Patent number: 9890147
Abstract: What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumor disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
Type:
Grant
Filed:
August 13, 2013
Date of Patent:
February 13, 2018
Assignee:
Bayer Pharma Aktiengesellshaft
Inventors:
Stephan Siegel, Stefan Bäurle, Arwed Cleve, Bernard Haendler, Amaury Ernesto Fernandez-Montalvan, Ursula Mönning, Sabine Krause, Pascale Lejeune, Norbert Schmees, Matthias Busemann, Simon Holton, Joachim Kuhnke
Publication number: 20160009725
Abstract: What is described are BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, bicyclo- and spino-substituted pyrrolo- and pyrazolodiazepines of the general formula I in which X, Y, n, m, R1, R2, R3, R4 and R5 are each as defined in the description, to intermediates for preparation of the inventive compounds, to pharmaceutical compositions comprising the inventive compounds, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for tumour disorders. Also described is the use of the compounds according to the invention as BET protein inhibitors for benign hyperplasias, for atherosclerotic disorders, for sepsis, for autoimmune disorders, for vascular disorders, for viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for male fertility control.
Type:
Application
Filed:
February 17, 2014
Publication date:
January 14, 2016
Applicant:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Norbert SCHMEES, Bernd BUCHMANN, Bernard HAENDLER, Roland NEUHAUS, Pascale LEJEUNE, Martin KRÜGER, Amaury Ernesto FERNANDEZ-MONTALVAN, Hermann KÜNZER
Publication number: 20150203483
Abstract: What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.
Type:
Application
Filed:
August 13, 2013
Publication date:
July 23, 2015
Applicant:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Stephan Siegel, Stefan Bäurle, Arwed Cleve, Bernard Haendler, Amaury Ernesto Fernandiez-Montalvan, Ursula Mönning, Sabine Krause, Pascale Lejeune, Norbert Schmees, Matthias Busemann, Simon Holton, Joachim Kuhnke