Patents by Inventor Klaus Paulini

Klaus Paulini has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors
    Patent number: 8546435
    Abstract: The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: October 1, 2013
    Assignees: AEterna Zentaris GmbH, Centre National de la Recherche Scientifique, University of Montpellier I, University of Montpellier II
    Inventors: Babette Aicher, Gilbert Mueller, Klaus Paulini, Lars Blumenstein, Peter Schmidt, Matthias Gerlach, Michael Teifel, Jean Martinez, Jean-Alain Fehrentz, Anne-Laure Blayo
  • Tetrahydrocarbazole derivatives as ligands of G-protein coupled receptors
    Patent number: 8541462
    Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: September 24, 2013
    Assignee: AEterna Zentaris GmbH
    Inventors: Tilmann Schuster, Klaus Paulini, Peter Schmidt, Silke Baasner, Emmanuel Polymeropoulos, Eckhard Guenther, Michael Teifel
  • Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
    Patent number: 8470776
    Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
    Type: Grant
    Filed: March 19, 2010
    Date of Patent: June 25, 2013
    Assignee: Aeterna Zentaris GmbH
    Inventors: Eckhard Guenther, Olaf Schaefer, Michael Teifel, Klaus Paulini
  • NOVEL TETRAHYDROCARBAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS
    Publication number: 20120122763
    Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
    Type: Application
    Filed: January 25, 2012
    Publication date: May 17, 2012
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Tilmann SCHUSTER, Klaus Paulini, Peter Schmidt, Silke Baasner, Emmanuel Polymeropoulos, Eckhard Guenther, Michael Teifel
  • NOVEL TRIAZOLE DERIVATIVES WITH IMPROVED RECEPTOR ACTIVITY AND BIOAVAILABILITY PROPERTIES AS GHRELIN ANTAGONISTS OF GROWTH HORMONE SECRETAGOGUE RECEPTORS
    Publication number: 20120083494
    Abstract: The present invention provides novel triazole derivatives with improved receptor activity and bioavailability properties as ghrelin analogue ligands of growth hormone secretagogue receptors according to formula (I) that are useful in the treatment or prophylaxis of physiological and/or pathophysiological conditions in mammals, preferably humans, that are mediated by GHS receptors.
    Type: Application
    Filed: September 16, 2011
    Publication date: April 5, 2012
    Applicants: AETERNA ZENTARIS GmbH, University of Montpellier Il, University of Montpellier I, Centre National De La Recherche Scient.
    Inventors: Babette Aicher, Gilbert Mueller, Klaus Paulini, Lars Blumenstein, Peter Schmidt, Matthias Gerlach, Michael Teifel, Jean Martinez, Jean-Alain Fehrentz, Anne-Laure Blayo
  • Tetrahydrocarbazole derivatives as ligands of G-protein coupled receptors
    Patent number: 8148546
    Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
    Type: Grant
    Filed: April 25, 2008
    Date of Patent: April 3, 2012
    Assignee: AEterna Zentaris GmbH
    Inventors: Tilmann Schuster, Klaus Paulini, Peter Schmidt, Silke Baasner, Emmanuel Polymeropoulos, Eckhard Guenther, Michael Teifel
  • Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs)
    Patent number: 8067456
    Abstract: The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
    Type: Grant
    Filed: February 14, 2008
    Date of Patent: November 29, 2011
    Assignee: AEterna Zentaris GmbH
    Inventors: Klaus Paulini, Matthias Gerlach, Eckhard Gunther, Emmanuel Polymeropoulos, Silke Baasner, Peter Schmidt, Ronald Kühne, Arvid Söderhäll
  • CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF
    Publication number: 20100323963
    Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
    Type: Application
    Filed: March 19, 2010
    Publication date: December 23, 2010
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Eckhard GUENTHER, Olaf Schaefer, Michael Teifel, Klaus Paulini
  • CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF
    Publication number: 20100317580
    Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
    Type: Application
    Filed: March 19, 2010
    Publication date: December 16, 2010
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Eckhard GUENTHER, Olaf Schaefer, Michael Teifel, Klaus Paulini
  • Conjugates of disorazoles and their derivatives with cell-binding molecules, novel disorazole derivatives, processes of manufacturing and uses thereof
    Patent number: 7741277
    Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
    Type: Grant
    Filed: September 6, 2007
    Date of Patent: June 22, 2010
    Assignee: Aeterna Zentaris GmbH
    Inventors: Eckhard Guenther, Olaf Schaefer, Michael Teifel, Klaus Paulini
  • NOVEL TETRAHYDROCARBAZOLE DERIVATIVES AS LIGANDS OF G-PROTEIN COUPLED RECEPTORS
    Publication number: 20090170783
    Abstract: The present invention provides novel tetrahydrocarbazole compounds according to formula (I) as ligands of G-protein coupled receptors (GPCR) which are useful in the treatment and/or prophylaxis of physiological and/or pathological conditions in mammals mediated by GPCR or of physiological and/or pathological conditions which can be treated by modulation of these receptors.
