The present disclosure relates to an isolated anti-FcRN antibody, which is an antibody binding to FcRN (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmunre diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
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 39/00 - Medicinal preparations containing antigens or antibodies
G01N 33/564 - ImmunoassayBiospecific binding assayMaterials therefor for pre-existing immune complex or autoimmune disease
G01N 33/566 - ImmunoassayBiospecific binding assayMaterials therefor using specific carrier or receptor proteins as ligand binding reagent
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
In one aspect of the present invention, there is provided a pharmaceutical formulation having a pH of 4.0 to 8.0, comprising (a) an HL161BKN antibody or a fragment thereof, (b) at least one additive selected from mannitol, sorbitol, arginine, histidine, glycine and salts thereof, (c) a buffer system selected from citrate or histidine, and (d) a surfactant. HL161BKN present in the formulation has improved stability and is non-toxic, and thus has a high potential for industrial application.
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 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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 47/22 - 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
3.
TREATMENT OF DRY EYE SYNDROME USING AN OPHTHALMIC COMPOSITION COMPRISING TANFANERCEPT
The present invention relates to treatment of dry eye syndrome using a tanfanercept-containing ophthalmic composition. According to the present invention, as a result of clinical trial on dry eye syndrome, the tanfanercept-containing ophthalmic composition demonstrated excellent effects with regard to improvement of a central corneal staining score (CCSS) and a total corneal staining score (TCSS), which is clinically important. Further, such improvement of a central corneal staining score (CCSS) and a total corneal staining score (TCSS) was more significantly demonstrated in the patients with moderate-to-severe severity of dry eye. In addition, the patients with higher ocular discomfort score or higher eye dryness score, which are subjective symptoms, also showed greater improvement. Even though the same dose of tanfanercept was used, the tanfanercept-containing ophthalmic composition showed superior efficacy in the patient having more serious or severe baseline sign or symptom scores. This result was unexpected and is meaningful under the existing conditions without therapeutics for moderate or severe dry eye syndrome, since a novel and alternative therapeutic idea may be provided.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical agents affecting sensory organs; thyroid and
para-thyroid hormone preparations; tonics [medicines];
parasiticides; antiemetics; bronchodilating preparations;
pharmaceutical preparations for treating diabetes;
pharmaceutical agents affecting metabolism; veterinary
preparations; prescription synthetic narcotics;
anaesthetics; pharmaceutical agents affecting peripheral
nervous system; pharmaceutical preparations for immunity
adjustment; pharmaceutical agents for treating physically
caused lesions; pharmaceuticals for the treatment of
erectile dysfunction; pharmaceutical preparations for
urogenital organs; vitamin preparations; pharmaceutical
products for the treatment of bone diseases; preparations of
trace elements for human and animal use; anti-inflammatory
and antipyretic preparations; pharmaceutical agents
affecting digestive organs; cardiovascular pharmaceutical
preparations; nervines; pharmaceutical preparations;
chemico-pharmaceutical preparations; medicines for the
treatment of gastrointestinal diseases; drugs for medical
purposes; medical diagnostic reagents; diuretics; medicines
for human purposes; antacids; haematogen; pharmaceutical
preparations for treating malignant tumours; pharmaceutical
preparations acting on the central nervous system;
pharmaceutical preparations for diagnosis; sedatives;
analgesics; medical preparations for slimming purposes;
embedding material for dental and dental technical purposes;
medicines for dental purposes; dermatological pharmaceutical
products; antibiotic preparations; antibiotics; anti-cancer
preparations; blood solvents for medical or veterinary
purposes; pharmaceutical preparations for respiratory
organs; preparations for the treatment of burns;
chemotherapeutics; medications to treat chemical disorders. Price comparison services; advertising; distribution of
samples; wholesale store services featuring nutraceuticals
for use as a dietary supplement; wholesale store services
featuring medical apparatus; wholesale store services
featuring medical apparatus and instruments; sales agency
services for pharmaceuticals; wholesale store services
featuring pharmaceuticals; wholesale store services
featuring medicines for human purposes; wholesale store
services featuring nutraceuticals via the internet;
wholesale store services featuring make-up preparations. Advice in the field of construction drafting; engineering
surveying; rental of scientific equipment; research relating
to mechanical engineering; meteorological observation;
services for assessing the safety of agricultural chemicals;
cosmetology research; styling [industrial design]; drug
development; pharmaceutical product evaluation;
pharmaceutical research services; scientific research in the
fields of medicine/health and pharmacology; medical
research; product safety testing; textile design; research
relating to computers; marine, aerial and land surveying;
oceanography research; chemical analysis; environmental
monitoring services.
5.
A STABLE OPHTHALMIC COMPOSITION COMPRISING TANFANERCEPT, WHICH IS FREE OF STABILIZER OR SUBSTANTIALLY FREE OF STABILIZER
The present invention relates to a stable ophthalmic composition comprising tanfanercept, which does not use a stabilizer, and methods of preparing and using the composition. According to the present invention, it was found that the use of a stabilizer such as histidine or sucrose causes the generation of impurities such as tanfanercept-derived acidic/basic variants, and affects biological activity. The ophthalmic pharmaceutical composition according to the present invention may control pH rather than excluding the use of such a stabilizer to significantly reduce the generation of impurities under not only a refrigerated storage condition but also accelerated conditions and a stress condition, thereby preparing a stable tanfanercept ophthalmic composition.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
Reagents for use in diagnostic testing of HBS antibody for
medical purposes pharmaceutical agents affecting sensory
organs; thyroid and para-thyroid hormone preparations;
tonics [medicines]; anthelmintics; antiemetics; local
anaesthetics; anti-cough drops; pituitary hormone
preparations; pharmaceutical preparations for treating
diabetes; pharmaceutical agents affecting metabolism;
veterinary preparations; prescription synthetic narcotics;
anaesthetics; pharmaceutical agents affecting peripheral
nervous system; pharmaceutical preparations for immunity
adjustment; pharmaceutical agents for treating physically
caused lesions; pharmaceuticals for the treatment of
erectile dysfunction; vesicants; vaccines; adrenal hormone
preparations; pharmaceutical preparations for urogenital
organs; vitamin preparations; pharmaceutical products for
the treatment of bone diseases; crude medicines;
anti-inflammatory and antipyretic preparations;
pharmaceutical agents affecting digestive organs; biological
preparations for veterinary purposes; chemical preparations
for veterinary purposes; cardiovascular pharmaceutical
preparations; chemico-pharmaceutical preparations;
pharmaceutical agents for epidermis; medicines for the
treatment of gastrointestinal diseases; diagnostic
preparations for medical or veterinary purposes; drugs for
medical purposes; medical diagnostic reagents; diuretics;
medicines for human purposes; antacids; haematogen;
pharmaceutical preparations for the treatment of tumours;
pharmaceutical preparations acting on the central nervous
system; analgesics; medical preparations for slimming
purposes; medicines for dental purposes; dermatological
pharmaceutical products; antibiotics; anti-cancer
preparations; blood solvents for medical or veterinary
purposes; pharmaceutical preparations for respiratory
organs; preparations for the treatment of burns;
chemotherapeutics. Price comparison services; distribution of samples;
wholesale store services featuring nutraceuticals for use as
a dietary supplement; retail store services featuring
nutraceuticals for use as a dietary supplement; wholesale
store services featuring medical apparatus; retail store
services featuring medical apparatus; wholesale store
services featuring medical apparatus and instruments; retail
store services featuring medical apparatus and instruments;
wholesale store services featuring pharmaceuticals; retail
store services featuring pharmaceuticals; wholesale store
services featuring medicines for human purposes; retail
store services featuring medicines for human purposes;
wholesale store services featuring fruit-based dietary
supplements via the internet; retail store services
featuring fruit-based dietary supplements via the internet;
wholesale store services featuring make-up preparations via
the internet; retail store services featuring make-up
preparations via the internet; wholesale store services
featuring nutraceuticals via the internet; retail store
services featuring nutraceuticals via the internet;
wholesale store services featuring make-up preparations;
retail store services featuring make-up preparations. Advice in the field of construction drafting; engineering
surveying; rental of scientific equipment; research relating
to mechanical engineering; meteorological observation;
services for assessing the safety of agricultural chemicals;
cosmetology research; styling [industrial design]; drug
development; pharmaceutical product evaluation;
pharmaceutical research; scientific research in the fields
of medicine/health and pharmacology; medical research;
product safety testing; textile design; research relating to
computers; marine, aerial and land surveying; oceanography
research; chemical analysis; environmental impact surveys.
