Abstract

In one aspect. methods are provided for treating a human subject having or susceptible to mucositis, comprising administering to the human subject an effective amount of EC-18, thereby treating or preventing the mucositis.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 31/155 - Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (HN=C(OH)NH2), isothiourea (HN=C(SH)—NH2)
• A61K 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• A61K 31/728 - Hyaluronic acid
• A61K 38/08 - Peptides having 5 to 11 amino acids
• A61K 38/18 - Growth factorsGrowth regulators
• A61K 38/44 - Oxidoreductases (1)
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection

Abstract

Provided herein, inter alia, are compounds of fatty acid glycerol derivatives and compositions including the same.

IPC Classes  ?

• C07D 207/27 - 2-Pyrrolidones with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
• C07C 69/732 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
• C07C 43/15 - Unsaturated ethers containing only non-aromatic carbon-to-carbon double bonds

Abstract

In one aspect, methods are provided for treating a human subject having or susceptible to mucositis, comprising administering to the human subject an effective amount of EC-18, thereby treating or preventing the mucositis.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 1/02 - Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis

Abstract

In one aspect, methods and compositions are provided for treating a neoplasia such as a solid tumor, the methods and composition comprising a) one or more chemotherapeutic agents such as a checkpoint inhibitor or doxorubicin and/or cyclophosamide; and b) a monoacetyl diacylglycerol compound such as 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG)

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• 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 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61P 35/00 - Antineoplastic agents

Abstract

In one aspect, methods for modulating an inflammatory response are provided comprising administration to a cell or organism a monoacetyl diacylglycerol compound.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection

Abstract

In one aspect, methods and compositions are provided for treating a neoplasia such as a solid tumor, the methods and composition comprising a) a granulocyte colony-stimulating factor (G-CSF) compound; and b) a monoacetyl diacylglycerol compound such as 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG).

IPC Classes  ?

• A61K 38/19 - CytokinesLymphokinesInterferons
• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• 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 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 33/243 - PlatinumCompounds thereof
• A61K 31/7068 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 31/10 - SulfidesSulfoxidesSulfones
• A61P 35/00 - Antineoplastic agents

Abstract

inter aliainter alia, are compounds of fatty acid glycerol derivatives and compositions including the same.

IPC Classes  ?

• C07D 307/32 - Oxygen atoms
• C07D 309/30 - Oxygen atoms, e.g. delta-lactones
• C07D 275/03 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
• C07D 279/02 - 1,2-ThiazinesHydrogenated 1,2-thiazines
• C07C 69/602 - Dicarboxylic acid esters having at least two carbon-to-carbon double bonds
• C07C 43/15 - Unsaturated ethers containing only non-aromatic carbon-to-carbon double bonds
• C07C 69/732 - Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety of unsaturated acids of unsaturated hydroxy carboxylic acids
• A61P 39/00 - General protective or antinoxious agents
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system

Abstract

It is disclosed a method for preparing calteridol used as MRI contrast agents. It provides a method for preparing calteridol comprising: obtaining teridol represented by the following Formula 2 by reacting gadoteridol represented by the following Formula 1 with decomplexing agent; and obtaining calteridol represented by the following Formula 3 by reacting calcium ion with teridol represented by following Formula 2.

IPC Classes  ?

• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings

Abstract

In one aspect, methods, compositions and kits for treating a COV-19 infection or symptoms of a COV-19 infection are provided and comprise use of a compound of Formula 1: wherein R1 and R2 are independently a fatty acid residue of 14 to 22 carbon atoms.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 31/14 - Antivirals for RNA viruses

Abstract

Disclosed are a glycerol derivative that is useful for improving, preventing or treating inflammation-related diseases by inhibiting overexpression of various inflammatory cytokines such as IL-4, IL-6 and so on, or chemokine CXCL8 and reducing migration of HL-60 cell lines, preparation method therefor, and an immunomodulator containing the same as active ingredient. It includes a glycerol derivative represented by Chemical formula 2 or 3 in the specification.

IPC Classes  ?

• C07C 233/20 - 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 carbon atom of an acyclic unsaturated carbon skeleton
• 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 233/38 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a carbon atom of an acyclic unsaturated carbon skeleton
• C07C 327/28 - Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
• C07C 235/06 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• C07C 69/708 - Ethers
• A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection

Abstract

In one aspect, methods and compositions are provided for treating a neoplasia such as a solid tumor, the methods and composition comprising a) one or more chemotherapeutic agents such as a checkpoint inhibitor or doxorubicin and/or cyclophosamide; and b) a monoacetyl diacylglycerol compound such as 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG).

