RESEARCH CENTER PHARMACEUTICAL ENGINEERING GMBH (Austria)
Inventor
Kappe, Oliver
Sommer, Florian
Cantillo, David
Abstract
The present disclosure relates to an electrochemical reactor capable of processing an organic mixture comprising a suspension of a solid and a liquid, wherein the electrochemical reactor comprises an inner electrode, an outer electrode, wherein the inner electrode and the outer electrode are arranged concentrically forming a first cavity therebetween, a first inlet configured for introducing the liquid into the first cavity of the electrochemical reactor, a second inlet configured for introducing the solid into the first cavity of the electrochemical reactor, wherein the first inlet and the second inlet are arranged such that the liquid and the solid are introduced separately, wherein the inner electrode is configured to be rotatable around its longitudinal axis, wherein the inner electrode comprises one or more mixing elements. The present disclosure further relates to processes for the electrochemical N-demethylation and N- and O-demethylation, respectively, of an opioid precursor by means of the electrochemical reactor. The present disclosure further relates to a one-pot process for the N- and O-demethylation of an opioid precursor.
The invention relates to a process for cleaving and at least partially recycling the starting components of a thermosetting epoxy resin which is a polymerisation product of a dicarboxylic acid diglycidyl ester of formula (I) and a diamine of formula (II): (I) wherein R11-2022N-R222 (II) wherein R21-201-20 alkylene group, but the two amino groups are not directly bonded to aromatic rings; the thermosetting epoxy resin having substantially the following structure: (III) wherein the wavy lines each symbolise the attachment of the nitrogen atom to a further 2-hydroxypropylene moiety; the process comprising the following steps a) to e): a) an alcoholysis of the resin to obtain the corresponding diester of the dicarboxylic acid according to formula (I) in question and the 2,3-dihydroxypropyl group-substituted diamine of formula (II) ("polyol") in question: polyol; b) an acetolysis at elevated temperature to obtain the acetamides of the diamines of formula (II) ("diamide") and of triacetin: triacetin diamide; c) the deacetylation of the diamide to obtain the diamine monomer of formula (II); d) the deacetylation of triacetin to obtain glycerol, which is subsequently converted to glycidol; and e) the transesterification of the diester obtained in step a) with the glycidol obtained in step d) to obtain the dicarboxylic acid diglycidyl ester of formula (I) in question; and furthermore a process for the preparation of such thermosetting epoxy resins and new resins prepared in this way.
C07C 31/22 - Trihydroxylic alcohols, e.g. glycerol
C07C 69/18 - Acetic acid esters of trihydroxylic compounds
C07C 211/36 - Compounds containing amino groups bound to a carbon skeleton having amino groups bound to carbon atoms of rings other than six-membered aromatic rings of a saturated carbon skeleton containing at least two amino groups bound to the carbon skeleton
C07C 215/14 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic the nitrogen atom of the amino group being further bound to hydrocarbon groups substituted by amino groups
C07C 233/41 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a ring other than a six-membered aromatic ring
C07C 67/18 - Preparation of carboxylic acid esters by conversion of a group containing nitrogen into an ester group
C07C 209/62 - Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
C07C 213/00 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
C07C 231/02 - Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
A01N 25/00 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of applicationSubstances for reducing the noxious effect of the active ingredients to organisms other than pests
A01N 65/36 - Rutaceae [Rue family], e.g. lime, orange, lemon, corktree or pricklyash
Sulfonate compounds according to formula (I) or (II), a preparation method, and their use as surfactants are provided.
Sulfonate compounds according to formula (I) or (II), a preparation method, and their use as surfactants are provided.
Sulfonate compounds according to formula (I) or (II), a preparation method, and their use as surfactants are provided.
Each R1 is selected from hydrocarbon radicals having 4 to 26 C atoms and optionally at least one O or S atom; R2 to R5 are each independently selected from hydrogen and hydrocarbon radicals having 1 to 26 C atoms and optionally at least one O or S atom; each R6 is independently selected from hydrogen and hydrocarbon radicals having 1 to 6 carbon atoms, optionally the two radicals R6 may be connected, as indicated by the dashed line, to form a five-or six-membered ring containing the carbonyl carbon atom; and each X is independently selected from mono-or polyvalent cations Xn+, wherein n is ≥1, including H+, wherein, in formula (I), optionally both X together may represent a polyvalent cation.
Amine N-oxide compounds having formula (I) or (II), a preparation method, and a surfactant containing the compounds:
Amine N-oxide compounds having formula (I) or (II), a preparation method, and a surfactant containing the compounds:
Amine N-oxide compounds having formula (I) or (II), a preparation method, and a surfactant containing the compounds:
R1 is a hydrocarbon residue with 4 to 26 carbon atoms and optionally at least one O or S; R2, R3 and R5 are each hydrogen, R1—O—, R8 and in formula (I) also optionally —CH2—N+(O−)R6R6; R8 is a hydrocarbon radical with 1 to 26 carbon atoms and optionally at least one O or S; R4 is hydrogen or R8; and each R6 is a hydrocarbon radical with 1 to 6 carbon atoms and optionally at least one N, O or S. Optionally two radicals R6 on the same nitrogen atom are connected to form a five- or six-membered, nitrogen-containing ring, or optionally radical(s) R6 of a moiety —N+(O−)R6R6 may be linked to radical(s) R6 of another formula (I) molecule, forming a bridge having the structure
Amine N-oxide compounds having formula (I) or (II), a preparation method, and a surfactant containing the compounds:
R1 is a hydrocarbon residue with 4 to 26 carbon atoms and optionally at least one O or S; R2, R3 and R5 are each hydrogen, R1—O—, R8 and in formula (I) also optionally —CH2—N+(O−)R6R6; R8 is a hydrocarbon radical with 1 to 26 carbon atoms and optionally at least one O or S; R4 is hydrogen or R8; and each R6 is a hydrocarbon radical with 1 to 6 carbon atoms and optionally at least one N, O or S. Optionally two radicals R6 on the same nitrogen atom are connected to form a five- or six-membered, nitrogen-containing ring, or optionally radical(s) R6 of a moiety —N+(O−)R6R6 may be linked to radical(s) R6 of another formula (I) molecule, forming a bridge having the structure
Amine N-oxide compounds having formula (I) or (II), a preparation method, and a surfactant containing the compounds:
R1 is a hydrocarbon residue with 4 to 26 carbon atoms and optionally at least one O or S; R2, R3 and R5 are each hydrogen, R1—O—, R8 and in formula (I) also optionally —CH2—N+(O−)R6R6; R8 is a hydrocarbon radical with 1 to 26 carbon atoms and optionally at least one O or S; R4 is hydrogen or R8; and each R6 is a hydrocarbon radical with 1 to 6 carbon atoms and optionally at least one N, O or S. Optionally two radicals R6 on the same nitrogen atom are connected to form a five- or six-membered, nitrogen-containing ring, or optionally radical(s) R6 of a moiety —N+(O−)R6R6 may be linked to radical(s) R6 of another formula (I) molecule, forming a bridge having the structure
and a dimer of formula (II).
C07C 209/60 - Preparation of compounds containing amino groups bound to a carbon skeleton by condensation or addition reactions, e.g. Mannich reaction, addition of ammonia or amines to alkenes or to alkynes or addition of compounds containing an active hydrogen atom to Schiff's bases, quinone imines, or aziranes
C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
C07D 211/94 - Oxygen atom, e.g. piperidine N-oxide
142354511010 group, wherein the at least one compound represented by Formula (I) is administered to a subject in an amount of 200 µg/kg body weight to 8000 µg/kg body weight.
