Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones 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:
Grant
Filed:
October 7, 2016
Date of Patent:
October 23, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Stefan Schunk, Melanie Reich, René Michael Koenigs
Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones 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:
Grant
Filed:
October 7, 2016
Date of Patent:
October 16, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Stefan Schunk, Melanie Reich, René Michael Koenigs
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:
May 15, 2018
Publication date:
October 4, 2018
Applicant:
GRUENENTHAL 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:
May 21, 2018
Publication date:
September 27, 2018
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:
May 15, 2018
Publication date:
September 27, 2018
Applicant:
GRUENENTHAL 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 method for producing a medicament dosage form which consists of at least one piece which in each case comprises at least one medicament and at least one additive, the medicament and the additive being mixed and extruded from a die as a strand and the strand being cut into pieces of precise weight. The invention additionally relates to a device.
Type:
Grant
Filed:
March 11, 2014
Date of Patent:
September 25, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elisabeth Arkenau-Marić, Johannes Bartholomäus, Dieter Schateikis, Kai-Uwe Ustorf
Abstract: The invention relates to a hot-melt extruded pharmaceutical dosage form with controlled release of a pharmacologically active ingredient (A) embedded in a matrix comprising a polymer (C), the dosage form exhibiting a breaking strength of at least 300 N and having an oblong shape comprising a longitudinal direction of extension, a transversal direction of extension orthogonal to the longitudinal direction of extension, a front side, an opposite back side and a circumferential rim between said front and back side; wherein the core of the pharmaceutical dosage form has a morphological orientation caused by hot-melt extrusion that is substantially orthogonal to the longitudinal direction of extension of the dosage form; and/or the release per area of the pharmacologically active ingredient (A) through the front side and the opposite back side is faster than the release through the circumferential rim.
Abstract: The invention relates to a pharmaceutical composition comprising a first pharmacologically active ingredient, which is 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, which is a propionic acid derivative selected from the group consisting of ibuprofen, naproxen, ketoprofen, flurbiprofen, fenoprofen, fenbufen, suprofen, pirprofen, indoprofen, tiaprofenic acid, oxaprozin, ibuproxam, flunoxaprofen, alminoprofen, naproxcinod, and the physiologically acceptable salts thereof.
Type:
Grant
Filed:
March 21, 2016
Date of Patent:
September 18, 2018
Assignee:
Gruenenthal GmbH
Inventors:
Stefanie Frosch, Klaus Linz, Klaus Schiene
Abstract: A thermoformed, tamper-resistant pharmaceutical dosage form comprises: a) a pharmacologically active ingredient; b) a polyalkylene oxide having a weight average molecular weight of more than 200,000 g/mol; and c) a zinc component, wherein the content of said zinc component is at least 1 ppm, relative to the total weight of the pharmaceutical dosage form. When the pharmacologically active ingredient is effective against pain, the pharmaceutical dosage form may be used in a method of treating pain. When the pharmacologically active ingredient has abuse potential, the pharmaceutical dosage form may be used in a method of reducing the incidence of the abuse of said pharmacologically active ingredient.
Type:
Grant
Filed:
May 10, 2013
Date of Patent:
September 4, 2018
Assignee:
GRUENENTHAL GMBH
Inventors:
Lutz Barnscheid, Eric Galia, Anja Geißler, Jana Pätz, Sebastian Schwier, Julia Baronsky-Probst
Abstract: The invention relates to a dosage form that is thermoshaped without being extruded and that 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 and optionally physiologically acceptable adjuvants. The invention also relates to a corresponding method for producing said dosage form.
Type:
Application
Filed:
April 27, 2018
Publication date:
August 30, 2018
Applicant:
Grünenthal Gmbh
Inventors:
Elisabeth Arkenau-Maric, Johannes Bartholomaus, Heinrich Kugelmann
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:
March 15, 2017
Date of Patent:
August 28, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elisabeth Arkenau-Maric, Johannes Bartholomaeus, Heinrich Kugelmann
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:
April 19, 2018
Publication date:
August 23, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich Kugelmann, Elisabeth Arkenau-Maric
Abstract: The invention relates to a monolithic pharmaceutical dosage form comprising a hot melt-extruded first segment (S1) and a second segment (S2); wherein the first segment (S1) contains at least a first pharmacologically active ingredient (A1) and/or the second segment (S2) contains at least a second pharmacologically active ingredient (A2); and the segment (S1) and/or the segment (S2) is tamper-resistant and/or exhibits a breaking strength of at least 300 N.
Type:
Application
Filed:
January 30, 2018
Publication date:
August 9, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
ANJA GEIßLER-FICHTNER, Klaus Wening, Lutz Barnscheid, Jana Pätz
Abstract: The invention relates to Cebranopadol or a physiologically acceptable salt thereof for use in the treatment or the prevention of pain and/or opioid drug dependence in a subject with impaired hepatic and/or renal function.
Type:
Grant
Filed:
January 22, 2016
Date of Patent:
July 17, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Elke Kleideiter, Annette Christoph, Rene Fussen, Joachim Ossig, Ramesh Boinpally
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:
Application
Filed:
February 21, 2018
Publication date:
June 28, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Lutz BARNSCHEID, Eric GALIA, Sebastian SCHWIER, Ulrike BERTRAM, Anja GEISSLER, Kornelia GRIESSMANN, Johannes BARTHOLOMÄUS
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:
January 24, 2018
Publication date:
May 31, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes Bartholomäus, Heinrich Kugelmann, Elisabeth Arkenau-Maric
Abstract: The use of tapentadol (i) in the treatment of pain in a subject suffering from depression and/or from anxiety, and/or (ii) in the treatment or the inhibition of depression or anxiety.
Type:
Grant
Filed:
March 27, 2017
Date of Patent:
May 29, 2018
Assignee:
Gruenenthal GmbH
Inventors:
Ilona Steigerwald, Ulrich Jahnel, Thomas Tzschentke
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:
September 1, 2015
Date of Patent:
March 27, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Lutz Barnscheid, Eric Galia, Sebastian Schwier, Ulrike Bertram, Anja Geissler, Kornelia Griessmann, Johannes Bartholomäus
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:
Grant
Filed:
January 12, 2017
Date of Patent:
March 27, 2018
Assignee:
GRÜNENTHAL GMBH
Inventors:
Stefan Schunk, Melanie Reich, Florian Jakob, Nils Damann, Michael Haurand, Achim Kless, Marc Rogers, Kathy Mackenzie
Abstract: The present invention relates to a compound according to general formula (I) which acts as a modulator of FPR2 and can be used in the treatment and/or prophylaxis of disorders which are at least partially mediated by FPR2.
Type:
Application
Filed:
September 20, 2017
Publication date:
March 22, 2018
Applicant:
GRÜNENTHAL GMBH
Inventors:
FLORIAN JAKOB, SONJA NORDHOFF, DAVID RIDER, MARKUS WAGENER, GREGOR BAHRENBERG, TORSTEN DUNKERN