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
• 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 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/513 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents
• A61K 39/00 - Medicinal preparations containing antigens or antibodies

Abstract

Disclosed is a method for producing 1-palmitoyl-2-linoleoyl-3-acetyl glycerol of Chemical formula 3, of high purity with high yield, by carrying out acetylation of 1- palmitoyl glycerol with acetic anhydride or a mixture of acetic anhydride and acetyl chloride. The method for producing 1-palmitoyl-2-linoleoyl-3-acetyl glycerol comprises the steps of: preparing 1-palmitoyl-3-acetyl glycerol intermediate of Chemical formula 2 by reacting 1-palmitoyl glycerol of Chemical formula 1 and an acetylating agent selected form the group consisting of (i) acetic anhydride and (ii) a mixture of acetic anhydride and acetyl chloride; and reacting the 1-palmitoyl-3-acetyl glycerol intermediate and linoleic acid. (see formula 1) (see formula 2) (see formula 3)

IPC Classes  ?

• C07C 67/12 - Preparation of carboxylic acid esters from asymmetrical anhydrides
• C07C 67/08 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds

Abstract

Disclosed are a novel diacylglycerol lactone compound for improving immunity and inhibiting infection by promoting neutrophil movement, a preparation method therefor, and an immunostimulator containing same as an active ingredient. The diacyloglycerol lactone compound is represented by chemical formula 1 of the specification. In chemical formula 1, R1 and R2 are respectively N and independently a C2-30 fatty acid group.

IPC Classes  ?

• C07D 307/32 - Oxygen atoms
• A23L 33/00 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof
• A23L 29/00 - Foods or foodstuffs containing additivesPreparation or treatment thereof
• A61P 31/04 - Antibacterial agents

Abstract

Disclosed are a novel 1,2-diacylglycerol compound that useful for improving, preventing or treating inflammation-related diseases by inhibiting overexpression of various inflammatory cytokines such as IL-4 and IL-6 or chemokine CXCL8 related to the migration of inflammatory cells, a method for preparing the same, and an immunomodulator containing the same as an active ingredient. The 1,2-diacylglycerol compound is represented by Chemical Formula 2 in the patent specification.

IPC Classes  ?

• C07C 41/09 - Preparation of ethers by dehydration of compounds containing hydroxy groups
• A23L 33/115 - Fatty acids or derivatives thereofFats or oils
• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 37/00 - Drugs for immunological or allergic disorders
• A61P 37/02 - Immunomodulators
• C07C 69/30 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds
• C07C 69/587 - Monocarboxylic acid esters having at least two carbon-to-carbon double bonds

Abstract

In one aspect, use of 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG) for treating or preventing acute radiation syndrome is provided.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 38/19 - CytokinesLymphokinesInterferons
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 39/00 - General protective or antinoxious agents
• A61P 43/00 - Drugs for specific purposes, not provided for in groups

Abstract

Disclosed is a method for producing calcobutrol used as an MRI contrast agent. The method comprises the steps of: obtaining butrol represented by chemical formula 2 in the specification by reacting a gadobutrol represented by chemical formula 1 in the specification and a decomplexing agent; and obtaining a calcobutrol represented by chemical Formula 3 in the specification by reacting butrol with calcium ions.

IPC Classes  ?

• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• A61K 49/10 - Organic compounds

Abstract

The disclosure provides methods for treating, controlling or mitigating leukopenia (e.g. neutropenia) and/or thrombocytopenia, for example in the context of cancer chemotherapy, comprising administration of a monoacetyl-diacyl-glycerol compound, as well as compositions useful therefor.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 33/243 - PlatinumCompounds thereof
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 38/19 - CytokinesLymphokinesInterferons

Abstract

Disclosed is a composition for treating fatty liver disease. The composition comprises a monoacetyldiacylglycerol compound of Formula 1 as an active ingredient for treating fatty liver disease wherein R1 and R2 are independently a fatty acid residue of 14 to 22 carbon atoms.

IPC Classes  ?

• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• 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
• A23L 33/115 - Fatty acids or derivatives thereofFats or oils

Abstract

In one aspect, methods and compositions are provided for treating a neoplasia such as a solid tumor, the methods and composition comprising a) a granulocyte colony-stimulating factor (G-CSF) compound; and b) a monoacetyl diacylglycerol compound such as 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG).

IPC Classes  ?

• A61K 38/19 - CytokinesLymphokinesInterferons
• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

In one aspect, methods and compositions are provided for treating a neoplasia such as a solid tumor, the methods and composition comprising a) a granulocyte colony-stimulating factor (G-CSF) compound; and b) a monoacetyl diacylglycerol compound such as 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG).

IPC Classes  ?

• A61K 38/19 - CytokinesLymphokinesInterferons
• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents

Abstract

In one aspect, methods for modulating an inflammatory response are provided comprising administration to a cell or organism a monoacetyl diacylglycerol compound.

IPC Classes  ?

• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61P 11/00 - Drugs for disorders of the respiratory system
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

The disclosure provides methods for treating, controlling or mitigating leukopenia (e.g. neutropenia) and/or thrombocytopenia, for example in the context of cancer chemotherapy, comprising administration of a monoacetyl-diacyl-glycerol compound, as well as compositions useful therefor.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 33/243 - PlatinumCompounds thereof
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 38/19 - CytokinesLymphokinesInterferons

Abstract

Disclosed are: an intermediate capable of high-purity synthesis of gadobutrol which can be used as an MRI contrast agent; and a gadobutrol production method using same. The gadobutrol intermediate is represented by Chemical Formula 2 in the specification.