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Pharmaceutical agents affecting sensory organs; thyroid and para-thyroid hormone preparations; tonics [medicines]; parasiticides; antiemetics; bronchodilating preparations; pharmaceutical preparations for treating diabetes; pharmaceutical agents affecting metabolism; veterinary preparations; prescription synthetic narcotics; anaesthetics; pharmaceutical agents affecting peripheral nervous system; pharmaceutical preparations for immunity adjustment; pharmaceutical agents for treating physically caused lesions; pharmaceuticals for the treatment of erectile dysfunction; pharmaceutical preparations for urogenital organs; vitamin preparations; pharmaceutical products for the treatment of bone diseases; preparations of trace elements for human and animal use; anti-inflammatory and antipyretic preparations; pharmaceutical agents affecting digestive organs; cardiovascular pharmaceutical preparations; nervines; pharmaceutical preparations; chemico-pharmaceutical preparations; medicines for the treatment of gastrointestinal diseases; drugs for medical purposes; medical diagnostic reagents; diuretics; medicines for human purposes; antacids; haematogen; pharmaceutical preparations for treating malignant tumours; pharmaceutical preparations acting on the central nervous system; pharmaceutical preparations for diagnosis; sedatives; analgesics; medical preparations for slimming purposes; embedding material for dental and dental technical purposes; medicines for dental purposes; dermatological pharmaceutical products; antibiotic preparations; antibiotics; anti-cancer preparations; blood solvents for medical or veterinary purposes; pharmaceutical preparations for respiratory organs; preparations for the treatment of burns; chemotherapeutics; medications to treat chemical disorders. (1) Price comparison services; advertising; distribution of samples; wholesale store services featuring nutraceuticals for use as a dietary supplement; wholesale store services featuring medical apparatus; wholesale store services featuring medical apparatus and instruments; sales agency services for pharmaceuticals; wholesale store services featuring pharmaceuticals; wholesale store services featuring medicines for human purposes; wholesale store services featuring nutraceuticals via the internet; wholesale store services featuring make-up preparations.
(2) Advice in the field of construction drafting; engineering surveying; rental of scientific equipment; research relating to mechanical engineering; meteorological observation; services for assessing the safety of agricultural chemicals; cosmetology research; styling [industrial design]; drug development; pharmaceutical product evaluation; pharmaceutical research services; scientific research in the fields of medicine/health and pharmacology; medical research; product safety testing; textile design; research relating to computers; marine, aerial and land surveying; oceanography research; chemical analysis; environmental monitoring services.
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical agents affecting sensory organs; thyroid and para-thyroid hormone preparations; tonics, namely, medicines for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; parasiticides; antiemetics; bronchodilating preparations; pharmaceutical preparations for treating diabetes; pharmaceutical agents affecting metabolism; veterinary preparations for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; prescription synthetic narcotics; anaesthetics; pharmaceutical agents affecting peripheral nervous system; pharmaceutical preparations for immunity improvement; pharmaceutical agents for treating physically caused lesions; pharmaceuticals for the treatment of erectile dysfunction; pharmaceutical preparations for the treatment of urogenital organs; vitamin preparations; pharmaceutical products for the treatment of bone diseases; preparations of trace elements for human and animal use for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; anti-inflammatory and antipyretic preparations; pharmaceutical agents affecting digestive organs; cardiovascular pharmaceutical preparations; nervines in the nature of herbal supplements; pharmaceutical preparations for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; chemico-pharmaceutical preparations for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; medicines for the treatment of gastrointestinal diseases; drugs for medical purposes for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; medical diagnostic reagents; diuretics; medicines for human purposes for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; antacids; haematogen; pharmaceutical preparations for treating malignant tumours; pharmaceutical preparations acting on the central nervous system; pharmaceutical preparations for diagnosis of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; sedatives; analgesics; medical preparations for slimming purposes; dental impression material for dental and dental technical purposes; medicines for dental purposes; dermatological pharmaceutical products; antibiotic preparations; antibiotics; anti-cancer preparations; blood solvents for medical or veterinary purposes; pharmaceutical preparations for the treatment of respiratory organs; preparations for the treatment of burns; chemotherapeutics; medications to treat chemical disorders Price comparison services; advertising services; distribution of samples; wholesale store services featuring nutraceuticals for use as a dietary supplement; wholesale store services featuring medical apparatus; wholesale store services featuring medical apparatus and instruments; advertising agency services for pharmaceuticals; wholesale store services featuring pharmaceuticals; wholesale store services featuring medicines for human purposes; wholesale store services featuring nutraceuticals via the internet; wholesale store services featuring make-up preparations Advice in the field of construction drafting; engineering surveying; rental of scientific equipment; research relating to mechanical engineering; meteorological observation for others; services for assessing the safety of agricultural chemicals; cosmetology research; industrial design; pharmaceutical drug development services; pharmaceutical product evaluation; pharmaceutical research services; scientific research in the fields of medicine, health and pharmacology; medical research; product safety testing; textile design; research in the field of computer software development; marine, aerial and land surveying; oceanography research; chemical analysis; scientific research in the nature of providing environmental monitoring services
9.
ANTI-FCRN ANTIBODY OR ANTIGEN BINDING FRAGMENT THEREOF WITH IMPROVED STABILITY
The present disclosure relates to an anti-FcRn antibody or an antigen binding fragment thereof with improved stability and uses thereof. The anti-FcRn antibody or antigen binding fragment thereof binds to FcRn non-competitively with IgG and the like compared to the parent antibody, HL161AN, thereby having improved stability, such as reducing the production rate of aggregates while maintaining the biological activity of significantly reducing the amount of pathogenic autoantibodies in the blood. Therefore, it may be utilized more efficiently for the treatment of an autoimmune disease.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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 39/00 - Medicinal preparations containing antigens or antibodies
11.
ANTI-FCRN ANTIBODY OR ANTIGEN BINDING FRAGMENT THEREOF WITH IMPROVED STABILITY
The present disclosure relates to an anti-FcRn antibody or an antigen binding fragment thereof with improved stability and uses thereof. The anti-FcRn antibody or antigen binding fragment thereof binds to FcRn non-competitively with IgG and the like compared to the parent antibody, HL161AN, thereby having improved stability, such as reducing the production rate of aggregates while maintaining the biological activity of significantly reducing the amount of pathogenic autoantibodies in the blood. Therefore, it may be utilized more efficiently for the treatment of an autoimmune disease.
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
Reagents for use in diagnostic testing of Hepatitis B surface antibody for medical purposes and pharmaceutical agents affecting sensory organs; thyroid and para-thyroid hormone preparations; tonics, namely, medicines for autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; anthelmintics; antiemetics; local anaesthetics; anti-cough drops; pituitary hormone preparations; pharmaceutical preparations for treating diabetes; pharmaceutical agents affecting metabolism; veterinary preparations for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; prescription synthetic narcotics; anaesthetics; pharmaceutical agents affecting peripheral nervous system; pharmaceutical preparations for immunity improvement; pharmaceutical agents for treating physically caused lesions; pharmaceuticals for the treatment of erectile dysfunction; vesicants for wart removal; vaccines; adrenal hormone preparations; pharmaceutical preparations for the treatment of urogenital organs; vitamin preparations; pharmaceutical products for the treatment of bone diseases; crude medicines for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; anti-inflammatory and antipyretic preparations; pharmaceutical agents affecting digestive organs; biological preparations for veterinary purposes for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; chemical preparations for veterinary purposes for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; cardiovascular pharmaceutical preparations; chemico-pharmaceutical preparations for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; pharmaceutical agents for epidermis; medicines for the treatment of gastrointestinal diseases; diagnostic preparations for medical or veterinary purposes; drugs for medical purposes for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; medical diagnostic reagents; diuretics; medicines for human purposes for the treatment of autoimmune disease, ocular disease, ear disease, neurodegenerative disease, and cancer; antacids; haematogen; pharmaceutical preparations for the treatment of tumours; pharmaceutical preparations acting on the central nervous system; analgesics; medical preparations for slimming purposes; medicines for dental purposes; dermatological pharmaceutical products; antibiotics; anti-cancer preparations; blood solvents for medical or veterinary purposes; pharmaceutical preparations for the treatment of respiratory organs; preparations for the treatment of burns; chemotherapeutics Price comparison services; distribution of samples; wholesale store services featuring nutraceuticals for use as a dietary supplement; retail store services featuring nutraceuticals for use as a dietary supplement; wholesale store services featuring medical apparatus; retail store services featuring medical apparatus; wholesale store services featuring medical apparatus and instruments; retail store services featuring medical apparatus and instruments; wholesale store services featuring pharmaceuticals; retail store services featuring pharmaceuticals; wholesale store services featuring medicines for human purposes; retail store services featuring medicines for human purposes; wholesale store services featuring fruit-based dietary supplements via the internet; retail store services featuring fruit-based dietary supplements via the internet; wholesale store services featuring make-up preparations via the internet; retail store services featuring make-up preparations via the internet; wholesale store services featuring nutraceuticals via the internet; retail store services featuring nutraceuticals via the internet; wholesale store services featuring make-up preparations; retail store services featuring make-up preparations Advice in the field of construction drafting; engineering surveying; rental of scientific equipment; research relating to mechanical engineering; meteorological observation for others; services for assessing the safety of agricultural chemicals; cosmetology research services; industrial design; pharmaceutical drug development services; pharmaceutical product evaluation; pharmaceutical research services; scientific research services in the fields of medicine, health and pharmacology; medical research; product safety testing; textile design; research in the field of computer software development; marine, aerial and land surveying; oceanography research; chemical analysis; scientific research in the nature of providing environmental impact surveys
