Compositions and methods for enhancing the absorption of therapeutic polypeptides from the intestines following oral administration The invention provides a method for increasing the systemic bioavailability of a polypeptide therapeutic agent undergoing oral, orogastric, nasogastric, or intragastric administration, said method comprising administering said polypeptide therapeutic agent together with (i) an alginate oligomer (ii) a compound of Formula (I), or a pharmaceutically acceptable salt thereof, (I) (iii) a compound of Formula (II), or a pharmaceutically acceptable salt thereof, (II) to a portion of the intestines of a human or non-human animal subject by oral, orogastric, nasogastric, or intragastric administration, wherein said portion of the intestines is contacted with (i), (ii), (iii) and said polypeptide therapeutic agent in amounts which result in uptake of the polypeptide therapeutic agent from said portion of the intestine. Such methods allow for systemic treatment or prevention of a disease or condition or complication thereof which is responsive to, or which is prevented by, a polypeptide therapeutic agent via oral, orogastric, nasogastric, or intragastric administration routes. Further provided are compositions for use in such methods.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
2.
COMBINATIONS OF GASTROINTESTINAL PERMEATION ENHANCERS FOR USE IN COMPOSITIONS AND METHODS TO ENHANCE THE SYSTEMIC BIOAVAILABILITY OF THERAPEUTIC POLYPEPTIDES UNDERGOING ORAL ADMINISTRATION
The invention provides a method for increasing the systemic bioavailability of a polypeptide therapeutic agent undergoing oral, orogastric, nasogastric, or intragastric administration, said method comprising administering said polypeptide therapeutic agent together with (i) a compound of Formula (I), or a pharmaceutically acceptable salt thereof, (I) and (ii) a compound of Formula (II), or a pharmaceutically acceptable salt thereof, (II) to a human or non-human animal subject by oral, orogastric, nasogastric, or intragastric administration. Such methods allow for systemic treatment or prevention of a disease or condition or complication thereof which is responsive to, or which is prevented by, a polypeptide therapeutic agent via oral, orogastric, nasogastric, or intragastric administration routes. Further provided are compositions for use in such methods.
The invention provides an antimycotic polyene-alginate oligomer conjugate comprising an antimycotic polyene connected covalently to at least one alginate oligomer, wherein one or other terminal uronic acid residues of each alginate oligomer in the conjugate is connected to the antimycotic polyene via a direct covalent bond or a covalent molecular linker, or a pharmaceutically acceptable salt, solvate, hydrate, diastereoisomer, tautomer, enantiomer, or active metabolite thereof. Also provided are methods for the preparation of said conjugate, pharmaceutical compositions comprising said conjugate and the use thereof in a method for the treatment or prevention of a fungal infection in a subject with, suspected to have, or at risk of, a fungal infection.
A61K 47/61 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
The present invention provides method for increasing the systemic bioavailability of a polypeptide therapeutic agent undergoing oral, orogastric, nasogastric, or intragastric administration, said method comprising administering said polypeptide therapeutic agent together with an alginate oligomer, and optionally a gastrointestinal permeation enhancer, to a stomach of a human or non-human animal as part of one or more dosage forms, wherein said one or more dosage forms do not carry a coating in addition to the polypeptide therapeutic agent, the alginate oligomer, and the gastrointestinal permeation enhancer if used, which would provide substantive protection from a gastric environment. Such methods allow for systemic treatment or prevention of a disease or condition or complication thereof which is responsive to, or which is prevented by, a polypeptide therapeutic agent via oral, orogastric, nasogastric, or intragastric administration routes. Further provided are compositions for use in such methods comprising alginate oligomers, polypeptide therapeutic agents, and optionally gastrointestinal permeation enhancers.
An alginate oligomer for use in the anticoagulation therapy of a human or non-human vertebrate subject at risk of blood clots which have an abnormally dense microstructure. In certain embodiments, the incidence of blood clots which have an abnormally dense microstructure in the subject is reduced and/or the occurrence of blood clots which have an abnormally dense microstructure in the subject is inhibited and/or the abnormal microstructure of the subject's clots is normalized. Corresponding methods of anticoagulation therapy and products of use therein are further provided.
Qualitative and quantitative methods are for the detection of alginate oligomers in body fluids based on analyzing the Fourier transform infrared spectroscopy (FTIR) spectrum of a body fluid sample, for example a sputum sample, at a specific wave number range and, more particularly, certain specific characteristic wavenumbers.
G01N 21/35 - Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry using infrared light
G01N 21/3577 - Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry using infrared light for analysing liquids, e.g. polluted water
G01N 33/487 - Physical analysis of biological material of liquid biological material
8.
Inhalable powder formulations of alginate oligomers
A method of preparing spray dried particles for inhalation comprising providing: (i) an aqueous liquid composition including the alginate oligomer and an aqueous liquid composition including an anti-adherent compound, or (ii) an aqueous liquid composition including the alginate oligomer and an anti-adherent compound; providing an organic liquid composition including a phospholipid; combining a volume of the organic liquid composition with a volume of the aqueous liquid composition, wherein the total volume of the organic liquid composition is smaller than the total volume of the aqueous liquid composition with which it is combined, and wherein the total volume of aqueous liquid composition and said total volume of organic liquid composition are sufficient to provide a combination; homogenizing the combination to form an organic-in-aqueous liquid emulsion for spray drying; and spray drying the organic-in-aqueous liquid emulsion to form the spray dried particles for inhalation.
A method for translocating a cationic micro/nanoparticle across a mucus layer, the method including (a) contacting the mucus layer with at least one alginate oligomer, the alginate oligomer having at least 70% mannuronate residues, together with the cationic micro/nanoparticle; or (b)(i) contacting the cationic micro/nanoparticle with an alginate oligomer having at least 70% mannuronate residues thereby forming a micro/nanoparticle carrying the alginate oligomer, and (b)(ii) contacting the mucus layer with the micro/nanoparticle prepared in step (b)(i). There is also provided a method for translocating a molecule of interest across a mucus layer including contacting the mucus layer with a micro/nanoparticle which is formed of self-assembling micro/nanoparticle forming components, wherein at least one is a cationic micro/nanoparticle forming agent and at least one is an alginate oligomer which has at least 70% mannuronate residues, and further comprises the molecule of interest, optionally wherein the molecule of interest is covalently bound to one or more of the self-assembling micro/nanoparticle forming components.
A61K 47/69 - 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 conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61K 47/61 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
10.
USE OF ALGINATE OLIGOMERS IN THE ANTICOAGULATION THERAPY OF SUBJECTS AT RISK OF BLOOD CLOTS WHICH HAVE AN ABNORMALLY DENSE MICROSTRUCTURE
The invention provides an alginate oligomer for use in the anticoagulation therapy of a human or non-human vertebrate subject at risk of blood clots which have an abnormally dense microstructure. In certain embodiments, the incidence of blood clots which have an abnormally dense microstructure in the subject is reduced and/or the occurrence of blood clots which have an abnormally dense microstructure in the subject is inhibited and/or the abnormal microstructure of the subject's clots is normalised. Corresponding methods of anticoagulation therapy and products of use therein are further provided.
The invention provides an alginate oligomer for use in the anticoagulation therapy of a human or non-human vertebrate subject at risk of blood clots which have an abnormally dense microstructure. In certain embodiments, the incidence of blood clots which have an abnormally dense microstructure in the subject is reduced and/or the occurrence of blood clots which have an abnormally dense microstructure in the subject is inhibited and/or the abnormal microstructure of the subject's clots is normalised. Corresponding methods of anticoagulation therapy and products of use therein are further provided.
The present invention provides qualitative and quantitative methods for the detection of alginate oligomers in body fluids based on analysing the Fourier transform infrared spectroscopy (FTIR) spectrum of a body fluid sample, e.g. a sputum sample, at a specific wave number range and, more particularly, certain specific characteristic wavenumbers.
G01N 21/3577 - Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry using infrared light for analysing liquids, e.g. polluted water
13.
USE OF ALGINATE OLIGOMERS TO ENHANCE THE TRANSLOCATION OF MICRO/NANOPARTICLES ACROSS MUCUS LAYERS
The invention provides methods for translocating micro/nanoparticles and molecules or interest carried thereby across mucus layers. More specifically there is provided a method for translocating a cationic micro/nanoparticle across a mucus layer said method comprising (a) contacting the mucus layer with at least one alginate oligomer, said alginate oligomer having at least 70% mannuronate residues, together with the cationic micro/nanoparticle; or (b)(i) contacting the cationic micro/nanoparticle with an alginate oligomer having at least 70% mannuronate residues thereby forming a micro/nanoparticle carrying said alginate oligomer, and (b)(ii) contacting the mucus layer with the micro/nanoparticle prepared in step (b)(i). There is also provided a method for translocating a molecule of interest across a mucus layer said method comprising contacting the mucus layer with a micro/nanoparticle which is formed of self-assembling micro/nanoparticle forming components, wherein at least one is a cationic micro/nanoparticle forming agent and at least one is an alginate oligomer which has at least 70% mannuronate residues, and further comprises said molecule of interest, optionally wherein the molecule of interest is covalently bound to one or more of the self-assembling micro/nanoparticle forming components. The invention further relates to the use of alginate oligomers in the methods of the invention and to micro/nanoparticles of the invention.
A61K 47/61 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
14.
USE OF ALGINATE OLIGOMERS TO ENHANCE THE TRANSLOCATION OF MICRO/NANOPARTICLES ACROSS MUCUS LAYERS
The invention provides methods for translocating micro/nanoparticles and molecules or interest carried thereby across mucus layers. More specifically there is provided a method for translocating a cationic micro/nanoparticle across a mucus layer said method comprising (a) contacting the mucus layer with at least one alginate oligomer, said alginate oligomer having at least 70% mannuronate residues, together with the cationic micro/nanoparticle; or (b)(i) contacting the cationic micro/nanoparticle with an alginate oligomer having at least 70% mannuronate residues thereby forming a micro/nanoparticle carrying said alginate oligomer, and (b)(ii) contacting the mucus layer with the micro/nanoparticle prepared in step (b)(i). There is also provided a method for translocating a molecule of interest across a mucus layer said method comprising contacting the mucus layer with a micro/nanoparticle which is formed of self-assembling micro/nanoparticle forming components, wherein at least one is a cationic micro/nanoparticle forming agent and at least one is an alginate oligomer which has at least 70% mannuronate residues, and further comprises said molecule of interest, optionally wherein the molecule of interest is covalently bound to one or more of the self-assembling micro/nanoparticle forming components. The invention further relates to the use of alginate oligomers in the methods of the invention and to micro/nanoparticles of the invention.
A61K 47/61 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule the organic macromolecular compound being a polysaccharide or a derivative thereof
15.
Alginate oligomers for the treatment or prevention of microbial overgrowth in the intestinal tract
The invention provides a method for the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject, said method comprising administering an effective amount of an alginate oligomer to a subject in need thereof. Also provided is an alginate oligomer for use in the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject and a product containing an alginate oligomer and further pharmaceutical for the treatment of intestinal microbial overgrowth and/or a CFTR modulator as a combined preparation for separate, simultaneous or sequential use in the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 36/03 - Phaeophycota or phaeophyta (brown algae), e.g. Fucus
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
The present invention provides a diagnostic method which may be used to determine the likelihood that a patient with cystic fibrosis will respond to treatment with an alginate oligomer. The method is based on analysingthe IR absorbance values and/or transmittance values, in particular a Fourier transform infrared spectroscopy (FTIR) spectrum, of a mucus sample from the respiratory system of a CF patient at certain specific wavenumbers.
G01N 21/359 - Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry using infrared light using near infrared light
A61K 31/00 - Medicinal preparations containing organic active ingredients
G01N 21/35 - Investigating relative effect of material at wavelengths characteristic of specific elements or molecules, e.g. atomic absorption spectrometry using infrared light
The invention provides abacitracin-alginate oligomer conjugate comprising a bacitracin-class antibiotic connected covalently to at least one alginate oligomer via a direct covalent bond or a covalent molecular linker, or a pharmaceutically acceptable salt, solvate, hydrate, diastereoisomer, tautomer, enantiomer or active metabolite thereof. Also provided are methods for the preparation of said conjugate, pharmaceutical compositions comprising said conjugate and the use thereof in a method for the treatment or prevention of a bacterial infection in a subject with, suspected to have, or at risk of, a bacterial infection.
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
A61K 47/50 - 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 invention provides apolymyxin-alginate oligomer conjugate comprising a polymyxin-class antibiotic connected covalently to at least one alginate oligomer via a direct covalent bond or a covalent molecular linker, or a pharmaceutically acceptable salt, solvate, hydrate, diastereoisomer, tautomer, enantiomer or active metabolite thereof. Also provided are methods for the preparation of said conjugate, pharmaceutical compositions comprising said conjugate and the use thereof in amethod for the treatment or prevention of a bacterial infection in a subject with, suspected to have, or at risk of, a bacterial infection.
The invention provides a method for combating biofilm, said method comprising contacting a biofilm with an alginate oligomer. The biofilm may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use in the treatment or prevention of a biofilm infection in a subject. In another aspect the method can be used to combat biofilms, on abiotic surfaces, e.g. for disinfection and cleaning purposes.
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61K 38/48 - Hydrolases (3) acting on peptide bonds (3.4)
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61Q 11/00 - Preparations for care of the teeth, of the oral cavity or of dentures, e.g. dentifrices or toothpastesMouth rinses
A61Q 17/00 - Barrier preparationsPreparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
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
A01N 63/02 - Substances produced by, or obtained from, microorganisms or animals
A method is for the treatment of a condition in a subject, which arises from or is associated with CFTR dysfunction. The method includes administering to the subject an effective amount of a CFTR modulator together with an effective amount of an alginate oligomer. The condition can be cystic fibrosis (CF), non-compound CFTR gene mutation heterozygosity, abnormal mucus clearance in the respiratory tract and/or breathing difficulties resulting from chronic particulate inhalation, COPD, chronic bronchitis, emphysema, bronchiectasis, asthma or chronic sinusitis, or a complication of any of these.
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/43 - Compounds containing 4-thia-1-azabicyclo [3.2.0] heptane ring systems, i.e. compounds containing a ring system of the formula , e.g. penicillins, penems
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
21.
ALGINATE OLIGOMERS FOR THE TREATMENT OR PREVENTION OF MICROBIAL OVERGROWTH IN THE INTESTINAL TRACT
The invention provides a method for the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject, said method comprising administering an effective amount of an alginate oligomer to a subject in need thereof. Also provided is an alginate oligomer for use in the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject and a product containing an alginate oligomer and further pharmaceutical for the treatment of intestinal microbial overgrowth and/or a CFTR modulator as a combined preparation for separate, simultaneous or sequential use in the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
The invention provides a method for the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject, said method comprising administering an effective amount of an alginate oligomer to a subject in need thereof. Also provided is an alginate oligomer for use in the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject and a product containing an alginate oligomer and further pharmaceutical for the treatment of intestinal microbial overgrowth and/or a CFTR modulator as a combined preparation for separate, simultaneous or sequential use in the treatment or prevention of microbial overgrowth in at least part of the intestinal tract of a subject.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
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 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
The disclosure relates to an alginate oligomer of 2 to 75 monomer residues, wherein said monomer residues do not carry a sulphate group, for use as a blood anticoagulant in clinical and non-clinical applications, including in vivo, ex vivo and in vitro contexts. The invention further provides for the use of such an alginate oligomer in preparing a product or device having a reduced capacity to promote blood coagulation, wherein said alginate oligomer is provided at or on a surface of said product or device. Such products and devices form a further aspect of the invention.
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
26.
USE OF ALGINATE OLIGOMERS AND CFTR MODULATORS IN THE TREATMENT OF CONDITIONS ASSOCIATED WITH CFTR DYSFUNCTION
The present invention provides a method for the treatment of a condition in a subject arising from or associated with CFTR dysfunction, said method comprising administering to said subject an effective amount of a CFTR modulator together with an effective amount of an alginate oligomer. In certain embodiments said condition is cystic fibrosis (CF), non-compound CFTR gene mutation heterozygosity, abnormal mucus clearance in the respiratory tract and/or breathing difficulties resulting from chronic particulate inhalation, COPD, chronic bronchitis, emphysema, bronchiectasis, asthma or chronic sinusitis, or a complication thereof.
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
A61P 11/00 - Drugs for disorders of the respiratory system
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cystic fibrosis, pulmonary diseases, acute and chronic infections, gastrointestinal disorders, for abnormal mucus accumulation, microbial infections, biofilm formation and antibiotic resistance and for wound care.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment of cystic fibrosis, pulmonary diseases, acute and chronic infections, gastrointestinal disorders, for the prevention and disruption of microbial biofilms, and for wound care.
29.
INHALABLE POWDER FORMULATIONS OF ALGINATE OLIGOMERS
The invention provides spray dried particles for inhalation, said particles consisting of (i) at least about 70% w/w of an alginate oligomer, (ii) at least about 10% w/w in total of a phospholipid and an anti-adherent compound, wherein said phospholipid is solid at room temperature, and wherein said phospholipid is present at no less than 0.5% w/w and said anti-adherent compound is present at no less than 0.5% w/w, and (iii) no greater than about 10% w/w of further excipients. The invention further provides a novel method for preparing said particles, capsules and dry powder inhalers comprising said particles and the therapeutic use of said particles, particularly in the treatment or prevention of a respiratory infection or a respiratory disorder.
The invention provides spray dried particles for inhalation, said particles consisting of (i) at least about 70% w/w of an alginate oligomer, (ii) at least about 10% w/w in total of a phospholipid and an anti-adherent compound, wherein said phospholipid is solid at room temperature, and wherein said phospholipid is present at no less than 0.5% w/w and said anti-adherent compound is present at no less than 0.5% w/w, and (iii) no greater than about 10% w/w of further excipients. The invention further provides a novel method for preparing said particles, capsules and dry powder inhalers comprising said particles and the therapeutic use of said particles, particularly in the treatment or prevention of a respiratory infection or a respiratory disorder.
A61K 31/685 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols one of the hydroxy compounds having nitrogen atoms, e.g. phosphatidylserine, lecithin
A61K 31/702 - Oligosaccharides, i.e. having three to five saccharide radicals attached to each other by glycosidic linkages
The invention provides a method for the treatment of a condition in a human patient arising from or associated with a defective cystic fibrosis transmembrane conductance regulator(CFTR) ion channel and/or abnormal mucus which is attached to underlying epithelium, said method comprising administering an alginate oligomer,wherein at least 30% of the monomer residues of the alginate oligomer are G residues,to the patient in an amount sufficient to achieve a local concentration of the alginate oligomer of 1to 6% w/v at at least part of a mucosal surface with a defective CFTR ion channel and/or said abnormal mucus in the patient, thereby to result in at least partial detachment of mucus from said mucosal surface. In certain embodiments said condition is cystic fibrosis (CF), non- compound CFTR gene mutation heterozygosity, abnormal mucus clearance in the respiratory tract and/or breathing difficulties resulting from chronic particulate inhalation, COPD, chronic bronchitis, emphysema, bronchiectasis, asthma or chronic sinusitis, or a complication thereof.
