The present disclosure comprises a method for administering 2,3-dihydro-isoindole-1-one compound or a pharmaceutically acceptable salt, ester, solvate and/or prodrug thereof, for the treatment of hematological cancers such as acute myeloid leukemia (AML). The present disclosure further relates to reducing or inhibiting cell-proliferation which is activated by wild-type or mutated Fms-like tyrosine kinase-3 receptor (FLT3). The present disclosure further relates to a method of inhibiting or reducing abnormal (e.g., overexpressed) wild-type or mutated BTK activity or expression in a subject in need thereof.
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61P 35/02 - Antineoplastic agents specific for leukemia
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
2.
2,3-DIHYDRO-ISOINDOLE-1-ON DERIVATIVE AS BTK KINASE SUPPRESSANT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME
The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
The present invention relates to a method for killing cancer cells by using a combination of an HDAC inhibitor and an anti-PD1 antibody or an anti PD-L1 antibody. The present invention can have an effective influence on: extending the survival of animals with cancer, tumors, tumor-related disorders and neoplastic diseases; inhibiting the growth of proliferative cells associated with neoplasms; or neoplastic degeneration.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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 relates to a pharmaceutical composition for the prevention or treatment of severe acute respiratory syndrome coronavirus 2 infection, the pharmaceutical composition containing a compound having a specific chemical structure, a derivative thereof or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition according to the present invention was confirmed to have an anti-inflammatory effect that alleviates acute pulmonary inflammatory lesions shown in a rodent model with induced severe acute respiratory syndrome coronavirus 2 infection, and was confirmed to suppress viral proliferation. Therefore, the pharmaceutical composition can effectively treat or prevent severe acute respiratory syndrome coronavirus 2 infection.
The present invention relates to a pharmaceutical composition for intravenous administration, containing a Fab I inhibitor, and a preparation method therefor. The present invention can be effectively applied to an infection caused by antibiotic-resistant bacteria. Specifically, the present invention enables treatment effects to be more rapidly initiated by improving solubility and dissolution rate, and enables bioavailability to be improved. In addition, by controlling the size of particles, mixing and content uniformity of a preparation can be improved.
A61K 9/00 - Medicinal preparations characterised by special physical form
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
A61K 47/32 - Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
6.
ORALLY ADMINISTERED PHARMACEUTICAL COMPOSITION COMPRISING FAB I INHIBITORS AND METHOD FOR PREPARING SAME
The present invention relates to an orally administered pharmaceutical composition comprising Fab I inhibitors, and to a method for preparing same. The present invention may be applied effectively to bacterial infections resistant to antibiotics and the like. More specifically, the present invention can more rapidly initiate therapeutic effects by improving dissolution and elution rates. Furthermore, the present invention can improve the mixing and content uniformity in preparations by regulating the particle size.
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
The present invention relates to a pharmaceutical composition containing an alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate compound (hereinafter referred to as CG200745PPA) or a derivative thereof, and can provide a pharmaceutical composition in a tablet, granule, powder, capsule, dry syrup or injection form. By providing the composition in various forms, a suitable form can be selected and easily applied when oral administration is difficult.
The present invention relates to a composite agent comprising polmacoxib and pregabalin. The present invention relates to a pharmaceutical composition and a drug or pain reliever, which each comprise the two active ingredients of polmacoxib and pregabalin and, more particularly, to a drug or pain reliever for treatment of moderately severe, acute, chronic, or neuropathic pain attributed to inflammation and various factors, an effect thereof, and a use thereof.
A61K 9/24 - Layered or laminated unitary dosage forms
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
9.
PHARMACEUTICAL COMPOSITION COMPRISING HDAC INHIBITOR AND ANTI-PD1 ANTIBODY OR ANTI PD-L1 ANTIBODY
The present invention relates to a method for killing cancer cells by using a combination of an HDAC inhibitor and an anti-PD1 antibody or an anti PD-L1 antibody. The present invention can have an effective influence on: extending the survival of animals with cancer, tumors, tumor-related disorders and neoplastic diseases; inhibiting the growth of proliferative cells associated with neoplasms; or neoplastic degeneration.
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
10.
PHARMACEUTICAL COMPOSITION COMPRISING HDAC INHIBITOR AND ANTI-PD1 ANTIBODY OR ANTI PD-L1 ANTIBODY
The present invention relates to a method for killing cancer cells by using a combination of an HDAC inhibitor and an anti-PD1 antibody or an anti PD-L1 antibody. The present invention can have an effective influence on: extending the survival of animals with cancer, tumors, tumor-related disorders and neoplastic diseases; inhibiting the growth of proliferative cells associated with neoplasms; or neoplastic degeneration.
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.
2,3-dihydro-isoindole-1-one derivative as BTK kinase suppressant, and pharmaceutical composition including same
The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by absormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
The present invention relates to a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof and a method for preparing same, and can improve moisture stability while maintaining the characteristics, such as the efficacy and effective dose, of a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof. In addition, the present invention can simplify the production and manufacturing process of a formulation by improving hygroscopicity.
C07C 233/40 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
C07C 231/12 - Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
13.
INJECTION COMPOSITION CONTAINING FAB I INHIBITOR, AND PREPARATION METHOD THEREFOR
The present invention relates to a pharmaceutical composition for intravenous administration, containing an Fab I inhibitor, and a preparation method therefor. The present invention can be effectively applied to an infection caused by antibiotic-resistant bacteria. Specifically, the present invention enables treatment effects to be more rapidly initiated by improving solubility and dissolution rate, and enables bioavailability to be improved. In addition, by controlling the size of particles, mixing and content uniformity of a preparation can be improved.
The present invention relates to a pharmaceutical composition containing an alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate compound (hereinafter referred to as CG200745PPA) or a derivative thereof, and can provide a pharmaceutical composition in a tablet, granule, powder, capsule, dry syrup or injection form. By providing the composition in various forms, a suitable form can be selected and easily applied when oral administration is difficult.
The present invention relates to a pharmaceutical composition containing an alkyl carbamoyl naphthalenyloxy octenoyl hydroxyamide phosphate compound (hereinafter referred to as CG200745PPA) or a derivative thereof, and can provide a pharmaceutical composition in a tablet, granule, powder, capsule, dry syrup or injection form. By providing the composition in various forms, a suitable form can be selected and easily applied when oral administration is difficult.
Provided in the present invention is the following compound effective in treating and preventing HIF-associated diseases including ischemia and hypoxia by regulating HIF and stabilizing HIF-α. In particular, the compound is effective in preventing and treating inflammatory bowel disease (IBD). The compound of the present invention is represented by chemical formula I, and in addition, provided are: a prodrug, a salt, and a solvate of the compound, and isomers thereof; a pharmaceutical composition comprising the same; and a preparation method thereof. [Chemical Formula 1] (In the formula, U, V, W, X, Y, R1, R2, and R5 are as defined in the description)
A61K 31/4365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
17.
ORALLY ADMINISTERED PHARMACEUTICAL COMPOSITION COMPRISING FAB I INHIBITORS AND METHOD FOR PREPARING SAME
The present invention relates to an orally administered pharmaceutical composition comprising Fab I inhibitors, and to a method for preparing same. The present invention may be applied effectively to bacterial infections resistant to antibiotics and the like. More specifically, the present invention can more rapidly initiate therapeutic effects by improving dissolution and elution rates. Furthermore, the present invention can improve the mixing and content uniformity in preparations by regulating the particle size.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
The present invention relates to an orally administered pharmaceutical composition comprising Fab I inhibitors, and to a method for preparing same. The present invention may be applied effectively to bacterial infections resistant to antibiotics and the like. More specifically, the present invention can more rapidly initiate therapeutic effects by improving dissolution and elution rates. Furthermore, the present invention can improve the mixing and content uniformity in preparations by regulating the particle size.
A61K 31/4436 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
The present invention relates to a composite agent comprising polmacoxib and pregabalin. The present invention relates to a pharmaceutical composition and a drug or pain reliever, which each comprise the two active ingredients of polmacoxib and pregabalin and, more particularly, to a drug or pain reliever for treatment of moderately severe, acute, chronic, or neuropathic pain attributed to inflammation and various factors, an effect thereof, and a use thereof.
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61P 25/00 - Drugs for disorders of the nervous system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
20.
PHARMACEUTICAL COMPOSITION FOR PREVENTION OR TREATMENT OF FIBROSIS
The present invention relates to a pharmaceutical composition comprising alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide, a derivative thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for prevention or treatment of fibrosis. Effectively suppressing the proliferation of fibrous tissues, the composition can be used for preventing and/or treating fibrosis.
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
21.
PHARMACEUTICAL COMPOSITION, COMPRISING POLMACOXIB AND PREGABALIN, FOR TREATMENT OF PAIN
The present invention relates to a composite agent comprising polmacoxib and pregabalin. The present invention relates to a pharmaceutical composition and a drug or pain reliever, which each comprise the two active ingredients of polmacoxib and pregabalin and, more particularly, to a drug or pain reliever for treatment of moderately severe, acute, chronic, or neuropathic pain attributed to inflammation and various factors, an effect thereof, and a use thereof.
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
The present invention relates to a transdermal absorption preparation containing polmacoxib, the preparation being capable of minimizing the influence of both extrinsic and intrinsic factors and maintaining stable blood concentrations for a predetermined period of time, while maintaining characteristics, such as efficacy and effective dose, of polmacoxib. In addition, side effects, caused by the administration of the preparation, on the internal organs can be minimized and administration frequency can be reduced, and thus patient compliance can be increased.
A61K 47/06 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
The present invention relates to a polmacoxib-containing injection solution and a preparation method therefor and to an injection composition in which polmacoxib, which is a poorly water-soluble nonsteroidal anti-inflammatory drug exhibiting an excellent effect even at a low dose, is solubilized and stabilized in an aqueous solution, and a preparation method therefor. According to the present invention, the utilization of a solubilizer and a stabilizer that are both available for injection agents allows the acquirement of a polmacoxib-containing injection composition excellent in stability without any deposition phenomenon.
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
24.
PHARMACEUTICAL COMPOSITION FOR TREATING ACUTE AND CHRONIC PAIN, CONTAINING POLMACOXIB AND TRAMADOL
The present invention relates to a complex comprising polmacoxib and tramadol. The present invention relates to a pharmaceutical composition and a medicine or an analgesic, all of which contain two types of active ingredients of polmacoxib and tramadol, and, more specifically, to effects and uses of the active ingredients in a medicine or an analgesic for the treatment of moderate acute and chronic pain caused by inflammatory and multiple factors.
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 9/24 - Layered or laminated unitary dosage forms
The present invention relates to a complex comprising polmacoxib and tramadol. The present invention relates to a pharmaceutical composition and a medicine or an analgesic, all of which contain two types of active ingredients of polmacoxib and tramadol, and, more specifically, to effects and uses of the active ingredients in a medicine or an analgesic for the treatment of moderate acute and chronic pain caused by inflammatory and multiple factors.
A61K 31/135 - Amines, e.g. amantadine having aromatic rings, e.g. methadone
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
26.
PHARMACEUTICALLY ACCEPTABLE SALT OF ALKYLCARBAMOYL NAPHTHALENYLOXY OCTENOYLHYDROXYAMIDE OR OF DERIVATIVE THEREOF AND METHOD FOR PREPARING SAME
The present invention relates to a phosphoric acid salt of alkylcarbamoyl naphthalenyloxy octenoyl hydroxyamide of Formula 1wherein RI is ____________________________________________________________ CH2CH2CH2N(CH3)2. Also described is a method for preparing same. Thedescribed compounds provide improved moisture stability while maintaining the characteristics, such as the efficacy and effective dose. The present invention can simplify the production and manufacturing process of a formulation with improved hygroscopicity.
The present invention relates to a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof and a method for preparing same, and can improve moisture stability while maintaining the characteristics, such as the efficacy and effective dose, of a pharmaceutically acceptable salt of alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide or of a derivative thereof. In addition, the present invention can simplify the production and manufacturing process of a formulation by improving hygroscopicity.
The present disclosure comprises a method for administering 2,3-dihydro-isoindole-1-one compound or a pharmaceutically acceptable salt, ester, solvate and/or prodrug thereof, for the treatment of hematological cancers such as acute myeloid leukemia (AML). The present disclosure further relates to reducing or inhibiting cell-proliferation which is activated by wild-type or mutated Fms-like tyrosine kinase-3 receptor (FLT3). The present disclosure further relates to a method of inhibiting or reducing abnormal (e.g., overexpressed) wild-type or mutated BTK activity or expression in a subject in need thereof.
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Analgesic preparations; pain relief preparations; topical
analgesics; anti-inflammatory preparations;
anti-inflammatory and antipyretic preparations;
anti-inflammatory analgesic preparations; antipyretic
analgesics; preparations for the treatment of arthritis;
preparations for the treatment of osteoarthritis;
preparations for the treatment of enthesitis-related
arthritis; preparations for the treatment of degenerative
arthritis; preparations for the treatment of muscular
rheumatism; preparations for the treatment of rheumatoid
arthritis; preparations for the treatment of musculoskeletal
system disorder; preparations for the treatment of
inflammatory disease or disorder; preparations for the
treatment of soft tissue disorder; pharmaceutical
preparations; pharmaceutical and veterinary preparations;
drugs for medical purposes.
30.
Oral pharmacological composition including 5-{4-(amino sulfonyl)phenyl}-2,2-dimethyl-4-(3-fluorophenyl)-3(2H)-furanone having crystalline structure with excellent stability
(0.9)) of 10 μm to 50 μm, (ii) a pharmaceutically acceptable diluent, and (iii) a pharmaceutically acceptable lubricant. The pharmaceutical composition of the present invention has the advantages of good stability, high dissolution rate, improved content uniformity, and excellent pharmacokinetic properties. Due to these advantages, as a non-steroidal anti-inflammatory drug, the pharmaceutical composition of the present invention may be effective in treating inflammation or pain.
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION (Republic of Korea)
Inventor
Park, Young-Joon
Park, Sang Mi
Cho, Joong Myung
Ro, Seong Gu
Abstract
The present invention relates to a pharmaceutical composition containing a potassium salt of telmisartan, which is an angiotensin II receptor antagonist, and a preparation method therefor. The present invention can provide a granule or powder form of a solid formulation with improved drug dissolution and stability of a telmisartan-containing formulation, and a method for preparing capsules and tablets containing the same. Also, the composition and preparation method according to the present invention are industrially advanced techniques which allow for very easier preparation of telmisartan as a single component or a composite agent combined with other diuretics or high blood pressure-related components compared to a pharmaceutical composition containing telmisartan or salts thereof, thereby achieving significant improvements in terms of production time and cost. The size of a dosage formulation can also be significantly reduced compared to conventional formulations, thereby enhancing medication compliance of patients taking the formulation for a long period of time. In addition, the present invention can provide a composition containing a potassium salt of telmisartan which is capable of significantly improving hygroscopicity of a product, which has been a problem of existing formulations, and maintaining stability in typical packing materials.
The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 233/58 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
34.
PHARMACEUTICAL COMPOSITION INCLUDING 5-{4-(AMINOSULFONYL)PHENYL}-2,2-DIMETHYL-4-(3-FLUOROPHENYL)-3(2H)-FURANONE AND CAPSULE FORMULATION INCLUDING THE PHARMACEUTICAL COMPOSITION
The present invention relates to a pharmaceutical composition including (i) the compound of Formula 1 described in the specification or a pharmaceutically acceptable salt thereof, (ii) a pharmaceutically acceptable diluent, and (iii) a pharmaceutically acceptable lubricant. The compound of Formula 1 or pharmaceutically acceptable salt thereof has a 50% volume particle diameter (d(0.5)) of 3 µm to 9 µm. The pharmaceutical composition of the present invention has the advantages of good stability, high dissolution rate, improved content uniformity, and excellent pharmacokinetic properties. Due to these advantages, the pharmaceutical composition of the present invention is effective in treating inflammation or pain.
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
PHARMACEUTICAL COMPOSITION INCLUDING 5-{4-(AMINOSULFONYL)PHENYL}-2,2-DIMETHYL-4-(3-FLUOROPHENYL)-3(2H)-FURANONE AND CAPSULE FORMULATION INCLUDING THE PHARMACEUTICAL COMPOSITION
The present invention relates to a pharmaceutical composition including (i) the compound of Formula 1 described in the specification or a pharmaceutically acceptable salt thereof, (ii) a pharmaceutically acceptable diluent, and (iii) a pharmaceutically acceptable lubricant. The compound of Formula 1 or pharmaceutically acceptable salt thereof has a 50% volume particle diameter (d(0.5)) of 3 μm to 9 μm. The pharmaceutical composition of the present invention has the advantages of good stability, high dissolution rate, improved content uniformity, and excellent pharmacokinetic properties. Due to these advantages, the pharmaceutical composition of the present invention is effective in treating inflammation or pain.
A61K 31/34 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
A61K 31/255 - Esters, e.g. nitroglycerine, selenocyanates of sulfoxy acids or sulfur analogues thereof
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
The present invention provides a compound selected from the group consisting of a compound of formula (1), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by absormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
37.
2,3-DIHYDRO-ISOINDOLE-1-ON DERIVATIVE AS BTK KINASE SUPPRESSANT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME
The present invention relates to a compound selected from the group consisting of a compound represented by chemical formula 1, a pharmaceutically acceptable salt thereof, an ester, a prodrug, a hydrate, a solvate, and an isomer thereof, to a use of said compound for treating, relieving, or preventing diseases related to the disorder or deregulated activity of a protein kinase, to a pharmaceutical composition comprising the compound as an active ingredient, and to a method for treatment, relief, or prevention using the compound. The compound of the present invention may be effectively used in treating, relieving, or preventing diseases related to the disorder or deregulated activity of a protein kinase.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
KOREA HEALTH INDUSTRY DEVELOPMENT INSTITUTE (Republic of Korea)
Inventor
Hong, Yong Rae
Lee, Mi Jung
Kim, Jeong Mi
Hong, Jang-Won
Chang, Ho Jin
Park, Soobong
Lee, Wheeseong
Choi, Jong-Ryoo
Ro, Seonggu
Cho, Joong Myung
Abstract
The present invention relates to a pharmaceutical composition for the treatment, alleviation or prevention of diseases associated with abnormal or deregulated kinase activity, the composition comprising a compound represented by chemical formula 1 and a pharmaceutically acceptable salt, hydrate, prodrug or solvate thereof. The compound and composition of the present invention inhibit various types of protein kinase activity, and hence can be used to advantage in the treatment, alleviation or prevention of diseases associated with abnormal or deregulated kinase activity.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 209/46 - Iso-indolesHydrogenated iso-indoles with an oxygen atom in position 1
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
The present invention relates to: a novel aminoquinazoline compound having an outstanding inhibiting action against protein-kinase; use of the compound in preventing or treating diseases associated with abnormal cell responses induced by protein-kinase; a pharmaceutical composition comprising the compound; and a treatment method in which the compound is used. The compound of the present invention can be used to advantage in preventing or treating diseases associated with abnormal cell responses induced by protein-kinase.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 37/00 - Drugs for immunological or allergic disorders
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The present invention provides a (di)azaindole derivative represented by the formula (I). A compound of the present invention inhibits a Cdc7 protein kinase activity and suppresses cell proliferation.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
Inventor
Choi, Eun Bok
Lee, Hyeon Kyu
Lee, Eun Sil
Pak, Chwang Siek
Shin, Dong Kyu
Bang, Mi Yeon
Ro, Seonggu
Cho, Joong Myong
Abstract
The present invention relates to a novel benzimidazole compound, a pharmaceutical composition for preventing or treating an inflammatory disease comprising said compound, a use of a novel benzimidazole compound for the manufacture of a medicament for preventing or treating an inflammatory disease, and a method of preventing or treating an inflammatory disease in a mammal comprising administering to the mammal said compound.
Disclosed herein are pyridine derivatives, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylation of HIFα in a subject, modulating expression of HIF-regulated genes in a subject, treating an HIF-related disorder in a subject, increasing levels of endogenous EPO in a subject, or treating a disorder in a subject, using the disclosed compounds.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
Disclosed is a thiazolidinone derivative. More specifically disclosed is a novel compound having a CDC7 inhibitory activity. The thiazolidinone derivative is represented by general formula (I). The compound inhibits the protein kinase activity of CDC7 and suppresses cell growth.
C07D 277/20 - Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 43/00 - Drugs for specific purposes, not provided for in groups
C07D 277/54 - Nitrogen and either oxygen or sulfur atoms
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
44.
Naphthalenyloxypropenyl derivatives having inhibitory activity against histone deacetylase and pharmaceutical composition comprising the same
Korea Research Institute of Chemical Technology (Republic of Korea)
Crystalgenomics, Inc. (Republic of Korea)
Inventor
Lee, Cheol Hae
Jung, Hee Jung
Kim, Jae Hak
Jeong, Won Jang
Cho, Joong Myung
Ro, Seong Gu
Hyun, Young Lan
Lee, Cheol Soon
Shin, Dongkyu
Abstract
The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
A61K 31/165 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/40 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
A61K 31/4468 - Non-condensed piperidines, e.g. piperocaine having a nitrogen atom directly attached in position 4, e.g. clebopride, fentanyl
C07D 295/027 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms containing only hydrogen and carbon atoms in addition to the ring hetero elements containing only one hetero ring
Disclosed herein are hydroxyaryl or hydroxyheteroaryl derivative compounds, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylation of HIFα in a subject, modulating expression of HIF-regulated genes in a subject, treating an HIF -related disorder in a subject, increasing levels of endogenous EPO in a subject, or treating a disorder in a subject, using the disclosed compounds.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
Disclosed herein are pyridine derivatives, or a pharmaceutically acceptable salt, ester, amide, or prodrug thereof, pharmaceutical compositions comprising the same, and methods of modulating the level or activity of HIF in a subject, inhibiting hydroxylation of HIF α in a subject, modulating expression of HIF -regulated genes in a subject, treating an HIF-related disorder in a subject, increasing levels of endogenous EPO in a subject, or treating a disorder in a subject, using the disclosed compounds.
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY of Yonsei University (Republic of Korea)
Inventor
Joo, Yung Hyup
Kang, Seung-Hyun
Hong, Yong Deog
Kim, Yeonjoon
Byoun, Kyounghee
Woo, Byoung Young
Park, Miyoung
Ha, Jun Yong
Koh, Hyunju
Lim, Kyung Min
Kim, Chae-Wook
Lee, Byoung-Seok
Kim, Jung Ju
Jang, Doo Ok
Tae, Jinsung
Shin, Dongkyu
Kim, Yong Eun
Lee, Kyung Ho
Lee, Jae Il
Hyun, Young-Lan
Ro, Seonggu
Cho, Joong Myung
Abstract
The present invention relates to a novel triazine derivative or a pharmaceutically acceptable salt thereof, and an Acetyl-CoA Carboxylase (ACC) comprising same as an active ingredient. The triazine derivative of the present invention effectively inhibits the activity of ACC and it may be used for preventing or treating obesity, diabetes, dyslipidemia and diseases related to metabolic syndrome.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 251/72 - Heterocyclic compounds containing 1,3,5-triazine rings condensed with carbocyclic rings or ring systems
C07D 251/02 - Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
C07D 215/00 - Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
C07D 265/00 - Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
C07D 207/00 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
C07D 221/00 - Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups
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
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
48.
