A liver-targeted drug and therapeutic use thereof for diseases requiring drug action in the liver are disclosed. A method in which a substance having activity with respect to glucagon is used so as to induce delivery of the liver-targeted drug to liver tissues or an increase in distribution of the drug in liver tissues after in vivo administration.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A liver-targeted drug and therapeutic use thereof for diseases requiring drug action in the liver are disclosed. Additionally, a method in which a substance having activity on glucagon is used so as to induce delivery of the drug to the liver tissue or an increase in distribution of the drug in the liver tissue after in vivo administration.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 14/00 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
Provided are mRNA comprising a non-natural 5'UTR exhibiting excellent activity in increasing an mRNA synthesis yield of a gene, a composition comprising the mRNA, a composition for delivering the mRNA or a polypeptide expressed thereby to an individual, and DNA encoding the mRNA.
Provided are: an mRNA comprising a non-natural 3'UTR having excellent activity of increasing the mRNA synthesis yield of a gene; a composition comprising the mRNA; a composition, comprising the mRNA, for delivering an mRNA or a polypeptide to an individual; and a DNA encoding the mRNA.
Provided are: an mRNA molecule comprising a modified polyadenylation sequence; a composition for delivering, to an individual, the mRNA or a product expressed by the mRNA; a method for delivering, to a host cell, the mRNA or a product expressed by the mRNA; a DNA molecule that encodes the mRNA molecule; and use thereof.
Provided are: an mRNA molecule comprising an OX40L extracellular domain-containing polypeptide-coding sequence and a modified polyadenylation sequence; a composition for delivering, to an individual, the mRNA or a product expressed by the mRNA; a method for delivering, to a host cell, the mRNA or a product expressed by the mRNA; and a nucleic acid molecule that encodes the mRNA molecule.
Provided are: a mRNA including a 5'UTR, a p53 coding sequence, and a 3'UTR; a composition for delivering mRNA or p53 to a subject, and a pharmaceutical composition for preventing or treating cancer, each comprising the mRNA; and a method for preventing or treating cancer.
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C12N 15/67 - General methods for enhancing the expression
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
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
8.
NUCLEIC ACID MOLECULE COMPRISING MODIFIED POLYADENYLATION SEQUENCE AND P53 PROTEIN CODING SEQUENCE
The present invention provides an mRNA molecule comprising a p53 protein coding sequence and a modified polyadenylation sequence, a composition for delivering the mRNA or a product expressed thereby to a subject, a method for delivering the mRNA or a product expressed thereby to a host cell, and a DNA molecule encoding the mRNA molecule.
C12N 15/11 - DNA or RNA fragmentsModified forms thereof
C12N 15/67 - General methods for enhancing the expression
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
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
A compound defined by chemical formula 1, a stereoisomer thereof, a tautomer thereof, and a pharmaceutically acceptable salt thereof are provided. The compound of the present invention can inhibit the activity of HER2 kinase. In chemical formula 1, R1to R3, A1to A4, L1nn are the same as those defined in the present specification.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 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
The present invention relates to a lyophilized formulation including a fusion protein of α-galactosidase A and a preparation method thereof, wherein the lyophilized formulation not only has storage stability by including a composition providing structural stability to a fusion protein of α-galactosidase A, but also has excellent stability although the fusion protein is contained at a high concentration.
The present disclosure relates to a thieno[3,2-d]pyrimidine derivative compound which is useful as a PIKfyve kinase inhibitor, a pharmaceutically acceptable salt thereof, a preparation method thereof, and an intermediate thereof.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
14.
METHOD FOR PREPARING ORAL COMPOSITE TABLET CONTAINING PROTON PUMP INHIBITOR AND ANTACID AND ORAL COMPOSITE TABLET PREPARED THEREBY
A method for preparing an oral composite tablet containing a proton pump inhibitor and an antacid and an oral composite tablet prepared by the method are disclosed. The method prepare an oral composite tablet with excellent appearance stability and high productivity. The proton pump inhibitor includes esomeprazole, omeprazole, lansoprazole, rabeprazole, pantoprazole, or combinations thereof.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 9/24 - Layered or laminated unitary dosage forms
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
This invention relates to pharmaceutical compositions, pharmaceutical combinations and methods for the treatment of acute myeloid leukemia by combined use of a therapeutically effective combination of a compound of Chemical Formula 1, or a pharmaceutically acceptable salt thereof, solvate thereof, stereoisomer thereof, tautomer thereof, or combination thereof, wherein Ea, Eb, Ec, Ed, Z′, X′, Q, and k are defined herein; and a Bcl-2 inhibitor, or a Bcl-2 inhibitor and a hypomethylating agent.