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
(1) Reagents for use in diagnostic testing of HBS antibody for medical purposes pharmaceutical agents affecting sensory organs; thyroid and para-thyroid hormone preparations; tonics [medicines]; anthelmintics; antiemetics; local anaesthetics; anti-cough drops; pituitary hormone preparations; pharmaceutical preparations for treating diabetes; pharmaceutical agents affecting metabolism; veterinary preparations; prescription synthetic narcotics; anaesthetics; pharmaceutical agents affecting peripheral nervous system; pharmaceutical preparations for immunity adjustment; pharmaceutical agents for treating physically caused lesions; pharmaceuticals for the treatment of erectile dysfunction; vesicants; vaccines; adrenal hormone preparations; pharmaceutical preparations for urogenital organs; vitamin preparations; pharmaceutical products for the treatment of bone diseases; crude medicines; anti-inflammatory and antipyretic preparations; pharmaceutical agents affecting digestive organs; biological preparations for veterinary purposes; chemical preparations for veterinary purposes; cardiovascular pharmaceutical preparations; chemico-pharmaceutical preparations; pharmaceutical agents for epidermis; medicines for the treatment of gastrointestinal diseases; diagnostic preparations for medical or veterinary purposes; drugs for medical purposes; medical diagnostic reagents; diuretics; medicines for human purposes; antacids; haematogen; pharmaceutical preparations for the treatment of tumours; pharmaceutical preparations acting on the central nervous system; analgesics; medical preparations for slimming purposes; medicines for dental purposes; dermatological pharmaceutical products; antibiotics; anti-cancer preparations; blood solvents for medical or veterinary purposes; pharmaceutical preparations for respiratory organs; preparations for the treatment of burns; chemotherapeutics. (1) Price comparison services; distribution of samples; wholesale store services featuring nutraceuticals for use as a dietary supplement; retail store services featuring nutraceuticals for use as a dietary supplement; wholesale store services featuring medical apparatus; retail store services featuring medical apparatus; wholesale store services featuring medical apparatus and instruments; retail store services featuring medical apparatus and instruments; wholesale store services featuring pharmaceuticals; retail store services featuring pharmaceuticals; wholesale store services featuring medicines for human purposes; retail store services featuring medicines for human purposes; wholesale store services featuring fruit-based dietary supplements via the internet; retail store services featuring fruit-based dietary supplements via the internet; wholesale store services featuring make-up preparations via the internet; retail store services featuring make-up preparations via the internet; wholesale store services featuring nutraceuticals via the internet; retail store services featuring nutraceuticals via the internet; wholesale store services featuring make-up preparations; retail store services featuring make-up preparations.
(2) Advice in the field of construction drafting; engineering surveying; rental of scientific equipment; research relating to mechanical engineering; meteorological observation; services for assessing the safety of agricultural chemicals; cosmetology research; styling [industrial design]; drug development; pharmaceutical product evaluation; pharmaceutical research; scientific research in the fields of medicine/health and pharmacology; medical research; product safety testing; textile design; research relating to computers; marine, aerial and land surveying; oceanography research; chemical analysis; environmental impact surveys.
14.
ANTIBODY BINDING TO FCRN FOR TREATING AUTOIMMUNE DISEASES
The present disclosure relates to an isolated anti-FcRN antibody, which is an antibody binding to FcRN (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
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
G01N 33/566 - ImmunoassayBiospecific binding assayMaterials therefor using specific carrier or receptor proteins as ligand binding reagent
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/564 - ImmunoassayBiospecific binding assayMaterials therefor for pre-existing immune complex or autoimmune disease
15.
TREATMENT OF DRY EYE SYNDROME USING TANFANERCEPT OPHTHALMIC COMPOSITION
The present invention relates to treatment of dry eye syndrome using a Tanfanercept ophthalmic composition. According to the present invention, an ophthalmic composition containing Tanfanercept exhibited an excellent effect in improving the clinically important central corneal and total corneal staining score as a result of a clinical test for dry eye syndrome. In addition, the improvement of the central corneal and total corneal staining score was greater in patients having moderate to severe dry eyes, and the degree of improvement was also greater in patients having higher ocular discomfort indexes or dry eye indexes, which are subjective symptoms. It is an unexpected effect that the ophthalmic composition containing Tanfanercept exhibits superior efficacy in patients having more severe signs or symptoms despite the use of the same dose of Tanfanercept, and this is meaningful in terms of providing a new therapeutic alternative in consideration of the fact that there is no treatment for moderate to severe dry eye syndrome.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention relates to: an ophthalmic composition that includes tanfanercept and exhibits stability without the use of a stabilizer; and a method for preparing and using the composition. The present invention has revealed that the use of stabilizers such as histidine and sucrose causes the production of impurities such as acidic/basic variants derived from tanfanercept, and affects biological activity. Such stabilizers are not used in the ophthalmic pharmaceutical composition according to the present invention, and instead, the pH of the composition is adjusted to significantly reduce the production of impurities not only in refrigerated storage conditions but also in accelerated and severe conditions. Therefore, a stable tanfanercept ophthalmic composition can be prepared.
The present invention relates to: an ophthalmic composition that includes tanfanercept and exhibits stability without the use of a stabilizer; and a method for preparing and using the composition. The present invention has revealed that the use of stabilizers such as histidine and sucrose causes the production of impurities such as acidic/basic variants derived from tanfanercept, and affects biological activity. Such stabilizers are not used in the ophthalmic pharmaceutical composition according to the present invention, and instead, the pH of the composition is adjusted to significantly reduce the production of impurities not only in refrigerated storage conditions but also in accelerated and severe conditions. Therefore, a stable tanfanercept ophthalmic composition can be prepared.
One aspect of the present invention provides an aqueous pharmaceutical formulation with a pH of 4.0 to 8.0, comprising (a) an HL161 BKN antibody or a fragment thereof, (b) one or more additives selected from mannitol, sorbitol, arginine, histidine, glycine and salts thereof, (c) a buffer system selected from citrate or histidine, and (d) polysorbate. The HL161 BKN antibody present in the formulation has improved stability and is non-toxic, and thus has high industrial applicability.
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 47/12 - 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 9/00 - Medicinal preparations characterised by special physical form
A61P 37/00 - Drugs for immunological or allergic disorders
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
A61K 39/00 - Medicinal preparations containing antigens or antibodies
One aspect of the present invention provides an aqueous pharmaceutical formulation with a pH of 4.0 to 8.0, comprising (a) an HL161 BKN antibody or a fragment thereof, (b) one or more additives selected from mannitol, sorbitol, arginine, histidine, glycine and salts thereof, (c) a buffer system selected from citrate or histidine, and (d) polysorbate. The HL161 BKN antibody present in the formulation has improved stability and is non-toxic, and thus has high industrial applicability.
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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 47/22 - 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
A61P 37/00 - Drugs for immunological or allergic disorders
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
20.
Antibody binding to FCRN for treating autoimmune diseases
The present disclosure relates to an isolated anti-FcRn antibody, which is an antibody binding to FcRn (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12P 21/06 - Preparation of peptides or proteins produced by the hydrolysis of a peptide bond, e.g. hydrolysate products
C12P 21/04 - Cyclic or bridged peptides or polypeptides, e.g. bacitracin
C12N 5/02 - Propagation of single cells or cells in suspensionMaintenance thereofCulture media therefor
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 39/40 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum bacterial
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
G01N 33/566 - ImmunoassayBiospecific binding assayMaterials therefor using specific carrier or receptor proteins as ligand binding reagent
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/564 - ImmunoassayBiospecific binding assayMaterials therefor for pre-existing immune complex or autoimmune disease
C07K 1/00 - General processes for the preparation of peptides
A61K 39/00 - Medicinal preparations containing antigens or antibodies
21.
Antibody binding to FcRn for treating autoimmune diseases
The present disclosure relates to an isolated anti-FcRn antibody, which is an antibody binding to FcRn (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
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
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/566 - ImmunoassayBiospecific binding assayMaterials therefor using specific carrier or receptor proteins as ligand binding reagent
C07K 1/00 - General processes for the preparation of peptides
A61K 39/00 - Medicinal preparations containing antigens or antibodies
22.
