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 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 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-(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 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 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
Abstract: A pharmaceutical dosage form is disclosed having a breaking strength of at least 300 N and comprising (i) an ephedrine component selected from the group consisting of ephedrine, pseudoephedrine and the physiologically acceptable salts thereof, wherein preferably the weight content of the ephedrine component is within the range of from 0.1 to 60 wt.-%, relative to the total weight of the pharmaceutical dosage form; and (ii) a physiologically acceptable conversion inhibitor that is capable of inhibiting the chemical conversion ex vivo of the ephedrine component into methamphetamine. Also disclosed is a method of treating a disease, disorder or condition, preferably selected from the group consisting of tissue hyperemia, edema, and nasal congestion, comprising the administration of the pharmaceutical dosage form to a subject in need thereof.
Type:
Application
Filed:
February 8, 2019
Publication date:
August 15, 2019
Applicant:
Grünenthal GmbH
Inventors:
Isabell IMMOHR, Peter PERSICH, Alexander WESQUET, Carmen STOMBERG, Klaus WENING, Sebastian SCHWIER
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:
July 11, 2018
Date of Patent:
August 6, 2019
Assignee:
GRÜNENTHAL GMBH
Inventors:
Johannes Bartholomaeus, Heinrich Kugelmann
Abstract: A tamper-resistant pharmaceutical dosage form comprising a pharmacologically active ingredient embedded in a prolonged release matrix, which comprises a prolonged release matrix material selected from the group consisting of nonionic acrylic polymers and waxy materials and which provides prolonged release of the pharmacologically active ingredient, resistance against solvent extraction, resistance against grinding, and resistance against dose-dumping in aqueous ethanol.
Type:
Grant
Filed:
April 17, 2013
Date of Patent:
July 2, 2019
Assignee:
GRUNENTHAL GMBH
Inventors:
Klaus Wening, Lutz Barnscheid, Sebastian Schwier
Abstract: Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
Type:
Grant
Filed:
November 21, 2017
Date of Patent:
June 18, 2019
Assignee:
GRUNENTHAL GMBH
Inventors:
Mazen Hanna, Ning Shan, Miranda L. Cheney, David R. Weyna, Raymond K. Houck
Abstract: A pharmaceutical dosage form exhibiting a breaking strength of at least 500 N, wherein the dosage form contains a pharmacologically active ingredient (A); an inorganic salt (B); and 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 inorganic salt (B) and the polyalkylene oxide (C) and wherein, under in vitro conditions, the release profile of the pharmacologically active ingredient (A) from the matrix comprises at least a time interval during which the release follows zero order kinetics.
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:
January 9, 2019
Publication date:
May 16, 2019
Applicant:
GRUNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
Abstract: Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.
Type:
Application
Filed:
November 12, 2018
Publication date:
May 16, 2019
Applicant:
GRUNENTHAL GMBH
Inventors:
Mazen HANNA, Ning SHAN, David R. WEYNA, Miranda L. CHENEY
Abstract: The invention relates to a tamper-resistant pharmaceutical dosage form comprising one or more particles, wherein each of said one or more particles comprises a pharmacologically active ingredient and a physiologically acceptable polymer; has a breaking strength of at least 300 N; has a weight of at least 2 mg; and optionally, comprises a film-coating; wherein the total weight of the pharmaceutical dosage form is greater than the total weight of said one or more particles.
Type:
Application
Filed:
November 9, 2018
Publication date:
May 16, 2019
Applicant:
GRÜNENTHAL GMBH
Inventors:
LUTZ BARNSCHEID, ANJA GEIßLER, KLAUS WENING, JANA PÄTZ