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

A technology of bisphosphonic acid and derivatives, applied in the field of new bisphosphonic acid derivatives, can solve problems such as not yet found

Inactive Publication Date: 2003-08-13
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, a class of drugs with significant effects on the prevention and treatment of bone and calcium metabolism diseases such as osteoporosis, hypercalcemia, and Paget's disease has not been found so far.

Method used

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Examples

Experimental program
Comparison scheme
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Embodiment

[0020] Example: 1. Tetramethyl (4-methylanilino) methylene bisphosphonate (B1)

[0021] 2.14g (20mmol) of p-methylaniline, 8.8g (80mmol) of dimethyl phosphinate, and 2.4g (24mmol) of triethyl orthoformate were successively added into a 100ml reaction flask. React at 150°C for 1.5h, and ethanol is continuously distilled off during the reaction. Excess reactants were sucked dry under reduced pressure, solid precipitated after cooling, filtered, washed repeatedly with ether, and recrystallized from ethyl acetate-ether to obtain 3.5 g of white crystals, mp 135-137°C, yield 51.9%. Elemental Analysis C 12 h 21 P 2 o 6 N, theoretical value (%): C42.73, H6.23, N4.15; measured value (%): C43.16, H6.56, N4.03. 1 H-NMR (DMSO) δppm: 1.17-1.19 (m, 1H, NH3 ), 3.58-3.69 (m, 12H, -OCH 3 ), 4.52-4.71 (m, 1H, -CH<), 6.75 (d, 2H, Ar-H), 6.88 (d, 2H, Ar-H). 2. (4-methylanilino) methylene bisphosphonic acid (B2)

[0022] 3.37 g (10 mmol) of compound B1 was dissolved in 20 ml of concentrated ...

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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...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/662A61P3/12A61P19/10C07F9/38
Inventor 谢雨礼谢毓元陈文致严雪铭
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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