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1. 发明申请

WO2002068377A1 OMEGA-AMINOALKYLAMIDES OF R-2-ARYL-PROPIONIC ACIDS AS INHIBITORS OF THE CHEMOTAXIS OF POLYMORPHONUCLEATE AND MONONUCLEATE CELLS 审中-公开
标题翻译：作为聚马来酸酐和单核细胞化合物的化学抑制剂的R-2-ARYL-PROPIONIC的OMEGA-氨基甲酰胺
公开(公告)号：WO2002068377A1
公开(公告)日：2002-09-06
申请号：PCT/EP2002/001974
申请日：2002-02-25
申请人： DOMPÉ S.P.A. , ALLEGRETTI, Marcello , BERTINI, Riccardo , BERDINI, Valerio , BIZZARRI, Cinzia , CESTA, Maria, Candida , DI CIOCCIO, Vito , CASELLI, Gianfranco , COLOTTA, Francesco , GANDOLFI, Carmelo
发明人： ALLEGRETTI, Marcello , BERTINI, Riccardo , BERDINI, Valerio , BIZZARRI, Cinzia , CESTA, Maria, Candida , DI CIOCCIO, Vito , CASELLI, Gianfranco , COLOTTA, Francesco , GANDOLFI, Carmelo
IPC分类号： C07C233/40
CPC分类号： C07C233/51 , A61K31/165 , A61K31/198 , A61K31/445 , A61K31/4453 , A61K31/5375 , C07B2200/07 , C07C231/02 , C07C231/16 , C07C233/40 , C07C233/44 , C07C235/34 , C07C235/70 , C07C235/78 , C07C237/20 , C07C237/22 , C07C279/12 , C07C281/16 , C07D211/04 , C07D211/58 , C07D233/24 , C07D233/46 , C07D295/13 , C07D451/04
摘要： (R) -2-Arylpropionamide compounds of formula (I) are described. The process for their preparation and pharmaceutical preparations thereof are also described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbate recruitment of polymorphonuclear leukocytes (Leukocytes PMN) and of monocytes at the inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use in the inhibition of he chemataxis of neutrophils and monocites induced by the C5a fraction of the complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of nutrophils and monocytes and the IL-8-induced chemotaxis of PMN leukocytes. The compounds of the invention are used in the treatment of psoriasis, ulcerative cholitis, glomerular nephritis, acute respiratory insufficiency, idiopathic fibrosis, rheumatoid arthritis and in the prevention and the treatment of injury caused by ischemia and reperfusion.
摘要翻译：描述了式（I）的（R）-2-芳基丙酰胺化合物。还描述了其制备方法及其制备药物。本发明的2-芳基丙酰胺可用于预防和治疗由于炎症部位多形核白细胞（白细胞PMN）和单核细胞的加剧性募集引起的组织损伤。特别地，本发明涉及式（I）的2-芳基丙酸的ω-氨基烷基酰胺的R对映异构体，用于抑制由补体的C5a部分诱导的嗜中性粒细胞和单核细胞的化学反应其生物活性与7-TD受体激活相关的趋化蛋白。选择的式（I）化合物是C5a诱导的营养物质和单核细胞的趋化性和IL-8诱导的PMN白细胞趋化性的双重抑制剂。本发明的化合物用于治疗牛皮癣，溃疡性胆囊炎，肾小球性肾炎，急性呼吸功能不全，特发性纤维化，类风湿性关节炎，以及预防和治疗由缺血和再灌注引起的损伤。

2. 发明申请

WO2010119284A1 BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE 审中-公开
标题翻译：作为用于治疗用途的FGFR激酶抑制剂的双相间苯二酚衍生物
公开(公告)号：WO2010119284A1
公开(公告)日：2010-10-21
申请号：PCT/GB2010/050617
申请日：2010-04-15
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
发明人： SAXTY, Gordon , BERDINI, Valerio , FREYNE, Eddy Jean Edgard , PAPANIKOS, Alexandra , BENDERITTER, Pascal , EMBRECHTS, Werner Constant Johan , WROBLOWSKI, Berthold , AKKARI, Rhalid
IPC分类号： C07D471/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及式（I）的新的双环杂环基衍生物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途，例如，癌症。