Disclosed is a peptide comprising a variant of the amino-acid sequence IGKEFKRIVERKKRFLRELVRPLR (SEQ ID NO: 1), wherein the peptide is cytotoxic to a glioblastoma cell line at a concentration of 20 µM in presence of human serum in vitro, and wherein the peptide has a hemolytic activity which is lower than the hemolytic activity of peptide OP-145 (acetyl- IGKEFKRIVERIKRFLRELVRPLR-amide (SEQ ID NO: 50)), and wherein the amino acid sequence comprises 1-8 amino acid substitutions independently selected from: substitution of an amino acid selected from the group of L, V, F, A, I, W, Y or Q by another amino acid selected from said group or by P, and substitution of an amino acid selected from the group of E, K and R, with the exception of K at position 12, by another amino acid selected from said group or by any one of L, I, V, F, A, W and V or by P. This peptide is suitable for prevention or treatment of a cancer, in particular glioblastoma or sarcoma.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
12345671234567177, is replaced by another amino acid selected from said group or by P. Particularly preferred peptides are IGKEFKRIVERKWRFLRELVRPLR (SEQ ID NO: 2), IGKKFKRIVRRKKRFLRKLVRPLR (SEQ ID NO: 3), IGKEFKRIVERKWRFLRKLVRPLR (SEQ ID NO: 4), IGKEFLRIVERKWRFLRKLVRPLL (SEQ ID NO: 5) and IGKEFLRIVERKWRFLVKLVRPLL (SEQ ID NO: 6).
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
RESEARCH CENTER PHARMACEUTICAL ENGINEERING GMBH (Austria)
Inventor
Kappe, Oliver
Sommer, Florian
Cantillo, David
Abstract
The present invention relates to an electrochemical reactor capable of processing an organic mixture comprising a suspension of a solid and a liquid, wherein the electrochemical reactor comprises an inner electrode, an outer electrode, wherein the inner electrode and the outer electrode are arranged concentrically forming a first cavity therebetween, a first inlet configured for introducing the liquid into the first cavity of the electrochemical reactor, a second inlet configured for introducing the solid into the first cavity of the electrochemical reactor, wherein the first inlet and the second inlet are arranged such that the liquid and the solid are introduced separately, wherein the inner electrode is configured to be rotatable around its longitudinal axis, wherein the inner electrode comprises one or more mixing elements. The present invention further relates to processes for the electrochemical N- demethylation and N- and O-demethylation, respectively, of an opioid precursor by means of the electrochemical reactor. The present invention further relates to a one-pot process for the N- and O-demethylation of an opioid precursor.
The invention relates a method for producing amine N-oxide compounds of the formula (I) or (II), in which the R1are selected from hydrocarbon groups with 4 to 26 C atoms and optionally at least one O or S atom; R2, R3, and R5are selected, independently of one another, from hydrogen, R1-O-, R822-N+(O-)R6R6as well, R8representing a hydrocarbon group with1 to 6 carbon atoms and optionally at least one O or S atom; R4is selected from hydrogen and R8; and the R6 are selected, independently of one another, from hydrocarbon groups with 1 to 6 C atoms and optionally at least one N, O, or S atom; wherein optionally two groups R6bonded to the same nitrogen atom are connected together in order to form a nitrogen-containing ring, or optionally one or the two groups R6 of a grouping -N+(O-)R6R6are connected to one or the two R6groups of such a grouping of another molecule of the formula (I) and form a dimer according to formula (II), thereby forming a bridge to the structure (formula A), in which the dashed line indicates an optional bond between the two R6and the asterisks indicate the connection of the bridge to the two aromatic rings. The method has the following steps: 1) reacting a phenol derivative of the following formula (III), in which R7are selected, independently of one another, from hydrogen, hydroxy, and R8, with a secondary amine HNR6R6by means of a Betti/Mannich-type amino alkylation reaction in the presence of formaldehyde in a polar solvent, whereby the hydrogen atom in the ortho position relative to the phenolic OH groups and optionally an additional substitutable hydrogen atom R722-NR6R6, and a corresponding Betti base of the formula (IV) or (V) are obtained, said R722-NR6R6as well; 2) reacting the (two) phenolic OH group(s) and optionally additional free OH groups R7of each Betti base of the formula (IV) or (V) with a compound of the formula R1-X, in which X represents a leaving group selected from halogenides and sulfonates, by means of a Williamson-type etherification reaction in the presence of a base in an organic solvent or without a solvent, whereby a corresponding ether of the formula (VI) or (VII) is obtained,in which the R7are selected, independently of one another, from hydrogen, R1-O-, R822-NR6R6as well; and 3) oxidizing each amino group -NR6R6 of the respective ether of the formula (VI) or (VII) by reacting same with an oxidizing agent in water and an organic solvent, or a mixture thereof, whereby the amine N-oxide compound of the formula (I) or (II) is obtained. The invention also relates to amine N-oxides produced in this matter and to the use thereof as surfactants.