IPC Classes  ?

• A61K 49/10 - Organic compounds
• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• C07F 5/00 - Compounds containing elements of Groups 3 or 13 of the Periodic Table

Abstract

Disclosed are a glycerol derivative that is useful for alleviation, prevention, or treatment of inflammation-related diseases by downregulating the overexpression of various inflammatory cytokines such as IL-4, IL-6, etc. or CXCL8 and reducing the migration of the HL-60 cell line, a preparation method therefor, and an immunomodulator comprising same as an effective ingredient. The glycerol derivative represented by chemical formula 2 or 2 in the specification is included.

IPC Classes  ?

• C07C 235/28 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being acyclic and unsaturated
• A61K 31/133 - Amines, e.g. amantadine having hydroxy groups, e.g. sphingosine
• A61P 31/12 - Antivirals
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
• A61P 35/00 - Antineoplastic agents

Abstract

Disclosed are a novel 1,2-diacylglycerol compound, a preparation method therefor, and an immunomodulator containing same as an active ingredient, the 1,2-diacylglycerol compound being useful in the amelioration, prevention, or treatment of inflammation-related diseases by suppressing the overexpression of chemokine CXCL8, which is related to the migration of inflammatory cells, or various inflammatory cytokines, such as IL-4 and IL-6. The 1,2-diacylglycerol compound is represented by chemical formula 2 in the specification.

IPC Classes  ?

• C07C 69/30 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds
• C07C 67/08 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds
• C07C 67/30 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group
• A23L 33/115 - Fatty acids or derivatives thereofFats or oils
• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

Disclosed are a novel diacylglycerol lactone compound for improving immunity and inhibiting infection by promoting neutrophil movement, a preparation method therefor, and an immunostimulator containing same as an active ingredient. The diacylglycerol lactone compound is represented by chemical formula 1 of the specification. In chemical formula 1, R1 and R2 are respectively and independently a C2-30 fatty acid group.

IPC Classes  ?

• C07D 307/32 - Oxygen atoms
• A61K 31/365 - Lactones
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives
• A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
• A61P 37/00 - Drugs for immunological or allergic disorders

Abstract

Disclosed is a composition for preventing or treating psoriasis containing a monoacetyl diacylglycerol compound which not only can effectively prevent and treat psoriasis, but also is safe without any side effects when used. The composition contains a monoacetyl diacylglycerol compound represented by Chemical Formula 1 in the specification as an active ingredient.

IPC Classes  ?

• A61K 31/201 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having one or two double bonds, e.g. oleic or linoleic acid
• A61P 17/06 - Antipsoriatics

Abstract

Disclosed is a method for producing calcobutrol used as an MRI contrast agent. The method for producing calcobutrol comprises the steps of: obtaining butrol represented by chemical formula 2 in the specification by reacting gadobutrol represented by chemical formula 1 in the specification with a decomplexing agent; and obtaining calcobutrol represented by chemical formula 3 in the specification by reacting the butrol with calcium ions.

IPC Classes  ?

• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• A61K 49/06 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations
• A61K 49/10 - Organic compounds

Abstract

Disclosed are an intermediate for gadoteridol used as an MRI contrast agent, and a method for preparing gadoteridol using same. Provided, as a gadoteridol intermediate, is 10-(2-hydroxypropyl)-1,4,7,10-tetraazacyclododecane, which is represented by chemical formula 1 in the description, or a hydrochloride thereof, which is represented by chemical formula 3 in the description.

IPC Classes  ?

• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• A61K 49/06 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations
• A61K 49/10 - Organic compounds

Abstract

In one aspect, use of 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG) for treating or preventing acute radiation syndrome is provided.

IPC Classes  ?

• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 38/19 - CytokinesLymphokinesInterferons

Abstract

In one aspect, use of 1-palmitoyl-2-linoleoyl-3-acetylglycerol (PLAG) for treating or preventing acute radiation syndrome is provided.

IPC Classes  ?

• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61K 31/232 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having three or more double bonds, e.g. etretinate
• A61K 38/19 - CytokinesLymphokinesInterferons
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives

Abstract

Disclosed are: an intermediate capable of high-purity synthesis of gadobutrol which can be used as an MRI contrast agent; and a gadobutrol production method using same. The gadobutrol intermediate is represented by Chemical Formula 2 in the specification.

IPC Classes  ?

• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• A61K 49/10 - Organic compounds

Abstract

Disclosed are: an intermediate capable of high-purity synthesis of gadobutrol which can be used as an MRI contrast agent; and a gadobutrol production method using same. The gadobutrol intermediate is represented by Chemical Formula 2: (see formula 2)

IPC Classes  ?

