Abstract: Imidazoquinolines of formula I that contain substituted amine or amide functionality at 1-position and that are effective as Toll like Receptor 7 activators are disclosed. These compounds are useful as anticancer agents.
Type:
Grant
Filed:
June 3, 2015
Date of Patent:
September 20, 2016
Assignee:
4SC AG
Inventors:
Volker Gekeler, Thomas Maier, Astrid Zimmermann, Hans-Peter Hofmann, Sanjeev A. Kulkarni, Anil P. Jagtap, Ganesh S. Chaure
Abstract: The present invention relates to the utilization of one or more genes selected from the group comprising ZFP64, DPP3, CCDC43, HIST2H4A/B, KDELC2 and MICALL1 as biomarkers for HDAC inhibitor treatment. The expression and/or change of the aforementioned genes are preferably determined via the respective corresponding mRNA or one or more proteins expressed by the aforementioned genes.
Type:
Application
Filed:
May 22, 2014
Publication date:
July 28, 2016
Applicant:
4SC AG
Inventors:
Hella KOHLHOF, Thomas HERZ, Robert DOBLHOFER, Thomas BECKERS (Deceased), Astrid ZIMMERMANN, Marina MOLLENHAUER-THEIN, Markus BOEHM, Volker GEKELER, Hans-Peter HOFMANN, Thomas MAIER, Eike STAUB, Timo WITTENBERGER, Martin ELMLINGER
Abstract: Imidazoquinolines of formula I that contain substituted amine or amide functionality at 1-position and that are effective as Toll like Receptor 7 activators are disclosed. These compounds are useful as anticancer agents.
Type:
Application
Filed:
June 3, 2015
Publication date:
November 26, 2015
Applicant:
4SC AG
Inventors:
Volker GEKELER, Thomas MAIER, Astrid ZIMMERMANN, Hans-Peter HOFMANN, Sanjeev A. KULKARNI, Anil P. JAGTAP, Ganesh S. CHAURE
Abstract: Imidazoquinolines of formula I that contain substituted amine or amide functionality at 1-position and that are effective as Toll like Receptor 7 activators are disclosed. These compounds are useful as anticancer agents.
Type:
Grant
Filed:
March 23, 2009
Date of Patent:
July 7, 2015
Assignee:
4SC AG
Inventors:
Volker Gekeler, Thomas Maier, Astrid Zimmermann, Hans-Peter Hofmann, Sanjeev A. Kulkarni, Anil P. Jagtap, Ganesh S. Chaure
Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.
Type:
Grant
Filed:
November 20, 2012
Date of Patent:
March 3, 2015
Assignee:
4SC AG
Inventors:
Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.
Type:
Grant
Filed:
December 1, 2009
Date of Patent:
August 26, 2014
Assignee:
4SC AG
Inventors:
Thomas Maier, Thomas Bär, Thomas Beckers, Astrid Zimmermann, Siegfried Schneider, Volker Gekeler
Abstract: Process for the preparation of a compound of formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, comprising the step of reacting an acrylic acid chloride compound of formula (II?): wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, with aqueous hydroxylamine and optionally converting the resulting compound into an acid addition salt thereof.
Type:
Grant
Filed:
March 11, 2009
Date of Patent:
July 22, 2014
Assignee:
4SC AG
Inventors:
Matthias Müller, Bernd Müller, Thomas Maier
Abstract: Compounds of a certain formula (I) wherein R1, R2, R3, X, Y, r, s, t, u and v have the meanings as defined in the specification, and the salts, solvates and hydrates thereof are novel effective HDAC 6 inhibitors.
Type:
Grant
Filed:
March 12, 2009
Date of Patent:
November 5, 2013
Assignee:
4SC AG
Inventors:
Thomas Maier, Christian Hesslinger, Barbara Beckers
Abstract: A salt of (E)-N-{2-amino-phenyl)-3-{1-[4-(1-methyl-1 H-pyrazol-4-yl)-be?zenesulfonyl]-1 H-pyrrol-3-yl)-acrylamide selected from the group consisting of the hydrobromide, methansulfonate, hemi ethane-1,2-disulfonate, benzenesulfonate, toiuenesulfonate and 2-naphthalenesulfonate.
