The present invention provides a new means for treating blood cancer by 1) a two-drug combination of a DNA methyl transferase inhibitor and a pharmaceutical composition containing as an active ingredient compound (I), or a pharmaceutically acceptable salt or hydrate thereof, and 2) a three-drug combination of a DNA methyl transferase inhibitor, a BCL-2 inhibitor, and a pharmaceutical composition containing as an active ingredient compound (I), or a pharmaceutically acceptable salt or hydrate thereof.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/7052 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
A61K 31/706 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
The present invention provides a fused-ring amine derivative that has a DYRK inhibitory effect and that is represented by formula (1)
The present invention provides a fused-ring amine derivative that has a DYRK inhibitory effect and that is represented by formula (1)
The present invention provides a fused-ring amine derivative that has a DYRK inhibitory effect and that is represented by formula (1)
(refer to the description with respect to A1, L1, T, Z and l in the formula), or a pharmaceutically acceptable salt thereof.
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 35/15 - Cells of the myeloid line, e.g. granulocytes, basophils, eosinophils, neutrophils, leucocytes, monocytes, macrophages or mast cellsMyeloid precursor cellsAntigen-presenting cells, e.g. dendritic cells
A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
A benzimidazole derivative represented by formula (I) (wherein A1 to A3 and R1 to R6 are as described in the description) or a pharmaceutically acceptable salt thereof, which inhibits activation of STING pathway and, therefore, which is useful as a prophylactic or therapeutic medicine for inflammatory diseases, autoimmune diseases, cancer, etc.
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 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - 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 three or more hetero 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
C07F 7/08 - Compounds having one or more C—Si linkages
Formula (Ia) or a salt thereof, provided by the present invention, is useful as a production intermediate for producing a compound (A) having a BTK inhibitory action.
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
A61K 35/15 - Cells of the myeloid line, e.g. granulocytes, basophils, eosinophils, neutrophils, leucocytes, monocytes, macrophages or mast cellsMyeloid precursor cellsAntigen-presenting cells, e.g. dendritic cells
A61K 35/17 - LymphocytesB-cellsT-cellsNatural killer cellsInterferon-activated or cytokine-activated lymphocytes
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
The present invention provides a thiazole derivative that has an ALK5 inhibitory action and that is represented by formula (1) (refer to the description with respect to R1, R2, and Z in the formula), or a pharmaceutically acceptable salt thereof.
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
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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
Provided is a novel cancer treatment means in which a reversible BTK inhibitor and immunity checkpoint inhibitor are combined. For example, provided is a pharmaceutical composition for treating cancer wherein BTK inhibitor (I-A) and anti PD-1 antibody are combined.
Provided is a novel cancer treatment means in which a reversible BTK inhibitor and immunity checkpoint inhibitor are combined. For example, provided is a pharmaceutical composition for treating cancer wherein BTK inhibitor (I-A) and anti PD-1 antibody are combined.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
The present invention provides an amine derivative having a DYRK-inhibiting activity and represented by formula (1):
The present invention provides an amine derivative having a DYRK-inhibiting activity and represented by formula (1):
The present invention provides an amine derivative having a DYRK-inhibiting activity and represented by formula (1):
wherein A1, A2, L1, L2, X, Z, R1 and R4 are as defined in the description,
or a pharmaceutically acceptable salt thereof.
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
10.
FLUOROISOQUINOLINE COMPOUND AND PRODUCTION METHOD THEREOF
The present invention provides a compound represented by formula (I), a production method thereof, a production intermediate of the same, and a method for producing compound B using the compound (I). Compound B is useful as an intermediate for producing compound A that is a BTK inhibitor.
The present invention provides a compound that has an inhibitory effect on DYRK and that is represented by general formula (I):
The present invention provides a compound that has an inhibitory effect on DYRK and that is represented by general formula (I):
The present invention provides a compound that has an inhibitory effect on DYRK and that is represented by general formula (I):
wherein Q, R1, R2 and R3 are as defined in the description.