C07C 291/04 - Compounds containing carbon and nitrogen and having functional groups not covered by groups containing nitrogen-oxide bonds containing amino-oxide bonds
C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
C07D 211/94 - Oxygen atom, e.g. piperidine N-oxide
C07C 213/02 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
C07C 213/06 - Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton from hydroxy amines by reactions involving the etherification or esterification of hydroxy groups
C07C 217/58 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
C07C 215/50 - Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups with amino groups and the six-membered aromatic ring, or the condensed ring system containing that ring, bound to the same carbon atom of the carbon chain
The invention relates to novel sulfonate compounds of the formula (I) or (II), in which the R1are selected from hydrocarbon groups with 4 to 26 C atoms and optionally at least one O or S atom; R2to R5are selected, independently of one another, from hydrogen and hydrocarbon groups with 1 to 26 C atoms and optionally at least one O or S atom; R6are selected, independently of one another, from hydrogen and hydrocarbon groups with 1 to 6 carbon atoms, wherein the two groups R6are optionally connected together, as indicated by the dashed line, in order to form a five- or six-membered ring comprising the carbonyl carbon; and the X are selected, independently of one another, from monovalent and multivalent cations Xn+, in which n ≥ 1, including H+. In formula (I), the two X optionally represent a multivalent cation together. The invention also relates to a method for producing same and to the use thereof as surfactants.
The present invention relates to novel inhibitors of adipose triglyceride lipase (ATGL) having an improved inhibitory activity against human ATGL (hATGL) as well as pharmaceutical compositions comprising these inhibitors, and their therapeutic use, particularly in the treatment or prevention of a lipid metabolism disorder, including, e.g., obesity, non-alcoholic fatty liver disease, type 2 diabetes, insulin resistance, glucose intolerance, hypertriglyceridemia, metabolic syndrome, cardiac and skeletal muscle steatosis, congenital generalized lipodystrophy, familial partial lipodystrophy, acquired lipodystrophy syndrome, atherosclerosis, or heart failure.
C07D 417/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 401/12 - 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 linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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 409/10 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
The present invention relates to methods and means for inhibiting or preventing the growth of fungal cells with at least one flavone selected from the group consisting of 5-methoxyflavone, 2′-methoxyflavone, 7-methoxyflavone, 3′,4′,5,7- tetrametoxyflavone, 3′,4′,5′,5,6,7-hexymethoxyflavone, 7,8-benzoflavone and 5,6-benzoflavone for inhibiting or preventing the growth of a fungal cell, wherein said flavone is used in combination with at least one further antimycotic compound selected from the group of azoles, both in an amount to exhibit a synergistic effect compared to the separate use of said flavone and said antimycotic compound.
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/4174 - Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
The present invention refers to a spray dried heparin preparation, in an antiviral effective amount for use as an antiviral substance in a pharmaceutical preparation for use in prophylactic or therapeutic treatment of a disease condition which is caused by or associated with an infection by a coronavirus or for preventing the person-to-person transmission of said virus.
The present invention relates to methods and means for inhibiting or preventing the growth of non-filamentous biofilm forming fungal cells with at least one flavone of formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are independently from each other H or OH.
