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1. 发明申请

WO2008044034A1 HYDROBENZAMIDE DERIVATIVES AS INHIBITORS OF HSP90 审中-公开
标题翻译：盐酸衍生物作为HSP90的抑制剂
公开(公告)号：WO2008044034A1
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003871
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
发明人： FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
IPC分类号： C07D209/44 , C07C65/05 , C07C69/02 , A61P35/00 , A61K31/496
CPC分类号： C07C67/317 , C07C59/08 , C07C67/313 , C07C69/92 , C07C235/60 , C07D209/44
摘要： The invention provides an acid addition salt of a compound of the formula (1) Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
摘要翻译：本发明提供式（1）化合物的酸加成盐本发明还提供了制备式（1）化合物及其烷基类似物的方法，用于该方法的新中间体和制备中间体的方法。本发明还提供式（1）化合物及其乙基类似物的新的医学用途。

2. 发明申请

WO2006109085A1 HYDROXYBENZAMIDE DERIVATIVES AND THEIR USE AS INHIBITORS OF HSP90 审中-公开
标题翻译：羟基苯甲酸衍生物及其作为HSP90的抑制剂
公开(公告)号：WO2006109085A1
公开(公告)日：2006-10-19
申请号：PCT/GB2006/001382
申请日：2006-04-13
申请人： ASTEX THERAPEUTICS LIMITED , CHESSARI, Gianni , CONGREVE, Miles, Stuart , NAVARRO, Eva, Figueroa , FREDERICKSON, Martyn , MURRAY, Christopher , WOOLFORD, Alison, Jo-Anne , CARR, Maria, Grazia , DOWNHAM, Robert , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WOODHEAD, Andrew, James
发明人： CHESSARI, Gianni , CONGREVE, Miles, Stuart , NAVARRO, Eva, Figueroa , FREDERICKSON, Martyn , MURRAY, Christopher , WOOLFORD, Alison, Jo-Anne , CARR, Maria, Grazia , DOWNHAM, Robert , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel , WOODHEAD, Andrew, James
IPC分类号： C07D209/44 , C07D209/08 , C07D215/08 , C07D491/10 , C07D471/04 , C07D471/10 , C07D491/08 , C07D401/04 , C07D401/12 , A61K31/438 , A61K31/439 , A61K31/403
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; optionally substituted C 1-5 hydrocarbyl and optionally substituted C 1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group -(O)n-R 7 where n is 0 or 1 and R 7 is an optionally substituted acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C 1-5 hydrocarbyl- amino; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR 5 R 6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
摘要翻译：本发明提供式（I）的化合物：或其盐，互变异构体，溶剂合物和N-氧化物; 其中R 1是羟基或氢; R 2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R 3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任选取代的C 1-5 - 烃氧基; R4选自氢; 其中n为0或1且R 7为 - 任选取代的无环C 1-5 - 烃基的基团 - （O）n R 7，或具有3-7个环成员的单环碳环或杂环基; 卤素; 氰基; 羟基; 氨基; 和任选取代的单或二-C 1-5烃基 - 氨基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; 并且NR 5 R 6形成具有8至12个环成员的任选取代的双环杂环基，其中多达5个环成员是选自氧，氮和硫的杂原子。该化合物具有作为Hsp90抑制剂的活性。

