Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of
(I) reacting a compound of formula (III)
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of
(I) reacting a compound of formula (III)
with an azide of formula (IV)
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of
(I) reacting a compound of formula (III)
with an azide of formula (IV)
to prepare a compound of formula (V)
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of
(I) reacting a compound of formula (III)
with an azide of formula (IV)
to prepare a compound of formula (V)
(II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI)
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of
(I) reacting a compound of formula (III)
with an azide of formula (IV)
to prepare a compound of formula (V)
(II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI)
resulting in a compound of formula (VII)
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of
(I) reacting a compound of formula (III)
with an azide of formula (IV)
to prepare a compound of formula (V)
(II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI)
resulting in a compound of formula (VII)
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Fundació Institut de Ciències Fotòniques ("ICFO") (Spain)
Forschungsverbund Berlin e.V. (Germany)
INSTITUCIÓ CATALANA DE RECERCA I ESTUDIS AVANÇATS (ICREA) (Spain)
Inventor
Ivanov, Mikhail
Smirnova, Olga
Jimenez-Galan, Alvaro
Tyulnev, Igor
Biegert, Jens
Poborska, Julita
Vamos, Lenard
Silva, Rui
Abstract
The present disclosure relates to a method for encoding information by valley polarization in a material using an electromagnetic field. The method comprises the steps of providing a material, and applying the electromagnetic field onto the material, wherein the electromagnetic field possesses an m-fold symmetry and the real-space lattice structure or real-space sub-lattice structure of the material possesses an n-fold symmetry, wherein the symmetry of the electromagnetic field corresponds to the symmetry of the real-space lattice structure or real-space sub-lattice structure of the material in such a way that n is an integer multiple of m, and wherein the electromagnetic field induces and/or manipulates valley polarization in the bandstructure of the material. The present disclosure further provides a device for generating an electromagnetic field suitable for inducing and/or manipulating valley polarization in a multilayer material.
G02F 1/09 - Devices or arrangements for the control of the intensity, colour, phase, polarisation or direction of light arriving from an independent light source, e.g. switching, gating or modulatingNon-linear optics for the control of the intensity, phase, polarisation or colour based on magneto-optical elements, e.g. exhibiting Faraday effect
G02F 1/01 - Devices or arrangements for the control of the intensity, colour, phase, polarisation or direction of light arriving from an independent light source, e.g. switching, gating or modulatingNon-linear optics for the control of the intensity, phase, polarisation or colour
Helmholtz Zentrum Muenchen Deutsches forschungszentrum für Gesundheit und Umwelt (GmbH) (Germany)
Inventor
Leonhardt, Heinrich
Stengl, Andreas
Roas, Maike
Schwach, Jonathan
Spiekermann, Karsten
Polzer, Harald
Able, Marina
Helma-Smets, Jonas
Schumacher, Dominik
Gerlach, Marcus
Hackenberger, Christian Peter Richard
Kasper, Marc-André
Jeremias, Irmela
Vick, Binje
Kremmer, Elisabeth
Abstract
The present invention relates to novel anti-FLT3 antibodies for specifically targeting extracellular domain of FLT3. The present invention further relates to targeting FLT3 by novel antibody-drug-conjugates (ADCs) based on the novel anti-FLT3 antibodies of the present invention, especially in combination with kinase inhibitors, for use in therapy and/or for use in a method of cancer treatment (e.g., acute myeloid leukemia (AML) with or without internal tandem duplication (ITD) mutations in the FLT3 gene (FLT3-ITD)).
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 35/02 - Antineoplastic agents specific for leukemia
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
4.
THIAZOLO TETRAHYDROCHINOLINE COMPOUNDS AS CLASS II PHOSPHOINOSITIDE 3-KINASE INHIBITORS
The invention relates to chemical compounds useful as inhibitors of class II phosphoinositide 3- kinase (PI3K) signalling. The invention further relates to the medical use of inhibitors of class II phosphoinositide 3-kinase (PI3K) signalling in the treatment of medical conditions associated with defective and/or pathologic class II phosphoinositide 3-kinase (PI3K) signaling, such as stroke, a cardiovascular disease related to endothelial cell dysfunction, cancer, cancer metastasis, myopathy and diabetes.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
5.
PYRAZOLO-QUINOLINES AS SELECTIVE INHIBITORS OF GENOTOXIC STRESS-INDUCED IKK/NF- KB PATHWAYS FOR CANCER THERAPY
Disclosed are novel conjugates and methods for the preparation thereof. One of the methods for the preparation of a conjugate comprises a step of: acting a compound of formula (I), with a thiol-containing molecule of formula (II), wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, a small molecule, an optionally substituted C1-C8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
C07F 9/6524 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having four or more nitrogen atoms as the only ring hetero atoms
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
7.
PEPTIDE CONJUGATES FOR LABELLING ENDOGENOUS GIPR AND GLP-1R
The invention relates to a peptide conjugate comprising a peptide covalently linked to a label, wherein the peptide comprises an amino acid sequence of a protein ligand that binds at least one class B1 G protein-coupled receptor, wherein the peptide is covalently linked to the label. The protein ligand is preferably an agonist, antagonist and/or co-agonist of at least one class B1 G protein-coupled receptor, preferably from the Glucagon-like subfamily. The agonist, antagonist and/or co-agonist is preferably selected from tirzepatide, LY3437943 or GIF. The invention further relates to kits comprising the peptide conjugate according to the invention or means for assembling the conjugate, as well as methods for using the peptide conjugate according to the invention.
An aluminium-containing bulk β-(AlxGa1-x)2O3 single crystal (7) directly grown from the melt with (x) between 0.1 – 0.35, that corresponds to 10 – 35 mol.% of Al. The single crystal (7) maintains its monoclinic, single crystalline structure with the following lattice parameters: a = 12.1780 – 12.0330 ± 0.015 Å, b = 3.0245 – 2.9795 ± 0.012 Å, c = 5.7870 – 5.7280 ± 0.012 Å, and β = 103.905 – 104.046 ± 0.01°, and has a volume of at least 5 cm3, preferably at least 100 cm3. The energy gap of the single crystal (7) increases in relation to pure β-Ga2O3 by 0.2 – 0.8 ± 0.05 eV for x = 0.1 – 0.35 for polarizations parallel to main crystallographic direction along the a-, b-, and c-axis. The bulk β-(AlxGa1-x)2O3 single crystal (7) can be an electrical insulator or semi-insulator, semiconductor, or degenerate semiconductor. Also, a method for producing aluminium-containing, bulk β-(AlxGa1-x)2O3 single crystal (7) directly grown from the melt, in particular from the melt contained within a metal crucible (3) is provided.
The invention relates to a crystal growth device for growing a semiconductor from a gas phase, the crystal growth device comprising, a crucible, a heater, and a holding plate. The crucible on a crucible vessel and a crucible lid supported on the crucible vessel, wherein the crucible vessel is configured to receive and hold a source material for the semiconductor during growth of the semiconductor. The heater is configured and arranged to heat the source material in the crucible vessel so that the source material at least partially changes to its gaseous phase and flows toward the crucible lid. The holding plate is configured to hold a seed crystal on a side of the holding plate facing the crucible lid, and to allow deposition of the source material that has changed into its gas phase on the seed crystal for growing the semiconductor. The holding plate is further configured to be spaced from a crucible bottom of the crucible vessel for growing the semiconductor, such that it is located between the source material and the crucible lid.
(I) reacting a compound of formula (III)
with an azide of formula (IV)
to prepare a compound of formula (V)
(II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI)
resulting in a compound of formula (VII)
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
H01L 21/00 - Processes or apparatus specially adapted for the manufacture or treatment of semiconductor or solid-state devices, or of parts thereof
H01L 21/02 - Manufacture or treatment of semiconductor devices or of parts thereof
H01L 29/04 - Semiconductor bodies characterised by their crystalline structure, e.g. polycrystalline, cubic or particular orientation of crystalline planes
H01L 29/207 - Semiconductor bodies characterised by the materials of which they are formed including, apart from doping materials or other impurities, only AIIIBV compounds further characterised by the doping material
12.
BIFUNCTIONAL PEPTIDE WITH MUCOADHESIVE AND VIRUS BINDING PROPERTIES
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
13.
