SeaLife Pharma GmbH
SeaLife Pharma GmbH
Sealife Pharma GmbH | Date: 2017-06-07
The invention relates to a method for producing polycondensation products of guanidine, aminoguanidine or diaminoguanidine G with one or more benzyl- or allyl-derivatives BA according to the following reaction scheme: wherein X represents, respectively independently, a leaving group; each R1 represents independently either an aromatic ring system with at least one aromatic ring, which optionally contains one or more heteroatoms selected from 0, N and S and which is optionally substituted with one or two vinyl groups, to which the group(s) -CH2-X is/are bound, or represents ethylene; Gua represents a guanidindiyl-, aminoguanidindiyl- or Ddaminoguanidindiyl-group; Y represent H-Gua and Z represents H; or Y and Z together represent a chemical bond in order to produce a cyclic structure; wherein at least one benzyl- or allyl-derivative BA is subjected to a polycondensation reaction with an excess of guanidine, aminoguanidine or diaminoguanidine G with the elimination of HX.
Sealife Pharma GmbH | Date: 2015-07-30
A method for preparing polycondensation products of guanidine, aminoguanidine or diaminoguanidine G with one or more benzyl or allyl derivatives BA according to the following reaction scheme is provided: wherein X, R_(1), Gua, Y and Z are as defined in the specification. In the disclosed method, at least one benzyl or allyl derivative BA is subjected to a polycondensation reaction with excessive guanidine, aminoguanidine or diaminoguanidine G upon elimination of HX.
Agency: European Commission | Branch: H2020 | Program: MSCA-RISE | Phase: MSCA-RISE-2015 | Award Amount: 373.50K | Year: 2015
Marine organisms have the capacity to produce a variety of biologically potent natural products. Such novel molecules have new mechanisms of action and therefore could be used to treat human diseases and enhance the quality of life, especially in the ageing segment of the population. However, although there is growing interest in marine natural products (MNP) as potential therapeutic agents for human age-related diseases, few MNPs have reached clinical trials and the market. To fully exploit these promising biological resources, new strategies in the pipeline as well as a new cohort of cross-disciplinary trained scientists are needed to overcome existing bottlenecks and ensure the production of high value biomolecules. Ocean Medicines is a network of academic, research centres and SMEs across Europe, with proven experience in higher education, training and endowed with state-of-the art scientific and technical expertise and infrastructures. Our aim is to establish a network of collaboration and knowledge-exchange between industrial and academic partners to further develop lead compounds from marine microorganisms having anticancer or anti-infective effects that have already been identified by the consortium. To achieve this a secondment programme will be set up to prepare a new generation of marine biodiscovery scientists that will be trained on how to isolate compounds from bioactive bacteria/microalgae and take these through to semi-industrial scale-up for further development and toxicity testing at the pre-clinical level. The Ocean Medicines programme also considers commercialization, innovation and entrepreneurship activities including how to start a new business and how to favour an industrial career to seconded researchers. We are confident that the establishment of this international research network, with its synergistic effects, will significantly contribute to advance all of the involved labs to the top level in the field of marine drug discovery.
Agency: European Commission | Branch: FP7 | Program: CP-TP | Phase: KBBE.2012.3.2-01 | Award Amount: 13.29M | Year: 2012
The PharmaSea project focuses on obstacles in marine biodiscovery research, development and commercialization and brings together a broad interdisciplinary team of academic and industry researchers and specialists to address and overcome these. The partners are ideally placed to demonstrate how to widen the bottlenecks and increase the flow of ideas and products derived from the marine microbiome towards a greater number of successes in a larger number of application areas. Despite the tremendous potential of marine biodiscovery, exploitation, particularly at a commercial scale, has been hampered by a number of constraints. These relate to access (physical and legal), genetics of the organisms, compound isolation, structure elucidation, early reliable validation of biological activity and best mechanisms of flow-through into exploitation. PharmaSea will solve these chronic bottlenecks by developing essential actions beyond the state of the art and linking them with best practice and appropriate pragmatic approaches. The robust pipeline structure established within PharmaSea will process a wide genetic basis including marine microbial strain collections held by partners and new strain collections from extreme environments (deep, cold and hot vent habitats) to produce new products with desirable characteristics for development by the SME partners in three accessible market sectors, health (infection, inflammation, CNS diseases), personal care and nutrition. The global aim of PharmaSea is to produce two compounds at larger scale and advance them to pre-clinical evaluation. To address relevant challenges in marine biodiscovery related to policy and legal issues, PharmaSea will bring together practitioners, legal experts, policy advisors/makers and other stakeholders, focusing on the feasibility of harmonising, aligning and complementing current legal frameworks with recommendations and ready to use solutions tailored to marine biodiscovery.
Agency: European Commission | Branch: FP7 | Program: CP-TP | Phase: KBBE.2012.3.2-02 | Award Amount: 11.97M | Year: 2012
Marine microorganisms form an almost untapped resource of biotechnological potential. However, its use is hindered by the low success rate of isolation of novel microorganisms and often by poor growth efficiency. Hence, the vast majority of marine microorganisms has not been cultivated and is often considered as unculturable. MaCuMBA aims at improving the isolation rate and growth efficiency of marine microorganisms from conventional and extreme habitats, by applying innovative methods, and the use of automated high throughput procedures. The approaches include the co-cultivation of interdependent microorganisms, as well as gradient cultures and other methods mimicking the natural environment, and the exploitation of cell-to-cell communication. Signaling molecules produced by microorganisms may be necessary for stimulating growth of the same or other species, or may prevent their growth. Signaling molecules also represent an interesting and marketable product. MaCuMBA will make use of high throughput platforms such Cocagne, using gel micro-droplet technology, or MicroDish in which many thousands of cultures are grown simultaneously. Various single-cell isolation methods, such as optical tweezers, will aid the isolation of specific target cells. Isolated microorganisms as well as their genomes will be screened for a wide range of bioactive products and other properties of biotechnological interest, such as genetic transformability. Growth efficiency and expression of silent genes of selected strains will be increased also by using the clues obtained from genomic information. MaCuMBA is targeted to SMEs and industry and they make a significant part of the consortium, ensuring that the project focuses on the interests of these partners. Moreover, MaCuMBA has adopted a comprehensive and professional exploitation, dissemination, implementation, and education strategy, ensuring that MaCuMBAs results and products will be directed to end-users and stakeholders.
