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Bisphosphonates as Potential Drug Candidates for Inflammatory Lung Diseases


15.02.2012
| Ref.Nr. 09061
Life Science › Pharma&Biotech

Biphosphonate with a prolonged carbon chain.Recent findings in animal models underline the potential role of the acid sphingomyelinase (aSMase) as an important drug target in inflammatory lung diseases like acute lung injury (ALI) - the main cause of death in intensive care units -, acute respiratory distress syndrome (ARDS), lung emphysema, and cystic fibrosis.

The invention offers simple geminal bisphosphonates with a prolonged carbon chain as potent and selective inhibitors of the acid sphingomyelinase. The compounds can be synthesized in a one-step or two-step procedure and show clear inhibition of cell death in vitro. First ex vivo data in rats show a reduction of platelet activating factor (PAF) – induced pulmonary edema in the presence of the bisphosphonates by at least 50 percent. Aerosols of bisphosphonates may be possible applicants for the treatment of pulmonary diseases.

Besides their use in inflammatory lung diseases the bisphosphonates with prolonged carbon chain may be used as a treatment option for cystic fibrosis and atherosclerosis.


IP Rights
EP Application (08/2009).
PCT Application (08/2010).
A PCT application was filed in August 2010.

Patent Owner
Humboldt-Universität zu Berlin
Rheinisch-Westfälische
Technische Hochschule Aachen (RWTH)

Application Area:
Drug candidates for the treatment of inflammatory lung diseases, cystic fibrosis and atherosclerosis.
Development Stage: Ex vivo
Bild des Benutzers Dr. Bettina Büttner
Licensing Manager: Dr. Bettina Büttner
T +49 30 2125 4835
F +49 30 2125 4822
Suitable Industry: Pharmaceuticals
Benefits:
  • Neutral sphingomyelinase is not influenced
  • First ex-vivo data in a PAF-induced edema rat model showed clear edema reduction by 50percent
  • Inhibition of dexamethasone induced apoptosis was proven in vitro
  • Substances can easily be synthesized in a one-step or two-step procedure
  • Prolongation from 6 to 8 C-atoms shows 40times higher inhibition rate

 

C3bot Peptides as Drugs for the Treatment of Traumatic or Degenerative Neuronal Injury


21.12.2011
| Ref.Nr. 08167
Life Science › Pharma&Biotech

Figure : Neurocyte Picture: Höltje et al. 2009Background
Peptide fragments of the C3 exoenzyme of Clostridium botulinum have been found to have neuritogenic effects on neurons as well as regenerative proper-ties in an animal model (mouse). The peptides represent promising drug candidates for the treatment of neurodegenerative disorders such as Morbus Alzheimer, Parkinson, Huntington chorea but also for spinal cord injury and traumatic brain injury.enic effects on neurons as well as regenerative properties in an animal model (mouse).

Technology
We offer neuron-specific short peptides for the treatment of neurodegene-rative disorders. Whereas a 26mer peptide stimulates both, dendritic and axonal growth, a 15mer peptide selectively promotes axonal growth. Both, the 15mer and the 26mer peptide trigger a strong transient activation of RhoA which mimics the physiological conditions of RhoA activation / inactivation cycles.
These properties make the peptides suitable for repeated administration and long term treatments. As the peptides only act on neurons and not on microglia or astrocytes, there is no risk for neuronal inflammation or glia scar formation.

 

IP Rights
PCT application in 2010
National applications in USA/Europe in 2011

Patent Owner
Charité – Universitätsmedizin Berlin
Hannover Medical School

Application Area:
Drug candidates for the treatment of neurodegenerative disorders
Development Stage: In vitro / in vivo
Weitere Kategorien: Life Science, Pharma & Biotech
Bild des Benutzers Dr. Janin Hofmann
Licensing Manager: Dr. Janin Hofmann
T +49 30 2125 4828
F +49 30 2125 4822
Benefits:
  • Physiological acting neuritogenic drug – small size and effective in nanomolar concentrations
  • Act neuron-specific -> reduced risk for neuronal inflammation or glia scar formation
  • Short peptides with low antigenicity and good kinetics
  • Broad application areas: Spinal cord injury, traumatic brain injury, Morbus Alzheimer, Parkinson, Huntington Chorea, etc.
  • In vivo data on spinal cord injury model show regenerative properties

Cytokinin Receptor Antagonists and Compositions Containing these Derivatives


08.12.2011
| Ref.Nr. 07114
Life Science › Nutrition

Generel formular of alylbenzylamino Picture: WO 2009/043320 A2 Background
Cytokinins are plant hormones involved in cell division, shoot meristem and leaf formation, chloroplast biogenesis, and senescence. The development of agonists and antagonists with a particular physiological effect is useful in mechanism-of-action studies of biologically active natural products. The potent naturally occurring cytokinin N6-isopentenyladenine served as the basis for initial structure-activity studies.