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 31/5365 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
Provided herein are novel compounds having an inhibitory effect on the activation of a STING pathway. The provided compounds are 1,2-diaminobenzimidazole derivatives represented by a compound formula (I) or a pharmaceutically acceptable salt thereof: (I) wherein R1, R2, R3, R4, R5, R6, R7, R20, and R21 are defined in the specification.
C07D 401/00 - 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
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
C07D 471/00 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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
This invention provides with a novel means to treat a cancer, in which reversible BTK inhibitor is combined with a BCL-2 inhibitor. Specifically an anticancer agent composition in which a BTK inhibitor below;
This invention provides with a novel means to treat a cancer, in which reversible BTK inhibitor is combined with a BCL-2 inhibitor. Specifically an anticancer agent composition in which a BTK inhibitor below;
This invention provides with a novel means to treat a cancer, in which reversible BTK inhibitor is combined with a BCL-2 inhibitor. Specifically an anticancer agent composition in which a BTK inhibitor below;
is combined with venetoclax.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
Provided herein are novel compounds having an inhibitory effect on the activation of a STING pathway. The provided compounds are 1,2-diaminobenzimidazole derivatives represented by a compound formula (I) or a pharmaceutically acceptable salt thereof:
5 are defined in the specification.
C07D 235/30 - Nitrogen atoms not forming part of a nitro radical
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
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present invention provides a fused-ring amine derivative that has a DYRK inhibiting action and that is represented by formula (1) (refer to the description with respect to A1, L1, T, Z, and I in the formula), or a pharmaceutically acceptable salt thereof.
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
The present invention provides a benzothiazole derivative represented by formula (I) (in the formula, A1, L and Q are as defined in the description) or a pharmaceutically acceptable salt thereof, which exhibits a DYRK inhibitory activity and is useful as a pharmaceutical.
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 5/14 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
A61P 5/16 - Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
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
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61P 25/00 - Drugs for disorders of the nervous 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
Provided herein are novel compounds having an inhibitory effect on the activation of a STING pathway. The provided compounds are 1,2-diaminobenzimidazole derivatives represented by a compound formula (I) or a pharmaceutically acceptable salt thereof: wherein A1, A2, R1, R2, R3, R4, and R5 are defined in the specification.
Provided herein are novel compounds having an inhibitory effect on the activation of a STING pathway. The provided compounds are 1,2-diaminobenzimidazole derivatives represented by a compound formula (I) or a pharmaceutically acceptable salt thereof: wherein A1, A2, R1, R2, R3, R4, and R5 are defined in the specification.
Provided is a novel cancer treatment means in which a reversible BTK inhibitor and an immunity checkpoint inhibitor are combined. For example, provided is a pharmaceutical composition for treating cancer wherein BTK inhibitor (I-A) and an anti PD-1 antibody are combined.
A61P 43/00 - Drugs for specific purposes, not provided for in groups
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
20.
siRNA AND PHARMACEUTICAL COMPOSITION, AND PROPHYLACTIC AND/OR THERAPEUTIC AGENT
[Problem] To provide a pharmaceutical composition containing siRNA, as an active ingredient, that suppresses the BAZF expression. Specifically, the pharmaceutical composition is a prophylactic and/or therapeutic agent that, through suppressing the BAZF expression, prevents and/or treats diseases associated with the VEGF action that promotes neoangiogenesis, e.g., various intraocular neoangiogenesis diseases including diabetic retinopathy such as proliferative diabetic retinopathy, retinopathy of prematurity, retinal branched vein occlusion, central retinal vein occlusion, neovascular glaucoma, neovascular maculopathy, diabetic macular edema, and age-related macular degeneration. [Solution] Provided are: siRNA characterized in that the nucleotide sequence represented by SEQ ID NO: 1 is the target gene sequence; and a pharmaceutical composition that contains the siRNA as an active ingredient.
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseasesGene therapy
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 an amine derivative having a DYRK-inhibiting activity and represented by formula (I) wherein A1, A2, L1, L2, X, Z, R1 and R4 are as defined in the description, or a pharmaceutically acceptable salt thereof.
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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
The present invention provides a compound that has an inhibitory effect on DYRK and is represented by general formula (I) (in the formula, A1, A2, L, R1, and R2 are as described in the specification).