Antibody binding to FcRn for treating autoimmune diseases
The present disclosure relates to an isolated anti-FcRn antibody, which is an antibody binding to FcRn (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12P 21/06 - Preparation of peptides or proteins produced by the hydrolysis of a peptide bond, e.g. hydrolysate products
C12P 21/04 - Cyclic or bridged peptides or polypeptides, e.g. bacitracin
C12N 5/02 - Propagation of single cells or cells in suspensionMaintenance thereofCulture media therefor
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 39/40 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum bacterial
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
G01N 33/566 - ImmunoassayBiospecific binding assayMaterials therefor using specific carrier or receptor proteins as ligand binding reagent
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
G01N 33/564 - ImmunoassayBiospecific binding assayMaterials therefor for pre-existing immune complex or autoimmune disease
A61K 39/00 - Medicinal preparations containing antigens or antibodies
23.
FcRn-specific human antibody and composition for treatment of autoimmune diseases
The present invention relates to a human antibody specific for FcRn that is a receptor with a high affinity for IgG, a production method thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune disease using the same. The FcRn-specific antibody according to the present invention can bind to FcRn non-competitively with IgG or the like to reduce serum auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
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
G01N 33/566 - ImmunoassayBiospecific binding assayMaterials therefor using specific carrier or receptor proteins as ligand binding reagent
ABSTRACT The present disclosure relates to an isolated anti-FcRn antibody, which is an antibody binding to FcRn (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases. Date Recue/Date Received 2020-10-05
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 21/04 - Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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
The present disclosure relates to an isolated anti-FcRn antibody, which is an antibody binding to FcRn (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61P 37/00 - Drugs for immunological or allergic disorders
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
The present disclosure relates to an isolated anti-FcRn antibody, which is an antibody binding to FcRn (stands for neonatal Fc receptor, also called FcRP, FcRB or Brambell receptor) that is a receptor with a high affinity for IgG or a fragment thereof, a method of preparing thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune diseases using the antibody. The FcRn-specific antibody according to the present disclosure binds to FcRn non-competitively with IgG to reduce serum pathogenic auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
HANALL BIOPHARMA CO., LTD. (Republic of Korea)
Inventor
Shin, Byung Cheol
Seong, Hasoo
Lee, Aeri
Kong, Jae Yang
Cheon, Hyae Gyeong
Cho, Young Sik
Jun, Sung Soo
Jo, Young Gwan
Abstract
The present invention relates to a composition for external application for improving a skin disease (e.g. psoriasis). The composition contains adenosylcobalamin (coenzyme B12), optionally in admixture with other cobalamins. The composition can be present in the form of liposomal preparations, which are made of a phospholipid and cholesterol.
A61K 31/714 - Cobalamins, e.g. cyanocobalamin, vitamin B12
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/575 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
A61K 31/683 - Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
The present invention relates to a human antibody specific for FcRn that is a receptor with a high affinity for IgG, a production method thereof, a composition for treating autoimmune disease, which comprises the antibody, and a method of treating and diagnosing autoimmune disease using the same. The FcRn-specific antibody according to the present invention can bind to FcRn non-competitively with IgG or the like to reduce serum auto-antibody levels, and thus can be used for the treatment of autoimmune diseases.
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
The present invention provides an N1-cyclic amine-N5-substituted biguanide derivative compound represented by Formula 1, a method of preparing the same and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an actice ingredient. The biguanide derivatives have an effect of inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence by activation of AMPK, even when administered in a small dose compared with conventional drugs.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 277/02 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of guanidine from cyanamide, calcium cyanamide or dicyandiamides
The present invention relates to new uses of modified human tumor necrosis factor receptor-1 (TNFRI) polypeptide, and more particularly, to uses thereof for prevention and treatment of dry eye syndrome. The modified TNFRI or modified TNFRI fragment of the present invention has excellent TNFα neutralizing activity, and inhibits TNFα activity on the ocular surface of the patient to suppress inflammation induction effects related to dry eye. Therefore, the modified TNFRI or modified TNFRI fragment of the present invention exhibits remarkable effects in the prevention and treatment of dry eye syndrome, and thus can be very useful in the prevention and treatment of dry eye syndrome.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
The present invention provides: a bosentan controlled release oral preparation comprising bosentan as an active ingredient, a pharmaceutically acceptable salt thereof, or a solvate thereof, and an extended release material; a method for preparing the bosentan controlled release oral preparation; and a method for treating pulmonary arterial hypertension.Since the frequency of administering bosentan, a pharmaceutically acceptable salt thereof, or a solvate thereof can be reduced by the present invention, it is possible to improve the convenience of drug administration, thereby improving compliance. In addition, it is possible to increase treatment effects and decrease side effects. Furthermore, a bosentan controlled release oral preparation can be effectively prepared by the present invention.
The present invention relates to a modified human tumor necrosis factor receptor-1 polypeptide which is capable of binding to a tumor necrosis factor in vivo or ex vivo, or to a fragment thereof. The modified human tumor necrosis factor receptor-1 polypeptide or the fragment thereof according to the present invention exhibit improved binding affinity to the tumor necrosis factor.
An N1-cyclic amine-N5-substituted phenyl biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 277/02 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of guanidine from cyanamide, calcium cyanamide or dicyandiamides
A N1-cyclic amine-N5-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 277/02 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of guanidine from cyanamide, calcium cyanamide or dicyandiamides
An N1-cyclic amine-N2-substituted biguanide derivative of Formula 1 or a pharmaceutically acceptable salt thereof, a method of manufacturing the same, and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient are provided. The biguanide derivatives have an effect of inhibiting cancer cell proliferation and also exhibit anticancer activity including inhibition of cancer metastasis and cancer recurrence, because they are effective in activating AMPK, which is associated with the control of energy metabolism, even when administered in a small dose compared with conventional drugs. Also, the biguanide derivatives are highly effective at lowering blood glucose and lipid concentration by AMPK activation, thus they may be effectively used to treat diabetes mellitus, obesity, hyperlipemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome and metabolic syndrome.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 277/02 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of guanidine from cyanamide, calcium cyanamide or dicyandiamides
The present invention relates to a pharmaceutical composition for inhibiting cancer recurrence or metastasis and a method for inhibiting cancer recurrence or metastasis using the same. The present invention identified the activity of 2-deoxy-D-glucose (2-DG, below) for the inhibition of mammosphere formation and EMT, indicating its inhibitory effect against proliferation of cancer stem cell and cancer metastasis, which has not been known hitherto. The present invention also identified that the combined use of a biguanide based antidiabetic agent or its pharmaceutically acceptable salt and 2-DG can inhibit cancer metastasis and steeply decrease cancer recurrence in comparison to the single use of said active ingredients, resulting in a superior effect in the inhibition of cancer metastasis and recurrence when the same dosage is applied. Therefore, the pharmaceutical composition of the present invention can be used to show substantially more excellent effect with less amount of each active ingredient, reducing the side effects due to the use of excess drug and due to their pharmacological action, and providing more efficacious treatment. Moreover, when it is used along with an anticancer agent to which resistance is shown, it is expected that more synergistic effect can be exhibited. Therefore, the pharmaceutical composition and method for inhibiting cancer recurrence or metastasis according to the present invention can be used very advantageously for the treatment and prevention of metastasis or recurrence of various cancer diseases.
A method of treating mild atopic dermatitis patients by locally administering an external composition containing adenosylcobalamin as an active ingredient is provided. The composition can effectively treat mild atopic dermatitis patients without side effects.
Provided is a modified human tumor necrosis factor receptor-1 polypeptide or a fragment thereof that binds to a tumor necrosis factor in vivo or ex vivo. The modified human tumor necrosis factor receptor-1 polypeptide or fragment exhibits improved ability to bind tumor necrosis factor and resistance to proteases.
C07K 14/715 - ReceptorsCell surface antigensCell surface determinants for cytokinesReceptorsCell surface antigensCell surface determinants for lymphokinesReceptorsCell surface antigensCell surface determinants for interferons
C12N 15/70 - Vectors or expression systems specially adapted for E. coli
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 5/00 - Drugs for disorders of the endocrine system
A61P 11/00 - Drugs for disorders of the respiratory system
A61K 31/7088 - Compounds having three or more nucleosides or nucleotides
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
A61P 41/00 - Drugs used in surgical methods, e.g. surgery adjuvants for preventing adhesion or for vitreum substitution
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
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
A61P 1/18 - Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
C12N 1/21 - BacteriaCulture media therefor modified by introduction of foreign genetic material
39.
Modified human tumor necrosis factor receptor-1 polypeptide or fragment thereof, and method for preparing same
The present invention relates to a modified human tumor necrosis factor receptor-1 polypeptide to be coupled to a tumor necrosis factor in vivo or ex vivo, or to a fragment thereof. The modified human tumor necrosis factor receptor-1 polypeptide or the fragment thereof according to the present invention exhibit improved resistance against in vivo protease activity, and thus exhibit improved bioavailability and an improved absorption rate.