The present invention relates to methods and means for inhibiting or preventing the growth of non-filamentous biofilm forming fungal cells with at least one flavone of formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are independently from each other H or OH.
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
RESEARCH CENTER PHARMACEUTICAL ENGINEERING GMBH (Austria)
KARL-FRANZENS-UNIVERSITÄT GRAZ (Austria)
Inventor
Glotz, Gabriel
Cantillo Nieves, David
Kappe, Christian Oliver
Abstract
The present invention relates to a process for preparing a nor-opioid compound wherein an opioid precursor compound is electrochemically N-demethylated. The present invention further relates to a process for preparing an opioid antagonist compound, wherein an opioid precursor compound is electrochemically N-demethylated and the thus obtained nor-opioid compound is alkylated again at its secondary amine functional group.
RESEARCH CENTER PHARMACEUTICAL ENGINEERING GMBH (Austria)
KARL-FRANZENS-UNIVERSITÄT GRAZ (Austria)
TECHNISCHE UNIVERSITÄT GRAZ (Austria)
Inventor
Eder, Simone
Koutsamanis, Ioannis
Klein, Thomas
Roblegg, Eva
Khinast, Johannes
Abstract
The invention relates to a method for producing an active ingredient carrier, the method comprising: i) providing a polymer (112) for hot-melt extrusion (150), ii) feeding an expanding agent (113) to the polymer (112), and iii) extruding the polymer (112) by means of the hot-melt extrusion (150) in such a way that the expanding agent (113) produces, by means of a reaction, pores (121) in the polymer (112) which are suitable for transporting active ingredients, in order to provide the active ingredient carrier (120). The pores (121) which are suitable for transporting active ingredients are designed to receive an active ingredient (111) and/or release the active ingredient (111).
The present invention relates to novel inhibitors of adipose triglyceride lipase (ATGL) having an improved inhibitory activity against human ATGL (hATGL) as well as pharmaceutical compositions comprising these inhibitors, and their therapeutic use, particularly in the treatment or prevention of a lipid metabolism disorder, including, e.g., obesity, non-alcoholic fatty liver disease, type 2 diabetes, insulin resistance, glucose intolerance, hypertriglyceridemia, metabolic syndrome, cardiac and skeletal muscle steatosis, congenital generalized lipodystrophy, familial partial lipodystrophy, acquired lipodystrophy syndrome, atherosclerosis, or heart failure.
C07D 213/04 - Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
C07D 277/06 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 401/10 - 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 linked by a carbon chain containing aromatic rings
C07D 417/12 - 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 linked by a chain containing hetero atoms as chain links
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
The present invention relates to methods and means for inhibiting or preventing the growth of fungal cells with at least one flavone selected from the group consisting of 5-methoxyflavone, 2'-methoxyflavone, 7-methoxyflavone, 3',4',5,7- tetrametoxyflavone, 3',4',5',5,6,7-hexymethoxyflavone, 7,8-benzoflavone and 5,6-benzoflavone for inhibiting or preventing the growth of a fungal cell, wherein said flavone is used in combination with at least one further antimycotic compound selected from the group of azoles, both in an amount to exhibit a synergistic effect compared to the separate use of said flavone and said antimycotic compound.
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/4174 - Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
The present invention relates to methods and means for inhibiting or preventing the growth of non-filamentous biofilm forming fungal cells with at least one flavone of formula (I) wherein R1, R2, R3, R4, R5, R6and R7 are independently from each other H or OH.
C07D 311/30 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 4 with aromatic rings attached in position 2 or 3 with aromatic rings attached in position 2 only not hydrogenated in the hetero ring, e.g. flavones
The invention relates to a fuel filter (1), in particular of a motor vehicle, having a housing (2), in which there is arranged a coalescer (4) for separating out water (6) contained in the fuel (5), which coalescer comprises a coalescer material (7) that is suitable for coalescing water (6), wherein the coalescer (4) is flowed through in the throughflow direction (8). In that context, what is essential to the invention is the fact that the coalescer material (7) has fibers (9) whose primary orientation is oriented essentially parallel to the throughflow direction (8).
