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Details for Patent: 4,746,654

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Details for Patent: 4,746,654

Title: Anti-inflammatory products derived from methylene-diphosphonic acid, and process for their preparation
Abstract:The present invention relates to products of the formula ##STR1## where R.sub.1 is H or alkyl, n is an integer from 0 to 10, and R.sub.2 is chosen from amongst H, unsubstituted or substituted alkyl radicals, a ##STR2## a substituted or unsubstituted phenyl radical, a ##STR3## where X is oxygen or sulfur, or a heterocyclic radical with 5 or 6 members, which may or may not be fused to a benzene ring and R.sub.3 is H or OH. The present invention also relates to a process for the preparation of the products of the formula (I), and to the drugs, having in particular an anti-inflammatory effect, containing a product of the formula (I).
Inventor(s): Breliere; Jean C. (Montpellier, FR), Emonds-Alt; Xavier (Montpellier, FR), Garcia; Georges (Saint-Gely-du-Fesc, FR)
Assignee: Sanofi (Paris, FR)
Filing Date:Apr 24, 1986
Application Number:06/858,573
Claims:1. A method for treating inflamation which comprises administering to an animal in need of such treatment an anti-inflammatory effective amount of a methylene-diphosphonic acid compound having the formula ##STR56## in which: R.sub.1 is hydrogen or a straight or branched lower alkyl group having from 1 to 4 carbon atoms,

R.sub.2 is:


an alkyl group having from 1 to 16 carbon atoms which is unsubstituted or substituted by a phenyl group, a hydroxyl group, a thiol group, one or more halogen atoms, ##STR57## where Z.sub.1 and Z.sub.2, considered independently of one another, are hydrogen or a lower alkyl group,

a phenyl group which is unsubstituted or substituted one or more times by halogen, a nitro group, a lower alkyl group, a lower alkoxy group, trifluoromethyl, an NH.sub.2 group, or a COOH group, or ##STR58## where X is oxygen or sulfur and Z.sub.1 and Z.sub.2 are as defined above, R.sub.3 is hydrogen or a hydroxyl group, and

n is an integer between 0 and 10, except that n cannot be 0 if R.sub.3 is OH, or a salt of such compound with an organic or inorganic bases when R.sub.1 =H.

2. The method of claim 1 wherein the anti-inflammatory effective amount contains from 10 to 500 mg and is administered orally, endorectally, or parenterally.
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