BIFUNCTIONAL PEPTIDE WITH MUCOADHESIVE AND VIRUS BINDING PROPERTIES
The present invention relates to a bifunctional peptide comprising a virus binding moiety (2) and a mucin binding moiety (1) covalently bound to the virus binding moiety (2). The virus binding moiety is chosen from peptides binding to SARS-CoV-2, to influenza A, to influenza B, to rhinoviruses and other enteroviruses, to human parainfluenza virus, and/or to metapneuvirus. The mucin binding moiety is chosen from lectins such as trefoil factor 3.
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The invention relates to a method for producing isotope-enriched germanium-hydrogen compounds, comprising the following method steps: a) providing a gas of a highly chemically pure germanium tetrafluoride; and b) providing a reducing solution in an inert reaction container, the reducing solution containing an organic solvent and an alkali-aluminum hydride as the reducing agent; c) introducing the gas in the reducing solution; and d) condensing the gaseous germanium-hydrogen compounds produced by the reduction.
The invention relates to an oxide crystal comprising a rare earth metal at a mole fraction of 45 at.% or more, aluminium at a mole fraction of 45 at.% or more, and chromium. Chromium is present in the oxide crystal at a certain mole fraction such that the oxide crystal has an absorption coefficient for at least one wavelength in a wavelength range of 600 nm to 800 nm, which absorption coefficient is smaller by a factor of 2 than for at least one wavelength in a wavelength range of 490 nm to 575 nm.
HELMHOLTZ ZENTRUM MUENCHEN DEUTSCHES FORSCHUNGSZENTRUM FÜR GESUNDHEIT UND UMWELT (GMBH) (Germany)
Inventor
Leonhardt, Heinrich
Stengl, Andreas
Roas, Maike
Schwach, Jonathan
Spiekermann, Karsten
Polzer, Harald
Able, Marina
Helma-Smets, Jonas
Schumacher, Dominik
Gerlach, Marcus
Hackenberger, Christian Peter Richard
Kasper, Marc-André
Jeremias, Irmela
Vick, Binje
Kremmer, Elisabeth
Abstract
The present invention relates to novel anti-FLT3 antibodies for specifically targeting extracellular domain of FLT3. The present invention further relates to targeting FLT3 by novel antibody-drug- conjugates (ADCs) based on the novel anti-FLT3 antibodies of the present invention, especially in combination with kinase inhibitors, for use in therapy and/or for use in a method of cancer treatment (e.g., acute myeloid leukemia (AML) with or without internal tandem duplication (ITD) mutations in the FLT3 gene (FLT3-ITD)).
A61K 31/00 - Medicinal preparations containing organic active ingredients
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 35/02 - Antineoplastic agents specific for leukemia
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
17.
CONJUGATES COMPRISING A PHOSPHORUS (V) AND A DRUG MOIETY
The present invention relates to a conjugate having the formula (I): wherein a receptor binding molecule (RBM) is connected with a drug moiety (D). The present invention also relates to intermediates for producing the same, methods of preparing the same, pharmaceutical compositions comprising the same, as well as uses thereof.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
18.
CONJUGATES COMPRISING A PHOSPHORUS (V) AND A DRUG MOIETY
The present invention relates to a conjugate having the formula (I): wherein a receptor binding molecule (RBM) is connected with a drug moiety (D). The present invention also relates to intermediates for producing the same, methods of preparing the same, pharmaceutical compositions comprising the same, as well as uses thereof.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
19.
Means and methods for site-specific functionalization of polypeptides
The present invention provides means and methods for equipping a polypeptide of interest at its C-terminus with a versatile adaptor amino acid that allows the functionalization of the polypeptide of interest.
188-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN IN DER HELMHOLTZ-GEMEINSCHAFT (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Stein, Ulrike
Kobelt, Dennis
Walther, Wolfgang
Nazaré, Marc
Specker, Edgar
Yan, Shixian
Abstract
The invention relates to MACC1 inhibitors for use as a medicament in the treatment of cancer. The general formula 1 provided by the invention shows beneficial effects in inhibiting the formation of metastasis, cell proliferation and cancer progression. The invention further relates to the MACC1 inhibitors of the invention for the treatment of a subject with elevated MACC1 levels and wherein said treatment inhibits MACC1 expression in said subject. The invention further relates to the MACC1 inhibitors of the invention in the treatment of subjects with a solid cancer at early stages of cancer progression such as stage I or II for colorectal or pancreatic cancer or metastatic cancer, and/or for the prevention of developing metastases.
Compounds of the following formula:
having defined substituents. The compounds can inhibit class II phosphoinositide 3-kinase (PI3K) signaling and are useful for the treatment of a medical condition associated with defective PI3K signaling, such as myopathy, cancer, diabetes, thrombosis or cardiovascular disease.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
23.
CELLULAR UPTAKE OF LARGE BIOMOLECULES ENABLED BY CELL-SURFACE-REACTIVE CELL-PENETRATING PEPTIDE ADDITIVES
The present invention is directed to a method for delivering a cargo into a cell, the method comprising incubating a compound comprising a moiety capable to bind to the cell surface and a guanidine moiety together with a cargo and a cell, wherein the cargo is connected with a group comprising guanidine moiety, thereby allowing delivering of the peptide or protein into the cell. The invention is further directed to a compound comprising a moiety capable to bind to the cell surface and guanidine moiety for use in delivering a cargo into a cell, distinct compounds, distinct compounds for use in delivering a cargo into a cell, a kit for use in delivering a cargo into a cell comprising a compound comprising a moiety capable to bind to the cell surface and a guanidine moiety.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
24.
IMPROVED CD30 TARGETING ANTIBODY DRUG CONJUGATES AND USES THEREOF
The present invention relates to an antibody-drug conjugate (ADC) comprising: (a) Brentuximab, wherein Brentuximab comprises at the C-terminus of the light chains, the heavy chains or all of the heavy and light chains of the Brentuximab a recognition sequence for tubulin tyrosine ligase and a non-natural amino acid; and (b) at least one drug moiety; wherein a drug moiety is coupled to each of the non-natural amino acids via a linker. The present invention further relates to methods of producing same, pharmaceutical compositions comprising same as well as uses thereof.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
25.
IMPROVED CD30 TARGETING ANTIBODY DRUG CONJUGATES AND USES THEREOF
The present invention relates to an antibody-drug conjugate (ADC) comprising: (a) Brentuximab, wherein Brentuximab comprises at the C-terminus of the light chains, the heavy chains or all of the heavy and light chains of the Brentuximab a recognition sequence for tubulin tyrosine ligase and a non-natural amino acid; and (b) at least one drug moiety; wherein a drug moiety is coupled to each of the non-natural amino acids via a linker. The present invention further relates to methods of producing same, pharmaceutical compositions comprising same as well as uses thereof.
A61K 47/65 - Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
26.
CD30 TARGETING ANTIBODY DRUG CONJUGATES AND USES THEREOF
The present invention relates to an antibody-drug conjugate (ADC) comprising: (a) Brentuximab, wherein Brentuximab comprises at the C-terminus of the light chains, the heavy chains or all of the heavy and light chains of the Brentuximab a recognition sequence for tubulin tyrosine ligase and a non-natural amino acid; and (b) at least one drug moiety; wherein a drug moiety is coupled to each of the non-natural amino acids via a linker. The present invention further relates to methods of producing same, pharmaceutical compositions comprising same as well as uses thereof.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
wkblockkbulkbulk of the corresponding semiconductor material (16, 12) for spatially selective heat transfer from the active zone (40) to a side of the corresponding semiconductor material (16, 12) opposite the active layer (14).
H01S 5/20 - Structure or shape of the semiconductor body to guide the optical wave
H01S 5/0237 - Fixing laser chips on mounts by soldering
H01S 5/323 - Structure or shape of the active regionMaterials used for the active region comprising PN junctions, e.g. hetero- or double- hetero-structures in AIIIBV compounds, e.g. AlGaAs-laser
28.
SILICON-BASED WAFERS AND METHOD FOR FABRICATING SILICON-BASED WAFERS
The invention relates to a method for fabricating silicon-based wafers which comprises the following steps, performed in sequence: a) providing a substrate which has an amorphous silicon layer on the surface of the substrate and a native silicon oxide layer (30) covering the amorphous silicon layer; b) (i) partially or completely removing the native silicon oxide layer and producing an artificial silicon oxide layer with a defined layer thickness on the amorphous silicon layer; or (ii) partially removing the native silicon oxide layer down to a predefined layer thickness; and c) growing a crystalline silicon layer on the surface of the (i) artificial silicon oxide layer or (ii) partially removed silicon oxide layer by means of a temperature difference method (TDM), from a metallic melt. Furthermore, the invention relates to a silicon-based wafer which can be fabricated according to the method.