B01D 29/11 - Filters with filtering elements stationary during filtration, e.g. pressure or suction filters, not covered by groups Filtering elements therefor with bag, cage, hose, tube, sleeve or like filtering elements
B01D 29/58 - Filters with filtering elements stationary during filtration, e.g. pressure or suction filters, not covered by groups Filtering elements therefor with multiple filtering elements, characterised by their mutual disposition in series connection arranged concentrically or coaxially
B01D 36/00 - Filter circuits or combinations of filters with other separating devices
B01D 39/16 - Other self-supporting filtering material of organic material, e.g. synthetic fibres
Method for processing of a grey scale image, in particular a dim grey scale image, comprising the following steps: a) receiving an initial grey scale image, said initial grey scale image having a plurality of pixels at an initial resolution, b) calculating parameters characterizing the luminance (gain, median_grey, var_grey) and the noise level (X, noise_estimate, radius_spatial_summation, grid_size, threshold_var) of the initial grey scale image of step a), c) creating a basic intermediate image, d) creating an averaged intermediate image, and e) creating an enhanced grey scale image by interpolation of pixels based on the averaged receptors (greyAvg) of the averaged intermediate image of step d).
RESEARCH CENTER PHARMACEUTICAL ENGINEERING GMBH (Austria)
KARL-FRANZENS-UNIVERSITÄT GRAZ (Austria)
Inventor
Glotz, Gabriel
Kappe, Christian
Abstract
A system for monitoring a property of a fluid during a flow process, the system comprising a flow apparatus, a supply apparatus configured to supply the fluid, and a monitoring apparatus configured for monitoring the property of the fluid during supplying the fluid by the supply apparatus. The flow apparatus comprises a flow unit which is movably arranged at a tube of the flow apparatus, wherein the fluid flows through the tube.
RESEARCH CENTER PHARMACEUTICAL ENGINEERING GMBH (Austria)
KARL-FRANZENS-UNIVERSITÄT GRAZ (Austria)
Inventor
Glotz, Gabriel
Kappe, Christian Oliver
Dallinger, Doris
Lebl, Rene
Abstract
The present invention relates to a process for generating cyanogen bromide (BrCN) comprising the steps of: mixing a fluid containing a bromine source with a fluid containing a cyanide source, reacting the bromine source and the cyanide source with each other to give a reaction mixture containing cyanogen bromide, and purifying the reaction mixture by means of a membrane-based separation to give (purified) cyanogen bromide. The present invention further relates to an apparatus configured for continuously generating cyanogen bromide and an apparatus configured for continuously generating bromine, which both apparatuses may be combined, as well as a process for synthesizing a nitrogen-containing compound.
C07D 417/12 - 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 linked by a chain containing hetero atoms as chain links
Method for processing of a grey scale image, in particular a dim grey scale image, comprising the following steps: a) receiving an initial grey scale image, said initial grey scale image having a plurality of pixels at an initial resolution, b) calculating parameters characterizing the luminance (gain, median_grey, var_grey) and the noise level (X, noise_estimate, radius_spatial_summation, grid_size, threshold_var) of the initial grey scale image of step a), c) creating a basic intermediate image, d) creating an averaged intermediate image, and e) creating an enhanced grey scale image by interpolation of pixels based on the averaged receptors (greyAvg) of the averaged intermediate image of step d).
The present invention relates to spermidine or spermidine comprising extracts for use in the treatment and/or amelioration of mitochondrial energy disorders or diseases.
The invention particularly relates to a method for temporal and spatial interpolation of fMRI time series with respect to a single subject, wherein an image has at least two spatial and at least one temporal dimension, wherein at least a first time series is recorded with respect to a single subject. The method comprises the step of taking a plurality N of functional images (100), wherein at least two images from the plurality N of functional images do not have an identical spatial and/or temporal resolution, and the step of interpolating the plurality N of functional images in a common "spatial" and/or "temporal"space (200), wherein the resolution of the common "spatial" or "temporal" space is at least as high as the highest "temporal" or "spatial" level of resolution of the plurality N of functional images.
