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1. 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。

2. 发明申请

US20110159111A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：US20110159111A1
公开(公告)日：2011-06-30
申请号：US12306383
申请日：2007-06-29
申请人： Jayne Elizabeth Curry , Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson
发明人： Jayne Elizabeth Curry , Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson
IPC分类号： A61K33/24 , A61P35/00 , A61K31/5377 , A61K31/7072
CPC分类号： A61K31/445 , A61K31/4155 , A61K31/416 , A61K31/4415 , A61K31/5377 , A61K2300/00
摘要： The invention provides combinations of an ancillary compound of the formula (0): and a compound of the formula (I′): Also provided are crystalline forms of the constituent compounds, methods for making them and their uses in treating cancers.
摘要翻译：本发明提供式（O）的辅助化合物与式（I'）的化合物的组合：还提供了组成化合物的结晶形式，其制备方法及其在治疗癌症中的用途。

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

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）。

5. 发明授权

US08435970B2 Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea 失效
标题翻译： 1-环丙基-3- [3-（5-吗啉-4-基甲基-1H-苯并咪唑-2-基）-1H-吡唑-4-基] - 脲的药物组合
公开(公告)号：US08435970B2
公开(公告)日：2013-05-07
申请号：US12306479
申请日：2007-06-29
申请人： Jayne Elizabeth Curry , Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson
发明人： Jayne Elizabeth Curry , Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson
IPC分类号： A61K31/56 , A61K31/535 , A61K31/52 , A61K31/44 , A61K31/445
CPC分类号： A61K45/06 , A61K31/337 , A61K31/475 , A61K31/5377 , A61K31/7072 , A61K33/24 , A61K2300/00
摘要： The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also provided are crystalline forms of the salts, methods for making the salts and their uses in treating cancers. The invention further provides combinations of an ancillary compound and a compound of the formula (I) as defined in PCT/GB2004/002824 (WO 2005/002552) or a compound of the formula (I′) or a salt, solvate, tautomer or N-oxide thereof, wherein R1, E, A and M are as defined in the claims.
摘要翻译：本发明提供了辅助化合物和化合物的组合，其是1-环丙基-3- [3-（5-吗啉-4-基甲基-1H-苯并咪唑-2-基）-1H-吡唑-4-基 ] - 选自乳酸盐和柠檬酸盐及其混合物。还提供盐的结晶形式，制备盐的方法及其在治疗癌症中的用途。本发明还提供了辅助化合物和如PCT / GB2004 / 002824（WO 2005/002552）中定义的式（I）化合物或式（I'）化合物或其盐，溶剂合物，互变异构体或其中R1，E，A和M如权利要求中所定义。

6. 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。

7. 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

8. 发明授权

US08399442B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US08399442B2
公开(公告)日：2013-03-19
申请号：US12159054
申请日：2006-12-29
申请人： Valerio Berdini , Jayne Elizabeth Curry , Neil James Gallagher , Adrian Liam Gill , John Francis Lyons
发明人： Valerio Berdini , Jayne Elizabeth Curry , Neil James Gallagher , Adrian Liam Gill , John Francis Lyons
IPC分类号： A61K31/33
CPC分类号： C07D403/04 , A61K31/4155 , A61K31/4184 , C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D487/04 , C07D491/056 , C07D513/04
摘要： A method for the treatment of: A. a disease state or condition mediated by a kinase wh ich is BCR-abl, VEGFR, PDGFR, EGFR, FLT3, JAK, C-abl, PDK1, Chk, FGFR, Ret, Eph, or Src; or B. a cancer in which the cancer cells thereof contain a drug resistant kinase mutation which is: (a) a threonine gatekeeper mutation; or (b) a drug-resistant gatekeeper mutation; or (c) an imatinib resistant mutation; or (d) a nilotinib resistant mutation; or (e) a dasatinib resistant mutation; or (f) a T670l mutation in KIT; or (g) a T674l mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315l mutation in abl; or C. a cancer which expresses a mutated molecular target which is a mutated form of BCRabl, c-kit, PDGF, EGF receptor or ErbB2; which method comprises administering to a patient in need thereof a therapeutically effective amount of a compound of the formula (l or l′): or a salt, solvate, tautomer or N-oxide thereof.
摘要翻译：一种治疗以下疾病的方法：A.由BCR-abl，VEGFR，PDGFR，EGFR，FLT3，JAK，C-abl，PDK1，Chk，FGFR，Ret，Eph或 Src 或B.一种其癌细胞含有耐药性激酶突变的癌症，其为：（a）苏氨酸关守突变; 或（b）耐药性守门人突变; 或（c）伊马替尼耐药突变; 或（d）尼洛替尼耐药突变; 或（e）达沙替尼抗性突变; 或（f）KIT中的T6701突变; 或（g）PDGFR中的T674l突变; 或（h）EGFR中的T790M突变; 或（i）abl中的T3151突变; 或C.表达突变形式的BCRab1，c-kit，PDGF，EGF受体或ErbB2的突变分子靶的癌症; 该方法包括向有需要的患者施用治疗有效量的式（I或1'）化合物或其盐，溶剂化物，互变异构体或N-氧化物。

9. 发明申请

US20100055094A1 PHARMACEUTICAL COMBINATIONS OF 1-CYCLOPROPYL-3- [3-(5-M0RPHOOLIN-4-YL-METHYL-1H-BENZOIMIDAZOL-2-YL)- LH-1-PYRAZOL-4-YL]- UREA 失效
标题翻译： 1-环丙基-3- [3-（5-M0RPHOOLIN-4-YL-甲基-1H-苯并咪唑-2-基）-LH-1-吡唑-4-基] - 尿素的药物组合
公开(公告)号：US20100055094A1
公开(公告)日：2010-03-04
申请号：US12306479
申请日：2007-06-29
申请人： Jayne Elizabeth Curry , Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson
发明人： Jayne Elizabeth Curry , Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson
IPC分类号： A61K31/4184 , A61K31/5377 , A61K31/4353 , A61K31/4439 , A61K31/454 , A61K31/52 , A61K39/395 , A61K31/56 , A61K33/24 , A61P35/04
CPC分类号： A61K45/06 , A61K31/337 , A61K31/475 , A61K31/5377 , A61K31/7072 , A61K33/24 , A61K2300/00
摘要： The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also provided are crystalline forms of the salts, methods for making the salts and their uses in treating cancers. The invention further provides combinations of an ancillary compound and a compound of the formula (I) as defined in PCT/GB2004/002824 (WO 2005/002552) or a compound of the formula (I′) or a salt, solvate, tautomer or N-oxide thereof, wherein R1, E, A and M are as defined in the claims.
摘要翻译：本发明提供了辅助化合物和化合物的组合，其是1-环丙基-3- [3-（5-吗啉-4-基甲基-1H-苯并咪唑-2-基）-1H-吡唑-4-基 ] - 选自乳酸盐和柠檬酸盐及其混合物。还提供盐的结晶形式，制备盐的方法及其在治疗癌症中的用途。本发明还提供了辅助化合物和如PCT / GB2004 / 002824（WO 2005/002552）中定义的式（I）化合物或式（I'）化合物或其盐，溶剂合物，互变异构体或其中R1，E，A和M如权利要求中所定义。

10. 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。

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