The present invention relates to a modified human tumor necrosis factor receptor-1 polypeptide or a fragment thereof which is bound to a tumor necrosis factor in vivo or ex vivo. The modified human tumor necrosis factor receptor-1 polypeptide or the fragment thereof according to the present invention exhibits improved binding force to the tumor necrosis factor and improved protease resistance.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The present invention relates to a modified human tumor necrosis factor receptor-1 polypeptide to bind to a tumor necrosis factor in vivo or ex vivo, or to a fragment thereof. According to the present invention, the modified human tumor necrosis factor receptor-1 polypeptide or the fragment thereof exhibits improved binding force to the tumor necrosis factor.
The present invention relates to N,N-dimethyl imidodicarbonimidic diamide acetate, a method of preparing the same and a pharmaceutical composition comprising the same, and more particularly, to N,N-dimethyl imidodicarbonimidic diamide acetate which is a crystalline acid addition salt prepared by reacting N,N-dimethyl imidodicarbonimidic diamide with acetic acid, and which is very effective as a therapeutic agent for treating metabolic syndromes that glycosuria and diabetes mellitus, obesity, hyperlipidemia, fatty liver, coronary heart disease, osteoporosis, polycystic ovarian syndrome, a cancer depleted of gene P53, etc. are complexly occurred; treating diabetes mellitus and preventing its complication; and treating a cancer and preventing myalgia, muscle cell cytotoxicity and rhabdomyolysis, etc. since the acid addition salt is excellent in physicochemical properties such as solubility, stability, non-hygroscopicity, anti-adhering property, etc., and low toxicity, a method of preparing the same and a pharmaceutical composition comprising the same.
A01N 37/52 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing groups, e.g. carboxylic acid amidines
C07C 277/00 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
C07C 279/00 - Derivatives of guanidine, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
The present invention relates to an anti-cancer pharmaceutical composition comprising phenformin or a pharmaceutically acceptable salt thereof and 2-deoxy-D-glucose as active ingredients, having anticancer activity. The pharmaceutical composition shows far superior anticancer effects through the synergistic action between each active ingredient over the case using a single active ingredient, and can reduce the side effects caused by drugs due to the decrease of dose. In addition, the present invention can remarkably reduce side effects such as lactic acidosis caused by phenformin through delayed release or delayed administration of active ingredients. Particularly, the pharmaceutical composition according to the present invention also has increased compliance of a patient, and thus can be very useful for treating various types of cancers.
Disclosed herein are a 1,3,5-triazine-2,4,6-triamine compound or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a composition for preventing or treating metabolic syndromes, diabetes, or cancers with deletion of P53 gene, which comprises the same.
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
C07D 403/00 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group
Disclosed herein is a combination therapy and a combination preparation of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor characterized in that the angiotensin-II-receptor blocker is absorbed substantially later than the HMG-CoA reductase inhibitor. As the angiotensin-II-receptor blocker and the HMG-CoA reductase inhibitor are released at different times, the present combination therapy prevents competitive inhibition between the two drugs and side effects, as well as simultaneously provides synergistic effects for each active ingredient and convenience of taking the drugs.
A01N 43/64 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with three nitrogen atoms as the only ring hetero atoms
46.
BIGUANIDE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ACTIVE INGREDIENT
The present invention provides a biguanide derivative or pharmaceutically acceptable salt thereof represented by Formula 1 with N4-N5-substitutions, a preparation method thereof and a pharmaceutical composition containing the biguanide derivative as an active ingredient. Compared with conventional drugs, even a small amount of the biguanide derivative of the present invention exhibits excellent effects of AMPKα activation and inhibition of cancer cell proliferation, which makes it useful for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer and the like.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 277/00 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
The present invention provides a biguanide derivative or pharmaceutically allowable salt thereof represented by Formula 1 with N1-N5 substitution, a preparation method thereof and a pharmaceutical composition containing the biguanide derivative as an active ingredient. Compared with conventional drugs, even a small amount of the biguanide derivative of the present invention exhibits excellent effects of AMPKα activation and inhibition of cancer cell proliferation, which makes it useful for the treatment of diabetes, obesity, hyperlipidemia, hypercholesterolemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovarian syndrome, metabolic syndrome, cancer and the like.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 277/02 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups of guanidine from cyanamide, calcium cyanamide or dicyandiamides
The present invention relates to a modified human tumor necrosis factor receptor-1 polypeptide to be coupled to a tumor necrosis factor in vivo or ex vivo, or to a fragment thereof. The modified human tumor necrosis factor receptor-1 polypeptide or the fragment thereof according to the present invention exhibit improved resistance against in vivo protease activity, and thus exhibit improved bioavailability and an improved absorption rate.
Provided is a use for anticancer of dichloroacetic acid salt or aminooxyacetic acid salt of N,N-dimethyl imidodicarbonimidic diamide (metformin). According to the present invention, the acid addition salt of metformin synergistically causes anticancer effect by AMPK enzyme activation of metformin and anticancer effect of organic acids used as a salt, and thus shows a remarkable anticancer effect. In addition, the acid addition salt has superior physiochemical properties such as solubility, stability, non-hygroscopicity, processibility as a tablet formulation and the like, and has lower toxicity compared with metformin hydrochloride. Therefore, the acid addition salt can be useful as a pharmaceutically acceptable salt.
The present invention relates to a pharmaceutical preparation comprising: an immediate-release compartment including beta-adrenergic blockers as pharmacologically active ingredients; and an extended-release compartment including angiotensin II receptor blockers as pharmacologically active ingredients. The preparation of the present invention exhibits uniform anti-tension effects and effects of preventing complications, and particularly, maintains the blood pressure at a constant level in the dangerous time period in which complications might occur, and thus can be effectively used for a hypertension patient suffering from complications and for a patient requiring the blood pressure thereof to be inhibited during sleep, and effectively reduces side effects caused by the interaction between drugs.
The present invention relates to metformin methanesulfonate, to a method for preparing same, to a pharmaceutical composition comprising same, and to a combined formulation comprising same. The metformin methanesulfonate of the present invention has superior stability, enables easy tabletting, has low toxicity, and exhibits excellent AMPKα-activating effects, and thus can be effectively used in treating glycosuria, diabetes, metabolic syndrome, diabetes complications, menstrual irregularities, hypertension, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome, cancer, myalgia, symptoms of muscle cell cytotoxicity, rhabdomyolysis and/or climacterium, etc.
The present invention relates to a metformin caffeic acid salt, to a method for preparing same, to a pharmaceutical composition comprising same, and to a combined formulation comprising same. The metformin caffeic acid salt of the present invention has superior stability, enables easy tabletting, and has low toxicity, thus can be valuably used in the treatment of glycosuria, diabetes, metabolic syndrome, diabetes complications, menstrual irregularities, hypertension, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome, cancer, myalgia, symptoms of muscle cell cytotoxicity, rhabdomyolysis, climacterium, etc., and/or provides antioxidant activity.
The present invention relates to metformin taurate, to a method for preparing same, to a pharmaceutical composition comprising same, and to a combined formulation comprising same. The metformin taurate of the present invention has superior stability, enables easy tabletting, has low toxicity, and exhibits excellent AMPKα-activating effects, and thus can be effectively used in treating glycosuria, diabetes, metabolic syndrome, diabetes complications, menstrual irregularities, hypertension, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome, cancer, myalgia, symptoms of muscle cell cytotoxicity, climacterium and rhabdomyolysis, etc., and provides antioxidant activity.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 309/14 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing nitrogen atoms, not being part of nitro or nitroso groups, bound to the carbon skeleton containing amino groups bound to the carbon skeleton
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N)Sulfinylamines (—N=SO)Sulfonylamines (—N=SO2)
54.
METFORMIN ASCORBATE, METHOD FOR PREPARING SAME, PHARMACEUTICAL COMPOSITION COMPRISING SAME, AND COMBINED FORMULATION COMPRISING SAME
The present invention relates to metformin ascorbate, to a method for preparing same, to a pharmaceutical composition comprising same, and to a combined formulation comprising same. The metformin ascorbate of the present invention has superior stability, enables easy tabletting, and has low toxicity, and thus can be effectively used in treating glycosuria, diabetes, metabolic syndrome, diabetes complications, menstrual irregularities, hypertension, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndrome, cancer, myalgia, symptoms of muscle cell cytotoxicity, rhabdomyolysis, climacterium, etc., and/or provides antioxidant activity.
C07D 493/22 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains four or more hetero rings
C07D 493/02 - Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
55.