Technology
We offer substituted 6-(alkylbenzylamino)-purin derivatives as cytokinin receptor antagonists to provide cytokinin analogons for growth regulation in plants and to offer the possibility for a specific selectivity for cytokinin receptors without being toxic for animal cells. The derivatives can be used to influence morphology, leading to:
  • Increased root growth, fruit or grain size
  • Stimulation of root branching and enhanced number of lateral roots
  • Accelerated seed germination
  • Enhanced yield and quality of crops

 
IP Rights
Czech Patent Application was filed in 2007
PCT Patent Application was filed in 2008
National applications filed in USA and Europe

Patent Owner

  • Freie Universität Berlin
  • Palacky University Olomouc (CZ)
Application Area:
Applicable as plant growth regulator
Development Stage: Green house (plant model Arabidopsis thaliana)
Weitere Kategorien: Life Science, Nutrition
Bild des Benutzers Dr. Bettina Büttner
Licensing Manager: Dr. Bettina Büttner
T +49 30 2125 4835
F +49 30 2125 4822
Suitable Industry: Agriculture industry
Benefits:
  • Non toxic for animal cells
  • Efficiency is proven in various test systems
  • Suitable regulator for proliferation and morphogenesis in tissue culture

Novel Screening Method for Agents suitable for Therapy of Alzheimer´s Disease


28.10.2011
| Ref.Nr. 07081
Life Science › Pharma&Biotech

Technology
We offer a screening method that allows the detection of novel drug candidates for the prophylaxis and causative therapy of Alzheimer’s Disease.

The identified drugs influence the substrat-enzyme interaction between amyloid precursor protein (APP) and gamma-secretase in a way that less Amyloid-β-peptide (Aβ42) is produced. Furthermore they have the ability to bind selectively and with high affinity the APP-GxxxG-motif and can pass the blood-brain barrier. It was shown that a drug capable of binding the APP GxxxG motif is weakening or inhibiting the dimerization of the APP trans-membrane sequence, leading to a decreased generation of Aβ42.

IP Rights
EP patent application was filed in November 2007.
PCT patent application was filed in November 2008.
US application was filed in April 2010.

Origin
Freie Universiät Berlin
Application Area:
Drug screening
Development Stage: Product
Bild des Benutzers Rafaela Kunz
Licensing Manager: Rafaela Kunz
T +49 30 2125 4825
F +49 30 2125 4822
Suitable Industry: Pharmaceuticals, Research & Development
Benefits:
  • Reliable, rapid, and easy screening assay for the identification of novel drug candidates
  • Applicable to blood samples

Assay for the Diagnosis of Alzheimer’s Disease based on the Determination of the Ratio of Aß38:Aß42


28.10.2011
| Ref.Nr. 06021
Life Science › Pharma&Biotech

Backgorund
Processing of the amyloid precursor protein (APP) by ß-and γ -secretases leads to the generation of amyloid-ß (Aß) peptides, which are the toxic agents in the pathogenesis of Alzheimer`s Disease. γ –secretase cleaves at variable sites producing Aß peptides with different C-termini, of which particularly Aß42 contributes to cytotoxicity and amyloid accumulation in Alzheimer Disease.

We discovered that dimerization of the APP trans-membrane sequence is mediated by glycine residues G29 and G33 of the three consecutive GxxxG motifs promoting helix-helix interactions. Mutations at the glycine positions attenuate the TMS dimerization strength and specifically reduce generation of Aß42. The level of reduced Aß42 is counterbalanced by increased Aß38, whereas the level of Aß40 remains unaffected.

Technology
We offer a novel assay for the diagnosis of early and late stages of Alzheimer’s Disease. The assay is very easy to use and allows a rapid and reliable detection of Aß38:Aß42. The ratio is used to make the diagnosis.

IP Rights
European Patent application was filed in June 2006.
PCT application was filed in April 2007.
Patent applications were filed in US, JP, IN, CN, CA, FR, GB, IT, ES, DE.

Origin
Freie Universität Berlin

 

Application Area:
Diagnosis of Alzheimer disease at all stages
Development Stage: Product
Bild des Benutzers Rafaela Kunz
Licensing Manager: Rafaela Kunz
T +49 30 2125 4825
F +49 30 2125 4822
Suitable Industry: Diagnostics, Pharmaceuticals
Benefits:
  • Suitable for diagnosing Alzheimer at early stage of disease
  • Reliable, easy, and rapid diagnosis
  • Screening of blood samples

Pharmaceutical Composition for the Treatment of Solar Urticaria


25.08.2011
| Ref.Nr. 09093
Life Science › Pharma&Biotech

Background
Solar urticaria is an uncommon but well-recognized disorder characterized by the early onset of itching, erythema, and whealing after exposure to UVA, visible light, less commonly UVB and rarely infrared radiation. Typically, symptoms occur within minutes after solar radiation and are limited to sun-exposed skin areas.


