Patents by Inventor Detlef Stockigt
Detlef Stockigt has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).
-
Publication number: 20190047980Abstract: The present invention covers heteroarylbenzimidazole 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 and/or inflammatory disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 15, 2016Publication date: February 14, 2019Inventors: Volker SCHULZE, Tobias HEINRICH, Florian PRINZ, Julien LEFRANC, Jens SCHRÖDER, Anne MENGEL, Wilhelm BONE, Joszef BÁLINT, Antje Margret WENGNER, Knut EIS, Horst IRLBACHER, Marcus KOPPITZ, Ulf BÖMER, Benjamin BADER, Hans BRIEM, Philip LIENAU, Clara CHRIST, Detlef STÖCKIGT, Roman HILLIG
-
Publication number: 20180263970Abstract: The present invention includes methods of treating patients with acute myeloid leukemia across a range of genetic subtypes with DHODH inhibitors, such as 6-fluoro-2-(2?-fluoro-[1,1?-biphenyl]-4-yl)-3-methylquinoline-4-carboxylic acid).Type: ApplicationFiled: August 29, 2016Publication date: September 20, 2018Applicants: THE BROAD INSTITUTE, INC., THE GENERAL HOSPITAL CORPORATION, PRESIDENT AND FELLOWS OF HARVARD COLLEGE, BAYER PHARMA AKTIENGESELLSCHAFTInventors: David B. Sykes, David Scadden, Timothy A. Lewis, Andreas Janzer, Hanna Meyer, Detlef Stöckigt
-
Patent number: 10023539Abstract: 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.Type: GrantFiled: December 8, 2015Date of Patent: July 17, 2018Assignee: Bayer Pharma AktiengesellschaftInventors: 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
-
Publication number: 20180118722Abstract: 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, R3, R4, R5 and n 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 hyperproliferative disorders, in particular for cancer, respectively tumour 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.Type: ApplicationFiled: April 14, 2016Publication date: May 3, 2018Applicant: Bayer Pharma AktiengesellschaftInventors: Timo STELLFELD, Carlo STRESEMANN, Roman HILLIG, Silke KÖHR, Detlef STÖCKIGT, Jörg WEISKE, Naomi BARAK, Clara CHRIST, Antonius TER LAAK, Volker BADOCK
-
Publication number: 20180099937Abstract: 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 and R5 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 hyperproliferative disorders, in particular for cancer, respectively tumour 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.Type: ApplicationFiled: April 14, 2016Publication date: April 12, 2018Applicant: Bayer Pharma AktiengesellschaftInventors: Timo STELLFELD, Jeffrey Stuart MOWAT, Carlo STRESEMANN, Roman HILLIG, Silke KÖHR, Detlef STÖCKIGT, Jörg WEISKE, Ingo HARTUNG, Naomi BARAK, Clara CHRIST, Antonius TER LAAK, Volker BADOCK, Rosemary Helen CRAMPTON, Ian STEFANUTI
-
Publication number: 20170342034Abstract: 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 tumour 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.Type: ApplicationFiled: December 8, 2015Publication date: November 30, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Jeffrey Stuart MOWAT, Timo STELLFELD, Carlo STRESEMANN, Roman HILLIG, Silke KÖHR, Detlef STÖCKIGT, Jörg WEISKE, Thomas BRUMBY, Naomi BARACK, Clara CHRIST, Antonius TER LAAK, Volker BADOCK, Rosemary Helen CRAMPTON, Ian STEFANUTI
-
Publication number: 20170334899Abstract: The present invention relates to amino-substituted isothiazoles of general formula (I): in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: January 26, 2015Publication date: November 23, 2017Inventors: Lars BÄRFACKER, Gerhard SIEMEISTER, Tobias HEINRICH, Stefan PRECHTL, Detlef STÖCKIGT, Antje ROTTMANN
-
Publication number: 20170217946Abstract: The present invention relates to amino-substituted isoxazoles of general formula (I): in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: July 22, 2015Publication date: August 3, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Lars BÄRFACKER, Tobias HEINRICH, Gerhard SIEMEISTER, Stefan PRECHTL, Detlef STÖCKIGT, Antje ROTTMANN
-
Patent number: 9682995Abstract: The present invention relates to isothiazoles of general formula (I) which inhibit the mitotic checkpoint: in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.Type: GrantFiled: January 28, 2014Date of Patent: June 20, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Lars Bärfacker, Stefan Prechtl, Gerhard Siemeister, Antje Margret Wengner, Jens Ackerstaff, Katrin Nowak-Reppel, Benjamin Bader, Philip Lienau, Detlef Stöckigt, Tobias Heinrich
-
Patent number: 9663510Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: GrantFiled: December 10, 2012Date of Patent: May 30, 2017Assignees: BAYER PHARMA AKTIENGESELLSCHAFT, BAYER INTELLECTUAL PROPERTY GMBHInventors: Volker Schulze, Dirk Kosemund, Antje Margret Wengner, Gerhard Siemeister, Detlef Stöckigt, Michael Brüning
-