BUTYRIC ACID SALT OF N,N-DIMETHYL IMIDOCARBON IMIDIC DIAMIDE, METHOD OF PREPARING SAME, AND PHARMACEUTICAL COMPOSITIONS AND COMBINATIONS CONTAINING SAME
The present invention provides metformin butyric acid salt, a method of preparing the same, and pharmaceutical compositions and combinations containing the same. The metformin butyric acid salt according to the present invention has an excellent pharmacological effect as compared with metformin hydrochloride and is capable of achieving a therapeutic purpose by administering an amount less than metformin hydrochloride. Furthermore, the metformin butyric acid salt has excellent physicochemical properties, such as solubility, stability, hygroscopicity and adsorption preventing property, in processibility of formulations and thereby is capable of being usefully utilized as a pharmaceutically acceptable salt of the metformin.
The present invention provides metformin propionate, a method of preparing the same, and pharmaceutical compositions and combinations containing the same. The metformin propionate according to the present invention has an excellent pharmacological effect as compared with metformin hydrochloride and is capable of achieving a therapeutic purpose by administering an amount less than metformin hydrochloride. Furthermore, the metformin propionate has excellent physicochemical properties, such as solubility, stability, hygroscopicity and adsorption preventing property, in processibility of formulations and thereby is capable of being usefully utilized as a pharmaceutically acceptable salt of the metformin.
C07C 279/26 - X and Y being nitrogen atoms, i.e. biguanides
C07C 277/00 - Preparation of guanidine or its derivatives, i.e. compounds containing the group the singly-bound nitrogen atoms not being part of nitro or nitroso groups
The present invention relates to a pharmaceutical composition containing fluvastatin with enhanced stability. Preferably, the present invention relates to a pharmaceutical composition of fluvastatin and a method for manufacturing the same. The composition contains fluvastatin with improved stability in long term storage and pharmaceutically acceptable salts or isomers thereof for preventing and treating hyperlipidemia or hepatitis C.
A61K 31/405 - Indole-alkanecarboxylic acidsDerivatives thereof, e.g. tryptophan, indomethacin
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
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
The present invention relates to a pharmaceutical preparation comprising an immediate-release compartment containing a renin inhibitor as a pharmacologically active ingredient, and an extended-release compartment containing a dihydropyridine calcium channel blocker as a pharmacologically active ingredient. The pharmaceutical preparation of the present invention can avoid in vivo pharmacokinetic interaction between the renin inhibitor and the dihydropyridine calcium channel blocker, induces optimum pharmacological effects in accordance with the in vivo absorption performance of each of the active ingredients, and enables drugs to be released at the time period in which each of the active ingredients exhibits the pharmacological effects thereof, to thereby increase clinical effects, and can thus be valuably used in the prevention or treatment of metabolic syndrome, cardiovascular disease, and kidney disease.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
The present invention relates to a pharmaceutical preparation comprising an immediate-release compartment and an extended-release compartment, wherein said immediate-release compartment and said extended-release compartment each contain different oral anticancer drugs as active ingredients. The pharmaceutical preparation of the present invention is advantageous in that drug interactions and side effects of oral anticancer drugs can be minimized, and the administration of the pharmaceutical preparation can be easily performed.
The prevent invention relates to an external use composition containing cholecalciferol or a derivative thereof for treating skin disorders. More specifically, the present invention relates to an external preparation composition for treating skin disorders such as atopic dermatitis and a method for manufacturing a liposome. The composition and method increase skin penetration by enclosing cholecalciferol (vitamin D3) or a derivative thereof as an active ingredient in a nanoscopic liposome so that skin penetration time can be minimized when applied to a lesion. Therefore, variations in drug effects due to light are reduced and drug effects are quickly expressed.
The present invention provides a modified human thrombopoietin polypeptide fragment that has platelet proliferative activity in vivo and in vitro and enhanced resistance to protease existing in vivo.
C12N 15/63 - Introduction of foreign genetic material using vectorsVectorsUse of hosts thereforRegulation of expression
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
Provided is an oral pharmaceutical composition comprising: a drug which is metabolised in the liver and a liver protectant. The composition of the present invention can prevent or alleviate drug-induced hepatotoxicity following the administration of a drug which is metabolised in the liver.
42 - Scientific, technological and industrial services, research and design
Goods & Services
Design and development of computer hardware and software; Scientific and industrial research; Design of commercial products; Creating, designing and maintaining web sites; Design of computer databases; Technical research services; Analysis of materials; Testing of products; Medical laboratory services; Biochemistry research services; Genetic research; Health and safety testing, research, design and auditing; Laboratory research; Provision of research services; Research into new products; Research relating to pharmaceuticals; Research relating to foods and dietary supplements; Research relating to cosmetics.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations; Medical preparations; Sanitary preparations for medical purposes; Biochemical preparations for medical use; Dietetic substances for medicinal purposes; disinfectants; Fungicides, herbicides; Plasters, materials for dressings; Agents for activating the metabolism; Nutritional supplements for medical use; Enzymes for medical use; Materials for use in applying pharmaceutical preparations; Diagnostic agents for pharmaceutical use; Pocket medicine cases [fitted]; Pharmaceutical preparations for hepatitis treatment; Pharmaceutical preparations for hepatitis C treatment; Interferon in dosage form adapted for oral administration; Immunological products for intravenous injections.
05 - Pharmaceutical, veterinary and sanitary products
35 - Advertising and business services
42 - Scientific, technological and industrial services, research and design
Goods & Services
Pharmaceutical preparations; Medical preparations; Sanitary preparations for medical purposes; Biochemical preparations for medical use; Dietetic substances for medicinal purposes; disinfectants; Fungicides, herbicides; Plasters, materials for dressings; Agents for activating the metabolism; Nutritional supplements for medical use; Enzymes for medical purposes; Materials for use in applying pharmaceutical preparations; Diagnostic agents for pharmaceutical use; Pocket medicine cases [fitted]; excluding vitamin and mineral preparations and dietetic products like sweeteners, dietetic sugars and sugars for diabetics. Advertising, marketing and promotion services; Business administration services; Business management services; Office functions services; Computer data processing; Computerised database management services; Export-import agency services; Wholesale and retail store services relating to pharmaceutical products; Brokerage services of pharmaceutical products; Sales arranging of pharmaceutical products; Commercial intermediary services in the field of pharmaceutical products; Wholesale and retail store services relating to foods and dietary supplements; Brokerage services of foods and dietary supplements; Sales arranging of foods and dietary supplements; Commercial intermediary services in the field of foods and dietary supplements; Wholesale and retail store services relating to cosmetics; Brokerage services of cosmetics; Sales arranging of cosmetics; Commercial intermediary services in the field of cosmetics. Design and development of computer hardware and software; Scientific and industrial research; Design of commercial products; Creating, designing and maintaining web sites; Design of computer databases; Technical research services; Analysis of materials; Testing of products; Medical laboratory services; Biochemistry research services; Genetic research; Health and safety testing, research, design and auditing; Laboratory research; Provision of research services; Research into new products; Research relating to pharmaceuticals; Research on foods and dietary supplements; Research relating to foods and dietary supplements; Research relating to cosmetics.
The present invention relates to pharmaceutical formulations containing antiviral drugs and sustained-release materials, and to pharmaceutical formulations having an immediate release compartment containing drugs associated with cytochrome P450, as well as an extended release compartment containing antiviral drugs and sustained-release materials. The formulations of the present invention reduce interactions between antiviral drugs to increase the effects of the drugs and to decrease side effects.
The present invention relates to a drug delivery system comprising: a plastic soft capsule having an enclosed space defined therein; a tablet to be kept in the interior space of the capsule; and a drug filling portion, wherein part of the tablet's surface is adhered closely to the inside surface of the capsule and the drug filling portion is composed of the remaining area of the interior space excluding the space occupied by the tablet. Examples of benefits of a drug delivery system according to the present invention include a system which is capable of controlling drug release, physically separating and then filling the same or different active ingredients contained in the system to prevent chemical reactions induced by physical blending of those ingredients, preventing interaction between drugs that can occur inside the body when different kinds of drugs are co-administered, and storing a large amount of active ingredients.
A61J 3/06 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms into the form of pills, lozenges or dragees
A61J 3/00 - Devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms
The present invention relates to sustained-release pharmaceutical formulations comprising beta-adrenergic blockers and HMG-CoA reductase inhibitors. The pharmaceutical formulations of the present invention are more effective, and may reduce side effects when the beta-adrenergic blockers and HMG-CoA reductase inhibitors are individually and simultaneously taken as a single formulation. The pharmaceutical formulations of the present invention are effective for treating hypertension in patients with complex diseases such as hyperlipidemia, coronary artery disease, etc. The pharmaceutical formulations of the present invention are also effective for preventing complications developed from the abovementioned diseases, and make it easy to give administration instructions to patients.
