Abstract: A low-molecular weight compound having an activity of inhibiting the functions of proprotein convertase subtilisin/kexin type 9 (PCSK9), a PCSK9 inhibitor containing a compound represented by formula (I), a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof, as an active component, and a medicament containing the PCSK9 inhibitor as an active component for use in prevention or treatment of one or more symptoms, diseases, or disorders, related to the functions of PCSK9.

Abstract: The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, from the open form.

Abstract: It is known that foods containing a carbohydrate, e.g., starch, in a large amount produce acrylamide upon heating at high temperatures. Some documents state that acrylamide is formed by the Maillard reaction of an amino acid, e.g., asparagine, with a reducing sugar. The purpose of the present invention is to provide a novel compound which is effective in inhibiting such foods from yielding acrylamide when treated at a high temperature. Specifically, the present invention provides a compound represented by General Formula (I).

Abstract: 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.

Abstract: 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.

Abstract: An object of the present invention is to provide enzymes and a DNA encoding the enzymes that are involved in biosynthesis of trehangelin which has the potential to be a therapeutic agent for photosensitivity disorder and cosmetics, and to provide a method for producing trehangelin by utilizing the enzymes and a recombinant microorganism. The present invention is directed to a protein having an amino acid sequence of SEQ ID NO: 3, 5, 7 or 9, or a protein having an amino acid sequence of SEQ ID NO: 3, 5, 7 or 9 in which one to several amino acids are deleted, substituted, added and/or inserted or an amino acid sequence having 60% or more homology with the amino acid sequence of SEQ ID NO: 3, 5, 7 or 9 and having an enzyme activity involved in biosynthesis of trehangelin; and a DNA encoding said protein.

Abstract: This invention provides a novel non-natural pharmaceutical compound having a different mechanism than statin drugs and having a selective inhibitory activity against ACAT2.

Abstract: An object of the present invention is to provide enzymes and a DNA encoding the enzymes that are involved in biosynthesis of trehangelin which has the potential to be a therapeutic agent for photosensitivity disorder and cosmetics, and to provide a method for producing trehangelin by utilizing the enzymes and a recombinant microorganism. The present invention is directed to a protein having an amino acid sequence of SEQ ID NO: 3, 5, 7 or 9, or a protein having an amino acid sequence of SEQ ID NO: 3, 5, 7 or 9 in which one to several amino acids are deleted, substituted, added and/or inserted or an amino acid sequence having 60% or more homology with the amino acid sequence of SEQ ID NO: 3, 5, 7 or 9 and having an enzyme activity involved in biosynthesis of trehangelin; and a DNA encoding said protein.

Abstract: The present invention relates to new macrolide derivatives, in particular new tylosin derivatives of the formula (IIa), a pharmaceutical or veterinary composition comprising the derivatives; a method for preparation thereof; a method for treating and/or preventing bacterial infections in an animal, wherein the method comprises administering the derivatives or the composition; and a use of the derivatives for the manufacture of medicaments for treating and/or preventing bacterial infections in an animal.

Abstract: The present invention provides a Peyer's patch activator containing a polysaccharide obtained from sugar cane as an active ingredient, wherein the polysaccharide contains ?-glucan as a main component and has a peak molecular weight within a range of 720,000 to 1,080,000, with a proportion of glucose in all component sugars being 80% or more, and proportions of nonreducing terminal glucose and ?-1,6-linked glucose being 20 to 30% and 15 to 25%, respectively.

Abstract: An objective of the present invention is to provide novel cyclic depsipeptide derivatives and harmful organism control agents including the same as each other. Specifically, the present invention provides compounds represented by formula (1) or stereoisomers thereof, harmful organism control agents containing them, and a process for producing them.

Abstract: This invention provides a novel non-natural pharmaceutical compound having a different mechanism than statin drugs and having a selective inhibitory activity against ACAT2.