Debbab A.,Heinrich Heine University Düsseldorf |
Aly A.H.,Heinrich Heine University Düsseldorf |
Edrada-Ebel R.,University of Strathclyde |
Wray V.,Helmholtz Center for Infection Research |
And 4 more authors.
European Journal of Organic Chemistry | Year: 2012
Three new anthracene derivatives, which include tetrahydroanthraquinone 1 and two tetrahydroanthraquinone heterodimers 2 and 3, were isolated from Stemphylium globuliferum, together with four known metabolites 4-7. Detailed analysis of the spectroscopic data allowed the unambiguous determination of the structures of 1 and 2 and a revision of the structure of alterporriol C and its atropisomer. Furthermore, alterporriol G, previously obtained as part of a mixture, was isolated in its pure form for the first time and its structure was also revised. The absolute configurations of 1, 2 and 3 were assigned by calculation of their CD spectra, which also allowed the configurational assignment of altersolanol A and the determination of the axial chirality of alterporriols D and E. All isolated compounds were analysed for their antimicrobial and cytotoxic activities. Compounds 1 and 5 inhibited the growth of most pathogenic microorganisms tested, whereas 2, 6 and 7 showed selective inhibition of bacteria but were inactive against fungi. Three new anthracene derivatives and four known metabolites were isolated from the extract of the endophytic Stemphylium globuliferum. The structures were determined by comprehensive NMR spectroscopy and MS, and the absolute configurations by TDDFT and ZINDO methods. All isolated compounds were tested for their cytotoxic and antimicrobial activities. Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Calvillo-Barahona M.,University of Valladolid |
Cordovilla C.,University of Valladolid |
Genov M.N.,University of Valladolid |
Genov M.N.,Sealife Pharma GmbH |
And 2 more authors.
Dalton Transactions | Year: 2013
Chiral 1,2-ethylenediamines have been previously reported as active catalysts in the enantioselective addition reactions of ZnR2 to either methyl- or trifluoromethyl-ketones. Subtle changes in the molecular structure of different catalysts are described herein and lead to a dramatic effect in their catalytic activity. From these findings, we demonstrate the selective reactivity of the ligands used in the addition of ZnR2 (R = Me, Et) to methyl- and trifluoromethyl-ketones offering an enantioselective access either to chiral non-fluorinated alcohols or to chiral fluorinated tertiary alcohols. Considering the importance of the chiral trifluoromethyl carbinol fragment in several biologically active compounds, we have extended the scope of the addition reaction of ZnEt2 to several trifluoromethylketones catalyzed by (R,R)-1,2-diphenylethylenediamine derivatives. This work explores a homogeneous approach that provides excellent yields and very high ee and the use of a heterogenized tail-tied ligand affording moderate ee, high yields and allowing an easier handling and recycling. © 2013 The Royal Society of Chemistry.
Sealife Pharma GmbH | Date: 2014-01-22
Polycondensation products of aminoguanidine and/or 1,3-diaminoguanidine with one or more diamines are provided including polyguanidine derivatives of the following formula (I) or a salt thereof: wherein X is selected from NH_(2), aminoguanidino and 1,3-diaminoguanidino; Y is selected from H and R_(1)NH_(2); or X and Y together represent a chemical bond to give a cyclic structure; R_(1 )is selected from divalent organic radicals having 2 to 20 carbon atoms, in which optionally one or more carbon atoms are replaced by O or N; a and b are each 0 or 1, wherein a+b2 if no 1,3-diaminoguanidine units are included; R_(2 )is selected from H and NH_(2), wherein R_(2 )is NH_(2 )if a+b=0, R_(2 )is H or NH_(2 )if a+b=1, and R_(2 )is H if a+b=2; and n2. Production methods and uses of the polyguanidine derivatives are also provided.
Sealife Pharma Gmbh | Date: 2010-05-31
The invention relates to two novel substances, namely (1R,2S,3S,4R)-3-acetoxy-1,2,4,5-tetrahydroxy-7-methoxy-2-methyl-1,2,3,4-tetrahydroanthracene-9,10-dione (3-O-acetyl altersolanol M) and 8-(4,5,6-trihydroxy-7-methyl-2-methoxy-9,10-dioxo-9H,10H-anthracen-1-yl)-(1S,2S,3R,4S)-1,2,3,4,5-pentahydroxy-7-methoxy-2-methyl-1,2,3,4-tetrahydro-9H,10H-anthracene-9,10-dione (the atropisomers alterporriol I and J) to their use as anti-infectives and as anti-cancer agents, as well as to methods of producing the same.
Sealife Pharma Gmbh | Date: 2010-05-31
The present invention relates to the use of the following anthracene derivatives as anti-infectives, preferably against multiply drug resistant pathogens: