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

US20100179145A1 PHARMACEUTICAL COMBINATIONS 有权
标题翻译：药物组合
公开(公告)号：US20100179145A1
公开(公告)日：2010-07-15
申请号：US12445180
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/4035 , A61K31/5377 , A61K31/496 , A61K31/437 , A61K31/454 , A61K31/415 , C07D471/04 , C07D209/44 , A61P31/12 , A61P35/00
CPC分类号： A61K31/403 , A61K31/4035 , A61K45/06 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 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-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 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 combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（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是羟基或氢; R2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; R3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，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 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。这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶抑制剂的活性。

2. 发明授权

US08883790B2 Pharmaceutical combinations 有权
标题翻译：药物组合
公开(公告)号：US08883790B2
公开(公告)日：2014-11-11
申请号：US12445136
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/497 , A61K31/535 , C07D401/14 , A61K31/403 , A61K31/438 , A61K31/439 , C07D209/08 , C07D209/44 , C07D215/08 , C07D401/04 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10 , A61K31/496 , A61K31/5375
CPC分类号： C07D401/14 , A61K31/403 , A61K31/438 , A61K31/439 , A61K31/496 , A61K31/5375 , C07D209/08 , C07D209/44 , C07D215/08 , C07D401/04 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 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-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 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 combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase and/or aurora kinase inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（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是羟基或氢; R2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; R3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，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 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。这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶和/或极光激酶抑制剂的活性。

3. 发明授权

US08277807B2 Pharmaceutical combinations 有权
标题翻译：药物组合
公开(公告)号：US08277807B2
公开(公告)日：2012-10-02
申请号：US12445141
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/404 , A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/438 , A61K31/5377 , A61K39/395 , A61K31/4745
CPC分类号： A61K45/06 , A61K31/403 , A61K31/4035 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 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-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 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 combinations have activity as Hsp90 inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（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是羟基或氢; R2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; R3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，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 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。这些组合具有作为Hsp90抑制剂的活性。

4. 发明申请

US20110105501A1 PHARMACEUTICAL COMBINATIONS 有权
标题翻译：药物组合
公开(公告)号：US20110105501A1
公开(公告)日：2011-05-05
申请号：US12445136
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/4035 , A61K31/438 , A61K31/5377 , A61K31/496 , A61P31/12 , A61P35/00
CPC分类号： C07D401/14 , A61K31/403 , A61K31/438 , A61K31/439 , A61K31/496 , A61K31/5375 , C07D209/08 , C07D209/44 , C07D215/08 , C07D401/04 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 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-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 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 combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase and/or aurora kinase inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（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是羟基或氢; R2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; R3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，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 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。这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶和/或极光激酶抑制剂的活性。

5. 发明申请

US20100092474A1 PHARMACEUTICAL COMBINATIONS 有权
标题翻译：药物组合
公开(公告)号：US20100092474A1
公开(公告)日：2010-04-15
申请号：US12445141
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/404 , A61K31/4035 , A61K31/47 , A61K31/472 , A61K31/438 , A61K31/437 , A61K31/5377 , A61K39/395 , A61K31/4745 , A61P35/00
CPC分类号： A61K45/06 , A61K31/403 , A61K31/4035 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 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-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 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 combinations have activity as Hsp90 inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（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是羟基或氢; R2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; R3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，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 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。这些组合具有作为Hsp90抑制剂的活性。

6. 发明授权

US08916552B2 Pharmaceutical combinations 有权
标题翻译：药物组合
公开(公告)号：US08916552B2
公开(公告)日：2014-12-23
申请号：US12445180
申请日：2007-10-12
申请人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
发明人： Neil James Gallagher , John Francis Lyons , Neil Thomas Thompson , Stephen Murray Yule , Christopher William Murray
IPC分类号： A61K31/535 , A61K31/497 , A01N43/40 , A61K31/435 , A61K31/445 , A01N43/56 , A61K31/415 , A01N43/38 , A61K31/40 , C07D209/44 , A61K45/06 , A61K31/4035 , A61K31/403
CPC分类号： A61K31/403 , A61K31/4035 , A61K45/06 , A61K2300/00
摘要： The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 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-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 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 combinations have activity as Hsp90 and/or glycogen synthase kinase-3 and/or cyclin dependent kinase inhibitors.
摘要翻译：本发明提供包含（或基本上由）一种或多种辅助化合物和式（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是羟基或氢; R2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; R3选自氢; 卤素; 氰基; 任选取代的C 1-5烃基和任意取代的C 1-5烃氧基; R4选自氢; 其中n为0或1，R7为任选取代的无环C 1-5烃基或具有3至7个环成员的单环碳环或杂环基团 - （O）n -R 7基团; 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。这些组合具有作为Hsp90和/或糖原合酶激酶-3和/或细胞周期蛋白依赖性激酶抑制剂的活性。

7. 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。

8. 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。

9. 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）。

10. 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。

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