Patents by Inventor Bernard Haendler
Bernard Haendler 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).
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Patent number: 11976334Abstract: The present invention covers 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine (in the following called “Compound A”), an inhibitor of ATR kinase, for use in a method of treating a hyper-proliferative disease in a subject.Type: GrantFiled: February 1, 2021Date of Patent: May 7, 2024Assignees: Bayer Aktiengesellschaft, Bayer Pharma AktiengesellschaftInventors: Antje Margret Wengner, Gerhard Siemeister, Bernard Händler, Sven Golfier, Andreas Schlicker, Li Liu
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Publication number: 20220118123Abstract: The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.Type: ApplicationFiled: February 17, 2020Publication date: April 21, 2022Applicants: Bayer Aktiengesellschaft, BAYER ASInventors: Stefanie HAMMER, Urs Beat HAGEMANN, Bernard HAENDLER, Pascale LEJEUNE, Sabine ZITZMANN-KOLBE, Christoph SCHATZ, Jenny KARLSSON
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Publication number: 20210404012Abstract: The present invention covers 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyrazol-5-yl)-1,7-naphthyridine (in the following called “Compound A”), an inhibitor of ATR kinase, for use in a method of treating a hyper-proliferative disease in a subject.Type: ApplicationFiled: February 1, 2021Publication date: December 30, 2021Applicants: Bayer Aktiengesellschaft, Bayer Pharma AktiengesellschaftInventors: Antje Margret WENGNER, Gerhard SIEMEISTER, Bernard HÄNDLER, Sven GOLFIER, Andreas SCHLICKER, Li LIU
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Publication number: 20210369724Abstract: The present invention relates to combinations of: component A: one or more 2,3-dihydroimidazo[1,2-c]quinazoline compounds of general formula (A1) or (A2) as defined herein, or a stereoisomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof; and component B: one or more ATR kinase inhibitor(s) as defined herein, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof; and, optionally, component C: one or more further pharmaceutical agent(s); and, optionally, in which either or both of components A and B in any of the above-mentioned combinations are in the form of a pharmaceutical composition which is ready for use to be administered simultaneously, concurrently, separately or sequentially. The components may be administered independently of one another by the oral, intravenous, topical, local installations, intraperitoneal or nasal route.Type: ApplicationFiled: October 9, 2019Publication date: December 2, 2021Applicant: Bayer AktiengesellschaftInventors: Antje Margret WENGNER, Gerhard SIEMEISTER, Sylvia GRÜNEWALD, Bernard HAENDLER, Ningshu LIU
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Patent number: 11185549Abstract: The present invention relates to: • combinations of: * a component A: which is a PI3K kinase inhibitor, such as copanlisib, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, in particular a physiologically acceptable salt, or a mixture of same, for example; * a component B: which is an androgen receptor antagonist, such as darolutamide or enzalutamide for example; and, optionally, * one or more pharmaceutical agents C; in which optionally either or both of said components A and B are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially; • use of such combinations: * in the treatment or prophylaxis of a cancer, particularly prostate cancer, or * for the preparation of a medicament for the treatment or prophylaxis of a cancer, particularly prostate cancer; • methods of treatment or prophylaxis of a cancer, particularly prostate cancer, in a subject, comprising administering to said subjectType: GrantFiled: June 21, 2018Date of Patent: November 30, 2021Assignees: BAYER CONSUMER CARE AG, BAYER PHARMA AKTIENGESELLSCHAFTInventor: Bernard Haendler
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Publication number: 20200222414Abstract: The present invention relates to: * combinations of: * a component A: which is a PI3K kinase inhibitor, such as co-panlisib, or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, or a salt thereof, in particular a physiologically acceptable salt, or a mixture of same, for example; * a component B: which is an androgen receptor antagonist, such as darolutamide or enzalutamide for example; and, optionally, * one or more pharmaceutical agents C; in which optionally either or both of said components A and B are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially; * use of such combinations: * in the treatment or prophylaxis of a cancer, particularly prostate cancer, or * for the preparation of a medicament for the treatment or prophylaxis of a cancer, particularly prostate cancer; * methods of treatment or prophylaxis of a cancer, particularly prostate cancer, in a subject, comprising administering to said subjecType: ApplicationFiled: June 21, 2018Publication date: July 16, 2020Applicants: BAYER CONSUMER CARE AG, BAYER PHARMA AKTIENGESELLSCHAFTInventor: Bernard HAENDLER
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Publication number: 20200063212Abstract: The present invention covers 2-[(3R)-3-methylmorpholin-4-yl]-4-(1-methyl-1H-pyrazol-5-yl)-8-(1H-pyra-zol-5-yl)-1,7-naphthyridine (in the following called “Compound A”), an inhibitor of ATR kinase, for use in a method of treating a hyper-proliferative disease in a subject.Type: ApplicationFiled: February 22, 2018Publication date: February 27, 2020Applicants: Bayer Aktiengesellschaft, Bayer Pharma AktiengesellschaftInventors: Antje Margret WENGNER, Gerhard SIEMEISTER, Bernard HÄNDLER, Sven GOLFIER, Andreas SCHLICKER, Li LIU
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Publication number: 20180164317Abstract: The present invention refers to a method and kit for stratification of melanoma patients by determining the OCR and levels of PPARGC1A, PPARGC1B and MITF RNA, derived cDNA, or corresponding protein. Especially, the invention is related to stratification kits to determine whether a patient with melanoma will respond to treatment with a BET inhibitor. In a further aspect, the invention is related to the use of a BET inhibitor for the treatment of melanoma in a patient by stratifying a sample of body fluid or tumor tissue in vitro and determining whether a patient suffering from melanoma will respond to treatment with a BET inhibitor.Type: ApplicationFiled: May 25, 2016Publication date: June 14, 2018Applicant: Bayer Pharma AktiengesellschaftInventors: Bernard HAENDLER, Kathy Ann GELATO, Laura SCHÖCKEL, Melanie HEROULT
