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1. 发明申请

WO2010139932A3 METHOD AND SYSTEM FOR CONFIGURING CRUDE OIL DISPLACEMENT SYSTEM 审中-公开
标题翻译：用于配置原油排放系统的方法和系统
公开(公告)号：WO2010139932A3
公开(公告)日：2011-04-28
申请号：PCT/GB2010001038
申请日：2010-05-26
申请人： BP EXPLORATION OPERATING , COLLINS IAN RALPH , HOUSTON STEPHANIE JANE , WEBB KEVIN JOHN
发明人： COLLINS IAN RALPH , HOUSTON STEPHANIE JANE , WEBB KEVIN JOHN
IPC分类号： E21B43/20
CPC分类号： E21B44/00 , C09K8/58 , E21B43/16 , E21B43/20 , G05B17/02
摘要： A computer-implemented method for determining one or more operating modes for a crude oil displacement system is provided. The crude oil displacement system is arranged to inject an aqueous displacement fluid into one or more reservoirs, each reservoir comprising a porous and permeable rock formation, wherein crude oil and formation water are contained within a pore space of the rock formation. The crude oil displacement system is for use in displacing crude oil from the pore space of the rock formation. The computer-implemented method comprises the steps of receiving measurement data associated with one or more chemical characteristics of the displacement fluid and one or more chemical characteristics of the rock formation, the crude oil and the formation water of the one or more reservoirs, and inputting the measurement data and data representing a predetermined volume of oil into a computer-implemented predictive model. The predictive model is operated so as to generate predicted data indicative of a predicted additional amount of oil, compared to the predetermined volume of oil, that will be displaced by configuring the crude oil displacement system so as to inject the displacement fluid having the chemical characteristics into the one or more reservoirs. On the basis of the predicted data, the one or more operating modes of the crude oil displacement system are determined. A further computer-implemented method employing the predictive model in which predicted data indicative of one or more predicted chemical characteristics of the displacement fluid are generated is also provided. Additionally, a system for configuring a crude oil displacement system is provided.
摘要翻译：提供了一种用于确定原油排放系统的一种或多种操作模式的计算机实现的方法。原油置换系统被布置成将含水置换流体注入到一个或多个储存器中，每个储存器包括多孔和可渗透的岩层，其中原油和地层水被包含在岩层的孔隙空间内。原油排放系统用于从岩层孔隙空间中排除原油。计算机实现的方法包括以下步骤：接收与位移流体的一种或多种化学特性相关联的测量数据和一个或多个储层的岩层，原油和地层水的一种或多种化学特征，以及输入测量数据和表示预定体积的油的数据转换成计算机实现的预测模型。操作该预测模型，以产生指示与预定体积的油相比预测的附加量的油的预测数据，该预定数据将通过配置原油排出系统而移位，以便注入具有化学特性的置换流体进入一个或多个水库。根据预测数据，确定原油排放系统的一种或多种运行模式。还提供了采用预测模型的另外的计算机实现的方法，其中产生指示位移流体的一种或多种预测化学特性的预测数据。另外，提供了一种用于配置原油排放系统的系统。

