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Biphosphonate

A technology of bisphosphonic acid and bisphosphonate compounds, which can be used in metabolic diseases, cardiovascular system diseases, organic active ingredients, etc., and can solve problems such as no reports

Inactive Publication Date: 2004-11-17
CHONGQING CONQUER PHARML
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Reaction of organic bisphosphonic acid anti-osteoporosis drugs with basic drugs with other drug functions to produce new bisphosphonate compounds with dual drug activity, especially bisphosphonic acid and a thiazolidine di Ketone anti-type II diabetes drugs or bisphosphonate compounds formed by the combination of bisphosphonic acid and a dihydropyridine antihypertensive drug, no reports so far

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] etidronate rosiglitazone

[0064] Put 35g of etidronic acid in a 1-liter beaker, add 700ml of distilled water, stir to dissolve into a solution, heat to 70-80°C and add 70g of rosiglitazone in portions while stirring, and add to form a solution, if there is any insoluble matter , removed by filtration. Cool to room temperature, place in the refrigerator overnight, filter, transfer the solid to a beaker, add 120ml of distilled water, stir well, form a paste, filter, drain the mother liquor, wash 3 times with distilled water (3×50ml), dry at 100-104°C for 80- 85 (83-89%), melting point 122-126°C.

[0065] 1 H NMRδ (ppm) (400MHZ, δ 6 -DMSO) 1.43 3.06(δ, 3H), 3.04-3.30(m, 2H), 3.93(t, 2H), 4.14(t, 2H), 4.83-4.86(m, 1H), 6.68(t, 1H), 6.82(d, 1H), 6.86(d, 2H), 7.14(d, 2H), 7.63(t, 1H), 8.05(d, 1H), 12.02(s, 1H)

Embodiment 2

[0067] risedronate amlodipine

[0068] Amlodipine 10.9g is heated and dissolved in hydrochloric acid (0.1008mol M / L, 270ml). If there is any insoluble matter, filter it out, risedronate monosodium 9.6g is dissolved in distilled water 270ml under stirring, and use sodium hydroxide (0.2M / L ) to adjust the pH to 5.4, pour this solution into the amlodipine hydrochloric acid solution at one time, stir at room temperature for 3 hours to form an emulsified suspension, heat and flow for 20 minutes, cool to room temperature, and place in the refrigerator overnight at 100-104°C for drying. 16 g (80.7%) mp 183-5°C.

[0069] 1 H NMRδ (ppm 400MHZ, δ 6 -DMSO) 1.01(t, 3H), 2.31(s, 3H), 3.02(s, 2H), 3.16(t, 2H), 3.50(s, 3H), 3.66(s, 2H), 4.01(m, 2H ), 4.60(dd, 2H), 5.29(s, 1H), 7.10-7.25(m, 4H), 7.35(d, 1H), 7.88(d, 1H), 8.26(d, 1H) 8.56(s, 1H ), 8.74(s, 1H)

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Abstract

The present invention relates to a kind of biphosphonates, which have double medicinal functions and are compounds formed with biphosphonic acid and medicinal organic base. The present invention also relates to their preparation and application.

Description

Technical field: [0001] The invention relates to a bisphosphonate compound formed from bisphosphonic acid and a medicinal organic base with dual drug effects, their preparation and application. Background technique: [0002] Many drugs are organic acids or organic bases. For the convenience of use or to change the physical and chemical properties such as solubility, these drugs are often converted into medicinal salts, such as the interaction of organic acid drugs with metal ion-containing compounds (usually metal hydroxides) Form sodium salts, potassium salts or calcium salts of pharmaceutical organic acids containing metal ions, and react organic base drugs with different acids to generate pharmaceutical organic base hydrochloride, maleate, citrate or Various sulfonates, etc. These metal ions or acids do not have specific pharmacological effects in the salt molecule, so the pharmacological effects of the original organic acid or organic base will not be changed after the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/675A61P3/10A61P9/12A61P19/10C07F9/38
Inventor 严燊和
Owner CHONGQING CONQUER PHARML
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