活性的式（I）化合物：还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

5. 发明授权

US08716473B2 Substituted benzotriazines and quinoxalines as inhibitors of P7OS6 kinase 有权
标题翻译：取代的苯并三嗪和喹喔啉作为P7OS6激酶的抑制剂
公开(公告)号：US08716473B2
公开(公告)日：2014-05-06
申请号：US13322775
申请日：2010-05-26
申请人： Robert George Boyle , David Winter Walker
发明人： Robert George Boyle , David Winter Walker
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , A61K31/53 , A61K31/498 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D409/14
摘要： The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O−); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.
摘要翻译：本发明提供式（1）化合物或其盐或互变异构体; 其中X1是N或N +（O-）; X2是N或CH; Q为C1-3亚烷基; R 1选自氢，C 1-4烃基和羟基-C 2-4烃基; R2，R3和R4相同或不同，各自选自氢，氟，氯和甲基; Ar1是任选取代的含有0,1或2个选自O，N和S的杂原子环成员或萘环的单环5或6元芳基或杂芳环，Ar 2是任选取代的单环5或6元杂芳基环含有1,2或3个选自O，N和S的杂原子环成员。式（1）化合物是p70S6激酶的抑制剂，可用于治疗增殖性疾病。

6. 发明授权

US08461339B2 Pharmaceutical compounds 有权
标题翻译：药物化合物
公开(公告)号：US08461339B2
公开(公告)日：2013-06-11
申请号：US13003945
申请日：2009-07-15
申请人： Robert George Boyle , David Winter Walker
发明人： Robert George Boyle , David Winter Walker
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C07D401/14
摘要： The invention provides kinase inhibitor compounds of the formula (1): or salts, solvates, tautomers or N-oxides thereof; wherein X is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; m is 0-2; n is 0-1; q is 0-2; A is C1-6 alkylene optionally interrupted by O; R1 is halogen, cyano, nitro, an optionally substituted acyclic C1-6 hydrocarbon group, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl, optionally substituted five membered heteroaryl, NR2R3, Ra—Rb, O—Rb or C(O)NR2R8; R4 is fluorine, chlorine, methyl or cyano; R2 is hydrogen or optionally substituted C1-4 alkyl; R3 is Ra—Rb; or NR2R3 forms a 4 to 7 membered non-aromatic heterocyclic ring; Ra is a bond, C(X2), C(X2)X1, SO, SO2 or SO2NRc; Rb is hydrogen or an optionally substituted 3 to 7-membered carbocyclic or heterocyclic ring or an optionally substituted C1-12 acyclic hydrocarbon group; Rc is hydrogen or a C1-4 hydrocarbon group; Rd is O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc or NRcSO2; X1 is O, S or NRc; X2 is ═O, ═S or ═NRc; but excluding the compound wherein m, n and q are all 0, A is CH2 and NR2R3 is a 2-phenylmorpholin-4-yl group.
摘要翻译：本发明提供式（1）的激酶抑制剂化合物：或其盐，溶剂合物，互变异构体或N-氧化物; 其中X是O，CO，X1C（X2），C（X2）X1，X1C（X2）X1，S，SO，SO2，NRc，SO2NRc或NRcSO2; m为0-2; n为0-1; q为0-2; A是任选被O中断的C 1-6亚烷基; R 1为卤素，氰基，硝基，任选取代的无环C 1-6烃基，任选取代的C 3-7环烷基，任选取代的苯基，任选取代的五元杂芳基，NR2R3，Ra-Rb，O-Rb或C（O）NR2R8 ; R4是氟，氯，甲基或氰基; R2是氢或任选取代的C 1-4烷基; R3是Ra-Rb; 或NR 2 R 3形成4至7元非芳族杂环; R a是键，C（X 2），C（X 2）X 1，SO，SO 2或SO 2 NR c; Rb是氢或任选取代的3至7元碳环或杂环或任选取代的C1-12无环烃基; Rc是氢或C 1-4烃基; Rd为O，CO，X1C（X2），C（X2）X1，X1C（X2）X1，S，SO，SO2，NRc，SO2NRc或NRcSO2; X1是O，S或NRc; X2 = O，= S或= NRc; 但不包括m，n和q全部为0的化合物，A为CH 2且NR 2 R 3为2-苯基吗啉-4-基。

7. 发明申请

US20110144080A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 有权
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：US20110144080A1
公开(公告)日：2011-06-16
申请号：US10596788
申请日：2004-12-23
申请人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hanna Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/415 , C07D231/12 , C07D401/10 , A61K31/454 , A61K31/4439 , C07D413/10 , A61K31/5377 , C07D403/10 , A61K31/4155 , A61K31/496 , A61K31/497 , A61K31/551 , C07D401/04 , C07D401/14 , A61K31/4545 , A61P35/00
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译：本发明提供下式的化合物：（I）具有蛋白激酶B抑制活性：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团在R1和NR2R3之间延伸的最大链长为5个原子并且在E和NR2R3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选地被氧或氮原子替代; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R 3基团位于碳原子a时，存在时的氧代基相对于NR 2 R 3基团位于碳原子a; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