2. 发明申请

WO2009060177A8 METHOD OF INJECTING CARBON DIOXIDE 审中-公开
标题翻译：注射二氧化碳的方法
公开(公告)号：WO2009060177A8
公开(公告)日：2010-06-10
申请号：PCT/GB2008003684
申请日：2008-10-30
申请人： BP EXPLORATION OPERATING , COLLINS IAN RALPH , MASON ANDREW RUSSELL
发明人： COLLINS IAN RALPH , MASON ANDREW RUSSELL
IPC分类号： E21B43/16
CPC分类号： E21B43/164 , Y02C10/14 , Y02P90/70
摘要： A method of storing CO2 in a porous and permeable hydrocarbon reservoir having at least one injection well and at least one production well penetrating said reservoir, which method comprises the steps of: (a) recovering a produced fluid stream comprising produced hydrocarbons, produced water, and produced CO2 from the production well; (b) passing the produced fluid stream to a production facility where a produced vapour stream comprising carbon dioxide and volatile hydrocarbons is separated from the produced fluid stream; (c) compressing the produced vapour stream to above the cricondenbar for the composition of the produced vapour stream; (d) cooling the compressed stream thereby forming a cooled stream that is in a dense phase state; (e) importing a CO2 stream to an injection facility wherein the imported CO2 is either in a liquid state or a supercritical state; (f) mixing the cooled stream from step (d) with the imported CO2 stream thereby forming a co-injection stream; and (g) injecting the co-injection stream into the hydrocarbon bearing reservoir from said injection well.
摘要翻译：一种将CO 2储存在具有至少一个注入井和穿过所述储存器的至少一个生产井的多孔且可渗透的烃储层中的方法，所述方法包括以下步骤：（a）回收包含生成的烃，生产水，从生产井中产出二氧化碳; （b）将产生的流体流送到生产设施，其中产生的包含二氧化碳和挥发性烃的蒸汽流与所产生的流体流分离; （c）将所产生的蒸气流压缩至产生的蒸气流的组成的三环网以上; （d）冷却压缩流，从而形成处于密相状态的冷却流; （e）向注入设施输入二氧化碳流，其中进口的二氧化碳处于液态或超临界状态; （f）将来自步骤（d）的冷却流与进口的CO 2流混合，从而形成共注射流; 和（g）从所述喷射井将共注射流注入含烃储层。

3. 发明申请

WO2008075110A1 SUBSTITUTED PIPERIDINES CONTAINING A HETEROARYLAMIDE OR HETEROARYLPHENYL MOIETY 审中-公开
标题翻译：含有异烟酰胺或邻苯二酚的取代的哌啶
公开(公告)号：WO2008075110A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050777
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard William, Arthur , MATUSIAK, Zbigniew, Stanley , CARR, Gregory, Richard , MORRIS, Jeffrey, James , CHEUNG, Kwai, Ming
IPC分类号： C07D487/04 , C07D473/34 , C07D471/04 , A61K31/519 , A61P35/00
CPC分类号： C07D473/34 , C07D487/04
摘要： The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R )x N * (GP1) (2) GP is a group GP2: 10 (R )r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claims
摘要翻译：本发明提供具有式（I）的PKA和PKB激酶抑制化合物的式（I）化合物：GP 1 JT 2 JN 4 RNH（I）或其盐，溶剂合物，互变异构体或N-氧化物，其中（1） GP是组GP1：HET 2a a QG（HNCO）f 7（R）x N *（GP1）（2）GP是组GP2：10（R）r O 2a a QG（CH 2）w NVHN * ）其中HET是含有至多4个杂原子环成员的单环或双环杂环基; 环V是5至10个环成员的单环或双环杂芳基; 并且J1，J2，R4，R7，R10，Q2a，Ga，x，w和f如权利要求中所定义

4. 发明申请

WO2007125321A3 PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：作为药物化合物的嘌呤和多巴林衍生物
公开(公告)号：WO2007125321A3
公开(公告)日：2007-12-27
申请号：PCT/GB2007001518
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , DAVIES THOMAS GLANMOR , GARRETT MICHELLE DAWN , BOYLE ROBERT GEORGE , COLLINS IAN
发明人： DAVIES THOMAS GLANMOR , GARRETT MICHELLE DAWN , BOYLE ROBERT GEORGE , COLLINS IAN
IPC分类号： A61K31/52 , A61K31/4523 , A61K31/519 , A61K31/522 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/00 , C07D471/04 , C07D473/34 , C07D487/04
CPC分类号： C07D471/04 , C07D473/34 , C07D487/04
摘要： The invention provides a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q 1 is a bond or a saturated C 1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, 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 may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen; R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase P70S6K is indicated.
摘要翻译：本发明提供式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中T为N或CR 5; J 1是N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q 1是一个键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选地被氧或氮原子代替，或相邻的一对碳原子可以被CONR Q或Q Q取代，其中R q是氢或甲基，或R 0 q是与R 1连接的C 1-4亚烷基链或Q 1的碳原子以形成环状的部分; 并且其中连接基团Q 1的碳原子可以任选地具有一个或多个选自氟和羟基的取代基; Q 2是含有1至3个碳原子的键或饱和烃连接基团，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; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q 2不是键; G是氢，NR 2 R 3，OH或SH，条件是当E是芳基或杂芳基且Q 2是键时，则G 是氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3 ，则Q 2是一个键; 和R 2，R 3，R 4，R 6和R 8，如权利要求中所定义，其中所述化合物用于：（a）治疗或预防其中指示调节（例如抑制）ROCK激酶或蛋白激酶P70S6K的疾病或病症; 和/或（b）治疗其中指示调节（例如抑制）ROCK激酶或蛋白激酶P70S6K的受试者或患者群体。}