The invention relates to a method for producing an oxide crystal having a perovskite structure and a chemical formula ABO3, wherein components A and B are different cations having different ionic radii, and the method comprises the step of: - monitoring at least one growth parameter during the production of the oxide crystal in such a way that the produced oxide crystal has a stoichiometry deviation which is caused by the fact that a number of those lattice sites of the oxide crystal which, without stoichiometry deviation, would be occupied by cations having a larger ionic radius are occupied by cations having a smaller ionic radius.
C23C 16/18 - Chemical coating by decomposition of gaseous compounds, without leaving reaction products of surface material in the coating, i.e. chemical vapour deposition [CVD] processes characterised by the deposition of metallic material from metallo-organic compounds
TECHNION RESEARCH & DEVELOPMENT FOUNDATION LIMITED (Israel)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Neufeld, Ofer
Ayuso, David
Lerner, Gavriel
Cireasa, Dana Raluca
Ivanov, Mikhail
Smirnova, Olga
Cohen, Oren
Abstract
Methods and systems for detecting chiral characteristic of an analyte, are provided. In some embodiments, the method disclosed herein (e.g. operated by a system) comprises receiving at least one spectral line of harmonic emission generated by an interaction between a laser field and the analyte; measuring a characteristic of an electric field of the at least one spectral line resulting from an electric dipole interaction between the laser field and the analyte; and determining the chiral characteristic of said analyte based on said measured characteristics of the at least one spectral line.
G01N 21/31 - Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry
The present invention relates to a method for microstructuring and more particularly to a method for producing locally defined microstructures (24) made of metals (20) on substrate surfaces (12). A method according to the invention for producing locally defined microstructures (24) on substrate surfaces (12) comprises: - providing a substrate surface (12) having a region of defined roughness (14); - locally reducing the roughness of the substrate surface (12) in the region of defined roughness (14) in order to form at least one region of reduced roughness (16); - depositing a metal (20) at a temperature of the substrate surface (12) above the melting point of the metal (20) in order to form localized metal drops (22) in regions of reduced roughness (16); and - cooling the substrate surface (12) in order to solidify the localized metal drops to form microstructures (24) in regions of reduced roughness (16).
(I) reacting a compound of formula (III)
with an azide of formula (IV)
to prepare a compound of formula (V)
(II) reacting a compound of formula (V) with a thiol-containing molecule of formula (VI)
resulting in a compound of formula (VII)
C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
MAX DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN IN DER HELMHOLTZ-GEMEINSCHAFT (Germany)
CHARITÉ - UNIVERSITÄTSMEDIZIN BERLIN (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Kettenmann, Helmut
Wolf, Susanne
Jordan, Philipp
Kleissle, Sabrina
Neuenschwander, Martin
Specker, Edgar
Nazare, Marc
Abstract
The invention relates to compounds useful as inhibitors of NO production, especially inhibitors of the inducible NO synthase iNOS expressed by microglia and macrophages. The invention also relates to pharmaceutical compositions comprising these compounds and to therapeutic uses of these compounds, especially in the prophylaxis or treatment of conditions characterized by excess NO production, such as ischemic stroke and retinopathies.
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
The invention relates to a method for growing a rare earth sesquioxide crystal with a cubic crystal structure from a melt. The rare earth sesquioxide crystal contains at least 5% yttrium oxide and at least 5% scandium oxide such that the liquidus temperature of the crystal lies below 2400°C. Alternatively, the rare earth sesquioxide crystal can also contain yttrium oxide and at least 5% scandium oxide, and the proportions of yttrium oxide and scandium oxide can be selected in a starting material such that the rare earth sesquioxide crystal to be grown has a liquidus temperature below 2400°C. The starting material can be melted at a temperature of 2400°C or lower in a crucible which consists of a material that has a melting temperature below 3000°C. The rare earth sesquioxide crystal can be grown from the molten starting material using a crystal growing method, for example the Czochralski method or the HEM method. A crucible-free growth of the rare earth sesquioxide crystal is also possible at a temperature of 2400°C or lower, for example using an optical zone melting process.
C30B 35/00 - Apparatus not otherwise provided for, specially adapted for the growth, production or after-treatment of single crystals or of a homogeneous polycrystalline material with defined structure
16 - Paper, cardboard and goods made from these materials
25 - Clothing; footwear; headgear
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Printed matter; photographs (prints). Clothing; headgear. Medical research laboratory services; scientific veterinary
laboratory services; medical laboratory services; ultrasound
imaging services (except for medical purposes). Consultation relating to veterinary services; provision of
information relating to veterinary services; veterinary
services; medical services.
16 - Paper, cardboard and goods made from these materials
25 - Clothing; footwear; headgear
42 - Scientific, technological and industrial services, research and design
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Printed matter, namely, paper signs, books, manuals, curricula, newsletters, informational cards, brochures in the field of veterinary services; printed photographs Clothing, namely, shirts, T-shirts; headwear Medical research laboratory services; scientific veterinary laboratory services; medical laboratory services; non-medical ultrasound imaging services Consultation relating to veterinary services; provision of information relating to veterinary services; veterinary services; medical services
The present invention relates to chemical compounds which can be used in particular as structural mimetics of proline-rich peptides. The compounds of the present invention are capable of selectively inhibiting Ena/VASP-EVH1-mediated protein-protein interactions. The invention further relates to the use of these compounds as pharmaceutical agents and the use of the pharmaceutical agents for the treatment of tumor diseases.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
39.
1,2,4-triazole derivatives as tankyrase inhibitors
1-3 alkyl). These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
The invention relates to a method for providing a transient grid on a surface of a layer system. The layer system comprises at least one optoacoustic converter layer. The method comprises the step: - illuminating the layer system by means of a spatially periodically modulated radiation pulse which has a pulse duration in the nanosecond range such that the optoacoustic converter layer thermally expands such that, as a result of the thermal expansion of the optoacoustic converter layer, the transient grid is created on the surface of the layer system.
G21K 1/06 - Arrangements for handling particles or ionising radiation, e.g. focusing or moderating using diffraction, refraction, or reflection, e.g. monochromators
41.
A LIPOSOME SYSTEM COMPRISING A LIPID, AN ACTIVE COMPOUND AND A VECTOR PEPTIDE
n42042020) alkylene group. The liposomes have an average diameter of 65 to 1000 nm. Furthermore, the present invention is directed to the use of the liposome-based carrier system for use in medicine, in particular for use in treating or preventing of peeling skin syndromes (PSS), the Netherton Syndrome, SAM Syndrome psoriasis vulgaris, atopic dermatitis, impetigo, microbial eczema, microbial eczema associated with dermatomycosis, NISCH Syndrome, androgenetic alopecia, alopecia areata, bullous immunodermatoses, and epidermolysis bullosa, skin tightening, and dry skin conditions. Moreover, the invention is directed to pharmaceutical compositions comprising the liposome- based carrier system
The invention relates to an apparatus and a method for UV sterilization, more particularly for intra-corporeal in vivo UV sterilization on the human and animal body in the event of colonization with multidrug-resistant (MDR) organisms such as methicillin-resistant Staphylococcus aureus (MRSA) and Staphylococcus epidermidis (MRSE). An apparatus (100) according to the invention for UV sterilization comprises a light-emitting diode chip, LED chip (12), designed to emit radiation in the UVC spectral range, wherein the LED chip (12) together with its packaging (16) forms a light-emitting diode, LED (10); a spectral filter element (14), set up to restrict the radiation emitted by the LED chip (12) substantially to wavelengths below 235 nm; and an optical element (18) for the targeted emission of the radiation emitted by the LED (10). A method according to the invention for UV sterilization comprises the irradiation of a surface (O) to be decolonized, using an apparatus (100) according to the invention.
The invention relates to one or more regions of the thyroid-stimulating hormone receptor (TSHR), identified herein as a TSHR ligand binding domain. Such a domain is considered a binding pocket for chemical compounds, for example S37 or derivatives thereof, that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists. Embodiments of the invention relate to proteins and corresponding coding nucleic acids for the proteins of the invention, for example the TSHR ligand binding domain and related proteins. The invention relates to methods of screening for or testing compounds that interact, bind and/or modify the TSHR ligand binding domain of the invention.
