Abstract: The present invention relates to compounds according to general formula (I) which act as modulators of the glucocorticoid receptor and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by the glucocorticoid receptor.
Type:
Application
Filed:
July 19, 2019
Publication date:
January 23, 2020
Applicant:
Grünenthal GmbH
Inventors:
Florian JAKOB, Jo ALEN, Simon LUCAS, Tobias CRAAN, Ingo KONETZKI, Achim KLESS, Stefan SCHUNK, Paul RATCLIFFE, Sebastian WACHTEN, Simon CRUWYS
Abstract: The use of tapentadol in the treatment of pain and/or pain chronification in a subject suffering from pain chronification and/or in the treatment of pain and inhibition of pain chronification in a subject suffering from pain and at risk of pain chronification, as well as the use of tapentadol for the treatment or inhibition of migraine.
Type:
Application
Filed:
July 19, 2019
Publication date:
January 9, 2020
Applicant:
Grünenthal GmbH
Inventors:
Klaus SCHIENE, Ilona STEIGERWALD, Michel HAMON, Johannes SCHNEIDER, Silvia REINARTZ, Ulrich JAHNEL, Thomas TZSCHENTKE
Abstract: The present invention relates to an abuse-proofed oral dosage form with controlled release of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)phenol for once daily administration, which comprises the active ingredient and/or one or more of the pharmaceutically acceptable salts thereof (A), at least one synthetic or natural polymer (C), delayed-release auxiliary substances, optionally physiologically acceptable auxiliary substances (B) and optionally a wax (D), 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:
July 19, 2019
Publication date:
January 9, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
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:
July 19, 2019
Publication date:
January 9, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEISSLER, JANA DENKER, LUTZ BARNSCHEID
Abstract: The invention relates to 3-((hetero-)aryl)-alkyl-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
Type:
Application
Filed:
February 1, 2019
Publication date:
January 2, 2020
Applicant:
GRUENENTHAL GMBH
Inventors:
Sven KUEHNERT, Rene Michael KOENIGS, Achim KLESS, Anita WEGERT, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER, Klaus SCHIENE, Ingo KONETZKI
Abstract: The invention relates to a pharmaceutical composition comprising Tapentadol or a physiologically acceptable salt thereof for use in local anesthesia.
Abstract: The invention relates to 1,3-diaza-spiro-[3.4]-octane derivatives, their preparation and use in medicine, particularly in various neurological disorders, including but not limited to pain, neurodegenerative disorders, neuroinflammatory disorders, neuropsychiatric disorders, substance abuse/dependence.
Type:
Application
Filed:
August 29, 2019
Publication date:
December 19, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Paul RATCLIFFE, Ingo KONETZKI, Nikolay SITNIKOV, Thomas KOCH, Ruth JOSTOCK
Abstract: The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
Type:
Application
Filed:
June 27, 2019
Publication date:
December 19, 2019
Applicant:
Grünenthal GmbH
Inventors:
Sven KUEHNERT, Rene Michael KOENIGS, Florian JAKOB, Achim KLESS, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER, Klaus SCHIENE, Anita WEGERT
Abstract: The invention relates to 8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
Type:
Application
Filed:
June 24, 2019
Publication date:
December 12, 2019
Applicant:
Grünenthal GmbH
Inventors:
Sven KUEHNERT, Rene Michael KOENIGS, Achim KLESS, Anita WEGERT, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER
Abstract: The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
Type:
Application
Filed:
June 24, 2019
Publication date:
December 12, 2019
Applicant:
Grünenthal GmbH
Inventors:
Sven KUEHNERT, Rene KOENIGS, Achim KLESS, Anita WEGERT, Ingo KONETZKI, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER
Abstract: The invention relates to 3-(carboxyethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.
