Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, 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 producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Application
Filed:
August 18, 2022
Publication date:
December 29, 2022
Applicant:
Adverio Pharma GmbH
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
Abstract: The present invention relates to a method of identifying a subgroup of patients suffering from diffuse cutaneous systemic sclerosis (dcSSc) which subgroup of patients benefits from a treatment with at least one sGC stimulator and/or sGC activator in a higher degree than patients not belonging to this subgroup.
Type:
Grant
Filed:
May 28, 2019
Date of Patent:
November 22, 2022
Assignee:
Adverio Pharma GmbH
Inventors:
Peter Sandner, Melanie Hemmrich, Janethe De Oliveira Pena, Stephen Dawe
Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, 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 producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
July 2, 2020
Date of Patent:
September 13, 2022
Assignee:
ADVERIO PHARMA GMBH
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
Abstract: The present application relates to a novel, cost-saving and efficient process for preparing 4-(2,2,3,3-tetrafluoropropyl)morpholine which serves as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Type:
Application
Filed:
January 15, 2020
Publication date:
March 24, 2022
Applicant:
Adverio Pharma GmbH
Inventors:
Peter Fey, Sergii Pazenok, Christian Funke, Natalya Pavlovna Kolesnik, Olexandr Ivanovich Guzyr, Yuriy Grigorievich Shermolovich
Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
Abstract: The present invention relates to methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate in the form of a novel active compound product having improved properties, for example in respect of the isolability of the active compound product, the dischargeability of the active compound product after isolation and drying and also conveyability, sieveability and micronizability of the active compound product, and to processes for the production and formulation thereof.
Type:
Application
Filed:
December 16, 2019
Publication date:
February 17, 2022
Applicant:
Adverio Pharma GmbH
Inventors:
Peter Fey, Michal Sowa, Joerg Brockob, Markus Longerich, Guido Becker, Heike Neumann
Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, 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 producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Application
Filed:
July 2, 2020
Publication date:
December 24, 2020
Applicant:
Adverio Pharma GmbH
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
Abstract: The present application relates to novel substituted 5-fluoro-1H-pyrazolopyridines, 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 producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
May 16, 2018
Date of Patent:
August 11, 2020
Assignee:
ADVERIO PHARMA GMBH
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Walter Kroh, Andreas Knorr, Eva-Maria Becker, Frank Wunder, Volkhart Min-Jian Li, Elke Hartmann, Joachim Mittendorf, Karl-Heinz Schlemmer, Rolf Jautelat, Donald Bierer
Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
Abstract: This present invention relates to forms of methyl {4.6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3.4-b]pyridino-3-yl]pyrimidino-5-yl}methylcarbamate comprising its Modification I. Modification II. mono-DMSO solvate. sesqui-DMSO solvate and ¼-ethyl acetate solvate.
Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
February 19, 2019
Date of Patent:
April 28, 2020
Assignee:
ADVERIO PHARMA GMBH
Inventors:
Peter Fey, Alfons Grunenberg, Donald Bierer
Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
Type:
Grant
Filed:
June 6, 2019
Date of Patent:
February 25, 2020
Assignee:
Adverio Pharma GmbH
Inventors:
Franz-Josef Mais, Joachim Rehse, Winfried Joentgen, Konrad Siegel
Abstract: The present invention relates to a method of identifying a subgroup of patients suffering from diffuse cutaneous systemic sclerosis (dcSSc) which subgroup of patients benefits from a treatment with at least one sGC stimulator and/or sGC activator in a higher degree than patients not belonging to this subgroup.
Type:
Application
Filed:
May 28, 2019
Publication date:
December 5, 2019
Applicant:
ADVERIO PHARMA GMBH
Inventors:
Peter SANDNER, Melanie HEMMRICH, Janethe DE OLIVEIRA PENA, Stephen DAWE
Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
Type:
Application
Filed:
June 6, 2019
Publication date:
September 19, 2019
Applicant:
ADVERIO PHARMA GmbH
Inventors:
Franz-Josef MAIS, Joachim Rehse, Winfried Joentgen, Konrad Siegel
Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
November 14, 2017
Date of Patent:
July 30, 2019
Assignee:
ADVERIO PHARMA GMBH
Inventors:
Peter Fey, Alfons Grunenberg, Donald Bierer
Abstract: The present invention relates to a process for preparing methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate of the formula (I) and to a process for purifying the crude product of the compound of the formula (I) for use as pharmaceutically active compound, where, for purification, methyl {4,6-diamino-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamate sulphinyldimethane (1:1), i.e. a compound of the formula (II), is isolated as intermediate or is generated as intermediate in this purification process, if appropriate present in a mixture.
Type:
Grant
Filed:
June 5, 2018
Date of Patent:
July 16, 2019
Assignee:
Adverio Pharma GmbH
Inventors:
Franz-Josef Mais, Joachim Rehse, Winfried Joentgen, Konrad Siegel
Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.
Type:
Application
Filed:
February 19, 2019
Publication date:
June 13, 2019
Applicant:
ADVERIO PHARMA GMBH
Inventors:
Peter FEY, Alfons Grunenberg, Donald Bierer
Abstract: The present application relates to a novel and efficient process for preparing novel substituted 5-fluoro-1H-pyrazolopyridines of the formula (VI) which are suitable as an intermediate for production of medicaments and for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders. More particularly, the 5-fluoro-1H-pyrazolopyridines of the formula (VI) are suitable for preparation of the compound of the formula (I) which serves for production of medicaments, for production of medicaments for treatment and/or prophylaxis of cardiovascular disorders.