    Type: Application
    Filed: April 25, 2008
    Publication date: July 2, 2009
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Tilmann Schuster, Klaus Paulini, Peter Schmidt, Silke Baasner, Emmanuel Polymeropoulos, Eckhard Guenther, Michael Teifel
  • Novel tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCPs)
    Publication number: 20080280965
    Abstract: The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
    Type: Application
    Filed: February 14, 2008
    Publication date: November 13, 2008
    Inventors: Klaus Paulini, Matthias Gerlach, Eckhard Gunther, Emmanuel Polymeropoulos, Silke Baasner, Peter Schmidt, Ronald Kuhne, Arvid Soderhall
  • Tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs)
    Patent number: 7375127
    Abstract: The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
    Type: Grant
    Filed: June 30, 2005
    Date of Patent: May 20, 2008
    Assignee: AE Zentaris GmbH
    Inventors: Klaus Paulini, Matthias Gerlach, Eckhard Günther, Emmanuel Polymeropoulos, Silke Baasner, Peter Schmidt, Ronald Kühne, Arvid Söderhäll
  • CONJUGATES OF DISORAZOLES AND THEIR DERIVATIVES WITH CELL-BINDING MOLECULES, NOVEL DISORAZOLE DERIVATIVES, PROCESSES OF MANUFACTURING AND USES THEREOF
    Publication number: 20080090758
    Abstract: The present invention provides conjugates of disorazoles and their derivatives with cell-binding molecules, such as peptides, proteins, hormones, blood proteins and antibodies. The present invention further provides novel disorazole derivatives and processes of manufacturing such conjugates and disorazole derivatives. These compounds can be used as medicaments for the treatment of physiological and/or pathophysiological conditions in mammals, in particular for the treatment of various tumors.
    Type: Application
    Filed: September 6, 2007
    Publication date: April 17, 2008
    Applicant: AETERNA ZENTARIS GmbH
    Inventors: Eckhard Guenther, Olaf Schaefer, Michael Teifel, Klaus Paulini
  • Tetrahydrocarbazol derivatives as ligands for G-protein-coupled receptors (GPCR)
    Patent number: 7122570
    Abstract: This invention provides new tetrahydrocarbazole derivatives that act as ligands for G-protein-coupled receptors (GPCR), especially as antagonists of the gonadotropin-releasing hormone (GnRH). A pharmaceutical composition that contains these new tetrahydrocarbazole derivatives as well as a process for the production of the new tetrahydrocarbazole derivatives are also provided. Moreover, this invention relates to the administration of tetrahydrocarbazole derivatives for treating pathologic conditions that are mediated by GPCR, especially for inhibiting GnRH, in mammals, especially humans, who require such an administration, as well as the use of tetrahydrocarbazole derivatives for the production of a pharmaceutical agent for treating GPCR-mediated pathologic conditions, especially for inhibiting GnRH.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: October 17, 2006
    Assignee: Zentaris AG
    Inventors: Marcus Karl Koppitz, Hans Peter Muhn, Kenneth Jay Shaw, Holger Hess-Stump, Klaus Paulini
  • Novel tetrahydrocarbazole derivatives having improved biological action and improved solubility as ligands of G-protein coupled receptors (GPCRs)
    Publication number: 20060014818
    Abstract: The present invention provides novel tetrahydrocarbazole derivatives which have improved properties and which can be employed as inhibitors of GPCRs. This results in the possibility of using the novel compounds to treat pathological conditions whose severity depends on the pathobiochemical effect of GPCRs. The compounds of the invention act in particular via an antagonistic inhibition of the LHRH receptor. The invention further provides medicaments which comprise one or more of the novel compounds as active ingredient. The medicaments are suitable in particular to be employed in an oral dosage form for a mammal, in particular a human.
    Type: Application
    Filed: June 30, 2005
    Publication date: January 19, 2006
    Inventors: Klaus Paulini, Matthias Gerlach, Eckhard Günther, Emmanuel Polymeropoulos, Silke Baasner, Peter Schmidt, Ronald Kühne, Arvid Soderhall
  • Acridine derivatives and their use as medicaments
    Publication number: 20050009809
    Abstract: The invention relates to novel acridine derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for the treatment of tumors.
    Type: Application
    Filed: June 29, 2004
    Publication date: January 13, 2005
    Inventors: Matthias Gerlach, Peter Emig, Klaus Paulini, Michael Czech, Tilman Schuster, Eckhard Gunther