Type:
Application
Filed:
June 24, 2019
Publication date:
December 12, 2019
Applicant:
Grünenthal GmbH
Inventors:
Sven KUEHNERT, Rene Michael KOENIGS, Florian JAKOB, Achim KLESS, Anita WEGERT, Paul RATCLIFFE, Ruth JOSTOCK, Thomas KOCH, Klaus LINZ, Wolfgang SCHROEDER
Abstract: A thermoformed pharmaceutical dosage form having a breaking strength of at least 300 N, said dosage form comprising a pharmacologically active ingredient (A), a free physiologically acceptable acid (B) in an amount of from 0.001 wt.-% to 5.0 wt.-%, based on the total weight of the pharmaceutical dosage form, and a polyalkylene oxide (C) having a weight average molecular weight Mw of at least 200,000 g/mol.
Type:
Grant
Filed:
February 21, 2018
Date of Patent:
December 3, 2019
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Eric Galia, Sebastian Schwier, Ulrike Bertram, Anja Geissler, Kornelia Griessmann, Johannes Bartholomäus
Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient selected from (1r,4r)-6?-fluoro-N,N-dimethyl-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine and the physiologically acceptable salts thereof, and a second pharmacologically active ingredient selected from paracetamol and propacetamol.
Type:
Application
Filed:
July 3, 2019
Publication date:
November 21, 2019
Applicant:
Gruenenthal GmbH
Inventors:
Stefanie FROSCH, Klaus LINZ, Klaus SCHIENE
Abstract: Combinations of certain analgesics with COX-II inhibitors, related pharmaceutical compositions, including advantageous galenical forms containing these combinations, and the use of such combinations in methods of treatment, in particular for the treatment of pain.
Type:
Grant
Filed:
June 7, 2016
Date of Patent:
November 12, 2019
Assignee:
GRUENENTHAL GMBH
Inventors:
Klaus Schiene, Guenter Haase, Babette-Yvonne Koegel, Elmar Friderichs, Ulrich Jahnel
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:
June 28, 2019
Publication date:
October 24, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMAEUS, Heinrich KUGELMANN
Abstract: A method for the preparation of a powdery pharmaceutical composition composed of a pharmaceutical excipient and a pharmaceutical component, among other possible ingredients, wherein the pharmaceutical excipient is a polyalkylene glycol, the method involving grinding a mixture of the pharmaceutical excipient and the pharmaceutical component at a temperature below ambient temperature.
Type:
Grant
Filed:
May 25, 2016
Date of Patent:
October 22, 2019
Assignee:
GRÜNENTHAL GMBH
Inventors:
Alessandro Grassano, Anna Perachiotti, Matteo Minelli, Daniele Volpi
Abstract: The use of tapentadol for the manufacture of a medicament comprising at least one administration unit A containing dose a of tapentadol and at least one administration unit B containing dose b of tapentadol, where dose a<dose b, for the treatment of pain.
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:
June 7, 2019
Publication date:
September 19, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN
Abstract: The use of tapentadol for the treatment of pain associated with disorders of the trigeminal nerve, in particular for use in the treatment of pain associated with trigeminal neuralgia.
Type:
Application
Filed:
May 28, 2019
Publication date:
September 12, 2019
Applicant:
GRUENENTHAL GMBH
Inventors:
Thomas CHRISTOPH, Jean De Vry, Thomas Tzschentke, Petra Bloms-Funke, Klaus Schiene, Michel Hamon
Abstract: The invention relates to a tamper-resistant tablet comprising (i) a matrix material in an amount of more than one third of the total weight of the tablet; and (ii) a plurality of particulates in an amount of less than two thirds of the total weight of the tablet; wherein said particulates comprise a pharmacologically active compound and a polyalkylene oxide; and form a discontinuous phase within the matrix material; and method of using said tablet to treat pain and other conditions.
Type:
Application
Filed:
May 20, 2019
Publication date:
September 5, 2019
Applicant:
Grünenthal GmbH
Inventors:
Sebastian SCHWIER, Marcel Haupts, Udo Rüttgers, Lutz Barnscheid, Jana DENKER