公开(公告)号：US11149018B2

公开(公告)日：2021-10-19

申请号：US16604157

申请日：2018-04-04

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Hartmut Beck ,  Raimund Kast ,  Mark Meininghaus ,  Chantal Fuerstner ,  Timo Stellfeld ,  Clemens-Jeremias Von Buehler ,  Lisa Dietz ,  Michaela Bairlein ,  Johanna Anlahr ,  Hannah Joerissen ,  Peter Hauff ,  Joerg Mueller ,  Karoline Droebner ,  Jens Nagel

IPC分类号： C07D401/04 ,  A61P1/16 ,  A61P13/12 ,  A61P11/00 ,  C07D215/50 ,  C07D417/04 ,  A61K45/06 ,  C07D413/04

摘要： The present application relates to novel substituted N-arylethyl-2-aminoquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.

公开(公告)号：US11787797B2

公开(公告)日：2023-10-17

申请号：US17161615

申请日：2021-01-28

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Mueller ,  Sherif El Sheikh ,  Han Jie Zhou ,  Changjia Zhao ,  David B. Sykes ,  Steven James Ferrara ,  Kery Liu ,  Simon Anthony Herbert ,  Claudia Merz ,  Michael Niehues ,  Carl Friedrich Nising ,  Martina Schäfer ,  Katja Zimmermann ,  Jörg Knäblein ,  Kai Thede ,  Thomas Faupel

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C12N1/20 ,  C12P17/18

CPC分类号： C07D471/04 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C12N1/20 ,  C12P17/18 ,  C12P17/182 ,  C12P17/188

摘要： The present invention provides triazolone compounds of general formula (I):




in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US11136296B2

公开(公告)日：2021-10-05

申请号：US16603719

申请日：2018-04-04

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft

发明人： Hartmut Beck ,  Raimund Kast ,  Mark Meininghaus ,  Lisa Dietz ,  Chantal Fuerstner ,  Timo Stellfeld ,  Sonja Anlauf ,  Clemens-Jeremias Von Buehler ,  Michaela Bairlein ,  Johanna Anlahr ,  Uwe Muenster ,  Carsten Terjung ,  Hannah Joerissen ,  Peter Hauff ,  Joerg Mueller ,  Karoline Droebner ,  Jens Nagel

IPC分类号： C07D215/50

摘要： The present application relates to novel substituted N-arylethyl-2-arylquinoline-4-carboxamide derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prevention of diseases, and to the use thereof for production of medicaments for treatment and/or prevention of diseases, especially for treatment and/or prevention of fibrotic and inflammatory disorders.

公开(公告)号：US11713304B2

公开(公告)日：2023-08-01

申请号：US17407951

申请日：2021-08-20

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Müller ,  Sherif El Sheikh ,  David B. Sykes ,  Steven James Ferrara ,  Michael Kröber ,  Claudia Merz ,  Michael Niehues ,  Martina Schäfer ,  Katja Zimmermann ,  Carl Friedrich Nising

IPC分类号： A61P35/00 ,  C07D401/12 ,  C07D249/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K45/06

CPC分类号： C07D401/12 ,  A61P35/00 ,  C07D249/12 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  A61K45/06

摘要： The present invention provides triazolone compounds of general formula (I):




in which R1, R2, R3, R4, and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment and prophylaxis of diseases, in particular hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US10968216B2

公开(公告)日：2021-04-06

申请号：US16345178

申请日：2017-10-25

申请人： BAYER AKTIENGESELLSCHAFT ,  BAYER PHARMA AKTIENGESELLSCHAFT ,  THE BROAD INSTITUTE, INC. ,  PRESIDENT AND FELLOWS OF HARVARD COLLEGE ,  THE GENERAL HOSPITAL CORPORATION

发明人： Stefan Nikolaus Gradl ,  Duy Nguyen ,  Knut Eis ,  Judith Günther ,  Timo Stellfeld ,  Andreas Janzer ,  Sven Christian ,  Thomas Mueller ,  Sherif El Sheikh ,  Han Jie Zhou ,  Changjia Zhao ,  David B. Sykes ,  Steven James Ferrara ,  Kery Liu ,  Simon Anthony Herbert ,  Claudia Merz ,  Michael Niehues ,  Carl Friedrich Nising ,  Martina Schäfer ,  Katja Zimmermann ,  Jörg Knäblein ,  Kai Thede ,  Thomas Faupel

IPC分类号： C07D471/04 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C12N1/20 ,  C12P17/18

摘要： The present invention provides triazolone compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

公开(公告)号：US10023539B2

公开(公告)日：2018-07-17

申请号：US15534404

申请日：2015-12-08

申请人： Bayer Pharma Aktiengesellschaft

发明人： Jeffrey Stuart Mowat ,  Timo Stellfeld ,  Carlo Stresemann ,  Roman Hillig ,  Silke Köhr ,  Detlef Stöckigt ,  Jörg Weiske ,  Thomas Brumby ,  Naomi Barak ,  Clara Christ ,  Antonius Ter Laak ,  Volker Badock ,  Rosemary Helen Crampton ,  Ian Stefanuti

IPC分类号： C07D231/06 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R1, R2, R3, R4, R5, X and r have the meaning as described and defined herein, as well as to pharmaceutical compositions comprising compounds according to the invention and to their prophylactic and therapeutic use for hyper-proliferative disorders, in particular for cancer, respectively tumor disorders. The present invention furthermore relates to the use of SMYD2 inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, neurodegenerative disorders, inflammatory disorders, atherosclerotic disorders and the control of male fertility.