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1. 发明申请

WO2003049735A1 CERTAIN GLYCINE DERIVATIVES AS FACTOR XA INHIBITORS FOR USE IN THE TREATMENT OF THROMBOTIC DISORDERS 审中-公开
标题翻译：某些谷氨酸衍生物作为用于治疗血栓性疾病的因子XA抑制剂
公开(公告)号：WO2003049735A1
公开(公告)日：2003-06-19
申请号：PCT/US2002/036150
申请日：2002-12-09
申请人： ELI LILLY AND COMPANY , WILEY, Michael, Robert , SALL, Daniel, Jon , MURRAY, Christopher, William , YOUNG, Stephen, Clinton , BASTIAN, Jolie, Anne
发明人： WILEY, Michael, Robert , SALL, Daniel, Jon , MURRAY, Christopher, William , YOUNG, Stephen, Clinton , BASTIAN, Jolie, Anne
IPC分类号： A61K31/445
CPC分类号： C07D401/14 , C07D211/26 , C07D211/58 , C07D401/04 , C07D401/12 , C07D409/12 , C07D409/14
摘要： Compounds of formula (I) in which R, R 1 , R 2 , n and X 1 have the meanings given in the specification are factor Xa inhibitors useful in the treatment of thrombotic disorders.
摘要翻译：其中R，R 1，R 2，R 2，X和X 1具有本说明书中给出的含义的式（I）化合物是因子可用于治疗血栓形成障碍的Xa抑制剂。

2. 发明公开

EP1192132A2 SERINE PROTEASE INHIBITORS 有权
标题翻译：抑制素血清蛋白
公开(公告)号：EP1192132A2
公开(公告)日：2002-04-03
申请号：EP00938916.4
申请日：2000-06-13
申请人： ELI LILLY AND COMPANY
发明人： LIEBESCHUETZ, John, Walter , LYONS, Amanda, Jane , MURRAY, Christopher, William , RIMMER, Andrew, David , YOUNG, Stephen, Clinton , CAMP, Nicholas, Paul , JONES, Stuart, Donald , MORGAN, Phillip, John , RICHARDS, Simon, James , WYLIE, William, Alexander , MASTERS, John, Joseph , WILEY, Michael, Robert
IPC分类号： C07D211/00
CPC分类号： C07D401/14 , C07C237/36 , C07C255/60 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07C2602/42 , C07D209/08 , C07D209/30 , C07D209/34 , C07D209/42 , C07D211/26 , C07D211/34 , C07D211/46 , C07D211/60 , C07D213/53 , C07D213/74 , C07D213/82 , C07D215/38 , C07D217/04 , C07D217/06 , C07D231/56 , C07D235/06 , C07D241/24 , C07D277/28 , C07D277/46 , C07D277/64 , C07D277/82 , C07D295/135 , C07D295/185 , C07D317/68 , C07D333/38 , C07D333/68 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/14 , C07D413/14 , C07D417/06 , C07D487/04
摘要： Compounds of formula (I) where R2, each X, L, Y, Cy, Lp, D and n are as defined in the specification, are serine protease inhibitors useful as antithrombotic agents.
摘要翻译：其中R2，X，L，Y，Cy，Lp，D和n如说明书中所定义的式（I）化合物是用作抗血栓形成剂的丝氨酸蛋白酶抑制剂。

3. 发明授权

EP1455787B1 CERTAIN GLYCINE DERIVATIVES AS FACTOR XA INHIBITORS FOR USE IN THE TREATMENT OF THROMBOTIC DISORDERS 有权
标题翻译：某些甘胺酸衍生物Xa因子抑制剂FOR USE IN治疗血栓形成
公开(公告)号：EP1455787B1
公开(公告)日：2005-06-22
申请号：EP02791222.9
申请日：2002-12-09
申请人： ELI LILLY AND COMPANY
发明人： WILEY, Michael, Robert , SALL, Daniel, Jon , MURRAY, Christopher, William , YOUNG, Stephen, Clinton , BASTIAN, Jolie, Anne
IPC分类号： A61K31/445
CPC分类号： C07D401/14 , C07D211/26 , C07D211/58 , C07D401/04 , C07D401/12 , C07D409/12 , C07D409/14

5. 发明公开

EP1455787A1 CERTAIN GLYCINE DERIVATIVES AS FACTOR XA INHIBITORS FOR USE IN THE TREATMENT OF THROMBOTIC DISORDERS 有权
标题翻译：某些甘胺酸衍生物Xa因子抑制剂FOR USE IN治疗血栓形成
公开(公告)号：EP1455787A1
公开(公告)日：2004-09-15
申请号：EP02791222.9
申请日：2002-12-09
申请人： ELI LILLY AND COMPANY
发明人： WILEY, Michael, Robert , SALL, Daniel, Jon , MURRAY, Christopher, William , YOUNG, Stephen, Clinton , BASTIAN, Jolie, Anne
IPC分类号： A61K31/445
CPC分类号： C07D401/14 , C07D211/26 , C07D211/58 , C07D401/04 , C07D401/12 , C07D409/12 , C07D409/14
摘要： Compounds of formula (I) in which R, R1, R2, n and X1 have the meanings given in the specification are factor Xa inhibitors useful in the treatment of thrombotic disorders.

