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

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

WO2008044034A1 HYDROBENZAMIDE DERIVATIVES AS INHIBITORS OF HSP90 审中-公开
标题翻译：盐酸衍生物作为HSP90的抑制剂
公开(公告)号：WO2008044034A1
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003871
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
发明人： FREDERICKSON, Martyn , LYONS, John, Francis , THOMPSON, Neil, Thomas , VINKOVIC, Mladen , WILLIAMS, Brian , WOODHEAD, Andrew James , WOOLFORD, Alison, Jo-Anne
IPC分类号： C07D209/44 , C07C65/05 , C07C69/02 , A61P35/00 , A61K31/496
CPC分类号： C07C67/317 , C07C59/08 , C07C67/313 , C07C69/92 , C07C235/60 , C07D209/44
摘要： The invention provides an acid addition salt of a compound of the formula (1) Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
摘要翻译：本发明提供式（1）化合物的酸加成盐本发明还提供了制备式（1）化合物及其烷基类似物的方法，用于该方法的新中间体和制备中间体的方法。本发明还提供式（1）化合物及其乙基类似物的新的医学用途。

3. 发明申请

WO2008044029A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2008044029A1
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003864
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil Thomas , YULE, Stephen, Murray , MURRAY, Christopher William
发明人： GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil Thomas , YULE, Stephen, Murray , MURRAY, Christopher William
IPC分类号： A61K31/403
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 R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; optionally substituted C 1-5 hydrocarbyl and optionally substituted C 1- 5 hydrocarbyloxy; R 4 is selected from hydrogen; a group -(O) n -R 7 where n is 0 or 1 and R 7 is an optionally substituted acyclic C 1-5 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-C 1- 5 hydrocarbyl-amino; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR 5 R 6 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R 1是羟基或氢; R 2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; R 3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; R 4选自氢; 其中n为0或1且R 7为任选取代的无环C 1 - （O）N - ， - -5个烃基或具有3〜7个环成员的单环碳环或杂环基; 卤素; 氰基; 羟基; 氨基; 和任选取代的单 - 或二-C 1 - 5 -

4. 发明申请

WO2008044027A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2008044027A2
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003860
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
发明人： CONGREVE, Miles Stuart , FAZAL, Lyndsey Helen , FREDERICKSON, Martyn , MURRAY, Christopher William , O'BRIEN, Michael Alistair , WOODHEAD, Andrew James , LYONS, John, Francis , THOMPSON, Neil Thomas
CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18
摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl 0 ) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is„ hydrogen, hydroxy, or O-R z; R 2a is hydroxy, methoxy or O-R z; provided that at least one of R 1 and R 2a is O-R z; R z is L p -R p1 ; SO 3 H; a glucuronide residue; a mono-, di- or tripeptide residue; or; L p is a bond, C=O, (C=O)O, (C=O)NR p1 or S(O) x NR p1 ; x is 1 or 2; R p1 is hydrogen or a an optionally substituted C 1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that R p1 is not hydrogen when L p is a bond, C=O or (C=O)O; and provided also that O-R z does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group R p1; and R 3 , R 4a , R 8 and R 10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R 1 and/or R 2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
摘要翻译：本发明提供了一种用于医药的化合物，该化合物为下式化合物：其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团选自：结构C1，C5和C6：其中n为0,1,2或3; R 1是氢，羟基或OR z; R 2是羟基，甲氧基或OR z; O / O >条件是R 1和R 2 2中的至少一个是OR z; R z是L SUP > p p> SO 3 H;葡糖苷酸残基;单 - ，二 - 或三肽残基;或●L < / SUP>是键，C = O，（C = O）O，（C = O）NR P1或S（O）x NR 6 x为1或2; R p1为氢或任选取代的含0,1或2个碳环的C 1-25烃基和0 ，1,2,3,4,5或6个碳 - 碳多重键，条件是当P = O时，R p2不是氢，C = O或（C = O）O;并且也提供OR 0不含0-0部分;并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，每个是基团R p1; R 3和R 3，R 4a，R 8和R 10 是定义在权利要求中。式（V10）化合物是其中R 1和/或R 2a的羟基的母体化合物的前体药物，其中母体化合物具有Hsp90抑制活性。