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
The invention provides a method of overcoming resistance to at least one antibiotic in a multidrug resistant bacterium, said method comprising contacting said bacterium with an alginate oligomer together with the antibiotic. The multidrug resistant bacterium may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with a multidrug resistant bacterium to overcome resistance to the antibiotic in said multidrug resistant bacterium. In another aspect the method can be used to combat contamination of a site with multidrug resistant bacteria, e.g. for disinfection and cleaning purposes.
A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
A61K 38/04 - Peptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A01N 43/22 - 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 rings with more than six members
A01N 43/72 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms
A01N 43/86 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with nitrogen atoms and oxygen or sulfur atoms, as ring hetero atoms six-membered rings with one nitrogen atom and either one oxygen atom or one sulfur atom in positions 1,3
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
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
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
The invention provides an alginate oligomer of 2 to 75 monomer residues, wherein said monomer residues do not carry a sulphate group, for use as a blood anticoagulant in clinical and non-clinical applications, including in vivo, ex vivo and in vitro contexts. The invention further provides for the use of such an alginate oligomer in preparing a product or device having a reduced capacity to promote blood coagulation, wherein said alginate oligomer is provided at or on a surface of said product or device. Such products and devices form a further aspect of the invention.
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
A61M 1/00 - Suction or pumping devices for medical purposesDevices for carrying-off, for treatment of, or for carrying-over, body-liquidsDrainage systems
The invention provides an alginate oligomer of 2 to 75 monomer residues, wherein said monomer residues do not carry a sulphate group, for use as a blood anticoagulant in clinical and non-clinical applications, including in vivo, ex vivo and in vitro contexts. The invention further provides for the use of such an alginate oligomer in preparing a product or device having a reduced capacity to promote blood coagulation, wherein said alginate oligomer is provided at or on a surface of said product or device. Such products and devices form a further aspect of the invention.
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
A61M 1/00 - Suction or pumping devices for medical purposesDevices for carrying-off, for treatment of, or for carrying-over, body-liquidsDrainage systems
The invention provides a method for combating biofilm, said method comprising contacting a biofilm with an alginate oligomer. The biofilm may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use in the treatment or prevention of a biofilm infection in a subject. In another aspect the method can be used to combat biofilms, on abiotic surfaces, e.g. for disinfection and cleaning purposes.
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 38/48 - Hydrolases (3) acting on peptide bonds (3.4)
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A01N 63/02 - Substances produced by, or obtained from, microorganisms or animals
A61Q 11/00 - Preparations for care of the teeth, of the oral cavity or of dentures, e.g. dentifrices or toothpastesMouth rinses
A61Q 17/00 - Barrier preparationsPreparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
36.
USE OF ALGINATE OLIGOMERS TO ENHANCE THE EFFECTS OF ANTIFUNGAL AGENTS
Use of alginate oligomers to enhance the effects of antifungal agents The invention provides a method to improve the efficacy of an antifungal agent against a fungus, said method comprising using said antifungal agent together with an alginate oligomer. The fungus may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antifungal agent in treating a subject infected, suspected to be infected, or at risk of infection, with a fungus. In another aspect the method can be used to combat fungal contamination of a site e.g. for disinfection and cleaning purposes.
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
A01N 43/90 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having two or more relevant hetero rings, condensed among themselves or with a common carbocyclic ring system
The invention provides a method of overcoming resistance to at least one antibiotic in a multidrug resistant bacterium, said method comprising contacting said bacterium with an alginate oligomer together with the antibiotic. The multidrug resistant bacterium may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with a multidrug resistant bacterium to overcome resistance to the antibiotic in said multidrug resistant bacterium. In another aspect the method can be used to combat contamination of a site with multidrug resistant bacteria, e.g. for disinfection and cleaning purposes.
