Abstract: This invention relates to a method for producing a high-purity cyclohexenone long-chain alcohol represented by formula I, and produces the compound of formula I by a metal-mediated Barbier reaction. The method of the present invention has advantages in its short scheme, high yield, and high-purity product, and is suitable for industrial scale up.

Abstract: The present invention provides a compound represented by Formula (I) or a salt thereof; an LSD1 inhibitor that contains the compound or a salt thereof as an active ingredient; a pharmaceutical composition that contains the compound or a salt thereof; and an antitumor agent that contains the compound or a salt thereof as an active ingredient.

Abstract: The invention provides new pyrazine derivatives of formula (I): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the substituents are as defined herein. The invention also provides pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Abstract: Provided is a novel method for treating cancer with a high antitumor effect. The present invention provides an antitumor agent comprising an azabicyclo compound of the following Formula (I) or a salt thereof and a poly(adenosine 5?-diphosphate-ribose) polymerase inhibitor which are administered in combination.

Abstract: There is provided a novel phosphate ester compound having a pyrrolopyrimidine skeleton having an excellent antitumor effect or a pharmaceutically acceptable salt thereof, and a method for preventing and/or treating a tumor in combination with an alkylating agent and/or a radiation therapy. According to one aspect of the present invention, there is provided a compound represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, and a method for preventing and/or treating a tumor in combination with an alkylating agent and/or a radiation therapy.

Abstract: The present invention provides a pharmaceutical composition for treating a patient with an FGFR1 mutant-positive brain tumor, the composition comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a pharmaceutically acceptable salt thereof as an active ingredient; and a therapeutic method using the pharmaceutical composition.

Abstract: There is provided a novel carbonate compound of a nucleoside having a pyrrolopyrimidine skeleton having an excellent antitumor effect, or a pharmaceutically acceptable salt thereof and a method for preventing and/or treating a tumor in combination with an alkylating agent and/or a radiation therapy. According to one aspect of the present invention, there is provided a compound represented by the following general formula (1): or a pharmaceutically acceptable salt thereof, and a method for preventing and/or treating a tumor in combination with an alkylating agent and/or a radiation therapy.

Abstract: This invention provides a method for enhancing antitumor effects of a ribonucleotide reductase (RNR) inhibitory compound. A pharmaceutical composition for treating and/or preventing a tumor used in combination with an immune checkpoint molecule regulator comprising a sulfonamide compound represented by Formula (I) or a salt thereof is also provided.

Abstract: The present invention provides an FTD and TPI-containing oral pharmaceutical composition which can be orally administered and is stable even under high humidity conditions. An oral pharmaceutical composition comprising ?,?,?-trifluorothymidine and 5-chloro-6-(2-iminopyrrolidine-1-yl)methyl-2,4(1H,3H)-pyrimidine dione hydrochloride as an active ingredient; and being substantially free of an additive comprising a metal salt.

Abstract: The problem to be solved by the present disclosure is to provide a novel combination therapy using (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof, the combination therapy exhibiting an excellent antitumor effect on cancer patients with resistance to immune checkpoint inhibitors. The present disclosure provides an antitumor agent comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient, the antitumor agent being administered in combination with pembrolizumab to a cancer patient with resistance to immune checkpoint inhibitors.

Abstract: The present invention provides a novel compound inhibiting EGFR or a salt of the compound. According to one embodiment of the present invention, provided is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The problem to be solved by the present disclosure is to provide a novel combination therapy using (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof, the combination therapy exhibiting an excellent antitumor effect on cancer patients with resistance to immune checkpoint inhibitors. The present disclosure provides an antitumor agent comprising (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a salt thereof as an active ingredient, the antitumor agent being administered in combination with an immune checkpoint inhibitor, except for pembrolizumab, to a cancer patient with resistance to immune checkpoint inhibitors.

Abstract: The present invention provides a compound represented by Formula (I) or a salt thereof; an LSD1 inhibitor that contains the compound or a salt thereof as an active ingredient; a pharmaceutical composition that contains the compound or a salt thereof; and an antitumor agent that contains the compound or a salt thereof as an active ingredient.

Abstract: Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.

Abstract: The present invention provides a novel RET inhibitor comprising, as an active ingredient, a compound or a salt thereof that have not been known for their RET inhibitory activity, and also provides an agent for preventing or treating diseases (e.g., malignant tumors) that can be prevented or treated by RET inhibitory activity. The RET inhibitor comprises, as an active ingredient, a compound represented by Formula (I) below or a salts thereof: wherein A, R1 to R3, X, and n are as defined in the specification.

Abstract: Provided is a novel treatment method for cancer tumors to which endocrine therapy is to be applied, using an FGFR inhibitor (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one or a pharmaceutically acceptable salt thereof. Further provided are a pharmaceutical composition comprising the above compound or a pharmaceutically acceptable salt thereof for use in treatment and/or prevention of tumors to which endocrine therapy is to be applied, the pharmaceutical composition being used in combination with endocrine therapy, as well as its related compound, use, method, and combination.

Abstract: Provided is a novel method for treating cancer using an HSP90 inhibitor which exhibits a markedly superior antitumor effect and has a reduced side effect. An antitumor agent is characterized in that an azabicyclo compound of the following Formula (1) or a salt thereof is administered in combination with other antitumor agent(s).

Abstract: This invention provides a water-in-oil (w/o) emulsion formulation that stably contains 3 types of peptides having 4 linked CTL epitopes. This invention also provides a method for efficiently preparing the w/o emulsion formulation containing 3 types of peptides having 4 linked CTL epitopes. This invention provides a w/o emulsion formulation that stably contains 3 types of peptides having 4 linked CTL epitopes and a method for efficiently preparing such w/o emulsion formulation. In addition, this invention provides an improved method and an apparatus to prepare such emulsion formulation.

Abstract: A method for producing a compound represented by formula (A-1) or a salt thereof, the method comprising reacting (S)-3-((3,5-dimethoxyphenyl)ethynyl)-1-(pyrrolidin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine or a salt thereof with a compound represented by formula (I-1-A). Formula (I-1-A) and formula (A-1) are as described in the specification.

Abstract: A compounds represented by any one of the following formulas (1) to (5) or a salt thereof, or a combination thereof: (1) 1,3-bis((S)-3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)propan-1-one; (2) 1-((S)-3-(4-((3-((S)-3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-3-oxopropyl)amino)-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)prop-2-en-1-one; (3) (S)-3-((1-(1-acryloylpyrrolidin-3-yl)-6-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)amino)propanoic acid; (4) (S)-3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidine-1-carbaldehyde; (5) (S)-1-(3-(4-amino-3-((3,5-dimethoxyphenyl)ethynyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)pyrrolidin-1-yl)-3-hydroxypropan-1-one.