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11. 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。

12. 发明授权

US08247576B2 Pyrazole derivatives as protein kinase modulators 有权
标题翻译：吡唑衍生物作为蛋白激酶调节剂
公开(公告)号：US08247576B2
公开(公告)日：2012-08-21
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 , 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： 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: 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。

13. 发明申请

US20110130394A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：US20110130394A1
公开(公告)日：2011-06-02
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： A61K31/541 , C07D401/14 , A61K31/4725 , A61K31/496 , C07D413/14 , A61K31/5377 , C07D417/14 , A61P35/00
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为═O，═S或= NRR; 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。

14. 发明申请

US20100210617A1 Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors 审中-公开
标题翻译：芳基烷基胺和杂芳基 - 烷基胺作为蛋白激酶抑制剂
公开(公告)号：US20100210617A1
公开(公告)日：2010-08-19
申请号：US11993835
申请日：2006-06-21
申请人： Steven John Woodhead , Robert Downham , Christopher Hamlett , Steven Howard , Hannah Fiona Sore , Marinus Leendert Verdonk , David Winter Walker , Richard William Arthur Luke
发明人： Steven John Woodhead , Robert Downham , Christopher Hamlett , Steven Howard , Hannah Fiona Sore , Marinus Leendert Verdonk , David Winter Walker , Richard William Arthur Luke
IPC分类号： A61K31/4155 , C07D231/12 , C07D403/10 , C07D413/10 , C07D413/14 , C07D401/10 , A61K31/415 , A61K31/496 , A61K31/5377 , A61K31/4178 , A61K31/4439 , A61K31/506 , A61K31/497 , A61K31/454 , A61P35/00
CPC分类号： C07D231/12
摘要： The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R25 is attached; and R4 and R5 each are hydrogen or a substituent as defined in the claims
摘要翻译：本发明提供式（II）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中n为0或1; Y1和Y2之一是CH，另一个选自CH，CR8和N; q为0,1或2，条件是当Y1或Y2为CR8时q为0或1; R 10芳环或5至10个环成员的杂芳基; R2a和R3a各自为氢，C1-4烃基或C1-4酰基，其中烃基和酰基部分任选被氟，羟基，氨基，甲基氨基，二甲基氨基或甲氧基取代; 或NR2aR3a形成任选含有选自O和N的第二杂原子环成员的咪唑基或饱和单环4-7元杂环基; R18是氢或甲基; R 19是氢或甲基; R 24是氢或R 24，R 2a，并且插入的氮原子和碳原子一起形成氮杂环丁烷，吡咯烷或哌啶环; R 25是氢或C 1-4烷基，其中C 1-4烷基任选被羟基或氨基取代，条件是羟基或氨基与R 25所连接的氧原子之间至少有两个碳原子; 且R 4和R 5各自为氢或如权利要求中所定义的取代基

15. 发明申请

US20100093748A1 SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY 审中-公开
标题翻译：具有蛋白激酶抑制活性的替代哌啶
公开(公告)号：US20100093748A1
公开(公告)日：2010-04-15
申请号：US12520303
申请日：2007-12-21
申请人： Steven John Woodhead , Martyn Frederickson , Christopher Hamlett , Andrew James Woodhead , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Peter Blurton , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Andrew Leach , Jeffrey James Morris
发明人： Steven John Woodhead , Martyn Frederickson , Christopher Hamlett , Andrew James Woodhead , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Peter Blurton , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Andrew Leach , Jeffrey James Morris
IPC分类号： A61K31/497 , C07D487/04 , A61K31/519 , C07D471/04 , A61K31/437
CPC分类号： C07D487/04 , C07D471/04 , C07D473/34 , C07D519/00
摘要： The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group 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); Q3 is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR2R3, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R1a and R1b are the same or different and each is hydrogen or a substituent R10; or R1a and R1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R10; and R2, R3, R4, R5, R7, R6, R8, and R10 are as defined in the claims.
摘要翻译：本发明提供式（I）的PKA和PKB激酶抑制化合物：或其盐，溶剂合物，互变异构体或N-氧化物，其中E是含有1,2,3或4个选自O， N和S的条件是不超过1个杂原子可以不是N; q和r各自为0或1; q + r为1或2; T为N或CR5基团; J1-J2是N = C（R6），（R7）C = N，（R8）N-C（O），（R8）2C-C（O），N = N或（R7）C = C ）; Q3是任选被氟和羟基取代的键或饱和C 1-3烃连接基团; G为NR2R3，CN或OH; m和n各自为0或1，条件是m + n为1或2，并且当环E的相邻环构件为S或O时，m或n各自为0; R1a和R1b相同或不同，各自为氢或取代基R10; 或R 1a和R 1b与它们所连接的碳原子或杂原子一起形成5或6元芳基或杂芳基环，其中芳基或杂芳基环任选被一个或多个取代基R 10取代; 并且R 2，R 3，R 4，R 5，R 7，R 6，R 8和R 10如权利要求中所定义。

