Abstract: The invention relates to certain compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders that are, at least partially, mediated by TSPO activity.
Type:
Grant
Filed:
October 11, 2013
Date of Patent:
October 3, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Petra Bloms-Funke, Gregor Bahrenberg, Wolfgang Schröder, Sven Kühnert, Simon Lucas
Abstract: The invention relates to certain compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders that are, at least partially, mediated by TSPO activity.
Type:
Application
Filed:
June 14, 2017
Publication date:
September 28, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
Petra BLOMS-FUNKE, Gregor Bahrenberg, Wolfgang Schröder, Sven Kühnert, Simon Lucas
Abstract: The invention relates to a pharmaceutical dosage form, preferably with controlled release of a pharmacologically active compound (A) contained therein, the pharmaceutical dosage form very preferably being tamper-resistant and most preferably having a breaking strength B1 of at least 500 N in direction of extension E1 and having a breaking strength B2 of less than 500 N in direction of extension E2.
Type:
Grant
Filed:
December 11, 2015
Date of Patent:
September 5, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Eugeen Marie Jozef Jans, Filip René Irena Kiekens, Jody Firmin Marceline Voorspoels, Anne Faure, Iris Ziegler, Elisabeth Arkenau-Maric, Lutz Barnscheid, Johannes Bartholomäus, Marc Frevel, Eric Galia, Andrea Schüessele
Abstract: A solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.
Type:
Application
Filed:
May 5, 2017
Publication date:
August 24, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN
Abstract: The invention relates to a pharmaceutical dosage form comprising (i) at least one formed segment (S1), which contains a first pharmacologically active ingredient (A1) and provides prolonged release thereof, and (ii) at least one further segment (S2), which contains a second pharmacologically active ingredient (A2) and provides immediate release thereof, wherein the at least one formed segment (S1) exhibits a higher breaking strength than the at least one further segment (S2) and the at least one formed segment (S1) exhibits a breaking strength of more than 500 N.
Type:
Grant
Filed:
May 27, 2014
Date of Patent:
August 22, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Anja Geiβler, Klaus Wening, Stefanie Strauch, Jana Pätz, Sebastian Schwier
Abstract: The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors. to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
April 23, 2015
Date of Patent:
August 8, 2017
Assignee:
GRUNENTHAL GMBH
Inventors:
Antonio Nardi, Paul Ratcliffe, Tobias Craan, Torsten Hertrampf, Bernhard Lesch, Robert Kime, Henning Steinhagen
Abstract: The present invention relates to an abuse-proofed, oral dosage form with controlled opioid-release for once daily administration, characterised in that it comprises at least one opioid with potential for abuse (A), at least one synthetic or natural polymer (C), optionally delayed-release matrix auxiliary substances, physiologically acceptable auxiliary substances (B), optionally a wax (D) and optionally at least one delayed-release coating, component (C) or (D) in each case exhibiting a breaking strength of at least 500 N, preferably of at least 1000 N.
Type:
Application
Filed:
March 1, 2016
Publication date:
July 27, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
Abstract: The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.
Type:
Application
Filed:
March 15, 2017
Publication date:
July 27, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMAEUS, Heinrich KUGELMANN
Abstract: Novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
Type:
Grant
Filed:
February 9, 2016
Date of Patent:
June 27, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Florian Jakob, Ingo Konetzki, Tobias Craan, Antonio Nardi, Christian Hesslinger
Abstract: Novel solution complexes of zoledronic acid are described which give rise to improved properties of zoledronic acid. The invention includes aqueous solution and molecular complexes of zoledronic acid with and optical isomers of asparagine, histidine, arginine and proline as well as pharmaceutical complexes containing them and methods of treatment using them.
Type:
Grant
Filed:
March 13, 2015
Date of Patent:
June 20, 2017
Assignee:
GRUNENTHAL GMBH
Inventors:
Mazen Hanna, Ning Shan, Miranda Cheney, David R. Weyna
Abstract: A solid administration form, protected from parenteral abuse and containing at least one viscosity-increasing agent in addition to one or more active substances that have parenteral abuse potential. The agent forms, when a necessary minimum amount of an aqueous liquid is added, on the basis of an extract obtained from the administration form, a preferably injectable gel that remains visually distinct when introduced into another quantity of an aqueous liquid.