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
Inventor
Kim, Sung Wuk
Jun, Sung Soo
Cheon, Hyae Gyeong
Kim, Kwang Rok
Rhee, Sang Dal
Jung, Won Hoon
Lee, Jong Cheol
Abstract
The present invention relates to an N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative expressed in chemical formula 1, to a pharmaceutically acceptable salt thereof, to a preparation method thereof, and to a pharmaceutical composition containing the same as an active ingredient. The N1-benzo[1,3]dioxol-5-ylmethyl-N2-substituted biguanide derivative of the present invention shows superior hypoglycemic action and superior hypolipidemic action even at a lower dosage as compared with conventional drugs, and thus can be used for the prevention and treatment of metabolic syndrome disorders such as diabetes, non-insulin-dependent diabetes, obesity, arteriosclerosis, and the like, or cancer involving P53 gene deficiency.
C07D 317/48 - Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
70.
Ｎ1-2-THIOPHENE-2-YLETHYL-Ｎ2-SUBSTITUTED BIGUANIDE DERIVATE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENTS
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
Inventor
Kim, Sung Wuk
Jun, Sung Soo
Cheon, Hyae Gyeong
Kim, Kwang Rok
Rhee, Sang Dal
Jung, Won Hoon
Lee, Jong Cheol
Abstract
The present invention relates to an Ｎ1-2-thiophene-2-ylethyl-Ｎ2-substituted biguanide derivate expressed in Chemical Formula 1, a pharmaceutically allowable salt thereof, a preparation method thereof, and a pharmaceutical composition containing the same as active ingredients. The Ｎ1-2-thiophene-2-ylethyl-Ｎ2-substituted biguanide derivate of the present invention shows a superior hypoglycemic action and a superior hypolipidemic action even at a low dosage as compared with conventional drugs, and thus can be used for prevention and treatment of diabetes, non-insulin-dependent diabetes, obesity, the metabolic syndrome and arteriosclerosis, or cancer involving P53 gene deficiency.
The present invention provides a drug delivery device comprising a hard capsule and a micro-aperture penetrating through the wall of the hard capsule. The interior of the hard capsule contains an immediate-release compartment and an extended-release compartment. The drug delivery device of the present invention is greatly effective in releasing one or more drugs which require controlled release in the body.
A61K 9/52 - Sustained or differential release type
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
Disclosed herein is a lag time delayed-release combination pharmaceutical composition comprising of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, as well as a preparation method thereof. The composition is designed based on chronotherapy in which active ingredients are administered to have different onset times, such that the release of each active ingredient of the composition in body can be lag time delayed to a specific rate. Also, the composition is very effective for the treatment of hypertension and the prevention of complications in patients having metabolic syndromes which show diabetes, obesity, hyperlipidemia, coronary artery diseases and the like. More specifically, the composition is a drug delivery system designed such that the release of each drug is controlled to a specific rate, and it can show the most ideal effect, when it is absorbed in body.
The present invention provides a pharmaceutical formulation for mornings comprising: an immediate release compartment containing a dihydropyridine calcium channel blocker as a pharmacologically active ingredient, and a sustained release compartment containing an HMG-CoA reductase inhibitor as a pharmacologically active ingredient. The formulation of the present invention reduces side effects caused by interaction between drugs and is effective in treating and preventing hypertension and hyperlipidemia and cardiovascular diseases or metabolic syndrome caused thereby due to pharmacological synergism. Also, the formulation can enhance drug compliance.
The present invention relates to a pharmaceutical formulation containing a calcium channel blocker as a pharmacologically active ingredient and a release control material, and a pharmaceutical formation including an immediate-release compartment containing a hepatitis preventive and inhibitor as a pharmacologically active ingredient, and an extended-release compartment containing a calcium channel blocker as a pharmacologically active ingredient. The formulation of the present invention has the advantages of maximizing the effects of pharmacological and clinical pressure resistance and the effects of preventing complication when taken, avoiding an interaction with the drugs metabolized by the same enzyme in the liver, and preventing and inhibiting drug-induced hepatitis caused by the medication being taken for a long time.
The present invention provides a pharmaceutical preparation comprising a prerelease compartment that includes an angiotension-2 receptor antagonist as its pharmacologically active ingredient and a delay-release compartment that includes a beta adrenalin blocker as its pharmacologically active ingredient; the preparation of the present invention acts to maintain a uniform constant pressure and prevent complications, and in particular, enables holding blood pressure uniform during the risk period for complications, so that it has the advantage of being useful for hypertension patients with complications, patients requiring blood pressure suppression during sleep, etc., and of reducing adverse reactions caused by drug interactions.
A61K 9/26 - Discrete particles in supporting matrix
A61K 9/22 - Sustained or differential release type
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
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
Modified erythropoietin (EPO) polypeptides and other modified therapeutic polypeptides are provided. The EPO polypeptides and other therapeutic polypeptides are modified to exhibit physical properties and activities that differ from the unmodified EPO polypeptides and other unmodified therapeutic polypeptides, respectively. Nucleic acid molecules encoding these polypeptides also are provided. Also provided are methods of treatment and diagnosis using the polypeptides.
Disclosed is a controlled-release pharmaceutical formulation comprising azelnidipine and HMG-CoA reductase inhibitor or an angiotensin II receptor blocker, wherein as it takes a different amount of time to exhibit a pharmacological effect of each individual ingredient of the pharmaceutical formulation in a human body, each of the ingredients can be control-released at a specific rate to exhibit the optimum effect on absorption in the human body. The pharmaceutical formulation of the present invention is highly effective in treating hypertension and preventing its complications in persons having a so-called metabolic syndrome, which is present as a complex of hyperlipidemia, coronary artery disease, heart disease, kidney disease or cerebrovascular disease, etc., wherein, by increasing patient compliance, the impact on external factors can also be maximized.
A61K 9/22 - Sustained or differential release type
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 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention provides a pharmaceutical preparation which comprises: an early release zone containing an HMG-CoA reductase inhibitor as a pharmacological active component; and a delayed release zone containing a fibric acid derivative as a pharmacological active component. The pharmaceutical preparation of the present invention is designed in such a way as to allow the controlled release of drugs over a specific time period and at a specific rate, and is highly efficacious in the treatment of hyperlipidaemia.
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
The present invention provides a pharmaceutical formulation containing an angiotensin-II receptor blocker and a release-control material as a pharmacologically active ingredient and a pharmaceutical formulation comprising an immediate-release compartment and an extended-release compartment. The immediate-release compartment contains an agent as a pharmacologically active ingredient for preventing and inhibiting hepatitis and the extended-release compartment has an angiotensin-II receptor blocker as a pharmacologically active ingredient. The formulation of the present invention maximizes the effectiveness on pharmacologically and clinically lowering blood pressure and preventing complications when taking the formulation, helps to avoid interaction with a drug which is metabolized by the same enzyme in the liver, and prevents and inhibits the incidence of drug-induced hepatitis which is caused by drug administration for a long time.
The present invention relates to a controlled-release combination of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor, in which each ingredient of the combination can be control-released at a specific rate based on the different in-vivo expressions of each ingredient. The present invention is a combined pharmaceutical composition which is effective for treatment of hypertension and prevention of complications in the medical complication known as the metabolic syndrome wherein diabetes, obesity, hyperlipidemia, coronary artery disease and the like, appear in combination, and to a preparation method thereof. More particularly, the present invention relates to a controlled-release drug delivery system for a combination of an angiotensin-II-receptor blocker and an HMG-CoA reductase inhibitor which releases the drugs at optimal rates for their in vivo absorption, maximizes effects and improves patient compliance.
A61K 9/26 - Discrete particles in supporting matrix
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/00 - 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 present invention provides (1) a release-controlled pharmaceutical formulation including an Atorvastatin-containing early release compartment and a Losartan-containing retarded release compartment, (2) a release-controlled pharmaceutical formulation including an Atorvastatin-containing early release compartment and an Irbesartan-containing retarded release compartment, (3) a release-controlled pharmaceutical formulation including an Atorvastatin-containing early release compartment and an Olmesartan-containing retarded release compartment, (4) a release-controlled pharmaceutical formulation including an Atorvastatin-containing early release compartment and a Valsartan-containing retard release compartment, (5) a release-controlled pharmaceutical formulation including an Atorvastatin-containing early release compartment and a Telmisartan-containing retarded release compartment, (6) a release-controlled pharmaceutical formulation including an Atorvastatin-containing early release compartment and a Candesartan-containing retarded release compartment, (7) a release-controlled pharmaceutical formulation including a Pitavastatin-containing early release compartment and a Losartan-containing retarded release compartment, and (8) release-controlled pharmaceutical formulation including a Pitavastatin-containing early release compartment and an Irbesartan-containing retard release compartment. The pharmaceutical formulation of the present invention minimizes an antagonism between drugs and side effects of the drugs and maximizes unique effects of drugs because different drugs contained in different compartments in the formulation are released with a time difference. The pharmaceutical formulation of the present invention prepared by the specific combination of two drugs exhibits remarkably excellent effects of treatment or prevention of disease as compared with with a single medication or a simply combined medication.