The present invention provides means and methods for equipping a polypeptide of interest at its C-terminus with a versatile adaptor amino acid that allows the functionalization of the polypeptide of interest.
The invention relates to an optical pulse generator and to a method for operating an optical pulse generator. In particular, an optical pulse generator according to the invention is to uniformly supply all emitters and their segments of a laser diode with power. The optical pulse generator according to the invention comprises: an active optical component (10) designed to emit optical radiation; a means for electrically controlling (20) the optical component (10), designed to cause the optical component (10) to emit optical radiation in a pulsed manner; wherein the active optical component (10) is divided into at least two groups (3) along a longitudinal axis (y), wherein each of the groups (3) contacts a respective electrically isolated power supply (11).
H03K 3/42 - Generators characterised by the type of circuit or by the means used for producing pulses by the use, as active elements, of opto-electronic devices, i.e. light-emitting and photoelectric devices electrically- or optically-coupled
H03K 17/78 - Electronic switching or gating, i.e. not by contact-making and -breaking characterised by the use of specified components by the use, as active elements, of opto-electronic devices, i.e. light-emitting and photoelectric devices electrically- or optically-coupled
46.
CHEMOSELECTIVE THIOL-CONJUGATION WITH ALKENE OR ALKYNE-PHOSPHONOTHIOLATES AND - PHOSPHONATES
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosohonothiolates and -phosphonates comprises the step of: reacting a compound of formula (I) with a thiol-containing molecule of formula (II) wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, an optionally substituted C1-C8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
HELMHOLTZ-ZENTRUM BERLIN FÜR MATERIALIEN UND ENERGIE GMBH (Germany)
Inventor
Heilmann, Martin
Höflich, Katja
Lopes, Joao Marcelo
Geelhaar, Lutz
Abstract
The invention relates to a method for producing a 2D material (100), which method comprises producing an atom layer (10) of a crystalline substance (11), such as graphene, on a carrier substrate (20), and irradiating the atom layer (10) with particles (30) in such a way that lattice defects (12) are produced in the atom layer (10), the lattice defects (12) being produced at defect positions according to a specified geometric pattern (13) along the atom layer (10), and termination of the lattice defects (12) is provided using impurity atoms (15, 16) which couple to unsaturated bonds of the lattice defects (12). The invention also relates to a 2D material in which lattice defects (12) are arranged at defect positions according to a specified geometric pattern (13) and are terminated using impurity atoms (14) which are coupled to unsaturated bonds of the lattice defects (12).
MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Bader, Michael
Specker, Edgar
Matthes, Susann
Schütz, Anja
Mallow, Keven
Grohmann, Maik
Nazaré, Marc
Abstract
The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative.
The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
The invention relates to a device for generating a laser beam. The aim of the invention is to provide a laser diode which simultaneously has a high degree of efficiency and a low degree of far field divergence. The diode laser according to the invention comprises a current barrier (5) which is characterized in that the current barrier (5) extends along a third axis (X), wherein the current barrier (5) has at least one opening, and a first width (W1) of the opening of the current barrier (5) along the third axis (X) is smaller than a second width (W2) of the metal p-contact (8) along the third axis (X).
The invention relates to a high-frequency power transistor (1) comprising a transistor (2), at least one capacitor (3) and a housing, which at least partially surrounds the transistor (2) and the capacitor (3). A first connection (4) for a high-frequency input and a gate DC supply is connected to a gate contact (5) of the transistor (2). The problem addressed by the present invention is that of providing a high-frequency power transistor having a behaviour that can be better defined. According to the invention, this problem is solved by virtue of the fact that a second connection (6) is connected to a drain contact (7) of the transistor (2) for a high-frequency output and drain DC supply. A third connection (9) and a fourth connection (10) are connected to a source contact (8) of the transistor (2). The first, second, third and fourth connections (4, 6, 9, 10) all lead out of the housing. The third connection (9) is connected to the source contact (8) via the capacitor (3) and the fourth connection (10) is connected to the source contact (8) via at least one inductive element (36, 11) in such a manner that the third connection (9) provides a high-frequency earth and the fourth connection (10) provides a potential-free low-frequency earth and source DC supply.
The present invention relates to a device for generating laser radiation. A problem addressed by the present invention is that of specifying a device for generating laser radiation using a nonlinear crystal, which device has a simple construction and low optical losses. The device according to the invention comprises an optical amplifier (1) having an active zone (17); wherein the optical amplifier (1) has a front facet (4) and a rear facet (2), between which the active zone (17) extends; and a resonator having a first resonator element (21) and a second resonator element (22), between which the optical amplifier (1) extends, wherein the first resonator element (21) is arranged on a side of the active zone (17) facing away from the front facet (4) and the second resonator element (22) is arranged on a side of the active zone (16) facing the front facet (4), wherein the second resonator element (22) comprises a nonlinear crystal (5, 11) having periodic poling (W5).
Light emitter device based on a photonic crystal with pillar- or wall-shaped semiconductor elements, and methods for the operation and production thereof
3) differ from the first period (d1), the first resonator section (22) forms a light-emitting medium and the third resonator section (24) forms a coupling-out region, through which a part of the light field in the first resonator section (22) can be coupled out of the resonator in a light outcoupling direction parallel to a substrate surface (11) of the substrate (10). Methods for operating and producing the light emitter device (100) are also described.
H01S 5/0625 - Arrangements for controlling the laser output parameters, e.g. by operating on the active medium by varying the potential of the electrodes in multi-section lasers
H01S 5/12 - Construction or shape of the optical resonator the resonator having a periodic structure, e.g. in distributed feedback [DFB] lasers
H01S 5/187 - Surface-emitting [SE] lasers, e.g. having both horizontal and vertical cavities having only horizontal cavities, e.g. horizontal cavity surface-emitting lasers [HCSEL] using Bragg reflection
H01S 5/34 - Structure or shape of the active regionMaterials used for the active region comprising quantum well or superlattice structures, e.g. single quantum well [SQW] lasers, multiple quantum well [MQW] lasers or graded index separate confinement heterostructure [GRINSCH] lasers
H01S 5/11 - Comprising a photonic bandgap structure
H01S 5/02 - Structural details or components not essential to laser action
H01S 5/04 - Processes or apparatus for excitation, e.g. pumping
H01S 5/10 - Construction or shape of the optical resonator
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
43 - Food and drink services, temporary accommodation
Goods & Services
Zoological garden services; Operation of botanical gardens; Running of museums; Organization of exhibitions for cultural or educational purposes; Arranging and conducting seminars and workshops; Arranging and conducting of conferences, concerts and symposiums; Practical training [demonstration]; Tuition; Presentation of films; Photographic reporting. Research services; Scientific testing services. Running of animal care centres; Rental of meeting rooms; Providing food and drink.
55.
Laser device on the basis of a photonic crystal having pillar-shaped or wall-shaped semiconductor elements, and methods for the operation and production thereof
The invention relates to a laser device (100) comprising a substrate (10), on the surface of which an optical waveguide (11) is arranged, which has an optical resonator (12, 13) with such a resonator length that at least one resonator mode forms a stationary wave in the resonator (12, 13), and an amplification medium that is arranged on a surface of the optical waveguide (11), wherein the amplification medium comprises a photonic crystal (20) having a plurality of column- and/or wall-shaped semiconductor elements (21) which are arranged periodically on the surface of the optical waveguide (11) while protruding from the optical waveguide (11), and wherein the photonic crystal (20) is designed to optically interact with the at least one resonator mode of the optical resonator (12, 13) and to amplify light having a wavelength of the at least one resonator mode of the optical resonator (12, 13). The invention also relates to methods for the operation and production of the laser device.
H01S 5/34 - Structure or shape of the active regionMaterials used for the active region comprising quantum well or superlattice structures, e.g. single quantum well [SQW] lasers, multiple quantum well [MQW] lasers or graded index separate confinement heterostructure [GRINSCH] lasers
H01S 5/343 - Structure or shape of the active regionMaterials used for the active region comprising quantum well or superlattice structures, e.g. single quantum well [SQW] lasers, multiple quantum well [MQW] lasers or graded index separate confinement heterostructure [GRINSCH] lasers in AIIIBV compounds, e.g. AlGaAs-laser
41 - Education, entertainment, sporting and cultural services
42 - Scientific, technological and industrial services, research and design
43 - Food and drink services, temporary accommodation
Goods & Services
Zoological garden services; Operation of botanical gardens; Running of museums; Organization of exhibitions for cultural or educational purposes; Arranging and conducting seminars and workshops; Arranging and conducting of conferences, concerts and symposiums; Practical training [demonstration]; Tuition; Presentation of films; Photographic reporting. Research services; Scientific testing services. Running of animal care centres; Rental of meeting rooms; Providing food and drink.
