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1.发明授权IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 有权咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂
公开(公告)号：EP2424843B1
公开(公告)日：2014-03-26
申请号：EP10719772.5
申请日：2010-04-30
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas , LU, Yipin
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
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2.发明公开IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 有权咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂
公开(公告)号：EP2424843A1
公开(公告)日：2012-03-07
申请号：EP10719772.5
申请日：2010-04-30
发明人： HOWARD, Steven , MORTENSON, Paul Neil , HISCOCK, Steven Douglas , WOOLFORD, Alison Jo-Anne , WOODHEAD, Andrew James , CHESSARI, Gianni , O'REILLY, Marc , CONGREVE, Miles Stuart , DAGOSTIN, Claudio , CHO, Young Shin , YANG, Fan , CHEN, Christine Hiu-Tung , BRAIN, Christopher Thomas , LAGU, Bharat , WANG, Yaping , KIM, Sunkyu , GRIALDES, John , LUZZIO, Michael Joseph , PEREZ, Lawrence Blas , LU, Yipin
IPC分类号： C07D233/22 , C07D235/12 , C07D401/06 , C07D401/10 , C07D401/14 , C07D409/10 , C07D409/14 , C07D413/14 , C07D417/10 , A61K31/4164 , A61K31/4178 , A61P35/00
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N
+ -O
- or CR
3 ; Y is N, N
+ -O
- or CR
3a ; R
1 and R
2 are independently selected from hydrogen and various substituents as defined in the claims; or R
1 and R
2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R
3 is selected from hydrogen and various substituents; and R
3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of
inter alia proliferative diseases such as cancers.-
3.发明公开
公开(公告)号：EP1979324A2
公开(公告)日：2008-10-15
申请号：EP06813032.7
申请日：2006-11-20
发明人： BERG, Stefan , BURROWS, Jeremy , CHESSARI, Gianni , CONGREVE, Miles, Stuart , HEDSTRÖM, Johan , HELLBERG, Sven , HÖGDIN, Katharina , KIHLSTRÖM, Jacob , KOLMODIN, Karin , LINDSTRÖM, Johan , MURRAY, Christopher , PATEL, Sahil
IPC分类号： C07D233/88 , A61K31/4168 , A61K31/4174 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/4725 , A61K31/497 , A61K31/506 , A61K31/538 , A61P25/16 , A61P25/28 , C07D233/86 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/10
CPC分类号： C07D233/88 , C07C25/22 , C07C25/24 , C07C39/373 , C07C43/1747 , C07C43/23 , C07C47/575 , C07C49/792 , C07C49/813 , C07C49/83 , C07C49/84 , C07D209/08 , C07D217/06 , C07D233/86 , C07D265/36 , C07D307/79 , C07D339/08 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D413/10 , C07D417/04 , C07F7/1856
摘要： This invention relates to novel compounds having the structural formula I below: 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.
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公开(公告)号：EP3868747A1
公开(公告)日：2021-08-25
申请号：EP20214100.8
申请日：2012-04-20
发明人： WOOLFORD, Alison Jo-Anne , HOWARD, Steven , BUCK, Ildiko Maria , CHESSARI, Gianni , JOHNSON, Christopher Norbert , TAMANINI, Emiliano , DAY, James Edward Harvey , CHIARPARIN, Elisabetta , HEIGHTMAN, Thomas Daniel , FREDERICKSON, Martyn , GRIFFITHS-JONES, Charlotte Mary
IPC分类号： C07D401/06 , C07D471/04 , C07D471/10
摘要： The invention relates to bicyclic heterocycle compounds of formula (I):
or tautomeric or stereochemically isomeric forms, N -oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R 1 , R 2a , R 2b , R 3a , R 3b , R 5 , R 6 , R 7 , R 8 , R 9 , p and E 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.-
公开(公告)号：EP2699574B1
公开(公告)日：2019-06-19
申请号：EP12717459.7
申请日：2012-04-20
发明人： BUCK, Ildiko Maria , CHESSARI, Gianni , HOWARD, Steven , REES, David Charles , WOOLFORD, Alison Jo-Anne
IPC分类号： C07D471/04 , C07D498/04 , A61K31/437 , A61K31/5383 , A61K31/4985 , A61K31/519 , A61P35/00
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公开(公告)号：EP2699574A1
公开(公告)日：2014-02-26
申请号：EP12717459.7
申请日：2012-04-20
发明人： BUCK, Ildiko Maria , CHESSARI, Gianni , HOWARD, Steven , REES, David Charles , WOOLFORD, Alison Jo-Anne
IPC分类号： C07D471/04 , C07D498/04 , A61K31/437 , A61K31/5383 , A61K31/4985 , A61K31/519 , A61P35/00
CPC分类号： C07D471/04 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/5383 , A61K31/5386 , A61K45/06 , C07D498/04 , C07D498/10 , A61K2300/00
摘要： The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V 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）的双环杂环化合物：或互变异构体或立体化学异构形式，N-氧化物，药学上可接受的盐或其溶剂合物; 其中R1，R2，R3，A，W，U和V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治疗疾病中的用途，例如， 癌症。
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7.发明公开PYRROLOPYRIDINE DERIVATIVES AND THEIR USE AS BACE INHIBITORS 审中-公开PYRROLOPYRIDINDERIVATE及其作为BACE抑制剂
公开(公告)号：EP2155749A1
公开(公告)日：2010-02-24
申请号：EP08827520.1
申请日：2008-05-14
发明人： CHESSARI, Gianni , CONGREVE, Miles Stuart , HOLENZ, Jörg , MURRAY, Christopher , PATEL, Sahil , RAKOS, Laszlo , ROTTICCI, Didier
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28
CPC分类号： C07D471/04
摘要： This invention relates to novel compounds having the structural formula I below: (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.
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公开(公告)号：EP2909197B1
公开(公告)日：2020-03-04
申请号：EP13780388.8
申请日：2013-10-18
发明人： CHESSARI, Gianni , JOHNSON, Christopher Norbert , PAGE, Lee William , MILLEMAGGI, Alessia , HOWARD, Steven , SAXTY, Gordon , HEIGHTMAN, Thomas Daniel
IPC分类号： C07D403/14 , C07D471/04 , C07D519/00 , A61K31/437 , A61P35/00
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公开(公告)号：EP3601251A1
公开(公告)日：2020-02-05
申请号：EP18715917.3
申请日：2018-03-28
IPC分类号： C07D401/06 , A61K31/4035 , A61K31/708 , C07D403/06 , C07D405/06 , C07D405/10 , C07D405/12 , C07H19/207 , C07C403/12 , C07D209/46 , A61P35/00
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公开(公告)号：EP2909198A1
公开(公告)日：2015-08-26
申请号：EP13780389.6
申请日：2013-10-18
发明人： CHESSARI, Gianni , JOHNSON, Christopher Norbert , PAGE, Lee William , BUCK, Ildiko Maria , DAY, James Edward Harvey , HOWARD, Steven , SAXTY, Gordon , MURRAY, Christopher William
IPC分类号： C07D403/14 , C07D471/04 , C07D519/00 , A61K31/437 , A61P35/00
CPC分类号： C07D403/14 , C07D471/04 , C07D519/00
摘要： The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
摘要翻译： 本发明涉及式（I）的新的双环杂环化合物：涉及包含所述化合物的药物组合物以及涉及所述化合物在治疗疾病中的用途， 癌症。
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