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1. 发明申请

WO2005061463A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：WO2005061463A1
公开(公告)日：2005-07-07
申请号：PCT/GB2004/005464
申请日：2004-12-23
申请人： ASTEX TECHNOLOGY LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , 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
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
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 R l and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , 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 NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR 2 R 3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R l is an aryl or heteroaryl group; and R 2 , R 3 , R 4 and R 5 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，该连接基团的最大链长度在R 1之间延伸 >和NR 2 R 3，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代替原子; 并且其中，墨水基团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'位于碳原子a时，并且条件是当存在的氧代基位于相对于NR 2 R 3基团的碳原子a时; E是单环或双环碳环或杂环基; R 1是芳基或杂芳基; 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。

2. 发明申请

WO2006136823A1 HETEROCYCLIC CONTAINING AMINES AS KINASE B INHIBITORS 审中-公开
标题翻译：含杂环化合物作为激酶B抑制剂
公开(公告)号：WO2006136823A1
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002278
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , TAYLOR, Richard, David , HAMLETT, Christopher , SORE, Hannah, Fiona
发明人： BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , TAYLOR, Richard, David , HAMLETT, Christopher , SORE, Hannah, Fiona
IPC分类号： C07D333/20 , C07D401/10 , A61K31/381 , A61K31/4409 , A61K31/506 , C07D307/52 , A61K31/341 , C07D249/08 , A61K31/4196 , C07D213/38 , A61P35/00
CPC分类号： C07D249/08 , C07D213/38 , C07D307/52 , C07D333/20 , C07D401/04 , C07D401/10 , C07D405/10 , C07D413/10
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof; for use as a PKB kinase inhibitor or PKA kinase inhibitor. In formula (I), A is a saturated hydrocarbon linker group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; HET is a monocyclic heterocyclic group; R 1 is an aryl or heteroaryl group; n is 0 to 4; and R 2 , R 3 and R 4 are as defined in the claims, provided that HET is other than an unsubstituted or substituted pyrazole-4-yl group.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 用作PKB激酶抑制剂或PKA激酶抑制剂。在式（I）中，A是饱和烃连接基团; E是单环或双环碳环或杂环基; HET是单环杂环基; R 1是芳基或杂芳基; n为0至4; R 2，R 3和R 4如权利要求中所定义，条件是HET不是未取代或取代的吡唑-4 - 基。

3. 发明申请

WO2008075109A1 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：WO2008075109A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050776
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
发明人： WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , C07D519/00 , A61K31/437 , A61K31/52 , A61P35/00
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 CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N- C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); Q 3 is a bond or a saturated C 1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR 2 R 3 , 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; R 1a and R 1b are the same or different and each is hydrogen or a substituent R 10 ; or R 1a and R 1b 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 R 10 ; and R 2 , R 3 , R 4 , R 5 , R 7 , R 6 , R 8 , and R 10 are as defined in the claims.
摘要翻译：本发明提供了式（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的杂原子的五元杂芳基环，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是N或CR 5; J 1是N = C（R 6），（R 7）C = N，（R 8）N C（O），（R 8）2 CC（O），N = N或（R 0 > 7 ）C = C（R ^{6 ）; Q 3是任选被氟和羟基取代的键或饱和C 1-3烃连接基团; G是NR 2 R 3，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; R 1a和R 1b相同或不同，各自为氢或取代基R 10; 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地被一个或多个取代基R 10取代; 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。}

