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1. 发明申请

US20090263398A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：US20090263398A1
公开(公告)日：2009-10-22
申请号：US12373713
申请日：2007-07-13
申请人： John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Neil James Gallagher , Jayne Elizabeth Curry
发明人： John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Neil James Gallagher , Jayne Elizabeth Curry
IPC分类号： A61K31/415 , A61K31/422 , A61K31/4178 , A61K31/4155 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/454 , A61K31/506 , A61K31/541 , A61K31/439 , A61P35/00 , A61K39/395
CPC分类号： A61K31/4453 , A61K31/415 , A61K2300/00
摘要： The invention provides a combination comprising an ancillary compound and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein 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, 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; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; 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, hydroxyl or C1-4 alkoxy.
摘要翻译：本发明提供包含辅助化合物和具有式（O）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X为基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A为键，SO 2，C-O，NR 9（C-O）或O（C-O），其中R 9为氢或任选被羟基或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，羟基，C 1-4烃氧基，氨基，一或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3-12个环成员的碳环或杂环基，并且其中所述烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基; 或任选被卤素，羟基或C 1-4烷氧基取代的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; R4是氢或任选被卤素，羟基或C 1-4烷氧基取代的C 1-4烃基。

2. 发明授权

US08404718B2 Combinations of pyrazole kinase inhibitors 有权
标题翻译：吡唑激酶抑制剂的组合
公开(公告)号：US08404718B2
公开(公告)日：2013-03-26
申请号：US12752772
申请日：2010-04-01
申请人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
发明人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
IPC分类号： A61K31/4465 , A61K31/4468 , A61K31/454 , C07D401/12
CPC分类号： A61K45/06 , A61K31/415 , A61K31/4439 , A61K31/497 , A61K33/24 , A61K2300/00
摘要： The invention provides a combination comprising a cytotoxic compound, a signalling inhibitor, an ancillary agent, or two or more further anti-cancer agents, and a compound having the formula (Ib): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4—; A is a bond, C═O, NRg(C═O) or O(C═O) wherein Rg 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 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 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 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：本发明提供了包含细胞毒性化合物，信号传导抑制剂，辅助剂或两种或更多种其它抗癌剂和具有式（Ib）的化合物或其盐或互变异构体或N-氧化物或溶剂合物的组合：其中X是基团R 1 -A-NR 4 - ; A是键，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; R1是具有3-12个环成员的碳环或杂环基; 或任选被一个或多个选自氟，羟基，C 1-4烃氧基，氨基，一或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3-12个环成员的碳环或杂环基，并且其中所述烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2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; R3选自具有3至12个环成员的碳环和杂环基; 和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。

3. 发明申请

US20110002879A1 Combinations of Pyrazole Kinase Inhibitors 有权
标题翻译：吡唑激酶抑制剂的组合
公开(公告)号：US20110002879A1
公开(公告)日：2011-01-06
申请号：US12752772
申请日：2010-04-01
申请人： Jayne Elizabeth CURRY , John Francis LYONS , Matthew Simon SQUIRES , Neil Thomas THOMPSON , Kyla Merriom THOMPSON , Paul Graham WYATT , Neil James GALLAGHER
发明人： Jayne Elizabeth CURRY , John Francis LYONS , Matthew Simon SQUIRES , Neil Thomas THOMPSON , Kyla Merriom THOMPSON , Paul Graham WYATT , Neil James GALLAGHER
IPC分类号： A61K38/19 , A61K31/415 , A61K31/4439 , A61K31/4196 , A61K31/454 , A61K31/496 , A61K31/4178 , A61K31/5377 , A61K31/497 , A61K31/4155 , A61K31/4709 , A61K31/422 , A61K31/506 , A61K31/541 , A61K31/4545 , A61K31/437 , A61K31/444 , A61K31/4375 , A61K39/395 , A61K38/22 , A61K31/69 , A61K31/665 , A61K31/573 , A61K31/7076 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K31/675 , A61K31/7048 , A61K38/14 , A61K38/18 , A61K31/663 , A61K31/522 , A61P35/00
CPC分类号： A61K45/06 , A61K31/415 , A61K31/4439 , A61K31/497 , A61K33/24 , A61K2300/00
摘要： The invention provides a combination comprising a cytotoxic compound, a signalling inhibitor, an ancillary agent, or two or more further anti-cancer agents, and a compound having the formula (Ib): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R1-A-NR4—; A is a bond, C═O, NRg(C═O) or O(C═O) wherein Rg 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 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 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 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：本发明提供了包含细胞毒性化合物，信号传导抑制剂，辅助剂或两种或更多种其它抗癌剂和具有式（Ib）的化合物或其盐或互变异构体或N-氧化物或溶剂合物的组合：其中X是基团R 1 -A-NR 4 - ; A是键，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; R1是具有3-12个环成员的碳环或杂环基; 或任选被一个或多个选自氟，羟基，C 1-4烃氧基，氨基，一或二-C 1-4烃基氨基的取代基取代的C 1-8烃基，以及具有3-12个环成员的碳环或杂环基，并且其中所述烃基的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2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; R3选自具有3至12个环成员的碳环和杂环基; 和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。