57.
1,2,4-TRIAZOLE DERIVATIVES AS TANKYRASE INHIBITORS
The present invention relates to compounds of formula (I), tautomers, stereoisomers, pharmaceutically acceptable salts and pro-drugs thereof, to processes for their preparation, to pharmaceutical compositions containing such compounds and to their use in therapy wherein a dashed line indicates an optional bond; X represents: a 5- or 6-membered, unsaturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, C1, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), -CN, -NO2, -N(R)2, and -SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); a C3-5 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, C1, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); Y represents: an aryl or heteroaryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); a 5- or 6-membered, saturated heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); or a C3-6 cycloalkyl group optionally substituted by one or more (e.g. 1 or 2) substituents independently selected from C1-6 alkyl (preferably C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), and C1-6 alkoxy (e.g. C1-3 alkoxy); and Z represents: an aryl group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, Cl, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), -CN, -NO2, -N(R)2, and -SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl); or an unsaturated, 5- to 10-membered mono- or bicyclic heterocyclic group optionally substituted by one or more (e.g. 1, 2 or 3) substituents independently selected from halogen (i.e. F, C1, Br, I), C1-6 alkyl (e.g. C1-3 alkyl), C1-6 haloalkyl (e.g. C1-3 haloalkyl), C1-6 alkoxy (e.g. C1-3 alkoxy), -CN, -NO2, -N(R)2, and -SO2R (where each R is independently H or C1-6 alkyl, e.g. H or C1-3 alkyl). These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
1-61-31-61-31-61-3221-61-33-51-61-31-61-31-61-31-61-3 1-61-31-61-31-61-31-61-31-61-31-6 1-31-61-31-61-33-61-61-31-61-31-61-31-61-31-61-31-61-32221-61-31-61-31-61-31-61-32221-61-31-3 alkyl). These compounds find particular use in the treatment and/or prevention of a disease or disorder responsive to inhibition of tankyrase 1 and/or 2, for example a disorder which is mediated by tankyrase 1 and/or 2 such as cancer.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
The present application relates to compounds of formula (1) and their use as medicament, in particular for the treatment of a medical condition associated with defective PI3K signalling.
The present application relates to compounds of formula (1) and their use as medicament, in particular for the treatment of a medical condition associated with defective PI3K signalling.
The present invention provides means and methods for equipping a polypeptide of interest at its C-terminus with a versatile adaptor amino acid that allows the functionalization of the polypeptide of interest.
Disclosed are novel conjugates and processes for the preparation thereof. A process tor the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III), with an azide of formula (IV), to prepare a compound of formula (V), reacting a compound of formula (V) with a thiol-containing molecule of formula (VI), resulting in a compound of formula (VII).
C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene-or alkyne-phosohonothiolates and -phosphonates comprises the step of: reacting a compound of formula (I) with a thiol-containing molecule of formula (II) wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, an optionally substituted C1-C8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5-or 6- membered heterocyclic system; resulting in a compound of formula (III)..
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
C07K 5/00 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof
C07K 7/00 - Peptides having 5 to 20 amino acids in a fully defined sequenceDerivatives thereof
C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
64.
Selective inhibitors of gentotoxic steress-induced IKK/NF-κB pathways
Max-Delbrück-Centrum für Molekulare Medizin in der Helmholtz-Gemeinschaft (Germany)
Forschungsverbund Berlin e.V (Germany)
Inventor
Scheidereit, Claus
Willenbrock, Michael
Lindemann, Peter
Radetzki, Silke
Von Kries, Jens-Peter
Nazare, Marc
Abstract
A method is for treatment of a disease associated with genotoxic stress-induced inhibitor of nuclear factor-κB kinase/nuclear factor kappa-light chain enhancer of activated B cells (IKK/NF-κB) signaling. The method can include administering a compound to a subject having a cancer exhibiting genotoxic stress induced IKK/NF-κB activation.
188-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5-or 6- membered heterocyclic system; resulting in a compound of formula (III)..
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
66.
SEMICONDUCTOR DEVICE WITH AT LEAST ONE FUNCTIONAL ELEMENT CONTAINING MULTIPLE ACTIVE REGIONS, AND METHOD OF MANUFACTURING THEREOF
A semiconductor device (100), in particular being configured for optical, optoelectronic,electronic and/or (photo-)electrochemical applications, comprises a substrate (10) and at least one nano-or microstructure functional element (20) standing on the substrate (10) and having a core region (21) extending in an upward direction deviating from a substrate plane, wherein the at least one functional element (20) further includes multiple different active regions (22, 22A, 23, 23A, 24 and 24A) being located on different lateral sides of the core region (21) having surface normals being directed in different azimuthal directions but having a common polar angle with reference to the substrate plane, in particular in different directions parallel to the substrate plane, wherein the active regions (22, 22A, 23, 23A, 24 and 24A) have different optical, optoelectronic, electronic and/or or (photo-)electrochemical properties.Furthermore, a method of manufacturing the semiconductor device (100) is described..
H01L 33/08 - SEMICONDUCTOR DEVICES NOT COVERED BY CLASS - Details thereof characterised by the semiconductor bodies with a plurality of light emitting regions, e.g. laterally discontinuous light emitting layer or photoluminescent region integrated within the semiconductor body
H01L 33/20 - SEMICONDUCTOR DEVICES NOT COVERED BY CLASS - Details thereof characterised by the semiconductor bodies with a particular shape, e.g. curved or truncated substrate
H01L 33/00 - SEMICONDUCTOR DEVICES NOT COVERED BY CLASS - Details thereof
H01L 33/38 - SEMICONDUCTOR DEVICES NOT COVERED BY CLASS - Details thereof characterised by the electrodes with a particular shape
H01L 33/32 - Materials of the light emitting region containing only elements of group III and group V of the periodic system containing nitrogen
The invention relates to chemical compounds that can be used in particular as structural mimetics of proline-rich peptides. The compounds of the invention are capable of selectively inhibiting ena/VASP-EVH1-mediated protein-protein interactions. The invention further relates to the use of said compounds as pharmaceutical active substances and to the use of the pharmaceutical active substances to treat tumor diseases.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
A nanoelement device 100 is disclosed, which comprises at least one nanoelement 10, like a nan- owire or nanowall, standing on a substrate 20 with a planar extension, wherein the at least one nanoelement 10 includes a core region 11 having at least one lateral side surface with an extension along a longitudinal core shape from a foot section 12 to a head section 13 of the at least one nanoelement, and a bending region 14 being configured on the at least one side surface of the core region 11, such that strain is induced in the at least one nanoelement 10 and the at least one nanoelement 10 has a curved shape with a bending angle between the directions of the foot section 12 and the head section 13, and wherein the at least one nanoelement 10 has a predetermined bending direction being set by the configuration of the bending region 14 and being select¬ ed such that the at least one nanoelement 10 is bent towards a neighboring nanoelement 10 on the substrate 20 and/or a predetermined coupling section 25 of the substrate 20, and the at least one nanoelement 10 electrically and/or optically couples with the neighboring nanoelement 10 and/or the coupling section 25 of the substrate 20. Furthermore, methods of manufacturing the nanoelement device are disclosed.
The invention relates to a laser module (LM) comprising a housing and, in the housing, a coolable laser source (LQ) for generating a laser beam and a gas cell (GZ) filled with gas for stabilizing a line width and/or a wavelength of the laser beam. The housing is designed to protect against condensation water, and the laser source (LQ) comprises a master oscillator (MO), an optical amplifier (PA) and an optical insulator (IS1) arranged between the master oscillator (MO) and the optical amplifier (PA). According to the invention, the laser module makes it possible to provide a miniaturized laser having a stable wavelength and/or line width, in a robust manner.
