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1. 发明申请

WO2004004730A3 2-AMINOPYRAZINE DERIVATIVES AS INHIBITORS OF CYCLIN DEPENDENT KINASES FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译：作为CYCLIN依赖性激素抑制剂治疗增生性疾病的2-氨基吡嗪衍生物
公开(公告)号：WO2004004730A3
公开(公告)日：2004-04-29
申请号：PCT/GB0302905
申请日：2003-07-04
申请人： ASTEX TECHNOLOGY LTD , WOOLFORD ALISON JO-ANNE , BERDINI VALERIO , OREILLY MARC , PADOVA ALESSANDRO , SAXTY GORDON , WYATT PAUL GRAHAM
发明人： WOOLFORD ALISON JO-ANNE , BERDINI VALERIO , OREILLY MARC , PADOVA ALESSANDRO , SAXTY GORDON , WYATT PAUL GRAHAM
IPC分类号： C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/14 , A61K31/4965 , A61K31/497
CPC分类号： C07D401/12 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/14
摘要： The invention provides a compound of the general formula (I) wherein R is selected from hydrogen, cycloalkyl and cycloalkenyl having 3 to 7 ring members; phenyl-C1-4 alkyl or a group R -A-CH2-, R is selected from aryl and heteroaryl having five to twelve ring members; cycloalkyl and cycloalkenyl having 3 to 7 ring members; a group (CR R )pE-R , or R and R together with the nitrogen atom to which they are attached form a heterocyclic group having 5 to 10 ring members; R is a substituent selected from halogen, CN, N-linked monocyclic nitrogen-containing heterocyclic groups having from 3 to 7 ring members and containing up to three heteroatoms; and a group R -R . The substituents R -R R and R are defined in claim 1. The compounds have activity as inhibitors of cyclin dependent kinases and are useful in the treatment of disease states and conditions, such as proliferative diseases, mediated by cyclin dependent kinases.
摘要翻译：本发明提供了通式（I）的化合物，其中R 1选自具有3-7个环成员的氢，环烷基和环烯基; 苯基-C 1-4烷基或基团R 4 -A-CH 2 - ，R 2选自具有五至十二个环成员的芳基和杂芳基; 环烷基和具有3-7个环成员的环烯基; 一个基团（CR 6 R 7）pE-R 8或R 1和R 2与它们所连接的氮原子一起形成具有5至10个环成员的杂环基; R 3是选自具有3至7个环成员并且含有至多3个杂原子的卤素，CN，N-连接的单环含氮杂环基的取代基; 和基团R a -R b。取代基R 4 -R R a和R b如权利要求1中所定义。化合物具有作为细胞周期蛋白依赖性激酶抑制剂的活性，并且可用于治疗疾病状态和病症，例如由细胞周期蛋白依赖性激酶介导的增殖性疾病。

