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公开(公告)号：US20190016724A1
公开(公告)日：2019-01-17
申请号：US15900725
申请日：2018-02-20
发明人： Dirk BROHM , Melanie HEROULT , Marie-Pierre COLLIN , Walter HÜBSCH , Mario LOBELL , Klemens LUSTIG , Sylvia GRÜNEWALD , Ulf BÖMER , Verena VÖHRINGER
IPC分类号： C07D487/04 , A61K31/541 , A61K31/5377 , A61K31/53 , A61K31/5355
摘要： This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(═O)-NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR9R10, —C(═O)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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公开(公告)号：US20220153745A1
公开(公告)日：2022-05-19
申请号：US17516542
申请日：2021-11-01
发明人： Dirk BROHM , Melanie HEROULT , Marie-Pierre COLLIN , Walter HÜBSCH , Mario LOBELL , Klemens LUSTIG , Sylvia GRÜNEWALD , Ulf BÖMER , Verena VÖHRINGER
IPC分类号： C07D487/04 , C07D409/14 , C07D409/04 , A61P35/00 , A61K31/53 , A61K31/5355 , A61K31/5377 , A61K31/541
摘要： This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(=0)-NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR9R10, —C(=0)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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公开(公告)号：US20130158000A1
公开(公告)日：2013-06-20
申请号：US13715553
申请日：2012-12-14
发明人： Dirk BROHM , Melanie HEROULT , Marie-Pierre COLLIN , Walter HÜBSCH , Mario LOBELL , Klemens LUSTIG , Sylvia GRÜNEWALD , Ulf BÖMER
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/53 , A61K31/5355 , A61K31/5377 , A61K31/541
摘要： This invention relates to novel substituted 5-(1-benzothiophen-2-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
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公开(公告)号：US20170320854A1
公开(公告)日：2017-11-09
申请号：US15581064
申请日：2017-04-28
发明人： Marie-Pierre COLLIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FÜRSTNER , Elisabeth POOK , Matthias Beat WITTWER , Klemens LUSTIG , Anja BUCHMÜLLER , Hanna TINEL , Karoline DRÖBNER , Thomas MONDRITZKI , Heiko SCHIRMER , Axel KRETSCHMER , Carsten SCHMECK , Pierre WASNAIRE , Hana CERNECKA
IPC分类号： C07D401/14 , A61K45/06 , A61K31/4439
CPC分类号： C07D401/14 , A61K31/4439 , A61K45/06
摘要： The present invention relates to novel 5-(carboxamide)-1-pyridinyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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公开(公告)号：US20180251447A1
公开(公告)日：2018-09-06
申请号：US15969222
申请日：2018-05-02
发明人： Marie-Pierre COLLIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FÜRSTNER , Elisabeth POOK , Matthias Beat WITTWER , Klemens LUSTIG , Anja BUCHMÜLLER , Hanna TINEL , Karoline DRÖBNER , Thomas MONDRITZKI , Heiko SCHIRMER , Axel KRETSCHMER , Carsten SCHMECK , Pierre WASNAIRE , Hana CERNECKA
IPC分类号： C07D401/14 , A61K45/06 , A61K31/4439
摘要： The present invention relates to novel 5-(carboxamide)-1-pyridinyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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公开(公告)号：US20160221965A1
公开(公告)日：2016-08-04
申请号：US15021372
申请日：2014-09-12
发明人： Alexander STRAUB , Marie-Pierre COLLIN , Michael KOCH , Jutta MEYER , Karl-Heinz SCHLEMMER , Carl Friedrich NISING , Nicole BIBER , Sonja ANLAUF , Matthias Beat WITTWER
IPC分类号： C07D239/47 , A61K45/06 , C07D401/12 , C07D239/56 , C07D239/36 , C07D401/06 , A61K31/513 , C07D239/52
CPC分类号： C07D239/47 , A61K31/513 , A61K45/06 , C07D239/36 , C07D239/52 , C07D239/54 , C07D239/545 , C07D239/56 , C07D401/06 , C07D401/12
摘要： The present application relates to novel 2,5-disubstituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.
摘要翻译： 本申请涉及新的2,5-二取代的6-（三氟甲基）嘧啶-4（3H） - 酮衍生物，其制备方法单独使用或组合用于治疗和/或预防疾病，以及 用于制备用于治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管，肾，炎症和纤维化疾病。
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公开(公告)号：US20200017473A1
公开(公告)日：2020-01-16
申请号：US16579341
申请日：2019-09-23
发明人： Marie-Pierre COLLIN , Peter KOLKHOF , Thomas NEUBAUER , Chantal FUERSTNER , Elisabeth POOK , Matthias Beat WITTWER , Klemens LUSTIG , Anja BUCHMUELLER , Hanna TINEL , Karoline DROEBNER , Thomas MONDRITZKI , Heiko SCHIRMER , Axel KRETSCHMER , Carsten SCHMECK , Pierre WASNAIRE , Hana CERNECKA
IPC分类号： C07D401/14 , A61P9/04 , A61P13/12 , A61P3/10 , A61P9/10 , A61K45/06 , A61K31/4439
摘要： The present invention relates to novel 5-(carboxamide)-1-pyridinyl-1,2,4-triazole derivatives, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
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公开(公告)号：US20160237059A1
公开(公告)日：2016-08-18
申请号：US15021559
申请日：2014-09-12
发明人： Alexander STRAUB , Marie-Pierre COLLIN , Michael KOCH , Jutta MEYER , Karl-Heinz SCHLEMMER , Carl Friedrich NISING , Nicole BIBER , Sonja ANLAUF , Alexey GROMOV , Matthias Beat WITTWER
IPC分类号： C07D401/04 , A61K31/513 , C07D411/04 , C07D403/04 , C07D413/04 , C07D417/04 , C07D413/06 , C07D403/06 , C07D401/06 , C07D409/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D405/06 , C07D417/06 , C07D471/04 , C07D405/12 , A61K31/5377 , C07D239/36 , A61K45/06
CPC分类号： C07D401/04 , A61K31/506 , A61K31/513 , A61K31/5377 , A61K45/06 , C07D239/36 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/04 , C07D409/06 , C07D411/04 , C07D413/04 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , C07D471/04
摘要： The present application relates to novel heterocyclically substituted 6-(trifluoromethyl)pyrimidin-4(3H)-one derivatives, to processes for their preparation, to their use alone or in combinations for the treatment and/or prevention of diseases, and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for treatment and/or prevention of cardiovascular, renal, inflammatory and fibrotic diseases.
摘要翻译： 本申请涉及新的杂环取代的6-（三氟甲基）嘧啶-4（3H） - 酮衍生物，其制备方法单独使用或组合用于治疗和/或预防疾病及其用途 用于制备用于治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管，肾，炎症和纤维化疾病。
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