3. 发明申请

WO2006109075A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006109075A2
公开(公告)日：2006-10-19
申请号：PCT/GB2006/001358
申请日：2006-04-13
申请人： ASTEX THERAPEUTICS LIMITED , CHESSARI, Gianni , CONGREVE, Miles, Stuart , NAVARRO, Eva, Figueroa , FREDERICKSON, Martyn , MURRAY, Christopher , WOOLFORD, Alison, Jo-Anne , CARR, Maria, Grazia , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James
发明人： CHESSARI, Gianni , CONGREVE, Miles, Stuart , NAVARRO, Eva, Figueroa , FREDERICKSON, Martyn , MURRAY, Christopher , WOOLFORD, Alison, Jo-Anne , CARR, Maria, Grazia , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James
IPC分类号： A61K31/401 , A61K31/445 , A61K31/5375 , A61K31/166 , C07C233/65
CPC分类号： C07D401/12 , C07C65/21 , C07D209/08 , C07D209/44 , C07D215/08 , C07D217/06 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy; wherein the C 1-5 hydrocarbyl and C 1-5 hydrocarbyloxy moieties are each optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; R 4 is selected from hydrogen; a group -(O) n -R 7 where n is 0 or 1 and R 7 is an acyclic C 1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and mono- or di-C 1-5 hydrocarbyl-amino, wherein the acyclic Ci-5 hydrocarbyl group and the mono and di-C 1-5 hydrocarbylamino moieties in each instance are optionally substituted by one or more substituents selected from hydroxy, halogen, C 1-2 alkoxy, amino, mono- and di-C 1-2 alkylamino, and aryl and heteroaryl groups of 5 to 12 ring members; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and R 5 and R 6 are as defined in the claims.
摘要翻译：本发明提供用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂化物和N-氧化物; 其中R 1是羟基或氢; R 2是羟基; 甲氧基或氢; 条件是R 1和R 2中的至少一个是羟基; R 3选自氢; 卤素; 氰基; C 1-5烃基和C 1-5氢烃氧基; 其中C 1-5烷基和C 1-5个碳环氧基部分各自任选被一个或多个选自羟基，卤素，C 1-2 烷氧基，氨基，单和二-C 1-12烷基氨基，以及5至12个环成员的芳基和杂芳基; R 4选自氢; 其中n为0或1且R 7为无环C 1-5的基团 - （O）N - ， - R 7 具有3〜7个环成员的单环碳环或杂环基; 卤素; 氰基; 羟基; 氨基; 和单 - 或二-C 1-5烃基 - 氨基，其中每个中的非环式C 1-5烃基和单和二-C 1-5烃基氨基部分实例任选被一个或多个选自羟基，卤素，C 1-12烷氧基，氨基，单和二-C 1-2烷基氨基的取代基取代，和芳基和5-12个环成员的杂芳基; 或R 3和R 4一起形成5至7个环成员的单环碳环或杂环; R 5和R 6如权利要求中所定义。

4. 发明申请

WO2006123165A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006123165A2
公开(公告)日：2006-11-23
申请号：PCT/GB2006/001851
申请日：2006-05-19
申请人： ASTEX THERAPEUTICS LIMITED , CHESSARI, Gianni , CONGREVE, Miles, Stuart , CALLAGHAN, Owen , COWAN, Suzanna, Ruth , MURRAY, Christopher, William , WOOLFORD, Alison, Jo-Anne , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James
发明人： CHESSARI, Gianni , CONGREVE, Miles, Stuart , CALLAGHAN, Owen , COWAN, Suzanna, Ruth , MURRAY, Christopher, William , WOOLFORD, Alison, Jo-Anne , O'BRIEN, Michael, Alistair , WOODHEAD, Andrew, James
CPC分类号： C07D413/04 , C07D239/42 , C07D239/47 , C07D239/48 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/04 , C07D409/04
摘要： The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): or salts, tautomers, solvates or N-oxides thereof; wherein: A is N or a group CR 3 ; R 1 is a monocyclic or bicyclic carbocyclic or heterocyclic ring of 5 to 10 ring members of which up to two ring members may be heteroatoms selected from N, O and S and the remainder are carbon atoms, the carbocyclic or heterocyclic ring being optionally substituted by one or more substituent groups independently selected from R 10 ; and R 2 , R 3 and R 10 are as defined in the claims.
摘要翻译：本发明提供了用作Hsp90抑制剂的化合物，具有式（I）的化合物：或其盐，互变异构体，溶剂合物或N-氧化物; 其中：A为N或基团CR 3; R 1是5至10个环成员的单环或双环碳环或杂环，其中多至两个环成员可以是选自N，O和S的杂原子，其余是碳原子，碳环或杂环任选被一个或多个独立地选自R 10的取代基取代; R 2，R 3和R 10如权利要求中所定义。