2. 发明申请

WO2005012256A8 3, 4-DISUBSTITUTED 1H-PYRAZOLE COMPOUNDS AND THEIR USE AS CYCLIN DEPENDENT KINASES (CDK) AND GLYCOGEN SYNTHASE KINASE-3 (GSK-3) MODULATORS 审中-公开
标题翻译： 3,4-取代的1H-吡唑类化合物及其作为依赖于细胞周期蛋白依赖性激酶（CDK）和糖原合成酶激酶-3（GSK-3）调节剂的用途
公开(公告)号：WO2005012256A8
公开(公告)日：2005-04-07
申请号：PCT/GB2004003179
申请日：2004-07-22
申请人： ASTEX TECHNOLOGY LTD , BERDINI VALERIO , O'BRIEN MICHAEL ALISTAIR , CARR MARIA GRAZIA , EARLY THERESA RACHEL , GILL ADRIAN LIAM , TREWARTHA GARY , WOOLFORD ALISON JO-ANNE , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
发明人： BERDINI VALERIO , O'BRIEN MICHAEL ALISTAIR , CARR MARIA GRAZIA , EARLY THERESA RACHEL , GILL ADRIAN LIAM , TREWARTHA GARY , WOOLFORD ALISON JO-ANNE , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
IPC分类号： A61P25/28 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/00 , C07D231/14 , C07D231/38 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04 , A61K31/4155 , C07D231/42
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/416 , A61K31/4178 , A61K31/4196 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/541 , A61K45/06 , C04B35/632 , C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D453/02 , C07D471/04
摘要： The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. Formula (0). In formula (0): X is a group R -A-NR - or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, S02, C=O, NR (C=O) or O(C=O) wherein R 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; R 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 (e.g. fluorine), 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 0, S, NH, SO, S02; R is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R is selected from hydrogen and carbocyclic and heterocyclic groups having from 3 to 12 ring members; and R is hydrogen or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy).
摘要翻译：本发明提供了用于预防或治疗疾病状态和病症（例如由细胞周期蛋白依赖性激酶和糖原合酶激酶-3介导的癌症）的式（0）化合物或其盐或互变异构体或N-氧化物或溶剂化物。公式（0）。在式（0）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 g（C = O）或O（C = O），其中R g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（例如氟），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4个碳原子的杂环基团取代的取代基取代的C 1-8烃基 12个环成员，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; R 2是氢; 卤素; C 1-4烷氧基（例如甲氧基）; 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（例如氟），羟基或C 1-4烷氧基（例如甲氧基）取代的C 1-4烃基。

3. 发明申请

WO2006051290A3 COMPOUNDS FOR TREATING PROTEIN-KINASE MEDIATED DISORDERS 审中-公开
标题翻译：用于治疗蛋白激酶介导性疾病的化合物
公开(公告)号：WO2006051290A3
公开(公告)日：2006-09-14
申请号：PCT/GB2005004323
申请日：2005-11-09
申请人： ASTEX THERAPEUTICS LTD , CANCER RES INST ROYAL , CANCER REC TECH LTD , BERDINI VALERIO , BOYLE ROBERT GEORGE , SAXTY GORDON , VERDONK MARINUS LEENDERT , WOODHEAD STEVEN JOHN , WYATT PAUL GRAHAM , SORE HANNAH FIONA , WALKER DAVID WINTER , CALDWELL JOHN , COLLINS IAN
发明人： BERDINI VALERIO , BOYLE ROBERT GEORGE , SAXTY GORDON , VERDONK MARINUS LEENDERT , WOODHEAD STEVEN JOHN , WYATT PAUL GRAHAM , SORE HANNAH FIONA , WALKER DAVID WINTER , CALDWELL JOHN , COLLINS IAN
IPC分类号： A61K31/505 , A61P35/00 , C07D239/88 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/12
CPC分类号： C07D403/12 , A61K31/505 , C07D239/88 , C07D239/91 , C07D239/96 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04
摘要： The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B, wherein the ring Q is a benzene ring; J 2 -J 1 is N=CR 7 or R 1a N-CO; G is OH or NR 5 R 6 ; E is CONR 7 , NR 7 CO, C(R 8 )=C(R 8 ) or (X) m (CR 8 R 8a ) n where X is O, S or NR 7 ; provided that when J 2 -J 1 is R 1a N-CO, E is other than NR 7 CO; m and n are each 0 or 1, where m + n = 1 or 2; A is a bond and R 4 and R 4a are absent, or A is a saturated optionally group having a maximum chain length of 5 atoms extending between E and G, one carbon atom in the linker group A being optionally replaced by O or N.
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，用于治疗或预防由蛋白激酶A和/或蛋白激酶B介导的疾病状态或病症，其中环Q是苯环; N 2是N = CR 7或R 1a N-CO; G是OH或NR 5 R 6; E是CONR 7，NR 7 CO，C（R 8）= C（R 8）或（R 8）其中X是O，S或NR 7（其中X是O，S或NR 7）其中X是O，S或NR 7 ; 条件是当J 2是-J 1，R 1是N-CO时，E不是NR 7 CO ; m和n各自为0或1，其中m + n = 1或2; A是键，R 4和R 4a不存在，或A是在E和G之间延伸的最大链长为5个原子的饱和任选基团，一个碳连接基团A中的原子任选被O或N取代。