Technology

We offer a lidocaine/prilocaine combination for the treatment or prevention of solar urticaria. Up to now the lidocaine/prilocaine combination is used for dermal anesthesia (marketed as EMLA). The inventors demonstrated in two of two patients with solar urticaria and an action spectrum to UVA that the combination of lidocaine and prilocaine protects the tissue and inhibits triggering of the cascade which usually leads to typical symptoms of solar urticaria.
The topical application of a lidocaine/prilocaine mixture prior to UV-provocation stabilizes or inhibits sensory nerve fibres of the skin and induces down-regulation or inhibition of the release of pro-inflammatory neuropeptides. Due to this more general concept it is assumed that (1) other local anesthetics in addition to lidocaine and prilocaine, (2) lidocaine alone or prilocaine alone, and (3) lidocaine and/or prilocaine in combination with other local anesthetics are effective as well.

IP Rights

A European patent application was filed in April 2010.

Patent Owner
Charité – Universitätsmedizin Berlin

Application Area:
Treatment or prevention of solar urticaria
Development Stage: Clinical
Weitere Kategorien: Life Science, Pharma & Biotech
Bild des Benutzers Dr. Janin Hofmann
Licensing Manager: Dr. Janin Hofmann
T +49 30 2125 4828
F +49 30 2125 4822
Suitable Industry: Pharmaceutical industry
Benefits:
  • Topical application on skin parts of patients leads to a reliable reduction of clinical symptoms of solar urticaria
  • The treatment is very effective and is associated with low side-effects
  • Topical application directly on the sun-exposed skin is more convenient to the patient than other application routes
  • The individual active ingredients of the pharmaceutical composition are already clinical approved for anesthesia
  • Low cost treatment

One-Plasmid Systems for Blue-light-regulated Gene Expression in Prokaryotes


18.08.2011
| Ref.Nr. 11043
Life Science › Pharma&Biotech

Background
Protein expression systems are very widely used in the life sciences, biotechnology and medicine. Traditional strategies for recombinant protein expression involve the transformation of a gene expression vector into prokaryotic expression hosts and culturing the cells so that they express the desired protein. Using an inducible expression cassette the onset of the protein expression can be controlled by several inducer (f.e. chemical, temperature, cold).

Technology
We offer two compact plasmids for facile light regulated expression of target proteins in prokaryotic hosts. Dependent from the application, one plasmid can be used for light activated and one for light inactivated gene expression. Both plasmids are working without exogenous addition of chromophores or expensive chemical inducers and allow a specific, spatially- and temporally precise control of protein expression. A competitive advantage is the use of light as inducer especially for the production of recombinant proteins. Another advantage is the very precise control of protein expression which is very relevant for several research applications. By using standard chemical inducers a spatially and temporally precise control of protein expression is not possible.

IP Rights

None

Origin
Humboldt University, Berlin
Application Area:
Production of proteins in prokaryotes Analysis of protein functions in prokaryotes Pulsed induction of protein expression for several research applications
Development Stage: Product
Weitere Kategorien: Life Science, Pharma & Biotech
Bild des Benutzers Dr. Bettina Büttner
Licensing Manager: Dr. Bettina Büttner
T +49 30 2125 4835
F +49 30 2125 4822
Suitable Industry: Biotechnology and pharmaceutical industry, Research & Development
Benefits:
  • One plasmid is designed for light inactivated and one for light activated gene expression
  • Both plasmids are compact and ready-to-use
  • No exogenous addition of chromophores or chemical inducers is required
  • System facilitates pulsed and/or automated induction of protein expression
  • Allows specific, spatially- and temporally-precise control of protein expression
  • Reduced production costs, because expensive chemical inducers are not required

Stereoselective Synthesis of cis-4-methylsphingosine and derivatives thereof


24.06.2011
| Ref.Nr. 10127
Life Science › Pharma&Biotech

Background
Sphingosine-1-phosphate is a bioactive lipid signaling molecule and an agonistic ligand of five specific G protein coupled receptors named S1P1-5.These receptors play a crucial role in the cardiovascular and immune system and in angiogenesis. The known compound FTY720 (Fingolimod) is a sphingosine analogue with immunosuppressive effects and was recently approved for treatment of multiple sclerosis in the United States and Russia.The synthetic sphingosine analogue Cis-4-methylsphingosine was firstly synthesized by R. R. Schmidt and coworkers in 1993 in nine steps.Similar to FTY720 this compound is phosphorylated in biological systems and inhibits the activity of different S1P-receptors, however the spectrum of receptors influenced by Cis-4-methylsphingosine is slightly different to that influenced by FTY720. Cis-4-methylsphingosine induces apoptosis of neuroblastoma cells.

