Abstract: Disclosed are N-(phenyl)-1H-indole-3-sulfonanmide and N-(phenyl)-1H-pyrrolo[2,3-b]pyridine-3-sulfonamide derivatives of formula I substituted at the 1- and 6-positions of the 1H-indole or 1H-pyrrolo[2,3-b]pyridine moiety, as well as structurally related compounds (e.g. the N-pyridin-2-yl and the N-pyridin-3-yl analogues thereof). The present compounds have GPR17 modulating properties which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating disorders such as multiple sclerosis.
Type:
Grant
Filed:
June 16, 2020
Date of Patent:
July 15, 2025
Assignee:
UCB Pharma GMBH
Inventors:
Cécile Pegurier, Silvia Lovera, Christa E. Mueller, Joerg Hockemeyer, Mahmoud Rashed, Ali El-Tayeb, Yong-Qiang Zhang
Abstract: Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.
Type:
Grant
Filed:
October 20, 2021
Date of Patent:
August 27, 2024
Assignee:
UCB Pharma GmbH
Inventors:
Christa E. Mueller, Cécile Pegurier, Michael Louis Robert Deligny, Ali El-Tayeb, Joerg Hockemeyer, Marie Ledecq, Joël Mercier, Laurent Provins, Nader M. Boshta, Sanjay Bhattarai, Vigneshwaran Namasivayam, Mario Funke, Lukas Schwach, Sabrina Gollos, Daniel Von Laufenberg, Anaïs Barré
Abstract: The present application relates to alkoxy-substituted pyridinyl indolsulfonamides. The compounds are negative GPR17 modulators and have utility in the treatment of various GPR17 associated disorders.
Type:
Grant
Filed:
June 19, 2019
Date of Patent:
May 7, 2024
Assignee:
UCB PHARMA GMBH
Inventors:
Cecile Pegurier, Laurent Provins, Emre M. Isin, Marie Ledecq
Abstract: The present invention relates to pyridinyl and pyrazinyl-(aza)indolsulfonamides having GPR17 modulator activity. The compounds have utility in the treatment of a variety of GPR17-associated disorders.
Type:
Grant
Filed:
June 18, 2019
Date of Patent:
March 26, 2024
Assignee:
UCB PHARMA GMBH
Inventors:
Cecile Pegurier, Laurent Provins, Alvaro Cardenas, Marie Ledecq, Christa E. Mueller, Joerg Hockemeyer, Ali El-Tayeb, Nader Boshta, Mahmoud Rashed
Abstract: Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.
Type:
Grant
Filed:
January 5, 2022
Date of Patent:
November 21, 2023
Assignee:
UCB PHARMA GMBH
Inventors:
Christa E. Mueller, Cécile Pegurier, Michael Louis Robert Deligny, Ali El-Tayeb, Joerg Hockemeyer, Marie Ledecq, Joël Mercier, Larurent Provins, Nader M. Boshta, Sanjay Bhattarai, Vigneshwaran Namasivayam, Mario Funke, Lukas Schwach, Sabrina Gollos, Daniel Von Laufenberg, Anaïs Barré
Abstract: Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.
Type:
Grant
Filed:
December 27, 2017
Date of Patent:
May 31, 2022
Assignee:
UCB Pharma GmbH
Inventors:
Christa E. Mueller, Cécile Pegurier, Michael Louis Robert Deligny, Ali El-Tayeb, Joerg Hockemeyer, Marie Ledecq, Joël Mercier, Laurent Provins, Nader M. Boshta, Sanjay Bhattarai, Vigneshwaran Namasivayam, Mario Funke, Lukas Schwach, Sabrina Gollos, Daniel Von Laufenberg, Anaïs Barré
Abstract: Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders.
Type:
Application
Filed:
December 27, 2017
Publication date:
November 14, 2019
Applicant:
UCB Pharma GmbH
Inventors:
Christa E. MUELLER, Cécile PEGURIER, Michael Louis Robert DELIGNY, Ali EL-TAYEB, Joerg HOCKEMEYER, Marie LEDECQ, Joël MERCIER, Laurent PROVINS, Nader M. BOSHTA, Sanjay BHATTARAI, Vigneshwaran NAMASIVAYAM, Mario FUNKE, Lukas SCHWACH, Sabrina GOLLOS, Daniel von LAUFENBERG, Anaïs BARRÉ
Abstract: The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a nom-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.