This invention relates to pharmaceutical compositions, pharmaceutical combinations and methods for the treatment of acute myeloid leukemia by combined use of a therapeutically effective combination of a compound of Chemical Formula 1, or a pharmaceutically acceptable salt thereof, solvate thereof, stereoisomer thereof, tautomer thereof, or combination thereof, wherein Ea, Eb, Ec, Ed, Z′, X′, Q, and k are defined herein; and a Bcl-2 inhibitor, or a Bcl-2 inhibitor and a hypomethylating agent.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61P 35/02 - Antineoplastic agents specific for leukemia
16.
SOLID DISPERSION OF MYELOID KINOME INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 35/02 - Antineoplastic agents specific for leukemia
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
17.
COMBINATION THERAPY WITH BELVARAFENIB AND COBIMETINIB OR WITH BELVARAFENIB, COBIMETINIB, AND ATEZOLIZUMAB
Combination therapies comprising belvarafenib and cobimetinib and comprising belvarafenib, cobimetinib, and atezolizumab are provided for the treatment of melanoma carrying a NRAS mutation.
A composition, suitable for an orally administered formulation, contains a GLP-1 analogue and, particularly, a hydrophobic ion-pair of a GLP-1 analogue and an oil phase. The pharmaceutical composition for oral administration forms an emulsion surrounding the hydrophobic ion-pair when exposed to a water phase, so as to be stably absorbed without being decomposed by digestive enzymes, and thus provides an effective and prolonged pharmacological effect. Methods for producing the composition for oral administration are also disclosed.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
19.
COMBINATION FORMULATION COMPRISING SACUBITRIL-VALSARTAN AND SGLT-2 INHIBITOR HAVING IMPROVED STABILITY AND DISSOLUTION RATE
The present invention relates to a pharmaceutical combination formulation comprising both sacubitril-valsartan and an SGLT-2 inhibitor as active ingredients, and having a synergistic effect in the treatment of heart failure while also minimizing the influence of dissolution between each drug, thereby ensuring bioequivalence, and suppressing generation of related substances, thereby also providing excellent stability of the active ingredients.
A61K 9/24 - Layered or laminated unitary dosage forms
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
20.
ORAL COMPLEX TABLET COMPRISING SITAGLIPTIN, DAPAGLIFLOZIN, AND METFORMIN
An oral dosage form in a form of a bi-layer complex tablet is disclosed. The bi-layer oral complex tablet contains colloidal silicon dioxide in an amount of 0.5 to 2% by weight based on a total weight of the first layer. A method for manufacturing the bi-layer oral complex tablet dosage form is also disclosed.
A61K 31/351 - 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 not condensed with another ring
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
21.
NON-NATURAL 5'-UNTRANSLATED REGION AND 3'-UNTRANSLATED REGION AND USE THEREOF
Provided is an isolated polynucleotide including a nucleotide sequence coding for a non-natural 5-untranslated region (5′-UTR) and a nucleotide sequence coding for a non-natural or natural 3-untranslated region (3′-UTR). As such, the polynucleotide increases mRNA stabilization and translation efficiency and thus can be used for effectively acquiring a desired polypeptide.
The present invention relates to the combined use of an interleukin-2 analog or a conjugate thereof and an immune checkpoint inhibitor for the prevention or treatment of cancer, and a pharmaceutical composition comprising the same.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present invention relates to a combination therapy using an insulinotropic peptide and GLP-2 for the prevention, improvement, or treatment of short bowel syndrome.
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The present invention relates to a pharmaceutical composition for preventing or treating cancer, including an Interleukin 2 analog or a conjugate thereof.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A combination including a peptide having activities to all of glucagon, GLP-1, and GIP receptors or a conjugate thereof; and an SGLT-2 inhibitor is disclosed. Uses of the combination are also disclosed. The combination is suitable for use in treating metabolic syndrome, liver disease, lung disease, or respiratory infections in a subject in need thereof.
A61K 31/351 - 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 not condensed with another ring
A61K 31/382 - Heterocyclic compounds having sulfur as a ring hetero atom having six-membered rings, e.g. thioxanthenes
A61K 31/7042 - Compounds having saccharide radicals and heterocyclic rings
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Provided are a use, a pharmaceutical composition, and a method for efpeglenatide for reducing a risk of developing a cardiovascular disease or renal dysfunction. The efpeglenatide may be used for cardiovascular or renal protection of patients having type 2 diabetes who have or are at risk of a cardiovascular disease or renal disease.
A combination therapy comprising a RAF inhibitor and a PD-1 axis inhibitor is provided for the treatment of cancer characterized by a mutated MAPK signaling pathway.