4. 发明申请

WO2006136829A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006136829A2
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002286
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , ASTRAZENECA AB , CANCER RESEARCH TECHNOLOGY LIMITED , SORE, Hannah, Fiona , BOYLE, Robert, George , HAMLETT, Christopher , SAXTY, Gordon , VERDONK, Marinus, Leendert , WALKER, David, Winter , WOODHEAD, Steven, John , HOWARD, Steven
发明人： CANCER RESEARCH TECHNOLOGY LIMITED , 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; L 1 is a bond or a linker selected from C 1 -C 4 alkenylene, C 1 -C 4 alkynylene, -CONR’, -NR’CO, -S, -C(O)-, -C(NR 11 )-, -C(S)-, -N(R 11 ) 2 , C(=CHR 11 ), -SO- and -SO 2- ; or L 1 together with t R 16 forms and 8-12 membered fused bicyclic heteroaryl ring system; L 3 is a bond or a linker selected from CONH and HNCO; provided that L 1 and L 3 cannot both be linkers simultaneously; and provided also that L 1 and L 3 cannot both be a bond simultaneously; R 16 is an optionally substituted 5- to 12-membered monocyclic or bicyclic carbocyclic or heterocyclic ring; L 2 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(=CHR 11 ), C(S)-, -N(R 11 ) 2 , C 3-4 cycloalkanediyl, -SO- and -SO2-; R 17 is absent or is C 1-6 alkyl or an optionally substituted 5 to 12 membered carbocyclic or heterocyclic ring; provided that when R 17 is absent, then L 2 is also absent; and R 2 , R 3 , R 4 , R 5 , R 11 and R’ are as defined in the claims.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中A是饱和烃连接基团; E是单环或双环碳环或杂环基; L 1是选自C 1 -C 4亚链烯基，C 1 -C 3链烯基的键或连接基团， -CONR'，-NR'CO，-S，-C（O） - ， - C（NR 11） - ， - C（S） - ， -N（R 11）2，C（= CHR 11），-SO-和-SO 2 - >; 或L 1连同t R 16形式和8-12元稠合双环杂芳基环系统; L 3是选自CONH和HNCO的键或接头; 条件是L 1和L 3不能同时都是接头; 并且还提供了L 1和L 3不能同时是键; R 16是任选取代的5至12元单环或双环碳环或杂环; L 2不存在或是选自C 1 -C 4亚烷基，C 1 -C 4亚烯基，C 1 -C 4亚炔基，-CONR' - ， - NR'CO - ， - O - ， - S - ， - （O） - ，C（= CHR 11），C（S） - ， - N（R 11） C 3-4环烷二基，-SO-和-SO 2 - ; R 17不存在或为C 1-6烷基或任选取代的5至12元碳环或杂环; 条件是当R 17不存在时，L 2也不存在; 和R 2，R 3，R 4，R 5，R 11，和R'如权利要求中所定义。

5. 发明申请

WO2006051290A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006051290A2
公开(公告)日：2006-05-18
申请号：PCT/GB2005/004323
申请日：2005-11-09
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , 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
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; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a are absent, or A is a saturated optionally substituted C 1-7 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; R 1 , R la , R 2 , and R 3 are each H; halogen; C 1-6 hydrocarbyl optionally substituted by halogen, OH or C 1-2 alkoxy; CN; CONHR 8 ; NH 2 ; NHCOR 10 or NHCONHR 10 ; R 4 is H or C 1-4 alkyl; R 4a is H, C 1-4 alkyl or a group R 9 ; R 5 and R 6 are each selected from H, R 9 and C 1-4 hydrocarbyl optionally substituted by halogen, C 1-2 alkoxy or R 9 ;or NR 5 R 6 forms a saturated 4-7 membered monocyclic heterocyclic group; R 7 is H or C 1-4 alkyl; R 8 and R 8a each H or saturated C 1-4 hydrocarbyl optionally substituted by fluorine; R 9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R 4 , R 4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR 5 R 6 , R 4 and A form a saturated 4-7 membered monocyclic heterocycle; or R 4 , together with R 7 or R 8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR 5 R 6 and R 7 or R 8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R 10 is optionally substituted phenyl or benzyl.
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，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症，其中环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7，NR 7 CO，C（R 8）= C（R 8）或（R 8）其中X是O，S或NR 7（其中X是O，S或NR 7）其中X是O，S或NR 7 ; 条件是当J 2是-J 1，R 1是N-CO时，E不是NR 7 CO ; m和n各自为0或1，其中m + n = 1或2; A是键，R 4和R 4a不存在，或A是饱和的任选取代的C 1-7烃连接基团，其具有在E和G之间延伸的5个原子的最大链长度，连接基团A中的一个碳原子任选地被O或N取代; R 1，R 2，R 2，R 3和R 3各自为H; 卤素; 任选被卤素，OH或C 1-12烷氧基取代的C 1-6烷基; CN; CONHR ^{8 ; NH _{2 ; NHCOR 10或NHCONHR 10; R 4是H或C 1-4烷基; R 4a是H，C 1-4烷基或基团R 9; R 5和R 6各自选自H，R 9和C 1-4烃基，任选被卤素，C 1-2烷氧基或R 9或NR 5 R 6形成饱和的4-7 元环杂环基; R 7是H或C 1-4烷基; 每个H或任选被氟取代的饱和C 1-4烃基的R 8和R 8 8a; R 9是含有至多3个选自N，O和S的环杂原子的单环或双环碳环或杂环基; 或R 4，R 4a和A一起形成饱和单环4-7元杂环; 或NR 5 R 6，R 4和A形成饱和的4-7元单环杂环; 或R 4，...，以及R 7或R 8，A和E形成4-7元饱和单环杂环; 或NR 5 R 6和R 7或R 8与A和E一起形成4-7元环饱和单环杂环; R 10是任选取代的苯基或苄基。}}