Technology
We offer a rapid and simple method for the stereoselective synthesis of cis-4-methylsphingosine and derivatives thereof in only two steps. The novel synthesis is characterized by using easily accessible starting material, and an overall yield of nearly 30% which is almost 100-fold compared to the synthesis known in the art. Since Cis-4-methylsphingosine also influences S1P-receptors like FTY70, however with a slight different spectrum, this compound might have similar effects or might support or supplement the activity of FTY720. Thereby Cis-4-methysphingosine has a great potential for pharmaceutical application.   

IP Rights
EP patent application was filed in May 2011
 
Patent Owner
Humboldt-Universität zu Berlin

 

Application Area:
Preparation of cis-4-methylsphingosine
Development Stage: Proof of concept
Weitere Kategorien: Life Science, Pharma & Biotech
Bild des Benutzers Dr. Bettina Büttner
Licensing Manager: Dr. Bettina Büttner
T +49 30 2125 4835
F +49 30 2125 4822
Suitable Industry: Chemical, biotechnology and pharmaceutical industry
Benefits:
  • Reliable, easy and rapid method for the preparation of cis-4-methylsphingosine
  • Only two steps form starting material to cis-4-methylsphingosine
  •  Cost- and time-effective synthesi100-fold higher yield compared to state of the art synthesis 

New Pill Package - Applicator for Ointments


12.05.2011
| Ref.Nr. 10049
Life Science › Pharma&Biotech

The invention offers two new packaging methods for pills and ointments. Advantage of the packagings is the one-hand operation and the sterile application of the drug.

Pills are fixed on a carrier item that is airtight sealed in a blister-like packaging. It enables the patient to take the pill sterile with one hand from the carrier item. Particularly, the pill goes straight to the mouth of the patient and any contact with the possibly unwashed hands or the non-sterile environment is avoided.

The invented pill dispenser can have marks for the weekdays and daytimes. Additionally it has a fixed patient information leatflet, so that a mixing up with other drugs becomes excluded.

For the sterile application of an ointment a small map packaging was invented. Therefore, the ointment is airtight sealed on a cushion at the end of a rodlike carrier item. The rodlike carrier items are alternating fixed on the map packaging and one map contains as many dosages as needed for one day.

The patient is able to apply target-oriented a defined dosage of one use sterile at every time and everywhere. Therefore, the packaging is special on the way extremely convenient.

IP Rights
German Patent Application, filed on August 6, 2010

Origin
Hochschule für Technik und Wirtschaft Berlin, Germany

Application Area:
Drug packaging
Development Stage: Prototyp
Type of Collaboration: License
Schlagworte: blister, dosage, one-hand, package, pill, sterile,
Bild des Benutzers Rafaela Kunz
Licensing Manager: Rafaela Kunz
T +49 30 2125 4825
F +49 30 2125 4822
Market Potential: Worldwide
Benefits:
  • Sterile application of drugs
  • One-hand operation
  • Simply application being on the way

Drug screening assay for the detection of Aß42 peptides in the cell nucleus


09.03.2011
| Ref.Nr. 09033
Life Science › Pharma&Biotech › Drug delivery

Time dependent accumulation of Aβ42 (A) and Aβ42G33A (B) in the nucleus of human neuroblastoma cells.It is known from the state of the art that Ab peptides with 42 amino acids appear to be the key pathogenic species in Alzheimer’s disease, as they are believed to initiate neuronal degeneration. The invention relates to the finding that Ab42 enters neuroblastoma cells and accumulates in the cell nucleus.

We offer a drug-screening assay for the detection of Ab42 accumulation in the cell nucleus of neuroblastoma cells. The new technology is based on the analysis of the cellular and subcellular localization of Ab42 and allows a high throughput identification of compounds that prevent the accumulation of Ab42 in the cell nucleus.
Due to the underlying mechanism that compounds could be:
  • Inhibitors of the transport of Ab42 into the cells and/or into the cell nucleus
  • Inhibitors of the dimerization of APP’s
  • Activator of Ab42 specific degradation
  • Inhibitor and/or modulator of generegulated function 

The identified compounds can preferably be used for the prophylaxis and treatment of neurodegenerative disease, such as Alzheimer’s disease.

IP Rights
A PCT patent application was filed on November 20th, 2010 with priority on November 20th, 2009.

Origin

The assay was developed at the Charité – Universitätsmedizin Berlin and FU Berlin (Germany).

Application Area:
Pharma
Development Stage: In vitro
Type of Collaboration: License
Bild des Benutzers Rafaela Kunz
Licensing Manager: Rafaela Kunz
T +49 30 2125 4825
F +49 30 2125 4822
Market Potential: Worldwide
Benefits:
  • Fast detection of new drug candidates
  • High throughput capable assay
  • Cost-saving technology
  • Insights for the mode of action and better chances for drug approval