Abstract: The present invention relates to a compound having RET kinase inhibiting action or a pharmaceutically acceptable salt thereof, useful in the treatment of diseases such as cancer. In particular a compound represented by the following general formula (I) as defined herein: (I) or a pharmaceutically acceptable salt thereof.

Abstract: The present disclosure provides a method for efficiently producing and providing compounds having a spirooxindole skeleton, for example compounds having a spirooxindole skeleton and having antitumor activity that inhibit the interaction between Mdm2 protein and p53 protein, or intermediates thereof, using an asymmetric catalyst. Compounds having optically active tricyclic dispiroindole skeletons are obtained through catalytic asymmetric 1,3-dipolar cycloaddition reaction using ketimine as a reaction substrate and using a chiral ligand and a Lewis acid.

Abstract: It is an object of the present invention to provide an antibody specifically binding to GPR20-positive tumor cells such as GIST, a pharmaceutical product comprising the antibody and having therapeutic effects on a tumor, a method for treating a tumor using the aforementioned pharmaceutical product, and the like. It is another object of the present invention to provide an anti-GPR20 antibody having internalization activity, an antibody-drug conjugate containing the antibody, and the like.

Abstract: An object of the present invention is to provide a novel anti-CD147 antibody exhibiting potent antitumor efficacy and having excellent safety. Another object of the present invention is to provide a pharmaceutical product comprising such an antibody. Another object of the present invention is to provide a method for treating tumors using the antibody or the pharmaceutical product, for example. The present invention provides a CD147-specific antibody that activates CD147 and exhibits high antitumor efficacy. The present invention provides the anti-CD147 antibody that exhibits high antitumor efficacy independent of effector functions. The present invention provides a pharmaceutical composition comprising such an anti-CD147 antibody. The present invention provides a method for treating tumors using such an anti-CD147 antibody and/or pharmaceutical composition.

Abstract: An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

Abstract: An object of the present invention is to provide a compound having an anti-inflammatory activity or a pharmacologically acceptable salt thereof. The solution of the present invention is a compound of general formula (1) or a pharmacologically acceptable salt thereof. wherein the symbols in the formula are defined below: A: e.g., Benzene, E: e.g., —CH2—, G: e.g., a 5-membered aromatic heterocyclic ring, X: e.g., cyclohexane, J: e.g., a 5-membered aromatic heterocyclic ring, Y: e.g., a phenyl group, R1, R2, R3: e.g., a halogen atom, R4: e.g., a C1-C6 alkyl group, R5: e.g., a hydrogen atom, R6a, R6b, R6c, R6d: e.g., a hydrogen atom, R7: e.g., a hydrogen atom, R8: e.g., a hydrogen atom, n1, n2, n3: e.g., 1.

Abstract: Provided are novel crystals of [2-(1-methyl-1H-pyrazol-4-yl)-6-(morpholin-4-yl)-9H-purin-8-yl][4-(morpholin-4-yl)piperidin-1-yl]methanone and a pharmaceutically acceptable salt thereof having advantageous characteristics. [2-(1-Methyl-1H-pyrazol-4-yl)-6-(morpholin-4-yl)-9H-purin-8-yl][4-(morpholin-4-yl)piperidin-1-yl]methanone and a pharmaceutically acceptable salt thereof provided by the present invention are excellent in stability and have satisfactory physical properties as a drug substance of a pharmaceutical product.

Abstract: An object of the present invention is to provide a medicine that can simply treat and/or prevent a retinal degenerative disease associated with photoreceptor degeneration, including retinitis pigmentosa. The solution is to provide an agent for treating and/or preventing a retinal degenerative disease associated with photoreceptor degeneration, containing a compound having a retinoic acid receptor agonistic activity (for example, tamibarotene, tamibarotene methyl ester, tamibarotene ethyl ester, tazarotene, tazarotenic acid, adapalene, palovarotene, retinol, isotretinoin, alitretinoin, etretinate, acitretin or bexarotene) or a salt thereof.

Abstract: The present invention relates to a terpenoid derivative that has the ability to activate the Keap1/Nrf2/ARE signaling pathway and is excellent in anti-inflammatory action and cytoprotective action, and a sustained-release pharmaceutical composition effective for the treatment and prevention of a posterior eye disease caused by oxidative stress, comprising the terpenoid derivative as an active ingredient. The present invention provides a local administration-type sustained-release pharmaceutical composition for the treatment or prevention of a posterior eye disease, comprising the terpenoid derivative of the present invention as an active ingredient, wherein the sustained-release pharmaceutical composition maintains a pharmacological action thereof for 1 week or longer by the sustained release of the terpenoid derivative under physiological conditions and has a base material administrable to the vitreous body and a form administrable to the vitreous body.

Abstract: Provided is a novel compound or a salt thereof inhibiting MTHFD2 and useful for treating a disease caused by overexpression of MTHFD2, a disease involved in overexpression of MTHFD2 and/or a disease associated with overexpression of MTHFD2. Solution Provided is a sulfonamide derivative having a coumarin skeleton represented by the following formula (I) and having various substituents: wherein R1, R2, R3, R4, R5, R6 and R7 are the same as defined in the specification, and a salt thereof.

Abstract: As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LF-NH—(CH2)n1-La-Lb-Lc- wherein the antibody is connected to the terminal of L1, and the antitumor compound is connected to the terminal of Lc with the nitrogen atom of the amino group at position 1 as a connecting position.

Abstract: The present invention relates to the amelioration of toxic effects that are caused by therapies aimed at FGFR4-inhibition. In particular, the invention relates to the combination of FGFR4 inhibitors and agents capable of reducing bile acid levels and to the use thereof in the treatment of diseases.

Abstract: It has been found that CBP and p300 are in the relationship of synthetic lethality, and treatment inhibiting p300 is a promising approach for the treatment of CBP-mutated cancer. It has also been revealed that this therapeutic strategy achieves efficient treatment based on companion diagnostics because a p300 inhibitor can be administered to a cancer patient selected with functional suppression of CBP as an index.

Abstract: An ophthalmic aqueous composition comprises levofloxacin, a salt thereof, or a solvate thereof; dexamethasone, an ester thereof, or a salt thereof; and one or at least two isotonic agents. The ophthalmic aqueous composition is substantially free of sodium chloride. This ophthalmic aqueous composition is excellent in drug stability and drug migration and has a clear appearance.

Abstract: There is a need for a new antibiotic having a novel mechanism of action, which exhibits strong antibacterial activity not only against sensitive bacteria, but also against resistant bacteria thereof, and at the same time possess excellent solubility and safety profile amenable to human use. As a result of intensive research, the present inventors have found that N-phosphonoxymethyl prodrugs of hydroxyalkyl thiadiazole derivatives represented by general formula (I), a regioisomer, a stereoisomer, or a pharmaceutically acceptable salt thereof possess excellent solubility and safety profile for use in human for the treatment of bacterial infectious diseases.

Abstract: Provided is a novel composition. Provided is a composition for cytotoxic T cell depletion, comprising an anti-LAG-3 antibody or a binding fragment thereof having the properties described in (i) to (iii) below: (i) having in vitro ADCC activity; (ii) reducing, in a low fucose form, the number of LAG-3 positive cells in vivo; and (iii) binding to activated human T cells.

Abstract: The present invention provides a novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, and a novel CLDN6 and/or CLDN9 antibody.

Abstract: The present disclosure provides processes for the preparation of a compound of formula I: or a salt thereof, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.

Abstract: As an antitumor drug which is excellent in terms of antitumor effect and safety, there is provided an antibody-drug conjugate in which an antitumor compound represented by the following formula (I) is conjugated to an antibody via a linker having a structure represented by the following formula: -L1-L2-LP-NH—(CH2)n1-La-Lb-Lc- or -L1-L2-LP- wherein the antibody is connected to the terminal of L1, the antitumor compound is connected to the terminal of Lc or LP, and any one or two or more of linkers of L1, L2, and LP has a hydrophilic structure.

Abstract: The present invention provides a compound represented by the formula (Ia) as a novel cationic lipid that forms a lipid particle and also provides a lipid particle comprising the compound. The present invention further provides a nucleic acid lipid particle containing the lipid particle, and a pharmaceutical composition containing the nucleic acid lipid particle as an active ingredient.