6. 发明申请

WO2007125320A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125320A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001517
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESERARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , SAXTY, Gordon , VERDONK, Marinus, Leendert , CALDWELL, John , COLLINS, Ian , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
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; R la is an optionally substituted aryl or heteroaryl group; R lb 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, R 2 , R 3 , R 4 , Q 1 and Q 2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q 2 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 CR Z ; J 1 -J 2 is selected from N=C(R Z ), (R Z )C=N, (R Z )N-C(O), (R Z ) 2 C-C(O), N=N and (R Z )C=C(R 6 ); J 4 - J 3 is a group N=C(R Z ) or a group (R Z )N-CO; and R Z 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，溶剂合物，互变异构体和N-氧化物; 其中TG选自基团（1）和（2）：其中星号（*）表示基团E与基团X的连接点; R 1是任选取代的芳基或杂芳基; R 1b是氢或基团R 1a; X是具有8至12个环成员的任选取代的双环杂环基，其中多达5个是选自O，N和S的杂原子; 和A，E，R 2，R 3，R 4，Q 1和Q 2 如权利要求中所定义; 条件是当E是芳基或杂芳基时，则Q 2不是键; 并且进一步规定部分（a）不是基团（BG1）或（BG2）; 其中（BG1）和（BG2）各自任选被取代; T是N或CR Z; J <1> 1 2 选自N = C（R Z），（R Z）Z = NC（O），（R）Z CC（O），N = N和（R O） >ž）C = C（R ^{6 ）; J 3 - N 3是基团N = C（R Z）或基团（R Z），的N- CO; 并且R Z是氢或取代基。式（I）化合物具有PKA和PKB激酶抑制活性，可用于治疗癌症。}

