Abstract: A process for producing a diazabicyclooctane derivative represented by Formula (IV) and intermediates thereof by carrying out the following steps: wherein P is an NH protecting group capable of being removed with acid; R1 is 2,5-dioxopyrrolidin-1-yl, 1,3-dioxo-3a,4,7,7a-tetrahydro-1H-isoindol-2(3H)-yl, 1,3-dioxohexahydro-1H-isoindol-2(3H)-yl, or 3,5-dioxo-4-azatricyclo[5.2.1.02.6]dec-8-en-4-yl; R2 is hydrogen, ClCO— or Cl3COCO—; R3 is C1-6 alkyl or heterocyclyl, or forms a 3- to 7-membered heterocyclic ring together with the —O—NH— to which it is attached; and OBn is benzyloxy.

Abstract: A method for producing a compound represented by formula (I) comprises the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of trifluoroacetic acid as an acylating agent to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B), as follows

Abstract: A dysphagia improving composition characterized in that a substance having an inhibitory action on an angiotensin converting enzyme, which is a degrading enzyme of substance P, is administered locally in a dosage not influencing blood pressure, and a pharmaceutical for improving dysphagia containing the composition.

Abstract: According to the present invention, it is possible to efficiently remove 13-dihydroepi-daunorubicin and 4?-epi-feudomycin, which are typical impurities possibly contained in 4?-epi-daunorubicin as a starting material, by using an organic acid salt of 4?-epi-daunorubicin or a hydrate or solvate thereof as a novel production intermediate, thus making it possible to produce high-purity epirubicin.

Abstract: Provided is a nitrogen-containing heterocyclic derivative having a 2-imino group, which is represented by the following Formula (I). [in the formula, Ar represents a phenyl group which may be substituted, a 5- to 6-membered heterocycle which may be substituted, or a 4- to 10-membered heterocycloalkyl group, A represents a heterocycle having a 5- to 10-membered unsaturated bond including one or more nitrogen atoms, and has an imino group substituted with an R group at a position adjacent to the nitrogen atom present on the cycle, Y represents a hydrogen atom, a halogen atom, a hydroxyl group, a C1 to C6 alkyl group which may be substituted with a halogen atom, a C1 to C6 alkyloxy group which may be substituted with a halogen atom, a cyano group, or a nitro group, and R represents any one of groups represented by the following Formulae (a) to (e), (y) or (z).

Abstract: Provided is a compound represented by formula (1a) or a pharmacologically acceptable salt thereof, which can be used as a phosphodiesterase (PDE) inhibitor. R1 to R6 in the formula each independently represent an alkyl group or the like.

Abstract: To supply a derivative having a 2-acyliminopyridine structure and being represented by the following formula (I) in an amount required as a pest control agent stably and at a low cost, provided is a method comprising the steps of: acylating an amino group at position 2 of a compound represented by formula (A) by use of an acylating agent, to thereby produce a compound represented by formula (B); and further alkylating a nitrogen atom at position 1 of the compound represented by formula (B): [where Ar represents a phenyl group or a 5- to 6-membered heterocycle, R1 represents a C1-6 alkyl group, and Y represents a hydrogen atom; a halogen atom; a hydroxyl group; a C1-6 alkyl group which may be substituted with a halogen atom; a C1-6 alkyloxy group which may be substituted with a halogen atom; a cyano group; a formyl group; or a nitro group].

Abstract: It has been found that a main effect (immunosuppressive activity) of an S1P1 receptor agonist correlates with the selectivity for cells expressing a combination of an S1P1 receptor with G?i2 or G?i3, and that an adverse effect (cardiotoxicity) of an S1P1 receptor agonist correlates with the selectivity for cells expressing a combination of an S1P1 receptor with G?i1.

Abstract: Provided is a compound represented by formula (1a) or a pharmacologically acceptable salt thereof, which can be used as a phosphodiesterase (PDE) inhibitor. R1 to R6 in the formula each independently represent an alkyl group or the like.

