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1. 发明申请

WO2008110846A3 COMPOSITIONS COMPRISING (S)-2-AMINO-1-(4-CHLOROPHENYL)-1-[4-(1H-PYRAZOL-4-YL)-PHENYL]-ETHANOL AS MODULATOR OF PROTEIN KINASES 审中-公开
标题翻译：包含（S）-2-氨基-1-（4-氯苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的组合物作为蛋白激酶的调节剂
公开(公告)号：WO2008110846A3
公开(公告)日：2009-03-05
申请号：PCT/GB2008050180
申请日：2008-03-14
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , WOODHEAD STEVEN JOHN , REES DAVID CHARLES , FREDERICKSON MARTYN , GRIMSHAW KYLA MERRIOM
发明人： WOODHEAD STEVEN JOHN , REES DAVID CHARLES , FREDERICKSON MARTYN , GRIMSHAW KYLA MERRIOM
IPC分类号： A61K31/415 , A61P35/00 , C07D231/12 , C07D301/00
CPC分类号： A61K31/415 , C07C215/32 , C07C247/10 , C07C309/30 , C07D231/12 , A61K2300/00
摘要： The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)- 1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)- phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H- pyrazol-4-yl)-phenyl]-ethanol, novel process intermediates and methods for making the novel process intermediates.
摘要翻译：本发明提供了包含（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的组合物，其中组合物基本上不含的（R）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇或该组合物含有（S）和（（S）对映异构体占优势。还提供了制备（S）2-氨基-1-（4-氯 - 苯基）-1- [4-（1H-吡唑-4-基） - 苯基] - 乙醇的方法，新工艺中间体和制备新工艺中间体的方法。

2. 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。

3. 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）。

4. 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.

6. 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.

8. 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.

9. 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.

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