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1. 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。

2. 发明专利

CA2548374C PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 未知
公开(公告)号：CA2548374C
公开(公告)日：2014-05-27
申请号：CA2548374
申请日：2004-12-23
申请人： ASTEX THERAPEUTICS LTD , CANCER REC TECH LTD , CANCER RES INST ROYAL
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 , A61K31/415 , A61P37/02 , C07D401/10 , 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.

4. 发明专利

HK1110503A1 ORTHO-CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E.G.PURINES) AS PROTEIN KINASES INHIBITORS 未知
公开(公告)号：HK1110503A1
公开(公告)日：2008-07-18
申请号：HK08101220
申请日：2008-01-31
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD
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： A61K20060101 , C07D20060101
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 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 ); E is a monocyclic carbocyclic or hctcrocyclic 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 ± 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.

6. 发明专利

MY144464A PYRAZOLE DERIVATIVES AS PROTIEN KINASE MODULATORS 未知
公开(公告)号：MY144464A
公开(公告)日：2011-09-30
申请号：MYPI20052573
申请日：2005-06-07
申请人： ASTEX THERAPEUTICS LTD , CANCER REC TECH LTD , CANCER RES INST ROYAL
发明人： BERDINI VALERIO , CARR ROBIN ARTHUR ELLIS , COLLINS IAN , SAXTY GORDON , VERDONK MARINUS LEENDERT , WOODHEAD STEVEN JOHN , WYATT PAUL GRAHAM , BOYLE ROBERT GEORGE , SORE HANNAH FIONA , WALKER DAVID WINTER , DOWNHAM ROBERT
IPC分类号： A61K31/415
摘要： THE INVENTION PROVIDES COMPOUNDS OF THE FORMULA (&Igr;) 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.

7. 发明专利

AT513549T 未知
公开(公告)号：AT513549T
公开(公告)日：2011-07-15
申请号：AT05797685
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD
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 , A61K31/437 , A61K31/519 , C07D471/04 , 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 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 ); E is a monocyclic carbocyclic or hctcrocyclic 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 ± 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.