16. 发明申请

US20100120798A1 SUBSTITUTED PIPERIDINES CONTAINING A HETEROARYLAMIDE OR HETEROARYLPHENYL MOIETY 审中-公开
标题翻译：含有异烟酰胺或邻苯二酚的取代的哌啶
公开(公告)号：US20100120798A1
公开(公告)日：2010-05-13
申请号：US12519993
申请日：2007-12-20
申请人： Steven John Woodhead , Christopher Hamlett , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Gregory Richard Carr , Jeffrey James Morris
发明人： Steven John Woodhead , Christopher Hamlett , Marinus Leendert Verdonk , Hannah Fiona Sore , David Winter Walker , Ian Collins , Kwai Ming Cheung , John Caldwell , Tatiana Faria Da Fonseca McHardy , Richard William Arthur Luke , Zbigniew Stanley Matusiak , Gregory Richard Carr , Jeffrey James Morris
IPC分类号： A61K31/522 , A61K31/52 , C07D473/34 , A61P37/00 , A61P9/00 , A61P11/06 , A61P25/00 , A61P29/00 , A61P35/00
CPC分类号： C07D473/34 , C07D487/04
摘要： The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R)x N * (GP1) (2) GP is a group GP2: 10 (R)r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claims
摘要翻译：本发明提供具有式（I）的PKA和PKB激酶抑制化合物的式（I）化合物：GP 1 JT 2 JN 4 RNH（I）或其盐，溶剂合物，互变异构体或N-氧化物，其中（1） GP是组GP1：HET 2a a QG（HNCO）f 7（R）x N *（GP1）（2）GP是组GP2：10（R）r O 2a a QG（CH 2）w NVHN * ）其中HET是含有至多4个杂原子环成员的单环或双环杂环基; 环V是5至10个环成员的单环或双环杂芳基; 并且J1，J2，R4，R7，R10，Q2a，Ga，x，w和f如权利要求中所定义

17. 发明申请

US20100016340A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：US20100016340A1
公开(公告)日：2010-01-21
申请号：US12298338
申请日：2007-04-25
申请人： Steven John Woodhead , Christopher Hamlett , Hannah Fiona Sore , David Winter Walker , Marinus Leendert Verdonk , Ian Collins , John Caldwell , Kwai-Ming Cheung , Tatiana Faria Da Fonseca McHardy
发明人： Steven John Woodhead , Christopher Hamlett , Hannah Fiona Sore , David Winter Walker , Marinus Leendert Verdonk , Ian Collins , John Caldwell , Kwai-Ming Cheung , Tatiana Faria Da Fonseca McHardy
IPC分类号： A61K31/522 , C07D401/14 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00 , C07D473/34
摘要： The invention provides compounds of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein J1-J2 is CH═CH, N═CH, CH═N, HN—C(O) or CH2CO; T is N or CH and GP is as defined in the claims. The compounds have activity as inhibitors of PKA and PKB kinases and are useful in the treatment of cancers.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中J1-J2是CH-CH，N-CH，CH-N，HN-C（O）或CH 2 CO; T是N或CH，GP如权利要求中所定义。该化合物具有作为PKA和PKB激酶抑制剂的活性，可用于治疗癌症。

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