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
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 31/454 - 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 31/4743 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having sulfur as a ring hetero atom
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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
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
C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen
C07F 7/18 - Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
C07F 9/6584 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
The invention of the present application provides an amine derivative having a DYRK-inhibiting activity and represented by formula (1) (see the description with respect to A1, A2, L1, L2, X, Z, R1and R4 in the formula), or a pharmaceutically acceptable salt thereof.
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 19/10 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 25/00 - Drugs for disorders of the nervous 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 43/00 - Drugs for specific purposes, not provided for in groups
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
24.
READILY-SOLUBLE SOLID PHARMACEUTICAL PREPARATION AND PRODUCTION METHOD FOR SAME
The present invention provides: a readily-soluble solid pharmaceutical preparation that is characterized by containing, as a BTK inhibitor, a solid dispersion of a useful 2-(3-{4-amino-6-[(1-methyl-1H-pyrazole-4-yl)amino]-1,3,5-triazine-2-yl}-2-(hydroxymethyl)phenyl)-6-cyclopropyl-8-fluoroisoquinoline-1(2H)-one; and a production method for the readily-soluble solid pharmaceutical preparation.
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
A61K 9/48 - Preparations in capsules, e.g. of gelatin, of chocolate
A benzimidazole derivative represented by formula (I) (wherein A1 to A3 and R1 to R6 are as described in the description) or a pharmaceutically acceptable salt thereof, which inhibits activation of STING pathway and, therefore, which is useful as a prophylactic or therapeutic medicine for inflammatory diseases, autoimmune diseases, cancer, etc.
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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 31/4439 - 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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
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 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 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - 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 three or more hetero rings
A benzimidazole derivative represented by formula (I) (wherein A1to A3and R1to R6 are as described in the description) or a pharmaceutically acceptable salt thereof, which inhibits activation of STING pathway and, therefore, which is useful as a prophylactic or therapeutic medicine for inflammatory diseases, autoimmune diseases, cancer, etc.
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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 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 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
C07D 405/14 - 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 three or more hetero 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
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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 31/4427 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention provides a novel cancer therapeutic means, which is a combination of a reversible BTK inhibitor and a BCL-2 inhibitor. Specifically, provided is an anticancer agent composition obtained by combining, for instance, BTK inhibitor (I-A) and venetoclax.
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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
The present invention provides a compound that has an inhibitory effect on DYRK and that is represented by general formula (I) (in the formula, Q, R1, R2, and R3 are as defined in the description).
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
A61K 31/429 - Thiazoles condensed with heterocyclic ring systems
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
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
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
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I):
wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
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 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
An oxoisoquinoline compound of the following formula:
or a pharmaceutically acceptable salt thereof; a pharmaceutical composition comprising the oxoisoquinoline compound or salt; and a method for treating B-cell lymphoma comprising administering the oxoisoquinoline compound or salt to a patient.
Disclosed is an oxoisoquinoline compound of the formula: or a pharmaceutically acceptable salt thereof. Also disclosed are uses of such compound, for example to prevent or to treat diseases involved in abnormal cell responses through Bruton's tyrosine kinase (BTK), such as self-immune diseases, inflammatory diseases, bone diseases and lymphoma.
In the present invention, an oxoisoquinoline derivative represented by formula (I) (in the formula, Q and R1 are as defined in the description), or a pharmaceutically acceptable salt thereof, is useful as a Bruton's tyrosine kinase inhibitor for treating cancer, B-cell lymphoma, chronic lymphocytic leukemia, and the like.
Herein disclosed are compounds, compositions, kits, and methods of treating cancers using 7-azaindolyl furanone/thiophene derivatives. These derivatives inhibit serine-threonine kinase Cdc7, a recognized anticancer target affecting DNA replication. Further, the compounds disclosed herein possess potent inhibitory activity in the presence of adenosine triphosphate (ATP), demonstrate significant kinase selectivity, and offer advantages over known Cdc7 inhibitors with prolonged half-life and inhibitory effects.