3. 发明申请

WO2006077419A1 PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDK' S AND GSK' S 审中-公开
标题翻译：用于抑制CDK和GSK'S的吡唑衍生物
公开(公告)号：WO2006077419A1
公开(公告)日：2006-07-27
申请号：PCT/GB2006/000196
申请日：2006-01-20
申请人： ASTEX THERAPEUTICS LIMITED , WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
发明人： WYATT, Paul, Graham , BERDINI, Valerio , GILL, Adrian, Liam , TREWARTHA, Gary , WOODHEAD, Andrew, James , NAVARRO, Eva, Figueroa , O'BRIEN, Michael, Alistair , PHILLIPS, Theresa, Rachel
IPC分类号： C07D453/02 , C07D401/14 , C07D401/12 , A61K31/44 , A61K31/4545 , A61K31/506 , A61P35/00 , A01N43/56
CPC分类号： C07D231/14 , C07D231/40 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D417/14
摘要： The invention provides compounds of the formula (I) or a salt, tautomer, solvate or N-oxides thereof; wherein: R 1 is selected from (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents are fluorine, chlorine, methyl or methoxy; and (d) a group R 0 wherein R 0 is a 3-12 membered carbocyclic or heterocyclic group; or optionally substituted C 1-8 hydrocarbyl; R 2a and R 2b are each hydrogen or methyl; and R 3 is as defined in the claims. The compounds have activity as inhibitors of Cyclin Dependent Kinases (CDK) and Glycogen Synthase Kinases (GSK) kinases and are useful in the treatment or prophylaxis of disease states or conditions mediated by the kinases.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，溶剂合物或N-氧化物; 其中：R 1选自（a）2,6-二氯苯基; （b）2,6-二氟苯基; （c）2,3,6-三取代的苯基，其中取代基是氟，氯，甲基或甲氧基; 和（d）R 0为0的基团，其中R 0为3-12元碳环或杂环基; 或任选取代的C 1-8烃基; R 2a和R 2b各自为氢或甲基; R 3和R 3如权利要求中所定义。该化合物具有作为细胞周期蛋白依赖性激酶（CDK）和糖原合酶激酶（GSK）激酶抑制剂的活性，可用于治疗或预防由激酶介导的疾病状态或病症。

4. 发明申请

WO2006070202A1 PYRAZOLE DERIVATIVES HAVING KINASE MODULATING ACTIVITY 审中-公开
标题翻译：具有激酶调节活性的吡唑衍生物
公开(公告)号：WO2006070202A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005109
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , NAVARRO, Eva, Figueroa , WYATT, Paul, Graham
IPC分类号： C07D413/14 , C07D403/04 , C07D407/14 , A01N43/56 , A61K31/4178 , A61K31/422 , A61P35/00
CPC分类号： C07D403/04 , C07D405/14 , C07D413/14
摘要： The invention provides a compound of the formula (I): or a salt, tautomer, N-oxide or solvate thereof; wherein A is selected from a bond, CH 2 and CH(CN); R l is selected from: (i) a cycloalkyl group of 3 to 6 ring members optionally substituted by one or more substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino and cyano; (ii) a phenyl group optionally substituted by up to three substituents selected from methyl, ethyl, fluorine, chlorine, methoxy, ethoxy and methylsulphonyl, but excluding 2,6-difluorophenyl, 2-fluoro-6-methoxy and 5-chloro-2-methoxyphenyl; (iii) a monocyclic heterocyclic group selected from furyl and isoxazolyl, the heterocyclic group being optionally substituted by one or two groups selected from methyl, ethyl, and a group CH 2 R 2 where R 2 is a five or six membered saturated heterocyclic ring containing one or two heteroatom ring members selected from O and N, the heterocyclic ring being optionally substituted by one or two methyl groups; and (iv) a bicyclic heterocyclic group selected from 2,3-dihydrobenzofuranyl and benzo[c]isoxazolyl, the bicyclic group being optionally substituted by one or two substituents selected from methyl, ethyl, hydroxy, methoxy, ethoxy, fluorine, amino, cyano and chlorine, the bicyclic heterocyclic group being other than a 2,2-dimethyl-2,3-dihydrobenzofuran-7-yl group.
摘要翻译：本发明提供式（I）化合物或其盐，互变异构体，N-氧化物或其溶剂合物; 其中A选自键，CH 2和CH（CN）; R 1选自：（i）任选被一个或多个选自甲基，乙基，羟基，甲氧基，乙氧基，氟，氨基和氰基的取代基取代的3至6个环成员的环烷基; （ii）任选被至多三个选自甲基，乙基，氟，氯，甲氧基，乙氧基和甲基磺酰基的取代基取代的苯基，但不包括2,6-二氟苯基，2-氟-6-甲氧基和5-氯-2 - 甲氧基; （iii）选自呋喃基和异恶唑基的单环杂环基，杂环基团任选被一个或两个选自甲基，乙基和CH 2 R 2 R 2 O 2基团取代其中R 2是含有一个或两个选自O和N的杂原子环成员的五或六元饱和杂环，杂环任选被一个或两个甲基取代; 和（iv）选自2,3-二氢苯并呋喃基和苯并[c]异恶唑基的双环杂环基，双环基团任选被一个或两个选自甲基，乙基，羟基，甲氧基，乙氧基，氟，氨基，氰基和氯，双环杂环基不同于2,2-二甲基-2,3-二氢苯并呋喃-7-基。

