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 present invention provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a therapeutically effective amount of a slow release Tapentadol Hydrochloride and therapeutically effective amount of a second analgesic, wherein the second analgesic is gamma-aminobutyric acid (GABA) analogue. The present invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a slow release Tapentadol Hydrochloride and a therapeutically effective amount of a second analgesic, wherein the second analgesic is gamma-aminobutyric acid (GABA) analogue.
Abstract: The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the ? opioid receptor and/or the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.
Type:
Application
Filed:
July 14, 2015
Publication date:
July 27, 2017
Applicant:
Gruenenthal GmbH
Inventors:
Anita WEGERT, Sven KUEHNERT, Rene Michael KOENIGS, Bert NOLTE, Klaus LINZ, Stephanie HARLFINGER, Babette-Yvonne KOEGEL, Paul RATCLIFFE, Fritz THEIL, Olga GROEGER, Birgit BRAUN
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: 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: 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: 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 present invention provides a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol. The present invention further provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol.
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 pharmaceutical dosage form and method of using same, the pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, said dosage form containing a pharmacologically active ingredient (A); a physiologically acceptable polymer (B) obtainable by polymerization of a monomer composition comprising an ethylenically unsaturated monomer bearing an anionic functional group, in protonated form or a physiologically acceptable salt thereof; a polyalkylene oxide (C) having a weight average molecular weight of at least 200,000 g/mol, wherein the content of the polyalkylene oxide (C) is at least 20 wt.-%, based on the total weight of the dosage form; wherein the pharmacologically active ingredient (A) is present in a controlled-release matrix comprising the polymer (B) and the polyalkylene oxide (C).
Type:
Grant
Filed:
September 1, 2011
Date of Patent:
May 2, 2017
Assignee:
GRUENENTHAL GMBH
Inventors:
Lutz Barnscheid, Sebastian Schwier, Johannes Bartholomäus
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