• C07D 257/02 - Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
• A61K 49/10 - Organic compounds

Abstract

The present invention relates to a pharmaceutical composition containing a monoacetyldiacyiglycerol compound as an active ingredient for preventing or treating asthma, and a functional health food composition for preventing or treating asthma. The monoacetyldiacylglycerol compound of the present invention inhibits the expression of IL-4 in EL-4 cells, which are mouse T cell lymphoma cells, reduces hypersensitivity of airway in an asthma-induced animal model, and inhibits the infiltration of inflammatory cells into the bronchial tube. In addition, the compounds of the present invention inhibit the generation of IgE in the serum and bronchoalveolar lavage fluid, have an excellent effect of inhibiting the expression of Th2 cytokines (IL-4, IL-5, and IL-13) in the lung, thereby overcome side effects of the currently used therapeutic agents for asthma, have no toxicity, and exhibit a superior therapeutic effect, and thus can be useful as a composition for preventing, treating, and alleviating asthma.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 35/32 - BonesOsteocytesOsteoblastsTendonsTenocytesTeethOdontoblastsCartilageChondrocytesSynovial membrane
• A23L 33/00 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof
• A23K 20/00 - Accessory food factors for animal feeding-stuffs

Abstract

The present invention provides methods for treating, controlling or mitigating hemolytic uremic syndrome (HUS), comprising administering a monoacetyldiacylglycerol compound to a patient in need thereof, as well as compositions useful therefor.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61P 7/06 - Antianaemics
• A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
• A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/739 - Lipopolysaccharides
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 31/7068 - 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 containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61K 31/15 - Oximes (C=N—O—)Hydrazines (N—N)Hydrazones (N—N=)

Abstract

The present invention relates to a pharmaceutical composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing or treating chronic obstructive pulmonary diseases, and a functional health food composition for treating or preventing chronic obstructive pulmonary diseases. The monoacetyldiacylglycerol compound of the present invention inhibits the IL-4 expression in EL-4 cells and inhibits the infiltration of inflammatory cells into the bronchial tube in an animal model. In addition, the compounds of the present invention have an excellent effect of inhibiting the expression of CXCL-1, TNF-α, or MIP-2, thereby overcoming side effects of the currently used therapeutic agents for chronic obstructive pulmonary diseases, having no toxicity, and exhibiting a superior therapeutic effect, and thus can be useful as a composition for preventing, treating, and alleviating chronic obstructive pulmonary diseases.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds

Abstract

Disclosed is a composition for preventing or treating psoriasis containing a monoacetyl diacylglycerol compound which not only can effectively prevent and treat psoriasis, but also is safe without any side effects when used. The composition contains a monoacetyl diacylglycerol compound represented by chemical formula 1 in the specification as an active ingredient.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives

Abstract

Disclosed is a composition for preventing or treating hepatitis containing a monoacetyl diacylglycerol compound which not only can effectively prevent and treat hepatitis, but also is safe without any side effects when used. The composition contains a monoacetyl diacylglycerol compound represented by chemical formula 1 in the specification as an active ingredient. In chemical formula 1 in the specification, R1 and R2 are independently a fatty acid group having a carbon number of 14 to 22.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives

Abstract

The invention provides a pharmaceutical composition for preventing or treating mucositis, for example oral mucositis (e.g., oral ulceration) and gastrointestinal mucositis, comprising a monoacetyldiacylglycerol compound, especially PLAG, and a method of preventing or treating mucositis using the same.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/375 - Ascorbic acid, i.e. vitamin CSalts thereof
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

본 발명은 모노아세틸디아실글리세롤 화합물, 특히 PLAG를 포함하는, 점막염, 예를 들어, 구강 점막염(예컨대, 구강 궤양) 및 위장 점막염의 예방 또는 치료를 위한 약학 조성물 및 이를 이용한 점막염의 예방 또는 치료 방법을 제공한다.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/375 - Ascorbic acid, i.e. vitamin CSalts thereof
• A61K 31/355 - Tocopherols, e.g. vitamin E
• 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

Abstract

The present invention provides a method for treating, controlling or alleviating paroxysmal nocturnal hemoglobinuria (PNH) comprising administering a monoacetyldiacylglycerol compound to a patient in need thereof, and a composition useful therefor.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/355 - Tocopherols, e.g. vitamin E
• 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

Abstract

The present invention provides a method for treating, suppressing or alleviating a hemolytic uremic syndrome (HUS), comprising administering a monoacetyl diacylglycerol compound to a patient in need thereof, and a composition useful therefor.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/355 - Tocopherols, e.g. vitamin E
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate

Abstract

The invention provides a pharmaceutical composition for preventing or treating mucositis, for example oral mucositis (e.g., oral ulceration) and gastrointestinal mucositis, comprising a monoacetyldiacylglycerol compound, especially PLAG, and a method of preventing or treating mucositis using the same.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 9/00 - Medicinal preparations characterised by special physical form
• 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
• A61N 5/06 - Radiation therapy using light
• A61N 5/067 - Radiation therapy using light using laser light

Abstract

The present invention relates to a method for preparing a contrast agent for magnetic resonance imaging (MRI) and, more particularly, to a method for preparing a contrast agent for magnetic resonance imaging, which has improved stability by minimizing side effects by removing unreacted substances generated during a preparation process. The preparation method comprises the steps of: reacting a lanthanide with a macrocyclic chelate to form a complex-containing aqueous solution; exchanging ions using one or more resins among a cation exchange resin, a chelate resin and an anion exchange resin in order to remove free lanthanide and unreacted macrocyclic chelate from the complex-containing aqueous solution; controlling the pH of the complex aqueous solution in a neutral range; and removing germs from the complex aqueous solution.

