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.

公开(公告)号：US20130158000A1

公开(公告)日：2013-06-20

申请号：US13715553

申请日：2012-12-14

申请人： BAYER INTELLECTUAL PROPERTY GmbH

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.

公开(公告)号：US20130190290A1

公开(公告)日：2013-07-25

申请号：US13748043

申请日：2013-01-23

申请人： BAYER INTELLECTUAL PROPERTY GmbH

发明人： Frank SÜßMEIER ,  Mario LOBELL ,  Sylvia GRÜNEWALD ,  Michael HÄRTER ,  Bernd BUCHMANN ,  Joachim TELSER ,  Hannah JÖRIßEN ,  Melanie HEROULT ,  Antje KAHNERT ,  Klemens LUSTIG ,  Niels LINDNER

IPC分类号： C07D487/04 ,  A61K31/4439 ,  A61K31/5377 ,  A61K31/4188 ,  A61K31/496 ,  A61K45/06

CPC分类号： C07D487/04 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06

摘要： The present application relates to novel 1-phenyl-1H-imidazo[1,2-b]pyrazole derivatives, to processes for their preparation, to their use 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 angiogenic disorders and hyperproliferative disorders, where neovascularization plays a role, such as, for example, neoplastic disorders and tumour disorders. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.

摘要翻译： 本申请涉及新颖的1-苯基-1H-咪唑并[1,2-b]吡唑衍生物，其制备方法，其用于治疗和/或预防疾病及其用于制备药物的用途 治疗和/或预防新生血管形成起作用的疾病，特别是血管生成障碍和过度增殖性疾病，例如肿瘤性疾病和肿瘤病症。 这样的治疗可以作为单一疗法进行，也可以与其他药物组合进行或进一步的治疗措施。

公开(公告)号：US20210147414A1

公开(公告)日：2021-05-20

申请号：US17046004

申请日：2019-04-03

申请人： Bayer Pharma Aktiengesellschaft

发明人： Mario LOBELL ,  Hartmut SCHIROK ,  Adrian TERSTEEGEN

IPC分类号： C07D471/04 ,  A01N1/00 ,  A61K9/20 ,  A61K47/36 ,  A61K9/00 ,  A61P7/02

摘要： The invention relates to 5-({6-amino-2-[4-(5-chloro-2-cyanophenyl)-5-methoxy-2-oxopyridin-1(2H)-yl]-3-methylhexanoyl}amino)pyrazolo[1,5-a]pyridine-3-carboxamide, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and edemas, and also ophthalmic disorders, and its use to inhibit disturbing plasma kallikrein activity for the conduct of extracorporeal procedures and analytical assays.

公开(公告)号：US20200339567A1

公开(公告)日：2020-10-29

申请号：US16758751

申请日：2018-10-18

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Daniel MEIBOM ,  Jutta MEYER ,  Karl COLLINS ,  Nuria ORTEGA HERNANDEZ ,  Jan STAMPFUSS ,  Frank WUNDER ,  Till FREUDENBERGER ,  Thomas MONDRITZKI ,  Nina Alexandra SCHEERER ,  Kirsten LEINEWEBER ,  Jens SCHAMBERGER ,  Alexander STRAUB ,  Kersten Matthias GERICKE ,  Walter KROH ,  Mario LOBELL ,  Klaus MÜNTER

IPC分类号： C07D471/04 ,  C07D519/00 ,  A61K31/444 ,  A61K45/06 ,  A61P9/10 ,  A61K31/437

摘要： The present application relates to novel substituted imidazopyridine amides of the formula (I), 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 the production of medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular, neurological and central nervous as well as metabolic disorders.

