专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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

3. 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。

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. 发明申请

US20100166699A1 PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 失效
标题翻译：包含作为蛋白激酶调节剂的吡唑衍生物的药物组合
公开(公告)号：US20100166699A1
公开(公告)日：2010-07-01
申请号：US11993823
申请日：2006-06-21
申请人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
发明人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
IPC分类号： A61K38/20 , A61K31/497 , A61K39/395 , A61K31/517 , A61K31/5377 , A61K31/4439 , A61K31/565 , A61K31/566 , A61K38/21 , A61K33/24 , A61K31/4375 , A61K31/675 , A61K31/551 , A61P35/00
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 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; R 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.
摘要翻译：本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团具有在R1和NR2R3之间延伸的5个原子的最大链长度，以及在E和NR 2 R 3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选被氧或氮取代原子; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R 3基团位于碳原子a时，存在时的氧代基相对于NR 2 R 3基团位于碳原子a; E是单环或双环碳环或杂环基; R是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。

6. 发明授权

US08541461B2 Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators 失效
标题翻译：包含吡唑衍生物作为蛋白激酶调节剂的药物组合
公开(公告)号：US08541461B2
公开(公告)日：2013-09-24
申请号：US11993823
申请日：2006-06-21
申请人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
发明人： Neil Thomas Thompson , Robert George Boyle , Ian Collins , Michelle Dawn Garrett , John Francis Lyons , Kyla Merriom Thompson
IPC分类号： A61K31/415
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.
摘要翻译：本发明提供包含辅助化合物（例如一种，两种或多种辅助化合物）和具有蛋白激酶B抑制活性的式（I）化合物的组合的组合：其中A是含有1至7个碳原子的饱和烃连接基团，连接基团具有在R1和NR2R3之间延伸的5个原子的最大链长度，以及在E和NR 2 R 3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选被氧或氮取代原子; 并且其中连接基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R 3基团位于碳原子α时，条件是存在时的氧代基位于相对于NR 2 R 3基团的碳原子α; E是单环或双环碳环或杂环基; R1是芳基或杂芳基; 并且R 2，R 3，R 4和R 5如权利要求中所定义。还提供了包含组合的患者包装，药物盒和包装和组合，用于制备组合的方法及其在联合治疗中作为抗癌剂的用途。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式