5. 发明申请

WO2006051290A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2006051290A2
公开(公告)日：2006-05-18
申请号：PCT/GB2005/004323
申请日：2005-11-09
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 , 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 , C07D401/12 , C07D401/04 , C07D401/06 , 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 substituted C 1-7 hydrocarbon linker 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; R 1 , R la , R 2 , and R 3 are each H; halogen; C 1-6 hydrocarbyl optionally substituted by halogen, OH or C 1-2 alkoxy; CN; CONHR 8 ; NH 2 ; NHCOR 10 or NHCONHR 10 ; R 4 is H or C 1-4 alkyl; R 4a is H, C 1-4 alkyl or a group R 9 ; R 5 and R 6 are each selected from H, R 9 and C 1-4 hydrocarbyl optionally substituted by halogen, C 1-2 alkoxy or R 9 ;or NR 5 R 6 forms a saturated 4-7 membered monocyclic heterocyclic group; R 7 is H or C 1-4 alkyl; R 8 and R 8a each H or saturated C 1-4 hydrocarbyl optionally substituted by fluorine; R 9 is a monocyclic or bicyclic carbocyclic or heterocyclic group containing up to 3 ring heteroatoms selected from N, O and S; or R 4 , R 4a and A together form a saturated monocyclic 4-7 membered heterocycle; or NR 5 R 6 , R 4 and A form a saturated 4-7 membered monocyclic heterocycle; or R 4 , together with R 7 or R 8 and A and E form a 4-7 membered saturated monocyclic heterocycle; or NR 5 R 6 and R 7 or R 8 together with A and E form a 4-7 membered saturated monocyclic heterocycle; and R 10 is optionally substituted phenyl or benzyl.
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是饱和的任选取代的C 1-7烃连接基团，其具有在E和G之间延伸的5个原子的最大链长度，连接基团A中的一个碳原子任选地被O或N取代; R 1，R 2，R 2，R 3和R 3各自为H; 卤素; 任选被卤素，OH或C 1-12烷氧基取代的C 1-6烷基; CN; CONHR ^{8 ; NH _{2 ; NHCOR 10或NHCONHR 10; R 4是H或C 1-4烷基; R 4a是H，C 1-4烷基或基团R 9; R 5和R 6各自选自H，R 9和C 1-4烃基，任选被卤素，C 1-2烷氧基或R 9或NR 5 R 6形成饱和的4-7 元环杂环基; R 7是H或C 1-4烷基; 每个H或任选被氟取代的饱和C 1-4烃基的R 8和R 8 8a; R 9是含有至多3个选自N，O和S的环杂原子的单环或双环碳环或杂环基; 或R 4，R 4a和A一起形成饱和单环4-7元杂环; 或NR 5 R 6，R 4和A形成饱和的4-7元单环杂环; 或R 4，...，以及R 7或R 8，A和E形成4-7元饱和单环杂环; 或NR 5 R 6和R 7或R 8与A和E一起形成4-7元环饱和单环杂环; R 10是任选取代的苯基或苄基。}}