公开(公告)号：US20170253602A1

公开(公告)日：2017-09-07

申请号：US15529043

申请日：2015-11-23

申请人： Bayer Pharma Aktiengesellschaft

发明人： Andreas SCHALL ,  Jürgen KLAR ,  Mario LOBELL ,  Hartmut SCHIROK ,  Joachim TELSER ,  Steffen MÜLLER ,  Dirk BROHM ,  Hans BRIEM ,  Hannah JÖRIßEN ,  Joerg KELDENICH (deceased) ,  Michael BÖTTGER ,  Georges DEGENFELD VON ,  Thomas SCHLANGE ,  Ulf BÖMER ,  Niels LINDNER ,  Hanna EILKEN ,  Dmitrij HRISTODOROV ,  Pierre WASNAIRE ,  Kersten Matthias GERICKE ,  Lars BÄRFACKER

IPC分类号： C07D487/04 ,  A61K39/395 ,  A61K31/5513

CPC分类号： C07D487/04 ,  A61K31/5513 ,  A61K39/39558

摘要： The present application relates to novel (3-hydroxyphenyl)amino-substituted pyrido[2,3-b][1,5]benzodiazepin-5-one derivatives, to processes for preparation thereof, to the use thereof alone or in combination for treatment and/or prevention of diseases and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially of angiogenic disorders and hyperproliferative disorders in which neovascularization plays a role, for example ophthalmological disorders and cancers and tumours. Such treatments can be effected as monotherapy or else in combination with other medicaments or further therapeutic measures.

公开(公告)号：US20170283412A1

公开(公告)日：2017-10-05

申请号：US15513853

申请日：2015-09-22

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Susanne RÖHRIG ,  Alexander HILLISCH ,  Julia STRAßBURGER ,  Stefan HEITMEIER ,  Martina Victoria SCHMIDT ,  Karl-Heinz SCHLEMMER ,  Adrian TERSTEEGEN ,  Anja BUCHMÜLLER ,  Christoph GERDES ,  Martina SCHÄFER ,  Henrik TELLER ,  Eloisa JIMÉNEZ NÚNEZ ,  Hartmut SCHIROK ,  Jürgen KLAR ,  Mario LOBELL

IPC分类号： C07D471/04

CPC分类号： C07D471/04

摘要： The invention relates to substituted oxopyridine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

公开(公告)号：US20160346402A1

公开(公告)日：2016-12-01

申请号：US15105486

申请日：2014-12-10

申请人： BAYER PHARMA AKTIENGESELLSCHAFT

发明人： Hans-Georg LERCHEN ,  Sven WITTROCK ,  Nils GRIEBENOW ,  Beatrix STELTE-LUDWIG ,  Anette SOMMER ,  Sandra BERNDT ,  Christoph MAHLERT ,  Mario LOBELL ,  Carsten TERJUNG ,  Simone GREVEN ,  Yolanda CANCHO GRANDE

IPC分类号： A61K47/48 ,  C07D233/64 ,  C07D403/12 ,  C07K5/062 ,  C07D207/337 ,  C07D403/14 ,  C07C53/18 ,  C07K16/32 ,  C07D231/12 ,  C07K16/28 ,  C07K5/107

CPC分类号： A61K47/6851 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6849 ,  C07C53/18 ,  C07D207/335 ,  C07D207/337 ,  C07D231/12 ,  C07D233/64 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07K5/06052 ,  C07K5/1016 ,  C07K16/2863 ,  C07K16/2875 ,  C07K16/32 ,  C07K2317/24 ,  C07K2317/565 ,  C07K2317/75 ,  C07K2317/92

摘要： The present application relates to novel antibody drug conjugates (ADCs), to active metabolites of these ADCs, to processes for preparing these ADCs, to the use of these ADCs for the treatment and/or prophylaxis of diseases and to the use of these ADCs for preparing medicaments for treatment and/or prevention of diseases, in particular hyperproliferative and/or angiogenic disorders such as, for example, cancer diseases. Such treatments can be carried out as monotherapy or else in combination with other medicaments or further therapeutic measures.

摘要翻译： 本申请涉及新型抗体药物偶联物（ADC），这些ADC的活性代谢物，制备这些ADC的方法，使用这些ADC用于治疗和/或预防疾病，以及使用这些ADC 制备用于治疗和/或预防疾病的药物，特别是过度增殖和/或血管生成疾病，例如癌症疾病。 这样的治疗可以作为单一疗法进行，也可以与其他药物组合进行或进一步的治疗措施。