专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2006046024A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046024A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004119
申请日：2005-10-25
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 , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
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
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 CR 5 ; J l -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 ); 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; Q 1 is a bond or a saturated C 1-3 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 CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 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 Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen; R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的化合物，该化合物是式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T是N或CR 5 >; N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; 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; Q 1是一个键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选地被氧或氮原子代替，或相邻的一对碳原子可以被CONR Q或Q Q取代，其中R q是氢或甲基，或R 0 q是与R 1连接的C 1-4亚烷基链或Q 1的碳原子以形成环状的部分; 并且其中连接基团Q 1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; Q 2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以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Q 2不是键; G是氢，NR 2 R 3，OH或SH，条件是当E是芳基或杂芳基且Q 2是键时，则G 是氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3 ，则Q 2是一个键; 和R 2，R 2，R 3，R 4，R 4， SUP＆gt;和R＆gt; 8如权利要求中所定义。}

2. 发明申请

WO2006046023A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046023A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004115
申请日：2005-10-25
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 , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria , DONALD, Alastair
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 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 ); A is an optionally substituted saturated C 1-7 hydrocarbon linker group having a maximum chain length of 5 atoms extending between R 1 and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , 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 CH 2 , O, S or NH and G is a C 1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R 1 is hydrogen or an aryl or heteroaryl group; R 2 and R 3 are each hydrogen, optionally substituted C 1-4 hydrocarbyl or optionally substituted C 1-4 acyl; or NR 2 R 3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR 2 R 3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C 1-4 alkyl; or NR 2 R 3 and the adjacent carbon atom of linker group A together form a cyano group; or R 1 , A and NR 2 R 3 together form a cyano group; and R 4 , R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen and various substituents as defined in the claims.
摘要翻译：本发明提供了一种用于预防或治疗由蛋白激酶B介导的疾病状态或病症的化合物，其具有式（I）：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 ; J 1是N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; A是在R 1和R 2之间延伸的最大链长为5个原子的任选取代的饱和C 1 -C 7烃连接基团连接基团中的一个碳原子是任选的，并且在E和NR 2 R 3之间延伸的最大链长为4个原子用氧或氮代替; E是单环或双环碳环或杂环基或非环基XG，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; R 1是氢或芳基或杂芳基; R 2和R 3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NR 2 R 3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，烷基; 或NR 2 R 3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; 和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所定义的各种取代基。}}

