Abstract: The invention relates to novel indole derivatives of the general formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.
Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumours and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.
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:
Grant
Filed:
September 26, 2003
Date of Patent:
February 8, 2011
Assignee:
Zentaris GmbH
Inventors:
Horst Bauer, Thomas Reissmann, Peter Romeis, Berthold Roessler
Abstract: The invention relates to the use of alkylphosphocholines in combination with antimetabolites for the treatment of multiple myeloma, colon cancer or renal cancer. Preferred alkylphosphocholines are described by the Formula II. A particularly effective treatment includes administering a combination of perifosine and capecitabine.
Type:
Application
Filed:
March 31, 2010
Publication date:
February 3, 2011
Applicant:
AEterna Zentaris GmbH
Inventors:
Jürgen Engel, Eckhard Günther, Herbert Sindermann, Babette Aicher
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:
Grant
Filed:
December 16, 2005
Date of Patent:
January 18, 2011
Assignee:
Zentaris GmbH
Inventors:
Matthias Rischer, Horst Mueller, Karl Werner, Juergen Engel
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:
September 13, 2010
Publication date:
December 30, 2010
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: 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
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
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:
Grant
Filed:
August 11, 2006
Date of Patent:
November 9, 2010
Assignees:
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: The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.
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
Abstract: The invention relates to peptides which contain N-methylated amino acid units and have improved water solubility. The invention also relates methods for treating a hormone-dependent tumor or a non-malignant indication that is treatable by LH-RH suppression, the method comprising administering to a patient in need of the treatment a therapeutically effective amount of a compound of the invention. Hormone-dependent cancers that can be treated with the methods of the invention include prostate cancer, breast cancer, ovarian cancer, endometrial cancer, and pancreatic cancer. Non-malignant indications which can be treated by the methods of the invention include benign prostate hyperplasia (BPH), endometriosis, acne, polycystic ovarian disease, dysmenorrhea, precocious puberty, and uterine fibroids and other leiomyomas.
Type:
Grant
Filed:
July 24, 2006
Date of Patent:
June 8, 2010
Assignee:
Zentaris GmbH
Inventors:
Michael Bernd, Bernhard Kutscher, Eckhard Gunther, Peter Romeis, Thomas Reissmann, Thomas Beckers
Abstract: The invention relates to pharmaceutical compositions suitable for parenteral administration comprising, peptides in the form of acetate, gluconate, glucuronate, lactate, citrate, ascorbate, benzoate or phosphate salts in dissolved or dispersed form and at least one of the acids for forming the salts in free acid form.
Type:
Grant
Filed:
May 18, 2001
Date of Patent:
May 18, 2010
Assignee:
AEterna Zentaris GmbH
Inventors:
Horst Bauer, Michael Damm, Werner Sarlikiotis
Abstract: A method for preventing aggregation of an LHRH antagonist in a pharmaceutical composition. The method comprises combining the LHRH antagonist in the form of an acetate, gluconate, glucuronate, lactate, citrate, ascorbate, benzoate or phosphate salt and at least one of the acids for forming the salts in free acid form.
Type:
Grant
Filed:
January 4, 2005
Date of Patent:
April 13, 2010
Assignee:
AEterna Zentaris GmbH
Inventors:
Horst Bauer, Michael Damm, Werner Sarlikiotis
Abstract: The invention relates to disorazoles of the general formula I, which are employed as medicaments, preferably for the treatment of oncoses, in particular in the case of pharmaceutical resistance to other active compounds and in the case of metastasizing carcinoma. The possible uses are not restricted to oncoses.
Type:
Application
Filed:
April 7, 2009
Publication date:
December 17, 2009
Applicant:
AEterna Zentaris GmbH
Inventors:
Herbert Irschik, Rolf Jansen, Florenz Sasse, Silke Baasner, Peter Schmidt, Eckhard Gunther
Abstract: The invention relates to pyrido[2,3-b]pyrazine compounds of general formulae (Ia) and (Ib), to their preparation and use, for example, for the treatment of malignant disorders and other disorders based on pathological cell proliferations.
Abstract: A novel lyophilizate and method of preparation as well as the use of the lyophilizate to treat female infertility and for gonad protection. Cetrorelix is dissolved in acetic acid 30% v/v, the solution is transferred to water and freeze dried.
Type:
Grant
Filed:
January 24, 2005
Date of Patent:
October 20, 2009
Assignee:
AEterna Zentaris GmbH
Inventors:
Jürgen Engel, Burkhard Wichert, Dieter Sauerbier, Gudrun Sauerbier, legal representative, Thomas Reissmann
Abstract: The invention provides 1,2,4-triazole compounds, compositions containing those compounds, methods of treating diseases and/or disorders with those compounds and processes of manufacturing 1,2,4-triazole compounds.
Type:
Application
Filed:
March 17, 2009
Publication date:
September 24, 2009
Applicants:
AETERNA ZENTARIS GmbH, CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE, University of Montpellier I, University of Montpellier II
Inventors:
Jean-Alain Fehrentz, Mathieu Bibian, Aline Moulin, Jean Martinez