Abstract: The present invention relates to new macrolide derivatives, in particular new tylosin derivatives of the formula (IIa), a pharmaceutical or veterinary composition comprising the derivatives; a method for preparation thereof; a method for treating and/or preventing bacterial infections in an animal, wherein the method comprises administering the derivatives or the composition; and a use of the derivatives for the manufacture of medicaments for treating and/or preventing bacterial infections in an animal.

Abstract: The present invention to provide a novel pyruvate dehydrogenase kinase inhibitors. A pyruvate dehydrogenase kinase inhibitor comprising a compound represented by the general formula (I) as an active ingredient (wherein, ring A represents a 6-membered aromatic hydrocarbon ring optionally substituted with 2-4 substituents, R1 and R4, which are the same or different, represent a hydrogen atom, a hydroxyl group, an optionally substituted C1-6 alkyl group, R2 and R3, which are the same or different, represent a hydrogen atom, a carboxyl group, an optionally substituted C1-6 alkyl group, an optionally substituted C6-10 aryl group, or a group represented by —C (?R9)—R10), a pharmaceutical composition for treatment or prophylaxis of diseases or disorders that pyruvate dehydrogenase kinase relates to its development or aggravation, and a cosmetic composition, and the like.

Abstract: The purpose of the present invention is to provide a therapeutic agent or preventive agent for exacerbation of influenza, specifically to provide a novel pyruvate dehydrogenase kinase 4 (PDK4) inhibitor. The present invention relates to a PDK4 inhibitor, medical composition or cosmetic composition containing as the active ingredient a compound represented by any one of the following general formulas (I) through (III) and a pharmaceutically acceptable ester derivative thereof, or a pharmaceutically acceptable salt of the same.

Abstract: A compound effective in prevention and treatment of arteriosclerosis with a mechanism different from that of statin drugs has the following formula or a pharmaceutically acceptable salt, solvate, or hydrate thereof: wherein R1 is an aliphatic, alicyclic, or aromatic acyloxy group, or a group of the formula —O—CH(R7)—R8 where R7 is a lower alkoxy group and R8 is an aryl group, and R2 is carboxyl, a lower alkoxycarbonyl group, or an arylmethylcarbamoyl group, or a —CH2-acyloxy group and R3 is an aliphatic, alicyclic or aromatic acyloxy group, provided that at least one of R4 and R3 is a group other than acetoxy, or R2 and R3 taken together form a group of the formula —O—CH(R5)—O— where R5 is an aryl group.

Abstract: The present invention provides a Peyer's patch activator containing a polysaccharide obtained from sugar cane as an active ingredient, wherein the polysaccharide contains ?-glucan as a main component and has a peak molecular weight within a range of 720,000 to 1,080,000, with a proportion of glucose in all component sugars being 80% or more, and proportions of nonreducing terminal glucose and ?-1,6-linked glucose being 20 to 30% and 15 to 25%, respectively.

Abstract: An objective of the present invention is to provide novel cyclic depsipeptide derivatives and harmful organism control agents including the same as each other. Specifically, the present invention provides compounds represented by formula (1) or stereoisomers thereof, harmful organism control agents containing them, and a process for producing them.

Abstract: The present invention addresses the problem of providing an anti-trypanosomal drug having a novel skeleton, in order to solve issues that occur with conventional technologies. The present invention is based on the discovery of a microbe that produces an anti-trypanosomal drug having a novel skeleton. Specifically, this invention provides: a compound indicated by formula (I) having a trypanosomal inhibitory activity; an analog thereof; a production method therefor; and a Lechevalieria sp. K10-0216 strain that produces said compound.

Abstract: The present invention relates to new macrolide derivatives, in particular new tylosin derivatives of the formula (I); a pharmaceutical or veterinary composition comprising the derivatives; a method for preparation thereof; a method for treating and/or preventing bacterial infections in an animal, wherein the method comprises administering the derivatives or the composition; and a use of the derivatives for the manufacture of medicaments for treating and/or preventing bacterial infections in an animal.