3. 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。}}

4. 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。

5. 发明申请

WO2005011697A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2005011697A2
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003196
申请日：2004-07-23
申请人： ASTEX TECHNOLOGY LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , MCDONALD, Edward , DE FONSECA, Tatiana, Faria , BAVETSIAS, Vassilios , CALDWELL, John , WYATT, Paul, Graham , BERDINI, Valerio
发明人： MCDONALD, Edward , DE FONSECA, Tatiana, Faria , BAVETSIAS, Vassilios , CALDWELL, John , WYATT, Paul, Graham , BERDINI, Valerio
IPC分类号： A61K31/472
CPC分类号： C04B35/632 , A61K31/472 , C07D217/02 , C07D401/12
摘要： The invention provides compounds for the prophylaxis or treatment of a disease state or condition mediated by protein kinase A or protein kinase B, the compounds having the formula (I°), or being salts or solvates thereof. In formula (I°), n is 0 or 1; A and E are alkylene 2-3 carbon atoms in length optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); G is hydrogen when n is 0 and, when n is 1, G is hydrogen or -X-CH(R 6 )(R 7 ); R 1 is an aryl or heteroaryl group having 5-12 ring members; R 2 and R 4 are selected from hydrogen, R 7 , R 11 and CH(R 6 )(R 7 ); R 3 , R 3a and R 5 are selected from hydrogen, R 11 and -X-CH(R 6 )(R 7 ); or any one pair or any two non-overlapping pairs selected from R 2 and R 3 ; R 3 and R 4 ; R 2 and R 5 ; R 3 and R 5 ; R 4 and R 5 ; R 3 and R 8 ; and R 4 and R 8 are linked together in a ring and together form an alkylene chain of 1-5 carbon atoms in length which may be optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); or the pair R 2 and R 4 are linked together in a ring and together form an alkylene chain of 2-5 carbon atoms in length which may be optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); and optionally R 3 and R 3a may be linked together in a ring and together form an alkylene chain of 1-6 carbon atoms in length which may be optionally substituted by R 11 and -X-CH(R 6 )(R 7 ); or R 6 and R 7 together with the carbon atom to which they are attached form a cyclic group having 5-12 ring members; X, R 6 , R 7 , R 8 , R 9 , R 10 and R 11 are each as defined in claim 1; and wherein the definitions of, A, E, G, X, n and R 1 to R 11 are subject to the provisos set ou in claim 1.
摘要翻译：本发明提供了用于预防或治疗由蛋白激酶A或蛋白激酶B，具有式（I°）的化合物或其盐或溶剂合物介导的疾病状态或病症的化合物。在式（I°）中，n为0或1; A和E是长度任选被R 11和-X-CH（R 6）（R 7）取代的2-3个碳原子的亚烷基; 当n为0时，G为氢，当n为1时，G为氢或-X-CH（R 6）（R 7）; R 1是具有5-12个环成员的芳基或杂芳基; R 2和R 4选自氢，R 7，R 7和CH（R 6）（R 7）; R 3，R 3a和R 5选自氢，R 11和-X-CH（R 6）（R 7）; 或选自R 2和R 3中的任何一对或任何两个非重叠对; R 3和R 4; R 2和R 5; R 3和R 5; R 4和R 5; R 3和R 8; 并且R 4和R 8以环连接在一起并且一起形成长度为1-5个碳原子的亚烷基链，其可任选地被R 11和-X-CH（R 6）取代，）（R <7>）; 或者R 2和R 4在环中连接在一起并且一起形成长度为2-5个碳原子的亚烷基链，其可以任选地被R 11和-X-CH（R' 6>）（R <7>）; 并且任选地R 3和R 3a可以以环连接在一起并且一起形成长度为1-6个碳原子的亚烷基链，其可任选地被R 11和-X-CH（R' 6>）（R <7>）; 或R 6和R 7与它们所连接的碳原子一起形成具有5-12个环成员的环状基团; X，R 6，R 7，R 8，R 9，R 10和R 11各自如权利要求1所定义; 并且其中A，E，G，X，n和R 1至R 11的定义符合权利要求1所述的限制条件。

6. 发明申请

WO2006077419A1 PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S 审中-公开
标题翻译：用于抑制CDK和GSK'S的吡唑衍生物
公开(公告)号：WO2006077419A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000196
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
发明人： WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
IPC分类号： C07D453/02 , C07D401/14 , C07D401/12 , A61K31/44 , A61K31/4545 , A61K31/506 , A61P35/00 , A01N43/56
CPC分类号： C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14
摘要： The invention provides compounds of the formula (I) or a salt, tautomer, solvate or N-oxides thereof; wherein: R 1 is selected from (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and (d) a group R 0 wherein R 0 is a 3-12 membered carbocyclic or heterocyclic group; or optionally substituted C 1-8 hydrocarbyl; R 2a and R 2b are each hydrogen or methyl; and R 3 is as defined in the claims. The compounds have activity as inhibitors of Cyclin Dependent Kinases (CDK) and Glycogen Synthase Kinases (GSK) kinases and are useful in the treatment or prophylaxis of disease states or conditions mediated by the kinases.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，溶剂合物或N-氧化物; 其中：R 1选自（a）2,6-二氯苯基; （b）2,6-二氟苯基; （c）2,3,6-三取代的苯基，其中取代基是氟，氯，甲基或甲氧基; 和（d）R 0为0的基团，其中R 0为3-12元碳环或杂环基; 或任选取代的C 1-8烃基; R 2a和R 2b各自为氢或甲基; R 3和R 3如权利要求中所定义。该化合物具有作为细胞周期蛋白依赖性激酶（CDK）和糖原合酶激酶（GSK）激酶抑制剂的活性，可用于治疗或预防由激酶介导的疾病状态或病症。