The present invention provides a small molecule inhibitor for adipose triglyceride lipase (ATGL) with the molecule having IC 50 concentrations in the submicromolar range. The inhibitor has the basic structure (I) as disclosed herein and is a competitive inhibitor that does not affect the activity of other known acylglycerol hydrolases. The inhibitor is orally bioavailable and capable of inhibiting lipolysis in vivo, such that it is therefore capable of serving as lead structure for the identification of further inhibitors.
C07C 275/28 - Derivatives of urea, i.e. compounds containing any of the groups the nitrogen atoms not being part of nitro or nitroso groups having nitrogen atoms of urea groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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
A61K 31/216 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
A61K 31/17 - Amides, e.g. hydroxamic acids having the group N—C(O)—N or N—C(S)—N, e.g. urea, thiourea, carmustine
A compound of formula (I) as defined herein
is useful in the treatment and prevention of a disorder such as cachexia, stroke, atherosclerosis, coronary artery disease, and diabetes and pharmaceutical compositions of the same. Also, a method of screening for lipase inhibitors using a compound of formula (I) and determining its lipase inhibitory activity. The method includes in vitro assays of compounds using ATGL and/or HSL, and cellular assays wherein inhibition is followed by observing indicators of efficacy. Also, methods for treatment or prevention of a condition involving cachexia, stroke, artherosclerosis, coronary artery disease, diabetes, preferably diabetes type II by administering a pharmaceutical composition comprising an agent which is able to inhibit ATGL. Also contemplated herein, are compositions comprising one or more ATGL-inhibiting agents optionally in combination with one or more lipase inhibitors or inhibitors of inflammatory cytokines.
C07C 69/94 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of polycyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of six-membered aromatic rings
C07C 229/52 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
C07D 231/14 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07C 65/24 - Compounds having carboxyl groups bound to carbon atoms of six-membered aromatic rings and containing any of the groups OH, O-metal, —CHO, keto, ether, groups, groups, or groups containing ether groups, groups, groups, or groups polycyclic
C12Q 1/44 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving hydrolase involving esterase
32.
DETERMINING NOVEL ENZYMATIC FUNCTIONALITIES USING THREE-DIMENSIONAL POINT CLOUDS REPRESENTING PHYSICO CHEMICAL PROPERTIES OF PROTEIN CAVITIES
The invention relates to a method for determining catalophores including the steps of creating a point cloud database for target protein structures; creating a query point cloud; and searching said database with said query to thereby identify one or more catalophores.
G06F 19/16 - for molecular structure, e.g. structure alignment, structural or functional relations, protein folding, domain topologies, drug targeting using structure data, involving two-dimensional or three-dimensional structures
33.
ASYMMETRIC HYDRATION OF 4-HYDROXYSTYRENE DERIVATIVES EMPLOYING DECARBOXYLASES
A promiscuous catalytic hydratase-activity of phenolic acid decarboxylases allows the asymmetric addition of H2O or of a non-natural nucleophile across the C=C bond of hydroxystyrene derivatives.
The present invention relates to the use of recombinant heme-containing horseradish peroxidase isoenzyme with improved technological properties such as altered glycosylation, improved catalytic properties or improved stability and different ranges of pH optima and improved surface interactions in the treatment of waste water.
The present invention relates to recombinant heme-containing horseradish peroxidase isoenzymes with improved properties. In particular, the present invention relates to a plant enzyme kit comprising recombinant peroxidase isoenzymes, preferably horseradish peroxidase isoenzymes.
C07C 51/15 - Preparation of carboxylic acids or their salts, halides, or anhydrides by reaction of organic compounds with carbon dioxide, e.g. Kolbe-Schmitt synthesis
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