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1. 发明申请

WO2009138799A1 THERAPEUTIC USES OF 1-CYCL0PR0PYL-3 - [3- ( 5 -MORPHOLIN- 4 -YLMETHYL- 1H-BENZ0IMIDAZ0L- 2 -YL) -LH-PYRAZOL-4-YL] -UREA 审中-公开
标题翻译： 1-CYCL0PR0PYL-3 - [3-（5-吗啉-4-基甲基-1H-苯并咪唑基）-2-基] -LH-吡唑-4-基] - 脲的治疗用途
公开(公告)号：WO2009138799A1
公开(公告)日：2009-11-19
申请号：PCT/GB2009/050520
申请日：2009-05-14
申请人： ASTEX THERAPEUTICS LIMITED , CURRY, Jayne, Elizabeth , LYONS, John, Francis , RAWLINS, David, Alexander , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , WALLIS, Nicola, Gail
发明人： CURRY, Jayne, Elizabeth , LYONS, John, Francis , RAWLINS, David, Alexander , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , WALLIS, Nicola, Gail
IPC分类号： A61K31/4184 , A61P25/00 , A61P31/04 , A61P35/00
CPC分类号： A61K31/4184 , Y02A50/469 , Y02A50/475 , Y02A50/478 , Y02A50/483
摘要： The invention provides a compound of Formula (I): or salts, solvates or tautomers thereof, for use: a) in the prophylaxis or treatment of a disease state or condition mediated by a kinase, or a mutated form thereof, which isa member of the AXL family, or the PKC family, or the CSF-1/PDGF receptor subfamily, or the Mitogen- and stress-activated kinase family, or the DAP kinase-related apoptosis-inducing protein kinase family; or is a Salt-inducible kinase; or is a member of the 90k Da ribosomal S6 kinase family, or the p21 activated kinase (PAK) family, or the Brain specific kinase family, or the Tousled-like kinase (TLK) family; or b) as an antibacterial agent; or c) as a neuroprotective agent, an immunosuppressive agent or anti-osteolytic agent; or d) in the prophylaxis or treatment of a disease or condition selected from the following: pain; coronary artery disease, myocardial contraction, cardiomyopathy, cardiac remodelling, and heart failure, hypertension, systemic vascular diseases and a range of lung conditions, lung injury;disease states or conditions resulting in excessive bone formation;bone diseases; and diseases in which bone resorption mediates morbidity;proliferative vitreoretinopathy, liver fibrosis, renal failure, irritable bowel syndrome, oxidative stress-related neurodegenerative disorders and diabetic nephro- and neuropathy;cerebral ischemia, Coffin-Lowry syndrome, Borna disease, spinocerebellarataxia type 14, schizophrenia, transplant rejection, organ transplantation, resistance to transplantation, graft vs. host disease, pancreatitis and metal poisoning;pancreatic adenocarcinoma, gastric adenocarcinomas; invasive and/or metastatic breast cancer; metastasis from various cancers;adenopathy, hepatosplenomegaly, and circulating lymphoblasts; andallodynia and hyperalgesia.
摘要翻译：本发明提供式（I）的化合物或其盐，溶剂合物或互变异构体，其用途为：a）预防或治疗由激酶或其突变形式介导的疾病状态或病症，其为 AXL家族或PKC家族，或CSF-1 / PDGF受体亚家族，或丝裂原和应激激活的激酶家族或DAP激酶相关凋亡诱导蛋白激酶家族; 或是盐诱导型激酶; 或者是90kDa核糖体S6激酶家族，或p21激活激酶（PAK）家族，或脑特异性激酶家族或Tousled样激酶（TLK）家族的成员; 或b）作为抗菌剂; 或c）作为神经保护剂，免疫抑制剂或抗溶骨质素剂; 或d）预防或治疗选自以下的疾病或病症：疼痛; 冠状动脉疾病，心肌收缩，心肌病，心脏重塑和心力衰竭，高血压，全身血管疾病和一系列肺部病症，肺损伤;导致骨形成过多的疾病状况或病症;骨病; 骨吸收介导发病的疾病;增殖性玻璃体视网膜病变，肝纤维化，肾衰竭，肠易激综合征，氧化应激相关神经变性疾病和糖尿病性肾病和神经病变;脑缺血，棺木 - Lowry综合征，博尔纳病，14型脊髓小脑下垂，精神分裂症，移植排斥反应，器官移植，抵抗移植，移植物抗宿主病，胰腺炎和金属中毒;胰腺腺癌，胃腺癌; 侵袭性和/或转移性乳腺癌; 各种癌症的转移;腺病，肝脾肿大和循环淋巴母细胞; 痛觉过敏和痛觉过敏。

