Abstract: The present invention relates to a pharmaceutical composition comprising a liquid composition containing p-boronophenylalanine, in which the liquid composition is accommodated in a packaging material and satisfies the following Condition I or Condition II: Condition I: the liquid composition comprises substantially no antioxidant and a concentration of dissolved oxygen in the liquid composition is 3.5 ppm or less; Condition II: the liquid composition comprises an antioxidant and a concentration of dissolved oxygen in the liquid composition is 3.0 ppm or less.

Abstract: To provide a novel boron-containing compound. A compound represented by the following formula: wherein black circle represents B, white circles represent B—H; —R1 represents —(CH2)n-X1—R3 (n represents an integer of 0 to 6; X1 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; R3 represents C6-C20 alkyl, hydroxy C6-C20 alkyl, amino C6-C20 alkyl, azido C6-C20 alkyl, hydroxycarbonyl C6-C20 alkyl, or the like), or a group having a repeating sequence of —(CH2)2—O— 3 times or more and 10 times or less and having a methyl group or an ethyl group at the end on the oxygen atom side; and —R2 is —(CH2)m-X2—R4 (m represents an integer from 0 to 8; X2 represents O, S, NH, S—S, O—CO, NHCO or SCO, or does not exist; and R4 represents a tumor recognition moiety), or does not exist are prepared and used.

Abstract: The present invention involves preparing compounds represented by the following formula: from a compound of the following formula: In these formulae: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N?N—NR7R8, OSO2R9, N R10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C?N, in which NR40R50 are together.

Abstract: The present invention involves preparing compounds represented by the formula. (In the formula: R1 represents a Br group, an iodine group, a Cl group, an NO2 group, or an NH2 group; R2 represents a halogen group, an NO2 group, an NH2 group, Sn(R6)3, N?N—NR7R8, OSO2R9, NR10R11, phenyliodonium, a heterocyclic group iodine, boric acid, or a borate ester; R30 represents a protective group PG1; R40 or R50 represent hydrogen, a protective group PG2, or C6H5(C6H5)C?N, wherein NR40R50 are together.

Abstract: 18F-labeled 4-boronophenylalanine (BPA) can be produced by preparing and further processing a precursor of 18F-labeled BPA represented by the following formula: in which R1 represents a bromo group, an iodo group, a fluoro group, a diazaborinane derivative, BX3? or BX3?M+ (wherein X represents a halogen atom; and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation).

Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.

Abstract: Provided are: a novel chiral 4-boronophenylalanine (BPA) derivative; a method for producing the derivative; and a method for producing 18F-2-fluoro-4-borono-L-phenylalanine (18F-labeled BPA; 18F-BPA) using the derivative. A compound represented by formula (1) is prepared. In the formula, R represents BR3R4, BX3? or BX3?M+ (wherein X represents a halogen atom, and M+ represents a monovalent monoatomic cation, a polyatomic cation or a complex cation); R1 represents a hydrogen atom or a protecting group PG1; R2 represents a hydrogen atom or a protecting group PG2; R3 and R4 independently represent OH, or R3, R4 and B together form a ring that serves as a protecting group; and Y represents a halogen atom, NO2, NH2, Sn(R6)3, N?N—NR7R8, OSO2R9, NR10R11, a substituted or unsubstituted phenyliodo group or a substituted or unsubstituted heterocyclic iodo group. The compound is reacted with a fluorination reagent to prepare 18F-labeled BPA.

Abstract: The purpose of the present invention is to provide a novel method for producing cereulide and a derivative thereof; an intermediate for cereulide; and a novel cereulide derivative. A novel didepsipeptide, a novel tetradepsipeptide, a novel octadepsipeptide and a novel dodecadepsipeptide are prepared. A linear precursor of cereulide or a derivative thereof, which is composed of any one of the novel depsipeptides, is cyclized by forming an intramolecular amide bond.

Abstract: It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved.

Abstract: It is an object of the present invention to provide a substance usable as an anticancer agent or DDS, which has intracellular stability, which is capable of evading side effects from functional disorder with respect to normal cells, or which has instantaneous effect. The inventors developed a novel chimeric peptide targeting cancer cells which overexpress EGFR or the like using a binding peptide such as a peptide sequence binding to EGFR, and a lytic peptide sequence, thereby solving such an object. Particularly, by using a chimeric peptide including an EGF receptor-binding peptide or the like and a cytotoxic peptide, this object was solved.

Abstract: The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a pharmaceutically acceptable salt thereof is prepared, said boron compound being represented by general formula (I) [wherein l is an integer of 1 to 6; m is 0, 1, or 2; and n is 0, 1 or 2].

Abstract: The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a pharmaceutically acceptable salt thereof is prepared, said boron compound being represented by general formula (I) [wherein l is an integer of 1 to 6; m is 0, 1, or 2; and n is 0, 1 or 2].

Abstract: Disclosed is the method for producing an optically active BSH amino acid, which comprises a step of reacting an optically active a-amino acid derivative having a halogen in a side chain with a cyanoethyl BSH compound represented by formula (1). An optically active BSH amino acid obtained by the method is also disclosed.

Abstract: Disclosed is a method for producing a BSH derivative, which comprises a step of addition-reacting BSH with an ?,?-unsaturated nitrile compound in the presence of a base. Various BSH derivatives obtained by the method are also disclosed.

Abstract: Disclosed is the method for producing an optically active BSH amino acid, which comprises a step of reacting an optically active a-amino acid derivative having a halogen in a side chain with a cyanoethyl BSH compound represented by formula (1). An optically active BSH amino acid obtained by the method is also disclosed.