US 6,607,710 B1 · Bisphosphonic acid derivative and compound thereof labeled with radioactive nuclide

Abstract

An object of the present invention is to provide a bisphosphonic acid derivative and said bisphosphonic acid derivative being labeled with a radioactive nuclide, which has properties of rapid accumulation to the bone and rapid urinary excretion. The present invention relates to a bisphosphonic acid derivative and said bisphosphonic acid derivative being labeled with a radioactive nuclide, which is represented by the following general formula (1), R—Y—A (1) wherein A is a bisphosphonic acid or a salt thereof, having P—C—P bond; Y is a bonding portion such as a methylene, an amido etc.; R is a group of any one of a polyaminopolycarboxylic acid, an aliphatic carboxylic acid, a mercaptoacetylpolyamino acid or its derivatives and a compound represented by the formula (2), X is a halogen atom or an isotope thereof or an alkyl tin; Z is a group of any one of compounds of an aminocarboxylic acid, an alkylcarboxylic acid or a substituted-alkylcarboxylic acid, an alkylsulfonic acid or a substituted-alkylsulfonic acid.

Claims24

Dependent claims

A bisphosphonic acid derivative or salt thereof represented by the following formula (1):

R—Y—A (1)
wherein A is a bisphosphonic acid or salt thereof, having a P—C—P bond;
Y is a bonding portion selected from the group consisting of —(CH2)—, —[(CH2)m(NHCO)r(CH2)n]q—, —[(CH2)m(CONH)r(CH2)n]q— and —(CH2)o—S—(CH2)p—;
k, l, m, n, o, p, q and r each represents independently an integer, and k=0 or 1, l=1 to 6, m=0 to 6, n=1 to 6, o=0 to 6, p=0 to 6, q=1 to 6, and r=1 to 6;
R is a group of any one of compounds selected from the group consisting of a polyaminopolycarboxylic acid, an aliphatic carboxylic acid, a mercaptoacetylpolyamino acid and a compound represented by the following formula (2),
and in the formula (2), X is a halogen atom or its isotope, or an alkyl tin;
Z is a group of any one of compounds selected from the group consisting of an aminocarboxylic acid, an alkylcarboxylic acid, a substituted-alkylcarboxylic acid, an alkylsulfonic acid and a substituted-alkylsulfonic acid.

4 more elements

Dependencies are inferred from the claim text.

Bisphosphonic acid derivative and compound thereof labeled with radioactive nuclide

Life of this patent

Bisphosphonic acid derivative and compound thereof labeled with radioactive nuclide

Life of this patent

Abstract

Claims24