2. 发明申请

WO2006077424A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006077424A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000204
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , CURRY, Jayne, Elizabeth , LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , THOMPSON, Kyla, Merriom , WYATT, Paul, Graham
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).
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是基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是键，SO 2，C = O，NR C（C = O）或O（C = O），其中R 0，是任选被羟基或C 1-4烷氧基取代的氢或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; 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，并且其中烃基中的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）。

3. 发明申请

WO2006077425A1 COMBINATIONS OF PYRAZOLE KINASE INHIBITORS AND FURTHER ANTITUMOR AGENTS 审中-公开
标题翻译：吡唑激酶抑制剂和进一步抗肿瘤药物的组合
公开(公告)号：WO2006077425A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000206
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , CURRY, Jayne, Elizabeth , LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , THOMPSON, Kyla, Merriom , WYATT, Paul, Graham
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： A61K31/4155 , A61K31/341 , A61K31/44 , A61K31/496 , A61K31/5355 , A61K31/00 , 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 R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C=O, NR 9 (C=O) or 0(C=O) wherein R 9 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).
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是基团R 1 -A-NR 4 - 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C 1 -4个任选被羟基或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，并且其中烃基中的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）。

4. 发明申请

WO2008007113A2 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2008007113A2
公开(公告)日：2008-01-17
申请号：PCT/GB2007/002640
申请日：2007-07-13
申请人： ASTEX THERAPEUTICS LIMITED , LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , GALLAGHER, Neil, James , CURRY, Jayne, Elizabeth
发明人： LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , GALLAGHER, Neil, James , CURRY, Jayne, Elizabeth
IPC分类号： A61K31/415 , A61K31/4453 , A61P35/00 , A61P43/00
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 R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO 2 , C=O, NR 9 (C=O) or 0(C=O) wherein R 9 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, 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; or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C 1-4 alkoxy; R 3 is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C 1-4 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是基团R 1 -A-NR 4 - 或5或6元碳环或杂环; A是一个键，SO 2，C = O，NR 9（C = O）或O（C = O）其中R 9，是任选被羟基或C 1-4烷氧基取代的氢或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; 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，羟基，C 1-4烷氧基，氨基，一或二-C 1的取代基取代的C 1-8烃基，具有3至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选自下列的原子或基团取代：O， S，NH，SO，SO 2; R 2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烷基; R 3选自具有3至12个环成员的氢和碳环和杂环基; R 4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。

5. 发明申请

WO2006077428A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006077428A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000210
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , CURRY, Jayne, Elizabeth , LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , THOMPSON, Kyla, Merriom , WYATT, Paul, Graham
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 R 1 -A-NR 4 - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO 2 , C=O, NR 9 (C=O) or 0(C=O) wherein R 9 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).
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，C = O，NR 9（C = O）或O（C = O）其中R 9，是任选被羟基或C 1-4烷氧基取代的氢或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; 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，并且其中烃基中的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

WO2008001115A2 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2008001115A2
公开(公告)日：2008-01-03
申请号：PCT/GB2007/002447
申请日：2007-06-29
申请人： ASTEX THERAPEUTICS LIMITED , CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil, Thomas
发明人： CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil, Thomas
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-1 H-benzoimidazol-2-yl)-1 H-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 R 1 , 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] - 脲，其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R 1，E，A和M如权利要求中所定义。

