Publication number: 20220153745
Abstract: This invention relates to novel substituted 5-(1-benzothiophen-2-yl) pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives of formula (I) wherein R1 is hydrogen, chloro, methyl or methoxy, R2 is hydrogen or methoxy, with the proviso that at least one of R1 and R2 is other than hydrogen, G1 represents chloro, (C1-C4)-alkyl, (C1-C4)-alkoxycarbonyl, 5-membered aza-heteroaryl, or the group —CH2—OR3, —CH2—NR4R5 or —C(=0)-NR4R6, and G2 represents chloro, cyano, (C1-C4)-alkyl, or the group —CR8AR8B—OH, —CH2—NR9R10, —C(=0)—NR11R12 or —CH2—OR15, having protein tyrosine kinase inhibitory activities, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for treating proliferative disorders, in particular cancer and tumor diseases.
Type:
Application
Filed:
November 1, 2021
Publication date:
May 19, 2022
Inventors:
Dirk BROHM, Melanie HEROULT, Marie-Pierre COLLIN, Walter HÜBSCH, Mario LOBELL, Klemens LUSTIG, Sylvia GRÜNEWALD, Ulf BÖMER, Verena VÖHRINGER
Patent number: 11298367
Abstract: The present invention relates to prodrugs of 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl ]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[3-(trifluoromethyl)-pyridin-2-yl ]-1H-1,2,4-triazole-5-carboxamide, 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl ]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[2-(trifluoromethyl)-phenyl]-1H-1,2,4-triazole-5-carboxamide and 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl ]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-(3-chloropyridin-2-yl)-1H-1,2,4-triazole-5-carboxamide, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
Type:
Grant
Filed:
October 17, 2018
Date of Patent:
April 12, 2022
Assignee:
Bayer Aktiengesellschaft
Inventors:
Marie-Pierre Collin-Kroepelin, Peter Kolkhof, Thomas Neubauer, Chantal Fuerstner, Elisabeth Pook, Matthias Beat Wittwer, Carsten Schmeck, Pierre Wasnaire, Heiko Schirmer, Hana Cernecka, Karoline Droebner, Hanna Tinel, Anja Buchmueller, Thomas Mondritzki, Axel Kretschmer, Klemens Lustig, Robert Fricke, Guillaume Levilain, Ursula Krenz, Norbert Witowski
Publication number: 20200338096
Abstract: The present invention relates to prodrugs of 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[3-(trifluoromethyl)-pyridin-2-yl]-1H-1,2,4-triazole-5-carboxamide, 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-[2-(trifluoromethyl)-phenyl]-1H-1,2,4-triazole-5-carboxamide and 3-({3-(4-chlorophenyl)-5-oxo-4-[(2S)-3,3,3-trifluoro-2-hydroxypropyl]-4,5-dihydro-1H-1,2,4-triazol-1-yl}methyl)-1-(3-chloropyridin-2-yl)-1H-1,2,4-triazole-5-carboxamide, to processes for the preparation of such compounds, to pharmaceutical compositions containing such compounds, and to the use of such compounds or compositions for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of renal and cardiovascular diseases.
Type:
Application
Filed:
October 17, 2018
Publication date:
October 29, 2020
Inventors:
Marie-Pierre COLLIN-KROEPELIN, Peter KOLKHOF, Thomas NEUBAUER, Chantal FUERSTNER, Elisabeth POOK, Matthias Beat WITTWER, Carsten SCHMECK, Pierre WASNAIRE, Heiko SCHIRMER, Hana CERNECKA, Karoline DROEBNER, Hanna TINEL, Anja BUCHMUELLER, Thomas MONDRITZKI, Axel KRETSCHMER, Klemens LUSTIG, Robert FRICKE, Guillaume LEVILAIN, Ursula KRENZ, Norbert WITOWSKI
Patent number: 10722501
Abstract: The present application relates to novel substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]triazol-3-ones of formula (I), to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of lung inflammation disorders.
Type:
Grant
Filed:
May 8, 2017
Date of Patent:
July 28, 2020
Assignees:
BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Nicole Biber, Damian Brockschnieder, Kersten Matthias Gericke, Florian Kölling, Klemens Lustig, Jörg Meding, Heinrich Meier, Thomas Neubauer, Martina Schäfer, Andreas Timmermann, Dmitry Zubov, Carsten Terjung, Niels Lindner, Volker Badock, Dieter Moosmayer, Hideki Miyatake Ondozabal, Stephen Moore, Alexander Schulz