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:
Grant
Filed:
March 31, 2010
Date of Patent:
February 26, 2013
Assignee:
AEterna Zentaris GmbH
Inventors:
Jürgen Engel, Eckhard Günther, Herbert Sindermann, Babette Aicher
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: 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: 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: The invention relates to pyrido[2,3-b]pyrazines 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 invention relates to pyrido[2,3-b]pyrazine compounds of formulae (Ia) and (Ib) which have activity to the modulation of misdirected cellular signal transduction processes such as tyrosine kinases, serine/threonine kinases and/or lipid kinases, their preparation and use as medicaments, especially for the treatment of malignant disorders and other disorders based on pathological cell proliferations:
Abstract: A method of assessing growth hormone deficiency in a human or animal subject, the method comprising administering orally to the subject EP 1572 (Formula I) or EP 1573 (Formula II), obtaining a post-administration sample from the subject, determining the level of growth hormone in the sample and assessing whether the level of growth hormone in the sample is indicative of growth hormone deficiency in the subject. Preferably, the GH level in the sample is measured by immunoassay. Also disclosed is a kit of parts constituting a diagnostic kit comprising: (a) EP 1572 or EP 1573 formulated for oral administration; and (b) means for determining the level of growth hormone in a sample.
Abstract: The invention relates to novel pyrido[2,3-b]pyrazine derivatives of the general Formula I, their preparation and use as medicaments, in particular for the treatment of malignant and other disorders based on pathological cell proliferations.
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
Abstract: A method of treating infertility disorders by 1) administering an LH-RH antagonist, preferably Cetrorelix, in amounts to selectively suppress endogenous LH but not FSH secretion and 2) inducing follicle growth by administration of exogenous gonadotropin. The selective suppression OF LH allows FSH secretion to be at natural level S thereby not affecting individual estrogen development. The LH-RH antagonist can be given as a single or dual subcutaneous dose in the range of 1 mg to 10 mg, preferably 2 mg-6 mg. In multiple dosing posology, LH-RH antagonist can be administered subcutaneously in an amount in the range of 0.1 to 0.5 mg of LH-RH antagonist/day . LH-RH antagonist is applied starting cycle day 1 to 10, preferably on day 4 to 8, and ovulation can be induced between day 9 and 20 of the menstruation cycle by administering rec. LH, native LH-RH, LH-RH agonist or by HCG. In addition rec.
Type:
Application
Filed:
November 8, 2010
Publication date:
December 15, 2011
Applicant:
Zentaris GmbH
Inventors:
PHILIPPE BOUCHARD, Rene Frydman, Paul Devroey, Klaus Diedrich, Jürgen Engel
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
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 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 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:
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 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