Type:
Grant
Filed:
August 24, 2016
Date of Patent:
June 13, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Johannes Bartholomaeus, Heinrich Kugelmann
Abstract: The invention relates to novel substituted condensed pyrimidine compounds of general formula (I) in which the chemical groupings, substituents and indices are as defined in the description, and to their use as medicaments, in particular as medicaments for the treatment of conditions and diseases that can be treated by inhibition of the PDE4 enzyme.
Type:
Grant
Filed:
August 4, 2015
Date of Patent:
June 6, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Ingo Konetzki, Florian Jakob, Tobias Craan, Christian Hesslinger, Paul Ratcliffe, Jason J. Shiers
Abstract: The invention relates to a pharmaceutical dosage form having a breaking strength of at least 300 N and comprising a pharmacologically active compound, an anionic polymer bearing carboxylic groups, wherein the content of the anionic polymer is ?20 wt.-%, based on the total weight of the pharmaceutical dosage form, and a nonionic surfactant.
Type:
Grant
Filed:
May 27, 2016
Date of Patent:
May 23, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Jessica Redmer, Sebastian Schwier
Abstract: The invention relates to pharmaceutical salts comprised of a pharmaceutical active substance and of at least one sugar substitute, to medicaments containing these salts, and to the use of these salts for producing medicaments.
Type:
Application
Filed:
February 1, 2017
Publication date:
May 18, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMÄUS, HEINRICH KUGELMAN
Abstract: The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Application
Filed:
January 12, 2017
Publication date:
May 4, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
STEFAN SCHUNK, Melanie Reich, Florian Jakob, Nils Damann, Michael Haurand, Achim Kless, Marc Rogers, Kathy Sutton
Abstract: A gastro-retentive pharmaceutical dosage form of a therapeutically effective amount of at least one GABA Analog, at least one opioid, and at least one pharmaceutically acceptable excipient wherein the said dosage form is retained in the stomach for at least four hours and is suitable for formulating for once daily or twice daily administration. Further provided is a method of treating a disorder by administering to a patient in need thereof, a gastro-retentive pharmaceutical dosage form of a therapeutically effective amount of at least one GABA Analog, at least one opioid, and at least one pharmaceutically acceptable excipient wherein the said dosage form is retained in the stomach for at least four hours and is suitable for once daily or twice daily administration. The opioid is either in slow release form or in immediate release form.
Abstract: A tamper-resistant pharmaceutical dosage form comprising a multitude of particles which comprise a pharmacologically active compound, a polyalkylene oxide, and a disintegrant; wherein the pharmacologically active compound is dispersed in a matrix comprising the polyalkylene oxide and the disintegrant; wherein the content of the disintegrant is more than 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; wherein the content of the polyalkylene oxide is at least 25 wt.-%, based on the total weight of the pharmaceutical dosage form and/or based on the total weight of the particles; and wherein the dosage form provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.
Type:
Application
Filed:
January 9, 2017
Publication date:
April 27, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEIßLER, JANA DENKER, LUTZ BARNSCHEID
Abstract: The invention relates to a dosage form that is thermoformed without discoloration and is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse. The invention also relates to a corresponding method for producing said dosage form.
Type:
Grant
Filed:
April 19, 2016
Date of Patent:
April 25, 2017
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elisabeth Arkenau-Maric, Johannes Bartholomaeus, Heinrich Kugelmann
Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Application
Filed:
October 7, 2016
Publication date:
April 13, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
Stefan SCHUNK, Melanie Reich, René Michael Koenigs
Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Application
Filed:
October 7, 2016
Publication date:
April 13, 2017
Applicant:
GRÜNENTHAL GMBH
Inventors:
Stefan Schunk, Melanie Reich, René Michael Koenigs