4. 发明申请

WO2005011697A3 SULFONAMIDE DERIVATIVES WITH ACTIVITY ON PROTEIN KINASE A AND B 审中-公开
标题翻译：蛋白激酶A和B具有活性的磺酰胺衍生物
公开(公告)号：WO2005011697A3
公开(公告)日：2005-04-21
申请号：PCT/GB2004003196
申请日：2004-07-23
申请人： ASTEX TECHNOLOGY LTD , CANCER REC TECH LTD , CANCER RES INST ROYAL , MCDONALD EDWARD , DE FONSECA TATIANA FARIA , BAVETSIAS VASSILIOS , CALDWELL JOHN , WYATT PAUL GRAHAM , BERDINI VALERIO
发明人： MCDONALD EDWARD , DE FONSECA TATIANA FARIA , BAVETSIAS VASSILIOS , CALDWELL JOHN , WYATT PAUL GRAHAM , BERDINI VALERIO
IPC分类号： A61K31/472 , C07D217/02 , C07D401/12
CPC分类号： C04B35/632 , A61K31/472 , C07D217/02 , C07D401/12
摘要： The invention provides compounds for the prophylaxis or treatment of a disease state or condition mediated by protein kinase A or protein kinase B, the compounds having the formula (I°), or being salts or solvates thereof. In formula (I°), n is 0 or 1; A and E are alkylene 2-3 carbon atoms in length optionally substituted by R and -X-CH(R )(R ); G is hydrogen when n is 0 and, when n is 1, G is hydrogen or -X-CH(R )(R ); R is an aryl or heteroaryl group having 5-12 ring members; R and R are selected from hydrogen, R , R and CH(R )(R ); R , R and R are selected from hydrogen, R and -X-CH(R )(R ); or any one pair or any two non-overlapping pairs selected from R and R ; R and R ; R and R ; R and R ; R and R ; R and R ; and R and R are linked together in a ring and together form an alkylene chain of 1-5 carbon atoms in length which may be optionally substituted by R and -X-CH(R )(R ); or the pair R and R are linked together in a ring and together form an alkylene chain of 2-5 carbon atoms in length which may be optionally substituted by R and -X-CH(R )(R ); and optionally R and R may be linked together in a ring and together form an alkylene chain of 1-6 carbon atoms in length which may be optionally substituted by R and -X-CH(R )(R ); or R and R together with the carbon atom to which they are attached form a cyclic group having 5-12 ring members; X, R , R , R , R , R and R are each as defined in claim 1; and wherein the definitions of, A, E, G, X, n and R to R are subject to the provisos set ou in claim 1.
摘要翻译：本发明提供了用于预防或治疗由蛋白激酶A或蛋白激酶B，具有式（I°）的化合物或其盐或溶剂合物介导的疾病状态或病症的化合物。在式（I°）中，n为0或1; A和E是长度任选被R 11和-X-CH（R 6）（R 7）取代的2-3个碳原子的亚烷基; 当n为0时，G为氢，当n为1时，G为氢或-X-CH（R 6）（R 7）; R 1是具有5-12个环成员的芳基或杂芳基; R 2和R 4选自氢，R 7，R 7和CH（R 6）（R 7）; R 3，R 3a和R 5选自氢，R 11和-X-CH（R 6）（R 7）; 或选自R 2和R 3中的任何一对或任何两个非重叠对; R 3和R 4; R 2和R 5; R 3和R 5; R 4和R 5; R 3和R 8; 并且R 4和R 8以环连接在一起并且一起形成长度为1-5个碳原子的亚烷基链，其可任选地被R 11和-X-CH（R 6）取代，）（R <7>）; 或者R 2和R 4在环中连接在一起并且一起形成长度为2-5个碳原子的亚烷基链，其可以任选地被R 11和-X-CH（R' 6>）（R <7>）; 并且任选地R 3和R 3a可以以环连接在一起并且一起形成长度为1-6个碳原子的亚烷基链，其可任选地被R 11和-X-CH（R' 6>）（R <7>）; 或R 6和R 7与它们所连接的碳原子一起形成具有5-12个环成员的环状基团; X，R 6，R 7，R 8，R 9，R 10和R 11各自如权利要求1所定义; 并且其中A，E，G，X，n和R 1至R 11的定义符合权利要求1所述的限制条件。