7. 发明申请

WO2008001101A2 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2008001101A2
公开(公告)日：2008-01-03
申请号：PCT/GB2007/002428
申请日：2007-06-29
申请人： ASTEX THERAPEUTICS LIMITED , CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil, Thomas
发明人： CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil, Thomas
IPC分类号： A61K31/4155 , A61K31/416 , A61K31/4415 , A61K31/445 , A61K31/5377 , A61P35/00 , A61P43/00
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. 发明申请

WO2007077435A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007077435A1
公开(公告)日：2007-07-12
申请号：PCT/GB2006/004954
申请日：2006-12-29
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , GILL, Adrian, Liam , LYONS, John, Francis
发明人： BERDINI, Valerio , CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , GILL, Adrian, Liam , LYONS, John, Francis
IPC分类号： A61K31/4155 , A61K31/4184 , C07D403/04 , A61P35/00
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： The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDKl , Chk (e.g. Cbkl or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); 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 T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I 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; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I’), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbBl), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I’) : or a salt, solvate, tautomer or N-oxide thereof; wherein R 0’ , R 1 , R 1’ , R 2’ , R 3’ , R 4’ , A’, X’, E, A and M are as defined in the claims.
摘要翻译：化合物用于制备用于预防或治疗以下药物的用途：A.由BCR-abl，VEGFR，PDGFR，EGFR，Flt3，JAK（例如JAK2或JAK3）的激酶介导的疾病状态或病症，，C-abl，PDK1，Chk（例如Cbk1或Chk2），FGFR（例如FGFR3），Ret，Eph（例如EphB2或EphB4）或Src（例如cSrc）; 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T670I突变; 或（g）PDGFR中的T674I突变; 或（h）EGFR中的T790M突变; 或（i）abl中的T315I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; 或D.由包含与其它癌症药物结合或与其它癌症药剂相互作用而不与式（I）或（I'）化合物结合或相互作用的蛋白质区域中的突变的激酶介导的疾病，例如选自c-abl，c-kit，PDGFR（包括PDGFR-β和PDGFR-α）的突变激酶和ErbB家族成员如EGFR（ErbB1），HER2（ErbB2），ErbB3和ErbB4，Ephrin受体家族的成员包括EK1A1，EphA2，EphA3，EphA4，EphA5，EphA8，EphA10，EphB1，EphB2，EphB3，EphB5，EphB6，c-Src和JAK家族的激酶如TYK2; 其中所述化合物是式（I或I'）的化合物：或其盐，溶剂合物，互变异构体或N-氧化物; 其中R 0'，R'1，R 1'，R 2'，R 3'， R 4，S 4，A'，X'，E，A和M如权利要求中所定义。

9. 发明公开

EP1968579A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：EP1968579A1
公开(公告)日：2008-09-17
申请号：EP06831505.0
申请日：2006-12-29
申请人： Astex Therapeutics Limited
发明人： BERDINI, Valerio , CURRY, Jayne, Elizabeth , GALLAGHER, Neil, James , GILL, Adrian, Liam , LYONS, John, Francis
IPC分类号： A61K31/4155 , A61K31/4184 , C07D403/04 , A61P35/00
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： The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDKl , Chk (e.g. Cbkl or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); 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 T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I 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; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I’), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbBl), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I’) : or a salt, solvate, tautomer or N-oxide thereof; wherein R0’, R1, R1’, R2’, R3’, R4’, A’, X’, E, A and M are as defined in the claims.

10. 发明公开

EP2049106A2 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：EP2049106A2
公开(公告)日：2009-04-22
申请号：EP07766218.7
申请日：2007-07-13
申请人： Astex Therapeutics Limited
发明人： LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , GALLAGHER, Neil, James , CURRY, Jayne, Elizabeth
IPC分类号： A61K31/415 , A61K31/4453 , A61P35/00 , A61P43/00
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（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，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12个环成员的碳环或杂环基团的取代基取代的C 1-8烃基，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; C1-4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; 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，羟基或C 1-4烷氧基取代的C 1-4烃基。

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