5. 发明申请

WO2007125315A3 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125315A3
公开(公告)日：2007-12-27
申请号：PCT/GB2007001510
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , DAVIES THOMAS GLANMOR , GARRETT MICHELLE DAWN , BOYLE ROBERT GEORGE , COLLINS IAN
发明人： DAVIES THOMAS GLANMOR , GARRETT MICHELLE DAWN , BOYLE ROBERT GEORGE , COLLINS IAN
IPC分类号： C07D471/04 , A61K31/407 , A61K31/4188 , A61P9/00 , A61P35/00 , A61P37/00 , C07D473/00 , C07D473/34 , C07D487/04
CPC分类号： C07D473/34 , C07D471/04 , C07D473/00 , C07D487/04
摘要： The invention provides a compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); A is an optionally substituted saturated C 1-7 hydrocarbon 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 , one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH 2 , O, S or NH and G is a C 1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R 1 is hydrogen or an aryl or heteroaryl group; R 2 and R 3 are each hydrogen, optionally substituted C 1-4 hydrocarbyl or optionally substituted C 1-4 acyl; or NR 2 R 3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR 2 R 3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C 1-4 alkyl; or NR 2 R 3 and the adjacent carbon atom of linker group A together form a cyano group; or R 1 , A and NR 2 R 3 together form a cyano group; and R 4 , R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen and various substituents as defined in the claims, wherein the compound is for use in: (a) the treatment or prophylaxis of a disease or condition in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated; and/or (b) the treatment of a subject or patient population in which the modulation (e.g. inhibition) of ROCK kinase or protein kinase p70S6K is indicated.
摘要翻译：本发明提供具有式（I）的化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T是N或CR 5; J 1是N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; A是在R 1和R 2之间延伸的最大链长为5个原子的任选取代的饱和C 1 -C 7烃连接基团连接基团中的一个碳原子是任选的，并且在E和NR 2 R 3之间延伸的最大链长为4个原子用氧或氮代替; E是单环或双环碳环或杂环基或非环基XG，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链其中一个碳原子任选被O，S或NH取代; R 1是氢或芳基或杂芳基; R 2和R 3各自为氢，任选取代的C 1-4 - 烃基或任选取代的C 1-4 - >酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 或NR 2 R 3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4烷基取代，烷基; 或NR 2 R 3和连接基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 和R 4，R 5，R 6，R 7和R 8，各自独立地选自氢和权利要求中定义的各种取代基，其中所述化合物用于：（a）治疗或预防其中调节（例如抑制）ROCK激酶或蛋白激酶p70S6K的疾病或病症被指示和/或（b）治疗其中指示ROCK激酶或蛋白激酶p70S6K的调节（例如抑制）的受试者或患者群体。}

6. 发明申请

WO2007125325A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2007125325A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001522
申请日：2007-04-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
发明人： WOODHEAD, Steven, John , HAMLETT, Christopher , SORE, Hannah, Fiona , WALKER, David, Winter , VERDONK, Marinus, Leendert , COLLINS, Ian , CALDWELL, John , CHEUNG, Kwai-Ming , DA FONSECA MCHARDY, Tatiana, Faria
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/00 , C07D473/34
摘要： The invention provides compounds of the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein J 1 -J 2 is CH=CH, N=CH, CH=N, HN-C(O) or CH 2 CO; T is N or CH and GP is as defined in the claims. The compounds have activity as inhibitors of PKA and PKB kinases and are useful in the treatment of cancers.
摘要翻译：本发明提供了式（I）化合物或其盐，溶剂化物，互变异构体或N-氧化物，其中J 1是H，CH = CH，N = CH，CH = N，HN-C（O）或CH 2 CO; T是N或CH，GP如权利要求中所定义。该化合物具有作为PKA和PKB激酶抑制剂的活性，可用于治疗癌症。

7. 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.

