公开(公告)号：US20220153745A1

公开(公告)日：2022-05-19

申请号：US17516542

申请日：2021-11-01

申请人： Bayer Intellectual Property GmbH ,  Bayer Pharma Aktiengesellschaft

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.

公开(公告)号：US20190016724A1

公开(公告)日：2019-01-17

申请号：US15900725

申请日：2018-02-20

申请人： Bayer Intellectual Property GmbH ,  BAYER PHARMA AKTIENGESELLSCHAFT

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.