Heterocyclic Compounds

Matches 551 - 600 out of 1,226	< 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 >

Document	Document Title
JP6417403B2	ACC inhibitor and its use The present invention provides for compounds of formula I as acetyl-CoA carboxylase (ACC) inhibitors. The ACC inhibitors are useful for the prevention or treatment of metabolic syndrome, including obesity, dyslipidemia and hyperlipidemia...
JP2018154614A	ANTIBODIES TO OPGL To provide antibodies that bind an osteoprotegerin ligand (OPGL) for treatment of bone diseases, such as osteoporosis, bone loss from arthritis, Paget's disease, and osteopenia.An antibody comprises an H chain comprising an amino acid se...
JP2018527360A	Modified Cytotoxicity and Its Therapeutic Use To widely provide a compound useful for treating cancer. In some embodiments, the invention provides a low molecular weight cytotoxic agent that has been chemically modified to include one or more moieties, such as a hydrophobic moiety. ...
JP2018525412A	Deuterated toll-like receptor regulator The present invention provides deuterated analogs of Toll-like receptor regulator compounds having a structure of formula (X) or (Y), processes for making analogs thereof, and therapeutic uses thereof. To do. The present invention is, fo...
JP6386467B2	A novel heterocyclic derivative as a modulator of kinase activity in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
JP2018135389A	DNA-PK INHIBITOR To provide a DNA-PK inhibitor.There is provided a compound (I) useful as a DNA-PK inhibitor. There are provided a pharmaceutically acceptable composition containing the compound, and a method using the compound in treatment of various di...
JP2018123058A	DIFLUOROMETHYLENE COMPOUND To provide a plant disease control agent that exhibits a high controlling effect on a wide range of plant pathogenic bacteria.The present invention provides a compound represented by formula (I)[where each symbol has the same meaning as ...
JP6360878B2	DNA-PK inhibitor The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various d...
JP6282759B2	The compound as a modulator of ROR gamma The present invention encompasses compounds of the formula (I) wherein the variables are defined herein which are suitable for the modulation of RORy and the treatment of diseases related to the modulation of RORy. The present invention ...
JP6280130B2	The new imidazole piperidinyl derivative as a modulator of kinase activity The invention provides novel imidazol-piperidinyl derivatives of formula (I) in which R 1 , R 2 , X 1 , X 2 , X 3 , X 4 and n have the meanings indicated in above, and their manufacture and use for the treatment of hyperproliferative dis...
JP6270981B2	Manufacture of an amino acid connection machine by which conjugate was carried out to a compound used for target type imaging of a tumor, and a composite method The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule t...
JP6198814B2	The folic acid / folic acid metabolic antagonist family object by which 18F sign was carried out The present invention is directed towards new 18F-folate/antifolate analog radiopharmaceuticals, wherein the phenyl group within folate structures has been replaced by an 18F-heterocycle, their precursors, a method of their preparation, ...
JP2017525711A	Novel N2, N4, N7,6-tetrasubstituted pteridine-2,4,7-triamine and 2,4,6,7-tetra-substituted pteridine compounds and their synthetic methods and uses Compounds as immune system regulators with pteridine nuclei are described. A pharmaceutical composition containing this, a method for producing the same, and a method for treating or preventing an autoimmune disease using the same are de...
JP2017525759A	Dihydropteridinone derivatives and their use The present disclosure provides a compound represented by the formula (I) and a pharmaceutical composition thereof. The compound of formula (I) was found to bind bromodomain and / or bromodomain-containing proteins (eg, bromo and specifi...
JP6192799B2	Composition and a constituent of an amino acid connection machine which are carrying out conjugate to a compound used for target imaging of a tumor The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule t...
JP2017149753A	SUBSTITUTED AMINOTHIAZOLE AS INHIBITOR OF CANCER, INCLUDING HEPATOCELLULAR CARCINOMA, AND AS INHIBITOR OF HEPATITIS VIRUS REPLICATION To provide a therapeutic agent for a cancer including hepatocellular carcinoma, and a viral infection by a hepatitis virus.There is provided a compound represented by Formula (1), and a hydrate, a solvate, a pharmaceutically acceptable s...