IPC Classes  ?

• A61K 49/06 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations
• A61K 49/10 - Organic compounds

Abstract

The present invention relates to a composition containing a monoacetyldiglyceride compound as an active ingredient, for inhibiting blood cancer or metastasis, and a use thereof. The monoacetyldiglyceride compound according to the present invention has excellent effects of inhibiting the expression of IL-4 and inhibiting the activity of STAT-6, and thereby is capable of overcoming side effects of currently used blood cancer or metastasis inhibiting agents. Also, the monoacetyldiglyceride compound is a non-toxic compound having superior therapeutic effects and thus can be useful as a composition for preventing, treating, or improving blood cancer and metastasis.

IPC Classes  ?

• A61K 31/225 - Polycarboxylic acids
• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61K 35/32 - BonesOsteocytesOsteoblastsTendonsTenocytesTeethOdontoblastsCartilageChondrocytesSynovial membrane
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives
• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin

Abstract

The present invention relates to a pharmaceutical composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing or treating asthma, and a functional health food composition for preventing or treating asthma. The monoacetyldiacylglycerol compound of the present invention inhibits the expression of IL-4 in EL-4 cells, which are mouse T cell lymphoma cells, reduces hypersensitivity of airway in an asthma-induced animal model, and inhibits the infiltration of inflammatory cells into the bronchial tube. In addition, the compounds of the present invention inhibit the generation of IgE in the serum and bronchoalveolar lavage fluid, have an excellent effect of inhibiting the expression of Th2 cytokines (IL-4, IL-5, and IL-13) in the lung, thereby overcome side effects of the currently used therapeutic agents for asthma, have no toxicity, and exhibit a superior therapeutic effect, and thus can be useful as a composition for preventing, treating, and alleviating asthma.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 35/32 - BonesOsteocytesOsteoblastsTendonsTenocytesTeethOdontoblastsCartilageChondrocytesSynovial membrane
• A23L 33/00 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof
• A23K 20/00 - Accessory food factors for animal feeding-stuffs

Abstract

The present invention relates to a pharmaceutical composition, functional health food composition, quasi-drug composition, and cosmetic composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing, treating or improving atopic dermatitis. The monoacetyldiacylglycerol compound of the present invention has an excellent effect of suppression of IL-4 and IgE secretion, thereby overcoming side effects of an atopic dermatitis treatment agent currently in use, having no toxicity, and exhibiting an excellent treatment effect, and thus can be useful as a composition for preventing, treating, and ameliorating atopic dermatitis.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/08 - Solutions
• 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 8/37 - Esters of carboxylic acids
• A61Q 19/00 - Preparations for care of the skin
• A23L 33/10 - Modifying nutritive qualities of foodsDietetic productsPreparation or treatment thereof using additives

Abstract

The invention relates to pharmaceutical compositions, as well as health functional food compositions and quasi-drug compositions, for preventing, treating, or improving rheumatoid arthritis, comprising a monoacetyldiacylglycerol compound as an active ingredient. The monoacetyldiacylglycerol of the invention is effective in inhibiting the phosphorylation of STAT-3 known to be a therapeutic target for rheumatoid arthritis. As the monoacetyldiacylglycerol is an effective therapeutic agent without toxicity, the monoacetyldiacylglycerol can overcome the side effects of the medicines currently used in the treatment of rheumatoid arthritis. Thus, the monoacetyldiacylglycerol can be used for preventing, treating or improving rheumatoid arthritis.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms

Abstract

The disclosure provides methods for treating, controlling or mitigating leukopenia (e.g. neutropenia) and/or thrombocytopenia, for example in the context of cancer chemotherapy, comprising administration of a monoacetyl-diacyl-glycerol compound, as well as compositions useful therefor.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 33/24 - Heavy metalsCompounds thereof
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 38/19 - CytokinesLymphokinesInterferons

Abstract

The disclosure provides methods for treating, controlling or mitigating leukopenia (e.g. neutropenia) and/or thrombocytopenia, for example in the context of cancer chemotherapy, comprising administration of a monoacetyl-diacyl-glycerol compound, as well as compositions useful therefor.

IPC Classes  ?

• A61K 31/231 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms having one or two double bonds
• A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
• A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
• A61K 31/185 - AcidsAnhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• 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 31/355 - Tocopherols, e.g. vitamin E
• A61K 31/138 - Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
• A61K 33/24 - Heavy metalsCompounds thereof
• A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 38/19 - CytokinesLymphokinesInterferons

Abstract

Disclosed are a method for preparing 1-palmitoyl-3-acetylglycerol in high purity and high yield without a purification process using a column chromatography, and a method for preparing 1-palmitoyl-2-linoleoyl-3-acetylglycerol in high purity and high yield using the same as a key intermediate. The method for preparing 1-palmitoyl-3-acetyl glycerol comprises the steps of: forming a reaction mixture including 1-palmitoyl-3-acetyl glycerol of the Formula 1 in the specification by reacting 1-palmitoylglycerol of the Formula 2 in the specification and an acetylating agent; and separating the optically active 1-palmitoyl-3-acetylglycerol by crystallizing the reaction mixture in a saturated hydrocarbon solvent having 5 to 7 carbon atoms.

