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1. 发明申请

WO2007125310A3 PHARMACEUTICAL COMBINATIONS OF PK INHIBITORS AND OTHER ACTIVE AGENTS 审中-公开
公开(公告)号：WO2007125310A3
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001502
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , THOMPSON, Neil, Thomas , LYONS, John, Francis , BOYLE, Robert, George , GRIMSHAW, Kyla, Merriom , GARRETT, Michelle, Dawn , COLLINS, Ian
发明人： THOMPSON, Neil, Thomas , LYONS, John, Francis , BOYLE, Robert, George , GRIMSHAW, Kyla, Merriom , GARRETT, Michelle, Dawn , COLLINS, Ian
IPC分类号： A61K31/52 , A61K31/5377 , A61K45/06 , A61P35/00 , A61P43/00
摘要： The invention provides a combination for use as a protein kinase B inhibitor, the combination comprising (or consisting essentially of) an ancillary compound and: (I) a compound of the formula: or salts, solvates, tautomers or N-oxides thereof, wherein R 1 , Q 1 , Q 2 , E, G, T, R 4 , J 1 and J 2 are as defined in the claims; or (II) a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein R 1 , R 2 , R 3 , R 4 , E, A, T, J 1 and J 2 are as defined in the claims.

2. 发明申请

WO2006136837A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006136837A2
公开(公告)日：2006-12-28
申请号：PCT/GB2006/002297
申请日：2006-06-21
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , THOMPSON, Neil, Thomas , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle, Dawn , LYONS, John, Francis , THOMPSON, Kyla, Merriom
发明人： THOMPSON, Neil, Thomas , BOYLE, Robert, George , COLLINS, Ian , GARRETT, Michelle, Dawn , LYONS, John, Francis , THOMPSON, Kyla, Merriom
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 R 1 and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , 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 NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom α with respect to the NR 2 R 3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R 1 is an aryl or heteroaryl group; and R 2 , R 3 , R 4 and R 5 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，在R 1和R 2之间延伸的最大链长为5个原子的连接基团和4个原子的最大链长度在E和NR 2 R 3之间延伸，其中连接基团中的一个碳原子可以任选被氧或氮原子取代; 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位于碳原子a时，并且条件是当存在的氧代基位于相对于NR 2 R 3 O 3的碳原子a时，组; E是单环或双环碳环或杂环基; R 1是芳基或杂芳基; 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。

3. 发明申请

WO2008007122A3 COMBINATIONS OF PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDKS AND GSK'S 审中-公开
公开(公告)号：WO2008007122A3
公开(公告)日：2008-01-17
申请号：PCT/GB2007/002654
申请日：2007-07-13
申请人： ASTEX THERAPEUTICS LIMITED , LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , GALLAGHER, Neil, James
发明人： LYONS, John, Francis , SQUIRES, Matthew, Simon , THOMPSON, Neil, Thomas , GALLAGHER, Neil, James
IPC分类号： A61K31/454 , A61P35/00
摘要： A combination comprising (a) a compound of formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is 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 to 3 carbon atoms; R 1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or an optionally substituted C 1-8 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, 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 R 4 is hydrogen or a C 1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or C 1-4 alkoxy; and (b) a compound of formula (I'") or salts, tautomers, solvates and N-oxides thereof: wherein R 1 is 2,6-dichlorophenyl; R 2a and R 2b are both hydrogen; and R 3 is a group: formula (A) where R 4 is C 1-4 alkyl.

4. 发明申请

WO2006040569A1 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噻吩类化合物
公开(公告)号：WO2006040569A1
公开(公告)日：2006-04-20
申请号：PCT/GB2005/003957
申请日：2005-10-14
申请人： ASTEX THERAPEUTICS LIMITED , 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 , A61K31/5377 , A61K31/496 , A61K31/4439 , 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，溶剂合物或N-氧化物，其中：R

5. 发明申请

WO2008044041A1 PHARMACEUTICAL COMBINATIONS 审中-公开
标题翻译：药物组合
公开(公告)号：WO2008044041A1
公开(公告)日：2008-04-17
申请号：PCT/GB2007/003879
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： 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 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 inhibitors.
摘要翻译：本发明提供了包含（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烃基氧基; R 4选自氢; 其中n为0或1，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抑制剂的活性。

6. 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。

7. 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。

8. 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 -

9. 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。

10. 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）。

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