Type:
Application
Filed:
May 23, 2019
Publication date:
October 17, 2019
Applicants:
UCB Pharma GmbH, LTS Lohmann Therapie-Systeme AG
Inventors:
Hans-Michael WOLFF, Christoph ARTH, Luc QUERE, Walter MÜLLER
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.
Type:
Grant
Filed:
May 17, 2018
Date of Patent:
July 16, 2019
Assignees:
UCB Pharma GmbH, LTS Lohmann Therapie-Systeme AG
Inventors:
Hans-Michael Wolff, Christoph Arth, Luc Quere, Walter Müller
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.
Type:
Grant
Filed:
January 31, 2018
Date of Patent:
November 20, 2018
Assignees:
UCB Pharma GmbH, LTS Lohmann Therapie-Systeme AG
Inventors:
Hans-Michael Wolff, Christoph Arth, Luc Quere, Walter Müller
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.
Type:
Application
Filed:
May 17, 2018
Publication date:
September 20, 2018
Applicants:
UCB Pharma GmbH, LTS Lohmann Therapie-Systeme AG
Inventors:
Hans-Michael WOLFF, Christoph ARTH, Luc QUERE, Walter MÜLLER
Abstract: Transdermal therapeutic system for the transdermal administration of a systemically active agent comprising a self-adhesive layer structure, comprising A) a backing layer, and B) a dried biphasic layer, the dried biphasic layer having a) an outer phase having a composition comprising 75% to 100% of a polymer or polymer mixture, and b) an inner phase having a composition comprising at least one active agent, wherein the inner phase forms dispersed deposits in the outer phase, and c) 0.1% to 3.5% of an interface mediator with a kinematic viscosity of from 10 cSt to 100 000 cSt at 25° C., and and C) optionally an additional skin contact layer.
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.
Type:
Application
Filed:
January 31, 2018
Publication date:
May 31, 2018
Applicants:
UCB Pharma GmbH, LTS Lohmann Therapie-Systeme AG
Inventors:
Hans-Michael Wolff, Christoph Arth, Luc Quere, Walter Müller
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 present invention provides a process for the preparation of lacosamide in substantially optically pure form, which in one aspect comprises the following steps: (i) resolution of O-methyl-D,L-serine to provide O-methyl-D-serine in substantially optically pure form; (ii) acetylation of O-methyl-D-serine thereby obtained to provide the N-acetyl 10 derivative thereof in substantially optically pure form; (iii) activating the carboxy group of the compound thereby obtained; and (iv) reacting the compound thereby obtained with benzylamine.
Type:
Grant
Filed:
August 17, 2015
Date of Patent:
April 25, 2017
Assignee:
UCB Pharma GmbH
Inventors:
Alain Merschaert, Christophe Joseph Szczepaniak, Joerg Hamann, Ralf Kanzler
Abstract: Transdermal therapeutic system for the transdermal administration of rotigotine containing an therapeutically effective amount of rotigotine base in a self-adhesive layer structure, comprising A) a backing layer, and B) a rotigotine-containing biphasic layer, the bi phasic layer having a) an outer phase having a composition comprising 75% to 100% of a polymer or a polymer mixture, and b) an inner phase having a composition comprising rotigotine base, wherein the inner phase forms dispersed deposits in the outer phase, and wherein the inner phase comprises i. rotigotine base, and ii.
Abstract: Use of an additive in a transdermal therapeutic system with an active agent-containing layer in the form of a biphasic layer having a hydrophilic inner phase and a hydrophobic outer phase, wherein the inner phase comprises the additive and an active agent dissolved therein, wherein the additive has a higher affinity to water than to the active agent, for the control of the permeation rate of the active agent in a manner which is independent from its concentration in the biphasic layer, wherein the maintenance of the permeation rate is proportional to the amount of active agent in the biphasic layer.