7. 发明申请

WO2006136829A3 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和PKB调节剂的用途
公开(公告)号：WO2006136829A3
公开(公告)日：2007-02-15
申请号：PCT/GB2006002286
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , ASTRAZENECA AB , CANCER RESEARCH TECHNOLOGY LIM , SORE HANNAH FIONA , BOYLE ROBERT GEORGE , HAMLETT CHRISTOPHER , SAXTY GORDON , VERDONK MARINUS LEENDERT , WALKER DAVID WINTER , WOODHEAD STEVEN JOHN , HOWARD STEVEN
发明人： CANCER RESEARCH TECHNOLOGY LIM , 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 , A61K31/415 , A61P43/00 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14
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; L 1 is a bond or a linker selected from C 1 -C 4 alkenylene, C 1 -C 4 alkynylene, -CONR', -NR'CO, -S-, -C(O)-, -C(NR 11 )-, -C(S)-, -N(R 11 ) 2 , C(=CHR 11 ), -SO- and -SO 2- ; or L 1 together with t R 16 forms an 8-12 membered fused bicyclic heteroaryl ring system; L 3 is a bond or a linker selected from CONH and HNCO; provided that L 1 and L 3 cannot both be linkers simultaneously; and provided also that L 1 and L 3 cannot both be a bond simultaneously; R 16 is an optionally substituted 5- to 12-membered monocyclic or bicyclic carbocyclic or heterocyclic ring; L 2 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(=CHR 11 ), C(S)-, -N(R 11 ) 2 , C 3-4 cycloalkanediyl, -SO- and -SO2-; R 17 is absent or is C 1-6 alkyl or an optionally substituted 5 to 12 membered carbocyclic or heterocyclic ring; provided that when R 17 is absent, then L 2 is also absent; and R 2 , R 3 , R 4 , R 5 , R 11 and R' are as defined in the claims. Compounds (I) modulate (PKA) and (PKB).
摘要翻译：本发明提供式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中A是饱和烃连接基团; E是单环或双环碳环或杂环基; L 1是选自C 1 -C 4亚链烯基，C 1 -C 3链烯基的键或连接基团， -CONR'， - NR'CO，-S - ， - C（O） - ， - C（NR 11） - ， - C（S） - ，-N（R 11）2，C（= CHR 11），-SO-和-SO 2 - SUB>; 或L 1连同t R 16一起形成8-12元稠合双环杂芳基环系; L 3是选自CONH和HNCO的键或接头; 条件是L 1和L 3不能同时都是接头; 并且还提供了L 1和L 3不能同时是键; R 16是任选取代的5至12元单环或双环碳环或杂环; L 2不存在或是选自C 1 -C 4亚烷基，C 1 -C 4亚烯基，C 1 -C 4亚炔基，-CONR' - ， - NR'CO - ， - O - ， - S - ， - （O） - ，C（= CHR 11），C（S） - ， - N（R 11） C 3-4环烷二基，-SO-和-SO 2 - ; R 17不存在或为C 1-6烷基或任选取代的5至12元碳环或杂环; 条件是当R 17不存在时，L 2也不存在; 和R 2，R 3，R 4，R 5，R 11，和R'如权利要求中所定义。化合物（I）调节（PKA）和（PKB）。

8. 发明申请

WO2006051290A3 COMPOUNDS FOR TREATING PROTEIN-KINASE MEDIATED DISORDERS 审中-公开
标题翻译：用于治疗蛋白激酶介导性疾病的化合物
公开(公告)号：WO2006051290A3
公开(公告)日：2006-09-14
申请号：PCT/GB2005004323
申请日：2005-11-09
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , 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
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 , C07D401/04 , C07D401/06 , C07D401/12 , 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; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a 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.
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，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症，其中环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7，NR 7 CO，C（R 8）= C（R 8）或（R 8）其中X是O，S或NR 7（其中X是O，S或NR 7）其中X是O，S或NR 7 ; 条件是当J 2是-J 1，R 1是N-CO时，E不是NR 7 CO ; m和n各自为0或1，其中m + n = 1或2; A是键，R 4和R 4a不存在，或A是在E和G之间延伸的最大链长为5个原子的饱和任选基团，一个碳连接基团A中的原子任选被O或N取代。

9. 发明申请

WO2008075110A1 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：WO2008075110A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050777
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
IPC分类号： C07D487/04 , C07D473/34 , C07D471/04 , A61K31/519 , 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

10. 发明申请

WO2007125325A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125325A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001522
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
IPC分类号： C07D471/04 , C07D487/04 , 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 J 1 -J 2 is CH=CH, N=CH, CH=N, HN-C(O) or CH 2 CO; 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：本发明提供了式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中J 1是H，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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