Abstract: The present invention provides novel triazole derivatives 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. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).
Type:
Application
Filed:
August 11, 2006
Publication date:
September 6, 2007
Applicants:
ZENTARIS GmbH, Le Centre National De La Recherche Scientifique
Inventors:
Daniel PERRISSOUD, Jean MARTINEZ, Aline MOULIN, Jean-Alain FEHRENTZ, Damien BOEGLIN, Luc DEMANGE
Abstract: The present invention provides novel alkyl phospholipid derivatives with reduced cytotoxicity that are useful for treating various diseases and/or pathophysiological conditions in mammals, preferably humans, that are caused by microorganisms, in particular bacteria, fungi, protozoa and/or viruses. Such alkyl phospholipids can be employed as single drugs or in the course of combination therapies and can also be used for the treatment of tumors.
Type:
Application
Filed:
December 19, 2006
Publication date:
July 19, 2007
Applicant:
ZENTARIS GmbH
Inventors:
Daniel PERRISSOUD, Mathias Pietras, Juergen Engel
Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general formulae (I) and (II), and to their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.
Abstract: An aqueous injectable soution of an LHRH antagonist, such as Cetrorelix, in an organic, pharmaceutically acceptable acid, such as gluconic acid.
Type:
Grant
Filed:
October 23, 2002
Date of Patent:
May 8, 2007
Assignee:
Zentaris GmbH
Inventors:
Werner Sarlikiotis, Horst Bauer, Matthias Rischer, Jürgen Engel, Frank Güthlein, Dominique Di Stefano
Abstract: The invention relates to novel N-substituted indolyl-3-glyoxylamides of the general formula I, their preparation and use as medicaments, in particular for the treatment of tumors
Abstract: The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.
Type:
Grant
Filed:
June 2, 2004
Date of Patent:
April 17, 2007
Assignee:
Zentaris GmbH
Inventors:
Matthias Gerlach, Tilmann Schuster, Peter Ernig, Peter Schmidt, Silke Baasner, Eckhard Günther
Abstract: The present invention provides novel triazole derivatives 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. The present invention further provides GHS receptor antagonists and agonists that can be used for modulation of these receptors and are useful for treating above conditions, in particular growth retardation, cachexia, short-, medium- and/or long term regulation of energy balance; short-, medium- and/or long term regulation (stimulation and/or inhibition) of food intake; adipogenesis, adiposity and/or obesity; body weight gain and/or reduction; diabetes, diabetes type I, diabetes type II, tumor cell proliferation; inflammation, inflammatory effects, gastric postoperative ileus, postoperative ileus and/or gastrectomy (ghrelin replacement therapy).
Type:
Application
Filed:
August 11, 2006
Publication date:
February 15, 2007
Applicants:
ZENTARIS GmbH, Le Centre National De La Recherche Scientifique, University of Montpellier I, University of Montpellier II
Inventors:
Daniel Perrissoud, Jean Martinez, Aline Moulin, Jean-Alain Fehrentz, Damien Boeglin, Luc Demange
Abstract: Compounds inhibiting phosphatidylinositol 3-kinase (PI 3-K) activities and methods of preparing and using thereof in treating diseases are disclosed. Compounds inhibiting PI 3-K activity and methods of using PI 3-K inhibitory compounds to inhibit cancer cell grwoth or to treat disorders of immunity and inflammation, in which PI 3-K plays a role in leukocyte function are also provided.
Type:
Application
Filed:
June 14, 2004
Publication date:
January 11, 2007
Applicant:
ZENTARIS GmbH
Inventors:
Beth Drees, Leena Chakravarty, Glenn Prestwich, Gyorgy Dorman, Mariann Kavecz, Andras Lukacs, Laszlo Urge, Ferenc Darvas, Piotr Rzepecki, Colin Ferguson
Abstract: The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. Medicaments in which the peptides according to the invention are contained can be used for the treatment of hormone-dependent tumors and hormone-influenced non-malignant disorders.
Type:
Grant
Filed:
September 29, 2003
Date of Patent:
December 12, 2006
Assignee:
Zentaris GmbH
Inventors:
Michael Bernd, Bernhard Kutscher, Eckhard Gunther, Peter Romeis, Thomas Reissmann, Thomas Beckers
Abstract: The invention relates to the use of a cell, which is charged with a micro-organism that contains foreign DNA, in particular a bacterial micro-organism, to produce a pharmaceutical composition. Preferably, the foreign DNA codes for a defined active agent and the pharmaceutical composition is designed for use in the prophylaxis or treatment of a disease that can be treated with said active agent.
Type:
Application
Filed:
June 7, 2004
Publication date:
October 26, 2006
Applicant:
ZENTARIS GmbH
Inventors:
Joachim Fensterle, Werner Goebel, Ulf Rapp, Jochen Stritzker, Andreas Schmidt, Ivatlo Gentschev, Tamara Potapenko
Abstract: The invention relates to novel, water-soluble porphyrin platinum compounds of the tetraarylporphyrin platinum derivatives type or of the hematoporphyrin platinum derivatives type with high tumor selectivity and their use for the treatment of benign and malignant tumor diseases. In particular, the compounds are suitable for photodynamic anti-tumor therapy.