8. 发明申请

WO2006111712A2 IONIC LIQUIDS AND USES THEREOF 审中-公开
标题翻译：离子液体及其用途
公开(公告)号：WO2006111712A2
公开(公告)日：2006-10-26
申请号：PCT/GB2006/001359
申请日：2006-04-13
申请人： BP P.L.C. , COLLINS, Ian, Ralph , EARLE, Martyn, John , EXTON, Simon, Peter , PLECHKOVA, Natalia, Vladimirovna , SEDDON, Kenneth, Richard
发明人： COLLINS, Ian, Ralph , EARLE, Martyn, John , EXTON, Simon, Peter , PLECHKOVA, Natalia, Vladimirovna , SEDDON, Kenneth, Richard
IPC分类号： B01F17/18 , B01F17/20 , B01F17/32 , B01F17/00 , B01F17/02 , B01F17/10 , B01F17/12 , B01F17/14
CPC分类号： C09K8/584 , B01F17/0042 , B01F17/0057 , B01F17/0064 , B01F17/0078 , B01F17/0085 , C07D213/02 , C07D233/58 , C07F9/5407 , C07F9/5456
摘要： The invention provides a water in oil or oil in water emulsion which comprises a (i) an oil phase, (ii) an aqueous phase and (iii) an ionic liquid surfactant wherein the ionic liquid surfactant is a salt of general formula (I): C + A - (I) the salt of general formula (I) existing in a liquid state at a temperature below 15O 0 C; at least one of the cation, C + , and anion, A - , comprising a hydrophobic tail group attached to an ionic head group; and A - represents an anion containing phosphorus, or an alkyl sulfate anion of general formula: ROSO 3 - wherein R is an alkyl group having at least 8 carbon atoms. Various novel ionic liquid salts in which at least one of the cation and anion comprises a hydrophobic tail group attached to an ionic head group, are also provided by the invention.
摘要翻译：本发明提供一种水包油或水包油乳液，其包含（i）油相，（ii）水相和（iii）离子液体表面活性剂，其中离子液体表面活性剂是通式（I）的盐，（I）在低于150℃的温度下以液态存在的通式（I）的盐;（I）通式（I）的盐，包含与离子头基团连接的疏水性尾基的至少一个阳离子C + +和阴离子，并且A 表示含有磷的阴离子或通式为ROSO 3的烷基硫酸盐阴离子。

9. 发明申请

WO2006046024A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046024A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004119
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , WALKER, David, Winter , WOODHEAD, Steven, John , WYATT, Paul, Graham , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria
IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , A61K31/4545 , A61K31/519 , A61K31/52 , A61K31/522 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J l -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Q 1 is a bond or a saturated C 1-3 hydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONR q or NR q CO where R q is hydrogen or methyl, or R q is a C 1-4 alkylene chain linked to R 1 or a carbon atom of Q 1 to form a cyclic moiety; and wherein the carbon atoms of the linker group Q 1 may optionally bear one or more substituents selected from fluorine and hydroxy; Q 2 is a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, 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 may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Q 2 is other than a bond; G is hydrogen, NR 2 R 3 , OH or SH provided that when E is aryl or heteroaryl and Q 2 is a bond, then G is hydrogen; R 1 is hydrogen or an aryl or heteroaryl group, with the proviso that when R 1 is hydrogen and G is NR 2 R 3 , then Q 2 is a bond; and R 2 , R 3 , R 4 , R 6 and R 8 are as defined in the claims.
摘要翻译：本发明提供了用作蛋白激酶B抑制剂的化合物，该化合物是式（I）化合物或其盐，溶剂合物，互变异构体或N-氧化物，其中T是N或CR 5 >; N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; E是5或6个环成员的单环碳环或杂环基，杂环基含有至多3个选自O，N和S的杂原子; Q 1是一个键或饱和的C 1-3烃连接基团，连接基团中的一个碳原子任选地被氧或氮原子代替，或相邻的一对碳原子可以被CONR Q或Q Q取代，其中R q是氢或甲基，或R 0 q是与R 1连接的C 1-4亚烷基链或Q 1的碳原子以形成环状的部分; 并且其中连接基团Q 1的碳原子可以任选地具有一个或多个选自氟和羟基的取代基; Q 2是含有1至3个碳原子的键或饱和烃连接基团，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; 并且其中所述连接基团的碳原子可以任选地具有一个或多个选自氟和羟基的取代基，条件是当存在的羟基不相对于G基团位于碳原子a时; 并且条件是当E是芳基或杂芳基时，则Q 2不是键; G是氢，NR 2 R 3，OH或SH，条件是当E是芳基或杂芳基且Q 2是键时，则G 是氢; R 1是氢或芳基或杂芳基，条件是当R 1是氢并且G是NR 2 R 3 ，则Q 2是一个键; 和R 2，R 2，R 3，R 4，R 4， SUP＆gt;和R＆gt; 8如权利要求中所定义。}