7. 发明申请

WO2006070202A1 PYRAZOLE DERIVATIVES HAVING KINASE MODULATING ACTIVITY 审中-公开
标题翻译：具有激酶调节活性的吡唑衍生物
公开(公告)号：WO2006070202A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005109
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa , WYATT, Paul, Graham
IPC分类号： C07D413/14 , C07D403/04 , C07D407/14 , A01N43/56 , A61K31/4178 , A61K31/422 , A61P35/00
CPC分类号： C07D403/04 , C07D405/14 , C07D413/14
摘要： The invention provides a compound of the formula (I): or a salt, tautomer, N-oxide or solvate thereof; wherein A is selected from a bond, CH 2 and CH(CN); R l is selected from: (i) a cycloalkyl group of 3 to 6 ring members optionally substituted by one or more substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino and cyano; (ii) a phenyl group optionally substituted by up to three substituents selected from methyl, ethyl, fluorine, chlorine, methoxy, ethoxy and methylsulphonyl, but excluding 2,6-difluorophenyl, 2-fluoro-6-methoxy and 5-chloro-2-methoxyphenyl; (iii) a monocyclic heterocyclic group selected from furyl and isoxazolyl, the heterocyclic group being optionally substituted by one or two groups selected from methyl, ethyl, and a group CH 2 R 2 where R 2 is a five or six membered saturated heterocyclic ring containing one or two heteroatom ring members selected from O and N, the heterocyclic ring being optionally substituted by one or two methyl groups; and (iv) a bicyclic heterocyclic group selected from 2,3-dihydrobenzofuranyl and benzo[c]isoxazolyl, the bicyclic group being optionally substituted by one or two substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino, cyano and chlorine, the bicyclic heterocyclic group being other than a 2,2-dimethyl-2,3-dihydrobenzofuran-7-yl group.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，N-氧化物或其溶剂合物; 其中A选自键，CH 2和CH（CN）; R 1选自：（i）任选被一个或多个选自甲基，乙基，羟基，甲氧基，乙氧基，氟，氨基和氰基的取代基取代的3至6个环成员的环烷基; （ii）任选被至多三个选自甲基，乙基，氟，氯，甲氧基，乙氧基和甲基磺酰基的取代基取代的苯基，但不包括2,6-二氟苯基，2-氟-6-甲氧基和5-氯-2 - 甲氧基; （iii）选自呋喃基和异恶唑基的单环杂环基，杂环基团任选被一个或两个选自甲基，乙基和CH 2 R 2 R 2 O 2基团取代其中R 2是含有一个或两个选自O和N的杂原子环成员的五或六元饱和杂环，杂环任选被一个或两个甲基取代; 和（iv）选自2,3-二氢苯并呋喃基和苯并[c]异恶唑基的双环杂环基，双环基团任选被一个或两个选自甲基，乙基，羟基，甲氧基，乙氧基，氟，氨基，氰基和氯，双环杂环基不同于2,2-二甲基-2,3-二氢苯并呋喃-7-基。

8. 发明申请

WO2006070192A1 THIAZOLE AND ISOTHIAZOLE DERIVATIVES THAT MODULATE THE ACIVITY OF CDK, GSK AND AURORA KYNASES 审中-公开
标题翻译：调节CDK，GSK和AURORA KYNASES的活性的噻唑和异噻唑衍生物
公开(公告)号：WO2006070192A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005089
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WYATT, Paul, Graham
IPC分类号： C07D417/04 , C07D417/14 , A61K31/427 , A61P35/00
CPC分类号： C07D417/14 , C07D417/04
摘要： The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR 5 or N; each of Q 1 and Q 2 is a carbon atom; Q 3 is selected from S and CH; Q 4 is selected from CR 2 and S; provided that one of Q 3 and Q 4 is S and the other of Q 3 and Q 4 is not S; wherein when Q 3 is S, there is a double bond between Q 1 and Q 4 and a double bond between Q 2 and the adjacent ring nitrogen atom N; and when Q 4 is S, there is a double bond between Q 1 and Q 2 , and a double bond between Q 3 and the adjacent ring nitrogen atom N; A is a bond or -(CH 2 ) m -(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R 1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R ° is hydrogen or, together with NR g when present, forms a group -(CH 2 ) p - wherein p is 2 to 4; R 1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C 1-8 hydrocarbyl group; R 2 is hydrogen, halogen, methoxy, or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R 3 and R 4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, 0 and S; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is as defined in the claims.The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物，互变异构体或溶剂合物，其中X为CR 5或N; Q 1和Q 2中的每一个是碳原子; Q 3和S 3选自S和CH; Q ^{4 选自CR 2和S; 只要Q 3和Q 4中的一个是S，Q 3和Q 4中的另一个不是 S; 其中当Q 3是S时，在Q 1和Q 2之间存在双键， / SUP>和相邻环氮原子N; 并且当Q 4是S时，Q 1和Q 2之间存在双键，并且Q 3 相邻环氮原子N; A是键或 - （CH 2）m - （B）n - B为C = O，NR（C = O）或O（C = O），其中R 1为氢或任选被羟基取代的C 1-4烃基或C}