C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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 31/36 - Compounds containing methylenedioxyphenyl groups, e.g. sesamin
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 31/444 - 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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
C07D 407/06 - 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 carbon chain containing only aliphatic carbon atoms
The present invention provides a novel 2,4,6-substituted pyrimidine derivative, which is a compound represented by formula (I) (in the formula, ring A is a 6-membered heteroaryl group having at least one N atom optionally substituted with R1, R2, and R3; Z is an optionally substituted alkoxy group, an optionally substituted amino group, an optionally substituted heterocycloalkyl group, or an optionally substituted heteroaryl group; and R1, R2, and R3 are each independently selected from the group consisting of a hydrogen atom, a halogen atom, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted alkoxy group, an optionally substituted cycloalkyloxy group, an optionally substituted heterocycloalkyloxy group, an optionally substituted phenoxy group, an optionally substituted amino group, a nitro group, and a hydroxy group) or a pharmaceutically acceptable salt thereof.
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I):
wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
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
C07D 498/02 - 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 two hetero rings
C07D 515/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
C07D 513/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
A61K 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4709 - Non-condensed quinolines containing further 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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
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 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
Provided is a pharmaceutical composition comprising a Cdc7 inhibitor and an M phase promoter. In particular, the Cdc7 inhibitor contained in the pharmaceutical composition is a furanone derivative represented by formula (I), or a pharmaceutically acceptable salt thereof. (In the formula, A is —COOR1 or a hydrogen atom; R1 is a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic condensed ring, or an optionally substituted amino group. Alternatively, R2 and R3 may, together with the nitrogen atoms bonding the same, form an optionally substituted heterocycle or optionally substituted heterocyclic condensed ring. R4 is a hydrogen atom or halogen atom. However, if A is —COOR1, R2 and R3 are not both simultaneously optionally substituted amino groups. When A is a hydrogen atom, R3 is a hydrogen atom.)
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
39.
NOVEL HETEROARYL DERIVATIVE HAVING ANTIMALARIAL ACTIVITY
Provided are: a compound that is a novel 2,4,6-substituted triazine derivative and a 2,4,6-substituted pyrimidine derivative, and is expressed by formula (I) (in the formula, A is CH or N, Z is an optionally substituted alkoxy group, an optionally substituted amino group, or the like, and R1, R2, and R3 are each independently a hydrogen atom, a halogen atom, an optionally substituted alkyl group, or the like); or a pharmaceutically-acceptable salt thereof.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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 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 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A61K 31/53 - 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 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
Provided is a pharmaceutical composition comprising a Cdc7 inhibitor and an M phase promoter. In particular, the Cdc7 inhibitor contained in the pharmaceutical composition is a furanone derivative represented by formula (I), or a pharmaceutically acceptable salt thereof. (In the formula, A is -COOR1 or a hydrogen atom; R1 is a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and are each a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic condensed ring, or an optionally substituted amino group. Alternatively, R2 and R3 may, together with the nitrogen atoms bonding the same, form an optionally substituted heterocycle or optionally substituted heterocyclic condensed ring. R4 is a hydrogen atom or halogen atom. However, if A is -COOR1, R2 and R3 are not both simultaneously optionally substituted amino groups. When A is a hydrogen atom, R3 is a hydrogen atom.)
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
The present invention provides a quinazoline derivative represented by formula (I) (in the formula, R1 and R2 represent a hydrogen atom, a halogen atom, or a lower alkyl group optionally having a substituent group, Z represents a cycloakyl group having a substituent group or a cycloalkenyl group having a substituent group, and Q represents a bicyclic heteroaryl group optionally having a substituent group) or a pharmaceutically acceptable salt thereof. The compound has an inhibitory action on the Wnt/β-catenin signaling pathway, and has an antitumor effect, and so is useful as a drug.
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 31/517 - 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 43/00 - Drugs for specific purposes, not provided for in groups
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 417/12 - 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 two hetero rings linked by a chain containing hetero atoms as chain links
[Problem] To provide a novel triazine derivative. [Solution] A triazine derivative or pharmaceutically acceptable salt thereof represented by formula (I). (In the formula: R1 represents a lower alkyl group which may have a substituent group, or an alkoxy group which may have a substituent group; Ar represents an aryl group which may have a substituent group, or a heteroaryl group which may have a substituent group; one of Z1 and Z2 represents a carbon atom, while the other represents a nitrogen atom, or both simultaneously represent nitrogen atoms; Q represents a structure selected from the structure (a) and the structure (b); R2 represents a lower alkyl group which may have a substituent group, or a cycloalkyl group which may have a substituent group; R3 represents a hydrogen atom or a halogen atom; Y represents a nitrogen atom or a carbon atom; and the double line comprising a dotted line and a solid line in the structure (a) represents a double bond or a single bond.)
