Abstract: The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds in hydrophilic or lipophilic form, which are useful as angiotensin II ATI receptor antagonists suitable for transdermal delivery. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases.
Type:
Grant
Filed:
May 23, 2008
Date of Patent:
October 22, 2013
Assignee:
Eldrug S.A.
Inventors:
John Matsoukas, Michael Maragoudakis, Dimitrios Vlaxakos
Abstract: A first aspect of the invention relates to a conjugate comprising: (i) mannan; and (ii) at least one epitope comprising a peptide fragment of a protein selected from myelin basic protein (MBP), myelin oligodentrocyte glycoprotein (MOG) and proteolipid protein (PLP), said peptide fragment being in linear or cyclic form; wherein said epitope is linked to mannan via a [(LyS-GIy)n] bridge, where n is an integer from 1 to 10. Further aspects of the invention relate to pharmaceutical compositions comprising said conjugates, and their use in the preparation of a medicament for treating an immune disorder.
Type:
Application
Filed:
January 22, 2009
Publication date:
October 6, 2011
Applicant:
Eldrug S.A.
Inventors:
John Matsoukas, Theodoros Tselios, Vasso Apostolopoulos, Vivian Tseveleki, Maria Katsara, Lesley Probert
Abstract: One aspect of the invention relates to a peptide comprising the amino acid sequence of formula (I), ENPVVHFFK91NIVTP96RTP?(I)? (SEQ?ID?NO:?3) wherein at least one of K91 and P96 is substituted by a natural or unnatural amino acid, wherein said peptide is in linear or cyclic form. Another aspect of the invention relates to a peptide comprising the amino acid sequence of formula (Ia), ENPVVHFFK91NIVT96RTP?(Ia), (SEQ?ID?NO:?4) wherein each of K91 and P96 is substituted by a natural or unnatural amino acid. Another aspect of the invention relates to a peptide comprising the amino acid sequence of formula (Ib), ENPVVHFFK91NIVT96RTP?(Ib) (SEQ?ID?NO:?5) wherein at least one of K91 and P96 is substituted by an amino acid selected from R, E, F and Y.
Type:
Application
Filed:
November 20, 2008
Publication date:
June 16, 2011
Applicant:
Eldrug S.A.
Inventors:
John Matsoukas, Vasso Apostolopoulos, Theodoros Tselios, Maria Katsara, George Deraos, Nikos Grigoriadis, Athanasios Lourbopoulos
Abstract: The present invention provides novel 1,5 and 1,3,5-substituted imidazole compounds of formulas (I), (IIa), (IIIb) in hydrophilic or lipophilic form, which are useful as angiotensin II AT1 receptor antagonists with sympathetic suppressant properties. In particular, the invention provides pharmaceutical compositions containing the pharmacophoric groups of Losartan and Clonidine as well compounds, processes and intermediates for preparing compounds and their use in methods of treating hypertension and cardiovascular diseases through Renin Angiotensin System (RAS) and Sympathetic System (SS). Alkylated histamine based double action Saltans are lipophilic and can act transdermally.
Type:
Application
Filed:
July 25, 2008
Publication date:
August 26, 2010
Applicant:
Eldrug S.A.
Inventors:
John Matsoukas, Charalambos Gavras, Dimitrios Vlaxakos, Michael Maragoudakis