IPC Classes  ?

• C07C 59/245 - Saturated compounds having more than one carboxyl group containing hydroxy or O-metal groups
• C07C 59/90 - Unsaturated compounds containing keto groups containing singly bound oxygen-containing groups
• C07C 67/08 - Preparation of carboxylic acid esters by reacting carboxylic acids or symmetrical anhydrides with the hydroxy or O-metal group of organic compounds
• C07B 57/00 - Separation of optically-active organic compounds
• C07C 67/14 - Preparation of carboxylic acid esters from carboxylic acid halides
• C07C 69/30 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds

Abstract

The disclosure provides methods of treating restless legs syndrome and/or leg cramps comprising administering an effective amount of a monoacetyldiacylglycerol derivative, for example 1-palmitoyl-2-linoleoyl-3-acetylglycerol, together with compositions for use in such methods.

IPC Classes  ?

• A01N 37/02 - Saturated carboxylic acids or thio-analogues thereofDerivatives thereof

Abstract

The disclosure provides methods for treating, controlling or mitigating leukopenia (e.g. neutropenia) and/or thrombocytopenia, for example in the context of cancer chemotherapy, comprising administration of a monoacetyl-diacyl-glycerol compound, as well as compositions useful therefor.

IPC Classes  ?

• A61K 31/25 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol
• A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

Abstract

The disclosure provides methods for treating, controlling or mitigating leukopenia (e.g. neutropenia) and/or thrombocytopenia, for example in the context of cancer chemotherapy, comprising administration of a monoacetyl-diacyl-glycerol compound, as well as compositions useful therefor.

IPC Classes  ?

• A61K 31/21 - Esters, e.g. nitroglycerine, selenocyanates
• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/23 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin of acids having a carboxyl group bound to a chain of seven or more carbon atoms

Abstract

The present invention relates to: a composition for promoting the differentiation or proliferation of erythrocytic cells, containing a monoacetyl diacylglycerol compound as an active ingredient; and a pharmaceutical composition and a dietary supplement composition for preventing, treating or alleviating erythrocytopenia, containing the same. The monoacetyl diacylglycerol compound of the present invention has a remarkable effect of promoting the differentiation or proliferation of erythrocytic cells, and thus can be useful in a composition for preventing, treating or alleviating erythrocytopenia as a compound overcoming the side effects of an anemia therapeutic agent, which is currently in use, having no toxicity and remarkable treatment effects.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid

Abstract

The present invention relates to a pharmaceutical composition, functional health food composition, quasi-drug composition, and cosmetic composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing, treating or improving atopic dermatitis. The monoacetyldiacylglycerol compound of the present invention has an excellent effect of suppression of IL- 4 and IgE secretion, thereby overcoming side effects of an atopic dermatitis treatment agent currently in use, having no toxicity, and exhibiting an excellent treatment effect, and thus can be useful as a composition for preventing, treating, and ameliorating atopic dermatitis.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 17/00 - Drugs for dermatological disorders

Abstract

The present invention relates to a pharmaceutical composition, functional health food composition, quasi-drug composition, and cosmetic composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing or treating atopic dermatitis. The monoacetyldiacylglycerol compound of the present invention has an excellent effect of suppressing IL-4 and IgE secretion, thereby overcoming side effects of an atopic dermatitis treatment agent currently in use, having no toxicity, and exhibiting an excellent treatment effect, and thus can be useful as a composition for preventing, treating, and ameliorating atopic dermatitis.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 17/00 - Drugs for dermatological disorders

Abstract

The present invention relates to a pharmaceutical composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing or treating asthma, and a functional health food composition for preventing or treating asthma. The monoacetyldiacylglycerol compound of the present invention inhibits the expression of IL-4 in EL-4 cells, which are mouse T cell lymphoma cells, reduces hypersensitivity of airway in an asthma-induced animal model, and inhibits the infiltration of inflammatory cells into the bronchial tube. In addition, the compounds of the present invention inhibit the generation of IgE in the serum and bronchoalveolar lavage fluid, have an excellent effect of inhibiting the expression of Th2 cytokines (IL-4, IL-5, and IL-13) in the lung, thereby overcome side effects of the currently used therapeutic agents for asthma, have no toxicity, and exhibit a superior therapeutic effect, and thus can be useful as a composition for preventing, treating, and alleviating asthma.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 11/06 - Antiasthmatics

