专利检索 ap:("Astex Therapeutics Limited" OR "The Institute of Cancer Research : The Royal Cancer Hospital" OR "Cancer Research Technology Limited") AND inv:"SAXTY, Gordon" 第 1 页

1.

发明公开
COMPOUNDS FOR TREATING PROTEIN-KINASE MEDIATED DISORDERS 审中-公开
标题翻译：化合物用于治疗由蛋白激酶介导的疾病

公开(公告)号：EP1814552A2

公开(公告)日：2007-08-08

申请号：EP05801609.8

申请日：2005-11-09

申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , Cancer Research Technology Limited

发明人： BERDINI, Valerio , BOYLE, Robert George , SAXTY, Gordon , VERDONK, Marinus Leendert , WOODHEAD, Steven John , WYATT, Paul Graham , SORE, Hannah Fiona , WALKER, David Winter , CALDWELL, John , COLLINS, Ian

IPC分类号： A61K31/505 , A61P35/00 , C07D239/88 , C07D401/12 , C07D401/04 , C07D401/06 , C07D403/12

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 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.

2.

发明公开
PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物

公开(公告)号：EP2013206A1

公开(公告)日：2009-01-14

申请号：EP07732554.6

申请日：2007-04-25

申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , Cancer Research Technology Limited

发明人： SAXTY, Gordon , VERDONK, Marinus, Leendert , CALDWELL, John , COLLINS, Ian , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria

IPC分类号： C07D471/04 , C07D495/04 , C07D498/04 , A61K31/506 , A61P35/00

CPC分类号： C07D471/04 , C07D495/04

摘要： Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof; wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; Rla is an optionally substituted aryl or heteroaryl group; Rlb is hydrogen or a group Rla; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R2, R3, R4, Q1 and Q2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BGl) and (BG2) are each optionally substituted; T is N or CRZ; J1-J2 is selected from N=C(RZ), (RZ)C=N, (RZ)N-C(O), (RZ)2C-C(O), N=N and (RZ)C=C(R6); J4 -J3 is a group N=C(RZ) or a group (RZ)N-CO; and RZ is hydrogen or a substituent. The compounds of the formula (I) have PKA and PKB kinase inhibiting activity and are useful in the treatment of cancers.

摘要翻译： 式（I）化合物及其盐，溶剂化物，互变异构体和N-氧化物; 其中TG选自组（1）和（2）：其中星号（*）表示基团E与基团X的连接点; R 1a是任选取代的芳基或杂芳基; R 1b是氢或基团R 1a; X是任选取代的具有8至12个环成员的双环杂环基团，其中至多5个是选自O，N和S的杂原子; 和A，E，R2，R3，R4，Q1和Q2如权利要求中所定义; 条件是当E是芳基或杂芳基时，则Q2不是键; 并进一步提供部分（a）不是基团（BG1）或（BG2）; 其中（BG1）和（BG2）各自任选被取代; T是N或CRZ; （RZ）C = N，（RZ）NC（O），（RZ）2C-C（O），N = N和（RZ）C = C（R 6））; J4-J3是基团N = C（RZ）或基团（RZ）N-CO; 并且RZ是氢或取代基。式（I）化合物具有PKA和PKB激酶抑制活性并可用于治疗癌症。

3.

发明公开
PYRAZOLE DERIVATIVES AND THEIR USE AS PKA AND PKB MODULATORS 审中-公开
标题翻译：吡唑衍生物及其作为PKA PKB和调制器

公开(公告)号：EP1919875A2

公开(公告)日：2008-05-14

申请号：EP06755590.4

申请日：2006-06-21

申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , AstraZeneca AB

发明人： SORE, Hannah, Fiona , BOYLE, Robert, George , HAMLETT, Christopher , SAXTY, Gordon , VERDONK, Marinus, Leendert , WALKER, David, Winter , WOODHEAD, Steven, John , HOWARD, Steven