Publication number: 20170121322Abstract: The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory 3,4-dihydropyrido[2,3-b]pyrazinones with a meta-substituted aromatic amino or ether group of the general formula (I) in which A, X, Y, R1, R2, R3, R4, R5, R6 and n are each as defined in the description, to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of tumour disorders. Furthermore, this invention relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammatory diseases, in atherosclerotic disorders and in male fertility control.Type: ApplicationFiled: June 15, 2015Publication date: May 4, 2017Applicant: Bayer Pharma AktiengesellschaftInventors: Norbert SCHMEES, Bernard HAENDLER, Detlef STÖCKIGT, Richard Alexander BISSELL, Richard Alexander BOUGLAS, Ian STEFANUTI, Stephan SIEGEL
-
Patent number: 9586958Abstract: The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.Type: GrantFiled: June 6, 2014Date of Patent: March 7, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Volker Schulze, Hans-Georg Lerchen, Donald Bierer, Antje Margret Wengner, Gerhard Siemeister, Philip Lienau, Ursula Krenz, Dirk Kosemund, Detlef Stöckigt, Michael Brüning, Ulrich Lücking, Ildikó Terebesi
-
Patent number: 9555022Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.Type: GrantFiled: June 14, 2011Date of Patent: January 31, 2017Assignee: Bayer Intellectual Property GmbHInventors: Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Marcus Koppitz, Detlef Stöckigt, Olaf Prien
-
Publication number: 20160264568Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: June 3, 2014Publication date: September 15, 2016Inventors: Volker K. SCHULZE, Andreas SCHALL, Hans BRIEM, Antje Margret WENGNER, Gerhard SIEMEISTER, Detlef STÖCKIGT, Philip LIENAU
-
Publication number: 20160207928Abstract: The present invention relates to novel compounds showing an inhibitory effect on Mps-1 kinase, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: June 4, 2014Publication date: July 21, 2016Inventors: Volker SCHULZE, Hartmut SCHIROK, Dirk KOSEMUND, Hans BRIEM, Benjamin BADER, Ulf BÖMER, Antje Margret WENGNER, Gerhard SIEMEISTER, Philip LIENAU, Detlef STÖCKIGT, Ulrich LÜCKING, Andreas SCHALL
-
Publication number: 20160207915Abstract: The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, processes for their preparation, and their use for the treatment and/or prophylaxis of diseases.Type: ApplicationFiled: June 6, 2014Publication date: July 21, 2016Inventors: Volker Schulze, Hans-Georg Lerchen, Donald Bierer, Antje Margret Wengner, Gerhard Siemeister, Philip Lienau, Ursula Krenz, Dirk Kosemund, Detlef Stockigt, Michael Bruning, Ulrich Lucking, Ildiko Terebesi
-
Publication number: 20160193206Abstract: The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory, dihydropyridopyrazinones of the general formula (I) in which A, X, R1, R2, R3, R4, R4, R6, R7 and n have the meanings given in the description, to intermediates for preparation of the compounds according to the invention, to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. This invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammation diseases, in atherosclerotic disorders and in male fertility control.Type: ApplicationFiled: December 17, 2013Publication date: July 7, 2016Inventors: Norbert SCHMEES, Benjamin BADER, Bernard HAENDLER, Detlef STÖCKIGT, Pascale LEJEUNE, Amaury Ernesto FERNANDEZ-MONTALVAN, Timo STELLFELD, Daniel GALLENKAMP
-
Publication number: 20160176867Abstract: The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory, dihydroquinoxalinones and dihydropyridopyrazinones of the general formula (I) in which A, X, R1, R2, R3, R4, R5, R6 and n 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 in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. This invention further relates to the use of BET protein inhibitors in viral infections, in neurodegenerative disorders, in inflammation diseases, in atherosclerotic disorders and in male fertility control.Type: ApplicationFiled: July 7, 2014Publication date: June 23, 2016Inventors: Norbert SCHMEES, Bernard HAENDLER, Detlef STÖCKIGT, Daniel GALLENKAMP, Richard BISSELL, Richard Alexander BOUGLAS
-
Publication number: 20160120854Abstract: The present invention relates to pharmaceutical compositions of substituted triazolopyridine compounds of general formula (I) as described and defined herein, to methods of preparing said compositions, and to the use of the compositions for the treatment or prophylaxis of a disease.Type: ApplicationFiled: June 5, 2014Publication date: May 5, 2016Inventors: Volker SCHULZE, Michael BRÜNING, Detlef STÖCKIGT
-
Publication number: 20150368260Abstract: The present invention relates to isothiazoles of general formula (I) which inhibit the mitotic checkpoint: in which A, R1 and R2 are as defined in the claims, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neoplasms, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: January 28, 2014Publication date: December 24, 2015Inventors: Lars BÄRFACKER, Stefan PRECHTL, Gerhard SIEMEISTER, Antje Margret WENGNER, Jens ACKERSTAFF, Katrin NOWAK-REPPEL, Benjamin BADER, Philip LIENAU, Detlef STÖCKIGT, Tobias HEINRICH