Abstract

The present invention relates to a pharmaceutical composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing or treating chronic obstructive pulmonary diseases, and a functional health food composition for treating or preventing chronic obstructive pulmonary diseases. The monoacetyldiacylglycerol compound of the present invention inhibits the IL-4 expression in EL-4 cells and inhibits the infiltration of inflammatory cells into the bronchial tube in an animal model. In addition, the compounds of the present invention have an excellent effect of inhibiting the expression of CXCL-1, TNF-.alpha., or MIP-2, thereby overcoming side effects of the currently used therapeutic agents for chronic obstructive pulmonary diseases, having no toxicity, and exhibiting a superior therapeutic effect, and thus can be useful as a composition for preventing, treating, and alleviating chronic obstructive pulmonary diseases.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

The present invention relates to a pharmaceutical composition for preventing, treating, or alleviating rheumatoid arthritis, a composition for a functional health food, and a medicinal compound. The monoacetyldiglyceride compound according to the present invention has excellent effects of inhibiting phosphorylation of STAT-3, which is known as a target material in treating rheumatoid arthritis, and thus can overcome side effects of currently used therapeutic agents for rheumatoid arthritis. Also, the monoacetyldiglyceride compound is a non-toxic compound having superior therapeutic effects and thus can be useful as a composition for preventing, treating, and alleviating rheumatoid arthritis.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
• A61P 19/00 - Drugs for skeletal disorders

Abstract

The present invention relates to a pharmaceutical composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing or treating chronic obstructive pulmonary diseases, and a functional health food composition for treating or preventing chronic obstructive pulmonary diseases. The monoacetyldiacylglycerol compound of the present invention inhibits the IL-4 expression in EL-4 cells and inhibits the infiltration of inflammatory cells into the bronchial tube in an animal model. In addition, the compounds of the present invention have an excellent effect of inhibiting the expression of CXCL-1, TNF-α, or MIP-2, thereby overcoming side effects of the currently used therapeutic agents for chronic obstructive pulmonary diseases, having no toxicity, and exhibiting a superior therapeutic effect, and thus can be useful as a composition for preventing, treating, and alleviating chronic obstructive pulmonary diseases.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
• A61P 11/00 - Drugs for disorders of the respiratory system

Abstract

The present invention relates to a composition containing a monoacetyldiglyceride compound as an active ingredient, for inhibiting blood cancer or metastasis, and a use thereof. The monoacetyldiglyceride compound according to the present invention has excellent effects of inhibiting the expression of IL-4 and inhibiting the activity of STAT-6, and thereby is capable of overcoming side effects of currently used blood cancer or metastasis inhibiting agents. Also, the monoacetyldiglyceride compound is a non-toxic compound having superior therapeutic effects and thus can be useful as a composition for preventing, treating, or alleviating blood cancer and metastasis.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 35/00 - Antineoplastic agents

Abstract

The invention relates to pharmaceutical compositions, as well as health functional food compositions and quasi-drug compositions, for preventing, treating, or improving rheumatoid arthritis, comprising a monoacetyldiacylglycerol compound as an active ingredient. The monoacetyldiacylglycerol of the invention is effective in inhibiting the phosphorylation of STAT-3 known to be a therapeutic target for rheumatoid arthritis. As the monoacetyldiacylglycerol is an effective therapeutic agent without toxicity, the monoacetyldiacylglycerol can overcome the side effects of the medicines currently used in the treatment of rheumatoid arthritis. Thus, the monoacetyldiacylglycerol can be used for preventing, treating or improving rheumatoid arthritis.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
• A61P 19/00 - Drugs for skeletal disorders
• A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis

Abstract

The present invention relates to a composition containing a monoacetyldiglyceride compound as an active ingredient, for inhibiting blood cancer or metastasis, and a use thereof. The monoacetyldiglyceride compound according to the present invention has excellent effects of inhibiting the expression of IL-4 and inhibiting the activity of STAT-6, and thereby is capable of overcoming side effects of currently used blood cancer or metastasis inhibiting agents. Also, the monoacetyldiglyceride compound is a non-toxic compound having superior therapeutic effects and thus can be useful as a composition for preventing, treating, or alleviating blood cancer and metastasis.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 35/00 - Antineoplastic agents

Abstract

The present invention relates to a pharmaceutical composition containing a monoacetyldiacylglycerol compound as an active ingredient for preventing or treating asthma, and a functional health food composition for preventing or treating asthma. The monoacetyldiacylglycerol compound of the present invention inhibits the expression of IL-4 in EL-4 cells, which are mouse T cell lymphoma cells, reduces hypersensitivity of airway in an asthma-induced animal model, and inhibits the infiltration of inflammatory cells into the bronchial tube. In addition, the compounds of the present invention inhibit the generation of IgE in the serum and bronchoalveolar lavage fluid, have an excellent effect of inhibiting the expression of Th2 cytokines (IL-4, IL-5, and IL-13) in the lung, thereby overcome side effects of the currently used therapeutic agents for asthma, have no toxicity, and exhibit a superior therapeutic effect, and thus can be useful as a composition for preventing, treating, and alleviating asthma.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
• A61P 11/06 - Antiasthmatics