5. 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）。

6. 发明申请

WO2008007113A3 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2008007113A3
公开(公告)日：2008-10-23
申请号：PCT/GB2007002640
申请日：2007-07-13
申请人： ASTEX THERAPEUTICS LTD , 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（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; 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烃氧基，氨基，单或二-C 1 -C 4烷基的取代基取代的C 1-8 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以下的原子或基团替代：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烃基; R 3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。}

7. 发明申请

WO2008044027A3 PHARMACEUTICAL COMPOUNDS HAVING HSP90 INHIBITORY OR MODULATING ACTIVITY 审中-公开
标题翻译：具有HSP90抑制或调节活性的药物化合物
公开(公告)号：WO2008044027A3
公开(公告)日：2008-06-19
申请号：PCT/GB2007003860
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LTD , CONGREVE MILES STUART , FAZAL LYNDSEY HELEN , FREDERICKSON MARTYN , MURRAY CHRISTOPHER WILLIAM , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , LYONS JOHN FRANCIS , THOMPSON NEIL THOMAS
发明人： CONGREVE MILES STUART , FAZAL LYNDSEY HELEN , FREDERICKSON MARTYN , MURRAY CHRISTOPHER WILLIAM , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , LYONS JOHN FRANCIS , THOMPSON NEIL THOMAS
IPC分类号： C07D209/08 , A61K31/438 , C07D209/44 , C07D215/08 , C07D401/04 , C07D401/12 , C07D419/10 , C07D471/04 , C07D471/10 , C07D491/08 , C07D491/10
CPC分类号： C07D403/06 , C07D209/08 , C07D209/44 , C07D215/08 , C07D215/14 , C07D217/06 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D491/08 , C07D491/10 , C07D491/107 , C07D491/18
摘要： The invention provides a compound for use in medicine, the compound being a compound of the formula (Vl 0 ) or a salt, solvate, tautomer or N-oxide thereof: wherein the bicyclic group: is selected from the structures C1, C5 and C6: wherein n is 0, 1, 2 or 3; R 1 : is" hydrogen, hydroxy, or O-R z; R 2a is hydroxy, methoxy or O-R z; provided that at least one of R 1 and R 2a is O-R z; R z is L p -R p1 ; SO 3 H; a glucuronide residue; a mono-, di- or tripeptide residue; or; L p is a bond, C=O, (C=O)O, (C=O)NR p1 or S(O) x NR p1 ; x is 1 or 2; R p1 is hydrogen or a an optionally substituted C 1-25 hydrocarbyl group containing 0, 1 or 2 carbocyclic rings and 0, 1, 2, 3, 4, 5 or 6 carbon-carbon multiple bonds, provided that R p1 is not hydrogen when L p is a bond, C=O or (C=O)O; and provided also that O-R z does not contain an 0-0 moiety; and excluding compounds wherein R1 is hydroxy and R2a is methoxy; Rp2 and Rp3 are the same or different and each is a group R p1; and R 3 , R 4a , R 8 and R 10 are defined in the claims. The compounds of formula (Vl0) are pro-drugs of parent compounds wherein R 1 and/or R 2a are hydroxy, wherein the parent compounds have Hsp90 inhibiting activity.
摘要翻译：本发明提供了一种用于医药的化合物，该化合物为下式化合物：其盐，溶剂化物，互变异构体或N-氧化物：其中双环基团选自：结构C1，C5和C6：其中n为0,1,2或3; R 1是氢，羟基或OR z; R 2是羟基，甲氧基或OR z; O / O >条件是R 1和R 2 2中的至少一个是OR z; R z是L SUP > p p> SO 3 H;葡糖苷酸残基;单 - ，二 - 或三肽残基;或●L < / SUP>是键，C = O，（C = O）O，（C = O）NR P1或S（O）x NR 6 x为1或2; R p1为氢或任选取代的含0,1或2个碳环的C 1-25烃基和0 ，1,2,3,4,5或6个碳 - 碳多重键，条件是当P = O时，R p2不是氢，C = O或（C = O）O;并且也提供OR 0不含0-0部分;并且不包括其中R 1是羟基并且R 2a是甲氧基的化合物; Rp2和Rp3相同或不同，每个是基团R p1; R 3和R 3，R 4a，R 8和R 10 是定义在权利要求中。式（V10）化合物是其中R 1和/或R 2a的羟基的母体化合物的前体药物，其中母体化合物具有Hsp90抑制活性。