4. 发明申请

US20090142337A1 Pharmaceutical Combinations of Diazole Derivatives for Cancer Treatment 审中-公开
标题翻译：二唑衍生物用于癌症治疗的药物组合
公开(公告)号：US20090142337A1
公开(公告)日：2009-06-04
申请号：US12300056
申请日：2007-05-04
申请人： Matthew Simon Squires
发明人： Matthew Simon Squires
IPC分类号： A61K39/395 , A61K31/454
CPC分类号： A61K31/4468 , A61K38/09 , A61K45/06 , A61K2300/00
摘要： The invention provides a combination comprising (or consisting essentially of) an ancillary compound and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein: R1 is 2,6-dichlorophenyl; R2a and R2b are both hydrogen; and R3 is a group: formula (A) where R4 is C1-4 alkyl. The combinations have activity as inhibitors of CDK kinases and inhibit the proliferation of cancer cells.
摘要翻译：本发明提供包含（或基本上由其组成）辅助化合物和式（I）化合物或其盐，互变异构体，溶剂合物和N-氧化物的组合; 其中：R1是2,6-二氯苯基; R2a和R2b都是氢; 并且R 3是下式：其中R 4是C 1-4烷基的式（A）。该组合具有作为CDK激酶抑制剂的活性并抑制癌细胞的增殖。

5. 发明申请

US20080161355A1 Combinations of Pyrazole Kinase Inhibitors and Further Antitumor Agents 审中-公开
标题翻译：吡唑激酶抑制剂和其他抗肿瘤剂的组合
公开(公告)号：US20080161355A1
公开(公告)日：2008-07-03
申请号：US11814455
申请日：2006-01-20
申请人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
发明人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
IPC分类号： A61K31/415 , A61K31/454 , A61P35/00 , A61P35/02
CPC分类号： A61K31/44 , A61K31/00 , A61K31/341 , A61K31/4155 , A61K31/496 , A61K31/5355 , A61K2300/00
摘要： The invention provides a combination of a compound having the formula (0) and two or more further anti-cancer agents: or salts or tautomers or N-oxides or solvates thereof; wherein 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：本发明提供具有式（O）的化合物和两种或更多种其它抗癌剂或其盐或互变异构体或N-氧化物或溶剂合物的组合; 其中X为基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，CO，NR 9（CO）或O（CO），其中R 9是氢或C 1-4烷基，任选被羟基或C 1-4烷氧基取代的烃基; 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 - 烷氧基，氨基，单 - 或四个取代基取代的C 1-8烷基二-C 1-4烃基氨基和具有3-12个环成员的碳环或杂环基团，并且其中烃基的1或2个碳原子可以任选地被原子或基团取代选自O，S，NH，SO，SO 2; 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个环成员的氢和碳环和杂环基; 和R 4是氢或任选被卤素（例如氟），羟基或C 1-4烷氧基取代的C 1-4烷基（如甲氧基）。