5. 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。

6. 发明申请

WO2005012256A1 3, 4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASES (CDK) AND GLYCOGEN SYNTHASE KINASE-3 (GSK-3) MODULATORS 审中-公开
标题翻译： 3，4-取代的1H-吡唑化合物及其作为循环激酶（CDK）和GLYCOGEN SYNTHASE KINASE-3（GSK-3）调节剂的用途
公开(公告)号：WO2005012256A1
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003179
申请日：2004-07-22
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul, Graham
IPC分类号： C07D231/38
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04
摘要： The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. Formula (0). In formula (0): X is a group R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S0 2 , 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; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R 1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C 1-4 hydrocarbyloxy, amino, mono- or di-C 1-4 hydrocarbylamino, and carbocyclic or heterocyclic groups having from 3 to 12 ring members, and wherein 1 or 2 of the carbon atoms of the hydrocarbyl group may optionally be replaced by an atom or group selected from 0, S, NH, SO, S0 2 ; 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 hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R 4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C 1-4 alkoxy (e.g. methoxy).
摘要翻译：本发明提供式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物，用于预防或治疗疾病状态和病症，例如由细胞周期蛋白依赖性激酶和糖原合酶激酶-3介导的癌症。公式（0）。在式（0）中：X是基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，C = O，NR g（C = O）或O（C = O），其中R g是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是长度为1,2或3个碳原子的键或亚烷基链; R 1是氢; 具有3-12个环成员的碳环或杂环基; 或任选被一个或多个选自卤素（例如氟），羟基，C 1-4烃氧基，氨基，单 - 或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3至 12个环成员，并且其中烃基中的1或2个碳原子可以任选地被选自0，S，NH，SO，SO 2的原子或基团取代; 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烃基; R 3选自具有3至12个环成员的氢和碳环和杂环基; 并且R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。

7. 发明申请

WO2005002552A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2005002552A2
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002824
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , HOWARD, Steven , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , EARLY, Theresa, Rachel , NAVARRO, Eva, Figueroa , GILL, Adrian, Liam , HOWARD, Steven , TREWARTHA, Gary , WOOLFORD, Alison, Jo-Anne , WOODHEAD, Andrew, James , WYATT, Paul
IPC分类号： A61K31/00
CPC分类号： A61K31/5377 , A61K31/00 , A61K31/4184 , A61K45/06 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D471/04 , C07D513/04
摘要： The invention provides compounds having activity as inhibitors of cyclin dependent kinases, glycogen synthase kinase-3 and Aurora kinases for use in the treatment of disease states and conditions such as cancer that are mediated by the kinases. The compounds have the general formula (I); wherein X is CR 5 or 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 g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; R 0 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, O and S; and R 5 is hydrogen, a group R 2 or a group R 10 wherein R 10 is selected from halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, mono- or di-C 1-4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members; a group R a -R b wherein R a is a bond, O, CO, X 1 C(X 2 ), C(X 2 )X 1 , X 1 C(X 2 )X 1 , S, SO, SO 2 , NR c , SO 2 NR c or NR c SO 2 ; and R b is selected from hydrogen, carbocyclic and heterocyclic groups having from 3 to 12 ring members, and a C 1-8 hydrocarbyl group optionally substituted by one or more substituents selected from hydroxy, oxo, halogen, cyano, nitro, carboxy, amino, mono- or di-C 1 - 4 hydrocarbylamino, carbocyclic and heterocyclic groups having from 3 to 12 ring members and wherein one or more carbon atoms of the C 1-8 hydrocarbyl group may optionally be replaced by O, S, SO, SO 2 , NR c , X 1 C(X 2 ), C(X 2 )X I or X 1 C(X 2 )X 1 ; R c is selected from hydrogen and C 1-4 hydrocarbyl; and X 1 is O, S or NR c and X 2 is =O, =S or =NR c . Also included within formula (I) are the salts, solvates and N-oxides of the compounds.
摘要翻译：本发明提供具有作为细胞周期蛋白依赖性激酶抑制剂，糖原合成酶激酶-3和极光激酶的活性的化合物，其用于治疗由激酶介导的疾病状态和病症如癌症。所述化合物具有通式（I）; 其中X是CR 5或N; A是键或 - （CH 2）m - （B）n-; B是C = O，NR g（C = O）或O（C = O），其中R g是氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; m为0,1或2; n为0或1; 当R 0为氢时，或与NR g一起形成基团 - （CH 2）p - ，其中p为2至4; R 1是氢，具有3至12个环成员的碳环或杂环基或任选取代的C 1-8烃基; R 2是氢，卤素，甲氧基或任选被卤素，羟基或甲氧基取代的C 1-4烃基; R 3和R 4与它们所连接的碳原子一起形成任选取代的稠合碳环或杂环，其具有5至7个环成员，其中多达3个可以是选自N，O和S的杂原子 ; R 5是氢，R 2或R 10基团，其中R 10选自卤素，羟基，三氟甲基，氰基，硝基，羧基，氨基，单或二-C1 具有3-12个环成员的烃基氨基，碳环和杂环基; 其中R a是键的基团R a -R b，O，CO，X C（X 2），C（X 2）X 1， C（X 2）X 1，S，SO，SO 2，NR c，SO 2 NR c或NR c SO 2; 并且R b选自具有3至12个环成员的氢，碳环和杂环基，以及任选被一个或多个选自羟基，氧代，卤素，氰基，硝基，羧基，具有3至12个环成员的氨基，单或二-C 1-4烃基氨基，碳环和杂环基，并且其中C 1-8烃基的一个或多个碳原子可以任选地被O，S，SO，SO 2， X c，X 1 C（X 2），C（X 2）X或X 1 X（X 2）X 1; R c选自氢和C 1-4烃基; 且X 1为O，S或NR c且X 2为= O，= S或= NR c。式（I）中还包括化合物的盐，溶剂合物和N-氧化物。