8. 发明授权

US08691806B2 Pyrazole derivatives as protein kinase modulators 失效
标题翻译：吡唑衍生物作为蛋白激酶调节剂
公开(公告)号：US08691806B2
公开(公告)日：2014-04-08
申请号：US13536174
申请日：2012-06-28
申请人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
发明人： Valerio Berdini , Gordon Saxty , Marinus Leendert Verdonk , Steven John Woodhead , Paul Graham Wyatt , Robert George Boyle , Hannah Fiona Sore , David Winter Walker , Ian Collins , Robert Downham , Robin Arthur Ellis Carr
IPC分类号： A61K31/397 , C07D231/12
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译：本发明提供具有蛋白激酶B抑制活性的式（I）化合物：还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

9. 发明授权

US08546407B2 Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors 有权
标题翻译：正构缩合的吡啶和嘧啶衍生物（如嘌呤）作为蛋白激酶抑制剂
公开(公告)号：US08546407B2
公开(公告)日：2013-10-01
申请号：US11577963
申请日：2005-10-25
申请人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
发明人： Valerio Berdini , Robert George Boyle , Gordon Saxty , David Winter Walker , Steven John Woodhead , Paul Graham Wyatt , Alastair Donald , John Caldwell , Ian Collins , Tatiana Faria Da Fonseca
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (Ic) or salts, tautomers or N-oxides thereof.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的化合物，该化合物是式（Ic）化合物或其盐，互变异构体或N-氧化物。

10. 发明申请

US20130065900A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20130065900A1
公开(公告)日：2013-03-14
申请号：US13697743
申请日：2011-05-12
申请人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
发明人： Robert George Boyle , David Winter Walker , Richard Justin Boyce
IPC分类号： A61K31/5377 , C07D241/26 , C07D405/12 , C07D403/12 , A61K31/4965 , A61N5/10 , C07D413/12 , C07D413/02 , A61K31/497 , C07D403/02
CPC分类号： C07D241/26 , A61K31/4965 , A61K31/497 , A61K31/5377 , A61N5/10 , C07D241/20 , C07D403/12 , C07D405/12 , C07D413/12
摘要： The invention provides a compound of the formula (1): or a salt, N-oxide or tautomer thereof; wherein R1 is cyano or C1-4 alkyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; R4 and R5 are the same or different and each is selected from hydrogen, saturated C1-4 hydrocarbyl and saturated C1-4 hydrocarbyloxy; R6 and R7 are the same or different and each is selected from hydrogen, halogen, CN, C1-4 alkyl and C1-4 alkoxy wherein the C1-4 alkyl and C1-4 alkoxy are each optionally substituted with hydroxy, C1-2 alkoxy or by one or more flourine atoms; R8 is hydrogen or C1-4 alkyl; Q is an alkylene chain of 1 to 4 carbon atoms in length between the moiety Ar and the nitrogen atom N, wherein one or more of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with one or two C1-4 alkyl groups, or wherein one carbon atom of the 1 to 4 carbon atoms of the alkylene chain may optionally be substituted with a group —CH2CH2— which together with the said one carbon atom forms a cyclopropyl group; m is 1, 2, 3 or 4; n is 0 or 1; and Ar is a monocyclic or bicyclic aryl or heteroaryl group of 5 to 10 ring members containing 0, 1, 2, 3 or 4 heteroatom ring members selected from O, N and S, the aryl or heteroaryl group being optionally substituted with one to four substituents R13 as defined in the claims.The compounds are inhibitors of Chk-1 kinase and are active against cancers.
摘要翻译：本发明提供式（1）化合物或其盐，N-氧化物或其互变异构体; 其中R1是氰基或C1-4烷基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; R4和R5相同或不同，各自选自氢，饱和C 1-4烃基和饱和C 1-4烃氧基; R 6和R 7相同或不同，各自选自氢，卤素，CN，C 1-4烷基和C 1-4烷氧基，其中C 1-4烷基和C 1-4烷氧基各自任选被羟基，C 1-2烷氧基或通过一个或多个荧光原子; R8是氢或C1-4烷基; Q是部分Ar和氮原子N之间的长度为1至4个碳原子的亚烷基链，其中亚烷基链的1至4个碳原子中的一个或多个可以任选被一个或两个C 1-4烷基取代基团，或其中亚烷基链的1至4个碳原子的一个碳原子可以任选被基团-CH 2 CH 2取代，所述基团与所述一个碳原子一起形成环丙基; m为1,2,3或4; n为0或1; 并且Ar是具有0至1个，2个，3个或4个选自O，N和S的杂原子环成员的5至10个环成员的单环或双环芳基或杂芳基，芳基或杂芳基任选被一至四个取代基R 13如权利要求中所定义。这些化合物是Chk-1激酶的抑制剂并且对癌症有活性。

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