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Boehringer Ingelheim
Covington
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Generated: April 24, 2018

DrugPatentWatch Database Preview

Claims for Patent: 4,876,248

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Summary for Patent: 4,876,248
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## group, a substituted or unsubstituted phenyl radical, a ##STR3## group, 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 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)
Application Number:07/165,080
Patent Claims: 1. 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 a phenyl group which is 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, a COOH group;

R.sub.3 is hydrogen or a hydroxyl group; and

n is an integer between 0 and 10, with the proviso that n cannot be 0 if R.sub.3 is OH, and with the further proviso that:

R.sub.2 is different from the group having the formula ##STR57## wherein Q is a halogen atom, a nitro group or a trifluoromethyl group and T is methyl, ethyl or butyl when R.sub.1 is a methyl or ethyl group, R.sub.3 is hydrogen and n=0;

and the salts of said compounds with inorganic or organic bases when R.sub.1 =H.

2. A methylene-disphosphonic acid compound according to claim 1, having the formula (I) in which n=0 and ##STR58## R.sub.3 =H, and the salts of said compounds with inorganic or organic bases when R.sub.1 =H.

3. A methylene-disphosphonic acid compound according to claim 1, having the formula: ##STR59## or one of its salts with inorganic or organic bases.

4. Pharmaceutical compositions which contain in association with a pharmaceutically acceptable carrier an effective amount of a compound of formula (I): ##STR60## 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 a phenyl group which is 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, a COOH group;

R.sub.3 is hydrogen or a hydroxyl group; and

n is an integer between 0 and 10, with the proviso that n cannot be 0 if R.sub.3 is OH;

or of one of its salts with inorganic or organic bases when R.sub.1 =H.

5. A pharmaceutical composition according to claim 4, which contains from 10 to 500 mg of the compound of formula I as an active ingredient.

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Serving hundreds of leading biopharmaceutical companies globally:

Daiichi Sankyo
Baxter
US Department of Justice
Covington
Farmers Insurance
Express Scripts
McKinsey
Merck
US Army

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