5. 发明申请

WO2005002576A3 BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS ROTEIN KINASES INHIBITORS 审中-公开
标题翻译：苯并咪唑衍生物及其作为罗茨金杀伤剂的用途
公开(公告)号：WO2005002576A3
公开(公告)日：2005-06-16
申请号：PCT/GB2004002913
申请日：2004-07-05
申请人： ASTEX TECHNOLOGY LTD , BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
发明人： BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
IPC分类号： A61K31/00 , A61K31/4184 , A61P31/10 , A61P35/00 , C07D403/04
CPC分类号： C07D401/14 , A61K31/00 , A61K31/4184 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention provides a compound of the formula (I) or a salt, N-oxide or solvate thereof. The compounds have activity against cyclin dependent kinases glycogen synthase kinase and Auroa kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物或其溶剂合物。该化合物具有抗细胞周期蛋白依赖性激酶糖原合酶激酶和Auroa激酶的活性。

6. 发明申请

WO2005002576A8 IMIDAZOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASES INHIBITORS 审中-公开
标题翻译：咪唑衍生物及其作为蛋白激酶抑制剂的用途
公开(公告)号：WO2005002576A8
公开(公告)日：2005-09-22
申请号：PCT/GB2004002913
申请日：2004-07-05
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
发明人： BERDINI VALERIO , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM , O'BRIEN MICHAEL ALISTAIR , NAVARRO EVA FIGUEROA
IPC分类号： A61K31/00 , A61K31/4184 , A61P31/10 , A61P35/00 , C07D403/04
CPC分类号： C07D401/14 , A61K31/00 , A61K31/4184 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The invention provides a compound of the formula (I) or a salt, N-oxide or solvate thereof. The compounds have activity against cyclin dependent kinases, glycogen synthase kinase and Auroa kinases.
摘要翻译：本发明提供式（I）化合物或其盐，N-氧化物或其溶剂合物。该化合物具有针对细胞周期蛋白依赖性激酶，糖原合成酶激酶和Auroa激酶的活性。

7. 发明申请

WO2006008545A3 THIAZOLE AND ISOTHIAZOLE DERIVATIVES AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的噻唑和异噻唑衍生物
公开(公告)号：WO2006008545A3
公开(公告)日：2006-03-30
申请号：PCT/GB2005002888
申请日：2005-07-22
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , EARLY THERESA RACHAEL , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
发明人： BERDINI VALERIO , EARLY THERESA RACHAEL , O'BRIEN MICHAEL ALISTAIR , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
IPC分类号： C07D417/12 , A61K31/425 , A61K31/426 , A61K31/427 , C07D275/02 , C07D277/56 , C07D417/14
CPC分类号： C07D275/03 , C07D277/56 , C07D417/12 , C07D417/14
摘要： The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by a cyclin dependent kinase, the compound having the formula (I): (I) and salts, tautomers, N-oxides or solvates thereof; wherein A is a bond, C=O, NR
摘要翻译：本发明提供一种用于预防或治疗由细胞周期蛋白依赖性激酶介导的疾病状态或病症的化合物，具有式（I）：（I）的化合物及其盐，互变异构体，N-氧化物或溶剂合物; 其中A是键，C = O，NR

