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2. 发明公开

EP1845974A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：EP1845974A1
公开(公告)日：2007-10-24
申请号：EP06700912.6
申请日：2006-01-20
申请人： Astex Therapeutics Limited
发明人： CURRY, Jayne Elizabeth , LYONS, John Francis , SQUIRES, Matthew Simon , THOMPSON, Neil Thomas , THOMPSON, Kyla Merriom , WYATT, Paul Graham
IPC分类号： A61K31/415 , A61K31/4155 , A61P35/00 , A61K33/24 , A61K31/70 , A61K31/047 , A61K31/505 , A61K31/337 , A61K38/01 , A61K39/395 , A61K31/4745 , A61K31/475
CPC分类号： A61K33/24 , A61K31/047 , A61K31/337 , A61K31/415 , A61K31/4155 , A61K31/4745 , A61K31/505 , A61K31/70 , A61K31/7068 , A61K38/01 , A61K39/395 , A61K45/06 , A61K47/545 , A61K47/6805 , A61K2300/00
摘要： The invention provides a combination of a cytotoxic compound or signalling inhibitor and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO 2 , C-O, NR g (C-O) or 0(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 O, S, NH, SO, SO 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).

3. 发明公开

EP1933832A2 PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：与吡衍生物作为蛋白激酶调节剂的药物组合
公开(公告)号：EP1933832A2
公开(公告)日：2008-06-25
申请号：EP06755597.9
申请日：2006-06-21
申请人： Astex Therapeutics Limited , The Institute of Cancer Research : The Royal Cancer Hospital , Cancer Research Technology Limited
发明人： THOMPSON, Neil Thomas , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle Dawn , LYONS, John Francis , THOMPSON, Kyla Merriom
IPC分类号： A61K31/415 , A61K31/454 , A61P35/00 , A61P37/00
CPC分类号： A61K45/06 , A61K31/415 , A61K31/454 , A61K2300/00
摘要： The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound 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 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 α with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom α 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 patient packs, pharmaceutical kits and packs and compositions containing the combinations, methods for preparing the combinations and their use in combination therapy as anticancer agents.

4. 发明公开

EP1845973A1 PHARMACEUTICAL COMPOUNDS 有权
标题翻译：药物化合物
公开(公告)号：EP1845973A1
公开(公告)日：2007-10-24
申请号：EP06700879.7
申请日：2006-01-20
申请人： Astex Therapeutics Limited
发明人： CURRY, Jayne Elizabeth , LYONS, John Francis , SQUIRES, Matthew Simon , THOMPSON, Neil Thomas , THOMPSON, Kyla Merriom , WYATT, Paul Graham
IPC分类号： A61K31/415 , A61K31/4155 , A61P35/00 , A61K31/4196 , A61K31/5685 , A61K31/135 , A61K31/565 , A61K31/4535 , A61K31/138 , A61K39/395 , A61K31/255 , A61K31/675 , A61K31/195 , A61K31/4188
CPC分类号： A61K31/5685 , A61K31/135 , A61K31/138 , A61K31/195 , A61K31/255 , A61K31/415 , A61K31/4155 , A61K31/4188 , A61K31/4196 , A61K31/4535 , A61K31/565 , A61K31/675 , A61K39/395 , A61K45/06 , A61K2300/00
摘要： The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR9(C=O) or 0(C=O) wherein R9 is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1 , 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g. fluorine), hydroxy, C1-4 hydrocarbyloxy, amino, mono- or di-C1-4 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 O, S, NH, SO, SO2; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).
摘要翻译：本发明提供了辅助剂和具有式（0）的化合物的组合：或其盐或互变异构体或N-氧化物或溶剂合物; 其中所述辅助剂选自：单克隆抗体，烷化剂，抗癌剂，另外的CDK抑制剂和激素，激素激动剂，激素拮抗剂或激素调节剂; X是基团R1-A-NR4-或5-或6-元碳环或杂环; A是键，SO 2，C = O，NR 9（C = O）或O（C = O），其中R 9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; R1是氢; 具有3至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烃基氨基和具有3至4个碳原子的杂环基团取代的取代基取代的C 1-8烃基 12个环成员，并且其中烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团替代; R2是氢; 卤素; C 1-4烷氧基（例如甲氧基）; 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; R3选自氢和具有3至12个环成员的碳环和杂环基团; 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。

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