8. 发明申请

WO2008044045A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2008044045A1
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003891
申请日：2007-10-12
申请人： ASTEX THERAPEUTICS LIMITED , GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil Thomas , YULE, Stephen, Murray , MURRAY, Christopher William
发明人： GALLAGHER, Neil, James , LYONS, John, Francis , THOMPSON, Neil Thomas , YULE, Stephen, Murray , MURRAY, Christopher William
IPC分类号： A61K31/438 , A61K31/439 , A61K31/403 , A61K31/00 , C07D209/44 , C07D209/08 , C07D215/08 , C07D491/10 , C07D471/04 , C07D471/10 , C07D491/08 , C07D401/04 , C07D401/12 , C07D419/10
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 R 1 is hydroxy or hydrogen; R 2 is hydroxy; methoxy or hydrogen; provided that at least one of R 1 and R 2 is hydroxy; R 3 is selected from hydrogen; halogen; cyano; optionally substituted C 1-5 hydrocarbyl and optionally substituted C 1-5 hydrocarbyloxy; R 4 is selected from hydrogen; a group -(O) n -R 7 where n is 0 or 1 and R 7 is an optionally substituted acyclic C 1-5 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-C 1-5 hydrocarbyl-amino; or R 3 and R 4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR 5 R 6 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R 1是羟基或氢; R 2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; R 3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; R 4选自氢; 其中n为0或1且R 7为任选取代的无环C 1 - （O）N - ， - -5个烃基或具有3〜7个环成员的单环碳环或杂环基; 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。

9. 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。

10. 发明申请

WO2006040569A8 THIOPHENE AMIDE COMPOUNDS FOR USE IN THE TREATMENT OR PROPHYLAXIS OF CANCERS 审中-公开
标题翻译：用于治疗或预防癌症的硫胺酰胺化合物
公开(公告)号：WO2006040569A8
公开(公告)日：2007-04-26
申请号：PCT/GB2005003957
申请日：2005-10-14
申请人： ASTEX THERAPEUTICS LTD , GILL ADRIAN LIAM , LYONS JOHN FRANCIS , THOMPSON NEIL THOMAS
发明人： GILL ADRIAN LIAM , LYONS JOHN FRANCIS , THOMPSON NEIL THOMAS
IPC分类号： A61K31/5386 , A61K31/4155 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61P35/00
CPC分类号： A61K31/4155 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/5386
摘要： The invention provides the use of a compound for the manufacture of a medicament for the prophylaxis or treatment of a cancer or a para-neoplastic effect associated with a cancer, the para-neoplastic effect being other than cachexia, and the compound being a compound of the formula (I), or a salt, solvate or N-oxide thereof, wherein: R 1 and R 2 are the same or different and each is selected from hydrogen, C 1-4 hydrocarbyl, halogen and cyano; X is selected from C=O, C=S, C(=O)NH, C(=S)NH, C(=O)O, C(=O)S, C(=S)O and C(=S)S; R 3 is an aryl or heteroaryl group of 5 to 12 ring members optionally substituted by one or more substituent groups R 7 wherein R 7 is as defined in the claims; R 4 is a group YR 5 or a group R 6 ; Y is NH, O or S; R 5 is selected from (a) optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members; and (b) optionally substituted C 1-8 hydrocarbyl 20 groups; and R 6 is an optionally substituted heterocyclic group having from 4 to 12 ring members and containing at least one ring nitrogen atom through which R 6 is linked to the adjacent carbonyl group.
摘要翻译：本发明提供化合物在制备用于预防或治疗与癌症相关的癌症或副肿瘤作用的药物中的用途，所述副肿瘤作用不是恶病质，所述化合物是化合物式（I）或其盐，溶剂化物或N-氧化物，其中：R 1和R 2相同或不同，各自选自氢， C 1-4烃基，卤素和氰基; X选自C = O，C = S，C（= O）NH，C（= S）NH，C（= O）O，C（= O）S，C（= S）O和C（= S）S; R 3是任选被一个或多个取代基R 7取代的5至12个环成员的芳基或杂芳基，其中R 7为在权利要求中限定; R 4是基团YR 5或基团R 6; Y是NH，O或S; R 5选自（a）具有3-12个环成员的任选取代的碳环和杂环基; 和（b）任选取代的C 1-8烃基20基团; 并且R 6是具有4-12个环成员并且含有至少一个环氮原子的任选取代的杂环基，R 6通过该环氮原子与相邻的羰基连接。

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