10. 发明专利

AR053778A1 COMPUESTOS DE QUINAZOLINA PARA EL TRATAMIENTO DE DESORDENES MEDIADOS POR LA PROTEINA QUINASA 未知
公开(公告)号：AR053778A1
公开(公告)日：2007-05-23
申请号：ARP050104700
申请日：2005-11-09
申请人： CANCER RES INST ROYAL , CANCER REC TECH LTD , ASTEX THERAPEUTICS LTD
发明人： BERDINI VALERIO , BOYLE ROBERT GEORGE , SAXTY GORDON , VERDONK MARINUS L , WOODHEAD STEVEN , WYATT PAUL GRAHAM , SORE HANNAH FIONA , WALKER DAVID WINTER , CALDWELL JOHN , COLLINS IAN
IPC分类号： C07D239/88 , A61K31/505 , A61P35/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12
摘要： Reivindicacion 1: Un compuesto para usar en el tratamiento o profilaxis de un estado de enfermedad o condicion mediado por la proteína quinasa A y/o proteína quinasa B, caracterizado porque es un compuesto de la formula (1), o una sal, solvato, tautomero o N-oxido del mismo, en donde: el anillo Q es un anillo benceno; J2-J1 es un grupo N=CR7 un grupo R1aN-CO; G es OH o NR5R6; E es un átomo o un grupo ligante que se seleccionan entre CONR7, NR7CO, C(R8)=C(R8), (X)m(CR8R8a)n donde X se selecciona entre O, S y NR7; con la salvedad de que cuando J2-J1 es un grupo R1aN-C, E es distinto de NR7CO; m y n son cada uno 0 o 1, con la salvedad de que la suma de m y n es 1 o 2; A es un enlace y R4 y R4a están ausentes, o A es un grupo ligante de hidrocarburo saturado que contiene entre 1 y 7 átomos de C, donde el grupo ligante tiene una longitud máxima de cadena de 5 átomos que se extiende entre E y G, en donde uno de los átomos de C en el grupo ligante A optativamente puede reemplazarse con un átomo de O o N; y en donde los átomos de C del grupo ligante A optativamente pueden tener uno o más sustituyentes que se seleccionan entre oxo, F y hidroxi, con la salvedad de que el grupo hidroxi y el grupo oxo cuando están presentes no estén ubicados en un átomo de C alfa con respecto al grupo G; R1, R1a, R2, y R3 se seleccionan cada uno en forma independiente entre H, halogeno; C1-6 hidrocarbilo opcionalmente sustituido con halogeno, hidroxi o 1-2 alcoxi; ciano, CONHR8, NH2, NHCOR10 y NHCONHR10; R4 es H o alquilo C1-4; R4a es H, alquilo C1-4 o un grupo R9; R5 y R6 se seleccionan cada uno entre H, un grupo R9 y hidrocarbilo C1-4 opcionalmente sustituido con halogeno o alcoxi C1-2 o por un grupo R9; o NR5R6 forma un grupo monocíclico heterocíclico saturado que tiene 4-7miembros en el anillo y que contiene optativamente un segundo heteroátomo en el anillo que se seleccionan entre O y N; R7 se selecciona entre H y alquilo C1-4; R8 y R8a se seleccionan entre H y hidrocarbilo C1-4 saturado opcionalmente sustituido con uno o más átomos de F; R9 es un grupo monocíclico o bicíclico carbocíclico o heterocíclico que contiene hasta 3 heteroátomos en el anillo que se seleccionan entre N, O y S; o R4 y R4a junto con el o los átomos intervinientes del grupo A forman un grupo monocíclico heterocíclico saturado que tiene 4-7 miembros en el anillo y que contiene optativamente un segundo heteroátomo en el anillo que se seleccionan entre O y N, o uno de R5 y R6 junto con el átomo de N al cual están unidos y R4 y uno o más átomos del grupo ligante A forman un grupo monocíclico heterocíclico saturado que tiene 4-7 miembros en el anillo y que contiene optativamente un segundo heteroátomo en el anillo que se seleccionan entre O y n; o R4 junto con R7 o R8 y los átomos intervinientes de los grupos A y E forman un grupo monocíclico heterocíclico saturado que tiene 4-7 miembros en el anillo y que contiene optativamente un segundo heteroátomo en el anillo que se seleccionan entre O y N; o uno de R5 y R6 junto con el átomo de N al cual están unidos y R7 o R8 y, los átomos intervinientes de los grupos A y E forman un grupo monocíclico heterocíclico saturado que tiene 4-7 miembros en el anillo y que contiene optativamente un segundo heteroátomo en el anillo que se seleccionan entre O y N; R10 es fenilo o bencilo cada uno opcionalmente sustituido con uno o más sustituyentes que se seleccionan entre halogeno, hidroxi, trifluorometilo, ciano, nitro, carboxi, amino, mono- o di-C1-4hidrocarbilamino; un grupo Ra-Rb en donde Ra es un enlace, O, CO, X1C(X2), C(X2)X1, X1C(X2)X1, S, SO, SO2, NRc, SO2NRc o NRcSO2; y Rb se selecciona entre H, grupos heterocíclicos que tienen entre 3 y 12 miembros en el anillo, y un grupo C1-8 hidrocarbilo opcionalmente sustituido con uno o más sustituyentes que se seleccionan entre hidroxi, oxo, halogeno, ciano, nitro, carboxi, amino, mono- o di-C14 hidrocarbilamino, grupos carbocíclicos y heterocíclicos que tienen entre 3 y 12 miembros en el anillo y en donde uno o más átomos de C del grupo C1-8 hidrocarbilo optativamente pueden reemplazarse con O, S, SO, SO2, NRc, X1C(X2), C(X2)X1 o X1C(X2)X1; Rc se selecciona entre H e hidrocarbilo C1-4; y X1 es O, S o NRc y X2 es =O, =S o =NRc.

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