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:
Grant
Filed:
July 19, 2019
Date of Patent:
April 20, 2021
Assignee:
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 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:
Application
Filed:
November 2, 2020
Publication date:
February 18, 2021
Applicant:
GRÜNENTHAL GMBH
Inventors:
KLAUS WENING, SEBASTIAN SCHWIER, ULRIKE BERTRAM
Abstract: A pharmaceutical dosage form for administration twice daily, once daily or less frequently, which contains 6?-fluoro-(N-methyl- or N,N-dimethyl)-4-phenyl-4?,9?-dihydro-3?H-spiro[cyclohexane-1,1?-pyrano[3,4,b]indol]-4-amine or a physiologically acceptable salt thereof.
Type:
Grant
Filed:
August 24, 2016
Date of Patent:
February 9, 2021
Assignee:
Grünenthal GmbH
Inventors:
Nadja Gruening, Marc Schiller, Ashish Hemani, Chris Kirby, Ingo Friedrich, John Bothmer, Andreas Scholz
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:
September 2, 2020
Publication date:
February 4, 2021
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 an an aqueous pharmaceutical composition for parenteral administration comprising Tapentadol or a physiologically acceptable salt thereof; wherein the concentration of Tapentadol is greater than 8.00 mg/mL, based on the weight of Tapentadol free base and based on the total volume of the composition; wherein the composition comprises a buffer system; and wherein the pH value of the composition is within the range of from greater than 3.0 to less than 6.7. The invention also relates to a kit comprising the composition according to the invention in a packaging. The pharmaceutical composition according to the invention is particularly useful for treating pain, especially acute pain, preferably in adult patients.
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 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 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-((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:
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, Klaus SCHIENE, lngo KONETZKI
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-(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