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
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 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
[Problem] To provide a novel 2,6-diaminopyrimidine derivative. [Solution] A 2,6-diaminopyrimidine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, R1 represents a lower alkyl group which may have a substituent, or an alkoxy group which may have a substituent; Ar represents an aryl group which may have a substituent, or a heteroaryl group which may have a substituent; each of Z1 and Z2 represents a carbon atom, or Z1 and/or Z2 represents a nitrogen atom; Q represents a structure selected from structures (a) and (b); R2 represents a lower alkyl group which may have a substituent, or a cycloalkyl group which may have a substituent; R3 represents a hydrogen atom or a halogen atom; Y represents a nitrogen atom or a carbon atom; and a double line composed of a dashed line and a solid line in structure (a) represents a double bond or a single bond.)
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 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
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
The purpose of the present invention is to provide a novel triazine derivative of the formula (I):(see formula I) whereinR1 represents a substituted or unsubstituted lower alkyl group,R2 represents a hydrogen atom or a substituted or unsubstituted lower alkyl group,A represents a nitrogen atom or C-R3,R3 represents a hydrogen atom, a cyano group, a substituted or unsubstituted acyl group, a substituted or unsubstituted sulfonyl group, or a substituted or unsubstituted carbamoyl group, andR4 represents a substituted or unsubstituted lower alkyl group, or a substituted or unsubstituted cycloalkyl group, or a pharmaceutically acceptable salt thereof.
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 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
The purpose of the present invention is to provide a triazine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, R1 represents a lower alkyl group which may have a substituent; R2 represents a hydrogen atom or a lower alkyl group which may have a substituent; A represents a nitrogen atom or C-R3; R3 represents a hydrogen atom, a cyano group, an acyl group which may have a substituent, a sulfonyl group which may have a substituent or a carbamoyl group which may have a substituent; and R4 represents a lower alkyl group which may have a substituent or a cycloalkyl group which may have a substituent.)
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
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
[Problem] To provide a novel thiazolidinone derivative. [Solution] A thiazolidinone derivative or a pharmaceutically acceptable salt thereof represented by formula (I) or (II). (I) (II)
C07D 417/06 - 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 two hetero rings linked by a carbon chain containing only aliphatic carbon 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
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
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
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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
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 43/00 - Drugs for specific purposes, not provided for in groups
To provide a novel furanone derivative, and a medicine including the same. The furanone derivative is represented by the formula (I):
wherein A represents —COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group, or an optionally substituted heterocycle; R2 and R3 are the same or different and each independently represent a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocycle, an optionally substituted heterocyclic fused ring, or an optionally substituted amino group; or alternatively, R2 and R3, taken together with the nitrogen atom to which they are attached, may form an optionally substituted heterocycle or an optionally substituted heterocyclic fused ring; and R4 represents a hydrogen atom or a halogen atom; with the proviso that when A represents —COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.
C07D 471/02 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed system contains two hetero rings
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
C07D 498/02 - 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 two hetero rings
C07D 513/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
C07D 515/02 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups , or in which the condensed system contains two hetero rings
The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.
C07D 417/12 - 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 two hetero rings linked by a chain containing hetero atoms as chain links
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
C07D 277/56 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
[Problem] To provide a novel 1,2,4-triazine derivative. [Solution] A 1,2,4-triazine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, R1 represents an aryl group which may have a substituent, a heterocyclic ring which may have a substituent, or a heterocyclic condensed ring which may have a substituent; R2 represents a hydrogen atom, a halogen atom, or a lower alkyl group which may have a substituent; R3 represents an aryl group which may have a substituent, a heterocyclic ring which may have a substituent, or a heterocyclic condensed ring which may have a substituent; and R4 represents a hydrogen atom or a lower alkyl group which may have a substituent, or R4 and R1 may together form a bond to form a saturated or unsaturated 5- to 6-membered ring which may have a substituent, thereby forming a polycyclic condensed ring.)