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 39/00 - Medicinal preparations containing antigens or antibodies
NOVEL TRIPLE ACTIVATOR HAVING ACTIVITY ON ALL OF GLP-1, GIP, AND GLUCAGON RECEPTORS, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING OBESITY COMPRISING SAME
The present invention relates to a novel trigonal agonist having activity on all of GLP-1, GIP, and glucagon receptors, and uses thereof in the prevention or treatment of obesity.
The present invention pertains to a prophylactic or therapeutic use of a GLP-2 derivative and/or a long-acting conjugate thereof against graft-versus-host disease. In addition, the present invention pertains to a prophylactic or therapeutic use of a combination of a GLP-2 derivative and/or a long-acting conjugate thereof and a steroid against steroid-resistant graft-versus-host disease.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/56 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
Provided are an antigenic peptide having multiple KRAS variant peptides linked thereto, mRNA encoding same, DNA encoding same, an immunogenic composition comprising an antigenic peptide having multiple KRAS variant peptides linked thereto or an mRNA encoding same, and a method for inducing an immune response to the KRAS variant peptides in a subject.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 9/19 - Particulate form, e.g. powders lyophilised
Provided are a glucagon derivative and use thereof. The pharmaceutical composition contains a glucagon derivative and a pharmaceutically acceptable excipient, wherein the glucagon derivative is a peptide including an amino acid sequence of the following General Formula 1: X1-X2-QGTF-X7-SD-X10-S-X12-X13-X14-X15-X16-X17-X18-X19-X20-X21-F-X23-X24-W-L-X27-X28-X29-X30 (General Formula 1, SEQ ID NO: 46). A method for treating chronic renal disease is also disclosed.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
33.
BELVARAFENIB FOR USE IN TREATMENT OF BRAIN CANCERS
Provided are methods for the use of belvarafenib to treat brain cancer including metastatic brain cancer carrying a BRAF mutation, a NRAS mutation, a KRAS mutation, or a combination thereof.
The present disclosure relates to solid forms of pyrimidine compounds, pharmaceutical compositions including the same and methods of use thereof. For example, the disclosure relates to crystalline polymorphs of a compound of Formula 1, or a pharmaceutically acceptable salt, solvate, or solvate salt thereof.
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 35/02 - Antineoplastic agents specific for leukemia
35.
NOVEL TRICYCLIC DERIVATIVE COMPOUND AND USES THEREOF
The present invention relates to a novel tricycle derivative compound and uses thereof, more specifically to a novel tricycle derivative compound having inhibitory activity for methionine adenosyltransferase 2A (MAT2A) and uses thereof.
A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
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
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
36.
NOVEL PYRIMIDINE DERIVATIVE AS BRUTON'S TYROSINE KINASE INHIBITOR
The present disclosure relates to a novel pyrimidine derivative, a solvate or stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including any of the foregoing as an active ingredient, the pyrimidine derivative being represented by Formula I and having inhibitory activity against Bruton's tyrosine kinase. The novel pyrimidine derivative of the present disclosure effectively inhibits the enzymatic activity of Bruton's tyrosine kinase (BTK), and thus may be useful as an active ingredient in a pharmaceutical composition for preventing or treating BTK-mediated disease such as autoimmune disease or cancer: [Formula I]
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 403/10 - 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 carbon chain containing aromatic rings
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
37.
NOVEL HETEROBICYCLIC COMPOUND FOR INHIBITING YAP-TEAD INTERACTION AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Provided are a compound, selected from compounds of Formula 1, enantiomers, diastereomers, solvates and hydrates thereof, and pharmaceutically acceptable salts thereof, methods of preparing the same, and use thereof.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
38.
NOVEL HETEROBICYCLIC COMPOUND FOR INHIBITING YAP-TEAD INTERACTION AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Provided are a compound, selected from compounds of Formula 1, enantiomers, diastereomers, solvates and hydrates thereof, and pharmaceutically acceptable salts thereof, a method of manufacturing the same, and use thereof.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
NOVEL GLP-1 RECEPTOR ANTAGONIST, AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING CONGENITAL HYPERINSULINEMIA OR HYPOGLYCEMIA, COMPRISING SAME
The present invention relates to a novel GLP-1 receptor antagonist analogue and an acylated GLP-1 receptor analogue, and use thereof for preventing or treating congenital hyperinsulinemia or hypoglycemia.
A61P 3/08 - Drugs for disorders of the metabolism for glucose homeostasis
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
40.
NOVEL TRICYCLIC HETEROCYCLIC CARBALDEHYDE COMPOUND AND PHARMACEUTICAL COMPOSITION, CONTAINING SAME, FOR IRE1α INHIBITION
The present invention relates to a novel tricyclic heterocyclic carbaldehyde compound and a pharmaceutical composition, containing same, for IRE1α inhibition and, more specifically, to a novel tricyclic heterocyclic carbaldehyde compound and a pharmaceutical composition, containing same, for treatment or prevention of IRE1α-related diseases.