10. 发明申请

WO2006046023A1 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的ORTHO-浓缩的吡啶和吡嗪衍生物（E.G.PININES）
公开(公告)号：WO2006046023A1
公开(公告)日：2006-05-04
申请号：PCT/GB2005/004115
申请日：2005-10-25
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria , DONALD, Alastair
发明人： BERDINI, Valerio , BOYLE, Robert, George , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , SORE, Hannah, Fiona , CALDWELL, John , COLLINS, Ian , DA FONSECA, Tatiana, Faria , DONALD, Alastair
IPC分类号： A61K31/52 , A61K31/519 , C07D473/34 , A61K31/437 , C07D471/04 , C07D487/04 , C07D473/00
CPC分类号： C07D471/04 , C07D473/00 , C07D473/34 , C07D487/04
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N-C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); A is an optionally substituted saturated C 1-7 hydrocarbon 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 , one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH 2 , O, S or NH and G is a C 1-4 alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R 1 is hydrogen or an aryl or heteroaryl group; R 2 and R 3 are each hydrogen, optionally substituted C 1-4 hydrocarbyl or optionally substituted C 1-4 acyl; or NR 2 R 3 forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR 2 R 3 and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C 1-4 alkyl; or NR 2 R 3 and the adjacent carbon atom of linker group A together form a cyano group; or R 1 , A and NR 2 R 3 together form a cyano group; and R 4 , R 5 , R 6 , R 7 and R 8 are each independently selected from hydrogen and various substituents as defined in the claims.
摘要翻译：本发明提供了一种用于预防或治疗由蛋白激酶B介导的疾病状态或病症的化合物，其具有式（I）：或其盐，溶剂合物，互变异构体或N-氧化物，其中T为N或 CR ^{5 ; J 1是N = C（R 6），（R 7）C = N，（R 8）NC（O），（R 8）2 CC（O），N = N或（R 7））C = C（R ^{6 ）; A是在R 1和R 2之间延伸的最大链长为5个原子的任选取代的饱和C 1 -C 7烃连接基团连接基团中的一个碳原子是任选的，并且在E和NR 2 R 3之间延伸的最大链长为4个原子用氧或氮代替; E是单环或双环碳环或杂环基或非环基XG，其中X是CH 2，O，S或NH，G是C 1-4亚烷基链其中一个碳原子任选被O，S或NH取代; R 1是氢或芳基或杂芳基; R 2和R 3各自为氢，任选取代的C 1-4 - 烃基或任选取代的C 1-4 - >酰基; 或NR 2 R 3形成具有4-7个环成员的咪唑基或饱和单环杂环基; 或NR 2 R 3和A一起形成具有4-7个环成员的饱和单环杂环基，其任选被C 1-4烷基取代，烷基; 或NR 2 R 3和连接基团A的相邻碳原子一起形成氰基; 或R 1，A和NR 2 R 3一起形成氰基; 和R 4，R 5，R 6，R 7和R 8，各自独立地选自氢和权利要求中所定义的各种取代基。}}

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