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1. 发明申请

US20100166699A1 PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 失效
标题翻译：包含作为蛋白激酶调节剂的吡唑衍生物的药物组合
公开(公告)号：US20100166699A1
公开(公告)日：2010-07-01
申请号：US11993823
申请日：2006-06-21
申请人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
发明人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
IPC分类号： A61K38/20 , A61K31/497 , A61K39/395 , A61K31/517 , A61K31/5377 , A61K31/4439 , A61K31/565 , A61K31/566 , A61K38/21 , A61K33/24 , A61K31/4375 , A61K31/675 , A61K31/551 , A61P35/00
CPC分类号： A61K45/06 , A61K31/415 , A61K31/454 , A61K2300/00
摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound 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; R is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims. Also provided are patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.
摘要翻译：本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团具有在R1和NR2R3之间延伸的5个原子的最大链长度，以及在E和NR 2 R 3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被氧或氮取代原子; 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; R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。还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。

2. 发明授权

US08541461B2 Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators 失效
标题翻译：包含吡唑衍生物作为蛋白激酶调节剂的药物组合
公开(公告)号：US08541461B2
公开(公告)日：2013-09-24
申请号：US11993823
申请日：2006-06-21
申请人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
发明人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
IPC分类号： A61K31/415
CPC分类号： A61K45/06 , A61K31/415 , A61K31/454 , A61K2300/00
摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound 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 α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α 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 patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.
摘要翻译：本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团具有在R1和NR2R3之间延伸的5个原子的最大链长度，以及在E和NR 2 R 3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被氧或氮取代原子; 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α时，条件是存在时的氧代基位于相对于NR 2 R 3基团的碳原子α; 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。还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。

3. 发明申请

US20090082370A1 Pharmaceutical Combinations of PK Inhibitors and Other Active Agents 审中-公开
标题翻译： PK抑制剂和其他活性剂的药物组合
公开(公告)号：US20090082370A1
公开(公告)日：2009-03-26
申请号：US12298286
申请日：2007-04-25
申请人： Neil Thomas Thompson , John Francis Lyons , Robert George Boyle , Kyla Merriom Grimshaw , Michelle Dawn Garrett , Ian Collins
发明人： Neil Thomas Thompson , John Francis Lyons , Robert George Boyle , Kyla Merriom Grimshaw , Michelle Dawn Garrett , Ian Collins
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00
CPC分类号： A61K45/06 , A61K31/52 , A61K31/5377 , A61K2300/00
摘要： The invention provides a combination for use as a protein kinase B inhibitor, the combination comprising (or consisting essentially of) an ancillary compound and: (I) a compound of the formula: or salts, solvates, tautomers or N-oxides thereof, wherein R1, Q1, Q2, E, G, T, R4, J1 and J2 are as defined in the claims; or (II) a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein R1, R2, R3, R4, E, A, T, J1 and J2 are as defined in the claims.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的组合，所述组合包含（或由其基本上由）辅助化合物组成，和：（I）下式化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中 R1，Q1，Q2，E，G，T，R4，J1和J2如权利要求中所定义; 或（II）具有式（I）的化合物：或其盐，溶剂化物，互变异构体或N-氧化物，其中R1，R2，R3，R4，E，A，T，J1和J2如权利要求中所定义。

4. 发明授权

US08796293B2 Purine and deazapurine derivatives as pharmaceutical compounds 有权
公开(公告)号：US08796293B2
公开(公告)日：2014-08-05
申请号：US12298462
申请日：2007-04-25
申请人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
发明人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
IPC分类号： A61K31/519 , A61K31/44 , C07D471/04 , C07D473/34
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： The invention provides 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 C1-4alkylene 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 α 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, NR2R3, 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, R3R4, R6 and R8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.

5. 发明申请

US20100022564A1 PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 有权
公开(公告)号：US20100022564A1
公开(公告)日：2010-01-28
申请号：US12298462
申请日：2007-04-25
申请人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
发明人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： The invention provides 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 C1-4alkylene 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 α 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, NR2R3, 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, R3R4, R6 and R8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.