6. 发明申请

US20100021420A1 COMBINATIONS OF PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDKS AND GSK'S 审中-公开
标题翻译：用于抑制CDKS和GSK'S的吡唑衍生物的组合
公开(公告)号：US20100021420A1
公开(公告)日：2010-01-28
申请号：US12373827
申请日：2007-07-13
申请人： John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Neil James Gallagher
发明人： John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Neil James Gallagher
IPC分类号： A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K39/395 , A61K38/21 , A61K38/20 , A61K33/24
CPC分类号： A61K31/454 , A61K45/06 , A61K2300/00
摘要： A combination comprising (a) a compound of formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is 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 to 3 carbon atoms; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or an optionally substituted C1-8 hydrocarbyl group 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; or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C1-4 alkoxy; 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, hydroxyl or C1-4 alkoxy; and (b) a compound of formula (I′″) or salts, tautomers, solvates and N-oxides thereof: wherein R1 is 2,6-dichlorophenyl; R2a and R2b are both hydrogen; and R3 is a group: formula (A) where R4 is C1-4 alkyl.
摘要翻译：包含（a）式（O）化合物或其盐或互变异构体或其N-氧化物或溶剂合物的组合; 其中X为R 1 -A-NR 4 - 或5或6元碳环或杂环; A为键，SO 2，C-O，NR 9（C-O）或O（C-O），其中R 9为氢或任选被羟基或C 1-4烷氧基取代的C 1-4烃基; Y是1〜3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; 或任选取代的C 1-8烃基，其中烃基中的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; C 1-4烷氧基; 或任选被卤素，羟基或C 1-4烷氧基取代的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; R4是氢或任选被卤素，羟基或C 1-4烷氧基取代的C 1-4烃基; 和（b）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R1是2,6-二氯苯基; R2a和R2b都是氢; 并且R 3是下式：其中R 4是C 1-4烷基的式（A）。

7. 发明申请

US20090036435A1 Pharmaceutical Compounds 审中-公开
标题翻译：药物化合物
公开(公告)号：US20090036435A1
公开(公告)日：2009-02-05
申请号：US11814461
申请日：2006-01-20
申请人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
发明人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
IPC分类号： A61K31/541 , A61K31/415 , A61K31/41 , A61K31/4439 , A61K31/4196 , A61K31/454 , A61K31/496 , A61P35/00 , A61K31/4155 , A61K31/4178 , A61K31/5377 , A61K31/497 , A61K31/422 , A61K31/4545
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 Ĉhydrocarbyl 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, Ĉhydrocarbyloxy, 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; Ĉalkoxy (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 Ĉhydrocarbyl 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（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物的组合：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R1-A-NR4-基团或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烷氧基取代的羟基; 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，羟基氧基，氨基，单 - 或二-C 1-4烃基氨基的取代基取代的C 1-8烃基和具有3-12个环成员的碳环或杂环基并且其中烃基中的1或2个碳原子可以任选地被选自O，S，NH，SO，SO 2的原子或基团取代; R2是氢; 卤素; Ĉ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; 和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）取代的烃基。

8. 发明申请

US20080161251A1 Pharmaceutical Compounds 审中-公开
标题翻译：药物化合物
公开(公告)号：US20080161251A1
公开(公告)日：2008-07-03
申请号：US11814456
申请日：2006-01-20
申请人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
发明人： Jayne Elizabeth Curry , John Francis Lyons , Matthew Simon Squires , Neil Thomas Thompson , Kyla Merriom Thompson , Paul Graham Wyatt
IPC分类号： A61K31/4155 , A61K31/415 , A61K31/4439 , A61K31/4196 , A61K31/454 , A61K31/496 , A61K31/4178 , A61K31/5377 , A61K31/497 , A61K31/4709 , A61K31/506 , A61K31/439 , A61P35/00 , A61K31/4375 , A61K31/337 , A61K31/7068 , A61K31/519 , A61K31/517 , A61K31/44 , A61K31/704
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 R1-A-NR4- or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C═O, NRg(C═O) or 0(C═O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4alkoxy; 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 C1-8hydrocarbyl 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; C1-4alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4alkoxy (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：本发明提供细胞毒性化合物或信号传导抑制剂与具有式（O）的化合物或其盐或互变异构体或N-氧化物或溶剂合物的组合：其中X为基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是一个键，SO 2，CO，NR（CO）或O（CO），其中R g是氢或C

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