公开(公告)号：EP1092723A2

公开(公告)日：2001-04-18

申请号：EP00308983.6

申请日：2000-10-12

申请人： NIHON MEDI-PHYSICS Co., Ltd.

发明人： Ito, Osamu, c/o Nihon Medi-Physics Co. Ltd. ,  Kanazashi, Nobuhiko, Nihon Medi-Physics Co. Ltd. ,  Morishita, Aki, c/o Nihon Medi-Physics Co. Ltd. ,  Hara, Masamichi c/o Nihon Medi-Physics Co. Ltd. ,  Kanagawa, Masaru, c/o Nihon Medi-Physics Co. Ltd. ,  Watanabe, Yasuko, c/o Nihon Medi-Physics Co. Ltd. ,  Itaya, Yoshitoshi, c/o Nihon Medi-Physics Co. Ltd.

IPC分类号： C07F9/38 ,  C07B59/00 ,  A61K51/00

CPC分类号： A61K51/0497 ,  C07B59/004 ,  C07F9/3865 ,  C07F9/3869 ,  C07F9/3873

摘要： 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 alkyloarboxylic acid or a substituted-alkylcarboxylic acid, an alkysulfonic acid or a substituted-alkysulfonic acid.

摘要翻译： 本发明的一个目的是提供双膦酸衍生物，并且所述双膦酸衍生物用放射性核素标记，所述放射性核素具有快速累积到骨骼和快速排泄尿液的性质。 本发明涉及双膦酸衍生物和所述双膦酸衍生物用以下通式（1）表示的放射性核素标记，RYA（1）其中A是双膦酸或其盐，具有PCP 键; Y是键合部分，例如亚甲基，酰胺基等; R为聚氨基多羧酸，脂肪族羧酸，巯基乙酰基聚氨基酸或其衍生物和式（2）表示的化合物中的任意一种基团，X为卤原子或其同位素或烷基锡; Z是氨基羧酸，烷基羧酸或取代烷基羧酸，烷基磺酸或取代烷基磺酸的化合物中的任一种的基团。