Abstract: A compound of formula (Ie?): wherein Ar?, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.

Abstract: A process for producing crystals of a compound represented by the following formula (l): by crystallizing the compound from an aqueous solution containing the compound and an inorganic salt, such as sodium chloride.

Abstract: A process for producing a compound represented by a Formula (III), including reacting a compound of the following formula with a compound selected from the group consisting of 1-hydroxypyrrolidine-2,5-dione, 2-hydroxy-3a,4,7,7a-tetrahydro-1H-isoindol-1,3(2H)-dione, 2-hydroxyhexahydro-1H-isoindol-1,3(2H)-dione and 4-hydroxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione, carrying out a carbonylation to obtain a compound of the following formula removing the NH protecting group P and treating the resultant compound with a base to produce a compound represented by the following formula wherein OBn is benzyloxy and R2 is hydrogen, ClCO— or Cl3COCO—.

Abstract: The genomic DNA of Streptoverticillium sp. 3-7, which produces UK-2, was analyzed to identify a region expected to be a UK-2 biosynthetic gene cluster. Moreover, by colony hybridization, DNAs in the region were successfully isolated. Further, the DNAs were used to prepare a strain in which the genes present in the region were disrupted. The strain was found not to produce UK-2. It was verified that the genomic region was the UK-2 biosynthetic gene cluster. Furthermore, Streptoverticillium sp. 3-7 was transformed by introduction of a vector in which the isolated UK-2 biosynthetic gene cluster was inserted. It was also found out that the UK-2 productivity by the transformant was improved about 10 to 60 times or more in comparison with that of the parental strain. Moreover, it was revealed that 2 copies of the UK-2 biosynthetic gene cluster were present per cell in these transformants, respectively.

Abstract: A dysphagia improving composition characterized in that a substance having an inhibitory action on an angiotensin converting enzyme, which is a degrading enzyme of substance P, is administered locally in a dosage not influencing blood pressure, and a pharmaceutical for improving dysphagia containing the composition.

Abstract: It has been found that adding carbon dioxide or the like to a solution containing arbekacin free base makes it possible to produce arbekacin derivatives including arbekacin carbonate and carbamic acid of arbekacin. Moreover, it has been found that the arbekacin derivatives have a high stability, and that the use thereof enables efficient productions of highly-pure arbekacin free base and pharmaceutically acceptable salt thereof.

Abstract: A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.

Abstract: A crystal form of 2-(3,5-dimethyl-1H-pyrazol-1-yl)-5-methylphenol which is stable and has high purity for preservation, industrial manufacturing, and circulation, and process for providing the same by using a boron compound.

Abstract: A compound of formula (Ie?): wherein Ar?, R1, R4e and Y are as defined herein and a method of controlling pests using the compound.

Abstract: A diazabicyclooctane compound, which is a beta-lactame inhibitor, represented by the following formula (I): wherein A represents Ra(Rb)N— or RcO—; B represents NH or NC1-6 alkyl; C represents benzyl, H or SO3M, wherein M represents H, an inorganic or an organic cation; Ra and Rb represent H, C1-6 alkyl or acyl; Rc represents C1-6 alkyl or a heterocyclyl; A is unsubstituted or substituted with 0 to 4 substituents Fn1, wherein Fn1 represents C1-6 alkyl, O?, or Rg-(CH2)0-3—, wherein Rg represents a heterocyclyl, phenyl, heteroaryl, acyl, RdO2S—, Re(Rf)N—, Re(Rf)NCO—, ReO—, ReOCO— or a protective group, wherein Rd represents C1-6 alkyl or MO—; Re and Rf represent H or C1-6 alkyl, and a heterocycle having at least one nitrogen atom may be formed between Ra and Rb, between Rc and B, or between Re and Rf.

Abstract: The present invention provides a stable aqueous adalimumab formulation by incorporating a histidine buffer solution and a phosphate buffer solution in combination. The incorporation of the histidine buffer solution and the phosphate buffer solution makes it possible to improve the stability of adalimumab.