Abstract

Disclosed are a method for preparing 1-palmitoyl-3-acetylglycerol in a high purity and a high yield without purification by column chromatography, and a method for preparing 1-palmitoyl-2-linoleoyl-3-acetylglycerol in a high purity and a high yield using the same as a core intermediate. The method for preparing 1-palmitoyl-3-acetylglycerol comprises the following steps: reacting 1-palmitoylglycerol represented by chemical formula 2 in the specification, a racemate or an optically active substance, with an acetylating agent to prepare a reaction mixture containing 1-palmitoyl-3-acetylglycerol represented by chemical formula 1 in the specification, a racemate or an optically active substance; and crystallizing the reaction mixture in a C5-C7 saturated hydrocarbon solvent to isolate the optically active 1-palmitoyl-3-acetylglycerol.

IPC Classes  ?

• C07C 67/14 - Preparation of carboxylic acid esters from carboxylic acid halides
• C07B 57/00 - Separation of optically-active organic compounds
• C07C 67/12 - Preparation of carboxylic acid esters from asymmetrical anhydrides
• C07C 67/52 - SeparationPurificationStabilisationUse of additives by change in the physical state, e.g. crystallisation
• C07C 69/30 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with trihydroxylic compounds
• C07C 69/587 - Monocarboxylic acid esters having at least two carbon-to-carbon double bonds

Abstract

Disclosed are a method for preparing 1-palmitoyl-3-acetylglycerol in a high purity and a high yield without purification by column chromatography, and a method for preparing 1-palmitoyl-2-linoleoyl-3-acetylglycerol in a high purity and a high yield using the same as a core intermediate. The method for preparing 1-palmitoyl-3-acetylglycerol comprises the following steps: reacting 1-palmitoylglycerol represented by chemical formula 2 in the specification, a racemate or an optically active substance, with an acetylating agent to prepare a reaction mixture containing 1-palmitoyl-3-acetylglycerol represented by chemical formula 1 in the specification, a racemate or an optically active substance; and crystallizing the reaction mixture in a C5-C7 saturated hydrocarbon solvent to isolate the optically active 1-palmitoyl-3-acetylglycerol.

IPC Classes  ?

• C07C 67/307 - Preparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by introduction of halogenPreparation of carboxylic acid esters by modifying the acid moiety of the ester, such modification not being an introduction of an ester group by substitution of halogen atoms by other halogen atoms
• C07C 67/52 - SeparationPurificationStabilisationUse of additives by change in the physical state, e.g. crystallisation
• C07C 69/34 - Esters of acyclic saturated polycarboxylic acids having an esterified carboxyl group bound to an acyclic carbon atom
• C07B 57/00 - Separation of optically-active organic compounds

Abstract

The present invention relates to a method for preparing ultra-high purity potassium salts (refer to Chemical Formula 2) of EXP-3174 known as a main metabolite of losartan, and to a method for preparing ultra-high purity EXP-3174·2H2O of Chemical Formula 1 by using the method. The method according to the present invention comprises the following steps: (a) performing a deprotective reaction to the compound of Chemical Formula 4 to prepare the compound of Chemical Formula 3; (b) selectively oxidizing, by using an oxidizing agent, aldehydes of the compound prepared in step (a), and preparing crude EXP-3174·2H2O having a structure of Chemical Formula 1, which has a dehydrate form; (c) heating and refluxing the compound having a structure of Chemical Formula 1, prepared in step (b), in a mixture solvent of water and ethyl acetate, and cooling and filtering the compound; (d) forming KOH and salts from the filtered product obtained in step (c) in a mixture solvent of isopropyl alcohol (IPA) and polar protic solvent to prepare the compound of Chemical Formula 2; and (e) neutralizing the compound of Chemical Formula 2, prepared in step (d), in a mixture solvent of water and ethyl acetate under an acid condition, and performing the process of step (c). According to the present invention, ultra-high purity potassium salts of EXP-3174 and EXP-3174·2H2O, are prepared, in which the content of single impurity does not exceed 0.1%.

IPC Classes  ?

• 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 403/06 - 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 only aliphatic carbon atoms

Abstract

The uses of mono acetyl diacyl glycerol derivatives extracted from deer antler for immunomodulating agent disclosed. Medical supplies and health foods containing the same as an effective ingredient also disclosed. Mono acetyl diacyl glycerol derivatives shows significantly effect for immuno modulation including immune enhancing. In the case of inducing cancer in a hamster by injecting cancer cell line, cancer development was delayed by activating lymphocytes, monocytes, and dendritic cells that are important factors to promote immunity and apoptosis of cancer cell was induced by promoting cytotoxicity of immune cell against cancer cell. Also in the case of mouse induced septic shock, it shows 100 % survival rate even after lapse of 120 hours by control of immune function and suppression effect apoptosis. Therefore, mono acetyl diacyl glycerol derivatives according to the present invention can be effectively used for an immunomodulating agent, a sepsis treatment, a cancer treatment, and a health food for an immune modulation or the prevention of cancer.

IPC Classes  ?

• A61K 31/22 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin