A galactoside compound of Formula (I) is disclosed. The galactoside compound of Formula (I) has the effect of inhibiting galectin-3 by having a structure in which a spiro ring is fused to C1, and appropriate substituents at other carbon positions. Therefore, the galactoside compound and a pharmaceutical composition containing the galactoside compound are effective in the prevention or treatment of diseases or disorders such as galectin-3-related fibrosis and cancer.
A galactoside compound of Formula (I) is disclosed. The galactoside compound of Formula (I) has the effect of inhibiting galectin-3 by having a structure in which a spiro ring is fused to C1, and appropriate substituents at other carbon positions. Therefore, the galactoside compound and a pharmaceutical composition containing the galactoside compound are effective in the prevention or treatment of diseases or disorders such as galectin-3-related fibrosis and cancer.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
C07H 19/01 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof sharing oxygen
C07H 19/24 - Heterocyclic radicals containing oxygen or sulfur as ring hetero atom
2.
COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
The present invention provides: a novel compound inhibiting the activity of bromodomain, a solvate thereof, a hydrate thereof, a prodrug thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition comprising same, and is very useful for preventing and treating diseases and disorders responding to the inhibition of bromodomain-containing proteins.
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
A61K 31/422 - Oxazoles 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 31/4365 - 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 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
According to an aspect of the technology disclosed by the present application, the present invention relates to a pharmaceutical composition for preventing or treating a tumor, including a low-molecular kinase inhibitor which blocks the signaling pathway of transforming growth factor-β (TGF-β), in which, by administration of the low-molecular kinase that blocks the TGF-β signaling pathway, in combination with at least one of an immune checkpoint regulator and a receptor tyrosine kinase inhibitor, a tumor therapeutic or tumor growth inhibitory effect is excellent in a patient who needs tumor therapy or tumor growth inhibition, compared to when the low-molecular kinase inhibitor, immune checkpoint regulator, or receptor tyrosine kinase inhibitor is administered alone.
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
4.
PYRAZOLOPYRIMIDINE DERIVATIVE AS CYCLIN-DEPENDENT KINASE 9 INHIBITOR
The novel pyrazolopyrimidine derivative represented by the chemical formula (I) of the present invention is effective as a CDK9 inhibitor. The pharmaceutical composition containing the derivative is useful for preventing or treating diseases or disorders mediated by CDK9, such as cancer, inflammation, and fibrosis.
According to an aspect of the technology disclosed by the present application, the present invention relates to a pharmaceutical composition for preventing or treating a tumor, including a low-molecular kinase inhibitor which blocks the signaling pathway of transforming growth factor-ß (TGF-ß), in which, by administration of the low-molecular kinase that blocks the TGF-ß signaling pathway, in combination with at least one of an immune checkpoint regulator and a receptor tyrosine kinase inhibitor, a tumor therapeutic or tumor growth inhibitory effect is excellent in a patient who needs tumor therapy or tumor growth inhibition, compared to when the low-molecular kinase inhibitor, immune checkpoint regulator, or receptor tyrosine kinase inhibitor is administered alone.
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
According to an aspect of the technology disclosed by the present application, the present invention relates to a pharmaceutical composition for preventing or treating a tumor, including a low-molecular kinase inhibitor which blocks the signaling pathway of transforming growth factor-β (TGF-β), in which, by administration of the low-molecular kinase that blocks the TGF-β signaling pathway, in combination with at least one of an immune checkpoint regulator and a receptor tyrosine kinase inhibitor, a tumor therapeutic or tumor growth inhibitory effect is excellent in a patient who needs tumor therapy or tumor growth inhibition, compared to when the low-molecular kinase inhibitor, immune checkpoint regulator, or receptor tyrosine kinase inhibitor is administered alone.
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A galactoside derivative according to the present invention has the effect of inhibiting galectin-3 by having a structure in which a spiro ring is fused to C1, and appropriate substituents at other carbon positions. Therefore, the galactoside derivative of the present invention and a pharmaceutical composition comprising same are effective in the prevention or treatment of diseases or disorders such as galectin-3-related fibrosis and cancer.
A61K 31/7048 - Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
C07H 19/01 - Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radicalNucleosidesMononucleotidesAnhydro derivatives thereof sharing oxygen
A galactoside derivative according to the present invention has the effect of inhibiting galectin-3 by having a structure in which a spiro ring is fused to C1, and appropriate substituents at other carbon positions. Therefore, the galactoside derivative of the present invention and a pharmaceutical composition comprising same are effective in the prevention or treatment of diseases or disorders such as galectin-3-related fibrosis and cancer.
A61K 31/7056 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
Salts and crystalline forms of (R)-4-((2-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-2,4-dioxo-1′-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-spiro[furo[3,4-d]pyrimidine-5,4′-piperidine]-3(2H,4H,7H)-yl)-1-phenylethyl)amino)butanoic acid (formula (1)) show excellent physicochemical properties including, for example, hygroscopicity, related substances, chemical stability. The salts and crystalline forms are useful and suitable for pharmaceutical uses such as the preparation of a pharmaceutical composition containing the same as an active ingredient.
Salts and crystalline forms of the compound of chemical formula 1, that is, (R)-4-((2-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-2,4-dioxo-1'-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-spiro[puro[3,4-d]pyrimidine-5,4'-piperidine]-3(2H,4H,7H)-yl)-1-phenylethyl)amino)butanoic acid according to the present invention are excellent in terms of general physicochemical properties, e.g., hygroscopicity, related substances, chemical stability, etc. and as such, can be utilized for pharmaceutical uses, such as the preparation of a pharmaceutical composition comprising same as an active ingredient.
C07D 498/12 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
11.
SALT AND CRYSTALLINE FORM OF FUROPYRIMIDINE COMPOUND AND PHARMACEUTICAL USE THEREOF
Salts and crystalline forms of the compound of chemical formula 1, that is, (R)-4-((2-(1-(2-fluoro-6-(trifluoromethyl)benzyl)-2,4-dioxo-1'-((5-(trifluoromethyl)furan-2-yl)methyl)-1H-spiro[furo[3,4-d]pyrimidine-5,4'-piperidine]-3(2H,4H,7H)-yl)-1-phenylethyl)amino)butanoic acid according to the present invention are excellent in terms of general physicochemical properties, e.g., hygroscopicity, related substances, chemical stability, etc. and as such, can be utilized for pharmaceutical uses, such as the preparation of a pharmaceutical composition comprising same as an active ingredient.
C07D 498/12 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
12.
Pharmaceutical composition with improved stability containing factor VII fusion protein
The present invention provides a pharmaceutical composition with improved stability, comprising a fusion protein comprising Factor VII (FVII) and transferrin, as an active ingredient, wherein the transferrin is linked to the C-terminus of the FVII; and trehalose or glycine as a bulking agent. The composition can store FVII and a variant thereof stably at room temperature for a long period of time. Thus it can be used as a useful therapeutic agent for patients suffering from hemophilia or congenital FVII deficiency.
A fusion protein comprising factor VII (FVII) and transferrin according to the present invention has an improved specific activity of FVII compared to existing FVII fusion proteins comprising other fusion partners than transferrin, and thus can be effectively used in a therapy using FVII.
The present invention relates to: a compound selected from the group consisting of a tricyclic compound having the structure of formula I, a pharmaceutically acceptable salt, an isomer, a solvate and a precursor thereof; and a use thereof. The compound effectively controls GPR40, and thus, can be effectively used for the prophylaxis or treatment of diseases associated with GPR40, for example, diabetes and many other diseases.
C07D 307/80 - Radicals substituted by oxygen atoms
C07D 313/10 - Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
C07D 335/02 - Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
C07D 405/12 - 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 chain containing hetero atoms as chain links
C07D 239/70 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
C07C 317/18 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to acyclic carbon atoms of the carbon skeleton
C07C 229/46 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino or carboxyl groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
C07C 59/72 - Unsaturated compounds containing ether groups, groups, groups, or groups containing six-membered aromatic rings and other rings
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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 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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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
15.
Gonadotropin releasing hormone receptor antagonists, method for the preparation thereof and pharmaceutical composition comprising the same
Disclosed are a gonadotropin releasing hormone receptor antagonist and a pharmaceutical composition including the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid-dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.
A61P 5/04 - Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin for decreasing, blocking or antagonising the activity of the hypothalamic hormones
A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
ABS TRACT The present invention relates to a compound selected from the group consisting of a tricyclic compound having the structure of formula I, R5 X 0 R44.( R3 n W y R2 R7 R1 V a pharmaceutically acceptable salt, a stereoisomer and a solvate thereof; and use thereof. The compound effectively controls GPR40, and thus, can be effectively used for the prophylaxis or treatment of diseases associated with GPR40, for example, diabetes and many other diseases. Date Recue/Date Received 2020-06-02
C07D 307/80 - Radicals substituted by oxygen atoms
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
C07D 313/10 - Seven-membered rings condensed with carbocyclic rings or ring systems condensed with two six-membered rings
Disclosed is a fusion protein comprising blood coagulation factor IX (FIX) and transferrin. The fusion protein exhibits improved specific FIX activity, as compared to native FIX, and can be useful in the treatment of FIX deficiency-associated diseases.
A fusion protein comprising factor VII (FVII) and transferrin according to the present invention has an improved specific activity of FVII compared to existing FVII fusion proteins comprising other fusion partners than transferrin, and thus can be effectively used in a therapy using FVII.
The present invention provides gonadotropin releasing hormone receptor antagonists of Formula (I) and the pharmaceutical composition comprising the same, which can be useful in preventing or treating a sex hormone-related disease such as endometriosis, amenorrhea, irregular menstruation, uterine myoma, uterine fibroids, polycystic ovarian disease, lupus erythematous, hypertrichosis, precocious puberty, short stature, acne, alopecia, gonadal steroid- dependent neoplasms, gonadotropin-producing pituitary adenoma, sleep apnea, irritable bowel syndrome, premenstrual syndrome, benign prostatic hyperplasia, contraception, and infertility, as well as Alzheimer disease.
C07D 491/02 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains two hetero rings
A61K 31/527 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
The present invention relates to a 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-.beta. (TGF-.beta.) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
21.
2-pyridyl substituted imidazoles as ALK5 and/or ALK4 inhibitors
The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-β (TGF-β) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
Disclosed is a fusion protein comprising blood coagulation factor IX (FIX) and transferrin. The fusion protein exhibits improved specific FIX activity, as compared to native FIX, and can be useful in the treatment of FIX deficiency-associated diseases.
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A fusion protein comprising factor VII (FVII) and transferrin according to the present invention has an improved specific activity of FVII compared to existing FVII fusion proteins comprising other fusion partners than transferrin, and thus can be effectively used in a therapy using FVII.
patents
