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：US20170233413A1

公开(公告)日：2017-08-17

申请号：US15503448

申请日：2015-08-25

申请人： Bayer Pharma Aktiengesellschaft

发明人： Walter HÜBSCH ,  Alexandros VAKALOPOULOS ,  Markus FOLLMANN ,  Gaelle VALOT ,  Johannes-Peter STASCH ,  Damian BROCKSCHNIEDER ,  Tobias MARQUARDT ,  Frank WUNDER ,  Adrian TERSTEEGEN ,  Lisa DIETZ ,  Dieter LANG ,  Niels LINDNER

IPC分类号： C07D519/00 ,  C07D487/04 ,  A61K9/08 ,  A61K31/519 ,  A61K9/20 ,  A61K9/00

CPC分类号： C07D519/00 ,  A61K9/0053 ,  A61K9/08 ,  A61K9/20 ,  A61K31/519 ,  C07D471/04 ,  C07D487/04

摘要： The present application relates to novel substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

公开(公告)号：US20140031391A1

公开(公告)日：2014-01-30

申请号：US13945675

申请日：2013-07-18

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Michael HAHN ,  Markus FOLLMANN ,  Walter HÜBSCH ,  Eva-Maria BECKER ,  Johannes-Peter STASCH ,  Joerg KELDENICH ,  Martina DELBECK ,  Hanna TINEL ,  Frank WUNDER ,  Joachim MITTENDORF ,  Ildiko TEREBESI ,  Dieter LANG ,  René MARTIN

IPC分类号： C07D215/48 ,  C07D401/12 ,  A61K45/06 ,  A61K31/4706 ,  A61K31/4709 ,  C07D413/12

CPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  A61K45/06 ,  C07D217/26 ,  C07D401/12 ,  C07D413/12

摘要： The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.

摘要翻译： 本申请涉及新的5-氨基-5,6,7,8-四氢喹啉-2-羧酸，其制备方法，其用于治疗和/或预防疾病的用途及其用于生产 用于治疗和/或预防疾病的药物，特别是用于治疗和/或预防心血管和心肺疾病的药物。

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.

公开(公告)号：US20150274754A1

公开(公告)日：2015-10-01

申请号：US14738148

申请日：2015-06-12

申请人： BAYER INTELLECTUAL PROPERTY GMBH ,  BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Markus FOLLMANN ,  Johannes-Peter STASCH ,  Gorden REDLICH ,  Nils GRIEBENOW ,  Dieter LANG ,  Frank WUNDER ,  Walter HÜBSCH ,  Alexandros VAKALOPOULOS ,  Adrian TERSTEEGEN

IPC分类号： C07D519/00 ,  A61K31/53 ,  A61K45/06 ,  A61K31/519

CPC分类号： C07D519/00 ,  A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D471/04

摘要： The present application relates to novel substituted fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

摘要翻译： 本申请涉及新颖的取代的稠合嘧啶和三嗪，其制备方法，单独使用或组合用于治疗和/或预防疾病及其用于生产药物用于治疗和/或预防 疾病，特别是用于治疗和/或预防心血管疾病。