6. 发明申请

WO2006065204A1 SUBSTITUTED AMINOPYRIDINES AND USES THEREOF 审中-公开
标题翻译：取代的氨基吡啶及其用途
公开(公告)号：WO2006065204A1
公开(公告)日：2006-06-22
申请号：PCT/SE2005/001891
申请日：2005-12-12
申请人： ASTRAZENECA AB , ASTEX THERAPEUTICS , ALBERT, Jeffrey, Scott , CALLAGHAN, Owen , CAMPBELL, James , CARR, Robin, Arthur, Ellis , CHESSARI, Gianni , COWAN, Suzanna , CONGREVE, Miles, Stuart , EDWARDS, Phil , FREDERICKSON, Martyn , MURRAY, Christopher, William , PATEL, Sahil
发明人： ALBERT, Jeffrey, Scott , CALLAGHAN, Owen , CAMPBELL, James , CARR, Robin, Arthur, Ellis , CHESSARI, Gianni , COWAN, Suzanna , CONGREVE, Miles, Stuart , EDWARDS, Phil , FREDERICKSON, Martyn , MURRAY, Christopher, William , PATEL, Sahil
IPC分类号： C07D213/73 , A61K31/44 , A61P25/16 , A61P25/28
CPC分类号： C07D213/73 , C07D213/74 , C07D213/81 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/10 , C07D409/14 , C07D413/12
摘要： This invention relates to novel compounds having the structural formula (I) and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有结构式（I）的新化合物及其药学上可接受的盐，组合物和使用方法。这些新化合物提供认知障碍，阿尔茨海默病，神经变性和痴呆症的治疗或预防。

7. 发明申请

WO2006041405A1 SUBSTITUTED AMINO-PYRIMIDONES AND USES THEREOF 审中-公开
标题翻译：取代的氨基吡啶酮及其用途
公开(公告)号：WO2006041405A1
公开(公告)日：2006-04-20
申请号：PCT/SE2005/001534
申请日：2005-10-14
申请人： ASTRAZENECA AB , ASTEX THERAPEUTICS , ALBERT, Jeffrey, Scott , ANDISIK, Don , ARNOLD, Jim , BROWN, Dean , CALLAGHAN, Owen , CAMPBELL, James , CARR, Robin, Arthur, Ellis , CHESSARI, Gianni , CONGREVE, Miles, Stuart , EDWARDS, Phil , EMPFIELD, James, R. , FREDERICKSON, Martyn , KOETHER, Gerard, M. , KRUMRINE, Jennifer , MAUGER, Russ , MURRAY, Christopher, William , PATEL, Sahil , SYLVESTER, Mark , THRONER, Scott
发明人： ALBERT, Jeffrey, Scott , ANDISIK, Don , ARNOLD, Jim , BROWN, Dean , CALLAGHAN, Owen , CAMPBELL, James , CARR, Robin, Arthur, Ellis , CHESSARI, Gianni , CONGREVE, Miles, Stuart , EDWARDS, Phil , EMPFIELD, James, R. , FREDERICKSON, Martyn , KOETHER, Gerard, M. , KRUMRINE, Jennifer , MAUGER, Russ , MURRAY, Christopher, William , PATEL, Sahil , SYLVESTER, Mark , THRONER, Scott
IPC分类号： C07D239/47 , A61K31/513 , A61P25/28 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10
CPC分类号： C07D239/47 , C07D401/10 , C07D403/06 , C07D403/10 , C07D405/10 , C07D405/14 , C07D409/10
摘要： This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia, Ib), and their pharmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Aß related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.
摘要翻译：本发明涉及具有结构式Ia或式Ib的新化合物：（Ia，Ib）及其药学上可接受的盐，互变异构体或体内可水解的前体，组合物及其使用方法。这些新化合物提供了Aß相关病理学的治疗或预防，例如认知障碍，阿尔茨海默病，神经退行性疾病和痴呆。

8. 发明申请

WO2009047506A1 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：WO2009047506A1
公开(公告)日：2009-04-16
申请号：PCT/GB2008/003418
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 , CARR, Maria, Grazia
发明人： SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher, William , GRIFFITHS-JONES, Charlotte, Mary , VICKERSTAFFE, Emma , BESONG, Gilbert, Ebai , CARR, Maria, Grazia
IPC分类号： C07D471/04 , C07D487/04 , A61P35/00 , A61K31/437
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R 1 , A, 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，A，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所述化合物在疾病的治疗，例如癌症。

9. 发明申请

WO2008078091A1 BICYCLIC HETEROCYCLIC COMPOUNDS AS FGFR INHIBITORS 审中-公开
标题翻译：作为FGFR抑制剂的双相杂环化合物
公开(公告)号：WO2008078091A1
公开(公告)日：2008-07-03
申请号：PCT/GB2007/004934
申请日：2007-12-21
申请人： ASTEX THERAPEUTICS LIMITED , BERDINI, Valerio , BESONG, Gilbert, Ebai , CALLAGHAN, Owen , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , GILL, Adrian, Liam , GRIFFITHS-JONES, Charlotte, Mary , MADIN, Andrew , MURRAY, Christopher, William , NIJJAR, Rajdeep, Kaur , O'BRIEN, Michael, Alistair , PIKE, Andrew , SAXTY, Gordon , TAYLOR, Richard, David , VICKERSTAFFE, Emma
发明人： BERDINI, Valerio , BESONG, Gilbert, Ebai , CALLAGHAN, Owen , CARR, Maria, Grazia , CONGREVE, Miles, Stuart , GILL, Adrian, Liam , GRIFFITHS-JONES, Charlotte, Mary , MADIN, Andrew , MURRAY, Christopher, William , NIJJAR, Rajdeep, Kaur , O'BRIEN, Michael, Alistair , PIKE, Andrew , SAXTY, Gordon , TAYLOR, Richard, David , VICKERSTAFFE, Emma
IPC分类号： C07D471/04 , C07D487/04 , A61K31/437 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , A61K31/437 , C07D471/04
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。

10. 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。

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