Aromatic nitrogen-contg. bis-phosphonic acid derivs., process for preparing same and use thereof

Abstract

A nitrogen-containing aromatic biphosphonate derivative used for preventing and treating osteoporosis, hypercalcemia, Paget's disease, etc is prepared from aromatic amine, triethyl orthoformate and dimethyl phosphonite in mole ratio of 1:(1-1.5):(3-5) through thermal reaction at 100-160 deg.C for 1-3 hr.

Description

technical field

[0001] The present invention relates to a novel bisphosphonic acid derivative developed for the purpose of preventing and treating osteoporosis, hypercalcemia, Paget's disease and other bone and calcium metabolism diseases. Background technique

[0002] Human beings are about to enter an unprecedented aging society, and in my country, the population over 60 years old will reach 11% by 2000. As one of the common diseases of the elderly, the increase of bone and calcium metabolism diseases such as osteoporosis has become a huge social problem. The salient feature of this type of disease is that bone resorption exceeds bone formation due to pathological or physiological reasons, resulting in decreased bone mass per unit volume, weakened bone strength, and elevated blood calcium content. Since alendronic acid and other nitrogen-containing bisphosphonates have been widely used clinically in bone and calcium metabolism diseases such as osteoporosis, nitrogen-contai...