Abstract: The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors. 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:
Application
Filed:
April 23, 2015
Publication date:
October 29, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
ANTONIO NARDI, PAUL RATCLIFFE, TOBIAS CRAAN, TORSTEN HERTRAMPF, BERNHARD LESCH, ROBERT KIME, HENNING STEINHAGEN
Abstract: The invention relates to amidic oxotetrahydro-2H-furo[3.2-b]pyrrol-4(5H)-yl) derivatives as dual CatS/K inhibitors exhibiting a pronounced CatK-inhibition, 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:
Application
Filed:
April 23, 2015
Publication date:
October 29, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Antonio NARDI, Paul RATCLIFFE, Tobias CRAAN, Torsten HERTRAMPF, Bernhard LESCH, Henning STEINHAGEN
Abstract: Substituted 6-amino-nicotinamides, pharmaceutical compositions containing these compounds and also use of these compounds in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Type:
Grant
Filed:
April 18, 2012
Date of Patent:
October 27, 2015
Assignee:
GRÜNENTHAL GMBH
Inventors:
Sven Kühnert, Gregor Bahrenberg, Achim Kless, Wolfgang Schröder, Simon Lucas
Abstract: Process for preparing a powder comprising the steps of providing at least one first component in liquid form at ambient temperature, providing at least one second component having a melting point or melting range in the range from above ambient temperature to below the degradation temperature of said first component, forming a homogenous liquid mixture comprising the at least one first component and the at least one second component by stirring and heating the mixture to or keeping the mixture at a temperature in the range from above the melting point or melting range of the second component and below the degradation temperature of the first component, transferring the liquid mixture to at least one spray congealing unit, spray congealing the mixture, and isolating the powder obtained upon spray congealing.
Type:
Grant
Filed:
November 1, 2010
Date of Patent:
October 20, 2015
Assignee:
GRÜNENTHAL GMBH
Inventors:
Anne Faure, Jody Firim Marceline Voorspoels, Roel Jos M. Mertens, Filip René Irena Kiekens
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:
Application
Filed:
April 14, 2015
Publication date:
October 15, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
STEFAN SCHUNK, MELANIE REICH, FLORIAN JAKOB, NILS DAMANN, MICHAEL HAURAND, ACHIM KLESS, MARC ROGERS, KATHY SUTTON
Abstract: The invention relates to certain compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders that are, at least partially, mediated by TSPO activity.
Type:
Application
Filed:
October 11, 2013
Publication date:
October 15, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Petra Bloms-Funke, Gregor Bahrenberg, Wolfgang Schröder, Sven Kühnert, Simon Lucas
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:
Application
Filed:
April 14, 2015
Publication date:
October 15, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
STEFAN SCHUNK, MELANIE REICH, FLORIAN JAKOB, RENÉ MICHAEL KOENIGS, NILS DAMANN, MICHAEL HAURAND, MARC ROGERS, KATHY SUTTON, RICHARD HAMLYN
Abstract: The invention relates to a dosage form comprising a physiologically effective amount of a physiologically active substance (A), a synthetic, semi-synthetic or natural polymer (C), optionally one or more physiologically acceptable auxiliary substances (B) and optionally a synthetic, semi-synthetic or natural wax (D), wherein the dosage form exhibits a resistance to crushing of at least 400 N and wherein under physiological conditions the release of the physiologically active substance (A) from the dosage form is at least partially delayed.
Type:
Application
Filed:
June 25, 2015
Publication date:
October 15, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMÄUS, Heinrich KUGELMANN
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:
Application
Filed:
June 22, 2015
Publication date:
October 8, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth ARKENAU-MARIC, Johannes BARTHOLOMÄUS
Abstract: The invention relates to a pharmaceutical dosage form having a breaking strength of at least 300 N and comprising a pharmacologically active compound, an anionic polymer bearing carboxylic groups, wherein the content of the anionic polymer is ?20 wt.-%, based on the total weight of the pharmaceutical dosage form, and a nonionic surfactant.
Type:
Application
Filed:
March 3, 2015
Publication date:
August 27, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Lutz BARNSCHEID, Jessica REDMER, Sebastian SCHWIER
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 14, 2015
Publication date:
August 6, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Johannes BARTHOLOMÄUS, Heinrich KUGELMANN, Elisabeth ARKENAU-MARIC
Abstract: The present invention relates to a process for the production of abuse-proofed, thermoformed dosage forms 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 with a breaking strength of at least 500 N.
Type:
Application
Filed:
December 23, 2014
Publication date:
June 18, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
ELISABETH ARKENAU-MARIC, JOHANNES BARTHOLOMÄUS
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:
December 15, 2014
Publication date:
June 18, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
ANJA GEISSLER, KLAUS WENING, LUTZ BARNSCHEID, JANA PÄTZ
Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to methods of using these compounds for the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.
Type:
Application
Filed:
December 18, 2014
Publication date:
June 18, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
FELIX VOSS, SONJA NORDHOFF, SEBASTIAN WACHTEN, ANDRÉ WELBERS, STEFANIE RITTER
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:
February 10, 2015
Publication date:
June 4, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Elisabeth Arkenau-Maric, Johannes Bartholomäus, Heinrich Kugelmann
Abstract: Crystalline, anhydrous hydrochloride salts of 4,5?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one (oxymorphone) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a method for the production of such salts, a pharmaceutical composition comprising an effective amount of such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.
Type:
Application
Filed:
February 4, 2015
Publication date:
May 28, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
Andreas FISCHER, Dagmar Peters-Groth, Dagmar Lischke
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:
Application
Filed:
December 9, 2014
Publication date:
April 2, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
ELISABETH ARKENAU-MARIC, JOHANNES BARTHOLOMÄUS
Abstract: Crystalline, anhydrous hydrochloride salts of 4,5?-epoxy-3,14-dihydroxy-17-methylmorphinan-6-one (oxymorphone) are disclosed and three polymorphic forms of these salts are reported. The invention further relates to a method for the production of such salts, a pharmaceutical composition comprising an effective amount of such a salt and such a salt as a medicament and for the treatment and/or prevention of pain.
Type:
Grant
Filed:
November 27, 2013
Date of Patent:
March 3, 2015
Assignee:
Grünenthal GmbH
Inventors:
Andreas Fischer, Dagmar Peters-Groth, 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:
October 30, 2014
Publication date:
February 26, 2015
Applicant:
GRÜNENTHAL GMBH
Inventors:
JOHANNES BARTHOLOMAEUS, HEINRICH KUGELMANN
Abstract: The present invention relates to a device for cutting a strand to a length with regard to a weight and to the use of such device in a method for producing a medicament dosage form of at least one piece composed of 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 using the device.
Type:
Grant
Filed:
November 30, 2009
Date of Patent:
January 27, 2015
Assignee:
Grünenthal GmbH
Inventors:
Elisabeth Arkenau-Maric, Johannes Bartholomäus, Dieter Schateikis, Kai-Uwe Ustorf