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Patent number: 9890147Abstract: 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: GrantFiled: August 13, 2013Date of Patent: February 13, 2018Assignee: Bayer Pharma AktiengesellshaftInventors: 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
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Patent number: 9663523Abstract: The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further 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: GrantFiled: September 25, 2013Date of Patent: May 30, 2017Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Norbert Schmees, Joachim Kuhnke, Bernard Haendler, Roland Neuhaus, Pascale Lejeune, Stephan Siegel, Martin Krüger, Amaury Ernesto Fernandez-Montalvan, Hermann Künzer, Daniel Gallenkamp
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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
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SUBSTITUTED DIHYDROPYRIDO[3,4-B]PYRAZINONES AS DUAL INHIBITORS OF BET PROTEINS AND POLO-LIKE KINASES
Publication number: 20160272635Abstract: The present invention relates to substituted dihydropyrido[3,4-b]pyrazinones as dual inhibitors of BET proteins, in particular BRD4 proteins, and Polo-like kinases, in particular Plk-1 proteins of the general formula (I) in which A, X, R1, R2, R3, R4, R5, R6, R7 and n are each as defined 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 tumour disorders. Furthermore, the present invention relates to the use of the dihydropyrido[3,4-b]pyrazinones according to the invention in viral infections, in neurodegenerative disorders, in inflammation disorders, in atherosclerotic disorders and in male fertility control.Type: ApplicationFiled: July 21, 2014Publication date: September 22, 2016Inventors: Norbert Schmees, Benjamin Bader, Bernard Haendler, Volker Schulze, Ingo Hartung, Niels Bohnke, Florian Puehler -
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
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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
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Publication number: 20160129011Abstract: BET-protein-inhibitory, in particular BRD4-inhibitory bicyclo- and spirocyclically substituted 2,3-benzodiazepines of the general formula (I), pharmaceutical compositions comprising the compounds according to the invention, and the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for tumour disorders, are described. Furthermore, the use of BET protein inhibitors in benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, in neurodegenerative disorders, in inflammatory disorders, in atherosclerotic disorders and in male fertility control is described.Type: ApplicationFiled: February 17, 2014Publication date: May 12, 2016Inventors: Stephan SIEGEL, Stefan BÄURLE, Arwed CLEVE, Bernard HAENDLER, Amaury Ernesto FERNÁNDEZ-MONTALVÁN, Ursula MÖNNING, Sabine KRAUSE, Pascale LEJEUNE, Matthias BUSEMANN, Joachim KUHNKE
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Publication number: 20160009725Abstract: 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: ApplicationFiled: February 17, 2014Publication date: January 14, 2016Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Norbert SCHMEES, Bernd BUCHMANN, Bernard HAENDLER, Roland NEUHAUS, Pascale LEJEUNE, Martin KRÜGER, Amaury Ernesto FERNANDEZ-MONTALVAN, Hermann KÜNZER
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Publication number: 20150376196Abstract: BET protein-inhibitory, especially BRD2-, BRD3- and BRD4-inhibitory, 4-substituted pyrrolo- and pyrazolodiazepines of the general formula I are described, in which X, Y, n, m, p, R1, R2, R3, R4 and R5 are each as defined in the description, as are pharmaceutical compositions comprising the inventive compounds, and the prophylactic and therapeutic use thereof in the case of hyperproliferative disorders, especially in the case of neoplastic disorders. Also described is the use of the inventive compounds as BET protein inhibitors in benign hyperplasias, in atherosclerotic disorders, in sepsis, in autoimmune disorders, in vascular disorders, in viral infections, in neurodegenerative disorders, in inflammatory disorders and in male fertility control.Type: ApplicationFiled: February 18, 2014Publication date: December 31, 2015Inventors: Norbert SCHMEES, Bernd BUCHMANN, Bernard HAENDLER, Roland NEUHAUS, Pascale LEJEUNE, Martin KRÜGER, Amaury Ernesto FERNANDEZ-MONTALVAN, Hermann KÜNZER, Hartmut REHWINKEL
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Publication number: 20150344444Abstract: The present invention relates to BET protein-inhibitory, especially BRD4-inhibitory, dihydroquinoxalinones of the general formula (I) in which A, X, R1, R2, R3, R4, R5, R6, R7 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 disorders, in atherosclerotic disorders and in male fertility control.Type: ApplicationFiled: December 17, 2013Publication date: December 3, 2015Inventors: Norbert SCHMEES, Bernard HAENDLER, Detlef STÖCKIGT, Daniel GALLENKAMP
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Publication number: 20150299201Abstract: The present invention relates to BET-protein-inhibitory, in particular BRD4-inhibitory 5-aryltriazoloazepines of the general formula (I) in which R1, R2, R3 and R4 have the meanings given for the general formula (I), to pharmaceutical compositions comprising the compounds according to the invention, and to the prophylactic and therapeutic use thereof for hyperproliferative disorders, especially for neoplastic disorders. The present invention further 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: September 25, 2013Publication date: October 22, 2015Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Norbert Schmees, Joachim Kuhnke, Bernard Haendler, Roland Neuhaus, Pascale Lejeune, Stephan Siegel, Martin Krüger, Amaury Ernesto Fernandez-Montalvan, Hermann Künzer, Daniel Gallenkamp
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Publication number: 20150203483Abstract: 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: ApplicationFiled: August 13, 2013Publication date: July 23, 2015Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: 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