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4025 - 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 not condensed and containing further heterocyclic rings, e.g. cromakalim
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
One aspect provides a pharmaceutical composition and a pharmaceutical combination formulation contains the same, the pharmaceutical composition containing as active ingredients: a proton pump inhibitor or a pharmaceutically acceptable salt thereof; and an antacid selected from magnesium hydroxide, magnesium oxide, or a mixture thereof.
A61K 9/24 - Layered or laminated unitary dosage forms
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
42.
LIQUID FORMULATION OF PROTEIN AND METHODS OF PREPARING THE SAME
Provided are a liquid formulation of protein and a method of preparing the same. According to a liquid formulation containing a high concentrate of eflapegrastim and a method of preparing the same, the liquid formulation may have excellent solubility and stability, may have a high concentration of protein, and may be injected in a patient-friendly manner due to reduced irritation/pain at the administration site or patient discomfort.
A method for lowering blood pressure is disclosed. The method includes administering a pharmaceutical composition to a subject in need thereof, wherein the composition contains a pharmaceutically acceptable excipient; and a peptide having an amino acid sequence of any one of SEQ ID NOS: 1 to 102. The peptide is in a form of a long-acting conjugate.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A use of a fusion protein of a therapeutic enzyme and an immunoglobulin Fe region is disclosed. The fusion protein is represented by the following chemical formula 1. The fusion protein shows protective effects on peripheral sensory nerves and exhibits an extended duration in the body. Thus, the fusion protein or a composition containing the fusion protein can be used in the prevention or improvement of neuropathy.
A use of a fusion protein of a therapeutic enzyme and an immunoglobulin Fe region is disclosed. The fusion protein is represented by the following chemical formula 1. The fusion protein shows protective effects on peripheral sensory nerves and exhibits an extended duration in the body. Thus, the fusion protein or a composition containing the fusion protein can be used in the prevention or improvement of neuropathy.
The present invention relates to use of a fusion protein of a therapeutic enzyme and an immunoglobulin Fc region in the prevention or improvement of renal diseases caused by or accompanied by Fabry disease.
A61K 38/47 - Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
47.
USE OF TRIGONAL AGONIST HAVING ACTIVITIES TO ALL OF GLUCAGON, GLP-1, AND GIP RECEPTORS IN TREATMENT OF SEQUELAE FOLLOWING RESPIRATORY INFECTIOUS DISEASES
Provided is use of a trigonal agonist having activities to all of glucagon, GLP-1, and GIP receptors, and/or a conjugate thereof in the prevention or treatment of sequelae following respiratory infectious diseases.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 11/00 - Drugs for disorders of the respiratory system
48.
PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING LUPUS-RELATED DISEASES COMPRISING GIP DERIVATIVE OR LONG-ACTING CONJUGATE THEREOF
Provided is a pharmaceutical composition for preventing or treating lupus-associated disease, including a GIP derivative, a pharmaceutically acceptable salt or solvate thereof, or a long-acting conjugate thereof.
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
49.
PHARMACEUTICAL COMPOSITION COMPRISING GLUCAGON/GLP-1/GIP TRIPLE AGONIST OR LONG-ACTING CONJUGATE THEREOF FOR PREVENTING OR TREATING LUPUS-RELATED DISEASES
Provided is a pharmaceutical composition for preventing or treating lupus-associated disease, including a glucagon/GLP-1/GIP triple agonist, a pharmaceutically acceptable salt thereof, a solvate thereof, or a long-acting conjugate thereof.
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
50.
NOVEL TRIPLE AGONIST HAVING ACTIVITIES ON ALL OF GLUCAGON, GLP-1, AND GIP RECEPTORS AND USE THEREOF
C07K 14/72 - ReceptorsCell surface antigensCell surface determinants for hormones
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
51.
GIP DERIVATIVE, LONG-ACTING CONJUGATE THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Provided are a GIP derivative, a pharmaceutically acceptable salt or solvate thereof, or a long-acting conjugate thereof, or a pharmaceutical composition including the same for preventing or treating inflammatory or autoimmune disease.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
52.
GLP-1/GIP DUAL AGONIST, LONG-ACTING CONJUGATE THEREOF, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
Provided is a GLP-1/GIP dual agonist, a pharmaceutically acceptable salt thereof, a solvate thereof, or a long-acting conjugate thereof, or a pharmaceutical composition for preventing or treating diabetes including the same.
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
53.