6. 发明申请

WO2009150240A1 IMIDAZOPYRIDINE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSINE KINASES 审中-公开
标题翻译：作为受体酪氨酸激酶抑制剂的咪唑吡啶衍生物
公开(公告)号：WO2009150240A1
公开(公告)日：2009-12-17
申请号：PCT/EP2009/057318
申请日：2009-06-12
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , FREDERICKSON, Martyn , GRIFFITHS-JONES, Charlotte, Mary , HAMLETT, Christopher, Charles, Frederick , MADIN, Andrew , MURRAY, Christopher, William , BENNING, Rajdeep Kaur , SAXTY, Gordon , VICKERSTAFFE, Emma , WOODHEAD, Andrew, James , WOODHEAD, Steven, John , FREYNE, Eddy, Jean, Edgard , GOVAERTS, Tom, Cornelis, Hortense , ANGIBAUD, Patrick, René , ASTEX THERAPEUTICS LIMITED
发明人： BERDINI, Valerio , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , FREDERICKSON, Martyn , GRIFFITHS-JONES, Charlotte, Mary , HAMLETT, Christopher, Charles, Frederick , MADIN, Andrew , MURRAY, Christopher, William , BENNING, Rajdeep Kaur , SAXTY, Gordon , VICKERSTAFFE, Emma , WOODHEAD, Andrew, James , WOODHEAD, Steven, John , FREYNE, Eddy, Jean, Edgard , GOVAERTS, Tom, Cornelis, Hortense , ANGIBAUD, Patrick, René
IPC分类号： C07D471/04 , C07D513/04 , A61P35/00 , A61K31/437 , A61K31/506 , A61K31/501 , A61K31/53 , A61K31/444 , A61K31/497 , A61K31/496 , A61K31/4545
CPC分类号： C07D471/04 , C07D513/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及新的双环杂环衍生物化合物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途。癌症。

7. 发明申请

WO2009047522A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白酪氨酸激酶抑制剂的双相杂环化合物
公开(公告)号：WO2009047522A1
公开(公告)日：2009-04-16
申请号：PCT/GB2008/003439
申请日：2008-10-10
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher, William , GRIFFITHS-JONES, Charlotte, Mary , VICKERSTAFFE, Emma , BESONG, Gilbert, Ebai
发明人： SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher, William , GRIFFITHS-JONES, Charlotte, Mary , VICKERSTAFFE, Emma , BESONG, Gilbert, Ebai
IPC分类号： C07D471/04 , C07D487/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R 1 , q, A, B, X 1 , X 2 , X 3 , X 4 , X 5 and R 2 are as defined herein, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及式（I）的新的双环杂环衍生物化合物：其中R1，q，A，B，X1，X2，X3，X4，X5和R2如本文所定义，包含所述化合物的药物组合物和使用的所述化合物治疗疾病，例如癌症。

8. 发明申请

WO2006070198A1 PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES 审中-公开
标题翻译：用于调节CDK，GSK和AURORA KINASES活性的吡唑衍生物
公开(公告)号：WO2006070198A1
公开(公告)日：2006-07-06
申请号：PCT/GB2005/005102
申请日：2005-12-30
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , O'BRIEN, Michael, Alistair , CARR, Maria, Grazia , DAVIES, Nicholas, Gareth, Morse , GILL, Adrian, Liam , NAVARRO, Eva, Figueroa , HOWARD, Steven , TREWARTHA, Gary , WOODHEAD, Andrew, James , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D417/04 , C07D413/04 , C07D471/04 , A61K31/4155 , A61K31/422 , A61K31/427 , A61P35/00
CPC分类号： C07D407/14 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/14 , C07D413/04 , C07D417/04 , C07D471/04
摘要： The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R 1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or -Y-(B) n -; B is C=O, NR g (C=O) or O(C=O) wherein R g is hydrogen or C 1-4 hydrocarbyl optionally substituted by hydroxy or C 1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; 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 optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C 1-8 hydrocarbyl group; with the proviso that R 1 is not formula (II): where X, R 3’ and R 4’ are defined in the claims.
摘要翻译：本发明提供式（I）化合物：用于医药：或其盐或互变异构体或N-氧化物或溶剂合物; 其中R 1是具有3至12个环成员的任选取代的杂环基，条件是连接到吡唑的环状基团含有至少一个选自N，O或S的杂原子; A是键或-Y-（B）n - B是C = O，NR（C = O）或O（C = O），其中R g是氢或C 1-4 >任选被羟基或C 1-4烷氧基取代的烃基; n为0或1; Y是长度为1,2或3个碳原子的键或亚烷基链; 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个环成员或任选取代的C 1-8烃基的任选取代的碳环和杂环基; 条件是R 1不是式（II）：其中X，R 3'和R 4'在权利要求中限定。