6. 发明授权

US08343953B2 Pharmaceutical compounds 有权
标题翻译：药物化合物
公开(公告)号：US08343953B2
公开(公告)日：2013-01-01
申请号：US11993831
申请日：2006-06-21
申请人： Thomas Glanmor Davies , Robert George Boyle , Ian Collins , Michelle Dawn Garrett
发明人： Thomas Glanmor Davies , Robert George Boyle , Ian Collins , Michelle Dawn Garrett
IPC分类号： A61K31/397
CPC分类号： C07D401/14 , C07D231/12 , C07D401/04 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10
摘要： The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K 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 α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α 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.
摘要翻译：本发明提供了具有ROCK激酶和/或蛋白激酶p70S6K抑制活性的式（I）化合物：其中A是含有1至7个碳原子的饱和烃连接基团，该连接基团具有5个原子的最大链长度在R 1和NR 2 R 3之间并且在E和NR 2 R 3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，条件是存在的羟基相对于NR 2 R 3基团不位于碳原子α，条件是存在时的氧代基相对于NR2R3基团位于碳原子α; 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。

7. 发明申请

US20100130464A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20100130464A1
公开(公告)日：2010-05-27
申请号：US11993831
申请日：2006-06-21
申请人： Thomas Glanmor Davies , Robert George Boyle , Ian Collins , Michelle Dawn Garrett
发明人： Thomas Glanmor Davies , Robert George Boyle , Ian Collins , Michelle Dawn Garrett
IPC分类号： A61K31/415 , A61K31/454 , A61K31/5377 , A61K31/496 , A61K31/397 , A61P35/00
CPC分类号： C07D401/14 , C07D231/12 , C07D401/04 , C07D401/10 , C07D403/10 , C07D403/12 , C07D413/10
摘要： The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K 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 α 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.
摘要翻译：本发明提供具有ROCK激酶和/或蛋白激酶p70S6K抑制活性的式（I）化合物：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团的最大链长度为5个原子延伸在R 1和NR 2 R 3之间并且在E和NR 2 R 3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NR2R3基团位于碳原子α; 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。

8. 发明申请

US20090253718A1 Pharmaceutical Compounds 审中-公开
标题翻译：药物化合物
公开(公告)号：US20090253718A1
公开(公告)日：2009-10-08
申请号：US12298117
申请日：2007-04-25
申请人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
发明人： Thomas Glanmor Davies , Michelle Dawn Garrett , Robert George Boyle , Ian Collins
IPC分类号： A61K31/522 , A61K31/52 , A61P35/04 , A61P35/00 , A61K31/519
CPC分类号： C07D473/34 , C07D471/04 , C07D473/00 , C07D487/04
摘要： The invention provides a compound having 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); A is an optionally substituted saturated C1-7 hydrocarbon 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, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH2, O, S or NH and G is a C1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R1 is hydrogen or an aryl or heteroaryl group; R2 and R3 are each hydrogen, optionally substituted C1-4 hydrocarbyl or optionally substituted C1-4 acyl; or NR2R3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR2R3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C1-4 alkyl; or NR2R3 and the adjacent carbon atom of linker group A together form a cyano group; or R1, A and NR2R3 together form a cyano group; and R4, R5, R6, R7 and R8 are each independently selected from hydrogen and various substituents as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated.
摘要翻译：本发明提供具有式（I）的化合物或其盐，溶剂化物，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） A是在R 1和NR 2 R 3之间延伸的最大链长度为5个原子并且在E和NR 2 R 3之间延伸的4个原子的最大链长度的任选取代的饱和C 1-7烃连接基团，连接基团中的一个碳原子是任选的用氧或氮代替; E是单环或双环碳环或杂环基或非环基X-G，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链，其中一个碳原子任选被O，S或NH取代; R1是氢或芳基或杂芳基; R2和R3各自为氢，任选取代的C 1-4烃基或任选取代的C 1-4酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 或NR2R3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4烷基取代; 或NR2R3和连接基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 并且R 4，R 5，R 6，R 7和R 8各自独立地选自氢和权利要求中定义的各种取代基，其中所述化合物用于：（a）治疗或预防其中调节表示ROCK激酶或蛋白激酶p70S6K的抑制作用）和/或（b）治疗其中指示ROCK激酶或蛋白激酶p70S6K的调节（例如抑制）的受试者或患者群体。

9. 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。

10. 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。

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