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公开(公告)号：US09403827B2
公开(公告)日：2016-08-02
申请号：US14762037
申请日：2014-01-21
申请人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Andrea Vaupel
发明人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Andrea Vaupel
IPC分类号： A61K31/522 , C07D473/28
CPC分类号： C07D473/28 , A61K31/522
摘要： The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of as MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译： 本发明涉及式（I）化合物：本文所述的（I）化合物，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM2的活性介导的病症或疾病的用途和用途的方法， 或MDM4，以及包含这些化合物的组合。
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公开(公告)号：US09365576B2
公开(公告)日：2016-06-14
申请号：US13900061
申请日：2013-05-22
申请人： Simona Cotesta , Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
发明人： Simona Cotesta , Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
IPC分类号： C07D487/04 , A61K31/407 , A61K31/44 , A61K31/5377 , A61K31/506 , A61K31/41 , A61K31/4439 , A61K45/06
CPC分类号： C07D487/04 , A61K31/407 , A61K31/41 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06
摘要： The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译： 本发明涉及式（I）化合物：如本文所述，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的这些化合物的用途和方法，以及 包含这些化合物的组合。
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公开(公告)号：US20130317024A1
公开(公告)日：2013-11-28
申请号：US13900061
申请日：2013-05-22
申请人： Simona Cotesta , Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
发明人： Simona Cotesta , Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
IPC分类号： C07D487/04 , A61K31/4439 , A61K45/06 , A61K31/5377 , A61K31/41 , A61K31/407 , A61K31/506
CPC分类号： C07D487/04 , A61K31/407 , A61K31/41 , A61K31/4439 , A61K31/506 , A61K31/5377 , A61K45/06
摘要： The invention relates to compounds of formula (I): as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译： 本发明涉及式（I）化合物：如本文所述，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的这些化合物的用途和方法，以及 包含这些化合物的组合。
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公开(公告)号：US08969341B2
公开(公告)日：2015-03-03
申请号：US14361068
申请日：2012-11-28
申请人： Pascal Furet , Vito Guagnano , Philipp Holzer , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
发明人： Pascal Furet , Vito Guagnano , Philipp Holzer , Robert Mah , Keiichi Masuya , Achim Schlapbach , Stefan Stutz , Andrea Vaupel
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/517 , A61K31/519 , A61K31/505 , A61K31/4709 , A61K31/4523 , A61K31/4155 , C07D413/14 , C07D487/14 , C07D239/02 , C07D403/14 , C07D215/00 , C07D211/80 , C07D401/14 , C07D257/02 , C07D487/04 , A61K31/41 , A61K31/4162 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/506
CPC分类号： C07D487/04 , A61K31/41 , A61K31/4162 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/519 , A61K31/5377
摘要： The invention relates to compounds of formula (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.
摘要翻译： 本发明涉及本文所述的式（I）化合物，包含这些化合物的药物制剂，用于治疗由MDM2和/或MDM4的活性介导的疾病或疾病的化合物的用途和用途，以及组合 包括这样的化合物。
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公开(公告)号：US08859586B2
公开(公告)日：2014-10-14
申请号：US14127159
申请日：2012-06-19
申请人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
发明人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
IPC分类号： C07D217/22 , A61K31/47 , A61K31/4725 , A61K31/472 , C07D405/08 , C07D401/08 , C07D217/24
CPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , C07D217/04 , C07D401/08 , C07D405/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译： 本发明涉及式（I）化合物：如申请中所定义。 这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。
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公开(公告)号：US20140275158A1
公开(公告)日：2014-09-18
申请号：US14127159
申请日：2012-06-19
申请人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
发明人： Pascal Furet , Vito Guagnano , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
IPC分类号： C07D217/24 , C07D405/08 , A61K31/4725 , A61K31/472 , C07D401/08
CPC分类号： C07D217/24 , A61K31/472 , A61K31/4725 , C07D217/04 , C07D401/08 , C07D405/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译： 本发明涉及式（I）化合物：如申请中所定义。 这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。
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公开(公告)号：US07795288B2
公开(公告)日：2010-09-14
申请号：US10578826
申请日：2004-11-12
申请人： Guido Bold , Andreas Floersheimer , Pascal Furet , Vito Guagnano , Keiichi Masuya , Andrea Vaupel , Joseph Schoepfer
发明人： Guido Bold , Andreas Floersheimer , Pascal Furet , Vito Guagnano , Keiichi Masuya , Andrea Vaupel , Joseph Schoepfer
IPC分类号： A61K31/426 , C07D277/20
CPC分类号： C07D277/42 , C07D231/38 , C07D409/04 , C07D417/04 , C07D417/10
摘要： The invention relates to thiazole and pyrazole derivatives of formula (I) wherein Q is S and X is C, or Q is CH and X is N; R1 is unsubstituted or substituted phenyl; and R2 is unsubstituted or substituted aryl or heteroaryl; or a salt of the said compounds, and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour disease, in particular such diseases which respond to an inhibition of the Flt-3 kinase.
