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:
August 31, 2020
Publication date:
December 24, 2020
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:
August 31, 2020
Publication date:
December 24, 2020
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: 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:
August 31, 2020
Publication date:
December 24, 2020
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 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:
September 2, 2020
Publication date:
December 24, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
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 coated 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 physiologically acceptable polymer, preferably a polyalkylene oxide; and form a discontinuous phase within the matrix material; which preferably provides under in vitro conditions immediate release of the pharmacologically active compound in accordance with Ph. Eur.; and method of using said tablet to treat pain and other conditions.
Type:
Grant
Filed:
December 19, 2018
Date of Patent:
December 15, 2020
Assignee:
Grünenthal GmbH
Inventors:
Sebastian Schwier, Marcel Haupts, Lutz Barnscheid, Jana Pätz
Abstract: A hitherto unknown crystalline form of (?)-(1R,2R)-3-(3-dimethylamino-1-ethyl-2-methylpropyl)-phenol hydrochloride, pharmaceutical compositions containing the new crystalline form, methods of producing the new crystalline form, and a related method of use including treatment of, e.g., pain and/or urinary incontinence.
Type:
Application
Filed:
June 23, 2020
Publication date:
December 10, 2020
Applicant:
Grünenthal GmbH
Inventors:
Andreas Fischer, Helmut Buschmann, Michael Gruss, Dagmar Lischke
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:
August 17, 2020
Publication date:
December 3, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN
Abstract: The invention relates to a pharmaceutical dosage form which is particularly useful for the prevention of an overdose of the pharmacologically active ingredient contained therein after accidental or intentional simultaneous administration of a plurality of the dosage forms containing an overall supratherapeutic dose of the pharmacologically active ingredient.
Type:
Grant
Filed:
September 9, 2016
Date of Patent:
November 24, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Klaus Wening, Sebastian Schwier, Ulrike Bertram
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:
Grant
Filed:
February 1, 2019
Date of Patent:
November 10, 2020
Assignee:
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: 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 14, 2020
Publication date:
October 29, 2020
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, ANJA GEIßLER- FICHTNER, JANA DENKER, LUTZ BARNSCHEID
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:
Grant
Filed:
July 19, 2019
Date of Patent:
October 27, 2020
Assignee:
Grünenthal GmbH
Inventors:
Klaus Schiene, Ilona Steigerwald, Michel Hamon, Johannes Schneider, Silvia Reinartz, Ulrich Jahnel, Thomas Tzschentke
Abstract: A pharmaceutical combination comprising as components (a) at least one 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol compound, and (b) at least one NMDA-antagonist, a pharmaceutical formulation and a dosage form comprising such a combination, and a method of treating pain, e.g. inflammatory pain or neuropathic pain, in which components (a) and (b) are administered simultaneously or sequentially to a mammal, with component (a) being administered either before or after component (b), and with components (a) or (b) being administered to the mammal either via the same pathway of administration or via different pathways of administration.
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:
Grant
Filed:
June 24, 2019
Date of Patent:
October 20, 2020
Assignee:
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-(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:
Grant
Filed:
June 27, 2019
Date of Patent:
October 20, 2020
Assignee:
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:
Grant
Filed:
June 24, 2019
Date of Patent:
October 6, 2020
Assignee:
GRUENENTHAL 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:
Grant
Filed:
June 24, 2019
Date of Patent:
October 6, 2020
Assignee:
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: The present invention relates to a device for the topical treatment of pain affecting the vulvar area of the female human genital organ, a formulation for use in the device according to the invention, and a kit comprising the device according to the present intention. Additionally, the present invention relates to a method of topical treatment of pain affecting the vulvar area of the female human genital organ, said method using the device according to the present invention. The device is a layered article shaped to be placed in use inside a female undergarment and at least partially in skin contact with the female vulvar area and comprises a topical formulation.
Type:
Grant
Filed:
November 14, 2016
Date of Patent:
September 8, 2020
Assignee:
GRUENENTHAL GMBH
Inventors:
Andre Dimino, Marco Pappagallo, Michael Richardson, Franz Gerstheimer, Emilio Garcia Quetglas, Jacqueline Delfgaauw, Andreas Scholz, Johannes Niel Van
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:
May 11, 2020
Publication date:
September 3, 2020
Applicant:
Grünenthal GMBH
Inventors:
KLAUS WENING, ANJA GEIßLER, JANA DENKER, LUTZ BARNSCHEID
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:
Grant
Filed:
August 29, 2019
Date of Patent:
August 11, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Paul Ratcliffe, Ingo Konetzki, Nikolay Sitnikov, Thomas Koch, Ruth Jostock
Abstract: The present invention relates to a process for the production of an abuse-proofed dosage form containing, apart from one or more active ingredients with potential for abuse and optionally physiologically acceptable auxiliary substances, at least one synthetic or natural polymer (C) with a breaking strength of at least 500 N, wherein the formulation mixture is combined with a solvent for the polymer (C) at least in quantities such that the formulation mixture is at least uniformly moistened, the at least moistened composition is optionally divided into sub-portions, dried and shaped to yield the dosage form.
Type:
Grant
Filed:
September 2, 2016
Date of Patent:
August 4, 2020
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elisabeth Arkenau-Marić, Johannes Bartholomäus