Type:
Grant
Filed:
January 27, 2003
Date of Patent:
August 8, 2006
Assignee:
Zentaris GmbH
Inventors:
Karl Christian Bart, Guenther Bernhardt, Henri Brunner, Christian Lottner
Abstract: The invention concerns the use of a bombesin/gastrin releasing peptide antagonist in the treatment of inflammatory and immune-mediated inflammatory conditions, in particular sepsis, acute lung injury and rheumatoid arthritis as well as for the treatment or prophylaxis of brain disorders, preferably bipolar disorder, and in particular the different forms and/or subforms of bipolar disorder, such as mania, acute mania, severe mania, hypomania, depression, moderate depression, dysthymia, severe depression, episodes of mania and/or depression, psychosis/psychotic symptoms (e.g. hallucinations, delusions), mixed bipolar state, bipolar I disorder, bipolar II disorder and/or rapid-cycling bipolar disorder. In particular, specific nonapeptides with antagonist properties against bombesin or bombesin-like peptides, such as the gastrin releasing peptide, may be used in the treatment of inflammatory and immune-mediated inflammatory conditions as well as brain disorders.
Type:
Application
Filed:
December 13, 2005
Publication date:
July 20, 2006
Applicant:
ZENTARIS GmbH
Inventors:
Gilberto Schwartsmann, Rafael Roesler, Felipe Dal Pizzol, Joao Quevedo, Flavio Kapczinski
Abstract: The present invention provides a novel process for producing sterile suspensions of slightly soluble basic peptide complexes. The present invention further provides a novel process for producing sterile lyophilizates of slightly soluble basic peptide complexes. In addition, a novel process for producing sterile suspensions suitable for the parenteral administration of slightly soluble basic peptide complexes is provided. The invention moreover provides sterile suspensions and sterile lyophilizates of slightly soluble basic peptide complexes, and pharmaceutical formulations comprising them. The provided sterile suspensions, sterile lyophilizates and pharmaceutical formulations comprising them are particularly suitable for use in a parenteral dosage form as medicaments for the treatment and prophylaxis of diseases and pathological states in mammals, especially in humans.
Type:
Application
Filed:
December 16, 2005
Publication date:
June 22, 2006
Applicant:
ZENTARIS GmbH
Inventors:
Matthias Rischer, Horst Mueller, Karl Werner, Juergen Engel
Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
Type:
Grant
Filed:
November 14, 2003
Date of Patent:
June 6, 2006
Assignee:
Zentaris GmbH
Inventors:
Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
Type:
Grant
Filed:
April 14, 2005
Date of Patent:
April 11, 2006
Assignee:
Zentaris GmbH
Inventors:
Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
Abstract: The present inventions provides a method for therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction by short term induction treatment with an LH-RH antagonist for 4 to 12 weeks. According to another aspect of the present invention, the short term LH-RH treatment is followed by the combined or separate administration of one or more active agents selected from the group consisting of a contraceptive, preferably an oral contraceptive, a non-steroidal anti-rheumatic agent, an analgetic, an androgen other than a 17-alpha-alkyl substituted testosterone or any combinations thereof.
Type:
Grant
Filed:
September 20, 2000
Date of Patent:
February 28, 2006
Assignee:
Zentaris GmbH
Inventors:
Hilde Riethmuller-Winzen, Jurgen Engel, Ricardo Felberbaum, Klaus Diedrich, Wolfgang Küpker
Abstract: The invention relates to pharmaceutical administration forms with sustained release comprising at least one pharmacologically active peptide. The invention also relates to a method for the production thereof, a kit comprising a lyophilised peptide and an aqueous solution of an inorganic salt or acetic acid salt and the use of an aqueous solution of an inorganic or acetic acid salt for producing a pharmaceutical administration form which releases peptides in a continuous manner over a long period of time.
Type:
Application
Filed:
September 26, 2003
Publication date:
December 22, 2005
Applicant:
ZENTARIS GmbH
Inventors:
Horst Bauer, Thomas Reissmann, Peter Romeis, Berthold Roessler
Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
Type:
Grant
Filed:
December 19, 2003
Date of Patent:
August 30, 2005
Assignee:
Zentaris GmbH
Inventors:
Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
Abstract: A method of treating protozoal and fungal diseases is described, in which an effective amount of a compound of formula I is administered to a host having a protozoal or fungal disease.
Type:
Grant
Filed:
November 8, 2002
Date of Patent:
June 7, 2005
Assignee:
Zentaris GmbH
Inventors:
Gerhard Nossner, Bernhard Kutscher, Jurgen Engel, Wolfgang Schumacher, Margrit Stekar, Peter Hilgard, Jurij Stekar