9. 发明申请

WO2004014922A1 3-(CARBONYL) 1H-INDAZOLE COMPOUNDS AS CYCLIN DEPENDENT KINASES (CDK) INHIBITORS 审中-公开
标题翻译：作为循环激酶（CDK）抑制剂的3-（羰基）1H-吲唑化合物
公开(公告)号：WO2004014922A1
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003474
申请日：2003-08-08
申请人： ASTEX TECHNOLOGY LIMITED , BERDINI, Valerio , CARR, Maria , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
发明人： BERDINI, Valerio , CARR, Maria , SAXTY, Gordon , WOOLFORD, Alison, Jo-Anne , WYATT, Paul, Graham
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： The invention provides a compound of the formula (I): wherein E is O, S, or NH; G is selected from hydrogen; carbocyclic and heterocyclic groups having from 3 to 12 ring members; and acyclic C 1-8 hydrocarbyl groups optionally substituted; provided that E-G is not OH or SH and further provided that E-G does not contain the group O-O; two adjacent moieties selected from R 3 , R 4 , R 5 and R 6 , together with the carbon atoms to which they are attached, form a fused heterocyclic group having from 5 to 7 ring members and 1, 2 or 3 ring heteroatoms selected from N, O and S; and the other two moieties selected from R 3 , R 4 , R 5 and R 6. are the same or different and are each as defined in the description. The Invention also provides compounds of the formula (I) for use as inhibitors of cyclin dependent kinases and for use in the treatment of disease states and conditions mediated by cyclin dependent kinases.
摘要翻译：本发明提供式（I）的化合物：其中E是O，S或NH; G选自氢; 具有3至12个环成员的碳环和杂环基; 和任选取代的非环状C 1-8烃基; 条件是E-G不是OH或SH，并且进一步规定E-G不含O-O基团; 选自R 3，R 4，R 5和R 6的两个相邻部分与它们所连接的碳原子一起形成具有5至7个环成员的稠合杂环基和1 ，2或3个选自N，O和S的环杂原子; 并且选自R 3，R 4，R 5和R 6的其它两个部分相同或不同，并且各自如描述中所定义。本发明还提供用作细胞周期蛋白依赖性激酶抑制剂的式（I）化合物，并用于治疗由细胞周期蛋白依赖性激酶介导的疾病状态和状况。

10. 发明申请

WO2012073017A1 SUBSTITUTED BENZOPYRAZIN DERIVATIVES AS FGFR KINASE INHIBITORS FOR THE TREATMENT OF CANCER DISEASES 审中-公开
标题翻译：作为FGFR激酶抑制剂治疗癌症疾病的替代苯并噻嗪衍生物
公开(公告)号：WO2012073017A1
公开(公告)日：2012-06-07
申请号：PCT/GB2011/052356
申请日：2011-11-29
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , WOODHEAD, Steven John , LIGNY, Yannick Aimé Eddy , ANGIBAUD, Patrick René
发明人： SAXTY, Gordon , MURRAY, Christopher William , BERDINI, Valerio , BESONG, Gilbert Ebai , HAMLETT, Christopher Charles Frederick , WOODHEAD, Steven John , LIGNY, Yannick Aimé Eddy , ANGIBAUD, Patrick René
IPC分类号： C07D403/04 , A61K31/502 , A61P35/00
CPC分类号： C07D403/04 , C07D401/14 , C07D403/14
摘要： The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及新的喹喔啉衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法和所述化合物在治疗疾病中的用途。癌症。

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