Abstract: The invention concerns novel derivatives of 3,3-diphenyl-propylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.
Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.
Abstract: The invention relates to the use of substituted 2-aminotetralins of general formula (I) as a medicament for the preventive treatment of Parkinson's disease.
Abstract: The present invention is directed to a pharmaceutical composition comprising a Compound (a) of a class of peptide Compounds and at least one further Compound (b) for the prevention, alleviation or/and treatment of epileptic seizures.
Abstract: An embodiment of the present invention relates to a therapeutic combination including (a) lacosamide and/or a pharmaceutically acceptable salt thereof; and (b) levetiracetam and/or a pharmaceutically acceptable salt thereof. The combination can be provided in a single dosage form or separate dosage forms.
Abstract: An improved Transdermal Delivery System (TDS) comprising a backing layer inert to the components of the matrix, a self-adhesive matrix containing rotigotine and a protective foil or sheet to be removed prior to use, characterized in that the self-adhesive matrix consists of a solid or semi-solid semi-permeable polymer (1) wherein rotigotine in its free base form has been incorporated, (2) which is saturated with rotigotine and contains said rotigotine as a multitude of microreservoirs within the matrix, (3) which is highly permeable for the free base of rotigotine, (4) which is impermeable for the protonated form of rotigotine, (5) wherein the maximum diameter of the microreservoirs is less than the thickness of the matrix. is provided. Said TDS provides for enhanced flux of rotigotine across the TDS/skin interface.
Type:
Application
Filed:
April 27, 2012
Publication date:
August 23, 2012
Applicant:
UCB Pharma GmbH
Inventors:
Dietrich Wilhelm Schacht, Mike Hannay, Hans-Michael Wolff
Abstract: An improved transdermal delivery system (TDS) comprises a self-adhesive matrix comprising a solid or semi-solid semi-permeable polymer which contains rotigotine in its free base form as a multitude of microreservoirs within the matrix. The self-adhesive matrix is highly permeable to the free base of rotigotine and is impermeable to the protonated form of rotigotine.
Type:
Grant
Filed:
July 22, 2003
Date of Patent:
August 21, 2012
Assignee:
UCB Pharma GmbH
Inventors:
Dietrich Wilhelm Schacht, Mike Hannay, Hans-Michael Wolff
Abstract: An improved transdermal delivery system (TDS) comprises a self-adhesive matrix comprising a solid or semi-solid semi-permeable polymer which contains an amine-functional drug in its free base form as a multitude of microreservoirs within the matrix. The self-adhesive matrix is highly permeable to the free base of the amine-functional drug and is impermeable to the protonated form of the amine-functional drug.
Type:
Grant
Filed:
July 28, 2003
Date of Patent:
August 21, 2012
Assignee:
UCB Pharma GmbH
Inventors:
Dietrich Wilhelm Schacht, Mike Hannay, Hans-Michael Wolff
Abstract: The present invention relates to a novel polymorphic form of rotigotine characterized by at least one of the following powder X-ray diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (° 2?), measured with a Cu—K? irradiation (1.54060 ?), and a process for production thereof, which is useful for the manufacture of a stable medicament for treating or alleviating symptoms of Parkinson's disease and other dopamine-related disorders.
Abstract: This patent application relates to a transdermal therapeutic system (TTS) that comprises a Rotigotine-containing cement layer, characterized in that the cement layer contains a hot-meltable adhesive in which Rotigotine as the active substance is dispersed and partly or completely dissolved. The patent application further relates to the use of Rotigotine in the production of the cement layer of a TTS by a hot-melt method.
Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fybromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
Type:
Application
Filed:
June 24, 2010
Publication date:
April 26, 2012
Applicant:
UCB Pharma GmbH
Inventors:
J.A. Bouwstra, O.W.G.M.K. Ackaert, J. Eikelenboom, Hans-Michael Wolff
Abstract: The present application relates to a pharmaceutical granulate comprising Fesoterodine or a pharmaceutically acceptable salt or solvate thereof and a pharmaceutically acceptable stabilizer, which can be selected from the group consisting of sorbitol, xylitol, polydextrose, isomalt, dextrose, and combinations thereof, and is preferably a sugar alcohol selected from the group consisting of xylitol and sorbitol. The granulate is suitable for incorporation into pharmaceutical compositions comprising a gel matrix formed by at least one type of hydroxypropyl methylcellulose into which the Fesoterodine is embedded and, optionally, further excipients. In certain embodiments, the granulate is formed by a process of wet granulation.
Type:
Grant
Filed:
December 23, 2008
Date of Patent:
January 3, 2012
Assignee:
UCB Pharma GmbH
Inventors:
Hans-Jürgen Mika, Christoph Arth, Michael Komenda, Fatima Bicane
Abstract: The present invention concerns the use of compounds of the Formula (I) for treating different types of acute and chronic pain, especially non neuropathic inflammatory pain in mammals. The pain to be treated may be e.g. chronic inflammatory pain, rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds show an antinociceptive profile and differ from classical analgesics like opioids and non-steroidal anti-inflammatory drugs (NSAIDs) and are useful as specific analgesics.
Abstract: The invention relates to a transdermal, especially dopaminergic patch, comprising a release liner film, an active substance layer, and a carrier film, wherein the active substance layer is applied between the release liner film and the carrier film. The release liner film and/or the carrier film thereby comprise at least one separation edge brought about thermally, at least partially defining a peripheral edge of the patch. The invention further relates to a method for producing such a transdermal patch and to a tool for producing the patch according to the method according to the invention. Crystal growth in the active substance layer can be reliably prevented by the patch according to the invention.
Abstract: The present patent application relates to an alternative process for the preparation of amino derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. In a particular aspect, the present invention relates to a process of manufacture of optically enriched (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (I) comprising resolution of 2-acetamido-N-benzyl-3-methoxypropion-amide (II).
Type:
Application
Filed:
November 6, 2009
Publication date:
October 27, 2011
Applicant:
UCB PHARMA GMBH
Inventors:
Didier Bouvy, Alain Merschaert, Véronique Pinilla, Joerg Hamann, Ralf Kanzler, Antoine Thomas
Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.
Type:
Grant
Filed:
December 21, 2007
Date of Patent:
October 25, 2011
Assignee:
UCB Pharma GmbH
Inventors:
Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
Abstract: The compound of formula (I): is provided. It may be produced by subjecting a compound of formula (IV) to a reduction reaction wherein R represents hydrogen, straight or branched C1-C6 alkyl. This compound is a valuable intermediate which may be used in the synthesis of fesoterodine, tolterodine, its active metabolite, and related compounds.
Abstract: The present invention is directed to the use of a class of peptide compounds for the prophylaxis and treatment of chronic headache, particularly migraines.
Abstract: The invention relates to a compound of general formula (I) wherein A represents deuterium or hydrogen, R represents a group selected from C1-6 alkyl, C3-10 cycloalkyl or phenyl, which can be substituted by C1-3 alkoxy, fluorine, chlorine, bromine, iodine, nitro, amino, hydroxyl, oxo, mercapto or deuterium. The C atom marked with a * (star) can be present in an (R) configuration, in an (S)-configuration or a mixture thereof. The invention is characterized in that the above-mentioned compounds are free bases with a degree of purity of more than 97 wt %. The invention also relates to a method for the production of highly pure compounds of general formula (I) and to the use thereof in the production of medicaments.
Type:
Grant
Filed:
June 18, 2008
Date of Patent:
August 2, 2011
Assignee:
UCB Pharma GmbH
Inventors:
Armin Breitenbach, Claus Meese, Hans-Michael Wolff, Roland Drews