IPC分类号： C07D231/12 , C07D401/10 , C07D401/12 , C07D401/14

CPC分类号： C07D231/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14

摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof; wherein A is a saturated hydrocarbon linker group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; L1 is a bond or a linker selected from C1-C4 alkenylene, C1-C4 alkynylene, -CONR’, -NR’CO, -S-, -C(O)-, -C(NR11)-, -C(S)-, -N(R11)2, C(=CHR11), -SO- and -SO2-; or L1 together with t R16 forms an 8-12 membered fused bicyclic heteroaryl ring system; L3 is a bond or a linker selected from CONH and HNCO; provided that L1 and L3 cannot both be linkers simultaneously; and provided also that L1 and L3 cannot both be a bond simultaneously; R16 is an optionally substituted 5- to 12-membered monocyclic or bicyclic carbocyclic or heterocyclic ring; L2 is absent or is a linker selected from C]-C4 alkylene, Ci-C4 alkenylene, Ci-C4 alkynylene, -CONR’-, -NR’CO-, -O-, -S-, -C(O)-, C(=CHR11), C(S)-, -N(R11)2, C3-4 cycloalkanediyl, -SO- and -SO2-; R17 is absent or is C1-6 alkyl or an optionally substituted 5 to 12 membered carbocyclic or heterocyclic ring; provided that when R17 is absent, then L2 is also absent; and R2, R3, R4, R5, R11 and R’ are as defined in the claims. Compounds (I) modulate (PKA) and (PKB).

4.

发明公开
ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 有权
标题翻译： ORTHO CONDENSED吡啶和PYRIDIMIDIN衍生物（例如嘌呤）作为蛋白激酶抑制剂

公开(公告)号：EP1812004A1

公开(公告)日：2007-08-01

申请号：EP05797685.4

申请日：2005-10-25

申请人： Astex Therapeutics Limited , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , Cancer Research Technology Limited

发明人： BERDINI, Valerio , BOYLE, Robert George , SAXTY, Gordon , WALKER, David Winter , WOODHEAD, Steven John , WYATT, Paul Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana Faria , DONALD, Alastair

IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04

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; Jl-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, 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, R3, R4, R6 and R8 are as defined in the claims.

5.

发明公开
PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 有权
标题翻译：吡唑衍生物作为蛋白激酶的调节剂

公开(公告)号：EP1706385A1

公开(公告)日：2006-10-04

申请号：EP04806258.2

申请日：2004-12-23

申请人： Astex Therapeutics Limited , Cancer Research Technology Limited , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL

发明人： BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis

IPC分类号： C07D231/12 , C07D413/10 , C07D401/10 , A61K31/415 , A61P37/02

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 Rl 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 inker 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; Rl 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.

6.

发明授权
ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 有权
标题翻译： ORTHO CONDENSED吡啶和PYRIDIMIDIN衍生物（例如嘌呤）作为蛋白激酶抑制剂

公开(公告)号：EP1812004B1

公开(公告)日：2011-06-22

申请号：EP05797685.4

申请日：2005-10-25

申请人： Astex Therapeutics Limited , The Institute of Cancer Research: Royal Cancer Hospital , Cancer Research Technology Limited

发明人： BERDINI, Valerio , BOYLE, Robert George , SAXTY, Gordon , WALKER, David Winter , WOODHEAD, Steven John , WYATT, Paul Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana Faria , DONALD, Alastair

IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04

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; Jl-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, 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, R3, R4, R6 and R8 are as defined in the claims.

7.

发明公开
ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：邻缩合吡啶和嘧啶衍生物（例如嘌呤）作为蛋白激酶抑制剂

公开(公告)号：EP1812003A1

公开(公告)日：2007-08-01

申请号：EP05796842.2

申请日：2005-10-25

申请人： Astex Therapeutics Limited , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , Cancer Research Technology Limited

发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria , DONALD, Alastair

IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04 , C07D473/00

CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04

摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the 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.