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
82.
PHARMACEUTICAL FORMULATION FOR TREATMENT OF CARDIOVASCULAR DISEASE
The present invention provides (1) a release-controlled pharmaceutical formulation including a Simvastatin-containing early release compartment and a Losartan-containing retarded release compartment, (2) a release-controlled pharmaceutical formulation including a Simvastatin-containing early release compartment and an Olmesartan-containing retarded release compartment, (3) a release-controlled pharmaceutical formulation including a Simvastatin-containing early release compartment and a Valsartan-containing retarded release compartment, (4) a release-controlled pharmaceutical formulation including a Simvastatin-containing early release compartment and a Candesartan-containing retarded release compartment, (5) a release-controlled pharmaceutical formulation including a Rosuvastatin-containing early release compartment and a Losartan-containing retarded release compartment, (6) a release-controlled pharmaceutical formulation including a Rosuvastatin-containing early release compartment and an Iresartan-containing retarded release compartment, and (7) a release-controlled pharmaceutical formulation including a Rosuvastatin-containing early release compartment and a Candesartan-containing retarded release compartment. The pharmaceutical formulation of the present invention minimizes an antagonism between drugs and side effects of the drugs and maximizes unique effects of drugs because different drugs contained in different compartments in the formulation are released with a time difference. The pharmaceutical formulation of the present invention prepared by the specific combination of two drugs exhibits remarkably excellent effects of treatment or prevention of disease as compared with a single medication or a simply combined medication.
The present invention relates to a pharmaceutical composition in which release of a thiazide-based compound and angiotensin-II-receptor blocker is controlled, and to a combination preparation technique for the same. More particularly, the present invention relates to a preparation technique capable of maximizing pharmacological and clinical blood pressure control effects and complication preventive effects and significantly reducing side effects by administrating a release-controlled combination preparation rather than administrating a single preparation of thiazide-based compound and a single preparation of angiotensin-II-receptor blocker at the same time.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
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
The present invention provides a pharmaceutical formulation comprising an immediate-release compartment containing hydrochlorothiazide as a pharmacologically active ingredient and an extended-release compartment containing losartan as a pharmacologically active ingredient. Since the formulation of the present invention can deliver hydrochlorothiazide and losartan at a specific rate at different times, it is very effective in treating hypertension and preventing complications, and has the effects of improving the adaptation rate of the patient, optimizing drug delivery time and reducing side effects.
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
A61K 9/26 - Discrete particles in supporting matrix
A61K 9/00 - Medicinal preparations characterised by special physical form
The present invention provides a pharmaceutical formulation comprising a compartment containing a rennin inhibitor as a pharmacologically active ingredient, and a compartment having an angiotensin-II-receptor blocker as a pharmacologically active ingredient. One of the compartments is an immediate-release compartment and the other one is an extended-release compartment. Since the disclosed formulation delivers the rennin inhibitor and angiotensin-II-receptor blocker at a specific delivery rate at a different time. It has an advantage in reducing the concern about side effects, improving drug effects, and simplifying the instructions for use of the drug. In addition, the formulation can pharmacologically, clinically, scientifically, and economically achieve more useful effects than the complex prescription case of taking the ingredients separately or each at once, in preventing and treating metabolic syndrome, cardiovascular disease and renal disease.
A61K 9/22 - Sustained or differential release type
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
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 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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
The present invention provides a pharmaceutical formulation comprising an immediate-release compartment containing an angiotensin-2 receptor blocker (ARB) as a pharmacologically active ingredient and an extended-release compartment containing a non-dihydropyridine calcium channel blocker as a pharmacologically active ingredient. Since the disclosed formulation enables the release of the two ingredients at a different time, it reduces side effects and increases the effects of the drug more than the case of separately administering the ingredients each at the same time. In addition, the formulation maximizes the effects of drug at the time of day when the complication risk of cardiovascular system diseases is highest.
A61K 9/22 - Sustained or differential release type
A61K 31/435 - 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
The present invention relates to a pharmaceutical formulation containing an extended-release compartment having a dihydropyridine calcium channel blocker and an immediate-release compartment having an angiotensin-2 receptor blocker. The present invention provides the pharmaceutical formulation in which the dihydropyridine calcium channel blocker and angiotensin-2 receptor blocker are separately contained in each compartment and of which release is controlled. Since each different drug contained in each different compartment of the formulation is released at a different time, the pharmaceutical formulation of the present invention minimizes the antagonism and side effects between drugs and maximizes the specific effect of the drugs. The pharmaceutical formulation by the specific combination between the two drugs according to the present invention has remarkably good effects in treating or preventing diseases compared with the single administration of each of the drugs or the simple combined administration of the drugs.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
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 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
Modified erythropoietin (EPO) polypeptides and other modified therapeutic polypeptides are provided. The EPO polypeptides and other therapeutic polypeptides are modified to exhibit physical properties and activities that differ from the unmodified EPO polypeptides and other unmodified therapeutic polypeptides, respectively. Nucleic acid molecules encoding these polypeptides also are provided. Also provided are methods of treatment and diagnosis using the polypeptides.
The invention provides a pharmaceutical formulation, which comprises a pre-release portion containing HMG-CoA (hydroxymethylglutaryl-CoA) reductase as a pharmacologically active component, and a sustained-release portion containing bis-dihydropyridine-class calcium-channel blocker as a pharmacologically active component. The formulation of the invention offers synergy effects through co-administration of the bis-dihydropyridine-class calcium-channel blocker/HMG-CoA (hydroxymethylglutaryl-CoA) reductase, and induces the time-dependent absorption, metabolism and mechanism of individual drug through the controlled release to avoid competitive antagonistic interactions between drugs, thus maximizing effects of each pharmacologically active component while minimizing side effects, for example, the risk of myopathy, and substantially increasing the compliance of patients by taking one tablet once per day.
Disclosed is a pharmaceutical preparation including a compartment containing a renin inhibitor as a pharmacologically active component, and a compartment containing HMG-CoA reductase inhibitor as a pharmacologically active component, wherein one of compartments is an advance release compartment and the other of the compartments is a retard release compartment. The combination preparation of the present invention delivers the renin inhibitor and HMG-CoA reductase inhibitor with a time difference at a specific speed, reducing undesirable side-effects, improving the potentiating effect and allowing for ease in teaching dosing regimens and enhanced patient compliance. Further, the pharmaceutical preparation of the present invention has pharmacological, clinical, scientific and economical advantages in the prevention or treatment of metabolic syndrome, cardiovascular disease, renal disease and the like as compared with the complex drug regimens in which medicament ingredients are taken individually or simultaneously.
A61K 9/52 - Sustained or differential release type
A61K 9/22 - Sustained or differential release type
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/41 - 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 47/00 - 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 present invention provides a composite preparation which comprises: a prior-release section comprising aspirin or a pharmaceutically acceptable salt thereof as a pharmacologically active component; and a delayed-release section comprising clopidogrel, an isomer thereof or a pharmaceutically acceptable salt thereof as a pharmacologically active component. The composite preparation of the present invention exhibits a far better effect in preventing platelet aggregation than does simultaneous oral therapy or treatment with the respective single preparations, and not only can it improve the patient's drug-taking compliance by administration once a day but it can also reduce the adverse reactions which follow long-term administration of aspirin. The composite preparation of the present invention is also advantageous in that it exhibits an outstanding effect in inhibiting blood platelet aggregation despite a reduction in the amount of aspirin ingested, and in that it converts clopidogrel resistance into susceptibility and prevents serious adverse reactions caused by clopidogrel resistance and in that it can be stored over the longer term since it is stable under common storage conditions.
A61K 9/22 - Sustained or differential release type
A61K 47/00 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient
92.
N,N-DIMETHYL IMIDODICARBONIMIDIC DIAMIDE NICOTINATE, METHOD FOR PRODUCING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
Disclosed herein are a novel nicotinic acid salt of N,N-dimethyl imidodicarbonimidic diamide, a preparation method thereof and a pharmaceutical composition comprising the same. More specifically, disclosed herein are the nicotinic acid salt of N,N-dimethyl imidodicarbonimidic diamide, which has improved physical and chemical properties including solubility, stability, non-hygroscopicity and anti-adhesive properties, and low toxicity, and thus is very effective in the prevention and treatment of not only diabetes and its complications in patients with so-called metabolic syndromes, in which diabetes, obesity, hyperlipidemia, fatty liver, coronary artery disease, osteoporosis, polycystic ovary syndromes, etc. appear in combination, but also of p53 gene-deficient cancers, muscular pain, muscle cytotoxicity and rhabdomyolysis, as well as the preparation method thereof and the pharmaceutical composition comprising the same.