PHARMACEUTICAL COMPOSITION COMPRISING GLUCAGON/GLP-1/GIP TRIPLE AGONIST OR LONG-ACTING CONJUGATE THEREOF FOR PREVENTING OR TREATING VASCULITIS
Provided is a pharmaceutical composition for preventing or treating vasculitis, including a glucagon/GLP-1/GIP triple agonist, a pharmaceutically acceptable salt thereof, a solvate thereof, or a long-acting conjugate thereof.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
New therapeutic uses of a triple agonist and/or a long-acting conjugate thereof are disclosed. The triple agonist and/or a long-acting conjugate thereof acts on all of glucagon, GLP-1 and GIP receptors, and is useful in treating multiple sclerosis. Thus, patients' options can be broadened by expanding the category of drugs applicable to multiple sclerosis and patients' convenience can be increased by significantly increasing blood half-life.
A61P 25/00 - Drugs for disorders of the nervous system
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
55.
THERAPEUTIC USE, FOR NEURODEGENERATIVE DISEASES, OF TRIPLE AGONIST HAVING ACTIVITY WITH RESPECT TO ALL OF GLUCAGON, GLP-1, AND GIP RECEPTORS, OR CONJUGATE THEREOF
New therapeutic uses of a triple agonist and/or a long-acting conjugate thereof are disclosed. The triple agonist and/or a long-acting conjugate thereof acts on all of glucagon receptor, glucagon-like peptide-1 (GLP-1) receptor, and glucose-dependent insulinotropic polypeptide (GIP) receptor, and is useful in treating neurodegenerative diseases. Thus, patients’ options can be broadened by expanding the category of drugs applicable to applicable to neurodegenerative diseases, and can increase convenience for patients by significantly increasing blood half-life.
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
56.
PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING BONE DISEASES, COMPRISING TRIPLE AGONIST OR CONJUGATE THEREOF HAVING ACTIVITY WITH RESPECT TO ALL OF GLUCAGON, GLP-1 AND GLP RECEPTORS
A therapeutic use of a triple agonist and/or a long-acting conjugate thereof having activity with respect to all of glucagon, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors is disclosed. The triple agonist and/or the long-acting conjugate thereof can significantly reduce symptoms of bone diseases, and enhance patient convenience through a dramatic increase in blood half-life and long-acting in-vivo effects.
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
57.
POLYETHYLENE GLYCOL DERIVATIVE, COMPOSITION COMPRISING SAME, AND METHOD FOR PREPARING BIOACTIVE POLYPEPTIDE CONJUGATE BY USING SAME
A polyethylene glycol derivative compound is represented by Formula 1 described in the detailed description. In Formula 1, n is a natural number of 30 to 115, and R1 and R2 are C1 to C5 alkyl that are identical to or different from each other.
C08G 65/331 - Polymers modified by chemical after-treatment with organic compounds containing oxygen
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
Modifications to interleukin-2 alpha receptors are disclosed. Interleukin-2 analogs with increased binding affinity for interleukin-2 beta receptors are disclosed.
The present invention relates to a combination therapy of GLP-2 with an insulinotropic peptide, a TNFα inhibitor or both for preventing, alleviating or treating intestinal diseases.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
The present invention relates to a pharmaceutical composition comprising: a first unit including acetylsalicylic acid or a pharmaceutically acceptable salt thereof; and a second unit comprising a proton pump inhibitor. The pharmaceutical composition according to the present invention is divided into the first unit and the second unit, thus preventing direct contact between the drugs. Therefore, stability is achieved and the effect on the individual release of the respective drugs is minimized, and thus improved elution is exhibited.
A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
61.
METHODS OF TREATING NEUTORPENIA USING G-CSF PROTEIN COMPLEX
This disclosure provides a method of preventing, alleviating or treating a condition (i.e., neutropenia) in a subject in need thereof, the condition characterized by compromised white blood cell production in the subject. The method includes administering to the subject a therapeutically effective amount of a protein complex on the same day as a chemotherapy regimen, wherein the protein complex is a modified human granulocyte-colony stimulating factor (hG-CSF) covalently linked to an immunoglobulin Fc region via a non-peptidyl polymer. The non-peptidyl polymer is site-specifically linked to an N-terminus of the immunoglobulin Fc region, and the modified hG-CSF comprises substitutions in at least one of Cys17 and Pro65.
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
62.
THERAPEUTIC USE OF COMBINATION COMPRISING TRIPLE AGONISTIC LONG-ACTING CONJUGATE OR TRIPLE AGONIST
New therapeutic uses of a triple agonistic long-acting conjugate or a triple and a farnesoid X receptor (FXR) agonist, or a combination further containing an acetyl-CoA carboxylase (ACC) inhibitor are disclosed. The triple agonistic long-acting conjugate or a triple and a farnesoid X receptor (FXR) agonist, or a combination further containing an acetyl-CoA carboxylase (ACC) inhibitor, may be for preventing or treating a liver disease.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
63.
THERAPEUTIC USE OF GLUCAGON DERIVATIVE OR CONJUGATE THEREOF FOR LIVER DISEASE
New therapeutic uses of a glucagon derivative or a conjugate thereof are disclosed. The glucagon derivative or a conjugate thereof is represented by the following formula: Y-X2-QGTF-X7-SDYSKY-X14-D-X16-X17-R-X19-X20-X21-FVQWLMNT-X30 (General Formula 1, SEQ ID NO: 46), and is effective in preventing or treating a liver disease. Therefore, the glucagon derivative or a conjugate thereof, or a pharmaceutical composition containing it as an active ingredient may be for preventing or treating a liver disease.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
64.
PHARMACEUTICAL COMPOSITION COMPRISING LONG-ACTING CONJUGATE OF TRIPLE GLUCAGON/GLP-1/GIP RECEPTOR AGONIST
Provided are a pharmaceutical composition including a long-acting conjugate of a triple agonist as an active ingredient and a method of treating obesity and/or a non-alcoholic fatty liver disease using the same. The pharmaceutical composition including the long-acting conjugate of the triple agonist of the present invention may be stably applied to treatment of obesity and/or a non-alcoholic fatty liver disease without side effects according to therapeutic effects on obesity and/or the non-alcoholic fatty liver disease.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
65.
LYOPHILIZED FORMULATION COMPRISING A FUSION PROTEIN INCLUDING α-GALACTOSIDASE A
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
66.
LYOPHILIZED FORMULATION COMPRISING A FUSION PROTEIN INCLUDING α-GALACTOSIDASE A
The present invention relates to a lyophilized formulation including a fusion protein of α-galactosidase A and a preparation method thereof, wherein the lyophilized formulation not only has storage stability by including a composition providing structural stability to a fusion protein of α-galactosidase A, but also has excellent stability although the fusion protein is contained at a high concentration.
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
A61K 38/47 - Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
68.
LIQUID FORMULATION COMPRISING A FUSION PROTEIN INCLUDING α-GALACTOSIDASE A
The present invention relates to a liquid formulation including a fusion protein of α-galactosidase A and a preparation method thereof, wherein the liquid formulation not only has storage stability by including a composition providing structural stability to a fusion protein of α-galactosidase A, but also has excellent stability although the fusion protein is contained at a high concentration.
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
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
A61K 38/47 - Hydrolases (3) acting on glycosyl compounds (3.2), e.g. cellulases, lactases
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 9/00 - Medicinal preparations characterised by special physical form
A liquid formulation of a long-acting conjugate of glucagon, GLP-1, and GIP trigonal agonist, and a method for preparing the liquid formulation are disclosed. The liquid formulation contains 18 nmol/mL to 920 nmol/mL of a long-acting conjugate, a buffering agent in an amount for maintaining the pH of the liquid formulation in the range of 5.0 to 7.0, and 0.5% (w/v) to 10% (w/v) of a sugar alcohol, saccharide, or a combination thereof.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
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
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
70.
LIQUID FORMULATION OF LONG-ACTING CONJUGATE OF GLP-2
A liquid formulation of a long-acting conjugate of GLP-2 and a method for preparing the liquid formulation are disclosed. The liquid formulation contains 18 nmol/mL to 18,630 nmol/mL of a long-acting conjugate, a stabilizer, and a buffering agent in an amount for maintaining the pH of the liquid formulation in the range of 4.5 to 6.5.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
71.
COMPOSITE FORMULATION COMPRISING SITAGLIPTIN AND DAPAGLIFLOZIN AND PREPARATION METHOD THEREFOR
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
72.
NOVEL METHOD FOR PREPARING LONG-ACTING DRUG CONJUGATE THROUGH PREPARATION OF INTERMEDIATE
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
Provided are a pharmaceutical composite formulation and a method of preparing the same, the pharmaceutical composite formulation including: a first layer containing, as an active ingredient, a proton pump inhibitor or a pharmaceutically acceptable salt thereof and a lubricant, and a second layer containing, as an active ingredient, an antacid selected from magnesium hydroxide, magnesium oxide, and a mixture thereof.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Provided are methods for the use of belvarafenib to treat cancer having at least one mutation selected from a BRAFV600E mutation, a KRASG12V mutation, a KRASG12D mutation, a KRASG12C mutation, a KRASG12R mutation, a KRASG13D mutation, a KRASQ61H mutation, a NRASG12D mutation, a NRASG13D mutation, a NRASQ61K mutation, a NRASQ61L mutation, a NRASQ61R mutation, and a NRASG12C mutation.
A method for improving the solubility of a physiologically active protein or peptide compared to that of a physiologically active protein or peptide which is not conjugated to an immunoglobulin Fc fragment is disclosed. The method includes steps of conjugating the physiologically active protein or peptide to an immunoglobulin Fc fragment. Also disclosed is a composition for improving the solubility of a physiologically active protein or peptide, which contains an immunoglobulin Fc fragment. The composition improves the solubility compared to a composition without an immunoglobulin Fc fragment.
A liquid formulation of a long-acting conjugate of a peptide having activities for a glucagon receptor and a GLP-1 receptor, and a method for preparing the liquid formulation are disclosed. The liquid formulation contains 18 nmol/mL to 940 nmol/mL of the long-acting conjugate, a buffering agent in an amount for maintaining the pH of the liquid formulation in the range of 4.5 to 7.5, and 1% (w/v) to 20% (w/v) of saccharide, and 0.001% (w/v) to 0.2% (w/v) of a nonionic surfactant.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
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
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Polyethylene glycol derivatives of the following formula I and uses thereof are disclosed. A method for manufacturing the polyethylene glycol derivatives is also disclosed.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
C07C 233/05 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 233/18 - 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 singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
C07C 237/04 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
C07C 323/12 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and singly-bound oxygen atoms bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
C07C 323/22 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and doubly-bound oxygen atoms bound to the same carbon skeleton
C07C 323/39 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
C07D 213/71 - Sulfur atoms to which a second hetero atom is attached
The present invention relates to a liver-targeted drug, and therapeutic use thereof for diseases requiring drug action in the liver. In addition, the present invention relates to a method in which a substance having activity with respect to glucagon is used so as to induce targeting of liver tissues or an increase in distribution in liver tissues after in vivo administration.
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
The present invention relates to a liver-targeted drug, and therapeutic use thereof for diseases requiring drug action in the liver. In addition, the present invention relates to a method in which a substance having activity with respect to glucagon is used so as to induce targeting of liver tissues or an increase in distribution in liver tissues after in vivo administration.
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
81.
METHOD FOR PREPARING ORAL COMPOSITE TABLET CONTAINING PROTON PUMP INHIBITOR AND ANTACID AND ORAL COMPOSITE TABLET PREPARED THEREBY
The present invention relates to a method for preparing an oral composite tablet containing a proton pump inhibitor and an antacid and an oral composite tablet prepared thereby and, more specifically, to a method for preparing an oral composite tablet superb in terms of property stability and productivity.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 33/00 - Medicinal preparations containing inorganic active ingredients
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
The present invention relates to an interleukin 2 analogue, which has greater binding affinity for an interleukin 2 alpha receptor than the wild type thereof.
A liquid formulation of a long-acting conjugate of glucagon, and a method for preparing the liquid formulation are disclosed. The liquid formulation contains 18 nmol/mL to 936 nmol/mL of a long-acting conjugate, a buffering agent in an amount for maintaining the pH of the liquid formulation in the range of 4.8 to 6.5, and 1.0% (w/v) to 20% (w/v) of a sugar alcohol, saccharide, or a combination thereof
C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
COMPOSITION FOR PREVENTION OR TREATMENT OF HYPERLIPIDEMIA COMPRISING TRIGONAL GLUCAGON/GLP-1/GIP RECEPTOR AGONIST OR CONJUGATE THEREOF AND METHOD USING THE SAME
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
C07K 14/72 - ReceptorsCell surface antigensCell surface determinants for hormones
86.
PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING MUCOSITIS INDUCED BY RADIOTHERAPY, CHEMOTHERAPY, OR COMBINATION THEREOF, COMPRISING GLP-2 DERIVATIVES OR LONG-ACTING CONJUGATE OF SAME
A use of GLP-2 and a long-acting conjugate thereof for preventing or treating mucositis induced by radiotherapy, chemotherapy, or a combination thereof is disclosed. The GLP-2, the long-acting conjugate thereof, or the composition including the same may be applied to preparation, treatment, and amelioration of mucositis induced by radiotherapy and/or chemotherapy.
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/04 - Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
87.
ORAL COMPLEX TABLET COMPRISING SITAGLIPTIN, DAPAGLIFLOZIN, AND METFORMIN
According to an aspect, provided are a composite tablet and a method of preparing the composite tablet, wherein the composite tablet may include a first layer including dry granules that include sitagliptin or a pharmaceutically acceptable salt thereof, or a hydrate thereof, and dapagliflozin or a pharmaceutically acceptable salt thereof, or a hydrate thereof, and a second layer including wet granules that include metformin or a pharmaceutically acceptable salt thereof and colloidal silicon dioxide.
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
One aspect of the present invention provides a compound in which a functional group capable of binding to a globulin Fc region or a physiologically active polypeptide is introduced at one end of a non-peptidic polymer and a functional group capable of a click reaction is introduced at the other end; a polypeptide conjugate in which a physiologically active polypeptide binds to one end of the compound; a physiologically active polypeptide conjugate in which a physiologically active polypeptide and an immunoglobulin Fc region bind to both ends thereof by using the compound as a linker; and methods for preparing the same compound, polypeptide conjugate, and physiologically active polypeptide conjugate.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
C07D 225/08 - Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with two six-membered rings
89.