9. 发明申请

WO2006070198A1 PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：用于调节CDK，GSK和AURORA KINASES活性的吡唑衍生物
公开(公告)号：WO2006070198A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005102
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04 , C07D413/04 , C07D471/04 , A61K31/4155 , A61K31/422 , A61K31/427 , A61P35/00
CPC分类号： C07D407/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D471/04
摘要： The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R 1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or -Y-(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; R 2 is hydrogen; halogen; C 1-4 alkoxy ( e.g . methoxy); or a C 1-4 hydrocarbyl group optionally substituted by halogen ( e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy); R 3 is selected from optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C 1-8 hydrocarbyl group; with the proviso that R 1 is not formula (II): where X, R 3’ and R 4’ are defined in the claims.
摘要翻译：本发明提供式（I）化合物：用于医药：或其盐或互变异构体或N-氧化物或溶剂合物; 其中R 1是具有3至12个环成员的任选取代的杂环基，条件是连接到吡唑的环状基团含有至少一个选自N，O或S的杂原子; A是键或-Y-（B）n - B是C = O，NR（C = O）或O（C = O），其中R g是氢或C 1-4 >任选被羟基或C 1-4烷氧基取代的烃基; n为0或1; Y是长度为1,2或3个碳原子的键或亚烷基链; R 2是氢; 卤素; C 1-4烷氧基（如甲氧基）; 或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烷基; R 3选自具有3至12个环成员或任选取代的C 1-8烃基的任选取代的碳环和杂环基; 条件是R 1不是式（II）：其中X，R 3'和R 4'在权利要求中限定。

10. 发明申请

WO2004014922A1 3-(CARBONYL) 1H-INDAZOLE COMPOUNDS AS CYCLIN DEPENDENT KINASES (CDK) INHIBITORS 审中-公开
标题翻译：作为循环激酶（CDK）抑制剂的3-（羰基）1H-吲唑化合物
公开(公告)号：WO2004014922A1
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003474
申请日：2003-08-08
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , CARR, Maria , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , CARR, Maria , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： The invention provides a compound of the formula (I): wherein E is O, S, or NH; G is selected from hydrogen; carbocyclic and heterocyclic groups having from 3 to 12 ring members; and acyclic C 1-8 hydrocarbyl groups optionally substituted; provided that E-G is not OH or SH and further provided that E-G does not contain the group O-O; two adjacent moieties selected from R 3 , R 4 , R 5 and R 6 , together with the carbon atoms to which they are attached, form a fused heterocyclic group having from 5 to 7 ring members and 1, 2 or 3 ring heteroatoms selected from N, O and S; and the other two moieties selected from R 3 , R 4 , R 5 and R 6. are the same or different and are each as defined in the description. The Invention also provides compounds of the formula (I) for use as inhibitors of cyclin dependent kinases and for use in the treatment of disease states and conditions mediated by cyclin dependent kinases.
摘要翻译：本发明提供式（I）的化合物：其中E是O，S或NH; G选自氢; 具有3至12个环成员的碳环和杂环基; 和任选取代的非环状C 1-8烃基; 条件是E-G不是OH或SH，并且进一步规定E-G不含O-O基团; 选自R 3，R 4，R 5和R 6的两个相邻部分与它们所连接的碳原子一起形成具有5至7个环成员的稠合杂环基和1 ，2或3个选自N，O和S的环杂原子; 并且选自R 3，R 4，R 5和R 6的其它两个部分相同或不同，并且各自如描述中所定义。本发明还提供用作细胞周期蛋白依赖性激酶抑制剂的式（I）化合物，并用于治疗由细胞周期蛋白依赖性激酶介导的疾病状态和状况。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式