Abstract

Temperature-stable, gastric-resistant formulation suitable for oral and sustained delivery of proteins, including insulin, and for nucleic acids (e.g., DNA, RNA), and related methods of making and use are described. In an embodiment, The thermostable and acid-stable pharmaceutical composition includes an inclusion complex, where the inclusion complex includes a lipophilic active pharmaceutical ingredient-carrier ionic association complex encapsulated in a β-cyclodextrin or derivative thereof. In an embodiment, the pharmaceutical composition ion-pair complex encapsulated in the β-cyclodextrin or derivative thereof is in the form of a convenient dissolvable tablet dosage form.

IPC Classes  ?

• A61K 9/20 - Pills, lozenges or tablets
• A61K 38/28 - Insulins
• A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics

Abstract

e.g.e.g., DNA, RNA), and related methods of making and use are described. In an embodiment, The thermostable and acid-stable pharmaceutical composition includes an inclusion complex, where the inclusion complex includes a lipophilic active pharmaceutical ingredient-carrier ionic association complex encapsulated in a β-cyclodextrin or derivative thereof. In an embodiment, the pharmaceutical composition ion-pair complex encapsulated in the β-cyclodextrin or derivative thereof is in the form of a convenient dissolvable tablet dosage form.

IPC Classes  ?

• C08L 5/16 - CyclodextrinDerivatives thereof
• 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

Abstract

Malaria transmission-blocking vaccines with good preservation stability and immunostimulatory action are provided. According the present invention, combination use of a pharmaceutical composition comprising (4E,8E,12E,16E,20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexan-3-yl]amino}-6-methylpyrimidin-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaeneamide, or a pharmaceutically acceptable salt thereof, as a vaccine adjuvant with enhanced specific immune response against antigens and good preservation stability and a malaria vaccine with non-glycosylation, homogeneity, and biological activity allow for the provision of malaria transmission-blocking vaccines with good preservation stability and immunostimulatory action.

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 39/015 - Hemosporidia antigens, e.g. Plasmodium antigens
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61P 33/06 - Antimalarials

Abstract

Pre-erythrocytic malaria vaccines with good preservation stability and immunostimulatory action are provided. According the present invention, combination use of a pharmaceutical composition comprising (4E,8E,12E,16E,20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexan-3-yl]amino}-6-methylpyrimidin-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaeneamide, or a pharmaceutically acceptable salt thereof, as a vaccine adjuvant with enhanced specific immune response against antigens and good preservation stability and a malaria vaccine with biological activity allow for the provision of pre-erythrocytic malaria vaccines with good preservation stability and immunostimulatory action.

IPC Classes  ?

• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61K 9/107 - Emulsions
• A61K 39/015 - Hemosporidia antigens, e.g. Plasmodium antigens
• A61K 47/06 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
• A61K 47/10 - AlcoholsPhenolsSalts thereof, e.g. glycerolPolyethylene glycols [PEG]PoloxamersPEG/POE alkyl ethers
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

Abstract

Malaria transmission-blocking vaccines with good preservation stability and immunostimulatory action are provided. According the present invention, combination use of a pharmaceutical composition comprising (4E,8E,12E,16E,20E)-N-{2-[{4-[(2-amino-4-{[(3S)-1-hydroxyhexan-3-yl]amino}-6-methylpyrimidin-5-yl)methyl]benzyl}(methyl)amino]ethyl}-4,8,12,17,21,25-hexamethylhexacosa-4,8,12,16,20,24-hexaeneamide, or a pharmaceutically acceptable salt thereof, as a vaccine adjuvant with enhanced specific immune response against antigens and good preservation stability and a malaria vaccine with non-glycosylation, homogeneity, and biological activity allow for the provision of malaria transmission-blocking vaccines with good preservation stability and immunostimulatory action.

IPC Classes  ?

• A61K 39/015 - Hemosporidia antigens, e.g. Plasmodium antigens
• A61K 39/39 - Medicinal preparations containing antigens or antibodies characterised by the immunostimulating additives, e.g. chemical adjuvants
• A61P 33/06 - Antimalarials

Abstract

The present disclosure provides nanostructures (e.g., monolayer or bilayer nanostructures) comprising porphyrins with cobalt chelated thereto such that the cobalt metal resides within monolayer or bilayer in the porphyrin macrocycle. The nanostructures can have presentation molecules comprising epitopes from microorganisms with a histidine tag attached thereto, such that at least a part of the his-tag is within the monolayer or bilayer and coordinated to the cobalt metal core and the presentation molecules are exposed to the outside of the nanostructures. The nanostructures can further comprise a cargo. The nanostructures can be used to deliver the cargo to an individual.

IPC Classes  ?

• A61K 31/409 - 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 having four such rings, e.g. porphine derivatives, bilirubin, biliverdine
• A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• A61K 38/41 - Porphyrin- or corrin-ring-containing peptides

Abstract

The present disclosure provides nanostructures (e.g., monolayer or bilayer nanostructures) comprising porphyrins with cobalt chelated thereto such that the cobalt metal resides within monolayer or bilayer in the porphyrin macrocycle. The nanostructures can have presentation molecules comprising epitopes from microorganisms with a histidine tag attached thereto, such that at least a part of the his-tag is within the monolayer or bilayer and coordinated to the cobalt metal core and the presentation molecules are exposed to the outside of the nanostructures. The nanostructures can further comprise a cargo. The nanostructures can be used to deliver the cargo to an individual.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• 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 39/145 - Orthomyxoviridae, e.g. influenza virus
• A61K 39/155 - Paramyxoviridae, e.g. parainfluenza virus
• A61K 39/02 - Bacterial antigens
• C12N 7/00 - Viruses, e.g. bacteriophagesCompositions thereofPreparation or purification thereof
• A61P 31/04 - Antibacterial agents
• A61P 31/14 - Antivirals for RNA viruses
• A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
• A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

The present disclosure provides nanostructures (e.g., monolayer or bilayer nanostructures) comprising porphyrins with cobalt chelated thereto such that the cobalt metal resides within monolayer or bilayer in the porphyrin macrocycle. The nanostructures can have presentation molecules with a histidine tag attached thereto, such that at least a part of the his-tag is within the monolayer or bilayer and coordinated to the cobalt metal core and the presentation molecules are exposed to the outside of the nanostructures. The nanostructures can further comprise a cargo. The nanostructures can be used to deliver the cargo to an individual.

IPC Classes  ?

• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• 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 38/41 - Porphyrin- or corrin-ring-containing peptides
• A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• C07K 14/795 - Porphyrin- or corrin-ring-containing peptides
• A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
• 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
• B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery

Abstract

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

IPC Classes  ?

• A61K 31/4245 - Oxadiazoles
• C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles

Abstract

The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas Ia, Ib, IIa, and IIb) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

IPC Classes  ?

• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/415 - 1,2-Diazoles
• C07D 231/20 - One oxygen atom attached in position 3 or 5
• C07D 403/12 - 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 linked by a chain containing hetero atoms as chain links
• A61P 1/12 - Antidiarrhoeals

Abstract

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

IPC Classes  ?

• A61K 31/4245 - Oxadiazoles
• C07D 271/06 - 1,2,4-OxadiazolesHydrogenated 1,2,4-oxadiazoles

Abstract

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-II) or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

IPC Classes  ?

• A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
• C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

Abstract

The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of the functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a cyclic or acyclic hydrazine derivative including those of formulas II or III: or compositions thereof, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.

IPC Classes  ?

• A01N 43/56 - 1,2-DiazolesHydrogenated 1,2-diazoles
• A61K 31/415 - 1,2-Diazoles
• C07D 401/00 - 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

Abstract

A contraceptive or non-contraceptive diaphragm having a rim (108) surrounding a thin membrane (110), the membrane having a cervical dome extending downwardly from a posterior portion of the membrane. The rim has a spring member (109) having non-uniform bending characteristics. The shape of the spring member can be contoured to provide a rim that curves slightly upwardly at the anterior end of the diaphragm and slightly downwardly at its posterior end.

IPC Classes  ?

• A61F 6/08 - Pessaries, i.e. devices worn in the vagina to support the uterus, remedy a malposition or prevent conception