THERAPEUTICALLY EFFECTIVE COMBINATION OF A FLT3 INHIBITOR AND A BCL-2 INHIBITOR FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA
This invention relates to pharmaceutical compositions, pharmaceutical combinations and methods for the treatment of acute myeloid leukemia by combined use of a therapeutically effective combination of a compound of Chemical Formula 1, or a pharmaceutically acceptable salt thereof, solvate thereof, stereoisomer thereof, tautomer thereof, or combination thereof, wherein Ea, Eb, Ec, Ed, Z', X', Q, and k are defined herein; and a Bcl-2 inhibitor, or a Bcl-2 inhibitor and a hypomethylating agent.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
90.
THERAPEUTICALLY EFFECTIVE COMBINATION OF A FLT3 INHIBITOR AND A BCL-2 INHIBITOR FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA
This invention relates to pharmaceutical compositions, pharmaceutical combinations and methods for the treatment of acute myeloid leukemia by combined use of a therapeutically effective combination of a compound of Chemical Formula 1, or a pharmaceutically acceptable salt thereof, solvate thereof, stereoisomer thereof, tautomer thereof, or combination thereof, wherein Ea, Eb, Ec, Ed, Z', X', Q, and k are defined herein; and a Bcl-2 inhibitor, or a Bcl-2 inhibitor and a hypomethylating agent.
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
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
The present invention relates to changes in interleukin-2 alpha receptors and interleukin-2 analogs with increased binding affinity for interleukin-2 beta receptors.
New uses of a triple agonist are disclosed. A triple agonist having activities to all of glucagon, GLP-1, and GIP receptors, or conjugates thereof exhibits an activity of preventing and/or treating lung diseases. A use of the triple agonist or a conjugate thereof as a preventive and/or therapeutic agent for lung disease, and compositions and methods for preventing and/or treating lung cancer employing the triple agonist having activities to all of glucagon, GLP-1, and GIP receptors, and/or conjugates are disclosed.
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 11/00 - Drugs for disorders of the respiratory system
-d-d]pyrimidine derivative compound which is useful as a PIKfyve kinase inhibitor, a pharmaceutically acceptable salt of same, a method of preparing same, and an intermediate of same.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 47/60 - 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 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A glucagon-like peptide-2 (GLP-2) derivative, a conjugate thereof, and a use thereof are disclosed. The GLP-2 derivative or a conjugate thereof are useful in preventing or treating one or more diseases selected from intestinal disease, intestinal injury, or gastrosia. Additionally, a method for preparing a glucagon-like peptide-2 (GLP-2) derivative and a conjugate thereof is disclosed.
A61K 47/62 - 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 a protein, peptide or polyamino acid
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
96.
THIENO[3,2-D]PYRIMIDINE DERIVATIVE COMPOUND HAVING INHIBITORY ACTIVITY FOR PROTEIN KINASE
The present invention relates to a compound, 4-amino-N-(1-((3-chloro-2-fluoro-4-hydroxyphenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide, and pharmaceutically acceptable salts thereof having inhibitory activity for protein kinases.
An aspect provides a pharmaceutical composite formulation containing: a first layer comprising a proton pump inhibitor or a pharmaceutically acceptable salt thereof as an active ingredient, a disintegrant, and a binder; and a second layer comprising, as an active ingredient, an antacid selected from magnesium hydroxide, magnesium oxide, or a mixture thereof.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 47/58 - 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 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
98.
COMPLEX FORMULATION COMPRISING SITAGLIPTIN AND DAPAGLIFLOZIN, AND PREPARATION METHOD THEREFOR
A61K 31/351 - 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 not condensed with another ring
The present invention relates to a composition, for an orally administered formulation, containing a GLP-1 analogue and, particularly, to a pharmaceutical composition for oral administration comprising a hydrophobic ion pair of a GLP-1 analogue and an oil phase, and a method for preparing the composition. The pharmaceutical composition for oral administration of the present invention forms an emulsion surrounding the hydrophobic ion pair when exposed to a water phase, so as to be stably absorbed without being decomposed by means of digestive enzymes, and thus provides a pharmacological effect. Therefore, the present invention may be utilized as a pharmaceutical composition for oral administration.
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/44 - Oils, fats or waxes according to two or more groups of Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
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
The present invention relates to an oral complex tablet in the form of a bilayer tablet and a preparation method therefor, wherein the oral complex tablet contains colloidal silicon dioxide in an amount of 0.5 to 2 weight% on the basis of the total weight of the first layer.
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
patents