C07D 401/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 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
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
[Problem] To provide a novel triazine derivative. [Solution] A triazine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, R1 represents an optionally substituted aryl group, an optionally substituted heterocyclic ring, an optionally substituted heterocyclic fused ring or an optionally substituted alkynyl group; R2 represents a hydrogen atom, a halogen atom, an optionally substituted lower alkyl group or an optionally substituted alkoxy group; R3 represents an optionally substituted aryl group, an optionally substituted heterocyclic ring or an optionally substituted heterocyclic fused ring; R4 represents a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted alkoxy group, an optionally substituted amino group or a halogen atom; and R5 represents a hydrogen atom or an optionally substituted lower alkyl group, or alternatively, R5 may combine with R1 and form an optionally substituted, five- or six-membered, saturated or unsaturated ring, thereby forming a polycyclic fused ring.)
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
[Problem] To provide a novel furanone derivative and a pharmaceutical product composed of the furanone derivative. [Solution] A compound represented by formula (I). (In the formula, A represents -COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic ring; R2 and R3 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocyclic ring, an optionally substituted heterocyclic fused ring or an optionally substituted amino group, or alternatively, R2 and R3 may form an optionally substituted heterocyclic ring or an optionally substituted heterocyclic fused ring together with a nitrogen atom to which R2 and R3 are bonded; and R4 represents a hydrogen atom or a halogen atom. In this connection, when A represents -COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.)
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 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
A61K 31/541 - Non-condensed thiazines containing further 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
[Problem] To provide a novel furanone derivative and a pharmaceutical product composed of the furanone derivative. [Solution] A compound represented by formula (I). (In the formula, A represents -COOR1 or a hydrogen atom; R1 represents a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic ring; R2 and R3 may be the same or different and each represents a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted phenyl group, an optionally substituted heterocyclic ring, an optionally substituted heterocyclic fused ring or an optionally substituted amino group, or alternatively, R2 and R3 may form an optionally substituted heterocyclic ring or an optionally substituted heterocyclic fused ring together with a nitrogen atom to which R2 and R3 are bonded; and R4 represents a hydrogen atom or a halogen atom. In this connection, when A represents -COOR1, R2 and R3 are not optionally substituted amino groups at the same time, and when A represents a hydrogen atom, R3 represents a hydrogen atom.)
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 31/4375 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
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 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5355 - Non-condensed oxazines containing further heterocyclic rings
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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
The present invention relates to Traf2- and Nck-interacting kinase (TNIK) inhibitors, pharmaceutical compositions, and methods for the treatment of cancer patients with TNIK inhibitors. And the present invention relates to a novel aminothiazole derivatives. The TNIK inhibitors are showed by a next formula (I). (I) Wherein R1, R2, R3, R4, R5 and R6 represent independently a hydrogen atom or a substituent group.
[PROBLEMS] To provide a method of screening a preventive or remedy for type I dipolar disorder by using a type I dipolar disorder-specialized disease model. [MEANS FOR SOLVING PROBLEMS] A method of screening a preventive or remedy for type I dipolar disorder characterized in that a disease model of type I dipolar disorder, which comprises a nonhuman animal deficient in the DGKβ function, is employed.
Disclosed is a compound represented by the formula (I) below, which is useful as a protein kinase inhibitor. (In the formula, R1 represents a lower alkyl group which may be substituted by a halogen atom, a halogen atom or the like; R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; and X, Y and Z independently represent a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like, or alternatively, X and Y combine together to form an optionally substituted 5-membered or 6-membered ring, thereby forming a bicyclic fused ring.)
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 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 25/00 - Drugs for disorders of the nervous 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 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 43/00 - Drugs for specific purposes, not provided for in groups
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 405/12 - 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 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 417/12 - 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 two hetero rings linked by a chain containing hetero atoms as chain links
57.