Type:
Grant
Filed:
March 11, 2009
Date of Patent:
October 15, 2013
Assignee:
4SC AG
Inventors:
Jürgen Volz, Martin Feth, Rolf-Peter Hummel, Matthias Müller, Thomas Maier, Bernd Müller
Abstract: Disclosed is a novel process for the preparation of pharmacologically interesting indolopyridine derivatives containing tetracyclic tetrahydro-11-carboline-hydantoines linked to a basic side chain and the corresponding salts, which can be used as Eg5 inhibitors, with very high overall chemical yield and enantiomeric purity.
Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5 and R6 have the meanings indicated in the description, are effective compounds with anti-proliferative and/or apoptosis inducing activity.
Type:
Grant
Filed:
February 21, 2007
Date of Patent:
September 10, 2013
Assignee:
4SC AG
Inventors:
Matthias Vennemann, Thomas Bãr, Jürgen Braunger, Astrid Zimmermann, Volker Gekeler
Abstract: The compounds of formula (I), wherein ring D and ring E together form a fused ring system selected from formula (II), (III), (IV), (V), (VI), (VII), and the salts of these compounds are novel, effective inhibitors of histone deacetylases.
Type:
Grant
Filed:
September 19, 2008
Date of Patent:
May 14, 2013
Assignee:
4SC AG
Inventors:
Thomas Maier, Thomas Beckers, Thomas Baer, Matthias Vennemann, Volker Gekeler, Astrid Zimmermann, Petra Gimmnich, Kamlesh Padiya, Hemant Joshi, Uday Joshi, Mahindra Makhija, Dipak Harel
Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.
Type:
Grant
Filed:
June 24, 2010
Date of Patent:
March 19, 2013
Assignee:
4SC AG
Inventors:
Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, for the use as a medicament.
Type:
Grant
Filed:
May 3, 2010
Date of Patent:
January 15, 2013
Assignee:
4SC AG
Inventors:
Daniel Vitt, Manfred Groeppel, Roland Baumgartner, Johann Leban
Abstract: The present invention relates to novel sulfamoyl-phenyl-ureido compounds having the formula (I) or a physiologically acceptable salt or derivative thereof which are suitable for the therapy of infections caused by protozoa and in particular uncomplicated or severe malaria caused by plasmodia.
Abstract: The invention relates to thiophene-imidazopyridine compounds according to formula (I), wherein the substituents and symbols are as defined in the description. The compounds are inhibitors of PIk1.
Type:
Grant
Filed:
June 26, 2008
Date of Patent:
September 25, 2012
Assignee:
4SC AG
Inventors:
Thomas Stengel, Mathias Schmidt, Steffen Weinbrenner, Alexander Weber, Petra Gimmnich, Volker Gekeler, Thomas Beckers, Astrid Zimmermann, Thomas Maier, Beate Schmidt, Florian Dehmel
Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.
Type:
Grant
Filed:
September 8, 2006
Date of Patent:
July 31, 2012
Assignee:
4SC AG
Inventors:
Thomas Maier, Thomas Beckers, Rolf-Peter Hummel, Martin Feth, Matthias Müller, Thomas Bär, Jürgen Volz
Abstract: This invention relates to novel aryloxypropanolamines. The invention also relates to the pharmaceutically acceptable salts and solvates containing said compounds, methods for the preparation thereof and to respective synthetic intermediates. Said compounds have agonistic activity at ?3 adrenergic receptors and are useful for treatment of ailments influenced by activation of ?3 adrenergic receptors.
Type:
Grant
Filed:
January 22, 2008
Date of Patent:
June 26, 2012
Assignee:
4SC AG
Inventors:
Stefan Tasler, Daniel Vitt, Kristina Wolf, Andrea Aschenbrenner, Peter Ney
Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.
Type:
Grant
Filed:
September 8, 2006
Date of Patent:
May 29, 2012
Assignee:
4SC AG
Inventors:
Thomas Maier, Thomas Beckers, Rolf-Peter Hummel, Martin Feth, Matthias Müller, Thomas Bär
Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.
Type:
Application
Filed:
July 1, 2011
Publication date:
February 9, 2012
Applicant:
4SC AG
Inventors:
Aldo AMMENDOLA, Julia DIEDERICHS, Johann LEBAN, Daniel VITT