JP2017149776A	SYNTHESIS AND COMPOSITION OF AMINO ACID LINKING GROUP CONJUGATED TO COMPOUND USED FOR THE TARGETED IMAGING OF TUMOR To provide a method of synthesizing and utilizing an amino acid linking group that is conjugated to a compound used for the targeted imaging of a tumor.The present disclosure relates to a compound that is useful as a near-infrared fluore...
JP6166736B2	How to manufacture the crystal form of (6S) -5-methyl tetrahydrofolic acid salt, and it Disclosed are a crystal form of (6S)-5-methyltetrahydrofolate salt and a method for preparing the same. The crystal form is: Form C of the crystal form of (6S)-5-methyltetrahydrofolate calcium salt, where the X-ray diffraction pattern ha...
JP6157455B2	Nitrogen-containing heterocyclic compound The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound re...
JP6152104B2	Horat conjugate of albumin joint substance The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method o...
JP2017512831A	Pharmaceutical formulation comprising substituted phenyl- (1,3-dihydro-isoindole-2-yl) -methanone Equation (I):(2,4-dihydroxy-5-isopropyl-phenyl)-[5- (4-methyl-piperazin-1-ylmethyl) -1,3-dihydro-isoindole-2-yl] -methanone, or its L- Formulations of lactate in phosphate buffers or succinic acid buffers are provided herein.
JP6134441B2	Ethynyl derivative It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsess...
JP2017512186A	Dihydropteridinone derivatives and their use The present invention provides a compound represented by the formula (I) and a pharmaceutical composition thereof. The compound of formula (I) is believed to be a binder for bromodomain and / or bromodomain-containing proteins (eg, bromo...
JP6114820B2	A Pteridinone derivative, EGFR, BLK, application as inhibitor of FLT3 Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the f...
JPWO2015125892A1	Protein labeling compound The present invention has the general formula (I) [formulation 1]. (In the formula, Z is [Chemical 2]Is shown. Y1Is N or CR1Indicates, Y2Is N or CR2Indicates, Y3Is N or CR3Indicates, Y4Is N or CR4Is shown, and R in these equations1~ R4On...
JP6104377B2	Inhibitor of a fibroblast growth factor receptor Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
JP6093759B2	A new immunity system regulation agent or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
JP6084967B2	A manufacturing process of sepia pterin and tetrahydro Lactoyl pterin To provide a method for producing sepiapterin, lactoylpterin or tetrahydrolactoylpterin. Sepiapterin, lactoylpterin and tetrahydrolactoylpterin are produced at high yield through the following reaction scheme.
JP6072308B2	Dihydro Pteridinone II The present invention relates to spiroheterocycl-dihydropyhmidines, their use as modulators of γ-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which int...
JP6057947B2	A constituent and a method of lowering the side effects and toxicity by prescribing methotrexate for the patient as an orotic acid derivative This invention is in the field of chemical restructuring of antimetabolite agents known to have poor oral bioavailability and to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concer...
JP2016216464A	ANTIBODIES TO OPGL To provide molecules which can control the activity of an osteoprotegerin ligand (OPGL) in the therapy of osteopenia.The invention relates to an antibody that interacts with OPGL and inhibits osteoclastic differentiation and the binding ...
JP6027610B2	A heterocyclic compound and its use Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, incl...
JP2016525532A	Treatment of myelodysplastic syndrome The present invention relates to the use of boraceltib or a pharmaceutically acceptable salt thereof or a hydrate thereof for the treatment of myelodysplastic syndrome (MDS).
JP5972867B2	A preparing method of a pteridine derivative
JP5942133B2	A fluorescent probe and an enzyme activity detecting method using this
JP5937087B2	How to manufacture dihydro Pteridinone and its intermediate The present invention relates to an improved process for manufacturing dihydropteridinones of general formula (12) as well as intermediates thereof, wherein the groups R1, R2, R3, R4, and R5 have the meanings given in the claims and spec...
JP5925381B2	Compound [4- (2-amino-10-methyl-4-oxo-6,7,8,9-tetrahydro-4a,7-epiminopyrimid [4,5-b] [1,4] diazepine-5 (4H)) -Il) Benzoyl] -Glutamate and its manufacture The present invention relates to the compound [4-(2-amino-10-methyl-4-oxo-6,7,8,9-tetrahydro-4a,7-cycloimi no-pyrimido[4,5-b] [1,4] diazepine-5(4H)-yl)benzoyl]-glutamate (JK12A for short) with the structure of Formula I. The present inve...
JP5916040B2	A constituent and a method of lowering the side effects and toxicity by prescribing methotrexate for the patient as an orotic acid derivative This invention is in the field of chemical restructuring of antimetabolite agents known to have poor oral bioavailability and to cause tissue toxicity as a side effect, by producing their orotate derivatives. More particularly, it concer...
JP5876527B2	Diagnostic images and radiotherapy folic acid complexes and corresponding metal chelate complexes The invention further contemplates the corresponding metal-chelate complexes as well as pharmaceutical compositions thereof, and their uses in diagnostic imaging and radiotherapy.
JP2016006111A	OPTICALLY PURE DIASTEREOMER OF 10-PROPARGYL-10-DEAZA AMINOPTERIN, AND METHOD OF USING THE SAME To provide a compound that is useful for the treatment of cancer and inflammatory disorder, and a pharmaceutical composition that contains the compound.Provided is: a compound comprising a substantially pure diastereomer of 10-propargyl-...
JP5841548B2	Dihydropteridinone, its manufacturing method and use The present invention relates to new dihydropteridinones of general formula (12) wherein the groups R1 to R5 and L, n, and m have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihy...
JP5802670B2	Their use as pteridine and pesticides The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and 1- or 2-(4-(heteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products.
JP5785622B2	A novel method for producing a folic acid antagonist having a glutamate moiety in its structure A method for producing antifolate agents having glutamic acid part in their structure is developed by protecting carboxyl groups of glutamic acid or its N-substituted derivatives as cyanomethyl ester to give compounds of formula (II) whi...
JP5781026B2	Ethylene dicysteine (EC) -drug conjugate The invention provides a conjugate comprising ethylenedicysteine (EC) conjugated to neomycin.
JP5767642B2	Dihydropteridinone derivative, its manufacturing method and pharmaceutical use Dihydroperidinone derivatives, preparation process and pharmaceutical use thereof are disclosed. Specially, new dihydroperidinone derivatives represented by general formula (I), wherein each substituent of the general formula (I) is defi...
JP2015110567A	STABLE COMPLEX OF ALKALINE EARTH METAL SALT OF N5-METHYL-TETRAHYDROFOLIC ACID AND POLYOL To provide a stable complex of an alkaline earth metal salt of (6RS)- or (6S)-N-methyl-(5,6,7,8)-tetrahydrofolic acid and a polyol, and a method for producing the same.There is provided a complex of an alkaline earth metal salt of N meth...
JP5710246B2	Diagnostic images and radiotherapy folic acid complexes and corresponding metal chelate complexes The invention further contemplates the corresponding metal-chelate complexes as well as pharmaceutical compositions thereof, and their uses in diagnostic imaging and radiotherapy.
JP2015078229A	NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS To provide lipids-therapeutic nucleic acid compositions useful for general therapeutic use.The present invention provides novel cationic lipids and lipid particles comprising the same. The lipid particles can further comprise active phar...
JP2015078205A	ANTIBODIES TO OPGL To provide a pharmaceutical composition for treating bone loss by binding to an osteoprotegerin ligand (OPGL).The invention provides a pharmaceutical composition for treatment of bone loss which contains an antibody containing H chain an...
JP5706926B2	A compound comprising a moiety for recognition of a biological target, coupled to a signal moiety capable of complexing with gallium. The invention concerns compounds comprising a biological target recognizing part, coupled to a signal part capable of complexing gallium. The invention also concerns methods for obtaining said compounds, screening methods capable of sele...

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