TRIAZOLOPYRIDAZINE DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST ACETYL-COA CARBOXYLASE
INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY (Republic of Korea)
CRYSTALGENOMICS, INC. (Republic of Korea)
Inventor
Hong, Yong Deog
Kang, Seung-Hyun
Kim, Yeonjoon
Byoun, Kyoung Hee
Woo, Byoung Young
Park, Miyoung
Joo, Yung Hyup
Kim, Jung Ju
Jang, Doo Ok
Tae, Jinsung
Shin, Dongkyu
Kim, Yong Eun
Cheon, Younghoon
Lee, Jae Il
Hyun, Young-Lan
Ro, Seonggu
Cho, Joong Myung
Abstract
The present invention relates to a novel triazolopyridazine derivative or a pharmaceutically acceptable salt thereof, and an Acetyl-CoA Carboxylase2 (ACC2) comprising same as an active ingredient. The triazolopyridazine derivative of the present invention effectively inhibits the activity of ACC2 and it may be used for preventing or treating obesity, diabetes, dyslipidemia and diseases related to metabolic syndrome.
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
CRYSTALGENOMICS, INC. (Republic of Korea)
Inventor
Lee, Cheol Hae
Jung, Hee Jung
Kim, Jae Hak
Jeong, Won Jang
Cho, Joong Myung
Ro, Seong Gu
Hyun, Young Lan
Lee, Cheol Soon
Abstract
The present invention discloses novel naphthalenyloxypropenyl derivatives useful for inhibiting the enzyme activity of histone deacetylase, leading effective suppression of cancer cell proliferation.
C07C 233/22 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
C07C 233/16 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
C07C 217/18 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
C07C 217/16 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring not being further substituted
50.
IMIDAZOPYRIDINE DERIVATIVES INHIBITING PROTEIN KINASE ACTIVITY, METHOD FOR THE PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
The inventive imidazopyridine derivative can be used in a pharmaceutical composition for preventing or treating diseases such as diabetes, obesity, dementia, cancer, and inflammation, since it can efficiently inhibit the activities of several protein kinases including glycogen synthase kinase-3 (GSK-3), aurora kinase, extracellular signal-regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions thereof.
A compound of formula 1 efficiently inhibit several protein kinases including glycogen synthase kinase 3 (GSK), aurora kinase, extracellular signal- regulated kinase (ERK), protein kinase B (AKT), and the likes, to control signal transductions involved in variable disorders such as diabetes, obesity, dementia, cancer, and inflammation.
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
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY (Republic of Korea)
CRYSTALGENOMICS, INC. (Republic of Korea)
Inventor
Lee, Cheol Hae
Jung, Hee Jung
Kim, Jae Hak
Jeong, Won Jang
Cho, Joong Myung
Ro, Seonggu
Hyun, Young Lan
Shin, Dongkyu
Lee, Cheol Soon
Abstract
This invention discloses a novel alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide derivative of formula (1) useful for inhibiting the enzyme activity of histone deacetylase, which leads to effective suppression of the cancer cell proliferation, a method for preparing same and a pharmaceutical composition comprising same.
C07C 237/32 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to an acyclic carbon atom of a hydrocarbon radical substituted by oxygen atoms
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/06 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 209/18 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