The invention relates to a device (CAP) for disinfecting liquid in a vessel (BOT), which device comprises the following: at least one light source (LUX) for ultraviolet light and a control unit (CON) for switching the light source (LUX) on and off, characterised by a movement detector (BWS), the control unit (CON) being designed not to switch the light source (LUX) on if the movement detector (BWS) does not detect movement. It is advantageous if the user is actually forced to shake the vessel to carry out the disinfection process. The user thus ensures that the mixture is always thoroughly mixed such that sufficient irradiation of all regions of the liquid volume is guaranteed.
MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Bader, Michael
Specker, Edgar
Matthes, Susann
Schütz, Anja
Mallow, Keven
Grohmann, Maik
Nazaré, Marc
Abstract
The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative.
The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
The present invention relates to a gate structure and to a method for producing same. In particular, the present invention relates to a gate structuring of a field effect transistor (FET), wherein the field effect transistor, for the same active layer, can be constructed as depletion type (or "D-type"), as enhancement type (or "E-type") and/or as low noise type (or "LN-type") on a common substrate base in a uniform method. The gate structure according to the invention comprises a substrate; a piezoelectric active layer (112, 212) arranged on the substrate (110, 210); a passivation layer (120, 220) arranged on the active layer (112, 212), wherein the passivation layer (120, 220) has a cutout (122, 222) extending through the entire passivation layer (120, 220) in the direction of the active layer (112, 212); a contact element (140, 240) arranged within the cutout (122, 222), wherein the contact element (140, 240) extends from the active layer (112, 212) to above the passivation layer (120, 220); and a cover layer (150, 250) covering the contact element (140, 240) above the passivation layer (120, 220); wherein at least one layer arranged above the active layer, in the region around the contact element, is embodied under tensile or compressive stress with a normal stress |σ| > 200 MPa, wherein by way of the individual stresses in the region around the contact element a resultant force is set at the interface between passivation layer and active layer, which force influences the electron density in the active layer in the region below the contact element by way of the piezoelectric effect.
H01L 29/778 - Field-effect transistors with two-dimensional charge carrier gas channel, e.g. HEMT
H01L 23/29 - Encapsulation, e.g. encapsulating layers, coatings characterised by the material
H01L 29/20 - Semiconductor bodies characterised by the materials of which they are formed including, apart from doping materials or other impurities, only AIIIBV compounds
Chemical compounds are useful in the treatment of a subject afflicted by a thyroid disease. The compounds exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and can be used in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61P 5/14 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
The invention relates to a device (100) for controlling a self-conducting n-channel output stage field effect transistor (V1), comprising a control signal input (110), a control signal output (120) for connection to a gate electrode (V1G) of the output stage field effect transistor (V1), a first node (N1), which is connected to the control signal output (120), a second node (N2) and first transistor (V4). A source electrode (V4S) of the first transistor (V4) is connected to the first node (N1), a gate electrode (V4G) of the first transistor (V4) is connected to the second node (N2) and a drain electrode (V4D) of the first transistor (V4) is connected either to the source electrode of the output stage field effect transistor (V1) or to a supply voltage (+Vdd). A resistor (R1), with one end thereof, is connected to the second node (N2). The device (100) is characterised in that the resistor (R1), with the other end thereof, is connected to the first node (N1). Use of the first transistor (V4) can thus ensure that the supply voltage (Vdd) is present on the control signal output when a low-level signal is present on the control signal input (110).
H03F 1/02 - Modifications of amplifiers to raise the efficiency, e.g. gliding Class A stages, use of an auxiliary oscillation
H03K 17/06 - Modifications for ensuring a fully conducting state
H03K 17/687 - Electronic switching or gating, i.e. not by contact-making and -breaking characterised by the use of specified components by the use, as active elements, of semiconductor devices the devices being field-effect transistors
H03F 3/21 - Power amplifiers, e.g. Class B amplifiers, Class C amplifiers with semiconductor devices only
H03F 3/217 - Class D power amplifiersSwitching amplifiers
77.
FOURIER SPECTROMETER HAVING A MULTI-MODE QUANTUM CASCADE LASER, AND METHOD FOR SPECTROSCOPIC ANALYSIS OF A SAMPLE
The invention relates to a Fourier spectrometer for spectroscopically analysing a sample, comprising: a multi-mode quantum cascade laser (QCL) that has an active QCL region in a laser resonator, which is configured to generate laser light with emission frequencies according to a plurality of resonator modes of said laser resonator, an excitation device configured to electrically excite said active QCL region using an electric pump current, and a tuning device by means of which the resonator modes can be set; an interferometer for producing an interferogram on the basis of the laser light; a detector device for detecting the interferogram following interaction with the sample and for acquiring a detector signal containing the detected interferogram, within a detector measuring time; and an evaluation device that is configured to acquire a spectrum of the sample using a Fourier transform of the detected interferogram. The QCL tuning device is designed to periodically and spectrally vary the resonator modes, with a tuning time period of less than 1 minute, in a spectral tuning interval which is at least equal to the spacing between consecutive resonator modes of the laser resonator, the active QCL region is configured to generate laser light with emission frequencies in the range of 1 THz to 6 THz, wherein the emission frequencies of the laser light cover a spectral emission range of at least 50 GHz, and the detector device is designed to temporally average the detector signal over the tuning time period of the QCL tuning device. The invention also relates to a method for spectroscopically analysing a sample using the spectrometer.
H01S 5/34 - Structure or shape of the active regionMaterials used for the active region comprising quantum well or superlattice structures, e.g. single quantum well [SQW] lasers, multiple quantum well [MQW] lasers or graded index separate confinement heterostructure [GRINSCH] lasers
The present invention relates to a radiation detector and a method for producing same. In particular, the present invention relates to a radiation detector for detecting THz radiation on the basis of a field effect transistor (FET) with an antenna structure that is monolithically integrated at the FET structure, and to a method for producing such a monolithically integrated detector arrangement. A radiation detector (100) according to the invention comprises an antenna structure (10); and a field effect transistor, FET, structure (20) with a source region (24), a gate region (26) and a drain region (28), these regions (24, 26, 28) being arranged on a substrate (70) and forming electrically conductive electrode structures (34, 36, 38) independently of one another by way of a metallization, and the gate electrode structure (36) completely surrounding the source electrode structure (34) or the drain electrode structure (38) in a first plane (E1); the surrounded electrode structure (34, 38) extends to above the gate electrode structure (36) and there areally covers, at least in portions, the surrounding structure in a second plane (E2) above the first plane (E1); and an electrically insulating region (42) for forming a capacitor (40) with a metal-insulator-metal, MIM, structure is arranged between the regions of the gate electrode structure (36) that are covered by the surrounded electrode structure (34, 38). The method according to the invention for producing a radiation detector (100) is suited to producing particularly preferred embodiments of a radiation detector (100) according to the invention.
H01L 31/02 - SEMICONDUCTOR DEVICES NOT COVERED BY CLASS - Details thereof - Details
H01L 31/112 - Devices sensitive to infrared, visible or ultraviolet radiation characterised by field-effect operation, e.g. junction field-effect photo- transistor
H01Q 1/22 - SupportsMounting means by structural association with other equipment or articles
H01Q 9/28 - Conical, cylindrical, cage, strip, gauze or like elements having an extended radiating surface Elements comprising two conical surfaces having collinear axes and adjacent apices and fed by two-conductor transmission lines
H01Q 23/00 - Antennas with active circuits or circuit elements integrated within them or attached to them
H01L 29/04 - Semiconductor bodies characterised by their crystalline structure, e.g. polycrystalline, cubic or particular orientation of crystalline planes
The present invention relates to a laser diode having an improved mode profile. In particular, the present invention relates to a broad stripe semiconductor laser based on an extreme double asymmetric structure (EDAS), wherein, by means of an optimized mode profile having an improved mode confinement, the leakage current rates and the series resistance can be lowered and the charge carrier density within the light-guiding waveguide and the active zone can be reduced. The diode laser according to the invention comprises a first cladding layer (14) of n-conducting configuration, a first waveguide layer (12) of n-conducting configuration, which is arranged on the first cladding layer (14), an active layer (10), which is suitable for generating radiation and which is arranged on the first waveguide layer (12), a second waveguide layer (16) of p-conducting configuration, which is arranged on the active layer (10), a second cladding layer (18) of p-conducting configuration, which is arranged on the second waveguide layer (16), wherein a first intermediate layer (11) of n-conducting configuration is configured as a transition region between the first waveguide layer (12) and the active layer (10), and a second intermediate layer (15) of p-conducting configuration is configured as a transition region between the second waveguide layer (16) and the active layer (10). In this case, the diode laser according to the invention is characterized in that the asymmetry ratio of the thickness of the first intermediate layer (11) to the sum of the thickness of the first intermediate layer (11) and the thickness of the second intermediate layer (15) is less than or greater than 0.5.