8. 发明申请

WO2004004730A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2004004730A2
公开(公告)日：2004-01-15
申请号：PCT/GB2003/002905
申请日：2003-07-04
申请人： ASTEX TECHNOLOGY LIMITED , WOOLFORD, Alison, Jo-Anne , BERDINI, Valerio , OREILLY, Marc , PADOVA, Alessandro , SAXTY, Gordon , WYATT, Paul, Graham
发明人： WOOLFORD, Alison, Jo-Anne , BERDINI, Valerio , OREILLY, Marc , PADOVA, Alessandro , SAXTY, Gordon , WYATT, Paul, Graham
IPC分类号： A61K31/4965
CPC分类号： C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/14
摘要： The invention provides a compound of the general formula (I) wherein R1 is selected from hydrogen, cycloalkyl and cycloalkenyl having 3 to 7 ring members; phenyl-C 1-4 alkyl or a group R 4 -A-CH 2 - wherein R 4 is selected from amino, mono- or di-C 1-4 alkylamino, hydroxyl, C 1-4 alkoxy, SH, S0 2 NR 9 R 9 , CONR 9 R 9 , NR 9 SO 2 R 10 and NR 9 COR 10 , and A is a C 1-4 alkylene chain or a group - (CH 2 ) m -B-(CH 2 ) n - wherein m and n are each independently 0, 1 or 2 and B is a divalent cycloalkyl or cycloalkenyl group having 3 to 7 ring members; the groups R 9 are the same or different and are each selected from hydrogen, C 1-4 hydrocarbyl optionally interrupted by O, NR c , S, SO or SO 2 and optionally substituted by a 5-7 membered carbocyclic or heterocyclic group, or two groups R 9 together with the nitrogen atom to which they are attached form a 5-7 membered heterocyclic group; and R 10 is hydrogen or C 1-4 hydrocarbyl optionally interrupted by O, S, SO or SO 2 and optionally substituted by a 5-7 membered carbocyclic or heterocyclic group; R 2 is selected from aryl and heteroaryl having five to twelve ring members; cycloalkyl and cycloalkenyl having 3 to 7 ring members; a group (CR 6 R 7 ) p E-R 8 wherein p is 1 or 2, E is a bond, O, S or NR 9 , R 6 and R 7 are the same or different and each is hydrogen, C 1-4 alkyl or phenyl provided that the group (CR 6 R 7 )p contains no more than one phenyl group, and R 8 is C 1-6 hydrocarbyl optionally interrupted by O, NR c , S, SO or SO 2 , a group R 4 , phenyl or a mono- or bicyclic heterocyclic group having from five to ten ring members; or R 1 and R 2 together with the nitrogen atom to which they are attached form a heterocyclic group having 5 to 10 ring members; R 3 is a substituent selected from halogen, CN, N-linked monocyclic nitrogen-containing heterocyclic groups having from 3 to 7 ring members and containing up to three heteroatoms; and a group R a -R b wherein R a is a bond, O, S, SO or SO 2 ; and R b is NR c R d or C 1-4 hydrocarbyl optionally interrupted by O, S, SO, SO 2 , NR c and optionally substituted by one or more substituents selected from hydroxy, halogen, cyano, nitro, amino, mono- or di-C 1-4 hydrocarbylamino; and R c and R d are the same or different and each is hydrogen or C 1-4 hydrocarbyl.The compounds have activity as inhibitors of cyclin dependent kinases and are useful in the treatment of disease states and conditions, such as proliferative diseases, mediated by cyclin dependent kinases.
摘要翻译：本发明提供通式（I）的化合物，其中R 1选自氢，环烷基和具有3-7个环成员的环烯基; 苯基-C 1-4烷基或基团R 4 -A-CH 2 - ，其中R 4选自氨基，单或二-C 1-4烷基氨基，羟基，C 1-4烷氧基，SH，SO 2 NR R 9，R 9，R 9，NR 9，SO 2 R 10和NR 9 COR 10，A是C 1-4亚烷基链或基团 - （CH 2） mB-（CH2）n-其中m和n各自独立地为0,1或2，B为具有3至7个环成员的二价环烷基或环烯基; 基团R 9相同或不同，各自选自氢，任选地被O，NR c，S，SO或SO 2中断的C 1-4烃基，并任选被5-7元碳环或杂环基取代或两个R 9与它们所连接的氮原子一起形成5-7元杂环基; 并且R 10是任选被O，S，SO或SO 2中断的且任选被5-7元碳环或杂环基取代的氢或C 1-4烃基; R 2选自具有5至12个环成员的芳基和杂芳基; 环烷基和具有3-7个环成员的环烯基; 基团（CR 6 R 7）pE-R 8其中p为1或2，E为键，O，S或NR 9，R 6和R 7为条件是基团（CR 6 R 7）p含有不多于一个苯基，R 8是任选地被C 1-6烃基取代的C 1-6烃基 O，NR c，S，SO或SO 2，基团R 4，苯基或具有5至10个环成员的单环或双环杂环基; 或R 1和R 2与它们所连接的氮原子一起形成具有5至10个环成员的杂环基; R 3是选自具有3至7个环成员并且含有至多3个杂原子的卤素，CN，N-连接的单环含氮杂环基的取代基; 和R a -R b基团，其中R a是键，O，S，SO或SO 2; 并且R b是任选地被O，S，SO，SO 2，NR c中断的NR c R d或C 1-4烃基，并任选地被一个或多个选自羟基，卤素，氰基，硝基，氨基，一或二-C 1-4烃基氨基; 且R c和R d相同或不同，各自为氢或C 1-4烃基。化合物具有作为细胞周期蛋白依赖性激酶抑制剂的活性，并且可用于治疗疾病状态和病症，例如增殖性由细胞周期蛋白依赖性激酶介导的疾病。