ANIMAL MODEL OF SCHIZOPHRENIA OR COGNITIVE IMPAIRMENT, SCREENING METHOD USING THE SAME AND PREVENTIVE OR THERAPEUTIC AGENT FOR SCHIZOPHRENIA OR COGNITIVE IMPAIRMENT
It is intended to provide an animal model which can develop schizophrenia or cognitive impairment more naturally without using a low molecular weight drug; a screening method for a preventive or therapeutic agent for schizophrenia or cognitive impairment using the animal model; and a preventive or therapeutic agent for schizophrenia or cognitive impairment. The animal model of schizophrenia or cognitive impairment comprising a nonhuman animal treated so as to reduce the expression level of a cell membrane-bound growth factor is developed and the preventive or therapeutic agent for schizophrenia or cognitive impairment is provided by utilizing the animal model for screening. In particular, the animal model is an animal model of schizophrenia or cognitive impairment in which the whole or a part of a sequence encoding a heparin-bound EGF-like growth factor has been deleted from a gene which can be expressed in vivo such that the factor is selectively reduced in the brain. Further, the preventive or therapeutic agent contains a substance that promotes signal transduction of a cell membrane-bound growth factor to a cell.
A01K 67/027 - New or modified breeds of vertebrates
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 25/00 - Drugs for disorders of the nervous 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
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Peptide; polypeptide; protein; chemical reagents other than
for medical or veterinary purposes; ferments for chemical
purposes. Chemical reagents for medical or veterinary purposes;
chemical preparations for medical purposes; chemical
preparations for pharmaceutical purposes; diagnostic
preparations for medical purposes; drugs for medical
purposes; medicines for human purposes; organotherapy
preparations; pharmaceutical preparations; serotherapeutic
medicines; pharmaceutical preparations for skin care;
biological preparations for medical purposes. Bacteriological research; biological research; chemical
analysis; chemical research; chemistry services; cosmetic
research; research and development for others; biological
research; mechanical research; calibration measuring;
biological or chemical research consultancy.
01 - Chemical and biological materials for industrial, scientific and agricultural use
05 - Pharmaceutical, veterinary and sanitary products
42 - Scientific, technological and industrial services, research and design
Goods & Services
Peptide for in vitro research use and for scientific and medical research; polypeptide for in vitro research use and for scientific and medical research; protein for in vitro research use and for scientific and medical research; chemical reagents for non-medical purposes and non-veterinary purposes; and ferments for in vitro research use and for scientific and medical research Chemical reagents for medical or veterinary purposes [; chemical preparations for medical purposes; chemical preparations for pharmaceutical purposes; diagnostic preparations for medical purposes; drugs for medical purposes for the treatment of cancer, inflammation, dermal diseases, heart diseases, respiratory diseases and disorders, gastrointestinal diseases, infectious diseases, bone diseases, circulatory disease, cerebral diseases and articular rheumatism; medicines for human purposes for the treatment of cancer, inflammation, dermal diseases, heart diseases, respiratory diseases and disorders, gastrointestinal diseases, infectious diseases, bone diseases, circulatory disease, cerebral diseases and articular rheumatism; organotherapy preparations for the treatment of cancer, inflammation, dermal diseases, heart diseases, respiratory diseases and disorders, gastrointestinal diseases, infectious diseases, bone diseases, circulatory disease, cerebral diseases and articular rheumatism; pharmaceutical preparations for the treatment of cancer, inflammation, dermal diseases, heart diseases, respiratory diseases and disorders, gastrointestinal diseases, infectious diseases, bone diseases, circulatory disease, cerebral diseases and articular rheumatism; serotherapeutic medicines for the treatment of cancer, inflammation, dermal diseases, heart diseases, respiratory diseases and disorders, gastrointestinal diseases, infectious diseases, bone diseases, circulatory disease, cerebral diseases and articular rheumatism; pharmaceutical preparations for skin care; biological preparations for medical purposes; and ferments for medical or veterinary use ] [ Bacteriological research; ] biological research; [ chemical analysis; chemical research; chemistry services; cosmetic research; mechanical research; calibration measuring; and ] biological or chemical research consultancy