H01S 5/20 - Structure or shape of the semiconductor body to guide the optical wave
H01S 5/32 - Structure or shape of the active regionMaterials used for the active region comprising PN junctions, e.g. hetero- or double- hetero-structures
The present invention relates to compounds of formula (I'), tautomers, stereoisomers, and pharmaceutically acceptable salts thereof, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy (I') (wherein: Z represents an optionally substituted, 5- or 6-membered unsaturated heterocyclic group comprising at least one nitrogen atom; L represents a 4-, 5- or 6-membered cycloalkyl group, preferably a cyclobutyl group; each R1 independently represents F, CI, Br, I, C1-3 alkyl, C1-3 haloalkyl (e.g. -CF3), -CN, -OH or -NO2, preferably F, CI, Br or 1, e.g. CI or F; each R2independently represents F, CI, Br, I, C1-3 alkyl, -CN, -OH or -NO2, preferably F, CI, Br, I or -CN, e.g. F or -CN; X represents -NR3- or -0-; R3 represents H or a C1-3 alkyl group (e.g. methyl); n is an integer from 0 to 5, preferably 0 to 3, more preferably 0, 1 or 2, e.g 1; and m is an integer from 0 to 5, preferably 0 to 3, more preferably 0, 1 or 2, e.g. 0 or 1). These compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the WNT pathway and increased presence of nuclear β-catenin. For example, these may be used in preventing and/or retarding proliferation of tumor cells and metastasis, for example carcinomas such as colon carcinomas.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
LIGHT EMITTER DEVICE BASED ON A PHOTONIC CRYSTAL WITH PILLAR- OR WALL-SHAPED SEMICONDUCTOR ELEMENTS, AND METHODS FOR THE OPERATION AND PRODUCTION THEREOF
A light emitter device (100) comprises a substrate (10) and a photonic crystal (20), which is arranged on the substrate (10) and comprises pillar- and/or wall-shaped semiconductor elements (21), which are arranged periodically standing out from the substrate (10), wherein the photonic crystal (20) forms a resonator, in which the semiconductor elements (21) are arranged in a first resonator section (22) with a first period (d1), in a second resonator section (23) with a second period (d2) and in a third resonator section (24) with a third period (d3), wherein on the substrate (10) the second resonator section (23) and the third resonator section (24) are arranged on two mutually opposing sides of the first resonator section (22) and the second period (d2) and the third period (d3) differ from the first period (d1), the first resonator section (22) forms a light-emitting medium and the third resonator section (24) forms a coupling-out region, through which a part of the light field in the first resonator section (22) can be coupled out of the resonator in a light outcoupling direction parallel to a substrate surface (11) of the substrate (10). Methods for operating and producing the light emitter device (100) are also described.
H01S 5/10 - Construction or shape of the optical resonator
82.
LASER DEVICE ON THE BASIS OF A PHOTONIC CRYSTAL HAVING COLUMN- OR WALL-SHAPED SEMICONDUCTOR ELEMENTS, AND METHODS FOR THE OPERATION AND PRODUCTION THEREOF
The invention relates to a laser device (100) comprising a substrate (10), on the surface of which an optical waveguide (11) is arranged, which has an optical resonator (12, 13) with such a resonator length that at least one resonator mode forms a stationary wave in the resonator (12, 13), and an amplification medium that is arranged on a surface of the optical waveguide (11), wherein the amplification medium comprises a photonic crystal (20) having a plurality of column- and/or wall-shaped semiconductor elements (21) which are arranged periodically on the surface of the optical waveguide (11) while protruding from the optical waveguide (11), and wherein the photonic crystal (20) is designed to optically interact with the at least one resonator mode of the optical resonator (12, 13) and to amplify light having a wavelength of the at least one resonator mode of the optical resonator (12, 13). The invention also relates to methods for the operation and production of the laser device.
H01S 5/02 - Structural details or components not essential to laser action
H01S 5/34 - Structure or shape of the active regionMaterials used for the active region comprising quantum well or superlattice structures, e.g. single quantum well [SQW] lasers, multiple quantum well [MQW] lasers or graded index separate confinement heterostructure [GRINSCH] lasers
H01S 5/10 - Construction or shape of the optical resonator
The present invention relates to a gate structure and to a method for producing same. In particular, the present invention relates to the gate structuring of a field effect transistor having reduced thermomechanical loading and increased reliability (reduced electromigration or diffusion of the gate metal). The gate structure according to the invention comprises a substrate (10); an active layer (20) arranged on the substrate (10); an intermediate layer (40) arranged on the active layer (20), wherein the intermediate layer (40) has a cutout (45) extending through the entire intermediate layer (40) in the direction of the active layer (20); and a contact element (50) arranged within the cutout (45), wherein the contact element (50) completely fills the cutout (45) and extends to above the intermediate layer (40), wherein the contact element (50), at least in sections, bears directly on the intermediate layer (40); wherein the contact element (50) is constructed from a Schottky metal (52) and the contact element (50) has internally a cavity (55) enclosed completely by the Schottky metal (52).
MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZIN IN DER HELMHOLTZ-GEMEINSCHAF (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Scheidereit, Claus
Willenbrock, Michael
Lindemann, Peter
Radetzki, Silke
Von Kries, Jens Peter
Nazare, Marc
Abstract
A compound according to Formula I or a pharmaceutically acceptable salt thereof is disclosed for use in the treatment of a subject suffering from cancer exhibiting genotoxic stress-induced IKK/NF-kB activation.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN IN DER HELMHOLTZ-GEMEINSCHAFT (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Scheidereit, Claus
Willenbrock, Michael
Lindemann, Peter
Radetzki, Silke
Von Kries, Jens Peter
Nazare, Marc
Abstract
The invention relates to chemical compounds and their use as a medicament in the treatment of a disease associated with genotoxic stress-induced I KK/NF-κΒ (NF-kappaB) activation, preferably in the treatment of a subject suffering from cancer exhibiting genotoxic stress-induced I KK/NF-κΒ activation. The invention further relates to a pharmaceutical composition comprising a compound of the invention for the treatment of a subject afflicted by a disease associated with genotoxic stress-induced I KK/NF-κΒ activation.
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
The invention relates to an optical pulse generator and to a method for operating an optical pulse generator. The invention particularly relates to an optical pulse generator for high-frequency (HF)-pulse width modulation in LiDAR systems. The optical pulse generator according to the invention comprises: an active optical component (10) designed to emit optical radiation, the optical component (10) comprising contact surfaces (12, 14) for electrical contacting; a means for the electronic control (20) of the optical component (10), designed to excite the optical component (10) to generate a pulsed emission of optical radiation, the means for electronic control (20) comprising contact surfaces (22, 24) for electrical contacting; a first module carrier (30), the means for electronic control (20) being arranged on the first module carrier (30); and a second module carrier (40), the optical component (10) being arranged on the second module carrier. The optical pulse generator according to the invention is characterised in that the optical component (10) is arranged between the first module carrier (30) and the second module carrier (40), at least one contact surface (22, 24) of the means for electronic control (20) being connected to at least one contact surface (12, 14) of the optical component (10), either directly or by means of solder points. The method according to the invention for operating an optical pulse generator is based on an application of the optical pulse generator according to the invention.
G01R 1/04 - HousingsSupporting membersArrangements of terminals
H01L 27/15 - Devices consisting of a plurality of semiconductor or other solid-state components formed in or on a common substrate including semiconductor components with at least one potential-jump barrier or surface barrier, specially adapted for light emission
87.
CHEMOSELECTIVE THIOL-CONJUGATION WITH ALKENE OR ALKYNE-PHOSPHONAMIDATES
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III), with an azide of formula (IV), to prepare a compound of formula (V), reacting a compound of formula (V) with a thiol-containing molecule of formula (VI), resulting in a compound of formula (VII).