A01N 37/18 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group —CO—N, e.g. carboxylic acid amides or imidesThio-analogues thereof
A61K 38/04 - Peptides having up to 20 amino acids in a fully defined sequenceDerivatives thereof
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
A61K 31/7036 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin having at least one amino group directly attached to the carbocyclic ring, e.g. streptomycin, gentamycin, amikacin, validamycin, fortimicins
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
The invention provides a method of overcoming resistance to at least one antibiotic in a multidrug resistant bacterium, said method comprising contacting said bacterium with an alginate oligomer together with the antibiotic. The multidrug resistant bacterium may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with a multidrug resistant bacterium to overcome resistance to the antibiotic in said multidrug resistant bacterium. In another aspect the method can be used to combat contamination of a site with multidrug resistant bacteria, e.g. for disinfection and cleaning purposes.
The invention provides a method of overcoming resistance to at least one antibiotic in a multidrug resistant bacterium, said method comprising contacting said bacterium with an alginate oligomer together with the antibiotic. The multidrug resistant bacterium may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with a multidrug resistant bacterium to overcome resistance to the antibiotic in said multidrug resistant bacterium. In another aspect the method can be used to combat contamination of a site with multidrug resistant bacteria, e.g. for disinfection and cleaning purposes.
The present invention provides a method for inhibiting the adherence of a microorganism to a surface, said method comprising contacting said microorganism and/or the surface with an alginate oligomer, wherein said alginate oligomer has a number average degree of polymerisation of 8-50 and wherein at least 90% of the monomer residues are guluronate. Both medical and non-medical uses are provided.
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 invention provides a method to improve the efficacy of an antibiotic to inhibit the growth of Acinetobacter, said method comprising using said antibiotic together with an alginate oligomer. The Acinetobacter may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with Acinetobacter. In another aspect the method can be used to combat Acinetobacter contamination of a site e.g. for disinfection and cleaning purposes.
The invention provides a method to improve the efficacy of an antibiotic to inhibit the growth of Acinetobacter, said method comprising using said antibiotic together with an alginate oligomer. The Acinetobacter may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use together with at least one antibiotic in treating a subject infected, suspected to be infected, or at risk of infection, with Acinetobacter. In another aspect the method can be used to combat Acinetobacter contamination of a site e.g. for disinfection and cleaning purposes.
The present invention provides a method for inhibiting the viability and/or growth of a microorganism, said method comprising contacting said microorganism with an alginate oligomer, wherein said alginate oligomer has a number average degree of polymerisation of 8-50 and wherein at least 90% of the monomer residues are guluronate. The invention is based on the surprising discovery that certain alginate oligomers are able directly to kill, or to inhibit the growth of microorganisms, and both medical and non-medical uses are provided to combat microbial infection or contamination
The invention provides a method for combating biofilm, said method comprising contacting a biofilm with an alginate oligomer. The biofilm may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use in the treatment or prevention of a biofilm infection in a subject. In another aspect the method can be used to combat biofilms, on abiotic surfaces, e.g., for disinfection and cleaning purposes.
A01N 43/04 - 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
A61K 31/715 - Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkagesDerivatives thereof, e.g. ethers, esters
The invention provides a method for combating biofilm, said method comprising contacting a biofilm with an alginate oligomer. The biofilm may be on an animate or inanimate surface and both medical and non-medical uses and methods are provided. In one aspect the invention provides an alginate oligomer for use in the treatment or prevention of a biofilm infection in a subject. In another aspect the method can be used to combat biofilms, on abiotic surfaces, e.g. for disinfection and cleaning purposes.
A01N 43/46 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom rings with more than six members
A01N 65/00 - Biocides, pest repellants or attractants, or plant growth regulators containing material from algae, lichens, bryophyta, multi-cellular fungi or plants, or extracts thereof
A01P 1/00 - DisinfectantsAntimicrobial compounds or mixtures thereof
