Anti-inflammatory products derived from methylene-diphosphonic acid, and process for their preparation
AssigneeSanofi
InventorsJean C. Breliere, Xavier Emonds-Alt, Georges Garcia
Life of this patent
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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).
Claims5
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.
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.
Dependencies are inferred from the claim text.