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07F 9/6553 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having sulfur atoms, with or without selenium or tellurium atoms, as the only ring hetero atoms
C07K 1/107 - General processes for the preparation of peptides by chemical modification of precursor peptides
C07K 1/113 - General processes for the preparation of peptides by chemical modification of precursor peptides without change of the primary structure
C07K 7/52 - Cyclic peptides containing at least one abnormal peptide link with only normal peptide links in the ring
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
88.
CHEMOSELECTIVE THIOL-CONJUGATION WITH ALKENE OR ALKYNE-PHOSPHONAMIDATES
Disclosed are novel conjugates and processes for the preparation thereof. A process for the preparation of alkene- or alkyne-phosphonamidates comprises the steps of (I) reacting a compound of formula (III), with an azide of formula (IV), to prepare a compound of formula (V), reacting a compound of formula (V) with a thiol-containing molecule of formula (VI), resulting in a compound of formula (VII).
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
The invention relates to a waveguide structure and an optical system with a waveguide structure. The waveguide structure (100) according to the invention comprises a first waveguide region (10), which has a constant first width (w1) and is designed to guide electromagnetic waves along the longitudinal axis (L10) of the region so as to maintain the mode, and a second waveguide region (20), which is designed to guide electromagnetic waves along the longitudinal axis (L20) of the region so as to maintain the mode. The longitudinal axis (L10) of the first waveguide region (10) and the longitudinal axis (L20) of the second waveguide region (20) form a common longitudinal axis (L 10, L 20) of the waveguide structure (100), and a first end surface of the first waveguide region (10) and a first end surface of the second waveguide region (20) are oriented towards each other. The width of the first end surface of the second waveguide region (20) corresponds to the first width (w1), and the width (w) of the second waveguide region (20) along the longitudinal axis (L20) of the second waveguide region expands to a second width (w2) which is larger than the first width (w1) from the first end surface to a second end surface. The waveguide structure also comprises a grid (40) with a plurality of webs (42) and trenches (44), wherein the grid (40) is arranged in the second waveguide region (20) along the common longitudinal axis (L10, L20).
MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Bader, Michael
Specker, Edgar
Matthes, Susann
Schütz, Anja
Mallow, Keven
Grohmann, Maik
Nazaré, Marc
Abstract
The invention relates to a xanthine derivative defined by chemical formula I or a salt thereof, its use as a medicament, especially for use in the treatment of serotonin-related diseases or disorders, and a pharmaceutical preparation comprising the xanthine derivative. The novel xanthine compounds are capable of inhibiting tryptophan hydroxylases (TPH) involved in the biosynthesis of serotonin and are effective in influencing the serotonin level in the body.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
91.
MOLECULAR SENSOR FOR NMR/MRI BASED ON ANALYTE-DEPENDENT SPECTRAL CHANGES OF TEMPORARILY ENCAPSULATED HYPERPOLARIZED 129XE
KLINIKUM RECHTS DER ISAR DER TECHNISCHEN UNIVERSITÄT MÜNCHEN (Germany)
FORSCHUNGSVERBUND BERLIN E.V. (Germany)
Inventor
Westmeyer, Gil Gregor
Truong, Dong-Jiunn Jeffery
Schröder, Leif
Rossella, Federica
Witte, Christopher
Abstract
The present invention relates to a precursor of a molecular sensor for determining analyte concentrations and/or measuring analyte concentration changes comprising a host for an active nucleus, an NMR-modulating moiety and an interacting moiety, wherein said NMR- modulating moiety changes the resonance frequency or the chemical exchange saturation transfer (CEST) signal of the active nucleus-host complex, and wherein said interacting moiety specifically responds to an environmental parameter, to an analyte or to a target molecule that binds the analyte or said interacting moiety specifically binds to a target molecule in an analyte-dependent manner. The present invention further relates to a molecular sensor comprising an active nucleus and said precursor. The present invention further relates to a molecular sensor for determining analyte concentrations and/or measuring analyte concentration changes inside a cell, wherein moiety/ies of the sensor are expressed in said cells and then assembled inside said cell. The present invention further relates to uses of the molecular sensors as well as to an in vitro method for determining metal concentration and/or measuring metal concentration changes and a method for diagnosing and/or monitoring treatment of diseases causing changes in metal concentrations.
The method comprises radiating excitation radiation (12, R1, R2) onto a sample (20) to be examined, wherein the sample (20) to be examined is irradiated at least with first excitation radiation (R1) of a first excitation wavelength (λ1) and second excitation radiation (R2) of a second excitation wavelength (λ2), wherein at least the first excitation wavelength (λ1) differs from the second excitation wavelength (λ2). Furthermore, wavelength-selective filtering of the first excitation radiation (R1') scattered by the sample (20) is carried out by means of a passive filter element (30), wherein a transmitted filter wavelength (λF) of the filter element (30) differs from at least the first excitation wavelength (λ1) and the second excitation wavelength (λ2), and wherein a first intensity (I1) is determined from the filtered first excitation radiation (R1") scattered by the sample (20) by means of a detector (40) assigned to the filter wavelength (λF). In addition, wavelength-selective filtering of the second excitation radiation (R2') scattered by the sample (20) is carried out by means of the filter element (30), wherein a second intensity (l2) is determined from the filtered second excitation radiation (R2) scattered by the sample (20) by means of the detector (40) assigned to the filter wavelength (λF).
3 single crystal from the melt at the growth temperature (GT) the growth oxygen concentration value (C2, C2′, C2″) is maintained within the oxygen concentration range (SC).
The present invention provides means and methods for equipping a polypeptide of interest at its C-terminus with a versatile adaptor amino acid that allows the functionalization of the polypeptide of interest.
The present invention relates to chemical compounds that can in particular be used as structural mimetics of proline-rich peptides. The compounds of the present invention are capable of selectively inhibiting ena/VASP-EVH1-mediated protein-protein interactions. The invention further relates to the use of said compounds as pharmaceutical agents and to the use of the pharmaceutical agents to treat tumor diseases. The chemical compounds of the present invention can significantly inhibit the chemotaxis and motility of invasive tumor cells and can therefore be used in the treatment and/or prevention of tumor metastases.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
C07K 7/06 - Linear peptides containing only normal peptide links having 5 to 11 amino acids
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
The invention relates to chemical compounds that are useful in the treatment of a subject afflicted by a thyroid disease, in particular to compounds that exhibit activity as thyroid-stimulating hormone receptor (TSHR) antagonists and their use in the treatment of hyperthyroidism, Graves' disease, Graves' Ophthalmopathy and thyroid cancer.
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61P 5/14 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
The present invention relates to a modulator for a digital amplifier and to an apparatus having such a modulator and a digital amplifier. The modulator (100) comprises a pulse former (110) and a control unit (120) for controlling the pulse former (110) for the purpose of converting an input signal into a bit stream (130) which is configured for a digital amplifier and codes an amplitude value for each clock pulse of a carrier signal. The pulse former (110) may represent a particular amplitude value of the input signal with different bit patterns. The bit pattern respectively used by the pulse former is determined by the control unit (120) on the basis of a corresponding associated control command. The modulator (100) is characterized in that an assignment (160) of the control commands to associated amplitude values resulting from amplification of the associated bit patterns using the digital amplifier (400) is stored in the control unit (120) or provision is at least made for the control unit (120) to select a control command for each clock pulse on the basis of the assignment (160) and the amplitude value of the input signal and to accordingly control the pulse former (110).
Described is a light-emitting semiconductor device (100) comprising at least one nanowire (10) having at least one (AI xGa1-xN)-based nanowire portion (12), where 0 ≤ x ≤ 1, and extending along an axial direction (z), wherein the nanowire (10) has at least one InN-based quantum dot (11), which is delimited at least on one side along the axial direction (z) by the at least one nanowire portion (12) of the nanowire (10), and the nanowire (10) has a thickness less than or equal to a critical thickness, at which the at least one quantum dot (11) and the adjacent nanowire portion (12) adjoin one another without dislocation. A method for producing the light-emitting semiconductor device (100) is also described.
H01L 33/06 - SEMICONDUCTOR DEVICES NOT COVERED BY CLASS - Details thereof characterised by the semiconductor bodies with a quantum effect structure or superlattice, e.g. tunnel junction within the light emitting region, e.g. quantum confinement structure or tunnel barrier
H01L 33/18 - SEMICONDUCTOR DEVICES NOT COVERED BY CLASS - Details thereof characterised by the semiconductor bodies with a particular crystal structure or orientation, e.g. polycrystalline, amorphous or porous within the light emitting region