摘要翻译： 本发明涉及式（I）的噻唑和吡唑衍生物，其中Q为S且X为C，或Q为CH且X为N; R1是未取代或取代的苯基; 并且R 2是未取代或取代的芳基或杂芳基; 或所述化合物的盐，以及其制备方法，包含该衍生物的药物组合物，以及这些衍生物在制备用于治疗特别是增殖性疾病如肿瘤疾病的药物组合物中的用途， 特别是对Flt-3激酶的抑制作出反应的这些疾病。
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公开(公告)号：US20070167449A1
公开(公告)日：2007-07-19
申请号：US10578826
申请日：2004-11-12
申请人： Guido Bold , Andreas Floersheimer , Pascal Furet , Vito Guagnano , Keiichi Masuya , Andrea Vaupel , Joseph Schoepfer
发明人： Guido Bold , Andreas Floersheimer , Pascal Furet , Vito Guagnano , Keiichi Masuya , Andrea Vaupel , Joseph Schoepfer
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/427 , A61K31/416 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D277/42 , C07D231/38 , C07D409/04 , C07D417/04 , C07D417/10
摘要： The invention relates to thiazole and pyrazole derivatives of formula (I) wherein Q is S and X is C, or Q is CH and X is N; R1 is unsubstituted or substituted phenyl; and R2 is unsubstituted or substituted aryl or heteroaryl; or a salt of the said compounds, and to processes for the preparation thereof, to pharmaceutical compositions comprising such derivatives and to the use of such derivatives for the preparation of pharmaceutical compositions for the treatment especially of a proliferative disease, such as a tumour disease, in particular such diseases which respond to an inhibition of the Flt-3 kinase.
摘要翻译： 本发明涉及式（I）的噻唑和吡唑衍生物，其中Q是S，X是C，或Q是CH，X是N; R 1是未取代或取代的苯基; R 2是未取代或取代的芳基或杂芳基; 或所述化合物的盐，以及其制备方法，包含该衍生物的药物组合物，以及这些衍生物在制备用于治疗特别是增殖性疾病如肿瘤疾病的药物组合物中的用途， 特别是对Flt-3激酶的抑制作出反应的这些疾病。
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9.发明申请TETRA-SUBSTITUTED HETEROARYL COMPOUNDS AND THEIR USE AS MDM2 AND/OR MDM4 MODULATORS 审中-公开TETRA取代的杂环化合物及其作为MDM2和/或MDM4调节剂的用途公开(公告)号：US20120149661A1
公开(公告)日：2012-06-14
申请号：US13392231
申请日：2010-08-24
申请人： Guido Bold , Pascal Furet , Francois Gessier , Joerg Kallen , Joanna Hergovich Lisztwan , Keiichi Masuya , Andrea Vaupel
发明人： Guido Bold , Pascal Furet , Francois Gessier , Joerg Kallen , Joanna Hergovich Lisztwan , Keiichi Masuya , Andrea Vaupel
IPC分类号： A61K31/4164 , C07D403/04 , A61K31/4178 , C07D413/12 , A61P35/00 , C07F9/40 , A61K31/675 , C07F7/18 , A61K31/695 , C07D233/90 , A61K31/5377
CPC分类号： C07D207/34 , C07D231/14 , C07D233/64 , C07D233/84 , C07D233/88 , C07D233/90 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/12 , C07D413/14 , C07F7/0812 , C07F9/6506
摘要： The invention relates to tetra-substituted heteroarylic compounds of the formula (I) wherein X1, X3 and X4 are independently C or N, Y is C—H, N—H or N, wherein the total number of nitrogen atoms represented by X1, X3, X4 and Y is 1 or 2; rings A and B are independently selected from phenyl or pyridyl; R1, R4, R′, R″, n and m are as defined herein. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译： 本发明涉及式（I）的四取代杂芳基化合物，其中X 1，X 3和X 4独立地为C或N，Y为C-H，N-H或N，其中由X1表示的总氮原子， X3，X4和Y为1或2; 环A和B独立地选自苯基或吡啶基; R 1，R 4，R'，R“，n和m如本文所定义。 这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。
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公开(公告)号：US08859535B2
公开(公告)日：2014-10-14
申请号：US14127155
申请日：2012-06-19
申请人： Nicole Buschmann , Pascal Furet , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
发明人： Nicole Buschmann , Pascal Furet , Philipp Holzer , Joerg Kallen , Keiichi Masuya , Stefan Stutz
IPC分类号： C07D409/10 , A61K31/472 , A61K31/4725 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/10 , C07D405/14 , C07D491/08 , C07D493/08 , C07D451/14 , C07D413/08 , C07D451/02
CPC分类号： A61K31/4725 , A61K31/472 , C07D217/24 , C07D401/04 , C07D401/10 , C07D401/14 , C07D405/10 , C07D405/14 , C07D409/10 , C07D413/08 , C07D451/02 , C07D451/14 , C07D491/08 , C07D493/08
摘要： The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.
摘要翻译： 本发明涉及式（I）化合物：如申请中所定义。 这些化合物适用于治疗由MDM2和/或MDM4或其变体的活性介导的病症或疾病。
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