9. 发明申请

WO2004014864A1 1H-INDAZOLE-3-CARBOXAMIDE COMPOUNDS AS CYCLIN DEPENDENT KINASES (CDK) INHIBITORS 审中-公开
标题翻译： 1H-吲唑-3-羧酰胺化合物作为循环激酶（CDK）抑制剂
公开(公告)号：WO2004014864A1
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003491
申请日：2003-08-08
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , PADOVA, Alessandro , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , PADOVA, Alessandro , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D231/56
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The invention provides a compound of the formula (I) for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase: wherein A is a group R 2 or CH 2 -R 2 where R 2 is a carbocyclic or heterocyclic group having from 3 to 12 ring members; B is a bond or an acyclic linker group having a linking chain length of up to 3 atoms selected from C, N, S and O; R 1 is hydrogen or a group selected from SO 2 R b ,SO 2 NR 7 R 8 ,CONR 7 R 8 ,NR 7 R 9 and carbocyclic and heterocyclic groups having from 3 to 7 ring members; R 3 , to R 9 are defined in the description but excluding the compounds N-[(morpholin-4-yl)phenyl-1H-indazole-3-carboxamide and N-[4-(acetylaminosulphonyl)phenyl-1H-indazole-3-carboxamide.
摘要翻译：本发明提供了用于预防或治疗由细胞周期蛋白依赖性激酶介导的疾病状态或病症的式（I）化合物：其中A是基团R 2或CH 2 -R 2，其中R 1， 2>是具有3至12个环成员的碳环或杂环基; B是具有至多3个选自C，N，S和O的原子的连接链长度的键或无环连接基团; R 1是氢或选自SO 2 R b，SO 2 NR 7 R 8，CONR 7 R 8，NR 7 R 9和具有3个碳原子的碳环和杂环基团的基团至7名成员; R 3至R 9在描述中定义，但不包括化合物N - [（吗啉-4-基）苯基-1H-吲唑-3-甲酰胺和N- [4-（乙酰氨基磺酰基）苯基-1H- - 吲唑-3-甲酰胺。

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。

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