8. 发明申请

WO2006070195A8 PYRAZOLE COMPOUNDS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：调节CDK，GSK和AURORA KINASES活性的吡咯化合物
公开(公告)号：WO2006070195A8
公开(公告)日：2006-08-24
申请号：PCT/GB2005005097
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LTD , BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
发明人： BERDINI VALERIO , CARR MARIA GRAZIA , GILL ADRIAN LIAM , HOWARD STEVEN , NAVARRO EVA FIGUEROA , TREWARTHA GARY , REES DAVID CHARLES , VINKOVIC MLADEN , WYATT PAUL GRAHAM
IPC分类号： C07D403/04 , A61K31/4184 , A61P35/00 , C07D407/14 , C07D513/04
CPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D413/14 , C07D487/04 , C07D513/04
摘要： The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R', E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.
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M选自D1和D2组：R'，E，A和X如上所定义在权利要求中。还提供了含有化合物的药物组合物，制备该化合物的方法以及该化合物在预防或治疗由CDK激酶，GSK-3激酶或极光激酶介导的疾病状态中的用途。

9. 发明申请

WO2007129066A8 4- (2,6-DICHLORO-BENZOYLAMINO) -1H-PYRAZOLE-3-CARBOXYLIC ACID (1-METHANESULPHONYL-PIPERIDIN-4-YL) -AMIDE FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的4-（2,6-二氯苯甲酰氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基）酰胺
公开(公告)号：WO2007129066A8
公开(公告)日：2008-02-21
申请号：PCT/GB2007001655
申请日：2007-05-04
申请人： ASTEX THERAPEUTICS LTD , TREWARTHA GARY , NAVARRO EVA FIGUEROA , REES DAVID CHARLES , VINKOVIC MLADEN , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
发明人： TREWARTHA GARY , NAVARRO EVA FIGUEROA , REES DAVID CHARLES , VINKOVIC MLADEN , WOODHEAD ANDREW JAMES , WYATT PAUL GRAHAM
IPC分类号： C07D401/12 , A61K31/4155 , A61P35/00
CPC分类号： C07D401/12
摘要： The invention provides the compound of formula (I) 4-(2,6-dichloro-benzoylamino)-1H-pyrazole- 3-carboxylic acid (l-methanesulphonyl-piperidin-4-yl)-amide in a substantially crystalline form, therapeutic uses thereof and pharmaceutical compositions containing the crystalline compound. The invention also provides novel pharmaceutical formulations containing 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide and novel processes for preparing the compound.
摘要翻译：本发明提供基本上为结晶形式的式（I）4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基） - 酰胺的化合物，治疗其用途和含有结晶化合物的药物组合物。本发明还提供了含有4-（2,6-二氯 - 苯甲酰氨基）-1H-吡唑-3-羧酸（1-甲磺酰基 - 哌啶-4-基） - 酰胺的新型药物制剂及其制备方法。

10. 发明申请

WO2006077426A3 4- (2, 6-DICHLOROBENZOYLAMINO) -lH-PYRAZOLE-3 -CARBOXYLIC ACID PIPERIDIN- 4 -YLAMID ACID ADDITION SALTS AS KINASE INHIBITORS 审中-公开
标题翻译： 4-（2,6-二氯苯甲酰氨基）-1H-吡唑-3-羧酸哌啶-4-基氨基酸添加剂作为激酶抑制剂
公开(公告)号：WO2006077426A3
公开(公告)日：2006-09-28
申请号：PCT/GB2006000207
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LTD , WYATT PAUL GRAHAM , REES DAVID CHARLES , VINKOVIC MLADEN , TREWARTHA GARY
发明人： WYATT PAUL GRAHAM , REES DAVID CHARLES , VINKOVIC MLADEN , TREWARTHA GARY
IPC分类号： C07D401/12 , A61K31/4155 , A61K31/454 , A61P35/00 , A61P35/02
CPC分类号： C07D231/40 , C07D401/12
摘要： The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-lH- pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-lH- pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4- (2,6-dichloro-benzoylamino)-lH-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates.
摘要翻译：本发明提供4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸哌啶-4-基酰胺及其晶体的酸加成盐，该盐与选自甲磺酸和乙酸的酸形成酸及其混合物。还提供4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸哌啶-4-基酰胺的盐的新用途，制备4-（2,6-二氯 - 苯甲酰基氨基）-1H-吡唑-3-羧酸哌啶-4-基酰胺及其盐和新的化学中间体。

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